Nitrogen Bonded Directly At 4-position Patents (Class 544/293)
  • Patent number: 11111234
    Abstract: Provided are a maleate of a quinazoline derivative-like tyrosine kinase inhibitor represented by Formula (1), and a crystal form thereof and a preparation method therefor, a pharmaceutical composition comprising the maleate and the crystal form thereof, as well as use of the maleate and the crystal form thereof in the manufacture of a medicament for treating and/or preventing a hyperproliferative disease and a chronic obstructive pulmonary disease.
    Type: Grant
    Filed: August 11, 2017
    Date of Patent: September 7, 2021
    Assignee: XUANZHU PHARMA CO., LTD.
    Inventors: Jinyuan Wang, Zhenhua Wang, Yuzhen Feng
  • Patent number: 10822334
    Abstract: Disclosed are compounds inhibiting ErbBs (e.g. HER2), pharmaceutically acceptable salts, hydrates, solvates or stereoisomers thereof and pharmaceutical compositions comprising the compounds. The compound and the pharmaceutical composition can effectively treat diseases associated ErbBs (especially HER2), including cancer.
    Type: Grant
    Filed: June 24, 2020
    Date of Patent: November 3, 2020
    Inventors: Zhengtao Li, Wei Zhong, Jiabing Wang, Qingbei Zeng, Honchung Tsui, Zhenfan Yang, Xiaolin Zhang
  • Patent number: 10329281
    Abstract: The present invention relates to Quinazolinyl derivatives polymorph, process and composition thereof.
    Type: Grant
    Filed: April 15, 2016
    Date of Patent: June 25, 2019
    Assignee: HETERO LABS LTD
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Bandi Vamsi Krishna, Nimmala Srinivas Rao
  • Patent number: 9796704
    Abstract: The present invention provides compounds of structural formula I, 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: Grant
    Filed: September 4, 2015
    Date of Patent: October 24, 2017
    Assignee: SYMPHONY EVOLUTION, INC.
    Inventors: Kenneth D. Rice, Neel K. Anand, Joerg Bussenius, Simona Costanzo, Abigail R. Kennedy, Csaba J. Peto, Tsze H. Tsang, Charles M. Blazey
  • Patent number: 9676691
    Abstract: A method is described for producing a compound having the formula (I) or an admixture comprising a compound having the formula (I), having the following steps: dissolving an indanone having the formula (II) in a solvent or in an admixture which contains a solvent, the solvent being selected from the group of solvents which form an azeotrope with water, converting the indanone having the formula (II) with an aromatic aldehyde having the formula (III) in the presence of at least one organic base, according to the drawing: where R1 and R2 independently of each other signify hydrogen or a branched or unbranched alkyl group having from 1 to 12 carbon atoms and where R3, R4, R5, R6, R7, R8, R9, R10 and R11 independently of each other signify hydrogen, hydroxy or a branched or unbranched alkyl or alkoxy group having from 1 to 12 carbon atoms and removing water formed from the reaction admixture during the conversion.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: June 13, 2017
    Assignee: SYMRISE AG
    Inventors: Oskar Koch, Dietmar Schatkowski, William Johncock, Christel Jahnke, Karl-Georg Fahlbusch
  • Patent number: 9518043
    Abstract: The present invention relates to a novel method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)prop-2-en-1-one in a simpler process as compared with conventional methods by allowing 4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-ol to react with an N-acyl piperidine derivative in an inert polar protic solvent in the presence of a base.
    Type: Grant
    Filed: January 27, 2014
    Date of Patent: December 13, 2016
    Assignee: Hanmi Pharm. Co., Ltd.
    Inventors: Keuk Chan Bang, Jae Hyuk Jung, Young Ho Moon
  • Patent number: 9359332
    Abstract: The present disclosure 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. The compounds are generally of formula (I): 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. Also disclosed are methods of making compounds for formula 8: comprising introducing group E2 into a compound of formula 7: wherein Ar, Z, P, and E2 are defined herein.
    Type: Grant
    Filed: October 22, 2013
    Date of Patent: June 7, 2016
    Assignee: Symphony Evolution, Inc.
    Inventors: Kenneth D. Rice, Neel K. Anand, Joerg Bussenius, Simona Costanzo, Abigail R. Kennedy, Csaba J. Peto, Tsze H. Tsang, Charles M. Blazey
  • Patent number: 9163006
    Abstract: The present disclosure 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. The compounds are generally of formula (I): 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. Also disclosed are methods of making compounds for formula 8: comprising introducing group E2 into a compound of formula 7: wherein Ar, Z, P, and E2 are defined herein.
    Type: Grant
    Filed: October 22, 2013
    Date of Patent: October 20, 2015
    Assignee: Symphony Evolution, Inc.
    Inventors: Kenneth D. Rice, Neel K. Anand, Joerg Bussenius, Simona Costanzo, Abigail R. Kennedy, Csaba J. Peto, Tsze H. Tsang, Charles M. Blazey
  • Publication number: 20150133460
    Abstract: This invention provides a compound of formula (I): or a crystalline form thereof, or a pharmaceutical composition thereof, or an oral pharmaceutical dosage form thereof; processes for the synthesis or manufacture of the compound of formula (I), or a crystalline form thereof, or a pharmaceutical composition thereof, or an oral pharmaceutical dosage form thereof; and the use of said compound, or a crystalline form thereof, or a pharmaceutical composition thereof, or an oral pharmaceutical dosage form thereof, for the treatment of patients suffering from or subject to diseases, disorders or conditions involving cell survival, proliferation, and migration, including cardiovascular disease (e.g., arteriosclerosis and vascular reobstruction), cancer, (e.g., AML and malignant glioma) glomerulosclerosis, fibrotic disease and inflammation.
    Type: Application
    Filed: November 11, 2013
    Publication date: May 14, 2015
    Applicant: Millennium Phamaceuticals, Inc.
    Inventors: Ian Armitage, Abu J. Ferdous, Michael E. Bourland, Craig S.J. Boyle, Martin Ian Cooper, Marianne Langston
  • Publication number: 20150132342
    Abstract: Provided herein are compounds and methods for modulating an immune response in a subject in need thereof. Further provided herein are compounds and methods for modulating a toll-like receptor protein.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 14, 2015
    Inventors: Dennis A. Carson, Howard B. Cottam, Tomoko Hayashi, Afshin Nour
  • Publication number: 20150133476
    Abstract: 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: Application
    Filed: November 18, 2014
    Publication date: May 14, 2015
    Inventors: Jianhui Guo, Yong Jiang
  • Publication number: 20150133439
    Abstract: The Present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.
    Type: Application
    Filed: July 9, 2014
    Publication date: May 14, 2015
    Inventors: Anjali Pandey, Robert M. Scarborough, Kenji Matsuno, Michio Ichimura, Yuji Nomoto, Shinichi Ide, Eiji Tsukuda, Junko Sasaki, Shoji Oda
  • Publication number: 20150126537
    Abstract: The present invention is directed to novel bicyclic compounds, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities and are useful for the treatment of protein kinases mediated diseases and conditions. Novel bicyclic compounds disclosed herein include quinazolines and quinolines.
    Type: Application
    Filed: May 13, 2013
    Publication date: May 7, 2015
    Inventor: Dawei Zhang
  • Publication number: 20150126539
    Abstract: The present invention is directed to novel quinazolines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities and are expected to be useful for the treatment of protein kinases mediated diseases and conditions.
    Type: Application
    Filed: May 7, 2013
    Publication date: May 7, 2015
    Inventors: Xiaoyang Xia, Dawei Zhang
  • Patent number: 9024024
    Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives of Formula (IV) below. These compounds have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and are useful in the treatment of EGFR-TK related diseases and disorders such as cancer. These compounds may further act as HDAC inhibitors.
    Type: Grant
    Filed: November 25, 2013
    Date of Patent: May 5, 2015
    Assignee: Curis, Inc.
    Inventors: Changgeng Qian, Xiong Cai, Stephen Gould, Haixiao Zhai
  • Publication number: 20150111847
    Abstract: The present invention relates to processes for the preparation of erlotinib and salts and polymorphs thereof preparable by said processes, to medical uses of said erlotinib, salts and polymorphs, and to pharmaceutical compositions comprising the same.
    Type: Application
    Filed: January 6, 2015
    Publication date: April 23, 2015
    Applicant: GENERICS [UK] LIMITED
    Inventors: Vinayak Govind Gore, Anilkumar Tripathi, Madhav Jadhav
  • Patent number: 9012464
    Abstract: Afatinib salts and crystalline forms thereof are described in the present application and processes for their preparation. Crystalline forms of Afatinib are also described in the present application and processes for their preparation. The present invention also includes pharmaceutical compositions of such Afatinib salts and crystalline forms thereof or crystalline forms of Afatinib, methods of their preparation and the use thereof in the treatment of a patient in need thereof.
    Type: Grant
    Filed: November 23, 2011
    Date of Patent: April 21, 2015
    Assignee: Ratiopharm GmbH
    Inventors: Ramesh Matioram Gidwani, Channaveerayya Hiremath, Manoj Dalsingar Yadav, Wolfgang Albrecht, Dirk Fischer
  • Patent number: 9006257
    Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: April 14, 2015
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Laxmikant Atmaram Gharat, Abhisek Banerjee, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Patent number: 9000162
    Abstract: The present disclosure relates to compounds of Formula 1,5,8-difluoro-4-(2-(4-(heteroaryloxy)phenyl)ethylamino)quinazolines, and their use as agrochemicals and animal health products.
    Type: Grant
    Filed: September 17, 2012
    Date of Patent: April 7, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: William K. Brewster, Carla J. R. Klittich, Chenglin Yao, Yuanming Zhu, Brent J. Rieder
  • Publication number: 20150094275
    Abstract: The present invention provides novel heteroaryl compounds having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.
    Type: Application
    Filed: November 13, 2014
    Publication date: April 2, 2015
    Applicants: THE SCRIPPS RESEARCH INSTITUTE, DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. GRAY, Jianming ZHANG, Barun OKRAM, Xianming DENG, Jae Won CHANG, Amy WOJCIECHOWSKI
  • Patent number: 8993579
    Abstract: There is provided a crystalline form of Lapatinib, termed APO-I, and methods for making APO-I. There is also provided a crystalline solvate form of Lapatinib, termed APO-II, and methods for making APO-II.
    Type: Grant
    Filed: April 21, 2011
    Date of Patent: March 31, 2015
    Assignee: Apotex Pharmachem Inc
    Inventors: Carlos Zetina-Rocha, Eduardo Gustavo Cammisa, Gamini Weeratunga
  • Patent number: 8975401
    Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives of Formula (I) below. These compounds have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and are useful in the treatment of EGFR-TK related diseases and disorders such as cancer. These compounds may further act as HDAC inhibitors.
    Type: Grant
    Filed: May 15, 2013
    Date of Patent: March 10, 2015
    Assignee: Curis, Inc.
    Inventors: Changgeng Qian, Xiong Cai, Stephen Gould
  • Publication number: 20150065710
    Abstract: The present invention refers to a new efficient process for the synthesis of the active pharmaceutical ingredient Lapatinib and salts thereof. In particular, the present synthesis is carried out employing new intermediates in which the amine function is protected by a group cleavable in basic milieu that provides a higher overall yield of the synthesis process.
    Type: Application
    Filed: September 3, 2013
    Publication date: March 5, 2015
    Applicant: F.I.S. - Fabbrica Italiana Sintetici S.p.A.
    Inventors: Francesco Fontana, Alfredo Paio
  • Publication number: 20150065527
    Abstract: A pharmaceutical formulation comprising the compound of formula
    Type: Application
    Filed: November 10, 2014
    Publication date: March 5, 2015
    Inventors: Malcolm Clive Carter, George Stuart Cockerill, Karen Elizabeth Lackey
  • Publication number: 20150065709
    Abstract: The invention discloses a new amino-quinazoline derivative and its use in preparing drugs for preventing and/or treating malignancies. The amino-quinazoline derivative of the invention is an ideal, high effective, dual and irreversible EGFR and HER2 kinase inhibitor, and can treat or prevent various malignancy diseases, such as breast cancer, ovarian cancer, gastrointestinal cancer, oesophageal cancer, lung cancer, head and neck squamous cancer, pancreatic cancer, epidermis squamous cell cancer, prostatic cancer, neuroglioma and nasopharynx cancer.
    Type: Application
    Filed: March 13, 2013
    Publication date: March 5, 2015
    Inventors: Jianming Yin, Junhua Tao
  • Patent number: 8952154
    Abstract: There is provided processes for preparing Lapatinib and pharmaceutically acceptable salts thereof by the reductive amination of the aldehyde of Formula II by treatment with 2-methanesulphonylethylamine followed by catalytic hydrogenation in the presence of a suitable hydrogenation catalyst.
    Type: Grant
    Filed: December 23, 2011
    Date of Patent: February 10, 2015
    Assignee: Apotex Pharmachem Inc.
    Inventors: Mohammed Abdul Raheem, Gamini Weeratunga, Carlos Zetina-Rocha, Eduardo Gustavo Cammisa
  • Patent number: 8937079
    Abstract: 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: Grant
    Filed: November 19, 2012
    Date of Patent: January 20, 2015
    Assignee: Shanghai Allist Pharmaceuticals, Inc.
    Inventors: Jianhui Guo, Yong Jiang
  • Patent number: 8936840
    Abstract: The purpose of the present invention is to provide a retardation film which has high retardation developability, good mechanical strength and good durability. This retardation film contains a cellulose derivative and at least one compound represented by general formula (1), wherein each of R1 and R2 independently represents an alkyl group, a cycloalkyl group, an aryl group or a heterocyclic group; X1 represents a single bond, —NR4—, —O— or —S—; X2 represents a single bond, —NR5—, —NR5—(C?O)—, —O— or —S—; each of R4 and R5 independently represents a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group or a heterocyclic group; R3 represents a substituent; n represents an integer of 0-4; and when n is 2 or more, a plurality of R3s may be the same or different and adjacent R3s may be joined together to form a ring).
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: January 20, 2015
    Assignee: Konica Minolta, Inc.
    Inventors: Takatsugu Suzuki, Issei Nakahara, Hiroyoshi Kiuchi, Kiyoshi Fukusaka
  • Publication number: 20150010545
    Abstract: The present invention provides a method of treating breast cancer that is nonresponsive to treatment with trastuzumab, comprising administering to a subject in need of such treatment a therapeutically effective amount of compound N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 27, 2012
    Publication date: January 8, 2015
    Inventors: Samuel Waksal, Lillian Chiang
  • Patent number: 8927711
    Abstract: Provided herein are quinazoline compounds of formula (I): The compounds are useful for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: January 6, 2015
    Assignee: Ambit Biosciences Corp.
    Inventors: Sunny Abraham, Qi Chao, Michael J. Hadd, Mark W. Holladay, Gang Liu, Eduardo Setti
  • Patent number: 8927558
    Abstract: Impurities of lapatinib such as N-{3-chloro-4-[(2-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)furan-2-yl]quinazoline-4-amine compound of formula (I) or a salt thereof: and analytical methods for identifying and quantifying such impurities of Lapatinib and salts thereof are provided. Also provided is Lapatinib containing less than about 0.05 percent of this and related impurities and methods for preparing such pure forms of Lapatinib.
    Type: Grant
    Filed: May 14, 2012
    Date of Patent: January 6, 2015
    Assignee: F.I.S.—Fabbrica Italiana Sintetici S.p.A.
    Inventors: Francesco Fontana, Alessandro Leganza, Sergio Osti
  • Publication number: 20150005278
    Abstract: This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I wherein Ar, R1 and R2 are as defined in the description and claims, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.
    Type: Application
    Filed: June 26, 2014
    Publication date: January 1, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Andreas BLUM, Dirk GOTTSCHLING, Armin HECKEL, Joerg P. HEHN, Bernhard SCHMID, Dieter WIEDENMAYER
  • Patent number: 8921336
    Abstract: The present invention provides novel heteroaryl compounds of formula (I) having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.
    Type: Grant
    Filed: November 28, 2008
    Date of Patent: December 30, 2014
    Assignees: Dana-Farber Cancer Institute, Inc., The Scripps Research Institute
    Inventors: Nathanael Gray, Jianming Zhang, Barun Okram, Xianming Deng, Jae Won Chang
  • Publication number: 20140378684
    Abstract: 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: Application
    Filed: September 9, 2014
    Publication date: December 25, 2014
    Applicant: ASTRAZENECA AB
    Inventors: Jorgen BLIXT, Michael David GOLDEN, Philip John HOGAN, David Michael Glanville MARTIN, Francis Joseph MONTGOMERY, Zakariya PATEL, John David PITTAM, George Joseph SEPENDA, Christopher John SQUIRE, Nicholas Cartwright Alexander WRIGHT
  • Publication number: 20140378683
    Abstract: The invention relates to the compounds and methods for inhibiting the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. More particularly, the invention relates to compounds and methods for inhibiting the CDKI pathway for studies of and intervention in senescence-related and other CDKI-related diseases.
    Type: Application
    Filed: June 21, 2013
    Publication date: December 25, 2014
    Inventors: DONALD C. PORTER, Igor B. Roninson, Mark P. Wentland
  • Publication number: 20140364420
    Abstract: The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.
    Type: Application
    Filed: January 13, 2014
    Publication date: December 11, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Kenneth G. Carson, Shomir Ghosh, Prakash Raman, Francois Soucy, Qing Ye
  • Patent number: 8901140
    Abstract: 6-amino quinazoline or 3-cyano quinoline derivatives, preparation methods and pharmaceutical uses thereof are disclosed. Specifically, the present disclosure discloses novel 6-amino quinazoline or 3-cyano quinoline derivatives presented by general formula (I), or tautomers, enantiomers, diastereomers, racemates or pharmaceutically acceptable salts thereof, or metabolites, metabolic precursors or prodrugs thereof, and their uses as treatment agents especially as protein kinase inhibitors, in which each substitutent group of general formula (I) is as defined in the specification.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: December 2, 2014
    Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Peng Cho Tang, Xin Li, Bin Wang, Jun Wang, Lijun Chen
  • Patent number: 8901138
    Abstract: This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I wherein Ar, R1 and R2 are as defined herein, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.
    Type: Grant
    Filed: November 7, 2013
    Date of Patent: December 2, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Andreas Blum, Dirk Gottschling, Armin Heckel, Joerg Hehn, Thorsten Lehmann-Lintz, Dieter Wiedenmayer
  • Publication number: 20140323464
    Abstract: Provided herein are kinase inhibiting compounds and methods of using the same.
    Type: Application
    Filed: May 16, 2012
    Publication date: October 30, 2014
    Inventors: John William Taunton, JR., Kenneth Albert Brameld, David Michael Goldstein, Jesse Mcfarland, Shyam Krishnan, Jonathan Choy
  • Patent number: 8865899
    Abstract: 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.
    Type: Grant
    Filed: December 7, 2011
    Date of Patent: October 21, 2014
    Assignee: AstraZeneca AB
    Inventors: Jorgen Blixt, Michael David Golden, Philip John Hogan, David Michael Glanville Martin, Francis Joseph Montgomery, Zakariya Patel, John David Pittam, George Joseph Sependa, Christopher John Squire, Nicholas Cartwright Alexander Wright
  • Patent number: 8865898
    Abstract: A nucleoside analog and a salt thereof represented by any of the general formulae (1) to (10) below: wherein R1, R2, and R3 are the same or different groups, and each of the R1, R2 and R3 is selected from a hydrogen atom, a protecting group for a functional group in nucleic acid synthesis, a phosphate group, a phosphate group protected by a protecting group in nucleic acid synthesis, and an activated phosphate group for solid phase synthesis; and Ar is one of an aromatic hydrocarbon group and a polyaromatic hydrocarbon group.
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: October 21, 2014
    Assignee: Japan Science and Technology Agency
    Inventor: Yoshihito Ueno
  • Patent number: 8859767
    Abstract: The present invention relates to an improved method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-prop-2-en-1-one hydrochloride, which selectively and effectively inhibits the growth of cancer cells induced by over-expression of an epidermal growth factor receptor (EGFR) and prevents the development of drug resistance caused by mutation of a tyrosine kinase, and intermediates used therein.
    Type: Grant
    Filed: October 5, 2012
    Date of Patent: October 14, 2014
    Assignee: Hanmi Science Co., Ltd
    Inventors: Keuk Chan Bang, Young Ho Moon, Young Kil Chang
  • Patent number: 8853396
    Abstract: Methods for the synthesis of the pharmaceutically active ingredient Lapatinib and the salts thereof are provided. In particular, such methods utilize intermediates in which the hydroxyl function is protected by a tetrahydropyranyl group providing greater solubility of the intermediates in common organic solvents.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: October 7, 2014
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventor: Francesco Fontana
  • Patent number: 8846699
    Abstract: The present invention relates to a novel quinazoline derivative compound having the formula (1) as follows: with the constituents defined in claim 1, and a pharmaceutically acceptable salt thereof as a multiplex inhibitor, a method for the preparation thereof, and a pharmaceutical composition and a therapeutic composition comprising same as an active ingredient. The inventive quinazoline derivative as a multiplex inhibitor can selectively and effectively inhibit diseases caused by the overactivity of a tyrosine kinase.
    Type: Grant
    Filed: November 8, 2006
    Date of Patent: September 30, 2014
    Assignee: Hanmi Pharm. Co., Ltd.
    Inventors: Young-Gil Ahn, Jong Woo Kim, Keuk Chan Bang, Bum Woo Park, Se Young Kim, Kyungik Lee, Kyuhang Lee, Myoung-Sil Ko, Han Kyong Kim, Young Hoon Kim, Maeng Sup Kim, Gwan Sun Lee
  • Patent number: 8846912
    Abstract: The present invention relates to tartrate salts of quinazoline containing zinc-binding moiety based derivatives of Formula II, below: These compounds are inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and may further act as HDAC inhibitors. The invention further relates to the use of these tartrate salts in the treatment of EGFR-TK related diseases and disorders such as cancer.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: September 30, 2014
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
  • Publication number: 20140275534
    Abstract: The present invention relates to an improved method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-prop-2-en-1-one hydrochloride, which selectively and effectively inhibits the growth of cancer cells induced by over-expression of an epidermal growth factor receptor (EGFR) and prevents the development of drug resistance caused by mutation of a tyrosine kinase, and intermediates used therein.
    Type: Application
    Filed: October 5, 2012
    Publication date: September 18, 2014
    Inventors: Keuk Chan Bang, Young Ho Moon, Young Kil Chang
  • Patent number: 8835446
    Abstract: The present invention relates to novel quinazoline derivatives with less skin irritation and an excellent action of strongly suppressing scratching behavior, and pharmaceutical compositions containing a quinazoline derivative as an active ingredient. The present invention is directed to the quinazoline derivatives represented by the general formula [1] or pharmaceutically acceptable salts thereof. In the general formula [1], R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 and R4 are the same or different and represent hydrogen, alkyl, alkoxy or halogen; R5 is combined with R6 to represent alkylene or represents hydrogen, hydroxy, alkyl, phenyl or alkoxy; R6 represents alkyl, cycloalkyl, phenyl, a 5- to 10-membered aromatic heterocyclic group containing one to three heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, or —N(R6-1)(R6-2).
    Type: Grant
    Filed: April 2, 2013
    Date of Patent: September 16, 2014
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Masahiko Okano, Tatsuya Oyama
  • Publication number: 20140255428
    Abstract: The invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof: which possess inhibitory activity against activating mutant forms of EGFR, and are accordingly useful for their anti-cancer activity and in methods of treatment of the human or animal body. The invention also relates 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: Application
    Filed: March 5, 2014
    Publication date: September 11, 2014
    Applicant: ASTRAZENECA AB
    Inventors: David Yunzhi LI, Jiabing WANG, Zhenfan YANG, Qingbei ZENG, Xiaolin ZHANG
  • Patent number: 8815879
    Abstract: Selenophene compounds of formula (I) are described herein. In the compounds of Formula (I), ring A is a 6-membered aromatic fused ring, optionally containing one, two or three nitrogen atoms; a 5-membered heteroaromatic fused ring; or a mono- or bicyclic saturated heterocyclic fused ring having at least one ring member selected from the group consisting of N, O, S, SO and SO2; Y in ring B is nitrogen or substituted carbon; X is NR6, O, S, S(O), or S(O)2. R1, R2, R3, R4, and R6 are defined in the specification. Selenophene compounds of formula (I) may be used in methods of treating cell proliferative disorders, particularly cancer. Pharmaceutical compositions containing selenophene compounds of formula (I) may be used for treatment, inhibition, or control of cancer.
    Type: Grant
    Filed: May 17, 2013
    Date of Patent: August 26, 2014
    Assignee: Kasina Laila Innova Pharmaceuticals Private Limited
    Inventors: Sudhakar Kasina, Ganga Raju Gokaraju, Venkateswarlu Somepalli, Rama Raju Gokaraju, Venkata Kanaka Ranga Raju Gokaraju, Kiran Bhupathiraju, Trimurtulu Golakoti, Krishanu Sengupta, Venkata Krishna Raju Alluri
  • Publication number: 20140234317
    Abstract: Methods are disclosed for preventing toxic drug-drug interactions during combination cancer therapy with a drug that is an anti-ErbB3 agent, such as an anti-ErbB3 antibody, together with a drug that is a tyrosine kinase inhibitor and/or a drug that binds to alpha-1 acid glycoprotein (e.g., erlotinib). Health care practitioners obtaining any one of the drugs are warned that when co-administering the drug that is an anti-ErbB3 agent with either or both of a drug that is a tyrosine kinase inhibitor and a drug that binds to alpha-1 acid glycoprotein, at least one of the co-administered drugs should be administered using a reduced dosage to prevent toxicity. In a reduced dosage, the amount of drug administered per unit time is reduced as compared to a dose that would be administered if the drug was administered as monotherapy. The reduced dosage can be, for example, a reduced drug dose or a reduced drug dosing frequency, or both. Compositions useful in practicing the disclosed methods are also provided.
    Type: Application
    Filed: May 4, 2012
    Publication date: August 21, 2014
    Applicant: Merrimack Pharmaceuticals, Inc.
    Inventors: Matthew David Onsum, Clet Niyikiza, Victor Moyo, William Kubasek, Akos Czibere