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: 20140094476Abstract: 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: December 5, 2013Publication date: April 3, 2014Inventors: James D. Rodgers, Hui-Yin Li
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Patent number: 8685988Abstract: The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.Type: GrantFiled: June 13, 2013Date of Patent: April 1, 2014Assignee: Acea Biosciences, Inc.Inventors: Xiao Xu, Xiaobo Wang, Long Mao, Li Zhao, Biao Xi
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Patent number: 8685983Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: November 30, 2011Date of Patent: April 1, 2014Assignee: Amgen Inc.Inventors: Tae-Seong Kim, David Bauer, Steven Bellon, Alessadro Boezio, Shon Booker, Deborah Choquette, Derin C. D'Amico, Noel D'Angelo, Celia Dominguez, Ingrid M. Fellows, Julie Germain, Russell Graceffa, Jean-Christophe Harmange, Satoko Hirai, Daniel La, Matthew Lee, Longbin Liu, Mark H. Norman, Michele Potashman, Philip Roveto, Aaron C. Siegmund, Ning Xi, Kevin Yang
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Patent number: 8685980Abstract: The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.Type: GrantFiled: August 20, 2009Date of Patent: April 1, 2014Assignees: Novartis AG, Astex Therapeutics, Ltd.Inventors: Gilbert Ebai Besong, Christopher Thomas Brain, Clinton Alan Brooks, Miles Stuart Congreve, Claudio Dagostin, Guo He, Ying Hou, Steven Howard, Yue Li, Yipin Lu, Paul Neil Mortenson, Troy D. Smith, Moo Je Sung, Steven John Woodhead, Wojciech Wrona, Bharat Lagu
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Publication number: 20140088099Abstract: Chemical compounds that modulate kinase activity, including PI3 kinase activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: November 20, 2013Publication date: March 27, 2014Applicant: Infinity Pharmaceuticals, Inc.Inventors: Pingda REN, Yi Liu, Liansheng Li, Katrina Chan, Alfredo C. Castro, Catherine A. Evans
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Publication number: 20140088096Abstract: Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Y is and W, Z, XY, RY1, RY2 and RY3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.Type: ApplicationFiled: February 14, 2013Publication date: March 27, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Roushan Afroze, Indu T. Bharathan, Jeffrey P. Ciavarri, Paul E. Fleming, Jeffrey L. Gaulin, Mario Girard, Steven P. Langston, Francois Soucy, Tzu-Tshin Wong, Yingchun Ye
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Publication number: 20140088123Abstract: Disclosed are methods of treating lung cancer by administering to a human in need thereof effective amounts of FTS, or various analogs thereof, or a pharmaceutically acceptable salt thereof, optionally, in combination with a chemotherapeutic agent. Chemotherapeutic agents, and combinations thereof, for use with FTS, its analogs, or its salts are also disclosed.Type: ApplicationFiled: November 27, 2013Publication date: March 27, 2014Applicant: RAMOT AT TEL-AVIV UNIVERSITY LTD.Inventors: Yoel Kloog, Adi Zundelevich, Roni Haklai
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Patent number: 8673928Abstract: and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds of Formula (I) 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: GrantFiled: November 18, 2010Date of Patent: March 18, 2014Assignee: Plexxikon Inc.Inventors: Prabha N. Ibrahim, Wayne Spevak, Hanna Cho, Songyuan Shi, Chao Zhang, Ying Zhang
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Publication number: 20140073657Abstract: The present invention relates to the Janus kinase (JAK) inhibitors 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile or 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile, as well as its compositions and methods of use, which is useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, skin disorders, cancer, and other diseases.Type: ApplicationFiled: November 8, 2013Publication date: March 13, 2014Inventors: Yun-Long Li, James D. Rodgers
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Publication number: 20140066463Abstract: There is provided polymorphs and amorphous form of pemetrexed or its pharmaceutical acceptable salts and process for making thereof.Type: ApplicationFiled: April 5, 2013Publication date: March 6, 2014Applicants: DR. REDDY'S LABORATORIES, INC., DR. REDDY'S LABORATORIES LTD.Inventors: Raghavendracharyulu Venkata Palle, Sekhar Munaswamy Nariyam, Vijay Bhailalbhai Patel, Raghupati Rama Subrahmanyam Vinjamuri, Surya Narayana Devarakonda, Sesha Reddy Yarraguntla, Vamsi Krishna Mudapaka, Venu Nalivela
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Publication number: 20140066464Abstract: A method of determining the susceptibility of a cancer in a subject to treatment with an antimetabolite includes obtaining a sample of cancer cells from the subject, measuring the level of UDG expression in the cancer cells, and comparing the measured levels of UDG expression in the cancer cells to a control level.Type: ApplicationFiled: May 22, 2013Publication date: March 6, 2014Applicant: Case Western Reserve UniversityInventor: Case Western Reserve University
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Publication number: 20140065153Abstract: The invention provides for methods for treating a hair loss disorder in a subject by administering a JAK/STAT inhibitor.Type: ApplicationFiled: May 2, 2013Publication date: March 6, 2014Applicant: The Trustees of Columbia University in the City of New YorkInventors: Angela M. Christiano, Raphael Clynes
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Patent number: 8658635Abstract: The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: GrantFiled: June 3, 2009Date of Patent: February 25, 2014Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Patent number: 8658637Abstract: Compounds of Formula (IA) wherein R1, R2, R3, A, B, C, D, E, G, X, Y, and Z are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: GrantFiled: November 29, 2007Date of Patent: February 25, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Daniel Kuzmich, Darren DiSalvo, Hossein Razavi, Michael Jason Burke
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Publication number: 20140051654Abstract: The present invention relates to substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: October 16, 2013Publication date: February 20, 2014Applicant: EPIZYME, INC.Inventors: Edward J. Olhava, Richard Chesworth, Kevin W. Kuntz, Victoria M. Richon, Roy M. Pollock, Scott R. Daigle
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Publication number: 20140045802Abstract: The present invention relates to novel 4-(4-cyano-2-thioaryl)dihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: ApplicationFiled: September 12, 2012Publication date: February 13, 2014Applicant: Bayer Intellectual Property GmbHInventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig, Jens Schamberger
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Patent number: 8648086Abstract: The present invention provides 5,6-bicyclic heteroaryl-containing urea compounds of Formula I or II and use of the same for treating conditions mediated by protein kinase such as VEGFR2, c-Met, PDGFR? c-Kit, CSF1R, or EphA2.Type: GrantFiled: August 20, 2010Date of Patent: February 11, 2014Assignee: Ascepion Pharmaceuticals, Inc.Inventors: Shan Jiang, Xinglong Xing, Qishan Wang, Ren Kong
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Publication number: 20140038956Abstract: The use of sGC stimulators, sGC activators alone, or in combination with PDE5 inhibitors for the prevention and treatment of fibrotic diseases, such as systemic sclerosis, scleroderma, and the concomitant fibrosis of internal organs.Type: ApplicationFiled: May 24, 2011Publication date: February 6, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Claudia Hirth-Dietrich, Peter Sandner, Johannes-Peter Stasch, Andreas Knorr, Georges Von Degenfeld, Michael Hahn, Markus Follmann
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Patent number: 8642604Abstract: The present invention provides novel compounds that are antagonists of PI3 kinase, PI3 kinase and tyrosine kinase, PI3 kinase and mTOR, or PI33 kinase, mTOR and tyrosine kinase.Type: GrantFiled: July 24, 2009Date of Patent: February 4, 2014Assignee: The Regents of the University of CaliforniaInventors: Zachary A. Knight, Beth Apsel, Kevan M. Shokat
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Publication number: 20140024661Abstract: A group of fused two ring pyrimidine compounds having a heterocycles substituent at the 2 position and a substituted amine at the 4 position as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the pyrimidine and other ring are disclosed. In addition a group of quinazoline compounds having similar substituents at the 2 and 4 positions as well as at other positions are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity.Type: ApplicationFiled: July 19, 2013Publication date: January 23, 2014Applicant: Cleave Biosciences, Inc.Inventors: Han-Jie Zhou, Francesco Parlati
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Publication number: 20140023642Abstract: Disclosed are 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones thereof, represented by the Formula (I) wherein Ar, R1-R6 are defined herein. Compounds having Formula (I) are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity.Type: ApplicationFiled: March 31, 2012Publication date: January 23, 2014Applicant: Impact Therapeutics, Inc.Inventors: Sui Xiong Cai, Ye Edward Tian, Haijun Dong, Qingbing Xu, Lizhen Wu, Lijun Liu, Yangzhen Jiang, Qingli Bao, Guoxiang Wang, Feng Yin, Chengyun Gu, Xiuhua Hu, Xiaozhu Wang, Sishun Kang, Shengzhi Chen
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Patent number: 8633206Abstract: Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation.Type: GrantFiled: October 13, 2010Date of Patent: January 21, 2014Assignee: Pfizer Inc.Inventors: Michele Ann Promo, Jin Xie, Brad A. Acker, Susan J. Hartmann, Sergey Gregory Wolfson, Horng-Chih Huang, Eric Jon Jacobsen
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Patent number: 8633205Abstract: The present invention relates to compounds of the following formula: which are useful as inhibitors of protein 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: GrantFiled: February 2, 2006Date of Patent: January 21, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark Ledeboer, Albert Pierce, Guy Bemis, Luc Farmer, Tiansheng Wang, David Messersmith, John Duffy, Francesco Salituro, Jian Wang
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Patent number: 8633193Abstract: Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: January 26, 2011Date of Patent: January 21, 2014Assignee: Novartis AGInventors: Jun Yuan, Peter Hrnciar, Qin Guo, George D. Maynard
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Publication number: 20140018374Abstract: 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: September 20, 2013Publication date: January 16, 2014Applicant: INCYTE CORPORATIONInventors: James D. Rodgers, Stacey Shepard, Jordan S. Fridman, Krishna Vaddi
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Publication number: 20140018361Abstract: The present invention provides furano- and pyrrolo-pyrimidine and pyridine compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: July 11, 2013Publication date: January 16, 2014Inventors: Geraldine C. Harriman, Donna L. Romero, Craig E. Masse, Shaughnessy Robinson, Matthew David Wessel, Jeremy Robert Greenwood
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Patent number: 8629152Abstract: Provided are processes for the preparation of lyophilized pharmaceutically acceptable salts of pemetrexed diacid, in particular, pemetrexed disodium salt, directly from pemetrexed diacid or salts thereof, i.e., without isolating the obtained pemetrexed salt prior to lyophilizing it.Type: GrantFiled: August 14, 2007Date of Patent: January 14, 2014Assignee: Sicor, Inc.Inventors: Jonathan Busolli, Nicola Diulgheroff, Moran Pirkes, Alessandro Pontiroli, Marco Villa, Zvi Harel
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Publication number: 20140005210Abstract: 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: September 6, 2013Publication date: January 2, 2014Applicant: Incyte CorporationInventors: James D. Rodgers, Stacey Shepard, Thomas P. Maduskuie, JR., Haisheng Wang, Nikoo Falahatpisheh, Maria Rafalski, Argyrios G. Arvanitis, Louis Storace, Ravi Kumar Jalluri, Jordan S. Fridman, Krishna Vaddi
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Publication number: 20140005183Abstract: The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4 and R5 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.Type: ApplicationFiled: June 27, 2013Publication date: January 2, 2014Inventors: Paul Galatsis, Matthew Merrill Hayward, Bethany Lyn Kormos, Travis T. Wager, Lei Zhang, Antonia Friederike Stepan, Jaclyn Louise Henderson, Ravi G. Kurumbail, Patrick Robert Verhoest
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Publication number: 20140005166Abstract: The present invention provides piperidinylcyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I, as defined herein, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: ApplicationFiled: May 17, 2013Publication date: January 2, 2014Applicant: Incyte CorporationInventors: JAMES D. RODGERS, Stacey Shepard, Wenyu Zhu, Lixin Shao, Joseph Glenn
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Publication number: 20140005209Abstract: A method for treating cancer tumors, particularly ovarian cancer tumors, is described, where fused cyclic pyrimidine having a cancer treating ability is selectively delivered to an FR expressing cancerous tumor.Type: ApplicationFiled: September 6, 2013Publication date: January 2, 2014Applicants: Wayne State University, Duquesne University of the Holy GhostInventors: Aleem Gangjee, Larry H. Matherly
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Publication number: 20140005198Abstract: The present invention comprises a new class of compounds capable of modulating the activity of Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I wherein each of A1, A2, A3, A4, A5, A6, A7, A8, A9, bond B, X, rings Z1 and Z2, R1 and R3 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: ApplicationFiled: August 28, 2013Publication date: January 2, 2014Applicant: AMGEN INC.Inventors: Adrian L. SMITH, Elizabeth M. DOHERTY, Qi HUANG, Gang LIU
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Publication number: 20130345219Abstract: The present invention relates to compounds according to formulae (IA) to (ID) and compositions that inhibit the activity of Hsp90. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: August 28, 2013Publication date: December 26, 2013Applicant: Synta Pharmaceuticals Corp.Inventors: Chi-Wan Lee, Teresa Prezewloka, Weiwen Ying, Minghu Song, Zhenjian Du, Kevin Foley, Dan Zhou, Shuzhen Qin
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Publication number: 20130344063Abstract: The use of specific microRNAs (miRNAs) present in CSF as biomarkers for particular brain malignancies and disease activity.Type: ApplicationFiled: November 16, 2011Publication date: December 26, 2013Applicants: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: Anna M. Krichevsky, Nadiya Teplyuk, Brit Mollenhauer, Santosh Kesari
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Publication number: 20130345192Abstract: The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same.Type: ApplicationFiled: October 28, 2011Publication date: December 26, 2013Applicants: SUNESIS PHARMACEUTICALS, INC., BIOGEN IDEC MA INC.Inventors: Brian T. Hopkins, Daniel Scott, Patrick Conlon, Tracy J. Jenkins, Noel Powell, Bing Guan, Julio H. Cuervo, Deping Wang, Art Taveras
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Publication number: 20130345243Abstract: The present invention relates to pyrimidinedione compounds of formula (I), salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds of formula (I) or salts thereof as activators of AMPK.Type: ApplicationFiled: March 5, 2012Publication date: December 26, 2013Applicant: GLAXOSMITHKLINE LLCInventors: Anne Marie Jeanne Bouillot, Alain Claude-Marie Daugan, Yann Lamotte, Olivier Mirguet
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Publication number: 20130344149Abstract: The invention essentially relates to oral dosage forms comprising a JAK3 inhibitor, preferably tasocitinib, suitable for modified release, and processes of preparing such oral dosage forms.Type: ApplicationFiled: January 26, 2012Publication date: December 26, 2013Applicant: RATIOPHARM GMBHInventors: Ralph Stefan, Frank Sievert
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Publication number: 20130338152Abstract: The present invention provides a compound the invention, and its use as a IGF-1R inhibitor. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: March 8, 2012Publication date: December 19, 2013Applicants: IRM LLC, NOVARTIS AGInventors: Bei Chen, Robin Alec Fairhurst, Songchun Jiang, Wenshuo Lu, Thomas H. Marsilje, III, Clive McCarthy, Pierre-Yves Michellys, Stefan Stutz
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Publication number: 20130338173Abstract: The present invention relates to carbocycle-substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 5, 2011Publication date: December 19, 2013Applicant: EPIZYME, INC.Inventors: Edward J. Olhava, Richard Chesworth, Kevin W. Kuntz
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Publication number: 20130338175Abstract: Among other aspects, provided herein are multi-arm polymeric prodrug conjugates of cabazitaxel-based compounds. Methods of preparing such conjugates as well as methods of administering the conjugates are also provided. Upon administration to a patient, release of the pemetrexed-based compound is achieved.Type: ApplicationFiled: December 21, 2011Publication date: December 19, 2013Applicant: Nektar TherapeuticsInventors: Lin Cheng, Jinnifer Riggs-Sauthier
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Publication number: 20130338168Abstract: The invention provides a pharmaceutical combination comprising: a) at least one agent selected from Bcr-Abl, Flt-3, FAK and RAF kinase inhibitors; and b) at least one JAK kinase inhibitor and a method for treating or preventing a proliferative disease using such a combination.Type: ApplicationFiled: June 12, 2013Publication date: December 19, 2013Applicant: Novartis AGInventors: Nigel Cooke, Paul Maniey
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Publication number: 20130338094Abstract: 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: December 19, 2013Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventors: Stephen CRITCHLEY, Thomas G. Gant, Steven P. Langston, Edward J. Olhava, Stephane Peluso
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Publication number: 20130338137Abstract: 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: ApplicationFiled: August 30, 2012Publication date: December 19, 2013Applicant: 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: 8609647Abstract: A compound of the following general formula [I]: wherein each symbol has the same meaning as defined herein, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical use of the same in treating organ transplant rejection, graft versus host reaction after transplantation, autoimmune disease, allergic disease and chronic myeloproliferative disease.Type: GrantFiled: July 30, 2010Date of Patent: December 17, 2013Assignee: Japan Tobacco Inc.Inventors: Satoru Noji, Makoto Shiozaki, Tomoya Miura, Yoshinori Hara, Hiroshi Yamanaka, Katsuya Maeda, Akimi Hori, Masafumi Inoue, Yasunori Hase
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Patent number: 8609690Abstract: The present invention relates to compounds defined by formula (I) wherein the groups R1 and R2 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.Type: GrantFiled: August 21, 2009Date of Patent: December 17, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Bradford S. Hamilton, Frank Himmelsbach, Stefan Peters
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Publication number: 20130330322Abstract: A method of reducing the appearance of skin aging comprising the step of applying a topical composition to the skin of a human exhibiting one or more signs of skin aging selected from fine lines, wrinkles, decreased skin elasticity, decreased light reflection, uneven pigmentation (dyschromia), coarse texture, dryness, solar lentigos, seborrheic keratoses, decreased dermal thickness, and/or increased sebum production, wherein the composition consists essentially of a dermatologically acceptable carrier and a targeted immune response modifier selected the group consisting of: (i) a 5-amino thiazolo[4,5-d]pyrimidin-one compound; (ii) an 8-hydroxyadenine compound; (iii) an imidazo-1,5-napthyridine compound; (iv) a 2-substituted-8-oxodeazapurine; (v) methyl 2-(3-{[6-amino-2-butoxy-8-oxo-7H-purin-9(8H)-yl]methyl}phenyl)acetate; (vi) 2-(3-{[6-amino-2-butoxy-8-oxo-7H-purin-9(8H)-yl]methyl}phenyl)acetic acid; and (iii) methyl 2-(3-(((3-(6-amino-2-butoxy-8-oxo-7H-purin-9(8H)-yl)propyl)(3-(dimethylamino)propyl)amino) phType: ApplicationFiled: August 14, 2013Publication date: December 12, 2013Applicant: Metabeauty, Inc.Inventor: Leslie Baumann
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Publication number: 20130331375Abstract: There are provided compounds of the formula (I) wherein Q, R1 and R2 are defined herein. The compounds have activity as anticancer agents.Type: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Inventors: Nancy-Ellen Haynes, Johannes Hermann, Kyungjin Kim, Nathan Robert Scott, Lin Yi, Mark Zak
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Publication number: 20130331404Abstract: The present invention is directed to methods and compositions for inhibition of viral nucleic acid polymerases, such as RNA and DNA polymerases, and methods and compositions that are useful for treating viral infections in subjects. The methods comprise administering to the subject a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or hydrate thereof, or a composition comprising a compound of formula I, or a pharmaceutically acceptable salt or hydrate thereof, and a pharmaceutically acceptable carrier. The composition or method may optionally comprise one or more additional anti-viral agents.Type: ApplicationFiled: October 14, 2011Publication date: December 12, 2013Applicant: BioCryst Pharmaceuticals, Inc.Inventors: Shanta Bantia, Pravin L. Kotian, Yarlagadda S. Babu
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Patent number: 8604032Abstract: Provided herein are compounds of formula (I), pharmaceutical compositions comprising the compounds, and methods of use thereof The compounds provided herein modulate kinase activity, including PI3 kinase activity, and are useful for treating diseases and conditions associated with kinase activity, including diseases and conditions associated with PI3 kinase activity.Type: GrantFiled: May 20, 2011Date of Patent: December 10, 2013Assignee: Infinity Pharmaceuticals, Inc.Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Alfredo C. Castro, Catherine A. Evans
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Patent number: 8604043Abstract: The present invention relates to the Janus kinase (JAK) inhibitors 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile or 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile, as well as its compositions and methods of use, which is useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, skin disorders, cancer, and other diseases.Type: GrantFiled: May 21, 2010Date of Patent: December 10, 2013Assignee: Incyte CorporationInventors: Yun-Long Li, James D. Rodgers