Nitrogen Bonded Directly At 4-position Patents (Class 544/293)
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Publication number: 20100009958Abstract: 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: June 30, 2008Publication date: January 14, 2010Applicant: Hutchison MediPharma Enterprises LimitedInventors: Weihan Zhang, Wei-Guo Su, Haibin Yang, Yumin Cui, Yongxin Ren, Xiaoqiang Yan
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Publication number: 20100010023Abstract: A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetra-hydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetra-hydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transductionType: ApplicationFiled: September 21, 2009Publication date: January 14, 2010Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KGInventors: Frank HIMMELSBACH, Elke LANGKOPF, Stefan BLECH, Birgit JUNG, Anke BAUM, Flavio SOLCA
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Publication number: 20100004449Abstract: The preparation of crystalline Erlotinib base form G2 is described. This crystalline form can be converted to an Erlotinib salt, such as Erlotinib HCl, which can be used in the treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC).Type: ApplicationFiled: July 7, 2009Publication date: January 7, 2010Applicant: PLUS CHEMICALS SAInventors: Ales GAVENDA, Pavel VRASPIR, Augusto CANAVESI, Judith ARONHIME, Ettore BIGATTI, Jiri FAUSTMANN, Alexandr JEGOROV, Peter W. STEPHENS, Giovanna LUX, Maurizio PAIOCCHI
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Publication number: 20090318479Abstract: The present invention relates to substituted ring fused azines and methods of using said compounds in treating cancers. More specifically, the present invention relates to the preparation of 4-alkyl-2-(heterocyclic)-azines and their use as cancer agents or drugs for cancer therapy. The compounds of the invention display favourable in vivo and in vitro activity against selected cancers.Type: ApplicationFiled: April 4, 2007Publication date: December 24, 2009Inventors: William Alexander Denny, Bruce Charles Baguley, Elaine Shirley Marshall, Hamish Scott Sutherland
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Publication number: 20090318373Abstract: The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.Type: ApplicationFiled: June 8, 2009Publication date: December 24, 2009Inventors: Kenneth D. Rice, Neel K. Anand, Joerg Bussenius, Simona Costanzo, Abigail R. Kennedy, Csaba J. Peto, Tsze H. Tsang, Charles M. Blazey
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Publication number: 20090312305Abstract: A compound represented by the structural formula: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: May 18, 2009Publication date: December 17, 2009Applicant: ALLERGAN, INC.Inventors: Richard L. Beard, Tien T. Duong, Thong H. Vu, Vidyasagar Voligonda, John E. Donello, Michael E. Garst, Gerard A. Rodrigues
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Publication number: 20090312343Abstract: The invention concerns quinazoline derivatives of the Formula I: wherein each of R1, R2, W, X1, X2, Z, a and b are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula I are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, particularly EGFR tyrosine kinase.Type: ApplicationFiled: June 11, 2009Publication date: December 17, 2009Inventors: Laurent Francois Andre HENNEQUIN, Christopher Thomas Halsall
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Publication number: 20090306378Abstract: The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) wherein the groups Ra, Rb, Rc and Rd have the meanings given in the claims, as well as sulphonyl derivatives of formula (XIII) and the use thereof as synthesis components for preparing quinazolines of formula (I). The quinazoline derivatives of formula (I) are inhibitors of signal transduction mediated by tyrosinekinases and by the Epidermal Growth Factor-Receptor (EGF-R) and are therefore particularly suitable for the treatment of tumoral diseases.Type: ApplicationFiled: January 25, 2007Publication date: December 10, 2009Inventors: Juergen Schroeder, Georg Dziewas, Thomas Fachinger, Burkhard Jaeger, Carsten Reichel, Svenja Renner
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Publication number: 20090306044Abstract: The present invention relates to the use of quinazolines of formula (I), wherein the groups Ra to Rd have the meanings given in the claims and specification, in cancer therapy.Type: ApplicationFiled: November 9, 2006Publication date: December 10, 2009Inventors: Flavio Solca, Andree Amelsberg, Gerd Stehle, Jacobus C.A. Van Meel, Anke Baum
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Publication number: 20090306105Abstract: The present invention relates to bicyclic heterocycles of the general formula (I), their tautomers, their stereoisomers, their mixtures and their salts, in particular physiologically tolerable salts with inorganic or organic acids, which have valuable pharmacological properties, in particular an inhibiting action on the signal transduction transmitted by tyrosinekinases, their use for the treatment of illnesses, in particular tumours and also benign prostatic hyperplasia (BPH), of disorders of the lungs and the bronchia and their preparation.Type: ApplicationFiled: February 20, 2007Publication date: December 10, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank Himmelsbach, Birgit Jung
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Publication number: 20090306377Abstract: The present invention discloses an improved and novel process for the preparation of erlotinib (N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine) of formula (1), which comprises: (i) demethylation of commercially available 6,7-dimethoxy-4(3H)-quinazolinone of formula (8); acetylation using acetic anhydride; (iii) introduction of a leaving group at C-4 position in quinazolinone; (iv) condensation with 3-ethynylaniline to get novel compound of formula (12); (v) deacetylation to get novel dihydroxy compound of formula (13); and (vi) O-alkylation with 2-iodoethylmethyl ether to get the erlotinib base of formula (1). Erlotinib base is purified by recrystallization from ethyl acetate to get a HPLC purity of >99.5%. Salt formation of this base with hydrogen chloride gave pharmaceutically acceptable erlotinib hydrochloride of formula (1a) with a HPLC purity of >99.8%. Erlotinib hydrochloride is useful for the treatment of proliferative disorders, such as cancers, in humans.Type: ApplicationFiled: November 22, 2006Publication date: December 10, 2009Applicant: Natco Pharma LimitedInventors: Ramanadham Jyothi Prasad, Bollepalli Nageshwar Rao, Nannapaneni Venkaiah Chowdary
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Publication number: 20090306106Abstract: The present invention provides new crystalline forms of lapatinib base, Form X and Form Y, and amorphous lapatinib base, pharmaceutical compositions comprising the new crystalline forms of lapatinib base, and/or the amorphous lapatinib base, and processes for their preparation.Type: ApplicationFiled: May 7, 2009Publication date: December 10, 2009Inventors: Leonid METSGER, Ariel MITTELMAN, Slavik YURKOVSKI
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Patent number: 7625911Abstract: The present invention relates to novel amorphous form of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl) (erlotinib hydrochloride), to solid amorphous dispersion of erlotinib hydrochloride and a carrier such as PVP or solid PEG, to processes for their preparations, to pharmaceutical compositions containing them and to method of treatment using the same. The amorphous form or solid amorphous dispersion of erlotinib hydrochloride obtained in this invention is useful in preparing pharmaceutical dosage forms.Type: GrantFiled: January 12, 2005Date of Patent: December 1, 2009Assignee: Mai De Ltd.Inventor: Le Huang
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Patent number: 7625908Abstract: 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: November 11, 2004Date of Patent: December 1, 2009Assignee: AstraZeneca ABInventors: Laurent Francois Andre Hennequin, Robert Hugh Bradbury, Jason Grant Kettle
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Publication number: 20090291950Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PD E4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.Type: ApplicationFiled: July 6, 2007Publication date: November 26, 2009Applicant: KALYPSYS, INC.Inventors: Steven P. Govek, Andrew K. Shiau, Stewart A. Noble, David J. Thomas
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Publication number: 20090286982Abstract: 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline difumarate, pharmaceutical compositions containing the difumarate, the use of the difumarate in the treatment of hyperproliferative disorders such as cancer and processes for the manufacture of the difumarate are described.Type: ApplicationFiled: May 11, 2009Publication date: November 19, 2009Applicant: ASTRAZENECA ABInventor: Andrew Hornby Dobson
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Patent number: 7618975Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof 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: GrantFiled: July 6, 2004Date of Patent: November 17, 2009Assignees: Myriad Pharmaceuticals, Inc., Cytovia, Inc.Inventors: Sui Xiong Cai, Nilantha Sudath Sirisoma, Azra Pervin, John A. Drewe, Shailaja Kasibhatla, Songchun Jiang, Hong Zhang, Chris Pleiman
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Publication number: 20090281315Abstract: The present invention provides novel polymorphs of lapatinib ditosylate, processes for preparing them, and pharmaceutical compositions comprising one or more of these polymorphs.Type: ApplicationFiled: May 7, 2009Publication date: November 12, 2009Inventors: Leonid METSGER, Ariel MITTELMAN, Slavik YURKOVSKI
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Publication number: 20090269354Abstract: 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: March 27, 2009Publication date: October 29, 2009Applicant: Concert Pharmaceuticals, Inc.Inventors: Craig E. Masse, Roger Tung
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Publication number: 20090270621Abstract: 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: July 2, 2009Publication date: October 29, 2009Applicant: ARRAY BIOPHARMA, INC.Inventors: Eli Wallace, George Topalov, Joseph Lyssikatos, Alexandre Buckmelter, Qian Zhao
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Publication number: 20090247519Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain amino-ethyl-amino-aryl (AEAA) compounds which, inter alia, inhibit protein kinase D (PKD) (e.g., PKD1, PKD2, PKD3). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PKD, and in the treatment of diseases and conditions that are mediated by PKD, that are ameliorated by the inhibition of PKD, etc., including proliferative conditions such as cancer, etc.Type: ApplicationFiled: April 26, 2007Publication date: October 1, 2009Inventors: Tony Michael Raynham, Timothy Robin Hammonds, Julia Helen Gilliatt, Mark David Charles, Gregoire Alexandre Pave, Caroline Heather Foxton, James Lindsay Carr, Neela Sumit Mistry
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Publication number: 20090226377Abstract: The present invention relates to a quinoline or quinazoline derivative having the general formula (A): in which R3, R4, W, Y and Q are indicated in the description and the claims, the use of the compounds of the general formula (A) for the treatment of various disorders, and the preparation of compounds of the general formula (A).Type: ApplicationFiled: May 23, 2008Publication date: September 10, 2009Inventors: Knut EIS, Olaf Prien, Ulrich Lucking, Judith Gunther, Dieter Zopf, Dirk Brohm, Verena Vohringer, Elisabeth Woltering, Hartmut Beck, Mario Lobell, Volkhart Min-Jian Li, Susanne Greschat
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Patent number: 7585869Abstract: The invention relates to compounds of formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R3, R4, R11, N, Z, A, m and p are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.Type: GrantFiled: May 20, 2004Date of Patent: September 8, 2009Assignee: Pfizer, Inc.Inventors: Samit Kumar Bhattacharya, Jinshan Chen, Richard Damian Connell, John Charles Kath, Goss S. Kauffman, Blaise S. Lippa, Joel Morris
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Publication number: 20090221614Abstract: Inhibition of protein kinases having one or more cysteine residues within the ATP binding site is effected by contacting the kinase, per se or in a cell or subject, with an inhibitory-effective amount of a compound having a heterocyclic core structure comprised of two or more fused rings containing at least one nitrogen ring atom, and an electrophilic substituent that is capable of reacting with a cysteine residue within the ATP binding site of a kinase. Preferred compounds include certain pyrrolopyrimidines and oxindoles having such an electrophilic substituent and optionally an aromatic or heteroaromatic substituent that is capable of interacting with a threonine or smaller residue located in the gatekeeper position of the kinase. Kinases lacking such cysteine residues may be engineered or modified so that they are capable of being inhibited by such compounds by replacing a valine or other amino acid residue within the ATP binding site by a cysteine residue.Type: ApplicationFiled: September 26, 2006Publication date: September 3, 2009Applicant: The Regents of the University of CaliforniaInventors: Jack Taunton, Michael Cohen, Kevin Shokat, Chao Zhang
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Publication number: 20090215802Abstract: The present application describes deuterium-enriched lapatinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 22, 2008Publication date: August 27, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090209758Abstract: 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: April 14, 2009Publication date: August 20, 2009Inventors: Changgeng Qian, Xiong Cai, Stephen Gould
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Patent number: 7576074Abstract: The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.Type: GrantFiled: July 14, 2003Date of Patent: August 18, 2009Inventors: Kenneth D. Rice, Neel K. Anand, Joerg Bussenius, Abigail R. Kennedy, Angie I. Kim, Csaba J. Peto, Tsze H. Tsang
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Publication number: 20090203905Abstract: The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline.Type: ApplicationFiled: September 27, 2006Publication date: August 13, 2009Inventors: Jorgen Blixt, Michael David Golden, Philip John Hogan, David Michael Glanville Martin, Francis Joeph Montgomery, Zakariya Patel, John David Pittam, George Joseph Sependa, Christopher John Squire, Nicholas Cartwright Alexander Wright
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Patent number: 7572798Abstract: The present invention relates to a series of new chemical agents that demonstrate anti-tumor activity. More particularly, the present invention relates to molecules, referred to as “combi-molecules”, that combine two major mechanisms of anti-tumor action. A combi-molecule is capable of degrading to a ligand involved in cell signaling pathways and to an agent capable of damaging DNA. More specifically, the present invention relates to molecules capable of blocking epidermal growth factor receptor (EGFR) mediated signal transduction and capable of damaging DNA. The present invention also relates to a general method of synthesis of these combi-molecules.Type: GrantFiled: February 26, 2002Date of Patent: August 11, 2009Assignee: McGill UniversityInventors: Bertrand J. Jean-Claude, Fabienne Dudouit, Stephanie Matheson
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Publication number: 20090197884Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: ApplicationFiled: October 26, 2006Publication date: August 6, 2009Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventors: Shomir Ghosh, Prakash Raman, Kevin Sprott, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
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Patent number: 7569577Abstract: The invention concerns quinazoline derivatives of the Formula (I); wherein each of R1, R2, W, X1, X2, Z, a and b are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula (I) are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, particularly EGFR tyrosine kinase.Type: GrantFiled: September 13, 2004Date of Patent: August 4, 2009Assignee: Astrazeneca ABInventors: Laurent Francois Andre Hennequin, Christopher Thomas Halsall
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Publication number: 20090186911Abstract: 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: ApplicationFiled: June 13, 2008Publication date: July 23, 2009Inventors: Duy NGUYEN, Arne von Bonin, Michael Haerter, Hartmut Schirok, Anne Mengel, Martina Schaefer, Oliver von Ahsen
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Patent number: 7560558Abstract: The present invention provides compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein X represents CH or N; Z represents —O—, —NH— or —C(?O)—; R and R? represent a hydrogen atom, hydroxyl, a halogen atom, optionally substituted alkyl, optionally substituted alkenyl optionally substituted alkoxy, amino, aminocarbonyl, or an optionally substituted heterocyclic group; and A represents an optionally substituted specific carbocyclic or heterocyclic group. The compounds according to the present invention have excellent TGF? inhibitory activity.Type: GrantFiled: August 22, 2003Date of Patent: July 14, 2009Assignee: Kirin Beer Kabushiki KaishaInventors: Kiyoshi Shimizu, Toshiyuki Shimizu, Kaname Kimura, Kazuki Kawakami, Masayoshi Nakoji
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Publication number: 20090171083Abstract: A 4-aminoquinazoline derivative can be obtained by the steps of reacting quinazolin-4-one or its derivative with a chlorinating agent in a first organic solvent in the presence of an organic base, and subsequently reacting the reaction product with an amine compound represented by the formula R5—NH—R6 (each of R5 and R6 represents hydrogen or an optionally substituted hydrocarbyl group) in the presence of a second organic solvent.Type: ApplicationFiled: March 10, 2009Publication date: July 2, 2009Applicant: UBE INDUSTRIES, LTD.Inventors: Shigeyoshi NISHINO, Kenji HIROTSU, Hidetaka SHIMA, Takashi HARADA, Hiroyuki ODA
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Patent number: 7547781Abstract: 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: GrantFiled: September 10, 2007Date of Patent: June 16, 2009Assignee: Curis, Inc.Inventors: Changgeng Qian, Xiong Cai, Stephen Gould
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Patent number: 7547702Abstract: 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 1bIX antagonists.Type: GrantFiled: September 17, 2001Date of Patent: June 16, 2009Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Werner Mederski, Maria Devant, legal representative, Gerhard Barnickel, Sabine Bernotat-Danielowski, James Vickers, Bertram Cezanne, Daljit Dhanoa, Bao-Ping Zhao, James Rinker, Mark R. Player, Edward Jaegar, Richard Soll, Ralf Devant
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Publication number: 20090137567Abstract: Methods of treating blood disorders are described.Type: ApplicationFiled: September 17, 2008Publication date: May 28, 2009Applicant: HEMAQUEST PHARMACEUTICALS, INC.Inventors: Susan P. Perrine, Regine Bojacek
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Publication number: 20090131665Abstract: The invention provides processes for preparing crystalline Forms A, B and pure crystalline Form A of Erlotinib hydrochloride.Type: ApplicationFiled: August 25, 2008Publication date: May 21, 2009Inventors: Ales Gavenda, Jiri Faustmann, Augusto Canavesi, Dietmar Flubacher
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Publication number: 20090131666Abstract: [Problem] To provide a compound which has an excellent activity to modulate the functions of CCR4 or TARC and/or MDC and can be used for the prevention and/or treatment of various inflammatory diseases, allergic diseases, autoimmune diseases and the like. [Means for Resolution] An acylaminopiperidine compound represented by the formula (I) or a pharmaceutically acceptable salt thereof. [Symbols in the formula represent the following meanings; A: a single bond or C1-C6 alkylene, R1: phenyl which may be substituted, etc., R2: —H or C1-C6 alkyl, R3: —H, C1-C6 alkyl or C3-C8 cycloalkyl, R4: pyrrolidin-2-yl which may be substituted, etc., and D: benzene ring or pyrazole ring].Type: ApplicationFiled: March 23, 2007Publication date: May 21, 2009Applicant: ASTELLAS PHARMA INC.Inventors: Toru Kontani, Noriyuki Kawano, Naoyuki Masuda, Koji Kato, Hiroshi Nagata, Hiroshi Inami, Tadashi Terasaka, Kazuhiro Yokoyama, Takahiro Miyazaki
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Publication number: 20090124642Abstract: The invention provides a novel crystalline form of Erlotinib HCl, processes for its preparation, and formulations thereof.Type: ApplicationFiled: August 25, 2008Publication date: May 14, 2009Inventors: Augusto Canavesi, Marco Villa, Ales Gavenda, Jiri Faustmann, Judith Aronhime, Ettore Gibatti, Alexandr Jegorov
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Publication number: 20090111772Abstract: The present invention relates to a composition comprising an inclusion complex of a cyclodextrin and quinazoline containing zinc-binding moiety based derivatives. The cyclodextrin is preferable a ?-cyclodextrin or a derivative thereof. The quinazolines have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.Type: ApplicationFiled: September 10, 2008Publication date: April 30, 2009Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai, Rudi Bao
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Publication number: 20090105247Abstract: 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: December 23, 2008Publication date: April 23, 2009Inventor: Hesheng ZHANG
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Patent number: 7521456Abstract: The present invention relates to the anhydrous and hydrate forms of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate. The invention also relates to pharmaceutical compositions containing N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate and to methods of treating hyperproliferative disorders, such as cancer, by administering N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate.Type: GrantFiled: November 17, 2003Date of Patent: April 21, 2009Assignee: OSI Pharmaceuticals, Inc.Inventors: Douglas John Meldrum Allen, Timothy Norris, Jeffrey William Raggon, Dinos Paul Santafianos, Ravi Mysore Shanker
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Publication number: 20090099196Abstract: The present invention relates to chemical processes useful in the manufacture of the compound 4-(6-chloro-2,3-methylenedioxyanilino)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-tetrahydropyran-4-yloxyquinazoline (the active entity within AZD0530), to intermediates useful in the manufacture of that compound and to processes for the manufacture of those intermediates. The invention also relates to particular crystalline forms of that compound such as a difumarate salt and a trihydrate and to pharmaceutical compositions containing such crystalline forms.Type: ApplicationFiled: December 14, 2005Publication date: April 16, 2009Inventors: James Gair Ford, James Francis McCabe, Anne O'Kearney-McMullan, Simon Mark Pointon, Lyn Powell, Philip O'Keefe, Mark Purdie, Jane Withnall
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Patent number: 7507741Abstract: Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.Type: GrantFiled: August 1, 2007Date of Patent: March 24, 2009Assignee: SmithKline Beecham CorporationInventors: George Stuart Cockerill, Karen Elizabeth Lackey
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Publication number: 20090076044Abstract: The present invention relates to VEGFR inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The said derivatives may further act as HDAC inhibitors.Type: ApplicationFiled: September 10, 2008Publication date: March 19, 2009Inventors: Changgeng Qian, Xiong Cai, Haixiao Zhai
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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: 7504408Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein each of Z, m, R1, n, R3, Z2 and R14 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive or anti-proliferative agent in the containment and/or treatment of solid tumour disease.Type: GrantFiled: July 4, 2003Date of Patent: March 17, 2009Assignee: AstraZeneca ABInventors: Laurent Francois Andre Hennequin, Keith Hopkinson Gibson, Kevin Michael Foote
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Patent number: RE41065Abstract: The invention relates to compounds of the formula and to pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, n and m are as defined herein. The compounds of formula I are useful in the treatment of hyperproliferative diseases, such as cancer. The invention further relates to processes of making the compounds of formula I and to methods of using such compounds in the treatment of hyperproliferative diseases.Type: GrantFiled: February 27, 2008Date of Patent: December 29, 2009Assignees: Pfizer, Inc., OSI Pharmaceuticals, Inc.Inventors: Rodney Caughren Schnur, Lee Daniel Arnold