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Attorney: Szatkowski; Thomas S.


Number of patents: 129
Last date: November 18, 2003

1        
NumberTitleIssue Date
6649756PROCESS IMPROVEMENT IN THE PREPARATION OF (4R, 5S, 6S)-3-[[(2R,3R)-2-[[[(S)-2-AMINO-3-METHYL-1-OXOBUTYL]AMINO]METHYL]TETRAHYD RO-3-FURANYL]THIO]-6-[(R)-1-HYDROXYETHYL]-4-METHYL-7-OXO-1-AZABICYCLO[3.2. 0]HEPT-2-ENE-2-CARBOXYLIC ACID
The invention is a process improvement for producing the carbapenem antibacterial agent (4R, 5S, 6S)-3-[[2R,3R)-2-[[[(S)-2-amino-3-methyl-1-oxobutyl]amino]methyl]tetrahydr o-3-furanyl]thio]-6-[R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2. 0]hept...
11/18/2003
6635261Adjuvant and vaccine compositions containing monophosphoryl lipid A
The invention pertains to adjuvant and vaccine compositions of monophosphoryl lipid A, sugar and optionally an amine based surfactant, which when frozen and thawed or lyophilized and reconstituted reform a colloidal suspension having a light transmission ...
10/21/2003
6306404Adjuvant and vaccine compositions containing monophosphoryl lipid A
The invention pertains to adjuvant and vaccine compositions of monophosphoryl lipid A, sugar and optionally an amine based surfactant, which when frozen and thawed or lyophilized and reconstituted reform a colloidal suspension having a light transmission ...
10/23/2001
54420599-[(substituted glycyl)amido)]-6-demethyl-6-deoxytetracyclines
The invention provides compounds of the formula: ##STR1## wherein R, and R1 and W are defined in the specification. These compounds are useful as antibiotic agents....
08/15/1995
5430150Retroviral protease inhibitors
Compounds of the formula I: ##STR1## wherein X, Y, Z, a, b, c, R1, R2, R3, R4 and R5 are defined in the specification are provided. The compounds are useful as inhibitors of retroviral protease e...
07/04/1995
5428167Asymmetric synthesis of intermediates for retroviral protease inhibitor compounds
The disclosure describes an improved process for producing optically active compounds of Formula II or III, which compounds are useful as intermediates for preparing compounds active as inhibitors of retroviral protease enzymes: ##STR1## wherein...
06/27/1995
5407917Compositions and methods for the enhancement of performance in meat-producing animals and for the treatment and control of disease therein
Methods for increasing the growth rate and increasing the efficiency of food utilization of meat-producing animals and for treating bacterial infections in said animals by administering an effective amount of selected antibiotics derived from the microorg...
04/18/1995
5405849Angiotensin II receptor blocking 2,3,6 substituted quinazolinones
Novel quinazolinone compounds of the formula: ##STR1## wherein R5, R6, R7, R8, R and X are defined in the specification, which have angiotensin II (AII) antagonizing activity, intermediates useful in the pr...
04/11/1995
54017297-(substituted)-9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines
The invention provides compounds of the formula: ##STR1## wherein R, R3, R4 and W are defined in the specification. These compounds are useful as antibiotic agents....
03/28/1995
54018639-amino-7-(substituted)-6-demethyl-6-deoxytetracyclines
Novel 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the no...
03/28/1995
5381912Package having a press-and-turn type cap and bottle with ramped gripping portions
An improved child-resistant package allowing improved access and closure by the user is provided. The improved packages is of the press-and-turn type and features ramped gripping portions on the perimeter of the side of the press-and-turn cap and on the b...
01/17/1995
53808887-(substituted)-9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines
The invention provides compounds of the formula: ##STR1## wherein R, R3, R4 and W are defined in the specification. These compounds are useful as antibiotic agents....
01/10/1995
53710769-[(substituted glycyl)amido]-6-(substituted)-5-hydroxy-6-deoxytetracyclines
The invention provides compounds of the formula: ##STR1## wherein R, R1, R2 and W are defined in the specification. These compounds are useful as antibiotic agents....
12/06/1994
53691022-substituted alkyl-3-carboxy carbopenems as antibiotics and a method of producing them
The invention relates to new 2-substituted alkyl-3-carboxy carbapenems having the formula: ##STR1## with R1, R2, R3, X and Y defined hereafter as antibiotics and beta lactamase inhibitors produced by a novel Michael ...
11/29/1994
5358947Angiotensin II receptor blocking 2,3-substituted pyrazolo[1,5-a]-1,3,5-triazin-4(3H)-ones
The invention provides novel 2,3-substituted pyrazolo[1,5-a]-1,3,5-triazin-4(3H)-ones having the formula: ##STR1## wherein R1, R2 and R3 are described in the specification which have activity as angiotensin II (AII) a...
10/25/1994
5358951Angiotensin II receptor blocking 2, 3, 6 substituted quinazolinones
This disclosure describes novel 2,3,6, substituted quinazolinones of the formula: ##STR1## wherein R1, R6 and X are described in the specification which have activity as angiotensin II (AII) antagonistis....
10/25/1994
5296480Angiotensin II receptor blocking 2,3,6-substituted 5,6,7,8-tetra-hydro-pyrido[4,3]pyrimidin-4(3H)-ones
The invention provides compounds having the formula ##STR1## wherein R, X and R6 are defined in the specification which have activity as angiotensin II antagonists....
03/22/1994
5292742Angiotensin II receptor blocking 2,3,6 substituted quinazolinones
The invention provides novel 2,3,6-substituted quinazolinones having the formula ##STR1## wherein X, R, R6 are described in the specification which have activity as angiotensin II (AII) antagonists....
03/08/1994
5290780Angiotensin II receptor blocking 2,3,6 substituted quinazolinones
Novel quinazolinone compounds of the formula: ##STR1## wherein R5, R6, R7, R8, R and X are defined in the specification, which have angiotensin II (AII) antagonizing activity, intermediates useful in the pr...
03/01/1994
5288720Angiotensin II receptor blocking 2,3,6 substituted quinazolinones
Novel 2, 3, 6 substituted quinazolinones of the formula: ##STR1## wherein R, R6 and X are described in the specification are disclosed. The compounds which have activity as angiotensin II (AII) antagonists....
02/22/1994
5286729Angiotensin II receptor blocking 2,3,6 substituted quinazolinones
The invention provides novel 2,3,6 substituted quinazolinones having the formula ##STR1## wherein R, R5, R6, R7, R8 and X are described in the specification which have activity as angiotensin II (AII) antag...
02/15/1994
5284853Angiotensin II receptor blocking 2,3,6 substituted quinazolinones
The invention provides novel 2, 3, 6 substituted quinazolinones of the formula ##STR1## wherein, R, R6 and X are defined in the specification which have activity as angiotensin II (AII) antagonists....
02/08/1994
5281603Angiotensin II receptor blocking 2,3,6 substituted quinazolinones
The invention provides novel 2,3,6-substituted quinazolinones having the formula ##STR1## wherein R6 is ##STR2## and X, R, R1, R2, R3, R4 and R8 are described in the specific...
01/25/1994
52816289-amino-7-(substituted)-6-demethyl-6-deoxytetracyclines
9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel co...
01/25/1994
5281604Angiotensin II receptor blocking 2,3,6-substituted quinazolinones
The invention provides novel 2,3,6 substituted quinazolinones of the formula ##STR1## wherein X, R and R6 are defined in the specification which have activity as angiotensin II (AII) antagonists....
01/25/1994
5281602Angiotensin II receptor blocking 2,3,6-substituted 5,6,7,8-tetrahydro-pyrido[4,3-D]pyrimidin-4(3H)-ones
The invention provides novel 2,3,6-substituted 5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4 (3H)-ones of the formula ##STR1## wherein X, R and R6 are described in the specification which have activity as angiotensin II (AII) antagonists....
01/25/1994
5262173Pulsatile once-a-day delivery systems for minocycline
Pharmaceutical delivery systems containing 7-dimethyl-6-deoxy-6-demethyltetracycline or a non-toxic acid addition salt thereof comprising mixtures of a minor proportion of slow-release blended polymer coated spherical granules adapted to release part of t...
11/16/1993
5248797Method for the production of 9-amino-6-demethyl-6-deoxytetracycline
The invention relates to a novel method for producing [4S-(4alpha, 12aalpha)]-9-amino-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3, 10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide, hereinafter called 9-amino-6-demethyl-6-deoxytetracycline...
09/28/1993
5229411Substituted benz[cd]indol-2-(1H)-ones and use as antihypertensive agents
Compounds of the formula: ##STR1## wherein R1, R2 and m are defined in the specification are provided. These compounds are useful as antihypertensive agents....
07/20/1993
5222529Filling apparatus
An apparatus for filling finely powdered material into a long and narrow cavity or hole having a relatively small opening is provided. The apparatus features a discharge port for a particulate laden gas stream directed toward the opening of the hole to be...
06/29/1993
5212291Anthracycline derivatives as solubilized pro-drugs
The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guanidine, isourea, isothiourea and biguanide functions ...
05/18/1993
5208223Phosphocholine derivative inhibitors of phospholipase A2
Phospocholine derivatives having the formula: ##STR1## in which W, Z, Q and R are described in the specification are disclosed as useful for inhibiting the enzyme phospholipase A2. Methods of making and using the compounds are also disclos...
05/04/1993
5173510Simplified thioester and isostere analogs of oleoyl coenzyme A as hypocholesterolemic agents
New thioester and ester, amide and ketone isostere analogs of oleoyl coenzyme A, useful as antiatherosclerotic agents, are provided. The compounds have the formula: ##STR1## wherein A is selected from the group consisting of ##STR2## Y is s...
12/22/1992
5173488Stable injectable pharmaceutical formulation for folic acid and leucovorin salts and method
Injectable aqueous compositions comprising folic acid and leucovorin and their salts, optionally including benzyl alcohol, sodium chloride and agents for adjusting pH are stabilized and buffered in the range of 6 to 10 by adding a combination of trometham...
12/22/1992
5162328N-[3-[2-(1H-imidazol-1-yl)ethoxy]phenyl]-4-(2-thienyl)-2-pyrimidinamine and pharmacologically acceptable salts
N-[3-[2-(1H-Imidazol-1-yl)ethoxy]phenyl]-4-(2-thienyl)-2-pyrimidinamine and pharmacologicaly acceptable salts, useful as antiasthma agents and treatment of allergic diseases and exhibiting improved bioavailability properties....
11/10/1992
5144045Phosphocholine derivative inhibitors of phospholipase A2
Phospocholine derivatives having the formula: ##STR1## in which W, Z, Q and R are described in the specification are disclosed as useful for inhibiting the enzyme phospholipase A2. Methods of making and using the compounds are also disclos...
09/01/1992
5116827Quinolinecarboxylic acid derivatives as solubilized pro-drugs
The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guanidine, isourea, isothiourea and biguanide functions ...
05/26/1992
5114720Gelatin coated tablets and method for producing same
Pharmaceutical tablets having increased slipperiness and swallowability are provided. The enhanced swallowability is imparted by an overcoat of a low bloom gelatin, which overcoat has a lower coefficient of friction than other known coatings....
05/19/1992
5114946Transdermal delivery of pharmaceuticals
Compositions and methods for the transdermal delivery of pharmacologically active chiral compounds are described which are based on the use of enantiomers or mixtures that contain a disproportionate amount of the enantiomers....
05/19/1992
51030155-(substituted)isoxazole compounds
A novel process for producing ଱-[(dialkylamino)substituted-methylene]ଲ-oxo-(substituted) propanenitriles of the formula: ##STR1## where R, R1 and R2 are defined in the specification by reacting a substituted iso...
04/07/1992
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