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| Number | Title | Issue Date |
| 6180786 | Heterocycle substituted propenoic acid derivatives as NMDA antagonist The present invention is new 3-(heterocyclic)-propenoic acid derivatives and pharmaceutical compositions thereof. These new 3-(heterocyclic)-propenoic acid derivatives are useful as NMDA antagonist.... | 01/30/2001 |
| 6156901 | Spiro[cyclopent[b]indole-piperidines] Novel spiro[cyclopent[b]indole-piperidines], intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the spiro[cyclopent[b]indole-piperidines] and intermediates, or composition... | 12/05/2000 |
| 6121463 | Alkyl-4-silylheterocyclic phenols and thiophenols useful as antioxidant agents The present invention provides compounds of the formula ##STR1## wherein R is hydrogen or --C(O)--(CH2)m --Q wherein Q is hydrogen or --COOH and m is an integer 1, 2, 3 or 4; R1, R5 and R6 are indepen... | 09/19/2000 |
| 6114572 | Substituted phenols and thiophenols useful as antioxidant agents The present invention provides compounds of the formula ##STR1## wherein X is selected from the group consisting of ##STR2## Y is thio, oxy or a methylene group; Z is hydrogen or --C(O)--(CH2)m --Q wherein Q is hydrogen or ... | 09/05/2000 |
| 6075144 | 9-hydroxyamino tetrahydroacridine and related compounds There are disclosed compounds having the formula ##STR1## wherein n is 1-4; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR2 | 06/13/2000 |
| 6069232 | Polyfluoroalkyl tryptophan tripeptide thrombin inhibitors This invention relates to polyfluoroalkyl tryptophan tripeptides and to compositions containing them. The compounds are highly selective thrombin inhibitors which provide anticoagulant effects useful in the treatment of thrombin conditions and in preventi... | 05/30/2000 |
| 6063793 | Esters of (+)--(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidi nemethanol The present invention is directed to esters of (+)--(2,3-Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidine methanol, pharmaceutical formulations, methods of making and methods of using these esters. These compounds antagonize the effects of ... | 05/16/2000 |
| 6039974 | Pharmaceutical composition for combination of piperidinoalkanol-decongestant The present invention provides a pharmaceutical composition in the form of a bilayer tablet comprising, (a) a first discrete zone made with Formulation (A) which comprises, a therapeutically effective decongestant amount of a sympathomimetic drug, or a ph... | 03/21/2000 |
| 6037353 | Method of providing an antihistaminic effect in a hepatically impaired patient The present invention relates to a method of providing an antihistaminic effect in a hepatically impaired patient in need thereof comprising administering to said patient an effective antihistaminic amount of a compound of the formula ##STR1## w... | 03/14/2000 |
| 6034241 | Process for converting hydroxy heteroaromatics to arylamines A process of converting a hydroxy heteroaromatic compound to an arylamine, comprising the steps of: (1) treating a salt of a hydroxy heteroaromatic compound with an alkylating agent; and (2) treating the reaction mixture with a Smiles solvent system and raisin... | 03/07/2000 |
| 6028083 | Esters of (+)--(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl) ethyl]-4-piperidinemethanol The present invention is directed to esters of (+)--(2,3 Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol, pharmaceutical formulations, methods of making and methods of using these esters. These compounds antagonize the effects of ... | 02/22/2000 |
| 6022880 | Substituted pyridylamino indoles There are disclosed various compounds of the formula below, ##STR1## where R, R1, W, X, Y and Z are as defined in the specification; which are useful for alleviating various memory dysfunctions such as Alzheimer's disease, as modulators of... | 02/08/2000 |
| 6022877 | Use of (+)--(2,3-dimethoxyphenyl-1-[2-(4-fluorophenyl)ethyl]-4-piperidin emethanol in treating depressive disorders and bipolar disorders The present invention is directed to the use of (+)--(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidine methanol in treating Depressive Disorders and Bipolar Disorders.... | 02/08/2000 |
| 6013645 | Hypocholesterolemic, antiatherosclerotic and hypotriglyceridemic mercaptoacetylamide disulfide derivatives The present invention relates certain mercaptoacetylamide disulfide derivatives of the formula ##STR1## useful in treating patients suffering from hypertriglyceridemia, atherosclerosis and hypercholestrolemia.... | 01/11/2000 |
| 6008196 | Perfluoroalkyl ketone inhibitors of elastase and processes for making the same This invention relates to compounds which are inhibitors of elastase, particularly human neutrophil elastase, and to novel processes for making the same. As inhibitors of human neutrophil elastase, the compounds are useful in the treatment of a patient af... | 12/28/1999 |
| 6008348 | Antipsychotic agents, compositions and method of use This invention relates to compounds of the formula wherein X, Y, Z, m, n and p are as defined within, pharmaceutical compositions containing these compounds and to their use as antipsychotic agents, particularly in the treatment of schizophrenia. Depot de... | 12/28/1999 |
| 6004999 | Triptolide derivatives useful in the treatment of autoimmune diseases The present invention relates to novel triptolide derivatives and a method of treating a patient suffering from an autoimmune disease comprising administering to a patient an effective amount of the novel triptolide derivatives.... | 12/21/1999 |
| 6004977 | N-(pyridinylamino) isoindolines and related compounds Novel N-(pyridinylamino)isoindolines and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the N-(pyridinylamino)isoindolines and related compounds, th... | 12/21/1999 |
| 6004959 | Alkyloxyamino substituted fluorenones and their use as protein kinase-C inhibitors The present invention describes certain alkyloxyamino-substituted fluorenones which inhibit protein kinase C, as well as pharmaceutical compositions including these compounds and methods of using these compounds to control protein kinase C activity in mam... | 12/21/1999 |
| 6004982 | 4-piperidinyl) H-2-benzopyran derivatives useful as antipsychotic agents The present invention comprises (4-Piperidinyl)-1H-2-Benzopyran derivatives useful as antipsychotic agents, their intermediates, pharmaceutical compositions and methods of making these compounds. These compounds are useful in treating psychosis.... | 12/21/1999 |
| 5998414 | Troponyl piperazines as dopamine D4 receptor ligands Described herein are compounds of the general formula: ##STR1## a stereoisomer, solvate, or pharmaceutically acceptable salt thereof, wherein: R1 is H, halo, aryl or aryl substituted with one or two groups independently selected from halo,... | 12/07/1999 |
| 5986097 | Spiro[cyclopent[b]indole-piperidines] Novel spiro[cyclopent[b]indole-piperidines], intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the spiro[cyclopent[b]indole-piperidines] and intermediates, or composition... | 11/16/1999 |
| 5981553 | Heterocycle substituted propenoic acid derivatives as NMDA antagonist The present invention is new 3-(heterocyclic)-propenoic acid derivatives and pharmaceutical compositions thereof. These new 3-(heterocyclic)-propenoic acid derivatives are useful as NMDA antagonist.... | 11/09/1999 |
| 5977147 | 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino- 1,3-propanediols and related compounds Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fu... | 11/02/1999 |
| 5972998 | Triptolide derivatives useful in the treatment of autoimmune diseases The present invention relates to novel triptolide derivatives and a method of treating a patient suffering from an autoimmune disease comprising administering to a patient an effective amount of the novel triptolide derivatives.... | 10/26/1999 |
| 5972963 | 3-aryl-2-(1-substituted 4-piperidinyl)-1,1-dioxo-3H-benzo[D]isothiazoles and related compounds This invention relates to 3-aryl-2-(1-substituted-4-piperidinyl)-1,1-dioxo-3H-benzo[d]isothiazoles and related compounds of the formula, ##STR1## where X and Y are independently halogen, loweralkyl, loweralkoxy, arylloweralkoxy, acyl, hydroxy, n... | 10/26/1999 |
| 5965554 | Antipsychotic agents, compositions and method of use This invention relates to compounds of the formula ##STR1## wherein X, Y, Z, m, n and p are as defined within, pharmaceutical compositions containing these compounds and to their use as antipsychotic agents, particularly in the treatment of schizophr... | 10/12/1999 |
| 5962435 | Method of lowering serum cholesterol levels with 2,6-di-alkyl-4-silyl-phenols A method of lowering plasma cholesterol level in a patient with hypercholesterolemia, by administration of a compound of formula (1) ##STR1## wherein: R1, R2, R3 and R4 are each independently a C1 | 10/05/1999 |
| 5959111 | Process for preparing 6-0-monoesters of castanospermine The present invention relates to a process for preparing a compound of formula (I): ##STR1## wherein R is C1 -C10 alkyl, phenyl or substituted phenyl, comprising treating a compound of formula (II): ##STR2## with bis(t... | 09/28/1999 |
| 5948886 | Acylated enol derivatives of -ketoesters and -ketoamides This invention relates to acylated enol derivatives of -ketoesters and -ketoamides. The compounds of this invention are either prodrugs of known elastase inhibitors or are elastase inhibitors in their own right and are useful in the treatmen... | 09/07/1999 |
| 5948798 | Pyridiniminyl-1,2-benzisoxazoles and -benzisothiazoles Novel pyridiniminyl-1,2-benzisoxazoles and -benzisothiazoles, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the 1,2-benzisoxazoles and -benzisothiazoles and intermedi... | 09/07/1999 |
| 5932571 | Substituted N-methyl-N-(4-(4-(1H-benzimidazol-2-yl) {1,4}diazepan-1-yl)-2-(aryl) butyl) benzamides useful for the treatment of allergic diseases The present invention relates to novel N-methyl-N-(4-(4-(1H-benzimidazol-2-yl)1,4!diazepan-1-yl)-2-(aryl)butyl)b enzamide derivatives of the formula: ##STR1## stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful... | 08/03/1999 |
| 5929079 | Trans cyclopentanyl azaadenyl analogs useful as immunosuppressants This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent, Y3, Y5 | 07/27/1999 |
| 5922737 | Substituted N-methyl-N-(4-(4-(1H-Benzimidazol-2-YL-amino) piperidin-1-YL)-2-(arlyl) butyl) benzamides useful for the treatment of allergic diseases The present invention relates to novel substituted N-methyl-N-(4-(4-(1H-benzimidazol-2-yl-amino)piperidin-1-yl)-2-(aryl)butyl )benzamide derivatives of the formula: ##STR1## stereoisomers thereof, and pharmaceutically acceptable salts thereof which ... | 07/13/1999 |
| 5922752 | NMDA (n-methyl-d-aspartate) antagonists The present invention is new excitatory amino acid antagonists (herein referred to as compounds of formula (1)): below: ##STR1## These new antagonists are useful as NMDA (N-methyl-D-aspartate) antagonists.... | 07/13/1999 |
| 5919631 | Method of determining the degree of aggregation of the ଲ-A4 peptide A method of determining the degree of aggregation of the peptide is disclosed. The method comprises reacting the protein with a suitable binding agent which is capable of binding the peptide only in its non-aggregated state to form an ... | 07/06/1999 |
| 5917057 | N-hydroxy-dibenzb,e!oxepinalkylamines, n-hydroxy-dibenzb,e!oxepinalkanoic acid amides and related heterocyclic analogues This invention relates to N-hydroxy-dibenzb,e!oxepinalkylamines, N-hydroxy-dibenzb,e!oxepinalkanoic acid amides and related heterocyclic analogues of the formula ##STR1## where X together with the carbon atoms to which it is attached forms a ... | 06/29/1999 |
| 5916892 | Trans cyclopentanyl deazaadenyl analogs useful as immunosuppressants This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent, Y3, Y5 | 06/29/1999 |
| 5905085 | Trans cyclopentanyl deazaadenyl analogs useful as immunosuppressants This invention relates to novel Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent, Y3 and Y... | 05/18/1999 |
| 5591866 | (1H-indol-1-yl)-2-(amino)acetamide derivatives and preparation thereof There are disclosed compounds having the formula ##STR1## wherein the variables are defined in the specification, and pharmaceutically acceptable addition salts thereof, or where applicable, the optical or geometrical isomers or racemic mixtures ther... | 01/07/1997 |
