10 results about "Thiomorpholine" patented technology

The invention discloses a flavonol-based fluorescent probe for continuously detecting hydrogen sulfide and hypochlorous acid as well as a preparation method and application of the flavonol-based fluorescent probe. The flavonol-based fluorescent probe is 3-(2, 4-dinitrophenoxy)-7-(4-(diphenylamino) phenyl)-2-(4-(thiomorpholinophenyl) chromone, and the structural formula of the flavonol-based fluorescent probe is shown in the specification. According to the invention, 7-(4-(diphenylamino) phenyl)-3-hydroxy-2-(4-thiomorpholinophenyl) chromone is used as an initial raw material, and the 7-(4-(diphenylamino) phenyl)-3-hydroxy-2-(4-thiomorpholinophenyl) chromone and 2, 4-dinitrofluorobenzene are subjected to nucleophilic substitution reaction to obtain the compound 3-(2, 4-dinitrophenoxy)-7-(4-(diphenylamino) phenyl)-2-(4-(thiomorpholinophenyl) chromone. The compound is firstly subjected to selective thiolysis reaction under the action of hydrogen sulfide, the fluorescence color of a solution of the compound is changed from colorless to bright orange under the irradiation of ultraviolet light with the wavelength of 365 nm, then hypochlorous acid is continuously added into the solution, and the compound can be further subjected to specific oxidation reaction with the hypochlorous acid, so that the compound can be obtained. And the fluorescence color of the solution is changed from bright orange to bright cyan. Therefore, the compound can be used as a fluorescent probe for continuously detecting hydrogen sulfide and hypochlorous acid, has the advantages of low detection limit, high response speed, good light stability, wide pH application range and the like, and shows a good application prospect.

Disclosed herein are certain therapeutic substituted heterocyclic bridged ring compounds, including substituted morpholine, thiomorpholine, and piperidine compounds and their homologues, having various advantages over current compounds used in certain methods of drug-assisted therapy, such as MDMA, together with pharmaceutical compositions containing such compounds, and methods of their use to treat mental health disorders and CNS disorders.

The invention belongs to the field of pharmacology, and discloses a crystal form II of an oxazolidinone antibacterial candidate new drug OTB-658, and a preparation method, a composition and application of the crystal form II of the oxazolidinone antibacterial candidate new drug OTB-658. In particular to a crystal form II of N-(((3S, 3aS)-8-fluoro-1-oxo-7-thiomorpholinyl-3a, 4-dihydro-1H, 3H-benzo [b] oxazole [3, 4-d] [1, 4] oxazine-3-yl) methyl) acetamide, namely OTB-658, and a preparation method of the crystal form II of N-(((3S, 3aS)-8-fluoro-1-oxo-7-thiomorpholinyl-3a, 4-dihydro-1H, 3H-benzo [b] oxazole [3, 4-d] [1, 4] oxazine-3-yl) methyl) acetamide. The OTB-658 crystal form II is used as an active pharmaceutical ingredient to prepare drugs for treating and / or preventing bacteria, especially mycobacterium tuberculosis infectious diseases.

The present invention relates to a Crystalline Form A of a compound of Chemical Formula 1 having physically and chemically outstanding characteristics compared to amorphous forms and other crystalline forms of the compound of Chemical Formula 1. Crystalline Form A of the compound of Chemical Formula 1 according to the present invention, compared to amorphous forms or other crystalline forms, does not denature even at prolonged exposure to harsh conditions, has low water sorption, is advantageous for formulation as the crystalline form does not change even under pressure or when pulverized, and the crystalline form itself has excellent stability, being useful for storage for extended periods.

The present invention relates to compounds that are cyclic carbamate and urea benzo-morpholine and benzo-thiomopoline derivatives of general formula (I) that inhibit the JAK family (JAK1, JAK2, JAK3 and TYK2) of non-receptor tyrosine protein kinases, methods for preparing the compounds, pharmaceutical compositions comprising the compounds, and therapeutic use thereof. The compounds of the present invention may be useful in the treatment of diseases or conditions associated with dysregulation of JAK family non-receptor kinases, particularly in the treatment of various inflammatory diseases including asthma, COPD, and other respiratory diseases.

The application belongs to the field of pharmacy, and discloses a crystal form I of an oxazolidinone antibacterial candidate new drug OTB-658, a preparation method of the crystal form I, and a composition and application of the crystal form I. Specifically, the application relates to a crystal form I of N-(((3S,3aS)-8-fluoro-1-oxo-7-thiomorpholinyl-3a,4-dihydro-1H,3H-benzo[b]oxazol[3,4-d][1,4]oxazin-3-yl)methyl)acetamide, i.e. OTB-658, and a preparation method of the crystal form I. The crystal form I of OTB-658 is used as a pharmaceutical active ingredient to prepare a drug for treating and / or preventing a bacterial, in particular Mycobacterium tuberculosis, infectious disease.

The invention belongs to the field of pharmacology, and discloses a crystal form III of an oxazolidinone antibacterial candidate new drug OTB-658, a preparation method of the crystal form III, a composition of the crystal form III and application of the crystal form III. Specifically, the invention relates to a crystal form III of N-(((3S, 3aS)-8-fluoro-1-oxo-7-thiomorpholinyl-3a, 4-dihydro-1H, 3H-benzo [b] oxazole [3, 4-d] [1, 4] oxazine-3-yl) methyl) acetamide, namely OTB-658, and a preparation method thereof. The OTB-658 crystal form III is used as an active pharmaceutical ingredient to prepare drugs for treating and / or preventing bacteria, especially mycobacterium tuberculosis infectious diseases.

The present invention relates to a new process for the preparation of N-((5-(5-(difluoromethyl)-1, 3, 4-oxadiazol-2-yl) pyridin-2-yl) methyl)-N-phenylthiomorpholine-4-carboxamide 1, 1-dioxide, and a new synthetic route of the main intermediates used in the process, as well as a new crystalline form of the compound and a process thereof.

The present invention relates to a compound of formula (I),whereinX1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two of X1, X2 and X3 are N;Y is N or CH;W is H or F; with the proviso that when W is F, then X1, X2 and X3 are N;R1 and R2 are independently of each other(i) a morpholinyl of formula (II)wherein the arrow denotes the bond in formula (I); andwherein R3 and R4 are independently of each other H, C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxy, C1-C2alkoxyC1-C3alkyl, CN, or C(O)O—C1-C2alkyl; or R3 and R4 form together a bivalent residue—R5R6— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2—O—CH2—, —CH2—NH—CH2—, or any of the structureswherein the arrows denote the bonds in formula (II); or(ii) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R7; wherein R7 is independently at each occurrence C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxyC1-C3alkyl, C3-C6cycloalkyl; or two R7 substituents form together a bivalent residue —R8R9— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2—O—CH2— or —O—CH2CH2—O—;with the proviso that at least one of R1 and R2 is a morpholinyl of formula II;and prodrugs, metabolites, tautomers, solvates and pharmaceutically acceptable salts thereof, for use in a method of treating a skin disorder in a subject, wherein said skin disorder is a genodermatosis, a vascular anomaly or a skin disorder selected from scleroderma, sclerodermatous chronic graft-versus-host disease, lichen sclerosus, lichen planus, lichen ruber planus and scars.

Use of antisense thiomorpholino oligonucleotides to treat, prevent, or ameliorate the progression of inflammatory skin diseases or conditions such as psoriasis. Specifically, thiomorpholino¬ containing ASOs that target pre-mRNAs associated with inflammatory skin diseases or conditions such as psoriasis.