Abstract: Compounds of the formula I ##STR1## in which A and X.sup.1 have the meaning given in patent claim 1 can be prepared in a simple manner, in a one-pot process and in high yields.
Type:
Grant
Filed:
December 6, 1989
Date of Patent:
December 24, 1991
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Richard Kirchlechner, Michael Casutt, Arno Basedow
Abstract: The present invention includes N-hydroxyamide, N-hydroxyurea, N-hydroxythioamide, and N-hydroxythiourea derivatives of fenamates, indomethacin, cicloprofen, oxepinac, and indoprofen as dual inhibitors or selective ihibitors of cyclooxygenase and 5-lipoxygenase.
Type:
Grant
Filed:
October 16, 1990
Date of Patent:
December 24, 1991
Assignee:
Warner-Lambert Co.
Inventors:
Thomas R. Belliotti, Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Catherine R. Kostlan, James B. Kramer, Jagadish C. Sircar
Abstract: A process for the preparation of compounds of formula I ##STR1## in which X is the radical OH or Cl, by the catalytic hydrogenation of 3,5-dimethyl-4-methoxy-2-cyanopyridine, subsequent reaction of the resulting 3,5-dimethyl-4-methoxy-2-aminomethylpyridine to give 3,5-dimethyl-4-methoxy-2-hydroxymethylpyridine and, if desired, chlorination to give 3,5-dimethyl-4-methoxy-2-chloromethylpyridine, and the novel intermediate 3,5-dimethyl-4-methoxy-2-aminomethylpyridine.
Abstract: The present invention provides polycarboxylic acid imidazolines of the general formula: ##STR1## wherein X is --Cl, --OH, --O--SO.sub.3 H, --O--PO.sub.3 H.sub.2, --O--CH.sub.2 --CH.sub.2 --COOH, --NH.sub.2, --NHalk or --N(alk).sub.2, alk being an alkyl radical containing up to 6 carbon atoms, n is a whole number of from 2 to 4, R is a C.sub.8 -C.sub.18 hydrocarbon radical which is straight-chained, branched, saturated or one to three times unsaturated, m is a whole number of from 2 to 5, R' is a hydrogen atom or a carboxyl group and R" is a hydrogen atom or a methyl radical. The present invention also provides a process for the preparation of these compounds and cleaning agents containing them.
Type:
Grant
Filed:
June 8, 1990
Date of Patent:
September 17, 1991
Assignees:
Chemisches Instutut Schaefer AG, Joh. A. Benskiser GmbH
Inventors:
Hans Hitz, Rolf Schaefer, Heinrich Baust, Wolfgang Gross
Abstract: The invention relates to N-substituted imidazoles, processes for their production as well as their use in pharmaceutical agents. The compounds according to the invention have aromatase-inhibiting properties.
Type:
Grant
Filed:
March 31, 1989
Date of Patent:
September 3, 1991
Assignee:
Schering Aktiengesellschaft
Inventors:
Peter Strehlke, Rolf Bohlmann, David Henderson, Yukishige Nishino
Abstract: 3-7-Diheterabicylo[3.3.1]nonanes and derivatives thereof are disclosed. Their method of preparation and use as antiarrhythmic agents is given.
Type:
Grant
Filed:
November 15, 1990
Date of Patent:
August 27, 1991
Assignee:
Oklahoma State University
Inventors:
Kenneth D. Berlin, Mark D. Thompson, Benjamin J. Scherlag, Gary S. Smith
Abstract: Novel hydrazinocarbonyloxylabdanes, intermediates and processes for the preparation thereof, and a method for treating cardiac failure utilizing compounds or compositions thereof are disclosed.
Type:
Grant
Filed:
August 30, 1989
Date of Patent:
August 20, 1991
Assignee:
Hoechst-Roussel Pharmaceuticals Inc.
Inventors:
Raymond W. Kosley, Jr., Gerard J. O'Malley
Abstract: The invention relates to the products of formula ##STR1## in which R represents the radical ##STR2## in which R.sub.1 at any position on the benzene ring represents linear, branched or cyclic alkyl, alkenyl or alkynyl containing up to 8 carbon atoms, or the radical ##STR3## in which R.sub.2 and R.sub.3, which may be identical or different, represents hydrogen or linear alkyl, alkenyl or alkynyl containing up to 8 carbon atoms or form, together with the nitrogen atom to which they are attached, a carbonaceous heterocyclic radical optionally containing another hetero atom, or the radical OR', R' representing hydrogen, a linear, branched or cyclic alkyl containing up to 8 carbon atoms or aryl containing up to 14 carbon atoms, or the radical SR.sub.4 or S(O)R.sub.5, R.sub.4 and R.sub.5 representing linear, branched or cyclic alkyl, alkenyl, or alkynyl containing up to 8 carbon atoms, or R represents naphthyl optionally substituted with the radical R'.sub.1, R'.sub.1 being as defined above for R.sub.
Type:
Grant
Filed:
February 21, 1990
Date of Patent:
August 20, 1991
Assignee:
Roussel Uclaf
Inventors:
Emilio Toja, Fernando Barzaghi, Giulio Galliani
Abstract: A method for providing enhanced antiviral activity with N-alkyl derivatives of 1,5-dideoxy-1,5-imino-D-glucitol is disclosed which comprises selectively increasing the alkyl chain length to at least 5 carbon atoms and up to about 10 carbon atoms to thereby improve the spectrum of enzyme inhibitory activity and the in vivo half life.
Abstract: The invention relates to indole derivatives of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl or phenylC.sub.1-3 alkyl;R.sup.2 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-7 cycloalkyl, phenyl or phenylC.sub.1-3 alkyl;X represents an oxygen atom or the group NR.sup.3 (where R.sup.3 represents a hydrogen atom or a C.sub.1-6 alkyl group);one of the groups represented by R.sup.4, R.sup.5 and R.sup.6 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;Q represents a hydrogen or a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenylC.sub.
Type:
Grant
Filed:
June 15, 1989
Date of Patent:
June 25, 1991
Assignee:
Glaxo Group Limited
Inventors:
Alexander W. Oxford, Peter C. North, David J. Cavalla
Abstract: Herein disclosed is a method of treating convulsions with a pharmaceutical composition containing a compound of the formula:(HO).sub.p --A--[OSO.sub.2 NR.sup.1 R.sup.2 ].sub.zwhere A is an aryl, arylalkyl, or aryloxyalkyl group and is substituted on 1 or more carbon atoms with a sulfamate group (--OSO.sub.2 NR.sup.1 R.sup.2) wherein R.sup.1 and R.sup.2, same or different, are hydrogen or loweralkyl wherein p is 0 or 1 and is the number of untreated hydroxyl groups and z is 1 or 2 and is the number of --OS(O.sub.2)NR.sup.1 R.sup.2 groups. Aryl is selected from phenyl, substituted phenyl, pyridinyl, naphthyl, quinolinyl, and the like. Phenyl substituents are selected from hydrogen, halo, hydroxy, phenyl, phenoxy, benzoyl, loweralkyl, loweralkoxy, carboxy, amino, loweralkylamino, diloweralkylamino, acetamido, cyano, nitro, loweralkoxycarboyl, aminosulfonyl, imidazolyl, triazolyl, and the like. Novel compounds not previously disclosed are also described.
Type:
Grant
Filed:
November 30, 1989
Date of Patent:
June 18, 1991
Assignee:
A. H. Robins Co., Inc.
Inventors:
Young S. Lo, David A. Walsh, Ibrahim M. Uwaydah
Abstract: Disclosed are the compounds of formula ##STR1## wherein A represents lower alkylene; B represents oxygen, sulfur, lower alkylene, lower alkylene interrupted by oxygen, sulfur, sulfinyl or sulfonyl, (oxy-, sulfinyl-, sulfonyl- or thio)-lower alkylene, lower alkenylene, phenylene or a direct bond; M represents lower alkylene, lower alkylene interrupted by oxygen, sulfur, sulfinyl or sulfonyl, (oxy-, sulfinyl, sulfonyl- or thio)-lower alkylene, lower alkenylene or a direct bond; or one of A, B and M represents lower alkylidenylene and the other two independently represent lower alkylene; R represents hydrogen unless A, B or M represents lower alkylidenylene in which case R represents the second bond to the adjacent aklylidenylene unsaturated carbon atom; Het represents 1-imidazolyl, 3-pyridyl, or 1-imidazolyl or 3-pyridyl substituted by lower alkyl; Ar represents carbocyclic or heterocyclic aryl; pharmaceutically acceptable ester and amide derivatives thereof; the N-oxides of said compounds wherein Het represent
Type:
Grant
Filed:
May 23, 1990
Date of Patent:
June 18, 1991
Assignee:
Ciba-Geigy Corporation
Inventors:
Shripad S. Bhagwat, Alan J. Main, Herman R. Rodriguez
Abstract: The present invention is directed to the preparation of benzimidazole derivatives of the formula (I), ##STR1## wherein A=stands for S, SO or SO.sub.2,R.sup.1 =stands for C.sub.1-4 alkyl group,R.sup.2 =stands for C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl or C.sub.6-10 aryl or aralkyl,comprising reacting a sulphochloride of the formula (II) ##STR2## with an alkyl aluminum compound of the formula (III).R.sub.n.sup.2 AlClhd (3-n) (III)The reaction is performed in one step.
Type:
Grant
Filed:
January 19, 1990
Date of Patent:
June 11, 1991
Assignee:
Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
Inventors:
Ferenc Sperber, Csaba Huszar, Attila Nemeth, Eva Somfai, Iren Pali nee Ivanics
Abstract: Novel imidazopyridine derivatives of formula: ##STR1## wherein, R represents an alkoxyalky radical having 4-6 carbon atoms or a benzyl radical optionally substituted by a halogen atom, an alkyl or alkoxy radical having up to 3 carbon atoms,X represents hydrogen or an alkyl radical having up to 3 carbon atoms,n represents 0 or 1m represents an integer of from 2 to 5 inclusive,R.sub.1 and R.sub.2 may be the same or different and represent a saturated or unsaturated alkyl radical containing up to 4 carbon atoms or they, taken together with the adjacent nitrogen atom, may form a pyrrolidine, piperazine or homopiperazine ring which may be optionally substituted by an alkyl radical containing up to 3 carbon atoms, provided that when n is zero also m is zero and --N(R.sub.1)R.sub.2 represents the above defined piperazine or homopiperazine ring.The compounds (I) have an antihistaminic activity.
Type:
Grant
Filed:
May 7, 1990
Date of Patent:
June 11, 1991
Assignee:
Dompe Farmaceutici S.p.A.
Inventors:
Giani Roberto, Parini Ettore, Borsa Massimiliano, Lavezzo Antonio
Abstract: A Reissert compound of bisbenzimidazole can be formed by first reacting benzimidazole with an aliphatic diacid chloride to form bisbenzimidazole and then reacting the bisbenzimidazole with an aliphatic acid chloride and cyanide to form the Reissert compound thereof.
Type:
Grant
Filed:
September 21, 1990
Date of Patent:
June 4, 1991
Assignee:
Virginia Tech Intellectual Properties, Inc.
Inventors:
Harry V. Gibson, Yajnanarayana H. R. Jois
Abstract: The present invention provides compounds of the general formula (I) which inhibit the aggregation of erythrocytes or thrombocytes ##STR1## wherein A is hydrogen or C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, benzyl or C.sub.3 -C.sub.7 -cycloalkyl radical, B is hydrogen, R.sub.1 is a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.3 -C.sub.7 -cycloalkyl radical, R.sub.2 is a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.1 -C.sub.6 -alkylcarbonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, aminocarbonyl or hydrazinocarbonyl radical, or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a C.sub.3 -C.sub.7 -cycloalkyl ring, n is 0, X is a valency bond or a C.sub.1 -C.sub.6 -alkylene radical, R.sub.3 is a carbocyclic aromatic ring, which may be substituted; and the tautomers, optically-active forms and physiologically acceptable salts thereof with organic and inorganic acids.
Type:
Grant
Filed:
June 5, 1989
Date of Patent:
May 28, 1991
Assignee:
Boehringer Mannheim GmbH
Inventors:
Wolfgang V. Von Der Saal, Alfred Mertens, Erwin Boehm