Nitrogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 548/233)
  • Publication number: 20150133431
    Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives, pharmaceutical compositions comprising GGA derivatives and the use of GGA derivatives.
    Type: Application
    Filed: July 10, 2014
    Publication date: May 14, 2015
    Applicant: COYOTE PHARMACEUTICALS, INC.
    Inventor: Gary C. Look
  • Publication number: 20150080412
    Abstract: The invention disclosed herein is directed to compounds of Formula (I) and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula (I), or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention disclosed herein is further directed to methods of treating prostate, breast, colon, pancreatic, chronic lymphocytic leukemia, melanoma and other cancers comprising administration of a of a therapeutically effective amount of a selective PPAR? antagonist.
    Type: Application
    Filed: March 7, 2013
    Publication date: March 19, 2015
    Applicant: INCEPTION 2, INC.
    Inventors: Nicholas Simon Stock, Austin Chih-Yu Chen, Yalda Mostofi Bravo, Jason Duarte Jacintho, Jill Melissa Baccei, Brian Andrew Stearns, Ryan Christopher Clark, Yen Pham Truong
  • Publication number: 20150011553
    Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the field of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.
    Type: Application
    Filed: July 3, 2014
    Publication date: January 8, 2015
    Inventors: Ulrich GÖRGENS, Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
  • Publication number: 20140329871
    Abstract: The present invention provides compounds having the general structural Formula (I): and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis or dysproliferation.
    Type: Application
    Filed: December 2, 2012
    Publication date: November 6, 2014
    Applicant: ANGION BIOMEDICA CORP.
    Inventors: Rama K. Mishira, Bijoy Panicker, James G. Tarrant, Dong Sung Lim, Lambertus J.W.M. Oehlen, Dawoon Jung
  • Patent number: 8846727
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: September 30, 2014
    Assignee: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Publication number: 20140275041
    Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicant: Sareum Limited
    Inventors: John Charles READER, John Mark ELLARD, Helen BOFFEY, Susanne TAYLOR, Andrew David CARR, Michael CHERRY, Michelle WILSON, Richard Boakye OWOARE
  • Patent number: 8729113
    Abstract: The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Grant
    Filed: February 24, 2011
    Date of Patent: May 20, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross
  • Patent number: 8710237
    Abstract: The present invention relates to compounds of formula Ia or Ib below and their tautomers and/or pharmaceutically acceptable salts and compositions and methods of uses thereof.
    Type: Grant
    Filed: June 29, 2011
    Date of Patent: April 29, 2014
    Assignees: The J. David Gladstone Institute, University of Maryland, Baltimore
    Inventors: Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
  • Patent number: 8673950
    Abstract: The invention relates to compounds of formula wherein R1, R2, R3, R4, X, Ar, and are defined herein or to a pharmaceutically suitable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm and cardiovascular disorders.
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: March 18, 2014
    Assignee: Hoffmann-LaRoche Inc.
    Inventors: Matthias Nettekoven, Roger Norcross, Alessandra Polara
  • Patent number: 8674111
    Abstract: The invention relates to oxazole and thiazole derivatives of formula (I), wherein A, E, X, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Grant
    Filed: June 11, 2010
    Date of Patent: March 18, 2014
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Patent number: 8629157
    Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain (I).
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: January 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Angela Berry, Rajashekhar Betageri, Eugene Richard Hickey, Someina Khor, Doris Riether, Lifen Wu, Renee M. Zindell
  • Patent number: 8623860
    Abstract: The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: January 7, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Bernd Nosse, Gerald Juergen Roth
  • Publication number: 20130345241
    Abstract: The invention relates to compounds of formula wherein R1, R2, R3, R4, X, Ar, and are defined herein or to a pharmaceutically acceptable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm and cardiovascular disorders.
    Type: Application
    Filed: August 30, 2013
    Publication date: December 26, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Matthias Nettekoven, Roger Norcross, Alessandra Polara
  • Patent number: 8604061
    Abstract: The invention relates to compounds of formula I wherein X, Y, R1, R2, and n are as defined herein or to a pharmaceutically suitable acid addition salt thereof. The invention also relates to pharmaceutical compositions containing such compounds and methods for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases include depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Grant
    Filed: March 22, 2012
    Date of Patent: December 10, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Publication number: 20130324537
    Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.
    Type: Application
    Filed: November 21, 2012
    Publication date: December 5, 2013
    Applicants: Abbott Laboratories, Abbott GmbH & Co. KG
    Inventors: Abbott GmbH & Co. KG, Abbott Laboratories, Andrea Hager-Wernet
  • Publication number: 20130289057
    Abstract: The invention relates to N-arylaminomethylenebenzothiophenones of General Formula (I) for use as a drug for the treatment of cardiovascular diseases: wherein E is S, O, or CH2, D is CH or NH, and Ar is a phenyl or naphtyl moiety substituted by an electron-withdrawing group, an unsubstituted heteroaryl residue, or a heteroaryl residue substituted by alkyl or an electron-withdrawing group.
    Type: Application
    Filed: January 12, 2012
    Publication date: October 31, 2013
    Applicants: FORSCHUNGSVERBUND BERLIN E.V., MAX-DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZIN
    Inventors: Enno Klussmann, Walter Rosenthal, Jelena Milic, Martin W. Bergmann
  • Patent number: 8541453
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: September 24, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
  • Publication number: 20130231342
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).
    Type: Application
    Filed: July 27, 2011
    Publication date: September 5, 2013
    Applicant: Oryzon Fenomics S.A.
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Iñigo Tirapu Fernandez de la Cuesta, Maria de los Ángeles Estirate-Martinez
  • Publication number: 20130172316
    Abstract: The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: December 14, 2012
    Publication date: July 4, 2013
    Inventors: Martin FLECK, Bernd NOSSE, Gerald Juergen ROTH
  • Publication number: 20130158063
    Abstract: Disclosed are compounds, compositions and methods related PPAR antagonists. Certain compounds are effective at inhibiting PPARs. The compositions can be used to inhibit PPARs, treat cancer and treat metabolic disorders.
    Type: Application
    Filed: August 24, 2011
    Publication date: June 20, 2013
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Milton Lang Brown, Yali Kong, Yong Liu, Robert Glazer, York Tomita
  • Patent number: 8466182
    Abstract: The present invention relates to compounds of Formula I below and their tautomers or pharmaceutically acceptable salts, compositions and methods of uses thereof.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: June 18, 2013
    Assignees: The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone, University of Maryland, Baltimore
    Inventors: Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
  • Publication number: 20130143927
    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: Application
    Filed: June 8, 2012
    Publication date: June 6, 2013
    Applicant: CalciMedica, Inc.
    Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
  • Patent number: 8431604
    Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.
    Type: Grant
    Filed: February 15, 2005
    Date of Patent: April 30, 2013
    Assignee: Abbott GmbH & Co. KG
    Inventors: Astrid Netz, Wilhelm Amberg, Udo Lange, Michael Ochse, Charles W. Hutchins, Francisco-Xavier Garcia-Ladona, Wolfgang Wernet, Andreas Kling
  • Patent number: 8410150
    Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: April 2, 2013
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
  • Patent number: 8404726
    Abstract: A compound represented by the following general formula (II) or a salt thereof is used as an activator of PPAR?. wherein Ga is O, CH2 or the like; Aa is thiazole, oxazole, or thiophene, which can have a substituent such as C1-8 alkyl, C1-8 alkoxy, halogen, C1-8 alkyl substituted with halogen or the like; Ba is a C1-8 alkylene or C2-8 alkenylene chain; and each of R1a and R2a independently is hydrogen, C1-8 alkyl, C1-8 alkoxy, halogen, C1-8 alkyl substituted with halogen or the like.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: March 26, 2013
    Assignee: Nippon Chemiphar Co. Ltd.
    Inventors: Shogo Sakuma, Nobutaka Mochiduki, Rie Takahashi, Masatoshi Ushioda, Tomio Yamakawa, Seiichiro Masui
  • Publication number: 20130032787
    Abstract: A heterocyclic compound represented by Formula 1 or Formula 2 below, and an organic light-emitting device including the heterocyclic compound. The organic light-emitting device may include an organic layer containing the heterocyclic compound, and thus may have a low driving voltage, a high-emission efficiency, and long lifespan characteristics. wherein R1 to R12, Ar1, Ar2, A, B, a, and b are defined as in the specification.
    Type: Application
    Filed: November 25, 2011
    Publication date: February 7, 2013
    Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.
    Inventors: Young-Kook Kim, Seok-Hwan Hwang, Hye-Jin Jung, Jin-O Lim, Sang-Hyun Han, Se-Jin Cho, Jong-Hyuk Lee
  • Patent number: 8357712
    Abstract: The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Grant
    Filed: February 24, 2011
    Date of Patent: January 22, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross
  • Patent number: 8354441
    Abstract: The invention relates to compounds of formula I wherein the definitions of X, R and R1 are as defined herein. The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Grant
    Filed: November 3, 2010
    Date of Patent: January 15, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Roger Norcross, Alessandra Polara
  • Publication number: 20130012502
    Abstract: Pharmaceutical or veterinary compositions to prevent or treat viral infections, in particular to prevent or treat influenza A, B and C virus infections.
    Type: Application
    Filed: December 7, 2010
    Publication date: January 10, 2013
    Applicants: HOSPICES CIVILS DE LYON, UNIVERSITE CLAUDE BERNARD LYON 1
    Inventors: Manuel Rosa-Calatrava, Jean-Jacques Diaz, Julien Textoris, Laurence Josset
  • Publication number: 20120322800
    Abstract: Disclosed herein are small molecule heterocyclic inhibitors of sepiapterin reductase (SPR), and prodrugs and pharmaceutically acceptable salts thereof. The Also featured are pharmaceutical compositions of the compounds and uses of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, and neuropathic pain).
    Type: Application
    Filed: October 14, 2010
    Publication date: December 20, 2012
    Inventor: Julian Blagg
  • Patent number: 8329918
    Abstract: Described herein are compounds useful as agonists of alpha 2B/2C receptors. Pharmaceutical compositions including the presently described compounds and methods of treatment of diseases and conditions with the presently described compounds also are disclosed.
    Type: Grant
    Filed: July 1, 2010
    Date of Patent: December 11, 2012
    Assignee: Allergan Inc.
    Inventors: Phong X. Nguyen, Ken Chow, Todd M. Heidelbaugh, Dario G. Gomez, Wenkui K. Fang, Santosh C. Sinha, Michael E. Garst, Daniel W. Gil
  • Patent number: 8242153
    Abstract: The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Grant
    Filed: September 14, 2009
    Date of Patent: August 14, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross
  • Publication number: 20120196903
    Abstract: The invention relates to compounds of formula I wherein X, Y, R?, R2, and n are as defined herein or to a pharmaceutically suitable acid addition salt thereof. The invention also relates to pharmaceutical compositions containing such compounds and methods for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases include depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Application
    Filed: March 22, 2012
    Publication date: August 2, 2012
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Patent number: 8211924
    Abstract: The present invention relates to 1-(azolin-2-yl)amino-1,2-diphenylethane compounds of the formula I and to their salts which are useful for combating animal pests. The invention also relates to a method for controlling animal pests by using these compounds, to seed and to an agricultural and veterinary composition comprising said compounds. wherein A is a radical of formulae A.1 or A.
    Type: Grant
    Filed: July 2, 2008
    Date of Patent: July 3, 2012
    Assignee: BASF SE
    Inventors: Markus Kordes, Christopher Koradin, Ronan Le Vezouet, Ernst Baumann, Deborah L. Culbertson, Douglas D. Anspaugh, Hassan Oloumi-Sadeghi, Cecille Ebuenga
  • Publication number: 20120165294
    Abstract: The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Application
    Filed: March 2, 2012
    Publication date: June 28, 2012
    Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross
  • Publication number: 20120149679
    Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.
    Type: Application
    Filed: February 20, 2012
    Publication date: June 14, 2012
    Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
  • Publication number: 20120149718
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein the variables 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: Application
    Filed: December 13, 2011
    Publication date: June 14, 2012
    Inventors: Christine E. Brotherton-Pleiss, Keith A. M. Walker
  • Publication number: 20120142666
    Abstract: Compounds of the formula (I), (II) and (III) which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: June 8, 2010
    Publication date: June 7, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Eugene Richard Hickey, Doris Riether, David Smith Thomson, Lifen Wu, Renee M. Zindell
  • Publication number: 20120142700
    Abstract: The present invention relates to heterocyclic compounds of formula (I) which have microbiocidal activity, in particular fungicidal activity, as well as methods of using the compounds of formula (I) to control microbes.
    Type: Application
    Filed: August 5, 2010
    Publication date: June 7, 2012
    Applicant: SYNGENTA CROP PROTECTION, LLC
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondex, Laura Quaranta
  • Publication number: 20120108609
    Abstract: The invention relates to compounds of formula wherein R1, R2, R3, R4, X, Ar, and are defined herein or to a pharmaceutically suitable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm and cardiovascular disorders.
    Type: Application
    Filed: October 24, 2011
    Publication date: May 3, 2012
    Inventors: Matthias Nettekoven, Roger Norcross, Alessandra Polara
  • Patent number: 8133911
    Abstract: The present invention relates to a novel class of (R)-4-(heteroaryl)phenylpropionic derivatives of formula (I), useful in the inhibition of the chemotactic activation induced by the fraction C5a of complement. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of autoimmune hemolytic anemia (AIHA), psoriasis, bullous pemphigoid, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
    Type: Grant
    Filed: October 17, 2008
    Date of Patent: March 13, 2012
    Assignee: Dompe S.p.A
    Inventors: Alessio Moriconi, Andrea Aramini
  • Patent number: 8110591
    Abstract: The present invention relates to novel compounds selected from 2-aminoaryloxazoles that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl, FGFR3 and/or Flt-3 inhibitors.
    Type: Grant
    Filed: January 11, 2010
    Date of Patent: February 7, 2012
    Assignees: AB Science, Centre National de la Recherche Scientifique (CNRS), Institut Curie
    Inventors: Alain Moussy, Camille Wermuth, David Grierson, Abdellah Benjahad, Martine Croisy, Marco Ciufolini, Bruno Giethlen
  • Patent number: 8080570
    Abstract: Described herein are compounds that can be useful as bioactive agents. More specifically, the compounds described herein can be useful as both ?2B and ?2C adrenergic agonists. Methods of synthesis and administration of the compounds are also disclosed.
    Type: Grant
    Filed: May 1, 2009
    Date of Patent: December 20, 2011
    Assignee: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ken Chow, Ling Li, Liming Wang
  • Patent number: 8080669
    Abstract: The present invention relates to a process for synthesizing in good yield substituted 2-aminoaryloxazole compounds of formula I which are useful as certain tyrosine kinase inhibitors and more particularly as c-kit, bcr-abl, Flt-3 and mutant forms thereof.
    Type: Grant
    Filed: May 11, 2007
    Date of Patent: December 20, 2011
    Assignee: AB Science
    Inventor: Abdellah Benjahad
  • Publication number: 20110306637
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: May 20, 2011
    Publication date: December 15, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
  • Publication number: 20110237589
    Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.
    Type: Application
    Filed: February 4, 2011
    Publication date: September 29, 2011
    Inventors: Astrid Netz, Wilhelm Amberg, Udo Lange, Michael Ochse, Charles W. Hutchins, Francisco-Xavier Garcia-Ladona, Wolfgang Wernet, Andreas Kling, Andrea Hager-Wernet
  • Patent number: 8017555
    Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.
    Type: Grant
    Filed: February 10, 2010
    Date of Patent: September 13, 2011
    Assignee: Divergence, Inc.
    Inventors: Urszula Slomczynska, Matt W. Dimmic, William P. Haakenson, Jr., Al Wideman
  • Patent number: 7989394
    Abstract: The present invention relates to 1-(azolin-2-yl)-amino-2-aryl-1-hetaryl-ethane compounds (I) and 1-(aminothiocarbonylamino)-2-aryl-1-hetaryl-ethane compounds (II) and their salts which are useful for combating animal pest, in particular insects, arachnids and nematodes. Furthermore, the present invention relates to a method for combating animal pests selected from insects, arachnids and nematodes, and to agricultural compositions for combating animal pests. Furthermore, the present invention relates to veterinary compositions for combating animal pests.
    Type: Grant
    Filed: June 29, 2007
    Date of Patent: August 2, 2011
    Assignee: BASF SE
    Inventors: Markus Kordes, Delphine Breuninger, Ronan Le Vezouet, Christopher Koradin, Livio Tedeschi, Michael Puhl, Deborah L. Culbertson
  • Patent number: 7989449
    Abstract: The present invention relates to a compounds of formula I wherein R1, R1?, R2, R3, R4, X, Ar, and m are as defined in the specification and claims and pharmaceutically active acid addition salts thereof. Compounds of the invention have Asp2 (?-secretase, BACE 1 or Memapsin-2) inhibitory activity and are useful for the treatment of diseases characterized by elevated ?-amyloid levels or ?-amyloid deposits, particularly Alzheimer's disease.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: August 2, 2011
    Assignees: Hoffman-La Roche Inc., Siena Biotech S.p.A.
    Inventors: Matteo Andreini, Emanuele Gabellieri, Wolfgang Guba, Guido Marconi, Robert Narquizian, Eoin Power, Massimiliano Travagli, Thomas Woltering, Wolfgang Wostl
  • Patent number: 7977332
    Abstract: Certain noel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, r, R, Ra, Rb, Rc, Rd, b, c, Re, Rf, Rg, Rh, R5, d, e, U, V, X, WR6 and R7 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Grant
    Filed: December 2, 2004
    Date of Patent: July 12, 2011
    Assignee: FMC Corporation
    Inventors: David M. Roush, John F. Chiarello, Jianming Yu, Benjamin J. Dugan, George Theodoridis, Manorama M. Patel, Walter H. Yeager, Steven W. Szczepanski