JP5927201B2 - Ａｓｋ１阻害ピロロピリミジン誘導体 - Google Patents

Ａｓｋ１阻害ピロロピリミジン誘導体 Download PDF

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JP5927201B2
JP5927201B2 JP2013543883A JP2013543883A JP5927201B2 JP 5927201 B2 JP5927201 B2 JP 5927201B2 JP 2013543883 A JP2013543883 A JP 2013543883A JP 2013543883 A JP2013543883 A JP 2013543883A JP 5927201 B2 JP5927201 B2 JP 5927201B2
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pyrrolo
pyrimidin
piperidinyl
methyl
benzamide
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JP2014505037A (ja
JP2014505037A5 (enExample
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アール．ウイトトイ ダビド
アール．ウイトトイ ダビド
ノルトン ダビド
ノルトン ダビド
パウル トイエルネイ ジャソン
パウル トイエルネイ ジャソン
ロルトヒオイル グヒスライネ
ロルトヒオイル グヒスライネ
シメ マイリ
シメ マイリ
ロウイセ プヒルポトト カレン
ロウイセ プヒルポトト カレン
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カルチャン リミテッド
カルチャン リミテッド
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    • C07—ORGANIC CHEMISTRY
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    • 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
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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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JP2013543883A 2010-12-16 2011-12-15 Ａｓｋ１阻害ピロロピリミジン誘導体 Expired - Fee Related JP5927201B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US42386510P 2010-12-16 2010-12-16
US61/423,865 2010-12-16
PCT/GB2011/052484 WO2012080735A1 (en) 2010-12-16 2011-12-15 Ask1 inhibiting pyrrolopyrimidine derivatives

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JP2014505037A JP2014505037A (ja) 2014-02-27
JP2014505037A5 JP2014505037A5 (enExample) 2016-01-07
JP5927201B2 true JP5927201B2 (ja) 2016-06-01

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US (3) US9045485B2 (enExample)
EP (1) EP2651417B1 (enExample)
JP (1) JP5927201B2 (enExample)
ES (1) ES2617339T3 (enExample)
PL (1) PL2651417T3 (enExample)
WO (1) WO2012080735A1 (enExample)

Families Citing this family (32)

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Publication number Priority date Publication date Assignee Title
TWI625121B (zh) 2009-07-13 2018-06-01 基利科學股份有限公司 調節細胞凋亡信號之激酶的抑制劑
PL2651417T3 (pl) * 2010-12-16 2017-08-31 Calchan Limited Pochodne pirolopirymidyny hamujące ASK1
UY34573A (es) 2012-01-27 2013-06-28 Gilead Sciences Inc Inhibidor de la quinasa que regula la señal de la apoptosis
ES2889757T3 (es) 2012-09-06 2022-01-13 Plexxikon Inc Compuestos y procedimientos para la modulación de quinasas e indicaciones para estos
CN104119342A (zh) * 2013-04-25 2014-10-29 苏州科捷生物医药有限公司 一种制备高纯度4-氯-5-甲基-7H-吡咯[2,3-d]嘧啶的方法
WO2015187499A1 (en) * 2014-06-03 2015-12-10 Gilead Sciences, Inc. Use of an ask1 inhibitor for the treatment of liver disease, optionally in combination with a loxl2 inhibitor
TW201618781A (zh) 2014-08-13 2016-06-01 吉李德科學股份有限公司 治療肺高血壓之方法
BR112017004589A2 (pt) * 2014-09-10 2018-01-23 Epizyme Inc composto, composição farmacêutica, método para tratar um paciente, uso de um composto, kit, e método para tratar um distúrbio mediado por proteína smyd
NZ729678A (en) 2014-09-24 2018-07-27 Gilead Sciences Inc Methods of treating non-alcoholic steatohepatitis using ask1 inhibitor in combination with a fxr agonist
TWI749934B (zh) 2014-12-23 2021-12-11 美商基利科學股份有限公司 製備2-氟-4-甲基-5-(4-環丙基-1h-咪唑-1-基)苯甲酸之方法
MA41252A (fr) 2014-12-23 2017-10-31 Gilead Sciences Inc Formes solides d'un inhibiteur d'ask 1
MX377489B (es) 2016-08-31 2025-03-10 Eisai R&D Man Co Ltd Compuesto de pirazolo[1,5-a]pirimidina.
JOP20190221A1 (ar) 2017-04-05 2019-09-23 Seal Rock Therapeutics Inc مركبات مثبطات كيناز منظم لإشارات الاستماتة 1 (ask1) واستخداماتها
EP3621615B1 (en) 2017-05-12 2023-11-15 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US10246439B2 (en) 2017-05-25 2019-04-02 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2018218042A1 (en) 2017-05-25 2018-11-29 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US10450301B2 (en) 2017-05-25 2019-10-22 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
GB201711234D0 (en) * 2017-07-12 2017-08-23 Galapagos Nv Pyrrolopyrimidine and pyrrolopyridine derivatives
CN107556318B (zh) * 2017-08-22 2020-08-11 山东大学 一种含哌啶的吡咯并嘧啶类化合物及其制备方法与应用
WO2019046186A1 (en) 2017-08-28 2019-03-07 Enanta Pharmaceuticals, Inc. INHIBITORS OF KINASE 1 REGULATING THE APOPTOTIC SIGNAL CONTAINING TETRAZOLES AND METHODS OF USE THEREOF
EP3735404B1 (en) 2018-01-02 2023-11-29 Seal Rock Therapeutics, Inc. Ask1 inhibitor compounds and uses thereof
WO2019163956A1 (ja) 2018-02-26 2019-08-29 エーザイ・アール・アンド・ディー・マネジメント株式会社 ピラゾロ［１，５－ａ］ピリミジン化合物の塩およびその結晶
MX2020011225A (es) 2018-05-02 2021-01-20 Enanta Pharm Inc Tetrazol que contiene inhibidores de la cinasa 1 reguladora de la señal de apoptosis y métodos de uso de los mismos.
WO2019213239A1 (en) 2018-05-02 2019-11-07 Enanta Pharmaceuticals Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
JPWO2020017569A1 (ja) * 2018-07-17 2021-12-02 日本ケミファ株式会社 Ｔ型カルシウムチャネル阻害剤
US10968199B2 (en) 2018-08-22 2021-04-06 Enanta Pharmaceuticals, Inc. Cycloalkyl-containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US11345699B2 (en) 2018-11-19 2022-05-31 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2020198214A1 (en) 2019-03-25 2020-10-01 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
CA3135344A1 (en) * 2019-03-29 2020-10-08 Nippon Chemiphar Co., Ltd. Use of t-type calcium channel blocker for treating pruritus
JP2022081710A (ja) * 2019-03-29 2022-06-01 ユーティアイ リミテッド パートナーシップ 関節リウマチを治療するためのｔ型カルシウムチャネル阻害剤の使用
CN111303155A (zh) * 2020-03-13 2020-06-19 深圳大学 靶向pak1抑制剂及其在抗肿瘤治疗药物中的应用
CN117285520A (zh) * 2022-06-24 2023-12-26 上海科技大学 甲酰胺类衍生物的医药用途、甲酰胺类衍生物、包含其的药物组合物

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR970009225B1 (ko) 1989-09-19 1997-06-09 데이진 가부시끼가이샤 피롤로[2,3-디] 피리미딘 유도체, 그의 제조방법 및 그것을 유효성분으로 하는 의약제제
DZ2805A1 (fr) 1998-06-02 2005-01-30 Cadus Pharmaceutical Corp Composition à pyrroloÄ2,,3dÜ pyrimidine et leurs usages.
US6878716B1 (en) 1998-06-02 2005-04-12 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptor and uses thereof
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
JP2003512466A (ja) * 1999-10-25 2003-04-02 アルタナ ファルマ アクチエンゲゼルシャフト Ｐｄｅ４インヒビターとしてのテトラヒドロチオピランフタラジノン誘導体
US7160890B2 (en) 1999-12-02 2007-01-09 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A3 receptor and uses thereof
US6680322B2 (en) 1999-12-02 2004-01-20 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptors and uses thereof
AU784878B2 (en) 1999-12-02 2006-07-13 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 A2A and A3 receptors and uses thereof
JP2005515173A (ja) 2001-10-31 2005-05-26 バイエル・ヘルスケア・アクチェンゲゼルシャフト ピリミド［４，５−ｂ］インドール誘導体
US20040138238A1 (en) 2002-08-08 2004-07-15 Dhanoa Dale S. Substituted aminopyrimidine compounds as neurokinin antagonists
EP1582586A4 (en) 2002-11-22 2007-03-14 Takeda Pharmaceutical APOPTOSIS ASSOCIATED PROTEIN AND ITS USE
WO2005117909A2 (en) 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods of use
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
DK3719018T3 (da) * 2006-04-25 2025-09-29 Astex Therapeutics Ltd Purin og deazapurinderivater som farmaceutiske forbindelser
EP2037931A2 (en) 2006-04-25 2009-03-25 Astex Therapeutics Limited Pharmaceutical combinations of pk inhibitors and other active agents
US20100016340A1 (en) 2006-04-25 2010-01-21 Astex Therapeutics Limited Pharmaceutical compounds
WO2008012635A2 (en) 2006-07-26 2008-01-31 Pfizer Products Inc. Amine derivatives useful as anticancer agents
WO2008016131A1 (en) 2006-08-04 2008-02-07 Takeda Pharmaceutical Company Limited Fused heterocyclic compound
EP2129660A2 (en) * 2006-12-19 2009-12-09 Pfizer Products Inc. Nicotinamide derivatives as inhibitors of h-pgds and their use for treating prostaglandin d2 mediated diseases
AR064416A1 (es) 2006-12-21 2009-04-01 Cancer Rec Tech Ltd Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas.
AR064415A1 (es) 2006-12-21 2009-04-01 Cancer Rec Tech Ltd Derivados de pirrolo-piperidinas y purinas,composiciones farmaceuticas que los contienen y usos en trastornos y/o enfermedades mediadas por pka y pkb.
EP2132196A1 (en) * 2007-02-26 2009-12-16 Pfizer Products Inc. Nicotinamide derivatives as inhibitors of h-pgds and their use for treating prostaglandin d2 mediated diseases
WO2008117796A1 (ja) 2007-03-28 2008-10-02 Dainippon Sumitomo Pharma Co., Ltd. 新規ムチリン誘導体
AU2008291075A1 (en) 2007-08-31 2009-03-05 Merck Serono S.A. Triazolopyridine compounds and their use as ask inhibitors
BRPI0818533B8 (pt) 2007-10-11 2021-05-25 Astrazeneca Ab composto, composição farmacêutica, uso de um composto, e, processo para a preparação de um composto
JP5432982B2 (ja) 2008-03-31 2014-03-05 武田薬品工業株式会社 アポトーシスシグナル調節キナーゼ１阻害剤
WO2009131940A1 (en) 2008-04-21 2009-10-29 Lexicon Pharmaceuticals, Inc. Limk2 inhibitors, compositions comprising them, and methods of their use
WO2010008843A1 (en) 2008-06-24 2010-01-21 Takeda Pharmaceutical Company Limited Apoptosis signal-regulating kinase 1 inhibitors
CN102143746A (zh) 2008-07-03 2011-08-03 埃克塞利希斯股份有限公司 Cdk 调节剂
CA2734305A1 (en) 2008-08-15 2010-02-18 Board Of Regents, The University Of Texas System 1,4-benzoxazine compounds and derivatives thereof as therapeutic drugs for the treatment of neurodegenerative conditions
BRPI1004899B8 (pt) 2009-01-08 2021-05-25 Curis Inc composto inibidor de fosfoinositida 3-quinase, composição farmacêutica e uso de um composto
WO2010121243A1 (en) 2009-04-17 2010-10-21 University Of Arizona Compounds, pharmaceutical compositions and methods of use of 2-aryl pyridylazoles
US9346809B2 (en) 2009-07-08 2016-05-24 Leo Pharma A/S Heterocyclic compounds as JAK receptor and protein tyrosine kinase inhibitors
TWI625121B (zh) 2009-07-13 2018-06-01 基利科學股份有限公司 調節細胞凋亡信號之激酶的抑制劑
TWI466885B (zh) 2009-07-31 2015-01-01 Japan Tobacco Inc 含氮螺環化合物及其醫藥用途
WO2011029043A1 (en) 2009-09-04 2011-03-10 Biogen Idec Ma Inc. Heteroaryl btk inhibitors
WO2011041293A1 (en) 2009-09-30 2011-04-07 Takeda Pharmaceutical Company Limited Pyrazolo [1, 5-a] pyrimidine derivatives as apoptosis signal-regulating kinase 1 inhibitors
HRP20140114T1 (hr) 2010-02-03 2014-03-14 Takeda Pharmaceutical Company Limited Inhibitori kinaze 1 koji reguliraju signal apoptoze
US9260417B2 (en) 2010-02-08 2016-02-16 Amitech Therapeutic Solutions, Inc. Therapeutic methods and compositions involving allosteric kinase inhibition
CA2794086A1 (en) 2010-03-24 2011-09-29 Amitech Therapeutic Solutions, Inc. Heterocyclic compounds useful for kinase inhibition
KR101759759B1 (ko) 2010-07-02 2017-07-19 길리애드 사이언시즈, 인코포레이티드 세포자멸사 신호-조절 키나아제 저해제
JP5525612B2 (ja) 2010-07-23 2014-06-18 国立大学法人 東京大学 含窒素複素環誘導体
WO2012022045A1 (en) 2010-08-20 2012-02-23 Hutchison Medipharma Limited Pyrrolopyrimidine compounds and uses thereof
US9346810B2 (en) 2010-08-20 2016-05-24 Hutchison Medipharma Limited Pyrrolopyrimidine compounds and uses thereof
CN102372717B (zh) 2010-08-20 2014-06-18 和记黄埔医药（上海）有限公司 吡咯并嘧啶类化合物及其用途
EP2629777B1 (en) 2010-10-22 2018-12-19 Merck Sharp & Dohme Corp. Bicyclic diamines as janus kinase inhibitors
WO2012058645A1 (en) 2010-10-29 2012-05-03 Biogen Idec Ma Inc. Heterocyclic tyrosine kinase inhibitors
PL2651417T3 (pl) * 2010-12-16 2017-08-31 Calchan Limited Pochodne pirolopirymidyny hamujące ASK1
UY34573A (es) 2012-01-27 2013-06-28 Gilead Sciences Inc Inhibidor de la quinasa que regula la señal de la apoptosis
JP6189948B2 (ja) 2012-06-29 2017-08-30 ファイザー・インク ＬＲＲＫ２阻害薬としての新規な４−（置換アミノ）−７Ｈ−ピロロ［２，３−ｄ］ピリミジン
ES2889757T3 (es) 2012-09-06 2022-01-13 Plexxikon Inc Compuestos y procedimientos para la modulación de quinasas e indicaciones para estos
US10865216B2 (en) 2012-09-12 2020-12-15 Merck Sharp & Dohme Corp. Tricyclic Gyrase inhibitors
UY35212A (es) 2012-12-21 2014-06-30 Gilead Sciences Inc Inhibidores de la quinasa que regula la señal de la apoptosis

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