- IMIDAZOTHIADIAZOLE AND IMIDAZOPYRIDAZINE DERIVATIVES AS PROTEASE ACTIVATED RECEPTOR 4 (PAR4) INHIBITORS FOR TREATING PLATELET AGGREGATION
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The present invention provides imidazothiadiazole compounds of Formula (I); Wherein W,Y, R0, R2, R4, Ra, Rb, X1, X2, X3 and X4 are as defined herein,, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
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Paragraph 00132; 00134
(2013/11/18)
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- Synthesis and applications of tert-alkoxysiloxane linkers in solid-phase chemistry
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Straightforward syntheses of two tert-alkoxysilyl chloride functionalised resins 3 and 31 that allow facile attachment of 1°, 2°, 3° alcohols and phenols to the solid-phase have been achieved. Resin 3 displayed useful loading levels (0.7 mmol/g), and it was stable to storage in activated form. Siloxanes from reaction of 3 with alcohols and phenols were compatible with a variety of reaction conditions commonly used in solid-phase synthesis.
- Meloni, Marco M.,White, Peter D.,Armour, Duncan,Brown, Richard C.D.
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p. 299 - 311
(2007/10/03)
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- Pd-mediated C-C and C-S bond formation on solid support: A scope and limitations study
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The scope and limitations of Pd(0)-mediated coupling reactions between aromatic halides linked to a polystyrene resin and boronic acid derivatives (Suzuki coupling), aromatic and vinylic tin compounds (Stille coupling), as well as thiols are reported. For all reactions, conditions were optimized and evaluated with various reagents. In many cases, upon cleavage from the solid support, products were obtained in excellent yields. In most cases, the optimized reaction conditions are superior to those previously reported in the literature.
- Wendeborn, Sebastian,Berteina, Sabine,Brill, Wolfgang K.-D.,De Mesmaeker, Alain
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p. 671 - 675
(2007/10/03)
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- Substituted alkylamine derivatives
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The substituted alkylamine derivatives represented by formula (I) STR1 wherein R1 represents (a) substituted or unsubstituted C2-6 alkenyl group, (b) substituted or unsubstituted C3-6 cycloalkenyl group, (c) substituted or unsubstituted C2-6 alkynyl group, (d) substituted or unsubstituted aryl group, (e) substituted or unsubstituted heterocyclic group, (f) fused heterocyclic group which may be substituted, or (g) group represented by the formula Ru11 -Ar wherein R11 is a heterocyclic group and Ar is a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and which may be substituted; STR2 represents a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and may be substituted by R7, X and Y are linking groups, R2 is H or lower alkyl, R3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or lower cycloalkyl, R4 and R5 are independently hydrogen or halogen atoms, R6 represents (a) substituted or unsubstituted acyclic hydrocarbon group which may be unsaturated, (b) substituted or unsubstituted cycloalkyl group, or (c) substituted or unsubstituted phenyl group, or non-toxic salts thereof. (E)-N-(6-6-dimethyl-2-hepten-4-ynyl)-N-ethyl-3-[4-(3-thienyl)-2-thienyl-methyloxy]benzylamine hydrochloride is a representative example. The substituted alkylamine derivatives are useful as pharmaceuticals, particularly for the treatment and prevention of hypercholesterolemia, hyperlipemia and arteriosclerosis.
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- Heterocyclic substituted benzyl alcohol, insecticidal ester derivatives, and intermediates
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Disclosed and exemplified are insecticidal and acaricidal optionally substituted furylbenzyl, thienylbenzyl, pyrazinylbenzyl, or pyridinzylbenzyl esters of the pyrethroid acids, novel pyrethroid alcohols and other intermediates, and compositions, a method of use and a process for preparation of the esters.
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