Plural Isoquinoline Ring Systems Attached Directly Or Indirectly To Each Other By Nonionic Bonding Patents (Class 546/140)
-
Publication number: 20110288293Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.Type: ApplicationFiled: December 25, 2009Publication date: November 24, 2011Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Tetsuo Takayama, Hajime Asanuma, Daisuke Wakasugi, Rie Nishikawa, Yoshinori Sekiguchi, Madoka Kawamura, Naoya Ono, Tetsuya Yabuuchi, Takahiro Oi, Yusuke Oka, Shoichi Kuroda, Fumito Uneuchi, Takeshi Koami
-
Publication number: 20110284832Abstract: A compound for an organic photoelectric device, the compound being represented by the following Chemical Formula 1:Type: ApplicationFiled: June 30, 2011Publication date: November 24, 2011Inventors: Kyu-Yeol In, Myeong-Soon Kang, Ho-Kuk Jung, Nam-Soo Kim, Eui-Su Kang, Mi-Young Chae
-
Patent number: 8030341Abstract: The present invention relates to symmetric and asymmetric dimeric Dmt (2?,6?-ditnethyl) compounds and Dmt derivative compounds with dual ? and ? opioid receptor antagonist activity. Also, the present invention provides compositions comprising these compounds and it provides methods of using these compounds.Type: GrantFiled: August 30, 2006Date of Patent: October 4, 2011Assignees: The United States of America as represented by the Secretary of the Department of Health and Human Services, Kobe Gakuin UniversityInventors: Lawrence H. Lazarus, Yoshio Okada, Tingyou Li
-
Publication number: 20110152282Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or GIi gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).Type: ApplicationFiled: August 24, 2009Publication date: June 23, 2011Applicant: IRM LLCInventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
-
Publication number: 20110117081Abstract: A compound of Formula (1) or a salt thereof, methods for the preparation and use of such a compound, especially as an IAP inhibitor, and related compounds, compositions, and methods.Type: ApplicationFiled: May 5, 2009Publication date: May 19, 2011Applicant: Aegera Therapeutics, Inc.Inventors: Alain Laurent, Melanie Proulx, James Jaquith
-
Publication number: 20110105556Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.Type: ApplicationFiled: December 22, 2006Publication date: May 5, 2011Applicant: UNIVERSITY OF KENTUCKY RESEARCH FOUNDATIONInventors: Peter A. Crooks, Linda P. Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
-
Patent number: 7932266Abstract: The invention relates to derivative compounds of partially-reduced isoquinoline with substitution of a sec-butyl group at position 3 with calpain inhibitor activity. The inventive compound comprises an ester or amide derived from (3-sec-butyl-1-oxo-2,3-dihydro-1H-isoquinolin-4-yliden)-acetic acid and (3-sec-butyl-1-thioxo-2, 3-dihydro-1H-isoquinolin-4-yliden)-acetic acid. Compounds having formula I or II can be used in the preventive or therapeutic treatment of a degenerative disease.Type: GrantFiled: December 5, 2005Date of Patent: April 26, 2011Assignee: Consejo Superior de Investigaciones CientificasInventors: Bernardo Herradon García, Roberto Chicharro Martin, Vicente Jesús Aran Redo, Mercedes Alonso Giner
-
Publication number: 20110024725Abstract: The present invention relates to a novel anthracene derivative and an organic electronic device using the same. The organic electronic device according to the present invention shows excellent characteristics in efficiency, driving voltage, and life time.Type: ApplicationFiled: May 16, 2008Publication date: February 3, 2011Inventors: Dong-Hoon Lee, Jae-Chol Lee, Jae-Soon Bae, Jun-Gi Jang, Kong-Kyeom Kim, Dae-Woong Lee
-
Patent number: 7872138Abstract: The present invention is directed to a process for the synthesis of substituted-1,2,3,4-tetrahydroisoquinoline derivatives, useful as intermediates in the synthesis of pharmaceutical agents.Type: GrantFiled: August 7, 2007Date of Patent: January 18, 2011Assignee: Janssen Pharmaceutica NVInventors: Frank J. Villani, Hua Zhong
-
Patent number: 7872137Abstract: A process for preparing the [R—[R*,R*-(E)]]-2,2?-(1,8-dioxo-4-octene-1,8-diyl) bis(oxy-3,1-propanediyl)bis(1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-[(3,4,5-trimethoxyphenyl) methyl]isoquinolinium) dichloride, commonly known as mivacurium chloride, useful as short-duration neuromuscular blocking agent.Type: GrantFiled: June 19, 2007Date of Patent: January 18, 2011Assignee: Farmabios S.p.A.Inventors: Maurizio Francesco Velati, Andrea Busca, Cristina Manfrotto, Marco Nicolini, Claudio Gianluca Pozzoli
-
Publication number: 20100286198Abstract: Anti-infective and biofilm-inhibiting activities of aryl isoquinoline-derivatives of the general formulae 1 to 3 are described.Type: ApplicationFiled: September 27, 2007Publication date: November 11, 2010Inventors: Gerhard Bringmann, Tanja Gulder, Ute Hentschel, Frank Meyer, Heidrun Moll, Joachim Morschhäuser, Alicia Ponte-Sucre De Vanegas, Wilma Ziebuhr, August Stich, Reto Brun, Werner E.G. Müller, Virima Mudogo
-
Publication number: 20100256381Abstract: The present invention provides a process of producing cisatracurium compounds, e.g., cisatracurium besylate, from isoquinolinium salts of the structural formula (VIIA) wherein X? is an anion and R is H or a C1-C6 alkyl, or an activated form of the carboxylic acid with 1,5-pentanediol to form a cisatracurium salt, optionally via an intermediate compound (VIII). The cisatracurium compounds can be purified using simple techniques to afford pure cisatracurium besylate without the need for HPLC purification.Type: ApplicationFiled: May 1, 2008Publication date: October 7, 2010Applicant: CHEMAGIS LTD.Inventors: Oded Arad, Vladimir Naddaka, Eyal Klopfer, Shady Saeed, Ofer Sharon
-
Publication number: 20100234602Abstract: The present invention provides R,R?-atracurium salts processes for producing and purifying such salts, and methods of using such salts to produce highly pure cisatracurium besylate.Type: ApplicationFiled: October 7, 2008Publication date: September 16, 2010Applicant: CHEMAGIS LTD.Inventors: Oded Arad, Ofer Sharon, Elena Ostrovsky
-
Publication number: 20100215616Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: February 8, 2010Publication date: August 26, 2010Inventors: Jeffrey Lee Romine, Denis R. St. Laurent, Makonen Belema, Lawrence B. Snyder, Lawrence G. Hamann, John F. Kadow, Jayne Kapur, Andrew C. Good, Omar D. Lopez, Rico Lavoie, John A. Bender
-
Publication number: 20100210622Abstract: In one aspect, the present invention provides for a compound of Formula I in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.Type: ApplicationFiled: December 17, 2009Publication date: August 19, 2010Inventors: Jonathan Bayldon Baell, Chinh Thien Bui, Peter Colman, Peter Czabotar, Danette A. Dudley, Wayne J. Fairbrother, John A, Flygare, Guillaume Laurent Lessene, Chudi Ndubaku, George Nikolakopoulos, Brad Edmund Sleebs, Brian John Smith, Keith Geoffrey Watson, Steven W. Elmore, Lisa A. Hasvold, Andrew M. Petros, Andrew J. Souers, Zhi-Fu Tao, Le Wang, Xilu Wang, Kurt Deshayes
-
Publication number: 20100187505Abstract: The present invention relates to the compounds of the formula (1) and to organic electroluminescent devices, in particular blue-emitting devices, in which these compounds are used as host material or dopant in the emitting layer and/or as hole-transport material and/or as electron-transport material.Type: ApplicationFiled: April 29, 2008Publication date: July 29, 2010Inventors: Philipp Stoessel, Arne Buesing, Holger Heil
-
Publication number: 20100174082Abstract: The present invention provides an improved method for obtaining cisatracurium besylate, which preferably chromatographically separating cisatracurium besylate from a mixture of (1R,1?R)-atracurium isomers via flash chromatographyType: ApplicationFiled: March 5, 2008Publication date: July 8, 2010Applicant: Chemagis Ltd.Inventors: Oded Arad, Elena Ostrovsky
-
Publication number: 20100168431Abstract: The present invention provides novel isoquinolinium compounds, methods of producing the isoquinolinium compounds, and methods for converting them into cisatracurium, e.g., cisatracurium besylate.Type: ApplicationFiled: May 1, 2008Publication date: July 1, 2010Applicant: Chemagis Ltd.Inventors: Vladimir Naddaka, Shen Jingshan, Oded Arad, Guo Hongli, Ofer Sharon, Eyal Klopfer, Shady Saeed
-
Publication number: 20100168160Abstract: Genipin derivatives and pharmaceutical compositions thereof that inhibit the activity of uncoupling protein-2 (UCP2) and are useful in treating deficient first-phase insulin secretion, non-insulin dependent diabetes mellitus, and ischemia in a mammal are disclosed.Type: ApplicationFiled: November 19, 2009Publication date: July 1, 2010Applicant: Beth Israel Deaconess Medical Center , Inc. And Trustees of Boston UniversityInventors: Chen-Yu Zhang, Bradford B. Lowell, John A. Porco, JR., Ruichao Shen, Cheng T. Lin, Stefan Krauss
-
Publication number: 20100099878Abstract: The present invention provides an improved method of chromatographically separating the isomers of (1R,rR)-atracurium salts by high-performance liquid chromatography (HPLC), in the absence of a strong acid. The separation is preferably performed on a silica gel HPLC column using an eluent containing an organic solvent, a polar aprotic co-solvent and a weak organic acid.Type: ApplicationFiled: March 5, 2008Publication date: April 22, 2010Applicant: Chemagis Ltd.Inventors: Oded Arad, Elena Ostrovsky
-
Publication number: 20100087650Abstract: Provided is a method for separating cisatracurium from a mixture of atracurium isomers, which method includes eluting from a Reverse Phase (RP) stationary phase with a mobile phase in which the isomers are stable. The method of the present invention can be conveniently and inexpensively scaled up.Type: ApplicationFiled: March 5, 2008Publication date: April 8, 2010Applicant: CHEMAGIS LTD.Inventors: Elena Ostrovsky, Oded Arad
-
Publication number: 20100069432Abstract: Provided are bis-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.Type: ApplicationFiled: May 14, 2007Publication date: March 18, 2010Applicant: University of Kentucky Research FoundationInventors: Peter Crooks, Linda P. Dwoskin, Guangrong Zheng, Zhenta Zheng, Sangeetha Sumithran, Marharyta Pivavarchyk
-
Publication number: 20100048618Abstract: The present application discloses derivatives of 8-epiblechnic acid and use thereof in treating a disease related to endothelin receptor A or endothelin-1 (ET-1) over-expression, such as hypertension, cancer, atherosclerosis, and myocardial infarction.Type: ApplicationFiled: August 18, 2009Publication date: February 25, 2010Inventors: Hardy Chan, Chung Faye Chao, Vallapa Soong
-
Publication number: 20100029658Abstract: The present invention relates to novel quinoxaline, quinazoline and phthalazine derivatives as well as multimeric derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds for the treatment and prevention of brain damage resulting from brain injury, especially secondary brain damage due to traumatic brain injury (TBI). The compounds of the invention are also useful in treating and preventing neurodegenerative diseases.Type: ApplicationFiled: August 22, 2006Publication date: February 4, 2010Inventors: Moshe Gavish, Jehuda Arieh Veenman, Alex Shterenberg, Ilan Marek
-
Publication number: 20100016596Abstract: A process for the preparation of neuromuscular blocking agents with isoquinoline structure, such as atracurium besylate, doxacurium chloride, mivacurium chloride and gantacurium chloride, by chromatographic purification of their mixtures of isomers using a silica modified by treatment with a tertiary amine of formula NR1R2R3 or a corresponding quaternary ammonium compound N+R1R2R3R4X? wherein R1, R2, R3 and R4, the same or different, are linear or branched C1-C4 alkyl groups or —CH2—Ar groups or two among R1, R2, R3 and R4 form a 5- or 6-membered cycle, optionally substituted with a —CH2—Ar group or condensed with an Ar group, Ar being an aryl optionally substituted with one or more electrodonating groups, and X? being a suitable anion, is described.Type: ApplicationFiled: July 10, 2009Publication date: January 21, 2010Applicant: FARMABIOS S.P.A.Inventors: Claudio Gianluca POZZOLI, Franco MALANGA, Vincenzoi Redaelli
-
Publication number: 20090273277Abstract: The present invention relates to novel organic electroluminescent compounds, and organic electroluminescent devices employing the same as electroluminescent material. Specifically, the organic electroluminescent compounds according to the invention are characterized in that they are represented by Chemical Formula (1): wherein, R1, R2, R3 and R4 are independently selected from the following structures: A represents (C6-C60)arylene or (C5-C60)heteroarylene; and m and n independently represent an integer from 0 to 4, provided that m+n is an integer from 1 to 8. Since the organic electroluminescent compounds according to the invention have good luminous efficiency and excellent color purity and life property of material, OLED's having very good operation life can be manufactured therefrom.Type: ApplicationFiled: March 19, 2009Publication date: November 5, 2009Applicant: Gracel Display Inc.Inventors: Soo Young Lee, Young Jun Cho, Hyuck Joo Kwon, Bong Ok Kim, Sung Min Kim, Seung Soo Yoon
-
Publication number: 20090209528Abstract: The present invention relates to substituted tetrahydroisoquinoline compounds of general formula (I), a process for their preparation, medicaments comprising said substituted tetrahydroisoquinoline compounds as well as the use of said substituted tetrahydroisoquinoline compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.Type: ApplicationFiled: March 23, 2007Publication date: August 20, 2009Applicant: LABORATORIOS DEL DR. ESTEVE S.A.Inventors: Josep Mas Prio, Adriana Port Casamitjana, Helmut Heinrich Buschmann
-
Patent number: 7572783Abstract: The present invention relates to the compounds of Formula I, their preparation and pharmaceutical compositions comprising them. The compounds and pharmaceutical compositions are useful, for example, for the treatment and prevention of obesity, obesity-related disorders and eating disorders.Type: GrantFiled: August 12, 2005Date of Patent: August 11, 2009Assignee: Amgen Inc.Inventors: Xi Chen, Xiaoqi Chen, Richard Victor Connors, Kang Dai, Ying Fu, Juan C. Jaen, Yong-Jae Kim, Leping Li, Mike E. Lizarzaburu, Jeffrey T. Mihalic, Stephen J. Shuttleworth
-
Publication number: 20090192146Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.Type: ApplicationFiled: February 9, 2009Publication date: July 30, 2009Applicant: ACEA BIOSCIENCES, INC.Inventors: Xiao XU, Haoyun An, Xiaobo Wang
-
Publication number: 20090143424Abstract: Provided are tetrakis-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.Type: ApplicationFiled: October 29, 2008Publication date: June 4, 2009Applicant: UNIVERSITY OF KENTUCKY RESEARCH FOUNDATIONInventors: PETER A. CROOKS, Linda P. Dwoskin, Zhenfa Zhang, Marharyta Pivavarchyk
-
Patent number: 7541467Abstract: A compound represented by the following general formula (I) or a salt thereof: wherein R1, R2, R3, and R4 independently represent 2-quinolyl group which may be substituted, 1-isoquinolyl group which may be substituted, or 3-isoquinolyl group which may be substituted; m, n, p, and q independently represent 1 or 2; and L represents a single bond, or an alkylene group having 1 to 5 carbon atoms wherein said alkylene group may contain one or more heteroatoms in the main chain, and may have one or more substituents on the main chain, which is useful as a fluorescent zinc ion sensor.Type: GrantFiled: July 30, 2004Date of Patent: June 2, 2009Assignees: Sekisui Medical Co., Ltd.Inventors: Shigenobu Yano, Yuji Mikata
-
Publication number: 20090126125Abstract: The present disclosure relates to the dyeing of keratin materials using thiol/disulfide styryl tetrahydroquinolinium fluorescent dyes. Disclosed herein is a dye composition comprising a thiol/disulfide styryl tetrahydroquinolinium fluorescent dye and a dyeing process with, for instance, a lightening effect on keratin materials such as hair, using said composition. Disclosed herein are thiol fluorescent dyes and the uses thereof in lightening keratin materials. This composition can be used to obtain a lightening effect which can be resistant and visible on dark keratin fibers.Type: ApplicationFiled: September 19, 2008Publication date: May 21, 2009Inventors: Andrew GREAVES, Nicolas DAUBRESSE, Franco MANFRE
-
Patent number: 7524861Abstract: A hydrate of an acid addition bis-salt of an anthranilic acid derivative is produced by a process which comprises: (a) combining, in any order, the anthranalic acid derivative, a pharmaceutically acceptable organic solvent, an excess of water and a pharmaceutically acceptable strong acid to form a mixture; (b) warming the mixture until a clear solution forms; (c) filtering the solution while it is warm, to yield a filtrate; and (d) recovering the hydrate as defined above from the filtrate. The hydrate has a defined number of moles of water of crystallization and possesses better storage stability and dissolution characteristics than conventionally produced hydrates of such acid addition bis-salts.Type: GrantFiled: May 13, 2003Date of Patent: April 28, 2009Inventors: David Frank Hayman, Michael Wright
-
Publication number: 20090093517Abstract: Use of Bis 1,2,3,4-tetrahydroisoquinoline derivatives represented by formula (I) as SK channel blockers and for the preparation of a medicament useful for the treatment of disorders of the central nervous system.Type: ApplicationFiled: March 3, 2007Publication date: April 9, 2009Applicant: UNIVERSITE DE LIEGEInventors: Amaury Graulich, Jean-Francois Liegeois, Jacqueline Moreau, Vincent Seutin
-
Publication number: 20090069370Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.Type: ApplicationFiled: September 11, 2008Publication date: March 12, 2009Applicant: WyethInventors: Dahui Zhou, Jonathan Laird Gross, Albert Jean Robichaud
-
Publication number: 20090069300Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.Type: ApplicationFiled: September 11, 2008Publication date: March 12, 2009Applicant: WyethInventors: Dahui Zhou, Jonathan Laird Gross, Albert Jean Robichaud
-
Patent number: 7476679Abstract: Compounds which bind to opioid receptors are provided. In a preferred embodiment of the invention, the compounds are opioid receptor antagonists. The present invention also provides methods of treating conditions which are mediated by an opioid receptor.Type: GrantFiled: July 26, 2005Date of Patent: January 13, 2009Assignee: Research Triangle InstituteInventors: Frank Ivy Carroll, Hernan A Navarro, S. Wayne Mascarella, James B. Thomas
-
Publication number: 20080287490Abstract: N-n-Alkylation of nicotine converts nicotine from an agonist into an antagonist specifically for neuronal nicotinic acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. Conformationally restricted analogs exhibit both high affinity and selectivity at this site, and are able to access the brain due to their ability to act as substrates for the blood-brain barrier choline transporter.Type: ApplicationFiled: July 17, 2008Publication date: November 20, 2008Applicant: UNIVERSITY OF KENTUCKY RESEARCH FOUNDATIONInventors: Peter A. Crooks, Linda P. Dwoskin, Joshua Ayers, Vladimir Grinevich, Sangeetha Sumithran
-
Publication number: 20080269143Abstract: The present invention relates to symmetric and asymmetric dimeric Dmt (2?,6?-ditnethyl) compounds and Dmt derivative compounds with dual ? and ? opioid receptor antagonist activity. Also, the present invention provides compositions comprising these compounds and it provides methods of using these compounds.Type: ApplicationFiled: August 30, 2006Publication date: October 30, 2008Applicant: GOVERNMENT OF THE UNITED STATES OF AMERICA, REPRESENTED BY THE SECRETARY,Inventors: Lawrence H. Lazarus, Yoshio Okada, Tingyou Li
-
Publication number: 20080227778Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: ApplicationFiled: September 17, 2004Publication date: September 18, 2008Inventors: Christopher J. Dinsmore, Jeffrey M. Bergman, Charles J. McIntyre, David A. Claremon
-
Publication number: 20080161346Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as VEGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: December 19, 2007Publication date: July 3, 2008Applicant: Amgen Inc.Inventors: Yuan Cheng, Deborah Choquette, Jean-Christophe Harmange, Andrew Tasker
-
Publication number: 20080145698Abstract: The invention relates to the improvement of organic electroluminescent devices, especially blue-emitting devices, by using compounds of formula (1) as dopants in the emitting layer.Type: ApplicationFiled: June 22, 2005Publication date: June 19, 2008Applicant: Merck Patent GmbHInventors: Holger Heil, Philipp Stossel, Horst Vestweber
-
Publication number: 20080033177Abstract: The present invention is directed to a process for the synthesis of substituted-1,2,3,4-tetrahydroisoquinoline derivatives, useful as intermediates in the synthesis of pharmaceutical agents.Type: ApplicationFiled: August 7, 2007Publication date: February 7, 2008Inventors: Frank J. Villani, Hua Zhong
-
Publication number: 20070293534Abstract: A process for preparing the [R-[R*,R*-(E)]]-2,2?-(1,8-dioxo-4-octene-1,8-diyl) bis(oxy-3,1-propanediyl)bis(1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-[(3,4,5-trimethoxyphenyl) methyl]isoquinolinium) dichloride, commonly known as mivacurium chloride, useful as short-duration neuromuscular blocking agent.Type: ApplicationFiled: June 19, 2007Publication date: December 20, 2007Inventors: Maurizio Francesco Velati, Andrea Busca, Cristina Manfrotto, Marco Nicolini, Claudio Gianluca Pozzoli
-
Publication number: 20070213335Abstract: The invention described herein relates to certain bicyclic heteroaromatic N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.Type: ApplicationFiled: March 6, 2007Publication date: September 13, 2007Inventors: Duke M. FITCH, Mariela Colon
-
Patent number: 7268142Abstract: The invention pertains to substituted quinazoline and isoquinoline compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE-10. The invention also relates to intermediates for preparation of said compounds; pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.Type: GrantFiled: February 18, 2005Date of Patent: September 11, 2007Assignee: Pfizer Inc.Inventors: Martin Patrick Allen, Thomas Allen Chappie, John Michael Humphrey, Spiros Liras, William Michael Whalen
-
Patent number: 7166617Abstract: Novel compounds represented by the following formula (I) that act as a ligand to sigma receptor/binding cite and a medicament comprising the same as an active ingredient: wherein X represents an alkyl group, an aryl group, a heterocyclic group or the like; Q represents a group represented by —CH2—, —CO—, —O—, —CH(OR7)— or the like wherein R7 represents a hydrogen atom, an alkyl group or the like; n represents an integer of from 0 to 5; R1 and R2 each represent a hydrogen atom, an alkyl group or the like; B represents either of the following groups: wherein R3, R4, R5, and R6 each represent a hydrogen atom, a halogen atom, an alkoxyl group or the like; m represents 1 or 2; and the ring of: represents an aromatic heterocyclic ring.Type: GrantFiled: February 26, 2001Date of Patent: January 23, 2007Assignee: Mitsubishi Pharma CorporationInventors: Haruko Yamabe, Masahiro Okuyama, Akira Nakao, Mitsuru Ooizumi, Ken-ichi Saito
-
Patent number: 7157463Abstract: The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunctionType: GrantFiled: January 23, 2002Date of Patent: January 2, 2007Assignee: Eli Lilly and CompanyInventors: Ryan Thomas Backer, Karin Briner, Christopher William Doecke, Matthew Joseph Fisher, Steven Lee Kuklish, Vincent Mancuso, Michael John Martinelli, Jeffrey Thomas Mullaney, Chaoyu Xie
-
Publication number: 20040230055Abstract: Substituted alkylmetal reagents such as (trimethylsilylmethyl)lithium are reacted with azaaromatic compounds and/or nitrogen heterocycle compounds to produce functionalized azaaromatic compounds and functionalized nitrogen heterocycle compounds.Type: ApplicationFiled: April 6, 2004Publication date: November 18, 2004Inventors: Christopher J. Woltermann, Douglas E. Sutton
-
Patent number: 6800645Abstract: This invention is directed to physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring is an azaheterocycle, and the ring represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; R1 represents hydrogen or a straight- or branched-chain alkyl group of 1 to about 4 carbon atoms, optionally substituted by hydroxy or one or more halogen atoms, or when Z1 represents a direct bond R1 may also represent a lower alkenyl or lower alkynyl group, or a formyl group; R2 represents hydrogen, alkenyl, alkoxy, alkyl, alkylsulphinyl, alkylsulphonyl, alkylthio, aryl, arylalkyloxy, arylalkylsulphinyl, arylalkylsulphonyl, arylalkylthio, aryloxy, arylsulphinyl, arylsulphonyl, arylthio, cyano, cycloalkenyl, cycloalkenyloxy, cycloalkyl, cycloalkyloxy, heteroaryl, heteroarylalkyloxy, heteroaryloxy, hydroxy, —SO2NR4R5, —NR4SO2R5, —Type: GrantFiled: July 7, 2000Date of Patent: October 5, 2004Assignee: Aventis Pharma LimitedInventors: Paul Joseph Cox, Shelley Bower, David John Aldous, Peter Charles Astles, Daniel Gerard McGarry, Christopher Hulme, John Robinson Regan, Fu-Chih Huang, Stevan Wakefield Djuric, Kevin Joseph Moriarty, Rose Mappilakunnel Mathew, Gregory Bernard Poli