PE20241476A1 - Inhibidores de la ras - Google Patents

Inhibidores de la ras

Info

Publication number
PE20241476A1
PE20241476A1 PE2024000685A PE2024000685A PE20241476A1 PE 20241476 A1 PE20241476 A1 PE 20241476A1 PE 2024000685 A PE2024000685 A PE 2024000685A PE 2024000685 A PE2024000685 A PE 2024000685A PE 20241476 A1 PE20241476 A1 PE 20241476A1
Authority
PE
Peru
Prior art keywords
optionally substituted
membered
cancer
compounds
heteroalkyl
Prior art date
Application number
PE2024000685A
Other languages
English (en)
Spanish (es)
Inventor
G Leslie Burnett
James Cregg
Anne V Edwards
Adrian L Gill
John E Knox
Elena S Koltun
Yang Liu
Christopher Semko
Andreas Buckl
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 PE20241476A1 publication Critical patent/PE20241476A1/es

Links

Classifications

    • 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
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • 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
    • 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
    • C07D498/16—Peri-condensed systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Saccharide Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Steroid Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
PE2024000685A 2021-10-08 2022-10-07 Inhibidores de la ras PE20241476A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202163254013P 2021-10-08 2021-10-08
PCT/US2022/077784 WO2023060253A1 (en) 2021-10-08 2022-10-07 Ras inhibitors

Publications (1)

Publication Number Publication Date
PE20241476A1 true PE20241476A1 (es) 2024-07-17

Family

ID=84044950

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2024000685A PE20241476A1 (es) 2021-10-08 2022-10-07 Inhibidores de la ras

Country Status (17)

Country Link
US (2) US12202845B2 (enExample)
EP (1) EP4413008A1 (enExample)
JP (2) JP7789906B2 (enExample)
KR (1) KR20240074849A (enExample)
CN (2) CN118679169A (enExample)
AR (1) AR127308A1 (enExample)
AU (2) AU2022360536B2 (enExample)
CA (1) CA3234100A1 (enExample)
CL (2) CL2024001023A1 (enExample)
CO (1) CO2024005879A2 (enExample)
CR (1) CR20240156A (enExample)
IL (1) IL311840A (enExample)
MX (1) MX2024004247A (enExample)
PE (1) PE20241476A1 (enExample)
TW (1) TW202315616A (enExample)
WO (1) WO2023060253A1 (enExample)
ZA (1) ZA202402878B (enExample)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202132316A (zh) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ｒａｓ抑制劑
EP4067343A4 (en) 2019-11-29 2024-01-03 Taiho Pharmaceutical Co., Ltd. NEW PHENOLIC COMPOUND OR SALT THEREOF
CA3194067A1 (en) 2020-09-15 2022-03-24 Revolution Medicines, Inc. Ras inhibitors
KR20240017811A (ko) * 2021-05-05 2024-02-08 레볼루션 메디슨즈, 인크. 암의 치료를 위한 ras 억제제
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
KR20250085767A (ko) 2022-09-29 2025-06-12 광조우 조요 파마테크 컴퍼니 리미티드 거대고리 유도체 및 이의 적용
CN118047797A (zh) * 2022-11-16 2024-05-17 杭州阿诺生物医药科技有限公司 一种pan-KRAS抑制剂化合物
CN120813588A (zh) 2023-02-14 2025-10-17 豪夫迈·罗氏有限公司 用于治疗癌症的三环化合物
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
CR20250420A (es) 2023-04-07 2025-11-20 Revolution Medicines Inc Inhibidores macrocíclicos de ras
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ｒａｓ相關疾病或病症之組合療法
CN116376844B (zh) * 2023-05-31 2023-08-11 四川大学华西医院 包含shp2 sh2结构域的靶向her2阳性肿瘤的car-t及制备方法和应用
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
AU2024354932A1 (en) 2023-10-03 2026-04-09 Revolution Medicines, Inc. Synthesis of ras inhibitors
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
AU2024361909A1 (en) 2023-10-20 2026-03-26 Merck Sharp & Dohme Llc Small molecule inhibitors of kras proteins
WO2025093625A1 (en) 2023-11-01 2025-05-08 F. Hoffmann-La Roche Ag Macrocycle compounds for the treatment of cancer
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025217307A1 (en) 2024-04-09 2025-10-16 Revolution Medicines, Inc. Methods for predicting response to a ras(on) inhibitor and combination therapies
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026010866A1 (en) * 2024-07-01 2026-01-08 Apertor Pharmaceuticals, Inc. Hetero-bifunctional molecules
WO2026015740A1 (en) * 2024-07-11 2026-01-15 Treeline Biosciences, Inc. Macrocyclic ras inhibitors
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026021499A1 (zh) * 2024-07-24 2026-01-29 苏州泽璟生物制药股份有限公司 卤代亚烷基取代环烷基或杂环基类抑制剂及其制备方法和应用
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

Family Cites Families (448)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0290762B1 (en) 1984-10-04 1993-05-12 Sandoz Ag Cyclosporins
EP0194972B1 (en) 1985-03-11 1992-07-29 Sandoz Ag Novel cyclosporins
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
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
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
US6905680B2 (en) 1988-11-23 2005-06-14 Genetics Institute, Inc. Methods of treating HIV infected subjects
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
CA2014590C (en) 1989-04-15 1999-12-14 Mitsuo Masaki Novel peptides, and antidementia agents containing the same
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
SG64322A1 (en) 1991-05-10 1999-04-27 Rhone Poulenc Rorer Int Bis mono and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
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
GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
ATE138807T1 (de) 1992-03-27 1996-06-15 American Home Prod 29-demethoxyrapamycin zur induktion der immunosuppression
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
ZA935112B (en) 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
ZA935111B (en) 1992-07-17 1994-02-04 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
WO1994011384A1 (en) 1992-11-13 1994-05-26 Immunex Corporation Novel cytokine designated elk ligand
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
CA2171629A1 (en) 1993-09-20 1995-03-30 Chaitan Khosla Recombinant production of novel polyketides
WO1995009847A1 (en) 1993-10-01 1995-04-13 Ciba-Geigy Ag 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
CA2175215C (en) 1993-11-19 2008-06-03 Yat Sun Or Semisynthetic analogs of rapamycin (macrolides) being immunomodulators
SK78196A3 (en) 1993-12-17 1997-02-05 Sandoz Ag Rapamycin demethoxy-derivatives, preparation method thereof and pharmaceutical agent containing them
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
WO1995024190A2 (en) 1994-03-07 1995-09-14 Sugen, Inc. 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
EP0756627A1 (en) 1994-04-15 1997-02-05 Amgen Inc. Hek5, hek7, hek8, hek11, new eph-like receptor protein tyrosine kinases
DE59500788D1 (de) 1994-05-03 1997-11-20 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
DE69536015D1 (de) 1995-03-30 2009-12-10 Pfizer Prod Inc Chinazolinone Derivate
CA2214086C (en) 1995-04-03 2008-07-29 Novartis Ag Pyrazole derivatives 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
US5650415A (en) 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
US5985890A (en) 1995-06-09 1999-11-16 Novartis Ag Rapamycin derivatives
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
AU1441497A (en) 1996-01-23 1997-08-20 Novartis Ag Pyrrolopyrimidines and processes for their preparation
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
GB9603097D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline compounds
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
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
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
WO1997034895A1 (de) 1996-03-15 1997-09-25 Novartis Ag NEUE N-7 HETEROCYCLYL-PYRROLO[2,3-d]PYRIMIDINE UND IHRE VERWENDUNG
EA001595B1 (ru) 1996-04-12 2001-06-25 Варнер-Ламберт Компани Необратимые ингибиторы тирозинкиназ
GB9607729D0 (en) 1996-04-13 1996-06-19 Zeneca Ltd Quinazoline derivatives
CA2258548C (en) 1996-06-24 2005-07-26 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
ES2244001T3 (es) 1996-07-05 2005-12-01 Biotica Technology Limited Eritromicinas y procedimiento para su preparacion.
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
AR007857A1 (es) 1996-07-13 1999-11-24 Glaxo Group Ltd Compuestos heterociclicos fusionados como inhibidores de proteina tirosina quinasa, sus metodos de preparacion, intermediarios uso en medicina ycomposiciones farmaceuticas que los contienen.
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
EA199900021A1 (ru) 1996-07-13 1999-08-26 Глаксо, Груп Лимитед Бициклические гетероароматические соединения в качестве ингибиторов протеинтирозинкиназы
KR20000067904A (ko) 1996-07-18 2000-11-25 디. 제이. 우드, 스피겔 알렌 제이 매트릭스 메탈로프로테아제의 포스피네이트계 억제제
ES2308787T3 (es) 1996-08-16 2008-12-01 Schering Corporation Antigenos de superficie de celular de mamiferos; reactivos relacionados.
US6111090A (en) 1996-08-16 2000-08-29 Schering Corporation Mammalian cell surface antigens; related reagents
KR20000068248A (ko) 1996-08-23 2000-11-25 디. 제이. 우드, 스피겔 알렌 제이 아릴설포닐아미노 하이드록삼산 유도체
WO1998007726A1 (en) 1996-08-23 1998-02-26 Novartis Ag Substituted pyrrolopyrimidines and processes for their preparation
SE9603465D0 (sv) 1996-09-23 1996-09-23 Astra Ab New compounds
AU4779897A (en) 1996-10-02 1998-04-24 Novartis Ag Fused pyrazole derivatives and processes for their preparation
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
US6251911B1 (en) 1996-10-02 2001-06-26 Novartis Ag Pyrimidine derivatives and processes for the preparation thereof
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
JP3338064B2 (ja) 1997-01-06 2002-10-28 ファイザー・インク 環状スルホン誘導体
NZ336840A (en) 1997-02-03 2001-01-26 Pfizer Prod Inc Arylsulfonylamino hydroxamic acid derivatives useful in the treatment of tumor necrosis factor and matrix metalloproteinase mediated diseases
WO1998033798A2 (en) 1997-02-05 1998-08-06 Warner Lambert Company Pyrido[2,3-d]pyrimidines and 4-amino-pyrimidines as inhibitors of cell proliferation
JP2000507975A (ja) 1997-02-07 2000-06-27 ファイザー・インク Ｎ−ヒドロキシ−β−スルホニルプロピオンアミド誘導体類及びそれらのマトリックスメタロプロテイナーゼ阻害薬としての使用
EP0960098A1 (en) 1997-02-11 1999-12-01 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives
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
AU8689298A (en) 1997-08-05 1999-03-01 Sugen, Inc. Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors
CA2299355C (en) 1997-08-08 2005-09-27 Pfizer Products Inc. Aryloxyarylsulfonylamino hydroxamic acid derivatives
JP2001520039A (ja) 1997-10-21 2001-10-30 ヒューマン ジノーム サイエンシーズ， インコーポレイテッド ヒト腫瘍壊死因子レセプター様タンパク質、ｔｒ１１，ｔｒ１１ｓｖ１および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
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
GB9800575D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
AU2591599A (en) 1998-02-09 1999-08-23 Genentech Inc. Novel tumor necrosis factor receptor homolog and nucleic acids encoding the same
CA2322311C (en) 1998-03-04 2009-10-13 Bristol-Myers Squibb Company Heterocyclo-substituted imidazopyrazine protein tyrosine kinase inhibitors
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
AU4093799A (en) 1998-05-22 1999-12-13 Board Of Trustees Of The Leland Stanford Junior University Bifunctional molecules and therapies based thereon
SK287132B6 (sk) 1998-05-29 2009-12-07 Sugen, Inc. Farmaceutická kompozícia obsahujúca pyrolom substituovaný 2-indolinón, súprava obsahujúca uvedenú kompozíciu a použitie pyrolom substituovaného 2-indolinónu
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
CA2336848A1 (en) 1998-07-10 2000-01-20 Merck & Co., Inc. Novel angiogenesis inhibitors
CA2341409A1 (en) 1998-08-31 2000-03-09 Merck And Co., Inc. Novel angiogenesis inhibitors
MXPA01003376A (es) 1998-10-02 2002-11-07 Kosan Biosciences Inc Enzimas policetido sintetasa y construcciones de acido desoxirribonucleico recombinante para las mismas.
US6686454B1 (en) 1998-10-09 2004-02-03 Isotechnika, Inc. Antibodies to specific regions of cyclosporine related compounds
EP1004578B1 (en) 1998-11-05 2004-02-25 Pfizer Products Inc. 5-oxo-pyrrolidine-2-carboxylic acid hydroxamide derivatives
US6753173B1 (en) 1999-02-09 2004-06-22 Board Of Trustees Of The Leland Stanford Junior University Methods to mediate polyketide synthase module effectiveness
CN1660840A (zh) 1999-03-30 2005-08-31 诺瓦提斯公司 治疗炎性疾病的酞嗪衍生物
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
ATE324444T1 (de) 1999-06-07 2006-05-15 Immunex Corp Tek-antagonisten
WO2001003720A2 (en) 1999-07-12 2001-01-18 Genentech, Inc. Promotion or inhibition of angiogenesis and cardiovascularization by tumor necrosis factor ligand/receptor homologs
ATE264863T1 (de) 1999-08-24 2004-05-15 Ariad Gene Therapeutics Inc 28-epirapaloge
KR100881105B1 (ko) 1999-11-05 2009-02-02 아스트라제네카 아베 Ｖｅｇｆ 억제제로서의 퀴나졸린 유도체
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
EP1230353A4 (en) 1999-11-19 2002-11-06 Univ Leland Stanford Junior BIFUNCTIONAL MOLECULES AND THEIR USE IN THE DESTRUCTION OF PROTEIN-PROTEIN INTERACTIONS
WO2001037820A2 (en) 1999-11-24 2001-05-31 Sugen, Inc. Ionizable indolinone derivatives and their use as ptk ligands
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
US7572631B2 (en) 2000-02-24 2009-08-11 Invitrogen Corporation Activation and expansion of T cells
US6867041B2 (en) 2000-02-24 2005-03-15 Xcyte Therapies, Inc. Simultaneous stimulation and concentration of cells
US6797514B2 (en) 2000-02-24 2004-09-28 Xcyte Therapies, Inc. Simultaneous stimulation and concentration of cells
KR20030032922A (ko) 2000-02-24 2003-04-26 싸이트 테라피스 인코포레이티드 세포의 동시 자극 및 농축
NZ521437A (en) 2000-02-25 2004-04-30 Immunex Corp Integrin antagonists suitable as inhibitors of angiogenesis
KR20020025959A (ko) 2000-05-23 2002-04-04 버텍스 파마슈티칼스 인코포레이티드 카스파제 억제제 및 이의 용도
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
BR0116452A (pt) 2000-12-21 2003-09-30 Glaxo Group Ltd Composto, composição farmacêutica, uso de um composto
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
US20020147198A1 (en) 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine derivatives and methods of use
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7105682B2 (en) 2001-01-12 2006-09-12 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
US7618632B2 (en) 2003-05-23 2009-11-17 Wyeth Method of treating or ameliorating an immune cell associated pathology using GITR ligand antibodies
US20060173033A1 (en) 2003-07-08 2006-08-03 Michaela Kneissel Use of rapamycin and rapamycin derivatives for the treatment of bone loss
WO2005007190A1 (en) 2003-07-11 2005-01-27 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
PT1660458E (pt) 2003-08-15 2012-04-27 Novartis Ag 2,4-pirimidinodiaminas úteis no tratamento de doenças neoplásicas, desordens inflamatórias e do sistema imunitário
WO2005055808A2 (en) 2003-12-02 2005-06-23 Genzyme Corporation Compositions and methods to diagnose and treat lung cancer
GB0409799D0 (en) 2004-04-30 2004-06-09 Isis Innovation Method of generating improved immune response
US20060002932A1 (en) 2004-06-04 2006-01-05 Duke University Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity
DE602005020465D1 (de) 2004-08-26 2010-05-20 Pfizer Enantiomerenreine aminoheteroaryl-verbindungen als proteinkinasehemmer
EP1799699A1 (en) 2004-10-13 2007-06-27 Wyeth Analogs of 17-hydroxywortmannin as pi3k inhibitors
PT2343320T (pt) 2005-03-25 2018-01-23 Gitr Inc Anticorpos anti-gitr e as suas utilizações
DK2439273T3 (da) 2005-05-09 2019-06-03 Ono Pharmaceutical Co Humane monoklonale antistoffer til programmeret død-1(pd-1) og fremgangsmåder til behandling af cancer ved anvendelse af anti-pd-1- antistoffer alene eller i kombination med andre immunterapeutika
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
KR20080040007A (ko) 2005-09-20 2008-05-07 화이자 프로덕츠 인크. 티로신 키나제 억제제를 이용한 치료의 투여형 및 방법
WO2007133822A1 (en) 2006-01-19 2007-11-22 Genzyme Corporation Gitr antibodies for the treatment of cancer
CA2643826A1 (en) 2006-02-27 2008-06-12 Paul A. Wender Compositions and methods for transport of molecules with enhanced release properties across biological barriers
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
MX2009005950A (es) 2006-12-07 2009-10-12 Genentech Inc Compuestos inhibidores de fosfoinositido 3-quinasas y metodos de uso.
US8591886B2 (en) 2007-07-12 2013-11-26 Gitr, Inc. Combination therapies employing GITR binding molecules
EP2205242B1 (en) 2007-09-12 2015-04-15 Genentech, Inc. Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
JP5348725B2 (ja) 2007-10-25 2013-11-20 ジェネンテック， インコーポレイテッド チエノピリミジン化合物の製造方法
KR100945483B1 (ko) 2007-10-25 2010-03-05 이화여자대학교 산학협력단 ｐｉｋＤ 조절유전자의 발현벡터를 이용한 스트렙토미세스베네주엘라에（Ｓｔｒｅｐｔｏｍｙｃｅｓｖｅｎｅｚｕｅｌａｅ）에서폴리케타이드（ｐｏｌｙｋｅｔｉｄｅ）의 생산성 증가방법
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
CN102149820B (zh) 2008-09-12 2014-07-23 国立大学法人三重大学 能够表达外源gitr配体的细胞
WO2010031185A1 (en) 2008-09-19 2010-03-25 Protox Therapeutics Inc. Treating cancer stem cells using targeted cargo proteins
CN102224242B (zh) 2008-09-24 2014-09-24 中国科学院上海有机化学研究所 新基因簇
KR20110111321A (ko) 2009-01-30 2011-10-10 이난타 파마슈티칼스, 인코포레이티드 Ｃ형 간염을 예방하거나 치료하기 위한 사이클로스포린 유사체
DK3000467T3 (da) 2009-04-06 2023-03-27 Wyeth Llc Behandling med neratinib mod brystkræft
AU2010273220B2 (en) 2009-07-13 2015-10-15 President And Fellows Of Harvard College Bifunctional stapled polypeptides and uses thereof
US8664186B2 (en) 2009-07-24 2014-03-04 Universite De Lorraine Stambomycin and derivatives, their production and their uses as drugs
KR101790802B1 (ko) 2009-09-03 2017-10-27 머크 샤프 앤드 돔 코포레이션 항-ｇｉｔｒ 항체
CN102712675A (zh) 2009-09-22 2012-10-03 爱勒让治疗公司 拟肽大环化合物
WO2011049157A1 (ja) 2009-10-22 2011-04-28 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
CA2785907A1 (en) 2009-12-29 2011-07-28 Emergent Product Development Seattle, Llc Ron binding constructs and methods of use thereof
US9119853B2 (en) 2010-02-09 2015-09-01 Neurovive Pharmaceutical Ab Sanglifehrin based compounds
US9250237B2 (en) 2010-11-30 2016-02-02 The Johns Hopkins University Hybrid cyclic libraries and screens thereof
PY1153144A (es) 2010-12-10 2015-01-01 Gilead Sciences Inc Inhibidores macrocíclicos de virus flaviviridae
US9428845B1 (en) 2010-12-28 2016-08-30 Warp Drive Bio, Inc. Identifying new therapeutic agents
EP2937349B1 (en) 2011-03-23 2016-12-28 Amgen Inc. Fused tricyclic dual inhibitors of cdk 4/6 and flt3
JO3063B1 (ar) 2011-03-29 2017-03-15 Neurovive Pharmaceutical Ab مركب مبتكر وطرق لانتاجه
PL2710018T3 (pl) 2011-05-19 2022-04-04 Fundación Del Sector Público Estatal Centro Nacional De Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Związki makrocykliczne jako inhibitory kinaz białkowych
WO2012174489A2 (en) 2011-06-15 2012-12-20 The Ohio State University Small molecule composite surfaces as inhibitors of protein-protein interactions
WO2013001310A1 (en) 2011-06-30 2013-01-03 Centro Nacional De Investigaciones Oncológicas (Cnio) Macrocyclic compounds and their use as cdk8 inhibitors
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
WO2013039954A1 (en) 2011-09-14 2013-03-21 Sanofi Anti-gitr antibodies
EP2836482B1 (en) 2012-04-10 2019-12-25 The Regents of The University of California Compositions and methods for treating cancer
BR112014030649A2 (pt) 2012-06-08 2017-06-27 Gilead Sciences Inc inibidores macrocíclicos da flaviviridae vírus
PT2861604T (pt) 2012-06-08 2017-05-05 Gilead Sciences Inc Inibidores macrocíclicos de vírus flaviridae
AR091279A1 (es) 2012-06-08 2015-01-21 Gilead Sciences Inc Inhibidores macrociclicos de virus flaviviridae
ES2781523T3 (es) 2012-07-12 2020-09-02 Hangzhou Dac Biotech Co Ltd Conjugados de moléculas de unión celular con agentes citotóxicos
CA2891280C (en) 2012-11-24 2018-03-20 Hangzhou Dac Biotech Co., Ltd. Hydrophilic linkers and their uses for conjugation of drugs to cell binding molecules
WO2014113584A1 (en) 2013-01-16 2014-07-24 Rhode Island Hospital Compositions and methods for the prevention and treatment of osteolysis and osteoporosis
HRP20171302T1 (hr) 2013-02-07 2017-10-20 Merck Patent Gmbh Makrociklički derivati piridazinona
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
CA2904393A1 (en) 2013-03-15 2014-09-25 Araxes Pharma Llc Covalent inhibitors of kras g12c
RU2015148359A (ru) 2013-04-12 2017-05-15 Асана Биосайенсис, Ллк Хиназолины и азахиназолины - двойные ингибиторы путей ras/raf/mek/erk и pi3k/akt/pten/mtor
CA2944198C (en) 2013-04-26 2021-11-16 Indiana University Research & Technology Corporation Hydroxyindole carboxylic acid based inhibitors for oncogenic src homology-2 domain containing protein tyrosine phosphatase-2 (shp2)
WO2014180271A1 (zh) 2013-05-10 2014-11-13 苏州明锐医药科技有限公司 阿法替尼及其中间体的制备方法
EP2806274A1 (en) 2013-05-24 2014-11-26 AIT Austrian Institute of Technology GmbH Lung cancer diagnostic method and means
EP3055290B1 (en) 2013-10-10 2019-10-02 Araxes Pharma LLC Inhibitors of kras g12c
ES2699351T3 (es) 2014-01-17 2019-02-08 Novartis Ag Derivados de 1-piridazin/triazin-3-il-piper(-azina)/idina/pirolidina y composiciones de las mismas para inhibir la actividad de 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
US10233431B2 (en) 2014-02-26 2019-03-19 The Regents Of The University Of California Producing 3-hydroxycarboxylic acid and ketone using polyketide synthases
WO2015132784A1 (en) 2014-03-03 2015-09-11 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Method and device for detection of pseudomonas aeruginosa
JO3474B1 (ar) 2014-08-29 2020-07-05 Amgen Inc مشتقات تيتراهيدرونافثالين التي تثبط بروتين mcl-1
JP2017528498A (ja) 2014-09-25 2017-09-28 アラクセス ファーマ エルエルシー Ｋｒａｓ ｇ１２ｃ変異体タンパク質のインヒビター
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
EP3247378B8 (en) 2015-01-09 2023-08-23 Revolution Medicines, Inc. Macrocyclic compounds that participate in cooperative binding and medical uses thereof
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
EP3277704A1 (en) 2015-03-31 2018-02-07 Allergan, Inc. Cyclosporins modified on the mebmt sidechain by heterocyclic rings
ES2898765T3 (es) 2015-04-10 2022-03-08 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos
US10428064B2 (en) 2015-04-15 2019-10-01 Araxes Pharma Llc Fused-tricyclic inhibitors of KRAS and methods of use thereof
WO2016191328A1 (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
US10532977B2 (en) 2015-06-01 2020-01-14 Indiana University Research And Technology Corporation Small molecule inhibitors of protein tyrosine phosphatases and uses thereof
EP3310779B1 (en) 2015-06-19 2019-05-08 Novartis AG Compounds and compositions for inhibiting the activity of shp2
US10287266B2 (en) 2015-06-19 2019-05-14 Novartis Ag Compounds and compositions for inhibiting the activity of SHP2
WO2016203405A1 (en) 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
WO2017015562A1 (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
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 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
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP4242304A3 (en) 2015-10-01 2024-02-07 Revolution Medicines, Inc. Methods and reagents for analyzing 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
US9988357B2 (en) 2015-12-09 2018-06-05 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
KR102444509B1 (ko) 2016-05-18 2022-09-19 미라티 테라퓨틱스, 인크. Kras g12c 억제제
WO2017210134A1 (en) 2016-05-31 2017-12-07 Board Of Regents, University Of Texas System Heterocyclic inhibitors of ptpn11
MX388576B (es) 2016-06-07 2025-03-20 Jacobio Pharmaceuticals Co Ltd Derivados heterociclicos novedosos utiles como inhibidores de shp2.
WO2017216706A1 (en) 2016-06-14 2017-12-21 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
EP4302834A3 (en) 2016-07-12 2024-07-17 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
WO2018057884A1 (en) 2016-09-22 2018-03-29 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
WO2018064510A1 (en) 2016-09-29 2018-04-05 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3523289A1 (en) 2016-10-07 2019-08-14 Araxes Pharma LLC Heterocyclic compounds as inhibitors of ras and methods of use thereof
TW202500565A (zh) 2016-10-24 2025-01-01 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
US11479797B2 (en) 2016-10-28 2022-10-25 Ginkgo Bioworks, Inc. Compositions and methods for the production of compounds
AU2017361856A1 (en) 2016-11-18 2019-05-23 Neurovive Pharmaceutical Ab Use of sanglifehrin macrocyclic analogues as anticancer compounds
KR20190095355A (ko) 2016-12-15 2019-08-14 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 암의 치료를 위한 조성물 및 방법
CN110366550A (zh) 2016-12-22 2019-10-22 美国安进公司 作为用于治疗肺癌、胰腺癌或结直肠癌的KRAS G12C抑制剂的苯并异噻唑、异噻唑并[3,4-b]吡啶、喹唑啉、酞嗪、吡啶并[2,3-d]哒嗪和吡啶并[2,3-d]嘧啶衍生物
EP3558979B1 (en) 2016-12-22 2021-02-17 Boehringer Ingelheim International GmbH Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors
WO2018129402A1 (en) 2017-01-06 2018-07-12 Oregon Health & Science University Compositions and methods used in diagnosing and treating colorectal cancer
CA3048340A1 (en) 2017-01-10 2018-07-19 Novartis Ag Pharmaceutical combination comprising an alk inhibitor and a shp2 inhibitor
JP7240319B2 (ja) 2017-01-23 2023-03-15 レヴォリューション・メディスンズ，インコーポレイテッド アロステリックｓｈｐ２阻害剤としての二環式化合物
KR20190110588A (ko) 2017-01-23 2019-09-30 레볼루션 메디슨즈, 인크. 알로스테릭 shp2 억제제로서의 피리딘 화합물
JP7327802B2 (ja) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ－ヘテロ二環式化合物およびその使用方法
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
WO2018140513A1 (en) 2017-01-26 2018-08-02 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
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
EP3573966A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused n-heterocyclic compounds and methods of use thereof
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone 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
WO2018172250A1 (en) 2017-03-21 2018-09-27 Bayer Pharma Aktiengesellschaft 2-methyl-quinazolines
EA202190196A1 (ru) 2017-03-23 2021-08-31 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
IL269779B2 (en) 2017-04-05 2026-04-01 Revolution Medicines Inc Methods and reagents for the analysis of protein-protein interfaces
CA3058953A1 (en) 2017-04-05 2018-10-11 Revolution Medicines, Inc. Compounds that participate in cooperative binding and uses thereof
WO2018191815A1 (en) 2017-04-20 2018-10-25 Apotex Inc. Processes for the preparation of acalabrutinib and intermediates thereof
WO2018204416A1 (en) 2017-05-02 2018-11-08 Revolution Medicines, Inc. Rapamycin analogs as mtor inhibitors
EP3621968A1 (en) 2017-05-11 2020-03-18 Astrazeneca AB Heteroaryl compounds that inhibit g12c mutant ras proteins
AU2018273356B2 (en) 2017-05-22 2021-09-16 Amgen Inc. KRAS G12C inhibitors and methods of using the same
CN110869357A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 化合物及其用于治疗癌症的使用方法
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
US10745385B2 (en) 2017-05-25 2020-08-18 Araxes Pharma Llc Covalent inhibitors of KRAS
EP3630770B1 (en) 2017-05-26 2024-08-28 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
AU2018329920B2 (en) * 2017-09-08 2022-12-01 Amgen Inc. Inhibitors of KRAS G12C and methods of using the same
JP7447002B2 (ja) 2017-09-11 2024-03-11 クルーゾン・ファーマシューティカルズ・インコーポレイテッド ＳＨＰ２のオクタヒドロシクロペンタ［ｃ］ピロールのアロステリック阻害剤
LT3710439T (lt) 2017-11-15 2023-05-10 Mirati Therapeutics, Inc. Kras g12c inhibitoriai
US10597405B2 (en) 2017-12-08 2020-03-24 Astrazeneca Ab Chemical compounds
HRP20230400T1 (hr) 2017-12-21 2023-06-23 Boehringer Ingelheim International Gmbh Benzilamino supstituirani piridopirimidinoni i derivati kao inhibitori sos1
WO2019152454A1 (en) 2018-01-30 2019-08-08 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
US11044675B2 (en) 2018-02-13 2021-06-22 Idac Holdings, Inc. Methods, apparatuses and systems for adaptive uplink power control in a wireless network
JP7335882B2 (ja) 2018-02-13 2023-08-30 ブルーレイ セラピューティクス （シャンハイ） カンパニー，リミティド ピリミジン縮合環式化合物及びその製造方法、並びに使用
WO2019165073A1 (en) 2018-02-21 2019-08-29 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
IL276232B2 (en) 2018-03-02 2024-04-01 Otsuka Pharma Co Ltd Pyrazine derivatives, pharmaceutical compositions comprising them and their use for treating diseases
US12138263B2 (en) 2018-03-21 2024-11-12 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine SHP2 phosphatase inhibitors and methods of use thereof
RU2020133727A (ru) 2018-03-21 2022-04-21 Сучжоу Пухе Биофарма Ко., Лтд. Ингибиторы shp2 и их применение
AU2019240299B2 (en) 2018-03-21 2023-06-22 D.E. Shaw Research, Llc SHP2 phosphatase inhibitors and methods of use thereof
US20220274979A1 (en) 2018-04-18 2022-09-01 Bayer Pharma Aktiengesellschaft 2-methyl-aza-quinazolines
MX2020011565A (es) 2018-05-01 2021-01-29 Revolution Medicines Inc Analogos de rapamicina ligados a c40, c28 y c-32 como inhibidores de mtor.
IL312291A (en) 2018-05-01 2024-06-01 Revolution Medicines Inc C-26-linked rapamycin analogs as MTOR inhibitors
MX2020011528A (es) 2018-05-02 2021-02-09 Navire Pharma Inc Inhibidores heterociclicos sustituidos de ptpn11.
CA3098574A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
EP3788053B1 (en) 2018-05-04 2024-07-10 Amgen Inc. Kras g12c inhibitors and methods of using the same
WO2019217307A1 (en) 2018-05-07 2019-11-14 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
MA52564A (fr) 2018-05-10 2021-03-17 Amgen Inc Inhibiteurs de kras g12c pour le traitement du cancer
US11096939B2 (en) 2018-06-01 2021-08-24 Amgen Inc. KRAS G12C inhibitors and methods of using the same
EP3801613A1 (en) 2018-06-04 2021-04-14 Bayer Aktiengesellschaft Inhibitors of shp2
MX2020012204A (es) 2018-06-11 2021-03-31 Amgen Inc Inhibidores de kras g12c para tratar el cáncer.
US11285156B2 (en) 2018-06-12 2022-03-29 Amgen Inc. Substituted piperazines as KRAS G12C inhibitors
MX2021000795A (es) 2018-07-24 2021-04-12 Taiho Pharmaceutical Co Ltd Compuestos heterociclicos para inhibir la actividad de shp2.
MX2021000887A (es) 2018-08-01 2021-03-31 Araxes Pharma Llc Compuestos espiroheterociclicos y metodos de uso de los mismos para el tratamiento de cancer.
US11518770B2 (en) 2018-08-06 2022-12-06 Purdue Research Foundation Sesquiterpenoid analogs
CN112601750B (zh) 2018-08-10 2023-10-31 纳维尔制药有限公司 Ptpn11（shp2）抑制剂
AU2019320945C1 (en) 2018-08-16 2021-09-30 F. Hoffmann-La Roche Ag Fused ring compounds
ES2961253T3 (es) 2018-08-31 2024-03-11 Mirati Therapeutics Inc Inhibidores de KRas G12C
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)
US20210393623A1 (en) 2018-09-26 2021-12-23 Jacobio Pharmaceuticals Co., Ltd. Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors
IL305106B2 (en) 2018-09-29 2025-08-01 Novartis Ag Process of manufacture of a compound for inhibiting the activity of shp2
CN112867718B (zh) 2018-09-29 2025-03-04 诺华股份有限公司 用于抑制shp2活性的化合物和组合物的制造
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
BR112021005733A2 (pt) 2018-10-17 2021-07-27 Array Biopharma Inc. inibidores de proteína tirosina fosfatase
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
JP2022506887A (ja) 2018-11-07 2022-01-17 シャンハイ リンジーン バイオファーマ カンパニー リミテッド 窒素含有縮合複素環系ｓｈｐ２阻害剤化合物、製造方法及び使用
AU2019384118B2 (en) 2018-11-19 2025-06-12 Amgen Inc. KRAS G12C inhibitors and methods of using the same
JP7454573B2 (ja) 2018-11-23 2024-03-22 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル インスリン抵抗性を処置するためのｓｈｐ２阻害剤の使用
EP3889153A4 (en) 2018-11-30 2022-09-07 Tuojie Biotech (Shanghai) Co., Ltd. PYRIMIDINE AND FIVE-MEMBERED HETEROCYCLIC NITROGEN DERIVATIVE, METHOD OF MANUFACTURE THEREOF AND MEDICAL USES THEREOF
BR112021012057A2 (pt) * 2018-12-21 2021-10-19 Revolution Medicines, Inc. Compostos que participam de ligação cooperativa e usos dos mesmos
JP2022516685A (ja) 2019-01-08 2022-03-01 イエール ユニバーシティ ホスファターゼ結合化合物およびそれらを使用する方法
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
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
US20220152026A1 (en) 2019-02-12 2022-05-19 Novartis Ag Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
MX2021009562A (es) 2019-02-12 2021-09-08 Novartis Ag Combinacion farmaceutica que comprende tno155 y un inhibidor de pd-1.
EP3923941B1 (en) 2019-02-12 2025-12-03 Novartis AG Pharmaceutical combination comprising tno155 and ribociclib
WO2020173935A1 (en) 2019-02-26 2020-09-03 Boehringer Ingelheim International Gmbh New isoindolinone substituted indoles and derivatives as ras inhibitors
MX2021010323A (es) 2019-03-01 2021-12-10 Revolution Medicines Inc Compuestos bicíclicos de heterociclilo y usos de este.
MX2021010319A (es) 2019-03-01 2021-12-10 Revolution Medicines Inc Compuestos biciclicos de heteroarilo y usos de estos.
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
US11033547B2 (en) 2019-03-07 2021-06-15 Merck Patent Gmbh Carboxamide-pyrimidine derivatives as SHP2 antagonists
CU20210080A7 (es) 2019-04-02 2022-05-11 Array Biopharma Inc Triazinas sustituidas como inhibidores de proteína tirosina fosfatasa
JP7586834B2 (ja) 2019-04-08 2024-11-19 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｓｈｐ２拮抗薬としてのピリミジノン誘導体
CN114008035A (zh) 2019-06-14 2022-02-01 北京盛诺基医药科技股份有限公司 一种shp2磷酸酶变构抑制剂
KR20220054285A (ko) 2019-06-28 2022-05-02 투오지에 바이오텍 (상하이) 컴퍼니 리미티드 피리미딘 5 원 질소 헤테로고리형 유도체, 이의 제조 방법 및 이의 약학적 용도
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
WO2021043077A1 (zh) 2019-09-06 2021-03-11 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
CN114502165A (zh) 2019-09-23 2022-05-13 苏州浦合医药科技有限公司 Shp2抑制剂及其用途
MX2022003454A (es) 2019-09-24 2022-04-19 Relay Therapeutics Inc Inhibidores de fosfatasa shp2 y metodos para su fabricacion y uso.
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
UA129778C2 (uk) 2019-10-28 2025-07-30 Мерк Шарп Енд Доум Елелсі Низькомолекулярні інгібітори g12c-мутантного kras
TW202132316A (zh) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ｒａｓ抑制劑
IL322454A (en) 2019-11-04 2025-09-01 Revolution Medicines Inc ras inhibitors
AU2020377925A1 (en) 2019-11-04 2022-05-05 Revolution Medicines, Inc. Ras inhibitors
WO2021088945A1 (zh) 2019-11-08 2021-05-14 南京圣和药业股份有限公司 作为shp2抑制剂的化合物及其应用
CA3156359A1 (en) 2019-11-08 2021-05-14 Adrian Liam Gill Bicyclic heteroaryl compounds and uses thereof
EP4065231A1 (en) 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
LT4065575T (lt) 2019-11-29 2024-05-27 Lupin Limited Pakeisti tricikliniai junginiai
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
WO2021126799A1 (en) 2019-12-18 2021-06-24 Merck Sharp & Dohme Corp. 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
CN114761408B (zh) 2019-12-19 2023-09-15 贝达药业股份有限公司 Kras g12c抑制剂及其在医药上的应用
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
IL293962B2 (en) 2019-12-19 2025-10-01 Jacobio Pharmaceuticals Co Ltd Mutant KRAS protein inhibitors
CA3164995A1 (en) 2019-12-20 2021-06-24 Erasca, Inc. Tricyclic pyridones and pyrimidones
PH12022551513A1 (en) 2019-12-20 2023-04-24 Mirati Therapeutics Inc Sos1 inhibitors
WO2021120890A1 (en) 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
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
JP7850663B2 (ja) 2019-12-27 2026-04-23 ウィゲン・バイオメディシン・テクノロジー・（シャンハイ）・カンパニー・リミテッド スピロ環含有キナゾリン化合物
PE20221283A1 (es) 2019-12-27 2022-09-05 Lupin Ltd Compuestos triciclicos sustituidos
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
WO2021139748A1 (en) 2020-01-08 2021-07-15 Ascentage Pharma (Suzhou) Co., Ltd. Spirocyclic tetrahydroquinazolines
US20210269434A1 (en) 2020-01-10 2021-09-02 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
CN114761394B (zh) 2020-01-16 2024-03-29 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
WO2021143680A1 (zh) 2020-01-16 2021-07-22 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
WO2021150613A1 (en) 2020-01-20 2021-07-29 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
CN114846005B (zh) 2020-01-21 2024-04-02 贝达药业股份有限公司 Shp2抑制剂及其应用
WO2021148010A1 (zh) 2020-01-22 2021-07-29 南京明德新药研发有限公司 吡唑并杂芳环类化合物及其应用
TW202140024A (zh) 2020-01-24 2021-11-01 日商大鵬藥品工業股份有限公司 Shp2抑制劑嘧啶酮與新穎癌症醫藥併用於癌症之抗腫瘤活性之增強
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
JP2023513675A (ja) 2020-02-06 2023-04-03 ウェルマーカー・バイオ・カンパニー・リミテッド Ｋｒａｓ変異に関連する癌の予防または治療のための医薬組成物
CN115135650A (zh) 2020-02-20 2022-09-30 贝达医药公司 作为kras抑制剂的吡啶并嘧啶衍生物
CN113637005B (zh) 2020-02-24 2024-05-24 泰励生物科技（上海）有限公司 用于癌症治疗的kras抑制剂
CN114845997B (zh) 2020-02-24 2024-03-29 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
US20230101312A1 (en) 2020-02-24 2023-03-30 Mirati Therapeutics, Inc. Sos1 inhibitors
EP4110338A1 (en) 2020-02-28 2023-01-04 Novartis AG A triple pharmaceutical combination comprising dabrafenib, an erk inhibitor and a shp2 inhibitor
US20210292330A1 (en) 2020-02-28 2021-09-23 Erasca, Inc. Pyrrolidine-fused heterocycles
CN114901663B (zh) 2020-03-02 2024-07-02 上海喆邺生物科技有限公司 一类芳香杂环类化合物及其在药物中的应用
IT202000004849A1 (it) 2020-03-06 2021-09-06 Univ Degli Studi Di Roma “Tor Vergata” Peptidi e loro usi
AU2021233058B2 (en) 2020-03-12 2024-05-16 D3 Bio(Wuxi) Co., Ltd Pyrimidoheterocyclic compounds and application thereof
TW202144345A (zh) 2020-03-17 2021-12-01 大陸商北京加科思新藥研發有限公司 Ｋｒａｓ突變蛋白抑制劑
CA3170068A1 (en) 2020-03-25 2021-09-30 Yuli Xie Spiro ring-containing quinazoline compound
EP4186903A4 (en) 2020-07-24 2024-08-07 Medshine Discovery Inc. Quinazoline compound
EP4188383A4 (en) 2020-07-28 2025-01-08 Mirati Therapeutics, Inc. SOS1 INHIBITORS
US20250195521A1 (en) 2020-09-03 2025-06-19 Revolution Medicines, Inc. Use of sos1 inhibitors to treat malignancies with shp2 mutations
CA3194067A1 (en) 2020-09-15 2022-03-24 Revolution Medicines, Inc. Ras inhibitors
US20230357239A1 (en) 2020-09-18 2023-11-09 Bayer Aktiengesellschaft Pyrido[2,3-d]pyrimidin-4-amines as sos1 inhibitors
JP2023544450A (ja) 2020-09-23 2023-10-23 エラスカ・インコーポレイテッド 三環式ピリドン及びピリミドン
WO2022081912A2 (en) 2020-10-15 2022-04-21 Kumquat Biosciences Inc. Heterocycles and uses thereof
US20240124478A1 (en) 2020-11-23 2024-04-18 Merck Sharp & Dohme Llc SPIROCYCLIC-SUBSTITUTED 6,7-DIHYDRO-PYRANO[2,3-d]PYRIMIDINE INHIBITORS OF KRAS G12C MUTANT
EP4247807A4 (en) 2020-11-23 2024-10-16 Merck Sharp & Dohme LLC 6,7-DIHYDRO-PYRANO[2,3-D PYRIMIDINE AS INHIBITORS OF THE KRAS G12C MUTANT
TWI880049B (zh) 2020-12-04 2025-04-11 美商美國禮來大藥廠 Kras g12c抑制劑
JP2023553492A (ja) 2020-12-15 2023-12-21 ミラティ セラピューティクス， インコーポレイテッド アザキナゾリン汎ＫＲａｓ阻害剤
EP4262803A4 (en) 2020-12-16 2025-03-12 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
WO2022133345A1 (en) 2020-12-18 2022-06-23 Erasca, Inc. Tricyclic pyridones and pyrimidones
WO2022135568A1 (zh) 2020-12-25 2022-06-30 江苏恒瑞医药股份有限公司 一种嘧啶并五元氮杂环类衍生物的晶型及其制备方法
JP2024503280A (ja) 2020-12-29 2024-01-25 レボリューション メディシンズ インコーポレイテッド Ｓｏｓ１阻害剤及びその使用
MX2023011608A (es) 2021-04-02 2023-12-14 Massachusetts Gen Hospital Metodos para inhibir ras.
WO2022217053A1 (en) 2021-04-09 2022-10-13 Revolution Medicines, Inc. Use of sos1 inhibitors with ras inhibitors to treat cancers
JP2024516450A (ja) 2021-05-05 2024-04-15 レボリューション メディシンズ インコーポレイテッド 共有結合性ｒａｓ阻害剤及びその使用
TW202309052A (zh) 2021-05-05 2023-03-01 美商銳新醫藥公司 Ｒａｓ抑制劑
KR20240017811A (ko) * 2021-05-05 2024-02-08 레볼루션 메디슨즈, 인크. 암의 치료를 위한 ras 억제제
AU2022281343A1 (en) 2021-05-25 2023-11-30 Revolution Medicines, Inc. Methods for inhibiting ras
WO2022271658A1 (en) 2021-06-23 2022-12-29 Erasca, Inc. Tricyclic kras inhibitors
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
US20250066386A1 (en) 2021-11-09 2025-02-27 Biomea Fusion, Inc. Inhibitors of kras
CN119156393A (zh) 2022-04-25 2024-12-17 翰森生物有限责任公司 环状化合物及其制备方法和医药用途
JP2025519199A (ja) 2022-06-01 2025-06-24 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト がんの治療のためのハロインドール大環状化合物
CN119546612A (zh) 2022-07-04 2025-02-28 豪夫迈·罗氏有限公司 用于治疗癌症的kras的大环抑制剂
JP2025525315A (ja) 2022-07-08 2025-08-05 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト Ｋｒａｓ阻害剤として有用な大員環化合物
AR129934A1 (es) 2022-07-20 2024-10-16 Hoffmann La Roche Compuestos macrocíclicos para el tratamiento de cáncer

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