C07C233/10

γ-aminobutyric acid (GABA) analogues for the treatment of pain and other disorders
09663479 · 2017-05-30 · ·

A compound of Formula (1) wherein R.sub.1 represents hydrogen, halo, a C1-C4 alkyl group, a C1-C4 alkylhalide group, a C1-C4 alkoxy-C2-C4 alkyl group, a C2-C4 alkenyl group, a C2-C4 alkynyl group or a C3-C7 cyclo alkyl group; R.sub.2 represents Formula (1) or Formula (1) a tautomer thereof; and R.sub.3 represents hydrogen, a C1-C4 alkyl group, a C1-C4 alkoxy-C2-C4 alkyl group or a C7 cyclo alkyl group; or a pharmaceutically acceptable salt or solvate thereof. Processes to prepare said compounds and novel intermediates are also claimed. Such compound finds utility in treating neuropathic pain and disorders of the central nervous system. ##STR00001##

γ-aminobutyric acid (GABA) analogues for the treatment of pain and other disorders
09663479 · 2017-05-30 · ·

A compound of Formula (1) wherein R.sub.1 represents hydrogen, halo, a C1-C4 alkyl group, a C1-C4 alkylhalide group, a C1-C4 alkoxy-C2-C4 alkyl group, a C2-C4 alkenyl group, a C2-C4 alkynyl group or a C3-C7 cyclo alkyl group; R.sub.2 represents Formula (1) or Formula (1) a tautomer thereof; and R.sub.3 represents hydrogen, a C1-C4 alkyl group, a C1-C4 alkoxy-C2-C4 alkyl group or a C7 cyclo alkyl group; or a pharmaceutically acceptable salt or solvate thereof. Processes to prepare said compounds and novel intermediates are also claimed. Such compound finds utility in treating neuropathic pain and disorders of the central nervous system. ##STR00001##

IMMUNOREGULATORY AGENTS

Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.

Immunoregulatory agents

Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.

NOVEL GAMMA-AMINOBUTYRIC ACID (GABA) ANALOGUES FOR THE TREATMENT OF PAIN AND OTHER DISORDERS
20170071909 · 2017-03-16 · ·

A compound of Formula 1

##STR00001## wherein R.sub.1 represents hydrogen, halo, a C1-C4 alkyl group, a C1-C4 alkylhalide group, a C1-C4 alkoxy-C2-C4 alkyl group, a C2-C4 alkenyl group, a C2-C4 alkynyl group or a C3-C7 cycloalkyl group; R.sub.2 represents

##STR00002##

or a tautomer thereof; and R.sub.3 represents hydrogen, a C1-C4 alkyl group, a C1-C4 alkoxy-C2-C4 alkyl group or a C3-C7 cycloalkyl group; or a pharmaceutically acceptable salt or solvate thereof.

Processes to prepare said compounds and novel intermediates are also claimed. Such compound finds utility in treating neuropathic pain and disorders of the central nervous system.

Opsin-Binding Ligands, Compositions and Methods of Use

Compounds and compositions of said compounds along with methods of use of compounds are disclosed for treating ophthalmic conditions related to mislocalization of opsin proteins, the misfolding of mutant opsin proteins and the production of toxic visual cycle products that accumulate in the eye. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described.

Opsin-Binding Ligands, Compositions and Methods of Use

Compounds and compositions of said compounds along with methods of use of compounds are disclosed for treating ophthalmic conditions related to mislocalization of opsin proteins, the misfolding of mutant opsin proteins and the production of toxic visual cycle products that accumulate in the eye. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described.

Opsin-binding ligands, compositions and methods of use

Compounds and compositions of said compounds along with methods of use of compounds are disclosed for treating ophthalmic conditions related to mislocalization of opsin proteins, the misfolding of mutant opsin proteins and the production of toxic visual cycle products that accumulate in the eye. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described.

Method for preparing primary amide compounds from secondary or tertiary amides

The present invention relates to a method for preparing primary amides from tertiary or secondary amides substituted with various alkyl groups through a transamidation reaction without a metal catalyst in room-temperature conditions by adding ammonium carbonate ((NH.sub.4).sub.2CO.sub.3), wherein the method is eco-friendly since various secondary and tertiary amides that are not toxic or corrosive are used as starting materials and ammonium carbonate ((NH.sub.4).sub.2CO.sub.3) that is neither a strong acid nor a strong base is used, and the method is economical since various primary amides can be synthesized with an excellent yield at room temperature without a metal catalyst.

Method for preparing primary amide compounds from secondary or tertiary amides

The present invention relates to a method for preparing primary amides from tertiary or secondary amides substituted with various alkyl groups through a transamidation reaction without a metal catalyst in room-temperature conditions by adding ammonium carbonate ((NH.sub.4).sub.2CO.sub.3), wherein the method is eco-friendly since various secondary and tertiary amides that are not toxic or corrosive are used as starting materials and ammonium carbonate ((NH.sub.4).sub.2CO.sub.3) that is neither a strong acid nor a strong base is used, and the method is economical since various primary amides can be synthesized with an excellent yield at room temperature without a metal catalyst.