Abstract: 3-[3-(1-Methyltetrazol-5-ylthio)-prop-1-(t)-enyl]-7.beta.-(.alpha.-substitu ted acetamido)-ceph-3-em-4-carboxylic acid; 7.beta.-(.alpha.-substituted acetamido)-3-[3-(1,2,4-triazol-5-ylthio)-prop-1-(t)-enyl]-ceph-3-em-4-carb oxylic acid derivatives and salts thereof; and ester intermediates and processes for preparing such compounds. The compounds are useful as antibacterials and are active against a wide variety of gram positive and gram negative bacteria.
Abstract: 1-Amino-3-[2-thiazoloxy]-2-propanol and substituted 1-amino derivatives thereof; 3-[2-thiazoloxy]-1,2-epoxypropane 5-[thiazol-2-oxymethylene]-oxazolidine and/or N-substituted and/or 2-substituted oxazolidine, derivatives thereof and methods of preparing such compounds. The above 1-amino-3-[2-thiazoloxy]-2-propanol and derivatives exhibit .beta.-adrenergic stimulating cardiovascular activity and are useful for the treatment of abnormal heart conditions in mammals. The above 3-[2-thiazoloxy]-1,2-epoxypropane and derivatives are useful as intermediates for the aforementioned cardiovascular agents. The 5-[thiazol-2-oxymethylene]-oxazolidine and derivatives are intermediates for aforementioned cardiovascular agents. The 1-amino-3-[2-thiazoloxy]-2-propanol and derivatives can be prepared by base or acid hydrolysis of the corresponding 5-[thiazol-2-oxymethylene]-oxazolidine or derivatives; or by treatment of the corresponding 3-[2-thiazoloxy]-2,3-epoxypropane or derivative with the desired amine or amino-derivative.
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, anti-pyretic 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: 2-(5H-dibenzo[a,d]cyclohepten-5-on-2-yl) acetic, propionic and butyric acids, and esters and salts thereof, are prepared by solvolysis of nitrile or amide intermediates, or of ketal-protected nitrile, amide, acid, ester or salt intermediates.
Type:
Grant
Filed:
September 8, 1975
Date of Patent:
September 7, 1976
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Peter H. Nelson, Karl G. Untch, James P. Dunn
Abstract: Compositions containing and methods employing, as the essential ingredient, novel disubstituted xanthone carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed. 5-Isopropyl-7-acetylxanthone-2-carboxylic acid is illustrated as a representative compound.
Type:
Grant
Filed:
December 4, 1975
Date of Patent:
September 7, 1976
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Jurg R. Pfister, Ian T. Harrison, John H. Fried
Abstract: Preparation of .alpha.,.beta.-unsaturated carbocyclic ketones by reacting an enol lactone with a carbanion generated by treatment of a methylphosphonate or a mono-substituted methylphosphonate with base.
Abstract: Novel 2-substituted-1,2,4-thiadiazolo-[2,3-a]-imidazoles of the formula ##SPC1##And the pharmaceutically acceptable salts thereof; and process for their preparation. These 2-substituted-1,2,4-thiadiazolo-[2,3-a]-imidazoles are useful as fungistatic and fungicidal agents.
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, anti-pyretic 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: 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, anti-pyretic 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: Novel 2-substituted-1,2,4-thiadiazolo-[2,3-a]-benzimidazoles of the formula ##SPC1##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: 2-(6-Methoxy-2-naphthyl)propionic acid is prepared by reacting di(6-methoxy-2-naphthyl)-zinc or 6-methoxy-2-naphthylzinc halide with a lower alkyl 2-halopropionate in a suitable solvent to form a lower alkyl 2-(6-methoxy-2-naphthyl)propionate and hydrolyzing the ester group thereof. The product has anti-inflammatory, analgesic and anti-pyretic activities.
Abstract: (d1)-13-Substituted sulfinyl-prostaglandin-like [(d1)-2.alpha.-substituted-3.beta.-(1.alpha.-substituted sulfinyl-trans-2-alkenyl)-1-oxygenated cyclopentane and (d1)-2.alpha.-substituted-3.beta.-(1.alpha.-substituted sulfinyl-trans-2-alkenyl-4.alpha.-hydroxy-1-oxygenated cyclopentane]compounds exhibiting prostaglandin-like biological properties are prepared from known prostaglandins and prostaglandin-like compounds.
Abstract: 2-Substituted-5-oxo-5H-dibenzo[a,d]cycloheptenes represented by the following formula: ##SPC1##Where one of R.sup.2 and R.sup.3 is hydrogen, and the other is hydrogen, methyl, or ethyl, or together R.sup.2 and R.sup.3 are methylene; and R' and R.sup.4 are alkoxy, or together R' and R.sup.4 are =O, =NOH, =NNHCONH.sub.2, or alkylenedioxy of the formula --O--CH.sub.2 --(CR.sup.5.sub.2).sub.n --CH.sub.2 --O-- where n.sub.5 is O--2, R.sup.5 is hydrogen or methyl when n is 1, and R.sup.5 is hydrogen when n is 2, or one of R' and R.sup.4 is --OH and the other is (SO.sub.3 Y) where Y is sodium or potassium. The compounds have anti-inflammatory, analgesic and anti-pyretic activities and, accordingly, are useful in the treatment of inflammation, pain and pyrexia.
Abstract: Novel compounds useful as anti-inflammatories are represented by the formula ##SPC1##Wherein Z is a single or double bond; X and X.sup.1 are independently H, F or Cl; and X.sup.2 is OH or when X.sup.1 is Cl X.sup.2 may also be Cl. The compounds are prepared by reacting a suitable 21-hydrocarbon sulfonate steroid with an alkali cyanide.
Abstract: This invention is a screening apparatus for retaining small marine animals in a growing container connected to closed-loop aquaculture system. The screening apparatus comprises (a) a first plate; (b) a second plate about the same size as the first plate and substantially parallel to and spaced from the first plate; (c) a conduit passing through a centrally-located aperture in the first plate, the end of the conduit being attached to a face of the second plate, the corresponding edges of said plates being about the same distance from the outer wall of the conduit; (d) a fluid permeable material extending between the edges of said plates and enclosing said conduit by being snugly fitted at least around the periphery of the first plate; (e) the conduit having apertures around its circumference; and (f) a pump means for transferring a fluid through the conduit. The screening device is particularly useful in a closed-loop aquaculture system which includes a biological filter means.
Abstract: An inhalation device having an elongate housing having an emptying chamber adjacent that end of housing which is adapted for insertion into the mouth or nose of a user. A plurality of passageways extending essentially perpendicular to the longitudinal axis of the housing intersect with the inner end of the emptying chamber. Adjacent that end of the emptying chamber closest to the passageways, the housing has means for receiving or presenting a unit dose of powdered medicament for administration. During inhalation, 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: Novel prostaglandin dehydro analogs of the PGA and PGB series and the 9-hydroxy-derivatives thereof, which possess a diethylenic unsaturation in the carboxylic acid chain and may be additionally substituted at C-4, C-6, C-9 and/or C-15 by a methyl, ethyl or propyl group, as well as the C-20-nor, bisnor or C-20 alkyl derivatives thereof, the alkyl group being of a straight chain and containing from 1 to 5 carbon atoms inclusive,, and processes for making same. 9-keto-15.alpha.-hydroxyprosta-4,5,10,13-trans-tetraenoic acid and 9-keto-15.alpha.-hydroxyprosta-4,5,8(12),13-trans-tetraenoic acid are representative of the class. Also included are the pharmaceutically acceptable, non toxic esters and salts of the carboxylic acid function and the pharmaceutically acceptable, non toxic esters and/or ethers of the secondary hydroxyl groups. These compounds possess prostaglandin-like activities and thus are useful in the treatment of mammals, where prostaglandins are indicated.
Type:
Grant
Filed:
July 15, 1974
Date of Patent:
July 20, 1976
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Pierre Crabbe, John H. Fried, Angel Guzman
Abstract: (dl)-13-Substituted sulfinyl-prostaglandin-like [(dl)-2.alpha.-substituted-3.beta.-(1.alpha.-substituted sulfinyl-trans-2-alkenyl)-1-oxygenated cyclopentane and (dl)-2.alpha.-substituted -3.beta.-(1.alpha.-substituted sulfinyl-trans-2-alkenyl)-4-oxygenated-1-oxygenated cyclopentane] compounds exhibit prostaglandin-like biological properties and are also useful intermediates in the preparation of known prostaglandins.
Abstract: The novel 16,17-secoestra-4,9(10)-diene, 16,17-secoestra-4,9(10),11-triene, 16,17-secogona-4,9(10)-diene and 16,17-secogona-4,9(10)-triene compounds and the 14.beta.-isomers thereof useful as antiandrogenic agents, and methods for their preparation.
Type:
Grant
Filed:
November 22, 1974
Date of Patent:
July 13, 1976
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Pierre Crabbe, John A. Edwards, John H. Fried
Abstract: This invention is a small, aquatic animal-collecting device which comprises a container for water being open at one end and closed at the other; a fluid inlet means to said container; a fluid conduit means positioned within and extending about the vertical length of the container and passing through the bottom of the container; a fluid outlet means positioned in the upper portion of the conduit; and a screening means positioned between the side walls of the container and the fluid outlet means so that the animals are retained in the container in sufficient water, while excess water passes through the screen and out the outlet means. This apparatus is particularly well suited for the process of collecting prawn larvae from a closed-loop aquaculture system.