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1. 发明授权

US4341698A Enkaphalin derivatives 失效
标题翻译：恩考芬素衍生物
公开(公告)号：US4341698A
公开(公告)日：1982-07-27
申请号：US130431
申请日：1980-03-14
申请人： Albert A. Carr , Robert A. Farr , John M. Kane
发明人： Albert A. Carr , Robert A. Farr , John M. Kane
IPC分类号： A61K38/00 , C07D241/08 , C07K5/078 , C07K5/117 , C07C103/52
CPC分类号： C07K5/06139 , C07D241/08 , C07K5/1024 , A61K38/00
摘要： Novel analgesic and antipsychotic agents having the formula ##STR1## wherein Q is ##STR2## in which R.sub.1 is hydrogen, hydroxy or halogen and R.sub.4 is hydrogen or, R.sub.1 and R.sub.4 are both hydroxy; Z is hydrogen or straight chain lower alkyl having from 1 to 4 carbon atoms and X is methylene, carbonyl, hydroxymethylene, thio, sulfinyl or sulfonyl, or Z and X, taken together, are methylidenyl, with the proviso that when X is sulfonyl or sulfinyl, Z is other than hydrogen; R.sub.5 is hydrogen or halogen, and R.sub.2 is H, a straight or branched lower alkyl group having from 1 to 4 carbon atoms, the group ##STR3## or the group ##STR4## wherein R.sub.3 is hydroxy, amino, alkylamino or dialkylamino wherein the alkyl moiety is straight or branched and has from 1 to 4 carbon atoms, diastereomers, enantiomers and pharmaceutically acceptable salts thereof.
摘要翻译：其中Q为的新型止痛剂和抗精神病药，其中R1为氢，羟基或卤素，R4为氢或R1和R4均为羟基; Z是氢或具有1至4个碳原子的直链低级烷基，X是亚甲基，羰基，羟基亚甲基，硫代，亚磺酰基或磺酰基，或Z和X一起是亚甲基，条件是当X是磺酰基或亚磺酰基，Z不是氢; R 5是氢或卤素，R 2是H，具有1至4个碳原子的直链或支链低级烷基，基团“IMAGE”或基团“IMAGE”，其中R 3是羟基，氨基，烷基氨基或二烷基氨基，其中烷基部分是直链或支链的并且具有1至4个碳原子，非对映异构体，对映异构体和药学上可接受的盐。

2. 发明授权

US4435571A 5-(Substituted benzyl)-6-oxo-2-piperazine carboxylic acids and esters 失效
标题翻译： 5-（取代的苄基）-6-氧代-2-哌嗪羧酸和酯
公开(公告)号：US4435571A
公开(公告)日：1984-03-06
申请号：US399553
申请日：1982-07-19
申请人： Albert A. Carr , Robert A. Farr , John M. Kane
发明人： Albert A. Carr , Robert A. Farr , John M. Kane
IPC分类号： A61K38/00 , C07D241/08 , A61K31/495
CPC分类号： C07D241/08 , A61K38/00
摘要： The present invention relates to compounds of the formula ##STR1## wherein R' is hydrogen, straight or branched chain lower alkyl having from 1 to 4 carbon atoms or benzyl, Z is hydrogen or straight chain lower alkyl having from 1 to 4 carbon atoms, Y is hydrogen or a nitrogen blocking group selected from the group consisting of tertiary alkoxycarbonyl, benzyloxycarbonyl, cycloalkoxycarbonyl and vinyloxycarbonyl, R.sub.c is hydrogen, halogen or benzyloxy and R.sub.d is hydrogen, or R.sub.c and R.sub.d are benzyloxy; or an individual diastereomer thereof. Said compounds having use as intermediates in the production of enkephalin derivatives which in turn are used as analgesic and antipsychotic agents.
摘要翻译：本发明涉及下式化合物，其中R'是氢，具有1至4个碳原子的直链或支链低级烷基或苄基，Z是氢或具有1至4个碳原子的直链低级烷基， Y是氢或选自叔烷氧基羰基，苄氧基羰基，环烷氧基羰基和乙烯氧基羰基的氮阻断基，Rc是氢，卤素或苄氧基，Rd是氢，或Rc和Rd是苄氧基; 或其单独的非对映异构体。所述化合物在生产脑啡肽衍生物中被用作中间体，其又被用作镇痛药和抗精神病药。

3. 发明授权

US4483988A Substituted derivatives of 4-t-alkoxycarbonyl-piperazin-2-ones 失效
标题翻译：取代的4-叔丁氧基羰基 - 哌嗪-2-酮的衍生物
公开(公告)号：US4483988A
公开(公告)日：1984-11-20
申请号：US399554
申请日：1982-07-19
申请人： Albert A. Carr , Robert A. Farr , John M. Kane
发明人： Albert A. Carr , Robert A. Farr , John M. Kane
IPC分类号： A61K38/00 , C07D241/08
CPC分类号： C07D241/08 , A61K38/00
摘要： Novel analgesic and antipsychotic agents having the formula ##STR1## in which R.sub.1 is hydrogen, hydroxy or halogen and R.sub.4 is hydrogen or, R.sub.1 and R.sub.4 are both hydroxy; Z is hydrogen or straight chain lower alkyl having from 1 to 4 carbon atoms and X is methylene, carbonyl, hydroxymethylene, thio, sulfinyl or sulfonyl, or Z and X, taken together, are methylidenyl, with the proviso that when X is sulfonyl or sulfinyl, Z is other than hydrogen; R.sub.5 is hydrogen or halogen, and R.sub.2 is H, a straight or branched lower alkyl group having from 1 to 4 carbon atoms, the group ##STR2## or the group ##STR3## wherein R.sub.3 is hydroxy, amino, alkylamino or dialkylamino wherein the alkyl moiety is straight or branched and has from 1 to 4 carbon atoms, diastereomers, enantiomers and pharmaceutically acceptable salts thereof.
摘要翻译：其中Q为或的新型止痛剂和抗精神病药，其中R 1为氢，羟基或卤素，R 4为氢或R 1和R 4均为羟基; Z是氢或具有1至4个碳原子的直链低级烷基，X是亚甲基，羰基，羟基亚甲基，硫代，亚磺酰基或磺酰基，或Z和X一起是亚甲基，条件是当X是磺酰基或亚磺酰基，Z不是氢; R 5是氢或卤素，R 2是H，具有1至4个碳原子的直链或支链低级烷基，基团“IMAGE”或基团“IMAGE”，其中R 3是羟基，氨基，烷基氨基或二烷基氨基，其中烷基部分是直链或支链的并且具有1至4个碳原子，非对映异构体，对映异构体和药学上可接受的盐。

4. 发明授权

US5962469A Cyclic nitrones 失效
标题翻译：环状硝酮
公开(公告)号：US5962469A
公开(公告)日：1999-10-05
申请号：US978971
申请日：1997-11-26
申请人： Craig E. Thomas , Thomas L. Fevig , Stephen M. Bowen , Robert A. Farr , Albert A. Carr , David A. Janowick
发明人： Craig E. Thomas , Thomas L. Fevig , Stephen M. Bowen , Robert A. Farr , Albert A. Carr , David A. Janowick
IPC分类号： A61K31/00 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/44 , A61K31/4427 , A61K31/4436 , A61K31/47 , A61K31/472 , A61K31/473 , A61K31/4747 , A61K31/55 , A61P39/00 , A61P39/06 , C07D209/44 , C07D217/08 , C07D217/24 , C07D221/10 , C07D221/20 , C07D223/14 , C07D223/16 , C07D491/04 , C07D491/048 , C07D491/10 , C07D491/107 , C07D495/04 , C07D221/06 , C07D491/02
CPC分类号： C07D221/20 , C07D209/44 , C07D217/08 , C07D217/24 , C07D221/10 , C07D223/14 , C07D223/16 , C07D491/04 , C07D491/10 , C07D495/04
摘要： The present invention is directed to novel cyclic nitrones and their use in the prevention of oxidation tissue damage by free radicals, their use in the treatment of a number of disease states in which radicals either damage or destroy tissues via oxidation, and pharmaceutical compositions containing these cyclic nitrones.
摘要翻译：本发明涉及新的环状硝酮及其用于预防自由基的氧化组织损伤，其用于治疗许多疾病状态，其中自由基通过氧化损伤或破坏组织，以及含有这些的药物组合物环状硝酮。

5. 发明授权

US4443462A Antipsychotic 4-(naphthalenyloxy)piperidine derivatives 失效
标题翻译：抗精神病药4-（萘氧基）哌啶衍生物
公开(公告)号：US4443462A
公开(公告)日：1984-04-17
申请号：US422819
申请日：1982-09-24
申请人： Albert A. Carr , Robert A. Farr
发明人： Albert A. Carr , Robert A. Farr
IPC分类号： C07D211/46 , A61K31/445 , C07D211/44
CPC分类号： C07D211/46
摘要： Novel compounds of the formula ##STR1## wherein n is an integer of from 2 to 5, R is hydrogen, alkyl, alkoxy, halogen or trifluoromethyl, R.sub.1 is hydrogen, alkyl, alkoxy or halogen, and Z is carbonyl or hydroxymethylene and their pharmaceutically acceptable acid addition salts are useful as antipsychotic agents having a low potential for extrapyramidal side effects. The novel compounds are prepared from novel intermediates of formula ##STR2## or their salts wherein R has the meanings defined above and R.sub.2 is hydrogen, lower alkyl or phenyl(lower alkyl).
摘要翻译：新颖的式（IMAGE）化合物，其中n为2至5的整数，R为氢，烷基，烷氧基，卤素或三氟甲基，R 1为氢，烷基，烷氧基或卤素，Z为羰基或羟基亚甲基，可接受的酸加成盐可用作具有锥体束外副作用潜力低的抗精神病药。新化合物由式（Ⅰ）的新型中间体或其盐，其中R具有上述定义，R 2为氢，低级烷基或苯基（低级烷基）。

6. 发明授权

US4283404A Aroylethenylpiperidinobutyrophenone antipsychotic agents 失效
标题翻译：抗坏血酸苯基哌啶基丙二酮抗精神病药
公开(公告)号：US4283404A
公开(公告)日：1981-08-11
申请号：US72499
申请日：1979-09-04
申请人： Albert A. Carr , Robert A. Farr
发明人： Albert A. Carr , Robert A. Farr
IPC分类号： A61K31/443 , A61K31/445 , A61K31/451 , A61P25/18 , A61P25/20 , C07D211/32 , C07D211/62 , C07D405/06 , C07D211/18
CPC分类号： C07D405/06 , C07D211/32
摘要： 4-Aroylethnyl-1-piperidinobutyrophenone derivatives and pharmaceutically acceptable salts thereof of the following general structure: ##STR1## wherein R is hydrogen, alkyl, alkoxy, halogen or trifluoromethyl; and R' is hydrogen or halogen, are useful as antipsychotic agents. The novel compounds are produced by aldol condensation of an acetophenone with a protected 4-(4-formyl-1-piperidino)-butyrophenone.
摘要翻译： 4-芳基-1-哌啶基丁酰苯衍生物及其药学上可接受的盐，具有以下通用结构：其中R是氢，烷基，烷氧基，卤素或三氟甲基; 和R'是氢或卤素，可用作抗精神病药。该新化合物通过苯乙酮与受保护的4-（4-甲酰基-1-哌啶子基） - 丁酰苯的醛醇缩合而产生。

7. 发明授权

US4284636A Cinnamoylpiperidinobutyrophenone antipsychotic agents 失效
标题翻译：肉桂酰哌啶基丁酰苯胺抗精神病药
公开(公告)号：US4284636A
公开(公告)日：1981-08-18
申请号：US072498
申请日：1979-09-04
申请人： Albert A. Carr , Robert A. Farr
发明人： Albert A. Carr , Robert A. Farr
IPC分类号： A61K31/443 , A61K31/445 , A61K31/451 , A61P25/20 , C07D211/32 , C07D211/62 , C07D405/06 , C07D211/70
CPC分类号： C07D211/32 , C07D211/62
摘要： Cinnamoylpiperidinobutyrophenone derivatives and pharmaceutically acceptable salts thereof of the following general structure: ##STR1## wherein R is hydrogen, alkyl, alkoxy, halogen or trifluoromethyl; and R' is hydrogen or halogen; are useful as antipsychotic agents. The novel compounds are produced by aldol condensation of a benzaldehyde with a protected 4-(4-acetyl-1-piperidino)-butyrophenone.
摘要翻译：肉桂酰基哌啶基丁酰苯衍生物及其药学上可接受的盐，具有以下通用结构：其中R是氢，烷基，烷氧基，卤素或三氟甲基; 和R'是氢或卤素; 可用作抗精神病药。新化合物通过苯甲醛与受保护的4-（4-乙酰基-1-哌啶子基） - 丁酰苯的醛醇缩合产生。

8. 发明授权

US5240707A Alpha-mannosidase and fucosidase inhibitors 失效
标题翻译： α-甘露糖苷酶和岩藻糖苷酶抑制剂
公开(公告)号：US5240707A
公开(公告)日：1993-08-31
申请号：US666742
申请日：1991-03-13
申请人： Robert A. Farr , Norton P. Peet
发明人： Robert A. Farr , Norton P. Peet
IPC分类号： C07C215/44 , C07H15/18 , C07H15/203
CPC分类号： C07H15/203 , C07C215/44 , C07H15/18 , C07C2101/08
摘要： Substituted (1.alpha.,2.beta.,3.alpha. or .beta.,4.alpha.,5.alpha. or .beta.)-2,3,4-trihydroxy-5-(hydroxymethyl)cyclopentylamines are inhibitors of alpha-mannosidase and alpha-fucosidase and are useful immunostimulants, antiviral and antimetastatic agents.
摘要翻译：取代的（1α，2β，3α或β，4α，5α或β）-2,3,4-三羟基-5-（羟甲基）环戊胺是α-甘露糖苷酶和α-岩藻糖苷酶的抑制剂，并且是有用的免疫刺激剂，抗病毒和抗转移剂。

9. 发明授权

US5563157A Heterocycle substituted propenoic acid derivatives and pharmaceutical compositions thereof 失效
标题翻译：杂环取代的丙烯酸衍生物及其药物组合物
公开(公告)号：US5563157A
公开(公告)日：1996-10-08
申请号：US332016
申请日：1994-10-31
申请人： Boyd L. Harrison , Philip L. Nyce , Robert A. Farr
发明人： Boyd L. Harrison , Philip L. Nyce , Robert A. Farr
IPC分类号： A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/28 , C07D401/06 , C07D405/06 , C07D407/06 , C07D409/06
CPC分类号： C07D401/06 , C07D407/06 , C07D409/06
摘要： The present invention is new 3-(heterocyclic)-propenoic acid derivatives and pharmaceutical compositions thereof. These new 3-(heterocyclic)-propenoic acid derivatives are useful as NMDA antagonist.
摘要翻译：本发明是新的3-（杂环） - 丙烯酸衍生物及其药物组合物。这些新的3-（杂环） - 丙烯酸衍生物可用作NMDA拮抗剂。

10. 发明授权

US4321382A 2-Amino-11b-aryl-benzo[a]quinolizines 失效
公开(公告)号：US4321382A
公开(公告)日：1982-03-23
申请号：US65668
申请日：1979-08-10
申请人： Charles A. Lundberg, Jr. , Robert A. Farr
发明人： Charles A. Lundberg, Jr. , Robert A. Farr
IPC分类号： C07D455/06
CPC分类号： C07D455/06
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, a straight or branched chain alkyl of 1-5 carbon atoms or a straight or branched chain alkanoyl of 1-5 carbon atoms;R.sub.2 is hydrogen, a straight or branched chain alkyl of 1-5 carbon atoms, phenyl, phenyl substituted with halogen, a straight or branched chain alkoxy of 1-5 carbon atoms, a straight or branched chain alkyl of 1-5 carbon atoms or trifluoromethyl or, when R.sub.1 is hydrogen, R.sub.2 can also be a straight or branched chain alkanoyl of 1-5 carbon atoms; orR.sub.1 and R.sub.2 taken together with the nitrogen atom to which they are attached form a saturated heterocyclic ring of 4-7 total ring atoms and 0 or 1 hetero N or O atom in addition to the connecting N atom; or the corresponding heterocyclic ring substituted by a C.sub.1-5 straight or branched chain alkyl group, aryl or aralkyl;R.sub.3 is hydrogen, primary or secondary alkyl of 1-5 carbon atoms, phenyl or phenyl substituted by halogen, a straight or branched chain alkoxy of 1-5 carbon atoms, a straight or branched chain alkyl of 1-5 carbon atoms or trifluoromethyl;R.sub.4 is hydrogen or a straight or branched chain alkyl of 1-5 carbon atoms;each of R.sub.5 and R.sub.6 is, independently, hydrogen, halogen, a straight or branched chain alkyl of 1-5 carbon atoms, a straight or branched chain alkoxy of 1-5 carbon atoms, trifluoromethyl, a C.sub.3-6 alkyleneimino attached via the nitrogen atom and optionally substituted by a straight or branched chain C.sub.1-5 alkyl, or NR'R" wherein each of R' and R" is, independently, hydrogen or a straight or branched chain alkyl of 1-5 carbon atoms; andeach of R.sub.7 and R.sub.8 is, independently, hydrogen, halogen, a straight or branched chain alkyl of 1-5 carbon atoms, a straight or branched chain alkoxy of 1-5 carbon atoms, hydroxy, carboxy or phenyl;and the pharmaceutically acceptable acid addition salts thereof;are useful as antisecretory, antiinflammatory, antihistaminic, antiallergenic, antiseritonin, anticonvulsant and analgesic agents.

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