At 2-position And At 4- Or 6-position Patents (Class 544/323)
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Patent number: 8431589Abstract: There are provided compounds of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as indicated in claim 1 , useful in disorders where ZAP-70 and/or Syk inhibition plays a role or caused by a malfunction of signal cascades connected with FAK.Type: GrantFiled: March 23, 2011Date of Patent: April 30, 2013Assignee: Novartis AGInventors: Rolf Baenteli, Gerhard Zenke, Nigel Graham Cooke, Rudolf Duthaler, Gebhard Thoma, Anette Von Matt, Toshiyuki Honda, Naoko Matsuura, Kazuhiko Nonomura, Osamu Ohmori, Ichiro Umemura, Klaus Hinterding, Christos Papageorgiou
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Publication number: 20130102781Abstract: Disclosed are processes for preparing cocrystals, including processes for scaling up of cocrystal formation, as well as scalable processes for preparing cocrystals. Also disclosed are processes for scaled-up preparation of pterostilbene, progesterone, p-coumaric, and minoxidil cocrystals. Minoxidil cocrystals, such as minoxidil:benzoic acid 1:1 monohydrate cocrystals are also disclosed herein.Type: ApplicationFiled: October 22, 2012Publication date: April 25, 2013Applicant: APTUIT (WEST LAFAYETTE), LLCInventor: Aptuit (West Lafayette), LLC
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Patent number: 8426434Abstract: This invention concerns polymorph I of TMC278, its use and preparation. It further concerns pharmaceutical formulations comprising this polymorph.Type: GrantFiled: July 11, 2008Date of Patent: April 23, 2013Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Sigrid Carl Maria Stokbroekx, Carina Leys, Elisabeth Maria Hélène Egide Ghislaine Theunissen, Lieven Elvire Colette Baert
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Patent number: 8426432Abstract: The compositions and methods described herein discloses the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus, fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii. These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.Type: GrantFiled: June 4, 2008Date of Patent: April 23, 2013Assignee: University of ConnecticutInventors: Amy C. Anderson, Dennis L. Wright, Phillip M. Pelphrey, Tammy M. Joska, Erin S. D. Bolstad, David B. Bolstad, Veljko Popov
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Patent number: 8426404Abstract: The invention provides a novel class of compounds having Formula Ia, wherein each variable is as defined; and pharmaceutical compositions comprising such compounds and methods of using such compounds for inhibiting c-Src, FGFR3, KDR and/or Lck.Type: GrantFiled: June 30, 2006Date of Patent: April 23, 2013Assignee: Novartis AGInventors: Guobao Zhang, Pingda Ren, Xia Wang, Nathanel Gray, Taebo Sim
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Patent number: 8420630Abstract: 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 characterized 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: February 24, 2010Date of Patent: April 16, 2013Assignees: 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: 8420659Abstract: 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: GrantFiled: August 7, 2012Date of Patent: April 16, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Somasekhar Bhamidipati, Hui Li, Rajinder Singh, Vanessa Taylor, Jeffrey Clough, Darren McMurtrie
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Publication number: 20130090310Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.Type: ApplicationFiled: November 26, 2012Publication date: April 11, 2013Applicant: RIGEL PHARMACEUTICALS, INC.Inventor: RIGEL PHARMACEUTICALS, INC.
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Patent number: 8415365Abstract: 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: February 12, 2008Date of Patent: April 9, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: 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
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Patent number: 8415366Abstract: 2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: GrantFiled: March 8, 2011Date of Patent: April 9, 2013Assignee: Janssen Pharmaceutica NVInventors: James P. Edwards, Brad M. Savall
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Patent number: 8415486Abstract: The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.Type: GrantFiled: May 27, 2010Date of Patent: April 9, 2013Assignee: TetraLogic Pharmaceuticals Corp.Inventors: Stephen M. Condon, Yijun Deng, Matthew D. Alexander, Matthew G. Laporte
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Patent number: 8410126Abstract: Compounds of general formula (1) wherein A, B, R1 to R5, Rx m, n and p are defined as described in the specification, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and the use thereof [as] medicaments.Type: GrantFiled: May 21, 2010Date of Patent: April 2, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Ioannis Sapountzis, Daniel Kuhn, Heinz Stadtmueller
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Publication number: 20130072469Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: November 7, 2012Publication date: March 21, 2013Applicant: CELGENE AVILOMICS RESEARCH, INC.Inventor: Celgene Avilomics Research, Inc.
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Patent number: 8399683Abstract: The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.Type: GrantFiled: September 16, 2009Date of Patent: March 19, 2013Assignee: TetraLogic PharmaceuticalsInventors: Stephen M. Condon, Matthew G. Laporte
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Patent number: 8399472Abstract: 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: August 18, 2008Date of Patent: March 19, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: 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
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Patent number: 8399450Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.Type: GrantFiled: June 29, 2011Date of Patent: March 19, 2013Assignee: IRM LLCInventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
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Publication number: 20130065879Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: November 7, 2012Publication date: March 14, 2013Applicant: CELGENE AVILOMICS RESEARCH, INC.Inventor: Celgene Avilomics Research, Inc.
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Patent number: 8389442Abstract: The use of fungicidal compounds of formula Ij wherein A and A? are both N or A and A? are both CH or A is CH and A? is N; j is 0 or 1 and the R groups are as defined in claim 1; their preparation and compositions 10 comprising the compounds.Type: GrantFiled: March 25, 2004Date of Patent: March 5, 2013Assignee: Syngenta Crop Protection LLCInventors: Peter Ackermann, Daniel Stierli, Martin Diggelmann, Fredrik Cederbaum, Jean Wenger, Ruud Titulaer
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Patent number: 8372858Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.Type: GrantFiled: March 15, 2011Date of Patent: February 12, 2013Assignee: IRM LLCInventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
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Patent number: 8367688Abstract: 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: April 13, 2010Date of Patent: February 5, 2013Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Christopher Michael Semko, Ying-zi Xu, Frank Stappenbeck, Jenifer Lea Smith, Kassandra Inez Rossiter, Juri Y. Fukuda, Andrei W. Konradi
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Patent number: 8367689Abstract: The present invention is directed to compounds of formula I and tautomers and pharmaceutically acceptable salts thereof which are selective inhibitors of JAK. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK activity, and methods to prevent or treat a number of conditions mediated at least in part by JAK activity.Type: GrantFiled: May 6, 2010Date of Patent: February 5, 2013Assignee: Portola Pharmaceuticals, Inc.Inventors: Shawn M. Bauer, Jack W. Rose, Yonghong Song, Qing Xu, Mukund Mehrotra, Wolin Huang, Anjali Pandey
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Publication number: 20130029987Abstract: Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.Type: ApplicationFiled: April 20, 2012Publication date: January 31, 2013Inventors: Brydon L. Bennett, Jan Elsner, Paul Erdman, Robert Hilgraf, Laurie Ann LeBrun, Meg McCarrick, Mehran F. Moghaddam, Mark A. Nagy, Stephen Norris, David A. Paisner, Marianne Sloss, William J. Romanow, Yoshitaka Satoh, Jayashree Tikhe, Won Hyung Yoon, Mercedes Delgado
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Publication number: 20130023532Abstract: Disclosed are compounds having the formula: or a salt thereof, wherein A, n, R1, R1A, and R2 are as defined herein, and methods of making and using the same.Type: ApplicationFiled: March 26, 2011Publication date: January 24, 2013Inventors: Linda N. Casillas, Subhas J. Chakravorty, Adam Kenneth Charnley, Pamela A. Haile, Terry Vincent Hughes, Jae U. Jeong, Jianxing Kang, Ami Lakdawala Shah, Lara Kathryn Leister, Robert W. Marquis, JR., Nathan Andrew Miller, Daniel J. Price, Clark A. Sehon, Gren Z. Wang, Daohua Zhang, Patrick Eidam
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Publication number: 20130018031Abstract: Aminoalkylpyrimidine derivatives of formula I, wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.Type: ApplicationFiled: December 22, 2010Publication date: January 17, 2013Applicant: MEDICIS PHARMACEUTICAL CORPORATIONInventors: Elena Carceller Gonzalez, Marina Virgili Bernado, Robert Soliva Soliva, Carles Ferrer Costa
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Patent number: 8354407Abstract: The present invention relates to 2-arylamino-4-(heterocyclic)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-(heterocyclic)amino-pyrimidines and to methods for controlling, abating, or otherwise slowing the progression of heart failure.Type: GrantFiled: May 14, 2009Date of Patent: January 15, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Jane Far-Jine Djung, Adam Golebiowski, Jack A. Hunter, Gary P. Schrum
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Publication number: 20130005964Abstract: 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: July 24, 2012Publication date: January 3, 2013Inventors: 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
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Patent number: 8344160Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R4, R5, R3, R3a, W, D, R2a, R2b and R2c are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression, anxiety or intestinal inflammation, by administration of a therapeutically effective dose of a compound according to Formula I.Type: GrantFiled: October 8, 2009Date of Patent: January 1, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Guohua Zhao, William N. Washburn, James J. Mignone
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Publication number: 20120329771Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R5 to R10, A, L1, B, m and p are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.Type: ApplicationFiled: December 19, 2011Publication date: December 27, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias TREU, Stephan Karl ZAHN, Patricia AMOUZEGH, Cristina LECCI, Heather TYE
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Patent number: 8338439Abstract: The present invention provides 2,4-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same. In some embodiments, the present invention provides a compound of formula I-a or I-b: wherein each of Ring A, Ring B, W1, W2, Ry, Rv, Rx, m, p, and R1 is described herein.Type: GrantFiled: December 29, 2009Date of Patent: December 25, 2012Assignee: Celgene Avilomics Research, Inc.Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
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Patent number: 8334296Abstract: 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: November 18, 2008Date of Patent: December 18, 2012Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald G 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: 8329717Abstract: Compounds of the formula (I) and their agrochemically compatible salts and their use in the field of crop protection are described.Type: GrantFiled: December 23, 2009Date of Patent: December 11, 2012Assignee: Bayer Cropscience AGInventors: Klemens Minn, Hansjörg Dietrich, Jan Dittgen, Dieter Feucht, Isolde Häuser-Hahn, Christopher Hugh Rosinger
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Patent number: 8318736Abstract: HIV replication inhibitors of formula wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and X have specific definitions, and pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.Type: GrantFiled: December 28, 2007Date of Patent: November 27, 2012Assignee: Janssen R&D IrelandInventors: Jerôme Emile Georges Guillemont, Céline Isabelle Mordant, Benoit Antoine Schmitt
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Publication number: 20120295911Abstract: The present invention includes compositions that are useful in the treatment of breathing control diseases or disorders in a subject in need thereof. The present invention also includes a method of treating a respiratory disease or disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention. The present invention further includes a method of preventing destabilization or stabilizing breathing rhythm in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention.Type: ApplicationFiled: May 29, 2012Publication date: November 22, 2012Inventors: James C. Mannion, Scott L. Dax, Duncan Euan MacIntyre, Francis John Golder, James Francis McLeod
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Publication number: 20120283261Abstract: In one aspect, the invention relates to substituted N-phenylpyrimidin-2-amine analogs, derivatives thereof, and related compounds, which are useful as inhibitors of Axl kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions for treating disorders associated with dysfunction of the Axl kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: March 31, 2012Publication date: November 8, 2012Inventors: David J. Bearss, Hariprasad Vankayalapati, Alexis Mollard, Steven L. Warner, Sunil Sharma
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Publication number: 20120270237Abstract: The present invention relates to immobilization compounds (I), immobilization products and preparations thereof as well as methods and uses for the identification of kinase interacting compounds or for the purification or identification of kinase proteins.Type: ApplicationFiled: March 31, 2010Publication date: October 25, 2012Applicant: Cellzone AGInventors: Nigel Ramsden, Jeremy Major, John Harrison, Daniel Leggate, Paola Grandi
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Patent number: 8293729Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.Type: GrantFiled: June 23, 2010Date of Patent: October 23, 2012Assignees: Boehringer Ingelheim International GmbH, Neurocrine Biosciences Inc.Inventors: Brian Dyck, Joe A. Tran, Junko Tamiya, Florence Jovic, Troy Vickers, Chen Chen, Nicole Harriott, Timothy Coon, Neil J. Ashweek
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Patent number: 8283356Abstract: Disclosed are pyrimidine derivatives of formula wherein R0, R1, R3 to R9, and Z have a signification as indicated in claim 1, which have interesting pharmaceutical properties.Type: GrantFiled: January 13, 2010Date of Patent: October 9, 2012Assignee: Novartis AGInventors: Rolf Baenteli, Marie Claude Bernhard, Peter Buehlmayer, Nigel Graham Cooke, Rudolf Duthaler, Klaus Hinterding, Gebhard Thoma, Maurice Van Eis, Anette Von Matt, Louis Walliser, Gerhard Zenke
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Publication number: 20120253039Abstract: 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 lupus erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: ApplicationFiled: April 9, 2012Publication date: October 4, 2012Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
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Patent number: 8277599Abstract: 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: GrantFiled: June 12, 2006Date of Patent: October 2, 2012Assignee: Commissariat a L'Energie AtomiqueInventors: Renaud Demadrille, Stéphane Guillerez
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Patent number: 8269009Abstract: The application relates to a method of using compositions having anti-alpha-4 integrin and/or anti-alpha-9 integrin activity to inhibit liquid tumor growth, malignancies thereof and/or development of metastases thereof that involve expression of an alpha-4 integrin and/or alpha-9 integrin. Pharmaceutical compositions and combination therapies (for example, with chemotherapies) for the inhibition of liquid tumor growth, malignancies thereof and/or development of metastases thereof are also provided.Type: GrantFiled: December 5, 2008Date of Patent: September 18, 2012Assignee: Elan Pharmaceuticals, Inc.Inventors: Elizabeth Messersmith, Ivan Lieberburg
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Patent number: 8268851Abstract: 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: GrantFiled: December 22, 2009Date of Patent: September 18, 2012Assignee: Rigel Pharmaceuticals, Inc.Inventors: Somasekhar Bhamidipati, Hui Li, Rajinder Singh, Vanessa Taylor, Jeffrey Clough, Darren McMurtrie
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Patent number: 8263590Abstract: Novel pyrimidine derivatives of formula I to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: April 27, 2011Date of Patent: September 11, 2012Inventors: Carlos Garcia-Echeverria, Takanori Kanazawa, Eiji Kawahara, Keiichi Masuya, Naoko Matsuura, Takahiro Miyake, Osamu Ohmori, Ichiro Umemura
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Patent number: 8258129Abstract: The present invention encompasses compounds of general formula (1) wherein X and R1 to R3 are as defined in the disclosure, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: GrantFiled: July 5, 2007Date of Patent: September 4, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Harald Engelhardt, Gerd Bader, Guido Boehmelt, Ralph Brueckner, Thomas Gerstberger, Maria Impagnatiello, Daniel Kuhn, Otmar Schaaf, Heinz Stadtmueller, Irene Waizenegger, Andreas Zoephel
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Patent number: 8252803Abstract: Compounds of formula I: I selectively inhibit production of Ab(1-42) and hence find use in treatment of Alzheimer's disease and other conditions associated with deposition of A(b) in the brain.Type: GrantFiled: February 8, 2008Date of Patent: August 28, 2012Assignee: Merck Sharp & Dohme Corp.Inventor: Alexey A. Rivkin
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Publication number: 20120213795Abstract: 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 are therapeutically useful.Type: ApplicationFiled: May 3, 2012Publication date: August 23, 2012Inventors: Hui Li, Ankush Argade, Sambaiah Thota, David Carroll, Arvinder Sran, Robin Cooper, Rajinder Singh, Kin Tso, Somasekhar Bhamidipati
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Patent number: 8247411Abstract: 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: GrantFiled: March 11, 2011Date of Patent: August 21, 2012Assignee: Pfizer IncInventors: 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
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Publication number: 20120202814Abstract: The present invention relates to the medical use of the compound of formula 1, 2, 3 or 4:Type: ApplicationFiled: October 4, 2010Publication date: August 9, 2012Applicants: UNIVERSITÀ DEGLI STUDI DI SIENA, CONSIGLIO NAZIONALE DELLE RICERCHEInventors: Marco Radi, Maurizio Botta, Federico Falchi, Giovanni Maga, Fausto Baldanti, Stefania Paolucci
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Patent number: 8232428Abstract: Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis.Type: GrantFiled: March 10, 2010Date of Patent: July 31, 2012Assignee: PolyMedix,Inc.Inventors: Shaker Mousa, Dahui Liu
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Publication number: 20120172385Abstract: The invention relates to compounds of formula (I) wherein X1 to X3, R, R2 to R7 and AA have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.Type: ApplicationFiled: September 7, 2010Publication date: July 5, 2012Inventors: Richard John Harrison, Andrew Hobson, Nigel Ramsden
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Publication number: 20120172596Abstract: The present invention relates to a method of making pyrimidines of formula (III) said method comprising reacting a compound of formula (I) with an oxygen, sulfur or nitrogen nucleophile of formula T-H; and reacting the compound obtained with an amine of formula (II) [HN(R1)R2] to form a compound of formula (III) wherein X1, X2, T, R1 and R2 have the meanings as defined herein.Type: ApplicationFiled: August 13, 2010Publication date: July 5, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Guenter Linz, Gerd Kraemer