Abstract: Amino acid derivatives of general formula ##STR1## (the definitions of the various symbols being explained in the specification) are suitable for treating high blood pressure and for cardioprotection. The new compounds are prepared and used in the usual way.
Type:
Grant
Filed:
September 6, 1989
Date of Patent:
April 16, 1991
Assignee:
Boehringer Ingelheim GmbH
Inventors:
Gerd Schnorrenberg, Otto Roos, Walter Losel, Ingrid Wiedemann, Wolfram Gaida, Wolfgang Hoefke, Dietrich Arndts, Ilse Streller
Abstract: A process for preparing a compound of Formula (I): ##STR1## wherein R is phenyl or phenyl substituted with hydroxy, lower alkoxy, halogen or lower alkyl; Y is unsubstituted or substituted methylene, ethylene, vinylene or oxygen; m is 0 or 1; n is 0, 1 or 2; and q is 1, 2, 3 or 4; with the limitation that when m is 0, n is not 0, and when m is 1, n is not 2, which process comprises:(a) reacting an aldehyde of Formula (II); ##STR2## wherein R, Y, m and n are as defined above, under reaction conditions for the Wittig Reaction with a ylide of Formula (III):(R.sup.1).sub.3 P.dbd.CH(CH.sub.2).sub.q COOM (III)wherein R.sup.1 is C.sub.1 -C.sub.
Abstract: 3-Hydroxyazabenzo[b]thiophene derivatives having optionally 2-aryl, 2-aralkyl, 2-alkyl or 2-alkenyl substituents were prepared by, among other methods, ring closure of an appropriately substituted benzylthio-alkoxycarbonyl-pyridine. These compounds are found to be useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases such as psoriasis and atopic eczema, cardiovascular disorders, inflammatory diseases and other leukotriene mediated diseases.
Type:
Grant
Filed:
December 8, 1989
Date of Patent:
April 9, 1991
Assignee:
Merck & Co. Inc., Inc.
Inventors:
Robert K. Baker, Arsenio A. Pessolano, Kathleen M. Rupprecht, Philippe L. Durette
Abstract: Novel N-(4-piperindyl)bicyclic condensed 2-imidazolamine derivatives and their pharmaceutically acceptable acid addition salts having anti-histaminic properties, compositions containing the same, and methods of treating allergic diseases in warm-blooded animals.
Type:
Grant
Filed:
December 4, 1989
Date of Patent:
April 9, 1991
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Frans E. Janssens, Joseph L. G. Torremans, Gasto S. M. Diels
Abstract: The invention relates to substituted pyridine-2,4-dicarboxylic acid derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings given. The invention also relates to a process for the preparation of the abovementioned compounds and to their use as medicaments, in particular as fibrosuppressants and immunosuppressants.
Type:
Grant
Filed:
March 4, 1988
Date of Patent:
April 2, 1991
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Ekkehard Baader, Martin Bickel, Dietrich Brocks, Volkmar Gunzler, Stephan Henke, Hartmut Hanauske-Abel
Abstract: This invention relates to the process for the preparation of certain 2-phenylalkylthio- and phenylalkylsulfinyl-imidazo[4,5-c]pyridines useful for the treatment of osteoporosis.
Abstract: A compound, or a solvate or salt thereof, of formula I: ##STR1## in which: R.CO-- is an acyl group containing a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic group;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;R.sub.4 is C.sub.1-6 alkyl, or phenyl;R.sub.5 is hydrogen or together with R.sub.4 forms a --(CH.sub.2).sub.n -- group in which n=1, 2 or 3; and `Het` is an optionally substituted single or fused ring heterocyclic group, containing from 5 to 12 ring atoms and comprising up to four hetero-atoms in the or each ring selected from oxygen, nitrogen and sulphur, with the proviso that when, simultaneously, R.sub.
Abstract: Compounds of formula I ##STR1## in which R is H, or an aliphatic or aromatic radical, R.sup.1 is alkyl, R.sup.2 is alkyl, alkoxy, aryl, aryloxy, aralkyl, alkaryl, aralkyloxy, alkaryloxy, alkaralkyl or alkaralkyloxy, and one of R.sup.1 and R.sup.2 is H and the other has the meaning given above. These compounds are intermediates for the preparation of herbicidal sulfonylureas.
Abstract: The present invention relates to (RS)-2-(2,3-dihydro-5-hydroxy-4,6,7-trimethylbenzofuranyl) acetic acids and 2-(2,3-dihydro-5-acyloxy-4,6,7-trimethylbenzofuranyl) acetic acids and esters thereof, the process for producing them and their relevant therapeutical use as mucoregulators and antiischemic agents.
Type:
Grant
Filed:
April 13, 1989
Date of Patent:
March 12, 1991
Assignee:
Biomedica Foscama Industria Chimico-Farmaceutica S.p.A.
Abstract: The carbamate salt of 2-(2'-thienyl)-alkylamines and particularly the ethylamine and its method of synthesis are disclosed. The carbamate salt of 2-(2'-thienyl)ethylamine is a stable, easily transportable crystalline material that can be converted to 2-(2'-thienyl)ethylamine, a useful intermediate in the synthesis of 5[(2-chlorophenyl)methyl]-4,5,6,7-tetrahydrothieno-[3,2-c]pyridine hydrochloride, also known as ticlopidine hydrochloride. The synthesis is carried out by reacting an amine of formula (I): ##STR1## with CO.sub.
Abstract: Compounds represented by the general formula ##STR1## in which R.sub.1 and R.sub.2 are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or benzyl, or R.sub.1 and R.sub.2 may form together with the nitrogen atom to which they are attached a C.sub.4 -C.sub.8 saturated heterocycle, R.sub.3 and R.sub.4 are independently selected from hydrogen or C hd 1-C.sub.6 alkyl, R.sub.5 is selected from hydrogen or halogen, or C.sub.1 -C.sub.4 alkyl, C.sub.1 -C hd 4 alkoxy, nitro or trifluoromethyl, n is 1, 2 or 3, and one of the symbols A, B, C or D represents N and the others represent CH, as well as the N-oxids and the the pharmaceutically acceptable acid addition salts and their salts with bases. The compounds have nervous system affecting properties.
Type:
Grant
Filed:
June 6, 1989
Date of Patent:
February 26, 1991
Assignee:
SANOFI
Inventors:
Etienne Mendes, Jean-Claude Vernieres, Jacques Simiaud, Peter E. Keane
Abstract: Insecticides of the general formula ##STR1## wherein R.sub.1 is an optionally substituted 5- to 10-member heterocyclic moiety; R.sub.2 is an optionally substituted alkyl, cycloalkyl or alkenyl moiety; X is oxygen, sulfur or --NH--; and R.sub.3 is: (a) an optionally substituted 3-phenoxyphenalkyl, 3-phenoxypyridylalkyl, 3-(pyridyloxy)phenalkyl, 3-phenylaminophenoalkyl, 3-benzylphenalkyl or 3-benzyloxyphenalkyl moiety; (b) a benzylfuranylmethyl moiety; (c) a 3- or 4-substituted benzyl or tetrafluorobenzyl moiety; (d) 4-phenoxy-2-butyn-2-yl; or (e) 2-methyl-3-phenylbenzyl.
Abstract: The disclosure deals with pyrazolopyridine compounds of the formula ##STR1## wherein the variables are defined in the specification. The compounds are useful in the treatment of bronchial asthma, immunosuppression, diabetes, etc.
Abstract: Compounds of the formula ##STR1## where R.sup.1 is lower alkyl, R.sup.2 is chlorophenyl, Y is alkylene, X is heterocyclic and Z is a fused ring are useful as antiinflammatory and antiallergy agents.
Type:
Grant
Filed:
May 8, 1989
Date of Patent:
February 12, 1991
Assignee:
Pfizer Inc.
Inventors:
Kelvin Cooper, Peter E. Cross, Michael J. Fray, Kenneth Richardson
Abstract: This invention relates to substituted imidazopyridine derivatives having the follow formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof: wherein the variables are described in the specification are useful in the treatment of diseases or disorders mediated by platelet-activating factor. This invention also relates to pharmaceutical compositions of such substituted imidazopyridines.
Abstract: 7-(1-Pyrrolidinyl)-3-quinolone- and -naphthyridonecarboxylic acid derivatives as antibacterial agents and feed additives, of the formula ##STR1## in which X.sup.1 is halogen,X.sup.2 is hydrogen, halogen, amino or other radical,R.sup.1 is alkyl, cycloalkyl, optionally substituted phenyl or other radical,R.sup.2 is hydrogen, alkyl or a dioxolylmethyl radical,R.sup.3 is ##STR2## A is N, CH, C-halogen, or the like, or forms a bridge with R.sup.1, and addition products thereof.
Type:
Grant
Filed:
June 30, 1989
Date of Patent:
February 5, 1991
Assignee:
Bayer Aktiengesellschaft
Inventors:
Uwe Petersen, Thomas Schenke, Andreas Krebs, Klaus Grohe, Michael Schriewer, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
Abstract: A compound which is a 3-(acylaminomethyl)imidazo[1,2-a]pyridine derivative of formula (I) ##STR1## in which R.sub.1 denotes hydrogen; linear or branched C.sub.1 -C.sub.4 alkyl; or benzyl;R.sub.2 denotes linear or branched C.sub.1 -C.sub.6 alkyl; cyclohexyl; trichloromethyl; 1-propenyl; allyl; phenyl; 4-chlorophenyl; or benzyl:or R.sub.1 and R.sub.2 together denote a C.sub.3 -C.sub.5 aliphatic chain:X denotes halogen; C.sub.1 -C.sub.3 alkyl; methylthio; trifluoromethyl; optionally esterified carboxy of formula --COOR in which R denotes hydrogen or C.sub.1 -C.sub.6 alkyl; cyano; optionally mono- or dialkylated aminocarbonyl of formula --CONR.sub.3 R.sub.4 in which R.sub.3 and R.sub.4 independently denote hydrogen or C.sub.1 -C.sub.4 alkyl or together denote a chain of formula --(CH.sub.2).sub.2 --Z--(CH.sub.2).sub.2 -- in which Z denotes a direct bond, oxygen, sulphur, or a divalent group of formula --CH.sub.2 --, --NH-- or --N(C.sub.1 -C.sub.4 alkyl)--; alkylamino of formula NHR.sub.5 in which R.sub.
Type:
Grant
Filed:
October 24, 1989
Date of Patent:
February 5, 1991
Assignee:
Synthelabo
Inventors:
Pascal George, Claudie Giron, Jacques Froissant