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41. 发明授权

US5550133A Carbamates of rapamycin 失效
标题翻译：雷帕霉素的氨基甲酸酯
公开(公告)号：US5550133A
公开(公告)日：1996-08-27
申请号：US448869
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 the variables are defined in the specification, 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，其中变量在说明书中定义，条件是R 1和R 2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，抗增殖和抗肿瘤药。

42. 发明授权

US5530013A Venlafaxine in the inducement of cognition enhancement 失效
标题翻译：文拉法辛诱导认知增强
公开(公告)号：US5530013A
公开(公告)日：1996-06-25
申请号：US442546
申请日：1995-05-16
申请人： G. E. Morris Husbands , Magid A. Abou-Gharbia , John A. Moyer , Eric A. Muth
发明人： G. E. Morris Husbands , Magid A. Abou-Gharbia , John A. Moyer , Eric A. Muth
IPC分类号： A61K31/135 , A61K31/41
CPC分类号： A61K31/135
摘要： This invention provides a method of inducing cognition enhancement in a mammal by administering to the mammal experiencing a cognition impairment an effective amount of a hydroxycycloalkanephenethyl amine compound of the following structural formula: ##STR1## in which A is a moiety of the formula ##STR2## wherein the dotted line represents optional unsaturation;R.sub.1 is hydrogen or alkyl;R.sub.2 is alkyl;R.sub.4 is hydrogen, alkyl, formyl, or alkanol;R.sub.5 and R.sub.6 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, cyano, nitro, alkylmercapto, amino, alkylamino, dialkylamino, alkanamido, halo, trifluoromethyl, or taken together, methylene dioxy;R.sub.7 is hydrogen or alkyl; andn is 0, 1, 2, 3, or 4;or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了通过向经历认知障碍的哺乳动物施用有效量的以下结构式的羟基环烷基甲苯胺化合物来诱导哺乳动物认知增强的方法：不饱和度; R1是氢或烷基; R2是烷基; R4是氢，烷基，甲酰基或烷醇; R 5和R 6独立地是氢，羟基，烷基，烷氧基，烷酰氧基，氰基，硝基，烷基巯基，氨基，烷基氨基，二烷基氨基，烷酰氨基，卤素，三氟甲基或一起，亚甲基二氧基; R7是氢或烷基; 且n为0,1,2,3或4; 或其药学上可接受的盐。

43. 发明授权

US5484790A Carbamates of rapamycin 失效
公开(公告)号：US5484790A
公开(公告)日：1996-01-16
申请号：US448812
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.

44. 发明授权

US5480988A Carbamates of rapamycin 失效
标题翻译：雷帕霉素的氨基甲酸酯
公开(公告)号：US5480988A
公开(公告)日：1996-01-02
申请号：US284764
申请日：1994-08-02
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, --CONR.sup.3 (CR.sup.4 R.sup.5).sub.m (CR.sup.4 R.sup.5).sub.n (CR.sup.8 R.sup.9).sub.p NR.sup.10 R.sup.11, or ##STR2## --R.sup.12, or --CONR.sup.3 R.sup.13 ; R.sup.3 is hydrogen, alkyl, or arylalkyl;R.sup.4, R.sup.5, R.sup.8, and R.sup.9 are each, independently, hydrogen, alkyl, p--OH, --CF.sub.3, or --F;R.sup.6 is hydrogen or --OR.sup.13 ;R.sup.7 is hydrogen or alkyl;R.sup.10 is hydrogen, alkyl, or arylalkyl;R.sup.11, R.sup.12, and R.sup.13 are each independently, --(CR.sup.15 R.sup.16).sub.r R.sup.17 ;R.sup.14 is hydrogen, alkyl of 1-6 carbon atoms, tri-(alkyl)silyl, Tri-(alkyl)silyethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, or tetrahydropyranyl;R.sup.15 and R.sup.16 are each independently, hydrogen or alkyl; ##STR3## R.sup.18, R.sup.19, R.sup.20, and R.sup.21 are each, independently, hydrogen, alkyl, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted; ##STR4## is a 5-7 membered saturated or partially unsaturated heterocyclic radical containing at least 2 ring nitrogens, wherein the heterocyclic ring may optionally contain NR.sup.22 in the heterocyclic ring, and the ring carbons may optionally be substituted by alkyll, arylalkyl, halogen, --CF.sub.3, ---OR.sup.14, or --CO.sub.2 R.sup.10 ;R.sup.22 is hydrogen, alkyl, or arylalkyl;m=0-6;n=1-6;p=0-6; andr=1-6with 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, anti inflammatory, 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，-CONR 3（CR 4 R 5）m（CR 4 R 5）n（CR 8 R 9）pNR 10 R 11或CONR 3（CR 4 R 5）m（CR 6 R 7）n（CR 8 R 9）pNR 10 R 11，或 -R12或-CONR3R13; R3是氢，烷基或芳基烷基; R 4，R 5，R 8和R 9各自独立地为氢，烷基，p-OH，-CF 3或-F; R6是氢或-OR13; R7是氢或烷基; R 10是氢，烷基或芳基烷基; R 11，R 12和R 13各自独立地为 - （CR 15 R 16）r R 17; R 14为氢，1-6个碳原子的烷基，三（烷基）甲硅烷基，三（烷基）甲硅烷基，三苯基甲基，苄基，烷氧基甲基，三（烷基）甲基乙氧基甲基或四氢吡喃基; R 15和R 16各自独立地为氢或烷基; R18，R19，R20和R21各自独立地为氢，烷基，卤素或苯基，其中苯基可以是任选的单，二或三取代; 含有至少2个环氮原子的5-7元饱和或部分不饱和杂环基，其中该杂环可以在杂环中任选地含有NR 22，并且该环碳可任选地被烷基，芳烷基，卤素， -CF 3，-OR 14或-CO 2 R 10; R 22是氢，烷基或芳基烷基; m = 0-6; n = 1-6; p = 0-6; 并且r = 1-6，条件是R 1和R 2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。

45. 发明授权

US5106849A Use of aryl- and heteroaryl piperazinyl carboxamides in the treatment of various central nervous system disorders 失效
标题翻译：芳基和杂芳基哌嗪基甲酰胺在治疗各种中枢神经系统疾病中的应用
公开(公告)号：US5106849A
公开(公告)日：1992-04-21
申请号：US689409
申请日：1991-04-22
申请人： Magid A. Abou-Gharbia , John P. Yardley , Wayne E. Childers, Jr. , John A. Moyer
发明人： Magid A. Abou-Gharbia , John P. Yardley , Wayne E. Childers, Jr. , John A. Moyer
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 the use of the 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 or 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, or pyrimidinyl 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; and m is the integer from 2 to 5 and the pharmaceutically acceptable salts thereof.
摘要翻译：公开了式（I）化合物（I）的用途，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-苯并呋喃基或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是未取代的或取代的苯基，苄基或嘧啶基，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; 且m为2至5的整数及其药学上可接受的盐。

46. 发明授权

US5036070A Polycyclic phenalkyl amines as psychotropic agents 失效
标题翻译：多环苯烷基胺作为精神药物
公开(公告)号：US5036070A
公开(公告)日：1991-07-30
申请号：US537551
申请日：1990-06-13
申请人： Magid A. Abou-Gharbia
发明人： Magid A. Abou-Gharbia
IPC分类号： C07D239/42 , C07D241/20 , C07D295/092 , C07D319/20
CPC分类号： C07D239/42 , C07D241/20 , C07D295/088 , C07D319/20
摘要： There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl, or phenyl, or R.sup.1 and R.sup.2 taken together represent --(CH.sub.2).sub.4 -- or ##STR2## where the dotted line represents an optional double bond; R.sup.3 is hydrogen, alkyl, alkoxy, or halo;Z is oxygen, or --N(R.sup.6), where R.sup.6 is hydrogen or alkyl;m is 1-4;n is 0-2; ##STR3## wherein R.sup.7 is unsubstituted or substituted phenyl, 2-pyridinyl, 2-pyrimidinyl, 2-pyrazinyl, 3-pyridazinyl, or diphenylmethyl, where the substituents are selected from the group of alkyl, alkoxy, halo, cyano, nitro and trifluoromethyl;R.sup.8 is hydrogen, hydroxy, cyano, alkyl, alkoxy, halo, or NHR.sup.9 where R.sup.9 is hydrogen, alkyl, phenyl, tolyl, xylyl, mesityl, methoxyphenyl, or halophenyl with the proviso when Z is oxygen, R.sup.7 is other than phenyl or pyridyl;or a pharmaceutically acceptable salt thereof, which by virtue of high affinity for the dopamine D-2 receptor and the serotonin 5-HT-.sub.1A receptor, are useful as antipsychotic and anxiolytic agents for the treatment of a variety of central nervous system disorders such as paranoia, schizophrenia, anxiety, sleep disorders, and related problems.
摘要翻译：公开了式（IMAGE）的化合物，其中R 1和R 2各自独立地为氢，烷基或苯基，或者R 1和R 2一起表示 - （CH 2）4 - 或，其中虚线表示任选的双键; R3是氢，烷基，烷氧基或卤素; Z是氧或-N（R6），其中R6是氢或烷基; m为1-4; n为0-2; 其中R 7为未取代或取代的苯基，2-吡啶基，2-嘧啶基，2-吡嗪基，3-哒嗪基或二苯基甲基，其中取代基选自烷基，烷氧基，卤素，氰基，硝基和三氟甲基; R8是氢，羟基，氰基，烷基，烷氧基，卤素或NHR9，其中R9是氢，烷基，苯基，甲苯基，二甲苯基，三甲苯基，甲氧基苯基或卤代苯基，条件是Z是氧时，R7不是苯基或吡啶基 ; 或其药学上可接受的盐，其由于对多巴胺D-2受体和5-羟色胺5-HT-1A受体的高亲和力可用作抗精神病药和抗焦虑剂，用于治疗各种中枢神经系统疾病，例如偏执狂，精神分裂症，焦虑症，睡眠障碍和相关问题。

47. 发明授权

US4968792A Psychotropic benzisothiazole derivatives 失效
标题翻译：精神药物苯并异噻唑衍生物
公开(公告)号：US4968792A
公开(公告)日：1990-11-06
申请号：US412256
申请日：1989-09-25
申请人： Gary P. Stack , Magid A. Abou-Gharbia , Thomas D. Golobish
发明人： Gary P. Stack , Magid A. Abou-Gharbia , Thomas D. Golobish
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： Disclosed herein are novel benzisothiazole derivatives having pharmacological activity, to a process for preparing them, to pharmaceutical compositions containing them, and to their use in the treatment of a variety of central nervous system disorders.
摘要翻译：本文公开了具有药理活性的新的苯并异噻唑衍生物，其制备方法，含有它们的药物组合物及其在治疗各种中枢神经系统疾病中的用途。

48. 发明授权

US4957909A Benzobicycloalkane derivatives as anticonvulsant neuroprotective agents 失效
公开(公告)号：US4957909A
公开(公告)日：1990-09-18
申请号：US459874
申请日：1990-01-02
申请人： Magid A. Abou-Gharbia , Ronald R. Notvest
发明人： Magid A. Abou-Gharbia , Ronald R. Notvest
IPC分类号： A61K31/135 , A61K31/34 , C07D307/52 , C07D333/20
CPC分类号： A61K31/135 , A61K31/34 , C07D307/52 , C07D333/20
摘要： The use of the compounds: ##STR1## where R is hydrogen, alkyl, alkoxy, hydroxy, alkanoyloxy, phenylalkoxy, halo or trifluoromethyl; R.sup.1 is alkyl, alkenyl or phenylalkyl; R.sup.2 is hydrogen, alkyl, phenylalkyl, alkenyl, alkynyl, thienylalkyl or furylalkyl; n is one of the integers 2, 3, 4, 5 or 6; or a pharmaceutically acceptable salt thereof, as NMDA antagonists in the treatment of convulsions and neurodegenerative disease states. The compounds in which R.sup.2 are heterocyclylalkylamines are novel and useful NMDA antagonists.

49. 发明授权

US4924008A Benzobicycloalkane derivatives as anticonvulsant neuroprotective agents 失效
标题翻译：苯并双环烷烃衍生物作为抗惊厥神经保护剂
公开(公告)号：US4924008A
公开(公告)日：1990-05-08
申请号：US347538
申请日：1989-05-04
申请人： Magid A. Abou-Gharbia , Ronald R. Notvest
发明人： Magid A. Abou-Gharbia , Ronald R. Notvest
IPC分类号： A61K31/135 , A61K31/34 , C07D307/52 , C07D333/20
CPC分类号： A61K31/135 , A61K31/34 , C07D307/52 , C07D333/20
摘要： The use of the compounds: ##STR1## where R is hydrogen, alkyl, alkoxy, hydroxy, alkanoyloxy, phenylalkoxy, halo or trifluoromethyl; R.sup.1 is alkyl, alkenyl or phenylalkyl; R.sup.2 is hydrogen, alkyl, phenylalkyl, alkenyl, alkynyl, thienylalkyl or furylalkyl; n is one of the integers 2, 3, 4, 5 or 6; or a pharmaceutically acceptable salt thereof, as NMDA antagonists in the treatment of convulsions and neurodegenerative disease states. The compounds in which R.sup.2 are heterocyclylalkylamines are novel and useful NMDA antagonists.
摘要翻译：化合物的用途：其中R是氢，烷基，烷氧基，羟基，烷酰氧基，苯基烷氧基，卤素或三氟甲基; R1是烷基，烯基或苯基烷基; R2是氢，烷基，苯基烷基，烯基，炔基，噻吩烷基或呋喃基烷基; n是整数2,3,4,5或6之一; 或其药学上可接受的盐作为治疗惊厥和神经变性疾病状态的NMDA拮抗剂。其中R2是杂环烷基胺的化合物是新的和有用的NMDA拮抗剂。

50. 发明授权

US4910302A Psychotropic polycyclic imides 失效
标题翻译：精神药物多环酰胺
公开(公告)号：US4910302A
公开(公告)日：1990-03-20
申请号：US286576
申请日：1988-12-19
申请人： Magid A. Abou-Gharbia , Gary P. Stack
发明人： Magid A. Abou-Gharbia , Gary P. Stack
IPC分类号： C07D405/12
CPC分类号： C07D405/12
摘要： Compounds of the formula: ##STR1## in which Z is ##STR2## wherein X is alkylene, ethanylene or alkylidene; Q is alkylene, alkylidene, ##STR3## or Q, taken together with the carbon atoms to which it is attached forms a benzene ring or a substituted benzene ring, in which said substituents are --OH, --OCH.sub.3, alkyl, halo, --CF.sub.3, --NH.sub.2, monoalkylamino, dialkylamino or alkanoylamino; R.sup.1 is hydrogen or alkyl; R.sup.2 and R.sup.3 are, independently, hydrogen or alkyl or taken together with the carbon atoms to which they are attached, they form a cycloalkane or cycloalkene ring; m is one of the integers 2-5; R.sup.4 is hydrogen, hydroxy, cyano, alkyl, alkoxy, halo, amino, alkylamino, phenylamino, tolylamino, xylylamino, mesitylamino, methoxyphenylamino, or halophenylamino; and the dotted lines represent optional unsaturation; or a pharmaceutically acceptable salt thereof.
摘要翻译：下式的化合物：其中Z是 + TR ，其中X是亚烷基，亚乙炔基或亚烷基; Q是与其连接的碳原子一起形成苯环或取代的苯环的亚烷基，亚烷基，或亚甲基，其中所述取代基是-OH，-OCH 3，烷基，卤素，-CF 3 ，-NH 2，单烷基氨基，二烷基氨基或烷酰基氨基; R1是氢或烷基; R2和R3独立地是氢或烷基或与它们所连接的碳原子一起形成环烷烃或环烯烃环; m是整数2-5之一; R4是氢，羟基，氰基，烷基，烷氧基，卤素，氨基，烷基氨基，苯基氨基，甲苯基氨基，二甲苯基氨基，均三甲氨基，甲氧基苯基氨基或卤代苯基氨基; 虚线表示可选的不饱和键; 或其药学上可接受的盐。

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