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).

  • Patent number: 5866611
    Abstract: 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: Grant
    Filed: May 19, 1994
    Date of Patent: February 2, 1999
    Assignee: Zeneca Limited
    Inventors: George Robert Brown, Murdoch Allan Eakin, Peter John Harrison, deceased, Keith Blakeney Mallion
  • Patent number: 5861516
    Abstract: 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: Grant
    Filed: April 9, 1997
    Date of Patent: January 19, 1999
    Assignee: Zeneca Limited
    Inventors: Elwyn Peter Davies, John David Pittam, Keith Blakeney Mallion, Nigel Philip Taylor
  • Patent number: 5792777
    Abstract: 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: Grant
    Filed: June 30, 1993
    Date of Patent: August 11, 1998
    Assignee: Zeneca Limited
    Inventors: George Robert Brown, Peter John Harrison, deceased, Keith Blakeney Mallion
  • Patent number: 5770608
    Abstract: 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: Grant
    Filed: February 24, 1997
    Date of Patent: June 23, 1998
    Assignee: Imperial Chemical Industries PLC
    Inventors: George Robert Brown, Keith Blakeney Mallion, Peter John Harrison, deceased
  • Patent number: 5714496
    Abstract: 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: Grant
    Filed: February 28, 1995
    Date of Patent: February 3, 1998
    Assignee: Zeneca Limited
    Inventors: George Robert Brown, Keith Blakeney Mallion, Paul Robert Owen Whittamore, David Robert Brittain
  • Patent number: 5691349
    Abstract: 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: Grant
    Filed: June 23, 1995
    Date of Patent: November 25, 1997
    Assignee: Zeneca Limited
    Inventors: Keith Blakeney Mallion, George Robert Brown, Paul Robert Owen
  • Patent number: 5654315
    Abstract: 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: Grant
    Filed: June 23, 1994
    Date of Patent: August 5, 1997
    Assignee: Imperial Chemical Industries PLC
    Inventors: George Robert Brown, Keith Blakeney Mallion, Peter John Harrison, deceased
  • Patent number: 4079055
    Abstract: 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: Grant
    Filed: May 21, 1976
    Date of Patent: March 14, 1978
    Assignee: Imperial Chemical Industries Limited
    Inventors: Keith Blakeney Mallion, Graham Ernest Robinson
  • Patent number: 4021425
    Abstract: 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: Grant
    Filed: November 13, 1975
    Date of Patent: May 3, 1977
    Assignee: Imperial Chemical Industries Limited
    Inventor: Keith Blakeney Mallion
  • Patent number: 4000305
    Abstract: 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: Grant
    Filed: October 1, 1975
    Date of Patent: December 28, 1976
    Assignee: Imperial Chemical Industries Limited
    Inventors: Jean Bowler, Keith Blakeney Mallion, Dora Nellie Richardson
  • Patent number: 3959273
    Abstract: 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: Grant
    Filed: September 27, 1974
    Date of Patent: May 25, 1976
    Assignee: Imperial Chemical Industries Limited
    Inventors: Keith Blakeney Mallion, Ralph William Turner, Alexander Henry Todd
  • Patent number: 3935240
    Abstract: 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: Grant
    Filed: October 26, 1973
    Date of Patent: January 27, 1976
    Assignee: Imperial Chemical Industries Limited
    Inventor: Keith Blakeney Mallion
  • Patent number: 3931206
    Abstract: 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: Grant
    Filed: September 14, 1973
    Date of Patent: January 6, 1976
    Assignee: Imperial Chemical Industries Limited
    Inventors: Jean Bowler, Keith Blakeney Mallion, Dora Nellie Richardson