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11. 发明授权

US06479482B2 Alkylamine derivatives of dihydropyridine NPY antagonists 有权
标题翻译：二氢吡啶NPY拮抗剂的烷基胺衍生物
公开(公告)号：US06479482B2
公开(公告)日：2002-11-12
申请号：US09852983
申请日：2001-05-10
申请人： Graham S. Poindexter , Marc Bruce , Sing-Yuen Sit , Scott W. Martin
发明人： Graham S. Poindexter , Marc Bruce , Sing-Yuen Sit , Scott W. Martin
IPC分类号： C07D41714
CPC分类号： C07D401/12 , C07D211/90
摘要： A series of non-peptidergic antagonists of NPY have been synthesized and are comprises of amino and piperazine derivatives of 4-phenyl-1,4-dihydropyridines of Formula 1. where X is CH or N As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
摘要翻译：已经合成了一系列NPY的非肽能拮抗剂，其由式1的4-苯基-1,4-二氢吡啶的氨基和哌嗪衍生物组成。其中X是NPY诱导行为的CH或NAs拮抗剂，这些化合物是预期在促进减肥和治疗进食障碍中起到有效的厌氧剂的作用。

12. 发明授权

US6054590A Imidazolone anorectic agents: II. phenyl derivatives 失效
标题翻译：咪唑安定食物：二。苯基衍生物
公开(公告)号：US6054590A
公开(公告)日：2000-04-25
申请号：US261670
申请日：1999-03-03
申请人： Graham S. Poindexter , Ildiko Antal , Leah M. Giupponi , Robert H. Stoffel , Kevin Gillman , Mendi Higgins
发明人： Graham S. Poindexter , Ildiko Antal , Leah M. Giupponi , Robert H. Stoffel , Kevin Gillman , Mendi Higgins
IPC分类号： A61K31/4164 , A61K31/4166 , A61K31/4178 , A61K31/4192 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/541 , A61P3/04 , A61P43/00 , C07D233/70 , C07D233/72 , C07D233/74 , C07D233/76 , C07D233/78 , C07D233/84 , C07D233/86 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/10 , C07D233/32 , C07D233/48
CPC分类号： A61K31/4174 , A61K31/4166 , A61K31/4178 , C07D233/70 , C07D233/74 , C07D233/76 , C07D233/78 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/06 , C07D409/06
摘要： A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of phenyl derivatives of imidazolone compounds of Formula I. ##STR1## As antagonists of NPY-induced feeding behavior, these compounds and known analogs are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
摘要翻译：已经合成了一系列NPY的非肽能拮抗剂，并且由式I的咪唑啉酮化合物的苯基衍生物组成。作为NPY诱导的进食行为的拮抗剂，这些化合物和已知的类似物被期望作为促进重量的有效的厌氧剂损失和治疗饮食失调。

13. 发明授权

US5889016A Dihydropyrimidone derivatives as NPY antagonists 失效
标题翻译：作为NPY拮抗剂的二氢嘧啶酮衍生物
公开(公告)号：US5889016A
公开(公告)日：1999-03-30
申请号：US9534
申请日：1998-01-20
申请人： Marc A. Bruce , Graham S. Poindexter , Graham Johnson
发明人： Marc A. Bruce , Graham S. Poindexter , Graham Johnson
IPC分类号： C07D401/12 , A61K31/505
CPC分类号： C07D401/12
摘要： The present invention provides a series of non-peptidergic antagonists of NPY comprising piperidine derivatives of 4-phenyl-1,4-dihydropyrimidinones of the Formula I ##STR1## wherein R, R.sup.1 and R.sup.2 are defined herein. As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
摘要翻译：本发明提供了一系列包含式I的4-苯基-1,4-二氢嘧啶酮的哌啶衍生物的NPY的非肽能拮抗剂，其中R，R 1和R 2在本文中定义。作为NPY诱导的饲养行为的拮抗剂，预期这些化合物可用作促进减肥和治疗进食障碍的有效厌氧剂。

14. 发明授权

US5554621A Dihydropyridine NPY antagonists: nitrogen heterocyclic derivatives 失效
标题翻译：二氢吡啶NPY拮抗剂：氮杂环衍生物
公开(公告)号：US5554621A
公开(公告)日：1996-09-10
申请号：US482354
申请日：1995-06-07
申请人： Graham S. Poindexter , Marc Bruce , Graham Johnson , Karen LeBoulluec , Jeffrey W. Noonan
发明人： Graham S. Poindexter , Marc Bruce , Graham Johnson , Karen LeBoulluec , Jeffrey W. Noonan
IPC分类号： A61K31/4427 , A61K31/455 , A61K31/47 , A61P1/00 , A61P3/04 , A61P25/00 , A61P43/00 , C07D401/12 , C07D413/14 , A61K31/16 , A61K31/17 , C07D401/10
CPC分类号： C07D401/12
摘要： A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of nitrogen heterocyclic derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I). ##STR1## As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
摘要翻译：已经合成了一系列NPY的非肽能拮抗剂，其由式（I）的4-苯基-1,4-二氢吡啶的氮杂环衍生物组成。（I）作为NPY诱导的摄食行为的拮抗剂，预期这些化合物可用作促进减肥和治疗饮食失调的有效厌氧剂。

15. 发明授权

US4814455A Dihydro-3,5-dicarboxylates 失效
标题翻译：二氢-3,5-二羧酸二乙酯
公开(公告)号：US4814455A
公开(公告)日：1989-03-21
申请号：US852856
申请日：1986-04-16
申请人： Graham S. Poindexter
发明人： Graham S. Poindexter
IPC分类号： A61K31/435 , A61K31/4427 , A61K31/455 , A61P7/02 , A61P9/08 , A61P9/10 , A61P9/12 , C07D211/90 , C07D401/12
CPC分类号： C07D401/12 , C07D211/90
摘要： A series of compounds of the 1,4-dihydropyridine class with a 3-carboxylate group linked to an alkyleneaminoalkylene heteroatom have been prepared possessing the general formula ##STR1## wherein R.sup.2, R.sup.5 and R.sup.6 are independently selected from lower (C.sub.1-4)alkyl, hydroxy-lower-alkylene, lower alkoxy-lower-alkylene, lower alkylamino-lower-alkylene or lower dialkyl-amino-lower-alkylene; R.sup.7 is selected from hydrogen, lower alkyl, phenyl-lower-alkylene, or phenylthio-lower-alkylene; n is the integer 2 or 3; X is a chemical bond, --O--, --S--, ##STR2## or --NR.sup.9 -- wherein R.sup.9 is hydrogen, lower alkyl, phenyl, or phenyl-lower-alkylene with the proviso that when X is a chemical bond, Z is a 3-indolyl ring; and Z is selected from the group consisting of phenyl substituted with 1 to 3 substituents independently chosen from among hydrogen, lower alkyl, or lower alkoxy, phenyl-lower-alkylene, or 3-indolyl.Compounds of this series possess calcium channel blocking properties, afford protection against ischemia and inhibit aggregation of blood platelets.
摘要翻译：已经制备了一系列具有与亚烷基氨基亚烷基杂原子连接的3-羧酸酯基的1,4-二氢吡啶类的化合物，其具有通式“IMAGE”，其中R 2，R 5和R 6独立地选自低级（C 1-4）烷基，羟基 - 低级 - 亚烷基，低级烷氧基 - 低级 - 亚烷基，低级烷基氨基 - 低级 - 亚烷基或低级二烷基 - 氨基 - 低级 - 亚烷基; R 7选自氢，低级烷基，苯基 - 低级亚烷基或苯硫基 - 低级 - 亚烷基; n是整数2或3; 其中R为氢，低级烷基，苯基或苯基 - 低级亚烷基，条件是当X为化学键时，Z为化学键，-O - ， - S-， 3-吲哚基环; 并且Z选自被1至3个独立地选自氢，低级烷基或低级烷氧基，苯基 - 低级亚烷基或3-吲哚基的取代基取代的苯基。该系列化合物具有钙通道阻断性质，提供防止缺血和抑制血小板聚集的保护作用。

16. 发明授权

US06979691B2 Compounds useful as modulators of melanocortin receptors and pharmaceutical compositions comprising same 有权
标题翻译：可用作黑皮质素受体调节剂的化合物和包含其的药物组合物
公开(公告)号：US06979691B2
公开(公告)日：2005-12-27
申请号：US10090582
申请日：2002-03-04
申请人： Guixue Yu , John Macor , Timothy Herpin , R. Michael Lawrence , George C. Morton , Rejean Ruel , Graham S. Poindexter , Edward H. Ruediger , Carl Thibault
发明人： Guixue Yu , John Macor , Timothy Herpin , R. Michael Lawrence , George C. Morton , Rejean Ruel , Graham S. Poindexter , Edward H. Ruediger , Carl Thibault
IPC分类号： C07D233/64 , A61K31/4178 , A61K31/438 , A61K31/451 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/4747 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/527 , A61K31/537 , A61K31/5377 , A61K31/5415 , A61K31/55 , A61K38/00 , A61P1/00 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/02 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/14 , A61P5/16 , A61P7/00 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/02 , A61P11/06 , A61P11/08 , A61P13/12 , A61P15/00 , A61P15/08 , A61P15/10 , A61P17/00 , A61P17/04 , A61P17/06 , A61P17/14 , A61P17/16 , A61P19/02 , A61P19/10 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/06 , A61P31/18 , A61P31/20 , A61P33/06 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D211/32 , C07D211/34 , C07D211/58 , C07D211/60 , C07D211/62 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/10 , C07D487/04 , C07D491/10 , C07D495/04 , C07D498/10 , C07K5/06 , C07K5/078 , A61K31/445
CPC分类号： C07D401/12 , A61K38/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/10 , C07D487/04 , C07D491/10 , C07D495/04 , C07K5/06139 , C07K5/06191 , Y02A50/411 , Y02A50/463
摘要： Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates and prodrugs thereof, in which E is X is N or CH, W is —NR16R17, —NR16C(═O)R22, —NR16CO2R22, —OR23, or a heteroaryl or heterocyclo group as defined in the specification, and R1 through R12, R16, R17, R22, R23, x, y, and z are as defined in the specification, are useful as modulaters of melanocortin receptors, particularly MC-1R and MC-4R.
摘要翻译：具有式（I）的化合物及其药学上可接受的盐，水合物和前药，其中E是X是N或CH，W是-NR 16 R 17，，-NR 16 C（-O）R 22，-NR 16 CO 2 R 22 或者如说明书中定义的杂芳基或杂环基，R 1至R 12，R 12， R 17，R 17，R 22，R 23，x，y和z定义如上说明书可用作黑皮质素受体的调节剂，特别是MC-1R和MC-4R。

17. 发明授权

US06713487B2 Compounds useful as modulators of melanocortin receptors and pharmaceutical compositions comprising same 有权
标题翻译：可用作黑皮质素受体调节剂的化合物和包含其的药物组合物
公开(公告)号：US06713487B2
公开(公告)日：2004-03-30
申请号：US10090288
申请日：2002-03-04
申请人： Guixue Yu , John Macor , Timothy Herpin , R. Michael Lawrence , George C. Morton , Rejean Ruel , Graham S. Poindexter , Edward H. Ruediger , Carl Thibault
发明人： Guixue Yu , John Macor , Timothy Herpin , R. Michael Lawrence , George C. Morton , Rejean Ruel , Graham S. Poindexter , Edward H. Ruediger , Carl Thibault
IPC分类号： A61K31445
CPC分类号： C07D401/12 , A61K38/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/10 , C07D487/04 , C07D491/10 , C07D495/04 , C07K5/06139 , C07K5/06191 , Y02A50/411 , Y02A50/463
摘要： Compounds having the formula (I), —NR11R12; G is a novel side chain selected from C2-6alkenyl, A3-aryl, —OR18, heteroaryl, A1-cyano, A2—OR17, A1—C(═O)R18, A1—CO2R18, A1—C(═O)NR18R19, A1—OC(═O)R18, A1—NR18C(═O)R19, A1—OC(═O)NR18R19, A1—NR18CO2R19, A1—NR18SO2R17, A1—SO2R17, A1—NR20C(═O)NR18R19, and A1—SR18; or when y is 0 or when W is not NHR22, G may be A1-heterocyclo, wherein A1 is a bond, C1-6alkylene or C2-alkenylene, A2 is C1-6alkylene or C2-6alkenylene, and A3 is C2-6alkenylene; W is selected from —NR21R22, —OR23, —NR21C(═O)R24, —NR21CO2R24, amidino, guanidino, or a heteroaryl, heterocyclo or C3-7cycloalkyl as defined in the specification, and X and R1 through R24 are as defined in the specification, are effective as modulators of melanocortin-receptors, particularly MC-1R and MC-4R.
摘要翻译：具有式（I），-NR 11 R 12的化合物; G是选自C2-6烯基，A3-芳基，-OR18，杂芳基，A1-氰基，A2-OR17，A1-C（= O）R18，A1-CO2R18，A1-C（= O）NR18R19 ，A1-OC（= O）R18，A1-NR18C（= O）R19，A1-OC（= O）NR18R19，A1-NR18CO2R19，A1-NR18SO2R17，A1-SO2R17，A1-NR20C（= O）NR18R19和 A1-SR18; 或当y为0或W不为NHR22时，G可为A1-杂环，其中A1为C1-6亚烷基或C2-亚烯基，A2为C1-6亚烷基或C2-6亚烯基，A3为C2-6亚烯基; W选自-NR 21 R 22，-OR 23，-NR 21 C（= O）R 24，-NR 21 CO 2 R 24，脒基，胍基或如说明书中定义的杂芳基，杂环或C 3-7环烷基，X和R 1至R 24如该说明书作为黑皮质素受体，特别是MC-1R和MC-4R的调节剂是有效的。

18. 发明授权

US6096745A Imidazolone anorectic agents: III. heteroaryl derivatives 有权
标题翻译：咪唑酮厌食症药：三。杂芳基衍生物
公开(公告)号：US6096745A
公开(公告)日：2000-08-01
申请号：US261658
申请日：1999-03-03
申请人： Graham S. Poindexter , Kevin Gillman
发明人： Graham S. Poindexter , Kevin Gillman
IPC分类号： A61K31/4164 , A61K31/4166 , A61K31/4178 , A61K31/4192 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/541 , A61P3/04 , A61P43/00 , C07D233/70 , C07D233/72 , C07D233/74 , C07D233/76 , C07D233/78 , C07D233/84 , C07D233/86 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/10 , C07D239/24 , C07D241/10
CPC分类号： A61K31/4174 , A61K31/4166 , A61K31/4178 , C07D233/70 , C07D233/74 , C07D233/76 , C07D233/78 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/06 , C07D409/06
摘要： A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of heteroaryl derivatives of imidazolone compounds of Formula 1. ##STR1## As antagonists of NPY-induced feeding behavior, these compounds and known analogs are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
摘要翻译：已经合成了一系列NPY的非肽能拮抗剂，并且由式1的咪唑啉酮化合物的杂芳基衍生物组成。作为NPY诱导的进食行为的拮抗剂，这些化合物和已知的类似物被期望作为促进重量的有效的厌氧剂损失和治疗饮食失调。

19. 发明授权

US6001836A Dihydropyridine NPY antagonists: cyanoguanidine derivatives 失效
标题翻译：二氢吡啶NPY拮抗剂：氰胍衍生物
公开(公告)号：US6001836A
公开(公告)日：1999-12-14
申请号：US84692
申请日：1998-05-26
申请人： Graham S. Poindexter , R. Thomas Swann , Marc A. Bruce , Mendi A. Morton , Yazhong Huang , Sing-Yuen Sit , James Guy Breitenbucher
发明人： Graham S. Poindexter , R. Thomas Swann , Marc A. Bruce , Mendi A. Morton , Yazhong Huang , Sing-Yuen Sit , James Guy Breitenbucher
IPC分类号： C07D211/90 , C07D401/14 , C07D401/10 , A61K31/445
CPC分类号： C07D211/90 , C07D401/14
摘要： A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of cyanoguanidine derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I). ##STR1## As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
摘要翻译：已经合成了一系列NPY的非肽能拮抗剂，其由式（I）的4-苯基-1,4-二氢吡啶的氰基胍衍生物组成。作为NPY诱导的饲养行为的拮抗剂，预期这些化合物可用作促进减肥和治疗进食障碍的有效厌氧剂。

20. 发明授权

US5677328A Ethylamino carbazole melatonergic agents 失效
标题翻译：乙基氨基咔唑褪黑激素药
公开(公告)号：US5677328A
公开(公告)日：1997-10-14
申请号：US741485
申请日：1996-10-30
申请人： Katherine S. Takaki , Marc A. Bruce , Graham S. Poindexter , Brett T. Watson , Joseph P. Yevich
发明人： Katherine S. Takaki , Marc A. Bruce , Graham S. Poindexter , Brett T. Watson , Joseph P. Yevich
IPC分类号： A61K31/40 , A61K31/403 , A61P25/20 , A61P43/00 , C07D209/88
CPC分类号： C07D209/88
摘要： Novel substituted carbazole compounds of Formula I are active as melatonergic agents: ##STR1## wherein: R.sub.1 is C(O)R.sub.3 or SO.sub.2 R.sub.4 ; R.sub.2 is H or C.sub.1-6 alkoxy; R.sub.3 is C.sub.1-6 alkyl, (CH.sub.2).sub.n SR.sub.4, (CH.sub.2).sub.n OR.sub.4, (CH.sub.2).sub.n SO.sub.2 R.sub.4, or NHR.sub.4 ; R.sub.4 is C.sub.1-4 alkyl; and m is 1 or 2; and n is 1 to 4.
摘要翻译：式I的新型取代的咔唑化合物作为褪黑激素作用是有活性的：其中：R 1是C（O）R 3或SO 2 R 4; R2为H或C1-6烷氧基; R3是C1-6烷基，（CH2）nSR4，（CH2）nOR4，（CH2）nSO2R4或NHR4; R4是C1-4烷基; m为1或2; n为1〜4。

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