Abstract: The novel compounds of formula I and salts thereof have a very powerful anti-depressive activity which for a considerable part, and in some substances even entirely, is based on serotonine potentiation. Moncamino oxidase inhibition does not contribute to the anti-depressive effect. The substances are little toxic and substantially free from side effects.The compounds can be synthesized and processed to compositions according to known methods.
Type:
Grant
Filed:
December 12, 1977
Date of Patent:
March 11, 1980
Assignee:
U.S. Philips Corporation
Inventors:
Hendricus B. A. Welle, Volkert Claassen
Abstract: m-Halobenzoyl halides are prepared by chlorinating or brominating benzoyl chloride or benzoyl bromide in the absence of a solvent and in the presence of FeCl.sub.3 or FeBr.sub.3 as the catalyst and of sulfur and/or at least one inorganic and/or organic sulfur compound as the cocatalyst, at a temperature of from about 0.degree. to 90.degree. C. The compounds are valuable starting products and intermediates for the manufacture of dyestuffs, pharmaceuticals and plant protectives.
Abstract: Penicillins of the formula ##STR1## wherein R is hydrogen , sodium, potassium or certain ester groups; R.sub.1 is in the .alpha.-configuration and is hydrogen or methoxy; R.sub.2 is hydrogen, lower aklkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, substituted or unsubstituted phenyl, benzyl, phenethyl, thienyl, furyl, or pyridyl, or 2-amino-4-thiazolyl; R.sub.3 is lower alkyl or substituted or unsubstituted phenyl, benzyl, phenethyl, thienyl or furyl; and R.sub.4 is hydrogen or lower alkyl; are disclosed. These compounds possess useful antibacterial activity.
Abstract: Novel .alpha.-haloethylcarbamyl halides and a process for their manufacture by reacting vinyl isocyanate with a hydrogen halide.The .alpha.-haloethylcarbamyl halides, especially .alpha.-chloroethylcarbamyl chloride, prepared by the process of the invention, are valuable starting materials for the manufacture of surface-coating raw materials, textile coatings, dyes, drugs and crop protection agents.
Abstract: Fluorine-substituted vitamin D compounds, methods for preparation of such compounds and fluorinated intermediate compounds used in such methods are disclosed. The fluorine-substituted vitamin D compounds are characterized by vitamin D-like activity in stimulating intestinal calcium transport and bone mobilization and in promoting the calcification of rachitic bone.
Type:
Grant
Filed:
July 26, 1978
Date of Patent:
February 12, 1980
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Hector F. DeLuca, Heinrich K. Schnoes, Joseph L. Napoli, Jr., Bruce L. Onisko
Abstract: Acylamino heteroaryl compounds in which the heteroaryl nucleus is a 5-membered ring containing a single heteroatom, which may be oxygen, or sulphur, methods of making the compounds and pharmaceutical formulations containing the compounds. The compounds have anti-allergy activity.
Type:
Grant
Filed:
January 19, 1978
Date of Patent:
February 5, 1980
Assignee:
Lilly Industries Limited
Inventors:
Delme Evans, Michael R. J. Jolley, William J. Ross, Brian P. Swann
Abstract: There is disclosed a process for preparing methoxymethyl 6-aminopenicillanate, its conversion to methoxymethyl amoxicillin and the use of the latter compound as an intermediate in the preparation of the methoxymethyl ester of p-hydroxyhetacillin which is the preferred product of this invention.
Abstract: The present invention provides novel biguanide compounds for use as agricultural fungicides. The compounds are 1-(alkoxyphenyl)-5-(substituted phenyl) biguanides having the formula: ##STR1## where R is alkyl C.sub.4 -C.sub.14,R' is hydrogen or alkyl C.sub.1 -C.sub.5,X is halo, nitro, cyano, trihalomethyl, alkyl C.sub.1 -C.sub.8, alkoxy C.sub.1 -C.sub.8, phenoxy, alkoxycarbonyl C.sub.2 -C.sub.4 or acyl C.sub.1 -C.sub.4, and,n is 1 or 2, and acid addition salts thereof.The invention further relates to a composition and method for controlling pathogenic fungi with a fungicidally effective amount of said compound.
Type:
Grant
Filed:
September 26, 1978
Date of Patent:
January 15, 1980
Assignee:
GAF Corporation
Inventors:
Michael J. Brown, Bruce M. Resnick, James H. R. Woodland
Abstract: Novel N'-(substituted phenyl)-N-(2-(halophenoxy)ethyl)alkylanimidamides are disclosed. Their method of use in the control and kill of bacteria and fungi, and compositions containing the novel compounds as the active ingredients therein are claimed.
Abstract: A process for preparing semi-synthetic penicillin antibiotics, especially ampicillin, is disclosed which comprises acylating a silylated 6-aminopenicillanic acid in the presence of primary or secondary carboxamide bases as hydrogen halide acceptors. The products may be obtained in good yield and high purity and the amount of toxic contaminants in the products is significantly reduced, thus substantially eliminating unpleasant side-effects.
Abstract: The present invention relates to hitherto unknown esters of the below formula I, to salts of the esters of formula I with pharmaceutically acceptable acids, to methods for producing said new compounds, to pharmaceutical compositions containing said new compounds, and to methods of treating patients suffering from infectious diseases using said new compounds.The compounds of the invention, which are valuable in the human and veterinary practice, have the formula I ##STR1## in which R.sub.1 and R.sub.
Abstract: .omega.-Iodoperfluoroalkylene oxide acyl fluorides are prepared by reacting a perfluoroalkylene oxide .alpha.,.omega.-diiodide with fuming sulfuric acid in the presence of zinc sulfate. The iodoacyl fluorides are intermediates for use in synthesizing perfluoroalkylene ether diimidate esters.
Type:
Grant
Filed:
October 24, 1978
Date of Patent:
January 1, 1980
Assignee:
The United States of America as represented by the Secretary of the Air Force
Abstract: A process for preparing semi-synthetic penicillin antibiotics, especially ampicillin, is disclosed which comprises silylating 6-aminopenicillanic acid using a silylating agent which generates a primary or secondary carboxamide base, and then acylating the silylated 6-aminopenicillanic acid in situ using the primary or secondary carboxamide base as hydrogen halide acceptor. No further base needs to be added, and the products may be obtained in good yield and high purity with the amount of toxic contaminants in the products significantly reduced. Unpleasant side-effects may thus be substantially eliminated.
Abstract: Symmetrical perfluoroalkylene oxide .alpha.,.omega.-diacyl fluoride is prepared by reacting a perfluoroalkylene oxide, .alpha., .omega.-diiodide with fuming sulfuric acid in the presence of zinc sulfate while adding chlorine.
Type:
Grant
Filed:
September 15, 1978
Date of Patent:
January 1, 1980
Assignee:
The United States of America as represented by the Secretary of the Air Force
Abstract: A method for preparing thienylacetic acid and its derivatives is disclosed, wherein a glyoxylic ester is made to react with hydrazine, and after with potash. Advantageously, the glyoxylic ester is prepared by condensation of a monoester monochloride of oxalic acid upon a thiophenic derivative, in the presence of titanium chloride.The so obtained products are useful as organic synthesis intermediaries for various products of pharmaceutical type.
Type:
Grant
Filed:
January 12, 1978
Date of Patent:
December 25, 1979
Assignee:
Produits Chimiques Auxiliaires et de Synthese, P.C.A.S.
Abstract: New N-fluoromethyl-carbamic acid fluorides and a new process for their manufacture by reacting N-halomethyl-carbamic acid halides with metal fluorides. The products are starting materials for the manufacture of drugs, dyes, pesticides, plastics, plastics auxiliaries and textile auxiliaries.
Type:
Grant
Filed:
January 13, 1978
Date of Patent:
December 18, 1979
Assignee:
BASF Aktiengesellschaft
Inventors:
Sabine Thym, Karl-Heinz Koenig, Gerhard Hamprecht
Abstract: Certain novel 6-acylamino-2,2-dimethyl-3-(5-tetrazolyl)penam derivatives, and salts thereof; their use as broad-spectrum antibacterial agents; and methods for their preparation. Their preparation comprises acylation of the novel intermediate, 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam or simple derivatives thereof, followed, in some cases, by further transformations of the 6-acylamino group or by removal of a protecting group from the 5-tetrazolyl moiety. Process for the preparation of 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam, simple derivatives thereof and intermediates therefor.