Patents by Inventor Alan C. White

Alan C. White 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: 4387230
    Abstract: Dihydropyridines of formula ##STR1## where R.sup.6 is lower alkyl and R.sup.5 is lower alkyl or aryl (lower)alkyl are prepared by a novel process from sodium or potassium salts of 1-substituted-1,6-dihydro-5-hydroxy-3[2H]-pyridones. The dihydropyridines are useful as intermediates for pharmacologically active 1-optionally substituted-3-phenyl or substituted phenylpiperidin-5-ols and esters. Some of the piperidinols and esters are novel; those where the 1-substituent is aryl(lower)alkyl are intermediates, those where the 1-substituent is cycloalkyl(lower)alkyl are analgesics or antidepressants and those in which the 1-position is unsubstituted are anti-secretory agents.
    Type: Grant
    Filed: August 20, 1981
    Date of Patent: June 7, 1983
    Assignee: John Wyeth and Brother Limited
    Inventors: Alan C. White, Robin G. Shepherd
  • Patent number: 4387097
    Abstract: Morpholine derivatives of the formula ##STR1## and their acid addition salts, wherein n represents 1, 2 or 3, R.sup.4 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl(lower)alkyl, 2-tetrahydrofurylmethyl or cyclo(lower)alkylmethyl, R.sup.2 and R.sup.3 are each hydrogen or alkyl of 1 to 10 carbon atoms and OR.sup.5 is hydroxy, acyloxy or a protected hydroxy group possess analgesic and/or opiate antagonistic activity or are useful as intermediates for other compounds of formula I possessing such activity.
    Type: Grant
    Filed: March 11, 1982
    Date of Patent: June 7, 1983
    Assignee: John Wyeth and Brother Limited
    Inventors: Alan C. White, Gerald Bradley
  • Patent number: 4360519
    Abstract: Morpholine derivatives of the formula ##STR1## and their pharmaceutically acceptable acid addition salts[wherein R.sup.1 represents lower alkyl. R.sup.2 represents hydrogen, lower alkyl, benzyl, lower alkoxymethyl or an acyl group; R.sup.3 represents hydrogen, lower alkyl or phenyl; R.sup.4, R.sup.5 and R.sup.6 are independently hydrogen or lower alkyl and R.sup.7 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl(lower)alkyl, tetrahydrofurylmethyl or cycloalkylmethyl] possess analgesic and/or opiate antagonistic activity.
    Type: Grant
    Filed: October 3, 1980
    Date of Patent: November 23, 1982
    Assignee: John Wyeth & Brother Limited
    Inventors: Alan C. White, Edwin T. Edington
  • Patent number: 4318909
    Abstract: Novel benzoxazocines of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R.sup.1 represents hydrogen, or one or more halogen, trifluoromethyl, lower alkyl, lower alkoxy, nitro, amino acylamino, mono- or di- (lower)alkyl-amino or cyano substituents, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each represent hydrogen or lower alkyl or R.sup.3 and R.sup.4 together represent --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, R.sup.5 represents hydrogen, lower alkyl, phenyl (lower)alkyl or cycloalkyl (lower)alkyl, and Ar is a phenyl radical optionally substituted by one or more halogen, trifluoromethyl, lower alkyl, lower alkoxy, nitro or amino groups exhibit activity on the central nervous system, particularly as antidepressants. The compounds can be prepared from novel alcohols of formula (II) ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Ar are as defined above and X is fluorine, chlorine or bromine.
    Type: Grant
    Filed: December 8, 1980
    Date of Patent: March 9, 1982
    Assignee: John Wyeth & Brother Limited
    Inventors: Alan C. White, Robin G. Shepherd
  • Patent number: 4296029
    Abstract: 2-Oxo-hexahydroazepine, -piperidine or pyrrolidines of formula ##STR1## wherein n is 2,3 or 4, R is hydrogen, lower alkyl, aryl(lower)alkyl, loweralkenylmethyl or cycloalkylmethyl, R.sup.1 is hydrogen or lower alkyl and R.sup.2 is hydrogen, lower alkyl or aryl(lower)alkyl are prepared by a novel process involving reaction of an anion of a lactam of formula ##STR2## where R.sup.3 is lower alkyl, aryl(lower)alkyl, trialkyl-, triaryl- or triarylalkyl-silyl with a benzyne of formula ##STR3## where R.sup.4 is lower alkyl, aryl(lower)alkyl or trialkyl-, triaryl- or triarylalkyl-silyl. The products are useful as intermediates for preparing pharmacologically active 2-unsubstituted -hexahydroazepine, -piperidine and pyrrolidine derivatives.
    Type: Grant
    Filed: June 23, 1980
    Date of Patent: October 20, 1981
    Assignee: John Wyeth & Brother Limited
    Inventors: Brian J. Bushell, John F. Cavalla, Robin G. Shepherd, Alan C. White
  • Patent number: 4272628
    Abstract: New 4-pyridinamine derivatives having the formula ##STR1## and their pharmaceutically acceptable acid addition salts, [wherein one of R.sup.1 and R.sup.2 is aryl or heteroaryl, the other of R.sup.1 and R.sup.2 is lower alkyl, R.sup.3 and R.sup.4 are independently hydrogen or lower alkyl, and n is 0 or 1] are described. They show CNS activity and may used as antidepressant drugs. N-([.alpha.-Phenyl]-n-propyl)-4-pyridinamine also shows anti-ulcer activity.
    Type: Grant
    Filed: June 22, 1979
    Date of Patent: June 9, 1981
    Assignee: John Wyeth & Brother Limited
    Inventors: Edwin T. Edington, Alan C. White
  • Patent number: 4271304
    Abstract: Pyridine derivatives having the formula ##STR1## and their N-oxides and pharmaceutically acceptable acid addition salts, wherein R.sup.1 and R.sup.2 are independently aryl, R.sup.3 is hydrogen or lower alkyl and n is 0, 1 or 2, have CNS activity and may be used as antidepressants.
    Type: Grant
    Filed: May 9, 1979
    Date of Patent: June 2, 1981
    Assignee: John Wyeth & Brother, Ltd.
    Inventors: Edwin T. Edington, Alan C. White
  • Patent number: 4248876
    Abstract: The invention concerns novel piperidine derivatives of the formula (I) ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein R.sup.1 represents (lower)alkyl, R.sup.2 represents a phenyl group optionally substituted by one or more (lower)alkyl, (lower)alkoxy, halogen, amino, (lower)alkylamino, di(lower)alkylamino or trifluoromethyl substituents and X represents=O; ##STR2## [where R.sup.3 and R.sup.4 both represent hydrogen, both represent the same (lower)alkyl or one is hydrogen and the other is (lower)alkyl or R.sup.3 and R.sup.4 together represent an alkylene group such that the ##STR3## is a cyclic ketal group containing 2 or 3 carbon atoms]; or ##STR4## [where OR is hydroxy, etherified hydroxy or esterified hydroxy]. The compounds possess anti-depressant activity.
    Type: Grant
    Filed: January 3, 1978
    Date of Patent: February 3, 1981
    Assignee: John Wyeth & Brother Ltd.
    Inventor: Alan C. White
  • Patent number: 4243808
    Abstract: Novel 4-pyridinamine derivatives having the formula ##STR1## and their pharmaceutically acceptable acid addition salts (wherein A is C.sub.1 to C.sub.4 alkylene, each of B.sub.1 and B.sub.2, together with the two carbon atoms joined thereto, forms arylene or heteroarylene, R.sub.3 and R.sub.4 are independently hydrogen or lower alkyl and n is 0 or 1) are described. They show CNS activity and may be used as anti-depressant drugs.
    Type: Grant
    Filed: June 22, 1979
    Date of Patent: January 6, 1981
    Assignee: John Wyeth & Brother Limited
    Inventors: Edwin T. Edington, Alan C. White
  • Patent number: 4197239
    Abstract: The invention concerns novel 2-oxo-hexahydroazepine, -piperidine and -pyrrolidine of formula I ##STR1## where n is 2,3 or 4, R is hydrogen, lower alkyl or aryl(lower)alkyl and R.sup.1 is lower alkyl. The compounds may be aromatized and the aromatized compounds converted to 3,3-disubstituted-hexahydroazepine, -piperidine and -pyrrolidine compounds having pharmacological activity, particularly analgesic activity.
    Type: Grant
    Filed: November 15, 1978
    Date of Patent: April 8, 1980
    Assignee: John Wyeth & Brother Limited
    Inventors: John F. Cavalla, Alan C. White, Robin G. Shepherd
  • Patent number: 4197241
    Abstract: The invention concerns novel 2-oxo-hexahydroazepine, -piperidine and -pyrrolidine derivatives of formula (I) and their aromatized derivatives of formula (II) ##STR1## where n is 2, 3 or 4, R is hydrogen, lower alkyl or aryl(lower)alkyl, R.sup.2 is hydrogen, lower alkyl or aryl(lower)alkyl and R.sup.3 is hydrogen, lower alkyl, aryl(lower)alkyl, lower alkenyl or lower alkynyl. The compounds are useful as intermediates for preparing 3,3-disubstituted -hexahydroazepine, -piperidine and -pyrrolidine compounds having pharmacological activity, particularly analgesic activity.
    Type: Grant
    Filed: November 15, 1978
    Date of Patent: April 8, 1980
    Assignee: John Wyeth & Brother Limited
    Inventors: John F. Cavalla, Alan C. White
  • Patent number: 4180670
    Abstract: Novel 4-pyridinamine derivatives having the formula ##STR1## [where R.sup.1 and R.sup.2 are aryl or heteroaryl (optionally linked together by a lower alkylene bridge) or one of R.sup.1 and R.sup.2 is aryl or heteroaryl and the other of R.sup.1 and R.sup.2 is lower alkyl or ar(lower)alkyl, R.sup.3 and R.sup.4 are each hydrogen or lower alkyl and n is 0 or 1] and their non-toxic acid addition salts are described. They show CNS activity and may be used as antidepressant drugs. Some also show stimulant activity.Novel intermediates having the formula ##STR2## are also described.
    Type: Grant
    Filed: January 30, 1978
    Date of Patent: December 25, 1979
    Assignee: John Wyeth & Brother Limited
    Inventors: Edwin T. Edington, Alan C. White
  • Patent number: 4126683
    Abstract: The invention concerns novel fused ring indole derivatives of the formula ##STR1## and the pharmaceutically acceptable acid addition and quaternary ammonium salts thereof, wherein n represents 1 or 2 and R.sup.1 represents hydrogen, hydroxyl, lower alkyl, lower alkoxy, trifluoromethyl, halogen, amino or mono- or di-(lower)alkylamino. The compounds are useful as anti-depressant agents.
    Type: Grant
    Filed: June 8, 1977
    Date of Patent: November 21, 1978
    Assignee: John Wyeth & Brother Limited
    Inventors: Alan C. White, Robert F. Sugden
  • Patent number: 4073906
    Abstract: The invention relates to pyrimido 1,2-b!isoquinolines of the formula ##STR1## and their pharmaceutically acceptable acid addition salts. In the formula, R.sup.1 and R.sup.2 each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, trifluoromethyl, halogen, amino or mono- or di-(lower)alkylamino and R.sup.3 and R.sup.4 each represent hydrogen or lower alkyl. The compounds have utility as anti-gastric ulcer agents.
    Type: Grant
    Filed: November 5, 1975
    Date of Patent: February 14, 1978
    Assignee: John Wyeth & Brother Limited
    Inventors: Alan C. White, Robin M. Black