Additional Hetero Ring Which Is Unsaturated Patents (Class 544/324)
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Patent number: 7253174Abstract: N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-? expression utilizing compounds of the present invention are also disclosed.Type: GrantFiled: July 12, 2006Date of Patent: August 7, 2007Assignees: Bristol-Myers Squibb Company, Pharmacopeia, Inc.Inventors: Gulzar Ahmed, Axel Metzger, Ian Henderson, David J. Diller, Jun Wen, Stephen T. Wrobleski, Katerina Leftheris, Chunjian Liu
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Patent number: 7241769Abstract: The present invention comprises compounds of general formula (1) wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, and the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.Type: GrantFiled: May 18, 2005Date of Patent: July 10, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Harald Engelhardt, Ulrich Reiser, Stephan Karl Zahn, Rudolf Hauptmann, Martin Steegmaier, Ulrich Guertler, Matthias Hoffmann, Matthias Grauert
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Patent number: 7235562Abstract: The present invention relates to a compound of the formula 1 wherein R1-R4 and Ar are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: May 12, 2005Date of Patent: June 26, 2007Assignee: Pfizer IncInventors: John Charles Kath, Michael Joseph Luzzio
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Patent number: 7230104Abstract: Pyrimidines of formula I in which R1 represents hydrogen or alkyl, haloalkyl, alkenyl, alkynyl, alkadienyl, alkoxy, cycloalkyl, phenyl, or 5- or 6-membered heteroaryl or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or tri-alkyl-silyl, formyl or alkoxy-carbonyl, wherein R1 groups are unsubstituted or substituted as defined in the specification; R2 represents phenyl, cycloalkyl or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, which are unsubstituted or substituted; R3 represents hydrogen, halogen or alkyl, alkoxy, alkylthio, alkylamino or dialkylamino; which are unsubstituted or substituted; R4 represents hydrogen or alkyl, alkenyl or alkynyl; which are unsubstituted or substituted; and X represents O, S, NR5 or a single bond, wherein R5 represents hydrogen or alkyl; or R1 and R5 together with the interjacent nitrogen atom form a heteroType: GrantFiled: July 22, 2005Date of Patent: June 12, 2007Assignee: BASF AktiengesellschaftInventors: Klaus-Juergen Pees, Waldemar Pfrengle, Gavin Heffernan
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Patent number: 7220736Abstract: A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ?CH— or ?N—, Y is —NH—, —NR4—, —S—, —O—, —CH?N—, —N?CH—, —N?N—, —CH?CH—, etc., R1 is a lower alkoxy group, an amino group, a heterocyclic ring containing N atom(s), or a hydroxy group substituted by a heterocyclic ring containing N atom(s) (each of which is optionally substituted), R2 is a lower alkylamino group which is optionally substituted by an aryl group, a lower alkoxy group which is optionally substituted by an aryl group, a lower alkoxy group substituted by an aromatic heterocyclic ring containing N atom(s), R3 is an aryl group, a heterocyclic ring containing N atom(s), a lower alkyl group, a lower alkoxy group, a cyclo lower alkoxy group, a hydroxy group substituted by a heterocyclic ring containing N atom(s), or an amino group (each of which is optionally substituted), and R3 and a substituent in Y may be combined to form a lactone ring.Type: GrantFiled: March 15, 2001Date of Patent: May 22, 2007Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Koichiro Yamada, Kenji Matsuki, Kenji Omori, Kohei Kikkawa
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Patent number: 7208499Abstract: The present invention relates to a compound of the formula 1 wherein A and Ar are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: May 6, 2005Date of Patent: April 24, 2007Assignee: Pfizer Inc.Inventors: John Charles Kath, Michael Joseph Luzzio
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Patent number: 7205307Abstract: The present invention provides a genus of pyrimidine amides that are useful as openers of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.Type: GrantFiled: November 27, 2002Date of Patent: April 17, 2007Assignee: Icagen, Inc.Inventors: Grant A. McNaughton-Smith, George S. Amato, Paul C. Fritch
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Patent number: 7205310Abstract: Disclosed are compounds which bind VLA-4 and/or LPAM-1. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4 and/or LPAM-1. 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: April 29, 2005Date of Patent: April 17, 2007Assignee: Elan Pharmaceuticals, Inc.Inventors: Andrei W. Konradi, Frank Stappenbeck, Michael A. Pleiss, Christopher Semko, Jenifer L. Smith
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Patent number: 7179816Abstract: The present invention relates to cancer therapy and to novel anticancer agents having a mechanism of action which inhibits telomerase. It also relates to novel chemical compounds as well as their therapeutic application in humans.Type: GrantFiled: September 30, 2004Date of Patent: February 20, 2007Assignee: Aventis Pharma S.A.Inventors: Patrick Mailliet, Jean-Francois Riou, Marcel Alasia, Thomas Caulfield, Gilles Doerflinger, Jean-Louis Mergny, Abdelazize Laoui, Odile Petitgenet, Emmanuelle Renou
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Patent number: 7173028Abstract: The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterised by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.Type: GrantFiled: October 16, 2002Date of Patent: February 6, 2007Assignees: Boehringer Ingelheim Pharma GmbH & Co. KG, Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Georg Dahmann, Frank Himmelsbach, Bernd Krist, Martin Lenter, Alexander Pautsch, Gisela Schnapp, Martin Steegmaier, Helmut Wittneben, Anthony S. Prokopowicz, Walter Spevak, Andreas Schoop, Steffen Steurer
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Patent number: 7166599Abstract: The present invention relates to trisubstituted pyrimidines of formula wherein Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses in which ?-amyloid modulators have a therapeutic benefit, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.Type: GrantFiled: December 9, 2004Date of Patent: January 23, 2007Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Klaus Bornemann, Hans Briem, Cornelia Dorner-Ciossek, Katja Fechteler, Klaus Fuchs, Frank Himmelsbach, Klaus Klinder, Markus Kostka
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Patent number: 7157455Abstract: Novel 4-aminopyrimidine-5-one derivatives are disclosed. These compounds inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors. Also disclosed are intermediates useful in the preparation of these novel 4-aminopyrimidine-5-one derivatives.Type: GrantFiled: February 2, 2004Date of Patent: January 2, 2007Assignee: Hoffmann-La Roche Inc.Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Qingjie Ding, Nan Jiang, Allen John Lovey, John Anthony Moliterni, John Guilfoyle Mullin, Jr., Binh Thanh Vu, Peter Michael Wovkulich
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Patent number: 7153860Abstract: The invention relates to 5-phenylpyrimidine of formula (I) wherein the substituents have the following designations: R1 represents a five to ten-membered saturated, partially unsaturated or aromatic monocyclic or bicyclic heterocycle which contains between one and four heteroatoms from the group O, N or S, and which can be substituted as defined in the description; R2 represents hydrogen, halogen, cyano, alkyl, halogenalkyl or alkoxy; R3 and R4 represent hydrogen, alkyl, halogenalkyl, cycloalkyl, halogencycloalkyl, alkenyl, halogenalkenyl, cycloalkenyl, alkinyl, halogenalkinyl or cycloalkinyl; together with the nitrogen atom to which they are bonded, R3 and R4 can also form a five or six-membered ring which can be split by a heteroatom and can carry at least one substituent; R5 and R6 represent hydrogen, halogen, alkyl, halogenalkyl or alkoxy; R1 and R8 represent hydrogen, halogen, alkyl or halogenalkyl; and R9 represents hydrogen, halogen, alkyl, alkoxy, cycloalkoxy, halogenalkoxy or alkoxycarbonyl.Type: GrantFiled: March 13, 2002Date of Patent: December 26, 2006Assignee: BASF AktiengesellschaftInventors: Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Ingo Rose, Peter Schäfer, Frank Schieweck, Hubert Sauter, Markus Gewehr, Bernd Müller, Jordi Tormo i Blasco, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Patent number: 7153964Abstract: Pyrimidine derivatives of formula (I) wherein: Qh1 and Q2 are independently selected from aryl or carbon linked heteroaryl optionally substituted as defined within; and one of Q1 and Q2 or both Q1 and Q2 is substituted on a ring carbon by one group selected from sulphamoyl, N—(C1-4alkyl)sulphamoyl (optionally substituted by halo or hydroxy), N,N-di-(C1-4alkyl)sulphamoyl (optionally substituted by halo or hydroxy), C1-4alkylsulphonyl (optionally substituted by halo or hydroxy) or a substituent of the formula (Ia) or (Ia?): wherein Q1, Q2, G, R1, Y, Z, Q3, n and m are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described.Type: GrantFiled: February 26, 2001Date of Patent: December 26, 2006Assignee: AstraZeneca ABInventors: Elizabeth Janet Pease, Gloria Anne Breault, Jeffrey James Morris
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Patent number: 7151106Abstract: The invention relates to a new crystalline form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide of formula 1, which may be used for example for tumor therapy.Type: GrantFiled: November 16, 2001Date of Patent: December 19, 2006Assignee: Novartis A.G.Inventor: Pekka Hayry
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Patent number: 7148219Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: GrantFiled: April 29, 2005Date of Patent: December 12, 2006Assignee: Rib-X Pharmaceuticals, Inc.Inventors: Rongliang Lou, Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Patent number: 7145008Abstract: The present invention relates to a compound of the formula 1 or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof, wherein R1–R4 and Ar are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: May 5, 2005Date of Patent: December 5, 2006Assignee: Pfizer IncInventors: John Charles Kath, Michael Joseph Luzzio
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Patent number: 7135477Abstract: 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: November 14, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Andrei W. Konradi, Christopher M. Semko, Ying-zi Xu, Frank Stappenbeck, Brian P. Stupi, Jenifer Smith, Michael A. Pleiss, Eugene D. Thorsett
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Patent number: 7122552Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of JAK and CDK2 mammalian protein kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.Type: GrantFiled: May 30, 2003Date of Patent: October 17, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventor: Brian E. Ledford
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Patent number: 7122670Abstract: The present invention relates to a method of making a compound of the formula wherein X1, X2 and R3—R4 are as defined herein. The method includes reacting a compound of the formula with an amine of formula 3 (HNR3R4) in the presence of a Lewis Acid and a non-nucleophilic base. The 2,4-diamino pyrimidine moiety is a common component in a variety of biologically active drug-like molecules and pyrimidine derivatives have been found to be useful in the treatment of abnormal cell growth, such as cancer, in mammals.Type: GrantFiled: August 27, 2004Date of Patent: October 17, 2006Assignee: Pfizer IncInventors: John Charles Kath, Daniel Tyler Richter, Michael Joseph Luzzio
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Patent number: 7115617Abstract: The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer.Type: GrantFiled: August 21, 2002Date of Patent: October 3, 2006Assignee: Amgen Inc.Inventors: John L. Buchanan, Stuart Chaffee, Jean-Christophe Harmange, Perry M. Novak, Xiaotian Zhu
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Patent number: 7109336Abstract: A compound represented by the following formula (I) or formula (2-I)Type: GrantFiled: April 8, 2002Date of Patent: September 19, 2006Assignee: Fuji Photo Film Co., Ltd.Inventors: Toshiki Fujiwara, Naoyuki Hanaki, Shigeaki Tanaka, Tadashi Omatsu, Yoshiharu Yabuki
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Patent number: 7109335Abstract: The present invention relates to a compound of the formula 1 wherein R1–R4 are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: December 11, 2003Date of Patent: September 19, 2006Assignee: Pfizer IncInventors: John Charles Kath, Michael Joseph Luzzio
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Patent number: 7109337Abstract: The present invention relates to a compound of the formula 1 wherein R1–R4 are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: May 12, 2005Date of Patent: September 19, 2006Assignee: Pfizer IncInventors: John Charles Kath, Michael Joseph Luzzio
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Patent number: 7109204Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: GrantFiled: July 26, 2002Date of Patent: September 19, 2006Assignee: Merck & Co., Inc.Inventors: Mark E. Fraley, Kenneth L. Arrington, William F. Hoffman, George D. Hartman, Jennifer P. Peckham
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Patent number: 7105530Abstract: Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also Includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.Type: GrantFiled: December 19, 2001Date of Patent: September 12, 2006Assignee: SmithKline Beecham CorporationInventors: Amogh Boloor, Mui Cheung, Ronda Davis, Philip Anthony Harris, Kevin Hinkle, Robert Anthony Mook, Jr., Jeffery Alan Stafford, James Marvin Veal
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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: 7091343Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: March 14, 2003Date of Patent: August 15, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M. C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
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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: 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: 7034031Abstract: The present invention provides compounds which are modulators of TNF-? signaling and methods of use thereof for treating a patient having a TNF-? mediated condition.Type: GrantFiled: March 10, 2004Date of Patent: April 25, 2006Assignee: Genzyme CorporationInventors: Scott F. Sneddon, John L. Kane, Bradford H. Hirth, Fred Vinick, Shuang Qiao, Sharon R. Nahill, John M. Williams, Hans-Peter Biemann
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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: 6958332Abstract: This invention features pyrimidine compounds of formula (I): each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.Type: GrantFiled: September 5, 2003Date of Patent: October 25, 2005Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Mitsunori Ono, Teresa Przewloka, Elena Kostik, Yumiko Wada
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Patent number: 6958340Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: GrantFiled: July 26, 2002Date of Patent: October 25, 2005Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, Peter J. Manley, Adrienne Balitza, George D. Hartman, Leonard Rodman
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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: 6939874Abstract: The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer.Type: GrantFiled: August 21, 2002Date of Patent: September 6, 2005Assignee: Amgen Inc.Inventors: Jean-Christophe Harmange, John L. Buchanan, Stuart Chaffee, Perry M. Novak, Simon Van Der Plas, Xiaotian Zhu
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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: 6921821Abstract: This invention provides compounds that are antagonists of melanin concentrating hormone receptor-1 (MCH-R1). The compounds are represented by formula I: where m is zero or one, n is zero to two, Y is oxygen or —N(R9)—, R1, R2, R3, R4, R5, R9 and Ring A are defined in the specification. Coumarin and quinolone compounds where R1 and R2 together form a fused benzo ring are preferred. The invention also provides compounds of formula VI where the coumarin moiety is replaced by a quinazolinone ring. The compounds are useful for treating MCH-R1-related disorders, particularly overweight conditions including obesity.Type: GrantFiled: June 11, 2003Date of Patent: July 26, 2005Assignee: Abbott LaboratoriesInventors: Christopher Blackburn, Su-Jen Lai, Jennifer L. Che, Martin P. Maguire, Michael A. Patane, Matthew J. LaMarche, Courtney A. Cullis, James Brown, Anil Vasudevan, Jennifer C. Freeman, Mathew M. Mulhern, John K. Lynch, Ju Gao, Dariusz Wodka, Andrew J. Souers, Rajesh Iyengar, Mary Katherin Verzal, Philip R. Kym
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Patent number: 6919347Abstract: Bradykinin B1-receptor antagonists of formula are disclosed. The compounds are useful for treating diseases associated with inappropriate bradykinin receptor activity, such as diabetic vasculopathy, inflammation, pain, hyperalgesia, asthma, rhinitis, septic shock, atherosclerosis and multiple sclerosis. Pyrimidines, triazines, and anilines in which Q is imidazolyl or pyrrolyl are particularly preferred.Type: GrantFiled: January 14, 2002Date of Patent: July 19, 2005Assignee: Pharmacopeia Drug Discovery, Inc.Inventors: Michael H. J. Ohlmeyer, John J. Baldwin, Roland E. Dolle, III, Vidyadhar Paradkar, Jorge Gabriel Quintero, Gonghua Pan
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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: 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: 6894061Abstract: This invention provides a compound of formulae (I) or (II) having the structure or a pharmaceutically acceptable salt thereof which are useful for the treatment of the inflammatory component of diseases and are particularly useful in treating atherosclerosis, myocardial infarction, congestive heart failure, inflammatory bowel disease, arthritis, type II diabetes, and autoimmune diseases such as multiple sclerosis and rheumatiod arthritis.Type: GrantFiled: November 20, 2003Date of Patent: May 17, 2005Assignee: WyethInventors: Albert John Molinari, Mark Antony Ashwell, Brian Hugh Ridgway, Amedeo Arturo Failli, William Jay Moore
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Patent number: 6891039Abstract: Compounds of formula (I) and pharmaceutically-acceptable and pharmaceutically-acceptable and -cleavable esters thereof and acid addition salts thereof, wherein the symbols are as defined are MAP kinase inhibitors, useful pharmaceutically for treating TNF? and IL-1 mediated diseases such as rheumatoid arthritis and diseases of bone metabolism, e.g. osteoporosis.Type: GrantFiled: June 23, 2003Date of Patent: May 10, 2005Assignee: Novartis AGInventor: Lászlo Révész