39 results about "OREXIN A RECEPTOR" patented technology

Methods and compositions for agonizing a type-2 orexin receptor (OX2R) in a cell determined to be in need thereof, including the general method of (a) administering to a subject a cyclic guanidinyl OX2R agonist and (b) detecting a resultant enhanced wakefulness or increased resistance to diet-induced accumulation of body fat, or abbreviated recovery from general anesthesia or jet lag.

An anxiolytic drug of the invention comprises an orexin receptor antagonist, a pharmacologically acceptable salt thereof, or a solvate thereof as an active ingredient. A method for screening a compound having an anxiolytic action of the invention comprises a step of using orexin-A.

In the present invention, compound such as (1R,2S)-2-(((2,4-dimethylpyrimidin-5-yl)oxy)methyl)-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl) cyclopropanecarboxamide have been found to be potent orexin receptor antagonists, and may be useful in the treatment of sleep disorders such as insomnia, as well as for other therapeutic uses.

This invention relates to imidazopyrimidine substituted piperidine derivatives and their use as pharmaceuticals.

Methods and compositions for agonizing a type-2 orexin receptor (OX2R) in a cell determined to be in need thereof, including the general method of (a) administering to a subject a cyclic guanidinyl OX2R agonist and (b) detecting a resultant enhanced wakefulness or increased resistance to diet-induced accumulation of body fat, or abbreviated recovery from general anesthesia or jet lag.

The present invention relates quinazolinone compounds of Formula (I), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses; wherein the compounds or pharmaceutical compositions disclosed herein can be used for antagonizing the orexin receptor. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing neurological and psychiatric disorders and diseases of the central nervous system in mammals, especially in humans.

A solid dispersion comprising suvorexant or a salt thereof in amorphous form and at least one pharmaceutically acceptable matrix compound, wherein the matrix compound is (i) a polymer and wherein the solid dispersion contains the suvorexant or salt thereof in an 5 amount of at least 50 weight-% based on the combined weight of the suvorexant or salt thereof and the at least one matrix compound, or (ii) a silicon-based inorganic adsorbent.

The present invention relates to compounds of the formula (I) wherein Ar1, R1, R2, R3, R4a, R4b and (R5)n are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.

The invention relates to crystalline forms of (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2- yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone, processes for the preparation thereof, pharmaceutical compositions containing such crystalline forms, pharmaceutical compositions prepared from such crystalline forms, and their use as a medicament, especially as orexin receptor antagonists.

The invention relates to octahydropyrrolo[3,4-c]pyrrole derivatives and a use thereof. The above compounds and a medicinal composition containing the compounds are used for suppressing an orexin receptor. The invention also relates to a method for preparing the compounds and the medicinal composition, and the use of the compounds and the medicinal composition in the treatment or prevention of orexin receptor related diseases.

The invention relates to an octahydropyrrolo[3,4-c]pyrrole derivative and application thereof. The compound and a pharmaceutical composition containing the compound are used for antagonizing orexin receptors. The invention also relates to a method for preparing the compound and the pharmaceutical composition, and application of the compound and the pharmaceutical composition in treating or preventing diseases related to orexin receptors.

The invention relates to an octahydropyrrolo[3,4-c]pyrrole derivative and an application method and application thereof. The compound and a pharmaceutical composition containing the compound are usedfor antagonizing orexin receptors. The invention also relates to a method for preparing the compound and the pharmaceutical composition and their application in treatment or prevention of diseases related to the orexin receptors.

Disclosed are a preparation method of an orexin receptor antagonist compound 5-3, Crystalline forms I-IV of an orexin receptor antagonist compound 5-3 are provided. Also provided are processes of the preparing the orexin receptor antagonist compound 5-3 and its crystalline forms, as well as methods of using the crystalline forms I-IV for treating an orexin-related disease.

The invention relates to a substituted aryl heteroaryl compound and application thereof, and further relates to a pharmaceutical composition containing the substituted aryl heteroaryl compound and application thereof. The compound or the pharmaceutical composition can be used for an antagonistic orexin receptor. The invention further relates to a method for preparing the compound and the pharmaceutical composition, and application of the compound and the pharmaceutical composition to preparation of drugs for treating or preventing nervous and psychogenic disorders and diseases of central nervous systems of mammals, especially human beings.

The present invention relates to crystal forms of octahydropyrrolo[3,4-c]pyrrole derivatives. The present invention also relates to a pharmaceutical composition comprising the crystalline form, and the use of the crystalline form or the pharmaceutical composition in the manufacture of a medicament for preventing, treating or alleviating orexin receptor-related diseases.

The present disclosure relates to human monoclonal antibodies against orexin receptor type 1 (OX1R, hyprocretin 1) and uses thereof for the treatment of cancer. The antibodies are characterized by their CDRs: NYYMN, YISGSSRNIYYADFVKG, SNYDGMDV (Heavy chain) and AGTSSDVGGSNYVS, PGKAP, SSYTYYSTRV (Light Chain)) or the CDRS having at least 50% or 70% identity with the above listed sequences.

The present invention relates to octahydropyrrolo[3,4-c]pyrrole derivatives and methods and uses thereof. The compounds of the present invention and pharmaceutical compositions comprising the compounds are used to antagonize orexin receptors. The present invention also relates to methods of preparing such compounds and pharmaceutical compositions, and their use in the treatment or prevention of diseases associated with orexin receptors.

The present invention relates to octahydropyrrolo[3,4-c]pyrrole derivatives and uses thereof. The compound of the present invention and the pharmaceutical composition comprising the compound are used for antagonizing orexin receptors. The present invention also relates to methods for preparing these compounds and pharmaceutical compositions, and their use in treating or preventing diseases related to orexin receptors.

The present invention relates to the compound of formula (I), wherein Ar1, R1, R2, R3, R4a, R4b and (R5)n are as described in the description; its preparation, its pharmaceutically acceptable salt and its use as medicine Uses, pharmaceutical compositions containing one or more compounds of formula (I), and especially with respect to their use as orexin receptor antagonists.

The invention relates to a crystal form of an octahydropyrrolo[3,4-c]pyrrole derivative. The invention also relates to a pharmaceutical composition containing the crystal form, and an application of the crystal form or the pharmaceutical composition in preparation of medicines for preventing, treating or relieving diseases related to orexin receptors.

The invention relates to an ctahydropyrrole[3, 4-c]pyrrole derivative and a using method and application thereof. A compound and a drug composition containing the same are used for resisting orexin receptors. The invention further relates to methods of preparing the compound and the drug composition and application of the compound and the drug composition in treating or preventing diseases related to the orexin receptors.

The present invention relates to octahydropyrrolo[3,4-c]pyrrole derivatives and uses thereof. The compound of the present invention and the pharmaceutical composition comprising the compound are used for antagonizing orexin receptors. The present invention also relates to methods for preparing these compounds and pharmaceutical compositions, and their use in treating or preventing diseases related to orexin receptors.

Processes for preparing (((3aR,6aS)-5-(4,6-dimethylpyrimidin-2-yl)hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)(2-fluoro-6-(2H-1,2,3-triazol-2-yl)phenyl)methanoneare described, which are useful for commercial manufacturing. Said compound is an orexin receptor modulator and may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia and depression.

The invention discloses a series of piperidine derivatives as orexin receptor antagonists and their compositions, and relates to their use in the preparation and treatment of insomnia, chronic obstructive pulmonary disease, obstructive sleep apnea, drowsiness, anxiety, compulsion, panic, Drug use in nicotine dependence or disordered eating disorders.

The present invention relates to (S)-proline sulfonamide compounds of formula (I), wherein R1 and R2 are as described in the description, or pharmaceutically acceptable salts thereof, for use in the prevention or treatment of diseases or disorders related to the orexin system. The present invention also relates to the use of (S)-proline sulfonamide compounds of formula (II) as pharmaceuticals, to pharmaceutical compositions comprising compounds of formula (II), and especially their use in the prevention or treatment of diseases or disorders related to the orexin system.

The present invention relates to crystal forms of octahydropyrrolo[3,4-c]pyrrole derivatives. The present invention also relates to a pharmaceutical composition comprising the crystalline form, and the use of the crystalline form or the pharmaceutical composition in the manufacture of a medicament for preventing, treating or alleviating orexin receptor-related diseases.

The present disclosure relates to human monoclonal antibodies against orexin receptor type 1 (OX1R, hyprocretin 1) and uses thereof for the treatment of cancer. The antibodies are characterized by their CDRs: NYYMN, YISGSSRNIYYADFVKG, SNYDGMDV (Heavy chain) and AGTSSDVGGSNYVS, PGKAP, SSYTYYSTRV (Light Chain)) or the CDRS having at least 50% or 70% identity with the above listed sequences.