Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/324.5)
  • Patent number: 8946282
    Abstract: A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer.
    Type: Grant
    Filed: April 3, 2013
    Date of Patent: February 3, 2015
    Assignee: Annji Pharmaceutical Co., Ltd.
    Inventors: Ji-Wang Chern, Ajit Dhananjay Jagtap, Hsiao-Chun Wang, Grace Shiahuy Chen
  • Publication number: 20140315079
    Abstract: A method for preparing an imidazole compound with the following formula: wherein Rf is a fluorinated alkyl group comprising between 1 and 5 carbon atoms, said method including: (a) the reaction of the diaminomaleonitrile with the following formula: with the compound with the following formula: wherein Y represents a chlorine atom or the OCORf group to form the salified amide compound with the following formula: at temperature T1, and (b) the dehydration of the salified amide compound with formula (IVa) and/or the corresponding amino (IVb) to form the imidazole compound with formula (III), at temperature T2 higher than T1.
    Type: Application
    Filed: October 29, 2012
    Publication date: October 23, 2014
    Inventors: Gregory Schmidt, Miguel Flasque
  • Patent number: 8828268
    Abstract: The present invention pertains to the field of thermosetting or thermoset polymers mainly used as materials, coatings or adhesives. The invention more specifically relates to the use of specific molecules having associative groups including a nitrogen heterocycle as a hardener or co-hardener of thermosetting polymers.
    Type: Grant
    Filed: June 3, 2013
    Date of Patent: September 9, 2014
    Assignee: Arkema France
    Inventors: Bruno Van Hemelryck, Manuel Hidalgo
  • Patent number: 8822701
    Abstract: The present invention relates to a method for preparing 1-(2-aminoethyl)imidazolidin-2-one or the thiocarbonyl thereof, and also to the product that can be obtained according to this method, and which has a purity of at least 98%, and to the uses thereof.
    Type: Grant
    Filed: July 17, 2013
    Date of Patent: September 2, 2014
    Assignee: Arkema France
    Inventors: Alain Baloche, Jean-Paul Gamet, Jean-Philippe Gillet
  • Patent number: 8637562
    Abstract: The invention relates to methods for detecting the presence of a compound of formula I in a biological test sample: where R2, R3, and R4 are as defined in the specification; or a salt thereof.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: January 28, 2014
    Assignee: Theravance, Inc.
    Inventors: Yuqin Dai, Donavon McConn, Huiyu Zhou
  • Publication number: 20130303784
    Abstract: The present invention relates to a method for preparing 1-(2-aminoethyl)imidazolidin-2-one or the thiocarbonyl thereof, and also to the product that can be obtained according to this method, and which has a purity of at least 98%, and to the uses thereof.
    Type: Application
    Filed: July 17, 2013
    Publication date: November 14, 2013
    Inventors: Alain Baloche, Jean-Paul Gamet, Jean-Philippe Gillet
  • Patent number: 8530671
    Abstract: The present invention relates to a method of preparing a material formed from arborescent-branched molecules comprising associative groups that includes the following successive steps: (a) the reaction of at least one at least trifunctional compound (A) bearing first and second functional groups with at least one bifunctional compound (B), the functional groups of which are capable of reacting with the first functional groups of the compound (A); and (b) the reaction of the compound(s) obtained in step (a) with at least one compound (C) bearing, on the one hand, at least one reactive group capable of reacting with the second functional groups of (A) and, on the other hand, at least one given associative group.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: September 10, 2013
    Assignees: Arkema France, Centre National de la Recherche Scientifique CNRS
    Inventors: François-Genes Tournilhac, Manuel Hidalgo, Ludwik Leibler
  • Patent number: 8513435
    Abstract: The present invention relates to a method for preparing 1-(2-aminoethyl)imidazolidin-2-one or the thiocarbonyl thereof, and also to the product that can be obtained according to this method, and which has a purity of at least 98%, and to the uses thereof.
    Type: Grant
    Filed: January 7, 2011
    Date of Patent: August 20, 2013
    Assignee: Arkema France
    Inventors: Alain Baloche, Jean-Paul Gamet, Jean-Philippe Gillet
  • Patent number: 8372848
    Abstract: This invention relates generally to N-benzylamino cyclic thioureas, pharmaceutical compositions containing them, and their use as antagonists of melanin-concentrating hormone receptor (MCH receptor).
    Type: Grant
    Filed: March 23, 2005
    Date of Patent: February 12, 2013
    Assignees: Mixture Sciences, Inc., The Regents of the University of California
    Inventors: Richard A. Houghten, Colette Dooley, Adel Nefzi, Zhiwei Wang, Oliver Civelli, Hiroshi Nagasaki
  • Patent number: 8362061
    Abstract: The invention relates to methods for detecting the presence of a compound of formula I in a biological test sample: where R2, R3, and R4 are as defined in the specification; or a salt thereof.
    Type: Grant
    Filed: June 27, 2012
    Date of Patent: January 29, 2013
    Assignee: Theravance, Inc.
    Inventors: Yuqin Dai, Donavon McConn, Huiyu Zhou
  • Publication number: 20130023667
    Abstract: The present invention relates to a method for preparing 1-(2-aminoethyl)imidazolidin-2-one or the thiocarbonyl thereof, and also to the product that can be obtained according to this method, and which has a purity of at least 98%, and to the uses thereof.
    Type: Application
    Filed: January 7, 2011
    Publication date: January 24, 2013
    Applicant: Arkema France
    Inventors: Alain Baloche, Jean-Paul Gamet, Jean-Philippe Gillet
  • Publication number: 20120252699
    Abstract: The present invention relates to novel fluorophores and their use in combination with novel nucleic acid molecules, called aptamers, that bind specifically to the fluorophore and thereby enhance the fluorescence signal of the fluorophore upon exposure to radiation of suitable wavelength. Molecular complexes formed between the novel fluorophores, novel nucleic acid molecules, and their target molecules are described, and the use of multivalent aptamer constructs as fluorescent sensors for target molecules of interest are also described.
    Type: Application
    Filed: February 18, 2010
    Publication date: October 4, 2012
    Applicant: CORNELL UNIVERSITY
    Inventors: Samie R. Jaffrey, Jeremy S. Paige
  • Publication number: 20120209008
    Abstract: The invention provides processes for preparing intermediates useful for preparing compounds of the formula: or a salt thereof, where R1-3 are as defined in the specification.
    Type: Application
    Filed: April 25, 2012
    Publication date: August 16, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Weijiang Zhang, Pierre-Jean Colson
  • Patent number: 8232306
    Abstract: The invention relates to methods for detecting the presence of a compound of formula I in a biological test sample: where R2, R3, and R4 are as defined in the specification; or a salt thereof.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: July 31, 2012
    Assignee: Theravance, Inc.
    Inventors: Yuqin Dai, Donavon McConn, Huiyu Zhou
  • Patent number: 8202895
    Abstract: The present application relates to new, substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: March 18, 2010
    Date of Patent: June 19, 2012
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Ulf Brüggemeier, Chantal Fürstner, Volker Geiβ, Joerg Keldenich, Armin Kern, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
  • Publication number: 20120074353
    Abstract: The present invention pertains to the field of thermosetting or thermoset polymers mainly used as materials, coatings, or adhesives. The invention more specifically relates to the use of specific molecules having associative groups including a nitrogen heterocycle as a hardener or co-hardener of thermosetting polymers.
    Type: Application
    Filed: June 4, 2010
    Publication date: March 29, 2012
    Applicant: Arkema France
    Inventors: Bruno Van Hemelryck, Manuel Hidalgo
  • Patent number: 7994204
    Abstract: The present invention aims to provide compounds which have an inhibitory effect on the binding between S1P and its receptor Edg-1(S1P1) and which are useful for pharmaceutical purposes. A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: [wherein Ar represents a monocyclic heterocyclic ring containing one or two nitrogen atoms, A represents an oxygen atom or the like, Y1, Y2 and Y3 each represent a carbon atom or a nitrogen atom, R1 represents a hydrogen atom, a C1-C6 alkyl group or the like, R2 represents a C1-C6 alkyl group, a C3-C8 cycloalkyl group or the like, R3 represents a C1-C18 alkyl group or the like, R4 represents a hydrogen atom or a C1-C6 alkyl group, and R5 represents a C1-C10 alkyl group or the like].
    Type: Grant
    Filed: February 6, 2007
    Date of Patent: August 9, 2011
    Assignee: Taisho Pharmaceutical Co., Ltd
    Inventors: Naoya Ono, Tetsuo Takayama, Fumiyasu Shiozawa, Hironori Katakai, Tetsuya Yabuuchi, Tomomi Ota, Takeshi Koami, Rie Nishikawa
  • Publication number: 20100305334
    Abstract: The present invention relates to a method of preparing a material formed from arborescent-branched molecules comprising associative groups that includes the following successive steps: (a) the reaction of at least one at least trifunctional compound (A) bearing first and second functional groups with at least one bifunctional compound (B), the functional groups of which are capable of, reacting with the first functional groups of the compound (A); and (b) the reaction of the compound(s) obtained in step (a) with at least one compound (C) bearing, on the one hand, at least one reactive group capable of reacting with the second functional groups of (A) and; on the other hand, at least one given associative group
    Type: Application
    Filed: December 19, 2008
    Publication date: December 2, 2010
    Applicant: Arkema France
    Inventor: Francois-Genes Tournilhac
  • Publication number: 20100286219
    Abstract: A method comprising utilizing a compound of formula I: where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkylaryl, alkyloxy, hydroxy, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies hydrogen, alkyl or alkylaryl group; X signifies CH2, oxygen atom or sulphur atom; n is 1, 2 or 3, with the proviso that when n is 1, X is not CH2; and the individual (R)- and (S)-enantiomers or mixtures of enantiomers and pharmaceutically acceptable salts thereof; wherein the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; the term halogen means fluorine, chlorine, bromine or iodine, in the manufacture of a medicament for the treatment of one or more of the following indications: congestive heart failure, angina
    Type: Application
    Filed: January 10, 2008
    Publication date: November 11, 2010
    Applicant: BIAL - PORTELA & CA S.A.
    Inventor: Patricio Manuel Vieira Araújo Soares Da Silva
  • Publication number: 20090149425
    Abstract: The present invention provides a malononitrile compound represented by the formula (I): wherein any one of X1, X2, X3 and X4 is CR100, wherein R100 is a group represented by the formula: the other three of X1, X2, X3 and X4 each represent nitrogen or CR5, provided that 1 to 3 of X1, X2, X3 and X4 represent nitrogen, and Z represents oxygen, sulfur or NR6, which has pest-controlling activity.
    Type: Application
    Filed: January 13, 2005
    Publication date: June 11, 2009
    Inventors: Hiromasa Mitsudera, Ken Otaka, Jun Fujiwara
  • Patent number: 7528200
    Abstract: An epoxy-hardener system is provided having relatively long latency periods combined with relatively short cure times at low cure temperatures. The hardeners of the present invention are ureidoamines and their derivatives, which are chelates of ureido compounds and amines. The ureidoamines are prepared by reacting an amine with the ureido compound and aqueous formaldehyde without a catalyst. Complexes of ureidoamine hardeners with various blocking agents are prepared in the melt. The hardener is prevented from curing the epoxy by the reaction between the hardener and the blocking agent. The blocked hardener is then blended with the epoxy, usually by warming the mixture briefly at about 50-60 degrees C.
    Type: Grant
    Filed: February 1, 2006
    Date of Patent: May 5, 2009
    Assignee: ARDES Enterprises, Inc.
    Inventor: Richard D. Schile
  • Patent number: 7488830
    Abstract: A polymer that includes at least one monomeric unit having a pendant substituent group according to formula (II): wherein: R1 is H, chloro, bromo, alkyl, hydroxyalkyl, aryl, or aralkyl, R2 and R3 are each independently H, alkyl, hydroxyalkyl, aryl, aralkyl, uriedo, or carboxyalkylene, R4 is alkylene or R5, R7, and R10 are each independently alkylene, R6, R8, and R9 are each independently H or alkyl, A is O or N—R11, provided if A is O and R4 is methylene, then R1 cannot be H, chloro, or bromo, R11 is H or alkyl, and X? is an anion, is useful in personal care application, such as hair styling compositions.
    Type: Grant
    Filed: July 26, 2006
    Date of Patent: February 10, 2009
    Assignee: Rhodia Inc.
    Inventors: Krishnamurthy Shanmuganandamurthy, Euen Gunn, Stewart Alexander Warburton
  • Patent number: 7439242
    Abstract: Modulators of PPAR? activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.
    Type: Grant
    Filed: April 15, 2002
    Date of Patent: October 21, 2008
    Assignee: Amgen Inc.
    Inventors: Jonathan B. Houze, Lawrence R. McGee, Steven Marc Rubenstein
  • Publication number: 20080255218
    Abstract: This invention relates generally to N-benzylamino cyclic thioureas, pharmaceutical compositions containing them, and their use as antagonists of melanin-concentrating hormone receptor (MCH receptor).
    Type: Application
    Filed: March 23, 2005
    Publication date: October 16, 2008
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Richard A. Houghten, Colette Dooley, Adel Nefzi, Zhiwei Wang, Oliver Civelli, Hiroshi Nagasaki
  • Publication number: 20080221169
    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: October 26, 2007
    Publication date: September 11, 2008
    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: 20080176919
    Abstract: This invention relates to benzonitrile derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R1 to R3 are defined in the description, to their use in medicine, and to compositions containing them. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof.
    Type: Application
    Filed: December 23, 2005
    Publication date: July 24, 2008
    Inventors: Lyn Howard Jones, Sandra Dora Newman, Nigel Alan Swain
  • Patent number: 7390829
    Abstract: A compound is disclosed herein comprising or a pharmaceutically acceptable salt or a prodrug thereof; wherein R is OH or NH2. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: June 29, 2005
    Date of Patent: June 24, 2008
    Assignee: Allergan, Inc.
    Inventors: Ken Chow, Todd M. Heidelbaugh, Phong X. Nguyen
  • Patent number: 7265135
    Abstract: The invention relates to novel 2-Oxy, 2-Amino, and 2-Thio-imidazole compounds of formula (I): wherein all variables are as herein defined, pharmaceutical compositions containing the compounds and methods of using them in the treatment of neurological disorders and other disorders and conditions mediated by the histamine H3 receptor.
    Type: Grant
    Filed: January 14, 2004
    Date of Patent: September 4, 2007
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Michael Bogenstaetter, Nicholas I. Carruthers, Jill A. Jablonowski, Timothy W. Lovenberg, Kiev S. Ly
  • Patent number: 7125904
    Abstract: Compounds of formula I: where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkylaryl, alkyloxy, hydroxy, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies hydrogen, alkyl or alkylaryl group; X is CH2, O or S, and n is 1, 2 or 3, with the proviso that if X is CH2, n is not 1, and a method for their preparation. The compounds have potentially valuable pharmaceutical properties for the treatment of cardiovascular disorders such as hypertension and chronic heart failure.
    Type: Grant
    Filed: October 8, 2003
    Date of Patent: October 24, 2006
    Assignee: Portela & C.A., S.A.
    Inventors: David Alexander Learmonth, Patricio Manuel Viera Araújo Soares da Silva, Alexander Beliaev
  • Patent number: 7045532
    Abstract: ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include compounds of formula (I): Z-???(I) Wherein Z is a zinc coordinating moiety and ? is an amino-acid mimicking moiety, and pharmaceutically acceptabale salts thereof. Methods of using the inhibitors and pharmaceutical compositions containing the inhibitors to treat a body weight disorder, to decrease appetite, to increase muscle mass, to decrease body fat, to treat diabetes and to treat a state associated with altered lipid metabolism, are also described.
    Type: Grant
    Filed: October 31, 2001
    Date of Patent: May 16, 2006
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Susan L. Acton, Timothy D. Ocain, Alexandra E. Gould, Natalie A. Dales, Bing Guan, James A. Brown, Michael Patane, Vivek J. Kadambi, Michael Solomon, Alain Stricker-Krongrad
  • Patent number: 6884815
    Abstract: This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors. Preferred compounds of the invention possess some or all of the following properties in that they are: 1) multi-aryl in structure, 2) heteroaryl in structure, 3) a pharmaceutically acceptable oral dose can provide a detectable in vitro effect, 4) comprise fewer than four or preferably no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar or sub-nanomolar concentrations. This invention also relates to pharmaceutical compositions comprising such compounds and the use of such compounds in treating a variety of inflammatory and immune system disorders. Additionally, this invention relates to the use such compounds as probes for the localization of C5a receptors.
    Type: Grant
    Filed: June 12, 2003
    Date of Patent: April 26, 2005
    Assignee: Neurogen Corporation
    Inventors: Andrew Thurkauf, Xiao-shu He, He Zhao, John Peterson, Xiaoyan Zhang, Robbin Brodbeck, James Krause, George Maynard, Alan Hutchison
  • Patent number: 6627758
    Abstract: Compositions and methods are described for hydrating terminal alkynes catalytically in anti-Markovnikov fashion. The compositions comprise a transition metal complex including at least one organic ligand having at least two heteroatoms, wherein the heteroatoms are directly bonded or located one atom away. Preferably, at least one of the heteroatoms is nitrogen, which is typically provided as part of a heterocyclic ring. Other preferred heteroatoms include S, P, N, As or Se. A particularly preferred catalyst employs a P-linked imidazole ligand bound to Ru. Such complexes have a controlled adaptable proton transfer ability and/or a hydrogen bonding ability making them particularly useful as chemical reaction facilitators.
    Type: Grant
    Filed: February 16, 2001
    Date of Patent: September 30, 2003
    Assignee: San Diego State University Foundation
    Inventor: Douglas Bryan Grotjahn
  • Patent number: 6362183
    Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: March 26, 2002
    Assignee: G. D. Searle & Company
    Inventors: John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
  • Patent number: 6288151
    Abstract: Novel alkyl aminoalkyl cyclic urea compounds of the structural formula: wherein each of m, n, and o are independently 1 or 2, p is 0 or 1, R1 is C1 to C4 linear or branched alkyl, R2 is C4 to C10 linear or branched alkyl, or, alternately, CHR1R2 forms a C6 to C12 substituted or unsubstituted cycloalkyl. These novel alkylated aminoalkyl cyclic ureas are useful as surfactants for reducing equilibrium and dynamic surface tension in water-based formulations, particularly coating, ink, and agricultural formulations.
    Type: Grant
    Filed: October 14, 1999
    Date of Patent: September 11, 2001
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Kevin Rodney Lassila, Kristen Elaine Minnich, Richard Van Court Carr
  • Patent number: 6229011
    Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.
    Type: Grant
    Filed: August 21, 1998
    Date of Patent: May 8, 2001
    Assignee: Hoffman-La Roche Inc.
    Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achyutharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull