Polycyclo Ring System Having The Asymmetrical Triazine Ring As One Of The Cyclos Patents (Class 544/183)
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Patent number: 7405213Abstract: The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.Type: GrantFiled: June 27, 2006Date of Patent: July 29, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Ping Chen, Derek J. Norris, Ashvinikumar V. Gavai
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Patent number: 7402582Abstract: The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.Type: GrantFiled: June 27, 2006Date of Patent: July 22, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Ashvinikumar V. Gavai, Ping Chen, Derek J. Norris
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Publication number: 20080171741Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.Type: ApplicationFiled: October 25, 2007Publication date: July 17, 2008Inventors: Stephen T. Wrobleski, Jagabandhu Das, T.G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
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Patent number: 7393667Abstract: The invention relates to a process for the enzymatic, stereoselective reduction of ketone compounds to provide chiral alcohols, for example the compound of formula Ib:Type: GrantFiled: May 31, 2006Date of Patent: July 1, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Ramesh N. Patel, Linda Nga Hoong Chu, Robert M. Johnson, Zhiwei Guo, Yijun Chen, Steven L. Goldberg, Ronald L. Hanson, Animesh Goswami, Kishta Katipally
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Patent number: 7388009Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.Type: GrantFiled: October 3, 2003Date of Patent: June 17, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Katerina Leftheris, Stephen T. Wrobleski, Alaric J. Dyckman
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Publication number: 20080139565Abstract: Therapeutically active anthranilic acid derivatives of Formula (I) wherein R1, R2, W, Y and Z are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.Type: ApplicationFiled: February 14, 2006Publication date: June 12, 2008Inventors: Matthew Campbell, Andrew McMurtrie Mason, Ivan Leo Pinto, Ian Edward David Smith
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Publication number: 20080119456Abstract: Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis; wherein X1 is —S—, —O—, —N?N—. —NR7—, —CR7?CR8—, —CR7?N—, wherein R7 and R8 are independently hydrogen or C1-C3 alkyl; A is a carboxyl group —COOH, or a carboxyl bioisostere; rings Ar2 and Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; ring B is as defined for Ar2 and Ar3, or an optionally substituted N-pyrrolidinyl, N-piperidinyl or N-azepinyl ring; s is 0 or 1; L1, L2 and L4 are linker radicals as defined in the description; Q1 and Q2 represent substituents as defined in the description.Type: ApplicationFiled: May 30, 2005Publication date: May 22, 2008Inventors: Trond Ulven, Thomas Frimurer, Oystein Rist, Evi Kostenis, Thomas Hogberg, Jean-Marie Receveur, Marie Grimstrup
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Patent number: 7348325Abstract: In general, the instant invention comprises compounds having Formulae I and II: including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.Type: GrantFiled: November 28, 2006Date of Patent: March 25, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Zhen-Wei Cai, Kyoung S. Kim, Robert M. Borzilleri
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Patent number: 7332485Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: July 8, 2004Date of Patent: February 19, 2008Assignee: SmithKline Beecham CorpInventors: Kelly M. Aubart, Siegfried Benjamin Christensen, IV, Chaya Duraiswami, Joseph M. Karpinski
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Patent number: 7314876Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are surprisingly advantageous as p38 kinase inhibitors, wherein R3 is hydrogen, methyl, perfluoromethyl, methoxy, halogen, cyano, NH2, or NH(CH3), preferably methyl; X is N or CH; and R1 through R6 are as described in the specification.Type: GrantFiled: April 22, 2003Date of Patent: January 1, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Alaric J. Dyckman, Katerina Leftheris, John Hynes, Arthur M P. Doweyko
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Patent number: 7297695Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: June 26, 2006Date of Patent: November 20, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Brian E. Fink, Ashvinikumar V. Gavai, Gregory D. Vite, Ping Chen, Harold Mastalerz, Derek J. Norris, John S. Tokarski, Yufen Zhao, Wen-Ching Han
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Patent number: 7265113Abstract: The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: January 13, 2005Date of Patent: September 4, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Rajeev S. Bhide, Zhen-Wei Cai, Ligang Qian, Stephanie Barbosa, Louis Lombardo, Jeffrey Robl
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Patent number: 7244733Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, PDGFR, HER-1, HER-2, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: February 2, 2006Date of Patent: July 17, 2007Assignee: Bristol-Myers Squibb CompanyInventors: John T. Hunt, Rajeev S. Bhide, Robert Michael Borzilleri, Ligang Qian
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Patent number: 7232901Abstract: Described herein is at least one pyrrolo[1,2-f][1,2,4]triazine-2,4(1H,3H)-dione, which is an intermediates useful in preparing 2,4-disubstituted pyrrolotriazine compounds, and at least one method for making such intermediate.Type: GrantFiled: June 27, 2006Date of Patent: June 19, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Harold Mastalerz, Guifen Zhang
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Patent number: 7211666Abstract: Methods of preparing kinase inhibiting pharmaceutical compounds having the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1 through R6 and Z are as described in the specification. The methods according to the invention utilize an amination process, in which a pyrrole is reacted with a haloamine, preferably chloramine. This step is followed by cyclization to form the pyrrolotriazine core.Type: GrantFiled: December 22, 2004Date of Patent: May 1, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Jollie Duaine Godfrey, Jr., John Hynes, Jr., Alaric J. Dyckman, Katerina Leftheris, Zhongping Shi, Stephen T. Wrobleski, Wendel William Doubleday, John A. Grosso
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Patent number: 7183273Abstract: Heterocyclic compounds that bind chemokine receptors and inhibit the binding of their natural ligands are disclosed. The invention compounds are protective against infection by HIV and exert effects characteristic of antagonists to the CXCR4 receptor.Type: GrantFiled: April 30, 2004Date of Patent: February 27, 2007Assignee: AnorMED, Inc.Inventors: Gary J. Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols
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Patent number: 7173031Abstract: In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.Type: GrantFiled: June 24, 2005Date of Patent: February 6, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Robert M. Borzilleri, Zhong Chen, John T. Hunt, Tram Huynh, Michael A. Poss, Gretchen M. Schroeder, Wayne Vaccaro, Tai W. Wong, Xiao-Tao Chen, Kyoung S. Kim
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Patent number: 7160883Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.Type: GrantFiled: April 22, 2003Date of Patent: January 9, 2007Assignee: Bristol-Myers-Squibb CompanyInventors: Alaric Dyckman, John Hynes, Katerina Leftheris, Chunjian Liu, Stephen T. Wrobleski
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Patent number: 7151176Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The compounds of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: October 19, 2005Date of Patent: December 19, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Ashvinikumar V. Gavai, Wen-Ching Han, Yufen Zhao, Ping Chen
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Patent number: 7148220Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: June 2, 2005Date of Patent: December 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Gregory D. Vite, Ashvinikumar V. Gavai, Brian E. Fink, Harold Mastalerz, John F. Kadow
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Patent number: 7148348Abstract: A process is provided for the process for preparing a pyrrolotriazine aniline p38 kinase inhibitor such as amide II by the direct aminolysis of the ester I wherein ester I is reacted with a strong organometallic base, such as hexyllithium or n-butyllithium and the desired amine such as n-propylamine to form the amide II.Type: GrantFiled: August 9, 2005Date of Patent: December 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Reginald O. Cann, Edward J. Delaney, Junying Fan, Luca Parlanti
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Patent number: 7141571Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: December 22, 2004Date of Patent: November 28, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Brian E. Fink, Ashvinikumar V. Gavai, Gregory D. Vite, Ping Chen, Harold Mastalerz, Derek J. Norris, John S. Tokarski, Yufen Zhao, Wen-Ching Han
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Patent number: 7129349Abstract: An improved method of producing 3-amino-1,2,4-benzotriazines using nitrobenzene or a derivative thereof, a guanidine salt and a base as reactants is provided. The method is carried out at a moderate reaction temperature without producing halide wastes derived from nucleophilic substitution and acid byproducts.Type: GrantFiled: October 8, 2003Date of Patent: October 31, 2006Assignee: Trustees of Dartmouth CollegeInventors: Nikolai V. Moskalev, Gordon W. Gribble
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Patent number: 7112675Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, PDGFR, HER-1, HER-2, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: July 27, 2005Date of Patent: September 26, 2006Assignee: Bristol-Myers Squibb CompanyInventors: John T. Hunt, Rajeev S. Bhide, Robert Michael Borzilleri, Ligang Qian
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Patent number: 7109214Abstract: The present invention relates to substituted cyclopentene compounds of the general formula I, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use thereof for the production of pharmaceutical preparations.Type: GrantFiled: November 19, 2004Date of Patent: September 19, 2006Assignee: Grunenthal GmbHInventors: Oswald Zimmer, Michael Haurand, Klaus Schiene, Clemens Gillen, Johannes Schneider, Gregor Bahrenberg
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Patent number: 7102003Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The compounds of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: June 21, 2005Date of Patent: September 5, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Ashvinikumar V. Gavai, Harold Mastalerz, Jean-Paul Daris, Pierre Dextraze, Philippe Lapointe, Edward H. Ruediger, Dolatrai M. Vyas, Guifen Zhang
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Patent number: 7102001Abstract: The present invention provides a process for preparing compounds of formula (I) or a pharmaceutically acceptable salt thereof. The compounds prepared by the process of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.Type: GrantFiled: December 9, 2004Date of Patent: September 5, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Shankar Swaminathan, Ashvinikumar V. Gavai, Junying Fan, Bharat P. Patel, Derek J. Norris, Richard Michael Corbett, Bin Zheng
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Patent number: 7102002Abstract: The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: June 14, 2005Date of Patent: September 5, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Zhen-wei Cai, Louis J. Lombardo, Rajeev S. Bhide, Ligang Qian, Donna D. Wei, Stephanie Barbosa
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Patent number: 7064203Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The compounds of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.Type: GrantFiled: December 22, 2004Date of Patent: June 20, 2006Assignee: Bristol Myers Squibb CompanyInventors: Ashvinikumar V. Gavai, Wen-Ching Han, Ping Chen, Edward H. Ruediger, Harold Mastalerz, Brian E. Fink, Derek J. Norris
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Patent number: 7034151Abstract: An improved process for the preparation of certain pyrrolotriazine compounds is disclosed. The compounds exhibit utility as kinase inhibitors.Type: GrantFiled: February 5, 2004Date of Patent: April 25, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Bang-Chi Chen, Rulin Zhao, Joseph Edward Sundeen, Katerina Leftheris, John Hynes, Stephen T. Wrobleski
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Patent number: 7030118Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof useful for inducing mitotic arrest thereby making them useful as anti-cancer agents and other diseases which can be treated by inducing mitotic arrest.Type: GrantFiled: May 20, 2003Date of Patent: April 18, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Louis J. Lombardo, Rajeev S. Bhide, Kyoung S. Kim, Songfeng Lu
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Patent number: 7001911Abstract: The invention pertains to fused cyclic compounds having the formula, wherein G is an optionally substituted aryl or heterocyclo, L is an optional linker, M is a bond, O, CR7R7? or NR10, and M? is a bond or NR10, with the proviso that at least one of M or M? must be a bond; E is C?Z2, CR7CR7?, SO2, P?OR2, or P?OOR2; Z1 is O, S, NH, or NR6; Z2 is O, S, NH, or NR6; A1 is CR7 or N; A2 is CR7 or N; Y is J—J?—J? where J is (CR7R7?)n and n=0-3, J? is a bond or O, S, S?O, SO2, NH, NR6, C?O, OC?O, NR1C?O, CR7R7?, C?CR8R8?, R2P?O, OPOOR2, OPO2, OSO2, C?N, NHNH, NHNR6, NR6NH, N?N, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo or aryl or substituted aryl, and J? is (CR7R7?)n and n=0-3; W is CR7R7?—CR7R7?, CR8?CR8?, CR7R7?—C?O, NR9—CR7R7?, N?CR8, N?N, NR9—NR9?, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, or aryl or substituted aryl; and O, R2, R6, R7, R7?, R8, R8?, R9, R9Type: GrantFiled: December 18, 2002Date of Patent: February 21, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Mark E. Salvati, James Aaron Balog, Weifang Shan, Sören Giese, Lalgudi S. Harikrishnan
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Patent number: 6982265Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, PDGFR, HER-1, HER-2, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: May 18, 2000Date of Patent: January 3, 2006Assignee: Bristol Myers Squibb CompanyInventors: John T. Hunt, Rajeev S. Bhide, Robert Michael Borzilleri, Ligang Qian
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Patent number: 6969717Abstract: The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: July 18, 2003Date of Patent: November 29, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Rajeev S. Bhide, Rejean Ruel, Carl Thibault, Alexandre L'Heureux
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Patent number: 6953852Abstract: Industrially applicable process for preparing 3-amino-1,2,4-benzotriazine 1,4-dioxide.Type: GrantFiled: November 8, 2002Date of Patent: October 11, 2005Assignee: Sanofi-AventisInventor: Alain Burgos
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Patent number: 6951859Abstract: The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: August 4, 2003Date of Patent: October 4, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Rajeev S. Bhide, Robert M. Borzilleri
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Patent number: 6939870Abstract: A compound represented by the formula I: wherein A represents the following heterocycles: and R1-9 are as defined herein, a composition containing this compound and methods for treating disorders of the serotonin-affected neurological systems utilizing such a compound or composition.Type: GrantFiled: August 29, 2003Date of Patent: September 6, 2005Assignee: WyethInventors: Aranapakam M. Venkatesan, Jamie M. Davis, Yansong Gu
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Patent number: 6933386Abstract: The present invention relates to a process for preparing certain pyrrolotriazine compounds of the formula and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: July 18, 2003Date of Patent: August 23, 2005Assignee: Bristol Myers Squibb CompanyInventors: Rajeev S. Bhide, Junying Fan, Luca Parlanti, Stephanie Barbosa, Ligang Qian, Zhen-Wei Cai, Francis S. Gibson
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Patent number: 6916815Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: December 15, 2003Date of Patent: July 12, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Gregory D. Vite, Ashvinikumar V. Gavai, Brian E. Fink, Harold Mastalerz, John F. Kadow
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Patent number: 6908916Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: November 14, 2002Date of Patent: June 21, 2005Assignee: Bristol Myers Squibb CompanyInventors: Harold Mastalerz, Guifen Zhang, James G. Tarrant, Gregory D. Vite
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Patent number: 6881753Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure: where A, B, D, Q, X1, R, R1, X2 and R2 are as defined herein. These compounds are useful as antiarrhythmic agents. In addition, a method is provided for preventing cardiac arrhythmia employing the above compounds.Type: GrantFiled: April 14, 2004Date of Patent: April 19, 2005Assignee: Bristol-Myers Squibb Co.Inventors: John Lloyd, Heather J. Finlay, Wayne Vaccaro, Karnail S. Atwal, Michael F. Gross, Kerry L. Spear
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Patent number: 6872720Abstract: A class of substituted pyrazolo[1,5-d][1,2,4]triazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 7-position, an alkyl group at the 4-position, and a substituted alkoxy moiety at the 2-position, are selective ligands for GABAA receptors, in particular having high affinity for the ?2 and/or ?3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.Type: GrantFiled: April 4, 2001Date of Patent: March 29, 2005Assignee: Merck Sharp & Dohme Ltd.Inventors: William Robert Carling, Andrew Mitchinson, Michael Geoffrey Russell, Leslie Joseph Street
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Patent number: 6872730Abstract: The present invention relates to novel substituted benzofurans and benzothiophenes compounds that are antagonists of alpha V (?v) integrins, for example ?v?3 and ?v?5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by ?v?3 and ?v?5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula I: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, m, n, i, j and k are defined herein.Type: GrantFiled: April 26, 2002Date of Patent: March 29, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Beth M. Anaclerio, Juan J. Marugan Sanchez, Victor J. Marder, David C. U'Prichard, Bruce E. Tomczuk
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Patent number: 6869952Abstract: The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: July 18, 2003Date of Patent: March 22, 2005Assignee: Bristol Myers Squibb CompanyInventors: Rajeev S. Bhide, Zhen-Wei Cai, Ligang Qian, Stephanie Barbosa
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Patent number: 6867300Abstract: Methods of preparing kinase inhibiting pharmaceutical compounds having the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1 through R6 and Z are as described in the specification. The methods according to the invention utilize an amination process, in which a pyrrole is reacted with a haloamine, preferably chloramine. This step is followed by cyclization to form the pyrrolotriazine core.Type: GrantFiled: November 6, 2002Date of Patent: March 15, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Jollie Duaine Godfrey, Jr., John Hynes, Jr., Alaric J. Dyckman, Katerina Leftheris, Zhongping Shi, Stephen T. Wrobleski, Wendel William Doubleday, John A. Grosso
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Patent number: 6858611Abstract: Compounds which are useful as potassium channel inhibitors and which because of their slow off-rates are especially useful for the treatment of cardiac arrhythmias are described.Type: GrantFiled: March 19, 2003Date of Patent: February 22, 2005Assignee: Icagen, Inc.Inventors: Aimee Dolores Reed, Michael Francis Gross, Serge Beaudoin
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Publication number: 20040266779Abstract: The present invention relates to the use of a c-kit inhibitor, especially a c-kit inhibitor of formula I, wherein the radicals and symbols have the meanings as defined in the specification, for the preparation of a medicament for the treatment of myeloma, in particular multiple myeloma, especially myeloma which is resistant to conventional chemotherapy; to a combination comprising a c-kit inhibitor and a compound effecting apoptosis of myeloma cells, preferably dexamethasone, for simultaneous, separate or sequential use; to methods of treating myeloma; and to a pharmaceutical composition comprising said combination.Type: ApplicationFiled: August 5, 2004Publication date: December 30, 2004Inventor: Kenneth C. Anderson
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Publication number: 20040254187Abstract: The invention relates to novel 5-Ethyl-imidazotriazinones, processes for their preparation and their use in medicaments, esp. for the treatment and/or prophylaxis of inflammatory processes and/or immune diseases.Type: ApplicationFiled: August 2, 2004Publication date: December 16, 2004Inventors: Cristina Alonso-Alija, Heike Gielen, Martin Hendrix, Ulrich Niewohner, Maria Theresia Niewohner, Dagmar Schauss, Hilmar Bischoff, Nils Burkhardt, Volker Geiss, Karl-Heinz Schlemmer, Nigel J Cuthbert, Mary F Fitzgerald, Richard Graham Sturton, Martin Michels
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Publication number: 20040249148Abstract: The invention relates to new imidazotriazines, processes for their preparation, and their use for the production of medicaments for the treatment and/or prophylaxis of neurodegenerative disorders, in particular Parkinson's disease.Type: ApplicationFiled: June 25, 2004Publication date: December 9, 2004Inventors: Jens-Kerim Erguden, Marcus Bauser, Nils Burkhardt, Dietmar Flubacher, Arno Friedl, Irene Gerlach, Volker Hinz, Reinhard Jork, Paul Naab, Ulrich Niewohner, Maria Theresia Niewohner, Thorsten Oliver Repp, Karl-Heinz Schlemmer, Jurgen Stoltefuss, David Bruckner, Martin Hendrix, Dagmar Schauss, Adrian Tersteegen
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Publication number: 20040242871Abstract: There are provided novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, T, U, X, Y, V and W are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.Type: ApplicationFiled: January 8, 2004Publication date: December 2, 2004Inventors: Tim Birkinshaw, Stephen Connolly, Timothy Luker, Antonio Mete, Ian Millichip