首页> 外国专利> GCs stimulators or GCs activators alone and in combination with PDE5 inhibitors for the treatment of cystic fibrosis

GCs stimulators or GCs activators alone and in combination with PDE5 inhibitors for the treatment of cystic fibrosis

机译:单独使用GC刺激物或GCs激活剂,并与PDE5抑制剂联合使用可治疗囊性纤维化

摘要

Use of a stimulator or activator of the GCs selected from the group comprising 2- [1- (2-fluorobenzyl) -1 Hpirazolo [3,4-b] pyridin-3-yl] -5- (4-morpholinyl) -4, 6-pyrimidinediamine (1), 2- [1- (2-fluorobenzyl) -1H-pyrazolo [3,4-b] pyridin-3-yl] -5- (4-pyridinyl) -4-pyrimidinamine (2), methyl-4,6-diamino-2- [1- (2-fluorobenzyl) -1 H -pyrazolo [3,4-b] pyridin-3-yl] -5-pyrimidinyl (methyl) carbamate (3), methyl-4 , 6-diamino-2- [1- (2-fluorobenzyl) -1 H -pyrazolo [3,4-b] pyridin-3-yl] -5-pyrimidinylcarbamate (4), 3- (4-amino-5-cyclopropylpyrimidin -2-yl) -1- (2-fluorbenzyl) 1H-pyrazolo [3,4-b] pyridine (4a), sodium salt of 5-chloro-2- (5-chlorothiophene-2-sulfonylamino-N- ( 4- (morpholine-4-sulfonyl) -phenyl) -benzamide (6), 2- (4-chlorophenylsulfonylamino) - 4,5-dimethoxy-N- (4- (thiomorpholine-4-sulfonyl) -phenyl) -benzamide ( 7) and / or 4 - ({(4-carboxybutyl) [2- (2- {[4- (2-phenylethyl) benzyl] oxy} phenyl) ethyl] amino} methyl) benzoic acid (5), 1- acid {6- [5-Chloro-2 - ({4-trans-4-} trifluoromethyl) cyclohexyl] benzyl} oxy) phenyl] pyridin-2-yl} -5- (trifluoromethyl) -1H-pyrazo l-4-carboxylic (8), 1- [6- (2- (2-methyl- 4- (4-trifluoromethoxyphenyl) benzyloxy) -phenyl) pyridin-2-yl] -5-trifluoromethyl-pyrazol-4- carboxylic (9), 1 [6- (3,4-dichlorophenyl) -2-pyridinyl-5- (trifluoromethyl) -1H-pyrazol-4-carboxylic acid (10), 1 - ({2- [3-chloro] -5- (trifluoromethyl) phenyl] -5-methyl-1,3-thiazol-4- yl} methyl) -1 H -pyrazol-4-carboxylic acid (11), 4 - ({2- [3- (trifluoromethyl) acid phenyl] -1,3-thiazol-4-yl} methyl) benzoic (12), 1 - ({2- [2-fluoro-3- (trifluoromethyl) phenyl] -5-methyl-1,3-thiazole- 4-yl} methyl) -1 H -pyrazol-4-carboxylic (13) for the manufacture of a medicament for the treatment of cystic fibrosis (CF).
机译:选自2- [1-(2-氟苄基)-1吡唑并[3,4-b]吡啶-3-基] -5-(4-吗啉基)-4的GC的刺激剂或活化剂的使用,6-嘧啶二胺(1),2- [1-(2-氟苄基)-1H-吡唑并[3,4-b]吡啶-3-基] -5-(4-吡啶基)-4-嘧啶胺(2) ,甲基-4,6-二氨基-2- [1-(2-氟苄基)-1 H-吡唑并[3,4-b]吡啶-3-基] -5-嘧啶基(甲基)氨基甲酸酯(3),甲基-4,6-二氨基-2- [1-(2-氟苄基)-1 H-吡唑并[3,4-b]吡啶-3-基] -5-嘧啶基氨基甲酸酯(4),3-(4-氨基- 5-环丙基嘧啶-2-基)-1-(2-氟苄基)1H-吡唑并[3,4-b]吡啶(4a),5-氯-2-(5-氯噻吩-2-磺酰基氨基-N)的钠盐-(4-(吗啉-4-磺酰基)-苯基)-苯甲酰胺(6),2-(4-氯苯基磺酰基氨基)-4,5-二甲氧基-N-(4-(硫代吗啉-4-磺酰基)-苯基)-苯甲酰胺(7)和/或4-({(4-羧基丁基)[2-(2- {[4-(2-(2-苯基乙基)苄基]氧基}苯基)乙基]氨基}甲基)苯甲酸(5),1 -酸{6- [5-Chloro-2-({4-trans- 4-}三氟甲基)环己基]苄基}氧基)苯基]吡啶-2-基} -5-(三氟甲基)-1H-吡唑1-4羧酸(8),1- [6-(2-(2-甲基-4-(4-三氟甲氧基苯基)苄氧基)-苯基)吡啶-2-基] -5-三氟甲基-吡唑-4-羧酸(9),1 [6-(3,4-二氯苯基)-2-吡啶基-5 -(三氟甲基)-1H-吡唑-4-羧酸(10),1-({2- [3-氯] -5-(三氟甲基)苯基] -5-甲基-1,3-噻唑-4-基}甲基)-1 H-吡唑-4-羧酸(11),4-({2- [3-(三氟甲基)酸苯基] -1,3-噻唑-4-基}甲基)苯甲酸(12), 1-({2- [2-氟-2-(三氟甲基)苯基] -5-甲基-1,3-噻唑-4-基}甲基)-1 H-吡唑-4-羧酸(13)用于制造用于治疗囊性纤维化(CF)的药物。

著录项

  • 公开/公告号ES2548394T3

    专利类型

  • 公开/公告日2015-10-16

    原文格式PDF

  • 申请/专利权人 ADVERIO PHARMA GMBH;

    申请/专利号ES20110701683T

  • 申请日2011-02-03

  • 分类号A61K31/18;A61K31/194;A61K31/427;A61K31/4418;A61K31/498;A61K31/4985;A61K31/506;A61K31/519;A61K31/53;A61K45/06;A61P11;

  • 国家 ES

  • 入库时间 2022-08-21 15:11:52

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