Nitrogen Bonded Directly To Ring Carbon Of The 1,3-diazine Ring Of The Quinazoline Ring System Patents (Class 514/266.4)
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Publication number: 20140134163Abstract: Provided is a method of treating a proliferative disease, condition, or disorder in a subject by administering a combination of an inhibitor of p53 and MDM2 binding and an EGFR inhibitor. Various embodiments of the disclosed methods provide a synergistic anti-proliferative or anti-apoptotic effect compared to administration of one agent alone.Type: ApplicationFiled: January 16, 2014Publication date: May 15, 2014Inventor: Joseph P. Errico
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Publication number: 20140135309Abstract: This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I wherein Ar, R1 and R2 are as defined herein, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.Type: ApplicationFiled: November 7, 2013Publication date: May 15, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Andreas BLUM, Dirk GOTTSCHLING, Armin HECKEL, Joerg HEHN, Thorsten LEHMANN-LINTZ, Dieter WIEDENMAYER
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Publication number: 20140127157Abstract: Antiviral activity of Nilotinib against Hepatitis C virus.Type: ApplicationFiled: November 4, 2013Publication date: May 8, 2014Inventors: Erica Canino, Adam Feire, Christopher Jones, Paul W. Manley
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Patent number: 8716285Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1 to R3 and X have the significances given herein. The present invention is also directed to processes for making said compounds and uses of said compounds, in particular their use as medicaments, more particularly their use as medicaments in the treatment of cancer.Type: GrantFiled: September 7, 2011Date of Patent: May 6, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Lei Guo, Guozhi Tang, Zhanguo Wang, Jason Christopher Wong, Weixing Zhang
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Patent number: 8710044Abstract: The invention provides novel bicyclic azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: GrantFiled: July 1, 2011Date of Patent: April 29, 2014Assignee: Merck Patent GmbHInventors: Bayard R. Huck, Constantin Neagu, Reinaldo Jones, Lizbeth Celeste DeSelm, Yufang Xiao, Srinivasa R. Karra, Ruoxi Lan, Igor Mochalkin, Amanda E. Sutton, Thomas E. Richardson
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Patent number: 8709419Abstract: The present invention relates to a combination therapy of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide, or a pharmaceutically acceptable salt thereof, and an EGFR inhibitor for treating a patient suffering from a proliferative disorder, in particular a solid tumor, for example, colorectal cancer, melanoma, and thyroid cancer.Type: GrantFiled: August 10, 2011Date of Patent: April 29, 2014Assignee: Hoffmann-La Roche, Inc.Inventors: Kapil Dhingra, Brian Higgins, Kenneth Kolinsky, Richard J. Lee, Brian Lestini, Kathryn Packman, Fei Su
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SYNERGISTIC PHARMACEUTICAL COMBINATION FOR THE TREATMENT OF SQUAMOUS CELL CARCINOMA OF HEAD AND NECK
Publication number: 20140112918Abstract: The present invention relates to a pharmaceutical combination for use in the treatment of squamous cell carcinoma, comprising a CDK inhibitor selected from the compounds of formula (I); or a pharmaceutically acceptable salt thereof and one or more antineoplastic agents selected from sorafenib, lapatinib, erlotinib, cisplatin, 5-fluorouracil, docetaxel or cetuximab or a pharmaceutically acceptable salt thereof. The said pharmaceutical combination exhibits synergy when used in the treatment of squamous cell carcinoma of head and neck (SCCHN). The invention also relates to a pharmaceutical composition comprising the said combination and a method for the treatment of squamous cell carcinoma of head and neck (SCCHN), using a therapeutically effective amount of said combination.Type: ApplicationFiled: May 30, 2012Publication date: April 24, 2014Applicant: PIRAMAL ENTERPRISES LIMITEDInventors: Veena Agarwal, Arun Balakrishnan, Giridharan Periyasamy -
Publication number: 20140105886Abstract: Glioblastoma multiforme (GBM) is an aggressive form of brain cancer. Biomarkers for GBM that provide prognostic and predictive information are useful because they provide the physician valuable information regarding treatment options for GBM. The present invention provides a method to quantify such biomarkers. Thus, the method relates to the quantification of GSK3?, S6, CREB, PTEN, AKT and mTOR biomarkers and the use of AQUA® analysis to estimate a patient's risk and benefit to treatment using an inhibitor of the AGC-family kinase. Unlike traditional IHC, the AQUA® system is objective and produces quantitative in situ protein expression data on a continuous scale. The present invention uses the AQUA system to provide a robust and standardized diagnostic assay that can be used in a clinical setting to provide prognostic and predictive information.Type: ApplicationFiled: July 9, 2013Publication date: April 17, 2014Inventors: Waldron Donald E., Pinard Robert, Gustavson Mark
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Publication number: 20140105969Abstract: The present invention provides, in part, compositions and methods for treating cancer using a combination of C6-ceramide and other anti-cancer agents.Type: ApplicationFiled: April 4, 2012Publication date: April 17, 2014Inventor: Harold J. Wanebo
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Publication number: 20140100195Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: ApplicationFiled: October 5, 2012Publication date: April 10, 2014Inventors: Richard D. Caldwell, Kevin M. GUCKIAN, Gnanasambandam KUMARA VEL, Wen-Cherng LEE, Edward Yin-Shiang LIN, Xiaogao LlU, Bin MA, Daniel M. SCOTT, Zhan SHl, Jermaine THOMAS, Arthur G. TAVERAS, Guo Zhu ZHENG
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Publication number: 20140100188Abstract: The present disclosure relates to an immune signature of tumor infiltrating leukocytes. In particular, the disclosure provides methods and kits for determining the immune signature of tumor infiltrating leukocytes for use in assessing risk of cancer recurrence and long term survival, and for developing a treatment regimen for a cancer patient.Type: ApplicationFiled: October 2, 2013Publication date: April 10, 2014Applicants: University College Dublin, The Regents of the University of CaliforniaInventors: Lisa M. COUSSENS, David G. DENARDO, Donal J. BRENNAN
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Publication number: 20140088100Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.Type: ApplicationFiled: July 11, 2013Publication date: March 27, 2014Applicant: BLUEPRINT MEDICINESInventors: Neil Bifulco, JR., Natasja Brooijmans, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu
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Publication number: 20140080780Abstract: Herein, methods of modulating inclusion formation and stress granules in cells are described. The methods comprise contacting a cell with an inclusion inhibitor. Methods for screening for modulators of TDP-43 aggregation are also described.Type: ApplicationFiled: May 21, 2012Publication date: March 20, 2014Inventor: Benjamin WOLOZIN
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Publication number: 20140080848Abstract: A series of mono- and di-substituted quinazoline and pyrimidine derivatives based on the skeleton of erlotinib (an EGFR inhibitor) were synthesized and their bioactivities against hepatocellular carcinoma and human lung adenocarcinoma were evaluated.Type: ApplicationFiled: September 13, 2013Publication date: March 20, 2014Applicants: National Taiwan University, National Yang-Ming UniversityInventors: Chung-Wai SHIAU, Kuen-Feng CHEN
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Publication number: 20140080783Abstract: The present invention relates to the field of oncology and provides compositions and methods for treating specific cancers, including non small cell lung cancer, breast cancer, thyroid cancer, pancreatic cancer, colon cancer, melanoma, hepatoma and adenocarcinoma. Particularly, compositions and methods involving administration, either simultaneously or sequentially, of pharmaceutical combinations comprising (S)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide with other compounds, to patients suffering from cancer are described.Type: ApplicationFiled: November 18, 2013Publication date: March 20, 2014Applicant: ARDEA BIOSCIENCES, INC.Inventor: Mark CHAPMAN
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Publication number: 20140079736Abstract: The invention provides methods of treating or preventing malaria comprising administering to an animal an effective amount of a compound of formula (I): Q-Y—R1—R2 (I), wherein Q, Y, R1, and R2 are as described herein. Methods of inhibiting a plasmodial surface anion channel of a parasite in an animal are also provided. The invention also provides pharmaceutical compositions comprising a compound represented by formula (I) in combination with any one or more compounds represented by formulas II, V, and VI. Use of the pharmaceutical compositions for treating or preventing malaria or for inhibiting a plasmodial surface anion channel in animals including humans are also provided. Also provided by the invention are clag3 amino acid sequences and related nucleic acids, vectors, host cells, populations of cells, antibodies, and pharmaceutical compositions.Type: ApplicationFiled: April 11, 2012Publication date: March 20, 2014Applicant: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventor: Sanjay A. Desai
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Publication number: 20140073642Abstract: This invention relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy of disorders in which the modulation of toll-like-receptors is involved.Type: ApplicationFiled: May 18, 2012Publication date: March 13, 2014Applicant: Janssen R&D IrelandInventors: David McGowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers, Stefaan Julien Last, Werner Embrechts, Serge Maria Aloysius Pieters
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Patent number: 8669265Abstract: The present invention provides a novel and stable hydrated form of erlotinib free base, and a process for its preparation thereof. The present invention also provides a process for preparation of erlotinib hydrochloride crystalline polymorph a substantially free of polymorph B. The present invention further relates to erlotinib hydrochloride crystalline particles having mean particle size (D50) ranging from about 4 ?m to 15 ?m and 90 volume-% of the particles (D90) ranging from about 14 ?m to 30 ?m, to the methods for the manufacture of said crystalline particles, and to pharmaceutical compositions comprising said crystalline particles.Type: GrantFiled: May 23, 2013Date of Patent: March 11, 2014Assignee: Hetero Drugs LimitedInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Thungathurthy Srinivas Rao
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Publication number: 20140066465Abstract: A method of treating cancer by administering to a subject in need thereof a therapeutically effective amount of a tyrosine kinase inhibitor and an NF-?B inhibitor is described. The method is useful for treating subjects having cancer that has developed resistance to tyrosine kinase inhibitors.Type: ApplicationFiled: September 4, 2013Publication date: March 6, 2014Applicant: The Cleveland Clinic FoundationInventors: George R. Stark, Kam Tai Dermawan
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Publication number: 20140056910Abstract: Provided are a pharmaceutical composition which enhances the sensitivity of a cancer to a molecular target drug, such as gefitinib and erlotinib, wherein the cancer has resistance to the molecular target drug, and a cancer therapeutic agent effective against a cancer having resistance to a molecular target drug, such as gefitinib and erlotinib. The pharmaceutical composition comprising an HGF-MET receptor pathway inhibitor enhances the sensitivity of a cancer to a molecular target drug, such as gefitinib and erlotinib, even though the cancer has resistance to the molecular target drug. The cancer therapeutic agent comprising a molecular target drug in combination with an HGF-MET receptor pathway inhibitor is effective against a cancer having resistance to the molecular target drug.Type: ApplicationFiled: October 18, 2013Publication date: February 27, 2014Applicant: Kringle Pharma Inc.Inventors: Seiji YANO, Kunio MATSUMOTO
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Patent number: 8658170Abstract: Provided is a method of treating a proliferative disease, condition, or disorder in a subject by administering a combination of an inhibitor of p53 and MDM2 binding and an EGFR inhibitor. Various embodiments of the disclosed methods provide a synergistic anti-proliferative or anti-apoptotic effect compared to administration of one agent alone.Type: GrantFiled: July 21, 2011Date of Patent: February 25, 2014Inventors: Joseph P. Errico, Benjamin Mugrage, Ignatius Turchi, Matthew Sills, Jane Ong, John Allocco, Pam Wines
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Publication number: 20140045841Abstract: The present invention provides a method for inhibiting the growth of cancer stem cells, particularly colorectal cancer stem cells, liver cancer stem cells, lung cancer stem cells or breast cancer stem cells, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of antimycin A or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier.Type: ApplicationFiled: October 18, 2013Publication date: February 13, 2014Inventors: Chi-Ying F. Huang, Chi-Tai Yeh, Chun-Hung Wu, Yu-Wen Liu
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Publication number: 20140038958Abstract: The invention relates to the compounds and methods for inhibiting the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. More particularly, the invention relates to compounds and methods for inhibiting the CDKI pathway for studies of and intervention in senescence-related and other CDKI-related diseases. The invention provides new compounds having improved solubility and/or potency, and methods for their use. In various aspects, the invention relates to the treatment of cancer. The invention provides methods for chemoprevention and prevention of tumor recurrence or metastasis. The invention further provides diagnostic techniques for treatment for certain cancer types. The invention utilizes specific inhibitors of CDK8/19 and/or measurement of CDK8 levels in a patient.Type: ApplicationFiled: February 1, 2013Publication date: February 6, 2014Applicant: SENEX BIOTECHNOLOGY INC.Inventors: Igor B. Ronnison, Donald C. Porter, Mark P. Wentland
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Publication number: 20140031310Abstract: In alternative embodiments the invention provides compositions, e.g., pharmaceutical compositions and preparations, formulations, kits and other products of manufacture, e.g., exemplary drug combinations packaged together or separately in blister packs, lidded blisters or blister cards, or wrapped in paper, plastic or cellophane wrappers (e.g., a shrink wrap), comprising combinations of beneficial ingredients that in alternative embodiments are serviceable as therapies or palliatives for treating, preventing or improving conditions, states and disease symptoms involving the use of targeted protein kinase inhibitors such as Multi-Kinase Inhibitors (MKIs) or Epidermal Growth Factor Receptor (EGFR) Inhibitors (EGFRIs), or the use of other oral oncolytics, such as capcitabine or erlotinib, known to be associated with drug-induced dermatological toxicity, e.g.Type: ApplicationFiled: January 18, 2012Publication date: January 30, 2014Inventors: John Maki, Newell Bascomb, Timothy J. Turner, Fredric Young
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Publication number: 20140030254Abstract: The present invention relates to the identification and diagnostic use of biomarkers in primary colorectal cancer tumors whose activation level are predictive of the likelihood of the onset of metastatic disease. These biomarkers may be used to determine the suitability of a patient for aggressive and/or targeted treatments. Kits and compositions of the invention are also provided.Type: ApplicationFiled: March 27, 2013Publication date: January 30, 2014Inventors: Emanuel F. Petricoin, III, Lance A. Liotta, Mariaelena Pierobon, Alessandra Silvestri
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Publication number: 20140031345Abstract: A compound of formula I wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.Type: ApplicationFiled: September 27, 2013Publication date: January 30, 2014Inventors: James A. Johnson, John Lloyd, Heather Finlay, Ji Jiang, James Neels, Naveen Kumar Dhondi, Prashantha Gunaga, Abhisek Banerjee
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Publication number: 20140018375Abstract: The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with an EGFR kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an EGFR kinase inhibitor, comprising assessing whether the tumor cell has undergone an epithelial to mesenchymal transition (EMT), by determining the expression level of epithelial and/or mesenchymal biomarkers, wherein tumor cells that have undergone an EMT are substantially less sensitive to inhibition by EGFR kinase inhibitors. Improved methods for treating cancer patients with EGFR kinase inhibitors that incorporate the above methodology are also provided. Additionally, methods are provided for the identification of new biomarkers that are predictive of responsiveness of tumors to EGFR kinase inhibitors.Type: ApplicationFiled: February 22, 2013Publication date: January 16, 2014Inventor: OSI Pharmaceuticals, LLC
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Publication number: 20140011821Abstract: The present invention relates to mutations in Epidermal Growth Factor Receptor (EGFR) and methods of detecting such mutations as well as prognostic methods method for identifying a tumors that are susceptible to anticancer therapy such as chemotherapy and/or kinase inhibitor treatment. The methods involve determining the presence of a mutated EGFR gene or mutated EGFR protein in a tumor sample whereby the presence of a mutated EGFR gene or protein indicates the tumor is susceptible to treatment.Type: ApplicationFiled: August 21, 2013Publication date: January 9, 2014Applicant: GENENTECH, INC.Inventor: Somasekar Seshagiri
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Publication number: 20140004192Abstract: The present invention relates to pharmaceutical formulations that increase the solubility and bioavailability of indibulin, such as a spray-dried solid dispersion of indibulin with at least one matrix polymer. The invention further provides dosage formulations comprising the dispersion and processes for making the dispersion. The present invention also discloses a method of treating immune system based disorders, hyper-proliferative disorders, angiogenesis, malignancies, and neoplasms with the indibulin formulations disclosed herein.Type: ApplicationFiled: March 12, 2013Publication date: January 2, 2014Inventors: John C. Amedio, JR., Barbara Wallner, Marsha G. Marande
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Publication number: 20130345236Abstract: A drug in a solubility-improved form is combined with a concentration-enhancing polymer in a sufficient amount so that the combination provides substantially enhanced drug concentration in a use environment relative to a control comprising the same amount of the same solubility-improved form of drug without the concentration-enhancing polymer.Type: ApplicationFiled: June 11, 2013Publication date: December 26, 2013Inventors: William J. Curatolo, Ravi M. Shanker, Walter C. Babcock, Dwayne T. Friesen, James A. S. Nightingale, Douglas A. Lorenz
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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: 20130338167Abstract: The present invention relates to tartrate salts of quinazoline containing zinc-binding moiety based derivatives of Formula II, below: These compounds are inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and may further act as HDAC inhibitors. The invention further relates to the use of these tartrate salts in the treatment of EGFR-TK related diseases and disorders such as cancer.Type: ApplicationFiled: May 22, 2013Publication date: December 19, 2013Applicant: CURIS, INC.Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
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Patent number: 8604044Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives of Formula (IV) below. These compounds have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and are useful in the treatment of EGFR-TK related diseases and disorders such as cancer. These compounds may further act as HDAC inhibitors.Type: GrantFiled: September 10, 2007Date of Patent: December 10, 2013Assignee: Curis, Inc.Inventors: Changgeng Qian, Xiong Cai, Stephen Gould, Haixiao Zhai
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Patent number: 8598344Abstract: The invention relates to compounds for inhibiting the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. More particularly, the invention relates to compounds for inhibiting the CDKI pathway for studies of and intervention in senescence-related and other CDKI-related diseases.Type: GrantFiled: November 30, 2010Date of Patent: December 3, 2013Assignee: Senex BiotechnologyInventors: Donald C. Porter, Igor B. Roninson, Mark P. Wentland
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Publication number: 20130302337Abstract: This disclosure relates to methods and compositions useful for treating Alzheimer's disease. In particular, the disclosure relates to pharmaceutical compositions containing an EGFR-inhibitory compound suitable for administration to treat Alzheimer's disease, as well as to related therapeutic methods. In addition, this disclosure relates to screening methods for identifying compounds useful for treating Alzheimer's disease based on the ability to inhibit the activity of EGFR.Type: ApplicationFiled: July 24, 2013Publication date: November 14, 2013Inventors: Yi Zhong, Hsueh-cheng Chiang, Lei Wang
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Publication number: 20130296271Abstract: Agri-horticultural pest control compositions having outstanding control effect on pests, in particular, agri-horticultural pests, which comprise as active ingredients one or more 4-(3-butynyl)aminopyrimidine derivatives represented by the general formula [I], namely, where R1 is typically selected from among: a) phenyl c) —SiR5R6R7 (R5, R6, and R7 which may be the same or different represent a linear or branched alkyl having 1-6 carbon atoms, a linear or branched haloalkyl having 1-3 carbon atoms which is substituted by one halogen atom, a linear or branched cyanoalkyl having 1-3 carbon atoms which is substituted by one cyano group, and phenyl); d) hydropgen atom; R2 typically represents a hydrogen atom; R3 typically represents a hydrogen atom; R4 represents a hydrogen atom and one or more agri-horticultural pest control compounds selected from among agri-horticultural antimicrobial compounds, say, multi-site contact active compouns, nucleic acids synthesis inhibitory active compounds, mitosis and cellType: ApplicationFiled: December 27, 2011Publication date: November 7, 2013Applicant: SDS Biotech K.K.Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Tomoko Muraki, Ryutaro Katsuki
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Publication number: 20130289044Abstract: The invention relates to aryl substituted quinazolines of Formula I, and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, A, and R1-R4 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: October 5, 2011Publication date: October 31, 2013Applicant: Purdue Pharma L.P.Inventors: R. Richard Goehring, Laykea Tafesse, Jiangchao Yao
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Publication number: 20130280241Abstract: The disclosure provides, among other things, a method of decreasing resistance to the chemopreventive properties of non-steroidal anti-inflammatory agents, e.g., celecoxib, particularly in the prevention of cancer, e.g., colon cancer, by increasing the levels or activity of 15-hydroxyprostaglandin dehydrogenase (15-PGDH). The disclosure also provides a method of identifying compounds that upregulate or reactivate 15-PGDH. The disclosure also provides a method of identifying an individual suitable for treatment with a non-steroidal anti-inflammatory agent in the treatment or prevention of colon cancer.Type: ApplicationFiled: June 20, 2013Publication date: October 24, 2013Inventors: Sanford D. Markowitz, Monica Bertagnolli
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Publication number: 20130281448Abstract: Provided herein are small molecule compounds for the treatment of inflammatory conditions, and pharmaceutical compositions and methods relating thereto. For example, provided herein are compositions comprising small molecule compounds for the treatment of conditions such as multiple sclerosis, type 2 diabetes, psoriasis, rheumatoid arthritis, Hashimoto's thyroiditis, and Crohn's disease. In some embodiments, the pharmaceutical composition and methods described herein pertain to small molecule compounds previously known for the treatment of another condition, such as non-small-cell lung cancer (NSCLC).Type: ApplicationFiled: April 18, 2013Publication date: October 24, 2013Inventor: Marvin B. Brooks
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Publication number: 20130280336Abstract: The present invention features methods for treating, stabilizing, preventing, and/or delaying cancer by administering nanoparticles that comprise rapamycin or a derivative thereof. The invention also provides compositions (e.g., unit dosage forms) comprising nanoparticles that comprise a carrier protein and rapamycin or a derivative thereof. The invention further provides combination therapy methods of treating cancer comprising administering to an individual an effective amount of nanoparticles that comprise rapamycin or a derivative thereof and a second therapy.Type: ApplicationFiled: February 27, 2013Publication date: October 24, 2013Inventors: Neil P. DESAI, Patrick SOON-SHIONG, Vuong TRIEU
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Publication number: 20130261139Abstract: Disclosed is a use of a quinazoline compound of Formula I having 2,4-diaminoquinazoline as a parent nucleus in preparation of a medicament for treating diseases caused by flaviviridae infection, especially a use in combating Hepatitis C virus infection and Dengue fever virus infection.Type: ApplicationFiled: December 2, 2011Publication date: October 3, 2013Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCESInventors: Jianping Zuo, Youhong Hu, Wei Tang, Bo Chao, Xiankun Tong, Dewen Li, Feihong Ji, Peilan He
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Publication number: 20130251702Abstract: Methods for screening compounds for treating sepsis are disclosed. The present methods and compositions are targeting NOD2 mediated signaling pathway and the agents identified by the present methods are qualified as drug candidates for clinical development. Further Methods and composition for treating sepsis are disclosed.Type: ApplicationFiled: March 21, 2013Publication date: September 26, 2013Applicant: SNU R&DB FOUNDATIONInventors: Doo Hyun CHUNG, Sae Jin OH, Ji Hyung KIM
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Publication number: 20130252978Abstract: The present invention provides a novel and stable hydrated form of erlotinib free base, and a process for its preparation thereof. The present invention also provides a process for preparation of erlotinib hydrochloride crystalline polymorph a substantially free of polymorph B. The present invention further relates to erlotinib hydrochloride crystalline particles having mean particle size (D50) ranging from about 4 ?m to 15 ?m and 90 volume-% of the particles (D90) ranging from about 14 ?m to 30 ?m, to the methods for the manufacture of said crystalline particles, and to pharmaceutical compositions comprising said crystalline particles.Type: ApplicationFiled: May 23, 2013Publication date: September 26, 2013Applicant: HETERO RESEARCH FOUNDATIONInventors: BANDI PARTHASARADHI REDDY, KURA RATHNAKAR REDDY, RAPOLU RAJI REDDY, DASARI MURALIDHARA REDDY, THUNGATHURTHY SRINIVAS RAO
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Publication number: 20130243754Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.Type: ApplicationFiled: December 20, 2012Publication date: September 19, 2013Applicant: TARGEGEN, INC.Inventors: Wolfgang WRASIDLO, Elena DNEPROVSKAIA
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Publication number: 20130236511Abstract: The present invention provides methods for impregnating a porous carrier with an active pharmaceutical ingredient (“AP”), the methods comprising steps: a) dissolving at least one API in a solvent to form an API solution; b) contacting a porous carrier with the at least one API of step (a) in a contactor to form an API impregnated porous carrier; and c) drying the at least one API impregnated porous carrier.Type: ApplicationFiled: August 19, 2011Publication date: September 12, 2013Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: Fernando J. Muzzio, Benjamin J. Glasser, Plamen I. Grigorov
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Publication number: 20130236473Abstract: A major object of the present invention is to provide a novel therapeutic or prophylactic agent for at least one disease or symptom selected from the group consisting of autoimmune diseases, inflammatory diseases, allergic diseases, and symptoms accompanying organ transplants; the therapeutic or prophylactic agent artificially controls the activity of IL-6 amplifier, thus controlling immune reactions in living organisms. Another object of the present invention is to provide an immunosuppressant, an inflammatory cytokine production inhibitor, and an IL-6 amplifier inhibitor. The compound that inhibits expression of the function of a protein belonging to ErbB1 pathway provided as means for achieving the object is capable of suppressing the activity of IL-6 amplifier, thereby reducing production of inflammatory cytokine such as IL-6.Type: ApplicationFiled: September 14, 2011Publication date: September 12, 2013Applicant: OSAKA UNIVERSITYInventors: Toshio Hirano, Masaaki Murakami
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Patent number: 8530654Abstract: Crystals, amorphous substances, salts, and hydrates of a salt of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]terephthalamic acid having PDE4 inhibitory action are provided. These compounds are useful for treating allergic diseases such as atopic dermatitis.Type: GrantFiled: February 15, 2008Date of Patent: September 10, 2013Assignee: Eisai R&D Management Co., Ltd.Inventors: Eiichi Yamamoto, Osamu Asano, Jun Niijima, Kazumasa Nara
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Patent number: 8530653Abstract: The present invention is directed to compounds that are specifically structured to provide enzyme inhibition. In specific embodiments, the enzyme inhibiting compounds exhibit antifolate activity. Particularly, the inventive compounds are formed of an antifolate residue that is active in inhibiting one or more of TS, DHFR, GAR, FPGS, and AICAR Tfase. The enzyme inhibiting compounds are useful in a variety of methods of treatment, including treating abnormal cell proliferation and treating inflammation.Type: GrantFiled: November 4, 2010Date of Patent: September 10, 2013Assignee: Chelsea Therapeutics, Inc.Inventor: Michael J. Roberts
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Publication number: 20130224192Abstract: The present invention relates to methods for the prognosis of the progression of cancer in a patient, and more particularly methods for the prediction of the occurrence of metastasis in one or more tissue or organ of patients affected with a cancer, in particular with a breast cancer, a lung cancer or other primary cancer, said methods comprising the step of detecting a higher expression level of FERMT1 gene in a tumour sample compared to a control reference values. The invention further relates to inhibitors of FERMT1 expression and their uses in the treatment of cancer or metastasis.Type: ApplicationFiled: September 2, 2011Publication date: August 29, 2013Applicant: Institut National de la Sante et de la Recherche Medicale (Inserm)Inventors: Rosette Lidereau, Keltouma Driouch, Soraya Sin, Florian Bonin
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Publication number: 20130225596Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compound of the formula (I): wherein ring A is substituted or unsubstituted 5 to 7-membered cycloalkane, substituted or unsubstituted 5 to 7-membered cycloalkene or the like; C is a carbon atom; —X— is —N(R16)— or the like; R16 is hydrogen, substituted or unsubstituted alkyl or the like; R7 is substituted or unsubstituted 5- or 6-membered heteroaryl, substituted or unsubstituted 6 to 10 membered aryl; Q1 and Q2 are each independently a carbon atom or a nitrogen atom; -L- is —O—, —S— or the like; R6 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl or the like; R2 is hydrogen, hydroxy or the like, or its pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: August 9, 2011Publication date: August 29, 2013Inventors: Hiroyuki Kai, Takeshi Endoh, Sae Jikihara, Kentaro Asahi, Tohru Horiguchi