CN104220429A - 非全身性tgr5激动剂 - Google Patents

非全身性tgr5激动剂 Download PDF

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Publication number
CN104220429A
CN104220429A CN201280069126.3A CN201280069126A CN104220429A CN 104220429 A CN104220429 A CN 104220429A CN 201280069126 A CN201280069126 A CN 201280069126A CN 104220429 A CN104220429 A CN 104220429A
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alkyl
group
carboxyl
carbalkoxy
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Chinese (zh)
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詹森·G·刘易斯
尼古拉斯·雷奇
陈涛
杰弗里·W·雅各布斯
多米尼克·沙尔莫
马克·纳夫雷亚
帕特丽夏·芬
克里斯多佛·卡雷拉斯
安德鲁·斯宾塞
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Ardelyx Inc
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Ardelyx Inc
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Publication of CN104220429A publication Critical patent/CN104220429A/zh
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Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106316975A (zh) * 2015-06-15 2017-01-11 山东轩竹医药科技有限公司 酰胺类化合物及其作为tgr5激动剂的应用
CN106397174A (zh) * 2016-08-24 2017-02-15 河北诚信有限责任公司 一种制备3,6‑二氯‑2‑甲氧基苯甲酸的方法
CN106543180A (zh) * 2016-10-28 2017-03-29 南京正大天晴制药有限公司 苯甲酸利格列汀晶型及其制备方法
CN108440455A (zh) * 2018-04-11 2018-08-24 上海馨远医药科技有限公司 一种3-氧杂环丁烷羧酸的制备方法
CN111763173A (zh) * 2020-07-14 2020-10-13 河南大学 苯乙基咪唑类衍生物及其用途
CN112794844A (zh) * 2019-11-13 2021-05-14 中国科学院上海药物研究所 酯类化合物及其制备方法和应用、酯类软药

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017042380A1 (en) 2015-09-11 2017-03-16 Universite De Lille 2 Droit Et Sante Novel 5-amino-2-thioimidazole compounds and their use
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US12084472B2 (en) 2015-12-18 2024-09-10 Ardelyx, Inc. Substituted 4-phenyl pyridine compounds as non-systemic TGR5 agonists
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US12186329B2 (en) 2018-08-23 2025-01-07 President And Fellows Of Harvard College Compositions and methods related to cholic acid 7-sulfate as a treatment for diabetes
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WO2021071837A1 (en) 2019-10-07 2021-04-15 Kallyope, Inc. Gpr119 agonists
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US20230101735A1 (en) 2020-01-22 2023-03-30 Jiangsu Hengrui Medicine Co., Ltd. Anti-trop-2 antidody-exatecan analog conjugate and medical use thereof
BR112022017039A2 (pt) 2020-02-28 2022-11-16 Kallyope Inc Agonistas de gpr40
JP2023519261A (ja) 2020-03-25 2023-05-10 江蘇恒瑞医薬股▲ふん▼有限公司 抗ｐｓｍａ抗体－エキサテカン類似体複合体及びその医薬用途
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BR112023003328A2 (pt) 2020-08-24 2023-03-21 Hua Medicine Shanghai Ltd Preparação de composto acrilato substituído
CN114516839B (zh) * 2020-11-20 2024-08-27 湖南海利常德农药化工有限公司 吡唑醚类化合物及其制备方法与应用
WO2022208356A1 (en) 2021-03-31 2022-10-06 Fedora Pharmaceuticals Inc. Lactivicin compounds, their preparation and use as antibacterial agents
KR102600176B1 (ko) * 2021-10-18 2023-11-10 주식회사 사피엔스바이오 신규한 화합물 및 이를 포함하는 약학적 조성물

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101253147A (zh) * 2005-08-31 2008-08-27 诺瓦提斯公司 有机化合物
US20110178089A1 (en) * 2010-01-21 2011-07-21 Caterina Bissantz 4-phenoxy-nicotinamide or 4-phenoxy-pyrimidine-5-carboxamide compounds
CN102203065A (zh) * 2008-10-29 2011-09-28 霍夫曼-拉罗奇有限公司 新的苯基酰胺或吡啶基酰胺衍生物和它们作为gpbar1激动剂的应用

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050228016A1 (en) * 2002-06-13 2005-10-13 Enrique Michelotti Tetrahydroquinolines for modulating the expression of exogenous genes via an ecdysone receptor complex

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101253147A (zh) * 2005-08-31 2008-08-27 诺瓦提斯公司 有机化合物
CN102203065A (zh) * 2008-10-29 2011-09-28 霍夫曼-拉罗奇有限公司 新的苯基酰胺或吡啶基酰胺衍生物和它们作为gpbar1激动剂的应用
US20110178089A1 (en) * 2010-01-21 2011-07-21 Caterina Bissantz 4-phenoxy-nicotinamide or 4-phenoxy-pyrimidine-5-carboxamide compounds

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106316975A (zh) * 2015-06-15 2017-01-11 山东轩竹医药科技有限公司 酰胺类化合物及其作为tgr5激动剂的应用
CN106397174A (zh) * 2016-08-24 2017-02-15 河北诚信有限责任公司 一种制备3,6‑二氯‑2‑甲氧基苯甲酸的方法
CN106397174B (zh) * 2016-08-24 2018-12-21 河北诚信集团有限公司 一种制备3,6-二氯-2-甲氧基苯甲酸的方法
CN106543180A (zh) * 2016-10-28 2017-03-29 南京正大天晴制药有限公司 苯甲酸利格列汀晶型及其制备方法
CN108440455A (zh) * 2018-04-11 2018-08-24 上海馨远医药科技有限公司 一种3-氧杂环丁烷羧酸的制备方法
CN112794844A (zh) * 2019-11-13 2021-05-14 中国科学院上海药物研究所 酯类化合物及其制备方法和应用、酯类软药
CN112794844B (zh) * 2019-11-13 2023-03-21 中国科学院上海药物研究所 酯类化合物及其制备方法和应用、酯类软药
CN111763173A (zh) * 2020-07-14 2020-10-13 河南大学 苯乙基咪唑类衍生物及其用途
CN111763173B (zh) * 2020-07-14 2022-11-01 河南大学 苯乙基咪唑类衍生物及其用途

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