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CO2023004548A2 - Derivados indólicos como inhibidores de ras en el tratamiento del cáncer - Google Patents

Derivados indólicos como inhibidores de ras en el tratamiento del cáncer

Info

Publication number
CO2023004548A2
CO2023004548A2 CONC2023/0004548A CO2023004548A CO2023004548A2 CO 2023004548 A2 CO2023004548 A2 CO 2023004548A2 CO 2023004548 A CO2023004548 A CO 2023004548A CO 2023004548 A2 CO2023004548 A2 CO 2023004548A2
Authority
CO
Colombia
Prior art keywords
cancer treatment
indole derivatives
ras inhibitors
treatment
ras
Prior art date
Application number
CONC2023/0004548A
Other languages
English (en)
Inventor
G Leslie Burnett
Adrian L Gill
Elena S Koltun
James Cregg
Andreas Buckl
John E Knox
Naing Aay
Yang Liu
Bianca Jennifer Lee
David E Wildes
Meghan A Rice
Mallika Singh
Original Assignee
Revolution Medicines Inc
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
Application filed by Revolution Medicines Inc filed Critical Revolution Medicines Inc
Publication of CO2023004548A2 publication Critical patent/CO2023004548A2/es

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D471/22—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 systems contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La descripción caracteriza compuestos macrocíclicos y composiciones farmacéuticas y sus complejos proteicos, capaces de inhibir proteínas Ras y sus usos en el tratamiento de cánceres.
CONC2023/0004548A 2020-09-15 2023-04-12 Derivados indólicos como inhibidores de ras en el tratamiento del cáncer CO2023004548A2 (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202063078802P 2020-09-15 2020-09-15
US202063129231P 2020-12-22 2020-12-22
US202163184412P 2021-05-05 2021-05-05
US202163192775P 2021-05-25 2021-05-25
PCT/US2021/050454 WO2022060836A1 (en) 2020-09-15 2021-09-15 Indole derivatives as ras inhibitors in the treatment of cancer

Publications (1)

Publication Number Publication Date
CO2023004548A2 true CO2023004548A2 (es) 2023-05-08

Family

ID=78086091

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2023/0004548A CO2023004548A2 (es) 2020-09-15 2023-04-12 Derivados indólicos como inhibidores de ras en el tratamiento del cáncer

Country Status (15)

Country Link
US (2) US11690915B2 (es)
EP (1) EP4214209A1 (es)
JP (1) JP2023541916A (es)
KR (1) KR20230067635A (es)
CN (2) CN117683049A (es)
AU (1) AU2021345111A1 (es)
CA (1) CA3194067A1 (es)
CL (2) CL2023000730A1 (es)
CO (1) CO2023004548A2 (es)
CR (1) CR20230165A (es)
IL (1) IL301298A (es)
MX (1) MX2023003060A (es)
PE (1) PE20231207A1 (es)
TW (1) TW202227460A (es)
WO (1) WO2022060836A1 (es)

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022553857A (ja) 2019-11-04 2022-12-26 レボリューション メディシンズ インコーポレイテッド Ｒａｓ阻害剤
KR20220109407A (ko) 2019-11-04 2022-08-04 레볼루션 메디슨즈, 인크. Ras 억제제
CN114786777A (zh) 2019-11-04 2022-07-22 锐新医药公司 Ras抑制剂
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
CN117683049A (zh) 2020-09-15 2024-03-12 锐新医药公司 作为ras抑制剂以治疗癌症的吲哚衍生物
CR20230500A (es) * 2021-04-02 2024-02-13 Massachusetts Gen Hospital Métodos para inhibir ras
IL308193A (en) 2021-05-05 2024-01-01 Revolution Medicines Inc RAS inhibitors
CN117500811A (zh) 2021-05-05 2024-02-02 锐新医药公司 共价ras抑制剂及其用途
AU2022268962A1 (en) 2021-05-05 2023-12-14 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
AU2022281343A1 (en) 2021-05-25 2023-11-30 Revolution Medicines, Inc. Methods for inhibiting ras
WO2023015559A1 (en) * 2021-08-13 2023-02-16 Nutshell Biotech (Shanghai) Co., Ltd. Macrocycle compounds as inhibitors of ras
AR126854A1 (es) * 2021-08-27 2023-11-22 Hoffmann La Roche Compuestos macrocíclicos para el tratamiento de cáncer
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023208005A1 (en) * 2022-04-25 2023-11-02 Hansoh Bio Llc Cyclic compounds, preparation methods and medicinal uses thereof
EP4532503A1 (en) * 2022-06-01 2025-04-09 F. Hoffmann-La Roche AG Haloindole macrocyclic compounds for the treatment of cancer
AU2023285116A1 (en) 2022-06-10 2024-12-19 Revolution Medicines, Inc. Macrocyclic ras inhibitors
AU2023297941A1 (en) 2022-06-30 2025-01-16 Eli Lilly And Company Kras g12c inhibitor for treating cancer
CN119546613A (zh) 2022-07-08 2025-02-28 豪夫迈·罗氏有限公司 可用作kras抑制剂的大环化合物
AR129934A1 (es) * 2022-07-20 2024-10-16 Hoffmann La Roche Compuestos macrocíclicos para el tratamiento de cáncer
WO2024040131A1 (en) * 2022-08-17 2024-02-22 Treeline Biosciences, Inc. Pyridopyrimidine kras inhibitors
CN117903169A (zh) * 2022-09-19 2024-04-19 杭州阿诺生物医药科技有限公司 一种pan-KRAS抑制剂化合物
WO2024067857A1 (zh) * 2022-09-29 2024-04-04 南京明德新药研发有限公司 大环衍生物及其应用
WO2024081363A1 (en) 2022-10-12 2024-04-18 Revolution Medicines, Inc. Composition comprising a first ras inhibitor, second ras inhibitor and a shp2 inhibitor for use in the treatment of cancer
CN118994202A (zh) * 2022-11-16 2024-11-22 杭州阿诺生物医药科技有限公司 一种pan-KRAS抑制剂化合物
WO2024149819A1 (en) * 2023-01-13 2024-07-18 F. Hoffmann-La Roche Ag Sulfonylvinyl compounds for the treatment of cancer
WO2024153208A1 (zh) * 2023-01-19 2024-07-25 劲方医药科技(上海)有限公司 大环化合物及其制法和用途
WO2024169914A1 (en) 2023-02-14 2024-08-22 F. Hoffmann-La Roche Ag Tricyclic compounds for the treatment of cancer
WO2024189481A1 (en) 2023-03-10 2024-09-19 Novartis Ag Panras inhibitor antibody-drug conjugates and methods of use thereof
WO2024206858A1 (en) 2023-03-30 2024-10-03 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
WO2024211663A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
WO2024211712A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
WO2024216048A1 (en) 2023-04-14 2024-10-17 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
WO2024216016A1 (en) 2023-04-14 2024-10-17 Revolution Medicines, Inc. Crystalline forms of a ras inhibitor
US20240368190A1 (en) 2023-04-14 2024-11-07 Revolution Medicines, Inc. Synthesis of ras inhibitors
WO2024222864A1 (en) * 2023-04-27 2024-10-31 Shanghai Yuyao Biotech Ltd. Macrocyclic compounds and therapeutic uses thereof
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
CN116509868B (zh) * 2023-07-04 2023-10-20 四川大学华西医院 Vs6766联合bay293的应用及药物组合物
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025051241A1 (zh) * 2023-09-06 2025-03-13 劲方医药科技(上海)股份有限公司 大环化合物及其抗体-药物偶联物

Family Cites Families (402)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CY1915A (en) 1984-10-04 1985-09-27 Sandoz Ag Cyclosporins
EP0194972B1 (en) 1985-03-11 1992-07-29 Sandoz Ag Novel cyclosporins
US6905680B2 (en) 1988-11-23 2005-06-14 Genetics Institute, Inc. Methods of treating HIV infected subjects
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
US6352694B1 (en) 1994-06-03 2002-03-05 Genetics Institute, Inc. Methods for inducing a population of T cells to proliferate using agents which recognize TCR/CD3 and ligands which stimulate an accessory molecule on the surface of the T cells
US5858358A (en) 1992-04-07 1999-01-12 The United States Of America As Represented By The Secretary Of The Navy Methods for selectively stimulating proliferation of T cells
US6534055B1 (en) 1988-11-23 2003-03-18 Genetics Institute, Inc. Methods for selectively stimulating proliferation of T cells
JP2762522B2 (ja) 1989-03-06 1998-06-04 藤沢薬品工業株式会社 血管新生阻害剤
DE69013742T2 (de) 1989-04-15 1995-03-23 Fujirebio Kk Peptide und diese Peptide enthaltende Wirkstoffe gegen Dementia.
US5112946A (en) 1989-07-06 1992-05-12 Repligen Corporation Modified pf4 compositions and methods of use
PT98990A (pt) 1990-09-19 1992-08-31 American Home Prod Processo para a preparacao de esteres de acidos carboxilicos de rapamicina
US5892112A (en) 1990-11-21 1999-04-06 Glycomed Incorporated Process for preparing synthetic matrix metalloprotease inhibitors
US5120842A (en) 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5100883A (en) 1991-04-08 1992-03-31 American Home Products Corporation Fluorinated esters of rapamycin
US5118678A (en) 1991-04-17 1992-06-02 American Home Products Corporation Carbamates of rapamycin
DK0584222T3 (da) 1991-05-10 1998-02-23 Rhone Poulenc Rorer Int Bis-mono- og bicycliske aryl- og heteroarylforbindelser, som inhiberer EGF- og/eller PDGF-receptor-tyrosinkinase
US5118677A (en) 1991-05-20 1992-06-02 American Home Products Corporation Amide esters of rapamycin
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
US5151413A (en) 1991-11-06 1992-09-29 American Home Products Corporation Rapamycin acetals as immunosuppressant and antifungal agents
GB9125660D0 (en) 1991-12-03 1992-01-29 Smithkline Beecham Plc Novel compound
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
EP0562853B1 (en) 1992-03-27 1996-06-05 American Home Products Corporation 29-Demethoxyrapamycin for inducing immunosuppression
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
ZA935111B (en) 1992-07-17 1994-02-04 Smithkline Beecham Corp Rapamycin derivatives
ZA935112B (en) 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
US5256790A (en) 1992-08-13 1993-10-26 American Home Products Corporation 27-hydroxyrapamycin and derivatives thereof
GB9221220D0 (en) 1992-10-09 1992-11-25 Sandoz Ag Organic componds
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
ES2279508T3 (es) 1992-11-13 2007-08-16 Immunex Corporation Ligando elk, una citoquina.
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
US5629327A (en) 1993-03-01 1997-05-13 Childrens Hospital Medical Center Corp. Methods and compositions for inhibition of angiogenesis
US5516658A (en) 1993-08-20 1996-05-14 Immunex Corporation DNA encoding cytokines that bind the cell surface receptor hek
AU678058B2 (en) 1993-09-20 1997-05-15 John Innes Centre Recombinant production of novel polyketides
US5612340A (en) 1993-10-01 1997-03-18 Ciba-Geigy Corporation Pyrimidineamine derivatives and processes for the preparation thereof
US5656643A (en) 1993-11-08 1997-08-12 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
EP0729471A1 (en) 1993-11-19 1996-09-04 Abbott Laboratories Semisynthetic analogs of rapamycin (macrolides) being immunomodulators
PL314238A1 (en) 1993-12-17 1996-09-02 Sandoz Ltd Rapamycin derivatives
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
AU2096895A (en) 1994-03-07 1995-09-25 Sugen, Incorporated Receptor tyrosine kinase inhibitors for inhibiting cell proliferative disorders and compositions thereof
IL112873A (en) 1994-03-08 2005-03-20 Wyeth Corp Rapamycin-fkbp12 binding proteins, their isolation and their use
EP1464706A3 (en) 1994-04-15 2004-11-03 Amgen Inc., HEK5, HEK7, HEK8, HEK11, EPH-like receptor protein tyrosine kinases
ATE159257T1 (de) 1994-05-03 1997-11-15 Ciba Geigy Ag Pyrrolopyrimidinderivate mit antiproliferativer wirkung
GB9410142D0 (en) 1994-05-20 1994-07-06 Univ Warwick Carbapenems
US7175843B2 (en) 1994-06-03 2007-02-13 Genetics Institute, Llc Methods for selectively stimulating proliferation of T cells
US6303769B1 (en) 1994-07-08 2001-10-16 Immunex Corporation Lerk-5 dna
US5919905A (en) 1994-10-05 1999-07-06 Immunex Corporation Cytokine designated LERK-6
GB9524630D0 (en) 1994-12-24 1996-01-31 Zeneca Ltd Chemical compounds
US6057124A (en) 1995-01-27 2000-05-02 Amgen Inc. Nucleic acids encoding ligands for HEK4 receptors
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
EP3103799B1 (en) 1995-03-30 2018-06-06 OSI Pharmaceuticals, LLC Quinazoline derivatives
NZ304859A (en) 1995-04-03 2000-01-28 Novartis Ag 4-amino-1H-pyrazolo[3,4-d]pyrimidine derivatives, medicaments and processes for the preparation thereof
ES2153031T4 (es) 1995-04-20 2001-05-16 Pfizer Derivados del acido arilsulfonil hidroxamico como inhibidores de mmp y tnf.
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US7067318B2 (en) 1995-06-07 2006-06-27 The Regents Of The University Of Michigan Methods for transfecting T cells
US6692964B1 (en) 1995-05-04 2004-02-17 The United States Of America As Represented By The Secretary Of The Navy Methods for transfecting T cells
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
US5650415A (en) 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds
SK284529B6 (sk) 1995-06-09 2005-05-05 Novartis Ag Deriváty rapamycínu, spôsob ich prípravy, farmaceutická kompozícia s ich obsahom a súprava alebo balenie na použitie pri imunosupresii, zápale alebo infekciách
US5624677A (en) 1995-06-13 1997-04-29 Pentech Pharmaceuticals, Inc. Controlled release of drugs delivered by sublingual or buccal administration
US6124453A (en) 1995-07-04 2000-09-26 Novartis Ag Macrolides
SI9620103A (sl) 1995-07-06 1998-10-31 Novartis Ag Pirolopirimidini in postopki za njihovo pripravo
DE19534177A1 (de) 1995-09-15 1997-03-20 Merck Patent Gmbh Cyclische Adhäsionsinhibitoren
AR004010A1 (es) 1995-10-11 1998-09-30 Glaxo Group Ltd Compuestos heterociclicos
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
ATE225343T1 (de) 1995-12-20 2002-10-15 Hoffmann La Roche Matrix-metalloprotease inhibitoren
PT888349E (pt) 1996-01-23 2002-10-31 Novartis Ag Pirrolopirimidinas e processos para a sua preparacao
JP3406763B2 (ja) 1996-01-30 2003-05-12 東レ・ダウコーニング・シリコーン株式会社 シリコーンゴム組成物
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
GB9603097D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline compounds
DE19629652A1 (de) 1996-03-06 1998-01-29 Thomae Gmbh Dr K 4-Amino-pyrimidin-Derivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE19608588A1 (de) 1996-03-06 1997-09-11 Thomae Gmbh Dr K Pyrimido [5,4-d]pyrimidine, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
AU716383B2 (en) 1996-03-15 2000-02-24 Novartis Ag Novel N-7-heterocyclyl pyrrolo(2,3-d)pyrimidines and the use thereof
US6344459B1 (en) 1996-04-12 2002-02-05 Warner-Lambert Company Irreversible inhibitors of tyrosine kinases
GB9607729D0 (en) 1996-04-13 1996-06-19 Zeneca Ltd Quinazoline derivatives
JP2000512990A (ja) 1996-06-24 2000-10-03 ファイザー・インク 過増殖性疾患を処置するためのフェニルアミノ置換三環式誘導体
GEP20012348B (en) 1996-07-05 2001-01-25 Pfizer Erythromycins and Process for Their Preparation
EP0818442A3 (en) 1996-07-12 1998-12-30 Pfizer Inc. Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor
AU735648B2 (en) 1996-07-12 2001-07-12 Ariad Pharmaceuticals, Inc. Materials and method for treating or preventing pathogenic fungal infection
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
CN1230185A (zh) 1996-07-13 1999-09-29 葛兰素集团有限公司 双环芳杂环化合物用作蛋白质酪氨酸激酶的抑制剂
EP0912559B1 (en) 1996-07-13 2002-11-06 Glaxo Group Limited Fused heterocyclic compounds as protein tyrosine kinase inhibitors
HUP9903014A3 (en) 1996-07-18 2000-08-28 Pfizer Phosphinate derivatives having matrix metalloprotease inhibitor effect and medicaments containing the same
US6111090A (en) 1996-08-16 2000-08-29 Schering Corporation Mammalian cell surface antigens; related reagents
DE69738749D1 (de) 1996-08-16 2008-07-17 Schering Corp Zelloberflächen-antigen aus säugetieren und verwandte reagenzien
US6180636B1 (en) 1996-08-23 2001-01-30 Novartis Ag Substituted pyrrolopyrimidines and processes for their preparation
SK21499A3 (en) 1996-08-23 2000-05-16 Pfizer Arylsulfonylamino hydroxamic acid derivatives
SE9603465D0 (sv) 1996-09-23 1996-09-23 Astra Ab New compounds
ATE291022T1 (de) 1996-10-02 2005-04-15 Novartis Pharma Gmbh Pyrimiderivate und verfahren zu ihrer herstellung
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
AU4779897A (en) 1996-10-02 1998-04-24 Novartis Ag Fused pyrazole derivatives and processes for their preparation
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
GB9621757D0 (en) 1996-10-18 1996-12-11 Ciba Geigy Ag Phenyl-substituted bicyclic heterocyclyl derivatives and their use
PT950059E (pt) 1997-01-06 2004-10-29 Pfizer Derivados de sulfona ciclicos
WO1998033768A1 (en) 1997-02-03 1998-08-06 Pfizer Products Inc. Arylsulfonylamino hydroxamic acid derivatives
ES2301194T3 (es) 1997-02-05 2008-06-16 Warner-Lambert Company Llc Pirido 2,3-d pirimidinas y 4-aminopirimidinas como inhibidores de la proliferacion celular.
AU5493598A (en) 1997-02-07 1998-08-26 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
BR9807678A (pt) 1997-02-11 2000-02-15 Pfizer Derivados de ácidos arilsulfonil-hidroxâmicos
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
US6902913B2 (en) 1997-04-30 2005-06-07 Kosan Biosciences, Inc. Recombinant narbonolide polyketide synthase
US6150395A (en) 1997-05-30 2000-11-21 The Regents Of The University Of California Indole-3-carbinol (I3C) derivatives and methods
WO1999007701A1 (en) 1997-08-05 1999-02-18 Sugen, Inc. Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors
IL134300A (en) 1997-08-08 2004-07-25 Pfizer Prod Inc Derivatives of aryloxyacrylylsulfonaminoaminoxamic acid derivatives, pharmaceutical preparations containing them and their use in the preparation of drugs for the treatment of arthritis, cancer and other diseases characterized by the activity of metalloproteinase-13 of matrix
WO1999020758A1 (en) 1997-10-21 1999-04-29 Human Genome Sciences, Inc. Human tumor necrosis factor receptor-like proteins tr11, tr11sv1, and tr11sv2
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
US6153383A (en) 1997-12-09 2000-11-28 Verdine; Gregory L. Synthetic transcriptional modulators and uses thereof
GB9800575D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
GB9800569D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
JP2002502607A (ja) 1998-02-09 2002-01-29 ジェネンテク・インコーポレイテッド 新規な腫瘍壊死因子レセプター相同体及びそれをコードする核酸
WO1999045009A1 (en) 1998-03-04 1999-09-10 Bristol-Myers Squibb Company Heterocyclo-substituted imidazopyrazine protein tyrosine kinase inhibitors
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
EP1079859B1 (en) 1998-05-22 2010-07-14 The Board Of Trustees Of The Leland Stanford Junior University Bifunctional molecules and therapies based thereon
EP2020408B1 (en) 1998-05-29 2013-06-26 Sugen, Inc. Pyrrole substituted 2-indolinone protein kinase inhibitor
UA60365C2 (uk) 1998-06-04 2003-10-15 Пфайзер Продактс Інк. Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця
AU747427B2 (en) 1998-07-10 2002-05-16 Merck & Co., Inc. Novel angiogenesis inhibitors
JP2002523459A (ja) 1998-08-31 2002-07-30 メルク エンド カムパニー インコーポレーテッド 新規血管形成阻害剤
KR20010085877A (ko) 1998-10-02 2001-09-07 추후제출 폴리케타이드 합성 효소와 그 재조합 ｄｎａ 구성물
US6686454B1 (en) 1998-10-09 2004-02-03 Isotechnika, Inc. Antibodies to specific regions of cyclosporine related compounds
PT1004578E (pt) 1998-11-05 2004-06-30 Pfizer Prod Inc Derivados hidroxamida do acido 5-oxo-pirrolidino-2-carboxilico
CA2359801A1 (en) 1999-02-09 2000-08-17 Rajesh S. Gokhale Methods to mediate polyketide synthase module effectiveness
AU766081B2 (en) 1999-03-30 2003-10-09 Novartis Ag Phthalazine derivatives for treating inflammatory diseases
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
US6521424B2 (en) 1999-06-07 2003-02-18 Immunex Corporation Recombinant expression of Tek antagonists
DK1187918T4 (da) 1999-06-07 2009-02-23 Immunex Corp TEK-antagonister
CA2378179A1 (en) 1999-07-12 2001-01-18 Genentech, Inc. Promotion or inhibition of angiogenesis and cardiovascularization by tumor necrosis factor ligand/receptor homologs
CN1293081C (zh) 1999-08-24 2007-01-03 阿里亚德基因治疗公司 28－表雷帕霉素类似物,其制备方法，药物组合物和用途
BR0015203A (pt) 1999-11-05 2002-07-16 Astrazeneca Ab Derivado de quinazolina, processo para a preparação de um derivado de quinazolina, composição farmacêutica, uso de um composto, e, processo para a produção de um efeito antiangiogênico e/ou redutor de permeabilidade vascular em um animal de sangue quente
GB9927191D0 (en) 1999-11-17 2000-01-12 Angeletti P Ist Richerche Bio Methods and means for regulation of gene expression
US7220552B1 (en) 1999-11-19 2007-05-22 The Board Of Trustees Of The Leland Stanford Junior University Bifunctional molecules and their use in the disruption of protein-protein interactions
AU1776501A (en) 1999-11-19 2001-05-30 Board Of Trustees Of The Leland Stanford Junior University Bifunctional molecules and their use in the disruption of protein-protein interactions
ATE514676T1 (de) 1999-11-24 2011-07-15 Sugen Inc Ionisierbare indolinon derivate und deren verwendung als ptk liganden
US6515004B1 (en) 1999-12-15 2003-02-04 Bristol-Myers Squibb Company N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
US6727225B2 (en) 1999-12-20 2004-04-27 Immunex Corporation TWEAK receptor
US7141660B2 (en) 2000-02-08 2006-11-28 Sinvent As Genes encoding a nystatin polyketide synthase and their manipulation and utility
CA2406864A1 (en) 2000-02-24 2001-08-30 Xcyte Therapies, Inc. Simultaneous stimulation and concentration of cells
US6867041B2 (en) 2000-02-24 2005-03-15 Xcyte Therapies, Inc. Simultaneous stimulation and concentration of cells
US7572631B2 (en) 2000-02-24 2009-08-11 Invitrogen Corporation Activation and expansion of T cells
US6797514B2 (en) 2000-02-24 2004-09-28 Xcyte Therapies, Inc. Simultaneous stimulation and concentration of cells
IL151032A0 (en) 2000-02-25 2003-04-10 Immunex Corp Integrin antagonists
TR200200767T1 (tr) 2000-05-23 2002-09-23 Vertex Pharmaceuticals Incorporated Kaspaz engelleyiciler ve kullanımları
US7176037B2 (en) 2000-07-13 2007-02-13 The Scripps Research Institute Labeled peptides, proteins and antibodies and processes and intermediates useful for their preparation
US6630500B2 (en) 2000-08-25 2003-10-07 Cephalon, Inc. Selected fused pyrrolocarbazoles
ATE430742T1 (de) 2000-12-21 2009-05-15 Smithkline Beecham Corp Pyrimidinamine als angiogenesemodulatoren
US20020147198A1 (en) 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine derivatives and methods of use
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
WO2003014311A2 (en) 2001-08-06 2003-02-20 Kosan Biosciences, Inc. Methods for altering polyketide synthase genes
US6809077B2 (en) 2001-10-12 2004-10-26 Enanta Pharmaceuticals, Inc. Cyclosporin analogs for the treatment of autoimmune diseases
US6987090B2 (en) 2002-05-09 2006-01-17 Lg Household & Health Care Ltd. Use of 3-position cyclosporin derivatives for hair growth
US7307088B2 (en) 2002-07-09 2007-12-11 Amgen Inc. Substituted anthranilic amide derivatives and methods of use
TWI329112B (en) 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
US7012065B2 (en) 2003-02-07 2006-03-14 Enanta Pharmaceuticals, Inc. Cyclosporins for the treatment of immune disorders
EP1477563A3 (en) 2003-05-16 2004-11-24 Wyeth Cloning genes from streptomyces cyaneogriseus subsp.noncyanogenus for biosynthesis of antibiotics and methods of use
WO2004107618A2 (en) 2003-05-23 2004-12-09 Wyeth Gitr ligand and gitr ligand-related molecules and antibodies and uses thereof
ES2316995T3 (es) 2003-07-08 2009-04-16 Novartis Ag Uso de rapamicina y derivados de rapamicida para el tratamiento de la perdida osea.
EP1660126A1 (en) 2003-07-11 2006-05-31 Schering Corporation Agonists or antagonists of the clucocorticoid-induced tumour necrosis factor receptor (gitr) or its ligand for the treatment of immune disorders, infections and cancer
WO2005016252A2 (en) 2003-07-11 2005-02-24 Ariad Gene Therapeutics, Inc. Phosphorus-containing macrocycles
AR045134A1 (es) 2003-07-29 2005-10-19 Smithkline Beecham Plc Compuesto de 1h - imidazo [4,5-c] piridin-ilo, composicion farmaceutica que lo comprende, proceso para prepararla, su uso para preparar dicha composicion farmaceutica, combinacion farmaceutica, uso de la combinacion farmaceutica para la preparacion de un medicamento, procedimientos para preparar dic
DK2287156T3 (da) 2003-08-15 2013-08-26 Novartis Ag 2,4-Di(phenylamino)-pyrimidiner egnede i behandling af neoplastiske sygdomme, inflammatoriske lidelser og lidelser i immunsystemet
JP2007518399A (ja) 2003-12-02 2007-07-12 ジェンザイム コーポレイション 肺癌を診断および治療する組成物並びに方法
GB0409799D0 (en) 2004-04-30 2004-06-09 Isis Innovation Method of generating improved immune response
WO2006083289A2 (en) 2004-06-04 2006-08-10 Duke University Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity
AP2373A (en) 2004-08-26 2012-03-07 Pfizer Enantiomerically pure aminoheteroaryl compounds asprotein kinase inhibitors.
MX2007004489A (es) 2004-10-13 2007-09-21 Wyeth Corp Analogos de 17-hidroxiwortamina como inhibidores pi3k.
AU2006230099B2 (en) 2005-03-25 2012-04-19 Gitr, Inc. GITR binding molecules and uses therefor
CN109485727A (zh) 2005-05-09 2019-03-19 小野药品工业株式会社 程序性死亡-1(pd-1)的人单克隆抗体及使用抗pd-1抗体来治疗癌症的方法
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
CN101267824A (zh) 2005-09-20 2008-09-17 辉瑞产品公司 使用酪氨酸激酶抑制剂的治疗剂型和方法
WO2007133822A1 (en) 2006-01-19 2007-11-22 Genzyme Corporation Gitr antibodies for the treatment of cancer
BRPI0708299A2 (pt) 2006-02-27 2011-05-24 Univ Leland Stanford Junior composições e métodos para o transporte de moléculas com propriedades melhoradas de liberação através de barreiras biológicas
US20070203168A1 (en) 2006-02-28 2007-08-30 Zhao Jonathon Z Isomers of rapamycin and 42-Epi-rapamycin, methods of making and using the same
US7601852B2 (en) 2006-05-11 2009-10-13 Kosan Biosciences Incorporated Macrocyclic kinase inhibitors
US7888352B2 (en) 2006-12-07 2011-02-15 Piramed Limited Phosphoinositide 3-kinase inhibitor compounds and methods of use
AU2008275589B2 (en) 2007-07-12 2013-11-21 Gitr, Inc. Combination therapies employing GITR binding molecules
PE20140100A1 (es) 2007-09-12 2014-02-12 Genentech Inc Combinaciones de compuestos inhibidores de fosfoinositida 3-quinasa y agentes quimioterapeuticos
KR100945483B1 (ko) 2007-10-25 2010-03-05 이화여자대학교 산학협력단 ｐｉｋＤ 조절유전자의 발현벡터를 이용한 스트렙토미세스베네주엘라에（Ｓｔｒｅｐｔｏｍｙｃｅｓｖｅｎｅｚｕｅｌａｅ）에서폴리케타이드（ｐｏｌｙｋｅｔｉｄｅ）의 생산성 증가방법
CA2701292C (en) 2007-10-25 2015-03-24 Genentech, Inc. Process for making thienopyrimidine compounds
GB0805363D0 (en) 2008-03-20 2008-04-30 Sinvent As Novel NRPS-PKS gene cluster and its manipulation and utility
NZ590667A (en) 2008-07-02 2013-01-25 Emergent Product Dev Seattle Tgf-b antagonist multi-target binding proteins
JPWO2010030002A1 (ja) 2008-09-12 2012-02-02 国立大学法人三重大学 外来性ｇｉｔｒリガンド発現細胞
US20110171219A1 (en) 2008-09-19 2011-07-14 Fahar Merchant Treating cancer stem cells using targeted cargo proteins
WO2010034243A1 (en) 2008-09-24 2010-04-01 Shanghai Institute Of Organic Chemistry, Chinese Academy Of Sciences Novel gene cluster
JP5406943B2 (ja) 2009-01-30 2014-02-05 エナンタ ファーマシューティカルズ インコーポレイテッド Ｃ型肝炎感染を予防または治療するためのシクロスポリンアナログ
JP2012532929A (ja) 2009-07-13 2012-12-20 プレジデント アンド フェロウズ オブ ハーバード カレッジ 二機能性のステープリングされたポリペプチドおよびそれらの使用
EP2456777A2 (en) 2009-07-24 2012-05-30 Université Henri Poincaré - Nancy 1 Stambomycin and derivatives, their production and their use as drugs
KR101790802B1 (ko) 2009-09-03 2017-10-27 머크 샤프 앤드 돔 코포레이션 항-ｇｉｔｒ 항체
WO2011038049A1 (en) 2009-09-22 2011-03-31 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
JP5174971B2 (ja) 2009-10-22 2013-04-03 ペプチドリーム株式会社 ペプチド翻訳合成におけるｒａｐｉｄディスプレイ法
GB0919054D0 (en) 2009-10-30 2009-12-16 Isis Innovation Treatment of obesity
EA201492253A1 (ru) 2009-12-29 2015-06-30 Эмерджент Продакт Дивелопмент Сиэтл, Ллс Конструкторы, связывающиеся с ron, и способы их использования
CN103282362B (zh) 2010-11-30 2016-06-29 约翰·霍普金斯大学 杂交环状文库和其筛选
UY33775A (es) 2010-12-10 2012-07-31 Gilead Sciences Inc Inhibidores macrocíclicos de virus flaviviridae, composiciones farmacéuticas que los comprenden y sus usos
US9428845B1 (en) 2010-12-28 2016-08-30 Warp Drive Bio, Inc. Identifying new therapeutic agents
WO2012129344A1 (en) 2011-03-23 2012-09-27 Amgen Inc. Fused tricyclic dual inhibitors of cdk 4/6 and flt3
RU2598840C2 (ru) 2011-05-19 2016-09-27 Фундасион Сентро Насиональ Де Инвестигасионес Онколохикас Карлос Iii Новые соединения
WO2012174489A2 (en) 2011-06-15 2012-12-20 The Ohio State University Small molecule composite surfaces as inhibitors of protein-protein interactions
TW201311689A (zh) 2011-08-05 2013-03-16 必治妥美雅史谷比公司 作為因子ｘｉａ抑制劑之新穎巨環化合物
DE102011111991A1 (de) 2011-08-30 2013-02-28 Lead Discovery Center Gmbh Neue Cyclosporin-Derivate
US20130108641A1 (en) 2011-09-14 2013-05-02 Sanofi Anti-gitr antibodies
WO2013155223A1 (en) 2012-04-10 2013-10-17 The Regents Of The University Of California Compositions and methods for treating cancer
PL2859009T3 (pl) 2012-06-08 2018-03-30 Gilead Sciences, Inc. Makrocykliczne inhibitory wirusów flaviviridae
NZ703040A (en) 2012-06-08 2016-11-25 Gilead Sciences Inc Macrocyclic inhibitors of flaviviridae viruses
AR091279A1 (es) 2012-06-08 2015-01-21 Gilead Sciences Inc Inhibidores macrociclicos de virus flaviviridae
US10501412B2 (en) 2012-07-12 2019-12-10 Hangzhou Dac Biotech Co., Ltd. Conjugates of cell binding molecules with cytotoxic agents
JP6133431B2 (ja) 2012-11-24 2017-05-24 ハンジョウ ディーエーシー バイオテック シーオー．，エルティディ．Ｈａｎｇｚｈｏｕ Ｄａｃ Ｂｉｏｔｅｃｈ Ｃｏ．，Ｌｔｄ． 親水性連結体及び薬物分子と細胞結合分子との共役反応における親水性連結体の使用
US20150352131A1 (en) 2013-01-16 2015-12-10 Rhode Island Hospital Compositions and Methods for the Prevention and Treatment of Osteolysis and Osteoporosis
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
TW201524952A (zh) 2013-03-15 2015-07-01 Araxes Pharma Llc Ｋｒａｓ ｇ１２ｃ之共價抑制劑
CN110423212B (zh) 2013-04-26 2023-05-09 美国印第安纳大学研究和技术公司 Shp2的基于羟基吲哚羧酸的抑制剂
EP2806274A1 (en) 2013-05-24 2014-11-26 AIT Austrian Institute of Technology GmbH Lung cancer diagnostic method and means
WO2015054572A1 (en) 2013-10-10 2015-04-16 Araxes Pharma Llc Inhibitors of kras g12c
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
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
US10233431B2 (en) 2014-02-26 2019-03-19 The Regents Of The University Of California Producing 3-hydroxycarboxylic acid and ketone using polyketide synthases
EP3114483A1 (en) 2014-03-03 2017-01-11 Yissum Research and Development Company of the Hebrew University of Jerusalem Ltd. Method and device for detection of pseudomonas aeruginosa
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
AR102094A1 (es) 2014-09-25 2017-02-01 Araxes Pharma Llc Inhibidores de proteínas kras con una mutación g12c
TW201629069A (zh) 2015-01-09 2016-08-16 霍普驅動生物科技股份有限公司 參與協同結合之化合物及其用途
EP3247378B8 (en) 2015-01-09 2023-08-23 Revolution Medicines, Inc. Macrocyclic compounds that participate in cooperative binding and medical uses thereof
EP3277704A1 (en) 2015-03-31 2018-02-07 Allergan, Inc. Cyclosporins modified on the mebmt sidechain by heterocyclic rings
JP2018513853A (ja) 2015-04-10 2018-05-31 アラクセス ファーマ エルエルシー 置換キナゾリン化合物およびその使用方法
JP6789239B2 (ja) 2015-04-15 2020-11-25 アラクセス ファーマ エルエルシー Ｋｒａｓの縮合三環系インヒビターおよびその使用の方法
CA2986732A1 (en) 2015-05-22 2016-12-01 Allosta Pharmaceuticals Methods to prepare and employ binding site models for modulation of phosphatase activity and selectivity determination
WO2016196569A1 (en) 2015-06-01 2016-12-08 Indiana University Research & Technology Corporation Small molecule inhibitors of protein tyrosine phosphatases and uses thereof
JP6718889B2 (ja) 2015-06-19 2020-07-08 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するための化合物および組成物
EP3310771B1 (en) 2015-06-19 2020-07-22 Novartis AG Compounds and compositions for inhibiting the activity of shp2
ES2741746T3 (es) 2015-06-19 2020-02-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
CA2993013A1 (en) 2015-07-22 2017-01-26 Araxes Pharma Llc Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058805A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356353A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058768A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058915A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058807A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3355930A4 (en) 2015-10-01 2019-03-06 Warp Drive Bio, Inc. METHOD AND REAGENTS FOR THE ANALYSIS OF PROTEIN-PROTEIN INTERFACES
WO2017078499A2 (ko) 2015-11-06 2017-05-11 경북대학교 산학협력단 단백질 타이로신 탈인산화효소 억제제를 포함하는 신경염증성 질환의 예방 또는 치료용 조성물
WO2017079723A1 (en) 2015-11-07 2017-05-11 Board Of Regents, The University Of Texas System Targeting proteins for degradation
KR20180081596A (ko) 2015-11-16 2018-07-16 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
US9932288B2 (en) 2015-12-09 2018-04-03 West Virginia University Chemical compound for inhibition of SHP2 function and for use as an anti-cancer agent
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
WO2017156397A1 (en) 2016-03-11 2017-09-14 Board Of Regents, The University Of Texas Sysytem Heterocyclic inhibitors of ptpn11
WO2017172979A1 (en) 2016-03-30 2017-10-05 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
SG11201810171SA (en) 2016-05-18 2018-12-28 Mirati Therapeutics Inc Kras g12c inhibitors
AU2017274199B2 (en) 2016-05-31 2021-09-23 Board Of Regents, The University Of Texas System Heterocyclic inhibitors of PTPN11
EP4108659A1 (en) 2016-06-07 2022-12-28 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
CN109415360B (zh) 2016-06-14 2021-11-02 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
KR20230156174A (ko) 2016-07-12 2023-11-13 레볼루션 메디슨즈, 인크. 다른자리 입체성 shp2 억제제로서의 2,5-이치환 3-메틸 피라진 및 2,5,6-3치환 3-메틸 피라진
WO2018057884A1 (en) 2016-09-22 2018-03-29 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
CN110036010A (zh) 2016-09-29 2019-07-19 亚瑞克西斯制药公司 Kras g12c突变蛋白的抑制剂
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
TWI848901B (zh) 2016-10-24 2024-07-21 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
EP3532633A4 (en) 2016-10-28 2020-09-09 Ginkgo Bioworks Inc. COMPOSITIONS AND PROCESSES FOR THE PRODUCTION OF COMPOUNDS
CN110062626A (zh) 2016-11-18 2019-07-26 纽维制药有限公司 sanglifehrin大环类似物作为抗癌化合物的用途
JP7191828B2 (ja) 2016-12-15 2022-12-19 ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア がん治療のための組成物および方法
ES2894255T3 (es) 2016-12-22 2022-02-14 Amgen Inc Derivados de benzoisotiazol, isotiazolo[3,4-b]piridina, quinazolina, ftalazina, pirido[2,3-d]piridazina y derivados de pirido[2,3-d]pirimidina como inhibidores de KRAS G12C para tratar el cáncer de pulmón, pancreático o colorrectal
WO2018115380A1 (en) 2016-12-22 2018-06-28 Boehringer Ingelheim International Gmbh Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors
US10988766B2 (en) 2017-01-06 2021-04-27 Oregon Health & Science University Compositions and methods used in diagnosing and treating colorectal cancer
JP7503380B2 (ja) 2017-01-10 2024-06-20 ノバルティス アーゲー Ａｌｋ阻害剤およびｓｈｐ２阻害剤を含む組合せ医薬
AU2018210770B2 (en) 2017-01-23 2022-03-24 Revolution Medicines, Inc. Bicyclic compounds as allosteric SHP2 inhibitors
CN110431134A (zh) 2017-01-23 2019-11-08 锐新医药公司 作为变构shp2抑制剂的吡啶化合物
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
EP3573971A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
CN110382482A (zh) 2017-01-26 2019-10-25 亚瑞克西斯制药公司 稠合的杂-杂二环化合物及其使用方法
WO2018140598A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused n-heterocyclic compounds and methods of use thereof
EP3573970A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
WO2018140512A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
JOP20190186A1 (ar) 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
WO2018160731A1 (en) 2017-02-28 2018-09-07 Novartis Ag Shp inhibitor compositions and uses for chimeric antigen receptor therapy
CA3056970A1 (en) 2017-03-21 2018-09-27 Bayer Pharma Aktiengesellschaft 2-methyl-quinazolines
ES2989888T3 (es) 2017-03-23 2024-11-28 Jacobio Pharmaceuticals Co Ltd Derivados heterocíclicos novedosos útiles como inhibidores de SHP2
CA3058953A1 (en) 2017-04-05 2018-10-11 Revolution Medicines, Inc. Compounds that participate in cooperative binding and uses thereof
JP2020520988A (ja) 2017-04-05 2020-07-16 レボリューション メディシンズ インコーポレイテッドＲｅｖｏｌｕｔｉｏｎ Ｍｅｄｉｃｉｎｅｓ，Ｉｎｃ． タンパク質−タンパク質界面を分析するための方法及び試薬
IL303660A (en) 2017-05-02 2023-08-01 Revolution Medicines Inc Rapamycin analogs as mtor inhibitors
CA3061650A1 (en) 2017-05-11 2018-11-15 Astrazeneca Ab Heteroaryl compounds that inhibit g12c mutant ras proteins
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
US10745385B2 (en) 2017-05-25 2020-08-18 Araxes Pharma Llc Covalent inhibitors of KRAS
EP3630746A1 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Compounds and methods of use thereof for treatment of cancer
JP2020521740A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー 変異体ｋｒａｓ、ｈｒａｓまたはｎｒａｓの調節因子としてのキナゾリン誘導体
WO2018218133A1 (en) 2017-05-26 2018-11-29 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
CA3074690A1 (en) 2017-09-07 2019-03-14 Revolution Medicines, Inc. Shp2 inhibitor compositions and methods for treating cancer
EP4141005B1 (en) 2017-09-08 2024-04-03 Amgen Inc. Inhibitors of kras g12c and methods of using the same
MA50245A (fr) 2017-09-11 2020-07-22 Krouzon Pharmaceuticals Inc Inhibiteurs allostériques octahydrocyclopenta[c]pyrrole de shp2
IL274601B2 (en) 2017-11-15 2024-04-01 Mirati Therapeutics Inc Kras g12c inhibitors
US10597405B2 (en) 2017-12-08 2020-03-24 Astrazeneca Ab Chemical compounds
LT3728254T (lt) 2017-12-21 2023-05-10 Boehringer Ingelheim International Gmbh Naujieji benzilaminu pakeistieji piridopirimidinonai ir jų dariniai kaip sos1 inhibitoriai
US11426422B2 (en) 2018-01-30 2022-08-30 Research Development Foundation SHP2 inhibitors and methods of use thereof
TW201942115A (zh) 2018-02-01 2019-11-01 美商輝瑞股份有限公司 作為抗癌藥之經取代的喹唑啉和吡啶並嘧啶衍生物
TW201942116A (zh) 2018-02-09 2019-11-01 美商輝瑞股份有限公司 作為抗癌劑之四氫喹唑啉衍生物
WO2019158019A1 (zh) 2018-02-13 2019-08-22 上海青煜医药科技有限公司 嘧啶并环化合物及其制备方法和应用
US11044675B2 (en) 2018-02-13 2021-06-22 Idac Holdings, Inc. Methods, apparatuses and systems for adaptive uplink power control in a wireless network
US20200392161A1 (en) 2018-02-21 2020-12-17 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
WO2019167000A1 (en) 2018-03-02 2019-09-06 Otsuka Pharmaceutical Co., Ltd. Pharmaceutical compounds
WO2019183364A1 (en) 2018-03-21 2019-09-26 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof
CN112368272B (zh) 2018-03-21 2023-04-21 苏州浦合医药科技有限公司 Shp2抑制剂及其用途
JP7418395B2 (ja) 2018-03-21 2024-01-19 リレー セラピューティクス， インコーポレイテッド Ｓｈｐ２ホスファターゼ阻害剤およびこれらの使用方法
CA3097231A1 (en) 2018-04-18 2019-10-24 Bayer Pharma Aktiengesellschaft 2-methyl-aza-quinazolines
CN112368289B (zh) 2018-05-01 2024-02-20 锐新医药公司 作为mtor抑制剂的c26-连接的雷帕霉素类似物
HRP20230488T1 (hr) 2018-05-01 2023-08-04 Revolution Medicines, Inc. C40-, C28- I C-32-VEZANI ANALOZI RAPAMICINA KAO INHIBITORI mTOR
CA3099151A1 (en) 2018-05-02 2019-11-07 Navire Pharma, Inc. Substituted heterocyclic inhibitors of ptpn11
CA3098574A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
AU2019262599B2 (en) 2018-05-04 2023-10-12 Amgen Inc. KRAS G12C inhibitors and methods of using the same
US11932633B2 (en) 2018-05-07 2024-03-19 Mirati Therapeutics, Inc. KRas G12C inhibitors
TW202012415A (zh) 2018-05-08 2020-04-01 瑞典商阿斯特捷利康公司 化學化合物
JP7361720B2 (ja) 2018-05-10 2023-10-16 アムジエン・インコーポレーテツド がんの治療のためのｋｒａｓ ｇ１２ｃ阻害剤
MA52765A (fr) 2018-06-01 2021-04-14 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
US20210230300A1 (en) 2018-06-04 2021-07-29 Bayer Aktiengesellschaft Inhibitors of shp2
JP7357644B2 (ja) 2018-06-11 2023-10-06 アムジエン・インコーポレーテツド がんを処置するためのｋｒａｓ ｇ１２ｃ阻害剤
JP7369719B2 (ja) 2018-06-12 2023-10-26 アムジエン・インコーポレーテツド ＫＲａｓ Ｇ１２Ｃ阻害剤及びそれを使用する方法
MA53395A (fr) 2018-07-24 2021-06-02 Otsuka Pharma Co Ltd Composés hétérobicycliques pour inhiber l'activité de shp2
CA3107168A1 (en) 2018-08-01 2020-02-06 Araxes Pharma Llc Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer
WO2020033286A1 (en) 2018-08-06 2020-02-13 Purdue Research Foundation Novel sesquiterpenoid analogs
SG11202100199UA (en) 2018-08-10 2021-02-25 Navire Pharma Inc 6-(4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-3-(2,3-dichlorophenyl)-2-methylpyrimidin-4(3h)-one derivatives and related compounds as ptpn11 (shp2) inhibitors for treating cancer
KR102495687B1 (ko) 2018-08-16 2023-02-07 에프. 호프만-라 로슈 아게 융합 고리 화합물
WO2020047192A1 (en) 2018-08-31 2020-03-05 Mirati Therapeutics, Inc. Kras g12c inhibitors
MX2021003158A (es) 2018-09-18 2021-07-16 Nikang Therapeutics Inc Derivados de anillo tricíclico condensado como inhibidores de la fosfatasa de homología a src 2.
CN112839935A (zh) 2018-09-26 2021-05-25 北京加科思新药研发有限公司 可用作shp2抑制剂的新型杂环衍生物
US12138262B2 (en) 2018-09-29 2024-11-12 Novartis Ag Process of manufacture of a compound for inhibiting the activity of SHP2, as well as products resulting from acid addition
CA3112322A1 (en) 2018-09-29 2020-04-02 Novartis Ag Manufacture of compounds and compositions for inhibiting the activity of shp2
EP3860717A1 (en) 2018-10-03 2021-08-11 Gilead Sciences, Inc. Imidozopyrimidine derivatives
CN111295384B (zh) 2018-10-10 2022-08-12 江苏豪森药业集团有限公司 双环类衍生物抑制剂、其制备方法和应用
TW202028183A (zh) 2018-10-10 2020-08-01 大陸商江蘇豪森藥業集團有限公司 含氮雜芳類衍生物調節劑、其製備方法和應用
CR20210189A (es) 2018-10-17 2021-09-14 Array Biopharma Inc Inhibidores de la proteina tirosina fosfatasa
CN117143079A (zh) 2018-11-06 2023-12-01 上海奕拓医药科技有限责任公司 一种螺芳环化合物及其应用
US20220127271A1 (en) 2018-11-07 2022-04-28 Shanghai Ringene Biopharma Co., Ltd. Nitrogen-containing fused heterocyclic shp2 inhibitor compound, preparation method, and use
MX2021005700A (es) 2018-11-19 2021-07-07 Amgen Inc Inhibidores de kras g12c y metodos de uso de los mismos.
EP3883574A1 (en) 2018-11-23 2021-09-29 Institut National de la Santé et de la Recherche Médicale (INSERM) Use of shp2 inhibitors for the treatment of insulin resistance
CA3120791A1 (en) 2018-11-30 2020-06-04 Tuojie Biotech (Shanghai) Co., Ltd. Pyrimidine and five-membered nitrogen heterocycle derivative, preparation method therefor, and medical uses thereof
WO2020132597A1 (en) 2018-12-21 2020-06-25 Revolution Medicines, Inc. Compounds that participate in cooperative binding and uses thereof
WO2020146470A1 (en) 2019-01-08 2020-07-16 Yale University Phosphatase Binding Compounds and Methods of Using Same
JP7592601B2 (ja) 2019-01-10 2024-12-02 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｃ阻害剤
WO2020156243A1 (zh) 2019-01-31 2020-08-06 贝达药业股份有限公司 Shp2抑制剂及其应用
WO2020156242A1 (zh) 2019-01-31 2020-08-06 贝达药业股份有限公司 Shp2抑制剂及其应用
WO2020165734A1 (en) 2019-02-12 2020-08-20 Novartis Ag Pharmaceutical combination comprising tno155 and ribociclib
JP7572958B2 (ja) 2019-02-12 2024-10-24 ノバルティス アーゲー Ｔｎｏ１５５及びｋｒａｓｇ１２ｃ阻害剤を含む医薬組合せ
AU2020222295B2 (en) 2019-02-12 2023-04-06 Novartis Ag Pharmaceutical combination comprising TNO155 and a PD-1 inhibitor
EP3931188B1 (en) 2019-02-26 2023-08-30 Boehringer Ingelheim International GmbH New isoindolinone substituted indoles and derivatives as ras inhibitors
CN113727758A (zh) 2019-03-01 2021-11-30 锐新医药公司 双环杂环基化合物及其用途
CN113767100A (zh) 2019-03-01 2021-12-07 锐新医药公司 双环杂芳基化合物及其用途
CN111647000B (zh) 2019-03-04 2021-10-12 勤浩医药（苏州）有限公司 吡嗪类衍生物及其在抑制shp2中的应用
WO2020181283A1 (en) 2019-03-07 2020-09-10 Merck Patent Gmbh Carboxamide-pyrimidine derivatives as shp2 antagonists
MX2021012122A (es) 2019-04-02 2021-11-03 Array Biopharma Inc Inhibidores de la proteina tirosina fosfatasa.
AU2020271838A1 (en) 2019-04-08 2021-08-19 Merck Patent Gmbh Pyrimidinone derivatives as SHP2 antagonists
EP3984999A4 (en) 2019-06-14 2023-11-22 Beijing Shenogen Pharma Group Ltd. ALLOSTERIC INHIBITOR OF SHP2 PHOSPHATASE
WO2020259679A1 (zh) 2019-06-28 2020-12-30 上海拓界生物医药科技有限公司 嘧啶并五元氮杂环类衍生物、其制备方法及其在医药上的应用
CN112300160A (zh) 2019-08-01 2021-02-02 上海奕拓医药科技有限责任公司 一种螺芳环化合物、其制备及应用
EP3772513A1 (en) 2019-08-09 2021-02-10 C.N.C.C.S. S.c.a.r.l. Collezione Nazionale Dei Composti Chimici e Centro Screening Shp2 inhibitors
GB201911928D0 (en) 2019-08-20 2019-10-02 Otsuka Pharma Co Ltd Pharmaceutical compounds
CN114127053B (zh) 2019-09-06 2023-06-13 四川科伦博泰生物医药股份有限公司 一种取代吡嗪化合物、其制备方法和用途
WO2021061515A1 (en) 2019-09-23 2021-04-01 Synblia Therapeutics, Inc. Shp2 inhibitors and uses thereof
CA3154862A1 (en) 2019-09-24 2021-04-01 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of making and using the same
CN112724145A (zh) 2019-10-14 2021-04-30 杭州雷索药业有限公司 用于抑制shp2活性的吡嗪衍生物
CN115315424A (zh) 2019-10-15 2022-11-08 拜耳公司 2-甲基-氮杂-喹唑啉
CN114786777A (zh) 2019-11-04 2022-07-22 锐新医药公司 Ras抑制剂
JP2022553857A (ja) 2019-11-04 2022-12-26 レボリューション メディシンズ インコーポレイテッド Ｒａｓ阻害剤
KR20220109407A (ko) * 2019-11-04 2022-08-04 레볼루션 메디슨즈, 인크. Ras 억제제
TW202120488A (zh) 2019-11-08 2021-06-01 大陸商南京聖和藥業股份有限公司 作為shp2抑制劑的化合物及其應用
BR112022008858A2 (pt) 2019-11-08 2022-09-06 Revolution Medicines Inc Composto, composição farmacêutica e métodos para inibir sos1 em um sujeito, para inibir a interação de sos1 e uma proteína, para tratar ou prevenir uma doença e para tratar ou prevenir câncer
SMT202400273T1 (it) 2019-11-29 2024-09-16 Lupin Ltd Composti triciclici sostituiti
EP4069301A1 (en) 2019-12-04 2022-10-12 Bayer Aktiengesellschaft Inhibitors of shp2
CN114829362A (zh) 2019-12-10 2022-07-29 成都倍特药业股份有限公司 一种可用作shp2抑制剂的含氮杂原子的六元并五元芳环衍生物
WO2021119525A1 (en) 2019-12-11 2021-06-17 Tiaki Therapeutics Inc. Shp1 and shp2 inhibitors and their methods of use
US20230028414A1 (en) 2019-12-16 2023-01-26 Amgen Inc. Dosing regimen of kras g12c inhibitor
US20230083431A1 (en) 2019-12-18 2023-03-16 Merck Sharp & Dohme Llc Macrocyclic peptides as potent inhibitors of k-ras g12d mutant
WO2021120045A1 (en) 2019-12-18 2021-06-24 InventisBio Co., Ltd. Heterocyclic compounds, preparation methods and uses thereof
CR20220351A (es) 2019-12-19 2022-10-31 Jacobio Pharmaceuticals Co Ltd Inhibidores de proteínas kras mutantes
WO2021121397A1 (zh) 2019-12-19 2021-06-24 首药控股(北京)股份有限公司 取代的炔基杂环化合物
WO2021121371A1 (zh) 2019-12-19 2021-06-24 贝达药业股份有限公司 Kras g12c抑制剂及其在医药上的应用
WO2021120890A1 (en) 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
AU2020408562A1 (en) 2019-12-20 2022-06-23 Erasca, Inc. Tricyclic pyridones and pyrimidones
IL294048A (en) 2019-12-20 2022-08-01 Mirati Therapeutics Inc Sos1 inhibitors
CA3165864A1 (en) 2019-12-27 2021-07-01 Lupin Limited Substituted tricyclic compounds
CN113045565A (zh) 2019-12-27 2021-06-29 微境生物医药科技(上海)有限公司 新型K-Ras G12C抑制剂
US20230002382A1 (en) 2019-12-27 2023-01-05 Wigen Biomedicine Technology (shanghai) Co., Ltd. Spiro ring-containing quinazoline compounds
WO2021139678A1 (zh) 2020-01-07 2021-07-15 广州百霆医药科技有限公司 吡啶并嘧啶类kras g12c突变蛋白抑制剂
TWI770760B (zh) 2020-01-08 2022-07-11 大陸商蘇州亞盛藥業有限公司 螺環四氫喹唑啉
AU2021206240A1 (en) 2020-01-10 2022-08-25 Incyte Corporation Tricyclic compounds as inhibitors of KRAS
WO2021143693A1 (zh) 2020-01-13 2021-07-22 苏州泽璟生物制药股份有限公司 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用
WO2021143823A1 (zh) 2020-01-16 2021-07-22 浙江海正药业股份有限公司 吡啶或嘧啶类衍生物及其制备方法和用途
CN114867720B (zh) 2020-01-16 2024-10-22 浙江海正药业股份有限公司 杂芳基类衍生物及其制备方法和用途
CN113135910A (zh) 2020-01-19 2021-07-20 北京诺诚健华医药科技有限公司 嘧啶-4(3h)-酮类杂环化合物、其制备方法及其在医药学上的应用
US11530218B2 (en) 2020-01-20 2022-12-20 Incyte Corporation Spiro compounds as inhibitors of KRAS
CN115003668A (zh) 2020-01-21 2022-09-02 南京明德新药研发有限公司 作为kras抑制剂的大环类化合物
WO2021147879A1 (zh) 2020-01-21 2021-07-29 贝达药业股份有限公司 Shp2抑制剂及其应用
CN115210232B (zh) 2020-01-22 2024-03-01 上海齐鲁制药研究中心有限公司 吡唑并杂芳环类化合物及其应用
US20230146795A1 (en) 2020-01-24 2023-05-11 Taiho Pharmaceutical Co., Ltd. Enhancement of anti-tumor activity of shp2 inhibitor pyrimidinone in combination with novel cancer medicines in cancers
GB202001344D0 (en) 2020-01-31 2020-03-18 Redx Pharma Plc Ras Inhibitors
CN112159405B (zh) 2020-02-04 2021-09-14 广州必贝特医药技术有限公司 吡啶并嘧啶酮类化合物及其应用
US20230346790A1 (en) 2020-02-06 2023-11-02 Wellmarker Bio Co., Ltd. Pharmaceutical composition for prevention or treatment of cancers associated with kras mutation
EP4077328A4 (en) 2020-02-20 2023-11-29 Beta Pharma, Inc. PYRIDOPYRIMIDE DERIVATIVES AS KRAS INHIBITORS
WO2021169990A1 (zh) 2020-02-24 2021-09-02 泰励生物科技（上海）有限公司 用于癌症治疗的kras抑制剂
US20230101312A1 (en) 2020-02-24 2023-03-30 Mirati Therapeutics, Inc. Sos1 inhibitors
WO2021169963A1 (zh) 2020-02-24 2021-09-02 上海喆邺生物科技有限公司 芳香类化合物及其在制备抗肿瘤药物中的应用
WO2021173923A1 (en) 2020-02-28 2021-09-02 Erasca, Inc. Pyrrolidine-fused heterocycles
WO2022060583A1 (en) 2020-09-03 2022-03-24 Revolution Medicines, Inc. Use of sos1 inhibitors to treat malignancies with shp2 mutations
CN117683049A (zh) 2020-09-15 2024-03-12 锐新医药公司 作为ras抑制剂以治疗癌症的吲哚衍生物

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