Patent classifications
C07D211/44
ANTIOXIDANT INFLAMMATION MODULATORS: OLEANOLIC ACID DERIVATIVES WITH AMINO AND OTHER MODIFICATIONS AT C-17
This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula:
##STR00001##
wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
ANTIOXIDANT INFLAMMATION MODULATORS: OLEANOLIC ACID DERIVATIVES WITH AMINO AND OTHER MODIFICATIONS AT C-17
This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula:
##STR00001##
wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
STERICALLY HINDERED ALKYL AND OXYALKYL AMINE LIGHT STABILIZERS
Compounds having hindered amine and oxyalkyl amine light stabilizers can mitigate the adverse effects of actinic radiation, such as visible and ultraviolet light, on polymers and copolymers. Polymers and copolymers derived from such compounds. Articles, such as coated articles and molded articles, containing such polymers or compounds.
STERICALLY HINDERED ALKYL AND OXYALKYL AMINE LIGHT STABILIZERS
Compounds having hindered amine and oxyalkyl amine light stabilizers can mitigate the adverse effects of actinic radiation, such as visible and ultraviolet light, on polymers and copolymers. Polymers and copolymers derived from such compounds. Articles, such as coated articles and molded articles, containing such polymers or compounds.
Immunomodulator compounds
Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I): ##STR00001##
including stereoisomers and pharmaceutically acceptable salts thereof, wherein Z, L, R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Immunomodulator compounds
Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I): ##STR00001##
including stereoisomers and pharmaceutically acceptable salts thereof, wherein Z, L, R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
1,4-substituted piperidine derivatives
Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses. ##STR00001##
1,4-substituted piperidine derivatives
Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses. ##STR00001##
ARYLMETHYLENE HETEROCYCLIC COMPOUNDS AS KV1.3 POTASSIUM SHAKER CHANNEL BLOCKERS
A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.
##STR00001##
METHOD FOR PRODUCING 1-(1-TERT-BUTOXYCARBONYL-4-PIPERIDYLACETYL)-4- MESYLOXYPIPERIDINE AND 1-(1-TERT-BUTOXYCARBONYL-4-PIPERIDYLACETYL)-4-MESYLOXYPIPERIDINE
The object of the present invention is to provide 1-(1-tert-butoxycarbonyl piperidylacetyl)-4-mesyloxypiperidine having a low content of impurities
The object can be solved by a method for preparing 1-(1-benzyl piperidylacetyl)-4-hydroxypiperidine, comprising the steps of: (1) reductively reacting 1-benzyl-4-piperidylidene acetic acid ethyl ester represented by the formula [1]:
##STR00001##
to obtain 1-benzyl-4-piperidyl acetic acid ethyl ester represented by the formula [2]:
##STR00002##
(2) adding an ammonium chloride aqueous solution and an organic solvent to the liquid containing 1-benzyl-4-piperidyl acetic acid ethyl ester, mixing the whole, and separating into an organic layer and an aqueous layer, (3) collecting 1-benzyl-4-piperidyl acetic acid ethyl ester from the organic layer, and (4) reacting the obtained 1-benzyl-4-piperidyl acetic acid ethyl ester with 4-hydroxypiperidine represented by the formula [3]:
##STR00003##
in the presence of base, to obtain 1-(1-benzyl-4-piperidylacetyl)-4-hydroxypiperidine represented by the formula [4]:
##STR00004##