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SmithKline Corporation Patents
Assignee:
SmithKline Corporation
Address:
Philadelphia, PA
No. of patents:
342
Patents:


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Patent Number Title Of Patent Date Issued
RE28939 3-Aminoindazole derivatives August 24, 1976
.Iadd.Pharmaceutical compositions having muscle relaxant and analgesic activity containing 3-aminoindazoles..Iaddend.
RE28691 Methods and compositions for increasing feed intake of animals using tertiary alcohols January 20, 1976
New methods and compositions for inducing polyphagia in growing or fattening meat producing animals such as sheep or cattle are described using as active ingredients tertiary alcohols or the corresponding carbamates, ureas, oxyureas or ureides. The active ingredients are used most us
7247748 Amide compounds and methods of using the same July 24, 2007
Disclosed is a compound having the formula (I) pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein. The compounds, salts and solvates of this invention are useful as LXR agon
4353902 Livestock feed and method for improving food utilization October 12, 1982
Supplemented livestock feedstuffs and methods of feeding using as active ingredient a chemical compound having histamine H.sub.2 antagonist activity improve the utilization of food by meat producing animals. A specific compound of use as the active ingredient is metiamide.
4352809 Method of producing alpha.sub.2 antagonism October 5, 1982
Method of producing alpha.sub.2 antagonism by administering thiadiazolo- and oxadiazolotetrahydroisoquinoline compounds.
4352754 3-Thienylmethyl-6-halo-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1 H-3-benzazepines October 5, 1982
3-Furylmethyl- and thienylmethyl-6-halo-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzaz epines have potent dopaminergic activity. As such they have utility an antihypertensive and anti-Parkinsonism agents.
4350698 Antiallergic imidosulfamides September 21, 1982
Imidosulfamide derivatives useful in the treatment of allergic conditions are prepared by reaction of an appropriately substituted tetrahydroisoquinoline and chlorosulfonylisocyanate in the presence of a non-nucleophilic organic base. Pharmaceutical compositions and methods of inhibi
4350685 Antiallergic imidodisulfamides September 21, 1982
Imidodisulfamide derivatives useful in the treatment of allergic conditions are prepared by reaction of an appropriately substituted phenylcycloalkylamine and bis(chlorosulfonyl)imide in the presence of a non-nucleophilic organic base. Pharmaceutical compositions and methods of inhib
4342686 Intermediates for preparing 6-lower alkyl-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzaze August 3, 1982
The preparation and use as intermediates is described for 7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines whose structures are characterized by having either an aralkyl or lower alkanoyl group at position 2 or an .alpha.-hydroxyalkyl or .alpha.-chloroalkyl group at positi
4341786 Pharmaceutical compositions and method of producing central alpha.sub.1 agonist activity utilizi July 27, 1982
Octahydrobenzo[f]quinoline compounds having 7- and 10-substituents are centrally acting alpha.sub.1 agonists.
4340733 Process for preparing 3-chloro-6-(2-hydroxyphenyl)-pyridazines July 20, 1982
A process for preparing 3-chloro-6-(2-hydroxyphenyl)pyridazines by the reaction of 6-(2-hydroxyphenyl)-3(2H)-pyridazinones with phosphorus oxychloride and a disubstituted formamide. The chloropyridazine compounds are useful intermediates for preparing compounds which have .beta.-adre
4340601 Dopaminergic isoquinolines July 20, 1982
A new series of compounds having renal vasodilating activity described. The compounds are 2-allyl-8-halo-4-(p-hydroxyphenyl)-1,2,3,4-tetrahydroisoquinolines.
4340600 Renal dilating methods and compositions using 4-(3,4-dihydroxyphenyl)-1,2,3,4-tetrahydroisoquino July 20, 1982
4-Phenyl-1,2,3,4-tetrahydroisoquinolines whose structures have two hydroxy groups substituted at the 3,4-position on the 4-phenyl ring have been found to have renal vasodilating activity upon internal administration. The active ingredients are prepared by cyclizing N-(2-substituted b
4336255 Pharmaceutical compositions containing guanidinopyrimidines June 22, 1982
Pharmaceutical compositions having as active diuretic ingredients certain 4-guanidinopyridines are described. Representative diuretic compounds are 5-amino-6-chloro-4-guanidinopyrimidine and 6-amino-5-nitro-4-guanidinopyrimidine.
4336254 Guanidinopyrimidine compounds, compositions and method of using as a diuretic June 22, 1982
2,4-Amino, guanidinopyrimidines have diuretic activity. A representative species of these compounds is 2-guanidino-4-amino-6-chloroguanidine which is prepared by the stepwise replacement of first the 2-halo of a 2,4,6-trihalopyrimidine by guanidino and then the 4-halo by ammonia.
4328153 Dopaminergic benzazepines May 4, 1982
A new series of compounds having renal vasodilating activity is described. The compounds are 3-cycloalkylmethyl-7,8-dihydroxy-6-halo-1-(p-hydroxyphenyl)-2,3,4,5-tetrah ydro-1H-3-benzazepines.
4327023 Intermediates for preparing 7,8-amino, hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines April 27, 1982
A group of new chemical compounds are described which are intermediates for preparing 7,8-amino, hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines. The intermediates are distinguished in structure by a benzyloxy substituent at either the 7 or 8-position.
4321399 Preparation of 2-thiophenecarbonyl chloride March 23, 1982
Thiophenecarbonyl chloride is produced in good yields by the direct acylation of thiophene in the presence of aluminum chloride with control of temperature and concentration.
4321393 Method for preparing 2-cyanamidobenzimidazoles or 2-cyanamidobenzoxazoles March 23, 1982
A method of preparing 2-cyanamidobenzimidazoles or 2-cyanamidobenzoxazoles comprising reacting N-cyanodiphenoxyiminocarbonate with an o-amino or o-hydroxy aniline.
4321254 Antiallergic imidodisulfamides March 23, 1982
Imidodisulfamide derivatives useful in the treatment of allergic conditions are prepared by reaction of an appropriately substituted tetrahydroisoquinoline and bis(chlorosulfonyl)imide in the presence of a tertiary amine. Pharmaceutical compositions and methods of inhibiting the symp
4321195 6 -Halo-7,8-dimethoxy-1-(methoxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine s March 23, 1982
Certain 6-halo-7,8-dimethoxy-1-(methoxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine s and N-[2-(2-halo-3,4-dimethoxyphenyl)ethyl]-2-hydroxy-2-(methoxyphenyl)ethylam ines are intermediates for preparing 6-halo-7,8-dihydroxy-1-(hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine s w
4320148 2-Aminotetralin compounds, pharmaceutical compositions and method of producing central alpha.sub March 16, 1982
2-Aminotetralin compounds having 5- and 8- substituents are centrally acting alpha.sub.1 agonists.
4317826 N,N'-Bis[substituted-1,2,3,4 tetrahydroisoquinolyl]disulfonylimides and antiallergic composition March 2, 1982
Imidodisulfamide derivatives useful in the treatment of allergic conditions are prepared by reaction of an appropriately substituted tetrahydroisoquinoline and bis (chlorosulfonyl)imide in the presence of a tertiary amine. Pharmaceutical compositions and methods of inhibiting the sym
4317812 Polynitroxin antibiotics produced by Nocardiopsis mutabilis Shearer sp. nov. ATCC 31520 March 2, 1982
A novel antibiotic, polynitroxin, is produced by the cultivation of a fermentation broth containing Nocardiopsis mutabilis Shearer sp. nov. ATCC 31520 in an aqueous nutrient medium under submerged aerobic conditions.
4315935 N,N'-Bis[substituted-1,2,3,4-tetrahydroisoquinolinolyl]disulfonylimides and antiallergic composi February 16, 1982
Imidodisulfamide derivatives useful in the treatment of allergic conditions are prepared by reaction of an appropriately substituted tetrahydroisoquinoline and bis(chlorosulfonyl)imide in the presence of a tertiary amine.
4314944 4-Aminoalkyl-7-hydroxy-2(3H)-indolones February 9, 1982
A new group of 2(3H)-indolones whose structures are characterized by having an aminoalkyl substituent at position 4 and a hydroxy group at position 7 of the indolone nucleus have beneficial activity on the cardiovascular system. A typical species of the group is 4-di-n-propylaminoeth
4308267 7-[2-Alkoxyimino-2-(amino-thiazole)acetami do]-3-[1-(sulfaminoalkly)tetrazolthiomethyl]cephalospo December 29, 1981
Novel cephalosporins with improved antibacterial and pharmacokinetic properties are disclosed. These compounds have a 2-alkoxyimino-2-(2-amino-4-thiazolyl)-acetamido group at position 7 and a sulfaminoalkyltetrazolythio group at position 3.
4299969 Method for preparing lower alkyl .beta.-(S-benzylmercapto)-.beta.,.beta.-pentamethylenepropionat November 10, 1981
Lower alkyl .beta.-(S-benzylmercapto)-.beta.,.beta.-pentamethylenepropionates are prepared in improved yields by reacting lower alkyl cyclohexylideneacetates with benzylmercaptan in the presence of an alkali metal mercaptide.
4293546 Anthracycline antibiotics produced by Streptosporangium fragilis Shearer sp. nov. ATCC 31519 October 6, 1981
A novel anthracycline antibiotic complex, fragilomycin complex, is produced by the cultivation of a fermentation broth containing Streptosporangium fragilis Shearer sp. nov. ATCC 31519 microorganisms in an aqueous nutrient medium under submerged aerobic conditions. The fragilomycin compl
4292305 Antiallergic imidodisulfamides September 29, 1981
Imidodisulfamide derivatives useful in the treatment of allergic conditions are prepared by reaction of an appropriately substituted primary amine and bis(chlorosulfonyl) imide in the presence of a tertiary amine.
4286089 7-Acyl-3-(substituted tetrazolyl thiomethyl)cephalosporins August 25, 1981
The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a substituted tetrazolyl thiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated compounds have antibacterial activity.
4285938 7,8-Dihydroxy-1-(sulfamylphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine derivatives August 25, 1981
New 7,8-dihydroxy-1-(sulfamylphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepines having pharmaceutical activity together with new intermediates and methods of synthesis for preparing them. The lead compound is 6-chloro-7,8-dihydroxy-1-(p-sulfamylphenyl)-2,3,4,5-tetrahydro-1H-3-benzaz epine w
4285878 N-Phenyl-N'-cyano-O-phenylisoureas August 25, 1981
N-Phenyl-N'-cyano-O-phenylisoureas are prepared from N-cyanodiphenoxyimidocarbonate and an optionally substituted o-phenylenediamine or o-aminophenol. The isoureas are new chemical intermediates especially useful for preparing 2-cyanamido and 2-carbomethoxyaminobenzimidazole and benz
4284556 7,8-Amino, hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines August 18, 1981
A group of 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines whose structures have amino, hydroxy substituents at the 7,8-positions of the benzazepine nucleus is disclosed. Novel intermediates and routes of synthesis used for preparing them are also described. The end products have pharmacod
4282227 Renal vasodilating 3,4-dihydroxyphenyltetrahydrothienopyridines August 4, 1981
3,4-Dihydroxyphenyltetrahydrothieno[2,3-c] or [3,2-c] pyridines are prepared by cyclization of a N-thienylmethyl-2-(3',4'-dimethoxyphenyl)-ethanolamine. These compounds have renal vasodilating activity. A species is 4-(3,4-dihydroxyphenyl)-1,2,3,4-tetrahydrothieno[2,3-c]pyridine and
4278670 7-Alpha-oxyiminoacylcephalosporins July 14, 1981
New semisynthetic cephalosporins having antibacterial activity are described. The structures of the new compounds are characterized by having an .alpha.-oxyimino group in the 7-acetamidomoiety plus a carboxyalkyltetrazolylthiomethyl group at position 3.
4272531 3,3'-Bis-methylene-1,3-benzo-thiazine compounds June 9, 1981
3,3'-Bis-Methylene-1,3-benzothiazine compounds are inhibitors of phenylethanolamine N-methyl-transferase.
4272440 Intermediates for preparing hydroxyphenylpyridazinones June 9, 1981
5-(5'-Halo-2'-methoxyphenyl)-3,4-dihalo-2(5H)-furanones are prepared by a Friedel-Crafts reaction using a p-haloanisole and a mucohalic acid in the presence of aluminum chloride. They are used as chemical intermediates for preparing hydroxyphenylpyridazinones.
4265890 6-Phenyl thio- and 6-cyclohexyl thio-2,3,4,5-tetrahydro-1H-3-benzazepines May 5, 1981
Mercapto substituted-2,3,4,5-tetrahydro-1H-3-benzazepines having dopamine receptor blocking activity are prepared from o-quinones or via standard preparative procedures.
4265889 6-Lower alkyl-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines May 5, 1981
A series of 6-lower alkyl-7,8-dihydroxyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines having dopaminergic activity together with intermediates and processes for their preparation are disclosed.
4263311 5,6-Phenyl-2,3-dihydroimidazo [2,1-b] thiazoles April 21, 1981
The compounds are 5,6-phenyl-2,3-dihydroimidazo[2,1-b]thiazoles which have antiarthritic activity. A preferred compound is 5,6-bis(p-anisyl)-2,3-dihydroimidazo[2,1-b]thiazole.
4258198 5-Cycloalkyl thio- and oxy-2-carbalkoxyaminobenzimidazoles March 24, 1981
New anthelmintic compounds, compositions and methods of use are described utilizing 5-cycloalkylthio and oxy-2-carbalkoxyaminobenzimidazole. Methods of preparation involve the reaction of 4-cycloalkylthio- or oxy-o-phenylenediamine with methyl cyanocarbamate in aqueous miscible organ
4258049 Inhibiting phenylethanolamine N-methyltransferase with thiadiazolo and oxadiazolotetrahydroisoqu March 24, 1981
Thiadiazolo- and oxadiazolotetrahydroisoquinoline compounds are inhibitors of phenylethanolamine N-methyltransferase.
4257947 3-Amino-2-hydroxy, halo or mercaptomethyl-4-oxoazetidines March 24, 1981
The stereospecific cycloaddition of nitrogen containing acetic acid halides or anhydrides with Schiff bases having a carbalkoxy group substituted on the methine carbon atom offers new intermediates and methods for preparing synthetic cephalosporin congeners having antibacterial activity.
4255445 8-Hydro xy-6,7-(2-methyl-2,3-dihydrofuro)-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzaz epines March 10, 1981
8-Hydroxy-6,7-(2,3-dihydrofuro)-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepin es are prepared by a reaction sequence whose key is a dual cyclization forming the 3-benzazepine ring and fused thereto a dihydrofuran.
4255422 6-Halo-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines March 10, 1981
7,8-Dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines having a halo substituent at the 6-position have potent dopaminergic activity. The 6-chloro congeners are most active.
4255413 Gelatin capsule dosage unit containing triamterene March 10, 1981
A gelatin capsule unit dosage form containing triamterene, 2,4,7-triamino-6-phenylpteridine, which results in rapid dissolution of the active ingredient. The dosage form comprises the addition of a combination of a surfactant and a carbonate or bicarbonate salt as diluents.
4254140 4-(2-Aminoethyl)-7-hydroxy-2-methyl-2,3-dihydrobenzofurans March 3, 1981
4-(2-Aminoethyl)-7-hydroxy-2-methyl-2,3-dihydrobenzofuran derivatives having dopaminergic activity are prepared by cyclizing a 2-allyl-3,4-dimethoxyphenethylamine such as by reacting the phenethylamine with hydrogen bromide.
4251660 Method for preparing tetrahydroisoquinolines February 17, 1981
A method for preparing 1,2,3,4-tetrahydroisoquinolines comprising heating N-halo or hydroxyethyl-N-benzylamines in an aluminum chloride melt at 160.degree.-210.degree..
4251525 3-Allyl-7,8-dihydroxy-6-halo-1-(4-hydr oxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine derivatives February 17, 1981
3-Allyl-7,8-dihydroxy-6-halo-1-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-be nzazepine derivatives are prepared by N-allylation of 7,8-dimethoxy-6-halo-1-(4-methoxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepi ne using an allyl halide in acetonitrile in the presence of base followed by O-de
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