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1. 发明授权

US11267786B2 [3.3.1] bicyclo compounds as indoleamine 2,3-dioxygenase inhibitors 有权
公开(公告)号：US11267786B2
公开(公告)日：2022-03-08
申请号：US17057959
申请日：2019-05-28
申请人： Merck Sharp & Dohme Corp. , Shuwen He , Yongxin Han , Alexander Pasternak
发明人： Shuwen He , Yongxin Han , Alexander Pasternak
IPC分类号： C07D215/14 , A61K45/06
摘要： Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

2. 发明申请

US20200230117A1 NOVEL SUBSTITUTED IMIDAZOPYRIDINE COMPOUNDS AS INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND/OR TRYPTOPHAN-2,3-DIOXYGENASE 审中-公开
公开(公告)号：US20200230117A1
公开(公告)日：2020-07-23
申请号：US16088873
申请日：2017-04-24
申请人： Phillip M. COWLEY , Meredeth Ann MCGOWAN , Thomas J. BROWN , WISE Alan , Hua ZHOU , Yongxin HAN , Kun LIU , Qinglin PU , Hongjun ZHANG , IOMet Pharma Ltd.
发明人： Phillip M. Cowley , Meredeth Ann McGowan , Thomas J. Brown , Yongxin Han , Kun Liu , Qinglin Pu , Alan Wise , Hongjun Zhang , Hua Zhou
IPC分类号： A61K31/438 , C07D519/00
摘要： Disclosed herein are substituted imidazopyridine compounds of formula (I) which are inhibitors of indoleamine 2,3-dioxygenase (IDO) and/or tryptophan-2,3-dioxygenase (TDO) enzymes: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO- and/or TDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO- and/or TDO-associated disease or disorder.

3. 发明授权

US10450309B2 Aryl sulfonamides as BLT1 antagonists 有权
公开(公告)号：US10450309B2
公开(公告)日：2019-10-22
申请号：US15769079
申请日：2016-11-28
申请人： Merck Sharp & Dohme Corp. , Yongxin Han , Phieng Siliphaivanh , Kerrie Spencer , Satyanarayana Tummanapalli
发明人： Yongxin Han , Satyanarayana Tummanapalli , Phieng Siliphaivanh , Kerrie Spencer
IPC分类号： A61K31/35 , A61P3/10 , C07D311/22 , C07D311/58 , C07D405/14 , C07D417/14
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.

4. 发明申请

US20180291017A1 ARYL ACYLSULFONAMIDES AS BLT1 ANTAGONISTS 审中-公开
公开(公告)号：US20180291017A1
公开(公告)日：2018-10-11
申请号：US15768097
申请日：2016-11-28
申请人： Yongxin HAN , Phieng SILIPHAIVANH , Kerrie SPENCER , Satyanarayana TUMMANAPALLI , Merck Sharp & Dohme Corp.
发明人： Yongxin Han , Satyanarayana Tummanapalli , Phieng Siliphaivanh , Kerrie Spencer
IPC分类号： C07D417/14 , A61P3/10
CPC分类号： C07D417/14 , A61K9/2054 , A61P3/10
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.

5. 发明授权

US08685999B2 Beta carboline sulphonylurea derivatives as EP4 receptor antagonists 有权
标题翻译： β咔啉磺酰脲衍生物作为EP4受体拮抗剂
公开(公告)号：US08685999B2
公开(公告)日：2014-04-01
申请号：US13120786
申请日：2009-09-22
申请人： Carl Berthelette , Michael Boyd , Jason Burch , Claude Dufresne , Julie Farand , Yongxin Han , Claudio F. Sturino
发明人： Carl Berthelette , Michael Boyd , Jason Burch , Claude Dufresne , Julie Farand , Yongxin Han , Claudio F. Sturino
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D471/04
摘要： The invention is directed to β-carboline sulphonylurea derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, inflammation, osteoarthritis, and rheumatoid arthritis. Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明针对可用于治疗EP4介导的疾病或病症（例如急性和慢性疼痛，炎症，骨关节炎和类风湿性关节炎）的EP4受体拮抗剂的β-咔啉磺酰脲衍生物。还包括药物组合物和使用方法。

6. 发明申请

US20120202837A1 SPIROCYCLIC PIPERIDINE DERIVATIVES USEFUL AS RENIN INHIBITORS 审中-公开
标题翻译：作为瑞宁抑制剂有用的螺环哌啶衍生物
公开(公告)号：US20120202837A1
公开(公告)日：2012-08-09
申请号：US13501401
申请日：2010-10-12
申请人： Austin Chen , Reneé Aspiotis , Daniel McKay , Yongxin Han , Pierre-André Fournier
发明人： Austin Chen , Reneé Aspiotis , Daniel McKay , Yongxin Han , Pierre-André Fournier
IPC分类号： A61K31/438 , C07D491/20 , A61P9/12 , A61P9/00 , A61P27/02 , A61P27/06 , A61P25/22 , C07D491/107 , A61P9/04
CPC分类号： C07D491/107 , C07D491/20
摘要： Renin inhibitors which are spirocyclic piperidine derivatives, of formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof, wherein: n, for each instance in which it occurs, is independently 0, 1, or 2; W is a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring, A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a first five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to a second five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is —(C═O)—, —CH2— or ═CH—; U is a bond or —CH2-, or, when V iS ═CH—, U is —CH═; X is ═CH—, ═CF—, ═C(OR3)—, or —(C═O)—; and Y is ═CH—, ═CF—, ═N—, or, for the case when X is —(C═O)—, Y is —N(R3)—.
摘要翻译：作为式（I）的螺环哌啶衍生物，可用于治疗心血管疾病和肾功能不全的药物组合物或其立体异构体或其药学上可接受的盐或其立体异构体的药学上可接受的盐的肾素抑制剂，其中：对于其发生的每个实例，n独立地为0,1或2; W是五或六元饱和或不饱和的杂环或碳环单环，A是（i）五或六元饱和或不饱和的杂环或碳环单环或（ii）第一个五元或六元饱和或不饱和的杂环或碳环，其与第二个五元或六元饱和或不饱和的杂环或碳环稠合，V是 - （C = O） - ， - CH 2 - 或= CH-; U是键或-CH 2 - ，或当V iS = CH-时，U是-CH =; X是≡CH-，≡CF-，≡C（OR3） - 或 - （C = O） - ; 并且Y为≡CH-，≡CF-，≡N-，或者对于X为 - （C = O） - 的情况，Y为-N（R 3） - 。

7. 发明授权

US08168815B2 Fused aromatic PTP-1B inhibitors 有权
标题翻译：融合芳香族PTP-1B抑制剂
公开(公告)号：US08168815B2
公开(公告)日：2012-05-01
申请号：US12518899
申请日：2008-01-24
申请人： John Colucci , Marie-Claire Wilson , Yongxin Han , Claude Dufresne , Michel Belley , Cheuk K. Lau , Christopher Bayly
发明人： John Colucci , Marie-Claire Wilson , Yongxin Han , Claude Dufresne , Michel Belley , Cheuk K. Lau , Christopher Bayly
IPC分类号： C07D215/38
CPC分类号： C07F9/60 , A61K31/662 , A61K45/06 , C07F9/3808 , C07F9/3834 , Y02A50/395
摘要： The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
摘要翻译：本发明包括由下式表示的新一类化合物，它们是PTP-1B酶的抑制剂。本发明还包括药物组合物，其包括上述化合物（式I）和治疗或预防PTP-1B介导的疾病包括糖尿病的方法。

8. 发明申请

US20120035214A1 RENIN INHIBITORS 审中-公开
标题翻译：雷宁抑制剂
公开(公告)号：US20120035214A1
公开(公告)日：2012-02-09
申请号：US13262781
申请日：2010-04-01
申请人： Daniel J. McKay , Melissa Arbour , Renee Aspiotis , Austin Chen , Pierre-Andre Fournier , Michel Gallant , Yongxin Han , Helene Juteau , Patrick Lacombe , Sebastien Laliberte , Sophie Lauzon , Carmela Molinaro , Paul O'Shea , Yeeman Ramtohul , Daniel Simard , Dwight MacDonald , Bruce Mackay , Christophe Mellon , Krista Morley , Chit Tsui , Sarah Jennifer Dolman , Greg Hughes , Jacob Janey
发明人： Daniel J. McKay , Melissa Arbour , Renee Aspiotis , Austin Chen , Pierre-Andre Fournier , Michel Gallant , Yongxin Han , Helene Juteau , Patrick Lacombe , Sebastien Laliberte , Sophie Lauzon , Carmela Molinaro , Paul O'Shea , Yeeman Ramtohul , Daniel Simard , Dwight MacDonald , Bruce Mackay , Christophe Mellon , Krista Morley , Chit Tsui , Sarah Jennifer Dolman , Greg Hughes , Jacob Janey
IPC分类号： A61K31/451 , C07D401/04 , C07D401/10 , C07D211/26 , C07D211/28 , C07D401/12 , A61K31/4545 , A61K31/454 , A61P9/12 , A61P9/04 , A61P9/10 , A61P27/06 , A61P25/22 , A61P25/00 , A61P13/12 , C07D211/22
CPC分类号： C07D211/26 , C07D211/22 , C07D211/28 , C07D211/52 , C07D401/04 , C07D401/12 , C07D413/04 , C07D413/14
摘要： The present invention relates to biaryl piperidine-based renin inhibitor compounds, and their use in treating cardiovascular events and renal insufficiency.
摘要翻译：本发明涉及联芳基哌啶基肾素抑制剂化合物及其在治疗心血管事件和肾功能不全中的用途。

9. 发明申请

US20110275660A1 BETA CARBOLINE SULPHONYLUREA DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS 有权
标题翻译：作为EP4受体拮抗剂的碳酰胺磺酰胺衍生物
公开(公告)号：US20110275660A1
公开(公告)日：2011-11-10
申请号：US13120786
申请日：2009-09-22
申请人： Carl Berthelette , Michael Boyd , Jason Burch , Claude Dufresne , Julie Farand , Yongxin Han , Claudio F. Sturino
发明人： Carl Berthelette , Michael Boyd , Jason Burch , Claude Dufresne , Julie Farand , Yongxin Han , Claudio F. Sturino
IPC分类号： A61K31/437 , A61K31/444 , A61P9/10 , A61P25/00 , A61P19/06 , C07D471/04 , A61P29/00
CPC分类号： C07D471/04
摘要： The invention is directed to β-carboline sulphonylurea derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, inflammation, osteoarthritis, and rheumatoid arthritis. Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明针对可用于治疗EP4介导的疾病或病症（例如急性和慢性疼痛，炎症，骨关节炎和类风湿性关节炎）的EP4受体拮抗剂的β-咔啉磺酰脲衍生物。还包括药物组合物和使用方法。

10. 发明申请

US20100022477A1 FUSED AROMATIC PTP-1B INHIBITORS 有权
标题翻译： FUSED AROMATIC PTP-1B抑制剂
公开(公告)号：US20100022477A1
公开(公告)日：2010-01-28
申请号：US12518899
申请日：2008-01-24
申请人： John Colucci , Marie-Claire Wilson , Yongxin Han , Claude Dufresne , Michel Belley , Cheuk K. Lau , Christopher Bayly
发明人： John Colucci , Marie-Claire Wilson , Yongxin Han , Claude Dufresne , Michel Belley , Cheuk K. Lau , Christopher Bayly
IPC分类号： A61K31/675 , C07F9/22 , C07F9/28 , A61K31/66 , A61P7/12 , A61P35/04
CPC分类号： C07F9/60 , A61K31/662 , A61K45/06 , C07F9/3808 , C07F9/3834 , Y02A50/395
摘要： The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
摘要翻译：本发明包括由下式表示的新一类化合物，它们是PTP-1B酶的抑制剂。本发明还包括药物组合物，其包括上述化合物（式I）和治疗或预防PTP-1B介导的疾病包括糖尿病的方法。

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