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| Number | Title | Issue Date |
| 8063234 | Substituted 7-sulfanylmethyl-, 7-sulfinylmethyl- and 7-sulfonylmethylindoles and the use thereof The present application relates to novel 7-sulfanylmethyl-, 7-sulfinylmethyl- and 7-sulfonylmethylindole derivatives, processes for the preparation thereof, the use thereof alone or in combinations for the treatment and/or prevention of diseases, and the use thereof... | 11/22/2011 |
| 7968732 | Process for the preparation of 5-benzyloxy-2-(4-benzyloxyphenyl)-3-methyl-1H-indole The present invention is related to a process for the preparation of 5-benzyloxy-2-(4-benzyloxyphenyl)-3-methyl-1H-Indole (formula-1, a useful intermediate for the synthesis of bazedoxifene) using 4-benzyloxy propiophenone and 4-benzyloxy phenyl hydrazine hydrochlor... | 06/28/2011 |
| 7582773 | Substituted phenyl indoles The present invention relates generally to substituted phenyl indoles and methods of using them, for example as PAI-1 inhibitors. ... | 09/01/2009 |
| 7407983 | Indole derivatives substituted with long-chain alcohols and medicaments containing them Provided is an indole long-chain alcohol, or a hydrate or an isomer thereof, represented by the following formula (I): wherein R1, R2, R3 and R4 each independently represent a hyd... | 08/05/2008 |
| 7405236 | Indole derivatives comprising an acetylene group This invention is directed to compounds of the formula (I): wherein one of R6, R7, R8 and R9 is and X, R1 to R12,... | 07/29/2008 |
| 7307098 | Indole derivatives and drugs containing the same An indole derivative represented by the following general formula (1): wherein at least one of R1, R2, R3, and R4 represents an alkoxy group containing 1 ... | 12/11/2007 |
| 7307099 | 4-(1-(sulfonyl)-1h-indol-2-yl)-4-(hydroxy)-cyclohexa-2,5-dienone compounds and analogs thereof as therapeutic agents This invention pertains to certain 4-(1-(sulfonyl)-1H-indol-2-yl)-4-(hydroxy)-cyclohexa-2,5-dienone compounds, and analogs thereof, including compounds of the following formula, which are, inter alia, antiproliferative agents, anticancer agents, and/or thioredoxin/t... | 12/11/2007 |
| 7288553 | Indole derivatives as selective androgen receptor modulator (SARMS) The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. ... | 10/30/2007 |
| 7176322 | Calcium receptor modulating agents The compounds of the invention are represented by the following general structure or a pharmaceutically acceptable salt thereof, and compositions containing them, wherein the variables are defined herein, and the... | 02/13/2007 |
| 7173129 | Sulfonamide-substituted chalcone derivatives and their use to treat diseases The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the ... | 02/06/2007 |
| 7138418 | Pentafluorobenzenesulfonamides and analogs The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states... | 11/21/2006 |
| 7109231 | Cyclohept[b]indole derivatives A novel class of tricyclic compounds of the following formula (I): (formula I); is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of inflammatory diseases such as septic shock | 09/19/2006 |
| 7087750 | Compounds, their use and preparation The invention provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): in which Ar, R2, R3, R4 and R5 ar... | 08/08/2006 |
| 7057052 | Heterocyclic quinones as pharmaceutical agents Pyrrolylquinones and indolylquinones useful for treating diseases such as neurodegenerative disease, viral infections and proliferative disease are described, along with methods of making such compounds and pharmaceutical formulations containing such compounds. ... | 06/06/2006 |
| 6962929 | Pentafluorobenzenesulfonamides and analogs The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states... | 11/08/2005 |
| 6924304 | Cell proliferation inhibitors Compounds having formula (I) inhibit cellular proliferation. Processes for the preparation of the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclo... | 08/02/2005 |
| 6867200 | (Hetero)aryl-bicyclic heteroaryl derivatives, their preparation and their use as protease inhibitors The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents ... | 03/15/2005 |
| 6852711 | HIV protease inhibitors The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the... | 02/08/2005 |
| 6825352 | Preparation and use of ortho-sulfonamido arylhydroxamic acids as matrix metalloproteinase inhibitors Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs. ... | 11/30/2004 |
| 6770638 | Tetrahydroindolone and purine derivatives linked to arylpiperazines Pharmaceutical composite compositions comprising tetrahydroindolones linked to arylpiperazines and derivatives thereof are disclosed. Specifically, composite compositions useful in treating anti-psychotic disorders are disclosed. The composite compositions disclosed... | 08/03/2004 |
| 6743810 | Indol-3-yl derivatives Indol-3-yl derivatives of the general formula I in which A, B, X, R1, R2, R3, R4, R5, n and m are as defined in patent claim 1, and their physiologically acce... | 06/01/2004 |
| 6727237 | Inhibitors of bacterial NAD synthetase The present invention provides methods of synthesizing and screening inhibitors of bacterial NAD synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections with inhibitors of bacterial NAD synthetase enzyme. ... | 04/27/2004 |
| 6673787 | Sulfonamide-containing indole compounds The present invention creates a novel antiangiogenic agent and provides an antitumor agent which shows high safety as compared with conventional antitumor agents, has a sure effect and is able to be administered for a long period. That is, it provides an ... | 01/06/2004 |
| 6503938 | 2-phenylindoles as antiestrogenic pharmaceutical agents 2-phenylindoles are described, as well as a process for making them, pharmaceutical preparations that contain them, methods of using them as pharmaceutical agents.... | 01/07/2003 |
| 6500853 | Inhibitors of phospholipase enzymes This invention concerns compounds and pharmaceutical compositions useful for treating or preventing inflammatory conditions in a mammal, the methods comprising administration of novel pharmaceutically useful compounds of the general formulae: ##STR1#... | 12/31/2002 |
| 6500852 | Inhibitors of bacterial NAD synthetase The present invention provides methods of synthesizing and screening inhibitors of bacterial NAD synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections with inhibitors of bacterial NAD synthetase enzyme.... | 12/31/2002 |
| 6495546 | Propanolamine derivatives Propanolamine derivatives represented by the following formula (I): ##STR1## These derivatives may be 댣 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria ac... | 12/17/2002 |
| 6482860 | Pentafluorobenzenesulfonamides and analogs The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of dis... | 11/19/2002 |
| 6469043 | Sulfonamide-containing indole compounds The present invention creates a novel antiangiogenic agent and provides an antitumor agent which shows high safety as compared with conventional antitumor agents, has a sure effect and is able to be administered for a long period. That is, it provides an ... | 10/22/2002 |
| 6448243 | 1,4-substituted cyclic amine derivatives A novel 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: ##STR1## (wherein A, B, C, D, T, Y and Z represent each methine or nitrogen; R1, R2, R3, ... | 09/10/2002 |
| 6414008 | Disubstituted bicyclic heterocycles, the preparation thereof, and their use as pharmaceutical compositions New disubstituted bicyclic heterocycles of general formula Ra --A--Het--B--Ar--E (I) Compounds of general formula I, wherein E is an Rb NH--C(.dbd.NH)-- group, have valuable pharmacological properties, particularly a thrombin-inhibiting ... | 07/02/2002 |
| 6365584 | Arylysulphonamide-substituted benzimidazoles having tryptase-inhibiting activity Arylsulphonamide-substituted benzimidazole derivatives of formula (I) ##STR1## having tryptase-inhibiting activity. Exemplary are: 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethylaminoethyl)-benzenesu lphonylamino]-benzimidazole; 1-Methyl-2-[2-(4-amidinop... | 04/02/2002 |
| 6323235 | Benzene-condensed heterocyclic derivatives and their uses Novel compounds having strong TXA2 receptor antagonist activities and PGI2 receptor agonist activities, which are effective for therapy and prevention of diseases related to TXA2, are disclosed. The compound of the present... | 11/27/2001 |
| 6277833 | Substituted triols Substituted triols are prepared by reducing appropriately substituted carboxylic esters. The substituted triols can be used as active substances in medicaments.... | 08/21/2001 |
| 6245761 | Indolyl neuropeptide Y receptor antagonists This invention provides a series of substituted indoles which are useful in treating or preventing a condition associated with an excess of neuropeptide Y. This invention also provides the novel substituted indoles as well as pharmaceutical formulations w... | 06/12/2001 |
| 6242637 | Substituted heterocylic compounds, method of preparing them and pharmaceutical compositions in which they are present The invention relates to compounds of the formula ##STR1## in which: A is a divalent radical selected from: A1) --O--CO-- A2) --CH2 --O--CO-- A3) --O--CH2 --CO-- A4) --O--CH2 --CH2 | 06/05/2001 |
| 6214790 | Neo-tryptophan The invention provides a novel amino acid, neo-tryptophan, as well as polypeptides containing this novel amino acid such as neurotensin analogs. In addition, the invention provides neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and... | 04/10/2001 |
| 6147082 | Chalcones having antiproliferative activity The invention relates to a novel class of compounds that have structures related to certain naturally occurring or synthetic chalcones. The invention also relates to pharmaceutical compositions comprising the compounds and methods for treating certain dis... | 11/14/2000 |
| 6133305 | 3-(substituted)-2-indolinones compounds and use thereof as inhibitors of protein kinase activity The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment... | 10/17/2000 |
| 6121308 | Disubstituted bicyclic heterocycles, the preparation thereof and their use as pharmaceutical compositions Novel disubstituted bicyclic heterocycles, of which the following are exemplary: (a) 1-methyl-2-[(4-amidinophenyl)-oxymethyl]-5-[N-(hydroxycarbonylmethyl)-quin oline-8-sulphonylamino]-benzimidazole, (b) 1-methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(N-(... | 09/19/2000 |
