BR0309475A - Derivados de pirazolo-[1,5-a]-pirimidina e inibidores de nad(p)h oxidase que contêm os mesmos - Google Patents

Derivados de pirazolo-[1,5-a]-pirimidina e inibidores de nad(p)h oxidase que contêm os mesmos

Info

Publication number
BR0309475A
BR0309475A BR0309475-8A BR0309475A BR0309475A BR 0309475 A BR0309475 A BR 0309475A BR 0309475 A BR0309475 A BR 0309475A BR 0309475 A BR0309475 A BR 0309475A
Authority
BR
Brazil
Prior art keywords
nad
pyrimidine derivatives
oxidase inhibitors
pyrazolo
inhibitors containing
Prior art date
Application number
BR0309475-8A
Other languages
English (en)
Inventor
Kaoru Seno
Koich Nishi
Toshio Fujishita
Yoshiyuki Matsuo
Original Assignee
Shionogi & Co
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 Shionogi & Co filed Critical Shionogi & Co
Publication of BR0309475A publication Critical patent/BR0309475A/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

"DERIVADOS DE PIRAZOLO-[1,5-a]-PIRIMIDINA E INIBIDORES DE NAD (P) H OXIDASE QUE CONTêM OS MESMOS". Descreve-se um composto representado pela fórmula (Ia) (onde R~ 1a~, R~ 2a~, e R~ 3~ a R~ 5~ são iguais aos definidos no relatório descritivo), um seu pró-medicamento, um seu sal farmaceuticamente aceitável, ou um seu solvato. Os compostos são úteis na prevenção ou tratamento de doenças relacionadas a NAD (P) H.
BR0309475-8A 2002-04-23 2003-04-18 Derivados de pirazolo-[1,5-a]-pirimidina e inibidores de nad(p)h oxidase que contêm os mesmos BR0309475A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2002121519 2002-04-23
PCT/JP2003/005024 WO2003091256A1 (en) 2002-04-23 2003-04-18 PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVE AND NAD(P)H OXIDASE INHIBITOR CONTAINING THE SAME

Publications (1)

Publication Number Publication Date
BR0309475A true BR0309475A (pt) 2005-03-01

Family

ID=29267410

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0309475-8A BR0309475A (pt) 2002-04-23 2003-04-18 Derivados de pirazolo-[1,5-a]-pirimidina e inibidores de nad(p)h oxidase que contêm os mesmos

Country Status (11)

Country Link
US (1) US7662826B2 (pt)
EP (1) EP1505068A4 (pt)
JP (1) JP4500055B2 (pt)
KR (1) KR20040097375A (pt)
CN (1) CN100343255C (pt)
AU (1) AU2003227437A1 (pt)
BR (1) BR0309475A (pt)
CA (1) CA2483306A1 (pt)
MX (1) MXPA04010441A (pt)
TW (1) TW200404804A (pt)
WO (1) WO2003091256A1 (pt)

Families Citing this family (137)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8580782B2 (en) 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
CA2497539A1 (en) 2002-09-04 2004-03-18 Schering Corporation Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors
US7119200B2 (en) * 2002-09-04 2006-10-10 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
DE60313872T2 (de) 2002-09-04 2008-01-17 Schering Corp. Pyrazoloä1,5-aüpyrimidine als hemmstoffe cyclin-abhängiger kinasen
ES2285164T3 (es) 2002-09-04 2007-11-16 Schering Corporation Pirazolopirimidinas como inhibidores de quinasas dependientes de ciclina.
US7196078B2 (en) 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
MY141978A (en) 2002-09-04 2010-08-16 Schering Corp Pyrazolopyrimidines as cyclin dependent kinase inhibitors
US8673924B2 (en) 2002-09-04 2014-03-18 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
US7161003B1 (en) 2002-09-04 2007-01-09 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
US7223788B2 (en) 2003-02-14 2007-05-29 Sanofi-Aventis Deutschland Gmbh Substituted N-aryl heterocycles, process for their preparation and their use as medicaments
DE10306250A1 (de) * 2003-02-14 2004-09-09 Aventis Pharma Deutschland Gmbh Substituierte N-Arylheterozyklen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US7557110B2 (en) 2003-02-28 2009-07-07 Teijin Pharma Limited Pyrazolo[1,5-A] pyrimidine derivatives
US20070179161A1 (en) * 2003-03-31 2007-08-02 Vernalis (Cambridge) Limited. Pyrazolopyrimidine compounds and their use in medicine
US20070043079A1 (en) * 2003-04-18 2007-02-22 Hiromu Habashita Heterocyclic compound containing nitrogen atom and use thereof
WO2004110454A1 (ja) * 2003-06-13 2004-12-23 Ishihara Sangyo Kaisha, Ltd. アデノシンＡ2ａ受容体アゴニストの投与が必要な疾患を治療又は予防するための組成物
WO2005049593A2 (en) * 2003-11-13 2005-06-02 Abbott Laboratories N-acylsulfonamide apoptosis promoters
US20070155738A1 (en) 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
JP5052518B2 (ja) 2005-10-06 2012-10-17 シェーリング コーポレイション プロテインキナーゼインヒビターとしてのピラゾロピリミジン
EP1873157A1 (en) * 2006-06-21 2008-01-02 Bayer Schering Pharma Aktiengesellschaft Pyrazolopyrimidines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
MX2009001036A (es) 2006-08-04 2009-04-23 Merz Pharma Gmbh & Co Kgaa Pirazolopirimidinas, proceso para su preparacion y su uso como medicina.
WO2008037477A1 (en) * 2006-09-29 2008-04-03 Novartis Ag Pyrazolopyrimidines as p13k lipid kinase inhibitors
CA2670083A1 (en) * 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic metalloprotease inhibitors
HRP20150642T1 (hr) * 2006-12-22 2015-08-14 Astex Therapeutics Limited BICIKLIÄŚKE HETEROCIKLIÄŚKE TVARI KAO INHIBITORI FGFR-a
US8513276B2 (en) 2006-12-22 2013-08-20 Astex Therapeutics Limited Imidazo[1,2-a]pyridine compounds for use in treating cancer
EP2002835A1 (en) * 2007-06-04 2008-12-17 GenKyo Tex Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
EP2000176A1 (en) * 2007-06-04 2008-12-10 GenKyo Tex Tetrahydroindole derivatives as NADPH Oxidase inhibitors
AR067326A1 (es) * 2007-05-11 2009-10-07 Novartis Ag Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido
KR20100087298A (ko) * 2007-09-28 2010-08-04 교와 핫꼬 기린 가부시키가이샤 피부 질환의 예방 및/또는 치료제
GB0720038D0 (en) 2007-10-12 2007-11-21 Astex Therapeutics Ltd New compounds
GB0720041D0 (en) 2007-10-12 2007-11-21 Astex Therapeutics Ltd New Compounds
EP2085398A1 (en) 2008-02-01 2009-08-05 Merz Pharma GmbH & Co. KGaA Pyrazolopyrimidines, a process for their preparation and their use as medicine
GB0810902D0 (en) 2008-06-13 2008-07-23 Astex Therapeutics Ltd New compounds
CN102131389A (zh) * 2008-06-20 2011-07-20 健泰科生物技术公司 三唑并吡啶jak抑制剂化合物和方法
WO2009155565A1 (en) * 2008-06-20 2009-12-23 Genentech, Inc. Triazolopyridine jak inhibitor compounds and methods
EP2166008A1 (en) * 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
EP2165707A1 (en) * 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
EP2166009A1 (en) 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as nadph oxidase inhibitors
EP2166010A1 (en) 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
MY169791A (en) * 2008-10-22 2019-05-15 Array Biopharma Inc Substituted pyrazolo [1,5-a] pyrimidine compounds as trk kinase inhibitors
EP2348860B1 (en) 2008-10-31 2015-05-27 Genentech, Inc. Pyrazolopyrimidine jak inhibitor compounds and methods
WO2010056631A1 (en) * 2008-11-12 2010-05-20 Schering Corporation Inhibitors of fatty acid binding protein (fabp)
US8591943B2 (en) 2009-04-09 2013-11-26 Merck Sharp & Dohme Corp. Pyrazolo[1,5-a]pyrimidine derivatives as mTOR inhibitors
GB0906472D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
GB0906470D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
WO2010126811A1 (en) 2009-04-27 2010-11-04 Boehringer Ingelheim International Gmbh Cxcr3 receptor antagonists
GB0908394D0 (en) 2009-05-15 2009-06-24 Univ Leuven Kath Novel viral replication inhibitors
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
US20110030037A1 (en) * 2009-07-07 2011-02-03 Vadim Olshansky Zone migration in network access
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
GB0913636D0 (en) 2009-08-05 2009-09-16 Univ Leuven Kath Novel viral replication inhibitors
EP2305679A1 (en) 2009-09-28 2011-04-06 GenKyoTex SA Pyrazoline dione derivatives as nadph oxidase inhibitors
US8759357B2 (en) 2009-10-08 2014-06-24 Merck Sharp & Dohme Corp. Inhibitors of fatty acid binding protein (FABP)
ES2555393T3 (es) 2009-12-18 2015-12-30 Glaxosmithkline Intellectual Property Limited Nuevos compuestos
US9452980B2 (en) * 2009-12-22 2016-09-27 Hoffmann-La Roche Inc. Substituted benzamides
WO2011084985A1 (en) * 2010-01-07 2011-07-14 Boehringer Ingelheim International Gmbh Cxcr3 receptor antagonists
MY183861A (en) 2010-03-05 2021-03-17 Kyowa Hakko Kirin Co Ltd Pyrazolopyrimidine derivative
BR112012028153A2 (pt) 2010-05-03 2018-08-07 Tsh Biopharm Corporation Ltd composição farmacêutica e método para o tratamento de hipertensão
ME03376B (me) 2010-05-20 2020-01-20 Array Biopharma Inc Makrociklička jedinjenja kао inhibiтori trk kinaze
KR20140003438A (ko) 2010-11-15 2014-01-09 카톨리에케 유니버시테이트 루벤 항바이러스성 축합 헤테로사이클릭 화합물
US8748435B2 (en) 2011-04-01 2014-06-10 Novartis Ag Pyrazolo pyrimidine derivatives
WO2012139876A1 (en) 2011-04-14 2012-10-18 Merz Pharma Gmbh & Co. Kgaa Enteric formulations of metabotropic glutamate receptor modulators
US10953012B2 (en) 2011-04-26 2021-03-23 Bioenergenix Llc Heterocyclic compounds for the inhibition of pask
TW201311693A (zh) 2011-09-02 2013-03-16 Kyowa Hakko Kirin Co Ltd 化學激活激素受體活性調節劑
JP2014530870A (ja) * 2011-10-20 2014-11-20 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ サーチュイン調節因子としての置換された二環式アザ複素環およびアナログ
JP6073343B2 (ja) 2011-10-20 2017-02-01 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ サーチュイン調節因子としての置換された二環式アザ複素環およびアナログ
WO2013087808A1 (en) 2011-12-15 2013-06-20 Merz Pharma Gmbh & Co. Kgaa Pharmaceutical composition comprising a pyrazolopyrimidme and cyclodextrin
WO2013087815A1 (en) 2011-12-15 2013-06-20 Merz Pharma Gmbh & Co. Kgaa Liquid pharmaceutical composition containing a pyrazolopyrimidine derivative and pharmaceutical uses thereof
RU2478640C1 (ru) * 2012-02-07 2013-04-10 Федеральное государственное бюджетное образовательное учреждение высшего профессионального образования "Пермский государственный национальный исследовательский университет" N-АРИЛ-2,3-ДИАРОИЛ-8,10-ДИМЕТИЛПИРИДО[2',3':3,4]ПИРАЗОЛО[1,5-α]ПИРИМИДИН-4-КАРБОКСАМИДЫ И СПОСОБ ИХ ПОЛУЧЕНИЯ
WO2014066743A1 (en) 2012-10-25 2014-05-01 Bioenergenix Heterocyclic compounds for the inhibition of pask
US10392389B2 (en) 2012-10-25 2019-08-27 Bioenergenix Llc Heterocyclic compounds for the inhibition of PASK
CA2889919C (en) 2012-11-16 2021-08-17 University Health Network Pyrazolopyrimidine compounds
LT2925757T (lt) 2012-11-19 2017-12-27 Novartis Ag Junginiai ir kompozicijos, skirti parazitinių ligų gydymui
US8871754B2 (en) 2012-11-19 2014-10-28 Irm Llc Compounds and compositions for the treatment of parasitic diseases
EP2922853A4 (en) 2012-11-20 2016-11-23 Discoverybiomed Inc SMALL MOLECULE BICYCLIC AND TRICYCLIC CFTR CORRECTING DEVICES
AU2013348018A1 (en) 2012-11-20 2015-06-04 Discoverybiomed, Inc. Small molecule CFTR correctors
SI2941432T1 (en) 2012-12-07 2018-07-31 Vertex Pharmaceuticals Incorporated 2-AMINO-6-FLUORO-N- (5-FLUORO-4- (4- (4- (OXETHAN-3-YL) PIPERAZIN-1-CARBONYL) PIPERIDIN-1-YLIPRIDIN-3-YL) 1,5 ALFA) PYRIMIDINE-3-CARBOXAMIDE AS ATR KINAZE INHIBITOR
ES2753386T3 (es) 2013-03-13 2020-04-08 Forma Therapeutics Inc Derivados de 2-hidroxi-1-{4-[(4-fenil)fenil]carbonil}piperazin-1-il}etano-1-ona y compuestos relacionados como inhibidores de sintasa de ácido graso (FASN) para el tratamiento del cáncer
EP2970288A1 (en) * 2013-03-15 2016-01-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2014143240A1 (en) * 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
US8957078B2 (en) * 2013-03-15 2015-02-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
TW201542550A (zh) * 2013-09-06 2015-11-16 Lexicon Pharmaceuticals Inc 吡唑并［１，５－ａ］嘧啶基化合物、包含彼之組合物以及使用彼之方法
PL407081A1 (pl) 2014-02-05 2015-08-17 Celon Pharma Spółka Akcyjna Pochodne pirazolo[1,5-a]pirymidyny jako inhibitory kinazy JAK-2
US10342795B2 (en) 2014-03-27 2019-07-09 Janssen Pharmaceutica Nv Substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrimidine derivatives and 2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives as ROS1 inhibitors
ES2715676T3 (es) 2014-03-27 2019-06-05 Janssen Pharmaceutica Nv Derivados de 4,5,6,7-tetrahidro-pirazolo[1,5-a]pirazina sustituidos y derivados de 5,6,7,8-tetrahidro-4h-pirazolo[1,5-a][1,4]diazepina como inhibidores de ros1
WO2015152319A1 (ja) * 2014-04-02 2015-10-08 株式会社 三和化学研究所 ５，７－無置換－ピラゾロ［１，５－ａ］ピリミジン－６－カルボン酸の製造方法
JP2017516850A (ja) 2014-05-23 2017-06-22 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｊａｋ阻害剤である５−クロロ−２−ジフルオロメトキシフェニルピラゾロピリミジン化合物
SG11201607895PA (en) * 2014-05-28 2016-12-29 Novartis Ag Novel pyrazolo pyrimidine derivatives and their use as malt1 inhibitors
CN113354649B (zh) 2014-11-16 2024-12-10 阵列生物制药公司 一种新的晶型
EP3034500A1 (en) * 2014-12-17 2016-06-22 Genkyotex Sa Amido thiazole derivatives as NADPH oxidase inhibitors
JO3637B1 (ar) 2015-04-28 2020-08-27 Janssen Sciences Ireland Uc مركبات بيرازولو- وترايازولو- بيريميدين مضادة للفيروسات rsv
AU2016331955B2 (en) 2015-09-30 2022-07-21 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors
WO2017070089A1 (en) 2015-10-19 2017-04-27 Incyte Corporation Heterocyclic compounds as immunomodulators
EP3368039A1 (en) 2015-10-26 2018-09-05 The Regents of The University of Colorado, A Body Corporate Point mutations in trk inhibitor-resistant cancer and methods relating to the same
AU2016352813B2 (en) * 2015-11-13 2019-09-19 Novartis Ag Novel pyrazolo pyrimidine derivatives
SG10202004618TA (en) 2015-11-19 2020-06-29 Incyte Corp Heterocyclic compounds as immunomodulators
MA44075A (fr) * 2015-12-17 2021-05-19 Incyte Corp Dérivés de n-phényl-pyridine-2-carboxamide et leur utilisation en tant que modulateurs des interactions protéine/protéine pd-1/pd-l1
AU2016379372A1 (en) 2015-12-22 2018-08-02 Incyte Corporation Heterocyclic compounds as immunomodulators
CN108713019B (zh) 2016-03-17 2021-06-15 豪夫迈·罗氏有限公司 具有作为taar的激动剂的活性的5-乙基-4-甲基-吡唑-3-甲酰胺衍生物
FI3439662T3 (fi) 2016-04-04 2024-09-04 Loxo Oncology Inc (s)-n-(5-((r)-2-(2,5-difluorifenyyli)pyrrolidin-1-yyli)pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidin nesteformulaatioita
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
AU2017251155B2 (en) 2016-04-15 2021-08-05 Elanco Animal Health Gmbh Pyrazolopyrimidine derivatives
AR108396A1 (es) 2016-05-06 2018-08-15 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
EP3458456B1 (en) 2016-05-18 2020-11-25 Loxo Oncology Inc. Preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
WO2017205464A1 (en) 2016-05-26 2017-11-30 Incyte Corporation Heterocyclic compounds as immunomodulators
HUE060256T2 (hu) 2016-06-20 2023-02-28 Incyte Corp Heterociklusos vegyületek mint immunmodulátorok
EP3484866B1 (en) 2016-07-14 2022-09-07 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2018044783A1 (en) 2016-08-29 2018-03-08 Incyte Corporation Heterocyclic compounds as immunomodulators
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
WO2018119221A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Pyridine derivatives as immunomodulators
US20180179202A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
JP7101678B2 (ja) 2016-12-22 2022-07-15 インサイト・コーポレイション 免疫調節剤としての複素環式化合物
LT3558990T (lt) 2016-12-22 2022-12-27 Incyte Corporation Tetrahidroimidazo[4,5-c]piridino dariniai kaip pd-l1 internalizavimo induktoriai
ES2874756T3 (es) 2016-12-22 2021-11-05 Incyte Corp Derivados de triazolo[1,5-A]piridina como inmunomoduladores
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
CN106866680B (zh) * 2017-03-31 2019-02-01 陕西理工大学 一种3-芳基-6-甲酰胺吡唑并[1,5-a]嘧啶类化合物及其应用
KR102596307B1 (ko) 2017-04-27 2023-10-30 바이엘 애니멀 헬스 게엠베하 새로운 비시클릭 피라졸 유도체
MX387969B (es) 2017-05-22 2025-03-19 Hoffmann La Roche Composiciones y compuestos terapéuticos, y métodos para su uso.
EP3664806B1 (en) * 2017-08-09 2025-04-30 Sanford Burnham Prebys Medical Discovery Institute 3-PHENYL-PYRAZOLO[1,5-A]PYRIMIDINE-5-CARBOXILIC ACID DERIVATIVES AS APELIN (APJ) RECEPTOR AGONISTS FOR THE TREATMENT OF CARDIOVASCULAR, METABOLIC, CNS, OR INFECTIOUS DISEASES OR DISORDERS
EP3479843A1 (en) 2017-11-01 2019-05-08 GenKyoTex Suisse SA Use of nox inhibitors for treatment of cancer
TW201932470A (zh) 2017-11-29 2019-08-16 愛爾蘭商健生科學愛爾蘭無限公司 具有抗ｒｓｖ活性之吡唑并嘧啶
SG11202006141RA (en) 2018-01-31 2020-07-29 Janssen Sciences Ireland Unlimited Co Cycloalkyl substituted pyrazolopyrimidines having activity against rsv
SMT202500157T1 (it) 2018-03-30 2025-05-12 Incyte Corp Composti eterociclici come immunomodulatori
US11708369B2 (en) 2018-04-23 2023-07-25 Janssen Sciences Ireland Unlimited Company Heteroaromatic compounds having activity against RSV
HUE061503T2 (hu) 2018-05-11 2023-07-28 Incyte Corp Tetrahidro-imidazo[4,5-C]piridin-származékok mint PD-L1 immunmodulátorok
US10793554B2 (en) 2018-10-29 2020-10-06 Forma Therapeutics, Inc. Solid forms of 4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone
US11155560B2 (en) 2018-10-30 2021-10-26 Kronos Bio, Inc. Substituted pyrazolo[1,5-a]pyrimidines for modulating CDK9 activity
JP7665593B2 (ja) 2019-08-09 2025-04-21 インサイト・コーポレイション Ｐｄ－１／ｐｄ－ｌ１阻害剤の塩
PE20221038A1 (es) 2019-09-30 2022-06-17 Incyte Corp Compuestos de pirido[3,2-d] pirimidina como inmunomoduladores
US12116420B1 (en) 2019-10-16 2024-10-15 United States of America as represented by the Administrator of NASA and the Secretary of the Interior Functionalizing biological substrates with bioengineered peptides to bind targeted molecules
CA3160131A1 (en) 2019-11-11 2021-05-20 Incyte Corporation Salts and crystalline forms of a pd-1/pd-l1 inhibitor
EP4146654A1 (en) * 2020-05-07 2023-03-15 Adorx therapeutics Limited Antagonists of the adenosine a2a receptor
TW202233615A (zh) 2020-11-06 2022-09-01 美商英塞特公司 Ｐｄ—１／ｐｄ—ｌ１抑制劑之結晶形式
CR20230230A (es) 2020-11-06 2023-07-27 Incyte Corp Proceso para hacer un inhibidor de pd-1/pdl1 y sales y formas cristalinas del mismo
WO2022099018A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process of preparing a pd-1/pd-l1 inhibitor
CN112876482B (zh) * 2020-12-31 2023-07-28 中国药科大学 一类多取代杂环衍生物、其制备方法及其在医药上的应用
EP4447971A4 (en) * 2021-12-17 2025-12-10 Merck Sharp & Dohme Llc PYRAZOLOPYRIMIDINE DERIVATIVES AND THEIR METHODS OF USE FOR THE TREATMENT OF HERPESVIRUS
AU2023228096A1 (en) * 2022-03-02 2024-10-17 Hangzhou Bio-Sincerity Pharma-Tech Co., Ltd. Histamine h3 receptor antagonist and medical use thereof

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1568962A (en) * 1975-10-31 1980-06-11 Beecham Group Ltd Reparation and compositions containing them (heterocyclic-carbonylamino)pencillins methods for their p
GB1579362A (en) * 1977-03-16 1980-11-19 Beecham Group Ltd 6-(a-heterocyclylcarbonyl amino-acetamido)-penicillins and compositions containing them
US4155817A (en) * 1978-08-11 1979-05-22 American Chemical And Refining Company, Inc. Low free cyanide high purity silver electroplating bath and method
US4918074A (en) * 1984-03-12 1990-04-17 Yoshitomi Pharmaceutical Industries, Ltd. Polyazaheterocycle compounds
CA1330079C (en) * 1988-10-13 1994-06-07 Michihiko Tsujitani Pyrrolo (3,2-e)pyrazolo(1,5-a)pyrimidine derivative and medicine comprising the same
WO1992006096A1 (fr) * 1990-10-09 1992-04-16 Otsuka Pharmaceutical Co., Ltd. Derive de pyrimidine, production de ce derive et inhibiteur d'androgenes
KR0133372B1 (ko) * 1991-09-06 1998-04-23 고야 다다시 4-아미노(알킬)시클로헥산-1-카르복사미드 화합물 및 그 용도
JPH069638A (ja) 1992-06-19 1994-01-18 Ube Ind Ltd ピラゾロピリミジン誘導体
JPH07242670A (ja) 1994-03-08 1995-09-19 Pola Chem Ind Inc ピロロ［３，２−ｅ］ピラゾロ［１，５−ａ］ピリミジン誘導体及びこれを含有する循環器系疾患治療剤
JPH07267960A (ja) 1994-03-28 1995-10-17 Lederle Japan Ltd ピロロ［３，２−ｅピラゾロ［１，５−ａピリミジン誘導体及びこれを含有する循環器系疾患治療剤
BR9606546A (pt) * 1995-08-02 1998-07-14 Uriach & Cia Sa J Novas carboxamidas com atividade fungicida
JP3898296B2 (ja) * 1996-08-28 2007-03-28 ポーラ化成工業株式会社 ピロロピラゾロピリミジン化合物及びこれを有効成分とする医薬
US6548524B2 (en) * 1996-10-16 2003-04-15 American Cyanamid Company Preparation and use of ortho-sulfonamido bicyclic heteroaryl hydroxamic acids as matrix metalloproteinase and TACE inhibitors
US6228869B1 (en) * 1996-10-16 2001-05-08 American Cyanamid Company Ortho-sulfonamido bicyclic hydroxamic acids as matrix metalloproteinase and TACE inhibitors
CN1276785A (zh) * 1997-08-22 2000-12-13 霍夫曼-拉罗奇有限公司 N－烷酰基苯丙氨酸衍生物
US6229011B1 (en) * 1997-08-22 2001-05-08 Hoffman-La Roche Inc. N-aroylphenylalanine derivative VCAM-1 inhibitors
PT1021413E (pt) 1997-10-06 2003-10-31 Wyeth Corp A preparacao e utilizacao de acidos orto-sulfonamido heterociclicos biciclicos hidroxamicos como inibidores de metaloproteinases de matriz e de tace
DZ2796A1 (fr) 1998-05-21 2003-12-01 Smithkline Beecham Corp Composés à fonction bis-aminométhyl-carbonyle nouveaux, procédé pour leur préparation et compositions pharmaceutiques les contenant.
JP2001302666A (ja) 1999-09-21 2001-10-31 Nissan Chem Ind Ltd アゾール縮合ヘテロ環アニライド化合物及び除草剤
OA12274A (en) * 2000-05-22 2006-05-09 Aventis Pharma Inc Arylmethylamine derivatives for use as tryptase inhibitors.
BR0114059A (pt) 2000-09-21 2003-07-01 Pfizer Prod Inc Derivados de resorcinol
FR2815030A1 (fr) * 2000-10-05 2002-04-12 Lipha Derives nitroso de la diphenylamine, compositions pharmaceutiques les contenant et leur utilisation pour la preparation de medicaments

Also Published As

Publication number Publication date
CN1662537A (zh) 2005-08-31
AU2003227437A1 (en) 2003-11-10
JPWO2003091256A1 (ja) 2005-09-02
CA2483306A1 (en) 2003-11-06
TW200404804A (en) 2004-04-01
CN100343255C (zh) 2007-10-17
MXPA04010441A (es) 2005-02-14
US7662826B2 (en) 2010-02-16
EP1505068A1 (en) 2005-02-09
JP4500055B2 (ja) 2010-07-14
EP1505068A4 (en) 2008-03-19
US20060089362A1 (en) 2006-04-27
WO2003091256A1 (en) 2003-11-06
KR20040097375A (ko) 2004-11-17

Similar Documents

Publication Publication Date Title
BR0309475A (pt) Derivados de pirazolo-[1,5-a]-pirimidina e inibidores de nad(p)h oxidase que contêm os mesmos
WO2005037836A3 (en) Imidazo ‘1, 5 - a ! pyrazine tyrosine kinase inhibitors
AP1911A (en) Pyrrolo[2,3-d]pyrimidine compounds.
WO2004056827A3 (en) Substituted pyrrolo-pyrazole derivatives as kinase inhibitors
DK1272477T3 (da) Pyrimidinforbindelser
BR0316001A (pt) Derivados de pirimido[4,5-d]pirimidina com atividade anticâncer
EA200500721A1 (ru) Пиримидины, ингибирующие chk, pdk и акт, их получение и применение в качестве лекарственных средств
WO2005060972A3 (en) Pyrrolo [2,3-d] pyrimidine compounds for treating transplant rejection
CA2309551A1 (en) Aminothiazole inhibitors of cyclin dependent kinases
WO2001005762A3 (de) Biphenylderivate, ihre herstellung und ihre verwendung als mtp-inhibitor
AU2003284632A1 (en) Isoquinoline compounds and medicinal use thereof
MA29857B1 (fr) Derives de triazolopyridine en tant qu'inhibiteurs de lipases et phospholipases
NO20014363L (no) 4-okso-4,7-dihydro-tieno[2,3-b]pyridin-5-karboksamider som antivirale midler
WO2005040170A8 (en) Pyrrolobenzodiazepine derivatives, compositions comprising the same and methods related thereto
BR9916781A (pt) 4-oxo-1,4-dihidro-3-quinolinacarboxamidas comoagentes antivirais
MXPA05007516A (es) Derivados de hexahidropirazino[1,2-a]pirimidina -4, 7-diona sustituidos, metodo para producirlos y su uso como medicamentos.
PT1078923E (pt) Processo para a preparacao de derivados de benzotiofeno
BRPI0414948A (pt) derivados de pirazolo-e-imidazo pirimidina
NO307463B1 (no) Galantaminderivater, en fremgangsmõte for fremstilling samt deres anvendelse som medikamenter
BRPI0416690A (pt) derivados de pirrol
WO2004014868A3 (en) Pyrimidine-2,4-dione derivatives as matrix metalloproteinase inhibitors
WO2006116733A3 (en) Protein kinase inhibitors
EP1477490A4 (en) PYRROLOPYRIMIDINE DERIVATIVE
WO2003068776A1 (en) [1,2,4]TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVES
BR0305041A (pt) Compostos orgânicos

Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 7A E 8A ANUIDADE(S).

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2116 DE 26/07/2011.