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1. 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。

2. 发明授权

US5470830A Motilin-like polypeptides that inhibit gastrointestinal motor activity 失效
公开(公告)号：US5470830A
公开(公告)日：1995-11-28
申请号：US103489
申请日：1993-08-06
申请人： Mark J. Macielag , Ramalinga Dharanipragada , Mary S. Marvin
发明人： Mark J. Macielag , Ramalinga Dharanipragada , Mary S. Marvin
IPC分类号： C07K7/04 , A61K38/00 , A61P1/00 , C07K14/575 , C07K14/63 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07K14/63 , A61K38/00
摘要： This invention pertains to polypeptides having gastrointestinal motor inhibitory activity represented by the formula: ##STR1## including optically active isomeric forms and the pharmaceutically acceptable acid addition salts thereof wherein A is the L-stereoisomer of a lipophilic aliphatic or alicyclic amino acid; B is selected from the group consisting of L and D aromatic, heteroaromatic, lipophilic aliphatic, and alicyclic amino acids; D is the L-stereoisomer of a lipophilic aliphatic or alicyclic amino acid; E is the L-stereoisomer of an aromatic, aliphatic, or alicyclic amino acid; F is the L-stereoisomer of an aromatic or heteroaromatic amino acid; G is glycine or D-alanine; H is L-glutamic acid or L-glutamine; I is L-glutamine, L-glutamic acid, or L-alanine; J is a direct bond between I and group --NH-- or is selected from the group consisting of Z, Z-Leu, Z-Leu-Gln, Z-Leu-Gln-Glu (SEQ ID NO:2), Z-Leu-Gln-Glu-Lys (SEQ ID NO:3), Zleu-Gln-Glu-Lys-Glu (SEQ ID NO:4), Z-Leu-Gln-Glu-Lys-Glu-Arg (SEQ ID NO:5), ZLeu-Gln-Glu-Lys-Glu-Arg-Asn (SEQ ID NO:6), Z-Leu-Gln-Glu-Lys-Glu-Arg-AsnLys (SEQ ID NO:7), and Z-Leu-Gln-Glu-Lys-Glu-Arg-Asn-Lys-Gly (SEQ ID NO:8), wherein Z is selected from the group consisting of arginine, D-arginine, D-homoarginine, D-lysine, D-ornithine, D-2,4-diaminobutyric acid, D-glutamine, D-asparagine, and D-alanine; R.sub.1 and R.sub.2 are independently hydrogen or lower alkyl; R.sub.3 is selected from the group consisting of lower-alkyl, cycloalkyl, substituted and unsubstituted aryl, and heteroaryl, wherein the aryl group may be substituted with one or more substituents selected from the group consisting of halogen, hydroxy, and lower-alkoxy; R.sub.4 is selected from the group consisting of --CH.sub.2 CONH.sub.2, aminoalkyl groups containing from 1 to 3 carbon atoms, and guanidinoalkyl groups containing 2 or 3 carbon atoms; R.sub.5 is --COOH or --CONH.sub.2 ; and the symbol * represents an asymmetric carbon atom which may be in the D or L configuration, and each lower-alkyl group contains from 1 to 4 carbon atoms, with the proviso that R.sub.4 is --CH.sub.2 CONH.sub.2 only when J is Z-Leu or Z-Leu-Gln-Glu-Lys-Glu-Arg-Asn-Lys-Gly (SEQ ID NO:8).

3. 发明授权

US5422341A Motilin-like polypeptides with gastrointestinal motor stimulating activity 失效
标题翻译：胃肠道运动刺激活性的胃动素样多肽
公开(公告)号：US5422341A
公开(公告)日：1995-06-06
申请号：US103490
申请日：1993-08-06
申请人： Mark J. Macielag , Ramalinga Dharanipragada , James R. Florance , Mary S. Marvin , Alphonse Galdes
发明人： Mark J. Macielag , Ramalinga Dharanipragada , James R. Florance , Mary S. Marvin , Alphonse Galdes
IPC分类号： C07K7/04 , A61K38/00 , A61P3/00 , A61P3/02 , C07K14/575 , C07K14/63 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07K14/63 , A61K38/00
摘要： This invention pertains to polypeptides, other than motilin, having gastrointestinal motor stimulating activity and represented by the formula: ##STR1## wherein A and D are lipophilic aliphatic or alicyclic amino acids; B is L-proline or L-alanine; E is an aromatic, lipophilic aliphatic, or alicyclic amino acid; F is an aromatic or heteroaromatic amino acid; G is glycine or D-alanine; H is L-glutamic acid or L-glutamine; I is L-glutamine, L-glutamic acid, or L-alanine; J is a direct bond or is selected from, inter alia Z, Z-Leu, Z-Leu-Gln, Z-Leu-Gln-Glu (SEQ ID NO:2) or Z-Leu-Gln-Glu-Lys (SEQ ID NO:3), wherein Z is, inter alia, arginine, D-arginine, D-homoarginine, or D-lysine, and further wherein the amino acids represented by A, D, E and F are L-stereoisomers; R.sub.1 is lower-alkyl or allyl; R.sub.2 is hydrogen, lower-alkyl, propargyl, or allyl; R.sub.3 is hydrogen, lower-alkyl, and allyl; R.sub.4 is lower-alkyl, cycloalkyl, heteroaryl, unsubstituted aryl, and aryl substituted by halogen, hydroxy, or lower-alkoxy; R.sub.5 is --CH.sub.2 CONH.sub.2, aminoalkyl, or guanidinoalkyl; R.sub.6 is --COOH or --CONH.sub.2 ; and m is 0 or 1, and the asymmetric carbon represented by * may be D or L configuration, with certain specified provisos.
摘要翻译：本发明涉及具有胃肠运动刺激活性并由下式表示的除胃动素以外的多肽：其中A和D是亲脂性脂族或脂环族氨基酸; B是L-脯氨酸或L-丙氨酸; E是芳族，亲脂性脂族或脂环族氨基酸; F是芳族或杂芳族氨基酸; G是甘氨酸或D-丙氨酸; H是L-谷氨酸或L-谷氨酰胺; 我是L-谷氨酰胺，L-谷氨酸或L-丙氨酸; J是直接键或选自Z，Z-Leu，Z-Leu-Gln，Z-Leu-Gln-Glu（SEQ ID NO：2）或Z-Leu-Gln-Glu-Lys（SEQ 其中Z特别是精氨酸，D-精氨酸，D-高精氨酸或D-赖氨酸，其中由A，D，E和F表示的氨基酸是L-立体异构体; R1是低级烷基或烯丙基; R2是氢，低级烷基，炔丙基或烯丙基; R3是氢，低级烷基和烯丙基; R4是低级烷基，环烷基，杂芳基，未取代的芳基和被卤素，羟基或低级烷氧基取代的芳基; R5是-CH2CONH2，氨基烷基或胍基烷基; R6是-COOH或-CONH 2; 并且m为0或1，并且由*表示的不对称碳可以是D或L构型，具有特定的条件。

4. 发明授权

US08809327B2 Sulfonamides as TRPM8 modulators 有权
标题翻译：磺酰胺作为TRPM8调节剂
公开(公告)号：US08809327B2
公开(公告)日：2014-08-19
申请号：US13407251
申请日：2012-02-28
申请人： Shawn T. Branum , Raymond W. Colburn , Scott L. Dax , Christopher M. Flores , Michele C. Jetter , Yi Liu , Donald Ludovici , Mark J. Macielag , Jay M. Matthews , James J. McNally , Laura M. Reaney , Ronald K. Russell , Ning Qin , Christopher Teleha , Kenneth M. Wells , Scott C. Youells , Mark A. Youngman
发明人： Shawn T. Branum , Raymond W. Colburn , Scott L. Dax , Christopher M. Flores , Michele C. Jetter , Yi Liu , Donald Ludovici , Mark J. Macielag , Jay M. Matthews , James J. McNally , Laura M. Reaney , Ronald K. Russell , Ning Qin , Christopher Teleha , Kenneth M. Wells , Scott C. Youells , Mark A. Youngman
IPC分类号： A61K31/381 , A61K31/541 , A61K31/4709 , A61K31/5377 , A61P29/02
CPC分类号： C07D333/66 , C07D333/36 , C07D409/12 , C07D409/14 , C07D417/12 , C07D495/04
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 A, B, G, Y, R1, R2, R3, and R4 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A，B，G，Y，R 1，R 2，R 3和R 4在本文中定义。

5. 发明授权

US08637498B2 Oxopiperazine-azetidine amides and oxodiazepine-azetidine amides as monoacylglycerol lipase inhibitors 失效
标题翻译：氧基哌嗪 - 氮杂环丁烷酰胺和氧代二氮杂吖啶啶酰胺作为单酰基甘油脂肪酶抑制剂
公开(公告)号：US08637498B2
公开(公告)日：2014-01-28
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： A61K31/496 , A61K31/506 , A61K31/551 , C07D403/04 , C07D403/14 , C07D409/14 , C07D417/14
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。这样的化合物和对映体，非对映异构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。

6. 发明申请

US20130102584A1 PIPERIDIN-4-YL-AZETIDINE DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS 有权
标题翻译：哌可啶-4-Y-AZETIDINE DIAMIDES作为单羟乙基脂肪酶抑制剂
公开(公告)号：US20130102584A1
公开(公告)日：2013-04-25
申请号：US13277702
申请日：2011-10-20
申请人： Peter J. Connolly , Haiyan Bian , Xun Li , Li Liu , Mark J. Macielag , Mark E. McDonnell
发明人： Peter J. Connolly , Haiyan Bian , Xun Li , Li Liu , Mark J. Macielag , Mark E. McDonnell
IPC分类号： A61K31/454 , A61P25/00 , A61P25/06 , C07D417/14
CPC分类号： 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 (I) as follows: wherein Y, Z, and R 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。这样的化合物和对映体，非对映异构体及其药学上可接受的盐由式（I）表示如下：其中Y，Z和R在本文中定义。

7. 发明申请

US20110105527A1 PYRAZINES AS DELTA OPIOID RECEPTOR MODULATORS 有权
标题翻译： PYRAZINES as DELTA OPIOID RECEPTOR MODULATORS
公开(公告)号：US20110105527A1
公开(公告)日：2011-05-05
申请号：US12913917
申请日：2010-10-28
申请人： PETER J. CONNOLLY , Shu-Chen Lin , Mark J. Macielag , Yue-Mei Zhang
发明人： PETER J. CONNOLLY , Shu-Chen Lin , Mark J. Macielag , Yue-Mei Zhang
IPC分类号： A61K31/4965 , C07D401/14 , C07D401/02 , A61P19/02 , A61P25/06 , A61P25/00 , A61P29/00 , A61P17/02 , A61P17/00 , A61P3/10 , A61P1/00 , A61P15/00 , A61P35/00 , A61P25/16 , A61P25/28 , A61P25/24 , A61P25/30 , A61P13/02
CPC分类号： C07D401/14 , C07D403/14
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, L, X, 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，L，X和Y如本文所定义。

8. 发明申请

US20110003800A1 BENZIMIDAZOLE DERIVATIVES USEFUL AS TRPM8 CHANNEL MODULATORS 有权
公开(公告)号：US20110003800A1
公开(公告)日：2011-01-06
申请号：US12797712
申请日：2010-06-10
申请人： Mark J. Macielag , Mingde Xia , Xiaoqing Xu
发明人： Mark J. Macielag , Mingde Xia , Xiaoqing Xu
IPC分类号： A61K31/5383 , C07D235/30 , C07D498/06 , A61K31/4184 , A61P9/12 , A61P9/00 , A61P25/04 , A61P29/00
CPC分类号： A61K31/5383 , A61K31/4184 , C07D233/52 , 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.

9. 发明申请

US20080234347A1 METHOD FOR TREATING CB2 RECEPTOR MEDIATED PAIN 审中-公开
标题翻译：用于治疗CB2受体介导的疼痛的方法
公开(公告)号：US20080234347A1
公开(公告)日：2008-09-25
申请号：US12038029
申请日：2008-02-27
申请人： Mingde Xia , Mark J. Macielag , Christopher M. Flores , Kevin Paul Pavlick
发明人： Mingde Xia , Mark J. Macielag , Christopher M. Flores , Kevin Paul Pavlick
IPC分类号： A61K31/416 , A61P29/00
CPC分类号： A61K31/415 , A61K31/416
摘要： The present invention is directed to a method for treating, ameliorating or preventing CB2 receptor mediated pain in a subject in need thereof comprising administering to the subject an effective amount of a compound of formula (I): or a form thereof, wherein X1R1, X2R2, X3R3, X4R4 and X5R5 are as defined herein.
摘要翻译：本发明涉及一种用于治疗，改善或预防有需要的受试者的CB2受体介导的疼痛的方法，其包括向所述受试者施用有效量的式（I）化合物或其形式，其中X

10. 发明申请

US20080070968A1 Hexahydro-Cycloheptapyrazole Cannabinoid Modulators 失效
标题翻译：六氢环庚三烯大麻素调节剂
公开(公告)号：US20080070968A1
公开(公告)日：2008-03-20
申请号：US11688552
申请日：2007-03-20
申请人： Fina Liotta , Mingde Xia , Huajun Lu , Meng Pan , Michael P. Wachter , Mark J. Macielag
发明人： Fina Liotta , Mingde Xia , Huajun Lu , Meng Pan , Michael P. Wachter , Mark J. Macielag
IPC分类号： A61K31/415 , A61P29/00 , C07D231/00
CPC分类号： C07D231/54 , C07D403/04
摘要： This invention is directed to a hexahydro-cycloheptapyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.
摘要翻译：本发明涉及式（I）的六氢 - 环庚三唑大麻素调节剂化合物：以及用于治疗，改善或预防大麻素受体介导的综合征，病症或疾病的方法。

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