公开(公告)号：US20090076004A1

公开(公告)日：2009-03-19

申请号：US11795628

申请日：2005-12-22

申请人： Benjamin Pelcman ,  Kristofer Olofsson ,  Martins Katkevics ,  Vita Ozola ,  Edgars Suna ,  Ivars Kalvins ,  Peteris Trapencieris ,  Dace Katkevica ,  Wesley Schaal

发明人： Benjamin Pelcman ,  Kristofer Olofsson ,  Martins Katkevics ,  Vita Ozola ,  Edgars Suna ,  Ivars Kalvins ,  Peteris Trapencieris ,  Dace Katkevica ,  Wesley Schaal

IPC分类号： A61K31/404 ,  C07D209/42 ,  C07D405/02 ,  C07D401/02 ,  C07D403/02 ,  C07D413/02 ,  A61K31/5377 ,  A61K31/4709 ,  A61K31/454 ,  A61K31/437

CPC分类号： C07D401/04 ,  C07D209/42 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04

摘要： There is provided compounds of formula (I), wherein X1, Q, T, Y, R1, R2, R3, R4 and R5 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 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，其中X 1，Q，T，Y，R 1，R 2，R 3，R 4和R 5具有本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MAPEG家族成员的活性抑制，特别是治疗炎症的疾病。

公开(公告)号：US20090048285A1

公开(公告)日：2009-02-19

申请号：US11795573

申请日：2006-01-19

申请人： Benjamin Pelcman ,  Kristofer Olofsson ,  Pavels Arsenjans ,  Ivars Kalvins ,  Edgars Suna ,  Martins Katkevics ,  Marina Madre ,  Vita Ozola

发明人： Benjamin Pelcman ,  Kristofer Olofsson ,  Pavels Arsenjans ,  Ivars Kalvins ,  Edgars Suna ,  Martins Katkevics ,  Marina Madre ,  Vita Ozola

IPC分类号： A61K31/437 ,  C07D471/04 ,  A61P25/00 ,  A61P37/00 ,  A61P31/00

CPC分类号： C07D471/04

摘要： There is provided compounds of formula (I), wherein X1, R1, R2, Y1, Y2, Y3 and Y4 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 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，其中X 1，R 1，R 2，Y 1，Y 2，Y 3和Y 4在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其中抑制 MAPEG家族成员的活性是期望和/或需要的，特别是治疗炎症。

公开(公告)号：US20080249091A1

公开(公告)日：2008-10-09

申请号：US11795627

申请日：2005-12-22

申请人： Benjamin Pelcman ,  Kristofer Olofsson ,  Martins Katkevics ,  Vita Ozola ,  Edgars Suna ,  Ivars Kalvins ,  Peteris Trapencieris

发明人： Benjamin Pelcman ,  Kristofer Olofsson ,  Martins Katkevics ,  Vita Ozola ,  Edgars Suna ,  Ivars Kalvins ,  Peteris Trapencieris

IPC分类号： A61K31/5377 ,  C07D209/42 ,  A61K31/404 ,  C07D413/02 ,  A61P29/00 ,  A61P11/00 ,  C07D401/02 ,  A61K31/4439

CPC分类号： C07D401/04 ,  C07D209/42 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12

摘要： There is provided compounds of formula I, wherein X1, R1, R2, R3, R4, R5 and R6 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 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，其中X 1，R 1，R 2，R 3，R 3，R 3， R 5，R 5和R 6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MAPEG家族成员的活性抑制，特别是治疗炎症的疾病。

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。

公开(公告)号：US20080146616A1

公开(公告)日：2008-06-19

申请号：US11629622

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： A61K31/4439 ,  C07D209/42 ,  C07D401/02 ,  A61P1/00 ,  A61P37/08 ,  A61P29/00 ,  A61K31/405

CPC分类号： C07D401/04 ,  C07D209/42 ,  C07D401/14

摘要： There is provided a compound of formula (I), wherein X, R1, R2, R3, R4, R5 and R6 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： 提供式（I）化合物，其中X，R 1，R 2，R 3，R 4， R 5，R 5和R 6具有本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其中抑制 微粒体前列腺素E合酶-1的活性是期望和/或需要的，特别是在治疗炎症中。

公开(公告)号：US07220752B2

公开(公告)日：2007-05-22

申请号：US10433015

申请日：2001-11-28

申请人： Benjamin Pelcman ,  Annika Gustafsson ,  Philip R. Kym

发明人： Benjamin Pelcman ,  Annika Gustafsson ,  Philip R. Kym

IPC分类号： A61K31/435 ,  A61K31/425 ,  A61K31/36 ,  C07D265/30 ,  C07D211/34 ,  C07D277/30 ,  C07D317/44

CPC分类号： C07D213/30 ,  C07C59/90 ,  C07C69/76 ,  C07C205/35 ,  C07C323/12 ,  C07D277/24 ,  C07D295/088 ,  C07D317/62

摘要： This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in therapy and in the regulation of metabolism, especially lowering blood glucose levels. The compounds referred to are compounds according to the formula 1: wherein the variables are as defined herein.

摘要翻译： 本发明涉及作为肝选择性糖皮质激素受体拮抗剂的新型化合物，制备这些化合物的方法，以及在治疗和调节代谢中尤其是降低血糖水平使用这些化合物的方法。 所指的化合物是根据式1的化合物：其中变量如本文所定义。

公开(公告)号：US06974825B1

公开(公告)日：2005-12-13

申请号：US10628309

申请日：2003-07-29

申请人： Benjamin Pelcman ,  Edward Roberts

发明人： Benjamin Pelcman ,  Edward Roberts

IPC分类号： A61K31/445 ,  A61K31/4468 ,  A61P1/00 ,  A61P25/00 ,  C07D207/14 ,  C07D211/58

CPC分类号： C07D211/58 ,  C07D207/14

摘要： Compounds of general formula (I) 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： 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：US08921405B2

公开(公告)日：2014-12-30

申请号：US13942077

申请日：2013-07-15

申请人： Roland Pfau ,  Kirsten Arndt ,  Henri Doods ,  Klaus Klinder ,  Raimund Kuelzer ,  Dimitrijs Lubriks ,  Juergen Mack ,  Benjamin Pelcman ,  Henning Priepke ,  Robert Roenn ,  Dirk Stenkamp ,  Edgars Suna

发明人： Roland Pfau ,  Kirsten Arndt ,  Henri Doods ,  Klaus Klinder ,  Raimund Kuelzer ,  Dimitrijs Lubriks ,  Juergen Mack ,  Benjamin Pelcman ,  Henning Priepke ,  Robert Roenn ,  Dirk Stenkamp ,  Edgars Suna

IPC分类号： A61K31/4168 ,  C07D235/30 ,  C07D403/12 ,  C07D401/12 ,  C07D409/12 ,  C07D405/12

CPC分类号： C07D235/30 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

摘要： The present invention relates to compounds of general formula I in which A, L, M, Q2, Q3, Q4, R1, R5, Ra, Rb, Rc, W, X, Y, Z1, Z2, Z3 are defined in the description, the salts thereof, particularly the physiologically acceptable salts thereof. The compounds are of potential utility in the treatment and/or prevention of inflammatory diseases and associated conditions, in particular, in the treatment and/or prevention of pain. The invention also relates to the use of such compounds as medicaments, to pharmaceutical compositions containing them, and to their preparation.

摘要翻译： 本发明涉及其中A，L，M，Q2，Q3，Q4，R 1，R 5，R a，R b，R c，W，X，Y，Z 1，Z 2，Z 3在说明书中定义的通式I化合物 ，其盐，特别是其生理上可接受的盐。 该化合物在治疗和/或预防炎性疾病和相关病症，特别是治疗和/或预防疼痛中具有潜在的用途。 本发明还涉及这些化合物作为药物，含有它们的药物组合物及其制备的用途。

公开(公告)号：US08486968B2

公开(公告)日：2013-07-16

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： A01N43/42 ,  A61K31/44 ,  A61K31/135 ,  A01N33/18 ,  A61K31/04

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, 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。