The Nitrogen Is Multiply Bonded To Carbon Patents (Class 548/336.1)
  • Patent number: 10689478
    Abstract: Provided is an amidate compound represented by the formula (1): wherein A is a substituted or unsubstituted hydrocarbon group, n is an integer of 1 or more, and D is a nitrogen-containing organic group represented by the formula (2): wherein R1, R2, and R3 are the same or different, and are each a hydrocarbon group that may contain a heteroatom; some or all of R1, R2, and R3 may be bonded together to form a ring structure; X is a nitrogen atom, an oxygen atom, or a sulfur atom; and a is 0 or 1, wherein a is 1 when X is a nitrogen atom, and a is 0 when X is an oxygen atom or a sulfur atom.
    Type: Grant
    Filed: August 3, 2017
    Date of Patent: June 23, 2020
    Assignee: KOEI CHEMICAL COMPANY, LIMITED
    Inventors: Motoyoshi Miyagi, Shingo Nitta, Hitomi Tsuboi, Shogo Takahashi
  • Publication number: 20150126746
    Abstract: A method for obtaining salts of bicyclic imidazole compounds (V) having general structural formulae in which A represents a monovalent cation, X represents independently a carbon atom, an oxygen atom, a sulphur atom or a nitrogen atom. Also, the associated production method and to the use thereof, in particular as an electrolyte component for batteries.
    Type: Application
    Filed: April 26, 2013
    Publication date: May 7, 2015
    Inventor: Grégory Schmidt
  • Publication number: 20140357673
    Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds.
    Type: Application
    Filed: July 31, 2014
    Publication date: December 4, 2014
    Inventors: Nicholas J. Donato, Christiane Wobus, Hollis D. Showalter, Moshe Talpaz, Jeffrey William Perry, Roderick Joseph Sorenson, Mary Xuan Dziem O'Riordan, Yafei Jin
  • Publication number: 20140275569
    Abstract: The present application provides methods for decarboxylation of amino acids via imine formation with a catalyst under superheated conditions in either a microwave or oil bath.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Inventors: Richard W. Morrison, Douglas Michael Jackson
  • Patent number: 8785654
    Abstract: A method for producing N-(2-amino-1,2-dicyanovinyl)imidates represented by the following formula (1-III) under low temperature conditions within a short period of time in high yield is provided. In addition, a method for producing N-(2-amino-1,2-dicyanovinyl)formamidine represented by the following formula (2-II) which is suitably applicable to a cyclization reaction for producing AlCN, AlCA or the like and which enhances yield of the cyclization reaction is provided. In addition, a method for producing aminoimidazole derivatives represented by the following formula (3-V) in high yield by using diaminomaleonitrile as a starting material is provided.
    Type: Grant
    Filed: January 31, 2012
    Date of Patent: July 22, 2014
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Mitsuru Takase, Fuminori Komatsu
  • Patent number: 8623942
    Abstract: The present invention provides a liquid curable epoxy resin composition that has excellent storage stability and curing properties and provides a cured product having excellent properties, particularly, excellent organic solvent resistance. For that purpose, a clathrate containing a carboxylic acid compound and at least one selected from the group consisting of an imidazole compound represented by formula (I), wherein R1 to R4 each represent a hydrogen atom or the like, and 1,8-diazabicyclo[5.4.0]undecene-7 (DBU) is mixed in an epoxy resin. The liquid curable epoxy resin composition uses a liquid epoxy resin or an organic solvent.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: January 7, 2014
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Masami Kaneko, Kazuo Ono, Natsuki Amanokura, Naoyuki Kamegaya
  • Patent number: 8518999
    Abstract: The present invention provides compounds which are modulators of TNF-? signaling and methods of use thereof for treating a patient having a TNF-? mediated condition.
    Type: Grant
    Filed: December 1, 2005
    Date of Patent: August 27, 2013
    Assignee: Genzyme Corporation
    Inventors: Scott F. Sneddon, John L. Kane, Bradford H. Hirth, Fred Vinick, Shuang Qiao, Sharon R. Nahill, John M. Williams, Hans-Peter Biemann
  • Publication number: 20130203895
    Abstract: The present invention relates to curatives for epoxy resins, and compositions (e.g. adhesives) containing such resins cured using the same, methods of preparation and uses therefor. More specifically, the present invention relates to hybrid curatives for epoxy resins comprising both aromatic amine, phenol and/or phenyl ester moieties. A further aspect of the current invention relates to new imidazole catalysts that posses a combination of excellent cure latency as well as low cure temperature onset.
    Type: Application
    Filed: March 15, 2013
    Publication date: August 8, 2013
    Applicant: DESIGNER MOLECULES, INC.
    Inventor: Designer Molecules, Inc.
  • Publication number: 20130123287
    Abstract: Providing a novel control agent for soft rot and a novel control method for the same. A compound having no antibacterial activity against Erwinia carotovora but having a control activity against fungi on soil surface, specifically containing, as the active ingredient, a fungicide comprising any of a strobilurin compound such as azoxystrobin and kresoxim-methyl, an azole compound such as triflumizol, cyazofamid, amisulbrom, and thiophanate-methyl, a carboxamide compound such as penthiopyrad and boscalid, a sulfonamide compound such as flusulfamide, an organic chlorine compound such as chlorothalonil, a dicarboximide compound such as pro-cymidone and iprodione, a phenylpyrrole compound such as fludioxonil, an anilinopyrimidine compound such as mepanipyrim, and a guanidine compound such as iminoctadine is the control agent for plant soft rot, which is applied to plant cultivation soil.
    Type: Application
    Filed: July 21, 2011
    Publication date: May 16, 2013
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Koji Sugimoto, Hiroyuki Hayashi
  • Patent number: 8383829
    Abstract: An electrochromic compound represented by Formula (1), wherein R1 is an alkyl group, an alkenyl group, an aryl group, or a heterocyclic group; R2 and R3 are each a hydrogen atom or a substituent; X is N—R4, an oxygen atom, or a sulfur atom; and R4 is a hydrogen atom or a substituent; provided that at least one of R1-R4 has a partial structure represented by Formula (2), —Si(Y)nR?(3-n)??Formula (2) wherein Y is a halogen atom or OR, R is an alkyl group, or an aryl group; R? is an alkyl group, an alkenyl group, an aryl group, or a heterocyclic group, and n is an integer of 1-3.
    Type: Grant
    Filed: April 7, 2009
    Date of Patent: February 26, 2013
    Assignee: Konica Minolta Holdings, Inc.
    Inventors: Kaori Ono, Osamu Ishige, Takeshi Hakii, Akihito Hisamitsu
  • Publication number: 20120108820
    Abstract: Novel chemical compounds of the general formula K+A? useful as industrial solvents, especially as ligands, for efficient catalyst recycling.
    Type: Application
    Filed: December 16, 2011
    Publication date: May 3, 2012
    Inventors: Paul Dyson, Dongbin Zhao, Zhaofu Fei
  • Publication number: 20120077806
    Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds.
    Type: Application
    Filed: September 23, 2011
    Publication date: March 29, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Nicholas J. Donato, Christiane Wobus, Hollis D. Showalter, Moshe Talpaz, Jeffrey W. Perry, Roderick J. Sorenson, Mary X. O'Riordan, Yafei Jin
  • Patent number: 8093267
    Abstract: Imidazole-based compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed.
    Type: Grant
    Filed: December 1, 2009
    Date of Patent: January 10, 2012
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: David J. Augeri, Jeffrey Bagdanoff, Lakmal W. Boteju, Kenneth G. Carson, Theodore C. Jessop, Spencer David Kimball
  • Publication number: 20110274907
    Abstract: Curative fibre components comprise one or more fibres for filaments of curative suitable to cure curable resins such as thermoset resin. In curative fibre components comprising a plurality of fibres of curative, the fibres can be commingled, such as twisting, to form a thread or yarn. Curative fibre components can be used to form a material in the form of a sheet, fabric, layer, textile or mat of woven or non-woven curative fibres. Curative fibre components can be used to produce composite materials such as fibre reinforced resinous composite materials. The curative fibre components can be commingled, including interwoven, stitched and layered with other fibres or fibrous materials, such as fibrous reinforcement, fibrous curable resin, fibrous thermoplastic, other non-reinforcing fibres to form composite materials, prepregs, preforms and articles.
    Type: Application
    Filed: November 24, 2009
    Publication date: November 10, 2011
    Inventors: Mark Raymond Steele, Andrew Gibbs, Amy Grace Atinkson
  • Publication number: 20110251200
    Abstract: The invention provides to a family of aryl guanidine-based F1F0-ATPase inhibitors, e.g., mitochondrial F1F0-ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.
    Type: Application
    Filed: September 11, 2009
    Publication date: October 13, 2011
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Gary D. Glick, Peter Toogood, Gina Ney
  • Publication number: 20110230428
    Abstract: Certain chemical entities are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
    Type: Application
    Filed: July 22, 2009
    Publication date: September 22, 2011
    Inventors: John Wityak, Leticia M. Toledo-sherman, Celia Dominguez, Stephen Martin Courtney, Christopher John Yarnold, Paula C. De Aguiar Pena, Andreas Scheel, Dirk Winkler
  • Patent number: 8022072
    Abstract: An azolylmethylidenehydrazine derivative represented by the formula (I) wherein Ar is an aryl group optionally having substituent(s) or a heteroaryl group optionally having substituent(s), R1 and R2 are the same or different and each is an alkyl group, a cycloalkyl group, an aralkyl group optionally having substituent(s), an aryl group optionally having substituent(s), a heteroarylalkyl group optionally having substituent(s), or R1 and R2 are bonded to each other to form a nitrogen-containing heterocyclic group optionally having substituent(s), and X is CH or a nitrogen atom, or a pharmacologically acceptable salt thereof is useful as a medicament, particularly as an antifungal agent, or an anti-inflammatory agent or an antiallergic agent.
    Type: Grant
    Filed: June 17, 2008
    Date of Patent: September 20, 2011
    Assignee: Kaken Pharmaceutical Co., Ltd.
    Inventors: Hironobu Ogura, Yoshiyuki Tatsumi, Yuji Fukamizu
  • Publication number: 20110224252
    Abstract: The present invention relates to novel imidazole derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R1 is halogen, C1-C4alkyl or C1-C4haloalkyl; R2 is an optionally substituted aryl or heteroaryl; R3 is halogen; R4 is hydrogen, halogen, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy or cyano; R5 is halogen; X is N or C(R); and R is hydrogen, halogen, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy or cyano; or an agrochemically usable salt form thereof; provided that when X is C(R), R2 cannot be an optionally substituted aryl.
    Type: Application
    Filed: October 24, 2008
    Publication date: September 15, 2011
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Raphael Dumeunier, Clemens Lamberth, Stephan Trah, Sebastian Wendeborn
  • Publication number: 20110152175
    Abstract: The invention provides dendrimeric compounds of the formula 1 comprising amino acids, wherein n is an integer of 1-4, T is an alkylidene —(CH2)2CONH(CH2)2- group, R2 is an —NH2 group or a moiety of a primary organic amine, and P is an amino acid and/or peptide moiety, wherein at least one hydrogen atom of at least one amino group is optionally replaced by a protective group, and a hyperbranched core compound of the formula 3, wherein T and R2 are as defined above. The invention provides also a process for the preparation of a dendrimeric compound and a hyperbranched core, wherein the process employs addition reactions of alkyl acrylate and a basic amino acid, and use of a hyperbranched core for the preparation of a dendrimeric compound comprising amino acids. The invention provides also use of dendrimeric compounds for the preparation of the medicament for inhibiting growth of bacterial cells, fungi and tumor cells.
    Type: Application
    Filed: September 18, 2009
    Publication date: June 23, 2011
    Applicant: Instytut Chemii Organicznej Polska Akademia Nauk
    Inventors: Zofia Lipkowska, Piotr Polcyn, Andrzej Wojciech Lipkowski
  • Publication number: 20110092557
    Abstract: The present invention provides compounds comprising amino acid R groups, compositions comprising the same, and methods of inhibiting neuraminidase and/or treating influenza, Pseudomonas aeruginosa, or Bacteroides fragilis infection in a mammal.
    Type: Application
    Filed: June 24, 2009
    Publication date: April 21, 2011
    Applicant: INFLUMEDIX INC.
    Inventors: Xiaodong Fan, Lidia Cristian
  • Publication number: 20110077409
    Abstract: Cyano-substituted sulfilimines are produced efficiently and in high yield from the corresponding sulfides by reaction with cyanamide and hypochlorite.
    Type: Application
    Filed: November 18, 2010
    Publication date: March 31, 2011
    Inventors: David E. Podhorez, Ronald Ross, JR., James R. McConnell
  • Publication number: 20110071303
    Abstract: Methods of preparing imidazole-based compounds are disclosed.
    Type: Application
    Filed: September 20, 2010
    Publication date: March 24, 2011
    Inventors: Wenxue Wu, Jie Yan, Haiming Zhang
  • Patent number: 7897633
    Abstract: The present invention relates to novel inhibitors of glutaminyl cyclase and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Chorea Huntington, pathogenic psychotic conditions, schizophrenia, impaired food intake, sleep-wakefulness, impaired homeostatic regulation of energy metabolism, impaired autonomic function, impaired hormonal balance, impaired regulation, body fluids, hypertension, fever, sleep dysregulation, anorexia, anxiety related disorders including depression, seizures including epilepsy, drug withdrawal and alcoholism, neurodegenerative disorders including cognitive dysfunction and dementia.
    Type: Grant
    Filed: October 24, 2007
    Date of Patent: March 1, 2011
    Assignee: Probiodrug AG
    Inventors: Stephan Schilling, Mirko Buchholz, Andre Niestroj, Ulrich Heiser, Hans-Ulrich Demuth
  • Publication number: 20100324273
    Abstract: The present application relates to compounds of formulae I and II: in which, X1, X2, R1, R2, R6, R7, R8, L1, L2, L3, T1, T2, Z1, Z2 are chosen from various possible groups or entities. For example, the compounds of formulae I and II are used as ligands for preparing complexes of various metals.
    Type: Application
    Filed: August 30, 2010
    Publication date: December 23, 2010
    Applicant: Saint Mary's University
    Inventors: Robert D. Singer, Prashant Upendra Naik
  • Publication number: 20100304966
    Abstract: Compounds of the formula I in which the substituents have the meaning given in the description, processes for preparing these compounds, compositions comprising them and their use for controlling harmful fungi.
    Type: Application
    Filed: October 9, 2008
    Publication date: December 2, 2010
    Applicant: BASF SE
    Inventors: Joachim Rheinheimer, Barbara Nave, Doris Kremzow, Stefan Redlich, Christian Pilger, Claudia Rosenbaum, Wassilios Grammenos
  • Publication number: 20100292229
    Abstract: The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. In general aspects, compounds of the present invention are tyrphostin-like in structure. Compounds of the present invention, in certain embodiments, display significant potency by causing, for example, inhibition of Stat3 activation, reduction in c-myc protein levels and/or induction of apoptosis in tumor cells. In general aspects, compounds of the present invention induce one or more of these activities at nanomolar concentrations and typically function through a unique mechanism involving the induction of stress granules that bind specific signaling molecules and prevent them from participating in signal transduction and oncogenesis.
    Type: Application
    Filed: July 2, 2007
    Publication date: November 18, 2010
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Nicholas J Donato, David Maxwell, Moshe Talpaz, William Bornmann, Zhenghong PENG, Ashutosh Pal, Dongmei Han, Shimei Wang, Geoffrey Bartholomeusz, Vaibhav Kapuria
  • Patent number: 7825150
    Abstract: Methods and compositions for treating immunological and inflammatory diseases and disorders are disclosed. Particular methods and compositions comprise the administration of an agent that inhibits S1P lyase activity and at least one additional immunosuppressive and/or anti-inflammatory agent.
    Type: Grant
    Filed: September 5, 2008
    Date of Patent: November 2, 2010
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventor: Tamas Oravecz
  • Patent number: 7799795
    Abstract: Provided herein are compounds of the formula where A1, A2, A3, A4, L, Q, R1, R2, R3, R4, Rx, Ry, Rz, X, Y1, Y2, Y4 and Z are as described herein, and compositions thereof that are useful in the treatment of inflammatory and immune conditions and diseases. In particular, the invention provides aryl nitrile compounds which modulate the expression and/or function of a chemokine receptor.
    Type: Grant
    Filed: June 26, 2006
    Date of Patent: September 21, 2010
    Assignee: Amgen Inc.
    Inventors: Philippe Bergeron, Xiaoqi Chen, Xiaohui Du, Jeffrey Deignan, Jason A. Duquette, Darin Gustin, Julio C. Medina, Jeffrey T. Mihalic, George R. Tonn
  • Publication number: 20100216854
    Abstract: The present invention provides novel 1,5 and 1,3,5-substituted imidazole compounds of formulas (I), (IIa), (IIIb) in hydrophilic or lipophilic form, which are useful as angiotensin II AT1 receptor antagonists with sympathetic suppressant properties. In particular, the invention provides pharmaceutical compositions containing the pharmacophoric groups of Losartan and Clonidine as well compounds, processes and intermediates for preparing compounds and their use in methods of treating hypertension and cardiovascular diseases through Renin Angiotensin System (RAS) and Sympathetic System (SS). Alkylated histamine based double action Saltans are lipophilic and can act transdermally.
    Type: Application
    Filed: July 25, 2008
    Publication date: August 26, 2010
    Applicant: Eldrug S.A.
    Inventors: John Matsoukas, Charalambos Gavras, Dimitrios Vlaxakos, Michael Maragoudakis
  • Patent number: 7741323
    Abstract: An indene derivative for selectively modulating the activities of peroxisome proliferator activated receptors (PPARs) having the following formula (I): wherein, R1 is C1-6 alkyl, C1-6 alkenyl, or C3-6 cycloalkyl, each of which is unsubstituted or substituted with one or more phenyl groups; R2 is H, CN, CO2Ra, CH2CO2Ra, CONRbRc, or phenyl; R3 is C1-6 alkyl, C3-6 cycloalkyl, naphthyl, phenyl, being each unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, CN, NH2, NO2, ORa, phenyloxy, C1-6 alkyl, and C3-6 cycloalkyl; and R4, R5, R6, and R7 are each independently H, OH, OSO2CH3, O(CH2)mRe, CH2Rf, OCOCH2ORg, OCH2CH2ORg, OCH2CH?CHRg, or pyridine-2-yloxy, or R5 and R6 together form OCH2O.
    Type: Grant
    Filed: April 13, 2005
    Date of Patent: June 22, 2010
    Assignees: Korea Research Institute of Chemical Technology, Jeil Pharm. Co., Ltd., Korea Research Institute of Bioscience and Biotechnology, CJ Corp.
    Inventors: Hyae Gyeong Cheon, Sung-Eun Yoo, Sung Soo Kim, Sung-Don Yang, Kwang-Rok Kim, Sang Dal Rhee, Jin Hee Ahn, Seung Kyu Kang, Won Hoon Jung, Sung Dae Park, Nam Gee Kim, Jang Hyuk Lee, Sun Chul Huh, Jae Mok Lee, Seog Beom Song, Soon Ji Kwon, Jong Hoon Kim, Jeong-Hyung Lee, Seung Jun Kim
  • Publication number: 20100152178
    Abstract: A CB2 receptor modulator comprising an imidazole derivative represented by the general formula (I): [wherein, R1 represents optionally substituted lower alkyl or the like; R2 represents optionally substituted cycloalkyl or the like; R3 represents optionally substituted aryl or the like; and n represents an integer of 0 to 3] or a pharmaceutically acceptable salt thereof as an active ingredient, and the like are provided.
    Type: Application
    Filed: September 5, 2007
    Publication date: June 17, 2010
    Applicant: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Naoto Osakada, Mariko Osakada, Takashi Sawada, Satoshi Kaneko, Atsuko Mizutani, Noriaki Uesaka, Yoshisuke Nakasato, Keishi Katayama, Masamori Sugawara, Yushi Kitamura
  • Patent number: 7714013
    Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, ?-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.
    Type: Grant
    Filed: August 28, 2006
    Date of Patent: May 11, 2010
    Assignee: Transtech Pharma, Inc.
    Inventors: Adnan M. M. Mjalli, Robert C. Andrews, Ramesh Gopalaswamy, Anitha Hari, Kwasi A. Avor, Ghassan Qabaja, Xiao-Chuan Guo, Suparna Gupta, David R. Jones, Xin Chen
  • Patent number: 7649098
    Abstract: Imidazole-based compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed.
    Type: Grant
    Filed: January 25, 2007
    Date of Patent: January 19, 2010
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: David J. Augeri, Jeffrey Bagdanoff, Lakmal W. Boteju, Kenneth G. Carson, Theodore C. Jessop, Spencer David Kimball
  • Publication number: 20090298901
    Abstract: (E)-1-(4-((1R,2S,3R)-1,2,3,4-tetrahydroxybutyl)-1H-imidazol-2-yl)-ethanone oxime dihydrate, compositions comprising it, and methods of its use are disclosed.
    Type: Application
    Filed: August 6, 2009
    Publication date: December 3, 2009
    Inventors: Wenxue Wu, Haiming Zhang
  • Publication number: 20090253656
    Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.
    Type: Application
    Filed: March 29, 2006
    Publication date: October 8, 2009
    Applicant: Kabushiki Kaisha Yakult Honsha
    Inventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
  • Publication number: 20090143597
    Abstract: Novel chemical compounds of the general formula K+A?, in which K+is a 5- or 6-membered heterocyclic ring having 1-3 hetereo atoms, which can be independently N, S, or O; with the proviso that at least one of the hetereo atoms must be a quaternized nitrogen atom having a —R?CN substituent, wherein R? is alkyl (C1 to C12); the heterocyclic ring having up to 4 or 5 substituents independently chosen from the moieties: (i) H; (ii) halogen or (iii) alkyl (C1 to C12), which is unsubstituted or partially or fully substituted by further groups, preferably F, Cl, N(CnF(2n+1?x)Hx)2, O(CnF(2n+1?x)Hx), SO2(CnF(2n+1?x)Hx)2 or CnF(2n+1?x)Hx where 1<n<6 and 0<x<13; and (iv) a phenyl ring which is unsubstituted or partially or fully substituted by further groups, preferably F, Cl, N(CnF(2n+1?x)Hx)2, O(CnF(2n+1?X)Hx), SO2(CnF(2n+1?x)Hx)2 or CnF(2n+1?x)Hx where 1<n<6 and 0<x?13; and A? is any anion that provides a salt with a low melting point, below about 100° C.
    Type: Application
    Filed: August 25, 2004
    Publication date: June 4, 2009
    Applicant: ECOLE POLYTECHNIQUE FEDERALE DE LAUSANNE
    Inventors: Paul Dyson, Dongbin Zhao, Zhaofu Fei
  • Publication number: 20090137817
    Abstract: Novel spatially-defined macrocyclic compounds containing specific conformational control elements are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target. In particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.
    Type: Application
    Filed: August 25, 2008
    Publication date: May 28, 2009
    Inventors: Pierre Deslongchamps, Yves Dory, Kamel Benakli, Eric Marsault, Luc Ouellet, Mahesh Ramaseshan, Martin Vezina, Daniel Fortin, Ruoxi Lan, Shigui Li, Gerald Villeneuve, Hamid R. Hoveyda, Sylvie Beaubien, Mark L. Peterson
  • Patent number: 7507757
    Abstract: Compounds are provided which are useful as antidiabetic agents and antiobesity agents and have the structure wherein m is 0, 1 or 2; n is 0, 1 or 2; Q is C or N; A is (CH2)x where x is 1 to 5, or A is (CH2)x1 where x1 is 1 to 5 with an alkenyl bond or an alkynyl bond embedded anywhere in the chain, or A is —(CH2)x2—O—(CH2)x3— where x2 is 0 to 5 and x3 is 0 to 5, provided that at least one of x2 and x3 is other than 0; B is a bond or is (CH2)x4 where x4 is 1 to 5; X is CH; X2 is N; X3 is C; X4 is N; X5 is C; X6 is C.
    Type: Grant
    Filed: December 17, 2004
    Date of Patent: March 24, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter T. W. Cheng, Sean Chen, Charles Z. Ding, Timothy F. Herpin
  • Publication number: 20080261985
    Abstract: This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-?, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.
    Type: Application
    Filed: November 16, 2007
    Publication date: October 23, 2008
    Inventors: Tadashi Honda, Chitra Sundararajan, Gordon W. Gribble, Michael B. Sporn, Karen T. Liby
  • Publication number: 20080166243
    Abstract: The invention relates to a liquid for compressing a gaseous medium which transfers the force required for compression directly to the gas. The liquid has a vapour pressure of less than 10?3 mbar.
    Type: Application
    Filed: May 3, 2006
    Publication date: July 10, 2008
    Inventors: Michael Kotschan, Roland Kalb
  • Publication number: 20080138704
    Abstract: An object of the present invention is to provide a material for an electrolytic solution having improved ionic conductivity and, showing excellent in low temperature property, being stable with time, and being electrochemically stable at a high potential, and an ionic material-containing composition exhibiting excellent fundamental performance such as electrochemical stability, and preferably used in a variety of utilities. Another object of the present invention is to provide utilities thereof. The material for an electrolytic solution is the material containing an ionic compound, and the material comprises a cyano group-containing anion represented by the formula (1); and 1 to 99% by mass of a solvent in 100% by mass of the material for an electrolytic solution.
    Type: Application
    Filed: May 9, 2005
    Publication date: June 12, 2008
    Applicant: Nippon Shokubai Co., Ltd.
    Inventors: Keiichiro Mizuta, Keiko Takebe
  • Publication number: 20080125473
    Abstract: This invention relates to a range of alpha substituted 2-benzyl substituted imidazole compounds and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.
    Type: Application
    Filed: November 26, 2007
    Publication date: May 29, 2008
    Applicant: PFIZER LIMITED
    Inventors: NATHAN ANTHONY LOGAN CHUBB, MARK ROGER COX, JEROME SEBASTIEN DAUVERGNE, RICHARD ANDREW EWIN, CHRISTELLE LAURET
  • Publication number: 20080119536
    Abstract: This invention relates to a range of alpha substituted 2-benzyl substituted imidazole compounds and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.
    Type: Application
    Filed: November 26, 2007
    Publication date: May 22, 2008
    Applicant: PFIZER LIMITED
    Inventors: NATHAN ANTHONY LOGAN CHUBB, MARK ROGER COX, JEROME SEBASTIEN DAUVERGNE, RICHARD ANDREW EWIN, CHRISTELLE LAURET
  • Patent number: 7361678
    Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, ?-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.
    Type: Grant
    Filed: March 5, 2003
    Date of Patent: April 22, 2008
    Assignee: TransTech Pharma, Inc.
    Inventors: Adnan M. M. Mjalli, Robert C. Andrews, Ramesh Gopalaswamy, Anitha Hari, Kwasi S. Avor, Ghassan Qabaja, Xiao-Chuan Guo, Suparna Gupta, David R. Jones, Xin Chen
  • Patent number: 7332608
    Abstract: The present invention is related to a process for preparing anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).
    Type: Grant
    Filed: November 9, 2006
    Date of Patent: February 19, 2008
    Assignee: SANOFI-AVENTIS Deutschland GmbH
    Inventors: Joachim Brendel, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
  • Patent number: 7323484
    Abstract: The present invention is directed to compounds of the formula wherein the variables are as defined in the specification. The compounds are useful for inhibiting farnesyl transferase and for the treatment of tumors and restenosis.
    Type: Grant
    Filed: November 28, 2005
    Date of Patent: January 29, 2008
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques, S.A.S.
    Inventors: Thomas D. Gordon, Barry A. Morgan
  • Patent number: 7271189
    Abstract: The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders in which cannabinoid receptors are involved. The compounds have the general formula (I) wherein R, R1-R4 and X have the meanings given in the specification.
    Type: Grant
    Filed: October 15, 2004
    Date of Patent: September 18, 2007
    Assignee: Solvay Pharmaceuticals, Inc.
    Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Herman H. Van Stuivenberg, Hiskias G. Keizer
  • Patent number: 7235690
    Abstract: The present invention is related to anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: June 26, 2007
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Joachim Brendel, Bernard Pirard, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
  • Patent number: 7164028
    Abstract: Cyanoacetamides of the formula: and corresponding salts thereof; N?-(cyanoacetyl)-L-histidines, of the formula: and salts, tautomers and esters thereof; and N?-(cyanoacetyl)-3-methyl-L-histidines of the formula: and salts and esters thereof.
    Type: Grant
    Filed: April 11, 2005
    Date of Patent: January 16, 2007
    Assignee: Lonza AG
    Inventors: Stefan Hildbrand, Thomas Ruppen, Dario Veghini
  • Patent number: RE39634
    Abstract: The present invention relates to bisarylimidazolyl derivatives and pharmaceutical compositions comprising said compounds inhibiting fatty acid amide hydrolase and useful for the treatment of pain, particularly neuropathic pain, psychomotor disorder, hypertension, cardiovascular disease, eating disorder, nausea, AIDS-related complex, glaucoma, inflammation, psoriasis or multiple sclerosis, and other conditions the treatment of which can be effected by inhibiting fatty acid amide hydrolase.
    Type: Grant
    Filed: July 1, 2004
    Date of Patent: May 15, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Sing-Yuen Sit, Kai Xie