- Cycloaddition reactions of polyfluoroalkylthioncarboxylic acid derivatives with dimethyl acetylenedicarboxylate (DMAD)
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Polyfluoroalkyldithiocarboxylates react with dimethyl acetylenedicarboxylate (DMAD) to give 2-polyfluoroalkyl-1,3-dithioles and/or 2-polyfluoroalkylidene-1,3-dithioles depending on the substituent at the thiolic sulfur atom and on the length of the polyfluoroalkyl chain. Amides of polyfluoroalkylthioncarboxylic acids with DMAD give 2-methoxy-2-polyfluoroalkyl-5-methoxycarbonylmethylene- thiazolidin-4-ones.
- Rudnichenko,Timoshenko,Shermolovich
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Read Online
- Compound synthesized from new thiazole monomer including electron withdrawing group and manufacturing method thereof
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The present invention relates to a compound synthesized with a novel thiazole monomer including an electron withdrawing group and a producing method thereof. The compound by the present invention is synthesized by using a thiazole monomer of a new structu
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Paragraph 0116-0121
(2019/10/08)
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- HETEROARYL SUBSTITUTED BETA-HYDROXYETHYLAMINES FOR USE IN TREATING HYPERGLYCAEMIA
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There is herein provided a compound of formula (I) or a pharmaceutically acceptable salt thereof,wherein the ring containing Q1to Q5, and the groups R1, R2 and R3, have meanings as provided in the description.
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Page/Page column 47
(2019/04/11)
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- SUBSTITUTED OXAZOLE- AND THIAZOLE-BASED CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS II
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The invention relates to oxazole and thiazole-based carboxamide and urea derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Paragraph 21-22
(2016/06/14)
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- BENZPYRAZOL DERIVATIVES AS INHIBITORS OF PI3 KINASES
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The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
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Page/Page column 109-110
(2009/12/28)
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- 2,3-SUBSTITUTED FUSED BICYCLIC PYRIMIDIN-4(3H)-ONES WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1)
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Compounds of formula (I) which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VRl, also known as TRPVl).
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Page/Page column 19
(2008/06/13)
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- PEPTIDIC COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
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- 5-carboxanilido-2,4-bis-trifluoromethylthiazoles and their use to control rice blast
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The present invention provides 5-carboxanilido-2,4-bis-trifluoromethylthiazoles and their compositions. The compounds and compositions are effective for controlling fungal diseases on plants. They are particularly effective for controlling rice blast.
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Page column 3
(2008/06/13)
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- 5-Carboxanilido-haloalkylthiazoles as antimicrobial and marine antifouling agents
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The present invention relates to a method for inhibiting the growth of microorganisms and marine organisms at a locus. In particular, the present invention relates to the use of certain 5-carboxanilido-haloalkylthiazoles as antimicrobial and marine antifouling agents.
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- Microbicidal salts of 5-carboxanilido-haloalkylthiazoles
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Compounds of the formula:whereinA is a strong base cation;R1and R2are independently (C1-C5)alkyl or (C1-C2)haloalkyl, provided that at least one of R1and R2is (C1-C2)haloalkyl;each R is independently halo, halo(C1-C5)alkyl, halo(C1-C5)alkoxy, nitro, cyano, pentahalosulfur, halomethylthio, haloethylthio, (C1-C2)alkylsulfinyl, halo(C1-C2)alkylsulfinyl, (C1-C2)alkylsulfonyl, or halo(C1-C2)alkylsulfonyl; andn is from one to five,are useful as fungicides, microbicides, marine antifoulants, and termiticides, compositions containing those compounds, and methods for their use.
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- THIONO COMPOUNDS. 7. OXIDATION OF THIOAMIDES IN RELATION TO ADVERSE BIOLOGICAL EFFECTS
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Thioacetamide, thioacetamide S-oxide (1), and thiopivalamide S-oxide (8) were oxidized with H2O2 in H2(18)O to generate the corresponding amides with at least 50percent 18O incorporation; hydrolysis of the S-oxides to the amides or 18O exchange with the amides occurs much more slowly.When 1 and trifluorothioacetamide (6) were oxidized with three and four equivalents of H2O2, respectively, in the presence of benzylamine, N-acetylbenzylamine (5) and N-benzyltrifluoroacetamide (7) were isolated in respective yields of 17percent and 37percent.These results are interpreted as evidence for an oxidative desulfurization mechanism involving nucleophilic attack at the carbon atom of an S,S-dioxide or trioxide intermediate as the major pathway; a minor pathway may involve the intermediacy of an oxathiirane S-oxide (3) or dioxide (4) species.Understanding is added to the behavior of S-oxides in aqueous solution, as well as to thermal stability in deuterochloroform.Also reported are studies of the preparation and properties of some N,N-dialkyl derivatives of 8, of reduction of 1 with NADH or NADPH, and of generation and trapping of species related to sulfoxylate ion.
- Hillhouse, John H.,Blair, Ian A.,Field, Lamar
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p. 169 - 184
(2007/10/02)
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- Synthesis and Platelet Aggregation Inhibitory Activity of 4,5-Bis(aryl)-2-substituted-thiazoles
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In our continuing effort to discover compounds which inhibit collagen-induced platelet aggregation, we have screened compounds in a mouse pulmonary thromboembolism screen.Methyl 4,5-bis(4-methoxyphenyl)-2-thiazoleacetate (3) was very active in the above screen.However, 3 was active for less than 5 min when given orally to guinea pigs.As a result, our synthetic goal was to prepare 2-substituted thiazoles with a much longer duration of activity.This paper describes the preparation of a number 4,5-bis(aryl)-2-substituted-thiazoles and their in vitro and ex vivo activity against collagen-induced platelet aggregation.It was determined that 4,5-bis(4-methoxyphenyl)-2-(trifluoromethyl)thiazole (16) is the most promising compound.
- Rynbrandt, Ronald H.,Nishizawa, Edward E.,Balogoyen, Doris P.,Mendoza, A. Rene,Annis, Kathleen A.
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p. 1507 - 1510
(2007/10/02)
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