At 2-position And At 4- Or 6-position Patents (Class 544/323)
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Patent number: 7101869Abstract: Novel compounds according to the formula and pharmaceutically acceptable salts, solvates, or hydrates thereof; wherein each occurrence of A is independently selected from CH or N; X is selected from the group consisting of —CH2—, —O—, —NH—, (C1-C6)alkylamino-, (C1-C6)alkylaminocarbonylamino-, (C1-C6)alkylcarbonylamino-, (C1-C6)alkylsulfonylamino-, phenylsulfonylamino-, carbonyl, —NH—C(O)—, —N(C1-C6)alkyl-C(O)—, —S(O)y— where y is 0, 1 or 2, and; n in —(CH2)n— is 1, 2 or 3; and R1, R2, and R3 are as described herein; pharmaceutical compositions that including these compounds, and methods for the treatment of autoimmune disease, inflammation, allergy, transplant rejection, and other circumstances where administration of an immunosuppressive agent is of therapeutic benefit.Type: GrantFiled: November 22, 2002Date of Patent: September 5, 2006Assignee: Pfizer Inc.Inventors: Todd A. Blumenkopf, Eileen Elliott Mueller, Eric Jan Roskamp
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Patent number: 7087614Abstract: Pyrimidine phosphodiesterase 7 (PDE 7) inhibitors of the following formula wherein R1, R2, Z, J and L are described herein, and analogs thereof are provided which are useful in treating T-cell mediated diseases.Type: GrantFiled: June 17, 2002Date of Patent: August 8, 2006Assignee: Bristol-Myers Squibb Co.Inventors: Junqing Guo, Joseph Barbosa, William John Pitts, Marianne Carlsen, Claude Quesnelle, Marco Dodier
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Patent number: 7087616Abstract: This invention relates to novel pyrazolylpyrimidines of the formula in which R1, R2, X, n, Y, Z and R have the meanings given in the disclosure, to a plurality of processes for preparing these substances, and to their use for controlling pests.Type: GrantFiled: February 11, 2002Date of Patent: August 8, 2006Assignee: Bayer CropScience AGInventors: Rüdiger Fischer, Bernd Alig, Thomas Bretschneider, Mazen Es-Sayed, Christoph Erdelen, Peter Lösel, Udo Reckmann
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Patent number: 7067522Abstract: Pyrimidine derivatives of formula (I) wherein Q1, Q2, G and R1 are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) and focal adhesion kinase (FAK) inhibitors are also described.Type: GrantFiled: November 24, 2004Date of Patent: June 27, 2006Assignee: AstraZeneca ABInventors: Elizabeth Janet Pease, Emma Jane Williams, Robert Hugh Bradbury, Stuart Eric Pearson
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Patent number: 7067670Abstract: A sulfamato hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a process for preparing the same, intermediate compounds useful in those syntheses, and a treatment process that comprises administering a contemplated sulfamato hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: July 8, 2004Date of Patent: June 27, 2006Assignee: Warner Lambert CompanyInventors: Terri L. Boehm, Deborah A. Mischke, Gary A. DeCrescenzo, Joseph G. Rico, Shashidhar N. Rao, Darren J. Kassab, Jeffery N. Carroll
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Patent number: 7060827Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: GrantFiled: June 1, 2004Date of Patent: June 13, 2006Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
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Patent number: 7030130Abstract: The invention relates to novel benzofuran derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as anti-infectives.Type: GrantFiled: July 20, 2001Date of Patent: April 18, 2006Assignee: Arpida AGInventors: Kaspar Burri, Dieter Gillessen, Sorana Greiveldinger-Poenaru, Khalid Islam
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Patent number: 7026328Abstract: Disclosed are compounds which bind ?4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by ?4 integrins, preferably VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: May 27, 2003Date of Patent: April 11, 2006Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Andrei W. Konradi, Christopher M. Semko, Ying-zi Xu, Frank Stappenbeck, Brian P. Stupl, Jenifer L. Smith, Michael A. Pleiss, Eugene D. Thorsett
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Patent number: 7008949Abstract: Disclosed are compounds which bind ?4 integrins, where the ?4 integrin is preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by ?4 integrins, where the ?4 integrin is preferably VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: May 27, 2003Date of Patent: March 7, 2006Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Andrei W. Konradi, Christopher M. Semko, Ying-zi Xu, Frank Stappenbeck, Brian P. Stupi, Jenifer L. Smith, Michael A. Pleiss, Eugene D. Thorsett
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Patent number: 7001910Abstract: The present invention refers to compounds of the general formula (I), to their possible pharmaceutically acceptable salts and tautomeric forms. The present invention also refers to a process for their production and to their use as antidiabetic and *hypoglycemic agents, alone or in combination with other antidiabetic agents, such as sulfonilureas or biguanides, as well as for the treatment of complications associated to the resistance to the insulin, such as hypertension, hyperuricemia or other cardiovascular, metabolic, endocrine conditions, or other conditions related with diabetes.Type: GrantFiled: November 15, 2000Date of Patent: February 21, 2006Assignee: Vita-Invest S.A.Inventors: Marisabel Mourelle Mancini, Juan Carlos Del Castillo Nieto, Elisabet De Ramon Amat
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Patent number: 6953802Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: July 20, 2001Date of Patent: October 11, 2005Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
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Patent number: 6951866Abstract: 1. A pyrimidine derivative of the formula (1) or a salt thereof; has an inhibitory activity of production of Th2 type cytokines such as IL-4, IL-5, etc., and is useful as an therapeutic agent for allergic diseases, autoimmune diseases such as systemic lupus erythemathosus, etc., and acquired immunodeficiecy syndrome (AIDS) and so on.Type: GrantFiled: August 19, 2002Date of Patent: October 4, 2005Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Hitoshi Fujita, Fujio Antoku, Norio Fujiwara, Kiyotaka Iwai, Hiroshi Tanaka, Hajime Kawakami
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Patent number: 6943172Abstract: Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.Type: GrantFiled: January 23, 2003Date of Patent: September 13, 2005Assignee: Bayer Pharmaceuticals CorporationInventors: Dhanapalan Nagarathnam, Jacques Dumas, Holia Hatoum-Mokdad, Stephen Boyer, Hans Pluempe
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Patent number: 6936607Abstract: This invention is directed to pyrimidine derivatives which are selective antagonists for the GalR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety.Type: GrantFiled: August 7, 2003Date of Patent: August 30, 2005Assignee: H. Lunobeck A/SInventor: Mathivanan Packiarajan
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Patent number: 6924290Abstract: Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.Type: GrantFiled: January 23, 2003Date of Patent: August 2, 2005Assignee: Bayer Pharmaceuticals CorporationInventors: Dhanapalan Nagarathnam, Jacques Dumas, Holia Hatoum-Mokdad, Stephen Boyer, Chunguang Wang, Hans Pluempe, Achim Feurer, Samir Bennabi
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Patent number: 6916820Abstract: The present invention relates to a series of substituted pyrimidines, to pharmaceutical compositions which contain them, to methods for their preparation and to their use in therapy, particularly in the treatment of neurodegenerative or other neurological disorders of the central and peripheral nervous systems.Type: GrantFiled: April 6, 2000Date of Patent: July 12, 2005Assignee: Krenitsky Pharmaceuticals, Inc.Inventors: James L. Kelley, Thomas A. Krenitsky, Lilia M. Beauchamp
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Patent number: 6908920Abstract: Compounds of formula (I), wherein R1, p, R2, q, R3 and R4 are defined within, and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described.Type: GrantFiled: July 6, 2001Date of Patent: June 21, 2005Assignee: AstraZeneca ABInventors: Andrew Peter Thomas, Nicholas John Newcombe, David William Heaton
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Patent number: 6906065Abstract: Compounds of formula (I) wherein: R1 is halo, nitro, cyano, hydroxy, amino, carboxy, carbamoyl, mercapto, C1-6alkyl, C2-6alkenyl or C2-6alkynyl; p is 0-4; wherein the values of R1 may be the same or different; R2 is sulphamoyl or a group B-E- ; wherein B is optionally substituted as defined within and is selected from C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C1-6alkyl, phenyl, a heterocyclic group, phenylC1-6alkyl or (heterocyclic group)C1-6alkyl; E is C(O)—, N(Ra)C(O)—, —C(O)N(Ra)—, —S(O)r—, —SO2N(Ra)— or —N(Ra)SO2—; wherein Ra is hydrogen or C1-6alkyl optionally substituted as defined within and r is 1-2; q is 0-2; wherein the values of R2 may be the same or different; and wherein p+q=1-5; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof are described.Type: GrantFiled: March 23, 2001Date of Patent: June 14, 2005Assignee: AstraZeneca ABInventor: Andrew Peter Thomas
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Patent number: 6906076Abstract: The present invention concerns alkyl aryl carbonyl compounds that possess anti-infective activity. The compounds of the invention can be used to target specific nuclear localization signal, thereby blocking importation of specific proteins or molecular complex into the nucleus of a cell. The invention encompasses methods of use of such compounds for treatment or prevention of infectious diseases, such as parasitic and viral diseases, including, for example, malaria and acquired immunodeficiency syndrome. The use of the compounds to detect certain specific protein structures which are present in nuclear localization sequences is also taught.Type: GrantFiled: September 12, 2003Date of Patent: June 14, 2005Assignee: Cytokine Pharmasciences, Inc.Inventors: Michael I. Bukrinsky, Anthony Cerami, Peter Ulrich, Bradley Berger
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Patent number: 6903213Abstract: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)-amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C16alkyloxy-carbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 or —X2-Alk-R7 wherein R6 and R7Type: GrantFiled: June 28, 2002Date of Patent: June 7, 2005Inventors: Koenraad Jozef Lodewijk Marcel Andries, Bart De Corte, Marc René De Jonge, Jan Heeres, Chih Yung Ho, Marcel August Constant Janssen, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
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Patent number: 6900214Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds induce mitotic arrest thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases which can be treated by inducing mitotic arrest.Type: GrantFiled: March 22, 2002Date of Patent: May 31, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Louis J. Lombardo, Laurence I. Wu
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Patent number: 6881740Abstract: This invention relates to compounds to formula (1) wherein B is optionally substituted aryl; R1 and R2 are the same or different and are independently selected from hydrogen or C1-3 alkyl; n is 1 or 2, preferably n is 1; m is 0 or 1; R3 is hydrogen or acyl, R4 and R5 are the same or different and are independently selected from amino, alkylamino, dialkylamino, arylamino and C2-C4 cycloalkylamino; X and Y are independently selected from C, H or N provided at least one of X and Y is N; and salts thereof, solvates thereof, pharmaceutically acceptable derivatives thereof, prodrugs thereof, tautomers thereof and/or isomers thereof, and processes for their reparation and methods of treatment, pharmaceutical formulations and uses involving them.Type: GrantFiled: July 8, 1999Date of Patent: April 19, 2005Assignee: Monash UniversityInventors: Bevyn Jarrott, Phillip Mark Beart, William Roy Jackson, Alan Duncan Robertson, Maree Patricia Collis, Alexandra Papanikos
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Patent number: 6878717Abstract: This invention concerns the use of compounds of formula: the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=-a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxy-carbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalo-methylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally subsType: GrantFiled: November 1, 1999Date of Patent: April 12, 2005Inventors: Bart De Corte, Marc Rene De Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
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Patent number: 6870053Abstract: The present invention relates to certain novel pyrimidine intermediates and their salts, processes for their preparation and processes for their conversion to 9-substituted-2-aminopurines which are useful in medical therapy.Type: GrantFiled: June 27, 2002Date of Patent: March 22, 2005Assignee: SmithKline Beecham CorporationInventors: Susan Mary Daluge, Michelle Joanne Fugett, Michael Tolar Martin
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Patent number: 6867205Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and X are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.Type: GrantFiled: February 10, 2003Date of Patent: March 15, 2005Assignee: Hoffman-La Roche Inc.Inventors: Markus Boehringer, Bernd Michael Loeffler, Jens-Uwe Peters, Matthias Steger, Peter Weiss
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Patent number: 6852739Abstract: The present invention describes novel nitrosated and/or nitrosylated proton pump inhibitor compounds, and novel compositions comprising at least one proton pump inhibitor compound that is optionally substituted with at least one NO and/or N02 group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one nonsteroidal antiinflammatory drug, selective COX-2 inhibitor, antacid, bismuth-containing reagent, acid-degradable antibacterial compound, and mixtures thereof.Type: GrantFiled: February 25, 2000Date of Patent: February 8, 2005Assignee: Nitromed Inc.Inventors: David S. Garvey, L. Gordon Letts, Sang William Tam
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Patent number: 6846833Abstract: Compounds of formula (1): wherein: G represents an optionally substituted phenyl or optionally substituted heterocycle, G1 and G2 being N or C, T1 represents —CH2—CH2—, —CH?CH— or ?CH—CH2—, and T2 is a bond, or T1 represents —CH2— or ?CH— and T2 is —CH2—, ?CH—, R5 represents —(CH2)m—COOR6, R6 and R6? represent hydrogen, alkyl, optionally substituted aryl or optionally substituted arylalkyl, A represents —CO—, —CH2—, ?CH— or —CH? and W represents —CH—, ?C— or —C?, or A represents —CO— or —CH2— and W represents N, X represents —CO—X1—, —CO—NR6—X1—, —NR6—CO—X1—, —O—X1—, —SO2—NR6—X1— or —S(O)n—X1—, Y represents —Y1—, —Y2—Y1— or —Y1—Y2—Y1—, Y1 being an alkylene, alkenylene or alkynylene, and Y2 being an arylene, heteroarylene, cycloalkylene or heterocycloalkylene, Z represents —Z1—, —Z10—NR6—, and —Z10—NR6—CO—, Z1 being a heteroaryl, heterocycloalkyl, heteroarylalkyl, heterocycloalkylalkyl, fused arylheteroaryl, fused arylheterocycloalkyl, fused heteroarylheterocycloalkyl, fused heterocycloalkylheteroarType: GrantFiled: March 6, 2001Date of Patent: January 25, 2005Assignee: Les Laboratories ServierInventors: Patrick Casara, Françoise Perron-Sierra, Ghanem Atassi, Gordon Tucker, Dominique Saint-Dizier
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Patent number: 6838414Abstract: The invention relates to novel substituted arylsulphonyl(thio)ureas in which A represents nitrogen or a CH grouping, Q represents oxygen or sulphur, R1 represents hydrogen, halogen or respectively optionally substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, cycloalkyl, cycloalkyloxy or heterocyclyloxy, R2 represents hydrogen, halogen or respectively optionally substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, cycloalkyl, cycloalkyloxy or heterocyclyloxy, R3 represents hydrogen or optionally substituted alkyl, R4 represents respectively optionally substituted alkyl, alkoxy, alkenyl, alkinyl, alkenyloxy, alkinyloxy, cycloalkyl, cycloalkyloxy or cycloalkylalkyl, and R5 represents hydrogen, formyl or respectively optionally substituted alkyl, alkylcarbonyl, alkoxycarbonyl, alkylsulphonyl, alkenyl, alkinyl, cycloalkyl, cycloalkylcarbonyl, cycloalkylsulphonyl or heterocyclyl, and to salts of compounds of the formula (I), except for the compound N-(4,6-dimethyl-pyrimidin-2-yl)-N?-[Type: GrantFiled: July 16, 2002Date of Patent: January 4, 2005Assignee: Bayer AktiengesellschaftInventors: Ernst Rudolf F. Gesing, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Müller, Mark Wilhelm Drewes, Johannes Rudolf Jansen, Ulrich Philipp, Hans-Jochem Riebel, Otto Schallner, Markus Dollinger, Hans-Joachim Santel
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Patent number: 6835726Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.Type: GrantFiled: January 24, 2003Date of Patent: December 28, 2004Assignee: Amgen Inc.Inventors: Timothy D. Cushing, Heather L. Mellon, Juan C. Jaen, John A. Flygare, Shi-Chang Miao, Xiaoqi Chen, Jay P. Powers
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Publication number: 20040248916Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof 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: ApplicationFiled: July 29, 2004Publication date: December 9, 2004Inventors: Malcolm C Carter, Alan Naylor, Jeremy J. Payne, Neil A Pegg
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Publication number: 20040242614Abstract: The present invention relates to dihydrofolate reductase inhibitors having an aromatic group and a heteroaromatic group linked by a methylene group; and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such dihydrofolate reductase inhibitors.Type: ApplicationFiled: May 17, 2004Publication date: December 2, 2004Applicant: Dana-Farber Cancer InstituteInventors: Andre Rosowsky, Ronald A. Forsch
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Patent number: 6818649Abstract: This invention is concerned with substituted chromene derivatives of the general formula (I) in which R1-R4 are as defined in the specification and claims. The invention further relates to the pharmaceutically acceptable acid addition salts of these compounds, their use as therapeutically active substances; medicaments based on these substances, optionally in combination with sulphonamides, and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula (I) and their pharmaceutically acceptable acid addition salts and intermediates for their manufacture.Type: GrantFiled: October 28, 2002Date of Patent: November 16, 2004Assignee: Basilea Pharmaceutica AGInventors: Peter Mohr, Philippe Pflieger
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Patent number: 6809102Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds induce mitotic arrest thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases which can be treated by inducing mitotic arrest.Type: GrantFiled: March 22, 2002Date of Patent: October 26, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Spencer David Kimball, Louis J. Lombardo, David B. Rawlins, Hai-Yun Xiao, Robert J. Schmidt, David K. Williams
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Publication number: 20040204386Abstract: The invention relates to pyrimidines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase &bgr; (LPAAT-&bgr;) activity and/or proliferation of cells such as tumor-cells.Type: ApplicationFiled: September 24, 2003Publication date: October 14, 2004Applicant: Cell Therapeutics, Inc.Inventors: Rama Bhatt, Baoqing Gong, Feng Hong, Scott A. Jenkins, J. Peter Klein, Cory T. Kohm, John Tulinsky
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Publication number: 20040186118Abstract: This invention relates to pyrimidine derivatives of general formula (I) as inhibitors of kinases, their production as well as their use as medications for treating various diseasesType: ApplicationFiled: November 28, 2003Publication date: September 23, 2004Inventors: Judi Bryant, Monica J. Kochanny, Shendong Yuan, Seock-Kyu Khim, Brad O. Buckman, Damian O. Arnaiz, Ulf Bomer, Hans Briem, Peter Esperling, Christoph Huwe, Joachim Kuhnke, Martina Schafer, Lars Wortmann, Dirk Kosemund, Emil Eckle, Richard J. Feldman, Gary B. Phillips
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Patent number: 6794377Abstract: Ortho, ortho-substituted nitrogen-containing bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparations including their use as antiarrhythmic active compounds, for example, for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters.Type: GrantFiled: December 5, 2001Date of Patent: September 21, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Stefan Peukert, Joachim Brendel, Horst Hemmerle, Heinz-Werner Kleemann
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Publication number: 20040180913Abstract: Compounds of the formula (I) wherein R1 represents a hydrogen atom or a 3-halogen atom, and R2 represents a straight-chain alkyl group containing up to 6 carbon atoms, a straight-chain alkyl group containing up to 3 carbon atoms with unsubstituted or substituted aromatic ring, or alkoxycarbonyl substituent at the end position, or aryloxyalkoxyalkyl group have been found to possess antimalarial activity against Plasmodium falciparum lines, including those resistant against pyrimethamine and other antifolates. The compounds themselves, methods of making these compounds, and methods of using these compounds are all disclosed.Type: ApplicationFiled: March 13, 2003Publication date: September 16, 2004Applicant: National Science and Technology Development AgencyInventors: Yongyuth Yuthavong, Bongkoch Tarnchompoo, Sumalee Kamchonwongpaisan
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Patent number: 6787539Abstract: The invention relates to compounds of the formula wherein R1 is lower alkyl, lower alkoxy, pyridinyl, pyrimidinyl, phenyl, —S-lower alkyl, —S(O)2-lower alkyl, —N(R)—(CH2)n—N(R)2, —O—(CH2)n—N(R)2, —N(R)2, or a cyclic tertiary amine of the group which may contain one additional heteroatom, selected from N, O or S, and wherein this group may be connected with the pyrimidine ring via the linker —O(CH2)n—; R2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R3/R3′ is, independently from each other, hydrogen or lower alkyl; R4 is independently from each other halogen, trifluoromethyl or lower alkoxy; R5 is hydrogen or lower alkyl; R is, independently from each other, hydrogen or lower alkyl; X is —C(O)N(R)— or —N(R)C(O)—; Y is —O—, —S—, —SO2—, - or —N(R)—; n is 1,2,3 or 4; and m is 0,1 or 2; or a pharmaceuticType: GrantFiled: October 15, 2001Date of Patent: September 7, 2004Assignee: Hoffmann-La Roche Inc.Inventor: Heinz Stadler
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Publication number: 20040142954Abstract: Disclosed are compounds which bind &agr;4 integrins, where the &agr;4 integrin is preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by &agr;4 integrins, where the &agr;4 integrin is preferably VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: ApplicationFiled: May 27, 2003Publication date: July 22, 2004Inventors: Andrei W. Konradi, Christopher M. Semko, Ying-zi Xu, Frank Stappenbeck, Brain P. Stupi, Jenifer L. Smith, Michael A. Pleiss, Eugene D. Thorsett
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Patent number: 6756380Abstract: Compounds of the general formula are described: wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R3 is halogen, trifluoromethyl, lower alkoxy or lower alkyl; R4/R4′are each independently hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, hydroxy, hydroxy-lower alkyl, —(CH2)n-piperazinyl, optionally substituted by lower alkyl, —(CH2)n-morpholinyl, —(CH2)n+1-imidazolyl, —O—(CH2)n+1-morpholinyl, —O—(CH2)n+1-piperidinyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH2)n+1N(R4″)2, —(CH2)n—NH—(CH2)n+1N(R4″)2, —(CH2)n+1N(R4″)2, or —O—(CH2)n+1N(R4″)2, wherein R4″ is hydrogen or lower alkyl; R6 is hydrogen; R2 and R6 or R1 and R6 may together be —CH═CH—CH═CH—, wherein R2 and R6 or R1 and R6, respectively, together with the two carbon rinType: GrantFiled: May 22, 2000Date of Patent: June 29, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bös, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
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Publication number: 20040097734Abstract: The invention relates to novel aryl- and heteroarylcarboxamides of the general formula (1), their preparation and use as medicaments, in particular for the treatment of tumors.Type: ApplicationFiled: June 27, 2003Publication date: May 20, 2004Inventors: Matthias Gerlach, Peter Emig, Emmanuel Polymeropoulos, Gilbert Muller, Peter Schmidt, Silke Baasner, Eckhard Gunther
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Publication number: 20040097375Abstract: The invention relates to substituted fluoroalkoxyphenylsulfonylureas of the general formula (I) 1Type: ApplicationFiled: January 7, 2004Publication date: May 20, 2004Inventors: Klaus-Helmut Muller, Ernst-Rudolf Gesing, Joachim Kluth, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen, Ulrike Wachendorff-Neumann
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Patent number: 6727249Abstract: The present invention relates compounds of the formula (I): wherein X represents hydrogen, C1-4alkyl optionally substituted by a hydroxy, methoxy or benzyloxy group, or CO2(C1-2alkyl); Z is —CR9R10CH2— or —CH2CR9R10—; and R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.Type: GrantFiled: April 1, 2002Date of Patent: April 27, 2004Assignee: Merck Sharp & Dohme Ltd.Inventors: Neil Roy Curtis, Ian Thomas Huscroft, Janusz Jozef Kulagowski, Piotr Antoni Raubo
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Publication number: 20040053927Abstract: A composition comprises a compound of Formula 1: 1Type: ApplicationFiled: June 23, 2003Publication date: March 18, 2004Inventors: James W. Darrow, Robert W. DeSimone, Douglas A. Pippin, Scott A. Mitchell
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Publication number: 20040049032Abstract: The present invention provides a facile process for the preparation of tri- and tetra-substituted pyrimidines. The process is useful for preparing inhibitors of protein kinases, especially Aurora kinase. These inhibitors are useful for treating or lessening the severity of Aurora-mediated diseases or conditions.Type: ApplicationFiled: June 18, 2003Publication date: March 11, 2004Inventors: Jean-Damien Charrier, Francesca Mazzei, David Kay, Andrew Miller
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Patent number: 6693121Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 4-pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: April 4, 2001Date of Patent: February 17, 2004Assignee: Pharmacia CorporationInventors: Michael S. South, Chun C. Ma, Kevin J. Koeller, Hayat K. Rahman, William L. Neumann
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Publication number: 20040029902Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: January 31, 2003Publication date: February 12, 2004Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sasha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
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Patent number: 6656935Abstract: An aromatic nitrogen-containing 6-membered cyclic compound of the formula (I): wherein Ring A is a substituted or unsubstituted nitrogen-containing heterocyclic group; R1 is a substituted or unsubstituted lower alkyl group, —NH—Q—R3 (R3 is a substituted or unsubstituted nitrogen containing heterocyclic group, and Q is a lower alkylene group or a single bond), or —NH—R4 (R4 is a substituted or unsubstituted cycloalkyl group); R2 is a substituted or unsubstituted aryl group; one of Y and Z is ═CH—, and the other is ═N—, or a pharmaceutically acceptable salt thereof, these compounds exhibiting excellent selective PDE V inhibitory activities, and hence, being useful in the prophylaxis or treatment of penile erectile dysfunction, etc.Type: GrantFiled: August 10, 2001Date of Patent: December 2, 2003Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Koichiro Yamada, Kenji Matsuki, Kenji Omori, Kohei Kikkawa
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Patent number: 6653317Abstract: Hair growth-/hair loss-affecting cosmetic/therapeutic compositions contain an effective amount of at least one 2-amino-4-alkylaminopyrimidine 3-oxide having the structural formula (I): in which R1 is an alkyl radical having from 5 to 20 carbon atoms, and Z is either a hydrogen atom or a radical −OR2, wherein R2 is an alkyl radical having from 1 to 12 carbon atoms, or an acyl derivative or acid addition salt thereof.Type: GrantFiled: November 22, 2002Date of Patent: November 25, 2003Assignee: Societe l'Oreal S.A.Inventors: Yann Mahe, Jean-François Michelet, Patrick Pichaud, Jean-Baptiste Galey
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Patent number: RE39056Abstract: Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5?-reductase inhibitory activity. These compounds inhibit 5?-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.Type: GrantFiled: September 11, 1996Date of Patent: April 4, 2006Assignee: Merck & Co, Inc.Inventors: Raman K. Bakshi, Soumya P. Sahoo, Richard L. Tolman