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1. 发明授权

US5719296A Pseudopeptide lactam inhibitors of peptide binding to MHC class II proteins 失效
标题翻译：肽结合到MHC II类蛋白上的肽的内肽抑制肽
公开(公告)号：US5719296A
公开(公告)日：1998-02-17
申请号：US736835
申请日：1996-10-28
申请人： John J. Acton, III , Alan D. Adams , Jeffrey D. Hermes , A. Brian Jones , William Hugh Parsons , Peter J. Sinclair
发明人： John J. Acton, III , Alan D. Adams , Jeffrey D. Hermes , A. Brian Jones , William Hugh Parsons , Peter J. Sinclair
IPC分类号： A61K38/00 , C07D207/26 , C07D207/273 , C07K5/078 , C07K5/097 , C07D207/12 , A61K31/40 , C07D207/24 , C07D207/36
CPC分类号： C07D207/273 , C07K5/06139 , C07K5/0821 , A61K38/00
摘要： Compounds of the formula ##STR1## are inhibitors of peptide binding to major histocompatibility complex type II proteins and are useful in the treatment and prevention of autoimmune diseases including: rheumatoid arthritis, Type I diabetes, multiple sclerosis, lupus erythematosis, Graves disease and pemphigus. The present invention also provides novel compositions, methods of treatment employing the compounds of the present invention and methods of manufacture of the compounds of structural formula (I).
摘要翻译：式（I）的化合物是肽与主要组织相容性复合物II型蛋白质结合的抑制剂，并且可用于治疗和预防自身免疫疾病，包括：类风湿性关节炎，I型糖尿病，多发性硬化，狼疮性疾病和天疱疮。本发明还提供新的组合物，使用本发明化合物的处理方法和结构式（I）化合物的制备方法。

2. 发明授权

US08933113B2 Mineralocorticoid receptor antagonists 有权
标题翻译：盐皮质激素受体拮抗剂
公开(公告)号：US08933113B2
公开(公告)日：2015-01-13
申请号：US13979875
申请日：2012-01-19
申请人： Alejandro Crespo , Ping Lan , Rudrajit Mal , Anthony Ogawa , Hong Shen , Peter J. Sinclair , Zhongxiang Sun , Ellen K. Vande Bunte , Zhicai Wu , Kun Liu , Robert J. DeVita , Dong-Ming Shen , Min Shu , John Qiang Tan , Changhe Qi , Yuguang Wang , Richard Beresis
发明人： Alejandro Crespo , Ping Lan , Rudrajit Mal , Anthony Ogawa , Hong Shen , Peter J. Sinclair , Zhongxiang Sun , Ellen K. Vande Bunte , Zhicai Wu , Kun Liu , Robert J. DeVita , Dong-Ming Shen , Min Shu , John Qiang Tan , Changhe Qi , Yuguang Wang , Richard Beresis
IPC分类号： A61K31/416 , C07D231/56 , A61K31/405 , A61K31/404 , C07D403/06 , C07D209/08 , C07D209/10 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K45/06 , C07D413/06
CPC分类号： C07D413/06 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/416 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K45/06 , C07D209/08 , C07D209/10 , C07D231/56 , C07D403/04 , C07D403/06 , C07D405/06
摘要： Disclosed are the compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, which are useful for treating aldosterone-mediated diseases. The processes for preparing compounds of the Formula (I), the use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and the pharmaceutical compositions which comprise compounds of the formula (I) are disclosed too.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐，其可用于治疗醛固酮介导的疾病。还公开了制备式（I）化合物，用于治疗和预防上述疾病和用于制备用于此目的的药物的方法和包含式（I）化合物的药物组合物。

3. 发明申请

US20090018054A1 Cholesteryl Ester Transfer Protein Inhibitors 有权
标题翻译：胆固醇酯转移蛋白抑制剂
公开(公告)号：US20090018054A1
公开(公告)日：2009-01-15
申请号：US12087189
申请日：2006-12-29
申请人： Amjad Ali , Peter J. Sinclair , Gayle E. Taylor
发明人： Amjad Ali , Peter J. Sinclair , Gayle E. Taylor
IPC分类号： A61K38/28 , C07D265/10 , A61K31/535 , A61K31/5355 , C07D413/06 , A61K31/45 , C07D211/76 , A61P9/10
CPC分类号： C07D265/10 , C07D413/06
摘要： Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), A1 is a cyclic group, and B is a cyclic group which is attached to the heterocyclic ring directly or through a methylene group.
摘要翻译：包括化合物的药学上可接受的盐的式（I）化合物是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。在式（I）的化合物中，A1是环状基团，B是直接或通过亚甲基与杂环连接的环状基团。

4. 发明授权

US5693648A O-aryl, O-alkyl, O-alkenyl and O-alkynyl-macrolides having immunosuppressive activity 失效
标题翻译：具有免疫抑制活性的O-芳基，O-烷基，O-烯基和O-炔基 - 大环内酯类
公开(公告)号：US5693648A
公开(公告)日：1997-12-02
申请号：US619638
申请日：1996-03-27
申请人： Mark Goulet , Helen M. Organ , William H. Parsons , Peter J. Sinclair , Frederick Wong , Matthew J. Wyvratt
发明人： Mark Goulet , Helen M. Organ , William H. Parsons , Peter J. Sinclair , Frederick Wong , Matthew J. Wyvratt
IPC分类号： C07D491/16 , A61K31/435
CPC分类号： C07D491/16
摘要： Substituted compounds of the FK-506 Type. These compounds are useful for the same or essentially the same purposes as FK-506 and are applied in the same or a similar manner. These compounds are immunosuppressants and useful for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. Still other uses are described in the disclosure.
摘要翻译： PCT No.PCT / US94 / 11114 Sec。 371日期：1996年3月27日 102（e）1996年3月27日PCT 1994年9月30日PCT公布。公开号WO95 / 09857 日期：1995年04月13日FK-506型的取代化合物。这些化合物可用于与FK-506相同或基本相同的目的，并以相同或相似的方式施用。这些化合物是免疫抑制剂，可用于治疗自身免疫疾病，感染性疾病和/或预防外来器官移植排斥反应。在本公开中描述了其他用途。

5. 发明授权

US5262533A Amino O-aryl macrolides having immunosuppressive activity 失效
标题翻译：具有免疫抑制活性的氨基O-芳基大环内酯类
公开(公告)号：US5262533A
公开(公告)日：1993-11-16
申请号：US876634
申请日：1992-05-06
申请人： Peter J. Sinclair , Helen M. Organ , Matthew J. Wyvratt
发明人： Peter J. Sinclair , Helen M. Organ , Matthew J. Wyvratt
IPC分类号： C07D498/18 , C07D491/16 , A61K31/395
CPC分类号： C07D498/18
摘要： Amino O-aryl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by arylation and amination at C-3"/C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma; as hair revitalizing agents, especially in the treatment of male pattern alopecia or alopecia senilis; in the reversal of multidrug resistance of tumor cells; in treatment of inflammation of mucosa and blood vessels, gastric ulcers, vascular damage, ischemic bowel disease, inflammatory bowel disease, necrotizing enterocolitis, intestinal lesions associated with thermal burns; in the treatment of cytomegalovirus infection; and in the treatment of idiopathic thrombocytopenic purpura and Basedow's disease.
摘要翻译：一般结构式I的氨基O-芳基大环内酯是通过在环己基环的C-3“/ C-4”处的芳基化和胺化由合适的前体制备的。这些大环内酯类免疫抑制剂可用于哺乳动物宿主用于治疗自身免疫性疾病，感染性疾病和/或预防外来器官移植排斥反应。此外，这些大环内酯类免疫抑制剂可用于局部治疗炎性和过度增生性皮肤病以及免疫介导疾病的皮肤表现。此外，这些大环内酯可用于治疗可逆性阻塞性气道疾病，特别是哮喘; 作为头发活化剂，特别是在治疗男性脱发或脱发性秃发症中，在逆转肿瘤细胞的多药耐药性; 治疗粘膜和血管的炎症，胃溃疡，血管损伤，缺血性肠病，炎性肠病，坏死性小肠结肠炎，与热灼伤相关的肠道损伤; 在治疗巨细胞病毒感染; 并在治疗特发性血小板减少性紫癜和基诺病。

6. 发明授权

US5252732A D-heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroarylmacrolides having immunosuppressive activity 失效
标题翻译：具有免疫抑制活性的D-杂芳基，O-烷基杂芳基，O-烯基杂芳基和O-炔基杂芳基大环内酯
公开(公告)号：US5252732A
公开(公告)日：1993-10-12
申请号：US921851
申请日：1992-08-05
申请人： Peter J. Sinclair , Joung Goulet , Frederick Wong , Mark Goulet , William H. Parsons , Matthew J. Wyvratt
发明人： Peter J. Sinclair , Joung Goulet , Frederick Wong , Mark Goulet , William H. Parsons , Matthew J. Wyvratt
IPC分类号： A61K31/40 , A61K31/445 , A61K31/495 , A61K31/70 , A61P37/06 , C07D498/18 , C07H19/01 , A61K31/395 , C07D491/16
CPC分类号： C07H19/01
摘要： O-Heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroarylmacrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-3" and/or C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.

7. 发明授权

US5250678A O-aryl, O-alkyl, O-alkenyl and O-alkynylmacrolides having immunosuppressive activity 失效
标题翻译：具有免疫抑制活性的O-芳基，O-烷基，O-烯基和O-炔基大环内酯
公开(公告)号：US5250678A
公开(公告)日：1993-10-05
申请号：US875036
申请日：1992-05-01
申请人： Mark Goulet , Frederick Wong , Peter J. Sinclair , Matthew J. Wyvratt
发明人： Mark Goulet , Frederick Wong , Peter J. Sinclair , Matthew J. Wyvratt
IPC分类号： A61K31/41 , A61K31/40 , A61K31/445 , A61P17/00 , A61P29/00 , A61P31/12 , A61P37/06 , C07D498/18 , C07D491/16 , A61K31/435
CPC分类号： C07D498/18
摘要： O-Aryl, O-alkyl, O-alkenyl and O-alkynyl-macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-3" and/or C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma; as hair revitalizing agents, especially in the treatment of male pattern alopecia or alopecia senilis; in the reversal of multidrug resistance of tumor cells; in treatment of inflammation of mucosa and blood vessels, gastric ulcers, vascular damage, ischemic bowel disease, necrotizing enterocolitis, intestinal lesions associated with thermal burns; in the treatment of cytomegalovirus infection; and in the treatment of idiopathic thrombocytopenic purpura and Basedow's disease.

8. 发明授权

US08445480B2 CETP inhibitors derived from benzoxazole arylamides 有权
标题翻译：衍生自苯并恶唑芳酰胺的CETP抑制剂
公开(公告)号：US08445480B2
公开(公告)日：2013-05-21
申请号：US12664757
申请日：2008-06-16
申请人： Julianne A. Hunt , Ramzi F. Sweis , Dooseop Kim , Florida Kallashi , Peter J. Sinclair
发明人： Julianne A. Hunt , Ramzi F. Sweis , Dooseop Kim , Florida Kallashi , Peter J. Sinclair
IPC分类号： A61K31/553 , A61K31/5377 , A61K31/506 , A61K31/443 , A61K31/4525 , A61K31/423 , A61K31/438 , C07D239/42 , C07D267/10 , C07D413/14 , C07D401/14 , C07D221/20 , C07D211/26 , C07D263/57
CPC分类号： C07D413/14 , C07D413/10 , C07D413/12
摘要： Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis Atherosclerosis and its clinical consequences, coronary heart disease (CHD), stroke and penpheral vascular disease, represent a truly enormous burden to the health care systems of the industrialized world In formula I, A-B is an arylamide moiety.
摘要翻译：具有式I结构的化合物，包括化合物的药学上可接受的盐，是有效的CETP（胆固醇酯转移蛋白）抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，并用于治疗或预防动脉粥样硬化。动脉粥样硬化及其临床后果，冠心病（CHD），中风和血管性血管疾病对工业化世界的保健系统来说是一个真正的巨大负担。在公式I中，AB是芳基酰胺部分。

9. 发明授权

US08436028B2 CETP inhibitors derived from benzoxazole arylamides 有权
标题翻译：衍生自苯并恶唑芳酰胺的CETP抑制剂
公开(公告)号：US08436028B2
公开(公告)日：2013-05-07
申请号：US12664715
申请日：2008-06-16
申请人： Julianne A. Hunt , Rogelio L. Martinez , Peter J. Sinclair , Ramzi F. Sweis
发明人： Julianne A. Hunt , Rogelio L. Martinez , Peter J. Sinclair , Ramzi F. Sweis
IPC分类号： A61K31/423 , C07D498/00
CPC分类号： C07D263/57 , C07D413/12 , C07D417/12 , C07F5/025
摘要： Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are potent CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In formula I, A-B is an arylamide moiety.
摘要翻译：具有式I结构的化合物，包括化合物的药学上可接受的盐，是有效的CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。在式I中，A-B是芳基酰胺部分。

10. 发明授权

US07935727B2 CETP inhibitors 失效
标题翻译： CETP抑制剂
公开(公告)号：US07935727B2
公开(公告)日：2011-05-03
申请号：US12083183
申请日：2006-10-13
申请人： Yi-Heng Chen , Zhijian Lu , Peter J. Sinclair
发明人： Yi-Heng Chen , Zhijian Lu , Peter J. Sinclair
IPC分类号： A01N47/10 , A61K31/27 , C07C331/00 , C07C381/00 , C07C333/00 , C07C261/00 , C07C269/00 , C07C271/00
CPC分类号： C07C271/22
摘要： Compounds having a biphenyl group substituted with a phenyl or heteroaromatic group, as shown in Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis:
摘要翻译：包含被苯基或杂芳基取代的联苯基的化合物，如式I所示，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化：

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