Oxy In Acid Moiety Patents (Class 560/29)
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Publication number: 20120171117Abstract: The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.Type: ApplicationFiled: March 8, 2012Publication date: July 5, 2012Applicant: HAMMERSMITH IMANET LIMITEDInventors: ERIK ARSTAD, MATTHIAS EBERHARD GLASER
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Publication number: 20120158127Abstract: Absorbable polyurethanes, polyamides and polyester urethanes prepared from at least one compound selected from: or the corresponding diamines or diisocyanates thereof, wherein each X independently represents —CH2COO—, —CH(CH3)COO—, —CH2CH2OCH2COO—, —CH2CH2CH2CH2CH2COO—, —(CH2)yCOO— where y is 2 to 4 or 6 to 24, or —(CH2CH2O)z?CH2COO— where z? is 2 to 24; each Y represents —COCH2O—, —COCH(CH3)O—, —COCH2OCH2CH2O—, —COCH2CH2CH2CH2CH2O—, —CO(CH2)mO— where m is 2 to 4 or 6 to 24, or —COCH2O(CH2CH2O)n— where n is 2 to 24; R? is hydrogen, benzyl or straight-chained or branched alkyl; p is 1 to 4; and Rn represents one or more members selected from H, alkoxy, benzyloxy, aldehyde, halogen, carboxylic acid and —NO2, which is attached directly to an aromatic ring or attached through an aliphatic chain. Absorbable polymers prepared from these compounds are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention and other implantable medical devices.Type: ApplicationFiled: February 22, 2012Publication date: June 21, 2012Applicant: BEZWADA BIOMEDICAL, LLCInventor: Rao S. Bezwada
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Publication number: 20120095251Abstract: The present invention relates to a method for producing (R)-2-acetamido-N-benzyl-3-methoxypropionamide (lacosamide), by methylation of (R)-2-acetamino-2-N-benzyl-3-hydroxy-propionamide (V), in which the methylation is carried out at a temperature below 20° C.Type: ApplicationFiled: October 17, 2011Publication date: April 19, 2012Inventors: Richard WISDOM, Joerg JUNG, Andreas MEUDT
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Publication number: 20120035226Abstract: The invention relates to oxadiazole compounds of formula I. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.Type: ApplicationFiled: March 29, 2010Publication date: February 9, 2012Applicant: MERCK SERONO SAInventors: Anna Quattropani, Cyril Montagne, Wolfgang Sauer, Stefano Crosignani, Agnés Bombrun
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Publication number: 20110319366Abstract: Compounds of the following formula (I), for example: wherein R1, R2, R3, and R4 are described herein, are useful as inhibitors of plasma carboxypeptidase B. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.Type: ApplicationFiled: August 29, 2011Publication date: December 29, 2011Inventors: Brad Buckman, Kumar Emayan, Imadul Islam, Karen May, Judi Bryant, Raju Mohan, Christopher West, Shendong Yuan
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Intermediate for producing lacosamide and a process for its preparation and conversion to lacosamide
Publication number: 20110319649Abstract: The invention relates to ((R)-1-Benzylcarbamoyl-2-hydroxy-ethyl)-carbamic acid tert-butyl ester (compound III) with an ee of greater than 90%. and a process for producing the same.Type: ApplicationFiled: June 20, 2011Publication date: December 29, 2011Inventors: Richard WISDOM, Joerg JUNG, Andreas MEUDT -
Publication number: 20110313154Abstract: A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c): (a) reacting an acyl phenylalanine derivative represented by the following formula (2): with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative; (b) converting the carboxy-asymmetric urea derivative into the corresponding quinazoline-dione derivative in the presence of a carboxyl group-activating agent: (c) if desired, substituting an N-alkyl group for the hydrogen atom bonded to the nitrogen atom present in the quinazoline-dione ring of the quinazoline-dione derivative using an N-alkylation agent and then deprotecting the resulting product, when the substituent R3? which is a group corresponding to R3 is protected.Type: ApplicationFiled: August 26, 2011Publication date: December 22, 2011Applicant: AJINOMOTO CO., INC.Inventors: Noriyasu KATAOKA, Kotaro OKADO, Tatsuhiro YAMADA, Koichi FUJITA, Tamotsu SUZUKI, Tatsuya OKUZUMI, Masayuki SUGIKI, Akinori TATARA
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Publication number: 20110294876Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of compounds of formula (I) given below, in particular as anti-ageing actives. wherein A denotes wherein X, Y and Z independently of one another denote hydrogen, C1-C4-alkyl or C2-C4-alkenyl, wherein optionally two of the radicals X, Y and Z are covalently bonded to one another under formation of a bicyclic ring system, in such a bicyclic ring system two of the radicals X, Y and Z together preferably form a radical having 1 to 4 carbon atoms, preferably a hydrocarbon radical having 1 to 3 carbon atoms, B denotes NR1R2, wherein R1 denotes hydrogen or an organic radical having 1 to 14 carbon atoms, R2 denotes an organic radical having 1 to 14 carbon atoms, and wherein optionally R1 and R2 are covalently bonded to one another, preferably so that B is a 3 to 8 membered ring.Type: ApplicationFiled: May 6, 2011Publication date: December 1, 2011Applicant: SYMRISE AGInventors: Thomas Küper, Heiko Oertling, Tilman Grune, Matthias Saathoff, Martina Herrmann, Julia Betke, Claudia Gömann, Rahim Brodhage, Imke Meyer
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Patent number: 8058474Abstract: A process for preparing a compound (C) represented by the following formula: wherein R1 represents hydrogen, C1-6 alkyl or C3-8 cycloalkyl, and R2 represents hydrogen or methoxy, characterized by reacting a compound (A-1) represented by the following formula: wherein R1 has the same definition as above, with a compound (B) represented by the following formula: wherein R2 has the same definition as above, and L represents a leaving group, is provided. Compound (C) is effective for prevention or treatment of various diseases associated with angiogenesis neoplasia.Type: GrantFiled: March 9, 2009Date of Patent: November 15, 2011Assignee: Eisai R&D Management Co., Ltd.Inventor: Toshihiko Naito
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Publication number: 20110237785Abstract: Novel spatially-defined macrocyclic compounds containing specific conformational control elements are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target. In particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.Type: ApplicationFiled: February 28, 2011Publication date: September 29, 2011Inventors: Éric Marsault, Kamel Benakli, Hamid R. Hoveyda, Mark L. Peterson, Sylvie Beaubien, Luc Ouellet, Carl St-Louis, Sophie Beauchemin
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Publication number: 20110190267Abstract: The present invention concerns prodrugs of opioid analgesics and pharmaceutical compositions containing such prodrugs. Methods for providing more consistent pain relief by increasing the bioavailability of the opioid analgesic with the aforementioned prodrugs are provided. The invention also provides for decreasing the adverse GI side effects of opioid analgesics.Type: ApplicationFiled: December 23, 2010Publication date: August 4, 2011Applicant: Shire Pharmaceuticals, Inc.Inventors: Richard Franklin, Karl Swift, Bernard T. Golding, Robert G. Tyson
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Publication number: 20110190527Abstract: The present invention provides a method for producing an optically active N-(halopropyl)amino acid derivative, wherein the method comprises the steps of obtaining a compound represented by formula (III) by reacting an optically active alanine ester represented by formula (I) or a salt thereof (hereinafter sometimes simply referred to as an “alanine ester”) with a halogenated propane represented by formula (II); and obtaining an optically active N-(halopropyl)amino acid derivative represented by formula (IV) by introducing a protecting group onto the nitrogen atom of the compound represented by formula (III). The present invention provides a method for efficiently producing an optically active N-(halopropyl)amino acid derivative.Type: ApplicationFiled: May 19, 2008Publication date: August 4, 2011Applicant: Nagase & Co., Ltd.Inventors: Jun Matsumoto, Toru Inoue
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Publication number: 20110178108Abstract: A group of amino substituted benzoyl derivatives, their preparation and their use. The screening and research on an antiviral drug with hA3G/Vif as a target point proves that the 3-amino benzoyl derivatives not only have the combined activity for the hA3G/Vif, but also have a function of inhibiting replication of viruses. The present invention provides the possible breakthrough progress for the problem of HIV drug resistance, thereby providing a novel clinical antiviral drug which has higher efficiency.Type: ApplicationFiled: September 28, 2009Publication date: July 21, 2011Applicant: Institute of Medicinal Biotechnology Academy of Medical ScienceInventors: Jian-Dong Jiang, Liyan Yu, Shan Cen, Zhourong Li, Yanping Li, Jlan Xu
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Publication number: 20110178305Abstract: The present invention relates to a process for the preparation of threo-3,4-epoxy-2-amino-1-substituted butane derivatives represented by general Formula I which comprises reacting compound of Formula III or salt thereof with an active ester of acid of Formula IV and treating the product thereof with base. The carbon atom bonded to the radical R3 in Formula I and IV is in the (R)-, (S)- or (R,S)-configuration. The compounds of Formula I and III, particularly in their (2S,3R) configuration are useful intermediates for the preparation of atazanavir bisulfate.Type: ApplicationFiled: May 5, 2009Publication date: July 21, 2011Applicant: RANBAXY LABORATORIES LIMITEDInventors: Rakesh Singh, Prasad Yeragorla, Mahavir Singh Khanna, Mohan Prasad
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Publication number: 20110152561Abstract: A method for production of an N-carboxy amino acid anhydride with efficiency is provided. The method for production of an N-carboxy amino acid anhydride includes a step of reaction of an amino acid organic salt compound with a carbonic acid diester.Type: ApplicationFiled: August 26, 2009Publication date: June 23, 2011Applicant: JSR CORPORATIONInventors: Takeshi Endo, Koichi Koga, Atsushi Sudo
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Publication number: 20110144177Abstract: Carbamoyl esters inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. In one embodiment, the carbamoyl ester has the following structure: wherein A is selected from the group consisting of an unsubstituted aryl, a substituted aryl, an unsubstituted heteroaryl and a substituted heteroaryl. The carbamoyl esters are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the carbamoyl esters can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.Type: ApplicationFiled: February 22, 2011Publication date: June 16, 2011Inventors: Jeroen C. Verheijen, ShouCheng Du
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Publication number: 20110129432Abstract: The present invention relates to the compound L-menthyl-N-(2-hydroxyphenyl)carbamate, which is effective against body perspiration odor bacteria, in particular against armpit perspiration odor bacteria, and simultaneously effective as an antioxidant, of the following formula, a method for the production thereof and its use.Type: ApplicationFiled: May 25, 2009Publication date: June 2, 2011Applicant: SYMRISE AGInventors: Stephan Hillers, Heiko Oertling, Claudia Goemann
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Publication number: 20110105482Abstract: A dual thyrointegrin antagonist and a method for treating an angiogenesis-mediated disorder and/or a hyperthyroidism disorders by introducing the dual thyrointegrin antagonist into animals (e.g., mammals, human beings). The dual thyrointegrin antagonist includes a chemical structure having a thyroid hormone antagonist and ?v?3 integrin antagonist in the same molecule.Type: ApplicationFiled: November 1, 2010Publication date: May 5, 2011Applicant: VASCULAR VISION PHARMACEUTICAL COMPANYInventor: Shaker A. Mousa
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Publication number: 20110065760Abstract: The present invention is related to a compound of the formula (I), (II), (III), (IV), (V): wherein Z1, Z2, Z3 and Z4 are each and independently selected from the group comprising C(O)—, —C(S)—, —C(O)—NR10—, —C(S)—NR11—, —C(N—CN)—NR12—, —S(O)—, —S(O2)—, —S(O)—NR13—, and S(O2)—NR14—, —O—, —S— or are each and individually absent; X is a spacer and is independently selected from the group comprising -M1-L1-K-L2-M2-, wherein Y.Type: ApplicationFiled: November 23, 2009Publication date: March 17, 2011Applicant: Jerini AGInventors: Jochen KNOLLE, Mike Schutkowski, Gerd Hummel, Thomas Tradler, Laurence Jobron, Claudia Christner, Dirk Scharn, Roland Stragies, Christoph Gibson, Frank Osterkamp
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Patent number: 7902401Abstract: Compounds of Formula I are useful in the treatment of epilepsy, neuropathic pain, acute and chronic inflammatory pain, migraine, tardive dyskinesia and other related CNS disorders. wherein: A and R1 to R8 are defined in the specification.Type: GrantFiled: December 14, 2006Date of Patent: March 8, 2011Assignee: NPS Pharmaceuticals, Inc.Inventors: Guy A. Higgins, Methvin Issac, Abdelmalik Slassi, Tao Xin
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Publication number: 20110039874Abstract: Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.Type: ApplicationFiled: April 16, 2010Publication date: February 17, 2011Applicant: Northeastern UniversityInventors: Alexandros Makriyannis, Spyridon P. Nikas, Shakiru O. Alapafuja, Vidyanand G. Shukla
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Publication number: 20100311991Abstract: The present invention disclosed an process for preparing docetaxel 1, including the following steps: a) hydroxyl acylation reaction of compound 2 and 3 to obtain compound 4; b) deprotection group R1 of the hydroxyl group of compound 4 obtained from step a to prepare compound 5; c) removing one tert-butoxycarbonyl of compound 5 obtained from step b to prepare compound 6; d) removing one acetyl of compound 6 obtained from step c to prepare compound 1; wherein, R1 represents tert-butyl dimethyl silyl, triethylsilyl, ethoxyethyl, tetrahydropyranyl, trichloroethoxycarbonyl or methoxymethyl, Boc is tert-butoxycarbonyl, Ac is acetyl, and Ph is phenyl. The present invention also disclosed intermediates of docetaxel and methods for preparation thereof.Type: ApplicationFiled: May 22, 2009Publication date: December 9, 2010Applicant: SHANGHAI PARLING PHARMA-TECH. CO., LTD.Inventors: Xin Shen, Huaxing Zhan, Jidong Yang, Xiao He, Fuxing Lin, Shaohong Wu
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Publication number: 20100298270Abstract: Described herein are novel HDAC modulators, formulations containing them and methods of using them. In some embodiments, the HDAC modulators possess specific stereo chemistry. In other embodiments, the compounds described herein are used in the treatment or prevention of histone deacetylase mediated disorders.Type: ApplicationFiled: July 23, 2008Publication date: November 25, 2010Applicant: SYNDAX PHARMACEUTICALS, INC.Inventors: John F.W. Keana, Peter Ordentlich, Robert Goodenow
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Patent number: 7838673Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.Type: GrantFiled: October 16, 2007Date of Patent: November 23, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Edward J. Olhava, Mihaela Diana Danca
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Publication number: 20100292439Abstract: A subject of the invention is the use of a salt with a dedicated task of formula (I): A+-L-R—OY, X? as soluble support for peptide synthesis, in which: X? represents a functional or non-functional anion, Y represents either a hydrogen atom, or a —COOR1 group, R1 representing in particular an alkyl group comprising 1 to 20 carbon atoms, A+ represents a cationic entity, L represents an arm, in particular an alkyl group of 3 to 20 carbon atoms, R represents in particular a group of formula —C(Ra)(Rb)—, Ra and Rb representing independently of one another in particular a hydrogen or an alkyl group, comprising 1 to 20 carbon atoms.Type: ApplicationFiled: July 5, 2006Publication date: November 18, 2010Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE`, UNIVERSITE DE RENNESInventors: Michel Vaultier, Céline Roche, Saïd Gmouh, Alain Commercon
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Publication number: 20100273836Abstract: The present invention provides a novel oxime ether derivative represented by the following formula (I), or salt thereof, that can be industrially produced advantageously, and can function as a fungicide for agricultural and horticultural use that has reliable effects and can be used safely, and a fungicide for agricultural and horticultural use that contains at least one of these compounds as an active ingredient thereof. In addition, the present invention provides a novel ketone derivative that is a production intermediate of the oxime ether derivative.Type: ApplicationFiled: December 11, 2008Publication date: October 28, 2010Applicant: Nippon Soda Co., Ltd.Inventors: Hironori Furukawa, Raito Kuwahara, Hiroyasu Hosokawa, Kazuya Shimizu
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Publication number: 20100267965Abstract: The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula II, or a salt thereof, and a compound of formula VI or a salt thereof, wherein R3 and R4 as well as Act are as defined in the specification, and processes of manufacturing these. Additionally transformation of compounds (VI) with metallo organic compounds (VII) give rise to the new compounds (VIII) which are direct precursors for the preparation of Aliskiren.Type: ApplicationFiled: June 25, 2010Publication date: October 21, 2010Inventors: Gottfried Sedelmeier, Dominique Grimler, Murat Acemoglu
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Publication number: 20100260702Abstract: Absorbable polyurethanes, polyamides and polyester urethanes prepared from at least one compound selected from: or the diamines and diisocyanates thereof, wherein each X represents a member independently selected from —CH2COO— (glycolic acid moiety), —CH(CH3)COO— (lactic acid moiety), —CH2CH2OCH2COO— (dioxanone), —CH2CH2CH2CH2CH2COO— (caprolactone moiety), —(CH2)yCOO— where y is one of the numbers 2, 3, 4 or 6-24 inclusive, and —(CH2CH2O)z?CH2COO— where z? is an integer between 2 and 24, inclusive; each Y represents a member independently selected from —COCH2O— (glycolic ester moiety), —COCH(CH3)O— (lactic ester moiety), —COCH2OCH2CH2O— (dioxanone ester), —COCH2CH2CH2CH2CH2O— (caprolactone ester), —CO(CH2)mO— where m is an integer between 2, 3, 4 or 6-24 inclusive, —COCH2O(CH2CH2O)n— where n is an integer between 2 and 24, inclusive; R? is hydrogen, benzyl or an alkyl group, the alkyl group being either straight-chained or branched; p is an integer between 1 and 4, inclusive; and Rn represents one or moreType: ApplicationFiled: June 25, 2010Publication date: October 14, 2010Applicant: Bezwada Biomedical LLCInventor: Rao S. Bezwada
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Publication number: 20100249393Abstract: The present invention provides for reagents for the introduction of colorimetric-oxycarbonyl protecting groups, compounds bearing colorimetric-oxycarbonyl protecting groups, and the use thereof in solid-supported organic syntheses of oligonucleotides, polypeptides, polysaccharides, and combinatorial libraries.Type: ApplicationFiled: March 30, 2009Publication date: September 30, 2010Applicant: Berry and Associates, Inc.Inventors: John C. Hodges, Yam Foo Poon, William H. Pearson
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Publication number: 20100217009Abstract: A process for preparing a compound of formula (22), comprising reducing a compound of formula (21), to produce a compound of formula (23), followed by the hydrogenolysis of the compound of formula 23 in a solvent comprising a C1 to C6 alkyl sulfonic acid and optionally a chlorinated solvent.Type: ApplicationFiled: May 21, 2008Publication date: August 26, 2010Applicant: BIAL - PORTELA & CA, S.A.Inventors: David Alexander Learmonth, Alexander Beliaev
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Publication number: 20100152188Abstract: The present invention relates to novel compounds of the general formula (I), their derivatives, their analogs, their stereoisomers, their pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel heterocyclic compounds of the general formula (I).Type: ApplicationFiled: August 4, 2006Publication date: June 17, 2010Inventors: Akella Satya Surya Visweswara Srinivas, Kasinathan Mathiyazhagan, Duddu Savaraiah Sharada, Thanasekaran Ponpandian, Kulasekharan Revathy, Gaddam Om Reddy, Mani Kamarai, Sriram Raiagopal
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Publication number: 20100145059Abstract: Provided are a novel method for producing a hydrazine compound useful as an insecticidal compound, and production intermediates which can be suitably used for the production method and methods for producing the intermediates. As the production intermediates, a specific isocyanate compound and an organomagnesium compound represented by the following general formula (IV) are provided. The organomagnesium compound can be synthesized from a corresponding dibromo compound.Type: ApplicationFiled: August 6, 2008Publication date: June 10, 2010Inventors: Taro Hirose, Kengo Kanematsu
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Publication number: 20100099898Abstract: Disclosed are intermediates and processes for preparing epoxides of the formula: where R and PROT are defined herein. These epoxides are useful as intermediates in the production of biologically active compounds, i.e., in the production of pharmaceutical agents.Type: ApplicationFiled: December 23, 2009Publication date: April 22, 2010Inventor: Michael R. Reeder
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Patent number: 7687656Abstract: The invention encompasses processes for the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, and intermediates of (S)-Pregabalin.Type: GrantFiled: October 28, 2008Date of Patent: March 30, 2010Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Vinod Kumar Kansal, Brijnath P. Chaurasia, V. Govardhan Rao, Anand Prakash Tiwari
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Patent number: 7652144Abstract: A compound of formula XIX wherein R1, R2, Z1, Z2, Q1, Q2 and Q3 as defined in the specification.Type: GrantFiled: June 18, 2007Date of Patent: January 26, 2010Assignee: Aventis Pharma LimitedInventors: Garry Fenton, Tahir Nadeem Majid, Malcolm Norman Palfreyman
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Patent number: 7629487Abstract: Provided herein are catalysts useful in enabling and promoting the insertion of alkylene oxides into ester linkages. The esters employed as a substrate to be alkoxylated include esters of fatty acids, such as methyl esters of C14 to C22 fatty acids, and mono-, di-, and tri-esters of glycerine, including vegetable oils, animal fats, and plant oils. A catalyst according to the invention includes at least two alkaline earth compounds, which may include any known stable compounds of the alkaline earths, and optionally contains one or more additional materials such as a carboxylic acid or a polyalkylene glycol having a molecular weight between about 100 and 1500 or a C1-C10 alkyl-capped polyalkylene glycol having molecular weight between about 100 and 1500, which has been acidified with a strong mineral acid. The preferred alkaline earths employed are salts and compounds of magnesium and calcium.Type: GrantFiled: May 31, 2005Date of Patent: December 8, 2009Assignee: Huntsman Petrochemical LLCInventors: George A. Smith, James O'Neill, Lindy R. Coker, legal representative, George Sneed, Christopher J. Whewell
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Patent number: 7625995Abstract: The present invention provides a compound having a formula: where R1 is selected from the group consisting of alkyl, CH2(OC2H4)OCH3, and —(OC2H4)OCH3; n is 0-4; Olig is an oligomer having a formula: -L-O-PAGR.R2]q where L is a optional linker moiety selected from the group consisting of —CH2O—, —CH2OX—, —OX—, —C(O)—, —C(O)X, —NH—, —NHC(O)—, —XNHC(O)—, —NHC(O)X—, —C(O)NH—, —C(O)NHX—, and where X is alky1-6 or is not present, Y is N or O or is not present, and R3 is alkyl1-6; PAG is a linear or branched polyalkylene glycol moiety; R2 is an alkyl1-22 capping moiety if X is present or alkyl2-22 if X is not present; and q is a number from 1 to the maximum number of branches on PAG; and m is 1-5.Type: GrantFiled: February 26, 2008Date of Patent: December 1, 2009Assignee: Biocon LimitedInventors: Nnochiri Ekwuribe, Amy L. Odenbaugh
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Publication number: 20090286875Abstract: The present invention relates to compounds of formula (I): wherein R1, R2, R4 and R4a are as defined herein. The invention also relates to the use of compounds of formula (I) for the treatment of pain.Type: ApplicationFiled: November 9, 2006Publication date: November 19, 2009Applicant: Pfizer, Inc.Inventor: Simon John Mantell
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Patent number: 7618999Abstract: The present invention relates to a process of obtaining taxosteroids and precursors thereof from the hydrindane bicyclic ring system. The compounds have a tetracyclic system which combines the structural characteristics of taxanes, such as the bicyclo[5.3.1]undecane system (cycles A and B), fused to a six-membered ring (C), and of steroids, such as the CD bicycle, the A ring and the side chain (Sc). The process of preparing the compounds and their application as compositions with pharmacological properties of interest are described.Type: GrantFiled: July 2, 2004Date of Patent: November 17, 2009Assignee: Universidade de Santiago de CompostelaInventors: Juan Granja Guillán, Luis Castedo Expósito, Rebeca García Fandiño
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Patent number: 7560483Abstract: The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.Type: GrantFiled: June 21, 2005Date of Patent: July 14, 2009Assignee: XenoPort, Inc.Inventors: Mark A. Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat, Cindy X. Zhou
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Publication number: 20090171112Abstract: A process for preparing a compound (C) represented by the following formula: wherein R1 represents hydrogen, C1-6 alkyl or C3-8 cycloalkyl, and R2 represents hydrogen or methoxy, characterized by reacting a compound (A-1) represented by the following formula: wherein R1 has the same definition as above, with a compound (B) represented by the following formula: wherein R2 has the same definition as above, and L represents a leaving group, is provided. Compound (C) is effective for prevention or treatment of various diseases associated with angiogenesis neoplasia.Type: ApplicationFiled: March 9, 2009Publication date: July 2, 2009Inventors: Toshihiko Naito, Kazuhiro Yoshizawa
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Patent number: 7547780Abstract: Disclosed are new dihydropteridinones of general formula (I) whereby the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.Type: GrantFiled: December 18, 2007Date of Patent: June 16, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Grauert, Matthias Hoffman, Christian Eickmeier
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Publication number: 20090137530Abstract: A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(?O)(OH)2, X is an oxygen atom or a sulfur atom, Y is CH2CH2 or CH?CH, R1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R3 and R4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5-8.Type: ApplicationFiled: December 15, 2006Publication date: May 28, 2009Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Masatoshi Kiuchi, Kaoru Marukawa, Nobutaka Kobayashi, Kunio Sugahara
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Patent number: 7534908Abstract: An enantioselective method for producing optically active 3-alkyl carboxylic acids comprises transforming an optically active secondary alcohol into an optically active, activated compound by introducing a leaving group; reacting the activated compound with a malonic acid derivative to obtain an optically active, alkylated malonic acid compound, the reaction taking place exclusively in ether and/or carboxylic acid ester solvents and one or more aprotic polar solvents or alcohols as a cosolvent in a maximum proportion of 30 volume percent of total solvent, wherein the added cosolvent is not hexamethyl phosphoric acid triamide; the malonic acid compound is hydrolyzed if necessary to obtain the corresponding acid; and the corresponding acid is decarboxylated.Type: GrantFiled: May 12, 2005Date of Patent: May 19, 2009Assignee: Wacker Chemie AGInventors: Klas Sorger, Jürgen Stohrer
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Publication number: 20090036659Abstract: To provide a method for efficiently and industrially deuterating the benzyl position of a —O-benzyl group formed by introducing a benzyl group, a benzyloxymethyl group and the like as a protecting group. The deuteration method for the benzyl position of a —O-benzyl group of a compound having the —O-benzyl group which may have a substituent, comprising reacting the compound with a heavy hydrogen source in the coexistence of a palladium/carbon-ethylenediamine complex and hydrogen.Type: ApplicationFiled: March 2, 2007Publication date: February 5, 2009Applicant: WAKO PURE CHEMICAL INDUSTRIES, LTD.Inventors: Hironao Sajiki, Tomohiro Maegawa, Takanori Kurita
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Publication number: 20080262246Abstract: The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula II, or a salt thereof, and a compound of formula VI or a salt thereof, wherein R3 and R4 as well as Act are as defined in the specification, and processes of manufacturing these. Additionally transformation of compounds (VI) with metallo organic compounds (VII) give rise to the new compounds (VIII) which are direct precursors for the preparation of Aliskiren.Type: ApplicationFiled: October 16, 2006Publication date: October 23, 2008Inventors: Gottfried Sedelmeier, Dominique Grimler, Murat Acemoglu
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Patent number: 7414145Abstract: A method of an enantioselective nucleophilic addition reaction to carbonyl, which enables an asymmetric synthesis of an optically active ?-hydroxy-?-keto acid ester, an optically active ?-hydroxy-?-amino acid ester, hydroxydiketone compounds, etc. being useful as a raw material or synthesis intermediate for producing a pharmaceutical preparation, an agricultural chemical, a fragrance, a functional polymer or the like. In this method, the nucleophilic addition reaction of enamide compound accompanied by hydroxyl (—OH) formation to carbonyl is carried out in the presence of a chiral catalyst with copper or nickel.Type: GrantFiled: January 24, 2005Date of Patent: August 19, 2008Assignee: Japan Science and Technology AgencyInventor: Shu Kobayashi
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Publication number: 20080194860Abstract: The present invention relates to a novel crystal of the Active Pharmaceutical Ingredient (API) (S)-(+)-2-(2-chlorophenyl)-2-hydroxy-ethyl carbamate, methods for the preparation of this crystal, pharmaceutical compositions comprising this crystal, and methods of treating a patient with this crystal.Type: ApplicationFiled: October 5, 2007Publication date: August 14, 2008Applicant: TRANSFORM PHARMACEUTICALS, INC.Inventor: Michael Tauber
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Publication number: 20080146778Abstract: The present invention provides a compound having a formula: where R1 is selected from the group consisting of alkyl, CH2(OC2H4)OCH3, and —(OC2H4)OCH3; n is 0-4; Olig is an oligomer having a formula: -L-O-PAGR.R2]q where L is a optional linker moiety selected from the group consisting of —CH2O—, —CH2OX—, —OX—, —C(O)—, —C(O)X, —NH—, —NHC(O)—, —XNHC(O)—, —NHC(O)X—, —C(O)NH—, —C(O)NHX—, and where X is alky1-6 or is not present, Y is N or O or is not present, and R3 is alkyl1-6; PAG is a linear or branched polyalkylene glycol moiety; R2 is an alkyl1-22 capping moiety if X is present or alkyl2-22 if X is not present; and q is a number from 1 to the maximum number of branches on PAG; and m is 1-5.Type: ApplicationFiled: February 26, 2008Publication date: June 19, 2008Applicant: BIOCON LIMITEDInventors: Nnochiri N. Ekwuribe, Amy L. Odenbaugh
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Publication number: 20080114175Abstract: The present invention is directed to a process for preparing certain cysteine protease inhibitors.Type: ApplicationFiled: September 16, 2005Publication date: May 15, 2008Inventor: Jiayao Li