Patent classifications
A61P25/24
OPIOID RECEPTOR AGONIST, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF
The invention belongs to the field of pharmacy, and relates to a class of opioid receptor agonists, their preparation method and the pharmaceutical use thereof, in particular to 3-(dimethylaminomethyl) cyclohex-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivative or salt thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivative or salt thereof and preparation method thereof, and relate to the use of said compounds in the treatment of opioid receptor-mediated diseases. The use of the compound or pharmaceutically acceptable salt, solvate or hydrate thereof in the preparation of a medicament for treating indications related to opioid receptors. The opioid receptor-related indications are pain, irritable bowel syndrome, pruritus, addiction and depression.
Treatment of unipolar depressive disorder
The invention relates to the treatment or control of unipolar depressive disorder by administering a compound of Formula I or a salt thereof to a subject; ##STR00001##
wherein:
E is S or Se;
R.sup.1 and R.sup.2 are optional substituents, and are at each occurrence independently selected from:
(1) a halogen, which is preferably selected from F, Cl and Br;
(2) C.sub.1-C.sub.4 alkyl, such as C.sub.1-C.sub.2 alkyl or C.sub.1 alkyl, optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br; and
(3) C.sub.1-C.sub.4 alkoxy, such as C.sub.1-C.sub.2 alkoxy or C.sub.1 alkoxy; optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br;
m is an integer in the range of from 0 to 5; and
n is an integer in the range of from 0 to 4.
Treatment of unipolar depressive disorder
The invention relates to the treatment or control of unipolar depressive disorder by administering a compound of Formula I or a salt thereof to a subject; ##STR00001##
wherein:
E is S or Se;
R.sup.1 and R.sup.2 are optional substituents, and are at each occurrence independently selected from:
(1) a halogen, which is preferably selected from F, Cl and Br;
(2) C.sub.1-C.sub.4 alkyl, such as C.sub.1-C.sub.2 alkyl or C.sub.1 alkyl, optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br; and
(3) C.sub.1-C.sub.4 alkoxy, such as C.sub.1-C.sub.2 alkoxy or C.sub.1 alkoxy; optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br;
m is an integer in the range of from 0 to 5; and
n is an integer in the range of from 0 to 4.
PYRAZINE DERIVATIVE AND APPLICATION THEREOF IN INHIBITING SHP2
The present invention relates to a pyrazine derivative, an application thereof in inhibiting SHP2, and a compound of formula (I) or pharmaceutically acceptable salts, esters, isomers, solvates, prodrugs or isotope labels thereof. The structure of the compound of formula (I) is as follows. The novel pyrazine derivative provided by the present invention has excellent inhibition of SHP2 activity and can be used to prevent and/or treat non-receptor protein tyrosine phosphatase-mediated or dependent diseases or disorders.
TETRAHYDROCANNABINOL DERIVATIVES, PREPARATION METHOD THEREOF AND USE THEREOF
Tetrahydrocannabinol derivatives and medical use thereof, in particular to the compounds represented by general formula (I), or stereoisomers, solvates, metabolites, pharmaceutically acceptable salts or cocrystals thereof, wherein the definitions of substituents in general formula (I) are the same as those in the description
##STR00001##
Organic compounds
This invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT.sub.2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D.sub.1/D.sub.2 receptor signaling systems, and/or the treatment of residual symptoms.
Organic compounds
This invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT.sub.2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D.sub.1/D.sub.2 receptor signaling systems, and/or the treatment of residual symptoms.
Compositions comprising (R)-2-amino-3-phenylpropyl carbamate and uses thereof
The present invention relates to a newly identified solvate form of (R)-2-amino-3-phenylpropyl carbamate (APC) hydrochloride, a method of preparing APC hydrochloride, and methods of using the same to treat disorders. The invention further relates to methods of producing APC hydrochloride with increased purity.
Compositions comprising (R)-2-amino-3-phenylpropyl carbamate and uses thereof
The present invention relates to a newly identified solvate form of (R)-2-amino-3-phenylpropyl carbamate (APC) hydrochloride, a method of preparing APC hydrochloride, and methods of using the same to treat disorders. The invention further relates to methods of producing APC hydrochloride with increased purity.
Psychoactive medicines and their use for treating psychiatric and neurological conditions and disorders
The invention relates to psychoactive medicines including 2C-B, methylone, MBDB, their respective metabolites, isomers, enantiomers, polymorphs, and analogues (2C-series and cathinones); their preparation, formulations, intermediates, routes of administration, dosing and schedule for medical uses for psychiatric and neurological conditions and disorders.