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20 条记录 (耗时 0.026 秒)

    Use of benzylideneaminoguanidines and hydroxyguanidines as melanocortin receptor ligands
    12.
    发明申请
    Use of benzylideneaminoguanidines and hydroxyguanidines as melanocortin receptor ligands 审中-公开
    使用亚苄氨基鸟嘌呤和羟基胍来作为黑皮质素受体配体

    公开(公告)号：US20070231267A1

    公开(公告)日：2007-10-04

    申请号：US11798669

    申请日：2007-05-16

    申请人： Torbjorn Lundstedt ,  Anna Skottner ,  Elisabeth Seifert

    发明人： Torbjorn Lundstedt ,  Anna Skottner ,  Elisabeth Seifert

    IPC分类号： A61K31/155 ,  A61K31/205 ,  A61K49/00

    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。

    Amides acting on the adenosine receptors
    13.
    发明授权
    Amides acting on the adenosine receptors 有权
    作用于腺苷受体的酰胺

    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。

    Novel Amides Acting on the Adenosine Receptors
    15.
    发明申请
    Novel Amides Acting on the Adenosine Receptors 有权
    新型酰胺作用于腺苷受体

    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。

    Novel Aminoguanidines as Melanocortin Receptor Ligands
    16.
    发明申请
    Novel Aminoguanidines as Melanocortin Receptor Ligands 有权
    新型氨基胍作为黑皮质素受体配体

    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。

    2,4-Diamino quinazoline and pyridopyrimidine ester derivatives as dihydrofolate reductase inhibitors
    17.
    发明申请
    2,4-Diamino quinazoline and pyridopyrimidine ester derivatives as dihydrofolate reductase inhibitors 审中-公开
    2,4-二氨基喹唑啉和吡啶并嘧啶酯衍生物作为二氢叶酸还原酶抑制剂

    公开(公告)号：US20060111376A1

    公开(公告)日：2006-05-25

    申请号：US10525906

    申请日：2003-08-27

    申请人： Anders Hallberg ,  Malin Graffner-Nordberg ,  Arne Boman ,  Elisabeth Seifert

    发明人： Anders Hallberg ,  Malin Graffner-Nordberg ,  Arne Boman ,  Elisabeth Seifert

    IPC分类号： A61K31/517 ,  C07D239/95

    CPC分类号： C07D239/95

    摘要： The invention provides novel compounds or the formula II: wherein R1, R2, R3 and R4 are independently hydrogen of a group that liberates the free amine in vivo, for example —CO-alkyl, preferably —CO—C1-C3 alkyl or pivalate; or —COhaloalkyl, preferably —CO—C1-C3 haloalkyl, most preferably —CO—C1-C3 chloroalkyl; wherein W is: and @ denotes the points of attachment and wherein the ester can be located in either direction; wherein n and m are independently 0-5; wherein one but not both or X and Y can be nitrogen, or X is C-A and/or Y is C—B; wherein A and B are independently selected from hydrogen, alkyl optionally substituted with a halogen, an electron donor group such as amino, alkylamino, dialkylamino or hydroxy, or an electron acceptor group such as nitro, cyano. trihaloalkyl or amido, alkoxy or halogen; and pharmacologically acceptable salts thereof. Provided that when R1 to R4 are hydrogen, both X and Y are C—H, n is 1 and —(CH2)n— is attached to the bridging oxygen of the ester group W, then m cannot be 0 or 1.

    摘要翻译： 本发明提供了新的化合物或式II：其中R 1，R 2，R 3和R 4， 独立地是在体内释放游离胺的基团的氢，例如-CO-烷基，优选-CO-C 1 -C 3烷基或特戊酸酯; 或-CO卤代烷基，优选-CO-C 1 -C 3卤代烷基，最优选-CO-C 1 -C 3 - / SUB-氯烷基; 其中W是：和@表示连接点，并且其中酯可以位于任一方向上; 其中n和m独立地为0-5; 其中一个但不是两个或X和Y可以是氮，或X是C-A和/或Y是C-B; 其中A和B独立地选自氢，任选被卤素取代的烷基，电子给体基团如氨基，烷基氨基，二烷基氨基或羟基，或电子受体基团如硝基，氰基。 三卤代烷基或酰氨基，烷氧基或卤素; 及其药理学上可接受的盐。 假设当R 1至R 4为氢时，X和Y都是CH，n是1和 - （CH 2 CH 2） n 连接到酯基W的桥连氧上，则m不能为0或1。