Abstract: This invention relates to a class of novel amino bi- and tri-carbocyclic alkane compounds having bis-aryl substitution which exhibit squalene synthase inhibition properties. The bi- and tri-carbocyclic alkane ring contains an amino group and the ring is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
Type:
Grant
Filed:
December 7, 1994
Date of Patent:
January 21, 1997
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Robert L. Morris, Kent W. Neuenschwander, Keith S. Learn, Anthony C. Scotese
Abstract: A method of inhibiting viruses in which a virus is contacted with diamondoid alcohol, ketone, ketone derivative, adamantyl amino acid, quaternary salt or combinations thereof which have antiviral properties. These diamondoid derivatives are shown to have antiviral activity against HIV.
Abstract: Novel tricyclic steriod analogs are disclosed which are 1H-benz[e]indene dodecahydro compounds that are useful for enhancing GABA-induced chloride currents at the GABA receptor/chloride ionophore complex and can be represented by the following structural formulas: ##STR1## wherein R.sub.1 =H or C.sub.1 -C.sub.4 alkyl or fluoroalkyl;R.sub.2 =H or C.sub.1 -C.sub.4 alkyl or fluoroalkyl, in which R.sub.1 and R.sub.2 can be the same or different;R.sub.3 =H or CH.sub.3 ;R.sub.4 =H or CH.sub.3, in which R.sub.3 and R.sub.4 can be the same or different;R.sub.5 =H;R.sub.6 =H;R.sub.5,R.sub.6 =.dbd.O(carbonyl);R.sub.7 =H;R.sub.8 =a hydrogen bond accepting group.R.sub.7,R.sub.8 =.dbd.O(carbonyl); andR'=an ester group.
Type:
Grant
Filed:
December 20, 1991
Date of Patent:
April 27, 1993
Assignee:
Washington University
Inventors:
Douglas F. Covey, Yuefei Hu, Charles F. Zorumski
Abstract: 2-(Substituted amino)-2-[2-hydroxy-2-alkyl (or phenyl)ethyl]tricyclo[3.3.1.1.sup.3,7 ]decane hydrohalides are described such as 2-(2-hydroxyoctyl)-2-(methylamino)-tricyclo[3.3.1.1.sup.3,7 ]decane hydrochloride. The compounds possess anti-inflammatory, analgesic, anticonvulsant and/or anti-hypoxia activity.
Type:
Grant
Filed:
January 22, 1986
Date of Patent:
March 10, 1987
Assignee:
Pennwalt Corporation
Inventors:
Vassil S. Georgiev, George B. Mullen, Patricia A. Swift
Abstract: The invention provides a novel explosive compound 1,3,5,7-tetranitroadamane, which possesses high explosive energy combined with excellent impact and thermal stability. The novel compound can be prepared by oxidation of 1,3,5,7-tetraaminoadamantane with permanganate.
Type:
Grant
Filed:
October 14, 1980
Date of Patent:
May 11, 1982
Assignee:
The United States of America as represented by the Secretary of the Army
Abstract: Novel 3-amino-4-homoisotwistane derivatives of the formula, ##STR1## wherein R.sub.1 is a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or a C.sub.3 -C.sub.5 alkenyl group, and R.sub.2 is a C.sub.1 -C.sub.4 alkyl group or a C.sub.3 -C.sub.5 alkenyl group, or non-toxic pharmaceutically acceptable salts thereof, which are very valuable as medicines for the treatment of virus-caused diseases and as antiviral agents for animals and useful for the treatment of parkinsonean disease.
Type:
Grant
Filed:
February 12, 1980
Date of Patent:
August 11, 1981
Assignees:
Sumitomo Chemical Company, Limited, Kao Soap Company, Limited
Abstract: Heavy reaction product after separation as by distillation of light reaction product or diadduct from a reaction mixture obtained by reaction of olefinically unsaturated nitriles with monoolefinic hydrocarbons containing an allylic hydrogen atom is hydrogenated to produce a polyamine mixture useful as an epoxy resin hardener yielding cured resins exhibiting low water absorption.
Abstract: 5-Amino-5,6-dihydro-dicyclopentadiene is prepared by reacting 5-isothiocyano-5,6-dihydro-dicyclopentadiene and an aqueous caustic medium at a temperature in excess of the melting point of 1,3-bis[5-(5,6-dihydro-dicyclopentadiene)]-2-thiourea while establishing and maintaining a pressure sufficient to maintain the water in the reaction mixture in a liquid state.
Abstract: 5-Isothiocyano-5,6-dihydro-dicyclopentadiene is hydrolyzed with caustic to 5-amino-5,6-dihydro-dicyclopentadiene in a reaction medium comprising a polar organic liquid which is inert under the reaction conditions and which at least partially dissolves the reactants and products.
Abstract: The invention provides novel 2-adamantyl hydrazine derivatives of the general formula A ##STR1## In this formula R.sub.1 is hydrogen or a lower alkyl group of 1-4 carbon atoms; R.sub.2 and R.sub.3 are the same or different and are each hydrogen, an unsubstituted or substituted radical being a lower alkyl of 1-4 carbon atoms, a lower alkanoic acid radical of 2-4 carbon atoms or a lower alkyl ester thereof, adamantyl, aryl, aralkyl, in which the alkyl moiety has from 1-4 carbon atoms or an unsubstituted or substituted heterocyclic radical of aromatic character; or R.sub.2 and R.sub.3 together with the nitrogen atom to which they are attached form an unsubstituted or substituted non-aromatic cyclic radical.The invention further provides pharmaceutically acceptable acid addition salts of the above compounds.Several methods of preparation of the new compounds are described.