[go: up one dir, main page]

PE20230249A1 - Compuestos de heteroarilo biciclicos y usos de estos - Google Patents

Compuestos de heteroarilo biciclicos y usos de estos

Info

Publication number
PE20230249A1
PE20230249A1 PE2022000740A PE2022000740A PE20230249A1 PE 20230249 A1 PE20230249 A1 PE 20230249A1 PE 2022000740 A PE2022000740 A PE 2022000740A PE 2022000740 A PE2022000740 A PE 2022000740A PE 20230249 A1 PE20230249 A1 PE 20230249A1
Authority
PE
Peru
Prior art keywords
group
alkyl
bicyclic heteroaryl
heteroaryl compounds
optionally substituted
Prior art date
Application number
PE2022000740A
Other languages
English (en)
Inventor
Adrian Liam Gill
Andreas Buckl
Elena S Koltun
Naing Aay
Arlyn A Tambo-Ong
Severin Thompson
Micah J Gliedt
John E Knox
James Joseph Cregg
Anne V Edwards
Yang Liu
G Leslie Burnett
William D Thomas
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 PE20230249A1 publication Critical patent/PE20230249A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6581Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6568Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus atoms as the only ring hetero atoms
    • C07F9/65685Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus atoms as the only ring hetero atoms the ring phosphorus atom being part of a phosphine oxide or thioxide
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers

Landscapes

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

Abstract

Referido a un compuesto de Formula I, o una sal, solvato, isomero, profarmaco, o tautomero farmaceuticamente aceptable del mismo, en donde R1 se selecciona del grupo que consiste en cicloalquilo de 3-6 miembros opcionalmente sustituidos, heterociclilo de 3-6 miembros opcionalmente sustituido, entre otros; R2 se selecciona del grupo que consiste en H, alquilo C1-6, halogeno, -NHR2a, entre otros; R3 se selecciona del grupo que consiste en H, alquilo C1-3, -OR3a, entre otros; L4 se selecciona del grupo que consiste en enlace, -C(O)-, -C(O)O-, entre otros; y R4 se selecciona del grupo que consiste en H, alquilo C1-6, cicloalquilo de 3-14 miembros, entre otros. Estos compuestos de heteroarilo biciclicos son moduladores de SOS1. Tambien se refiere a metodos para sintetizar estos compuestos, composiciones farmaceuticas que los comprenden y su uso en el tratamiento de enfermedades o trastornos asociados con la actividad aberrante de SOS1, como el cancer..
PE2022000740A 2019-11-08 2020-11-05 Compuestos de heteroarilo biciclicos y usos de estos PE20230249A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201962933141P 2019-11-08 2019-11-08
US202063031318P 2020-05-28 2020-05-28
US202063070593P 2020-08-26 2020-08-26
PCT/US2020/059024 WO2021092115A1 (en) 2019-11-08 2020-11-05 Bicyclic heteroaryl compounds and uses thereof

Publications (1)

Publication Number Publication Date
PE20230249A1 true PE20230249A1 (es) 2023-02-07

Family

ID=73646489

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022000740A PE20230249A1 (es) 2019-11-08 2020-11-05 Compuestos de heteroarilo biciclicos y usos de estos

Country Status (17)

Country Link
US (3) US20210139517A1 (es)
EP (2) EP4620531A3 (es)
KR (1) KR20220100903A (es)
CN (2) CN116425742A (es)
AU (1) AU2020380315A1 (es)
BR (1) BR112022008858A2 (es)
CA (1) CA3156359A1 (es)
CL (1) CL2023000416A1 (es)
CO (1) CO2022005968A2 (es)
CR (1) CR20220200A (es)
IL (1) IL292679A (es)
MX (1) MX2022005525A (es)
PE (1) PE20230249A1 (es)
PH (1) PH12022551102A1 (es)
SA (1) SA522432518B1 (es)
TW (1) TW202128688A (es)
WO (1) WO2021092115A1 (es)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021092115A1 (en) * 2019-11-08 2021-05-14 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
EP4166555A1 (en) * 2020-06-11 2023-04-19 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Pyridine-pyrimidine derivative, preparation method therefor and pharmaceutical use thereof
CN113801114B (zh) * 2020-06-11 2022-11-18 江苏恒瑞医药股份有限公司 稠合二环杂芳基类衍生物、其制备方法及其在医药上的应用
EP4497473A3 (en) 2020-08-26 2025-04-23 Haisco Pharmaceuticals Pte. Ltd. Nitrile derivative that acts as inhibitor of dipeptidyl peptidase 1 and use thereof
AU2021333776A1 (en) 2020-08-26 2023-03-16 Vertex Pharmaceuticals Incorporated Inhibitors of APOL1 and methods of using same
CA3187757A1 (en) 2020-09-03 2022-03-24 Ethan AHLER Use of sos1 inhibitors to treat malignancies with shp2 mutations
AU2021340716A1 (en) 2020-09-11 2023-03-30 Mirati Therapeutics, Inc. Crystalline forms of a KRas G12C inhibitor
IL301298A (en) 2020-09-15 2023-05-01 Revolution Medicines Inc Indole derivatives as RAS inhibitors in cancer therapy
US20240336606A1 (en) * 2020-10-20 2024-10-10 Suzhou Zelgen Biopharmaceuticals Co., Ltd. Substituted benzo or pyridopyrimidine amine inhibitor, preparation method therefor, and application thereof
US12398154B2 (en) 2020-12-15 2025-08-26 Mirati Therapeutics, Inc. Azaquinazoline pan-KRas inhibitors
EP4262803A4 (en) 2020-12-16 2025-03-12 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
WO2022135590A1 (zh) * 2020-12-27 2022-06-30 上海凌达生物医药有限公司 一类嘧啶并杂环类化合物、制备方法和用途
WO2022170802A1 (zh) * 2021-02-09 2022-08-18 苏州阿尔脉生物科技有限公司 一种作为sos1抑制剂的嘧啶并吡啶酮类衍生物、其制备方法及用途
WO2022171018A1 (zh) * 2021-02-09 2022-08-18 苏州泽璟生物制药股份有限公司 取代苯并或吡啶并嘧啶胺类抑制剂及其制备方法和应用
WO2022187411A1 (en) 2021-03-02 2022-09-09 Kumquat Biosciences Inc. Heterocycles and uses thereof
US20220324862A1 (en) * 2021-03-31 2022-10-13 Acerand Therapeutics (Usa) Limited Pyridopyrimidinone compounds
EP4319757A1 (en) 2021-04-09 2024-02-14 Boehringer Ingelheim International GmbH Anticancer therapy
WO2022240947A1 (en) * 2021-05-12 2022-11-17 Revolution Medicines, Inc. Use of sos1 inhibitors with mtor inhibitors to treat cancers
CN115246841B (zh) * 2021-09-14 2024-02-09 北京福元医药股份有限公司 苄氨基取代的嘧啶并吡喃酮衍生物及其组合物、制剂和用途
JP2024533787A (ja) 2021-09-29 2024-09-12 ハイファ バイオファーマ カンパニー リミテッド ピリド六員環構造を有するsos1阻害剤
US20250000863A1 (en) 2021-10-05 2025-01-02 Mirati Therapeutics, Inc. Combination therapies of kras g12d inhibitors with sos1 inhibitors
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
CN119212994A (zh) 2021-12-17 2024-12-27 建新公司 作为shp2抑制剂的吡唑并吡嗪化合物
WO2023118250A1 (en) * 2021-12-23 2023-06-29 Boehringer Ingelheim International Gmbh 8-aza quinazolines as brain-penetrant sos1-inhibitors
US20250154147A1 (en) 2022-01-14 2025-05-15 Jazz Pharmaceuticals Ireland Limited Novel amine-substituted phthalazines and derivatives as sos1 inhibitors
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
GB202203976D0 (en) 2022-03-22 2022-05-04 Jazz Pharmaceuticals Ireland Ltd Tricyclic phthalazines and derivatives as sos1 inhibitors
IL316144A (en) * 2022-04-20 2024-12-01 Kumquat Biosciences Inc Macrocyclic heterocycles and their uses
WO2023215257A2 (en) * 2022-05-03 2023-11-09 Revolution Medicines, Inc. Sos1 inhibitors and uses thereof
WO2023215256A1 (en) * 2022-05-03 2023-11-09 Revolution Medicines, Inc. Sos1 inhibitors and uses thereof
WO2023220421A1 (en) * 2022-05-13 2023-11-16 Ranok Therapeutics (Hangzhou) Co. Ltd. Inhibitors of kras(g12d)
CN120504682A (zh) 2022-06-10 2025-08-19 锐新医药公司 大环ras抑制剂
EP4573095A1 (en) 2022-08-17 2025-06-25 Treeline Biosciences, Inc. Pyridopyrimidine kras inhibitors
CN121263418A (zh) 2023-04-07 2026-01-02 锐新医药公司 大环ras抑制剂
KR20260005904A (ko) 2023-04-07 2026-01-12 레볼루션 메디슨즈, 인크. 매크로사이클릭 ras 억제제
CN121100123A (zh) 2023-04-14 2025-12-09 锐新医药公司 Ras抑制剂的结晶形式
TW202448897A (zh) 2023-04-14 2024-12-16 美商銳新醫藥公司 Ras抑制劑之結晶形式、含有其之組合物及其使用方法
TW202500126A (zh) 2023-05-24 2025-01-01 美商金橘生物科技公司 雜環化合物及其用途
CN119139313A (zh) * 2023-06-15 2024-12-17 石药集团中奇制药技术(石家庄)有限公司 一种杂环类抗肿瘤化合物的用途
TW202502779A (zh) 2023-06-30 2025-01-16 美商金橘生物科技公司 取代的雜芳族胺及其用途
TW202515575A (zh) 2023-09-11 2025-04-16 美商金橘生物科技公司 細胞增殖調節劑及其用途
WO2025064848A1 (en) 2023-09-21 2025-03-27 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyridine kras inhibitors
WO2025090810A1 (en) 2023-10-25 2025-05-01 Kumquat Biosciences Inc. Use of sos1 inhibitors and amivantamab to treat cancer
WO2025090808A1 (en) 2023-10-25 2025-05-01 Kumquat Biosciences Inc. Combinations of sos-1 inhibitors with osimertinib and/or met inhibitors to treat cancer
WO2025171055A1 (en) 2024-02-06 2025-08-14 Kumquat Biosciences Inc. Heterocyclic conjugates and uses thereof
WO2025230971A1 (en) 2024-04-30 2025-11-06 Kumquat Biosciences Inc. Macrocyclic heterocycles as anticancer agents
WO2025245127A1 (en) 2024-05-21 2025-11-27 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors

Family Cites Families (238)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
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
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
DE4221054A1 (de) 1992-06-30 1994-01-05 Herbst Bremer Goldschlaegerei Präparat zur prophylaktischen und therapeutischen Behandlung von Karies sowie Verfahren zum Herstellen desselben
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
US5262564A (en) 1992-10-30 1993-11-16 Octamer, Inc. Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
CA2148484A1 (en) 1992-11-13 1994-05-26 Stewart Lyman 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
CA2148931A1 (en) 1993-10-01 1995-04-13 Jurg Zimmermann 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
WO1995024190A2 (en) 1994-03-07 1995-09-14 Sugen, Inc. Receptor tyrosine kinase inhibitors for inhibiting cell proliferative disorders and compositions thereof
EP0756627A1 (en) 1994-04-15 1997-02-05 Amgen Inc. Hek5, hek7, hek8, hek11, new eph-like receptor protein tyrosine kinases
DK0682027T3 (da) 1994-05-03 1998-05-04 Ciba Geigy Ag Pyrrolopyrimidinderivater med antiproliferativ virkning
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
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
EP2163546B1 (en) 1995-03-30 2016-06-01 Pfizer Products Inc. Quinazoline derivatives
DE69609602T2 (de) 1995-04-03 2001-04-12 Novartis Ag, Basel Pyrazolderivate und verfahren zu deren herstellung
US5861510A (en) 1995-04-20 1999-01-19 Pfizer Inc Arylsulfonyl hydroxamic acid derivatives as MMP and TNF inhibitors
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
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
US7067318B2 (en) 1995-06-07 2006-06-27 The Regents Of The University Of Michigan 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
CA2219659C (en) 1995-06-09 2008-03-18 Novartis Ag Rapamycin derivatives
TR199800012T1 (xx) 1995-07-06 1998-04-21 Novartis Ag Piroloprimidinler ve preparasyon i�in tatbikler.
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
DE69624081T2 (de) 1995-12-20 2003-06-12 Agouron Pharmaceuticals, Inc. Matrix-metalloprotease Inhibitoren
JP4275733B2 (ja) 1996-01-23 2009-06-10 ノバルティス アクチエンゲゼルシャフト ピロロピリミジンおよびその製造法
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
DE69710712T3 (de) 1996-04-12 2010-12-23 Warner-Lambert Co. Llc Umkehrbare inhibitoren von tyrosin kinasen
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
EP0937082A2 (en) 1996-07-12 1999-08-25 Ariad Pharmaceuticals, Inc. Materials and method for treating or preventing pathogenic fungal infection
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
EP0912559B1 (en) 1996-07-13 2002-11-06 Glaxo Group Limited Fused heterocyclic compounds as protein tyrosine kinase inhibitors
ES2191187T3 (es) 1996-07-13 2003-09-01 Glaxo Group Ltd Compuestos heteroaromaticos biciclicos como inhibidores de la proteina tirosin-quinasa.
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
EA199900036A1 (ru) 1996-07-18 1999-06-24 Пфайзер Инк Ингибиторы металлопротеаз матрикса на основе фосфинатов, фармацевтическая композиция, способ лечения
US6111090A (en) 1996-08-16 2000-08-29 Schering Corporation Mammalian cell surface antigens; related reagents
AU4055697A (en) 1996-08-16 1998-03-06 Schering Corporation Mammalian cell surface antigens; related reagents
PL331895A1 (en) 1996-08-23 1999-08-16 Pfizer Arylosulphonylamino derivatives of hydroxamic acid
ATE384062T1 (de) 1996-08-23 2008-02-15 Novartis Pharma Gmbh Substituierte pyrrolopyrimidine und verfahren zu ihrer herstellung
EP0929553B1 (en) 1996-10-02 2005-03-16 Novartis AG Pyrimidine derivatives and processes for the preparation thereof
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
WO1998014449A1 (en) 1996-10-02 1998-04-09 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
DK0950059T3 (da) 1997-01-06 2004-11-01 Pfizer Cycliske sulfonderivater
ATE248812T1 (de) 1997-02-03 2003-09-15 Pfizer Prod Inc Arylsulfonylhydroxamsäurederivate
KR20000070751A (ko) 1997-02-05 2000-11-25 로즈 암스트롱, 크리스틴 에이. 트러트웨인 세포 증식 억제제로서의 피리도[2,3-d]피리미딘 및 4-아미노피리미딘
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
PL334997A1 (en) 1997-02-11 2000-03-27 Pfizer Derivatives or arylosulphonyl-hydroxamic acid
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
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
BR9811868A (pt) 1997-08-08 2000-08-15 Pfizer Prod Inc Derivados de ácido ariloxiarilsulfonilamino hidroxâmico
AU1102399A (en) 1997-10-21 1999-05-10 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
GB9800575D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
IL137409A0 (en) 1998-02-09 2001-07-24 Genentech Inc Novel tumor necrosis factor receptor homolog and nucleic acids encoding the same
AU756838B2 (en) 1998-03-04 2003-01-23 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
HUP0103617A2 (hu) 1998-05-29 2002-02-28 Sugen, Inc. Protein kinázt gátló, pirrolilcsoporttal helyettesített 2-indolszármazékok, e vegyületeket tartalmazó gyógyászati készítmények, valamint e vegyületek alkalmazása
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
EP1097147A4 (en) 1998-07-10 2001-11-21 Merck & Co Inc NEW ANGIOGENESIS INHIBITORS
AU760020B2 (en) 1998-08-31 2003-05-08 Merck & Co., Inc. Novel angiogenesis inhibitors
ES2213985T3 (es) 1998-11-05 2004-09-01 Pfizer Products Inc. Derivados de hidroxiamida de acido 5-oxo-pirrolidin-2-carboxilico.
DE60028740T2 (de) 1999-03-30 2007-05-24 Novartis Ag Phthalazinderivate zur behandlung von entzündlichen erkrankungen
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
CA2383451A1 (en) 1999-08-24 2001-03-01 Ariad Gene Therapeutics, Inc. 28-epirapalogs
EP1676845B1 (en) 1999-11-05 2008-06-11 AstraZeneca AB New quinazoline derivatives
EP1233943B1 (en) 1999-11-24 2011-06-29 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
US6797514B2 (en) 2000-02-24 2004-09-28 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
US6867041B2 (en) 2000-02-24 2005-03-15 Xcyte Therapies, Inc. Simultaneous stimulation and concentration of cells
ES2302726T3 (es) 2000-02-24 2008-08-01 Invitrogen Corporation Estimulacion y concentracion simultanea de celulas.
US7074408B2 (en) 2000-02-25 2006-07-11 Immunex Corporation Use of integrin antagonists to inhibit angiogenesis
US6630500B2 (en) 2000-08-25 2003-10-07 Cephalon, Inc. Selected fused pyrrolocarbazoles
CN1307173C (zh) 2000-12-21 2007-03-28 葛兰素集团有限公司 作为血管生成调节剂的嘧啶胺
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
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
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
KR20060052681A (ko) 2003-05-23 2006-05-19 와이어쓰 Gitr 리간드, gitr 리간드-연관 분자, 항체 및그의 용도
PT1646634E (pt) 2003-07-08 2009-02-16 Novartis Ag Utilização de rapamicina e derivados de rapamicina para o tratamento de perda óssea
WO2005016252A2 (en) 2003-07-11 2005-02-24 Ariad Gene Therapeutics, Inc. Phosphorus-containing macrocycles
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
TW200523262A (en) 2003-07-29 2005-07-16 Smithkline Beecham Corp Inhibitors of AKT activity
EP2287156B1 (en) 2003-08-15 2013-05-29 Novartis AG 2,4-Di(phenylamino)-pyrimidines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders
WO2005055808A2 (en) 2003-12-02 2005-06-23 Genzyme Corporation Compositions and methods to diagnose and treat lung cancer
WO2005094314A2 (en) 2004-03-26 2005-10-13 The Burnham Institute Modulators of shp2 tyrosine phosphatase and their use in the treatment of body weight disorders
GB0409799D0 (en) 2004-04-30 2004-06-09 Isis Innovation Method of generating improved immune response
EP1765402A2 (en) 2004-06-04 2007-03-28 Duke University Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity
PL1786785T3 (pl) 2004-08-26 2010-08-31 Pfizer Enancjomerycznie czyste związki aminoheteroarylowe jako kinazy białkowe
MX2007004489A (es) 2004-10-13 2007-09-21 Wyeth Corp Analogos de 17-hidroxiwortamina como inhibidores pi3k.
CA2602777C (en) 2005-03-25 2018-12-11 Tolerrx, Inc. Gitr binding molecules and uses therefor
EP1885369B1 (en) 2005-05-04 2015-09-23 Evotec AG Fused heterocyclic compounds, and compositions and uses thereof
PL2161336T5 (pl) 2005-05-09 2017-10-31 Ono Pharmaceutical Co Ludzkie przeciwciała monoklonalne przeciwko białku Programmed Death 1 (PD-1) oraz sposoby leczenia raka z zastosowaniem samych przeciwciał anty-PD-1 lub w połączeniu z innymi środkami immunoterapeutycznymi
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
WO2007117699A2 (en) 2006-04-07 2007-10-18 University Of South Florida Inhibition of shp2/ptpn11 protein tyrosine phosphatase by nsc-87877, nsc-117199 and their analogs
AU2007329352B2 (en) 2006-12-07 2013-01-17 F. Hoffmann-La Roche Ag Phosphoinositide 3-kinase inhibitor compounds and methods of use
WO2008124815A1 (en) 2007-04-10 2008-10-16 University Of South Florida Method of activating nk cells
ES2591281T3 (es) 2007-07-12 2016-11-25 Gitr, Inc. Terapias de combinación que emplean moléculas de enlazamiento a GITR
PE20090678A1 (es) 2007-09-12 2009-06-27 Genentech Inc Combinaciones de compuestos inhibidores de fosfoinositida 3-quinasa y agentes quimioterapeuticos y los metodos de uso
WO2009049098A2 (en) 2007-10-09 2009-04-16 Indiana University Research & Technology Corporation Materials and methods for regulating the activity of phosphatases
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
WO2009135000A2 (en) 2008-04-30 2009-11-05 H. Lee Moffitt Cancer Center And Research Institute, Inc. Inhibition of shp2/ptpn11 protein tyrosine phosphatase by nsc-117199 and analogs
AU2009266873A1 (en) 2008-07-02 2010-01-07 Emergent Product Development Seattle, Llc TGF-beta antagonist multi-target binding proteins
WO2010011666A2 (en) 2008-07-21 2010-01-28 University Of South Florida Indoline scaffold shp-2 inhibitors and cancer treatment method
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
WO2010121212A2 (en) 2009-04-17 2010-10-21 H. Lee Moffit Cancer Center And Research Institute, Inc. Indoline scaffold shp-2 inhibitors and method of treating cancer
BR112012003637A2 (pt) 2009-08-17 2017-04-25 Memorial Sloan Kettering Cancer Center "compostos de ligação de proteína de choque térmico, composições, e métodos para preparar e usar os mesmos"
CA2772613C (en) 2009-09-03 2020-03-10 Schering Corporation Anti-gitr antibodies
GB0919054D0 (en) 2009-10-30 2009-12-16 Isis Innovation Treatment of obesity
HUE029257T2 (en) 2009-12-29 2017-02-28 Aptevo Res And Dev Llc Heterodimer binding proteins and their use
US8637684B2 (en) 2010-05-12 2014-01-28 Wisconsin Alumni Research Foundation Tautomycetin and tautomycetin analog biosynthesis
WO2012041524A1 (en) 2010-10-01 2012-04-05 Max-Delbrück-Centrum Für Molekulare Medizin (Mdc) Hydrazonopyrazolones as protein tyrosine phosphatase inhibitors
ES2764848T3 (es) 2010-12-20 2020-06-04 Incyte Holdings Corp N-(1-(fenilo sustituido)etilo)-9H-purina-6-aminas como inhibidores de PI3K
MX2013010871A (es) 2011-03-23 2014-01-31 Amgen Inc Inhibidores dobles triciclicos fusionados de cdk 4/6 y flt3.
US20130108641A1 (en) 2011-09-14 2013-05-02 Sanofi Anti-gitr antibodies
US9475824B2 (en) 2012-07-20 2016-10-25 Cleave Biosciences, Inc. Fused pyrimidines as inhibitors of p97 complex
WO2014113584A1 (en) 2013-01-16 2014-07-24 Rhode Island Hospital Compositions and methods for the prevention and treatment of osteolysis and osteoporosis
JP6333943B2 (ja) 2013-03-15 2018-05-30 ノバルティス アーゲー 抗体薬物コンジュゲート
AU2014256984B2 (en) 2013-04-26 2019-02-14 Indiana University Research & Technology Corporation Hydroxyindole carboxylic acid based inhibitors for oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2)
EP3016652A4 (en) 2013-07-03 2017-03-08 Indiana University Research and Technology Corporation Shp2 inhibitors and methods of treating autoimmune and/or glomerulonephritis-associated diseases using shp2 inhibitors
ES2699354T3 (es) 2014-01-17 2019-02-08 Novartis Ag Derivados de 1-(triazin-3-il/piridazin-3-il)-piper(-azin)idina 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
WO2015107493A1 (en) 2014-01-17 2015-07-23 Novartis Ag 1 -pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
CN105418632B (zh) 2014-09-19 2020-02-21 上海创诺医药集团有限公司 噻吩并嘧啶类衍生物、其制备方法及其在医药上的应用
WO2016077793A1 (en) 2014-11-14 2016-05-19 Children's Hospital Medical Center Sos1 inhibitors for cancer treatment
TW202204345A (zh) 2015-01-16 2022-02-01 美商通用醫院公司 改善mRNA剪接之化合物
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
WO2016196591A1 (en) 2015-06-01 2016-12-08 Indiana University Research & Technology Corporation Protein tyrosine phosphatases or shp2 inhibitors and uses thereof
WO2016203404A1 (en) 2015-06-19 2016-12-22 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
CN107922388B (zh) 2015-06-19 2020-12-29 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
CA2993312A1 (en) 2015-07-23 2017-01-26 Takeda Pharmaceutical Company Limited 1-substituted 1,2,3,4-tetrahydro-1,7-naphthyridin-8-amine derivatives and their use as ep4 receptor antagonists
WO2017078499A2 (ko) 2015-11-06 2017-05-11 경북대학교 산학협력단 단백질 타이로신 탈인산화효소 억제제를 포함하는 신경염증성 질환의 예방 또는 치료용 조성물
US11008372B2 (en) 2015-11-07 2021-05-18 Board Of Regents, The University Of Texas System Targeting proteins for degradation
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
WO2017156397A1 (en) 2016-03-11 2017-09-14 Board Of Regents, The University Of Texas Sysytem Heterocyclic inhibitors of ptpn11
AU2017274199B2 (en) 2016-05-31 2021-09-23 Board Of Regents, The University Of Texas System Heterocyclic inhibitors of PTPN11
JP6751203B2 (ja) 2016-06-07 2020-09-02 ジャコバイオ ファーマスーティカルズ カンパニー リミテッドJacobio Pharmaceuticals Co., Ltd. Shp2阻害剤として有用な新規複素環式誘導体
TWI806832B (zh) 2016-07-12 2023-07-01 美商銳新醫藥公司 作為異位shp2抑制劑之2,5-雙取代型3-甲基吡嗪及2,5,6-三取代型3-甲基吡嗪
EP3515916B1 (en) 2016-09-22 2023-06-07 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors 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
US10898487B2 (en) 2016-12-22 2021-01-26 Boehringer Ingelheim International Gmbh 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
ES2964956T3 (es) 2017-01-10 2024-04-10 Novartis Ag Combinación farmacéutica que comprende un inhibidor de ALK y un inhibidor de SHP2
BR112019014527A2 (pt) 2017-01-23 2020-02-27 Revolution Medicines, Inc. Compostos de piridina como inibidores de shp2 alostéricos
AU2018210770B2 (en) 2017-01-23 2022-03-24 Revolution Medicines, Inc. Bicyclic compounds as allosteric SHP2 inhibitors
EP3589647A1 (en) 2017-02-28 2020-01-08 Novartis AG Shp inhibitor compositions and uses for chimeric antigen receptor therapy
US20220235013A1 (en) 2017-03-21 2022-07-28 Bayer Pharma Aktiengesellschaft 2-methyl-quinazolines
SG11201908820VA (en) 2017-03-23 2019-10-30 Jacobio Pharmaceuticals Co Ltd Novel heterocyclic derivatives useful as shp2 inhibitors
JP7348071B2 (ja) 2017-05-02 2023-09-20 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 mTOR阻害剤としてのラパマイシン類似体
WO2018218133A1 (en) 2017-05-26 2018-11-29 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
SG11202001282UA (en) 2017-09-07 2020-03-30 Revolution Medicines Inc Shp2 inhibitor compositions and methods for treating cancer
WO2019051469A1 (en) 2017-09-11 2019-03-14 Krouzon Pharmaceuticals, Inc. Octahydrocyclopenta[c]pyrrole allosteric inhibitors of shp2
EP3687997A1 (en) 2017-09-29 2020-08-05 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
MY208632A (en) * 2017-12-21 2025-05-21 Boehringer Ingelheim Int Novel benzylamino substituted pyridopyrimidinones and derivatives as sos1 inhibitors
WO2019152454A1 (en) 2018-01-30 2019-08-08 Research Development Foundation Shp2 inhibitors and methods of use thereof
AU2019222026B2 (en) 2018-02-13 2022-05-12 Shanghai Blueray Biopharma Co., Ltd. Pyrimidine-fused cyclic compound, preparation method therefor and application thereof
EP3755699A1 (en) 2018-02-21 2020-12-30 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
US11466016B2 (en) 2018-03-02 2022-10-11 Otsuka Pharmaceutical Co., Ltd. Pharmaceutical compounds
EP3768680A1 (en) 2018-03-21 2021-01-27 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof
EP3768668B1 (en) 2018-03-21 2024-08-28 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
AU2019239658A1 (en) 2018-03-21 2020-11-12 Suzhou Puhe BioPharma Co., Ltd. SHP2 inhibitors and uses thereof
CN112203689A (zh) 2018-04-10 2021-01-08 锐新医药公司 治疗癌症的shp2抑制剂组合物和方法
CA3097231A1 (en) 2018-04-18 2019-10-24 Bayer Pharma Aktiengesellschaft 2-methyl-aza-quinazolines
MX2020011564A (es) 2018-05-01 2021-01-29 Revolution Medicines Inc Analogos de rapamicina unidos a c26 como inhibidores de mtor.
CN118978535A (zh) 2018-05-01 2024-11-19 锐新医药公司 作为mTOR抑制剂的C40-、C28-及C-32连接的雷帕霉素类似物
CA3099151A1 (en) 2018-05-02 2019-11-07 Navire Pharma, Inc. Substituted heterocyclic inhibitors of ptpn11
US20210230300A1 (en) 2018-06-04 2021-07-29 Bayer Aktiengesellschaft Inhibitors of shp2
JP7174143B2 (ja) 2018-07-24 2022-11-17 大鵬薬品工業株式会社 Shp2活性を阻害するヘテロ二環性化合物
WO2020033286A1 (en) 2018-08-06 2020-02-13 Purdue Research Foundation Novel sesquiterpenoid analogs
MX2021001608A (es) 2018-08-10 2021-07-15 Navire Pharma Inc Inhibidores de ptpn11.
BR112021005082A2 (pt) 2018-09-18 2021-06-08 Nikang Therapeutics, Inc. derivados de anel tricíclico fundido como inibidores de src homologia-2 fosfatase
WO2020063760A1 (en) 2018-09-26 2020-04-02 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
WO2020072656A1 (en) 2018-10-03 2020-04-09 Gilead Sciences, Inc. Imidozopyrimidine derivatives
EP3863636A1 (en) 2018-10-08 2021-08-18 Revolution Medicines, Inc. Shp2 inhibitor compositions for use in treating cancer
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
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
CA3116561C (en) 2018-10-17 2023-09-12 Array Biopharma Inc. Protein tyrosine phosphatase inhibitors
EP3930845A1 (en) 2019-03-01 2022-01-05 Revolution Medicines, Inc. Bicyclic heterocyclyl compounds and uses thereof
WO2020180768A1 (en) 2019-03-01 2020-09-10 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
WO2021074227A1 (en) 2019-10-15 2021-04-22 Bayer Aktiengesellschaft 2-methyl-aza-quinazolines
WO2021092115A1 (en) * 2019-11-08 2021-05-14 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
EP4166555A1 (en) * 2020-06-11 2023-04-19 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Pyridine-pyrimidine derivative, preparation method therefor and pharmaceutical use thereof
WO2022170802A1 (zh) 2021-02-09 2022-08-18 苏州阿尔脉生物科技有限公司 一种作为sos1抑制剂的嘧啶并吡啶酮类衍生物、其制备方法及用途

Also Published As

Publication number Publication date
IL292679A (en) 2022-07-01
EP4620531A2 (en) 2025-09-24
BR112022008858A2 (pt) 2022-09-06
CN116425742A (zh) 2023-07-14
CO2022005968A2 (es) 2022-07-29
CN114901662A (zh) 2022-08-12
AU2020380315A1 (en) 2022-05-26
EP4055017A1 (en) 2022-09-14
US20210139517A1 (en) 2021-05-13
KR20220100903A (ko) 2022-07-18
MX2022005525A (es) 2022-06-08
JP2023500328A (ja) 2023-01-05
TW202128688A (zh) 2021-08-01
CA3156359A1 (en) 2021-05-14
CR20220200A (es) 2022-07-28
US12258366B2 (en) 2025-03-25
US20230365605A1 (en) 2023-11-16
EP4620531A3 (en) 2025-11-26
US11168102B1 (en) 2021-11-09
CL2023000416A1 (es) 2023-07-28
WO2021092115A1 (en) 2021-05-14
PH12022551102A1 (en) 2023-11-20
SA522432518B1 (ar) 2024-07-23

Similar Documents

Publication Publication Date Title
PE20230249A1 (es) Compuestos de heteroarilo biciclicos y usos de estos
CO2022008997A2 (es) Compuestos tricíclicos sustituidos
PE20241068A1 (es) Moduladores de profarmacos de la via de estres integrada
SA522433155B1 (ar) مركبات ثلاثية الحلقة مستبدلة
PE20220140A1 (es) Compuestos triciclicos condensados utiles como agentes anticancerigenos
PE20212303A1 (es) Inhibidores aza-heterobiciclicos de mat2a y metodos de uso en el tratamiento de cancer
CL2019003049A1 (es) Compuestos de heteroarilo bicíclicos 6-6 fusionados y su uso como inhibidores de lats.
PE20221457A1 (es) Degradadores de moleculas pequenas de helios y procedimientos de uso
PE20220762A1 (es) Derivados de acido itaconico y usos de estos en el tratamiento de una enfermedad inflamatoria asociada con una respuesta inmunitaria indeseable
PE20231311A1 (es) Inhibidores de gcn2 y perk quinasas y metodos de uso de los mismos
PE20190656A1 (es) Compuestos de tiazolo-piridina sustituida como inhibidores de malt1
AR083849A1 (es) Antagonistas de mdm2 de espiro-oxindol
PE20241129A1 (es) Inhibidores de parp1 de azetidina y pirrolidina y usos de estos
DOP2018000187A (es) Derivados de pirazolo[1,5-a]pirazin-4-ilo
AR089641A1 (es) COMPUESTOS BICICLICOS Y SUS USOS COMO INHIBIDORES DUALES DE c-SRC/JAK
AR073551A1 (es) Pirimidinas macrociclicas como inhibidores de proteina cinasa
PE20150774A1 (es) Aminoquinolinas como inhibidores de cinasa
PE20220937A1 (es) Compuestos macrociclicos como agonistas de sting y metodos y usos de los mismos
PE20211769A1 (es) Compuestos heteroaromaticos como inhibidores de vanina
PE20240691A1 (es) Compuestos moduladores de gcn2 y usos de los mismos
PE20211447A1 (es) Indazol-3-carboxamidas sustituidas con 5-heteroarilo y preparacion y uso de las mismas
PE20251600A1 (es) Compuestos que contienen heteroatomos y usos de estos
PE20190964A1 (es) Inhibidores de dopamina-b-hidroxilasa penetrantes de la barrera hematoencefalica
UY39181A (es) COMPUESTOS Y COMPOSICIONES PARA INHIBIR LA ACTIVIDAD DE HIF2a Y SUS MÉTODOS DE USO
PE20232047A1 (es) Quinolinas y azaquinolinas como inhibidores de cd38