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公开(公告)号:US5661147A
公开(公告)日:1997-08-26
申请号:US424274
申请日:1995-04-26
申请人: Daisuke Machii , Kenji Matsuno , Iwao Kinoshita , Yuji Nomoto , Haruki Takai , Tetsuji Ohno , Ken Nagashima , Tomoko Ishikawa , Koji Yamada , Michio Ichimura , Hiroshi Kase
发明人: Daisuke Machii , Kenji Matsuno , Iwao Kinoshita , Yuji Nomoto , Haruki Takai , Tetsuji Ohno , Ken Nagashima , Tomoko Ishikawa , Koji Yamada , Michio Ichimura , Hiroshi Kase
IPC分类号: C07D487/04 , C07D417/04 , A61K31/505 , C07D243/08 , C07D413/04
CPC分类号: C07D487/04
摘要: The present invention relates to imidazoquinazoline derivatives represented by the general formula (I): ##STR1## or pharmacologically acceptable salts thereof. The compounds of the present invention have strong and selective cGMP-specific PDE inhibitory activity and are useful for treating or ameliorating cardiovascular diseases such as thrombosis, angina pectoris, hypertension, arterial sclerosis and the like, as well as asthma and the like.
摘要翻译: PCT No.PCT / JP94 / 01456 Sec。 371日期1995年04月26日 102(e)日期1995年4月26日PCT 1994年9月2日PCT PCT。 出版物WO95 / 06648 日期:1995年3月9日本发明涉及由通式(I)表示的咪唑并喹唑啉衍生物或其药理学上可接受的盐。 本发明的化合物具有强的选择性cGMP特异性PDE抑制活性,可用于治疗或改善心血管疾病如血栓形成,心绞痛,高血压,动脉硬化等,以及哮喘等。
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公开(公告)号:US5698560A
公开(公告)日:1997-12-16
申请号:US727598
申请日:1996-10-23
申请人: Yasuo Onoda , Shin-ichi Sasaki , Daisuke Machii , Haruki Takai , Tetsuji Ohno , Koji Yamada , Michio Ichimura , Hiroshi Kase
发明人: Yasuo Onoda , Shin-ichi Sasaki , Daisuke Machii , Haruki Takai , Tetsuji Ohno , Koji Yamada , Michio Ichimura , Hiroshi Kase
IPC分类号: C07D487/04 , A61K31/505 , A61K31/535 , C07D417/02 , C07D487/02
CPC分类号: C07D487/04
摘要: The present invention relates to imidazoquinazoline derivatives represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, cycloalkyl, lower alkenyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroarylalkyl, or substituted or unsubstituted heteroaryl, R.sup.2 and R.sup.3 represent independently hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroarylalkyl, or substituted or unsubstituted heteroaryl, or R.sup.2 and R.sup.3 are combined to represent a heterocyclic group containing a nitrogen atom, R.sup.4 represents hydrogen or substituted or unsubstituted lower alkyl, X represents O or S, Y represents a single bond or O, n represents 0, 1, 2, or 3, and pharmaceutically acceptable salts thereof.
摘要翻译: PCT No.PCT / JP96 / 00497 Sec。 371日期:1996年10月23日 102(e)日期1996年10月23日PCT 1996年3月1日PCT公布。 第WO96 / 26940号公报 日本1996年9月6日本发明涉及由式(I)表示的咪唑并喹唑啉衍生物:其中R1表示氢,取代或未取代的低级烷基,环烷基,低级烯基,取代或未取代的芳烷基,取代或未取代的芳基 取代或未取代的芳基,取代或未取代的杂芳基,或取代或未取代的杂芳基,或者取代或未取代的杂芳基,或者取代或未取代的杂芳基,或R 2和R 3 合并表示含有氮原子的杂环基,R4表示氢或取代或未取代的低级烷基,X表示O或S,Y表示单键或O,n表示0,1,2或3,以及药学上可接受的 的盐。
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公开(公告)号:US6127541A
公开(公告)日:2000-10-03
申请号:US65061
申请日:1998-04-27
申请人: Yasuo Onoda , Yuji Nomoto , Tetsuji Ohno , Koji Yamada , Michio Ichimura
发明人: Yasuo Onoda , Yuji Nomoto , Tetsuji Ohno , Koji Yamada , Michio Ichimura
IPC分类号: C07D487/04 , C07D487/02
CPC分类号: C07D487/04
摘要: Imidazoquinoline derivatives of the formula ##STR1## (wherein X may be O or S) provide selective cyclic guanosine 3',5' monophosphate (cGMP)--specific phosphodiesterase (PDE) inhibitory activity. The compounds are useful for treating or ameliorating cardiovascular disease such as thrombosis, angina pectoris, hypertension, heart failure and arterial sclerosis, as well as asthma, impotence and the like.
摘要翻译: PCT No.PCT / JP97 / 03023 Sec。 371日期:1998年4月27日 102(e)日期1998年4月27日PCT 1997年8月29日PCT公布。 出版物WO98 / 08848 日期:1998年3月5日式(其中X可以是O或S)的咪唑并喹啉衍生物提供选择性环状鸟苷3',5'单磷酸(cGMP)特异性磷酸二酯酶(PDE)抑制活性。 该化合物可用于治疗或改善心血管疾病如血栓形成,心绞痛,高血压,心力衰竭和动脉硬化,以及哮喘,阳ence等。
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公开(公告)号:US5478840A
公开(公告)日:1995-12-26
申请号:US294978
申请日:1994-08-24
申请人: Etsuo Ohshima , Fumihiko Kanai , Hideyuki Sato , Hiroyuki Obase , Toshiaki Kumazawa , Shiho Takahara , Tetsuji Ohno , Tomoko Ishikawa , Koji Yamada
发明人: Etsuo Ohshima , Fumihiko Kanai , Hideyuki Sato , Hiroyuki Obase , Toshiaki Kumazawa , Shiho Takahara , Tetsuji Ohno , Tomoko Ishikawa , Koji Yamada
IPC分类号: C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D471/04 , C07D521/00 , A61K31/44
CPC分类号: C07D249/08 , C07D231/12 , C07D233/56 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D471/04
摘要: A tricyclic compound represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, halogen or lower alkyl; A represents cyano, carboxyl, tetrazolyl, cyano-substituted phenyl, carboxyl-substituted phenyl or tetrazolyl-substituted phenyl; V represents --(CH.sub.2).sub.m --(wherein m is an integer of 0 to 2); W represents ##STR2## (wherein R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, halogen, lower alkyl, cycloalkyl, halogenated lower alkyl, hydroxy, lower alkoxy, amino, lower alkylamino, carboxyl or lower alkoxycarbonyl; and Q.sup.1 --Q.sup.2 --Q.sup.3 --Q.sup.4 represents N.dbd.CH--CH.dbd.CH; X.sup.1 --X.sup.2 --X.sup.3 represents CH.dbd.CH--CH.dbd.CH, S--CH.dbd.CH or CH.dbd.CH--S; Y represents a single bond, CH.sub.2, O, S, CH.sub.2 O, OCH.sub.2, CH.sub.2 S, SCH.sub.2, CH.sub.2 CH.sub.2 or CH.dbd.CH; and Z.sup.1 --Z.sup.2 represents C.dbd.CH, CH--CH.sub.2 or CH--CH(COOH)-- or a pharmaceutically acceptable salt thereof. The compound of the present invention exhibits antagonism to angiotensin II receptors.
摘要翻译: 由下式(I)表示的三环化合物:其中R 1表示氢,卤素或低级烷基; A代表氰基,羧基,四唑基,氰基取代的苯基,羧基取代的苯基或四唑基取代的苯基; V表示 - (CH 2)m - (其中m为0〜2的整数); W表示
(其中R2,R3和R4独立地表示氢,卤素,低级烷基,环烷基,卤代低级烷基,羟基,低级烷氧基,氨基,低级烷基氨基,羧基或低级烷氧基羰基;以及Q1-Q2-Q3-Q4 表示N = CH-CH = CH; X 1 -X 2 -X 3表示CH = CH-CH = CH,S-CH = CH或CH = CH-S; Y表示单键,CH 2,O,S,CH 2 O,OCH 2 ,CH2S,SCH2,CH2CH2或CH = CH; Z1-Z2表示C = CH,CH-CH2或CH-CH(COOH) - 或其药学上可接受的盐。本发明化合物显示对血管紧张素II受体的拮抗作用。 -
公开(公告)号:US5607955A
公开(公告)日:1997-03-04
申请号:US431425
申请日:1995-05-01
申请人: Etsuo Ohshima , Fumihiko Kanai , Hideyuki Sato , Hiroyuki Obase , Toshiaki Kumazawa , Shiho Takahara , Tetsuji Ohno , Tomoko Ishikawa , Koji Yamada
发明人: Etsuo Ohshima , Fumihiko Kanai , Hideyuki Sato , Hiroyuki Obase , Toshiaki Kumazawa , Shiho Takahara , Tetsuji Ohno , Tomoko Ishikawa , Koji Yamada
IPC分类号: C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D471/04 , C07D521/00 , A61K31/41 , A61K31/415 , C07D233/54 , C07D235/04 , C07D257/04
CPC分类号: C07D249/08 , C07D231/12 , C07D233/56 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D471/04
摘要: A tricyclic compound represented by the following formula (I): ##STR1## exhibits antagonism to angiotensin II receptors.
摘要翻译: 由下式(I)表示的三环化合物:显示对血管紧张素II受体的拮抗作用。
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公开(公告)号:US5378701A
公开(公告)日:1995-01-03
申请号:US65916
申请日:1993-05-25
申请人: Etsuo Ohshima , Fumihiko Kanai , Hideyuki Sato , Hiroyuki Obase , Toshiaki Kumazawa , Shiho Takahara , Tetsuji Ohno , Tomoko Ishikawa , Koji Yamada
发明人: Etsuo Ohshima , Fumihiko Kanai , Hideyuki Sato , Hiroyuki Obase , Toshiaki Kumazawa , Shiho Takahara , Tetsuji Ohno , Tomoko Ishikawa , Koji Yamada
IPC分类号: C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D471/04 , C07D521/00 , A61K31/55 , C07D223/16 , C07D223/22
CPC分类号: C07D249/08 , C07D231/12 , C07D233/56 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D471/04
摘要: A tricyclic compound represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, halogen or lower alkyl; A represents cyano, carboxyl, tetrazolyl, cyano-substituted phenyl, carboxyl-substituted phenyl or tetrazolyl-substituted phenyl; V represents --(CH.sub.2).sub.m -- wherein m is an integer of 0 to 2; W represents ##STR2## and Q.sup.1 --Q.sup.2 --Q.sup.3 --Q.sup.4 represents N.dbd.CH--CH.dbd.CH, CH.dbd.CH--CH.dbd.CH or CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2, ##STR3## and Q represents N or CH; X.sup.1 --X.sup.2 --X.sup.3 represents CH.dbd.CH--CH.dbd.CH, S--CH.dbd.CH or CH.dbd.CH--S; Y represents CH.sub.2 CH.sub.2 ; and Z.sup.1 --Z.sup.2 represents N--(CH.sub.2).sub.n -- wherein n is an integer of 1 to 3 or a pharmaceutically acceptable salt thereof.
摘要翻译: 由下式(I)表示的三环化合物:其中R 1表示氢,卤素或低级烷基; A代表氰基,羧基,四唑基,氰基取代的苯基,羧基取代的苯基或四唑基取代的苯基; V表示 - (CH 2)m - ,其中m是0至2的整数; W表示
,Q1-Q2-Q3-Q4表示N = CH-CH = CH,CH = CH-CH = CH或CH2-CH2-CH2-CH2, N或CH; X1-X2-X3表示CH = CH-CH = CH,S-CH = CH或CH = CH-S; Y表示CH 2 CH 2; Z1-Z2表示N-(CH2)n-,其中n为1〜3的整数或其药学上可接受的盐。 -
公开(公告)号:US20070185168A1
公开(公告)日:2007-08-09
申请号:US11547810
申请日:2005-04-07
申请人: Haruki Takai , Shunji Kunori , Shiro Shirakura , Katsumi Shinoda , Atsuko Mizutani , Koji Yamada , Shinichiro Toki , Tomoyuki Nishikawa
发明人: Haruki Takai , Shunji Kunori , Shiro Shirakura , Katsumi Shinoda , Atsuko Mizutani , Koji Yamada , Shinichiro Toki , Tomoyuki Nishikawa
IPC分类号: A61K31/4439
CPC分类号: C07D409/14
摘要: For example, a piperidine derivative represented by following formula (I) (wherein, —C(═O)-Z- represents —C(═O)—CH2—, —C(═O)—C(CH3)2—, —C(═O)—NH—, —C(═O)—O—, —C(═O)—S—, —C(═O)—CH2CH2—, —C(═O)—CH═CH—, —C(═O)—CH2O—, —C(═O)—CH2S—, —C(═O)—CH2CH2CH2— or —C(═O)—NR8CH2—; R1 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R2 represents a hydrogen atom or hydroxy; R3 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R5 represents a hydrogen atom, hydroxy, or the like; R6 represents a hydrogen atom, hydroxy, substituted or unsubstituted lower alkyl, or the like, etc.; R7 represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like; n and k each independently represents an integer of 0 to 2; and ---- represents a single bond, or a double bond together with R4, where in case ---- is a single bond, R4 represents a hydrogen atom, hydroxy, or the like) or a pharmaceutically acceptable salt thereof and the like having an antagonistic activity for a glutamic acid receptor (NR2B/NMDA receptor) of an N-methyl-D-aspartic acid (NMDA) type containing an NR2B subunit are provided.
摘要翻译: 例如,由下式(I)表示的哌啶衍生物(其中,-C(-O)-Z-表示-C(-O)-CH 2 - , - C( - -C(= O)-NH-, - C(-O)-O - , - C(-O) - S - , - C(-O)-CH 2 CH 2 - , - C(-O)-CH-CH - , - C(-O)-CH O - , - C(-O)-CH 2 S - , - C(-O)-CH 2 CH 2 2-CH 2 - 或-C( - )-NR 8 CH 2 - ; R 1 - SUP>表示氢原子,取代或未取代的低级烷基等; R 2表示氢原子或羟基; R 3表示氢原子,取代或未取代的 低级烷基等; R 5表示氢原子,羟基等; R 6表示氢原子,羟基,取代或未取代的低级烷基,或 R 7表示氢原子,卤素,取代或未取代的低级烷基等; n和k各自独立地表示0〜2的整数;< U STYLE = “ SINGLE“> ----表示单键,或与R 4连接的双键,其中如果是单键,则R” 对于N-甲基-D-葡萄糖酸的谷氨酸受体(NR2B / NMDA受体)具有拮抗作用的氨基酸或其药学上可接受的盐等) 提供了含有NR2B亚基的天冬氨酸(NMDA)型。
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公开(公告)号:US5631222A
公开(公告)日:1997-05-20
申请号:US382013
申请日:1995-02-10
申请人: Kenji Shibata , Toshiyuki Suzawa , Motoo Yamasaki , Takeo Tanaka , Eiji Tsukuda , Koji Yamada , Tetsuji Ohno
发明人: Kenji Shibata , Toshiyuki Suzawa , Motoo Yamasaki , Takeo Tanaka , Eiji Tsukuda , Koji Yamada , Tetsuji Ohno
IPC分类号: A61K38/00 , C07K7/06 , C07K14/575 , C07K5/12 , C07K7/08
CPC分类号: C07K7/06 , C07K14/57536 , A61K38/00
摘要: Disclosed is a peptide compound represented by the following formula (I):R.sup.1 -R.sup.2 -R.sup.3 -R.sup.4 -R.sup.5 -R.sup.6 -R.sup.7 -R.sup.8 -R.sup.9 -R.sup.10 -R.sup.11 -R.sup.12 -Phe-R.sup.14 -R.sup.15 -R.sup.16 -R.sup.17 -R.sup.18 -Ile-R.sup.20 -Z SEQ. ID NO. 64, (I)wherein R.sup.1-12, R.sup.14-18, and R.sup.20 are as defined in the specification.
摘要翻译: PCT No.PCT / JP94 / 01011 Sec。 371日期1995年2月10日 102(e)1995年2月10日PCT PCT 1994年6月23日PCT公布。 第WO95 / 00546号公报 日期:1995年5月1日公开了由下式(I)表示的肽化合物:R1-R2-R3-R4-R5-R6-R7-R8-R9-R10-R11-R12-Phe-R14-R15-R16- R17-R18-Ile-R20-Z SEQ。 证件号码。 64,(I)其中R1-12,R14-18和R20如说明书中所定义。
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公开(公告)号:US5223637A
公开(公告)日:1993-06-29
申请号:US889388
申请日:1992-05-28
申请人: Kazutoshi Kuroda , Hiroshi Kase , Katsuhiko Ando , Isao Kawamoto , Toru Yasuzawa , Hiroshi Sano , Joji Goto , Koji Yamada
发明人: Kazutoshi Kuroda , Hiroshi Kase , Katsuhiko Ando , Isao Kawamoto , Toru Yasuzawa , Hiroshi Sano , Joji Goto , Koji Yamada
IPC分类号: C07C323/20 , C07C327/26 , C12P7/00
CPC分类号: C07C323/20 , C07C327/26 , C12P7/00
摘要: KS-506a, KS-506x and KS-506g having an activity to inhibit cyclic nucleotide phosphodiesterase and KS-506m and KS-506h having an activity to inhibit histamine release are produced by culturing a microorganism belonging to the genus Mortierella.
摘要翻译: 通过培养属于被孢霉属属的微生物来产生具有抑制环核苷酸磷酸二酯酶的活性的KS-506a,KS-506x和KS-506g以及具有抑制组胺释放活性的KS-506m和KS-506h。
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10.
公开(公告)号:US4990693A
公开(公告)日:1991-02-05
申请号:US465892
申请日:1990-01-16
申请人: Satoshi Nakanishi , Koji Yamada , Katsuhiko Ando , Isao Kawamoto , Toru Yasuzawa , Hiroshi Sano , Noriaki Hirayama , Hiroshi Kase , Joji Goto , Etsuyo Shimizu
发明人: Satoshi Nakanishi , Koji Yamada , Katsuhiko Ando , Isao Kawamoto , Toru Yasuzawa , Hiroshi Sano , Noriaki Hirayama , Hiroshi Kase , Joji Goto , Etsuyo Shimizu
CPC分类号: C12R1/645 , C07C35/48 , C07C45/58 , C07C47/46 , C07D303/48 , C12P17/02 , C12P7/02 , C12P7/24
摘要: Novel physiologically active substances KS-504a, KS-504b and KS-504d having a vasodilative activity and a novel physiologically active substance KS-504e having an activity to inhibit histamine secretion are produced by culturing a microorganism of the genus Mollisia.
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