[go: up one dir, main page]

AR065937A2 - Compuesto derivado indazol, composicion farmaceutica que lo comprende y su uso en la fabricacion de medicamentos para modular la actividad de proteina quinasa - Google Patents

Compuesto derivado indazol, composicion farmaceutica que lo comprende y su uso en la fabricacion de medicamentos para modular la actividad de proteina quinasa

Info

Publication number
AR065937A2
AR065937A2 ARP080101395A ARP080101395A AR065937A2 AR 065937 A2 AR065937 A2 AR 065937A2 AR P080101395 A ARP080101395 A AR P080101395A AR P080101395 A ARP080101395 A AR P080101395A AR 065937 A2 AR065937 A2 AR 065937A2
Authority
AR
Argentina
Prior art keywords
refers
aryl
heteroaryl
term
substituted
Prior art date
Application number
ARP080101395A
Other languages
English (en)
Inventor
Stephan James Cripps
Theodore O Johnson Jr
Min Teng
R Kania
Adam Thomas Russell
C Thomas
Yande Huan
Regina A Reichert
John F Braganza
Hiep The Luu
S Bender
A Borchardt
C Palmer
M Vamey
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=AR065937(A2) "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 AR065937A2 publication Critical patent/AR065937A2/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Emergency Medicine (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)

Abstract

Compuesto derivado de indazol que responde a la formula (1) donde: R1 es un arilo o heteroarilo sustituido, o un grupo de formula CH=CH-R3 o CH=N-R3, donde R3 es un alquilo, alquenilo, cicloalquilo, heterocicloalquilo, arilo o heteroarilo sustituidoo no sustituido; y R2 es Y-Ar, donde Y es NH y Ar es arilo sustituido o no sustituido; donde el término alquilo hace referencia a grupos C1-12 alquilo de cadena recta y ramificada, el término alquenilo hacer referencia grupos C2-12 alquenilo decadena recta y ramificada, el término cicloalquilo hace referencia a C3-12 carbociclos saturados o parcialmente insaturados, el término heterocicloalquilo hace referencia a radicales monocíclicos saturados o parcialmente insaturados, el términoheterocicloalquilo hace referencia a radicales monocíclicos saturados o parcialmente insaturados que contienen átomos de carbono y al menos un heteroátomo seleccionado entre nitrogeno, oxígeno y azufre, los términos arilo y heteroarilo hacenreferencia a estructuras de anillos aromáticos monocíclicos y policíclicos, donde arilo hace referencia a aquellos que con carbociclos y heteroarilo hace referencia a aquellos que son heterociclos, y los grupos arilo y heteroarilo pueden estaropcionalmente sustituidos con una estructura de anillo fusionado o un puente, o una sal de éste aceptable para el uso farmacéutico. También se describen composiciones farmacéuticas que comprenden estos compuestos y el uso de los mismos en lafabricacion de medicamentos para modular la actividad de proteina quinasa.
ARP080101395A 1999-07-02 2008-04-03 Compuesto derivado indazol, composicion farmaceutica que lo comprende y su uso en la fabricacion de medicamentos para modular la actividad de proteina quinasa AR065937A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US14213099P 1999-07-02 1999-07-02

Publications (1)

Publication Number Publication Date
AR065937A2 true AR065937A2 (es) 2009-07-15

Family

ID=22498654

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP000103381A AR035554A1 (es) 1999-07-02 2000-06-30 Compuesto derivado de indazol, composicion farmaceutica que lo comprende y su uso en la fabricacion de medicamentos para modular la actividad de quinasa proteina.
ARP080101395A AR065937A2 (es) 1999-07-02 2008-04-03 Compuesto derivado indazol, composicion farmaceutica que lo comprende y su uso en la fabricacion de medicamentos para modular la actividad de proteina quinasa

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP000103381A AR035554A1 (es) 1999-07-02 2000-06-30 Compuesto derivado de indazol, composicion farmaceutica que lo comprende y su uso en la fabricacion de medicamentos para modular la actividad de quinasa proteina.

Country Status (52)

Country Link
EP (2) EP1614683B1 (es)
JP (2) JP3878849B2 (es)
KR (1) KR100529639B1 (es)
CN (2) CN1137884C (es)
AP (1) AP1486A (es)
AR (2) AR035554A1 (es)
AT (1) ATE376543T1 (es)
AU (1) AU777701B2 (es)
BE (1) BE2013C015I2 (es)
BG (1) BG66070B1 (es)
BR (1) BRPI0012352B8 (es)
CA (1) CA2383630C (es)
CO (1) CO5190686A1 (es)
CR (2) CR6517A (es)
CY (3) CY1107147T1 (es)
CZ (1) CZ301667B6 (es)
DE (2) DE60037211T2 (es)
DK (2) DK1614683T3 (es)
DZ (1) DZ3191A1 (es)
EA (1) EA004460B1 (es)
EE (1) EE05585B1 (es)
ES (2) ES2296014T3 (es)
FR (1) FR13C0010I2 (es)
GE (1) GEP20063885B (es)
GT (1) GT200000107A (es)
HK (3) HK1065037A1 (es)
HR (1) HRP20020109B1 (es)
HU (1) HU228502B1 (es)
IL (1) IL146710A0 (es)
IS (1) IS2791B (es)
JO (1) JO2319B1 (es)
LU (1) LU92154I2 (es)
MA (1) MA26803A1 (es)
ME (1) ME00385B (es)
MX (1) MXPA01012795A (es)
MY (2) MY139999A (es)
NO (3) NO322507B1 (es)
NZ (1) NZ516676A (es)
OA (1) OA11980A (es)
PA (1) PA8498001A1 (es)
PE (1) PE20010306A1 (es)
PL (1) PL212108B1 (es)
PT (2) PT1218348E (es)
RS (1) RS50339B (es)
SI (2) SI1614683T1 (es)
SK (1) SK286936B6 (es)
SV (1) SV2002000121A (es)
TN (1) TNSN00146A1 (es)
UA (1) UA66933C2 (es)
UY (1) UY26231A1 (es)
WO (1) WO2001002369A2 (es)
ZA (1) ZA200110061B (es)

Families Citing this family (346)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SK288365B6 (sk) 1999-02-10 2016-07-01 Astrazeneca Ab Medziprodukty pre chinazolínové deriváty ako inhibítory angiogenézy
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
NZ519121A (en) 1999-12-24 2004-05-28 Aventis Pharma Ltd Azaindoles useful as Syk kinase inhibitors
JP2003522174A (ja) 2000-02-07 2003-07-22 ブリストル−マイヤーズ スクイブ カンパニー サイクリン依存性キナーゼの3−アミノピラゾール阻害剤
WO2001068585A1 (fr) * 2000-03-14 2001-09-20 Fujisawa Pharmaceutical Co., Ltd. Nouveaux composes amides
WO2001081348A1 (en) 2000-04-25 2001-11-01 Bristol-Myers Squibb Company USE OF 5-THIO-, SULFINYL- AND SULFONYLPYRAZOLO[3,4-b]-PYRIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS
CN1315822C (zh) 2000-08-09 2007-05-16 阿斯特拉曾尼卡有限公司 具有vegf抑制活性的喹啉衍生物
NZ523388A (en) 2000-08-09 2004-09-24 Astrazeneca Ab Cinnoline compounds
ES2334641T3 (es) 2000-09-01 2010-03-15 Novartis Vaccines And Diagnostics, Inc. Derivados aza heterociclicos y su uso terapeutico.
EA006711B1 (ru) 2000-09-11 2006-02-24 Чирон Корпорейшн Хинолиноновые производные в качестве ингибиторов тирозинкиназы
KR100589032B1 (ko) 2000-10-20 2006-06-14 에자이 가부시키가이샤 질소 함유 방향환 유도체
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
JP2004536113A (ja) * 2001-07-03 2004-12-02 カイロン コーポレイション チロシンキナーゼおよびセリン/スレオニンキナーゼのインヒビターとしてのインダゾールベンズイミダゾール化合物
US7101884B2 (en) 2001-09-14 2006-09-05 Merck & Co., Inc. Tyrosine kinase inhibitors
BR0213562A (pt) * 2001-10-26 2004-08-31 Aventis Pharma Inc Benzimidazóis e análogos e seu uso como inibidores de cinases de proteìna
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
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
WO2003064413A1 (en) 2002-02-01 2003-08-07 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
BR0313396A (pt) 2002-08-12 2005-06-28 Sugen Inc 3-pirrolil-piridopirazóis e 3-pirrolil-indazóis, como inibidores de quinase
KR20050037585A (ko) 2002-08-23 2005-04-22 카이론 코포레이션 벤지미다졸 퀴놀리논 및 그들의 사용
US20060058366A1 (en) * 2002-12-03 2006-03-16 Kyowa Hakko Kogyo Co., Ltd. Jnk inhibitor
CN1747950A (zh) * 2002-12-19 2006-03-15 美国辉瑞有限公司 用于治疗眼病的作为蛋白激酶抑制剂的2-(1h-吲唑-6-基氨基)-苯甲酰胺化合物
US7192976B2 (en) 2002-12-21 2007-03-20 Angion Biomedica Corporation Small molecule modulators of hepatocyte growth factor (scatter factor) activity
CA2517517C (en) 2003-03-03 2012-12-18 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
US7135575B2 (en) 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
BRPI0409230A (pt) * 2003-04-03 2006-03-28 Pfizer formas de dosagem compreendendo ag013736
EP1618133A1 (en) * 2003-04-17 2006-01-25 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
EP1651612B9 (en) 2003-07-22 2012-09-05 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
WO2005009389A2 (en) 2003-07-23 2005-02-03 Exelixis, Inc. Anaplastic lymphoma kinase modulators and methods of use
CN100390149C (zh) 2003-07-30 2008-05-28 协和发酵工业株式会社 吲唑衍生物
JP4363530B2 (ja) * 2003-07-30 2009-11-11 協和発酵キリン株式会社 タンパク質キナーゼ阻害剤
US7494983B2 (en) * 2003-09-04 2009-02-24 Merck & Co. Inc. Ophthalmic compositions for treating ocular hypertension
WO2005028624A2 (en) * 2003-09-15 2005-03-31 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
KR101167573B1 (ko) 2003-11-07 2012-07-30 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 개선된 약학적 성질을 갖는 퀴놀리논 화합물의 약학적으로허용가능한 염
WO2005044788A1 (ja) 2003-11-11 2005-05-19 Eisai Co., Ltd. ウレア誘導体およびその製造方法
EP2065383A1 (en) * 2003-11-19 2009-06-03 Signal Pharmaceuticals, Inc. 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
JP2007526324A (ja) * 2004-03-02 2007-09-13 スミスクライン・ビーチャム・コーポレイション Akt活性のある阻害剤
JPWO2005094823A1 (ja) * 2004-03-30 2007-08-16 協和醗酵工業株式会社 Flt−3阻害剤
JPWO2005108370A1 (ja) * 2004-04-16 2008-03-21 味の素株式会社 ベンゼン化合物
AU2005325271A1 (en) 2004-05-06 2006-07-27 Plexxikon, Inc. PDE4B inhibitors and uses therefor
CN101006078A (zh) 2004-06-17 2007-07-25 惠氏公司 促性腺素释放激素受体拮抗剂
CN1968948A (zh) * 2004-06-17 2007-05-23 惠氏公司 用于制备促性腺激素释放激素受体拮抗剂的方法
EP1786777A1 (en) * 2004-08-26 2007-05-23 Pfizer, Inc. Aminoheteroaryl compounds as protein tyrosine kinase inhibitors
JP2008512380A (ja) * 2004-09-03 2008-04-24 プレキシコン,インコーポレーテッド Pde4b阻害剤
AU2005283422C1 (en) 2004-09-17 2017-02-02 Eisai R & D Management Co., Ltd. Medicinal composition
EP1647549A1 (en) * 2004-10-14 2006-04-19 Laboratoire Theramex Indazoles, benzisoxazoles and benzisothiazoles as estrogenic agents
JP2008518901A (ja) * 2004-11-02 2008-06-05 ファイザー・インク インダゾール化合物を調製するための方法
WO2006048751A1 (en) * 2004-11-02 2006-05-11 Pfizer Inc. Polymorphic forms of 6-[2-(methylcarbamoyl)phenylsulfanyl]-3-e-[2-(pyridin-2-yl)ethenyl]indazole
AU2005300241A1 (en) * 2004-11-02 2006-05-11 Pfizer Inc. Methods for preparing indazole compounds
JP2008520744A (ja) 2004-11-19 2008-06-19 ザ・レジェンツ・オブ・ザ・ユニバーシティ・オブ・カリフォルニア 抗炎症性ピラゾロピリミジン
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
US8110573B2 (en) 2004-12-30 2012-02-07 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of CDK, GSK and aurora kinases
US7622583B2 (en) 2005-01-14 2009-11-24 Chemocentryx, Inc. Heteroaryl sulfonamides and CCR2
US20090036435A1 (en) 2005-01-21 2009-02-05 Astex Therapeutics Limited Pharmaceutical Compounds
JP5475234B2 (ja) 2005-01-21 2014-04-16 アステックス・セラピューティクス・リミテッド 医薬化合物
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.
DE602006010991D1 (de) * 2005-01-26 2010-01-21 Schering Corp 3-(indazol-5-yl)-(1,2,4)triazinderivate und verwandte verbindungen als proteinkinaseinhibitoren zur behandlung von krebs
CA2596527C (en) * 2005-01-27 2013-02-12 Kyowa Hakko Kogyo Co., Ltd. Igf-1r inhibitors
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
US7534796B2 (en) 2005-02-18 2009-05-19 Wyeth Imidazo[4,5-b]pyridine antagonists of gonadotropin releasing hormone receptor
EP1888556B1 (en) 2005-05-17 2011-10-26 Novartis AG Methods for synthesizing heterocyclic compounds
US7531542B2 (en) 2005-05-18 2009-05-12 Wyeth Benzooxazole and benzothiazole antagonists of gonadotropin releasing hormone receptor
EP1885338A1 (en) * 2005-05-19 2008-02-13 Pfizer, Inc. Pharmaceutical compostions comprising an amorphous form of a vegf-r inhibitor
EP2354140A1 (en) * 2005-05-20 2011-08-10 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
EP2281901B1 (en) 2005-08-02 2013-11-27 Eisai R&D Management Co., Ltd. Anti-tumour pharmaceutical composition with angiogenesis inhibitors
CA2627544C (en) 2005-11-29 2015-07-07 Novartis Ag Formulations of quinolinones for the treatment of cancer
TW200732305A (en) * 2005-12-23 2007-09-01 Yung Shin Pharmaceutical Ind Cancer chemotherapy
BRPI0707401B8 (pt) 2006-01-31 2022-12-20 Array Biopharma Inc compostos inibidores de cinase, composição farmacêutica, processo para a preparação e usos dos referidos compostos ou de um pró-fármaco de um composto
WO2007107346A1 (en) * 2006-03-23 2007-09-27 F. Hoffmann-La Roche Ag Substituted indazole derivatives, their manufacture and use as pharmaceutical agents
PT2004654E (pt) 2006-04-04 2013-08-27 Univ California Derivados de pirazolopirimidina para utilização como antagonistas da quinase
CN104706637A (zh) 2006-05-18 2015-06-17 卫材R&D管理有限公司 针对甲状腺癌的抗肿瘤剂
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
CN101484427A (zh) 2006-06-30 2009-07-15 协和发酵麒麟株式会社 Abl激酶抑制剂
US8519135B2 (en) 2006-07-14 2013-08-27 Chemocentryx, Inc. Heteroaryl sulfonamides and CCR2/CCR9
WO2008020606A1 (fr) * 2006-08-16 2008-02-21 Kyowa Hakko Kirin Co., Ltd. Agent anti-angiogénique
KR101472600B1 (ko) 2006-08-28 2014-12-15 에자이 알앤드디 매니지먼트 가부시키가이샤 미분화형 위암에 대한 항종양제
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.
JP5319306B2 (ja) 2007-01-29 2013-10-16 エーザイ・アール・アンド・ディー・マネジメント株式会社 未分化型胃癌治療用組成物
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
EP2002836B1 (en) 2007-05-31 2010-10-20 Nerviano Medical Sciences S.r.l. Cyclocondensed azaindoles active as kinase inhibitors
PL2175859T3 (pl) 2007-07-12 2012-09-28 Chemocentryx Inc Skondensowane heteroarylopirydylo- i fenylo-benzenosulfonamidy jako modulatory CCR2 do leczenia zapalenia
US20110160232A1 (en) 2007-10-04 2011-06-30 Pingda Ren Certain chemical entities and therapeutic uses thereof
MX2010003865A (es) * 2007-10-11 2010-06-01 Vertex Pharma Aril amidas utiles como inhibidores de canales de sodio dependientes de voltaje.
AU2008331733A1 (en) 2007-11-02 2009-06-11 Vertex Pharmaceuticals Incorporated [1H- pyrazolo [3, 4-b] pyridine-4-yl] -phenyle or -pyridin-2-yle derivatives as protein kinase C-theta
KR101513326B1 (ko) 2007-11-09 2015-04-17 에자이 알앤드디 매니지먼트 가부시키가이샤 혈관 신생 저해 물질과 항종양성 백금 착물의 병용
NZ613219A (en) 2008-01-04 2014-11-28 Intellikine Llc Heterocyclic containing entities, compositions and methods
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
WO2009114874A2 (en) 2008-03-14 2009-09-17 Intellikine, Inc. Benzothiazole kinase inhibitors and methods of use
JP5547099B2 (ja) 2008-03-14 2014-07-09 インテリカイン, エルエルシー キナーゼ阻害剤および使用方法
KR101269393B1 (ko) 2008-04-28 2013-05-29 아사히 가세이 파마 가부시키가이샤 페닐프로피온산 유도체 및 이의 용도
MX2011000216A (es) 2008-07-08 2011-03-29 Intellikine Inc Inhibidores de cinasa y metodos para su uso.
WO2010006072A2 (en) 2008-07-08 2010-01-14 The Regents Of The University Of California Mtor modulators and uses thereof
CN102149379A (zh) 2008-07-10 2011-08-10 安吉翁生物医药有限公司 调节肝细胞生长因子(分散因子)活性的方法和肝细胞生长因子(分散因子)活性的小分子调节剂组合物
CA2738429C (en) 2008-09-26 2016-10-25 Intellikine, Inc. Heterocyclic kinase inhibitors
ES2570429T3 (es) 2008-10-16 2016-05-18 Univ California Inhibidores de heteroaril quinasa de anillo condensado
US8476282B2 (en) 2008-11-03 2013-07-02 Intellikine Llc Benzoxazole kinase inhibitors and methods of use
MY159575A (en) * 2009-04-02 2017-01-13 Merck Serono Sa Dihydroorotate dehydrogenase inhibitors
JP5789252B2 (ja) 2009-05-07 2015-10-07 インテリカイン, エルエルシー 複素環式化合物およびその使用
BR112012002854B1 (pt) 2009-08-10 2020-02-18 Samumed, Llc Composto ou sal farmaceuticamente aceitável, composição farmacêutica e uso dos mesmos
WO2011047384A2 (en) 2009-10-16 2011-04-21 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
EP3001903B1 (en) 2009-12-21 2017-10-25 Samumed, LLC 1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
EP2937345B1 (en) 2009-12-29 2018-03-21 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
KR20130006664A (ko) * 2010-03-16 2013-01-17 다나-파버 캔서 인스티튜트 인크. 인다졸 화합물 및 그의 용도
WO2011146882A1 (en) 2010-05-21 2011-11-24 Intellikine, Inc. Chemical compounds, compositions and methods for kinase modulation
JP5898074B2 (ja) 2010-06-25 2016-04-06 エーザイ・アール・アンド・ディー・マネジメント株式会社 キナーゼ阻害作用を有する化合物の併用による抗腫瘍剤
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
WO2012064973A2 (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
WO2012080260A1 (en) 2010-12-13 2012-06-21 Novartis Ag Dimeric iap inhibitors
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
CA2824197C (en) 2011-01-10 2020-02-25 Michael Martin Processes for preparing isoquinolinones and solid forms of isoquinolinones
JP6130305B2 (ja) 2011-02-23 2017-05-17 インテリカイン, エルエルシー キナーゼ阻害剤の組み合わせおよびそれらの使用
WO2012135799A1 (en) 2011-04-01 2012-10-04 University Of Utah Research Foundation Substituted 3-(1h-benzo{d}imidazol-2-yl)-1h-indazole-analogs as inhibitors of the pdk1 kinase
KR101762999B1 (ko) 2011-04-18 2017-07-28 에자이 알앤드디 매니지먼트 가부시키가이샤 종양 치료제
EP3444363B1 (en) 2011-06-03 2020-11-25 Eisai R&D Management Co., Ltd. Biomarkers for prediciting and assessing responsiveness of thyroid and kidney cancer subjects to lenvatinib compounds
MX2014000648A (es) 2011-07-19 2014-09-25 Infinity Pharmaceuticals Inc Compuestos heterociclicos y sus usos.
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
MX2014002542A (es) 2011-08-29 2014-07-09 Infinity Pharmaceuticals Inc Compuestos heterociclicos y usos de los mismos.
JP6342805B2 (ja) 2011-09-02 2018-06-13 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 置換ピラゾロ[3,4−d]ピリミジンおよびその用途
CN109705097B (zh) 2011-09-14 2022-02-01 萨穆梅德有限公司 吲唑-3-羧酰胺及其作为WNT/β-CATENIN信号传导通路抑制剂的用途
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
PH12014500682A1 (en) 2011-09-27 2014-05-12 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
EP2822935B1 (en) 2011-11-17 2019-05-15 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
US20140329858A1 (en) 2011-12-05 2014-11-06 Novartis Ag Cyclic Urea Derivatives As Androgen Receptor Antagonists
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
EP2802658A2 (en) 2012-01-09 2014-11-19 Novartis AG Rnai agents to treat beta-catenin related diseases
UY34591A (es) 2012-01-26 2013-09-02 Novartis Ag Compuestos de imidazopirrolidinona
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
DK2770994T3 (da) 2012-05-04 2019-11-11 Samumed Llc 1h-pyrazolo[3,4-b]pyridiner og terapeutiske anvendelser deraf
SMT202000673T1 (it) 2012-06-13 2021-01-05 Incyte Holdings Corp Composti triciclici sostituiti come inibitori di 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
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
EP2900673A4 (en) 2012-09-26 2016-10-19 Univ California IRE1 MODULATION
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
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
IL291945A (en) 2012-11-01 2022-06-01 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
MX2015004979A (es) 2012-12-21 2015-07-17 Eisai R&D Man Co Ltd Forma amorfa de derivado de quinolina y metodo para su produccion.
CN105120862A (zh) 2013-01-08 2015-12-02 萨穆梅德有限公司 Wnt信号途径的3-(苯并咪唑-2-基)-吲唑抑制剂及其治疗应用
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
WO2014117718A1 (zh) * 2013-02-02 2014-08-07 正大天晴药业集团股份有限公司 取代的2-氨基吡啶类蛋白激酶抑制剂
MA38325B1 (fr) 2013-02-19 2019-03-29 Novartis Ag Dérivés de benzothiophène et compositions correspondantes en tant qu'agents de dégradation sélectifs des récepteurs des œstrogènes
BR112015023412A8 (pt) 2013-03-14 2018-01-23 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inibidores de idh mutante, sua composição farmacêutica e seu uso.
BR112015022483A2 (pt) 2013-03-14 2017-07-18 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inibidores de idh mutante
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
SG11201508328PA (en) 2013-04-19 2015-11-27 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
SG11201509278XA (en) 2013-05-14 2015-12-30 Eisai R&D Man Co Ltd Biomarkers for predicting and assessing responsiveness of endometrial cancer subjects to lenvatinib compounds
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
US9751888B2 (en) 2013-10-04 2017-09-05 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9359365B2 (en) 2013-10-04 2016-06-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
EP3057956B1 (en) 2013-10-18 2021-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
CA2927917C (en) 2013-10-18 2022-08-09 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of proliferative 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
EP3094627B1 (en) 2014-01-17 2018-08-22 Novartis AG 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and 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
WO2015107494A1 (en) 2014-01-17 2015-07-23 Novartis Ag 1 -(triazin-3-yi_/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions thereof for inhibiting the activity of shp2
CN106456628A (zh) 2014-03-19 2017-02-22 无限药品股份有限公司 用于治疗PI3K‑γ介导的障碍的杂环化合物
EP3127900B1 (en) * 2014-03-31 2017-10-18 Senju Pharmaceutical Co., Ltd. Alkynyl indazole derivative and use thereof
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
JP2017516779A (ja) 2014-05-28 2017-06-22 アイデニクス・ファーマシューティカルズ・エルエルシー 癌治療のためのヌクレオシド誘導体
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
RS63559B1 (sr) 2014-08-28 2022-10-31 Eisai R&D Man Co Ltd Derivat hinolina velike čistoće i postupak za njegovu proizvodnju
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
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
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
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
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
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
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
ES2751464T3 (es) 2014-09-17 2020-03-31 Celgene Quanticel Res Inc Inhibidores de histona desmetilasa
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
US10086000B2 (en) 2014-12-05 2018-10-02 Merck Sharp & Dohme Corp. Tricyclic compounds as inhibitors of mutant IDH enzymes
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
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
JP6854762B2 (ja) 2014-12-23 2021-04-07 ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド サイクリン依存性キナーゼ7(cdk7)の阻害剤
JP6852848B2 (ja) 2015-01-13 2021-03-31 国立大学法人京都大学 筋萎縮性側索硬化症の予防及び/又は治療剤
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
UA121669C2 (uk) 2015-02-20 2020-07-10 Інсайт Корпорейшн Біциклічні гетероцикли як інгібітори fgfr
SG11201706630UA (en) 2015-02-25 2017-09-28 Eisai R&D Man Co Ltd Method for suppressing bitterness of quinoline derivative
AU2015384801B2 (en) 2015-03-04 2022-01-06 Eisai R&D Management Co., Ltd. Combination of a PD-1 antagonist and a VEGFR/FGFR/RET tyrosine kinase inhibitor for treating cancer
CA2978518C (en) 2015-03-27 2023-11-21 Nathanael S. Gray 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
EP4335418A3 (en) 2015-06-06 2024-05-22 Cloudbreak Therapeutics, LLC Compositions and methods for treating pterygium
EP3307728A4 (en) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. ASSOCIATION THERAPY USING TRANSCRIPTION INHIBITORS AND KINASE INHIBITORS
CA2988707C (en) 2015-06-16 2023-10-10 Eisai R&D Management Co., Ltd. Combination of cbp/catenin inhibitor and immune checkpoint inhibitor for treating cancer
EP3310774B1 (en) 2015-06-19 2020-04-29 Novartis AG Compounds and compositions for inhibiting the activity of shp2
US10975080B2 (en) 2015-06-19 2021-04-13 Novartis Ag Compounds and compositions for inhibiting the activity of SHP2
US10308660B2 (en) 2015-06-19 2019-06-04 Novartis Ag Compounds and compositions for inhibiting the activity of 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
WO2017023972A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017023975A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]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
US10188634B2 (en) 2015-08-03 2019-01-29 Samumed, Llc 3-(3H-imidazo[4,5-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017023984A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
WO2017024026A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
WO2017023989A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[4,3-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
US10206909B2 (en) 2015-08-03 2019-02-19 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017023980A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines 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
WO2017023996A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines 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
WO2017024010A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-indazoles 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
US10231956B2 (en) 2015-08-03 2019-03-19 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1 H-pyrazolo[4,3-B]pyridines 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
TN2018000023A1 (en) 2015-08-13 2019-07-08 Merck Sharp & Dohme Cyclic di-nucleotide compounds as sting agonists.
US11453697B1 (en) 2015-08-13 2022-09-27 Merck Sharp & Dohme Llc Cyclic di-nucleotide compounds as sting agonists
RU2718048C2 (ru) 2015-08-20 2020-03-30 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Противоопухолевое терапевтическое средство
US11142507B2 (en) 2015-09-09 2021-10-12 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
CA2998469A1 (en) 2015-09-14 2017-03-23 Infinity Pharmaceuticals, Inc. Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same
CA3001489C (en) * 2015-10-07 2024-01-16 Diane Tang-Liu Compositions and methods of treating skin fibrotic disorders
MX2018004879A (es) * 2015-10-22 2019-02-28 Selvita S A Nuevos derivados de piridona y su uso como inhibidores de quinasas.
AU2016348639B2 (en) 2015-11-06 2022-09-08 Samumed, Llc Treatment of osteoarthritis
US10538497B2 (en) 2015-12-15 2020-01-21 Merck Sharp & Dohme Corp. 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
EP3452465B1 (en) 2016-05-04 2020-11-04 Genoscience Pharma Substituted 2, 4-diamino-quinoline derivatives for use in the treatment of proliferative diseases
JP7010851B2 (ja) 2016-06-01 2022-02-10 バイオスプライス セラピューティクス インコーポレイテッド N-(5-(3-(7-(3-フルオロフェニル)-3H-イミダゾ[4,5-c]ピリジン-2-イル)-1H-インダゾール-5-イル)ピリジン-3-イル)-3-メチルブタンアミドを調製するための方法
US10919914B2 (en) 2016-06-08 2021-02-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
PT3468972T (pt) 2016-06-14 2020-08-21 Novartis Ag Compostos e composições para inibir a atividade da shp2
CN109640999A (zh) 2016-06-24 2019-04-16 无限药品股份有限公司 组合疗法
SG10202008647TA (en) 2016-10-04 2020-10-29 Merck Sharp & Dohme BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS
WO2018075858A1 (en) 2016-10-21 2018-04-26 Samumed, Llc Methods of using indazole-3-carboxamides and their use as wnt/b-catenin signaling pathway inhibitors
WO2018085865A1 (en) 2016-11-07 2018-05-11 Samumed, Llc Single-dose, ready-to-use injectable formulations
US20190365788A1 (en) 2016-11-21 2019-12-05 Idenix Pharmaceuticals Llc Cyclic phosphate substituted nucleoside derivatives for the treatment of liver diseases
RU2022102328A (ru) 2016-11-23 2022-04-01 Хемоцентрикс, Инк. Способ лечения фокально-сегментарного гломерулосклероза
US11492367B2 (en) 2017-01-27 2022-11-08 Janssen Biotech, Inc. Cyclic dinucleotides as sting agonists
EP3573717B1 (en) 2017-01-27 2021-07-28 Janssen Biotech, Inc. Cyclic dinucleotides as sting agonists
US20190388407A1 (en) 2017-02-12 2019-12-26 Aiviva Biopharma, Inc. Multikinase inhibitors of vegf and tfg beta and uses thereof
WO2018151126A1 (ja) * 2017-02-14 2018-08-23 富士フイルム株式会社 インダゾール化合物の製造方法およびインダゾール化合物
WO2018208667A1 (en) 2017-05-12 2018-11-15 Merck Sharp & Dohme Corp. Cyclic di-nucleotide compounds as sting agonists
CN108947970B (zh) * 2017-05-18 2022-04-05 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
EP3661498A4 (en) 2017-08-04 2021-04-21 Merck Sharp & Dohme Corp. STING THIOPHENE BENZO [B] AGONISTS FOR CANCER TREATMENT
JP2020529421A (ja) 2017-08-04 2020-10-08 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. がんの処置のためのPD−1アンタゴニストおよびベンゾ[b]チオフェンSTINGアゴニストの組み合わせ
CN118903386A (zh) 2017-08-24 2024-11-08 诺和诺德股份有限公司 Glp-1组合物及其用途
MA50245A (fr) 2017-09-11 2020-07-22 Krouzon Pharmaceuticals Inc Inhibiteurs allostériques octahydrocyclopenta[c]pyrrole de shp2
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
EP3694504A4 (en) 2017-10-11 2021-07-14 ChemoCentryx, Inc. TREATMENT OF FOCAL SEGMENTAL GLOMERULOSCLEROSIS WITH CRC2 ANTAGONISTS
EP3703692A4 (en) 2017-11-01 2021-04-28 Merck Sharp & Dohme Corp. Novel substituted tetrahydroquinolin compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
US11498904B2 (en) 2017-11-14 2022-11-15 Merck Sharp & Dohme Llc 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
JP7317014B2 (ja) 2017-12-15 2023-07-28 ヤンセン バイオテツク,インコーポレーテツド Stingアゴニストとしての環状ジヌクレオチド
US11685761B2 (en) 2017-12-20 2023-06-27 Merck Sharp & Dohme Llc Cyclic di-nucleotide compounds as sting agonists
US11702430B2 (en) 2018-04-03 2023-07-18 Merck Sharp & Dohme Llc Aza-benzothiophene compounds as STING agonists
CA3095646A1 (en) 2018-04-03 2019-10-10 Merck Sharp & Dohme Corp. Benzothiophenes and related compounds as sting agonists
FI3788047T3 (fi) 2018-05-04 2024-11-02 Incyte Corp Fgft-estäjän kiinteitä muotoja ja menetelmiä niiden valmistamiseksi
MX2020011639A (es) 2018-05-04 2021-02-15 Incyte Corp Sales de un inhibidor de receptores de factor de crecimiento de fibroblastos (fgfr).
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
US11352320B2 (en) 2018-05-31 2022-06-07 Merck Sharp & Dohme Corp. Substituted [1.1.1] bicyclo compounds as indoleamine 2,3-dioxygenase inhibitors
US12187701B2 (en) 2018-06-25 2025-01-07 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
CR20210175A (es) 2018-09-18 2021-06-01 Nikang Therapeutics Inc Derivados de anillo tricíclico condensado como inhibidores de la fosfatasa de homología a src 2 (shp2)
CA3113241A1 (en) 2018-09-25 2020-04-02 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
MX2021003459A (es) 2018-09-29 2021-06-18 Novartis Ag Proceso de fabricacion de un compuesto para la inhibicion de la actividad de shp2.
US12091405B2 (en) 2018-11-01 2024-09-17 Merck Sharp & Dohme Llc Substituted pyrazole compounds as indoleamine 2,3-dioxygenase inhibitors
WO2020096871A1 (en) 2018-11-06 2020-05-14 Merck Sharp & Dohme Corp. Novel 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
EP3886845B1 (en) 2018-11-28 2024-09-04 Merck Sharp & Dohme LLC Novel substituted piperazine amide compounds as indoleamine 2, 3-dioxygenase (ido) inhibitors
EP3917911A1 (en) * 2019-01-31 2021-12-08 Kyorin Pharmaceutical Co., Ltd. 15-pgdh inhibitors
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
US20220177465A1 (en) 2019-04-04 2022-06-09 Merck Sharp & Dohme Corp. Inhibitors of histone deacetylase-3 useful for the treatment of cancer, inflammation, neurodegeneration diseases and diabetes
BR112021020367A2 (pt) 2019-04-11 2021-12-07 Angion Biomedica Corp Formas sólidas de (e)-3-[2-(2-tienil)vinil] -1h-pirazol
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
EA202193065A1 (ru) 2019-05-09 2022-03-02 Синтон Б.В. Фармацевтическая композиция, содержащая акситиниб
EP3990635A1 (en) 2019-06-27 2022-05-04 Rigontec GmbH Design method for optimized rig-i ligands
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR20220056176A (ko) 2019-08-02 2022-05-04 메르사나 테라퓨틱스, 인코포레이티드 암 치료를 위한 sting(인터페론 유전자의 자극인자) 작용제로서의 비스-[n-((5-카바모일)-1h-벤조[d]이미다졸-2-일)-피라졸-5-카복사미드] 유도체 및 관련 화합물
KR20220047810A (ko) 2019-08-15 2022-04-19 블랙 다이아몬드 테라퓨틱스, 인코포레이티드 알키닐 퀴나졸린 화합물
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
WO2021035360A1 (en) * 2019-08-30 2021-03-04 Risen (Suzhou) Pharma Tech Co., Ltd. Prodrugs of the tyrosine kinase inhibitor for treating cancer
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JOP20220083A1 (ar) 2019-10-14 2023-01-30 Incyte Corp حلقات غير متجانسة ثنائية الحلقة كمثبطات لـ fgfr
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
PE20221504A1 (es) 2019-12-04 2022-09-30 Incyte Corp Derivados de un inhibidor de fgfr
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US20230074558A1 (en) 2019-12-06 2023-03-09 Mersana Therapeutics, Inc. Dimeric compounds as sting agonists
WO2021146424A1 (en) 2020-01-15 2021-07-22 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
CN115335374A (zh) 2020-01-29 2022-11-11 吉利德科学公司 Glp-1r调节化合物
BR112022013746A2 (pt) 2020-02-18 2022-10-11 Novo Nordisk As Formulação aquosa de cagrilintida, formulação aquosa de semaglutida, dispositivo médico, e, combinação de dose fixa
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
CN115768485A (zh) 2020-04-02 2023-03-07 梅尔莎纳医疗公司 包含sting激动剂的抗体药物缀合物
CN115836054B (zh) 2020-05-06 2024-12-10 默沙东有限责任公司 Il4i1抑制剂和使用方法
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
AU2021409561A1 (en) 2020-12-22 2023-07-06 Nikang Therapeutics, Inc. Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway
EP4277901A1 (en) 2021-01-13 2023-11-22 Monte Rosa Therapeutics, Inc. 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
WO2022219412A1 (en) 2021-04-14 2022-10-20 Monte Rosa Therapeutics Ag Isoindolinone amide compounds useful to treat diseases associated with gspt1
EP4323350A1 (en) 2021-04-14 2024-02-21 Monte Rosa Therapeutics AG Isoindolinone compounds
WO2022227015A1 (en) 2021-04-30 2022-11-03 Merck Sharp & Dohme Corp. Il4i1 inhibitors and methods of use
JP2024522189A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Fgfr阻害剤としての三環式ヘテロ環
EP4370522A1 (en) 2021-07-14 2024-05-22 Nikang Therapeutics, Inc. Alkylidene derivatives as kras inhibitors
CN115701423A (zh) * 2021-08-02 2023-02-10 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
WO2023192801A1 (en) 2022-03-28 2023-10-05 Nikang Therapeutics, Inc. Sulfonamido derivatives as cyclin-dependent kinase 2 inhibitors
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
WO2024102849A1 (en) 2022-11-11 2024-05-16 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway
WO2024206357A1 (en) 2023-03-29 2024-10-03 Merck Sharp & Dohme Llc Il4i1 inhibitors and methods of use

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
JPH10509708A (ja) * 1994-11-10 1998-09-22 コア セラピューティクス,インコーポレイティド プロテイン・キナーゼのインヒビターとして有用な医薬ピラゾール組成物
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
US6514971B1 (en) * 1996-03-15 2003-02-04 Zeneca Limited Cinnoline derivatives and use as medicine
EP0934307B1 (en) * 1996-06-19 2011-04-27 Aventis Pharma Limited Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase
IL128642A0 (en) * 1996-09-04 2000-01-31 Pfizer Indazole derivatives and their use as inhibitors of phosphodiesterase (pde) type iv and the production of tumor necrosis factor (tnf)
PL342447A1 (en) * 1997-10-27 2001-06-04 Agouron Pharma Substituted 4-amino thiazol-2-yl compounds as inhibitors of cyclin-dependent kinases
EA200000385A1 (ru) * 1997-11-04 2000-10-30 Пфайзер Продактс Инк. Терапевтически активные соединения на основе индазольной биоизостерической замены катехина в ингибиторах фосфодиэстеразы типа vi (pde4)
IL135900A0 (en) * 1997-11-04 2001-05-20 Pfizer Prod Inc Indazole bioisostere replacement of catechol in therapeuticaly active compounds
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
CY2013009I2 (el) 2016-04-13
AP2002002392A0 (en) 2002-03-31
CN1234693C (zh) 2006-01-04
FR13C0010I1 (es) 2013-03-22
JO2319B1 (en) 2005-09-12
MEP45108A (en) 2011-05-10
NO20015797D0 (no) 2001-11-28
PL212108B1 (pl) 2012-08-31
CR10194A (es) 2008-09-30
DZ3191A1 (fr) 2001-01-11
NZ516676A (en) 2003-09-26
PE20010306A1 (es) 2001-03-29
CO5190686A1 (es) 2002-08-29
HK1065037A1 (en) 2005-02-08
PA8498001A1 (es) 2002-08-26
WO2001002369A3 (en) 2002-04-25
BR0012352A (pt) 2002-05-14
CN1495171A (zh) 2004-05-12
AP1486A (en) 2005-11-01
CZ301667B6 (cs) 2010-05-19
MY139999A (en) 2009-11-30
UY26231A1 (es) 2001-01-31
CY1107148T1 (el) 2012-01-25
BG106380A (bg) 2002-09-30
PT1218348E (pt) 2007-12-14
IL146710A0 (en) 2002-07-25
NO2013004I1 (no) 2013-03-18
IS6207A (is) 2001-12-19
DK1218348T3 (da) 2008-02-25
DE60037211D1 (de) 2008-01-03
DE60037211T2 (de) 2008-12-11
HUP0202490A3 (en) 2003-01-28
CY1107147T1 (el) 2012-10-24
HRP20020109B1 (en) 2008-07-31
BG66070B1 (bg) 2011-01-31
ES2293906T3 (es) 2008-04-01
CA2383630A1 (en) 2001-01-11
AU5785200A (en) 2001-01-22
GEP20063885B (en) 2006-08-10
LU92154I2 (fr) 2013-04-22
EP1218348A2 (en) 2002-07-03
FR13C0010I2 (fr) 2013-08-16
HRP20020109A2 (en) 2003-12-31
NO20060596L (no) 2002-03-01
KR100529639B1 (ko) 2006-01-16
KR20020027379A (ko) 2002-04-13
YU92901A (sh) 2004-09-03
CZ20014634A3 (cs) 2002-09-11
JP3969669B2 (ja) 2007-09-05
PL355757A1 (en) 2004-05-17
NO322507B1 (no) 2006-10-16
MXPA01012795A (es) 2002-09-02
AR035554A1 (es) 2004-06-16
EP1614683A1 (en) 2006-01-11
TNSN00146A1 (fr) 2005-11-10
GT200000107A (es) 2001-12-21
BRPI0012352B8 (pt) 2021-05-25
SK19252001A3 (sk) 2002-11-06
SV2002000121A (es) 2002-12-02
BE2013C015I2 (es) 2019-05-21
SK286936B6 (sk) 2009-07-06
EP1218348B1 (en) 2007-10-24
ZA200110061B (en) 2003-02-06
AU777701B2 (en) 2004-10-28
CY2013009I1 (el) 2016-04-13
EA200200120A1 (ru) 2002-08-29
JP2006348043A (ja) 2006-12-28
EE200100717A (et) 2003-02-17
MA26803A1 (fr) 2004-12-20
DE60036879D1 (de) 2007-12-06
RS50339B (sr) 2009-11-10
ATE376543T1 (de) 2007-11-15
EE05585B1 (et) 2012-10-15
JP3878849B2 (ja) 2007-02-07
IS2791B (is) 2012-06-15
ES2296014T3 (es) 2008-04-16
NO2013004I2 (no) 2014-06-02
CR6517A (es) 2006-09-21
HUP0202490A2 (hu) 2002-11-28
CN1374950A (zh) 2002-10-16
UA66933C2 (uk) 2004-06-15
NO20015797L (no) 2002-03-01
HK1085470A1 (en) 2006-08-25
CA2383630C (en) 2008-11-18
DK1614683T3 (da) 2008-03-25
WO2001002369A2 (en) 2001-01-11
HU228502B1 (en) 2013-03-28
CN1137884C (zh) 2004-02-11
SI1218348T1 (sl) 2008-02-29
PT1614683E (pt) 2008-01-24
MY137622A (en) 2009-02-27
EP1614683B1 (en) 2007-11-21
EA004460B1 (ru) 2004-04-29
SI1614683T1 (sl) 2008-02-29
JP2003503481A (ja) 2003-01-28
DE60036879T2 (de) 2008-02-14
BRPI0012352B1 (pt) 2016-08-16
ME00385B (me) 2011-05-10
OA11980A (en) 2006-04-18
HK1048813A1 (en) 2003-04-17

Similar Documents

Publication Publication Date Title
AR065937A2 (es) Compuesto derivado indazol, composicion farmaceutica que lo comprende y su uso en la fabricacion de medicamentos para modular la actividad de proteina quinasa
EA200200708A1 (ru) Производные бензазола и их применение в качестве модуляторов jnk
AR048642A1 (es) Compuestos de metil-aril o heteroaril-amida sustituida utiles como antagonistas del receptor de prostaglandinas e2; composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento
AR018634A1 (es) Derivados de benzo(b)tiepin-1,1,-dioxido, procedimiento para su preparacion, medicamentos conteniendo estos compuestos, procedimiento para la preparacion de medicamentos y su empleo para la preparacion de medicamentos.
FI934274A (fi) N-sulfonyl-2-oxi-indolderivat, deras framstaellning och dessa innehaollande farmaceutiska kompositioner
AR048641A1 (es) Compuestos de aril- o heteroarilamida ortosustituidos utiles como antago-nistas del receptor de prostaglandinas e2; composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicame
FI950016A0 (fi) Heterosykliset yhdisteet lääkeaineena
AR036598A1 (es) Derivados de 4,5-dihidro-1h-pirazol que tienen potente actividad antagonista de cb1
ATE73815T1 (de) Adenosin-derivate und pharmazeutische zusammenstellungen, welche diese als aktiven bestandteil enthalten.
AR020851A2 (es) Compuestos macrolidos, composiciones y su uso para la preparacion de medicamentos
BR0014137A (pt) Composto, método para inibir a aurora 2 quinase em um animal de sangue quente, uso de um composto, e, composição farmacêutica
UY27336A1 (es) Derivados de 4-piperacinilindol con afinidad receptora de 5-ht6
MX9300031A (es) Derivados de piperazina, procedimiento para su preparacion y composicion farmaucetica que los contiene.
ATE158288T1 (de) Antiatherosklerotische und antithrombotische 1- benzopyran-4-on- und 2-amino-1,3-benzoxazin-4-on- derivate
AR019427A1 (es) Compuestos heterociclicos como inhibidores de enzimas de rotamasa, procedimiento para su preparacion, su uso para la preparacion de medicamentos, composiciones farmaceuticas y compuestos intermediarios utiles para su preparacion
AR012622A1 (es) Inhibidores de proteasas, procedimiento para su preparacion, composicion farmaceutica que los comprende y el uso de los mismos en la fabricacion de unmedicamento
ES2170759T3 (es) Derivados de galantamina, un procedimiento para su preparacion y su uso como medicamentos.
AR016551A1 (es) Derivados de 2-oxindol, composiciones farmaceuticas que los comprenden y el uso de los mismos para la manufactura de medicamentos
PE20021018A1 (es) DERIVADOS DE ß - CARBOLINA
AR013152A1 (es) Derivados de 2-alquilheterodihidropirimidina, proceso para su preparacion, composiciones farmaceuticas que contienen dichos derivados y el uso de dichosderivados y composiciones como ligandos para canales de calcio neuronales de tipo n.
MX9203939A (es) Derivados de hidroisoquinolina y composiciones farmaceuticas que los contienen.
ATE13423T1 (de) Guanidinderivate und diese enthaltende pharmazeutische zusammensetzungen.
AR036092A1 (es) Un derivado de benzoxazepina, su uso y una composicion farmaceutica que lo comprende
AR028606A1 (es) Nuevos inhibidores de mmp-2/mmp-9
AR027454A1 (es) Derivados de beta-alanina, utiles como antagonistas de receptores, las composiciones farmaceuticas que las contienen y el uso de los mismos para lapreparacion de medicamentos

Legal Events

Date Code Title Description
FB Suspension of granting procedure