JP5406039B2 - タンパク質キナーゼ阻害剤として有用な５−シアノ−４−（ピロロ［２，３ｂ］ピリジン−３−イル）−ピリミジン誘導体 - Google Patents

タンパク質キナーゼ阻害剤として有用な５−シアノ−４−（ピロロ［２，３ｂ］ピリジン−３−イル）−ピリミジン誘導体 Download PDF

Info

Publication number
JP5406039B2
JP5406039B2 JP2009542940A JP2009542940A JP5406039B2 JP 5406039 B2 JP5406039 B2 JP 5406039B2 JP 2009542940 A JP2009542940 A JP 2009542940A JP 2009542940 A JP2009542940 A JP 2009542940A JP 5406039 B2 JP5406039 B2 JP 5406039B2
Authority
JP
Japan
Prior art keywords
group
compound
alkyl
optionally
independently
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 - Fee Related
Application number
JP2009542940A
Other languages
English (en)
Japanese (ja)
Other versions
JP2010514676A (ja
JP2010514676A5 (enExample
Inventor
マイケル・モーティモア
スティーブン・クリントン・ヤング
サイモン・ロバート・ロリー・エバリット
ロナルド・クネフテル
ジョアン・ルイーズ・ピンダー
アリステア・ピーター・ラザフォード
スティーブン・デュラント
ガイ・ブレンチリー
ジャン・ダミアン・シャリエール
マイケル・オドネル
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
Publication of JP2010514676A publication Critical patent/JP2010514676A/ja
Publication of JP2010514676A5 publication Critical patent/JP2010514676A5/ja
Application granted granted Critical
Publication of JP5406039B2 publication Critical patent/JP5406039B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • 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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • AIDS & HIV (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
JP2009542940A 2006-12-21 2007-12-21 タンパク質キナーゼ阻害剤として有用な５−シアノ−４−（ピロロ［２，３ｂ］ピリジン−３−イル）−ピリミジン誘導体 Expired - Fee Related JP5406039B2 (ja)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US87630706P 2006-12-21 2006-12-21
US60/876,307 2006-12-21
US92229107P 2007-04-06 2007-04-06
US60/922,291 2007-04-06
US94770707P 2007-07-03 2007-07-03
US60/947,707 2007-07-03
US98901407P 2007-11-19 2007-11-19
US60/989,014 2007-11-19
PCT/US2007/026190 WO2008079346A1 (en) 2006-12-21 2007-12-21 5-cyan0-4- (pyrrolo [2, 3b] pyridine-3-yl) -pyrimidine derivatives useful as protein kinase inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2013227246A Division JP2014051516A (ja) 2006-12-21 2013-10-31 タンパク質キナーゼ阻害剤として有用な５−シアノ−４−（ピロロ［２，３ｂ］ピリジン−３−イル）−ピリミジン誘導体

Publications (3)

Publication Number Publication Date
JP2010514676A JP2010514676A (ja) 2010-05-06
JP2010514676A5 JP2010514676A5 (enExample) 2011-06-30
JP5406039B2 true JP5406039B2 (ja) 2014-02-05

Family

ID=39272205

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2009542940A Expired - Fee Related JP5406039B2 (ja) 2006-12-21 2007-12-21 タンパク質キナーゼ阻害剤として有用な５−シアノ−４−（ピロロ［２，３ｂ］ピリジン−３−イル）−ピリミジン誘導体
JP2013227246A Pending JP2014051516A (ja) 2006-12-21 2013-10-31 タンパク質キナーゼ阻害剤として有用な５−シアノ−４−（ピロロ［２，３ｂ］ピリジン−３−イル）−ピリミジン誘導体

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2013227246A Pending JP2014051516A (ja) 2006-12-21 2013-10-31 タンパク質キナーゼ阻害剤として有用な５−シアノ−４−（ピロロ［２，３ｂ］ピリジン−３−イル）−ピリミジン誘導体

Country Status (13)

Country Link
US (3) US8247421B2 (enExample)
EP (2) EP2124951B1 (enExample)
JP (2) JP5406039B2 (enExample)
KR (1) KR20090091350A (enExample)
CN (1) CN101678022A (enExample)
AR (1) AR064675A1 (enExample)
AU (1) AU2007338754A1 (enExample)
CA (1) CA2673472A1 (enExample)
MX (1) MX2009006700A (enExample)
NO (1) NO20092668L (enExample)
NZ (1) NZ577798A (enExample)
TW (1) TW200838517A (enExample)
WO (1) WO2008079346A1 (enExample)

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA200706804B (en) 2005-02-03 2008-10-29 Gen Hospital Corp Method for treating gefitinib resistant cancer
NZ564065A (en) * 2005-05-20 2011-03-31 Vertex Pharma Pyrrolopyridines useful as inhibitors of protein kinase
KR101354828B1 (ko) 2005-11-04 2014-02-18 와이어쓰 엘엘씨 ｍＴＯＲ 저해자, 헤르셉틴, 및/또는 ＨＫＩ-272의항신생물성 조합
US8247421B2 (en) * 2006-12-21 2012-08-21 Vertex Pharmaceuticals Incorporated 5-cyano-4-(pyrrolo [2,3B] pyridine-3-yl)-pyrimidine derivatives useful as protein kinase inhibitors
CN101778825A (zh) * 2007-03-22 2010-07-14 沃泰克斯药物股份有限公司 适用作詹纳斯激酶抑制剂的n-杂环类化合物
AU2008309383B2 (en) 2007-10-11 2012-04-19 Astrazeneca Ab Pyrrolo [2, 3 -D] pyrimidin derivatives as protein kinase B inhibitors
US8022216B2 (en) 2007-10-17 2011-09-20 Wyeth Llc Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof
EP2262498A2 (en) * 2008-03-10 2010-12-22 Vertex Pharmceuticals Incorporated Pyrimidines and pyridines useful as inhibitors of protein kinases
CA2725598C (en) 2008-06-17 2013-10-08 Wyeth Llc Antineoplastic combinations containing hki-272 and vinorelbine
MX2011001318A (es) 2008-08-04 2011-03-04 Wyeth Llc Combinaciones antineoplasicas de 4-anilino-3-cianoquinolinas y capecitabina.
MX2011009700A (es) 2009-03-17 2011-12-08 Daiichi Sankyo Co Ltd Derivado de amida.
EP2416774B1 (en) 2009-04-06 2015-11-04 Wyeth LLC Treatment regimen utilizing neratinib for breast cancer
NZ596123A (en) * 2009-05-19 2014-08-29 Dow Agrosciences Llc Compounds and methods for controlling fungi
GEAP202213376A (en) 2009-06-17 2022-02-25 Vertex Pharmaceuticals Incorporated Us Inhibitors of influenza viruses replication
US8933227B2 (en) 2009-08-14 2015-01-13 Boehringer Ingelheim International Gmbh Selective synthesis of functionalized pyrimidines
EP2464633A1 (en) 2009-08-14 2012-06-20 Boehringer Ingelheim International GmbH Regioselective preparation of 2-amino-5-trifluoromethylpyrimidine derivatives
JP2013545818A (ja) * 2010-12-16 2013-12-26 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 インフルエンザウイルス複製阻害物質
CN103492381A (zh) 2010-12-16 2014-01-01 沃泰克斯药物股份有限公司 流感病毒复制的抑制剂
BR112013025410A2 (pt) 2011-04-01 2016-12-20 Astrazeneca Ab tratamento terapêutico
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
CA2856646C (en) 2011-11-30 2020-01-14 Astrazeneca Ab Combination treatment of cancer
AU2013204533B2 (en) 2012-04-17 2017-02-02 Astrazeneca Ab Crystalline forms
WO2014004543A1 (en) * 2012-06-25 2014-01-03 Mone Zaidi Consulting, Inc. Combination cancer therapy using bisphosphonates and anti-egfr agents
KR102212923B1 (ko) 2012-12-21 2021-02-04 플렉시콘 인코퍼레이티드 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증
GB2515785A (en) * 2013-07-03 2015-01-07 Redx Pharma Ltd Compounds
WO2015007206A1 (zh) * 2013-07-16 2015-01-22 杭州普晒医药科技有限公司 阿法替尼酸加成盐及其晶型、其制备方法及药物组合物
LT3068776T (lt) 2013-11-13 2019-08-12 Vertex Pharmaceuticals Incorporated Gripo virusų replikacijos inhibitoriai
HUE052178T2 (hu) 2013-11-13 2021-04-28 Vertex Pharma Eljárások influenzavírus-replikáció inhibitorainak elõállítására
CA2946538A1 (en) 2014-04-04 2015-10-08 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
JP6857617B2 (ja) 2015-05-13 2021-04-14 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
WO2016183116A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
WO2016210345A1 (en) * 2015-06-25 2016-12-29 The California Institute For Biomedical Research Composition and methods for inhibiting mammalian sterile 20-like kinase 1
CA3003741A1 (en) * 2015-11-02 2017-05-11 University Of Rochester Bortezomib conjugates and methods using same
EP3383875B1 (en) 2015-11-30 2022-02-09 Council Of Scientific & Industrial Research 3-pyrimidinyl pyrrolo [2,3-b] pyridine as anticancer agents and the process for the preparation thereof
IL288024B2 (en) 2019-05-14 2025-12-01 Provention Bio Inc Methods and compositions for preventing type
CN110372713B (zh) * 2019-08-15 2022-05-17 广州市汉普医药有限公司 一种普拉洛芬的精制纯化方法
MX2022007265A (es) * 2019-12-20 2022-09-09 Nuevolution As Compuestos activos frente a receptores nucleares.
BR112022021920A2 (pt) 2020-04-29 2023-01-17 Plexxikon Inc Síntese de compostos heterocíclicos
US12006366B2 (en) 2020-06-11 2024-06-11 Provention Bio, Inc. Methods and compositions for preventing type 1 diabetes
JP2024515964A (ja) * 2021-04-26 2024-04-11 オハイオ ステート イノベーション ファウンデーション 脂質ナノ材料及びその使用
MX2023013851A (es) 2021-05-24 2023-12-08 Provention Bio Inc Metodos para el tratamiento de diabetes tipo 1.
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors
WO2025228376A1 (zh) * 2024-04-30 2025-11-06 阿诺医药 (新加坡) 有限公司 Cyclin K降解剂药物及其抗体偶联物

Family Cites Families (78)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ221717A (en) 1986-09-10 1990-08-28 Sandoz Ltd Azaindole and indolizine derivatives and pharmaceutical compositions
JP2779403B2 (ja) 1988-11-29 1998-07-23 日本バイエルアグロケム株式会社 殺虫性ニトロ化合物
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
FR2687402B1 (fr) 1992-02-14 1995-06-30 Lipha Nouveaux azaindoles, procedes de preparation et medicaments les contenant.
US5886026A (en) 1993-07-19 1999-03-23 Angiotech Pharmaceuticals Inc. Anti-angiogenic compositions and methods of use
WO1995033748A1 (en) 1994-06-09 1995-12-14 Smithkline Beecham Corporation Endothelin receptor antagonists
US6221894B1 (en) 1995-03-20 2001-04-24 Merck & Co., Inc. Nodulisporic acid derivatives
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
GB9721437D0 (en) 1997-10-10 1997-12-10 Glaxo Group Ltd Heteroaromatic compounds and their use in medicine
JP2002527359A (ja) * 1998-09-18 2002-08-27 ビーエーエスエフ アクチェンゲゼルシャフト キナーゼインヒビターとしての４−アミノピロリピリミジン
WO2000040581A1 (en) 1999-01-07 2000-07-13 American Home Products Corporation 3,4-dihydro-2h-benzo[1,4]oxazine derivatives
US6265403B1 (en) 1999-01-20 2001-07-24 Merck & Co., Inc. Angiogenesis inhibitors
US20030153560A1 (en) * 1999-04-23 2003-08-14 Salituro Francesco G. Inhibitors of c-Jun N-terminal kinases (JNK)
JP2003503456A (ja) 1999-07-02 2003-01-28 スチュアート エイ． リプトン 神経傷害またはアポトーシスを軽減する方法
US7041277B2 (en) 2000-03-10 2006-05-09 Cadbury Adams Usa Llc Chewing gum and confectionery compositions with encapsulated stain removing agent compositions, and methods of making and using the same
HK1053129A1 (zh) 2000-09-06 2003-10-10 Ortho-Mcneil Pharmaceutical, Inc. 治疗变态反应的方法
JP4307073B2 (ja) 2000-12-22 2009-08-05 ワイス ５−ヒドロキシトリプトアミン−６リガンドとしてのヘテロサイクルインダゾールおよびアザインダゾール化合物
CA2439263C (en) 2001-03-02 2012-10-23 Frank Becker Three hybrid assay system
PT1392697E (pt) 2001-03-14 2005-01-31 Wyeth Corp Antidepressivos derivados aza-heterociclilmetilo de 2,3- di-hidro-1,4-dioxino[2,3-f]quinolina
US7081454B2 (en) * 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors
EP1381600A1 (en) 2001-04-24 2004-01-21 Wyeth, A Corporation of the State of Delaware Antidepressant azaheterocyclylmethyl derivatives of 2,3-dihydro-1,4-benzodioxan
US6656950B2 (en) 2001-04-25 2003-12-02 Wyeth Antidepressant azaheterocyclylmethyl derivatives of 1,4-dioxino[2,3-b]pyridine
JP2004527563A (ja) 2001-04-26 2004-09-09 ワイス 抗うつ作用を有する、２，３−ジヒドロ−１，４−ジオキシノ［２，３−ｆ］キノキサリンのアザへテロシクリルメチル誘導体
BR0209408A (pt) 2001-04-26 2004-07-06 Wyeth Corp Antidepressivos de azaheterociclilmetila derivados de 7,8-dihidro-3h-6,9-dioxa-1,3-diaza-ciclopenta[a]naftal eno, método de tratamento usando tais compostos e processo para prepará-los
JP2004532236A (ja) 2001-04-26 2004-10-21 ワイス 抗うつ作用を持つ、オキサヘテロ環結合［１、４］−ベンゾジオキサンのアザヘテロシクリルメチル誘導体
CN1256337C (zh) 2001-04-30 2006-05-17 惠氏公司 抗抑郁的7,8－二氢－1,6,9－三氧杂－3－氮杂－环戊二烯并[a]萘的氮杂环基甲基衍生物
MXPA03010524A (es) 2001-05-17 2005-03-07 Wyeth Corp Proceso para la sintesis de derivados de la 2,3-dihidro-1,4-dioxino-[2,3-f]-quinolina.
US6825190B2 (en) * 2001-06-15 2004-11-30 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
US20040236110A1 (en) * 2001-09-26 2004-11-25 Ladouceur Gaetan H Substituted 3-pyridyl indoles and indazoles as c17,20 lyase inhibitors
TW200306819A (en) * 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
US7304061B2 (en) 2002-04-26 2007-12-04 Vertex Pharmaceuticals Incorporated Heterocyclic inhibitors of ERK2 and uses thereof
DE60302150D1 (en) * 2002-04-26 2005-12-08 Pfizer Prod Inc N-substituiete heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trion metalloproteinase inhibitoren
UA78999C2 (en) 2002-06-04 2007-05-10 Wyeth Corp 1-(aminoalkyl)-3-sulfonylazaindoles as ligands of 5-hydroxytryptamine-6
DE60308387T2 (de) * 2002-08-02 2007-09-20 Vertex Pharmaceuticals Inc., Cambridge Pyrazolenthaltende zusammensetzungen und ihre verwendung als gsk-3 inhibitoren
SE0202463D0 (sv) 2002-08-14 2002-08-14 Astrazeneca Ab Novel compounds
US7262200B2 (en) * 2002-10-25 2007-08-28 Vertex Pharmaceuticals Incorporated Indazolinone compositions useful as kinase inhibitors
WO2004043936A1 (ja) * 2002-11-14 2004-05-27 Kyowa Hakko Kogyo Co., Ltd. Ｐｌｋ阻害剤
UA80743C2 (en) 2003-02-26 2007-10-25 Boehringer Ingelheim Pharma Dihydropteridinones, method for the production and use thereof in the form of drugs
EP2295433A3 (en) 2003-03-06 2011-07-06 Eisai R&D Management Co., Ltd. JNK inhibitors
JP2006520796A (ja) 2003-03-17 2006-09-14 タケダ サン ディエゴ インコーポレイテッド ヒストンデアセチラーゼインヒビター
GB0308466D0 (en) 2003-04-11 2003-05-21 Novartis Ag Organic compounds
WO2005000813A1 (en) 2003-05-30 2005-01-06 Imclone Systems Incorporated Heteroarylamino-phenylketone derivatives and their use as kinase inhibitors
WO2004106298A1 (en) 2003-05-30 2004-12-09 Janssen Pharmaceutica N.V. Indole derivatives with an improved antipsychotic activity
AR045595A1 (es) 2003-09-04 2005-11-02 Vertex Pharma Composiciones utiles como inhibidores de proteinas quinasas
WO2005044181A2 (en) 2003-09-09 2005-05-19 Temple University-Of The Commonwealth System Of Higher Education Protection of tissues and cells from cytotoxic effects of ionizing radiation by abl inhibitors
CN1897950A (zh) * 2003-10-14 2007-01-17 惠氏公司 稠合芳基和杂芳基衍生物及其使用方法
CN1925855B (zh) 2003-12-19 2010-06-16 普莱希科公司 开发Ret调节剂的化合物和方法
GB0405055D0 (en) 2004-03-05 2004-04-07 Eisai London Res Lab Ltd JNK inhibitors
NZ584499A (en) 2004-03-30 2011-08-26 Vertex Pharma Azaindoles Useful as Inhibitors of Jak and Other Protein Kinases
TW200604168A (en) 2004-04-02 2006-02-01 Vertex Pharma Azaindoles useful as inhibitors of rock and other protein kinases
ITMI20040874A1 (it) 2004-04-30 2004-07-30 Ist Naz Stud Cura Dei Tumori Derivati indolici ed azaindolici con azione antitumorale
CA2570817A1 (en) 2004-06-17 2006-01-26 Plexxikon, Inc. Azaindoles modulating c-kit activity and uses therefor
US20060122213A1 (en) 2004-06-30 2006-06-08 Francoise Pierard Azaindoles useful as inhibitors of protein kinases
US7361763B2 (en) 2004-07-27 2008-04-22 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
AU2005278292B2 (en) * 2004-08-31 2011-09-08 Msd K.K. Novel substituted imidazole derivatives
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
WO2006038001A1 (en) 2004-10-06 2006-04-13 Celltech R & D Limited Aminopyrimidine derivatives as jnk inhibitors
WO2006050076A1 (en) * 2004-10-29 2006-05-11 Janssen Pharmaceutica, N.V. Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
EP1814883A1 (en) * 2004-11-22 2007-08-08 Vertex Pharmaceuticals Incorporated Bicyclic inhibitors or rho kinase
EP1831168B1 (en) * 2004-12-16 2014-07-02 Vertex Pharmaceuticals Inc. Pyrid-2-ones useful as inhibitors of tec family protein kinases for the treatment of inflammatory, proliferative and immunologically-mediated diseases.
RU2434871C2 (ru) 2005-02-03 2011-11-27 Вертекс Фармасьютикалз Инкорпорейтед Пирролопиримидины, применимые в качестве ингибиторов протеинкиназы
AU2006247322A1 (en) * 2005-05-16 2006-11-23 Irm Llc Pyrrolopyridine derivatives as protein kinase inhibitors
NZ564065A (en) 2005-05-20 2011-03-31 Vertex Pharma Pyrrolopyridines useful as inhibitors of protein kinase
PL2395004T3 (pl) 2005-06-22 2016-08-31 Plexxikon Inc Pochodne pirolo[2,3-b]pirydyny jako inhibitory kinazy białkowej
TW200800921A (en) 2005-09-19 2008-01-01 Astrazeneca Ab Novel compounds
EP2532667A1 (en) 2005-09-30 2012-12-12 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
AR060316A1 (es) 2006-01-17 2008-06-11 Vertex Pharma Azaindoles de utilidad como inhibidores de janus quinasas
CA2641254A1 (en) * 2006-02-14 2007-08-23 Vertex Pharmaceuticals Incorporated Pyrrolo(3,2-c) pyridines useful as inhibitors of protein kinases
DE102006012617A1 (de) 2006-03-20 2007-09-27 Merck Patent Gmbh 4-(Pyrrolopyridinyl)-pyrimidinyl-2-amin-derivate
CN101460499A (zh) * 2006-04-05 2009-06-17 沃泰克斯药物股份有限公司 可用作janus激酶抑制剂的去氮杂嘌呤
EP2038272B8 (en) * 2006-06-30 2013-10-23 Sunesis Pharmaceuticals, Inc. Pyridinonyl pdk1 inhibitors
US8247421B2 (en) 2006-12-21 2012-08-21 Vertex Pharmaceuticals Incorporated 5-cyano-4-(pyrrolo [2,3B] pyridine-3-yl)-pyrimidine derivatives useful as protein kinase inhibitors
WO2008112642A1 (en) 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
EP2137183B1 (en) 2007-03-09 2011-09-28 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
EP2134709A1 (en) 2007-03-09 2009-12-23 Vertex Pharmaceuticals, Inc. Aminopyridines useful as inhibitors of protein kinases
CA2704266A1 (en) * 2007-11-02 2009-06-11 Vertex Pharmaceuticals Incorporated [1h- pyrazolo [3, 4-b] pyridine-4-yl] -phenyle or -pyridin-2-yle derivatives as protein kinase c-theta
EP2262498A2 (en) 2008-03-10 2010-12-22 Vertex Pharmceuticals Incorporated Pyrimidines and pyridines useful as inhibitors of protein kinases

Also Published As

Publication number Publication date
MX2009006700A (es) 2009-06-30
EP2124951B1 (en) 2014-05-21
CN101678022A (zh) 2010-03-24
US20140045812A1 (en) 2014-02-13
NO20092668L (no) 2009-09-21
AR064675A1 (es) 2009-04-15
KR20090091350A (ko) 2009-08-27
US8530489B2 (en) 2013-09-10
AU2007338754A1 (en) 2008-07-03
JP2010514676A (ja) 2010-05-06
US20100189773A1 (en) 2010-07-29
CA2673472A1 (en) 2008-07-03
TW200838517A (en) 2008-10-01
WO2008079346A1 (en) 2008-07-03
NZ577798A (en) 2012-04-27
US8247421B2 (en) 2012-08-21
EP2124951A1 (en) 2009-12-02
JP2014051516A (ja) 2014-03-20
US20120309963A1 (en) 2012-12-06
EP2815750A1 (en) 2014-12-24
US8962642B2 (en) 2015-02-24

Similar Documents

Publication Publication Date Title
JP5406039B2 (ja) タンパク質キナーゼ阻害剤として有用な５−シアノ−４−（ピロロ［２，３ｂ］ピリジン−３−イル）−ピリミジン誘導体
TWI863945B (zh) 2-側氧基喹唑啉衍生物作為甲硫胺酸腺苷基轉移酶２ａ抑制劑
JP6026427B2 (ja) 置換６，６−縮合窒素複素環化合物及びその使用
JP5389785B2 (ja) キナーゼ阻害剤として有用なチアゾールおよびピラゾール
ES2715611T3 (es) Compuestos novedosos de 3H-imidazo[4,5-b]piridina-3,5-disustituida y 3H-[1,2,3]triazolo[4,5-b]piridina 3,5-disustituida como moduladores de proteína cinasas
JP5572087B2 (ja) キナーゼ阻害として有用なアミノピリミジン
JP5389786B2 (ja) キナーゼ阻害として有用なアミノピリミジン
CN105566321B (zh) 杂芳化合物及其在药物中的应用
AU2014234909B2 (en) Acyclic cyanoethylpyrazolo pyridones as Janus kinase inhibitors
KR20110039563A (ko) 피라졸로피리딘 키나제 억제제
EP3883575B1 (en) Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use
JP2010524962A (ja) オーロラキナーゼ阻害剤のための創薬法
KR20110033299A (ko) 트리-사이클릭 피라졸로피리딘 키나제 억제제
KR20160086930A (ko) 피롤로피롤론 유도체 및 bet 억제제로서의 그의 용도
JP2013256532A (ja) キナーゼインヒビターとして有用なアミノピリミジン
EP3194390A1 (en) Pyrrolcarboxamide derivatives for the inhbition of erk5
KR20220070229A (ko) 아자-퀴놀린 화합물 및 그의 용도
JP2013518111A (ja) ピラゾロピリジンキナーゼ阻害剤
JP2023545196A (ja) 三複素環誘導体、その医薬組成物及び使用
TWI690528B (zh) 稠環雙環吡啶基衍生物
HK1142267A (en) 5-cyan0-4- (pyrrolo [2,3b] pyridine-3-yl)-pyrimidine derivatives useful as protein kinase inhibitors
HK1156026B (en) Pyrazolopyridine kinase inhibitors

Legal Events

Date Code Title Description
A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20101220

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20110510

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20130129

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20130226

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20130521

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20130528

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20130619

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20130626

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20130826

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20131001

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20131031

LAPS Cancellation because of no payment of annual fees