JP7187037B2 - ｐ－タウを減少させ、認知機能を改善させるアロステリック副腎皮質刺激ホルモン放出因子受容体１（ＣＲＦＲ１）アンタゴニスト - Google Patents

ｐ－タウを減少させ、認知機能を改善させるアロステリック副腎皮質刺激ホルモン放出因子受容体１（ＣＲＦＲ１）アンタゴニスト Download PDF

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JP7187037B2
JP7187037B2 JP2019533307A JP2019533307A JP7187037B2 JP 7187037 B2 JP7187037 B2 JP 7187037B2 JP 2019533307 A JP2019533307 A JP 2019533307A JP 2019533307 A JP2019533307 A JP 2019533307A JP 7187037 B2 JP7187037 B2 JP 7187037B2
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モハマド・パルヴェーズ・アラム
ヴァーギーズ・ジョン
バーバラ・ヤゴジンスカ
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University of California San Diego UCSD
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JP2019533307A 2016-09-07 2017-09-06 ｐ－タウを減少させ、認知機能を改善させるアロステリック副腎皮質刺激ホルモン放出因子受容体１（ＣＲＦＲ１）アンタゴニスト Active JP7187037B2 (ja)

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PCT/US2017/050347 WO2018048953A1 (en) 2016-09-07 2017-09-06 Allosteric corticotropin-releasing factor receptor 1 (crfr1) antagonists that decrease p-tau and improve cognition

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CN113710147B (zh) 2019-04-15 2025-01-28 詹森药业有限公司 使用语音分析检测认知衰退的系统和方法
CN116832160A (zh) * 2023-03-15 2023-10-03 上海市宝山区吴淞中心医院 Aβ1-42在制备子痫前期治疗药物或诊断试剂盒中的用途
CN118121593B (zh) * 2024-02-26 2025-02-14 首都医科大学宣武医院 一种用于预防和/或治疗阿尔茨海默病的药物组合物及其用途

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009520019A (ja) 2005-12-20 2009-05-21 ファイザー・リミテッド ピリミジン誘導体

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB590706A (en) * 1945-02-27 1947-07-25 Frederick Robert Basford New pyrimidine compounds
TW574214B (en) * 1994-06-08 2004-02-01 Pfizer Corticotropin releasing factor antagonists
US6020492A (en) 1995-05-12 2000-02-01 Neurogen Corporation Deazapurine derivatives; a new class of CRF1 specific ligands
US6956047B1 (en) * 1995-06-06 2005-10-18 Pfizer Inc. Corticotropin releasing factor antagonists
US6403599B1 (en) * 1995-11-08 2002-06-11 Pfizer Inc Corticotropin releasing factor antagonists
AU738304B2 (en) 1995-10-13 2001-09-13 Neurogen Corporation Certain pyrrolopyridine derivatives; novel CRF 1 specific ligands
US5760225A (en) 1996-11-15 1998-06-02 Neurogen Corporation Certain pyrazole derivatives as corticotropin-releasing factor receptor CRF1 specific ligands
CA2275686C (en) 1996-12-18 2006-10-17 Neurogen Corporation Isoquinolinamine and phthalazinamine derivatives which interact with crf receptors
US6756367B2 (en) 1998-02-03 2004-06-29 Novartis Ag Benzo-oxadiazoles, -thiadiazoles and -1,4-diazines, pharmaceutical compositions containing them and a process for preparing them
GB9802251D0 (en) 1998-02-03 1998-04-01 Ciba Geigy Ag Organic compounds
US6472402B1 (en) 1998-04-02 2002-10-29 Neurogen Corporation Aminoalkyl substituted 5,6,7,8-Tetrahydro-9H-Pyridino [2,3-B]indole derivatives
AU4556999A (en) 1998-06-09 1999-12-30 Neurogen Corporation Pyrido[2,3-b]indolizine derivatives and aza analogues thereof; crf1 specific ligands
EP1175421A1 (en) 1999-04-30 2002-01-30 Neurogen Corporation 9H-PYRIMIDO[4,5-b]INDOLE DERIVATIVES: CRF1 SPECIFIC LIGANDS
US6387894B1 (en) * 1999-06-11 2002-05-14 Pfizer Inc. Use of CRF antagonists and renin-angiotensin system inhibitors
US6548509B2 (en) 1999-10-22 2003-04-15 Neurogen Corporation 3-aryl substituted pyrazolo[4,3-D]pyrimidine derivatives; corticotropin-releasing factor receptor (CRF1) specific ligands
HRP20020599A2 (en) * 2000-01-18 2004-08-31 Pfizer Prod Inc Corticotropin releasing factor antagonists
BRPI0409505A (pt) 2003-05-09 2006-04-18 Pharmacia & Upjohn Co Llc compostos como antagonistas do receptor crf1
EP1626965A1 (en) 2003-05-09 2006-02-22 Pharmacia & Upjohn Company LLC Pyrazinones as crf1 receptor antagonists for the treatment of cns disorders
CN1878773A (zh) 2003-09-05 2006-12-13 神经能质公司 作为crf1受体配位体的杂芳基稠合的吡啶,吡嗪及嘧啶
EP1718311A1 (en) * 2004-02-13 2006-11-08 Pfizer Products Incorporated Therapeutic combinations of atypical antipsychotics with corticotropin releasing factor antagonists
US20080015196A1 (en) 2004-04-16 2008-01-17 Neurogen Corporation Imidazopyrazines, Imidazopyridines, and Imidazopyrimidines as Crf1 Receptor Ligands
MY148521A (en) * 2005-01-10 2013-04-30 Arena Pharm Inc Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto
EP1834641A1 (en) 2006-03-16 2007-09-19 Sanofi-Aventis Use of CRF1 receptor antagonists for preparing a drug for treating metabolic syndrome and/or obesity and/or dyslipoproteinemia
JP5161226B2 (ja) 2006-09-20 2013-03-13 イーライ リリー アンド カンパニー Ｃｒｆ１受容体アンタゴニストとしてのチアゾールピラゾロピリミジン
TW200906825A (en) * 2007-05-30 2009-02-16 Scripps Research Inst Inhibitors of protein kinases
CA2683152A1 (en) 2007-06-11 2008-12-18 Miikana Therapeutics, Inc. Substituted pyrazole compounds
US20100249138A1 (en) 2007-09-14 2010-09-30 Koob George F Mpzp: a small molecule corticotropin-releasing factor type 1 receptor (crf1) antogonist
US20110301087A1 (en) 2008-11-04 2011-12-08 Mcbride Edward Crf1 receptor compounds
WO2013123426A1 (en) * 2012-02-18 2013-08-22 Buck Institute For Research On Aging Formulations and methods for the treatment or prophylaxis of pre-mci and/or pre-alzheimer's conditions
TWI557112B (zh) * 2012-03-05 2016-11-11 百靈佳殷格翰國際股份有限公司 β－分泌酶抑制劑
EP2970219B1 (en) * 2013-03-15 2019-02-27 Epizyme, Inc. Carm1 inhibitors and uses thereof
CA3155599A1 (en) 2014-01-21 2015-07-30 Neurocrine Biosciences, Inc. Crf1 receptor antagonists for the treatment of congenital adrenal hyperplasia

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009520019A (ja) 2005-12-20 2009-05-21 ファイザー・リミテッド ピリミジン誘導体

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
The Journal of Pharmacology and Experimental Therapeutics，2012年，Vol.341, No.2，pp.518-531

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CN109906222B (zh) 2023-08-01
KR102571296B1 (ko) 2023-08-28
EP3510029A4 (en) 2020-03-11
JP2019526639A (ja) 2019-09-19
KR20190057316A (ko) 2019-05-28

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