Patents by Inventor Harry J. Wadsworth

Harry J. Wadsworth 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: 5541194
    Abstract: Novel compounds of formula (I), processes for their preparation, and their use as pharmaceutical agents are described: ##STR1## in which p represents an integer of 2 to 4; r represents an integer of 1 or 2; s represents 0 or 1; and X represents a group ##STR2## in which A.sub.1 is oxygen or sulphur, one of A.sub.2 and A.sub.3 is CR.sub.1 and the other is nitrogen or CR.sub.2, or A.sub.2 is oxygen or sulphur, A.sub.1 is CH and A.sub.3 is CR.sub.1, where R.sub.1 and R.sub.2 are independently selected from hydrogen and C.sub.1-2 alkyl, with the proviso that when r is 2, R.sub.1 and R.sub.2 are hydrogen or methyl. The novel compounds of this invention may be used to treat or to prevent dementia in mammals.
    Type: Grant
    Filed: January 6, 1995
    Date of Patent: July 30, 1996
    Assignee: Beecham Group p.l.c.
    Inventors: Barry S. Orlek, Paul A. Wyman, Harry J. Wadsworth
  • Patent number: 5470859
    Abstract: A pharmaceutical composition useful to treating dementia which comprises a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which p is 1 and either m is 0 and n is 2 or 3 or m is 1 and n is 2, or p is 2, m is 0 and n is 2, and Z is a heterocyclic group ##STR2## in which Q represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises one or two heteroatoms selected from oxygen, nitrogen and sulphur, or three nitrogen atoms, any amino nitrogen being substituted by a C.sub.1-2 alkyl, cyclopropyl or propargyl group, and any ring carbon atom being optionally substituted by a group R.sub.1 ; or a group ##STR3## which A.sub.1, A.sub.2 and A.sub.3 complete a 5-membered aromatic ring and A.sub.1 is oxygen or sulphur, one of A.sub.2 and A.sub.3 is CR.sub.2 and the other is nitrogen or CR.sub.3, or A.sub.2 is oxygen or sulphur, one of A.sub.1 and A.sub.3 is CR.sub.2 and the other is CR.sub.3 ; and R.sub.1, R.sub.2 and R.sub.
    Type: Grant
    Filed: August 2, 1990
    Date of Patent: November 28, 1995
    Assignee: Beecham Group p.l.c.
    Inventors: Harry J. Wadsworth, Paul A. Wyman, Steven Dabbs, Sarah M. Jenkins
  • Patent number: 5217975
    Abstract: A compound of formula (I) useful for treating dementia or a pharmaceutically acceptable salt thereof: ##STR1## in which one of X and Y represents hydrogen and the other represents Z, where Z is a group in which Q represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises two or three nitrogen atoms, any amino nitrogen being substituted by a C.sub.1-2 alkyl, cyclopropyl or propargyl group, r represents the integer of 2 or 3, s represents an integer of 1 or 2 and t represents 0, with the proviso that when Y is hydrogen s is 1.
    Type: Grant
    Filed: June 4, 1990
    Date of Patent: June 8, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Harry J. Wadsworth, Sarah M. Jenkins
  • Patent number: 5091397
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which one of X and Y represents hydrogen and the other represents --CH.sub.2 --Z where Z is a group ##STR2## in which Q represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises one or two heteroatoms selected from oxygen, nitrogen and sulphur, or three nitrogen atoms, any amino nitrogen being optionally substituted by a C.sub.1-2 alkyl, cyclopropyl or propargyl group, and any ring carbon atom being optionally substituted by a group R.sub.1 ; or a group ##STR3## in which A.sub.1, A.sub.2 and A.sub.3 complete a 5-membered aromtic ring and A.sub.1 is oxygen or sulphur, one of A.sub.2 and A.sub.3 is CR.sub.2 and the other is nitrogen or CR.sub.3, or A.sub.2 is oxygen or sulphur, one of A.sub.1 and A.sub.3 is CR.sub.2 and the other is CR.sub.3 ; and R.sub.1, R.sub.2 and R.sub.3 are independently selected from hydrogen, halogen, CN, OR.sub.4, SR.sub.4, N(R.sub.4).sub.2, NHCOR.sub.4, NHCOOCH.sub.
    Type: Grant
    Filed: September 29, 1989
    Date of Patent: February 25, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Harry J. Wadsworth, Michael S. Hadley, Paul A. Wyman, Sarah M. Jenkins
  • Patent number: 4988706
    Abstract: Novel compounds of formula (I), processes for their preparation, and their use as pharmaceutical agents are described: ##STR1## in which X represents a group ##STR2## wherein one of Y and Z represents nitrogen and the other represents CR where R is selected from halogen, CN, OR.sup.1, SR.sup.1, N(R.sup.1).sub.2, NHR.sup.1, NHCOR.sup.1, NHCOOCH.sub.3, NHCOOC.sub.2 H.sub.5, NHOR.sup.1, NHNH.sub.2, COR.sup.1, COR.sup.2, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl or C.sub.1-2 alkyl substituted with OR.sup.1, N(R.sup.1).sub.2, SR.sup.1, CO.sub.2 R.sup.1, CON(R.sup.1).sub.2 or one or two halogen atoms, in which R.sup.1 is hydrogen or C.sub.1-2 alkyl and R.sup.2 is OR.sup.1, NH.sub.2 or NHR.sup.1 ; and each of p and q independently represents an integer of 2 to 4.
    Type: Grant
    Filed: April 13, 1989
    Date of Patent: January 29, 1991
    Assignee: Beecham Group P.L.C.
    Inventors: Michael S. Hadley, Barry S. Orlek, Paul A. Wyman, Harry J. Wadsworth
  • Patent number: 4968691
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which X represents a group ##STR2## in which p represents an integer of 2 to 4; r represents an integer of 1 or 2; s represents 0 or 1; and A represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises one or two heteroatoms selected from oxygen, nitrogen and sulphur, any amino nitrogen optionally substituted by a C.sub.1-4 alkyl group, and when (p,r,s) is (2,2,0) or (2,2,1) any A comprising 2 heteroatoms is optionally C-substituted by a methyl group, and when (p,r,s) is (2,1,0), (2,1,1) or (3,1,0) any A comprising 2 heteroatoms is optionally C-substituted by C.sub.1-2 alkyl and any A comprising one heteroatom is optionally C-substituted by a methyl group, and wherein compounds of formula (I) having two asymetric centers have the stereo-chemical configuration in which the group X and the (CH.sub.2).sub.
    Type: Grant
    Filed: March 7, 1989
    Date of Patent: November 6, 1990
    Assignee: Beecham Group P.L.C.
    Inventors: Barry S. Orlek, Michael S. Hadley, Howard E. Rosenberg, Harry J. Wadsworth
  • Patent number: 4870081
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which A represents a bond or --CH.sub.2 -- and B represents hydrogen, or A and B together with the carbon atom to which they are both attached represents a group ##STR2## R represents R.sub.1 OOC-- in which R.sub.1 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl; R.sub.2 O-- in which R.sub.2 is C.sub.1-3 alkyl, C.sub.1-2 alkylcarbonyl or aminocarbonyl optionally substituted by one or two methyl groups; or R.sub.3 CH.sub.2 - in which R.sub.3 is C.sub.1-2 alkoxy; and p represents an integer of 2 to 4, and wherein compounds of formula (I) where B is hydrogen have the stereochemical configuration in which the group R and the methylene bridge are both on the same side of the plane of the molecule which contains both bridge head atoms and the ring carbon atom bonded to the group R.
    Type: Grant
    Filed: June 26, 1987
    Date of Patent: September 26, 1989
    Assignee: Beecham Group p.l.c.
    Inventors: Barry S. Orlek, Michael S. Hadley, Harry J. Wadsworth, Howard E. Rosenberg
  • Patent number: 4681966
    Abstract: This invention relates to compounds of the formula ##STR1## wherein R.sub.1 represents lower alkyl, phenyl, or phenyl lower alkyl; R.sub.2 represents lower alkyl; and R.sub.5 represents lower alkyl. These compounds are useful as intermediates in the preparation of collagenase inhibiting compounds which are useful in the treatment of arthritis and are of the formula ##STR2## wherein R.sub.1 represents lower alkyl, phenyl or phenyl lower alkyl; R.sub.2 and R.sub.4 represent lower alkyl; and R.sub.3 represents lower alkyl, benzyloxyalkyl, alkoxybenzyl or benzyloxybenzyl wherein the oxyalkyl or alkoxy moiety contain 1 to 6 carbon atoms; and a, b, and c represent chiral centers with optional R or S stereochemistry.
    Type: Grant
    Filed: April 2, 1986
    Date of Patent: July 21, 1987
    Assignee: G. D. Searle & Co.
    Inventors: David K. Donald, Michael M. Hann, John Saunders, Harry J. Wadsworth
  • Patent number: 4595700
    Abstract: This invention relates to compounds of the formula: ##STR1## wherein R.sub.1 represents lower alkyl, phenyl or phenyl lower alkyl;R.sub.2 and R.sub.4 represent lower alkyl; andR.sub.3 represents lower alkyl, benzyloxyalkyl, alkoxybenzyl or benzyloxybenzyl wherein the oxyalkyl or alkoxy moiety contain 1 to 6 carbon atoms; and a, b, and c represent chiral centers with optional R or S stereochemistry. These compounds inhibit collagenase and are useful in the treatment of arthritis. Also disclosed are processes for manufacture of the compounds and pharmaceutical compositions containing them.
    Type: Grant
    Filed: February 21, 1985
    Date of Patent: June 17, 1986
    Assignee: G. D. Searle & Co.
    Inventors: David K. Donald, Michael M. Hann, John Saunders, Harry J. Wadsworth
  • Patent number: 4568666
    Abstract: This invention encompasses novel carboxyalkyl peptide derivatives which are collagenase inhibitors.
    Type: Grant
    Filed: October 18, 1984
    Date of Patent: February 4, 1986
    Assignee: G. D. Searle & Co.
    Inventors: Keith G. McCullagh, Harry J. Wadsworth, Michael M. Hann
  • Patent number: 4511504
    Abstract: This invention encompasses novel carboxyalkyl peptide derivatives which are collagenase inhibitors.
    Type: Grant
    Filed: April 12, 1984
    Date of Patent: April 16, 1985
    Assignee: G.D. Searle & Co.
    Inventors: Keith G. McCullagh, Harry J. Wadsworth, Michael M. Hann