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E. R. Squibb & Sons, Inc. Patents
Assignee:
E. R. Squibb & Sons, Inc.
Address:
Princeton, NJ
No. of patents:
1537
Patents:


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Patent Number Title Of Patent Date Issued
4311840 2,3,6,7-Tetrahydro-2-thioxo-4H-oxazolo[3,2-a]-1,3,5 triazin-4-ones January 19, 1982
A compound of the formula ##STR1## wherein R.sub.1 is phenyl or substituted phenyl when R.sub.2 is hydrogen or lower alkyl; andR.sub.2 is phenyl or substituted phenyl when R.sub.1 is hydrogen or lower alkyl.These compounds are useful as anti-inflammatory agents.
4311705 Carboxyalkanoyl and hydroxycarbamoylalkanoyl derivatives of substituted prolines January 19, 1982
Compounds, compositions and method of alleviating hypertension using a compound of the formula ##STR1## wherein R is hydrogen or lower alkyl;R.sub.1 is hydrogen, lower alkyl or phenyl-lower alkyl;R.sub.2 is hydrogen, lower alkyl or phenyl lower alkyl or halo substituted lower alkyl;R
4311697 Derivatives of mercaptoacyl prolines and pipecolic acids January 19, 1982
This invention is directed to compounds of the formula ##STR1## and various intermediates therefore. The final products possess useful hypotensive activity.
4311644 Method for preparing 10,10-difluoro prostacyclin intermediates and new compounds produced thereb January 19, 1982
A method is provided for preparing intermediates for use in 10,10-difluoro prostacyclin syntheses which method includes the steps of aceylating ketopinic acid or its acid halide to form the corresponding ketopinoyl diene ester intermediate, subjecting the diene ester to a Diels-Alder
4310461 Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids January 12, 1982
Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids are useful for the treatment of hypertension.
4308392 Hydroxamic acid derivatives of mercaptoacyl amino acids December 29, 1981
Hydroxamic acid derivatives of certain mercaptoacyl amino acids inhibit the conversion of angiotensin I to angiotensin II in mammals and are useful for the treatment of hypertension.
4308388 4-Azido-1-mercaptoacyl pipecolic acid December 29, 1981
1-Mercaptoacyl proline or pipecolic acid having an azido group in the 4-position inhibits the conversion of angiotensin I to angiotensin II in mammals and is useful for the treatment of hypertension.
4308375 Method for purifying water-insoluble polyene antibiotics December 29, 1981
A method for purifying water-insoluble polyene antibiotics, such as amphotericin and nystatin, is provided which method includes the step of passing a mixture of the polyene antibiotic dispersed in methanol through an ion exchange column whereby gram positive and gram negative bacteria
4307110 Mercaptoacyl derivatives of 3-substituted proline derivatives December 22, 1981
New mercaptoacyl derivatives of 3-substituted proline derivatives are provided which have the general formula ##STR1## and are useful as hypotensive agents.
4307105 Imidazolylethoxymethyl derivatives of thiazole December 22, 1981
New imidazolylethoxymethyl derivatives of thiazole are provided having the general formula ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenoxy-lower alkyl, phenyl-lower alkyl or substituted or unsubstituted phenyl;R.sup.2 is hydrogen or halogen;R.
4307099 Reaction products of pyrazolo[1,5-c]quinazoline derivatives and proline derivatives and methods December 22, 1981
Compounds of the following structure are provided ##STR1## wherein R.sup.1 is hydrogen or lower alkanoyl, R.sup.2 is hydrogen or lower alkyl, and R.sup.3 is hydrogen, lower alkyl or trifluoromethyl. The above compounds have useful hypotensive activity and anti-allergy activity.
4304773 Novel bendroflumethiazide formulations and method December 8, 1981
New bendroflumethiazide formulations in solid form are provided which are characterized by excellent disintegration and dissolution capabilities even after long periods of storage. The new bendroflumethiazide formulations, for example, in the form of tablets, contain in addition to b
4303795 Substituted .beta.-anilino-.gamma.-methoxy-crotonates December 1, 1981
A process is provided for preparing pyrazolo-[1,5-c]quinazoline derivatives of the structure ##STR1## wherein X is O or S; R.sup.1 is hydrogen, lower alkyl, hydroxymethyl, phenyl-lower alkyl, phenyl or phenyl substituted with halogen, lower alkyl, lower alkoxy, or trifluoromethyl
4303662 Carboxyacyl, mercapto and acylmercapto derivatives of heterobicyclo compounds December 1, 1981
A compound of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, phenyl lower alkyl or halo substituted lower alkyl;R.sub.2 is hydrogen, lower alkyl, phenyl lower alkyl or halo substituted lower alkyl;n is 0, 1 or 2;X is--(CH.sub.2).sub.m Z--;Z is oxygen, sulfur or imino;
4302453 Antiarrhythmic tetrahydronaphthalene derivatives November 24, 1981
Compounds are provided having the structure ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and are hydrogen, lower alkyl, lower alkenyl, or hydroxy-lower alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached also form a hetero
4299828 Corticosteroid stick formulations November 10, 1981
Corticosteroid formulations in the form of a lipophilic stick are provided which are used as anti-inflammatory agents; the lipophilic stick includes the corticosteroid, such as halcinonide or triamcinolone acetonide, dissolved in an oleaginous solvent which is miscible with the other sti
4297275 Inhibitors of mammalian collagenase October 27, 1981
Mammalian collagenase is inhibited by compounds having the formula ##STR1## and salts thereof, wherein R.sub.1 is hydrogen or alkanoyl of 2 to 10 carbon atoms;R.sub.2 is hydroxy, amino, or ##STR2## R.sub.3 is hydrogen, alkyl of 1 to 4 carbon atoms, ##STR3## R.sub.4 is hyd
4296113 Mercaptoacyl derivatives of keto substituted proline and pipecolic acid October 20, 1981
This invention is directed to compounds of the formula ##STR1## which are useful in the treatment of hypertension.
4296101 Antibiotic kristenin October 20, 1981
A new antibiotic, designated kristenin, is produced by the microorganism Bacillus subtilis. The antibiotic possesses activity against gram positive bacteria.
4296033 4-Azido-1-mercaptoacyl proline October 20, 1981
1-Mercaptoacyl proline having an azido group in the 4-position inhibits the conversion of angiotensin I to angiotensin II in mammals and is useful for the treatment of hypertension.
4294894 Transparent toothpaste having a medicinal action and process for its production October 13, 1981
A transparent medicated toothpaste is provided which contains amorphous silica gel in finely divided form as a polishing cleaning component combined with a saline electrolyte having a decongestive-antiedematous action. A process for preparing such toothpaste is also provided.
4293569 Substituted phenylguanindines and method October 6, 1981
Phenylguanidine derivatives are provided having the structure ##STR1## wherein R is hydrogen, lower alkyl, cycloalkyl, lower alkoxy, phenyl, phenylalkyl, phenoxy, phenylalkoxy, lower alkoxyalkyl, phenoxyalkyl, alkylamino, dialkylaminoalkyl, alkylthio, phenylthio, phenylthioalkyl, and
4293481 Tripeptide inhibitors of angiotensin-converting enzyme October 6, 1981
Peptides having the formula ##STR1## wherein R.sub.1 is hydrogen and R.sub.2 is hydroxyl, alkyl, aryl, arylalkyl, alkoxy, alkylthio, aryloxy, arylthio, halogen or azido, or R.sub.1 and R.sub.2 are the same and each is hydrogen, halogen, alkoxy or alkylthio, or R.sub.1 and R.sub.2
4292972 Lyophilized hydrocolloio foam October 6, 1981
A lyophilized foam sponge product having medically useful hemostatic and adhesive properties formed from the hydrocolloids, gelatin, pectin, and sodium carboxymethylcellulose and having a density of from about 0.01 to about 0.10 grams/cc. The gelatin is present at from about 20% to about
4291040 Mercaptoacyl derivatives of 4-disubstituted prolines and 4-substituted dehydroprolines September 22, 1981
This invention is directed to compounds of the formulas ##STR1## and various intermediates therefore. The final products possess useful hypotensive activity.
4288456 Compositions containing 1-aryl-5-(2-propenylamino)-1-penten-3-ones and method for treating infla September 8, 1981
Pharmaceutical compositions containing 1-aryl-5-(2-propenylamino)-1-penten-3-ones and salts thereof having the structure ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy, halogen, hydroxy, lower alkanoyloxy, nitro, cyano, amino, carboxy or lower alkoxycarbonyl,
4288368 Dithioacylproline derivatives September 8, 1981
Compounds having the formula ##STR1## wherein: R.sub.1 is hydrogen, alkyl, aryl or arylalkyl;R.sub.2 is hydrogen and R.sub.3 is hydrogen, hydroxy, alkoxy or halogen, or together R.sub.2 and R.sub.3 can be .dbd.O or --X--(CH.sub.2).sub.t --X-- wherein X is oxygen or sulfur and t is 2
4284780 Amino acid derivatives August 18, 1981
New substituted acyl derivatives of amino acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.
4284779 Amino acid derivatives August 18, 1981
New substituted acyl derivatives of amino acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.
4284624 Mixed disulfides August 18, 1981
This invention is directed to compounds of the formula ##STR1## wherein A and A.sub.1 are amino acid residues, X is and .alpha.-imino acid residue, and R.sub.1 is hydrogen, lower alkyl, or halo substituted lower alkyl. These compounds are useful as hypotensive agents.
4284561 Hydroxamic acid derivatives of mercaptoacyl amino acids August 18, 1981
Hydroxamic acid derivatives of certain mercaptoacyl amino acids inhibit the conversion of angiotensin I to angiotensin II in mammals and are useful for the treatment of hypertension.
4282235 Derivatives of thiazolidinecarboxylic acids and related acids August 4, 1981
New substituted derivatives of thiazolidine-, thiazane and related carboxylic acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.
4282230 Imidazolylethoxy derivatives of quinoline-2- or 4-methanols, antimicrobial compositions containi August 4, 1981
Imidazolylethoxy derivatives of quinoline-2- or 4-methanols having the general formula ##STR1## and their acid addition salts are useful as antifungal and antibacterial agents.
4282226 Thioxopyrazolo[1,5-c]quinazoline derivatives, anti-allergic compositions and methods for treatin August 4, 1981
Compounds are provided having the structure ##STR1## wherein R.sup.1 is hydrogen or lower alkyl of 1-3 carbons, R.sup.2 is carboxyl, hydroxymethyl, lower alkanoyloxymethyl, or lower alkoxycarbonyl, R.sup.3 is hydrogen, lower alkyl or benzyl, and R.sup.4 and R.sup.5 are the same o
4279902 Anti-arrhythmia agents July 21, 1981
Acetamide derivatives are provided having the structure ##STR1## wherein X is a single bond, --CH.sub.2 -- or --O--, R.sup.1 and R.sup.2 may be the same or different and are lower alkyl, phenyl-lower alkoxy-lower alkyl, lower alkenyl, phenyl-lower alkyl or lower alkoxy, or ##STR2
4275062 Aminothiazolyl ureido sulfoxide cephalosporins June 23, 1981
Cephalosporins of the formula ##STR1## R represents hydrogen, sodium, potassium, or certain ester groups, R.sub.1 is in the .alpha.-configuration and is hydrogen or methoxy, X represents hydrogen ##STR2## R.sub.3 represents hydrogen or lower alkyl, R.sub.4 is hydrogen, lower
4273776 Antibacterial and antifungal derivatives of 3-(1H-imidazol-1-yl)-2-propen-1-ones June 16, 1981
Compounds are provided having the structure ##STR1## wherein R.sup.1 is lower alkyl; phenyl-lower alkyl; phenyl; substituted phenyl wherein the phenyl group bears one or two halogen, hydroxy, lower alkyl, lower alkoxy, lower alkylothio, cyano or nitro groups; 5- or 6-membered mon
4271157 Imidazole derivatives of 7-[(2-amino-4-thiazolyl)-oximino] cephalosporins June 2, 1981
A compound of the formula ##STR1## wherein R is hydrogen, alkali metal, ##STR2## R.sub.1 is hydrogen or methyl; R.sub.2 is hydrogen or methyl;R.sub.3 is hydrogen or methyl;R.sub.4 is hydrogen, --OCONH.sub.2, ##STR3## R.sub.5 is hydrogen or methyl;R.sub.6 is hydrogen, methyl,
4269836 4H-Pyrazolo[4',3':5,6]pyri do[4,3-d][1,2,4]triazolo[3,2-b]-pyrimidin-5(8H)one and derivatives May 26, 1981
New 4H-pyrazolo[4',3':5,6]pyrido[3,4-e][1,2,4]triazolo[1,5-a]pyrimidin-5(8H)on e and new derivatives thereof have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
4267373 5,6,7,8-Tetrahydronaphthalene hypotensive agents May 12, 1981
5,6,7,8-Tetrahydronaphthalenes having the structure ##STR1## and the pharmaceutically acceptable salts thereof, are useful as blood pressure lowering agents. In the above formula R.sub.1 can be hydrogen or alkyl; R.sub.2 is alkyl; R.sub.3 and R.sub.4 can each be hydrogen, hydroxy
4267354 Substituted amides having antiinflammatory activity and intermediates May 12, 1981
Compounds having the formula ##STR1## wherein R.sub.1 is alkoxycarbonyl, amido, alkylamido, or dialkylamido; R'.sub.3 is alkylbenzylamino, dialkylamino, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, or 4-alkyl-1-piperazinyl; A.sub.1 is an alkylene group having 2 to 5 carbon atoms
4266065 Mercaptoacyldihydropyrazole carboxylic acid derivatives May 5, 1981
Compounds having the formula ##STR1## and basic salts thereof, wherein R.sub.1 is hydrogen, alkyl, aryl, arylalkyl or ##STR2## wherein R.sub.6 is alkyl or aryl; R.sub.2 is hydrogen, alkyl, trifluoromethyl or pentafluoroethyl;R.sub.3 is hydrogen or alkyl;R.sub.4 is hydrogen,
4265815 17-(Substituted thio)androst-4-ene[16,17,-b]-[1,4]benzodioxin-3-ones May 5, 1981
Steroids having the formula ##STR1## are useful intermediates for the preparation of novel antiinflammatory agents having the formula ##STR2## In the above formulas, X is S, ##STR3## R.sub.1 is alkyl, aryl, arylalkyl or acyloxyalkyl; R.sub.2 is fluoro, chloro, bromo o
4263293 Heterocyclic containing amides as inhibitors of mammalian collagenase April 21, 1981
Mammalian collagenase is inhibited by compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, alkanoyl of 2 to 10 carbon atoms or arylcarbonyl;R.sub.2 is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 1-piperazinyl, or 4-alkyl-1-piperazinyl;R.sub.3 is alkyl of 3 to 8 carbon
4260751 Pyrazolo [1,2-a][1,2,4] benzotriazines April 7, 1981
Pyrazolo[1,2-a][1,2,4] benzotriazines having the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, nitro, amino, lower alkylamino, di(lower alkyl)amino, --SR.sub.4, --OR.sub.4 or halogen;R.sub.2 is hydrogen, lower alkyl or aralkyl;R.sub.3 is hydrogen, lower alkyl or a salt formi
4260616 Antimicrobial imidazolylethoxymethyl derivatives of 1,3-dioxolo quinolines April 7, 1981
Imidazolylethoxymethyl derivatives of dioxoloquinolines having the general formula ##STR1## and their acid addition salts are useful as antifungal and antibacterial agents.
4260614 4-(2-(1H-Imidazol-1-ylmethyl)-1,3-dioxol an-4-yl)methoxypyrazolo(3,4-b)pyridines April 7, 1981
Compounds are provided having the formula ##STR1## wherein R.sup.1 is hydrogen, lower alkyl; substituted or unsubstituted phenyl-lower alkyl; substituted or unsubstituted phenyl; substituted or unsubstituted 5- or 6-membered monocyclic aromatic heterocyclic containing one O, S or
4257969 16,17-Dihydroxypregnene-21-carboxylic acids and derivatives March 24, 1981
Topical antiinflammatory activity is exhibited by 16,17-dihydroxypregnene-21-carboxylic acids and esterified derivatives thereof.
4254267 Mercaptoacyldihydropyrazole carboxylic acid derivatives March 3, 1981
Hypotensive activity is exhibited by compounds having the formula ##STR1## wherein: R.sub.1 is hydrogen, alkyl, aryl, arylalkyl or ##STR2## wherein R.sub.5 is alkyl or aryl; R.sub.2 is hydrogen, alkyl, or haloalkyl;R.sub.3 is furanyl, thienyl or pyridyl;R.sub.4 is hydrogen, alk
4254044 7-Oxabicycloheptane- and 7-oxabicycloheptene compounds March 3, 1981
New compounds having the general formula ##STR1## are useful as cardiovascular agents, and as intermediates for the preparation of compounds having the general formula ##STR2## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2 is --CHO--, CH.sub.2 OH or --CH.dbd.CH--R.sup.3
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