Patent classifications
C07D231/18
Pyrazole compounds and preparation thereof
The present invention provides processes for preparation of substituted pyrazole compounds of formula II, that can be used as intermediates for preparation of substituted piperidine urea compounds useful for the treatment of dilated cardiomyopathy (DCM). R.sup.2 is independently selected from F, C1-C4 alkyl, C1-C4 haloalkyl, R.sup.3 is independently selected from H, F, C1-C4 alkyl, C1-C4 haloalkyl, R.sup.4 is C1-C4 alkyl, R.sup.6 is H or a protecting group and R.sup.7 is selected from H, CI or trialkylsilyl. ##STR00001##
ACLY INHIBITORS AND USES THEREOF
The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.
SPIROHEPTANE SALICYLAMIDES AND RELATED COMPOUNDS AS INHIBITORS OF ROCK
The present invention provides compounds of Formula (I):
##STR00001##
or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
SPIROHEPTANE SALICYLAMIDES AND RELATED COMPOUNDS AS INHIBITORS OF ROCK
The present invention provides compounds of Formula (I):
##STR00001##
or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
TETRALIN AND INDANE DERIVATIVES AND USES THEREOF
The application discloses pharmaceutical compounds of formula I useful for treating CNS diseases wherein m, s, R.sup.1 R.sup.5, R.sup.6 and R.sup.7 are as defined herein.
##STR00001##
TETRALIN AND INDANE DERIVATIVES AND USES THEREOF
The application discloses pharmaceutical compounds of formula I useful for treating CNS diseases wherein m, s, R.sup.1 R.sup.5, R.sup.6 and R.sup.7 are as defined herein.
##STR00001##
Spiroheptane salicylamides and related compounds as inhibitors of rock
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same. ##STR00001##
High-solubility thioether quinones
Substituted hydroquinones and quinones and methods of synthesizing such compounds are disclosed herein. The substituted hydroquinones have the formula: ##STR00001##
while the substituted quinones have the corresponding oxidized structure (1,4-benzoquinones). One, two, three, or all four of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 comprise a thioether moiety and a sulfonate moiety, and wherein each R.sup.1, R.sup.2, R.sup.3 and R.sup.4 that does not comprise a thioether and a sulfonate moiety sulfonate moiety is independently a hydrogen, an alkyl or an electron withdrawing group. The substituted hydroquinones and quinones are soluble in water, stable in aqueous acid solutions, and have a high reduction potential in the oxidized form. Accordingly, they can be used as redox mediators in emerging technologies, such as in mediated fuel cells or organic-mediator flow batteries.
High-solubility thioether quinones
Substituted hydroquinones and quinones and methods of synthesizing such compounds are disclosed herein. The substituted hydroquinones have the formula: ##STR00001##
while the substituted quinones have the corresponding oxidized structure (1,4-benzoquinones). One, two, three, or all four of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 comprise a thioether moiety and a sulfonate moiety, and wherein each R.sup.1, R.sup.2, R.sup.3 and R.sup.4 that does not comprise a thioether and a sulfonate moiety sulfonate moiety is independently a hydrogen, an alkyl or an electron withdrawing group. The substituted hydroquinones and quinones are soluble in water, stable in aqueous acid solutions, and have a high reduction potential in the oxidized form. Accordingly, they can be used as redox mediators in emerging technologies, such as in mediated fuel cells or organic-mediator flow batteries.
N-HYDROXYLSULFONAMIDE DERIVATIVES AS NEW PHYSIOLOGICALLY USEFUL NITROXYL DONORS
The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release HNO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.