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1. 发明授权

US06759401B2 Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases 有权
公开(公告)号：US06759401B2
公开(公告)日：2004-07-06
申请号：US10269670
申请日：2002-10-11
申请人： Björn Nilsson , Jan Tejbrant , Benjamin Pelcman , Erik Ringberg , Markus Thor , Jonas Nilsson , Mattias Jönsson
发明人： Björn Nilsson , Jan Tejbrant , Benjamin Pelcman , Erik Ringberg , Markus Thor , Jonas Nilsson , Mattias Jönsson
IPC分类号： A61K3133
摘要： The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are as defined in the claims, and n is 0 or 1; and pharmaceutically acceptable salts, hydrates and prodrug forms thereof The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder, such as eating disorders, especially obesity, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctions, and urinary disorders The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of formula (I)

2. 发明授权

US06465467B1 Certain aryl-aliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases 有权
标题翻译：某些芳基 - 脂族和杂芳基 - 脂族哌嗪基吡嗪及其在治疗5-羟色胺相关疾病中的应用
公开(公告)号：US06465467B1
公开(公告)日：2002-10-15
申请号：US09589282
申请日：2000-06-08
申请人： Björn Nilsson , Jan Tejbrant , Benjamin Pelcman , Erik Ringberg , Markus Thor , Jonas Nilsson , Mattias Jönsson
发明人： Björn Nilsson , Jan Tejbrant , Benjamin Pelcman , Erik Ringberg , Markus Thor , Jonas Nilsson , Mattias Jönsson
IPC分类号： A61K31495
CPC分类号： C07D401/12 , C07D241/18 , C07D241/20 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D491/04
摘要： Compounds of the general formula (I): wherein the variables are as defined in the specification are useful for the prophylaxis or treatment of serotonin-related, especially 5-HT2 receptor-related, diseases in human beings or animals, particularly diseases related to the 5-HT2c receptor, especially diseases such as eating disorders, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctionions, and urinary disorders.
摘要翻译：通式（I）的化合物：其中变量如本说明书中所定义，可用于预防或治疗人类或动物中5-羟色胺相关的，特别是5-HT2受体相关的疾病，特别是与特别是进食障碍，记忆障碍，精神分裂症，情绪障碍，焦虑障碍，疼痛，性功能障碍和尿失调等疾病。

3. 发明授权

US07071180B2 Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases 失效
公开(公告)号：US07071180B2
公开(公告)日：2006-07-04
申请号：US10873852
申请日：2004-06-22
申请人： Björn Nilsson , Jan Tejbrant , Benjamin Pelcman , Erik Ringberg , Markus Thor , Jonas Nilsson , Mattias Jönsson
发明人： Björn Nilsson , Jan Tejbrant , Benjamin Pelcman , Erik Ringberg , Markus Thor , Jonas Nilsson , Mattias Jönsson
IPC分类号： A61K31/33 , A61K31/502 , A61K31/497 , C07D401/04 , C07D241/36
CPC分类号： C07D401/12 , C07D241/18 , C07D241/20 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D491/04
摘要： The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are as defined in the claims, and n is 0 or 1; and pharmaceutically acceptable salts, hydrates and prodrug forms thereof. The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder, such as eating disorders, especially obesity, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctions, and urinary disorders. The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of formula (I).

4. 发明授权

US07534794B2 Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases 失效
标题翻译：某些芳基脂族和杂芳基 - 脂族哌嗪基吡嗪及其在治疗5-羟色胺相关疾病中的应用
公开(公告)号：US07534794B2
公开(公告)日：2009-05-19
申请号：US10269670
申请日：2002-10-11
申请人： Björn Nilsson , Jan Tejbrant , Benjamin Pelcman , Erik Ringberg , Markus Thor , Jonas Nilsson , Mattias Jönsson
发明人： Björn Nilsson , Jan Tejbrant , Benjamin Pelcman , Erik Ringberg , Markus Thor , Jonas Nilsson , Mattias Jönsson
IPC分类号： A61K31/50 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00
CPC分类号： C07D401/12 , C07D241/18 , C07D241/20 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D491/04
摘要： The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are as defined in the claims, and n is 0 or 1; and pharmaceutically acceptable salts, hydrates and prodrug forms thereof. The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder, such as eating disorders, especially obesity, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctions, and urinary disorders The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of formula (I).
摘要翻译：本发明涉及通式（I）的化合物：其中Ar为任选取代的芳基或杂芳基; A是（ⅰ）-O - ， - S - ， - SO 2 - ， - NH - ，（ⅱ）C 1-4 - 烷基 - 或C 1-6 - 酰基取代的氮原子或（ⅲ）亚烷基链或具有2至8个链原子的杂亚烷基链，其任选地包含至少一个不饱和键，并且其可以被取代和/或含有桥以形成具有3-8个环成员的饱和或部分或完全不饱和的环; B是-C（R 4）（R 5） - ， - OC（R 4）（R 5） - ， - N（R 6）或-SO 2 - ; R是任选取代的C 3-8 - 环烷基，芳基或杂芳基; R1是（i）饱和或不饱和的氮杂环或氨基氮杂环或饱和的二氮环或氨基二氮环，其具有4至7个环成员，或具有7至10个环成员的饱和氨基氮杂双环，氮杂双环或二氮杂双环，其任选地环在一个或多个位置被取代，或基团 - [C（R 4）（R 5）] x N（R 2a）（R 3a）]; R2a，R3a，R4，R5，R6和x如权利要求中所定义，n为0或1; 及其药学上可接受的盐，水合物和前药形式。化合物可以通过本身的常规方法制备，并且可以用于治疗患有5-羟色胺相关病症的人或动物受试者，例如进食障碍，特别是肥胖，记忆障碍，精神分裂症，情绪障碍，焦虑症，疼痛，性功能障碍和尿失调本发明还涉及这样的用途以及包含式（I）化合物的药物组合物。

5. 发明授权

US08951999B2 Compounds 有权
标题翻译：化合物
公开(公告)号：US08951999B2
公开(公告)日：2015-02-10
申请号：US12908172
申请日：2010-10-20
申请人： Henning Priepke , Henri Doods , Raimund Kuelzer , Roland Pfau , Dirk Stenkamp , Robert Roenn , Benjamin Pelcman
发明人： Henning Priepke , Henri Doods , Raimund Kuelzer , Roland Pfau , Dirk Stenkamp , Robert Roenn , Benjamin Pelcman
IPC分类号： A61K31/445 , C07D211/32 , C07C311/14 , C07D213/82 , C07C237/42 , C07C237/44 , C07C255/23 , C07C255/60 , C07D205/04 , C07D207/10 , C07D207/22 , C07D207/34 , C07D209/08 , C07D211/14 , C07D211/16 , C07D211/18 , C07D211/38 , C07D213/40 , C07D213/75 , C07D213/81 , C07D215/42 , C07D237/30 , C07D277/46 , C07D277/56 , C07D277/60 , C07D277/82 , C07D295/15 , C07D295/155 , C07D307/20 , C07D307/24 , C07D309/12 , C07D309/14 , C07D333/38 , C07D335/02 , C07D417/04
CPC分类号： C07D213/82 , C07C237/42 , C07C237/44 , C07C255/23 , C07C255/60 , C07C311/14 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/10 , C07D207/22 , C07D207/34 , C07D209/08 , C07D211/14 , C07D211/16 , C07D211/18 , C07D211/38 , C07D213/40 , C07D213/75 , C07D213/81 , C07D215/42 , C07D237/30 , C07D277/46 , C07D277/56 , C07D277/60 , C07D277/82 , C07D295/15 , C07D295/155 , C07D307/20 , C07D307/24 , C07D309/12 , C07D309/14 , C07D333/38 , C07D335/02 , C07D417/04
摘要： This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
摘要翻译：本发明涉及式I化合物，它们作为微粒体前列腺素E2合成酶-1（mPGES-1）的抑制剂的用途，含有它们的药物组合物及其用作治疗和/或预防炎性疾病和相关病症的药物如炎性/伤害性疼痛。 A，M，R 1，R 2，R 7，R a，R b，Q 3，Q 4，Q 6，Z 2，Z 4，Z 5，Z 6和W具有说明书中给出的含义。

6. 发明申请

US20120004244A1 Bis Aromatic Compounds for Use as LTC4 Synthase Inhibitors 审中-公开
标题翻译：用作LTC4合酶抑制剂的双芳香族化合物
公开(公告)号：US20120004244A1
公开(公告)日：2012-01-05
申请号：US13256003
申请日：2010-03-12
申请人： Peter Nilsson , Benjamin Pelcman , Martins Katkevics
发明人： Peter Nilsson , Benjamin Pelcman , Martins Katkevics
IPC分类号： A61K31/44 , C07D401/10 , A61K31/4439 , C07D405/10 , A61K31/443 , C07D239/42 , A61K31/505 , C07D213/79 , A61P37/08 , A61P11/00 , A61P17/00 , A61P1/00 , A61P29/00 , A61P9/00 , A61P11/02 , A61P31/04 , A61P31/12 , A61P31/10 , A61P27/02 , A61P25/00 , C07D213/74
CPC分类号： C07D405/12 , C07D213/50 , C07D213/65 , C07D213/74 , C07D401/10 , C07D409/12
摘要： There is provided compounds of formula I, wherein E1, E2a, E2b, E2c, E4, D1, D2, D3, L1, Y1, L2 and Y2 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.
摘要翻译：提供式I化合物，其中E1，E2a，E2b，E2c，E4，D1，D2，D3，L1，Y1，L2和Y2具有说明书中给出的含义及其药学上可接受的盐，该化合物是有用的用于治疗期望和/或需要抑制白细胞三烯C4合酶的疾病，特别是治疗呼吸障碍和/或炎症的疾病。

7. 发明申请

US20110319431A1 Bis Aromatic Compounds for Use as LTC4 Synthase Inhibitors 审中-公开
标题翻译：用作LTC4合酶抑制剂的双芳香族化合物
公开(公告)号：US20110319431A1
公开(公告)日：2011-12-29
申请号：US13256122
申请日：2010-03-15
申请人： Peter Nilsson , Benjamin Pelcman , Martins Katkevics
发明人： Peter Nilsson , Benjamin Pelcman , Martins Katkevics
IPC分类号： A61K31/505 , A61K31/196 , C07D239/47 , C07D213/78 , C07C59/84 , A61P31/12 , A61P11/00 , A61P29/00 , A61P37/08 , A61P11/06 , A61P9/00 , A61P27/16 , A61P27/02 , A61P17/00 , A61P1/00 , A61P13/00 , A61P25/00 , A61P7/06 , A61P31/04 , A61P31/10 , A61K31/44
CPC分类号： C07C323/63 , C07C317/48 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07C2603/74 , C07D213/50 , C07D213/65 , C07D213/74 , C07D317/46 , C07D335/02 , C07D401/10 , C07D405/12 , C07D409/12
摘要： There is provided compounds of formula I, wherein Y, ring A, D1, D2a, D2b, D3, L1, Y1, L3 and Y3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.
摘要翻译：提供了式I化合物，其中Y，环A，D1，D2a，D2b，D3，L1，Y1，L3和Y3具有说明书中给出的含义及其药学上可接受的盐，该化合物可用于治疗需要和/或需要抑制白细胞三烯C4合酶的疾病，特别是治疗呼吸障碍和/或炎症的疾病。

8. 发明申请

US20090258917A1 Benzoxazoles Useful in the Treatment of Inflammation 审中-公开
标题翻译：苯并恶唑可用于治疗炎症
公开(公告)号：US20090258917A1
公开(公告)日：2009-10-15
申请号：US12083384
申请日：2006-10-12
申请人： Benjamin Pelcman , Kristofer Olofsson , Wesley Schaal , Ivars Kalvins , Martins Katkevics , Vita Ozola , Edgars Suna
发明人： Benjamin Pelcman , Kristofer Olofsson , Wesley Schaal , Ivars Kalvins , Martins Katkevics , Vita Ozola , Edgars Suna
IPC分类号： A61K31/423 , C07D263/54 , A61P29/00
CPC分类号： A61K31/423 , A61K31/4439 , A61K31/497 , C07D263/57 , C07D413/12
摘要： There is provided the use of a compound of formula I, wherein Y, W1 to W4, Z1 to Z4 and R have meanings given in the description, and pharmaceutically-acceptable salts thereof, for the manufacture of a medicament for the treatment of a disease in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.
摘要翻译：提供式I化合物的用途，其中Y，W1至W4，Z1至Z4和R具有本说明书中给出的含义及其药学上可接受的盐在制备用于治疗疾病的药物中的用途其中希望和/或需要MAPEG家族成员的活性的抑制，特别是在治疗炎症中。

9. 发明申请

US20080188473A1 Indoles Useful in the Treatment of Inflammation 审中-公开
标题翻译：有用的治疗炎症的吲哚
公开(公告)号：US20080188473A1
公开(公告)日：2008-08-07
申请号：US11629627
申请日：2005-06-17
申请人： Kristofer Olofsson , Benjamin Pelcman , Wesley Schaal , Ivars Kalvins , Edgars Suna , Vita Ozola , Martins Katkevics
发明人： Kristofer Olofsson , Benjamin Pelcman , Wesley Schaal , Ivars Kalvins , Edgars Suna , Vita Ozola , Martins Katkevics
IPC分类号： A61K31/404 , A61P29/00 , A61P1/00 , A61P31/00 , A61P9/10 , A61P11/00 , A61P25/00 , A61P17/00 , C07D209/42 , C07D401/12 , C07D413/02 , C07D401/14 , A61K31/5377 , A61K31/4439
CPC分类号： C07D401/12 , C07D209/42
摘要： There is provided a compound of formula: (I) wherein X, R1, R2, R3, R4, R5, R6, R7 and R8 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of microsomal prostaglandin E synthase-1 is desired and/or required, and particularly in the treatment of inflammation.
摘要翻译：提供了式（I）的化合物，其中X，R 1，R 2，R 3，R 4， R 5，R 5，R 6，R 7和R 8具有说明书中给出的含义，和其药学上可接受的盐，该化合物可用于治疗期望和/或需要抑制微粒体前列腺素E合酶-1的活性，特别是治疗炎症的疾病。

10. 发明授权

US6153626A Compounds with analgesic effect 失效
标题翻译：化合物具有镇痛作用
公开(公告)号：US6153626A
公开(公告)日：2000-11-28
申请号：US29468
申请日：1998-03-03
申请人： Benjamin Pelcman , Edward Roberts
发明人： Benjamin Pelcman , Edward Roberts
IPC分类号： A61K31/00 , A61K31/40 , A61K31/445 , A61K31/4462 , A61K31/4468 , A61K31/63 , A61K51/04 , A61P1/00 , A61P25/00 , A61P29/00 , C07D207/14 , C07D211/56 , C07D211/58
CPC分类号： C07D211/58 , A61K51/0446 , A61K51/0455 , C07D207/14 , C07D211/56 , A61K2123/00
摘要： Compounds of general formula (I) ##STR1## wherein m is 0 or 1, and n is 1 or 2; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
摘要翻译： PCT No.PCT / SE97 / 02051 Sec。 371日期1998年3月3日 102（e）1998年3月3日PCT 1997年12月9日PCT公布。公开号WO98 / 28270 日期1998年7月2日通式（I）的化合物，其中m为0或1，n为1或2; 在本申请中公开和要求保护，以及它们的药学上可接受的盐，包含新化合物的药物组合物及其在治疗中的用途，特别是在疼痛的治疗中的用途。

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