- PRODUCTION METHOD OF HETEROCYCLIC MERCAPTO COMPOUND
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A method of the invention industrially produces heterocyclic mercapto compounds useful as raw materials or intermediates in the synthesis of medicaments or pesticides, or as permanent wave agent, with a high yield and high productivity using easily available starting materials. A heterocyclic mercapto compound represented by Formula (1) (wherein X represents any structure of -O-, -S-, -NH-, and -NR1-; R1 represents any of an alkyl group, alkoxy group and alkoxyalkyl group each having 1 to 6 carbon atoms; Y represents an oxygen atom, a sulfur atom or -NR2-; R2represents a hydrogen atom or alkyl group having 1 to 6 carbon atoms; and Z1 represents a divalent organic residue having at least one mercapto group) is produced by reacting a metal sulfide or a metal hydrosulfide with a compound represented by Formula (2) (wherein X and Y are as defined in Formula (1); and Z2 represents a divalent organic residue having at least one halogen group) in the presence of a solvent at a pH of 7.0 to 11.0.
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Page/Page column 49-50
(2008/06/13)
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- HAIR PROCESSING AGENT AND METHOD FOR PERMANENT WAVING HAIR
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Provided are hair processing agents capable of permanent waving hair even at a neutral to weakly acidic pH range that causes less irritation to the skin, and hair processing agents in which an unpleasant odor is masked. Hair processing agents contain at least one compound represented by the formula (2). Hair processing agents contain a compound of the formula (2) and at least one compound (ii) selected from thioglycolic acid, thiolactic acid, cysteine, acetylcysteine, cysteamine, acylcysteamine, salts thereof and ester derivatives thereof. Hair processing agents contain a compound of the formula (2), a surfactant and water, and are emulsified. Hair processing agents contain a compound of the formula (2) and a specific perfume. wherein X is a structure selected from -O-, -S-, -NH- and -NR1-; R1 is an alkyl group of 1 to 6 carbon atoms; Y is an oxygen atom or a sulfur atom; in the formula (1), Z is a divalent organic residue having at least one mercapto group; in the formula (2), R is a divalent organic residue optionally having a mercapto group; and R2 is a hydrogen atom or an alkyl group of 1 to 6 carbon atoms.
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Page/Page column 118
(2008/06/13)
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- THIAZOL-COMPOUNDS AS 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS
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The present invention relates to compounds with the formula (I), wherein R1, R2, R3, X, and Y are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.
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Page/Page column 128-129
(2008/06/13)
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- Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
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Peptido and peptidomimetic compounds of the formula: wherein the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compos
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- Chemoenzymatic enantioselective synthesis of 3-hydroxy-2-pyrrolidinones and 3-hydroxy-2-piperidinones
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The enantioselective synthesis of 3-hydroxypyrrolidin-2-ones and 3-hydroxy piperidin-2-ones has been carried out in high enantiomeric excess employing immobilized lipase from Pseudomonas cepacia.
- Kamal, Ahmed,Ramana, K. Venkata,Ramana, A. Venkata,Babu, A. Hari
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p. 2587 - 2594
(2007/10/03)
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- Structure-based design of a parallel synthetic array directed toward the discovery of irreversible inhibitors of human rhinovirus 3C protease
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Utilizing the tools of parallel synthesis and structure-based design, a new class of Michael acceptor-containing, irreversible inhibitors of human rhinovirus 3C protease (HRV 3CP) was discovered. These inhibitors are shown to inhibit HRV-14 3CP with rates
- Johnson, Theodore O.,Hua, Ye,Luu, Hiep T.,Brown, Edward L.,Chan, Fora,Chu, Shao Song,Dragovich, Peter S.,Eastman, Brian W.,Ferre, Rose Ann,Fuhrman, Shella A.,Hendrickson, Thomas F.,Maldonado, Fausto C.,Matthews, David A.,Meador III, James W.,Patick, Amy K.,Reich, Siegfried H.,Skalitzky, Donald J.,Worland, Stephen T.,Yang, Michelle,Zalman, Leora S.
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p. 2016 - 2023
(2007/10/03)
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- Process for preparing pyrrolidinones
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A process for the preparation of a compound of general formula II: STR1 wherein R1 is hydrogen, or C1 -C10 hydrocarbyl or heterocyclyl having 3 to 8 ring atoms, either of which may optionally be substituted; each R2, R3, R4 and R5 is independently hydrogen or C1 -C4 alkyl; A is an optionally substituted aromatic or heteroaromatic ring system; and R21 is hydrogen, halogen, OH or OCONHR1, wherein R1 is as defined above; the process comprising cyclizing a compound of general formula III: STR2 wherein A, R2, R3, R4, R5 and R21 are as defined in general formula II and R25 is a leaving group such as a halogen atom; under basic conditions.
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- Synthesis and structure-activity relationship of (lactamylvinyl)cephalosporins exhibiting activity against staphylococci, pneumococci, and enterococci
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The synthesis and structure-activity relationships of a new class of vinylcephalosporins substituted with a lactamyl residue (1) are described. These compounds show excellent activity against enterococci and retain the broad spectrum activity of third-gen
- Heinze-Krauss, Ingrid,Angehrn, Peter,Guerry, Philippe,Hebeisen, Paul,Hubschwerlen, Christian,Kompis, Ivan,Page, Malcolm G. P.,Richter, Hans G. F.,Runtz, Valérie,Stalder, Henri,Weiss, Urs,Wei, Chung-Chen
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p. 1864 - 1871
(2007/10/03)
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- Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones
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A series of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones was synthesized and evaluated as candidate antiinflammatory/analgesic agents as well as dual inhibitors of prostaglandin and leukotriene synthesis. Some compounds that showed dual inh
- Ikuta,Shirota,Kobayashi,Yamagishi,Yamada,Yamatsu,Katayama
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p. 1995 - 1998
(2007/10/02)
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