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Attorney: Richardson; Peter C., Lumb; J. Trevor, Blackwood; Robert K.


Number of patents: 37
Last date: October 22, 1991

NumberTitleIssue Date
5059609Substituted tetralins, chromans and related compounds in the treatment of asthma, arthritis and related diseases
Substituted tetralins, chromans and related compounds which, by inhibiting 5-lipoxygenase enzyme and/or blocking leukotriene receptors, are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related di...
10/22/1991
5036099Anhydrous, crystalline sodium salt of 5-chloro-3-(2-thenoyl)-2-oxindole-1-carboxamide
Anhydrous, crystalline sodium salt of 5-chloro-3-(2-thenoyl)-2-oxindole-1-carboxamide having advantageous properties for formulation as an analgesic or antiinflammatory agent....
07/30/1991
5036104Cycloalkyl-substituted glutaramide diuretic agents
2-Acylaminoalkyl-3-[1-(carboxycycloalkylcarbamoyl)cycloalkyl]propanoic acid derivatives (which may also be viewed as glutaramide derivatives) are useful in the treatment of hypertension, heart failure and renal insufficiency, based upon their inhibition o...
07/30/1991
5036155Process for isopropyl 3S-amino-2R-hydroxy-alkanoates
Process and intermediates for isopropyl 3S-amino-4-cyclohexyl-2R-hydroxybutyrate and 3S-amino-2R-hydroxy-5-methylhexanoate from R-malic acid. These products are of known utility in the synthesis of certain renin inhibitors....
07/30/1991
5023085Transdermal flux enhancers in combination with iontophoresis in topical administration of pharmaceuticals
Transdermal flux enhancers such as oleic acid and 1-dodecylazacycloheptan-2-one are used in combination with iontophoresis in the topical administration of pharmaceutical agents....
06/11/1991
5013729Diastereomeric 5R,6S-6-(1R-hydroxyethyl)-2-(cis-1-oxo-3-thiolanylthio)-2-penem-3-carbox ylic acids
Diastereomeric 5R,6S-6-(1R-hydroxyethyl)-2-(1S-oxo-3R-thiolanylthio)-2-penem-3-carboxylic acid and 5R,6S-6-(1R-hydroxyethyl)-2-(1R-oxo-3S-thiolanylthio )-2-penem-3-carboxylic acid, and pharmaceutically-acceptable salts and in vivo hydrolyzable esters...
05/07/1991
5013839Process for optically active 2-alkyl-2,5-diazabicyclo(2.2.1) heptanes
1S,4S and 1R,4R-2-alkyl-2,5-diazabicyclo[2.2.1]-heptanes useful as intermediates in the synthesis of certain antibacterial quinolones, are prepared respectively, from trans-4-hydroxy-L-proline and trans-4-hydroxy-D-proline via multistep procedures....
05/07/1991
5010185Processes for tigogenin beta-cellobioside
Improved processes for the synthesis of tigogenin beta-cellobioside, a known hypocholesterolemic agent, using cellobiose heptaacetate and tigogenin as starting materials....
04/23/1991
4997949Crystalline 2-(1-pentyl-3-guanidino)-4-(2-methyl-4-imidazolyl) thiazole dihydrochloride trihydrate
Crystalline 2-(1-pentyl-3-guanidino)-4-(2-methyl-4-imidazolyl)thiazole dihydrochloride trihydrate having advantageous properties....
03/05/1991
4997981Processes for 2-(1-pentyl-3-guanidino)-4-(2-methyl-4-imidazolyl) thiazole and analogs
An amine substituion process for 2-(1-pentyl-3-guanidino)-4-(2-methyl-4-imidazolyl)thiazole, for precursor N-(pentylamidino)thiourea, and for analogs thereof of said compounds....
03/05/1991
4994457Antiinflammatory compositions and methods
An improved antiinflammatory composition and method of treating inflammation which employs a combination of a non-steroidal antiinflammatory agent such as piroxicam, or a pharmaceutically acceptable salt thereof, with 5'-guanylic acid or N-acetyl-L-methio...
02/19/1991
4992562Renin 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...
02/12/1991
4992543Penem derivatives
An efficient, multistep process for the synthesis of certain 6-(1-hydroxyethyl) 2-substituted penem antibiotics from 2-[4R-(triphenylmethylthio)-3S-(1R-(dimethyl-t-butylsilyloxy)ethyl)-2-azet idon-1 yl]acetic acid ester....
02/12/1991
4992369Fermentation process for glycopeptide antibiotic
A new glycopeptide antibiotic UK-68,597 can be prepared by submerged aerobic propagation in aqueous nutrient media of Actinoplanes sp. ATCC 53533. The antibiotic and its cationic salts are active against a variety of microorganisms and are effective in co...
02/12/1991
4987231Optical resolution method for 3R-(3-carboxybenzyl)-6-(5-fluoro-2-benzothiazolyl)methoxy-4R-chromanol
Preparative method for 3R-(3-carboxybenzyl)-6-(5-fluoro-2-benzothiazolyl)methoxy-4R-chromanol via its salt with quinine....
01/22/1991
4977178Method of treating anxiety and depression with 1-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...
12/11/1990
4968707Oxazolidin-2-one derivatives as hypoglycemic agents
Certain 4-[2-(5-(optionally-substituted-aryl- and heteroaryl)oxazolidin-2-on-3-yl)alkyl]benzoic acids and ester, glycinamide, oxazole and thiazolidinedione derivatives thereof are useful as hypoglycemic agents....
11/06/1990
4965372Process and intermediates for isopropyl 3S-amino-2R-hydroxy-alkanoates
Process and intermediates for isopropyl 3S-amino-4-cyclohexyl-2R-hydroxybutyrate and 3S-amino-2R-hydroxy-5-methylhexanoate from R-malic acid. These products are of known utility in the synthesis of certain renin inhibitors....
10/23/1990
4960792Cycloalkyl-substituted glutaramide diuretic agents
2-Acylaminoalkyl-3-[1-(carboxycycloalkylcarbamoyl)cycloalkyl]propanoic acid derivatives (which may also be viewed as glutaramide derivatives) are useful in the treatment of hypertension, heart failure and renal insufficiency, based upon their inhibition o...
10/02/1990
4959365Topical compositions of lipophilic pharmaceuticals agents
Improved pharmaceutical compositions for the topical administration of a lipophilic, pharmaceutical agent to a human or lower animal subject comprising a safe and effective amount of a pharmaceutical agent, an aqueous solvent system comprising from about ...
09/25/1990
4954647Process for optically active 3-(methane-sulfonyloxy) thiolane and analogs
Intermediates and a stepwise process for the conversion of D-methionine or certain of its derivatives to optically active compounds of the formula ##STR1## wherein R is (C1 -C3)alkyl, phenyl or tolyl. The latter compounds are in...
09/04/1990
4954482New glycopeptide antibiotic
A new glycopeptide antibiotic UK-68,597 can be prepared by submerged aerobic propagation in aqueous nutrient media of Actinoplanes sp. ATCC 53533. The antibiotic and its cationic salts are active against a variety of microorganisms and are effective in co...
09/04/1990
4948913Renin 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...
08/14/1990
4940823Process for optically active 3-thiolanyl sulfonate esters
Intermediates and a stepwise process for the conversion of an alkyl 4-chloro-3R-hydroxybutyrate to optically active compounds of the formula ##STR1## wherein R is (C1 -C3) alkyl, phenyl or tolyl. The latter compounds are in turn...
07/10/1990
4937184N-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....
06/26/1990
4933475Pharmacologically active 4-[2-hydroxy-4-(substituted)phenyl]naphthalen-2(1H)-ones and 2-ols, derivatives thereof and intermediates therefor
Compounds having the formula ##STR1## R1 is hydrogen, benzyl or alkanoyl, X is C2-4 alkylene; and Z-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidia...
06/12/1990
4921994Pharmacologically active 2-hydroxy-4-(substituted) phenyl cycloalkanes and derivatives thereof
Compounds having the formula ##STR1## R1 is hydrogen, benzyl or an ester moiety; Y is --CH(R2 ")CH(R2)-- or --CH(R3)CH2 --; R2 " is hydrogen or methyl; R2 is OH or X-substituted ...
05/01/1990
4921972Process for optically active 3-thiolanyl sulfonate esters
Intermediates and a stepwise process for the conversion of an alkyl 4-chloro-3R-hydroxybutyrate to optically active compounds of the formula ##STR1## wherein R is (C1 -C3)alkyl, phenyl or tolyl. The latter compounds are in turn ...
05/01/1990
4920224Quinazolin-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 the...
04/24/1990
4920050Acidic polycyclic ether antibiotic
An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Streptomyces sp. ATCC 53862. This novel antibiotic is useful as an anticoccidial in chickens, in the preventi...
04/24/1990
4920215Antibiotic produced by fermentation
The antibiotic of the formula: ##STR1## wherein R is ##STR2## The antibiotic is useful for the treatment of swine dysentery and for promoting growth and/or increasing the efficiency of food utilization in poultry, swine and ruminants....
04/24/1990
4916226Optical resolution method for 3S-(3-pyridylmethyl)-6-(2-quinolyl)-methoxy-4S-chromanol
Preparative method for 3S-(3-pyridylmethyl)-6-(2-quinolyl)methoxy-4S-chromanol via its salt with natural tartaric acid....
04/10/1990
4895940Process for the preparation of penems
An efficient, multistep process for the synthesis of 6-(1-hydroxyethyl) 2-thio-substituted penem antibiotics from 2-[4R-(triphenylmethy lthio)-3S-(1S-(dimethyl-t-butylsilyloxy)ethyl)-2-azetidon-1-yl]acetic acid esters....
01/23/1990
4885370Synthetic 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....
12/05/1989
48793911-Phenyl-2(1H,3H)-indolone psychotherapeutic 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...
11/07/1989
4874757Antinflammatory 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...
10/17/1989
4874877Process for optically active 3-(methane-sulfonyloxy)thiolane and analogs
Intermediates and a stepwise process for the conversion of D-methionine or certain of its derivatives to optically active compounds of the formula ##STR1## wherein R is (C1 -C3) alkyl, phenyl or tolyl. The latter compounds are i...
10/17/1989
 
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