Abstract: The invention relates to cyclic urea derivatives of general formula ##STR1## wherein R.sub.a, R.sub.b, X and Y are as defined herein, pharmaceutical compositions containing the derivatives and processes for preparing them.
Type:
Grant
Filed:
August 29, 1995
Date of Patent:
July 22, 1997
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Guenter Linz, Thomas Mueller, Johannes Weisenberger, Wolfgang Eisert
Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.
Type:
Grant
Filed:
December 29, 1994
Date of Patent:
July 15, 1997
Assignee:
Allergan
Inventors:
Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
Abstract: Substituted 1,2,3,4-tetrahydrocarbazoles of the formula ##STR1## having the meaning for R.sup.1 to R.sup.8 indicated in the description, can be prepared by catalytically hydrogenating a substituted phenol of the formula ##STR2## reacting the hydrogenation solution with a phenylhydrazine of the formula ##STR3## to give the hydrazone and cyclizing the hydrazone under acidic conditions.
Type:
Grant
Filed:
February 29, 1996
Date of Patent:
July 15, 1997
Assignee:
Bayer Aktiengesellschaft
Inventors:
Heinz Landscheidt, Alexander Klausener, Eberhard Zirngiebl, Jorg-Dietrich Jentsch
Abstract: Compounds of use in therapy and having the formula: ##STR1## in which R.sub.2 and R.sub.3 independently denote H, C.sub.1 -C.sub.4 alkoxy or OH and (A, B)=(oxygen, oxygen) in which case one out of R and R.sub.1 denotes OH, halogen, secondary amino or tertiary amine and the other denotes NHCOR.sub.4, NHNHCOR.sub.5 or NHNHCOCONH.sub.2, or R and R.sub.1 together form .dbd.N--NH--CO--R'.sub.5, .dbd.N--NH--CO--CO--NH.sub.2, (.dbd.N--NH--R.sub.6, .dbd.N--R.sub.7, .dbd.N--O--CO--R.sub.8 or .dbd.C(CH.sub.3)--NH--NH--CO--R.sub.9 ; or (A, B) .dbd.(N--NH--CX--NHR.sub.10, oxygen) in which case R and R.sub.1 together form .dbd.N--OH.
Type:
Grant
Filed:
March 24, 1994
Date of Patent:
July 15, 1997
Assignee:
Innothera
Inventors:
Michel P. Cugnon de Sevricourt, Catherine G. Dacquet, Michel A. Finet, Florence J. Le Marquer, Max F. Robba, Norbert O. Tembo, Sylvie J. Yannic-Arnoult, Jean-Luc Torregrosa
Abstract: D-2-Alkyl Tryptophan compounds for incorporation into various peptides during manufacture thereof or for substitution for D-Tryptophan residues in such peptides to provide a D-2-alkyl Tryptophan residue therein which enhances the stability and biological activity of the peptide.
Abstract: Disclosed is a novel blowing agent of tetrazoles and their derivatives. The blowing agent comprising tetrazole derivatives is harmless, odorless and inexpensive. Moreover, the agent is low in physical sensitivities and safe in use, and generates clean gas by being sharply decomposed only due to temperature. The blowing agent of tetrazoles and their derivatives employs aminotetrazole derivatives represented by the general formula (1). The blowing agent offers foaming agents for resin molded bodies having good thermal properties, inflators for air bags serving as automobile safety protection, or smoking agents for diffusing chemicals by a low-cost inexpensive synthetic process.
Abstract: The invention relates to tricyclic pyrrole derivatives useful as 5-HT selective agents of the formula ##STR1## wherein R.sup.1 to R.sup.4 are, independently, hydrogen, halogen, lower alkyl, phenyl, cycloalkyl or lower alkoxy and R.sup.2 additionally is lower alkoxycarbonyl, acyloxy or mesyloxy;R.sup.5 to R.sup.7 are, independently, hydrogen or lower alkyl;X is --CH.sub.2 CH(C.sub.6 H.sub.5)--, --CH.dbd.C(C.sub.6 H.sub.5)--, --YCH.sub.2 --, --CH.dbd.CH-- or --(CR.sup.11 R.sup.12).sub.n ;R.sup.11 and R.sup.12 are, independently, hydrogen, phenyl, lower alkyl or halogen;n is 1 to 3 andy is O or S,as well as pharmaceutically acceptable salts of basic compounds of formula I with pharmaceutically acceptable acids.
Type:
Grant
Filed:
February 21, 1996
Date of Patent:
July 8, 1997
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Michael Bos, Jurgen Wichmann, Ulrich Widmer
Abstract: The new dyestuffs of the formula (I) ##STR1## wherein the substituents R and R.sup.1 and the index n have the meaning given in the description, are outstandingly suitable for dyeing and printing cellulose-containing materials, in particular for the preparation of recording liquids for ink jet recording systems.
Type:
Grant
Filed:
November 18, 1994
Date of Patent:
July 8, 1997
Assignee:
Bayer Aktiengesellschaft
Inventors:
Karin Hassenruck, Karl-Heinz Reinhardt, Peter Wild, Klaus Wunderlich
Abstract: Compounds of the formula ##STR1## wherein the substituents are as defined herein, are disclosed. Pharmaceutical compositions and methods of treating allergic and inflammatory diseases are also taught.
Abstract: A description is given of tachyquinine antagonists having general formula (I) ##STR1## their preparation and use in pharmaceutical formulations.
Abstract: Novel butadiene derivatives of the formula [I]: ##STR1## wherein Ring A is tri-lower alkoxyphenyl, R.sup.1 and R.sup.2 combine each other to form a group of the formula: ##STR2## or one of R.sup.1 and R.sup.2 is lower alkoxy, and the other is group of the formula: -NHR.sup.3, in which R.sup.3 is hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted amino, hydroxy or pyridylcarbonyl, or salts thereof, these compounds have excellent antithrombotic activity and are useful as antithrombotic drug, or synthetic intermediate for preparing other antithrombotic drug.
Abstract: A compound of formula (I) and pharmaceutically acceptable salts thereof, where Z is R.sub.3 and X and Y form (a), or X is R.sub.3 and Y and Z form (a) or (b); R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, --CH.sub.2 --C.sub.3-7 cycloalkyl, phenyl (optionally substituted with halogen or C.sub.1-6 alkyl), -thiophenyl (optionally substituted with halogen or C.sub.1-6 alkyl), or C.sub.1-6 alkyl phenyl; R.sub.3 are independently hydrogen, halogen, --O--C.sub.1-6 alkyl or C.sub.1-6 alkyl; R.sub.4 is a valence bond, CH.sub.2 or oxygen; R.sub.5 and R.sub.6 are independently hydrogen, sulfur, --S--C.sub.1-6 alkyl, halogen, CON(R.sub.3).sub.2, --COCF.sub.3, --CO--C.sub.1-6 alkyl, --CO phenyl, oxygen, --CHO, CN except that when Y and Z form (b), R.sub.1 and R.sub.2 are hydrogen or a C.sub.1-6 alkyl and R.sub.3 is hydrogen, then at least one of R.sub.5 and R.sub.6 must be other than hydrogen.
Type:
Grant
Filed:
September 7, 1995
Date of Patent:
June 17, 1997
Assignee:
Pharmacia & Upjohn Company
Inventors:
Bengt R. Andersson, Per A. E. Carlsson, Lars O. Hansson, Clas A. Sonesson, N. Peter Stjernlof, Kjell A. I. Svensson, R. Nicholas Waters, Susanne R. Haadsma-Svensson
Abstract: The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof.
Abstract: A compound of structure (I), in which A.sup.1 is O, S(O).sub.n in which n is 0, 1 or 2, NR, CH.sub.2, or CH(OH); A.sup.2 is a bond or CH.sub.2 ; or A.sup.1 A.sup.2 is CH.dbd.CH; R is hydrogen or C.sub.1-4 alkyl; R.sup.1 is an optionally substituted 6- to 10-membered aryl or heteroaryl ring; suitably R.sup.1 is an optionally substituted 6- 10-membered aryl ring such as phenyl or naphthyl; suitably R.sup.1 is optionally substituted 6- to 10-membered heteroaryl ring, containing from 1 to 4 nitrogen atoms; R.sup.2 is hydrogen, halogen, C.sub.1-4 alkyl, CN, NO.sub.2 or CF.sub.3 ; R.sup.3 is C(R.sup.4)(R.sup.5)CH.sub.2 NR.sup.6 R.sup.7, --CH.dbd.NNHC(NH)NH.sub.2 or a; R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1-4 alkyl; R.sup.6 and R.sup.7 are the same or different and are each hydrogen or C.sub.1-4 alkyl or together with the nitrogen atom to which they are attached form a ring; R.sup.8 is hydrogen, C.sub.1-4 alkyl, or C.sub.
Abstract: New azo dyestuffs of the formula (I) ##STR1## wherein n in each case independently of one another represents 0 or 1,a, b and c independently of one another denote 1 or 2,a+c<4, a+b+c=3 or 5andX and Y denote different mono- or bivalent radicals,a process for their preparation and their use for dyeing and printing cellulose-containing fibre materials, in particular paper by means of the ink jet process, have been found.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
June 10, 1997
Assignee:
Bayer Aktiengesellschaft
Inventors:
Karin Hassenruck, Peter Wild, Frank-Michael Stohr
Abstract: The compounds of the present invention are adaptable as blocking or protecting groups for an amine composition useful in peptide synthesis. The present invention is directed to a method of protecting an amino group of an organic molecule during a reaction which modifies a portion of the molecule other than the protected amino group.
Abstract: Sulfur compounds of the formula ##STR1## where n is 0 or 2,R.sup.1 and R.sup.2 are hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, halogen, nitro, amino, hydroxysulfonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl or unsubstituted or substituted carbamoyl,A is methylene, sulfonyl or a radical of the formula CH.sub.2 --CO or CH.sub.2 --SO.sub.2,X is a direct bond or unsubstituted or substituted C.sub.1 -C.sub.8 -alkylene andY is vinyl or a radical of the formula C.sub.2 H.sub.4 Q, where Q is hydroxyl or a group which can be removed under alkaline reaction conditions,and a process for their preparation are described.
Abstract: This invention relates to substituted benzenesulfonylureas and -thioureas, processes for their preparation, and uses of the pharmaceutical products based on these compounds. The substituted benzenesulfonylureas and -thioureas are of the formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 E, and y are as defined in the specification. The compounds of formula I have antiarrhythmic activity.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
May 20, 1997
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Heinrich Englert, Dieter Mania, Jens Hartung, Heinz G ogelein, Joachim Kaiser, Uwe Gerlach