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公开(公告)号:US06103231A
公开(公告)日:2000-08-15
申请号:US890756
申请日:1997-12-09
申请人: Shigeru Matsutani , Tadashi Yoshida , Ryuji Sakazaki , Koichi Matsumoto , Shigeo Yagi , Bunji Kageyama , Yoshimi Kawamura , Toshiyuki Kamigauchi , Susumu Kamata
发明人: Shigeru Matsutani , Tadashi Yoshida , Ryuji Sakazaki , Koichi Matsumoto , Shigeo Yagi , Bunji Kageyama , Yoshimi Kawamura , Toshiyuki Kamigauchi , Susumu Kamata
摘要: Novel antibiotic stalobacins H-1 and I-1 having physico-chemical properties as shown in Table 4 are provided, which are excellent antibiotics showing marked effects on Gram-positive bacteria.
摘要翻译: 提供了具有如表4所示的具有物理化学性质的新型抗生素stalobacins H-1和I-1,其是对革兰氏阳性菌显示出显着作用的优异的抗生素。
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公开(公告)号:US5456910A
公开(公告)日:1995-10-10
申请号:US243780
申请日:1994-05-17
申请人: Shigeru Matsutani , Tadashi Yoshida , Ryuji Sakazaki , Koichi Matsumoto , Shigeo Yagi , Bunji Kageyama , Yoshimi Kawamura , Toshiyuki Kamigauchi , Susumu Kamata
发明人: Shigeru Matsutani , Tadashi Yoshida , Ryuji Sakazaki , Koichi Matsumoto , Shigeo Yagi , Bunji Kageyama , Yoshimi Kawamura , Toshiyuki Kamigauchi , Susumu Kamata
摘要: Novel antibiotic stalobacins A to I having physico-chemical properties as shown in Tables 1 to 4 are provided, which are excellent antibiotics showing marked effects on Gram-positive bacteria.
摘要翻译: 提供了具有如表1至4所示的具有物理化学性质的新型抗生素stalobacins A至I,其是对革兰氏阳性细菌具有显着影响的优异的抗生素。
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公开(公告)号:US5473096A
公开(公告)日:1995-12-05
申请号:US93953
申请日:1993-07-21
IPC分类号: A61K31/235 , A61K31/24 , A61P29/00 , A61P43/00 , C07C69/86 , C07C69/92 , C07C69/94 , C07C219/22 , C07C229/38 , C07C237/06 , C07C271/22 , C07C229/36
CPC分类号: C07C271/22 , C07C229/38 , C07C69/92
摘要: The present invention relates to the compounds of the formula: ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are independently hydrogen, lower alkyl which is optionally substituted, lower alkoxy which is optionally substituted, hydroxy, acyloxy, or halogen; R.sup.9 is hydrogen, hydroxy, acyloxy, lower alkyl which is optionally substituted, lower alkoxy which is optionally substituted, or lower alkylamino which is optionally substituted; E.sup.1 is hydrogen, or an ester residue; m is an integer of from 1 to 4;or a pharmaceutically acceptable salt thereof. The compounds of the present invention exhibit phospholipase A.sub.2 inhibitory activity, and can be used in treating inflammatory conditions.
摘要翻译: 本发明涉及下式的化合物:其中R 1,R 2,R 3,R 4,R 5,R 6,R 7和R 8独立地为氢,任选取代的低级烷基,任选取代的低级烷氧基, 羟基,酰氧基或卤素; R9是氢,羟基,酰氧基,任选被取代的低级烷基,任选被取代的低级烷氧基或任选被取代的低级烷基氨基; E1是氢或酯残基; m为1〜4的整数, 或其药学上可接受的盐。 本发明化合物表现出磷脂酶A2抑制活性,可用于治疗炎性病症。
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公开(公告)号:US5011952A
公开(公告)日:1991-04-30
申请号:US516982
申请日:1990-04-30
申请人: Tadashi Yoshida , Keizo Inoue , Hitoshi Arita , Shigeru Matsutani , Jun'ichi Shoji , Yoshimi Kawamura
发明人: Tadashi Yoshida , Keizo Inoue , Hitoshi Arita , Shigeru Matsutani , Jun'ichi Shoji , Yoshimi Kawamura
IPC分类号: C12P1/02 , A61K38/55 , A61P3/00 , A61P7/00 , A61P9/02 , A61P25/08 , C07D311/82 , C07K14/005 , C07K14/195 , C07K14/37 , C07K14/41 , C12N9/99 , C12P17/06 , C12R1/645
CPC分类号: C12R1/645 , C07D311/82 , C12P17/06
摘要: A compound of the formula: ##STR1## wherein the wave line means .alpha.-bond or .beta.-bond, which compound is useful as a phospholipase A.sub.2 inhibitor. Process for the production of the compound, pharmaceutical composition containing the compound, and a cell culture of a microorganism Thielavia terricola RF-143 producing the compound are also provided.
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公开(公告)号:US5597943A
公开(公告)日:1997-01-28
申请号:US571698
申请日:1995-12-13
申请人: Mitsuaki Ohtani , Shigeru Matsutani , Tadashi Yoshida , Kazushige Tanaka , Yasuhiko Fujii , Kazuhiro Shirahase
发明人: Mitsuaki Ohtani , Shigeru Matsutani , Tadashi Yoshida , Kazushige Tanaka , Yasuhiko Fujii , Kazuhiro Shirahase
IPC分类号: C07C69/773 , C07C69/90 , C07C69/92 , C07C229/36 , C07C271/22 , C07C317/44 , C07C323/62 , C07D309/38 , C07D493/10 , C07C69/76
CPC分类号: C07D493/10 , C07C229/36 , C07C271/22 , C07C317/44 , C07C323/62 , C07C69/90 , C07C69/92 , C07D309/38
摘要: The present invention relates to the new thielocin derivatives, which exhibit phospholipase A.sub.2 inhibitory activity of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are independently hydrogen, lower alkyl, lower alkoxy, hydroxy, or halogen;E.sub.1 and E.sub.2 are independently hydrogen, or an ester residue;m and n are independently an integer of 0 to 4;--Y-- is a bivalent group which is selected from the group consisiting of the following radicals: ##STR2## or the salts thereof.
摘要翻译: 本发明涉及新的thielocin衍生物,其表现出下式的磷脂酶A2抑制活性:其中R 1,R 2,R 3,R 4,R 5,R 6,R 7和R 8独立地为氢,低级烷基,低级烷氧基, 羟基或卤素; E1和E2独立地是氢或酯残基; m和n分别为0〜4的整数。 -Y-是选自以下基团的二价基团:CH 2 CH 2,CHCH,其中图像。
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公开(公告)号:US4476133A
公开(公告)日:1984-10-09
申请号:US397855
申请日:1982-07-13
IPC分类号: C07D267/14 , C07D498/04 , A61K31/55
CPC分类号: C07D267/14
摘要: 4,1-Benzoxazepines of the following formula are novel central nervous system: ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.5 alkyl;X is hydrogen, halogen, or nitro;Y is phenyl, 2-halophenyl, 4-halophenyl, 2-trifluoromethylphenyl, or pyridyl; and ##STR2## is a group of the formula: ##STR3## (wherein Q is oxygen, sulfur, or hydrazono, with a proviso that, when Y is phenyl or 2-halophenyl and R is hydrogen, Q is neither oxygen nor sulfur;R.sup.1 is hydrogen, halogen, C.sub.1 to C.sub.5 alkyl, C.sub.1 to C.sub.5 alkylthio, 5- or 6-membered heterocycle or C.sub.1 to C.sub.5 alkyl substituted by a substituent selected from the group consisting of halogen, hydroxy, mercapto, C.sub.1 to C.sub.5 alkoxy, C.sub.1 to C.sub.5 alkanoyloxy, C.sub.1 to C.sub.5 alkylthio, C.sub.7 to C.sub.9 aralkyldithio, C.sub.2 to C.sub.10 dialkylamino, C.sub.3 to C.sub.15 dialkylaminoalkoxy, C.sub.3 to C.sub.15 dialkylaminoalkylthio, and 5- or 6-membered heterocycle;R.sup.2 is C.sub.1 to C.sub.5 alkyl;and R.sup.3 is C.sub.1 to C.sub.5 alkyl or C.sub.3 to C.sub.10 dialkylaminoalkyl;with a proviso that when R.sup.1 is C.sub.1 to C.sub.5 alkyl and R is hydrogen, Y is neither phenyl nor 2-halophenyl)
摘要翻译: 下式的4,1-苯并氧氮杂是新的中枢神经系统:其中R是氢或C1至C5烷基; X是氢,卤素或硝基; Y是苯基,2-卤代苯基,4-卤代苯基,2-三氟甲基苯基或吡啶基; 并且
是下列基团:其中Q是氧,硫或亚肼基,条件是当Y是苯基或2-卤代苯基且R是氢时,Q是 氧还不硫; R1是氢,卤素,C1至C5烷基,C1至C5烷硫基,5-或6-元杂环或被选自卤素,羟基,巯基,C1的取代基取代的C1至C5烷基 C 1-5烷酰氧基,C 1至C 5烷硫基,C 7至C 9芳烷基二硫代,C 2至C 10二烷基氨基,C 3至C 15二烷基氨基烷氧基,C 3至C 15二烷基氨基烷硫基以及5-或6-元杂环; R 2为C 1至C 5烷基; 且R 3为C 1至C 5烷基或C 3至C 10二烷基氨基烷基;条件是当R 1为C 1至C 5烷基且R为氢时,Y -
公开(公告)号:US4564623A
公开(公告)日:1986-01-14
申请号:US573685
申请日:1984-01-25
申请人: Kentaro Hirai , Teruyuki Ishiba , Shigeru Matsutani , Itsuo Makino , Toshio Fujishita , Masami Doteuchi , Koichi Otani
发明人: Kentaro Hirai , Teruyuki Ishiba , Shigeru Matsutani , Itsuo Makino , Toshio Fujishita , Masami Doteuchi , Koichi Otani
IPC分类号: C07D295/18 , A61K31/16 , A61K31/165 , A61K31/34 , A61K31/341 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/4245 , A61K31/435 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/445 , A61K31/455 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P43/00 , C07C67/00 , C07C231/00 , C07C233/18 , C07C233/20 , C07C233/22 , C07C233/60 , C07C233/69 , C07C235/20 , C07C235/48 , C07C235/72 , C07C237/08 , C07C237/32 , C07C237/42 , C07C239/00 , C07C261/04 , C07C301/00 , C07C311/18 , C07C313/00 , C07C323/29 , C07C323/39 , C07C323/41 , C07C325/00 , C07C327/40 , C07C327/46 , C07C327/48 , C07C327/50 , C07D207/16 , C07D207/28 , C07D211/60 , C07D213/81 , C07D213/82 , C07D233/90 , C07D249/10 , C07D257/04 , C07D261/18 , C07D271/06 , C07D295/08 , C07D295/096 , C07D295/14 , C07D295/15 , C07D307/68 , C07D333/38 , C07D335/06 , C07D498/04 , C07D207/04
CPC分类号: C07D213/81 , C07C323/29 , C07D207/16 , C07D207/28 , C07D213/82 , C07D257/04 , C07D261/18 , C07D271/06 , C07D295/096 , C07D295/15 , C07D333/38 , C07D335/06 , Y10S514/927
摘要: An aminoalkylbenzene derivative of the formula: ##STR1## [wherein A is oxygen or sulfur;Y is oxo, thioxo, or cyanoimino;a is an integer of 1 to 3;b is an integer of 0 to 3;c is an integer of 1 to 4;R.sup.1 is alkyl;R.sup.2 is hydrogen or alkyl; orR.sup.1 and R.sup.2 taken together represent pyrrolidinyl;R is hydrogen, cycloaklkyl, trihaloalkyl, alkoxy, dialkylamino, aryl, aroyl, heterocyclic group, or a group of the formula: ##STR2## (wherein R.sup.3 is hydrogen, halogen, amino, alkyl, alkylamino, dialkylamino, alkylthio, or aryloxy;R.sup.4 is hydrogen, alkyl, alkenyl, aryl, or heterocyclic group; orR.sup.3 and R.sup.4 taken together represent alkylidene or aralkylidene);with the proviso that the above aryl, aroyl, and heterocyclic group can be substituted by 1 to 3 substituents] and its pharmaceutically acceptable acid addition salts being useful as histamine H.sub.2 blockers, especially peptic ulcer remedies, are provided via several routes.
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公开(公告)号:US4927829A
公开(公告)日:1990-05-22
申请号:US306752
申请日:1989-02-06
申请人: Shigeru Matsutani , Yukio Mizushima
发明人: Shigeru Matsutani , Yukio Mizushima
IPC分类号: A61K31/435 , A61K31/505 , A61P1/04 , C07D455/02 , C07D471/04 , C07D487/04
CPC分类号: C07D471/04 , C07D455/02 , C07D487/04
摘要: Novel heterocyclic compounds of the formula: ##STR1## or pharmaceutically acceptable acid addition salts thereof having a more potent and longer lasting cytoprotective anti-ulcer action than known analogues, useful in the treatment or prophylaxis of gastric ulcer at an oral dose of 10-500 mg, preferably 20 mg-100 mg per day to an adult, are provided through several routes.
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公开(公告)号:US4482566A
公开(公告)日:1984-11-13
申请号:US277161
申请日:1981-06-25
申请人: Kentaro Hirai , Teruyuki Ishiba , Shigeru Matsutani , Itsuo Makino , Toshio Fujishita , Masami Doeteuchi , Koichi Otani
发明人: Kentaro Hirai , Teruyuki Ishiba , Shigeru Matsutani , Itsuo Makino , Toshio Fujishita , Masami Doeteuchi , Koichi Otani
IPC分类号: C07D295/18 , A61K31/16 , A61K31/165 , A61K31/34 , A61K31/341 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/4245 , A61K31/435 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/445 , A61K31/455 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P43/00 , C07C67/00 , C07C231/00 , C07C233/18 , C07C233/20 , C07C233/22 , C07C233/60 , C07C233/69 , C07C235/20 , C07C235/48 , C07C235/72 , C07C237/08 , C07C237/32 , C07C237/42 , C07C239/00 , C07C261/04 , C07C301/00 , C07C311/18 , C07C313/00 , C07C323/29 , C07C323/39 , C07C323/41 , C07C325/00 , C07C327/40 , C07C327/46 , C07C327/48 , C07C327/50 , C07D207/16 , C07D207/28 , C07D211/60 , C07D213/81 , C07D213/82 , C07D233/90 , C07D249/10 , C07D257/04 , C07D261/18 , C07D271/06 , C07D295/08 , C07D295/096 , C07D295/14 , C07D295/15 , C07D307/68 , C07D333/38 , C07D335/06 , C07D498/04 , C07D207/04 , A61K31/135 , C07C103/34 , C07C103/37
CPC分类号: C07D213/81 , C07C323/29 , C07D207/16 , C07D207/28 , C07D213/82 , C07D257/04 , C07D261/18 , C07D271/06 , C07D295/096 , C07D295/15 , C07D333/38 , C07D335/06 , Y10S514/927
摘要: An aminoalkylbenzene derivative of the formula: ##STR1## [wherein A is oxygen or sulfur;Y is oxo, thioxo, or cyanoimino;a is an integer of 1 to 3;b is an integer of 0 to 3;c is an integer of 1 to 4;R.sup.1 is alkyl;R.sup.2 is hydrogen or alkyl; orR.sup.1 and R.sup.2 taken together represent pyrrolidinyl;R is hydrogen, cycloalkyl, trihaloalkyl, alkoxy, dialkylamino, aryl, aroyl, heterocyclic group, or a group of the formula: ##STR2## (wherein R.sup.3 is hydrogen, halogen, amino, alkyl, alkylamino, dialkylamino, alkylthio, or aryloxy;R.sup.4 is hydrogen, alkyl, alkenyl, aryl, or heterocyclic group; orR.sup.3 and R.sup.4 taken together represent alkylidene or aralkylidene);with the proviso that the above aryl, aroyl, and heterocyclic group can be substituted by 1 to 3 substituents] and its pharmaceutically acceptable acid addition salts being useful as histamine H.sub.2 blockers, especially peptic ulcer remedies, are provided via several routes.
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公开(公告)号:US4374842A
公开(公告)日:1983-02-22
申请号:US250299
申请日:1981-04-02
IPC分类号: C07D267/14 , C07D498/04 , A61K31/55 , C07D498/14
CPC分类号: C07D267/14
摘要: 4,1-Benzoxazepines of the following formula are central nervous system drugs: ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.5 alkyl; X is hydrogen, halogen, or nitro; Y is phenyl, 2-halophenyl, 4-halophenyl, 2-trifluoromethylphenyl, or pyridyl; and ##STR2## is a group of the formula: ##STR3## (wherein Q is oxygen, sulfur, or hydrazono, with a proviso that, when Y is phenyl or 2-halophenyl and R is hydrogen, Q is neither oxygen nor sulfur;R.sup.1 is hydrogen, halogen, C.sub.1 to C.sub.5 alkyl, C.sub.1 to C.sub.5 alkylthio, 5- or 6-membered heterocycle or C.sub.1 to C.sub.5 alkyl substituted by a substituent selected from the group consisting of halogen, hydroxy, mercapto, C.sub.1 to C.sub.5 alkoxy, C.sub.1 to C.sub.5 alkanoyloxy, C.sub.1 to C.sub.5 alkylthio, C.sub.7 to C.sub.9 aralkyldithio, C.sub.2 to C.sub.10 dialkylamino, C.sub.3 to C.sub.15 dialkylaminoalkoxy, C.sub.3 to C.sub.15 dialkylaminoalkylthio, and 5- or 6-membered heterocycle;R.sup.2 is C.sub.1 to C.sub.5 alkyl;and R.sup.3 is C.sub.1 to C.sub.5 alkyl or C.sub.3 to C.sub.10 dialkylaminoalkyl;with a proviso that when R.sup.1 is C.sub.1 to C.sub.5 alkyl and R is hydrogen, Y is neither phenyl nor 2-halophenyl).
摘要翻译: 下式的4,1-苯并氧氮杂是中枢神经系统药物:其中R是氢或C1至C5烷基; X是氢,卤素或硝基; Y是苯基,2-卤代苯基,4-卤代苯基,2-三氟甲基苯基或吡啶基; 并且
是下列基团:其中Q是氧,硫或亚肼基,条件是当Y是苯基或2-卤代苯基且R是氢时,Q是 氧还不硫; R1是氢,卤素,C1至C5烷基,C1至C5烷硫基,5-或6-元杂环或被选自卤素,羟基,巯基,C1的取代基取代的C1至C5烷基 C 1-5烷酰氧基,C 1至C 5烷硫基,C 7至C 9芳烷基二硫代,C 2至C 10二烷基氨基,C 3至C 15二烷基氨基烷氧基,C 3至C 15二烷基氨基烷硫基以及5-或6-元杂环; R 2为C 1至C 5烷基; 并且R 3为C 1至C 5烷基或C 3至C 10二烷基氨基烷基;条件是当R 1为C 1至C 5烷基且R为氢时,Y不为苯基或2-卤代苯基)。
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