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71. 发明授权

US06403593B1 Triazole compounds and the use thereof 有权
标题翻译：三唑化合物及其用途
公开(公告)号：US06403593B1
公开(公告)日：2002-06-11
申请号：US09481976
申请日：2000-01-13
申请人： Beate Hellendahl , Annegret Lansky , Rainer Munschauer , Siegfried Bialojan , Liliane Unger , Hans-Jürgen Teschendorf , Karsten Wicke , Karla Drescher
发明人： Beate Hellendahl , Annegret Lansky , Rainer Munschauer , Siegfried Bialojan , Liliane Unger , Hans-Jürgen Teschendorf , Karsten Wicke , Karla Drescher
IPC分类号： C07D40312
CPC分类号： C07D403/12 , C07D249/12
摘要： The present invention relates to triazole compounds of the following formula: where R1, R2, A, B and Ar have the meanings stated in the description. The compounds according to the invention have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders which respond to dopamine D3 ligands.
摘要翻译：本发明涉及下式的三唑化合物：其中R1，R2，A，B和Ar具有说明书中所述的含义。根据本发明的化合物对多巴胺D3受体具有高亲和力，因此可用于治疗对多巴胺D3配体作出反应的病症。

72. 发明授权

US07320979B2 N-[(piperazinyl)hetaryl]arylsulfonamide compounds 失效
公开(公告)号：US07320979B2
公开(公告)日：2008-01-22
申请号：US10823317
申请日：2004-04-13
申请人： Wilfried M. Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Hervé Geneste , Liliane Unger , Daryl R. Sauer , Sean C. Turner
发明人： Wilfried M. Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Hervé Geneste , Liliane Unger , Daryl R. Sauer , Sean C. Turner
IPC分类号： A61K31/496 , A61K31/506 , C07D213/72 , C07D213/74 , C07D239/48
CPC分类号： C07D213/76 , C07D213/74 , C07D239/69 , C07D401/04 , C07D487/08
摘要： The invention relates to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula I in which Q is a bivalent, 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Ra which is/are selected, independently of each other, from halogen, CN, NO2, CO2R4, COR5, C1-C4-alkyl and C1-C4-haloalkyl; Ar is phenyl or a 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Rb, which is/are selected from halogen, NO2, CN, CO2R4, COR5, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl and C1-C4-haloalkyl, with it also being possible for two radicals Rb which are bonded to adjacent C atoms of Ar to be together C3-C4-alkylene; R1 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy-C1-C4-alkyl, C3-C4-alkenyl or C3-C4-alkynyl; with the radicals n, R1, R2, R3, R4 and R5 having the meanings given in the patent claims, to the N-oxides and to the physiologically tolerated acid addition salts of these compounds and to pharmaceutical compositions which comprise at least one N-[(piperazinyl)hetaryl]arylsulfonamide compound as claimed in one of claims 1 to 10 and/or at least one physiologically tolerated acid addition salt of I and/or an N-oxide of I, where appropriate together with physiologically acceptable carriers and/or auxiliary substances for treating diseases which respond to influencing by dopamine D3 receptor antagonists or agonists, in particular for treating diseases of the central nervous system and disturbances of kidney function.

73. 发明授权

US08772313B2 Benzenesulfonyl or sulfonamide compounds suitable for treating disorders that respond to the modulation of the serotonin 5-HT6 receptor 有权
标题翻译：适用于治疗对5-羟色胺5-HT 6受体调节作出反应的病症的苯磺酰基或磺酰胺化合物
公开(公告)号：US08772313B2
公开(公告)日：2014-07-08
申请号：US13286387
申请日：2011-11-01
申请人： Andreas Haupt , Frauke Pohlki , Liliane Unger , Ana Lucia Relo , Karsten Wicke , Min Zhang
发明人： Andreas Haupt , Frauke Pohlki , Liliane Unger , Ana Lucia Relo , Karsten Wicke , Min Zhang
IPC分类号： A61K31/435 , A61K31/451 , A61K31/40 , A61K31/403 , A61P3/04 , A61P25/30 , A61P25/28 , A61P25/18 , A61P25/00 , C07D211/28 , C07D209/52 , C07D221/04
CPC分类号： C07D209/52 , C07D211/24 , C07D221/06
摘要： The present invention relates to benzenesulfonyl or sulfonamide compounds of formulae IA and IB wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.
摘要翻译：本发明涉及式IA和IB的苯磺酰基或磺酰胺化合物，其中变量具有权利要求书和说明书中给出的含义，含有它们的药物组合物及其在治疗中的用途。该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT6受体的调节作出反应的疾病。

74. 发明授权

US08710059B2 N-phenyl-(homo)piperazinyl-benzenesulfonyl or benzenesulfonamide compounds suitable for treating disorders that respond to the modulation of the serotonin 5-HT6 receptor 有权
标题翻译： N-苯基 - （高）哌嗪基 - 苯磺酰基或苯磺酰胺化合物，适用于治疗对5-羟色胺5-HT 6受体的调节作用的病症
公开(公告)号：US08710059B2
公开(公告)日：2014-04-29
申请号：US13286446
申请日：2011-11-01
申请人： Andreas Haupt , Frauke Pohlki , Liliane Unger , Ana Lucia Relo , Karsten Wicke , Min Zhang
发明人： Andreas Haupt , Frauke Pohlki , Liliane Unger , Ana Lucia Relo , Karsten Wicke , Min Zhang
IPC分类号： A61K31/495 , C07D241/04
CPC分类号： C07D295/096 , C07D243/08
摘要： The present invention relates to N-Phenyl-(homo)piperazinyl-benzenesulfonyl or benzenesulfonamide compounds of formula I wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.
摘要翻译：本发明涉及式I的N-苯基 - （同）哌嗪基 - 苯磺酰基或苯磺酰胺化合物，其中变量具有权利要求书和说明书中给出的含义，含有它们的药物组合物及其在治疗中的用途。该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT6受体的调节作出反应的疾病。

75. 发明申请

US20120142674A1 N-PHENYL-(HOMO)PIPERAZINYL-BENZENESULFONYL OR BENZENESULFONAMIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO THE MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 有权
标题翻译： N-苯基 - （HOMO）哌嗪二苯并呋喃或苯并呋喃半导体化合物，适用于治疗依托莫司汀5-HT6受体调节的病症
公开(公告)号：US20120142674A1
公开(公告)日：2012-06-07
申请号：US13286446
申请日：2011-11-01
申请人： Andreas Haupt , Frauke Pohlki , Liliane Unger , Ana Lucia Relo , Karsten Wicke , Min Zhang
发明人： Andreas Haupt , Frauke Pohlki , Liliane Unger , Ana Lucia Relo , Karsten Wicke , Min Zhang
IPC分类号： A61K31/551 , C07D243/08 , A61K31/495 , A61P25/18 , A61P25/30 , A61P3/04 , A61P25/28 , C07D295/135 , A61P25/00
CPC分类号： C07D295/096 , C07D243/08
摘要： The present invention relates to N-Phenyl-(homo)piperazinyl-benzenesulfonyl or benzenesulfonamide compounds of formula I wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.
摘要翻译：本发明涉及式I的N-苯基 - （同）哌嗪基 - 苯磺酰基或苯磺酰胺化合物，其中变量具有权利要求书和说明书中给出的含义，含有它们的药物组合物及其在治疗中的用途。该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT6受体的调节作出反应的疾病。

76. 发明申请

US20120129883A1 BENZENESULFONYL OR SULFONAMIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO THE MODULATION OFTHE SEROTONIN 5-HT6 RECEPTOR 有权
标题翻译：适用于治疗血清丝素5-HT6受体调节障碍的苯并呋喃或磺酰胺化合物
公开(公告)号：US20120129883A1
公开(公告)日：2012-05-24
申请号：US13286387
申请日：2011-11-01
申请人： Andreas Haupt , Frauke Pohlki , Liliane Unger , Ana Lucia Relo , Karsten Wicke , Min Zhang
发明人： Andreas Haupt , Frauke Pohlki , Liliane Unger , Ana Lucia Relo , Karsten Wicke , Min Zhang
IPC分类号： A61K31/435 , C07D211/28 , A61K31/451 , A61K31/40 , A61P3/04 , A61P25/30 , A61P25/28 , A61P25/18 , C07D209/52 , C07D221/04 , A61K31/403 , C07D207/09 , A61P25/00
CPC分类号： C07D209/52 , C07D211/24 , C07D221/06
摘要： The present invention relates to benzenesulfonyl or sulfonamide compounds of formulae IA and IB wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.
摘要翻译：本发明涉及式IA和IB的苯磺酰基或磺酰胺化合物，其中变量具有权利要求书和说明书中给出的含义，含有它们的药物组合物及其在治疗中的用途。该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT6受体的调节作出反应的疾病。

77. 发明授权

US08008488B2 Pyrimidin-2-one compounds and their use as dopamine D3 receptor ligands 有权
标题翻译：嘧啶-2-酮化合物及其作为多巴胺D3受体配体的用途
公开(公告)号：US08008488B2
公开(公告)日：2011-08-30
申请号：US10548931
申请日：2004-03-12
申请人： Hervé Geneste , Andreas Kling , Wilfried Braje , Andreas Haupt , Liliane Unger
发明人： Hervé Geneste , Andreas Kling , Wilfried Braje , Andreas Haupt , Liliane Unger
IPC分类号： C07D403/06 , C07D403/14 , C07D401/06 , C07D401/14 , A61K31/505 , A61K31/506 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/22 , A61P25/30
CPC分类号： C07D239/36 , C07D239/52 , C07D239/54 , C07D239/553 , C07D239/56 , C07D401/12 , C07D403/14 , C07D405/14 , C07D409/14
摘要： The invention relates to pyrimidin 2-one compounds of general formula (I), in addition to the derivatives and tautomers of (I) and the physiologically acceptable salts of said compounds. In said formula, A represents linear or branched C3-C6 alkene, which can have a double bond or triple bond and/or a group Z, which is not adjacent to the nitrogen atom of the pyrimidinone ring and is selected from O, S, C(O), NR3, C(O)NR3, NR3C(O), OC(O) and C(O)O; B represents a group of the formula (II), in which X stands for CH2 or N and Y stands for CH2 or CH2CH2, or X—Y can also jointly represent C═CH, C═CH—CH2 or CH—CH═CH; R1 and R2 are defined as cited in the description and the claims; and Ar represents an optionally substituted aromatic group. The invention also relates to a pharmaceutical agent, containing at least one compound (I) and the tautomers, derivatives and/or acid addition salts of said compound, optionally together with physiologically acceptable carriers and/or auxiliary agents. The invention also relates to the use of compounds of formula (I), and their tautomers, derivatives and pharmacologically acceptable acid addition salts for producing a pharmaceutical agent for treating diseases which respond to the influence of dopamine D3 receptor ligands.
摘要翻译：除了（I）的衍生物和互变异构体以及所述化合物的生理学上可接受的盐之外，本发明涉及通式（I）的嘧啶-2-酮化合物。在所述式中，A表示可以具有双键或三键的直链或支链C 3 -C 6烯基和/或不与嘧啶酮环的氮原子相邻并且选自O，S， C（O），NR 3，C（O）NR 3，NR 3 C（O），OC（O）和C（O）O; B表示式（II）的基团，其中X表示CH2或N，Y表示CH2或CH2CH2，或X-Y也可共同表示C = CH，C = CH-CH 2或CH-CH = CH ; R1和R2定义为在说明书和权利要求书中引用的; 并且Ar表示任选取代的芳族基团。本发明还涉及含有至少一种化合物（I）和所述化合物的互变异构体，衍生物和/或酸加成盐，任选地与生理上可接受的载体和/或辅助剂一起的药剂。本发明还涉及式（I）化合物及其互变异构体，衍生物和药理学上可接受的酸加成盐的用途，用于制备用于治疗对多巴胺D3受体配体的影响作出反应的疾病的药剂。

78. 发明授权

US08350055B2 Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing them 有权
公开(公告)号：US08350055B2
公开(公告)日：2013-01-08
申请号：US12839612
申请日：2010-07-20
申请人： Thorsten Oost , Wilfried Hornberger , Herve Geneste , Daryl Richard Sauer , Wolfgang Wernet , Andrea Hager-Wernet, legal representative , Liliane Unger , Wilfried Lubisch
发明人： Thorsten Oost , Wilfried Hornberger , Herve Geneste , Daryl Richard Sauer , Wolfgang Wernet , Liliane Unger , Wilfried Lubisch
IPC分类号： C07D411/00
CPC分类号： C07D401/14 , C07D401/12 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D513/04
摘要： The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6, and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.

79. 发明申请

US20110077241A1 HETEROARYL-SUBSTITUTED 1,3-DIHYDROINDOL-2-ONE DERIVATIVES AND MEDICAMENTS CONTAINING THEM 有权
标题翻译：异取代的1,3-二氢吲哚-2-酮衍生物和含有它们的药物
公开(公告)号：US20110077241A1
公开(公告)日：2011-03-31
申请号：US12839595
申请日：2010-07-20
申请人： Wilfried Lubisch , Wilfried Hornberger , Thorsten Oost , Daryl Richard Sauer , Liliane Unger , Wolfgang Wernet , Hervé Geneste , Andrea Hager-Wernet
发明人： Wilfried Lubisch , Wilfried Hornberger , Thorsten Oost , Daryl Richard Sauer , Liliane Unger , Wolfgang Wernet , Hervé Geneste , Andrea Hager-Wernet
IPC分类号： A61K31/538 , C07D417/14 , A61K31/428 , C07D403/14 , A61K31/506 , C07D401/14 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/4725 , A61K31/4709 , C07D409/14 , A61K31/404 , C07D413/14 , A61K31/5377 , A61K31/496 , A61P25/28 , A61P5/46 , A61P25/24 , A61P25/18 , A61P25/00
CPC分类号： C07D403/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/14 , C07D409/04 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6, and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.
摘要翻译：本发明涉及式（I）的新的1,3-二氢吲哚-2-酮（羟吲哚）衍生物，其中A，R3，R4，R5，R6和R7如权利要求1所定义，他们为治疗疾病。特别地，新型羟基吲哚衍生物可用于控制和/或预防各种加压素依赖性或催产素依赖性疾病。

80. 发明申请

US20110071132A1 SUBSTITUTED OXINDOLE DERIVATIVES, DRUGS CONTAINING SAID DERIVATIVES AND THE USE THEREOF 有权
标题翻译：取代的氧化衍生物，含有所述衍生物的药物及其用途
公开(公告)号：US20110071132A1
公开(公告)日：2011-03-24
申请号：US12847529
申请日：2010-07-30
申请人： Thorsten Oost , Wilfried Lubisch , Wolfgang Wernet , Andrea Hager-Wernet , Wilfried Hornberger , Liliane Unger
发明人： Thorsten Oost , Wilfried Lubisch , Wolfgang Wernet , Andrea Hager-Wernet , Wilfried Hornberger , Liliane Unger
IPC分类号： A61K31/404 , C07D403/14 , C07D403/04 , C07D401/14 , C07D413/14 , C07D209/34 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/475 , A61P9/12 , A61P9/04 , A61P9/10 , A61P9/00 , A61P13/12 , A61P1/00 , A61P1/04 , A61P25/22 , A61P25/28 , A61P25/18 , A61P25/00 , A61P25/24
CPC分类号： C07D403/14 , C07D401/14 , C07D403/04 , C07D409/14
摘要： The invention relates to novel oxindol derivative of general formula (I), wherein substituents R1, R2, A, B and Y are such as defined in a claim 1. Drugs containing said derivatives and the use thereof for preventing and/or treating vassopress- and/or oxytocin-dependent-diseases are also disclosed.
摘要翻译：本发明涉及通式（I）的新型羟吲哚衍生物，其中取代基R 1，R 2，A，B和Y如权利要求1中所定义。含有所述衍生物的药物及其用于预防和/ 和/或催产素依赖性疾病也被公开。

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