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1. 发明授权

US5473096A Substituted benzoate derivatives 失效
标题翻译：取代苯甲酸酯衍生物
公开(公告)号：US5473096A
公开(公告)日：1995-12-05
申请号：US93953
申请日：1993-07-21
申请人： Shigeru Matsutani , Tadashi Yoshida , Ryuji Sakazaki , Yasuhiko Fujii , Kazushige Tanaka
发明人： Shigeru Matsutani , Tadashi Yoshida , Ryuji Sakazaki , Yasuhiko Fujii , Kazushige Tanaka
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。

2. 发明授权

US5456910A Antibiotic stalobacins 失效
标题翻译：抗生素stalobacins
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
IPC分类号： A61K38/00 , C07K4/04 , C12P21/02 , A61K35/74 , C12P1/04
CPC分类号： C12R1/38 , C07K4/04 , C12P21/02 , A61K38/00
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。

3. 发明授权

US4476133A Triazolo-4,1-benzoxazepines having CNS activity 失效
标题翻译：具有中枢神经系统活性的三氮唑-4,1-苯并氧氮杂
公开(公告)号：US4476133A
公开(公告)日：1984-10-09
申请号：US397855
申请日：1982-07-13
申请人： Kentaro Hirai , Shigeru Matsutani , Itsuo Makino , Teruyuki Ishiba
发明人： Kentaro Hirai , Shigeru Matsutani , Itsuo Makino , Teruyuki Ishiba
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

4. 发明授权

US5597943A Phospholipase A.sub.2 inhibitor 失效
标题翻译：磷脂酶A2抑制剂
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。

5. 发明授权

US4840953A 9-(Substituted thio)-4H-pyrido[1,2,-A]pyrimidin-4-one derivatives 失效
标题翻译： 9-（取代的硫代）-4H-吡啶并[1,2-a]嘧啶-4-酮衍生物
公开(公告)号：US4840953A
公开(公告)日：1989-06-20
申请号：US206665
申请日：1988-06-15
申请人： Shigeru Matsutani , Yukio Mizushima , Masami Doteuchi , Yasunobu Ishihara
发明人： Shigeru Matsutani , Yukio Mizushima , Masami Doteuchi , Yasunobu Ishihara
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： 9-(Substituted thio)-4H-pyrido[1,2-a]pyrimidin-4-one derivatives of the formula: ##STR1## wherein n is 0 or 1, R is --COR.sup.1, --CONR.sup.4 R.sup.5 or --CH.sub.2 R.sup.6, R.sup.1 is C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl, allythio, styryl, phenoxymethyl, thienylmethyl, C.sub.6 -C.sub.10 aryl optionally substituted, benzyl optionally substituted or 5- or 6-membered heterocyclic group optionally substituted, R.sup.2 and R.sup.3 each is hydrogen, C.sub.1 -C.sub.5 alkyl, carboxy, C.sub.2 -C.sub.5 alkoxycarbonyl or benzyloxycarbonyl optionally substituted, R.sup.4 and R.sup.5 each is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl or phenyl optionally substituted, and R.sup.8 is pyridyl or phenyl optionally substituted) being useful as antiulcer agents are provided through several routes.
摘要翻译： 9-（取代的硫代）-4H-吡啶并[1,2-a]嘧啶-4-酮衍生物其中n为0或1，R为-COR 1，-CONR 4 R 5或-CH 2 R 6 R1是C1-C5烷基，C3-C7环烷基，烯硫基，苯乙烯基，苯氧基甲基，噻吩基甲基，任选取代的C 6 -C 10芳基，任选取代的苄基，或任选被取代的5或6元杂环基，R 2和R 3各自是氢， C 1 -C 5烷基，羧基，C 2 -C 5烷氧基羰基或任选取代的苄氧基羰基，R 4和R 5各自为氢，C 1 -C 5烷基，C 3 -C 7环烷基或任选取代的苯基，R 8为任选取代的吡啶基或苯基）可用作抗溃疡剂代理商通过几条路线提供。

6. 发明授权

US4341704A 4,1-Benzoxazepines and thia analogs thereof 失效
标题翻译： 4,1-苯并氧氮杂及其类似物
公开(公告)号：US4341704A
公开(公告)日：1982-07-27
申请号：US276632
申请日：1981-06-23
申请人： Kentaro Hirai , Shigeru Matsutani , Teruyuki Ishiba , Itsuo Makino
发明人： Kentaro Hirai , Shigeru Matsutani , Teruyuki Ishiba , Itsuo Makino
IPC分类号： A61K31/395 , A61K31/4196 , A61K31/55 , A61K31/553 , A61K31/554 , A61P21/02 , A61P25/00 , A61P25/02 , A61P25/08 , A61P25/20 , A61P25/22 , C07D249/08 , C07D249/10 , C07D267/14 , C07D273/00 , C07D281/10 , C07D285/36 , C07D498/04 , C07D513/04 , C07D521/00
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D249/10 , C07D267/14 , C07D273/00 , C07D285/36 , C07D513/04
摘要： 4,1-Benzoxazepines and thia analogs thereof of the formula: ##STR1## (wherein --A--B-- is the following group: ##STR2## (wherein R.sup.1 is hydrogen, C.sub.1 to C.sub.3 alkyl, or C.sub.7 to C.sub.9 aralkyl;R.sup.2 is C.sub.1 to C.sub.3 alkyl or C.sub.1 to C.sub.3 .alpha.-aminoalkyl;R.sup.3 is C.sub.2 to C.sub.6 dialkylamino;R.sup.4 is C.sub.2 to C.sub.6 dialkylamino or C.sub.5 to C.sub.7 alkylpiperazino;R.sup.5 is C.sub.1 to C.sub.3 alkyl; andQ is oxygen or sulfur);D is oxygen or sulfur;X is halogen or nitro;Y is hydrogen or halogen; andZ is hydrogen, C.sub.1 to C.sub.3 alkoxy, or C.sub.3 to C.sub.9 dialkylaminoalkoxy;with the proviso that when --A--B-- is ##STR3## Z is not hydrogen.) useful as novel central nervous system drugs are prepared by various synthetic routes.
摘要翻译：（其中-AB-是下列基团：其中R 1是氢，C 1至C 3烷基或C 7至C 9芳烷基） ; R2是C1-C3烷基或C1-C3α-氨基烷基; R3是C2-C6二烷基氨基; R4是C2-C6二烷基氨基或C5-C7烷基哌嗪基; R5是C1-C3烷基; Q是氧或硫）; D 是氧或硫; X是卤素或硝基; Y是氢或卤素; Z是氢，C 1至C 3烷氧基或C 3至C 9二烷基氨基烷氧基;条件是当-AB-不是氢时。）作为新型中枢神经系统药物通过各种合成途径制备。

7. 发明授权

US4318858A Thioethylamide derivatives 失效
标题翻译：硫代乙酰胺衍生物
公开(公告)号：US4318858A
公开(公告)日：1982-03-09
申请号：US212222
申请日：1980-12-02
申请人： Kentaro Hirai , Shigeru Matsutani , Teruyuki Ishiba , Itsuo Makino , Masami Doteuchi , Koichi Otani
发明人： Kentaro Hirai , Shigeru Matsutani , Teruyuki Ishiba , Itsuo Makino , Masami Doteuchi , Koichi Otani
IPC分类号： C07D333/16 , A61K31/34 , A61K31/341 , A61P43/00 , C07D307/52 , C07D307/68 , C07D333/20 , C07D333/38 , C07D405/12 , C07D409/12 , C07D207/04 , C07D333/18
CPC分类号： C07D307/68 , C07D307/52 , C07D333/20 , C07D333/38 , Y10S514/927
摘要： A compound of the formula: ##STR1## [wherein R is dimethylamino or 1-pyrrolidinyl;R.sup.1 and R.sup.2 each is hydrogen or C.sub.1 -C.sub.3 alkyl;R.sup.3 is hydrogen, C.sub.1 -C.sub.3 alkyl (optionally substituted by one member selected from the group consisting of cyano, C.sub.1 -C.sub.3 alkoxy, phenyl, and 5- or 6-membered heterocyclic group), C.sub.3 -C.sub.6 cycloalkyl, C.sub.2 -C.sub.5 alkenyl (optionally substituted by one member selected from the group consisting of C.sub.1 -C.sub.3 alkoxy, phenyl, and phenoxy), C.sub.6 -C.sub.10 aryl (optionally substituted by one or two members selected from the group consisting of hydroxy, halogen, nitro, sulfamoyl, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkanoyl, C.sub.2 -C.sub.4 alkoxycarbonyl, C.sub.2 -C.sub.4 dialkylamino, and C.sub.1 -C.sub.3 alkanesulfonyl), or 5- or 6-membered heterocyclic group (optionally substituted by one member selected from the group consisting of oxo, halogen, C.sub.1 -C.sub.3 alkyl, and C.sub.1 -C.sub.3 alkoxy);and X is oxygen or sulfur]and its pharmaceutically acceptable acid addition salts is useful as histamine H.sub.2 blockers.
摘要翻译：下式的化合物：其中R是二甲基氨基或1-吡咯烷基; R1和R2各自为氢或C1-C3烷基; R 3是氢，C 1 -C 3烷基（任选地被选自氰基，C 1 -C 3烷氧基，苯基和5-或6-元杂环基中的一个取代），C 3 -C 6环烷基，C 2 -C 5烯基（任选地被选自C 1 -C 3烷氧基，苯基和苯氧基的一个取代基取代），C 6 -C 10芳基（任选被一个或两个选自羟基，卤素，硝基，氨磺酰基，C1- C 3烷基，C 1 -C 3烷氧基，C 1 -C 3烷酰基，C 2 -C 4烷氧基羰基，C 2 -C 4二烷基氨基和C 1 -C 3烷磺酰基）或5或6元杂环基（任选被一个选自的氧代，卤素，C 1 -C 3烷基和C 1 -C 3烷氧基）; 并且X是氧或硫]，其药学上可接受的酸加成盐可用作组胺H2阻断剂。

8. 发明授权

US4309433A Pyridinecarbonamido-oxy or thio loweralkyl-1-(diloweralkylaminoloweralkyl)benzene and derivatives thereof, compositions containing same and method of using same 失效
标题翻译：吡啶羰基酰氧基或硫代低级烷基-1-（二低烷基氨基低级烷基）苯及其衍生物，含有它们的组合物及其使用方法
公开(公告)号：US4309433A
公开(公告)日：1982-01-05
申请号：US164016
申请日：1980-06-30
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 , C07D213/56 , C07D401/10
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.
摘要翻译：下式的氨基烷基苯衍生物：其中A是氧或硫; Y是氧代，硫代或氰基亚氨基; a为1〜3的整数， b为0〜3的整数; c为1〜4的整数， R1是烷基; R2是氢或烷基; 或者R 1和R 2一起代表吡咯烷基; R是氢，环烷基，三卤代烷基，烷氧基，二烷基氨基，芳基，芳酰基，杂环基或下式基团：其中R 3是氢，卤素，氨基，烷基，烷基氨基，二烷基氨基，烷硫基或芳氧基; R4是氢，烷基，烯基，芳基或杂环基;或R3和R4一起代表亚烷基或亚烷叉基;条件是上述芳基，芳酰基和杂环基可以被1至3个取代基取代] 作为组胺H2阻断剂，特别是消化性溃疡治疗剂可用的可接受的酸加成盐通过几种途径提供。

9. 发明授权

US06103231A Antibiotic stalobacins 失效
标题翻译：抗生素stalobacins
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
IPC分类号： A61K38/00 , C07K7/06 , A61K35/74 , C12P1/04
CPC分类号： C07K7/06 , A61K38/00
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。

10. 发明授权

US5011952A Phospholipase A2 inhibitor 失效
标题翻译：磷脂酶A2抑制剂
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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