- 2-AMINO-N-(AMINO-OXO-ARYL-LAMBDA6-SULFANYLIDENE)ACETAMIDE COMPOUNDS AND THEIR THERAPEUTIC USE
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The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 2-amino-N-(amino-oxo-aryl-λ6- sulfanylidene)acetamide compounds (referred to herein as ANASIA compounds) that, inter alia, inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase (aaRS) (e.g., bacterial leucyl-tRNA synthetase, LeuRS). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase; to treat disorders that are ameliorated by the inhibition (e.g., selective inhibition) of bacterial aminoacyl-tRNA synthetase; to treat bacterial infections; etc.
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Page/Page column 222
(2021/06/26)
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- THIOPHENE, MANUFACTURING METHOD THEREOF, AND PHARMACEUTICAL APPLICATION OF SAME
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The present invention discloses a thiophene used as a uric acid transporter (URAT1) inhibitor and applicantion of the thiophene in preparing a pharmaceutical product for treating a disease related to abnormal uric acid levels, specifically in preparing a pharmaceutical product for treating hyperuricemia and gouty arthritis. The invention specifically relates to a compound as represented by formula (I) or a pharmaceutically acceptable salt thereof.
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Paragraph 0111; 0112; 0113
(2019/04/25)
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- CYCLIC SULFAMIDE COMPOUNDS AND METHODS OF USING SAME
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The present disclosure provides, in part, cyclic sulfamide compounds, and pharmaceutical compositions thereof, useful as modulators of Hepatitis B (HBV) core protein, and methods of treating Hepatitis B (HBV) infection.
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Page/Page column 309
(2018/09/21)
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- Pyrrole inhibitors of S-nitrosoglutathione reductase as therapeutic agents
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The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
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Page/Page column 304
(2015/11/16)
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- PRODUCTION METHOD OF DITHIENOBENZODITHIOPHENE
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PROBLEM TO BE SOLVED: To provide an efficient production method of dithienobenzodithiophene and its derivatives which imparts high carrier mobility by application and enables easy and efficient film production of an organic semiconductor layer. SOLUTION: A production method of dithienobenzodithiophene is characterized by producing dithienobenzodithiophene by using 2,3-dihalothiophene whose halogen at 2-position is equal in atomic number to, or larger than, the halogen at 3-position. COPYRIGHT: (C)2016,JPOandINPIT
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Paragraph 0047
(2016/12/01)
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- 4,6-DIARYLAMINOTHIAZINES AS BACE1 INHIBITORS AND THEIR USE FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION
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Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: (I) wherein R1 and R2 are independently hydrogen, or -CH3; or R1 and R2 can join together in a ring by adding -(CH2)4-; R3 is hydrogen or C1-C3 al-kyl; Y and Z are independently a C6-C10- aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, hydroxy, amino, C1-4 alkylamino, C1-4 dialkylamino, halo C1-4 alkyl, CN, C1-C6, alkyl or cycloalkyl, C1-C6 alkoxy, -C=OC1-4 alkyl, -SO2C1-4 alkyl, and C2-C4 alkynyl; A is selected from the group of phenyl, ben-zyl, oxazolyl, thiazolyl, isoxazolyl, imidazolyl, pyrazolyl, pyridyl, pyrimidinyl, and pyrazinyl groups which can be further substituted with from 0-3 substituents selected from the group of halogen, hydroxy, amino, C1-4 alkylamino, C1-4 dialkylamino, haloC1-4 alkyl, hydroxyC1-6 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is -NHCO-, or is a single bond; and L and Z to-gether can be absent
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Page/Page column 64
(2014/07/08)
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- HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF
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Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
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Page/Page column 72
(2013/08/28)
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- HYDANTOIN DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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This invention relates to compounds of the Formula: (I); or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-α or combinations thereof.
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Page/Page column 154
(2008/06/13)
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- Acyl sulfonamide anti-proliferatives. Part 2: Activity of heterocyclic sulfonamide derivatives
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The anti-proliferative activity of acylated heterocyclic sulfonamides is described in Vascular Endothelial Growth Factor-dependent Human Umbilical Vascular Endothelial Cells (VEGF-HUVEC) and in HCT116 tumor cells in a soft agar diffusion assay.
- Mader, Mary M.,Shih, Chuan,Considine, Eileen,De Dios, Alfonso,Grossman, Cora Sue,Hipskind, Philip A.,Lin, Ho-Shen,Lobb, Karen L.,Lopez, Beatriz,Lopez, Jose E.,Cabrejas, Luisa M. Martin,Richett, Michael E.,White, Wesley T.,Cheung, Yiu-Yin,Huang, Zhongping,Reilly, John E.,Dinn, Sean R.
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p. 617 - 620
(2007/10/03)
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- Novel aminophenyl ketone derivatives
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Novel heteroaryl aminophenyl ketone derivatives which are inhibitors of MAP kinases, in particular the p38 MAP kinase, are useful as anti-inflammatory agents in the prophylaxis or treatment of inflammatory diseases or conditions.
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- Piperidine derivatives for treating psychoses
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The present invention relates to certain novel piperidine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of psychotic disorders.
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- A convenient synthesis of 3-fluorothiophene
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2-bromo-3-chlorothiophene 2 underwent nucleophilic aromatic substitution using cyanocupper to give 2-cyano-3-chlorothiophene 3 which, after fluoration with CsF, hydrolysis and decarboxylation gave 3-fluorothiophene 6 in good yield. The electropolymerisation of 6 is also described.
- El Kassmi,Fache,Lemaire
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