公开(公告)号：US08148429B2

公开(公告)日：2012-04-03

申请号：US11639190

申请日：2006-12-15

申请人： Torbjörn Lundstedt ,  Anna Skottner ,  Elisabeth Seifert

发明人： Torbjörn Lundstedt ,  Anna Skottner ,  Elisabeth Seifert

IPC分类号： A61K31/155 ,  A01N37/52 ,  A01N37/30

CPC分类号： C07C281/16 ,  A61K31/155 ,  C07C53/10 ,  C07C309/30 ,  C07C309/46 ,  C07D317/58

摘要： The present invention relates to the use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is H or OH; R1, R2, R3, R4 and R5 are 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 the pharmacologically active salts thereof.

摘要翻译： 本发明涉及通式（I）的化合物作为黑皮质素受体的配体和/或用于治疗黑皮质素系统中的病症的用途：其中X是H或OH; R 1，R 2，R 3，R 4和R 5相同或不同，选自氢，卤素，具有1-5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 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; 及其药理学活性盐。

公开(公告)号：US20110015437A1

公开(公告)日：2011-01-20

申请号：US12892402

申请日：2010-09-28

申请人： Torbjörn Lundstedt ,  Anna Skottner ,  Elisabeth Seifert

发明人： Torbjörn Lundstedt ,  Anna Skottner ,  Elisabeth Seifert

IPC分类号： C07C281/16 ,  C07C53/10

CPC分类号： C07C281/16 ,  A61K31/155 ,  C07C53/10 ,  C07C309/30 ,  C07C309/46 ,  C07D317/58

摘要： The present invention relates to the use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is H or OH; R1, R2, R3, R4 and R5 are 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 the pharmacologically active salts thereof.

摘要翻译： 本发明涉及通式（I）的化合物作为黑皮质素受体的配体和/或用于治疗黑皮质素系统中的病症的用途：其中X是H或OH; R 1，R 2，R 3，R 4和R 5相同或不同，选自氢，卤素，具有1-5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; 及其药理学活性盐。

公开(公告)号：US07186748B2

公开(公告)日：2007-03-06

申请号：US10484444

申请日：2002-08-06

申请人： Torbjörn Lundstedt ,  Anna Skottner ,  Arne Boman ,  Per Andersson ,  Elisabeth Seifert ,  Victor Andrianov

发明人： Torbjörn Lundstedt ,  Anna Skottner ,  Arne Boman ,  Per Andersson ,  Elisabeth Seifert ,  Victor Andrianov

IPC分类号： A61K31/402 ,  C07D207/335

CPC分类号： C07D207/335 ,  C07D207/34 ,  C07D207/36 ,  C07D207/38 ,  C07D207/42

摘要： The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH2)n where n is 0, 1 or 2; R1, R2, R3, R4 and R5 may be the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, alkylsulphonyloxy, cyano, nitro, trihaloalkyl, sulpho or one of the structures given in Scheme 1; or two of R1, R2, R3, R4 and R5 may together form a methylenedioxy or ethylenedioxy moiety; R6, R7, R8 and R9 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, amines (primary, secondary or tertiary) having 0, 1 or 2 carbon atoms, cyano, nitro, trihaloalkyl, amide or sulpho, and z where shown represents the point of attachment of the residue to the phenyl or pyrrole ring; and the pharmacologically active salts thereof.

摘要翻译： 本发明提供了作为黑皮质素受体的配体和/或用于治疗黑皮质素系统中的病症的通式（I）的新化合物：其中X是（CH 2） / SUB>其中n为0,1或2; R 1，R 2，R 3，R 4和R 5可以是 羟基，烷基磺酰氧基，氰基，硝基，三卤代烷基，磺基或方案1中给出的结构之一;其中R 1，R 2， 或R 1，R 2，R 3，R 4和R 5中的两个， 可以一起形成亚甲二氧基或亚乙二氧基部分; R 6，R 7，R 8和R 9相同或不同，并且选自氢， 卤素，具有1至5个碳原子的烷基，具有1至5个碳原子的烷氧基，羟基，具有0,1或2个碳原子的胺（伯，仲或叔），氰基，硝基，三卤代烷基，酰胺或磺基，和z 显示残基与苯基或吡咯环的连接点; 及其药理学活性盐。

公开(公告)号：US08410174B2

公开(公告)日：2013-04-02

申请号：US13426096

申请日：2012-03-21

申请人： Torbjörn Lundstedt ,  Anna Skottner ,  Elisabeth Seifert

发明人： Torbjörn Lundstedt ,  Anna Skottner ,  Elisabeth Seifert

IPC分类号： A61K31/155 ,  A01N37/52 ,  A01N37/30

CPC分类号： C07C281/16 ,  A61K31/155 ,  C07C53/10 ,  C07C309/30 ,  C07C309/46 ,  C07D317/58

摘要： The present invention relates to the use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is H or OH; R1, R2, R3, R4 and R5 are 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 the pharmacologically active salts thereof.

摘要翻译： 本发明涉及通式（I）的化合物作为黑皮质素受体的配体和/或用于治疗黑皮质素系统中的病症的用途：其中X是H或OH; R 1，R 2，R 3，R 4和R 5相同或不同，选自氢，卤素，具有1-5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 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; 及其药理学活性盐。

公开(公告)号：US08309609B2

公开(公告)日：2012-11-13

申请号：US12892402

申请日：2010-09-28

申请人： Torbjörn Lundstedt ,  Anna Skottner ,  Elisabeth Seifert

发明人： Torbjörn Lundstedt ,  Anna Skottner ,  Elisabeth Seifert

IPC分类号： A61K31/55 ,  A01N37/52 ,  A01N37/30

CPC分类号： C07C281/16 ,  A61K31/155 ,  C07C53/10 ,  C07C309/30 ,  C07C309/46 ,  C07D317/58

摘要： The present invention relates to the use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is H or OH; R1, R2, R3, R4 and R5 are 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 the pharmacologically active salts thereof.

公开(公告)号：US07442807B2

公开(公告)日：2008-10-28

申请号：US11374956

申请日：2006-03-15

申请人： Torbjörn Lundstedt ,  Anna Skottner ,  Arne Boman ,  Per Andersson ,  Elisabeth Seifert ,  Victor Andrianov

发明人： Torbjörn Lundstedt ,  Anna Skottner ,  Arne Boman ,  Per Andersson ,  Elisabeth Seifert ,  Victor Andrianov

IPC分类号： C07D207/325 ,  C07D207/335 ,  C07D413/10

CPC分类号： C07D207/335 ,  C07D207/34 ,  C07D207/36 ,  C07D207/38 ,  C07D207/42

摘要： The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH2)n where n is 0, 1 or 2; R1, R2, R3, R4 and R5 may be the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, alkylsulphonyloxy, cyano, nitro, trihaloalkyl, sulpho or one of the structures given in Scheme 1; or two of R1, R2, R3, R4 and R5 may together form a methylenedioxy or ethylenedioxy moiety; R6, R7, R8 and R9 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, amines (primary, secondary or tertiary) having 0, 1 or 2 carbon atoms, cyano, nitro, trihaloalkyl, amide or sulpho, and z where shown represents the point of attachment of the residue to the phenyl or pyrrole ring; and the pharmacologically active salts thereof.

摘要翻译： 本发明提供了作为黑皮质素受体的配体和/或用于治疗黑皮质素系统中的病症的通式（I）的新化合物：其中X是（CH 2） / SUB>其中n为0,1或2; R 1，R 2，R 3，R 4和R 5可以是 羟基，烷基磺酰氧基，氰基，硝基，三卤代烷基，磺基或方案1中给出的结构之一;其中R 1，R 2， 或R 1，R 2，R 3，R 4和R 5中的两个， 可以一起形成亚甲二氧基或亚乙二氧基部分; R 6，R 7，R 8和R 9相同或不同，并且选自氢， 卤素，具有1至5个碳原子的烷基，具有1至5个碳原子的烷氧基，羟基，具有0,1或2个碳原子的胺（伯，仲或叔），氰基，硝基，三卤代烷基，酰胺或磺基，和z 显示残基与苯基或吡咯环的连接点; 及其药理学活性盐。

公开(公告)号：US20090018183A1

公开(公告)日：2009-01-15

申请号：US12232399

申请日：2008-09-17

申请人： Torbjorn Lundstedt ,  Anna Skottner ,  Arne Boman ,  Per Andersson ,  Elisabeth Seifert ,  Victor Andrianov

发明人： Torbjorn Lundstedt ,  Anna Skottner ,  Arne Boman ,  Per Andersson ,  Elisabeth Seifert ,  Victor Andrianov

IPC分类号： A61K31/40 ,  A61P3/00 ,  A61P25/00

CPC分类号： C07D207/335 ,  C07D207/34 ,  C07D207/36 ,  C07D207/38 ,  C07D207/42

摘要： The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH2)n where n is 0, 1 or 2; R1, R2, R3, R4 and R5 may be the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, alkylsulphonyloxy, cyano, nitro, trihaloalkyl, sulpho or one of the structures given in Scheme 1; or two of R1, R2, R3, R4 and R5 may together form a methylenedioxy or ethylenedioxy moiety; R6, R7, R8 and R9 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, amines (primary, secondary or tertiary) having 0, 1 or 2 carbon atoms, cyano, nitro, trihaloalkyl, amide or sulpho, and z where shown represents the point of attachment of the residue to the phenyl or pyrrole ring; and the pharmacologically active salts thereof.

摘要翻译： 本发明提供了作为黑皮质素受体配体和/或用于治疗黑皮质素系统中的病症的通式（I）的新化合物：其中X是（CH 2）n，其中n是0,1或2; R 1，R 2，R 3，R 4和R 5可以相同或不同，并且选自氢，卤素，具有1-5个碳原子的烷基，具有1至5个碳原子的烷氧基，羟基，烷基磺酰氧基，氰基，硝基，三卤代烷基，磺基 或方案1中给出的结构之一; 或者R 1，R 2，R 3，R 4和R 5中的两个可以一起形成亚甲二氧基或亚乙二氧基部分; R 6，R 7，R 8和R 9相同或不同，并且选自氢，卤素，具有1至5个碳原子的烷基，具有1至5个碳原子的烷氧基，羟基，具有0,1 或2个碳原子，氰基，硝基，三卤代烷基，酰胺或磺基，z表示残基与苯基或吡咯环的连接点; 及其药理学活性盐。

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：US20070088085A1

公开(公告)日：2007-04-19

申请号：US11639190

申请日：2006-12-15

申请人： Torbjorn Lundstedt ,  Anna Skottner ,  Elisabeth Seifert

发明人： Torbjorn Lundstedt ,  Anna Skottner ,  Elisabeth Seifert

IPC分类号： A61K31/205 ,  A61K31/155

CPC分类号： C07C281/16 ,  A61K31/155 ,  C07C53/10 ,  C07C309/30 ,  C07C309/46 ,  C07D317/58

摘要： The present invention relates to the use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is H or OH; R1, R2, R3, R4 and R5 are 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 the pharmacologically active salts thereof.

公开(公告)号：US20060148798A1

公开(公告)日：2006-07-06

申请号：US11374956

申请日：2006-03-15

申请人： Torbjorn Lundstedt ,  Anna Skottner ,  Arne Boman ,  Per Andersson ,  Elisabeth Seifert ,  Victor Andrianov

发明人： Torbjorn Lundstedt ,  Anna Skottner ,  Arne Boman ,  Per Andersson ,  Elisabeth Seifert ,  Victor Andrianov

IPC分类号： A61K31/5377 ,  A61K31/4025 ,  C07D413/02 ,  C07D403/02 ,  C07D207/30

CPC分类号： C07D207/335 ,  C07D207/34 ,  C07D207/36 ,  C07D207/38 ,  C07D207/42

摘要： The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH2)n where n is 0, 1 or 2; R1, R2, R3, R4 and R5 may be the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, alkylsulphonyloxy, cyano, nitro, trihaloalkyl, sulpho or one of the structures given in Scheme 1; or two of R1, R2, R3, R4 and R5 may together form a methylenedioxy or ethylenedioxy moiety; R6, R7, R8 and R9 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, amines (primary, secondary or tertiary) having 0, 1 or 2 carbon atoms, cyano, nitro, trihaloalkyl, amide or sulpho, and z where shown represents the point of attachment of the residue to the phenyl or pyrrole ring; and the pharmacologically active salts thereof.

摘要翻译： 本发明提供了作为黑皮质素受体的配体和/或用于治疗黑皮质素系统中的病症的通式（I）的新化合物：其中X是（CH 2） / SUB>其中n为0,1或2; R 1，R 2，R 3，R 4和R 5可以是 羟基，烷基磺酰氧基，氰基，硝基，三卤代烷基，磺基或方案1中给出的结构之一;其中R 1，R 2， 或R 1，R 2，R 3，R 4和R 5中的两个， 可以一起形成亚甲二氧基或亚乙二氧基部分; R 6，R 7，R 8和R 9相同或不同，并且选自氢， 卤素，具有1至5个碳原子的烷基，具有1至5个碳原子的烷氧基，羟基，具有0,1或2个碳原子的胺（伯，仲或叔），氰基，硝基，三卤代烷基，酰胺或磺基，和z 显示残基与苯基或吡咯环的连接点; 及其药理学活性盐。