Abstract: The present invention provides a compound of formula (I): ##STR1## wherein Y is sulfur; R.sup.2 and R.sup.3 are the same or different and are hydrogen or C.sub.1-4 alkyl; R.sup.4 is NR.sup.11 R.sup.12 ; R.sup.11, R.sup.12, R.sup.5 and R.sup.6 are the same or different and are hydrogen, C.sub.1-4 alkyl or C.sub.1-12 acyl; R.sup.7, R.sup.8, R.sup.9 and R.sup.10 are the same or different and are hydrogen, halo, C.sub.1-4 haloalkyl, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; and n is 2, 3, 4 or 5; m is 0 or an integer from 1 to 5; or a salt thereof, methods for the preparation of the compounds of the formula (I), intermediates in their preparations, pharmaceutical formulations containing them, and their use in the treatment of neoplastic growth.
Abstract: The peptides of the formula ##STR1## together with their pharmacologically acceptable salts, which have been described as exhibiting analgesic, antidiarrhoeal and antitussive activity, are effective in reversing neuronally-mediated bronchoconstriction in mammals. The said compounds have application in the palliation of conditions characterized by such a state, in particular asthma in human beings.
Type:
Grant
Filed:
March 7, 1989
Date of Patent:
May 1, 1990
Assignee:
Burroughs Wellcome Co.
Inventors:
Geoffrey Allan, John J. Adcock, Terence W. Smith
Abstract: The present invention relates to certain 2',3'-dideoxynucleosides and pharmaceutically acceptable derivatives thereof, methods for preparing them, their use in the treatment and prophylaxis of viral, especially retroviral, infections, and pharmaceutical formulations containing them.
Type:
Grant
Filed:
May 15, 1986
Date of Patent:
April 24, 1990
Assignee:
Burroughs Wellcome Co.
Inventors:
George W. Koszalka, Thomas A. Krenitsky
Abstract: The invention relates to pharmaceutical formulations comprising discrete units of zidovudine provided with a controlled release coating in which the said units are preferably in the form of spheroids.
Type:
Grant
Filed:
March 25, 1988
Date of Patent:
April 17, 1990
Assignee:
Burroughs Wellcome Co.
Inventors:
Harry P. Jones, Robert J. Mackey, Michael J. D. Gamlen
Abstract: The present invention relates to antitumor compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fused tetracyclic aromatic ring system comprised of 5-membered and 6-membered rings and contains at least one heteroatom and 3 aromatic rings and a total of no more than 18 ring atoms, or a substituted derivative thereof; the heteroatom is preferably oxygen, sulfur or nitrogen; when it is nitrogen this is substituted by hydrogen, methyl or ethyl;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is O or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-5 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.
Abstract: The present invention relates to anti tumor compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fused tetracyclic aromatic ring system comprised of 5-membered and 6-membered rings and contains at least one heteroatom and 3 aromatic rings and a total of no more than 18 ring atoms, or a substituted derivative thereof; the heteroatom is preferably oxygen, sulfur or nitrogen; when it is nitrogen this is substituted by hydrogen, methyl or ethyl; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-5 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.
Abstract: Potent antiproliferative activity in combination with low inhibition of histamine N-methyltransferase has been found in a class of 2,4-diamino-6-(2,5-dialkoxybenzyl)-5-methylpyrido[2,3-d]pyrimidines.
Type:
Grant
Filed:
November 30, 1987
Date of Patent:
January 30, 1990
Assignee:
Burroughs Wellcome Co.
Inventors:
David S. Duch, Charles A. Nichol, Carl W. Sigel
Abstract: This invention relates to synergistic combinations of nucleoside analogues, which are converted to viral DNA polymerase inhibitors through the action of at least one virus-induced enzyme, and nucleoside transport inhibitors. These combinations are especially useful in combatting herpes virus infections.
Abstract: A method of controlling veterinary ectoparasites of mammals and birds of the sub-Orders Ixodoidea and Sarcoptiformes comprising the application of a parasiticidally effective, non-toxic amount of a pyrethroid of formula ##STR1## together with at least one parasiticidal organophosphoruscompound active against said ectoparasites.
Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4 or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar being planar or deviating only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.
Abstract: The present invention provides a compound of formula (I): ##STR1## wherein R.sup.1 is hydrogen , C.sub.1-4 alkyl, acetyl or formyl; R.sup.2 and R.sup.3 are the same or different and are hydrogen or C.sub.1-4 alkyl; R.sup.4 is NR.sup.11 R.sup.12 ; R.sup.11, R.sup.12, R.sup.5 and R.sup.6 are the same or different and are hydrogen, C.sub.1-4 alkyl or C.sub.1-12 acyl; R.sup.7, R.sup.8, R.sup.9 and R.sup.10 are the same or different and are hydrogen, halo, C.sub.1-4 haloalkyl, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; and n is 2, 3, 4 or 5; m is 0 or an integer from 1 to 6; or a salt thereof, methods for the preparation of the compounds of the formula (I), intermediates in their preparations, pharmaceutical formulations containing them, and their use in the treatment of tumors.
Abstract: The present invention relates to certain novel 8-phenylxanthines substituted in the 3 or 4 position of the phenyl group by an alkenylene, alkenyleneoxy, alkynylene or alkynyleneoxy bearing a terminal acidic grouping, and to their use in human and veterinary therapy, particularly for conditions associated with the cell surface effects of adenosine.
Abstract: Treatment of susceptible gram-negative infections in animals is disclosed using the compound 3'-azido-3'-deoxythymidine or a pharmaceutically acceptable basic salt thereof.Also disclosed is the use of the 5'-mono-, di- and triphosphate of 3'-azido-3'-deoxythymidine or a pharmaceutically acceptable basic salt thereof for the same purpose.
Type:
Grant
Filed:
December 2, 1988
Date of Patent:
October 17, 1989
Assignee:
Burroughs Wellcome Co.
Inventors:
Lowrie M. Beacham, III, Harry S. LeBlanc, George A. Freeman
Abstract: Treatment of AIDS or humans carrying or infected with the AIDS virus or having antibodies to the AIDS virus is disclosed using the compound 3'-azido-3'-deoxythymidine or a pharmaceutically acceptable basic salt thereof.Also disclosed is the use of the 5'-mono-, di- and triphosphate of 3'-azido-3'-deoxythymidine or a pharmaceutically acceptable basic salt thereof for the same purpose.
Type:
Grant
Filed:
February 8, 1988
Date of Patent:
October 17, 1989
Assignee:
Burroughs Wellcome Co.
Inventors:
Janet L. Rideout, David W. Barry, Sandra N. Lehrman, Martha H. St. Clair, Phillip A. Furman
Abstract: The present invention relates to antitumor compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fused tetracyclic aromatic ring system comprised of 5-membered and 6-membered rings and contains at least one heteroatom and 3 aromatic rings and a total of no more than 18 ring atoms, or a substituted derivative thereof; the heteroatom is preferably oxygen, sulfur or nitrogen; when it is nitrogen this is substituted by hydrogen, methyl or ethyl;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-5 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.
Abstract: The present invention relates to compounds of formula I ##STR1## or a salt, ester or amide thereof; wherein R.sup.1 is --CH.sub.2 --CH.sub.2 --, CH.sub.2 --O-- or --O--CH.sub.2 --; R.sup.2 and R.sup.3 are the same or different and are each hydrogen, C.sub.1-4 alkyl or taken together with the nitrogen comprise a nitrogen-containing heterocyclic ring having four to six ring members; R.sup.4 is a single bond or a C.sub.1-7 bivalent aliphatic hydrocarbon group and may be joined to the aromatic ring system at the 2,3,8 or 9 positions; n is 0 to 3, and their use as anithistamine and antiasthma agents.
Type:
Grant
Filed:
August 7, 1986
Date of Patent:
October 3, 1989
Assignee:
Burroughs Wellcome Co.
Inventors:
O. William Lever, Jr., Harry J. Leighton
Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a C.sub.8-13 fused heterotricyclic ring system containing at least two aromatic rings and no more than 3 heteroatoms (in separate rings), or a C.sub.10-17 fused heterotetracyclic ring system containing at least two aromatic rings and no more than 4 heteroatoms (in separate rings) or a C.sub.
Abstract: A method of treating an animal for the prevention or control of infestation by insects of the Order Diptera which comprises application to the animal of a compound of formula ##STR1##
Type:
Grant
Filed:
October 27, 1987
Date of Patent:
October 3, 1989
Assignee:
Burroughs Wellcome Co.
Inventors:
Michael D. Matthewson, Gerald G. Blackman