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1. 发明申请

US20120302541A1 4-SUBSTITUTED-2-PHENOXY-PHENYLAMINE DELTA OPIOID RECEPTOR MODULATORS 有权
标题翻译： 4-取代-2-苯基 - 苯甲酰三嗪类阿片受体调节剂
公开(公告)号：US20120302541A1
公开(公告)日：2012-11-29
申请号：US13503433
申请日：2010-10-28
申请人： Steven J. Coats , Haiyan Bian , Chaozhong Cai , Bart L. DeCorte , Li Liu , Mark J. Macielag , Scott L. Dax , Philip M. Pitis , Peter J. Connolly , Wei He
发明人： Steven J. Coats , Haiyan Bian , Chaozhong Cai , Bart L. DeCorte , Li Liu , Mark J. Macielag , Scott L. Dax , Philip M. Pitis , Peter J. Connolly , Wei He
IPC分类号： A61K31/40 , C07D211/26 , A61K31/445 , C07D401/12 , A61K31/4439 , C07D405/12 , A61K31/4025 , C07D409/12 , C07D403/12 , A61K31/506 , C07D295/096 , A61K31/495 , C07D413/12 , A61K31/4245 , C07D451/02 , A61K31/46 , C07C217/84 , A61K31/136 , C07D205/04 , A61K31/397 , C07D453/02 , A61K31/439 , A61P29/00 , A61P19/02 , A61P25/06 , A61P11/02 , A61P13/10 , A61P17/00 , A61P11/12 , A61P25/00 , A61P25/02 , A61P1/00 , A61P35/00 , A61P25/24 , A61P25/16 , A61P25/30 , A61P25/32 , A61P13/00 , A61P15/00 , A61P1/12 , A61P9/00 , A61P11/00 , C07D207/14
CPC分类号： C07D401/12 , C07C211/48 , C07C211/50 , C07C233/08 , C07C233/11 , C07C233/65 , C07C255/50 , C07D205/04 , C07D207/09 , C07D211/56 , C07D405/12 , C07D409/12 , C07D413/12 , C07D451/04 , C07D453/02
摘要： Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Ra, and Y are defined herein.
摘要翻译：公开了用于治疗各种疾病，综合征，病症和障碍（包括疼痛）的化合物，组合物和方法。这样的化合物由式I表示如下：其中R1，R2，R3，Ra和Y如本文所定义。

2. 发明授权

US08242157B2 Benzimidazole derivatives useful as TRPM8 channel modulators 有权
标题翻译：苯并咪唑衍生物可用作TRPM8通道调节剂
公开(公告)号：US08242157B2
公开(公告)日：2012-08-14
申请号：US12797743
申请日：2010-06-10
申请人： Michele C. Jetter , Mark J. Macielag , Mingde Xia , Xiaoqing Xu
发明人： Michele C. Jetter , Mark J. Macielag , Mingde Xia , Xiaoqing Xu
IPC分类号： C07D401/00 , C07D235/12 , C07D235/22 , A01N43/52 , A61K31/415
CPC分类号： C07D235/30 , C07D498/06
摘要： Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R0, R1, R2, R3, R4 and a are defined herein.
摘要翻译：公开了用于治疗各种疾病，综合征，病症和障碍（包括疼痛）的化合物，组合物和方法。这样的化合物由式I表示如下：其中R 0，R 1，R 2，R 3，R 4和a在本文中定义。

3. 发明申请

US20120077797A1 OXOPIPERAZINE-AZETIDINE AMIDES AND OXODIAZEPINE-AZETIDINE AMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS 失效
标题翻译：作为单加性胆碱酯酶抑制剂的奥西维他嗪 - 阿魏酸和氧化吖嗪 - 阿魏酸
公开(公告)号：US20120077797A1
公开(公告)日：2012-03-29
申请号：US13246232
申请日：2011-09-27
申请人： Peter J. Connolly , Mark J. Macielag , Mark E. McDonnell , Bin Zhu
发明人： Peter J. Connolly , Mark J. Macielag , Mark E. McDonnell , Bin Zhu
IPC分类号： A61K31/506 , A61P25/00 , A61K31/496 , C07D417/14 , C07D409/14 , C07D403/04
CPC分类号： C07D403/14 , C07D403/04 , C07D409/14 , C07D417/14
摘要： Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (Ia) and Formula (Ib) as follows: wherein Y, Z, and n are defined herein; and wherein Yb and Zb are as defined herein.
摘要翻译：公开了用于治疗各种疾病，综合征，病症和障碍（包括疼痛）的化合物，组合物和方法。这样的化合物及其对映体，非对映体及其药学上可接受的盐由式（Ia）和式（Ib）表示如下：其中Y，Z和n如本文所定义; 并且其中Yb和Zb如本文所定义。

4. 发明授权

US07732612B2 7-amino alkylidenyl-heterocyclic quinolones and naphthyridones 有权
标题翻译： 7-氨基亚烷基 - 杂环喹诺酮和萘啶酮
公开(公告)号：US07732612B2
公开(公告)日：2010-06-08
申请号：US11084987
申请日：2005-03-21
申请人： Eugene B. Grant , Mark J. Macielag , Steven David Paget , Michele Ann Weidner-Wells , Xiaoqing Xu , Xiaodong Xu
发明人： Eugene B. Grant , Mark J. Macielag , Steven David Paget , Michele Ann Weidner-Wells , Xiaoqing Xu , Xiaodong Xu
IPC分类号： C07D215/38
CPC分类号： C07D215/56 , C07D401/04 , C07D471/04
摘要： The present invention relates to compounds having a structure according to Formula I wherein n, m, z, R, R2, R3, R4, R5, R6, A, E, X, Y, a and b are as defined above; or an optical isomer, diastereomer or enantiomer thereof; a pharmaceutically acceptable salt, hydrate, or prodrug thereof.
摘要翻译：本发明涉及具有式I结构的化合物，其中n，m，z，R，R 2，R 3，R 4，R 5，R 6，A，E，X，Y，a和b如上所定义; 或其光学异构体，非对映异构体或对映异构体; 其药学上可接受的盐，水合物或前药。

5. 发明申请

US20090156577A1 7-AMINO ALKYLIDENYL-HETEROCYCLIC QUINOLONES AND NAPHTHYRIDONES 审中-公开
标题翻译： 7-氨基亚苄基 - 杂环喹啉和萘胺
公开(公告)号：US20090156577A1
公开(公告)日：2009-06-18
申请号：US12268529
申请日：2008-11-11
申请人： Benjamin Davis , Eugene B. Grant, III , Shu-Chen Lin , Mark J. Macielag , Michele Ann Weidner-Wells , Xiaoqing Xu , Xiaodong Xu , Bin Zhu
发明人： Benjamin Davis , Eugene B. Grant, III , Shu-Chen Lin , Mark J. Macielag , Michele Ann Weidner-Wells , Xiaoqing Xu , Xiaodong Xu , Bin Zhu
IPC分类号： A61K31/5365 , C07D471/04 , A61K31/4375 , C07D401/04 , A61K31/4709 , C07D498/16
CPC分类号： C07D471/04 , C07D401/04 , C07D401/14 , C07D498/04 , C07D498/14 , C07D519/00
摘要： The present invention relates to compounds having a structure according to Formula (I) wherein n, m, z, R, R2, R3, R4, R5, R6, A, E, X, Y, a and b are as defined above; or an optical isomer, diastereomer or enantiomer thereof; a pharmaceutically acceptable salt, hydrate, or prodrug thereof.
摘要翻译：本发明涉及具有式（I）结构的化合物，其中n，m，z，R，R 2，R 3，R 4，R 5，R 6，A，E，X，Y，a和b如上所定义; 或其光学异构体，非对映异构体或对映异构体; 其药学上可接受的盐，水合物或前药。

6. 发明申请

US20090029980A1 C-7 Isoxazolinyl Quinolone / Naphthyridine Derivatives Useful as Antibacterial Agents 有权
标题翻译：用作抗菌剂的C-7异恶唑啉酮/萘啶衍生物
公开(公告)号：US20090029980A1
公开(公告)日：2009-01-29
申请号：US12180641
申请日：2008-07-28
申请人： Mark J. Macielag , Michele A. Weidner-Wells , Shu-Chen Lin
发明人： Mark J. Macielag , Michele A. Weidner-Wells , Shu-Chen Lin
IPC分类号： A61K31/5383 , A61K31/4375 , C07D471/04 , A61P31/04 , C07D498/04 , A61K31/4709
CPC分类号： C07D498/04 , C07D519/00
摘要： The present invention relates to C-7 isoxazolyl quinoline/naphthyridine derivatives useful as antimicrobial compounds, pharmaceutical compositions comprising said derivatives and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes.
摘要翻译：本发明涉及可用作抗微生物化合物的C-7异恶唑基喹啉/萘啶衍生物，包含所述衍生物的药物组合物以及所述衍生物和药物组合物作为抗病原微生物，特别是抗性微生物的抗微生物剂的用途。

7. 发明授权

US07179805B2 7-amino alkylidenyl-heterocyclic quinolones and naphthyridones 有权
标题翻译： 7-氨基亚烷基 - 杂环喹诺酮和萘啶酮
公开(公告)号：US07179805B2
公开(公告)日：2007-02-20
申请号：US10937238
申请日：2004-09-09
申请人： Eugene B. Grant, III , Mark J. Macielag , Xiaoqing Xu , Steven David Paget , Michele Ann Weidner-Wells
发明人： Eugene B. Grant, III , Mark J. Macielag , Xiaoqing Xu , Steven David Paget , Michele Ann Weidner-Wells
IPC分类号： A61K31/4353 , A61K31/5383 , C07D215/14 , C07D471/14 , C07D498/04
CPC分类号： C07D403/04 , C07D401/04 , C07D471/04
摘要： The present invention relates to compounds having a structure according to Formula I wherein n, m, z, R, R2, R3, R4, R5, R6, A, E, X, Y, a and b are as defined above; or an optical isomer, diastereomer or enantiomer thereof; a pharmaceutically acceptable salt, hydrate, or prodrug thereof.
摘要翻译：本发明涉及具有式I结构的化合物，其中n，m，z，R，R 2，R 3，R 4， R 5，R 6，A，E，X，Y，a和b如上所定义; 或其光学异构体，非对映异构体或对映异构体; 其药学上可接受的盐，水合物或前药。

8. 发明授权

US06818646B2 Substituted pyrrolopyridinone derivatives useful as phosphodiesterase inhibitors 有权
标题翻译：用作磷酸二酯酶抑制剂的取代的吡咯并吡喃酮衍生物
公开(公告)号：US06818646B2
公开(公告)日：2004-11-16
申请号：US10638901
申请日：2003-08-11
申请人： Zhihua Sui , Mark J. Macielag , Jihua Guan , Weigin Jiang , James C. Lanter
发明人： Zhihua Sui , Mark J. Macielag , Jihua Guan , Weigin Jiang , James C. Lanter
IPC分类号： A61K314965
CPC分类号： C07D471/04
摘要： The invention relates to novel pyrrolopyridinone derivatives of the formula (I) or (II): pharmaceutical compositions containing the compounds and their use for the treatment of sexual dysfunction.
摘要翻译：本发明涉及式（I）或（II）的新型吡咯并吡喃酮衍生物：含有化合物的药物组合物及其用于治疗性功能障碍的用途。

9. 发明授权

US06635638B2 Substituted pyrrolopyridinone derivatives useful as phosphodiesterase inhibitors 有权
标题翻译：用作磷酸二酯酶抑制剂的取代的吡咯并吡喃酮衍生物
公开(公告)号：US06635638B2
公开(公告)日：2003-10-21
申请号：US09847749
申请日：2001-05-02
申请人： Zhihua Sui , Mark J. Macielag , Jihua Guan , Weiqin Jiang , James C. Lanter
发明人： Zhihua Sui , Mark J. Macielag , Jihua Guan , Weiqin Jiang , James C. Lanter
IPC分类号： C07D47104
CPC分类号： C07D471/04
摘要： The invention relates to novel pyrrolopyridinone derivatives of the formula (I) or (II): pharmaceutical compositions containing the compounds and their use for the treatment of sexual dysfunction.
摘要翻译：本发明涉及式（I）或（II）的新型吡咯并吡喃酮衍生物：含有化合物的药物组合物及其用于治疗性功能障碍的用途。

10. 发明授权

US5734012A Cyclic motilin-like polypeptides with gastrointestinal motor stimulating activity 失效
标题翻译：循环促胃动素样多肽与胃肠运动刺激活性
公开(公告)号：US5734012A
公开(公告)日：1998-03-31
申请号：US648644
申请日：1996-05-16
申请人： Ramalinga Dharanipragada , Mark J. Macielag , Jung Kim-Dettelback , James Florance
发明人： Ramalinga Dharanipragada , Mark J. Macielag , Jung Kim-Dettelback , James Florance
IPC分类号： A61K38/00 , A61P1/00 , C07K14/63 , C07K5/12 , C07K7/00 , C07K7/08
CPC分类号： C07K14/63 , A61K38/00
摘要： This invention pertains to cyclic polypeptides having gastrointestinal motor stimulating activity which may be represented by formula (1): ##STR1## including optically active isomeric forms and the pharmaceutically acceptable acid addition salts thereof, wherein groups A and D are linked to from a cyclic structure; and R.sub.1 is lower alkyl; R.sub.2 is hydrogen or lower alkyl; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is phenyl or substituted phenyl, wherein the phenyl group may be substituted with one or more substituents selected from the group consisting of halogen, hydroxy, and lower alkoxy; R.sub.5 is --OH or --NH.sub.2 ; A is selected from the group consisting of L-glutamic acid, L-aspartic acid, L-lysine, L-ornithine, and L-2,4-diaminobutyric acid; B is L-alanine or L-glutamine; C is L-arginine or D-arginine; D is selected from the group consisting of L-lysine, L-ornithine, L-2,4-diaminobutyric acid, L-glutamic acid, and L-aspartic acid; E is a direct bond between group D and group R.sub.5 or is L-lysine or D-lysine; m is 0 or 1; the symbol * represents an asymmetric carbon atom which may be in the D or L configuration, with the proviso that: (a) when A is L-glutamic acid or L-aspartic acid, D is L-lysine, L-ornithine, or L-2,4-diaminobutyric acid; and (b) when A is L-lysine, L-ornithine, or L-2,4-diaminobutyric acid, D is L-glutamic acid or L-aspartic acid. This invention also pertains to methods for using the novel cyclic polypeptides.
摘要翻译：本发明涉及具有胃肠运动刺激活性的环状多肽，其可以由式（1）表示：（1）包括旋光异构体形式及其药学上可接受的酸加成盐，其中基团A和D与循环结构; 且R 1为低级烷基; R2是氢或低级烷基; R3是氢或低级烷基; R4是苯基或取代的苯基，其中苯基可以被一个或多个选自卤素，羟基和低级烷氧基的取代基取代; R5是-OH或-NH2; A选自L-谷氨酸，L-天冬氨酸，L-赖氨酸，L-鸟氨酸和L-2,4-二氨基丁酸; B是L-丙氨酸或L-谷氨酰胺; C是L-精氨酸或D-精氨酸; D选自L-赖氨酸，L-鸟氨酸，L-2,4-二氨基丁酸，L-谷氨酸和L-天冬氨酸; E是D组和R5组之间的直接键，或是L-赖氨酸或D-赖氨酸; m为0或1; 符号*表示可以是D或L构型的不对称碳原子，条件是：（a）当A是L-谷氨酸或L-天冬氨酸时，D是L-赖氨酸，L-鸟氨酸或 L-2,4-二氨基丁酸; 和（b）当A是L-赖氨酸，L-鸟氨酸或L-2,4-二氨基丁酸时，D是L-谷氨酸或L-天冬氨酸。本发明还涉及使用新型环状多肽的方法。

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