At 2-position And At 4- Or 6-position Patents (Class 544/323)
-
Publication number: 20090233908Abstract: A compound represented by formula (I): (wherein the symbols are the same as defined in the description), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medicinal use thereof. The compound represented by formula (I) has CXCR4 antagonistic activity. It is hence useful as, e.g., a preventive and/or therapeutic agent for CXCR4-mediated diseases such as inflammatory/immunologic diseases (e.g., rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, and rejection reactions of transplanted organs), allergic diseases, infections diseases (e.g., human immunodeficiency virus infection and acquired immunologic deficiency syndrome), psychoneurotic diseases, cerebral diseases, cardiac/vascular disease, metabolic diseases, cancer diseases (e.g., cancer, cancer metastasis) or as an agent for regeneration therapy.Type: ApplicationFiled: February 24, 2006Publication date: September 17, 2009Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiroshi Ochiai, Akira Ohhata, Yoshikazu Takaoka, Shiro Shibayama
-
Patent number: 7589200Abstract: 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: August 3, 2004Date of Patent: September 15, 2009Assignee: 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
-
Patent number: 7585870Abstract: This invention concerns HIV replication inhibitors of formula (I), the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.Type: GrantFiled: February 20, 2004Date of Patent: September 8, 2009Assignee: Tibotec BVBAInventors: Jerôme Emile Georges Guillemont, Elisabeth Thérese Jeanne Pasquier, Jan Heeres, Kurt Hertogs, Eva Bettens, Paulus Joannes Lewi, Marc René De Jonge, Lucien Maria Henricus Koymans, Frederik Frans Desiré Daeyaert, Hendrik Maarten Vinkers, Frank Xavier Jozef Herwig Arts
-
Publication number: 20090221555Abstract: The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.Type: ApplicationFiled: October 23, 2007Publication date: September 3, 2009Applicants: Cephalon, Inc., Pharmacopeia Drug Discovery, Inc.Inventors: Gulzar Ahmed, Adolph Bohnstedt, Henry Joseph Breslin, Jason Burke, Matthew A. Curry, James L. Diebold, Bruce Dorsey, Benjamin J. Dugan, Daming Feng, Diane E. Gingrich, Tao Guo, Koc-Kan Ho, Keith S. Learn, Joseph G. Lisko, Rong-qiang Liu, Eugen Mesaros, Karen Milkiewicz, Gregory R. Ott, Jonathan Parrish, Jay P. Theroff, Tho V. Thieu, Rabindranath Tripathy, Theodore L. Underiner, Jason C. Wagner, Linda Weinberg, Gregory J. Wells, Ming You, Craig A. Zificsak
-
Patent number: 7582646Abstract: Pyrimidine derivatives of formula (I) in which J and Y represent aromatic or heteroaromatic rings; R2, G, G?, and G? represent substituent groups and R2a represents H or halogen; L represents a linking group; and M represents CH or N. Pharmaceutical compositions containing these compounds, and methods of using these compounds in treatment of hyperproliferative diseases such as cancer are also disclosed and claimed.Type: GrantFiled: March 10, 2005Date of Patent: September 1, 2009Assignee: Bayer Pharmaceuticals CorporationInventors: Julie A. Dixon, Dhanapalan Nagarathnam, Lei Zhang, Chunguang Wang, Lin Yi, Yuanwei Chen, Jianqing Chen, Brian R. Bear, Michael Brands, Alexander Hillisch, Donald Bierer, Ming Wang, Wenlang Fu, Martin F. Hentemann, Ann-Marie Bullion, Manoj Patel
-
Patent number: 7582645Abstract: Pyrimidine derivatives of formula (I) in which J and Y represent aromatic or heteroaromatic rings; R2, G, G?, and G? represent substituent groups and R2a represents H or halogen; L represents a linking group; and M represents CH or N. Pharmaceutical compositions containing these compounds, and methods of using these compounds in treatment of hyperproliferative diseases such as cancer are also disclosed and claimed.Type: GrantFiled: October 8, 2004Date of Patent: September 1, 2009Assignee: Bayer Pharmaceuticals CorporationInventors: Julie A. Dixon, Dhanapalan Nagarathnam, Lei Zhang, Chunguang Wang, Lin Yi, Yuanwei Chen, Jianqing Chen, Brian Bear, Michael Brands, Alexander Hillisch, Donald Bierer, Ming Wang, Wenlang Fu, Martin F. Hentemann, Ann-Marie Bullion
-
Patent number: 7582648Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: GrantFiled: October 5, 2006Date of Patent: September 1, 2009Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Hui Li, Holger Keim
-
Patent number: 7579466Abstract: 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 human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, Crohn's 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: February 26, 2007Date of Patent: August 25, 2009Assignee: Elan Pharmaceuticals, Inc.Inventors: Jenifer Smith, Christopher Semko, Ying-Zi Xu, Andrei W. Konradi
-
Publication number: 20090181995Abstract: The present invention relates to 2-arylamino-4-(aminoalkylene)aminopyrimidines inhibitors which are inhibitors and therefore inhibit Protein Kinase C-alpha (PKC-?). The PKC-? inhibitors of the present invention are important for improving myocardial intracellular calcium cycling, resulting in improved myocardial contraction and relaxation performance and thereby slowing the progression of heart failure. The present invention further relates to compositions comprising said 2-arylamino-4-(aminoalkylene)amino-pyrimidines and to methods for controlling, abating, or otherwise slowing the progression of heart failure.Type: ApplicationFiled: March 26, 2009Publication date: July 16, 2009Applicant: Boehringer Ingelheim International GmbHInventors: Jane Far-Jine DJUNG, Adam GOLEBIOWSKI, Jack A. HUNTER, Gary P. SCHRUM
-
Patent number: 7560466Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: GrantFiled: October 6, 2006Date of Patent: July 14, 2009Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
-
Patent number: 7560464Abstract: The present invention provides a genus of polycyclic pyrimidines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods.Type: GrantFiled: April 13, 2005Date of Patent: July 14, 2009Assignee: Icagen, Inc.Inventors: Xiaodong Wang, Kerry Leigh Spear, Alan Bradley Fulp, Darrick Seconi, Takeshi Suzuki, Takahiro Ishii, Ayako Moritomo
-
Patent number: 7557210Abstract: 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: January 31, 2003Date of Patent: July 7, 2009Assignee: 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
-
Publication number: 20090170854Abstract: The present invention relates to a new use of certain pharmaceutically active compounds in the treatment and/or prevention of medicament induced gastric ulcer. More particularly the invention is directed to the use of said compounds, and pharmaceutically acceptable salts thereof, for the treatment and/or prevention of NSAID (non-steroidal antiinflammatory drugs) induced gastric ulcer as well as a pharmaceutical composition in the unit dosage form for the prevention of NSAID induced gastric ulcer in a mammal comprising an NSAID together with a 6-carboxamido-imidazo[1,2-a]pyridine compounds. Other pharmaceutically active compounds used in the present invention comprises COX-2 inhibitors, NO-NSAIDs and bisphosphonates.Type: ApplicationFiled: August 4, 2008Publication date: July 2, 2009Inventor: Arne Eek
-
Publication number: 20090171085Abstract: 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: November 10, 2008Publication date: July 2, 2009Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Someasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
-
Publication number: 20090163467Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2, R4, X, m, n and p are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: May 11, 2007Publication date: June 25, 2009Inventors: Stephan Karl Zahn, Bojan Bister, Guido Boehmelt, Ulrich Guertler, Andreas Mantoulidis, Ulrich Reiser, Andreas Schoop, Flavio Solca, Ulrike Tontsch-Grunt, Matthias Treu
-
Patent number: 7550460Abstract: 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: July 24, 2007Date of Patent: June 23, 2009Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
-
Patent number: 7550473Abstract: Disclosed are novel compounds of formula (I): wherein R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: September 3, 2004Date of Patent: June 23, 2009Assignees: Boehringer Ingelheim Pharmaceuticals, Inc., Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Mario G. Cardozo, Derek Cogan, Charles Lawrence Cywin, George Dahmann, Darren DiSalvo, John David Ginn, Anthony S. Prokopowicz, III, Denice M. Spero, Erick Richard Roush Young
-
Patent number: 7541360Abstract: The present invention relates to the area of NO synthase inhibition and, more particularly, relates to novel 4-amino-7,8-dihydropteridines, pharmaceutical compositions containing said compounds, and the use of said compounds in the treatment of a disorder characterized by a disturbed nitric oxide level.Type: GrantFiled: December 30, 2003Date of Patent: June 2, 2009Assignee: Vasopharm GmbHInventors: Robert Doblhofer, Frank Tegtmeier
-
Publication number: 20090130487Abstract: The inventive method for placing and fixing (bonding) a first object, whose surface is functionalized by compounds of formula I Y (X), A? (I), on the surface of a second object whose surface is functionalized by compounds of formula II Y (X)n A (II), wherein A and A? are functional groups enabling to be bonded at least by a link in a covalent manner to an object surface X and X? are aliphatic, linear, branched or cyclic spacers which can comprise one or several hetero, or aromatic, or heteroaromatic atoms or consist of several aromatic or heteroaromatic cycles and optionally of alternating aliphatic chains having aromatic or heteroaromatic groups, n and n?=0 or 1 and Y and Y are functions for generating one or several non-covalent bonds wherein said Y or Y? are selected such that they are complementary or can complex a metal atom or an identical metal compound.Type: ApplicationFiled: June 12, 2006Publication date: May 21, 2009Applicant: Commissariat A L'Energie AtomiqueInventors: Renaud Demadrille, Stephane Guillerez
-
Publication number: 20090124644Abstract: HIV replication inhibitors of formula pharmaceutically acceptable addition salts or stereochemically isomeric forms thereof, wherein X is NR4, S, SO or SO2; the preparation of these compounds as well as pharmaceutical compositions comprising these compounds; the use of these compounds for the prevention or the treatment of HIV infection.Type: ApplicationFiled: January 27, 2006Publication date: May 14, 2009Applicant: JANSSEN PHARMACEUTICA N.V.Inventors: Jan Heeres, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, Rudolf Leemans, Luc Jozef Raphael Moens
-
Patent number: 7531547Abstract: Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): wherein D, X, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.Type: GrantFiled: August 25, 2006Date of Patent: May 12, 2009Assignee: Roche Palo Alto LLCInventors: Michael Patrick Dillon, Alam Jahangir, Amy Geraldine Moore, Paul J. Wagner
-
Patent number: 7528143Abstract: The invention provides biaryl meta-pyrimidine compounds having the general structure (A). The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Jak kinase family, and various other specific receptor and non-receptor kinases.Type: GrantFiled: October 26, 2006Date of Patent: May 5, 2009Assignee: TargeGen, Inc.Inventors: Glenn Noronha, Chi Ching Mak, Jianguo Cao, Joel Renick, Andrew McPherson, Binqi Zeng, Ved P. Pathak, Daniel L. Lohse, John D. Hood, Richard M. Soll
-
Patent number: 7524849Abstract: This invention relates to certain 5-arylpyrimidine compounds or a pharmaceutically acceptable salt thereof, and compositions containing said compounds or a pharmaceutically acceptable salt thereof, wherein said compounds are anti-cancer agents useful for the treatment of cancer in mammals. This invention further relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal and further provides a method for the treatment or prevention of cancerous tumors that express multiple drug resistance (MDR) or are resistant because of MDR, in a mammal in need thereof which method comprises administering to said mammal an effective amount of said compounds or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 24, 2004Date of Patent: April 28, 2009Assignee: Wyeth Holdings CorporationInventors: Nan Zhang, Semiramis Ayral-Kaloustian, Thai Nguyen
-
Patent number: 7521457Abstract: The present invention encompasses compounds of general formula (1), wherein A, W, X, Y, Z, Ra, Rb, Rc, R1 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: GrantFiled: August 17, 2005Date of Patent: April 21, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Harald Engelhardt, Martin Steegmaier, Anke Baum, Ulrich Guertler, Andreas Schoop, Jens Juergen Quant, Flavio Solca, Rudolf Hauptmann, Ulrich Reiser, Stephan Karl Zahn, Lars Herfurth
-
Patent number: 7521446Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.Type: GrantFiled: April 26, 2006Date of Patent: April 21, 2009Assignee: Signal Pharmaceuticals, LLCInventors: Ronald J. Albers, Leticia Ayala, Steven S. Clareen, Maria Mercedes Delgado Mederos, Robert Hilgraf, Kevin Hughes, Adam Kois, Veronique Plantevin-Krenitsky, Meg McCarrick, Lisa Nadolny, Moorthy S. S. Palanki, Kiran Sahasrabudhe, Yoshitaka Satoh, Marianne K. Sloss, Elise Sudbeck, Jonathan Wright
-
Publication number: 20090099183Abstract: The invention relates to pyrimidines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase ? (LPAAT-?) activity and/or proliferation of cells such as tumor-cells.Type: ApplicationFiled: August 19, 2008Publication date: April 16, 2009Applicant: Cell Therapeutics, Inc.Inventors: Rama BHATT, Baoqing GONG, Feng HONG, Scott A. JENKINS, J. Peter KLEIN, Cory T. KOHM, John TULINSKY
-
Publication number: 20090099220Abstract: The present invention relates to novel compounds that are inhibitors of wild type and mutant dihydrofolate reductase (DHFR) of Plasmodium falciparum, which are useful for the treatment of malaria. It also relates to processes of making and using such compounds. The antimalarial compounds of the present invention have low toxicity to a host infected with the malarial parasite, and are potent when administered in pharmaceutical compositions.Type: ApplicationFiled: October 8, 2008Publication date: April 16, 2009Inventors: Yongyuth YUTHAVONG, Tirayut Vilaivan, Sumalee Kamchonwongpaisan, Bongkoch Tarnchompoo, Chawanee Thongpanchang, Penchit Chitnumsub, Jirundon Yuvaniyama, David Matthews, William Charman, Susan Charman, Livia Vivas, Sanjay Babu Katiyar
-
Patent number: 7511052Abstract: 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 human or animal subject 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: September 28, 2006Date of Patent: March 31, 2009Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Christopher Michael Semko, Ying-zi Xu, Frank Stappenbeck, Jenifer Lea Smith, Kassandra Inez Rossiter, Juri Y. Fukuda, Andrei W. Konradi
-
Publication number: 20090081145Abstract: The present invention relates to an improved method of formation of disulfide bridges in substances bearing SH groups, in particular peptides, for example by formation of intramolecular disulfide bridges, in which a heterocyclic compound having at least one nitrogen atom (e.g. caffeine or a caffeine-like substance) is used for catalysis of the reaction. It was found, surprisingly, that addition of the heterocyclic substance increases both the yield and the purity of the product bearing disulfide bridges.Type: ApplicationFiled: December 23, 2006Publication date: March 26, 2009Applicant: AplaGen GmbHInventors: Karsten Knorr, Marco Emgenbroich, Carsten Bungener
-
Publication number: 20090075188Abstract: This invention provides an azo compound represented by Formula (I), Formula (II), or Formula (III): wherein R1 and R2 each independently represent a hydrogen atom or a substituent; D1 and D2 each independently represent a coupler residue; Z1 and Z2 each independently represent —C(R3)? or —N?; and R3 represents a hydrogen atom or a substituent.Type: ApplicationFiled: September 12, 2008Publication date: March 19, 2009Applicant: FUJIFILM CORPORATIONInventors: Yuki MIZUKAWA, Hideki Takakuwa, Toru Fujimori
-
Patent number: 7504410Abstract: 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 diseases.Type: GrantFiled: November 28, 2003Date of Patent: March 17, 2009Assignee: Schering AktiengesellschaftInventors: 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 I. Feldman, Gary B. Phillips
-
Patent number: 7498435Abstract: 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: October 5, 2006Date of Patent: March 3, 2009Assignee: 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
-
Publication number: 20090054395Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide 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: ApplicationFiled: April 17, 2008Publication date: February 26, 2009Inventors: Michael Joseph Luzzio, Kevin Daniel Freeman-Cook, Samit Kumar Bhattacharya, Matthew Merrill Hayward, Catherine Angela Hulford, Christopher Lowell Autry, Xumiao Zhao, Jun Xiao, Kendra Louise Nelson
-
Patent number: 7491732Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.Type: GrantFiled: June 8, 2006Date of Patent: February 17, 2009Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, David Carroll, Ankush Argade, Robin Cooper, Rajinder Singh
-
Publication number: 20090041786Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.Type: ApplicationFiled: August 18, 2008Publication date: February 12, 2009Inventors: Hui Li, Sambaiah Thota, David Carroll, Ankush Argade, Kin Tso, Arvinder Sran, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Vanessa Taylor, Robin Cooper, Rajinder Singh, Brian Wong
-
Patent number: 7485724Abstract: 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: October 5, 2006Date of Patent: February 3, 2009Assignee: 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
-
Publication number: 20090023729Abstract: The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted heterocyclic group, and the like; R1 is an optionally substituted alkyl group, wherein the alkyl group further may optionally be substituted by an optionally substituted homocyclic group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.Type: ApplicationFiled: July 28, 2008Publication date: January 22, 2009Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Yoshinori Nakamura, Norimitsu Hayashi, Takanori Higashijima, Hitoshi Kubota, Kozo Oka
-
Patent number: 7479495Abstract: 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: June 2, 2005Date of Patent: January 20, 2009Assignees: Pharmacopeia, Inc., Bristol-Myers Squibb CompanyInventors: Kevin Joseph Moriarty, Yvonne Shimshock, Gulzar Ahmed, Junjun Wu, James Wen, Wei Li, Shawn David Erickson, Jeffrey John Letourneau, Edward McDonald, Katerina Leftheris, Stephen T. Wrobleski, Zahid Hussain, Ian Henderson, Axel Metzger, John J. Baldwin, Alaric J. Dyckman
-
Publication number: 20090012108Abstract: The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethyl-phenyl]amino]-2-pyrimidinyl]amino]benzonitrile and to processes for their preparation.Type: ApplicationFiled: July 7, 2008Publication date: January 8, 2009Inventors: Jerome Emile Guillemont, Paul Theodoor Agnes Stevens, Alex Herman Copmans, Jozef Peeters, Alfred Elisabeth Stappers, Roger Petrus Gerebern Vandecruys, Paul Stoffels
-
Patent number: 7470700Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV inhibitors comprising Formula I: wherein the substituents are as described herein.Type: GrantFiled: August 12, 2004Date of Patent: December 30, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Jun Feng, Stephen L. Gwaltney, II, Stephen W. Kaldor, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
-
Publication number: 20080318929Abstract: Disclosed are novel compounds of formula (I) wherein R1, R2, R3, and R4 and A are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: December 12, 2006Publication date: December 25, 2008Inventors: Antonio J.M. Barbosa, Steven Richard Brunette, Eugene Richard Hickey, Michael David Lawlor, Matt Aaron Tschantz
-
Publication number: 20080318989Abstract: The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula (I) wherein ring A, X, Y, Z, R1, R2, R3, R4, m and n are as defined herein.Type: ApplicationFiled: December 15, 2006Publication date: December 25, 2008Inventors: Daniel J. Burdick, Jun Liang
-
Publication number: 20080312438Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: ApplicationFiled: October 5, 2006Publication date: December 18, 2008Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder SINGH, Ankush ARGADE, Hui Li, Somasekhar BHAMIDIPATI, David CARROLL, Catherine SYLVAIN, Jeffrey CLOUGH, Holger KEIM
-
Patent number: 7465736Abstract: An azole derivative of formula (I) a medicament that contains the azole derivative of formula (I), a method of treating a disease with the azole derivative of formula (I), and a method of preparing the azole derivative of formula (I).Type: GrantFiled: June 13, 2003Date of Patent: December 16, 2008Assignee: Laboratoires Serono S.A.Inventors: Pascale Gaillard, Jean-Pierre Gotteland, Isabelle Jeanclaude-Etter, Matthias Schwarz, Russel J. Thomas
-
Patent number: 7459455Abstract: Pyrimidine derivatives, which are useful as TIE-2 and/or VEGFR-2 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: February 7, 2003Date of Patent: December 2, 2008Assignee: SmithKline Beecham CorporationInventors: Mui Cheung, Kristen Elizabeth Nailor, Douglas McCord Sammond, James Marvin Veal
-
Patent number: 7452879Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: GrantFiled: October 5, 2006Date of Patent: November 18, 2008Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
-
Publication number: 20080279867Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.Type: ApplicationFiled: March 21, 2008Publication date: November 13, 2008Inventors: Andy Atuegbu, Vadim Markovtsov, Somasekhar Bhamidipati, Rajinder Singh, Vanessa Taylor, Sambaiah Thota, Jeffrey Wayne Clough, David Carroll, Hui Li, Robin Cooper
-
Patent number: 7449474Abstract: The present invention relates to 1,1,3-tri-substituted ureas which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions comprising said 1,1,3-tri-substituted ureas which inhibit the extracellular release of inflammatory cytokines, and methods for preventing, abating, or otherwise controlling enzymes which are understood to be the active components responsible for the herein described disease states.Type: GrantFiled: April 21, 2005Date of Patent: November 11, 2008Assignee: The Procter & Gamble CompanyInventors: Todd Andrew Brugel, Jennifer Anne Townes, Michael Philip Clark, Mark Sabat, Adam Golebiowski, Biswanath De, Stephen Matthew Berberich, Gregory Kent Bosch
-
Patent number: 7449456Abstract: A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.Type: GrantFiled: June 26, 2003Date of Patent: November 11, 2008Assignee: Astellas Pharma, Inc.Inventors: Shinya Nagashima, Hiroshi Nagata, Masahiro Iwata, Masaki Yokota, Hiroyuki Moritomo, Eiichi Nakai, Sadao Kuromitsu, Keiko Ohga, Makoto Takeuchi
-
Patent number: 7442698Abstract: The present invention relates to pyrimidine or pyridine carbamate compounds having the general Formula I: and pharmaceutically acceptable salts or derivatives thereof. Also included are methods of treatment of various diseases and conditions, including inflammation, inhibition of T cell activation and proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma, thymoma, just to name a few, in a mammal, the methods comprising administering a therapeutically-effective amount a compound of Formula I, or a salt or derivative form thereof, as described above.Type: GrantFiled: July 13, 2004Date of Patent: October 28, 2008Assignee: Amgen Inc.Inventors: John L. Buchanan, Daniel Elbaum, Matthew W. Martin, David C. McGowan, Perry M. Novak, Joseph J. Nunes