Acyclic Nitrogen Bonded Directly To The -c(=x)- Group Patents (Class 546/169)
  • Patent number: 10080753
    Abstract: The invention provides novel heterocyclic carboxamide compounds according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: August 3, 2016
    Date of Patent: September 25, 2018
    Assignee: Merck Patent GmbH
    Inventors: Bayard R. Huck, Xiaoling Chen, Yufang Xiao, Ruoxi Lan, Lizbeth Celeste De Selm, Constantin Neagu, Justin Potnick, Srinivasa R. Karra, Theresa L Johnson
  • Patent number: 9686986
    Abstract: The present invention relates to a method of controlling weeds at a locus, said method comprising application to the locus of a weed controlling amount of a herbicidal composition comprising a compound of Formula (I), or an agronomically acceptable salt of said compounds wherein X, R1, R2, R4 and R5 are as defined herein. The invention further relates novel herbicidal compounds, to herbicidal compositions comprising said compounds and to their use for controlling weeds, in particular in crops of useful plants.
    Type: Grant
    Filed: May 9, 2016
    Date of Patent: June 27, 2017
    Assignee: Syngenta Limited
    Inventors: Alison Clare Elliott, Glynn Mitchell
  • Patent number: 9452986
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein R1, R2, and R3 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by voltage-gated sodium channels, e.g., Nav1.7 and/or Nav1.8. Methods for making the compounds are disclosed. Also disclosed are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
    Type: Grant
    Filed: February 4, 2015
    Date of Patent: September 27, 2016
    Assignee: AbbVie Inc.
    Inventors: Andrew Bogdan, Marlon D. Cowart, David A. DeGoey, Tammie K. Jinkerson, John R. Koenig, Michael E. Kort, Bo Liu, Mark A. Matulenko, Derek W. Nelson, Meena V. Patel, Hillary Peltier, Marc J. Scanio, Brian D. Wakefield
  • Patent number: 9375012
    Abstract: The present invention relates to a method of controlling weeds at a locus, said method comprising application to the locus of a weed controlling amount of a herbicidal composition comprising a compound of Formula (I), or an agronomically acceptable salt of said compounds wherein X, R1, R2, R4 and R5 are as defined herein. The invention further relates novel herbicidal compounds, to herbicidal compositions comprising said compounds and to their use for controlling weeds, in particular in crops of useful plants.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: June 28, 2016
    Inventors: Glynn Mitchell, Alison Clare Elliott
  • Patent number: 9346821
    Abstract: The present invention provides a blood glucose elevation inhibitor having a serine protease inhibitory action, which is a novel therapeutic or prophylactic agent for obesity. A compound represented by the following formula (I) wherein each symbol is as described in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: May 24, 2016
    Assignee: AJINOMOTO CO., INC.
    Inventors: Tamotsu Suzuki, Takahiro Koshiba, Munetaka Tokumasu, Koji Ohsumi
  • Patent number: 9040553
    Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: May 26, 2015
    Assignee: CELL VIABLE CORPORATION
    Inventors: Iraj Lalezari, Jill Fabricant
  • Patent number: 9023340
    Abstract: Methods and small molecule compounds for stem cell differentiation and treatment of animals with diseases are provided. One example of a class of compounds that may be used is represented by the compound of Formula I and II: or a pharmaceutically acceptable salt or solvate thereof, wherein A, X, Q, R1, R2, R3, R4 are as described herein.
    Type: Grant
    Filed: July 2, 2012
    Date of Patent: May 5, 2015
    Assignee: ChemRegen, Inc.
    Inventors: John Cashman, Marion Lanier, Mark Mercola, Dennis Schade, Erik Willems
  • Publication number: 20150111750
    Abstract: N-(tetrazol-5-yl)- and N-(triazol-5-yl)hetarylcarboxamides of formula I and their use as herbicides. The invention relates to N-(tetrazol-5-yl)- and N-(triazol-5-yl)hetarylcarboxamides of formula I and their use as herbicides. In said formula I, B represents N or CH, whereas X1 is N or CR1, X2 is N or CR2, X3 is N or CR3 and X4 is N or CR4; provided that a least one of X1, X3 and X4 is N; R, R1, R2, R3, R4 and R5 represent groups such as hydrogen, halogen or organic groups such as alkyl or phenyl.
    Type: Application
    Filed: April 16, 2013
    Publication date: April 23, 2015
    Inventors: Helmut Kraus, Matthias Witschel, Thomas Seitz, Trevor William Newton, Liliana Parra Rapado, Klaus Kreuz, Johannes Hutzler, Maciej Pasternak, Jens Lerchl, Richard Roger Evans
  • Publication number: 20150073016
    Abstract: The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR.
    Type: Application
    Filed: April 30, 2013
    Publication date: March 12, 2015
    Inventors: Anderson GAWECO, Jefferson TILLEY, John WALKER, Samantha PALMER, James BLINN
  • 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: 8940765
    Abstract: The present invention is directed to N-linked quinoline amide compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: May 11, 2012
    Date of Patent: January 27, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Christina Ng DiMarco, Zhi-Qiang Yang
  • Publication number: 20140378459
    Abstract: [Problem] Provided is a compound which is useful as an agent for preventing and/or treating renal diseases. [Means for Solution] The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.
    Type: Application
    Filed: September 14, 2012
    Publication date: December 25, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Jiro Fujiyasu, Kazuhiko Ohne, Susumu Yamaki, Tomoyoshi Imaizumi, Takeshi Hondo, Keisuke Matsuura, Tomohki Satou, Satoshi Sasamura
  • Publication number: 20140378429
    Abstract: The disclosure relates particularly to certain carboxamide, sulfonamide and amine compounds and pharmaceutical compositions thereof, and to methods of treating and ameliorating disorders and conditions related to the adiponectin pathway, sphingolipid metabolism, oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. In certain embodiments, the compounds have the structures (I-1), (2-I) and (3-I) (The chemical formulas should be inserted here) in which the variables are as described herein.
    Type: Application
    Filed: January 31, 2013
    Publication date: December 25, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, David Carroll, Simon Shaw, Hitoshi Yasumichi
  • Publication number: 20140364433
    Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 11, 2014
    Inventors: Theodore M. KAMENECKA, Yuanjun HE, Rong JIANG, William NGUYEN, Xinyi SONG
  • Publication number: 20140364432
    Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
    Type: Application
    Filed: February 12, 2014
    Publication date: December 11, 2014
    Inventors: Theodore M. KAMENECKA, Yuanjun HE, William NGUYEN, Rong Jiang, Xinyi Song
  • Publication number: 20140357650
    Abstract: The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.
    Type: Application
    Filed: January 17, 2013
    Publication date: December 4, 2014
    Applicant: Fox Chase Cancer Center
    Inventors: Koen Jansen, Ingrid De Meester, Leen Heirbaut, Jonathan D. Cheng, Jurgen Joossens, Koen Augustyns, Pieter Van Der Veken
  • Publication number: 20140350263
    Abstract: Reagents comprising MS active, fluorescent molecules with an activated functionality for reaction with amines useful in tagging biomolecules such as N-glycans and uses thereof are taught and described.
    Type: Application
    Filed: August 13, 2014
    Publication date: November 27, 2014
    Applicant: WATERS TECHNOLOGIES CORPORATION
    Inventors: Darryl W. Brousmiche, Ying-Qing Yu, Matthew Lauber
  • Publication number: 20140350045
    Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
    Type: Application
    Filed: July 11, 2013
    Publication date: November 27, 2014
    Inventors: IRAJ LALEZARI, JILL FABRICANT
  • Publication number: 20140336377
    Abstract: The present invention relates to arylamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Application
    Filed: October 18, 2011
    Publication date: November 13, 2014
    Applicant: RAQUALIA PHARMA INC.
    Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Yoshimasa Arano, Mikio Morita
  • Publication number: 20140336221
    Abstract: This invention provides a family of compounds that inhibit Class II fructose 1,6-bisphosphate aldolase (FBA), which is implicated in the pathogenic activity of a broad range of bacterial and parasitic agents. The compounds were identified by empirical testing, and provide a basis for further derivatization and optimization of 8-hydroxyquinoline-2-carboxylic acid and related compounds. Crystal structure shows that the compounds don't bind directly to the catalytic site of the enzyme, and so are not defined simply as substrate analogs. Instead, they create a pocket by induced fit, resulting a powerful and specific inhibitory effect on FBA activity.
    Type: Application
    Filed: May 8, 2014
    Publication date: November 13, 2014
    Applicants: Colorado Seminary, Which Owns and Operates The University Of Denver, Regis University
    Inventors: Scott Dusan Pegan, Kateri Ahrendt, Glenn C. Capodagli, Bryan Cowen
  • Publication number: 20140329854
    Abstract: Provided are novel heterocyclic sirtuin binding agents, e.g., N-aryl substituted pyridine dicarboxamides, which are useful as sirtuin modulators. Also provided are methods of using the pyridine dicarboxamide compounds for treating sirtuin mediated disorders and conditions, such as diabetes, cancers, and obesity and diseases related to aging.
    Type: Application
    Filed: December 12, 2012
    Publication date: November 6, 2014
    Applicant: SMB Innovation
    Inventors: Bjarne Due Larsen, Soren Andersen, Marianne Spanget Larsen
  • Patent number: 8877780
    Abstract: This invention relates to 5-substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Grant
    Filed: May 30, 2008
    Date of Patent: November 4, 2014
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Roger Shen-Chu Chen, Alexander L. Ruchelman, Hon-Wah Man, Weihong Zhang, Ehab M. Khalil
  • Patent number: 8877778
    Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, x, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
    Type: Grant
    Filed: December 7, 2011
    Date of Patent: November 4, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
  • Publication number: 20140315944
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, Y, and n have any of the values described herein and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting MAO, and MAO-B selectively, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders (including obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.
    Type: Application
    Filed: March 11, 2014
    Publication date: October 23, 2014
    Inventors: Jillian Basinger, James Breitenbucher, Graeme Freestone, Varsha Gupta, Alan Kaplan, Chi-Ching Mak, Benjamin Pratt, Vincent Santora, Dipanjan Sengupta, Lino Valdez
  • Patent number: 8865742
    Abstract: The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes.
    Type: Grant
    Filed: November 28, 2011
    Date of Patent: October 21, 2014
    Assignee: Mapi Pharma Ltd.
    Inventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov
  • Publication number: 20140309227
    Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Inventors: Christopher James Bungard, Antonella Converso, Pablo De Leon, Barbara Hanney, Timothy John Hartingh, Jesse Josef Manikowski, Peter J. Manley, Robert Meissner, Zhaoyang Meng, James J. Perkins, Michael T. Rudd, Youheng Shu
  • Publication number: 20140309245
    Abstract: The invention provides novel heterocyclic carboxamide compounds compounds according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Application
    Filed: December 17, 2012
    Publication date: October 16, 2014
    Inventors: Bayard R. Huck, Xiaoling Chen, Yufang Xiao, Ruoxi Lan, Lizbeth Celeste De Selm, Constantin Neagu, Justin Potnick, Srinivasa R. Karra, Theresa L. Johnson
  • Publication number: 20140309116
    Abstract: The present invention relates to substituted 1,2,5-oxadiazole compounds of the formula (I) and the N-oxides and salts thereof and to compositions comprising the same. The invention also relates to the use of the 1,2,5-oxadiazole compounds or of the compositions comprising such compounds for controlling unwanted vegetation. Furthermore, the invention relates to methods of applying such compounds.
    Type: Application
    Filed: November 15, 2012
    Publication date: October 16, 2014
    Applicant: BASF SE
    Inventors: Helmut Kraus, Matthias Witschel, Thomas Seitz, Trevor William Newton, Liliana Parra Rapado, Raphael Aponte, Klaus Kreuz, Klaus Grossmann, Jens Lerchl, Richard Roger Evans
  • Publication number: 20140309115
    Abstract: The present invention relates to substituted 1,2,5-oxadiazole compounds of the formula I and the N-oxides and salts thereof and to compositions comprising the same. The invention also relates to the use of the 1,2,5-oxadiazole compounds or of the compositions comprising such compounds for controlling unwanted vegetation. wherein X1 is N or CR1; X2 is N or CR2; X4 is N or CR4; provided that a least one of X1, X2 and X4 is N; R is e.g. selected from the group consisting of hydrogen, cyano, nitro, halogen, C1-C6-alkyl, C3-C7-cycloalkyl, C3-C7-cycloalkyl-C1-C4-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-haloalkenyl, C2-C6-alkynyl, C2-C6-haloalkynyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-haloalkoxy-C1-C4-alkyl, O—Ra, Z—S(O)n—Rb, Z—C(?O)—Rc, Z—C(?O)—ORd, Z—C(?O)—NReRf, Z—NRgRh, Z-phenyl and Z-heterocyclyl; R1 is e.g.
    Type: Application
    Filed: November 16, 2012
    Publication date: October 16, 2014
    Applicant: BASF SE
    Inventors: Helmut Kraus, Matthias Witschel, Thomas Seitz, Trevor William Newton, Liliana Parra Rapado, Raphael Aponte, Klaus Kreuz, Klaus Grossmann, Jens Lerchl, Richard Roger Evans
  • Publication number: 20140302069
    Abstract: Heterocyclic compounds that modulate C3a receptors and their use in the treatment or prevention of inflammatory diseases, infectious diseases, cancers, metabolic disorders, obesity, type 2 diabetes, metabolic syndrome and associated cardiovascular diseases are described. The use of the compounds in stimulating or suppressing an immune response is also described together with pharmaceutical compositions comprising the compounds or their pharmaceutically acceptable salts.
    Type: Application
    Filed: November 7, 2012
    Publication date: October 9, 2014
    Inventors: David Fairlie, Robert C. Reid
  • Patent number: 8853242
    Abstract: [Object] An excellent agent for preventing or treating dementia, schizophrenia, and the like, based on serotonin 5-HT5A receptor modulating action, is provided. [Means for Solution] It was confirmed that acylguanidine derivatives (the following formula I; any one of Z1, Z2, Z3, Z4 and Z5 is nitrogen atom, and the others are carbon atoms) which have the characteristic structure in which the guanidine is bonded to one ring of the quinoline or isoquinoline via a carbonyl group, and a cyclic group is bonded to the other ring, exhibit potent 5-HT5A receptor modulating actions and excellent pharmacological actions based on the 5-HT5A receptor modulating action, and thus can be excellent agents for preventing or treating dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder. Thus, the present invention has been completed.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: October 7, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Isao Kinoyama, Takehiro Miyazaki, Yohei Koganemaru, Takuya Washio, Wataru Hamaguchi
  • Publication number: 20140275548
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, Y, and n have any of the values described herein and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting MAO, and MAO-B selectively, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating treating peripheral disorders (including obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Inventors: Jillian Basinger, James Breitenbucher, Graeme Freestone, Varsha Gupta, Alan Kaplan, Chi-Ching Mak, Benjamin Pratt, Vincent Santora, Dipanjan Sengupta, Lino Valdez
  • Patent number: 8822691
    Abstract: To provide novel carboxamides which exhibit an excellent pesticidal activity as pesticides. Carboxamides represented by the following Formula (I) and use thereof as pesticides and an animal parasite control agent: wherein each substituent is as defined in the specification.
    Type: Grant
    Filed: July 10, 2010
    Date of Patent: September 2, 2014
    Assignee: Bayer CropScience AG
    Inventors: Jun Mihara, Koichi Araki, Takuma Mori, Tetsuya Murata, Yasushi Yoneta, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Görgens
  • Patent number: 8815902
    Abstract: The present invention is directed to tetrahydroquinoline amide compounds of formula (I) (Formula should be inserted here) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: June 10, 2011
    Date of Patent: August 26, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin F. Gilbert, Scott D. Kuduk
  • Publication number: 20140235548
    Abstract: Compounds, pharmaceutical compositions, and methods of using such compounds to treat or prevent diseases or disorders associated with or mediated by JAMM proteins are disclosed. The compounds and compositions inhibit the enzymatic activity of a JAMM domain, including the JAMM domain of the CSN5 subunit of the COP9-signalsome (CSN), the JAMM domain of the Rpn11/Poh1/Psmd14 subunit of the 26S proteasome, the JAMM domain of AMSH, the JAMM domain of AMSH-LP, the JAMM domain of BRCC36, among other JAMM domains.
    Type: Application
    Filed: May 10, 2012
    Publication date: August 21, 2014
    Applicant: Cleave Biosciences, Inc.
    Inventors: Han-Jie Zhou, Francesco Parlati, Matthieu Roufflet, Ethan D. Emberley, Raymond J. Deshaies, Seth Cohen
  • Publication number: 20140227320
    Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.
    Type: Application
    Filed: September 27, 2012
    Publication date: August 14, 2014
    Inventors: Shawn P. Iadonato, Kristin Bedard, Myra Wang Imanaka, Kerry W. Fowler
  • Publication number: 20140213611
    Abstract: The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R1 to R9 are as defined herein.
    Type: Application
    Filed: July 6, 2012
    Publication date: July 31, 2014
    Applicant: KalVista Pharmaceuticals Limited
    Inventors: David Michael Evans, Rebecca Louise Davie, Hannah Joy Edwards, David Philip Rooker
  • Publication number: 20140199348
    Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.
    Type: Application
    Filed: February 12, 2013
    Publication date: July 17, 2014
    Applicant: KINETA, INC.
    Inventors: Shawn P. Iadonato, Kristin M. Bedard, Ernesto J. Muñoz, Myra W. Imanaka, Kerry W. Fowler
  • Publication number: 20140200222
    Abstract: The present invention is directed to N-linked quinoline amide compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: May 11, 2012
    Publication date: July 17, 2014
    Inventors: Scott D. Kuduk, Christina Ng DiMarco, Zhi-Qiang Yang
  • Publication number: 20140179011
    Abstract: Reagents comprising MS active, fluorescent molecules with an activated functionality for reaction with amines useful in tagging biomolecules such as N-glycans and uses thereof are taught and described.
    Type: Application
    Filed: February 28, 2014
    Publication date: June 26, 2014
    Applicant: Waters Technologies Corporation
    Inventors: Darryl W. Brousmiche, Ying-Qing Yu
  • Patent number: 8759539
    Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
  • Publication number: 20140171639
    Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: February 24, 2014
    Publication date: June 19, 2014
    Applicant: AMGEN INC.
    Inventors: Kaustav Biswas, James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Vu Van Ma, Holger Monenschein, Thomas T. Nguyen, David J. St. Jean, JR., Chester Chenguang Yuan, Wenge Zhong
  • Publication number: 20140142137
    Abstract: Provided herein, inter alia, are novel compounds for the inhibition of HIV integrase. The compounds disclosed herein are useful for methods of treating HIV infection in a subject in need thereof.
    Type: Application
    Filed: August 2, 2013
    Publication date: May 22, 2014
    Applicants: National Institutes of Health, The Regents of the University of California
    Inventors: Seth M. Cohen, Arpita Agrawal, Jamie DeSoto, Yves Pommier, Kasthuraiah Maddali
  • Publication number: 20140128391
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.
    Type: Application
    Filed: November 1, 2013
    Publication date: May 8, 2014
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Publication number: 20140128427
    Abstract: Provided are a novel derivative of 5-carbamoyl adamantan-2-yl amide or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof for inhibiting the activity of 11?-hydroxystreroid dehydrogenase type 1 (11b-HSD1) or for preventing and/or treating various diseases mediated by 11?-hydroxystreroid dehydrogenase type 1.
    Type: Application
    Filed: June 11, 2012
    Publication date: May 8, 2014
    Applicant: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Coo-Min Chung, Choon-Ho Ryu, Yoon-Kyeong Lee, Jin-Sook Moon, Hye-Sung Lee, Seon-Jeong Lee, Kyung-Seok Oh
  • Patent number: 8710043
    Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Grant
    Filed: June 21, 2012
    Date of Patent: April 29, 2014
    Assignee: Amgen Inc.
    Inventors: Jian J. Chen, Daniel B. Horne, Matthew R. Kaller, Vu Van Ma
  • Publication number: 20140114068
    Abstract: Disclosed are novel indanone derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The indanone derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.
    Type: Application
    Filed: June 18, 2012
    Publication date: April 24, 2014
    Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN K.U. LEUVEN R & D, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Young Sik Jung, Chong Kgo Lee, Hae Soo Kim, Hee Chun Jeong, Pil Ho Kim, Soo Bong Han, Jin Soo Shin, Johan Neyts, Hendrik Jan Thibaut
  • Publication number: 20140107153
    Abstract: Disclosed herein is a stable compound having a structure: therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Application
    Filed: December 13, 2013
    Publication date: April 17, 2014
    Applicant: Allergan, Inc.
    Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello, Michael E. Garst
  • Publication number: 20140107094
    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 17, 2014
    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, Joan Pierce, Steven Goldberg, Anne Fourie, Xiaohua Xue
  • Patent number: 8669246
    Abstract: A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula: In this formula, A is an optionally substituted aryl, etc.; B is an optionally substituted 5-membered aromatic hetero ring group; X is a single bond or —(CRX1RX2)n—; n is 1, 2, 3, or 4; RX1 and RX2 are hydrogen, etc.; Y1 to Y5 are each CRY or N; each RY is hydrogen, etc.; R1 and R2 are hydrogen, etc.; m is 1, 2, or 3; R3 is hydrogen, etc.; and R4 is an optionally substituted lower alkyl, etc.
    Type: Grant
    Filed: September 24, 2010
    Date of Patent: March 11, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Eiji Kawaminami, Tatsuhisa Takahashi, Takatoshi Kanayama, Yuta Fukuda, Hiroyuki Kaizawa, Yutaka Kondoh, Ryushi Seo, Kazuyuki Kuramoto, Kazuhiko Take, Kazuyuki Sakamoto