Cyano Attached Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/230)
  • Patent number: 10196373
    Abstract: In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: August 5, 2014
    Date of Patent: February 5, 2019
    Assignees: THE GOVERNING COUNCIL OF THE UNIVERSITY OF TORONTO, UNIVERSITY OF CENTRAL FLORIDA RESEARCH FOUNDATION, INC.
    Inventors: James Turkson, Patrick Gunning
  • Patent number: 9023869
    Abstract: Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N?-substituted aryl urea compounds; N-substituted aryl, N?-substituted heteroaryl urea compounds; N-substituted aryl, N?-substituted aryl thiourea compounds and N-substituted aryl, N?-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.
    Type: Grant
    Filed: November 26, 2012
    Date of Patent: May 5, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Publication number: 20150031726
    Abstract: Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N?-substituted aryl urea compounds; N-substituted aryl, N?-substituted heteroaryl urea compounds; N-substituted aryl, N?-substituted aryl thiourea compounds and N-substituted aryl, N?-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.
    Type: Application
    Filed: October 15, 2014
    Publication date: January 29, 2015
    Inventors: Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Patent number: 8921555
    Abstract: The present invention relates to substituted 1,3,8-triazaspiro[4.5]decame-2,4-diones useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: June 7, 2010
    Date of Patent: December 30, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joan M. Pierce, Jeffrey J. Hale, Shouwu Miao, Petr Vachal
  • Publication number: 20140371239
    Abstract: The present invention relates generally to compounds that inhibit the binding of menin and MLL or MLL fusion proteins and methods of use thereof. In particular embodiments, the present invention provides compositions comprising piperidine-containing compounds and methods of use thereof to inhibit the interaction of menin with MLL oncoproteins (e.g., MLL1, MLL2, MLL-fusion oncoproteins), for example, for the treatment of leukemia, solid cancers, diabetes, and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, MLL-PTD and/or menin.
    Type: Application
    Filed: June 11, 2014
    Publication date: December 18, 2014
    Inventors: Jolanta Grembecka, Tomasz Cierpicki, Sunil Kumar Upadhyay, Shaun R. Stauffer, Rocco D. Gogliotti, Timothy J. Senter
  • Patent number: 8895746
    Abstract: The present invention provides compounds S3I-201.1066 (Formula 1) and S3I-201.2096 (Formula 2) as selective Stat3 binding agents that block Stat3 association with cognate receptor pTyr motifs, Stat3 phosphorylation and nuclear translocation, Stat3 transcriptional function, and consequently induced Stat3-specific antitumor cell effects in vitro and antitumor response in vivo.
    Type: Grant
    Filed: November 10, 2013
    Date of Patent: November 25, 2014
    Assignees: University of Central Florida Research Foundation, Inc., The Governing Council of the University of Toronto
    Inventors: James Turkson, Patrick Gunning
  • Patent number: 8895551
    Abstract: The invention relates to acrylamide compounds of Formula I mentioned below. The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: April 2, 2010
    Date of Patent: November 25, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hidenori Mikamiyama, Akira Matsumura, Moriyasu Masui, Kosuke Anan, Kayoko Hata
  • Publication number: 20140066446
    Abstract: Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists, e.g., compounds of Formula I, and pharmaceutical compositions thereof: Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Application
    Filed: August 30, 2013
    Publication date: March 6, 2014
    Applicant: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Garrett Thomas Potter
  • Patent number: 8586749
    Abstract: The present invention provides compounds S3I-201.1066 (Formula 1) and S3I-201.2096 (Formula 2) as selective Stat3 binding agents that block Stat3 association with cognate receptor pTyr motifs, Stat3 phosphorylation and nuclear translocation, Stat3 transcriptional function, and consequently induced Stat3-specific antitumor cell effects in vitro and antitumor response in vivo.
    Type: Grant
    Filed: April 5, 2010
    Date of Patent: November 19, 2013
    Assignees: University of Central Florida Research Foundation, Inc., Governing Council of the University of Toronto
    Inventors: James Turkson, Patrick Gunning
  • Publication number: 20130225621
    Abstract: In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: August 2, 2011
    Publication date: August 29, 2013
    Applicants: University of Toronto Mississauga, University of Central Florida Research Foundation, Inc.
    Inventors: James Turkson, Patrick Gunning
  • Patent number: 8487109
    Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R1; R2; R3; R4; R5; J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process for aryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional aryl-1-alkynes of the formula I.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: July 16, 2013
    Assignee: Sanofi
    Inventors: Omar Rkyek, Marc Nazare, Andreas Lindenschmidt, Matthias Urmann, Nis Halland, Jorge Alonso
  • Publication number: 20130079372
    Abstract: Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N?-substituted aryl urea compounds; N-substituted aryl, N?-substituted heteroaryl urea compounds; N-substituted aryl, N?-substituted aryl thiourea compounds and N-substituted aryl, N?-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.
    Type: Application
    Filed: November 26, 2012
    Publication date: March 28, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventors: Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Patent number: 8399456
    Abstract: Provided herein are 2,5-disubstituted arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Grant
    Filed: April 21, 2010
    Date of Patent: March 19, 2013
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Marie Chantal Siu-Ying Tran, Erik Dean Raaum
  • Publication number: 20130065889
    Abstract: Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists, e.g., compounds of Formula I, and pharmaceutical compositions thereof: Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Application
    Filed: October 26, 2012
    Publication date: March 14, 2013
    Applicant: AXIKIN PHARMACEUTICALS, INC.
    Inventor: Axikin Pharmaceuticals, Inc.
  • Publication number: 20120287354
    Abstract: The present invention relates to an electro-optical light modulation element and to electro-optical displays and display systems, such as television screens and computer monitors, containing elements of this type. The light modulation elements according to the invention contain a mesogenic modulation medium which is in the isotropic phase during operation of the light modulation elements and are particularly distinguished by very short response times in addition to good contrast and low viewing-angle dependence. The mesogenic modulation media used in the electro-optical light modulation elements are likewise a subject-matter of the present invention.
    Type: Application
    Filed: June 7, 2012
    Publication date: November 15, 2012
    Applicant: MERCK Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Michael HECKMEIER, Achim Götz
  • Publication number: 20120226033
    Abstract: The present invention relates to novel benzene-carboxamide compounds having a structure that corresponds to the general formula (I) below: and also to their method of synthesis and to their use in pharmaceutical compositions intended for use in human or veterinary medicine or else to their use in cosmetic compositions.
    Type: Application
    Filed: September 16, 2010
    Publication date: September 6, 2012
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Laurence Clary, Jean-Claude Pascal
  • Publication number: 20120130079
    Abstract: The present invention provides compounds S3I-201.1066 (Formula 1) and S3I-201.2096 (Formula 2) as selective Stat3 binding agents that block Stat3 association with cognate receptor pTyr motifs, Stat3 phosphorylation and nuclear translocation, Stat3 transcriptional function, and consequently induced Stat3-specific antitumor cell effects in vitro and antitumor response in vivo.
    Type: Application
    Filed: April 5, 2010
    Publication date: May 24, 2012
    Applicants: UNIVERSITY OF TORONTO MISSISSAUGA, UNIVERSITY OF CENTRAL FLORIDA RESEARCH FOUNDATION, INC.
    Inventors: James Turkson, Patrick Gunning
  • Publication number: 20120022069
    Abstract: The invention relates to acrylamide compounds of Formula I mentioned below. The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: April 2, 2010
    Publication date: January 26, 2012
    Applicant: Shionogi & Co., Ltd.
    Inventors: Hidenori Mikamiyama, Akira Matsumura, Moriyasu Masui, Kosuke Anan, Kayoko Hata
  • Publication number: 20110275670
    Abstract: The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.
    Type: Application
    Filed: June 4, 2009
    Publication date: November 10, 2011
    Inventors: Emma Chapman, Michael Higginbottom, Anne Viet-Anh Horgan (nee Nguyen), Iain Simpson
  • Publication number: 20110218217
    Abstract: This invention relates to novel piperidine-4-propionamide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: August 25, 2009
    Publication date: September 8, 2011
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, John Paul Redrobe, Elsebet Østergaard Nielsen
  • Publication number: 20110105506
    Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.
    Type: Application
    Filed: May 28, 2010
    Publication date: May 5, 2011
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
  • Patent number: 7884102
    Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.
    Type: Grant
    Filed: April 28, 2008
    Date of Patent: February 8, 2011
    Assignee: Adolor Corporation
    Inventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
  • Publication number: 20100317630
    Abstract: The invention is directed to methods of using antagonists selective for the metabotropic mGlu5 receptor to treat conditions of neuromuscular dysfunction of the lower urinary tract in a mammal. Provided are methods of treating a mammal suffering from a condition of neuromuscular dysfunction of the lower urinary tract by administering a selective mGlu5 antagonist. The selective mGlu5 antagonist may be administered alone or in combination with one or more additional therapeutic agents for treating such a condition. Also provided are methods of identifying selective mGlu5 antagonists that are useful for treating neuromuscular dysfunction of the lower urinary tract in a mammal. Methods for treating migraine and gastroesophageal reflux disease (GERD) using selective mGlu5 antagonists are also disclosed.
    Type: Application
    Filed: February 4, 2010
    Publication date: December 16, 2010
    Applicant: RECORDATI IRELAND LIMITED
    Inventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Elena Poggesi, Davide Graziani
  • Patent number: 7834063
    Abstract: This invention relates to benzonitryl and nitrobenzyl derivatives that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds. These compounds are useful, for example, in the treatment or prophylaxis of conditions or disorders that respond to selective androgen receptor modulation.
    Type: Grant
    Filed: October 13, 2005
    Date of Patent: November 16, 2010
    Assignee: GlaxoSmithKline LLC
    Inventors: Philip Stewart Turnbull, Andrew Lamont Larkin, Istvan Kaldor, Rodolfo Cadilla, David John Cowan, Eugene Lee Stewart
  • Publication number: 20100273785
    Abstract: Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists of Formula I or II, and pharmaceutical compositions thereof: wherein X, Y, Z, and R1-R5 are as defined herein. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Application
    Filed: April 21, 2010
    Publication date: October 28, 2010
    Inventors: Tai Wei Ly, Garrett Thomas Potter
  • Publication number: 20100273782
    Abstract: Provided herein are 2,5-disubstituted arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Application
    Filed: April 21, 2010
    Publication date: October 28, 2010
    Applicant: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Marie Chantal Siu-Ying Tran, Erik Dean Baaum
  • Publication number: 20100261910
    Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R1; R2; R3; R4; R5; J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process for aryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional aryl-1-alkynes of the formula I.
    Type: Application
    Filed: December 23, 2009
    Publication date: October 14, 2010
    Applicant: sanofi-aventis
    Inventors: Omar RKYEK, Marc NAZARE, Andreas LINDENSCHMIDT, Matthias URMANN, Nis HALLAND, Jorge ALONSO
  • Publication number: 20100256162
    Abstract: Compounds of general formula (I) in which R1, m, X, n, Y and R3 have any of the meanings given in the specification, have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.
    Type: Application
    Filed: October 10, 2006
    Publication date: October 7, 2010
    Applicant: AGY THERAPEUTICS, INC.
    Inventor: Connie L Sun
  • Publication number: 20100256163
    Abstract: The present invention relates to compounds which have therapeutic effects against disorders in the central nervous system, and in particular new 4-(ortho,meta-disubstituted phenyl)-1-alkypiperidines and piperazines. wherein R1, R2, R3 and X are as defined.
    Type: Application
    Filed: June 14, 2010
    Publication date: October 7, 2010
    Inventors: Clas Sonesson, Lars Swanson, Nicholas Ross Waters
  • Patent number: 7763639
    Abstract: The present invention relates to compounds which have therapeutic effects against disorders in the central nervous system, and in particular new 4-(ortho, meta-disubstituted phenyl)-1-alkypiperidines and piperazines. wherein R1, R2, R3 and X are as defined.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: July 27, 2010
    Assignee: NSAB, Filial AF Neurosearch Sweden AB, Sverige
    Inventors: Clas Sonesson, Lars Swanson, Nicholas Ross Waters
  • Patent number: 7662849
    Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
    Type: Grant
    Filed: June 4, 2004
    Date of Patent: February 16, 2010
    Assignee: ViroBay, Inc.
    Inventors: John W. Patterson, Soon H. Woo
  • Patent number: 7645754
    Abstract: The subject invention provides compounds having the structure: wherein, R1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(?O)NRaRb, —NRaRb, —NRaC(?O)NRaRb, —NRaC(?O)ORa, —OC(?O)NRaRb, or —NHC(?O) Ra; R2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(?O)NRaRb, —NRaRb, —NRaC(?O)NRaRb, —NRaC(?O)ORa, —OC(?O)NRaRb, or —NHC(?O)Ra, or R1, R2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH2)2OH or —CH2C(?O)OH; R3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C1-C15)alkyl, (C1-C15)alkoxy, or —NRaRb; R4 is hydrogen or substituted or unsubstituted (C1-C15)alkyl; R5 is —(CH2)mOR6, —CHNOR7, —C(?O)NR8R9, —(CH2)mC(?O)OR10, —(CH2)kC(?O)NR11R12; wherein R6 is a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl
    Type: Grant
    Filed: June 19, 2007
    Date of Patent: January 12, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Arlindo Castelhano, Bryan McKibben, Arno Steinig
  • Publication number: 20090186884
    Abstract: Described are diaminopropanols of which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of renin activity or in the treatment of aspartic protease mediated disorders. Also described is a method for the use of the diaminopropanols in ameliorating or treating renin related disorders in a subject in need thereof.
    Type: Application
    Filed: April 5, 2007
    Publication date: July 23, 2009
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty
  • Patent number: 7452891
    Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
    Type: Grant
    Filed: January 28, 2005
    Date of Patent: November 18, 2008
    Assignee: Schering Corporation
    Inventors: John W. Clader, Hubert B. Josien, Anandan Palani, Tin Yau Chan
  • Publication number: 20080255124
    Abstract: This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.
    Type: Application
    Filed: October 13, 2005
    Publication date: October 16, 2008
    Applicant: Smithkline Beecham Corporation
    Inventors: Philip Stewart Turnbull, Andrew Lamont Larkin, Istvan Kaldor, Rodolfo Cadilla, David John Cowan, Eugene Stewart
  • Patent number: 7381721
    Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.
    Type: Grant
    Filed: March 17, 2003
    Date of Patent: June 3, 2008
    Assignee: Adolor Corporation
    Inventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
  • Patent number: 7259173
    Abstract: This invention relates to organic compounds of formula I, in which Ar1 is unsubstituted phenyl substituted by one or more halogen atoms; Ar2 is unsubstituted phenyl or phenyl substituted by one or more substituents selected from the group consisting of halogen, cyano and C1-C8-alkoxy; R1 is hydrogen or methyl optionally substituted by hydroxy; R10 is hydrogen or hydroxy; and pharmaceutically acceptable salts thereof. Compositions containing them, methods for their preparation and their use as pharmaceuticals are also described.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: August 21, 2007
    Assignee: Novartis AG
    Inventors: Gurdip Bhalay, Clive Victor Walker
  • Patent number: 7074820
    Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
    Type: Grant
    Filed: April 23, 2001
    Date of Patent: July 11, 2006
    Assignee: AstraZeneca AB
    Inventor: Thomas Antonsson
  • Patent number: 7015218
    Abstract: The present invention relates to a compound of the formula wherein R1 is substituted aryl, heteroaryl and the like, R2 and R3 are hydrogen, alkyl, halogen, hydroxyl group and the like, Q is N, CH and the like, W is hydrogen, alkyl, hydroxycarbonylalkyl and the like, X is halogen, cyano, nitro, amino and the like, X? is hydrogen, halogen, cyano, nitro, and Y is alkyl, hydroxyl group, alkoxy, mercapto and the like and a salt thereof, and a medicine containing the said compound. The compound of the present invention shows a superior inhibitory effect on activated lymphocytes proliferation and is useful as an agent for the prophylaxis or treatment of various autoimmune diseases.
    Type: Grant
    Filed: February 10, 2000
    Date of Patent: March 21, 2006
    Assignee: Mitsubishi Pharma Corporation
    Inventors: Hiroyuki Ushio, Seigo Ishibuchi, Youichiro Naito, Naoki Sugiyama, Takafumi Kawaguchi, Kenji Chiba, Makio Ohtsuki, Yoichi Naka
  • Patent number: 6998488
    Abstract: A novel process is provided for the preparation of 4-aryl piperidines, and the useful intermediates obtained therein. These compounds are intermediates for the synthesis of melanocortin-4 receptor (MC-4R), which are useful for the treatment of disorders such as obesity, diabetes, male sexual dysfunction, and female sexual dysfunction.
    Type: Grant
    Filed: March 8, 2004
    Date of Patent: February 14, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Genevieve N. Boice, Karen M. Conrad, Edward G. Corley, Louis Matty, Jr., Jerry A. Murry, Cecile G. Savarin
  • Patent number: 6995283
    Abstract: The present invention is directed to beazophenone compounds useful in the inhibition of HIV reverse transcriptase, particularly its resistant varieties.
    Type: Grant
    Filed: February 28, 2002
    Date of Patent: February 7, 2006
    Assignee: SmithKline Beecham Corporation
    Inventor: Joseph Howing Chan
  • Patent number: 6903120
    Abstract: New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, OSO2CH3, SOR3, SO2R3, COR3, NO2, or CONHR3 and when X is CH or C R1 may also be CF3, CN, F, Cl, Br, or I; R2 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4,-trifluorobutyl, or —(CH2)—R4; R3 is a C1-C3 alkyl CF3, or N(R2)2; R4 is a C3-C6 cycloalkyl, 2-tetrahydrofurane or 3-tetra-hydrofurane, as well as pharmaceutically acceptable salts thereof are disclosed.
    Type: Grant
    Filed: December 22, 2000
    Date of Patent: June 7, 2005
    Assignee: A. Carlsson Research AB
    Inventors: Clas Sonesson, Ingela Marianne Svan, Anders Kristoffer Lilja, Liselott Lilja Rönnqvist, Jenny Maria Carlberg, Susanna Waters, Nicholas Waters, Joakim Tedroff, Bengt Andersson
  • Patent number: 6887889
    Abstract: In one embodiment, this invention provides a novel class of compounds as antagonists of the MCH receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration or one or more of diseases associated with the MCH receptor.
    Type: Grant
    Filed: April 10, 2002
    Date of Patent: May 3, 2005
    Assignee: Pharmacopeia Drug Discovery, Inc.
    Inventors: Douglas W. Hobbs, Tao Guo, Rachael C. Hunter, Huizhong Gu, Suresh D. Babu, Yuefei Shao
  • Publication number: 20040186287
    Abstract: The invention relates to novel cyclic imines of the formula (I) 1
    Type: Application
    Filed: January 30, 2004
    Publication date: September 23, 2004
    Inventors: Andrew Plant, Gerd Kleefeld, Thorsten Potter, Christoph Erdelen, Norbert Mencke, Andreas Turberg, Ulrike Wachendorff-Neumann
  • Publication number: 20040181070
    Abstract: A novel process is provided for the preparation of 4-aryl piperidines, and the useful intermediates obtained therein. These compounds are intermediates for the synthesis of melanocortin-4 receptor (MC-4R), which are useful for the treatment of disorders such as obesity, diabetes, male sexual dysfunction, and female sexual dysfunction.
    Type: Application
    Filed: March 8, 2004
    Publication date: September 16, 2004
    Inventors: Genevieve N. Boice, Karen M. Conrad, Edward G. Corley, Louis Matty, Jerry A. Murry, Cecile G. Savarin
  • Publication number: 20040180892
    Abstract: The present invention relates to urotensin II receptor antagonists, CCR-9 antagonists, pharmaceutical compositions containing them and their use.
    Type: Application
    Filed: February 18, 2004
    Publication date: September 16, 2004
    Applicant: Encysive Pharmaceuticals Inc.
    Inventors: Chengde Wu, C. Eric Anderson, Huong Bui, Daxin Gao, Jamal Kassir, Wen Li, Junmei Wang, Robert V. Market
  • Patent number: 6753336
    Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.
    Type: Grant
    Filed: March 11, 2003
    Date of Patent: June 22, 2004
    Assignee: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Andrew Thurkauf, Alan Hutchison
  • Publication number: 20030208068
    Abstract: The present invention relates to processes for the production of &agr;-aryl-&bgr;-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.
    Type: Application
    Filed: March 13, 2003
    Publication date: November 6, 2003
    Inventors: Jiacheng Zhou, Lynette May Oh, Philip Ma
  • Patent number: 6642239
    Abstract: Dipeptide nitrile Cathepsin K inhibitors of formula I, and pharmaceutically acceptable salts or esters thereof: In which R1 and R2 are independently H or C1-C7lower alkyl, or R1 and R2 together with the carbon atom to which they are attached form a C3-C8cycloalkyl ring, and Het is an optionally substituted nitrogen-containing heterocyclic substituent, are provided, useful e.g. for therapeutic or prophylactic treatment of a disease or medical condition in which cathepsin K is implicated.
    Type: Grant
    Filed: February 7, 2001
    Date of Patent: November 4, 2003
    Assignee: Novartis AG
    Inventor: Martin Missbach
  • Patent number: 6642386
    Abstract: The invention is concerned with water soluble N-(4-carbamimidoyl-phenyl)-glycine derivatives of formula (I) wherein R1 to R4 and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.
    Type: Grant
    Filed: January 24, 2003
    Date of Patent: November 4, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Katrin Groebke Zbinden, Ulrike Obst