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: 7932261Abstract: The present invention is directed to macrocycle 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, BACE1, Asp2 and memapsin2.Type: GrantFiled: February 6, 2007Date of Patent: April 26, 2011Assignee: Janssen Pharmaceutica NVInventors: Ellen W. Baxter, François P. Bischoff, Hans De Winter, Chih Yung Ho, Yifang Huang, Michael H. Parker, Allen B. Reitz, Charles H. Reynolds, Eric D. Strobel
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Patent number: 7932262Abstract: The invention provides quinazoline compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.Type: GrantFiled: April 5, 2007Date of Patent: April 26, 2011Assignee: Novartis AGInventors: Savithri Ramurthy, Xiaodong Lin, Sharadha Subramanian, Alice Rico, Xiaojong M. Wang, Rama Jain, Jeremy M. Murray, Stephen E. Basham, Robert L. Warne, Wei Shu, Yasheen Zhou, Jeffrey Dove, Mina Aikawa, Payman Amiri, Weibo Wang, Johanna M. Jansen, Allan S. Wagman, Keith B. Pfister, Simon Ng
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Publication number: 20110086039Abstract: This invention relates generally to a therapeutic use of epidermal growth factor receptor inhibitors to reduce fibrosis, e.g., liver fibrosis, or pre-cirrhosis in a subject.Type: ApplicationFiled: October 8, 2010Publication date: April 14, 2011Applicant: GENERAL HOSPITAL CORPORATION, THEInventors: Kenneth Tanabe, Bryan C. Fuchs
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Publication number: 20110077246Abstract: The present invention relates methods for treating disease conditions selected from the list consisting of benign or malignant tumors, diseases of the airways and lungs, diseases of the gastrointestinal tract, the bile duct and the gall bladder by administration to a patient in need thereof of a therapeutically effective amount of a bicyclic heterocyclic groups of general formula wherein said substituents are as defined herein.Type: ApplicationFiled: December 6, 2010Publication date: March 31, 2011Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO.Inventors: Frank HIMMELSBACH, Birgit JUNG, Flavio SOLCA
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Publication number: 20110077233Abstract: 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: October 25, 2010Publication date: March 31, 2011Applicant: 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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Publication number: 20110071144Abstract: The invention relates to quinazoline derivatives of formula (1) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group seleType: ApplicationFiled: April 23, 2010Publication date: March 24, 2011Inventors: Andrew Peter THOMAS, Craig Johnstone, Edward Clayton, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin
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Publication number: 20110065735Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: March 17, 2011Applicant: Shire LLCInventors: Bernard Golding, Richard Franklin, Peter Cicala
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Publication number: 20110065734Abstract: The present invention relates to a bifunctional compound of formula I or its pharmaceutically acceptable salts or solvates A-L-B (I) wherein A is a histone deacetylase (HDAC) inhibitory moiety, L is a single bond or a linker group and B is a protein kinase inhibitory moiety. The bifunctional compound according to formula (I) is useful for the treatment of malignant and non-malignant neoplasia and diseases related to abnormal cell growth.Type: ApplicationFiled: November 14, 2008Publication date: March 17, 2011Applicant: 4SC AGInventors: Thomas Bar, Thomas Maier, Thomas Beckers, Thomas Clossek, Siavosh Mahboobi, Andreas Sellmer
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Patent number: 7906522Abstract: The present invention provides 2-aminoquinazoline derivatives represented by formula (I): wherein R1 and R2 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, and the like; X represents a bond or CR7aR7b wherein R7a and R7b may be the same or different and each represents a hydrogen atom, and the like; when X is a bond, R3 represents substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; when X is CR7aR7b wherein R7a and R7b have the same meanings as defined above, respectively, R3 represents substituted or unsubstituted lower alkoxy, substituted or unsubstituted aryl, and the like; R4 represents a hydrogen atom, hydroxy, substituted or unsubstituted lower alkoxy, and the like; and R5 represents a hydrogen atom, substituted or unsubstituted aryl, and the like, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 28, 2006Date of Patent: March 15, 2011Assignee: Kyowa Hakko Kirin Co., LtdInventors: Kuniyuki Kishikawa, Hidetomo Imase, Hajime Kashima, Kiyotoshi Mori, Toshihide Ikemura, Yoshisuke Nakasato, Misato Tomuro
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Publication number: 20110053963Abstract: 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: November 8, 2010Publication date: March 3, 2011Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
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Publication number: 20110053932Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of Alk, Abl, Aurora-A, B-Raf, C-Raf, Bcr-Abl, BRK, Blk, Bmx, BTK, C-Kit, C-Raf, C-Src, EphB1, EphB2, EphB4, FGFR1, FGFR2, FGFR3, FLT1, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFR?, PDGFR?, PKC?, p38, Src, SIK, Syk, Tie2 and TrkB kinases.Type: ApplicationFiled: June 18, 2008Publication date: March 3, 2011Inventors: Taebo Sim, Truc Ngoc Nguyen, Baogen Wu, Yun He, Yongping Xie, Xing Wang, Guobao Zhang, Nathanael Schiander Gray
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Publication number: 20110052570Abstract: The present invention provides methods to determine the likelihood of effectiveness of an EGFR targeting treatment in a subject affected with a tumor based on the expression of EGFR of endothelial cells associated with the tumor. The present invention also provides methods of treating a subject affected with, or at risk for developing cancer with an EGFR targeting treatment and methods to screen for an EGFR targeting treatment.Type: ApplicationFiled: October 24, 2006Publication date: March 3, 2011Applicant: CHILDREN'S MEDICAL CENTER CORPORATIONInventors: Michael Klagsbrun, Dhara N. Amin, Kyoko Hida
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Publication number: 20110052583Abstract: The invention is directed to pyridinone compounds useful for modulating Met kinase, having the following structure: and is further directed to pharmaceutical compositions comprising the compound; and methods for treating proliferative diseases, such as cancer by the administration of this compound.Type: ApplicationFiled: November 8, 2010Publication date: March 3, 2011Inventors: Robert M. Borzilleri, Gretchen M. Schroeder, Zhen-Wei Cai
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Publication number: 20110044938Abstract: Compounds of a certain formula I, in which Ra and Rb have the meanings indicated in the description, are novel effective compounds with anti-proliferative and apoptosis inducing activity.Type: ApplicationFiled: August 15, 2007Publication date: February 24, 2011Applicant: NYCOMED GMBHInventors: Bjorn Bartels, Mathias Schmidt, Klaus Pekari, Thomas Beckers, Astrid Zimmermann, Volker Gekeler
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Publication number: 20110039845Abstract: A 2-aminoquinazoline derivative represented by formula (I) {wherein R1 represents a hydrogen atom, or the like, R2 represents a hydrogen atom, R3 represents formula (II) [wherein A1 represents formula (III), or the like, R8 represents lower alkyl, or the like, and R9 represents optionally substituted aryl, or the like], R4 represents hydroxy, or the like, and R5 represents optionally substituted aryl, or the like}, or a pharmaceutically acceptable salt thereof is provided.Type: ApplicationFiled: April 23, 2009Publication date: February 17, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Hajime Kashima, Tomoyuki Nishikawa, Yusuke Yamada, Toshihiro Seike, Yoshisuke Nakasato, Hiroshi Umehara
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Patent number: 7888366Abstract: 2,4-Diaminoquinazolines of formulae I-IV and VI are useful for treating spinal muscular atrophy (SMA).Type: GrantFiled: June 7, 2005Date of Patent: February 15, 2011Assignee: Families of Spinal Muscular AtrophyInventors: Jasbir Singh, Mark E. Gurney
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Publication number: 20110033461Abstract: Compositions which act synergistically to inhibit the growth of cancer cells and methods of use thereof are disclosed.Type: ApplicationFiled: March 12, 2009Publication date: February 10, 2011Inventors: Vladimir Ratushny, Erica Golemis, Igor Astsaturov, Iiya G. Serebriiskii, Louis M. Weiner
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Publication number: 20110028473Abstract: Methods employing and uses of a compound of formula (I) in inhibiting the growth of a tumor cell in a subject in need thereof. Methods employing and uses of a compound of formula (I) in treating pancreatic cancer in a subject in need of treatment for pancreatic cancer. Methods employing and uses of a compound of formula (I) in treating HER-2 positive breast cancer in a subject in need of treatment for HER-2 positive breast cancer. Methods employing and uses of a compound of formula (I) in treating drug resistant non-small cell lung cancer in a subject in need of treatment for drug resistant non-small cell lung cancer. Each of these methods can include administering to the subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: July 9, 2010Publication date: February 3, 2011Applicant: Natco Pharma Ltd.Inventors: Bhujanga rao ADIBHATLA KALI SATYA, Ramanadham JYOTHI PRASAD, Bollepalli NAGESHWARA RAO, Nannapaneni VENKAIAH CHOWDARY
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Publication number: 20110021545Abstract: 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: ApplicationFiled: August 15, 2008Publication date: January 27, 2011Applicant: Eisai R&D Management Co., Ltd.Inventors: Chiharu Kimura, Maho Sakurai
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Publication number: 20110021546Abstract: In accordance with the invention, novel gene deletions and translocations involving chromosome 2 resulting in fusion proteins combining part of Anaplastic Lymphoma Kinase (ALK) kinase with part of a secondary protein have now been identified in human solid tumors, e.g. non-small cell lung carcinoma (NSCLC). Secondary proteins include Echinoderm Microtubule-Associated Protein-Like 4 (EML-4) and TRK-Fusion Gene (TFG). The EML4-ALK fusion protein, which retains ALK tyrosine kinase activity, was confirmed to drive the proliferation and survival of NSCLC characterized by this mutation. The invention therefore provides, in part, isolated polynucleotides and vectors encoding the disclosed mutant ALK kinase polypeptides, probes for detecting it, isolated mutant polypeptides, recombinant polypeptides, and reagents for detecting the fusion and truncated polypeptides.Type: ApplicationFiled: September 28, 2010Publication date: January 27, 2011Applicant: CELL SIGNALING TECHNOLOGY, INC.Inventors: Klarisa Rikova, Herbert Haack, Laura Sullivan, Ailan Guo, Anthony Possemato, Joan MacNeill, Ting-Lei Gu, Jian Yu
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Publication number: 20110014204Abstract: The present invention relates to targets of loss of imprinting (LOI) affected IGF2 gene products in pre-malignant tissues, where methods of inhibiting those targets, including IGFR1, are disclosed to prevent tumor development in subjects at risk for developing colorectal cancer (CRC). The present invention also relates to methods of identifying increased risk in developing CRC in a subject, including methods of assessing the efficacy of a chemotherapeutic regimen. Further, the present invention relates to methods for identifying anti-neoplastic agents.Type: ApplicationFiled: December 7, 2007Publication date: January 20, 2011Inventors: Andrew P. Feinberg, Andre Levchenko, Dan L. Longo, Minoru S.H. Ko
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Patent number: 7863333Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.Type: GrantFiled: November 28, 2007Date of Patent: January 4, 2011Assignee: Bristol-Myers Squibb CompanyInventor: Percy H. Carter
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Patent number: 7863283Abstract: The present invention relates to sulphoximine-substituted quinazoline derivatives of the formula (I), processes for their preparation and their use as a medicament for the treatment of various diseases.Type: GrantFiled: June 13, 2008Date of Patent: January 4, 2011Assignee: Bayer Schering Pharma AGInventors: Duy Nguyen, Arne von Bonin, Michael Haerter, Hartmut Schirok, Anne Mengel, Martina Schaefer, Oliver von Ahsen
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Publication number: 20100330082Abstract: NLRR-1 antagonists and methods of their use in treating cancer and other disorders are provided.Type: ApplicationFiled: October 1, 2008Publication date: December 30, 2010Applicant: GENENTECH INC.Inventors: Meredith Hazen, Jo-Anne S. Hongo, Victoria Smith, Susanna Stinson
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Publication number: 20100317607Abstract: Compounds of a compound of compound of general formula (I) wherein X1, X2, A, R1R2, R3 and R4 are as defined herein; are useful as anti-mycobacterial agents, especially agents for the treatment of tuberculosis.Type: ApplicationFiled: June 24, 2008Publication date: December 16, 2010Applicant: INFECTIOUS DISEASE RESEARCH INSTITUTEInventors: Graham Michael Wynne, Olivier De Moor, Peter David Johnson, Richard John Vickers
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Publication number: 20100311742Abstract: The present invention provides methods of killing, inhibiting the growth, and/or inhibiting the reproduction of kine-toplastid or apicomplexan protozoan with tyrosine kinase inhibitors.Type: ApplicationFiled: November 21, 2007Publication date: December 9, 2010Applicant: University of Georgia Research Foundation, Inc.Inventor: Kojo Mensa-Wilmot
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Publication number: 20100310503Abstract: The present invention relates to the composition and methods of use of Stat3 pathway inhibitors or cancer stem cell inhibitors in combination treatment of cancer.Type: ApplicationFiled: September 10, 2008Publication date: December 9, 2010Inventors: Chiang Jia Li, Keith Mikule, Youzhi Li
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Publication number: 20100310675Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: June 8, 2010Publication date: December 9, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Hayley Binch, Michael Mortimore, Chris Davis, Dean Boyall, Simon Everitt, Daniel Robinson, Sharn Ramaya, Damien Fraysse, John Studley, Andrew Miller, Michael O'Donnell, Alistair Rutherford, Joanne Pinder
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Patent number: 7846938Abstract: 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: GrantFiled: September 10, 2008Date of Patent: December 7, 2010Assignee: Curis, Inc.Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
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Publication number: 20100303809Abstract: The present disclosure provides methods for determining if PTEN is elevated or reduced in one or more tumor cells relative to one or more normal cells in the same biological sample by obtaining a biological sample comprising one or more tumor cells and one or more normal cells; assaying the biological sample for expression of PTEN; quantitating an amount of PTEN expression in the one or more tumor cells and an amount of PTEN expression in the one or more normal cells; comparing the amount of PTEN expression in the tumor cells to the amount of PTEN expression in the normal cells; and determining that PTEN is elevated in the tumor cells where the amount of expression of PTEN is greater in the tumor cells as compared to the normal cells or determining that PTEN is reduced in the tumor cells where the amount of expression of PTEN is less in the tumor cells than in the normal cells.Type: ApplicationFiled: June 1, 2010Publication date: December 2, 2010Applicant: TARGETED MOLECULAR DIAGNOSTICS, LLCInventor: Sarah S. Bacus
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Publication number: 20100297118Abstract: Provided are methods for treating non-small cell lung cancer by administering a therapeutically effective amount of a hedgehog inhibitor.Type: ApplicationFiled: April 16, 2010Publication date: November 25, 2010Inventors: John MacDougall, Kip A. West
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Publication number: 20100297075Abstract: The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or a pyrroloquinolinyl-pyrrolidine-2,5-dione compound in combination with a therapeutically effective amount of a second anti-proliferative agent.Type: ApplicationFiled: February 11, 2010Publication date: November 25, 2010Applicants: ArQule, Inc., Kyowa Hakko Kirin Co., Ltd.Inventors: Thomas C.K. Chan, Dennis S. France, Kenichi Ishii, Paolo Pucci
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Publication number: 20100291025Abstract: The present invention relates to new indazole inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 13, 2010Publication date: November 18, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Tadimeti Rao, Chengzhi Zhang
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Publication number: 20100292209Abstract: The invention relates to screening for compounds and compositions that modulate neurotrophic factor signaling as reflected by modulation of factor-induced neurite outgrowth. The compounds and compositions are useful in the treatment of a variety of disorders. The invention also provides methods for preparing compounds for treatment of such disorders.Type: ApplicationFiled: March 28, 2008Publication date: November 18, 2010Applicants: Massachusetts Institute of Technology, The General Hospital Corporation d/b/a Massachuset ts General HospitalInventors: Letian Kuai, Stephen J. Haggarty
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Publication number: 20100286143Abstract: This invention relates generally to methods and materials for rapid detection of mutations for tumor genotyping.Type: ApplicationFiled: April 23, 2010Publication date: November 11, 2010Inventors: Dora Dias-Santagata, Anthony John Iafrate
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Patent number: 7829566Abstract: Quinazolines of the formula I in which R, R1, R2, R3, R4 and Y have the meaning indicated in Patent Claim 1, and their salts or solvates as glycoprotein IbIX antagonists.Type: GrantFiled: December 14, 2005Date of Patent: November 9, 2010Inventors: Werner Mederski, Ralf Devant, Gerhard Barnickel, Sabine Bernotat-Danielowski, James Vickers, Bertram Cezanne, Daljit Dhanoa, Bao-Ping Zhao, James Rinker, Mark R. Player, Edward Jaeger, Richard Soll
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Publication number: 20100273711Abstract: Provided herein are methods for the use of gene expression profiling to determine whether an individual afflicted with cancer will respond to a therapy, and in particular to therapeutic agents such as platinum-based agents and antimetabolite agents. Methods for the treatment of individuals with the therapeutic agents are also provided. Methods of predicting the efficacy of cancer therapeutic agents such as platinum-based and antimetabolite therapeutic agents are also provided. Kits including gene chips and instructions for predicting responsiveness are also provided.Type: ApplicationFiled: September 29, 2008Publication date: October 28, 2010Inventors: Anil Potti, Holly K. Dressman, Joseph R. Nevins
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Patent number: 7820683Abstract: A quinazoline derivative of the Formula I: wherein the substituents are as defined in the text for use in the production of an anti-proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal such as man.Type: GrantFiled: September 14, 2006Date of Patent: October 26, 2010Assignee: AstraZeneca ABInventors: Robert Hugh Bradbury, Bernard Christophe Barlaam, Richard Ducray
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Publication number: 20100261739Abstract: A method of treating non-small cell lung cancer (NSCLC), and especially NSCLC that has metastasized to brain is disclosed.Type: ApplicationFiled: February 16, 2010Publication date: October 14, 2010Applicant: Myriad Pharmaceuticals, Inc.Inventor: Mark Laughlin
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Publication number: 20100260674Abstract: This invention relates to novel quinazoline derivatives, and their pharmaceutically acceptable salts. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by inhibiting cell surface tyrosine receptor kinases.Type: ApplicationFiled: January 26, 2010Publication date: October 14, 2010Applicant: Concert Pharmaceuticals, Inc.Inventor: Roger Tung
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Publication number: 20100261738Abstract: The present invention relates to three novel crystalline forms of Erlotinib hydrochloride and method of preparation thereof. Erlotinib hydrochloride is N-(3-ethynylphenyl)-6,7-bis(2-methoxy ethoxy)-4-quinazolinamine hydrochloride of formula-(I). The present invention provides stable novel crystalline forms of Erlotinib hydrochloride designated as Form-M, Form-N and Form-P, and processes for the preparation of the same. Erlotinib hydrochloride can be used as medicament for the treatment of hyperproliferative disorders, such as cancers, in humans.Type: ApplicationFiled: September 11, 2007Publication date: October 14, 2010Applicant: NATCO PHARMA LIMITEDInventors: Ramanadham Jyothi Prasad, Bhujanga rao Adibhatla Kali Satya, Nannapaneni Venkaiah Chowdary
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Publication number: 20100256136Abstract: A method for treating hyperproliferative tissue in a mammal which tissue expresses ABCG2 including the steps of: a) systemically introducing from about 100 to about 1000 mg/kg of body weight of a tyrosine kinase inhibiting compound into the mammal; b) within from about 0.5 to about 24 hours after the introducing in step a) systemically introducing from about 0.05 to about 0.5 ?mol per kilogram of body weight of a tumor avid photosensitizing compound, that acts as a substrate for ABC family transport protein, ABCG2 and that has a preferential light absorbance frequency; and c) exposing the hyperproliferative tissue to light at a fluence of from about 50 to about 150 J/cm2 delivered at a rate of from about 5 to about 25 mW/cm2 at the light absorbance frequency.Type: ApplicationFiled: June 29, 2007Publication date: October 7, 2010Inventors: Ravindra K. Pandey, Allan Oseroff, Stephanie Pincus, Janet Morgan, Xiang Zheng, Weiguo Liu
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Publication number: 20100255004Abstract: The invention provides novel methods for designing and administering therapeutic treatments for subjects afflicted with cancer. One aspect provides methods of identifying RTK pathways in a cancer and formulating treatment plans based on a plurality of RTK inhibitors. The invention further provides methods for evaluating candidate tyrosine kinase inhibitors for therapeutic efficacy.Type: ApplicationFiled: April 11, 2008Publication date: October 7, 2010Applicant: Dana Farber Cancer InstituteInventors: Ronald A. DePinho, Jayne M. Stommel
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Publication number: 20100240649Abstract: A compound of formula (I), a pharmaceutically acceptable salt, or hydrate thereof, and a method of preparing the same. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase activity in a mammal comprising administering to said mammal a pharmaceutical composition comprising a compound of formula (I).Type: ApplicationFiled: May 26, 2010Publication date: September 23, 2010Inventor: Hesheng ZHANG
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Publication number: 20100239656Abstract: Compositions and methods for the treatment and diagnosis of cancer are disclosed.Type: ApplicationFiled: May 10, 2010Publication date: September 23, 2010Inventors: Igor Astsaturov, Erica A. Golemis, Ilya G. Serebriiskii, Louis M. Weiner
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Publication number: 20100234324Abstract: Novel quinazolinamide derivatives of the formula (I), in which R1-R3 have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: June 16, 2008Publication date: September 16, 2010Applicant: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Hans-Michael Eggenweiler, Christian Sirrenberg, Hans-Peter Buchstaller
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Publication number: 20100234371Abstract: The invention relates to bicyclic heterocycles of general formula (I), in which Ra, Rb, Rc, Rd, Re and X are as defined in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, in particular, the physiologically-acceptable salts thereof with inorganic and organic acids with useful pharmacological properties, in particular, an inhibitory effect on signal transduction brought about by tyrosine kinases, the use thereof for the treatment of diseases, in particular of tumour diseases and benign prostatic hyperplasia (BPH), diseases of the lungs and airways and production thereof.Type: ApplicationFiled: August 3, 2006Publication date: September 16, 2010Inventors: Frank Himmelsbach, Birgit Jung
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Patent number: 7790732Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3 are as described in the specification and pharmaceutically acceptable acid addition salts and tautomers thereof. Compounds of formula I have good activity on the 5-HT5A receptor. Therefore, the invention provides a method for treating diseases related to this receptor, for example, anxiety, depression, sleep disorders and schizophrenia.Type: GrantFiled: June 21, 2006Date of Patent: September 7, 2010Assignee: Hoffman-La Roche Inc.Inventors: Alexander Alanine, Luca Claudio Gobbi, Sabine Kolczewski, Thomas Luebbers, Jens-Uwe Peters, Lucinda Steward
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Patent number: 7790733Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, and n are as described in the specification and pharmaceutically acceptable acid addition salts thereof. The compounds of formula I can be used for the treatment of 5-HT5A receptor antagonists related diseases, which include depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, disorders of eating behaviors, sexual dysfunction, sleep disorders, withdrawal from abuse of drugs, motor disorders such as Parkinson's disease, dementia in Parkinson's disease, neuroleptic-induced Parkinsonism and tardive dyskinesias, as well as other psychiatric disorders and gastrointestinal disorders such as irritable bowel syndrome.Type: GrantFiled: June 21, 2006Date of Patent: September 7, 2010Assignee: Hoffman-La Roche Inc.Inventors: Alexander Alanine, Luca Claudio Gobbi, Sabine Kolczewski, Thomas Luebbers, Jens-Uwe Peters, Lucinda Steward
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Publication number: 20100222371Abstract: The present invention relates to methods for treatment (particularly the prevention or suppression) of formation or reformation of adhesions, particularly in the peritoneal or pelvic cavities resulting from wound, surgery, infection, inflammation or trauma. The invention provides methods useful for inhibiting, suppressing or ameliorating adhesion formation in mammals, including humans wherein an individual is administered a compound selected from the group consisting of sunitinib malate, axitinib, semaxanib, sorafenib, ZD1839, and erlotinib. The invention applies to human and veterinary applications. The inventive method has been shown to be especially effective in preventing adhesion formation in the peritoneum following surgery.Type: ApplicationFiled: November 18, 2009Publication date: September 2, 2010Applicant: CHILDREN'S MEDICAL CENTER CORPORATIONInventors: Mark Puder, Arin K. Greene