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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
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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.)
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Publication date
Application filed by Wyeth Corp filed Critical Wyeth Corp
Publication of PE20081888A1 publication Critical patent/PE20081888A1/es

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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (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 (111)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1679668B1 (en) * 1996-09-04 2010-01-27 Intertrust Technologies Corp. Trusted infrastructure support systems, methods and techniques for secure electronic commerce, electronic transactions, commerce process control and automation, distributed computing, and rights management
ES2385692T3 (es) * 2007-07-09 2012-07-30 Astrazeneca Ab Derivados de morfolino pirimidina usados en enfermedades relacionadas con mTOR quinasa y/o PI3K
EP2231656A1 (en) 2007-12-19 2010-09-29 Amgen Inc. Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors
CA2710194C (en) 2007-12-19 2014-04-22 Amgen Inc. Inhibitors of p13 kinase
CN101981037B (zh) * 2008-01-30 2013-09-04 吉宁特有限公司 吡唑并嘧啶pi3k抑制剂化合物及使用方法
MX2010010975A (es) 2008-04-07 2010-11-01 Amgen Inc Amino piridinas/pirimidinas gem-disustituidas y espirociclicas como inhibidores de ciclo celular.
JP2011529920A (ja) * 2008-07-31 2011-12-15 ジェネンテック， インコーポレイテッド ピリミジン化合物、組成物及び使用方法
CA2738026C (en) 2008-09-22 2017-01-24 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors
TWI378933B (en) 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
EP2725028B1 (en) 2008-10-22 2016-05-25 Array Biopharma, Inc. Substituted pyrazolo[1,5-]pyrimidine compounds as intermediates in the synthesis of TRK kinase inhibitors
JP5877064B2 (ja) * 2008-11-11 2016-03-02 エックスカバリー ホールディング カンパニー エルエルシー ＰＩ３Ｋ／ｍＴＯＲキナーゼ阻害剤
EP2406258B1 (en) 2009-03-13 2014-12-03 Cellzome Limited PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
NZ595372A (en) * 2009-03-27 2013-11-29 Vetdc 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
WO2010151601A1 (en) * 2009-06-24 2010-12-29 Genentech, Inc. Oxo-heterocycle fused pyrimidine compounds, compositions and methods of use
WO2011002887A1 (en) * 2009-07-02 2011-01-06 Schering Corporation FUSED TRICYCLIC COMPOUNDS AS NOVEL mTOR INHIBITORS
DK3072890T3 (en) 2009-07-07 2019-02-11 Mei Pharma Inc Pyrimidinyl and 1,3,5-triazinylbenzimidazoles 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
EA026693B1 (ru) * 2009-08-17 2017-05-31 Интелликайн ЭлЭлСи Производные бензоксазола и бензотиазола в качестве ингибиторов pi3-киназы
RU2595718C2 (ru) * 2009-09-09 2016-08-27 Селджен Авиломикс Рисерч,Инк. Ингибиторы pi3-киназы и их применение
DE102009049679A1 (de) 2009-10-19 2011-04-21 Merck Patent Gmbh Pyrazolopyrimidinderivate
RU2515541C2 (ru) * 2009-11-12 2014-05-10 Ф.Хоффманн-Ля Рош Аг N-7 замещенные пурины и пиразолопиримидины, их композиции и способы применения
MX2012005463A (es) * 2009-11-12 2012-09-12 Hoffmann La Roche Compuestos de purina n/9 sustituida, composiciones y metodos de uso.
BR112012019459A2 (pt) 2010-02-03 2017-10-17 Signal Pharm Llc identificação de mutação de lkb1 como um biomarcador preditivo para sensibilidade para inibidores de tor quinase.
WO2011107585A1 (en) 2010-03-04 2011-09-09 Cellzome Limited Morpholino substituted urea derivatives as mtor inhibitors
US8912178B2 (en) * 2010-05-19 2014-12-16 Xcovery Holdings Company, LLC mTOR selective kinase inhibitors
JP5832527B2 (ja) 2010-05-20 2015-12-16 アレイ バイオファーマ、インコーポレイテッド Ｔｒｋキナーゼ阻害剤としてのマクロ環化合物
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
WO2012099581A1 (en) 2011-01-19 2012-07-26 Takeda Pharmaceutical Company Limited Dihydrofuropyrimidine compounds
EP2678016B1 (en) 2011-02-23 2016-08-10 Intellikine, LLC Heterocyclic compounds and uses thereof
CN103491962B (zh) 2011-02-23 2016-10-12 因特利凯有限责任公司 激酶抑制剂的组合及其用途
PT2688887E (pt) 2011-03-23 2015-07-06 Amgen Inc Inibidores duais tricíclicos fusionados de cdk 4/6 e flt3
ES2608967T3 (es) 2011-03-28 2017-04-17 Mei Pharma, Inc. (Aralquilamino sustituido en alfa y heteroarilalquilamino)pirimidinil y 1,3,5-triazinil benzimidazoles, composiciones farmacéuticas que los contienen, y estos compuestos para usar en el tratamiento de enfermedades proliferativas
US20140163023A1 (en) 2011-04-04 2014-06-12 Cellzome Limited Dihydropyrrolo pyrimidine derivatives as mtor inhibitors
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
KR20140070616A (ko) 2011-09-21 2014-06-10 셀좀 리미티드 Mtor 저해제로서의 모르폴리노 치환된 우레아 또는 카바메이트 유도체
CA2850852A1 (en) 2011-10-07 2013-04-11 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
EP2852661A1 (en) 2012-05-23 2015-04-01 F. Hoffmann-La Roche AG Compositions and methods of obtaining and using endoderm and hepatocyte cells
WO2013182546A1 (en) * 2012-06-07 2013-12-12 F. Hoffmann-La Roche Ag Pyrazolopyrimidone and pyrazolopyridone inhibitors of tankyrase
DK3176170T3 (en) 2012-06-13 2019-01-28 Incyte Holdings Corp SUBSTITUTED TRICYCLIC RELATIONS AS FGFR INHIBITORS
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines 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
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
EP3640249A1 (en) 2013-03-15 2020-04-22 Dow AgroSciences LLC 4-amino-6-(heterocyclic)picolinates and 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their use as herbicides
EP2970186B1 (en) * 2013-03-15 2020-06-10 Dow AgroSciences LLC 4-amino-6-(heterocyclic)picolinates and 6-amino-2-(heterocyclic) pyrimidine-4-carboxylates and their use as herbicides
JP6382947B2 (ja) 2013-04-17 2018-08-29 シグナル ファーマシューティカルズ，エルエルシー 前立腺癌を治療するためのジヒドロピラジノ−ピラジン化合物及びアンドロゲン受容体アンタゴニストを含む組合せ療法
PE20160041A1 (es) 2013-04-17 2016-01-28 Signal Pharm Llc FORMULACIONES FARMACEUTICAS, PROCESO, FORMAS SOLIDAS Y METODOS DE USO RELACIONADOS CON 1-ETIL-7-(2-METIL-6-(1H-1,2,4-TRIAZOL-3-IL)PIRIDIN-3-IL)-3,4-DIHIDROPIRAZINO[2,3-b]PIRAZIN-2(1H)-ONA
AU2014254052B2 (en) 2013-04-17 2019-06-06 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
KR102242505B1 (ko) 2013-04-17 2021-04-20 시그날 파마소티칼 엘엘씨 암 치료용 tor 키나제 억제제 및 시티딘 유사체를 포함하는 병용 요법
CA2909579A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and n-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer
TWI656875B (zh) 2013-04-17 2019-04-21 美商標誌製藥公司 藉二氫吡并吡治療癌症
WO2014172436A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer
CA3130452C (en) 2013-04-19 2023-10-31 Incyte Holdings Corporation Bicyclic heterocycles as fgfr inhibitors
NZ629486A (en) 2013-05-29 2017-11-24 Signal Pharm Llc Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use
SG11201607586UA (en) * 2014-03-13 2016-10-28 Agency Science Tech & Res Fused pyrimidine-based hydroxamate derivatives
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
US9512129B2 (en) 2014-04-16 2016-12-06 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
EP3143021B1 (en) 2014-05-14 2019-06-12 Pfizer Inc Pyrazolopyridines and pyrazolopyrimidines
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
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）
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
WO2016044276A1 (en) 2014-09-15 2016-03-24 Dow Agrosciences Llc Synergistic weed control from applications of pyridine carboxylic acid herbicides and photosystem ii inhibitors
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
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
AU2015346046B2 (en) 2014-11-16 2020-06-25 Array Biopharma, Inc. Crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate
SG11201703826TA (en) * 2014-12-17 2017-07-28 Pfizer Formulations of a pi3k/mtor-inhibitor for intravenous administration
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
MX373169B (es) 2015-02-20 2020-04-24 Incyte Holdings Corp Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr).
CA3003153A1 (en) 2015-10-26 2017-05-04 Loxo Oncology, Inc. Point mutations in trk inhibitor-resistant cancer and methods relating to the same
WO2017176751A1 (en) 2016-04-04 2017-10-12 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
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
LT3800189T (lt) 2016-05-18 2023-10-10 Loxo Oncology, Inc. (s)-n-(5-((r)-2-(2,5-difluorfenil)pirolidin-1-il)pirazolo[1,5-a]pirimidin-3- il)-3-hidroksipirolidin-1-karboksamido gavimas
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
IL303660A (en) 2017-05-02 2023-08-01 Revolution Medicines Inc Rapamycin analogs as mtor inhibitors
CA3063976A1 (en) 2017-05-23 2018-11-29 Mei Pharma, Inc. Combination therapy
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
SG11201912403SA (en) 2017-06-22 2020-01-30 Celgene Corp Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection
US20200283444A1 (en) * 2017-08-02 2020-09-10 Northwestern University Substituted fused pyrimidine compounds and uses thereof
RU2020109775A (ru) 2017-08-14 2021-09-16 Мей Фарма, Инк. Комплексная терапия
SG11202010560QA (en) 2018-05-01 2020-11-27 Revolution Medicines Inc C26-linked rapamycin analogs as mtor inhibitors
PE20212112A1 (es) 2018-05-01 2021-11-04 Revolution Medicines Inc Analogos de rapamicina ligados a c40, c28 y c-32 como inhibidores de mtor
CN112867716B (zh) 2018-05-04 2024-09-13 因赛特公司 Fgfr抑制剂的固体形式和其制备方法
AU2019262579B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Salts of an FGFR inhibitor
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
US12054488B2 (en) * 2018-09-27 2024-08-06 Suzhou Raymon Pharmaceuticals Company, Ltd. Pyrazolopyrimidine compound and preparation method therefor and use thereof in preparation of anti-cancer drug
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
EP3980010A4 (en) * 2019-06-04 2023-06-07 Arcus Biosciences, Inc. 2,3,5-TRISUBSTITUTED PYRAZOLO[1,5-A]PYRIMIDINE COMPOUNDS
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
EP3800188A1 (en) * 2019-10-02 2021-04-07 Bayer AG Substituted pyrazolopyrimidines as irak4 inhibitors
PH12022550892A1 (en) 2019-10-14 2023-05-03 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CA3162010A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Derivatives of an fgfr inhibitor
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
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
JP2024506381A (ja) 2021-02-16 2024-02-13 ヴァクシテック ノース アメリカ， インコーポレイテッド 両親媒性ペプチドに基づく自己集合ナノ粒子
JP2024513575A (ja) 2021-04-12 2024-03-26 インサイト・コーポレイション Ｆｇｆｒ阻害剤及びネクチン－４標的化剤を含む併用療法
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
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
EP4531859A1 (en) 2022-05-25 2025-04-09 Revolution Medicines, Inc. Methods of treating cancer with an mtor inhibitor
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
US20240269269A1 (en) 2022-10-25 2024-08-15 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
CA2599320A1 (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
KR20130087054A (ko) * 2006-04-04 2013-08-05 더 리젠트스 오브 더 유니이버시티 오브 캘리포니아 키나제 길항물질

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