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21. 发明授权

US4178442A Novel cinnamoyles piperazines and homopiperazines, the method of preparing them and their application in therapeutics 失效
标题翻译：新型肉桂酰基哌嗪和高哌嗪，其制备方法及其在治疗中的应用
公开(公告)号：US4178442A
公开(公告)日：1979-12-11
申请号：US894965
申请日：1978-04-10
申请人： Guy R. Bourgery , Alain P. Lacour , Gerard H. Moinet , Bernard M. Pourrias , Anne-Marie P. Ruch
发明人： Guy R. Bourgery , Alain P. Lacour , Gerard H. Moinet , Bernard M. Pourrias , Anne-Marie P. Ruch
IPC分类号： C07D243/08 , A61K31/395 , A61K31/495 , A61P9/08 , A61P43/00 , C07C273/18 , C07C275/34 , C07D241/04 , C07D295/08 , C07D295/16 , C07D295/18 , C07D295/185 , C07D303/22 , C07D313/08 , C07D317/00 , C07D317/54 , C07D317/64 , C07D317/66 , C07D317/68 , C07D319/00 , C07D319/18 , C07D321/00 , C07D321/10 , C07D325/00 , C07D405/12 , C07D407/12 , C07D413/12
CPC分类号： C07D295/185 , C07C273/1827 , C07C323/00 , C07D303/22 , C07D317/54 , C07D317/64 , C07D317/66 , C07D317/68 , C07D319/18 , C07D321/10
摘要： Cinnamoyl piperazine and homopiperazine derivatives which possess antiangorous activity and activities on the peripheral and cerebral circulation.
摘要翻译：肉桂酰哌嗪和具有抗周血和脑循环活性的抗高血压的高哌嗪衍生物。

22. 发明授权

US4150029A 3-Aryl 2-oxazolidinones, their process of preparation and their therapeutical application 失效
标题翻译： 3-芳基2-恶唑烷酮，其制备方法及其治疗应用
公开(公告)号：US4150029A
公开(公告)日：1979-04-17
申请号：US771814
申请日：1977-02-23
申请人： Philippe L. Dostert , Colette A. Douzon , Guy R. Bourgery , Claude J. Gouret , Gisele C. Mocquet , Jean A. Coston
发明人： Philippe L. Dostert , Colette A. Douzon , Guy R. Bourgery , Claude J. Gouret , Gisele C. Mocquet , Jean A. Coston
IPC分类号： A61K31/42 , A61K31/421 , A61P25/24 , A61P25/26 , C07D263/24
CPC分类号： C07D263/24
摘要： Compounds having the formula ##STR1## wherein R.sub.1 is hydrogen or CONHR.sub.7 and R.sub.7 is methyl or isopropyl,And whereinWhen R.sub.1 is hydrogen: R is p-nitro, p-cyano; p-aldehydo; p-acetyl; m-ethyl; m-nitro; m-bromo; 3,4-dimethyl; m-NH.sub.2 ; p-methylamino; p-dimethylamino; p-diethylamino; p-methylbenzylamino; p-pyrrolidino; p-piperidino; SR.sub.4 in para position in which R.sub.4 is alkyl having 1 to 4 carbon atoms or cyclohexyl; OR.sub.5 is para position in which R.sub.5 is alkyl having 2 to 7 carbon atoms, cyclohexyl, cyclohexylmethyl, acetylmethyl; cyanomethyl, alkene-2 yl having 3 to 5 carbon atoms, butene-3 yl, cyclohexene-1 methyl, propargyl, butyne-2 yl, ##STR2## in which n is one or 2 and when n is one, R.sub.6 is hydrogen, o-fluoro, o-methyl, m-chloro, m-fluoro, m-methyl, m-trifluoromethyl, p-chloro, p-bromo-, p-fluoro, p-cyano, p-nitro or p-dimethylamino and when n is 2, R.sub.6 is hydrogen; and 3-methyl-4-benzyloxy:When R.sub.1 is CONHR.sub.7 and R.sub.7 is methyl: R is m-trifluoromethyl; m-bromo; p-chloro; p-fluoro; 3,4-dichloro; p-thiomethyl; p-acetyl; OR.sub.8 in para position wherein R.sub.8 is alkyl having 2 to 5 carbon atoms, cyanomethyl, acetylmethyl, propargyl or ##STR3## in which R.sub.9 is hydrogen, m-chloro, m-bromo, m-fluoro, p-fluoro, p-chloro or p-nitro;And when R.sub.1 is CONHR.sub.7 and R.sub.7 is isopropyl; R is m-trifluoromethyl or p-benzyloxy.The compounds are prepared by cyclizing 1-phenylamino-2,3-propandiol derivatives to form 5-hydroxymethyl-3 phenyl-2-oxozolidinone derivatives. The 5-hydroxymethyl group can be transformed to --CH.sub.2 OCONHR.sub.7 by reaction with methyl isocyanate or isopropyl isocyanate. The compounds possess psychotropic, particularly antidepressant, activity.
摘要翻译：具有式“IMAGE”的化合物，其中R1是氢或CONHR7，R7是甲基或异丙基，当R1是氢时，R是对硝基，对氰基; 对醛对乙酰基; 甲基; 间硝基溴代 3,4-二甲基 m-NH2; 对甲基氨基; 对二甲基氨基; 对二乙基氨基; 对甲基苄基氨基; 对 - 吡咯烷子; 对哌啶子其中R4是具有1-4个碳原子的烷基的对位的SR4或环己基; OR5是R5是具有2至7个碳原子的烷基的对位，环己基，环己基甲基，乙酰基甲基; 氰基甲基，具有3至5个碳原子的烯-2，丁烯-3，环己烯-1甲基，炔丙基，丁炔-2基，其中n为1或2，当n为1时，R6为氢，邻 - 甲基，间 - 氯，间氟，间甲基，间三氟甲基，对氯，对溴 - ，对氟，对氰基，对硝基或对二甲基氨基，当 n为2，R6为氢; 和3-甲基-4-苄氧基：

23. 发明授权

US4031089A Furo (2,3d) pyrimidines 失效
标题翻译：呋喃（2,3d）嘧啶
公开(公告)号：US4031089A
公开(公告)日：1977-06-21
申请号：US715377
申请日：1976-08-18
申请人： Claude P. Fauran , Guy R. Bourgery , Guy M. Raynaud , Nicole A. M. Dorme
发明人： Claude P. Fauran , Guy R. Bourgery , Guy M. Raynaud , Nicole A. M. Dorme
IPC分类号： C07D491/04 , C07D491/048
CPC分类号： C07D491/04 , Y10S514/869 , Y10S514/927
摘要： Compounds of the formula ##STR1## wherein R is alkyl of 1-4 carbon atoms, phenyl, or phenyl substituted by one or more halogen or trifluoromethyl, and Z is ##STR2## wherein R.sub.1 is hydrogen, alkyl of 1-4C, 2,2-dimethyldioxolan-4-yl methyl, or 2,3-dihydroxy prop-1-yl, R.sub.2 is ##STR3## wherein ##STR4## is morpholino, pyrrolidino, piperidino or hexamethyleneimino, and n is an integer from 4 to 7.The compounds are prepared by reacting R-substituted 4-chloro-2-methyl furo (2,3d) pyrimidine with HZ. The compounds possess antiulcerous, antibronchoconstrictive and anticholinergic, analgesic, antihistamine, diuretic, cardiovascular analeptic, antiinflammatory and hypertensive properties.
摘要翻译：其中R是1-4个碳原子的烷基，苯基或被一个或多个卤素或三氟甲基取代的苯基，Z是下式的化合物，其中R 1是氢，1-4C的烷基，2,2-二甲基二氧杂环戊烷-4-基甲基或2,3-二羟基丙-1-基，其中，作为吗啉，吡咯烷子基，哌啶子基或哌啶子基，六亚甲基亚氨基，n为4〜7的整数。

24. 发明授权

US3971793A Certain 6-(dialkylamino, pyrrolidino and piperidino)ethoxy-4,7-dimethoxy-5-(3-phenyl-1-hydroxypropyl)2,3-dihydrob enzofurans 失效
标题翻译：某些6-（二烷基氨基，吡咯烷子基和哌啶子基）乙氧基-4,7-二甲氧基-5-（3-苯基-1-羟丙基）2,3-二氢苯并呋喃
公开(公告)号：US3971793A
公开(公告)日：1976-07-27
申请号：US438744
申请日：1974-02-01
申请人： Claude P. Fauran , Jeannine A. Eberle , Guy R. Bourgery , Guy M. Raynaud , Bernard M. Pourrias
发明人： Claude P. Fauran , Jeannine A. Eberle , Guy R. Bourgery , Guy M. Raynaud , Bernard M. Pourrias
IPC分类号： C07D307/86 , C07D211/22
CPC分类号： C07D307/86 , Y10S514/821 , Y10S514/869 , Y10S514/929
摘要： A compound of the formula ##SPC1##In which R is hydrogen, hydroxy, halogen or alkoxy containing up to 3 carbon atoms, and ##EQU1## is dialkylamino in which the alkyls contain up to 3 carbon atoms, or pyrrolidino, piperidino, morpholino or hexamethyleneimino, and n is 2 or 3. The compounds are prepared by reacting R substituted benzaldehyde with a 2,3-dihydrobenzofuran derivative and then reducing that reaction product. The compounds possess antihypertensive, hypotensive, vasodilatatory, spasmolytic, diuretic, sedative, anti-arythmic and anti-inflammatory properties.
摘要翻译：式中R为氢，羟基，卤素或至多3个碳原子的烷氧基的化合物，R 1 -N ANGLE R 2为烷基含有最多3个碳原子的二烷基氨基，或吡咯烷基，哌啶子基，吗啉代或六亚甲基亚氨基，n为2或3.通过使R取代的苯甲醛与2,3-二氢苯并呋喃衍生物反应然后还原该反应产物来制备化合物。该化合物具有抗高血压，降血压，血管扩张，解痉，利尿，镇静，抗胂和抗炎等功能。

25. 发明授权

US4153620A Certain N-5-[4,7-dimethoxy)-6-(monoalkylaminoethoxy, monocycloalkylaminoethoxy, or dialkylaminoethoxy) benzofuranyl], N'-methyl or ethyl ureas 失效
标题翻译：某些N-5- {8 4,7-二甲氧基）-6-（单烷基氨基乙氧基，单环烷基氨基乙氧基或二烷基氨基乙氧基）苯并呋喃基{9，N {40-甲基或乙基脲
公开(公告)号：US4153620A
公开(公告)日：1979-05-08
申请号：US914872
申请日：1978-06-12
申请人： Guy R. Bourgery , Alain P. Lacour , Bernard M. Pourrias , Genevieve C. Bregeon
发明人： Guy R. Bourgery , Alain P. Lacour , Bernard M. Pourrias , Genevieve C. Bregeon
IPC分类号： C07D307/86
CPC分类号： C07D307/86
摘要： Aminoalkoxybenzofurans having the formula ##STR1## wherein ##STR2## are either (1) ##STR3## is monoalkylamino, dialkylamino, cycloalkylamino or heterocyclic amino, or (2) ##STR4## (H, 1, 4-methyl piperazino), ##STR5## is piperidino. The compounds possess antidysrhythmic properties.
摘要翻译：具有式的氨基烷氧基苯并呋喃是其中（IMAGE）是（1）IMAMA是单烷基氨基，二烷基氨基，环烷基氨基或杂环氨基，或（2）（H，1,4-甲基哌嗪子基）是哌啶子该化合物具有抗心律不齐的特性。

26. 发明授权

US4061855A Pyrimidin-6-yl acethydroxamic acids 失效
标题翻译：嘧啶-6-基乙酸异羟肟酸
公开(公告)号：US4061855A
公开(公告)日：1977-12-06
申请号：US749221
申请日：1976-12-10
申请人： Claude P. Fauran , Jeannine A. Eberle , Guy R. Bourgery , Guy R. Raynaud , Claude J. Gouret
发明人： Claude P. Fauran , Jeannine A. Eberle , Guy R. Bourgery , Guy R. Raynaud , Claude J. Gouret
IPC分类号： C07D413/12 , A61K31/535
CPC分类号： C07D413/12 , Y10S514/869 , Y10S514/925 , Y10S514/929
摘要： Compounds of the formula ##STR1## IN WHICH R is aminocarbonylphenyl in which amino is --NH.sub.2, pyrrolidino, piperidino or morpholino, and Ar is phenyl substituted with chloro, fluoro, trifluoromethyl, methylenedioxy or one or more methoxy. The compounds are prepared by reacting 2-Ar-4-chloropyrimidin-6-yl ethylacetate with ##STR2## and then reacting that reaction product with hydroxylamine hydrochloride. The compounds possess vasodilatatory, anti-ulcerous, respiratory analeptic, hypotensive, diuretic, anti-depressive, analgesic, anti-inflammatory and neurotropic properties.
摘要翻译：其中R为氨基羰基苯基的化合物，其中氨基为-NH 2，吡咯烷子基，哌啶子基或吗啉代，Ar为被氯，氟，三氟甲基，亚甲二氧基或一个或多个甲氧基取代的苯基。该化合物通过使2-氨基-4-氯嘧啶-6-基乙酸乙酯与“IMAGE”反应，然后使该反应产物与盐酸羟胺反应制备。该化合物具有血管舒张，抗溃疡，呼吸消炎，降血压，利尿，抗抑郁，镇痛，抗炎和神经营养特性。

27. 发明授权

US4041072A Acetamidoxime compounds 失效
标题翻译：乙酰肟化合物
公开(公告)号：US4041072A
公开(公告)日：1977-08-09
申请号：US668061
申请日：1976-03-18
申请人： Claude P. Fauran , Guy R. Bourgery , Claude J. Gouret
发明人： Claude P. Fauran , Guy R. Bourgery , Claude J. Gouret
IPC分类号： A61K31/165 , A61K31/15 , C07C251/32 , C07C259/14 , C07C103/28 , C07C103/365 , C07C103/76
CPC分类号： C07C259/14
摘要： Compounds having the formula ##STR1## wherein R is hydrogen, or chlorine, or alkyl having one to 4 carbons, or alkoxy having one to 3 carbons, and R.sub.1 is hydrogen, or ##STR2## or --CONH--R.sub.3, wherein R.sub.2 is hydrogen, or chlorine, or nitro, or alkoxy having no more than 3 carbons, or trifluoromethyl, and R.sub.3 is alkyl having one to 4 carbons, or cycloalkyl having no more than 6 carbons, or phenyl.The compounds are prepared by reacting R-substituted cyano-2 acetanilides with hydroxylamine to obtain compounds in which R.sub.1 is hydrogen, and then reacting with acid chlorides containing R.sub.2 or isocyanates containing R.sub.3. The compounds possess psychtropic properties.
摘要翻译：具有式“IMAGE”的化合物，其中R是氢或氯，具有1至4个碳的烷基或具有1至3个碳原子的烷氧基，R 1是氢，或者R 3是-CONH-R 3，其中R 2是氢或氯或硝基，或不多于3个碳原子的烷氧基，或三氟甲基，R3是具有1-4个碳原子的烷基，或不多于6个碳的烷基或苯基。

28. 发明授权

US4007187A Furo (2,3d) pyrimidines 失效
标题翻译：呋喃（2,3d）嘧啶
公开(公告)号：US4007187A
公开(公告)日：1977-02-08
申请号：US506826
申请日：1974-09-17
申请人： Claude P. Fauran , Guy R. Bourgery , Guy M. Raynaud , Nicole A. M. Dorme
发明人： Claude P. Fauran , Guy R. Bourgery , Guy M. Raynaud , Nicole A. M. Dorme
IPC分类号： A61K31/519 , C07D491/04 , C07D491/048 , C07D239/00
CPC分类号： C07D491/04
摘要： Compounds of the formula ##STR1## wherein R is alkyl of 1-4 carbon atoms, phenyl, or phenyl substituted by one or more halogen or trifluoromethyl, and Z is ##STR2## wherein R.sub.1 is hydrogen, alkyl of 1-4C, 2,2-dimethyldioxolan-4-yl methyl, or 2,3-dihydroxy prop-1-yl, R.sub.2 is ##STR3## wherein ##STR4## is morpholino, pyrrolidino, piperidino or hexamethyleneimino, and n is an integer from 4 to 7. The compounds are prepared by reacting R-substituted 4-chloro-2-methyl furo (2,3d) pyrimidine with HZ. The compounds possess antiulcerous, antibronchoconstrictive and anticholinergic, analgesic, antihistamine, diuretic, cardiovascular analeptic, antiinflammatory and hypertensive properties.
摘要翻译：其中R是1-4个碳原子的烷基，苯基或被一个或多个卤素或三氟甲基取代的苯基，Z是下式的化合物，其中R 1是氢，1-4C的烷基，2,2-二甲基二氧杂环戊烷-4-基甲基或2,3-二羟基丙-1-基，其中，作为吗啉，吡咯烷子基，哌啶子基或哌啶子基，六亚甲基亚氨基，n为4〜7的整数。该化合物通过R-取代的4-氯-2-甲基呋喃（2,3d）嘧啶与HZ反应来制备。该化合物具有抗溃疡，抗纤维蛋白胆固醇和抗胆碱能药，止痛药，抗组胺药，利尿剂，心血管镇痛药，抗炎和高血压药物。

29. 发明授权

US3978055A Arylamino pyrimidinic derivatives 失效
标题翻译：芳基嘧啶衍生物
公开(公告)号：US3978055A
公开(公告)日：1976-08-31
申请号：US502285
申请日：1974-09-03
申请人： Claude P. Fauran , Guy R. Bourgery , Guy M Raynaud , Claude J. Gouret
发明人： Claude P. Fauran , Guy R. Bourgery , Guy M Raynaud , Claude J. Gouret
IPC分类号： A61K31/505 , C07D239/42 , C07D401/10 , C07D401/12 , C07D403/10 , C07D413/10
CPC分类号： C07D239/42 , C07D401/12 , Y10S514/869 , Y10S514/906 , Y10S514/927 , Y10S514/929
摘要： Compounds of the formula ##SPC1##Wherein Ar is phenyl or phenyl substituted by one or more halogens, by a trifluoromethyl or a methylenedioxy, by one or more methoxy, by an alkyl having one to 4 carbon atoms or by a dimethylamino,And R is ##EQU1## or --O-- ##EQU2## or ##EQU3## wherein R.sub.1 and R.sub.2 each are hydrogen or alkyl of 1 to 4 carbon atoms, or ##EQU4## is pyrrolidino, morpholino, piperidino or piperazino N'-substituted by alkyl of 1 to 4 carbon atoms, or phenyl; R.sub.3 and R.sub.4 each are alkyl of 1 to 3 carbon atoms or ##EQU5## is morpholino, pyrrolidino, piperidino or hexamethyleneimino, n is an integer of 1 to 5; and R.sub.5 is alkyl of 1 to 4 carbon atoms, 2,3-dihydroxypropyl or 2,2-dimethyl dioxolan-4-yl methyl or hydroxycarbonylmethyl.The compounds are obtained by reacting 2-Ar-2-chloro-6-methyl pyrimidine, with ##SPC2##The compounds possess sedative, antiinflammatory, antiulcerous, vasodilatatory, antibronchoconstrictive, anticholinergic, diuretic, spasmolytic, cardiac analeptic, analgesic and myorelaxant properties.
摘要翻译：式WHEREIN Ar的化合物是苯基或被一个或多个卤素，三氟甲基或亚甲二氧基，一个或多个甲氧基，具有1至4个碳原子的烷基或二甲基氨基取代的苯基，并且R 1是R 1 -CN ANGLE，PARALLEL OR2或-O- R3（CH2）nN ANGLE，R4或OC ANGLE OR5，其中R1和R2各自为氢或1-4个碳原子的烷基，或R1-ANGLE R2为吡咯烷子基，吗啉代，哌啶子基或哌嗪基 N'被1至4个碳原子的烷基取代，或苯基; R3和R4各自为1至3个碳原子的烷基或R3-ANGLE R4为吗啉代，吡咯烷子基，哌啶子基或六亚甲基亚氨基，n为1至5的整数; R5为1-4个碳原子的烷基，2,3-二羟基丙基或2,2-二甲基二氧戊环-4-基甲基或羟基羰基甲基。

30. 发明授权

US4386090A Nitrogen containing 2,3-dihydro naphthalenes, compositions and use 失效
标题翻译：含2,3-二氢萘的氮，组成和用途
公开(公告)号：US4386090A
公开(公告)日：1983-05-31
申请号：US331484
申请日：1981-12-16
申请人： Gerard H. Moinet , Philippe L. Dostert , Guy R. Bourgery
发明人： Gerard H. Moinet , Philippe L. Dostert , Guy R. Bourgery
IPC分类号： C07D213/81 , C07D217/14 , C07D217/16 , C07D267/14 , C07D317/28 , C07D317/30 , C07D295/02 , A61K31/135 , A61K31/535 , C07D295/06
CPC分类号： C07D213/81 , C07D217/14 , C07D217/16 , C07D267/14 , C07D317/28 , C07D317/30
摘要： The present invention concerns heterocyclic aminoalcoyl derivatives having the formula: ##STR1## wherein n=1, 2 or 3; A represents a nitrogen atom or the CH group, X=CH.sub.2 or CH.sub.2 O; R represents a phenyl nucleus possibly substituted; NR.sub.1 R.sub.2 =amino, methylamino, N,N-dialkylamino or an heterocyclic radical; and R.sub.3 =H, halogen, alkyl, alkyloxy or methoxy.These derivatives are useful as drugs, especially as analgesics and antidepressants.
摘要翻译：本发明涉及具有下式的杂环氨基羰基衍生物：其中n = 1,2或3; A表示氮原子或CH基团，X = CH 2或CH 2 O; R代表可能被取代的苯基核; NR 1 R 2 =氨基，甲基氨基，N，N-二烷基氨基或杂环基; R3 = H，卤素，烷基，烷氧基或甲氧基。这些衍生物可用作药物，特别是作为镇痛药和抗抑郁药。

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