摘要:
Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidino carbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.
摘要:
Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidino carbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.
摘要:
Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidinocarbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.
摘要:
Compounds of formula 1: are disclosed, wherein V is CH2; W is S(O)m; m is the integer 0, 1 or 2; U is O, C(O), CR13R14 or NR15; where R13 is H, alkyl; R14 is H, OH, OR13 or OCOR13; R15 is H, alkyl, cycloalkyl, alkenyl, C(O)R13, C(O)OR13 or alkylaminocarbonyl; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. These compounds are inhibitors of tumor necrosis factor-alpha (TNF-α) and are useful as medicaments for the treatment and prevention of disorders caused by increased TNF-α activity, in particular inflammations.
摘要翻译:公开了式1化合物,其中V是CH 2; W为S(O)m; m是整数0,1或2; U是O,C(O),CR 13 R 14或NR 15; 其中R 13为H,烷基; R14是H,OH,OR13或OCOR13; R 15是H,烷基,环烷基,烯基,C(O)R 13,C(O)OR 13或烷基氨基羰基; R1,R2,R3,R4,R5,R6,R7和R8如本文所定义。 这些化合物是肿瘤坏死因子-α(TNF-α)的抑制剂,可用作治疗和预防由增加的TNF-α活性引起的疾病,特别是炎症的药物。
摘要:
Compounds of formula 1: are disclosed, wherein V is CH2; W is S(O)m; m is the integer 0, 1 or 2; U is O, C(O), CR13R14 or NR15; where R13 is H, alkyl; R14 is H, OH, OR13 or OCOR13; R15 is H, alkyl, cycloalkyl, alkenyl, C(O)R13, C(O)OR13 or alkylaminocarbonyl; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. These compounds are inhibitors of tumor necrosis factor-alpha (TNF-α) and are useful as medicaments for the treatment and prevention of disorders caused by increased TNF-α activity, in particular inflammations.
摘要翻译:公开了式1化合物,其中V是CH 2; W为S(O)m; m是整数0,1或2; U是O,C(O),CR 13 R 14或NR 15; 其中R 13为H,烷基; R14是H,OH,OR13或OCOR13; R 15是H,烷基,环烷基,烯基,C(O)R 13,C(O)OR 13或烷基氨基羰基; R1,R2,R3,R4,R5,R6,R7和R8如本文所定义。 这些化合物是肿瘤坏死因子-α(TNF-α)的抑制剂,可用作治疗和预防由增加的TNF-α活性引起的疾病,特别是炎症的药物。
摘要:
Compounds of formula 1: are disclosed, wherein V is CH2; W is S(O)m; m is the integer 0, 1 or 2; U is O, C(O), CR13R14 or NR15; where R13 is H, alkyl; R14 is H, OH, OR13 or OCOR13; R15 is H, alkyl, cycloalkyl, alkenyl, C(O)R13, C(O)OR13 or alkylaminocarbonyl; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. These compounds are inhibitors of tumor necrosis factor-alpha (TNF-α) and are useful as medicaments for the treatment and prevention of disorders caused by increased TNF-α activity, in particular inflammations.
摘要翻译:公开了式1化合物,其中V是CH 2; W为S(O)m; m是整数0,1或2; U是O,C(O),CR 13 R 14或NR 15; 其中R 13为H,烷基; R14是H,OH,OR13或OCOR13; R 15是H,烷基,环烷基,烯基,C(O)R 13,C(O)OR 13或烷基氨基羰基; R1,R2,R3,R4,R5,R6,R7和R8如本文所定义。 这些化合物是肿瘤坏死因子-α(TNF-α)的抑制剂,可用作治疗和预防由增加的TNF-α活性引起的疾病,特别是炎症的药物。
摘要:
Compounds of formula 1: are disclosed, wherein V is CH2; W is S(O)m; m is the integer 0, 1 or 2; U is O, C(O), CR13R14 or NR15; where R13 is H, alkyl; R14 is H, OH, OR13 or OCOR13; R15 is H, alkyl, cycloalkyl, alkenyl, C(O)R13, C(O)OR13 or alkylaminocarbonyl; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. These compounds are inhibitors of tumor necrosis factor-alpha (TNF-α) and are useful as medicaments for the treatment and prevention of disorders caused by increased TNF-α activity, in particular inflammations.
摘要翻译:公开了式1化合物,其中V是CH 2; W为S(O)m; m是整数0,1或2; U是O,C(O),CR 13 R 14或NR 15; 其中R 13为H,烷基; R14是H,OH,OR13或OCOR13; R 15是H,烷基,环烷基,烯基,C(O)R 13,C(O)OR 13或烷基氨基羰基; R1,R2,R3,R4,R5,R6,R7和R8如本文所定义。 这些化合物是肿瘤坏死因子-α(TNF-α)的抑制剂,可用作治疗和预防由增加的TNF-α活性引起的疾病,特别是炎症的药物。
摘要:
Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidino carbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.
摘要:
Compounds of formula 1: are disclosed, wherein V is CH2; W is S(O)m; m is the integer 0, 1 or 2; U is O, C(O), CR13R14 or NR15; where R13 is H, alkyl; R14 is H, OH, OR13 or OCOR13; R15 is H, alkyl, cycloalkyl, alkenyl, C(O)R13, C(O)OR13 or alkylaminocarbonyl; R1, R2, R3, R4, R5, R6, R7 and R5 are as defined herein. These compounds are inhibitors of tumor necrosis factor-alpha (TNF-α) and are useful as medicaments for the treatment and prevention of disorders caused by increased TNF-α activity, in particular inflammations.
摘要翻译:公开了式1化合物,其中V是CH 2; W为S(O)m; m是整数0,1或2; U是O,C(O),CR 13 R 14或NR 15; 其中R 13为H,烷基; R14是H,OH,OR13或OCOR13; R 15是H,烷基,环烷基,烯基,C(O)R 13,C(O)OR 13或烷基氨基羰基; R1,R2,R3,R4,R5,R6,R7和R5如本文所定义。 这些化合物是肿瘤坏死因子-α(TNF-α)的抑制剂,可用作治疗和预防由增加的TNF-α活性引起的疾病,特别是炎症的药物。
摘要:
Compounds of formula 1: are disclosed, wherein V is CH2; W is S(O)m; m is the integer 0, 1 or 2; U is O, C(O), CR13R14 or NR15; where R13 is H, alkyl; R14 is H, OH, OR13 or OCOR13; R15 is H, alkyl, cycloalkyl, alkenyl, C(O)R13, C(O)OR13 or alkylaminocarbonyl; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. These compounds are inhibitors of tumor necrosis factor-alpha (TNF-α) and are useful as medicaments for the treatment and prevention of disorders caused by increased TNF-α activity, in particular inflammations.
摘要翻译:公开了式1的化合物,其中V是CH 2 2; W是S(O)m。 m是整数0,1或2; U是O,C(O),CR 13 R 14或NR 15; 其中R 13是H,烷基; R 14是H,OH,OR 13或OCOR 13; R 15是H,烷基,环烷基,烯基,C(O)R 13,C(O)OR 13或烷基氨基羰基; R 1,R 2,R 3,R 4,R 5, R 6,R 7和R 8是如本文所定义的。 这些化合物是肿瘤坏死因子-α(TNF-α)的抑制剂,可用作治疗和预防由增加的TNF-α活性引起的疾病,特别是炎症的药物。