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Attorney: Whitaker; Leroy


Number of patents: 218
Last date: October 24, 1989

1            
NumberTitleIssue Date
4876044Thiadiazole compounds and methods of use
Novel thiadiazole compounds are produced having the following general formula: ##STR1## wherein X is S or SO2 R1 is a lower alkyl (cyclic or non-cyclic) radical R2 is hydrogen or a lower acyclic hydrocarbon radical R3...
10/24/1989
4870169Intermediates for beta-lactam antibiotics
1-Benzyl(or substituted benzyl)-3ଲ-[4(S)-aryloxazolidin-2-one-3-yl]-4ଲ-(2-arylvinyl)azet idin-2-ones are provided via cycloaddition of a 4(S)-aryloxazolidin-2-one-3-ylacetyl halide and an imine formed with a benzylamine and a 3-arylacrolei...
09/26/1989
4870185Hapalindoles
New alkaloids called hapalindoles J-Q and T-V, which are antibacterial and antifungal agents, and methods of preparing these alkaloids by culturing the blue-green alga Hapalosiphon fontinalis ATCC 39694, are provided....
09/26/1989
4870021Pure culture of antibiotic A42125-producing strains of Nocardia aerocolonigenes
Antibiotic A42125, which is produced by a new strain of Nocardia aerocolonigenes, NRRL 18049, is a useful inhibitor of Gram-positive and methane-generating microorganisms. A42125 also increases feed utilization efficiency in ruminants. A biologically puri...
09/26/1989
4870109Control of ectoparasites
A series of 1,3-propanediones having a perfluoroalkyl group or a perfluorocycloalkyl group on one carbonyl, and a 3,5-disubstituted phenyl group on the other, are useful when administered to animals for the control of ectoparasites....
09/26/1989
4863923Method of inhibiting superoxide release
A method of inhibiting superoxide release and reducing tissue damage following an inflammatory or ischemic event employing benzothiophenes, benzofurans, and naphthalenes is disclosed....
09/05/1989
4863955Scytophycins
Scytophycins A, B, C, D and E, an aldehyde and alcohol derivative of scytophycin B and the specified alkanoyl and benzoyl esters of scytophycins A, B, C, D and E and the B derivatives (scytophycin compounds) are novel antineoplastic and antifungal agents....
09/05/1989
4855418Process for production of ceophalosporins
Cephalosporin and 1-carba(1-dethia)cephalosporin antibiotics substituted in the 3-position with, inter alia, alkyl, alkenyl and alkynyl, are provided via process comprising conversion of a cephalosporin or 1-carba(1-dethia)-3-cephem substituted in the 3-p...
08/08/1989
4853398Leukotriene antagonists and use thereas
This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes....
08/01/1989
4849453Growth promotion
ଲ-Phenethanolamines are effective in promoting growth and improving feed efficiency and leanness in animals....
07/18/1989
4847092Orally administerable sustained release pharmaceutical formulations
This invention provides orally administerable pharmaceutical formulations having a semi-solid matrix containing a hydrophilic substance capable of creating channels in a hydrophobic carrier matrix thereby providing a sustained rate of release of an active...
07/11/1989
4847261Alkoxy cycloalkanol esters of dihydrolysergic acid having peripheral serotonin antagonists properties
Alkoxycycloalkyl esters of 1-substituted-6-C1-4 straight chain alkyl (or allyl)ergoline-8ଲ-carboxylic acids, useful as 5HT receptor antagonists....
07/11/1989
4845127Phenethanolamines, compositions containing the same and method for effecting weight control
Optically active N-3-(4-substituted phenyl)propyl-ଲ-phenethanolamines are provided as well as pharmaceutical compositions containing such compounds. A method for effecting weight control in obese animals utilizing optically active phenethanolamine i...
07/04/1989
4845110Organic compounds and their pharmaceutical use
There are provided anti-allergic pharmaceutical compounds of formula: ##STR1## in which n is 0, 1 or 2; R1 is a hydrocarbyl group containing 6 to 30 carbon atoms and optionally substituted with an optionally substituted phenyl group; R
07/04/1989
4845229Process for intermediates to 1-carbapenems and 1-carbacephems
A stereoselective process for chiral intermediates to 1-carbapenem and 1-carbacephalosporins is provided comprising the use of an N-acyl-(4R)-substituted-1,3-thiazolidine-2-thione as a chiral auxiliary in boron enolate mediated aldol condensation with a p...
07/04/1989
4845227Aromatase inhibitors from azoles
This invention provides azole derivatives, their pharmaceutical formulations, and their use in methods of inhibiting aromatase and treating or preventing estrogen-dependent diseases in mammals....
07/04/1989
4845224Cycloalkanol esters of dihydrolysergic acid having peripheral serotonin antagonist properties
Cycloalkyl or ketocycloalkyl esters of 1-substituted-6-C1-4 straight chain alkyl (or allyl)-ergoline-8ଲ-carboxylic acids, useful as 5HT receptor antagonists....
07/04/1989
4845200Immunoglobulin conjugates
A conjugate comprising a vinca moiety convalently linked at the 4-position via a group of the formula --OCOXCO-- where X represents a single chemical bond or an optionally substituted C1-10 chain, to an immunoglobulin or an immunoglobulin fragm...
07/04/1989
4845194Glycopeptide recovery process
An improvement in the large-scale recovery of vancomycin-type glycopeptide antibiotics which comprises (1) commingling the fermentation medium in which the antibiotic is produced with a polystyrene divinylbenzene resin such as Dow XFS-43278.00, (2) separa...
07/04/1989
4845128N([(4-trifluoromethylphenyl)amino]carbonyl)benzene sulfonamides
This invention provides the use of certain benzenesulfonamide derivatives in the treatment of susceptible neoplasms in mammals. Also provided are certain novel benzenesulfonamide derivatives and their pharmaceutical formulations....
07/04/1989
4843002Method of selecting recombinant DNA-containing streptomyces
A novel method of selecting Streptomyces recombinant DNA-containing host cells and vectors useful in exemplifying the method are described. The vectors confer apramycin resistance to sensitive Streptomyces host cells and thus provide a convenient method o...
06/27/1989
4841056Substituted hexahydro-4H-indolo[6,5,4-cd]indoles
There are disclosed intermediates to pharmaceutical compounds of the formula ##STR1## in which R1 is an aliphatic or aromatic function, and R2 and R3 are each hydrogen, C1-4 alkyl or a protecting group; and...
06/20/1989
4839341Stabilized insulin formulations
This invention provides an insulin formulation stabilized against aggregation containing a hydroxybenzene and a polyethylene glycol-polypropylene glycol polymer of the formula ##STR1## having an average molecular weight of about 8350 and in which the...
06/13/1989
4835159Ergoline esters useful as serotonin antagonists
The present invention provides novel bicyclic ergoline esters useful as serotonin antagonists....
05/30/1989
4835168Thiadiazole antiviral agents
Compounds of formula (I) ##STR1## wherein R1 is hydrogen, and R2 is cyano or --C(.dbd.S)--NH--R3 ; or R1 and R2 taken together are .dbd.C(NH2)2 or .dbd.C(R5)(NHR
05/30/1989
4835181Anticonvulsant agents using cyano dimethylphenyl benzamides
This invention provides certain 4-substituted benzamide derivatives, their pharmaceutical formulations, and their use as anticonvulsant agents....
05/30/1989
4835254Process for reducing methionine sulfoxide residues in peptides or proteins
This application discloses a process for reducing methionine sulfoxide residues in peptides and proteins to methionine residues. The process comprises subjecting said peptide or protein to a substantially anhydrous trifluoroacetic acid reaction medium con...
05/30/1989
48311457-phenylsulfonyloxymethylene-6-oxo-perhydroquinolines
This invention provides a process for preparing trans 2-aminopyrimido[4,5-g]quinolines employing novel intermediates....
05/16/1989
4830967Process for producing antibiotic A80438
A new strain of Streptomyces pactum, NRRL 15970, and an improved fermentation process for producing the polyether antibiotic A80438 using this microorganism are provided....
05/16/1989
4826993Substituted diazolidinones
4-Substituted 1-(optionally substituted)diazolidinones are intermediates to 7-substituted bicyclic pyrazolidinone antimicrobials....
05/02/1989
48269866-Oxo-trans-octa- and decahydroquinolines
7- or 8-Substituted, partially hydrogenated pyrazolo[3,4-g]quinoline, thiazolo[4,5-g]quinoline, oxazolo[4,5-g]quinoline, and pyrrolo[3,4-g]quinoline derivatives, and 8- or 9-substituted, partially hydrogenated pyrido[2,3-g]quinazoline derivatives are D-2 ...
05/02/1989
4826841Alkanoyl anilides as pesticides
The present invention is in alkanoyl anilides exhibiting insecticidal and arachnicidal activity, wherein the alkanoyl is both branched and substantially or totally fluorinated....
05/02/1989
48269922,3-(Dihydro) bicyclic pyrazolidinones
2,3-(Dihydro) bicyclic pyrazolidinones are intermediates for bicyclic pyrazolidinone antimicrobials....
05/02/1989
4824863Antibiotic A80438
New polyether antibiotic A80438, its acyl and alkyl ester, alkyl ether and urethane derivatives, and salts thereof, are useful antibacterial and anticoccidial agents and increase feed-utilization efficiency in animals. Method of making A80438 by culture o...
04/25/1989
4822618Capsules
A gelatin capsule cap has an annular groove in the region of its open end to reduce ovality....
04/18/1989
4820694Modifications of 3-O-demethylmycinose in macrocin and lactenocin
New 3'" and/or 4'"-modified macrocin and 3" and/or 4"-modified-lactenocin derivatives of formula 1 have significant antibacterial activity. Compositions positions containing and methods of using these derivatives are also provided....
04/11/1989
4820832Process for preparing 3-unsubstituted cephalosporins and 1-carba(dethia)cephalosporins
A process for preparing 7ଲ-acylamino (or 7ଲ-protected amino)-3-H-1-carba(1-dethia)-3-cephem-4-carboxylic acid esters and the corresponding cephalosporins is provided. 7ଲ-Acylamino (or 7ଲ-protected amino)-3-halo (or 3-sulfonyl ...
04/11/1989
4820845Alkylation of 3(5)-cyano-1H-pyrazole-4-carboxylic acid esters
The present invention provides a process for selectively alkylating pyrazoles comprising reacting a 3(5)-cyano-1H-pyrazole-4-carboxylic acid ester with a C4 -C8 alkene, or a C5 -C6 cycloalkene substituted at the...
04/11/1989
48208163-trifuoromethylsulfonyloxy-substituted 1-carbacephalosporins as intermediates for antibiotics
7ଲ-Acylamino-3-trifluoromethylsulfonyloxy-1-carba-3-cephem-4-carboxyli c acid antibiotic compounds, esters and salts thereof, and the corresponding 7-amino and protected 7-amino 1-carbacephalosporins are provided. The 3-trifluoromethylsulfonyloxy-sub...
04/11/1989
4820815Azetidinone N-phosphonomethyl esters
The invention provides azetidinones of the formula ##STR1## where R4 is hydrogen, amino or protected amino; R0 is H when R4 is amino or protected amino, or C1 -C4 alkyl when R4 is H; R...
04/11/1989
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