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1. 发明申请

WO1997003965A1 INDOLE DERIVATIVES 审中-公开
标题翻译： INDOLE DORIVATIVES
公开(公告)号：WO1997003965A1
公开(公告)日：1997-02-06
申请号：PCT/JP1996001980
申请日：1996-07-16
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： KYOWA HAKKO KOGYO CO., LTD. , MACHII, Daisuke , TAKAI, Haruki , SUZUKI, Koji , KOSAKA, Nobuo , SATO, Soichiro
IPC分类号： C07D209/42
CPC分类号： C07D209/42
摘要： Indole derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, wherein R represents hydrogen, lower alkyl, hydroxy, lower alkoxy, halogeno, (a): -O-(CH2)n-OR or (b), R represents hydrogen, lower alkyl or halogeno; R represents hydrogen, lower alkyl or (c) and R represents hydroxy, lower alkoxy, optionally substituted aryloxy or -NR R , provided that R represents -NR R when R is hydrogen or lower alkyl.
摘要翻译：通式（I）表示的吲哚衍生物或其药学上可接受的盐，其中R 1表示氢，低级烷基，羟基，低级烷氧基，卤代，（a）：-O-（CH 2）n -OR 5或（b）中，R 2表示氢，低级烷基或卤素; R 3表示氢，低级烷基或（c），R 4表示羟基，低级烷氧基，任选取代的芳氧基或-NR 10 R 11，条件是R 4表示-NR 10，当R 3为氢或低级烷基时，R 11为。

2. 发明申请

WO1997003963A1 INDOLE DERIVATIVES 审中-公开
标题翻译： INDOLE DORIVATIVES
公开(公告)号：WO1997003963A1
公开(公告)日：1997-02-06
申请号：PCT/JP1996001981
申请日：1996-07-16
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： KYOWA HAKKO KOGYO CO., LTD. , MACHII, Daisuke , TAKAI, Haruki , SUZUKI, Koji , KOSAKA, Nobuo , SATO, Soichiro
IPC分类号： C07D209/30
CPC分类号： C07D403/12 , C07D209/30
摘要： Indole derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, wherein R and R are the same or different and each represents hydrogen, lower alkyl, hydroxy, lower alkoxy, halogeno, (a): -O-(CH2)n-OR or (b), R represents hydrogen, lower alkyl or (c) and R represents hydroxy, lower alkoxy, optionally substituted aryloxy or -NR R .
摘要翻译：通式（I）表示的吲哚衍生物或其药理学上可接受的盐，其中R 1和R 2相同或不同，各自代表氢，低级烷基，羟基，低级烷氧基，卤素，（a）： - O-（CH 2）n -OR 5或（b），R 3表示氢，低级烷基或（c），R 4表示羟基，低级烷氧基，任选取代的芳氧基或-NR 10 R <11>。

3. 发明申请

WO1997003964A1 INDOLE DERIVATIVES 审中-公开
标题翻译： INDOLE DORIVATIVES
公开(公告)号：WO1997003964A1
公开(公告)日：1997-02-06
申请号：PCT/JP1996001979
申请日：1996-07-16
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： KYOWA HAKKO KOGYO CO., LTD. , MACHII, Daisuke , TAKAI, Haruki , SUZUKI, Koji , KOSAKA, Nobuo , SATO, Soichiro
IPC分类号： C07D209/42
CPC分类号： C07D231/12 , C07D209/42 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： Indole derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, wherein R and R are the same or different and each represents hydrogen, lower alkyl, -(CH2)n-OR or (a); R represents hydrogen, lower alkyl or (b); and R and R represent each hydrogen, lower alkyl, alicyclic alkyl, optionally substituted aryl, optionally substituted heterocycle, (c) or -(CH2)r-R .
摘要翻译：由通式（I）表示的吲哚衍生物或其药理学上可接受的盐，其中R 1和R 2相同或不同，各自表示氢，低级烷基， - （CH 2）n -OR 6或（一个）; R 3表示氢，低级烷基或（b）; R 4和R 5各自代表氢，低级烷基，脂环族烷基，任选取代的芳基，任选取代的杂环，（c）或 - （CH 2）r -R 13。

4. 发明授权

EP0919233B1 THERAPEUTIC AGENT FOR KIDNEY DISEASES 失效
标题翻译：治疗肾病的治疗剂
公开(公告)号：EP0919233B1
公开(公告)日：2003-06-04
申请号：EP97904570.5
申请日：1997-02-19
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： FUJIWARA, Shigeki , OKAMURA, Yuko , TAKAI, Haruki , NONAKA, Hiromi , MORIYAMA, Takahiro , YAO, Kozo , KARASAWA, Akira
IPC分类号： A61K31/505 , A61K31/535 , A61K31/54 , A61K31/55 , A61P13/12
CPC分类号： C07D401/14 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K31/55
摘要： A therapeutic agent for kidney diseases which comprises as the active ingredient a quinazoline derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, wherein R1 represents hydrogen, lower alkyl, alkenyl, aralkyl, etc.; R?2, R3, R4, and R5¿ may be the same or different and each represents hydrogen, lower alkyl, lower alkoxy, lower alkanoyl, etc.; R?6, R7, R8, and R9¿ may be the same or different and each represents hydrogen, lower alkyl, lower alkoxy, aralkyloxy, lower alkanoyloxy, etc., or adjacent two of these may be bonded to each other to thereby form methylenedioxy, etc.; R10 represents hydrogen, lower alkyl, etc.; R?11 and R12¿ may be the same or different and each represents hydrogen, lower alkyl, cycloalkyl, phenyl, aralkyl, etc., or R?11 and R12¿ may be bonded to each other to thereby form a heterocycle with the nitrogen atom; and n is 0, 1, or 2. The therapeutic agent is useful for the prevention or treatment of kidney diseases such as nephritis and diabetic nephropathy.
摘要翻译： 1。一种肾病治疗剂，其特征在于，以通式（I）表示的喹唑啉衍生物或其药理学上可接受的盐作为有效成分，其中，R 1表示氢，低级烷基，链烯基，芳烷基等。 R 2，R 3，R 4和R 5可以相同或不同，各自代表氢，低级烷基，低级烷氧基，低级烷酰基等; R 6，R 7，R 8和R 9可以相同或不同，并且各自代表氢，低级烷基，低级烷氧基，芳烷氧基，低级烷酰氧基等，或者它们中的相邻两个可以彼此键合从而形成亚甲二氧基等; R10代表氢，低级烷基等; R11和R12可以相同或不同，各自代表氢，低级烷基，环烷基，苯基，芳烷基等，或者R11和R12可以相互键合从而与氮形成杂环原子; 并且n是0,1或2.治疗剂可用于预防或治疗肾病如肾炎和糖尿病性肾病。

5. 发明授权

EP0798288B1 TRICICLIC COMPOUNDS 失效
标题翻译：三元化合物
公开(公告)号：EP0798288B1
公开(公告)日：2001-05-16
申请号：EP96935342.4
申请日：1996-10-16
申请人： KYOWA HAKKO KOGYO CO., Ltd.
发明人： YOSHIDA, Makoto , SASAKI, Shin-ichi , AONO, Shigeru , FUJIWARA, Shigeki , TAKAI, Haruki , YAMAGATA, Tsuyoshi , NAGASAHIMA, Ken , KARASAWA, Akira
IPC分类号： C07C235/16 , C07D221/06 , C07D307/93 , C07D313/12 , C07D333/78 , C07D337/12 , C07D491/044 , C07D495/04 , A61K31/35 , A61K31/38 , A61K31/435
CPC分类号： C07D491/04 , C07C235/16 , C07C2603/16 , C07C2603/18 , C07C2603/32 , C07D221/16 , C07D307/93 , C07D313/12 , C07D333/80 , C07D337/12 , C07D493/04 , C07D495/04
摘要： Triciclic compounds represented by general formula (I) which are useful as a remedy for urinary incontinence, wherein R1 represents hydrogen, etc.; and -X1-X2-X3- represents -CR?2=CR3-CR4=CR5¿- (wherein R?2, R3, R4 and R5¿ represent each hydrogen, etc.); and Y represents -CH¿2?O- etc.
摘要翻译：用作尿失禁治疗药的有用的通式（I）所示的三元系化合物，其中R1表示氢等。 -X 1 -X 2 -X 3 - 表示-CR 2 = CR 3 -CR 4 = CR 5 - （其中R 2，R 3，R 4和R 5'各自代表氢等）。 Y代表-CH 2 O-等。

6. 发明公开

EP0741132A1 INDOLE DERIVATIVE 失效
标题翻译：吲哚衍生物
公开(公告)号：EP0741132A1
公开(公告)日：1996-11-06
申请号：EP95905756.3
申请日：1995-01-11
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： MACHII, Daisuke , TAKAI, Haruki , KOSAKA, Nobuo , SEO, Hisakatsu , SUGIYAMA, Tomomi , NAKAMURA, Joji , ISHIDA, Hiroyuki , GOMI, Katsushige , SATO, Soichiro , UCHII, Masako
IPC分类号： C07D209/42 , A61K31/40
CPC分类号： C07D209/42
摘要： The present invention relates to indole derivatives represented by formula (I):
wherein R 1 and R 2 independently represent hydrogen, lower alkyl, -(CH 2 ) n -OR 6 (wherein R 6 represents hydrogen or lower alkyl, and n is an integer of 1 to 6), or
(wherein R 7 and R 8 independently represent hydrogen or lower alkyl, or R 7 and R 8 are combined together with the adjacent nitrogen atom to form a substituted or unsubstituted alicyclic heterocyclic group, and m represents an integer of 2 to 6), R 3 represents hydrogen, lower alkyl, or
(wherein R 9 and R 10 independently represent hydrogen or lower alkyl, or R 9 and R 10 are combined together with the adjacent nitrogen atom to form a substituted or unsubstituted alicyclic heterocyclic group, and p represents an integer of 2 to 6), R 4 and R 5 independently represent hydrogen, lower alkyl, alicyclic alkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted heterocyclic group, or R 4 and R 5 are combined together with the adjacent nitrogen atom to form a substituted or unsubstituted alicyclic heterocyclic group, or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及由式（I）表示的吲哚衍生物：其中R 1和R 2独立地代表氢，低级烷基， - （CH 2）n -OR 6（其中R 6）表示氢或低级烷基，n为1至6的整数）或（其中R 7和R 8独立地表示氢或低级烷基，或R 7和R 8为与相邻的氮原子一起形成取代或未取代的脂环族杂环基，m表示2〜6的整数），R 3表示氢，低级烷基或（其中R 9和R R 10和R 10独立地表示氢或低级烷基，或者R 9和R 10与相邻的氮原子一起形成取代或未取代的脂环族杂环基，p表示2〜6的整数），R R 4和R 5独立地表示氢，低级烷基，脂环族烷基，取代或未取代的芳基或取代或未取代的杂环基，或R 4和R 5 与相邻的氮原子一起形成取代或未取代的脂环族杂环基，或其药学上可接受的盐。

7. 发明公开

EP0668280A1 IMIDAZOQUINAZOLINE DERIVATIVE 失效
标题翻译：咪唑中和唑衍生物
公开(公告)号：EP0668280A1
公开(公告)日：1995-08-23
申请号：EP94925621.8
申请日：1994-09-02
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： MACHII, Daisuke , MATSUNO, Kenji , KINOSHITA, Iwao , NOMOTO, Yuji , TAKAI, Haruki , OHNO, Tetsuji , NAGASHIMA, Ken , ISHIKAWA, Tomoko , YAMADA, Koji , ICHIMURA, Michio , KASE, Kiroshi
IPC分类号： C07D487/04 , A61K31/505
CPC分类号： C07D487/04
摘要： An imidazoquinazoline derivative represented by formula (I) or a pharmacologically acceptable salt thereof, wherein R 1 andR 2 may be the same or different from each other and each represents hydrogen, lower alkyl, lower alkenyl, aryl, etc.; R 3 represents hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aryl, etc.; and X represents O or S. This compound has a potent and selective cCMP-specific PDE inhibitor activity and is useful for treating or mitigating cardiovascular diseases such as thrombosis, angina pectoris, hypertension and arteriosclerosis, asthma, and so forth.
摘要翻译：由式（I）表示的咪唑并喹唑啉衍生物或其药学上可接受的盐，其中R 1和R 2可以相同或不同，各自表示氢，低级烷基，低级烯基，芳基等; R 3表示氢，低级烷基，环烷基，低级烯基，芳基等; X表示O或S.该化合物具有有效和选择性的cCMP特异性PDE抑制剂活性，可用于治疗或缓解心血管疾病如血栓形成，心绞痛，高血压和动脉硬化，哮喘等。

8. 发明授权

EP0726267B1 QUINAZOLINE DERIVATIVES 失效
标题翻译：喹唑啉衍生物
公开(公告)号：EP0726267B1
公开(公告)日：2000-11-22
申请号：EP95929231.9
申请日：1995-08-25
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： FUJIWARA, Shigeki , OKAMURA, Yuko , TAKAI, Haruki , NONAKA, Hiromi , MORIYAMA, Takahiro , YAO, Kozo , KARASAWA, Akira
IPC分类号： C07D401/14 , A61K31/55 , A61K31/505
CPC分类号： C07D401/14
摘要： A quinazoline derivative represented by general formula (I) or a pharmacologically acceptable salt thereof (wherein R1 represents hydrogen, lower alkyl, alkenyl or aralkyl; R?2, R3, R4 and R5¿ represent each hydrogen, lower alkyl, lower alkoxy, lower alkanolyl, etc.; R?6, R7, R8 and R9¿ represent each hydrogen, lower alkyl, lower alkoxy, aralkyloxy, etc., or two adjacent members thereof are combined together to represent methylenedioxy, etc; R10 represents hydrogen, lower alkyl, etc.; R?11 and R12¿ either represent each hydrogen, lower alkyl, cycloalkyl, phenyl or aralkyl, or are combined together with the nitrogen atom to which they are bonded to represent a heterocyclic group; and n represents 0, 1 or 2). The compound has the effect of inhibiting adenosine incorporation and is useful for protecting cardiac muscles and preventing or treating inflammations such as podedema.
摘要翻译：通式（I）表示的喹唑啉衍生物或其药理学上可接受的盐（式中，R1表示氢，低级烷基，链烯基或芳烷基，R2，R3，R4和R5分别表示氢，低级烷基，低级烷氧基，低级烷氧基等; R 6，R 7，R 8和R 9代表氢，低级烷基，低级烷氧基，芳烷氧基等，或其相邻的两个成员结合在一起代表亚甲二氧基等; R 10代表氢，低级烷基等; R 11和R 12或者各自代表氢，低级烷基，环烷基，苯基或芳烷基，或者与它们所连接的氮原子一起代表杂环基;和n代表0,1或1。 2）。该化合物具有抑制腺苷掺入的作用，并且可用于保护心肌和预防或治疗如podedema等炎症。

9. 发明公开

EP0979821A1 TRICYCLIC COMPOUNDS 失效
标题翻译：三环化合物
公开(公告)号：EP0979821A1
公开(公告)日：2000-02-16
申请号：EP98914022.3
申请日：1998-04-15
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： YOSHIDA, Makoto , SEISHI, Takashi , AONO, Shigeru , TAKAI, Haruki , SUZUKI, Koji , YAMAGATA, Tsuyoshi , ATSUKI, Kaoru , KARASAWA, Akira , KUMAZAWA, Toshiaki
IPC分类号： C07D313/12 , C07D333/06 , C07D333/12 , C07D495/04 , A61K31/335 , A61K31/38 , A61K31/435
CPC分类号： C07D495/04 , C07D313/12 , C07D337/12
摘要： The present invention provides tricyclic compounds which are useful for the treatment of pollakiuria and urinary incontinence and which are represented by general formula (I):
(wherein R 1 represents hydrogen, substituted or unsubstituted lower alkyl, etc.; X 1 -X 2 -X 3 represents CR 5 =CR 6 -CR 7 =CR 8 (wherein R 5 , R 6 , R 7 and R 8 , which may be the same or different, each represents hydrogen, substituted or unsubstituted lower alkyl, hydroxy, substituted or unsubstituted lower alkoxy, etc.), N(O)m=CR 5 -CR 6 -CR 7 (wherein R 5 , R 6 and R 7 have the same significances as defined above, and m represents 0 or 1), S-CR 7 =CR 8 (wherein R 7 and R 8 have the same significances as defined above), etc.;
and when R 2 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, a substituted or unsubstituted N-substituted heterocyclic group,
(wherein n is 0 or 1; R 3 and R 4 , which may be the same or different, each represents hydrogen, substituted or unsubstituted lower alkyl, trifluoromethyl, etc., or R 3 and R 4 may be combined together to form cyclic alkyl; and Q represents hydroxy, halogen, etc.), etc., Y represents -CH 2 SO 2 -, -SCH 2 -, -SOCH 2 -, -SO 2 CH 2 -, etc.) and pharmaceutically acceptable salts thereof.
摘要翻译：本发明提供了可用于治疗尿频和尿失禁的三环化合物，其由通式（I）表示：（其中R 1表示氢，取代或未取代的低级烷基等; X 1 -X 2 -X 3表示CR 5 （其中R5，R6，R7和R8可以相同或不同，各自代表氢，取代的或未取代的低级烷基，羟基，取代的或未取代的低级烷氧基等），N（O）= CR6- m = CR 5 -CR 6 -CR 7（其中R 5，R 6和R 7具有与上述定义相同的含义，并且m表示0或1），S-CR 7 = CR 8（其中R 7和R 8具有与上述定义相同的含义）等 ;当R2代表氢时，取代或未取代的低级烷基，取代或未取代的低级烷氧基，取代或未取代的N-取代的杂环基，（其中n是0或1; R3和R4可以相同或不同，各自代表氢，取代或未取代的低级烷基，t 三氟甲基等，或者R3和R4可以结合在一起形成环烷基; Q表示羟基，卤素等）等，Y表示-CH 2 SO 2 - ， - SCH 2 - ， - SOCH 2 - ，-SO 2 CH 2 - 等）及其药学上可接受的盐。

10. 发明公开

EP0798288A1 TRICICLIC COMPOUNDS 失效
标题翻译：三环化合物
公开(公告)号：EP0798288A1
公开(公告)日：1997-10-01
申请号：EP96935342.4
申请日：1996-10-16
申请人： Kyowa Hakko Kogyo Co., Ltd.
发明人： YOSHIDA, Makoto , SASAKI, Shin-ichi , AONO, Shigeru , FUJIWARA, Shigeki , TAKAI, Haruki , YAMAGATA, Tsuyoshi , NAGASAHIMA, Ken , KARASAWA, Akira
IPC分类号： C07C235/16 , C07D221/06 , C07D307/93 , C07D313/12 , C07D333/78 , C07D337/12 , C07D491/044 , C07D495/04 , A61K31/35 , A61K31/38 , A61K31/435
CPC分类号： C07D491/04 , C07C235/16 , C07C2603/16 , C07C2603/18 , C07C2603/32 , C07D221/16 , C07D307/93 , C07D313/12 , C07D333/80 , C07D337/12 , C07D493/04 , C07D495/04
摘要： The present invention relates to tricyclic compounds represented by general formula (I) which are useful as therapeutic agents for urinary incontinence:
wherein R 1 represents hydrogen and the like; -X 1 -X 2 -X 3 -represents -CR 2 =CR 3 -CR 4 =CR 5 - (wherein R 2 , R 3 , R 4 , and R 5 represent hydrogen and the like) and the like; and Y represents -CH 2 O- and the like.

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