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1. 发明授权

US4661607A Furoxanthone derivatives useful as diuretics 失效
标题翻译：呋喃西酮衍生物可用作利尿剂
公开(公告)号：US4661607A
公开(公告)日：1987-04-28
申请号：US775240
申请日：1985-09-12
申请人： Hiroshi Koga , Takashi Mori , Takashi Dan , Michitaka Akima
发明人： Hiroshi Koga , Takashi Mori , Takashi Dan , Michitaka Akima
IPC分类号： A61K31/35 , C07D311/86 , C07D493/04
CPC分类号： C07D493/04 , C07D311/86 , Y10S514/869
摘要： Xanthone derivatives of the formula (I): ##STR1## (wherein W, X, Y and Z which may be the same or different represent a hydrogen atom, a halogen atom or a lower alkyl group having 1 to 4 carbon atoms; A is hydrogen atom or together with Z forms a --CH.sub.2 -- group which binds to a phenyl carbon adjacent the phenyl carbon to which the oxygen of the group ##STR2## is attached to form a cyclic methylene chain; B is a hydroxymethyl group, a lower alkoxycarbonyl group having 1 to 4 carbon atoms, or a carboxyl group, provided that W is neither a hydrogen atom nor a 7-position methyl group when X, Y and Z are each a hydrogen atom, and A is a hydrogen atom and B is a carboxyl group or a lower alkoxycarbonyl group), as well as non-toxic salts thereof when B is a carboxyl group, and a process for preparing the same are disclosed.The compounds of formula (I) in accordance with the present invention are useful as diuretics having uricosuric activity and can be used in the treatment of edema or hypertension.
摘要翻译：式（I）的呫吨酮衍生物：其中W，X，Y和Z可以相同或不同，表示氢原子，卤素原子或碳原子数1〜4的低级烷基 ; A是氢原子或与Z一起形成-CH 2 - 基团，其结合与苯基碳相邻的苯基碳，所述基团的氧连接到其上以形成环状亚甲基链; B是羟甲基，具有1至4个碳原子的低级烷氧基羰基或羧基，条件是当X，Y和Z各自为氢原子时，W既不是氢原子也不是7-位甲基，A为氢原子， B为羧基或低级烷氧基羰基），以及B为羧基时的无毒性盐，以及其制备方法。根据本发明的式（I）化合物可用作具有尿酸活性的利尿剂，并且可用于治疗水肿或高血压。

2. 发明授权

US4732906A Dioxolobenzizoxazole derivatives 失效
标题翻译：二氧代苯并恶唑衍生物
公开(公告)号：US4732906A
公开(公告)日：1988-03-22
申请号：US840680
申请日：1986-03-18
申请人： Hiroshi Koga , Takashi Dan , Haruhiko Sato , Etsuro Onuma
发明人： Hiroshi Koga , Takashi Dan , Haruhiko Sato , Etsuro Onuma
IPC分类号： A61K31/357 , A61K31/42 , A61P7/10 , C07D261/00 , C07D317/00 , C07D498/04 , C07D261/20
CPC分类号： C07D498/04
摘要： Dioxolobenzisoxazole derivatives of the formula ##STR1## wherein R.sub.1 is a phenyl group which may be substituted with a halogen atom, a lower alkyl group having 1-3 carbon atoms or a lower haloalkyl group, or a thienyl group; R.sub.2 is a hydrogen atom or a lower alkyl group having 1-4 carbon atoms; and X and Y which may be the same or different represent a hydrogen atom or a halogen atom, as well as non-toxic salts thereof wherein R.sub.2 is a hydrogen atom, a process for preparing the same and a pharmaceutical composition containing the same are disclosed.The derivatives have diuretic and uricosuric activities and, therefore, are useful as a drug for treating hyperuricemia or hypertension.
摘要翻译：其中R 1是可以被卤素原子取代的苯基，具有1-3个碳原子的低级烷基或低级卤代烷基，或噻吩基的式Ⅱ的二氧代联苯并恶唑衍生物; R2是氢原子或具有1-4个碳原子的低级烷基; 和可以相同或不同的X和Y表示氢原子或卤素原子，以及其中R2是氢原子的无毒盐，其制备方法和含有它们的药物组合物。衍生物具有利尿和尿酸活性，因此可用作治疗高尿酸血症或高血压的药物。

3. 发明授权

US4816479A Xanthone derivatives and process for producing the same 失效
标题翻译：呫吨衍生物及其制备方法
公开(公告)号：US4816479A
公开(公告)日：1989-03-28
申请号：US937101
申请日：1986-12-02
申请人： Hiroshi Koga , Takashi Mori , Takashi Dan , Michitaka Akima
发明人： Hiroshi Koga , Takashi Mori , Takashi Dan , Michitaka Akima
IPC分类号： A61K31/35 , C07D311/86 , C07D493/04
CPC分类号： C07D493/04 , C07D311/86 , Y10S514/869
摘要： Xanthone derivatives of the formula (I): ##STR1## wherein W, X, Y and Z which may be the same or different represent a hydrogen atom, a halogen atom or a lower alkyl group having 1 to 4 carbon atoms; A is a hydrogen atom B is a hydroxymethyl group, a lower alkoxycarbonyl group having 1 to 4 carbon atoms, or a carboxyl group, provided that a --O--CH.sub.2 --B group is bonded to the 2- or 3-position of the xanthone ring and that there is no case in which X, Y, and Z are each a hydrogen atom concurrently; as well as intoxic salts thereof when B is a carboxyl group, and a process for preparing the same are disclosed.The compounds of formula (I) in accordance with the present invention are useful as diuretics having uricosuric activity and can be used in the treatment of edema or hypertension.

4. 发明授权

US4791209A Furobenzisoxazole derivatives 失效
标题翻译：呋喃苯并恶唑衍生物
公开(公告)号：US4791209A
公开(公告)日：1988-12-13
申请号：US860210
申请日：1986-05-06
申请人： Haruhiko Sato , Hiroshi Koga , Takashi Dan , Etsuro Onuma
发明人： Haruhiko Sato , Hiroshi Koga , Takashi Dan , Etsuro Onuma
IPC分类号： C07D498/04 , A61K31/42
CPC分类号： C07D498/04
摘要： Novel furobenzisoxazole derivatives of the formula (I): ##STR1## (wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 which may be the same or different represent a hydrogen atom, a halogen atom, or a lower alkyl group having 1-4 carbon atoms; R.sub.5 is a hydroxymethyl group, a carboxyl group or a lower alkoxy carbonyl group having 1-3 carbon atoms; and X is a sulfur atom or a --CH.dbd.CH-- group), as well as intoxic salts thereof when R.sub.5 is a carboxyl group, and process for preparing the same are disclosed.The derivatives of formula (I) and nontoxic salts thereof have hypotensive, uricosuric and diuretic activities and hence ae useful as therapeutics for treating hyperuricemia, edema and hypertension.
摘要翻译：式（I）的新型呋喃苯并异恶唑衍生物：其中R 1，R 2，R 3和R 4可以相同或不同，表示氢原子，卤素原子或具有1-4个碳原子的低级烷基碳原子; R5是羟基甲基，羧基或具有1-3个碳原子的低级烷氧基羰基; X是硫原子或-CH = CH-基团），以及当其为R5时的中性盐羧基，及其制备方法。式（I）的衍生物及其无毒盐具有降血压，尿酸和利尿活性，因此可用作治疗高尿酸血症，水肿和高血压的治疗剂。

5. 发明授权

US4500714A 3-Substituted-ureido-N-pyridyl benzamides 失效
标题翻译： 3-取代的脲基-N-吡啶基苯甲酰胺
公开(公告)号：US4500714A
公开(公告)日：1985-02-19
申请号：US435541
申请日：1982-10-07
申请人： Masamitsu Honda , Hideaki Nagai , Shoko Takishima , Akinori Kawamura , Noriko Kawamura , Takashi Dan , Masuo Koizumi , Yasushi Murakami , Yoshikazu Hinohara , Hideki Nakano , Yoshio Takagaki
发明人： Masamitsu Honda , Hideaki Nagai , Shoko Takishima , Akinori Kawamura , Noriko Kawamura , Takashi Dan , Masuo Koizumi , Yasushi Murakami , Yoshikazu Hinohara , Hideki Nakano , Yoshio Takagaki
IPC分类号： C07D213/40 , C07D213/75
CPC分类号： C07D213/40 , C07D213/75
摘要： Benzamide derivatives of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom, a methyl group or a methoxy group; R.sub.2 is a straight-chain or branched-chain alkyl group having 2 to 8 carbon atoms, a substituted phenyl group, or group --NHR.sub.4, R.sub.4 being a hydrogen atom, a straight-chain or branched-chain or cyclic alkyl group having 1 to 6 carbon atoms, or a phenyl group that may have a substituent on the nucleus; R.sub.3 is a hydrogen atom or one or two alkyl groups having 1 to 4 carbon atoms and n is 0 or 1, a process for preparing these derivatives, and pharmaceutical compositions containing the same are provided.The compounds of the above formula have the action to reduce the blood glucose level and, therefore, are useful as medicines.
摘要翻译：下式的苯甲酰胺衍生物：其中R1是氢原子，甲基或甲氧基; R2是具有2-8个碳原子的直链或支链烷基，取代的苯基或-NHR4基，R4是氢原子，直链或支链或环状烷基具有1〜 6个碳原子，或在核上可以具有取代基的苯基; R3是氢原子或一个或两个具有1至4个碳原子的烷基，n是0或1，提供这些衍生物的制备方法和含有它们的药物组合物。上述化合物具有降低血糖水平的作用，因此可用作药物。

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