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: 20090076022Abstract: The present invention relates to tartrate salts of quinazoline containing zinc-binding moiety based derivatives that are 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 tartrate salts may further act as HDAC inhibitors.Type: ApplicationFiled: September 10, 2008Publication date: March 19, 2009Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
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Publication number: 20090076042Abstract: The present application describes deuterium-enriched erlotinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 22, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Patent number: 7504409Abstract: The claimed invention relates to methods of modulating mucin synthesis and the therapeutic application of compounds in controlling mucin over-production associated with diseases such as chronic obstructive pulmonary diseases (COPD) including asthma and chronic bronchitis, inflammatory lung diseases, cystic fibrosis and acute or chronic respiratory infectious diseases.Type: GrantFiled: May 5, 2004Date of Patent: March 17, 2009Assignee: Genaera CorporationInventors: Yuhong Zhou, Roy C. Levitt, Nicholas C. Nicolaides, Steve Jones, Mike McLane
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Publication number: 20090069350Abstract: The present invention relates to pharmaceutical compositions and dosage compositions of compounds, including injectable formulations for the parenteral delivery of such compounds into patients in need of such treatment. Also featured are methods of making and using the compositions, including methods for the treatment of neoplastic diseases.Type: ApplicationFiled: November 17, 2008Publication date: March 12, 2009Applicant: Myriad Genetics, IncorporatedInventors: Gaylen M. Zentner, Chung Shih, James C. McRea
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Publication number: 20090069320Abstract: Substituted 4-amino-quinazoline compounds corresponding to formula I methods for their production, pharmaceutical compositions containing these compounds as active agents, and the uses thereof for treating or inhibiting disorders or disease states.Type: ApplicationFiled: September 15, 2008Publication date: March 12, 2009Applicant: Gruenenthal GmbHInventors: Melanie REICH, Stefan Oberboersch, Sven Kuehnert, Michael Haurand, Klaus Schiene
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Patent number: 7498335Abstract: The invention concerns the use of a quinazoline derivative of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2 and R3 is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human.Type: GrantFiled: March 1, 2001Date of Patent: March 3, 2009Assignee: AstraZeneca ABInventors: Laurent Francois Andre Hennequin, Graham Charles Crawley, Darren McKerrecher, Patrick Ple, Jeffrey Philip Poyser, Christine Marie Paul Lambert
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Publication number: 20090047278Abstract: The present invention relates to a pharmaceutical composition, a kit and a method for treating cancer, comprising a sulfonamide compound in combination with a substance having an EGF inhibitory activity.Type: ApplicationFiled: February 28, 2006Publication date: February 19, 2009Applicant: Eisai R & D Management Co., Ltd.Inventors: Takashi Owa, Yoichi Ozawa, Taro Semba, Toshiaki Wakabayashi
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Publication number: 20090048278Abstract: This invention relates to novel quinazoline-2,4-diamine derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: December 6, 2006Publication date: February 19, 2009Inventors: Ulrik Svane Sorensen, Birgitte L. Eriksen, Lene Teuber, Dan Peters, Dorte Strobaek, Tina Holm Johansen, Palle Christophersen
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Publication number: 20090048265Abstract: Antitumor compounds based on the ?1-adrenoceptor antagonist, doxazosin, as well as compositions and methods of use. The disclosed compounds induce apoptosis in cancer cells.Type: ApplicationFiled: June 17, 2005Publication date: February 19, 2009Applicant: THE OHIO STATE UNIVERSITY RESEARCH FOUNDATIONInventors: Ching-Shih Chen, Yeng-Jeng Shaw
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Publication number: 20090048279Abstract: This invention provides quinazoline analogs of Formula I: where A is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to two independent R3 groups. The invention also includes methods of using compounds of Formula I as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.Type: ApplicationFiled: October 10, 2008Publication date: February 19, 2009Applicant: ARRAY BIOPHARMA INC.Inventors: Eli Wallace, George Topalov, Joseph Lyssikatos, Alexandre Buckmelter, Qian Zhao
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Patent number: 7488823Abstract: 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: November 10, 2003Date of Patent: February 10, 2009Assignee: Array Biopharma, Inc.Inventors: Eli Wallace, George Topolov, Qian Zhao, Joseph P. Lyssikatos
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Publication number: 20090028868Abstract: Method of treating persons having carcinoma, sarcoma or hematopoietic cancer by administering (i) a compound of the formula (I) and (ii) an epidermal growth factor receptor (EGFR) inhibitor, a vascular endothelial growth factor receptor (VEGFR) inhibitor and pharmaceutical compositions for use in said method. A method for treating gastric cancer, colon cancer, lung cancer, breast cancer, pancreas cancer, kidney cancer, prostate cancer, medulloblastoma, rhabdomyosarcoma, Ewing sarcoma, liposarcoma, multiple myeloma and leukemia by administering a compound of the formula (I).Type: ApplicationFiled: July 30, 2008Publication date: January 29, 2009Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kosaku Fujiwara, Naomi Shimazaki
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Publication number: 20090030021Abstract: 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: ApplicationFiled: June 16, 2008Publication date: January 29, 2009Applicant: Rexahn Pharmaceuticals, Inc.Inventors: Young B. Lee, Chang H. Ahn
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Publication number: 20090017024Abstract: 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: July 11, 2008Publication date: January 15, 2009Applicant: Tragara Pharmaceuticals, Inc.Inventors: Thomas M. Estok, Sara L. Zaknoen, Robert K. Mansfield, Tracy Lawhon
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Publication number: 20090004185Abstract: The present invention relates to amino-substituted quinazoline derivatives as inhibitors of ?-catenin/tcf-4 pathway, which can be useful in the treatment of cancer; to processes for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.Type: ApplicationFiled: January 10, 2008Publication date: January 1, 2009Applicant: WYETHInventors: Aranapakam M. VENKATESAN, Christoph DEHNHARDT, Zecheng CHEN, Osvaldo Dos SANTOS, Efren Delos SANTOS, Kevin CURRAN, Semiramis AYRAL-KALOUSTIAN, Lei CHEN
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Publication number: 20080318959Abstract: The present invention describes novel methods of identifying compounds which inhibit HIV particle formation and Rev-dependent HIV production. The present invention also provides methods and compounds for inhibiting HIV particle formation and or treating patients infected with HIV.Type: ApplicationFiled: February 1, 2005Publication date: December 25, 2008Inventors: David Rekosh, Marie-Louise Hammarskjold
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Publication number: 20080312260Abstract: The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with inhibitors of EGFR kinase, PDGFR kinase, or FGFR kinase. Based on the surprising discovery that tumors cells after having undergone an EMT, while being mesenchymal-like, still express characteristics of both epithelial and mesenchymal cells, and that such cells have altered sensitivity to inhibition by receptor protein-tyrosine kinase inhibitors, in that they have become relatively insensitive to EGFR kinase inhibitors, but have frequently acquired sensitivity to inhibitors of other receptor protein-tyrosine kinases such as PDGFR or FGFR, methods have been devised for determining levels of specific epithelial and mesenchymal biomarkers that identify such “hybrid” tumor cells (e.g. determination of co-expression of vimentin and epithelial keratins), and thus predict the tumor's likely sensitivity to inhibitors of EGFR kinase, PDGFR kinase, or FGFR kinase.Type: ApplicationFiled: April 14, 2008Publication date: December 18, 2008Inventors: John D. Haley, Stuart Thomson
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Patent number: 7465738Abstract: The present invention relates to compounds useful as promoters of the SMN2 gene. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of Spinal Muscular Atrophy.Type: GrantFiled: June 16, 2004Date of Patent: December 16, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jill Jarecki, Xiaocun Chen, Dennis James Hurley, Lewis R. Makings, Mark T. Miller, Brian Pollok, Jeffrey H. Stack, Michael A. Whitney
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Publication number: 20080306093Abstract: The present invention provides screening methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors as well as modifiers capable of modulating chemosensory receptors and their ligands.Type: ApplicationFiled: June 8, 2007Publication date: December 11, 2008Applicant: SENOMYX, INC.Inventors: Guy Servant, Xiaodong Li, Feng Zhang, Haitian Liu, Catherine Tachdjian, Xiao-Qing Tang, Sara Werner, Marketa Rinnova, Qing Chen, Albert Zlotnik, Mark Zoller, Boris Klebansky, Richard Fine, Xinshan Kang
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Publication number: 20080306096Abstract: The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.Type: ApplicationFiled: December 19, 2006Publication date: December 11, 2008Applicant: ASTRAZENECA ABInventors: Brian Aquila, Jayachandran Ezhuthachan, Paul Lyne, Timothy Pontz, Xiaolan Zheng
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Publication number: 20080300248Abstract: The present invention has disclosed a compound of formula I and a pharmaceutically acceptable salt or a solvate thereof, wherein the substituents are as defined in the description. The invention has also disclosed a method for preparing the compound of formula I, the pharmaceutical compositions comprising the same and their uses in the preparation of an anti-tumor medicament.Type: ApplicationFiled: October 20, 2006Publication date: December 4, 2008Applicant: SHANGHAI ALLIST PHARMACEUTICALS, INC.Inventors: Jianhui Guo, Meng Wang, Yong Jiang, Xiaofang Zhang
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Publication number: 20080293709Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: November 13, 2006Publication date: November 27, 2008Applicant: AstraZeneca ABInventors: Jeffrey Albert, Gianni Chessari, Miles Stuart Congreve, Phil Edwards, Christopher Murray, Sahil Patel, Mark Sylvester
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Patent number: 7456189Abstract: Compounds of the formula having an inhibitory action on the signal transduction mediated by tyrosine kinases, and being useful for the treatment of oncoses and of benign prostate hyperplasia (BPH), of diseases of the lung and of the airways. Exemplary compounds are: (R)-4-(1-Phenylethylamino)-6-[1-(tert-butyloxycarbonyl)piperidin-4-yloxy]-7-methoxy-quinazoline and (R)-4-(1-Phenylethylamino)-6-(piperidin-4-yloxy)-7-methoxyquinazoline dihydrochloride.Type: GrantFiled: September 23, 2004Date of Patent: November 25, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Birgit Jung
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Publication number: 20080287474Abstract: The present invention is related to a novel series of pyrimidyl or fused pyrimidyl hydrazones. Compounds of Formula (I) wherein A is selected from the group consisting of Formulas (A1), (A2), (A3), (A4), (A5) are useful for the treatment and/or prevention of a proliferative disease.Type: ApplicationFiled: December 8, 2006Publication date: November 20, 2008Applicant: LABORATOIRES SERONO SAInventors: Brian Healey, Zhong Zhao, Amanda Sutton, Matthias Schwarz
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Patent number: 7452912Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: December 11, 2002Date of Patent: November 18, 2008Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Francine S. Grant, Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett
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Publication number: 20080267905Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of a selective cytokine inhibitory drug alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of a selective cytokine inhibitory drug. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: ApplicationFiled: May 5, 2004Publication date: October 30, 2008Applicant: CELGENE CORPORATIONInventor: Jerome B. Zeldis
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Publication number: 20080269262Abstract: 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: May 23, 2005Publication date: October 30, 2008Inventor: Gerard M. Housey
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Publication number: 20080249117Abstract: The invention relates to a cosmetic composition containing at least one 15-hydroxy-prostaglandin dehydrogenase inhibitor and cosmetically acceptable excipients. It also relates to a method of cosmetic treatment for promoting the growth and/or preventing or delaying the loss of hair, and the use of a 15-hydroxyprostaglandin dehydrogenase inhibitor for the preparation of a composition intended for controlling hair loss and/or for promoting hair regrowth.Type: ApplicationFiled: November 15, 2007Publication date: October 9, 2008Applicant: SOCIETE LOREAL S.A.Inventors: Jean-Francois MICHELET, Bruno Bernard, Roger Rozot, Christophe Boulle
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Patent number: 7432275Abstract: Acid-substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: GrantFiled: December 12, 2003Date of Patent: October 7, 2008Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Charles A. Blum, Harry Brielmann, Timothy M. Caldwell, Stéphane DeLombaert, Kevin J. Hodgetts, Xiaozhang Zheng
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Publication number: 20080241274Abstract: 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 27, 2007Publication date: October 2, 2008Applicant: ZIOPHARM Oncology, Inc.Inventors: Barbara P. Wallner, Brian Eric Schwartz, Philip B. Komarnitsky, Gerald Bacher, Bernhard Kutscher, Gerhard Raab
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Patent number: 7429597Abstract: The present invention relates to new substituted nitrogen-containing heterobicyclic compounds of general formula wherein B, X1 to X3 and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties. The compounds of the above general formula I as well as the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, and their stereoisomers have valuable pharmacological properties, particularly an antithrombotic activity and a factor Xa-inhibiting activity.Type: GrantFiled: December 18, 2003Date of Patent: September 30, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co., KGInventors: Henning Priepke, Roland Pfau, Kai Gerlach, Uwe Ries, Wolfgang Wienen, Eckhart Bauer, Herbert Nar
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Publication number: 20080234265Abstract: Disclosed is the use of a combination of histone deacetylase inhibitors and epidermal growth factor receptor (EGFR) inhibitors to treat cancer.Type: ApplicationFiled: March 13, 2006Publication date: September 25, 2008Applicant: THE REGENTS OF THE UNIVERSITY OF COLORADOInventors: Samir E. Witta, Paul A. Bunn, Harry A. Drabkin, Robert M. Gemmill, Daniel Chuen-Fong Chan
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Publication number: 20080234264Abstract: The present invention is directed to a method for determining the responsiveness of cancer to an epidermal growth factor receptor (EGFR) treatment. In a preferred embodiment, the presence of at least one variance in the kinase domain of the erbB1 gene confers sensitivity to the tyrosine kinase inhibitor gefitinib. Thus, a diagnostic assay for these mutations will allow for the administration of gefitinib, erlotinib and other tyrosine kinase inhibitors to those patients most likely to respond to the drug.Type: ApplicationFiled: August 20, 2007Publication date: September 25, 2008Applicants: The General Hospital Corporation, Dana Farber Cancer Institute, Inc.Inventors: Daphne Winifred Bell, Daniel A. Haber, Pasi Antero Janne, Bruce E. Johnston, Thomas J. Lynch, Matthew Meyerson, Juan Guillermo Paez, William R. Sellers, Jeffrey E. Settleman, Raffaella Sordella
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Publication number: 20080221138Abstract: The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor such as suberoylanilide hydroxamic acid (SAHA), or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of one or more anti-cancer agents, including Erlotinib. The HDAC inhibitor and the anti-cancer agent may be administered to comprise therapeutically effective amounts. In various aspects, the effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.Type: ApplicationFiled: May 2, 2008Publication date: September 11, 2008Inventors: Paul Bunn, Samir Witta, Victoria M. Richon, Stanley R. Frankel, Paul J. Deutsch, Sophia Randolph
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Publication number: 20080214586Abstract: Novel phenylquinazoline derivatives of the formula (I), in which R1, R2, R3, R4 and R5 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: April 24, 2006Publication date: September 4, 2008Inventors: Hans-Michael Eggenweiler, Michael Wolf, Hans-Peter Buchstaller
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Publication number: 20080213399Abstract: The present invention pertains to a method for treating cancer, such as lung cancer, multiple myeloma, lymphoma, and epithelial ovarian cancer, comprising the administration to a patient in need thereof a first amount or dose of a histone deacetylase (HDAC) inhibitor, such as PXD-101, and a second amount or dose of another chemotherapeutic agent, such as dexamethasone or 5-fluorouracil, or an epidermal growth factor receptor (EGFR) inhibitor, such as TarcevaÚ, wherein the first and second amounts or doses together comprise a therapeutically effective amount.Type: ApplicationFiled: February 3, 2006Publication date: September 4, 2008Applicants: TOPOTARGET UK LIMITED, CURAGEN CORPORATIONInventors: Henri Lichenstein, Mike Jeffers, Xiaozhang Qian, Maxwell Sehested, Kamille Dumong Petersen, James Ritchie
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Publication number: 20080207615Abstract: The present invention is directed to a method for determining the responsiveness of cancer to an epidermal growth factor receptor (EGFR) treatment. In a preferred embodiment, the presence of at least one variance in the kinase domain of the erbB1 gene confers sensitivity to the tyrosine kinase inhibitor gefitinib. Thus, a diagnostic assay for these mutations will allow for the administration of gefitinib, erlotinib and other tyrosine kinase inhibitors to those patients most likely to respond to the drug.Type: ApplicationFiled: August 20, 2007Publication date: August 28, 2008Applicants: The General Hospital Corporation, Dana Farber Cancer Institute, Inc.Inventors: Daphne Winifred Bell, Daniel A. Haber, Pasi Antero Janne, Bruce E. Johnston, Thomas J. Lynch, Matthew Meyerson, Juan Guillermo Paez, William R. Sellers, Jeffrey E. Settleman, Raffaella Sordella
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Publication number: 20080206320Abstract: The invention relates to a cosmetic composition containing at least one 15-hydroxy-prostaglandin dehydrogenase inhibitor and cosmetically acceptable excipients. It also relates to a method of cosmetic treatment for promoting the growth and/or preventing or delaying the loss of hair, and the use of a 15-hydroxyprostaglandin dehydrogenase inhibitor for the preparation of a composition intended for controlling hair loss and/or for promoting hair regrowth.Type: ApplicationFiled: November 15, 2007Publication date: August 28, 2008Applicant: SOCIETE L'OREAL S.A.Inventors: Jean-Francois MICHELET, Bruno Bernard, Roger Rozot, Christophe Boulle
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Publication number: 20080207563Abstract: Disclosed are methods for synergistically inhibiting the proliferation of tumor cells by contacting the tumor cells with a MEK inhibitor compound and erlotinib, either sequentially or simultaneously. Also disclosed are methods for inhibiting the proliferation of tumor cells in a human, by administering to the human, sequentially or simultaneously, an amount of erlotinib and a MEK inhibitor compound, wherein the amounts are effective, in combination, to synergistically inhibit the proliferation of the tumor cells in the human.Type: ApplicationFiled: February 21, 2008Publication date: August 28, 2008Inventor: Huifeng Niu
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Publication number: 20080193448Abstract: The invention provides methods of treating cancer using a compound of formula (1) or a pharmaceutically acceptable salt thereof, particularly a malate salt, in combination with various additional therapeutic agents. The invention also provides therapeutic dosing regimens, using the compound of formula (1) and an additional therapeutic agent.Type: ApplicationFiled: May 4, 2006Publication date: August 14, 2008Applicant: PFIZER INC.Inventor: Charles M. Baum
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Publication number: 20080194578Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives that 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: September 10, 2007Publication date: August 14, 2008Inventors: Changgeng Qian, Xiong Cai, Stephen Gould, Haixiao Zhai
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Publication number: 20080194596Abstract: This invention relates to a method of treatment of cancer with a combination of an additional therapeutic agent in mammals. This invention also relates to a kit useful in the treatment of abnormal cell growth in mammals, especially humans.Type: ApplicationFiled: May 22, 2006Publication date: August 14, 2008Inventor: Stephen Paul Letrent
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Publication number: 20080194558Abstract: This invention concerns quinazoline analogs of Formula I: where an A group is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to three independent R3 groups. The invention also includes methods of using these compounds as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.Type: ApplicationFiled: April 21, 2008Publication date: August 14, 2008Applicant: ARRAY BIOPHARM, INC.Inventors: Eli Wallace, George Topalov, Joseph Lyssikatos, Alexandre Buckmelter, Qian Zhao
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Patent number: 7410975Abstract: The invention provides methods and compositions useful for modulating signaling through Toll-like receptors. The methods involve contacting a TLR-expressing cell with a small molecule having a core structure including at least two rings. Certain of the compounds are 4-primary amino quinolines. Many of the compounds and methods are useful specifically for inhibiting immune stimulation involving at least one of TLR9, TLR8, TLR7, and TLR3. The methods may have use in the treatment of autoimmunity, inflammation, allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer, and immunodeficiency.Type: GrantFiled: June 18, 2004Date of Patent: August 12, 2008Assignees: Coley Pharmaceutical Group, Inc., Coley Pharmaceutical GmbHInventors: Grayson B. Lipford, Alexandra Forsbach, Charles Zepp
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Publication number: 20080188499Abstract: The present invention relates to compounds of the formula (1.0); and pharmaceutically acceptable salts of such compounds. The present invention relates to chemical entities containing a nitrofuran or other antibiotic linked to an activity enhancing distal ring system either directly or via an imine group, the vinyl group, the carbo- or hetero-cyclic chain or ring or a combination of an imine group or a vinyl group and a carbo- or hetero-cyclic chain or ring. Antibiotic activity is obtained, for example, by the nitrofuran moiety, while the remaining structure of the molecule contributes to additional antimicrobial activity and/or extends the antimicrobial spectrum of activity, by facilitating nitroreduction by microorganisms, uptake in target bacterial, and/or intracellular penetration, while also contributing to pharmacological properties (absorption, body distribution, and others).Type: ApplicationFiled: September 22, 2005Publication date: August 7, 2008Applicant: ULYSSES PHARMACEUTICAL PRODUCTS INC.Inventors: Suzanne Chamberland, Francois Malouin
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Publication number: 20080175797Abstract: Hypersecretion of mucus in the lungs is inhibited by the administration of an epidermal growth factor receptor (EGF-R) antagonist. The EGF-R antagonist may be in the form of a small organic molecule, an antibody, or portion of an antibody that binds to and blocks the EGF receptor. The EGF-R antagonist is preferably administered by injection in an amount sufficient to inhibit formation of goblet cells in pulmonary airways. The degranulation of goblet cells that results in airway mucus production is thereby inhibited. Assays for screening candidate agents that inhibit goblet cell proliferation are also provided.Type: ApplicationFiled: February 27, 2008Publication date: July 24, 2008Inventors: Jay A. Nadel, Kiyoshi Takeyama
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Publication number: 20080176875Abstract: This invention relates to the discovery of prodrugs of 3- or 5-substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting the formation of blood platelets.Type: ApplicationFiled: November 28, 2007Publication date: July 24, 2008Applicant: SHIRE LLCInventors: Richard Franklin, Bernard T. Golding, Peter A. Cicala
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Publication number: 20080167327Abstract: Erlotinib hydrochloride hydrate is formed from an aqueous solution and is useful as a pharmaceutical and as a purification intermediate.Type: ApplicationFiled: October 25, 2007Publication date: July 10, 2008Inventor: Raymond J. H. Westheim
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Publication number: 20080167328Abstract: The present invention relates to quinazoline derivatives of formula I: wherein X, Y, Z, R1, R2, R3, and R4 are as defined herein. The invention also relates to a method of preparing these compounds, and use of these compounds for inhibiting tumor growth.Type: ApplicationFiled: November 13, 2007Publication date: July 10, 2008Inventors: Wenlin Huang, Xiaohong Zhou
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Publication number: 20080166358Abstract: 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: December 15, 2007Publication date: July 10, 2008Applicant: Concert Pharmaceuticals Inc.Inventor: Roger Tung