Nitrogen Bonded Directly At 4-position Patents (Class 544/293)
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Publication number: 20120046269Abstract: The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: February 4, 2010Publication date: February 23, 2012Applicant: Merck Patent GmbHInventors: Amanda E. Sutton, Ruoxi Lan, Thomas E. Richardson, David Perrey, Harold George Vandeveer, Bayard R. Huck, Srinivasa R. Karra, Xiaoling Chen, Lesley Liu-Bujalski, Andreas Goutopoulos, Frank Steiber, Brian L. Hodous, Hui Qiu, Reinaldo C. Jones, Brian H. Heasley
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Publication number: 20120046284Abstract: The present invention relates to a compound of formula (I), wherein x Q denotes x H2O x HCl; or x 0.5 HCl x 1.5 H2O, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, processes for the stereoselective preparation of this compound, particularly for the inhalation of suitable pharmaceutical formulations and their use for the treatment of diseases, particularly tumour diseases, benign prostatic hyperplasia and diseases of the lungs and airways.Type: ApplicationFiled: February 14, 2011Publication date: February 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Marc EGEN, Werner RALL, Marco SANTAGOSTINO, Juergen SCHNAUBELT, Peter SIEGER, Rainer SOYKA
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Publication number: 20120035363Abstract: 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: October 14, 2011Publication date: February 9, 2012Applicant: ASTRAZENECA ABInventor: Andrew Hornby Dobson
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Publication number: 20120022256Abstract: The present invention provides a novel and stable hydrated form of erlotinib free base, and a process for its preparation thereof. The present invention also provides a process for preparation of erlotinib hydrochloride crystalline polymorph a substantially free of polymorph B. The present invention further relates to erlotinib hydrochloride crystalline particles having mean particle size (D50) ranging from about 4 ?m to 15 ?m and 90 volume-% of the particles (D90) ranging from about 14 ?m to 30 ?m, to the methods for the manufacture of said crystalline particles, and to pharmaceutical compositions comprising said crystalline particles.Type: ApplicationFiled: August 31, 2011Publication date: January 26, 2012Applicant: HETERO DRUGS LIMITEDInventors: BANDI PARTHASARADHI REDDY, KURA RATHNAKAR REDDY, RAPOLU RAJI REDDY, DASARI MURALIDHARA REDDY, THUNGATHURTHY SRINIVASA RAO
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Publication number: 20120004249Abstract: The present invention relates to polymorphic forms of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazolin-6-yl}-acrylamide p-toluenesulfonate with the characteristic X-ray powder diffraction data as stated in the description, preparation methods thereof, pharmaceutical compositions comprising the same and the use thereof.Type: ApplicationFiled: March 25, 2009Publication date: January 5, 2012Inventors: Jianhui Guo, Yong Jiang
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Patent number: 8088782Abstract: 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline difumarate, pharmaceutical compositions containing the difumarate, the use of the difumarate in the treatment of hyperproliferative disorders such as cancer and processes for the manufacture of the difumarate are described.Type: GrantFiled: May 11, 2009Date of Patent: January 3, 2012Assignee: AstraZeneca ABInventor: Andrew Hornby Dobson
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Patent number: 8088766Abstract: Cyanoguanidine quinazoline and cyanoamidine quinazolamine derivatives that are useful in the treatment of hyperproliferative diseases are disclosed. Methods of treating hyperproliferative diseases in mammals are also disclosed.Type: GrantFiled: September 12, 2008Date of Patent: January 3, 2012Assignee: Array BioPharma Inc.Inventors: Eli Wallace, George Topolov, Qian Zhao, Joseph P. Lyssikatos
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Publication number: 20110312908Abstract: The present invention provides novel heteroaryl compounds that are linked to an aryl group via an amine linker. Such compounds are useful for the treatment of cancers.Type: ApplicationFiled: November 28, 2008Publication date: December 22, 2011Applicants: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael S. Gray, Jianming Zhang, Barun Okram, Xianming Deng, Jae Won Chang, Amy Wojciechowski
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Publication number: 20110305762Abstract: The present invention relates to a pharmaceutical composition comprising N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine as active pharmaceutical ingredient and a process of preparing such composition.Type: ApplicationFiled: August 24, 2009Publication date: December 15, 2011Applicant: ratiopharm GmbHInventors: Katrin Rimkus, Frank Muskulus, Sandra Brueck, Jana Paetz
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Publication number: 20110295004Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives of formula I 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.Type: ApplicationFiled: June 8, 2011Publication date: December 1, 2011Inventors: Changgeng Qian, Xiong Cai
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Patent number: 8067593Abstract: 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 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: GrantFiled: May 5, 2011Date of Patent: November 29, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Juergen Schroeder, Georg Dziewas
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Patent number: 8067457Abstract: 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: GrantFiled: October 26, 2006Date of Patent: November 29, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Shomir Ghosh, Prakash Raman, Kevin Sprott, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
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Publication number: 20110281896Abstract: Optical pure quinazoline compounds, especially compounds of the general formula (I), wherein R1 and Y are defined as the specification, preparation methods of them, pharmaceutical compositions containing them and their uses are provided. Compounds of the general formula (VII), which are intermediates in the synthesis of the compounds of the general formula (I), wherein Ar, R2, R3, m, n, T and carbon atom with * are defined as the specification, are also provided.Type: ApplicationFiled: January 7, 2010Publication date: November 17, 2011Inventors: Jiadeng Tang, Xuesong Wu
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Publication number: 20110269772Abstract: Axl kinase inhibitory compounds are disclosed, as well as compositions and methods of using the same in the treatment of cancer and other conditions mediated by and/or associated with Axl kinase.Type: ApplicationFiled: July 14, 2011Publication date: November 3, 2011Applicant: SUPERGEN, INC.Inventors: David J. BEARSS, Hariprasad VANKAYALAPATI, Yong XU
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Publication number: 20110263852Abstract: The present invention relates to an improved and novel process for the preparation of high purity crystalline base of Lapatinib of formula-(1) having chemical name N-{3-chloro-4-[(3-fluorobenzyloxy]phenyl}-6-[5-({[2-(methanesulfonyl)ethyl]amino}methyl]-2-furyl]-4-quin-azolinamine and its pharmaceutically acceptable salts.Type: ApplicationFiled: August 12, 2009Publication date: October 27, 2011Applicant: Natco Pharma LimitedInventors: Ramanadham Jyothi Prasad, Bhujanga Rao Adibhatla Kali Satya, Nannapaneni Venkaiah Chowdary
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Publication number: 20110257391Abstract: A process for preparing a compound (III) is provided, in which the compound (III) is prepared from a methoxycarbonyl derivative through a methoxyamide derivative. These two reaction steps are continuously carried out and substantially the same as one step. The compound (III) is useful as a synthetic intermediate for preparing a dual tyrosine kinase inhibitor and can be conveniently prepared in high yield according to the present invention.Type: ApplicationFiled: December 24, 2009Publication date: October 20, 2011Inventors: Motoyuki Hagihara, Shoji Shinomoto
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Publication number: 20110245496Abstract: Salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorders characterized by aberrant erbB family PTK activity.Type: ApplicationFiled: June 9, 2008Publication date: October 6, 2011Inventors: Andrew Simon Craig, David Malcolm Crowe, Tim Chien Ting Ho, Michael S. McClure
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Publication number: 20110237610Abstract: The invention concerns quinazoline derivatives of Formula I wherein each of R1a, R1b, R2, R3 and a have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases.Type: ApplicationFiled: October 12, 2010Publication date: September 29, 2011Applicant: AstraZeneca ABInventors: Bernard Christophe Barlaam, Laurent Francois Andre Hennequin, Christopher Thomas Halsall
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Publication number: 20110207932Abstract: 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 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: May 5, 2011Publication date: August 25, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Juergen SCHROEDER, Georg DZIEWAS, Thomas FACHINGER, Burkhard JAEGER, Carsten REICHEL, Svenja RENNER
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Publication number: 20110207929Abstract: 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 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: May 5, 2011Publication date: August 25, 2011Applicant: Boehringer Ingelheim International GmbHInventors: Juergen SCHROEDER, Georg DZIEWAS, Thomas FACHINGER, Burkhard JAEGER, Cartsen REICHEL, Svenja RENNER
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Patent number: 8003787Abstract: 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: GrantFiled: May 23, 2008Date of Patent: August 23, 2011Assignee: Bayer Schering Pharma AGInventors: Knut Eis, Olaf Prien, Ulrich Lücking, Judith Günther, Dieter Zopf, Dirk Brohm, Verena Vöhringer, Elisabeth Woltering, Hartmut Beck, Mario Lobell, Volkhart Min-Jian Li, Susanne Greschat
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Publication number: 20110201592Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain oxy phenyl aryl compounds (referred to herein as OPA compounds), as described herein, which, inter alia, inhibit Checkpoint Kinase 2 (CHK2) kinase function. 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 CHK2 kinase function, and in the treatment of diseases and conditions that are mediated by CHK2, that are ameliorated by the inhibition of CHK2 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.Type: ApplicationFiled: October 23, 2008Publication date: August 18, 2011Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Ian Collins, John Jamieson Caldwell, Antony William Oliver, Tony Michael Raynham, Emma Jane Welsh, Cornelius Albertus Johannes Matijssen
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Patent number: 7998949Abstract: The present invention relates to bicyclic heterocycles of general formula wherein Ra, Rb and Rc are defined as in claim 1, their tautomers, their stereoisomers, their mixtures and their salts, in particular their physiologically acceptable salts with inorganic or organic acids and bases, which have valuable pharmacological properties, in particular an inhibitory action on the signal transduction mediated by tyrosine kinases, their use for the treatment of illnesses, in particular of tumoral diseases and of benign prostatic hyperplasia (BPH), of diseases of the lung and of the airways, and the preparation thereof.Type: GrantFiled: January 30, 2008Date of Patent: August 16, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Birgit Jung, Ralf Lotz, Markus Ostermeier
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Publication number: 20110190248Abstract: The present invention relates to cyclohexyloxy-substituted heterocycles of general formula (I) the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways and the preparation thereof.Type: ApplicationFiled: July 23, 2009Publication date: August 4, 2011Applicant: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Birgit Jung, Ralf Lotz
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Patent number: 7989463Abstract: Novel bicyclic compounds of the formula (I), stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided. Additionally, methods of forming novel bicyclic compounds, stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided: wherein R1, R2, m, and n are defined herein.Type: GrantFiled: September 3, 2009Date of Patent: August 2, 2011Assignee: Dr. Reddy's Laboratories LimitedInventors: Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti
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Patent number: 7989462Abstract: 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 3, 2007Date of Patent: August 2, 2011Assignee: Myrexis, Inc.Inventors: Sui Xiong Cai, Mark B. Anderson, Adam Willardsen, Nilantha Sudath Sirisoma, Hong Zhang, Kazuyuki Suzuki
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Patent number: 7977347Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives of formula I 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.Type: GrantFiled: September 10, 2007Date of Patent: July 12, 2011Assignee: Curis, Inc.Inventors: Changgeng Qian, Xiong Cai
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Publication number: 20110166168Abstract: The present invention relates to sulphone-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: July 18, 2009Publication date: July 7, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Bernd Buchmann, Dirk Kosemund, Duy Nguyen, Arne Von Bonin
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Patent number: 7968568Abstract: This invention is concerned with compounds of the formula wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: GrantFiled: November 19, 2009Date of Patent: June 28, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Andreas D. Christ, Rainer E. Martin
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Publication number: 20110152297Abstract: The invention concerns quinazoline derivatives of the Formula I, or pharmaceutically acceptable salts thereof: wherein each of R1, R2, R3, R4 and m 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, and, for example, EGFR tyrosine kinase.Type: ApplicationFiled: February 24, 2006Publication date: June 23, 2011Inventors: Christopher Thomas Halsall, Laurent Francois Andre Hennequin, Alleyn Thomas Plowright, Richard Storey, Kieran Lennon
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Patent number: 7960545Abstract: 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: GrantFiled: November 22, 2006Date of Patent: June 14, 2011Assignee: Natco Pharma LimitedInventors: Ramanadham Jyothi Prasad, Bollepalli Nageshwar Rao, Nannapaneni Venkaiah Chowdary
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Patent number: 7960546Abstract: 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: GrantFiled: January 25, 2007Date of Patent: June 14, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Juergen Schroeder, Georg Dziewas, Thomas Fachinger, Burkhard Jaeger, Carsten Reichel, Svenja Renner
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Publication number: 20110136806Abstract: 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: February 15, 2011Publication date: June 9, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Birgit JUNG
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Publication number: 20110136805Abstract: The present invention relates to bicyclic heterocycles of general formula the tautomers, the stereoisomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, as well as benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.Type: ApplicationFiled: November 3, 2007Publication date: June 9, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank Himmelsbach, Birgit Jung
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Publication number: 20110117084Abstract: This invention relates to novel quinazoline derivatives and their acceptable acid addition 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 inhibitory activity against the VEGF receptor tyrosine kinase.Type: ApplicationFiled: January 22, 2009Publication date: May 19, 2011Applicant: Concert Pharmaceuticals, Inc.Inventor: Roger Tung
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Patent number: 7928107Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: March 3, 2006Date of Patent: April 19, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean Wilson, Andreas Termin, Jesus Gonzalez, Lev Fanning, Timothy Neubert, Paul Krenitsky, Pramod Joshi, Dennis Hurley, Urvi Sheth
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Patent number: 7928114Abstract: Crystalline Forms of erlotinib are made. The crystalline materials are useful as pharmaceutical active agents in treating various cancers as well as in forming erlotinib salts.Type: GrantFiled: July 27, 2007Date of Patent: April 19, 2011Assignee: Synthon BVInventor: Raymond J. H. Westheim
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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: 20110071169Abstract: The present invention is directed to two novel polymorph form (Form A and Form B) of lapatinib ditosylate, wherein Form A is the hydrate ditosylate salt of lapatinib, and Form B is anhydrate ditosylate salt of lapatinib. The present invention is further directed to amorphous form of lapatinib ditosylate and its solid dispersion. The present invention further provides processes for the preparation of Form A, Form B, Amorphous form and solid dispersion of lapatinib ditosyalte, and a pharmaceutical composition comprising the said forms. Form A and Form B were characterized by X-RPD, DSC, TGA and FT-IR, and can be prepared from recrystallizing lapatinib ditosylate in a mixture of tetrahydrofuran (THF) and water.Type: ApplicationFiled: August 14, 2010Publication date: March 24, 2011Inventors: Hui Min He Huang, Hu Yang
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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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Patent number: 7910731Abstract: 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: GrantFiled: February 26, 2008Date of Patent: March 22, 2011Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Birgit Jung, Flavio Solca
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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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Publication number: 20110053964Abstract: This invention relates to novel 4-aminoquinazolines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of the EGFR and HER-2.Type: ApplicationFiled: September 10, 2010Publication date: March 3, 2011Inventors: Roger Tung, Adam J. Morgan
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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: 20110034459Abstract: Compounds of formula (I) in which: R1 is: R2 is —CH3 or —CH2CH3; or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions including the compound of formula (I) and a pharmaceutically acceptable carrier. Processes for preparing the compound of formula (I). Methods of inhibiting a receptor tyrosine kinase in a subject in need thereof. Methods of inhibiting the growth of a tumor cell in a subject in need thereof. Methods of treating pancreatic cancer in a subject in need of treatment for pancreatic cancer. Methods of treating HER2 positive breast cancer in a subject in need of treatment for HER2 positive breast cancer. Methods of 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 10, 2011Applicant: Natco Pharma Ltd.Inventors: Bhujanga rao ADIBHATLA KALI SATYA, Ramanadham Jyothi Prasad, Bollepalli Nageshwara Rao, Nannapaneni Venkaiah Chowdary
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Patent number: 7879861Abstract: A series of new chemical agents that demonstrate anti-tumor activity are described. The new chemical agents combine two major mechanisms of anti-tumor action. In an embodiment, the agents are capable of both inhibiting EGFR and damaging DNA while also, upon degradation, degrading to an inhibitor of EGFR and to an agent capable of damaging DNA. Moreover, a novel series of molecules capable of releasing two moles of EGFR inhibitor and a potent bi-functional alkylating agent are also described.Type: GrantFiled: June 14, 2005Date of Patent: February 1, 2011Inventors: Bertrand Jean-Claude, Zakaria Rachid, Fouad Brahimi
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Publication number: 20110021495Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: January 15, 2010Publication date: January 27, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jesus Gonzalez, III, Dean Wilson, Andreas Termin, Peter D. J. Grootenhuis, Yulian Zhang, Benjamin Petzoldt, Lev T.D. Fanning, Timothy Neubert, Roger Tung, Esther Martinborough, Nicole Hilgraf
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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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Patent number: RE42353Abstract: 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: GrantFiled: September 23, 1997Date of Patent: May 10, 2011Assignee: AstraZeneca UK LimitedInventors: Andrew Peter Thomas, Craig Johnstone, Edward Clayton, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin