Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/371.7)
  • Patent number: 9802899
    Abstract: The present application relates to the use of heterocyclic compounds for controlling animal pests including arthropods, insects and nematodes, to novel heterocyclic compounds, to processes for their preparation and to intermediates for preparing the heterocyclic compounds.
    Type: Grant
    Filed: September 30, 2013
    Date of Patent: October 31, 2017
    Assignee: BAYER CROPSCIENCE AG
    Inventors: Eike Kevin Heilmann, Joerg Greul, Axel Trautwein, Hans-Georg Schwarz, Isabelle Adelt, Roland Andree, Peter Luemmen, Maike Hink, Martin Adamczewski, Mark Drewes, Angela Becker, Arnd Voerste, Ulrich Goergens, Kerstin Ilg, Johannes-Rudolf Jansen, Daniela Portz
  • Patent number: 9593112
    Abstract: Provided is a compound capable of effectively control worst weeds of higher leaf stages that present practical problems. A specific pyrazolylpyrazole derivative of formula (I) is disclosed that is able to solve the above-mentioned problems.
    Type: Grant
    Filed: August 11, 2014
    Date of Patent: March 14, 2017
    Assignee: KYOYU AGRI CO., LTD.
    Inventors: Ken Matsubara, Makoto Niino
  • Publication number: 20150119439
    Abstract: The invention provides saturated acyl guanidine compounds that inhibit F1F0-ATPase, and methods of using saturated acyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: June 7, 2013
    Publication date: April 30, 2015
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood, Chad A. Van Huis
  • Publication number: 20150119243
    Abstract: The present invention relates to novel 1-methyl-pyrazole(thio)indanyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.
    Type: Application
    Filed: May 6, 2013
    Publication date: April 30, 2015
    Applicant: Bayer Cropscience AG
    Inventors: Simon Maechling, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Jean-Pierre Vors, Stephane Brunet, Helene Lachaise, Pierre Genix
  • Publication number: 20150105389
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: Erik Dean RAAUM, Garrett Thomas POTTER, Tai Wei LY
  • Patent number: 8993752
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R4, and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: March 31, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Roland Gendron, Adam D. Hughes
  • Publication number: 20150080397
    Abstract: Provided herein are pharmaceutically acceptable salts of 3,5-diaminopyrazoles, for example, pharmaceutically acceptable salts of compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: September 17, 2014
    Publication date: March 19, 2015
    Inventors: Tai Wei LY, Erik Dean RAAUM
  • Publication number: 20150057166
    Abstract: Certain embodiments provide a method for crystallizing a GPCR. The method may employ a fusion protein comprising, from N-terminus to C-terminus: a) a first portion of a family C G-protein coupled receptor (GPCR), wherein the first portion comprises the TM1, TM2 and TM3, regions of the GPCR; b) a stable, folded protein insertion; and c) a second portion of the GPCR, wherein the second portion comprises the TM4, TM5 TM6 and TM7 regions of the GPCR.
    Type: Application
    Filed: October 17, 2014
    Publication date: February 26, 2015
    Inventor: BRIAN KOBILKA
  • Patent number: 8962608
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: February 24, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jason Brubaker, Christopher Dinsmore, Dawn Marie Hoffman, Joon Jung, Duan Liu, Scott Peterson, Tony Siu, Luis E. Torres, Hongjun Zhang, Zhongyong Wei, Feng Shi
  • Patent number: 8916555
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: December 23, 2014
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
  • Publication number: 20140315933
    Abstract: The present invention relates to new sulfonamide URAT-1 inhibitor compounds of formula (I) or pharmaceutically acceptable salts thereof: to compositions containing them, to processes for their preparation and to intermediates used in such processes and to methods of treatment; wherein R1, R2, R3, R4, R5 and R6 are as defined in the description.
    Type: Application
    Filed: April 17, 2014
    Publication date: October 23, 2014
    Applicant: PFIZER LIMITED
    Inventors: Robert McKenzie Owen, Robert Ian Storer
  • Publication number: 20140315971
    Abstract: The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.
    Type: Application
    Filed: July 7, 2014
    Publication date: October 23, 2014
    Inventors: Izumi SASAKI, Tomohiro TOYODA, Hidefumi YOSHINAGA, Itaru NATSUTANI, Yoko TAKAHASHI
  • Patent number: 8846936
    Abstract: Compounds of formula (I) and formula (II) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: September 30, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Eugene Richard Hickey, Doris Riether, Monika Ermann
  • Publication number: 20140243309
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: September 21, 2012
    Publication date: August 28, 2014
    Inventors: Jason Brubaker, Christopher Dinsmore, Dawn Marie Hoffman, Joon Jung, Duan Liu, Scott Peterson, Tony Siu, Luis E. Torres, Hongjun Zhang, Zhongyong Wei, Feng Shi
  • Patent number: 8815910
    Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: August 26, 2014
    Assignee: Ardelyx, Inc.
    Inventors: Jason G. Lewis, Jeffrey W. Jacobs, Nicholas Reich, Michael R. Leadbetter, Noah Bell, Han-Ting Chang, Tao Chen, Marc Navre, Dominique Charmot, Christopher Carreras, Eric Labonte
  • Publication number: 20140228348
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: September 21, 2012
    Publication date: August 14, 2014
    Inventors: Jason Brubaker, Matthew Lloyd Childers, Matthew Christopher, Joshua T. Close, Jason David Katz, Joon Jung, Scott Peterson, Phieng Siliphaivanh, Tony Siu, Graham Frank Smith, Luis E. Torres, Hyun Chong Woo, Jonathan R. Young, Hongjun Zhang
  • Publication number: 20140228358
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: September 21, 2012
    Publication date: August 14, 2014
    Inventors: Jason Brubaker, Joshua T. Close, Joon Jung, Michelle Martinez, Catherine White, Kevin Wilson, Jonathan R. Young, Hongjun Zhang
  • Publication number: 20140221448
    Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2, R4, R5 and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 or Formula 1A and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: April 10, 2014
    Publication date: August 7, 2014
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Jeffrey Keith Long, Mary Ann Hanagan, Eric Allen Marshall, Amy X. Ding
  • Patent number: 8754115
    Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2, R4, R5 and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 or Formula 1A and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: June 17, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Jeffrey Keith Long, Paula Louise Sharpe, Amy X Ding
  • 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: 20140107125
    Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.
    Type: Application
    Filed: April 29, 2013
    Publication date: April 17, 2014
    Applicant: Dermira (Canada), Inc.
    Inventor: Dermira (Canada), Inc.
  • Publication number: 20140073783
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R4, and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: July 8, 2013
    Publication date: March 13, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Roland Gendron, Adam D. Hughes
  • Patent number: 8653112
    Abstract: The invention provides a compound of formula (I) wherein G is a pyrazole ring as defined in the specification and R4, R5, R6 and R7 are as defined in the specification; or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: February 18, 2014
    Assignee: Karo Bio AB
    Inventors: Joakim Löfstedt, Xiongyu Wu, Lars Krüger
  • Patent number: 8614243
    Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.
    Type: Grant
    Filed: June 8, 2010
    Date of Patent: December 24, 2013
    Assignee: Dendreon Corporation
    Inventors: Ofir Moreno, Sateesh Natarajan, David F. Duncan
  • Publication number: 20130324536
    Abstract: The invention provides pyrazolyl guanidine compounds that inhibit F1Fo-ATPase, and methods of using pyrazolyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: December 8, 2011
    Publication date: December 5, 2013
    Applicant: Lycera Corporation
    Inventors: Gary D. Glick, Alexander R. Hurd, Clarke B. Taylor, Chad A. Van Huis
  • Publication number: 20130303492
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: March 14, 2013
    Publication date: November 14, 2013
    Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
  • Publication number: 20130274227
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: March 14, 2013
    Publication date: October 17, 2013
    Applicant: Axikin Pharmaceuticals, Inc.
    Inventors: Erik Dean RAAUM, Garrett Thomas Potter, Tai Wei Ly
  • Publication number: 20130269064
    Abstract: Novel heteroaromatic compounds of formula (I): wherein A1, A2, A3, A4, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.
    Type: Application
    Filed: November 18, 2011
    Publication date: October 10, 2013
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Pierre Joseph Marcel Jung, Ottmar Franz Hueter, Peter Renold
  • Publication number: 20130143940
    Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2, R4, R5 and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 or Formula 1A and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: August 31, 2011
    Publication date: June 6, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Jeffrey Keith Long, Mary Ann Hanagan, Eric Allen Marshall, Paula Louise Sharpe, Amy X. Ding
  • Patent number: 8445694
    Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.
    Type: Grant
    Filed: December 23, 2010
    Date of Patent: May 21, 2013
    Assignee: Dermira (Canada), Inc.
    Inventors: Zaihui Zhang, Timothy S. Daynard, Mikhail A. Chafeev, Shisen Wang, Gregory B. Chopiuk, Serguei V. Sviridov
  • Patent number: 8420824
    Abstract: The disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R1, R2, R3, R4a, R4b, and R5 are as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: April 16, 2013
    Assignee: Sanofi
    Inventors: Kirsten Bjergarde, Mark Dodson, Jacques Mauger, Anil Nair, Marcel Patek, Michel Tabart
  • Patent number: 8415346
    Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
    Type: Grant
    Filed: July 21, 2009
    Date of Patent: April 9, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Altman, Kevin Wilson
  • Patent number: 8410159
    Abstract: The present invention relates to compounds of formula (I), methods for their preparation, medicaments comprising these compounds as well their use in the manufacture of a medicament for the treatment of humans and animals.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: April 2, 2013
    Assignee: Laboratories del Dr. Esteve, S.A.
    Inventors: Rosa Cuberes-Altisent, Joerg Holenz
  • Patent number: 8410286
    Abstract: The disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R1, R2, R3, R4a, R4b, and R5 are as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: April 2, 2013
    Assignee: Sanofi-Aventis
    Inventors: Kirsten Bjergarde, Mark Dodson, Jacques Mauger, Anil Nair, Marcel Patek, Michel Tabart
  • Publication number: 20130053416
    Abstract: 3-Heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals The present invention relates to compounds of the formula I, wherein Ht, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: July 26, 2012
    Publication date: February 28, 2013
    Applicant: SANOFI
    Inventors: Sven RUF, Josef PERNERSTORFER, Thorsten SADOWSKI, Georg HORSTICK, Herman SCHREUDER, Christian BUNING, Klaus WIRTH
  • Publication number: 20130030180
    Abstract: Disclosed are compounds and methods for treating neurological and other disorders by administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for GFR? receptor molecules, which can be mimetics of glial-derived neurotrophic factor (GDNF) family ligands (GFLs), GFR?/RET signaling pathway agonists, and/or direct RET agonists (activators).
    Type: Application
    Filed: December 13, 2010
    Publication date: January 31, 2013
    Applicant: GeneCode AS
    Inventors: Mart Saarma, Mati Karelson, Maxim Bespalov, Mehis Pilv
  • Publication number: 20130005784
    Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.
    Type: Application
    Filed: December 23, 2011
    Publication date: January 3, 2013
    Applicant: JENRIN DISCOVERY
    Inventors: John F. McElroy, Robert J. Chorvat
  • Publication number: 20120316150
    Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1, R2, R3, R4, R5 and R6 are as defined herein: and compositions, processes for the preparation, and uses thereof, e.g. in the treatment of endometriosis or uterine fibroids.
    Type: Application
    Filed: June 18, 2012
    Publication date: December 13, 2012
    Inventors: KARL RICHARD GIBSON, Martin Peter Green, Toby James Underwood, Florian Wakenhut
  • Publication number: 20120309673
    Abstract: Compounds of Formula II wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4? is C1-C6alkyl, C1-C6haloalkyl or oxetany-3-yl. for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.
    Type: Application
    Filed: December 10, 2010
    Publication date: December 6, 2012
    Applicant: Medivir UK Ltd
    Inventors: Susana Ayesa, Karolina Ersmark, Urszula Grabowska, Ellen Hewitt, Daniel Jönsson, Pia Kahnberg, Björn Klasson, Peter Lind, Stina Lundgren, Lourdes Odén, Kevin Parkes, Daniel Wiktelius
  • Publication number: 20120270918
    Abstract: The invention relates to pyrazole derivatives of general formula (I): in which X represents chlorine or fluorine; to a process for preparing said derivatives, and to therapeutic uses of said derivatives.
    Type: Application
    Filed: December 23, 2011
    Publication date: October 25, 2012
    Applicant: Sanofi
    Inventors: Pierre Yves ABECASSIS, Pascal DESMAZEAU, Michel TABART
  • Patent number: 8288563
    Abstract: The present invention refers to a process for the preparation of pyrazole derivatives of formula (I) wherein W is nitrogen or CR1, R1, R2, R4 and R5 are each independently selected from hydrogen, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, R7S(O)n, nitro, cyano, and pentafluorothio; R3 is hydrogen, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, R7S(O)n, nitro, cyano, pentafluorothio or phenyl which is unsubstituted or substituted by 1 to 5 members of the group consisting of halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, R7S(O)n, nitro, cyano, and pentafluorothio which are the same or different; R7 is C1-C6-alkyl or C1-C6-haloalkyl; and n is 0, 1, or 2; characterized in that hydrazines of formula (II) wherein W, R2, R3, R4, and R5 are as defined for pyrazole derivatives of formula (I), are reacted with a compound of formula (III)
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: October 16, 2012
    Assignee: BASF SE
    Inventors: Maximilian Dochnahl, Martin Sukopp, Alexander Korte
  • Publication number: 20120232112
    Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, G, R10, R11, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: January 24, 2012
    Publication date: September 13, 2012
    Applicant: SANOFI
    Inventors: Sven RUF, Thorsten SADOWSKI, Georg HORSTICK, Herman SCHREUDER, Christian BUNING, Thomas OLPP, Klaus WIRTH
  • Publication number: 20120225871
    Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.
    Type: Application
    Filed: June 8, 2010
    Publication date: September 6, 2012
    Applicant: Dendreon Corporation
    Inventors: Ofir Moreno, Sateesh Natarajan, David F. Duncan
  • Publication number: 20120220769
    Abstract: A process for preparing 7-[2-[4-(6-fluoro-3-methyl-1,2-benzisoxazol-5-yl)-1-piperazinyl]ethyl]-2-(1-propynyl)-7H-pyrazolo-[4,3-e]-[1,2,4]-triazolo[1,5-c]pyrimidin-5-amine, intermediates useful in that process, and processes for preparing said intermediates are disclosed.
    Type: Application
    Filed: August 3, 2010
    Publication date: August 30, 2012
    Applicant: Schering Corporation
    Inventors: Shen-Chun Kuo, Yonggang Chen, Jeffrey M. Eckert, William W. Leong, Nanfei Zou, Gabriel C. Kuklis
  • Publication number: 20120202853
    Abstract: The invention provides a compound of formula (I) wherein G is a pyrazole ring as defined in the specification and R4, R5, R6 and R7 are as defined in the specification; or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
    Type: Application
    Filed: October 6, 2010
    Publication date: August 9, 2012
    Applicant: KARO BIO AB
    Inventors: Joakim Löfstedt, Xiongyu Wu, Lars Krüger
  • Publication number: 20120164102
    Abstract: The pharmaceutically acceptable salts of bicycle-substituted pyrazolon azo derivatives represented by the general formula (I), their preparation methods, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor. The definitions of substituents in the general formula (I) are the same as the description.
    Type: Application
    Filed: May 28, 2010
    Publication date: June 28, 2012
    Inventors: Peng Cho Tang, Hejun Lü, Hongbo Fei, Yiqian Chen
  • Publication number: 20120142668
    Abstract: Disclosed are 4-amino-2-butenamides of Formula (I) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin C enzyme such as chronic obstructive pulmonary disease.
    Type: Application
    Filed: August 11, 2010
    Publication date: June 7, 2012
    Inventors: Niall Anderson, Ann M. Bullion, Neysa Nevins, Michael R. Palovich, Steven L. Sollis, Michael D. Wall, Jakob Busch-Petersen, Brian Evans, Huijie Li
  • Publication number: 20120129893
    Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
    Type: Application
    Filed: January 12, 2012
    Publication date: May 24, 2012
    Inventors: Jacques DUMAS, Uday Khire, Timothy B. Lowinger, Holger Paulsen, Bernd Riedl, William J. Scott, Roger A. Smith, Jill E. Wood, Holia Hatoum-Mokdad, Jeffrey Johnson, Wendy Lee, Aniko Redman, Robert Sibley, Joel Renick
  • Publication number: 20120108573
    Abstract: The present invention relates to compounds of the formula I wherein A1, A2, R1, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula fare capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.
    Type: Application
    Filed: January 6, 2012
    Publication date: May 3, 2012
    Inventors: Ursula SCHINDLER, Karl SCHÖNAFINGER, Hartmut STROBEL
  • Publication number: 20120071475
    Abstract: Provided is a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a urea derivative shown in the present specification, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 26, 2010
    Publication date: March 22, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Daisuke Taniyama, Yasunori Mitsuoka, Kayoko Hata