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Attorney: Richardson; Peter C., Benson; Gregg C., Jones; James T.


Number of patents: 56
Last date: June 03, 2003

1    
NumberTitleIssue Date
6573383Preparation of anhydrous CETP inhibitor
This invention relates to methods for preparing anhydrous CETP inhibitor, (2R,4S)-4-[(3,5-bis-trifluoromethyl-benzyl)-methoxycarbonyl-amino]-2-ethyl -6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester....
06/03/2003
6537573Combination dosage form comprising cetirizine and pseudoephedrine
A dosage form containing cetirizine as an immediate release component and pseudoephedrine or a pharmaceutically acceptable salt thereof as a controlled release component. A portion of the pseudoephedrine can also be incorporated as an immediate release co...
03/25/2003
6534511Bicyclic heterocyclic compounds for the treatment of impotence
The use of certain 6-arylpyrazolo[3,4-d]pyrimidin-4-ones, 2 arylquinazolin-4-ones, 2-arylpurin-6-ones and 2-arylpyrido[3,2-d]pyrimidin-4-ones, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing either entity, for the...
03/18/2003
6503908Pharmaceutically active compounds
There is provided compounds of formula I, ##STR1## wherein R1, R2, R3 and Het1 have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which ...
01/07/2003
6469012Pyrazolopyrimidinones for the treatment of impotence
The use of a compound of formula (I) ##STR1## wherein R1 is H; C1 -C3 alkyl; C1 -C3 perfluoroalkyl; or C3 -C5 cycloalkyl; R2 is H; optionally substituted C1...
10/22/2002
6458951Pyrazolopyrimidinone cGMP PDE5 inhibitors for the treatment of sexual dysfunction
Compounds of the formulae (IA) and (IB): ##STR1## wherein R1 is C1 to C3 alkyl optionally substituted with phenyl, Het or a N-linked heterocyclic group selected from piperidinyl and morpholinyl; wherein said phenyl group i...
10/01/2002
6420557Crystalline therapeutic agent
A polymorph of 1-{6-ethoxy-5-[3-ethyl-6,7-dihydro-2-(2-methoxyethyl)-7-oxo-2H-pyrazolo[4, 3-d]pyrimidin-5-yl]-3-pyridylsulfonyl}-4-ethylpiperazine....
07/16/2002
6407114Pyrazolopyrimidinone CGMP PDE5 inhibitors for the treatment of sexual dysfunction
There is provided compounds of formula IA and of formula IB, ##STR1## wherein R1, R2, R3, R4 and A have meanings given in the description, which are useful in the curative and prophylactic treatment of a medical...
06/18/2002
6399777Inclusion complexes of aryl-heterocyclic salts
The esylate, mesylate, and tartrate salts of ziprasidone exhibit excellent solubilities in cyclodextrins....
06/04/2002
6333330Pyrazolopyrimidinone CGMP PDE5 inhibitors for the treatment of sexual dysfunction
There is provided compounds of formula IA and of formula IB, ##STR1## wherein R1, R2, R3, R4 and A have meanings given in the description, which are useful in the curative and prophylactic treatment of medical c...
12/25/2001
63003354-aminoquinazoline derivative cGMP-PDE inhibitors for the treatment of erectile dysfunction
4-aminoquinazoline derivatives which are selective inhibitors of cGMP PDE are useful in the treatment of erectile dysfunction (impotence) in male animals, including man....
10/09/2001
6251904Pyrazolopyrimidinone cGMP PDE5 inhibitors for the treatment of sexual dysfunction
Compounds of the formulae (IA) and (IB): ##STR1## wherein R1 is C1 to C3 alkyl optionally substituted with phenyl, Het or a N-linked heterocyclic group selected from piperidinyl and morpholinyl; wherein said phenyl group i...
06/26/2001
62357425-substituted pyrazolo[4,3-D]pyrimidin-7-ones
Compounds are disclosed which are useful as PDE1 inhibitors. The compounds have the formula: ##STR1##...
05/22/2001
6232304Inclusion complexes of aryl-heterocyclic salts
Compositions of matter comprising a pharmaceutically acceptable salt of an aryl-heterocyclic compound, such as ziprasidone, in a cyclodextrin. Preferred cyclodextrins are SBECD and HPBCD. The composition can comprise a dry mixture, a dry inclusion complex...
05/15/2001
6171618Combination dosage form comprising cetirizine and pseudoephedrine
A dosage form containing cetirizine as an immediate release component and pseudoephedrine or a pharmaceutically acceptable salt thereof as a controlled release component. A portion of the pseudoephedrine can also be incorporated as an immediate release co...
01/09/2001
6166025Pharmaceutical compositions containing eletriptran hemisulphate and caffeine
The present invention provides an aqueous pharmaceutical composition comprising 5 to 200 mg/ml of eletriptan hemisulfate and from 0.5 to 2.0% weight/volume of caffeine....
12/26/2000
6153746Process for making a cyclodextrin
Sulfoalkyl ether cyclodextrins are produced by a process of treating an unsubstituted cyclodextrin starting material with an alkyl sultone in the presence of a base. The base is added in a stepwise, pH controlled manner so that substantially the entire in...
11/28/2000
6150366Ziprasidone formulations
Compositions comprising crystalline ziprasidone free base or crystalline ziprasidone hydrochloride particles having a mean particle size less than 85 μm, and a pharmaceutically acceptable carrier, are substantially bioequivalent and can be used to treat ...
11/21/2000
6106864Pharmaceutical formulations containing darifenacin
There is provided a pharmaceutical dosage form adapted for administration to the gastrointestinal tract of a patient, comprising darifenacin, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable adjuvant, diluent or carrier, ch...
08/22/2000
6100270Bicyclic heterocyclic compounds for the treatment of impotence
A method of treating male erectile dysfunction comprising administering to a male human a pyrimidine compound of formula I....
08/08/2000
6080761Inhibition of smooth muscle cell migration by (R)-amlodipine
The R(+) isomer of amlodipine is a potent inhibitor of smooth muscle cell migration despite its lack of calcium channel-blocking activity. It is useful for treating atherosclerosis, re-stenosis after angioplasty and endometriosis....
06/27/2000
6071938Benzopyrans
A compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein X, O R, R1, R2, R3, and R4 are defined in the specification; compositions containing such compounds; intermediates ...
06/06/2000
6068859Controlled-release dosage forms of Azithromycin
A controlled-release dosage form of azithromycin having an improved side effect profile; a process for preparing the dosage form; and a method of treating a microbial infection, comprising administering azithromycin in such a controlled-release dosage for...
05/30/2000
6066735Process for preparing sildenafil
A process for the preparation of a compound of formula (I): ##STR1## which comprises cyclization of a compound of formula (II): ##STR2##...
05/23/2000
6046338Separation of the enantiomers of amlodipine via their diastereomeric tartrates
A method for the separation of R-(+)- and S-(-)-isomers of amlodipine (I) from mixtures thereof, which comprises the reaction of the mixture of isomers with either L- or D-tartaric acid in an organic solvent containing sufficient dimethyl sulphoxide (DMSO...
04/04/2000
5977124ଲ-adrenergic agonists
ଲ-adrenergic agonists for the treatment of diseases/conditions such as obesity and diabetes. The compounds have formula (I), wherein R1, R2, R3, R4, R5, R6, R7, W, X, Y and Z ar...
11/02/1999
5955611Process for preparing sildenafil
A process for the preparation of a compound of formula (I): ##STR1## which comprises cyclization of a compound of formula (II): ##STR2##...
09/21/1999
5952326Tetralin and chroman derivatives useful in the treatment of asthma, arthritis and related diseases
Compounds of the formula ##STR1## wherein R is an optionally substituted heteroaryl group such as 2-chromanyl, 2-pyridyl or 5-fluoro-2-benzothiazoyl; X is O, S or (CH2)m ; R1 is phenyl or pyridyl, optionally substituted by...
09/14/1999
5922747Indole derivatives as steroid 5଱-reductase inhibitors
A method of treatment of a human to inhibit a steroid 5଱-reductase, particularly a testosterone 5଱-reductase, which comprises treating said human with an effective amount of a compound of the formula (I) ##STR1## or a pharmaceutically acc...
07/13/1999
5919795Biphenyl-2-carboxylic acid-tetrahydro-isoquinolin-6-yl amide derivatives, their preparation and their use as inhibitors of microsomal triglyceride transfer protein and/or apolipoprotein B (Apo B) secretion
Compounds of formula (I), ##STR1## wherin X is CH2, CO, CS or SO2 ; Y is selected from: a direct link, aliphatic hydrocarbylene radicals having up to 20 carbon atoms, which radical may be mono-substituted by hydroxy, (C1
07/06/1999
5912244Benzopyrans
A compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein X is O, S or NH; R and R1 are each independently selected from H and C1 -C4 alkyl or taken together represent C2 -C...
06/15/1999
5876752Use of interfacially-polymerized membranes in delivery devices
Devices for controlled release of active substances in the form of tablets, capsules and beads comprised of a porous substructure surrounded by one or more interfacial membranes....
03/02/1999
5763467Hypoglycemic hydroxyurea derivatives
Certain 1-(benzyl or 5-benzofuranylmethyl)-1-hydroxyurea derivatives are useful as hypoglycemic and hypocholesterolemic agents....
06/09/1998
5750707Separation of the enantiomers of amlodipine via their diastereomeric tartrates
A method for the separation of R-(+)- and S-(-)-isomers of amlodipine (I) from mixtures thereof, which comprises the reaction of the mixture of isomers with either L- or D-tartaric acid in an organic solvent containing sufficient dimethyl sulphoxide (DMSO...
05/12/1998
5719283Intermediates useful in the synthesis of pyrazolopyrimidinone antianginal agents
Compounds of the formula ##STR1## wherein R1 is H, C1 -C3 alkyl, C3 -C5 cycloalkyl or C1 -C3 perfluoroalkyl; R2 is H, C1 -C6 alkyl optionally sub...
02/17/1998
5698550Tetralin and chroman derivatives useful in the treatment of asthma, arthritis and related diseases
Compounds of the formula ##STR1## wherein R is an optionally substituted heteroaryl group such as 2-chromanyl, 2-pyridyl or 5-fluoro-2-benzothiazoyl; X is O, S or (CH2)m ; R1 is phenyl or pyridyl, optionally substituted by...
12/16/1997
5696146Indole derivatives as steroid 5଱-reductase inhibitors
Compounds of formula (I) ##STR1## and the pharmaceutically acceptable base salts thereof, wherein R is --CO2 H or tetrazol-5 yl; R1 is C3 -C8 alkyl optionally substituted by fluoro; and R2 is C
12/09/1997
5686587Intermediate for azithromycin
A compound having formula (III). Also, a process of making azithromycin comprising reducing the compound of formula (III) and N-methylating the reduced product....
11/11/1997
5677324Benzopyranes as potassium channel openers
The present invention relates to compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein the dashed line represents an optional covalent bond; X is O, NH, S or a direct link; R3 is hydroxy when the dashed line does n...
10/14/1997
5648502Regioselective synthesis of 4-chloro-2-thiophenecarboxylic acid
4-Chloro-2-thiophenecarboxylic acid is made by forming a compound of formula (Ia), disclosed herein, wherein R3 is (C1 -C6) alkyl, phenyl, or benzyl; converting the compound to a compound of formula (IVa), disclosed herein...
07/15/1997
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