公开(公告)号：US20080275129A1

公开(公告)日：2008-11-06

申请号：US11885594

申请日：2006-03-06

申请人： Torbjorn Lundstedt ,  Elisabeth Seifert ,  Per Lek ,  Arne Boman ,  Anna Skottner

发明人： Torbjorn Lundstedt ,  Elisabeth Seifert ,  Per Lek ,  Arne Boman ,  Anna Skottner

IPC分类号： A61K31/155 ,  A61P25/00

CPC分类号： A61K31/155

摘要： The invention relates to a method of treating neurological damage, preferably spinal chord injury, said treatment comprising the topical administration of guanabenz. The invention also relates to the use of guanabenz for the preparation of a medicament for the treatment of neurological damage, preferably spinal chord injury, wherein said treatment comprises the topical administration of guanabenz to the site of said neurological damage. The invention is also directed to pharmaceutical compositions comprising guanabenz wherein said compositions are in the form of an aqueous gel or non-aqueous ointment.

摘要翻译： 本发明涉及一种治疗神经损伤的方法，优选脊髓损伤，所述治疗包括局部给予胍那苯。 本发明还涉及胍苯醌用于制备用于治疗神经损伤（优选脊髓损伤）的药物的用途，其中所述治疗包括将神经系统局部施用于所述神经损伤部位。 本发明还涉及包含胍苯甲酸酯的药物组合物，其中所述组合物为水性凝胶或非水性软膏剂的形式。

公开(公告)号：US20120190751A1

公开(公告)日：2012-07-26

申请号：US13388174

申请日：2010-07-30

申请人： Niklas Palmqvist ,  Anders Sjödin ,  Christina Wenglén ,  Christofer Flood ,  Lennart Lundberg ,  Elisabeth Seifert ,  Per Lek ,  Arne Boman

发明人： Niklas Palmqvist ,  Anders Sjödin ,  Christina Wenglén ,  Christofer Flood ,  Lennart Lundberg ,  Elisabeth Seifert ,  Per Lek ,  Arne Boman

IPC分类号： A61K31/155 ,  A61P19/02 ,  A61P25/00 ,  A61P29/00

CPC分类号： A61K31/385 ,  A61K31/155 ,  A61K31/36

摘要： The present invention relates to the use of benzylideneaminoguanidines for the treatment of inflammation and pain. In one preferred embodiment, the invention relates to the use of N-(2-chloro-3,4-dimethoxybenzylideneamino)guanidine for the treatment of rheumatoid arthritis.

摘要翻译： 本发明涉及亚苄氨基鸟嘌呤用于治疗炎症和疼痛的用途。 在一个优选的实施方案中，本发明涉及N-（2-氯-3,4-二甲氧基亚苄基氨基）胍用于治疗类风湿性关节炎的用途。

公开(公告)号：US20100098629A1

公开(公告)日：2010-04-22

申请号：US12514634

申请日：2007-11-09

申请人： Torbjorn Lundstedt ,  Elisabeth Seifert ,  Per Lek ,  Arne Boman

发明人： Torbjorn Lundstedt ,  Elisabeth Seifert ,  Per Lek ,  Arne Boman

IPC分类号： A61K31/404 ,  C07D209/14 ,  A61K51/04 ,  A61P29/00 ,  A61P19/02 ,  A61P25/00

CPC分类号： C07D209/14

摘要： There are described Compounds of formula (I) in which R3 to R8 are independently selected from hydrogen, halogen, trihaloalkyl, alkyl having 1, 2, 3, 4 or 5 carbon atoms, electron donor groups selected from alkoxy having 1, 2, 3, 4 or 5 carbon atoms, trihaloalkoxy, hydroxy or amino, electron acceptor groups selected from cyano, sulphonic, nitro, or amide; R1 is an optionally substituted phenyl, benzyl or cyclohexyl group; R2 is selected from amino, substituted amino or guanidino groups, Z is a saturated or unsaturated C1-5 hydrocarbon chain, and salts thereof. A process for their preparation and compositions containing them are also described. The Compounds are either agonists or antagonists of a specific adenosine receptor or a number of adenosine receptors and have usefulness for the treatment of inflammation, arthritic conditions, rheumatoid arthritis, Osteoarthritis, mental disorders, or for inducing central nerve regeneration.

摘要翻译： 描述了其中R 3至R 8独立地选自氢，卤素，三卤代烷基，具有1,2,3,4或5个碳原子的烷基的式（I）化合物，选自具有1,2,3或4个碳原子的烷氧基的电子给体基团 4或5个碳原子，三卤代烷氧基，羟基或氨基，选自氰基，磺酸，硝基或酰胺的电子受体基团; R1是任选取代的苯基，苄基或环己基; R2选自氨基，取代的氨基或胍基，Z是饱和或不饱和的C 1-5烃链及其盐。 还描述了其制备方法和含有它们的组合物。 化合物是特定腺苷受体的激动剂或拮抗剂或多种腺苷受体，并且可用于治疗炎症，关节炎病症，类风湿性关节炎，骨关节炎，精神障碍或诱导中枢神经再生。

公开(公告)号：US20100056641A1

公开(公告)日：2010-03-04

申请号：US12518335

申请日：2007-12-13

申请人： Torbjorn Lundstedt ,  Elisabeth Seifert ,  Per Lek ,  Arne Boman

发明人： Torbjorn Lundstedt ,  Elisabeth Seifert ,  Per Lek ,  Arne Boman

IPC分类号： A61K31/155 ,  C07C277/08 ,  A61P37/06

CPC分类号： C07D339/08 ,  C07C281/18 ,  C07C323/48

摘要： There are described compounds of general formula (I) and isomeric forms thereof wherein n is 0, 1, 2 or 3, saturated or unsaturated; most preferably at least one of R1 to R5 represents halogen; at least one of R1, R2, R3, R4 and R5 is selected from —S—R or —COOR, or two or more Of R1-R5 comprise a linking group such as —S—(CH2)mS—, where m is 1, 2 or 3 and R is selected from alkyl having 1 to 5 carbon atoms, cycloalkyl having 3-6 carbon atoms, hydroxy, and aryl having 6 to 10 carbon atoms, such groups being optionally substituted, and when R1 is selected from —S—R, then at least one of R2, R3 and R5 is most preferably selected from halogen; and R1, R2, R3, R4 and R5 are otherwise the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and pharmacologically acceptable salts thereof. Compounds described have activity on the melanocortin receptors and have application in the treatment of a wide range of inflammatory, arthritic or central nerve regeneration conditions.

摘要翻译： 描述了通式（I）的化合物及其异构体形式，其中n为0,1,2或3，饱和或不饱和; 最优选R 1至R 5中的至少一个表示卤素; R 1，R 2，R 3，R 4和R 5中的至少一个选自-S-R或-COOR，或者R 1 -R 5中的两个或多个包含连接基团，例如-S-（CH 2）m S-，其中m是 1,2或3，并且R选自具有1至5个碳原子的烷基，具有3-6个碳原子的环烷基，羟基和具有6至10个碳原子的芳基，这些基团任选被取代，并且当R 1选自 - S-R，则R 2，R 3和R 5中的至少一个最优选选自卤素; R 1，R 2，R 3，R 4和R 5相同或不同，选自氢，卤素，具有1至5个碳原子的烷基，电子给体基团如具有1-5个碳原子的烷氧基或羟基，电子受体基团 选自氰基，硝基，三氟烷基或酰胺; 烷基氨基，苯甲酰氧基，硝酰基，苯基或磺基; 及其药理学上可接受的盐。 所描述的化合物对黑皮质素受体具有活性，并且可用于治疗广泛的炎性，关节炎或中枢神经再生条件。

公开(公告)号：US08372878B2

公开(公告)日：2013-02-12

申请号：US12518335

申请日：2007-12-13

申请人： Torbjorn Lundstedt ,  Elisabeth Seifert ,  Per Lek ,  Arne Boman

发明人： Torbjorn Lundstedt ,  Elisabeth Seifert ,  Per Lek ,  Arne Boman

IPC分类号： A61K31/38 ,  C07D339/00

CPC分类号： C07D339/08 ,  C07C281/18 ,  C07C323/48

摘要： There are described compounds of general formula (I) and isomeric forms thereof wherein n is 0, 1, 2 or 3, saturated or unsaturated; most preferably at least one of R1 to R5 represents halogen; at least one of R1, R2, R3, R4 and R5 is selected from —S—R or —COOR, or two or more Of R1-R5 comprise a linking group such as —S—(CH2)mS—, where m is 1, 2 or 3 and R is selected from alkyl having 1 to 5 carbon atoms, cycloalkyl having 3-6 carbon atoms, hydroxy, and aryl having 6 to 10 carbon atoms, such groups being optionally substituted, and when R1 is selected from —S—R, then at least one of R2, R3 and R5 is most preferably selected from halogen; and R1, R2, R3, R4 and R5 are otherwise the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and pharmacologically acceptable salts thereof. Compounds described have activity on the melanocortin receptors and have application in the treatment of a wide range of inflammatory, arthritic or central nerve regeneration conditions.

摘要翻译： 描述了通式（I）的化合物及其异构体形式，其中n为0,1,2或3，饱和或不饱和; 最优选R 1至R 5中的至少一个表示卤素; R 1，R 2，R 3，R 4和R 5中的至少一个选自-S-R或-COOR，或者R 1 -R 5中的两个或多个包含连接基团，例如-S-（CH 2）m S-，其中m是 1,2或3，并且R选自具有1至5个碳原子的烷基，具有3-6个碳原子的环烷基，羟基和具有6至10个碳原子的芳基，这些基团任选被取代，并且当R 1选自 - S-R，则R 2，R 3和R 5中的至少一个最优选选自卤素; R 1，R 2，R 3，R 4和R 5相同或不同，选自氢，卤素，具有1至5个碳原子的烷基，电子给体基团如具有1-5个碳原子的烷氧基或羟基，电子受体基团 选自氰基，硝基，三氟烷基或酰胺; 烷基氨基，苯甲酰氧基，硝酰基，苯基或磺基; 及其药理学上可接受的盐。 所描述的化合物对黑皮质素受体具有活性，并且可用于治疗广泛的炎性，关节炎或中枢神经再生条件。

公开(公告)号：US08227502B2

公开(公告)日：2012-07-24

申请号：US12514634

申请日：2007-11-09

申请人： Torbjorn Lundstedt ,  Elisabeth Seifert ,  Per Lek ,  Arne Boman

发明人： Torbjorn Lundstedt ,  Elisabeth Seifert ,  Per Lek ,  Arne Boman

IPC分类号： A61K31/404 ,  C07D209/14

CPC分类号： C07D209/14

摘要： There are described Compounds of formula (I) in which R3 to R8 are independently selected from hydrogen, halogen, trihaloalkyl, alkyl having 1, 2, 3, 4 or 5 carbon atoms, electron donor groups selected from alkoxy having 1, 2, 3, 4 or 5 carbon atoms, trihaloalkoxy, hydroxy or amino, electron acceptor groups selected from cyano, sulphonic, nitro, or amide; R1 is an optionally substituted phenyl, benzyl or cyclohexyl group; R2 is selected from amino, substituted amino or guanidino groups, Z is a saturated or unsaturated C1-5 hydrocarbon chain, and salts thereof. A process for their preparation and compositions containing them are also described. The Compounds are either agonists or antagonists of a specific adenosine receptor or a number of adenosine receptors and have usefulness for the treatment of inflammation, arthritic conditions, rheumatoid arthritis, osteoarthritis, mental disorders, or for inducing central nerve regeneration.

摘要翻译： 描述了其中R 3至R 8独立地选自氢，卤素，三卤代烷基，具有1,2,3,4或5个碳原子的烷基的式（I）化合物，选自具有1,2,3或4个碳原子的烷氧基的电子给体基团 4或5个碳原子，三卤代烷氧基，羟基或氨基，选自氰基，磺酸，硝基或酰胺的电子受体基团; R1是任选取代的苯基，苄基或环己基; R2选自氨基，取代的氨基或胍基，Z是饱和或不饱和的C 1-5烃链及其盐。 还描述了其制备方法和含有它们的组合物。 化合物是特定腺苷受体的激动剂或拮抗剂或多种腺苷受体，并且可用于治疗炎症，关节炎病症，类风湿性关节炎，骨关节炎，精神障碍或用于诱导中枢神经再生。