Oxygen Attched Directly Or Indirectly To Morpholine Ring By Nonionic Bonding Patents (Class 544/170)
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Patent number: 12013637Abstract: An oxime ester compound is useful as a photopolymerization initiator used in a polymerizable composition. A photopolymerization initiator contains the oxime ester compound. The oxime ester compound contains, in the same molecule: a group represented by the following Formula (I); and a photoradical cleavable group containing no oxime ester group.Type: GrantFiled: June 27, 2019Date of Patent: June 18, 2024Assignee: ADEKA CORPORATIONInventors: Yoshitomo Takeuchi, Taiki Mihara, Naomi Sato, Kazushi Matsukawa
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Patent number: 10758465Abstract: Disclosed herein are compositions of synephrine and a penetration enhancer and methods of reducing hair loss from pulling by applying the compositions. In one embodiment, the composition is a prewash composition comprising water, synephrine, and PEG-6 caprylic/capric glycerides.Type: GrantFiled: July 16, 2018Date of Patent: September 1, 2020Assignee: Follea InternationalInventors: John McCoy, Ofer A. Goren
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Publication number: 20150133431Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives, pharmaceutical compositions comprising GGA derivatives and the use of GGA derivatives.Type: ApplicationFiled: July 10, 2014Publication date: May 14, 2015Applicant: COYOTE PHARMACEUTICALS, INC.Inventor: Gary C. Look
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Publication number: 20150057443Abstract: Cycloalkyl amine compounds of Formula (I), wherein ring A is C3-C6 cycloalkyl, optionally substituted with one or more C1-C3 alkyl, and R5 is ORS2, in which RS2 is H or C1-C6 alkyl, or R5 and R6, together with the carbon atom to which they are attached, form C?O, for use in treating CNS disorders, including movement disorders, depressive disorders, sleep disorders, cognitive dysfunctions, obesity, sexual dysfunction and substance abuse.Type: ApplicationFiled: August 21, 2014Publication date: February 26, 2015Inventors: Philip Huxley, Jonathan R. Heal, Richard S. Todd
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Patent number: 8906908Abstract: The invention provides hydroxybupropion analogues capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and/or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity.Type: GrantFiled: November 19, 2012Date of Patent: December 9, 2014Assignees: Research Triangle Institute, Dignity Health, Virginia Commonwealth UniversityInventors: F. Ivy Carroll, Bruce E. Blough, Hernan A. Navarro, S. Wayne Mascarella, Ana Zamfira Muresan, M. Imad Damaj, Ronald J. Lukas
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Patent number: 8877971Abstract: The present invention relates to a method for preparing formamide compounds using carbon dioxide, and to the use of said method for manufacturing vitamins, pharmaceutical products, adhesives, acrylic fibers, synthetic leathers, pesticides and fertilizers. The invention also relates to a method for manufacturing vitamins, pharmaceutical products, adhesives, acrylic fibers, synthetic leathers, pesticides and fertilizers which includes a step of preparing formamide compounds by the method according to the invention.Type: GrantFiled: April 4, 2012Date of Patent: November 4, 2014Assignee: Commissariat a l'Energie Atomique et aux Energies AlternativesInventors: Thibault Cantat, Christophe Gomes, Olivier Jacquet
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Publication number: 20140187554Abstract: The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as ROR?, ROR?, or ROR?. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.Type: ApplicationFiled: May 16, 2012Publication date: July 3, 2014Applicant: The Scripps Research InstituteInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Youseung Shin, Yuanjun He, Anne-Laure Blayo, Brent R. Lyda, Marcel Koenig, Naresh Kumar, Thomas Burris
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Patent number: 8648190Abstract: The invention relates to a production method of a 2-hydroxymethylmorpholine salt, which includes crystallization from a solution containing 2-hydroxymethylmorpholine of formula (1) 1,4-oxazepane compound of formula (2) and an acid.Type: GrantFiled: January 15, 2010Date of Patent: February 11, 2014Assignee: Daiso Co., Ltd.Inventors: Yoshifumi Nagano, Keisuke Yaegashi, Shingo Iwashina
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Patent number: 8460851Abstract: A salt represented by the formula (I): wherein Q1 and Q2 each independently represent a fluorine atom or a C1-C6 perfluoroalkyl group, L1 represents *—CO—O-La- or *—CH2—O-Lb-, * represents a binding position to —C(Q1)(Q2)-, La and Lb independently represent a C1-C15 divalent saturated hydrocarbon group in which one or more —CH2— can be replaced by —O— or —CO—, ring W1 represents a C2-C36 nitrogen-containing heterocyclic group in which one or more —CH2— can be replaced by —O—, and Z1? represents an organic counter ion.Type: GrantFiled: January 6, 2011Date of Patent: June 11, 2013Assignee: Sumitomo Chemical Company, LimitedInventors: Satoshi Yamaguchi, Koji Ichikawa
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Patent number: 8338439Abstract: The present invention provides 2,4-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same. In some embodiments, the present invention provides a compound of formula I-a or I-b: wherein each of Ring A, Ring B, W1, W2, Ry, Rv, Rx, m, p, and R1 is described herein.Type: GrantFiled: December 29, 2009Date of Patent: December 25, 2012Assignee: Celgene Avilomics Research, Inc.Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
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Patent number: 8217063Abstract: The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: GrantFiled: March 15, 2008Date of Patent: July 10, 2012Assignee: Bayer Intellectual Property GmbHInventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Dieter Lang
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Patent number: 8143201Abstract: Morpholine derivatives useful as ashless TBN sources for lubricating oil compositions that are compatible with fluoroelastomeric engine seal materials, and lubricating oil compositions containing such compounds.Type: GrantFiled: March 9, 2010Date of Patent: March 27, 2012Assignee: Infineum International LimitedInventors: Jacob Emert, Jie Cheng, Jun Hua, Tushar K. Bera, Mark L. Bushey, Jesse D. Dambacher
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Publication number: 20120035175Abstract: The present invention relates to a salt selected from the group comprising the N-methyl-D-glucamine salt (NMG), the diethylamine salt (DEA) salt, the magnesium salt, the tromethamine salt, the choline salt, the L-arginine salt, the zinc salt, and the 4-(2-hydroxyethyl)morpholine (HEM) salt of compounds of the general formula (I) wherein X is selected from the group consisting of CH2, S, or O; D is O or S; R8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1; and q is 0 or 1; with the proviso that compounds wherein X?CH2, q=0, Y=unsubstituted phenyl and E=unsubstituted phenylene are excluded; or a hydrate thereof.Type: ApplicationFiled: July 1, 2011Publication date: February 9, 2012Applicant: 4SC AGInventors: Aldo AMMENDOLA, Julia DIEDERICHS, Johann LEBAN, Daniel VITT
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Publication number: 20120016120Abstract: The invention relates to a production method of a 2-hydroxymethylmorpholine salt, which includes crystallization from a solution containing 2-hydroxymethylmorpholine of formula (1) 1,4-oxazepane compound of formula (2) and an acid.Type: ApplicationFiled: January 15, 2010Publication date: January 19, 2012Applicant: DAISO CO., LTD.Inventors: Yoshifumi Nagano, Keisuke Yaegashi, Shingo Iwashina
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Publication number: 20110251198Abstract: Provided here are methods of manufacture of viloxazine and its various salts, as well as viloxazine-related compounds, such as novel intermediate reaction products and polymorphs thereof. In particular, the methods provide a substantially pure API of viloxazine HCl while avoiding undesirable impurities. The methods further provide for separating, identifying, and characterizing novel polymorphs of viloxazine. Further provided are methods for synthesis and identification and characterization of novel intermediates of viloxazine, as well as for some important metabolites and precursors of metabolites of viloxazine.Type: ApplicationFiled: April 12, 2011Publication date: October 13, 2011Applicant: Supernus Pharmaceuticals Inc.Inventors: Likan Liang, Padmanabh P. Bhatt, David Dain, Jean-Philippe Taquet, Aleksandr Pechenov, Alexei Tchesnokov, Reynold Mariaux
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Publication number: 20110172417Abstract: This invention relates to a heterogeneous copper nanocatalyst composed of copper nanoparticles immobilized on a boehmite support, a method of preparing the same, and the use thereof. The copper nanocatalyst composed of the copper nanoparticles supported on boehmite exhibits excellent performance in a Huisgen cycloaddition reaction and an A3 coupling reaction of aldehyde, amine and alkyne. The copper nanocatalyst is able to be prepared in a large scale and shows superior reactivity even when used in a small amount under mild conditions without an additive in an organic reaction. This heterogeneous catalyst is easy to separate and reuse after the reaction.Type: ApplicationFiled: July 9, 2008Publication date: July 14, 2011Applicant: Postech Academy-Industry FoundationInventors: Jai Wook Park, In Soo Park
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Patent number: 7910078Abstract: The present invention relates to a method for removing carbon dioxide (CO2) from a gas stream. Particularly, the present invention relates to a method for removing CO2 from a gas stream by a liquid absorbent having an amino alcohol derived from 4-amino-2-butanol. In comparison to conventional amines, the amino alcohols of the present invention have been found to provide a higher CO2 absorption capacity and a higher cyclic capacity for CO2 removal.Type: GrantFiled: August 23, 2007Date of Patent: March 22, 2011Assignee: University of ReginaInventors: Paitoon Tontiwachwuthikul, Andrew G. H. Wee, Raphael Idem, Kreangkrai Maneeintr, Gao-jun Fan, Amornvadee Veawab, Amr Henni, Adisorn Aroonwilas, Amit Chakma
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Patent number: 7902357Abstract: A process for the preparation of delmopinol (3-(4-propylheptyl)-4-morpholinethanol) or a derivative or a pharmaceutically acceptable salt, or a solvate thereof, including an hydrate, comprises reacting oxazolidin [2, 3-c] morpholine and a grignard reagent, and optionally converting the delmopinol (or derivative) free base into a pharmaceutically acceptable salt. The oxazolidin [2, 3-c] morpholine and the grignard reagent are useful as intermediates in the production process.Type: GrantFiled: November 17, 2006Date of Patent: March 8, 2011Assignee: Sinclair Pharmaceuticals LimitedInventors: Juan Jose Artus Surroca, David Fernandez Bleda, Tommaso Iacoangeli, Jordi Lluis Tous
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Patent number: 7893258Abstract: It comprises a preparation process of delmopinol or a pharmaceutically acceptable salt and/or a solvate thereof, by submitting the compound of formula (II) where R1 and R2 are the same or different, independently selected from the group consisting of H, (C1-C6)-alkyl or, alternatively, R1 and R2 form, together with the carbon atom to which they are attached, a (C5-C6)-cycloalkyl radical; and R3 is a radical selected from the group consisting of CF3, (C1-C4)-alkyl, phenyl, and phenyl mono- or disubstituted by a radical selected from the group consisting of (C1-C4)-alkyl, halogen and nitro to a deprotection and cyclisation reaction. The process is useful to prepare delmopinol or its salts on an industrial scale. The compound of formula (II) is new and also forms part of the present invention, as well as its preparation process and other new intermediates of said preparation process.Type: GrantFiled: January 10, 2007Date of Patent: February 22, 2011Assignee: Sinclair Pharmaceuticals LimitedInventors: Alexander Comely, Llorenç Rafecas Jane, Nicolas Tesson, Antoni Riera Escale
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Patent number: 7847096Abstract: The invention relates to novel aminophenylmorpholinone derivates (I) in which S represents an optionally substituted morpholinone radical, to a process for their preparation and to their use.Type: GrantFiled: October 1, 2005Date of Patent: December 7, 2010Assignee: Saltigo GmbHInventors: Albrecht Marhold, Wolfgang Ebenbeck
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Publication number: 20100222579Abstract: A process for the preparation of delmopinol (3-(4-propylheptyl)-4-morpholinethanol) or a derivative or a pharmaceutically acceptable salt, or a solvate thereof, including a hydrate, comprises reacting oxazolidin [2,3-c] morpholine and a Grignard reagent, and optionally converting the delmopinol (or derivative) free base into a pharmaceutically acceptable salt. The oxazolidin [2,3-c] morpholine and the Grignard reagent are useful as intermediates in the production process.Type: ApplicationFiled: May 13, 2010Publication date: September 2, 2010Inventors: Juan Jose ARTUS SURROCA, David Fernandez Bleda, Tommaso Iacoangeli, Jordi Lluis Tous
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Publication number: 20100168422Abstract: Provided herein are compounds and methods useful for preparing hexahydrofuro[2,3-b]furan-3-ol. Hexahydrofuro[2,3-b]furan-3-ol can be efficiently synthesized in four steps from readily available starting materials.Type: ApplicationFiled: December 30, 2008Publication date: July 1, 2010Inventor: Weiping Chen
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Publication number: 20100137316Abstract: The present invention provides compounds of Formula I wherein R1, R2, R3, and n have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of conditions including urinary disorders, pain, premature ejaculation, ADHD and fibromyalgia. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.Type: ApplicationFiled: February 9, 2010Publication date: June 3, 2010Inventors: Paul Vincent Fish, Malcolm Christian MacKenny, Alan Stobie, Florian Wakenhut, Gavin Alistair Whitlock
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Publication number: 20100048550Abstract: The present invention relates to novel compounds of general formula (I) which are thyroid receptor ligands and are preferably selective for the thyroid hormone receptor beta(TR-Beta). Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them.Type: ApplicationFiled: October 15, 2007Publication date: February 25, 2010Inventors: Saurin Raval, Preeti Raval, Braj Lohray, Vidya Bhushan Lohray, Pankaj R. Patel
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Publication number: 20090264651Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.Type: ApplicationFiled: May 8, 2009Publication date: October 22, 2009Inventor: Thomas Daly
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Publication number: 20090238773Abstract: Use of a morpholino compound having the general formula (I) wherein R1 is a straight or branched alkyl group containing 8 to 16 carbon atoms at the 2- or 3-position of the morpholino ring, and R2 is a straight or branched alkyl group containing 2 to 10 carbon atoms, substituted with a hydroxy group except in the alpha-position, or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the prevention or treatment of halitosis.Type: ApplicationFiled: January 5, 2007Publication date: September 24, 2009Inventor: Rolf Valter Attstrom
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Patent number: 7585856Abstract: The present invention is generally drawn to novel isolated therapeutic agents, termed resolvins, generated from the interaction between a dietary omega-3 polyunsaturated fatty acid (PUFA) such as eicosapentaenoic acid (EPA) or docosahexaenoic acid (DHA), cyclooxygenase-II (COX-2) and an analgesic, such as aspirin (ASA). Surprisingly, careful isolation of compounds generated from the combination of components in an appropriate environment provide di- and tri-hydroxy EPA or DHA compounds having unique structural and physiological properties. The present invention therefore provides for many new useful therapeutic di- or tri-hydroxy derivatives of EPA or DHA (resolvins) that diminish, prevent, or eliminate inflammation or PMN migration, for example. The present invention also provides methods of use, methods of preparation, and packaged pharmaceuticals for use as medicaments for the compounds disclosed throughout the specification.Type: GrantFiled: August 12, 2003Date of Patent: September 8, 2009Assignee: The Brigham and Women's Hospital, Inc.Inventor: Charles N. Serhan
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Publication number: 20090137798Abstract: A process for the preparation of delmopinol (3-(4-propylheptyl)-4-morpholinethanol) or a derivative or a pharmaceutically acceptable salt, or a solvate thereof, including an hydrate, comprises reacting oxazolidin [2, 3-c] morpholine and a grignard reagent, and optionally converting the delmopinol (or derivative) free base into a pharmaceutically acceptable salt. The oxazolidin [2, 3-c] morpholine and the grignard reagent are useful as intermediates in the production process.Type: ApplicationFiled: November 17, 2006Publication date: May 28, 2009Inventors: Juan Jose Artus Surroca, David Fernandez Bleda, Tommaso Iacoangeli, Jordi Lluis Tous
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Publication number: 20090131441Abstract: Metabolites of 2-(R)-4-isobutylarylpropionamides and pharmaceutical compositions containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: ApplicationFiled: January 24, 2006Publication date: May 21, 2009Applicant: DOMPE phar.r.ma S.p.A.Inventors: Riccardo Bertini, Cinzia Bizzarri, Marco Mosca, Marcello Allegretti, Francesco Colotta
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Patent number: 7534880Abstract: The present invention relates to clear photopolymerisable systems for the preparation of high thickness coatings, to a procedure for their application and to the solid surfaces coated with them.Type: GrantFiled: August 3, 2004Date of Patent: May 19, 2009Assignee: Lamberti SpAInventors: Gabriele Norcini, Stefano Romagnano, Marco Visconti, Giuseppe Li Bassi
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Patent number: 7521552Abstract: There is provided a process for the preparation of substituted amino alcohols HO—(CH2)n—NR1R2 from haloalcohols HO—(CH2)n—X, where X is Cl, Br or I, by reaction with an amine HNR1R2, in water as solvent at a temperature range of about 20° C. to about 90° C. optionally in the presence of a catalytic amount of an iodide source metal iodides. The haloalcohols are useful in the preparation of 6-[(substituted)phenyl]-triazolopyrimidine compounds which are useful in the treatment of cancer.Type: GrantFiled: December 8, 2004Date of Patent: April 21, 2009Assignee: WyethInventors: Yanzhong Wu, Arkadiy Rubezhov, Jean Schmid, Jay Thomas Afragola
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Publication number: 20090036677Abstract: It comprises a preparation process of delmopinol or a pharmaceutically acceptable salt and/or a solvate thereof, by submitting the compound of formula (II) where R1 and R2 are the same or different, independently selected from the group consisting of H, (C1-C6)-alkyl or, alternatively, R1 and R2 form, together with the carbon atom to which they are attached, a (C5-C6)-cycloalkyl radical; and R3 is a radical selected from the group consisting of CF3, (C1-C4)-alkyl, phenyl, and phenyl mono- or disubstituted by a radical selected from the group consisting of (C1-C4)-alkyl, halogen and nitro to a deprotection and cyclisation reaction. The process is useful to prepare delmopinol or its salts on an industrial scale. The compound of formula (II) is new and also forms part of the present invention, as well as its preparation process and other new intermediates of said preparation process.Type: ApplicationFiled: January 10, 2007Publication date: February 5, 2009Inventors: Alexander Comely, Llorenc Rafecas Jane, Nicolas Tesson, Atoni Riera Escale
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Publication number: 20090023731Abstract: Disclosed are urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases.Type: ApplicationFiled: March 21, 2008Publication date: January 22, 2009Inventors: Richard D. Gless, JR., Sampath Kumar Anandan
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Publication number: 20090018103Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.Type: ApplicationFiled: October 7, 2005Publication date: January 15, 2009Applicant: VITAE PHARMACEUTICAL, INCInventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillar, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
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Publication number: 20080176838Abstract: The invention relates to compounds of formula (I) wherein R1-9, Z, n, X, A, and Rb have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament for the treatment of type 2 diabetes mellitus, obesity and lipid disorders.Type: ApplicationFiled: June 8, 2005Publication date: July 24, 2008Applicant: SANTHERA PHARMACEUTICALS (DEUTSCHLAND) AGInventors: Paul John Edwards, Silvia Cerezo-Galvez, Achim Feurer, Oliver Hill, Meinolf Thiemann, Victor Giulio Matassa, Sonja Nordhoff, Meritxell Lopez-Canet
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Patent number: 7378521Abstract: The invention relates to a process for the preparation of substituted 2-vinyl-2-arylmorpholine derivatives as described herein. This invention also relates to 2-vinyl-2-arylmorpholine derivatives as well as intermediates therefor.Type: GrantFiled: March 29, 2007Date of Patent: May 27, 2008Assignee: Sanofi-AventisInventors: Alain Aulombard, Francoise Bernon, Alain Burgos, Claude Cabos, Eric Lucas, Sabrina Bonnefoy
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Publication number: 20080113976Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.Type: ApplicationFiled: November 28, 2007Publication date: May 15, 2008Inventor: Percy H. Carter
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Publication number: 20080102405Abstract: A resist composition comprising as a quencher a nitrogen-containing organic compound bearing a nitrogen-containing heterocycle and having a molecular weight of at least 380 exhibits a high resolution and satisfactory mask coverage dependence and is useful in microfabrication using electron beam or deep-UV.Type: ApplicationFiled: October 24, 2007Publication date: May 1, 2008Inventors: Takeru Watanabe, Youichi Ohsawa, Masaki Ohashi, Wataru Kusaki, Tomohiro Kobayashi
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Patent number: 7361757Abstract: A process for the synthesis of compounds of formula (I): wherein R represents a linear or branched (C1-C6)alkyl group. Application in the synthesis of perindopril and its pharmaceutically acceptable salts.Type: GrantFiled: August 31, 2004Date of Patent: April 22, 2008Assignee: Les Laboratoires ServierInventors: Fabienne Breard, Claude Fugier
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Patent number: 7354920Abstract: Compounds of formula (I) wherein Rx is H; Ry is H or C1-C4 alkyl; each Rz is independently H or C1-C4 alkyl; X represents O; Y represents OH or OR; R is C1-C4 alkyl; and Ar1 and Ar2 are optionally substituted phenyl or 5- or 6-membered heteroaryl rings are selective inhibitors of the reuptake of norepinephrine.Type: GrantFiled: August 18, 2003Date of Patent: April 8, 2008Assignee: Eli Lilly and CompanyInventors: Manuel Javier Cases-Thomas, Helen Louise Haughton, Robin George Simmonds, Hélène Catherine Eugénie Rudyk, Magnus Wilhelm Walter, Sivi Ouwerkerk-Mahadevan, John Joseph Masters, Carlos Lamas-Peteira
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Patent number: 7323563Abstract: A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof:Type: GrantFiled: August 22, 2005Date of Patent: January 29, 2008Assignee: British Biotech Pharmaceuticals Ltd.Inventors: Michael George Hunter, Paul Raymond Beckett, John Martin Clements, Mark Whittaker, Zoe Marie Spavold
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Patent number: 7323466Abstract: The present invention refers to chemical compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5 have the significance given in claim 1. These compounds can be used for the preparation of medicaments.Type: GrantFiled: January 13, 2006Date of Patent: January 29, 2008Assignees: Hoffman-La Roche Inc., Vernalis Research LimitedInventors: Jonathan Mark Bentley, Claire Elizabeth Dawson, Wolfgang Guba, Paul Hebeisen, Nathaniel Monck, Robert Mark Pratt, Hans Richter, Stephan Roever, Vicki Ruston
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Patent number: 7279478Abstract: This invention relates to class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: September 3, 2003Date of Patent: October 9, 2007Assignee: Merck Frosst Canada & Co.Inventors: Michael Boyd, Marc Gagnon, Cheuk Lau, Christophe Mellon, John Scheigetz
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Patent number: 7229803Abstract: The invention relates to methods for reacting (di)amines as substrates in the presence of a lysine oxidase arid a reducing agent, resulting in alcohols, diols or cyclic secondary amines. In a particular embodiment, the invention is directed to methods of preparing cyclic secondary amines suitable for ultimately synthesizing piperidine-2-carboxylic acid and proline derivatives, useful, for example as thrombin inhibitors.Type: GrantFiled: April 8, 2002Date of Patent: June 12, 2007Assignee: BASF AktiengesellschaftInventors: Thomas Friedrich, Norbert Zimmermann, Rainer Stürmer
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Patent number: 7223860Abstract: The invention relates to a process for the preparation of substituted 2-vinyl-2-arylmorpholine derivatives as described herein. This invention also relates to 2-vinyl-2-arylmorpholine derivatives as well as intermediates therefor.Type: GrantFiled: March 8, 2006Date of Patent: May 29, 2007Assignee: Sanofi-AventisInventors: Alain Aulombard, Francoise Bernon, Alain Burgos, Claude Cabos, Eric Lucas, Sabrina Bonnefoy
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Patent number: 7101882Abstract: The present invention relates to novel morpholin-acetamide compounds of formula (I) useful for the treatment of inflammatory diseases. Compounds of formula (I) wherein R1, R2, R3, R4, R5, X, a, b and Z are as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.Type: GrantFiled: September 28, 2001Date of Patent: September 5, 2006Assignee: Glaxo Group LimitedInventors: Rachael Anne Ancliff, Caroline Mary Cook, Colin David Eldred, Paul Martin Gore, Lee Andrew Harrison, Simon Teanby Hodgson, Duncan Bruce Judd, Suzanne Elaine Keeling, Xiao Qing Lewell, Graeme Michael Robertson, Stephen Swanson
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Patent number: 7071359Abstract: A compound represented by the Formula below, and an agent for the remedy of neural damage having the said compound as the active ingredient. [Here, G represents G1 shown below R4 represents, hydrogen atoms and acyl groups, W represents single bonds and alkylenes, m represents 0 or 1, R5 and R6 represent hydrogen atoms, aliphatic hydrocarbon groups, alicyclic hydrocarbon groups, aromatic hydrocarbon groups and heterocyclic groups, and R7 represents hydrogen atoms, acyl groups and alkoxycarbonyl groups. A2 represents, single bonds, —O—, —NR3—, and —S(?O)n—, A1 and A3 represent single bonds, aliphatic hydrocarbon groups, alicyclic hydrocarbon groups, heterocyclic groups and phenylene groups, and A4 represents single bonds, carbonyl groups and aliphatic hydrocarbon groups. R1 and R2 represent hydrogen atoms, alkyl groups, cycloalkyl groups, phenyl groups and heterocyclic groups. The previously mentioned functional groups may be substituted.Type: GrantFiled: August 7, 2000Date of Patent: July 4, 2006Assignee: Teijin LimitedInventors: Satoshi Sugiura, Takaharu Tsutsumi, Yorimasa Suwa, Takami Arai, Katsutoshi Sakurai, Noboru Yoshioka, Akira Tanokura, Jun Suzuki
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Patent number: 7038044Abstract: The invention relates to a process for the preparation of substituted 2-(2-arylmorpholin-2-yl)ethanol derivatives.Type: GrantFiled: July 7, 2000Date of Patent: May 2, 2006Assignee: sanofi-aventisInventors: Alain Aulombard, Françoise Bernon, Sabrina Bonnefoy, Alain Burgos, Claude Cabos, Eric Lucas
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Patent number: 7030111Abstract: The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to DNA-damaging agents by abrogating the cell cycle G2 checkpoint. Compounds of the invention are used to treat proliferative disorders such as cancer. The invention provides compositions and methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA-damaging agents and treatments.Type: GrantFiled: June 6, 2003Date of Patent: April 18, 2006Assignee: Canbas Co., Ltd.Inventors: Takumi Kawabe, Hidetaka Kobayashi
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Patent number: 6998400Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions comprising them, and processes for their preparation; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, pain, sexual dysfunction, Parkinson's disease, Alzheimer's disease, addiction to cocaine or tobacco products, seasonal affective disorder, chronic fatigue, narcolepsy or cognitive impairment using such compound, salts, solvates or compositions.Type: GrantFiled: May 17, 2002Date of Patent: February 14, 2006Assignee: Smithkline Beecham CorporationInventors: John A. Ascher, Joseph Andrews Johnston, Susan Marie Learned-Coughlin, Alan Bye