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
JP2010514676A5 (https=
JP2010514676A (ja
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

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Virology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Molecular Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (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 (https=) 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 (https=)
EP (2) EP2124951B1 (https=)
JP (2) JP5406039B2 (https=)
KR (1) KR20090091350A (https=)
CN (1) CN101678022A (https=)
AR (1) AR064675A1 (https=)
AU (1) AU2007338754A1 (https=)
CA (1) CA2673472A1 (https=)
MX (1) MX2009006700A (https=)
NO (1) NO20092668L (https=)
NZ (1) NZ577798A (https=)
TW (1) TW200838517A (https=)
WO (1) WO2008079346A1 (https=)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101313702B1 (ko) 2005-02-03 2013-10-04 와이어쓰 제피티니브 및/또는 에를로티니브 내성암 치료용 약제학적 조성물
EP2354140A1 (en) * 2005-05-20 2011-08-10 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
EP1942937A1 (en) 2005-11-04 2008-07-16 Wyeth Antineoplastic combinations with mtor inhibitor, herceptin, and/or hki-272
CN101678022A (zh) * 2006-12-21 2010-03-24 弗特克斯药品有限公司 可用作蛋白激酶抑制剂的5-氰基-4-(吡咯并[2,3b]吡啶-3-基)嘧啶衍生物
MX2009010127A (es) * 2007-03-22 2009-11-05 Vertex Pharma Compuestos utiles como inhibidores de janus cinasas.
PL2201012T3 (pl) 2007-10-11 2014-11-28 Astrazeneca Ab Pochodne pirolo[2,3-d]pirymidyny jako inhibitory kinazy białkowej b
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
JP2011513483A (ja) * 2008-03-10 2011-04-28 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 タンパク質キナーゼの阻害剤として有用なピリミジンおよびピリジン
BRPI0914790A2 (pt) 2008-06-17 2015-10-20 Wyeth Llc uso de um composto de vinorelbina e um composto de hki-272, composição farmacêutica e produto e kit para o tratamento de neoplasma
US8669273B2 (en) 2008-08-04 2014-03-11 Wyeth Llc Antineoplastic combinations of 4-anilino-3-cyanoquinolines and capecitabine
BRPI1014125A2 (pt) 2009-03-17 2016-04-12 Daiichi Sankyo Co Ltd composto, composição farmacêutica, e, uso de um composto.
DK3000467T3 (da) 2009-04-06 2023-03-27 Wyeth Llc Behandling med neratinib mod brystkræft
MX2011012343A (es) * 2009-05-19 2011-12-14 Dow Agrosciences Llc Compuestos y metodos para controlar hongos.
LT3141252T (lt) 2009-06-17 2018-11-12 Vertex Pharmaceuticals Inc. Gripo virusų replikacijos inhibitoriai
US8933227B2 (en) 2009-08-14 2015-01-13 Boehringer Ingelheim International Gmbh Selective synthesis of functionalized pyrimidines
WO2011018517A1 (en) * 2009-08-14 2011-02-17 Boehringer Ingelheim International Gmbh Regioselective preparation of 2-amino-5-trifluoromethylpyrimidine derivatives
RU2013132681A (ru) 2010-12-16 2015-01-27 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы репликации вирусов гриппа
CN103562205A (zh) 2010-12-16 2014-02-05 沃泰克斯药物股份有限公司 流感病毒复制的抑制剂
EA027506B1 (ru) 2011-04-01 2017-08-31 Астразенека Аб Способ лечения рака молочной железы
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
HRP20191982T4 (hr) 2011-11-30 2023-01-06 Astrazeneca Ab Kombinacijsko liječenje raka
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
MX365640B (es) 2012-12-21 2019-06-10 Plexxikon Inc Compuestos y metodos para la modulacion de quinasas y sus indicaciones.
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
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
SG11201608303QA (en) 2014-04-04 2016-11-29 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
EP3294717B1 (en) 2015-05-13 2020-07-29 Vertex Pharmaceuticals Inc. Methods of preparing inhibitors of influenza viruses replication
EP3294735B8 (en) 2015-05-13 2022-01-05 Vertex Pharmaceuticals Incorporated 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
WO2020232247A1 (en) 2019-05-14 2020-11-19 Provention Bio, Inc. Methods and compositions for preventing type 1 diabetes
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
WO2021222442A1 (en) 2020-04-29 2021-11-04 Plexxikon Inc. Synthesis of heterocyclic compounds
IL298999A (en) 2020-06-11 2023-02-01 Provention Bio Inc Methods and compositions for the prevention of type 1 diabetes
AU2022264775A1 (en) * 2021-04-26 2023-11-09 Ohio State Innovation Foundation Lipid nanomaterials and uses thereof
JP2024520444A (ja) 2021-05-24 2024-05-24 プロヴェンション・バイオ・インコーポレイテッド 1型糖尿病を治療するための方法
US12084453B2 (en) 2021-12-10 2024-09-10 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
JPH10510510A (ja) 1994-06-09 1998-10-13 スミスクライン・ビーチャム・コーポレイション エンドセリン受容体拮抗物質
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
ES2253930T3 (es) * 1998-09-18 2006-06-01 ABBOTT GMBH & CO. KG 4-aminopirrolopirimidinas como inhibidores de quinasa.
AU2494300A (en) 1999-01-07 2000-07-24 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)
ES2260033T3 (es) 1999-07-02 2006-11-01 Stuart A. Lipton Uso de los inhibidores p38 mapk en efermadades oftalmicas.
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
US6369032B1 (en) 2000-09-06 2002-04-09 Ortho-Mcneil Pharmaceutical, Inc. Method for treating allergies
WO2002051837A2 (en) 2000-12-22 2002-07-04 Wyeth Heterocyclindazole and azaindazole compounds as 5-hydroxytryptamine-6 ligands
ATE497603T1 (de) 2001-03-02 2011-02-15 Gpc Biotech Ag Drei-hybrid-assaysystem
SI1392697T1 (en) 2001-03-14 2005-02-28 Wyeth Antidepressant azaheterocyclymethyl derivatives of 2,3-dihydro-1,4-dioxino 2,3-f)quinoline
US7081454B2 (en) * 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors
US6559169B2 (en) 2001-04-24 2003-05-06 Wyeth Antidepressant azaheterocyclymethyl 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
ES2229138T3 (es) 2001-04-26 2005-04-16 Wyeth Derivados antidepresivos azaheterociclilmetilicos de (1,4)- benzodiaxanos condensados con oxaheterociclos.
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
ES2247327T3 (es) 2001-04-26 2006-03-01 Wyeth Derivados azaheterociclimetilicos antidepresivos (isrs) de 7,8-dihidro-3h-6,9-dioxa-1,3-diazaciclopenta(a) naftaleno.
BR0209407A (pt) 2001-04-30 2004-07-06 Wyeth Corp Antidepressivos de azaheterociclilmetila derivados de 7,8-dihidro-1,6,9-trioxa-3-aza-ciclopenta[a[]naftaleno , método de tratamento usando tais compostos e processo para prepará-los
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.
CA2450769A1 (en) * 2001-06-15 2002-12-27 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors
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
AU2003216660A1 (en) * 2002-04-26 2003-11-10 Pfizer Products Inc. N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors
UA78999C2 (en) 2002-06-04 2007-05-10 Wyeth Corp 1-(aminoalkyl)-3-sulfonylazaindoles as ligands of 5-hydroxytryptamine-6
CN1319968C (zh) 2002-08-02 2007-06-06 沃泰克斯药物股份有限公司 用作gsk-3的抑制剂的吡唑组合物
SE0202463D0 (sv) 2002-08-14 2002-08-14 Astrazeneca Ab Novel compounds
AU2003286711A1 (en) * 2002-10-25 2004-05-13 Vertex Pharmaceuticals Incorporated Indazolinone compositions useful as kinase inhibitors
AU2003284399A1 (en) * 2002-11-14 2004-06-03 Kyowa Hakko Kogyo Co., Ltd. Plk inhibitors
JP3876265B2 (ja) 2003-02-26 2007-01-31 ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト ジヒドロプテリジノン、その製造方法及び薬物形態での使用
EP2295433A3 (en) 2003-03-06 2011-07-06 Eisai R&D Management Co., Ltd. JNK inhibitors
US7381825B2 (en) 2003-03-17 2008-06-03 Takeda San Diego, Inc. Histone deacetylase inhibitors
GB0308466D0 (en) 2003-04-11 2003-05-21 Novartis Ag Organic compounds
WO2004106298A1 (en) 2003-05-30 2004-12-09 Janssen Pharmaceutica N.V. Indole derivatives with an improved antipsychotic activity
WO2005000813A1 (en) 2003-05-30 2005-01-06 Imclone Systems Incorporated Heteroarylamino-phenylketone derivatives and their use as kinase inhibitors
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
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
ES2364340T3 (es) 2004-03-30 2011-08-31 Vertex Pharmaceuticals Incorporated Azaindoles útiles como inhibidores de jak y otras proteína quinasas.
AR049333A1 (es) 2004-04-02 2006-07-19 Vertex Pharma Azaindoles inhibidores de proteinquinasas rock y otras proteinas quinasas. composiciones farmaceuticas.
ITMI20040874A1 (it) 2004-04-30 2004-07-30 Ist Naz Stud Cura Dei Tumori Derivati indolici ed azaindolici con azione antitumorale
JP2008503473A (ja) 2004-06-17 2008-02-07 プレキシコン,インコーポレーテッド C−kit活性を調節する化合物
US20060122213A1 (en) 2004-06-30 2006-06-08 Francoise Pierard Azaindoles useful as inhibitors of protein kinases
WO2006015123A1 (en) * 2004-07-27 2006-02-09 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
WO2006058120A1 (en) * 2004-11-22 2006-06-01 Vertex Pharmaceuticals Incorporated Bicyclic inhibitors or rho kinase
US8101770B2 (en) * 2004-12-16 2012-01-24 Vertex Pharmaceuticals Incorporated Pyridones useful as inhibitors of kinases
KR20070104641A (ko) 2005-02-03 2007-10-26 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제의 억제제로 유용한 피롤로피리미딘
RU2387653C2 (ru) * 2005-05-16 2010-04-27 Айрм Ллк Соединения и композиции в качестве ингибиторов протеинкиназ
EP2354140A1 (en) * 2005-05-20 2011-08-10 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
UA95244C2 (ru) 2005-06-22 2011-07-25 Плексикон, Инк. Соединения и способ модулирования активности киназ, и показания для их применения
TW200800921A (en) 2005-09-19 2008-01-01 Astrazeneca Ab Novel compounds
ZA200802685B (en) 2005-09-30 2009-10-28 Vertex Pharma Deazapurines useful as inhibitors of janus kinases
UA95940C2 (uk) 2006-01-17 2011-09-26 Вертекс Фармасьютикалс Інкорпорейтед Азаіндоли як інгібітори кіназ януса
WO2007095223A2 (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
SG170828A1 (en) * 2006-04-05 2011-05-30 Vertex Pharmaceuticals Inc Us Deazapurines useful as inhibitors of janus kinases
EP2038272B8 (en) * 2006-06-30 2013-10-23 Sunesis Pharmaceuticals, Inc. Pyridinonyl pdk1 inhibitors
CN101678022A (zh) 2006-12-21 2010-03-24 弗特克斯药品有限公司 可用作蛋白激酶抑制剂的5-氰基-4-(吡咯并[2,3b]吡啶-3-基)嘧啶衍生物
EP2134709A1 (en) 2007-03-09 2009-12-23 Vertex Pharmaceuticals, Inc. Aminopyridines useful as inhibitors of protein kinases
AU2008226457B2 (en) 2007-03-09 2014-03-20 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
TW200924762A (en) * 2007-11-02 2009-06-16 Vertex Pharma Kinase inhibitors
JP2011513483A (ja) 2008-03-10 2011-04-28 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 タンパク質キナーゼの阻害剤として有用なピリミジンおよびピリジン

Also Published As

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

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
WO2016042341A1 (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
TWI690528B (zh) 稠環雙環吡啶基衍生物
JP2023545196A (ja) 三複素環誘導体、その医薬組成物及び使用
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