Patent classifications
C07D303/46
Hydroxamic acids and uses thereof
Compounds of formula I are provided: ##STR00001##
R.sub.1 is an alkoxy or O(CH.sub.2).sub.pX, p is an integer from 2 to 3 and X is OH, NH.sub.2, or CO.sub.2H, m is an integer from 0 to 5, n is an integer from 0 to 5, each R.sub.2 is independently selected from hydrogen, alkenyl, hydroxyalkyl, alkoxymethyl, heterocyclyl, hetereocyclylmethyl, amino, amido, hydroxamido, any of which may be optionally substituted with one or more of acyl, alkyl, alkoxy, hydroxyalkyl, or halogen, each R.sub.3 is independently selected from hydrogen, halogen, alkyl, alkenyl, carboxy, hydroxymethyl, amido, and at least one of R.sub.2 and R.sub.3 is not hydrogen.
Hydroxamic acids and uses thereof
Compounds of formula I are provided: ##STR00001##
R.sub.1 is an alkoxy or O(CH.sub.2).sub.pX, p is an integer from 2 to 3 and X is OH, NH.sub.2, or CO.sub.2H, m is an integer from 0 to 5, n is an integer from 0 to 5, each R.sub.2 is independently selected from hydrogen, alkenyl, hydroxyalkyl, alkoxymethyl, heterocyclyl, hetereocyclylmethyl, amino, amido, hydroxamido, any of which may be optionally substituted with one or more of acyl, alkyl, alkoxy, hydroxyalkyl, or halogen, each R.sub.3 is independently selected from hydrogen, halogen, alkyl, alkenyl, carboxy, hydroxymethyl, amido, and at least one of R.sub.2 and R.sub.3 is not hydrogen.
FUMAGILLOL DERIVATIVES AND POLYMORPHS THEREOF
The present disclosure relates to salts and polymorphs of aminoalkylfumagillol carbamates (e.g., fumagill-6-yl N-(trans-4-aminocyclohexyl)carbamate benzenesulfonic acid salt and fumagill-6-yl N-(trans-4-aminocyclohexyl)carbamate hydroxynaphthoic acid salt). The polymorphs are characterized by X-ray powder diffraction, differential scanning calorimetry, and thermogravimetric analysis, among other methods. The polymorphs and salts can be used as intermediates in the production of fumagillol derivatives (e.g., polymer-conjugated fumagillol derivatives) as well as therapeutic agents for the treatment of various diseases and conditions such as cancer.
Fumigillol compounds and methods of making and using same
The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided.
Fumigillol compounds and methods of making and using same
The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided.
Oxaspiro[2.5]Octane Derivatives and Analogs
The invention provides oxaspiro[2.5]octane derivatives and analogs, methods for preparation thereof, intermediates thereto, pharmaceutical compositions, and uses thereof in the treatment of various disorders and conditions, such as overweight and obesity.
Oxaspiro[2.5]Octane Derivatives and Analogs
The invention provides oxaspiro[2.5]octane derivatives and analogs, methods for preparation thereof, intermediates thereto, pharmaceutical compositions, and uses thereof in the treatment of various disorders and conditions, such as overweight and obesity.
HYDROXAMIC ACIDS AND USES THEREOF
Compounds of formula I are provided:
##STR00001##
R.sub.1 is an alkoxy or O(CH.sub.2).sub.pX, p is an integer from 2 to 3 and X is OH, NH.sub.2, or CO.sub.2H, m is an integer from 0 to 5, n is an integer from 0 to 5, each R.sub.2 is independently selected from hydrogen, alkenyl, hydroxyalkyl, alkoxymethyl, heterocyclyl, hetereocyclylmethyl, amino, amido, hydroxamido, any of which may be optionally substituted with one or more of acyl, alkyl, alkoxy, hydroxyalkyl, or halogen, each R.sub.3 is independently selected from hydrogen, halogen, alkyl, alkenyl, carboxy, hydroxymethyl, amido, and at least one of R.sub.2 and R.sub.3 is not hydrogen.
HYDROXAMIC ACIDS AND USES THEREOF
Compounds of formula I are provided:
##STR00001##
R.sub.1 is an alkoxy or O(CH.sub.2).sub.pX, p is an integer from 2 to 3 and X is OH, NH.sub.2, or CO.sub.2H, m is an integer from 0 to 5, n is an integer from 0 to 5, each R.sub.2 is independently selected from hydrogen, alkenyl, hydroxyalkyl, alkoxymethyl, heterocyclyl, hetereocyclylmethyl, amino, amido, hydroxamido, any of which may be optionally substituted with one or more of acyl, alkyl, alkoxy, hydroxyalkyl, or halogen, each R.sub.3 is independently selected from hydrogen, halogen, alkyl, alkenyl, carboxy, hydroxymethyl, amido, and at least one of R.sub.2 and R.sub.3 is not hydrogen.
METAP2 INHIBITORS AND USES THEREOF
Novel inhibitors of MetAp2 enzymatic activity and uses thereof are provided.