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| Number | Title | Issue Date |
| 5262412 | Substituted pyrazoles, compositions and use Substituted pyrazole compounds are angiotensin II antagonists and therefore useful in the treatment of hypertension, and related cardiovascular disorders and ocular hypertension. These compounds have the general formula I: ##STR1##... | 11/16/1993 |
| 5254567 | Amorphous (quinolin-2-ylmethoxy)indole compounds which have useful pharmaceutical utility A form of 3-[N-(p-chlorobenzyl)-3-(t-butylthio)-5-(quinolin-2-ylmethoxy)indol-2-yl]- 2,2-dimethylpropanoic acid sodium salt, obtained by freeze or spray drying, is more soluble in water than the crystalline form thereof. The compound is useful as an a... | 10/19/1993 |
| 5254541 | (Quinolin-2-ylmethoxy)indole/cyclodextrin complex A complex of cyclodextrin and 3-[N-(p-chlorobenzyl)-3-(t-buthylthio)-5-(quinolin-2-ylmethoxy)indol-2-yl] -2,2-dimethylpropanoic acid, sodium salt is more soluble in water than the sodium salt alone. The complex is useful as an anti-asthmatic, anti-all... | 10/19/1993 |
| 4871727 | Anti-inflammatory and antidegenerative compounds isolated from L-681,512 There are disclosed anti-inflammatory and antidegenerative compounds which are natural products produced by cultivation of sail microorganism L-681,512 under controlled fermentation conditions.... | 10/03/1989 |
| 4871873 | Process for synthesis of arylglyoxal arylimines A process for producing arylglyoxal arylimine intermediates, by the DMSO/HBr oxidation of arylmethylketones. The imine compounds are intermediates in the synthesis of carbapenem antibiotics, i.e. imipenem.... | 10/03/1989 |
| 4870080 | Polyhydro derivatives of 10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine 10,11-Dihydro-5H-dibenzo[a,d] cyclohepten-5,10-imines and derivatives thereof wherein one or the other or both benzo rings are hydrogenated are active anticonvulsants and atagonists of N-methyl-D-aspartate.... | 09/26/1989 |
| 4870079 | Derivatives of 5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine Fluoro-and hydroxy-derivatives of 5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines wherein the substituents are on non-benzenoid carbons are active anticonvulsants and antagonists of N-methyl-D-aspartate.... | 09/26/1989 |
| 4869791 | Process for preparing 10,11-dihydro-11-exo-hydroxy-5-methyldibenzo[a,d]cyclohepten-5,10-imine 10,11 Dihydro-11-exo-hydroxy-5-methyldibenzo[a,d]cyclohepten-5,10-imine is prepared in a four step synthesis which uses an electrochemical cyclization to form the 5,10-imine bridge in about a 50% yield.... | 09/26/1989 |
| 4868208 | Antifungal agent and method Novel semi-synthetic antifungal compounds which may be produced from 10-[(3-chloro-4-methoxyphenyl)methyl]-6- methyl-3-(2-methylpropyl)-16-[1-(3-phenyloxiranyl)ethyl]-1,4-dioxa- 8,11-diazacyclohexadec-13-ene-2,5,9,12-tetrone isolated from the ferment... | 09/19/1989 |
| 4866186 | Process for the formation of 6-desmethyl-6-exo-methylene derivatives of lovastatin and analogs thereof A process and intermediates in preparation of 6-exomethylene derivatives of lovastatin and 8-acyl and di- and tetrahydro analogs thereof is disclosed.... | 09/12/1989 |
| 4866090 | Novel HMG-CoA reductase inhibitors Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1##... | 09/12/1989 |
| 4866087 | Carboxyalkyl urea compounds and derivatives thereof useful as angiotensin converting enzyme inhibitors and as antihypertensives Carboxyalkyl urea compounds and derivatives thereof are disclosed which are useful as angiotensin converting enzyme (ACE) inhibitors and as antihypertensives. These compounds and derivatives are represented by the general formula: ##STR1## An il... | 09/12/1989 |
| 4866068 | Novel HMG-CoA reductase inhibitors Novel HMG-CoA reductase inhibitors of formulae (I) and (II) are disclosed: ##STR1##... | 09/12/1989 |
| 4864035 | Hydrogenation process for the formation of tetrahydro HMG-CoA reductase inhibitors A novel hydrogenation process, using a homogenous iridium or rhodium catalyst for the reduction of both double bonds of des-(-methylbutyryl)-C-8-hydroxy lovastatin and C-8-amino, C-8-alkoxy and C-6-substituted analogs, is disclosed.... | 09/05/1989 |
| 4863953 | [3R]-3-amino-1-hydroxy pyrrolidin-2-one and its use as a neuroprotective agent The present invention provides R(+)-3-amino-1-hydroxypyrrolidin-2-one of formula I: ##STR1## or pharmaceutically acceptable acid addition salt thereof, which compound is useful as an anticonvulsant agent and in the treatment and/or prevention of... | 09/05/1989 |
| 4863922 | Substituted aromatic sulfonamides as antiglaucoma agents, compositions and use Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.... | 09/05/1989 |
| 4864038 | Antihypercholesterolemic compounds Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1## and pharmaceutically acceptable sal... | 09/05/1989 |
| 4861760 | Ophthalmological composition of the type which undergoes liquid-gel phase transition The present invention relates to a pharmaceutical composition intended for contacting with a physiological liquid characterized in that said composition is intended to be administered as a non-gelled liquid form and is intended to gel in situ, this compos... | 08/29/1989 |
| 4857547 | Novel HMG-CoA reductase inhibitors Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1##... | 08/15/1989 |
| 4857546 | Novel HMG-CoA reductase inhibitors Novel 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1##... | 08/15/1989 |
| 4855481 | Process for the preparation of HMG-CoA reductase inhibitors and intermediate compounds employed therein An intermediate compound of the formula ##STR1## wherein Y is chloro or bromo: Pr is a protecting group selected from benzoyl, acetyl, triphenylsilyl or t-butyldiphenylsilyl: R5 is C1-5 alkyl or benzyl; and R7 is C1-5... | 08/08/1989 |
| 4855456 | Intermediates for 6-alpha-hydroxymethyl HMG-CoA reductase inhibitors This invention discloses intermediates and a process for the preparation of 6-desmethyl-6--hydroxymethyl derivatives of lovastatin and analogs thereof at the 8-acyl side chain.... | 08/08/1989 |
| 4855321 | Antihypercholesterolemic compounds Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1## and pharmaceutically acceptable sal... | 08/08/1989 |
| 4851436 | HMG-CoA reductase inhibitors Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) or (II): ##STR1## wherein: n is 1 to 5; R is hydrogen ... | 07/25/1989 |
| 4847271 | Antihypercholesterolemic ଲ-lactones The compounds of the following general structural formula (I) ##STR1## are 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) synthase inhibitors and useful as antihypercholesterolemic agents for the treatment of disease in which the inhibition of chole... | 07/11/1989 |
| 4847306 | Antihypercholesterolemic compounds Novel 3-hydroxy-3-methylglutaryl-Coenzyme A(HMG-CoA) reductase inhibitors, which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II) ##STR1## and pharmaceutically acceptable salt... | 07/11/1989 |
| 4845237 | Acylation process for the synthesis of HMG-CoA reductase inhibitors A novel acylation process using an alkali metal bromide and a dialkylaminopyridine to form a sterically hindered ester functionality from an alkanoyl chloride and an alcohol is disclosed.... | 07/04/1989 |
| 4841074 | Intermediates and processes for 6-carboxy HMG-CoA reductase inhibitors This invention discloses intermediates and a process for the preparation of 6-desmethyl-6-carboxy derivatives of lovastatin and analogs thereof at the 9-acyl side chain.... | 06/20/1989 |
| 4837205 | Prodrugs of antihypercholesterolemic compounds Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## are disclosed.... | 06/06/1989 |
| 4833258 | Intermediates useful in the preparation of HMG-COA reductase inhibitors Novel intermediates and a novel process for their preparation, where said intermediates are useful in the preparation of 6-hydroxymethyl and related oxidation derivatives of mevinolin and analogs thereof, are disclosed.... | 05/23/1989 |
| 4831165 | Hydrogenation process for the formation of 3,4-dihydro HMG-CoA reductase inhibitors A novel hydrogenation process using a homogenous rhodium catalyst for selectively reducing the 3,4 double bond in the polyhydronaphthyl ring of lovastatin, simvastatin or C-8-acyl or C-6-substituted analogs thereof is disclosed.... | 05/16/1989 |
| 4828992 | Process for the manufacture of an antifungal antihypercholesterolemic .beta . The process for the manufacture of the compound of the general structural formula ##STR1## which is a 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) synthase inhibitor and useful as an antihypercholesterolemic agent for the treatment of disease ... | 05/09/1989 |
| 4826999 | Hydrogenation process for the formation of 3,5-dihydro HMG-CoA reductase inhibitors A novel hydrogenation process, using a homogenous iridium or rhodium catalyst for selectively adding hydrogen to the 3,5 positions in the polyhydronaphthyl ring of lovastatin, simvastatin or C-8-acyl or C-6-substituted analogs thereof, is disclosed.... | 05/02/1989 |
| 4820850 | Process for -C-alkylation of the 8-acyl group on mevinolin and analogs thereof A process for alkylating the alpha position of the 8-acyl side chain in mevinolin and analogs thereof is disclosed. The process proceeds with a single charge of base and alkyl halide to give products with a pharmaceutically acceptable purity.... | 04/11/1989 |
| 4795811 | Intermediates for preparing HMG-CoA reductase inhibitors A process for converting 6-carboxy to 6-hydroxymethyl mevinolin analogs and novel intermediates formed in this process are disclosed.... | 01/03/1989 |
| 4789682 | Antihypercholesterolemic compounds Novel antihypercholesterolemic compounds of structure (I) or (II), ##STR1## pharmaceutically acceptable salts, thereof and a novel process for preparing compounds of structure I, are disclosed.... | 12/06/1988 |
| 4772626 | Antihypercholesterolemic compounds Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1## and pharmaceutically acceptable sal... | 09/20/1988 |
| 4771071 | Antihypercholesterolemic compounds Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1## and pharmaceutically acceptable sal... | 09/13/1988 |
| 4766145 | Antihypercholesterolemic compounds Novel 3-hydroxy-3-methylglutaryl-Coenzyme A(HMG-CoA) reductase inhibitors, which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II) ##STR1## and pharmaceutically acceptable salt... | 08/23/1988 |
| 4751244 | Compounds useful in treating sickle cell anemia The present invention is directed to compounds of the general formula I and pharmaceutically acceptable salts thereof: ##STR1## wherein: R1 =HO or HOOC(CH2)x CHR2 NH--; R2 =H, lower alkyl, benzyl or -... | 06/14/1988 |
