Patents Represented by Attorney Lawrence A. Nielsen
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Patent number: 5104870Abstract: Novel (2S, 3S, 5R) morpholinols of formula (I) ##STR1## together with the (+-)-(2R*,3R*,5S*) racemates thereof, and their salts, whereinX is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms or a group --CH.sub.2 --X.sup.1 where X.sup.1 is cycloalkyl of 3 to 6 carbon atoms.The compounds have a variety of uses in human medicine, in particular in the treatment of mental disorders such as depression.Type: GrantFiled: April 2, 1991Date of Patent: April 14, 1992Assignee: Burroughs Wellcome Co.Inventors: James L. Kelley, David L. Musso, Grady E. Boswell, Barrett R. Cooper
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Patent number: 5104897Abstract: A class of halogen-substituted diphenylsulfide compounds are disclosed which produce a large selective inhibition of serotonin uptake in brain. Such compounds are useful in the treatment of depression, anxiety, obsessive compulsive disorders and substance abuse disorders such as alcoholism.Type: GrantFiled: June 28, 1991Date of Patent: April 14, 1992Assignee: Burroughs Wellcome Co.Inventors: Lawrence E. Brieaddy, Claudia E. B. Hollingsworth, Barrett R. Cooper
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Patent number: 5102914Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein R.sub.1 is hydrogen;R.sub.2 is carbonyl; andR.sub.3 is hydroxy;and salts thereof, with processes for preparing same and with their use in medicine for the treatment of hypertension.Type: GrantFiled: December 18, 1989Date of Patent: April 7, 1992Assignee: Burroughs Wellcome Co.Inventors: John D. McDermed, Anjaneyulu S. Tadepalli, Vincent H. Chang, Kevin P. Hurley
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Patent number: 5095018Abstract: 3-benzyl-1,2,4-triazolo [4,3-.alpha.] pyrazines are prepared. They are useful as anticonvulsants.Type: GrantFiled: March 22, 1991Date of Patent: March 10, 1992Assignee: Burroughs Wellcome Co.Inventor: James L. Kelley
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Patent number: 5095039Abstract: A halogen-substituted diphenylsulfide compound is disclosed which produce a large selective inhibition of serotonin uptake in brain. This compound is useful in the treatment of depression as well as anxiety, obsessive compulsive disorders and alcoholism.Type: GrantFiled: June 5, 1990Date of Patent: March 10, 1992Assignee: Burroughs Wellcome Co.Inventors: Nariman B. Mehta, Lawrence E. Brieaddy
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Patent number: 5093114Abstract: 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: GrantFiled: November 30, 1990Date of Patent: March 3, 1992Assignee: Burroughs Wellcome Co.Inventors: Janet L. Rideout, David W. Barry, Sandra N. Lehrmaan, Martha H. St. Clair, Phillip A. Furman
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Patent number: 5091531Abstract: Compounds of general formula (I) ##STR1## wherein R.sup.1 represents an optinally substituted carbocyclic or heterocyclic aryl group, or an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R.sup.2 represents an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl group or an optionally substituted carbocyclic or heterocyclic aryl or aralkyl group; R.sup.3 represents a hydrogen atom or an alkyl group; and either X represents an oxygen or sulphur atom, a group --CH.sub.2 -- or a group NR.sup.4 where R.sup.4 represents a hydrogen atom or a C.sub.1-4 alkyl group; and Y represents a group --CH.sub.2 -- or --CH.sub.2 CH.sub.2 -- X-Y together represent the group --CH.dbd.CH--; and salts and physiologically functional derivatives thereof are useful in the treatment of tumours. Processes for preparing the compounds, intermediates useful in their preparation, pharmaceutical compositions containing them and their use in the treatment of tumours are also described.Type: GrantFiled: August 12, 1988Date of Patent: February 25, 1992Assignee: Burroughs Wellcome Co.Inventor: Simon T. Hodgson
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Patent number: 5089500Abstract: The present invention relates to 6-substituted purine carbocyclic nucleosides and their use in medical therapy particularly in the treatment of HIV and HBV infections. Also provided are pharmceutical formulations and processes for the preparation of compounds according to the invention.Type: GrantFiled: May 8, 1991Date of Patent: February 18, 1992Assignee: Burroughs Wellcome Co.Inventor: Susan M. Daluge
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Patent number: 5087697Abstract: The present invention relates to 6-substituted purine carbocyclic nucleosides and their use in medical therapy particularly in the treatment of HIV and HBV infections. The invention also relates to pharmaceutical formulations and processes for the preparation of compounds according to the invention.Type: GrantFiled: December 19, 1990Date of Patent: February 11, 1992Assignee: Burroughs Wellcome Co.Inventor: Susan M. Daluge
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Patent number: 5086044Abstract: 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. Additionally, there is disclosed the treatment of Kaposi's sarcoma with 3'-azido-3'-deoxythymidine (AZT) and the synergistic activity in the treatment of humans infected with HTLV-III of AZT and interferon as well as AZT and acyclovir.Type: GrantFiled: April 18, 1990Date of Patent: February 4, 1992Assignee: Burroughs Wellcome Co.Inventors: Janet L. Rideout, David W. Barry, Sandra N. Lehrman, Martha H. St. Clair, Phillip A. Furman
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Patent number: 5075455Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.Type: GrantFiled: August 29, 1989Date of Patent: December 24, 1991Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 5071983Abstract: This invention relates to certain derivatives of 2', 3'-dideoxycytidine and their use in medical therapy particularly in the treatment of HIV infections. Also provided are pharmaceutical formulations and processes for the manufacture of the compounds according to the invention.Type: GrantFiled: October 6, 1989Date of Patent: December 10, 1991Assignee: Burroughs Wellcome Co.Inventors: George W. Koszalka, Thomas A. Krenitsky
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Patent number: 5070078Abstract: 2',3'-Dideoxy-3'-fluoro pyrimidine nucleosides particularly 2',3'-dideoxy-3'-fluorothymidine have been found to have particularly potent activity against adenovirus infections especially those caused by adenoviruses of serotype 8. Such compounds are preferably presented in pharmaceutical formulations adapted for ophthalmic administration.Type: GrantFiled: August 19, 1988Date of Patent: December 3, 1991Assignee: Burroughs Wellcome Co.Inventors: John W. T. Selway, Lowrie M. Beacham, III, Susan M. Daluge, Joel Van Tuttle, Thomas A. Krenitsky
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Patent number: 5068320Abstract: This invention relates to certain 6-substituted 2',3'-dideoxypurine nucleosides and derivatives thereof. The compounds are useful as antivirals.Type: GrantFiled: October 6, 1989Date of Patent: November 26, 1991Assignee: Burroughs Wellcome Co.Inventors: George W. Koszalka, Charlene L. Burns, Thomas A. Krenitsky, Janet L. Rideout
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Patent number: 5061708Abstract: The present invention relates to certain amino acid esters of the purine nucleoside acyclovir, pharmaceutically acceptable salts thereof and their use in the treatment and prophylaxis of herpes virus infections. The invention also includes pharmaceutical formulations and processes for the preparation of such compounds.Type: GrantFiled: November 21, 1989Date of Patent: October 29, 1991Assignee: Burroughs Wellcome Co.Inventor: Thomas A. Krenitsky
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Patent number: 5059604Abstract: A group of 2-aminopurine compounds, which have in the 6-position a hydrogen and in the 9-position an acyclic moiety ##STR1## wherein X is oxygen or sulphur and Y is hydrogen or CH.sub.2 OH (provided than when X is oxygen Y may not be hydrogen), are converted enzymatically in vivo into the corresponding 6-hydroxy (i.e. guanine) derivatives which are potent antiviral compounds. The enzymatic conversion may also be effected ex vivo (i.e. in vitro) as a method of synthesizing the corresponding 6-hydroxy derivatives.Type: GrantFiled: January 27, 1984Date of Patent: October 22, 1991Assignee: Burroughs Wellcome Co.Inventors: Thomas A. Krenitsky, Lilia M. Beauchamp
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Patent number: 5053432Abstract: Novel antiprotozoal naphthoquinones having the general formula ##STR1## (wherein either R.sup.1 is hydrogen and R.sup.2 is selected from C.sub.1-6 alkoxy, aralkoxy, C.sub.1-6 alkyl-C.sub.1-6 alkoxy, phenyl substituted by one or two groups selected from halogen and C.sub.1-6 alkyl, halogen and perhalo-C.sub.1-6 alkyl; or R.sup.1 and R.sup.2 are both C.sub.1-6 alkyl or phenyl; and n is 0 or 1) and salt thereof. The compounds of formula (I) are useful for the treatment or prophylaxis of protozoal diseases including malaria, theileriosis and coccidiosis. Various processes for preparing compounds of formula (I) are described.Type: GrantFiled: December 26, 1989Date of Patent: October 1, 1991Assignee: Burroughs Wellcome Co.Inventors: Alan T. Hudson, Anthony W. Randall
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Patent number: 5049581Abstract: The present invention relates to compounds of formula(I) ArCh.sub.Type: GrantFiled: August 25, 1989Date of Patent: September 17, 1991Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 5049671Abstract: The present invention relates to 6-substituted purine carbocyclic nucleosides and their use in medical therapy particularly in the treatment of HIV and HBV infections. Also provided are pharmaceutical formulations and processes for the preparation of compounds according to the invention.Type: GrantFiled: December 22, 1989Date of Patent: September 17, 1991Assignee: Burroughs Wellcome Co.Inventor: Susan M. Daluge
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Patent number: 5043339Abstract: The present invention relates to amino acid esters of pyrimidine and purine nucleosides containing an acyclic side chain, and their use in medical therapy, particularly the treatment of herpes virus infections. Also provided are pharmaceutical formulations and processes for the preparation of compounds according to the invention.Type: GrantFiled: December 18, 1989Date of Patent: August 27, 1991Assignee: Burroughs Wellcome Co.Inventor: Lilia M. Beauchamp