| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 201 | Histone deacetylase inhibitors and methods of use thereof | US12911145 | 2010-10-25 | US08222451B2 | 2012-07-17 | Alan P. Kozikowski; Anatoly Dritschilo; Mira Jung; Pavel A. Petukhov; Bin Chen |
| The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention. | ||||||
| 202 | Renin inhibitors | US12665219 | 2008-06-20 | US08106221B2 | 2012-01-31 | John J. Baldwin; Salvacion Cacatian; David A. Claremon; Lawrence W. Dillard; Patrick T. Flaherty; Alexey V. Ishchenko; Lanqi Jia; Gerard McGeehan; Robert D. Simpson; Suresh B. Singh; Colin M. Tice; Zhenrong Xu; Jing Yuan; Wei Zhao; Linghang Zhuang |
| The present invention is directed to aspartic protease inhibitors. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors. | ||||||
| 203 | Cure accelerators for anaerobic curable compositions | US12116572 | 2008-05-07 | US08106141B2 | 2012-01-31 | Anthony F. Jacobine; Andrew Messana; David M. Glaser; Steven Thomas Nakos |
| Reaction products prepared from reactants including: (a) at least one compound of structural Formula (I): wherein R1 is selected from aryl and heteroaryl; X is selected from a direct bond, —O—, —S—, —NH—, alkylene, cycloalkylene, heterocyclylene, arylene, alkarylene, and heteroarylene; Y is a substituted alkylene group having at least two contiguous carbon atoms and which can be interrupted by one or more —O—, —S—, or —NH— moieties as defined herein, wherein the alkylene group of Y has substituents independently selected from —OH, —NH2, —SH, cycloalkyl, heterocyclyl, aryl, and heteroaryl, or two hydrogen atoms on the same carbon atom of Y are replaced by carbonyl, and wherein at least two substituents of Y are each independently selected from —OH, —NH2, and —SH, as defined herein; and (b) at least one isocyanate functional material. | ||||||
| 204 | HETERODIMERS OF GLUTAMIC ACID | US11936659 | 2007-11-07 | US20080193381A1 | 2008-08-14 | John W. Babich; Craig N. Zimmerman; Kevin P. Maresca |
| Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR′R′, Q is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R′ is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR′R′ or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage. | ||||||
| 205 | Process for preparing highly reactive (semi) crystalline and amorphous blocked polyisocyanates | US09899240 | 2001-07-06 | US20020028948A1 | 2002-03-07 | Andreas Wenning; Thomas Weihrauch |
| The present invention provides a solventless, continuous process, which includes: in at least one extruder, intensive compounder, intensive mixer or static mixer, mixing and heating a reaction mixture including the following (A), (B), and one or both of (C) and (D): (A) at least one aliphatic, (cyclo)aliphatic and/or cycloaliphatic C3-C50 diisocyanate compound; (B) at least one aliphatic, (cyclo)aliphatic and/or cycloaliphatic C3-C50 polyisocyanate compound containing one or more isocyanurate groups; (C) 1,2,4-triazole; (D) one or more pyrazole having the formula: 1 where R1, R2 and R3 simultaneously or independently of one another are hydrogen or alkyl, alkenyl, aralkyl, aryl or N-substituted carbamoyl groups, halogen or nullC(nullO)nullOnullR4, where Rnullis a C1-C12 alkyl group; to obtain a product mixture including at least one (semi)crystalline, blocked C3-C50 isocyanate compound and at least one amorphous, blocked C3-C50 isocyanate compound. The present invention also provides a composition prepared by the process and methods of using the composition. | ||||||
| 206 | Substituted benzyloxy-carbonylguanidines, a process for their preparation, their use as a medicament or diagnostic, and a medicament containing them | US5163 | 1998-01-09 | US6022899A | 2000-02-08 | Heinz-Werner Kleemann; Joachim Brendel; Jan-Robert Schwark; Andreas Weichert; Hans-Jochen Lang; Udo Albus; Wolfgang Scholz |
| There are described compounds of the formula I ##STR1## in which the substituents R(1) to R(7) and X have the meanings shown in the claims, and their pharmaceutically tolerable salts. These are effective inhibitors of the cellular sodium proton antiporter (Na.sup.+ /H.sup.+ exchanger). They are therefore outstandingly suitable for the treatment of all diseases which can be attributed to increased Na.sup.+ /H.sup.+ exchange. | ||||||
| 207 | New urea derivatives, their preparation and their application in therapy | US918424 | 1992-07-22 | US5288758A | 1994-02-22 | Jean-Louis Vidaluc; Dennis Bigg |
| New urea derivatives corresponding to the general formula 1 ##STR1## in which: R.sup.1 represents a C.sub.1 -C.sub.4 alkyl group;R.sup.2 represents:a C.sub.5 -C.sub.7 cycloalkyl groupa cycloalkylmethyl group in which the cycloalkyl radical contains from 5 to 7 carbon atomsa benzyl groupa benzyl group in which the aromatic ring bears a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a halogen atom or a nitro group;A represents an oxygen atom or a methylene radical;n represents 1 or 2;X represents an oxygen or sulfur atom;B represents a direct bond, a methylene radical or a carbonyl radical;as well as the therapeutically acceptable salts of these molecules.The invention also relates to the application of the compounds of general formula 1 in therapy, and to the preparation processes. | ||||||
| 208 | Acid-cleavable compounds, positive-working radiation-sensitive mixture containing these compounds, and radiation-sensitive recording material produced with this mixture | US871009 | 1992-04-20 | US5286602A | 1994-02-15 | Georg Pawlowski; Horst Roeschert; Walter Spiess; Ralph Dammel |
| Compounds having repeating units of the formula I ##STR1## in which R.sup.1 is an alkylene, cycloalkylene, alkenylene, alkynylene, or arylenebisalkyl group, in which one or more aliphatic CH.sub.2 groups may be replaced by oxygen or sulfur atoms,R.sup.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, alkoxyalkyl, aryl, aralkyl or aryloxyalkyl radical,R.sup.3 is an alkyl or aryl radical,X is --CO--, --O--CO-- or --NH--CO--, andn is an integer greater than 1, especially from 3 to 50.are cleavable by acid and, in combination with photolytic acid donors and alkali-soluble binders, are constituents of positive-working mixtures which are used especially in recording materials for UV radiation and high-energy radiation. The materials are distinguished by a high resolution in conjunction with high image contrast. | ||||||
| 209 | Cationic reaction products of basic carbamides and epithalohydrins | US327354 | 1989-03-21 | US5081294A | 1992-01-14 | Rosemarie Topfl; Jorg Binz |
| There are disclosed quaternary ammonium salts which are obtainable by reacting basic carbamides containing a quaternisable nitrogen atom with epihalohydrins.These quaternary ammonium salts are particularly suitable for enhancing the color yield and the wet fastness properties of dyeings or printings produced on cellulosic fibre materials with anionic dye, e.g. reactive or direct dyes. | ||||||
| 210 | Novel process for the synthesis of the enantiomers of bicyclo(4.2.0)oct-2-en-7-one and derivatives | US900029 | 1986-08-25 | US5049497A | 1991-09-17 | Arthur F. Kluge; Dennis J. Kertesz |
| The enantiomers of formulas ##STR1## are prepared in a sequence starting from the racemic compound of formula ##STR2## wherein X is hydro or bromo when Y is bromo, or X is chloro when Y is chloro. The key step of this process involves a microbial reduction of the compound of formula (3) to give a ketone and an alcohol of high enantiomeric purity. | ||||||
| 211 | Method of preparation of optically active alpha-amino-acids | US181673 | 1988-04-14 | US4925978A | 1990-05-15 | Sandro Di Gioacchino; Antonio Paolinelli; Luciano Re |
| A new process of synthesis of optically active .alpha.-amino acids is described through nitrosation in a non-aqueous, aprotic system, of the corresponding N-carbamyl derivatives followed by decomposition of the thus obtained N-nitroso derivatives in aqueous acidic medium. The process, which is of a general applicability, leads to a remarkable increase in the reaction yields, due to the suppression of the main side reaction leading to the corresponding .alpha.-hydroxy-acid. Some N-nitroso intermediates, which can be recovered from the process of the invention, are also described. | ||||||
| 212 | 1,3 Disubstituted-5-diazobarbituric acids | US140447 | 1987-12-28 | US4902784A | 1990-02-20 | Frederick R. Hopf; Michael J. McFarland |
| Disclosed are substituted derivatives of 5-diazobarbituric acid selected from those having the formulas: ##STR1## wherein R.sub.1 and R.sub.2 are substituents selected from the group consisting of C.sub.3 to C.sub.12 alkyl, cyclohexyl, benzyl and C.sub.2 to C.sub.6 aralkyl groups, wherein R.sub.3 and R.sub.4 are substituents selected from the group consisting of C.sub.1 to C.sub.12 alkyl, cyclohexyl, benzyl or other C.sub.2 to C.sub.6 aralkyl groups and R.sub.5 is selected from the group consisting of .alpha.,.omega.-disubstituted C.sub.2 to C.sub.12 alkyl, methylene dicyclohexyl, or C.sub.1 to C.sub.6 dialkylphenylene.These compounds provide DUV response with an absorption maximum near 260 nm. The substituents are chosen to be nonabsorbing alkyl groups that allow efficient photobleaching of the sensitizer during exposure.The sensitizers of the present invention are designed to function in the DUV region and are useful in the manufacture of semi-conductor devices. | ||||||
| 213 | Amino acid analogs | US874928 | 1986-06-16 | US4880938A | 1989-11-14 | Roger M. Freidinger |
| Analogs of glutamic acid and related amino acids and pharmaceutically-acceptable salts thereof which antagonize the function of cholecystokinins and gastrin disease states in animals and compositions for and methods of preventing or treating disorders of the gastrointestinal, central nervous and appetite regulatory systems of mammals, especially of humans. | ||||||
| 214 | Substituted ureas for ennobling cellulose fibres | US167510 | 1988-03-14 | US4854934A | 1989-08-08 | Didier Wilhelm; Antonio Gelabert; Alain Blanc |
| They have the formula: ##STR1## where either R.sub.1 and R.sub.2 are identical and represent --CH.sub.2 R where R=H or a C.sub.1 to C.sub.4 alkyl group or R.sub.1 and R.sub.2 together form the --CH.sub.2 (CR.sub.4 R.sub.4).sub.n --CH.sub.2 group where n=0 or 1, R.sub.4 =H or --CH.sub.3, R.sub.3 =H or --CH.sub.2 R.sub.5 where R.sub.5 =H or a C.sub.1 to C.sub.4 alkyl group. A and A.sub.1 are either identical and represent H or A and A.sub.1 together form an ethylene, trimethylene or --CH(OCH.sub.2 R.sub.6)--CH(OCH.sub.2 R.sub.6)-- radical where R.sub.6 =H or a C.sub.1 to C.sub.4 alkyl group or, when R.sub.3 =H, a 1,2 dihydroxy-ethylene group.They are obtained by reacting a disubstituted ethanal ##STR2## with a urea ANH--CO--NHA, followed if required by etherification with an alcohol R.sub.5 CH.sub.2 OH. | ||||||
| 215 | Process for the preparation of crystalline salts or aryloxy-propanolamines | US203390 | 1988-06-06 | US4849530A | 1989-07-18 | Gerhard Zol; Gerhard Pfarrhofer |
| The invention relates to novel crystalline salts of aryloxypropanolamines with diphenylacetic acid, a process for their preparation and the use of these salts for the preparation of chemically pure aryloxy-propanolamines or pharmaceutically acceptable salts thereof. | ||||||
| 216 | Novel crystalline salts of aryloxy-propanolamines, a process for their preparation and their use | US935917 | 1986-11-28 | US4767784A | 1988-08-30 | Gerhard Zolss; Gerhard Pfarrhofer |
| The invention relates to novel crystalline salts of aryloxypropanolamines with diphenylacetic acid, a process for their preparation and the use of these salts for the preparation of chemically pure aryloxy-propanolamines or pharmaceutically acceptable salts thereof. | ||||||
| 217 | 9-Substituted carbacyclin analogs | US360090 | 1982-03-19 | US4490555A | 1984-12-25 | John C. Sih |
| Novel compounds of the following general formula: ##STR1## | ||||||
| 218 | 9-Substituted carbacyclin analogs | US349145 | 1982-02-16 | US4487961A | 1984-12-11 | Paul A. Aristoff |
| Novel compounds of the following general formula: ##STR1## | ||||||
| 219 | Preparation of trans cyclohexane 1,4-diurea | US420187 | 1982-09-20 | US4467114A | 1984-08-21 | Hans Zengel; Manfred Bergfeld |
| A process is disclosed for selectively making trans-cyclohexane-1,4-diisocyanate, trans-cyclohexane-1,4-diamine, a trans-cyclohexane-1,4-diurethane, a trans-cyclohexane-1,4-diurea and trans-cyclohexane-1,4-disulphonyl urea by reacting ammonia with a mixture of cis and trans-cyclohexane-1,4-dicarboxylic acid, a lower alkyl ester, a glycol ester, an oligomeric ester or a polyester to make a solid trans-dicarboxylic acid diamide in a first step. The diamide is chlorinated to form cyclohexane-1,4-dicarboxylic acid-bis-N-chloramide. The latter compound is then converted into a(a) trans-cyclohexane-1,4-diamine with an alkali metal hydroxide or alkaline earth metal hydroxide; or into a(b) a trans-cyclohexane-1,4-diurethane by reaction with an alcohol or glycol in a reaction mixture containing an alkali metal hydroxide or alkaline earth metal hydroxide; or into(c) a trans-cyclohexane-1,4-diurea by reaction with a primary or secondary amine in a reaction mixture containing an alkali metal hydroxide or alkaline earth metal hydroxide; or into a(d) trans-cyclohexane-1,4-sulphonyl urea by reaction with a primary sulphonamide in a reaction mixture containing an alkali metal hydroxide and dimethyl formamide and water.The diurea prepared in (c) may be converted into trans-cyclohexane-1,4-diisocyanate with gaseous hydrogen chloride in an inert solvent. The diurethane prepared in (b) and the disulphonyl urea prepared in (d) may be thermally decomposed into trans-cyclohexane-1,4-diisocyanate. | ||||||
| 220 | Preparation of trans cyclohexane 1,4-diisocyanate | US420184 | 1982-09-20 | US4439370A | 1984-03-27 | Hans Zengel; Manfred Bergfeld |
| A process is disclosed for selectively making trans-cyclohexane-1,4-diisocyanate, trans-cyclohexane-1,4-diamine, a trans-cyclohexane-1,4-diurethane, a trans-cyclohexane-1,4-diurea and trans-cyclohexane-1,4-disulphonyl urea by reacting ammonia with a mixture of cis and trans cyclohexane-1,4-dicarboxylic acid, a lower alkyl ester, a glycol ester, an oligomeric ester or a polyester to make a solid trans-dicarboxylic acid diamide in a first step. The diamide is chlorinated to form trans-cyclohexane-1,4-dicarboxylic acid-bis-N-chloramide. The latter compound is then converted into a(a) trans-cyclohexane-1,4-diamine with an alkali metal hydroxide or alkaline earth metal hydroxide; or into a(b) a trans-cyclohexane-1,4-diurethane by reaction with an alcohol or glycol in a reaction mixture containing an alkali metal hydroxide or alkaline earth metal hydroxide; or into(c) a trans-cyclohexane-1,4-diurea by reaction with a primary or secondary amine in a reaction mixture containing an alkali metal hydroxide or alkaline earth metal hydroxide; or into a(d) trans-cyclohexane-1,4-sulphonyl urea by reaction with a primary sulphonamide in a reaction mixture containing an alkali metal hydroxide and dimethyl formamide and water.The diurea prepared in (c) may be converted into trans-cyclohexane-1,4-diisocyanate with gaseous hydrogen chloride in an inert solvent. The diurethane prepared in (b) and the disulphonyl urea prepared in (d) may be thermally decomposed into trans-cyclohexane-1,4-diisocyanate. | ||||||
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