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1. 发明申请

US20090069242A1 THERAPEUTICALLY ACTIVE ALPHA MSH ANALOGUES 失效
标题翻译：治疗活性阿尔法MSH类似物
公开(公告)号：US20090069242A1
公开(公告)日：2009-03-12
申请号：US12064923
申请日：2005-08-26
申请人： Thomas E.N. Jonassen , Soren Nielsen , Jorgen Frokiaer , Bjarne Due Larsen
发明人： Thomas E.N. Jonassen , Soren Nielsen , Jorgen Frokiaer , Bjarne Due Larsen
IPC分类号： A61K38/00 , C07K7/00 , A61P9/00
CPC分类号： C07K7/08 , C07K14/685 , C07K2319/31
摘要： The invention describes peptide analogues of a-melanocyte-stimulating hormone (a-MSH), which posses an increased efficacy compared to the native α-MSH peptide. The α-MSH analogues exhibit increased anti-inflammatory effects and increased capability to prevent ischemic conditions compared to α-MSH. The invention further discloses use of the peptides for the manufacture of pharmaceutical compositions for the treatment or prophylaxis of a condition in the tissue of one or more organs of a mammal, and moreover pharmaceutical compositions.
摘要翻译：本发明描述了与天然α-MSH肽相比具有增加的功效的α-黑素细胞刺激激素（a-MSH）的肽类似物。与α-MSH相比，α-MSH类似物表现出增加的抗炎作用和增强的预防缺血状况的能力。本发明进一步公开了该肽用于制备用于治疗或预防哺乳动物的一种或多种器官的组织中的病症的药物组合物的用途，以及药物组合物。

2. 发明授权

US07186748B2 N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands 失效
标题翻译： N-苯基吡咯胍衍生物作为黑皮质素受体配体
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。

3. 发明申请

US20060148798A1 N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands 失效
标题翻译： N-苯基吡咯胍衍生物作为黑皮质素受体配体
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。

4. 发明授权

US08058306B2 Phenyl pyrrole aminoguanidine derivatives 有权
标题翻译：苯基吡咯氨基胍衍生物
公开(公告)号：US08058306B2
公开(公告)日：2011-11-15
申请号：US12304065
申请日：2007-06-11
申请人： Arne Boman , Thomas Engelbrecht Norkild Jonassen , Torbjorn Lundstedt
发明人： Arne Boman , Thomas Engelbrecht Norkild Jonassen , Torbjorn Lundstedt
IPC分类号： A61K31/40 , C07D207/30
CPC分类号： C07D207/42 , C07D207/335 , C07D207/34 , C07D207/36 , C07D207/38 , C07D207/416
摘要： The present invention relates to phenyl pyrrole aminoguanidine derivatives of the general formula (I): (I) including tautomeric forms thereof, wherein n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof. The present invention further relates to the use of such phenyl pyrrole aminoguanidine derivatives for the treatment of diseases associated with the melanocortin receptors or related systems, e.g. the melanocyte stimulating hormones.
摘要翻译：本发明涉及通式（I）的苯基吡咯氨基胍衍生物：（I）包括其互变异构形式，其中n为1,2或3; 或其药学上可接受的盐。本发明还涉及这种苯基吡咯氨基胍衍生物用于治疗与黑皮质素受体或相关系统有关的疾病的用途，例如，黑素细胞刺激激素。

5. 发明申请

US20090018183A1 N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands 审中-公开
标题翻译： N-苯基吡咯胍衍生物作为黑皮质素受体配体
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。

6. 发明授权

US07008925B1 Melanocortin 1 receptor selective compounds 失效
标题翻译：黑皮质素1受体选择性化合物
公开(公告)号：US07008925B1
公开(公告)日：2006-03-07
申请号：US09674733
申请日：1999-05-05
申请人： Michael Szardenings , Ruta Muceniece , Ilze Mutule , Felikss Mutulis , Jarl Wikberg
发明人： Michael Szardenings , Ruta Muceniece , Ilze Mutule , Felikss Mutulis , Jarl Wikberg
IPC分类号： A61K38/00
CPC分类号： C07K14/685 , A61K38/00
摘要： A compound of general formula (1) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are H or methyl, R13, R14, R15 and R16 are H or alkyl, wherein L1 and L2 are linkers selected from single bond, methyl, ethyl, wherein R19, R20 and R21 are H or —CH2X, NT is selected from H, hydroxyl, alkyl, aminoacid, aminoacid analogue, polypeptide and functional group, CT is selected from hydrogen, hydroxyl, alkyl, aminoacid, aminoacid analogue, polypeptide and functional group shows high selectivity and high affinity for MC1-receptors in combination with effective stimulation or inhibiton of cAMP formation in MC1-receptor expressing cells but low affinity for other subtypes of MC-receptors and may be used to treat a wide range of inflammatory conditions. Also disclosed is a DNA molecule and a corresponding vector encoding the compound, a fusion protein comprising a copy of it, a vector comprising DNA encoding the fusion protein, and a pharmaceutical composition comprising the compound.
摘要翻译：通式（1）的化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 11和R 12为H或甲基，R 13，R 14，R 15和R 16为H或烷基， L1和L2是选自单键，甲基，乙基的连接体，其中R 19，R 20和R 21是H或-CH 2 X，NT选自H，羟基，烷基，氨基酸，氨基酸类似物，多肽和官能团，CT选自氢，羟基，烷基，氨基酸，氨基酸类似物，多肽和官能团对MC1受体具有高选择性和高亲和力，并与MC1受体表达细胞中有效刺激或抑制cAMP形成相结合但对MC-受体的其它亚型的亲和力低，可用于治疗广泛的炎性病症。还公开了编码该化合物的DNA分子和相应的载体，包含其拷贝的融合蛋白，包含编码融合蛋白的DNA的载体和包含该化合物的药物组合物。

7. 发明申请

US20110082183A1 PHENYL PYRROLE AMINOGUANIDINE DERIVATIVES 有权
标题翻译：苯胺微量氨基嘌呤衍生物
公开(公告)号：US20110082183A1
公开(公告)日：2011-04-07
申请号：US12304065
申请日：2007-06-11
申请人： Arne Boman , Thomas Engelbrecht Norkild Jonassen , Torbjorn Lundstedt
发明人： Arne Boman , Thomas Engelbrecht Norkild Jonassen , Torbjorn Lundstedt
IPC分类号： A61K31/40 , C07D207/34 , A61P3/10 , C07D207/42 , A61P15/00 , A61P15/10 , A61P3/04 , A61P9/00 , A61P25/00
CPC分类号： C07D207/42 , C07D207/335 , C07D207/34 , C07D207/36 , C07D207/38 , C07D207/416
摘要： The present invention relates to phenyl pyrrole aminoguanidine derivatives of the general formula (I): (I) including tautomeric forms thereof, wherein n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof. The present invention further relates to the use of such phenyl pyrrole aminoguanidine derivatives for the treatment of diseases associated with the melanocortin receptors or related systems, e.g. the melanocyte stimulating hormones.
摘要翻译：本发明涉及通式（I）的苯基吡咯氨基胍衍生物：（I）包括其互变异构形式，其中n为1,2或3; 或其药学上可接受的盐。本发明还涉及这种苯基吡咯氨基胍衍生物用于治疗与黑皮质素受体或相关系统有关的疾病的用途，例如，黑素细胞刺激激素。

8. 发明授权

US07662782B2 Melanocortin 1 receptor selective compounds 失效
标题翻译：黑皮质素1受体选择性化合物
公开(公告)号：US07662782B2
公开(公告)日：2010-02-16
申请号：US11319584
申请日：2005-12-29
申请人： Michael Szardenings , Ruta Muceniece , Ilze Mutule , Felikss Mutulis , Jarl Wikberg
发明人： Michael Szardenings , Ruta Muceniece , Ilze Mutule , Felikss Mutulis , Jarl Wikberg
IPC分类号： A61K38/00
CPC分类号： C07K14/685 , A61K38/00
摘要： The invention relates to methods of treatment comprising administering a compound of the general formula (1): to a patient or a healthy individual.
摘要翻译：本发明涉及治疗方法，其包括向患者或健康个体施用通式（1）的化合物：

9. 发明授权

US07442807B2 N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands 失效
标题翻译： N-苯基吡咯胍衍生物作为黑皮质素受体配体
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。

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