Abstract: The present invention relates to novel compounds of formula (I) which has inhibitory activities against human immunodeficiency virus ("HIV") protease, a process for the preparation thereof, and compositions for prevention or treatment of AIDS by HIV infection comprising the above compounds as active ingredients. ##STR1## wherein: R.sup.1 is an aromatic group, a nitrogen-containing aromatic group, C.sub.1-4 alkyl group optionally substituted with an aromatic group or a nitrogen-containing aromatic group, C.sub.1-4 alkoxy group optionally substituted with an aromatic group or a nitrogen-containing aromatic group;R.sup.2 is an amino acid residue or a C.sub.1-8 alkyl group substituted with a C.sub.1-4 alkylsulfonyl group;R.sup.3 is a C.sub.1-4 alkyl group optionally substituted with an aromatic group;R.sup.4 is hydrogen or a C.sub.1-2 alkyl group;R.sup.5 is a C.sub.1-10 alkyl group optionally substituted with an aromatic group; andn is 1 or 2.
Type:
Grant
Filed:
June 6, 1996
Date of Patent:
September 23, 1997
Assignee:
LG Chemical Limited
Inventors:
Nakyen Choy, Hoil Choi, Chi-Hyo Park, Young-Chan Son, Chang-Sun Lee, Heungsik Yoon, Sung-Chun Kim, Jong-Sung Koh, Chung-Ryeol Kim
Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
September 23, 1997
Assignee:
Cambridge NeuroScience, Inc.
Inventors:
Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew Gannett Knapp, Lee David Margolin
Abstract: This invention pertains to a novel group of 1,2-dithiin compounds useful as antiinfective agents, and a novel synthetic process to produce the same. The compounds are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans or Aspergillus fumigatus.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
September 16, 1997
Assignees:
Shaman Pharmaceuticals, Inc., The Regents of the University of Michigan
Inventors:
Thien V. Truong, Donald E. Bierer, Jeffrey M. Dener, Richard Hector, Michael S. Tempesta, Bernard Loev, Wu Yang, Masato Koreeda
Abstract: A method of treatment for atherosclerosis and/or reducing cholesterol using an angiotensin II antagonist. This method of treatment can be used in conjunction with the treatment of hypertension. Substituted imidazoles such as ##STR1## are useful as angiotensin II receptor antagonists for this method of treatment. A method of treatment for atherosclerosis and/or reducing cholesterol using an angiotensin II receptor antagonist in combination with an HMG-Co A reductase inhibitor. A method of treatment for atherosclerosis and/or reducing cholesterol using an angiotensin II receptor antagonist in combination with an HMG-Co A reductase inhibitor and an angiotensin converting enzyme inhibitor. Also within the scope of this invention are pharmaceutical compositions for this method of use.
Abstract: This invention relates to novel diastereomeric acid addition salts of homochiral hydroxylamines, to processes for obtaining such, to processes for the conversion thereof to the corresponding homochiral hydroxylamines, to certain novel homochiral hydroxylamines and the processes for using these as intermediates.
Abstract: Disclosed are (2-one (or thione)-1,3-dithiole-4,5-diyl)bis(thiomethylthiocyanate) compounds corresponding to the formula: ##STR1## wherein Z is oxygen or sulfur, compositions containing said compounds and their use as antimicrobial and marine antifouling agents.
Type:
Grant
Filed:
July 10, 1996
Date of Patent:
August 26, 1997
Assignee:
The Dow Chemical Company
Inventors:
Duane R. Romer, Weishi W. Wu, Ravi B. Shankar, R. Garth Pews
Abstract: A process for preparing alkyl 5-oxo-6-heptenoates of the formula I ##STR1## where X and Y are hydrogen or methyl, and R.sup.1 is C.sub.1 -C.sub.8 -alkyl, byA) reacting 5-acetyl-2-norbornene with a dialkyl carbonate [CO(OR.sup.2).sub.2, where R.sup.2 is C.sub.1 -C.sub.4 -alkyl,] in the presence of a base to give an alkyl 3-(2-norbornen-5-yl)-3-oxopropionate II,B) reacting the ester II on the presence of a base with an unsaturated compound of the formula III ##STR2## where Z is CN or CO.sub.2 R.sup.3, where R.sup.3 is C.sub.1 -C.sub.4 -alkyl, and hydrolyzing the product of the reaction of compound II with compound III to a 5-(2-norbornen-5-yl)-5-oxopentanoic acid of the formula IV,C) esterifying the acid IV to give a 5-(2-norbornen-5-yl)-5-oxopentanoic ester of the formula V, andD) converting the ester V by thermal cleavage into an alkyl 5-oxo-6-heptenoate I.
Type:
Grant
Filed:
February 1, 1996
Date of Patent:
August 19, 1997
Assignee:
BASF Aktiengesellschaft
Inventors:
Klaus Ebel, Matthias Eiermann, Thomas Papkalla
Abstract: A method is disclosed for the treatment of anxiety by the administration of 3-amino-5-carbamoyl-chromans and 8-fluoro-3-amino-5-carbamoylchromans or enantiomers or salts thereof.
Type:
Grant
Filed:
May 30, 1995
Date of Patent:
August 12, 1997
Assignee:
Astra Aktiebolag
Inventors:
Eva Maria Hammarberg, Lars George Johansson, Lars-Gunnar Larsson, Rolf Noreen, Lucy Anna Renyi, Svante Bertil Ross, Daniel Dungan Sohn, Bjorn Eric Svensson, Seth-Olov Thorberg
Abstract: 3-amino-5-carbonylchromans, as well as enantiomers and salts thereof are disclosed. Pharmaceutical compositions containing the compounds as active ingredients are also disclosed. The compounds are useful in the treatment of 5-hydroxytryptamine-mediated disorders of the central nervous system.
Type:
Grant
Filed:
May 30, 1995
Date of Patent:
August 12, 1997
Assignee:
Astra Aktiebolag
Inventors:
Eva Maria Hammarberg, Lars George Johansson, Lars-Gunnar Larsson, Rolf Noreen, Lucy Anna Renyi, Svante Bertil Ross, Daniel Dungan Sohn, Bjorn Eric Svensson, Seth-Olov Thorberg
Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
July 29, 1997
Assignee:
Cambridge NeuroScience, Inc.
Inventors:
Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew Gannett Knapp, Lee David Margolin
Abstract: Process for the preparation of derivatives having general formula (I) ##STR1## wherein the meaning of R will be defined in the text, characterized by the reaction between a compound having formula ##STR2## wherein X is an halogen, and an alkaline salt of a methyl dialkylmalonate.
Type:
Grant
Filed:
June 14, 1996
Date of Patent:
July 22, 1997
Assignee:
Erregierre S.P.A.
Inventors:
Antonio Bonaldi, Massimo Ferrari, Egidio Molinari, Fabrizio Zinetti
Abstract: The present invention provides a method for sensitizing hypoxic cells in a tumor to radiation, wherein nitric oxide is delivered to target hypoxic cells through the administration of a nitric oxide-containing compound that spontaneously releases nitric oxide under physiological conditions without requiring the presence of oxygen. Also provided are methods of protecting noncancerous cells or tissues in a mammal from radiation, sensitizing cancerous cells in a mammal to chemotherapeutic agents, and protecting noncancerous cells or tissues in a mammal from chemotherapeutic agents, all by administration of the same compounds.
Type:
Grant
Filed:
October 7, 1994
Date of Patent:
July 22, 1997
Assignee:
The United States of America as represented by the Department of Health and Human Services
Inventors:
James B. Mitchell, Angelo Russo, Murali C. Krishna, David A. Wink, Jr., James E. Liebmann
Abstract: A process for the production of N-acylaminophenols by the concurrent hydrogenation of a nitrophenol to an aminophenol and the acylation of the aminophenol with acyl anhydride takes place on a continuous basis in a stirred tank reactor in which liquid product is continuously withdrawn from the reactor. Of particular interest is the manufacture of acetaminophen, N-acetyl-p-aminophenol by continuous reaction of p-ntirophenol, hydrogen and acetic anhydride.
Type:
Grant
Filed:
May 26, 1995
Date of Patent:
July 15, 1997
Assignee:
Hoechst Celanese Corp.
Inventors:
James A. Foster, Werner H. Mueller, Debra A. Ryan, Hartmut Wiezer
Abstract: The invention relates to a new process for the synthesis of a disubstituted carbodiimide, including a first stage of phosgenation of an N,N'-disubstituted urea in an organic solvent medium.After this first stage ammonia is added to the reaction mixture without preliminary isolation of any intermediate compound.The process is simple, relatively inexpensive and the yield is high.Disubstituted carbodiimides are organic synthesis intermediates used especially in pharmaceutical chemistry as coupling agents in peptide synthesis.
Type:
Grant
Filed:
January 16, 1996
Date of Patent:
July 15, 1997
Assignee:
Societe Nationale des Poudres et Explosifs
Inventors:
Patricia Hussenet, Philippe Le Goff, Gerard Sennyey
Abstract: Water soluble microbubble generating microparticle contrast agents which are comprised of a carbohydrate and a non-triglyceride, non-surface active material for use in image enhancement wherein the non-surface active material is less soluble in water than the carbohydrate.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
July 15, 1997
Assignee:
Nycomed Imaging AS
Inventors:
Jo Klaveness, Pal Rongveo, Lars Stubberud
Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are employed as intermediates in the synthesis of aminochroman compounds useful in the treatment of CNS disorders.
Type:
Grant
Filed:
May 30, 1995
Date of Patent:
July 8, 1997
Assignee:
Astra Aktiebolag
Inventors:
Eva Maria Hammarberg, Lars George Johansson, Lars-Gunnar Larsson, Rolf Noreen, Lucy Anna Renyi, Svante Bertil Ross, Daniel Dungan Sohn, Bjorn Eric Svensson, Seth-Olov Thorberg
Abstract: This invention relates to bis mono- and/or bicyclic aryl and/or heteroaryl compounds exhibiting protein tyrosine kinase inhibition activity. More specifically, it relates to the method of inhibiting abnormal cell proliferation in a patient suffering from a disorder characterized by such proliferation comprising the administration thereto of an EGF and/or PDGF receptor inhibiting effective amount of said bis mono- and/or bicyclic aryl and/or heteroaryl compound and to the preparation of said compounds and their use in pharmaceutical compositions used in this method.
Type:
Grant
Filed:
May 11, 1995
Date of Patent:
July 8, 1997
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Alfred P. Spada, Michael R. Myers, Martin P. Maguire, Paul E. Persons
Abstract: A method is disclosed for the treatment of depression by the administration of 3-amino-5-carbamoylchromans and 8-fluoro-3-amino-5-carbamoylchromans or enantiomers or salts thereof.
Type:
Grant
Filed:
May 30, 1995
Date of Patent:
June 24, 1997
Assignee:
Astra Aktiebolag
Inventors:
Eva Maria Hammarberg, Lars George Johansson, Lars-Gunnar Larsson, Rolf Noreen, Lucy Anna Renyi, Svante Bertil Ross, Daniel Dungan Sohn, Bjorn Eric Svensson, Seth-Olov Thorberg
Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocycle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.
Type:
Grant
Filed:
September 8, 1994
Date of Patent:
June 24, 1997
Assignee:
Cell Therapeutics, Inc.
Inventors:
J. Peter Klein, Gail E. Underiner, Anil M. Kumar
Abstract: A method for the treatment of a cutaneous, ocular, or mucosal pathological condition which is associated with immune response in a human or other mammal, that includes topical application of an effective amount of spiperone or a spiperone derivative or its pharmaceutically acceptable salt, in a pharmaceutically-acceptable diluent or carrier for topical application.
Type:
Grant
Filed:
September 13, 1993
Date of Patent:
June 17, 1997
Assignee:
Beth Israel Deaconess Medical Center, Inc.
Inventors:
Richard J. Sharpe, Kenneth A. Arndt, Stephen J. Galli