Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/117)
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Patent number: 8846656Abstract: The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: July 19, 2012Date of Patent: September 30, 2014Assignee: Novartis AGInventors: Christopher Michael Adams, Veronique Darsigny, Alec Nathanson Flyer, Christine Fang Gelin, Timothy Brian Hurley, Nan Ji, Rajeshri Ganesh Karki, Toshio Kawanami, Erik Meredith, Chang Rao, Michael H. Serrano-Wu, Catherine Fooks Solovay
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Patent number: 8846670Abstract: The invention relates to compounds of the formula: or their racemic, enantiomeric or diastereoisomeric isomers, or pharmaceutically acceptable salts of the compounds of formula I or the racemic, enantiomeric or diasteroisomeric isomers.Type: GrantFiled: July 1, 2010Date of Patent: September 30, 2014Assignee: SanofiInventors: Eric Bacque, Maurice Brollo, Annie Clauss, Youssef El Ahmad, Bruno Filoche-Romme, Frank Halley, Karl Andreas Karlsson, Gilbert Marciniak, Baptiste Ronan, Laurent Schio, Bertrand Vivet, Fabrice Viviani, Andre Zimmermann
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Publication number: 20140288069Abstract: The present invention relates to amino imidazopyridazine compounds of general formula (I): in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said 10 compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: May 14, 2012Publication date: September 25, 2014Applicant: Bayer Intellectual Property GmbHInventors: Knut Eis, Florian Pühler, Ludwig Zorn, Arne Scholz, Philip Lienau, Mark Jean Gnoth, Ulf Bömer, Judith Günther, Jörg Fanghänel, Daniel Korr
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Publication number: 20140288070Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of B-Raf V600E mutant protein kinase, including melanoma, glioma, glioblastoma multiforme, pilocytic astrocytoma, colorectal cancer, thyroid cancer, lung cancer, ovarian cancer, prostate cancer, liver cancer, gallbladder cancer, gastrointestinal stromal tumors, biliary tract cancer, and cholangiocarcinoma.Type: ApplicationFiled: March 17, 2014Publication date: September 25, 2014Inventors: Prabha N. Ibrahim, Wayne Spevak, Hanna Cho, Songyuan Shi, Chao Zhang, Ying Zhang
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Publication number: 20140288066Abstract: The invention relates to compounds of formula (I) wherein m, o, Ra, Rb, R1 and T1 have the meaning as cited in the description and the claims. The compounds are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including the compounds, the preparation of the compounds as well as their use as medicaments.Type: ApplicationFiled: October 5, 2012Publication date: September 25, 2014Inventors: Rosemary Lynch, Andrew David Cansfield, Daniel Paul Hardy, John Thomas Feutrill, Rita Adrego, Katie Ellard, Tammy Ladduwahetty
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Publication number: 20140288053Abstract: The invention relates to new pyridopyrazine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: October 26, 2012Publication date: September 25, 2014Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio Berdini, Gordon Saxty, Patrick Rene Angibaud, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet, Bruno Roux, Lieven Meerpoel
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Publication number: 20140288052Abstract: Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: October 19, 2012Publication date: September 25, 2014Inventors: Charles A. Blum, Jeremy S. Disch, Stephanie K. Springer
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Publication number: 20140288071Abstract: Compounds are disclosed for the treatment, management and prevention of diseases and disorders affecting the bone. Particular compounds are potent inhibitors of Notum Pectinacetylesterase, and are of the formula: wherein E, G, Y, Z, R1, R2, and R3 are defined herein.Type: ApplicationFiled: June 10, 2014Publication date: September 25, 2014Inventors: Joseph BARBOSA, Kenneth Gordon CARSON, Michael Walter GARDYAN, Wei HE, Victoria LOMBARDO, Praveen PABBA, James TARVER, JR.
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Publication number: 20140275009Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.Type: ApplicationFiled: December 6, 2013Publication date: September 18, 2014Inventors: Guy Brenchley, Jean-Damien Charrier, Chris Davis, Steven Durrant, Gorka Etxebarria I Jardi, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Francoise Pierard, Joanne Pinder, David Shaw, Pierre-Henri Storck, John Studley, Heather Twin
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Publication number: 20140275070Abstract: The present invention relates generally to thienopyrimidine and thienopyridine class compounds and methods of use thereof. In particular embodiments, the present invention provides compositions comprising thienopyrimidine class compounds and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins (e.g., for the treatment of leukemia, solid cancers and other diseases dependent on activity of MLL1 and MLL2 or menin).Type: ApplicationFiled: March 10, 2014Publication date: September 18, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Jolanta Grembecka, Tomasz Cierpicki, Dmitry Borkin, Jay L. Hess, Duxin Sun, Xiaoqin Li
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Publication number: 20140275021Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables R1, R2, R3, and R4 are as defined herein.Type: ApplicationFiled: December 6, 2013Publication date: September 18, 2014Inventors: Jean-Damien Charrier, Chris Davis, Steven Durrant, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Michael O'Donnell, Francoise Pierard, Joanne Pinder, Pierre-Henri Storck, Heather Twin
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Publication number: 20140275069Abstract: The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: In formula I the variables X1 is CH or N, X2 is O or S and where R1, R2, R3, R4 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: ApplicationFiled: February 25, 2014Publication date: September 18, 2014Inventors: Katja JANTOS, Michael OCHSE, Hervé GENESTE, Jayne FROGGETT, Clarissa JAKOB, Karla DRESCHER, Jürgen DINGES
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Patent number: 8828997Abstract: The invention relates to a product of formula (I) where R1, R2, R3, and R4 are as defined herein, the therapeutic use of the product, a process to make the product, and a pharmaceutical composition comprising the product.Type: GrantFiled: July 1, 2010Date of Patent: September 9, 2014Assignee: SanofiInventors: Maurice Brollo, Annie Clauss, Youssef El Ahmad, Bruno Filoche-Romme, Frank Halley, Karl Andreas Karlsson, Gilbert Marciniak, Baptiste Ronan, Laurent Schio, Bertrand Vivet, Fabrice Viviani, Andre Zimmermann
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Publication number: 20140249145Abstract: Substituted pyrazolopyrimidines and dihydropyrazolopyrimidines and related compounds, their methods of manufacture, compositions containing these compounds, and methods of use of these compounds in treating lysosomal storage disorders such as Gaucher disease are described herein. The compounds are of general Formula (I) in which variables R1-R7 and X are described in the application.Type: ApplicationFiled: December 8, 2011Publication date: September 4, 2014Applicant: THE UNITED STATES OF AMERICA, as represented by the Secretary, Department of Health and Human ServInventors: Juan Jose Marugan, Noel Southall, Ehud Goldin, Wei Zheng, Samarjit Patnaik, Ellen Sidransky, Omid Motabar, Wendy Westbroek
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Publication number: 20140249131Abstract: The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer.Type: ApplicationFiled: February 26, 2014Publication date: September 4, 2014Inventors: Andrew TASKER, Ryan WURZ, Liping H. PETTUS, Bradley J. HERBERICH
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Publication number: 20140249139Abstract: The invention relates to substituted quinazoline derivative of the formula (I), wherein A, X1, X2, X3, X4 and R5 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.Type: ApplicationFiled: October 19, 2012Publication date: September 4, 2014Applicant: NOVARTIS AGInventors: Pascal Furet, Christina Hebach, Klemens Hogenauer, Gregory Hollingworth, Ian Lewis, Alexander Baxter Smith, Nicolas Solvermann, Frederic Stauffer, Romain Wolf, Frederic Zecri
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Patent number: 8822684Abstract: The presently-disclosed subject matter relates to compounds of the formula: and methods for use thereof. The presently-disclosed subject matter relates methods of selectively differentiating a stem cell, and methods of screening for compounds useful for enhancing terminal differentiation of committed cardiac progenitor cells.Type: GrantFiled: August 6, 2009Date of Patent: September 2, 2014Assignee: Vanderbilt UniversityInventors: Charles C. Hong, Corey R. Hopkins, Antonis K. Hatzopoulos, Craig Lindsley, Jijun Hao
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Publication number: 20140243308Abstract: The present invention relates to substituted imidazopyridazines and substituted benzimidazoles, as well as pharmaceutical compositions comprising the same, which are FGFR3 inhibitors useful in the treatment of cancer and other diseases.Type: ApplicationFiled: May 1, 2014Publication date: August 28, 2014Applicant: Incyte CorporationInventors: Wenqing Yao, Colin Zhang, Meizhong Xu, Jincong Zhuo, Chunhong He
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Publication number: 20140243330Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.Type: ApplicationFiled: March 5, 2014Publication date: August 28, 2014Applicant: Curis, Inc.Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Changgeng Qian, Rudi Bao
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Publication number: 20140243315Abstract: The ectopic expression of Mer receptor tyrosine kinase (Mer) has been identified as a tumor cell survival gene product in Acute Lymphoblastic Leukemia (ALL) cells and a potential cause of ALL chemoresistance. Hence, we investigated whether the development of small molecule Mer inhibitors was possible. A first aspect of the present invention is a compound (sometimes referred to as an “active compound” herein) of Formula I, IA, or IB.Type: ApplicationFiled: October 1, 2012Publication date: August 28, 2014Applicant: The University of North Carolina at Chapel HillInventors: Xiaodong Wang, Jing Liu, Weihe Zhang, Stephen Frye, Dmitri Kireev
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Patent number: 8815853Abstract: The invention relates to novel products of formula (Ia) or (Ib): these products being in all the isomeric forms and salts as drugs, notably as anticancer drugs.Type: GrantFiled: December 22, 2011Date of Patent: August 26, 2014Assignee: SanofiInventors: Jerome Arigon, Maurice Brollo, Jacques Clement, Romain Combet, Florence Durand, Youssef El Ahmad, Jean-Robert Labrosse, Jean-Philippe Letallec, Baptiste Ronan
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Publication number: 20140235615Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.Type: ApplicationFiled: March 24, 2014Publication date: August 21, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Misaki HOMMA, Toru MIYAZAKI, Yuya OGURO, Osamu KURASAWA
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Publication number: 20140221333Abstract: Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.Type: ApplicationFiled: July 19, 2012Publication date: August 7, 2014Inventors: Adrianus Petrus Antonius De Man, Jan-Gerard Sterrenburg, Han C.A. Raaijmakers, Allard Kaptein, Arthura A. Oubrie, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Jacobus C.H.M. Wijkamans, Tjeerd A. Barf, Alan B. Cooper, Ronald M. Kim, Sobhana Babu Boga, Hugh Y. Zhu, Xiaolei Gao, Xin Yao, Rajan Anand, Hao Wu, Shilan Liu, Chundao Yang, Abdul-Basit Alhassan, James Wang, Younong Yu, Jian Liu, Henry M. Vaccaro
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Patent number: 8796259Abstract: N3-Heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: October 4, 2012Date of Patent: August 5, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Pingyu Ding, Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Joane Litvak
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Patent number: 8791108Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: GrantFiled: August 9, 2012Date of Patent: July 29, 2014Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Manoj Patel
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Patent number: 8791118Abstract: The invention provides new pyridopyrazine compounds according to formula (I) which are highly selective as Ras-Raf-Mek-Erk signal transduction pathway inhibitors and in particular are highly selective Erk inhibitors.Type: GrantFiled: April 4, 2012Date of Patent: July 29, 2014Assignee: Aeterna Zentaris GmbHInventors: Matthias Gerlach, Irene Seipelt, Lars Blumenstein, Gilbert Mueller, Eckhard Guenther, Tilmann Schuster, Michael Teifel
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Publication number: 20140200197Abstract: The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: September 9, 2013Publication date: July 17, 2014Inventors: JOHN A. MCCAULEY, CHRISTIAN BEAULIEU, DAVID J. BENNETT, CHRISTOPHER J. BUNGARD, RONALD K. CHANG, SHELDON CRANE, THOMAS J. GRESHOCK, LI HAO, KATE HOLLOWAY, JESSE J. MANIKOWSKI, DANIEL MCKAY, CARMELA MOLINARO, OSCAR MIGUEL MORADEI, PHILIPPE G. NANTERMET, CHRISTIAN NADEAU, TUMMANAPALLI SATYANARAYANA, WILLIAM SHIPE, SANJAY KUMAR SINGH, VOUY LINH TRUONG, SIVALENKA VIJAYARADHI, PETER D. WILLIAMS, CATHERINE M. WISCOUNT
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Publication number: 20140200207Abstract: Provided herein are Pyrrolopyrimidine Compounds having the following structure: wherein R1, R2, R3, and L are as defined herein, compositions comprising an effective amount of a Pyrrolopyrimidine Compound, and methods for treating or preventing breast cancer, more particularly triple negative breast cancer, comprising administering an effective amount of such Pyrrolopyrimidine Compounds to a subject in need thereof.Type: ApplicationFiled: January 15, 2014Publication date: July 17, 2014Applicant: Signal Pharmaceutical LLCInventors: Andrew Antony Calabrese, Brandon Jeffy, Dale Robinson, Dan Zhu, Dehua Huang, Jan Elsner, John Boylan, Lida Tehrani, Mark A. Nagy, Mehran Fallah Moghaddam, Raj Kumar Raheja, Paul Erdman, Rama K. Narla, Roy L. Harris, Tam Minh Tran, Jennifer Riggs, Yuhong Ning
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Publication number: 20140200206Abstract: Provided herein are Pyrrolopyrimidine Compounds having the following structure: wherein R1, R2, R3, and L are as defined herein, compositions comprising an effective amount of a Pyrrolopyrimidine Compound, and methods for treating or preventing breast cancer, more particularly triple negative breast cancer, comprising administering an effective amount of such Pyrrolopyrimidine Compounds to a subject in need thereof.Type: ApplicationFiled: January 15, 2014Publication date: July 17, 2014Applicant: Signal Pharmaceutical LLCInventors: Andrew Antony Calabrese, Brandon Jeffy, Dale Robinson, Dan Zhu, Dehua Huang, Jan Elsner, John Boylan, Lida Tehrani, Mark A. Nagy, Mehran Fallah Moghaddam, Raj Kumar Raheja, Paul Erdman, Rama K. Narla, Roy L. Harris, Tam Minh Tran, Jennifer Riggs, Yuhong Ning
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Patent number: 8778942Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: GrantFiled: March 13, 2013Date of Patent: July 15, 2014Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
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Patent number: 8778935Abstract: There is provided compounds of formula (I), wherein R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.Type: GrantFiled: April 16, 2010Date of Patent: July 15, 2014Assignee: Centro Nacional de Investigaciones Oncologicas (CNIO)Inventors: Joaquin Pastor Fernández, Sonia Martínez Gonzalez, Julen Oyarzabal Santamarina
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Publication number: 20140194418Abstract: Compounds of formula (I) or pharmaceutical acceptable salts are provided, wherein X1˜X5, R1˜R3, A, B, Z and n are defined in the description. And compositions containing said compounds, and the uses for inhibitors of kinases such as ALK, and the uses for treating cancer thereof are provided.Type: ApplicationFiled: January 20, 2012Publication date: July 10, 2014Applicant: ABBVIE INC.Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Fengchun Wu, Yan Shen, Cuihua Liu, Zhenguang Zou, Marina Pliushchev
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Publication number: 20140194404Abstract: This invention relates to amidopyrazole compounds that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment of cellular proliferative diseases, for example, cancer, hyperplasia, restenosis, cardiac hypertrophy, immune disorders and inflammation.Type: ApplicationFiled: March 21, 2012Publication date: July 10, 2014Inventors: William T. McElroy, Guoqing Li, Ginny Dai Ho, Zheng Tan, Sunil Paliwal, William Michael Seganish, Deen Tulshian, John Lampe, Joey L. Methot, Hua Zhou, Michael D. Altman, Liang Zhu
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Patent number: 8772279Abstract: There are provided 3,5-disubstituted derivatives of 6,7-dihydroimidazo[1,5-a]pyrazin-8(5H)-one compounds of formula (I) or a pharmaceutically acceptable salt thereof as defined in the present specification, which modulate the activity of protein kinases. The compounds are therefore useful in treating diseases caused by dysregulated protein kinase activity. In particular, such diseases to be treated with a compound of formula (I) of the present invention is one caused by and/or associated with disregulated protein kinase activity selected from the group consisting of cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders. The present invention also relates to processes for preparing the compounds of formula (I), combinatorial libraries thereof, pharmaceutical compositions comprising them, and methods of treating diseases utilizing pharmaceutical compositions comprising a compound of formula (I).Type: GrantFiled: January 21, 2011Date of Patent: July 8, 2014Assignee: Nerviano Medical Sciences S.R.L.Inventors: Danilo Mirizzi, Sten Christian Orrenius, Paolo Trifirò
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Patent number: 8772481Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatments of protein kinase mediated diseases, including inflammation and related conditions.Type: GrantFiled: October 7, 2009Date of Patent: July 8, 2014Assignee: Amgen Inc.Inventors: Andrew Tasker, Liping H. Pettus, Ryan Wurz
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Publication number: 20140187545Abstract: PI3K? selective compounds having the structureType: ApplicationFiled: June 29, 2012Publication date: July 3, 2014Applicant: GlaxoSmithKline LLCInventors: Hong Lin, Juan Luengo, Michael Lee Moore, Junya Qu, Ralph A. Rivero, Rosanna Tedesco, Hongyi Yu
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Publication number: 20140187548Abstract: The present invention relates to substituted imidazopyrazine compounds of general formula (I) in which R1, R2, R3, R4 and R5 are as defined in the claims, to methods of and intermediates for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: December 13, 2011Publication date: July 3, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Marcus Koppitz, Ulrich Klar, Rolf Jautelat, Dirk Kosemund, Rolf Bohlmann, Benjamin Bader, Philip Lienau, Gerhard Siemeister
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Patent number: 8765761Abstract: An imidazopyrazine having the structure or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: GrantFiled: April 23, 2013Date of Patent: July 1, 2014Assignee: Gilead Connecticut, Inc.Inventors: Scott A. Mitchell, Kevin S. Currie
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Patent number: 8754079Abstract: The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.Type: GrantFiled: February 25, 2011Date of Patent: June 17, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Thorsten Lehmann-Lintz, Armin Heckel, Joerg Kley, Elke Langkopf, Norbert Redemann, Achim Sauer, Leo Thomas, Dieter Wiedenmayer, Matthias Austen, John Danilewicz, Martin Schneider, Kay Schreiter, Phillip Black, Wesley Blackaby, Ian Linney
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Patent number: 8754080Abstract: The present invention relates to a purine compound useful as a kinase inhibitor. The compound has the structure (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 3, 2009Date of Patent: June 17, 2014Assignee: Verastem, Inc.Inventors: DiZhong Chen, Meredith Williams
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Publication number: 20140163000Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as defined herein. Moreover, The compounds of this invention have formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.Type: ApplicationFiled: December 6, 2013Publication date: June 12, 2014Inventors: Nadia Ahmad, Dean Boyall, Jean-Damien Charrier, Chris Davis, Rebecca Davis, Steven Durrant, Gorka Etxebarria I Jardi, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Donald Middleton, Michael O'Donnell, Maninder Panesar, Francoise Pierard, Joanne Pinder, David Shaw, Pierre-Henri Storck, John Studley, Heather Twin
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Publication number: 20140163023Abstract: The invention relates to compounds of formula (I) wherein X, R1, R2, T0, o have the meaning as cited in the description and the claims. The compounds of formula I are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including the compounds of formula I, the preparation of such compounds as well as the use as medicaments.Type: ApplicationFiled: April 2, 2012Publication date: June 12, 2014Applicant: Cellzome LimitedInventors: Rosemary Lynch, Andrew David Cansfield, Daniel Paul Hardy, Jane Elizabeth Scanlon, Rita Joana Rodrigues Adrego
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Publication number: 20140163026Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders or neurofibromatosis. Also described herein are methods of utilizing PAK inhibitors for the treatment of cancer.Type: ApplicationFiled: April 9, 2012Publication date: June 12, 2014Applicant: Afraxis Holdings, Inc.Inventors: David Campbell, Sergio G. Duron
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Publication number: 20140163007Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Publication number: 20140163226Abstract: The present invention relates to a compound represented by formula (I) for inhibiting the activity of diacylglycerol O-acyltransferase type 1 (DGAT1), and pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising same as an active ingredient. The compound of the present invention may be used effectively in the treatment or prevention of a disease or condition mediated by the activity of DGAT1 such as obesity, type II diabetes, dyslipidemia, metabolic syndrome, and the like, without any adverse effects: wherein A, B, X, and R5 to R7 are the same as defined in the specification.Type: ApplicationFiled: June 29, 2012Publication date: June 12, 2014Applicant: HANMI PHARMACEUTICAL CO., LTD.Inventors: Chul Hyun Park, Won Jeoung Kim, Young Hee Jung, Nam Du Kim, Young Kil Chang, Maeng Sup Kim
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Publication number: 20140163003Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Publication number: 20140163223Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Publication number: 20140163222Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Patent number: 8748607Abstract: Certain imidazopyrazines having the structure of formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are as defined herein, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: GrantFiled: April 23, 2013Date of Patent: June 10, 2014Assignee: Gilead Connecticut, Inc.Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford, James P. Harding, Antonio J. M. Barbosa, Jr., Zhongdong Zhao, David M. Armistead, Soumya Mitra
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Publication number: 20140155595Abstract: The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.Type: ApplicationFiled: May 13, 2013Publication date: June 5, 2014Applicant: Curis, Inc.Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Changgeng Qian