Nothing Special   »   [go: up one dir, main page]

PE20081888A1 - ANALOGOS DE PIRAZOLOPIRIMIDINA Y SU USO COMO INHIBIDORES DE CINASA mTOR Y CINASA PI3 - Google Patents

ANALOGOS DE PIRAZOLOPIRIMIDINA Y SU USO COMO INHIBIDORES DE CINASA mTOR Y CINASA PI3

Info

Publication number
PE20081888A1
PE20081888A1 PE2008000501A PE2008000501A PE20081888A1 PE 20081888 A1 PE20081888 A1 PE 20081888A1 PE 2008000501 A PE2008000501 A PE 2008000501A PE 2008000501 A PE2008000501 A PE 2008000501A PE 20081888 A1 PE20081888 A1 PE 20081888A1
Authority
PE
Peru
Prior art keywords
kinase
pyridin
inhibitors
morfolin
pyrimidin
Prior art date
Application number
PE2008000501A
Other languages
English (en)
Inventor
Arie Zask
Pawel Nowak
Jeroen Verheijen
Kevin CURRAN
Joshua Kaplan
Davil Malwitz
Matthew Gregory Bursavich
Derek Cecil Cole
Semiramis Ayral-Kaloustian
Ker Yu
David James Richard
Mark Lefever
Original Assignee
Wyeth Corp
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 Wyeth Corp filed Critical Wyeth Corp
Publication of PE20081888A1 publication Critical patent/PE20081888A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE PIRAZOLOPIRIMIDINA DE FORMULA (Ia) DONDE R1 ES UN COMPUESTO DE FORMULA (i) EN DONDE X5 ES -O-, -CH2-O- O -S(O)n; n ES DE 0 A 2; R2 ES ARILO(C6-C14) OPCIONALMENTE SUSTITUIDO CON HALOGENO, ALQUILO(C1-C6), ALCOXI(C1-C6), ENTRE OTROS SUSTITUYENTES, HETEROARILO, -HC=CH-ARILO(C6-C14), ENTRE OTROS; R3 ES H, ALQUENILO(C2-C10), ALQUINILO(C2-C10), ARILO(C6-C14), HIDROXIALQUILO(C1-C6), ENTRE OTROS; R13 ES H, HALOGENO, ALQUILO(C1-C6), ALQUENILO(C2-C6), ALQUINILO(C2-C6), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 1-(4-{4-MORFOLIN-4-IL-1-[1-(PIRIDIN-3-ILCARBONIL)PIPERIDIN-4-IL]-1H-PIRAZOLO[3,4-d]PIRIMIDIN-6-IL}FENIL)-3-PIRIDIN-3-ILUREA, 1-(4-{4-MORFOLIN-4-IL-1-[1-(PIRIDIN-3-ILCARBONIL)PIPERIDIN-4-IL]-1H-PIRAZOLO[3,4-d]PIRIMIDIN-6-IL}FENIL)-3-(3-TIENIL)UREA, 1-(4-{4-MORFOLIN-4-IL-1-[1-(PIRIDIN-3-ILCARBONIL)PIPERIDIN-4-IL]-1H-PIRAZOLO[3,4-d]PIRIMIDIN-6-IL}FENIL)-3-PIRIDIN-4-ILUREA, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE mTOR Y DE LA CINASA FOSFATIDILINOSITOL-3 (PI3K) SIENDO UTILES EN EL TRATAMIENTO DE CANCER, ATEROSCLEROSIS, ARTRITIS, PSORIASIS
PE2008000501A 2007-03-21 2008-03-19 ANALOGOS DE PIRAZOLOPIRIMIDINA Y SU USO COMO INHIBIDORES DE CINASA mTOR Y CINASA PI3 PE20081888A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US91930107P 2007-03-21 2007-03-21

Publications (1)

Publication Number Publication Date
PE20081888A1 true PE20081888A1 (es) 2008-12-20

Family

ID=39766744

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008000501A PE20081888A1 (es) 2007-03-21 2008-03-19 ANALOGOS DE PIRAZOLOPIRIMIDINA Y SU USO COMO INHIBIDORES DE CINASA mTOR Y CINASA PI3

Country Status (13)

Country Link
US (1) US20080234262A1 (es)
EP (1) EP2078021A2 (es)
JP (1) JP2010522195A (es)
CN (1) CN101675051A (es)
AR (1) AR065812A1 (es)
AU (1) AU2008228964A1 (es)
BR (1) BRPI0809239A2 (es)
CA (1) CA2681501A1 (es)
CL (1) CL2008000815A1 (es)
MX (1) MX2009010132A (es)
PE (1) PE20081888A1 (es)
TW (1) TW200900404A (es)
WO (1) WO2008115974A2 (es)

Families Citing this family (110)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE456836T1 (de) * 1996-09-04 2010-02-15 Intertrust Tech Corp Zuverlässige infrastrukturhilfssysteme, verfahren und techniken für sicheren elektronischen handel, elektronische transaktionen, handelsablaufsteuerung und automatisierung, verteilte verarbeitung und rechteverwaltung
ATE554075T1 (de) * 2007-07-09 2012-05-15 Astrazeneca Ab Bei mit mtor-kinase und/oder pi3k in zusammenhang stehenden krankheiten angewendete morpholinopyrimidinderivate
JP5520831B2 (ja) 2007-12-19 2014-06-11 アムジエン・インコーポレーテツド Ｐｉ３キナーゼの阻害薬
CN101945867A (zh) 2007-12-19 2011-01-12 安姆根有限公司 作为细胞周期抑制剂的稠合吡啶、嘧啶和三嗪化合物
US8987280B2 (en) * 2008-01-30 2015-03-24 Genentech, Inc. Pyrazolopyrimidine PI3K inhibitor compounds and methods of use
WO2009126584A1 (en) 2008-04-07 2009-10-15 Amgen Inc. Gem-disubstituted and spirocyclic amino pyridines/pyrimidines as cell cycle inhibitors
UA101676C2 (uk) * 2008-07-31 2013-04-25 Дженентек, Инк. Піримідинові сполуки, композиції і способи застосування
ES2464461T3 (es) 2008-09-22 2014-06-02 Array Biopharma, Inc. Compuestos de imidazo[1,2B]piridazina sustituidos como inhibidores de la TRK cinasa
TWI378933B (en) 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
KR101853026B1 (ko) 2008-10-22 2018-04-27 어레이 바이오파마 인크. ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물
KR20110098908A (ko) * 2008-11-11 2011-09-02 엑스커버리 홀딩 컴퍼니 엘엘씨 ＰＩ3Ｋ/ｍＴＯＲ 키나제 억제제
ES2529205T3 (es) 2009-03-13 2015-02-17 Cellzome Limited Derivados de pirimidina como inhibidores de mTOR
SG174527A1 (en) 2009-03-27 2011-11-28 Pathway Therapeutics Inc Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy
WO2010114894A1 (en) 2009-03-31 2010-10-07 Arqule, Inc. Substituted heterocyclic compounds
US20120114637A1 (en) * 2009-05-04 2012-05-10 Santen Pharmaceutical Co., Ltd. Mtor pathway inhibitors for treating ocular disorders
SG176959A1 (en) * 2009-06-24 2012-01-30 Genentech Inc Oxo-heterocycle fused pyrimidine compounds, compositions and methods of use
EP2448942B1 (en) * 2009-07-02 2014-09-24 Merck Sharp & Dohme Corp. FUSED TRICYCLIC COMPOUNDS AS mTOR INHIBITORS
EP2532659A1 (en) 2009-07-07 2012-12-12 Pathway Therapeutics, Inc. Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
WO2011022439A1 (en) * 2009-08-17 2011-02-24 Intellikine, Inc. Heterocyclic compounds and uses thereof
SG10201405598QA (en) * 2009-09-09 2014-11-27 Celgene Avilomics Res Inc Pi3 kinase inhibitors and uses thereof
DE102009049679A1 (de) * 2009-10-19 2011-04-21 Merck Patent Gmbh Pyrazolopyrimidinderivate
KR101469334B1 (ko) * 2009-11-12 2014-12-04 에프. 호프만-라 로슈 아게 Ｎ-9-치환된 퓨린 화합물, 조성물 및 사용 방법
RU2515541C2 (ru) * 2009-11-12 2014-05-10 Ф.Хоффманн-Ля Рош Аг N-7 замещенные пурины и пиразолопиримидины, их композиции и способы применения
WO2011097333A1 (en) 2010-02-03 2011-08-11 Signal Pharmaceuticals, Llc Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors
WO2011107585A1 (en) 2010-03-04 2011-09-09 Cellzome Limited Morpholino substituted urea derivatives as mtor inhibitors
EP2571884A4 (en) * 2010-05-19 2014-03-19 Xcovery Holding Co Llc SELECTIVE MTOR KINASE HEMMER
MY191934A (en) 2010-05-20 2022-07-19 Array Biopharma Inc Macrocyclic compounds as trk kinase inhibitors
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
WO2012099581A1 (en) 2011-01-19 2012-07-26 Takeda Pharmaceutical Company Limited Dihydrofuropyrimidine compounds
US9127000B2 (en) 2011-02-23 2015-09-08 Intellikine, LLC. Heterocyclic compounds and uses thereof
AR085397A1 (es) 2011-02-23 2013-09-25 Intellikine Inc Combinacion de inhibidores de quinasa y sus usos
DK2688887T3 (en) 2011-03-23 2015-06-29 Amgen Inc DEHYDRATED tricyclic DUALINHIBITORER OF CDK 4/6 AND FLT3
TWI572599B (zh) 2011-03-28 2017-03-01 Ｍｅｉ製藥公司 （α－經取代之芳烷胺基及雜芳烷胺基）嘧啶基及１，３，５－三基苯并咪唑，其醫藥組合物及其在治療增生性疾病之用途
JP2014510122A (ja) 2011-04-04 2014-04-24 セルゾーム リミテッド ｍＴＯＲ阻害剤としてのジヒドロピロロピリミジン誘導体
CN103857804A (zh) 2011-08-03 2014-06-11 西格诺药品有限公司 作为lkb1状态的预测性生物标志物的基因表达谱的鉴定
CN103917530B (zh) 2011-09-21 2016-08-24 塞尔佐姆有限公司 作为mtor抑制剂的吗啉代取代的脲或氨基甲酸衍生物
AU2012320465B2 (en) 2011-10-07 2016-03-03 Cellzome Limited Morpholino substituted bicyclic pyrimidine urea or carbamate derivatives as mTOR inhibitors
CN103130793B (zh) * 2011-11-30 2016-09-21 中国人民解放军军事医学科学院毒物药物研究所 3-(1-芳基哌啶-4-基)-2-芳基噻唑啉-4-酮类化合物、其制备方法及用途
KR20160027217A (ko) 2012-05-23 2016-03-09 에프. 호프만-라 로슈 아게 내배엽 및 간세포를 수득하고 사용하는 조성물 및 방법
BR112014030410A2 (pt) * 2012-06-07 2017-06-27 Hoffmann La Roche inibidores de pirazolopirimidona e pirazolopiridona de tanquirase
SG10201610416TA (en) 2012-06-13 2017-01-27 Incyte Corp Substituted tricyclic compounds as fgfr inhibitors
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
AU2013203714B2 (en) 2012-10-18 2015-12-03 Signal Pharmaceuticals, Llc Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
TWI629275B (zh) * 2013-03-13 2018-07-11 賽諾菲公司 Ｎ－（４－（氮雜吲唑－６－基）－苯基）－磺醯胺及其作為醫藥之用途
WO2014151009A1 (en) * 2013-03-15 2014-09-25 Dow Agrosciences Llc 4-amino-6-(heterocyclic)picolinates and 6-amino-2-(heterocyclic) pyrimidine-4-carboxylates and their use as herbicides
UA126851C2 (uk) 2013-03-15 2023-02-15 Кортева Аґрисайєнс Елелсі 4-аміно-6-(гетероцикліл)піколінати і 6-аміно-2-(гетероцикліл)піримідин-4-карбоксилати і їхнє застосування як гербіцидів
US9637505B2 (en) 2013-03-15 2017-05-02 Dow Agrosciences Llc 4-amino-6-(heterocyclic)picolinates and 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their use as herbicides
AU2014254053B2 (en) 2013-04-17 2019-06-06 Signal Pharmaceuticals, Llc Treatment of cancer with Dihydropyrazino-Pyrazines
TWI654979B (zh) 2013-04-17 2019-04-01 美商標誌製藥公司 使用ｔｏｒ激酶抑制劑組合療法以治療癌症之方法
MY189663A (en) 2013-04-17 2022-02-23 Signal Pharm Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer
JP2016516818A (ja) 2013-04-17 2016-06-09 シグナル ファーマシューティカルズ，エルエルシー 癌を治療するためのｔｏｒキナーゼ阻害剤及びｎ−（３−（５−フルオロ−２−（４−（２−メトキシエトキシ）フェニルアミノ）ピリミジン−４−イルアミノ）フェニル）アクリルアミドを含む組合せ療法
SG11201508223YA (en) 2013-04-17 2015-11-27 Signal Pharm Llc Treatment of cancer with dihydropyrazino-pyrazines
AU2014254059B2 (en) 2013-04-17 2019-06-06 Signal Pharmaceuticals, Llc Combination therapy comprising a TOR kinase inhibitor and a cytidine analog for treating cancer
US9359364B2 (en) 2013-04-17 2016-06-07 Signal Pharmaceuticals, Llc Pharmaceutical formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b] pyrazin-2(1H)-one
HUE036571T2 (hu) 2013-04-19 2018-07-30 Incyte Holdings Corp Biciklusos heterociklusok mint FGFR inhibitorok
CN109503591B (zh) 2013-05-29 2022-03-01 西格诺药品有限公司 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途
CN106414446A (zh) * 2014-03-13 2017-02-15 新加坡科技研究局 基于稠合嘧啶的异羟肟酸盐衍生物
EP3131551A4 (en) 2014-04-16 2017-09-20 Signal Pharmaceuticals, LLC SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL) PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-b)PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF
NZ714742A (en) 2014-04-16 2017-04-28 Signal Pharm Llc Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use
MX2016014878A (es) 2014-05-14 2017-03-08 Pfizer Pirazolopiridinas y pirazolopirimidinas.
TWI689252B (zh) 2014-09-15 2020-04-01 美商陶氏農業科學公司 源自於施用吡啶羧酸除草劑與乙醯乳酸合成酶（ａｌｓ）抑制劑的協同性雜草控制
TWI694770B (zh) 2014-09-15 2020-06-01 美商陶氏農業科學公司 包含吡啶羧酸除草劑之安全的除草組成物（二）
TWI685302B (zh) 2014-09-15 2020-02-21 美商陶氏農業科學公司 包含吡啶羧酸除草劑之安全的除草組成物
TWI689251B (zh) 2014-09-15 2020-04-01 美商陶氏農業科學公司 源自於施用吡啶羧酸除草劑與合成生長素除草劑及/或生長素轉運抑制劑的協同性雜草控制
AR101863A1 (es) 2014-09-15 2017-01-18 Dow Agrosciences Llc Control sinérgico de malezas a partir de aplicaciones de herbicidas de ácido piridín carboxílico e inhibidores de fotosistema ii
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
FI3699181T3 (fi) 2014-11-16 2023-03-28 Array Biopharma Inc Kiteinen muoto (s)-n-(5-((r)-2-(2,5-diluorifenyyli)-pyrrolidin-1-yyli)-pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidivetyysulfaatista
LT3233054T (lt) * 2014-12-17 2021-07-26 Pfizer Inc. Pi3k/mtor inhibitoriaus vaisto formos, skirtos intraveniniam įvedimui
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
EP3259269B9 (en) 2015-02-20 2020-03-04 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3003153A1 (en) 2015-10-26 2017-05-04 Loxo Oncology, Inc. Point mutations in trk inhibitor-resistant cancer and methods relating to the same
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
CA3019671C (en) 2016-04-04 2024-02-20 Loxo Oncology, Inc. Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
RS61463B1 (sr) 2016-05-18 2021-03-31 Loxo Oncology Inc Priprema (s)-n-(5-((r)-2-(2,5-difluorofenil)pirolidin-1-il)pirazolo[1,5-a]pirimidin-3-il) -3-hidroksipirolidin-1-karboksamida
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
CA3061907A1 (en) 2017-05-02 2018-11-08 Revolution Medicines, Inc. Rapamycin analogs as mtor inhibitors
JP2020521739A (ja) 2017-05-23 2020-07-27 エムイーアイ ファーマ，インク． 併用療法
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
WO2018237114A1 (en) 2017-06-22 2018-12-27 Celgene Corporation TREATMENT OF HEPATOCELLULAR CARCINOMA CHARACTERIZED BY HEPATITIS B VIRUS INFECTION
MX2020001261A (es) * 2017-08-02 2020-08-17 Univ Northwestern Compuestos de pirimidina fusionada sustituida y usos de los mismos.
AU2018318129A1 (en) 2017-08-14 2020-03-26 Mei Pharma, Inc. Combination therapy
PL3788049T3 (pl) 2018-05-01 2023-06-19 Revolution Medicines, Inc. Połączone z C40, C28 i C32 analogi rapamycyny jako inhibitory mTOR
EP3788050B1 (en) 2018-05-01 2024-08-28 Revolution Medicines, Inc. C26-linked rapamycin analogs as mtor inhibitors
MX2020011639A (es) 2018-05-04 2021-02-15 Incyte Corp Sales de un inhibidor de receptores de factor de crecimiento de fibroblastos (fgfr).
JP2021523121A (ja) 2018-05-04 2021-09-02 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｆｇｆｒ阻害剤の固体形態及びその調製プロセス
CN110833551B (zh) * 2018-08-15 2023-03-24 广西梧州制药（集团）股份有限公司 吡唑并嘧啶衍生物在治疗急性胰腺炎的用途
CN110950868B (zh) * 2018-09-27 2022-05-13 苏州锐明新药研发有限公司 吡唑并嘧啶化合物及制备方法与制备抗癌症药物的应用
CN111646995B (zh) * 2019-03-04 2023-03-21 四川大学 4-氨基-嘧啶并氮杂环-苯基脲类衍生物及其制备方法和用途
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
EP3800188A1 (en) * 2019-10-02 2021-04-07 Bayer AG Substituted pyrazolopyrimidines as irak4 inhibitors
PE20221085A1 (es) 2019-10-14 2022-07-05 Incyte Corp Heterociclos biciclicos como inhibidores de fgfr
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US11897891B2 (en) 2019-12-04 2024-02-13 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
PE20221504A1 (es) 2019-12-04 2022-09-30 Incyte Corp Derivados de un inhibidor de fgfr
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2022106579A1 (en) * 2020-11-20 2022-05-27 Institut National De La Sante Et De La Recherche Medicale (Inserm) Compounds for treating a disease associated with macrophage senescence
CN112552312B (zh) * 2020-12-07 2022-08-05 杭州科巢生物科技有限公司 一种瑞卢戈利或其盐的合成方法
CA3207998A1 (en) 2021-02-16 2022-08-25 Geoffrey M. Lynn Self-assembling nanoparticles based on amphiphilic peptides
US12065494B2 (en) 2021-04-12 2024-08-20 Incyte Corporation Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent
JP2024522189A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式ヘテロ環
WO2022268025A1 (zh) * 2021-06-22 2022-12-29 成都苑东生物制药股份有限公司 Atr抑制剂及其用途
TW202402277A (zh) 2022-05-25 2024-01-16 美商銳新醫藥公司 以mtor抑制劑治療癌症之方法
CN115304600B (zh) * 2022-09-29 2023-01-13 北京鑫开元医药科技有限公司 mTOR抑制剂、制备方法及用途
WO2024092030A1 (en) 2022-10-25 2024-05-02 Vaccitech North America, Inc. Self-assembling nanoparticles

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3847908A (en) * 1973-03-05 1974-11-12 Squibb & Sons Inc 6-styrylpyrazolo(3,4-d)pyrimidinones and pyrimidines
AU2006217742A1 (en) * 2005-02-25 2006-08-31 Kudos Pharmaceuticals Limited Hydrazinomethyl, HYDR zonomethyl and 5-membered heterocylic compounds which act as MTOR inhibitors and their use as anti cancer agents
GB0510390D0 (en) * 2005-05-20 2005-06-29 Novartis Ag Organic compounds
EA200870409A1 (ru) * 2006-04-04 2009-04-28 Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния Антагонисты киназы pi3

Also Published As

Publication number Publication date
CA2681501A1 (en) 2008-09-25
WO2008115974A3 (en) 2008-12-18
US20080234262A1 (en) 2008-09-25
AU2008228964A1 (en) 2008-09-25
WO2008115974A2 (en) 2008-09-25
TW200900404A (en) 2009-01-01
AU2008228964A8 (en) 2009-11-19
JP2010522195A (ja) 2010-07-01
BRPI0809239A2 (pt) 2014-11-25
EP2078021A2 (en) 2009-07-15
MX2009010132A (es) 2009-10-12
CL2008000815A1 (es) 2008-05-30
CN101675051A (zh) 2010-03-17
AR065812A1 (es) 2009-07-01

Similar Documents

Publication Publication Date Title
PE20081888A1 (es) ANALOGOS DE PIRAZOLOPIRIMIDINA Y SU USO COMO INHIBIDORES DE CINASA mTOR Y CINASA PI3
PE20141050A1 (es) Inhibidores de quinasa relacionados con pirrolo (2,3-d) pirimidina tropomiosina
PE20151249A1 (es) Derivados de pirazolopirimidina como inhibidores de jak quinasas
PE20110545A1 (es) Compuestos de triazolopiridina como inhibidores de jak
PE20070855A1 (es) Derivados de 4-amino-pirrolotriazina sustituida como inhibidores de quinasas
PE20110828A1 (es) Compuestos de pirazolopirimidina como inhibidores de jak
NZ591712A (en) Imidazopyridazinecarbonitriles useful as kinase inhibitors
CL2011001360A1 (es) Compuestos derivados de imidazol[1,2-a]pirazin-8-amina, inhibidores de tirosina quinasa esplenica; composicion farmaceutica que comprende un compuesto; uso de los compuestos en la preparacion de medicamentos para el tratamiento de trastornos alergicos, enfermedades autoinmunes y enfermedades inflamatorias; y metodo in vitro.
PE20120493A1 (es) Pirimidinonas como inhibidores de pi3k
PE20090887A1 (es) DERIVADOS DE 1H-PIRAZOL-[3,4-d]-PIRIMIDINA, 9H-PURINA Y 7H-PIRROL-[2,3-d]-PIRIMIDINA COMO INHIBIDORES DE CINASA P70 S6
PE20140192A1 (es) Derivados de bencimidazol como inhibidores de cinasa pi3
PE20121180A1 (es) (heteroarilmetil) tiohidantoinas sustituidas como drogas anticancer
PE20190656A1 (es) Compuestos de tiazolo-piridina sustituida como inhibidores de malt1
PE20091068A1 (es) Compuestos pirrolo[3,2-d]pirimidina y su uso como inhibidores de quinasa pi3 y quinasa mtor
PE20080527A1 (es) Derivado de pirimidina como inhibidor de la fosfatidilinositol 3-quinasa (pi3k)
CL2011000880A1 (es) Compuestos derivados de pirazolo[1,5-a]pirimidin-3-il, inhibidores de tirosina de la familia trk cinasa; proceso para la preparacion de los compuestos; composicion farmaceutica que comprende a uno de los compuestos; y uso de los compuestos en la preparacion de medicamentos utiles para el tratamiento del dolor y del cancer.
EA201001017A1 (ru) 3h-[1,2,3]триазоло[4,5-d]пиримидиновые соединения, их применение в качестве ингибиторов киназы mtor и киназы pi3 и их синтезы
PE20090210A1 (es) Compuestos derivados de pirazolo pirimidina como inhibidores de jak quinasa
PE20170663A1 (es) Compuestos de 5- cloro- 2- difluorometoxifenil pirazolopirimidina, composiciones y metodos de uso de los mismos
ATE545647T1 (de) 5,6,7,8-tetrahydro-imidazoä1,5-aüpyrazinderivat
EA201301319A1 (ru) Производные пиридин-2(1н)-она, применимые в качестве лекарственных средств для лечения миелопролиферативных нарушений, отторжения трансплантата, иммунологически обусловленных и воспалительных заболеваний
PE20121529A1 (es) Compuestos derivados de piridopirimidina como inhibidores de pde4
PE20080931A1 (es) Imidazopirazinas como inhibidores de proteina quinasa
ECSP045253A (es) Derivados de 5-feniltiazol y uso como inhibidores de pi3 cinasa
AR062886A1 (es) Compuestos de tiazol pirazolopirimidina, composicion farmaceutica que lo comprende y su uso para preparar un medicamento

Legal Events

Date Code Title Description
FD Application declared void or lapsed