[go: up one dir, main page]

CR20220200A - Compuestos de heteroarilo bicíclicos y usos de estos - Google Patents

Compuestos de heteroarilo bicíclicos y usos de estos

Info

Publication number
CR20220200A
CR20220200A CR20220200A CR20220200A CR20220200A CR 20220200 A CR20220200 A CR 20220200A CR 20220200 A CR20220200 A CR 20220200A CR 20220200 A CR20220200 A CR 20220200A CR 20220200 A CR20220200 A CR 20220200A
Authority
CR
Costa Rica
Prior art keywords
bicyclic heteroaryl
heteroaryl compounds
compounds
sos1
modulators
Prior art date
Application number
CR20220200A
Other languages
English (en)
Inventor
Arlyn A Tambo-Ong
Adrian Liam Gill
G Leslie Burnett
Anne V Edwards
Yang Liu
William D Thomas
James Joseph Cregg
Severin Thompson
John E Knox
Andreas Buckl
Elena S Koltun
Naing Aay
Micah J Gliedt
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 CR20220200A publication Critical patent/CR20220200A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic 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
    • C07F9/6581—Heterocyclic 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
    • C07F9/6584—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic 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
    • C07F9/6568—Heterocyclic 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
    • C07F9/65685—Heterocyclic 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
    • 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
    • C07B2200/07—Optical isomers

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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

La presente descripción está dirigida a moduladores de SOS1 y su uso en el tratamiento de enfermedades. También se describen composiciones farmacéuticas que los comprenden.
CR20220200A 2019-11-08 2020-11-05 Compuestos de heteroarilo bicíclicos y usos de estos CR20220200A (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
CR20220200A true CR20220200A (es) 2022-07-28

Family

ID=73646489

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20220200A CR20220200A (es) 2019-11-08 2020-11-05 Compuestos de heteroarilo bicíclicos y usos de estos

Country Status (18)

Country Link
US (3) US20210139517A1 (es)
EP (1) EP4055017A1 (es)
JP (1) JP2023500328A (es)
KR (1) KR20220100903A (es)
CN (2) CN114901662A (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 (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023500328A (ja) * 2019-11-08 2023-01-05 レボリューション メディシンズ インコーポレイテッド 二環式ヘテロアリール化合物及びその使用
MX2022015531A (es) * 2020-06-11 2023-01-16 Jiangsu Hengrui Pharmaceuticals Co Ltd Derivado de piridina-pirimidina, metodo de preparacion y uso farmaceutico del mismo.
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
MX2023002371A (es) 2020-08-26 2023-05-19 Haisco Pharmaceuticals Pte Ltd Derivado de nitrilo que actua como inhibidor de la dipeptidil peptidasa 1 y uso del mismo.
CN116209438A (zh) 2020-09-03 2023-06-02 锐新医药公司 使用sos1抑制剂治疗具有shp2突变的恶性疾病
EP4210833A4 (en) 2020-09-11 2024-09-11 Mirati Therapeutics, Inc. CRYSTALLINE FORMS OF A KRAS G12C INHIBITOR
PE20231207A1 (es) 2020-09-15 2023-08-17 Revolution Medicines Inc Derivados indolicos como inhibidores de ras en el tratamiento del cancer
WO2022083657A1 (zh) * 2020-10-20 2022-04-28 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
US20240254117A1 (en) * 2020-12-27 2024-08-01 Shanghai Ringene Biopharma Co., Ltd. Pyrimido-heterocyclic compounds, and preparation method therefor and 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
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
US20240238294A1 (en) 2021-04-09 2024-07-18 Boehringer Ingelheim International Gmbh Anticancer therapy
EP4337678A1 (en) * 2021-05-12 2024-03-20 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
WO2023051628A1 (zh) 2021-09-29 2023-04-06 上海海和药物研究开发股份有限公司 一类具有吡啶并六元环结构的sos1抑制剂
AU2022361380A1 (en) * 2021-10-05 2024-04-11 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
WO2023114954A1 (en) 2021-12-17 2023-06-22 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
WO2023118250A1 (en) * 2021-12-23 2023-06-29 Boehringer Ingelheim International Gmbh 8-aza quinazolines as brain-penetrant sos1-inhibitors
WO2023135260A1 (en) 2022-01-14 2023-07-20 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
CN119095849A (zh) 2022-04-20 2024-12-06 金橘生物科技公司 大环杂环及其用途
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
IL317476A (en) 2022-06-10 2025-02-01 Revolution Medicines Inc Macrocyclic RAS inhibitors
WO2024040131A1 (en) 2022-08-17 2024-02-22 Treeline Biosciences, Inc. Pyridopyrimidine kras inhibitors
WO2024211663A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
WO2024211712A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
WO2024216016A1 (en) 2023-04-14 2024-10-17 Revolution Medicines, Inc. Crystalline forms of a ras inhibitor
US20240352038A1 (en) 2023-04-14 2024-10-24 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
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
WO2024255827A1 (zh) * 2023-06-15 2024-12-19 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
WO2025007000A1 (en) 2023-06-30 2025-01-02 Kumquat Biosciences Inc. Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors
WO2025059046A1 (en) 2023-09-11 2025-03-20 Kumquat Biosciences Inc. Sos1 inhibitors for use in the treatment of philadelphia chromosome positive blood cancers
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

Family Cites Families (238)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
US6352694B1 (en) 1994-06-03 2002-03-05 Genetics Institute, Inc. Methods for inducing a population of T cells to proliferate using agents which recognize TCR/CD3 and ligands which stimulate an accessory molecule on the surface of the T cells
US5858358A (en) 1992-04-07 1999-01-12 The United States Of America As Represented By The Secretary Of The Navy Methods for selectively stimulating proliferation of T cells
US6534055B1 (en) 1988-11-23 2003-03-18 Genetics Institute, Inc. Methods for selectively stimulating proliferation of T cells
US6905680B2 (en) 1988-11-23 2005-06-14 Genetics Institute, Inc. Methods of treating HIV infected subjects
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
ES2108120T3 (es) 1991-05-10 1997-12-16 Rhone Poulenc Rorer Int Compuestos bis arilicos y heteroarilicos mono- y biciclicos que inhiben tirosina quinasa receptora de egf y/o pdgf.
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
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
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
ATE350386T1 (de) 1992-11-13 2007-01-15 Immunex Corp Elk ligand, ein cytokin
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
JPH08503971A (ja) 1993-10-01 1996-04-30 チバ−ガイギー アクチェンゲゼルシャフト ピリミジンアミン誘導体及びその調製のための方法
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
BR9408323A (pt) 1993-12-17 1997-08-19 Sandoz Ag Derivados de rapamicina
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
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
AU2096895A (en) 1994-03-07 1995-09-25 Sugen, Incorporated 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
EP0682027B1 (de) 1994-05-03 1997-10-15 Novartis AG Pyrrolopyrimidinderivate mit antiproliferativer Wirkung
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
EP0817775B1 (en) 1995-03-30 2001-09-12 Pfizer Inc. Quinazoline derivatives
AU711592B2 (en) 1995-04-03 1999-10-14 Novartis Ag Pyrazole derivatives and processes for the preparation thereof
DE69519751T2 (de) 1995-04-20 2001-04-19 Pfizer Inc., New York Arylsulfonamido-substituierte hydroxamsäure derivate als inhibitoren von mmp und tnf
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
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
US5650415A (en) 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds
US5985890A (en) 1995-06-09 1999-11-16 Novartis Ag Rapamycin derivatives
US6140332A (en) 1995-07-06 2000-10-31 Novartis Ag Pyrrolopyrimidines and processes for the preparation thereof
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
EP0888349B1 (en) 1996-01-23 2002-05-22 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
DE19629652A1 (de) 1996-03-06 1998-01-29 Thomae Gmbh Dr K 4-Amino-pyrimidin-Derivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE19608588A1 (de) 1996-03-06 1997-09-11 Thomae Gmbh Dr K Pyrimido [5,4-d]pyrimidine, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE59710417D1 (de) 1996-03-15 2003-08-14 Novartis Ag N-7 HETEROCYCLYL-PYRROLO[ 2,3-d]PYRIMIDINE UND IHRE VERWENDUNG
WO1997038983A1 (en) 1996-04-12 1997-10-23 Warner-Lambert Company Irreversible inhibitors of tyrosine kinases
GB9607729D0 (en) 1996-04-13 1996-06-19 Zeneca Ltd Quinazoline derivatives
DE69734513T2 (de) 1996-06-24 2006-07-27 Pfizer Inc. Phenylamino-substituierte tricyclische derivate zur behandlung hyperproliferativer krankheiten
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
EP0937082A2 (en) 1996-07-12 1999-08-25 Ariad Pharmaceuticals, Inc. Materials and method for treating or preventing pathogenic fungal infection
ATE227283T1 (de) 1996-07-13 2002-11-15 Glaxo Group Ltd Kondensierte heterozyklische verbindungen als protein kinase inhibitoren
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
AR007855A1 (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 medicinay composiciones farmaceuticas que los contienen
KR20000067904A (ko) 1996-07-18 2000-11-25 디. 제이. 우드, 스피겔 알렌 제이 매트릭스 메탈로프로테아제의 포스피네이트계 억제제
US6111090A (en) 1996-08-16 2000-08-29 Schering Corporation Mammalian cell surface antigens; related reagents
ES2308787T3 (es) 1996-08-16 2008-12-01 Schering Corporation Antigenos de superficie de celular de mamiferos; reactivos relacionados.
CA2264284A1 (en) 1996-08-23 1998-02-26 Ralph P. Robinson Arylsulfonylamino hydroxamic acid derivatives
DK0938486T3 (da) 1996-08-23 2008-07-07 Novartis Ag Substituerede pyrrolopyrimidiner og fremgangsmåder til deres fremstilling
JP4205168B2 (ja) 1996-10-02 2009-01-07 ノバルティス アクチエンゲゼルシヤフト ピリミジン誘導体およびその製造法
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
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
ES2224277T3 (es) 1997-01-06 2005-03-01 Pfizer Inc. Derivados de sulfonas ciclicas.
CN1113862C (zh) 1997-02-03 2003-07-09 辉瑞产品公司 芳基磺酰氨基异羟肟酸衍生物
DE69839338T2 (de) 1997-02-05 2008-07-10 Warner-Lambert Company Llc Pyrido (2,3-d) pyrimidine und 4-amino-pyrimidine als inhibitoren der zellulären proliferation
CA2279863A1 (en) 1997-02-07 1998-08-13 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
AU722784B2 (en) 1997-02-11 2000-08-10 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
US6150395A (en) 1997-05-30 2000-11-21 The Regents Of The University Of California Indole-3-carbinol (I3C) derivatives and methods
US6329375B1 (en) 1997-08-05 2001-12-11 Sugen, Inc. Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors
NZ502309A (en) 1997-08-08 2002-02-01 Pfizer Prod Inc Aryloxyarylsulfonylamino hydroxamic acid derivatives and pharmaceutical use
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
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
WO1999040196A1 (en) 1998-02-09 1999-08-12 Genentech, Inc. Novel tumor necrosis factor receptor homolog and nucleic acids encoding the same
DE69940808D1 (de) 1998-03-04 2009-06-10 Bristol Myers Squibb Co Heterocyclen substituierte imidazopyrazine als protein- tyrosin-kinase-inhibitoren
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
JP4528440B2 (ja) 1998-05-29 2010-08-18 スージェン， インク． ピロール置換２−インドリノンタンパク質キナーゼ阻害剤
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
EP1109555A4 (en) 1998-08-31 2001-11-21 Merck & Co Inc NEW ANGIOGENIC INHIBITORS
EP1004578B1 (en) 1998-11-05 2004-02-25 Pfizer Products Inc. 5-oxo-pyrrolidine-2-carboxylic acid hydroxamide derivatives
ES2265929T3 (es) 1999-03-30 2007-03-01 Novartis Ag Derivados de ftalazina para el tratamiento de enfermedades inflamatorias.
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
PT1187918E (pt) 1999-06-07 2006-08-31 Immunex Corp Antagonistas de tek
US6521424B2 (en) 1999-06-07 2003-02-18 Immunex Corporation Recombinant expression of Tek antagonists
JP2003504343A (ja) 1999-07-12 2003-02-04 ジェネンテック・インコーポレーテッド 腫瘍壊死因子リガンド／レセプター相同体による血管形成及び心血管形成の促進と抑制
DE60010098T2 (de) 1999-08-24 2005-03-31 Ariad Gene Therapeutics, Inc., Cambridge 28-epirapaloge
UA72946C2 (uk) 1999-11-05 2005-05-16 Астразенека Аб Похідні хіназоліну як інгібітори васкулярного ендотеліального фактора росту (vegf)
AU1928501A (en) 1999-11-24 2001-06-04 Sugen, Inc. Formulations for pharmaceutical agents ionizable as free acids or free bases
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
KR20030032922A (ko) 2000-02-24 2003-04-26 싸이트 테라피스 인코포레이티드 세포의 동시 자극 및 농축
US7572631B2 (en) 2000-02-24 2009-08-11 Invitrogen Corporation Activation and expansion of T cells
US6797514B2 (en) 2000-02-24 2004-09-28 Xcyte Therapies, Inc. Simultaneous stimulation and concentration of cells
US6867041B2 (en) 2000-02-24 2005-03-15 Xcyte Therapies, Inc. Simultaneous stimulation and concentration of cells
IL151032A0 (en) 2000-02-25 2003-04-10 Immunex Corp Integrin antagonists
US6630500B2 (en) 2000-08-25 2003-10-07 Cephalon, Inc. Selected fused pyrrolocarbazoles
WO2002059110A1 (en) 2000-12-21 2002-08-01 Glaxo Group Limited Pyrimidineamines as angiogenesis modulators
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
US6878714B2 (en) 2001-01-12 2005-04-12 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
US20050026868A1 (en) 2003-07-11 2005-02-03 Metcalf Chester A. Phosphorus-containing macrocycles
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
NZ543654A (en) 2003-05-23 2009-05-31 Wyeth Corp GITR ligand and GITR ligand-related molecules and antibodies and uses thereof
BRPI0412404A (pt) 2003-07-08 2006-09-05 Novartis Ag uso de rapamicina e de derivado da rapamicina para o tratamento da perda óssea
EP1660126A1 (en) 2003-07-11 2006-05-31 Schering Corporation Agonists or antagonists of the clucocorticoid-induced tumour necrosis factor receptor (gitr) or its ligand for the treatment of immune disorders, infections and cancer
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
JP2007518399A (ja) 2003-12-02 2007-07-12 ジェンザイム コーポレイション 肺癌を診断および治療する組成物並びに方法
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
WO2006083289A2 (en) 2004-06-04 2006-08-10 Duke University Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity
UA87153C2 (ru) 2004-08-26 2009-06-25 Пфайзер Инк. Энантиомерно чистые аминогетероарильные соединения как ингибиторы протеинкиназы
WO2006044453A1 (en) 2004-10-13 2006-04-27 Wyeth Analogs of 17-hydroxywortmannin as pi3k inhibitors
EP2343320B1 (en) 2005-03-25 2017-10-25 GITR, Inc. Anti-gitr antibodies and uses thereof
JP5198256B2 (ja) 2005-05-04 2013-05-15 エボテク エージー 縮合複素環式化合物、並びにそれらの組成物及び使用
EP3530736A3 (en) 2005-05-09 2019-11-06 ONO Pharmaceutical Co., Ltd. Human monoclonal antibodies to programmed death 1 (pd-1) and methods for treating cancer using anti-pd-1 antibodies alone or in combination with other immunotherapeutics
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
CA2622870A1 (en) 2005-09-20 2007-03-29 Pfizer Products Inc. Dosage forms and methods of treatment using a tyrosine kinase inhibitor
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
US8591886B2 (en) 2007-07-12 2013-11-26 Gitr, Inc. Combination therapies employing GITR binding molecules
CN101939006B (zh) 2007-09-12 2015-09-16 吉宁特有限公司 磷酸肌醇3-激酶抑制剂化合物与化疗剂的联合以及使用方法
WO2009049098A2 (en) 2007-10-09 2009-04-16 Indiana University Research & Technology Corporation Materials and methods for regulating the activity of phosphatases
CN101909631B (zh) 2007-10-25 2012-09-12 健泰科生物技术公司 制备噻吩并嘧啶化合物的方法
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
CA2729810A1 (en) 2008-07-02 2010-01-07 Emergent Product Development Seattle, Llc Tgf-.beta. antagonist multi-target binding proteins
US9174969B2 (en) 2008-07-21 2015-11-03 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"
CA3067609A1 (en) 2009-09-03 2011-03-10 Merck Sharp & Dohme Corp. Anti-gitr antibodies
GB0919054D0 (en) 2009-10-30 2009-12-16 Isis Innovation Treatment of obesity
AU2010343057B2 (en) 2009-12-29 2017-02-23 Aptevo Research And Development Llc Heterodimer binding proteins and uses thereof
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
TW201249844A (en) 2010-12-20 2012-12-16 Incyte Corp N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
DK2937349T3 (en) 2011-03-23 2017-02-20 Amgen Inc CONDENSED TRICYCLIC DUAL INHIBITORS OF CDK 4/6 AND FLT3
WO2013039954A1 (en) 2011-09-14 2013-03-21 Sanofi Anti-gitr antibodies
MX2015000908A (es) 2012-07-20 2015-09-21 Cleave Biosciences Inc Pirimidinas fusionadas como inhibidores del complejo p97.
WO2014113584A1 (en) 2013-01-16 2014-07-24 Rhode Island Hospital Compositions and methods for the prevention and treatment of osteolysis and osteoporosis
NZ710929A (en) 2013-03-15 2018-02-23 Novartis Ag Antibody drug conjugates
CN105142634B (zh) 2013-04-26 2020-06-12 美国印第安纳大学研究和技术公司 包含Src同源-2结构域的致癌性蛋白酪氨酸磷酸酶-2(SHP2)的基于羟基吲哚羧酸的抑制剂
WO2015003094A2 (en) 2013-07-03 2015-01-08 Indiana University Research & Technology Corporation Shp2 inhibitors and methods of treating autoimmune and/or glomerulonephritis-associated diseases using shp2 inhibitors
EP3094629B1 (en) 2014-01-17 2018-08-22 Novartis AG 1-(triazin-3-yl/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions thereof for inhibiting the activity of shp2
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
CN105899491B (zh) 2014-01-17 2019-04-02 诺华股份有限公司 用于抑制shp2活性的1-哒嗪-/三嗪-3-基-哌(-嗪)/啶/吡咯烷衍生物及其组合物
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
MX2017009295A (es) 2015-01-16 2018-03-07 Massachusetts Gen Hospital Compuestos para mejorar el empalme del acido ribonucleico mensajero (arnm).
US20180121597A1 (en) 2015-05-22 2018-05-03 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
ES2741746T3 (es) 2015-06-19 2020-02-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
ES2824576T3 (es) 2015-06-19 2021-05-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
US10287266B2 (en) 2015-06-19 2019-05-14 Novartis Ag Compounds and compositions for inhibiting the activity of SHP2
WO2017014323A1 (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
WO2017100279A1 (en) 2015-12-09 2017-06-15 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
CA3024706A1 (en) 2016-05-31 2017-12-07 Board Of Regents, The 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.
IL264186B2 (en) 2016-07-12 2024-08-01 Revolution Medicines Inc 2,5-dimutomers of 3-methylpyrazines and 2,5,6-dimutomers of 3-methylpyrazines as allosteric SHP2 inhibitors
EP3515916B1 (en) 2016-09-22 2023-06-07 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
TWI848901B (zh) 2016-10-24 2024-07-21 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
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
US20190343836A1 (en) 2017-01-10 2019-11-14 Novartis Ag Pharmaceutical combination comprising an alk inhibitor and a shp2 inhibitor
MX2019008695A (es) 2017-01-23 2019-09-11 Revolution Medicines Inc Compuestos biciclicos como inhibidores alostericos de shp2.
RU2019126455A (ru) 2017-01-23 2021-02-24 Революшн Медсинз, Инк. Пиридиновые соединения в качестве аллостерических ингибиторов shp2
WO2018160731A1 (en) 2017-02-28 2018-09-07 Novartis Ag Shp inhibitor compositions and uses for chimeric antigen receptor therapy
CA3056970A1 (en) 2017-03-21 2018-09-27 Bayer Pharma Aktiengesellschaft 2-methyl-quinazolines
KR20210130254A (ko) 2017-03-23 2021-10-29 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체
KR20200012876A (ko) 2017-05-02 2020-02-05 레볼루션 메디슨즈, 인크. mTOR 억제제로서의 파라마이신 유사체
EP3630770B1 (en) 2017-05-26 2024-08-28 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
TWI852912B (zh) 2017-09-07 2024-08-21 美商銳新醫藥公司 Shp2抑制劑組合物以及治療癌症的方法
CN111201223B (zh) 2017-09-11 2024-07-09 克鲁松制药公司 SHP2的八氢环戊二烯并[c]吡咯别构抑制剂
EP3687997A1 (en) 2017-09-29 2020-08-05 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
US10829487B2 (en) * 2017-12-21 2020-11-10 Boehringer Ingelheim International Gmbh 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
EP3753941B1 (en) 2018-02-13 2024-05-01 Shanghai Blueray Biopharma Co., Ltd. Pyrimidine-fused cyclic compound, preparation method therefor and application thereof
US20200392161A1 (en) 2018-02-21 2020-12-17 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
AU2019226480B2 (en) 2018-03-02 2022-12-15 Otsuka Pharmaceutical Co., Ltd. Pharmaceutical compounds
US10561655B2 (en) 2018-03-21 2020-02-18 Synblia Therapeutics, Inc. SHP2 inhibitors and uses thereof
MX2020009782A (es) 2018-03-21 2021-01-20 Relay Therapeutics Inc Inhibidores de la fosfatasa shp2 y métodos para su uso.
EP3768680A1 (en) 2018-03-21 2021-01-27 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use 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
CN118894869A (zh) 2018-05-01 2024-11-05 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
EP3788050B1 (en) 2018-05-01 2024-08-28 Revolution Medicines, Inc. C26-linked rapamycin analogs as mtor inhibitors
IL278297B2 (en) 2018-05-02 2023-12-01 Navire Pharma Inc Substituted heterocyclic inhibitors of ptpn11
EP3801613A1 (en) 2018-06-04 2021-04-14 Bayer Aktiengesellschaft Inhibitors of shp2
AU2019309987B2 (en) 2018-07-24 2022-08-18 Otsuka Pharmaceutical Co., Ltd. Heterobicyclic compounds for inhibiting the activity of shp2
US11518770B2 (en) 2018-08-06 2022-12-06 Purdue Research Foundation Sesquiterpenoid analogs
PL3833670T3 (pl) 2018-08-10 2024-08-19 Navire Pharma, Inc. Pochodne 6-(4-amino-3-metylo-2-oksa-8-azaspiro[4.5]dekan-8-ylo)-3-(2,3-dichlorofenylo)-2-metylopirymidyn-4(3h)-onu oraz powiązane związki jako inhibitory ptpn11 (shp2) do leczenia raka
AU2019344897B2 (en) 2018-09-18 2024-01-18 Nikang Therapeutics, Inc. Tri-substituted heteroaryl derivatives AS SRC homology-2 phosphatase inhibitors
US20210393623A1 (en) 2018-09-26 2021-12-23 Jacobio Pharmaceuticals Co., Ltd. Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors
US11179397B2 (en) 2018-10-03 2021-11-23 Gilead Sciences, Inc. Imidazopyrimidine derivatives
CN113473990A (zh) 2018-10-08 2021-10-01 锐新医药公司 用于治疗癌症的shp2抑制剂组合物
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
EP3867238B1 (en) 2018-10-17 2023-06-07 Array BioPharma Inc. Protein tyrosine phosphatase inhibitors
CN113767100A (zh) 2019-03-01 2021-12-07 锐新医药公司 双环杂芳基化合物及其用途
CN113727758A (zh) 2019-03-01 2021-11-30 锐新医药公司 双环杂环基化合物及其用途
CN115315424A (zh) 2019-10-15 2022-11-08 拜耳公司 2-甲基-氮杂-喹唑啉
JP2023500328A (ja) * 2019-11-08 2023-01-05 レボリューション メディシンズ インコーポレイテッド 二環式ヘテロアリール化合物及びその使用
MX2022015531A (es) * 2020-06-11 2023-01-16 Jiangsu Hengrui Pharmaceuticals Co Ltd Derivado de piridina-pirimidina, metodo de preparacion y uso farmaceutico del mismo.
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
BR112022008858A2 (pt) 2022-09-06
PH12022551102A1 (en) 2023-11-20
TW202128688A (zh) 2021-08-01
IL292679A (en) 2022-07-01
EP4055017A1 (en) 2022-09-14
AU2020380315A1 (en) 2022-05-26
CA3156359A1 (en) 2021-05-14
US20210139517A1 (en) 2021-05-13
CN114901662A (zh) 2022-08-12
PE20230249A1 (es) 2023-02-07
MX2022005525A (es) 2022-06-08
CO2022005968A2 (es) 2022-07-29
KR20220100903A (ko) 2022-07-18
JP2023500328A (ja) 2023-01-05
US12258366B2 (en) 2025-03-25
US20230365605A1 (en) 2023-11-16
CN116425742A (zh) 2023-07-14
US11168102B1 (en) 2021-11-09
CL2023000416A1 (es) 2023-07-28
SA522432518B1 (ar) 2024-07-23
WO2021092115A1 (en) 2021-05-14

Similar Documents

Publication Publication Date Title
CO2022005968A2 (es) Compuestos de heteroarilo bicíclicos y usos de estos
MX2021010319A (es) Compuestos biciclicos de heteroarilo y usos de estos.
MX2021010323A (es) Compuestos bicíclicos de heterociclilo y usos de este.
CO2020005887A2 (es) Compuestos policíclicos como inhibidores alostéricos de shp2
CO2020003714A2 (es) Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostéricos
DOP2019000005A (es) 3-metil pirazinas 2,5-disustituidas y 3-metil pirazinas 2,5,6-trisustituidas como inhibidores alostéricos de shp2
ECSP20040257A (es) Nuevas piridopirimidinonas sustituidas con bencilamino y derivados como inhibidores de sos1
ECSP20033467A (es) Compuestos macrocíclicos para tratar enfermedades
CO2022010547A2 (es) Compuestos y usos de los mismos
CO2018014339A2 (es) Formas sólidas cristalinas de un inhibidor de bet
UY36371A (es) Compuestos de indolcarboxamida inhibidores de quinasas tipo btk y tipo tec
MX2018001756A (es) Benzimidazoles sustituidos, su preparacion y su uso como productos farmaceuticos.
CO2022018636A2 (es) Moduladores de il-17a
CO2022000749A2 (es) Inhibidores de monoacilglicerol lipasa (magl) heterocíclicos
MX2021004566A (es) Compuestos terapeuticos.
UY31990A (es) Nuevos derivados
CO2022016899A2 (es) Moduladores de il-17a
DOP2016000064A (es) Derivados de fenilalanina sustituidos
CL2021003228A1 (es) Compuestos tricíclicos y su uso
MX2022013396A (es) Compuestos de tetrahidroisoquinolina como activadores de nrf2.
UY37729A (es) NUEVOS COMPUESTOS QUE INHIBEN LA ACTIVIDAD DE Nav1.7
CL2019002480A1 (es) Derivados de pirazol como inhibidores de bromodominio.
BR112021009616A8 (pt) Composição cicatrizante que compreende água eletrolisada e máscara de aplicação cutânea
CL2022001138A1 (es) Anticuerpos tmem219 y usos terapéuticos de los mismos
CL2021000282A1 (es) Inhibidores de ckd8/19