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81. 发明授权

US4734419A Quinazoline derivatives, compositions thereof and their use in treating diabetic complications 失效
标题翻译：喹唑啉衍生物，其组合物及其在治疗糖尿病并发症中的用途
公开(公告)号：US4734419A
公开(公告)日：1988-03-29
申请号：US908005
申请日：1986-09-16
申请人： Masashi Hashimoto , Teruo Oku , Yoshikuni Ito , Takayuki Namiki , Kozo Sawada , Chiyoshi Kasahara , Yukihisa Baba
发明人： Masashi Hashimoto , Teruo Oku , Yoshikuni Ito , Takayuki Namiki , Kozo Sawada , Chiyoshi Kasahara , Yukihisa Baba
IPC分类号： C12N9/99 , A61K31/505 , A61K31/517 , A61K31/54 , A61K31/5415 , A61P1/16 , A61P3/08 , A61P3/10 , A61P13/02 , A61P15/00 , A61P25/00 , A61P27/02 , A61P27/12 , A61P43/00 , C07D239/80 , C07D239/91 , C07D239/93 , C07D239/95 , C07D239/96 , C07D265/26 , C07D285/24 , C07D401/06 , C07D409/06 , C07D521/00
CPC分类号： C07D401/06 , C07D239/95 , C07D239/96 , C07D285/24 , C07D409/06
摘要： The invention relates to compounds of the formula: ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, halogen, lower alkoxy or halo(lower)alkyl,R.sup.3 is dihalophenyl, naphthyl(lower)alkyl, phenyl(lower)alkyl substituted by one or two substituent(s) selected from the group consisting of halogen, lower alkoxy, halo(lower)alkyl and lower alkyl, or thienyl(lower)alkyl,R.sup.4 is carboxy or protected carboxy,Y is carbonyl, thiocarbonyl or sulfonyl andZ is lower alkylene, and pharmaceutically acceptable salts thereof, useful in the treatment of diabetic complications.
摘要翻译：本发明涉及下式的化合物：其中R 1和R 2各自为氢，卤素，低级烷氧基或卤代（低级）烷基，R 3为二卤代苯基，萘基（低级）烷基，苯基（低级）烷基）或低级烷基，或噻吩基（低级）烷基，R4为羧基或被保护的羧基，Y为羰基，硫代羰基或磺酰基，Z为低级亚烷基及其药学上可接受的盐，可用于治疗糖尿病并发症。

82. 发明授权

US4698349A Quinolizinone compounds, and pharmaceutical composition comprising the same, useful as anti-ulcerative and anti-allergic agents 失效
标题翻译：喹诺酮酮化合物和包含其的药物组合物，其可用作抗溃疡和抗过敏剂
公开(公告)号：US4698349A
公开(公告)日：1987-10-06
申请号：US770953
申请日：1985-08-30
申请人： Yoshihiko Kitaura , Teruo Oku , Hideo Hirai , Tosiyuki Yamamoto , Masashi Hashimoto
发明人： Yoshihiko Kitaura , Teruo Oku , Hideo Hirai , Tosiyuki Yamamoto , Masashi Hashimoto
IPC分类号： A61K31/435 , A61K31/47 , A61P1/04 , A61P37/08 , A61P43/00 , C07D455/00 , C07D455/02 , C07D455/03 , C07D455/04 , C07D455/06 , C07F7/18 , A61K31/345
CPC分类号： C07D455/00 , C07D455/02 , C07D455/04 , C07D455/06 , C07F7/1856 , Y02P20/55
摘要： The invention relates to novel quinolizinone compounds, of inhibitory activity on allergies and ulcers, of the formula: ##STR1## wherein R.sup.1 is carboxy, carbamoyl Y.sup.1, phenylcarbamoyl which may have hydroxy, cyano or thiocarbamoyl,R.sup.7 is hydrogen or aryl selected from phenyl, tolyl, xylyl, cumenyl, naphthyl and biphenylyl;R.sup.2 is hydrogen, hydroxy, lower alkyl or lower alkoxy; andR.sup.3 is hydrogen, hydroxy, lower alkyl, lower alkoxy, lower alkenyloxy, phenyl, naphthyl, biphenylyl, phenyl having one or more substituent(s) selected from halogen, lower alkyl and lower alkoxy, arylthio selected from phenylthio, tolylthio, xylylthio, cumenylthio, naphthylthio and biphenylylthio, aroyl selected from benzoyl, toluoyl and naphthoyl, ar(lower)alkyl selected from phenyl(lower)alkyl, tolyl(lower)alkyl, xylyl(lower)alkyl, cumenyl(lower)alkyl, naphthyl(lower)alkyl and biphenylyl(lower)alkyl, arenesulfonyl selected from benzenesulfonyl and p-toluenesulfonyl, arylamino selected from phenylamino, naphthylamino, biphenylylamino, phenylamino having lower alkyl on the nitrogen atom or aryloxy selected from phenoxy and tolyloxy; or pharmaceutically acceptable salts thereof.

83. 发明授权

US4585762A Phospholipid derivatives, processes for use thereof and pharmaceutical composition of the same 失效
标题翻译：磷脂衍生物，其使用方法及其药物组合物
公开(公告)号：US4585762A
公开(公告)日：1986-04-29
申请号：US513451
申请日：1983-07-13
申请人： Tsutomu Teraji , Eishiro Todo , Norihiko Shimazaki , Teruo Oku , Takayuki Namiki
发明人： Tsutomu Teraji , Eishiro Todo , Norihiko Shimazaki , Teruo Oku , Takayuki Namiki
IPC分类号： A01N57/12 , A61K31/66 , A61P35/00 , C07D309/12 , C07F9/09 , C07F9/10 , C07F9/117 , C07H9/04 , C07H11/04 , C07H13/04 , C07H13/08
CPC分类号： C07H9/04 , C07C309/00 , C07D309/12 , C07F9/091 , C07F9/10 , C07F9/117 , C07H11/04 , C07H13/04 , C07H13/08
摘要： New phospholipid derivatives represented by the formula: ##STR1## wherein R.sup.1 is alkyl, alkoxy, alkylthio or alkylsulfonyl;R.sup.2 is hydrogen, hydroxy, alkoxy, lower alkanoyloxy or lower alkylcarbamoyloxy;n is 0 or 1;R.sup.3 is hydroxy or protected hydroxy; andR.sup.4 is lower alkoxy or lower alicyclic-oxy group which is substituted with 2 or more hydroxy or protected hydroxy groups, and may be substituted with lower alkoxy or another alicyclic-oxy group having two or more hydroxy or protected hydroxy groups, in which the alicyclic ring may contain an oxygen atom;and pharmaceutically acceptable salt thereof, which exhibit antitumor activity.
摘要翻译：由下式表示的新型磷脂衍生物：其中R 1是烷基，烷氧基，烷硫基或烷基磺酰基; R2是氢，羟基，烷氧基，低级烷酰氧基或低级烷基氨基甲酰氧基; n为0或1; R3是羟基或被保护的羟基; R4为被2个以上羟基或被保护的羟基取代的低级烷氧基或低级脂环氧基，可以被低级烷氧基或具有两个以上羟基或保护羟基的另一个脂环氧基取代，其中脂环可以含有氧原子; 和其药学上可接受的盐，其具有抗肿瘤活性。

84. 发明授权

US4472300A Azetidinone derivatives and process for preparation thereof 失效
标题翻译：氮杂环丁酮衍生物及其制备方法
公开(公告)号：US4472300A
公开(公告)日：1984-09-18
申请号：US130205
申请日：1980-03-13
申请人： Takashi Kamiya , Yoshihisa Saito , Masashi Hashimoto , Osamu Nakaguti , Teruo Oku , Youichi Shiokawa , Takao Takaya , Tadaaki Komori , Tsutomu Teraji , Keiji Hemmi , Hisashi Takasugi
发明人： Takashi Kamiya , Yoshihisa Saito , Masashi Hashimoto , Osamu Nakaguti , Teruo Oku , Youichi Shiokawa , Takao Takaya , Tadaaki Komori , Tsutomu Teraji , Keiji Hemmi , Hisashi Takasugi
IPC分类号： C07D205/085 , C07D473/00 , C07D205/08 , C07D401/12 , C07D403/12 , C07D409/12
CPC分类号： C07D473/00 , C07D205/085
摘要： New antimicrobial azetidinone derivatives and their salt of the formula: ##STR1## wherein R.sub.1 amino or acylamino, and A is selected from a variety of groups.
摘要翻译：新的抗微生物氮杂环丁酮衍生物及其下式的盐：其中R 1氨基或酰氨基，A选自多种基团。

85. 发明授权

US4397849A Benzothiazine derivatives 失效
标题翻译：苯并噻嗪衍生物
公开(公告)号：US4397849A
公开(公告)日：1983-08-09
申请号：US329862
申请日：1981-12-11
申请人： Tsutomu Teraji , Teruo Oku , Youichi Shiokawa
发明人： Tsutomu Teraji , Teruo Oku , Youichi Shiokawa
IPC分类号： A61K31/54 , A61K31/5415 , A61P37/06 , C07D279/16 , C07D417/12
CPC分类号： C07D279/16
摘要： This invention relates to novel benzothiazine derivatives having therapeutic effect on autoimmune diseases, to processes for preparation of such derivatives, and to pharmaceutical compositions containing such derivatives, the derivatives having the formula: ##STR1## wherein R.sup.1 is lower alkyl which may have one or more substituents selected from carboxy, aryl and carboxy(lower)cycloalkyl; aryl which may have one or more substituents selected from halogen, lower alkyl, halo(lower)alkyl and lower alkoxy; haloarylamino; or heterocyclic group;R.sup.2 is hydrogen, lower alkyl, lower alkylamino(lower)alkyl, aryl or ar(lower)alkyl;R.sup.3 is hydrogen, halogen, lower alkyl or lower alkoxy; andn is an integer 0 to 2.
摘要翻译：本发明涉及对自身免疫性疾病具有治疗作用的新的苯并噻嗪衍生物，该衍生物的制备方法，以及含有该衍生物的药物组合物，具有下式的衍生物：其中R 1为低级烷基，可以具有一个或多个取代基选自羧基，芳基和羧基（低级）环烷基; 可以具有一个或多个选自卤素，低级烷基，卤代（低级）烷基和低级烷氧基的取代基的芳基; 卤代芳基氨基; 或杂环基; R2是氢，低级烷基，低级烷基氨基（低级）烷基，芳基或芳（低级）烷基; R3是氢，卤素，低级烷基或低级烷氧基; n为0〜2的整数。

86. 发明授权

US4304718A 2-Azetidinone compounds and processes for preparation thereof 失效
标题翻译： 2-氮杂环丁酮化合物及其制备方法
公开(公告)号：US4304718A
公开(公告)日：1981-12-08
申请号：US71280
申请日：1979-08-30
申请人： Takashi Kamiya , Masashi Hashimoto , Osamu Nakaguti , Teruo Oku , Yoshiharu Nakai , Hidekazu Takeno
发明人： Takashi Kamiya , Masashi Hashimoto , Osamu Nakaguti , Teruo Oku , Yoshiharu Nakai , Hidekazu Takeno
IPC分类号： C07C323/25 , C07D205/08 , C07D205/085 , C07D205/095 , C07D251/04 , A61K31/42 , C07D403/04 , C07D409/06
CPC分类号： C07C323/25 , C07D205/08 , C07D205/085 , C07D205/095 , C07D251/04
摘要： This invention relates to new 2-azetidinone compounds, which have antimicrobial activities, and to processes for the preparation thereof, and more particularly, this invention provides new 2-azetidinone compounds, especially ones having various substituted carboxyalkyl radicals at the first position and having various groups at the fourth position of the azetidinone nucleus, which have antimicrobial activities against various pathogenic microorganisms and are useful as antibiotics in treatment for microbial infections in mammal including human being and animals.
摘要翻译：本发明涉及具有抗菌活性的新的2-氮杂环丁酮化合物及其制备方法，更具体地说，本发明提供新的2-氮杂环丁酮化合物，特别是在第一位置具有各种取代的羧基烷基的化合物，在氮杂环丁酮核的第四位置的组，其具有针对各种致病微生物的抗微生物活性，并且可用作治疗哺乳动物包括人和动物的微生物感染的抗生素。

87. 发明授权

US4267340A Disulfide substituted oxazetidine derivatives 失效
标题翻译：二硫化物取代的氧氮杂环丁烷衍生物
公开(公告)号：US4267340A
公开(公告)日：1981-05-12
申请号：US852053
申请日：1977-11-16
申请人： Takashi Kamiya , Yoshihisa Saito , Tsutomu Teraji , Osamu Nakaguti , Teruo Oku , Hitoshi Nakamura , Masashi Hashimoto
发明人： Takashi Kamiya , Yoshihisa Saito , Tsutomu Teraji , Osamu Nakaguti , Teruo Oku , Hitoshi Nakamura , Masashi Hashimoto
IPC分类号： C07D205/095 , C07D499/00 , C07D501/10 , C07D277/20 , C07D263/30
CPC分类号： C07D499/00 , C07D205/095
摘要： An oxoazetidine derivative compound of the formula: ##STR1## wherein R.sub.1 represents a substituted or unsubstituted amino radical and R.sub.3 represents a radical selected from the group consisting of carboxy, protected carboxy, ester, acid amide, acid anhydride, acid halide, acid azide and carboxy salt, and --SR.sub.2 is a residue of a thiophilic sulphur nucleophile.
摘要翻译：下式的氧代氮杂环丁啶衍生物化合物，其中R 1表示取代或未取代的氨基，R 3表示选自羧基，保护的羧基，酯，酰胺，酸酐，酰卤，酸叠氮化物和羧基盐，-SR2是亲硫性亲核试剂的残基。

88. 发明授权

US4207234A 4-Unsubstituted azetidinone derivatives and process for preparation thereof 失效
标题翻译： 4-取代氮杂环丁酮衍生物及其制备方法
公开(公告)号：US4207234A
公开(公告)日：1980-06-10
申请号：US858375
申请日：1977-12-07
申请人： Takashi Kamiya , Yoshihisa Saito , Masashi Hashimoto , Osamu Nakaguti , Teruo Oku , Youichi Shiokawa , Takao Takaya , Tadaaki Komori , Tsutomu Teraji , Keiji Hemmi , Hisashi Takasugi
发明人： Takashi Kamiya , Yoshihisa Saito , Masashi Hashimoto , Osamu Nakaguti , Teruo Oku , Youichi Shiokawa , Takao Takaya , Tadaaki Komori , Tsutomu Teraji , Keiji Hemmi , Hisashi Takasugi
IPC分类号： C07D205/085 , C07D473/00 , C07D205/08 , C07D401/12 , C07D403/12 , C07D409/12
CPC分类号： C07D205/085 , C07D473/00
摘要： New antimicrobial azetidinone derivatives and their salt of the formula: ##STR1## wherein R.sub.1 is amino or acylamino, and A is selected from a variety of groups.
摘要翻译：新的抗微生物氮杂环丁酮衍生物及其下式的盐：其中R 1是氨基或酰氨基，A选自多种基团。

89. 发明授权

US4056521A Penam and cepham derivatives and preparation thereof 失效
标题翻译： PENAM和CEPHAM衍生物及其制备方法
公开(公告)号：US4056521A
公开(公告)日：1977-11-01
申请号：US648492
申请日：1976-12-01
申请人： Takashi Kamiya , Tsutomu Teraji , Masashi Hashimoto , Osamu Nakaguti , Teruo Oku
发明人： Takashi Kamiya , Tsutomu Teraji , Masashi Hashimoto , Osamu Nakaguti , Teruo Oku
IPC分类号： C07D205/095 , C07D499/00 , C07D499/06 , C07D499/21 , C07D499/44 , C07D501/08 , C07D501/10
CPC分类号： C07D205/095 , C07D499/00
摘要： Disclosed are antibacterial penicillins of the formula ##STR1## wherein Y" is a residue of a strong nucleophile and processes for preparing same.

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