Abstract: 2-(5H-Dibenzo[a,d]cyclohepten-5-on-2-yl)acetic, propionic and butyric acids, are prepared from glycidonitrile intermediates. The acid products exhibit anti-inflamatory, analgesic and anti-pyretic activity.
Abstract: 7(8)-substituted triazinobenzimidazoles represented by the formula: ##STR1## where R is a lower alkyl group having 1 to 4 carbon atoms; R' is diloweralkylaminoalkyl (C.sub.2-6) or alkyl having 1 to 18 carbon atoms; R.sup.2 is phenylsulfinyl, phenoxyethoxy, benzyloxyethoxy, methoxyethylsulfinyl, or 3-chloroprop-1-ylsulfinyl; the R.sup.2 -substitution being at the 7(8)-position; or a pharmaceutically acceptable salt thereof.The compounds are useful as pesticides, particularly as antifungal and anthelmintic agents.
Type:
Grant
Filed:
March 8, 1976
Date of Patent:
March 8, 1977
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Colin C. Beard, John A. Edwards, John H. Fried
Abstract: A pharmaceutical preparation having a minor amount of a tetracycline medicament, and a major amount of a dialkylated mono- or poly-alkylene glycol vehicle therefor, and, optionally, a minor amount of one or more antioxidants for the dialkylated glycol vehicle. The preparations are stable topical tetracycline formulations having good release and skin penetration characteristics.
Abstract: 2-(5H-Dibenzo[a,d]cyclohepten-5-on-2-yl)acetic, propionic and butyric acids are prepared by oxidation of the corresponding 5-oxo- or ketal-protected oxoalcohols and aldehydes. The acid products exhibit anti-inflammatory, analgesic and anti-pyretic activity.
Abstract: 2-(6'-Substituted-2'-naphthyl)acetic acid derivatives substituted at the 2-position of the acetic acid moiety with methyl, methylene or halomethylene and the salts and esters thereof have anti-inflammatory, analgesic and anti-pyretic activities.
Abstract: Novel 2-substituted-1,2,4-thiadiazolo-[2,3-a]-benzimidazoles of the formula ##STR1## and the pharmaceutically acceptable salts thereof; and process for their preparation. These 2-substituted-1,2,4-thiadiazolo-[2,3-a]-benzimidazoles are useful as fungistatic and fungicidal agents.
Abstract: An NPN ruminant feed supplement having a high percentage of chemically bound urea is prepared from cellulose commodities by an efficient process involving reaction with urea and a concentrated mineral acid.
Type:
Grant
Filed:
December 8, 1975
Date of Patent:
February 1, 1977
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Kenneth L. Berger, Ronald J. Amen, Jorge J. Nassar, William B. Benken
Abstract: An inhalation device having an elongate housing having a passageway for the passage of air therethrough. The passageway, of relatively small diameter, opens into an emptying chamber, of relatively greater diameter, adjacent that end of the housing which is adapted for insertion into the mouth or nose of the user. Adjacent that end of the emptying chamber closest to the passageway, the housing has means for receiving or presenting a unit dose of powdered medicament for administration. During inhalation, a portion of the air stream passing through the passageway into the emptying chamber is deflected by a beveled deflector causing sufficient air flow to come into contact with the powdered medicament whereby the powdered medicament is entrained in the air stream being inhaled, and is carried into the nose, throat or lungs of the user where beneficial or therapeutic action of the medicament occurs.
Abstract: Benzene ring substituted benzimidazole-2-carbamate derivatives represented by the formula: ##STR1## where R is a lower alkyl group having 1 to 4 carbon atoms; R.sup.1 is a heterocyclic ring having 1-4 hetero atoms; and M is O, S, or ##STR2## The R.sup.1 M-substitution is at the 5(6)-position. The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.
Type:
Grant
Filed:
September 22, 1975
Date of Patent:
January 25, 1977
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Colin C. Beard, John A. Edwards, John H. Fried
Abstract: A highly efficient process for preparing a nutritionally acceptable mixture of amino acids from erythrocytes comprises the steps of denaturization, hydrolysis and neutralization, desludging, decolorization, deionization, concentration and sterilization.
Type:
Grant
Filed:
June 16, 1975
Date of Patent:
January 18, 1977
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Myron A. Beigler, William B. Benken, Jorge J. Nassar
Abstract: Benzene ring substituted benzimidazole-2-carbamate derivatives represented by the formula: ##STR1## where R is a lower alkyl group having 1 to 4 carbon atoms; R.sup.1 is -SOR.sup.2, -SO.sub.2 R.sup.2, -SCN, -SR.sup.5, -OR.sup.5 or M'(CH.sub.2).sub.n MR.sup.7 where M and M' are independently O, S, ##STR2## R.sup.7 is lower alkyl having 1 to 4 carbon atoms, or aryl, and n is 1-4; R.sup.2 is lower alkyl having from 1 to 6 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, lower alkenyl or lower alkynyl having 3 to 6 carbon atoms, or aralkyl or aryl; and R.sup.5 is lower alkenyl, lower alkynyl, or aralkyl. The R.sup.1 substitution is at the 5(6)-position.The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.
Type:
Grant
Filed:
November 3, 1975
Date of Patent:
January 11, 1977
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Colin C. Beard, John A. Edwards, John H. Fried
Abstract: 1-Amino-3-(4- or 5-substituted thiazol-2-oxy)-2-propanol and/or substituted amino derivatives thereof; 3-(4- or 5-substituted thiazol-2-oxy)-1,2-epoxypropane and 5-(4- or 5-substituted thiazol-2-oxymethylene)-oxazolidine and/or N- and/or 2-substituted oxazolidine derivatives thereof, are methods of making such compounds. The compounds are characterized by an aminocarbonyl or carbonylamino type substituent at the 5- or 4-position on the thiazole ring. The above 1-amino-3-(4- or 5-substituted thiazol-2-oxy)-2-propanol and derivatives exhibit cardiovascular activity and are useful in the treatment of abnormal heart conditions in mammals. The 3-(4- or 5-substituted thiazol-2-oxy)-1,2-epoxypropanes are useful as intermediates for the aforementioned cardiovascular agents.
Abstract: Novel racemic and antimeric prostaglandin analogs having a difluoromethylene group attached to the C-11,12 positions of the molecule, and oxygenated functions at C-9 and C-15, which may be further substituted at C-15 by a methyl group and processes for the production of such compounds. Also included are the lower alkyl esters of the carboxylic acid function and pharmaceutically acceptable salts thereof. These compounds possess prostaglandin-like activities and thus are useful in the treatment of mammals, where prostaglandins are indicated.
Abstract: 2-Naphthyl acetic acid derivatives and the corresponding amides, esters, hydroxamic acids and addition salts thereof, optionally substituted at the .alpha.-position on the acetic acid moiety and/or at position 6 and/or at positions 1, 4, 7 or 8 on the naphthyl ring and optionally saturated at positions 3 and 4, are anti-inflammatory, analgesic, antipyretic and anti-pruritic agents. A pharmaceutical method of effecting treatment of inflammation, pain, pyrexia and pruritus by the administration of naphthyl acetic acid derivatives. A pharmaceutical composition for use in the treatment of the above maladies comprising a naphthyl acetic acid derivative.
Abstract: A method for lowering elevated serum lipid concentrations comprising administering a composition containing, as the active ingredient, a 3.beta.-substituted-16.alpha.-cyanopreg-5-en-20-one wherein the substituent at the 3.beta.-position is selected from the group consisting of hydroxy, alkoxy having 1 to 6 carbon atoms, cycloalkoxy having 3 to 6 carbon atoms, acyloxy wherein the acyl moiety has 2 to 7 carbon atoms tetrahydrofuran-2'-yloxy, tetrahydropyran-2'-yloxy, and 4'-alkoxytetrahydropyran-4'-yloxy where the alkoxy moiety has 1 to 6 carbon atoms. Representative active ingredients are 3.beta.-acetoxy-16.alpha.-cyanopreg-5-en-20-one and 3.beta.-cyclopentyloxy-16.alpha.-cyanopregn-5-en-20-one. These representative agents are also useful in the therapeutic method of protecting and regenerating damaged hepatic tissue.
Abstract: An axial tomographic scanner having means for supporting a plurality of cables leading to the X-ray source including a yoke upon which the X-ray source is mounted, first bracket means mounted on the yoke adjacent the X-ray source for restraining cable movement, second bracket means mounted on the yoke remote from the X-ray source for restraining cable movement, and means disposed between the first and second bracket means for maintaining the cables passing therethrough in a gradual arc while preventing undue flexing of the cables and undesirable movement of the cables into interfering position with other components of the axial tomographic scanner.
Abstract: Novel prostaglandin intermediates and process for the production thereof. Compounds, and process for the production thereof, useful in the production of (dl)-[1.alpha.-hydroxy-3.beta.-(3S-tetrahydropyranyloxy-trans-1-octenyl)-4 .alpha.-tetrahydropyranyloxycyclopent-1.alpha.-yl] acetaldehyde hemiacetal and [1.alpha.-hydroxy-3.beta.-(3S-tetrahydropyranyloxy-trans-1-octenyl)-4.alph a.-tetrahydropyranyloxycyclopent-1.alpha.-yl] acetaldehyde hemiacetal.
Type:
Grant
Filed:
January 15, 1975
Date of Patent:
December 21, 1976
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Francisco S. Alvarez, Albert R. Van Horn
Abstract: 3'-O-Acyl- and 3-'-O-acyl-5-'-O-acyl- derivatives of 1-(.beta.-D-arabinofuranosyl)-cytosines and methods of preparing these compounds and also O.sup.2,2'-anhydro-1-(3'-O-acyl-5'-O-acyl-.beta.-D-arabinofuranosyl)-cytos ine salts. The O.sup.2,2'-anhydro-1-(3'-O-acyl-5'-O-acyl-.beta.-D-arabinofuranosyl)-cytos ine nucleoside salts are prepared by direct acid catalyzed acylation of the salts of the corresponding O.sup.2,2'-anhydro-1-(.beta.-D-arabinofuranosyl)-cytosines or 3'-O-acyl- derivatives, under carefully controlled conditions. The 3'-O-acyl- and 3'-O-acyl-5'-O-acyl-1-(.beta.-D-arabinofuranosyl)-cytosines are prepared from the corresponding O.sup.2,2'-anhydro nucleosides via selective cleavage of the O.sup.2,2'-anhydro bridge under carefully controlled conditions. The compounds exhibit anti-viral, cytotoxic and anti-neoplastic activity, and thus are useful for the treatment of mammals where such agents are indicated.