Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 546/224)
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Patent number: 8404693Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: GrantFiled: January 17, 2011Date of Patent: March 26, 2013Assignee: Adolor CorporationInventors: Roland E. Dolle, Bertrand Le Bourdonnec
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Patent number: 8399677Abstract: The invention provides a method for the preparation of fentanyl comprising: (a) reacting 4-piperidone hydrochloride monohydrate with aniline in presence of reducing environment to produce 4-anilinopiperidine (4-AP), (b) reacting the 4-AP as obtained from step (a) with phenethyl halide under reflux conditions in highly alkaline medium to give 4-anilino-N-phenethylpiperidine, and (c) converting the 4-anilino-N-phenethylpiperidine to fentanyl by reacting with propionyl chloride in presence of halogenated hydrocarbons, then isolating fentanyl by solvent extraction and purifying by crystallization from petroleum ether at a temperature ranging from 60-80° C.Type: GrantFiled: March 9, 2009Date of Patent: March 19, 2013Assignee: Defence Research & Development OrganisationInventors: Pradeep Kumar Gupta, Laxmi Manral, Kumaran Ganesan, Ramesh Chandra Malhotra, Krishnamurthy Sekhar
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Publication number: 20130065756Abstract: Compounds of the formula I wherein the substituents are as defined in claim 1, are useful as a pesticides.Type: ApplicationFiled: November 22, 2010Publication date: March 14, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
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Publication number: 20130053392Abstract: A carbonic anhydrase IX (CA IX) inhibitor which comprises a compound of general formula: R—NH—CX—NH—(CH2)n—Ar-Q-SO2—NH2 or a pharmaceutically-acceptable salt, derivative or prodrug thereof; wherein n=0, 1 or 2; Q is O or NH; X is O or S; and R comprises an organic substituent group.Type: ApplicationFiled: February 14, 2011Publication date: February 28, 2013Inventors: Peter Ebbesen, Claudlu T. Supuran, Andrea Scozzafava, Erik Olai Pettersen, Kaye Williams, Ludwig Dubois, Philippe Lambin
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Publication number: 20130030184Abstract: A radioisotope labeled reagent includes a compound having the general formula (I), L-(aCbH2)naCbH3??(I) where a in each occurrence independently is a carbon mass number between 11 and 14 inclusive, b in each occurrence independently is a hydrogen mass number between 1 and 3 inclusive, such that a in each occurrence is not 12 simultaneously with b in each occurrence being 1; L is a leaving group R1SO2—O—, R1—S—, 12C1H3(12C3H2)n—S—R1C(O)O—, NC—, (R1)3P—, XMg—and Li—, where n is an integer between 0 and 3 inclusive, where X is chloro, bromo or iodine, where R1 is H, aryl, a substituent containing aryl, C1-C20 alkyl, a substituent containing C1-C20 alkyl, C2-C20 alkenyl, a substitute containing C2-C20 alkenyl, C2-C20 alkynyl, and a substitute containing C2-C20 alkynyl with the proviso that when n is 0, a is 13 and b is 2 and R1 in R1—S is not aryl.Type: ApplicationFiled: October 4, 2012Publication date: January 31, 2013Applicant: PERKINELMER HEALTH SCIENCES, INC.Inventor: PerkinElmer Health Sciences, Inc.
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Publication number: 20120329649Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.Type: ApplicationFiled: June 21, 2012Publication date: December 27, 2012Inventors: James E. Hunter, William C. Lo, Gerald B. Watson, Akshay Patny, Gary D. Gustafson, Dan Pernich, William K. Brewster, Debra L. Camper, Beth Lorsbach, Michael R. Loso, Thomas C. Sparks, Hemant Joshi, Adiraj Mandaleswaran, Ramadevi Sanam, Rambabu Gundla, Pravin S. Iyer
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Publication number: 20120322761Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.Type: ApplicationFiled: August 29, 2012Publication date: December 20, 2012Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
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Publication number: 20120316169Abstract: (R,S) 2-aryl-propionamide derivatives, or their single enantiomers (R) and (S) are disclosed useful in the treatment or prevention of symptoms and disorders such as pain and inflammation associated with the bradykinin B1 pathway.Type: ApplicationFiled: October 28, 2010Publication date: December 13, 2012Applicant: DOMPÉ S.P.A.Inventors: Andrea Beccari, Andrea Aramini, Gianluca Bianchini, Alessio Moriconi
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Publication number: 20120302539Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.Type: ApplicationFiled: May 7, 2012Publication date: November 29, 2012Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas Macdonald, John Wityak
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Patent number: 8299258Abstract: The present invention relates to a process for the preparation of piperidine derivatives including sufentanil, and their pharmaceutically acceptable salts, such as the citrate salt in which a quaternary ammonium (nosylate) salt of an appropriate piperidine is reacted with a corresponding 4-NO2 sulfonate ester to produce the desired piperidine derivative at a high purity.Type: GrantFiled: November 4, 2009Date of Patent: October 30, 2012Assignee: Cambrex Charles CityInventors: Greg S. Buenger, Paul A. Jass, Kezia Peixoto Schutz
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Patent number: 8288368Abstract: (R)-2-Arylpropionamide compounds of formula (I) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The 2-Arylpropionamides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear leukocytes (leukocytes PMN) and of monocytes at the inflammatory sites. In particular, the invention relates to the R enantiomers of omega-aminoalkylamides of 2-aryl propionic acids, of formula (I), for use in the inhibition of the chemotaxis of neutrophils and monocytes induced by the C5a fraction of the complement and by other chemotactic proteins whose biological activity is associated with activation of a 7-TD receptor. Selected compounds of formula (I) are dual inhibitors of both the C5a-induced chemotaxis of neutrophils and monocytes and the IL-8-induced chemotaxis of PMN leukocytes.Type: GrantFiled: February 25, 2002Date of Patent: October 16, 2012Assignee: Dompé Pha.R.Ma S.p.A.Inventors: Marcello Allegretti, Riccardo Bertini, Valerio Berdini, Cinzia Bizzarri, Maria Candida Cesta, Vito Di Cioccio, Gianfranco Caselli, Fracesco Colotta, Carmelo Gandolfi, Janete Peloia Barroso Gandolfi, legal representative, Giulio Agostino Gandolfi, legal representative, Maria Carla Gandolfi, legal representative, Arrigo Aldo Gandolfi, legal representative
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Publication number: 20120238452Abstract: Compounds of the formula (I), wherein the substituents are as defined in claim 1, are useful as a pesticides.Type: ApplicationFiled: November 29, 2010Publication date: September 20, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
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Publication number: 20120220629Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor.Type: ApplicationFiled: February 24, 2012Publication date: August 30, 2012Inventors: Silvina GARCIA RUBIO, Claudio Pietra, Claudio Giuliano, Zhigang Li
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Publication number: 20120184581Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.Type: ApplicationFiled: July 21, 2010Publication date: July 19, 2012Applicant: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Timothy A. Riley
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Publication number: 20120178741Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: March 21, 2012Publication date: July 12, 2012Applicant: JANSSEN PHARMACEUTICA N.V.Inventors: Kristof Van Emelen, Leo Jacobus Jozel Backx, Sven Franciscus Anna Van Brandt, Patrick René Angibaud, Isabelle Noélle Constance Pilatte, Marc Gustaaf Celine Verdonck, Hans Louis Jos De Winter, Jimmy Arnold Viviane Van heusden
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Publication number: 20120172387Abstract: The present invention relates to an opioid controlled release oral dosage form comprising at least one opioid for the manufacture of a medicament to treat patients with restless leg syndrome (RLS).Type: ApplicationFiled: December 21, 2011Publication date: July 5, 2012Applicant: Euro-Celtique S.A.Inventors: Wolfgang FLEISCHER, Karen REIMER, Karin GAWORA
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Patent number: 8207373Abstract: HPV inhibitors with formula (I) where G1 represents a hydrocarbonated bond or chain possibly substituted by one or two alkyl groups, G2 represents a group (see formula Ia+Ib) or R represents a hydrogen, an alkyl, halogenoalkyl, or a prodrug radical such as carbamate, acetyl or dialkylaminomethyl, G represents a bond or a hydrocarbonated chain possibly substituted by one or two alkyls, W represents an oxygen or sulphur, R1 and R2 each represent a group chosen from among hydrogen, halogen, hydroxyl, thio, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, amino, monoalkylamino, dialkylamino, cycloalkyl, alkyl or halogenoalkyl, R3 represents an acid or a prodrug radical of the acid function or a bioisostere of the acid function, A represents an aryl, cycloalkyl, cycloalkenyl or a heterocycle, each possibly substituted, and B represents an aryl or a heterocycle with 6 chains, each possibly substituted, and pharmaceutically acceptable salts.Type: GrantFiled: May 18, 2007Date of Patent: June 26, 2012Assignee: Anaconda PharmaInventors: Marta Blumenfeld, Delphine Compere, Jean-Michel Gauthier
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Publication number: 20120122784Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating substituted cyclopentylene compounds represented in formula I and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.Type: ApplicationFiled: May 26, 2010Publication date: May 17, 2012Applicant: LEO PHARMA A/SInventors: Bjarne Nørremark, Lars Kristian Albert Blæhr, Anne Eeg Knapp, Kristoffer Månsson
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Publication number: 20120115907Abstract: The present invention relates to novel renin inhibitors of general formula (1), novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (1), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.Type: ApplicationFiled: April 22, 2010Publication date: May 10, 2012Applicant: CADILA HEALTHCARE LIMITEDInventors: Pravain Thombare, Jigar Desai, Mukul R. Jain
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Publication number: 20120094989Abstract: The present invention relates to compounds having 5-hydroxytryptamine receptor modulating activity, in particular compounds having an acidic moiety held distant from the 5-HT pharmacophore by a rigid linker group, to compositions containing such compounds and methods of treatment using them. Such compounds have an increased affinity for the 5-HT receptor and a reduced hERG effect. Certain compounds of the invention further exhibit an angiotensin II receptor modulating activity. Claimed are compounds of formula (I): HT-L-A. HT is a 5-HT receptor modulating moiety containing a basic nitrogen atom; A is an acid moiety; L is a linker moiety.Type: ApplicationFiled: April 1, 2010Publication date: April 19, 2012Applicant: SERODUS ASInventors: Jo Klaveness, Bjame Brudeli, Finn Olav Levy, Lise Roman Moltzau, Trygve Gulbrandsen
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Patent number: 8148405Abstract: The invention provides N-{2-[((2S)-3-{[1-(4-chlorobenzyl)piperidin-4-yl]amino}-2-hydroxy-2-methylpropyl)oxy]-4-hydroxyphenyl}acetamide benzoate or a solvate thereof, pharmaceutical compositions containing the salt or solvate and use of the salt or solvate in therapy.Type: GrantFiled: July 31, 2006Date of Patent: April 3, 2012Assignee: AstraZeneca ABInventors: Julien Giovannini, Bo-Goran Josefsson
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Patent number: 8129376Abstract: The present invention relates to piperidine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: GrantFiled: March 20, 2009Date of Patent: March 6, 2012Inventors: Kumar Sundaresan, P. Bala Koteswara Rao, Bharathiraja Ainan, Hariharasubramanian Ayyamperumal, Girish A R, Srinivas Tatiparthy, Ganesh Prabhu, Hosahalli Subramanya, Alexander Bischoff
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Patent number: 8110574Abstract: A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.Type: GrantFiled: November 15, 2010Date of Patent: February 7, 2012Assignee: Ipsen Pharma S.A.S.Inventors: Christophe Thurieau, Jérôme Gonzalez, Christophe Moinet
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Publication number: 20120022100Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: ApplicationFiled: September 28, 2011Publication date: January 26, 2012Inventors: Juergen Klaus Maibaum, Daniel K. Baeschlin, Holger Sellner
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Publication number: 20120004413Abstract: A radioisotope labeled reagent includes a compound having the general formula (I), L-(aCbH2)naC5bH3??(I) where a in each occurrence independently is a carbon mass number between 11 and 14 inclusive, b in each occurrence independently is a hydrogen mass number between 1 and 3 inclusive, such that a in each occurrence is not 12 simultaneously with b in each occurrence being 1; L is a leaving group R1SO2—O—, R1—S—, 12C1H3(12C1H2)n—S—R1C(O)O—, NC—, (R1)3P—, XMg— and Li—, where n is an integer between 0 and 3 inclusive, where X is chloro, bromo or iodine, where R1 is H, aryl, a substituent containing aryl, C1-C20 alkyl, a substituent containing C1-C20 alkyl, C2-C20 alkenyl, a substituent containing C2-C20 alkenyl, C2-C20 alkynyl, and a substitute containing C2-C20 alkynyl with the proviso that when n is 0, a is 13 and b is 2 and R1 in R1—S is not aryl.Type: ApplicationFiled: September 13, 2011Publication date: January 5, 2012Applicant: PerkinElmer Health Sciences, Inc.Inventor: Jerry Scot Pounds
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Publication number: 20110294775Abstract: Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumour pain and headache diseases.Type: ApplicationFiled: August 12, 2008Publication date: December 1, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
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Publication number: 20110269747Abstract: Polyarylcarboxamide compounds of formula (I) are useful as lipid lowering agents.Type: ApplicationFiled: July 13, 2011Publication date: November 3, 2011Inventors: Lieven Meerpoel, Peter Walter Maria Roevens, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken, Marcel Viellevoye
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Publication number: 20110270011Abstract: The use of opioids or opioid mimetics is suggested for the manufacture of a medicament for the treatment of resistant cancer patients.Type: ApplicationFiled: January 29, 2009Publication date: November 3, 2011Applicant: Universität UlmInventors: Erich Miltner, Claudia Friesen, Andreas Alt
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Publication number: 20110263628Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: ApplicationFiled: June 8, 2011Publication date: October 27, 2011Applicant: APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.Inventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Publication number: 20110230487Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: March 17, 2011Publication date: September 22, 2011Inventors: Tai Wei LY, Garrett Thomas Potter, Jared Andrew Forrester
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Publication number: 20110230351Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or fungicides. Moreover, the invention relates to selectively herbicidal compositions comprising, firstly, the spiroheterocyclically substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising in particular spiroheterocyclically substituted tetramic acid derivatives through the addition of ammonium or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or acaricides and/or fungicides and/or for preventing unwanted vegetation.Type: ApplicationFiled: February 10, 2011Publication date: September 22, 2011Applicant: BAYER CROPSCIENCE AGInventors: Reiner FISCHER, Arnd Voerste, Isolde Häuser-Hahn, Stefan Lehr, Elmar Gatzweiler, Ulrich Görgens, Ines Heinemann
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Publication number: 20110224079Abstract: Novel compounds of the formula (I), wherein the substituents are as defined in claim 1; compositions containing them and their use as insecticides, acaricides, nematicides or molluscicides.Type: ApplicationFiled: November 30, 2009Publication date: September 15, 2011Applicant: SYNGENTA CROP PROTECTION LLCInventors: Michel Muehlebach, Thomas Pitterna, Andre Jeanguenat, Myriem El Qacemi, Roger Graham Hall, Andrew Edmunds, Camilla Corsi, Andre Stoller, Christopher Richard Godfrey, Jurgen Harry Schaetzer, Olivier Loiseleur, Peter Maienfisch, Jerome Yves Cassayre
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Publication number: 20110214590Abstract: The present invention relates to the use of sterically hindered amines comprising one or more groups of the general formula (I) to stabilize inanimate organic material, more particularly plastics or coating materials, where R1 and R2 each independently, alike or different, are H, C1-C20 alkyl, C3-C15 cycloalkyl, aryl, hetaryl or a heterocycle, R4, R5, R6, and R7 each independently, alike or different, are C1-C20 alkyl, or R4 and R6 or R5 and R7 together are a tetramethylene or pentamethylene group, and R3 is aryl or hetaryl. The invention further relates to methods of stabilizing inanimate organic material, especially plastics or coating materials. Additionally provided by the invention are selected sterically hindered amines comprising one or more groups of the general formula (I). Additionally provided by the invention are materials that comprise selected sterically hindered amines.Type: ApplicationFiled: August 14, 2009Publication date: September 8, 2011Applicant: BASF SEInventors: Alban Glaser, Sylke Haremza, Simon Schambony
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Publication number: 20110184179Abstract: Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2-methylpropyloxy)-phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and methods for obtaining the salt. Further disclosed are various crystalline forms of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and its hemi-tartrate salt including various polymorphs and solvates.Type: ApplicationFiled: April 6, 2011Publication date: July 28, 2011Inventors: Mikkel Boas THYGESEN, Nathalie Schlienger, Bo-Ragnar Tolf, Carl-Magnus A. Andersson, Fritz Blatter, Jörg Berghausen
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Publication number: 20110178060Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like.Type: ApplicationFiled: September 18, 2009Publication date: July 21, 2011Inventors: Junya Shirai, Hideyuki Sugiyama, Taku Kamei, Hironobu Maezaki
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Publication number: 20110152520Abstract: A compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof: (wherein each symbol is as defined in the description.) The compounds represented by formula (I) has the antagonistic activity against CCR5, so they are useful in preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, inflammatory bowel disease such as ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation (rejection of graft of solid organ, rejection of graft of pancreatic islet cells in therapy for diabetes, graft-versus-host disease, etc.), immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (infection with human immunodeficiency virus, acquired immunodeficiency syndrome, infection with RSV, etc.Type: ApplicationFiled: January 28, 2011Publication date: June 23, 2011Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Yoshikazu TAKAOKA, Shiro SHIBAYAMA, Rena NISHIZAWA
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Publication number: 20110144346Abstract: The invention relates to a method for producing N-phenyl-N-(4-piperidinyl)amide salts, particularly pharmaceutically tolerable addition salts of the compound Remifentanil, in that a compound of the formula (III) is reacted with an acrylic acid alkyl ester of the formula CH2?CH—C(O)—OR: where independently of each other R denotes low-molecular alkyl, preferably (C1-4)alkyl, preferably methyl or ethyl, R1 denotes low-molecular alkyl, preferably (C1-4)alkyl, preferably methyl or ethyl; and HX denotes an inorganic or organic acid, wherein the components are optionally reacted in the presence of a catalyst, preferably at a higher temperature, thereby obtaining the salt of the compound of formula (I).Type: ApplicationFiled: July 3, 2008Publication date: June 16, 2011Applicant: CILAG AGInventors: Oliver Flogel, Ulrich Weigl
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Publication number: 20110117591Abstract: Chemical stain compounds containing a fluorophore and a reducible quenching unit are disclosed. The reducible quenching unit quenches the fluorophore while in its oxidized state. Upon reduction, the quenching properties of the quenching unit are diminished or eliminated. The chemical compounds can be used in a variety of applications, including the detection of bacterial cells, monitoring the electron transport chain function of bacterial cells, monitoring the oxidation state of non-biological systems, and assaying the effectiveness of antibacterial or antimicrobial agents.Type: ApplicationFiled: October 20, 2010Publication date: May 19, 2011Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Ching-Ying CHEUNG, Diane R. Gray, Stephen T. Yue
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Publication number: 20110112062Abstract: This invention relates to novel compounds of the Formula I, II, III, IHa, NIb, IV, IVa, IVb, IVc, IVd, IVe, V, Va, Vb1 V1, V1a, VIb, VII, Vi1a, VIIb, VIII, V111a, VIIIb, IX, IXa, X, and Xa, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.Type: ApplicationFiled: April 21, 2009Publication date: May 12, 2011Inventors: David A. Claremon, Linghang Zhuang, Yuanjie Ye, Suresh B. Singh, Colin M. Tice
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Publication number: 20110098281Abstract: The invention relates to pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula I: and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1, R2, Z and m are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: April 8, 2008Publication date: April 28, 2011Applicant: Purdue Pharma L.P.Inventors: Donald J. Kyle, Jiangchao Yao
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Publication number: 20110098322Abstract: The present invention provides compounds that can inhibit the activity of soluble epoxide hydrolases. In particular, the present invention provides compounds of Formula I.Type: ApplicationFiled: August 5, 2008Publication date: April 28, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: James R. Sanborn, Bruce D. Hammock, Sung Hee Hwang, Paul D. Jones, Christophe Morisseau
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Publication number: 20110059971Abstract: A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.Type: ApplicationFiled: November 15, 2010Publication date: March 10, 2011Applicant: IPSEN S.A.S.Inventors: Christophe THURIEAU, Jérôme Gonzalez, Christophe Moinet
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Publication number: 20110046180Abstract: This invention relates to novel N-aryl-N-piperidin-4-yl-propionamide derivatives useful as opioid receptor ligands. In other aspects the invention relates to the use of these compounds in a method for therapy, such as for the treatment of pain, and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: December 18, 2008Publication date: February 24, 2011Applicant: NeuroSearch A/SInventors: Dan Peters, Birgitte L. Eriksen, Gordon Munro, Elsebet Østergaard Nielsen
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Publication number: 20110034511Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable acid addition salt thereof, wherein X is C(R3c)? or N?; R1 is C2-C6 alkyl, substituted C2-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 n-alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II provided that when R1 is C2-C6 alkyl or substituted C2-C6 alkyl, R2 is hydrogen or methyl; R3a, R3b and, when X is —C(R3c)?, R3c, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R3a, R3b, and R3c may be other than hydrogen; R4 is hydrogen or C1-C3 alkyl; R5 is hydrogen, C1-C3 alkyl, or C3-C6 cycloalkylcarbonyl, provided that when R3a is other than hydrogen, R5 is hydrogen; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively.Type: ApplicationFiled: September 28, 2010Publication date: February 10, 2011Applicant: Eli Lilly and CompanyInventors: Maria-Jesus Blanco-Pillado, Michael Philip Cohen, Sandra Ann Filla, Kevin John Hudziak, Daniel Timothy Kohlman, Dana Rae Benesh, Frantz Victor, Yao-Chang Xu, Bai-Ping Ying, DeAnna Piatt Zacherl, Deyi Zhang, Brian Michael Mathes
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Patent number: 7884102Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: GrantFiled: April 28, 2008Date of Patent: February 8, 2011Assignee: Adolor CorporationInventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
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Publication number: 20110021781Abstract: The invention provides a method for the preparation of fentanyl comprising: (a) reacting 4-piperidone hydrochloride (NPP) with aniline in presence of reducing environment to produce 4-anilinopiperidine (4-ANPP), (b) reacting the 4-ANPP as obtained from step (a) with phenethyl halide under reflux conditions in highly alkaline medium to give 4-anilino-N-phenethylpiperidine, and (c) converting the 4-anilino-N-phenethylpiperidine to fentanyl by reacting with propionyl chloride in presence of halogenated hydrocarbons, then isolating fentanyl by solvent extraction and purifying by crystallization from petroleum ether at a temperature ranging from 60-80° C.Type: ApplicationFiled: March 9, 2009Publication date: January 27, 2011Applicant: Director General Defence Research & Development Organization, Ministry of DefenceInventors: Pradeep Kumar Gupta, Laxmi Manral, Kumaran Ganesan, Ramesh Chandra Malhotra, Krishnamurthy Sekhar
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Publication number: 20110015174Abstract: A CPT1 inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 1, 2008Publication date: January 20, 2011Applicant: University Health NetworkInventors: Heinz W. Pauls, Bryan T. Forrest, Peter Brent Sampson, Yong Liu, Radoslaw Laufer, Yunhui Lang, Miklos Feher, Yi Yao, Guohua Pan
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Publication number: 20110009449Abstract: This invention relates to N-aryl-N-piperidin-4-yl-propionamide derivatives for use as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy, such as for the treatment of pain, and to pharmaceutical compositions comprising the compounds, and to novel compounds.Type: ApplicationFiled: December 18, 2008Publication date: January 13, 2011Inventors: Dan Peters, Birgitte L. Eriksen, Gordon Munro, Elsebet Østergaard Nielsen
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Patent number: 7868176Abstract: Disclosed herein are salts of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2-methylpropyloxy) phenylmethyl)carbamide including the citrate, fumarate, maleate, malate, phosphate, succinate, sulphate, and edisylate salts.Type: GrantFiled: September 26, 2005Date of Patent: January 11, 2011Assignee: ACADIA Pharmaceuticals, Inc.Inventors: Mikkel Boas Thygesen, Nathalie Schlienger, Bo-Ragnar Tolf, Fritz Blatter, Jörg Berghausen
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Patent number: RE42412Abstract: The subject invention provides novel compounds and compositions for the safe and effective treatment of gastroesophageal reflux and related conditions. In a preferred embodiment, the compositions of the subject invention comprise esterified cisapride derivatives. These compositions possess potent activity in treating gastroesophageal reflux disease and substantially reduce adverse effects associated with the administration of cisapride. These adverse effects include, but are not limited to, diarrhea, abdominal cramping and elevations of blood pressure and heart rate.Type: GrantFiled: December 21, 2007Date of Patent: May 31, 2011Assignee: ARYx Therapeutics, Inc.Inventors: Pascal Druzgala, Peter G. Milner, Jurg Pfister, Cyrus Becker