Abstract: Inflammation is prevented, reduced or inhibited by administering muramyl and desmethylmuramyl dipeptides of the general formula: ##STR1## wherein each of R.sup.1 through R.sup.5 can independently be hydrogen or a variety of substituted or unsubstituted acyl, alkyl, aryl, or arylalkyl substituents. Pharmaceutical compositions containing such compounds useful for reducing inflammation are described.
Type:
Grant
Filed:
July 29, 1980
Date of Patent:
November 2, 1982
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Wendell H. Rooks, II, Neil R. Ackerman, Albert J. Tomolonis
Abstract: Compounds useful in the prevention and/or treatment of hypertension, congestive heart failure, arrhythmia, migraine, vasospastic disorders, and asthma are represented by the formula: ##STR1## wherein:R.sup.1 is ##STR2##R.sup.2, R.sup.3, and R.sup.4 are independently hydrogen or lower alkyl of one to four carbon atoms;X is hydrogen, lower alkyl of one to four carbon atoms, lower alkoxy of one to four carbon atoms or halo;m is 1 or 2; andn is 1, 2 or 3; andthe pharmaceutically acceptable acid addition salts thereof.
Abstract: Compounds of the formula ##STR1## wherein the serrated lines denote both endo and exo forms; R.sub.1 and R.sub.2 are the same or different and are C.sub.1 to C.sub.6 alkyl, C.sub.5 or C.sub.6 cycloalkyl, C.sub.5 or C.sub.6 cycloalkenyl, phenyl optionally substituted with C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy or halo, or 5 or 6 membered heterocyclic aryl wherein the heteroatom is oxygen, nitrogen or sulfur; R.sub.3 is a C.sub.1 to C.sub.6 alkyl radical; R.sub.4 and X are optionally present, and when present R.sub.4 is a C.sub.1 to C.sub.6 alkyl radical or hydrogen and X is an inorganic or organic anion which forms a pharmaceutically acceptable salt. Methods for preparing these compounds are also disclosed. The compounds of the present invention are useful as anticholinergic agents.
Abstract: Compounds useful in the prevention and/or treatment of hypertension, congestive heart failure, arrhythmia, migraine, vasospastic disorders, and asthma are represented by the formula ##STR1## wherein: R.sup.1 is ##STR2## wherein X is hydrogen, lower alkyl, lower alkoxy, halo, carboxamido or hydroxy; m is 1, 2 or 3; and n is 1, 2 or 3;R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen or lower alkyl; andthe pharmaceutically acceptable acid addition salts thereof.
Abstract: An improved process for 5-aroylation of 1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic esters and nitriles and for subsequent hydrolysis thereof is disclosed. In the improved process, an aroyl morpholide is reacted with the pyrrolo pyrrole system and the resultant decomposed with base.
Abstract: Novel compounds of the 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, hydroxy, lower alkyl, lower alkoxy or halo;R is hydrogen or lower alkyl; andA is selected from the group consisting of:2-(benzodioxan-2-yl)-2-hydroxyethyl;.omega.-(benzodioxan-2-yl)-alkyl (1-4);3-(aryloxy)-2-hydroxypropyl, wherein aryloxy is phenyloxy optionally substituted by 1-3 moieties selected from the group consisting of lower alkyl, lower alkoxy, halo, alkylsulfamido, lower alkoxycarbonyl, cyano and trifluoromethyl;.omega.-arylalkyl (1-4), wherein aryl is phenyl optionally substituted by 1-3 moieties selected from the group consisting of lower alkyl, lower alkoxy, halo, alkylsulfamido, lower alkoxycarbonyl, cyano and trifluoromethyl;.omega.-aryl-.omega.-oxoalkyl (1-4), wherein aryl is as herein defined;.omega.-aryl-.omega.-hydroxyalkyl (1-4), wherein aryl is as herein defined; and.omega.
Type:
Grant
Filed:
May 18, 1981
Date of Patent:
September 14, 1982
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Adolph P. Roszkowski, Robin D. Clark, Arthur F. Kluge
Abstract: 5-Substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids of the formula ##STR1## wherein: X is hydrogen, lower alkyl, chloro or bromo; Ar is a moiety selected from the group consisting of ##STR2## in which: Y is oxygen or sulfur;R is hydrogen, methyl, chloro, or bromo, the R substitution being at the 3, 4 or 5 position of the ring;R.sup.1 is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, lower alkylcarbonyl, fluoro, chloro or bromo, the R.sup.1 substitution being at any available position in the ring;R.sup.2 is hydrogen or lower alkyl; are prepared by .beta.-decarboxylation of the corresponding dialkyl-1,1-dicarboxylates. Certain substituted pyrroles are useful as intermediates for preparing the compounds of formula I.
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: 5-Substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids of the formula ##STR1## wherein: X is hydrogen or lower alkyl; Ar is a moiety selected from the group consisting of ##STR2## in which: Y is oxygen or sulfur;R is hydrogen, methyl, chloro, or bromo, the R substitution being at the 3, 4 or 5 position of the ring;R.sup.1 is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, lower alkylcarbonyl, fluoro, chloro or bromo, the R.sup.1 substitution being at any available position in the ring;R.sup.2 is hydrogen or lower alkyl;are prepared by .beta.-decarboxylation of the corresponding dialkyl-1,1-dicarboxylates. Certain substituted pyrroles are useful as intermediates for preparing the compounds of formula I.
Abstract: Novel 5-aroyl-6-chloro- or 6-bromo-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-7-carboxylic acids represented by the formula ##STR1## and the pharmaceutically acceptable, non-toxic esters and salts thereof, wherein Y is chloro or bromo and Ar is an optionally substituted phenyl, 2-furyl, or 2-thienyl ring or a 3-furyl, 3-thienyl, 2-pyrrolyl or 1-alkyl-2-pyrrolyl ring. These compounds are useful as anti-inflammatory, analgesic and antipyretic agents and as smooth muscle relaxants.
Abstract: Flexible polyvinyl chloride having improved flame retardancy and reduced smoke generating properties. The plastics are characterized in that they contain about from 0.01 to 0.2 parts, by wt., based on the iron content, of a high molecular weight ferrocene derivative and about 0.1 to 20 parts, by wt., of antimony oxide per 100 parts of polyvinyl chloride resin. A composition comprising the ferrocene derivative and antimony oxide useful for preparing the improved plastic is also disclosed.
Abstract: Nonapeptide and decapeptide analogs of LHRH which have the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein: X is a D-alanyl residue wherein one hydrogen on C-3 is replaced by:(a) a carbocyclic aryl-containing radical selected from the group consisting of phenyl substituted with three or more straight chain lower alkyl groups, naphthyl, anthryl, fluorenyl, phenanthryl, biphenylyl and benzhydryl; or(b) a saturated carbocyclic radical selected from the group consisting of cyclohexyl substituted with three or more straight chain lower alkyl groups, perhydronaphthyl, perhydrobiphenylyl, perhydro-2,2-diphenylmethyl, and adamantyl; or(c) a heterocyclic aryl containing radical selected from the group consisting of radicals represented by the following structural formulas: ##STR2## wherein A" and A' are independently selected from the group consisting of hydrogen, lower alkyl, chlorine, and bromine, and G is selected from the group consisting of oxygen, nitrogen, and sulfur;A is an aminoac
Type:
Grant
Filed:
October 6, 1980
Date of Patent:
July 27, 1982
Assignee:
Syntex Inc.
Inventors:
John J. Nestor, Gordon H. Jones, Brian H. Vickery
Abstract: The invention provides a method of treating hydrogels formed from the polymerization of monomers having reactive olefinic double bonds by contacting them with reactive thiol compounds. In a preferred embodiment where the hydrogel structure includes a cis-glycol containing unit, a suitable thiol is used in conjunction with a borate buffer. The present invention also provides materials that are treated with the above thiol compounds.
Abstract: This invention relates to a motion mechanism for moving an X-ray film in a panoramic X-ray machine in a predetermined pattern and rate of travel relative to a source of radiation. The mechanism includes a cassette holder on which is carried a rotatable rod or roller driven by a traction wheel, a lever assembly for changing the drive angle between the traction wheel and the rod and a moving or rotatable supporting column or structure on which the motion mechanism is mounted. The panoramic X-ray machine also has a radiation source suspended from one end of the supporting structure at a position opposite the cassette holder. The object or patient to be radiographed is placed between the radiation source and the cassette holder and the supporting structure is rotated at a selected rotational speed about the object.
Abstract: N-Vinyl carbazoles are prepared by reacting an N-unsubstituted carbazole with a dihaloethane in the presence of a phase transfer catalyst followed by reaction with an aqueous solution containing a highly basic agent. These N-vinyl carbazoles are useful, singly or in combination with other materials, as electrical capacitors and insulators, in thermal foam insulators, as components in copolymers and in image-recording systems, and as photoconductive materials in electrophotography.
Abstract: Compounds useful in the prevention and/or treatment of hypertension, congestive heart failure, arrhythmia, migraine, vasospastic disorders, and asthma are represented by the formula ##STR1## wherein: R, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently hydrogen or lower alkyl of one to four carbon atoms; andR.sup.5 and R.sup.6 are independently hydrogen, lower alkyl of one to four carbon atoms or lower alkoxy of one to four carbon atoms; andthe pharmaceutically acceptable acid addition salts thereof.
Abstract: A dental scaler is disclosed wherein an air-driven rotor is driven about a shaft to impart vibrations thereto and drive a work tool or other object attached to the shaft. The vibratory device includes means on the shaft for correcting displacement of the rotor from its drive position. That means comprises a portion of the shaft beneath the rotor means having an enlarged diameter such that movement of the rotor caused by shaft wear is corrected. Additional means may be associated with the rotor, e.g., chamfered end edges of the rotor, which minimize pressure differentials at the end of the rotor edges and consequently assist in centralization of the rotor about the outlet means on the shaft. The fluid outlet means comprises outlet ports in the shaft wall beneath the area of rotation of the rotor, the outlet ports having chamfered outside end edges to minimize power losses from turbulence. Additionally, means are provided along the shaft for selecting the vibrational mode in which the vibratory device operates.