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)

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。

公开(公告)号：US08759537B2

公开(公告)日：2014-06-24

申请号：US13211470

申请日：2011-08-17

申请人： Henning Priepke ,  Henri Doods ,  Raimund Kuelzer ,  Roland Pfau ,  Dirk Stenkamp ,  Benjamin Pelcman ,  Robert Roenn

发明人： Henning Priepke ,  Henri Doods ,  Raimund Kuelzer ,  Roland Pfau ,  Dirk Stenkamp ,  Benjamin Pelcman ,  Robert Roenn

IPC分类号： A61K31/427 ,  A61K31/428 ,  A61K31/422 ,  A61K31/4439 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D235/30 ,  C07D417/12

CPC分类号： C07D235/30 ,  C07C211/29 ,  C07C211/52 ,  C07C233/36 ,  C07C233/62 ,  C07C271/20 ,  C07C331/28 ,  C07C2601/02 ,  C07D277/56 ,  C07D277/82 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

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. A, M, W, R1, R2, R6, R7, R8 have meanings given in the description.

摘要翻译： 本发明涉及式I化合物，其用作微粒体前列腺素E2合酶-1（mPGES-1）的抑制剂，含有它们的药物组合物及其作为用于治疗和/或预防炎性疾病及相关病症的药物的用途。 A，M，W，R 1，R 2，R 6，R 7，R 8具有说明书中给出的含义。

公开(公告)号：US20060183780A1

公开(公告)日：2006-08-17

申请号：US10547996

申请日：2004-03-12

申请人： Anders Hallberg ,  Wesley Schaal ,  Mats Larhed ,  Kristofer Olofsson ,  Benjamin Pelcman ,  Andrei Sanin

发明人： Anders Hallberg ,  Wesley Schaal ,  Mats Larhed ,  Kristofer Olofsson ,  Benjamin Pelcman ,  Andrei Sanin

IPC分类号： A61K31/4439 ,  A61K31/427 ,  A61K31/4152 ,  C07D417/02 ,  C07D403/02

CPC分类号： C07D231/14 ,  C07D231/18 ,  C07D231/40 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14

摘要： There is provided a compound of formula (I), wherein R1, R2, R3, X and Y 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 a lipoxygenase (e.g. 15-lipoxygenase) is desired and/or required, and particularly in the treatment of inflammation.

摘要翻译： 提供式（I）的化合物，其中R 1，R 2，R 3，X和Y具有在 描述及其药学上可接受的盐，该化合物可用于治疗期望和/或需要抑制脂氧合酶（例如，15-脂肪氧合酶）的活性，特别是治疗炎症的疾病。

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。

公开(公告)号：US08586604B2

公开(公告)日：2013-11-19

申请号：US13211471

申请日：2011-08-17

申请人： Henning Priepke ,  Henri Doods ,  Raimund Kuelzer ,  Roland Pfau ,  Dirk Stenkamp ,  Benjamin Pelcman ,  Robert Roenn ,  Dimitrijs Lubriks ,  Edgars Suna

发明人： Henning Priepke ,  Henri Doods ,  Raimund Kuelzer ,  Roland Pfau ,  Dirk Stenkamp ,  Benjamin Pelcman ,  Robert Roenn ,  Dimitrijs Lubriks ,  Edgars Suna

IPC分类号： A61K31/437 ,  A61P29/00 ,  C07D471/04

CPC分类号： C07D471/04

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. A, M, W, R1, R2, R6, R7 have meanings given in the description.

摘要翻译： 本发明涉及式I化合物，其用作微粒体前列腺素E2合酶-1（mPGES-1）的抑制剂，含有它们的药物组合物及其作为用于治疗和/或预防炎性疾病及相关病症的药物的用途。 A，M，W，R 1，R 2，R 6，R 7具有在说明书中给出的含义。

公开(公告)号：US20120309738A1

公开(公告)日：2012-12-06

申请号：US13314565

申请日：2011-12-08

申请人： Henning Priepke ,  Raimund Kuelzer ,  Juergen Mack ,  Roland Pfau ,  Dirk Stenkamp ,  Benjamin Pelcman ,  Robert Roenn ,  Dimitrijs Lubriks ,  Edgars Suna

发明人： Henning Priepke ,  Raimund Kuelzer ,  Juergen Mack ,  Roland Pfau ,  Dirk Stenkamp ,  Benjamin Pelcman ,  Robert Roenn ,  Dimitrijs Lubriks ,  Edgars Suna

IPC分类号： A61K31/497 ,  A61K31/454 ,  C07D403/10 ,  A61K31/4184 ,  C07D413/10 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/4709 ,  C07D409/14 ,  C07D405/14 ,  C07D417/14 ,  A61K31/427 ,  C07D403/14 ,  C07D235/30 ,  C07D401/14 ,  A61K31/4439 ,  A61K31/422 ,  C07D413/14 ,  A61K31/4545 ,  A61P29/00 ,  C07D401/10

CPC分类号： C07D403/04 ,  C07D235/30 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

摘要： This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), to pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R3, R4, R6, R2, R7, R8, R9, Ra, Rb have meanings given in the description.

摘要翻译： 本发明涉及式I化合物，其用作微粒体前列腺素E2合成酶-1（mPGES-1）的抑制剂，含有它们的药物组合物及其作为治疗和/或预防炎性疾病和相关病症的药物的用途 。 A，M，W，R 1，R 2，R 3，R 4，R 6，R 2，R 7，R 8，R 9，R a，R b具有在说明书中给出的含义。

公开(公告)号：US20100004301A1

公开(公告)日：2010-01-07

申请号：US12518370

申请日：2007-12-12

申请人： Benjamin Pelcman ,  Kristofer Olofsson ,  Ivars Kalvins ,  Edgars Suna ,  Vita Ozola ,  Wesley Schaal

发明人： Benjamin Pelcman ,  Kristofer Olofsson ,  Ivars Kalvins ,  Edgars Suna ,  Vita Ozola ,  Wesley Schaal

IPC分类号： A61K31/423 ,  C07D263/56

CPC分类号： C07D263/57

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。

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).

公开(公告)号：US20120309755A1

公开(公告)日：2012-12-06

申请号：US13314574

申请日：2011-12-08

申请人： Henning Priepke ,  Henri Doods ,  Raimund Kuelzer ,  Roland Pfau ,  Dirk Stenkamp ,  Benjamin Pelcman ,  Robert Roenn ,  Dimitrijs Lubriks ,  Edgars Suna

发明人： Henning Priepke ,  Henri Doods ,  Raimund Kuelzer ,  Roland Pfau ,  Dirk Stenkamp ,  Benjamin Pelcman ,  Robert Roenn ,  Dimitrijs Lubriks ,  Edgars Suna

IPC分类号： C07D471/04 ,  A61K31/5377 ,  A61P29/00 ,  A61K31/437

CPC分类号： C07D471/04

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. A, L, M, W, R1, R2, R3, R4, R6, R7, Ra, Rb have meanings given in the description.

摘要翻译： 本发明涉及式I化合物，其用作微粒体前列腺素E2合酶-1（mPGES-1）的抑制剂，含有它们的药物组合物及其作为用于治疗和/或预防炎性疾病及相关病症的药物的用途。 A，L，M，W，R 1，R 2，R 3，R 4，R 6，R 7，R a，R b具有说明书中给出的含义。