17 results about "Methylone" patented technology

The application discloses a benzothiophenone derivative, a preparation method and application thereof. The benzothiophenone derivative, a tautomer, an optical isomer, a hydrate, a solvate, a pharmaceutically acceptable salt or a prodrug thereof, and the chemical structure of the benzothiophenone derivative is shown as formula (I), wherein R is any one of the following groups: a substituted alkane and N-benzyl-2-chloroformamide. The benzothiophenone derivative can regulate a PPARγ target as an anti-type 2 diabetes drug, can reserve insulin sensitivity, can avoid related side effects caused by a PPARγ full agonist, and has a 'highly efficient and safe' hypoglycemic effect.

The invention relates to psychoactive medicines including methylone, 2C-B, MBDB, their respective salts, metabolites, isomers, enantiomers, solvates, isotopologues and isotopomers, polymorphs, prodrugs and analogs (2C-series and cathinones); their preparation, formulations, intermediates, routes of administration, dosing and schedule for medical uses for psychiatric and neurological conditions and disorders.

The present disclosure relates to amorphous forms of (6-(4-((4-(1H-pyrazol-4- yl)phenyl)amino)pyrimidin-2-yl)-1-methyl-1H-indol-2-yl)(3,3-difluoroazetidin-1-yl)methanone (Compound A) and processes for preparing amorphous forms of Compound A. The present disclosure also provides pharmaceutical dosage forms comprising the amorphous forms of Compound A as an active pharmaceutical ingredient and methods of preparing the pharmaceutical dosage forms.

The invention relates to psychoactive medicines including methylone, 2C-B, MBDB, their respective salts, metabolites, isomers, enantiomers, solvates, isotopologues and isotopomers, polymorphs, prodrugs and analogs (2C-series and cathinones); their preparation, formulations, intermediates, routes of administration, dosing and schedule for medical uses for psychiatric and neurological conditions and disorders.

The present disclosure relates to the technical field of pharmaceutical formulations and particularly provides, in the specification, a stable imidazo[1,2-a]pyridine derivative pharmaceutical composition, a preparation method therefor, and use thereof. The pharmaceutical composition comprises an active pharmaceutical ingredient and auxiliary materials, wherein the active pharmaceutical ingredient is (azetidin-1-yl)(8-(2,6-dimethylbenzylamino)-2,3-dimethylimidazo[1,2-a]pyridin-6-yl)methanone citrate; the auxiliary materials include one or more selected from cyclodextrin, a salt of cyclodextrin, propylene glycol, and PEG400.

The application discloses a preparation method of flumetover intermediate (E)-(5,6-dihydro-[1,4,2]-dioxazin-3-yl)-(2-hydroxyphenyl)-methanone-O-methyl oxime, which is obtained by converting the configuration of (Z)-(5,6-dihydro-[1,4,2]-dioxazin-3-yl)-(2-hydroxyphenyl)-methanone-O-methyl oxime into (E)-(5,6-dihydro-[1,4,2]-dioxazin-3-yl)-(2-hydroxyphenyl)-methanone-O-methyl oxime by using an acidic reagent in the presence of a phase transfer catalyst. The application innovatively converts the useless (Z) structure, which is usually abandoned as an impurity, into the valuable flumetover intermediate (E) structure through configuration conversion, so that the useless substance can be turned into treasure, resources can be optimized, and the problems in the synthesis of the flumetover intermediate (E) structure in the prior art can be solved.

The present invention relates to a crystalline form of an imidazo[1,2-a]pyridine compound, and more specifically to a monohydrate crystalline form, crystalline form A, and crystalline form B serving as an active pharmaceutical ingredient of azetidin-1-yl{8-[(2,6-dimethylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyridin-6-yl}methanone and as an intermediate of a final salt addition compound, and a method for preparing same. The monohydrate crystalline form, crystalline form A, and crystalline form B of the compound of chemical formula I according to the present invention have excellent stability under high-humidity or high-temperature conditions, and thus can be usefully applied to the formulation of pharmaceuticals.

The invention relates to a pharmaceutical preparation, a preparation method thereof and a tablet composition. The pharmaceutical formulation according to the present invention comprises azetidine-1-yl {8-[(2, 6-dimethylbenzyl) amino]-2, 3-dimethylimidazo [1, 2-a] pyridin-6-yl} ketone citrate as an active ingredient and microcrystalline cellulose as an excipient.

The present invention relates to a pharmaceutical formulation, a method for producing the same, and a tablet composition. The pharmaceutical formulation according to the present invention contains azetidin-1-yl{8-[(2,6-dimethylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyridin-6-yl}methanone citrate as an active ingredient and microcrystalline cellulose as an excipient.

The invention discloses an application of a trimethylbenzofuran piperidinone derivative in sensitizing STING agonist antineoplastic treatment, and the derivative is (7-((3, 4-dihydroisoquinoline-2 (1H)-yl) sulfonyl)-3, 5, 6-trimethylbenzofuran-2-yl) (piperidin-1-yl) ketone. The invention also discloses an application of the trimethylbenzofuran piperidinone derivative in sensitizing STING agonist antineoplastic treatment, and the derivative is (7-((3, 4-dihydroisoquinoline-2 (1H)-yl) sulfonyl)-3, 5, 6-trimethylbenzofuran-2-yl) (piperidin-1-yl) ketone. In the prior art, through a strategy of knocking out STIM1 through CRISPR-Cas9, although cGAMP-mediated I-type interferon secretion is improved, intracellular calcium ion concentration is remarkably reduced due to irreversibility of knockout, calcium ion balance is destroyed, and processes of subsequent antigen cross presentation and the like are not facilitated. According to the present invention, the small molecule is developed to achieve the separation of STIM1 and STING, and the intracellular calcium ion steady state is maintained while the STING endoplasmic reticulum retention is released, such that the tumor treatment effect of the STING agonist is effectively enhanced, and the clinical immune response rate is expected to be significantly improved. Specifically, the invention provides a small molecule compound (7-((3, 4-dihydroisoquinoline-2 (1H)-yl) sulfonyl)-3, 5, 6-trimethylbenzofuran-2-yl) (piperidine-1-yl) ketone, which has excellent biological activity, can promote the separation of STIM1 and STING and promote the transport of STING from endoplasmic reticulum to a Golgi apparatus, and obviously improves the level of an STING agonist secreting IFN-beta.

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.

In one aspect, the present disclosure provides a method of synthesis for methylone HCl, with 3,4-methylenedioxypropiophenone (MDP) as the starting material. In another aspect, the present disclosure provides stereoisomers of methylone. In another aspect, the present disclosure provides phenethylamines or cathinones covalently bound to a chemical moiety in a prodrug form. The presently described prodrug form allows slow / sustained / controlled delivery of the parent phenethylamines or cathinones into the blood system in a manner that would increase the duration of therapeutic efficacy.

The invention relates to an application of a (1-phenyl-1H-pyrazole-3, 4, 5-triyl) tri (phenyl ketone) derivative in preparation of a medicine for resisting bone resorption and inhibiting osteoclast differentiation, and the (1-phenyl-1H-pyrazole-3, 4, 5-triyl) tri (phenyl ketone) derivative X-1 and X-4 inhibit formation of TRAP + mononuclear osteoclast precursor cells, and the (1-phenyl-1H-pyrazole-3, 4, 5-triyl) tri (phenyl ketone) derivative X-1 and the (1-phenyl-1H-pyrazole-3, 4, 5-triyl) tri (phenyl ketone) derivative X-4 inhibit formation of TRAP + mononuclear osteoclast precursor cells. And the (1-phenyl-1H-pyrazole-3, 4, 5-triyl) tri (phenyl ketone) derivatives X-2, X-3 and X-5 selectively block the further differentiation of the TRAP + osteoclast precursor cells into the mature osteoclast. The (1-phenyl-1H-pyrazole-3, 4, 5-triyl) tri (phenyl ketone) derivative has the beneficial effects that the (1-phenyl-1H-pyrazole-3, 4, 5-triyl) tri (phenyl ketone) derivative provided by the invention can be used as a novel candidate drug molecule of an inhibitor for resisting bone resorption and osteoclast differentiation, and is used for developing a novel inhibitor for osteoclast differentiation.

The invention relates to the technical field of pharmaceutical preparations, and particularly provides a stable imidazo '1, 2-a' pyridine derivative pharmaceutical composition as well as a preparation method and application thereof.The pharmaceutical composition comprises an active pharmaceutical ingredient and auxiliary materials, the active pharmaceutical ingredient is (azetidine-1-yl) (8-(2, 6-dimethyl benzylamino)-2, 3, 4-triazole-1-yl)-2, 3, 4-triazole-1-yl)-2, 3, 4-triazole-1-yl)-2, 3, 4-triazole-1-yl)-2, 3, 4-triazole-1-yl)-2, 3, 4-triazole-1 the auxiliary material comprises citrate of 2, 3-dimethylimidazo [1, 2-a] pyridine-6-yl) ketone, and the auxiliary material comprises one or more selected from cyclodextrin, a cyclodextrin salt, propylene glycol and PEG400 (Polyethylene Glycol 400).

Applicant discloses methods and compositions for treating a patient suffering from amyotrophic lateral sclerosis (ALS) comprising administration of a heteroaryl ketone fused azadecalin compound. In embodiments, the heteroaryl ketone fused azadecalin compound is dazucorilant: (R)-(1-(4-fluorophenyl)-6-((4-(trifluoromethyl)phenyl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1-H-pyrazolo[3,4-g]isoquinolin-4a-yl)(pyridin-2-yl)methanone, having the chemical structure illustrated asSuitable doses include daily administration of 150 milligrams and 300 milligrams of dazucorilant. Suitable doses include daily administration of dazucorilant with food, or with water, or with food and water. Daily administration of dazucorilant is effective to increase dazucorilant exposure up to about 2-fold when continued for seven days or more. Administration of such a heteroaryl ketone fused azadecalin compound may comprise oral administration, enteral administration, or other administration. Pharmaceutical compositions comprising dazucorilant are useful in the treatment of patients suffering from ALS. Suitable pharmaceutical compositions comprising dazucorilant include, e.g., pharmaceutical compositions for oral administration and pharmaceutical compositions for enteral administration.

The invention relates to psychoactive medicines including methylone, 2C-B, MBDB, their respective salts, metabolites, isomers, enantiomers, solvates, isotopologues and isotopomers, polymorphs, prodrugs and analogs (2C-series and cathinones); their preparation, formulations, intermediates, routes of administration, dosing and schedule for medical uses for psychiatric and neurological conditions and disorders.