Abstract: Novel benzoic acid or benzoic acid ester derivatives, pharmaceutical compositions and methods of use thereof are the present invention. Utility is for the treatment of arthritis, asthma, Raynaud's disease, inflammatory bowel disorders, trigeminal or herpetic neuralgia, inflammatory eye disorders, psoriasis, dental pain, and headaches, particularly vascular headaches, such as migraine, cluster, mixed vascular syndromes, as well as nonvascular, tension headaches.
Abstract: A novel pyrrolizidine derivative of the formula, ##STR1## which has potent antiarrhythmic activity and low toxicity is produced. The derivative can be synthesized: by acylating 2,6-xylidine to protect the amino group, nitrating the protected xylidine to introduce a nitro group at 3-position, reducing the nitro group to an amino group, followed by diazotizing and hydrolyzing, and then the resulted 3-hydroxy-2,6-dimethylaniline being condensed with 8-halocarbonylmethylpyrrolizidine; or by nitrating N-(2',6'-dimethyl)phenyl-8-pyrrolizidineacetamide to introduce a nitro group at 3'-position, reducing the nitro group to amino group, diazotizing the amino group and hydrolyzing the diazonium compound.
Abstract: Novel 2,3,4,5-tetrahydro-1H-3-benzazepines which in the 5-position have furyl, thienyl, pyridyl, or ring systems consisting of phenyl ortho condensed with a benzen, cyclohexan, cyclohexen, cyclopentan or cyclopenten ring wherein one of the carbon atoms may be exchanged with oxygen, sulphur or nitrogen, have interesting central nervous system and cardiovascular effects.
Type:
Grant
Filed:
April 21, 1986
Date of Patent:
June 14, 1988
Assignee:
Novo Industri A/S
Inventors:
Claus Braestrup, Peter H. Andersen, Poul Borrevang, Frederik C. Gr nvald, Louis B. Hansen, Rolf Hohlweg
Abstract: Novel 8-thiotetrahydroquinolines of the formula ##STR1## wherein X is selected from the group consisting of ##STR2## Alk is alkyl of 1 to 6 carbon atoms, R.sub.1 and R.sub.2 are Alk individually selected from the group consisting of hydrogen and aryl or taken together with the carbon atoms to which they are attached form a phenyl optionally substituted with at least one member of the group consisting of alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, halogen, ##STR3## and Alk' is alkyl of 1 to 6 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having antiallergic activity and their preparation.
Type:
Grant
Filed:
February 26, 1986
Date of Patent:
June 14, 1988
Assignee:
Roussel Uclaf
Inventors:
Stephen Clements-Jewery, Peter D. Kennewell, Robert Westwood
Abstract: There are used for the protection of cultivated plants against the harmful effects of agricultural chemicals quinoline derivatives of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 independently of one another are each hydrogen, halogen, nitro, cyano, alkyl, alkoxy or acyl,R.sub.4, R.sub.5 and R.sub.
Abstract: The present invention is for compounds having the formula of N-1H-tetrazol-5-yl-2-thiophenecarboxamides, N-1H-tetrazol-5-yl-2-pyrrolecarboxamides, N-1H-tetrazol-5-yl-2-furancarboxamides or analogs of each of the carboxamides. The compounds are useful for the treatment of allergic or inflammatory conditions or diseases. Thus, pharmaceutical compositions and methods of use are also the invention. Processes of preparation for the compounds are also the invention.
Type:
Grant
Filed:
March 18, 1987
Date of Patent:
May 31, 1988
Assignee:
Warner-Lambert Company
Inventors:
Wiaczeslaw A. Cetenko, David T. Connor, Michael D. Mullican, Roderick J. Sorenson
Abstract: Process for producing 2,2,4-trimethyl-1,2-dihydroquinoline by reacting aniline with an acetone compound at 80.degree.-150.degree. C. in the presence of, as catalyst, both hydrogen fluoride and boron trifluoride.
Abstract: A new catalytic process for the isomerization of asocainol isomers at the 6-position which provides an inexpensive, rapid, and simple method for large scale production of the (R,R) isomer of (R,S) asocainol is asocainol. The (R,R) isomer of (R,S) asocainol is treated with small amounts of a salt and an oxidizing agent at an elevated temperature. The compounds and their pharmaceutically acceptable salts are useful as potent antiarrhythmic agents and local anesthetics.
Abstract: There are described the novel compound bis-(trimethaphan)-nitroprusside of formula ##STR1## and solvates, especially hydrates or alcoholates thereof, as well as a process for the manufacture thereof from an alkali nitroprusside and a soluble trimethaphan salt, especially sodium nitroprusside and trimethaphan camsylate, in solution, especially in water.Furthermore, there are described pharmaceutical compositions which contain the novel active substance (I) in solid form, in form of concentrated solutions or in form of diluted solutions suitable for infusion purposes.In particular there are described compositions which contain (I) in concentrated solution in at least 40% ethanol or in solid form as well as compositions which contain, in addition to (I), a soluble, physiologically acceptable thiosulphate, in particular sodium thiosulphate.
Abstract: There are described compounds of the formula ##STR1## in which R.sup.1 is hydrogen or C.sub.1-6 alkyl, R.sup.2 is hydrogen, C.sub.1-6 alkyl or C.sub.3-6 alkenyl, X and Y are each oxygen, sulphur, sulphinyl or sulphonyl, n is 2 to 6 and Z is 1H-tetrazol-5-yl, 1H-tetrazol-5-ylthio, 1H-tetrazol-5-ylsulphinyl, 1H-tetrazol-5-ylsulphonyl, cyano or thiocyano, provided that when both X and Y are oxygen Z is 1H-tetrazol-5-ylthio, 1H-tetrazol-5-ylsulphinyl, 1H-tetrazol-5-ylsulphonyl or thiocyano; and salts thereof. The compounds in which Z is other than cyano or thiocyano have pharmaceutical activity and inhibit leukotriene action or formation.
Type:
Grant
Filed:
May 27, 1986
Date of Patent:
April 26, 1988
Assignee:
Lilly Industries Limited
Inventors:
John Goldsworthy, Winston S. Marshall, John P. Verge
Abstract: (1H-Tetrazol-5-yl)-2(1H)-quinolones useful as antiallergic agents are described herein. The compounds are prepared by the reaction of sodium azide and ammonium chloride with an appropriate 3-cyano-2(1H)-quinolinone.
Abstract: The disclosure herein pertains to 2-haloacetamides characterized by substitution on the nitrogen atom of certain heterocyclymethyl radicals and by substituted or unsubstituted cycloalkenyl or phenyl radicals and to a process for the preparation thereof. These compounds are useful as herbicides.
Abstract: A chromene derivative having the general formula (I): ##STR1## wherein n is 1 to 5 and --O--CH.sub.2).sub.n CO.sub.2 H group is attached to 5-position, 6-position, 7-position or 8-position, or salts thereof, a process for preparing the same and antiallergic agents containing the same.The compounds of the present invention inhibit the immunological release of chemical mediators such as SRS-A and histamine from mast cell and have an excellent effect in preventing and treating the various allergic diseases such as allergic asthma, allergic dermatitis, allergic nasitis, hives, allergic enteritis and allergic conjunctivitis, especially allergic asthma.
Abstract: 3,7-Dichloroquinoline derivatives which are substituted in the 8-position by --CH.dbd.CHR or --CH.dbd.NR.sup.5, and their use for controlling undesirable plant growth.
Type:
Grant
Filed:
August 3, 1983
Date of Patent:
January 5, 1988
Assignee:
BASF Aktiengesellschaft
Inventors:
Helmut Hagen, Rolf-Dieter Kohler, Juergen Markert, Bruno Wuerzer
Abstract: Phosphorus containing compounds of the formula ##STR1## wherein X is a substituted or unsubstituted imino or amino acid and A is ##STR2## These compounds possess angiotensin converting enzyme activity and are thus useful as hypertensive agents.
Type:
Grant
Filed:
January 25, 1985
Date of Patent:
December 29, 1987
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Donald S. Karanewsky, Edward W. Petrillo, Jr.
Abstract: Quinoline derivatives of the formula ##STR1## where X, n, R.sup.1, R.sup.2 and Y have the meanings given in the description, are used for controlling undesirable plant growth.
Type:
Grant
Filed:
September 7, 1983
Date of Patent:
December 29, 1987
Assignee:
BASF Aktiengesellschaft
Inventors:
Helmut Hagen, Rolf-Dieter Kohler, Jurgen Markert, Bruno Wuerzer
Abstract: N-(2,10-dioxa-tricyclo-[5,3,1,0.sup.3,8 ]-undecane-5-yl)-tryptamine compounds corresponding to the formula ##STR1## with blood-pressure lowering effects, a method of producing such compounds and pharmaceutical compositions incorporating such compounds, wherein R.sub.1 is hydrogen, a benzyl or lower alkyl group; R.sub.2 is a lower alkyl or lower alkanoyl group; R.sub.3 is hydrogen or a lower alkyl group; R.sub.4 is hydrogen, benzyloxy, hydroxy or a lower alkoxy group; R.sub.5 is hydrogen, benzyloxy, hydroxy or a lower alkoxy group; and A and B either are both hydrogen or together represent a bond between their respective carbons.
Type:
Grant
Filed:
September 24, 1984
Date of Patent:
December 22, 1987
Assignee:
Kali-Chemie Pharma GmbH
Inventors:
Peter W. Thies, Samuel David, Ulrich Kuehl, Gerd Buschmann, Peter Flecker
Abstract: The invention relates to derivatives of cis,endo-2-azabicyclo[5.3.0]decane-3-carboxylic acid of the formula I ##STR1## in which R denotes hydrogen, alkyl, alkenyl or aralkyl, R.sup.1 denotes hydrogen, allyl, vinyl or a side chain of an optionally protected naturally occurring .alpha.-aminoacid, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen, or Y and Z together denote oxygen, X denotes alkyl, alkenyl, cycloalkyl, aryl which can be substituted once, twice or three times by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, and their physiologically acceptable salts, a process for their preparation, agents containing them and their use.
Abstract: The present invention provides a process for the preparation of herbicidal 2-(4,4-disubstituted-5-oxo-2-imidazolin-2-yl) benzoic, nicotinic and quinoline-3-carboxylic acids, esters and salts.
Type:
Grant
Filed:
June 13, 1985
Date of Patent:
November 24, 1987
Assignee:
American Cyanamid Company
Inventors:
Marinus Los, Don W. Long, Gregory P. Withers
Abstract: A soil disease controlling agent for preventing and controlling diseases caused by pathogenic fungi living in soil, which comprises an effective amount of at least one of a 2-cycloalkenylamine derivative and its salts as an active ingredient, and at least one inert carrier or diluent.