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1. 发明授权

US06716840B2 Guanidino compounds 失效
标题翻译：胍基化合物
公开(公告)号：US06716840B2
公开(公告)日：2004-04-06
申请号：US10118730
申请日：2002-04-08
申请人： Daniel Chu , Rustum S. Boyce , David Duhl , Bryan H. Chang
发明人： Daniel Chu , Rustum S. Boyce , David Duhl , Bryan H. Chang
IPC分类号： A61K315375
CPC分类号： C07D209/46 , C07D209/48 , C07D217/24 , C07D235/08 , C07D235/10
摘要： Compounds having the general structure I are provided: X and Y are independently selected from the group consisting of CH2, N, NR9, C═O, C═S, S═O, SO2, S, O, (CR6R7)n, C(═O)—(CR6R7)n, and C(═S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of and L is selected from the group consisting of N, O, S, S═O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r”) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.
摘要翻译：提供具有通式结构I的化合物：X和Y独立地选自CH 2，N，NR 9，C = O，C = S，S = O，SO 2，S，O，（R 6 R 7）n，C（= O） - （CR 6 R 7）n和C（= S） - （CR 6 R 7）n，其中n为1 W选自N，O，S，S = O，SO 2，C（O），NC（O），NC（S），OC （O），OC（S），C（NR 10），C（NOR 10））和共价键。 Z 1，Z 2和Z 3独立地选自取代的碳和氮。式I化合物是黑皮质素-4受体（“MC-4r”）的激动剂，因此可能具有控制人类MC-4r作用相关疾病如肥胖和II型糖尿病的有用性质。

2. 发明授权

US06995269B2 Guanidinobenzamides 失效
标题翻译：胍基苯甲酰胺
公开(公告)号：US06995269B2
公开(公告)日：2006-02-07
申请号：US10379397
申请日：2003-03-04
申请人： Paul A. Renhowe , Daniel Chu , Rustum S. Boyce , David Duhl
发明人： Paul A. Renhowe , Daniel Chu , Rustum S. Boyce , David Duhl
IPC分类号： C07D211/72 , C07D295/20 , A61K31/44
CPC分类号： C07D233/64 , C07B2200/07 , C07B2200/09 , C07C279/18 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/10 , C07C2602/42 , C07C2603/74 , C07D209/16 , C07D215/12 , C07D241/08 , C07D241/42 , C07D295/215 , C07D307/24 , C07D309/14 , C07D333/20 , C07D487/04 , C07D487/08
摘要： Compounds of formula IIA and IIB are novel guanidine compounds where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.
摘要翻译：式IIA和IIB的化合物是新的胍化合物，化学式id =“CHEM-US-00001”num =“000

3. 发明授权

US06638927B2 Guanidinobenzamides 失效
标题翻译：胍基苯甲酰胺
公开(公告)号：US06638927B2
公开(公告)日：2003-10-28
申请号：US09945384
申请日：2001-08-31
申请人： Paul A. Renhowe , Daniel Chu , Rustum S. Boyce , Zhi-Jie Ni , David Duhl , Effie Tozzo , Kirk Johnson , David C. Myles
发明人： Paul A. Renhowe , Daniel Chu , Rustum S. Boyce , Zhi-Jie Ni , David Duhl , Effie Tozzo , Kirk Johnson , David C. Myles
IPC分类号： C07D29520
CPC分类号： C07D233/64 , C07B2200/07 , C07B2200/09 , C07C279/18 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/10 , C07C2602/42 , C07C2603/74 , C07D209/16 , C07D215/12 , C07D241/08 , C07D241/42 , C07D295/215 , C07D307/24 , C07D309/14 , C07D333/20 , C07D487/04 , C07D487/08
摘要： Compounds of formula IA and IB are new where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.
摘要翻译：式IA和IB的化合物是新的，其中变量R 1至R 10具有本文所述的值。这些化合物可用于治疗诸如肥胖症和II型糖尿病的疾病，并且可以作为药物制剂与药学上可接受的载体一起提供。

4. 发明授权

US08735599B2 Substituted imidazole derivates 有权
标题翻译：取代的咪唑衍生物
公开(公告)号：US08735599B2
公开(公告)日：2014-05-27
申请号：US13613977
申请日：2012-09-13
申请人： Weibo Wang , Paul A. Barsanti , Xia Yia , Rustum S. Boyce , Sabina Pecchi , Nathan Brammeier , Megan C. Phillips , Kris Mendenhall , Kelly Wayman , Liana Marie Lagnition , Ryan N. Constantine , Hong Yang , Elizabeth Mieuli , Savithri Ramurthy , Elisa Jazan , Anu Sharma , Rama Jain , Sharadha Subramanian , Paul A. Renhowe , Kenneth W. Bair , David Duhl , Annette Walter , Tinya Abrams , Kay Huh , Eric Martin , Mark Knapp , Vincent P. Le
发明人： Weibo Wang , Paul A. Barsanti , Xia Yia , Rustum S. Boyce , Sabina Pecchi , Nathan Brammeier , Megan C. Phillips , Kris Mendenhall , Kelly Wayman , Liana Marie Lagnition , Ryan N. Constantine , Hong Yang , Elizabeth Mieuli , Savithri Ramurthy , Elisa Jazan , Anu Sharma , Rama Jain , Sharadha Subramanian , Paul A. Renhowe , Kenneth W. Bair , David Duhl , Annette Walter , Tinya Abrams , Kay Huh , Eric Martin , Mark Knapp , Vincent P. Le
IPC分类号： A61K31/4174 , C07D233/00 , C07D233/54
CPC分类号： C07D233/54 , C07D233/24 , C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D498/10
摘要： The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds. The compounds of the invention have the following general formula:
摘要翻译：本发明涉及新的取代的咪唑化合物及其药学上可接受的盐，酯或前药，新化合物的组合物和药学上可接受的载体，以及新化合物的用途。本发明的化合物具有以下通式：

5. 发明授权

US07858631B2 Substituted pyrido [2,3-d] pyrimidinone compounds 失效
标题翻译：取代的吡啶并[2,3-d]嘧啶酮化合物
公开(公告)号：US07858631B2
公开(公告)日：2010-12-28
申请号：US10515434
申请日：2003-05-23
申请人： Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
发明人： Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
IPC分类号： A61K31/519
CPC分类号： C07D253/08 , C07D217/24 , C07D239/88 , C07D239/90 , C07D239/91 , C07D239/96 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D417/04 , C07D471/04
摘要： A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure of Formulas (IA), (IB), or (IC): where the values of the variable are defined herein.
摘要翻译：提供了能够作为MC4-R激动剂的各种低分子量含胍基分子。该化合物可用于治疗MC4-R介导的疾病。化合物具有式（IA），（IB）或（IC）的结构：其中变量的值在本文中定义。

6. 发明授权

US07034033B2 Substituted quinazolinone compounds 失效
公开(公告)号：US07034033B2
公开(公告)日：2006-04-25
申请号：US10444495
申请日：2003-05-23
申请人： Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
发明人： Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
IPC分类号： C07D239/90 , A61K31/517 , A61P3/04 , A61P3/10
CPC分类号： C07D253/08 , C07D217/24 , C07D239/88 , C07D239/90 , C07D239/91 , C07D239/96 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D417/04 , C07D471/04
摘要： A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure IA, IB, or IC where the values of the variable are defined herein.

7. 发明授权

US07858641B2 Substituted dihydroisoquinolinone compounds 失效
标题翻译：取代的二氢异喹啉酮化合物
公开(公告)号：US07858641B2
公开(公告)日：2010-12-28
申请号：US11248040
申请日：2005-10-11
申请人： Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
发明人： Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
IPC分类号： A61K31/47
CPC分类号： C07D253/08 , C07D217/24 , C07D239/88 , C07D239/90 , C07D239/91 , C07D239/96 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D417/04 , C07D471/04
摘要： A variety of low molecular weight, guanidino-containing dihydroisoquinolinoines capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure ID where the values of the variable are defined herein.
摘要翻译：提供了能够作为MC4-R激动剂的各种低分子量含胍基的二氢异喹啉基。该化合物可用于治疗MC4-R介导的疾病。化合物具有其中在此定义变量的值的结构ID。

8. 发明授权

US07625909B2 Substituted quinazolinone compounds 失效
标题翻译：取代喹唑啉酮化合物
公开(公告)号：US07625909B2
公开(公告)日：2009-12-01
申请号：US10850967
申请日：2004-05-21
申请人： Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Christopher R. Conlee , Brian D. Thompson , Judith de Armas Kuntz , David L. Musso , Kevin K. Barvian , Stephen A. Thomson , William R. Swain , Kien S. Du , Brian A. Chauder , Jason D. Speake , Michael J. Bishop
发明人： Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Christopher R. Conlee , Brian D. Thompson , Judith de Armas Kuntz , David L. Musso , Kevin K. Barvian , Stephen A. Thomson , William R. Swain , Kien S. Du , Brian A. Chauder , Jason D. Speake , Michael J. Bishop
IPC分类号： A61K31/517 , A61K31/519 , A61P5/50 , C07D239/88 , C07D239/95 , C07D471/04 , C07D487/04
CPC分类号： C07D217/24 , C07D239/91 , C07D239/95 , C07D239/96 , C07D253/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04
摘要： A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the structure IA, IB, and IC where the values of the variables are defined herein.
摘要翻译：提供了能够作为MC4-R激动剂的各种小分子，含胍分子。当给予受试者时，这些化合物可用于治疗MC4-R介导的疾病。化合物具有结构IA，IB和IC，其中变量的值在本文中定义。

9. 发明授权

US07037918B2 Inhibitors of glycogen synthase kinase 3 失效
公开(公告)号：US07037918B2
公开(公告)日：2006-05-02
申请号：US10309535
申请日：2002-12-03
申请人： John M. Nuss , Stephen D. Harrison , David B. Ring , Rustum S. Boyce , Sean P. Brown , Dane A. Goff , Kirk W. Johnson , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Lynn Seely , Sharadha Subramanian , Allan S. Wagman , Xiaohui A. Zhou
发明人： John M. Nuss , Stephen D. Harrison , David B. Ring , Rustum S. Boyce , Sean P. Brown , Dane A. Goff , Kirk W. Johnson , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Lynn Seely , Sharadha Subramanian , Allan S. Wagman , Xiaohui A. Zhou
IPC分类号： A61K31/505 , A61K31/535 , A61K31/47 , A61K31/475 , A61K31/52
CPC分类号： C07D213/74 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/12
摘要： New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

10. 发明授权

US06489344B1 Inhibitors of glycogen synthase kinase 3 失效
标题翻译：糖原合酶激酶抑制剂3
公开(公告)号：US06489344B1
公开(公告)日：2002-12-03
申请号：US09336098
申请日：1999-06-18
申请人： John M. Nuss , Stephen D. Harrison , David B. Ring , Rustum S. Boyce , Sean P. Brown , Dane A. Goff , Kirk W. Johnson , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Lynn Seely , Sharadha Subramanian , Allan S. Wagman , Xiaohui A. Zhou
发明人： John M. Nuss , Stephen D. Harrison , David B. Ring , Rustum S. Boyce , Sean P. Brown , Dane A. Goff , Kirk W. Johnson , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Lynn Seely , Sharadha Subramanian , Allan S. Wagman , Xiaohui A. Zhou
IPC分类号： C07D40104
CPC分类号： C07D213/74 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/12
摘要： New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
摘要翻译：提供了新的嘧啶或吡啶类化合物，体外抑制糖原合成酶激酶（GSK3）活性和体内GSK3介导的病症治疗的组合物和方法。本发明的方法，化合物和组合物可以单独使用或与其它药理活性剂组合用于治疗由GSK3活性介导的病症，例如治疗糖尿病，阿尔茨海默病和其他神经变性疾病，肥胖症，动脉粥样硬化心血管疾病，原发性高血压，多囊卵巢综合征，X综合征，缺血，创伤性脑损伤，双相情感障碍，免疫缺陷或癌症。

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