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1. 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。

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

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。

4. 发明授权

US5153183A Methylenediphosphonic acid compounds and methods of use for the treatment of rheumatism and osteophorosis 失效
标题翻译：甲基磷酸化合物及其用于治疗恶病质和卵巢功能的方法
公开(公告)号：US5153183A
公开(公告)日：1992-10-06
申请号：US663958
申请日：1991-05-06
申请人： Norio Kawabe , Keijiro Takanishi , Shu Matsumoto
发明人： Norio Kawabe , Keijiro Takanishi , Shu Matsumoto
IPC分类号： A61K31/66 , A61P3/02 , A61P29/00 , A61P43/00 , C07F9/38 , C07F9/40
CPC分类号： C07F9/386 , C07F9/3865 , C07F9/4043
摘要： This invention relates to a methylenediphosphonic acid compound expressed by the formula (1). The compound has a marked effect as an anti-inflammatory agent or, more particularly, against inflammations accompanying disturbances in bone metabolism. ##STR1##

5. 发明授权

US5478823A Composition for suppressing infiltration of eosinophils 失效
标题翻译：用于抑制嗜酸性粒细胞浸润的组合物
公开(公告)号：US5478823A
公开(公告)日：1995-12-26
申请号：US244891
申请日：1994-08-22
申请人： Katsuhiro Shibayama , Naoki Hirayama , Tetsuya Katou , Shu Matsumoto
发明人： Katsuhiro Shibayama , Naoki Hirayama , Tetsuya Katou , Shu Matsumoto
IPC分类号： C07D487/04 , A61K31/55 , A61K31/41 , A61K31/445 , A61K31/495 , A61K31/50
CPC分类号： C07D487/04
摘要： An agent for suppressing infiltration of eosinophils comprising as an effective ingredient a tricyclic triazolo derivative, which strongly suppresses infiltration of eosinophils into inflammatory regions, of the formula (I): ##STR1## wherein R.sup.1 represents hydrogen, lower alkyl, C.sub.3 -C.sub.5 cycloalkyl or substituted or non-substituted aryl; R.sup.2 and R.sup.3 independently represent hydrogen, lower alkyl, lower alkoxy or halogen; W represents C.dbd.O or CR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 independently represent hydrogen or lower alkyl; A represents C.sub.1 -C.sub.5 straight or branched saturated or unsaturated alkylene with the proviso that it may contain one or more hetero atoms; 1 represents 0 to 2, n represents 1 to 3, -- represents single bond or double bond; Y represents N or C; Z represents C(B)Ar.sup.1 Ar.sup.2 wherein B represents hydrogen, hydroxy or methoxy, Ar.sup.1 and Ar.sup.2 independently represent hydrogen or substituted or non-substituted aryl, CAr.sup.1 Ar.sup.2 wherein Ar.sup.1 and Ar.sup.2 represent the same meanings as mentioned above, O--CHAr.sup.1 Ar.sup.2 wherein Ar.sup.1 and Ar.sup.2 represent the same meanings as mentioned above or a condensed aromatic ring or a pharmaceutically acceptable salt thereof.
摘要翻译：抑制嗜酸性粒细胞浸润的药剂，其包含作为有效成分的三环三唑衍生物，其将强烈抑制嗜酸性粒细胞浸润至炎性区域的式（I）：其中R1表示氢，低级烷基，C3- C5环烷基或取代或未取代的芳基; R2和R3独立地表示氢，低级烷基，低级烷氧基或卤素; W表示C = O或CR 4 R 5，其中R 4和R 5独立地表示氢或低级烷基; A表示C1-C5直链或支链饱和或不饱和亚烷基，条件是其可以含有一个或多个杂原子; 1表示0〜2，n表示1〜3， - 表示单键或双键; Y表示N或C; Z表示C（B）Ar1Ar2其中B表示氢，羟基或甲氧基，Ar1和Ar2独立地表示氢或取代或未取代的芳基，CAr1Ar2其中Ar1和Ar2表示与上述相同的含义，O-CHAr1Ar2其中Ar1和Ar2 表示与上述相同的含义或稠合芳环或其药学上可接受的盐。

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