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1. 发明授权

US4780472A Hydantoin derivatives for treating complications of diabetes 失效
标题翻译：用于治疗糖尿病并发症的乙内酰脲衍生物
公开(公告)号：US4780472A
公开(公告)日：1988-10-25
申请号：US117887
申请日：1987-11-02
申请人： Kouichiro Ueda , Satoru Tanaka , Toshinobu Kunii , Kengo Kagei , Tadashi Sato , Hideki Ono , Issei Ohtsuka , Mayumi Kawase , Toshiharu Ohgoh , Tsuneo Wakabayashi
发明人： Kouichiro Ueda , Satoru Tanaka , Toshinobu Kunii , Kengo Kagei , Tadashi Sato , Hideki Ono , Issei Ohtsuka , Mayumi Kawase , Toshiharu Ohgoh , Tsuneo Wakabayashi
IPC分类号： A61K31/415 , A61P3/08 , A61P3/10 , A61P9/10 , A61P25/02 , A61P27/02 , A61P27/12 , C07D233/72 , C07D491/107 , C07D493/10 , C07D495/10
CPC分类号： C07D493/10 , C07D495/10
摘要： Hydantoin derivatives and salts thereof, the process for the preparation thereof, and medicines containing the same, wherein the hydantoin derivatives are represented by the general formula: ##STR1## wherein the substituents are defined hereinbelow. The hydantoin derivatives and salts thereof have excellent effects for the treamtment of the complications of the diabetes mellitus.
摘要翻译：乙内酰脲衍生物及其盐，其制备方法和含有其的药物，其中乙内酰脲衍生物由以下通式表示：其中取代基在下文定义。乙内酰脲衍生物及其盐对糖尿病并发症的改善具有优异的效果。

2. 发明授权

US4874869A Hydantoin derivatives and medicines containing the same 失效
标题翻译：乙内酰脲衍生物和含有它们的药物
公开(公告)号：US4874869A
公开(公告)日：1989-10-17
申请号：US73915
申请日：1987-07-13
申请人： Kouichiro Ueda , Satoru Tanaka , Toshinobu Kunii , Kengo Kagei , Tadashi Sato , Hideki Ono , Issei Ohtsuka , Mayumi Kawase , Toshiharu Ohgoh , Tsuneo Wakabayashi
发明人： Kouichiro Ueda , Satoru Tanaka , Toshinobu Kunii , Kengo Kagei , Tadashi Sato , Hideki Ono , Issei Ohtsuka , Mayumi Kawase , Toshiharu Ohgoh , Tsuneo Wakabayashi
IPC分类号： A61K31/415 , A61P3/08 , A61P3/10 , A61P9/10 , A61P25/02 , A61P27/02 , A61P27/12 , C07D233/72 , C07D491/107 , C07D493/10 , C07D495/10
CPC分类号： C07D493/10 , C07D495/10
摘要： Novel hydantoin derivatives and salts thereof, the process for the preparation thereof, and medicines containing the same, wherein the hydantoin derivatives are represented by the general formula: ##STR1## wherein X.sub.1 and X.sub.2, which may be the same or different, mean independently hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; Y means oxygen atom or sulfur atom, R.sub.1 and R.sub.2, which may be the same or different, mean independently hydrogen atom, a lower alkyl group or phenyl group, or the both may form a ring with a carbon atom which is combined with them, excluding the case wherein both R.sub.1 and R.sub.2 are hydrogen atom at the same time, and n means an integer of 0 or 1. The novel hydantoin derivatives and salts thereof have excellent effects for the treatment of the complications of the diabetes mellitus.
摘要翻译：新颖的乙内酰脲衍生物及其盐，其制备方法和含有它们的药物，其中乙内酰脲衍生物由以下通式表示：其中X1和X2可以相同或不同，独立地表示氢原子，卤素原子，低级烷基或低级烷氧基; Y表示氧原子或硫原子，可以相同或不同的R 1和R 2独立地表示氢原子，低级烷基或苯基，或者二者可以与与它们结合的碳原子形成环，不包括R1和R2同时为氢原子的情况，n表示0或1的整数。新的乙内酰脲衍生物及其盐对于治疗糖尿病并发症具有优异的效果。

3. 发明授权

US4540704A Treating complications of diabetes mellitus with hydantoin derivatives 失效
标题翻译：用乙内酰脲衍生物治疗糖尿病并发症
公开(公告)号：US4540704A
公开(公告)日：1985-09-10
申请号：US500801
申请日：1983-06-07
申请人： Kouichiro Ueda , Satoru Tanaka , Toshinobu Kunii , Kengo Kagei , Tadashi Sato , Ono Hideki , Issei Ohtsuka , Mayumi Kawase , Toshiharu Ohgoh , Tsuneo Wakabayashi
发明人： Kouichiro Ueda , Satoru Tanaka , Toshinobu Kunii , Kengo Kagei , Tadashi Sato , Ono Hideki , Issei Ohtsuka , Mayumi Kawase , Toshiharu Ohgoh , Tsuneo Wakabayashi
IPC分类号： A61K31/415 , A61P3/08 , A61P3/10 , A61P9/10 , A61P25/02 , A61P27/02 , A61P27/12 , C07D233/72 , C07D491/107 , C07D493/10 , C07D495/10
CPC分类号： C07D493/10 , C07D495/10
摘要： Novel hydantoin derivatives and salts thereof, the process for the preparation thereof, and medicines containing the same, wherein the hydantoin derivatives are represented by the general formula: ##STR1## wherein X.sub.1 and X.sub.2, which may be the same or different, independently represent a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; Y represents an oxygen atom or sulfur atom, R.sub.1 and R.sub.2, which may be the same or different, independently represent a hydrogen atom, a lower alkyl group or phenyl group, or both may form a ring with carbon atoms, excluding the case wherein both R.sub.1 and R.sub.2 are hydrogen atom, and n represents 0 or 1. The novel hydantoin derivatives and salts thereof have excellent effects for the treatment of the complications of diabetes mellitus.
摘要翻译：新颖的乙内酰脲衍生物及其盐，其制备方法和含有它们的药物，其中乙内酰脲衍生物由以下通式表示：其中X1和X2可以相同或不同，独立地表示氢原子，卤素原子，低级烷基或低级烷氧基; Y表示氧原子或硫原子，可以相同或不同的R 1和R 2独立地表示氢原子，低级烷基或苯基，或两者可以形成具有碳原子的环，不同之处在于两者 R1和R2是氢原子，n代表0或1.新的乙内酰脲衍生物及其盐具有治疗糖尿病并发症的优异效果。

4. 发明授权

US5668136A Trisubstituted benzene derivatives, composition and methods of treatment 失效
标题翻译：三取代苯衍生物，组成及处理方法
公开(公告)号：US5668136A
公开(公告)日：1997-09-16
申请号：US757908
申请日：1991-09-11
申请人： Teiji Kimura , Nobuhisa Watanabe , Yasutaka Takase , Kenji Hayashi , Makoto Matsui , Hironori Ikuta , Youji Yamagishi , Kozo Akasaka , Hiroshi Tanaka , Issei Ohtsuka , Takao Saeki , Motoji Kogushi , Tohru Fujimori , Isao Saito
发明人： Teiji Kimura , Nobuhisa Watanabe , Yasutaka Takase , Kenji Hayashi , Makoto Matsui , Hironori Ikuta , Youji Yamagishi , Kozo Akasaka , Hiroshi Tanaka , Issei Ohtsuka , Takao Saeki , Motoji Kogushi , Tohru Fujimori , Isao Saito
IPC分类号： A61K31/135 , A61K31/165 , A61K31/17 , A61K31/18 , A61K31/27 , A61K31/275 , A61K31/415 , A61K31/505 , A61P3/06 , A61P9/10 , C07C233/18 , C07C255/58 , C07C255/59 , C07C255/60 , C07C275/34 , C07C275/40 , C07D211/14 , C07D213/02 , C07D233/54 , C07D233/60 , C07D233/68 , C07D233/90 , C07D233/96 , C07D235/02 , C07D235/06 , C07D235/12 , C07D235/14 , C07D249/04 , C07D249/06 , C07D249/18 , C07D253/08 , C07D257/04 , C07D295/08 , C07D295/092 , C07D401/04 , C07D401/12 , C07D403/12 , C07D521/00 , A61K31/495 , C07D241/04
CPC分类号： C07D233/64 , C07C275/40 , C07D211/14 , C07D231/12 , C07D233/56 , C07D233/68 , C07D233/90 , C07D235/02 , C07D235/06 , C07D235/12 , C07D235/14 , C07D249/06 , C07D249/08 , C07D249/18 , C07D257/04 , C07D295/088 , C07D401/12 , C07D403/12
摘要： A benzene, pyridine or pyrimidine derivative having the below shown formula is novel and useful as an anti-arteriosclerotic agent. ##STR1## wherein R.sup.1 stands for a lower alkyl group, an amino group which may be substituted, or the like; R.sup.2 stands for a group represented by the formula: ##STR2## (wherein R.sup.16 stands for an alkyl group having 1 to 6 carbon atoms, or the like) or the like; R.sup.3 stands for a group represented by the formula: --O--(CH.sub.2).sub.m --Y (Y stands for an imidazolyl or piperazinyl group, or the like and m is 1 to 6) or the like; R.sup.5 stands for a hydrogen atom, a lower alkyl group, or the like; A stands for a group represented by the formula: ##STR3## (wherein R.sup.6 stands for a hydrogen atom, a lower alkyl group, or the like), --N.dbd., or the like; and B stands for a group represented by the formula: ##STR4## (wherein R.sup.4 stands for a hydrogen or the like), --N.dbd., or the like.
摘要翻译：具有下式所示的苯，吡啶或嘧啶衍生物是新颖的，可用作抗动脉硬化剂。（I）其中R1代表低级烷基，可被取代的氨基等; R2代表由下式表示的基团：其中R16表示碳原子数1〜6的烷基等）等。 R3表示由下式表示的基团：-O-（CH 2）m -Y（Y表示咪唑基或哌嗪基等，m为1至6）等; R5代表氢原子，低级烷基等; A表示由下式表示的基团：其中R6表示氢原子，低级烷基等，-N =等; B代表由下式表示的基团：其中R4代表氢等，-N =等。

5. 发明授权

US5462958A Benzene derivatives and method of treating arteriosclerosis with benzene derivatives 失效
标题翻译：苯衍生物和苯衍生物治疗动脉硬化的方法
公开(公告)号：US5462958A
公开(公告)日：1995-10-31
申请号：US182061
申请日：1994-05-19
申请人： Kenji Hayashi , Nobuhisa Watanabe , Koichi Nose , Hiroshi Tanaka , Issei Ohtsuka , Motoji Kokushi , Hironobu Hiyoshi , Hiroko Kobayashi , Toshie Yamada , Toru Horie
发明人： Kenji Hayashi , Nobuhisa Watanabe , Koichi Nose , Hiroshi Tanaka , Issei Ohtsuka , Motoji Kokushi , Hironobu Hiyoshi , Hiroko Kobayashi , Toshie Yamada , Toru Horie
IPC分类号： C07C275/34 , C07D233/54 , C07D233/60 , C07D233/64 , A61K31/415 , A61K31/195
CPC分类号： C07D233/64 , C07C275/34
摘要： The present invention provides a novel benzene derivative useful as a preventive and medically treating medicine for arteriosclerosis, and a cholesterol O-acyl transferase inhibitor comprising the benzene derivative as an active ingredient.The benzene derivative according to the present invention is represented by the following general formula (I): ##STR1## wherein R.sup.1 represents a carboxyl group which may be protected or a group represented by the formula: ##STR2## wherein R.sup.5 represents a lower alkyl group or a hydroxyalkyl group and R.sup.6 represents a hydrogen atom or a hydroxyl group; R.sup.2 represents a hydrogen atom, a lower alkyl group or the like; R.sup.3 and R.sup.4 each represent a hydrogen atom or a hydroxyl group; and p is an integer of 1 to 6.
摘要翻译： PCT No.PCT / JP93 / 00961 Sec。 371日期1994年5月19日 102（e）日期1994年5月19日PCT提交1993年7月12日PCT公布。出版物WO94 / 02452 日本1993年3月2日。本发明提供了可用作预防和医学治疗动脉硬化药物的苯衍生物，以及含有苯衍生物作为活性成分的胆固醇O-酰基转移酶抑制剂。根据本发明的苯衍生物由以下通式（I）表示：其中R 1表示可被保护的羧基或由下式表示的基团：其中R5表示低级烷基或羟烷基，R6表示氢原子或羟基; R2表示氢原子，低级烷基等; R3和R4各自表示氢原子或羟基; p为1〜6的整数。

6. 发明授权

US5453524A Phosphorus-containing isoprenoid derivatives 失效
标题翻译：含磷类异戊二烯衍生物
公开(公告)号：US5453524A
公开(公告)日：1995-09-26
申请号：US199231
申请日：1994-02-22
申请人： Katsuya Tagami , Ichirou Yoshida , Naoki Kobayashi , Yoshio Fukuda , Yoshihito Eguchi , Makoto Nakagawa , Hironobu Hiyoshi , Hironori Ikuta , Makoto Kaino , Kenji Hayashi , Issei Ohtsuka , Shinya Abe , Shigeru Souda
发明人： Katsuya Tagami , Ichirou Yoshida , Naoki Kobayashi , Yoshio Fukuda , Yoshihito Eguchi , Makoto Nakagawa , Hironobu Hiyoshi , Hironori Ikuta , Makoto Kaino , Kenji Hayashi , Issei Ohtsuka , Shinya Abe , Shigeru Souda
IPC分类号： A61K31/66 , A61P3/06 , C07C211/21 , C07C233/03 , C07F9/38 , C07F9/40 , C07F9/02
CPC分类号： C07F9/405 , C07C211/21 , C07C233/03 , C07F9/3808 , C07F9/3826 , C07F9/3843 , C07F9/3873 , C07F9/4006 , C07F9/4015 , C07F9/4025
摘要： The present invention provides a phosphorus-containing isoprenoid derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is useful as a preventive and therapeutic agent for diseases for which a squalene synthetase inhibiting action is efficacious: ##STR1## wherein R.sup.1 and R.sup.2 each represent a hydrogen atom, a lower alkyl, cycloalkyl, alkenyl or alkynyl group, an aryl group which may be substituted, an arylalkyl group in which the aryl group may be substituted, or a heteroaryl or heteroarylalkyl group: R.sup.3 and R.sup.4 each represent a hydrogen atom, a lower alkyl group or an alkali metal; Y represents a group represented by the formula: ##STR2## (wherein R.sup.5 and R.sup.6 each represent a hydrogen atom, a lower alkyl group or an alkali metal or a group represented by the formula: --CO.sub.2 R.sup.7 (wherein R.sup.7 represents a hydrogen atom, a lower alkyl group or an alkali metal); Z represents a group represented by the Formula: --(CH.sub.2).sub.m -- (wherein m is an integer of 0 to 3), a group represented by the formula: --(CH.sub.2).sub.p --CH.dbd.CH--(CH.sub.2).sub.q -- (wherein p is 0 or 1 and q is 1 or 2) or a group represented by the Formula: ##STR3## (wherein R.sup.8 represents a hydrogen atom or a lower alkyl group; A represents an alkylene chain which has 1 to 5 carbon atoms and which may have a substituent on each carbon atom; and r is zero or an integer of 1 to 5); and n is zero or an integer of 1 to 5.
摘要翻译： PCT No.PCT / JP92 / 01082 Sec。 371日期：1994年2月22日 102（e）日期1994年2月22日PCT提交1992年8月27日PCT公布。公开号WO93 / 04073 日本1993年3月4日。本发明提供由以下通式（I）表示的含磷类异戊二烯衍生物或其药理学上可接受的盐，其可用作抑制角鲨烯合成酶的疾病的预防和治疗剂作用有效：其中R 1和R 2各自表示氢原子，低级烷基，环烷基，烯基或炔基，可被取代的芳基，芳基可以被取代的芳基烷基或杂芳基或杂芳基烷基：R 3和R 4各自表示氢原子，低级烷基或碱金属; Y表示由下式表示的基团：其中R 5和R 6各自表示氢原子，低级烷基或碱金属或由下式表示的基团：-CO 2 R 7（其中R 7表示氢原子，低级烷基或碱金属）; Z表示由下式表示的基团： - （CH 2）m - （其中m为0至3的整数），由下式表示的基团： - （CH 2）p-CH = CH-（CH 2）q - （其中p为0或1，q为1或2）或由下式表示的基团：其中R8表示氢原子或低级烷基; A表示亚烷基具有1至5个碳原子并且在每个碳原子上可以具有取代基的链;并且r为0或1至5的整数）; n为0或1至5的整数。

7. 发明授权

US5719303A Phosphonic acid derivatives 失效
标题翻译：膦酸衍生物
公开(公告)号：US5719303A
公开(公告)日：1998-02-17
申请号：US530311
申请日：1995-09-06
申请人： Ichirou Yoshida , Hironori Ikuta , Yoshio Fukuda , Yoshihito Eguchi , Makoto Kaino , Katsuya Tagami , Naoki Kobayashi , Kenji Hayashi , Hironobu Hiyoshi , Issei Ohtsuka , Makoto Nakagawa , Shinya Abe , Shigeru Souda
发明人： Ichirou Yoshida , Hironori Ikuta , Yoshio Fukuda , Yoshihito Eguchi , Makoto Kaino , Katsuya Tagami , Naoki Kobayashi , Kenji Hayashi , Hironobu Hiyoshi , Issei Ohtsuka , Makoto Nakagawa , Shinya Abe , Shigeru Souda
IPC分类号： A61K31/66 , A61K31/675 , A61P3/06 , A61P9/12 , C07F9/38 , C07F9/40 , C07F9/547 , C07F9/572 , C07F9/58 , C07F9/59 , C07F9/60 , C07F9/62 , C07F9/6503 , C07F9/6506 , C07F9/6509 , C07F9/6512 , C07F9/653 , C07F9/6533 , C07F9/6539 , C07F9/6541 , C07F9/655 , C07F9/6553 , C07F9/6558 , C07F9/6574
CPC分类号： C07F9/65746 , C07F9/3808 , C07F9/3826 , C07F9/3839 , C07F9/386 , C07F9/3873 , C07F9/4006 , C07F9/4015 , C07F9/4025 , C07F9/404 , C07F9/405 , C07F9/4056 , C07F9/4075 , C07F9/5721 , C07F9/5727 , C07F9/5728 , C07F9/582 , C07F9/588 , C07F9/591 , C07F9/592 , C07F9/598 , C07F9/60 , C07F9/62 , C07F9/65038 , C07F9/65061 , C07F9/65068 , C07F9/650958 , C07F9/650994 , C07F9/65127 , C07F9/653 , C07F9/65324 , C07F9/6533 , C07F9/6539 , C07F9/6541 , C07F9/65505 , C07F9/65515 , C07F9/65517 , C07F9/6552 , C07F9/65522 , C07F9/655345 , C07F9/65583 , C07F9/65586 , C07F9/65742
摘要： A phosphonic acid derivative which is useful for medically treating hyperlipemia, represented by the following general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## Representative example of the compound according to the present invention is one represented by the following formula: ##STR2##
摘要翻译： PCT No.PCT / JP94 / 00354 Sec。 371日期：1995年9月6日 102（e）日期1995年9月6日PCT 1994年3月4日PCT公布。 WO94 / 20508 PCT公开号日期：1994年9月15日由以下通式（I）表示的用于医疗治疗高脂血症的膦酸衍生物或其药理学上可接受的盐：（I）本发明化合物的代表性实例是一个由以下公式表示：

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