The Other Cyclo In The Bicyclo Ring System Is A Pyrrole Ring (including Hydrogenated) (e.g., Pyrrolo[3,2-d]pyrimidine, Etc.) Patents (Class 514/265.1)
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Publication number: 20140328793Abstract: Compounds, compositions, and methods of treatment and prevention of HIV infection are disclosed. The compounds are pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidine JAK inhibitors. Combinations of these JAK inhibitors and additional antiretroviral compounds, such as NRTI, NNRTI, integrase inhibitors, entry inhibitors, protease inhibitors, and the like, are also disclosed. In one embodiment, the combinations include a combination of adenine, cytosine, thymidine, and guanine nucleoside antiviral agents, optionally in further combination with at least one additional antiviral agent that works via a different mechanism than a nucleoside analog. This combination has the potential to eliminate the presence of HIV in an infected patient.Type: ApplicationFiled: November 30, 2012Publication date: November 6, 2014Applicant: Emory UniversityInventors: Christina Gavegnano, Raymond F. Schinazi
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Publication number: 20140329786Abstract: The present invention relates to a combination comprising AZD5363, or a pharmaceutically acceptable salt thereof, and at least one androgen receptor signalling modulator selected from MDV-3100 (also known as enzalutamide), AZD3514, abiraterone (or an ester prodrug thereof: e.g. abiraterone acetate), and bicalutamide; or a pharmaceutically acceptable salt thereof. Each of these combinations may be useful in the treatment of cancer. The invention also relates to pharmaceutical compositions comprising such combinations, and further relates to methods of treatment comprising the simultaneous, sequential or separate administration of AZD5363, or a pharmaceutically acceptable salt thereof, with at least one androgen receptor signalling modulator as described above, to warm-blooded animal, such as a human for the treatment of cancer. The invention also relates to a kit comprising such combinations.Type: ApplicationFiled: November 30, 2012Publication date: November 6, 2014Applicant: ASTRAZENECA ABInventor: Barry Robert Davies
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Publication number: 20140322211Abstract: The present invention provides a method of determining the rheumatoid arthritis status of a subject, or the progression of rheumatoid arthritis, or the appropriate treatment for a subject with rheumatoid arthritis, comprising the steps of (a) determining the level of tenascin-C in a sample from said subject; and (b) comparing the level of tenascin-C determined in step (a) with one or more reference values. Preferably the rheumatoid arthritis referred to is erosive rheumatoid arthritis. The be accompanied when published by FIG. 5.Type: ApplicationFiled: December 12, 2012Publication date: October 30, 2014Inventor: Kim Suzanne Midwood
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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: 20140323504Abstract: The present invention relates to compounds of formula (I) wherein X1 to X5, Y, ZA, ZB, R and A have the meaning as cited in the description and the claims. Said compounds are useful as kinase inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds as well as the use as medicaments.Type: ApplicationFiled: September 20, 2012Publication date: October 30, 2014Inventors: Claudio Dagostin, Nigel Ramsden
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Publication number: 20140315931Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: April 11, 2014Publication date: October 23, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Mark Ledeboer, David Messersmith, Francois Maltais, Huai Gao, Tiansheng Wang, Jingrong Cao, John Duffy, Gabriel Martinez-Botella, Cornelia Forster, Marion Wannamaker, Francesco Salituro, Albert Pierce, Luc Farmer, Valerie Marone
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Publication number: 20140315889Abstract: The present invention relates to a novel hydroxamate derivatives, more specifically, to novel hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC), isomers thereof, pharmaceutically acceptable salts thereof, hydrates or solvates thereof, use for preparing pharmaceutical compositions, pharmaceutical compositions comprising the same, treatment method using said composition, and a preparing method of novel hydroxamate derivatives. The novel selective hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC) compositions can be used for treatment of inflammatory disease, rheumatoid arthritis, or degenerative disease.Type: ApplicationFiled: October 26, 2012Publication date: October 23, 2014Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: Yuntae Kim, Changsik Lee, Hyun-mo Yang, Hojin Choi, Jaeki Min, Soyoung Kim, Dal-Hyun Kim, Nina Ha, Jung-Min Kim, Hyojin Lim, Eunhee Ko
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Publication number: 20140314750Abstract: Described herein are methods of predicting the risk of developing ovarian cancer recurrence of a subject comprising the steps of detecting the expression levels of at least four of the six genes selected from the group consisting of AKT2, KRAS, RAC1, CALM3, RPS6KA2 and YWHAB or the gene products thereof, wherein the presence of increased expression levels of the genes or the gene products is predictive of the increased risk of developing ovarian cancer recurrence in the subject. Kits for practicing the methods are also disclosed.Type: ApplicationFiled: April 11, 2014Publication date: October 23, 2014Applicant: Wisconsin Alumni Research FoundationInventors: Christina Kendziorski Newton, Kevin Hasegawa Eng
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Patent number: 8865711Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: GrantFiled: February 3, 2012Date of Patent: October 21, 2014Assignee: H. Lundbeck A/SInventors: Andreas Ritzén, Jan Kehler, Morten Langgård, Jacob Nielsen, John Paul Kilburn, Mohamed M. Farah
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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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Patent number: 8859569Abstract: The present application relates to novel substituted annellated pyrimidines, methods for production thereof, use thereof alone or in combinations for treating and/or preventing diseases and use thereof for the production of medicinal products for treating and/or preventing diseases, in particular for treating and/or preventing cardiovascular diseases.Type: GrantFiled: August 30, 2012Date of Patent: October 14, 2014Assignees: Bayer Pharma Aktiengesellschaft, Bayer Intellectual Property GmbHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Nils Griebenow, Dieter Lang, Frank Wunder, Walter Hübsch, Niels Lindner, Alexandros Vakalopoulos, Adrian Tersteegen
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Patent number: 8859568Abstract: There are disclosed novel compounds of formula (I) wherein R1, R12, L, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders, cardiovascular disorders and respiratory disorders.Type: GrantFiled: November 3, 2010Date of Patent: October 14, 2014Assignee: Astrazeneca ABInventors: Anders Bögevig, Yvonne Lo-Alfredsson, Donald Pivonka, Anna-Karin Tidén
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Publication number: 20140303177Abstract: The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N?C(R6), (R7)C?N, (R8)N—C(O), (R8)2C—C(O), N?N or (R7)C?C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of theType: ApplicationFiled: June 20, 2014Publication date: October 9, 2014Applicants: ASTEX THERAPEUTICS LIMITED, THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL, CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Valerio BERDINI, Robert George BOYLE, Gordon SAXTY, David Winter WALKER, Steven John WOODHEAD, Paul Graham WYATT, Alastair DONALD, John CALDWELL, Ian COLLINS, Tatiana Faria DA FONSECA
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Publication number: 20140303160Abstract: The present disclosure provides compositions, pharmaceutical preparations and methods for the diagnosis and treatment of cancers expressing a GLI polypeptide. The disclosed compositions and pharmaceutical preparations may comprise one or more pyrazolyl-containing compounds, or an analog or derivative thereof.Type: ApplicationFiled: July 20, 2012Publication date: October 9, 2014Applicant: The Regents of the University of CaliforniaInventors: Biao He, Michael Mann, David M. Jablons
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Publication number: 20140303181Abstract: Disclosed herein are methods and kits used in treating a cancer characterized by aberrant activity of CSF3R. These methods involve detecting a mutation in exon 14 of CSF3R such as a mutation of T615 or T618 and treating the subject with a JAK inhibitor and/or detecting a mutation in exon 17 of CSF3R and treating with dasatinib or tyrosine kinase inhibitor with one or more targets in common with dasatinib.Type: ApplicationFiled: April 4, 2014Publication date: October 9, 2014Inventors: Jeffrey Tyner, Julia Maxson, Brian Druker
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Publication number: 20140303196Abstract: The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: ApplicationFiled: May 6, 2014Publication date: October 9, 2014Inventors: James D. Rodgers, Hui-Yin Li
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Publication number: 20140303180Abstract: Disclosed herein are methods and kits used in treating a cancer characterized by aberrant activity of CSF3R. These methods involve detecting a mutation in exon 14 of CSF3R such as a mutation of T615 or T618 and treating the subject with a JAK inhibitor and/or detecting a mutation in exon 17 of CSF3R and treating with dasatinib or tyrosine kinase inhibitor with one or more targets in common with dasatinib.Type: ApplicationFiled: April 4, 2014Publication date: October 9, 2014Inventors: Jeffrey Tyner, Julia Maxson, Brian Druker
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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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Patent number: 8853212Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: February 17, 2011Date of Patent: October 7, 2014Assignee: Merck Sharp & Dohme CorpInventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
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Patent number: 8853224Abstract: The invention relates to compounds of the general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNPs) and/or nucleoside hydrolases (NHs). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds.Type: GrantFiled: September 7, 2007Date of Patent: October 7, 2014Assignees: Industrial Research Limited, Albert Einstein College of Medicine of Yeshiva UniversityInventors: Keith Clinch, Gary Brian Evans, Richard Hubert Furneaux, Shivali Ashwin Gulab, Peter Michael Kelly, Vern L. Schramm, Peter Charles Tyler, Anthony David Woolhouse
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Publication number: 20140296176Abstract: The invention provides a method of treating a subject with cancer, particularly leukemia, lymphoma, solid cancer such as colorectal cancer, gastric cancer, bladder cancer, non-small cell lung cancer, and breast cancer, comprising administering to the subject a compound of formulae (I) 40 or (Ia) in combination with an antimetabolite such as methotrexate, pemetrexed, cytarabine or nelarabine, or 5-fluorouracil, or capecitabine or their derivatives.Type: ApplicationFiled: August 17, 2012Publication date: October 2, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: David Proia, Julie Friedland
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Publication number: 20140296260Abstract: The invention relates to novel quinazolinone compounds and their use as inhibitors of PI3 kinases, for example, PI3K?, for treating and/or preventing diseases, disorder, and conditions associated with modulating PI3 kinase activity. Novel 3-aryl-2-((arylamino)methyl)quinazolin-4(3H)-one derivatives and pharmaceutically acceptable salts or solvates thereof and their use for the treatment or prevention of diseases, disorders, and conditions associated with the activity of one or more PI3 kinase, such as PI3K?, are disclosed.Type: ApplicationFiled: March 28, 2014Publication date: October 2, 2014Inventors: Ben C. Askew, Takeru Furuya
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Publication number: 20140296204Abstract: The invention is directed to substituted heteroaryl derivatives. Specifically, the invention is directed to compounds according to Formula Q: wherein D, L, M, W, X, Y, and Z are defined herein. The compounds of the invention are inhibitors of DNA methyltransferase (DNMT) activity—including DNMT1, DNMT3a, or DNMT3b—and are useful in the treatment of cancer and hyperproliferative diseases. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: October 23, 2012Publication date: October 2, 2014Inventors: Thomas Francis Hendrickson, Koc-Kan Ho, Michael David Saunders, Brian John Stevens, Krzysztof Swierczek, Kevin Bret Wright
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Publication number: 20140296261Abstract: The invention provides a compound represented by formula (I) which may modulate a kinase, and a pharmaceutical composition thereof, as well as the method for preventing or treating a protein kinase mediated disease or condition.Type: ApplicationFiled: November 14, 2012Publication date: October 2, 2014Applicants: CENTAURUS BIOPHARMA CO., LTD., CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD,Inventors: Dengming Xiao, Jijun Li, Yan Zhu, Yuandong Hu, Huting Wang, Zhe Wang, Zanping Wang, Yongheng Wei, Yinghui Sun, Qiong Wu, Hui Zhang, Yong Peng, Fansheng Kong, Ying Sun, Hong Luo, Yongxin Han
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Patent number: 8846698Abstract: 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: GrantFiled: April 4, 2012Date of Patent: September 30, 2014Assignee: 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: 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: 20140288084Abstract: In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: October 28, 2012Publication date: September 25, 2014Applicant: VANDERBILT UNIVERSITYInventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Woods, Corey R. Hopkins, Bruce J. Melancon, Michael S. Poslusney, Darren W. Engers
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Publication number: 20140288096Abstract: The present invention provides novel PI3-Kinase antagonists and methods of use thereof.Type: ApplicationFiled: October 18, 2013Publication date: September 25, 2014Applicant: The Regents of the University of CaliforniaInventors: Zachary A. Knight, Olusegun Williams, Kevan M. Shokat
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Publication number: 20140271489Abstract: Provided herein are polymeric particles and compounds and processes that can be used to prepare polymer-based particles and methods of using those particles to localize or concentrate a subsequently delivered agent to an in vivo site.Type: ApplicationFiled: October 17, 2012Publication date: September 18, 2014Applicant: TRUSTEES OF BOSTON UNIVERSITYInventors: Mark W. Grinstaff, Aaron H. Colby, Yolonda Colson
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Publication number: 20140275004Abstract: Disclosed are compound of Formula (Ia), wherein R1, R2, and R3 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions, comprising one or more compounds of Formula (Ia).Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Alan S. Florjancic, Yunsong Tong, Thomas D. Penning, Andrew J. Souers, Rajeev Goswami
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Publication number: 20140271842Abstract: The present invention relates to oral sustained release formulations of tofacitinib and pharmaceutical acceptable salts thereof. The formulations described herein have desirable pharmacokinetic characteristics.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Pfizer Inc.Inventors: Scott Max Herbig, Sriram Krishnaswami, Joseph Kushner, IV, Manisha Lamba, Thomas C Stock
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Patent number: 8835444Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF) receptor antagonists Formula (I).Type: GrantFiled: January 31, 2011Date of Patent: September 16, 2014Assignee: Novartis AGInventors: David Beattie, Ian Bruce, Anny-Odile Colson, Andrew James Culshaw, Thomas Sharp
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Publication number: 20140256668Abstract: The present disclosure relates to compounds of formula (I-A) using the compounds wherein Ring A and the variables X, Y, R3a, R3b, R3c, R3d, R4, R5, R5?, and m are defined herein, to pharmaceutical compositions comprising the compounds, and methods of using the compounds.Type: ApplicationFiled: May 23, 2013Publication date: September 11, 2014Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventors: Stephen CRITCHLEY, Thomas G. Gant, Steven P. Langston, Edward J. Olhava, Stephane Peluso
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Publication number: 20140256705Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).Type: ApplicationFiled: March 11, 2014Publication date: September 11, 2014Inventors: Lisa A. Hasvold, Dachun Liu, Keith F. McDaniel, John Pratt, George S. Sheppard, Carol K. Wada, Kevin R. Woller
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Patent number: 8829012Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.Type: GrantFiled: January 23, 2014Date of Patent: September 9, 2014Assignee: G1 Therapeutics, Inc.Inventors: Francis X. Tavares, Jay C. Strum
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Patent number: 8829013Abstract: The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: April 18, 2014Date of Patent: September 9, 2014Assignee: Incyte CorporationInventors: James D. Rodgers, Hui-Yin Li
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Publication number: 20140249156Abstract: There is provided a method of treatment of a patient suffering from blood lipid abnormality comprises the administration of a GPR119 agonist.Type: ApplicationFiled: October 31, 2012Publication date: September 4, 2014Applicant: GlaxoSmithKline LLCInventors: Kathleen Brown, Andrew James Carpenter, Derek J.R. Nunez, Andrew Young
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Publication number: 20140249167Abstract: Disclosed are methods for the treatment of patients with diseases, disorders or conditions responsive to the inhibition of NAE (Nedd8-activating enzyme), e.g., cancer. The methods comprise administering a clinically effective amount of the NAE-inhibitor ((1S,2S,4R)-4-(4-((1S)-2,3-dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate (MLN4924) according to an intermittent dosing regimen in which there is a rest period of at least two days between each administration.Type: ApplicationFiled: October 8, 2013Publication date: September 4, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Bruce J. Dezube, Lilli M. Petruzzelli
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Publication number: 20140249168Abstract: The present application relates to novel trifluoromethyl-substituted fused pyrimidines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: February 28, 2014Publication date: September 4, 2014Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Markus FOLLMANN, Johannes-Peter STASCH, Gorden REDLICH, Dieter LANG, Alexandros VAKALOPOULOS, Frank WUNDER, Adrian TERSTEEGEN
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Patent number: 8822480Abstract: The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) such as GPR119 in a patient.Type: GrantFiled: July 15, 2009Date of Patent: September 2, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Santhosh Francis Neelamkavil, Craig D. Boyle, Samuel Chackalamannil, William J. Greenlee, Bernard R. Neustadt, Andrew W. Stamford
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Patent number: 8822481Abstract: The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: April 18, 2014Date of Patent: September 2, 2014Assignee: Incyte CorporationInventors: James D. Rodgers, Hui-Yin Li
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Publication number: 20140243306Abstract: The present invention describes new pyrrolo pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel pyrrolo pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.Type: ApplicationFiled: July 7, 2012Publication date: August 28, 2014Applicant: NOVARTIS AGInventors: Richard Heng, Elizabeth Kate Hoegenauer, Guido Koch, Robert Alexander Pulz, Anna Vulpetti, Rudolf Waelchli
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Publication number: 20140243312Abstract: Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.Type: ApplicationFiled: February 19, 2014Publication date: August 28, 2014Applicant: Pfizer Inc.Inventors: Matthew Frank Brown, Ashley Edward Fenwick, Mark Edward Flanagan, Andrea Gonzales, Timothy Allan Johnson, Neelu Kaila, Mark J. Mitton-Fry, Joseph Walter Strohbach, Ruth E. TenBrink, John David Trzupek, Rayomand Jal Unwalla, Michael L. Vazquez
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Publication number: 20140243360Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: ApplicationFiled: May 12, 2014Publication date: August 28, 2014Applicant: Incyte CorporationInventors: James D. Rodgers, Stacey Shepard
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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: 8815876Abstract: The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient. The compounds are of structure (I).Type: GrantFiled: July 15, 2009Date of Patent: August 26, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Santhosh Francis Neelamkavil, Craig D. Boyle, Bernard R. Neustadt, Samuel Chackalamannil, William J. Greenlee
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Patent number: 8815858Abstract: The invention is related to anti-viral compounds of formula (A) as defined in the claims, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well to processes and intermediates useful for preparing such compounds.Type: GrantFiled: May 20, 2011Date of Patent: August 26, 2014Assignee: Gilead Sciences, Inc.Inventors: Kyla Bjornson, Steven S. Bondy, You-chul Choi, Chien-Hung Chou, Ruchika Mishra, James D. Trenkle, Winston C. Tse, Randall W. Vivian, James G. Taylor
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Patent number: 8815877Abstract: Compounds having the formula I wherein A, R1a, R1b, R2, R3, R4, R5, R6, R7, R8, Ra, Rb, X1, X2, X3 and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.Type: GrantFiled: December 21, 2012Date of Patent: August 26, 2014Assignee: Genentech, Inc.Inventors: Ignacio Aliagas-Martin, James Crawford, Wendy Lee, Simon Mathieu, Joachim Rudolph
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Patent number: 8809336Abstract: The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N?C(R6), (R7)C?N, (R8)N—C(O), (R8)2C—C(O), N?N or (R7)C?C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R1 or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of theType: GrantFiled: September 4, 2013Date of Patent: August 19, 2014Assignees: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology LimitedInventors: Valerio Berdini, Robert George Boyle, Gordon Saxty, David Winter Walker, Steven John Woodhead, Paul Graham Wyatt, Alastair Donald, John Caldwell, Ian Collins, Tatiana Faria Da Fonseca
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Patent number: 8809352Abstract: The present invention includes novel compound and methods of treating a disease or disorder by antagonizing Bcl-2 family proteins, particularly compounds of formula (I): or pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Bcl-2 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof.Type: GrantFiled: September 8, 2010Date of Patent: August 19, 2014Assignee: Novartis AGInventors: Karen Miller-Moslin, Bakary-Barry Toure, Michael Scott Visser, Naeem Yusuff