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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Patent number: 8202879Abstract: A compound which inhibits both of EGF receptor tyrosine kinase and HER2 tyrosine kinase is provided. A compound represented by the general formula (I): wherein RX is a group represented by the formula: wherein R1 is a hydrogen atom, optionally substituted alkyl, etc.; Z is —O—, —N(R10)—, etc.; R10 is a hydrogen atom, alkyl, etc.; R2 is a hydrogen atom, optionally substituted alkyl, etc.; R18 is a hydrogen atom, optionally substituted alkyl, etc.; R19 is optionally substituted alkyl, etc.; W1 is an optionally substituted non-aromatic nitrogen-containing group; R17 is a hydrogen atom, optionally substituted alkyl, etc.; R3 and R4 are independently a hydrogen atom, optionally substituted alkyl, etc.; X is —O—, —S—, or —N(R12)—, etc.; R12 is a hydrogen atom, alkyl, etc.; and A is phenyl optionally having a substituent, etc., its pharmaceutically acceptable salt, or a solvate thereof.Type: GrantFiled: February 22, 2006Date of Patent: June 19, 2012Assignee: Shionogi & Co., Ltd.Inventors: Masaharu Kume, Kenji Matsuo, Naoki Omori, Masami Takayama
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Publication number: 20120141472Abstract: Disclosed herein are methods of predicting prognosis of a neoplastic disease (such as lung cancer, for example NSCLC), including determining the IGF1R gene copy number in a biological sample from a patient having a neoplastic disease; wherein an increase in IGF1R copy number predicts a good prognosis of the neoplastic disease in the patient. Also disclosed herein are methods of scoring copy number of a gene of interest in a biological sample. The method includes identifying individual cells in the sample having highest number of signals for the gene of interest detected by in situ hybridization, counting the number of signals for the gene of interest in the identified individual cells and determining an average number of signals per cell.Type: ApplicationFiled: May 28, 2010Publication date: June 7, 2012Inventors: Shalini Singh, Fabien Gaire, James Ranger-Moore
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Publication number: 20120136014Abstract: The present disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R5, R6 and Z are as described herein. The disclosure also provides pharmaceutical compositions thereof; and methods for inhibiting DHFR activity; and methods for treating cell proliferative diseases, autoimmune disease, inflammatory disease or bacterial, fungal or parasitic infection by administering a compound of Formula I.Type: ApplicationFiled: June 2, 2011Publication date: May 31, 2012Applicant: TRIUS THERAPEUTICS, INC.Inventors: Zhiyong Chen, Christopher J. Creghton, Mark Cunningham, John Finn, Mark Hilgers, Michael Jung, Lucy Aguirre Kohnen, Thanh Lam, Xiaoming Li, Mark Stidham, Les Tari, Michael Trzoss, Junhu Zhang
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Patent number: 8188102Abstract: The present invention provides a novel amide derivative of formula (I) and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising same as an active ingredient.Type: GrantFiled: June 5, 2008Date of Patent: May 29, 2012Assignee: Hanmi Holdings Co., Ltd.Inventors: Kwang-Ok Lee, Mi Young Cha, Mi Ra Kim, Young Hee Jung, Chang Gon Lee, Se Young Kim, Keukchan Bang, Bum Woo Park, Bo Im Choi, Yun Jung Chae, Mi Young Ko, Han Kyong Kim, Young-Gil Ahn, Maeng Sup Kim, Gwan Sun Lee
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Publication number: 20120129869Abstract: The invention related to the use of high-density loss of heterozygosity (LOH) mapping in lung adenocarcinoma to identify intragenic LOH and driver mutations in different domains of ALK resulted in enhanced tumor growth in xenografted mouse. Mutant (H694R and E1384K) ALKs showed activation of Y1604 ALK and downstream AKT, STAT3 and ERK signaling pathways. Increases of oncogenic signalings resulted in enhanced cell proliferation, colony-formation, cell-migration and tumor-growth in xenografted mouse. Western blot and immunohistochemistry analysis using antibody against phospho-Y1604 ALK on 11 lung cancer cell-lines and 263 cancer specimens indicated ALK activation in all lung cancers regardless of tumor stages. Treating mutant-bearing mice with ALK inhibitor WHI-P 154 resulted in tumor shrinkage, metastasis suppression, and improved survival. Hyperphosphorylation of Y1604 ALK occurred early and continuously throughout tumor progression and could be used as a biomarker to detect lung cancer.Type: ApplicationFiled: November 11, 2011Publication date: May 24, 2012Applicant: Academia SinicaInventors: Yuh-Shan Jou, Yi-Wei Wang
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Publication number: 20120128665Abstract: The present invention provides methods for the preselection of a subject for therapeutic treatment with an agent based on modulated levels of hypoxia in cancerous cells in the subject. In one embodiment, the invention provides methods for the preselection of a subject for therapeutic treatment with an agent based on modulated levels of lactate dehydrogenase (LDH) in a cell, e.g., a cancerous cell. The invention also provides methods for treating cancer in a subject by administering an effective amount of an agent to the subject, wherein the subject has been selected based on a modulated level of hypoxia. The invention further provides kits to practice the methods of the invention.Type: ApplicationFiled: November 18, 2011Publication date: May 24, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Ronald K. Blackman, Vojo Vukovic
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Publication number: 20120128625Abstract: Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.Type: ApplicationFiled: January 12, 2010Publication date: May 24, 2012Inventors: Robert Shalwitz, Kevin G. Peters
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Publication number: 20120128732Abstract: The present invention provides combination therapy methods of treating a proliferative disease (such as cancer) comprising a first therapy comprising administering to an individual an effective amount of a taxane in a nanoparticle composition, and a second therapy which may include the administration of an effective amount of at least one other agent that inhibits a pro survival and/or inflammatory signal.Type: ApplicationFiled: December 11, 2009Publication date: May 24, 2012Inventors: Vuong Trieu, Osmond D'Cruz, Neil P. Desai
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Publication number: 20120122881Abstract: The present invention relates to a composition comprising an inclusion complex of a cyclodextrin and quinazoline containing zinc-binding moiety based derivatives. The cyclodextrin is preferable a ?-cyclodextrin or a derivative thereof. The quinazolines have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.Type: ApplicationFiled: January 17, 2012Publication date: May 17, 2012Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai, Rudi Bao
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Patent number: 8178546Abstract: 2,5-Diaryl-1,2,4-triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase Type 1 enzyme (11?-HSD-1). The compounds are useful for the treatment of diabetes, hyperglycemia, obesity, insulin resistance, atherosclerosis, dyslipidemia, hyperlipidemia, hypertension, and Metabolic Syndrome. Also disclosed are novel compounds of structural formula II which are inhibitors of 11?-HSD-1.Type: GrantFiled: April 14, 2010Date of Patent: May 15, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Susan D. Aster, James M. Balkovec, Donald W. Graham, Xin Gu, Nancy J. Kevin, Gool F. Patel, Mitree Ponpipom
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Patent number: 8178544Abstract: This invention provides 2,3-diamino-quinazolinone compounds of Formula (I) stereoisomers thereof, pharmaceutically-acceptable addition salts thereof, and N-oxides thereof, wherein the variables are as defined in the specification. The 2,3-diamino-quinazolinone compounds have medical utility. The 2,3-diamino-quinazolinone compounds can be used for the manufacture of medicaments, including pharmaceutical compositions. This invention also provides methods of treating disorders, diseases, or conditions which are responsive to activation of Kv7 channels.Type: GrantFiled: May 22, 2008Date of Patent: May 15, 2012Assignee: Neurosearch A/SInventors: Carsten Jessen, William Dalby Brown, Joachim Demnitz, Dorte Strøbæk, Mads P. G. Korsgaard, Palle Christophersen
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Publication number: 20120114643Abstract: Disclosed are compounds of Formula (I): and salts thereof. Also, disclosed are methods of using the compounds in the treatment of proliferative diseases, such as cancer, and to pharmaceutical compositions comprising at least one compound of Formula (I) or a pharmaceutically acceptable salt.Type: ApplicationFiled: January 12, 2012Publication date: May 10, 2012Inventors: Robert M. Borzilleri, Zhen-Wei Cai
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Publication number: 20120114639Abstract: We describe herein compositions and methods related to inferring with microbial infection. Generally, the compositions include an infection antagonist that inhibits formation of a heparin sulfonated proteoglycan (HSPG)-containing infection complex. Generally, the methods include administering to a subject an amount of a composition as described herein effective to inhibit infection by a microorganism that that infects a host through interactions that involve HSPG.Type: ApplicationFiled: November 4, 2011Publication date: May 10, 2012Inventors: MICHELLE ADAIR OZBUN, Zurab Surviladze
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Publication number: 20120114745Abstract: A method for treating or ameliorating mucocutaneous, ocular toxicities, or side effects induced by blocking cellular growth and survival signal transduction pathways. The method comprises administering to a subject in need thereof an effective amount of a histone deacetylase inhibitor and a pharmaceutically acceptable carrier, salt or solvate thereof, wherein the cell growth and survival signal transduction pathways are blocked by an antibody targeted therapy agent, antibody fragment, targeted small-molecule chemical compound, low-molecular-weight tyrosine kinase inhibitor, peptide mimetic, anti-sense oligonucleotide (DNA and/or RNA), or ribozyme.Type: ApplicationFiled: June 26, 2009Publication date: May 10, 2012Inventors: Nam-Mew Pui, Yih-Lin Chung
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Publication number: 20120108615Abstract: Certain compounds are provided that can selectively inhibit motile bacteria such as V. cholerae motility. These compounds can indirectly diminish production of cholera toxin and other major virulence required by the cholera bacterium to cause disease.Type: ApplicationFiled: October 28, 2011Publication date: May 3, 2012Applicant: Southern Research Institute and IPInventors: Ashish K. Pathak, Jorge A. Benitez, Anisia J. Silva-Benitez
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Patent number: 8168646Abstract: Disclosed are 3,4-dihydroquinazoline derivatives of formula (I), a process of preparing them and a pharmaceutical composition including them.Type: GrantFiled: May 6, 2008Date of Patent: May 1, 2012Assignee: Dongwoo Syntech Co., Ltd.Inventors: Jae Yeol Lee, Dong Joon Choo, Young Deuk Kim, Chun Rim Oh
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Publication number: 20120101116Abstract: The present invention is directed to novel quinolines and quniazolines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof which are useful for the treatment of protein kinases mediated diseases and conditions. The compounds of this invention have a general Formula (I) wherein R1 to R11 and X are defined herein.Type: ApplicationFiled: June 24, 2010Publication date: April 26, 2012Applicant: MEDOLUTION LIMITEDInventor: Dawei Zhang
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Publication number: 20120094983Abstract: A compound of formula I wherein R1, R2, R3, R4 and R5 are described herein.Type: ApplicationFiled: March 15, 2011Publication date: April 19, 2012Inventors: James A. Johnson, Yoon Jeon, John Lloyd, Heather Finlay
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Publication number: 20120094998Abstract: The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water soluble, non peptidic oligomer.Type: ApplicationFiled: April 19, 2010Publication date: April 19, 2012Applicant: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Wen Zhang
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Publication number: 20120095030Abstract: Methods of using specific microRNA to identify subjects with non-small cell lung cancer likely or unlikely to respond to treatment with tyrosine kinase inhibitors such as erlotinib, sunitinib, or vandetanib; methods of treating subjects based on identification of said subjects as likely to respond to treatment with tyrosine kinase inhibitors; and kits that facilitate the performance of the methods are disclosed.Type: ApplicationFiled: April 19, 2010Publication date: April 19, 2012Applicant: THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTEInventor: Glen Weiss
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Publication number: 20120095029Abstract: The present invention provides biomarkers which are predictive for the clinical benefit of erlotinib hydrochloride treatment in cancer patients.Type: ApplicationFiled: October 11, 2011Publication date: April 19, 2012Applicant: Hoffmann-La Roche Inc.Inventors: Angélique Augustin, Guillemette Duchateau-Nguyen, Laurent Essioux, Sabrina Golling, Barbara Klughammer, Jens Lamerz, Hanno Langen, Héléne Meistermann, Stefan Scheiblich, Manuel Tzouros
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Publication number: 20120087914Abstract: The present invention provides methods to treat cancers using inhibitors of the TRIM62 protein and methods to identify inhibitors and other modulators of the TRIM62 protein. Pharmaceutical compositions that contain an inhibitor of a TRIM62 protein are also provided.Type: ApplicationFiled: March 25, 2009Publication date: April 12, 2012Inventors: James M. Roberts, Erik Eide, Claire Faltermeier
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Publication number: 20120089541Abstract: The present invention concerns cancer biomarkers. In particular, the invention concerns c-met as biomarkers for patient selection and patient prognosis in cancer, as well as methods of therapeutic treatment, articles of manufacture and methods for making them, diagnostic kits, methods of detection and methods of advertising related thereto.Type: ApplicationFiled: August 31, 2011Publication date: April 12, 2012Applicant: Genentech, Inc.Inventors: Premal H. Patel, Amy C. Peterson, Robert L. Yauch, Jiping Zha
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Publication number: 20120077811Abstract: The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the compounds are of Formula I: where: X is any negatively charged counterion; R1 is a group of the formula —(CH2)nTr, where Tr is an aromatic nitroheterocycle or aromatic nitrocarbocycle and —(CH2)nTr acts as a reductively-activated fragmenting trigger; and n is an integer from 0 to 6; R2, R3 and R4 may each independently be selected from aliphatic or aromatic groups of a tertiary amine kinase inhibitor (R2)(R3)(R4)N, or two of R2, R3, and R4 may form an aliphatic or aromatic heterocyclic amine ring of a kinase inhibitor, or one of R2, R3 and R4 may be absent and two of R2, R3 and R4 form an aromatic heterocyclic amine ring of a kinase inhibitor. The compounds of the invention are useful in treating proliferative diseases such as cancer.Type: ApplicationFiled: March 11, 2010Publication date: March 29, 2012Inventors: Jeffrey Bruce Smaill, Adam Vorn Patterson, Michael Patrick Hay, William Alexander Denny, William Robert Wilson, Guo-Liang Lu, Robert Forbes Anderson, Ho Huat Lee, Amir Ashoorzadeh
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Publication number: 20120076775Abstract: The present invention is directed toward a method of treating cancer by administering to a patient an inhibitor of Hepatocyte Growth Factor and an inhibitor of, e.g., Epidermal Growth Factor.Type: ApplicationFiled: December 8, 2010Publication date: March 29, 2012Inventors: John Laterra, Bachchu Lal, Kyung Jin Kim
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Patent number: 8142782Abstract: Compositions and methods for promoting neural regeneration in a patient determined to have a lesion in a mature CNS neuron are disclosed. The method comprises the step of contacting the neuron with an EGFR inhibitor sufficient to promote regeneration of the neuron.Type: GrantFiled: February 18, 2009Date of Patent: March 27, 2012Assignee: Children's Medical Center CorporationInventors: Zhigang He, Vuk Koprivica
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Publication number: 20120071435Abstract: 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: March 11, 2010Publication date: March 22, 2012Applicant: Ardea Biosciences, Inc.Inventor: Mark Chapman
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Publication number: 20120070404Abstract: The present invention discloses and claims compositions, methods of treatment, and kits which cause an increase in the time of survival in cancer patients, wherein the cancer: (i) overexpresses thioredoxin or glutaredoxin and/or (ii) exhibits evidence of thioredoxin- or glutaredoxin-mediated resistance to one or more chemotherapeutic interventions. The present invention also discloses and claims methods and kits for the administration of said compositions to properly treat cancer patients. Additionally, the present invention discloses and claims methods and kits for quantitatively determining the level of expression of thioredoxin or glutaredoxin in the cancer cells of a cancer patient, methods of using those determined levels in the initial diagnosis and/or planning of subsequent treatment methodologies for said cancer patient, as well as ascertaining the potential growth “aggressiveness” of the particular cancer and treatment responsiveness of the particular type of cancer.Type: ApplicationFiled: September 16, 2010Publication date: March 22, 2012Inventor: Frederick H. Hausheer
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Publication number: 20120071477Abstract: 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.Type: ApplicationFiled: November 30, 2010Publication date: March 22, 2012Applicant: Senex Biotechnology, Inc.Inventors: Donald C. Porter, Igor B. Roninson, Mark P. Wentland
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Publication number: 20120065204Abstract: 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: ApplicationFiled: September 7, 2011Publication date: March 15, 2012Inventors: Lei Guo, Guozhi Tang, Zhanguo Wang, Jason Christopher Wong, Weixing Zhang
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Publication number: 20120058112Abstract: The combination of an IGF-1R antagonist such as a humanized antibody and an anti-proliferative drug is described. In a preferred embodiment, the present invention describes the combination of an IGF-1R antibody and an anti-proliferative drug belonging to the EGFR-inhibitor class, which is preferably erlotinib. The combination according to the present invention is useful for the treatment of tumours, including IGF-1R and/or EGFR mediated or dependent tumours.Type: ApplicationFiled: April 6, 2010Publication date: March 8, 2012Inventors: Sriram Sathyanarayanan, Shailaja Kashibhatla, Christopher Winter, Michael Chastain
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Publication number: 20120046269Abstract: The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: February 4, 2010Publication date: February 23, 2012Applicant: Merck Patent GmbHInventors: Amanda E. Sutton, Ruoxi Lan, Thomas E. Richardson, David Perrey, Harold George Vandeveer, Bayard R. Huck, Srinivasa R. Karra, Xiaoling Chen, Lesley Liu-Bujalski, Andreas Goutopoulos, Frank Steiber, Brian L. Hodous, Hui Qiu, Reinaldo C. Jones, Brian H. Heasley
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Publication number: 20120045434Abstract: 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: ApplicationFiled: August 10, 2011Publication date: February 23, 2012Inventors: Kapil Dhingra, Brian Higgins, Kenneth Kolinsky, Richard J. Lee, Brian Lestini, Kathryn Packman, Fei Su
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Publication number: 20120040916Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by the Wnt/?-catenin pathway by selecting a subject with a condition mediated by the Wnt/?-catenin pathway and administering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof. A method of similarly inhibiting the Wnt/?-catenin pathway in a subject is also disclosed.Type: ApplicationFiled: December 21, 2009Publication date: February 16, 2012Applicants: MASSACHUSETTS INSTITUTE OF TECHNOLOGY, UNIVERSITY OF WASHINGTONInventors: Randall T. Moon, Travis L. Biechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass
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Publication number: 20120035194Abstract: The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein: R1, R2, Z1, t, and ring A are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of JNK, such as diabetes, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: ApplicationFiled: August 8, 2011Publication date: February 9, 2012Applicant: Pfizer Inc.Inventors: Liming Huang, Song Liu, Elizabeth A. Lunney, Simon P. Planken
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Publication number: 20120022065Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: ApplicationFiled: September 30, 2011Publication date: January 26, 2012Applicant: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
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Patent number: 8093258Abstract: The present invention relates to methods and compositions for the treatment and/or prevention of neuropathological and/or neurodegenerative diseases. In particular, the invention delivers novel uses of inhibitors of Urokinase-type Plasminogen activator in the treatment of amyotrophic lateral sclerosis.Type: GrantFiled: June 22, 2006Date of Patent: January 10, 2012Assignee: Wilex AGInventors: Stefan Lorenzl, Wolfgang Schmalix
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Publication number: 20120004249Abstract: The present invention relates to polymorphic forms of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazolin-6-yl}-acrylamide p-toluenesulfonate with the characteristic X-ray powder diffraction data as stated in the description, preparation methods thereof, pharmaceutical compositions comprising the same and the use thereof.Type: ApplicationFiled: March 25, 2009Publication date: January 5, 2012Inventors: Jianhui Guo, Yong Jiang
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Patent number: 8088766Abstract: Cyanoguanidine quinazoline and cyanoamidine quinazolamine derivatives that are useful in the treatment of hyperproliferative diseases are disclosed. Methods of treating hyperproliferative diseases in mammals are also disclosed.Type: GrantFiled: September 12, 2008Date of Patent: January 3, 2012Assignee: Array BioPharma Inc.Inventors: Eli Wallace, George Topolov, Qian Zhao, Joseph P. Lyssikatos
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Patent number: 8088782Abstract: 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline difumarate, pharmaceutical compositions containing the difumarate, the use of the difumarate in the treatment of hyperproliferative disorders such as cancer and processes for the manufacture of the difumarate are described.Type: GrantFiled: May 11, 2009Date of Patent: January 3, 2012Assignee: AstraZeneca ABInventor: Andrew Hornby Dobson
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Publication number: 20110318336Abstract: This invention relates to the identification and treatment of aggressive lung cancer tumors in patients. More particularly, it provides a method of identifying patients with non-small cell lung carcinoma (NSCLC) who have an aggressive node-negative (N0) tumor and a likelihood of a poor overall survival. The method comprises the step of determining if one or more of certain identified proteins are activated in tumor cells obtained from the patient's tumor, wherein the activation of one or more of the proteins indicates that the patient has an aggressive N0 tumor and is likely to have a poor overall-survival. The invention also provides a method for selecting a treatment for an NSCLC patient with an N0 tumor and a method for treating such patients. It further provides a kit for identifying an NSCLC patient with an aggressive N0 tumor and a likelihood of a poor overall survival and a pharmaceutical composition for treating such patients.Type: ApplicationFiled: March 29, 2011Publication date: December 29, 2011Applicant: George Mason Intellectual Properties, Inc.Inventors: Emanuel Petricoin, III, Julia Wulfkuhle, Angela Zupa
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Publication number: 20110319354Abstract: The invention relates to combination anticancer therapy with certain Akt inhibitor and other anticancer agents such as anticancer antimetabolites, anticancer antibiotics, plant-derived anticancer agents, anticancer platinum-coordinated complex compounds, anticancer camptothecin derivatives and anticancer tyrosine kinase inhibitors.Type: ApplicationFiled: February 23, 2010Publication date: December 29, 2011Inventors: Mark E. Layton, Hiroshi Hirai, Hidehito Kotani
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Publication number: 20110312919Abstract: The teachings relate to methods of identifying inhibitors of dimerization of tyrosine receptor kinases such as EGFR. The methods comprise providing, on a digital computer, a molecular model comprising a complex of extracellular dimerization domains of an RTK, docking a chemical databases to the molecular model, scoring the compounds comprised by the database, and identifying one or more high-scoring compounds. The methods further comprise testing a compound for RTK inhibitory activity in vitro, and testing a compound for specificity as an RTK inhibitor. Also disclosed are compounds selected by the described methods, and methods of treatment using the compounds. Two compounds (NSC11241 and NSC56452) are disclosed that inhibit EGF receptor kinase activation in a dose-dependent manner.Type: ApplicationFiled: June 10, 2011Publication date: December 22, 2011Applicant: Washington UniversityInventors: Garland R. Marshall, Linda J. Pike, Robert Yang
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Publication number: 20110312908Abstract: The present invention provides novel heteroaryl compounds that are linked to an aryl group via an amine linker. Such compounds are useful for the treatment of cancers.Type: ApplicationFiled: November 28, 2008Publication date: December 22, 2011Applicants: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael S. Gray, Jianming Zhang, Barun Okram, Xianming Deng, Jae Won Chang, Amy Wojciechowski
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Publication number: 20110312981Abstract: The present invention provides a biomarker SFRS7 which is predictive for the clinical benefit of EGFR inhibitor treatment in cancer patients.Type: ApplicationFiled: August 7, 2008Publication date: December 22, 2011Inventors: Paul Delmar, Barbara Klughammer, Verena Lutz, Patricia McLoughlin
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Publication number: 20110300137Abstract: The present application discloses the use of the anti-malarial drug lumefantrine and related compounds in the treatment of cancer.Type: ApplicationFiled: June 1, 2011Publication date: December 8, 2011Inventor: Douglas Tyler McKenzie
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Publication number: 20110293575Abstract: The present invention relates to a method for enhancing the activity of kinase inhibitors in target cells, and more specifically for enhancing the activity of tyrosine kinase inhibitors (TKIs), said method comprising contacting a cell with a kinase inhibitor and a photosensitizing agent and irradiating said cell with light of a wavelength effective to activate the photosensitizing agent, and to the use of this method for enhancing the effects of kinase inhibitors or kinase inhibitor-based drugs in particular to achieve cell death, for example, in cancer treatment and other diseases or conditions in which kinase inhibitors, such as TKIs, have a beneficial effect.Type: ApplicationFiled: June 26, 2009Publication date: December 1, 2011Applicant: PCI BIOTECH ASInventors: Anders Høgset, Anette Weyergang, Pål Kristian Selbo, Kristian Berg
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Publication number: 20110288082Abstract: Compounds of Formulas I-XLIII are identified as direct inhibitors of p97 ATPase or of the degradation of a p97-dependent ubiquitin-proteasome system (UPS) substrate.Type: ApplicationFiled: May 6, 2011Publication date: November 24, 2011Inventors: Raymond J. Deshaies, Tsui-Fen Chou, Frank J. Schoenen, Kelin Li, Kevin J. Frankowski, Jeffrey Aube, Samuel W. Gerritz, Han-Jie Zhou
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Patent number: 8063055Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein A0-3 and R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: GrantFiled: February 23, 2010Date of Patent: November 22, 2011Assignee: Amgen Inc.Inventors: Essa Hu, Jason Brooks Human, Roxanne Kunz, Andrew Tasker, Ryan White
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Patent number: RE43431Abstract: A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetrahydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetrahydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction medType: GrantFiled: August 18, 2009Date of Patent: May 29, 2012Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Stefan Blech, Birgit Jung, Anke Baum, Flavio Solca