Abstract: A temporomandibular joint (TMJ) articulator, capable of simulating common dental occlusion defects, has a maxillary frame on which may be releasably retained a maxillary practice denture, jaw movement guides slidably attached at the left and right sides of the frame, the lower end of each guide having a shaped recess functionally simulating a human TMJ socket, and a mandibular assembly having arcuate left and right jaw plates each bearing a slidably mounted roller and a condyle, the roller and condyle cooperating with the shaped recess to functionally simulate a human TMJ, and the assembly including means for releasably retaining a mandibular practice denture. The articulator is designed to fit within a dental manikin head, especially suitable for student training, which incorporates a solid skull and a flexible face, the face optionally having a tubular waste drain integral therewith.
Type:
Grant
Filed:
March 18, 1985
Date of Patent:
July 22, 1986
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Cosmo D. Bertino, III, N. Dominic Marucci
Abstract: Compounds of the formula ##STR1## wherein n is 1-3; R.sup.1, R.sup.2 and R.sup.3 are the same or different and are hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl or aryl lower alkyl wherein when aryl is phenyl it is unsubstituted or independently substituted with one or more halo, lower alkyl or lower alkoxy groups; and R.sup.4 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, trialkylsilyl, aryl or aryl lower alkyl wherein when aryl is phenyl it is unsubstituted or independently substituted by one or more halo, lower alkyl or lower alkoxy groups; excluding those compounds wherein R.sup.1 and R.sup.2 are hydrogen and R.sup.4 is ethyl, propyl or butyl. These compounds are useful as protease inhibitors.
Type:
Grant
Filed:
May 9, 1984
Date of Patent:
July 22, 1986
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Alexander Krantz, Tim F. Tam, Robin W. Spencer
Abstract: This invention relates to a process for making an enantiomer or racemic mixture of a compound of the formula ##STR1## wherein R is hydrogen, lower alkyl or a pharmaceutically acceptable, non-toxic salt of a compound wherein R is hydrogen; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is a .alpha. the other is .beta.; novel intermediates useful for preparing these compounds; and processes for making the intermediates.
Type:
Grant
Filed:
December 22, 1983
Date of Patent:
July 15, 1986
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Gary F. Cooper, Douglas L. Wren, Albert R. Van Horn, Tsung-Tee Li, Colin C. Beard
Abstract: This invention provides a method for inhibiting angiogenesis in mammals. A pharmaceutically acceptable formulation containing a compound of the formula ##STR1## where X.sub.1 X.sub.2 and X.sub.3 are H, C1, or F and X.sub.3 must be H if the substituent of R.sub.1 is .alpha.OH;R.sup.1 is chosen from the group consisting of hydroxyl and hydrogen;R.sub.2 is chosen from the group of alkyloxy or thioalkyls wherein said alkyls have less than 5 carbon atomsR.sub.3 is H or an alkyl having less than 6 carbon atoms, is administered to the mammal having undesirable angiogenesis.The wavy line at C-16 refers to either .alpha. or .beta..
Type:
Grant
Filed:
December 24, 1984
Date of Patent:
July 8, 1986
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Alain B. Schreiber, William J. Kowalski, Stefan H. Unger
Abstract: Conjugates of penicilloic acid derivatives and certain poly(amino acids), which are either antigenic or enzymatic, are provided. Antibodies raised against the antigenic poly(amino acids) and the enzyme conjugates are used as reagents in immunoassays. In particular, the compounds of the present invention can be used for measuring the presence of a .beta.-lactamase in a patient serum sample by adding a known amount of penicillin to the sample and observing the production of penicilloic acid over a fixed period of time.
Type:
Grant
Filed:
November 2, 1983
Date of Patent:
June 24, 1986
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Prithipal Singh, Danton K. Leung, Richard Rodgers
Abstract: Novel dihydropyridine derivatives which are useful for treating congestive heart failure, hypertension, and angina have the formula 1: ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein: n is an integer from 0 to 8;Y is --O, --NH, --NR.sub.2, --S, --S(O), --S(O).sub.2, or a bond;R.sub.1 and R.sub.2 are each independently A.sub.1, A.sub.2, A.sub.3 or A.sub.4 where:A.sub.1 is --(CH.sub.2).sub.m (CHOH).sub.p CH.sub.2 OH;A.sub.2 is --(CH.sub.2).sub.q CH.sub.(3-r) [(CH.sub.2).sub.s OH].sub.r ;A.sub.3 is --(CH.sub.2).sub.q CH.sub.(3-r) [(CH.sub.2).sub.p COOR.sub.3 ].sub.r ; andA.sub.4 is --(CH.sub.2).sub.m COOR.sub.3 ; where:m is an integer from 1 to 8;p is an integer from 0 to 4;q is an integer from 0 to 8;r is 2 or 3;s is an integer from 1 to 4; andR.sub.3 is H or alkyl of 1 to 18 carbon atoms;R.sub.4 is --NO.sub.2, --CF.sub.3, or halo; andR.sub.5 is lower alkyl or --CH.sub.2 CH.sub.2 OCH.sub.3.
Abstract: Methods and compositions are provided for performing an assay on whole blood samples. The method is for a determination of an analyte which is a member of a specific binding pair (sbp) consisting of ligand and homologous receptor. The method involves a binding agent for the red blood cells in such sample, a solid bibulous element to which is bound at least one sbp member, and a signal-producing system. The method comprises combining the whole blood sample, the binding agent, and none or, where appropriate, one or more members of the signal producing system. The medium is next contacted with a portion of a solid bibulous element to which is bound one of the members of the specific binding pair to allow the medium to traverse such element (immunochromatography). The solid bibulous element is contacted with any remaining members of the signal producing system. Signal resulting from the signal producing system is detected and is related to the amount of the analyte in the sample.
Abstract: Novel compound of the formula ##STR1## wherein n is an integer of 1 to 8;R.sub.1 is hydrogen or alkyl of 1-6 carbons;R.sub.2 is hydrogen;R.sub.3 is hydrogen, alkyl of 1-6 carbons, phenyl, benzyl, hydroxy lower alkyl, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl;R.sub.4 is hydrogen, alkyl of 1-6 carbons, benzyl, or hydroxy lower alkyl;Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy;any of its optical isomers, the mixture thereof, or the pharmaceutically acceptable acid addition salt.These compounds are inhibitors of thromboxane synthetase and cyclic AMP phosphodiesterase and are therefore potential cardiovascular agents particularly useful as platelet aggregation inhibitors and anti-thrombotic agents. Accordingly, these compounds will preferably be useful in treating cardiovascular disorders with thrombotic complications. However, they also possess vasodilatory, antisecretory, antihypertensive, inotropic and antimetastatic activities.
Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy, lower alkylthio, optionally substituted phenoxy or optionally substituted phenylthio,R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2 or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2; andW is alkyl of one to seven carbon atoms, optionally substituted phenyl or optionally substituted benzyl.
Type:
Grant
Filed:
December 22, 1983
Date of Patent:
June 3, 1986
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Gordon H. Jones, Michael C. Venuti, John M. Young
Abstract: A novel pharmaceutical composition which comprises an acid salt of a thieno-pyridine derived compound, a pharmaceutically acceptable, non-volatile organic acid (particularly citric acid) and optionally other suitable pharmaceutical excipients.
Abstract: An improved process for preparing the cyclic phosphate ester of substituted 9-(1,3-dihydroxy-2-propoxymethyl)purines which are useful as antiviral agents.
Abstract: A sampling device is disclosed. The device comprises a capillary tube having a first orifice for collecting and dispensing a liquid at one end of the tube and a second orifice at the other end of the tube. A chamber encloses the second orifice. The device has a small opening to the outside atmosphere, other than the first orifice, communicating with the capillary tube. Also included is substantially non-compressible means movable with respect to said opening for concomitantly sealing said opening and forcing air from said chamber through said capillary tube.
Abstract: Fluorescent antigen conjugates are provided comprising antigens covalantly bonded to at least one 2,7-dialiphatic substituted-9-phenyl-6-hydroxy-3H-xanthen-3-one, wherein the 1- and 8-positions are unsubstituted. Also provided are novel fluorescent compounds absorbing at wavelengths in excess of 500 nm, having active functionalities for linking to the antigen. Finally, methods are provided for analyzing antigens in serum, whereby serum interference is avoided.
Abstract: A door and drawer front particularly for use in clean-rooms has an outer member and a recessed area having a top grasping surface and a bottom grasping surface extending back into the outer member. A cleaning access area is also provided. The intersections and corners of the member, the recess and the grasping surfaces forming rounded junctions to facilitate easy cleaning and disinfecting of the door and drawer front.
Type:
Grant
Filed:
July 18, 1983
Date of Patent:
May 6, 1986
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Joe H. Kennedy, A. Ronald Holland, Thomas Richey, James D. Alsup, Jr.
Abstract: Methods are provided for rapidly determining a number of parameters in a few determinations. Particularly, the method is applicable to blood typing, determining the blood type as to the ABO and Rh type, as well as the determination of isoantibodies to the antigens. The method employs fluorescent particles having a plurality of fluorescers, where the presence or absence of light emission of a particular wavelength can be determined.
Abstract: Novel compositions and methods are provided for detecting the presence of a material of interest in a specimen on a solid surface. A composition useful for detecting the presence of a material of interest in a specimen comprises (1) a detector conjugate comprising a fluorescing moiety bonded to a compound capable of specific binding with the material of interest, or a derivative thereof, and (2) a non-detector conjugate comprising a poly(amino acid) and a compound having substantial structural and charge similarity to the fluorescing compound and no observable fluorescence, or low level fluorescence of a different wavelength than that of the fluoresing compound, in the region of fluorescence of the fluorescing compound. In the method of the invention, a specimen, on a solid surface, is combined with the detector conjugate and the non-detector conjugate, and the combination is incubated.
Type:
Grant
Filed:
October 7, 1983
Date of Patent:
April 15, 1986
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Pyare L. Khanna, Jimmy D. Allen, Ian Gibbons
Abstract: Synthetic nona-peptide and deca-peptide LHRH antagonist analogs have a novel guanido-substituted, amidine, tertiary or quaternary aminoacyl residue at position 6.
Abstract: An improved immunoassay for determining the presence of an analyte in a serum sample and conjugates therefor are described. The known method comprises combining the sample with a conjugate of the analyte and an enzyme and with a receptor for analyte, and determining the presence of analyte in the sample from the effect that the sample has on the enzymatic activity when compared to the enzymatic activity in the absence of analyte or in the presence of known amounts of analyte. The present invention resides in the conjugation to the enzyme label of a label protectant which allows modulation of the enzymatic activity to occur and minimizes background interference between the enzyme label and the sample, which would alter the enzymatic activity.
Abstract: Rates of binding between members of a specific binding pair, e.g., ligand-receptor, are greatly enhanced by short-term ultrasonication of an aqueous medium containing the specific binding pair. The enhanced rates find particular use in specific binding protein assays.