Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/349)
  • Patent number: 11085918
    Abstract: The present invention relates to use of inhibitors of Notch signalling pathway selected from the group consisting of 6-(4-Tert-Butylphenoxy)Pyridin-3-Amine (I3), its derivatives, in treating and/or preventing cancers.
    Type: Grant
    Filed: March 25, 2019
    Date of Patent: August 10, 2021
    Assignee: ECOLE POLYTECHNIQUE FEDERALE DE LAUSANNE (EPFL)
    Inventors: Freddy Radtke, Rajwinder Lehal, Viktoria Reinmüller, Jieping Zhu
  • Patent number: 10875875
    Abstract: Provided herein are compounds and pharmaceutical compositions of formula I where R1, R2, R3, R4, R5 and R6 are as described herein. Also provided pharmaceutically acceptable salts or stereoisomers of these compounds. In addition methods are provided for inhibiting the binding of an integrin to treat various pathophysiological conditions.
    Type: Grant
    Filed: April 26, 2017
    Date of Patent: December 29, 2020
    Assignee: Aviara Pharmaceuticals, Inc.
    Inventors: Ronald J. Biediger, Michele A. Benish, Lindsay Bonner Hardy, Vincent A. Boyd, Robert V. Market, Thomas P. Thrash, Brandon M. Young
  • Patent number: 10494367
    Abstract: Provided herein are methods for antagonizing the action of an ?4-integrin to treat various pathophysiological conditions utilizing pharmaceutical compositions of compounds or pharmaceutically acceptable salts or stereoisomer(s) thereof of formula I where R1, R2, R3, R4, R5, X and R6 are as described herein.
    Type: Grant
    Filed: April 1, 2019
    Date of Patent: December 3, 2019
    Assignee: Aviara Pharmaceuticals, Inc.
    Inventors: Ronald J. Biediger, Michele A. Benish, Robert V. Market, Michael M. Savage, Brandon M. Young
  • Patent number: 10407509
    Abstract: The invention provides to NTRK (“Neurotrophic Tyrosine Receptor Kinase) gene fusions, NTRK, fusion proteins, and fragments of those genes and polypeptides. The invention further provides methods of diagnosing and treating diseases or disorders associated with NTRK fusions, such as conditions mediated by aberrant NTRK expression or activity, or overexpression of NTRK.
    Type: Grant
    Filed: July 30, 2014
    Date of Patent: September 10, 2019
    Assignee: Blueprint Medicines Corporation
    Inventors: Nicolas Stransky, Ethan G. Cerami, Christoph Lengauer
  • Patent number: 10246451
    Abstract: Provided herein are compounds and pharmaceutical compositions of formula I where R1, R2, R3, R4, R5, X and R6 are as described herein. Also provided pharmaceutically acceptable salts or stereoisomer(s) of these compounds. In addition methods are provided for antagonizing the action of an ?4-integrin to treat various pathophysiological conditions.
    Type: Grant
    Filed: April 26, 2017
    Date of Patent: April 2, 2019
    Assignee: Aviara Pharmaceuticals, Inc.
    Inventors: Ronald J. Biediger, Michele A. Benish, Robert V. Market, Michael M. Savage, Brandon M. Young
  • Patent number: 9751837
    Abstract: There are provided compounds of formula I, wherein R1A to R1E, R2 to R4, R5a, L and X1 to X3 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: September 5, 2017
    Assignees: RESPIVERT LIMITED, TOPIVERT PHARMA LIMITED
    Inventors: Thomas Matthew Baker, Matthew Colin Thor Fyfe, Geraint Jones, Stephen Malcolm Thom
  • Patent number: 9370507
    Abstract: The invention provides pyridonyl guanidine compounds that inhibit F1F0-ATPase, and methods of using pyridonyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Grant
    Filed: April 1, 2015
    Date of Patent: June 21, 2016
    Assignee: Lycera Corporation
    Inventors: Gary D. Glick, Alexander R. Hurd, Matthew N. Mattson, Clarke B. Taylor, Chad A. Van Huis
  • Patent number: 9102659
    Abstract: Multifunctional nitroxide derivatives comprising a potassium channel opener and a reactive oxygen species (ROS) degradation catalyst that can act as an anti-oxidant, as well as pharmaceutical compositions comprising them are provided. The multifunctional compounds and pharmaceutical compositions are useful for treatment of diseases, disorders or conditions associated with oxidative stress or endothelial dysfunction.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: August 11, 2015
    Assignee: RADIKAL THERAPEUTICS INC.
    Inventors: Prakash Jagtap, Andrew Lurie Salzman
  • Publication number: 20150141465
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 21, 2015
    Inventors: Calvin W. YEE, Zhe Li
  • Publication number: 20150133407
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of respiratory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of viscid or excessive mucus, cough, inflammation, redness in sore throat, infection in the throat, sore throat, abnormal mucus secretion, impaired mucus transport, allergic rhinitis, asthma, COPD, respiratory muscular disorders and pain in acute sore throat.
    Type: Application
    Filed: May 14, 2013
    Publication date: May 14, 2015
    Inventor: Mahesh Kandula
  • 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
  • Patent number: 9000014
    Abstract: The invention provides pyridonyl guanidine compounds that inhibit F1F0-ATPase, and methods of using pyridonyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: April 7, 2015
    Assignee: Lycera Corporation
    Inventors: Gary D. Glick, Alexander R. Hurd, Matthew N. Mattson, Clarke B. Taylor, Chad A. Van Huis
  • Publication number: 20150094310
    Abstract: The present invention relates to a corticotropin releasing hormone receptor type 1 (CRHR1) antagonist for use in the treatment of depressive symptoms and/or anxiety symptoms in a novel group of patients, i.e. patients having corticotropin releasing hormone (CRH) overactivity.
    Type: Application
    Filed: April 23, 2013
    Publication date: April 2, 2015
    Inventor: Florian Holsboer
  • Patent number: 8993630
    Abstract: The present invention relates to substituted sulphonamido phenoxybenzamide compounds of general formula (I): in which A, R1, R2, R3, R4, R5, R6, R7, R8 and n are as defined in the claims, to pharmaceutical compositions and combinations containing said compounds, to methods of preparing said compounds, and to the use of said compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: March 31, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Ingo Hartung, Marion Hitchcock, Florian Puhler, Gerhard Siemeister, Roland Neuhaus
  • Patent number: 8981106
    Abstract: There is disclosed pyridine- and pyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include pyridine- and pyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders.
    Type: Grant
    Filed: March 26, 2014
    Date of Patent: March 17, 2015
    Assignee: Syntrix Biosystems, Inc.
    Inventors: Dean Y. Maeda, John A. Zebala
  • Patent number: 8980629
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Grant
    Filed: August 23, 2013
    Date of Patent: March 17, 2015
    Assignee: CalciMedica, Inc.
    Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20150045364
    Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Application
    Filed: October 23, 2014
    Publication date: February 12, 2015
    Applicant: NOVARTIS AG
    Inventors: Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
  • Patent number: 8951999
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: February 10, 2015
    Assignee: Orexo AB
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
  • Patent number: 8946437
    Abstract: The present invention provides a novel compound having an excellent antitumor effect, stability and metabolic stability. The compound of the present invention is represented by the following general formula (1) wherein R1 represents a halogen atom, an aryl group, an aryloxy group or a lower alkyl group optionally substituted with one or more halogen atoms; R2 represents hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; and; m represents an integer of 1 to 3; provided that when m represents 2 or 3, R1s are the same or different.
    Type: Grant
    Filed: October 3, 2011
    Date of Patent: February 3, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Takashi Nakagawa, Makoto Sakamoto, Kazuya Yamaguchi, Yuki Terauchi, Masamichi Shirakura, Yasuo Harada, Yutaka Kojima, Takumi Sumida
  • Patent number: 8937096
    Abstract: The present invention is a method for the treatment of mania and/or bipolar disorder comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as herein defined.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: January 20, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Virginia L. Smith-Swintosky, Allen B. Reitz
  • Publication number: 20140371229
    Abstract: The present invention relates to compositions and methods for the treatment of Parkinson's disease and related disorders. More specifically, the present invention relates to novel combinatorial therapies of Parkinson's disease and related disorders targeting the alpha-synuclein aggregation network. In particular, the invention relates to compounds which, alone or in combination(s), can effectively protect neuronal cells from alpha-synuclein aggregates. The invention also relates to methods of producing a drug or a drug combination for treating Parkinson's disease and to methods of treating Parkinson's disease or a related disorder.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Inventors: DANIEL COHEN, SERGUEI NABIROCHKIN, ILYA CHUMAKOV, RODOLPHE HAJJ
  • Publication number: 20140371277
    Abstract: The present invention relates to compositions and methods for the treatment of amyotrophic lateral sclerosis. More specifically, the present invention relates to novel combinatorial therapies for treating amyotrophic lateral sclerosis or a related disorder.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Inventors: DANIEL COHEN, SERGUEI NABIROCHKIN, ILYA CHUMAKOV, RODOLPHE HAJJ
  • Publication number: 20140343000
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 20, 2014
    Inventors: Alicia Regueiro-Ren, Zheng Liu, Jacob Swidorski, Ny Sin, Brian Lee Venables, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell
  • Publication number: 20140336227
    Abstract: Compounds, pharmaceutical compositions of general formula (I) or (I?) or a pharmaceutically acceptable salt thereof, and methods for treating an inflammatory disorder: wherein: z is 1, 2 or 4; X is —CO—Yk—(R1)n; k is 0 or 1; Y is a cycloalkyl or polycycloalkyl, cycloalkenyl or polycycloalkenyl group; each R1 is a branched chain alkyl group; n is any integer from 1 to m, where m is the maximum number of substitutions permissible on the cyclo-group Y; and the compound comprises an amino lactam ring linked to an alkyl group —Yk—(R1)n by an amide group, wherein the carbon atom in the alkyl group at the 2-position relative to the carbon atom of the amide carbonyl is linked to each of the carbon atom of the amide carbonyl and three other carbon atoms by a single bond, and wherein the 2-position carbon atom has essentially tetrahedral bond angles.
    Type: Application
    Filed: November 4, 2013
    Publication date: November 13, 2014
    Applicant: CAMBRIDGE ENTERPRISE LIMITED
    Inventors: David J Grainger, David John Fox
  • Publication number: 20140335201
    Abstract: The present invention provides a composition comprising a combination of components A) and B), wherein component A) is a compound of formula (I) and the component (B) is a further fungicide, insecticide or herbicide.
    Type: Application
    Filed: April 9, 2012
    Publication date: November 13, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Ulrich Johannes Haas, Dietrich Hermann, Gabriel Didier Scalliet, Kurt Nebel, Long Lu, Jianzhong Yang, Qiang Lu, Thomas James Hoffman, Renaud Beaudegnies, Werner Zambach, Olivier Jacob
  • Publication number: 20140329867
    Abstract: The present invention relates to use of inhibitors of Notch signalling pathway selected from the group consisting of 6-(4-Tert-Butylphenoxy)Pyridin-3-Amine (I3), its derivatives, in treating and/or preventing cancers.
    Type: Application
    Filed: December 21, 2012
    Publication date: November 6, 2014
    Applicant: Ecole Polytechnique Federale de Lausanne
    Inventors: Freddy Radtke, Rajwinder Lehal, Viktoria Reinmuller, Jieping Zhu
  • Publication number: 20140288086
    Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.
    Type: Application
    Filed: June 6, 2014
    Publication date: September 25, 2014
    Applicants: PFIZER INC., AGOURON PHARMACEUTICALS, INC.
    Inventors: Jingrong Jean CUI, Lee Andrew FUNK, Lei JIA, Pei-Pei KUNG, Jerry Jialun MENG, Mitchell David NAMBU, Mason Alan PAIRISH, Hong SHEN, Michelle TRAN-DUBE
  • Publication number: 20140243337
    Abstract: The invention provides certain phenyl carboxamide-containing compounds of the Formula (I); or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: October 1, 2012
    Publication date: August 28, 2014
    Inventors: Michael D. Altman, Maria Emilia Di Francesco, John Michael Ellis, Sandra Lee Knowles, Alan B. Northrup
  • Publication number: 20140213589
    Abstract: The invention relates to hydroxyphenyl derivatives of formula (I); and uses thereof as anti-bacterial and/or anti-parasitic agents.
    Type: Application
    Filed: March 28, 2014
    Publication date: July 31, 2014
    Applicant: FAB PHARMA S.A.S.
    Inventors: Alexis DENIS, Vincent Gerusz, Yannick Bonvin
  • Publication number: 20140206727
    Abstract: A compound represented by Formula (1): The compound can be used as insecticides.
    Type: Application
    Filed: March 20, 2014
    Publication date: July 24, 2014
    Applicant: MITSUI CHEMICALS, INC.
    Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
  • Patent number: 8785632
    Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: July 22, 2014
    Assignees: Agouron Pharmaceuticals, Inc., Pfizer Inc.
    Inventors: Jingrong Jean Cui, Lee Andrew Funk, Lei Jia, Pei-Pei Kung, Jerry Jialun Meng, Mitchell David Nambu, Mason Alan Pairish, Hong Shen, Michelle Tran-Dube
  • Publication number: 20140200225
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 17, 2014
    Applicant: ORION CORPORATION
    Inventors: Rajeev GOSWAMI, Anil Kumar VUPPALA, Ramesh VELUDANDI, Ramesh SISTLA, Chakshusmathi GHADIYARAM, Muralidhara RAMACHANDRA
  • Patent number: 8779149
    Abstract: There is disclosed aminopyridine- and aminopyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include aminopyridine- and aminopyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: July 15, 2014
    Assignee: Syntrix Biosystems, Inc.
    Inventors: Dean Y. Maeda, John A. Zebala, Aaron D. Schuler
  • Publication number: 20140194405
    Abstract: The disclosed compounds are useful in the treatment of mammalian cancers and especially human cancers. Compounds, pharmaceutical compositions, and methods of Formula I are disclosed: or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, stereoisomer, or tautomer thereof.
    Type: Application
    Filed: December 20, 2013
    Publication date: July 10, 2014
    Applicant: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Michael D. Kaufman
  • Patent number: 8765776
    Abstract: Provided is an antihypertensive pharmaceutical composition containing Fimasartan, a pharmaceutically acceptable salt thereof, a solvate thereof or a hydrate thereof as an angiotensin II receptor blocker, and Amlodipine, an isomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof or a hydrate thereof as a calcium channel blocker.
    Type: Grant
    Filed: August 8, 2011
    Date of Patent: July 1, 2014
    Assignee: Boryung Pharmaceutical Co., Ltd.
    Inventors: Seung Ho Kim, Ji Han Kim, Je Hak Kim, Kyung Wan Nam, Yong Ha Chi, Joo Han Lee, Soo Heui Paik, So Jeong Yi, Tae Eun Kim, Seo Hyun Yoon, Joo Youn Cho, Sang Goo Shin, In Jin Jang, Kyung Sang Yu
  • Publication number: 20140162983
    Abstract: The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.
    Type: Application
    Filed: June 10, 2012
    Publication date: June 12, 2014
    Applicant: Merck Patent GmbH
    Inventors: Brian L. Hodous, Lesley Liu-Bujalski, Reinaldo Jones, Donald Bankston, Theresa L. Johnson, Igor Mochalkin, Ngan Nguyen, Hui Qiu, Andreas Goutopoulos, Nadia Brugger
  • Patent number: 8748623
    Abstract: There is disclosed pyridine-and pyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include pyridine-and pyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders.
    Type: Grant
    Filed: February 17, 2010
    Date of Patent: June 10, 2014
    Assignee: Syntrix Biosystems, Inc.
    Inventors: Dean Y. Maeda, John A. Zebala
  • Publication number: 20140135298
    Abstract: This invention is in the fields of cancer therapy. More particularly it concerns compounds which are useful agents for treating cell proliferative disorders, especially those disorders characterized by over activity and/or inappropriate activity of a EGFR, including EGFR-related cancers, particularly for expanding the efficacy of drugs previously developed for this purpose, and for methods of treatments using the compounds for this purpose.
    Type: Application
    Filed: March 16, 2012
    Publication date: May 15, 2014
    Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventors: Alan Berezov, Mark I. Greene, Natalie Minkovsky, Zheng Cai, Hongtao Zhang
  • Publication number: 20140135329
    Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Application
    Filed: June 20, 2013
    Publication date: May 15, 2014
    Inventors: Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
  • Patent number: 8722930
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: May 13, 2014
    Assignee: Orion Corporation
    Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
  • Patent number: 8716318
    Abstract: This invention concerns N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: May 6, 2014
    Assignee: Ardea Biosciences
    Inventors: Shunqi Yan, Jean-Michel Vernier, Zhi Hong, Suetying Chow, Yung-hyo Koh
  • Publication number: 20140088159
    Abstract: Covalent conjugates of an ?,?-disubstituted glycine ester and 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 and the ?,?-disubstituted glycine ester is conjugated to the modulator at a position remote from the binding interface between the inhibitor and the target enzyme or receptor pass into cells and the active acid hydrolysis product accumulates within the cells.
    Type: Application
    Filed: November 27, 2013
    Publication date: March 27, 2014
    Applicant: Chroma Therapeutics Ltd.
    Inventors: Alan Hastings Drummond, Alan Hornsby Davidson, David Festus Charles Moffat, Alastair David Graham Donald, Stephen John Davies
  • Publication number: 20140088105
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.
    Type: Application
    Filed: November 22, 2013
    Publication date: March 27, 2014
    Applicant: NOVARTIS AG
    Inventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
  • Patent number: 8673919
    Abstract: This invention concerns N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: March 18, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Jean-Michel Vernier, Hong Woo Kim, Marion Hitchcock, Shunqi Yan
  • Patent number: 8669209
    Abstract: Soluble granule formulations of amine salts of pyridine containing carboxylic acids with improved handling properties are provided by an improved process in which the pyridine containing carboxylic acid is partially neutralized with an amine.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: March 11, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Franklin N. Keeney, Neil A. Foster, Martin C. Logan, Maria G. Perry
  • Patent number: 8658791
    Abstract: 6-Amino-4-pyrimidinecarboxylic acids having alkyl, alkenyl or alkynyl substituents in the 5-position and 4-aminopicolinic acids having alkyl, alkenyl or alkynyl substituents in the 3-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: February 25, 2014
    Assignee: Dow AgroSciences, LLC
    Inventors: Jeffrey B. Epp, Paul R. Schmitzer, Terry W. Balko, Carla N. Yerkes
  • Publication number: 20140038963
    Abstract: The present disclosure provides methods for identifying therapeutic agents that are multifunctional radical quenchers. It also provides compounds of formula (I), (II), or (II-A): and pharmaceutically acceptable salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.
    Type: Application
    Filed: April 4, 2012
    Publication date: February 6, 2014
    Inventors: Sidney Hecht, Omar Khdour, Sandipan Roy Chowdhury, Poulami Talukder
  • Patent number: 8642278
    Abstract: The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.
    Type: Grant
    Filed: November 22, 2006
    Date of Patent: February 4, 2014
    Assignee: University of South Florida
    Inventors: Said M. Sebti, Srikumar Chellappan, Nicholas James Lawrence
  • Publication number: 20140031348
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.
    Type: Application
    Filed: July 9, 2013
    Publication date: January 30, 2014
    Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M.K. Pennell, John J. Wright
  • Publication number: 20140031395
    Abstract: The present invention relates to compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of ?7nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also inflammatory diseases.
    Type: Application
    Filed: February 2, 2012
    Publication date: January 30, 2014
    Applicant: Bionomics Limited
    Inventors: Andrew Harvey, Audrey Fluck, Bruno Giethlen, Dharam Paul, Laurent Schaeffer