Abstract: Compounds of the formula ##STR1## in which the variables are as defined in the claims, which are suitable as fibre-reactive dyes for dyeing widely varying fibre materials, are described.
Type:
Grant
Filed:
November 26, 1997
Date of Patent:
October 19, 1999
Assignee:
Ciba Specialty Chemicals Corporation
Inventors:
Rolf Deitz, Bernhard Muller, Athanassios Tzikas
Abstract: The invention relates to novel, androstane steroids which are the ligand semiochemicals which bind to neuroepithelial receptors. The steroids are useful as ligands to neuroepithelial receptors in the human vomeronasal gland to stimulate autonomic and hypothalamic activity.
Type:
Grant
Filed:
September 29, 1994
Date of Patent:
October 19, 1999
Assignee:
Pherin Corporation
Inventors:
David L. Berliner, Nathan W. Adams, Clive L. Jennings-White
Abstract: The invention relates to a method of altering hypothalamic function in an individual. The method comprises nasally administering a human semiochemical, e.g. an Androstane steroid, or a pharmaceutical composition containing a semiochemical, such that the ligand semiochemical binds to a specific neuroepithelial receptor. The steroid or steroids is/are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Other embodiments of the invention include pharmaceutical compositions containing the steroids.
Type:
Grant
Filed:
December 15, 1998
Date of Patent:
October 12, 1999
Assignee:
Pherin Pharmaceuticals, Inc.
Inventors:
David L. Berliner, Nathan William Adams, Clive L. Jennings-White
Abstract: The invention is directed to 17.beta.-nitro-11.beta.-arylsteroids of formula I: ##STR1## wherein R.sup.1, R.sup.6, R.sup.7, R.sup.12 and X are as defined by the specification. The compounds exhibit potent antiprogestational activity and are useful in the treatment of fibroids, endometriosis, cervical ripening prior to delivery, hormone replacement therapy and in the control of fertility.
Type:
Grant
Filed:
May 29, 1998
Date of Patent:
October 5, 1999
Assignee:
Research Triangle Institute
Inventors:
C. Edgar Cook, John A. Kepler, Rupa S. Shetty, Gary S. Bartley, David Yue-wei Lee
Abstract: Disclosed are polyamines having the formula: ##STR1## or salts or stereoisomers thereof wherein R.sub.1 -R.sub.4 and ALK.sub.1 -ALK.sub.3 are as defined in the specification. Pharmaceutical compositions and therapeutic methods of treatment utilizing the compounds are also disclosed.
Type:
Grant
Filed:
February 6, 1996
Date of Patent:
October 5, 1999
Assignee:
University of Florida Research Foundation, Inc.
Abstract: The present invention provides novel phosphonic acid-based cationic lipids of the general structure: ##STR1## or a salt, or solvate, or enantiomers thereof wherein; (a) R.sub.1 is a lipophilic moiety; (b) R.sub.2 is a positively charged moiety; (c) R.sub.3 is a lipophilic moiety of 1 to about 24 carbon atoms, a positively charged moiety, or a negatively charged moiety; (d) n is an integer from 0 to 8; (e) X.sup.- is an anion or polyanion; (f) Y is N or O, and (g) m is an integer from 0 to a number equivalent to the positive charge(s) present on the lipid.The present invention further provides compositions of these lipids with polyanionic macromolecules, methods for interfering with protein expression in a cell utilizing these compositions and a kit for preparing the same.
Type:
Grant
Filed:
June 5, 1996
Date of Patent:
September 28, 1999
Assignee:
Genta Incorporated
Inventors:
Brian Patrick Dwyer, Alexandre V. Lehedev, Bob Dale Brown, David Aaron Schwartz
Abstract: The invention relates to a method for the preparation of a compound of formula II: ##STR1## wherein a compound of formula V: ##STR2## is condensed with a compound of the formula CH.sub.3 -C(OR.sub.4 O)-(CH.sub.2).sub.3 -XHal and R.sub.1, R.sub.2, R.sub.3, R.sub.4, X and Hal are as defined by the specification.
Type:
Grant
Filed:
August 5, 1998
Date of Patent:
September 21, 1999
Assignee:
Akzo Nobel, N.V.
Inventors:
Franciscus Theodorus Leonardus Brands, Pieter Vrijhof
Abstract: Cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.
Type:
Grant
Filed:
May 8, 1997
Date of Patent:
September 14, 1999
Assignee:
Genzyme Corporation
Inventors:
Craig S. Siegel, Edward R. Lee, David J. Harris
Abstract: An androgenic steroid compound of the formula: ##STR1## wherein: X, Y, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are as defined herein.
Type:
Grant
Filed:
November 26, 1997
Date of Patent:
September 14, 1999
Assignee:
Research Triangle Institute
Inventors:
C. Edgar Cook, John A. Kepler, Yue-Wei Lee, Mansukh C. Wani
Abstract: A methotrexate conjugated to 1-3 acyl groups derived from fatty acids. In particular the invention relates to altering the pharmacokinetic profile and mode of delivery of methotrexate by conjugating it to 1.2 or 3 acyl derivatives of fatty acids.
Type:
Grant
Filed:
September 25, 1997
Date of Patent:
September 14, 1999
Assignee:
Commonwealth Scientific and Industrial Research Organisation
Inventors:
Robert George Whittaker, Veronika Judith Bender, Wayne Gerrard Reilly, Minoo Moghaddam
Abstract: Cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.
Type:
Grant
Filed:
May 6, 1997
Date of Patent:
September 7, 1999
Assignee:
Genzyme Corporation
Inventors:
Mikaela N. Keynes, Craig S. Siegel, Edward R. Lee, David J. Harris
Abstract: A compound of the formula ##STR1## wherein the A.sub.1 and B.sub.1 rings are as defined by the specification. The compounds are intermediates in the preparation of oxoetiocholenic acid.
Abstract: Cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.
Type:
Grant
Filed:
May 9, 1997
Date of Patent:
August 24, 1999
Assignee:
Genzyme Corporation
Inventors:
Craig S. Siegel, Edward R. Lee, David J. Harris
Abstract: Methods, compositions, and compounds for modulating the GABA.sub.A receptor-chloride ionophore complex to alleviate stress, anxiety, seizures, mood disorders, PMS and PND and to induce anesthesia.
Type:
Grant
Filed:
July 2, 1997
Date of Patent:
August 17, 1999
Assignee:
CoCensys, Inc.
Inventors:
Ravindra B. Upasani, Haiji Xia, Derk Hogenkamp
Abstract: This invention relates to certain steroidal glycosides useful as hypocholesterolemic agents and antiatherosclerosis agents and certain protected intermediates useful in the preparation of said steroidal glycosides.
Abstract: A compound of formula (I): ##STR1## wherein A is oxygen, W is CH.sub.3 O.CH.dbd.CCO.sub.2 CH.sub.3 and R.sup.1, R.sup.2, R.sup.3, X, Y and Z are as defined in the specification. The compounds are useful as plant fungicides and insecticides.
Type:
Grant
Filed:
July 31, 1995
Date of Patent:
August 10, 1999
Assignee:
Zeneca Limited
Inventors:
Paul Anthony Worthington, Ian Henry Aspinall
Abstract: The invention relates to compounds of formula (I): ##STR1## wherein Q and R are as defined in the specification. The compounds are useful in the treatment of a number of disorders including osteoporosis, inflammation and psoriasis.
Abstract: Methods for the preparation of the 19-norprogesterone of formula I ##STR1## and its intermediates, in crystalline and amorphous forms are disclosed. The process is performed by (1) protecting the hydroxyl group of a compound of formula II ##STR2## (2) reacting the protected compound with an alkali or alkaline earth metal anion radical, (3) hydrolyzing the resulting compound, (4) ketalizing the carbonyl groups, (5) epoxidizing the compound, (6) opening the epoxide ring and introducing an N,N,dimethylamino-phenyl functional group into the axial position of C.sub.11, (7) deketalizing and dehydrating the resulting compound, and (8) acetylating to provide 17.alpha.-acetoxy-11.beta.-(4-N,N-dimethylaminophenyl)-19-norpregna-4,9-di ene-3,20-dione (I).
Type:
Grant
Filed:
March 30, 1995
Date of Patent:
July 27, 1999
Assignee:
The United States of America as represented by the Department of Health and Human Services
Inventors:
Hyun K. Kim, Pemmaraju Narasinha Rao, James E. Burdett, Jr., Carmie K. Acosta
Abstract: A process for preparing an optically active dihydrosphingosine derivative is disclosed, comprising reducing a (2R,3R)-2-amino-3-hydroxyalkanoic acid derivative represented by formula (III): ##STR1## wherein R.sup.3 represents a straight-chain alkyl group having 7 to 21 carbon atoms; and R.sup.4 represents an amino group protecting group, (e.g., (2R,3R)-2-benzylamino-3-hydroxyoctadecanoic acid) with sodium tetrahydroborate in the presence of an acid. The process makes it feasible to produce an optically active dihydrosphingosine at high optical purity and through a simple process that is safe and easy to industrialize.
Abstract: Cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.
Type:
Grant
Filed:
March 31, 1997
Date of Patent:
July 20, 1999
Assignee:
Genzyme Corporation
Inventors:
Edward R. Lee, David J. Harris, Craig S. Siegel