Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, wherein G1, R2, R3, R4, R5, n, p, q, Ar1, and Ar2 are defined in the description. The present invention relates also to methods of making said compounds, and compositions comprising said compounds which are useful for inhibiting kinases such as IGF-1R.
Type:
Grant
Filed:
May 26, 2010
Date of Patent:
January 15, 2013
Assignee:
Abbott Laboratories Inc.
Inventors:
Richard F. Clark, Randy L. Bell, Nwe Y. Ba-maung, Scott A. Erickson, Steve D. Fidanze, Robert A. Mantei, George S. Sheppard, Bryan K. Sorensen, Gary T. Wang, Jieyi Wang
Abstract: The invention relates to the 6-cycloamino-3-(pyridin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I): Wherein R2, R3, R7, R8, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.
Type:
Grant
Filed:
December 24, 2009
Date of Patent:
January 15, 2013
Assignee:
Sanofi
Inventors:
Antonio Almario Garcia, Matthieu Barrague, Philippe Burnier, Cécile Enguehard, Zhongli Gao, Pascal George, Alain Gueiffier, Adrien Tak Li, Frédéric Puech, Roy Vaz, Qiuxia Zhao
Abstract: The present invention relates to tetraaza phenalen-3-one compounds which inhibit poly (ADP-ribose) polymerase (PARP) and are useful in the chemosensitization of cancer therapeutics. The induction of peripheral neuropathy is a common side-effect of many of the conventional and newer chemotherapies. The present invention further provides means to reliably prevent or cure chemotherapy-induced neuropathy. The invention also relates to the use of the disclosed PARP inhibitor compounds in enhancing the efficacy of chemotherapeutic agents such as temozolomide. The invention also relates to the use of the disclosed PARP inhibitor compounds to radio sensitize tumor cells to ionizing radiation. The invention also relates to the use of the disclosed PARP inhibitor compounds for treatment of cancers with DNA repair defects.
Type:
Application
Filed:
June 19, 2012
Publication date:
January 10, 2013
Applicant:
EISAI INC.
Inventors:
Weizheng XU, Greg Delahanty, Ling Wei, Jie Zhang
Abstract: The invention relates to compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, which are soluble guanylate cyclase activators. The compounds are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.
Type:
Application
Filed:
March 22, 2011
Publication date:
January 10, 2013
Inventors:
Darby Schmidt, Subharekha Raghavan, John Stelmach, Jian Guo, Jonathan Groeper, Linda Brockunier, Keith Rosauer, Hong Shen, Rui Liang, Fa-Xiang Ding
Abstract: The invention relates to the 6-cycloamino-3-(pyridin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I): Wherein R2, R3, R7, R8, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.
Type:
Application
Filed:
September 14, 2012
Publication date:
January 10, 2013
Applicant:
SANOFI
Inventors:
Antonio ALMARIO GARCIA, Matthieu BARRAGUE, Philippe BURNIER, Cécile ENGUEHARD, Zhongli GAO, Pascal GEORGE, Alain GUEIFFIER, Adrien Tak LI, Frédéric PUACH, Roy VAZ, Qiuxia ZHAO
Abstract: The present invention relates to novel phthalazine derivatives and, more particularly, to phthalazine derivatives that are useful as protein kinase inhibitors. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and methods of treatment using the compounds.
Type:
Grant
Filed:
June 1, 2011
Date of Patent:
January 8, 2013
Inventors:
Gian-Luca Araldi, Matthew Ronsheim, Melanie Ronsheim
Abstract: The invention relates to a controlled release composition comprising a combination of isosorbide dinitrate and hydralazine, such as hydralazine hydrochloride, that in operation delivers the drug in a pulsed or multi-modal manner for the treatment of angina, ischaemic heart disease, arterial hypertension and related disease conditions. Preferably, the isosorbide dinitrate and hydralazine hydrochloride can be released from the dosage form in an erodable, diffusion and/or osmotic-controlled release profile.
Type:
Application
Filed:
September 7, 2012
Publication date:
January 3, 2013
Applicant:
Alkermes Pharma Ireland Limited
Inventors:
Gurvinder Singh Rekhi, Richard Sidwell, Sharon Hamm
Abstract: Phenoxymethyl compounds that inhibit at least one phosphodiesterase 10 are described as are pharmaceutical compositions containing such compounds an methods for treating various CNS disorders by administering such compounds to a patient in need thereof.
Type:
Grant
Filed:
December 18, 2009
Date of Patent:
January 1, 2013
Assignee:
EnVivo Pharmaceuticals, Inc.
Inventors:
Amy Ripka, Gideon Shapiro, Richard Chesworth
Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
Type:
Application
Filed:
June 21, 2012
Publication date:
December 27, 2012
Inventors:
James E. Hunter, William C. Lo, Gerald B. Watson, Akshay Patny, Gary D. Gustafson, Dan Pernich, William K. Brewster, Debra L. Camper, Beth Lorsbach, Michael R. Loso, Thomas C. Sparks, Hemant Joshi, Adiraj Mandaleswaran, Ramadevi Sanam, Rambabu Gundla, Pravin S. Iyer
Abstract: The invention relates to the provision of two novel crystalline forms I and II for 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt. Surprisingly, it was discovered that form I and form II have differing immunological effects. This advantageous property is useful for immunospecific applications. In addition, both forms have advantageous physicochemical properties, which are useful in the production, further processing and/or use of a pharmaceutical preparation of form I or form II or a mixture of both.
Type:
Application
Filed:
March 1, 2011
Publication date:
December 27, 2012
Applicant:
Metriopharm AG
Inventors:
Josef Breu, Wolfgang Brysch, Astrid Kaiser, Beate Ludescher, Gerrit Maass, Thomas Martin, Wolfgang Milius, Michael Niedermaier
Abstract: The present invention is directed to tertiary carbinamine compounds having substituted heterocycles, which are inhibitors of the beta-secretase enzyme, and are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
Type:
Grant
Filed:
January 13, 2006
Date of Patent:
December 25, 2012
Assignee:
Merck, Sharp & Dohme Corp.
Inventors:
Georgia B. McGaughey, Philippe G. Nantermet, Hemaka A. Rajapakse, Shaun R. Stauffer
Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
Type:
Grant
Filed:
May 13, 2011
Date of Patent:
December 25, 2012
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Guy W. Bemis, Francesco G. Salituro, John P. Duffy, John E. Cochran, Edmund M. Harrington, Mark A. Murcko, Keith P. Wilson, Michael Su, Vincent P. Galullo
Abstract: The use of a compound of formula I wherein Y is a single bond, C?O, C?S or S(O)m, where m is 0, 1 or 2; the ring is a 6-membered aromatic or is a 5 or 6 membered heteroaromatic ring; Z and Z? are joined by a single or a double bond and are ?C— or —N— provided that both are not N; Ra, R1, R2, R3, R3a, R4 and R8 are specified organic groups; n is 2, 3 or 4 and p is 0-4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.
Type:
Grant
Filed:
December 6, 2006
Date of Patent:
December 25, 2012
Assignee:
Syngenta Crop Protection LLC
Inventors:
Jérôme Cassayre, Peter Maienfisch, Fredrik Cederbaum, Louis-Pierre Molleyres
Abstract: Disclosed herein is a method for predicting the prognosis, the likelihood of metastasis in, or the desirability of administering an aggressive therapy to, a subject with colorectal cancer, comprising determining, in a sample from the subject, the level of phosphorylation of one or more of certain proteins compared to a positive and/or negative reference standard; or the total amount of COX-2 protein compared to a positive and/or negative reference standard. Also described are methods for treating subjects likely to develop metastatic colorectal carcinoma, and pharmaceutical compositions and kits for implementing the methods of the invention.
Type:
Application
Filed:
May 25, 2012
Publication date:
December 20, 2012
Inventors:
Emanuel Petricoin, III, Lance A. Liotta, Mariaelena Pierobon, Valerie Calvert
Abstract: The present invention relates to compounds of formula I, wherein the groups R1, LP, LQ, X1, X2, X3, Ar and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
Type:
Application
Filed:
December 16, 2011
Publication date:
December 20, 2012
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Frank HIMMELSBACH, Matthias ECKHARDT, Niklas HEINE, Elke LANGKOPF, Bernd NOSSE
Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.
Abstract: The invention features methods, kits, and pharmaceutical compositions for treating cancer using 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)-methyl)-3-(trifluoromethyl)phenyl)benzamide.
Type:
Application
Filed:
November 1, 2010
Publication date:
December 13, 2012
Applicant:
ARIAD Pharmaceuticals, Inc.
Inventors:
Wei-Sheng Huang, Victor M. Rivera, Timothy P. Clackson, William C. Shakespeare, Rachel M. Squillace, Joseph M. Gozgit
Abstract: The present invention is related to pyrazolo piperidine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
Type:
Application
Filed:
February 17, 2011
Publication date:
December 13, 2012
Applicant:
GENKYOTEX SA
Inventors:
Patrick Page, Benoît Laleu, Francesca Gaggini, Mike Orchard
Abstract: The invention relates to annelated pyrrolidin sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula (I), in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.
Type:
Grant
Filed:
May 22, 2009
Date of Patent:
December 11, 2012
Assignee:
Sanofi
Inventors:
Stefanie Keil, Matthias Urmann, Wolfgang Wendler, Ulrike Wendler, Maike Glien, Hans Matter, Eugen Falk
Abstract: The present invention provides compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.
Type:
Application
Filed:
February 1, 2012
Publication date:
December 6, 2012
Applicant:
EISAI INC.
Inventors:
Vincent J. Kalish, Jie Zhang, Weizheng Xu, Jia-He Li, Amy Dongxia Xing, Qun Liu
Abstract: Provided herein are Compounds that induce interferon production and methods for identifying such Compounds. Also provided herein are compositions comprising such Compounds and methods of using such Compounds to treat interferon-sensitive diseases such as viral infections, cancer, and multiple sclerosis.
Type:
Application
Filed:
January 31, 2011
Publication date:
December 6, 2012
Inventors:
Megan Shaw, Mila Ortigoza, Adolfo Garcia-Sastre, Peter Palese
Abstract: Disclosed are triazolopyridine compounds of Formula (I), including pharmaceutically acceptable salts thereof. Also, disclosed are methods of using the compound in the treatment of obesity, dyslipidemia, diabetes and atherosclerosis, and to pharmaceutical compositions comprising at least one compound of Formula (I) or a stereoisomer or pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 7, 2009
Date of Patent:
December 4, 2012
Assignee:
Bristol-Myers Squibb Company
Inventors:
Yanting Huang, Chongqing Sun, R. Michael Lawrence, William R. Ewing, Huji Turdi
Abstract: The present invention provides compositions and methods of use thereof to prevent and/or treat pathogenic infection. In particular, the present invention provides the use of kinase inhibitors to inhibit kinases that involve in pathogen-host cell interactions that are associated with or cause pathogenic infections, therefore, to effectively prevent and/or treat pathogenic infections with far less likely to engender resistance as compared to conventional antibiotics and anti-viral drugs. The present invention further provides the use of kinase inhibitors for the treatment of acute pathogenic infections for a short period of time to avoid toxicities that may caused by long term use of these kinase inhibitors.
Type:
Application
Filed:
August 3, 2012
Publication date:
November 29, 2012
Applicants:
M.D. ANDERSON CANCER CENTER, EMORY UNIVERSITY
Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HW).
Type:
Application
Filed:
January 25, 2012
Publication date:
November 29, 2012
Inventors:
Gary BRIDGER, Al KALLER, Curtis HARWIG, Renato SKERLJ, David BOGUCKI, Trevor R. WILSON, Jason CRAWFORD, Ernest J. MCEACHERN, Bem ATSMA, Siqiao NAN, Yuanxi ZHOU, Dominique SCHOLS, Christopher D. SMITH, Maria R. DI FLURI
Abstract: Novel compound having the following formula: Also disclosed are a pharmaceutical compositions comprising the same, methods for treating cancer using the same, and methods for the synthesis of the same. The novel compounds of the present invention are found to inhibit protein kinases, especially Checkpoint kinase Chk1/Chk2.
Abstract: The present invention relates in general to therapeutic compositions and methods of use. In preferred embodiments, the invention relates to the field of eye health. In some embodiments, the invention relates to the prevention and treatment of macular degeneration by administering compounds disclosed herein. In some embodiments, the invention relates to compositions and methods of improving vision.
Abstract: The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.
Type:
Application
Filed:
August 1, 2012
Publication date:
November 22, 2012
Applicant:
INCYTE CORPORATION
Inventors:
Chu-Biao Xue, Ganfeng Cao, Taisheng Huang, Lihua Chen, Ke Zhang, Anlai Wang, David Meloni, Rajan Anand, Joseph Glenn, Brian W. Metcalf
Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth.
Type:
Application
Filed:
February 23, 2012
Publication date:
November 22, 2012
Applicant:
Intellikine LLC
Inventors:
Pingda Ren, Yi Liu, Katayoun Jessen, Xin Guo, Christian Rommel, Troy Edward Wilson
Abstract: This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
Type:
Application
Filed:
May 16, 2012
Publication date:
November 22, 2012
Inventors:
Roland Joseph Billedeau, Rama K. Kondru, Francisco Javier Lopez-Tapia, Yan Lou, Timothy D. Owens, Yimin Qian, Sung-Sau So, Kshitij C. Thakkar, Jutta Wanner
Abstract: The present invention provides compositions for reducing amyloid plaque burden associated with Alzheimer's disease and methods of using the same.
Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
Type:
Application
Filed:
May 8, 2012
Publication date:
November 15, 2012
Inventors:
Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Gregory Notte, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
Abstract: Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.
Type:
Application
Filed:
July 6, 2012
Publication date:
November 15, 2012
Applicant:
NEOPHARM CO., LTD.
Inventors:
Tae-Seong KIM, Eunkyung LEE, Doyoung KIM, Bu-mahn PARK, Jiyeon PARK, JungJe JOO
Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring G1, R1, and R2 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
Type:
Application
Filed:
May 8, 2012
Publication date:
November 15, 2012
Applicant:
ABBOTT LABORATORIES
Inventors:
Brian S. Brown, Tongmei Li, Sridhar Peddi, Arturo Perez-Medrano, David DeGoey
Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
Type:
Grant
Filed:
May 23, 2012
Date of Patent:
November 13, 2012
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Jesus E. Gonzalez, III, Andreas P. Termin, Esther Martinborough, Nicole Hilgraf
Abstract: Compounds of formula (I) are inhibitors of CD80 and useful in immunomodulation therapy: wherein R1 and R3 independently represent H; F; Cl; Br; —NO2; —CN; C1-C6 alkyl optionally substituted by F or Cl; or C1-C6 alkoxy optionally substituted by F; R4 represents a carboxylic acid group (—COOH) or an ester thereof, or —C(?O)NR6R7, —NR7C(?O)R6, —NR7C(?O)OR6, —NHC(?O)NR7R6 or —NHC(?S)NR7R6 wherein R6 represents H, or a radical of formula -(Alk)m-Q wherein m is 0 or 1, Alk is an optionally substituted divalent straight or branched C1-C12 alkylene, or C2-C12 alkenylene, or C2-C12 alkynylene radical or a divalent C3-C12 carbocyclic radical, any of which radicals may contain one or more —O—, —S— or —N(R8)— links wherein R8 represents H or C1-C4 alkyl, C3-C4 alkenyl, C3-C4 alkynyl, or C3-C6 cycloalkyl, and Q represents H; —NR9R10 wherein R9 and R10 independently represents H; C1-C4 alkyl; C3-C4 alkenyl; C3-C4 alkynyl; C3-C6 cycloalkyl; an ester group; an optionally substituted carbocyclic or heterocyclic group; or
Abstract: The present application relates to novel azabicyclic compounds, processes for their preparation, their use alone or in combinations for the treatment and/or prevention of diseases, and their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
Type:
Grant
Filed:
September 1, 2007
Date of Patent:
November 13, 2012
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Hartmut Schirok, Joachim Mittendorf, Johannes-Peter Stasch, Frank Wunder, Friederike Stoll, Karl-Heinz Schlemmer
Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.
Type:
Application
Filed:
July 19, 2012
Publication date:
November 8, 2012
Inventors:
Brian E. Fink, Libing Chen, Ashvinikumar V. Gavai, Liqi He, Soong-Hoon Kim, Andrew James Nation, Yufen Zhao, Litai H. Zhang
Abstract: Compounds having inverse agonist functional selectivity for GABAA receptors containing the ?5 subunit for use as a medicament in the treatment of cognitive impairments in subjects suffering from Down syndrome. The use of these compounds is disclosed. Pharmaceutical compositions for such treatment can comprise these compounds or suitable pharmaceutically acceptable salt thereof, a polyethoxylated castor oil and dimethyl sulfoxide (DMSO). Methods are disclosed for enhancing cognitive function, or treating or lessening the severity of cognitive impairments, in subjects suffering from Down syndrome by administering to a subject in need thereof a pharmaceutically effective amount of one or more of these compounds.
Type:
Application
Filed:
August 24, 2010
Publication date:
November 8, 2012
Applicant:
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE - CNRS
Abstract: The present invention generally relates to the modulation of hypoxia-inducible factor (HIF) using the compounds and methods disclosed herein. These compounds and methods can be applied to the prevention, pretreatment, and/or treatment of conditions or states associated with HIF, such as hypoxia- and ischemia-related conditions and the induction of stasis.
Abstract: The present invention relates to novel compounds of formula I wherein W, n, X and W? are defined in the description; invention compounds are modulators of metabotropic glutamate receptors—subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
Type:
Application
Filed:
December 20, 2011
Publication date:
November 1, 2012
Applicant:
Addex Pharma SA
Inventors:
Anne-Sophie Bessis, Christelle Bolea, Beatrice Bonnet, Mark Epping-Jordan, Nicolas Poirier, Sonia-Maria Poli, Jean-Philippe Rocher, Yves Thollon
Abstract: Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.
Type:
Application
Filed:
July 6, 2012
Publication date:
November 1, 2012
Applicant:
Pharmacyclics, Inc.
Inventors:
Lee Honigberg, Erik J. Verner, Joseph J. Buggy, David J. Loury, Wei Chen
Abstract: This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formula I-III: wherein, variables Q, R, X, X?, Y1, Y2, Y2?, Y3, Y4, Y5, m, and n are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I-III and at least one carrier, diluent or excipient.
Type:
Grant
Filed:
February 24, 2010
Date of Patent:
October 30, 2012
Assignee:
Roche Palo Alto LLC
Inventors:
Steven Berthel, Fariborz Firooznia, Daniel Fishlock, Jun-Bae Hong, Yan Lou, Matthew Lucas, Timothy D. Owens, Keshab Sarma, Zachary Kevin Sweeney, Joshua Paul Gergely Taygerly
Abstract: Disclosed are crystalline forms of 2-(2-fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
Type:
Grant
Filed:
May 17, 2006
Date of Patent:
October 30, 2012
Assignees:
Array Biopharma Inc., Astrazeneca AB
Inventors:
Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, Jim Blake, Richard Anthony Storey, Rebecca Jane Booth, John David Pittam, John Leonard, Mark Richard Fielding
Abstract: Disclosed are CCR1 receptor antagonists of the formula (I) wherein Ar1, Ar2, R1-R3, X and L are disclosed herein. Also disclosed are compositions, methods of making and using compounds of the formula (I).
Type:
Application
Filed:
October 21, 2010
Publication date:
October 25, 2012
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Abstract: The present invention relates to ophthalmic depot formulations comprising an active agent, e.g. embedded in a pharmacologically acceptable biocompatible polymer or a lipid encapsulating agent, e.g. for periocular or subconjunctival administration.
Type:
Application
Filed:
June 14, 2012
Publication date:
October 25, 2012
Inventors:
Marklus AHLHEIM, Michael AUSBORN, David BODMER, Christian SCHOCH
Abstract: The present invention is directed to heterocyclic fused cinnoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.