CN110072857A - 作为造血前列腺素d合酶抑制剂的1,3-二取代的环丁酮或氮杂环丁烷衍生物 - Google Patents

作为造血前列腺素d合酶抑制剂的1,3-二取代的环丁酮或氮杂环丁烷衍生物 Download PDF

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CN110072857A
CN110072857A CN201780075127.1A CN201780075127A CN110072857A CN 110072857 A CN110072857 A CN 110072857A CN 201780075127 A CN201780075127 A CN 201780075127A CN 110072857 A CN110072857 A CN 110072857A
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trans
thiazol
yloxy
cyclobutanecarboxamide
substituted
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Chinese (zh)
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D.N.迪顿
Y.郭
A.P.汉考克
C.舒尔特
B.G.希勒
E.D.史密斯
E.L.斯图尔特
S.A.汤姆森
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GlaxoSmithKline Intellectual Property Development Ltd
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GlaxoSmithKline Intellectual Property Development Ltd
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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CN201780075127.1A 2016-10-13 2017-10-12 作为造血前列腺素d合酶抑制剂的1,3-二取代的环丁酮或氮杂环丁烷衍生物 Pending CN110072857A (zh)

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US201662407634P 2016-10-13 2016-10-13
US62/407,634 2016-10-13
PCT/IB2017/056320 WO2018069863A1 (en) 2016-10-13 2017-10-12 1,3 di-substituted cyclobutane or azetidine derivatives as hematopoietic prostaglandin d synthase inhibitors

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CN111549000A (zh) * 2020-06-18 2020-08-18 中国医学科学院整形外科医院 一种过表达Hpgds的重组脂肪干细胞、制备方法及其应用
CN113582880A (zh) * 2020-04-30 2021-11-02 南京药石科技股份有限公司 一种(3-氨基二环[1.1.1]戊烷-1-基)氨基甲酸叔丁酯的制备方法
CN114085167A (zh) * 2021-12-13 2022-02-25 华中药业股份有限公司 一种杂质ts-3a的制备方法
CN115916776A (zh) * 2020-06-09 2023-04-04 艾尼莫生物科技公司 胶原蛋白1翻译抑制剂及其使用方法

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JOP20190072A1 (ar) 2016-10-13 2019-04-07 Glaxosmithkline Ip Dev Ltd مشتقات 1، 3 سيكلوبوتان ثنائي الاستبدال أو آزيتيدين كمثبطات للإنزيم المخلق للبروستاجلاندين d المكون للدم
EP3638672A1 (en) * 2017-06-13 2020-04-22 GlaxoSmithKline Intellectual Property Development Limited Chemical compounds as h-pgds inhibitors
CA3071024A1 (en) 2017-08-09 2019-02-14 Denali Therapeutics Inc. Compounds, compositions and methods
CN111201245B (zh) 2017-09-01 2024-04-05 戴纳立制药公司 化合物、组合物和方法
EP3924341A4 (en) 2019-02-13 2022-11-02 Denali Therapeutics Inc. Compounds, compositions and methods
SG11202108552QA (en) 2019-02-13 2021-09-29 Denali Therapeutics Inc Compounds, compositions and methods
WO2021152113A1 (en) 2020-01-31 2021-08-05 Bayer Aktiengesellschaft Substituted 2,3-benzodiazepines derivatives
WO2021207310A1 (en) 2020-04-08 2021-10-14 Agios Pharmaceuticals, Inc. Menin inhibitors and methods of use for treating cancer
CN111574473A (zh) * 2020-06-04 2020-08-25 宁夏农林科学院农业资源与环境研究所(宁夏土壤与植物营养重点实验室) 一种氨基噻唑类化合物的合成方法
WO2021256569A1 (ja) 2020-06-19 2021-12-23 佐藤製薬株式会社 H-pgdsを阻害する縮環化合物
CA3240926A1 (en) 2021-12-17 2023-06-22 Sato Pharmaceutical Co., Ltd. Azaindole derivative inhibiting h-pgds
EP4448492B1 (en) 2021-12-17 2026-03-04 Reglagene, Inc. Compositions and methods of making and using small molecules in the treatment of cancer
US20250250265A1 (en) * 2022-04-15 2025-08-07 Vanderbilt University Benzothiazole-phenylsulfonyl-piperidine analogs as activators of nacylphosphatidylethanolamine hydrolyzing phospholipase d
US12215102B2 (en) 2023-02-28 2025-02-04 Reglagene, Inc. Compositions and methods for making and using small molecules for tubulin-targeted therapy in the treatment of cancers and related conditions

Citations (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4031221A (en) * 1974-06-17 1977-06-21 American Hoechst Corporation Method of treating pain and hypertension
WO1999037614A1 (en) * 1998-01-23 1999-07-29 Vernalis Research Limited Azetidinecarboxamide derivatives for the treatment of cns disorders
WO2005105779A1 (en) * 2004-04-28 2005-11-10 Pfizer Limited 3-heterocyclyl-4-phenyl-triazole derivatives as inhibitors of the vasopressin v1a receptor
WO2006077496A1 (en) * 2005-01-20 2006-07-27 Pfizer Limited Substituted triazole derivatives as oxytocin antagonists
WO2007106705A1 (en) * 2006-03-10 2007-09-20 Boehringer Ingelheim International Gmbh Soluble epoxide hydrolase inhibitors and methods of using same
US20080146569A1 (en) * 2006-12-19 2008-06-19 Blake Tanisha D Nicotinamide Derivatives
WO2009109743A1 (en) * 2008-03-04 2009-09-11 Vernalis (R&D) Ltd. Azetidine derivatives
WO2011143495A1 (en) * 2010-05-13 2011-11-17 Amgen Inc. Heteroaryloxyheterocyclyl compounds as pde10 inhibitors
WO2012009649A1 (en) * 2010-07-16 2012-01-19 Anderson Gaweco Mif inhibitors and their uses
WO2012035023A1 (en) * 2010-09-13 2012-03-22 Novartis Ag Triazine-oxadiazoles
WO2012142498A2 (en) * 2011-04-13 2012-10-18 Innovimmune Biotherapeutics, Inc. Mif inhibitors and their uses
WO2013074387A1 (en) * 2011-11-14 2013-05-23 Merck Sharp & Dohme Corp. Imidazole derivatives
US20150038483A1 (en) * 2012-03-27 2015-02-05 Shionogi & Co., Ltd. Aromatic 5-membered heterocyclic derivative having trpv4-inhibiting activity
EP2857404A1 (en) * 2012-06-04 2015-04-08 Daiichi Sankyo Co., Ltd. IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVE AS KINASE INHIBITOR
CN105764900A (zh) * 2014-09-13 2016-07-13 广东东阳光药业有限公司 Crth2拮抗剂化合物及其用途
WO2016156816A1 (en) * 2015-03-30 2016-10-06 Mission Therapeutics Limited 1-cyano-pyrrolidine compounds as usp30 inhibitors

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4956359A (en) 1985-02-28 1990-09-11 A. H. Robins Company, Inc. 3-aryloxy and 3-arylthioazetidinecarboxamides as anticonvulsants and antiepileptics
IE58943B1 (en) 1985-02-28 1993-12-01 Robins Co Inc A H 3-Aryloxy-azetidine-carboxamides
US6809088B2 (en) * 1997-03-24 2004-10-26 Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them
GB9917385D0 (en) 1999-07-23 1999-09-22 Cerebrus Ltd Chemical compounds-I
US6576265B1 (en) 1999-12-22 2003-06-10 Acell, Inc. Tissue regenerative composition, method of making, and method of use thereof
EP1217000A1 (en) 2000-12-23 2002-06-26 Aventis Pharma Deutschland GmbH Inhibitors of factor Xa and factor VIIa
JP2007522233A (ja) * 2004-02-11 2007-08-09 アムジエン・インコーポレーテツド バニロイド受容体リガンド及び治療におけるそれらの使用
WO2005094805A1 (ja) 2004-04-01 2005-10-13 Institute Of Medicinal Molecular Design. Inc. イミン誘導体及びアミド誘導体
WO2007003961A2 (en) 2005-06-30 2007-01-11 Prosidion Limited Gpcr agonists
GB0514017D0 (en) * 2005-07-07 2005-08-17 Ionix Pharmaceuticals Ltd Chemical compounds
TW200720255A (en) 2005-07-13 2007-06-01 Taiho Pharmaceutical Co Ltd Benzoimidazole compound capable of inhibiting prostaglandin d synthetase
JP2007051121A (ja) 2005-07-22 2007-03-01 Taiho Yakuhin Kogyo Kk プロスタグランジンd合成酵素を阻害するピリミジン化合物
PE20110118A1 (es) 2005-10-04 2011-03-08 Aventis Pharma Inc Compuestos de pirimidina amida como inhibidores de pgds
US20070208426A1 (en) * 2006-03-03 2007-09-06 Sdgi Holdings, Inc. Spinal implant with improved surface properties for delivery
US20110172230A1 (en) 2006-08-23 2011-07-14 Takahiro Ishii Urea compound or salt thereof
DK2142516T3 (da) 2007-03-30 2013-04-15 Sanofi Sa Pyrimidinhydrazidforbindelser i ders egenskab af pgds-inhibitorer
GB0706793D0 (en) 2007-04-05 2007-05-16 Evotec Ag Compounds
CA2725481A1 (en) 2008-06-18 2009-12-23 Pfizer Limited Nicotinamide derivatives
TW201010997A (en) 2008-06-18 2010-03-16 Pfizer Ltd Nicotinamide derivatives
WO2010024903A1 (en) * 2008-08-29 2010-03-04 Yangbo Feng BENZO[d]OXAZOLES AND BENZO[d]THIAZOLES AS KINASE INHIBITORS
US8536185B2 (en) 2008-09-22 2013-09-17 Cayman Chemical Company, Incorporated Multiheteroaryl compounds as inhibitors of H-PGDS and their use for treating prostaglandin D2 mediated diseases
RU2496778C2 (ru) 2009-03-09 2013-10-27 Тайхо Фармасьютикал Ко., Лтд. Пиперазиновое соединение, ингибирующее простагландин-d-синтазу
JPWO2011043359A1 (ja) 2009-10-06 2013-03-04 協和発酵キリン株式会社 芳香族複素環化合物を含有する医薬
CN107875155A (zh) 2009-10-08 2018-04-06 赛诺菲 苯基噁二唑衍生物在制备治疗变应性或炎性疾病的药物中的用途
EP2527340B1 (en) 2010-01-22 2016-08-17 Taiho Pharmaceutical Co., Ltd. Piperazine compound having a pgds inhibitory effect
AU2011253058A1 (en) * 2010-05-13 2012-12-06 Amgen Inc. Heteroaryloxycarbocyclyl compounds as PDE10 inhibitors
KR101400192B1 (ko) 2010-12-31 2014-05-27 제일모직 주식회사 포지티브형 감광성 수지 조성물, 이를 사용하여 제조된 감광성 수지막 및 상기 감광성 수지막을 포함하는 반도체 소자
CN103702961A (zh) 2011-05-23 2014-04-02 赛诺菲 含有n-烷基的氘代化合物的制备方法
WO2014127350A1 (en) 2013-02-18 2014-08-21 The Scripps Research Institute Modulators of vasopressin receptors with therapeutic potential
WO2014179144A1 (en) 2013-04-29 2014-11-06 E. I. Du Pont De Nemours And Company Fungicidal heterocyclic compounds
ES2842592T3 (es) 2014-05-19 2021-07-14 Boehringer Ingelheim Animal Health Usa Inc Compuestos antihelmínticos
CN108430992A (zh) 2015-12-17 2018-08-21 阿斯特克斯医疗公司 作为h-pgds抑制剂的喹啉-3-甲酰胺
JOP20190072A1 (ar) 2016-10-13 2019-04-07 Glaxosmithkline Ip Dev Ltd مشتقات 1، 3 سيكلوبوتان ثنائي الاستبدال أو آزيتيدين كمثبطات للإنزيم المخلق للبروستاجلاندين d المكون للدم

Patent Citations (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4031221A (en) * 1974-06-17 1977-06-21 American Hoechst Corporation Method of treating pain and hypertension
WO1999037614A1 (en) * 1998-01-23 1999-07-29 Vernalis Research Limited Azetidinecarboxamide derivatives for the treatment of cns disorders
WO2005105779A1 (en) * 2004-04-28 2005-11-10 Pfizer Limited 3-heterocyclyl-4-phenyl-triazole derivatives as inhibitors of the vasopressin v1a receptor
WO2006077496A1 (en) * 2005-01-20 2006-07-27 Pfizer Limited Substituted triazole derivatives as oxytocin antagonists
WO2007106705A1 (en) * 2006-03-10 2007-09-20 Boehringer Ingelheim International Gmbh Soluble epoxide hydrolase inhibitors and methods of using same
US20080146569A1 (en) * 2006-12-19 2008-06-19 Blake Tanisha D Nicotinamide Derivatives
WO2009109743A1 (en) * 2008-03-04 2009-09-11 Vernalis (R&D) Ltd. Azetidine derivatives
WO2011143495A1 (en) * 2010-05-13 2011-11-17 Amgen Inc. Heteroaryloxyheterocyclyl compounds as pde10 inhibitors
WO2012009649A1 (en) * 2010-07-16 2012-01-19 Anderson Gaweco Mif inhibitors and their uses
WO2012035023A1 (en) * 2010-09-13 2012-03-22 Novartis Ag Triazine-oxadiazoles
WO2012142498A2 (en) * 2011-04-13 2012-10-18 Innovimmune Biotherapeutics, Inc. Mif inhibitors and their uses
WO2013074387A1 (en) * 2011-11-14 2013-05-23 Merck Sharp & Dohme Corp. Imidazole derivatives
US20150038483A1 (en) * 2012-03-27 2015-02-05 Shionogi & Co., Ltd. Aromatic 5-membered heterocyclic derivative having trpv4-inhibiting activity
EP2857404A1 (en) * 2012-06-04 2015-04-08 Daiichi Sankyo Co., Ltd. IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVE AS KINASE INHIBITOR
CN105764900A (zh) * 2014-09-13 2016-07-13 广东东阳光药业有限公司 Crth2拮抗剂化合物及其用途
WO2016156816A1 (en) * 2015-03-30 2016-10-06 Mission Therapeutics Limited 1-cyano-pyrrolidine compounds as usp30 inhibitors

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
ALAN BROWN等: "Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》 *
JEVGEŅIJA LUGIŅINA等: "Ring-Opening of Carbamate-Protected Aziridines and Azetidines in Liquid Sulfur Dioxide", 《EUR. J. ORG. CHEM.》 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113582880A (zh) * 2020-04-30 2021-11-02 南京药石科技股份有限公司 一种(3-氨基二环[1.1.1]戊烷-1-基)氨基甲酸叔丁酯的制备方法
CN113582880B (zh) * 2020-04-30 2023-11-17 南京药石科技股份有限公司 一种(3-氨基二环[1.1.1]戊烷-1-基)氨基甲酸叔丁酯的制备方法
CN115916776A (zh) * 2020-06-09 2023-04-04 艾尼莫生物科技公司 胶原蛋白1翻译抑制剂及其使用方法
CN111549000A (zh) * 2020-06-18 2020-08-18 中国医学科学院整形外科医院 一种过表达Hpgds的重组脂肪干细胞、制备方法及其应用
CN111549000B (zh) * 2020-06-18 2022-07-29 中国医学科学院整形外科医院 一种过表达Hpgds的重组脂肪干细胞、制备方法及其应用
CN114085167A (zh) * 2021-12-13 2022-02-25 华中药业股份有限公司 一种杂质ts-3a的制备方法

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