Patents by Inventor Keith Blakeney Mallion
Keith Blakeney Mallion has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 5866611Abstract: Compounds of formula I, and their pharmaceutically acceptable salts, ##STR1## in which R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkenyl; or NR.sup.1 R.sup.2 is a heterocyclic group; A is trimethylene optionally substituted by alkyl and the phenyl ring is optionally substituted by substituents such as halogeno, alkenyl, amino, cyano, ureido, alkyl, carbamoylalkyl, alkanoylamino, alkoxycarbonyl, N-alkyl-alkanoylamino, alkanoyl and amines thereof; are inhibitors of squalene synthese and hence useful in treating diseases in which a lowering of cholesterol is desirable. As well as the use of these compounds in medicine, novel compounds, processes for their preparation and pharmaceutical compositions are also referred to.Type: GrantFiled: May 19, 1994Date of Patent: February 2, 1999Assignee: Zeneca LimitedInventors: George Robert Brown, Murdoch Allan Eakin, Peter John Harrison, deceased, Keith Blakeney Mallion
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Patent number: 5861516Abstract: A process for preparing an antifungal azole compound of formula (I) by reacting an epoxide with hydrazine to from a hydrazino compound which is subsequently reacted with an iminoether. The amidrazone product is subsequently reacted with an orthoformate to provide the antifungal azole. The azole, known as ZD0870, shows good activity against human fungal infections including Candida albicans, Cryptococcus neoformans and Aspergillus fumigatus.Type: GrantFiled: April 9, 1997Date of Patent: January 19, 1999Assignee: Zeneca LimitedInventors: Elwyn Peter Davies, John David Pittam, Keith Blakeney Mallion, Nigel Philip Taylor
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Patent number: 5792777Abstract: Biphenylylquinuclidine compounds of the formula I: ##STR1## and pharmaceutically-acceptable salts thereof; wherein R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen; or R.sup.1 and R.sup.2 are joined together so that CR.sup.1 -CR.sup.2 is a double bond; and one or both ring A and ring B may be optionally unsubstituted or independently substituted by one or more substituents selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, (1-6C)alkyl, (1-6C)alkoxy, (1-6C)alkylamino, di-?(1-6C)alkyl!amino, N-?(1-6C)alkyl!carbamoyl, N,N-di-?(1-6C)alkyl!carbamoyl, (1-6C)alkoxycarbonyl, (1-6C)alkylthio, (1-6C)alkylsulphinyl, (1-6C)alkylsulphonyl and halogeno-(1-6C)alkyl; are inhibitors of squalene synthase and are hence useful in treating diseases or medical conditions such as hypercholesterolemia, atherosclerosis and fungal diseases.Type: GrantFiled: June 30, 1993Date of Patent: August 11, 1998Assignee: Zeneca LimitedInventors: George Robert Brown, Peter John Harrison, deceased, Keith Blakeney Mallion
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Patent number: 5770608Abstract: Quinuclidine compounds of the formula I: ##STR1## R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen;or R.sup.1 and R.sup.2 are joined together so that CR.sup.1 --CR.sup.2 is a double bond;X is selected from --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 NH--, --NHCH.sub.2 --, --CH.sub.2 CO--, --COCH.sub.2 --, --CH.dbd.N--, --N.dbd.CH--, --CH.sub.2 S--, --SCH.sub.Type: GrantFiled: February 24, 1997Date of Patent: June 23, 1998Assignee: Imperial Chemical Industries PLCInventors: George Robert Brown, Keith Blakeney Mallion, Peter John Harrison, deceased
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Patent number: 5714496Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts in which R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen; or R.sup.1 and R.sup.2 are joined together so that CR.sup.1 -CR.sup.2 is a double bond; X is selected from --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 O--, --CH.sub.2 NH--, --NHCH.sub.2 --, --CH.sub.2 CO--, --COCH.sub.2 --, --CH.sub.2 S-- and --SCH.sub.2 --; Ar.sup.1 is a phenylene moiety; Ar.sup.2 is a heteroaryl moiety; and wherein one or both of Ar.sup.1 and Ar.sup.2 may optionally bear one or more substituents independently selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, di-alkylamino, N-alkylcarbamoyl, di-N,N-alkylcarbamoyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, halogeno-alkyl, carboxyalkyl and alkanoylamino; provided that when R.sup.1 is hydroxy, X is not selected from --NHCH.sub.2 -- and --SCH.sub.Type: GrantFiled: February 28, 1995Date of Patent: February 3, 1998Assignee: Zeneca LimitedInventors: George Robert Brown, Keith Blakeney Mallion, Paul Robert Owen Whittamore, David Robert Brittain
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Patent number: 5691349Abstract: Quinuclidine derivatives of formula, and their pharmaceutically acceptable salts, in which: R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen; pr R.sup.1 and R.sup.2 are joined together so that CR.sup.1 -CR.sup.2 is a double bond; X is selected from --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.dbd.C--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 NH--, NHCH.sub.2 --, --CH.sub.2 CO--, --COCH.sub.2 --, --CH.sub.2 S(O).sub.n -- and --S(O).sub.n CH.sub.2 -- wherein n is 0, 1 or 2; and AR is phenyl which may be optionally unsubstituted or substituted by one or more substituents such as halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, dialkylamino, N-alkylcarbamoyl, N,N-di-alkylcarbamoyl, alkoxycarbonyl, alkythio, alkylsulphinyl, alkylsulphonyl, halogeno alkyl, alkanoylamino, alkylenedioxy, alkanoyl and oxime derivatives thereof and O-alkyl ethers of said oximes; provided that when X is selected from --OCH.sub.2 --, --NHCH.sub.2 --, and SCH.sub.2 --, R.sup.Type: GrantFiled: June 23, 1995Date of Patent: November 25, 1997Assignee: Zeneca LimitedInventors: Keith Blakeney Mallion, George Robert Brown, Paul Robert Owen
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Patent number: 5654315Abstract: Quinuclidine compounds of the formula I: ##STR1## R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen;or R.sup.1 and R.sup.2 are joined together so that CR.sup.1 --CR.sup.2 is a double bond;X is selected from --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 NH--, --NHCH.sub.2 --, --CH.sub.2 CO--, --COCH.sub.2 --, --CH.dbd.N--, --N.dbd.CH--, --CH.sub.2 S--, --SCH.sub.Type: GrantFiled: June 23, 1994Date of Patent: August 5, 1997Assignee: Imperial Chemical Industries PLCInventors: George Robert Brown, Keith Blakeney Mallion, Peter John Harrison, deceased
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Patent number: 4079055Abstract: The disclosure relates to a novel chemical process whereby enone intermediates for prostaglandins are reduced steroselectively to the .alpha.-enols, the .alpha.-hydroxy of which corresponds to the prostaglandin 15.alpha.-hydroxy group.Type: GrantFiled: May 21, 1976Date of Patent: March 14, 1978Assignee: Imperial Chemical Industries LimitedInventors: Keith Blakeney Mallion, Graham Ernest Robinson
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Patent number: 4021425Abstract: The disclosure relates to a novel four-stage reaction sequence whereby known enone intermediates for prostaglandin analogues may be obtained from 4.beta.-dimethoxymethyl-2,3,3.alpha..beta.,6.alpha..beta.-tetrahydro-5.alp ha.-hydroxy-6.beta.-iodo-2-oxocyclopenteno[b]furan in substantially increased yield. A novel intermediate produced in the novel four-stage reaction sequence is also claimed.Type: GrantFiled: November 13, 1975Date of Patent: May 3, 1977Assignee: Imperial Chemical Industries LimitedInventor: Keith Blakeney Mallion
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Patent number: 4000305Abstract: This invention relates to novel 15-, 16- and 17-heterocyclyl nor-prostanoic acid derivatives, for example 9.alpha.,11.alpha.,15-trihydroxy-16-(indol-5-yloxy)-17,18,19,20-tetranor-5 -cis, 13-trans-prostadienoic acid, which have a unique profile of Prostaglandin-like properties, and to processes for their manufacture, and also to pharmaceutical or veterinary compositions containing one of said novel derivatives, and a method of inducing luteolysis in an animal host by administering one of said novel derivatives.Type: GrantFiled: October 1, 1975Date of Patent: December 28, 1976Assignee: Imperial Chemical Industries LimitedInventors: Jean Bowler, Keith Blakeney Mallion, Dora Nellie Richardson
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Patent number: 3959273Abstract: The disclosure relates to new 2-aryloxymethylmorpholine derivatives which possess antidepressant properties, and to processes for the manufacture of the said morpholine derivatives, to pharmaceutical compositions containing them, and to a method of preventing or relieving depression in warm-blooded animals including man. Typical of the morpholine derivatives disclosed is 2-(o-ethoxyphenoxymethyl)morpholine.Type: GrantFiled: September 27, 1974Date of Patent: May 25, 1976Assignee: Imperial Chemical Industries LimitedInventors: Keith Blakeney Mallion, Ralph William Turner, Alexander Henry Todd
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Patent number: 3935240Abstract: The disclosure relates to novel intermediates, for use in the manufacture of known prostaglandins and prostaglandin-like compounds, for example aldehydes such as methyl 7-[2.beta.-formyl-3.alpha.-hydroxy-5.alpha.-(4-phenylbenzoyloxy)cyclopent- 1.alpha.-yl]hetp-5-cis-enoate and enones such as methyl 15-oxo-9.alpha.,11.alpha.-di(4-phenylbenzoyloxy)-5-cis,13-trans-prostadien oate, processes for their manufacture, and their conversion to prostaglandins or prostaglandin-like compounds.Type: GrantFiled: October 26, 1973Date of Patent: January 27, 1976Assignee: Imperial Chemical Industries LimitedInventor: Keith Blakeney Mallion
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Patent number: 3931206Abstract: Prostanoic acid derivatives having luteolytic activity are provided. A representative compound is 16-(6-chloropyrid-2-yloxy)-9.alpha., 11.alpha., 15-trihydroxy-17, 18, 19, 20-tetranor-5-cis, 13-trans-prostadienoic acid.Type: GrantFiled: September 14, 1973Date of Patent: January 6, 1976Assignee: Imperial Chemical Industries LimitedInventors: Jean Bowler, Keith Blakeney Mallion, Dora Nellie Richardson