Carbocyclic Ring Bonded Directly At 3-position Patents (Class 544/290)
  • Patent number: 9102653
    Abstract: The present specification relates to the use of a quinazolinone compound of the formula (I) wherein R1, R2, R3, R4, R5 and m are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in acid addition salt form.
    Type: Grant
    Filed: July 2, 2014
    Date of Patent: August 11, 2015
    Assignee: NOVARTIS AG
    Inventors: Timothy John Ritchie, Andrew James Culshaw, Christopher Thomas Brain, Edward Karol Dziadulewicz, Terance William Hart
  • Patent number: 8993583
    Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: March 31, 2015
    Assignee: ICOS Corporation
    Inventors: Kerry W. Fowler, Danwen Huang, Edward A. Kesicki, Hua Chee Ooi, Amy Oliver, Fuqiang Ruan, Jennifer Treiberg, Kamal Deep Puri
  • Patent number: 8980901
    Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: March 17, 2015
    Assignee: Icos Corporation
    Inventors: Kerry W. Fowler, Danwen Huang, Edward A. Kesicki, Hua Chee Ooi, Amy Oliver, Fuqiang Ruan, Jennifer Treiberg, Kamal Deep Puri
  • Publication number: 20140378475
    Abstract: Disclosed are compounds of Formula (I) wherein: the two dotted lines represent either two single or two double bonds; Q is: R1 is F, Cl, —CN, or —CH3; R2 is Cl or —CH3; R3 is —C(CH3)2OH or —CH2CH2OH; Ra is H or —CH3; each Rb is independently F, Cl, —CH3, and/or —OCH3; and n is zero, 1, or 2. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Application
    Filed: June 25, 2014
    Publication date: December 25, 2014
    Inventors: Douglas G. Batt, Myra Beaudoin Bertrand, George Delucca, Michael A. Galella, Soo Sung Ko, Charles M. Langevine, Qingjie Liu, Qing Shi, Anurag S. Srivastava, Joseph A. Tino, Scott Hunter Watterson
  • Publication number: 20140315932
    Abstract: The present specification relates to the use of a quinazolinone compound of the formula (I) wherein R1, R2, R3, R4, R5 and m are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in acid addition salt form.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Applicant: NOVARTIS AG
    Inventors: Timothy John RITCHIE, Andrew James CULSHAW, Christopher Thomas BRAIN, Edward Karol DZIADULEWICZ, Terance William HART
  • Patent number: 8828991
    Abstract: The invention relates to azacyclyl-substituted arylthienopyrimidinones and their derivatives, of the Formula (I); and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one azacyclyl-substituted arylthienopyrimidinone according to Formula (I) or its derivative, and the use of the azacyclyl-substituted arylthienopyrimidinones according to Formula (I) and their derivatives as MCH antagonists.
    Type: Grant
    Filed: August 14, 2008
    Date of Patent: September 9, 2014
    Assignee: Sanofi
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Torsten Haack, Petra Lennig
  • Publication number: 20140213445
    Abstract: The present invention relates to agricultural methods and the use of 3-arylquinazolin-4-one derivatives of formula (I) wherein R1, R2, R3, R4, k and n are defined in the description in soil application methods. The compounds of the formula (I) are highly suitable for controlling animal pests such as insects and/or spider mites and/or nematodes by treating the soil/growth substrate by drenching or drip application or dipping or soil injection.
    Type: Application
    Filed: August 31, 2012
    Publication date: July 31, 2014
    Applicant: BASF SE
    Inventors: Florian Kaiser, Steffen Gross, Arun Narine, Koshi Gunjima
  • Publication number: 20140155417
    Abstract: The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.
    Type: Application
    Filed: August 30, 2013
    Publication date: June 5, 2014
    Applicant: HYDRA BIOSCIENCES, INC.
    Inventors: Jayhong A. Chong, Christopher Fanger, Glenn R. Larsen, William C. Lumma, JR., Anu Mahadevan, Peter Meltzer, Magdalene M. Moran, Amy Ripka, Dennis Underwood, Manfred Weigele, Xiaoguang Zhen
  • Publication number: 20130317221
    Abstract: The present invention provides 3-arylethynyl substituted quinazolinone compounds of formula (A) as potential anticancer agents against sixty human cancer cell lines. R1=H, OH, OCH3; R2=H, OH, CH3,OCH3, NO2; R3=H, OH, OCH3, F, Cl; R2+R3=—OCH2O—; R4=H, OH, CH3, OCH3; R5=H, OH, CH3, OCH3; R6=H, OCH3.
    Type: Application
    Filed: March 31, 2011
    Publication date: November 28, 2013
    Applicant: Council of Scientific & Industrial Research
    Inventors: Ahmed Kamal, Farheen Sultana, Erla Vijaya Bharathi, Yellamelli Valli Venkata Srikanth, Arutla Viswanath, Ponnampalli Swapna
  • Patent number: 8524721
    Abstract: Novel compounds of formulae (I) and (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 10, 2011
    Date of Patent: September 3, 2013
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-Maguire
  • Publication number: 20130210805
    Abstract: This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.
    Type: Application
    Filed: October 6, 2011
    Publication date: August 15, 2013
    Inventors: Robert G. Aslanian, Christopher W. Boyce, Robert D. Mazzola, JR., Brian A. McKittrick, Kevin D. McCormick, Anandan Palani, Jun Qin, Haiqun Tang, Dong Xiao, Younong Yu, John P. Caldwell, Elizabeth Helen Kelley, Hongjun Zhang, Phieng Siliphaivanh, Rachel N. MacCoss, Joey L. Methot, Jolicia Polivina Gauuan, Qin Jiang, Andrew J. Leyhane, Johny Biju, Li Dong, Xian Huang, Ning Shao, Wei Zhou, Pawan K. Dhondi
  • Publication number: 20130190495
    Abstract: This invention generally relates to compositions and methods for cancer treatment and, in particular, to compositions able to interact (e.g., bind to) with MUC1 growth factor receptor or its ligands, and methods for treating the same. The invention also relates to assays or use of such compositions for the treatment of patients susceptible to or exhibiting symptoms characteristic of cancer or tumorigenesis. Other compositions of the present invention useful for the treatment or prevention of cancer or tumorigenesis include homologs, analogs, derivatives, enantiomers or functional equivalents. The present compositions can also be packaged in kits in some cases.
    Type: Application
    Filed: December 7, 2012
    Publication date: July 25, 2013
    Applicant: MINERVA BIOTECHNOLOGIES CORPORATION
    Inventor: MINERVA BIOTECHNOLOGIES CORPORATION
  • Publication number: 20130060029
    Abstract: There is described a process for the manufacture of compounds of the formula I said process comprising reacting a compound of the formula II as described herein, or a salt thereof, under simultaneous or sequential condensation and cyclisation conditions with an aniline compound of the formula III, wherein R2 and m are as defined for a compound of the formula I. Further reactions and related embodiments are also claimed and disclosed.
    Type: Application
    Filed: September 12, 2012
    Publication date: March 7, 2013
    Inventors: Weichun Chen, Hong-Yong Kim, Jessica Liang, Michael Mutz, Mahavir Prashad, Christopher Towler, Ruoqiu Wu
  • Patent number: 8349853
    Abstract: This invention generally relates to compositions and methods for cancer treatment and, in particular, to compositions able to interact (e.g., bind to) with MUC1 growth factor receptor or its ligands, and methods for treating the same. The invention also relates to assays or use of such compositions for the treatment of patients susceptible to or exhibiting symptoms characteristic of cancer or tumorigenesis. Other compositions of the present invention useful for the treatment or prevention of cancer or tumorigenesis include homologs, analogs, derivatives, enantiomers or functional equivalents. The present compositions can also be packaged in kits in some cases.
    Type: Grant
    Filed: September 5, 2002
    Date of Patent: January 8, 2013
    Assignee: Minerva Biotechnologies Corporation
    Inventor: Cynthia C. Bamdad
  • Patent number: 8349852
    Abstract: There is described a new polymorphic form of 4-(7-Hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile and a method of preparing it.
    Type: Grant
    Filed: January 6, 2010
    Date of Patent: January 8, 2013
    Assignee: Novartis AG
    Inventors: Weichun Chen, Hong-Yong Kim, Jessica Liang, Michael Mutz, Mahavir Prashad, Christopher Towler, Ruoqiu Wu
  • Patent number: 8268842
    Abstract: The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist activity, is useful in the prophylaxis or therapy of metabolic diseases, circulatory diseases, or nervous system diseases. [where, for example, Ar is a divalent group formed by eliminating two hydrogen atoms from benzene, X1 is a nitrogen atom, sulfur atom or oxygen atom, R1 is a 5- to 6-membered heteroaryl group, Ring A is a 5- to 6-membered heteroaryl ring, R2 and R3 are amino groups or alkylamino groups, and X2 is represented by formula (II): (where R4 and R5 are lower alkyl groups, and n is an integer from 2 to 4).
    Type: Grant
    Filed: February 11, 2009
    Date of Patent: September 18, 2012
    Assignee: MSD K.K.
    Inventors: Tsuyoshi Nagase, Nagaaki Sato, Akio Kanatani, Shigeru Tokita
  • Publication number: 20120189614
    Abstract: Organic compounds showing the ability to inhibit viral glycoprotein (GP)-mediated entry of a filovirus into a host cell are disclosed. The disclosed filovirus entry inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by filovirus including the type species Marburg virus (MARV) and Ebola virus (EBOV). Preferred inhibitors of the invention provide therapeutic agents for combating the Ivory Coast, Sudan, Zaire, Bundibugyo, and Reston Ebola virus strains.
    Type: Application
    Filed: July 10, 2010
    Publication date: July 26, 2012
    Applicant: Crobiotix, Inc.
    Inventors: Arnab Basu, Debra M. Mills, Norton P. Peet, John D. Williams
  • Publication number: 20120184571
    Abstract: The present invention relates to the use of a quinazolinone compound of the formula (I) wherein R1, R2, R3, R4, R5 and m are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in acid addition salt form, as a vanilloid.
    Type: Application
    Filed: March 29, 2012
    Publication date: July 19, 2012
    Inventors: Timothy John RITCHIE, Andrew James Culshaw, Christopher Thomas Brain, Edward Karol Dziadulewicz, Terance William Hart
  • Patent number: 8211902
    Abstract: The present invention relates to the use of a quinazolinone compound of the formula (I) wherein R1, R2, R3, R4, R5 and m are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in acid addition salt form, as a vanilloid.
    Type: Grant
    Filed: April 19, 2011
    Date of Patent: July 3, 2012
    Assignee: Novartis AG
    Inventors: Timothy John Ritchie, Andrew James Culshaw, Christopher Thomas Brain, Edward Karol Dziadulewicz, Terance William Hart
  • Publication number: 20120165330
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: December 22, 2010
    Publication date: June 28, 2012
    Applicant: Sirtris Pharmaceuticals, Inc.
    Inventor: Chi B. Vu
  • Publication number: 20120094997
    Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, Ra, R2a, R2b, R1, and X have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: October 14, 2011
    Publication date: April 19, 2012
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Dylan B. England, Kenneth M. Gigstad, Alexandra E. Gould, Liting Ma, He Xu
  • Publication number: 20120053052
    Abstract: The present invention relates to the 3-arylquinazolin-4-one compounds of the formula I and the salts thereof, wherein n is 0, 1 or 2; X is O, S or N—R4; Y1 is N or CH; Y2 is N or C—R5; R1 is C1-C10-alkyl, C1-C10-haloalkyl, C2-C10-alkenyl, C2-C10-haloalkenyl, C2-C10-alkynyl, C2-C10-haloalkynyl, C3-C12-cycloalkyl, C5-C12-cycloalkenyl, C3-C12-cycloalkyl-C1-C4-alkyl, C5-C12-cycloalkenyl-C1-C4-alkyl, where the cycloalkyl radical and the cycloalkenyl radical in the last four mentioned radicals are unsubstituted, partially or fully halogenated and/or carry 1, 2, 3, 4, or 5 C1-C4-alkyl radicals; R2 is hydrogen, halogen, CN, C(Z)NH2, C1-C4-alkyl or C1-C4-haloalkyl, wherein Z is O, S or NR6; and the variables k, R, R3, R4, R5 and R6 are as defined in the claims. The invention also relates to the use of novel compounds of formula I for combating invertebrate pests and to a method for controlling invertebrate pests.
    Type: Application
    Filed: March 3, 2010
    Publication date: March 1, 2012
    Applicant: BASF SE
    Inventors: Steffen Gross, Karsten Körber, Wolfgang von Deyn, Florian Kaiser, Prashant Deshmukh, Joachim Dickhaut, Nina Gertrud Bandur, Arun Narine, Matthias Pohlman, Michael Puhl, Sarah Thompson, Cecille Ebuenga, Douglas D. Anspaugh, Deborah L. Culbertson, Hassan Oloumi-Sadeghi, Faraneh Oloumi
  • Patent number: 8067428
    Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 14, 2009
    Date of Patent: November 29, 2011
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-McGuire
  • Publication number: 20110195983
    Abstract: The present invention relates to the use of a quinazolinone compound of the formula (I) wherein R1, R2, R3, R4, R5 and m are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in acid addition salt form, as a vanilloid.
    Type: Application
    Filed: April 19, 2011
    Publication date: August 11, 2011
    Inventors: Timothy John Ritchie, Andrew James Culshaw, Christopher Thomas Brain, Edward Karol Dziadulewicz, Terance William Hart
  • Publication number: 20110172195
    Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.
    Type: Application
    Filed: March 15, 2011
    Publication date: July 14, 2011
    Applicant: ARIZONA BOARD OF REG. ON BEHALF OF THE UNIV. OF AZ
    Inventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
  • Publication number: 20110092489
    Abstract: Compounds represented by Structural Formula (I): are useful, for example, in the effective killing or reducing the rate of proliferation of cancer cells, such as in patients suffering from cancer. In addition to the compounds themselves, the invention provides pharmaceutical compositions of the compounds and method of treatment using the compounds.
    Type: Application
    Filed: December 22, 2006
    Publication date: April 21, 2011
    Applicant: Prolexys Pharmaceuticals ,Inc.
    Inventors: Longwu QI, Raj Gopal Venkat, Michael Pierce, Paul B. Robbins, Sudhir R. Sahasrabudhe, Robert Selliah
  • Publication number: 20110077256
    Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function by contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize hedgehog activity.
    Type: Application
    Filed: April 28, 2010
    Publication date: March 31, 2011
    Inventors: Oivin M. Guicherit, Lee Rubin
  • Patent number: 7906521
    Abstract: The present invention relates to compounds useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: September 17, 2004
    Date of Patent: March 15, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: B. Wesley Trotter, Richard Isaacs
  • Patent number: 7790731
    Abstract: The present invention is directed to a form I crystal of 2-methyl 3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone that is useful for example in the treatment of sleep disorders or various sleep disorder-associated diseases.
    Type: Grant
    Filed: February 13, 2006
    Date of Patent: September 7, 2010
    Assignee: Banyu Pharmaceutical Co. Ltd.
    Inventors: Akio Kanatani, Nagaaki Sato, Tsuyoshi Nagase, Shigeru Tokita
  • Publication number: 20100197705
    Abstract: There is described a new polymorphic form of 4-(7-Hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile having structural formula I(B) and to a method of preparing it. There is further a process or method for the manufacture of a pharmaceutically active quinazolinone compounds of the formula I wherein the symbols have the meanings given in the description, said process comprising reacting a compound of the formula II, wherein R4* is R1*—C(?O)— wherein R1* is independently selected from the group of meanings of R1 as defined for a compound of the formula I so that R1* and R1 are identical to or different from each other, or R4* is especially H, and R1 and R3, R5 and R6 are as defined for a compound of the formula I, or a salt thereof, under simultaneous or sequential condensation and cyclisation conditions with an aniline compound of the formula III, wherein R2 and m are as defined for a compound of the formula I. Further reactions and related embodiments are also claimed and disclosed.
    Type: Application
    Filed: January 6, 2010
    Publication date: August 5, 2010
    Inventors: Weichun Chen, Hong-Yong Kim, Jessica Liang, Michael Mutz, Mahavir Prashad, Christopher Towler, Ruoqiu Wu
  • Publication number: 20100152209
    Abstract: The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.
    Type: Application
    Filed: November 3, 2006
    Publication date: June 17, 2010
    Applicant: Hydra Biosciences Inc.
    Inventors: Jayhong A. Chong, Christopher Fanger, Glenn R. Larsen, William C. Lumma, JR., Anu Mahadevan, Peter Meltzer, Magdalene M. Moran, Amy Ripka, Dennis John Underwood, Manfred Weigele, Xiaoguang Zhen
  • Patent number: 7696215
    Abstract: The invention concerns a compound of the Formula (I) wherein m is 1-2 and each R1 is a group such as cyano, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is trifluoromethyl or (1-6C)alkyl; R3 is hydrogen or halogeno; and R4 is isoxazolyl; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
    Type: Grant
    Filed: February 23, 2006
    Date of Patent: April 13, 2010
    Assignee: AstraZeneca AB
    Inventors: Ian Alun Nash, Jonathan Erle Finlayson, Caroline Rachel Thompson
  • Patent number: 7622474
    Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 20, 2007
    Date of Patent: November 24, 2009
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-McGuire
  • Publication number: 20090209562
    Abstract: The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist activity, is useful in the prophylaxis or therapy of metabolic diseases, circulatory diseases, or nervous system diseases. [where, for example, Ar is a divalent group formed by eliminating two hydrogen atoms from benzene, X1 is a nitrogen atom, sulfur atom or oxygen atom, R1 is a 5- to 6-membered heteroaryl group, Ring A is a 5- to 6-membered heteroaryl ring, R2 and R3 are amino groups or alkylamino groups, and X2 is represented by formula (II): (where R4 and R5 are lower alkyl groups, and n is an integer from 2 to 4).
    Type: Application
    Filed: February 11, 2009
    Publication date: August 20, 2009
    Applicant: Banyu Pharmaceutical Co., Ltd.
    Inventors: Tsuyoshi Nagase, Nagaaki Sato, Akio Kanatani, Shigeru Tokita
  • Publication number: 20090082339
    Abstract: The invention relates to azacyclyl-substituted arylthienopyrimidinones and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one azacyclyl-substituted arylthienopyrimidinone of the invention or its derivative, and the use of the azacyclyl-substituted arylthienopyrimidinones of the invention and their derivatives as MCH antagonists.
    Type: Application
    Filed: August 14, 2008
    Publication date: March 26, 2009
    Applicant: SANOFI-AVENTIS
    Inventors: Lothar SCHWINK, Siegfried STENGELIN, Matthias GOSSEL, Gerhard HESSLER, Torsten HAACK, Petra LENNIG
  • Publication number: 20080299076
    Abstract: The present invention relates to erastin analogs, particularly compounds of formulae I and II, including compounds 1-20, 22-24, 34, and 40. The invention also relates to pharmaceutical compositions containing such analogs and to methods of treating conditions in a mammal with such analogs and pharmaceutical compositions.
    Type: Application
    Filed: February 28, 2008
    Publication date: December 4, 2008
    Inventor: Brent R. Stockwell
  • Publication number: 20080194595
    Abstract: The present invention relates to the use of a quinazolinone compound of the formula (I) wherein R1, R2, R3, R4, R5 and m are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in acid addition salt form, as a vanilloid.
    Type: Application
    Filed: June 8, 2005
    Publication date: August 14, 2008
    Inventors: Timothy John Ritchie, Andrew James Culshaw, Christopher Thomas Brain, Edward Karol Dziadulewicz, Terance William Hart
  • Publication number: 20080194597
    Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: August 20, 2007
    Publication date: August 14, 2008
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: ROBERT M. SCARBOROUGH, Wolin Huang, Charles K. Marlowe, Kim A. Kane-Maguire
  • Publication number: 20080132499
    Abstract: Compounds are provided which are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.
    Type: Application
    Filed: September 17, 2007
    Publication date: June 5, 2008
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Robert M. Scarborough, Carroll Anna Crew Scarborough, Shawn M. Bauer, Anjali Pandey
  • Patent number: 7294634
    Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed.
    Type: Grant
    Filed: July 20, 2004
    Date of Patent: November 13, 2007
    Assignee: Cytokinetics, Inc.
    Inventors: Jeffrey T. Finer, Gustave Bergnes, Whitney W. Smith, John C. Chabala, Bainian Feng
  • Patent number: 6992084
    Abstract: The invention provides compounds and compositions of the formula: wherein, the subscript n is an integer of from 0 to 4; Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl, R1 is a member selected from the group consisting of substituted or unsubstituted (C5–C15)alkyl and (C8–C14)acyl group; R2 is a member selected from the group consisting of substituted or unsubstituted (C1–C8)alkyl; each R3 is independently a substituent Y is a member selected from the group consisting of substituted or unsubstituted (C2–C8)alkylene and substituted or unsubstituted (C2–C8)heteroalkylene; Z is —NR4R5 R4 and R5 are independently selected from the group consisting of hydrogen and (C1–C8)alkyl or taken together with the nitrogen atom to which each is attached to form a heterocyclyl or heteroaryl; These compounds and compositions bind to the CXCR3 chemokine receptor and are useful for treating diseases and conditions responsive to the mo
    Type: Grant
    Filed: October 23, 2002
    Date of Patent: January 31, 2006
    Assignee: ChemoCentryx, Inc.
    Inventors: Thomas J. Schall, Daniel J. Dairaghi, Brian E. McMaster
  • Patent number: 6949535
    Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.
    Type: Grant
    Filed: October 30, 2003
    Date of Patent: September 27, 2005
    Assignee: ICOS Corporation
    Inventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
  • Patent number: 6800620
    Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K&dgr;) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K&dgr; plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K&dgr;, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K&dgr; activity, including compounds that selectively inhibit PI3K&dgr; activity. Methods of using PI3K&dgr; inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K&dgr; inhibitory compounds to inhibit PI3K&dgr;-mediated processes in vitro and in vivo.
    Type: Grant
    Filed: January 6, 2003
    Date of Patent: October 5, 2004
    Assignee: ICOS
    Inventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
  • Patent number: 6667300
    Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K&dgr;) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K&dgr; plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K&dgr;, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K&dgr; activity, including compounds that selectively inhibit PI3K&dgr; activity. Methods of using PI3K&dgr; inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K&dgr; inhibitory compounds to inhibit PI3K&dgr;-mediated processes in vitro and in vivo.
    Type: Grant
    Filed: October 19, 2001
    Date of Patent: December 23, 2003
    Assignee: ICOS Corporation
    Inventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
  • Patent number: 6630479
    Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: October 7, 2003
    Assignee: Cytokinetics, Inc.
    Inventors: Jeffrey T. Finer, Gustave Bergnes, Whitney W. Smith, John C. Chabala, Bainian Feng
  • Patent number: 6627634
    Abstract: Bicyclic heterocycles of general formula wherein: Ra to Rd, A to C and X are as defined herein, the tautomers, the stereoisomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tract, and the preparation thereof.
    Type: Grant
    Filed: March 23, 2001
    Date of Patent: September 30, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
  • Patent number: 6627755
    Abstract: The present invention relates to novel quinazolin-4-one derivatives of the formula wherein A is a benzo or thieno fused aromatic ring; B is phenyl, pyridyl or pyrimidyl; X is N or CH; and Y-Z is —CH2NH— or —NHCH2—; and to pharmaceutical compositions containing such compounds, and the use of such compounds to treat neurodegenerative, psychotropic, and drug and alcohol induced central and peripheral nervous system disorders.
    Type: Grant
    Filed: May 14, 1998
    Date of Patent: September 30, 2003
    Assignee: Pfizer INC
    Inventors: Bertrand L. Chenard, Willard M. Welch, Anthony R. Reinhold
  • Publication number: 20030176422
    Abstract: Pyridoarylphenyl oxazolidinone compounds of the formula: 1
    Type: Application
    Filed: February 6, 2002
    Publication date: September 18, 2003
    Inventors: Steven D. Paget, Michele A. Weidner-Wells, Harvey M. Werblood
  • Patent number: 6559160
    Abstract: The invention provides compounds and compositions of the formula: wherein the subscript n is an integer of from 0 to 4; Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl; R1 is a member selected from the group consisting of substituted or unsubstituted (C5-C15)alkyl; R2 is a member selected from the group consisting of substituted or unsubstituted (C1-C8)alkyl; each R3 is independently a substituent selected from -halogen, —OR′, —OC(O)R′, —NR′R″, —SR′, —R′, —CN, —NO2, —CO2R′, —CONR′R″, —C(O)R′, —OC(O)NR′R″, —NR″C(O)R′, —NR″C(O)2R′, , —NR′—C(O)NR″R′″, —NH—C(NH2)═NH, —NR′C(NH2)═NH, —NH—C(NH2)═NR—, —S(O)R′, —S(O)2R′, —
    Type: Grant
    Filed: August 25, 2000
    Date of Patent: May 6, 2003
    Assignee: Chemocentryx, Inc.
    Inventors: Thomas J. Schall, Daniel J. Dairaghi, Brian E. McMaster
  • Patent number: 6545005
    Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function by contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize hedgehog activity.
    Type: Grant
    Filed: September 15, 2000
    Date of Patent: April 8, 2003
    Assignee: Curtis, Inc.
    Inventors: Anthony David Baxter, Edward Andrew Boyd, Oivin M. Guicherit, Stephen Price, Lee D. Rubin