Oxy In Acid Moiety Patents (Class 560/39)
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Publication number: 20110269848Abstract: Biocompatible, bioresorbable polymers comprising a plurality of monomeric repeating units containing an amide group, wherein said amide groups are N-substituted and the N-substituent and degree of N-substitution are effective to lower the melt viscosity, the solution viscosity, or both, compared to the same polymer without N-substitution.Type: ApplicationFiled: July 14, 2011Publication date: November 3, 2011Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: Joachim B. Kohn, Durgadas Bolikal, Jaap Schut, Ernest G. Baluca
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Publication number: 20110263626Abstract: The present invention relates to compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7 and R8 are defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.Type: ApplicationFiled: August 28, 2008Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert Hauel, Angelo Ceci, Enzo Cereda, Henri Doods, Ingo Konetzki, Juergen Mack, Henning Priepke, Annette Schuler-metz, Rainer Walter
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Publication number: 20110263658Abstract: The present invention relates to biphenyl-based renin inhibitor compounds having amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: August 18, 2008Publication date: October 27, 2011Inventors: Helene Juteau, Michel Gallant, Daniel Dube, Patrick Roy, Renee Aspiotis, Rejean Fortin, Patrick Lacombe, Daniel McKay, Tom Yao-Hsiang Wu
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Publication number: 20110263539Abstract: The present invention provides the use of pelorol analogs of Formula, (I) and pharmaceutical compositions thereof as modulators of SHIP 1 activity. A compound or a pharmaceutical composition of the present invention may be used for the treatment or prophylaxis of an inflammatory, neoplastic, hematopoetic or immune disorder or condition in addition to other disorders and conditions.Type: ApplicationFiled: June 21, 2007Publication date: October 27, 2011Applicant: THE UNIVERSITY OF BRITISH COLUMBIAInventors: Raymond Andersen, Matthew Nodwell, Alice Mui
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Publication number: 20110257408Abstract: A process for preparing an enantiomerically enriched cycloalkene-substituted alanine compound having the structure: by asymmetrically hydrogenating a dehydro amino acid compound having the structure: in a suitable reaction media in the presence of a catalyst having a transition metal moiety complexed to a chiral phosphine ligand to prepare enantiomerically enriched cycloalkene substituted alanine compounds having the structure of Formula (IA) or (IB), which are key intermediates for the ACE inhibitors ramipril and perindolpril:Type: ApplicationFiled: April 20, 2011Publication date: October 20, 2011Applicant: Chiral Quest, Inc.Inventors: Zijun Liu, Sanhui Lin, Wenge Li, Jingyang Zhu, Xinjun Liu, Xiaojuan Zhang, Hui Lu, Fei Xiong, Zhongwei Tian
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Publication number: 20110223254Abstract: 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: ApplicationFiled: March 25, 2011Publication date: September 15, 2011Applicant: BEZWADA BIOMEDICAL, LLCInventor: Rao S. Bezwada
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Publication number: 20110171150Abstract: A compound of the formula (I): where m is an integer equal to 0 or 1, and p is an integer equal to 0, 1, 2 or 3. A method for preparing the compound of the formula (I), and the use thereof as a skin lightening agent. A cosmetic composition and a drug containing the compound of the formula (I).Type: ApplicationFiled: September 14, 2009Publication date: July 14, 2011Applicant: SOCIETE DEXPLOITATION DE PRODUITS POUR LES INDUSTRIES CHIMQUES SEPPICInventors: Sandy Dumont, Cecile Taillebois, Jerome Guilbot, Corinne Stoltz, Sebastien Kerverdo
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Patent number: 7973181Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers: wherein Y1 is a bond, —(C?O)—, —S(O2)—, —C(?O)O—, —OC(?O)—, —(C?O)NR3—, —NR3(C?O)—, —S(O2)NR3—, —NR3S(O2)—, or —NR3(C?O)NR5—, wherein R3 and R5 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p wherein m, n, p, Alk1, Alk2 and Q are as defined in the claims; z is 0 or 1; A represents an optionally substituted mono-, bi— or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker]- represents a divalent linker radical; R is a radical of formula (X) or (Y): wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, —(C?O)R3, —(C?O)OR3, or —(C?O)NR3 wherein RType: GrantFiled: May 4, 2006Date of Patent: July 5, 2011Assignee: Chroma Therapeutics Ltd.Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, David Festus Charles Moffat
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Patent number: 7968597Abstract: (2R)-2-Phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and crystalline form thereof, methods of making the same, pharmaceutical compositions thereof, and methods of using the same to treat diseases or disorders such as Parkinson's disease are provided.Type: GrantFiled: December 31, 2008Date of Patent: June 28, 2011Assignee: XenoPort, Inc.Inventors: Jia-Ning Xiang, Xuedong Dai, Cindy X. Zhou, Jianhua Li, Mark Q. Nguyen
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Publication number: 20110137025Abstract: The disclosure provides metal organic frameworks useful for sensing, gas sorption, microelectronics and switches.Type: ApplicationFiled: June 5, 2009Publication date: June 9, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Omar M Yaghi, Qiaowei Li, Ognjen S Miljanic, Wenya Zhang, James Frasere Stoddart
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Patent number: 7956212Abstract: Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.Type: GrantFiled: February 2, 2009Date of Patent: June 7, 2011Assignee: XenoPort, Inc.Inventors: Jia-Ning Xiang, Mark A. Gallop, Cindy X. Zhou, Mark Nguyen, Xuedong Dai, Jianhua Li, Kenneth C. Cundy, Nelson L. Jumbe
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Publication number: 20110063388Abstract: A polymerizable Type II photoinitiator according to Formula (I): wherein: A represents a Norrish Type II initiating group; L represents a divalent linking group positioning the Norrish Type II initiating group A and the CR2R3-group in a 1-5 to a 1-8 position wherein position 1 is defined as the first atom in the aromatic or alicyclic ring of A to which L is covalently bonded and the position 5 to 8 is defined as the carbon atom of the CR2R3-group to which L is covalently bonded, with the proviso that L does not contain an amine. Radiation curable compositions and inks include the multifunctional Type II photoinitiator.Type: ApplicationFiled: May 28, 2009Publication date: March 17, 2011Applicant: AGFA GRAPHICS NVInventors: Johan Loccufier, Jaymes Van Luppen
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Patent number: 7906675Abstract: A biologically active agent, wherein the agent is a compound of the formula: Wherein A, R5, R9, X, Q and n, m, q are defined herein below.Type: GrantFiled: August 16, 2004Date of Patent: March 15, 2011Assignee: Wellstat Therapeutics CorporationInventor: Shalini Sharma
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Patent number: 7902394Abstract: Novel calcilytic compounds of Formula (I), pharmaceutical compositions, methods of synthesis, and methods of using them are provided.Type: GrantFiled: December 18, 2007Date of Patent: March 8, 2011Assignee: GlaxoSmithKline LLCInventors: Robert W. Marquis, Jr., Joshi M. Ramanjulu, Robert Trout
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Publication number: 20110020324Abstract: A compound having an ability to bind to an S1P receptor (particularly EDG-6, preferably EDG-1 and EDG-6), for example, the compound represented by formula (I) of the present invention, a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like. wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.Type: ApplicationFiled: September 10, 2010Publication date: January 27, 2011Applicant: ONO PHARMACEUTICAL CO., LTDInventors: Shinji NAKADE, Hirotaka Mizuno, Takeji Ono, Masashi Minami, Hiroshi Saga, Hiroshi Hagiya, Takaki Komiya, Hiromu Habashita, Haruto Kurata, Kazuhiro Ohtsuki, Kensuke Kusumi
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Publication number: 20110015425Abstract: The present invention relates to improved processes for the production of 2-amino-2-[2-(4-C2-20-alkyl-phenyl)ethyl]propane-1,3-diols, and to compounds for use therein.Type: ApplicationFiled: March 17, 2009Publication date: January 20, 2011Inventor: Gottfried Sedelmeier
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Patent number: 7872151Abstract: The present invention relates to a phenylalanine derivative of Formula (I) wherein X1 is a halogen atom, X2 is a halogen atom, Q is a CH2R— is a carboxyl group which may be esterified; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 7, 2010Date of Patent: January 18, 2011Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Takayuki Kawaguchi, Sumihiro Nomura, Mikiko Tsukimoto, Toshiyuki Kume, Ila Sircar
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Publication number: 20100317854Abstract: The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.Type: ApplicationFiled: August 23, 2010Publication date: December 16, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Cristina Alonso-Alija, Markus Heil, Dietmar Flubacher, Paul Naab, Josef Pernerstorfer, Johannes-Peter Stasch, Frank Wunder, Klaus Dembowsky, Elizabeth Perzborn, Elke Stahl
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Publication number: 20100311827Abstract: The invention provides chlorogenic acid derivatives of Formula (I) that are capable of inhibiting the growth of fungal cells and are useful as anti-fungal agents. The invention further provides the methods of inhibiting the growth of fungal cells and methods of treating a fungal infection in an animal by administering to the animal an effective amount of a compound of Formula I, either alone or in combination with another anti-fungal agent.Type: ApplicationFiled: July 23, 2007Publication date: December 9, 2010Inventors: Mohsen Daneshtalab, Chao-Mei Ma
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Publication number: 20100292480Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.Type: ApplicationFiled: September 11, 2008Publication date: November 18, 2010Applicant: Gilead Sciences, IncInventors: Eric Dowdy, Steven Pfeiffer
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Publication number: 20100280108Abstract: A compound of general formula (I) wherein, R11, R12, R13, R14, R15, W, Y, R1, R2, R3, R4, R5, and R6 take various meanings for use in the treatment of cancer.Type: ApplicationFiled: December 19, 2008Publication date: November 4, 2010Applicant: Pharma Mar, S.A.Inventors: Alberto Rodriguez Vicente, Maria Garranzo García-Ibarrola, Carmen Murcia Pérez, Francisco Sánchez Sancho, Maria del Carmen Cuevas Marchante, Cristina Mateo Urbano, Isabel Digón Juárez
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Publication number: 20100274026Abstract: The object of the present invention is to provide a pharmaceutical composition for preventing or treating viral infectious diseases. The compounds of the present invention have extremely potent anti-HCV activity and HCV growth inhibitory effects, and since they also only demonstrate mild cytotoxicity in vivo, a pharmaceutical composition containing the compound of the present invention is extremely useful as an anti-HCV preventive/therapeutic agent.Type: ApplicationFiled: July 6, 2010Publication date: October 28, 2010Inventors: Masahiro Aoki, Hideyuki Kato, Masayuki Sudoh, Takuo Tsukuda, Miyako Masubuchi, Kenichi Kawasaki
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Publication number: 20100204271Abstract: Provision of a stabilized crystal of 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound A). A crystal of compound A, which shows a particular X-ray powder diffraction pattern of a characteristic diffraction peaks at diffraction angles 2?(°) as measured by X-ray powder diffractometry.Type: ApplicationFiled: August 10, 2009Publication date: August 12, 2010Inventors: MOTOHIDE SATOH, TAKAHISA MOTOMURA, TAKASHI MATSUDA, KENTARO KONDO, KOJI ANDO, KOJI MATSUDA, SHUJI MIYAKE, HIDETO UEHARA
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Publication number: 20100190852Abstract: The present invention relates to the use of a pharmaceutically effective amount of an short-acting calcium channel blocking compound to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension before, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.Type: ApplicationFiled: June 19, 2008Publication date: July 29, 2010Applicant: MILESTONE PHARMACEUTICALS INC.Inventors: Martin P. Maguire, Elise Rioux, Harry J. Leighton
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Publication number: 20100190725Abstract: Compounds of formula (I) or formula (II) have dopaminergic activity: wherein: R1 is a carboxyl, carboxyl ester, or carboxamide group; R2 is a group —C(?O)—NR3R4, or —S(?O)2—NR3R4; R3 and R4 are independently selected from hydrogen, optionally substituted C1-C6 alkyl, (C1-C5 fluoroalkyl)-CH2—, -Q, and —CH2Q, wherein Q is an optionally substituted monocyclic carbocyclic or heterocyclic ring of (3) to (6) ring atoms; or R3 and R4 together with the nitrogen to which they are attached form an optionally substituted monocyclic cycloalkyl or non-aromatic heterocyclic ring of (3) to (8) ring atoms; R5 is hydrogen, or a natural or non-natural alpha amino acid residue linked via a peptide bond; R6 is hydrogen or a group R7C(?O)—; and R7 is C1-C6 alkyl, C1-C6 fluoroalkyl or cyclopropyl.Type: ApplicationFiled: July 4, 2008Publication date: July 29, 2010Applicant: PROXIMAGEN LTD.Inventor: Christopher Hobbs
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Publication number: 20100179216Abstract: Provided is a novel amine compound represented by the following formula (I) having a superior peripheral blood lymphocyte decreasing action and superior in the immunosuppressive action, rejection suppressive action and the like, which shows decreased side effects of, for example, bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof. wherein each symbol is as defined in the specification.Type: ApplicationFiled: June 13, 2008Publication date: July 15, 2010Inventors: Masatoshi Kiuchi, Kaoru Tashiro, Maiko Hamada, Kunio Sugahara
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Publication number: 20100174084Abstract: The invention relates to novel 2-alkoxy-6-alkylphenyl-substituted spirocyclic tetramic acid derivatives of the formula (I) in which A, B, D, G, X, Y and Z are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the 2-alkoxy-6-alkylphenyl-substituted spirocyclic tetramic acid derivatives of the formula (I) and, secondly, at least one crop plant tolerance promoter compound.Type: ApplicationFiled: March 16, 2010Publication date: July 8, 2010Applicant: Bayer CropScience AGInventors: Reiner FISCHER, Stefan Lehr, Mark Wilhelm Drewes, Dieter Feucht, Olga Malsam, Guido Bojack, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Chris Rosinger
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Publication number: 20100113778Abstract: An improved process for preparing o-chloromethylphenylglyoxylic esters of the formula which comprises converting a compound of the formula by reaction with magnesium into the corresponding Grignard reagent which is then reacted with a compound of the formula to give the compound of the formula which is then cleaved by reaction with a chloroformic ester of the formula CICOOR4 or by reaction with phosgene to give the compound of the formula (I), followed by the isolation of the compound of the formula (I), and also an improved process for preparing (E)-2-(2-chloromethylphenyl)-2-alkoximinoacetic esters of the formula and intermediates for their preparation.Type: ApplicationFiled: April 10, 2008Publication date: May 6, 2010Inventors: John-Matthias Wiegand, Karsten Luettgen, Wolfgang Skranc
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Publication number: 20100063242Abstract: The present invention is directed to polyarylates comprising repeating units having the structure: as well as their preparation and use as cell growth substrates.Type: ApplicationFiled: July 31, 2009Publication date: March 11, 2010Applicant: Rutgers, The State University of New JerseyInventors: Ken James, Brochini Stephen, Varawut Tangpasuthadol, Joachim B. Kohn
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Patent number: 7671090Abstract: The present invention relates to a phenylalanine derivative of Formula (I) wherein X1 is a halogen atom, X2 is a halogen atom, Q is a CH2R— is a carboxyl group which may be esterified; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 7, 2008Date of Patent: March 2, 2010Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Takayuki Kawaguchi, Sumihiro Nomura, Mikiko Tsukimoto, Toshiyuki Kume, Ila Sircar
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Patent number: 7666906Abstract: L-threo-?-benzyloxyaspartate derivatives having a substituent on the benzene ring, represented by the following formula (1): wherein R is hydrogen, a linear or branched lower aliphatic acyl group with the acyl portion optionally substituted, an alicyclic acyl group, an aromatic acyl group with a substituent on the aromatic ring, an amino acid-derived group or a biotin derivative-derived group, having an amino substituent on the benzene ring, and salts thereof, which can easily bind to affinity column chromatography carriers as ligands of glutamate transporter proteins.Type: GrantFiled: June 14, 2007Date of Patent: February 23, 2010Assignee: Suntory Holdings LimitedInventor: Keiko Shimamoto
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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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Publication number: 20100016403Abstract: Compounds of Formula I are useful for the treatment of anxiety disorders such as generalized anxiety disorder (GAD), panic attack, post traumatic stress disorder (PTSD), obsessive compulsive disorder (OCD) and social phobias. wherein: A is chosen from: aryl or heteroaryl, A being optionally substituted with up to 5 independently-selected groups R8; R1 is chosen from: alkyl or haloalkyl; R2 is chosen from: H, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7; R3, R4 and R5 are independently chosen from: H or alkyl; R6 and R7 are independently chosen from: H or alkyl; and R8 is chosen from: OH, CN, halo, alkyl, alkoxy, haloalkyl, haloalkoxy, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7.Type: ApplicationFiled: December 14, 2007Publication date: January 21, 2010Inventors: Guy Higgins, Abdelmalik Slassi, Methvin Isaac
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Publication number: 20100010010Abstract: Compounds of formula (I) inhibit HDAC activity, wherein A, B and D independently represent ?C— or ?N—; W is a divalent radical —CH?CH— or CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.Type: ApplicationFiled: September 14, 2007Publication date: January 14, 2010Applicant: CHROMA THERAPEUTICS LTD.Inventors: Alan Hornsby Davidson, David Festus Charles Moffat, Francesca Ann Day, Alastair David Graham Donald
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Publication number: 20100010000Abstract: An amino alcohol derivative useful as an excellent immunosuppressive agent is provided. As a result of intensive research to create a highly safe compound which has an excellent immunosuppressive activity, it was discovered that an amino alcohol derivative represented by the general formula (1), has excellent immunosuppressive activity.Type: ApplicationFiled: August 7, 2007Publication date: January 14, 2010Inventors: Yasushi Kohno, Kiyoshi Fujii, Tatsuhiro Saito, Kazuhiko Kuriyama, Tokutarou Yasue
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Publication number: 20090318702Abstract: The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, the present invention provides, for example, compounds represented by the formulas (6), (7-1), (7-2) and (8): wherein R is a fluorine atom or a methoxy group, R1 is a C1-C4 alkyl group, R2 is a hydroxyl-protecting group, and X2 is a halogen atom, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.Type: ApplicationFiled: March 6, 2007Publication date: December 24, 2009Inventors: Koji Matsuda, Koji Ando, Shigeji Ohki, Takahiro Yamasaki, Jun-ichi Hoshi
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Publication number: 20090298924Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers: wherein Y1 is a bond, —(C?O)—, —S(O2)—, —C(?O)O—, —OC(?O)—, —(C?O)NR3—, —NR3(C?O)—, —S(O2)NR3—, —NR3S(O2)—, or —NR3(C?O)NR5—, wherein R3 and R5 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent radical of formula -(Alk1)m(O)n(Alk2)p— wherein m, n, p, Alk1, Alk2 and Q are as defined in the claims; z is 0 or 1; A represents an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker]- represents a divalent linker radical; R is a radical of formula (X) or (Y): wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, —(C?O)R3, —(C?O)OR3, or —(C?O)NR3 wherein RType: ApplicationFiled: May 4, 2006Publication date: December 3, 2009Applicant: Chroma Therapeutics LtdInventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, David Festus Charles Moffat
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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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Publication number: 20090281103Abstract: The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: July 20, 2006Publication date: November 12, 2009Inventors: Christopher I. Bayly, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
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Publication number: 20090239832Abstract: The present invention relates to nitrooxyderivatives or salts thereof having the following general formula (I): R—NR1c—(K)k0—(B)b0—(C)c0—NO2??(I) wherein c0, b0 and k0 are 0 or 1; R is the radical of an analgesic drug for chronic pain, for instance neurophatic pain; R1c is H or alkyl with from 1 to 5 carbon atoms; B is such that its precursor is selected from amino acids, hydroxy acids, polyalcohol, compounds; C is a bivalent radical containing an aliphatic, heterocyclic or aromatic radical.Type: ApplicationFiled: June 2, 2009Publication date: September 24, 2009Applicant: NICOX SAInventors: Ennio Ongini, Nicoletta Almirante, Piero Del Soldato
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Publication number: 20090203906Abstract: The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.Type: ApplicationFiled: April 13, 2009Publication date: August 13, 2009Applicant: Bayer AktiengesellschaftInventors: Cristina Alonso-Alija, Markus Heil, Dietmar Flubacher, Paul Naab, Josef Pernerstorfer, Johannes-Peter Stasch, Frank Wunder, Klaus Dembowsky, Elizabeth Perzborn, Elke Stahl
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Publication number: 20090203663Abstract: The present invention relates to compounds that inhibit a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins.Type: ApplicationFiled: February 7, 2007Publication date: August 13, 2009Applicant: AstraZeneca ABInventors: Jean Claude Arnould, Benedicte Delouvrie, Jason Grant Kettle
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Publication number: 20090198050Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.Type: ApplicationFiled: October 31, 2008Publication date: August 6, 2009Inventors: Eric Marsault, Luc Ouellet, Carl St-Louis, Sylvie Beaubien, Kamel Benakli, Hamid R. Hoveyda, Mark L. Peterson, Shridhar Bhat
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Publication number: 20090184294Abstract: Described are antioxidant macromolecules and methods of making and using same.Type: ApplicationFiled: January 5, 2009Publication date: July 23, 2009Inventors: Ashok L. Cholli, Rajesh Kumar
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Patent number: 7563821Abstract: (2R)-2-Phenylcarbonyloxypropyl(2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and crystalline form thereof, methods of making the same, pharmaceutical compositions thereof, and methods of using the same to treat diseases or disorders such as Parkinson's disease are provided.Type: GrantFiled: December 4, 2006Date of Patent: July 21, 2009Assignee: XenoPort, Inc.Inventors: Jia-Ning Xiang, Xuedong Dai, Cindy X. Zhou, Jianhua Li, Mark Q. Nguyen
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Publication number: 20090156585Abstract: A specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi are used in the treatment of hypertension.Type: ApplicationFiled: November 8, 2006Publication date: June 18, 2009Inventors: Lili Feng, Sven Erik Godtfredsen, Bin Hu, Yugang Liu, Piotr Karpinski, Paul Allen Sutton, Mahavir Prashad, Michael J. Girgis, Thomas J. Blacklock
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Patent number: 7544833Abstract: Disclosed are improved methods for the synthesis of N-(8-[2-hydroxybenzoyl]-amino)caprylic acid. Certain compounds have been found useful for preventing the formation of a colored impurity when included in an ester hydrolysis reaction. Conducting ester hydrolysis in anaerobic conditions has also been found to minimize the formation of the color impurity. Also disclosed are improved methods for synthesizing the sodium salt of N-(8-[2-hydroxybenzoyl]-amino)caprylic acid.Type: GrantFiled: August 30, 2007Date of Patent: June 9, 2009Assignees: Hoffmann-La Roche Inc., Emisphere Technologies, Inc.Inventors: William Elliott Bay, Joseph Norman Bernadino, George Frederick Klein, Yi Ren, Pingsheng Zhang
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Patent number: 7514555Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyper-lipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed.Type: GrantFiled: April 8, 2004Date of Patent: April 7, 2009Assignee: Wellstat Therapeutics CorporationInventors: Kirvin L. Hodge, Shalini Sharma, Reid W. von Borstel, Stephen D. Wolpe
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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: 20090082589Abstract: Provided are compounds of formula A and formula I: A compound of formula A: wherein n is an integer from 6 to 17 and a compound of formula I:Type: ApplicationFiled: November 14, 2008Publication date: March 26, 2009Inventors: Bernd Junker, Javier Manero