C07D211/34

Aromatic compounds with GPR40 agonistic activity

Provided is a novel aromatic ring compound having a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula: ##STR00001##
wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity and a GLP-1 secretagogue action, is useful for the prophylaxis or treatment of cancer, obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and affords superior efficacy.

Aromatic compounds with GPR40 agonistic activity

Provided is a novel aromatic ring compound having a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula: ##STR00001##
wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity and a GLP-1 secretagogue action, is useful for the prophylaxis or treatment of cancer, obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and affords superior efficacy.

Lipids and Lipid Compositions for the Delivery of Active Agents

This invention provides for a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R.sup.A, R.sup.B, R.sub.2 and R.sub.4 are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

##STR00001##

AGONISTS OF ROR GAMMAt

The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

##STR00001##

AGONISTS OF ROR GAMMAt

The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

##STR00001##

HDAC inhibitors

Compounds of formula (I) inhibit HDAC activity: ##STR00001##
wherein A, B and D independently represent ═C— or ═N—; W is a divalent radical —CH═CH— or CH.sub.2CH.sub.2—; R.sub.1 is an ester group; R.sub.2 is the side chain of a natural or non-natural alpha-amino acid; z is 0 or 1; and Y, L.sup.1, and X.sup.1 are as defined in the claims.

HDAC inhibitors

Compounds of formula (I) inhibit HDAC activity: ##STR00001##
wherein A, B and D independently represent ═C— or ═N—; W is a divalent radical —CH═CH— or CH.sub.2CH.sub.2—; R.sub.1 is an ester group; R.sub.2 is the side chain of a natural or non-natural alpha-amino acid; z is 0 or 1; and Y, L.sup.1, and X.sup.1 are as defined in the claims.

INHIBITORS OF HISTONE DEACETYLASE

The present invention relates to compounds of formula (I):

##STR00001##

or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R.sup.1a, R.sup.2b, R.sup.2c, R.sup.5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.

INHIBITORS OF HISTONE DEACETYLASE

The present invention relates to compounds of formula (I):

##STR00001##

or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R.sup.1a, R.sup.2b, R.sup.2c, R.sup.5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.

A Process for Preparation of Dexmethylphenidate Hydrochloride

The present invention relates to a process for preparation of dexmethylphenidate hydrochloride from racemic methylphenidate. The process involves the treatment of racemic mixture of dl-throe-methylphenidate base in the presence of di-pivaloyl-D-tartaric acid (D-DPTA) in a solvent to isolate dipivaloyl tartrate salt of d-threo-methylphenidate. The dipivaloyl tartrate salt of d-threo-methylphenidate is treated with a base to obtain a d-threo-methylphenidate base, which is extracted using a suitable solvent. The d-threo-methylphenidate base is treated with hydrochloric acid-isopropyl alcohol solution to obtain slurry of d-threo-methylphenidate hydrochloride also known as dexmethylphenidate hydrochloride. The dexmethylphenidate hydrochloride slurry is filtered and washed with acetone. The invention also discloses a process for recovery of D-DPTA from the salt mother liquor and from the spent aqueous layer. The process is economical, environmental friendly and results in increased yield and optically pure dexmethylphenidate hydrochloride.