Abstract: There are provided according to the invention novel compounds of formula (I)
wherein R1 represents C1-4alkyl or C3-8cycloalkyl, R2 represents C1-4alkyl or C3-4alkenyl, R3 represents hydrogen, C1-3alkyl or halogen, and R4 represents C1-6alkyl, processes for preparing them, pharmaceutical formulations containing them and their use in therapy particularly as thrombin inhibitors.
Type:
Grant
Filed:
January 10, 2002
Date of Patent:
December 30, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Henry Anderson Kelly, Martin Pass, David Neil Smith
Abstract: The invention relates to piperazine derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to their medical use. The novel compounds are antagonists of tachykinins, including substance P and other neurokinins.
Type:
Grant
Filed:
July 3, 2002
Date of Patent:
November 4, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Giuseppe Alvaro, Romano Di Fabio, Riccardo Giovannini, Giuseppe Guercio, Yves St-Denis, Antonella Ursini
Abstract: The present invention relates to novel amidino compound of formula (I):
to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use as selective inhibitors of inducible nitric oxide synthase.
Type:
Grant
Filed:
August 15, 2001
Date of Patent:
September 16, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Richard Mansfield Beams, Martin James Drysdale, Karl Witold Franzmann, Anthony Joseph Frend, Harold Francis Hodson, Richard Graham Knowles, Daryl David Rees, David Alan Sawyer
Abstract: The present invention relates to novel compounds of formula (I):
wherein
Z represents a 5 or 6 membered cycloalkyl, aryl, substituted cycloalkyl, or substituted aryl, said cycloalkyl, aryl, substituted cycloalkyl or substituted aryl optionally containing one or more heteroatoms selected from 0, N or S;
k represents 0 or 1;
n represents an integer of 1 to 50;
X represents —O—, —N(H)—, —N(C1-6alkyl)-, —N(C3-8cycloalkyl)-, —N(C1-8alkyl)(C3-8 cycloalkyl), —N[(CH2CH2O)m(C1-12 alkyl, aryl, or aralkyl)]-, —CH2O—, —CH2NH—, —CH2N(C1-6alkyl)-, —CH2N(C3-8cycloalkyl)-, or —C1-12alkyl-;
Q represents (—CH2)p, (—CH═CH—)p, (—C≡C—)p, (—(O)p1CH2—)p or (—CH2(O)p1)p R6 and R7 independently represent O or S; and all other variables are as defined herein;
processes for their preparation, pharmaceutical formulations containing them, and their use in me
Type:
Grant
Filed:
February 9, 2001
Date of Patent:
August 19, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Susan Mary Daluge, Michael Tolar Martin, Martin Howard Osterhout
Abstract: The invention provides the compounds of formula (I)
wherein:
R0 and R1 are independently selected from H, halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms;
R2 is halogen, CN, CONR4R5, CO2H, CO2C1-6alkyl, or NHSO2R4;
R3 is C1-6alkyl or NH2; and
R4 and R5 are independently selected from H, C1-6alkyl, phenyl, phenyl substituted by one or more atoms or groups (selected from halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms), or together with the nitrogen atom to which they are attached form a saturated 4 to 8 membered ring; and
pharmaceutically acceptable derivatives thereof.
Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.
Type:
Grant
Filed:
August 30, 2001
Date of Patent:
December 24, 2002
Assignee:
SmithKline Beecham Corporation
Inventors:
Ian Baxter Campbell, Paul Francis Lambeth, Alan Naylor, Neil Anthony Pegg
Abstract: The present invention relates to novel amidino compounds of formula (I),
or a salt, solvate, or physiologically functional derivative thereof;
wherein R1 is selected from C1-4 alkyl, C3-4 cycloalkyl, C1-4 hydroxyalkyl, and C1-4 haloalkyl; to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use as selective inhibitors of inducible nitric oxide synthase.
Type:
Grant
Filed:
November 26, 2001
Date of Patent:
December 17, 2002
Assignee:
SmithKline Beecham Corporation
Inventors:
Paul John Beswick, Savvas Kleanthous, Robert John Young
Abstract: The present invention provides compounds of formula (I)
or a salt or a non-toxic metabolically labile ester thereof, processes for their preparation, pharmaceutical compositions containing the same and to their use in medicine.
Abstract: The invention relates to Form VI 5,6-dichloro-2-(isopropylamino)-1-&bgr;-L-ribofuranosyl-1H-benzimidazole, pharmaceutical compositions comprising the same, and their use in medical therapy.
Abstract: The invention relates to Form physical forms of 5,6-dichloro-2-(isopropylamino)-1-&bgr;-L-ribofuranosyl-1H-benzimidazole, pharmaceutical compositions comprising the same, and their use in medical therapy.
Type:
Grant
Filed:
October 6, 2000
Date of Patent:
October 22, 2002
Assignee:
SmithKline Beecham Corporation
Inventors:
Bobby Neal Glover, Lian-Feng Huang, Robert William Lancaster, Stacey Todd Long, Michele Catherine Rizzolio, Eric Allen Schmitt, Barry Riddle Sickles
Abstract: The invention is concerned with novel hypolipidemic compounds of formula (I),
wherein R1 is H or methyl, and salts, solvates or physiologically functional derivatives thereof, with processes and novel intermediates for their preparation, pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions and associated diseases, such as atherosclerosis.
Abstract: The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof in which: R0 is halogen, C1-6alkyl, C1-6alkoxy, C1-6alkoxy substituted by one or more fluorine atoms, or O(CH2)nNR4R5; R1 and R2 are independently selected from H, C1-6alkyl, C1-6alkyl, substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5, (CH2)nSC1-6alkyl or C(O)NR4R5; with the proviso that when R0 is at the 4-position and is halogen, at least one of R1 and R2 is C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5 or (CH2)nSC1-6alkyl, C(O)NR4R5; R3 is C1-6alkyl or NH2; R4 and R5 are independently selected from H, or C1-6alkyl or, together with the nitrogen atom to which they are attached, form a 4-8 membered saturated ring; and n is 1-4.
Type:
Grant
Filed:
June 13, 2000
Date of Patent:
September 17, 2002
Assignee:
Smithkline Beecham Corporation
Inventors:
Paul John Beswick, Ian Baxter Campbell, Neil Mathews, Alan Naylor
Abstract: There are provided according to the invention novel compounds of formula (I)
wherein R1 represents C1-4alkyl or C3-8cycloalkyl, R2 represents C1-4alkyl or C3-4alkenyl, R3 represents hydrogen, C1-3alkyl or halogen, and R4 represents C1-6alkyl, processes for preparing them, pharmaceutical formulations containing them and their use in therapy particularly as thrombin inhibitors.
Type:
Grant
Filed:
March 30, 2001
Date of Patent:
August 27, 2002
Assignee:
SmithKline Beecham Corporation
Inventors:
Henry Anderson Kelly, Martin Pass, David Neil Smith
Abstract: The present invention provides a compound of formula (I)
or a solvate thereof wherein:
X is —O— or —NH—;
Q is (—CH2—)p, (—CH═CH—)p, (—C≡C—)p where p is an integer of from 0 to 4;
R1 is hydrogen or methyl;
R2 and R3 independently represent O or S
n is an integer of 1 to 50; and
R is hydrogen or methyl.
The present invention also provides pharmaceutical compositions and methods of treatment using the compounds of formula (I).
Type:
Grant
Filed:
June 1, 2001
Date of Patent:
August 20, 2002
Assignee:
SmithKline Beecham Corporation
Inventors:
Susan Mary Daluge, Gerald Wolberg, Douglas Alan Livingston
Abstract: The present invention provides compounds of formula (I)
or a salt or a non-toxic metabolically labile ester thereof, processes for their preparation, pharmaceutical compositions containing the same and to their use in medicine.
Abstract: The present invention relates to novel amidino compound of formula (I).
to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use as selective inhibitors of inducible nitric oxide synthase.
Type:
Grant
Filed:
August 24, 1999
Date of Patent:
April 9, 2002
Assignee:
GlaxoSmithKline
Inventors:
Richard Mansfield Beams, Martin James Drysdale, Karl Witold Franzmann, Anthony Joseph Frend, Harold Francis Hodson, Richard Graham Knowles, Daryl David Rees, David Alan Sawyer
Abstract: The present invention provides compounds of formula (I)
or a salt or a non-toxic metabolically labile ester thereof, processes for their preparation, pharmaceutical compositions containing the same and to their use in medicine.
Abstract: The present invention provides a compound of formula (I)
or a solvate thereof wherein:
X is —O— or —NH—;
Q is (—CH2—)p, (—CH═CH—)p, (—C≡C—)p where p is an integer of from 0 to 4;
R1 is hydrogen or methyl;
R2 and R3 independently represent O or S
n is an integer of 1 to 50; and
R is hydrogen or methyl.
The present invention also provides pharmaceutical compositions and methods of treatment using the compounds of formula (I). The compounds of the present invention are useful for the prophylaxis and treatment of septic shock, inflammatory conditions and immune disorders.
Type:
Grant
Filed:
December 22, 1999
Date of Patent:
March 12, 2002
Assignee:
Glaxo Wellcome Inc.
Inventors:
Susan Mary Daluge, Gerald Wolberg, Douglas Alan Livingston
Abstract: The present invention relates to novel amidino compounds of formula (I),
or a salt, solvate, or physiologically functional derivative thereof;
wherein R1 is selected from C1-4 alkyl, C3-4 cycloalkyl, C1-4 hydroxyalkyl, and C1-4 haloalkyl; to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use as selective inhibitors of inducible nitric oxide synthase.
Type:
Grant
Filed:
November 29, 2000
Date of Patent:
March 12, 2002
Assignee:
SmithKline Beecham Corporation
Inventors:
Paul John Beswick, Savvas Kleanthous, Robert John Young