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1. 发明授权

US5326780A Imidazole derivatives having anti-HIV activity 失效
标题翻译：具有抗HIV活性的咪唑衍生物
公开(公告)号：US5326780A
公开(公告)日：1994-07-05
申请号：US3126
申请日：1993-01-12
申请人： Hirohiko Sugimoto , Masaru Ogata , Hiroshi Matsumoto , Ken-ichi Sugita , Akihiko Sato , Tamio Fujiwara
发明人： Hirohiko Sugimoto , Masaru Ogata , Hiroshi Matsumoto , Ken-ichi Sugita , Akihiko Sato , Tamio Fujiwara
IPC分类号： A61K31/415 , A61K31/44 , A61K31/4427 , A61P31/12 , C07D233/54 , C07D233/60 , C07D233/64 , C07D233/70 , C07D233/80 , C07D233/84 , C07D233/86 , C07D233/90 , C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06 , C07D233/66
CPC分类号： C07D233/56 , C07D233/64 , C07D233/80 , C07D233/84 , C07D233/86 , C07D233/90 , C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06
摘要： A novel imidazole derivatives of formula I: ##STR1## wherein R.sup.1 is hydrogen, alkyl, halogen, or optionally substituted aryl; R.sup.2 is alkyl, optionally substituted aryl optionally substituted aralkyl, or optionally substituted hetero ring group; R.sup.3 is hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl, or optionally substituted hydroxyalkyl; R.sup.4 is hydrogen, alkyl, halogen, acyl, optionally substituted hydroxyalkyl, optionally esterified or amidated carboxyl group, hydroxy group, aryl or arylthio; X is S, SO, SO.sub.2, CH.sub.2, or Se; n is an integer of 1 to 3, or a pharmaceutically acceptable salt thereof, said derivative having anti-HIV activity and being useful for the treatment of HIV infections.
摘要翻译：式I的新型咪唑衍生物：其中R 1是氢，烷基，卤素或任选取代的芳基; R 2是烷基，任选取代的芳基任选取代的芳烷基或任选取代的杂环基团; R 3是氢，烷基，任选取代的芳基，任选取代的芳烷基或任选取代的羟烷基; R 4为氢，烷基，卤素，酰基，任选取代的羟基烷基，任选酯化或酰胺化的羧基，羟基，芳基或芳硫基; X是S，SO，SO 2，CH 2或Se; n为1〜3的整数，或其药学上可接受的盐，所述衍生物具有抗HIV活性，可用于治疗HIV感染。

2. 发明授权

US5472965A Imidazole derivatives having anti-HIV activity 失效
标题翻译：具有抗HIV活性的咪唑衍生物
公开(公告)号：US5472965A
公开(公告)日：1995-12-05
申请号：US209627
申请日：1994-03-14
申请人： Hirohiko Sugimoto , Masaru Ogata , Hiroshi Matsumoto , Ken-ichi Sugita , Akihiko Sato , Tamio Fujiwara
发明人： Hirohiko Sugimoto , Masaru Ogata , Hiroshi Matsumoto , Ken-ichi Sugita , Akihiko Sato , Tamio Fujiwara
IPC分类号： A61K31/415 , A61K31/44 , A61K31/4427 , A61P31/12 , C07D233/54 , C07D233/60 , C07D233/64 , C07D233/70 , C07D233/80 , C07D233/84 , C07D233/86 , C07D233/90 , C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06 , A01N43/54 , A01N43/50 , A01N43/58 , A01N43/60 , C07D401/12 , C07D403/12
CPC分类号： C07D233/56 , C07D233/64 , C07D233/80 , C07D233/84 , C07D233/86 , C07D233/90 , C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06
摘要： A novel imidazole derivatives of formula I: ##STR1## wherein R.sup.1 is hydrogen, alkyl, halogen, or optionally substituted aryl; R.sup.2 is alkyl, optionally substituted aryl optionally substituted aralkyl, or optionally substituted hetero ring group; R.sup.3 is hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl, or optionally substituted hydroxyalkyl; R.sup.4 is hydrogen, alkyl, halogen, acyl, optionally substituted hydroxyalkyl, optionally esterified or amidated carboxyl group, hydroxy group, aryl or arylthio; X is S, SO, SO.sub.2, CH.sub.2, or Se; n is an integer of 1 to 3, or a pharmaceutically acceptable salt thereof, said derivative having anti-HIV activity and being useful for the treatment of HIV infections.
摘要翻译：式I的新型咪唑衍生物：其中R 1是氢，烷基，卤素或任选取代的芳基; R 2是烷基，任选取代的芳基任选取代的芳烷基或任选取代的杂环基团; R 3是氢，烷基，任选取代的芳基，任选取代的芳烷基或任选取代的羟烷基; R 4为氢，烷基，卤素，酰基，任选取代的羟基烷基，任选酯化或酰胺化的羧基，羟基，芳基或芳硫基; X是S，SO，SO 2，CH 2或Se; n为1〜3的整数，或其药学上可接受的盐，所述衍生物具有抗HIV活性，可用于治疗HIV感染。

3. 发明授权

US5017708A Azabicycloalkanes 失效
标题翻译：氮杂双环烷烃
公开(公告)号：US5017708A
公开(公告)日：1991-05-21
申请号：US404449
申请日：1989-09-08
申请人： Masaru Ogata , Hiroshi Matsumoto , Sumio Shimizu , Shiro Kida
发明人： Masaru Ogata , Hiroshi Matsumoto , Sumio Shimizu , Shiro Kida
IPC分类号： C07D209/08 , C07D209/44 , C07D209/48 , C07D209/52 , C07D491/044
CPC分类号： C07D209/52 , C07D209/44 , Y02P20/55
摘要： A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 each is hydrogen, hydroxy, oxo, halogen, azido, amino, C.sub.1 -C.sub.3 alkylamino, or aminomethyl, in which said amino, C.sub.1 -C.sub.3 alkylamino and aminomethyl each is optionally substituted by one or two members selected from the group consisting of C.sub.1 -C.sub.3 alkyl and amino-protecting group; n is an integer of 1 to 3; p and q each is an integer of 0 to 3 with proviso that p+q=1 to 4 or acid-addition salts thereof, being useful materials for preparing side chains of antibacterial quinolonecarboxylic acids, cephalosporines, or other antibiotics.

4. 发明授权

US4350635A N(2-Pyrrolidinylmethyl)meta-sulfonamido-benzamides 失效
标题翻译： N（2-吡咯烷基甲基）间 - 磺酰氨基 - 苯甲酰胺
公开(公告)号：US4350635A
公开(公告)日：1982-09-21
申请号：US124726
申请日：1980-02-26
申请人： Masaru Ogata , Hiroshi Matsumoto
发明人： Masaru Ogata , Hiroshi Matsumoto
IPC分类号： C07D207/09 , C07D207/14 , C07D307/14 , A61K31/40
CPC分类号： C07D207/14 , C07D207/09 , C07D307/14 , Y10S514/872 , Y10S514/96
摘要： Meta-sulfonamido-benzamide derivatives of the formula: ##STR1## wherein R is a hydrogen atom or a lower alkyl, cyano, or lower alkanesulfonyl group;R.sup.1 is a lower alkyl, phenyl, amino, lower alkylamino, di(lower)alkylamino, or C.sub.4 -C.sub.5 alkyleneamino group;R.sup.2 is a hydrogen or halogen atom or a lower alkyl, di(lower)alkylamino, or lower alkoxy group;R.sup.3 is a hydrogen atom or a methyl or methoxy group;R.sup.4 is a hydrogen or halogen atom;R.sup.5 is a lower alkyl, lower alkenyl, C.sub.3 -C.sub.6 cycloalkyl, benzyl, or halogenobenzyl group; andn is 1 or zeroor their acid addition salts, showing pharmacological activity such as anti-emetic or psychotropic activity, are provided via several routes.
摘要翻译：亚磺酰氨基 - 苯甲酰胺衍生物，其分子式如下：其中R是氢原子或低级烷基，氰基或低级链烷磺酰基; R 1是低级烷基，苯基，氨基，低级烷基氨基，二（低级）烷基氨基或C 4 -C 5亚烷基氨基; R2是氢或卤素原子或低级烷基，二（低级）烷基氨基或低级烷氧基; R3是氢原子或甲基或甲氧基; R4是氢或卤素原子; R5是低级烷基，低级烯基，C3-C6环烷基，苄基或卤代苄基; 并且n是1或0，或者它们的酸加成盐，显示药理活性，如抗呕吐或精神活性，通过几种途径提供。

5. 发明授权

US4330472A Meta-sulfonamido-benzamide derivatives 失效
标题翻译：亚磺酰氨基 - 苯甲酰胺衍生物
公开(公告)号：US4330472A
公开(公告)日：1982-05-18
申请号：US162793
申请日：1980-06-25
申请人： Masaru Ogata , Hiroshi Matsumoto
发明人： Masaru Ogata , Hiroshi Matsumoto
IPC分类号： C07D207/09 , C07D207/14 , C07D307/14 , C07D207/08
CPC分类号： C07D207/14 , C07D207/09 , C07D307/14 , Y10S514/872 , Y10S514/96
摘要： Meta-sulfonamido-benzamide derivatives of the formula: ##STR1## [wherein R is a hydrogen atom or a lower alkyl, cyano, or lower alkanesulfonyl group;R.sup.1 is a lower alkyl, phenyl, amino, lower alkylamino, di(lower)alkylamino, or C.sub.4 -C.sub.5 alkyleneamino group;R.sup.2 is a hydrogen or halogen atom or a lower alkyl, di(lower)alkylamino, or lower alkoxy group;R.sup.3 is a hydrogen atom or a methyl or methoxy group;R.sup.4 is a hydrogen or halogen atom;R.sup.5 is a lower alkyl, lower alkenyl, C.sub.3 -C.sub.6 cycloalkyl, benzyl, or halogenobenzyl group; and n is 1 or zero]or their acid addition salts, showing pharmacological activity such as anti-emetic or psychotropic activity, are provided via several routes.
摘要翻译：下式的亚磺酰氨基 - 苯甲酰胺衍生物：其中R是氢原子或低级烷基，氰基或低级链烷磺酰基; R 1是低级烷基，苯基，氨基，低级烷基氨基，二（低级）烷基氨基或C 4 -C 5亚烷基氨基; R2是氢或卤素原子或低级烷基，二（低级）烷基氨基或低级烷氧基; R3是氢原子或甲基或甲氧基; R4是氢或卤素原子; R5是低级烷基，低级烯基，C3-C6环烷基，苄基或卤代苄基; 并且n为1或0]或其酸性加成盐，显示出药理活性，如抗呕吐或精神活性，通过多种途径提供。

6. 发明授权

US4228165A Phenyl isothiocyanate derivatives and their production 失效
标题翻译：异硫氰酸苯酯衍生物及其生产
公开(公告)号：US4228165A
公开(公告)日：1980-10-14
申请号：US47803
申请日：1979-06-11
申请人： Masaru Ogata , Yoshihachi Watanabe , Hiroshi Matsumoto , Katsuya Tawara
发明人： Masaru Ogata , Yoshihachi Watanabe , Hiroshi Matsumoto , Katsuya Tawara
IPC分类号： C07D295/18 , A01N47/46 , C07C67/00 , C07C325/00 , C07C331/28 , C07D295/192 , C07D307/14 , A01N43/84 , C07C161/04 , C07D295/12 , C07D307/64
CPC分类号： C07D295/192 , A01N47/46 , C07C331/28
摘要： A compound of the formula: ##STR1## wherein X is oxygen or sulfur;R.sup.1 is hydroxy, C.sub.1 -C.sub.4 alkoxy, phenoxy, amino, C.sub.1 -C.sub.4 alkylamino, C.sub.2 -C.sub.8 dialkylamino, C.sub.6 -C.sub.10 arylamino, tetrahydrofurfurylamino, morpholino or methylpiperazino, but when X is sulfur R.sup.1 must be amino, C.sub.1 -C.sub.4 alkylamino, C.sub.2 -C.sub.8 dialkylamino or morpholino;R.sup.2 is C.sub.1 -C.sub.4 alkoxy or C.sub.2 -C.sub.5 alkoxycarbonyl;R.sup.3 is hydrogen C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.8 dialkylamino or halogenand its salts being useful as agricultural fungicides are provided.
摘要翻译：下式的化合物：其中X是氧或硫; R1是羟基，C1-C4烷氧基，苯氧基，氨基，C1-C4烷基氨基，C2-C8二烷基氨基，C6-C10芳基氨基，四氢糠基氨基，吗啉代或甲基哌嗪基，但是当X是硫时，R1必须是氨基，C1-C4烷基氨基，C2 -C8二烷基氨基或吗啉代; R2是C1-C4烷氧基或C2-C5烷氧基羰基; R3是氢C1-C4烷基，C1-C4烷氧基，C2-C8二烷基氨基或卤素，其盐可用作农业杀真菌剂。

7. 发明授权

US4988709A Quinolone-carboxylic acids as antibacterial agents 失效
标题翻译：喹诺酮 - 羧酸作为抗菌剂
公开(公告)号：US4988709A
公开(公告)日：1991-01-29
申请号：US353321
申请日：1989-05-15
申请人： Masaru Ogata , Hiroshi Matsumoto , Sumio Shimizu , Shiro Kida
发明人： Masaru Ogata , Hiroshi Matsumoto , Sumio Shimizu , Shiro Kida
IPC分类号： A61K31/435 , A61K31/47 , A61K31/475 , A61K31/535 , A61K31/55 , A61P31/04 , C07D401/04 , C07D471/04 , C07D498/06
CPC分类号： C07D401/04 , C07D471/04 , Y02P20/55
摘要： Novel pyridonecarboxylic acids of the formula: ##STR1## or the pharmaceutically acceptable salts thereof having a more potent and longer lasting antibacterial activities against gram-positive and gram-negative bacteria than known analogues, useful for antibacterial agents at an oral dose of 1-500 mg, preferably 50-100 mg per day to an adult.

8. 发明授权

US4328348A Novel benzylimidazole derivatives 失效
标题翻译：新型苄基咪唑衍生物
公开(公告)号：US4328348A
公开(公告)日：1982-05-04
申请号：US157166
申请日：1980-06-06
申请人： Masaru Ogata , Katsuya Tawara , Yoshihachi Watanabe , Hiroshi Matsumoto , Toshio Takahashi
发明人： Masaru Ogata , Katsuya Tawara , Yoshihachi Watanabe , Hiroshi Matsumoto , Toshio Takahashi
IPC分类号： A01N43/50 , C07C53/08 , C07C55/06 , C07C55/10 , C07C59/245 , C07C59/255 , C07C59/265 , C07C65/10 , C07D233/54 , C07D233/56 , C07D233/60 , C07D521/00 , C07D233/96
CPC分类号： C07D233/64 , A01N43/50 , C07C53/08 , C07C55/06 , C07C55/10 , C07C59/245 , C07C59/255 , C07C59/265 , C07C65/10 , C07D231/12 , C07D233/56 , C07D249/08
摘要： Novel benzylimidazole derivatives of the formula: ##STR1## wherein X is halogen, nitro, alkyl, alkoxy, or halobenzyloxy;m is an integer of 0 to 3;Y is oxa, thia or substituted- or unsubstituted-imino;R.sup.1 is alkyl, dialkylaminoalkyl, dibenzylaminoalkyl, 1-pyrrolidinyl, 2-imidazolin-2-yl, or a group of --(CH.sub.2)n--Z--Q(whereinn is an integer of 0 to 4;Z is oxa, thia, or a single bond; andQ is substituted- or unsubstituted-phenyl or thienyl) ##STR2## is methylene, 1-(1-imidazolyl)-1-methylmethylene, 1-(1-imidazolyl)-1-phenylmethylene, 1-phenylmethylene, or substituted or unsubstituted alkylidene;the benzene ring of the above formula being optionally condensed with another benzene ringwith the proviso that when ##STR3## is methylene said benzene ring is condensed with another benzene ring, and acid addition salts thereof which are useful as an antimycotic drug or agricultural fungicide.
摘要翻译：下式的新型苄基咪唑衍生物：其中X是卤素，硝基，烷基，烷氧基或卤代苄氧基; m为0〜3的整数。 Y是氧杂，硫杂或取代或未取代的亚氨基; R1是烷基，二烷基氨基烷基，二苄基氨基烷基，1-吡咯烷基，2-咪唑啉-2-基或 - （CH2）nZQ（其中n是0-4的整数; Z是氧杂，硫杂或单键） ;和Q是取代或未取代的苯基或噻吩基）是甲亚甲基，1-（1-咪唑基）-1-甲基亚甲基，1-（1-咪唑基）-1-苯基亚甲基，1-苯基亚甲基，或取代或未取代的未取代的亚烷基; 上式的苯环任选地与另一个苯环稠合，条件是当亚甲基时，苯环与另一个苯环缩合，其酸加成盐可用作抗真菌药物或农药杀真菌剂。

9. 发明授权

US4041026A 1,5-Dihydro-2H-1,4-benzodiazepin-2-one derivatives 失效
标题翻译： 1,5-二氢-2H-1,4-苯并二氮杂-2-酮衍生物
公开(公告)号：US4041026A
公开(公告)日：1977-08-09
申请号：US720832
申请日：1976-09-07
申请人： Masaru Ogata , Hiroshi Matsumoto
发明人： Masaru Ogata , Hiroshi Matsumoto
IPC分类号： A61K31/55 , A61K31/551 , A61P25/08 , A61P25/20 , A61P25/26 , C07D243/16 , C07D243/18 , C07D243/24 , C07D243/26
CPC分类号： C07D243/24
摘要： 1,5-Dihydro-2H-1,4-benzodiazepin-2-one derivatives of the formula: ##STR1## (wherein Ar represents pyridyl, phenyl, or halogenophenyl; R represents C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkyl substituted by a member selected from the group consisting of trifluoromethyl, cyano, carbamoyl, C.sub.2 -C.sub.10 dialkylamino, and hydroxy; R.sup.1 represents halogen, nitro, trifluoromethyl, or cyano; and R.sup.2 represents C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkyl substituted by a member selected from the group consisting of halogen, hydroxy, and C.sub.1 -C.sub.6 alkoxy), being useful as anxiolytics, sedatives, anticonvulsants, hypnotics, or their synthetic intermediates, are prepared.
摘要翻译：（其中Ar表示吡啶基，苯基或卤代苯基; R表示C 1 -C 6烷基或被C 1 -C 6烷基取代的C 1 -C 6烷基）的1,5-二氢-2H-1,4-苯并二氮杂- 选自三氟甲基，氰基，氨基甲酰基，C 2 -C 10二烷基氨基和羟基的基团; R 1表示卤素，硝基，三氟甲基或氰基; R 2表示被选自下列的基团取代的C 1 -C 6烷基或C 1 -C 6烷基：由卤素，羟基和C 1 -C 6烷氧基组成的组）可用作抗焦虑剂，镇静剂，抗惊厥药，催眠药或其合成中间体。

10. 发明授权

US4612322A Azole type dioxolane derivatives 失效
标题翻译：唑型二氧戊环衍生物
公开(公告)号：US4612322A
公开(公告)日：1986-09-16
申请号：US632852
申请日：1984-07-20
申请人： Masaru Ogata , Hiroshi Matsumoto , Shiro Kida , Katsuya Tawara
发明人： Masaru Ogata , Hiroshi Matsumoto , Shiro Kida , Katsuya Tawara
IPC分类号： A01N43/653 , A01N43/832 , A61K31/41 , A61P31/04 , A61P31/10 , C07D249/08 , C07D317/00 , C07D327/00 , C07D405/06 , C07D411/06 , C07D521/00 , A01N43/50
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： A compound of the formula: ##STR1## (wherein Az is imidazolyl or triazolyl;R is C.sub.1 -C.sub.5 alkyl or phenyl optionally substituted by 1 to 3 members selected from halogen, C.sub.1 -C.sub.5 alkyl, and C.sub.1 -C.sub.5 alkoxy;X.sup.1 and X.sup.2 each is hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, or C.sub.1 -C.sub.5 alkoxy;Y is C.dbd.O, C.dbd.S, S.dbd.O, or R.sup.1 --C--R.sup.2 ; andR.sup.1 and R.sup.2 each is hydrogen, C.sub.1 -C.sub.3 alkyl or, taken together may form C.sub.4 -C.sub.6 alkylene)or its acid addition salt being useful as an antimycotic agent is prepared by reacting a corresponding diol with a cyclizing agent.
摘要翻译：下式的化合物（其中Az为咪唑基或三唑基; R为C1-C5烷基或任选被1至3个选自卤素，C 1 -C 5烷基和C 1 -C 5烷氧基的成员取代的苯基; X 1和X 2 各自为氢，卤素，C1-C5烷基或C1-C5烷氧基; Y为C = O，C = S，S = O或R1-C-R2; R1和R2各自为氢，C1-C3烷基或一起可以形成C4-C6亚烷基）或其酸加成盐可用作抗真菌剂通过使相应的二醇与环化剂反应来制备。

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