Abstract: 1R-cis,1'R-cis isomer of a 2',2'-(3,11-dioxo-4,10-dioxatridecylene)-bis(1,2,3,4-tetrahydro-6, 7-dimethoxy-2-methyl-1-veratrylisoquinolium) said, substantially free from other geometrical and optical isomers thereof. The 1R-cis,1'R-cis isomer has been found to have an advantageous combination of pharmacological properties, notably greater neuromuscular blocking potency, weaker histamine-releasing potency, and at equivalent levels of neuromuscular blockade, fewer potential adverse effects on the autonomic nervous system (sympathetic and parasympathetic blockage), in comparison with the known mixture of geometrical and optical isomers.
Abstract: Use of Methyl N-[6-(3,4,5-trimethoxybenzyloxy)imidazo [1,2-6]pyridazin-2-yl]carbamate or pharmaceutically acceptable salt to treat lymphocytic leukemia is disclosed.
Abstract: Purified Bordetella pertussis antigen having a molecular weight between 67,000 and 69,000 and determined by 12% (W/W) polyacrylamide gel electrophoresis and a proline glutamic acid ratio of substantially 1:1 as determined by amino acid analysis.
Abstract: The use of 1-(.beta.-D-arabinofuranosyl)-5-propynyluracil or a pharmaceutically acceptable salt or physiologically labile ester thereof for lowering serum cholesterol, particularly low density lipoprotein cholesterol levels in a human subject.
Type:
Grant
Filed:
February 11, 1993
Date of Patent:
July 11, 1995
Assignee:
Burroughs Wellcome Co.
Inventors:
Richard W. Peck, John Posner, Kenneth Powell
Abstract: A controlled sustained release tablet having at least one year shelf life and containing bupropion hydrochloride, hydroxypropyl methylcellulose and cysteine hydrochloride or glycine hydrochloride with the tablet having a surface area to volume ratio to effectively control bupropion hydrochloride release in the body.
Type:
Grant
Filed:
August 12, 1993
Date of Patent:
June 27, 1995
Assignee:
Burroughs Wellcome Co.
Inventors:
Jennie Sue G. Ludwig, William L. Bass, Jr., Joel E. Sutton, Jr.
Abstract: The compound 9-B-D-arabinofuranosyl-2-amino-6-methoxy-9H-purine along with its 5'-acetyl and 5'-(4-methoxy-4-oxobutyryl derivatives are disclosed as inhibitors of Varicella Zoster virus (VZV).
Type:
Grant
Filed:
August 23, 1993
Date of Patent:
June 13, 1995
Assignee:
Burroughs Wellcome Co.
Inventors:
Thomas A. Krenitsky, David J. T. Porter
Abstract: Diaryl urea compounds having anti-atherosclerosis activity are disclosed. Preferred compounds include the compounds 1-[4-(1,2-dimethoxyethoxy)benzyl-3-(2,4-dimethoxyphenyl)-l-heptylumea and 1-heptyl-3-(2,4-dimethoxyphenyl)-l-[4-(2-methoxyethoxymethoxy)-benzyl]urea .
Abstract: A method for treating two specific protozoal infections, Trichomonas vaginalis and Giardia lamblia, comprising the administration to a mammal in need thereof one of the following purine nucleosides:2,6-diamino-9-(2-deoxy-2-fluoro-.beta.-D-ribofuranosyl)-9H-purine2-amino-9-(2-deoxy-2-fluoro-.beta.-D-ribofuranosyl)-9H-purine2-amino-9-(2-deoxy-2-fluoro-.beta.-D-ribofuranosyl)-6-methoxy-9H-purine.
Type:
Grant
Filed:
September 2, 1992
Date of Patent:
May 30, 1995
Assignee:
Burroughs Wellcome Co.
Inventors:
Sylvia M. Tisdale, Joel Van Tuttle, Martin J. Slater, Susan M. Daluge, Wayne H. Miller, Thomas A. Krenitsky, George W. Koszalka
Abstract: A method of treating multiple drug resistance of susceptible tumor cells in a subject in need of such treatment by using the compounds of formula (II): ##STR1##
Abstract: This invention relates to a methodology for assessing the sensitivity of an HIV-1 sample to zidovudine and to diagnostic assays for use in such assessment.
Abstract: This invention relates to tetralin derivatives useful in medicine for the treatment of hypertension, to the synthesis of the compounds, to the pharmaceutical formulations containing the compounds and the use of the compounds in medical practice.
Type:
Grant
Filed:
March 22, 1993
Date of Patent:
April 11, 1995
Assignee:
Burroughs Wellcome Co.
Inventors:
John D. McDermed, Kevin P. Hurley, Vincent H. Chang, Anjaneyulu S. Tadepalli
Abstract: The present invention relates to novel benzoquinazoline thymidylate synthase inhibitors, to pharmaceutical formulations containing them and to their use in medicine.
Type:
Grant
Filed:
April 16, 1992
Date of Patent:
April 11, 1995
Assignee:
Burroughs Wellcome Co.
Inventors:
William Pendergast, Scott H. Dickerson, Julius V. Johnson, Robert Ferone
Abstract: The present invention relates to a novel ribonucleotide reductase inhibitor and new combinations comprising an antiviral compound, such as acyclovir, and a thiocarbonohydrazone ribonucleotide reductase inhibitor for the chemo-therapeutic treatment of virus infections, especially viruses of the herpes group.
Abstract: A compound of formula (I): ##STR1## wherein R.sup.1 represents a hydrogen or halogen atom, or a cyano group;R.sup.2 represents an optionally substituted carbocyclic group having 6 to 10 ring atoms and containing at least one aromatic ring; an optionally substituted heterocyclic group having 5 to 10 ring atoms, including 1 to 4 heteroatoms selected from O, N and S, and containing at least one aromatic ring; or an optionally substituted C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl- C.sub.1-6 alkyl, or C.sub.1-10 alkyl group;R.sup.3 and R.sup.4, which may be the same or different, each represent a hydrogen or halogen atom, or a C.sub.1-6 alkyl group optionally substituted by 1 to 3 halogen atoms; andR.sup.5 represents a hydrogen atom, a hydroxyl group, or a C.sub.1-6 alkyl group, optionally substituted by hydroxy, carboxy, amino or mono- or di-(C.sub.1-4)alkyl amino,and salts and other physiologically functional derivative thereof.The compounds are useful in the treatment of parasitic infections eg.
Abstract: Antiviral nucleoside analogues containing a substituted benzimidazole base attached to a carbocyclic ring in place of the conventional sugar residue, particularly those in which the 2-, 5- and 6-positions of the benzimidazole base are substituted by halogen, have activity against hepatitis B virus infections.
Abstract: Potentiating agents which enhance the efficacy of antineoplastic agents are disclosed. The potentiating agents disclosed are dibenz[b,e]oxepins such as doxepin.
Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, orPh(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, orR.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, orR.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; ##STR2## Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.
Type:
Grant
Filed:
November 24, 1993
Date of Patent:
March 7, 1995
Assignee:
Burroughs Wellcome Co.
Inventors:
William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
Abstract: The present invention relates to novel ribonucleotide reductase inhibitors and new combinations comprising an antiviral compound, such as acyclovir, and a thiocarbonohydrazone ribonucleotide reductase inhibitor for the chemotherapeutic treatment of virus infections, especially viruses of the herpes group.
Type:
Grant
Filed:
February 7, 1992
Date of Patent:
February 28, 1995
Assignee:
Burroughs Wellcome Co.
Inventors:
Todd A. Blumenhopf, Thomas Spector, Devron R. Averett, Robert W. Morrison, Jr., Eric C. Bigham, Virgil L. Styles