JP5739446B2 - ピロロ[2,3−d]ピリミジン化合物 - Google Patents

ピロロ[2,3−d]ピリミジン化合物 Download PDF

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JP5739446B2
JP5739446B2 JP2012544596A JP2012544596A JP5739446B2 JP 5739446 B2 JP5739446 B2 JP 5739446B2 JP 2012544596 A JP2012544596 A JP 2012544596A JP 2012544596 A JP2012544596 A JP 2012544596A JP 5739446 B2 JP5739446 B2 JP 5739446B2
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alkyl
group
methyl
amino
cyclohexyl
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JP2013514356A (ja
JP2013514356A5 (enExample
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シェ ジン
シェ ジン
アン プロモ ミシェル
アン プロモ ミシェル
ジョン ジャコブセン エリック
ジョン ジャコブセン エリック
フアング ホーング−チフ
フアング ホーング−チフ
マダックス トッド
マダックス トッド
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ファイザー・インク
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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
    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • 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
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
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    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/04—Artificial tears; Irrigation solutions
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
JP2012544596A 2009-12-18 2010-12-06 ピロロ[2,3−d]ピリミジン化合物 Expired - Fee Related JP5739446B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US28792409P 2009-12-18 2009-12-18
US61/287,924 2009-12-18
PCT/US2010/059046 WO2011075334A1 (en) 2009-12-18 2010-12-06 Pyrrolo[2,3-d]pyrimidine compounds

Publications (3)

Publication Number Publication Date
JP2013514356A JP2013514356A (ja) 2013-04-25
JP2013514356A5 JP2013514356A5 (enExample) 2014-01-09
JP5739446B2 true JP5739446B2 (ja) 2015-06-24

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JP2012544596A Expired - Fee Related JP5739446B2 (ja) 2009-12-18 2010-12-06 ピロロ[2,3−d]ピリミジン化合物

Country Status (6)

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US (1) US8372854B2 (enExample)
EP (1) EP2513114B1 (enExample)
JP (1) JP5739446B2 (enExample)
CA (1) CA2782720A1 (enExample)
ES (1) ES2461967T3 (enExample)
WO (1) WO2011075334A1 (enExample)

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HUE028588T2 (hu) 2005-12-13 2016-12-28 Incyte Holdings Corp Heteroaril-szubsztituált pirrolo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok
CA2792508C (en) 2010-03-10 2018-01-16 Incyte Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
US8691807B2 (en) 2011-06-20 2014-04-08 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
BR112014002472A2 (pt) 2011-08-12 2017-04-11 Nissan Chemical Ind Ltd "compostos heterocíclicos tricíclicos, seu uso, agente terapêutico para reumatismo articular e medicamento"
AU2012312303B2 (en) 2011-09-22 2016-09-15 Merck Sharp & Dohme Corp. Cyanomethylpyrazole carboxamides as janus kinase inhibitors
EP2788000B1 (en) * 2011-12-06 2018-05-30 Merck Sharp & Dohme Corp. Pyrrolopyrimidines as janus kinase inhibitors
CN104619693B (zh) * 2012-07-17 2019-08-13 葛兰素史克知识产权第二有限公司 作为选择性雄激素受体调节剂的吲哚腈类
KR102242077B1 (ko) 2012-11-15 2021-04-20 인사이트 홀딩스 코포레이션 룩솔리티니브의 서방성 제형
WO2014118388A1 (en) 2013-02-04 2014-08-07 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for assaying jak2 activity in red blood cells and uses thereof
JP6248948B2 (ja) 2013-02-08 2017-12-20 日産化学工業株式会社 3環性ピロロピリジン化合物及びjak阻害剤
EA027879B1 (ru) * 2013-02-22 2017-09-29 Пфайзер Инк. ПРОИЗВОДНЫЕ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-РОДСТВЕННЫХ КИНАЗ (JAK)
MX376856B (es) 2013-08-07 2025-03-07 Incyte Holdings Corp Formas de dosificacion de liberacion prolongada para un inhibidor de jak 1 (cinasa de janus 1).
EP2924026A1 (en) * 2014-03-28 2015-09-30 Novartis Tiergesundheit AG Aminosulfonylmethylcyclohexanes as JAK inhibitors
JP6561984B2 (ja) 2014-05-14 2019-08-21 日産化学株式会社 3環性化合物及びjak阻害剤
WO2016024185A1 (en) 2014-08-12 2016-02-18 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase
TWI679205B (zh) 2014-09-02 2019-12-11 日商日本新藥股份有限公司 吡唑并噻唑化合物及醫藥
RU2699034C1 (ru) * 2016-02-16 2019-09-03 ЗОИТИС СЕРВИСЕЗ ЭлЭлСи Способ получения соединений 7H-пирроло[2,3-d]пиримидина
CN107098908B (zh) * 2016-02-23 2021-01-08 欣凯医药科技(上海)有限公司 一种吡咯并嘧啶类化合物的制备方法和应用
TWI712604B (zh) 2016-03-01 2020-12-11 日商日本新藥股份有限公司 具jak抑制作用之化合物之結晶
CN107365312B (zh) * 2016-05-13 2021-10-01 瑞博(杭州)医药科技有限公司 一种制备Oclacitinib的新方法
WO2018167283A1 (en) 2017-03-17 2018-09-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling
US20200088732A1 (en) 2017-04-13 2020-03-19 INSERM (Institut National de la Santé et de la Recherche Mèdicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
DK3915989T3 (da) * 2019-01-30 2023-09-18 Felicamed Biotechnology Co Ltd Jak inhibitor and preparation method therefor
EP3969458A4 (en) 2019-05-13 2023-05-17 Borah, Inc. CHEMICAL COMPOUNDS
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN114605420B (zh) * 2022-04-25 2024-07-12 江苏慧聚药业股份有限公司 马来酸奥拉替尼的合成方法
CN118255769A (zh) * 2022-12-28 2024-06-28 格格巫(珠海)生物科技有限公司 一种立体异构体的制备方法及中间体

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PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
OA12118A (en) 1999-12-10 2006-05-04 Pfizer Prod Inc PyrroloÄ2,3-dÜpyrimidine compounds.
OA12292A (en) * 2000-06-26 2003-11-11 Pfizer Prod Inc PyrroloÄ2,3-dÜpyrimidine compounds as immunosuppressive agents.
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
RS20050380A (sr) 2002-11-21 2007-11-15 Pfizer Products Inc., Derivati 3-aminopiperidina i postupci njihove proizvodnje
WO2006133426A2 (en) 2005-06-08 2006-12-14 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
CN102127078A (zh) 2005-07-14 2011-07-20 安斯泰来制药株式会社 Janus激酶3的杂环类抑制剂
WO2007012953A2 (en) 2005-07-29 2007-02-01 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidine derivatives; their intermediates and synthesis
CN101801971A (zh) 2005-09-30 2010-08-11 沃泰克斯药物股份有限公司 可用作janus激酶抑制剂的脱氮嘌呤
WO2007053452A1 (en) 2005-11-01 2007-05-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
WO2007098507A2 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
BRPI0806811A2 (pt) * 2007-01-23 2011-09-13 Palau Pharma Sa derivados de purina
RS53382B (sr) * 2008-08-20 2014-10-31 Zoetis Llc Jedinjenja pirol [2,3-d]pirimidina
AU2010308028A1 (en) * 2009-10-15 2012-04-19 Pfizer Inc. Pyrrolo[2,3-d] pyrimidine compounds

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Publication number Publication date
ES2461967T3 (es) 2014-05-21
CA2782720A1 (en) 2011-06-23
JP2013514356A (ja) 2013-04-25
WO2011075334A1 (en) 2011-06-23
EP2513114A1 (en) 2012-10-24
US8372854B2 (en) 2013-02-12
US20110294826A1 (en) 2011-12-01
EP2513114B1 (en) 2014-04-02

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