摘要:
Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are gem-disubstituted or spirocyclic pyridine, pyrimidine and triazine derivatives.
摘要:
Selected compounds are effective for prophylaxis and treatment of inflammation and inflammatory disorders, such as NIK-mediated disorders. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, inflammation and the like.
摘要:
The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.
摘要:
Salts and polymorphs of a compound useful in the treatment of inflammatory and metabolic conditions and diseases are provided herein. In particular, the invention provides salts and polymorphs of a compound which modulates the expression and/or function of a peroxisome proliferator-activated receptor. The salts and polymorphs are useful for the treatment or prevention of conditions and disorders associated with energy homeostasis such as type II diabetes, lipid metabolism, adipocyte differentiation and inflammation.
摘要:
Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.
摘要:
Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are gem-disubstituted or spirocyclic pyridine, pyrimidine and triazine derivatives.
摘要:
Modulators of PPARη activity are provided having formula (I): in which the symbol Ar represents an aryl group; the letter X represents a divalent linkage selected from the group consisting of =C1-C6alkylene, -(C1-C6)alkylenoxy, -O-, -C(O)-, -N(R11)-, -N(R11)C(O)-, -S(O)¿k?- and a single bond, in which R?11¿ is a member selected from the group consisting of hydrogen, alkyl, heteroalkyl, and arylalkyl and the subscript k is an integer of from 0 to 2. The letter Y, in formula (I) represents a divalent linkage selected from the group consisting of alkylene, -O-, -C(O)-, -N(R12)-S(O)¿m?-, -N(R?13¿)-S(O)¿m-N(R?13)-, -N(R12)C(O)-, -S(O)¿n?-, a single bond, and combinations thereof in which R?12 and R13¿ are members independently selected from the group consisting of hydrogen, alkyl, heteroalkyl and arylalkyl; and the subscripts m and n independently integers of from 0 to 2. The symbol R1 represents a member selected from the group consisting of hydrogen, alkyl, heteroalkyl, aryl, arylalkyl, -CO¿2R?14, -CO(R)14, -C(O)NR15R16, -S(O)¿p-R?14, -S(O)¿q?-NR?15R16¿, -O-C(O)-OR17, -O-C(O)-R17, -O-C(O)-NR?15R16, -N(R14¿)-C(O)-NR?15R16, -N(R14¿)-C(O)-R17 and -N(R14)-C(O)-OR17, in which R14 is a member selected from the group consisting of hydrogen, alkyl, heteroalkyl, aryl and arylalkyl, and R?15 and R16¿ are members independently selected from the group consisting of hydrogen, alkyl, heteroalkyl, aryl and arylalkyl, or taken together with the nitrogen to which each is attached from a 5-, 6- or 7-membered ring. The symbol R17 represents a member selected from the group consisting of alkyl, heteroalkyl, aryl and arylalkyl. Additionally, for the R1 groups described above, the subscript p is an integer of from 0 to 3, and the subscript q is an integer of from 1 to 2. The symbol R2 represents a member selected from the group consisting of alkyl, heteroalkyl, aryl and arylalkyl. In another aspect, the present invention provides compounds of formula (I), as well as pharmaceutical compositions containing the compounds described above for the treatment of conditions such as type II diabetes and obesity.
摘要:
Salts and polymorphs of a compound useful in the treatment of inflammatory and metabolic conditions and diseases are provided herein. In particular, the invention provides salts and polymorphs of a compound which modulates the expression and/or function of a peroxisome proliferator-activated receptor. The salts and polymorphs are useful for the treatment or prevention of conditions and disorders associated with energy homeostasis such as type II diabetes, lipid metabolism, adipocyte differentiation and inflammation.