Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 514/234.2)
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Publication number: 20140364430Abstract: Provided herein are PAK inhibitors.Type: ApplicationFiled: August 14, 2014Publication date: December 11, 2014Inventors: Jay LICHTER, David CAMPBELL, Benedikt VOLLRATH, Sergio G. DURÓN
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Publication number: 20140364415Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.Type: ApplicationFiled: August 26, 2014Publication date: December 11, 2014Applicant: PFIZER LIMITEDInventors: Mark David Andrews, Sharanjeet Kaur Bagal, Karl Richard Gibson, Kiyoyuki Omoto, Thomas Ryckmans, Sarah Elizabeth Skerratt, Paul Anthony Stupple
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Publication number: 20140364423Abstract: 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: ApplicationFiled: August 26, 2014Publication date: December 11, 2014Inventors: Wei-Sheng Huang, Ranny M. Thomas
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Patent number: 8906910Abstract: This invention relates to the use of imidizopyridine derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K?, PI3K?, and/or PI3K?. Suitably, the present invention relates to the use of imidizopyridines in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K? selective imidizopyridine compounds for treating cancer.Type: GrantFiled: October 16, 2012Date of Patent: December 9, 2014Assignee: GlaxoSmithKline LLCInventors: Ralph A. Rivero, Rosanna Tedesco
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Patent number: 8906909Abstract: 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: GrantFiled: May 13, 2013Date of Patent: December 9, 2014Assignee: Curis, Inc.Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Changgeng Qian
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Publication number: 20140357618Abstract: The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.Type: ApplicationFiled: August 21, 2014Publication date: December 4, 2014Inventors: Matthew P. Christopher, Francesc Xavier Fradera Llinas, Michelle Machacek, Michelle Martinez, Michael Hale Reutershan, Manami Shizuka, Binyuan Sun, Christopher Francis Thompson, B. Wesley Trotter, Matthew E. Voss, Michael D. Altman, Stephane L. Bogen, Ronald J. Doll
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Patent number: 8901118Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described, wherein the compounds have formula I: In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on one or more of Fms, Kit, Flt3, TrkA, TrkB and TrkC kinase protein.Type: GrantFiled: April 20, 2011Date of Patent: December 2, 2014Assignee: Plexxikon Inc.Inventors: Jiazhong Zhang, Prabha N. Ibrahim, Wayne Spevak, Jianming Tsai, Todd Ewing, Ying Zhang, Chao Zhang
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Publication number: 20140350011Abstract: This application relates to compounds of the Formula I as defined herein, and/or salts thereof. This application further relates to compositions and methods of using these compounds and/or salts thereof. The compounds of Formula I are useful as ALK and JAK modulators for the treatment of proliferative disorders.Type: ApplicationFiled: July 30, 2014Publication date: November 27, 2014Inventors: Henry J. Breslin, Matthew A. Curry, Diane E. Gingrich, Keith S. Learn, Gregory R. Ott, Jason C. Wagner
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Publication number: 20140349998Abstract: The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I.Type: ApplicationFiled: November 30, 2012Publication date: November 27, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Sean P Ahearn, Matthew Christopher, Christopher Dinsmore, Joon Jung, Qinglin Pu, Alexey Rivkin, Mark E. Scott, David J. Witter, Hyun Chong Woo, Brandon Cash
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Publication number: 20140350012Abstract: The invention further relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —S(?O)p-; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —O—C(?O)—; —C(?O)—C(?O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5- or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-Type: ApplicationFiled: August 11, 2014Publication date: November 27, 2014Inventors: Jean-Pierre Andre Marc Bongartz, Lieven Meerpoel, Maria Gustaaf Boeckx, Guy Rosalia Eugeen Van Lommen, Christophe Francis Robert Nestor Buyck, Daniel Obrecht, Philipp Ermert, Anatol Luther
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Publication number: 20140349995Abstract: The present invention provides a compound of formula 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: ApplicationFiled: August 8, 2014Publication date: November 27, 2014Applicant: 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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Publication number: 20140350006Abstract: The invention relates to FGF-inhibiting pyrazolopyrimidine derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.Type: ApplicationFiled: December 13, 2012Publication date: November 27, 2014Inventors: Chantal Alcouffe, Kirsten Bjegarde, Jacques Mauger
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Publication number: 20140350002Abstract: The present invention is directed to imidazopyridin-2-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: June 14, 2012Publication date: November 27, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Hannah D. Fiji, Michael J. Kelly, III, Jeffrey C. Kern, Mark E. Layton, Joseph E. Pero, Alexander J. Reif, Michael A. Rossi
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Publication number: 20140350010Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: ApplicationFiled: November 28, 2012Publication date: November 27, 2014Applicant: NOVARTIS AGInventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
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Patent number: 8895544Abstract: A method of treating a disease or condition for which a JAK inhibitor is indicated in a subject in need of such treatment, comprising administering to the subject a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, and particularly, a method for the treatment of various inflammatory diseases, particularly psoriasis, asthma and COPD.Type: GrantFiled: September 30, 2013Date of Patent: November 25, 2014Assignee: Pfizer LimitedInventors: Jotham Wadsworth Coe, Christoph Martin Dehnhardt, Peter Jones, Steven Wade Korturn, Yogesh Anil Sabnis, Florian Michel Wakenhut, Gavin Alistair Whitlock
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Publication number: 20140343056Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: ApplicationFiled: September 12, 2012Publication date: November 20, 2014Applicant: GlaxoSmithKline LLCInventors: Joelle Lorraine Burgess, Neil W. Johnson, Steven David Knight, Louis Vincent LaFrance, III, William Henry Miller, Kenneth Allen Newlander, Stuart Paul Romeril, Meagan B. Rouse, Dominic Suarez, Xinrong Tian, Sharad Kumar Verma
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Publication number: 20140343057Abstract: Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating lupus, a fibrotic condition, or inflammatory myopathies and other conditions (e.g., skin conditions).Type: ApplicationFiled: July 31, 2014Publication date: November 20, 2014Inventors: Vito J. PALOMBELLA, David G. WINKLER
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Patent number: 8883781Abstract: The present invention relates to compounds of formula IA-i useful as inhibitors of ion 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: GrantFiled: June 12, 2007Date of Patent: November 11, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Lev T. D. Fanning, Pramod Joshi, Paul Krenitsky, Andreas Termin, Dean Wilson, Yulian Zhang
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Patent number: 8883784Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.Type: GrantFiled: August 12, 2013Date of Patent: November 11, 2014Assignee: AbbVie Inc.Inventors: Andrew S. Judd, Andrew J. Souers, Zhi-Fu Tao
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Publication number: 20140329799Abstract: This invention relates to aminopyrimidinone compounds of Formula (I) that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment or prevention of inflammatory diseases, including rheumatoid arthritis and inflammatory bowel disease.Type: ApplicationFiled: October 26, 2012Publication date: November 6, 2014Inventors: W. Michael Seganish, Stephanie Nicole Brumfield, Jongwon Lim, Julius J. Matasi, William T. Mcelroy, Deen B. Tulshian, Brian J. Lavey, Michael D. Altman, Criag R. Gibeau, John William Lampe, Joey Methot, Liang Zhu
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Publication number: 20140323479Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:Type: ApplicationFiled: July 15, 2014Publication date: October 30, 2014Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
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Publication number: 20140323435Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, R6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.Type: ApplicationFiled: May 22, 2014Publication date: October 30, 2014Applicants: Cancer Research Technology Limited, Cephalon, Inc.Inventors: Bruce D. Dorsey, Keith S. Learn, Emma L. Morris, Gregory R. Ott, Jonathan R.A. Roffey, Christelle N. Soudy, Jason C. Wagner
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Publication number: 20140323480Abstract: This invention relates to the use of imidizopyridine derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K?, PI3K?, and/or PI3K?. Suitably, the present invention relates to the use of imidizopyridines in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K? selective imidizopyridine compounds for treating cancer.Type: ApplicationFiled: October 16, 2012Publication date: October 30, 2014Inventors: Ralph A. Rivero, Rosanna Tedesco
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Publication number: 20140323478Abstract: Compounds having the formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, X1, X2, and Ar are as defined herein, are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.Type: ApplicationFiled: April 30, 2014Publication date: October 30, 2014Applicant: AFRAXIS HOLDINGS, INC.Inventors: Sergio DURÓN, David CAMPBELL, Chudi NDUBAKU, Joachim RUDOLPH
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Publication number: 20140323438Abstract: The disclosure provides compounds for reducing the prevalence of the perinucleolar compartment in cells, for example, of formula (I), wherein R1, R2, R3, and R4 are as defined herein, that are useful in treating a disease or disorder associated with increased prevalence of the perinucleolar compartment, such as cancer. Also disclosed is a composition containing a pharmaceutically acceptable carrier and at least one compound embodying the principles of the invention, and a method of treating or preventing cancer in a mammal.Type: ApplicationFiled: December 17, 2012Publication date: October 30, 2014Inventors: Kevin Frankowski, Samarjit Patnaik, Sui Huang, Juan Jose Marugan, John Norton, Frank J. Schoenen, Noel Terrence Southall, Steven Titus, Wei Zheng
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Publication number: 20140323477Abstract: Compounds having the formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, X1, X2, and Ar are as defined herein, are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders using such compounds.Type: ApplicationFiled: April 30, 2014Publication date: October 30, 2014Applicant: GENENTECH, INC.Inventors: James J. CRAWFORD, Wendy LEE, Joachim RUDOLPH
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Publication number: 20140322355Abstract: Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.Type: ApplicationFiled: June 25, 2014Publication date: October 30, 2014Applicant: 3-V BIOSCIENCES, INC.Inventors: Johan D. Oslob, Robert S. McDowell, Russell Johnson, Hanbiao Yang, Marc Evanchik, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu
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Publication number: 20140315900Abstract: Provided herein are methods for treating or preventing a cancer, comprising administering an effective amount of a Dihydropyrazino-Pyrazine Compound and an effective amount of an androgen receptor antagonist to a patient having a cancer.Type: ApplicationFiled: April 16, 2014Publication date: October 23, 2014Applicant: Signal Pharmaceuticals, LLCInventors: HEATHER RAYMON, TOSHIYA TSUJI, RAMA K. NARLA, KRISTEN MAE HEGE
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Publication number: 20140315885Abstract: A series of thiazolo[5,4-d]pyrimidine derivatives of formula (I) or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof: (I) Q represents a group of formula (Qa), (Qb), (Qc), (Qd) or (Qe) are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.Type: ApplicationFiled: November 8, 2012Publication date: October 23, 2014Inventors: Daniel Christopher Brookings, Daniel James Ford, Richard Jeremy Franklin, Anant Ramrao Ghawalkar, Claire Louise Kulisa, Judi Charlotte Neuss, James Thomas Reuberson
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Patent number: 8865705Abstract: Benzimidazoles having inhibitory activity on RSV replication and having the formula the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof, compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.Type: GrantFiled: December 16, 2011Date of Patent: October 21, 2014Assignee: Janssen R&D IrelandInventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Patent number: 8865712Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.Type: GrantFiled: December 20, 2013Date of Patent: October 21, 2014Assignee: Novartis AGInventors: Sangamesh Badiger, Murali Chebrolu, Konstanze Hurth, Sebastien Jacquier, Rainer Martin Lueoend, Rainer Machauer, Heinrich Rueeger, Marina Tintelnot-Blomley, Siem Jacob Veenstra, Markus Voegtle
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Publication number: 20140309216Abstract: Compounds of Formulae Ia, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: June 26, 2014Publication date: October 16, 2014Inventors: Adrian Folkes, Stephen Shuttleworth, Irina Chuckowree, Sally Oxenford, Nan Chi Wan, Georgette Castanedo, Richard Goldsmith, Janet Gunzer-Toste, Tim Heffron, Simon Mathieu, Alan Olivero, Daniel P. Sutherlin, Bing-Yan Zhu
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Publication number: 20140309222Abstract: A series of monocyclic or bicyclic diamine-substituted thieno[2,3-d]pyrimidine and isothiazolo[5,4-d]pyrimidine derivatives are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.Type: ApplicationFiled: August 15, 2012Publication date: October 16, 2014Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&D, UCB PHARMA S.A.Inventors: Daniel Christopher Brookings, Daniel James Ford, Anant Ramrao Ghawalkar, Jean Herman, Qiuya Huang, Claire Louise Kulisa, Thierry Louat, Judi Charlotte Neuss, James Thomas Reuberson, Bart Vanderhoydonck
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Publication number: 20140309212Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.Type: ApplicationFiled: June 26, 2014Publication date: October 16, 2014Inventors: Minna Bui, Patrick Conlon, Julio H. Cuervo, Daniel A. Erlanson, Junfa Fan, Bing Guan, Brian T. Hopkins, Tracy J. Jenkins, Gnanasambandam Kumaravel, Alexey A. Lugovskoy, Doug Marcotte, Noel Powell, Daniel Scott, Laura Silvian, Art Taveras, Deping Wang, Min Zhong
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Publication number: 20140309195Abstract: Provided herein are small molecules for the induction of fibroblast proliferation and increased secretion or production of proteins. The small molecules described herein can be used for the promotion of skin regeneration. Also provided herein are methods for promoting skin regeneration and wound healing.Type: ApplicationFiled: January 8, 2014Publication date: October 16, 2014Applicant: INTERNATIONAL STEM CELL CORPORATIONInventors: Rodolfo Gonzalez, Maxim Poustovoitov, Ruslan Semechkin
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Publication number: 20140309223Abstract: The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 17, 2014Publication date: October 16, 2014Applicant: Principia Biopharma Inc.Inventor: David Michael GOLDSTEIN
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Publication number: 20140309211Abstract: Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds.Type: ApplicationFiled: May 29, 2014Publication date: October 16, 2014Applicant: ARRIEN PHARMACEUTICALS LLCInventors: Hariprasad Vankayalapati, Rajendra P. Appalaneni, Y. Venkata Krishna Reddy
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Patent number: 8859545Abstract: Tetrahydronaphthyridine and tetrahydropyrido[4,3-d]pyrimidine compounds are disclosed that have formula 1: where A, B, L, N, R1, R3, R4?, Y and Z are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, respiratory conditions, and others.Type: GrantFiled: March 1, 2010Date of Patent: October 14, 2014Assignee: Evotec AGInventors: Michael G. Kelly, John Kincaid, Carl J. Kaub
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Publication number: 20140303162Abstract: It is intended to provide a novel azabicyclo compound which exhibits both HSP90 inhibitory activity and cell proliferation inhibitory effect. Specifically disclosed is a compound represented by the following general formula (I) or a salt thereof: wherein X1 represents CH or N; any one of X2, X3 and X4 represents N, and the others represent CH; any one or two of Y1, Y2, Y3 and Y4 represent C—R4, and the others are the same or different and represent CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S and O; R2 represents an alkyl group having 1 to 6 carbon atoms, or the like; and R3 and R4 represent —CO—R5 or the like.Type: ApplicationFiled: April 1, 2014Publication date: October 9, 2014Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Makoto KITADE, Shuichi Ohkubo, Chihoko Yoshimura, Satoshi Yamashita, Hiromi Oshiumi, Takao Uno, Yuichi Kawai
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Publication number: 20140303161Abstract: The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 9, 2013Publication date: October 9, 2014Inventor: Principia Biopharma, Inc.
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Publication number: 20140303153Abstract: 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 Het, A, X, Y, Z, R1, R2, R3, R4, R5 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: March 13, 2014Publication date: October 9, 2014Inventors: Hervé GENESTE, Michael OCHSE, Karla DRESCHER, Berthold BEHL, Loic LAPLANCHE, Jürgen DINGES, Clarissa JAKOB
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Patent number: 8853193Abstract: 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: October 7, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Armin Heckel, Frank Himmelsbach, Joerg Kley, Thorsten Lehmann-Lintz, Norbert Redemann, Achim Sauer, Leo Thomas, Dieter Wiedenmayer, Phillip Black, Wesley Blackaby, Ian Linney, Matthias Austen, John Danilewicz, Martin Schneider, Kay Schreiter
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Patent number: 8853208Abstract: The invention relates to amino alcohol-substituted arylthienopyrimidinones having a formula I and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one amino alcohol-substituted arylthienopyrimidinone of the invention or its derivative, and the use of the amino alcohol-substituted arylthienopyrimidinones of the invention and their derivatives as MCH antagonists.Type: GrantFiled: August 14, 2008Date of Patent: October 7, 2014Assignee: SanofiInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Torsten Haack, Petra Lennig
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Publication number: 20140296216Abstract: A compound of formula (I) or (II) and use of the compound in the preparation of drugs for treating cancer are disclosed. The study shows that the compounds can inhibit the growth of many kinds of tumor cells, can be used for targeting epidermal growth factor receptor (EGFR), and particularly can inhibit tumor cells with single or multiple mutations of EGFR (T790M). Therefore, the compound can be used as EGFR inhibitor to treat cancer and has a relatively large application value.Type: ApplicationFiled: December 21, 2011Publication date: October 2, 2014Applicant: GUANGZHOU INSTITUTE OF BIOMEDICINE AND HEALTH, CHINESE ACADEMY OF SCIENCESInventors: Ke Ding, Shaohua Chang, Shilin Xu, Lianwen Zhang, Zhengchao Tu, Jian Ding, Meiyu Geng, Yi Chen
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Publication number: 20140296234Abstract: The invention relates to compounds of formula (I) wherein X, R1, R2, T, m, n, o have the meaning as cited in the description and the claims. Said 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 said compounds, the preparation of such compounds as well as the use as medicaments.Type: ApplicationFiled: June 13, 2014Publication date: October 2, 2014Inventors: Rosemary LYNCH, Andrew David CANSFIELD, Helen Sarah NIBLOCK, Daniel HARDY, Jane Elizabeth SCANLON, Rita ADREGO, Nigel RAMSDEN
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Publication number: 20140296203Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).Type: ApplicationFiled: October 25, 2012Publication date: October 2, 2014Inventors: Jongwon Lim, Elizabeth Helen Kelley, Joey L. Methot, Hua Zhou, Alessia Petrocchi, Faruk Mansoor, Christian Fischer, Brendan O'Boyle, David Joseph Guerin, Corey E. Bienstock, Christopher W. Boyce, Matthew H. Daniels, Danielle Falcone, Ronald D. Ferguson, Salem Fevrier, Xianhai Huang, Kathryn Ann Lipford, David L. Sloman, Kevin Wilson, Wei Zhou, David Witter, Milana M. Maletic, Phieng Siliphaivanh
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Publication number: 20140296207Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the isoquinolone entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein.Type: ApplicationFiled: June 11, 2014Publication date: October 2, 2014Inventors: Pingda REN, Yi LIU, Liansheng LI, Troy Edward WILSON
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Publication number: 20140294946Abstract: Fused pyrimidines of formula (I): wherein R1-R3, A and n have any of the values described in the specification; and pharmaceutically acceptable salts thereof; have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.Type: ApplicationFiled: June 17, 2014Publication date: October 2, 2014Inventors: Stephen J. Shuttleworth, Adrian J. Folkes, Irina S. Chuckowree, Nan Chi Wan, Timothy C. Hancox, Stewart J. Baker, Sukhjit Sohal, Mohammed A. Latif
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Publication number: 20140296169Abstract: The present disclosure relates to substituted isothiazolo[5,4-b]pyridine-2-carboxamides of the formula I, in which R1, R2, R3, R10, R11 and X are as defined in the claims. The compounds of the formula I are inhibitors of transglutaminases, in particular transglutaminase 2 (TGM2), and are suitable for the treatment of various diseases, for example degenerative joint diseases such as osteoarthritis. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: June 18, 2014Publication date: October 2, 2014Inventors: Hauke SZILLAT, Thomas LEEUW, Martin LORENZ
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Publication number: 20140296233Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: March 14, 2014Publication date: October 2, 2014Applicants: Sanofi, Celgene Avilomics Research, Inc.Inventors: Laura Akullian D'Agostino, Robert Tjin Tham Sjin, Deqiang Niu, Joseph John McDonald, Zhendong Zhu, Haibo Liu, Hormoz Mazdiyasni, Russell C. Petter, Juswinder Singh, Matthieu Barrague, Alexandre Gross, Mark Munson