Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/153)
  • Patent number: 10766863
    Abstract: The invention generally relates to the field of monocarboxylate transport modulators, e.g., monocarboxylate transport inhibitors, and more particularly to new substituted-quinolone compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in treating, modulating, forestalling and/or reducing physiological conditions associated with monocarboxylate transport activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, obesity, diabetes, cardiovascular diseases, tissue and organ transplant rejection, and malaria.
    Type: Grant
    Filed: November 17, 2015
    Date of Patent: September 8, 2020
    Assignee: NIROGYONE THERAPEUTICS, INC.
    Inventors: Vincent Sandanayaka, Qiong Wu
  • Patent number: 10723701
    Abstract: The present application provides a quinolyl-substituted carboxylic acid compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, as well as a method for preparing the compound, a use of the compound, and a formulation containing the quinolyl-substituted carboxylic acid compound or the pharmaceutically acceptable salt thereof. This type of compounds are inhibitors for AXL and/or VEGFR2 protein kinase, and can be used to treat diseases caused by abnormality of the two protein kinases, such as, tumor, etc.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: July 28, 2020
    Assignee: BEIJING KONRUNS PHARMACEUTICAL CO., LTD.
    Inventors: Zhiqiang Zhang, Xijuan Wang, Xuehui Zhang, Junxia Qiu, Jiehe Yang, Xiaokai Zhang, Peng Yao
  • Patent number: 10709704
    Abstract: Provided herein are methods of treating or preventing a neurodegenerative disease, a myodegenerative disease or a prion disease in a subject comprising administering a tyrosine kinase inhibitor.
    Type: Grant
    Filed: May 6, 2016
    Date of Patent: July 14, 2020
    Assignee: Georgetown University
    Inventor: Charbel Moussa
  • Patent number: 10577349
    Abstract: Provided herein are compounds and pharmaceutical compositions comprising quinolinones. The quinolinones and compositions thereof are useful as eukaryotic translation initiation factor 4F (eIF4F) complex modulators.
    Type: Grant
    Filed: March 1, 2016
    Date of Patent: March 3, 2020
    Assignees: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE, THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING/MCGILL UNIVERSITY, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
    Inventors: Ze'ev Ronai, Anthony B. Pinkerton, Yongmei Feng, Ivan Topisirovic, Kevin Brown, Christian A. Hassig
  • Patent number: 10532983
    Abstract: Disclosed are derivative compounds of ELQ-300 that include an ester at position 4. These compounds have enhanced properties relative to ELQ-300. Also disclosed are pharmaceutical compositions comprising the compounds and methods of treating and preventing malaria infections involving administering the pharmaceutical compositions to the subject.
    Type: Grant
    Filed: July 20, 2016
    Date of Patent: January 14, 2020
    Assignee: Oregon Health & Science University
    Inventors: Michael Riscoe, Aaron Nilsen, Galen Miley, Rolf Winter, Sovitj Pou, Jane Xu Kelly, Rozalia Dodean
  • Patent number: 10407393
    Abstract: Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less.
    Type: Grant
    Filed: December 21, 2018
    Date of Patent: September 10, 2019
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Taiju Nakamura, Taichi Abe, Yusuke Miyashita, Hirofumi Kuroda, Yusuke Ayata, Atsushi Akao
  • Patent number: 10259791
    Abstract: Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less.
    Type: Grant
    Filed: August 26, 2015
    Date of Patent: April 16, 2019
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Taiju Nakamura, Taichi Abe, Yusuke Miyashita, Hirofumi Kuroda, Yusuke Ayata, Atsushi Akao
  • Patent number: 10000452
    Abstract: Provided herein are quinolone-based compounds that can be used for treatment and/or prevention of malaria and formulations thereof. Also provided herein are methods of treating and/or preventing malaria in a subject by administering a quinolone-based compound or formulation thereof provided herein.
    Type: Grant
    Filed: January 23, 2017
    Date of Patent: June 19, 2018
    Assignees: University of South Florida, Northeastern University
    Inventors: Roman Manetsch, Dennis E. Kyle, Raghupathi Neelarapu, Jordany R. Maignan, Cynthia L. Lichorowic, Alexis N. LaCrue
  • Patent number: 9873689
    Abstract: The present invention relates to methods and strategies for large-scale synthesis of compounds having the chemical structure: The R substituents are H, methyl, isopropyl, benzyl, cyclohexyl, cyclopropylmethyl, methoxy, tert-butyloxycarbonyl, methanesulfonyl, p-toluenesulfonyl, quinolinesulfonyl, or thiophenesulfonyl groups. The method comprises condensing prothionamide with a halo nitroacetophenone to form a nitrophenyl substituted thiazole, reducing the nitro group to form an amine and derivatizing the amine to produce the compound.
    Type: Grant
    Filed: November 6, 2015
    Date of Patent: January 23, 2018
    Assignee: FGH BIOTECH, INC.
    Inventor: William R. Cantrell, Jr.
  • Patent number: 9862714
    Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.
    Type: Grant
    Filed: July 14, 2016
    Date of Patent: January 9, 2018
    Assignee: STEMSYNERGY THERAPEUTICS, INC.
    Inventor: Darren Orton
  • Patent number: 9796702
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, m and n are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: April 27, 2017
    Date of Patent: October 24, 2017
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Bernd Kuhn, Yongfu Liu, Hans P. Maerki, Rainer E. Martin, Alexander V. Mayweg, Xuefei Tan, Lisha Wang, Dongbo Li, Jun Wu
  • Patent number: 9789118
    Abstract: The present invention provides compounds of formula (IV); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (IV), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.
    Type: Grant
    Filed: February 24, 2014
    Date of Patent: October 17, 2017
    Assignee: NOVARTIS AG
    Inventors: David Weninger Barnes, Gregory Raymond Bebernitz, Kevin Clairmont, Scott Louis Cohen, Robert Edson Damon, II, Robert Francis Day, Stephanie Kay Dodd, Christoph Gaul, Hatice Belgin Gulgeze Efthymiou, Monish Jain, Rajeshri Ganesh Karki, Louise Clare Kirman, Kai Lin, Justin Yik Ching Mao, Tajesh Jayprakash Patel, Brian Kenneth Raymer, Su Liansheng
  • Patent number: 9790200
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R15, R16, R17 and n are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: April 27, 2017
    Date of Patent: October 17, 2017
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Bernd Kuhn, Hans P. Maerki, Rainer E. Martin, Alexander V. Mayweg, Xuefei Tan
  • Patent number: 9750714
    Abstract: The present invention is directed to a method of treating inflammation or pain. The present invention is also directed to a method of treating an inflammatory skin disease or disorder, such as dermatitis, psoriasis, acne, or rosacea. The method comprises administering to the subject 3, 4-bis-benzylsulfonylbutyronitrile in an amount effective to reduce or eliminate the symptoms of the disease or disorder. Topical administration and oral administration are preferred route of administration.
    Type: Grant
    Filed: September 12, 2016
    Date of Patent: September 5, 2017
    Assignee: Olatec Therapeutics LLC
    Inventors: Joseph P. St. Laurent, Gerald S. Jones, David M. Bresse, Scott A. Goodrich
  • Patent number: 9751859
    Abstract: The present invention relates a new process to synthesize 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)cyclopropanamine (AL3818). A stable crystalline form of Al3818 has been prepared. Salts and their crystalline forms of AL3818 have been also prepared. Anti-cancer and optometric activities of AL3818 and its salts have been further tested. New process has been outlined in Scheme I.
    Type: Grant
    Filed: May 2, 2016
    Date of Patent: September 5, 2017
    Assignee: Advenchen Pharmaceuticals, LLC
    Inventors: Guoqing Paul Chen, Changren Yan
  • Patent number: 9440916
    Abstract: The present invention is directed to a method of treating an inflammatory skin disease or disorder, such as dermatitis, psoriasis, acne, or rosacea. The method comprises administering to the subject 3, 4-bis-benzylsulfonylbutyronitrile in an amount effective to reduce or eliminate the symptoms of the inflammatory skin disease or disorder. Topical administration and oral administration are preferred route of administration.
    Type: Grant
    Filed: March 23, 2016
    Date of Patent: September 13, 2016
    Assignee: OLATEC THERAPEUTICS LLC
    Inventors: Joseph P. St. Laurent, Gerald S. Jones, David M. Bresse, Scott A. Goodrich
  • Patent number: 9416101
    Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.
    Type: Grant
    Filed: October 31, 2014
    Date of Patent: August 16, 2016
    Assignee: STEMSYNERGY THERAPEUTICS, INC.
    Inventor: Darren Orton
  • Patent number: 9403773
    Abstract: The present invention provides a quinolone compound represented by General Formula (1) or a salt thereof, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, etc.; R3 represents a phenyl group optionally being substituted with one or more substituents, etc.; R4 represents a halogen atom; R5 represents a hydrogen atom or halogen atom; R6 represents a hydrogen atom; and R7 represents a hydroxyl group, etc. The quinolone compound have a functional improvement effect, which suppresses progression of neurological dysfunction by inhibiting the chronic progression of Parkinson's disease or protecting dopamine neurons from the disease etiology, thereby prolonging the period before first administration begins.
    Type: Grant
    Filed: April 15, 2015
    Date of Patent: August 2, 2016
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Kenji Otsubo, Yuji Ochi, Masami Nakai, Atsushi Mori
  • Patent number: 9249090
    Abstract: The present invention provides a method for producing N-substituted carbamic acid-O-aryl ester derived from a compound having an ureido group, the method comprising the step of carrying out esterification or esterification and transesterification from the compound having the ureido group and a hydroxy composition containing one type or a plurality of types of hydroxy compounds.
    Type: Grant
    Filed: September 18, 2014
    Date of Patent: February 2, 2016
    Assignee: Asahi Kasei Chemicals Corporation
    Inventors: Nobuhisa Miyake, Masaaki Shinohata, Atsushi Okubo
  • Patent number: 9062025
    Abstract: The present invention relates to a supported catalyst for olefin polymerization to which a novel transition metal compound and a co-catalyst compound are bound, and a preparation method for polyolefin using the supported catalyst. The transition metal compound bound to the catalyst of the present invention provides high activity for olefin-based monomers in heterogeneous reaction as well as in homogeneous system. Particularly, a polyolefin with higher molecular weight can be prepared by using the supported catalyst containing the transition metal compound bound to a support, rather than using the novel transition metal compound in a non-supported status, or the conventional transition metal compound in a supported or non-supported status.
    Type: Grant
    Filed: April 12, 2011
    Date of Patent: June 23, 2015
    Assignee: Lotte Chemical Corporation
    Inventors: Bun-Yeoul Lee, Ji-Hae Park, Seung-Hyun Do, Young-Kook Kim, Hwa-Kyu Kim, In-Sung Nam, Seung-Woong Yoon
  • Patent number: 9029393
    Abstract: The present invention provides new compounds with high affinity for adenosine A2A receptors. It also provides antagonists of adenosine A2A receptors and their use as medicaments for the treatment and/or prophylaxis of diseases and disorders where the partial or total inactivation of adenosine A2A receptors signalling pathways could be beneficial such as Alzheimer's disease, Parkinson's disease, attention deficit and hyperactivity disorders (ADHD), Huntington's disease, neuroprotection, schizophrenia, anxiety and pain. The present invention further relates to pharmaceutical compositions containing such new compounds with high affinity for adenosine A2A receptors and their use for the treatment and/or prophylaxis of diseases and disorders where the partial or total inactivation of adenosine A2A receptors could be beneficial.
    Type: Grant
    Filed: January 25, 2010
    Date of Patent: May 12, 2015
    Assignee: Kaldi Pharma, SAS
    Inventors: Stephan Schann, Stanislas Mayer
  • Publication number: 20150126493
    Abstract: The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 7, 2015
    Inventors: Thomas D. Aicher, Kenneth J. Barr, Vladimir Simov, Willam D. Thomas, Peter L. Toogood, Chad A. Van Huis
  • Publication number: 20150126534
    Abstract: Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.
    Type: Application
    Filed: October 7, 2014
    Publication date: May 7, 2015
    Inventors: Alan Hornsby Davidson, Alan Hastings Drummond, Lindsey Ann Needham
  • Publication number: 20150105365
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7 R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 16, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings
  • Publication number: 20150105366
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 16, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings, William Moore Jones, Steven Goldberg
  • Patent number: 9006423
    Abstract: The invention provides a process of preparing 4-amino-4-oxobutanoyl peptides and cyclic analogues thereof of Compound I and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: April 14, 2015
    Assignee: Achillion Pharmaceuticals Inc.
    Inventors: Avinash Phadke, Akihiro Hashimoto
  • Publication number: 20150099781
    Abstract: Described herein are compounds, and pharmaceutically acceptable salts and prodrugs thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound of the invention selectively inhibits a parasitic IMPDH versus a host IMPDH. Further, the invention provides pharmaceutical compositions comprising one or more compounds of the invention. The invention also relates to methods of treating various parasitic and bacterial infections in mammals. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.
    Type: Application
    Filed: December 16, 2014
    Publication date: April 9, 2015
    Inventors: Lizbeth K. Hedstrom, Gregory D. Cuny, Deviprasad R. Gollapalli, Sivapriya Kirubakaran, Sushil K. Maurya, Boris Striepen, Suresh K. Gorla, Corey R. Johnson, Mandapati Kavitha, Jihan Khan
  • Patent number: 9000037
    Abstract: This invention relates to novel precursors suitable for 18F radiolabeling of glutamate derivatives, methods for preparing such compounds and its intermediates, compositions comprising such compounds, kits comprising such compounds or compositions and methods for 18F radiolabeling of glutamate derivatives wherein the obtained 18F radiolabeled glutamate derivatives are suitable for diagnostic imaging by Positron Emission Tomography (PET) of proliferative diseases e.g. tumor in mammals.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: April 7, 2015
    Assignee: Piramal Imaging SA
    Inventors: Christina Hultsch, Michael Harre, Filip Novak, Mathias Berndt, Matthias Friebe, Heribert Schmitt-Willich, Dae Yoon Chi, Byoung Se Lee, Sang Don Park
  • Patent number: 8987301
    Abstract: Novel hetarylaminoquinoline derivatives of formula (I) wherein X, Z, Het, R1, R2, R3 and R4 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: October 12, 2010
    Date of Patent: March 24, 2015
    Assignee: Merck Patent GmbH
    Inventors: Alfred Jonczyk, Christiane Amendt, Frank Zenke
  • Publication number: 20150080373
    Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.
    Type: Application
    Filed: November 25, 2014
    Publication date: March 19, 2015
    Inventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
  • Publication number: 20150072977
    Abstract: New compounds of formula I are described. The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.
    Type: Application
    Filed: November 14, 2014
    Publication date: March 12, 2015
    Inventors: David Alexander LEARMONTH, Laszlo Erno KISS, Pedro Nuno LEAL PALMA, Humberto DOS SANTOS FERREIRA, Patricio Manuel Vieira ARAUJO SOARES DA SILVA
  • Publication number: 20150065716
    Abstract: Disclosed is a compound represented by chemical formula (1): or chemical formula (2):
    Type: Application
    Filed: August 29, 2014
    Publication date: March 5, 2015
    Inventors: Masashi MITA, Kenji HAMASE, Tsubasa OYAMA
  • Patent number: 8969352
    Abstract: The present invention is directed to compounds of Formula I: wherein X is N or CR1; Y is N or CR2; R1 is H, alkoxy, halo, triazolyl, pyrimidinyl, oxazolyl, isoxazole, oxadiazolyl, or pyrazolyl; R2 is H, alkyl, alkoxy, or halo; Z is NH or O; R3 is H, alkyl, alkoxy, halo, or triazolyl; R4 is H or alkyl; or R3 and R4, together with the atoms to which they are attached, form a 6-membered aryl ring or a 5- or 6-membered heteroaryl ring; R5 is pyridyl, pyrazinyl, or pyrimidinyl, wherein the pyridyl, pyrazinyl, or pyrimidinyl is optionally substituted with halo or alkyl; and n is 1 or 2. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: March 3, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Christine F. Gelin, Terry P. Lebold, Brock T. Shireman
  • Publication number: 20150057218
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: November 3, 2014
    Publication date: February 26, 2015
    Inventors: Min ZHONG, Leping LI
  • Publication number: 20150057310
    Abstract: Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide.
    Type: Application
    Filed: July 25, 2014
    Publication date: February 26, 2015
    Inventors: Adrian St. Clair Brown, Peter Lamb, William P. Gallagher
  • Patent number: 8962655
    Abstract: Disclosed are: a therapeutic agent, a kit and a treatment method for undifferentiated gastric cancer; and a pharmaceutical composition, a kit and a treatment method which are more effective on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR2 and a cell expressing a mutant FGFR2. A combination of a FGFR2 inhibitor and a therapeutic substance for gastric cancer is more effective on undifferentiated gastric cancer. The combination of a FGFR2 inhibitor and a therapeutic substance for gastric cancer is more effective on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR2 and a cell expressing a mutant FGFR2.
    Type: Grant
    Filed: January 28, 2008
    Date of Patent: February 24, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventor: Yuji Yamamoto
  • Publication number: 20150051177
    Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Inventor: Darren Orton
  • Publication number: 20150038714
    Abstract: The present invention relates to novel and concise process for the construction of chiral 3-substituted tetrahyroquinoline derivatives based on proline catalyzed asymmetric ?-functionalization of aldehyde, followed by in situ reductive cyclization of nitro group under catalytic hydrogenation condition with high optical purities. Further the invention relates to conversion of derived chiral 3-substituted tetrahydroquinoline derivatives into therapeutic agents namely (?)-sumanirole (96% ee) and 1-[(S)-3-(di-methylamino)-3,4-dihydro-6,7-dimethoxy-quinolin-1(2H)-yl]propanone[(S)-903] (92% ee).
    Type: Application
    Filed: March 19, 2013
    Publication date: February 5, 2015
    Applicant: Council of Scientific & Industrial Research
    Inventors: Varun Rawat, Senthil Kumar Boopathi, Arumugam Sudalai
  • Patent number: 8946431
    Abstract: Provided is a 2-(substituted ethynyl)quinoline derivative having an mGluR5 antagonistic activity and pharmaceutically acceptable salts thereof. The compound of the present invention can be useful as a medicament for treating and preventing mGluR5 receptor-mediated diseases such as Alzheimer's disease, senile dementia, Parkinson's disease, L-DOPA-induced dyskinesia, Huntington's chorea, amyotrophic lateral sclerosis, multiple sclerosis, schizophrenia, anxiety disorder, depression, neuropathic pain, drug dependence, fragile X syndrome, autism, migraine and gastroesophageal reflux disease (GERD).
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: February 3, 2015
    Assignee: Korea Institute of Science and Technology
    Inventors: Sun Joon Min, Yong Seo Cho, Ae Nim Pae, Eun Jeong Lim, Ji Yeong Kim, Myung Hee Son, Jae Kyun Lee
  • Patent number: 8940375
    Abstract: The present invention relates to a liquid-crystal (LC) display of the PS (polymer stabilized) or PSA (polymer sustained alignment) type, and to polymerizable compounds and LC media for use in PS (polymer stabilized) and PSA displays.
    Type: Grant
    Filed: July 3, 2008
    Date of Patent: January 27, 2015
    Assignee: Merck Patent GmbH
    Inventors: Matthias Bremer, Georg Bernatz
  • Patent number: 8933230
    Abstract: Phosphorus-containing group-substituted quinolines of formula (I) are provided in the present invention. The preparation process and application of the compound, and formulation comprising phosphorus-containing group-substituted quinolines are also disclosed. The compounds are protein kinase inhibitor and can be used for treating protein kinase abnormal activity-associated diseases, such as tumor, etc.
    Type: Grant
    Filed: April 6, 2011
    Date of Patent: January 13, 2015
    Assignee: Beijing Konruns Pharmaceutical Co., Ltd.
    Inventors: Ziwei Yun, Hongtao Wang
  • Patent number: 8927576
    Abstract: The present invention is directed to a combination product for treating or ameliorating hepatitis C virus (HCV) infection or disorders or symptoms associated therewith in a subject in need thereof comprising, a HCV inhibitor and one or more therapeutic agents selected from either or both a HCV protease inhibitor and one or more different therapeutic agents administered in combination in an effective amount to the subject.
    Type: Grant
    Filed: April 6, 2010
    Date of Patent: January 6, 2015
    Assignee: PTC Therpeutics, Inc.
    Inventor: Zhengxian Gu
  • Publication number: 20140364431
    Abstract: The present invention relates to a series of quinoline and cinnoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof. And the compounds of general formula I show potent inhibitory activity gainst c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and/or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and/or prevention of cancer.
    Type: Application
    Filed: December 7, 2012
    Publication date: December 11, 2014
    Inventors: Ping Gong, Yanfang Zhao, Yajing Liu, Xin Zhai, Sai Li, Wufu Zhu, Mingze Qin
  • Publication number: 20140357626
    Abstract: Inhibitors of HCV replication of formula I, including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
    Type: Application
    Filed: December 27, 2012
    Publication date: December 4, 2014
    Inventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 8901306
    Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.
    Type: Grant
    Filed: March 2, 2010
    Date of Patent: December 2, 2014
    Assignee: StemSynergy Therapeutics, Inc.
    Inventor: Darren Orton
  • Publication number: 20140328796
    Abstract: The invention provides 4-amino-4-oxobutanoyl peptide compounds of Formula I and the pharmaceutically salts and hydrates thereof. The variables R1-R9, R16, R18, R19, n, M, n, M, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain 4-amino-4-oxobutanoyl peptide compounds disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide compounds and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain 4-amino-4-oxobutanoyl peptide compound as the only active agent or may contain a combination of 4-amino-4-oxobutanoyl peptide containing peptides compound and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in mammals.
    Type: Application
    Filed: July 21, 2014
    Publication date: November 6, 2014
    Inventors: Avinash Phadke, Xiangzhu Wang, Suoming Zhang, Atul Agarwal
  • Patent number: 8877752
    Abstract: Provided are 4(1H)-quinolone derivatives effective in inhibiting or eliminating the viability of at least one of the stages in the life-cycle of the malarial parasite, and to show a reduced propensity to induce resistance to the compound by the target parasite. In particular, the compounds can be derivatives of phenoxyethoxy-quinolones, and including, but not only, 7-(2-phenoxyethoxy)quinolin derivatives. These compounds may be administered by themselves, with at least one other derivative compound, or with other antimalarial compounds, to an animal or human subject. The therapeutic compositions can be and formulated to reduce the extent of a Plasmodium infection in the recipient subject, or to reduce the likelihood of the onset or establishment of a Plasmodium infection if administered prior to the parasite contacting the subject. The therapeutic compositions can be formulated to provide an effective single dose amount of an antimalarial compound or multiple doses for administering over a period of time.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: November 4, 2014
    Assignee: University of South Florida
    Inventors: Roman Manetsch, Richard Matthew Cross, Niranjan Kumar Namelikonda, Dennis Edward Kyle, Tina Susanna Mutka, Alexis Nichole LaCrue, Jordany Richarlson Maignan, Fabian Ernesto Saenz
  • Patent number: 8877776
    Abstract: Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane -1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-ffuorophenyl)cyclopropane-1,1-dicarboxamide.
    Type: Grant
    Filed: January 15, 2010
    Date of Patent: November 4, 2014
    Assignee: Exelixis, Inc.
    Inventors: Adrian St. Clair Brown, Peter Lamb, William P. Gallagher
  • Patent number: 8877930
    Abstract: The present invention provides various methods for the synthesis of chemical species in a microreactor environment. In some cases, reaction products of the present invention may be valuable as intermediates and/or products in pharmaceutical and polymer research. For example, the method may involve the synthesis of amino alcohols within a microchannel. Embodiment described herein may allow for reactions with significantly shorter reaction times and increased efficiency.
    Type: Grant
    Filed: November 4, 2010
    Date of Patent: November 4, 2014
    Assignee: Massachusetts Institute of Technology
    Inventors: Matthew W. Bedore, Nikolay Zaborenko, Klavs F. Jensen, Timothy F. Jamison
  • Publication number: 20140323522
    Abstract: This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and bone metastases, with a dual inhibitor of MET and VEGF.
    Type: Application
    Filed: November 8, 2012
    Publication date: October 30, 2014
    Inventors: Dana T. Aftab, Frauke Schimmoller