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1. 发明授权

US08455511B2 Pyrrolopyridine derivatives substituted with cyclic amino group 失效
标题翻译：被环状氨基取代的吡咯并吡啶衍生物
公开(公告)号：US08455511B2
公开(公告)日：2013-06-04
申请号：US12951556
申请日：2010-11-22
申请人： Atsuro Nakazato , Taketoshi Okubo , Dai Nozawa , Mikako Yamaguchi , Tomoko Tamita , Ludo E. J. Kennis , Marcel F. L. De Bruyn , Jean-Pierre A. M. Bongartz , Frans M. A. Van Den Keybus , Yves E. M. Van Roosbroeck , Marcel G. M. Luyckx , Robert J. M. Hendrickx
发明人： Atsuro Nakazato , Taketoshi Okubo , Dai Nozawa , Mikako Yamaguchi , Tomoko Tamita , Ludo E. J. Kennis , Marcel F. L. De Bruyn , Jean-Pierre A. M. Bongartz , Frans M. A. Van Den Keybus , Yves E. M. Van Roosbroeck , Marcel G. M. Luyckx , Robert J. M. Hendrickx
IPC分类号： C07D471/04 , A61K31/437 , C07D487/04 , A61K31/519 , A61P25/28 , A61P25/24 , A61P25/18
CPC分类号： C07D471/04 , C07D487/04 , C07F9/6561
摘要： An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastric diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. This problem can be solved with a pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by formula [I] below which has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.
摘要翻译：本发明的目的是提供一种抗CRF受体的拮抗剂，其作为治疗或预防药物是有效的，其涉及CRF被认为涉及的疾病，例如抑郁症，焦虑症，阿尔茨海默氏病，帕金森病，亨廷顿氏舞蹈病，进食疾病，高血压，胃疾病，药物依赖，癫痫，脑梗塞，脑缺血，脑水肿，头部外伤，炎症，免疫相关疾病，脱发，肠易激综合征，睡眠障碍，癫痫，皮肤病，精神分裂症等。可以用由以下式[I]表示的环氨基取代的吡咯并嘧啶或吡咯并吡啶衍生物来解决问题，其具有对CRF受体的高亲和力，并且对于CRF被认为涉及的疾病是有效的。

2. 发明授权

US07932259B2 Pyrrolo[2,3-d]pyrimidine derivatives substituted with a cyclic amino group 失效
标题翻译：被环状氨基取代的吡咯并[2,3-d]嘧啶衍生物
公开(公告)号：US07932259B2
公开(公告)日：2011-04-26
申请号：US12106873
申请日：2008-04-21
申请人： Atsuro Nakazato , Taketoshi Okubo , Dai Nozawa , Mikako Yamaguchi , Tomoko Tamita , Ludo E. J. Kennis , Marcel F. L. De Bruyn , Jean-Pierre A. M. Bongartz , Frans M. A. Van Den Keybus , Yves E. M. Van Roosbroeck , Marcel G. M. Luyckx , Robert J. M. Hendrickx
发明人： Atsuro Nakazato , Taketoshi Okubo , Dai Nozawa , Mikako Yamaguchi , Tomoko Tamita , Ludo E. J. Kennis , Marcel F. L. De Bruyn , Jean-Pierre A. M. Bongartz , Frans M. A. Van Den Keybus , Yves E. M. Van Roosbroeck , Marcel G. M. Luyckx , Robert J. M. Hendrickx
IPC分类号： C07D487/04 , A61K31/519 , A61P25/24 , A61P25/28 , A61P25/18 , A61P29/00
CPC分类号： C07D471/04 , C07D487/04 , C07F9/6561
摘要： An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastric diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. This problem can be solved with a pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by formula [I] below which has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.
摘要翻译：本发明的目的是提供一种抗CRF受体的拮抗剂，其作为治疗或预防药物是有效的，其涉及CRF被认为涉及的疾病，例如抑郁症，焦虑症，阿尔茨海默氏病，帕金森病，亨廷顿氏舞蹈病，进食疾病，高血压，胃疾病，药物依赖，癫痫，脑梗塞，脑缺血，脑水肿，头部外伤，炎症，免疫相关疾病，脱发，肠易激综合征，睡眠障碍，癫痫，皮肤病，精神分裂症等。可以用由以下式[I]表示的环氨基取代的吡咯并嘧啶或吡咯并吡啶衍生物来解决问题，其具有对CRF受体的高亲和力，并且对于CRF被认为涉及的疾病是有效的。

3. 发明授权

US5607949A [(Benzodioxan, benzofuran or benzopyran) alkylamino] alkyl substituted guanidines 失效
标题翻译： [（苯并二恶烷，苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍
公开(公告)号：US5607949A
公开(公告)日：1997-03-04
申请号：US632227
申请日：1996-04-15
申请人： Guy R. E. Van Lommen , Marcel F. L. De Bruyn , Walter J. J. Janssens
发明人： Guy R. E. Van Lommen , Marcel F. L. De Bruyn , Walter J. J. Janssens
IPC分类号： C07C279/00 , C07D307/78 , A61K31/34 , A61K31/343 , A61K31/35 , A61K31/352 , A61K31/415 , A61K31/443 , A61K31/445 , A61K31/505 , A61K31/53 , A61P9/00 , A61P9/02 , A61P25/04 , C07C277/00 , C07D307/81 , C07D311/58 , C07D319/08 , C07D319/20 , C07D405/06 , C07D405/12 , C07D405/14
CPC分类号： C07D405/12 , C07D307/81 , C07D311/58 , C07D319/20 , C07D405/14
摘要： The present invention is concerned with vasoconstricive [(benzodioxan, benzofuran or benzopyran)alkylamino]alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is a bivalent C.sub.1-3 alkanediyl radical; A is a bivalent radical of formula: ##STR2## wherein each R.sup.5 is hydrogen or C.sub.1-4 alkyl; wherein each R.sup.6 is hydrogen or C.sub.1-4 alkyl; Alk.sup.2 is C.sub.2-15 alkanediyl or C.sub.5-7 cycloalkanediyl; and each p is 0, 1 or 2; provided that [2-[(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amino]ethyl guanidine is excluded. Pharmaceuticals which are useful as vasoconstrictors. Compositions comprising said guanidine derivatives as active ingredients, processes for preparing said guanidine derivatives and novel N-cyano guanidine, intermediates; and a use as a medicine are described.
摘要翻译：本发明涉及具有下式的[（苯并二恶烷，苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍，（I）其药学上可接受的酸加成盐及其立体化学异构形式，其中X是O，CH 2 或直接债券; R1是氢或C1-6烷基; R2是氢，C1-6烷基，C3-6烯基或C3-6炔基; R3是氢或C1-6烷基; 或者R 2和R 3可以一起形成式 - （CH 2）m - 的二价基团，其中m为4或5; 或R 1和R 2一起形成式-CH = CH-或式 - （CH 2）n - 的二价基团，其中n为2,3或4; 或者当R 1和R 2一起形成式-CH = CH-CH =，-CH = CH-N =或-CH = N-CH =的二价基团时，R 3可以表示键。 R4是氢或C1-6烷基; Alk1是二价C 1-3烷二基; （a）其中每个R 5为氢或C 1-4烷基;（e）其中每个R 5为氢或C 1-4烷基;（c）其中每个R 6是氢或C 1-4烷基; Alk2是C2-15烷二基或C5-7环烷二基; 每个p为0,1或2; 条件是排除[2 - [（2,3-二氢-1,4-苯并二恶英-2-基）甲基]氨基]乙基胍。可用作血管收缩药物的药物。包含所述胍衍生物作为活性成分的组合物，制备所述胍衍生物的方法和新的N-氰基胍，中间体; 并描述了作为药物的用途。

4. 发明授权

US4878940A Herbicidal 1,5-substituted 1H-imidazoles 失效
标题翻译：除草剂1,5-取代的1H-咪唑
公开(公告)号：US4878940A
公开(公告)日：1989-11-07
申请号：US173511
申请日：1988-03-25
申请人： Marcel F. L. De Bruyn , Guy R. E. Van Lommen , William R. Lutz
发明人： Marcel F. L. De Bruyn , Guy R. E. Van Lommen , William R. Lutz
IPC分类号： A01N43/50 , C07D233/54 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D401/04 , C07D401/06 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04
CPC分类号： C07D233/64 , A01N43/50 , C07D233/84 , C07D401/04 , C07D401/06 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04
摘要： Novel herbicidal 1,5-substituted 1H-imidazole derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants. Further the invention also relates to a process for making these novel compounds.

5. 发明授权

US4994103A 1,5-substituted 1H-imidazoles 失效
标题翻译： 1,5-取代的1H-咪唑
公开(公告)号：US4994103A
公开(公告)日：1991-02-19
申请号：US420248
申请日：1989-10-12
申请人： Marcel F. L. De Bruyn , Guy R. E. Van Lommen , William R. Lutz
发明人： Marcel F. L. De Bruyn , Guy R. E. Van Lommen , William R. Lutz
IPC分类号： A01N43/50 , C07D233/54 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D401/04 , C07D401/06 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04
CPC分类号： C07D233/64 , A01N43/50 , C07D233/84 , C07D401/04 , C07D401/06 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04
摘要： Novel herbicidal 1,5-substituted 1H-imidazole derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants. Further the invention also relates to a process for making these novel compounds.

6. 发明授权

US5624952A [(Benzodioxan, benzofuran or benzopyran) alkylamino] alkyl substituted guanidines 失效
标题翻译： [（苯并二恶烷，苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍
公开(公告)号：US5624952A
公开(公告)日：1997-04-29
申请号：US632226
申请日：1996-04-15
申请人： Guy R. E. Van Lommen , Marcel F. L. De Bruyn , Walter J. J. Janssens
发明人： Guy R. E. Van Lommen , Marcel F. L. De Bruyn , Walter J. J. Janssens
IPC分类号： C07C279/00 , C07D307/78 , A61K31/34 , A61K31/343 , A61K31/35 , A61K31/352 , A61K31/415 , A61K31/443 , A61K31/445 , A61K31/505 , A61K31/53 , A61P9/00 , A61P9/02 , A61P25/04 , C07C277/00 , C07D307/81 , C07D311/58 , C07D319/08 , C07D319/20 , C07D405/06 , C07D405/12 , C07D405/14 , A61K31/40
CPC分类号： C07D405/12 , C07D307/81 , C07D311/58 , C07D319/20 , C07D405/14
摘要： The present invention is concerned with vasoconstricive [(benzodioxan, benzofuran or benzopyran)alkylamino]alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sub.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is a bivalent C.sub.1-3 alkanediyl radical; A is a bivalent radical of formula: ##STR2## wherein each R.sup.5 is hydrogen or C.sub.1-4 alkyl; wherein each R.sup.6 is hydrogen or C.sub.1-4 alkyl; Alk.sup.2 is C.sub.2-15 alkanediyl or C.sub.5-7 cycloalkanediyl; and each p is 0, 1 or 2; provided that [2-[(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amino]ethyl guanidine is excluded. Pharmaceuticals which are useful as vaseconstrictors. Compositions comprising said guanidine derivatives as active ingredients, processes for preparing said guanidine derivatives and novel N-cyano guanidine, intermediates; and a use as a medicine are described.
摘要翻译：本发明涉及具有下式的[（苯并二恶烷，苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍，（I）其药学上可接受的酸加成盐及其立体化学异构形式，其中X是O，CH 2 或直接债券; R1是氢或C1-6烷基; R2是氢，C1-6烷基，C3-6烯基或C3-6炔基; R3是氢或C1-6烷基; 或者R 2和R 3可以一起形成式 - （CH 2）m - 的二价基团，其中m为4或5; 或R 1和R 2一起形成式-CH = CH-或式 - （CH 2）n - 的二价基团，其中n为2,3或4; 或者当R 1和R 2一起形成式-CH = CH-CH =，-CH = CH-N =或-CH = N-CH =的二价基团时，R 3可以表示键。 R4是氢或C1-6烷基; Alk1是二价C 1-3烷二基; （a）其中每个R 5为氢或C 1-4烷基;（e）其中每个R 5为氢或C 1-4烷基;（c）其中每个R 6是氢或C 1-4烷基; Alk2是C2-15烷二基或C5-7环烷二基; 每个p为0,1或2; 条件是排除[2 - [（2,3-二氢-1,4-苯并二恶英-2-基）甲基]氨基]乙基胍。用作血管收缩药物的药物。包含所述胍衍生物作为活性成分的组合物，制备所述胍衍生物的方法和新的N-氰基胍，中间体; 并描述了作为药物的用途。

7. 发明授权

US5541180A [(benzodioxan, benzofuran or benzopyran) alkylamino] alkyl substituted guanidines 失效
标题翻译： [（苯并二恶烷，苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍
公开(公告)号：US5541180A
公开(公告)日：1996-07-30
申请号：US256995
申请日：1994-07-29
申请人： Guy R. E. Van Lommen , Marcel F. L. De Bruyn , Walter J. J. Janssens
发明人： Guy R. E. Van Lommen , Marcel F. L. De Bruyn , Walter J. J. Janssens
IPC分类号： C07C279/00 , C07D307/78 , A61K31/34 , A61K31/343 , A61K31/35 , A61K31/352 , A61K31/415 , A61K31/443 , A61K31/445 , A61K31/505 , A61K31/53 , A61P9/00 , A61P9/02 , A61P25/04 , C07C277/00 , C07D307/81 , C07D311/58 , C07D319/08 , C07D319/20 , C07D405/06 , C07D405/12 , C07D405/14 , A61K31/33 , C07D239/42 , C07D243/04
CPC分类号： C07D405/12 , C07D307/81 , C07D311/58 , C07D319/20 , C07D405/14
摘要： The present invention is concerned with vasoconstricive [(benzodioxan, benzofuran or benzopyran)alkylamino]alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl;Alk.sup.1 is a bivalent C.sub.1-3 alkanediyl radical; A is a bivalent radical of formula: ##STR2## wherein each R.sup.5 is hydrogen or C.sub.1-4 alkyl; wherein each R.sup.6 is hydrogen or C.sub.1-4 alkyl; Alk.sup.2 is C.sub.2-15 alkanediyl or C.sub.5-7 cycloalkanediyl; and each p is 0, 1 or 2; provided that [2-[(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amino]ethyl guanidine is excluded. Pharmaceuticals which are useful as vasoconstrictors. Compositions comprising said guanidine derivatives as active ingredients, processes for preparing said guanidine derivatives and novel N-cyano guanidine, intermediates; and a use as a medicine are described.
摘要翻译： PCT No.PCT / EP93 / 00435 Sec。 371日期1994年7月29日第 102（e）日期1994年7月29日PCT提交1993年2月19日PCT公布。出版物WO93 / 17017 日本1993年9月2日本发明涉及具有式（I）表示的药物上可接受的酸加成盐的血管收缩素[（苯并二恶烷，苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍及其立体化学异构形式，其中 X是O，CH 2或直接键; R1是氢或C1-6烷基; R2是氢，C1-6烷基，C3-6烯基或C3-6炔基; R3是氢或C1-6烷基; 或者R 2和R 3可以一起形成式 - （CH 2）m - 的二价基团，其中m为4或5; 或R 1和R 2一起形成式-CH = CH-或式 - （CH 2）n - 的二价基团，其中n为2,3或4; 或者当R 1和R 2一起形成式-CH = CH-CH =，-CH = CH-N =或-CH = N-CH =的二价基团时，R 3可以表示键。 R4是氢或C1-6烷基; Alk1是二价C1-3烷二基; （a）其中每个R 5为氢或C 1-4烷基;（e）其中每个R 5为氢或C 1-4烷基;（c）其中每个R 6是氢或C 1-4烷基; Alk2是C2-15烷二基或C5-7环烷二基; 每个p为0,1或2; 条件是排除[2 - [（2,3-二氢-1,4-苯并二恶英-2-基）甲基]氨基]乙基胍。可用作血管收缩药物的药物。包含所述胍衍生物作为活性成分的组合物，制备所述胍衍生物的方法和新的N-氰基胍，中间体; 并描述了作为药物的用途。

8. 发明授权

US4654362A Derivatives of 2,2'-iminobisethanol 失效
标题翻译： 2,2'-亚氨基双酚的衍生物
公开(公告)号：US4654362A
公开(公告)日：1987-03-31
申请号：US660355
申请日：1984-10-12
申请人： Guy R. E. Van Lommen , Marcel F. L. De Bruyn , Marc F. J. Schroven
发明人： Guy R. E. Van Lommen , Marcel F. L. De Bruyn , Marc F. J. Schroven
IPC分类号： C07D307/81 , C07D311/22 , C07D311/58 , C07D311/66 , C07D311/92 , C07D407/04 , A61K31/35 , A61K31/34 , C07D307/87
CPC分类号： C07D407/04 , C07D307/81 , C07D311/22 , C07D311/58 , C07D311/66 , C07D311/92
摘要： Derivatives of 2,2'-iminobisethanol having useful properties in the treatment and/or the prevention of disorders of the coronary-vascular system.
摘要翻译：具有治疗和/或预防冠状动脉血管系统障碍的有用性质的2,2'-亚氨基双酚的衍生物。

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