The Nitrogen Is Multiply Bonded To Carbon Patents (Class 548/336.1)
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Patent number: 10689478Abstract: 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: GrantFiled: August 3, 2017Date of Patent: June 23, 2020Assignee: KOEI CHEMICAL COMPANY, LIMITEDInventors: Motoyoshi Miyagi, Shingo Nitta, Hitomi Tsuboi, Shogo Takahashi
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Publication number: 20150126746Abstract: 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: ApplicationFiled: April 26, 2013Publication date: May 7, 2015Inventor: Grégory Schmidt
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Publication number: 20140357673Abstract: 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: ApplicationFiled: July 31, 2014Publication date: December 4, 2014Inventors: Nicholas J. Donato, Christiane Wobus, Hollis D. Showalter, Moshe Talpaz, Jeffrey William Perry, Roderick Joseph Sorenson, Mary Xuan Dziem O'Riordan, Yafei Jin
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Publication number: 20140275569Abstract: 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: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Inventors: Richard W. Morrison, Douglas Michael Jackson
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Patent number: 8785654Abstract: 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: GrantFiled: January 31, 2012Date of Patent: July 22, 2014Assignee: Nippon Soda Co., Ltd.Inventors: Mitsuru Takase, Fuminori Komatsu
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Patent number: 8623942Abstract: 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: GrantFiled: March 9, 2010Date of Patent: January 7, 2014Assignee: Nippon Soda Co., Ltd.Inventors: Masami Kaneko, Kazuo Ono, Natsuki Amanokura, Naoyuki Kamegaya
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Patent number: 8518999Abstract: 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: GrantFiled: December 1, 2005Date of Patent: August 27, 2013Assignee: Genzyme CorporationInventors: Scott F. Sneddon, John L. Kane, Bradford H. Hirth, Fred Vinick, Shuang Qiao, Sharon R. Nahill, John M. Williams, Hans-Peter Biemann
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Publication number: 20130203895Abstract: 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: ApplicationFiled: March 15, 2013Publication date: August 8, 2013Applicant: DESIGNER MOLECULES, INC.Inventor: Designer Molecules, Inc.
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Publication number: 20130123287Abstract: 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: ApplicationFiled: July 21, 2011Publication date: May 16, 2013Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Koji Sugimoto, Hiroyuki Hayashi
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Patent number: 8383829Abstract: 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: GrantFiled: April 7, 2009Date of Patent: February 26, 2013Assignee: Konica Minolta Holdings, Inc.Inventors: Kaori Ono, Osamu Ishige, Takeshi Hakii, Akihito Hisamitsu
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Publication number: 20120108820Abstract: Novel chemical compounds of the general formula K+A? useful as industrial solvents, especially as ligands, for efficient catalyst recycling.Type: ApplicationFiled: December 16, 2011Publication date: May 3, 2012Inventors: Paul Dyson, Dongbin Zhao, Zhaofu Fei
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Publication number: 20120077806Abstract: 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: ApplicationFiled: September 23, 2011Publication date: March 29, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Nicholas J. Donato, Christiane Wobus, Hollis D. Showalter, Moshe Talpaz, Jeffrey W. Perry, Roderick J. Sorenson, Mary X. O'Riordan, Yafei Jin
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Patent number: 8093267Abstract: 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: GrantFiled: December 1, 2009Date of Patent: January 10, 2012Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David J. Augeri, Jeffrey Bagdanoff, Lakmal W. Boteju, Kenneth G. Carson, Theodore C. Jessop, Spencer David Kimball
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Publication number: 20110274907Abstract: 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: ApplicationFiled: November 24, 2009Publication date: November 10, 2011Inventors: Mark Raymond Steele, Andrew Gibbs, Amy Grace Atinkson
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Publication number: 20110251200Abstract: 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: ApplicationFiled: September 11, 2009Publication date: October 13, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Gary D. Glick, Peter Toogood, Gina Ney
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Publication number: 20110230428Abstract: 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: ApplicationFiled: July 22, 2009Publication date: September 22, 2011Inventors: John Wityak, Leticia M. Toledo-sherman, Celia Dominguez, Stephen Martin Courtney, Christopher John Yarnold, Paula C. De Aguiar Pena, Andreas Scheel, Dirk Winkler
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Patent number: 8022072Abstract: 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: GrantFiled: June 17, 2008Date of Patent: September 20, 2011Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Hironobu Ogura, Yoshiyuki Tatsumi, Yuji Fukamizu
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Publication number: 20110224252Abstract: 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: ApplicationFiled: October 24, 2008Publication date: September 15, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Raphael Dumeunier, Clemens Lamberth, Stephan Trah, Sebastian Wendeborn
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Publication number: 20110152175Abstract: 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: ApplicationFiled: September 18, 2009Publication date: June 23, 2011Applicant: Instytut Chemii Organicznej Polska Akademia NaukInventors: Zofia Lipkowska, Piotr Polcyn, Andrzej Wojciech Lipkowski
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Publication number: 20110092557Abstract: 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: ApplicationFiled: June 24, 2009Publication date: April 21, 2011Applicant: INFLUMEDIX INC.Inventors: Xiaodong Fan, Lidia Cristian
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Publication number: 20110077409Abstract: Cyano-substituted sulfilimines are produced efficiently and in high yield from the corresponding sulfides by reaction with cyanamide and hypochlorite.Type: ApplicationFiled: November 18, 2010Publication date: March 31, 2011Inventors: David E. Podhorez, Ronald Ross, JR., James R. McConnell
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Publication number: 20110071303Abstract: Methods of preparing imidazole-based compounds are disclosed.Type: ApplicationFiled: September 20, 2010Publication date: March 24, 2011Inventors: Wenxue Wu, Jie Yan, Haiming Zhang
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Patent number: 7897633Abstract: 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: GrantFiled: October 24, 2007Date of Patent: March 1, 2011Assignee: Probiodrug AGInventors: Stephan Schilling, Mirko Buchholz, Andre Niestroj, Ulrich Heiser, Hans-Ulrich Demuth
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Publication number: 20100324273Abstract: 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: ApplicationFiled: August 30, 2010Publication date: December 23, 2010Applicant: Saint Mary's UniversityInventors: Robert D. Singer, Prashant Upendra Naik
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Publication number: 20100304966Abstract: 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: ApplicationFiled: October 9, 2008Publication date: December 2, 2010Applicant: BASF SEInventors: Joachim Rheinheimer, Barbara Nave, Doris Kremzow, Stefan Redlich, Christian Pilger, Claudia Rosenbaum, Wassilios Grammenos
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Publication number: 20100292229Abstract: 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: ApplicationFiled: July 2, 2007Publication date: November 18, 2010Applicant: The Board of Regents of the University of Texas SystemInventors: Nicholas J Donato, David Maxwell, Moshe Talpaz, William Bornmann, Zhenghong PENG, Ashutosh Pal, Dongmei Han, Shimei Wang, Geoffrey Bartholomeusz, Vaibhav Kapuria
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Patent number: 7825150Abstract: 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: GrantFiled: September 5, 2008Date of Patent: November 2, 2010Assignee: Lexicon Pharmaceuticals, Inc.Inventor: Tamas Oravecz
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Patent number: 7799795Abstract: 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: GrantFiled: June 26, 2006Date of Patent: September 21, 2010Assignee: 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
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Publication number: 20100216854Abstract: 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: ApplicationFiled: July 25, 2008Publication date: August 26, 2010Applicant: Eldrug S.A.Inventors: John Matsoukas, Charalambos Gavras, Dimitrios Vlaxakos, Michael Maragoudakis
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Patent number: 7741323Abstract: 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: GrantFiled: April 13, 2005Date of Patent: June 22, 2010Assignees: 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
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Publication number: 20100152178Abstract: 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: ApplicationFiled: September 5, 2007Publication date: June 17, 2010Applicant: 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
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Patent number: 7714013Abstract: 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: GrantFiled: August 28, 2006Date of Patent: May 11, 2010Assignee: 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
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Patent number: 7649098Abstract: 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: GrantFiled: January 25, 2007Date of Patent: January 19, 2010Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David J. Augeri, Jeffrey Bagdanoff, Lakmal W. Boteju, Kenneth G. Carson, Theodore C. Jessop, Spencer David Kimball
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Publication number: 20090298901Abstract: (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: ApplicationFiled: August 6, 2009Publication date: December 3, 2009Inventors: Wenxue Wu, Haiming Zhang
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Publication number: 20090253656Abstract: 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: ApplicationFiled: March 29, 2006Publication date: October 8, 2009Applicant: Kabushiki Kaisha Yakult HonshaInventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
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Publication number: 20090143597Abstract: 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: ApplicationFiled: August 25, 2004Publication date: June 4, 2009Applicant: ECOLE POLYTECHNIQUE FEDERALE DE LAUSANNEInventors: Paul Dyson, Dongbin Zhao, Zhaofu Fei
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Publication number: 20090137817Abstract: 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: ApplicationFiled: August 25, 2008Publication date: May 28, 2009Inventors: 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
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Patent number: 7507757Abstract: 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: GrantFiled: December 17, 2004Date of Patent: March 24, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. W. Cheng, Sean Chen, Charles Z. Ding, Timothy F. Herpin
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Publication number: 20080261985Abstract: 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: ApplicationFiled: November 16, 2007Publication date: October 23, 2008Inventors: Tadashi Honda, Chitra Sundararajan, Gordon W. Gribble, Michael B. Sporn, Karen T. Liby
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Publication number: 20080166243Abstract: 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: ApplicationFiled: May 3, 2006Publication date: July 10, 2008Inventors: Michael Kotschan, Roland Kalb
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Publication number: 20080138704Abstract: 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: ApplicationFiled: May 9, 2005Publication date: June 12, 2008Applicant: Nippon Shokubai Co., Ltd.Inventors: Keiichiro Mizuta, Keiko Takebe
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Publication number: 20080125473Abstract: 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: ApplicationFiled: November 26, 2007Publication date: May 29, 2008Applicant: PFIZER LIMITEDInventors: NATHAN ANTHONY LOGAN CHUBB, MARK ROGER COX, JEROME SEBASTIEN DAUVERGNE, RICHARD ANDREW EWIN, CHRISTELLE LAURET
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Publication number: 20080119536Abstract: 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: ApplicationFiled: November 26, 2007Publication date: May 22, 2008Applicant: PFIZER LIMITEDInventors: NATHAN ANTHONY LOGAN CHUBB, MARK ROGER COX, JEROME SEBASTIEN DAUVERGNE, RICHARD ANDREW EWIN, CHRISTELLE LAURET
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Patent number: 7361678Abstract: 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: GrantFiled: March 5, 2003Date of Patent: April 22, 2008Assignee: 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
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Patent number: 7332608Abstract: 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: GrantFiled: November 9, 2006Date of Patent: February 19, 2008Assignee: SANOFI-AVENTIS Deutschland GmbHInventors: Joachim Brendel, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
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Patent number: 7323484Abstract: 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: GrantFiled: November 28, 2005Date of Patent: January 29, 2008Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques, S.A.S.Inventors: Thomas D. Gordon, Barry A. Morgan
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Patent number: 7271189Abstract: 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: GrantFiled: October 15, 2004Date of Patent: September 18, 2007Assignee: Solvay Pharmaceuticals, Inc.Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Herman H. Van Stuivenberg, Hiskias G. Keizer
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Patent number: 7235690Abstract: 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: GrantFiled: April 26, 2002Date of Patent: June 26, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Joachim Brendel, Bernard Pirard, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
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Patent number: 7164028Abstract: 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: GrantFiled: April 11, 2005Date of Patent: January 16, 2007Assignee: Lonza AGInventors: Stefan Hildbrand, Thomas Ruppen, Dario Veghini
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Patent number: RE39634Abstract: 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: GrantFiled: July 1, 2004Date of Patent: May 15, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Sing-Yuen Sit, Kai Xie