JP2008520738A - プロテインキナーゼの阻害剤として有用なピロロピラジンおよびピラゾロピラジン - Google Patents

プロテインキナーゼの阻害剤として有用なピロロピラジンおよびピラゾロピラジン Download PDF

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JP2008520738A
JP2008520738A JP2007543441A JP2007543441A JP2008520738A JP 2008520738 A JP2008520738 A JP 2008520738A JP 2007543441 A JP2007543441 A JP 2007543441A JP 2007543441 A JP2007543441 A JP 2007543441A JP 2008520738 A JP2008520738 A JP 2008520738A
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aliphatic
optionally substituted
compound according
membered
compound
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JP2008520738A5 (enExample
Inventor
ヘイリー ビンチ，
ダニエル ロビンソン，
アンドリュー ミラー，
ダミアン フレイス，
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Publication of JP2008520738A publication Critical patent/JP2008520738A/ja
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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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P27/02—Ophthalmic agents
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • 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
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    • 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
    • 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
    • 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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Virology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Gynecology & Obstetrics (AREA)
JP2007543441A 2004-11-22 2005-11-22 プロテインキナーゼの阻害剤として有用なピロロピラジンおよびピラゾロピラジン Pending JP2008520738A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US63011504P 2004-11-22 2004-11-22
PCT/US2005/042455 WO2006058074A1 (en) 2004-11-22 2005-11-22 Pyrrolopyrazines and pyrazolopyrazines useful as inhibitors of protein kinases

Related Child Applications (1)

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JP2008235263A Division JP2009024024A (ja) 2004-11-22 2008-09-12 プロテインキナーゼの阻害剤として有用なピロロピラジンおよびピラゾロピラジン

Publications (2)

Publication Number Publication Date
JP2008520738A true JP2008520738A (ja) 2008-06-19
JP2008520738A5 JP2008520738A5 (enExample) 2008-11-06

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ID=35953926

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JP2007543441A Pending JP2008520738A (ja) 2004-11-22 2005-11-22 プロテインキナーゼの阻害剤として有用なピロロピラジンおよびピラゾロピラジン
JP2007543468A Pending JP2008520745A (ja) 2004-11-22 2005-11-22 Ｒｈｏキナーゼの二環式阻害剤
JP2008235263A Pending JP2009024024A (ja) 2004-11-22 2008-09-12 プロテインキナーゼの阻害剤として有用なピロロピラジンおよびピラゾロピラジン

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JP2007543468A Pending JP2008520745A (ja) 2004-11-22 2005-11-22 Ｒｈｏキナーゼの二環式阻害剤
JP2008235263A Pending JP2009024024A (ja) 2004-11-22 2008-09-12 プロテインキナーゼの阻害剤として有用なピロロピラジンおよびピラゾロピラジン

Country Status (14)

Country Link
US (3) US20060122185A1 (enExample)
EP (3) EP2316835A1 (enExample)
JP (3) JP2008520738A (enExample)
KR (1) KR20070089201A (enExample)
CN (1) CN101098872B (enExample)
AU (2) AU2005309566A1 (enExample)
CA (2) CA2587926A1 (enExample)
IL (1) IL183318A0 (enExample)
MX (1) MX2007006103A (enExample)
NO (1) NO20073140L (enExample)
NZ (1) NZ555566A (enExample)
RU (1) RU2394825C2 (enExample)
WO (2) WO2006058120A1 (enExample)
ZA (1) ZA200704888B (enExample)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012510972A (ja) * 2008-12-05 2012-05-17 エフ．ホフマン−ラ ロシュ アーゲー ピロロピラジニル尿素キナーゼ阻害薬
JP2012533551A (ja) * 2009-07-15 2012-12-27 アボット・ラボラトリーズ ピロロピラジン系キナーゼ阻害薬
JP2013529643A (ja) * 2010-06-23 2013-07-22 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 Ａｔｒキナーゼ阻害剤として有用なピロロピラジン誘導体
JP2013534223A (ja) * 2010-08-04 2013-09-02 武田薬品工業株式会社 縮合複素環化合物
JP2015533151A (ja) * 2012-10-16 2015-11-19 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト セリン／スレオニンキナーゼ阻害剤
KR20190092545A (ko) * 2016-12-15 2019-08-07 선샤인 레이크 파르마 컴퍼니 리미티드 인플루엔자 바이러스 복제의 억제제 및 이의 용도

Families Citing this family (135)

* Cited by examiner, † Cited by third party
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HN2005000795A (es) * 2004-10-15 2010-08-19 Aventis Pharma Inc Pirimidinas como antagonistas del receptor de prostaglandina d2
JP2008545660A (ja) * 2005-05-20 2008-12-18 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 プロテインキナーゼ阻害剤として有用なピロロピリジン化合物
CN101253152A (zh) 2005-09-02 2008-08-27 安斯泰来制药株式会社 作为rock抑制剂的酰胺衍生物
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
WO2007076423A2 (en) * 2005-12-22 2007-07-05 Smithkline Beecham Corporation INHIBITORS OF Akt ACTIVITY
NZ592968A (en) 2006-01-17 2012-08-31 Vertex Pharma Azaindoles substituted with either triazine or pyrimidine useful as inhibitors of janus kinases consisting of JAK1, JAK2, JAK3, and TYK2
BRPI0713187A2 (pt) * 2006-07-20 2012-10-16 Mehmet Kahraman método de inibir rho-quinase, método de tratamento de doença mediada por rho-quinase, composto e composição farmacêutica
CL2007002617A1 (es) * 2006-09-11 2008-05-16 Sanofi Aventis Compuestos derivados de pirrolo[2,3-b]pirazin-6-ilo; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar inflamacion de las articulaciones, artritis reumatoide, tumores, linfoma de las celulas del manto.
JP2010505962A (ja) 2006-10-09 2010-02-25 武田薬品工業株式会社 キナーゼ阻害剤
WO2008079346A1 (en) 2006-12-21 2008-07-03 Vertex Pharmaceuticals Incorporated 5-cyan0-4- (pyrrolo [2, 3b] pyridine-3-yl) -pyrimidine derivatives useful as protein kinase inhibitors
SI2124944T1 (sl) 2007-03-14 2012-05-31 Ranbaxy Lab Ltd Derivati pirazolo b piridina kot inhibitorji fosfodiesteraze
KR20090129488A (ko) * 2007-03-22 2009-12-16 버텍스 파마슈티칼스 인코포레이티드 야누스 키나아제의 억제제로서 유용한 ｎ-헤테로사이클릭 화합물
ATE517107T1 (de) * 2008-02-25 2011-08-15 Hoffmann La Roche Pyrrolopyrazinkinaseinhibitoren
ATE522536T1 (de) * 2008-02-25 2011-09-15 Hoffmann La Roche Pyrrolopyrazin-kinasehemmer
CN101952295B (zh) * 2008-02-25 2013-11-20 霍夫曼-拉罗奇有限公司 吡咯并吡嗪激酶抑制剂
ATE519763T1 (de) * 2008-02-25 2011-08-15 Hoffmann La Roche Pyrrolopyrazin-kinasehemmer
RU2503676C2 (ru) * 2008-02-25 2014-01-10 Ф.Хоффманн-Ля Рош Аг Пирролопиразиновые ингибиторы киназы
EP2262498A2 (en) * 2008-03-10 2010-12-22 Vertex Pharmceuticals Incorporated Pyrimidines and pyridines useful as inhibitors of protein kinases
CN104530052A (zh) * 2008-06-10 2015-04-22 普莱希科公司 用于激酶调节的5h-吡咯[2,3-b]吡嗪衍生物和其适应症
NZ590784A (en) * 2008-07-23 2012-12-21 Vertex Pharma Pyrazolopyridine kinase inhibitors
MX2011000837A (es) * 2008-07-23 2011-04-05 Vertex Pharma Inhibidores de pirazolpiridina cinasa triciclica.
WO2010011762A1 (en) * 2008-07-23 2010-01-28 Vertex Pharmaceuticals Incorporated Pyrazolopyridine kinase inhibitors
MX2011001370A (es) * 2008-08-05 2011-03-15 Abbott Lab Compuestos utiles como inhibidores de cinasas de proteina.
KR101712576B1 (ko) 2008-11-10 2017-03-06 버텍스 파마슈티칼스 인코포레이티드 Ａｔｒ 키나제의 억제제로서 유용한 화합물
PL3354650T3 (pl) 2008-12-19 2022-06-13 Vertex Pharmaceuticals Incorporated Związki przydatne jako inhibitory kinazy atr
GEP20207129B (en) 2009-06-17 2020-07-10 Vertex Pharma Inhibitors of influenza viruses replication
US8435980B2 (en) 2009-07-15 2013-05-07 Abbvie Inc. Pyrrolopyridine inhibitors of kinases
EP4782062A2 (en) 2009-12-01 2026-07-29 AbbVie Inc. Novel tricyclic compounds
DE102009060175A1 (de) * 2009-12-23 2011-06-30 Merck Patent GmbH, 64293 Pyrrolo[2,3-d] pyrazin-7-yl-pyrimidin-Verbindungen
MX2012008642A (es) * 2010-01-27 2012-11-23 Vertex Pharma Inhibidores de cinasas de pirazolopiridinas.
AU2011209649A1 (en) * 2010-01-27 2012-08-09 Vertex Pharmaceuticals Incorporated Pyrazolopyrazine kinase inhibitors
EP2528917B1 (en) * 2010-01-27 2016-10-19 Vertex Pharmaceuticals Incorporated Pyrazolopyridines useful for the treatment of autoimmune, inflammatory or (hyper)proliferative diseases
CN101817823B (zh) * 2010-03-31 2012-09-12 上海毕得医药科技有限公司 4，7-二氮杂吲哚及其5位取代物的制备方法
EP2560488B1 (en) 2010-04-23 2015-10-28 Cytokinetics, Inc. Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use
AR081626A1 (es) 2010-04-23 2012-10-10 Cytokinetics Inc Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos
AR081331A1 (es) 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
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