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81. 发明授权

US5530121A Carbamates of rapamycin 失效
公开(公告)号：US5530121A
公开(公告)日：1996-06-25
申请号：US451104
申请日：1995-05-25
申请人： Wenling Kao , Magid A. Abou-Gharbia , Robert L. Vogel
发明人： Wenling Kao , Magid A. Abou-Gharbia , Robert L. Vogel
IPC分类号： A61K31/395 , A61K31/44 , A61K31/675 , C07D491/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONH--[(CR.sup.3 R.sup.4).sub.m (--A--(CR.sup.5 R.sup.6).sub.n).sub.p ].sub.q --B; ##STR2## R.sup.3, R.sup.4, R.sup.5, R.sup.6, and B are each, independently, hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, cycloalkyl, --OR.sup.7, --SR.sup.7, halogen, --CN, --NO.sub.2, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.2 R.sup.7, --OSO.sub.3 R.sup.7, --NR.sup.7 R.sup.8, --NHCOR.sup.7, --NHSO.sub.2 R.sup.7, or Ar;R.sup.7 and R.sup.8 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl;R.sup.9 and R.sup.10 are each, independently, alkyl , alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.2 R.sup.7, or Ar;A is --CH.sub.2 --, --NR.sup.7, --O--, --S--, --SO--, --SO.sub.2 --, --PR.sup.7, --CO--, --NHCO--, --NHSO--, or --P(O)(R.sup.7)--;Ar is phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, quinoxalyl, thienyl, thionaphthyl, furyl, benzofuryl, benzodioxyl, benzoxazolyl, benzoisoxazolyl, indolyl, thiazolyl, isoxazolyl, pyrimidinyl, pyrazinyl, imidazolyl, benzopyranyl, benz[b]thiophenolyl, benzimidazolyl, benzthiazolyl, benzodioxolyl, piperidinyl, morpholinyl, piperazinyl, tetrahydrofuranyl, or pyrrolidinyl; wherein the Ar group may be optionally mono-, di-, or tri-substituted; ##STR3## is a nitrogen containing heterocycle that may be saturated, unsaturated, or partially unsaturated, and may be optionally mono-, di-, or tri- substituted; with the proviso that R.sup.1 and R.sup.2 are not both hydrogen;m=0-6;n=0-6;p=0-1;q=0-1;or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

82. 发明授权

US5508401A Substituted dibenzo[a,d]cycloheptene NMDA antagonists 失效
标题翻译：取代的二苯并[a，d]环庚烯NMDA拮抗剂
公开(公告)号：US5508401A
公开(公告)日：1996-04-16
申请号：US658283
申请日：1991-02-20
申请人： Wayne E. Childers, Jr. , Magid A. Abou-Gharbia , Edward J. Podlesny
发明人： Wayne E. Childers, Jr. , Magid A. Abou-Gharbia , Edward J. Podlesny
IPC分类号： A61K31/55 , A61P25/08 , A61P25/28 , C07D471/08 , C07D487/08
CPC分类号： C07D471/08
摘要： This invention involves novel neuroprotectant agents of the formula: ##STR1## in which R.sup.1 and R.sup.3 are, independently, hydrogen, cyano, nitro, halo or perhaloalkyl, with the proviso that one of R.sup.1 and R.sup.3 is other than hydrogen; R.sub.2 is alkyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及下式的新型神经保护剂：其中R 1和R 3独立地为氢，氰基，硝基，卤素或全卤代烷基，条件是R 1和R 3中的一个不是氢; R2是烷基; 或其药学上可接受的盐。

83. 发明授权

US5486524A Carbamates of rapamycin 失效
标题翻译：雷帕霉素的氨基甲酸酯
公开(公告)号：US5486524A
公开(公告)日：1996-01-23
申请号：US449166
申请日：1995-05-24
申请人： Amedeo A. Failli , Oleg I. Bleyman , Wenling Kao , Magid A. Abou-Gharbia
发明人： Amedeo A. Failli , Oleg I. Bleyman , Wenling Kao , Magid A. Abou-Gharbia
IPC分类号： A61K31/395 , A61K31/44 , A61K31/675 , C07D491/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## where the substituents are defined in the specification.
摘要翻译：其中取代基在说明书中定义的结构式II的化合物。

84. 发明授权

US5484791A Carbamates of rapamycin 失效
标题翻译：雷帕霉素的氨基甲酸酯
公开(公告)号：US5484791A
公开(公告)日：1996-01-16
申请号：US449443
申请日：1995-05-24
申请人： Amedeo A. Failli , Oleg I. Bleyman , Wenling Kao , Magid A. Abou-Gharbia
发明人： Amedeo A. Failli , Oleg I. Bleyman , Wenling Kao , Magid A. Abou-Gharbia
IPC分类号： A61K31/395 , A61K31/44 , A61K31/675 , C07D491/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, or --CONH--O--(CR.sup.3 R.sup.4).sub.m Z;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, cycloalkyl, --CF.sub.3, or F;Z is hydrogen, alkyl, --OR.sup.5, --SR.sup.5, --NR.sup.5 R.sup.6, --CN, --CF.sub.3, --OAr, --Ar, or R.sup.7 ;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, or Ar;R.sup.7 is ##STR2## or --C.tbd.C--R.sup.11 ; R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted;Ar is an aryl radical that may be optionally mono-, di-, or tri-substituted; andm=1-6;with the proviso that R.sup.1 and R.sup.2 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译：结构式II的化合物，其中R 1和R 2各自独立地为氢或-CONH-O-（CR 3 R 4）m Z; R 3和R 4各自独立地为氢，烷基，环烷基，-CF 3或F; Z是氢，烷基，-OR 5，-SR 5，-NR 5 R 6，-CN，-CF 3，-OAr，-Ar或R 7; R 5和R 6各自独立地为氢，烷基，芳基烷基，烯基，炔基，烷氧基烷基，烷基硫代烷基，烷基氨基烷基，二烷基氨基烷基，环烷基或Ar; R7是或-C 3BOND C-R11; R 8，R 9，R 10和R 11各自独立地为氢，1-6个碳原子的烷基，卤素或苯基，其中苯基可以是任选的单，二或三取代; Ar是可以任选被单，二或三取代的芳基; m = 1-6; 条件是R1和R2都不是氢，或其药学上可接受的盐，其可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。

85. 发明授权

US5010078A Aryl- and heteroaryl piperazinyl carboxamides having central nervous system activity 失效
标题翻译：具有中枢神经系统活性的芳基和杂芳基哌嗪基甲酰胺
公开(公告)号：US5010078A
公开(公告)日：1991-04-23
申请号：US493179
申请日：1990-03-14
申请人： Magid A. Abou-Gharbia , John P. Yardley , Wayne E. Childers, Jr.
发明人： Magid A. Abou-Gharbia , John P. Yardley , Wayne E. Childers, Jr.
IPC分类号： C07D209/42 , C07D239/42 , C07D295/13
CPC分类号： C07D239/42 , C07D209/42 , C07D295/13
摘要： There are disclosed compounds of the formula (I) ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 3-noradamantyl, unsubstituted or substituted-2-indolyl, 3-indolyl, 2-benzofuranyl and 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, pyridinyl, pyrimidinyl or pyrazinyl, wherein the substituents are selected from lower alkyl, lower alkoxy, trifluoromethyl and halo; R.sup.3 is H or lower alkyl of 1 to 3 carbon atoms; n is the integer 0 or 1; m is the integer from 2 to 5; and the pharmaceutically acceptable salts thereof.
摘要翻译：公开了式（I）的化合物其中R1是1-金刚烷基，3-甲基-1-金刚烷基，3-降金刚烷基，未取代的或取代的-2-吲哚基，3-吲哚基，2-苯并呋喃基和3-苯并呋喃基，其中取代基选自低级烷基，低级烷氧基和卤素; R2是未取代或取代的苯基，苄基，吡啶基，嘧啶基或吡嗪基，其中取代基选自低级烷基，低级烷氧基，三氟甲基和卤素; R3是H或1〜3个碳原子的低级烷基; n是整数0或1; m是2至5的整数; 及其药学上可接受的盐。

86. 发明授权

US4988814A Tertiary alkyl functionalized piperazine derivatives 失效
标题翻译：叔烷基官能化哌嗪衍生物
公开(公告)号：US4988814A
公开(公告)日：1991-01-29
申请号：US428148
申请日：1989-10-27
申请人： Magid A. Abou-Gharbia , John P. Yardley , Ian A. Cliffe
发明人： Magid A. Abou-Gharbia , John P. Yardley , Ian A. Cliffe
IPC分类号： C07D239/42 , C07D295/13 , C07D295/15
CPC分类号： C07D295/13 , C07D239/42 , C07D295/15
摘要： Compounds of the formula: ##STR1## in which R.sup.1 is alkyl; R.sup.2 and R.sup.3 are alkyl or taken together they are polymethylene, R.sup.2 and R.sup.3 complete a 5-norbornen-2-yl moiety; X is --CO.sub.2 --, --OCO--, --OCO.sub.2 --, --N(R.sup.7)CO--, --NHNHCO--, --ON(R.sup.7)CO--, --CON(R.sup.7)--, --N(R.sup.7)CO.sub.2 --, --OCON(R.sup.7)-- or --N(R.sup.7)CON(R.sup.8)--, wherein R.sup.7 and R.sup.8 are, independently, hydrogen, alkyl, phenyl, benzyl, substituted phenyl or substituted benzyl in which the substituents are halo, alkyl alkoxy, cyano, nitro or perhalomethyl; R.sup.4 is hydrogen or alkyl; R.sup.5 is hydrogen, alkyl, hydroxyalkyl, phenyl, benzyl, substituted phenyl or substituted benzyl in which the substituents are hydroxy, halo, alkyl alkoxy, trifluoromethyl, nitro, cyano, carbalkoxy, carboxamido, amino, alkylamino or dialkylamino; R.sup.6 is phenyl, benzyl, 2-, 3-, or 4-pyridinyl, 2-pyrimidinyl or 2-pyrazinyl any of which may be substituted by one or more hydroxy, halo, alkyl alkoxy, trifluoromethyl, nitro, cyano, carbalkoxy, carboxamido, amino, alkylamino or dialkylamino; n is one of the integers 0, 1, 2, 3, 4 or 5; or a pharmaceutically acceptable salt thereof, with the proviso that when X is --CON(R.sup.7)-- and R.sup.7 is alkyl, R.sup.6 is other than 2-pyrimidinyl, and when X is --CO.sub.2 -- and R.sup.1, R.sup.2 and R.sup.3 are methyl and n is 1, R.sup.6 is other than 3,5-di(trifluoromethyl)phenyl are antidepressant and/or anxiolytic agents.

87. 发明授权

US4957913A Antihypertensive polycyclic imides 失效
标题翻译：抗高血压多环酰胺
公开(公告)号：US4957913A
公开(公告)日：1990-09-18
申请号：US440573
申请日：1989-11-22
申请人： Magid A. Abou-Gharbia , Gary P. Stack , Rodney W. Lappe
发明人： Magid A. Abou-Gharbia , Gary P. Stack , Rodney W. Lappe
IPC分类号： A61K31/495 , A61K31/505
CPC分类号： A61K31/505 , A61K31/495
摘要： Hypertension in the mammal is controlable by administration of a compound of the formula: ##STR1## wherein R is ##STR2## in which X is methylene, ethylene or ethylidene and Q is alkylene, alkylidene, or Q is a ##STR3## in which the dotted line represents optional unsaturation; n is one of the integers 2,3 or 4;Ar is phenyl or phenyl substituted with halo. trifluoromethyl or alkoxy, or Ar is 2-pyrimidinyl or halopyrimidin-2-yl, 2-pyrazinyl or halo-pyrazin-2-yl, 2-pyridinyl, cyanopyridin-2-yl or halopyridin-2-yl;or a pharmaceutically acceptable salt thereof.
摘要翻译：哺乳动物的高血压可以通过给予下式化合物来控制：其中R是其中X是亚甲基，亚乙基或亚乙基且Q是亚烷基，亚烷基或Q是一个“IMAGE”，其中虚线表示可选的不饱和度; n是整数2,3或4之一; Ar是苯基或被卤素取代的苯基。三氟甲基或烷氧基，或Ar为2-嘧啶基或卤代嘧啶-2-基，2-吡嗪基或卤代吡嗪-2-基，2-吡啶基，氰基吡啶-2-基或卤代吡啶-2-基; 或其药学上可接受的盐。

88. 发明授权

US4940789A 10,11-dihydro-5-alkyl-12-substituted-10,5-(iminomethano)-5H-d ibenzo[a,d]cycloheptenes as neuroprotectant agents 失效
标题翻译： 10,11-二氢-5-烷基-12-取代-10-（亚氨基甲酰基）-5H-二苯并[a，d]环庚烯作为神经保护剂
公开(公告)号：US4940789A
公开(公告)日：1990-07-10
申请号：US418591
申请日：1989-10-10
申请人： Wayne E. Childers, Jr. , Magid A. Abou-Gharbia
发明人： Wayne E. Childers, Jr. , Magid A. Abou-Gharbia
IPC分类号： A61K31/55 , A61P25/28 , A61P43/00 , C07D471/08
CPC分类号： C07D471/08
摘要： This invention involves novel neuroprotectant agents of the formula: ##STR1## in which R.sup.1 and R.sup.3 are, independently, hydrogen, alkyl, alkoxy, hydroxy, cyano, nitro, halo, trifluoromethyl, amino, alkylamino or dialkylamino; R.sup.2 is alkyl; R.sup.4 is alkyl, phenyl or benzyl; n is 0 or 1; m is one of the integers 0,1,2,3,4,5 or 6; and X is alkyl, alkylamino, dialkylamino, alkanoyl or substituted or unsubstituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl, quinolyl, morpholinyl, furyl thienyl, pyrrolyl, tetrahydrofuryl, tetrahydrothienyl, pyrrolidinyl, piperidinyl, piperazinyl or perhydropyridminyl, in which the subsitutent is alkyl, alkoxy, halo, trifluoromethyl, cyano, nitro or hydroxy; or a pharmaceutically acceptable salt thereof; and their use in control of degenerative CNS disease states.
摘要翻译：本发明涉及下式的新型神经保护剂：其中R 1和R 3独立地为氢，烷基，烷氧基，羟基，氰基，硝基，卤素，三氟甲基，氨基，烷基氨基或二烷基氨基; R2是烷基; R4是烷基，苯基或苄基; n为0或1; m是整数0,1,2,3,4,5或6之一; X是烷基，烷基氨基，二烷基氨基，烷酰基或取代或未取代的苯基，吡啶基，嘧啶基，吡嗪基，喹啉基，吗啉基，呋喃基噻吩基，吡咯基，四氢呋喃基，四氢噻吩基，吡咯烷基，哌啶基，哌嗪基或全氢吡啶基，其中所述取代基是烷基，烷氧基，卤素，三氟甲基，氰基，硝基或羟基; 或其药学上可接受的盐; 及其在控制退行性CNS疾病状态中的应用。

89. 发明授权

US4921958A Piperazinylalkylcarboxylic acid adamantylamides 失效
标题翻译：哌嗪基烷基羧酸金刚烷基酰胺
公开(公告)号：US4921958A
公开(公告)日：1990-05-01
申请号：US413407
申请日：1989-09-27
申请人： Magid A. Abou-Gharbia , John P. Yardley , Wayne E. Childers, Jr. , Ian A. Cliffe
发明人： Magid A. Abou-Gharbia , John P. Yardley , Wayne E. Childers, Jr. , Ian A. Cliffe
IPC分类号： C07D239/42 , C07D295/13 , C07D295/15
CPC分类号： C07D295/13 , C07D239/42 , C07D295/15
摘要： The compounds of the formula: ##STR1## wherein Ad is 1-adamantyl, 2-adamantyl or 3-noradamantyl; n is 1,2,3,4 or 5; R.sup.1 hydrogen, alkyl, phenyl, benzyl, or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, cyano, nitro or trifluoromethyl; R.sup.2 is phenyl, benzyl or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhalomethyl, 2-, 3-, or 4-pyridinyl, 2-, 4- or 5-pyrimidinyl or 2- or 3-pyrazinyl; R.sup.3 and R.sup.4 are, independently, hydrogen, methyl, phenyl or benzyl; or a pharmaceutically acceptable salt thereof, are useful anxiolytic/antidepressant agents, with elements of antipsychotic activity.
摘要翻译：下式的化合物：其中Ad是1-金刚烷基，2-金刚烷基或3-降金刚烷基; n为1,2,3,4或5; 烷基，苯基，苄基或取代的苯基或苄基，其中取代基是烷基，烷氧基，卤素，氰基，硝基或三氟甲基; R2是苯基，苄基或取代的苯基或苄基，其中取代基是烷基，烷氧基，卤素，硝基，氰基或全卤代甲基，2-，3-或4-吡啶基，2-，4-或5-嘧啶基或2- 或3-吡嗪基; R 3和R 4独立地是氢，甲基，苯基或苄基; 或其药学上可接受的盐是具有抗精神病活性成分的抗焦虑/抗抑郁药。

90. 发明授权

US4883875A Antipsychotic imides 失效
标题翻译：抗精神病药
公开(公告)号：US4883875A
公开(公告)日：1989-11-28
申请号：US335172
申请日：1989-04-07
申请人： Magid A. Abou-Gharbia
发明人： Magid A. Abou-Gharbia
IPC分类号： C07D401/06 , C07D401/14
CPC分类号： C07D401/06 , C07D401/14
摘要： The compounds: ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or alkyl and R.sup.6 and R.sup.7, taken together, are tetramethylene, pentamethylene or hexamethylene;p is one of the integers 2, 3, 4 or 5;and ##STR2## where R.sup.4 is hydrogen, alkyl, alkoxy or halo;or a pharmaceutically acceptable salt thereof are antipsychotic and anxiolytic agents.
摘要翻译：化合物：其中R 1和R 2是氢或烷基，R 6和R 7一起是四亚甲基，五亚甲基或六亚甲基的化合物： p是整数2,3,4或5之一; 和其中R 4是氢，烷基，烷氧基或卤素的或其药学上可接受的盐是抗精神病药和抗焦虑药。

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