Abstract: The present invention relates to the compounds of general formula ##STR1## used as medicaments possessing therapeutic activity for the treatment of anxiety, psychosis, epilepsy, convulsion, motoricity problems, amnesia, cerebrovascular diseases or senile dementia.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
March 24, 1998
Assignee:
Laboratorios Del Dr. Esteve, S.A.
Inventors:
Ramon Merce-Vidal, Jordi Frigola-Constansa
Abstract: Aralkylamino substituted azacyclic compounds of formula (I) and their salts and prodrugs. The variables are defined herein. The compounds are useful as tachykinin antagonists and are of particular use in the treatment of pain, inflammation, migraine, and emesis.
Type:
Grant
Filed:
July 11, 1996
Date of Patent:
March 17, 1998
Assignee:
Merck Sharp & Dohme Limited
Inventors:
Malcolm MacCoss, Christopher John Swain
Abstract: Compound of Formula (I), wherein W.sub.1 is an oxygen atom; an --NR-- group wherein R is hydrogen, C.sub.1 -C.sub.7 alkyl or benzyl; and B is for example a substituted piperidine or quinuclidine. The disclosed compounds are useful as neurokinin receptor antagonists.
Type:
Grant
Filed:
November 29, 1995
Date of Patent:
March 10, 1998
Assignee:
Sanofi
Inventors:
Jean-Philippe Ducoux, Patrick Gueule, Xavier Emonds-Alt
Abstract: Fused-ring system N-alkylpiperidinyl-4-methyl carboxylic acid ester or amide derivs. and analogues (D, having formula (I-1)-(I-5), and their salts. The variables are defined herein. The compounds (I) are 5-HT4 receptor antagonists, and are useful for treatment or prophylaxis of gastrointestinal, cardiovascular or CNS disorders. Typically (I) are used for treatment of irritable bowel syndrome (including associated diarrhea and urinary incontinence); for treatment of the nausea and gastric symptoms of gastro-oesophageal reflux disease and dyspepsia; as antiemetics (e.g. against cytotoxin agent or radiation-induced emesis); for preventing atrial fibrillation and other atrial arrhythmias and reducing occurrence of stroke; as anxiolytics; and for treatment of migraine, schizophrenia, Parkinson's disease and Huntington's chorea.
Type:
Grant
Filed:
April 14, 1995
Date of Patent:
March 10, 1998
Assignee:
SmithKline Beecham plc
Inventors:
Laramie Mary Gaster, Graham Francis Joiner, Keith Raymond Mulholland, Paul Adrian Wyman
Abstract: The compound of the formula (I) or its salt or a medicament containing the same ##STR1## wherein, A and B represent a carbonyl group or sulfonyl group, m and p are different and represent 0 or 1,R.sup.1 and R.sup.2 may be the same or different from each other and represent a hydrogen atom, an unsubstituted or substituted alkyl group, an unsubstituted or substituted aryl group, an unsubstituted or substituted aralkyl group, an unsubstituted or substituted heterocyclic group containing nitrogen or an unsubstituted or substituted heterocyclic group containing oxygen, or R.sup.1 and R.sup.2, taken together with the nitrogen atom to which they are linked, may form an unsubstituted or substituted heterocyclic group, provided that when B is a sulfonyl group, R.sup.
Abstract: A diuretic compound of Formula I ##STR1## or pharmaceutically acceptable salt thereof where R.sup.1 is a C.sub.1-6 alkyl; R.sup.2 is halogen, C.sub.1-4 alkyl; and R.sup.3 is C.sub.1-4 alkoxy are disclosed, preferably, benzamide, 3-chloro-N-(2-ethyl-2-(3-methoxyphenyl)-4-(1-piperidinyl)butyl), monohydrochloride. The compounds are effective diuretics which increase the excretion of water with little increase in electrolyte excretion.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
February 10, 1998
Assignee:
Pharmacia & Upjohn Company
Inventors:
Stephen J. Humphrey, James T. Curry, E. Jon Jacobsen
Abstract: In a process for preparing 3-methylpiperidine or 3-methylpyridine from 2-methyl-1,5-diaminopentane in the gaseous phase, the initial product is made to flow over catalysts. In the first step, 3-methylpiperidine is produced, and if required 3-methylpyridine is produced in a second step.
Type:
Grant
Filed:
November 2, 1995
Date of Patent:
February 3, 1998
Assignee:
Lonza Ltd.
Inventors:
Josef Heveling, Erich Armbruster, Walter Siegrist
Abstract: A process is disclosed for the selective hydrogenation of butynediol to 2-butene-1,4-diol using a palladium catalyst to which either copper and zinc, or silver and zinc, or copper, silver and zinc are added as doping agents. In the preferred embodiment, it has been possible, by optimizing the composition of the catalyst, to improve the activity and selectivity of the catalysts in question while also eliminating the need to handle toxic substances during the catalyst manufacturing process.
Type:
Grant
Filed:
March 20, 1997
Date of Patent:
February 3, 1998
Assignee:
BASF Aktiengesellschaft
Inventors:
Matthias Irgang, Volkmar Menger, Ernest Miesen, Peter Stops, Fritz Graf
Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
Type:
Grant
Filed:
June 17, 1994
Date of Patent:
February 3, 1998
Assignee:
Corvas International, Inc.
Inventors:
Joseph E. Semple, Odile E. Levy, Ruth F. Nutt, William C. Ripka
Abstract: N,N'-bridged bistetramethylpiperidinyl compounds of Formula I ##STR1## useful as light stabilizers and stabilizers for organic material which are prepared starting from tetramethylpiperidinyl compounds of Formula II ##STR2## by reacting a compound of Formula II with a cyclic carbonate of Formula III.
Abstract: The invention relates to quaternary basic amides of the formula ##STR1## in which Ar is an optionally substituted mono-, di- or tri-cyclic aromatic or heteroaromatic group;T is a direct bond, a hydroxymethylene group, an alkoxymethylene group in which the alkoxy group is C.sub.1 -C.sub.4, or a C.sub.1 -C.sub.5 -alkylene group;Ar' is an unsubstituted or mono- or poly-substituted phenyl, a thienyl, a benzothienyl, a naphthyl or an indolyl;R is hydrogen or a C.sub.1 -C.sub.4 -alkyl, or a C.sub.1 -C.sub.4 -.omega.-alkoxy(C.sub.2 -C.sub.4)alkyl, or a C.sub.2 -C.sub.4 -.omega.-alkanoyloxy (C.sub.1 -C.sub.4)alkyl;Q is hydrogen;or else Q and R together form a 1,2-ethylene, 1,3-propylene or 1,4-butylene group;Am.sup..sym. is the radical ##STR2## in which X.sub.1, X.sub.2 and X.sub.3, together with the nitrogen atom to which they are bonded, form a 1-azoniabicyclo?2.2.2!octane optionally substituted by a phenyl or benzyl group; andA.sup..crclbar. is a pharmaceutically acceptable anion.
Type:
Grant
Filed:
October 18, 1996
Date of Patent:
January 27, 1998
Assignee:
Sanofi
Inventors:
Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
Abstract: The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, thalidomide and various related compounds such as thalidomide precursors, analogs, metabolites and hydrolysis products have been shown to inhibit angiogenesis. Importantly, these compounds can be administered orally.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
January 27, 1998
Assignee:
The Children's Medical Center Corporation
Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4, and Q.sup.5 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of SP and NKA are useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
Abstract: The present invention relates to certain substituted 17.beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), wherein R.sup.1 and R.sup.2 i) are independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, or ii) taken together are a --CH.sub.2 -- group forming a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond; R.sup.3 is preferably hydrogen, halogen or lower alkyl, R.sup.4 is preferably hydrogen or lower alkyl, X is preferably CH.sub.2, Y is preferably hydrogen and Z is preferably CONR.sup.14 R.sup.15 and R.sup.14 and R.sup.15 are a variety of organic groups, and pharmaceutically acceptable salts thereof, preparation, medical use and pharmaceutical formulations.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
January 13, 1998
Assignee:
Glaxo Wellcome Inc.
Inventors:
Robert Carl Andrews, Cynthia Markert Cribbs, Stephen Vernon Frye, Curt Dale Haffner, Patrick Reed Maloney
Abstract: The reaction of cyanoolefins, aminocarbonylolefins or hydroxyiminoolefins with a Vilsmeier reagent leads to 2-halogenopyridines which bear aldehyde groups in the 3 and/or 5 position. These pyridinealdehydes are valuable intermediates for the preparation of pharmaceuticals and crop protection agents.
Abstract: A catalyst for oxidizing ethylene and producing ethylene oxide, said catalyst being prepared by pretreating a porous carrier with a solution containing a lithium compound and a cesium compound, thereafter, impregnating a solution containing a silver compound and a cesium compound in the pretreated porous carrier and then heat-treating the impregnated porous carrier.The use of the catalyst of this invention provides high selectivity in the production of ethylene oxide by the vapor contact oxidation of ethylene.
Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X.sub.1 --(CH.sub.2).sub.x --X.sub.2 and the aromatic carbon atoms to which they are attached form 5-7 membered ring wherein X.sub.1 is O or S; X.sub.2 is O, S, NR.sub.5 or NR.sub.6 CO wherein R.sub.5 is hydrogen or C.sub.1-6 alkyl; or one of X.sub.1 and X.sub.2 is O, S or CH.sub.2 and the other is CH.sub.2 ; x is 1, 2 or 3; R.sub.1 and R.sub.2 together are Q--CH.sub.2 --CH.sub.2, Q--CH.dbd.CH, or Q--CH.dbd.N where Q is linked either to the R.sub.1 or the R.sub.2 substitution position and Q is O, S or NR.sub.t wherein R.sub.t is hydrogen or C.sub.1-6 alkyl; R.sub.3 is hydrogen halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or amino; R.sub.4.sup.1 and R.sub.4.sup.2 are independently hydrogen or C.sub.1-6 alkyl; Y is O or NH; Z is of sub-formula (a), (b) or (c) and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
Abstract: Propylene is oxidized to propylene oxide in the vapor phase using oxygen and a supported catalyst comprising silver, gold, a potassium promoter such as potassium nitrate or potassium carbonate and a support comprised in whole or in substantial part of an alkaline earth metal carbonate.
Type:
Grant
Filed:
October 2, 1996
Date of Patent:
December 30, 1997
Assignee:
Arco Chemical Technology, L.P.
Inventors:
Anne M. Gaffney, Andrew P. Kahn, Rangasamy Pitchai
Abstract: This invention relates to certain steroidal glycosides of Formula I ##STR1## wherein the values for the variables are described herein, which are useful as hypocholesterolemic agents and antiatherosclerosis agents and certain protected intermediates useful in the preparation of said steroidal glycosides.
Abstract: Tertiary diamines having two saturated heterocyclic rings joined by an aliphatic carbon chain, of the general formula ##STR1## in which each A is a two- to four-membered aliphatic carbon chain substituted if desired by one or more C.sub.1 -C.sub.4 -alkyl groups, are prepared in one stage by catalytic hydrogenation of the corresponding dinitriles of the general formulaN.tbd.C--A--C.tbd.N IIThe diamines preparable in accordance with the invention are particularly suitable as catalysts for the production of polyurethanes.
Type:
Grant
Filed:
January 30, 1997
Date of Patent:
December 16, 1997
Assignee:
Lonza AG
Inventors:
Josef Heveling, Andreas Gerhard, Ulrich Daum