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1.发明公开
公开(公告)号：EP0715624A1
公开(公告)日：1996-06-12
申请号：EP94924368.0
申请日：1994-08-25
发明人： SEMPLE, Graeme , RYDER, Hamish , SZELKE, Michael , SATOH, Masato , OHTA, Mitsuaki , MIYATA, Keiji , NISHIDA, Akito , ISHII, Masato
CPC分类号： C07D401/04 , C07D403/04 , C07D417/04
摘要： A benzodiazepine derivative of formula (I), or a pharmaceutically acceptable salt thereof, wherein: (a) R4 is an alkyl, cycloalkyl or aryl group; (b) R10 is chosen from halo, OH, CH¿3?, OCH3, NR?11R12, NO¿2, NHCHO, CO2H and CN, and R?11 and R12¿ are independently selected from H and alkyl (C¿1?-C5) or together NR?11R12¿ form a cyclic structure (II), wherein a is 1-6; and (c) R2 is an aromatic 5- or 6-membered, substituted or unsubstituted heterocycle containing at least two heteroatoms of which at least one is nitrogen. These compounds are gastrin and/or CCK-B receptor antagonists.
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公开(公告)号：EP0628033B1
公开(公告)日：2003-07-23
申请号：EP93905480.5
申请日：1993-02-26
发明人： RYDER, Hamish , SEMPLE, Graeme , KENDRICK, David, Alan , SZELKE, Michael , SATOH, Masato , OHTA, Mitsuaki , MIYATA, Keiji , NISHIDA, Akito
IPC分类号： C07D243/24 , C07D401/12 , C07D403/06 , C07D405/06
CPC分类号： C07D401/04 , C07D243/24 , C07D403/06
摘要： A benzodiazepine derivative of formula (I), or a pharmaceutically acceptable salt thereof, wherein (a) R1 is -CH¿2?CHOH(CH2)aR?4¿ or a ketone group -CH¿2?CO(CH2)aR?5¿ in which a is 0 or 1 and R?4 and R5¿ are selected from alkyl and cycloalkyl groups and saturated heterocyclic groups optionally substituted at a hetero-atom; (b) R?2 and R3¿ are independently selected from aromatic carbocyclic and heterocylic residues; and (c) W and X are selected independently from halogen and hydrogen atoms and alkyl and alkoxy groups. These compounds are gastrin and/or CCK-B receptor antagonists.
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公开(公告)号：EP0628033A1
公开(公告)日：1994-12-14
申请号：EP93905480.0
申请日：1993-02-26
发明人： RYDER, Hamish , SEMPLE, Graeme , KENDRICK, David, Alan , SZELKE, Michael , SATOH, Masato , OHTA, Mitsuaki , MIYATA, Keiji , NISHIDA, Akito
CPC分类号： C07D401/04 , C07D243/24 , C07D403/06
摘要： L'invention concerne un dérivé de benzodiazépine de la formule (I) ou un sel pharmaceutiquement acceptable de celui-ci, dans laquelle: (a) R1 représente -CH2CHOH(CH2)aR4 ou un groupe cétone -CH2CO(CH2)aR5 dans lequel a est 0 ou 1 et R4 et R5 sont sélectionnés parmi des groupes alkyle et cycloalkyle, ainsi que parmi des groupes hétérocycliques saturés éventuellement substitués au niveau d'un hétéro-atome; (b) R2 et R3 sont indépendamment sélectionnés parmi des résidus carbocycliques et hétérocycliques aromatiques; et (c) W et X sont indépendamment sélectionnés parmi halogène et des atomes d'hydrogène, et parmi des groupes alkyle et alcoxy. Ces composés sont des antagonistes récepteurs de gastrine et/ou de CCK-B.
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公开(公告)号：EP0647632A1
公开(公告)日：1995-04-12
申请号：EP93913562.0
申请日：1993-06-22
发明人： SATOH, Masato , OKAMOTO, Yoshinori , KOSHIO, Hiroyuki , NISHIDA, Akito , MIYATA, Keiji , OHTA, Mitsuaki , RYDER, Hamish , KENDRICK, David, A. , SEMPLE, Graeme , SZELKE, Michael
IPC分类号： C07D243/24 , A61K31/55 , C07D403/12 , C07D401/12 , C07D401/04
CPC分类号： C07D401/04 , C07D243/24 , C07D401/12 , C07D403/12
摘要： A novel benzodiazepine derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof. These compounds are useful as medicines, in particular, for treating and preventing diseases in which CCK-B receptor and gastrin receptor participate, because they have CCK-B receptor antagonism, gastrin receptor antagonism and the effect of inhibiting gastric juice secretion.
摘要翻译：
由通式（I）表示的新型苯二氮卓衍生物或其药学上可接受的盐。 这些化合物可用作药物，特别是用于治疗和预防CCK-B受体和胃泌素受体参与的疾病，因为它们具有CCK-B受体拮抗作用，胃泌素受体拮抗作用和抑制胃液分泌的作用。 -
5.发明授权PROCESS FOR THE PREPARATION OF BENZODIAZEPINE COMPOUNDS USEFUL AS ANTAGONISTS OF CCK OR OF GASTRINE 失效用于生产苯二氮类化合物的AS CCK或胃泌素拮抗剂
公开(公告)号：EP0715624B1
公开(公告)日：1998-04-08
申请号：EP94924368.7
申请日：1994-08-25
发明人： SEMPLE, Graeme , RYDER, Hamish , SZELKE, Michael , SATOH, Masato , OHTA, Mitsuaki , MIYATA, Keiji , NISHIDA, Akito , ISHII, Masato
IPC分类号： C07D243/14 , C07D403/04 , C07D417/04 , A61K31/55
CPC分类号： C07D401/04 , C07D403/04 , C07D417/04
摘要： A benzodiazepine derivative of formula (I), or a pharmaceutically acceptable salt thereof, wherein: (a) R4 is an alkyl, cycloalkyl or aryl group; (b) R10 is chosen from halo, OH, CH¿3?, OCH3, NR?11R12, NO¿2, NHCHO, CO2H and CN, and R?11 and R12¿ are independently selected from H and alkyl (C¿1?-C5) or together NR?11R12¿ form a cyclic structure (II), wherein a is 1-6; and (c) R2 is an aromatic 5- or 6-membered, substituted or unsubstituted heterocycle containing at least two heteroatoms of which at least one is nitrogen. These compounds are gastrin and/or CCK-B receptor antagonists.
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公开(公告)号：EP0591529A1
公开(公告)日：1994-04-13
申请号：EP92900534.6
申请日：1991-12-17
发明人： SATOH, Masato , KONDOH, Yutaka , OKAMOTO, Yoshinori , NISHIDA, Akito , HONDA, Kazuo , SAITO, Masayuki
IPC分类号： C07D243/24 , C07D243/26 , A61K31/55 , C07D401/06 , C07D409/06 , C07D403/06
CPC分类号： C07D401/06 , B65D83/0847 , B65H35/10 , B65H2701/11231 , C07D243/24 , C07D403/04 , C07D409/06
摘要： A novel benzodiazepine derivative represented by general formula (I), a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof, and a process for producing the same. In formula (I), R¹ represents optionally substituted aryl, five-membered monocyclic group, six-membered monocyclic group or aromatic heterocyclic group comprising five-membered and six-membered rings; and R² represents optionally substituted aryl. The compound (I) has a CCK-B receptor antagonism and an action of inhibiting pentagastrin-stimulated gastric secretion and hence is useful in treating and preventing the diseases wherein a CCK-B receptor and a gastrin receptor participate.
摘要翻译： 一种由通式（I）表示的新型苯并二氮杂衍生物，其药学上可接受的盐，其药物组合物及其制备方法。 在式（I）中，R 1表示任选取代的芳基，五元单环基，六元单环基或含有五元和六元环的芳族杂环基; 且R 2表示任选取代的芳基。 化合物（I）具有CCK-B受体拮抗作用和抑制五肽胃泌素刺激的胃分泌的作用，因此可用于治疗和预防CCK-B受体和胃泌素受体参与的疾病。
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