专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

61. 发明申请

US20100105718A1 NAPHTHALENE AND QUINOLINE SULFONYLUREA DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS 有权
标题翻译：作为EP4受体拮抗剂的萘磺隆和喹啉磺酰胺衍生物
公开(公告)号：US20100105718A1
公开(公告)日：2010-04-29
申请号：US12529271
申请日：2008-03-25
申请人： Jason Burch , Julie Farand , Yongxin Han , Claudio Sturino
发明人： Jason Burch , Julie Farand , Yongxin Han , Claudio Sturino
IPC分类号： A61K31/437 , C07D471/04 , A61K31/403 , C07D209/56
CPC分类号： C07D209/64 , C07D471/04
摘要： The invention is directed to naphthalene and quinoline sulfonylurea 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：本发明涉及作为可用于治疗EP4介导的疾病或病症如急性和慢性疼痛，骨关节炎，类风湿性关节炎和癌症的EP4受体拮抗剂的萘和喹啉磺酰脲衍生物。还包括药物组合物和使用方法。

62. 发明申请

US20050239872A1 1,5-distributed pyrrolid-2-one derivatives for use as ep4 receptor agonists in the teatment of eye diseases such as glaucoma 审中-公开
标题翻译： 1,5-分布的吡咯烷-2-酮衍生物，用作眼部疾病如青光眼的ep4受体激动剂
公开(公告)号：US20050239872A1
公开(公告)日：2005-10-27
申请号：US10511736
申请日：2003-06-02
申请人： Xavier Billot , Robert Young , Yongxin Han
发明人： Xavier Billot , Robert Young , Yongxin Han
IPC分类号： C07D403/06 , A61K31/13 , A61K31/137 , A61K31/138 , A61K31/382 , A61K31/4015 , A61K31/41 , A61K31/416 , A61K31/4164 , A61K31/4168 , A61K31/4178 , A61K31/433 , A61K31/4412 , A61K31/498 , A61K31/5377 , A61K31/5575 , A61K31/559 , A61K45/00 , A61K45/06 , A61P3/14 , A61P19/00 , A61P19/02 , A61P19/08 , A61P19/10 , A61P25/02 , A61P27/02 , A61P27/06 , A61P29/00 , A61P35/00 , A61P43/00 , C07D207/26 , C07D403/12
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 of formula (1), 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 the patient.
摘要翻译：本发明涉及式（1）的前列腺素E2受体的EP 4亚型的有效选择性激动剂，它们在治疗与眼内压升高有关的青光眼和其它病症中的用途或制剂在病人眼中。

63. 发明申请

US20050130954A1 AKT protein kinase inhibitors 审中-公开
标题翻译： AKT蛋白激酶抑制剂
公开(公告)号：US20050130954A1
公开(公告)日：2005-06-16
申请号：US10993173
申请日：2004-11-19
申请人： Ian Mitchell , Keith Spencer , Peter Stengel , Yongxin Han , Nicholas Kallan , Mark Munson , Guy Vigers , James Blake , Anthony Piscopio , John Josey , Scott Miller , Dengming Xiao , Riu Xu , Chang Rao , Bin Wang , April Bernacki
发明人： Ian Mitchell , Keith Spencer , Peter Stengel , Yongxin Han , Nicholas Kallan , Mark Munson , Guy Vigers , James Blake , Anthony Piscopio , John Josey , Scott Miller , Dengming Xiao , Riu Xu , Chang Rao , Bin Wang , April Bernacki
IPC分类号： A61K20060101 , A61K31/496 , A61K31/519 , A61K31/53
CPC分类号： C07D239/94 , B41M3/008 , B44F1/10 , C07D231/56 , C07D237/28 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/04 , C07D409/12 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04 , G09F13/16 , Y10T428/24802 , Y10T428/24851 , Y10T428/25 , Y10T428/31507 , Y10T428/31551 , Y10T428/31786 , Y10T428/31855
摘要： The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
摘要翻译：本发明提供包括拆分的对映异构体，非对映异构体，溶剂合物和药学上可接受的盐的化合物，其包含式：<？在线公式描述=“在线公式”end =“lead”→> AL-CR < in-line-formula description =“In-line Formulas”end =“tail”？>其中CR是循环核心组，L是连接组，A如本文所定义。还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。

64. 发明授权

US6096881A Sulfur transfer reagents for oligonucleotide synthesis 失效
标题翻译：用于寡核苷酸合成的硫转移试剂
公开(公告)号：US6096881A
公开(公告)日：2000-08-01
申请号：US865666
申请日：1997-05-30
申请人： Yongxin Han , Jimmy Tang , Zhoada Zhang , Jin-Yan Tang
发明人： Yongxin Han , Jimmy Tang , Zhoada Zhang , Jin-Yan Tang
IPC分类号： C07D285/12 , C07D285/125 , C07D285/135 , C07D285/16 , C07H21/00 , C07D285/01 , C07H21/02
CPC分类号： C07D285/16 , C07H21/00
摘要： In our research, two commercially available compounds, 3-amino-1,2,4-dithiazole-5-thione (1) and xanthane hydride (2), and their derivatives 3-6 are found to be potential sulfur-transfer reagents. The efficiency and optimization of these new sulfur-transfer reagents were investigated by solid-phase syntheses of dinudeotide and oligonucleotide phosphorothioates. The results show that both compounds 1 and 2 are highly efficient sulfurizing reagents, and better than 99% sulfur transfer efficiency can be achieved at each step. In contrast to Beaucage reagent, these novel sulfur-transfer reagents are very stable in various solvents, and are available in bulk quantities at low cost. Due to these advantages, compounds 1 and 2 can be considered alternatives to Beaucage reagent, especially in large-scale preparation of oligonucleotide phosphorothioates. Furthermore, compounds 1 and 2 were modified to enhance their solubility in acetonitrile. Three types of structure, as described as Formulae I, II, and III, are considered as potential efficient sulfur-transfer reagents based on our results.
摘要翻译：在我们的研究中，发现两种市售化合物，3-氨基-1,2,4-二噻唑-5-硫酮（1）和氢化蒽（2）及其衍生物3-6是潜在的硫转移试剂。通过二肽和寡核苷酸硫代磷酸酯的固相合成研究了这些新型硫转移试剂的效率和优化。结果表明，化合物1和化合物2均为高效硫化试剂，每步可达99％以上的硫转移效率。与Beaucage试剂相反，这些新型硫转移试剂在各种溶剂中非常稳定，并且可以以低成本批量获得。由于这些优点，化合物1和2可以被认为是拜耳试剂的替代物，特别是在大规模制备寡核苷酸硫代磷酸酯时。此外，化合物1和2被修饰以增强其在乙腈中的溶解度。根据我们的结果，三种类型的结构，如式I，II和III所述被认为是潜在的有效的硫转移试剂。

65. 发明授权

US11319295B2 Substituted phenyloxetane and phenyltetrahydrofuran compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors 有权
公开(公告)号：US11319295B2
公开(公告)日：2022-05-03
申请号：US16753043
申请日：2018-10-04
申请人： MERCK SHARP & DOHME CORP. , Catherine M. White , Meredeth Ann McGowan , Yongxin Han , Nunzio Sciammetta
发明人： Catherine M. White , Meredeth Ann McGowan , Yongxin Han , Nunzio Sciammetta
IPC分类号： C07D305/08 , A61P37/00 , A61P25/28 , A61P31/12 , A61P25/24 , A61P27/12 , A61P35/00 , C07D307/22 , C07D307/24 , C07D405/04 , A61K45/06
摘要： Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (Formula (I)). Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

66. 发明申请

US20210214308A1 NOVEL [3.3.1] BICYCLO COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE INHIBITORS 有权
公开(公告)号：US20210214308A1
公开(公告)日：2021-07-15
申请号：US17057959
申请日：2019-05-28
申请人： Shuwen HE , Yongxin HAN , Alexander PASTERNAK , Merck Sharp & Dohme Corp.
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 DO-associated disease or disorder.

67. 发明授权

US10927086B2 Substituted sulfoximine compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors 有权
公开(公告)号：US10927086B2
公开(公告)日：2021-02-23
申请号：US16483957
申请日：2018-02-19
申请人： Merck Sharp & Dohme Corp. , Kun Liu , Dane Clausen , Liangqin Guo , Yongxin Han , Shuwen He , Joseph Kozlowski , Derun Li , Qinglin Pu , Wensheng Yu , Hongjun Zhang
发明人： Kun Liu , Dane Clausen , Liangqin Guo , Yongxin Han , Shuwen He , Joseph Kozlowski , Derun Li , Qinglin Pu , Wensheng Yu , Hongjun Zhang
IPC分类号： C07D271/08 , C07D413/12
摘要： Compounds of Formula I, or a pharmaceutically acceptable salt, solvate or hydrate thereof: (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

68. 发明申请

US20200239423A1 NOVEL SUBSTITUTED PHENYLOXETANE AND PHENYLTETRAHYDROFURAN COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS 审中-公开
公开(公告)号：US20200239423A1
公开(公告)日：2020-07-30
申请号：US16753043
申请日：2018-10-04
申请人： Catherine M. WHITE , Meredeth Ann MCGOWAN , Yongxin HAN , Nunzio SCIAMMETTA , MERCK SHARP & DOHME CORP.
发明人： Catherine M. White , Meredeth Ann McGowan , Yongxin Han , Nunzio Sciammetta
IPC分类号： C07D305/08 , C07D307/24 , C07D307/22 , C07D405/04 , A61P35/00 , A61P31/12 , A61P25/24 , A61P25/28 , A61P27/12 , A61P37/00
摘要： Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (Formula (I)). Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

69. 发明授权

US10370368B2 Aryl acylsulfonamides as BLT1 antagonists 有权
公开(公告)号：US10370368B2
公开(公告)日：2019-08-06
申请号：US15768097
申请日：2016-11-28
申请人： Merck Sharp & Dohme Corp. , Yongxin Han , Satyanarayana Tummanapalli , Phieng Siliphaivanh , Kerrie Spencer
发明人： Yongxin Han , Satyanarayana Tummanapalli , Phieng Siliphaivanh , Kerrie Spencer
IPC分类号： A61K9/20 , A61P3/10 , 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.

70. 发明申请

US20140057836A1 HCV NS3 PROTEASE INHIBITORS 有权
标题翻译： HCV NS3蛋白酶抑制剂
公开(公告)号：US20140057836A1
公开(公告)日：2014-02-27
申请号：US13960343
申请日：2013-08-06
申请人： Thomas BARA , Sathesh Bhat , Dipshika Biswas , Linda Brockunier , Duane Burnette , Samuel Chackalamannil , Mariappan Vasu Cheliah , Austin Chen , Martin Clasby , Vince J. Colandrea , Zhuyan Guo , Yongxin Han , Charles Jayne , Hubert Josien , Karen Marcantonio , Shouwu Miao , Santhosh Neelamkavil , Patrick Pinto , Murali Rajogopalan , Unmesh Shah , Francisco Velazquez , Srikanth Venkatraman , Yan Xia
发明人： Thomas BARA , Sathesh Bhat , Dipshika Biswas , Linda Brockunier , Duane Burnette , Samuel Chackalamannil , Mariappan Vasu Cheliah , Austin Chen , Martin Clasby , Vince J. Colandrea , Zhuyan Guo , Yongxin Han , Charles Jayne , Hubert Josien , Karen Marcantonio , Shouwu Miao , Santhosh Neelamkavil , Patrick Pinto , Murali Rajogopalan , Unmesh Shah , Francisco Velazquez , Srikanth Venkatraman , Yan Xia
IPC分类号： C07K5/08 , A61K45/06 , A61K38/06
CPC分类号： C07K5/08 , A61K38/06 , A61K45/06 , C07D419/00 , C07D491/22
摘要： The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.
摘要翻译：本发明涉及含有螺环状的丙型肝炎病毒（HCV）NS3蛋白酶抑制剂，这些化合物的用途，以及这些化合物的合成。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式