Abstract: New compounds of the formula ##STR1## wherein: R.sup.1 is cycloalkyl of five to seven carbon atoms optionally substituted with one or more lower alkyl groups;R.sup.2 is alkyl of two to twelve carbon atoms, cycloalkyl of five to seven carbon atoms, or cycloalkylalkyl of six to ten carbon atoms wherein the cycloalkyl group may be optionally substituted with one or more lower alkyl groups;R.sup.3 is hydrogen or lower alkyl;a is 0, 1, 2 or 3; andb is 1, 2 or 3;and the pharmaceutically acceptable acid addition salts thereof are useful as spermicidal and spermatostatic agents.
Abstract: A compound useful as antifungal, antibacterial and antiprotozoal agents and as spermicides have the formula ##STR1## and the acid addition salts thereof wherein Z is oxygen or sulfur;m is 0, 1, 2 or 3;n is 1, 2 or 3;R.sup.1 is hydrogen; alkyl; cycloalkyl; cycloalkyl-lower-alkyl; optionally substituted phenyl; phenyl-lower-alkyl; monocyclic heteroaromatic ring; monocyclic heteroaromatic-lower-alkyl; naphthyl; or naphthyl-lower-alkyl.A and B are independently hydrogen, halo, lower alkyl or lower alkoxy and either one of A or B may be nitro, amino or alkanoylamino;Q is (a) NR.sup.2 R.sup.3 or (b) NR.sup.4 C(X)YR.sup.5 whereinX is oxygen or sulfur;Y is oxygen, sulfur, NR.sup.6 or a bond;R.sup.2 is hydrogen; alkyl; cycloalkyl; cycloalkyl-lower-alkyl; optionally substituted phenyl or optionally substituted phenyl-lower-alkyl;R.sup.3 is hydrogen or lower alkyl; orR.sup.2 and R.sup.3 together with N is a five or six membered optionally substituted ring;R.sup.4 and R.sup.6 are independently hydrogen or lower alkyl;R.
Abstract: Methods are provided for reducing non-specific interference in competitive protein binding assays employing as the labeled reagent a fluorescent conjugate of a hydrophobic ligand conjugated to a fluorescer, which in turn is bound to a water soluble polysaccharide carrier ("fluorescer conjugate reagent"). In order to reduce non-specific interference from physiologic samples, the fluorescent reagent is combined with a lipid substituted neutral support, under conditions which provides two binding fractions: a first weakly binding fraction which is relatively free of non-specific interference in a competitive protein binding assay employing physiological fluids; and a second fraction, which more strongly binds to the lipid substituted support.
Abstract: Disclosed herein are novel allene-containing compounds of the formula ##STR1## wherein R is hydrogen, alkyl of 1 to 6 carbon atoms or a pharmaceutically acceptable salt; X is CH.dbd.CH, OCH.sub.2, CH.sub.2 O, CH.sub.2 S, SCH.sub.2, O or S; n is 1 or 2 but is 1 when X is CH.dbd.CH; m is 0-6; and the dotted lines represent a single or double bond. These compounds mediate leukotriene-caused physiological changes in mammals.
Type:
Grant
Filed:
October 13, 1982
Date of Patent:
May 7, 1985
Assignee:
SYNTEX (U.S.A.) Inc.
Inventors:
John W. Patterson, Jr., Jurg R. Pfister
Abstract: Compounds of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: Z is S;Y is halo, alkoxy, alkyl, or dialkylamino;a is 0, 1 or 2;b is an integer from 2-12 with the proviso that if b is 2 or 3, a cannot be 0, and with the further proviso that if X is OH, b cannot be 2-5 and with the further proviso that if X is --NH.sub.2, b cannot be 2-5; andX is selected from the group consisting of: --OH, OR.sup.1, --NH.sub.2, --NHR.sup.1, NR1/2, ##STR2## and --NHCONHR.sup.2 in which each R.sup.1 is independently alkyl or cycloalkyl or, in --NR1/2, both R.sup.1 s together are alkylene or form a piperazine ring optionally substituted at the ring N by alkyl or --CH.sub.2 CH.sub.2 OH; andR.sup.2 is alkyl, cycloalkyl, or optionally substituted phenyl;have antiinflammatory properties and are useful in the treatment of conditions characterized by inflammation and swelling.
Type:
Grant
Filed:
February 18, 1982
Date of Patent:
April 23, 1985
Assignee:
Syntex (U.S.A.), Inc.
Inventors:
Peter H. Nelson, Howard J. Ringold, Stefan H. Unger, Thomas R. Thieme
Abstract: 5-benzoyl-7-halo-1,2-dihydro-3H-pyrrolo[1,2-a]-pyrrole-1-carboxylic acids, represented by the formula ##STR1## and the pharmaceutically acceptable non-toxic esters and salts thereof, wherein:R is hydrogen or lower alkyl;X is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, carboxyl, lower alkylcarbonyl, sulfonic acid, sulfonic acid alkyl ester, fluoro, chloro, or bromo; and Y is chloro or bromo, which are novel, and 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids which are represented by the formula ##STR2## wherein X and R are as above defined except that X cannot be chloro or bromo, are prepared by decarboxylation of the corresponding 1,1 dicarboxylates. Intermediates in said preparation are also disclosed.
Abstract: Novel compounds of the general formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each independently hydrogen, lower alkyl, lower alkoxy, trifluoromethyl, halo, lower alkylthio, lower alkyl sulfinyl or lower alkyl sulfonyl;R.sup.5 is hydrogen or lower alkyl;m is 0 or 1;W is alkylene, --CH.dbd.CH--, --O--, or --N(R.sup.6)--, where R.sup.6 is lower alkyl or hydrogen;n is 0 or 1; andQ is lower alkyl, cycloalkyl or optionally substituted phenyl.These compounds combine .beta.-blockade and calcium entry blockade properties in the same compound and therefore are useful in therapy in the treatment of cardiovascular diseases, including myocardial infarction, hypertension, arrhythmia and variant and exercise induced angina. The compounds are also useful in immunosuppressant therapy for immune diseases, such as rheumatoid arthritis.
Abstract: 2-(1,4-Benzodioxan-2-ylalkyl)imidazoles having the general formula: ##STR1## wherein R.sup.1, and R.sup.2 and R.sup.3 are independently selected from the group consisting of hydrogen, and alkyl (1-6C), and wherein n is an integer equal to 0, 1 or 2, and the pharmaceutically acceptable acid addition salts thereof, are .alpha..sub.2 blockers and thus are useful as affectors of the CNS, specifically as platelet aggregation inhibitors and as antihypertensives.
Type:
Grant
Filed:
August 5, 1981
Date of Patent:
February 5, 1985
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Arthur F. Kluge, Arthur M. Strosberg, Roger L. Whiting, George A. Christie
Abstract: Novel compounds of this invention are tetrazole, acylhydroxylamine, hydroxymethylketone and amide derivatives of unsaturated fatty acids which are selective inhibitors of the enzymes lipoxygenase and cyclooxygenase involved in the production of pain, inflammation, bronchoconstriction and allergic reactions. These compounds are beneficial in the treatment of a number of inflammatory and/or painful conditions and allergic reactions.
Abstract: Chloramphenicol derivatives are provided for use in preparing antigen conjugates for the production of antibodies specific for chloramphenicol. Specifically, the aryl group is derivatized with a side chain functionalized to provide for a carbonyl functionality to react with amino groups of a poly(amino acid). The conjugate is then injected into a vertebrate for production of antisera which are isolated in conventional ways and find particular use in competitive protein binding assays.
Abstract: This invention relates to novel imidazolidinone prostaglandin compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1 and R.sup.2 are independently hydrogen or alkyl of 1 to 4 carbons; R.sup.3 is hydrogen or methyl; and R4 is --(CH.sub.2).sub.n CH.sub.3 wherein n is 3-7, cycloalkyl of 5-7 carbons, a substituent of the formula ##STR2## wherein R.sup.5 is hydrogen, alkyl of 1 to 4 carbons, alkoxy of 1 to 4 carbons, halo or trifluoromethyl. These compounds are inhibitors of blood platelet aggregation.
Abstract: The present invention relates to novel synthetic antigens, conjugates and antibodies based upon specific peptide sequences and the production thereof. More particularly, the invention relates to a polypeptide which is a determinant site of a protein, the polypeptide having from 8 to 20 amino acid residues, having an amino-terminal amino acid and a carboxyl-terminal amino acid, wherein the polypeptide includes:(a) a four amino acid sequence which corresponds to the four amino acid sequence of a .beta.-turn of the protein;(b) a sequence of two to eight amino acid residues attached to the amino terminal (H.sub.2 N--) of the four amino acid sequence; and(c) a sequence of two to eight amino acid residues attached to the carboxyl terminal (--COOH) of the four amino acid sequence,wherein the amino acid residues of subparts (b) and (c) correspond to those attached to the amino terminal and the carboxyl terminal, respectively of the .beta.
Type:
Grant
Filed:
October 17, 1983
Date of Patent:
January 15, 1985
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
John J. Nestor, Jr., John G. Moffatt, Hardy W. Chan
Abstract: A transverse motion linkage for a patient support has a four-bar linkage connecting the seat of the support and the base for forward transverse motion upon simultaneous reclining of the backrest and lifting of the leg rest through action of a three-bar, motion-imparting linkage.
Abstract: Compounds according to the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein: n is an integer of 1 to 6;R.sub.1 is hydrogen or alkyl of 1 to 4 carbons;R.sub.2 is hydrogen or R.sub.1 and R.sub.2 are combined to form an oxo group;R.sub.3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl or hydroxy lower alkyl;R.sub.4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl;Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy;A is an amide forming group wherein the nitrogen substituents are: hydrogen; alkyl of 1 to 6 carbon atoms; hydroxyalkyl of 1 to 6 carbon atoms and its aliphatic acylates of 1 to 6 carbon atoms or aryl acylates of 7 to 12 carbon atoms; cycloalkyl of 3 to 7 carbon atoms or cycloalkyl lower alkyl of 4 to 11 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lower alkoxy, OH, --OCOR.sub.5, halo, --NH.sub.2, --N(R.sub.5).sub.2, --NHCOR.sub.5, --COOH, or --COO(R.sub.5) group wherein R.sub.
Type:
Grant
Filed:
February 16, 1983
Date of Patent:
December 25, 1984
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Gordon H. Jones, Michael C. Venuti, Robert Alvarez, John J. Bruno
Abstract: A stable pharmaceutical composition which comprises an acid salt of a thieno-pyridine derived compound, a pharmaceutically acceptable, non-volatile acid and optionally other suitable pharmaceutical excipients.
Abstract: Compounds of the formula: ##STR1## wherein R is alkyl of 1 to 12 carbon atoms, cyclopentyl, cyclohexyl, cyclopentylloweralkyl or cyclohexylloweralkyl;Z is ethylene or propylene, optionally substituted with a single substituent which is lower alkyl;A is the integer 1, 2, or 3; andthe pharmaceutically acceptable acid addition salts thereof, said compounds being useful as spermicidal, antimicrobial and anticonvulsant agents and thromboxane synthetase inhibitors.
Abstract: An injection device particularly suitable for the intraruminal injection of ruminants is described. The injection device is characterized by a needle carrying means and a needle actuation means, which are operatively coupled such that the needle actuation means permits movement of the needle carrying means from a retracted position to an extended position, wherein the needle is capable of piercing the rumen, only when the needle carrying means is in a preferred orientation (e.g. perpendicular) to the surface of the host animal at the injection site. The injection device is further characterized by a dose delivery actuation means which is responsive to the relative position of the needle carrying means and the needle actuation means such that the dose is delivered to the host animal only when the needle carrying means and the needle actuation means are in a preferred position relative to each other.
Type:
Grant
Filed:
September 13, 1983
Date of Patent:
December 11, 1984
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Terrence B. Christensen, Allen D. McNaughton, Steven R. Umbach
Abstract: A vibratory endodontic device is described for mechanical preparation of dental radicular canals, i.e., root canals, prior to their obturation. The device includes a housing, a vibratory drive means supported within the housing to minimize the transfer of vibration to the housing, an endodontic file connected to the drive means for vibratory movement and stop means operatively connected to the housing and substantially isolated from the mechanical vibrations created by the vibratory drive means. Additionally, fluid transport means are provided for maintaining a continuous flow of irrigation fluid along the endodontic file. Various assemblies for retaining the endodontic files on the operative end of the vibrating device are also described.