ES2354824T3 - Pirazolo[1,5-a]pirimidinas útiles como inhibidores de proteínas cinasas. - Google Patents

Pirazolo[1,5-a]pirimidinas útiles como inhibidores de proteínas cinasas. Download PDF

Info

Publication number
ES2354824T3
ES2354824T3 ES05816516T ES05816516T ES2354824T3 ES 2354824 T3 ES2354824 T3 ES 2354824T3 ES 05816516 T ES05816516 T ES 05816516T ES 05816516 T ES05816516 T ES 05816516T ES 2354824 T3 ES2354824 T3 ES 2354824T3
Authority
ES
Spain
Prior art keywords
alkyl
aliphatic
aryl
heterocyclyl
optionally
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES05816516T
Other languages
English (en)
Spanish (es)
Inventor
Dean Stamos
Juan-Miguel Jimenez
Alex Aronov
Ronald Knegtel
Jon R. Come
Jean-Damien Charrier
Pan Li
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals 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 Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Application granted granted Critical
Publication of ES2354824T3 publication Critical patent/ES2354824T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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
    • 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
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/08—Antiseborrheics
    • 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
    • A61P17/10—Anti-acne agents
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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
    • A61P37/04—Immunostimulants
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • 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
    • 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
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Biochemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
ES05816516T 2004-11-04 2005-11-04 Pirazolo[1,5-a]pirimidinas útiles como inhibidores de proteínas cinasas. Expired - Lifetime ES2354824T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US62544604P 2004-11-04 2004-11-04
US625446P 2004-11-04

Publications (1)

Publication Number Publication Date
ES2354824T3 true ES2354824T3 (es) 2011-03-18

Family

ID=35809833

Family Applications (1)

Application Number Title Priority Date Filing Date
ES05816516T Expired - Lifetime ES2354824T3 (es) 2004-11-04 2005-11-04 Pirazolo[1,5-a]pirimidinas útiles como inhibidores de proteínas cinasas.

Country Status (20)

Country Link
US (1) US7528138B2 (https=)
EP (1) EP1812440B1 (https=)
JP (2) JP5030229B2 (https=)
KR (1) KR20070090172A (https=)
CN (1) CN101094853B (https=)
AT (1) ATE482213T1 (https=)
AU (1) AU2005304784B2 (https=)
CA (1) CA2586375A1 (https=)
DE (1) DE602005023763D1 (https=)
DK (1) DK1812440T3 (https=)
ES (1) ES2354824T3 (https=)
IL (1) IL182893A0 (https=)
MX (1) MX337817B (https=)
NO (1) NO20072795L (https=)
NZ (1) NZ555236A (https=)
PT (1) PT1812440E (https=)
RU (1) RU2417996C2 (https=)
SI (1) SI1812440T1 (https=)
WO (1) WO2006052913A1 (https=)
ZA (1) ZA200704476B (https=)

Families Citing this family (108)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE0104140D0 (sv) * 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
PT1812440E (pt) * 2004-11-04 2011-01-25 Vertex Pharma Pirazolo[1,5-a]pirimidinas úteis enquanto inibidores de proteínas cinases
SI1853588T1 (sl) * 2005-02-16 2008-10-31 Astrazeneca Ab Kemične spojine
US20090156617A1 (en) * 2005-05-12 2009-06-18 Northrup Alan B Tyrosine kinase inhibitors
US20080287437A1 (en) * 2005-05-16 2008-11-20 Astrazeneca Ab Pyrazolylaminopyrimidine Derivatives Useful as Tyrosine Kinase Inhibitors
WO2007046867A2 (en) * 2005-05-19 2007-04-26 Xenon Pharmaceuticals Inc. Piperidine derivatives and their uses as therapeutic agents
EP2354140A1 (en) * 2005-05-20 2011-08-10 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
JP2009513615A (ja) * 2005-10-28 2009-04-02 アストラゼネカ アクチボラグ 癌の治療においてチロシンキナーゼ阻害剤として使用するための４−（３−アミノピラゾール）ピリミジン誘導体
SG10202003901UA (en) 2005-12-13 2020-05-28 Incyte Holdings Corp Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
GB0601638D0 (en) * 2006-01-27 2006-03-08 Merck Sharp & Dohme Therapeutic treatment
US8198448B2 (en) 2006-07-14 2012-06-12 Amgen Inc. Fused heterocyclic derivatives and methods of use
PE20080403A1 (es) 2006-07-14 2008-04-25 Amgen Inc Derivados heterociclicos fusionados y metodos de uso
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
CA2668286C (en) 2006-11-03 2014-09-16 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
MX2009010127A (es) * 2007-03-22 2009-11-05 Vertex Pharma Compuestos utiles como inhibidores de janus cinasas.
JP2010524911A (ja) * 2007-04-18 2010-07-22 アストラゼネカ アクチボラグ ５−アミノピラゾール−３−イル−３Ｈ−イミダゾ［４，５−ｂ］ピリジン誘導体と癌の治療のためのその使用
UA99459C2 (en) * 2007-05-04 2012-08-27 Астразенека Аб 9-(pyrazol-3-yl)- 9h-purine-2-amine and 3-(pyraz0l-3-yl)-3h-imidazo[4,5-b]pyridin-5-amine derivatives and their use for the treatment of cancer
WO2008135786A1 (en) * 2007-05-04 2008-11-13 Astrazeneca Ab Amino-thiazolyl- pyrimidine derivatives and their use for the treatment of cancer
KR20150036210A (ko) 2007-06-13 2015-04-07 인사이트 코포레이션 야누스 키나제 억제제（Ｒ）―３―（４―（７Ｈ―피롤로［２，３－ｄ］피리미딘―4―일）―1Ｈ―피라졸―1―일）―３―사이클로펜틸프로판니트릴의 염
KR20100087298A (ko) * 2007-09-28 2010-08-04 교와 핫꼬 기린 가부시키가이샤 피부 질환의 예방 및/또는 치료제
UA104849C2 (uk) * 2007-11-16 2014-03-25 Інсайт Корпорейшн 4-піразоліл-n-арилпіримідин-2-аміни і 4-піразоліл-n-гетероарилпіримідин-2-аміни як інгібітори кіназ janus
AU2008343813B2 (en) * 2007-12-19 2012-04-12 Amgen Inc. Inhibitors of PI3 kinase
CN101932583A (zh) * 2007-12-19 2010-12-29 沃泰克斯药物股份有限公司 用作JAK2抑制剂的吡唑并[1,5-a]嘧啶类
JP5638961B2 (ja) * 2008-03-13 2014-12-10 ザ ジェネラル ホスピタル コーポレイション Ｂｍｐシグナル伝達経路のインヒビター
KR20110017445A (ko) * 2008-06-11 2011-02-21 아스트라제네카 아베 암 및 골수증식성 장애의 치료에 유용한 트리시클릭 2,4-디아미노-ｌ,3,5-트리아진 유도체
JP5746032B2 (ja) * 2008-09-19 2015-07-08 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ ３，４−ジヒドロ−２Ｈ−ピロロ［１，２−ａ］ピラジン−１−オン誘導体
WO2010033941A1 (en) 2008-09-22 2010-03-25 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors
BRPI0919488A2 (pt) * 2008-09-30 2015-12-01 Astrazeneca Ab composto, uso de um composto, método para tratar câncer em um animal de sangue quente, composição farmacêutica, e, processo para preparar um composto
EP2348860B1 (en) * 2008-10-31 2015-05-27 Genentech, Inc. Pyrazolopyrimidine jak inhibitor compounds and methods
GB0821913D0 (en) 2008-12-02 2009-01-07 Price & Co Antibacterial compounds
AR076794A1 (es) 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
SI2432472T1 (sl) * 2009-05-22 2019-11-29 Incyte Holdings Corp 3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK
CA2762479A1 (en) * 2009-05-28 2010-12-02 Vertex Pharmaceuticals Incorporated Inhibitors of c-met protein kinase
LT3141252T (lt) 2009-06-17 2018-11-12 Vertex Pharmaceuticals Inc. Gripo virusų replikacijos inhibitoriai
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
NZ598985A (en) 2009-09-04 2013-07-26 Biogen Idec Inc Bruton's tyrosine kinase inhibitors
EP3354652B1 (en) 2010-03-10 2020-05-06 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
US20130096160A1 (en) * 2010-04-14 2013-04-18 Secretary, Department Of Health And Human Services Arylthiazolyl piperidines and related compounds as modulators of survival motor neuron (smn) protein production
NZ604306A (en) 2010-05-17 2015-02-27 Incozen Therapeutics Pvt Ltd Novel 3,5-disubstitued-3h-imidazo[4,5-b]pyridine and 3,5- disubstitued -3h-[1,2,3]triazolo[4,5-b] pyridine compounds as modulators of protein kinases
ME03376B (me) 2010-05-20 2020-01-20 Array Biopharma Inc Makrociklička jedinjenja kао inhibiтori trk kinaze
PE20130216A1 (es) 2010-05-21 2013-02-27 Incyte Corp Formulacion topica para un inhibidor de jak
GB2480814A (en) * 2010-06-01 2011-12-07 Summit Corp Plc Compounds for the treatment of clostridium difficile-associated disease
ES2803556T3 (es) 2010-06-01 2021-01-27 Summit Oxford Ltd Compuestos para el tratamiento de enfermedades asociadas a clostridium difficile
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
RU2013132681A (ru) * 2010-12-16 2015-01-27 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы репликации вирусов гриппа
MX354412B (es) * 2011-06-10 2018-03-05 Merck Patent Gmbh Composiciones y metodos para la produccion de compuestos de pirimidina con actividad inhibidora de tirosina cinasa de bruton.
CN103797010B (zh) 2011-06-20 2016-02-24 因塞特控股公司 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物
US9309250B2 (en) 2011-06-22 2016-04-12 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
WO2013028263A1 (en) * 2011-08-24 2013-02-28 Glaxosmithkline Llc Pyrazolopyrimidine derivatives as pi3 kinase inhibitors
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
CN107082779A (zh) 2012-03-30 2017-08-22 理森制药股份公司 作为c‑met 蛋白激酶调节剂的新化合物
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
AR091273A1 (es) * 2012-06-08 2015-01-21 Biogen Idec Inc Inhibidores de pirimidinil tirosina quinasa
WO2014028829A1 (en) * 2012-08-16 2014-02-20 The Scripps Research Institute Novel kappa opioid ligands
PH12020551186B1 (en) 2012-11-15 2024-03-20 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
WO2014081996A1 (en) * 2012-11-23 2014-05-30 Glaxosmithkline Llc Novel compounds as diacylglycerol acyltransferase inhibitors
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
TW201501713A (zh) * 2013-03-01 2015-01-16 Kyowa Hakko Kirin Co Ltd 眼炎症性疾病之預防及／或治療劑
RS62867B1 (sr) 2013-03-06 2022-02-28 Incyte Holdings Corp Postupci i intermedijeri za dobijanje inhibitora jak
WO2014160203A2 (en) 2013-03-14 2014-10-02 The Brigham And Women's Hospital, Inc. Bmp inhibitors and methods of use thereof
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
WO2014175370A1 (ja) * 2013-04-25 2014-10-30 塩野義製薬株式会社 ピロリジン誘導体およびそれらを含有する医薬組成物
SMT202000315T1 (it) 2013-08-07 2020-07-08 Incyte Corp Forme di dosaggio a rilascio prolungato per un inibitore di jak1
JP6618901B2 (ja) 2013-11-13 2019-12-11 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ インフルエンザウイルスの複製の阻害剤を調製する方法
LT3068776T (lt) 2013-11-13 2019-08-12 Vertex Pharmaceuticals Incorporated Gripo virusų replikacijos inhibitoriai
WO2015073267A1 (en) * 2013-11-15 2015-05-21 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
CN104650092B (zh) * 2013-11-16 2017-11-10 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
PT3077397T (pt) 2013-12-06 2020-01-22 Vertex Pharma Composto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-carboxamida útil como inibidor da atr quinase, a sua preparação, diferentes formas sólidas e derivados radiomarcados do mesmo
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
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
MX373102B (es) 2014-06-05 2020-04-17 Vertex Pharma Derivados radiomarcados de un compuesto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida útil como inhibidor de ataxia telangiectasia mutada y rad3 relacionado (atr) cinasa, preparación de tal compuesto y diferentes formas sólidas del mismo.
SG11201610500WA (en) 2014-06-17 2017-01-27 Vertex Pharma Method for treating cancer using a combination of chk1 and atr inhibitors
US10513521B2 (en) 2014-07-15 2019-12-24 The Brigham And Women's Hospital, Inc. Compositions and methods for inhibiting BMP
CN113354649B (zh) 2014-11-16 2024-12-10 阵列生物制药公司 一种新的晶型
EP3294735B8 (en) 2015-05-13 2022-01-05 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
EP3294717B1 (en) 2015-05-13 2020-07-29 Vertex Pharmaceuticals Inc. Methods of preparing inhibitors of influenza viruses replication
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
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
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
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
PL3484888T3 (pl) * 2016-07-18 2023-06-26 University Health Network Stałe postacie inhibitora TTK
JP7214632B2 (ja) 2016-07-21 2023-01-30 バイオジェン エムエー インク． ブルトン型チロシンキナーゼ阻害剤のコハク酸塩形態および組成物
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
EP3615538B1 (en) 2017-04-27 2024-02-07 The Brigham and Women's Hospital, Inc. Novel alk2 inhibitors and methods for inhibiting bmp signaling
PL233595B1 (pl) * 2017-05-12 2019-11-29 Celon Pharma Spolka Akcyjna Pochodne pirazolo[1,5-a]pirymidyny jako inhibitory kinazy JAK
MX387969B (es) 2017-05-22 2025-03-19 Hoffmann La Roche Composiciones y compuestos terapéuticos, y métodos para su uso.
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
BR112020015396A2 (pt) 2018-01-29 2020-12-08 Merck Patent Gmbh Inididores de gcn2 e usos dos mesmos
JP7229257B2 (ja) * 2018-01-29 2023-02-28 メルク パテント ゲーエムベーハー Ｇｃｎ２阻害剤およびその使用
SG11202007164UA (en) 2018-01-30 2020-08-28 Incyte Corp Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
SMT202400306T1 (it) 2018-03-30 2024-09-16 Incyte Corp Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak.
EP3870181B1 (en) * 2018-10-26 2024-08-14 Keros Therapeutics, Inc. Crystal forms of an alk2 inhibitor
CA3124088A1 (en) * 2018-12-20 2020-06-25 Incyte Corporation Imidazopyridazine and imidazopyridine compounds as inhibitors of activin receptor-like kinase-2
US12508262B2 (en) 2020-04-30 2025-12-30 Keros Therapeutics, Inc. Methods of using ALK2 inhibitors
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022098812A1 (en) 2020-11-04 2022-05-12 Keros Therapeutics, Inc. Methods of treating iron overload
EP4392418A4 (en) * 2021-08-24 2025-06-18 The Johns Hopkins University Compositions and methods for treating proteotoxicity-associated diseases
CN116987083A (zh) * 2022-04-25 2023-11-03 杭州健崃生物科技有限公司 吡唑并[1,5-a]嘧啶衍生物及其制备方法和用途
KR102912267B1 (ko) 2023-04-20 2026-01-15 한국화학연구원 신규한 헤테로고리 화합물 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 포함하는 바이러스성 질환의 예방 또는 치료용 약학적 조성물

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002501532A (ja) * 1997-05-30 2002-01-15 メルク エンド カンパニー インコーポレーテッド 新規血管形成阻害薬
US6194410B1 (en) * 1998-03-11 2001-02-27 Hoffman-La Roche Inc. Pyrazolopyrimidine and pyrazolines and process for preparation thereof
US6245759B1 (en) * 1999-03-11 2001-06-12 Merck & Co., Inc. Tyrosine kinase inhibitors
GB0103926D0 (en) * 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
US7550470B2 (en) * 2002-12-11 2009-06-23 Merck & Co. Inc. Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors
PT1812440E (pt) * 2004-11-04 2011-01-25 Vertex Pharma Pirazolo[1,5-a]pirimidinas úteis enquanto inibidores de proteínas cinases

Also Published As

Publication number Publication date
CN101094853B (zh) 2011-07-13
WO2006052913A1 (en) 2006-05-18
EP1812440B1 (en) 2010-09-22
ZA200704476B (en) 2008-09-25
RU2007120518A (ru) 2008-12-10
MX337817B (es) 2011-11-04
DE602005023763D1 (de) 2010-11-04
US7528138B2 (en) 2009-05-05
AU2005304784B2 (en) 2011-03-24
US20060135537A1 (en) 2006-06-22
ATE482213T1 (de) 2010-10-15
CN101094853A (zh) 2007-12-26
JP2009067803A (ja) 2009-04-02
CA2586375A1 (en) 2006-05-18
AU2005304784A1 (en) 2006-05-18
SI1812440T1 (sl) 2011-04-29
JP2008519059A (ja) 2008-06-05
MX2007005439A (es) 2008-02-19
NZ555236A (en) 2010-10-29
NO20072795L (no) 2007-06-01
JP5030229B2 (ja) 2012-09-19
PT1812440E (pt) 2011-01-25
DK1812440T3 (da) 2011-01-31
HK1113569A1 (en) 2008-10-10
IL182893A0 (en) 2007-08-19
EP1812440A1 (en) 2007-08-01
RU2417996C2 (ru) 2011-05-10
KR20070090172A (ko) 2007-09-05

Similar Documents

Publication Publication Date Title
ES2354824T3 (es) Pirazolo[1,5-a]pirimidinas útiles como inhibidores de proteínas cinasas.
ES2528451T3 (es) Inhibidores de esfingosina cinasa
AR060432A1 (es) Tetrahidropteridinas utiles como inhibidores de las proteinas quinasas
AR045261A1 (es) Compuestos que contienen imidazo quinolina o imidazo piridina sustituidos; composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos inmunomoduladores
AR069326A1 (es) Derivados bis-(sulfonilamino), proceso de preparacion, composiciones farmaceuticas que los contienen y su uso en terapia.
AR049443A1 (es) Derivados de pirrolpiridinas
AU592839B2 (en) Pyri (mi) dyl-oxy- and -thio-benzoic acid derivatives
EA201692215A1 (ru) Пирролбензодиазепины и конъюгаты направленного действия
PT1477063E (pt) Misturas herbicidas sinergicas contendo um derivado de uma sulfonilureia e dicamba
MA27475A1 (fr) Composes de pyrazolo [3,4-b] pyridine et leur utilisation en tant qu'inhibiteurs de phosphodiesterase
AR078012A1 (es) Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
AR083933A1 (es) Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
AR086983A1 (es) Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
AR071823A1 (es) Derivados heterociclicos de imidazol y pirazol, inhibidores del factor ixa de coagulacion, composiciones farmaceuticas que los contienen y uso de los mismos para tratar diversos trastornos tromboembolicos.
AR087760A1 (es) Heterociclilaminas como inhibidores de pi3k
CO6170361A2 (es) Composiciones y metodos para modular receptores de c-kit y pdgfr
AR083525A1 (es) Derivados de acido picolinico sustituidos con heterociclos, metodo para prepararlos, uso de los mismos como herbicidas y composiciones herbicidas que los contienen
PE20050308A1 (es) Compuestos heterociclicos n-aril carboxamidas como inhibidores de citoquinas
AR045930A1 (es) Compuestos de quinoxalina
AR056863A1 (es) Compuestos sulfoximino-macrociclicos y sus sales, composiciones farmaceuticas, metodos de preparacion y usos de los mismos
AR061346A1 (es) Pirazolopiridinas sustituidas y sus sales composiciones farmaceuticas que las comprenden metodos para prepararlas y sus usos
HUT60603A (en) Herbicidal compositions comprising n-phenylsulfonyl-n'-heteroaryl urea as active ingredient and process for producing the active ingredients
AR086086A1 (es) Derivados glucosidos y usos de los mismos
AR038404A1 (es) Derivados de nicotinamida utiles como inhibidores de pde4, procedimiento para la preparacion del compuesto y composicion farmaceutica que lo incluye
PE20130640A1 (es) Compuestos heterociclicos, su preparacion y su aplicacion terapeutica