公开(公告)号：US20120190701A1

公开(公告)日：2012-07-26

申请号：US13390465

申请日：2010-08-17

申请人： Austin Chih-Yu Chen ,  Sebastien Laliberte ,  Guillaume Larouche ,  Yongxin Han ,  Daniel McKay

发明人： Austin Chih-Yu Chen ,  Sebastien Laliberte ,  Guillaume Larouche ,  Yongxin Han ,  Daniel McKay

IPC分类号： A61K31/438 ,  C07D491/20 ,  A61K31/4709 ,  A61K31/4725 ,  A61P9/12 ,  A61P25/22 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P25/00 ,  A61P27/02 ,  A61P27/06 ,  C07D491/107 ,  A61P9/04

CPC分类号： A61K31/438 ,  C07D491/107 ,  C07D519/00

摘要： Renin inhibitors, which are spirocyclic piperidine amides, of structural formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency. wherein n, for each instance in which it occurs, is independently 0, 1, or 2; R1 is hydrogen, C1-6-alkyl or C3-6-cycloalkyl, wherein said C1-6-alkyl or C3-6-cycloalkyl group can be independently substituted with 1-3 halogens; A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to another five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is a bond or —(C═O)—, —CH(OH)—, —CH2—or ═CH—; U is a bond or —CH2-, or for the case 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： 作为结构式（I）的螺环哌啶酰胺的肾素抑制剂及其用于治疗心血管疾病和肾功能不全的药物组合物。 其中对于其发生的每个实例，n独立地为0,1或2; R 1是氢，C 1-6 - 烷基或C 3-6 - 环烷基，其中所述C 1-6 - 烷基或C 3-6 - 环烷基可以独立地被1-3个卤素取代; A是（i）五或六元饱和或不饱和杂环或碳环单环或（ii）五元或六元饱和或不饱和的杂环或碳环，其与另一个五元或六元饱和 或不饱和杂环或碳环，V是一个键或 - （C = O） - ， - CH（OH） - ， - CH 2 - 或= CH-; U是键或-CH 2 - ，或者当V是= CH-的情况下，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） - 。

公开(公告)号：US06699856B2

公开(公告)日：2004-03-02

申请号：US10202817

申请日：2002-07-25

申请人： Yongxin Han ,  Andre Giroux ,  Robert Zamboni ,  Daniel J. McKay ,  Christopher I. Bayly ,  Erich L. Grimm ,  John Colucci

发明人： Yongxin Han ,  Andre Giroux ,  Robert Zamboni ,  Daniel J. McKay ,  Christopher I. Bayly ,  Erich L. Grimm ,  John Colucci

IPC分类号： A61K314965

CPC分类号： C07D403/12 ,  C07D241/20 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters, N-oxides and hydrates thereof are disclosed. Pharmaceutical compositions and methods of use are also included. The compounds are active against the caspase-3 enzyme, and thus are useful to treat caspase-3 mediated diseases and conditions.

摘要翻译： 公开了由式I表示的化合物及其药学上可接受的盐，酯，N-氧化物和水合物。 还包括药物组合物和使用方法。 这些化合物对半胱天冬酶-3酶具有活性，因此可用于治疗半胱天冬酶-3介导的疾病和病症。

公开(公告)号：US20200247754A1

公开(公告)日：2020-08-06

申请号：US16341595

申请日：2017-10-09

申请人： Michael T. RUDD ,  Zhaoyang MENG ,  Jenny WAI ,  David Jonathan BENNETT ,  Edward J. BRNARDIC ,  Nigel J. LIVERTON ,  Shawn J. STACHEL ,  Yongxin HAN ,  Paul TEMPEST ,  Jiuxiang ZHU ,  Xuewang XU ,  Bin ZHU ,  Merck Sharp & Dohme Corp.

发明人： Michael T. Rudd ,  Zhaoyang Meng ,  Jenny Wai ,  David Jonathan Bennett ,  Edward J. Brnardic ,  Nigel J. Liverton ,  Shawn J. Stachel ,  Yongxin Han ,  Paul Tempest ,  Jiuxiang Zhu ,  Xuewang Xu ,  Bin Zhu

IPC分类号： C07D221/20 ,  C07D401/12 ,  C07D417/12 ,  C07D405/12 ,  C07D211/22 ,  C07D401/14 ,  C07D417/14

摘要： In its many embodiments, the present invention provides certain substituted aryl and heteroaryl ether compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

公开(公告)号：US10336733B2

公开(公告)日：2019-07-02

申请号：US15767371

申请日：2016-11-28

申请人： Merck Sharp & Dohme Corp. ,  Yongxin Han ,  Jongwon Lim ,  Satyanarayana Tummanapalli ,  Phieng Siliphaivanh ,  Kerrie Spencer

发明人： Yongxin Han ,  Jongwon Lim ,  Satyanarayana Tummanapalli ,  Phieng Siliphaivanh ,  Kerrie Spencer

IPC分类号： C07D417/06 ,  C07D413/06 ,  C07D311/22 ,  C07D405/06 ,  A61K31/353 ,  A61K9/20

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 steatoepatitis, metabolic syndrome, atherosclerosis, and cancer.

公开(公告)号：US20150045325A1

公开(公告)日：2015-02-12

申请号：US14525396

申请日：2014-10-28

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： C07F9/60 ,  C07F9/38

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。

公开(公告)号：US08158671B2

公开(公告)日：2012-04-17

申请号：US12527736

申请日：2008-02-22

申请人： Michael Boyd ,  John Colucci ,  Yongxin Han

发明人： Michael Boyd ,  John Colucci ,  Yongxin Han

IPC分类号： A61K31/404 ,  A61K31/437 ,  C07D209/08 ,  C07D487/04

CPC分类号： C07D209/08 ,  C07D209/42 ,  C07D403/12

摘要： The invention is directed to indole and indoline cyclopropyl amide derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.

摘要翻译： 本发明涉及吲哚和二氢吲哚环丙酰胺衍生物作为EP4受体拮抗剂，其可用于治疗EP4介导的疾病或病症，例如急性和慢性疼痛，骨关节炎，类风湿性关节炎和癌症。 还包括药物组合物和使用方法。

公开(公告)号：US08013159B2

公开(公告)日：2011-09-06

申请号：US11920275

申请日：2006-05-15

申请人： Michel Belley ,  Jason Burch ,  John Colucci ,  Julie Farand ,  Mario Girard ,  Yongxin Han

发明人： Michel Belley ,  Jason Burch ,  John Colucci ,  Julie Farand ,  Mario Girard ,  Yongxin Han

IPC分类号： C07D471/00

CPC分类号： C07D471/04

摘要： The invention is directed to quinoline derivatives as prostaglandin E type receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. The derivatives have the following structure of formula (I): wherein A and B represents either a nitrogen atom or a CH group with the proviso that they cannot both simultaneously be CH, Q can represent a nitrogen or a carbon atom, and Y and Z are either a nitrogen atom, a N(O) group or a C(R5) group. Pharmaceutical compositions comprising the derivatives of formula (I) are also included.

摘要翻译： 本发明涉及可用于治疗EP4介导的疾病或病症（例如急性和慢性疼痛，骨关节炎，类风湿性关节炎和癌症）的前列腺素E型受体拮抗剂的喹啉衍生物。 衍生物具有式（I）的以下结构：其中A和B表示氮原子或CH基团，条件是它们不能同时为CH，Q可以表示氮或碳原子，Y和Z 是氮原子，N（O）基或C（R5）基团。 还包括包含式（I）的衍生物的药物组合物。

公开(公告)号：US20090258918A1

公开(公告)日：2009-10-15

申请号：US12455971

申请日：2009-06-10

申请人： Xavier Billot ,  Robert N. Young ,  Yongxin Han

发明人： Xavier Billot ,  Robert N. Young ,  Yongxin Han

IPC分类号： A61K31/41 ,  C07D257/04 ,  A61P25/00

CPC分类号： A61K31/41 ,  A61K31/4015 ,  A61K45/06 ,  C07D403/12 ,  A61K2300/00

摘要： This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of a patient.

摘要翻译： 本发明涉及前列腺素E2受体的EP4亚型的有效选择性激动剂，它们在治疗与患者眼睛中眼内压升高有关的青光眼和其它病症中的用途或制剂。

公开(公告)号：US20090247596A1

公开(公告)日：2009-10-01

申请号：US12309941

申请日：2007-08-10

申请人： Marc Blouin ,  Jason Burch ,  Yongxin Han ,  Christophe Mellon

发明人： Marc Blouin ,  Jason Burch ,  Yongxin Han ,  Christophe Mellon

IPC分类号： A61K31/41 ,  C07D333/22 ,  A61K31/381 ,  C07D409/12 ,  A61P29/00

CPC分类号： C07D409/12 ,  C07D333/38

摘要： The invention is directed to thiophenecarboxamide derivatives of formulae I and II as EP4 receptor ligands, antagonists or agonists, useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, cancer and glaucoma. Pharmaceutical compositions and methods of use are also included. (Formulas I and II).

摘要翻译： 本发明涉及式I和II的噻吩甲酰胺衍生物作为EP4受体配体，拮抗剂或激动剂，其可用于治疗EP4介导的疾病或病症，例如急性和慢性疼痛，骨关节炎，类风湿性关节炎，癌症和青光眼。 还包括药物组合物和使用方法。 （式I和II）。

公开(公告)号：US20090105234A1

公开(公告)日：2009-04-23

申请号：US11989643

申请日：2006-07-28

申请人： John Colucci ,  Yongxin Han ,  Julie A. Farand

发明人： John Colucci ,  Yongxin Han ,  Julie A. Farand

IPC分类号： A61K31/5355 ,  C07D413/06 ,  A61P27/02

CPC分类号： C07D413/06

摘要： This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.

摘要翻译： 本发明涉及前列腺素E2受体的EP4亚型的有效选择性激动剂，它们在治疗青光眼和其它病症中的用途或其制剂，其与患者眼睛中的眼内压升高有关。 本发明还涉及本发明化合物用于介导成骨细胞和破骨细胞的骨建模和重塑过程的用途。