[go: up one dir, main page]

NO20015797L - Indazolforbindelser og farmasöytiske forbindelser for inhibering av proteinkinaser, og fremgangsmåter til anvendelsederav - Google Patents

Indazolforbindelser og farmasöytiske forbindelser for inhibering av proteinkinaser, og fremgangsmåter til anvendelsederav

Info

Publication number
NO20015797L
NO20015797L NO20015797A NO20015797A NO20015797L NO 20015797 L NO20015797 L NO 20015797L NO 20015797 A NO20015797 A NO 20015797A NO 20015797 A NO20015797 A NO 20015797A NO 20015797 L NO20015797 L NO 20015797L
Authority
NO
Norway
Prior art keywords
compounds
inhibition
methods
protein kinases
indazole
Prior art date
Application number
NO20015797A
Other languages
English (en)
Other versions
NO322507B1 (no
NO20015797D0 (no
Inventor
Robert Steven Kania
Steven Lee Bender
Allen J Borchardt
John F Braganza
Stephan James Cripps
Ye Hua
Michael David Johnson
Jr Theodore Otto Johnson
Hiep The Luu
Cynthia Louise Palmer
Siegfried Heinz Reich
Anna Maria Tempczyk-Russell
Min Teng
Christine Thomas
Michael David Varney
Michael Brennan Wallace
Michael Raymond Collins
Original Assignee
Agouron Pharma
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22498654&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NO20015797(L) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Agouron Pharma filed Critical Agouron Pharma
Publication of NO20015797D0 publication Critical patent/NO20015797D0/no
Publication of NO20015797L publication Critical patent/NO20015797L/no
Publication of NO322507B1 publication Critical patent/NO322507B1/no

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
NO20015797A 1999-07-02 2001-11-28 Indazolforbindelser og farmasøytisk materiale derav for inhibering av proteinkinaser, og bruk derav som et medikament. NO322507B1 (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US14213099P 1999-07-02 1999-07-02
PCT/US2000/018263 WO2001002369A2 (en) 1999-07-02 2000-06-30 Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use

Publications (3)

Publication Number Publication Date
NO20015797D0 NO20015797D0 (no) 2001-11-28
NO20015797L true NO20015797L (no) 2002-03-01
NO322507B1 NO322507B1 (no) 2006-10-16

Family

ID=22498654

Family Applications (3)

Application Number Title Priority Date Filing Date
NO20015797A NO322507B1 (no) 1999-07-02 2001-11-28 Indazolforbindelser og farmasøytisk materiale derav for inhibering av proteinkinaser, og bruk derav som et medikament.
NO20060596A NO20060596L (no) 1999-07-02 2006-02-06 Indazolforbindelser og farmasoytiske forbindelser for inhibering av proteingkinaser, og fremgangsmater til anvendelse derav
NO2013004C NO2013004I2 (no) 1999-07-02 2013-02-26 Axitinib, valgfritt i form av et farmasøytisk aksentabelt salt

Family Applications After (2)

Application Number Title Priority Date Filing Date
NO20060596A NO20060596L (no) 1999-07-02 2006-02-06 Indazolforbindelser og farmasoytiske forbindelser for inhibering av proteingkinaser, og fremgangsmater til anvendelse derav
NO2013004C NO2013004I2 (no) 1999-07-02 2013-02-26 Axitinib, valgfritt i form av et farmasøytisk aksentabelt salt

Country Status (51)

Country Link
EP (2) EP1218348B1 (no)
JP (2) JP3878849B2 (no)
KR (1) KR100529639B1 (no)
CN (2) CN1137884C (no)
AP (1) AP1486A (no)
AR (2) AR035554A1 (no)
AT (1) ATE376543T1 (no)
AU (1) AU777701B2 (no)
BE (1) BE2013C015I2 (no)
BG (1) BG66070B1 (no)
BR (1) BRPI0012352B8 (no)
CA (1) CA2383630C (no)
CO (1) CO5190686A1 (no)
CR (2) CR6517A (no)
CY (3) CY1107147T1 (no)
CZ (1) CZ301667B6 (no)
DE (2) DE60036879T2 (no)
DK (2) DK1218348T3 (no)
DZ (1) DZ3191A1 (no)
EA (1) EA004460B1 (no)
EE (1) EE05585B1 (no)
ES (2) ES2293906T3 (no)
FR (1) FR13C0010I2 (no)
GE (1) GEP20063885B (no)
GT (1) GT200000107A (no)
HR (1) HRP20020109B1 (no)
HU (1) HU228502B1 (no)
IL (1) IL146710A0 (no)
IS (1) IS2791B (no)
JO (1) JO2319B1 (no)
LU (1) LU92154I2 (no)
MA (1) MA26803A1 (no)
ME (1) ME00385B (no)
MX (1) MXPA01012795A (no)
MY (2) MY139999A (no)
NO (3) NO322507B1 (no)
NZ (1) NZ516676A (no)
OA (1) OA11980A (no)
PA (1) PA8498001A1 (no)
PE (1) PE20010306A1 (no)
PL (1) PL212108B1 (no)
PT (2) PT1218348E (no)
RS (1) RS50339B (no)
SI (2) SI1218348T1 (no)
SK (1) SK286936B6 (no)
SV (1) SV2002000121A (no)
TN (1) TNSN00146A1 (no)
UA (1) UA66933C2 (no)
UY (1) UY26231A1 (no)
WO (1) WO2001002369A2 (no)
ZA (1) ZA200110061B (no)

Families Citing this family (361)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ303692B6 (cs) 1999-02-10 2013-03-13 Astrazeneca Ab Chinazolinové deriváty jako inhibitory angiogeneze
PE20010306A1 (es) * 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
SK287882B6 (sk) 1999-12-24 2012-02-03 Aventis Pharma Limited Azaindoles derivatives, pharmaceutical composition containing thereof and their use
CA2399274A1 (en) 2000-02-07 2001-08-09 Mark E. Salvati 3-aminopyrazole inhibitors of cyclin dependent kinases
US20040087798A1 (en) * 2000-03-14 2004-05-06 Akira Yamada Novel amide compounds
ES2236217T3 (es) 2000-04-25 2005-07-16 Bristol-Myers Squibb Company Uso de 5.tio.,sulfinil- y sulfonilpirazolo 3,4-b)-piridinas como inhibidores de la quinasa dependiente de la ciclina.
BR0113057A (pt) 2000-08-09 2003-07-08 Astrazeneca Ab Composto, processo para a preparação de um composto, composição farmacêutica, uso de um composto, e, método para produzir um efeito antiangiogênico e/ou efeito de redução da permeabilidade vascular em um animal de sangue quente em necessidade de tal tratamento
US7371765B2 (en) 2000-08-09 2008-05-13 Astrazeneca Ab Quinoline derivatives having VEGF inhibiting activity
WO2002018383A2 (en) 2000-09-01 2002-03-07 Chiron Corporation Aza heterocyclic derivatives and their therapeutic use
AP1666A (en) 2000-09-11 2006-09-29 Chiron Corp Quinolinone derivatives as tyrosine kinase inhibitors.
AU9598601A (en) 2000-10-20 2002-04-29 Eisai Co Ltd Nitrogenous aromatic ring compounds
TWI243164B (en) 2001-02-13 2005-11-11 Aventis Pharma Gmbh Acylated indanyl amines and their use as pharmaceuticals
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
US7642278B2 (en) 2001-07-03 2010-01-05 Novartis Vaccines And Diagnostics, Inc. Indazole benzimidazole compounds
US7064215B2 (en) 2001-07-03 2006-06-20 Chiron Corporation Indazole benzimidazole compounds
WO2003024969A1 (en) 2001-09-14 2003-03-27 Merck & Co., Inc. Tyrosine kinase inhibitors
FR2831536A1 (fr) * 2001-10-26 2003-05-02 Aventis Pharma Sa Nouveaux derives de benzimidazoles, leur procede de preparation, leur application a titre de medicament, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de kdr
US6897208B2 (en) * 2001-10-26 2005-05-24 Aventis Pharmaceuticals Inc. Benzimidazoles
JP5039268B2 (ja) * 2001-10-26 2012-10-03 アベンティス・ファーマスーティカルズ・インコーポレイテツド ベンゾイミダゾールおよび類縁体および蛋白キナーゼ阻害剤としてのその使用
FR2831537B1 (fr) * 2001-10-26 2008-02-29 Aventis Pharma Sa Nouveaux derives de benzimidazoles, leur procede de preparation, leur application a titre de medicament, compositions pharmaceutiques et nouvelle utilisation
PL371486A1 (en) 2002-02-01 2005-06-13 Astrazeneca Ab Quinazoline compounds
US7166293B2 (en) 2002-03-29 2007-01-23 Carlsbad Technology, Inc. Angiogenesis inhibitors
US20050119278A1 (en) * 2002-05-16 2005-06-02 Che-Ming Teng Anti-angiogenesis methods
CA2495216A1 (en) 2002-08-12 2004-02-19 Sugen, Inc. 3-pyrrolyl-pyridopyrazoles and 3-pyrrolyl-indazoles as novel kinase inhibitors
AU2003288899B2 (en) 2002-08-23 2009-09-03 Novartis Vaccines And Diagnostics, Inc. Benzimidazole quinolinones and uses thereof
AU2003289287A1 (en) * 2002-12-03 2004-06-23 Kyowa Hakko Kogyo Co., Ltd. Jnk inhibitor
DK1585743T3 (da) * 2002-12-19 2007-09-17 Pfizer 2-(H-indazol-6-ylamino)-benzamid forbindelser som protein kinase inhibitorer, nyttige til behandling opthalmiske sygdomme
US7192976B2 (en) 2002-12-21 2007-03-20 Angion Biomedica Corporation Small molecule modulators of hepatocyte growth factor (scatter factor) activity
US7135575B2 (en) 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
PL214032B1 (pl) 2003-03-03 2013-06-28 Array Biopharma Zwiazki bedace inhibitorami kinazy p38, kompozycja farmaceutyczna je zawierajaca oraz ich zastosowanie do wytwarzania leku do leczenia stanu, w którym posredniczy kinaza p38
JP2006522087A (ja) * 2003-04-03 2006-09-28 ファイザー・インク Ａｇ０１３７３６を含んでなる剤形
WO2004092217A1 (en) * 2003-04-17 2004-10-28 Pfizer Inc. Crystal structure of vegfrkd: ligand complexes and methods of use thereof
FR2854159B1 (fr) * 2003-04-25 2008-01-11 Aventis Pharma Sa Nouveaux derives de l'indole, leur preparation a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de kdr
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
WO2005012256A1 (en) 2003-07-22 2005-02-10 Astex Therapeutics Limited 3, 4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators
JP4836788B2 (ja) * 2003-07-23 2011-12-14 エグゼリクシス， インコーポレイテッド 未分化リンパ腫キナーゼ変調因子及びその使用法
ES2384568T3 (es) 2003-07-30 2012-07-09 Kyowa Hakko Kirin Co., Ltd. Derivados de indazol
EP1650194A4 (en) * 2003-07-30 2008-10-01 Kyowa Hakko Kogyo Kk INHIBITOR OF PROTEIN KINASE
JP2007504236A (ja) * 2003-09-04 2007-03-01 メルク　エンド　カムパニー　インコーポレーテッド 高眼圧症を治療するための眼用組成物
US20050164300A1 (en) * 2003-09-15 2005-07-28 Plexxikon, Inc. Molecular scaffolds for kinase ligand development
US20050182061A1 (en) * 2003-10-02 2005-08-18 Jeremy Green Phthalimide compounds useful as protein kinase inhibitors
EP1692085A4 (en) 2003-11-07 2010-10-13 Novartis Vaccines & Diagnostic INHIBITION OF FGFR3 AND TREATMENT OF MULTIPLE MYELOMA
JP4303726B2 (ja) 2003-11-11 2009-07-29 エーザイ・アール・アンド・ディー・マネジメント株式会社 ウレア誘導体およびその製造方法
WO2005051942A1 (en) * 2003-11-19 2005-06-09 Signal Pharmaceuticals, Llc Indazole compounds and methods of use thereof as protein kinase inhibitors
GB0330002D0 (en) 2003-12-24 2004-01-28 Astrazeneca Ab Quinazoline derivatives
RU2006134022A (ru) * 2004-02-27 2008-04-10 Ф.Хоффманн-Ля Рош Аг (Ch) Производные индазола и содержащие их фармацевтические композиции
EP1720855A4 (en) * 2004-03-02 2008-12-17 Smithkline Beecham Corp HEMMER OF ACT ACTIVITY
WO2005094823A1 (ja) * 2004-03-30 2005-10-13 Kyowa Hakko Kogyo Co., Ltd. Ｆｌｔ－３阻害剤
WO2005108370A1 (ja) * 2004-04-16 2005-11-17 Ajinomoto Co., Inc. ベンゼン化合物
EP1742627A4 (en) 2004-05-06 2009-08-26 Plexxikon Inc PDE4B HEMMER AND ITS USE
AU2005264996A1 (en) * 2004-06-17 2006-01-26 Wyeth Gonadotropin releasing hormone receptor antagonists
RU2007101509A (ru) * 2004-06-17 2008-07-27 Уайт (Us) Способ получения антагонистов рецепторов гормона, высвобождающего гонадотропин
WO2006021886A1 (en) * 2004-08-26 2006-03-02 Pfizer Inc. Aminoheteroaryl compounds as protein tyrosine kinase inhibitors
AU2005279795A1 (en) * 2004-09-03 2006-03-09 Plexxikon, Inc. Bicyclic heteroaryl PDE4B inhibitors
JP4834553B2 (ja) 2004-09-17 2011-12-14 エーザイ・アール・アンド・ディー・マネジメント株式会社 医薬組成物
EP1647549A1 (en) * 2004-10-14 2006-04-19 Laboratoire Theramex Indazoles, benzisoxazoles and benzisothiazoles as estrogenic agents
RU2007120635A (ru) * 2004-11-02 2008-12-10 Пфайзер Инк. (US) Способы получения индазольных соединений
CA2586176A1 (en) * 2004-11-02 2006-05-11 Srinivasan Babu Methods for preparing indazole compounds
EP1819696A1 (en) * 2004-11-02 2007-08-22 Pfizer, Inc. Polymorphic forms of 6-2-(methylcarbamoyl)phenysulfanyl|-3-e-2-(pyridin-2-yl)ethenyl indazole
EP1831225A2 (en) 2004-11-19 2007-09-12 The Regents of the University of California Anti-inflammatory pyrazolopyrimidines
FR2878442B1 (fr) * 2004-11-29 2008-10-24 Aventis Pharma Sa THIENO(2,3-c)PYRAZOLES SUBSTITUES, PROCEDE DE PREPARATION, COMPOSITIONS LES CONTENANT ET UTILISATION
US20060142247A1 (en) * 2004-12-17 2006-06-29 Guy Georges Tricyclic heterocycles
RU2416610C2 (ru) 2004-12-30 2011-04-20 Астекс Терапьютикс Лимитед Фармацевтические соединения
US7622583B2 (en) 2005-01-14 2009-11-24 Chemocentryx, Inc. Heteroaryl sulfonamides and CCR2
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
WO2006077424A1 (en) 2005-01-21 2006-07-27 Astex Therapeutics Limited Pharmaceutical compounds
ES2552338T3 (es) 2005-01-21 2015-11-27 Astex Therapeutics Limited Compuestos farmacéuticos
ATE451363T1 (de) * 2005-01-26 2009-12-15 Schering Corp 3-(indazol-5-yl)-(1,2,4)triazinderivate und verwandte verbindungen als proteinkinaseinhibitoren zur behandlung von krebs
JPWO2006080450A1 (ja) 2005-01-27 2008-06-19 協和醗酵工業株式会社 Ｉｇｆ−１ｒ阻害剤
US7534796B2 (en) 2005-02-18 2009-05-19 Wyeth Imidazo[4,5-b]pyridine antagonists of gonadotropin releasing hormone receptor
US7538113B2 (en) 2005-02-18 2009-05-26 Wyeth 4-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor
US7582634B2 (en) 2005-02-18 2009-09-01 Wyeth 7-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor
JP5545925B2 (ja) 2005-05-17 2014-07-09 ノバルティス アーゲー ヘテロ環化合物の合成方法
US7531542B2 (en) 2005-05-18 2009-05-12 Wyeth Benzooxazole and benzothiazole antagonists of gonadotropin releasing hormone receptor
WO2006123223A1 (en) * 2005-05-19 2006-11-23 Pfizer Inc. Pharmaceutical compostions comprising an amorphous form of a vegf-r inhibitor
WO2006127587A1 (en) * 2005-05-20 2006-11-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
US7582636B2 (en) 2005-05-26 2009-09-01 Wyeth Piperazinylimidazopyridine and piperazinyltriazolopyridine antagonists of Gonadotropin Releasing Hormone receptor
US7541367B2 (en) 2005-05-31 2009-06-02 Janssen Pharmaceutica, N.V. 3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders
US7888381B2 (en) 2005-06-14 2011-02-15 Bristol-Myers Squibb Company Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity, and use thereof
US9006240B2 (en) 2005-08-02 2015-04-14 Eisai R&D Management Co., Ltd. Method for assay on the effect of vascularization inhibitor
AU2006320591B2 (en) 2005-11-29 2010-06-03 Novartis Ag Formulations of quinolinones
TW200732305A (en) * 2005-12-23 2007-09-01 Yung Shin Pharmaceutical Ind Cancer chemotherapy
SI1981851T1 (sl) 2006-01-31 2012-05-31 Array Biopharma Inc Kinazni inhibitorji in postopki za njihovo uporabo
JP2009530337A (ja) * 2006-03-23 2009-08-27 エフ．ホフマン−ラ ロシュ アーゲー 置換インダゾール誘導体、その製造方法、及びその薬剤としての利用法
CA2909277A1 (en) 2006-04-04 2007-10-11 Kevan M. Shokat Kinase antagonists
CN101443009A (zh) 2006-05-18 2009-05-27 卫材R&D管理有限公司 针对甲状腺癌的抗肿瘤剂
WO2008001885A1 (fr) 2006-06-30 2008-01-03 Kyowa Hakko Kirin Co., Ltd. INHIBITEUR DE KINASE Abl
JPWO2008001886A1 (ja) 2006-06-30 2009-11-26 協和発酵キリン株式会社 オーロラ（Ａｕｒｏｒａ）阻害剤
US8519135B2 (en) 2006-07-14 2013-08-27 Chemocentryx, Inc. Heteroaryl sulfonamides and CCR2/CCR9
JPWO2008020606A1 (ja) * 2006-08-16 2010-01-07 協和発酵キリン株式会社 血管新生阻害剤
US8865737B2 (en) 2006-08-28 2014-10-21 Eisai R&D Management Co., Ltd. Antitumor agent for undifferentiated gastric cancer
CL2007002617A1 (es) 2006-09-11 2008-05-16 Sanofi Aventis Compuestos derivados de pirrolo[2,3-b]pirazin-6-ilo; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar inflamacion de las articulaciones, artritis reumatoide, tumores, linfoma de las celulas del manto.
CA2676796C (en) 2007-01-29 2016-02-23 Eisai R & D Management Co., Ltd. Composition for treatment of undifferentiated gastric cancer
WO2008111441A1 (ja) 2007-03-05 2008-09-18 Kyowa Hakko Kirin Co., Ltd. 医薬組成物
CN101730703B (zh) * 2007-03-16 2012-12-26 中国人民解放军军事医学科学院放射与辐射医学研究所 具有抗增殖活性的苯甲酰胺类衍生物及其药用制剂
PT2134702T (pt) * 2007-04-05 2017-07-31 Pfizer Prod Inc Formas cristalinas de 6-[2-(metilcarbamoil)fenilsulfanil]-3-e-[2-(piridin-2-il)etenil]indazol adequadas para o tratamento de crescimento celular anormal em mamíferos
DE602008003055D1 (de) 2007-05-31 2010-12-02 Nerviano Medical Sciences Srl Zyklokondensierte Azaindole, die als Kinase-Hemmer wirken
AU2008275000B2 (en) 2007-07-12 2013-02-07 Chemocentryx, Inc. Fused heteroaryl pyridyl and phenyl benzenesulfonamides as CCR2 modulators for the treatment of inflammation
GB2467670B (en) 2007-10-04 2012-08-01 Intellikine Inc Chemical entities and therapeutic uses thereof
US8779197B2 (en) * 2007-10-11 2014-07-15 Vertex Pharmaceuticals Incorporated Aryl amides useful as inhibitors of voltage-gated sodium channels
NZ585063A (en) 2007-11-02 2012-05-25 Vertex Pharma [1h- pyrazolo [3, 4-b] pyridine-4-yl] -phenyle or -pyridin-2-yle derivatives as protein kinase c-theta
WO2009060945A1 (ja) 2007-11-09 2009-05-14 Eisai R & D Management Co., Ltd. 血管新生阻害物質と抗腫瘍性白金錯体との併用
SG10201605472WA (en) 2008-01-04 2016-09-29 Intellikine Llc Certain Chemical Entities, Compositions And Methods
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
WO2009114870A2 (en) 2008-03-14 2009-09-17 Intellikine, Inc. Kinase inhibitors and methods of use
WO2009114874A2 (en) 2008-03-14 2009-09-17 Intellikine, Inc. Benzothiazole kinase inhibitors and methods of use
KR101269393B1 (ko) 2008-04-28 2013-05-29 아사히 가세이 파마 가부시키가이샤 페닐프로피온산 유도체 및 이의 용도
WO2010006072A2 (en) 2008-07-08 2010-01-14 The Regents Of The University Of California Mtor modulators and uses thereof
MX2011000216A (es) 2008-07-08 2011-03-29 Intellikine Inc Inhibidores de cinasa y metodos para su uso.
CA2767331A1 (en) 2008-07-10 2010-01-14 Angion Biomedica Corp. Methods and compositions of small molecule modulators of hepatocyte growth factor (scatter factor) activity
CA2738429C (en) 2008-09-26 2016-10-25 Intellikine, Inc. Heterocyclic kinase inhibitors
CA2740885C (en) 2008-10-16 2018-04-03 The Regents Of The University Of California Fused ring heteroaryl kinase inhibitors
US8476282B2 (en) 2008-11-03 2013-07-02 Intellikine Llc Benzoxazole kinase inhibitors and methods of use
EP2414328B1 (en) 2009-04-02 2021-05-26 Merck Serono S.A. Dihydroorotate dehydrogenase inhibitors
WO2010129816A2 (en) 2009-05-07 2010-11-11 Intellikine, Inc. Heterocyclic compounds and uses thereof
EP2987487B1 (en) 2009-08-10 2020-10-07 Samumed, LLC Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
US8980899B2 (en) 2009-10-16 2015-03-17 The Regents Of The University Of California Methods of inhibiting Ire1
WO2011073521A1 (en) 2009-12-15 2011-06-23 Petri Salven Methods for enriching adult-derived endothelial progenitor cells and uses thereof
SMT201700581T1 (it) 2009-12-21 2018-01-11 Samumed Llc 1h-pirazolo[3,4-b]piridine e loro usi terapeutici
WO2011090738A2 (en) 2009-12-29 2011-07-28 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
UY33236A (es) 2010-02-25 2011-09-30 Novartis Ag Inhibidores dimericos de las iap
JP2013522292A (ja) * 2010-03-16 2013-06-13 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド インダゾール化合物およびそれらの使用
AU2011255218B2 (en) 2010-05-21 2015-03-12 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
CA2802644C (en) 2010-06-25 2017-02-21 Eisai R & D Management Co., Ltd. Antitumor agent using compounds having kinase inhibitory effect in combination
CN103261225A (zh) 2010-07-23 2013-08-21 波士顿大学董事会 作为用于抑制病理性血管生成和肿瘤细胞侵袭力的治疗剂以及用于分子成像和靶向递送的抗DEspR抑制剂
CA2817577A1 (en) 2010-11-10 2012-05-18 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
UY33794A (es) 2010-12-13 2012-07-31 Novartis Ag Inhibidores diméricos de las iap
CN103261186A (zh) 2010-12-13 2013-08-21 诺瓦提斯公司 二聚化iap抑制剂
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
TWI659956B (zh) 2011-01-10 2019-05-21 美商英菲尼提製藥股份有限公司 製備異喹啉酮之方法及異喹啉酮之固體形式
TWI592411B (zh) 2011-02-23 2017-07-21 英特爾立秦有限責任公司 激酶抑制劑之組合及其用途
JP2014509660A (ja) 2011-04-01 2014-04-21 ユニバーシティ・オブ・ユタ・リサーチ・ファウンデイション ＰＤＫ１キナーゼの阻害剤としての置換３−（１Ｈ−ベンゾ｛ｄ｝イミダゾール−２−イル）−１Ｈ−インダゾール類似体
BR112013021941B1 (pt) 2011-04-18 2022-11-16 Eisai R & D Management Co., Ltd Agente terapêutico para tumor
ES2841809T3 (es) 2011-06-03 2021-07-09 Eisai R&D Man Co Ltd Biomarcadores para pronosticar y evaluar el grado de respuesta de sujetos con cáncer de tiroides y de riñón a compuestos de lenvatinib
HK1198475A1 (en) 2011-07-19 2015-05-08 无限药品股份有限公司 Heterocyclic compounds and uses thereof
JP6027610B2 (ja) 2011-07-19 2016-11-16 インフィニティー ファーマシューティカルズ， インコーポレイテッド 複素環式化合物及びその使用
US8575336B2 (en) * 2011-07-27 2013-11-05 Pfizer Limited Indazoles
AR091790A1 (es) 2011-08-29 2015-03-04 Infinity Pharmaceuticals Inc Derivados de isoquinolin-1-ona y sus usos
MX370814B (es) 2011-09-02 2020-01-08 Univ California Pirazolo[3,4-d]pirimidinas sustituidas y usos de las mismas.
MX390742B (es) 2011-09-14 2025-03-21 Samumed Llc Indazol-3-carboxamidas y su uso como inhibidores de la trayectoria de señalizacion de wnt/b-catenina.
CN102432595B (zh) * 2011-09-14 2013-09-25 湖南有色凯铂生物药业有限公司 N-吲哚-1-酰胺类化合物及作为抗癌药物的应用
EA025183B1 (ru) 2011-09-27 2016-11-30 Новартис Аг 3-пиримидин-4-ил-оксазолидин-2-оны в качестве ингибиторов мутантной idh
CA2856291C (en) 2011-11-17 2020-08-11 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
KR20140098242A (ko) 2011-12-05 2014-08-07 노파르티스 아게 안드로겐 수용체 길항제로서의 시클릭 우레아 유도체
FR2985257B1 (fr) * 2011-12-28 2014-02-14 Sanofi Sa Composes dimeres agonistes des recepteurs des fgfs (fgfrs), leur procede de preparation et leur application en therapeutique
AU2013208720A1 (en) 2012-01-09 2014-07-24 Arrowhead Research Corporation RNAi agents to treat Beta-Catenin related diseases
JO3357B1 (ar) 2012-01-26 2019-03-13 Novartis Ag مركبات إيميدازوبيروليدينون
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
PT2770994T (pt) 2012-05-04 2019-11-04 Samumed Llc 1h-pirazolo[3,4-b]piridinas e utilizações terapêuticas destas
PT3495367T (pt) 2012-06-13 2020-11-12 Incyte Holdings Corp Compostos tricíclicos substituídos como inibidores de fgfr
JP6231262B2 (ja) * 2012-06-20 2017-11-15 大日本印刷株式会社 ピタバスタチンカルシウムの前駆体の製造法
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
SG11201502331RA (en) 2012-09-26 2015-04-29 Univ California Modulation of ire1
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
USRE48175E1 (en) 2012-10-19 2020-08-25 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
CN103804349A (zh) * 2012-11-01 2014-05-21 杨子娇 一类治疗青光眼的化合物及其用途
NZ744567A (en) 2012-11-01 2020-03-27 Infinity Pharmaceuticals Inc Treatment of cancers using pi3 kinase isoform modulators
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
EP2937337A4 (en) 2012-12-21 2016-06-22 Eisai R&D Man Co Ltd AMORPHIC FORM OF CHINOLINE DERIVATIVES AND METHOD FOR THE PRODUCTION THEREOF
EP2943198B1 (en) 2013-01-08 2019-07-17 Samumed, LLC 3-(benzoimidazol-2-yl)-indazole inhibitors of the wnt signaling pathway and therapeutic uses thereof
CN104370889A (zh) * 2013-01-24 2015-02-25 韩冰 一类降低眼压的化合物及其制备方法和用途
PT2952510T (pt) * 2013-02-02 2019-04-16 Centaurus Biopharma Co Ltd Inibidor de proteína-cinase de 2-aminopiridina substituída
PE20151428A1 (es) 2013-02-19 2015-09-24 Novartis Ag Derivados de benzotiofeno y composiciones de los mismos como degradantes selectivos de los receptores de estrogeno
EA028033B1 (ru) 2013-03-14 2017-09-29 Новартис Аг 3-пиримидин-4-ил-оксазолидин-2-оны в качестве ингибиторов мутантного idh
EA028122B1 (ru) 2013-03-14 2017-10-31 Новартис Аг 3-пиримидин-4-илоксазолидин-2-оны в качестве ингибиторов мутантного idh
US9481667B2 (en) 2013-03-15 2016-11-01 Infinity Pharmaceuticals, Inc. Salts and solid forms of isoquinolinones and composition comprising and methods of using the same
WO2014147586A1 (en) 2013-03-22 2014-09-25 Novartis Ag 1-(2-(ethylamino)pyrimidin-4-yl)pyrrolidin-2-ones as inhibitors of mutant idh
PE20152033A1 (es) 2013-04-19 2016-01-21 Incyte Holdings Corp Heterociclos bicicliclos como inhibidores de fgfr
MX368099B (es) 2013-05-14 2019-09-19 Eisai R&D Man Co Ltd Biomarcadores para predecir y evaluar el grado de respuesta de sujetos con cancer de endometrio a compuestos de tipo lenvatinib.
US20150018376A1 (en) * 2013-05-17 2015-01-15 Novartis Ag Pyrimidin-4-yl)oxy)-1h-indole-1-carboxamide derivatives and use thereof
CN103387565B (zh) * 2013-07-29 2014-10-29 苏州明锐医药科技有限公司 阿西替尼的制备方法
TWI657085B (zh) 2013-10-04 2019-04-21 英菲尼提製藥股份有限公司 雜環化合物及其用途
US9751888B2 (en) 2013-10-04 2017-09-05 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
WO2015058140A1 (en) 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
EP3057955B1 (en) 2013-10-18 2018-04-11 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
CN103570696B (zh) * 2013-11-06 2016-02-24 湖南欧亚生物有限公司 一种阿西替尼中间体的制备方法以及在制备阿西替尼中的应用
WO2015067224A1 (en) 2013-11-08 2015-05-14 Zentiva, K.S. Salts of 6-[2-(methylcarbamoyl)phenylsulfanyl]-3-e-[2-(pyridin-2-yl)ethanyl] indazole
WO2015092634A1 (en) 2013-12-16 2015-06-25 Novartis Ag 1,2,3,4-tetrahydroisoquinoline compounds and compositions as selective estrogen receptor antagonists and degraders
CN105899491B (zh) 2014-01-17 2019-04-02 诺华股份有限公司 用于抑制shp2活性的1-哒嗪-/三嗪-3-基-哌(-嗪)/啶/吡咯烷衍生物及其组合物
EP3094629B1 (en) 2014-01-17 2018-08-22 Novartis AG 1-(triazin-3-yl/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions thereof for inhibiting the activity of shp2
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
NZ724368A (en) 2014-03-19 2023-07-28 Infinity Pharmaceuticals Inc Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders
CN106458920B (zh) * 2014-03-31 2019-02-15 千寿制药株式会社 炔基吲唑衍生物及其用途
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
WO2015181624A2 (en) 2014-05-28 2015-12-03 Idenix Pharmaceuticals, Inc Nucleoside derivatives for the treatment of cancer
CN104072484B (zh) * 2014-07-07 2016-07-06 渤海大学 氮-(4-(芳巯基)-1氢-吲唑-3-基)-1-(芳杂环取代)甲基亚胺类化合物及其药学上可接受的盐及其制备方法和应用
AR101196A1 (es) 2014-07-16 2016-11-30 Gruenenthal Gmbh Compuestos de pirimidina sustituidos
AR101198A1 (es) 2014-07-16 2016-11-30 Gruenenthal Gmbh Pirimidinas 2,5-sustituidas como inhibidores de pde4b
SI3524595T1 (sl) 2014-08-28 2022-10-28 Eisai R&D Management Co., Ltd. Derivat kinolina visoke čistosti in postopek njegove proizvodnje
WO2016040190A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
WO2016040181A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040193A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
WO2016040182A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 2-(1h-indazol-3-yl)-1h-imidazo[4,5-c]pyridine and therapeutic uses thereof
WO2016040184A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040185A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof
WO2016040188A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040180A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
BR112017005510A2 (pt) 2014-09-17 2018-08-14 Celgene Quanticel Res Inc inibidores da histona-desmetilase.
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US10508108B2 (en) 2014-12-05 2019-12-17 Merck Sharp & Dohme Corp. Tricyclic compounds as inhibitors of mutant IDH enzymes
WO2016089797A1 (en) 2014-12-05 2016-06-09 Merck Sharp & Dohme Corp. Novel tricyclic compounds as inhibitors of mutant idh enzymes
EP3226690B1 (en) 2014-12-05 2020-05-20 Merck Sharp & Dohme Corp. Novel tricyclic compounds as inhibitors of mutant idh enzymes
MA41140A (fr) 2014-12-12 2017-10-17 Cancer Research Tech Ltd Dérivés de 2,4-dioxo-quinazoline-6-sulfonamide en tant qu'inhibiteurs de la parg
MA41179A (fr) * 2014-12-19 2017-10-24 Cancer Research Tech Ltd Composés inhibiteurs de parg
AU2015371251B2 (en) 2014-12-23 2020-06-11 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
EP3246046A4 (en) 2015-01-13 2018-12-05 Kyoto University Agent for preventing and/or treating amyotrophic lateral sclerosis
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
PE20171514A1 (es) 2015-02-20 2017-10-20 Incyte Corp Heterociclos biciclicos como inhibidores de fgfr
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US20180028662A1 (en) 2015-02-25 2018-02-01 Eisai R&D Management Co., Ltd. Method for Suppressing Bitterness of Quinoline Derivative
CA2978226A1 (en) 2015-03-04 2016-09-09 Merck Sharpe & Dohme Corp. Combination of a pd-1 antagonist and a vegfr/fgfr/ret tyrosine kinase inhibitor for treating cancer
AU2016243529B2 (en) 2015-03-27 2021-03-25 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
US9580406B2 (en) 2015-04-28 2017-02-28 Signa S.A. De C.V. Processes for the preparation of axitinib
US10815264B2 (en) 2015-05-27 2020-10-27 Southern Research Institute Nucleotides for the treatment of cancer
EP3302379B1 (en) 2015-06-06 2023-11-22 Cloudbreak Therapeutics, LLC Compositions and methods for treating pterygium
EP3307728A4 (en) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. COMBINATION THERAPY OF TRANSCRIPTION INHIBITORS AND CHINESE INHIBITORS
MX373231B (es) 2015-06-16 2020-05-08 Eisai R&D Man Co Ltd Agente anticancerigeno.
ES2741746T3 (es) 2015-06-19 2020-02-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
US10287266B2 (en) 2015-06-19 2019-05-14 Novartis Ag Compounds and compositions for inhibiting the activity of SHP2
ES2824576T3 (es) 2015-06-19 2021-05-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
GB201511382D0 (en) 2015-06-29 2015-08-12 Imp Innovations Ltd Novel compounds and their use in therapy
GB201511790D0 (en) 2015-07-06 2015-08-19 Iomet Pharma Ltd Pharmaceutical compound
WO2017024004A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10463651B2 (en) 2015-08-03 2019-11-05 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-indazoles and therapeutic uses thereof
WO2017024021A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
WO2017024025A1 (en) 2015-08-03 2017-02-09 Sunil Kumar Kc 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10206908B2 (en) 2015-08-03 2019-02-19 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
US10383861B2 (en) 2015-08-03 2019-08-20 Sammumed, LLC 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
US10195185B2 (en) 2015-08-03 2019-02-05 Samumed, Llc 3-(1H-imidazo[4,5-C]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
US10166218B2 (en) 2015-08-03 2019-01-01 Samumed, Llc 3-(1H-indol-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
US10392383B2 (en) 2015-08-03 2019-08-27 Samumed, Llc 3-(1H-benzo[d]imidazol-2-yl)-1H-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017024003A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10226453B2 (en) 2015-08-03 2019-03-12 Samumed, Llc 3-(1H-indol-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017023988A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10604512B2 (en) 2015-08-03 2020-03-31 Samumed, Llc 3-(1H-indol-2-yl)-1H-indazoles and therapeutic uses thereof
WO2017023987A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
US10285983B2 (en) 2015-08-03 2019-05-14 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-B] pyridines and therapeutic uses thereof
WO2017024015A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10285982B2 (en) 2015-08-03 2019-05-14 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
US11453697B1 (en) 2015-08-13 2022-09-27 Merck Sharp & Dohme Llc Cyclic di-nucleotide compounds as sting agonists
CA2995365C (en) 2015-08-13 2021-10-12 Merck Sharp & Dohme Corp. Cyclic di-nucleotide compounds as sting agonists
KR102587702B1 (ko) 2015-08-20 2023-10-12 에자이 알앤드디 매니지먼트 가부시키가이샤 종양 치료제
CA2996978A1 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
US10160761B2 (en) 2015-09-14 2018-12-25 Infinity Pharmaceuticals, Inc. Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same
KR102317700B1 (ko) * 2015-10-07 2021-10-26 아이비바 바이오파마, 인크. 피부 섬유성 장애를 치료하는 조성물 및 방법
BR112018007720A2 (pt) * 2015-10-22 2018-10-23 Selvita S A novos derivados de piridona e seu uso como inibidores da quinase
EP3371187A4 (en) 2015-11-06 2019-09-04 Samumed, LLC 2- (1H-INDAZOLE-3-YL) -3H-IMIDAZO [4,5-C] PYRIDINE AND ITS USE AS AN INHIBITOR OF INHIBITOR
WO2017106062A1 (en) 2015-12-15 2017-06-22 Merck Sharp & Dohme Corp. Novel compounds as indoleamine 2,3-dioxygenase inhibitors
WO2017161116A1 (en) 2016-03-17 2017-09-21 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors
AR108325A1 (es) 2016-04-27 2018-08-08 Samumed Llc Isoquinolin-3-il carboxamidas y preparación y uso de las mismas
US10577362B2 (en) 2016-05-04 2020-03-03 Genoscience Pharma Substituted 2, 4-diamino-quinoline derivatives for use in the treatment of proliferative diseases
HUE060797T2 (hu) 2016-06-01 2023-04-28 Biosplice Therapeutics Inc Eljárás N-(5-(3-(7-(3-fluorfenil)-3H-imidazo[4,5-c]piridin-2-il)-1H-indazol-5-il)- piridin-3-il)-3-metilbutánamid elõállítására
US10919914B2 (en) 2016-06-08 2021-02-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
KR102457146B1 (ko) 2016-06-14 2022-10-19 노파르티스 아게 Shp2의 활성을 억제하기 위한 화합물 및 조성물
UA125216C2 (uk) 2016-06-24 2022-02-02 Інфініті Фармасьютікалз, Інк. Комбінована терапія
MX386187B (es) 2016-10-04 2025-03-18 Merck Sharp & Dohme Llc Compuestos de benzo[b]tiofeno como agonistas de sting.
MX391624B (es) 2016-10-21 2025-03-04 Samumed Llc Métodos de uso de indazol-3-carboxamidas y su uso como inhibidores de la ruta de señalización de wnt/b-catenina.
EP3534878A1 (en) 2016-11-07 2019-09-11 Samumed, LLC Single-dose, ready-to-use injectable formulations
WO2018091542A1 (en) 2016-11-21 2018-05-24 Idenix Pharmaceuticals Llc Cyclic phosphate substituted nucleoside derivatives for the treatment of liver diseases
JP7013464B2 (ja) 2016-11-23 2022-02-15 ケモセントリックス， インコーポレイテッド 巣状分節性糸球体硬化症を治療する方法
WO2018138685A2 (en) 2017-01-27 2018-08-02 Janssen Biotech, Inc. Cyclic dinucleotides as sting agonists
CN110234404A (zh) 2017-01-27 2019-09-13 詹森生物科技公司 作为sting激动剂的环状二核苷酸
JP6581320B2 (ja) 2017-02-08 2019-09-25 エーザイ・アール・アンド・ディー・マネジメント株式会社 腫瘍治療用医薬組成物
US20190388407A1 (en) 2017-02-12 2019-12-26 Aiviva Biopharma, Inc. Multikinase inhibitors of vegf and tfg beta and uses thereof
EP3584241B1 (en) 2017-02-14 2023-04-26 FUJIFILM Corporation Method for producing indazole compound, and indazole compound
WO2018208667A1 (en) 2017-05-12 2018-11-15 Merck Sharp & Dohme Corp. Cyclic di-nucleotide compounds as sting agonists
MX2019013014A (es) 2017-05-16 2020-08-06 Eisai R&D Man Co Ltd Tratamiento de carcinoma hepatocelular.
CN108947961B (zh) * 2017-05-18 2021-06-04 四川大学 吲唑类衍生物及其制备方法和用途
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EP3661499A4 (en) 2017-08-04 2021-04-21 Merck Sharp & Dohme Corp. COMBINATIONS OF PD-1 ANTAGONISTS AND STING BENZO AGONISTS [B
WO2019027858A1 (en) 2017-08-04 2019-02-07 Merck Sharp & Dohme Corp. BENZO [B] STING THIOPHEN AGONISTS FOR THE TREATMENT OF CANCER
EP4360651A3 (en) 2017-08-24 2024-07-17 Novo Nordisk A/S Glp-1 compositions and uses thereof
CN111201223B (zh) 2017-09-11 2024-07-09 克鲁松制药公司 SHP2的八氢环戊二烯并[c]吡咯别构抑制剂
WO2019067332A1 (en) 2017-09-27 2019-04-04 Merck Sharp & Dohme Corp. COMPOSITIONS AND METHODS FOR TREATING CANCER THROUGH A COMBINATION OF PROGRAMMED DEATH ANTIBODY ANTIBODIES (PD-1) AND A CXCR2 ANTAGONIST
JP2020536919A (ja) 2017-10-11 2020-12-17 ケモセントリックス， インコーポレイテッド Ｃｃｒ２アンタゴニストによる巣状分節性糸球体硬化症の治療
WO2019089412A1 (en) 2017-11-01 2019-05-09 Merck Sharp & Dohme Corp. Novel substituted tetrahydroquinolin compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
EP3709986B1 (en) 2017-11-14 2023-11-01 Merck Sharp & Dohme LLC Novel substituted biaryl compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
JP7269928B2 (ja) 2017-11-14 2023-05-09 メルク・シャープ・アンド・ドーム・エルエルシー インドールアミン ２，３－ジオキシゲナーゼ（ｉｄｏ）阻害剤としての新規の置換ビアリール化合物
KR20200099178A (ko) 2017-12-15 2020-08-21 얀센 바이오테크 인코포레이티드 Sting 작용제로서의 환상 다이뉴클레오티드
EP3727401A4 (en) 2017-12-20 2022-04-06 Merck Sharp & Dohme Corp. CYCLIC DI-NUCLEOTIDE COMPOUNDS AS STING AGONISTS
US12215116B2 (en) 2018-03-13 2025-02-04 Merck Sharp & Dohme Llc Arginase inhibitors and methods of use
US11702430B2 (en) 2018-04-03 2023-07-18 Merck Sharp & Dohme Llc Aza-benzothiophene compounds as STING agonists
CN111971277B (zh) 2018-04-03 2023-06-06 默沙东有限责任公司 作为sting激动剂的苯并噻吩及相关化合物
CR20200591A (es) 2018-05-04 2021-03-31 Incyte Corp Sales de un inhibidor de fgfr
CN119241541A (zh) 2018-05-04 2025-01-03 因赛特公司 Fgfr抑制剂的固体形式和其制备方法
CN110452176A (zh) * 2018-05-07 2019-11-15 四川大学 吲唑类衍生物及其制备方法和用途
WO2019231870A1 (en) 2018-05-31 2019-12-05 Merck Sharp & Dohme Corp. Novel substituted [1.1.1] bicyclo compounds as indoleamine 2,3-dioxygenase inhibitors
EP3810615A4 (en) 2018-06-20 2022-03-30 Merck Sharp & Dohme Corp. Arginase inhibitors and methods of use
CA3099763A1 (en) 2018-06-25 2020-01-02 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
AU2019344897B2 (en) 2018-09-18 2024-01-18 Nikang Therapeutics, Inc. Tri-substituted heteroaryl derivatives AS SRC homology-2 phosphatase inhibitors
SG11202102981SA (en) 2018-09-25 2021-04-29 Black Diamond Therapeutics Inc Quinazoline derivatives as tyrosine kinase inhibitor, compositions, methods of making them and their use
WO2020068873A1 (en) 2018-09-25 2020-04-02 Black Diamond Therapeutics, Inc. Tyrosine kinase inhibitor compositions, methods of making and methods of use
IL305106B1 (en) 2018-09-29 2025-04-01 Novartis Ag Process for producing a compound for inhibiting the activity of SHP2
WO2020092183A1 (en) 2018-11-01 2020-05-07 Merck Sharp & Dohme Corp. Novel substituted pyrazole compounds as indoleamine 2,3-dioxygenase inhibitors
US12065438B2 (en) 2018-11-06 2024-08-20 Merck Sharp & Dohme Llc Substituted tricyclic compounds as indoleamine 2,3-dioxygenase inhibitors
CN111205227A (zh) * 2018-11-22 2020-05-29 四川大学 3-乙烯基吲唑类衍生物及其制备方法和用途
US12264134B2 (en) 2018-11-28 2025-04-01 Merck Sharp & Dohme Llc Substituted piperazine amide compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors
WO2020131598A1 (en) 2018-12-18 2020-06-25 Merck Sharp & Dohme Corp. Arginase inhibitors and methods of use
US12281126B2 (en) 2018-12-28 2025-04-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
JP7532385B2 (ja) * 2019-01-31 2024-08-13 杏林製薬株式会社 １５－ｐｇｄｈ阻害薬
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
EP3946324B1 (en) 2019-04-04 2025-07-30 Merck Sharp & Dohme LLC Inhibitors of histone deacetylase-3 useful for the treatment of cancer, inflammation, neurodegeneration diseases and diabetes
JP2022526827A (ja) 2019-04-11 2022-05-26 アンジオン バイオメディカ コーポレーション （ｅ）－３－［２－（２－チエニル）ビニル］－１ｈ－ピラゾールの固体形態
WO2020212253A1 (en) 2019-04-18 2020-10-22 Synthon B.V. Process for preparing axitinib, process for purifying the intermediate 2-((3-iodo-1h-indazol-6-yl)thio)-n-methylbenzamide, process for purifying axitinib via the axitinib hcl salt, solid form of the axitinib hcl salt
WO2020225413A1 (en) 2019-05-09 2020-11-12 Synthon B.V. Pharmaceutical composition comprising axitinib
WO2020260547A1 (en) 2019-06-27 2020-12-30 Rigontec Gmbh Design method for optimized rig-i ligands
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
AU2020324388A1 (en) 2019-08-02 2022-02-24 Mersana Therapeutics, Inc. Bis-[N-((5-carbamoyl)-1H-benzo[d]imidazol-2-yl)-pyrazol-5-carboxamide] derivatives and related compounds as STING (Stimulator of Interferon Genes) agonists for the treatment of cancer
EP4013749A1 (en) 2019-08-15 2022-06-22 Black Diamond Therapeutics, Inc. Alkynyl quinazoline compounds
CN112442011B (zh) * 2019-08-30 2023-11-14 润佳（苏州）医药科技有限公司 一种前药化合物及其在治疗癌症方面的应用
CN112442010B (zh) * 2019-08-30 2023-10-03 润佳（苏州）医药科技有限公司 一类前药化合物及其在治疗癌症方面的应用
CA3147801A1 (en) * 2019-08-30 2021-03-04 Jiasheng LU Prodrugs of the tyrosine kinase inhibitor for treating cancer
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
AU2020366006A1 (en) 2019-10-14 2022-04-21 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN112694474B (zh) * 2019-10-23 2022-03-18 四川大学 吲唑类衍生物及其制备方法和用途
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
EP4069683A1 (en) 2019-12-06 2022-10-12 Mersana Therapeutics, Inc. Dimeric compounds as sting agonists
WO2021126725A1 (en) 2019-12-17 2021-06-24 Merck Sharp & Dohme Corp. Novel substituted 1,3,8-triazaspiro[4,5]decane-2,4-dione compounds as indoleamine 2,3-dioxygenase (ido) and/or tryptophan 2,3-dioxygenase (tdo) inhibitors
US20230140132A1 (en) 2020-01-07 2023-05-04 Merck Sharp & Dohme Llc Arginase inhibitors and methods of use
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN111829859B (zh) * 2020-01-20 2024-01-05 北京林业大学 一种高效杨树种子透明染色及其三维成像的方法
CA3168543A1 (en) 2020-01-29 2021-08-05 Gilead Sciences, Inc. Glp-1r modulating compounds
TWI878456B (zh) 2020-02-18 2025-04-01 丹麥商諾佛 儂迪克股份有限公司 Glp-1組成物及其用途
BR102020005423A2 (pt) * 2020-03-18 2021-09-28 Faculdades Catolicas Compostos n-acil-hidrazônicos, uso no tratamento de agregopatias degenerativas amiloides e não-amiloides, e composição farmacêutica
WO2021195206A1 (en) 2020-03-24 2021-09-30 Black Diamond Therapeutics, Inc. Polymorphic forms and related uses
BR112022019919A2 (pt) 2020-04-02 2023-02-14 Mersana Therapeutics Inc Conjugado de anticorpo-fármaco compreendendo agonistas de sting
CR20220565A (es) 2020-05-06 2023-01-13 Merck Sharp & Dohme Llc Inhibidores de il4i1 y métodos de uso
WO2021232367A1 (zh) * 2020-05-21 2021-11-25 四川大学 3-乙烯基吲唑类衍生物及其制备方法和用途
CN113943271B (zh) * 2020-07-15 2023-11-14 鲁南制药集团股份有限公司 一种阿昔替尼晶型及其制备方法
CN112028831A (zh) * 2020-09-24 2020-12-04 山东大学 一种苯并吡唑类化合物、其制备方法及作为抗肿瘤药物的应用
EP4259619A1 (en) * 2020-12-08 2023-10-18 Disarm Therapeutics, Inc. Benzopyrazole inhibitors of sarm1
IL303661A (en) 2020-12-22 2023-08-01 Nikang Therapeutics Inc Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway
CA3208313A1 (en) 2021-01-13 2022-07-21 Monte Rosa Therapeutics Ag Isoindolinone compounds
WO2022170052A1 (en) 2021-02-05 2022-08-11 Black Diamond Therapeutics, Inc. Quinazoline derivatives, pyridopyrimidine derivatives, pyrimidopyrimidine derivatives, and uses thereof
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
WO2022219407A1 (en) 2021-04-14 2022-10-20 Monte Rosa Therapeutics Ag Isoindolinone compounds
EP4323349A1 (en) 2021-04-14 2024-02-21 Monte Rosa Therapeutics AG Isoindolinone amide compounds useful to treat diseases associated with gspt1
WO2022227015A1 (en) 2021-04-30 2022-11-03 Merck Sharp & Dohme Corp. Il4i1 inhibitors and methods of use
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
EP4370522A1 (en) 2021-07-14 2024-05-22 Nikang Therapeutics, Inc. Alkylidene derivatives as kras inhibitors
CN115701423B (zh) * 2021-08-02 2025-03-25 沈阳化工大学 三氟乙基硫醚（亚砜）取代苯类化合物的制备方法及其中间体
IL315722A (en) 2022-03-23 2024-11-01 Ideaya Biosciences Inc Piperazine-substituted indazole compounds as PARG inhibitors
TW202346292A (zh) 2022-03-28 2023-12-01 美商尼坎醫療公司 作為週期蛋白依賴性激酶２抑制劑的磺醯胺基衍生物
EP4282415A1 (en) 2022-05-26 2023-11-29 Genepharm S.A. A stable tablet composition of axitinib
WO2023240024A1 (en) 2022-06-08 2023-12-14 Nikang Therapeutics, Inc. Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors
WO2024032584A1 (zh) * 2022-08-08 2024-02-15 苏州必扬医药科技有限公司 一种蛋白酪氨酸激酶抑制剂及其医疗用途
AU2023375457A1 (en) 2022-11-11 2025-05-01 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway
US20240336608A1 (en) 2023-03-29 2024-10-10 Merck Sharp & Dohme Llc Il4i1 inhibitors and methods of use
WO2025072462A1 (en) 2023-09-27 2025-04-03 Nikang Therapeutics, Inc. Sulfonamide derivatives as cyclin-dependent kinase 2 inhibitors
WO2025082316A1 (zh) * 2023-10-17 2025-04-24 苏州必扬医药科技有限公司 一种眼用制剂及其制备方法和应用
WO2025117616A1 (en) 2023-11-27 2025-06-05 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and cyclin-dependent kinase 4 via ubiquitin proteasome pathway
WO2025117981A1 (en) 2023-12-02 2025-06-05 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5625031A (en) * 1994-02-08 1997-04-29 Bristol-Myers Squibb Company Peptide inhibitors of the p33cdk2 and p34cdc2 cell cycle regulatory kinases and human papillomavirus E7 oncoprotein
US5631156A (en) * 1994-06-21 1997-05-20 The University Of Michigan DNA encoding and 18 KD CDK6 inhibiting protein
CA2203517A1 (en) * 1994-11-10 1996-05-23 Alan M. Laibelman Pharmaceutical pyrazole compositions useful as inhibitors of protein kinases
ZA951822B (en) * 1994-12-23 1996-09-26 Glaxo Group Ltd Chemical compounds
US5710173A (en) * 1995-06-07 1998-01-20 Sugen, Inc. Thienyl compounds for inhibition of cell proliferative disorders
US5733920A (en) * 1995-10-31 1998-03-31 Mitotix, Inc. Inhibitors of cyclin dependent kinases
US5760028A (en) * 1995-12-22 1998-06-02 The Dupont Merck Pharmaceutical Company Integrin receptor antagonists
AU2103097A (en) * 1996-03-15 1997-10-10 Zeneca Limited Cinnoline derivatives and use as medicine
EP2223920A3 (en) * 1996-06-19 2011-09-28 Aventis Pharma Limited Substituted azabicyclic compounds
CA2264798A1 (en) * 1996-09-04 1998-03-12 Pfizer Inc. Indazole derivatives and their use as inhibitors of phosphodiesterase (pde) type iv and the production of tumor necrosis factor (tnf)
CN1158269C (zh) * 1997-10-27 2004-07-21 阿古龙制药公司 作为cdk抑制剂的取代的4-氨基-噻唑-2-基化合物
PL340753A1 (en) * 1997-11-04 2001-02-26 Pfizer Prod Inc Substitution of indazolic bioisoster for cathechol in therapeutically active compounds
TR200001256T2 (tr) * 1997-11-04 2000-11-21 Pfizer Products Inc. Terapötik olarak aktif bileşimler.
PE20010306A1 (es) * 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa

Also Published As

Publication number Publication date
SI1614683T1 (sl) 2008-02-29
EA200200120A1 (ru) 2002-08-29
BRPI0012352B8 (pt) 2021-05-25
EE200100717A (et) 2003-02-17
EP1614683A1 (en) 2006-01-11
BG66070B1 (bg) 2011-01-31
FR13C0010I1 (no) 2013-03-22
DE60037211D1 (de) 2008-01-03
MY137622A (en) 2009-02-27
YU92901A (sh) 2004-09-03
CN1374950A (zh) 2002-10-16
CY1107147T1 (el) 2012-10-24
EA004460B1 (ru) 2004-04-29
NO2013004I2 (no) 2014-06-02
DZ3191A1 (fr) 2001-01-11
ES2296014T3 (es) 2008-04-16
IS2791B (is) 2012-06-15
RS50339B (sr) 2009-11-10
PT1614683E (pt) 2008-01-24
CR6517A (es) 2006-09-21
DK1614683T3 (da) 2008-03-25
SI1218348T1 (sl) 2008-02-29
JP3878849B2 (ja) 2007-02-07
CY2013009I1 (el) 2016-04-13
CY2013009I2 (el) 2016-04-13
NO20060596L (no) 2002-03-01
CZ301667B6 (cs) 2010-05-19
CN1495171A (zh) 2004-05-12
GT200000107A (es) 2001-12-21
CN1234693C (zh) 2006-01-04
HRP20020109A2 (en) 2003-12-31
SK19252001A3 (sk) 2002-11-06
SV2002000121A (es) 2002-12-02
ZA200110061B (en) 2003-02-06
CZ20014634A3 (cs) 2002-09-11
BG106380A (bg) 2002-09-30
NO2013004I1 (no) 2013-03-18
KR100529639B1 (ko) 2006-01-16
MEP45108A (en) 2011-05-10
PL355757A1 (en) 2004-05-17
JP3969669B2 (ja) 2007-09-05
EP1218348B1 (en) 2007-10-24
JO2319B1 (en) 2005-09-12
MA26803A1 (fr) 2004-12-20
HU228502B1 (en) 2013-03-28
ES2293906T3 (es) 2008-04-01
WO2001002369A3 (en) 2002-04-25
HUP0202490A3 (en) 2003-01-28
CA2383630C (en) 2008-11-18
PT1218348E (pt) 2007-12-14
BR0012352A (pt) 2002-05-14
WO2001002369A2 (en) 2001-01-11
AU777701B2 (en) 2004-10-28
CO5190686A1 (es) 2002-08-29
DE60036879T2 (de) 2008-02-14
GEP20063885B (en) 2006-08-10
AP2002002392A0 (en) 2002-03-31
HK1085470A1 (en) 2006-08-25
DK1218348T3 (da) 2008-02-25
UA66933C2 (uk) 2004-06-15
EE05585B1 (et) 2012-10-15
BRPI0012352B1 (pt) 2016-08-16
AU5785200A (en) 2001-01-22
HUP0202490A2 (hu) 2002-11-28
CY1107148T1 (el) 2012-01-25
PL212108B1 (pl) 2012-08-31
LU92154I2 (fr) 2013-04-22
IS6207A (is) 2001-12-19
AR065937A2 (es) 2009-07-15
EP1218348A2 (en) 2002-07-03
EP1614683B1 (en) 2007-11-21
JP2003503481A (ja) 2003-01-28
ME00385B (me) 2011-05-10
SK286936B6 (sk) 2009-07-06
BE2013C015I2 (no) 2019-05-21
CA2383630A1 (en) 2001-01-11
NZ516676A (en) 2003-09-26
DE60037211T2 (de) 2008-12-11
DE60036879D1 (de) 2007-12-06
CR10194A (es) 2008-09-30
HK1048813A1 (en) 2003-04-17
NO322507B1 (no) 2006-10-16
KR20020027379A (ko) 2002-04-13
ATE376543T1 (de) 2007-11-15
JP2006348043A (ja) 2006-12-28
IL146710A0 (en) 2002-07-25
HK1065037A1 (en) 2005-02-08
HRP20020109B1 (en) 2008-07-31
MXPA01012795A (es) 2002-09-02
AR035554A1 (es) 2004-06-16
MY139999A (en) 2009-11-30
PA8498001A1 (es) 2002-08-26
CN1137884C (zh) 2004-02-11
AP1486A (en) 2005-11-01
OA11980A (en) 2006-04-18
NO20015797D0 (no) 2001-11-28
TNSN00146A1 (fr) 2005-11-10
FR13C0010I2 (fr) 2013-08-16
UY26231A1 (es) 2001-01-31
PE20010306A1 (es) 2001-03-29

Similar Documents

Publication Publication Date Title
NO20015797D0 (no) Indazolforbindelser og farmasöytiske forbindelser for inhibering av proteinkinaser, og fremgangsmåter til anvendelsederav
NO20022117L (no) Indazolforbindelser, farmasöytiske preparater, og fremgangsmåte til mediering eller inhibering av celleprofilerasjon
DK1202965T3 (da) Indolderivater, fremgangsmåde til fremstilling deraf, farmaceutiske præparater indeholdende disse og deres medicinske anvendelse
NO20016185L (no) Bicykliske heterocykler, medikamenter inneholdende disse forbindelser, deres anvendelse og fremgangsmåte for fremstillingderav
DK1345910T3 (da) Quinazolinderivater, lægemidler indeholdende forbindelserne, deres anvendelse og fremgangsmåde til fremstilling deraf
NO20016277D0 (no) Systemer og fremgangsmåter for aerolisering av farmasöytiske formuleringer
EE200100659A (et) Diaminotiasoolid ja nende kasutamine proteiinikinaaside pärssimiseks
DK0927555T3 (da) Anvendelse af cyclooxygenase-2-hæmmere til behandling og forebyggelse af tumorer, tumorrelaterede forstyrrelser og kakesi
NO20020635L (no) Hemmere av proteinpolymeriserings og metodene som brukes
EE200300475A (et) Türosiini kinaasi inhibiitorid, neid sisaldavad ravimkoostised ja nimetatud ühendid kasutamiseks haiguste ravis
ATE380814T1 (de) Kinaseinhibitoren als arzneimittel
IS6560A (is) Lyfjasamsetning fyrir meðhöndlun á bráðum, þrálátum sársauka og/eða taugakerfissársauka og mígreni
NO20002721D0 (no) Heterocykliske forbindelser for inhibitering av gastrisk syresekresjon, fremgangsmÕter for deres fremstilling og farmasøytiske preparater derav
NO20031152D0 (no) Befruktningshindrende fremgangsmåte og administrasjonsform for det samme
NO20032332L (no) Benzodiazepinderivatforbindelser, fremgangsmåte til fremstilling og anvendelse derav
IS6202A (is) Lyfjauppskriftir og aðferðir til að gefa morfín ínös
NO20024775D0 (no) Hydroksyfenyl-piperidin-4-yliden-metyl-benzamidderivater til behandling av smerte
NO20015542D0 (no) Fremgangsmåte for fremstilling og anvendelse av N- desmetylzopikloner
NO20026212D0 (no) Forbindelse for medikamentavleveringssystem og fremgangsmåte for fremstilling av forbindelsen
AU1189201A (en) Therapeutic compositions including protein kinase c inhibitors
NO20024777D0 (no) Kinolinyl-piperidin-4-yliden-metyl-benzamidderivater til behandling av smerte
NO20024776D0 (no) Hydroksyfenyl-piperazinyl-metyl-benzamidderivater til behandling av smerte
IS6172A (is) Notkun melatoníns til lækninga
IS2331B (is) 2-arýlimínó-2,3-díhýdróþíasólafleiður, aðferðir til að framleiða þær og meðferðarfræðileg notkun þeirra
DK1228026T3 (da) 15-Hydroxyicosatetraensyrerelaterede forbindelser og fremgangsmåde til anvendelse

Legal Events

Date Code Title Description
SPCF Filing of supplementary protection certificate

Free format text: PRODUCT NAME: INLYTA-AXITINIB; REG. NO/DATE: EU/1/12/777/001-006 20120903

Spc suppl protection certif: 2013004

Filing date: 20130226

SPCG Granted supplementary protection certificate

Free format text: PRODUCT NAME: INLYTA-AXITINIB; REG. NO/DATE: EU/1/12/777/001-006 20120903

Spc suppl protection certif: 2013004

Filing date: 20130226

Extension date: 20250630

CHAD Change of the owner's name or address (par. 44 patent law, par. patentforskriften)

Owner name: AGOURON PHARMACEUTICALS, US

SPCS Change of name or address of the owner of a supplementary protection certificate

Owner name: AGOURON PHARMACEUTICALS INC, US

Spc suppl protection certif: 2013004

Effective date: 20180406

MK1K Patent expired