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1. 发明申请

US20100324140A1 GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES 审中-公开
标题翻译： GLUCAGON受体拮抗剂，制剂和治疗用途
公开(公告)号：US20100324140A1
公开(公告)日：2010-12-23
申请号：US12868773
申请日：2010-08-26
申请人： Scott Eugene CONNER , Guoxin ZHU , Jianke LI
发明人： Scott Eugene CONNER , Guoxin ZHU , Jianke LI
IPC分类号： A61K31/197 , C07C229/38 , A61P3/10
CPC分类号： C07D213/89 , C07C235/42 , C07C251/48 , C07C255/54 , C07C323/60 , C07C323/62 , C07C323/65 , C07C2601/02 , C07C2601/14 , C07D213/30 , C07D213/64 , C07D213/65 , C07D295/096 , C07D319/06 , C07D319/20
摘要： The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
摘要翻译：本发明公开了具有胰高血糖素受体拮抗剂或反向激动剂活性的新颖的式I化合物或其药学上可接受的盐，以及制备这些化合物的方法。在另一个实施方案中，本发明公开了包含式I化合物的药物组合物以及使用它们治疗糖尿病和其它与胰高血糖素相关的代谢紊乱等的方法。

2. 发明授权

US07396850B2 Pyrazole derivative as PPAR modulator 失效
标题翻译：吡唑衍生物作为PPAR调节剂
公开(公告)号：US07396850B2
公开(公告)日：2008-07-08
申请号：US10537282
申请日：2003-12-31
申请人： Scott Eugene Conner , Nathan Bryan Mantlo , Daniel Ray Mayhugh , Guoxin Zhu
发明人： Scott Eugene Conner , Nathan Bryan Mantlo , Daniel Ray Mayhugh , Guoxin Zhu
IPC分类号： A61K31/415 , C07D231/10
CPC分类号： C07D231/12 , C07D233/20 , C07D233/22 , C07D233/64 , C07D249/06 , C07D253/04 , C07D261/08
摘要： The present invention is directed to a compound, {2-Methyl-4-[3-methyl-1-(4-trifluoromethyl-phenyl)-1H-pyrazol-4-ylmethylsulfanyl]-phenoxy}-acetic acid and pharmaceutical uses thereof.
摘要翻译：本发明涉及化合物{2-甲基-4- [3-甲基-1-（4-三氟甲基 - 苯基）-1H-吡唑-4-基甲基硫烷基] - 苯氧基} - 乙酸及其药物用途。

3. 发明授权

US07259175B2 Peroxisome proliferator activated receptor modulators 失效
标题翻译：过氧化物酶体增殖物激活受体调节剂
公开(公告)号：US07259175B2
公开(公告)日：2007-08-21
申请号：US10505103
申请日：2003-02-13
申请人： Scott Eugene Conner , Nathan Bryan Mantlo , Guoxin Zhu
发明人： Scott Eugene Conner , Nathan Bryan Mantlo , Guoxin Zhu
IPC分类号： A61K31/497 , A61K31/501 , A61K31/506 , A61K31/4439 , C07D417/10 , C07D413/10
CPC分类号： C07D413/04 , C07D263/32 , C07D277/24 , C07D277/26 , C07D413/10 , C07D417/04 , C07D417/10
摘要： The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I: wherein: (a) R5 is selected from the group consisting of (C1-C6) alkyl, (C1-C6) alkenyl, substituted aryl(C0-C4)alkyl, substituted aryloxy(C0-C4)alkyl, substituted arylthio(C0-C4)alkyl, unsubstituted aryl(C0-C4)alkyl, unsubstituted aryloxy(C0-C4)alkyl, and unsubstituted arylthio(C0-C4)alkyl; (b) T1 is C or N; (c) Q is selected from the group consisting of O, a single bond, O(CH2)q and C; (d) q is 1 or 2; (e) W is selected from the group consisting of O, S, (CH2)rN(R20)(CH2)k, NHSO2, C(O)N(R20)(CH2)r, (CH2)rN(R20)C(O), and SO2; (f) X is CmH2m; (g) m is 0, 1 or 2; (h) A is an functional group selected from the group consisting of carboxyl, C1-C3 alkylnitrile, carboxamide, and (CH2)n COOR19; and (i) R19 is selected from the group consisting of hydrogen, optionally substituted C1-C4alkyl and optionally substituted arylmethyl
摘要翻译：本发明涉及由以下结构式表示的化合物及其药学上可接受的盐，式I：其中：（a）R 5选自（C 1 -C 3）（C 1 -C 6）烷基，（C 1 -C 6 -C 6）链烯基，取代的芳基（C 0 -C 6 - 取代的芳氧基（C 0 -C 4 -C 4烷基）烷基，取代的芳硫基（C 0 -C 4 - 烷基，未取代的芳基（C 0 -C 4 -C 4）烷基，未取代的芳氧基（C 0 -C 4 - 烷基和未取代的芳硫基（C 0 -C 4 -C 4）烷基; （b）T1为C或N; （c）Q选自O，单键，O（CH 2 CH 2）q C和C; （d）q为1或2; （e）W选自O，S，（CH 2）n N（R 20）（CH 2 CH 2） C（O）N（R 20）（CH 2）n），（CH

4. 发明授权

US07989457B2 Glucagon receptor antagonists, preparation and therapeutic uses 有权
标题翻译：胰高血糖素受体拮抗剂，制剂和治疗用途
公开(公告)号：US07989457B2
公开(公告)日：2011-08-02
申请号：US11569273
申请日：2005-05-13
申请人： Mark Donald Chappell , Scott Eugene Conner , Isabel Cristina Gonzalez Valcarcel , Jason Eric Lamar , Jianke Li , Julie Sue Moyers , Rebecca Anne Owens , Allie Edward Tripp , Guoxin Zhu
发明人： Mark Donald Chappell , Scott Eugene Conner , Isabel Cristina Gonzalez Valcarcel , Jason Eric Lamar , Jianke Li , Julie Sue Moyers , Rebecca Anne Owens , Allie Edward Tripp , Guoxin Zhu
IPC分类号： C07D239/26 , A61K31/505
CPC分类号： C07D213/16 , C07D213/26 , C07D213/30 , C07D213/32 , C07D213/643 , C07D239/26 , C07D401/04
摘要： The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
摘要翻译：本发明公开了具有胰高血糖素受体拮抗剂或反向激动剂活性的式（I）的新化合物或其药学上可接受的盐，以及制备这些化合物的方法。在另一个实施方案中，本发明公开了包含式（I）化合物的药物组合物以及使用它们治疗糖尿病和其它与胰高血糖素相关的代谢紊乱等的方法。

5. 发明申请

US20110124648A1 GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES 有权
标题翻译： GLUCAGON受体拮抗剂，制剂和治疗用途
公开(公告)号：US20110124648A1
公开(公告)日：2011-05-26
申请号：US13013280
申请日：2011-01-25
申请人： Scott Eugene CONNER , Guoxin ZHU , Jianke LI
发明人： Scott Eugene CONNER , Guoxin ZHU , Jianke LI
IPC分类号： A61K31/5375 , C07C55/34 , A61K31/195 , C07D213/56 , A61K31/4418 , C07D213/65 , C07D319/20 , A61K31/357 , C07D265/30 , A61P3/10
CPC分类号： C07D213/89 , C07C235/42 , C07C251/48 , C07C255/54 , C07C323/60 , C07C323/62 , C07C323/65 , C07C2601/02 , C07C2601/14 , C07D213/30 , C07D213/64 , C07D213/65 , C07D295/096 , C07D319/06 , C07D319/20
摘要： The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
摘要翻译：本发明公开了具有胰高血糖素受体拮抗剂或反向激动剂活性的新颖的式I化合物或其药学上可接受的盐，以及制备这些化合物的方法。在另一个实施方案中，本发明公开了包含式I化合物的药物组合物以及使用它们治疗糖尿病和其它与胰高血糖素相关的代谢紊乱等的方法。

6. 发明申请

US20090054479A1 FUSED HETEROCYCLIC DERIVATIVES AS PPAR MODULATORS 失效
标题翻译：作为PPAR调节剂的熔融杂环衍生物
公开(公告)号：US20090054479A1
公开(公告)日：2009-02-26
申请号：US12099929
申请日：2008-04-09
申请人： Scott Eugene Conner , Nathan Bryan Mantlo , Guoxin Zhu
发明人： Scott Eugene Conner , Nathan Bryan Mantlo , Guoxin Zhu
IPC分类号： A61K31/437 , C07D277/66 , A61K31/428 , C07D263/57 , A61P3/10 , A61K31/423 , C07D471/04
CPC分类号： C07D209/10 , C07D235/18 , C07D263/57 , C07D277/60 , C07D277/66 , C07D413/12 , C07D417/12 , C07D471/04 , C07D513/04
摘要： The present invention is directed to compounds represented by the following structural formula, Formula I: wherein: (a) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (b) U is an aliphatic linker; (c) Y is selected from the group consisting of C, O, S, NH and a single bond; (d) E is C(R3)(R4)A or A and wherein (i) A is selected from the group consisting of carboxyl, tetrazole, C1-C6 alkylnitrile, carboxamide, sulfonamide and acylsulfonamide; (e) B is selected from the group consisting of S, O, C, and N; (f) Z is selected from the group consisting of N and C; with the proviso that when B is C then Z is N.
摘要翻译：本发明涉及由以下结构式（I）表示的化合物：其中：（a）X选自单键，O，S，S（O）2和N; （b）U是脂族连接体; （c）Y选自C，O，S，NH和单键; （d）E是C（R3）（R4）A或A，其中（i）A选自羧基，四唑，C 1 -C 6烷基腈，甲酰胺，磺酰胺和酰基磺酰胺; （e）B选自S，O，C和N; （f）Z选自N和C; 条件是当B为C时，则Z为N.

7. 发明申请

US20080300289A1 Glucagon Receptor Antagonists, Preparation and Therapeutic Uses 有权
公开(公告)号：US20080300289A1
公开(公告)日：2008-12-04
申请号：US12094406
申请日：2006-11-21
申请人： Mark Donald Chappell , Scott Eugene Conner , Philip-Arthur Hipskind , Allie Edward Tripp , Guoxin Zhu
发明人： Mark Donald Chappell , Scott Eugene Conner , Philip-Arthur Hipskind , Allie Edward Tripp , Guoxin Zhu
IPC分类号： A61K31/41 , C07D257/04 , A61P3/10
CPC分类号： C07D409/12
摘要： The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

8. 发明授权

US07405305B2 Pyrrole-2, 5dione derivatives and their used as GSK-3 inhibitors 失效
标题翻译：吡咯-2,5-二酮衍生物，用作GSK-3抑制剂
公开(公告)号：US07405305B2
公开(公告)日：2008-07-29
申请号：US10506029
申请日：2003-03-05
申请人： Pamela Ann Albaugh , Jochen Ammenn , Timothy Paul Burkholder , Joshua Ryan Clayton , Scott Eugene Conner , Brian Eugene Cunningham , Thomas Albert Engler , Kelly Wayne Furness , James Robert Henry , Sushant Malhotra , Mark Joseph Tebbe , Guoxin Zhu , YiHong Li , Brian Raymond Berridge , Charles Edward Ruegg , John Morris Sullivan
发明人： Pamela Ann Albaugh , Jochen Ammenn , Timothy Paul Burkholder , Joshua Ryan Clayton , Scott Eugene Conner , Brian Eugene Cunningham , Thomas Albert Engler , Kelly Wayne Furness , James Robert Henry , Sushant Malhotra , Mark Joseph Tebbe , Guoxin Zhu , YiHong Li , Brian Raymond Berridge , Charles Edward Ruegg , John Morris Sullivan
IPC分类号： C07D209/12 , C07D207/24 , C07D211/06
CPC分类号： C07D451/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D471/04 , C07D491/04
摘要： The present invention provides kinase inhibitors of Formula (I)
摘要翻译：本发明提供式（I）的激酶抑制剂，

9. 发明申请

US20080125468A1 Glucagon Receptor Antagonists, Preparation and Therapeutic Uses 有权
公开(公告)号：US20080125468A1
公开(公告)日：2008-05-29
申请号：US11569273
申请日：2005-05-13
申请人： Mark Donald Chappell , Scott Eugene Conner , Isabel Cristina Gonzalez Valcarcel , Jason Eric Lamar , Jianke Li , Julie Sue Moyers , Rebecca Anne Owens , Allie Edward Tripp , Guoxin Zhu
发明人： Mark Donald Chappell , Scott Eugene Conner , Isabel Cristina Gonzalez Valcarcel , Jason Eric Lamar , Jianke Li , Julie Sue Moyers , Rebecca Anne Owens , Allie Edward Tripp , Guoxin Zhu
IPC分类号： A61K31/44 , C07D211/70 , A61P3/10 , A61K31/165 , C07C233/00
CPC分类号： C07D213/16 , C07D213/26 , C07D213/30 , C07D213/32 , C07D213/643 , C07D239/26 , C07D401/04
摘要： The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

10. 发明授权

US08691856B2 Glucagon receptor antagonists, preparation and therapeutic uses 失效
标题翻译：胰高血糖素受体拮抗剂，制剂和治疗用途
公开(公告)号：US08691856B2
公开(公告)日：2014-04-08
申请号：US12093601
申请日：2006-11-16
申请人： Scott Eugene Conner , Philip Arthur Hipskind , Jianke Li , Guoxin Zhu
发明人： Scott Eugene Conner , Philip Arthur Hipskind , Jianke Li , Guoxin Zhu
IPC分类号： A01N43/64 , A61K31/41 , C07D257/04 , C07D257/10 , C07D403/00 , C07D487/00
CPC分类号： C07D257/06 , C07D257/04
摘要： The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
摘要翻译：本发明公开了具有胰高血糖素受体拮抗剂或反向激动剂活性的式（I）的新化合物或其药学上可接受的盐，以及制备这些化合物的方法。在另一个实施方案中，本发明公开了包含式（I）化合物的药物组合物以及使用它们治疗糖尿病和其它与胰高血糖素相关的代谢紊乱等的方法。

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