Patents by Inventor David C. Humber

David C. Humber 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: 5578628
    Abstract: The invention relates to the use of compounds of the general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.-7 cycloalkyl-(C.sub.1-4) alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-C.sub.1-3 alkyl group; and one of the groups represented byR.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkynyl, C.sub.2-6 alkenyl or phenyl-C.sub.1-3 alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; and physiologically acceptable salts and solvates thereof, for the relief of nausea and vomiting.
    Type: Grant
    Filed: March 30, 1990
    Date of Patent: November 26, 1996
    Assignee: Glaxo Group Limited
    Inventors: Michael B. Tyers, Ian H. Coates, David C. Humber, George B. Ewan, James A. Bell
  • Patent number: 5240954
    Abstract: The invention relates to the use of compounds of the general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4) alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-C.sub.1-3 alkyl group; and one of the groups represented byR.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl-C.sub.1-3 alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; and physiologically acceptable salts and solvates thereof, for the relief of nausea and vomiting and/or the promotion of gastric emptying and for the manufacture of a medicament for this purpose. Promotion of gastric emptying may be for the relief of gastro-intestinal disorders associated with gastric stasis or may be of advantage in radiological examination procedures.
    Type: Grant
    Filed: December 9, 1991
    Date of Patent: August 31, 1993
    Assignee: Glaxo Group Limited
    Inventors: Michael B. Tyers, Ian H. Coates, David C. Humber, George B. Ewan, James A. Bell
  • Patent number: 5202343
    Abstract: The invention relates to compounds of the general formula (I): ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 ;R.sup.5 and R.sup.6, which may be the same or different, each represents a hydrogen atom, a C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl group, or a phenyl or phenylC.sub.1-4 alkyl group, in which the phenyl group is optionally substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy groups or halogen atoms, with the proviso that R.sup.5 does not represent a hydrogen atom when R.sup.1 represents a group --CO.sub.2 R.sup.5 or --SO.sub.2 R.sup.5 ;one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.
    Type: Grant
    Filed: May 22, 1992
    Date of Patent: April 13, 1993
    Assignee: Glaxo Group Limited
    Inventors: Ian H. Coates, John Bradshaw, James A. Bell, David C. Humber, George B. Ewan, William L. Mitchell, Barry J. Price
  • Patent number: 4957609
    Abstract: The invention relates to a process for the preparation of compounds of general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4)alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-(C.sub.1-3)alkyl group, and one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl-phenyl-(C.sub.1-3)alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; or a salt or protected derivative thereof by cyclization of a compound of general formula (II) ##STR2## wherein X represents a hydrogen atom or a halogen atom and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined above, or a salt or a protected derivative thereof.The compounds of formula (I) are potent and selective antagonists at "neuronal" 5-hydroxytryptamine receptors.
    Type: Grant
    Filed: February 21, 1989
    Date of Patent: September 18, 1990
    Assignee: Glaxo Group Limited
    Inventors: Neil Godfrey, Ian H. Coates, James A. Bell, David C. Humber, George B. Ewan
  • Patent number: 4939144
    Abstract: The invention relates to ketones of the general formula (I): ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenyl C.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;n represents 1, 2 or 3;Q represents a hydrogen atom, a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenyl C.sub.1-3 alkoxy or C.sub.1-6 alkyl group, or a group --NR.sup.4 R.sup.5 or --CONR.sup.4 R.sup.5, (wherein R.sup.4 and R.sup.5, which may be the same or different, each represents a hydrogen atom or a C.sub.1-4 alkyl or C.sub.
    Type: Grant
    Filed: October 21, 1988
    Date of Patent: July 3, 1990
    Assignee: Glaxo Group Limited
    Inventors: Ian H. Coates, David C. Humber, James A. Bell, George B. Ewan, Alexander W. Oxford, William L. Mitchell
  • Patent number: 4929632
    Abstract: The invention relates to the use of compounds of the general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4) alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-C.sub.1-3 alkyl group; and one of the groups represented byR.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl - C.sub.1-3 alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; and physiologically acceptable salts and solvates thereof, for the relief of nausea and vomiting and/or the promotion of gastric emptying and for the manufacture of a medicament for this purpose. Promotion of gastric emptying may be for the relief of gastro-intestinal disorders associated with gastric stasis or may be of advantage in radiological examination procedures.
    Type: Grant
    Filed: April 4, 1988
    Date of Patent: May 29, 1990
    Assignee: Glaxo Group Limited
    Inventors: Michael B. Tyers, Ian H. Coates, David C. Humber, George B. Ewan, James A. Bell
  • Patent number: 4859662
    Abstract: The invention relates to compounds of the general formula (I): ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and the various substituents are defined hereinbelow. The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety, and nausea and vomiting.
    Type: Grant
    Filed: December 7, 1988
    Date of Patent: August 22, 1989
    Assignee: Glaxo Group Limited
    Inventors: Ian H. Coates, John Bradshaw, James A. Bell, David C. Humber, George B. Ewan, William L. Mitchell, Barry J. Price
  • Patent number: 4822881
    Abstract: The invention relates to compounds of the general formula (I): ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and the various substituents are defined hereinbelow. The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety, and nausea and vomiting.
    Type: Grant
    Filed: November 27, 1987
    Date of Patent: April 18, 1989
    Assignee: Glaxo Group Limited
    Inventors: Ian H. Coates, John Bradshaw, James A. Bell, David C. Humber, George B. Ewan, William L. Mitchell
  • Patent number: 4814344
    Abstract: The invention relates to compounds of formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-10 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, phenyl, or phenyl C.sub.1-3 alkyl, --CO.sub.2 R.sup.10, --COR.sup.10, --CONR.sup.10 R.sup.11 or --SO.sub.2 R.sup.10 (wherein R.sup.10 and R.sup.11, which may be the same or different, each represents a hydrogen atom, a C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl group, or a phenyl or phenylC.sub.1-4 alkyl group, in which the phenyl group is optionally substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy groups or halogen atoms, with the proviso that R.sup.10 does not represent a hydrogen atom when R.sup.1 represents a group --CO.sub.2 R.sup.10 or --SO.sub.2 R.sup.10);R.sub.2 represents a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-7 cycloalkyl, phenyl or phenyl C.sub.1-3 alkyl group;R.sub.3 and R.sub.
    Type: Grant
    Filed: October 2, 1987
    Date of Patent: March 21, 1989
    Assignee: Glaxo Group Limited
    Inventors: David C. Humber, Ian H. Coates, James A. Bell, George B. Ewan
  • Patent number: 4753789
    Abstract: The invention relates to the use of compounds of the general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycoalkyl-(C.sub.1-4) alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-C.sub.1-3 alkyl group, and one of the groups represented byR.sup.2,R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl - C.sub.1-3 alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;and physiologically acceptable salts and solvates thereof, for the relief of nausea and vomiting and/or the promotion of gastric emptying and for the manufacture of a medicament for this purpose. Promotion of gastric emptying may be for the relief of gastro-intestinal disorders associated with gastric stasis or may be of advantage of radiological examination procedures.
    Type: Grant
    Filed: June 24, 1986
    Date of Patent: June 28, 1988
    Assignee: Glaxo Group Limited
    Inventors: Michael B. Tyers, Ian H. Coates, David C. Humber, George B. Ewan, James A. Bell
  • Patent number: 4749718
    Abstract: The invention relates to compounds of the general formula (I): ##STR1## wherein R.sup.1 represents a group CO.sub.2 R.sup.5, COR.sup.5, CONR.sup.5 R.sup.6 or SO.sub.2 R.sup.5 (wherein R.sup.5 and R.sup.6, which may be the same or different, each represents a hydrogen atom, a C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl group, or a phenyl or phenyl-(C.sub.1-4)alkyl group in which the phenyl group is optionally substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy groups or halogen atoms, with the proviso that R.sup.5 does not represent a hydrogen atom when R.sup.1 represents a group CO.sub.2 R.sup.5 or SO.sub.2 R.sup.5);and one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl-(C.sub.1-3)alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; and physiologically acceptable salts and solvates thereof.
    Type: Grant
    Filed: July 23, 1986
    Date of Patent: June 7, 1988
    Assignee: Glaxo Group Limited
    Inventors: Ian H. Coates, James A. Bell, David C. Humber, George B. Ewan
  • Patent number: 4739072
    Abstract: The invention relates to a process for the preparation of a compound of general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4)alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-(C.sub.1-3)alkyl group, and one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl-(C.sub.1-3)alkyl group and each of the other two groups, which may be the same or different, represent a hydrogen atom or a C.sub.1-6 alkyl group;or a salt or protected derivative thereof, by cyclization of a compound of general formula (II) ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined above, or a salt or a protected derivative thereof.The compounds of formula (I) are potent and selective antagonists at "neuronal" 5-hydroxytryptamine receptors.
    Type: Grant
    Filed: July 23, 1986
    Date of Patent: April 19, 1988
    Assignee: Sanofi
    Inventors: Alexander W. Oxford, Colin D. Eldred, Ian H. Coates, James A. Bell, David C. Humber, George B. Ewan
  • Patent number: 4725615
    Abstract: The invention relates to compounds of the general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4)-alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-(C.sub.1-3)alkyl group;one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl-(C.sub.1-3)alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; and X represents a halogen atom or a hydroxy, C.sub.1-4 alkoxy, phenyl-(C.sub.1-3)-alkoxy or C.sub.1-6 alkyl group or a group NR.sup.5 R.sup.6 or CONR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6, which may be the same or different, each represents a hydrogen atom or a C.sub.1-4 alkyl or C.sub.
    Type: Grant
    Filed: July 23, 1986
    Date of Patent: February 16, 1988
    Assignee: Glaxo Group Limited
    Inventors: Ian H. Coates, James A. Bell, David C. Humber, George B. Ewan
  • Patent number: 4695578
    Abstract: The invention relates to compounds of formula (I). ##STR1## wherein R.sub.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, C.sub.3-7 cycloalkyl-(C.sub.1-4) alkyl, C.sub.3-10 alkynyl, phenyl or phenyl-C.sub.1-3 alkyl group, and one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl-(C.sub.1-3) alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; and physiologically acceptable salts and solvates, e.g. hydrates thereof.The compounds are potent selective antagonists at "neuronal" 5-hydroxytryptamine receptors and are useful in the treatment of migraine and psychotic disorders such as schizophrenia.
    Type: Grant
    Filed: November 17, 1986
    Date of Patent: September 22, 1987
    Assignee: Glaxo Group Limited
    Inventors: Ian H. Coates, James A. Bell, David C. Humber, George B. Ewan
  • Patent number: 4515786
    Abstract: R.sup.3 is a C.sub.1-6 alkyl group or a C.sub.3-7 cycloalkyl group; andR.sup.4 is a group --OR.sup.5 or --OCOR.sup.6 whereR.sup.5 is an optionally substituted alkyl or alkenyl group which may contain up to 6 carbon atoms, an optionally substituted C.sub.3-7 cycloalkyl group, a phenyl group or a carbon-attached 5-7 membered heterocyclic ring in which the hetero-atom is selected from nitrogen, oxygen and sulphur, andR.sup.6 is a hydrogen atom or a group R.sup.5 as defined above;provided that when the compounds contain a 5.beta.-hydrogen atom, R.sup.2 is a hydrogen atom and salts thereof, which compounds have activity as antidysthythmic agents.
    Type: Grant
    Filed: June 30, 1983
    Date of Patent: May 7, 1985
    Assignee: Glaxo Group Limited
    Inventors: Gordon H. Phillipps, David C. Humber, George B. Ewan, Barry A. Coomber
  • Patent number: 4497805
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a C.sub.1-8 alkyl group or a C.sub.3-7 cycloalkyl group;R.sup.2 is a C.sub.1-6 alkyl group or a C.sub.3-7 cycloalkyl group;R.sup.3 is a hydroxy group or a group of formula --OR.sup.4 or --OCOR.sup.5 whereR.sup.4 is an alkyl or alkenyl group which may contain up to 6 carbon atoms (or such a group substituted by halogen, C.sub.1-6 alkoxy, carboxyl, phenyl, phenyl substituted by nitro, halo, C.sub.1-4 alkoxy or C.sub.1-4 alkyl), a C.sub.3-7 cycloalkyl group, a phenyl group (or such a group substituted by nitro, halo, C.sub.1-4 alkoxy or C.sub.1-4 alkyl), or a carbon-attached 5-7 membered heterocyclic ring in which the hetero atom is selected from nitrogen, oxygen and sulphur, andR.sup.5 is a hydrogen atom or a group R.sup.4 as defined above;and the D-homo analogues thereof having the group --CO.sub.2 R.sup.2 (wherein R.sup.2 is as defined above) at the 17a.beta.
    Type: Grant
    Filed: March 16, 1983
    Date of Patent: February 5, 1985
    Assignee: Glaxo Group Limited
    Inventors: Gordon H. Phillipps, David C. Humber, George B. Ewan, Barry A. Coomber, Anthony J. Pateman
  • Patent number: 4451405
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a C.sub.1-8 alkyl group or a C.sub.3-7 cycloalkyl group, and R.sup.2 is a C.sub.1-6 alkyl group or a C.sub.3-6 cycloalkyl group and the D-homo analogues thereof having the group --CO.sub.2 R.sup.2 (wherein R.sup.2 is as defined above) at the 17.alpha..beta.-position, and acid addition salts thereof have activity as antidysthythmic agents and may be applicable for the treatment of dysrthymias in humans or animals. The compounds may be provided in the form of compositions in admixture with pharmaceutical carriers and excipients and may be prepared by a variety of processes known for producing steroids of this type. The invention also provides intermediates for the preparation of the compounds of formula (I) wherein R.sup.2 and/or R.sup.1 are replaced with hydrogen atoms, and processes for the preparation of such intermediates.
    Type: Grant
    Filed: December 6, 1982
    Date of Patent: May 29, 1984
    Assignee: Glaxo Group Limited
    Inventors: Gordon H. Phillipps, David C. Humber, David B. Ewan, Barry A. Coomber
  • Patent number: 4353898
    Abstract: Compounds of formula ##STR1## wherein: R.sup.1 is a C.sub.1-8 alkyl group or a C.sub.3-7 cycloalkyl group;R.sup.2 is a hydrogen atom, a C.sub.1-6 alkoxy group or a C.sub.2-5 alkanoyloxy group; andR is a C.sub.1-8 alkyl group or a C.sub.3-7 cycloalkyl group;provided that when the compounds contain a 5.beta.-hydrogen atom, R.sup.2 is a hydrogen atom, and the D-homo analogues thereof having the group --CO.sub.2 R.sup.3 (wherein R.sup.3 is as defined above) at the 17a.beta.-position, and salts thereof have activity as antidysrhythmic agents and may be applicable for treatment of ventricular dysrhythmias in humans or animals. The compounds may be provided in the form of compositions in admixture with pharmaceutical carriers and excipients and may be prepared by a variety of processes known for producing steroids of this type. The invention also provides intermediates for the preparation of the compounds of formula (I), wherein R.sup.3 and/or R.sup.
    Type: Grant
    Filed: July 15, 1981
    Date of Patent: October 12, 1982
    Assignee: Glaxo Group Limited
    Inventors: Gordon H. Phillipps, David C. Humber, George B. Ewan, Barry A. Coomber
  • Patent number: 4352798
    Abstract: Compounds of formula ##STR1## (wherein): R.sup.1 is a hydrogen atom, a C.sub.1-8 alkyl group or a C.sub.3-7 cycloalkyl group; andR.sup.2 is a hydrogen atom, a C.sub.1-6 alkyl group or a C.sub.3-6 cycloalkyl group; and the D-homo analogues thereof having the group --CO.sub.2 R.sup.2 (wherein R.sup.2 is as defined above) at the 17a.beta.-position and salts and zwitterionic forms thereof have activity as antidysrhythmic agents and may be applicable for treatment of ventricular dysrhythmias in humans or animals. The compounds may be provided in the form of compositions in admixture with pharmaceutical carriers and excipients and may be prepared by a variety of processes known for producing steroids of this type.
    Type: Grant
    Filed: July 15, 1981
    Date of Patent: October 5, 1982
    Assignee: Glaxo Group Limited
    Inventors: Gordon H. Phillipps, David C. Humber, George B. Ewan, Barry A. Coomber
  • Patent number: 4284767
    Abstract: A process for the preparation of a 3-carbamoyloxymethyl cephalosporin compound which comprises reacting a 3-hydroxymethyl cephalosporin with dihalophosphinyl isocyanate and converting the resulting 3-phosphonocarbamoyloxymethyl cephalosporin reaction product by hydrolysis to the desired compound. The isocyanates used in the process are readily available and easy to handle and thus the process avoids the use of hazardous and/or expensive reagents.
    Type: Grant
    Filed: January 15, 1980
    Date of Patent: August 18, 1981
    Assignee: Glaxo Group Limited
    Inventors: David C. Humber, Stuart B. Laing, Gordon G. Weingarten