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1. 发明授权

US6063934A Imidazolone anorectic agents: 1. 2-substituted-3,5-dihydro-5,5-diphenyl-4H-imidazol-4-ones 失效
标题翻译：咪唑酮厌食剂：1,1-取代-3,5-二氢-5,5-二苯基-4H-咪唑-4-酮
公开(公告)号：US6063934A
公开(公告)日：2000-05-16
申请号：US261374
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 , C07D233/30 , A61K31/415 , C07D233/32
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 acyclic 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无环衍生物组成。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。

2. 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。

3. 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。

4. 发明授权

US06916812B2 Alpha-aminoamide derivatives as melanocortin agonists 有权
标题翻译： α-氨基酰胺衍生物作为黑皮质素激动剂
公开(公告)号：US06916812B2
公开(公告)日：2005-07-12
申请号：US10264709
申请日：2002-10-04
申请人： Graham S. Poindexter , Guanglin Luo , Ling Chen
发明人： Graham S. Poindexter , Guanglin Luo , Ling Chen
IPC分类号： A61K31/496 , A61K31/5377 , A61K31/55 , A61K31/551 , C07D209/14 , C07D209/86 , C07D213/64 , C07D215/12 , C07D243/08 , C07D295/185 , C07D307/52 , C07D307/91 , C07D317/62 , C07D327/08 , C07D333/20 , C07D333/22 , C07D333/58 , C07D333/76 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , A61K31/495 , C07D295/192 , C07D405/10 , C07D409/10
CPC分类号： C07D213/64 , A61K31/496 , A61K31/5377 , A61K31/55 , A61K31/551 , C07D209/14 , C07D209/86 , C07D215/12 , C07D243/08 , C07D295/185 , C07D307/52 , C07D307/91 , C07D317/62 , C07D327/08 , C07D333/20 , C07D333/22 , C07D333/58 , C07D333/76 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06
摘要： Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of the melanocortin receptors. The compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders such as obesity, diabetes, and sexual dysfunction.
摘要翻译：新型哌嗪和高哌嗪衍生物是黑皮质素受体的激动剂，并且可用于治疗，控制或预防对黑皮质素受体的活化有反应的疾病和病症。因此，本发明的化合物可用于治疗或预防疾病和障碍，例如肥胖症，糖尿病和性功能障碍。

5. 发明授权

US4895846A Pharmaceutically useful dihydropyridinyldicarboxylate amides and esters incorporating arylpiperazinylalkyl moieties 失效
标题翻译：药学上有用的二氢吡啶基二羧酸酯酰胺和加入芳基哌嗪基烷基部分的酯
公开(公告)号：US4895846A
公开(公告)日：1990-01-23
申请号：US134715
申请日：1987-12-18
申请人： Graham S. Poindexter , Davis L. Temple, Jr.
发明人： Graham S. Poindexter , Davis L. Temple, Jr.
IPC分类号： C07C205/56 , C07D209/18 , C07D211/90 , C07D213/55 , C07D213/70 , C07D271/12 , C07D285/14 , C07D295/088 , C07D307/54 , C07D333/24 , C07D401/12
CPC分类号： C07D213/70 , C07C205/56 , C07D209/18 , C07D211/90 , C07D213/55 , C07D271/12 , C07D285/14 , C07D295/088 , C07D307/54 , C07D333/24 , C07D401/12
摘要： A series of 1,4-dihydropyridin-3,5-yl dicarboxylic acid amides and esters incorporating an arylpiperazinylalkyl moiety have been prepared possessing the general formula ##STR1## wherein R.sup.4 is cycloalkyl, aryl or hetaryl, generally with electron-withdrawing substituents; R.sup.2 and R.sup.6 are lower alkyl, alkanol, alkoxyalkyl, or alkylaminoalkyl; R.sup.5 is R.sup.2 or arylpiperazinylalkyl; X is O or NH; Y is lower alkylene, alkoxyalkylene, alkylaminoalkylene; and Z is phenyl, substituted pheny, pyridinyl, substituted pyridinyl, or pyrimidinyl. Compounds of this series demonstrate activity as calcium and alpha-adrenergic blockers in in vitro testing and antihypertensive, anti-ischemic, and platelet function inhibiting actions in in vivo screens.
摘要翻译：制备了具有芳基哌嗪基烷基部分的一系列1,4-二氢吡啶-3,5-基二羧酸酰胺和具有芳基哌嗪基烷基部分的酯，其具有通式为：其中R 4是环烷基，芳基或杂芳基，通常具有吸电子取代基; R2和R6是低级烷基，链烷醇，烷氧基烷基或烷基氨基烷基; R5是R2或芳基哌嗪基烷基; X是O或NH; Y是低级亚烷基，烷氧基亚烷基，烷基氨基亚烷基; Z是苯基，取代的苯基，吡啶基，取代的吡啶基或嘧啶基。该系列的化合物在体内筛选中体外测试和抗高血压，抗缺血和血小板功能抑制作用中表现出钙和α-肾上腺素能阻滞剂的活性。

6. 发明授权

US06596724B2 Oxadiazole and thiadiazole derivatives of dihydropyridine NPY antagonists 失效
标题翻译：二氢吡啶NPY拮抗剂的恶二唑和噻二唑衍生物
公开(公告)号：US06596724B2
公开(公告)日：2003-07-22
申请号：US09897532
申请日：2001-07-02
申请人： Graham S. Poindexter , Mendi Higgins , James Guy Breitenbucher
发明人： Graham S. Poindexter , Mendi Higgins , James Guy Breitenbucher
IPC分类号： A61K31495
CPC分类号： C07D413/12 , C07D211/90 , C07D413/14 , C07D417/12 , C07D417/14
摘要： A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of oxadiazole, thiadiazole and thiadiazole oxide derivatives of dihydropyridines of Formula I. wherein B is with X being O, S or and X1 is O or S. 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I的二氢吡啶的恶二唑，噻二唑和噻二唑氧化物衍生物组成。其中B是X是O，S或X 1是O或S.作为NPY诱导的拮抗剂行为，这些化合物预期作为促进减肥和治疗进食障碍的有效厌氧剂。

7. 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。

8. 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。

9. 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。

10. 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。

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