摘要:
The invention provides compounds of the formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia, and also provided are pharmaceutical compositions containing such compounds.
摘要:
The invention provides compounds of the formula I wherein the substitutents are as described herein.Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia, and also provided are pharmaceutical compositions containing such compounds.
摘要:
Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.
摘要:
The present invention is directed to compounds having the formula (I), and/or pharmaceutically-acceptable salts thereof, useful in the treatment of androgen-receptor associated conditions, wherein Ar is aryl, substituted aryl, heteroaryl, or substituted heteroaryl; L is a linker as defined in the specification; R1 may be hydrogen, cyano, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, substituted cycloalkyl, heterocyclo, substituted heterocyclo, heteroaryl, or substituted heteroaryl, as defined in the specification; R2 is hydrogen, lower alkyl, or substituted lower alkyl; and R3, R4 and R5 are optionally non-interfering substituents as defined in the specification.
摘要翻译:本发明涉及可用于治疗雄激素受体相关病症的式(I)化合物和/或其药学上可接受的盐,其中Ar为芳基,取代的芳基,杂芳基或取代的杂芳基; L是说明书中定义的接头; R 1可以是如本说明书中定义的氢,氰基,烷基,取代的烷基,芳基,取代的芳基,环烷基,取代的环烷基,杂环,取代的杂环,杂芳基或取代的杂芳基; R2是氢,低级烷基或取代的低级烷基; 并且R 3,R 4和R 5是本说明书中定义的任选的非干扰取代基。
摘要:
Disclosed are compounds having the formula (I): including compounds of formulae (Ia) and (Ib): wherein G is an optionally substituted aryl or heterocyclo, L is an optional linker, M is a bond, O, CR7R7′ or NR10, and M′ is a bond or NR10, with the proviso that at least one of M or M′ must be a bond; E is C=Z2, CR7CR7′, SO2, P═OR2, or P═OOR2; Z1 is O, S, NH, or NR6; A1 is CR7 or N; A2 is CR7 or N; Y is J-J′-J″ where J is (CR7R7′)n and n=0−3, J′ is a bond or O, S, S═O, SO2, NH, NR6, C═O, CO═O, NR1C═O, CR7R7′, C═CR8R8′, R2P═O, OPOOR2, OPO2, OSO2, C═N, NHNH, NHNR6, NR6NH, N═N, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo or aryl or substituted aryl, and J″ is (CR7R7′)n and n=0−3; and W, Q, R2, R6, R7, R7′, R8, R8′, R9, R9′, and R10 are as defined in the specification and/or claims herein, to methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and to pharmaceutical compositions containing such compounds.
摘要:
Disclosed are pyrrolopyridazine compounds of the formula, wherein the substituents are defined herein, methods of preparing such compounds, and their use for the treatment of proliferative, inflammatory, and other disorders.
摘要:
The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.
摘要翻译:本发明涉及制备式I的5-(2-恶唑基烷硫基)-2-氮杂环烷酰氨基噻唑化合物或其药学上可接受的盐的新的,有效的方法,其中:R是烷基,芳基或杂芳基; R 1,R 2 R 3,R 4和R 5各自独立地为氢,烷基,芳基或杂芳基; R 6和R 7各自独立地为氢,烷基,芳基,杂芳基,卤素 ,羟基或烷氧基; R 8是氢,烷基,芳基,杂芳基,CONR 9 R 10,COR 11或COOR 12; R 9,R 10,R 11 且R 12各自独立地为氢,烷基或芳基; m等于0至5; 和等于0至5,这是细胞周期蛋白依赖性激酶(cdks)的新型有效抑制剂。 本发明还涉及新的关键中间体化合物,式III'的季铵盐和式IX的2-恶唑基烷基衍生物。
摘要:
This invention provides compounds of formula I having the structure wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.