Chalcogen Or Nitrogen Attached Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/491)
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Publication number: 20130025618Abstract: The present invention relates to a cationic 4-aminoindole of general formula (I), addition salts thereof with an acid and solvates thereof: in which: R1 is a linear or branched, saturated C2-C20 alkyl radical, substituted and/or interrupted with a cationic radical. The present invention is also directed towards a process for synthesizing this cationic 4-aminoindole, to the compositions, the uses, the hair dyeing processes and the devices using this cationic 4-aminoindole.Type: ApplicationFiled: December 6, 2010Publication date: January 31, 2013Inventor: Aziz Fadli
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Patent number: 8362112Abstract: The present invention relates to cure accelerators useful for anaerobic curable compositions, such as adhesives and sealants. The cure accelerators are constructed as urethane/urea/thiourethane (meth)acrylate resins from diols and include a unit embraced within structure A where X is C1-20 alkyl, C2-20 alkenyl, or C7-20 alkaryl, any of which may be interrupted by one or more hereto atoms, and which are functionalized by at least one and preferably at least two groups selected from —OH, —NH2 or —SH and z is 1-3.Type: GrantFiled: October 28, 2011Date of Patent: January 29, 2013Assignees: Henkel Ireland Limited, Henkel CorporationInventors: David P. Birkett, Martin Wyer, Andrew Messana, David P. Dworak, Anthony F. Jacobine
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Patent number: 8350047Abstract: The present application relates to novel methods for the preparation of secondary carbinamine compounds, particularly the preparation of secondary carbinamine compounds of the formula Ia, formula Ib or formula IV from aldehydes of the formula II and boronic acids of the formula III or formula V, in the presence of ammonia or an ammonia equivalent of the formula NH4+X?.Type: GrantFiled: March 28, 2008Date of Patent: January 8, 2013Inventors: Avinash N. Thadani, Bhartesh Dhudshia
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Publication number: 20120330008Abstract: A novel process is described for the preparation of pharmaceutically useful compounds such as 1-{4-[2-(azepan-1-yl)ethoxy]benzyl}-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol acetic acid commonly known as bazedoxifene acetate of the formula-1 using 2-(4-{[5-(benzyloxy)-2-[4-(benzyloxy)phenyl]-3-methyl-1H-indol-1-yl]methyl}phenoxy)ethyl-4-methylbenzenzene-1-sulfonate (formula 2a)Type: ApplicationFiled: September 8, 2011Publication date: December 27, 2012Applicant: DIVI'S LABORATORIES LIMITEDInventors: Murali Krishna Prasad Divi, Gundu Rao Padakandla, Bolneni Nageswara Rao, Dandu Venkata Suresh
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Publication number: 20120318348Abstract: Photoactive layers for use in a photovoltaic cell are described. The photoactive layers comprise at least one photoactive ion paired with another ion. This photoactive ion pair can be in the form of an ionic liquid, hydrogen bonded ion pair, cocrystal, or complex to allow for greater flexibility and portability. Also described are photovoltaic cells that contain the described photoactive layers sandwiched between two electrodes.Type: ApplicationFiled: June 18, 2012Publication date: December 20, 2012Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ALABAMAInventors: Rachel M. Frazier, Daniel T. Daly, Scott K. Spear, Robin D. Rogers, Whitney Hough
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Patent number: 8324384Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: February 3, 2010Date of Patent: December 4, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Songnian Lin, Xibin Liao, Edward Metzger, Emma R. Parmee, Sheryl D. Debenham
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Publication number: 20120252792Abstract: The invention provides methods, compositions, and kits for the inhibition of members of the Rho GTPase family. Specifically, the invention provides methods, compositions and kits for the inhibition of RhoA and/or RhoC transcriptional signalling. The invention finds use in treatment of Rho-mediated disease states (e.g., tumor metastasis, inflammation, inflammatory disease), Rho-mediated biological conditions, and in cell signaling research.Type: ApplicationFiled: September 17, 2010Publication date: October 4, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Richard Neubig, Chris Evelyn, Jenny Ryu, Scott Larsen, Jessica Bell
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Publication number: 20120220782Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, or especially of amides of the formula II, wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.Type: ApplicationFiled: April 30, 2012Publication date: August 30, 2012Inventors: Ulrich BERENS, Oliver DOSENBACH, Daniel SPRENGER
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Publication number: 20120214770Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.Type: ApplicationFiled: May 1, 2012Publication date: August 23, 2012Applicant: BIONOMICS LIMITEDInventors: JASON HUGH CHAPLIN, GURMIT SINGH GILL, DAMIAN WOJCIECH GROBELNY, BERNARD LUKE FLYNN, GABRIEL KREMMIDIOTIS
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Publication number: 20120196884Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).Type: ApplicationFiled: June 14, 2010Publication date: August 2, 2012Applicant: BIOTIE THERAPIES CORPORATIONInventors: Jarkko Tapani Koivunen, Jani Korhonen, Anne Marjamäki, Liisa Nissinen, Marjo Pihlavisto, Olli Taneli Pentikäinen
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Patent number: 8232312Abstract: The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.Type: GrantFiled: March 14, 2008Date of Patent: July 31, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
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Publication number: 20120190820Abstract: Provided are methods for forming a reactive S-nitroso thioacid (NTA), comprising nitrosation of a thioacid with a nitrosation reagent. Also provided are methods for: acylating a nucleophile including selective acylation with a high degree of selectivity toward amines over hydroxyls; amide or peptide bond formation; forming a dipeptide or polypeptide; and peptide coupling/ligation, comprising use of thioacid and amine starting materials, wherein the reactions are mediated by very reactive S-nitroso thioacid (NTA) intermediates enabling extremely fast reactions under mild conditions, providing for broad applications.Type: ApplicationFiled: January 26, 2012Publication date: July 26, 2012Inventors: Ming Xian, Jia Pan
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Patent number: 8222417Abstract: The present invention provides compounds having excellent 11?-HSD1 inhibitory activity. A compound represented by the following formula (I): [wherein X1 represents an oxygen atom, or the formula —(CR11R12)p—, etc., Y1 represents a hydrogen atom, a hydroxyl group, etc., Z1 represents an oxygen atom or the formula —(NR14)—, R1 represents a hydrogen atom, a halogen atom, a cyano group, a C1-4 alkyl group, a C1-4 alkyl group substituted with 1 to 3 halogen atoms, a C1-4 alkoxy group, a C1-4 alkoxycarbonyl group, a carboxyl group, a carbamoyl group, or an amino group, and m represents an integer of 1 or 2, and R2 represents a hydrogen atom or a C1-4 alkyl group, and n represents an integer of 1 or 2].Type: GrantFiled: June 24, 2008Date of Patent: July 17, 2012Assignee: Taisho Pharmaceutical Co., LtdInventors: Ryo Suzuki, Ayako Mikami, Hiroaki Tanaka, Hiroshi Fukushima
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Publication number: 20120165548Abstract: Processes for the preparation of Silodosin and its intermediates comprising reductive amination of compound of Formula (VIII) with a compound of Formula (VII) or a compound of Formula (XV) in a suitable solvent using a reducing agent.Type: ApplicationFiled: September 13, 2010Publication date: June 28, 2012Applicant: SANDOZ AGInventors: Shreerang Joshi, Sachin Bhuta, Sanjay Talukdar, Sudhir Sawant, Deepak Venkataraman, Abhinay Pise, Shashikant Metkar, Dattatraya Chavan, Parven Kumar Luthra
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Publication number: 20120157387Abstract: Provided are compounds which are prodrugs of D-gamma-glutamyl-D-tryptophan, methods of making the compounds and methods for using the compounds.Type: ApplicationFiled: February 20, 2012Publication date: June 21, 2012Applicant: APOTEX TECHNOLOGIES INC.Inventors: Tim Fat TAM, Regis Leung-Toung, Yingsheng Wang, Yanqing Zhao, Tao Xin, Wanren Li, Jolanta Maria Wodzinska, Vrajlal S. Rabadia, Birenkumar Shah, Christopher John Feeney
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Publication number: 20120157641Abstract: The present invention relates to cure accelerators useful for anaerobic curable compositions, such as adhesives and sealants.Type: ApplicationFiled: October 7, 2011Publication date: June 21, 2012Applicants: Loctite (R&D) Limited, Henkel CorporationInventors: David Birkett, Martin Wyer, Andrew Messana, Philip Klemarczyk, Anthony F. Jacobine
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Publication number: 20120108631Abstract: The invention relates to sulfonamide compounds and methods for activating PKM2. The compounds and methods are useful in treating or preventing a disease or disorder selected from cancer, cell proliferative disorder, inflammatory disorder, metabolic disorder, and immune system disorder.Type: ApplicationFiled: October 26, 2011Publication date: May 3, 2012Inventors: Oren M. Becker, Alina Shitrit, Nili Schutz, Efrat Ben-Zeev, Avihai Yacovan, Rachel Ozeri, Tzofit Kehat, Sima Mirilashvili, Alex Aizikovich, Daniel Sherman, Vered Behar, Osnat Kashtan
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Patent number: 8163932Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: GrantFiled: February 8, 2010Date of Patent: April 24, 2012Assignee: Alinea Pharmaceuticals, Inc.Inventors: Michael Lee Jones, David Gunn, John Howard Jones, Michael C. Van Zandt
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Publication number: 20120095048Abstract: The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds.Type: ApplicationFiled: February 19, 2010Publication date: April 19, 2012Applicants: REGION MIDT JYLLAND, AARHUS UNIVERSITETInventors: Henrik Amtoft Neubauer, Ove Kjaer Wiborg, Henrik Helligsø Jensen
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Patent number: 8143259Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, L, Q, R1, R2, and R3 are defined herein.Type: GrantFiled: August 11, 2009Date of Patent: March 27, 2012Assignee: Janssen Pharmaceutica, NVInventors: Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Donald W. Ludovici, Jay M. Matthews, Mingde Xia, Xiaoqing Xu, Mark A. Youngman, Bin Zhu
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Publication number: 20120046307Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.Type: ApplicationFiled: October 16, 2009Publication date: February 23, 2012Applicant: UNIVERSITAET DES SAARLANDESInventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
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Patent number: 8115014Abstract: As a compound having a potent oral activity and a long-lasting cysLT1/cysLT2 receptor antagonistic activity, the compound of the formula (I): which exhibits potent antagonistic activity against the cysLT1/cysLT2 receptor, and have long-lasting effects even in case of oral administration, and therefore is useful as an oral agent for preventing and/or treating a variety of diseases, for example, respiratory disease (for example, asthma (bronchial asthma, etc.), chronic obstructive pulmonary disease (COPD), pulmonary emphysema, chronic bronchitis, pneumonia (interstitial pneumonia, etc.), severe acute respiratory syndrome (SARS), acute respiratory distress syndrome (ARDS), apnea syndrome, allergic rhinitis, sinusitis (acute sinusitis, chronic sinusitis, etc.), pulmonary fibrosis, coughing (chronic coughing, etc.), and the like) was developed.Type: GrantFiled: December 22, 2009Date of Patent: February 14, 2012Assignee: ONO Pharmaceuticals, Co., Ltd.Inventors: Kazuyuki Ohmoto, Satoshi Itadani, Yoshisuke Nakayama, Jun Takeuchi, Manabu Fujita
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Patent number: 8115013Abstract: The present invention relates to a novel process for the preparation of the HMG-CoA reductase inhibitor, fluvastatin, more specifically to a process for the preparation of amorphous form of fluvastatin sodium.Type: GrantFiled: October 5, 2004Date of Patent: February 14, 2012Assignee: Biocon LimitedInventors: Sumithra Srinath, Tom Thomas Puthiaprampil, Ravindra Chandrapa, Sambasivam Ganesh
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Publication number: 20120034270Abstract: The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with in-appropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.Type: ApplicationFiled: October 16, 2009Publication date: February 9, 2012Applicant: Akaal Pharma Pty LtdInventors: Damian W. Grobelny, Gurmit S. Gill
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Publication number: 20120035373Abstract: The present invention relates to processes of producing glutamic acid compounds, for example, monatin, which are useful as, for example, production intermediates for sweetener or pharmaceutical products.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Applicant: AJINOMOTO CO. INCInventors: Shigeru KAWAHARA, Nao FUNAKOSHI
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Publication number: 20120028995Abstract: The invention relates to compounds of general formula (I) as set forth in the claims as well as to the use of the compounds of the general formula (1) in the medical field, specifically for use in the suppression of DNA synthesis and inflammatory cytokine production as well as in the stimulation of anti-inflammatory cytokine production in vitro and in vivo. This abstract is neither intended to define the invention disclosed in this specification nor intended to limit the scope of the invention in any way.Type: ApplicationFiled: July 19, 2011Publication date: February 2, 2012Applicant: IMTM GMBHInventors: Siegfried ANSORGE, Ute BANK, Anke HEIMBURG, Heiko JULIUS, Karsten NORDHOFF, Michael TAEGER
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Publication number: 20120029016Abstract: There is provided compounds of formula I, wherein ring R1a to R1c, R2a to R2e, and X have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.Type: ApplicationFiled: December 30, 2009Publication date: February 2, 2012Applicant: BIOLIPOX ABInventor: Peter Nilsson
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Publication number: 20120022057Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below (I).Type: ApplicationFiled: March 16, 2010Publication date: January 26, 2012Applicant: Schering CorporationInventors: Gang Zhou, Grant Wishart, Pauline C. Ting, Robert G. Aslanian, Nicolas Zorn, Jianhua Cao
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Publication number: 20120022121Abstract: Indole derivatives and analogous compounds and pharmaceutical compositions comprising the same are provided. Also provided are methods of using these compounds to inhibit tubulin polymerization in a cell associated with a proliferative disease or to treat cancer, metastatic cancer, resistant cancer or multidrug resistant cancer, including inter-alia: prostate cancer, breast cancer, melanoma, colon cancer and bladder cancer.Type: ApplicationFiled: July 25, 2011Publication date: January 26, 2012Inventors: James T. DALTON, Duane D. MILLER, Sunjoo AHN, Charles DUKE, Dong Jin HWANG, Jun YANG
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Publication number: 20110306624Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: February 3, 2010Publication date: December 15, 2011Inventors: Songnian Lin, Xibin Liao, Edward Metzger, Emma R. Parmee, Sheryl D. Debenham
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Publication number: 20110301180Abstract: It has been discovered that inhibiting mitochondrial respiration in platelets reduces platelet activation or platelet aggregation. Certain heterocyclic compounds significantly reduced one or more platelet functions including clumping, sticking or platelet-stimulated clotting. Thus diseases or disorders mediated by inappropriately high levels of platelet activation or platelet aggregation can be treated by administering a therapeutically effective amount of a heterocyclic compound or nonheterocyclic mitochondrial inhibitor that significantly reduces one or more platelet functions including clumping, sticking or platelet-stimulated clotting, preferably in a reversible manner.Type: ApplicationFiled: April 25, 2011Publication date: December 8, 2011Applicant: Stanford UniversityInventors: James P. Collman, Paul Clifford Herrmann, David Alvin Tyvoll, Richard Decreau, Brian Stanley Bull, Christopher Jeffrey Barile
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Publication number: 20110294850Abstract: The present invention provides a novel indoline derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or a salt thereof represented by the following formula (1) that has an excellent butyrylcholinesterase inhibitory activity. In the formula, R1 represents an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a heteroaryl group, an arylalkyl group, a heteroarylalkyl group, a cycloalkylalkyl group, a heterocycloalkylalkyl group, a dihydrofurylalkyl group, an alkenyl group, a tetrahydronaphthyl group, or an indanyl group; R2 represents a hydrogen atom, an alkyl group, an arylalkyl group, a cycloalkylalkyl group, a heteroarylalkyl group, a heterocycloalkylalkyl group, an aryl group, or an acyl group; R3 each independently represents a hydrogen atom, an alkyl group, or a dialkylaminocarbonyl group; R4 each independently represents a hydrogen atom or an alkyl group; and R5 represents a hydrogen atom or an alkyl group.Type: ApplicationFiled: February 3, 2010Publication date: December 1, 2011Applicants: TOKYO INSTITUTE OF TECHNOLOGY, KYOTO UNIVERSITYInventors: Hachiro Sugimoto, Jun Takahashi, Takashi Takahashi, Ichiro Hijikuro
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Publication number: 20110294793Abstract: The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds.Type: ApplicationFiled: June 8, 2009Publication date: December 1, 2011Inventors: kyoung S Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
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Patent number: 8063094Abstract: Heterocyclic compounds which are inhibitors of Mitrogen-Activated Protein Kinase-Activated Protein Kinase-2 (MAPKAP-K2) as described, in addition to their use in the treatment of cytokine mediated diseases.Type: GrantFiled: February 7, 2008Date of Patent: November 22, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Asitha Abeywardane, Denise Andersen, Tina Marie Morwick, Roger John Snow, Yancey David Ward
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Publication number: 20110281811Abstract: The invention relates to the use of at least one leukotriene inhibitor for preparing a pharmaceutical composition for the prophylaxis and/or treatment of lung diseases, more particularly of bronchopulmonary dysplasia, in prematurely born infants. The invention further relates to a pharmaceutical composition for the prophylaxis and/or treatment of lung diseases, more particularly of bronchopulmonary dysplasia, in prematurely born infants, the pharmaceutical composition comprising at least one leukotriene inhibitor. The invention additionally relates to a method for the treatment and/or prophylaxis of a lung disease, more particularly of a bronchopulmonary dysplasia, in a prematurely born infant, where the prematurely born infant is administered a pharmacologically active amount of at least one leukotriene inhibitor.Type: ApplicationFiled: November 12, 2009Publication date: November 17, 2011Inventor: Sabine Rupprecht
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Publication number: 20110269972Abstract: The present invention relates to a compound of general Formula (XX), its formation and its use in asymmetric catalysis. In Formula (XX) R and R31 are independently —COOR3, —R4COOR3, —R4CHO, —R4COR3, —R4CONR5R6, —R4COX, —R4OP(?O)(OH)2, —R4P(?O)(OH)2), —R4C(O)C(R3)CR5R6 and —R4CO2COR3. In addition, R31 may also be hydrogen. R3, R5 and R6 are independently hydrogen, an aliphatic group with a main chain having 1 to about 20 carbon atoms, an alicyclic group, an aromatic group, an arylaliphatic group or an arylalicyclic group, comprising 0 to about 3 heteroatoms independently selected from the group consisting of N, O, S, Se and Si. R4 an aliphatic bridge with a main chain having 1 to about 20 carbon atoms, an alicyclic bridge, an aromatic bridge, an arylaliphatic bridge or an arylalicyclic bridge, comprising 0 to about 3 heteroatoms independently selected from the group consisting of N, O, S, Se and Si, and X is halogen.Type: ApplicationFiled: September 3, 2009Publication date: November 3, 2011Applicant: NANYANG TECHNOLOGICAL UNIVERSITYInventors: Teck Peng Loh, Jian Xiao
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Publication number: 20110269736Abstract: The present invention relates to compounds defined by formula (I) wherein the group R is defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases.Type: ApplicationFiled: July 24, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Eckhardt, Bradford S. Hamilton, Frank Himmelsbach
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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: 20110263567Abstract: The present invention relates to compounds of general formula (i) having an oxime moiety or a pharmaceutically acceptable salt, hydrate or solvate thereof and its use for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1), a pharmaceutical composition comprising the compound or a salt, hydrate or solvate thereof as an active ingredient, a method for the prevention or the treatment of a SSAO/VAP-1 related disease, said diseases including acute or chronic inflammatory diseases, diseases related to carbohydrate metabolism, diabetes-associated complications, diabetic retinopathy and macular oedema, diseases related to adipocyte or smooth muscle dysfunctions, neurodegenerative diseases and vascular diseases.Type: ApplicationFiled: September 11, 2009Publication date: October 27, 2011Applicant: Semmelweis EgyetemInventors: Péter Mátyus, Kálmán Magyar, Marjo Pihlavisto, Klára Gyires, Norbert Haider, Yinghua Wang, Patrick Woda, Petra Dunkel, Éva Tóth-Sarudy, Gÿorgy Túrós
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Publication number: 20110263553Abstract: Provided are steroid analogues functionalized with polar substituents at the C3 and/or C20 positions of the steroid ring system that exhibit improved water solubility. Also provided are pharmaceutical compositions comprising the steroid analogues and methods using the novel steroid analogues for the treatment and prevention of neurodegeneration in a patient following injury to the central nervous system.Type: ApplicationFiled: February 26, 2009Publication date: October 27, 2011Inventors: Christopher Macnevin, Donald G. Stein, Dennis C. Liotta, Iqbal Sayeed, David B. Guthrie, Mark A. Lockwood, Michael G. Natchus
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Publication number: 20110251171Abstract: Compounds of the formula provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.Type: ApplicationFiled: June 22, 2011Publication date: October 13, 2011Inventors: Andrew Thomas Bach, Prasad Koteswara Kapa, George Tien-San Lee, Eric M. Loeser, Michael Lloyd Sabio, James Lawrence Stanton, Thalaththani Ralalage Vedananda
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Patent number: 8030489Abstract: Provided is a compound which is useful as a therapeutic agent for chronic renal insufficiency and a therapeutic agent for diabetic nephropathy. The present inventors have made extensive studies on an ornithine derivative having an antagonistic action against an EP4 receptor, and as a result, they have found that by introducing cycloalkanediyl at a C terminal of the ornithine part of the compound of the present invention, the physicochemical properties such as solubility, and the like can be improved, thereby giving further preferred properties as a pharmaceutical. Therefore, they have completed the present invention. The compound of the present invention exhibits a good antagonistic action against an EP4 receptor, and thus, it is useful as a therapeutic agent for chronic renal insufficiency and diabetic nephropathy.Type: GrantFiled: March 25, 2008Date of Patent: October 4, 2011Assignee: Astellas Pharma Inc.Inventors: Tatsuya Zenkoh, Eisuke Nozawa, Keisuke Matsuura, Ryushi Seo
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Patent number: 8013007Abstract: This invention relates to novel compounds that are dihydroindoles derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel dihydroindoles derivatives that are derivatives of silodosin. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an ?-1A-adrenoreceptor antagonist, such as silodosin.Type: GrantFiled: February 26, 2008Date of Patent: September 6, 2011Assignee: Concert Pharmaceuticals, Inc.Inventor: Julie F. Liu
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Patent number: 7985764Abstract: It was found that a compound according to the following formula: or a pharmaceutically acceptable salt thereof, has a strong antagonism for both the 5-HT2B and 5-HT7 receptors. In addition, the compound shows good pharmacological action as compared to antagonists selective for only one of these receptors. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).Type: GrantFiled: February 7, 2007Date of Patent: July 26, 2011Assignee: Astellas Pharma Inc.Inventors: Hidetaka Kaku, Hiroyoshi Yamada, Daisuke Kaga, Ryushi Seo, Shinobu Akuzawa
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Patent number: 7985763Abstract: A compound of the following formula: in which R1, R2, R3, U, V, T, W, X, Y, Z, m, n, p, x, y, and z are as defined herein. Also disclosed are (1) a pharmaceutical composition containing such a compound, and (2) a method for treating Hepatitis C virus infection using such a compound.Type: GrantFiled: March 26, 2008Date of Patent: July 26, 2011Assignee: National Health Research InstitutesInventors: Li-Wen Wang, Tsu-An Hsu, Yen-Chun Lee, Iou-Jiun Kang, Chung-Chi Lee, Yu-Sheng Chao, Jyh-Haur Chern
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Patent number: 7973069Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.Type: GrantFiled: June 14, 2010Date of Patent: July 5, 2011Assignee: PTC Therapeutics, Inc.Inventors: Gary M. Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony A. Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey Allen Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Jin Zhu, Xiaoyan Zhang
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Patent number: 7973070Abstract: New (2R,4R) monatin monosodium salt hydrate crystals characterized by having specific characteristic X-ray diffraction peaks provide general-purpose, stable, and safe monatin sodium salt crystals incorporating no organic solvent. These crystal may be prepared by a method that requires no organic solvent in the crystallization, separation, and drying steps. These crystal are useful as sweeteners and for the preparation of orally consumed products, such as foods, beverages, pharmaceutical products, topical pharmaceutical products, and feeds containing general-purpose, stable, and safe monatin sodium salt crystals.Type: GrantFiled: March 11, 2009Date of Patent: July 5, 2011Assignee: Ajinomoto Co., Inc.Inventors: Kenichi Mori, Eriko Ono
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Patent number: 7968721Abstract: This invention relates to a process for preparing a selective androgen receptor modulator (SARM) compound represented by the structure of formula I: wherein X is O; and T, Z, Y, Q, R and R1 are defined herein. The process includes coupling between an amide of formula II and a phenol of formula III followed by a purification step consisting of precipitating the compound of formula (I) in a mixture of alcohol and water alone.Type: GrantFiled: January 12, 2004Date of Patent: June 28, 2011Assignee: University of Tennessee Research FoundationInventors: Duane D. Miller, Karen A. Veverka, Kiwon Chung
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Patent number: 7960568Abstract: The present invention relates to heterocyclyl-substituted sulfonamides with 5-HT6 receptor affinity, and compositions thereof, and the use of said compounds for the treatment or prophylaxis of various disorders.Type: GrantFiled: January 30, 2008Date of Patent: June 14, 2011Assignee: Laboratorios Del Dr. Esteve, S.A.Inventor: José-Luis Diaz-Fernández
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Patent number: 7927830Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.Type: GrantFiled: May 29, 2008Date of Patent: April 19, 2011Assignee: Life Technologies CorporationInventors: Ching-Ying Cheung, Stephen Yue, Wai-Yee Leung