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1. 发明申请

US20050070719A1 Inhibitors of dipeptidyl peptidase iv 审中-公开
标题翻译：二肽基肽酶抑制剂
公开(公告)号：US20050070719A1
公开(公告)日：2005-03-31
申请号：US10499675
申请日：2002-12-26
申请人： Sergei Belyakov , Gregory Hamilton , David Hurst , Vincent Kalish , Weixing Li , Eric Wang , Douglas Wilkinson , Yong-Qian Wu , Weizheng Xu
发明人： Sergei Belyakov , Gregory Hamilton , David Hurst , Vincent Kalish , Weixing Li , Eric Wang , Douglas Wilkinson , Yong-Qian Wu , Weizheng Xu
IPC分类号： C07D295/18 , A61K31/397 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/404 , A61K31/426 , A61K31/427 , A61K31/4453 , A61K31/472 , A61K31/4725 , A61K31/5375 , A61K38/00 , A61K45/00 , A61P1/14 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P7/02 , A61P9/00 , A61P9/10 , A61P15/00 , A61P15/16 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/02 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/04 , A61P37/00 , A61P37/06 , A61P39/02 , A61P41/00 , A61P43/00 , C07D205/04 , C07D207/04 , C07D207/16 , C07D207/20 , C07D207/22 , C07D209/18 , C07D209/42 , C07D209/46 , C07D209/48 , C07D217/14 , C07D217/16 , C07D217/22 , C07D217/26 , C07D233/60 , C07D263/06 , C07D277/04 , C07D277/06 , C07D295/125 , C07D295/185 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D409/06 , C07D417/06 , C07K5/078 , C07K5/097
CPC分类号： C07D209/48 , A61K38/00 , C04B35/632 , C07D205/04 , C07D207/04 , C07D207/16 , C07D207/20 , C07D207/22 , C07D209/42 , C07D209/46 , C07D217/14 , C07D217/16 , C07D217/26 , C07D263/06 , C07D277/04 , C07D277/06 , C07D295/125 , C07D295/185 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D409/06 , C07D417/06 , C07K5/06156 , C07K5/0821
摘要： Novel inhibitors of dipeptidyl peptidase IV (DPP IV), pharmaceutical compositions comprising therapeutically effective amounts of novel inhibitors of DPP IV, and novel methods of treating medical conditions are provided. The novel inhibitors of DPP IV described herein are useful in the treatment of neurological disorders, diabetes, inflammatory disorders such as arthritis, obesity, osteoporosis, and of such other enumerated conditions as can be treated with inhibitors of DPP IV.
摘要翻译：提供了二肽基肽酶IV（DPP IV）的新型抑制剂，包含治疗有效量的新型DPP IV抑制剂的药物组合物，以及治疗医学病症的新方法。本文描述的DPP IV的新型抑制剂可用于治疗神经障碍，糖尿病，炎症性疾病如关节炎，肥胖症，骨质疏松症以及可用DPP IV抑制剂治疗的其他列举的病症。

2. 发明授权

US06656971B2 Trisubstituted carbocyclic cyclophilin binding compounds and their use 失效
公开(公告)号：US06656971B2
公开(公告)日：2003-12-02
申请号：US10057203
申请日：2002-01-25
申请人： Yong-Qian Wu , Sergei Belyakov , Gregory S. Hamilton , David Limburg , Joseph P. Steiner , Mark Vaal , Ling Wei , Douglas Wilkinson
发明人： Yong-Qian Wu , Sergei Belyakov , Gregory S. Hamilton , David Limburg , Joseph P. Steiner , Mark Vaal , Ling Wei , Douglas Wilkinson
IPC分类号： A61K31166
CPC分类号： C07D209/48 , A61K31/325 , C07C233/29 , C07C233/66 , C07C233/75 , C07C233/76 , C07C235/42 , C07C235/56 , C07C243/38 , C07C255/54 , C07C275/42 , C07C311/46 , C07C311/48 , C07C335/18 , C07C335/36 , C07C337/06 , C07C2602/10 , C07D213/56 , C07D213/74 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/135 , Y02A50/409 , Y02A50/411 , Y02A50/421 , Y02A50/422 , Y02A50/423
摘要： The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins, and to pharmaceutical compositions comprising one or more of the said compounds. The invention further relates to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders.

3. 发明授权

US07078424B2 N-linked sulfonamides of N-heterocyclic carboxylic acids or carboxylic acid isosteres 失效
公开(公告)号：US07078424B2
公开(公告)日：2006-07-18
申请号：US10601607
申请日：2003-06-24
申请人： Gregory S. Hamilton , Mark H. Norman , Yong-Qian Wu
发明人： Gregory S. Hamilton , Mark H. Norman , Yong-Qian Wu
IPC分类号： A61K31/41 , C07D403/04
CPC分类号： C07D207/08 , A61K8/4913 , A61Q7/00 , C07D207/16 , C07D403/04
摘要： This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.

4. 发明授权

US07153883B2 Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds 失效
公开(公告)号：US07153883B2
公开(公告)日：2006-12-26
申请号：US09920017
申请日：2001-08-02
申请人： Gregory S. Hamilton , Mark H. Norman , Yong-Qian Wu
发明人： Gregory S. Hamilton , Mark H. Norman , Yong-Qian Wu
IPC分类号： A61K31/40 , C07D207/10
CPC分类号： C07D403/04 , A61K31/401 , A61K31/4025 , A61K31/41 , A61K31/445 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/55 , C07D207/09 , C07D207/12 , C07D207/16 , C07D211/34 , C07D403/06 , C07D405/12 , C07D409/12 , C07D413/04
摘要： This invention relates to novel N-heterocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, for treating alopecia and promoting hair growth, for treating vision disorders and/or improving vision, and for treating memory impairment and/or enhancing memory performance by administering such compounds.

5. 发明授权

US07459473B2 N-linked sulfonamides of N-heterocyclic carboxylic acids or carboxylic acid isosteres 失效
标题翻译： N-杂环羧酸或羧酸异构体的N-连接磺酰胺
公开(公告)号：US07459473B2
公开(公告)日：2008-12-02
申请号：US09204236
申请日：1998-12-03
申请人： Gregory S. Hamilton , Mark H. Norman , Yong-Qian Wu
发明人： Gregory S. Hamilton , Mark H. Norman , Yong-Qian Wu
IPC分类号： A61K31/40 , A61K31/41 , A61K31/42
CPC分类号： C07D207/08 , A61K8/4913 , A61Q7/00 , C07D207/16 , C07D403/04
摘要： This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.
摘要翻译：本发明涉及N-杂环羧酸和羧酸异构体的新型N-连接磺酰胺及其制备方法，以及用于治疗神经系统疾病，包括物理损伤的神经和神经变性疾病，以及治疗脱发和促进毛发生长的用途。

6. 发明授权

US06331537B1 Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds 失效
标题翻译：羧酸和N-杂环化合物的羧酸等离子体
公开(公告)号：US06331537B1
公开(公告)日：2001-12-18
申请号：US09453571
申请日：1999-12-02
申请人： Gregory S. Hamilton , Mark H. Norman , Yong-Qian Wu
发明人： Gregory S. Hamilton , Mark H. Norman , Yong-Qian Wu
IPC分类号： A01N4346
CPC分类号： C07D403/04 , A61K31/401 , A61K31/4025 , A61K31/41 , A61K31/445 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/55 , C07D207/09 , C07D207/12 , C07D207/16 , C07D211/34 , C07D403/06 , C07D405/12 , C07D409/12 , C07D413/04
摘要： This invention relates to novel N-heteorocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodengenerative diseases, for treating alopecia and promoting hair growth, for treating vision disorders and/or improving vision, and for treating memory impairment and/or enhancing memory performance by administering such compounds.
摘要翻译：本发明涉及新型N-单环素羧酸和羧酸等体积，它们的制备和用途，用于治疗神经系统疾病，包括物理损伤的神经和神经再生疾病，用于治疗脱发和促进毛发生长，用于治疗视力障碍和/或改善视力，以及用于通过施用这些化合物来治疗记忆障碍和/或增强记忆性能。

7. 发明授权

US5981507A Polymeric carriers linked to nucleotide analogues via a phosphoramide bond 失效
标题翻译：通过磷酰胺键与核苷酸类似物连接的聚合载体
公开(公告)号：US5981507A
公开(公告)日：1999-11-09
申请号：US766597
申请日：1996-12-12
申请人： Lee Josephson , Ernest V. Groman , Yong-Qian Wu
发明人： Lee Josephson , Ernest V. Groman , Yong-Qian Wu
IPC分类号： A61K47/48 , A01N43/04
CPC分类号： A61K47/48038 , A61K47/4823 , A61K47/48315
摘要： Novel compositions of nucleotide analog prodrugs for the treatment of viral infections and cancer are herein disclosed. The prodrugs have a biocompatible polymeric carrier conjugated to the nucleotide analog via an amino-phosphate linkage. The amino group is provided by the carrier, which either inherently possesses a primary amine, or is modified with reactive groups that incorporate the primary amine onto the carrier. The carrier can be a polyamino acid, a polyvinylic polymer, a polysaccharide or combinations thereof, such as polylysine, HPMA, dextran, hydroxyethyl starch, or polyethylene glycol; the nucleotide analog can be ribavirin araA, AZT, acyclovir, 5-FUDR, araC or ddI. Methods of treating a viral infection of cancer using these prodrugs are also disclosed. The prodrugs endow the nucleotide analogs with substantially enhanced therapeutic efficacy and reduces toxicity in comparison to the nucleotide analog alone.
摘要翻译：本文公开了用于治疗病毒感染和癌症的核苷酸类似物前药的新型组合物。前药具有通过氨基 - 磷酸键连接至核苷酸类似物的生物相容性聚合物载体。氨基由载体提供，其本身具有伯胺，或者由将伯胺掺入到载体上的反应性基团进行改性。载体可以是聚氨基酸，聚乙烯基聚合物，多糖或其组合，例如聚赖氨酸，HPMA，葡聚糖，羟乙基淀粉或聚乙二醇; 核苷酸类似物可以是利巴韦林araA，AZT，阿昔洛韦，5-FUDR，araC或ddI。还公开了使用这些前药治疗癌症病毒感染的方法。与单独的核苷酸类似物相比，前药使核苷酸类似物具有显着增强的治疗功效并降低毒性。

8. 发明授权

US07253169B2 Aza compounds, pharmaceutical compositions and methods of use 失效
标题翻译：氮杂化合物，药物组合物和使用方法
公开(公告)号：US07253169B2
公开(公告)日：2007-08-07
申请号：US09835523
申请日：2001-04-17
申请人： Yong-Qian Wu , Wei Huang , Gregory S. Hamilton
发明人： Yong-Qian Wu , Wei Huang , Gregory S. Hamilton
IPC分类号： A61K31/50 , A61K31/501 , A61K31/551 , A61K31/675 , C07D413/02 , C07D43/02
CPC分类号： C07D231/04 , C07D237/04 , C07D401/06 , C07D401/12 , C07D487/04
摘要： The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities.
摘要翻译：本发明涉及N-取代的环状氮杂化合物，包含这些化合物的药物组合物及其用于实现神经元活性的方法。

9. 发明授权

US06417189B1 AZA compounds, pharmaceutical compositions and methods of use 失效
标题翻译： AZA化合物，药物组合物和使用方法
公开(公告)号：US06417189B1
公开(公告)日：2002-07-09
申请号：US09551618
申请日：2000-04-17
申请人： Yong-Qian Wu , Wei Huang , Gregory S. Hamilton
发明人： Yong-Qian Wu , Wei Huang , Gregory S. Hamilton
IPC分类号： A61K31495
CPC分类号： C07D401/06 , C07D231/04 , C07D237/04 , C07D401/12 , C07D487/04
摘要： The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities.
摘要翻译：本发明涉及N-取代的环状氮杂化合物，包含这些化合物的药物组合物及其用于实现神经元活性的方法。

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