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1. 发明公开

EP0184822A3 Novel anilide derivatives of substituted arylacetic acids 失效
标题翻译：取代的ARYLACETIC酸的新型酰胺衍生物
公开(公告)号：EP0184822A3
公开(公告)日：1987-12-09
申请号：EP85115720
申请日：1985-12-10
申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
发明人： Kawakami, Hajime , Hashimoto, Katsuhiro , Tamoto, Katsumi , Ono, Keiichi , Yamamoto, Michihiro
IPC分类号： C07C103/28 , C07C143/80 , C07C103/30 , C07D213/56 , A61K31/63 , A61K31/165 , A61K31/16 , C07D307/54 , C07D333/24 , A61K31/34
CPC分类号： C07D307/54 , C07D213/56 , C07D333/24
摘要： A compound of the formula I:
wherein Ar is a heterocyclic group or an aromatic hydrocarbon group optionally having one or two substituents selected from the group consisting of halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, nitro, cyano, di(C 1 -C 4 ) alkylamino, benzyloxy, hydroxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1- C 4 alkylsulfonyl and C 1 -C 4 alkanoylamino, X is a hydroxyl group or either one of the following groups:
(in which R 2 , R 3 , R 4 and R 5 are each independently hydrogen or C 1 -C 4 alkyl or, when R 2 and R 3 or R 4 and R 5 are taken together with the adjacent nitrogen atom to which they are attached, they represent pyrrolidino, piperidino, morpholino, N-(C 1 -C 4 )-alkylpiperazino or N-phenylpipera- zino), R is an aromatic hydrocarbon or heterocyclic group and n is an integer of 1 to 4, or its acid addition salt, which is useful as a cerebral metabolism stimulant or a nootropic agent.

2. 发明公开

EP0248399A1 Aminoazole derivatives and their production and use 失效
标题翻译：氨基唑衍生物，Herstellung und Anwendung。
公开(公告)号：EP0248399A1
公开(公告)日：1987-12-09
申请号：EP87107959.6
申请日：1987-06-02
申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
发明人： Ozato, Yukinori , Tamura, Nobuhiko , Masumori, Hiroaki , Yamamoto, Michihiro , Kojima, Atsuyuki , Nishikaku, Fumio , Kimura, Yoshihiko
IPC分类号： C07D277/38 , C07D261/14 , C07D263/48 , C07D271/06 , C07D413/06 , C07D413/10 , A61K31/41 , C07D417/06 , C07D417/10
CPC分类号： C07D271/07 , C07D261/14 , C07D263/48 , C07D277/40 , C07D277/42 , C07D277/46 , C07D277/48 , C07D413/06 , C07D413/10
摘要： A compound of the formula:
wherein A is the group of the formula:
wherein Ar 1 is a phenyl or thienyl group which may be optionally substituted with at least one of the same or different halogen atom; Ar 2 is a phenylene or thienylene group which may be optionally substituted with at least one of the same or different halogen atom; D is a divalent radical selected from the group consisting of
[wherein R 4 is a hydrogen atom or lower alkyl group],
radical, or single bond,
wherein R 5 is a lower alkoxy or a phenyl group which may be optionally substituted with at least one of the same or different halogen atom; E is a methine group or a nitrogen atom; F is a vinylene group or an oxygen atom,
wherein R 6 is a lower alkoxy group; R 7 is a lower alkyl group; R 8 is a benzoyl group which may be optionally substituted with at least one of the same or different halogen atom,

B is a divalent azole group;
R I is a hydrogen atom or a lower alkyl group;
R 2 is a hydrogen atom, lower alkyl, aryl-lower alkyl, or the group of the formula:
wherein R 9 is a hydrogen atom, lower alkyl, halo-lower alkyl, amino-lower alkyl, aryl or aryl-lower alkyl group or the group of the formula:
wherein R 10 is a hydrogen atom or lower alkyl group; R 11 is a hydrogen atom, lower alkyl, lower alkenyl, lower cycloalkyl, aryl-lower alkyl, aryl or aroyl group; or the group of the formula: -NR 10 R 11 is a 5-, 6-or 7- membered saturated heterocyclic ring; or the group of the formula:
wherein R 12 is a lower alkyl or polyhalo-lower alkyl group;
G is a divalent group selected from the group consisting of
radical; or the group of the formula: -NR 1 R 2 is a 5-, 6-or 7-membered saturated heterocyclic ring:
R 3 is a hydrogen atom or lower alkyl group, or its acid addition salts, which is useful for immunomodulator.
摘要翻译：下式的化合物：其中A是下列基团：Ar 1 -D-Ar 2 - ，其中Ar 1是苯基或噻吩基，其可任选被至少一个相同或不同的卤素原子取代; Ar 2是可以被至少一个相同或不同的卤素原子任选取代的亚苯基或亚噻吩基; D是选自 [其中R 4是氢原子或低级烷基]，基或单键的二价基团，其中R 5是低级烷氧基或可任选被至少一个相同或不同卤素原子取代的苯基; E是次甲基或氮原子; F是亚乙烯基或氧原子，CHEM，其中R 6是低级烷氧基; R 7是低级烷基; R 8是任选被相同或不同的卤素原子中的至少一个取代的苯甲酰基，B是二价的唑基; R 1是氢原子或低级烷基; R 2是氢原子，低级烷基，芳基 - 低级烷基或下式基团：R 9 -G-，其中R 9是氢原子，低级烷基，卤代低级烷基，氨基 - 低级烷基，芳基或芳基 - 低级烷基或下式基团：其中R 1为氢原子或低级烷基; R 1是氢原子，低级烷基，低级烯基，低级环烷基，芳基 - 低级烷基，芳基或芳酰基; 或者-NR 1 R 1 R 1基团是5-，6-或7-元饱和杂环; 或下式的基团：R 1 2 O - ，其中R 1 2是低级烷基或多卤代低级烷基; G是选自基团的二价基团; 或-NR 1 R 2的基团是5-，6-或7-元饱和杂环：R 3是氢原子或低级烷基，或其酸加成盐，这对免疫调节剂是有用的。

3. 发明授权

EP0177965B1 Novel oxa- and thiadiazolyl derivatives and their use 失效
标题翻译：新型OXA和THIADIAZOLYL衍生物及其用途
公开(公告)号：EP0177965B1
公开(公告)日：1990-03-21
申请号：EP85112872.8
申请日：1985-10-10
申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
发明人： Yamamoto, Michihiro , Ozato, Yukinori , Tamura, Nobuhiko , Miyagishi, Akira , Hara, Youichi
IPC分类号： C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , A61K31/41
CPC分类号： C07D271/06 , C07D271/10 , C07D285/08 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/14

4. 发明公开

EP0177965A3 Novel oxa- and thiadiazolyl derivatives and their use 失效
标题翻译：新型OXA和THIADIAZOLYL衍生物及其用途
公开(公告)号：EP0177965A3
公开(公告)日：1987-08-19
申请号：EP85112872
申请日：1985-10-10
申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
发明人： Yamamoto, Michihiro , Ozato, Yukinori , Tamura, Nobuhiko , Miyagishi, Akira , Hara, Youichi
IPC分类号： C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , A61K31/41 , C07D271/06 , C07D271/10 , C07D285/06
CPC分类号： C07D271/06 , C07D271/10 , C07D285/08 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/14
摘要： This disclosure describes novel oxadiazolyl-1,4-dihydropyridines and analogues thereof useful in treatment of cardiovascular disorders.

5. 发明公开

EP0177965A2 Novel oxa- and thiadiazolyl derivatives and their use 失效
标题翻译： Oxa和Thiadiazolylderivate und ihre Verwendung。
公开(公告)号：EP0177965A2
公开(公告)日：1986-04-16
申请号：EP85112872.8
申请日：1985-10-10
申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
发明人： Yamamoto, Michihiro , Ozato, Yukinori , Tamura, Nobuhiko , Miyagishi, Akira , Hara, Youichi
IPC分类号： C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , A61K31/41
CPC分类号： C07D271/06 , C07D271/10 , C07D285/08 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/14
摘要： This disclosure describes novel oxadiazolyl-1,4-dihydropyridines and analogues thereof useful in treatment of cardiovascular disorders.
摘要翻译：本公开描述了可用于治疗心血管疾病的新型恶二唑基-1,4-二氢吡啶及其类似物。

6. 发明公开

EP0184822A2 Novel anilide derivatives of substituted arylacetic acids 失效
标题翻译： Anilidderivate von substituteierterArylessigsäure。
公开(公告)号：EP0184822A2
公开(公告)日：1986-06-18
申请号：EP85115720.6
申请日：1985-12-10
申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
发明人： Kawakami, Hajime , Hashimoto, Katsuhiro , Tamoto, Katsumi , Ono, Keiichi , Yamamoto, Michihiro
IPC分类号： C07C103/28 , C07C143/80 , C07C103/30 , C07D213/56 , A61K31/63 , A61K31/165 , A61K31/16 , C07D307/54 , C07D333/24 , A61K31/34
CPC分类号： C07D307/54 , C07D213/56 , C07D333/24
摘要： A compound of the formula I:
wherein Ar is a heterocyclic group or an aromatic hydrocarbon group optionally having one or two substituents selected from the group consisting of halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, nitro, cyano, di(C 1 -C 4 ) alkylamino, benzyloxy, hydroxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1- C 4 alkylsulfonyl and C 1 -C 4 alkanoylamino, X is a hydroxyl group or either one of the following groups:
(in which R 2 , R 3 , R 4 and R 5 are each independently hydrogen or C 1 -C 4 alkyl or, when R 2 and R 3 or R 4 and R 5 are taken together with the adjacent nitrogen atom to which they are attached, they represent pyrrolidino, piperidino, morpholino, N-(C 1 -C 4 )-alkylpiperazino or N-phenylpipera- zino), R is an aromatic hydrocarbon or heterocyclic group and n is an integer of 1 to 4, or its acid addition salt, which is useful as a cerebral metabolism stimulant or a nootropic agent.
摘要翻译：式I的化合物：其中Ar是杂环基或任选具有一个或两个选自卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，硝基，氰基，二（C 1 -C 4）烷基氨基，苄氧基，羟基，C 1 -C 4烷硫基，C 1 -C 4烷基亚磺酰基，C 1 -C 4烷基磺酰基和C 1 -C 4烷酰氨基，X为羟基或下列基团之一： R 2，R 3，R 4和R 5各自独立地是氢或C 1 -C 4烷基，或者当R 2和R 3或R 4和R 5 它们与相邻的氮原子连在一起，它们代表吡咯烷子基，哌啶子基，吗啉代，N-（C 1 -C 4） - 烷基哌嗪基或N-苯基哌嗪基），R是芳族烃或杂环基，n是 1〜4的整数，或其酸加成盐，其可用作脑代谢兴奋剂或诱发剂。

7. 发明公开

EP0183177A1 Unsaturated fatty acid derivatives and their production 失效
标题翻译： UngesättigteFettsäurederivateund deren Herstellung。
公开(公告)号：EP0183177A1
公开(公告)日：1986-06-04
申请号：EP85114733.0
申请日：1985-11-19
申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
发明人： Nakamura, Toshio , Muraoka, Masami , Ono, Keiichi , Yamamoto, Michihiro
IPC分类号： C07C103/56 , C07C103/30 , A61K31/16 , C07D295/18 , A61K31/23 , A61K31/19 , C07C69/732 , C07C69/734 , C07C59/42 , C07C59/46
CPC分类号： C07D295/185 , C07C59/42 , C07C59/46 , C07D309/12
摘要： A compound of the formula:
wherein Y is a free or esterified carboxyl group, or a group of the formula:
(wherein R a and R b are each independently a hydrogen atom, a C 1 -C 4 alkyl group, a C 3 -C 7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C 1 -C 4 alkyl group, or, when taken together with the adjacent nitrogen atom, they represent a 5 to 7 membered saturated heterocyclic goup); R' is a C 1 -C 12 alkyl group, a C 2 -C 12 alkenyl group, a C 2 -C 12 alkynyl group, a C 3 -C 10 cycloalkyl group, a C 4 -C 10 cycloalkenyl group, a hydroxy C 1 -C 13 alkyl group, an C 1 -C 12 alkyl group substituted with a group of the formula:
(wherein R c and R d are each independently a hydrogen atom, or a C,-C 4 alkyl group), a C 3 -C 10 heterocyclic group, a phenyl group optionally substituted with one to three substituents selected from the group consisting of halogen atom, hydroxyl group, C 1 -C 4 alkyl group, trifluoromethyl group, C 1 -C 4 alkoxy group, and group of the formula:
(wherein R c and R d are as defined above) or a group of the formula:
[wherein A is a C 1 -C 7 alkylene chain and B is a C 3 -C 10 cycloalkyl group, a C 4 -C 10 cycloalkenyl group, a C 1 -C 12 alkoxy group, a C 1 -C 12 alkylthio group, a C 3 -C 10 cycloalkoxy group, a C 4 -C 10 cycloalkenyloxy group, a C 3 -C 10 heterocyclic group, or a phenyl or phenoxy group optionally substituted with one to three substituents selected from the group consisting of halogen atom, hydroxy group, C 1 -C 4 alkyl group, group of the formula:
(wherein R c and R d are as defined above), trifluoromethyl group, C 1 -C 4 alkylthio group and C,-C 4 alkoxy group]; n is 2, 3 or 4; R 2 and R 3 are hydrogen atoms or, when taken together, they mean a single linkage to form a trans double bond between the adjacent carbon atoms, and E is a cis or trans vinylene group; provided that when n is 3 and R' is a n-octyl group, a 2-octenyl group or a 2,5-octadienyl group, R 2 and R 3 are hydrogen atoms, and that when n is 2, E is a trans vinylene group or a non-toxic pharmaceutically acceptable salt thereof. Said compound have potent anti-leucotriene B 4 action, and are useful in the treatment of inflammation and allergy.
摘要翻译：下式的化合物：其中Y是游离或酯化的羧基，或下式的基团：其中R a和R b各自独立地为氢原子，C1- C4烷基，C3-C7环烷基，苄基，苯基，被卤素原子或C1-C4烷基取代的苯基，或者当与相邻的氮原子一起时，它们代表5 至7元饱和杂环苷）; R 1是C 1 -C 12烷基，C 2 -C 12烯基，C 2 -C 12炔基，C 3 -C 10环烷基，C 4 -C 10环烯基，羟基C 1 -C 13烷基，C 1 被下式基团取代的-C 12烷基：其中R c和R d各自独立地为氢原子或C 1 -C 4烷基，C 3 -C 10杂环基，任选被一至三个选自卤素原子，羟基，C 1 -C 4烷基，三氟甲基，C 1 -C 4烷氧基的取代基取代的苯基，和下式基团：其中R c >和R d如上定义）或下式的基团：AB [其中A是C 1 -C 7亚烷基链，B是C 3 -C 10环烷基，C 4 -C 10环烯基，C 1 -C 12 烷氧基，C1-C12烷硫基，C3-C10环烷氧基，C4-C10环烯基氧基，C3-C10杂环基或苯基或苯氧基，任选被一至三个选自由卤素原子，羟基，C 1 -C 4烷基组成的基团，其结构式为：CHEM（其中R c和R d如上所定义），三氟甲基，C 1 -C 4烷硫基和C 1 -C4烷氧基]; n为2,3或4; R 2和R 3是氢原子，或者当它们一起表示单键以在相邻碳原子之间形成反式双键时，E是顺式或反式亚乙烯基; 条件是当n为3且R 1为正辛基，2-辛烯基或2,5-辛二烯基时，R 2和R 3为氢原子，当n为 2，E是反式亚乙烯基或其无毒的药学上可接受的盐。所述化合物具有有效的抗白三烯B4作用，并且可用于治疗炎症和变态反应。

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