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: 20130225613Abstract: The present invention relates to novel quinazoline derivatives with less skin irritation and an excellent action of strongly suppressing scratching behavior, and pharmaceutical compositions containing a quinazoline derivative as an active ingredient. The present invention is directed to the quinazoline derivatives represented by the general formula [1] or pharmaceutically acceptable salts thereof. In the general formula [1], R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 and R4 are the same or different and represent hydrogen, alkyl, alkoxy or halogen; R5 is combined with R6 to represent alkylene or represents hydrogen, hydroxy, alkyl, phenyl or alkoxy; R6 represents alkyl, cycloalkyl, phenyl, a 5- to 10-membered aromatic heterocyclic group containing one to three heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, or —N(R6-1) (R6-2).Type: ApplicationFiled: April 2, 2013Publication date: August 29, 2013Applicant: NIPPON SHINYAKU CO., LTD.Inventors: Masahiko OKANO, Tatsuya OYAMA
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Publication number: 20130217713Abstract: The present invention provides a biomarker which is predictive for the clinical benefit of EGFR inhibitor treatment in cancer patients.Type: ApplicationFiled: April 1, 2013Publication date: August 22, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130216523Abstract: Methods are provided for facilitating the diagnosis of subjects with HER1-activated cancers. In addition, method of treating subjects with a cancer characterized as having high levels of activated HER1 are provided. Also provided are methods for determining or otherwise assessing the prognosis of an subject with a HER1-activated cancer. The methods include the analysis of samples for the presence or the absence of activated HER1 markers as indicated by HER1-HER1 homodimers, HER1 phosphorylation at position 1173, pan-phosphorylation of HER1 or associated molecules, or HER1-HER2 heterodimers. Activated HER1 measurements can be used to track a subject's response to a treatment regimen, predict the success of using a particular treatment regimen, determine the effects of a treatment regimen, or for categorizing a subject in order to create a homogenous group for a clinical trial.Type: ApplicationFiled: April 2, 2012Publication date: August 22, 2013Applicant: LABORATORY CORPORATION OF AMERICA HOLDINGSInventors: Gerald J. Wallweber, John William Winslow
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Publication number: 20130217712Abstract: The present invention provides a biomarker that is predictive for the response to treatment with an EGFR inhibitor in cancer patients.Type: ApplicationFiled: April 1, 2013Publication date: August 22, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130217661Abstract: Quinazoline derivatives of the following formula: wherein R1, R2, R3, R4, R5, X, Y, and Z are defined herein. It also discloses a method of treating cancer with one of these compounds.Type: ApplicationFiled: March 18, 2013Publication date: August 22, 2013Applicant: HUTCHISON MEDIPHARMA ENTERPRISES LIMITEDInventor: Hutchison Medipharma Enterprises Limited
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Patent number: 8513269Abstract: A compound represented by the formula (I), salt thereof, or hydrate thereof has an excellent anti-pruritic effect and an excellent effect in terms of metabolism. The topical formulation of the present invention has excellent skin absorption properties of the compound represented by the formula (I), salt thereof, or hydrate thereof. Furthermore, the topical formulation of the present invention is excellent in stability because ingredients are hardly bled after long-term storage. wherein R represents hydroxyl, C1-6 alkoxy optionally substituted with C1-6 alkoxy, or amino optionally substituted with C1-6 alkyl.Type: GrantFiled: August 15, 2008Date of Patent: August 20, 2013Assignee: Eisai R&D Management Co., Ltd.Inventors: Chiharu Kimura, Maho Sakurai
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Publication number: 20130210842Abstract: The present invention relates to processes for the preparation of erlotinib and salts and polymorphs thereof, preferably of high purity. The present invention also relates to erlotinib and salts and polymorphs thereof preparable by said processes, to medical uses of said erlotinib, salts and polymorphs, and to pharmaceutical compositions comprising the same.Type: ApplicationFiled: July 22, 2011Publication date: August 15, 2013Applicant: GENERICS [UK] LIMITEDInventors: Vinayak Govind Gore, Anilkumar Tripathi, Madhav Jadhav
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Publication number: 20130210844Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.Type: ApplicationFiled: February 7, 2013Publication date: August 15, 2013Applicant: Glenmark Pharmaceuticals S.A.Inventor: Glenmark Pharmaceuticals S.A.
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Publication number: 20130210843Abstract: The present invention provides a biomarker which is predictive for the clinical benefit of EGFR inhibitor treatment in cancer patients.Type: ApplicationFiled: April 1, 2013Publication date: August 15, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8507010Abstract: The present invention provides a pharmaceutical composition, useful for the treatment of diseases characterized by abnormal PTKs activity of erbB family in a mammal, comprising pharmaceutically acceptable salts of N-{4-[3-chloro-4-(3-fluoro-benzyloxy) phenylamino]quinazolin-6-yl}-acrylamide, optionally a pharmaceutically applicable carrier or diluent, and a stabilizer having a dispersing and/or protective effect on the active ingredient. The present invention further provides a pharmaceutical formulation comprising said composition, methods for preparation of said composition and said formulation, as well as use of said composition and said formulation for treating diseases characterized by abnormal PTKs activity of erbB family in a mammal.Type: GrantFiled: May 21, 2009Date of Patent: August 13, 2013Assignee: Shanghai Allist Pharmaceuticals, Inc.Inventors: Jianhui Guo, Haiying He
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Patent number: 8507502Abstract: Fused bicyclic or tricyclic compounds of formula (I): wherein A, B, C, X, Y, m, and n are defined herein. Also disclosed are a method for inhibiting EGFR kinase activity and a method for treating cancer with these compounds.Type: GrantFiled: November 9, 2009Date of Patent: August 13, 2013Assignee: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Selvaraj Mohane Coumar, Tsu-An Hsu, Wen-Hsing Lin, Yi-Rong Chen, Yu-Sheng Chao
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Publication number: 20130203788Abstract: The present invention relates to mutations in Epidermal Growth Factor Receptor (EGFR) and KRAS and methods of detecting such mutations as well as prognostic methods for identifying 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 and/or a mutated KRAS gene or mutated KRAS protein in a tumor sample.Type: ApplicationFiled: June 7, 2012Publication date: August 8, 2013Inventor: Kenneth J. Hillan
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Publication number: 20130190310Abstract: We identify markers capable of guiding the decision to incorporate epidermal growth factor receptor (EGFR) inhibitors, in particular EGFR tyrosine kinase inhibitors (TKIs), into chemotherapeutic regimens. Mitogen-inducible gene 6 (Mig6), a negative regulator of EGFR, is selectively upregulated during the development of resistance to the EGFR tyrosine kinase inhibitor (TKI) erlotinib, resulting in decreased EGFR phosphorylation. The ratio of Mig6/EGFR expression highly correlates with erlotinib sensitivity. A low Mig6/EGFR ratio correlates with a high response rate to gefitinib and a marked increase in progression-free survival for patients. The ratio of Mig6 to EGFR is a major predictor of biologic and clinical responses to EGFR inhibitors.Type: ApplicationFiled: July 26, 2011Publication date: July 25, 2013Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: David Sidransky, Xiaofei Chang
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Publication number: 20130183297Abstract: The method of treating a person having a cancer selected from carcinoma, sarcoma or hematopoietic cancer by administering (a) an effective amount of at least one anti-cancer drug selected from the group consisting of an epidermal growth factor receptor (EGFR) inhibitor, a vascular endothelial growth factor receptor (VEGFR) inhibitor and a Raf kinase inhibitor and (b) an effective amount of 5-(4-(6-(4-amino-3,5-dimethyl-phenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy)-benzyl)-thiazolidine-2,4-dione.dihydrochloride provided that said carcinoma is not lung cancer when an EGFR inhibitor is erlotinib. The invention also provides a pharmaceutical composition that may be used in practicing said method.Type: ApplicationFiled: February 26, 2013Publication date: July 18, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventor: DAIICHI SANKYO COMPANY, LIMITED
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Publication number: 20130172656Abstract: Novel Uses of an aromatic ester isolated from Armillaria mellea, particularly, armillaridin, are disclosed herein. The armillaridin is useful for manufacturing a medicament or a pharmaceutical composition for suppressing the growth of cancerous cells or for enhancing susceptibility of esophageal cancerous cells to a radiation treatment, in a subject.Type: ApplicationFiled: January 3, 2012Publication date: July 4, 2013Inventors: Yu-Jen Chen, Chien-Chih Chen
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Publication number: 20130164218Abstract: This disclosure relates to Hypoxia Inducible Factor-1 pathway inhibitors and uses as anticancer and imaging agents. In certain embodiments, the disclosure contemplates compounds and pharmaceutical compositions disclosed herein.Type: ApplicationFiled: December 27, 2012Publication date: June 27, 2013Applicant: EMORY UNIVERSITYInventor: EMORY UNIVERSITY
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Publication number: 20130165458Abstract: A compound for treating protein kinase-related disease or disorder having a structure of formula (A): wherein X is N or CH; Y is NH, O, or CH2; Z is an aryl or a heteroaryl; and R1, R2, R3, and R4 are independently H, halo, nitro, cyano, aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, —ORa, —C(O)Ra, —C(O)NRaRb, —NRaC(O)Rb, —NRaRb, —S(O)2Ra, —S(O)2NRa Rb, —NRaS(O)2Rb, —N?CRaRb, or —NRaC(O)NHRb, wherein each of Ra and Rb, independently, is H, alkyl, alkenyl, alkynyl, aryl, aryloxy, alkoxy, hydroxy, heteroaryl, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl, or Ra and Rb, together with the nitrogen atom to which they are bonded, form heteroaryl, heterocycloalkyl, or heterocycloalkenyl; or R3 and R4 are as defined above, and R1 and R2 together with the carbons, to which they are attached, form a heterocycloalkenyl or heteroaryl.Type: ApplicationFiled: December 27, 2011Publication date: June 27, 2013Applicant: DEVELOPMENT CENTER FOR BIOTECHNOLOGYInventors: Jiann-Jyh Huang, Chu-Bin Liao, Pao-Nien Chen
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Publication number: 20130156727Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.Type: ApplicationFiled: November 21, 2012Publication date: June 20, 2013Applicant: Pharmacyclics, Inc.Inventor: Pharmacyclics, Inc.
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Publication number: 20130150358Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.Type: ApplicationFiled: February 4, 2013Publication date: June 13, 2013Applicant: HMI MEDICAL INNOVATIONS, LLC.Inventor: HMI MEDICAL INNOVATIONS, LLC.
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Publication number: 20130150385Abstract: A pharmaceutical combination comprising an EGFR inhibitor and an Hsp90 inhibitor according to the following formulae (I) or (Ia) a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables in the structural formulae are defined herein. Also provided are methods for treating a proliferative disorder in a subject in need thereof using pharmaceutical combinations disclosed herein.Type: ApplicationFiled: April 19, 2011Publication date: June 13, 2013Applicant: Synta Pharmaceuticals Corp.Inventors: Ronald K. Blackman, Kevin Paul Foley, David Proia
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Publication number: 20130150386Abstract: Described herein are methods for the treatment of lung cancer in a subject. In particular, methods are provided for the treatment of resistant lung cancer with a combination of entinostat and an EGFR inhibitor.Type: ApplicationFiled: December 7, 2012Publication date: June 13, 2013Applicant: SYNDAX PHARMACEUTICALS, INC.Inventor: Syndax Pharmaceuticals, Inc.
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Publication number: 20130150311Abstract: In one aspect, the present invention is directed to a dry, flowable and compressible composition, useful as a pharmaceutical excipient, which composition comprises a mixture of hydrophobic and hydrophilic poly(ethylene oxide)-polypropylene oxide)-poly(ethylene oxide) block copolymers, and which possesses a Carr index of less than about 20. In other aspects, the present invention is directed a pharmaceutical composition comprising such adjuvant and a pharmaceutically active ingredient; as well as to a method of making the compositions.Type: ApplicationFiled: December 13, 2011Publication date: June 13, 2013Inventors: Grzegorz Pietrzynski, Valery Alakhov, Kishore Patel
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Patent number: 8455506Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives of Formula (I) 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: April 14, 2009Date of Patent: June 4, 2013Assignee: Curis, Inc.Inventors: Changgeng Qian, Xiong Cai, Stephen Gould
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Publication number: 20130137708Abstract: The present invention sets forth a new chemical genetic approach for engineering kinase enzymes with a cysteine gatekeeper residue as well as for developing electrophilic inhibitors thereto. The present invention also provides a Src proto-oncogenic tyrosine kinase with a cysteine gatekeeper that recapitulates wild type activity and can be irreversibly inhibited both in vitro and in cells. The present invention also provides methods and compositions for modulating kinases and for treating kinase-associated diseases.Type: ApplicationFiled: November 30, 2012Publication date: May 30, 2013Applicant: The Regents of The University of CaliforniaInventor: The Regents of The University of California
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Publication number: 20130137711Abstract: 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: November 19, 2012Publication date: May 30, 2013Inventors: Shanghai Allist Pharmaceuticals, Inc., Jun Cheng
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Publication number: 20130137677Abstract: 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: ApplicationFiled: July 1, 2011Publication date: May 30, 2013Applicant: 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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Publication number: 20130121996Abstract: Six new mutations were found in exon 19 of the EGFR gene, the exon that is often mutated in tumors. The invention comprises methods of detecting the mutations, methods of prognosis and methods of predicting response to treatment based on the presence of absence of the mutations.Type: ApplicationFiled: October 30, 2012Publication date: May 16, 2013Applicant: ROCHE MOLECULAR SYSTEMS, INC.Inventor: Roche Molecular Systems, Inc.
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Publication number: 20130123203Abstract: Disclosed herein are methods and compositions for treating autism. Disclosed herein are methods and compositions for treating an autism spectrum disorder.Type: ApplicationFiled: October 31, 2012Publication date: May 16, 2013Inventors: Paul Talalay, Andrew W. Zimmerman, Kirby D. Smith
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Publication number: 20130123271Abstract: The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder.Type: ApplicationFiled: June 22, 2011Publication date: May 16, 2013Applicant: FOVEA PHARMACEUTICALSInventors: David Middlemiss, Caroline Leriche
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Patent number: 8436006Abstract: The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of ?-secretase, also known as ?-site cleaving enzyme and BACE.Type: GrantFiled: August 4, 2005Date of Patent: May 7, 2013Assignee: Jansssen Pharmaceutica N.V.Inventors: Francois Paul Bischoff, Mirielle Braeken, Serge Maria Aloysius Pieters, Mark Hubert Mercken, Hans Louis Jos De Winter, Didier Jean-Claude Berthelot
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Publication number: 20130109706Abstract: Quinazoline derivatives are provided that specifically inhibit proliferation of T cells without affecting the level of IL-2 secreted from said T cells. These compounds as well as pharmaceutical composition comprising them are useful for the treatment of indications mediated by T cell proliferation.Type: ApplicationFiled: January 27, 2011Publication date: May 2, 2013Applicant: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERSALEM LTD.Inventors: Alexander Levitzki, Idit Sagiv
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Patent number: 8431586Abstract: The present invention relates to novel quinazoline derivatives with less skin irritation and an excellent action of strongly suppressing scratching behavior, and pharmaceutical compositions containing a quinazoline derivative as an active ingredient. The present invention is directed to the quinazoline derivatives represented by the general formula [1] or pharmaceutically acceptable salts thereof. In the general formula [1], R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 and R4 are the same or different and represent hydrogen, alkyl, alkoxy or halogen; R5 is combined with R6 to represent alkylene or represents hydrogen, hydroxy, alkyl, phenyl or alkoxy; R6 represents alkyl, cycloalkyl, phenyl, a 5- to 10-membered aromatic heterocyclic group containing one to three heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, or —N(R6-1)(R6-2).Type: GrantFiled: October 3, 2006Date of Patent: April 30, 2013Assignee: Nippon Shinyaku Co., Ltd.Inventors: Masahiko Okano, Tatsuya Oyama
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Patent number: 8431585Abstract: The present invention relates to the use of specific EGF-receptor antagonists for preparing a pharmaceutical composition for the prevention and/or treatment of benign prostatic hyperplasia and/or prostatic hypertrophy, a method for the treatment or prevention of benign prostatic hyperplasia/prostatic hypertrophy comprising administering an EGF-receptor antagonist of groups (A), (B) or (C), described herein optionally in combination with known compounds for the treatment of benign prostatic hyperplasia/prostatic hypertrophy, as well as associated pharmaceutical compositions.Type: GrantFiled: February 17, 2010Date of Patent: April 30, 2013Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Thomas Singer, Stefan Platz, Florian Colbatzky
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Patent number: 8426430Abstract: Quinazoline derivatives of the following formula: wherein R1, R2, R3, R4, R5, X, Y, and Z are defined herein. It also discloses a method of treating cancer with one of these compounds.Type: GrantFiled: June 30, 2008Date of Patent: April 23, 2013Assignee: Hutchison Medipharma Enterprises LimitedInventors: Weihan Zhang, Wei-Guo Su, Haibin Yang, Yumin Cui, Yongxin Ren, Xiaoqiang Yan
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Patent number: 8426429Abstract: The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of ?-secretase, also known as ?-site cleaving enzyme and BACE.Type: GrantFiled: August 4, 2005Date of Patent: April 23, 2013Assignee: Jansssen Pharmaceutica N.V.Inventors: Ellen Baxter, Robert Boyd, Steven J. Coats, Alfonzo D. Jordan, Allen B. Reitz, Charles H. Reynolds, Mark Schulz, Malcolm Scott
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Publication number: 20130084286Abstract: The present invention provides methods of predicting response to a cancer therapy based on the methylation status of the ERBB2 gene. One aspect of the invention provides a method of predicting response to an EGFR inhibitor therapy based on the methylation status of the ERBB2 gene.Type: ApplicationFiled: August 30, 2012Publication date: April 4, 2013Inventors: Thomas E. Januario, David Shames
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Publication number: 20130084345Abstract: The invention provides combination therapy, wherein one or more other therapeutic agents are administered with indibulin or a pharmaceutically acceptable salt thereof and the combination is synergistic. Another aspect of the invention relates to the treatment of cancer with indibulin as a single agent. Another aspect of the invention relates to dosing regimen for administration of oral dosage forms of indibulin.Type: ApplicationFiled: November 20, 2012Publication date: April 4, 2013Applicant: ZIOPHARM ONCOLOGY, INC.Inventor: Ziopharm Oncology, Inc.
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Publication number: 20130084287Abstract: The present invention provides methods for determining epithelial and mesenchymal phenotype of tumors and predicting whether tumor growth will be sensitive or resistant to treatment with an EGFR inhibitor.Type: ApplicationFiled: September 28, 2012Publication date: April 4, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Publication number: 20130084281Abstract: Described herein are compositions and methods for using these compositions in the treatment of cancer, tumors, and tumor-related disorders in a subject.Type: ApplicationFiled: June 21, 2012Publication date: April 4, 2013Applicant: Tragara Pharmaceuticals, Inc.Inventors: Thomas M. Estok, Sara L. Zaknoen, Robert K. Mansfield, Tracy Lawhon
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Publication number: 20130085152Abstract: The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EOF dependency of a tumor cell for proliferation and/or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and/or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity.Type: ApplicationFiled: September 21, 2012Publication date: April 4, 2013Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Junji Matsui, Yuji Yamamoto, Toshimitsu Uenaka
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Patent number: 8404698Abstract: Quinazoline derivatives represented by the general formula pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for using the compounds for treatment of hyperproliferative disorders are also disclosed.Type: GrantFiled: June 16, 2008Date of Patent: March 26, 2013Assignee: Rexahn Pharmaceuticals, Inc.Inventors: Young Bok Lee, Chang Ho Ahn
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Publication number: 20130072484Abstract: The present invention provides methods of killing, inhibiting the growth, and/or inhibiting the reproduction of kinetoplastid or apicomplexan protozoan with tyrosine kinase inhibitors.Type: ApplicationFiled: November 14, 2012Publication date: March 21, 2013Applicant: UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.Inventor: UNIVERSITY OF GEORGIA RESEARCH FOUND
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Publication number: 20130071382Abstract: 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: June 29, 2012Publication date: March 21, 2013Inventor: Somasekar Seshagiri
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Patent number: 8399461Abstract: The present invention relates to bicyclic heterocycles of general formula the tautomers, the stereoisomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, as well as benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.Type: GrantFiled: November 3, 2007Date of Patent: March 19, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Birgit Jung
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Patent number: 8383637Abstract: The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of ?-secretase, also known as ?-site cleaving enzyme and BACE.Type: GrantFiled: August 4, 2005Date of Patent: February 26, 2013Assignee: Jansssen Pharmaceutica N.V.Inventors: Ellen Baxter, Francois Paul Bischoff, Robert E. Boyd, Mirielle Braeken, Steve Coats, Yifang Huang, Alfonzo D. Jordan, Chi Luo, Marc Hubert Mercken, Serge Maria Aloysius Pieters, Allen B. Reitz, Charles H. Reynolds, Tina Morgan Ross, Brett A. Tounge, Mark J. Schulz, Hans Louis Jos De Winter
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Patent number: 8372856Abstract: Erlotinib hydrochloride hydrate is formed from an aqueous solution and is useful as a pharmaceutical and as a purification intermediate.Type: GrantFiled: October 25, 2007Date of Patent: February 12, 2013Assignee: Synthon BVInventor: Raymond J. H. Westheim
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Publication number: 20130035350Abstract: This disclosure concerns novel quinazoline compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful anticancer agents, especially in inhibiting the function of the EGF receptor tyrosine kinases, HER1 tyrosine kinase, and HER2 tyrosine kinase. Thus, the disclosure also concerns a method of treating hyperproliferative diseases or conditions, such as various cancers and benign prostate hyperplasia (BPH), by use of these novel compounds or a composition comprising such novel compounds.Type: ApplicationFiled: December 21, 2010Publication date: February 7, 2013Inventors: Qiang Zhang, Hongwen Zhu
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Publication number: 20130029942Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: ApplicationFiled: October 4, 2012Publication date: January 31, 2013Applicant: Myrexis, Inc.Inventor: Myrexis, Inc.
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Publication number: 20130017950Abstract: The present disclosure relates to 5,8-difluoro-4-(2-(4-(heteroaryloxy)-phenyl)ethylamino)quinazolines and their use as agrochemicals and animal health products.Type: ApplicationFiled: September 17, 2012Publication date: January 17, 2013Applicant: DOW AGROSCIENCES LLCInventors: William K. Brewster, Carla J.R. Klittich, Chenglin Yao, Yuanming Zhu, Brent J. Rieder
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Publication number: 20130018062Abstract: The perception of pain precedes the manifestation of measurable and quantifiable clinical symptoms of most diseases. Pain is an early warning signal at the beginning of a physical abnormality. The present invention discloses novel methods to ameliorate or reverse diseases at their warning stages by therapeutic intervention of pain before a definite clinical diagnosis of the abnormality can be made. Unprecedented methods to eliminate pain caused by inflammatory autoimmune response or inflammatory allergic response or malignant and benign neoplastic growth by administering metabolism blocked antifolate compounds are described.Type: ApplicationFiled: July 12, 2011Publication date: January 17, 2013Inventor: Madhavan G. Nair