The Six-membered Hetero Ring Is Unsubstituted Or Alkyl Substituted Only Patents (Class 546/166)
  • Patent number: 9403805
    Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: June 9, 2015
    Date of Patent: August 2, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Adrian Wai-Hing Cheung, Ryan Craig Schoenfeld, Weiya Yun, Shu-Hai Zhao
  • Publication number: 20150141407
    Abstract: The present invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, its preparation method, a pharmaceutical composition comprising the compound, and its use in manufacture of a medicament for treatment of a disease or disorder, wherein R1, R2, R5, R6, X, Y, Q, W, n1 and n2 are defined as those stated in the description.
    Type: Application
    Filed: May 30, 2013
    Publication date: May 21, 2015
    Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Lan Xie, Xiaofeng Wang, Kuo-Hsiung Lee
  • Publication number: 20150094330
    Abstract: The invention provides compositions and methods for wound healing and scar reduction. The compositions and methods of the invention include at least one EP4 agonist set forth herein. Wounds and or scars that can be treated by the compositions and methods of the invention can arise from events such as surgery, trauma, disease, mechanical injury, burn, radiation, poisoning, and the like.
    Type: Application
    Filed: September 26, 2014
    Publication date: April 2, 2015
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Publication number: 20150057295
    Abstract: This invention relates to 6-alkynyl-pyridine of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R5 have the meanings given in the claims and in the specification.
    Type: Application
    Filed: August 20, 2014
    Publication date: February 26, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Ulrich REISER, James MADDEN
  • Publication number: 20150018366
    Abstract: The invention relates to compounds of formula IA and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof.
    Type: Application
    Filed: September 26, 2014
    Publication date: January 15, 2015
    Inventor: Laykea TAFESSE
  • Publication number: 20150011527
    Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
    Type: Application
    Filed: June 11, 2014
    Publication date: January 8, 2015
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs
  • Publication number: 20150011770
    Abstract: The present invention relates to a novel ligand derived from a tetrahydroquinoline derivative, and a transition metal compound prepared using the ligand, where an amido ligand is linked to an ortho-phenylene ligand to form a condensed ring and a 5-membered cyclic pi-ligand linked to the ortho-phenylene ligand is fused with a heterocyclic thiophene ligand. Compared with the catalysts not fused with a heterocyclic thiophene ligand, the transition metal compound of the present invention as activated with a co-catalyst has higher catalytic activity in olefin polymerization and provides a polymer with higher molecular weight.
    Type: Application
    Filed: September 24, 2014
    Publication date: January 8, 2015
    Inventors: Bun-Yeoul Lee, Ji-Hae Park, Seung-Hyun Do
  • Publication number: 20150005283
    Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 1, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Adrian Wai-Hing Cheung, Ryan Craig Schoenfeld, Weiya Yun, Shu-Hai Zhao
  • Publication number: 20140378474
    Abstract: The invention relates to a compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: January 25, 2013
    Publication date: December 25, 2014
    Applicant: NOVARTIS AG
    Inventors: Stefanie Flohr, Christian Markert, Kenji Namoto, Bernard Pirard
  • Publication number: 20140374721
    Abstract: Benzotriazole derivatives represented by the following general formula (1), wherein Ar1 and Ar2 are, for example, aromatic hydrocarbon groups or aromatic heterocyclic ring groups, and A is a group including a pyridine ring. The compounds excel in electron injection/transport capability, feature a high hole-blocking power and a high stability in their thin-film form, and are useful as materials for producing highly efficient and highly durable organic electroluminescent devices.
    Type: Application
    Filed: October 5, 2012
    Publication date: December 25, 2014
    Applicant: HODOGAYA CHEMICAL CO., LTD
    Inventors: Norimasa Yokoyama, Shigetaka Numazawa, Shirou Irisa, Shuichi Hayashi
  • Publication number: 20140371459
    Abstract: Provided is a method for producing a compound represented by formula (7) or a salt thereof: the method comprising the steps of: removing a R1 group and a R2 group from a compound represented by formula (5) or a salt thereof: and reacting the compound (in which R1 and R2 in formula (5) are hydrogen atoms) obtained in the removing step or a salt thereof with a compound represented by formula (d): or a salt thereof in the presence of a base. The method is a method for producing a 1,2-dihydroquinoline derivative having glucocorticoid receptor binding activity or a salt thereof. This method does not require a purification step by column chromatography and is suitable for industrial production.
    Type: Application
    Filed: January 21, 2013
    Publication date: December 18, 2014
    Applicants: SANTEN PHARMACEUTICAL CO., LTD., KYOWA HAKKO BIO CO., LTD.
    Inventors: Noriyoshi Yamamoto, Atsushi Ohno, Kazuhiro Kudou, Masakazu Ban, Takashi Mimura, Takashi Ohtani
  • Publication number: 20140364454
    Abstract: The invention relates to metal-chelating compounds comprising one or more 8-hydroxyquinoline units substituted in position 2 with a nitrogenous group comprising a polyamino chain, wherein the polyamino chain is N-substituted on said nitrogenous group, to the composition containing same, and to the uses thereof in the therapeutic field and in particular in the treatment of diseases associated with an abnormality in the regulation of metal metabolism resulting in a metal overload in human or animal cells.
    Type: Application
    Filed: December 18, 2012
    Publication date: December 11, 2014
    Inventors: Francois Gaboriau, David Deniaud, Vincent Corce, Karine Julienne Aphecetche, Eric Renault
  • Publication number: 20140364393
    Abstract: The present invention is directed to novel piperidinyl-carboxamide derivatives, pharmaceutical compositions containing them and their use as inhibitors of SCD1, useful in the treatment of obesity, type-II diabetes and other related metabolic disorders.
    Type: Application
    Filed: December 5, 2012
    Publication date: December 11, 2014
    Inventors: Shyh-Ming Yang, Gee-Hong Kuo, Micheal D. Gaul, Thomas A. Rano
  • Publication number: 20140315949
    Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
    Type: Application
    Filed: November 19, 2012
    Publication date: October 23, 2014
    Applicant: CONSTELLATION PHARMACEUTICALS, INC.
    Inventors: Brian K. Albrecht, James Edmund Audia, Alexandre Gagnon, Jean-Christophe Harmange, Christopher G. Nasveschuk
  • Patent number: 8729076
    Abstract: The present invention provides new secondary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful as antifungal agents. Specifically, these compounds were tested against Tricophyton Rubrum, Tricophyton Mentagrophytes, Aspergillus Niger and Scopulariopsis Brevicaulis. Many of these compounds are active against Candida species such as Candida Albicans and Candida Glabrata.
    Type: Grant
    Filed: December 28, 2010
    Date of Patent: May 20, 2014
    Assignee: Polichem SA
    Inventors: Stefania Gagliardi, Simone Del Sordo, Federico Mailland, Michela Legora
  • Publication number: 20140121181
    Abstract: A hydrophobic polymer compound is capable of inhibiting the blood coagulation reactions in both the primary hemostasis stage involving platelets and the coagulation thrombus formation stage involving blood coagulation factors, which hydrophobic polymer compound can be firmly immobilized on the surface of a medical device or medical material in a state where the compound retains its anticoagulant activity. A hydrophobic polymer compound in which a polymer compound inhibiting platelet adhesion is bound with a compound inhibiting blood coagulation reaction.
    Type: Application
    Filed: June 22, 2012
    Publication date: May 1, 2014
    Applicant: TORY INDUSTRIES, INC.
    Inventors: Kazuhiro Tanahashi, Hirokazu Sakaguchi, Yuka Sakaguchi
  • Publication number: 20140076726
    Abstract: The present invention provides methods for determining the presence of immobilized nucleic acid employing unsymmetrical cyanine dyes that are derivatives of thiazole orange, a staining solution and select fluorogenic compounds that are characterized as being essentially non-genotoxic. The methods comprise immobilizing nucleic acid, single or double stranded DNA, RNA or a combination thereof, on a solid or semi solid support, contacting the immobilized nucleic acid with an unsymmetrical cyanine dye compound and then illuminating the immobilized nucleic acid with an appropriate wavelength whereby the presence of the nucleic acid is determined. The cyanine dye compounds are typically present in an aqueous staining solution comprising the dye compound and a tris acetate or tris borate buffer wherein the solution facilitates the contact of the dye compound and the immobilized nucleic acid.
    Type: Application
    Filed: May 15, 2013
    Publication date: March 20, 2014
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Matthew BEAUDET, William Gregory Cox, Stephen Yue
  • Publication number: 20130324573
    Abstract: The present invention relates to novel substituted 1,2,3,4-tetrahydroquinolin-7-yl carbamates, their preparation, and use as therapeutic agents, particularly in the prevention or treatment of neurodegenerative or Alzheimer's disease, or senile dementia, or memory disturbances, and more particularly to the prevention, treatment and amelioration of Alzheimer's disease with the novel substituted 1,2,3,4-tetrahydroquinolin-7-yl carbamates, which act as inhibitors of central cholinesterase enzymes, particularly acetylcholinesterase (AChE) following the indirect cholinomimetic pathway. The present invention particularly relates to compounds of formula A: Formula A wherein R1=alkyl, aryl, substituted aryl; R2?H, methyl; R3?H, alkyl, alkenyl, alkynyl, aralkyl, substituted aralkyl, aryl, heteroaryl.
    Type: Application
    Filed: January 24, 2012
    Publication date: December 5, 2013
    Applicant: Council of Scientific & Industrial Research
    Inventors: Kuldeep Kumar Roy, Santoshkumar Tota, Chandishwar Nath, Rakesh Shukla, Anil Kumar Saxena
  • Publication number: 20130324523
    Abstract: An object of the present invention is to provide a probe for imaging a ?-sheet structure protein which can be used for the diagnosis of conformational diseases, particularly disease (tauopathy) having a cardinal symptom such as intracerebral accumulation of tau protein, for example, Alzheimer's disease. Another object of the present invention is to provide a compound which is highly specific to tau and can image tau with satisfactory sensitivity, and also has high brain transition, low or non-recognized bone-seeking properties and low or non-recognized toxicity. According to the present invention, the above problems are solved by providing a compound of a formula I (wherein A, R1, R2, R3, R4, R5, R6, Ra and Rb are as defined in the present description) or a pharmaceutically acceptable salt or solvate thereof.
    Type: Application
    Filed: October 28, 2011
    Publication date: December 5, 2013
    Applicant: CLINO LTD.
    Inventors: Yukitsuka Kudo, Shozo Furumoto, Nobuyuki Okamura
  • Publication number: 20130264547
    Abstract: An organic electroluminescent element including a substrate, a pair of electrodes including an anode and a cathode, disposed on the substrate, and at least one layer of organic layers including a light emitting layer, disposed between the electrodes, in which at least one of the organic layers contains a compound represented by the following general formula: (R1 to R18 each independently represent a hydrogen atom or a substituent, and at least one of R1 to R8 and R10 to R17 represents -L-NR19R20 (R19 and R20 each independently represent any of an alkyl group, an aryl group, a heteroaryl group. R19 and R20 may be combined to each other to form a ring. L represents a single bond or a divalent linking group). X1 to X18 each independently represent a carbon atom or a nitrogen atom, and when X1 to X18 represent nitrogen atoms, R1 to R18 for bonding do not present.
    Type: Application
    Filed: February 4, 2013
    Publication date: October 10, 2013
    Applicant: UDC Ireland Limited
    Inventors: Tetsu Kitamura, Tenka Ouyo, Yuki Hirai, Koji Takaku, Wataru Sotoyama, Masaru Kinoshita, Kuniyuki Kaminaga, Yosuke Yamamoto
  • Publication number: 20130236888
    Abstract: Enzyme substrates and associated technology of the present invention are provided. An enzyme substrate of the invention may comprise a biologically functional fluorescent dye and an enzyme-specific substrate moiety attached in such a way that the functionality of the functional dye is diminished. An enzymatic reaction may cleave at least a portion of the substrate moiety from the enzyme substrate to provide a more functional product dye. This product dye may be nonfluorescent or weakly fluorescent, in general, and relatively fluorescent, in a particular condition, such as when bound to a partner biological molecule or an assembly of partner biological molecules. An enzyme substrate of the present invention may thus be useful in fluorescence detection, and/or in any of a variety of useful applications, such as the detection of enzymatic activity in a cell-free system or in a living cell, the screening of drugs, or the diagnosis of disease.
    Type: Application
    Filed: May 10, 2013
    Publication date: September 12, 2013
    Applicant: Biotium, Inc.
    Inventors: Fei Mao, Hui Cen
  • Publication number: 20130203949
    Abstract: The present invention relates to a novel ligand derived from a tetrahydroquinoline derivative, and a transition metal compound prepared using the ligand, where an amido ligand is linked to an ortho-phenylene ligand to form a condensed ring and a 5-membered cyclic pi-ligand linked to the ortho-phenylene ligand is fused with a heterocyclic thiophene ligand. Compared with the catalysts not fused with a heterocyclic thiophene ligand, the transition metal compound of the present invention as activated with a co-catalyst has higher catalytic activity in olefin polymerization and provides a polymer with higher molecular weight.
    Type: Application
    Filed: April 12, 2011
    Publication date: August 8, 2013
    Applicant: OTTE CHEMICAL CORPORATION
    Inventors: Bun-Yeoul Lee, Ji-Hae Park, Seung-Hyun Do
  • Publication number: 20130178420
    Abstract: The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
    Type: Application
    Filed: December 12, 2012
    Publication date: July 11, 2013
    Applicant: RECEPTOS, INC.
    Inventor: RECEPTOS, INC.
  • Publication number: 20130011927
    Abstract: The present invention provides methods for determining the presence of immobilized nucleic acid employing unsymmetrical cyanine dyes that are derivatives of thiazole orange, a staining solution and select fluorogenic compounds that are characterized as being essentially non-genotoxic. The methods comprise immobilizing nucleic acid, single or double stranded DNA, RNA or a combination thereof, on a solid or semi solid support, contacting the immobilized nucleic acid with an unsymmetrical cyanine dye compound and then illuminating the immobilized nucleic acid with an appropriate wavelength whereby the presence of the nucleic acid is determined. The cyanine dye compounds are typically present in an aqueous staining solution comprising the dye compound and a tris acetate or tris borate buffer wherein the solution facilitates the contact of the dye compound and the immobilized nucleic acid.
    Type: Application
    Filed: June 18, 2012
    Publication date: January 10, 2013
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Matthew Paul Beaudet, W. Gregory Cox, Stephen Yue
  • Publication number: 20120196994
    Abstract: The present invention relates to a novel post metallocene-type ligand compound, to a metal compound containing the ligand compound, to a catalytic composition containing the metal compound, and to a method for preparing same, as well as to a method for preparing olefin polymers using the catalytic composition.
    Type: Application
    Filed: July 23, 2010
    Publication date: August 2, 2012
    Inventors: Sang-Jin Jeon, Hoon Chae, Cheon-Il Park, Kyung-Seop Noh, Won-Hee Kim
  • Publication number: 20120165370
    Abstract: Quinoline derivatives showing anticancer activities against cancer cell lines of hepatocellular carcinoma (Hep3B), lung carcinoma (A549), esophageal squamous cell carcinoma (HKESC-1, HKESC-4 and KYSE150).
    Type: Application
    Filed: December 22, 2011
    Publication date: June 28, 2012
    Inventors: Johnny Cheuk-on TANG, Albert Sun Chi CHAN, Kim Hung LAM, Sau Hing CHAN
  • Publication number: 20120157641
    Abstract: The present invention relates to cure accelerators useful for anaerobic curable compositions, such as adhesives and sealants.
    Type: Application
    Filed: October 7, 2011
    Publication date: June 21, 2012
    Applicants: Loctite (R&D) Limited, Henkel Corporation
    Inventors: David Birkett, Martin Wyer, Andrew Messana, Philip Klemarczyk, Anthony F. Jacobine
  • Publication number: 20120149728
    Abstract: The disclosure relates to fumarate salts of 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide, to pharmaceutical compositions thereof, processes for making the same, and methods of use thereof.
    Type: Application
    Filed: December 8, 2011
    Publication date: June 14, 2012
    Applicant: SANOFI
    Inventors: Beverly C. LANGEVIN, Robert Allan FARR, Dinubhai H. SHAH, Daniel SHERER
  • Publication number: 20120115827
    Abstract: The present invention relates to a novel 3-aminobenzamide, compound represented by the following formula which effectively inhibits vanilloid receptor subtype 1 (VR1) activity (wherein, for example, R1 is a C1-6 alkyl group which may be substituted, R2 is a hydrogen atom, a C1-6 alkyl group or a C1-6 alkoxy group which may be substituted, R3 is a hydrogen atom or a C1-6 alkyl group, R4 is a C1-6 alkyl group, a C1-6 alkoxy group, or a halo C1-6 alkyl group, m is an integer of 1 to 5 and P is a carbon or hetero ring) or a pharmaceutically acceptable salt thereof. The pharmaceutical composition comprising as active ingredients the 3-aminobenzamide, compound or a pharmaceutically acceptable salt thereof is useful for treating diseases involved in VR1 activity such as pain, acute pain, chronic pain, neuropathicpain, rheumatoid arthritis pain, and neuralgia.
    Type: Application
    Filed: June 7, 2011
    Publication date: May 10, 2012
    Applicant: Japan Tobacco Inc.
    Inventors: Yoshihisa Koga, Shinji Yata, Takashi Watanabe, Takuya Matsuo, Masahiro Sakata, Wataru Kondo
  • Publication number: 20120115870
    Abstract: An ophthalmic pharmaceutical composition useful in the treatment of glaucoma and control of intraocular pressure comprising an effective amount of a selective modulator of ALK5 receptor activity is disclosed. Also disclosed is a method of treating glaucoma and controlling intraocular pressure comprising applying a therapeutically effective amount of a pharmaceutical composition comprising a selective modulator of ALK5 receptor activity to an affected eye of a patient.
    Type: Application
    Filed: January 11, 2012
    Publication date: May 10, 2012
    Applicant: ALCON RESEARCH, LTD.
    Inventors: Debra L. Fleenor, Iok-Hou Pang, Allan R. Shepard, Mark R. Hellberg, Peter G. Klimko, Abbot F. Clark
  • Publication number: 20120088916
    Abstract: The present invention relates to an octahydro biquinoline compound. Provided is also a method of separating the octahydro biquinoline compound into enantiomers. The octahydro biquinoline compound is of the general formula (V): In formula (V) R1 is one of H, a protective group and an aliphatic group, with the aliphatic group having a main chain of a length of 1 to about 10 carbon atoms, comprising 0 to about 6 heteroatoms selected from the group consisting of N, O, S, Se and Si. R2 and R3 are independent from one another selected from the group consisting of (i) H, (ii) one of an aliphatic, an alicyclic, an aromatic, an arylaliphatic, and an arylalicyclic group comprising 0 to about 6 heteroatoms selected from the group consisting of N, O, S, Se and Si, an ester, a carbonate group, a carbamoyl group and a phosphate ester.
    Type: Application
    Filed: May 17, 2010
    Publication date: April 12, 2012
    Applicant: Nanyang Technological University
    Inventors: Teck Peng Loh, Jian Xiao
  • Patent number: 8143259
    Abstract: 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: Grant
    Filed: August 11, 2009
    Date of Patent: March 27, 2012
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Donald W. Ludovici, Jay M. Matthews, Mingde Xia, Xiaoqing Xu, Mark A. Youngman, Bin Zhu
  • Publication number: 20120058566
    Abstract: The present invention provides methods for determining the presence of immobilized nucleic acid employing unsymmetrical cyanine dyes that are derivatives of thiazole orange, a staining solution and select fluorogenic compounds that are characterized as being essentially non-genotoxic. The methods comprise immobilizing nucleic acid, single or double stranded DNA, RNA or a combination thereof, on a solid or semi solid support, contacting the immobilized nucleic acid with an unsymmetrical cyanine dye compound and then illuminating the immobilized nucleic acid with an appropriate wavelength whereby the presence of the nucleic acid is determined. The cyanine dye compounds are typically present in an aqueous staining solution comprising the dye compound and a tris acetate or tris borate buffer wherein the solution facilitates the contact of the dye compound and the immobilized nucleic acid.
    Type: Application
    Filed: August 30, 2011
    Publication date: March 8, 2012
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Matthew Paul BEAUDET, W. Gregory Cox, Stephen Yue
  • Patent number: 8110562
    Abstract: This invention provides nuclear hormone receptor binding compounds, compositions comprising the same and methods of uses thereof in treating a variety of diseases or conditions in a subject, including, inter-alia, prostate cancer and/or diseases or disorders of bone and muscle.
    Type: Grant
    Filed: July 19, 2007
    Date of Patent: February 7, 2012
    Assignees: University of Tennessee Research Foundation, The Ohio State University Research Foundation
    Inventors: James T. Dalton, Duane D. Miller, Igor Rakov, Casey Bohl, Michael L. Mohler
  • Patent number: 8022217
    Abstract: Disclosed herein in the embodiments of the present invention are the compounds suitable as modulators of HDL having general formula (1), novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (1), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
    Type: Grant
    Filed: July 27, 2007
    Date of Patent: September 20, 2011
    Assignee: Cadila Healthcare Limited
    Inventors: Pravin S. Thombare, Braj Bhushan Lohray, Vidya Bhushan Lohray, Pankaj Ramanbhai Patl
  • Publication number: 20110207704
    Abstract: Novel oxadiazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions as agonists or antagonists of the S1P family of G protein-coupled receptors for treating diseases associated with modulation of S1P family receptor activity, in particular by affording a beneficial immunosuppressive effect are disclosed.
    Type: Application
    Filed: August 24, 2010
    Publication date: August 25, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Kevin P. Cusack, Eric C. Breinlinger, Shannon R. Fix-Stenzel, Robert H. Stoffel, Kevin R. Woller, Adrian D. Hobson, Pintipa Grongsaard
  • Publication number: 20110178089
    Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.
    Type: Application
    Filed: January 13, 2011
    Publication date: July 21, 2011
    Inventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Kyungjin Kim, Rainer E. Martin, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ulmer
  • Publication number: 20110166349
    Abstract: Methods are provided for the catalytic hydroamination of compounds having an alkyne or allene functional group, in which the compound is contacted with ammonia or an amine in the presence of a catalytic amount of a gold complex under conditions sufficient for hydroamination to occur.
    Type: Application
    Filed: May 8, 2009
    Publication date: July 7, 2011
    Applicant: The Regents of the University of California
    Inventors: Guy Bertrand, Vincent Lavallo, Guido D. Frey, Bruno Donnadieu, Michele Soleil-Havoup
  • Publication number: 20110152529
    Abstract: Provided are a novel transition metal complex where a monocyclopentadienyl ligand to which an amido group is introduced is coordinated, a catalyst composition including the same, and an olefin polymer using the catalyst composition. The transition metal complex has a pentagon ring structure having an amido group connected by a phenylene bridge in which a stable bond is formed in the vicinity of a metal site, and thus, a sterically hindered monomer can easily approach the transition metal complex. By using a catalyst composition including the transition metal complex, a linear low density polyolefin copolymer having a high molecular weight and a very low density polyolefin copolymer having a density of 0.910 g/cc or less can be produced in a polymerization of monomers having large steric hindrance. Further, the reactivity for the olefin monomer having large steric hindrance is excellent.
    Type: Application
    Filed: March 7, 2011
    Publication date: June 23, 2011
    Applicant: LG CHEM, LTD.
    Inventors: Choong Hoon LEE, Eun Jung LEE, Seungwhan JUNG, Boram LEE, Jung A. Lee, Bun Yeoul LEE
  • Publication number: 20110082133
    Abstract: [Problems] A useful compound which can be used as a pharmaceutical, in particular, an agent for treating peripheral arterial occlusive disease is provided. [Means for Solution] The present inventors have conducted extensive studies on EP4 receptor agonists, and as a result, have found that a novel pyridone compound, in which a group having an acidic group is substituted at the 1-position of the pyridone ring, the 6-position is bonded with an aromatic ring group via a linking part, and the linking part contains a nitrogen atom, has an excellent EP4 receptor agonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor agonistic action, it is useful as a pharmaceutical, in particular, as an agent for treating peripheral arterial occlusive disease.
    Type: Application
    Filed: June 16, 2009
    Publication date: April 7, 2011
    Inventors: Takashi Kamikubo, Masanori Miura, Takao Okuda, Keisuke Maki, Fukushi Hirayama, Ayako Moritomo, Yuriko Komiya, Keisuke Matsuura, Ryotaro Ibuka
  • Publication number: 20110077221
    Abstract: This invention provides nuclear hormone receptor binding compounds, compositions comprising the same and methods of uses thereof in treating a variety of diseases or conditions in a subject, including, inter-alia, prostate cancer and/or diseases or disorders of bone and muscle.
    Type: Application
    Filed: July 19, 2007
    Publication date: March 31, 2011
    Inventors: James T. Dalton, Duane D. Miller, Igor Rakov, Casey Bohl, Michael L. Mohler
  • Publication number: 20110059939
    Abstract: Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, a dashed line represent the presence or absence of a double bond, are disclosed, wherein J1, J2, U1, B, Y, and A are as described in claims 1-12. Methods, compositions, and medicaments related thereto are also disclosed, for treating glaucoma, inflammatory bowel disease and baldness.
    Type: Application
    Filed: May 4, 2009
    Publication date: March 10, 2011
    Applicant: ALLERGAN ,INC
    Inventors: David W. Old, Vinh X. Ngo
  • Patent number: 7879863
    Abstract: The present invention provides a novel compound having a kininogenase-inhibitory action and its pharmaceutical use. The compounds are represented by the formulas (A), (B), (C), (E) and (H): wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 29, 2006
    Date of Patent: February 1, 2011
    Assignee: Ajinomoto Co., Inc.
    Inventors: Munetaka Tokumasu, Masayuki Sugiki, Haruko Hirashima, Hideki Matsumoto, Toshihiko Yoshimura, Yasuko Nogi, Mitsuo Takahashi, Manabu Kitazawa, Akiko Oonuki, Naoyuki Fukuchi, Yoichiro Shima
  • Publication number: 20110015178
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
    Type: Application
    Filed: March 13, 2009
    Publication date: January 20, 2011
    Applicant: THE UNIVERSITY OF EDINBURGH
    Inventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
  • Patent number: 7807692
    Abstract: Phenoxyphenyl and phenoxybenzyl oxazolidine-2,4-diones and thiazolidine-2,4-diones are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
    Type: Grant
    Filed: June 30, 2006
    Date of Patent: October 5, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James F. Dropinski, Peter T. Meinke, Guo Q. Shi, Yong Zhang
  • Publication number: 20100179161
    Abstract: Compounds of the formula (I) and pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, useful in the treatment of Mycobacterium tuberculosis (M.tb).
    Type: Application
    Filed: August 16, 2006
    Publication date: July 15, 2010
    Applicant: ASTRAZENECA AB
    Inventors: Balachandra Shankar Bandodkar, Stefan Schmitt
  • Publication number: 20100120856
    Abstract: The invention relates to compounds of the animated hydroxyquinoline type capable of preventing the migration of metastases or tumoral cells. Such compounds are useful for treating cancers.
    Type: Application
    Filed: March 25, 2008
    Publication date: May 13, 2010
    Applicant: BIOPHARMED
    Inventors: Jean-Louis Kraus, Olivier Blin, Frederic Champavere
  • Publication number: 20100086615
    Abstract: To provide a pulmonary disease therapeutic drug exhibiting high efficacy and reduced side effects. The pulmonary disease therapeutic drug of the invention for intratracheal administration contains biocompatible polymer nanoparticles including an HMG-CoA reductase inhibitor.
    Type: Application
    Filed: April 25, 2008
    Publication date: April 8, 2010
    Applicants: KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION, KOWA CO., LTD
    Inventors: Kensuke Egashira, Junji Kojima, Megumi Sakamoto
  • Publication number: 20100048589
    Abstract: 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: Application
    Filed: August 11, 2009
    Publication date: February 25, 2010
    Inventors: Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Donald W. Ludovici, Jay M. Matthews, Mingde Xia, Xiaoqing Xu, Mark A. Youngman, Bin Zhu
  • Publication number: 20100029615
    Abstract: The present invention relates to a compound of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, A, X, n, and are as defined herein. Such novel benzamidazole derivatives are useful in trv treatment of abnormal cell growth, such as cancer, in mammals. This invention ate relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing sue compounds.
    Type: Application
    Filed: December 5, 2007
    Publication date: February 4, 2010
    Inventors: Michael John Munchhof, Lawrence Alan Reiter, Andrei Shavnya, Christopher Scott Jones, Qifang Li, Robert Gerald Linde ll