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1. 发明授权

US5539119A Indole derivatives 失效
标题翻译：吲哚衍生物
公开(公告)号：US5539119A
公开(公告)日：1996-07-23
申请号：US36521
申请日：1993-03-24
申请人： Hiroshi Nagase , Akira Mizusuna , Yoshihiro Onoda , Koji Kawai , Shu Matsumoto , Takashi Endo
发明人： Hiroshi Nagase , Akira Mizusuna , Yoshihiro Onoda , Koji Kawai , Shu Matsumoto , Takashi Endo
IPC分类号： C07D217/06 , C07D217/24 , C07D471/04 , C07D491/056 , C07D217/14
CPC分类号： C07D471/04 , C07D217/06 , C07D217/24 , Y10S514/885
摘要： This invention is directed to a indole derivative represented by the general formula (1) ##STR1## wherein R.sub.1 stands for alkyl of 1 to 5 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms, cycloalkenylalkyl of 5 to 7 carbon atoms, aralkyl of 7 to 14 carbon atoms, trans-alkenyl of 4 or 5 carbon atoms, allyl, furanyl-2-ylalkyl of 1 to 5 carbon atoms, thienyl-2-ylalkyl of 1 to 5 carbon atoms, vinyloxycarbonyl, trichloroethoxycarbonyl, benzyloxycarbonyl, alkanoyl of 1 to 5 carbon atoms, aralkylcarbonyl of 7 to 14 carbon atoms, 2-furoyl, thiophene-2-carbonyl, cycloalkylcarbonyl of 4 to 7 carbon atoms, alkenylcarbonyl of 3 to 8 carbon atoms, or anisoyl, providing that said general formula (1) embraces a (+) form, a (-) form, and a (.+-.) form, or a pharmacologically acceptable salt thereof and to an immunorepressing agent having as an active component thereof the indole derivative or the pharmacologically acceptable salt thereof.
摘要翻译：本发明涉及由通式（1）表示的吲哚衍生物，其中R1表示1至5个碳原子的烷基，4至7个碳原子的环烷基烷基，5至7个碳原子的环烯基烷基， 7至14个碳原子的芳烷基，4或5个碳原子的反式链烯基，1至5个碳原子的烯丙基，呋喃基-2-基烷基，1至5个碳原子的噻吩基-2-基烷基，乙烯氧基羰基，三氯乙氧羰基，苄氧羰基，具有1至5个碳原子的烷酰基，7至14个碳原子的芳烷基羰基，2-糠酰基，噻吩-2-羰基，4至7个碳原子的环烷基羰基，3至8个碳原子的链烯基羰基或茴香酰基，条件是所述通式（1）包含（+）形式，（ - ）形式和（+/-）形式或其药理学上可接受的盐，并且具有作为其活性成分的吲哚衍生物或药理学上可接受的盐的免疫抑制剂其中。

2. 发明授权

US5244904A Indole derivatives 失效
标题翻译： INDOLE DORIVATIVES
公开(公告)号：US5244904A
公开(公告)日：1993-09-14
申请号：US828889
申请日：1992-01-29
申请人： Hiroshi Nagase , Akira Mizusuna , Yoshihiro Onoda , Koji Kawai , Shu Matsumoto , Takashi Endo
发明人： Hiroshi Nagase , Akira Mizusuna , Yoshihiro Onoda , Koji Kawai , Shu Matsumoto , Takashi Endo
IPC分类号： C07D217/06 , C07D217/24 , C07D471/04 , C07D491/056
CPC分类号： C07D471/04 , C07D217/06 , C07D217/24 , Y10S514/885
摘要： This invention is directed to a indole derivative represented by the general formula (1) ##STR1## wherein R.sub.1 stands for alkyl of 1 to 5 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms, cycloalkenylalkyl of 5 to 7 carbon atoms, aralkyl of 7 to 14 carbon atoms, trans-alkenyl of 4 to 5 carbon atoms, allyl, furanyl-2-ylalkyl of 1 to 5 carbon atoms, thienyl-2-ylalkyl of 1 to 5 carbon atoms, vinyloxycarbonyl, trichloroethoxycarbonyl, benzyloxycarbonyl, alkanoyl of 1 to 5 carbon atoms, aralkylcarbonyl of 7 to 14 carbon atoms, 2-furoyl, thiophene-2-carbonyl, cycloalkylcarbonyl of 4 to 7 carbon atoms, alkenylcarbonyl of 3 to 8 carbon atoms, or anisoyl, R.sub.2 for a hydrogen atoms, alkyl of 1 to 3 carbon atoms, benzyl, or alkanoyl of 1 to 5 carbon atoms, R.sub.3 for a hydrogen atoms, a fluorine atom, a chlorine atom, a bromine atom, nitro, or alkyl of 1 to 5 carbon atoms, R.sub.4 for a hydrogen atom, alkyl of 1 to 5 carbon atoms, benzyl, or phenyl, and R.sub.5 for a hydrogen atom, hydroxy, or alkanoyloxy of 1 to 5 carbon atoms, providing that said general formula (1) embraces a (+) form, a (-) form, and a (.+-.) form, or a pharmacologically acceptable salt thereof and to an immunorepressing agent having as an active component thereof the indole derivative or the pharmacologically acceptable salt thereof.
摘要翻译： PCT No.PCT / JP91 / 00759 Sec。 371日期1992年1月29日 102（e）日期1992年1月29日PCT Filed 1991年6月5日PCT公布。 WO91 / 18901 PCT出版物日本1991年12月12日。本发明涉及由通式（1）表示的吲哚衍生物，其中R1代表1至5个碳原子的烷基，4至7个碳原子的环烷基烷基，环烯基烷基 5至7个碳原子的芳烷基，7至14个碳原子的芳烷基，4至5个碳原子的反式链烯基，1至5个碳原子的烯丙基，呋喃基-2-基烷基，1至5个碳原子的噻吩基-2-基烷基，乙氧基羰基，三氯乙氧基羰基，苄氧基羰基，1〜5个碳原子的烷酰基，7〜14个碳原子的芳烷基羰基，2-糠酰基，噻吩-2-羰基，4〜7个碳原子的环烷基羰基，3〜8个碳原子的链烯基羰基，甲氧基苯甲酰基，R2为氢原子，1〜3个碳原子的烷基，苄基或1〜5个碳原子的烷酰基，R3为氢原子，氟原子，氯原子，溴原子，硝基或烷基 1至5个碳原子，R4代表氢原子，1至5个碳原子的烷基，苄基或苯基，R5代表氢原子，羟基 y）或1至5个碳原子的烷酰氧基，条件是所述通式（1）包含（+）形式，（ - ）形式和（+/-）形式或其药理学上可接受的盐，以及作为活性成分的吲哚衍生物或其药理学上可接受的盐的免疫抑制剂。

3. 发明授权

US06337330B1 Antitussives 失效
标题翻译：镇咳药
公开(公告)号：US06337330B1
公开(公告)日：2002-01-08
申请号：US09254427
申请日：1999-05-18
申请人： Hiroshi Nagase , Koji Kawai , Akira Mizusuna , Junzo Kamei
发明人： Hiroshi Nagase , Koji Kawai , Akira Mizusuna , Junzo Kamei
IPC分类号： A61K31495
CPC分类号： C07D471/04
摘要： An antitussive agent containing an octahydroisoquinoline derivative represented by the following compound or pharmacologically acceptable acid addition salt thereof: The compounds of the present invention have the significant antitussive action, and can thus be expected as medicines which can be used for all diseases accompanied with coughs, for example, various respiratory diseases such as cold, acute bronchitis, chronic bronchitis, bronchiectasis, pneumonia, pulmonary tuberculosis, silicosis and silicotuberculosis, lung cancer, upper respiratory inflammation (pharyngitis, laryngitis, nasal catarrhalis), asthmatic bronchitis, bronchial asthma, infantile asthma, (chronic) pulmonary emphysema, pneumoconiosis, pulmonary fibrosis, silicosis, pulmonary suppuration, pleurisy, tonsillitis, tussive urticaria, pertussis, etc. and coughs caused in bronchography or bronchoscopy, etc.
摘要翻译：含有由以下化合物或其药理学上可接受的酸加成盐代表的八氢异喹啉衍生物的镇咳剂：本发明的化合物具有显着的镇咳作用，因此可以预期作为可用于伴有咳嗽的所有疾病的药物，例如，感冒，急性支气管炎，慢性支气管炎，支气管扩张症，肺炎，肺结核，矽肺和硅肺结核等各种呼吸系统疾病，肺癌，上呼吸道炎症（咽炎，喉炎，鼻粘膜炎），哮喘性支气管炎，支气管哮喘，婴儿哮喘，慢性肺气肿，肺尘埃沉着病，肺纤维化，矽肺，肺部脓肿，胸膜炎，扁桃腺炎，咳嗽荨麻疹，百日咳等，以及支气管镜或支气管镜引起的咳嗽等。

4. 发明授权

US6087369A Indole derivatives, process for producing the same and medicinal uses of the same 失效
标题翻译：吲哚衍生物，其制备方法和药物用途
公开(公告)号：US6087369A
公开(公告)日：2000-07-11
申请号：US135580
申请日：1998-08-18
申请人： Hiroshi Nagase , Akira Mizusuna , Koji Kawai , Izumi Nakatani
发明人： Hiroshi Nagase , Akira Mizusuna , Koji Kawai , Izumi Nakatani
IPC分类号： A61K31/44 , A61K31/485 , C07D489/10 , C07D491/20 , C07D491/22
CPC分类号： C07D491/20 , C07D491/22
摘要： A novel compound which is a .delta.-opioid antagonist having high selectivity and activity, that exhibits immunosuppressive action, antiallergic action, anti-inflammatory action and brain cell-protecting action is disclosed. The compound according to the present invention is an indole derivative represented by the formula (I): ##STR1## and pharmaceutically acceptable acid addition salts thereof. The present invention also provides an immunosuppressive agent, antiallergic agent, anti-inflammatory agent and brain cell-protecting agent comprising the derivative or the salt as an effective ingredient.
摘要翻译：公开了具有高选择性和活性的具有免疫抑制作用，抗过敏作用，抗炎作用和脑细胞保护作用的具有高选择性和活性的δ-阿片拮抗剂的新型化合物。根据本发明的化合物是由式（I）表示的吲哚衍生物：及其药学上可接受的酸加成盐。本发明还提供了包含该衍生物或盐作为有效成分的免疫抑制剂，抗过敏剂，抗炎剂和脑细胞保护剂。

5. 发明授权

US5852030A Indole derivatives, process for producing the same and medicinal uses of the same 失效
标题翻译：吲哚衍生物，其制备方法和药物用途
公开(公告)号：US5852030A
公开(公告)日：1998-12-22
申请号：US709835
申请日：1996-09-10
申请人： Hiroshi Nagase , Akira Mizusuna , Koji Kawai , Izumi Nakatani
发明人： Hiroshi Nagase , Akira Mizusuna , Koji Kawai , Izumi Nakatani
IPC分类号： C07D491/20 , C07D491/22 , C07D489/10 , A61K31/485
CPC分类号： C07D491/20 , C07D491/22
摘要： A novel compound which is a .delta.-opioid antagonist having high selectivity and activity, that exhibits immunosuppressive action, antiallergic action, anti-inflammatory action and brain cell-protecting action is disclosed. The compound according to the present invention is an indole derivative represented by the formula (I): ##STR1## and pharmaceutically acceptable acid addition salts thereof. The present invention also provides an immunosuppressive agent, antiallergic agent, anti-inflammatory agent and brain cell-protecting agent comprising the derivative or the salt as an effective ingredient.
摘要翻译：公开了具有高选择性和活性的具有免疫抑制作用，抗过敏作用，抗炎作用和脑细胞保护作用的具有高选择性和活性的δ-阿片拮抗剂的新型化合物。根据本发明的化合物是由式（I）表示的吲哚衍生物：其药学上可接受的酸加成盐。本发明还提供了包含该衍生物或盐作为有效成分的免疫抑制剂，抗过敏剂，抗炎剂和脑细胞保护剂。

6. 发明授权

US06291470B1 Indole derivatives process for producing the same and medicinal uses of the same 失效
标题翻译：吲哚衍生物的制备方法及其药用用途
公开(公告)号：US06291470B1
公开(公告)日：2001-09-18
申请号：US09469544
申请日：1999-12-22
申请人： Hiroshi Nagase , Akira Mizusuna , Koji Kawai , Izumi Nakatani
发明人： Hiroshi Nagase , Akira Mizusuna , Koji Kawai , Izumi Nakatani
IPC分类号： A61K31485
CPC分类号： C07D491/20 , C07D491/22
摘要： A novel compound which is a &dgr;-opioid antagonist having high selectivity and activity, that exhibits immunosuppressive action, antiallergic action, anti-inflammatory action and brain cell-protecting action is disclosed. The compound according to the present invention is an indole derivative represented by the formula (I): and pharmaceutically acceptable acid addition salts thereof. The present invention also provides an immunosuppressive agent, antiallergic agent, anti-inflammatory agent and brain cell-protecting agent comprising the derivative or the salt as an effective ingredient.
摘要翻译：公开了一种新型化合物，其是具有高选择性和活性的Δ-阿片样物质拮抗剂，其具有免疫抑制作用，抗过敏作用，抗炎作用和脑细胞保护作用。根据本发明的化合物是由式（I）表示的吲哚衍生物：及其药学上可接受的酸加成盐。本发明还提供了包含该衍生物或盐作为有效成分的免疫抑制剂，抗过敏剂，抗炎剂和脑细胞保护剂。

7. 发明授权

US5332818A Immunosuppressive agent and process of producing the same 失效
标题翻译：免疫抑制剂及其制备方法
公开(公告)号：US5332818A
公开(公告)日：1994-07-26
申请号：US34669
申请日：1993-03-22
申请人： Hiroshi Nagase , Koji Kawai , Shu Matsumoto , Takashi Endoh , Yoshiaki Katsura , Kohei Arakawa
发明人： Hiroshi Nagase , Koji Kawai , Shu Matsumoto , Takashi Endoh , Yoshiaki Katsura , Kohei Arakawa
IPC分类号： C07D489/09 , A61K20060101 , A61K31/485 , A61P25/04 , A61P37/06 , C07D491/18 , C07D491/20 , C07D721/72
CPC分类号： C07D491/18 , A61K31/485 , C07D491/20
摘要： An immunosuppressive agent which has low toxicity and which exhibits excellent effectiveness even if it is orally administered is presented. The immunosuppressive agent of the present invention is characterized in that it contains .delta.-opioid antagonist having high selectivity to .delta.-opioid receptor. The present invention also provides a process of producing a naltrindole derivative characterized by reacting naltrexone or a salt thereof with a phenylhydrazine derivative in a solvent in the presence of methanesulfonic acid.
摘要翻译：本发明提供一种毒性低，即使口服给药也具有优异效果的免疫抑制剂。本发明的免疫抑制剂的特征在于其含有对δ-阿片受体具有高选择性的δ-阿片样物质拮抗剂。本发明还提供一种制备纳吲哚衍生物的方法，其特征在于在甲磺酸存在下，在溶剂中使纳曲酮或其盐与苯肼衍生物反应。

8. 发明授权

US5849731A Indole derivatives and medical application thereof 失效
标题翻译：吲哚衍生物及其医疗应用
公开(公告)号：US5849731A
公开(公告)日：1998-12-15
申请号：US836742
申请日：1997-05-16
申请人： Hiroshi Nagase , Koji Kawai , Takashi Endo , Shinya Ueno , Masayuki Maeda , Satoshi Sakami
发明人： Hiroshi Nagase , Koji Kawai , Takashi Endo , Shinya Ueno , Masayuki Maeda , Satoshi Sakami
IPC分类号： C07D491/22 , A61K31/475
CPC分类号： C07D491/22
摘要： The present invention relates to indole derivatives represented by the following compound 1 and the pharmacologically acceptable acid addition salt thereof. ##STR1## The compounds of the present invention were found to exhibit strong antitussive and analgesic actions as a result of pharmacological evaluation, and can be used in the pharmaceutical field as effective antitussives and analgesics.
摘要翻译： PCT No.PCT / JP96 / 02791 Sec。 371日期：1997年5月16日 102（e）日期1997年5月16日PCT提交1996年9月26日PCT公布。公开号WO97 / 11948 PCT 日期1997年4月3日本发明涉及由以下化合物1表示的吲哚衍生物及其药理学上可接受的酸加成盐。发现本发明的化合物作为药理学评价的结果表现出强烈的镇咳和镇痛作用，并且可以在制药领域中用作有效的镇咳药和镇痛药。

9. 发明授权

US5714483A Antitussive 失效
标题翻译：镇咳药
公开(公告)号：US5714483A
公开(公告)日：1998-02-03
申请号：US290837
申请日：1994-10-13
申请人： Hiroshi Nagase , Junzo Kamei , Koji Kawai , Takashi Endo
发明人： Hiroshi Nagase , Junzo Kamei , Koji Kawai , Takashi Endo
IPC分类号： A61K31/485 , A61K31/495 , C07D489/00 , C07D491/18 , C07D491/22 , A61K31/535
CPC分类号： A61K31/495 , A61K31/485 , C07D489/00
摘要： An antitussive having high activity, which is free from side effects such as psychotomimetic, which may also be administered orally is disclosed. The antitussive according to the present invention comprises as an effective ingredient a .delta.-opioid antagonist or a pharamaceutically acceptable salt thereof.
摘要翻译： PCT No.PCT / JP93 / 01855 Sec。 371日期：1994年10月13日 102（e）日期1994年10月13日PCT 1993年12月22日PCT公布。公开号WO94 / 14445 PCT 日期：1994年7月7日公开了一种具有高活性的镇咳药，其也没有副作用，如精神病药，也可以口服给药。根据本发明的止咳剂包含作为有效成分的δ-阿片样拮抗剂或其药物上可接受的盐。

10. 发明授权

US06187782B1 Morphinane derivatives and medicinal use thereof 失效
标题翻译：吗啡衍生物及其药用
公开(公告)号：US06187782B1
公开(公告)日：2001-02-13
申请号：US09194366
申请日：1998-11-25
申请人： Hiroshi Nagase , Hideaki Fujii , Takashi Endoh , Koji Kawai
发明人： Hiroshi Nagase , Hideaki Fujii , Takashi Endoh , Koji Kawai
IPC分类号： A61K31445
CPC分类号： C07D489/12
摘要： Novel morphinan derivatives and pharmaceutically acceptable acid addition salts thereof as compounds having abilities to bind to opioid &egr;-receptor, which have agonist or antagonist activities, are disclosed. The morphinan derivatives according to the present invention are represented by the formula (I).
摘要翻译：公开了作为具有结合具有激动剂或拮抗剂活性的阿片样物质受体的能力的化合物的新型吗啡喃衍生物及其药学上可接受的酸加成盐。根据本发明的吗啡喃衍生物由式（I）表示。

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