MX2022005357A - Inhibidores de ras. - Google Patents

Inhibidores de ras.

Info

Publication number
MX2022005357A
MX2022005357A MX2022005357A MX2022005357A MX2022005357A MX 2022005357 A MX2022005357 A MX 2022005357A MX 2022005357 A MX2022005357 A MX 2022005357A MX 2022005357 A MX2022005357 A MX 2022005357A MX 2022005357 A MX2022005357 A MX 2022005357A
Authority
MX
Mexico
Prior art keywords
ras inhibitors
cancers
treatment
pharmaceutical compositions
protein complexes
Prior art date
Application number
MX2022005357A
Other languages
English (en)
Inventor
James Aggen
Elena S Koltun
Christopher Semko
Jennifer Pitzen
Andreas Buckl
G Leslie Burnett
John E Knox
Adrian L Gill
James Cregg
Anne V Edwards
Micah James 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 MX2022005357A publication Critical patent/MX2022005357A/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/504Pyridazines; Hydrogenated pyridazines forming part of bridged ring 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings

Landscapes

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

Abstract

La descripción presenta compuestos macrocíclicos y composiciones farmacéuticas y complejos proteicos de los mismos, capaces de inhibir las proteínas Ras, y sus usos en el tratamiento de cánceres.
MX2022005357A 2019-11-04 2020-11-04 Inhibidores de ras. MX2022005357A (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201962930406P 2019-11-04 2019-11-04
US201962951562P 2019-12-20 2019-12-20
US202063000355P 2020-03-26 2020-03-26
US202063043523P 2020-06-24 2020-06-24
PCT/US2020/058817 WO2021091967A1 (en) 2019-11-04 2020-11-04 Ras inhibitors

Publications (1)

Publication Number Publication Date
MX2022005357A true MX2022005357A (es) 2022-06-02

Family

ID=73646455

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2022005357A MX2022005357A (es) 2019-11-04 2020-11-04 Inhibidores de ras.

Country Status (16)

Country Link
US (1) US11739074B2 (es)
EP (1) EP4054720A1 (es)
JP (1) JP2022553857A (es)
KR (1) KR20220109406A (es)
CN (2) CN114901366A (es)
AU (1) AU2020379731A1 (es)
BR (1) BR112022008534A2 (es)
CA (1) CA3159559A1 (es)
CL (1) CL2023000973A1 (es)
CO (1) CO2022006030A2 (es)
CR (1) CR20220240A (es)
IL (1) IL292642A (es)
MX (1) MX2022005357A (es)
PE (1) PE20221277A1 (es)
TW (1) TW202132315A (es)
WO (1) WO2021091967A1 (es)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3030167A1 (en) 2016-07-12 2018-01-18 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
IL296456A (en) 2017-01-23 2022-11-01 Revolution Medicines Inc Bicyclics as allosteric shp2 inhibitors
BR112019014527A2 (pt) 2017-01-23 2020-02-27 Revolution Medicines, Inc. Compostos de piridina como inibidores de shp2 alostéricos
SG11202002941WA (en) 2017-10-12 2020-04-29 Revolution Medicines Inc Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors
AU2018385713A1 (en) 2017-12-15 2020-06-18 Revolution Medicines, Inc. Polycyclic compounds as allosteric SHP2 inhibitors
EP3790551A4 (en) 2018-05-07 2022-03-09 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
CN114615981B (zh) 2019-08-29 2024-04-12 米拉蒂治疗股份有限公司 Kras g12d抑制剂
US11890285B2 (en) 2019-09-24 2024-02-06 Mirati Therapeutics, Inc. Combination therapies
TW202132315A (zh) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ras 抑制劑
MX2022005359A (es) 2019-11-04 2022-06-02 Revolution Medicines Inc Inhibidores de ras.
BR112022008535A2 (pt) 2019-11-04 2022-08-09 Revolution Medicines Inc Composto, composição farmacêutica, métodos para tratar câncer e um distúrbio relativo à proteína ras
KR20220130126A (ko) 2019-12-20 2022-09-26 미라티 테라퓨틱스, 인크. Sos1 억제제
JP2023530351A (ja) * 2020-06-18 2023-07-14 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 Ras阻害剤への獲得耐性を遅延させる、防止する、及び、治療する方法
CN117683049A (zh) 2020-09-15 2024-03-12 锐新医药公司 作为ras抑制剂以治疗癌症的吲哚衍生物
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
MX2023008460A (es) 2021-01-19 2023-09-12 Lupin Ltd Combinaciones farmacéuticas de inhibidores de sos1 para el tratamiento y/o prevención del cáncer.
AU2022270116A1 (en) 2021-05-05 2023-12-21 Revolution Medicines, Inc. Ras inhibitors
AU2022268962A1 (en) 2021-05-05 2023-12-14 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
EP4334324A1 (en) 2021-05-05 2024-03-13 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
IL308771A (en) 2021-05-25 2024-01-01 Revolution Medicines Inc Methods of inhibiting RAS
WO2023015559A1 (en) * 2021-08-13 2023-02-16 Nutshell Biotech (Shanghai) Co., Ltd. Macrocycle compounds as inhibitors of ras
AR126854A1 (es) * 2021-08-27 2023-11-22 Hoffmann La Roche Compuestos macrocíclicos para el tratamiento de cáncer
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023086341A1 (en) * 2021-11-09 2023-05-19 Biomea Fusion, Inc. Inhibitors of kras
WO2023114954A1 (en) 2021-12-17 2023-06-22 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
TW202330553A (zh) * 2022-01-10 2023-08-01 美商銳新醫藥公司 Ras抑制劑
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
TW202400607A (zh) * 2022-04-25 2024-01-01 美商翰森生物有限責任公司 環狀化合物、製備方法及其醫藥用途
WO2023232776A1 (en) * 2022-06-01 2023-12-07 F. Hoffmann-La Roche Ag Haloindole macrocyclic compounds for the treatment of cancer
WO2023240263A1 (en) * 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2024008834A1 (en) * 2022-07-08 2024-01-11 F. Hoffmann-La Roche Ag Macrocycle compounds useful as kras inhibitors
WO2024060966A1 (zh) * 2022-09-19 2024-03-28 杭州阿诺生物医药科技有限公司 一种pan-KRAS抑制剂化合物
WO2024067857A1 (zh) * 2022-09-29 2024-04-04 南京明德新药研发有限公司 大环衍生物及其应用
WO2024102421A2 (en) 2022-11-09 2024-05-16 Revolution Medicines, Inc. Compounds, complexes, and methods for their preparation and of their use

Family Cites Families (320)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE92501T1 (de) 1984-10-04 1993-08-15 Sandoz Ag Monoklonale antikoerper gegen zyklosporine.
EP0194972B1 (en) 1985-03-11 1992-07-29 Sandoz Ag Novel cyclosporins
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
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
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
EP0393934B1 (en) 1989-04-15 1994-11-02 Nippon Chemiphar Co., Ltd. Novel peptides, and antidementia agents containing the same
US5112946A (en) 1989-07-06 1992-05-12 Repligen Corporation Modified pf4 compositions and methods of use
PT98990A (pt) 1990-09-19 1992-08-31 American Home Prod Processo para a preparacao de esteres de acidos carboxilicos de rapamicina
US5892112A (en) 1990-11-21 1999-04-06 Glycomed Incorporated Process for preparing synthetic matrix metalloprotease inhibitors
US5120842A (en) 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5100883A (en) 1991-04-08 1992-03-31 American Home Products Corporation Fluorinated esters of rapamycin
US5118678A (en) 1991-04-17 1992-06-02 American Home Products Corporation Carbamates of rapamycin
EP0584222B1 (en) 1991-05-10 1997-10-08 Rhone-Poulenc Rorer International (Holdings) Inc. Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
US5118677A (en) 1991-05-20 1992-06-02 American Home Products Corporation Amide esters of rapamycin
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
US5151413A (en) 1991-11-06 1992-09-29 American Home Products Corporation Rapamycin acetals as immunosuppressant and antifungal agents
GB9125660D0 (en) 1991-12-03 1992-01-29 Smithkline Beecham Plc Novel compound
GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
EP0562853B1 (en) 1992-03-27 1996-06-05 American Home Products Corporation 29-Demethoxyrapamycin for inducing immunosuppression
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
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
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
DK0669929T3 (da) 1992-11-13 2007-01-29 Immunex Corp Elk-ligand, et 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
WO1995008548A1 (en) 1993-09-20 1995-03-30 The Leland Stanford Junior University Recombinant production of novel polyketides
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
SK78196A3 (en) 1993-12-17 1997-02-05 Sandoz Ag Rapamycin demethoxy-derivatives, preparation method thereof and pharmaceutical agent containing them
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
AU2096895A (en) 1994-03-07 1995-09-25 Sugen, Incorporated Receptor tyrosine kinase inhibitors for inhibiting cell proliferative disorders and compositions thereof
IL112873A (en) 1994-03-08 2005-03-20 Wyeth Corp Rapamycin-fkbp12 binding proteins, their isolation and their use
CA2189028A1 (en) 1994-04-15 1995-10-26 Gary M. Fox Hek5, hek7, hek8, hek11, new eph-like receptor protein tyrosine kinases
ATE159257T1 (de) 1994-05-03 1997-11-15 Ciba Geigy Ag Pyrrolopyrimidinderivate mit antiproliferativer wirkung
GB9410142D0 (en) 1994-05-20 1994-07-06 Univ Warwick Carbapenems
US7175843B2 (en) 1994-06-03 2007-02-13 Genetics Institute, Llc Methods for selectively stimulating proliferation of T cells
US6303769B1 (en) 1994-07-08 2001-10-16 Immunex Corporation Lerk-5 dna
US5919905A (en) 1994-10-05 1999-07-06 Immunex Corporation Cytokine designated LERK-6
GB9524630D0 (en) 1994-12-24 1996-01-31 Zeneca Ltd Chemical compounds
US6057124A (en) 1995-01-27 2000-05-02 Amgen Inc. Nucleic acids encoding ligands for HEK4 receptors
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
ES2332984T3 (es) 1995-03-30 2010-02-16 Pfizer Products Inc. Derivados de quinazolinas.
CA2214086C (en) 1995-04-03 2008-07-29 Novartis Ag Pyrazole derivatives and processes for the preparation thereof
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
US7067318B2 (en) 1995-06-07 2006-06-27 The Regents Of The University Of Michigan Methods for transfecting T cells
US6692964B1 (en) 1995-05-04 2004-02-17 The United States Of America As Represented By The Secretary Of The Navy Methods for transfecting T cells
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5650415A (en) 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
CN1124276C (zh) 1995-06-09 2003-10-15 诺瓦蒂斯有限公司 雷帕霉素衍生物
US5624677A (en) 1995-06-13 1997-04-29 Pentech Pharmaceuticals, Inc. Controlled release of drugs delivered by sublingual or buccal administration
US6124453A (en) 1995-07-04 2000-09-26 Novartis Ag Macrolides
BR9609617B1 (pt) 1995-07-06 2010-07-27 derivados de 7h-pirrol[2,3-d]pirimidina, e composição farmacêutica.
AR004010A1 (es) 1995-10-11 1998-09-30 Glaxo Group Ltd Compuestos heterociclicos
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
ATE225343T1 (de) 1995-12-20 2002-10-15 Hoffmann La Roche Matrix-metalloprotease inhibitoren
ES2177925T3 (es) 1996-01-23 2002-12-16 Novartis Ag Pirrolopirimidinas y procedimientos para su preparacion.
JP3406763B2 (ja) 1996-01-30 2003-05-12 東レ・ダウコーニング・シリコーン株式会社 シリコーンゴム組成物
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
GB9603097D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline compounds
DE19629652A1 (de) 1996-03-06 1998-01-29 Thomae Gmbh Dr K 4-Amino-pyrimidin-Derivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE19608588A1 (de) 1996-03-06 1997-09-11 Thomae Gmbh Dr K Pyrimido [5,4-d]pyrimidine, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
KR20000064601A (ko) 1996-03-15 2000-11-06 한스 루돌프 하우스, 헨리테 브룬너, 베아트리체 귄터 신규의n-7-헤테로시클릴피롤로[2,3-d]피리딘및�그의용도
SI0892789T2 (sl) 1996-04-12 2010-03-31 Warner Lambert Co Ireverzibilni inhibitorji tirozin kinaz
GB9607729D0 (en) 1996-04-13 1996-06-19 Zeneca Ltd Quinazoline derivatives
WO1997049688A1 (en) 1996-06-24 1997-12-31 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
EA001744B1 (ru) 1996-07-05 2001-08-27 Байотика Текнолоджи Лимитед (Gb) Новые эритромицины и способы их получения
US6258823B1 (en) 1996-07-12 2001-07-10 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
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
PT912559E (pt) 1996-07-13 2003-03-31 Glaxo Group Ltd Compostos heterociclicos fundidos como inibidores de proteina tirosina quinase
BR9710362A (pt) 1996-07-13 1999-08-17 Glaxo Group Ltd Composto formula-ao farmaceutica utiliza-ao de um composto processos de tratamento de um ser humano ou animal sofrendo de uma mediada por atividade anormal de cinase de proteina tirosina e para a prepara-ao de um composto
BR9710381A (pt) 1996-07-18 1999-08-17 Pfizer Inibidores de metaloproteases de matriz - base de fosfinato
EP1947183B1 (en) 1996-08-16 2013-07-17 Merck Sharp & Dohme Corp. Mammalian cell surface antigens; related reagents
US6111090A (en) 1996-08-16 2000-08-29 Schering Corporation Mammalian cell surface antigens; related reagents
JP2000501423A (ja) 1996-08-23 2000-02-08 ファイザー インク. アリールスルホニルアミノヒドロキサム酸誘導体
JP4242928B2 (ja) 1996-08-23 2009-03-25 ノバルティス アクチエンゲゼルシャフト 置換ピロロピリミジンおよびその製造方法
SE9603465D0 (sv) 1996-09-23 1996-09-23 Astra Ab New compounds
US6251911B1 (en) 1996-10-02 2001-06-26 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
AU4779897A (en) 1996-10-02 1998-04-24 Novartis Ag Fused pyrazole derivatives and processes for their preparation
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
GB9621757D0 (en) 1996-10-18 1996-12-11 Ciba Geigy Ag Phenyl-substituted bicyclic heterocyclyl derivatives and their use
US6077864A (en) 1997-01-06 2000-06-20 Pfizer Inc. Cyclic sulfone derivatives
PL335027A1 (en) 1997-02-03 2000-03-27 Pfizer Prod Inc Derivatives of arylsulphonylamino hydroxamic acid
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
BR9807824A (pt) 1997-02-07 2000-03-08 Pfizer Derivados de n-hidróxi-beta-sulfonil-propionamida e seu uso como inibidores de metaloproteinases de matriz
IL131123A0 (en) 1997-02-11 2001-01-28 Pfizer Arylsulfonyl hydroxamic acid derivatives
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
US6902913B2 (en) 1997-04-30 2005-06-07 Kosan Biosciences, Inc. Recombinant narbonolide polyketide synthase
US6150395A (en) 1997-05-30 2000-11-21 The Regents Of The University Of California Indole-3-carbinol (I3C) derivatives and methods
AU8689298A (en) 1997-08-05 1999-03-01 Sugen, Inc. Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors
SK1362000A3 (en) 1997-08-08 2000-10-09 Pfizer Prod Inc Aryloxyarylsulfonylamino hydroxamic acid derivatives
JP2001520039A (ja) 1997-10-21 2001-10-30 ヒューマン ジノーム サイエンシーズ, インコーポレイテッド ヒト腫瘍壊死因子レセプター様タンパク質、tr11,tr11sv1およびtr11sv2
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
US6153383A (en) 1997-12-09 2000-11-28 Verdine; Gregory L. Synthetic transcriptional modulators and uses thereof
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
GB9800575D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
WO1999040196A1 (en) 1998-02-09 1999-08-12 Genentech, Inc. Novel tumor necrosis factor receptor homolog and nucleic acids encoding the same
ATE430149T1 (de) 1998-03-04 2009-05-15 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
WO1999061055A1 (en) 1998-05-22 1999-12-02 The Board Of Trustees Of The Leland Stanford Junior University Bifunctional molecules and therapies based thereon
AU759226B2 (en) 1998-05-29 2003-04-10 Sugen, Inc. Pyrrole substituted 2-indolinone protein kinase inhibitors
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
CA2341409A1 (en) 1998-08-31 2000-03-09 Merck And Co., Inc. Novel angiogenesis inhibitors
KR20010085877A (ko) 1998-10-02 2001-09-07 추후제출 폴리케타이드 합성 효소와 그 재조합 dna 구성물
US6686454B1 (en) 1998-10-09 2004-02-03 Isotechnika, Inc. Antibodies to specific regions of cyclosporine related compounds
DE69915004T2 (de) 1998-11-05 2004-09-09 Pfizer Products Inc., Groton 5-Oxo-pyrrolidine-2-Carbonsäure-Hydroxamidderivate
AU2876300A (en) 1999-02-09 2000-08-29 Board Of Trustees Of The Leland Stanford Junior University Methods to mediate polyketide synthase module effectiveness
CN1221262C (zh) 1999-03-30 2005-10-05 诺瓦提斯公司 治疗炎性疾病的酞嗪衍生物
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
US6521424B2 (en) 1999-06-07 2003-02-18 Immunex Corporation Recombinant expression of Tek antagonists
AU783960B2 (en) 1999-06-07 2006-01-05 Immunex Corporation Tek antagonists
ES2295040T3 (es) 1999-07-12 2008-04-16 Genentech, Inc. Promocion o inhibicion de la angiogenesis y cardiovascularizacion mediante homologos del ligando / receptor del factor de necrosis del tumor.
IL147803A0 (en) 1999-08-24 2002-08-14 Ariad Gene Therapeutics Inc 28-epirapalogs
UA72946C2 (uk) 1999-11-05 2005-05-16 Астразенека Аб Похідні хіназоліну як інгібітори васкулярного ендотеліального фактора росту (vegf)
GB9927191D0 (en) 1999-11-17 2000-01-12 Angeletti P Ist Richerche Bio Methods and means for regulation of gene expression
WO2001036612A1 (en) 1999-11-19 2001-05-25 The Board Of Trustees Of The Leland Stanford Junior University Bifunctional molecules and their use in the disruption of protein-protein interactions
US7220552B1 (en) 1999-11-19 2007-05-22 The Board Of Trustees Of The Leland Stanford Junior University Bifunctional molecules and their use in the disruption of protein-protein interactions
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
EP1255840A2 (en) 2000-02-08 2002-11-13 Norges Teknisk Naturvitenskapelige Universitet Gene cluster encoding a nystatin polyketide synthase and its manipulation and utility
AU2001243288B2 (en) 2000-02-24 2005-11-24 Life Technologies Corporation Simultaneous stimulation and concentration of cells
US6867041B2 (en) 2000-02-24 2005-03-15 Xcyte Therapies, Inc. Simultaneous stimulation and concentration of cells
US7572631B2 (en) 2000-02-24 2009-08-11 Invitrogen Corporation Activation and expansion of T cells
US6797514B2 (en) 2000-02-24 2004-09-28 Xcyte Therapies, Inc. Simultaneous stimulation and concentration of cells
NZ521437A (en) 2000-02-25 2004-04-30 Immunex Corp Integrin antagonists suitable as inhibitors of angiogenesis
MXPA02000823A (es) 2000-05-23 2002-07-30 Vertex Pharma Inhibidores de caspasa y uso de los mismos.
US7176037B2 (en) 2000-07-13 2007-02-13 The Scripps Research Institute Labeled peptides, proteins and antibodies and processes and intermediates useful for their preparation
US6630500B2 (en) 2000-08-25 2003-10-07 Cephalon, Inc. Selected fused pyrrolocarbazoles
US7105530B2 (en) 2000-12-21 2006-09-12 Smithkline Beecham Corporation Pyrimidineamines as angiogenesis modulators
US20020147198A1 (en) 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine derivatives and methods of use
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US20030153053A1 (en) 2001-08-06 2003-08-14 Ralph Reid Methods for altering polyketide synthase genes
US6809077B2 (en) 2001-10-12 2004-10-26 Enanta Pharmaceuticals, Inc. Cyclosporin analogs for the treatment of autoimmune diseases
US6987090B2 (en) 2002-05-09 2006-01-17 Lg Household & Health Care Ltd. Use of 3-position cyclosporin derivatives for hair growth
US7307088B2 (en) 2002-07-09 2007-12-11 Amgen Inc. Substituted anthranilic amide derivatives and methods of use
TWI329112B (en) 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
US7012065B2 (en) 2003-02-07 2006-03-14 Enanta Pharmaceuticals, Inc. Cyclosporins for the treatment of immune disorders
EP1477563A3 (en) 2003-05-16 2004-11-24 Wyeth Cloning genes from streptomyces cyaneogriseus subsp.noncyanogenus for biosynthesis of antibiotics and methods of use
BRPI0410785A (pt) 2003-05-23 2006-06-20 Wyeth Corp molécula de ácido nucleico isolada, célula hospedeira, animal transgênico não humano, proteìna isolada, oligonucleotìdeo anti-sentido, molécula de sirna, anticorpo isolado, métodos de triagem quanto aos compostos de teste capazes de inibir, de intensificar ou imitar a interação do gitrl com o gitr, para diagnosticar doenças, para tratar um paciente em risco ou diagnosticado com uma doença, para induzir e para inibir a proliferação de uma população celular contendo células t efetoras, de bloquear a supressão e de supressão de uma população celular que inclua células t efetoras na presença de células t reguladoras cd4+cd25+, e para tratar uma doença, composição farmacêutica, e, adjuvante de vacina
US20060173033A1 (en) 2003-07-08 2006-08-03 Michaela Kneissel Use of rapamycin and rapamycin derivatives for the treatment of bone loss
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
AR045134A1 (es) 2003-07-29 2005-10-19 Smithkline Beecham Plc Compuesto de 1h - imidazo [4,5-c] piridin-ilo, composicion farmaceutica que lo comprende, proceso para prepararla, su uso para preparar dicha composicion farmaceutica, combinacion farmaceutica, uso de la combinacion farmaceutica para la preparacion de un medicamento, procedimientos para preparar dic
EP1660458B1 (en) 2003-08-15 2012-01-25 Novartis AG 2, 4-pyrimidinediamines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders
EP1692318A4 (en) 2003-12-02 2008-04-02 Genzyme Corp COMPOSITIONS AND METHODS FOR DIAGNOSIS AND TREATMENT OF 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
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
ES2341351T3 (es) 2004-08-26 2010-06-18 Pfizer, Inc. Compuestos de aminoheteroarilo enantiomericamente puros como inhibidores de proteina cinasas.
PE20060608A1 (es) 2004-10-13 2006-08-22 Wyeth Corp Analogos de 17-hidroxiwortmanina como inhibidores de pi3k
PT2343320T (pt) 2005-03-25 2018-01-23 Gitr Inc Anticorpos anti-gitr e as suas utilizações
CA3151350A1 (en) 2005-05-09 2006-11-16 E. R. Squibb & Sons, L.L.C. 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
MX2008001041A (es) 2005-09-20 2008-03-19 Pfizer Prod Inc Formas farmaceuticas y metodos de tratamiento que usan un inhibidor de la tirosinacinasa.
WO2007133822A1 (en) 2006-01-19 2007-11-22 Genzyme Corporation Gitr antibodies for the treatment of cancer
BRPI0708299A2 (pt) 2006-02-27 2011-05-24 Univ Leland Stanford Junior composições e métodos para o transporte de moléculas com propriedades melhoradas de liberação através de barreiras biológicas
US20070203168A1 (en) 2006-02-28 2007-08-30 Zhao Jonathon Z Isomers of rapamycin and 42-Epi-rapamycin, methods of making and using the same
US8987474B2 (en) 2006-04-07 2015-03-24 University Of South Florida Inhibition of Shp2/PTPN11 protein tyrosine phosphatase by NSC-87877, NSC-117199 and their analogs
US7601852B2 (en) 2006-05-11 2009-10-13 Kosan Biosciences Incorporated Macrocyclic kinase inhibitors
EP2114949A1 (en) 2006-12-07 2009-11-11 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
DK2175884T3 (en) 2007-07-12 2016-09-26 Gitr Inc Combination USING 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
KR100945483B1 (ko) 2007-10-25 2010-03-05 이화여자대학교 산학협력단 pikD 조절유전자의 발현벡터를 이용한 스트렙토미세스베네주엘라에(Streptomycesvenezuelae)에서폴리케타이드(polyketide)의 생산성 증가방법
ES2439705T3 (es) 2007-10-25 2014-01-24 Genentech, Inc. Proceso para la preparación de compuestos de tienopirimidina
GB0805363D0 (en) 2008-03-20 2008-04-30 Sinvent As Novel NRPS-PKS gene cluster and its manipulation and utility
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
WO2010011666A2 (en) 2008-07-21 2010-01-28 University Of South Florida Indoline scaffold shp-2 inhibitors and cancer treatment method
WO2010030002A1 (ja) 2008-09-12 2010-03-18 国立大学法人三重大学 外来性gitrリガンド発現細胞
US20110171219A1 (en) 2008-09-19 2011-07-14 Fahar Merchant Treating cancer stem cells using targeted cargo proteins
US8962329B2 (en) 2008-09-24 2015-02-24 Shanghai Institute Of Organic Chemistry, Chinese Academy Of Sciences Gene cluster
CN102365094A (zh) 2009-01-30 2012-02-29 英安塔制药有限公司 用于预防或者治疗肝炎感染的环孢菌素类似物
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
CA2768299C (en) 2009-07-13 2018-03-20 President And Fellows Of Harvard College Bifunctional stapled polypeptides and uses thereof
WO2011009938A2 (en) 2009-07-24 2011-01-27 Universite Henri Poincare Nancy 1 Stambomycin and derivatives, their production and their use as drugs
ES2817700T3 (es) 2009-08-17 2021-04-07 Memorial Sloan Kettering Cancer Center Derivados de 2-(pirimidin-5-il)-tiopirimidina como moduladores de Hsp70 y Hsc70 para el tratamiento de trastornos proliferativos
US8709424B2 (en) 2009-09-03 2014-04-29 Merck Sharp & Dohme Corp. Anti-GITR antibodies
EP2480565A4 (en) 2009-09-22 2014-01-01 Aileron Therapeutics Inc PEPTIDOMIMETIC MACROCYCLES
US20120208720A1 (en) 2009-10-22 2012-08-16 Kenji Kashiwagi Rapid display method in translational synthesis of peptide
GB0919054D0 (en) 2009-10-30 2009-12-16 Isis Innovation Treatment of obesity
NZ600820A (en) 2009-12-29 2014-12-24 Emergent Product Dev Seattle 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
WO2012075048A2 (en) 2010-11-30 2012-06-07 The Johns Hopkins University Hybrid cyclic libraries and screens thereof
UY33775A (es) 2010-12-10 2012-07-31 Gilead Sciences Inc Inhibidores macrocíclicos de virus flaviviridae, composiciones farmacéuticas que los comprenden y sus usos
US9428845B1 (en) 2010-12-28 2016-08-30 Warp Drive Bio, Inc. Identifying new therapeutic agents
MY161199A (en) 2011-03-23 2017-04-14 Amgen Inc Fused tricyclic dual inhibitors of cdk 4/6 and flt3
HRP20220319T1 (hr) 2011-05-19 2022-05-13 Fundación Del Sector Público Estatal Centro Nacional De Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Makrociklički spojevi kao inhibitori protein kinaze
US9260484B2 (en) 2011-06-15 2016-02-16 Ohio State Innovation Foundation Small molecule composite surfaces as inhibitors of protein-protein interactions
TW201311689A (zh) 2011-08-05 2013-03-16 必治妥美雅史谷比公司 作為因子xia抑制劑之新穎巨環化合物
DE102011111991A1 (de) 2011-08-30 2013-02-28 Lead Discovery Center Gmbh Neue Cyclosporin-Derivate
WO2013039954A1 (en) 2011-09-14 2013-03-21 Sanofi Anti-gitr antibodies
WO2013155223A1 (en) 2012-04-10 2013-10-17 The Regents Of The University Of California Compositions and methods for treating cancer
AR091279A1 (es) 2012-06-08 2015-01-21 Gilead Sciences Inc Inhibidores macrociclicos de virus flaviviridae
KR20150040265A (ko) 2012-06-08 2015-04-14 길리애드 사이언시즈, 인코포레이티드 플라비비리대 바이러스의 마크로시클릭 저해제
BR112014030649A2 (pt) * 2012-06-08 2017-06-27 Gilead Sciences Inc inibidores macrocíclicos da flaviviridae vírus
PT2872157T (pt) 2012-07-12 2020-04-30 Hangzhou Dac Biotech Co Ltd Conjugados de moléculas de ligação celular com agentes citotóxicos
CN105849086B (zh) 2012-11-24 2018-07-31 杭州多禧生物科技有限公司 亲水性链接体及其在药物分子和细胞结合分子共轭反应上的应用
WO2014113584A1 (en) 2013-01-16 2014-07-24 Rhode Island Hospital Compositions and methods for the prevention and treatment of osteolysis and osteoporosis
JP6473133B2 (ja) 2013-03-15 2019-02-20 アラクセス ファーマ エルエルシー Krasg12cの共有結合性阻害剤
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
SG11201506395RA (en) 2013-03-15 2015-09-29 Novartis Ag Antibody drug conjugates
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)
EP2806274A1 (en) 2013-05-24 2014-11-26 AIT Austrian Institute of Technology GmbH Lung cancer diagnostic method and means
CA2953482A1 (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
EP2826586A1 (en) 2013-07-18 2015-01-21 Siemens Aktiengesellschaft A method and a system for machining an object
EP3055290B1 (en) 2013-10-10 2019-10-02 Araxes Pharma LLC Inhibitors of kras g12c
US10093646B2 (en) 2014-01-17 2018-10-09 Novartis Ag 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and compositions thereof for inhibiting the activity of SHP2
CN105899493B (zh) 2014-01-17 2019-03-29 诺华股份有限公司 用于抑制shp2活性的1-(三嗪-3-基/哒嗪-3-基)-哌(-嗪)啶衍生物及其组合物
US10233431B2 (en) 2014-02-26 2019-03-19 The Regents Of The University Of California Producing 3-hydroxycarboxylic acid and ketone using polyketide synthases
CN106255882A (zh) 2014-03-03 2016-12-21 耶路撒冷希伯来大学伊森姆研究发展公司 用于检测铜绿假单胞菌的方法和装置
JO3474B1 (ar) * 2014-08-29 2020-07-05 Amgen Inc مشتقات تيتراهيدرونافثالين التي تثبط بروتين mcl-1
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
JP2017528498A (ja) 2014-09-25 2017-09-28 アラクセス ファーマ エルエルシー Kras g12c変異体タンパク質のインヒビター
TW201629069A (zh) 2015-01-09 2016-08-16 霍普驅動生物科技股份有限公司 參與協同結合之化合物及其用途
US10533016B2 (en) 2015-01-09 2020-01-14 Revolution Medicines, Inc. Compounds that participate in cooperative binding and uses thereof
US10077289B2 (en) 2015-03-31 2018-09-18 Allergan, Inc. Cyclosporins modified on the MeBmt sidechain by heterocyclic rings
CA2981530A1 (en) 2015-04-10 2016-10-13 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
MX2017013275A (es) 2015-04-15 2018-01-26 Araxes Pharma Llc Inhibidores triciclicos fusionados de kras y metodos de uso de los mismos.
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
EP3310774B1 (en) 2015-06-19 2020-04-29 Novartis AG Compounds and compositions for inhibiting the activity of shp2
CN107787323B (zh) 2015-06-19 2020-09-01 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
US10975080B2 (en) 2015-06-19 2021-04-13 Novartis Ag Compounds and compositions for inhibiting the activity of SHP2
CA2993013A1 (en) 2015-07-22 2017-01-26 Araxes Pharma Llc Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins
US10875842B2 (en) 2015-09-28 2020-12-29 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356339A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10730867B2 (en) 2015-09-28 2020-08-04 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10647703B2 (en) 2015-09-28 2020-05-12 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356353A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US9989535B2 (en) 2015-10-01 2018-06-05 Warp Drive Bio, Inc. Methods and reagents for analyzing protein-protein interfaces
WO2017078499A2 (ko) 2015-11-06 2017-05-11 경북대학교 산학협력단 단백질 타이로신 탈인산화효소 억제제를 포함하는 신경염증성 질환의 예방 또는 치료용 조성물
WO2017079723A1 (en) 2015-11-07 2017-05-11 Board Of Regents, The University Of Texas System Targeting proteins for degradation
KR20180081596A (ko) 2015-11-16 2018-07-16 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
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
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
WO2017156397A1 (en) 2016-03-11 2017-09-14 Board Of Regents, The University Of Texas Sysytem Heterocyclic inhibitors of ptpn11
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
CA3024523A1 (en) 2016-05-18 2017-11-23 Mirati Therapeutics, Inc. Kras g12c inhibitors
CN109475531B (zh) 2016-05-31 2021-08-17 得克萨斯州立大学董事会 Ptpn11的杂环抑制剂
US10858359B2 (en) 2016-06-07 2020-12-08 Jacobio Pharmaceuticals Co., Ltd. Heterocyclic ring derivatives useful as SHP2 inhibitors
CA3030167A1 (en) 2016-07-12 2018-01-18 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
US10280172B2 (en) 2016-09-29 2019-05-07 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3523289A1 (en) 2016-10-07 2019-08-14 Araxes Pharma LLC Heterocyclic compounds as inhibitors of ras and methods of use thereof
AU2017350900A1 (en) 2016-10-28 2019-06-13 Ginkgo Bioworks, Inc. Compositions and methods for the production of compounds
US10857150B2 (en) * 2016-11-18 2020-12-08 Abliva Ab Use of sanglifehrin macrocyclic analogues as anticancer compounds
EP3555077B1 (en) 2016-12-15 2023-04-19 The Regents of The University of California Compositions and methods for treating cancer
UA124474C2 (uk) 2016-12-22 2021-09-22 Емджен Інк. БЕНЗІЗОТІАЗОЛЬНІ, ІЗОТІАЗОЛО[3,4-b]ПІРИДИНОВІ, ХІНАЗОЛІНОВІ, ФТАЛАЗИНОВІ, ПІРИДО[2,3-d]ПІРИДАЗИНОВІ Й ПІРИДО[2,3-d]ПІРИМІДИНОВІ ПОХІДНІ ЯК ІНГІБІТОРИ G12C KRAS ДЛЯ ЛІКУВАННЯ РАКУ ЛЕГЕНІ, РАКУ ПІДШЛУНКОВОЇ ЗАЛОЗИ АБО КОЛОРЕКТАЛЬНОГО РАКУ
US10988766B2 (en) 2017-01-06 2021-04-27 Oregon Health & Science University Compositions and methods used in diagnosing and treating colorectal cancer
CN110730678B (zh) 2017-01-10 2022-07-15 诺华股份有限公司 包含alk抑制剂和shp2抑制剂的药物组合
BR112019014527A2 (pt) 2017-01-23 2020-02-27 Revolution Medicines, Inc. Compostos de piridina como inibidores de shp2 alostéricos
IL296456A (en) 2017-01-23 2022-11-01 Revolution Medicines Inc Bicyclics as allosteric shp2 inhibitors
EP3573971A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
EP3573964A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Benzothiophene and benzothiazole compounds and methods of use thereof
EP3573967A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused hetero-hetero bicyclic compounds and methods of use thereof
EP3573970A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
US11274093B2 (en) 2017-01-26 2022-03-15 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
US20200385364A1 (en) 2017-01-26 2020-12-10 Araxes Pharma Llc Fused n-heterocyclic compounds and methods of use thereof
JOP20190186A1 (ar) 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
WO2018160731A1 (en) 2017-02-28 2018-09-07 Novartis Ag Shp inhibitor compositions and uses for chimeric antigen receptor therapy
KR102317480B1 (ko) 2017-03-23 2021-10-25 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체
AU2018250186A1 (en) 2017-04-05 2019-11-14 Revolution Medicines, Inc. Methods and reagents for analyzing protein-protein interfaces
US20200199102A1 (en) 2017-04-05 2020-06-25 Revolution Medicines, Inc. Compounds that participate in cooperative binding and uses thereof
IL303660A (en) 2017-05-02 2023-08-01 Revolution Medicines Inc Rapamycin derivatives as MTOR tracers
EP3621968A1 (en) 2017-05-11 2020-03-18 Astrazeneca AB Heteroaryl compounds that inhibit g12c mutant ras proteins
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
EP3630746A1 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Compounds and methods of use thereof for treatment of cancer
AU2018271990A1 (en) 2017-05-25 2019-12-12 Araxes Pharma Llc Covalent inhibitors of KRAS
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
TW201918260A (zh) 2017-09-07 2019-05-16 美商銳新醫藥公司 Shp2抑制劑組合物以及治療癌症的方法
AU2018329920B2 (en) 2017-09-08 2022-12-01 Amgen Inc. Inhibitors of KRAS G12C and methods of using the same
WO2019051469A1 (en) 2017-09-11 2019-03-14 Krouzon Pharmaceuticals, Inc. SHP2 OCTAHYDROCYCLOPENTA [C] PYRROLE ALLOSTERIC INHIBITORS
UA125802C2 (uk) 2017-11-15 2022-06-08 Міраті Терапьютікс, Інк. Інгібітори kras g12c
US10597405B2 (en) 2017-12-08 2020-03-24 Astrazeneca Ab Chemical compounds
TW201942115A (zh) 2018-02-01 2019-11-01 美商輝瑞股份有限公司 作為抗癌藥之經取代的喹唑啉和吡啶並嘧啶衍生物
TW201942116A (zh) 2018-02-09 2019-11-01 美商輝瑞股份有限公司 作為抗癌劑之四氫喹唑啉衍生物
MX2020011565A (es) 2018-05-01 2021-01-29 Revolution Medicines Inc Analogos de rapamicina ligados a c40, c28 y c-32 como inhibidores de mtor.
EP3788050A1 (en) 2018-05-01 2021-03-10 Revolution Medicines, Inc. C26-linked rapamycin analogs as mtor inhibitors
JP7266043B2 (ja) 2018-05-04 2023-04-27 アムジエン・インコーポレーテツド KRas G12C阻害剤及びそれを使用する方法
MA52496A (fr) 2018-05-04 2021-03-10 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
EP3790551A4 (en) 2018-05-07 2022-03-09 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
TW202012415A (zh) 2018-05-08 2020-04-01 瑞典商阿斯特捷利康公司 化學化合物
AU2019265822A1 (en) 2018-05-10 2020-11-19 Amgen Inc. KRAS G12C inhibitors for the treatment of cancer
EP3802535B1 (en) 2018-06-01 2022-12-14 Amgen, Inc Kras g12c inhibitors and methods of using the same
EP4268898A3 (en) 2018-06-11 2024-01-17 Amgen Inc. Kras g12c inhibitors for treating cancer
MX2020012261A (es) 2018-06-12 2021-03-31 Amgen Inc Inhibidores de kras g12c que comprenden un anillo de piperazina y uso de estos en el tratamiento del cancer.
AU2019312670A1 (en) 2018-08-01 2021-02-04 Araxes Pharma Llc Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer
MX2021001706A (es) 2018-08-16 2021-04-19 Hoffmann La Roche Compuestos de anillo fusionado.
ES2961253T3 (es) 2018-08-31 2024-03-11 Mirati Therapeutics Inc Inhibidores de KRas G12C
EP3883565A1 (en) 2018-11-19 2021-09-29 Amgen Inc. Kras g12c inhibitors and methods of using the same
EP3897644A4 (en) * 2018-12-21 2022-09-07 Revolution Medicines, Inc. CONNECTIONS INVOLVING IN A COOPERATIVE BINDING AND USES THEREOF
MX2022005359A (es) 2019-11-04 2022-06-02 Revolution Medicines Inc Inhibidores de ras.
BR112022008535A2 (pt) 2019-11-04 2022-08-09 Revolution Medicines Inc Composto, composição farmacêutica, métodos para tratar câncer e um distúrbio relativo à proteína ras
TW202132315A (zh) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ras 抑制劑
WO2022060583A1 (en) 2020-09-03 2022-03-24 Revolution Medicines, Inc. Use of sos1 inhibitors to treat malignancies with shp2 mutations
CN117683049A (zh) 2020-09-15 2024-03-12 锐新医药公司 作为ras抑制剂以治疗癌症的吲哚衍生物

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