The Nitrogen Is Not Bonded Directly To A Ring Patents (Class 560/37)
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Publication number: 20110124859Abstract: The present invention relates to a process for preparing betamimetics of formula 1, wherein n denotes 1 or 2; R1 denotes hydrogen, halogen, C1-4-alkyl or O—C1-4-alkyl; R2 denotes hydrogen, halogen, C1-4-alkyl or O—C1-4-alkyl; R3 denotes hydrogen, C1-4-alkyl, OH, halogen, O—C1-4-alkyl, O—C1-4-alkylene-COOH, O—C1-4-alkylene-COO—C1-4-alkyl.Type: ApplicationFiled: February 7, 2011Publication date: May 26, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thomas KRUEGER, Uwe RIES, Juergen SCHNAUBELT, Werner RALL, Zeno A. LEUTER, Adil DURAN, Rainer SOYKA
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Patent number: 7939689Abstract: The invention provides compounds compositions and methods useful for inducing or maintaining general anesthesia or sedation in mammals.Type: GrantFiled: March 10, 2009Date of Patent: May 10, 2011Assignee: Theravance, Inc.Inventors: Thomas E. Jenkins, Sabine Axt, Jennifer Bolton
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Publication number: 20110104748Abstract: The present invention describes a process for the synthesis of a semi-synthetic ?-lactam compound from a nucleus and a side chain selected from the group consisting of D-phenylglycine and D-dihydro-phenylglycine in the form of a side chain ester and an enzyme catalyzing the coupling of the side chain ester to the nucleus characterized in that the side chain ester is not isolated as a solid intermediate.Type: ApplicationFiled: March 10, 2008Publication date: May 5, 2011Inventors: Thomas Van Der Does, Harold Monro Moody, Theodorus Johannes Godfried Maria Van Dooren
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Patent number: 7935843Abstract: The present invention relates to dephenolic compounds, an example of which is shown below, which are functionalized, and polymers formed from the same. Polymers formed from the functionalized diphenolics are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.Type: GrantFiled: December 8, 2006Date of Patent: May 3, 2011Assignee: Bezwada Biomedical, LLCInventor: Rao S Bezwada
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Publication number: 20110071310Abstract: Provided is an efficient technology for synthesizing diamino acids (diamino acid derivatives). Disclosed is a manufacturing method for diamino acid derivatives wherein the fluorenyl groups of the diamino acid derivative starting materials represented by General Formula [II] or [IV] are removed.Type: ApplicationFiled: February 27, 2009Publication date: March 24, 2011Applicant: Japan Science and Technology AgencyInventors: Shu Kobayashi, Yasuhiro Yamashita, Kazutaka Seki
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Publication number: 20110039852Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: January 29, 2009Publication date: February 17, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Jill Melissa Scott, Yen Pham Truong, Jeffrey Roger Roppe, Nicholas Simon Stock, Jeannie M. Arruda, Thomas Jon Seiders, Bowei Wang, Deborah Volkots
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Publication number: 20110034553Abstract: A conjugate comprising L-DOPA covalently linked to at least one y-aminobutyric acid (GABA) moiety, an ester and/or an addition salt thereof are disclosed, as well as uses thereof for treating a neurodegenerative disease or disorder.Type: ApplicationFiled: February 11, 2009Publication date: February 10, 2011Applicant: Ramot at Tel-Aviv University Ltd.Inventors: Gideon Stein, Abraham Nudelman, Ada Rephaeli, Irit Gil-Ad, Abraham Weizman
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Publication number: 20110034552Abstract: [Problems to be Solved] It is an object of the present invention to provide a gelator containing a long chain oxyaminopolyol capable of forming a gel with a small amount thereof over a liquid property range from acidic to alkaline, and a gel having high environmental suitability, biocompatibility and biodegradability. [Means for Solving the Problems] A gelator, characterized by containing a long chain oxyaminopolyol of Formula (I): (where R1 is a C12-16 saturated aliphatic group or a C12-16 unsaturated aliphatic group having one double bond; R2 is a substituent which an amino acid has; and X is an oxygen atom or NH) and a pharmaceutically acceptable salt thereof; a self-assembly formed by the self-assembly of the gelator; and a gel containing the gelator or the self-assembly, and water, an aqueous solution, a hydrophilic organic solvent or a hydrophilic organic solution, or a hydrophobic organic solvent or a hydrophobic organic solution.Type: ApplicationFiled: January 25, 2010Publication date: February 10, 2011Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventor: Tatsuo MARUYAMA
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Publication number: 20110027274Abstract: Antiproliferative compounds having a structure represented by formula (II), where n, R1, R2, R3, R4, and R5 are as defined herein, can be used to treat tumors, optionally when conjugated to a ligand such as an antibody:Type: ApplicationFiled: July 29, 2010Publication date: February 3, 2011Applicant: Medarex, Inc.Inventors: Heng Cheng, Qiang Cong, Sanjeev Gangwar, Qian Zhang
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Publication number: 20100311593Abstract: The invention relates to novel compounds of the formula (I), in which W, X, Y, Z and CKE are each as defined above, to several methods and intermediates for preparation thereof and to the use thereof as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions which comprise firstly haloalkylmethyleneoxyphenyl-substituted ketoenols and secondly a compound which improves crop plant compatibility. The present invention further relates to the enhancement of the action of crop protection compositions comprising especially haloalkylmethyleneoxyphenyl-substituted ketoenols, by the addition of ammonium or phosphonium salts and optionally penetration enhancers, to the corresponding compositions, to methods for production thereof and to the use thereof in crop protection as insecticides and/or acaricides and/or for preventing undesired plant growth.Type: ApplicationFiled: March 11, 2010Publication date: December 9, 2010Applicant: Bayer Cropscience AGInventors: Reiner Fischer, Thomas Bretschneider, Stefan Lehr, Eva-Maria Franken, Olga Malsam, Arnd Voerste, Ulrich Görgens, Jan Dittgen, Dieter Feucht, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Alfred Angermann
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Patent number: 7777073Abstract: This invention relates to certain hydroxyaryl alkanols, alkyl amines, alkyl amino acids, alkyl amino esters, and alkyl amino alkanols (“Hydroxyaryl compounds”) of formula (I). A method of topical application of said hydroxyaryl compounds is also disclosed.Type: GrantFiled: November 29, 2008Date of Patent: August 17, 2010Assignee: Bioderm ResearchInventor: Shyam K Gupta
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Publication number: 20100203611Abstract: The present invention provides a peptide comprising amino acid sequences R I, F I and R I G C and containing 25 or fewer amino acid residues, and capable of transporting a functional molecule into a cell, and also into a nucleus, more efficiently than a previous PTD.Type: ApplicationFiled: March 6, 2008Publication date: August 12, 2010Inventors: Yukihito Ishizaka, Masakatsu Hasegawa, Satoshi Nohara
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Patent number: 7772425Abstract: The present invention relates to novel, non-secosteroidal, diaryl compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1?,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.Type: GrantFiled: May 22, 2009Date of Patent: August 10, 2010Assignee: Eli Lilly and CompanyInventors: Emilio Enrique Bunel, Robert Peter Gajewski, Charles David Jones, Jianliang Lu, Tianwei Ma, Sunil Nagpal, Ying Kwong Yee
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Patent number: 7767811Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.Type: GrantFiled: June 5, 2006Date of Patent: August 3, 2010Assignee: Brandeis UniversityInventors: Li Deng, Jianfeng Hang, Liang Tang
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Publication number: 20100168460Abstract: A process for the enantioselective preparation of (2R,3S)-3-phenylisoserine methyl ester acetate salt of formula (I) which is an useful building block for the synthesis of taxane derivatives. The process involves the resolution of racemic threo-phenylisoserine amide and its conversion into (I).Type: ApplicationFiled: February 11, 2008Publication date: July 1, 2010Inventors: Daniele Ciceri, Bruno Gabetta, Nicola Vignola, Frieder Mitzel, Beat T. Weber
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Publication number: 20100137583Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.Type: ApplicationFiled: September 8, 2008Publication date: June 3, 2010Inventors: Robert Edward Babine, Shu-Hui Chen, Jason Eric Lamar, Nancy June Snyder, Xicheng Sun, Mark Joseph Tebbe, Frantz Victor, Q. May Wang, Yvonne Yee Mai Yip, Ivan Collado, Cristina Garcia-Paredes, Raymond Samuel Parker, III, Ling Jin, Deqi Guo, John Irvin Glass
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Publication number: 20100125146Abstract: A method of making a phenylethylamine of formula B: wherein R2, R3, R4, R5, R6, R?, R? and Rn are each independently selected from hydrogen, alkyl, acyl, aryl, amido, amino acids, sugars and nucleotides. The method includes the reduction of a compound of formula A in the absence of base: wherein R2, R3, R4, R5, R6, R?, R? and Rn are as defined above.Type: ApplicationFiled: November 19, 2008Publication date: May 20, 2010Applicant: Johnson Matthey Public Limited CompanyInventors: James J. Mencel, Paul Fishbein
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Patent number: 7718703Abstract: Norvaline derivative of the formula [I] or pharmaceutically acceptable salt thereof, method for preparing the same, pharmaceutical composition containing the same, and use of the compound for inhibiting transporting activity of glycine transporter type 2 (GlyT2) wherein X is —CH2—, —O—, —S— or single bond; Ar is optionally substituted aryl or lower cycloalkyl; n is 0 to 2; R1 and R2 are (i) each is hydrogen or lower alkyl; (ii) R1 and R2 are combined to form lower alkylene; or (iii) R1 is hydrogen or lower alkyl and R2 is combined with R4 or R6 to form lower alkylene; R3 and R4 are (i) each is hydrogen or lower alkyl; (ii) R3 and R4 are combined to form lower alkylene; or (iii) R3 is hydrogen or lower alkyl and R4 is combined with R2 or R6 to form lower alkylene; R is ?or —OR7; R5 and R6 are (i) each is optionally substituted lower alkyl, or hydrogen; (ii) R5 and R6 are combined to form aliphatic 5- to 6-membered heterocyclic group; or (iii) R5 is optionally substituted lower alkyl or hydrogen and RType: GrantFiled: January 24, 2006Date of Patent: May 18, 2010Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Naoyuki Harada, Masataka Hikota
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Publication number: 20100105097Abstract: A two-photon probe for real-time monitoring of intracellular calcium ions is provided. The two-photon probe is very suitable for real-time imaging of intracellular calcium ions, shows 20-5 O-fold TPEF enhancement in response to Ca2+, has a dissociation constant (Kd?p) of 0.14±0.02 to 0.25±0.03 ?M, and emits 5-fold stronger TPEF than currently available one-photon fluorescent Ca2+ probes. Unlike the previously available probes, the two-photon probe can selectively detect dynamic levels of intracellular free Ca2+ in live cells and living tissues without interference from other metal ions and from the membrane-bound probes. Moreover, the two-photon probe is capable of monitoring the calcium waves at a depth of 100-300 ?m in live tissues for 1,100-4,000 s using two-photon microscopy (TPM) with no artifacts of photo-bleaching. Further provided are a method for preparing the two-photon probe and a method for real-time monitoring of intracellular calcium ions using the two-photon probe.Type: ApplicationFiled: January 21, 2008Publication date: April 29, 2010Inventor: Bong-Rae Cho
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Publication number: 20100056776Abstract: Disclosed are methods of preparing a macromolecular conjugated ligand and a metal complex thereof. The metal complex is targeted for use as a contrast agent, for example, in MRI. The method of preparing a macromolecular conjugated ligand comprises: (a) providing a compound of formula (I) wherein R, A, and Pg are as defined herein, (b) reacting the compound of formula (I) with a macromolecular compound (e.g., dendrimer) in an organic solvent medium which is substantially free of water to obtain a macromolecular conjugated compound, and (c) removing the carboxyl-protecting groups to obtain a carboxyl-deprotected macromolecular conjugated compound. The metal complex can be prepared by reacting the carboxyl-deprotected macromolecular conjugated compound with an ion (e.g., Gd(III)). Also disclosed are two carboxyl-protected 1B4M-DTPA intermediate compounds.Type: ApplicationFiled: November 6, 2007Publication date: March 4, 2010Applicant: The United States of America, as represented by the Secretary, Dept. of Health and Human ServicesInventors: Martin W. Brechbiel, Heng Xu
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Publication number: 20090326058Abstract: A compound represented by the following formula (1), a pharmaceutically acceptable salt thereof or an optically active form thereof: wherein each symbol is as defined in the specification. A compound having a calcium-sensing receptor antagonistic action, a pharmaceutical composition comprising the compound, particularly a calcium receptor antagonist and a therapeutic drug for osteoporosis are provided.Type: ApplicationFiled: March 27, 2009Publication date: December 31, 2009Applicant: JAPAN TOBACCO INC.Inventors: YUKO SHINAGAWA, TERUHIKO INOUE, TOSHIHIRO KIGUCHI, TAKU IKENOGAMI, NAOKI OGAWA, KENJI FUKUDA, TAKASHI NAKAGAWA, MASANORI SHINDO, YUKI SOEJIMA
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Publication number: 20090318688Abstract: 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: May 22, 2009Publication date: December 24, 2009Applicant: 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: 20090306421Abstract: The present disclosure relates to a process for the preparation of 2-(3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)phenol or its phenolic monoesters or salts thereof, characterized by the steps of a) reacting a compound of formula (II) with a mixture of a Grignard initiator and Mg in a solvent; b) optionally reducing the temperature of the Grignard reagent to a lower temperature than in step a), and reacting the resulting Grignard reagent with an excess of a carbonate in a solvent, to obtain a compound of formula (III) wherein A is a C1-C6 alkyl, and the further reacting the compound of formula (III) in a known manner to obtain the desired end product.Type: ApplicationFiled: May 26, 2007Publication date: December 10, 2009Applicant: SCHWARZ PHARMA LTD.Inventors: Roisin Browne, Michael Kilkelly
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Publication number: 20090281347Abstract: To provide a production method of phosphates of amino acids, typified by ?-aminolevulinic acid phosphate, or esters thereof. A method for producing phosphates of an amino acid or an ester thereof, which comprises allowing an amino acid, an ester thereof or a salt thereof to coexist with phosphoric acids and a basic nitrogen-containing compound.Type: ApplicationFiled: March 1, 2007Publication date: November 12, 2009Applicant: COSMO OIL CO., LTD.Inventor: Naohisa Tachiya
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Patent number: 7592477Abstract: The present invention is related to substituted methylene amide derivatives of formula (I) and use thereof for the treatment and/or prevention of metabolic disorders mediated by insulin resistance or pyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, obesity, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of substituted methylene amide derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs. Also the present invention relates to a method of treating diabetes type II, obesity and to regulate the appetite of mammals. The present invention is furthermore related to novel substituted methylene amide derivatives and method of preparation thereof. Formula (I).Type: GrantFiled: January 27, 2003Date of Patent: September 22, 2009Assignee: Laboratoires Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Patrick Gerber, Pierre-Andre Pittet
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Publication number: 20090221640Abstract: Novel crystal modifications of (5S)-5-[4-(5-chloro-pyridin-2-yloxy)-piperidine-1-sulfonylmethyl]-5-methyl-imidazolidine-2,4-dione are disclosed together with processes for preparing such modifications, pharmaceutical compositions comprising such a modification, and the use of such a modification in therapy.Type: ApplicationFiled: March 15, 2007Publication date: September 3, 2009Applicant: ASTRAZENECA ABInventors: Lars-Erik Briggner, Anders Eriksson, Neil Barnwell, Andrea Cole, Jacob Perkins, Luis-Manuel Vaz, Andrew Wells
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Publication number: 20090221836Abstract: This invention relates to a process for preparing intermediates useful in preparing Valsartan and to a process for preparing the latter, together with synthesis intermediates of formula (IV), (V) and (VI), useful for manufacturing a medicament for the treatment of arterial hypertension or heart failure. The process for preparing Valsartan permits it to be prepared on an industrial scale with high yields and without racemisation problems, in addition to using simple and available starting products. The invention also provides a process for preparing the intermediate of formula (VI), from an intermediate of formula (V) that does not require protection of the carboxylic acid prior to N-acylation.Type: ApplicationFiled: April 18, 2005Publication date: September 3, 2009Inventors: Jordi Bessa Bellmunt, Joan Huguet Clotet, Juan Antonio Perez Andres, Pere Dalmases Barjoan
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Publication number: 20090192326Abstract: Intermediate compounds in the synthesis of Sitagliptin, 3-amino-4-(2,4,5-trifluorophenyl)but-2-enoic acid alkyl ester, and amino protected-3-amino-4-(2,4,5-trifluorophenyl)but-2-enoic acid alkyl ester, and the stereoselective reduction of these compound to give Synthon I, or the amino-protected Synthon I, are provided.Type: ApplicationFiled: November 13, 2008Publication date: July 30, 2009Inventors: Nurit Perlman, Marina Etinger, Valerie Niddam-Hildesheim, Mili Abramov
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Patent number: 7566803Abstract: The present invention relates to novel, non-secosteroidal, diaryl compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1?,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.Type: GrantFiled: November 20, 2003Date of Patent: July 28, 2009Assignee: Eli Lilly and CompanyInventor: Jianliang Lu
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Publication number: 20090186825Abstract: The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.Type: ApplicationFiled: September 26, 2008Publication date: July 23, 2009Applicant: SHIRE LLCInventors: Travis Mickle, Suma Krishnan, Barney Bishop, Christopher Lauderback, James Scott Moncrief, Robert Oberlender, Thomas Piccariello, Bernhard J. Paul, Christopher A. Verbicky
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Publication number: 20090137799Abstract: Cycloalkylcarbonylamino acid ester derivatives, which are raw material intermediates for a novel cycloalkane carboxamide derivative having an action that selectively inhibits cathepsin K, and a production process thereof, are provided. A cycloalkylcarbonylamino acid ester derivative represented by formula (I), or a pharmaceutically acceptable salt thereof: (wherein, R1 and R2 represent alkyl groups, alkenyl groups, alkynyl groups, aromatic hydrocarbon groups, heterocyclic groups, etc., R8 represents an alkyl group having 1 to 6 carbon atoms, and ring A represents a cyclic alkylidene group having 5, 6 or 7 carbon atoms).Type: ApplicationFiled: January 10, 2007Publication date: May 28, 2009Applicant: SEIKAGAKU CORPORATIONInventors: Nobuo Kobayashi, Tsuneo Koji, Hisatomo Kunii
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Patent number: 7538124Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: GrantFiled: June 24, 2008Date of Patent: May 26, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobs Jozef Backx
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Patent number: 7528276Abstract: The present invention provides a process for preparing the compounds of formula (II) according to a single reaction, which is an important intermediate compound for synthesizing GW7647 (III) and GW9578 (IV) activating Peroxisome Proliferator Activated Receptor (hPPAR ?).Type: GrantFiled: September 26, 2005Date of Patent: May 5, 2009Assignee: Seoul National University Industry FoundationInventors: Heonjoong Kang, Jungyeob Ham
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Publication number: 20090110796Abstract: The present invention relates to the use of a compound or a mixture consisting of two or more compounds or containing one or more compounds selected from the group consisting of compounds of Formulae (I) and (ent-I) wherein in Formulae (I) and (ent-I) the following applies: the aromatic radical Ar is selected from the group consisting of: wherein in the aromatic radicals A and B the following applies: R1 and R2 are selected independently of one another from the group consisting of H, OH, OCH3, OCH2CH3, OCH(CH3)2, COOCH3, COOCH2CH3, COOCH(CH3)2, or R1 and R2 are adjacent and jointly form an OCH2O group, and wherein in the aromatic radical C the following applies: X is O or S as a flavoring substance or flavoring substance mixture.Type: ApplicationFiled: October 30, 2008Publication date: April 30, 2009Applicant: SYMRISE GmbH & Co. KGInventors: Michael Backes, Tobias Vossing, Ingo Wohrle
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Patent number: 7514578Abstract: The invention relates to a method for producing enantiomeris form of 2, 3-diaminopropionic acid derivatives of formula (I) by asymetric hydrogenation from compounds of formula (II).Type: GrantFiled: January 10, 2007Date of Patent: April 7, 2009Assignee: sanofi-aventis Deutschland GmbHInventors: Joerg Rieke-Zapp, Guenter Billen
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Publication number: 20090036311Abstract: The present invention relates to benzoyl-substituted alanines of the formula I in which the variables R1 to R12 are as defined in the description, and to their agriculturally useful salts, to processes and intermediates for their preparation, and to the use of these compounds or of compositions comprising these compounds for controlling unwanted plants.Type: ApplicationFiled: February 7, 2007Publication date: February 5, 2009Applicant: BASF SEInventors: Matthias Witschel, Cyrill Zagar, Eike Hupe, Toralf Kuhn, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Robert Reinhard, Bernd Sievernich, Klaus Grossmann, Thomas Ehrhardt
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Publication number: 20090018058Abstract: The present invention relates to novel, non-secosteroidal, diaryl compounds with vitamin D receptor (VDR) modulating and psoriasis.Type: ApplicationFiled: November 20, 2003Publication date: January 15, 2009Applicant: ELI LILLY AND COMPANYInventors: Emilio Enrique Bunel, Robert Peter Gajewski, Charles David Jones, Jianliang Lu, Tianwei Ma, Sunil Nagpal, Ying Kwong Yee
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Publication number: 20080318976Abstract: ?-Hydroxy amide derivatives of the general formula (I) are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. R2a is selected from (1) a group selected from Ra. (2)(CH2)nNRbC(O)Ra. (3)(CH2)nNRbSO2Rd. (4)(CH2)nNRbCO2Ra.(5)(CH2)k-heterocycle optionally substituted with 1 to 3 groups independently selected from halogen.nitro, cyano.ORa.SRa.C1-4 alkyl and C1-3 haloakyl wherein said heterocycle is (a) a 5-membered heteroaromatic ring having a ring heteroatom selected from N.O and S. and optionally having up to 3 additional ring nitrogen atoms wherein said ring is optionally benzo-fused; or (b) a 6-membered heteromatic ring containing from 1 to 3 ring nitrogen atoms and N-oxydes thereof. Wherein said ring is optionally benzo-fused. (6)(CH2)kCO2Ra. and (7)(CH2)C(O)NRbRc.Type: ApplicationFiled: December 17, 2004Publication date: December 25, 2008Inventors: Michael R. Wood, Neville J. Anthony, Mark G. Bock, Scott D. Kuduk
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Publication number: 20080275087Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: ApplicationFiled: June 24, 2008Publication date: November 6, 2008Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx
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Patent number: 7446128Abstract: A compound which can be used as an agent for treating interstitial cystitis. An agent for treating interstitial cystitis, which comprises a phenoxyacetic acid derivative represented by a general formula (I) wherein R1 represents hydroxyl group or a lower alkoxy group, or a pharmacologically acceptable salt thereof. Since the phenoxyacetic acid derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof or a hydrate or solvate thereof has a selective ?3-adrenoceptor stimulating activity and a remarkable action to inhibit a capsaicin-sensitive sensory nerve, it can be used as a preventive or therapeutic agent for interstitial cystitis and hyperactive bladder which are accompanied by pain, other diseases in which the capsaicin-sensitive sensory nerve is concerned (e.g., acute or chronic and systemic or topical pain and inflammation) and irritable bowel syndrome (IBS) and the like.Type: GrantFiled: November 7, 2005Date of Patent: November 4, 2008Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kouichi Kaidoh, Satoshi Akahane
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Publication number: 20080255369Abstract: 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 III, wherein R, R1, and R? are as defined in the specification, or a salt thereof, and a compound of formula IV wherein R, R1, R2 and R? are as defined in the specification, and processes of manufacturing these.Type: ApplicationFiled: September 26, 2006Publication date: October 16, 2008Inventors: Stuart John Mickel, Wolfgang Marterer
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Publication number: 20080248485Abstract: The present invention provides a radiolabeled ligand which is highly selective and potent for glutamate transporters and is usable in specifically detecting the glutamate transporter. Specifically, the present invention provides a 3-[3-(benzoylamido)benzyloxy]aspartic acid having a radioactive substituent on the benzoyl group which is represented by the following formula (1), or an ester or salt thereof: wherein X represents a substituent containing a radioactive atom(s) which is selected from a straight or branched lower aliphatic alkyl group, a hydroxyl group, a straight or branched lower aliphatic alkoxy group, an amino group, a straight or branched lower aliphatic acylamido group, a halogen atom and a straight or branched lower aliphatic haloalkyl group; and R1 and R2 each represents a hydrogen atom, a straight or branched lower aliphatic alkyl group or an acetoxymethyl group.Type: ApplicationFiled: March 18, 2005Publication date: October 9, 2008Inventors: Keiko Shimamoto, Hideo Saji, Yuji Kuge, Masashi Ueda, Masamichi Satoh, Takayuki Nakagawa
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Publication number: 20080234508Abstract: Disclosed relates to a process for preparing N(5)-ethylglutamines economically without a specific purification process via a simplified and safe process, in which glutamic acid derivatives, represented by formula 1, protected by phthaloyl groups react with ethylamine to cause an amidation and a deprotection reaction in turn under the same reaction condition, thus preparing N(5)-ethylglutamines.Type: ApplicationFiled: May 18, 2006Publication date: September 25, 2008Applicants: DONGBU FINE CHEMICALS CO., LTD, CHIROCHEM CO., LTDInventors: Ho Seong Lee, Jeong Ho Song, Ho Cheol Kim
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Patent number: 7427688Abstract: The present invention provides a production method including reacting a diphenylmethylene halide compound represented by the following formula (1) with a malonic acid diester compound represented by the following formula (2) in an organic solvent selected from N-methyl-2-pyrrolidone, N-ethyl-2-pyrrolidone and N,N-dimethylformamide, in the presence of a base selected from an alkali metal hydride and an alkali metal t-butoxide to give a diester compound represented by the following formula (3), and then subjecting the diester compound to hydrolysis and decarboxylation to give a diphenylalanine compound represented by the following formula (4). According to the present invention, diphenylalanine compound (4) can be obtained industrially advantageously in a high yield. wherein each symbol is as defined in the specification.Type: GrantFiled: May 10, 2006Date of Patent: September 23, 2008Assignee: Ajinomoto Co., Inc.Inventors: Takayuki Hamada, Masanobu Yatagai
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Publication number: 20080214663Abstract: Levodopa dimethyl-substituted diester prodrugs pharmaceutical, compositions comprising levodopa dimethyl-substituted diester prodrugs, and methods of using such prodrugs and pharmaceutical compositions for treating diseases such as Parkinson's disease are provided.Type: ApplicationFiled: December 20, 2007Publication date: September 4, 2008Inventors: Jia-Ning Xiang, Cindy X. Zhou, Fenmei Yao, Mark Q. Nguyen
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Publication number: 20080199922Abstract: A process is described for the preparation of escitalopram and the pharmaceutically acceptable salts thereof starting from 5-cyanophthalide by a process which provides an enantioselective enzymatic deacylation reaction of a complex of the formula (IV) where R represents a C1-C4 alkyl residue or an aryl residue under the action of an esterase from Aspergillus niger.Type: ApplicationFiled: June 14, 2006Publication date: August 21, 2008Applicant: ADORKEM TECHNOLOGY SPAInventors: Giovanni Cotticelli, Raul Salvetti, Chiara Bertoni
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Publication number: 20080194859Abstract: The invention is directed to novel compounds that are used in the formation of polyurea compositions, including one-part and two-part polyurea compositions. The invention is also directed to polyureas formed from such compounds, cross-linked polyureas, and UV-stabilized polyureas.Type: ApplicationFiled: May 16, 2005Publication date: August 14, 2008Inventors: Kenneth I. Sawyer, Robert J. Kupper
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Patent number: 7410965Abstract: A delayed release pharmaceutical formulation containing 1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol or a pharmaceutically acceptable salt thereof in a matrix; said matrix containing from 1 to 80 wt. % of at least one pharmaceutically acceptable, matrix-forming, hydrophilic or hydrophobic polymer and having the following in vitro dissolution rate relative to 100 wt. % of the 1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol contained in the formulation: 3-35 wt. % released after 0.5 hour, 5-50 wt. % released after 1 hour, 10-75 wt. % released after 2 hours, 15-82 wt. % released after 3 hours, 30-97 wt. % released after 6 hours, more than 50 wt. % released after 12 hours, more than 70 wt. % released after 18 hours, and more than 80 wt. % released after 24 hours.Type: GrantFiled: November 29, 2004Date of Patent: August 12, 2008Assignee: Gruenenthal GmbHInventors: Johannes Bartholomaeus, Iris Ziegler
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Publication number: 20080139455Abstract: Novel compounds, compositions comprising compounds, and methods for preparing and using compounds are described herein. Methods of treating or ameliorating various conditions, including insulin resistance, pancreatic beta cell apoptosis, obesity, pro-thrombotic conditions, myocardial infarction, hypertension, dyslipidemia, manifestations of Syndrome X, congestive heart failure, inflammatory disease of the cardiovascular system, atherosclerosis, restenosis, sepsis, type 1 diabetes, liver damage, and cachexia, by administering compounds described herein. Compounds presented herein may be used to modulate serine palmitoyltransferase activity.Type: ApplicationFiled: October 12, 2007Publication date: June 12, 2008Applicant: Forbes Medi-Tech (Research), Inc.Inventor: John J. Nestor
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Publication number: 20080125483Abstract: The invention provides novel compounds of Formula (I), pharmaceutical compositions and methods of synthesis thereof.Type: ApplicationFiled: November 21, 2007Publication date: May 29, 2008Inventors: Jenn-Tsang Hwang, Chrong-Shiong Hwang, Yow-Lone Chang, Chung-Niang Yao