Abstract: Novel pyrroles, pyrazoles and triazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
Abstract: Novel pyridines, pyrimidines, pyrazines, pyridazines and triazines, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
Abstract: This invention relates to derivatives of furan and thiophene, their composition, process of making and method of use as endothelin receptor antagonists.
Type:
Grant
Filed:
February 2, 1998
Date of Patent:
January 25, 2000
Assignee:
SmithKline Beecham Corporation
Inventors:
John Duncan Elliott, Aiming Gao, Jia-Ning Xiang
Abstract: A compound of formula (I) or a salt thereof: ##STR1## wherein: P.sup.1 is pyridyl;P.sup.2 is phenyl;A is a bond or a chain of 1 to 5 atoms optionally substituted by C.sub.1-6 alkyl;R.sup.1 and R.sup.2 groups are each independently hydrogen, C.sub.1-6 alkyl optionally substituted by NR.sup.12 R.sup.13, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, cyano, halogen, CF.sub.3, NR.sup.12 R.sup.13, CHO, OCF.sub.3, COR.sup.14, CH.sub.2 OR.sup.14 or OR.sup.14 where R.sup.12, R.sup.13 and R.sup.14 are independently hydrogen or C.sub.1-6 alkyl;n and m are independently 0, 1 or 2;R.sup.3 is hydrogen or C.sub.1-6 alkyl;R.sup.4 is a group of formula (i): ##STR2## in which: R.sup.6 and R.sup.7 are independently hydrogen, C.sub.1-6 alkyl optionally substituted by one or more fluorine atoms, C.sub.1-6 alkylthio, C.sub.1-6 alkoxy or halogen.
Type:
Grant
Filed:
October 16, 1997
Date of Patent:
November 23, 1999
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Laramie Mary Gaster, Paul Adrian Wyman, Keith Raymond Mulholland, David Thomas Davies, David Malcolm Duckworth, Ian Thomson Forbes, Graham Elgin Jones
Abstract: The invention relates to heterocyclic families of compounds having pharmacological activity, in particular possessing 5HT.sub.2C receptor antagonist activity processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders.
Type:
Grant
Filed:
September 16, 1997
Date of Patent:
October 26, 1999
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Laramie Mary Gaster, Paul Adrian Wyman, Keith Raymond Mulholland, David Thomas Davies
Abstract: Novel furans and thiophenes, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
Abstract: This is a continuation of application Ser. No. 08/718,562, filed Sep. 30, 1996, which is a 371 of International Application No. PCT/US96/12581, filed Aug. 2, 1996; which claims the benefit of priority from the following provisional applications: 60/001,792, filed Aug. 2 1995 and 60/010,982, filed Feb. 1, 1996.
Type:
Grant
Filed:
July 23, 1998
Date of Patent:
October 19, 1999
Assignee:
SmithKline Beecham Corporation
Inventors:
Juan Ignacio Luengo, John Duncan Elliott
Abstract: Novel pyrroles, pyrazoles and triazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
Type:
Grant
Filed:
January 8, 1999
Date of Patent:
September 28, 1999
Assignee:
SmithKline Beecham Corporation
Inventors:
Juan Ignacio Luengo, John Duncan Elliott
Abstract: Novel pyridines, pyrimidines, pyrazines, pyridazines and triazines, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
Type:
Grant
Filed:
September 27, 1996
Date of Patent:
August 24, 1999
Inventors:
John Duncan Elliott, Deborah Lynne Bryan
Abstract: Dihydroisoindole compounds of formula (I), wherein the substituents are as defined herein, are disclosed as being useful as endothelin receptor antagonists. The compounds are applied in the treatment of cardiovascular and renal diseases.
Type:
Grant
Filed:
October 27, 1997
Date of Patent:
July 27, 1999
Assignee:
SmithKline Beecham Corporation
Inventors:
John Duncan Elliott, Robert Gene Franz, M. Amparo Lago, Aiming Gao
Abstract: Novel heterocyclic compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders are disclosed.
Type:
Grant
Filed:
June 30, 1997
Date of Patent:
July 13, 1999
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Ian Thomson Forbes, Graham Elgin Jones, Francis David King, Peter Ham, David Thomas Davies, Angela Moghe
Abstract: A method of enhancing amyloid precursor protein processing along a non-amyloidogenic pathway in patients suffering from, or at risk of developing, Alzheimer's disease and a method of treatment or prophylaxis of Alzheimer's disease by reducing .beta.A4 production in patients suffering from, or at risk of developing, Alzheimer's disease comprising administering to the patient an effective, non-toxic amount of an acetonitrile compound, use of the compound in preparation of a medicament for use in the method and a composition for use in the method.
Type:
Grant
Filed:
April 25, 1997
Date of Patent:
April 6, 1999
Inventors:
Roger Edward Markwell, Julie Hawkins, Carol Wendy Gray
Abstract: The invention relates to heterocyclic compounds of formula (I) having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders, wherein P represents phenyl, a quinoline or isoquinoline residue, or a 5 -membered or 6 -membered aromatic heterocyclic ring containing up to three heteroatoms selected from nitrogen, oxygen or sulphur; R.sup.3 is a group of formula (i) or (ii).
Abstract: The invention concerns compounds of the following formulae: ##STR1## wherein the variables are defined in the specification. The compounds are useful as endothelin receptor antagonists.
Abstract: The invention provides compounds of the general formula (I):A.sup.1 --B.sup.1 --X.sup.1 --(CH.sub.2).sub.m --(CON(R.sub.1)).sub.r --(CH.sub.2).sub.s --Y.sup.1 --(CH.sub.2).sub.s --(N(R.sub.1)CO).sub.r --(CH.sub.2).sub.n --X.sup.1 --B.sup.1 --A.sup.1The compounds of this invention are also illustrated by the Formula (II):A.sup.2 --B.sup.2 --X.sup.2 --(CH.sub.2).sub.m --(N(R.sub.1)CO).sub.r --(CH.sub.2).sub.s --Y.sup.2 --(CH.sub.2).sub.s --(CON(R.sub.1)).sub.r --(CH.sub.2).sub.n --X.sup.2 --B.sup.2 --A.sup.2The compounds have hemoregulatory activities and can be used to stimulate haematopoiesis and for the prevention and treatment of viral, fungal and bacterial infectious diseases.
Type:
Grant
Filed:
January 30, 1996
Date of Patent:
November 3, 1998
Assignees:
SmithKline Beecham Corporation, Nycomed Pharma AS
Inventors:
Pradip Kumar Bhatnagar, Dirk Heerding, Peter Martin Fischer