Nitrogen Attached Directly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/244)
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Patent number: 8188277Abstract: The present invention provides a novel compound, which has an excellent effect of suppressing the generation of collagen and less side effects, with being excellent in terms of safety. The compound of the present invention is represented by the following general formula (1): [wherein X1 represents a nitrogen atom or a group —CH?; R1 represents a group —Z—R6, wherein Z represents a group —CO—, a group —CH(OH)—, or the like, and R6 represents a 5- to 15-membered monocyclic, dicyclic, or tricyclic, saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms, or sulfur atoms; R2 represents a hydrogen atom, a halogen atom or a lower alkylene group; Y represents a group —O—, a group —CO—, a group —CH(OH)—, a lower alkylene group, or the like; and A represents a group or the like, wherein R3 represents a hydrogen atom, a lower alkoxy group, or the like, p represents 1 or 2, and R4 represents an imidazolyl lower alkyl group or the like.Type: GrantFiled: August 3, 2005Date of Patent: May 29, 2012Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Tae Fukushima, Shuji Matsumura, Noriaki Takemura, Hideaki Satou, Nobuaki Ito, Takuya Shitsuta, Hironori Tsutsui, Michinori Tanaka, Keizo Kan, Hitoshi Nagao, Kenji Watanabe, Kuninori Tai, Takashi Nakagawa, Hideki Takasu, Makoto Sakamoto, Keisuke Miyajima, Satoshi Yamada, Yutaka Kojima, Koichi Yasumura, Naoto Ohi, Mitsuhiro Okuno, Kazuhisa Sugiyama, Kunihiko Kiyono, Takashi Suzuki, Seiji Akamatsu, Takeshi Kodama, Yasuo Yanagihara, Takumi Sumida
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Publication number: 20120071659Abstract: The present disclosure generally related to an improved process for the preparation of various piperidine derivatives. More particularly, the present disclosure related to an improved process for preparing sufentanil base (1) and related compounds, which advantageously utilizes more cost effective and/or less hazardous reagents, including a dispersion comprising between about 50% and about 70% by weight (based on the total weight of the dispersion) of an alkali metal hydride, such as sodium hydride, as well as eliminates the need for expensive and/or time consuming purification techniques.Type: ApplicationFiled: September 15, 2011Publication date: March 22, 2012Applicant: Mallinckrodt LLCInventors: Brian ORR, Joseph P. HAAR, JR., George H. KLEMM, Keith G. TOMAZI
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Patent number: 8138259Abstract: The invention relates to a housing from a polyamide molding compound containing 70 to 99.5% by weight of at least one thermoplastic polyamide and 0.5 to 30% by weight of at least one polyamide oligomer with linear or branched chain structure with a number average molar mass of 800 to 5000 g/mol with basic end groups which are at least partially NH2 end groups, and carboxyl end groups, one of these end groups being present in excess and the concentration of the end group present in excess being at most 300 mmol/kg.Type: GrantFiled: August 28, 2009Date of Patent: March 20, 2012Assignee: Ems-Chemie AGInventors: Paul Schwitter, Georg Stoeppelmann, Alex Stolarz, Helmut Thullen
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Publication number: 20120029021Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.Type: ApplicationFiled: January 17, 2011Publication date: February 2, 2012Applicant: THE TRUSTEES OF CALIFORNIA STATE UNIVERSITYInventors: Yong Ba, Errol V. Mathias
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Publication number: 20120029188Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.Type: ApplicationFiled: October 7, 2011Publication date: February 2, 2012Applicant: UCB Pharma S.A.Inventors: Andrew David Carr, Judi Charlotte Neuss, Michael Glen Orchard, David William Porter
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Publication number: 20110311583Abstract: (A1) Translate this text The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells.Type: ApplicationFiled: November 10, 2009Publication date: December 22, 2011Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah Manoharan, kallanthottathil G. Rajeev, Muthusamy Jayaraman, David Butler, Jayaprakash K. Narayanannair, Martin Maier, Laxman Eltepu
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Patent number: 8071605Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: GrantFiled: December 10, 2009Date of Patent: December 6, 2011Assignee: AstraZeneca ABInventors: Gregory Basarab, Pamela Hill, Brian Sherer, Fei Zhou
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Publication number: 20110275797Abstract: An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.Type: ApplicationFiled: January 29, 2010Publication date: November 10, 2011Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe
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Patent number: 8026255Abstract: This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: GrantFiled: May 10, 2010Date of Patent: September 27, 2011Assignee: Hoffman-La Roche Inc.Inventors: Alfred Binggeli, Andreas D. Christ, Hans P. Maerki, Rainer E. Martin
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Publication number: 20110224337Abstract: The present invention relates to a process for purifying an N-alkyllactam which comprises contacting N-alkyllactams with carbon. The present invention also relates to mixtures comprising poly(vinylidene fluodride) (PVDF) and N-alkyllactams, in which the N-alkyllactams have been purified by contacting the N-alkyllactam as well as a method for their production. The present invention also relates to the use of said mixtures in processing PVDF for applications in which improved color is a quality requirement.Type: ApplicationFiled: November 18, 2009Publication date: September 15, 2011Applicant: BASF SEInventors: Yoshihisa Fujii, Kanno Hiroyasu
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Publication number: 20110207926Abstract: A compound represented by formula (1), a tautomer thereof, or a salt of the compound or tautomer, which is useful as a bactericide/disinfectant. In the formula, R1 represents a hydrogen atom, an optionally substituted alkyl group or the like, R2 represents a hydrogen atom or an optionally substituted alkyl group, or alternatively R1 and R2 may combine together with an adjacent nitrogen atom to form an optionally substituted nitrogen-containing heterocyclic group; R4 represents a hydrogen atom or an optionally substituted alkyl group; R3 represents an optionally substituted alkyl group; and R5 and R6 each represents a hydrogen atom or a methyl group, excluding a compound wherein both R2 and R4 represent a hydrogen atom and a compound wherein both R1 and R4 represent a hydrogen atom are excluded.Type: ApplicationFiled: August 24, 2009Publication date: August 25, 2011Applicant: HAMARI CHEMICALS, LTD.Inventors: Shirou Maeda, Akihisa Maeda
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Patent number: 7968568Abstract: This invention is concerned with compounds of the formula wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: GrantFiled: November 19, 2009Date of Patent: June 28, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Andreas D. Christ, Rainer E. Martin
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Publication number: 20110129419Abstract: The present invention relates to the field of medical imaging, and in particular to imaging of disease states associated with the upregulation of the chemokine receptor 5 (CCR5). Imaging agents, precursors and methods are provided which are useful in imaging such disease states.Type: ApplicationFiled: December 19, 2007Publication date: June 2, 2011Applicants: GE HEALTHCARE LIMITED, HAMMERSMITH IMANET LIMITEDInventors: Anthony Eamon Storey, Julie Davis, Erik Arstad, Benedicte Guilbert, Alessandra Gaeta
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Patent number: 7951952Abstract: The invention concerns a novel method for preparing N-aminopiperidine of formula (I):Type: GrantFiled: June 30, 2008Date of Patent: May 31, 2011Assignee: Sanofi-AventisInventors: Pierre Jean Grossi, Raphael Sole
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Publication number: 20110104162Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.Type: ApplicationFiled: June 15, 2009Publication date: May 5, 2011Applicant: Cytomics SystemsInventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
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Patent number: 7910652Abstract: The invention relates to a polyamide moulding compound containing 70 to 99.5% by weight of at least one thermoplastic polyamide and 0.5 to 30% by weight of at least one polyamide oligomer with linear or branched chain structure with a number average molar mass of 800 to 5000 g/mol with basic end groups which are at least partially NH2 end groups, and carboxyl end groups, one of these end groups being present in excess and the concentration of the end group present in excess being at most 300 mmol/kg.Type: GrantFiled: March 24, 2006Date of Patent: March 22, 2011Assignee: Ems-Chemie AGInventors: Paul Schwitter, Georg Stoeppelmann, Alex Stolarz, Helmut Thullen
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Patent number: 7879999Abstract: The invention relates to a method for the synthesis of exocyclic derivatives of cycloalkyl-hydrazines and exocyclic derivatives of heterocycloalkyl-hydrazines The invention is characterised in that the method comprises a step consisting in demixing a solution containing said synthesised derivative, by reacting a heterocyclic amine with monochloramine, in an organic phase and an aqueous phase with the addition of anhydrous sodium hydroxide. According to the invention, the starting amine which has not reacted is collected and reused directly without any additional treatment. The inventive method can also be used to obtain the corresponding exocyclic heterocycloalkyl-hydrazine or cycloalkyl-hydrazinederivative derivative at a low cost compared to that of other known methods.Type: GrantFiled: December 17, 2004Date of Patent: February 1, 2011Assignees: Isochem, Centre National de la Recherche Scientifique (CNRS), Universite Claude Bernard Lyon, 1Inventors: Henri Delalu, Cécile Colas-Duriche, Jacques Berthet, Philippe Leurent
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Publication number: 20110021780Abstract: Provided is a manufacturing method for a piperidine-3-ylcarbamate compound in which a pyridine-3-ylcarbamate compound and hydrogen are brought into contact in the presence of a palladium catalyst.Type: ApplicationFiled: March 18, 2009Publication date: January 27, 2011Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yosuke Watanabe, Junichi Yasuoka, Tetsuya Ikemoto
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Publication number: 20110003855Abstract: Disclosed are compounds and methods of synthesis of Formula I for the development of antiviral drugs for the treatment of HCV infection.Type: ApplicationFiled: January 29, 2009Publication date: January 6, 2011Applicant: The Regents of the University of CaliforniaInventors: Thomas C. Hermann, Maia Carnevali
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Publication number: 20100331546Abstract: Disclosed is a method for optical resolution of an alkylpiperidin-3-yl carbamate, the method including bringing an RS mixture of an alkylpiperidin-3-yl carbamate into contact with an optically active tartaric acid in the presence of a solvent.Type: ApplicationFiled: February 17, 2009Publication date: December 30, 2010Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yosuke Watanabe, Junichi Yasuoka, Tetsuya Ikemoto
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Publication number: 20100311791Abstract: The present invention relates to active bactericidal, antibacterial, anti-infective, antimicrobial, sporicidal, disinfectant, antifungal and antiviral compounds and compositions and to new uses of these compositions in therapy. This specification also describes methods of use for the new compounds and compositions. The specification further describes methods for preparing these compounds.Type: ApplicationFiled: December 28, 2007Publication date: December 9, 2010Inventors: Ramin Najafi, Rakesh K. Jain, Timothy P. Shiau, Eddy Low, Satheesh K. Nair
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Patent number: 7825140Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.Type: GrantFiled: October 19, 2007Date of Patent: November 2, 2010Assignee: Astex Therapeutics, Ltd.Inventors: Valerio Berdini, Michael Alistair O'Brien, Maria Grazia Carr, Theresa Rachel Early, Adrian Liam Gill, Gary Trewartha, Alison Jo-Anne Woolford, Andrew James Woodhead, Paul Graham Wyatt
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Publication number: 20100267697Abstract: The present teachings provide compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.Type: ApplicationFiled: December 11, 2007Publication date: October 21, 2010Applicant: WyethInventors: Vincent P. Galullo, Robert Zelle, Danielle Soenen, Christopher Todd Baker, Paul Will, Hormoz Mazdiyasni, Jinsong Guo, Andrew Fensome, Jeffrey Curtis Kern, William Jay Moore, Edward George Melenski, Justin Kaplan
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Publication number: 20100267669Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.Type: ApplicationFiled: June 10, 2010Publication date: October 21, 2010Inventors: 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: 20100249049Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: ApplicationFiled: May 7, 2010Publication date: September 30, 2010Inventors: Hiroshi MIYAZAKI, Junko TSUBAKIMOTO, Kosuke YASUDA, Iwao TAKAMURO, Osamu SAKURAL, Tetsuya YANAGIDA, Yataka HISADA
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Publication number: 20100234353Abstract: 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 15, 2010Publication date: September 16, 2010Applicant: Janssen Pharmaceutica N.V.Inventors: Kristof Van Emelen, Leo Jacobus Jozef Backx, Sven Franciscus Anna Van Brandt, Patrick René Angibaud, Isabelle Noëlle Constance Pilatte, Marc Gustaaf Celine Verdonck, Hans Louis Jos De Winter, Jimmy Arnold Viviane Van Heusden
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Patent number: 7786222Abstract: The present invention relates to polyamide oligomers with linear or branched chain structure with a number average molar mass of 800 to 5000 g/mol, with basic end groups which are at least partially NH2 end groups and carboxyl end groups, produced by condensation of polyamide-forming monomers, the concentration of NH2 end groups being at most 300 mmol/kg and in that these end groups are present in excess in a ratio to the carboxyl end groups.Type: GrantFiled: April 24, 2006Date of Patent: August 31, 2010Assignee: EMS-Chemie AGInventors: Eduard Schmid, Botho Hoffmann
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Patent number: 7786308Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: GrantFiled: March 28, 2006Date of Patent: August 31, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ioana Drutu, Miguel Garcia-Guzman Blanco, Lewis R. Makings, Gabriel Raffai, Valentin Boris Zunic
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Publication number: 20100197928Abstract: The disclosure relates to a method for preparing a compound of formula (I), wherein P1 and P2 are groups protecting the carboxylic acid and oxyamine functions, starting from pyroglutamic acid (S). The disclosure also relates to novel intermediates.Type: ApplicationFiled: September 12, 2008Publication date: August 5, 2010Applicant: NOVEXELInventors: Alain Priour, Alain Bonnet, Gilles Oddon, Alain Mazurie
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Patent number: 7767692Abstract: 4-substituted 1-amidomethylcarbonyl-piperidine compounds having motilin-agonistic properties and their acid addition salts, pharmaceutical compositions containing these compounds, processes and intermediate products for the preparation of these compounds, and methods of treatment utilizing these compounds.Type: GrantFiled: November 10, 2003Date of Patent: August 3, 2010Assignee: Solvay Pharmaceuticals GmbHInventors: Daniel Jasserand, Jochen Antel, Ulf Preuschoff, Reinhard Brueckner, Holger Sann, Michael Wurl, Peter Eickelmann
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Publication number: 20100152452Abstract: This invention relates to dialdehyde or dinitrile compounds, which are useful for stereoselective synthesis of piperidine, pyrrolidine, and azepane derivatives.Type: ApplicationFiled: December 14, 2009Publication date: June 17, 2010Applicant: TaiGen Biotechnology Co., Ltd.Inventors: Shan-Yen Chou, Chi-Hsin Richard King
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Publication number: 20100152439Abstract: The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein R1 is defined as in claim 1.Type: ApplicationFiled: February 23, 2010Publication date: June 17, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Guenther HUCHLER, Werner RALL, Uwe RIES
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Patent number: 7728008Abstract: The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.Type: GrantFiled: June 26, 2006Date of Patent: June 1, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Jennifer Qiao, Tammy C. Wang, James C. Sutton, Timur Gungor
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Publication number: 20100105917Abstract: The present invention relates to a method for producing an optically active 3-aminopiperidine or salt thereof. In the method, a racemic nipecotamide is stereoselectively hydrolyzed to obtain an optically active nipecotamide and an optically active nipecotic acid in the presence of an enzyme source derived from an organism, and then the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by aroylation, Hofmann rearrangement, deprotection of the amino group and further deprotection; or the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by selective protection with BOC, Hofmann rearrangement and further deprotection. It is possible by the present invention to produce an optically active 3-aminopiperidine or salt thereof useful as a pharmaceutical intermediate from an inexpensive and easily available starting material by easy method applicable to industrial manufacturing.Type: ApplicationFiled: February 18, 2008Publication date: April 29, 2010Applicant: KANEKA CORPORATIONInventors: Kohei Mori, Masutoshi Nojiri, Akira Nishiyama, Naoaki Taoka
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Publication number: 20100105894Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.Type: ApplicationFiled: June 9, 2009Publication date: April 29, 2010Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafuml Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
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Publication number: 20100099880Abstract: An alternate process for synthesizing opiate or opioid analgesics and anesthetics, and intermediates thereof is provided. In particular, a process of synthesizing synthetic opiate or opioid compounds such as, for example, remifentanil, carfentanil, sufentanil, fentanyl, and alfentanil are disclosed.Type: ApplicationFiled: September 20, 2007Publication date: April 22, 2010Inventor: Brian Cheng
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Patent number: 7700622Abstract: Compounds and compositions for modulating the activity of p38 kinases are provided, including p38? and p38? kinase. Methods for treating, preventing or ameliorating one or more symptoms of a p38 kinase mediated disease or disorder are also provided.Type: GrantFiled: July 23, 2004Date of Patent: April 20, 2010Assignee: Novartis AGInventors: Hengyuan Lang, Jiong Lan, Yunfeng Fang
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Publication number: 20100069630Abstract: The present invention discloses novel naphthalenyloxypropenyl derivatives useful for inhibiting the enzyme activity of histone deacetylase, leading effective suppression of cancer cell proliferation.Type: ApplicationFiled: November 1, 2007Publication date: March 18, 2010Applicants: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY, CRYSTALGENOMICS, INCInventors: Cheol Hae Lee, Hee Jung Jung, Jae Hak Kim, Won Jang Jeong, Joong Myung Cho, Seong Gu Ro, Young Lan Hyun, Cheol Soon Lee
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Publication number: 20100069413Abstract: This invention is concerned with compounds of the formula wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: ApplicationFiled: November 19, 2009Publication date: March 18, 2010Inventors: Andreas D. Christ, Rainer E. Martin
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Publication number: 20100016600Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.Type: ApplicationFiled: September 28, 2009Publication date: January 21, 2010Applicant: WAYNE STATE UNIVERSITYInventor: Aloke K. Dutta
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Publication number: 20100016601Abstract: A process for preparing remifentanil by conversion of the nitrile group of a cyanopiperidinyl propanoate derivative to an ester group. Advantageously, with this process the number of steps for preparing remifentanil from commercial products is significantly reduced, compared to the processes known in the art.Type: ApplicationFiled: June 13, 2007Publication date: January 21, 2010Applicant: KERN PHARMA, S.L.Inventors: Jorge Cervelló Pagès, Maria Cantó Vallverdú
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Patent number: 7645822Abstract: Process for preparation of polyoxymethylenes via polymerization of the monomers a) in the presence of cationic initiators b) and also, if appropriate, in the presence of regulators c), followed by deactivation and discharge from the reactor, which comprises using, as deactivator (d) at least one basic compound having at least 2 amino functions of different reactivity in one molecule.Type: GrantFiled: November 5, 2005Date of Patent: January 12, 2010Assignee: BASF SEInventors: Jens Assmann, Knut Zollner
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Publication number: 20090306382Abstract: The instant invention relates to cationic alkoxyamines, which are useful as polymerization initiators/regulators in a controlled stable free radical polymerization process to produce intercalated and/or exfoliated nanoparticles from natural or synthetic clays, The invention also relates to improved nanocomposites produced by this process and to the use of these nanocomposite compositions as, for example, coatings, sealants, caulks, adhesives and as plastic additives.Type: ApplicationFiled: August 5, 2009Publication date: December 10, 2009Inventors: ANDREAS Mühlebach, Peter Nesvadba, Andreas Kramer
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Publication number: 20090298878Abstract: The invention relates to oxime compounds of Formula (I) and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X is hydrogen, optionally substituted aryl, optionally substituted heteroaryl or the like; Y is CO, SO2, CR3R4 or the like; Z is optionally substituted lower alkyl, optionally substituted aryl or the like; W is optionally substituted lower alkylene or optionally substituted lower alkenylene, R3 and R4 are each independently hydrogen, lower alkyl or the like; p is 0, 1, or 2 and q is 0, 1 or 2. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate 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: July 12, 2007Publication date: December 3, 2009Inventors: Akira Matsumura, Hidenori Mikamiyama, Naoki Tsuno, Donald J. Kyle, Bin Shao, Jiangchao Yao
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Patent number: 7626032Abstract: This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.Type: GrantFiled: April 24, 2008Date of Patent: December 1, 2009Assignee: Wockhardt LimitedInventors: Noel John De Souza, Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Shiv Kumar Agarwal, Kandepu Sreenivas, Sheela Chandrasekharan Nair, Yati Chugh, Milind Chintaman Shukla
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Publication number: 20090258061Abstract: A method and a daily replacement patch for transdermally administering an opioid for analgesic effect. The patch is applied to a subject to deliver the opioid through the skin. The patch may be replaced daily and over an extended period of time.Type: ApplicationFiled: October 15, 2008Publication date: October 15, 2009Applicant: JOHNSON & JOHNSONInventors: Stephen S. Hwang, Robert M. Gale
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Publication number: 20090239910Abstract: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula I and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate 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: March 29, 2007Publication date: September 24, 2009Inventors: Zhengning Chen, Khondaker Islam, Bin Shao, Jiangchao Yao, Xiaoming Zhou, Donald J. Kyle
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Publication number: 20090227566Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor. An example of a compound of formula (I) is (a).Type: ApplicationFiled: November 10, 2005Publication date: September 10, 2009Inventors: Ankush Baburao Argade, Theodore Goodson, JR., David Kent Herron, Sajan Joseph, Salvatore Donato Lepore, Angela Lynn Marquart, John Joseph Masters, David Mendel, Leander Merritt, Andrew Michael Ratz, Gerald Floyd Smith, Anne Lousie Tebbe, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20090215765Abstract: Neuroprotective compounds for treating optic neuropathies and screening methods for identifying neuroprotective compounds.Type: ApplicationFiled: April 24, 2006Publication date: August 27, 2009Applicant: The Johns Hopkins UniversityInventors: John Barnwell Kerrison, Donald J. Zack
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Publication number: 20090208413Abstract: The present invention provides compositions and methods for synthesizing labeled drugs. The present invention further provides methods for preventing or stopping prescription drug abuse for all agents registered as a Drug Enforcement Agency (DEA) schedule II through schedule V medications. According to the present invention, methods are provided for monitoring patient compliance with prescribed drug treatment. The present invention also provides methods for facilitating a replacement prescription when a patient is left without access to their prescribed drug. Furthermore, the present invention provides a method to improve employee compliance with an employer's drug policies via either a voluntary or compulsory system for enhanced drug testing.Type: ApplicationFiled: February 23, 2006Publication date: August 20, 2009Inventors: Alan J Reis, Christian Schafmeister