Abstract: The present invention involves certain 8-ureido and 8-thioureido, 1,2-benzothiazines, 1,2,4-benzothioxazines and 1,2,4-benzothiodiazines useful in the treatment of disease states mediated by the chemokine, Interleukin-8.
Inventors:
Pradip Kumar Bhatnagar, Joelle Lorraine Burgess, James Francis Callahan, Raul Rolando Calvo, Eric G. Del Mar, Maria Amparo Lago, Thomas The Nguyen
Abstract: A compound according to Formula (I), hereinbelow:
wherein A represents a covalent bond, or a 1,2, 1,3 or 1,4-disubstituted aryl amine ring selected from the group consisting of:
wherein
R is independently selected from the group consisting of H, OMe, Cl, Br, F, NO2, and CN;
n is an integer from 1 to 4;
each X is independently selected from the group consisting of H, Br, CH3, NO2, CN, and NR1R2;
each Ar is independently optionally substituted phenyl or an optionally substituted 5 or 6 membered heterocyclic ring comprising one or more heteroatoms selected from N, O and S; and
R1 and R2 are, independently, hydrogen or C1-4 alkyl, branched or cyclic, optionally containing O or N.
Abstract: A method of treating ADHD comprising administering a 5-HT6 receptor antagonist according to formula (A) hereinbelow:
wherein:
P is phenyl, naphthyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulphur;
A is a single bond, a C1-6alkylene or a C1-6alkenylene group;
R1 is halogen, C1-6alkyl optionally substituted by one or more halogen atoms, C3-6cycloalkyl, C1-6alkoxy, OCF3, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, C1-6alkanoyl, nitro, amino, C1-6alkylamino or diC1-6alkylamino, cyano or R1 is phenyl, naphthyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulphur;
n is 0, 1, 2, 3, 4, 5 or 6,
R2 is hydrogen, C1-6 alkyl or aryl C1-6 alkyl;
R3 is a group R5 or together with R5 forms a group (CH2)2O or (CH2)3O or R3 is linked to R2 to form a group (CH2)2 or (CH2)3;
R4 is &mdash
Abstract: This invention relates to a process for making certain phenyl urea compounds by using a Lewis acid to effect the ring opening of a benzoxazolinone by an amine.
Type:
Grant
Filed:
February 27, 2001
Date of Patent:
April 16, 2002
Assignee:
SmithKline Beecham Corporation
Inventors:
Neil H. Baine, Ann Marie Eldridge, Marvin Sungwhan Yu
Abstract: The invention relates to compounds of formula (I) or a salt thereof
wherein X is CH or N; R1 is hydrogen or C1-6 alkyl; R2 and R3 groups are independently C1-6 alkyl, or trifluoromethyl, having pharmacological activity, processes for their preparation, compositions containing them and to their use in the treatment of CNS disorders such as anxiety.
Type:
Grant
Filed:
December 21, 1998
Date of Patent:
April 9, 2002
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Steven Mark Bromidge, Ian Thomson Forbes
Abstract: Heterocycle-condensed morphinoid derivatives of formula (I), or solvates or salts thereof,
are potent and selective delta opioid agonists and antagonists and are useful as i.a. analgesics. Pharmaceutical compositions containing such compounds, the use of such compounds as therapeutic agents, a method of treatment comprising the administration of such compounds, and a process for the preparation of such compounds are also described.
Type:
Grant
Filed:
February 22, 1999
Date of Patent:
April 2, 2002
Assignee:
SmithKline Beecham S.p.A.
Inventors:
Giulio Dondio, Silvano Ronzoni, Pier Andrea Gatti, Davide Graziani
Abstract: This invention relates to novel spiro compound derivatives of benzoisothiazolyl-urea and -thiourea and compositions thereof. These compounds are useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
Abstract: The invention relates to novel compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders.
Type:
Grant
Filed:
January 10, 2000
Date of Patent:
November 13, 2001
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Steven Mark Bromidge, Stephen Frederick Moss
Abstract: This invention relates to novel benzo-2-triazole substituted compounds, pharmaceutical compositions, processes for their preparation, and use thereof in treating IL-8, GRO&agr;, GRO&bgr;, GRO&ggr; and NAP-2 mediated diseases.
Type:
Grant
Filed:
July 9, 1999
Date of Patent:
October 9, 2001
Assignee:
SmithKline Beecham Corporation
Inventors:
Katherine L. Widdowson, Melvin C. Rutledge
Abstract: This invention relates to novel benzoisothiazole substituted compounds, pharmaceutical compositions, processes for their preparation, and use thereof in treating IL-8, GRO&agr;, GRO&bgr;, GRO&ggr;, ENA-78 and NAP-2 mediated diseases.
Abstract: Novel arylalkylamino compounds exhibiting calcilytic properties are provided.
Type:
Grant
Filed:
October 1, 1999
Date of Patent:
September 25, 2001
Assignee:
SmithKline Beecham Corporation
Inventors:
Robert M. Barmore, Pradip Kumar Bhatnagar, William M. Bryan, Joelle Lorraine Burgess, James Francis Callahan, Raul Rolando Calvo, Eric G. Del Mar, Maria Amparo Lago, Thomas The Nguyen, Derek Sheehan, Robert Lawrence Smith, Linda Sue Southall, Bradford C. Van Wagenen