Patents Assigned to Wyeth
  • Patent number: 4900750
    Abstract: This invention concerns compounds of formula ##STR1## or salts thereof, wherein: Ar is an optionally substituted aryl radical;R represents hydrogen or an optionally substituted alkyl, aralkyl, or aryl group;R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen and saturated or unsaturated, cyclic or acyclic aliphatic hydrocarbon residues optionally substituted by one or more groups selected from halogen, OH, carboxy, CN, alkoxy, alkylthio, aryloxy, alkoxycarbonyl, amino, substituted amino, and optionally substituted aryl;A and B independently represent a group of formula --XR.sup.3 whereinX is a group of formula --(CHR.sup.6).sub.p Y(CHR.sup.7).sub.q --whereinY represents --O--, --S--, --NR.sup.8 -- or a direct bond; p and q each represent 0, 1 or 2 providing that p and q do not both represent O when Y is a direct bond; and R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or alkyl; and R.sup.
    Type: Grant
    Filed: August 3, 1987
    Date of Patent: February 13, 1990
    Assignee: John Wyeth & Brother, Limited
    Inventors: John L. Archibald, Terence J. Ward, Albert Opalko
  • Patent number: 4889936
    Abstract: The invention concerns a process for preparng a thiazolo[3,2-a]benzimidazole of formula I ##STR1## in which formula n is 1 or 2, and R.sub.1 is hydrogen, lower alkyl, lower alkoxy, trifluoromethyl or halo, or a salt thereof which comprises dehydrating a compound of formula II, ##STR2## or a salt thereof wherein n and R, are a defined above, and COOR is an acid or ester function in the presence of an acid selected from sulphuric, sulphonic and phosphoric acid or mixtures thereof and if desired or required an inert solvent provided that if water is present then the amount of water is less than about 15% by volume of the acid, the reaction being carried out with heating if necessary.
    Type: Grant
    Filed: January 10, 1989
    Date of Patent: December 26, 1989
    Assignee: John Wyeth & Brotyher Limited
    Inventors: Robin G. Shepherd, Sie-Yearl Chai, Maynard E. Lichty, Arnold S. Milowsky
  • Patent number: 4889846
    Abstract: The invention concerns azo compounds of formula ##STR1## or a salt thereof, in which formula R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are each independently hydrogen or lower alkyl, R.sup.7 and R.sup.8 are each independently alkyl of 1 to 7 carbon atom or cycloalkyl of 5 to 7 carbon atoms optionally substituted by lower alkyl which possess anti-inflammatory activity.
    Type: Grant
    Filed: April 15, 1988
    Date of Patent: December 26, 1989
    Assignee: John Wyeth & Brother Limited
    Inventor: Roger Crossley
  • Patent number: 4873237
    Abstract: The invention relates to a method of treatment of ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--(CHR.sup.5).sub.n --CHR.sup.6 -- (Ia)R represents an optionally substituted aryl or heteroaryl radical,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent and said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur;R.sup.5 and R.sup.
    Type: Grant
    Filed: May 22, 1986
    Date of Patent: October 10, 1989
    Assignee: John Wyeth & Brother Limited
    Inventor: Roger Crossley
  • Patent number: 4866075
    Abstract: The invention concerns compounds of formula: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, halogen, lower alkoxy or hydroxy; R.sub.2 represents hydrogen or lower alkyl; A represents an alkylene, oxoalkylene or hydoxyalkylene chain each having 2 to 6 carbon atoms, R.sub.3 and R.sub.4 may be in the same or different rings and independently represent hydrogen, lower alkyl, lower alkoxy, amino or halogen and one of X and Y represents nitrogen the other represents CR.sub.5 wherein R.sub.5 is one of the values for R.sub.3 or R.sub.5 is the bond to the NHCO group; or a pharmaceutically acceptable salt thereof, which compounds possess antihypertensive activity whilst exhibiting reduced CNS depressant properties. Also disclosed are processes for preparing the compounds and pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 12, 1988
    Date of Patent: September 12, 1989
    Assignee: John Wyeth and Brother Limited
    Inventors: John L. Archibald, Terence J. Ward, Janet C. White
  • Patent number: 4812574
    Abstract: The invention concerns a process for preparing a thiazolo[3,2-a]benzimidazole of formula I ##STR1## in which formula n is 1 or 2, and R.sub.1 is hydrogen, lower alkyl, lower alkoxy, trifluoromethyl or halo, or a salt thereof which comprises dehydrating a compound of formula II, ##STR2## or a salt thereof wherein n and R, are as defined above, and COOR is an acid or ester function in the presence of an acid selected from sulphuric, sulphonic and phosphoric acid or mixtures thereof and if desired or required an inert solvent provided that if water is present then the amount of water is less than about 15% by volume of the acid, the reaction being carried out with heating if necessary.
    Type: Grant
    Filed: December 23, 1987
    Date of Patent: March 14, 1989
    Assignees: John Wyeth & Brother Ltd., American Home Products Corporation
    Inventors: Robin G. Shepherd, Sie-Yearl Chai, Maynard E. Lichty, Arnold S. Milowsky
  • Patent number: 4808715
    Abstract: Novel quinazoline and cinnoline derivatives having the formula ##STR1## (wherein one of A and B is CH and the other one of A and B is N; X.sub.1 is halogen or CF.sub.3 and X.sub.3 is one of the groups II, III, IV or V ##STR2## where Q is lower alkylene; R.sub.1 is hydrogen or lower alkyl; R.sub.2 and R.sub.3 are independently lower alkyl or R.sub.2 and R.sub.3 are a divalent radical such that HNR.sub.2 R.sub.3 is a secondary cyclic amine with 5 to 7 ring atoms; R.sub.4 is lower alkyl; n is 0 or 1; the rings shown in formulae III and IV are piperidine or pyrrolidine optionally substituted by lower alkyl; and the ring shown in formula V is piperazine optionally substituted by lower alkyl) and their pharmaceutically acceptable salts are useful as pharmaceuticals particularly as anti-hypertensives. Novel intermediates are also described including the corresponding sulphonic acids of formula I ( (where A, B and X.sub.1 are defined above and X.sub.3 is OH).
    Type: Grant
    Filed: January 6, 1988
    Date of Patent: February 28, 1989
    Assignee: John Wyeth & Brother Limited
    Inventors: John T. A. Boyle, Richard S. Todd
  • Patent number: 4806552
    Abstract: The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O, S, --CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --NM.dbd.N--; R.sup.4, R.sup.5 and R.sup.6 ; and R.sup.7 and R.sup.8 when present, each represent hydrogen or a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.
    Type: Grant
    Filed: November 12, 1986
    Date of Patent: February 21, 1989
    Assignee: John Wyeth & Brother, Limited
    Inventors: John L. Archibald, Terence J. Ward
  • Patent number: 4803207
    Abstract: Pyrimidoindoles of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R represents lower alkyl a mono- or bicyclic aryl radical or a group of mormula R.sup.3 O--B--[where R.sup.3 O is (lower)alkoxy,aryl(lower)alkoxy or hydroxy and B is a lower alkylene chain optionally containing one double or triple bond], R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, halo(lower)alkyl, halogen, amino or mono- or di(lower) alkylamino and A, together with the carbon atom to which it is attached, represents 5, 6 or 7 membered saturated carbocyclic or heterocyclic ring, are useful as hypoglyceamics.
    Type: Grant
    Filed: March 9, 1987
    Date of Patent: February 7, 1989
    Assignee: John Wyeth & Brother Ltd.
    Inventors: Alan C. White, Ian A. Cliffe, Richard S. Todd
  • Patent number: 4801007
    Abstract: A teat unit for insertion into a liquid container formed of a plastics/paper laminate comprises a tubular teat mounting having one end adapted for insertion through the liquid container and the other end adapted to receive a teat. Various methods of securing and sealing the unit to the container are disclosed.
    Type: Grant
    Filed: August 27, 1987
    Date of Patent: January 31, 1989
    Assignee: John Wyeth & Brother, Limited
    Inventor: Arthur W. T. Rule
  • Patent number: 4801595
    Abstract: The invention concerns compounds of formula: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, halogen, lower alkoxy or hydroxy; R.sub.2 represents hydrogen or lower alkyl; A represents an alkylene, oxoalkylene or hydroxyalkylene chain each having 2 to 6 carbon atoms, R.sub.3 and R.sub.4 may be in the same or different rings and independently represent hydrogen, lower alkyl, lower alkoxy, amino or halogen and one of X and Y represents nitrogen the other represents CR.sub.5 wherein R.sub.5 is one of the values for R.sub.3 or R.sub.5 is the bond to the NHCO group; or a pharmaceutically acceptable salt thereof, which compounds possess antihypertensive activity while exhibiting reduced CNS depressant properties. Also disclosed are processes for preparing the compounds and pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 15, 1986
    Date of Patent: January 31, 1989
    Assignee: John Wyeth & Brother Limited
    Inventors: John L. Archibald, Terence J. Ward, Janet C. White
  • Patent number: 4794123
    Abstract: This invention relates to a method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--CR.sup.5 .dbd.CR.sup.6 -- (Ib)or--(CHR.sup.5).sub.n --CR.sup.6 .dbd. (Ic);R represents an optionally substituted aryl or heteroaryl radical; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur. Novel compositions and compounds of formula I are also disclosed.
    Type: Grant
    Filed: October 13, 1987
    Date of Patent: December 27, 1988
    Assignee: John Wyeth & Brother Limited
    Inventors: Roger Crossley, Peter J. Meade
  • Patent number: 4789677
    Abstract: New compounds having the formula I ##STR1## where one of A and B is CH or N, the other of A and B is CH, Q is lower alkylene, R is lower alkyl, X.sub.1 is halogen or trifluoromethyl and X.sub.2 and X.sub.3 are independently selected from hydrogen, halogen, trifluoromethyl, lower alkoxy and lower alkyl and the pharmaceutically acceptable acid additions are disclosed as anti-hypertensive agents. New compounds having the formula II ##STR2## where Q, R, X.sub.2 and X.sub.3 are as explained above and n is 0 or 1 and their acid addition salts are useful as intermediates.
    Type: Grant
    Filed: September 2, 1987
    Date of Patent: December 6, 1988
    Assignee: John Wyeth and Brothers Limited
    Inventors: John T. A. Boyle, Richard S. Todd
  • Patent number: 4788202
    Abstract: The invention concerns sulphonamides of general formula ##STR1## and their pharmaceutically acceptable acid addition salts. In formula (I), R represents hydrogen or lower alkyl, R.sup.1 and R.sup.2 which may be the same or different each represents hydrogen, lower alkyl, lower alkoxy or halogen, R.sup.3 and R.sup.4 which may be the same or different each represents lower alkyl, halo(lower)alkyl or aryl, A represents a lower alkylene group having 1 to 3 carbon atoms in the chain between the two N atoms and X represents O, S or NR.sup.5 (where R.sup.5 is hydrogen or lower alkyl). The compounds possess .alpha..sub.2 -adrenoceptor antagonistic activity in warm blooded animals.
    Type: Grant
    Filed: July 9, 1987
    Date of Patent: November 29, 1988
    Assignee: John Wyeth & Brother Limited
    Inventor: Terence J. Ward
  • Patent number: 4786636
    Abstract: This invention relates to a method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 - represents a chain of formula--CR.sup.5 .dbd.CR.sup.6 -- (Ib)or--(CHR.sup.5).sub.n --CR.sup.6 .dbd. (Ic);R represents an optionally substituted aryl or heteroaryl radical; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur. Novel compositions and compounds of formula I are also disclosed.
    Type: Grant
    Filed: October 13, 1987
    Date of Patent: November 22, 1988
    Assignee: John Wyeth & Brother Limited
    Inventors: Roger Crossley, Peter J. Meade
  • Patent number: 4784996
    Abstract: Compounds of formula ##STR1## wherein A represents a lower alkylene chain optionally containing one double or triple bond, RO represents (lower)alkoxy, aryl(lower)alkoxy, hydroxy or protected hydroxy, R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, halo(lower)alkyl, halogen, amino or mono- or di(lower)alkylamino and R.sup.3 and R.sup.4 each independently represent hydrogen or lower alkyl and their pharmaceutically acceptable acid addition salts are useful as hypoglycaemics or as intermediates for hypoglycaemics.
    Type: Grant
    Filed: March 9, 1987
    Date of Patent: November 15, 1988
    Assignee: John Wyeth & Brother Ltd.
    Inventors: Alan C. White, Ian A. Cliffe, Richard S. Todd
  • Patent number: 4783455
    Abstract: Compounds of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R represents lower alkyl or a mono- or bicyclic aryl or heteroaryl radical, R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, halo(lower)alkyl, halogen, amino or mono- or di(lower)alkylamino, X represents--CH.sub.2 CR.sup.3 R.sup.4 CH.sub.2 --or --(CH.sub.2).sub.4 --where R.sup.3 and R.sup.4 each independently represent hydrogen or lower alkyl or R.sup.3 and R.sup.4 together with the carbon atom to which they are attached represent a 5, 6 or 7 membered carbocyclic ring and R.sup.5 represents acyl and R.sup.6 represents hydrogen or R.sup.5 and R.sup.6 each independently represent hydrogen or lower alkyl, are useful as hypoglycaemics.
    Type: Grant
    Filed: May 22, 1987
    Date of Patent: November 8, 1988
    Assignee: John Wyeth and Brother Ltd.
    Inventor: Ian A. Cliffe
  • Patent number: 4778802
    Abstract: The invention relates to compounds of formula ##STR1## or a salt thereof, wherein .dbd.X-- is .dbd.CH-- or .dbd.N--, R and R.sup.1 independently represent hydrogen, halogen or lower alkoxy and R.sup.2 is hydrogen or a substituent selected from halogen, lower alkyl, lower alkoxy or halolower alkyl which compounds exhibit psychotropic activity and are useful as antidepressants.
    Type: Grant
    Filed: November 12, 1986
    Date of Patent: October 18, 1988
    Assignee: John Wyeth & Brother, Ltd.
    Inventors: John L. Archibald, Terence J. Ward
  • Patent number: 4772617
    Abstract: The invention concerns indole derivatives of formula I ##STR1## in which R.sub.1 is hydrogen, lower alkyl, halogen, lower alkoxy or hydroxy,R.sub.2, R.sub.3 and R.sub.4 independently represent hydrogen or lower alkyl,A represents an alkylene, oxoalkylene or hydroxyalkylene chain each having 2 to 6 carbon atoms or a pharmaceutically acceptable salt thereof, which compounds possess antihypertensive activity while exhibiting reduced CNS depressant properties.Also disclosed are methods for preparing the compounds of formula I and pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 15, 1986
    Date of Patent: September 20, 1988
    Assignee: John Wyeth & Brother Limited
    Inventors: John L. Archibald, Terence J. Ward
  • Patent number: 4760158
    Abstract: Novel 3-halo-2,2-disubstituted propanenitriles of formula ##STR1## wherein Z represents bromo or chloro and A, together with the carbon atom to which it is attached, represents a 5,6 or 7 membered saturated carbocyclic or heterocyclic ring, are useful as intermediates for preparing substituted pyrimido[1,2-a]indoles. The intermediates can be prepared by a novel process which comprises condensing a 2,2-disubstituted ethanenitrile with a dihalomethane in the presence of a non-nucleophilic strong base.
    Type: Grant
    Filed: March 9, 1987
    Date of Patent: July 26, 1988
    Assignee: John Wyeth & Brother Limited
    Inventors: Ian A. Cliffe, Richard S. Todd