Abstract: Esters of 2-substituted-5-oxo-5H-dibenzo[a,d]cycloheptenes represented by the following formula: ##STR1## where R' is --CH.sub.2 --CH.dbd.CH.sub.2, --CH.sub.2 --CH(OH)--CH.sub.2 OH, ##STR2## where Y is either O or S, or ##STR3## where R.sup.4 and R.sup.5 are independently hydrogen, alkyl having 1 to 6 carbon atoms, phenyl, or benzyl, or together R.sup.4 and R.sup.5 form an alkylene bridge having 4, 5 or 6 carbon atoms; 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. The compounds have anti-inflammatory, analgesic, and antipyretic activities and, accordingly, are useful in the treatment of inflammation, pain and/or pyrexia.
Abstract: Compounds represented by the formula ##STR1## wherein R is hydrogen or alkyl of 1-4 carbons, R.sup.1 is alkyl of 1-6 carbons and the naphthyl group is attached to the imidazole ring at the 1 or 2 positions of the naphthyl ring and the pharmaceutically acceptable salts thereof are useful as centrally acting skeletal muscle relaxants.
Type:
Grant
Filed:
June 3, 1977
Date of Patent:
August 29, 1978
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Colin C. Beard, Marshall B. Wallach, Klaus Weinhardt
Abstract: Apparatus for subcutaneously implanting drug-containing pellets in animals. The apparatus comprises a handle; attached to the handle, a track along which a carriage moves; a carriage which moves along the track, the carriage having (i) a front part adapted to receive and retain a detachable needle having a passageway extending the length of the needle and (ii) a passageway extending the length of the carriage and corresponding to the needle passageway when retained in the carriage; a means to propel the carriage from the front to the rear of the track; means at the front and rear of the track to stop the carriage; a straight, retractable rod detachably attached to the rear stopping means so that the rod extends straight through the carriage passageway; a finger actuatable trigger attached to the handle to actuate the retraction of the carriage.
Abstract: An inhalation device having an elongate housing having a passageway for the movement of air therethrough. The passageway terminates in an emptying chamber adjacent that end of the housing which is adapted for insertion into the mouth or nasal passages of a user thereof. The housing has means for receiving and opening a container holding a unit dose of powdered medicament for administration. The opening means includes first means for placing the interior of the opened capsule in communication with the atmosphere and second means for placing the interior of the opened capsule in communication with the emptying chamber via the passageway in the housing. During inhalation, air drawn through the first means causes the powdered medicament to be expelled from the container through the second means, the passageway and the emptying chamber into the nose, throat or lungs of the user where beneficial or therapeutic action of the medicament occurs.
Abstract: Novel dibenzo[b.f]thiepin and oxepin compounds of the formula and the pharmaceutically acceptable esters and salts thereof, wherein R is hydrogen or methyl; X is oxygen or S(O).sub.n in which n is the integer 0, 1 or 2 and Z is a single or double bond, provided that when Z is a double bond X is not SO, and when R is methyl the compounds are (dl) mixtures, and methods for the production thereof.
Abstract: A breath actuated inhalation device having a 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 device has means for receiving and opening 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: Novel 5-(2-pyrroyl) and 5-(N-lower alkyl-2-pyrroyl)-1,2-dihydro-3H-pyrrolo?1,2-a!pyrrole-1-carboxylic acid compounds represented by the formula: ##STR1## and the pharmaceutically acceptable, non-toxic esters and salts thereof, wherein each of R and R.sup.1 is independently hydrogen or a lower alkyl group having from 1 to 4 carbon atoms and process for the production of such compounds; 5-(N-methyl-2-pyrroyl)-1,2-dihydro-3H-pyrrolo?1,2-a!pyrrole-1-carboxylic acid is representative of the class. These compounds are useful as anti-inflammatory analgesic and anti-pyretic agents and as smooth muscle relaxants.
Type:
Grant
Filed:
March 31, 1977
Date of Patent:
June 27, 1978
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Joseph Martin Muchowski, Arthur Frederick Kluge
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: A novel spherical implant pellet containing estradiol, estradiol benzoate, or mixtures thereof as the sole active ingredients which exhibits a substantially constant drug release rate over a timer period and substantially abrupt termination of drug release at the end of the time period is prepared which has an inert spherical core of a diameter of about 2-10 mm and a uniform coating of about 0.05-1 mm completely covering the core, the coating comprising about 5-99% suitable carrier and 1-95% drug. A drug may be administered at a constant rate over a chosen period by implanting the novel pellet and the release is substantially abruptly terminated at the end of said period without removing the pellet.
Abstract: 3-(3-hydroxyprop-1-(t)-enyl)-7.beta.-(.alpha.-substituted acetamido)-ceph-3-em-4-carboxylic acids; 3-(3-carbamoyloxyprop-1-(t)-enyl)-7.beta.-(.alpha.-substituted acetamido)-ceph-3-em-4-carboxylic acids; and 3-[3-(N-substituted carbamoyloxy)prop-1-(t)-enyl]-7.beta.-(.alpha.-substituted acetamido)-ceph-3-em-4-carboxylic acids and derivatives and salts thereof and process 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: Novel 5-aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid compounds represented by the formula ##STR1## and the pharmaceutically acceptable, non-toxic esters and salts thereof, wherein R is hydrogen or a lower alkyl group containing from 1 to 4 carbon atoms and R.sup.1 is hydrogen, a lower alkyl group having from 1 to 4 carbon atoms, a lower alkoxy group of 1 to 4 carbon atoms, chloro, fluoro or bromo, the R.sup.1 substitution being at the ortho, meta or para positions of the aroyl group and process for the production of such compounds; 5-p-toluoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid is representative of the class. These compounds, as the racemic mixture or the (1)-isomer, are useful as anti-inflammatory, analgesic and antipyretic agents and as smooth muscle relaxants.
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 dilute mineral acid at low pH.
Type:
Grant
Filed:
February 25, 1977
Date of Patent:
May 16, 1978
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Kenneth L. Berger, Jorge J. Nassar, William B. Benken
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, and 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: 1-Lower alkyl-4,5-dihydro-5-phenyl-2-lower alkoxycarbonylaminoimidazoles, and substituted phenyl derivatives thereof, and pharmaceutically acceptable salts thereof, and methods of preparing such compounds. In one method, the compounds can be prepared by treating the corresponding .beta.-lower alkylamino-.beta.-(phenyl or substituted phenyl)-ethylamine with the desired 1,3-bis (alkoxycarbonyl)-S-methylisothiourea or 1-alkoxycarbonyl-S-methylisothiourea. The compounds can also be prepared by treating the corresponding 1-lower alkyl-2-amino-4,5-dihydro-5-(phenyl or substituted phenyl)-imidazole with the desired dialkylcarbonate. The subject compounds are useful as psychotherapeutic agents in treating or palliating abnormal conditions, in mammals, which involve the central nervous system.
Type:
Grant
Filed:
July 26, 1976
Date of Patent:
May 9, 1978
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Adolph P. Roszkowski, Colin C. Beard, Charles Dvorak, Klaus Weinhardt
Abstract: The racemic mixtures dl-6-(4-carbo lower alkoxybutyl)-4H-6H-thieno[3,4-d]furoxan are novel. The dl mixtures are prepared by reacting the lower alkyl ester of dl-7-thia-6-nitromethyl-9-nitrononenoic acid with phosphorus oxychloride and a tertiary amine catalyst.
Abstract: Novel 5-substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid compounds represented by the formulas ##STR1## and the pharmaceutically acceptable, non-toxic esters and salts thereof, wherein X is oxygen or sulphur, R is hydrogen or a lower alkyl group having from 1 to 4 carbon atoms and R.sup.1 is hydrogen, methyl, chloro or bromo, the R.sup.1 substitution being at the 3, 4 or 5 positions of the furan or thiophene ring in the compounds of Formula (A), and process for the production thereof; 5-(2-thenoyl)-1,2-dihydro-3H-pyrrolo-[1,2-a]pyrrole-1-carboxylic acid and 5-(3-furoyl)-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid are representative of the class. These compounds, as the racemic mixture or the (1)-isomer, are useful as anti-inflammatory, analgesic and antipyretic agents and as smooth muscle relaxants.
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' is lower alkyl having 1 to 6 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, lower alkenyl or lower alkynyl having 3 to 6 carbon atoms, or phenyl; R.sup.2 is hydrogen or R'; the R'R.sup.2 NC(O)- substitution being at the 5(6)-position; and the pharmaceutically acceptable salts thereof.The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.
Abstract: This application relates to novel immunological adjuvant compounds of the formula: ##STR1## wherein each of R and R.sup.1 are the same or different and are hydrogen or an acyl radical; R.sup.2 is an unsubstituted or substituted alkyl radical, or an unsubstituted or substituted aryl radical; X is an aminoacyl moiety; and Y is D-isoasparagine or D-isoglutamine.
Type:
Grant
Filed:
April 26, 1976
Date of Patent:
April 4, 1978
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Gordon H. Jones, John G. Moffatt, John J. Nestor, Jr.