Quinolines (including Hydrogenated) Patents (Class 546/152)
  • Patent number: 10301284
    Abstract: Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for inhibiting plasma kallikrein. Furthermore, the subject compounds and compositions are useful for the treatment of diseases wherein the inhibition of plasma kallikrein inhibition has been implicated, such as angioedema and the like.
    Type: Grant
    Filed: June 22, 2018
    Date of Patent: May 28, 2019
    Assignee: LIFESCI PHARMACEUTICALS, INC.
    Inventors: Andrew McDonald, Shawn Qian
  • Patent number: 10173984
    Abstract: Disclosed herein, inter alia, are compositions and methods for inhibiting DNA2.
    Type: Grant
    Filed: January 9, 2018
    Date of Patent: January 8, 2019
    Assignee: City of Hope
    Inventors: Binghui Shen, Judith Campbell, Li Zheng, Hongzhi Li, David Horne, Jun Xie, Kenneth Karanja
  • Patent number: 10118915
    Abstract: The invention provides novel ligands of Kappa (?) opioid receptors, such as can be used to modulate a Kappa opioid receptor. Methods of synthesis and methods of use are also provided. Compounds of the invention can be used therapeutically in the treatment of dissociative disorders or pain, or to provide neuroprotection, or to induce diuresis, or to modulate the immune system, or for treatment of one or more of an affective disorders comprising depression or stress/anxiety; an addictive disorder; alcoholism, epilepsy; a cognition deficiency; schizophrenia; Alzheimer's disease; or pain.
    Type: Grant
    Filed: May 15, 2017
    Date of Patent: November 6, 2018
    Assignee: The Scripps Research Institute
    Inventors: Edward Roberts, Miguel A. Guerrero, Mariangela Urbano, Hugh Rosen
  • Patent number: 10039764
    Abstract: Disclosed are methods for treating cancer and precancerous conditions with PDE10A specific inhibitors and diagnosis of neoplastic diseases based on elevated levels of PDE10A.
    Type: Grant
    Filed: July 11, 2014
    Date of Patent: August 7, 2018
    Assignee: University of South Alabama
    Inventor: Gary A. Piazza
  • Patent number: 9879026
    Abstract: This invention relates to a compound of formula I wherein A and Cy have one of the meanings as indicated in the specification and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Grant
    Filed: November 29, 2016
    Date of Patent: January 30, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Viktor Vintonyak, Matthias Grauert, Marc Grundl, Alexander Pautsch
  • Patent number: 9771374
    Abstract: Provided herein are compounds of the formulas (I) and (II): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: September 26, 2017
    Assignee: INNOV17 LLC
    Inventors: Anderson Gaweco, Jefferson Tilley, James Blinn
  • Patent number: 9611223
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2/-/-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc.
    Type: Grant
    Filed: September 11, 2014
    Date of Patent: April 4, 2017
    Assignee: INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)
    Inventors: Alan Ashworth, Christopher James Lord, Richard James Rowland Elliott, Dan Niculescu-Duvaz, Roderick Alan Porter, Rehan Aqil, Raymond John Boffey, Melanie Jayne Bayford, Stuart Firth-Clark, Anna Hopkins, Ashley Nicholas Jarvis, Trevor Robert Perrior, Philip Alan Skone, Rebekah Elisabeth Key
  • Patent number: 9440960
    Abstract: This invention relates to a compound of formula I and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Grant
    Filed: July 31, 2015
    Date of Patent: September 13, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Ralf Anderskewitz, Achim Bixenmann, Marc Grundl, Peter Wilhelm Haebel, Alexander Pautsch
  • Patent number: 9217104
    Abstract: This invention relates to compounds of general formula (R?)xZny(L)z(A)n(XR)m, where L is a bi- or multifunctional organic neutral ligand or its deprotonated form, containing at least two heteroatoms selected from N, O, S, wherein at least one of the functional groups of the ligand is selected from —OH, —SH, —NH2, —NHR, —COOH, —CONH2, —CONRH or their deprotonated equivalents; A is an inorganic anion, X is oxygen or sulfur, R? is C1-C10 alkyl, straight or branched, benzyl, phenyl cyclohexyl or halogen, R is hydrogen, alkyl or aryl, x is a number from 0 to 6, y is a number from 1 to 12, z is a number from 1 to 12, n is a number from 0 to 6, m is a number from 0 to 6, wherein x?0, n?0 and m?0 at the same time and if n and m=0, then x?z. The invention also relates to the method of preparation of these compounds and applications thereof.
    Type: Grant
    Filed: July 6, 2011
    Date of Patent: December 22, 2015
    Assignee: Instytut Chemii Fizycznej Polskiejakademii Nauk
    Inventors: Janusz Zbigniew Lewinski, Kamil Sokolowski
  • Patent number: 9073869
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.2]octane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Grant
    Filed: September 11, 2014
    Date of Patent: July 7, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ralf Anderskewitz, Matthias Grauert, Marc Grundl, Thorsten Oost, Alexander Pautsch, Stefan Peters
  • Patent number: 9062048
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R4, J, Q, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: June 23, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui
  • 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
  • Patent number: 8993595
    Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula Ia or Ib, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
    Type: Grant
    Filed: January 10, 2013
    Date of Patent: March 31, 2015
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Christophe Claude Parsy, Francois-Rene Alexandre, Michel Derock, Frederic Leroy, Jean-Christophe Meillon, Thierry Convard, Dominique Surleraux
  • 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
  • Patent number: 8975278
    Abstract: The present invention describes a method for the treatment of a neurological condition in a subject which comprises administering to a subject in need thereof a therapeutically effect amount of a compound of the formula or pharmaceutically acceptable salts, hydrates, or solvates thereof.
    Type: Grant
    Filed: September 19, 2007
    Date of Patent: March 10, 2015
    Assignee: Prana Biotechnology Limited
    Inventors: Kevin Jeffrey Barnham, Elisabeth Colette Louise Gautier, Gaik Beng Kok, Guy Krippner
  • Patent number: 8951831
    Abstract: The present invention relates to a new binaphthalene derivative, a preparation method thereof, and an organic electronic device using the same. The binaphthalene derivative according to the present invention can perform functions of hole injection and transportation, electron injection and transportation, or light emission in an organic electronic device including an organic light-emitting device, and the device according to the present invention has excellent characteristics in terms of efficiency, drive voltage and stability, and in particular excellent effects such as a low voltage and a long life time.
    Type: Grant
    Filed: February 6, 2014
    Date of Patent: February 10, 2015
    Assignee: LG Chem, Ltd.
    Inventors: Jae Soon Bae, Dae Woong Lee, Dong Hoon Lee, Jae Chol Lee, Jun Gi Jang
  • Patent number: 8946230
    Abstract: Aryl- and heteroaryl-nitrogen heterocyclic compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein m, p, q, R1, R2, R3, X1, X2, X3, Y1 and Y2 are defined herein; and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: May 9, 2011
    Date of Patent: February 3, 2015
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Kristin L. Andrews, Michael J. Frohn, Paul E. Harrington, Alexander J. Pickrell, Robert M. Rzasa
  • Patent number: 8927548
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Grant
    Filed: January 13, 2012
    Date of Patent: January 6, 2015
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Weiwen Ying, David James, Shijie Zhang, Junghyun Chae, Teresa Kowalczyk-Przewloka, Howard P. Ng, Hao Li, Zachary Demko, Dinesh U. Chimmanamada, Chi-wan Lee, Zhenjian Du, Kevin Foley, Minghu Song, Lijun Sun, Keizo Koya, Dan Zhou, Shuzhen Qin
  • Publication number: 20150001178
    Abstract: A monomer for a hardmask composition is represented by the following Chemical Formula 1,
    Type: Application
    Filed: April 22, 2014
    Publication date: January 1, 2015
    Inventors: Hyun-Ji SONG, Yun-Jun KIM, Go-Un KIM, Young-Min KIM, Hea-Jung KIM, Joon-Young MOON, Yo-Choul PARK, Yu-Shin PARK, You-Jung PARK, Seung-Wook SHIN, Yong-Woon YOON, Chung-Heon LEE, Yoo-Jeong CHOI, Seung-Hee HONG
  • Patent number: 8916586
    Abstract: A styrylquinoline derivative of structure I or IV or a benzodioxol isoquinoline of structure II or III for use in the treatment of an angiogenesis-related disease or disorder. The invention also provides a composition comprising a styrylquinoline derivative of structure I or IV or a benzodioxol isoquinoline of structure II or III for use as a medicament.
    Type: Grant
    Filed: January 16, 2012
    Date of Patent: December 23, 2014
    Assignee: University College Dublin—National University of Ireland, Dublin
    Inventors: Breandan Kennedy, Yolanda Alvarez, Jacintha O'Sullivan
  • Patent number: 8912188
    Abstract: Disclosed herein are substituted quinoxaline carboxylic acids of Formula (I): and compositions thereof, which may be useful as inhibitors of PAS Kinase (PASK) activity in a human or animal for the treatment of diseases such as diabetes mellitus.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: December 16, 2014
    Assignee: BioEnergenix, LLC
    Inventors: John M. McCall, Donna L. Romero, Robert C. Kelly
  • Patent number: 8883801
    Abstract: The present invention relates to certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrimidine compounds.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: November 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Lianyun Zhao, Duan Liu, Shuyi Tang, Amit K. Mandal, Umar Faruk Mansoor, Lalanthi Dilrukshi Vitharana, Panduranga Adulla P. Reddy, M. Arshad Siddiqui
  • Patent number: 8877775
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.2]octane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ralf Anderskewitz, Matthias Grauert, Marc Grundl, Thorsten Oost, Alexander Pautsch, Stefan Peters
  • Patent number: 8871760
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, and R3 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: October 28, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Christine E. Brotherton-Pleiss, Ralph New Harris, III, Bradley E. Loe, Francisco Javier Lopez-Tapia, Pankaj D. Rege, David Bruce Repke, Russell Stephen Stabler, Keith Adrian Murray Walker
  • 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: 20140309244
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, A, X, D1, D2 and Y3 are as defined in the claims. The invention further provides intermediates used in the preparation of these compounds, to compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
    Type: Application
    Filed: September 23, 2011
    Publication date: October 16, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Werner Zambach, Daniel Stierli, Kurt Nebel, Andrea Bortolato, Clara Massol
  • Patent number: 8859599
    Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: October 14, 2014
    Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.
    Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
  • Patent number: 8853258
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives of Formula I, wherein the variables G, T, D, L, A, X, R1 and R2 are as described hereinabove, and their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Grant
    Filed: October 4, 2010
    Date of Patent: October 7, 2014
    Assignee: Pfizer Inc.
    Inventors: Matthew Frank Brown, Anthony Marfat, Michael Joseph Melnick, Usa Reilly
  • Patent number: 8835461
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: September 16, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
  • Patent number: 8802701
    Abstract: The present invention refers to new compounds represented by the general formula (I) where X is represented by the general formula (II) and Y is represented by the general formula (III). The relation X to Y may vary from 1:1 to 1:7. The radicals R1, R2, R3, R4, R5, and R6 in formula (II) are represented by: R1=H, CF3, CH3, OCH3, NH2, halogen; R2=H, CH3, NH2, halogen, NH—CHCH3(CH2)3N(C2H5)(CH2CH2OH), CH(OH)-2(C5H11N), NH—R7—N—(C2H5)2; R3=H, m-OC6H4CF3, NH2; R4=H, CH3, OCH3, NH2, halogen; R5=H, CH3, CF3, NH2, halogen; R6=H, CF3, CH3, NH2, halogen, NH—R8—N—(C2H5)2, NHCH(CH3)(CH2)3NH2; R7=(CH2)2, (CH2)3, CHCH3CH2, (CH2)4, (CH2)5, CHCH3(CH2)3, (CH2)6, (CH2)8, (CH2)10, (CH2)12; R8=CHCH3(CH2)3, CHCH3(CH2)CHCH3, (CH2)2, (CH2)3, (CH2)6, (CH2)3O(CH2)3. This invention also refers to a process of preparation of these compounds (formula I), and antiparasitic pharmaceutical compositions thereof.
    Type: Grant
    Filed: November 27, 2012
    Date of Patent: August 12, 2014
    Assignee: Fundação Oswaldo Cruz
    Inventors: Nubia Boechat, Marcus Vinicius Nora de Souza, Alessandra Leda Valverde, Antoniana Ursine Krettli
  • Publication number: 20140206876
    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: Application
    Filed: July 16, 2013
    Publication date: July 24, 2014
    Inventors: Sun Joon MIN, Yong Seo CHO, Ae Nim PAE, Eun Jeong LIM, Ji Yeong KIM, Myung Hee SON, Jae Kyun LEE
  • Patent number: 8785639
    Abstract: The invention provides a compound of Formula (Ie), pharmaceutically acceptable salts, or stereoisomers thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: July 22, 2014
    Assignee: AbbVie Inc.
    Inventors: Neil Wishart, Maria A. Argiriadi, David J. Calderwood, Anna M. Ericsson, Kristine E. Frank, Dawn M. George, Eric R. Goedken, Michael Friedman, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Jeffrey W. Voss, Lu Wang, Eric C. Breinlinger, Kelly D. Mullen, Gagandeep Somal, Michael Z Hoemann
  • Patent number: 8778840
    Abstract: The present invention relates to novel soluble liquid (SL) formulations comprising A) quinclorac ammonium salts of formula I wherein R1, R2, R3 and R4 are independently hydrogen or optionally substituted alkyl, and B) a solvents of formula IIa wherein R5 is alkyl; A is alkylene or oxyalkylene; and m is 0, 1, 2 or 3; and/or a solvent of formula IIb HO—B—OH??(IIb) wherein B is a straight-chain or branched alkylene or alkyleneoxyalkylene or alkyleneoxyalkyleneoxyalkylene.
    Type: Grant
    Filed: July 7, 2008
    Date of Patent: July 15, 2014
    Assignee: BASF SE
    Inventors: Rainer Berghaus, Terrance Cannan, Joseph Zawierucha, Glenn W. Oliver
  • 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
  • Patent number: 8748453
    Abstract: The present invention is directed to novel quinolines and quniazolines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof which are useful for the treatment of protein kinases mediated diseases and conditions. The compounds of this invention have a general Formula (I) wherein R1 to R11 and X are defined herein.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: June 10, 2014
    Assignee: Medolution Limited
    Inventor: Dawei Zhang
  • Publication number: 20140148461
    Abstract: The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Application
    Filed: November 22, 2013
    Publication date: May 29, 2014
    Inventors: Hervé GENESTE, Sean Colm TURNER, Michael OCHSE, Karla DRESCHER, Lawrence A. BLACK, Katja JANTOS
  • Patent number: 8710076
    Abstract: The present invention is directed to 2,5-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: April 29, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, Anthony J. Roecker, John D. Schreier
  • Patent number: 8691986
    Abstract: Azetidine and piperidine compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: June 14, 2013
    Date of Patent: April 8, 2014
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Matthew R. Kaller, Qingyian Liu, Thomas T. Nguyen, Alexander J. Pickrell, Wenyuan Qian, Robert M. Rzasa, Wenge Zhong
  • Patent number: 8680114
    Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: March 25, 2014
    Assignees: Array Biopharma, Inc., Genentech, Inc.
    Inventors: Ian S. Mitchell, Keith L. Spencer, Peter Stengel, Yongxin Han, Nicholas C. Kallan, Mark Munson, Guy P. A. Vigers, James Blake, Anthony Piscopio, John Josey, Scott Miller, Dengming Xiao, Rui Xu, Chang Rao, Bing Wang, April L. Bernacki
  • Patent number: 8680278
    Abstract: The present invention is directed to a process for enantioselectively preparing substituted piperidine alkanoic acid integrin antagonist compounds.
    Type: Grant
    Filed: October 30, 2008
    Date of Patent: March 25, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: William A. Kinney, Christopher A. Teleha, Shyamali Ghosh, Bruce E. Maryanoff, Gabriela Grasa, Antonio Zanotti-Gerosa, Jonathan Alan Medlock
  • Patent number: 8674138
    Abstract: The present invention relates to a new binaphthalene derivative, a preparation method thereof, and an organic electronic device using the same. The binaphthalene derivative according to the present invention can perform functions of hole injection and transportation, electron injection and transportation, or light emission in an organic electronic device including an organic light-emitting device, and the device according to the present invention has excellent characteristics in terms of efficiency, drive voltage and stability, and in particular excellent effects such as a low voltage and a long life time.
    Type: Grant
    Filed: October 20, 2006
    Date of Patent: March 18, 2014
    Assignee: LG Chem. Ltd.
    Inventors: Jae Soon Bae, Dae Woong Lee, Dong Hoon Lee, Jae Chol Lee, Jun Gi Jang
  • Publication number: 20140054577
    Abstract: A photoelectric conversion element comprises a first photoelectric conversion part, the first photoelectric conversion part comprising: a pair of electrodes; and a photoelectric conversion film between the pair of electrodes, wherein the photoelectric conversion film comprises an organic photoelectric conversion material having an absorption peak in an infrared region of an absorption spectrum within a combined range of a visible region and the infrared region and generating an electric charge according to light absorbed, and the first photoelectric conversion part as a whole transmits 50% or more of light in the visible region.
    Type: Application
    Filed: November 4, 2013
    Publication date: February 27, 2014
    Applicant: FUJIFILM Corporation
    Inventors: Tetsuro MITSUI, Tetsu KITAMURA, Kimiatsu NOMURA, Toru HARADA
  • Patent number: 8658646
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: August 31, 2012
    Date of Patent: February 25, 2014
    Assignee: Hoffmann-LaRoche Inc.
    Inventors: Shaoqing Chen, Javier de Vicente Fidalgo, Matthew Michael Hamilton, Johannes Cornelius Hermann, Joshua Kennedy-Smith, Hongju Li, Allen John Lovey, Matthew C. Lucas, Kin-Chun Thomas Luk, Stephen M. Lynch, Counde O'yang, Fernando Padilla, Ryan Craig Schoenfeld, Achyutharao Sidduri, Michael Soth, Ce Wang, Peter Michael Wovkulich, Xiaohu Zhang
  • Patent number: 8653105
    Abstract: A series of quinoline derivatives, substituted by an optionally substituted bicyclic heteroaryl moiety consisting of two fused six-membered aromatic rings attached via an alkylene chain optionally linked to a heteroatom, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: February 18, 2014
    Assignee: UCB Pharma S.A.
    Inventors: Daniel Rees Allen, Roland Bürli, Alan Findlay Haughan, Mizio Matteucci, Andrew Pate Owens, Gilles Raphy, Andrew Sharpe
  • Patent number: 8653071
    Abstract: The present invention relates to novel ?4?2 neuronal nicotinic acetylcholine receptor ligand compounds of the formula (I), and their derivatives, stereoisomers, pharmaceutically acceptable salts and compositions containing them. The present invention relates to novel ?4?2 neuronal nicotinic acetylcholine receptor ligand compounds of the formula (I), and their derivatives, stereoisomers, pharmaceutically acceptable salts and compositions containing them.
    Type: Grant
    Filed: May 3, 2010
    Date of Patent: February 18, 2014
    Assignee: Suven Life Sciences Limited
    Inventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Kana Ram Kumawat, Ishtiyaque Ahmad, Pradeep Jayarajan, Anil Karbhari Shinde, Nagaraj Vishwottam Kandikere, Koteshwara Mudigonda, Venkateswarlu Jasti
  • 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
  • Patent number: 8637543
    Abstract: A series of quinoline and quinoxaline derivatives, substituted by a fused bicyclic pyridine or pyrimidine moiety attached via an alkylene chain optionally linked to a heteroatom, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: January 28, 2014
    Assignee: UCB Pharma S.A.
    Inventors: Roland Bürli, Alan Findlay Haughan, Mizio Matteucci, Andrew Pate Owens, Gilles Raphy, Andrew Sharpe
  • Patent number: 8614229
    Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: August 27, 2008
    Date of Patent: December 24, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
  • Patent number: 8614328
    Abstract: Provided are 4?-O substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Grant
    Filed: March 1, 2012
    Date of Patent: December 24, 2013
    Assignee: Celgene Corporation
    Inventors: Alexander L. Ruchelman, George W. Muller, Hon-Wah Man, Roger Shen-Chu Chen
  • Patent number: 8586570
    Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: November 19, 2013
    Assignee: Massachusetts Institute of Technology
    Inventors: Barbara Imperiali, Elvedin Lukovic, Dora Carrico-Moniz