Abstract: A dispensing and packaging system for pellets such as ampules or vials. The system comprises an elongated resilient plastic tube in which the pellets are arranged in a line. The tube is of slightly smaller inner diameter than the pellets; and it is slit along its length so that it expands circumferentially to accomodate the pellets. The plastic material of the tube is sufficiently flexible and resilient at room temperatures to neck down in regions between adjacent pellets or in regions of the pellets which are of small diameter. This necking down provides restraint against axial movement of the pellets to hold them securely in the tube while allowing them to be dispensed individually with a minimum of difficulty.
Abstract: Cephamycin C is concentrated and purified by subjecting a fermentation broth which contains Cephamycin C to the following sequence of steps: filtration at acidic pH, adsorption of filtrate on activated carbon, removing the adsorbed antibiotic by contacting the carbon with a mixture of water and a polar organic solvent, contacting the eluate with an anion exchange resin, and eluting the resin with a salt solution at a pH of from about 5.5 to about 10.
Abstract: Pure isomannide monooleate and pure aluminum monostearate are used singularly or in combination in the preparation of emulsion type adjuvant vaccines to yield an adjuvant superior to prior art adjuvants which employ commercial mannide monooleate and aluminum monostearate. Highly desirable formulations are obtained by the inclusion of pure aluminum monostearate as a stabilizer in combination with the pure isomannide monooleate.
Abstract: A process for preparing (1-oxo-2-cyclopentyl-2-methyl-6,7-dichloro-5-indanyloxy)acetic acid comprising reacting 5-cyclopentyl-5-methyl-2-cyclopentenone with a 4-carbon conjugated (open or cyclic) diene bearing vicinal chlorines adjacent to an ether group; aromatizing the resulting adduct to yield the desired indanone.
Abstract: The new 1-alkyl-4-(10-oxo or -hydroxy-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidine compounds are prepared from the corresponding 10-desoxy compounds having a double bond at the 10,11-position by a process involving bromination, dehydrobomination of the resulting dibromo compound, followed by enamine formation and hydrolysis to give the desired 10-oxo compound. The compounds prepared in this manner are active as antihistamines and as appetite stimulants.
Abstract: Process for preparing (1-oxo-2-phenyl, halophenyl or thienyl-2-methyl-6,7-dichloro-5-indanyloxy)acetic acid, pharmaceutically acceptable salt, ester and amide derivatives thereof and intermediate 5-ether derivatives thereof comprising reacting under Friedel-Crafts conditions a 2-phenyl, halophenyl or thienyl-2-propionyl halide or an anhydride thereof with an ether derivative of 2,3-dichlorophenyl; and reacting the resulting propiophenone with formaldehyde in the presence of acid to yield the desired indanone.
Type:
Grant
Filed:
July 30, 1974
Date of Patent:
September 21, 1976
Assignee:
Merck & Co., Inc.
Inventors:
Warren K. Russ, Jr., George G. Hazen, Earl M. Chamberlin
Abstract: This invention relates to new derivatives of dibenzocycloheptenes and to processes for making them. More particularly, the invention includes 5H-dibenzo[a,d]cycloheptenes and 10,11-dihydro-5H-dibenzo[a,d]cycloheptenes which are substituted at their 5-carbon atom with an aminopropyl or an aminopropylidene radical. The amino entity may be either primary or secondary and if secondary, the substituent may be either a lower alkyl or alkenyl radical having up to 6 carbon atoms, cycloalkyl having up to 8 carbon atoms or an aralkyl radical. The dibenzocycloheptene nucleus may be further substituted. The invention also includes the intermediates used for obtaining these products. Also included are derivatives such as acyl derivatives which yield the active compound under physiological conditions.
Abstract: The new 1-alkyl-4-(1, 2, or 3-carboxy-5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidine compounds are prepared from the corresponding 1, 2 or 3-carboxy-5H-dibenzo[a,d]cyclohepten-5-one by reaction with a Grignard reagent prepared from a 1-alkyl-4-halo piperidine to form an intermediate carbinol, or a 1, 2 or 3-carboxy-5-(1-alkyl-4-piperidyl)-5H-dibenzo[a,d]cyclohepten-5-ol which is then dehydrated to produce the desired 1-alkyl-4-(1, 2 or 3-carboxy-5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidine, or alternatively by hydrolysis of a 1-alkyl-4-(1, 2 or 3-cyano-5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidine compound to form the corresponding 1-alkyl-4-(1, 2 or 3-carboxy-5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidine compound.
Abstract: A dispensing container for pellets such as capsules and pills and comprising an elongated tubular member holding the pellets in a line, the member being slit helically along its length and being resilient so that when twisted about its longitudinal axis the slit opens for dispensing a pellet.
Abstract: Sulfoxides and sulfones of the formula ##SPC1##Wherein R.sub.1 is COOH, COOR.sub.4, CH.sub.2 OH, or CH.sub.2 OR.sub.5 ; R.sub.2 is CH.sub.3 or C.sub.2 H.sub.5 ; R.sub.3 is H, F, Cl, or Br; R.sub.4 is alkyl of 1-8 carbon atoms; R.sub.5 is alkanoyl of 2-4 carbon atoms; one of the Y groups is SO or SO.sub.2 and the other Y group is CH.sub.2, O, S, SO, or SO.sub.2 ; and the physiologically acceptable salts thereof, which compounds possess anti-inflammatory activity, can be produced by converting in a compound of the formula ##SPC2##Wherein X is a group convertible into the group --CHR.sub.1 R.sub.2 wherein R.sub.1, R.sub.2, R.sub.3, and Y have the values given above, the group X into the group --CHR.sub.1 R.sub.3.
Type:
Grant
Filed:
July 31, 1974
Date of Patent:
September 21, 1976
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Joachim Gante, Hans-Adolf Kurmeier, Werner Mehrhof, Albrecht Wild
Abstract: Cyanopyridines are prepared by bringing a reactant stream comprising an alkyl substituted pyridine, ammonia, steam and oxygen into contact with a novel catalyst composition which results in high selectivity to the desired cyanopyridine.
Abstract: Hexahydro-diazepino-indoles of the formula ##SPC1##Wherein R.sup.1 is H, F, Cl, CF.sub.3, alkyl or alkoxy each of 1 to 3 carbon atoms; R.sup.2 is H, alkyl or cycloalkyl or alkenyl each of up to 6 carbon atoms, or alkyl of up to 6 carbon atoms substituted by oxo oxygen and/or amino or alkylated amino of 2 to 6 carbon atoms and/or aryl of 6 to 8 carbon atoms; and Z is 0 or (H,H), and physiologically acceptable acid addition salts thereof, possess CNS depressant activity.
Type:
Grant
Filed:
June 13, 1975
Date of Patent:
September 14, 1976
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Rochus Jonas, Helmut Muller-Calgan, Hans-Jochen Schliep
Abstract: Pyrazolidinones of the formula ##SPC1##Wherein R is a phenyl, phenoxy or a corresponding group monosubstituted or polysubstituted by one or more of F, Cl and Br possess anti-inflammatory activity.
Type:
Grant
Filed:
November 5, 1975
Date of Patent:
September 14, 1976
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Joachim Gante, Hans-Adolf Kurmeier, Erich Schacht, Werner Mehrhof, Albrecht Wild
Abstract: This invention relates to novel organic compounds and to methods for preparing them. More particularly, this invention provides new and useful cephalosporin compounds which are active antibiotics against both gram-positive and gram-negative microorganisms and compounds which are useful intermediates in the preparation of other new cephalosporin compounds.
Type:
Grant
Filed:
March 20, 1975
Date of Patent:
September 7, 1976
Assignee:
Merck & Co., Inc.
Inventors:
Raymond A. Firestone, John L. Fahey, Burton G. Christensen
Abstract: Thioformamide is prepared from hydrogen cyanide and hydrogen sulfide in an improved process employing a tertiary amino ion exchange resin as the catalyst. The process provides for nearly quantitative yields, and affords a purer, more stable product, and the elimination of polluting by-products.
Abstract: 2-Aminomethylphenol products and their non-toxic, pharmaceutically acceptable salts useful in the treatment of edema and inflammation are disclosed. The products may be prepared by treating an N-(2-hydroxybenzyl)carboxamide with an aqueous solution of an acid or a base.
Type:
Grant
Filed:
August 1, 1975
Date of Patent:
September 7, 1976
Assignee:
Merck & Co., Inc.
Inventors:
Everett M. Schultz, Edward J. Cragoe, Jr.
Abstract: A drilling fluid containing a novel heteropolysaccharide, Heteropolysaccharide S-7. A method for the drilling of oil wells, gas wells and the like which involves the circulation of the above drilling fluid within the well bore.
Abstract: Compounds of 5H dibenzo[a,d]-cycloheptenes and 10,11-dihydro-5H-dibenzo[a,d]cycloheptenes which are substituted at their 5-carbon atom with an N-cyanoaminopropyl or an N-cyanoaminopropylidene radical.