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1.发明申请公开(公告)号：US20180015106A1
公开(公告)日：2018-01-18
申请号：US15715446
申请日：2017-09-26
发明人： Zhiqiang Yang , Guizhen Dong , Milana Maletic
IPC分类号： A61K31/60 , C07D405/14 , A61K45/06 , A61K31/444 , A61K31/4439 , A61K31/4365 , A61K31/4245 , C07D413/14 , A61K31/4155
CPC分类号： A61K31/60 , A61K31/4155 , A61K31/4245 , A61K31/4365 , A61K31/4439 , A61K31/444 , A61K45/06 , C07D405/14 , C07D413/14 , A61K2300/00
摘要： The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof wherein: R1 is W is and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ASC, secondary prevention of myocardial infarction or stroke, or PAD.
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2.发明申请SULFONAMIDE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG 有权磺酰胺衍生物及其用于改善药物药物动力学的方法公开(公告)号：US20150197531A1
公开(公告)日：2015-07-16
申请号：US14410846
申请日：2013-06-25
发明人： Craig A. Coburn , Milana Maletic , Richard Soll , Chunsing Li , Yunfu Luo , Zhiqi Qi
IPC分类号： C07D498/04 , A61K31/496 , C07D471/10 , C07D417/14 , A61K31/4402 , A61K31/4985 , A61K31/5383 , A61K31/5377 , A61K45/06 , A61K31/513 , C07D417/12 , C07D487/04
CPC分类号： C07D498/04 , A61K31/4402 , A61K31/496 , A61K31/4985 , A61K31/513 , A61K31/5377 , A61K31/5383 , A61K38/05 , A61K45/06 , C07D401/14 , C07D403/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D491/04
摘要： The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.
摘要翻译： 本发明涉及式（I）的磺酰胺衍生物及其药学上可接受的盐，其中A，W，X，R 1，R 2，R 3，R 4和R 5如本文所定义。 本发明还涉及包含至少一种磺酰胺衍生物的组合物，以及使用磺酰胺衍生物来改善药物的药代动力学的方法。
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公开(公告)号：US09018200B2
公开(公告)日：2015-04-28
申请号：US14351723
申请日：2012-10-18
发明人： Milana Maletic , Harold B. Wood , Wanying Sun
IPC分类号： C07D417/12 , C07D401/12 , C07D405/12 , C07D211/22 , C07D413/12
CPC分类号： C07D413/12 , C07D211/22 , C07D401/12 , C07D405/12 , C07D417/12
摘要： Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
摘要翻译： 公开了式（I）的取代的哌啶基化合物：用于治疗或预防2型糖尿病和类似病症。 也包括药学上可接受的盐。 该化合物可用作g-蛋白偶联受体GPR-119的激动剂。
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公开(公告)号：US10322140B2
公开(公告)日：2019-06-18
申请号：US15715446
申请日：2017-09-26
发明人： Zhiqiang Yang , Guizhen Dong , Milana Maletic
IPC分类号： C07D405/14 , C07D413/14 , A61K31/60 , A61K31/4439 , A61K45/06 , A61K31/4155 , A61K31/4245 , A61K31/4365 , A61K31/444
摘要： The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof wherein: R1 is W is and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ASC, secondary prevention of myocardial infarction or stroke, or PAD.
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5.发明授权公开(公告)号：US09981969B2
公开(公告)日：2018-05-29
申请号：US14895406
申请日：2014-06-02
发明人： Craig A. Coburn , Milana Maletic , Yunfu Luo , Zhiqi Qi , Chunsing Li , Tingting Yu , Richard Soll
IPC分类号： C07D487/04 , C07D401/14 , C07D413/14 , A61K31/4985 , A61K31/5365 , C07D401/06 , C07D471/04 , C07D498/04 , A61K45/06 , A61K31/4375 , A61K31/4545 , A61K31/513 , A61K31/55 , C07D405/14 , A61K31/454 , A61K31/496 , A61K31/5383 , A61K31/551
CPC分类号： C07D487/04 , A61K31/4375 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K31/513 , A61K31/5365 , A61K31/5383 , A61K31/55 , A61K31/551 , A61K45/06 , C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14 , C07D471/04 , C07D498/04 , A61K2300/00
摘要： The present invention relates to Imidazole Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, B, Y, R1 and R2 are as defined herein. The present invention also relates to compositions comprising at least one Imidazole Derivative, and methods of using the Imidazole Derivatives for inhibiting CYP450 3A. Inhibition of CYP450 3A can be used to improve the pharmacokinetics of a drug that is metabolized by CYP450 3A4.
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公开(公告)号：US20170240539A1
公开(公告)日：2017-08-24
申请号：US15518804
申请日：2015-10-09
发明人： Andrew W. Stamford , Zhi-Qiang Yang , Milana Maletic , Senlin Cai , Xiaobang Duan , Jianhua Cao
IPC分类号： C07D417/06 , C07D417/14
CPC分类号： C07D417/06 , C07D417/14
摘要： The present invention relates to cyclic sulfonamide derivatives of Formula (I) or a pharmaceutically acceptable salt thereof.
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7.发明申请SULFONAMIDE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG 审中-公开磺酰胺衍生物及其用于改善药物药物动力学的方法公开(公告)号：US20140005103A1
公开(公告)日：2014-01-02
申请号：US13926481
申请日：2013-06-25
发明人： Craig A. Coburn , Milana Maletic , Richard Soll , Chunsing Li , Yunfu Luo , Zhiqi Qi
IPC分类号： A61K31/496 , C07D471/10 , C07D471/04 , A61K31/4985 , A61K38/05 , A61K31/5383 , A61K31/5377 , C07D487/04 , A61K31/513 , C07D417/12 , C07D498/04
CPC分类号： C07D498/04 , A61K31/4402 , A61K31/496 , A61K31/4985 , A61K31/513 , A61K31/5377 , A61K31/5383 , A61K38/05 , A61K45/06 , C07D401/14 , C07D403/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D491/04
摘要： The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.
摘要翻译： 本发明涉及式（I）的磺酰胺衍生物及其药学上可接受的盐，其中A，W，X，R 1，R 2，R 3，R 4和R 5如本文所定义。 本发明还涉及包含至少一种磺酰胺衍生物的组合物，以及使用磺酰胺衍生物来改善药物的药代动力学的方法。
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8.发明申请PREPARATION AND USE OF 7A-HETEROCYCLE SUBSTITUTED- 6,6-DIFLUORO BICYCLIC HIMBACINE DERIVATIVES AS PAR-1 RECEPTOR ANTAGONISTS 审中-公开作为PAR-1受体拮抗剂的7-取代的6,6-二氟基双环衍生物的制备和使用公开(公告)号：US20160200715A1
公开(公告)日：2016-07-14
申请号：US14912212
申请日：2014-08-18
发明人： Zhiqiang Yang , Guizhen Dong , Milana Maletic
IPC分类号： C07D413/14 , A61K31/444 , C07D405/14 , A61K31/4439 , A61K45/06
CPC分类号： A61K31/60 , A61K31/4155 , A61K31/4245 , A61K31/4365 , A61K31/4439 , A61K31/444 , A61K45/06 , C07D405/14 , C07D413/14 , A61K2300/00
摘要： The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof wherein: R1 is W is and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ASC, secondary prevention of myocardial infarction or stroke, or PAD.
摘要翻译： 本发明涉及下式的双环烟肼衍生物或其药学上可接受的盐，其中：R1是W，其余变量在本文中描述。 本发明的化合物是PAR-1受体的有效抑制剂。 本发明化合物可用于治疗或预防疾病状态如ASC，二次预防心肌梗塞或中风或PAD。
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9.发明申请PREPARATION AND USE OF 3-PYRIDYL SUBSTITUTED- 6,6-DIFLUORO BICYCLIC HIMBACINE DERIVATIVES AS PAR-1 RECEPTOR ANTAGONISTS 有权作为PAR-1受体拮抗剂的3-吡啶基取代的6,6-二氟双环衍生物衍生物的制备和使用公开(公告)号：US20160200713A1
公开(公告)日：2016-07-14
申请号：US14912315
申请日：2014-08-18
IPC分类号： C07D405/14 , A61K45/06 , C07D409/14 , A61K31/444
CPC分类号： A61K31/60 , A61K31/343 , A61K31/4365 , A61K31/444 , A61K45/06 , C07D405/14 , C07D409/04 , C07D409/14 , A61K2300/00
摘要： The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof wherein: R1 is halo; —CN; alkyl; cycloalkyl; alkoxy; phenyl, which is optionally substituted one or twice independently by alkyl, halo, or —CN; or a thiophene ring, which is optionally substituted once or twice independently by alkyl. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ASC, secondary prevention of myocardial infarction or stroke, or PAD.
摘要翻译： 本发明涉及下式的双环吗巴肼衍生物或其药学上可接受的盐，其中：R1是卤素; -CN; 烷基; 环烷基 烷氧基 苯基，其任选被烷基，卤素或-CN独立地取代一次或两次; 或噻吩环，其任选被烷基独立地取代一次或两次。 本发明的化合物是PAR-1受体的有效抑制剂。 本发明化合物可用于治疗或预防疾病状态如ASC，二次预防心肌梗塞或中风或PAD。
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10.发明申请PREPARATION AND USE OF 7A-AMIDE SUBSTITUTED- 6,6-DIFLUORO BICYCLIC HIMBACINE DERIVATIVES AS PAR-1 RECEPTOR ANTAGONISTS 有权作为PAR-1受体拮抗剂的7A-酰胺取代-6,6-二氟双环衍生物衍生物的制备和使用公开(公告)号：US20160185764A1
公开(公告)日：2016-06-30
申请号：US14912233
申请日：2014-08-18
IPC分类号： C07D405/14 , A61K31/444 , A61K45/06 , C07D405/06 , A61K31/443
CPC分类号： C07D405/14 , A61K31/4365 , A61K31/443 , A61K31/444 , A61K31/616 , A61K45/06 , C07D405/06 , A61K2300/00
摘要： The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof wherein: R1 is —[C(Ra)(Rb)]x—[C(Rb)(Rb)]y—C(O)NH2, or —N(H)—[(CH2)]z—C(O)—NH2, W is and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ASC, secondary prevention of myocardial infarction or stroke, or PAD.
摘要翻译： 本发明涉及下式的双环和啶衍生物或其药学上可接受的盐，其中：R 1是 - [C（R a）（R b）] x- [C（R b）（R b）] y -C（O） 或-N（H） - [（CH 2）] z -C（O）-NH 2，W和其余变量在本文中描述。 本发明的化合物是PAR-1受体的有效抑制剂。 本发明化合物可用于治疗或预防疾病状态如ASC，二次预防心肌梗塞或中风或PAD。
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