Nitrogen Attached Indirectly To The Thiocarbonyl By Nonionic Bonding Patents (Class 564/27)
  • 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: 8859812
    Abstract: Described herein are compounds of formula (I), related compositions, and their use, for example in the formation of ?-amino acids or a precursor thereof such as an ?-aminonitrile.
    Type: Grant
    Filed: September 8, 2010
    Date of Patent: October 14, 2014
    Assignee: President and Fellows of Harvard College
    Inventors: Eric N. Jacobsen, Stephan J. Zuend
  • Publication number: 20140127130
    Abstract: The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.
    Type: Application
    Filed: January 9, 2014
    Publication date: May 8, 2014
    Applicant: HAMMERSMITH IMANET LIMITED
    Inventors: ERIK ARSTAD, MATTHIAS EBERHARD GLASER
  • Patent number: 8629299
    Abstract: The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.
    Type: Grant
    Filed: May 20, 2013
    Date of Patent: January 14, 2014
    Assignee: Hammersmith Imanet Limited
    Inventors: Erik Arstad, Matthias Eberhard Glaser
  • Publication number: 20140011857
    Abstract: The invention provides for novel compounds which are inhibitors of lysine-specific demethylase 1 (LSD1). Such compounds may be used to treat disorders, including cancer.
    Type: Application
    Filed: September 12, 2011
    Publication date: January 9, 2014
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Robert A. Casero, Ian Bytheway, Patrick M. Woster
  • Publication number: 20130261178
    Abstract: A compound of formula I-0, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein Z1 is C1-C4 linear or branched alkyl or alkenyl; R4 is selected from unsubstituted and substituted C3-C3 cycloalkyl, C1-C8 linear or branched alkyl, C2-5 alkenyl, C6-C10 heteroaryl or aryl, or C3-C8 heterocyclyl which may be part unsaturated, and combinations thereof; Z is linear C2-3 alkylene; X1 is selected from NH and O; X2 is selected from unsaturated C and unsaturated S; and X3 is selected from NH and CH2; or one of X1 and X3 is a single bond; or X1 is O and X2 and X3 together are a single bond; and R7 is selected from oxo, F, Cl, Br, CN, NH2, NR92, NO2, CF3, OR9, COR9, OCOR9, COOR9, NR9COR9, CONR92SO2NR92, NR9SO2R9; and R8 is selected from C1-5 alkyl, C1-5 alkoxyl, C2-5 alkenyl or alkynyl, C6-10 aryl and C3-8 cycloalkyl and combinations thereof, which may be unsubstituted or further substituted by one or more F, Cl, Br, CN, NH2, NR32, NO2, CF3;
    Type: Application
    Filed: July 5, 2010
    Publication date: October 3, 2013
    Inventors: Shailesh Mistry, Etienne Daras, Christophe Fromont, Gopal Jadhav, Peter Martin Fischer, Barrie Kellam, Stephen John Hill, Jillian Glenda Baker
  • Publication number: 20130244944
    Abstract: Provided herein are self-assembling compounds that can form ion channels in lipid bilayers or cell membranes and ion-channel-forming compositions comprising the self-assembling compounds. Also provided are methods of making and using the ion channels formed from a plurality of molecules of the self-assembling compounds. Further, provided are methods of treating or preventing conditions and diseases that are related to the dysfunction of ion channels, including chloride channels.
    Type: Application
    Filed: December 31, 2012
    Publication date: September 19, 2013
    Applicants: VERSITECH LIMITED, THE UNIVERSITY OF HONG KONG
    Inventors: Dan Yang, Xiang Li, Huiyan Zha
  • Publication number: 20130158022
    Abstract: The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate of the compound, and to a composition comprising the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents. The present invention also relates to use of the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, and for preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.
    Type: Application
    Filed: May 14, 2010
    Publication date: June 20, 2013
    Applicant: CHINESE PLA GENERAL HOSPITAL
    Inventors: Kunlun He, Song Li, Wu Zhong, Juan Liu, Lili Wang, Xin Li, Guoliang Hu, Jie Wang, Long Long, Junhai Xiao, Zhibing Zheng, Wei Li, Ruijun Li, Chunlei Liu, Jie Tang
  • Publication number: 20130137755
    Abstract: The present invention relates to a novel delivery system for delivering therapeutic agents into living cells, and more particularly, to novel chemical moieties that are designed capable of targeting and/or penetrating cells or other targets of interest and further capable of binding therapeutic agents to be delivered to these cells, and to delivery systems containing same.
    Type: Application
    Filed: October 22, 2012
    Publication date: May 30, 2013
    Applicant: Segev Laboratories Limited
    Inventor: Segev Laboratories Limited
  • Patent number: 8445721
    Abstract: The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: May 21, 2013
    Assignee: Hammersmith Imanet Limited
    Inventors: Erik Arstad, Matthias Eberhard Glaser
  • Publication number: 20130078283
    Abstract: Disclosed herein is a compound of structure (A): In this compound, X is either O or S, R1 is a rigid group, R2 is a hydrophilic group such that (A) is capable of self-assembly in water, and R3 is an organic group.
    Type: Application
    Filed: January 6, 2011
    Publication date: March 28, 2013
    Inventors: Yi-Yan Yang, Shrinivas Venkataraman
  • Publication number: 20130066109
    Abstract: Described herein are compounds of formula (I), related compositions, and their use, for example in the formation of ?-amino acids or a precursor thereof such as an ?-aminonitrile.
    Type: Application
    Filed: September 8, 2010
    Publication date: March 14, 2013
    Applicant: PRESIDENTS AND FELLOWS OF HARVARD COLLEGE
    Inventors: Eric N. Jacobsen, Stephan J. Zuend
  • Publication number: 20120322877
    Abstract: The invention provides for novel (bis)urea and (bis)thiourea compounds which are inhibitors of lysine-specific demethylase 1 (LSD1). Such compounds may be used to treat disorders, including cancer.
    Type: Application
    Filed: August 18, 2010
    Publication date: December 20, 2012
    Inventors: Robert A. Casero, Patrick M. Woster
  • Patent number: 8148575
    Abstract: The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.
    Type: Grant
    Filed: April 20, 2007
    Date of Patent: April 3, 2012
    Assignee: Hammersmith Imanet Limited
    Inventors: Erik Arstad, Matthias Eberhard Glaser
  • Patent number: 8084641
    Abstract: The present invention is directed to compositions comprising organocatalysts that facilitate stereo-selective reactions and the method of their synthesis and use. Particularly, the invention relates to metal-free organocatalysts for facilitation of stereo-selective reactions, and the method of their synthesis and use.
    Type: Grant
    Filed: October 11, 2006
    Date of Patent: December 27, 2011
    Assignee: STC.UNM
    Inventor: Wei Wang
  • Patent number: 8071650
    Abstract: The present invention relates to novel thiourea derivatives as a modulator for vanilloid receptor (VR) and the pharmaceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.
    Type: Grant
    Filed: March 26, 2007
    Date of Patent: December 6, 2011
    Assignee: Pacific Corporation
    Inventors: Young Ger Suh, Uh Taek Oh, Hee Doo Kim, Jee Woo Lee, Hyeung Geun Park, Ok Hui Park, Yong Sil Lee, Young Ho Park, Yung Hyup Joo, Jin Kyu Choi, Kyung Min Lim, Sun Young Kim, Jin Kwan Kim, Hyun Ju Koh, Joo Hyun Moh, Yeon Su Jeong, Jung Bum Yi, Young Im Oh
  • Patent number: 7964642
    Abstract: The invention relates to compounds of formula (I), wherein R, R1, R2, X and n are as defined in the description, and their use for the preparation of pharmaceutical compositions for the treatment of inflammatory states.
    Type: Grant
    Filed: June 16, 2005
    Date of Patent: June 21, 2011
    Assignee: Pharmeste S.R.L.
    Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti
  • Patent number: 7718671
    Abstract: Substituted arylthiourea compounds of Formula I, and the pharmaceutically acceptable salts of such compounds, useful as antiviral agents, are provided herein. Certain substituted arylthioureas disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions containing one or more substituted arylthiourea compounds and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein. Such pharmaceutical compositions may contain a substituted arylthiourea as the only active agent or may contain a combination of a substituted arylthiourea derivative and one or more other pharmaceutically active agents. Methods of treating Hepatitis C viral infections in mammals are also provided herein.
    Type: Grant
    Filed: July 8, 2004
    Date of Patent: May 18, 2010
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Avinash Phadke, Jesse Quinn, Junko Ohkanda, Andrew Thurkauf, Yiping Shen, Cuixian Liu, Dawei Chen, Shouming Li, Xiangzhu Wang
  • Publication number: 20090253919
    Abstract: Chiral thioureas are effective catalysts for the borane reduction of prochiral ketones to optically active alcohols. A prochiral ketone may be reduced to an optically active alcohol in the presence of a substantially sub-stoichiometric amount of chiral thiourea. The asymmetric thiourea compound of the present invention may be produced according to a production method described herein.
    Type: Application
    Filed: April 3, 2008
    Publication date: October 8, 2009
    Applicant: Board of Regents
    Inventors: Derun Li, John R. Falck
  • Publication number: 20090253799
    Abstract: Provided herein are divalent hydrazide-polyethylene glycol conjugates that inhibit the ion transport activity of a cystic fibrosis transmembrane conductance regulator (CFTR). The conjugates described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, secretory diarrhea.
    Type: Application
    Filed: April 3, 2009
    Publication date: October 8, 2009
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Alan S. Verkman, Nitin D. Sonawane
  • Publication number: 20090247627
    Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: March 31, 2009
    Publication date: October 1, 2009
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
  • Publication number: 20090215902
    Abstract: The present invention is directed to the use of a compound of formula (I) or pharmaceutically acceptable salt thereof, for the treatment of disorders mediated by the melanocortin-5 receptor, particularly dermatological disorders; and further directed to pharmaceutical compositions containing the compound of formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 20, 2009
    Publication date: August 27, 2009
    Inventors: Magdalena Eisinger, Fa Zhang
  • Patent number: 7579378
    Abstract: The invention relates to sulfonamido derivatives of formula (I) wherein R1-R7 are as defined in the description. Compounds (I) antagonize the vanilloid receptor and can be used for the preparation of medicaments for the treatment of inflammatory states.
    Type: Grant
    Filed: October 18, 2005
    Date of Patent: August 25, 2009
    Assignee: Pharmeste S.R.L.
    Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti
  • Patent number: 7560591
    Abstract: Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta p
    Type: Grant
    Filed: April 30, 2008
    Date of Patent: July 14, 2009
    Assignee: Rotta Research Laboratorium S.p.A.
    Inventors: Francesco Makovec, Simona Zanzola, Roberto Artusi, Lucio Claudio Rovati
  • Publication number: 20090137594
    Abstract: The present invention relates to pentafluorosulphanyl-substituted compounds, methods for their production, medicaments containing such compounds and the use of such compounds for producing medicaments.
    Type: Application
    Filed: May 17, 2006
    Publication date: May 28, 2009
    Applicant: Gruenenthal GmgH
    Inventors: Robert Frank, Bernd Sundermann, Hans Schick
  • Publication number: 20090118374
    Abstract: The invention relates to sulfonamido derivatives of formula (I) wherein R1-R7 are as defined in the description. Compounds (I) antagonize the vanilloid receptor and can be used for the preparation of medicaments for the treatment of inflammatory states.
    Type: Application
    Filed: October 18, 2005
    Publication date: May 7, 2009
    Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti
  • Publication number: 20090087379
    Abstract: The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.
    Type: Application
    Filed: April 20, 2007
    Publication date: April 2, 2009
    Inventors: Erik Arstad, Matthias Eberhard Glaser
  • Publication number: 20090088588
    Abstract: The present invention is directed to compositions comprising organocatalysts that facilitate stereo-selective reactions and the method of their synthesis and use. Particularly, the invention relates to metal-free organocatalysts for facilitation of stereo-selective reactions, and the method of their synthesis and use.
    Type: Application
    Filed: October 11, 2006
    Publication date: April 2, 2009
    Inventor: Wei Wang
  • Patent number: 7351389
    Abstract: Novel metal-chelate complexes comprising aminocarboxylate ligands including substituted aromatic amide moieties, such as those having the formula wherein R13, A1, R1 and R2 are as defined herein, are disclosed.
    Type: Grant
    Filed: October 13, 2004
    Date of Patent: April 1, 2008
    Assignee: Bracco International B.V.
    Inventors: Radhakrishna K. Pillai, Sang I. Kang, Edmund R. Marinelli, Ramachandran S. Ranganathan, Michael F. Tweedle
  • Patent number: 7202269
    Abstract: Certain ?-, ?-, and ?-amino acid derivatives are disclosed as selective GlyT2 inhibitors for the treatment of central nervous system (CNS) conditions such as muscle spasticity, tinnitus, epilepsy and neuropathic pain.
    Type: Grant
    Filed: October 28, 2004
    Date of Patent: April 10, 2007
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Tristin K. Barclay, Alejandro Santillán, Jr., Liu Y. Tang, Hariharan Venkatesan, Ronald L. Wolin
  • Patent number: 7173045
    Abstract: The invention concerns 4-aminomethyl-1-aryl-cyclohexylamine compounds, methods for producing same, pharmaceutical formulations containing said compounds and the use of 4-aminomethyyl-1-aryl-cyclohexylamine compounds for producing medicines and in related methods of treatment.
    Type: Grant
    Filed: May 10, 2005
    Date of Patent: February 6, 2007
    Assignee: Gruenenthal GmbH
    Inventors: Bernd Sundermann, Hans Schick, Claudia Hinze
  • Patent number: 7115664
    Abstract: One aspect of the present invention relates to novel peptidomimetic compounds. A second aspect of the present invention relates to the use of the novel peptidomimetic compounds as ligands—agonists or antagonists—for various cellular receptors, e.g., G-protein-coupled receptors and opioid receptors, and various cellular ion channels, e.g., sodium and calcium. In certain embodiments, compounds of the present invention preferentially or selectively inhibit sodium or calcium ion channels. In certain embodiments, compounds of the present invention preferentially or selectively agonize or antagonize $gm opioid receptors.
    Type: Grant
    Filed: February 27, 2001
    Date of Patent: October 3, 2006
    Assignee: Sepracor Inc.
    Inventors: Paul E. Persons, Joanne M. Holland, James Hauske
  • Patent number: 7094807
    Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.
    Type: Grant
    Filed: November 18, 2003
    Date of Patent: August 22, 2006
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Dawei Chen, Milind Deshpande, Andrew Thurkauf, Avinash Phadke, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
  • Patent number: 7067553
    Abstract: The present invention relates to thiourea compounds and the pharmaceutical compositions containing the same, and particularly, to novel thiourea compounds as an antagonist against vanilloid receptor (VR) and the pharmaceutical compositions thereof. As diseases associated with the activity of vanilloid receptor, pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.
    Type: Grant
    Filed: August 20, 2001
    Date of Patent: June 27, 2006
    Assignee: Pacific Corporation
    Inventors: Young Ger Suh, Uh Taek Oh, Hee Doo Kim, Jee Woo Lee, Hyeung Geun Park, Young Ho Park, Jung Bum Yi
  • Patent number: 7034015
    Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.
    Type: Grant
    Filed: August 28, 2002
    Date of Patent: April 25, 2006
    Assignee: Leo Pharma A/S
    Inventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
  • Patent number: 6949567
    Abstract: The invention relates to new diphenylurea having the formula (I) or a salt thereof, where Y is C?O, C?S, C?NH, (C?O)2 or SO2; and to processes for the preparation of these compounds and to their use in the treatment of protozoal diseases and to diseases where the inhibition of intracellular protein-degradation pathways is of benefit.
    Type: Grant
    Filed: February 26, 2002
    Date of Patent: September 27, 2005
    Assignee: 4SC AG
    Inventors: Andrea Aschenbrenner, Katharina Aulinger Fuchs, Matthias Dormeyer, Gabriel Garcia, Bernd Kramer, Jürgen Kraus, Rolf Krauss, Johan Leban, Stefano Pegoraro, Wael Saeb, Kristina Wolf
  • Patent number: 6946474
    Abstract: The present invention provides trichloroethyl-sulfonylurea-containing compounds that inhibit glycing transporters, pharmaceutical compositions comprising such compounds, methods for using such compounds for inhibiting glycine transporters and methods for using such compounds for the treatment of disease states in which glycine is involved.
    Type: Grant
    Filed: September 13, 2001
    Date of Patent: September 20, 2005
    Assignee: Merck & Co., Inc.
    Inventors: Syed M. Ali, Kurt R. Brunden, Jack B. Jiang
  • Publication number: 20040176443
    Abstract: Disclosed are diaryl piperazines and related compounds. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.
    Type: Application
    Filed: March 12, 2004
    Publication date: September 9, 2004
    Applicant: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Alan Hutchison, Robert W. DeSimone, Kevin J. Hodgetts, James E. Krause, Geoffrey G. White
  • Publication number: 20040152740
    Abstract: The present invention relates to compounds of Formula 1: 1
    Type: Application
    Filed: September 8, 2003
    Publication date: August 5, 2004
    Applicant: NPS Allelix Corporation
    Inventors: Methvin Isaac, Tao Xin, Tomislav Stefanac, Anne O'Brien, Kathleen Da Silva-Turcot, Jalaj Arora, Shawn Maddaford, Abdelmalik Slassi
  • Publication number: 20040138205
    Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I 1
    Type: Application
    Filed: November 18, 2003
    Publication date: July 15, 2004
    Inventors: Dawei Chen, Milind Deshpande, Andrew Thurkauf, Avinash Phadke, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
  • Patent number: 6743790
    Abstract: The present invention relates to compounds of the formula I, in which R1, R2, R3, R4, R5, R6, A, X, m and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, for example as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
    Type: Grant
    Filed: June 6, 2001
    Date of Patent: June 1, 2004
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Otmar Klingler, Manfred Schudok, Hans-Peter Nestler, Hans Matter, Herman Schreuder
  • Publication number: 20040059111
    Abstract: A novel fluorescent group-containing carbodiimide compound having at least one group selected from a carboxyl group, a sulfo group, a phosphono group and a phospho group which have substitution of an alkali metal, an alkaline earth metal or a basic group containing a nitrogen or phosphorus atom, which is prepared by using a novel fluorescent group-containing carbodiimide compound precursor having a halogen atom or a sulfonic acid group; and a method for detecting a nucleic acid by hybridization utilizing a nucleic acid labeled with a labeling substance, which utilizes the fluorescent group-containing carbodiimide compound as the labeling substance.
    Type: Application
    Filed: September 2, 2003
    Publication date: March 25, 2004
    Inventors: Naoki Kimura, Namiko Shiohata, Yoko Yoshikawa
  • Publication number: 20040029913
    Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.
    Type: Application
    Filed: February 24, 2003
    Publication date: February 12, 2004
    Inventors: James T. Dalton, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka
  • Publication number: 20030207864
    Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
    Type: Application
    Filed: March 11, 2003
    Publication date: November 6, 2003
    Applicant: Tulark Inc.
    Inventor: Jonathan B. Houze
  • Publication number: 20030158226
    Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.
    Type: Application
    Filed: September 17, 2002
    Publication date: August 21, 2003
    Applicant: Roche Bioscience, a division of Syntex (U.S.A.) LLC
    Inventors: Paula Nanette Belloni, Denis John Kertesz, Michael Klaus, Jean-Marc Lapierre
  • Publication number: 20030119876
    Abstract: The invention relates to new diphenylurea having the formula (I) 1
    Type: Application
    Filed: February 26, 2002
    Publication date: June 26, 2003
    Inventors: Andrea Aschenbrenner, Katharina Aulinger Fuchs, Matthias Dormeyer, Gabriel Garcia, Bernd Kramer, Jurgen Kraus, Rolf Krauss, Johan Leban, Stefano Pegoraro, Wael Saeb, Kristina Wolf
  • Patent number: 6534546
    Abstract: Compounds represented by the general formula (1):   (where R1 is SR6 or NR7R8, where R6 is typically an alkyl group having 1-6 carbon atoms, R7 is a hydrogen atom, an alkyl group having 1-6 carbon atoms or a nitro group, and R8 is a hydrogen atom or an alkyl group having 1-6 carbon atoms; R2 and R3 are each typically a hydrogen atom or an alkyl group having 1-6 carbon atoms; R4 is a hydrogen atom, an alkyl group having 1-6 carbon atoms or an amidino group of which the amine portion may be substituted by an alkyl or nitro group; R5 is a hydrogen atom or an alkyl group having 1-6 carbon atoms; Y1, Y2, Y3 and Y4 which may be the same or different are each typically a hydrogen atom, a halogen atom or an alkoxy group having 1-6 carbon atoms; n and m are each an integer of 0 or 1), or possible stereoisomers or optically active forms of the compounds or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 6, 1997
    Date of Patent: March 18, 2003
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Toshio Honda, Toshihiko Makino, Toshiaki Nagafuji, Yasushi Kitoh, Nobuaki Kimura
  • Publication number: 20030050298
    Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Application
    Filed: September 5, 2002
    Publication date: March 13, 2003
    Inventors: Michael R Palovich, Katherine L Widdowson, Hong Nie
  • Patent number: 6391917
    Abstract: Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the determination of calcitonin receptor activity.
    Type: Grant
    Filed: April 19, 2001
    Date of Patent: May 21, 2002
    Assignee: ZymoGenetics, Inc.
    Inventors: Charles R. Petrie, Patricia A. McKernan, Emma E. Moore, John M. Ostresh, Jean-Philippe Meyer, Richard A. Houghten, Clemencia Pinilla
  • Patent number: 6380422
    Abstract: Compounds of the formula I and disulfides thereof and salts thereof are important intermediate products for the preparation of compounds having a microbicidal and plant-immunizing action, of the formula III In the compounds of the formulae I and III: X is halogen, n is 0, 1, 2 or 3; Z is CN, CO—A or CS—A, A is hydrogen, halogen, OR1, SR2 and N(R3)R4; R1 to R4 are hydrogen, a substituted or unsubstituted, open-chain, saturated or unsaturated hydrocarbon radical containing not more than 8 carbon atoms, a substituted or unsubstituted cyclic, saturated or unsaturated hydrocarbon radical containing not more than 10 carbon atoms, substituted or unsubstituted benzyl or phenethyl, a substituted or unsubstituted alkanoyl group containing not more than 8 carbon atoms, a substituted or unsubstituted benzoyl group or a substituted or unsubstituted heterocyclyl radical; or R3 and R4, together with the nitrogen atom to which they are bonded, are a 5- or 6-membered, subs
    Type: Grant
    Filed: February 26, 1999
    Date of Patent: April 30, 2002
    Assignee: Syngenta Investment Corportion
    Inventors: Walter Kunz, Beat Jau