专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US4508724A Aryloxymethylpyrrolidinols and piperidinols having antidepressant, antiarrhythmic or hypotensive activity 失效
标题翻译：具有抗抑郁，抗心律失常或降血压活性的芳氧基甲基吡咯烷醇和哌啶醇
公开(公告)号：US4508724A
公开(公告)日：1985-04-02
申请号：US576904
申请日：1984-02-03
申请人： Chandler R. Taylor, Jr. , Harold F. Stauffer, Jr.
发明人： Chandler R. Taylor, Jr. , Harold F. Stauffer, Jr.
IPC分类号： A61K31/40 , A61K31/445 , A61K31/4465 , A61P9/06 , A61P9/12 , A61P25/24 , A61P25/26 , C07D207/12 , C07D211/42 , C07D211/48 , C07D491/107
CPC分类号： C07D211/42 , C07D207/12 , C07D211/48
摘要： Novel aryloxymethylpyrrolidinols and piperidinols are provided of the formula: ##STR1## wherein R.sup.1 is hydrogen, loweralkyl and phenylloweralkyl; R.sup.2 is hydrogen, loweralkyl and acyl; R.sup.3 is phenyl, naphthyl, 4-indanyl and 5-indanyl; m is 2 or 3 and n is 1 or 2; and the pharmaceutically acceptable salts thereof, having antiarrhythmic, antidepressant and antihypertensive activity.
摘要翻译：提供下式的新型芳氧基甲基吡咯烷醇和哌啶醇：其中R 1是氢，低级烷基和苯基低级烷基; R2是氢，低级烷基和酰基; R3是苯基，萘基，4-二氢化茚基和5-二氢化茚基; m为2或3，n为1或2; 和其药学上可接受的盐，具有抗心律失常药，抗抑郁药和抗高血压药。

2. 发明授权

US5151418A Method of treating muscular tension, muscle spasticity and anxiety with 3-aryloxy and 3-arylthioazetidinecarboxamides 失效
标题翻译：用3-芳氧基和3-芳硫基氮杂环丁烷酰胺治疗肌肉紧张，肌肉痉挛和焦虑的方法
公开(公告)号：US5151418A
公开(公告)日：1992-09-29
申请号：US743486
申请日：1991-08-09
申请人： Chandler R. Taylor, Jr. , Albert D. Cale, Jr. , David N. Johnson , Harold F. Stauffer, Jr.
发明人： Chandler R. Taylor, Jr. , Albert D. Cale, Jr. , David N. Johnson , Harold F. Stauffer, Jr.
IPC分类号： A61K31/395 , A61K31/415 , A61K31/44 , A61K31/495 , C07D205/04 , C07D401/12 , C07D521/00
CPC分类号： C07D231/12 , A61K31/395 , A61K31/415 , A61K31/44 , A61K31/495 , C07D205/04 , C07D233/56 , C07D249/08 , C07D401/12
摘要： A method of treating animals to obtain muscle relaxation and/or to relieve anxiety is disclosed utilizing novel and known 3-aryloxy and 3-arylthioazetidinecarboxamides having the formula: ##STR1## wherein Z is oxygen or sulfur; B is oxygen or sulfur; Ar is pyridyl or halo substituted pyridyl, phenyl or substituted phenyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, aryl, allyl groups, propargyl, cycloalkyl, loweralkylcycloalkyl, cycloalkylloweralkyl, arylloweralkyl and diloweralkylaminoalkyl, and R.sup.1 and R.sup.2 when taken together with the adjacent nitrogen atom may form a heterocyclic amine radical; R.sup.3 is hydrogen, loweralkyl, aryl or arylloweralkyl, and the geometrical isomers thereof and pharmaceutical salts thereof and hydrates thereof when they are possible.
摘要翻译：公开了一种用于治疗动物以获得肌肉松弛和/或缓解焦虑的方法，其利用新颖且已知的具有下列结构式的3-芳氧基和3-芳硫基氮杂环丁烷酰胺：其中Z是氧或硫; B是氧或硫; Ar是吡啶基或卤素取代的吡啶基，苯基或取代的苯基; R1和R2是氢，低级烷基，芳基，烯丙基，炔丙基，环烷基，低级烷基环烷基，环烷基低级烷基，芳基低级烷基和二低级烷基氨基烷基，当与相邻的氮原子一起时，R 1和R 2可以形成杂环胺基; 当可能时，R3是氢，低级烷基，芳基或芳基低级烷基，及其几何异构体及其药用盐及其水合物。

3. 发明授权

US5114944A 2-phenylpyrazolo[1,5-a]pyrimidine-3-acetic acid derivatives exhibiting therapeutic effects 失效
标题翻译：具有治疗作用的2-苯基吡唑并[1,5-a]嘧啶-3-乙酸衍生物
公开(公告)号：US5114944A
公开(公告)日：1992-05-19
申请号：US684247
申请日：1991-04-12
申请人： Chandler R. Taylor, Jr. , Harold F. Stauffer, Jr. , Bruce E. Tomczuk
发明人： Chandler R. Taylor, Jr. , Harold F. Stauffer, Jr. , Bruce E. Tomczuk
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： This invention provides a 2-arylpyrazolo[1,5-a]pyrimidine-3-acetic acid corresponding to the formula: ##STR1## where X is hydrogen or a halogen, hydroxy, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy substituent; Y is hydrogen or a halogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy substituent; Z is a hydroxy, C.sub.1 -C.sub.4 alkoxy or --NRR substituent; and R is hydrogen or a C.sub.1 -C.sub.4 alkyl substituent; or a pharmaceutically acceptable salt thereof which is useful as a therapeutic agent which exhibits anxiolytic, anticonvulsant and muscle relaxant effects in a warm blooded animal.
摘要翻译：本发明提供对应于下式的其中X为氢或卤素，羟基，C 1 -C 4烷基或C 1 -C 4烷氧基的2-芳基吡唑并[1,5-a]嘧啶-3-乙酸取代基; Y是氢或卤素，C 1 -C 4烷基或C 1 -C 4烷氧基取代基; Z是羟基，C 1 -C 4烷氧基或-NRR取代基; 且R为氢或C 1 -C 4烷基取代基; 或其药学上可接受的盐，其可用作在温血动物中表现出抗焦虑，抗惊厥和肌肉松弛作用的治疗剂。

4. 发明授权

US5057534A 3-amino-5-arylpyrazole-4-acetic acid derivatives exhibiting therapeutic effects 失效
标题翻译：具有治疗作用的3-氨基-5-芳基吡唑-4-乙酸衍生物
公开(公告)号：US5057534A
公开(公告)日：1991-10-15
申请号：US684325
申请日：1991-04-12
申请人： Chandler R. Taylor, Jr. , Harold F. Stauffer, Jr. , Bruce E. Tomczuk
发明人： Chandler R. Taylor, Jr. , Harold F. Stauffer, Jr. , Bruce E. Tomczuk
IPC分类号： C07D231/38
CPC分类号： C07D231/38
摘要： This invention provides novel pyrazole-4-acetic acid derivatives which have utility as therapeutic agents which exhibit anxiolytic, anticonvulsant and muscle relaxant effects in warm blooded animals.Illustrative of an invention compound is 3-(dimethylamino)-5-(4-methylphenyl)-1H-pyrazole-4-acetamide: ##STR1##
摘要翻译：本发明提供了新的吡唑-4-乙酸衍生物，其具有在温血动物中表现出抗焦虑，抗惊厥和肌肉松弛作用的治疗剂。示例性的本发明化合物是3-（二甲基氨基）-5-（4-甲基苯基）-1H-吡唑-4-乙酰胺：

5. 发明授权

US5183902A Method of treating muscular tension, muscle spasticity and anxiety with 3-aryloxy and 3-arylthioazetidinecarboxamides 失效
标题翻译：用3-芳氧基和3-芳硫基氮杂环丁烷酰胺治疗肌肉紧张，肌肉痉挛和焦虑的方法
公开(公告)号：US5183902A
公开(公告)日：1993-02-02
申请号：US743059
申请日：1991-08-09
申请人： Chandler R. Taylor, Jr. , Albert D. Cale, Jr. , Harold F. Stauffer, Jr.
发明人： Chandler R. Taylor, Jr. , Albert D. Cale, Jr. , Harold F. Stauffer, Jr.
IPC分类号： A61K31/395 , A61K31/415 , A61K31/44 , A61K31/495 , C07D205/04 , C07D401/12 , C07D521/00
CPC分类号： C07D231/12 , A61K31/395 , A61K31/415 , A61K31/44 , A61K31/495 , C07D205/04 , C07D233/56 , C07D249/08 , C07D401/12
摘要： A method of treating animals to obtain muscle relaxation and/or to relieve anxiety is disclosed utilizing novel and known 3-aryloxy and 3-arylthioazetidinecarboxamides having the formula: ##STR1## wherein Z is oxygen or sulfur; B is oxygen or sulfur; Ar is pyridyl or halo substituted pyridyl, phenyl or substituted phenyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, aryl, allyl groups, propargyl, cycloalkyl, loweralkylcycloalkyl, cycloalkylloweralkyl, arylloweralkyl and diloweralkylaminoalkyl, and R.sup.1 and R.sup.2 when taken together with the adjacent nitrogen atom may form a heterocyclic amine radical; R.sup.3 is hydrogen, loweralkyl, aryl or arylloweralkyl, and the geometrical isomers thereof and pharmaceutical salts thereof and hydrates thereof when they are possible.
摘要翻译：公开了一种用于治疗动物以获得肌肉松弛和/或缓解焦虑的方法，其利用新颖且已知的具有下列结构式的3-芳氧基和3-芳硫基氮杂环丁烷酰胺：其中Z是氧或硫; B是氧或硫; Ar是吡啶基或卤素取代的吡啶基，苯基或取代的苯基; R1和R2是氢，低级烷基，芳基，烯丙基，炔丙基，环烷基，低级烷基环烷基，环烷基低级烷基，芳基低级烷基和二低级烷基氨基烷基，当与相邻的氮原子一起时，R 1和R 2可以形成杂环胺基; 当可能时，R3是氢，低级烷基，芳基或芳基低级烷基，及其几何异构体及其药用盐及其水合物。

6. 发明授权

US5068231A Method of treating muscular tension, muscle spasticity and anxiety with 3-aryloxy and 3-arylthioazetidinecarboxamides 失效
标题翻译：用3-芳氧基和3-芳硫基氮杂环丁烷酰胺治疗肌肉紧张，肌肉痉挛和焦虑的方法
公开(公告)号：US5068231A
公开(公告)日：1991-11-26
申请号：US921521
申请日：1986-10-22
申请人： Chandler R. Taylor, Jr. , Albert D. Cale. Jr. , David N. Johnson , Harold F. Stauffer. Jr.
发明人： Chandler R. Taylor, Jr. , Albert D. Cale. Jr. , David N. Johnson , Harold F. Stauffer. Jr.
IPC分类号： A61K31/395 , A61K31/415 , A61K31/44 , A61K31/495 , C07D205/04 , C07D401/12 , C07D521/00
CPC分类号： C07D231/12 , A61K31/395 , A61K31/415 , A61K31/44 , A61K31/495 , C07D205/04 , C07D233/56 , C07D249/08 , C07D401/12
摘要： A method of treating animals to obtain muscle relaxation and/or to relieve anxiety is disclosed utilizing novel and known 3-aryloxy and 3-arylthioazetidinecarbonxamides having the formula: ##STR1## wherein Z is oxygen or sulfur; B is oxygen or sulfur; Ar is pyridyl or halo substituted pyridyl, phenyl or substituted phenyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, aryl, allyl groups, propargyl, cycloalkyl, loweralkylcycloalkyl, cycloakylloweralkyl, arylloweralkyl and diloweralkylaminoalkyl, and R.sup.1 and R.sup.2 when taken together with the adjacent nitrogen atom may form a heterocyclic amine radical; R.sup.3 is hydrogen, loweralkyl, aryl or arylloweralkyl, and the geometrical isomers thereof and pharmaceutical salts thereof and hydrates thereof when they are possible.
摘要翻译：公开了一种用于治疗动物以获得肌肉松弛和/或减轻焦虑的方法，其利用新颖且已知的具有下式的其中Z为氧或硫的3-芳氧基和3-芳基硫代氮杂环丁烷酰胺。 B是氧或硫; Ar是吡啶基或卤素取代的吡啶基，苯基或取代的苯基; R1和R2是氢，低级烷基，芳基，烯丙基，炔丙基，环烷基，低级烷基环烷基，环亚烷基低级烷基，芳基低级烷基和二低级烷基氨基烷基，当与相邻的氮原子一起时，R 1和R 2可以形成杂环胺基; 当可能时，R3是氢，低级烷基，芳基或芳基低级烷基，及其几何异构体及其药用盐及其水合物。

7. 发明授权

US4956359A 3-aryloxy and 3-arylthioazetidinecarboxamides as anticonvulsants and antiepileptics 失效
标题翻译： 3-芳氧基和3-芳基硫代氮杂环丁烷酰胺作为抗惊厥药和抗癫痫药
公开(公告)号：US4956359A
公开(公告)日：1990-09-11
申请号：US921466
申请日：1986-10-22
申请人： Chandler R. Taylor, Jr. , Albert D. Cale, Jr. , Harold F. Stauffer, Jr.
发明人： Chandler R. Taylor, Jr. , Albert D. Cale, Jr. , Harold F. Stauffer, Jr.
IPC分类号： A61K31/395 , A61K31/415 , A61K31/44 , A61K31/495 , C07D205/04 , C07D401/12 , C07D521/00
CPC分类号： C07D231/12 , A61K31/395 , A61K31/415 , A61K31/44 , A61K31/495 , C07D205/04 , C07D233/56 , C07D249/08 , C07D401/12
摘要： Novel 3-aryloxy and 3-arylthioazetidinecarboxamides having utility in a method of treating convulsions and epilepsy and compositions therefor are disclosed having the formula: ##STR1## wherein Z is oxygen or sulfur; B is oxygen or sulfur; Ar is pyridyl or halo-substituted-pyridyl, phenyl or substituted phenyl; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, aryl, allyl, substituted allyl, propargyl, cycloalkyl, loweralkylcycloalkyl, cycloalkylloweralkyl, arylloweralkyl, diloweralkylaminoloweralkyl, and R.sup.1 and R.sup.2 when taken with the adjacent nitrogen atom may form a heterocyclic radical; R.sup.3 is hydrogen, loweralkyl, aryl or arylloweralkyl, and the geometrical isomers thereof, excepting that when R.sup.3 is hydrogen, Z is oxygen, B is oxygen, and Ar is phenyl or phenyl substituted by trifluoromethyl or aminocarbonyl, then R.sup.1 and R.sup.2 cannot be a combination of hydrogen and loweralkyl, and the further exception that when R.sup.3 is hydrogen, Z is oxygen, B is oxygen, and Ar is phenyl or phenyl substituted by fluoro, loweralkyl, loweralkoxy, trifluoromethyl, acetyl, or aminocarbonyl, then R.sup.1 and R.sup.2 cannot both be hydrogen.
摘要翻译：公开了一种在治疗惊厥和癫痫的方法中有效的新型3-芳氧基和3-芳硫基氮杂环丁烷甲酰胺及其组合物，其具有下式：其中Z为氧或硫; B是氧或硫; Ar是吡啶基或卤素取代的吡啶基，苯基或取代的苯基; R 1和R 2选自氢，低级烷基，芳基，烯丙基，取代的烯丙基，炔丙基，环烷基，低级烷基环烷基，环烷基低级烷基，芳基低级烷基，二低级烷基氨基低级烷基，当与相邻的氮原子一起使用时，R 1和R 2可以形成杂环基; R3是氢，低级烷基，芳基或芳基低级烷基，及其几何异构体，不同之处在于当R3为氢时，Z为氧，B为氧，Ar为苯基或被三氟甲基或氨基羰基取代的苯基，则R1和R2不能为氢和低级烷基的组合，另外例外的是当R3为氢时，Z为氧，B为氧，Ar为苯基或被氟，低级烷基，低级烷氧基，三氟甲基，乙酰基或氨基羰基取代的苯基，则R1和R2不能都是氢气。

8. 发明授权

US4871737A 3-Amino-5-methyl-1H-pyrazole-4-carboxylic acids and esters thereof as anticonvulsants muscle relaxants and anxiolytics 失效
标题翻译： 3-氨基-5-甲基-1H-吡唑-4-羧酸及其作为抗惊厥药的肌肉松弛剂和抗焦虑药
公开(公告)号：US4871737A
公开(公告)日：1989-10-03
申请号：US324074
申请日：1989-03-16
申请人： Chandler R. Taylor, Jr. , Harold F. Stauffer, Jr.
发明人： Chandler R. Taylor, Jr. , Harold F. Stauffer, Jr.
IPC分类号： C07D231/38 , C07D401/12
CPC分类号： C07D231/38 , C07D401/12
摘要： A novel method of controlling epilepsy, muscle tension, muscular spasticity, and anxiety in living animal bodies by administering compounds of the formula: ##STR1## wherein: R.sup.1 is hydrogen, loweralkyl or a pharmaceutically acceptable cation;R.sup.2 and R.sup.3, same or different, are hydrogen, loweralkyl, aryl, cycloalkyl, loweralkenyl, 1-adamantyl, heterocyclicaminoalkyl, diloweralkylaminoloweralkyl, or R.sup.2 with R.sup.3 and adjacent nitrogen may form a heterocyclic ring structure; and the pharmaceutical acceptable acid salts, and tautomeric isomers thereof; and novel pharmaceutical compositions therefor are disclosed.
摘要翻译：一种通过施用下式的化合物来控制活体动物体内的癫痫，肌肉紧张，肌肉痉挛和焦虑的新方法：其中：R1是氢，低级烷基或药学上可接受的阳离子; R 2和R 3相同或不同，为氢，低级烷基，芳基，环烷基，低级烯基，1-金刚烷基，杂环氨基烷基，二低级烷基氨基低级烷基，或具有R 3和相邻氮的R 2可以形成杂环结构; 和药学上可接受的酸式盐及其互变异构体; 并公开了其新颖的药物组合物。

9. 发明授权

US5095014A 3-(2-chloro-4-(trifluoromethyl)phenoxy)-1-azetidine carboxamides having anticonvulsant activity 失效
标题翻译：具有抗惊厥活性的3-（2-氯-4-（三氟甲基）苯氧基）-1-氮杂环丁烷甲酰胺
公开(公告)号：US5095014A
公开(公告)日：1992-03-10
申请号：US623517
申请日：1990-12-07
申请人： Chandler R. Taylor, Jr. , Albert D. Cale, Jr. , Harold F. Stauffer, Jr.
发明人： Chandler R. Taylor, Jr. , Albert D. Cale, Jr. , Harold F. Stauffer, Jr.
IPC分类号： A61K31/40 , A61K31/397 , A61P25/08 , C07D205/04
CPC分类号： C07D205/04
摘要： The present invention relates to novel 3-(2-chlor-4-trifluoromethylphenoxy)-1-azetidine carboxamides having the formula: ##STR1## wherein R1 and R2, same or different, are selected from hydrogen, C.sub.1 -C.sub.4 alkyl, and allyl.In a series of 3-(substitutedphenoxy)-1-azetidinecarboxamides, introduction of a chlorine atom at the 2-position of the phenoxy group of the corresponding 4-trifluoromethylphenoxy-1-azetidinecarboxamides resulted in unexpected increased potency in anticonvulsant pharmacological tests.
摘要翻译：本发明涉及具有下式的新型3-（2-氯-4-三氟甲基苯氧基）-1-氮杂环丁烷羧酰胺，其中R1和R2相同或不同，选自氢，C1-C4烷基和烯丙基。在一系列3-（取代的苯氧基）-1-氮杂环丁烷酰胺中，在相应的4-三氟甲基苯氧基-1-氮杂环丁烷酰胺的苯氧基的2-位上引入氯原子导致抗惊厥药理学试验中意想不到的增加的效力。

10. 发明授权

US4826866A 3-amino-5-methyl-1H-pyrazole-4-carboxylic acids and esters thereof as anticonvulsants, muscle relaxants and anxiolytics 失效
标题翻译： 3-氨基-5-甲基-1H-吡唑-4-羧酸及其酯作为抗惊厥剂，肌肉松弛剂和抗焦虑剂
公开(公告)号：US4826866A
公开(公告)日：1989-05-02
申请号：US115918
申请日：1987-11-02
申请人： Chandler R. Taylor, Jr. , Harold F. Stauffer, Jr.
发明人： Chandler R. Taylor, Jr. , Harold F. Stauffer, Jr.
IPC分类号： A61K31/415 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/535 , A61P21/02 , A61P25/08 , A61P25/20 , C07D231/38 , C07D401/12
CPC分类号： C07D231/38 , C07D401/12
摘要： A novel method of controlling epilepsy, muscle tension, muscular spasticity, and anxiety in living animal bodies by administering compounds of the formula: ##STR1## wherein: R.sup.1 is hydrogen, loweralkyl or a pharmaceutically acceptable cation;R.sup.2 and R.sup.3, same or different, are hydrogen, loweralkyl, aryl, cycloalkyl, loweralkenyl, 1-adamantyl, heterocyclicaminoalkyl, diloweralkylaminoloweralkyl, or R.sup.2 with R.sup.3 and adjacent nitrogen may form a heterocyclic ring structure; and the pharmaceutical acceptable acid salts, and tautomeric isomers thereof; and novel pharmaceutical compositions therefor are disclosed.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式