Patent classifications
C07D209/20
Compounds
The present invention relates to compounds of formula I, or pharmaceutically acceptable salts thereof, as well as compositions comprising such compounds. These compounds and compositions have uses in the treatment of psychiatric or neurological disorders. Compounds of formula I comprise at least one deuterium atom at the α-position and consequently have improved oral bioavailability relative to α-diprotic analogues. ##STR00001##
Compounds
The present invention relates to compounds of formula I, or pharmaceutically acceptable salts thereof, as well as compositions comprising such compounds. These compounds and compositions have uses in the treatment of psychiatric or neurological disorders. Compounds of formula I comprise at least one deuterium atom at the α-position and consequently have improved oral bioavailability relative to α-diprotic analogues. ##STR00001##
NOVEL GLUTAMINE ANTAGONISTS AND USES THEREOF
Glutamine antagonists and their use for treating oncological, immunological, and neurological diseases are disclosed. Also disclosed are methods for treating an oncological, immunological, infectious or neurological disease or disorder, the method comprising administering to a subject in need of treatment thereof a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof. Also disclosed are methods of enhancing the effects of an immune checkpoint inhibitor, enabling a subject to respond to an immune checkpoint inhibitor, or enabling the toxicity or the dose or number of treatments with an immune checkpoint inhibitor to be reduced, comprising administering to a subject in need of treatment thereof a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof, and an immune checkpoint inhibitor. Also disclosed are methods for treating an oncological, immunological, infectious or neurological disease or disorder that is refractory to checkpoint inhibitor therapy, the method comprising administering to a subject in need thereof, and having the refractory disease or disorder, a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof.
NOVEL GLUTAMINE ANTAGONISTS AND USES THEREOF
Glutamine antagonists and their use for treating oncological, immunological, and neurological diseases are disclosed. Also disclosed are methods for treating an oncological, immunological, infectious or neurological disease or disorder, the method comprising administering to a subject in need of treatment thereof a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof. Also disclosed are methods of enhancing the effects of an immune checkpoint inhibitor, enabling a subject to respond to an immune checkpoint inhibitor, or enabling the toxicity or the dose or number of treatments with an immune checkpoint inhibitor to be reduced, comprising administering to a subject in need of treatment thereof a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof, and an immune checkpoint inhibitor. Also disclosed are methods for treating an oncological, immunological, infectious or neurological disease or disorder that is refractory to checkpoint inhibitor therapy, the method comprising administering to a subject in need thereof, and having the refractory disease or disorder, a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof.
C4-carbonothioate-substituted tryptamine derivatives and methods of using
Disclosed are novel C.sub.4-carbonothioate-substituted tryptamine derivative compounds and pharmaceutical and recreational drug formulations containing the same. The pharmaceutical formulations may be used to treat brain neurological disorders.
C4-carbonothioate-substituted tryptamine derivatives and methods of using
Disclosed are novel C.sub.4-carbonothioate-substituted tryptamine derivative compounds and pharmaceutical and recreational drug formulations containing the same. The pharmaceutical formulations may be used to treat brain neurological disorders.
5-METHOXYTRYPTOPHAN AND ITS DERIVATIVES AND USES THEREOF
A 5-methoxytryptophan and its derivatives are disclosed, wherein the 5-methoxytryptophan and its derivatives are represented by the following formula (I):
##STR00001##
wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and n are defined in the specification. In addition, the present invention also provides novel used of the 5-methoxytryptophan and its derivatives for treating inflammatory-related disease and cancers.
5-METHOXYTRYPTOPHAN AND ITS DERIVATIVES AND USES THEREOF
A 5-methoxytryptophan and its derivatives are disclosed, wherein the 5-methoxytryptophan and its derivatives are represented by the following formula (I):
##STR00001##
wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and n are defined in the specification. In addition, the present invention also provides novel used of the 5-methoxytryptophan and its derivatives for treating inflammatory-related disease and cancers.
NOVEL ANALOGS OF PTEROSTILBENE AMINO ACID BEARING CARBONATES FOR TREATING A NON-ALCOHOLIC FATTY LIVER DISEASE AND NONALCOHOLIC STEATOHEPATITIS
A series of novel analogs of water soluble pterostilbene amino acid bearing carbonates were synthesized, which show activities in treating a non-alcoholic fatty liver disease and a nonalcoholic steatohepatitis (NASH).
Use of ester derivative of tryptophan as deodorant and/or perfume agent
This invention relates to the use of at least one following compound having formula (I), as well as the salts thereof, the optical and geometric isomers thereof, and the solvates thereof, as deodorant agent for treating body odor, preferably underarm odor: ##STR00001##