20 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 present invention relates to antisense oligonucleotides (ASO) for use in treating, preventing, or ameliorating the progression of conditions such as type 2 diabetes mellitus (T2DM) and insulin resistance, leptin resistance, and obesity, Rater Syndrome, and cancer. Specifically, a thiomorpholino-containing ASO targets a protein tyrosine phosphatase non-receptor type 1 (PTPN1) gene transcript and induces exon skipping (including exon 2) of the transcript during RNA processing, thereby inhibiting expression of the protein tyrosine phosphatase-1B (PTP1B) protein.

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 application belongs to the technical field of bulk drug preparation and relates to a synthesis method of Filgotinib. The synthesis method of Filgotinib takes bromobenzaldehyde (compound 1) as a starting material, and boron esterification reaction is carried out under the catalysis of palladium to obtain intermediate 3. Intermediate 3 is subjected to Suzuki coupling reaction with 2-amino-6-bromopyridine (compound 4) to obtain intermediate 5. Intermediate 5 is reacted with thiomorpholine-1,1-dioxide (compound 6) to generate intermediate 7. Intermediate 7 is condensed with cyclopropylcarbonyl chloride (compound 8) and potassium thiocyanate (compound 9) to obtain intermediate 10. Intermediate 10 is subjected to cyclization with hydroxylamine hydrochloride (compound 11) to obtain the final product Filgotinib. The synthesis method solves the problems of the prior art, such as difficulty in obtaining starting materials, harsh reaction conditions and complicated process route, and has the advantages of a short synthesis route, easy availability of materials used in the reaction and simple reaction operation.

The invention discloses a small organic molecule eutectic crystal photoresist, a preparation method thereof and application of the small organic molecule eutectic crystal photoresist in near ultraviolet photoetching. The small organic molecule eutectic crystal photoresist disclosed by the invention is obtained by co-assembling 9, 10-anthracene dicarboxylic acid and amine small molecules; the co-assembly is realized through intermolecular hydrogen bonds and electrostatic interaction combination; the amine small molecules are selected from at least one of morpholine, thiomorpholine, triethylamine, triethanolamine and methyl piperazine. The small organic molecule eutectic crystal photoresist disclosed by the invention can be used for forming a forward photoetching structure through photo-induced molecular cascade decarboxylation and oxidation reaction in an absorbable low-energy ultraviolet wavelength range. The organic micromolecule eutectic crystal photoresist has the advantages of simple preparation process, high photoetching efficiency, high controllability of a three-dimensional structure and the like, and has a wide application prospect in the field of micro-nano processing.

The present invention relates to antisense oligonucleotides (ASOs) used to treat, prevent, or mitigate the progression of conditions such as type 2 diabetes mellitus (T2DM) and insulin resistance, leptin resistance and obesity, Rett syndrome, and cancer. Specifically, thiomorpholino-containing ASOs target the protein tyrosine phosphatase non-receptor type 1 (PTPN1) gene transcript during RNA processing and induce exon skipping (including exon 2), thereby inhibiting the expression of protein tyrosine phosphatase-1B (PTP1B) protein.

To provide a synthesis method that is efficient and desirable in terms of green chemistry for producing 6-(4,4-dimethylcyclohexyl)-4-[(1,1-dioxo-1λ6-thiomorpholin-4-yl)methyl]-2-methylthieno[2,3-d]pyrimidine and a salt thereof.SOLUTION: 6-(4,4-dimethylcyclohexyl)-4-[(1,1-dioxo-1λ6-thiomorpholin-4-yl)methyl]-2-methylthieno[2,3-d]pyrimidine is safely and efficiently synthesized by a method including a step of adding 4,4-dimethylcyclohexanone to the 6-position of the compound represented by the following formula [where Hal represents a halogen].SELECTED DRAWING: None

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 present invention provides carvacrol quaternary ammonium salt derivatives, their synthesis methods, and their use as antibacterial agents, belonging to the field of pharmaceutical chemistry technology. The structure of the carvacrol quaternary ammonium salt derivatives of the present invention is shown in Formula (I), where n is the number of carbon atoms between the oxygen and nitrogen atoms, and is 3, 4, or 5; and R is selected from n-propylamine, n-butylamine, n-pentylamine, n-hexylamine, dipropylamine, dibutylamine, diisopropylamine, diisobutylamine, morpholine, or thiomorpholinyl. This series of carvacrol quaternary ammonium salt derivatives exhibits excellent antibacterial activity and can be used as a potential antibacterial agent. #imgabs0#

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.

The present invention relates to a compound of formula (I), wherein X1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two of X1X2 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); and wherein 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(0)0-C1-C2alkyl; or R3 and R4 form together a bivalent residue —R5R6— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2-0-CH2—, —CH2—NH—CH2—, or any of the structures wherein 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, —CH2-0-CH2— or -0-CH2CH2-0- 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.

The invention discloses a method for regulating and controlling the light color of an organic-inorganic hybrid crystal. Two crystals are synthesized by adopting an evaporative crystallization method, and when a (Ph3S) 2InCl5 crystal is synthesized, 1.5 mmol of Ph3SCl (triphenyl sulfonium chloride salt) and 0.5 mmol of In2O3 are added into a three-necked flask, 6 mL of HCl is added, a reaction is performed for 2 h in a heating jacket at the temperature of 120 DEG C, and a target product is obtained after the product is cooled to the room temperature. After being doped with Sb < 3 + >, the crystal emits orange red light under the irradiation of an ultraviolet lamp, the emission wavelength range is 400-800 nm, and the strongest emission wavelength is 624 nm. When the (Ph3S) (C4H10NS) 2InCl6 crystal is synthesized, 1 mL of C4H9NS (thiomorpholine) is added on the basis of the synthesis, other conditions are the same, the synthesized crystal emits bright yellow light under the irradiation of an ultraviolet lamp, the emission wavelength range is 400-800 nm, and the strongest emission wavelength is 560 nm. The light color regulation is realized by introducing a C4H10NS unit, the method is simple and convenient to operate, and a new way is provided for application of the organic-inorganic hybrid crystal in the field of luminescent materials for display, illumination and the like.

Composition and methods for treating neurodegenerative diseases, such as Amyotrophic Lateral Sclerosis (ALS), Frontotemporal Dementia (FTD), and Angelman's Syndrome (AS), the compositions specifically including antisense oligonucleotides (ASOs) containing thiomorpholino nucleotides configured to inhibit ribosomal frameshifting of paternally expressed gene 10 (PEG 10) mRNA during translation, thereby inhibiting the formation of the long form gag-pol protein.