[go: up one dir, main page]

TR199900066T2 - Matriks metalloproteazlarin fosfinat bazli inhibitörleri - Google Patents

Matriks metalloproteazlarin fosfinat bazli inhibitörleri

Info

Publication number
TR199900066T2
TR199900066T2 TR1999/00066T TR9900066T TR199900066T2 TR 199900066 T2 TR199900066 T2 TR 199900066T2 TR 1999/00066 T TR1999/00066 T TR 1999/00066T TR 9900066 T TR9900066 T TR 9900066T TR 199900066 T2 TR199900066 T2 TR 199900066T2
Authority
TR
Turkey
Prior art keywords
matrix
rleri
metalloprotateazlar
bazl
phosphinate
Prior art date
Application number
TR1999/00066T
Other languages
English (en)
Inventor
Alan Reiter Lawrence
Original Assignee
Pfizer 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 Pfizer Inc. filed Critical Pfizer Inc.
Publication of TR199900066T2 publication Critical patent/TR199900066T2/tr

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
    • C07F9/6553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms
    • C07F9/655345—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a five-membered ring
    • 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
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/02—Local antiseptics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • C07F9/301—Acyclic saturated acids which can have further substituents on alkyl
    • 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
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • C07F9/306—Arylalkanephosphinic acids, e.g. Ar-(CH2)n-P(=X)(R)(XH), (X = O,S, Se; n>=1)
    • 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
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/58—Pyridine rings
    • 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
    • C07F9/655—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
    • C07F9/65525—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a seven-(or more) membered ring
    • C07F9/65527—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a seven-(or more) membered ring condensed with carbocyclic rings or carbocyclic ring systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Artrit, kanser, sitotoksik antikanser ajanlar ile sinerji, doku ülserasyonu, maküler dejenerasyon ( beneklenme), restenozis (genisletilmis bir kanalin tekrar daraltilmasi), periodontal hastaliklar, epidemolizis bulloza, skleritten (sklera iltihabi) meydana gelen gruptan seçilen bir gruptan seçilen bir durumun tedavisinde yararli olan, standart NSAID'lar ve analjezikler ile kombinasyon halinde ve AIDS, sepsis, septik sok ve TNF üretimini içine alan diger hastaliklar, matriks metalloproteinaz aktivite ile karakterize olan diger hastaliklarin tedavisinde yararli olan, R1, R2, R3, R4, R5, R6 ve Ar'nin, yukarida tarif edildigi gibi oldugu, formül (I)'in bir bilesigi.
TR1999/00066T 1996-07-18 1997-06-30 Matriks metalloproteazlarin fosfinat bazli inhibitörleri TR199900066T2 (tr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US2195996P 1996-07-18 1996-07-18

Publications (1)

Publication Number Publication Date
TR199900066T2 true TR199900066T2 (tr) 1999-04-21

Family

ID=21807061

Family Applications (1)

Application Number Title Priority Date Filing Date
TR1999/00066T TR199900066T2 (tr) 1996-07-18 1997-06-30 Matriks metalloproteazlarin fosfinat bazli inhibitörleri

Country Status (40)

Country Link
US (1) US6147061A (tr)
EP (1) EP0923585B1 (tr)
JP (1) JP3299975B2 (tr)
KR (1) KR20000067904A (tr)
CN (1) CN1225639A (tr)
AP (1) AP761A (tr)
AR (1) AR008260A1 (tr)
AT (1) ATE217315T1 (tr)
AU (1) AU712973B2 (tr)
BG (1) BG103111A (tr)
BR (1) BR9710381A (tr)
CA (1) CA2260898C (tr)
CO (1) CO4890852A1 (tr)
CZ (1) CZ11899A3 (tr)
DE (1) DE69712496T2 (tr)
DK (1) DK0923585T3 (tr)
EA (1) EA199900036A1 (tr)
ES (1) ES2175415T3 (tr)
GT (1) GT199700085A (tr)
HN (1) HN1997000099A (tr)
HR (1) HRP970391A2 (tr)
HU (1) HUP9903014A3 (tr)
ID (1) ID19443A (tr)
IL (1) IL127567A0 (tr)
IS (1) IS4928A (tr)
MA (1) MA24270A1 (tr)
NO (1) NO990184L (tr)
NZ (1) NZ333303A (tr)
OA (1) OA10956A (tr)
PA (1) PA8433701A1 (tr)
PE (1) PE88198A1 (tr)
PL (1) PL331254A1 (tr)
PT (1) PT923585E (tr)
SI (1) SI0923585T1 (tr)
SK (1) SK3799A3 (tr)
TN (1) TNSN97122A1 (tr)
TR (1) TR199900066T2 (tr)
WO (1) WO1998003516A1 (tr)
YU (1) YU1899A (tr)
ZA (1) ZA976330B (tr)

Families Citing this family (291)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EE200100027A (et) 1998-07-15 2002-06-17 Jomaa Hassan Fosfororgaanilised ühendid, neid sisaldav farmatseutiline preparaat ja nende kasutamine
US6858598B1 (en) 1998-12-23 2005-02-22 G. D. Searle & Co. Method of using a matrix metalloproteinase inhibitor and one or more antineoplastic agents as a combination therapy in the treatment of neoplasia
US6833373B1 (en) 1998-12-23 2004-12-21 G.D. Searle & Co. Method of using an integrin antagonist and one or more antineoplastic agents as a combination therapy in the treatment of neoplasia
FR2788525B1 (fr) * 1999-01-19 2002-11-29 Commissariat Energie Atomique Pseudo-peptides phosphiniques, utilisables comme inhibiteurs des metalloproteases a zinc matricielles
IL132315A0 (en) * 1999-10-11 2001-03-19 Yissum Res Dev Co Compositions comprising oxophosphonate-based metalloproteinase inhibitors
UA74803C2 (uk) 1999-11-11 2006-02-15 Осі Фармасьютікалз, Інк. Стійкий поліморф гідрохлориду n-(3-етинілфеніл)-6,7-біс(2-метоксіетокси)-4-хіназолінаміну, спосіб його одержання (варіанти) та фармацевтичне застосування
US6458822B2 (en) 2000-03-13 2002-10-01 Pfizer Inc. 2-oxo-imidazolidine-4-carboxylic acid hydroxamide compounds that inhibit matrix metalloproteinases
AR032028A1 (es) 2001-01-05 2003-10-22 Pfizer Anticuerpos contra el receptor del factor de crecimiento similar a insulina
US6995171B2 (en) 2001-06-21 2006-02-07 Agouron Pharmaceuticals, Inc. Bicyclic pyrimidine and pyrimidine derivatives useful as anticancer agents
AR039067A1 (es) 2001-11-09 2005-02-09 Pfizer Prod Inc Anticuerpos para cd40
PE20030701A1 (es) 2001-12-20 2003-08-21 Schering Corp Compuestos para el tratamiento de trastornos inflamatorios
WO2003061566A2 (en) * 2002-01-24 2003-07-31 Yissum Research Development Company Of The Hebrew University Of Jerusalem Anti-cancer combination and use thereof
JP2005527511A (ja) 2002-03-01 2005-09-15 ファイザー インコーポレイテッド 抗血管形成剤として有用なチエノピリジンのインドリル−尿素誘導体およびその使用法
CA2478374C (en) 2002-03-13 2009-01-06 Eli M. Wallace N3 alkylated benzimidazole derivatives as mek inhibitors
UA77303C2 (en) 2002-06-14 2006-11-15 Pfizer Derivatives of thienopyridines substituted by benzocondensed heteroarylamide useful as therapeutic agents, pharmaceutical compositions and methods for their use
BR0317548A (pt) 2002-12-19 2005-11-22 Pfizer Compostos de indazole e composições farmacêuticas para a inibição de proteìnas-cinases e métodos para o seu uso
CA2511521C (en) 2002-12-30 2012-02-07 Angiotech International Ag Drug delivery from rapid gelling polymer composition
DK1603570T5 (da) 2003-02-26 2013-12-09 Sugen Inc Aminoheteroarylforbindelser som proteinkinaseinhibitorer
HN2004000285A (es) 2003-08-04 2006-04-27 Pfizer Prod Inc ANTICUERPOS DIRIGIDOS A c-MET
CN1835975B (zh) 2003-08-13 2012-11-21 辉瑞产品公司 经修饰的人类igf-1r抗体
JP2007504122A (ja) 2003-08-29 2007-03-01 ファイザー・インク 新規抗血管形成剤として有用なチエノピリジン−フェニルアセトアミドおよびその誘導体
US7144907B2 (en) 2003-09-03 2006-12-05 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
AR045563A1 (es) 2003-09-10 2005-11-02 Warner Lambert Co Anticuerpos dirigidos a m-csf
JP4869075B2 (ja) 2003-11-19 2012-02-01 アレイ バイオファーマ、インコーポレイテッド Ｍｅｋの複素環阻害剤及びその使用方法
ATE473967T1 (de) * 2003-11-26 2010-07-15 Pfizer Prod Inc Aminopyrazolderivate als gsk-3-inhibitoren
BRPI0513200A (pt) 2004-07-16 2008-04-29 Pfizer Prod Inc uso de um anticorpo anti-igf-1r na preparação de um medicamento para tratamento combinado para malignidades não-hematológicas
JP4242911B2 (ja) 2004-08-26 2009-03-25 ファイザー・インク プロテインキナーゼ阻害薬としてのエナンチオピュアなアミノヘテロアリール化合物
MY146381A (en) 2004-12-22 2012-08-15 Amgen Inc Compositions and methods relating relating to anti-igf-1 receptor antibodies
US7429667B2 (en) 2005-01-20 2008-09-30 Ardea Biosciences, Inc. Phenylamino isothiazole carboxamidines as MEK inhibitors
RU2500673C2 (ru) 2005-05-18 2013-12-10 Астразенека Аб Гетероциклические ингибиторы мек и способы их применения
RU2007148927A (ru) * 2005-05-26 2009-07-10 Метабэйзис Терапьютикс, Инк. (Us) Новые тиреомиметики, содержащие фосфиновую кислоту
US20090232879A1 (en) 2005-05-26 2009-09-17 Metabasis Therapeutics, Inc. Thyromimetics for the Treatment of Fatty Liver Diseases
US8101799B2 (en) 2005-07-21 2012-01-24 Ardea Biosciences Derivatives of N-(arylamino) sulfonamides as inhibitors of MEK
AU2006292278B2 (en) 2005-09-20 2012-03-08 Osi Pharmaceuticals, Inc. Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
TWI405756B (zh) 2005-12-21 2013-08-21 Array Biopharma Inc 新穎硫酸氫鹽
US7842836B2 (en) 2006-04-11 2010-11-30 Ardea Biosciences N-aryl-N'alkyl sulfamides as MEK inhibitors
CN101454004B (zh) 2006-04-18 2013-12-04 阿迪亚生命科学公司 作为mek抑制剂的吡啶酮磺酰胺类和吡啶酮硫酰胺类
US20080146524A1 (en) * 2006-12-14 2008-06-19 Solvay Pharmaceuticals B.V. Selective inhibitors of neurotensin degrading enzymes
JP2010513263A (ja) 2006-12-15 2010-04-30 ファイザー・プロダクツ・インク ベンズイミダゾール誘導体
CA2675358C (en) 2007-01-19 2016-01-05 Ardea Biosciences, Inc. Inhibitors of mek
JP4782239B2 (ja) 2007-04-18 2011-09-28 ファイザー・プロダクツ・インク 異常細胞増殖治療のためのスルホニルアミド誘導体
US8530463B2 (en) 2007-05-07 2013-09-10 Hale Biopharma Ventures Llc Multimodal particulate formulations
CA2694646C (en) 2007-07-30 2017-09-05 Ardea Biosciences, Inc. Combinations of mek inhibitors and raf kinase inhibitors and uses thereof
PL2222675T3 (pl) 2007-12-19 2014-02-28 Genentech Inc 5-anilinoimidazopirydyny i sposoby zastosowania
KR20100099185A (ko) 2007-12-21 2010-09-10 제넨테크, 인크. 아자인돌리진 및 이용 방법
MX358640B (es) 2008-01-04 2018-08-29 Intellikine Llc Isoquinolin-1 (2h) -onas y tieno [2,3-d]pirimidin-4(3h) -onas substituidas, y metodos de uso de las mismas.
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
JP5547099B2 (ja) 2008-03-14 2014-07-09 インテリカイン， エルエルシー キナーゼ阻害剤および使用方法
EP2271347B1 (en) 2008-03-28 2016-05-11 Hale Biopharma Ventures, Llc Administration of benzodiazepine compositions
US9096611B2 (en) 2008-07-08 2015-08-04 Intellikine Llc Kinase inhibitors and methods of use
CA2737597C (en) 2008-10-16 2017-03-14 University Of Pittsburgh-Of The Commonwealth System Of Higher Education Fully human antibodies to high molecular weight-melanoma associated antigen and uses thereof
US8476431B2 (en) 2008-11-03 2013-07-02 Itellikine LLC Benzoxazole kinase inhibitors and methods of use
US8426402B2 (en) 2009-02-05 2013-04-23 Immunogen, Inc. Benzodiazepine derivatives
EP2393814A1 (en) 2009-02-09 2011-12-14 SuperGen, Inc. Pyrrolopyrimidinyl axl kinase inhibitors
EP2400985A2 (en) 2009-02-25 2012-01-04 OSI Pharmaceuticals, LLC Combination of an either an anti-igf-1r antibody or an igf binding protein and a small molecule igf-1r kinase inhibitor
JP2012519170A (ja) 2009-02-26 2012-08-23 オーエスアイ・ファーマシューティカルズ，エルエルシー 生体内の腫瘍細胞のｅｍｔステータスをモニターするためのｉｎｓｉｔｕ法
WO2010099138A2 (en) 2009-02-27 2010-09-02 Osi Pharmaceuticals, Inc. Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
JP2012519281A (ja) 2009-02-27 2012-08-23 オーエスアイ・ファーマシューティカルズ，エルエルシー 間葉様腫瘍細胞またはその生成を阻害する薬剤を同定するための方法
JP2012519282A (ja) 2009-02-27 2012-08-23 オーエスアイ・ファーマシューティカルズ，エルエルシー 間葉様腫瘍細胞またはその生成を阻害する薬剤を同定するための方法
WO2010098866A1 (en) 2009-02-27 2010-09-02 Supergen, Inc. Cyclopentathiophene/cyclohexathiophene dna methyltransferase inhibitors
CN106478496A (zh) 2009-03-27 2017-03-08 阿迪生物科学公司 作为mek抑制剂的二氢吡啶磺酰胺和二氢吡啶硫酰胺
JP5789252B2 (ja) 2009-05-07 2015-10-07 インテリカイン， エルエルシー 複素環式化合物およびその使用
EP2459191A1 (en) 2009-07-31 2012-06-06 OSI Pharmaceuticals, LLC Mtor inhibitor and angiogenesis inhibitor combination therapy
HRP20190016T1 (hr) 2009-08-17 2019-03-08 Intellikine, Llc Heterociklički spojevi i njihova upotreba
EP2473500A2 (en) 2009-09-01 2012-07-11 Pfizer Inc. Benzimidazole derivatives
CA2814617C (en) 2009-10-13 2017-12-19 Allostem Therapeutics Llc Novel mek inhibitors, useful in the treatment of diseases
WO2011049625A1 (en) 2009-10-20 2011-04-28 Mansour Samadpour Method for aflatoxin screening of products
HRP20171537T1 (hr) 2009-11-05 2017-12-15 Rhizen Pharmaceuticals S.A. Novi modulatori benzopiran kinaze
US9173961B2 (en) 2010-02-10 2015-11-03 Immunogen, Inc. CD20 antibodies and uses thereof
CA3024216C (en) 2010-02-12 2021-03-30 Pfizer Inc. Salts and polymorphs of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-cd]indol-6-one
US20110217309A1 (en) 2010-03-03 2011-09-08 Buck Elizabeth A Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
AU2011223643A1 (en) 2010-03-03 2012-06-28 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
ES2715611T3 (es) 2010-05-17 2019-06-05 Incozen Therapeutics Pvt Ltd Compuestos novedosos de 3H-imidazo[4,5-b]piridina-3,5-disustituida y 3H-[1,2,3]triazolo[4,5-b]piridina 3,5-disustituida como moduladores de proteína cinasas
EP2571357B1 (en) 2010-05-21 2016-07-06 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
ES2611479T3 (es) 2010-06-16 2017-05-09 University Of Pittsburgh- Of The Commonwealth System Of Higher Education Anticuerpos contra endoplasmina y su uso
CA2813162C (en) 2010-10-20 2015-06-16 Pfizer Inc. Pyridine-2- derivatives as smoothened receptor modulators
CN103298474B (zh) 2010-11-10 2016-06-29 无限药品股份有限公司 杂环化合物及其用途
TWI546305B (zh) 2011-01-10 2016-08-21 英菲尼提製藥股份有限公司 製備異喹啉酮之方法及異喹啉酮之固體形式
CA2825894C (en) 2011-02-02 2021-11-30 Amgen Inc. Prognosis of cancer using a circulating biomarker
IL279304B (en) 2011-02-15 2022-07-01 Immunogen Inc Method for producing an indolinobenzodiazepine
WO2012116040A1 (en) 2011-02-22 2012-08-30 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors in hepatocellular carcinoma
JP5808826B2 (ja) 2011-02-23 2015-11-10 インテリカイン， エルエルシー 複素環化合物およびその使用
US9150644B2 (en) 2011-04-12 2015-10-06 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Human monoclonal antibodies that bind insulin-like growth factor (IGF) I and II
CA3019531A1 (en) 2011-04-19 2012-10-26 Pfizer Inc. Combinations of anti-4-1bb antibodies and adcc-inducing antibodies for the treatment of cancer
EP2702173A1 (en) 2011-04-25 2014-03-05 OSI Pharmaceuticals, LLC Use of emt gene signatures in cancer drug discovery, diagnostics, and treatment
KR101992311B1 (ko) 2011-05-04 2019-09-27 리젠 파마슈티컬스 소시에떼 아노님 단백질 키나아제의 조절제로서 신규한 화합물
EP2720699B1 (en) 2011-06-14 2018-05-16 Hale Biopharma Ventures, Llc Administration of benzodiazepine
WO2013012918A1 (en) 2011-07-19 2013-01-24 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
AU2012284088B2 (en) 2011-07-19 2015-10-08 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
US9416132B2 (en) 2011-07-21 2016-08-16 Tolero Pharmaceuticals, Inc. Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors
CA2846431A1 (en) 2011-08-29 2013-03-07 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
CN103814030A (zh) 2011-09-22 2014-05-21 辉瑞大药厂 吡咯并嘧啶及嘌呤衍生物
US9630979B2 (en) 2011-09-29 2017-04-25 Infinity Pharmaceuticals, Inc. Inhibitors of monoacylglycerol lipase and methods of their use
WO2013050725A1 (en) 2011-10-04 2013-04-11 King's College London Ige anti -hmw-maa antibody
WO2013068902A1 (en) 2011-11-08 2013-05-16 Pfizer Inc. Methods of treating inflammatory disorders using anti-m-csf antibodies
ES2668044T3 (es) 2012-02-22 2018-05-16 The Regents Of The University Of Colorado, A Body Corporate Derivados de bouvardina y usos terapéuticos de los mismos
US9452215B2 (en) 2012-02-22 2016-09-27 The Regents Of The University Of Colorado Bourvadin derivatives and therapeutic uses thereof
KR102164317B1 (ko) 2012-03-30 2020-10-13 리젠 파마슈티컬스 소시에떼 아노님 C-met 단백질 키나제의 조절제로서의 신규한 3,5-디치환-3h-이미다조[4,5-b]피리딘 및 3,5- 디치환 -3h-[1,2,3]트리아졸로[4,5-b] 피리딘 화합물
WO2013152252A1 (en) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
SG11201408161RA (en) 2012-06-08 2015-01-29 Sutro Biopharma Inc Antibodies comprising site-specific non-natural amino acid residues, methods of their preparation and methods of their use
EP3135690A1 (en) 2012-06-26 2017-03-01 Sutro Biopharma, Inc. Modified fc proteins comprising site-specific non-natural amino acid residues, conjugates of the same, methods of their preparation and methods of their use
EP2887965A1 (en) 2012-08-22 2015-07-01 ImmunoGen, Inc. Cytotoxic benzodiazepine derivatives
ES2728864T3 (es) 2012-08-31 2019-10-29 Sutro Biopharma Inc Aminoácidos modificados que comprenden un grupo azido
JP6243918B2 (ja) 2012-10-16 2017-12-06 トレロ ファーマシューティカルズ， インコーポレイテッド Ｐｋｍ２調節因子およびそれらの使用方法
CN105102000B (zh) 2012-11-01 2021-10-22 无限药品公司 使用pi3激酶亚型调节剂的癌症疗法
US9999680B2 (en) 2013-02-28 2018-06-19 Immunogen, Inc. Conjugates comprising cell-binding agents and maytansinoids as cytotoxic agents
HK1219423A1 (zh) 2013-02-28 2017-04-07 Immunogen, Inc. 包含细胞结合剂及细胞毒素剂的轭合物
DK2970205T3 (da) 2013-03-14 2019-07-29 Tolero Pharmaceuticals Inc JAK2- og ALK2-inhibitorer og fremgangsmåder til anvendelse deraf
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
AU2014239542A1 (en) 2013-03-15 2015-10-01 Araxes Pharma Llc Covalent inhibitors of KRas G12C
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
HK1219421A1 (zh) 2013-03-15 2017-04-07 因特利凯有限责任公司 激酶抑制剂的组合及其用途
EP2970194A1 (en) 2013-03-15 2016-01-20 Infinity Pharmaceuticals, Inc. Salts and solid forms of isoquinolinones and composition comprising and methods of using the same
SG10201709926VA (en) 2013-05-30 2017-12-28 Infinity Pharmaceuticals Inc Treatment of cancers using pi3 kinase isoform modulators
WO2014194030A2 (en) 2013-05-31 2014-12-04 Immunogen, Inc. Conjugates comprising cell-binding agents and cytotoxic agents
ES2658039T3 (es) 2013-07-10 2018-03-08 Sutro Biopharma, Inc. Anticuerpos que comprenden múltiples residuos de aminoácidos no naturales sitio-específicos, métodos para su preparación y métodos de uso
PT3052096T (pt) 2013-10-03 2018-04-04 Kura Oncology Inc Inibidores de erk e métodos de utilização
US9751888B2 (en) 2013-10-04 2017-09-05 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
MX389256B (es) 2013-10-04 2025-03-20 Infinity Pharmaceuticals Inc Compuestos heterociclicos y usos de los mismos.
WO2015054572A1 (en) 2013-10-10 2015-04-16 Araxes Pharma Llc Inhibitors of kras g12c
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
EP3055298B1 (en) 2013-10-11 2020-04-29 Sutro Biopharma, Inc. Modified amino acids comprising tetrazine functional groups, methods of preparation, and methods of their use
WO2015061204A1 (en) 2013-10-21 2015-04-30 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
UA115388C2 (uk) 2013-11-21 2017-10-25 Пфайзер Інк. 2,6-заміщені пуринові похідні та їх застосування в лікуванні проліферативних захворювань
WO2015155624A1 (en) 2014-04-10 2015-10-15 Pfizer Inc. Dihydropyrrolopyrimidine derivatives
WO2015168079A1 (en) 2014-04-29 2015-11-05 Infinity Pharmaceuticals, Inc. Pyrimidine or pyridine derivatives useful as pi3k inhibitors
MX2016014143A (es) 2014-04-30 2017-02-15 Pfizer Derivados de diheterociclo enlazado a cicloalquilo.
EP3157916B1 (en) 2014-06-19 2018-12-12 ARIAD Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
WO2016001789A1 (en) 2014-06-30 2016-01-07 Pfizer Inc. Pyrimidine derivatives as pi3k inhibitors for use in the treatment of cancer
EP3473271B1 (en) 2014-07-31 2022-07-20 The Government of the United States of America as represented by the Secretary of the Department of Health and Human Services Human monoclonal antibodies against epha4 and their use
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
WO2016049524A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
WO2016097918A1 (en) 2014-12-18 2016-06-23 Pfizer Inc. Pyrimidine and triazine derivatives and their use as axl inhibitors
EA201792214A1 (ru) 2015-04-10 2018-01-31 Араксис Фарма Ллк Соединения замещенного хиназолина
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC Fused-tricyclic inhibitors of kras and methods of use thereof
JP6851978B2 (ja) 2015-04-20 2021-03-31 スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド ミトコンドリアプロファイリングによるアルボシジブ応答の予測
US10011629B2 (en) 2015-05-01 2018-07-03 Cocrystal Pharma, Inc. Nucleoside analogs for treatment of the flaviviridae family of viruses and cancer
JP6510075B2 (ja) 2015-05-18 2019-05-08 トレロ ファーマシューティカルズ， インコーポレイテッド バイオアベイラビリティが高いアルボシジブプロドラッグ
TWI703150B (zh) 2015-06-04 2020-09-01 美商庫拉腫瘤技術股份有限公司 用於抑制ｍｅｎｉｎ及ｍｌｌ蛋白之交互作用的方法及組合物
WO2017009751A1 (en) 2015-07-15 2017-01-19 Pfizer Inc. Pyrimidine derivatives
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
EP3331510A4 (en) 2015-08-03 2019-04-03 Tolero Pharmaceuticals, Inc. COMBINATION THERAPIES FOR THE TREATMENT OF CANCER
CN108349985A (zh) 2015-09-14 2018-07-31 无限药品股份有限公司 异喹啉酮的固体形式、其制备方法、包含其的组合物及其使用方法
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10858343B2 (en) 2015-09-28 2020-12-08 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
EP3356339A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058915A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10730867B2 (en) 2015-09-28 2020-08-04 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10875842B2 (en) 2015-09-28 2020-12-29 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
JP2018533939A (ja) 2015-10-19 2018-11-22 アラクセス ファーマ エルエルシー Ｒａｓの阻害剤をスクリーニングするための方法
TW201726656A (zh) 2015-11-16 2017-08-01 亞瑞克西斯製藥公司 包含經取代雜環基團之２－經取代喹唑啉化合物及其使用方法
US20180371551A1 (en) 2015-12-03 2018-12-27 Agios Pharmaceuticals, Inc. Mat2a inhibitors for treating mtap null cancer
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
US11708413B2 (en) 2016-01-27 2023-07-25 Sutro Biopharma, Inc. Anti-CD74 antibody conjugates, compositions comprising anti-CD74 antibody conjugates and methods of using anti-CD74 antibody conjugates
KR102419524B1 (ko) 2016-03-16 2022-07-08 쿠라 온콜로지, 인크. 메닌-mll의 가교된 이환식 억제제 및 사용 방법
EP3429591B1 (en) 2016-03-16 2023-03-15 Kura Oncology, Inc. Substituted thieno[2,3-d]pyrimidine derivatives as inhibitors of menin-mll and methods of use
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
US20170283445A1 (en) * 2016-04-05 2017-10-05 University Of South Carolina Small Molecule Inhibitors Selective For Polo-Like Kinase Proteins
US11883381B2 (en) 2016-05-12 2024-01-30 The Regents Of The University Of Michigan ASH1L inhibitors and methods of treatment therewith
US11118233B2 (en) 2016-05-18 2021-09-14 The University Of Chicago BTK mutation and ibrutinib resistance
WO2017214269A1 (en) 2016-06-08 2017-12-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
EP3507305A1 (en) 2016-09-02 2019-07-10 Dana-Farber Cancer Institute, Inc. Composition and methods of treating b cell disorders
JP2019529484A (ja) 2016-09-29 2019-10-17 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阻害剤
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
US11279694B2 (en) 2016-11-18 2022-03-22 Sumitomo Dainippon Pharma Oncology, Inc. Alvocidib prodrugs and their use as protein kinase inhibitors
JP2020500199A (ja) 2016-11-21 2020-01-09 バイキング・セラピューティクス・インコーポレイテッド グリコーゲン蓄積症の治療方法
WO2018098352A2 (en) 2016-11-22 2018-05-31 Jun Oishi Targeting kras induced immune checkpoint expression
CA3047557A1 (en) 2016-12-19 2018-06-28 Tolero Pharmaceuticals, Inc. Profiling peptides and methods for sensitivity profiling
EP3558955B1 (en) 2016-12-22 2021-08-11 Amgen Inc. Benzisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives as kras g12c inhibitors for treating lung, pancreatic or colorectal cancer
US11274093B2 (en) 2017-01-26 2022-03-15 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
EP3573966A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused n-heterocyclic compounds and methods of use thereof
JP7117311B2 (ja) 2017-01-26 2022-08-12 ゼットリップ ホールディング リミテッド Ｃｄ４７抗原結合単位およびその使用
EP3573971A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
CN110382482A (zh) 2017-01-26 2019-10-25 亚瑞克西斯制药公司 稠合的杂-杂二环化合物及其使用方法
WO2018140514A1 (en) 2017-01-26 2018-08-02 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
US11944627B2 (en) 2017-03-24 2024-04-02 Kura Oncology, Inc. Methods for treating hematological malignancies and Ewing's sarcoma
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
TW201900633A (zh) 2017-05-25 2019-01-01 美商亞瑞克西斯製藥公司 Kras之共價抑制劑
WO2018218071A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Compounds and methods of use thereof for treatment of cancer
JP2020521740A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー 変異体ｋｒａｓ、ｈｒａｓまたはｎｒａｓの調節因子としてのキナゾリン誘導体
AU2018280118B2 (en) 2017-06-05 2021-07-15 Viking Therapeutics, Inc. Compositions for the treatment of fibrosis
US11542248B2 (en) 2017-06-08 2023-01-03 Kura Oncology, Inc. Methods and compositions for inhibiting the interaction of menin with MLL proteins
EP3658588A1 (en) 2017-07-26 2020-06-03 Sutro Biopharma, Inc. Methods of using anti-cd74 antibodies and antibody conjugates in treatment of t-cell lymphoma
EP3679040B1 (en) 2017-09-08 2022-08-03 Amgen Inc. Inhibitors of kras g12c and methods of using the same
WO2019055579A1 (en) 2017-09-12 2019-03-21 Tolero Pharmaceuticals, Inc. TREATMENT REGIME FOR CANCERS THAT ARE INSENSITIVE TO BCL-2 INHIBITORS USING THE MCL-1 ALVOCIDIB INHIBITOR
SG11202002310UA (en) 2017-09-18 2020-04-29 Sutro Biopharma Inc Anti- folate receptor alpha antibody conjugates and their uses
TW201920170A (zh) 2017-09-20 2019-06-01 美商庫拉腫瘤技術股份有限公司 經取代之menin-mll 抑制劑及使用方法
WO2019075367A1 (en) 2017-10-13 2019-04-18 Tolero Pharmaceuticals, Inc. PKM2 ACTIVATORS IN COMBINATION WITH OXYGEN REACTIVE SPECIES FOR THE TREATMENT OF CANCER
US11110177B2 (en) 2017-11-10 2021-09-07 The Regents Of The University Of Michigan ASH1L degraders and methods of treatment therewith
CN112040947A (zh) 2017-12-07 2020-12-04 密歇根大学董事会 Nsd家族抑制剂及用其进行治疗的方法
EA202091979A1 (ru) 2018-03-22 2021-06-22 Вайкинг Терапьютикс, Инк. Кристаллические формы и способы получения кристаллических форм соединения
WO2019195753A1 (en) 2018-04-05 2019-10-10 Tolero Pharmaceuticals, Inc. Axl kinase inhibitors and use of the same
ES2995514T3 (en) 2018-05-04 2025-02-10 Amgen Inc Kras g12c inhibitors and methods of using the same
AU2019262589B2 (en) 2018-05-04 2022-07-07 Amgen Inc. KRAS G12C inhibitors and methods of using the same
MX2020011907A (es) 2018-05-10 2021-01-29 Amgen Inc Inhibidores de kras g12c para el tratamiento de cancer.
ES2938987T3 (es) 2018-06-01 2023-04-18 Amgen Inc Inhibidores de KRAS G12c y métodos de uso de los mismos
CN112533581B (zh) 2018-06-07 2024-08-30 密歇根大学董事会 Prc1抑制剂及用其进行治疗的方法
MX2020012204A (es) 2018-06-11 2021-03-31 Amgen Inc Inhibidores de kras g12c para tratar el cáncer.
CA3100390A1 (en) 2018-06-12 2020-03-12 Amgen Inc. Kras g12c inhibitors encompassing piperazine ring and use thereof in the treatment of cancer
CN112512597A (zh) 2018-07-26 2021-03-16 大日本住友制药肿瘤公司 用于治疗与acvr1表达异常相关的疾病的方法以及用于此的acvr1抑制剂
US12134620B2 (en) 2018-08-01 2024-11-05 Araxes Pharma Llc Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer
US20220047716A1 (en) 2018-09-17 2022-02-17 Sutro Biopharma, Inc. Combination therapies with anti-folate receptor antibody conjugates
KR20210083286A (ko) 2018-10-24 2021-07-06 아락세스 파마 엘엘씨 종양 전이를 억제하기 위한 g12c 돌연변이 kras 단백질의 억제제로서 2-(2-아크릴로일-2,6-디아자스피로[3.4]옥탄-6-일)-6-(1h-인다졸-4-일)-벤조니트릴 유도체 및 관련 화합물
JP7516029B2 (ja) 2018-11-16 2024-07-16 アムジエン・インコーポレーテツド Ｋｒａｓ ｇ１２ｃ阻害剤化合物の重要な中間体の改良合成法
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法
WO2020106640A1 (en) 2018-11-19 2020-05-28 Amgen Inc. Kras g12c inhibitors and methods of using the same
AU2019388998A1 (en) 2018-11-29 2021-06-03 Araxes Pharma Llc Compounds and methods of use thereof for treatment of cancer
US11034710B2 (en) 2018-12-04 2021-06-15 Sumitomo Dainippon Pharma Oncology, Inc. CDK9 inhibitors and polymorphs thereof for use as agents for treatment of cancer
US12102646B2 (en) 2018-12-05 2024-10-01 Viking Therapeutics, Inc. Compositions for the treatment of fibrosis and inflammation
WO2020132651A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Kif18a inhibitors
MA54546A (fr) 2018-12-20 2022-03-30 Amgen Inc Amides d'hétéroaryle utiles en tant qu'inhibiteurs de kif18a
JP7676308B2 (ja) 2018-12-20 2025-05-14 アムジエン・インコーポレーテツド Ｋｉｆ１８ａ阻害剤として有用なヘテロアリールアミド
CA3123871A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Kif18a inhibitors
CA3127502A1 (en) 2019-02-12 2020-08-20 Sumitomo Dainippon Pharma Oncology, Inc. Formulations comprising heterocyclic protein kinase inhibitors
WO2020180768A1 (en) 2019-03-01 2020-09-10 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
MX2021010323A (es) 2019-03-01 2021-12-10 Revolution Medicines Inc Compuestos bicíclicos de heterociclilo y usos de este.
US11793802B2 (en) 2019-03-20 2023-10-24 Sumitomo Pharma Oncology, Inc. Treatment of acute myeloid leukemia (AML) with venetoclax failure
WO2020198077A1 (en) 2019-03-22 2020-10-01 Sumitomo Dainippon Pharma Oncology, Inc. Compositions comprising pkm2 modulators and methods of treatment using the same
US20220362394A1 (en) 2019-05-03 2022-11-17 Sutro Biopharma, Inc. Anti-bcma antibody conjugates
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
PH12021552922A1 (en) 2019-05-21 2022-04-04 Amgen Inc Solid state forms
US11529350B2 (en) 2019-07-03 2022-12-20 Sumitomo Pharma Oncology, Inc. Tyrosine kinase non-receptor 1 (TNK1) inhibitors and uses thereof
JP7756070B2 (ja) 2019-08-02 2025-10-17 アムジエン・インコーポレーテツド Ｋｉｆ１８ａ阻害剤としてのピリジン誘導体
JP7640521B2 (ja) 2019-08-02 2025-03-05 アムジエン・インコーポレーテツド Ｋｉｆ１８ａ阻害剤として有用なヘテロアリールアミド
MX2022001295A (es) 2019-08-02 2022-02-22 Amgen Inc Inhibidores de kif18a.
AU2020324406A1 (en) 2019-08-02 2022-03-17 Amgen Inc. KIF18A inhibitors
EP4031542B1 (en) 2019-09-18 2025-10-15 Merck Sharp & Dohme LLC Small molecule inhibitors of kras g12c mutant
TW202126636A (zh) 2019-09-30 2021-07-16 美商阿吉歐斯製藥公司 作為ｍｅｎｉｎ抑制劑之六氫吡啶化合物
AU2020369569A1 (en) 2019-10-24 2022-04-14 Amgen Inc. Pyridopyrimidine derivatives useful as KRAS G12C and KRAS G12D inhibitors in the treatment of cancer
UA129778C2 (uk) 2019-10-28 2025-07-30 Мерк Шарп Енд Доум Елелсі Низькомолекулярні інгібітори g12c-мутантного kras
CN119424423A (zh) 2019-10-31 2025-02-14 大鹏药品工业株式会社 4-氨基丁-2-烯酰胺衍生物及其盐
WO2021091956A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
CA3159561A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
AU2020379731A1 (en) 2019-11-04 2022-05-05 Revolution Medicines, Inc. Ras inhibitors
MX2022005525A (es) 2019-11-08 2022-06-08 Revolution Medicines Inc Compuestos de heteroarilo bicíclicos y usos de estos.
US12466825B2 (en) 2019-11-14 2025-11-11 Amgen Inc. Synthesis of KRAS G12C inhibitor compound
AR120456A1 (es) 2019-11-14 2022-02-16 Amgen Inc Síntesis mejorada del compuesto inhibidor de g12c de kras
EP4065231A1 (en) 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
WO2021106231A1 (en) 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
MX2022008305A (es) 2020-01-07 2022-08-08 Revolution Medicines Inc Dosificacion de inhibidores de shp2 y metodos de tratamiento del cancer.
WO2021155006A1 (en) 2020-01-31 2021-08-05 Les Laboratoires Servier Sas Inhibitors of cyclin-dependent kinases and uses thereof
EP4114852A1 (en) 2020-03-03 2023-01-11 Sutro Biopharma, Inc. Antibodies comprising site-specific glutamine tags, methods of their preparation and methods of their use
TW202204334A (zh) 2020-04-08 2022-02-01 美商阿吉歐斯製藥公司 Menin抑制劑及治療癌症之使用方法
TW202204333A (zh) 2020-04-08 2022-02-01 美商阿吉歐斯製藥公司 Menin抑制劑及治療癌症之使用方法
US20230174518A1 (en) 2020-04-24 2023-06-08 Taiho Pharmaceutical Co., Ltd. Kras g12d protein inhibitors
US20230181536A1 (en) 2020-04-24 2023-06-15 Taiho Pharmaceutical Co., Ltd. Anticancer combination therapy with n-(1-acryloyl-azetidin-3-yl)-2-((1h-indazol-3-yl)amino)methyl)-1h-imidazole-5-carboxamide inhibitor of kras-g12c
TW202214253A (zh) 2020-06-18 2022-04-16 美商銳新醫藥公司 延遲、預防及治療對ｒａｓ抑制劑之後天抗性之方法
EP4178571A4 (en) 2020-07-10 2024-07-17 The Regents Of The University Of Michigan GAS41 INHIBITORS AND METHODS OF USE
KR20230031926A (ko) 2020-07-15 2023-03-07 다이호야쿠힌고교 가부시키가이샤 종양의 치료에 사용되는 피리미딘 화합물을 포함하는 조합
CA3187757A1 (en) 2020-09-03 2022-03-24 Ethan AHLER Use of sos1 inhibitors to treat malignancies with shp2 mutations
PE20231207A1 (es) 2020-09-15 2023-08-17 Revolution Medicines Inc Derivados indolicos como inhibidores de ras en el tratamiento del cancer
TW202237119A (zh) 2020-12-10 2022-10-01 美商住友製藥腫瘤公司 Ａｌｋ﹘５抑制劑和彼之用途
CN117396472A (zh) 2020-12-22 2024-01-12 上海齐鲁锐格医药研发有限公司 Sos1抑制剂及其用途
EP4323356A1 (en) 2021-04-13 2024-02-21 Nuvalent, Inc. Amino-substituted heterocycles for treating cancers with egfr mutations
US11931420B2 (en) 2021-04-30 2024-03-19 Celgene Corporation Combination therapies using an anti-BCMA antibody drug conjugate (ADC) in combination with a gamma secretase inhibitor (GSI)
PE20240089A1 (es) 2021-05-05 2024-01-16 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cancer
MX2023013085A (es) 2021-05-05 2023-11-16 Revolution Medicines Inc Inhibidores de ras.
CN117500811A (zh) 2021-05-05 2024-02-02 锐新医药公司 共价ras抑制剂及其用途
WO2022250170A1 (en) 2021-05-28 2022-12-01 Taiho Pharmaceutical Co., Ltd. Small molecule inhibitors of kras mutated proteins
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023056589A1 (en) 2021-10-08 2023-04-13 Servier Pharmaceuticals Llc Menin inhibitors and methods of use for treating cancer
TW202340214A (zh) 2021-12-17 2023-10-16 美商健臻公司 做為shp2抑制劑之吡唑并吡𠯤化合物
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
JP2025509217A (ja) 2022-03-07 2025-04-11 アムジエン・インコーポレーテツド ４－メチル－２－プロパン－２－イル－ピリジン－３－カルボニトリルを調製するための方法
CN119136806A (zh) 2022-03-08 2024-12-13 锐新医药公司 用于治疗免疫难治性肺癌的方法
WO2023211812A1 (en) 2022-04-25 2023-11-02 Nested Therapeutics, Inc. Heterocyclic derivatives as mitogen-activated protein kinase (mek) inhibitors
CN120504682A (zh) 2022-06-10 2025-08-19 锐新医药公司 大环ras抑制剂
CN120076831A (zh) 2022-06-30 2025-05-30 苏特罗生物制药公司 抗ror1抗体和抗体缀合物、包含抗ror1抗体或抗体缀合物的组合物、以及制备和使用抗ror1抗体和抗体缀合物的方法
MA71389A (fr) 2022-07-08 2025-04-30 Nested Therapeutics, Inc. Inhibiteurs de protéine kinase activée par mitogène (mek)
IL320217A (en) 2022-10-14 2025-06-01 Black Diamond Therapeutics Inc Methods for treating cancer using isoquinoline or 6-azaquinoline derivatives
KR20250164828A (ko) 2023-03-30 2025-11-25 레볼루션 메디슨즈, 인크. Ras gtp 가수분해 유도를 위한 조성물 및 이의 용도
AU2024253668A1 (en) 2023-04-07 2025-11-13 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2024211712A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
CN121100123A (zh) 2023-04-14 2025-12-09 锐新医药公司 Ras抑制剂的结晶形式
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
WO2024226579A1 (en) 2023-04-24 2024-10-31 Nested Therapeutics, Inc. Heterocyclic derivative as mitogen-activated protein kinase (mek) inhibitor
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ｒａｓ相關疾病或病症之組合療法
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
TW202515582A (zh) 2023-08-24 2025-04-16 日商大塚製藥股份有限公司 西區嘧啶(cedazuridine)之固定劑量組合
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors
WO2025081117A2 (en) 2023-10-13 2025-04-17 Sutro Biopharma, Inc. Anti-tissue factor antibodies and antibody conjugates, compositions comprising anti-tissue factor antibodies or antibody conjugates, and methods of making and using anti-tissue factor antibodies and antibody conjugates
TW202535891A (zh) 2023-10-20 2025-09-16 美商默沙東有限責任公司 Ｋｒａｓ蛋白之小分子抑制劑
WO2025090905A1 (en) 2023-10-26 2025-05-01 Nested Therapeutics, Inc. Crystalline forms of 3-[[3-fluoro-2-(methylsulfamoylamino)-4-pyridyl]methyl]-7-[(3-fluoro-2-pyridyl)oxy]-4-methyl-chromen-2-one
WO2025137507A1 (en) 2023-12-22 2025-06-26 Regor Pharmaceuticals, Inc. Sos1 inhibitors and uses thereof
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025250825A1 (en) 2024-05-30 2025-12-04 Sutro Biopharma, Inc. Anti-trop2 antibodies, compositions comprising anti-trop2 antibodies and methods of making and using anti-trop2 antibodies

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZW23187A1 (en) * 1986-12-15 1988-06-29 Hoffmann La Roche Phosphinic acid derivatives
CA2058797A1 (en) * 1991-02-01 1992-08-02 Michael John Broadhurst Amino acid derivatives
WO1993014112A1 (en) * 1992-01-15 1993-07-22 Merck & Co., Inc. Substituted phosphinic acid-containing peptidyl derivatives as antidegenerative agents
UA48121C2 (uk) * 1993-11-04 2002-08-15 Сінтекс (С.Ш.А.) Інк. Інгібітори матричних металопротеаз і фармацетична композиція на їх основі

Also Published As

Publication number Publication date
CA2260898A1 (en) 1998-01-29
CO4890852A1 (es) 2000-02-28
HN1997000099A (es) 1997-12-28
CN1225639A (zh) 1999-08-11
CZ11899A3 (cs) 1999-11-17
PT923585E (pt) 2002-08-30
CA2260898C (en) 2002-05-14
AU712973B2 (en) 1999-11-18
NZ333303A (en) 2000-06-23
JP3299975B2 (ja) 2002-07-08
BR9710381A (pt) 1999-08-17
GT199700085A (es) 1999-01-06
ES2175415T3 (es) 2002-11-16
OA10956A (en) 2001-10-30
PL331254A1 (en) 1999-07-05
EA199900036A1 (ru) 1999-06-24
DK0923585T3 (da) 2002-07-01
ID19443A (id) 1998-07-09
HRP970391A2 (en) 1998-08-31
PA8433701A1 (es) 1999-12-27
PE88198A1 (es) 1998-12-21
ATE217315T1 (de) 2002-05-15
AU3104297A (en) 1998-02-10
IS4928A (is) 1998-12-18
EP0923585B1 (en) 2002-05-08
NO990184L (no) 1999-03-15
DE69712496D1 (de) 2002-06-13
ZA976330B (en) 1999-01-19
AR008260A1 (es) 1999-12-29
DE69712496T2 (de) 2002-08-29
AP761A (en) 1999-09-13
EP0923585A1 (en) 1999-06-23
JPH11514673A (ja) 1999-12-14
HUP9903014A2 (en) 2000-07-28
US6147061A (en) 2000-11-14
SI0923585T1 (en) 2002-08-31
TNSN97122A1 (fr) 2005-03-15
AP9701043A0 (en) 1997-07-31
YU1899A (sh) 2000-03-21
WO1998003516A1 (en) 1998-01-29
MA24270A1 (fr) 1998-04-01
IL127567A0 (en) 1999-10-28
BG103111A (en) 1999-11-30
KR20000067904A (ko) 2000-11-25
NO990184D0 (no) 1999-01-15
HUP9903014A3 (en) 2000-08-28
SK3799A3 (en) 2000-03-13

Similar Documents

Publication Publication Date Title
TR199900066T2 (tr) Matriks metalloproteazlarin fosfinat bazli inhibitörleri
YU37499A (sh) Derivati arilsulfonil hidroksamske kiseline
AP9801174A0 (en) Cyclic sulfone derivatives.
MY121754A (en) Arylsulfonylamino hydroxamic acid derivatives
MY113586A (en) Aylsulfonylamino hydroxamic acid derivatives
TR199801151T2 (tr) Trombin inhibitörü ön ilaçlar.
TR200000059T2 (tr) Piridin türevleri
TR200000289T2 (tr) Kimyasal bileşimler
ATE165830T1 (de) Dihydro pyrazolopyrrole
BG106586A (en) Pyrazolopyramidines as therapeutic agents
CA2218503A1 (en) Arylsulfonyl hydroxamic acid derivatives
DE69713151D1 (de) Cyclosporinderivat, dessen herstellung und pharmazeutische zusammensetzung
FR2781218B1 (fr) Compositions pharmaceutiques comprenant des 2-quinolones
NO20011453L (no) Arylsulfonanilid urea
TR200000223T2 (tr) XA faktörünü engelleyen heterosiklik türevler
TR200101978T2 (tr) 3,3-Biarilpiperidin ve 2,2-biarilmorfolin türevleri.
AP2000001761A0 (en) Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase.
DE69622260D1 (de) 2-arylbenzazole verbindungen
TR200000637T2 (tr) Benzoksazin ve benzotiazin türevleri ve bunların ilaçlarda kullanımı.
EP0831869A4 (en) DIPHOSPHONATE DERIVATIVES OF THERAPEUTIC AGENTS
TR200001941T1 (tr) TNF ve PDE-IV önleyici aktiviteye sahip heterosiklik bileşiklerin N-oksitleri.
DE69911017D1 (en) Arylsulfonanilid-phosphate
MX9801892A (es) Nitrones ciclicos y composiciones farmaceuticas que los contienen.
TR200100059T2 (tr) Yeni antimikrobik bileşimler
TR200102306T2 (tr) Faktör Xa önleyici olarak heterosiklik türevler.