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Attorney: Blackwood; Robert K.


Number of patents: 128
Last date: September 26, 1989

1        
NumberTitleIssue Date
4870170Process for 2-(1-oxo-3-thiolanyl)-2-penem antibiotics
Process and intermediates for the conversion of 3R,4R-4-acetoxy-3-[1R-1-(silyloxy)ethyl]-2-acetidinones to antibacterial 5R,6S-6-(1R-1-hydroxyethyl)-2-(1-oxo-3-thiolanylthio)-2-penem-3-carboxylic acids, and the pharmaceutically-acceptable salts and pivalo...
09/26/1989
48682966-(1-carbamoyl-1-hydroxymethyl) penicillanic acid derivatives
6-(1-Carbamoyl-1-hydroxymethyl)penicillanic acid derivatives are useful as antibacterials and/or beta-lactamase inhibitors....
09/19/1989
4868297Process for preparing sultamicillin and analogs
6-Halo- and 6,6-dihalo-1,1-dioxopenicillanoyloxymethyl 6-[D-2-(2-alkoxycarbonyl-1-methylvinylamino- and 1-methyl-3-oxo-1-butenylamino)-2-phenylacetamido]penicillanates and analogs; process for their conversion to sultamicillin and analogs; and proces...
09/19/1989
4864046Process for optically active 3-thiolanyl sulfonate esters
Intermediates and a stepwise process for the conversion of ethyl 4-chloro-3R-hydroxybutyrate to optically active compounds of the formula ##STR1## wherein R is (C1 -C3)alkyl, phenyl or tolyl. The later compounds are in turn usef...
09/05/1989
48618801-phenyl-2(1H,3H)-indolone psycho-therapeutic agents
Certain substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones are highly potent gabaergic agents, valuable in the treatment of individuals suffering from schizophrenia or reversing the side effects of a previously or concurrently administered neurol...
08/29/1989
4859679Antiulcer (alkyldithio) quinoline derivatives
Quaternary 8-(alkyldithio)-1-(2-pyrimidyl)-quinolinium salts, inhibitors of the H30 /K+ ATPase enzyme, are useful in the treatment of ulcers....
08/22/1989
4857641C.12 modified erythromycin A derivatives
Antibacterial 12,12'-anhydro-9R-hydroxy-9-deoxoerythromycin A derivatives, intermediate therefor and process of 12,12'-dehydration....
08/15/1989
4853410Hydroxyacetic acid derivatives for the treatment of diabetic complications
Racemic and chiral (2R,4R)-4-c-hydroxy-2-4-(substituted)chroman(and thiochroman)-4-acetic acids and their pharmaceutically acceptable salts, their use in the treatment of diabetic complications and intermediates therefor....
08/01/1989
4849518Quinazolin-4(3H)-one derivatives as anticoccidial agents
Variously substituted trans-3-[3-(3-hydroxypiperid-2-yl)-2-oxopropyl]quinazoline-4(3H)-ones, a method of controlling or preventing coccidiosis in poultry therewith, intermediates therefor, and a process for the preparation of certain intermediates th...
07/18/1989
4847245N-demethylefrotomycin
N-Demethylefrotomycin, a valuable new antibiotic substance, is produced by the microbial conversion of mocimycin using a novel, efrotomycin-producing, microbial species ATCC 53758....
07/11/1989
4812455Antiinflammatory compositions and methods
An improved antiinflammatory composition and method of treating inflammation which employs a combination of antiinflammatory piroxicam, or a pharmaceutically acceptable salt thereof, with analgesic acetaminophen, antidepressant doxepin, bronchodilator pir...
03/14/1989
4812471Hypoglycemic 5-(isoxazolyl or isothiazolyl)-oxazolidine-2,4-diones
Hypoglycemic 5-chromanyl, 2,3-dihydro-5-benzo[b]-furanyl, 5-pyridyl, 5-quinolyl, 5-pyrrolyl, 5-indolyl, 5-thiazolyl, 5-oxazolyl, 5-isothiazolyl and 5-isoxazolyl oxazolidine-2.4-diones and the pharmacetically-acceptable salts thereof; certain 3-acylated de...
03/14/1989
4803076Controlled release device for an active substance
A device for the controlled release of a substance having useful activity into a fluid medium at a substantially constant rate, said substance contained in a shape which is substantially that of a truncated cone by means of an impermeable wall or coating ...
02/07/1989
4797486Heterocyclic ring fused pyrimidine-4(3H)-ones as anticoccidial agents
Certain trans-3-[3-(3-hydroxy-2-piperidyl)-2-oxopropyl]thieno[3,2-d]pyrimidin-4(3H )-one and furo[3,2-d]pyrimidin-4(3H)-one derivatives, a method of using same as anticoccidial agents, intermediates therefor, and a process for certain intermediates th...
01/10/1989
47973946-(1-carbamoyl-1-hydroxymethyl)penicillanic acid derivatives
6-(1-Carbamoyl-1-hydroxymethyl)penicillanic acid derivatives are useful as antibacterials and/or beta-lactamase inhibitors....
01/10/1989
47941792-(1-oxo-3-thiolanyl)-2-penem antibiotics
Process and intermediates for the conversion of 3R,4R-4-acetoxy-3-[1R-1-(silyloxy)ethyl]-2-azetidinones to antibacterial 5R,6S-6-(1R-1-hydroxyethyl)-2-(1-oxo-3-thiolanylthio)-2-penem-3-carboxylic acids, and the pharmaceutically-acceptable salts and pivalo...
12/27/1988
4782165Process for biotin intermediates
In the synthesis of biotin and decarboxybiotin, a more direct method for the conversion of 1,3-diacyl-4-(bromomethyl)-5-[(5-alkoxycarbonylpentanoyl) or hexanoyl]-4-imidazolin-2-ones to 1,3-diacyl-4-[(4-alkoxybutanoyl) or pentanoyl]-1H,3H-thieno (3,4-...
11/01/1988
4782146Process for the synthesis of penems
A process for the synthesis of penems from azetidinones via 1-aza-4,5-dithiabicyclo[4.2.0]oct-2-en-8-one-2-carboxylate esters....
11/01/1988
4782145Process for penem derivatives
An efficient process for converting readily available 4-acetoxy-2-azetidinones to allyl 2-thioxopenam-3-carboxylates, intermediates useful for the synthesis of penem antibiotics....
11/01/1988
4769232Parenteral formulations of indolmycin
Solutions of indolmycin in a pharmaceutically-acceptable solvent are of special value in the treatment of susceptible bacterial infections in mammals, particularly swine....
09/06/1988
4766117Antiinflammatory compositions and methods
An improved antiinflammatory composition and method of treating inflammation which employs a combination of antiinflammatory piroxicam, or a pharmaceutically acceptable salt thereof, with analgesic acetaminophen, antidepressant doxepin, bronchodilator pir...
08/23/1988
4762838Quinazolin-4(3H)-one derivatives as anticoccidial agents
Variously substituted trans-3-[3-(3-hydroxypiperid-2-yl)-2-oxopropyl]quinazolin-4-(3H)-ones, a method of controlling or preventing coccidiosis in poultry therewith, intermediates therefor, and a process for the preparation of certain intermediates th...
08/09/1988
47629216-(1-acyl-1-hydroxymethyl)penicillanic acid derivatives
6-(1-Acyl-1-hydroxymethyl)penicillanic acid derivatives are useful as antibacterials and/or beta-lactamase inhibitors....
08/09/1988
4761485Synthetic method for indol-2(3H)-ones
A two-step process for the synthesis of certain indol-2(3H)-ones from indoles, and the 3,3-dibromoindol-2(3H)-ones which are intermediates in that process....
08/02/1988
4753956Hypoglycemic 5-substituted oxazolidine-2,4-diones
Hypoglycemic 5-chromanyl, 2,3-dihydro-5-benzo[b]-furanyl, 5-pyridyl, 5-quinolyl, 5-pyrrolyl, 5-indolyl, 5-thiazolyl, 5-oxazolyl, 5-isothiazolyl and 5-isoxazolyl oxazolidine-2,4-diones and the pharmaceutically-acceptable salts thereof; certain 3-acylated d...
06/28/1988
4751297Method for preparation of azetidinone-1-oxoacetate by oxidation of the corresponding 2-hydroxyacetate
A process for production of a 2-azetidinone-1-oxoacetate of the formula ##STR1## useful as an intermediate for preparation of 2-SR2 -substituted-2-penem-3-carboxylate andtibacterial agents; R is a conventional hydroxy protecting group, R1
06/14/1988
4743632Polyetherurethane urea polymers as space filling tissue adhesives
Purified diisocyanate polyetherurethane prepolymers and process therefor. Polyetherurethane urea polymers prepared by mixing said prepolymers with an aqueous solution of an amino, ureido or hydroxy substituted amine or a like-substituted alpha-amino acid,...
05/10/1988
4738972Hypoglycemic thiazolidinediones
Hypoglycemic 5-[1-(5,6,7,8-tetrahydro-2-napthyl-; 1,2,3,4-tetrahydro-6-quinolyl-; 2-indanyl-; and 2-indolyl)alkyl]thiazolidine-2,4-dione derivatives, pharmaceutically acceptable salts thereof, and a method for their use in the treatment of hyperglyce...
04/19/1988
4739047Intermediates for 2-(1-oxo-3-thiolanyl)-2-penem antibiotics
Process and intermediates for the conversion of 3R,4R-4-acetoxy-3-[1R-1-(silyloxy)ethyl]-2-azetidinones to antibacterial 5R,6S-6-(1R-1-hydroxyethyl)-2-(1-oxo-3-thiolanylthio)-2-penem-3-carboxylic acids, and the pharmaceutically-acceptable salts and pivalo...
04/19/1988
4732907Antiprotozoal diamidines and bis-imidazoline
Diamidines of the formula ##STR1## wherein X is a propylene, isobutylene, guanidine, pyrrole, tetrazole, imidazole or substituted imidazole group; and 2-[4-(2-imidazolinyl)phenyl]-6-(2-imidazolinyl)indole, are useful in the treatment of certain ...
03/22/1988
4729985Renin inhibitors containing 5-amino-2,5-disubstituted-4-hydroxypentanoic acid residues
A series of novel polypeptide derivatives, containing 5-amino-2,5-disubstituted-4-hydroxypentanoic acid residues, which are useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin. Particularly valuable precursors for many of these c...
03/08/1988
4727159Triazoles
Antifungal 1-[3-(substituted)-2-hydroxy-2-(perfluoroalkyl)-propyl]triazole derivatives wherein the 3-propyl substituent represents optionally substituted phenoxy, heteroaryloxy, alkylthio, alkylsulfinyl, alkylsulfonyl or optionally substituted carbamoyl....
02/23/1988
4725599Heterocyclic ring fused pyrimidine-4 (3H)-ones as anticoccidial agents
Certain trans-3-[3-(3-hydroxy-2-piperidyl)-2-oxopropyl]thieno[3,2-d]pyrimidin-4(3H )-one and furo[3,2-d]pyrimidin-4(3H)-one derivatives, a method of using same as anticoccidial agents, intermediates therefor, and a process for certain intermediates th...
02/16/1988
4709044Biotin intermediates
In the synthesis of biotin and decarboxybiotin, a more direct method for the conversion of 1,3-diacyl-4-(bromomethyl)-5-[(5-alkoxycarbonylpentanoyl) or hexanoyl]-4-imidazolin-2-ones to 1,3-diacyl-4-[(4-alkoxybutanoyl) or pentanoyl]-1H,3H-thieno(3,4-b...
11/24/1987
4704456Process for sultamicillin intermediate
An improved process for the preparation of the chloromethyl ester of sulbactam (chloromethyl penicillanate 1,1-dioxide), an intermediate in the synthesis of sultamicillin (the mixed methanediol ester of sulbactam and ampicillin)....
11/03/1987
4704461Processes and intermediates for sorbinil
Chiral sorbinil intermediates of the formula ##STR1## wherein R is hydrogen or benzyloxycarbonyl and Y is hydroxy or amino, processes therefor, and processes for the conversion thereof to sorbinil....
11/03/1987
4703052Hypoglycemic thiazolidinediones
Hypoglycemic 2,3-dihydro-5-benzo[b]furanyl-2,3-dihydro-5-benzo[b]thienyl-, 3,4-dihydro(2H)-6-benzopyranyl- and 6-thiochromanyl-thiazolidine-2,4-diones and pharmaceutically acceptable salts thereof, method for their use in treatment of hyperglycemic animal...
10/27/1987
46984441,1-bis(p-fluorophenyl)urea
1,1-Di(p-fluorophenyl)urea, 2-carbobenzoxy-8-fluoro-5-(p-fluorophenyl)-2,3,4,5-tetrahydro-1H-pyrido[4, 3-b]indole, an efficient process for converting the former to the latter, further comprising conversion of the latter to 8-fluoro-5-(p-fluorophenyl)...
10/06/1987
46956261-aza-4,5-dithiabicyclo [4.2.0] oct-2-en-8-one-2 carboxylate esters
1-aza-4,5-dithiabicyclo [4.2.0] oct-2-en-8-one-2 carboxylate ester intermediates useful for the synthesis of penems....
09/22/1987
4695634Hypoglycemic 5-substituted oxazolidine-2,4-diones
Hypoglycemic 5-furyl and 5-thienyl derivatives of oxazolidine-2,4-dione and the pharmaceutically-acceptable salts thereof; certain 3-acylated derivatives thereof; and intermediates useful in the preparation of said compounds....
09/22/1987
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