Plural Hetero Rings Patents (Class 549/414)
  • Patent number: 9573892
    Abstract: The subject of the invention is process for the preparation of the prostaglandin amides of the general formula I, where in the formula, the bonds marked with dotted lines may be single or double bonds, in the case of double bounds at positions 5,6 and 13,14 they may be in cis or in trans orientation, Q stands for a hydroxyl-group and Z stands for a hydroxyl- or oxo-group, R1 and R2 independently represent hydrogen atom or a straight or branched C1-10 alkyl- or aralkyl-group, optionally substituted with —ONO2 group, or an aralkyl- or aryl-group, which contains heteroatom, R3 represents a straight or branched, saturated or unsaturated C4-6 hydrocarbon group, or a C4-10 alkylcycloalkyl- or cycloalkyl-group, or an optionally with alkyl group or halogen atom substituted phenyl-, C7-10 alkylaryl- or hetaryl-group, Y represents (CH2)n group or O atom or S atom, and where n=0-3.
    Type: Grant
    Filed: December 10, 2015
    Date of Patent: February 21, 2017
    Assignee: CHINOIN ZRT
    Inventors: Gábor Havasi, Tibor Kiss, Irén Hortobágyi, Zsuzsanna Kardos, István Lászlófi, Zoltán Bischof, Ádám Bódis
  • Patent number: 9034921
    Abstract: A compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney is disclosed. A pharmaceutical composition including the compound as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes is disclosed. A method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound is provided.
    Type: Grant
    Filed: June 1, 2012
    Date of Patent: May 19, 2015
    Assignee: GREEN CROSS CORPORATION
    Inventors: Soongyu Choi, Kwang Seop Song, Suk Ho Lee, Min Ju Kim, Hee Jeong Seo, Eun-Jung Park, Younggyu Kong, So Ok Park, Hyunku Kang, Myung Eun Jung, Kinam Lee, Hyun Jung Kim, Jun Sung Lee, Min Woo Lee, Mi-Soon Kim, Dong Ho Hong, Misuk Kang
  • Patent number: 8981128
    Abstract: The present invention relates to the production of compounds comprising nitrile functions and of cyclic imide compounds. It relates more particularly to the production of compounds comprising nitrile functions from compounds comprising carboxylic functions, advantageously of natural and renewable origin, and from 2-methylglutaronitrile (MGN) or a mixture N of dinitriles comprising 2-methylglutaronitrile (MGN), 2-ethylsuccinonitrile (ESN) and adiponitrile (AdN).
    Type: Grant
    Filed: July 5, 2012
    Date of Patent: March 17, 2015
    Assignee: Rhodia Operations
    Inventors: Philippe Marion, Roland Jacquot
  • Publication number: 20150072969
    Abstract: The present invention relates to phenyl alkanoic acid derivatives (the compounds of Formula (I)); and their isotopic forms, stereoisomeric and tautomeric forms and mixtures thereof in all ratios, or pharmaceutically acceptable salts, pharmaceutically acceptable solvates, prodrugs, polymorphs, N-oxides, S-oxides or carboxylic acid isosteres thereof. The invention also relates to processes for the preparation of compounds of Formula (I) and pharmaceutical compositions comprising one or more of the compounds of Formula (I). The said compounds and the pharmaceutical composition function as GPR (G-protein coupled receptor) agonists, particularly as GPR40 agonists, and are useful in the treatment of diseases or conditions mediated by GPR40. The present invention further relates to a method of treatment of diseases or conditions mediated by GPR40 comprising administering to a subject in need thereof a therapeutically effective amount of the compounds of Formula (I).
    Type: Application
    Filed: February 27, 2013
    Publication date: March 12, 2015
    Applicant: PIRAMAL ENTERPRISES LIMITED
    Inventors: Sanjay Kumar, Rajiv Sharma, Vishal Ashok Mahajan, Sangameshwar Prabhakar Sawargave
  • Patent number: 8956999
    Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds of formula (I), which are suitable for use as herbicides.
    Type: Grant
    Filed: June 26, 2008
    Date of Patent: February 17, 2015
    Assignees: Syngenta Limited, Syngenta Crop Protection LLC
    Inventors: Stephane André Marie Jeanmart, Christopher John Mathews, John Benjamin Taylor, Mangala Govenkar, Stephen Christopher Smith
  • Patent number: 8957097
    Abstract: The present invention is directed to hemi phorboxazole A: and its stereoisomers, as well as derivatives of hemi phorboxazole A of formula I: wherein ring A is aryl or a 5- or 6-membered heteroaryl optionally substituted with one or more of halogen, —OH, or —C1-6alkyl; and R is —CN, a 5- or 6-membered heteroaryl, or halogen; and the pharmaceutically acceptable salt forms thereof, in addition to methods of using these compounds.
    Type: Grant
    Filed: July 23, 2010
    Date of Patent: February 17, 2015
    Assignees: The Trustees Of The University Of Pennsylvania, The Regents Of The University Of California
    Inventors: Amos B. Smith, III, Zhuqing Liu, Anne-Marie L. Hogan, Doralyn S. Dalisay, Tadeusz F. Molinski
  • Publication number: 20150034871
    Abstract: An object is to provide a polymerizable compound having high polymerization reactivity, a high conversion ratio and high solubility in a liquid crystal composition, a polymerizable composition containing the compound, a liquid crystal composite prepared from the composition, and a liquid crystal display device having the composite. A solution is a polymerizable compound represented by formula (1). In the formula, for example, P1 and P2 are —OCO—(CH3)C?CH2; S1 and S2 are a single bond; ring A1, ring A2 and ring A3 are 1,4-phenylene; Z1, Z2 and Z3 are a single bond; two of G is —CH? or —N?; and a is 0 or 1.
    Type: Application
    Filed: July 31, 2014
    Publication date: February 5, 2015
    Applicants: JNC PETROCHEMICAL CORPORATION, JNC CORPORATION
    Inventors: Yasuyuki GOTOH, Teizi SATOU
  • Publication number: 20150038566
    Abstract: The invention provides novel compounds of Formulas (I)-(IV), as described herein. Also provided are compositions of these compounds, method of making the compounds, and methods of using the compounds. The compounds can be used to regulate cholesterol homeostasis and to treat conditions and diseases associated with cholesterol homeostasis, including lysosomal lipid storage disorders such as Niemann-Pick Disease type C.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Applicant: UNIVERSITY OF NOTRE DAME DU LAC
    Inventor: Richard Taylor
  • Publication number: 20150025069
    Abstract: This invention is directed to analogs of 5-(tetradecyloxy)-2-furancarboxylic acid (TOFA) and their use in the treatment of dermatological disorders or conditions characterized by sebaceous gland hyperactivity, such as acne and oily skin, and other dermatological disorders and conditions. This invention is also directed to pharmaceutical compositions comprising analogs of TOFA and a pharmaceutically acceptable excipient for dermatological or oral administration.
    Type: Application
    Filed: October 3, 2014
    Publication date: January 22, 2015
    Inventors: Timothy Scott Daynard, Geoffrey C. Winters, David W.C. Hunt
  • Patent number: 8927597
    Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate.
    Type: Grant
    Filed: January 7, 2013
    Date of Patent: January 6, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Atsushi Endo, Charles E. Chase, Francis G. Fang
  • Publication number: 20140356625
    Abstract: The present invention provides methods for manufacturing neuraminic acid derivatives. [Means for solution] Methods for manufacturing compounds represented by the formula (I): [wherein R1 represents a C1-C19 alkyl group], or a pharmacologically acceptable salt thereof, using N-acetylneuraminic acid dihydrate as a starting raw material are provided.
    Type: Application
    Filed: December 13, 2012
    Publication date: December 4, 2014
    Inventors: Tomohito Sakurai, Takumi Nakajima, Masakazu Wakayama, Fumihiko Toriyama, Yasuhisa Kuwahara
  • Publication number: 20140309427
    Abstract: Certain 3,6-disubstituted and 2, 4, 5-trisubstituted pyran derivatives that exhibit potent activity on monoamine transport systems are provided. The 3, 6 and 2, 4, 5 pyrans are useful in probing the effects of their binding to monoamine transporter systems and the corresponding relationships to various afflictions affecting the CNS, or as a treatment for various CNS-related disorders in which the monoamine transport and related systems are implicated.
    Type: Application
    Filed: February 6, 2014
    Publication date: October 16, 2014
    Inventor: Aloke K. DUTTA
  • Publication number: 20140309208
    Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are disclosed that are represented by general formula (I). Also disclosed, are pharmaceutical compositions including these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated pathologies.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Inventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
  • Publication number: 20140088079
    Abstract: The present invention relates to a compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. The present invention also provides a method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound.
    Type: Application
    Filed: June 1, 2012
    Publication date: March 27, 2014
    Applicant: GREEN CROSS CORPORATION
    Inventors: Soongyu Choi, Kwang Seop Song, Suk Ho Lee, Min Ju Kim, Hee Jeong Seo, Eun-Jung Park, Younggyu Kong, So Ok Park, Hyunku Kang, Myung Eun Jung, Kinam Lee, Hyun Jung Kim, Jun Sung Lee, Min Woo Lee, Mi-Soon KIM, Dong Ho Hong, Misuk Kang
  • Publication number: 20140051872
    Abstract: The present invention provides catalysts, methods, and reactor systems for converting oxygenated hydrocarbons to oxygenated compounds. The invention includes methods for producing cyclic ethers, monooxygenates, dioxygenates, ketones, aldehydes, carboxylic acids, and alcohols from oxygenated hydrocarbons, such as carbohydrates, sugars, sugar alcohols, sugar degradation products, and the like, using catalysts containing palladium, molybdenum, tin, and tungsten. The oxygenated compounds produced are useful in the production of liquid fuels, chemicals, and other products.
    Type: Application
    Filed: August 15, 2012
    Publication date: February 20, 2014
    Applicant: Virent, Inc.
    Inventors: Brian Blank, Randy Cortright, Taylor Beck, Elizabeth Woods, Mike Jehring
  • Patent number: 8637496
    Abstract: The invention relates to the use of compounds having a monogalactosyldiacylglycerol (MGDG) synthase inhibitory activity as herbicide or algaecide, and to herbicide and algaecide compositions containing at least one of these compounds.
    Type: Grant
    Filed: June 2, 2008
    Date of Patent: January 28, 2014
    Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche Scientifique
    Inventors: Anne-Laure Bonneau, Cyrille Botte, Michael Deligny, Nadia Saidani, Hélène Hardre, Bernard Rousseau, Roman Lopez, Eric Marechal
  • Publication number: 20130324525
    Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: August 6, 2013
    Publication date: December 5, 2013
    Applicant: Gilead Sciences, Inc.
    Inventors: Matthew Abelman, Robert H. Jiang, Jeff Zablocki
  • Patent number: 8575370
    Abstract: Methods for manufacturing neuraminic acid compounds and synthetic intermediates of neuraminic acid compounds, including a method for manufacturing a compound represented by wherein R2 represents a C1-C4 alkyl, R3 represents a C1-C6 alkyl, R4 and R5 represent a hydrogen atom, a C1-C6 alkyl or a phenyl, or R4 and R5 together form a tetramethylene, a pentamethylene or an oxo, and Ac represents an acetyl, comprising reacting a compound represented by wherein R2 represents a C1-C4 alkyl, R3 represents a C1-C6 alkyl, R4 and R5 represent a hydrogen atom, a C1-C6 alkyl or a phenyl, or R4 and R5 together form a tetramethylene, a pentamethylene or an oxo, with trimethylsilyl azide in the presence of a Lewis acid.
    Type: Grant
    Filed: March 12, 2013
    Date of Patent: November 5, 2013
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Yoshitaka Nakamura, Masakazu Wakayama, Kazuhiro Umeo
  • Publication number: 20130252937
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: March 14, 2013
    Publication date: September 26, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Matthias ECKHARDT, Sara FRATTINI, Dieter HAMPRECHT, Frank HIMMELSBACH, Elke LANGKOPF, Iain LINGARD, Stefan PETERS, Holger WAGNER
  • Publication number: 20130237536
    Abstract: Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.
    Type: Application
    Filed: April 26, 2013
    Publication date: September 12, 2013
    Applicant: The Cleveland Clinic Foundation
    Inventors: Mohamed Naguib Attala, Philippe Diaz
  • Publication number: 20130197072
    Abstract: Methods for manufacturing neuraminic acid compounds and synthetic intermediates of neuraminic acid compounds, including a method for manufacturing a compound represented by wherein R2 represents a C1-C4 alkyl, R3 represents a C1-C6 alkyl, R4 and R5 represent a hydrogen atom, a C1-C6 alkyl or a phenyl, or R4 and R5 together form a tetramethylene, a pentamethylene or an oxo, and Ac represents an acetyl, comprising reacting a compound represented by wherein R2 represents a C1-C4 alkyl, R3 represents a C1-C6 alkyl, R4 and R5 represent a hydrogen atom, a C1-C6 alkyl or a phenyl, or R4 and R5 together form a tetramethylene, a pentamethylene or an oxo, with trimethylsilyl azide in the presence of a Lewis acid.
    Type: Application
    Filed: March 12, 2013
    Publication date: August 1, 2013
    Applicant: DAIICHI SANKYO CO., LTD.
    Inventor: DAIICHI SANKYO CO., LTD.
  • Publication number: 20130123519
    Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate.
    Type: Application
    Filed: January 7, 2013
    Publication date: May 16, 2013
    Inventors: Atsushi Endo, Charles E. Chase, Francis G. Fang
  • Patent number: 8440832
    Abstract: Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: July 14, 2008
    Date of Patent: May 14, 2013
    Assignee: Board of Regents, The University of Texas System
    Inventors: Mohamed Naguib Attala, Philippe Diaz
  • Patent number: 8415121
    Abstract: Improved process for the isolation of laidlomycin from a fermentation broth includes increasing the pH of the fermentation broth and centrifuging the pH adjusted fermentation broth, resulting in an aqueous layer and a wet solid layer containing laidlomycin. After the aqueous layer is removed, the wet solid layer containing laidlomycin is dried. The process provides an efficient and high yielding method.
    Type: Grant
    Filed: September 22, 2010
    Date of Patent: April 9, 2013
    Assignee: Alpharma, LLC
    Inventor: Robert Sheridan
  • Patent number: 8389073
    Abstract: The invention provides a liquid crystal compound that has a large negative dielectric anisotropy (??) and also has at least one of characteristics such as the stability to heat, light or the like, a high clearing point, a suitable refractive index anisotropy (?n), a large negative dielectric anisotropy (??) and an excellent compatibility with other liquid crystal compounds. An excellent effect in which especially the value of the dielectric anisotropy (??) is increased negatively is achieved by use of the compound having two moieties of 1) a tetrahydropyran ring and and thus the effect is utilized.
    Type: Grant
    Filed: February 1, 2010
    Date of Patent: March 5, 2013
    Assignees: JNC Corporation, JNC Petrochemical Corporation
    Inventors: Kenji Hirata, Tokifumi Masukawa, Junichi Yamashita, Maiko Ito
  • Patent number: 8383651
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: February 26, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Doris Riether, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Monika Ermann, Innocent Mushi, Robert John Scott
  • Publication number: 20120302566
    Abstract: The present invention relates to compounds defined by formula (I) wherein the variables R1, R2, R3, m, and n are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are activators of the receptor GPR40 and thus are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: November 30, 2011
    Publication date: November 29, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank Himmelsbach, Remko Bakker, Matthias Eckhardt, Dieter Hamprecht, Elke Langkopf, Holger Wagner
  • Publication number: 20120283198
    Abstract: A halogenated dideoxy sugar derivative, having the following general structure I wherein X is halogen, R1 and R2 are H or Br; R3 and R4 are OH or OAc. The compounds 1-14 of the current invention has strong inhibition effect on human nasopharyngeal cancer CNE-2Z cells, human lung cancer A549 cells. human colon cancer HT-29 cells, human liver cancer Bel-7402 cells, human rectum cancer cells HCE 8693, human stomach cancer BGC-803 cells, human esophagus cancer CaEs-17 cells, human breast cancer cells MCF-7, human ovarian cancer cells A2780, pancreatic cancer cells PC-3, human bladder cells EJ, human brain glia cells TG-905, human leukemia cells K562, human melanoma M 14 cells and human anaplastic thyroid carcinoma TA-K cells. They can be used to prepare anti-tumor medicament and have significant clinic value.
    Type: Application
    Filed: July 2, 2012
    Publication date: November 8, 2012
    Applicant: SUZHOU HARMONY BIOTECHNOLOGY CO., LTD.
    Inventor: Hua MAO
  • Publication number: 20120101091
    Abstract: The present application provides compounds of formula I wherein X, Y, R2, n, R5 and R6 are defined herein, useful as inhibitors of the hepatitis C virus NS5B polymerase The present application also provides pharmaceutical compositions containing said compounds, methods of using said compounds as pharmaceuticals alone or with other antiviral agent in the treatment of a hepatitis C viral infection in a mammal having or at risk of having the infection.
    Type: Application
    Filed: October 1, 2009
    Publication date: April 26, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Pierre Beaulieu, Pierre Bonneau, René Coulombe, Pasquale Forgione, James Gillard, Araz Jakalian, Jean Rancourt
  • Patent number: 8148554
    Abstract: The invention provides methods and compositions for use in treating diseases associated with excessive cellular proliferation, such as cancer, and intermediates for the synthesis of such compositions.
    Type: Grant
    Filed: August 12, 2010
    Date of Patent: April 3, 2012
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Boris M. Seletsky, Melvin J. Yu, Wanjun Zheng
  • Publication number: 20110295023
    Abstract: The nucleotide sequence of a DNA involved in the biosynthesis of herboxidiene was determined. Utilizing this DNA, herboxidiene and analogues thereof can be efficiently produced.
    Type: Application
    Filed: May 27, 2009
    Publication date: December 1, 2011
    Applicants: MERCIAN CORPORATION
    Inventors: Kazuhiro Machida, Kaoru Okayama, Masashi Itoh, Asako Toyoda
  • Publication number: 20110230551
    Abstract: The present invention provides a novel class of withanolides that have been isolated from W. somnifera under aeroponic conditions or produced semi-synthetically from withanolide natural products. The invention also provides pharmaceutical compositions thereof and methods for using the same in proliferative diseases, neurodegenerative diseases, autoimmune, and inflammatory diseases.
    Type: Application
    Filed: September 15, 2009
    Publication date: September 22, 2011
    Inventors: Leslie Gunatilaka, Ekanayake Mudiyanselage Kithsiri Wijeratne, Ya-Ming Xu, Luke Whitesell, Susan L. Lindquist
  • Publication number: 20110190127
    Abstract: Pyranone, thiopyranone and cyclohexenedione compounds of formula (I), which are suitable for use as herbicides.
    Type: Application
    Filed: June 4, 2009
    Publication date: August 4, 2011
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: James Nicholas Scutt, Christopher John Mathews
  • Publication number: 20110184190
    Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate.
    Type: Application
    Filed: January 26, 2011
    Publication date: July 28, 2011
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Atsushi Endo, Charles E. Chase, Francis G. Fang
  • Publication number: 20110015413
    Abstract: Provided herein are methods of preparing crystalline mupirocin calcium dihydrate comprising combining solid mupirocin, solid calcium carbonate, and water in an amount sufficient to form a heterogeneous mixture and precipitate crystalline mupirocin calcium dihydrate from the mixture. In some embodiments, the methods produce nanocrystalline mupirocin calcium dihydrate, suitable for use in pharmaceutical formulations.
    Type: Application
    Filed: December 30, 2008
    Publication date: January 20, 2011
    Inventors: Nafis Defterdarovic, Marijan Tudja, Drazen Cavuzic
  • Patent number: 7868191
    Abstract: The present invention relates to methods for the preparation and purification of mupirocin calcium. The process comprises adsorbing mupirocin to a hydrophobic adsorbent resin, exposing the bound mupirocin to a calcium-containing solution, washing impurities from the resin and eluting purified mupirocin calcium from the resin.
    Type: Grant
    Filed: August 29, 2007
    Date of Patent: January 11, 2011
    Assignee: Xellia Pharmaceuticals ApS
    Inventor: Lene Aassveen
  • Patent number: 7833756
    Abstract: Dibenzorhodamine compounds having the structure are disclosed, including nitrogen- and aryl-substituted forms thereof. In addition, two intermediates useful for synthesizing such compounds are disclosed, a first intermediate having the structure including nitrogen- and aryl-substituted forms thereof, and a second intermediate having the structure including nitrogen- and aryl-substituted forms thereof, wherein substituents at positions C-14 to C18 taken separately are selected from the group consisting of hydrogen, chlorine, fluorine, lower alkyl, carboxylic acid, sulfonic acid, —CH2OH, alkoxy, phenoxy, linking group, and substituted forms thereof. The invention further includes energy transfer dyes comprising the dibenzorhodamine compounds, nucleosides labeled with the dibenzorhodamine compounds, and nucleic acid analysis methods employing the dibenzorhodamine compounds.
    Type: Grant
    Filed: July 8, 2008
    Date of Patent: November 16, 2010
    Assignee: Applied Biosystems, LLC
    Inventors: Scott C. Benson, Joe Y. L. Lam, Steven Michael Menchen
  • Publication number: 20100256156
    Abstract: The present invention provides a heterocyclic compound represented by the following formula (I), which has a glucagon antagonistic action and is useful for the prophylaxis or treatment of diabetes and the like, a compound represented by wherein ring A is an optionally substituted benzene ring and the like; Y is a nitrogen atom and the like; X is —O— and the like; R4 is a hydrogen atom and the like; R5 and R6 are each independently a hydrogen atom and the like; R1 is an optionally substituted hydrocarbon group and the like; R2 is a hydrogen atom and the like; and R3 is —(CH2)3—COOH and the like, or a salt thereof.
    Type: Application
    Filed: October 31, 2008
    Publication date: October 7, 2010
    Inventors: Yoshihiro Banno, Ryoma Hara, Ryosuke Tokunoh
  • Publication number: 20100204220
    Abstract: Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.
    Type: Application
    Filed: July 14, 2008
    Publication date: August 12, 2010
    Inventors: Mohamed Naquib Attala, Philippe Diaz
  • Publication number: 20100197684
    Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: February 9, 2010
    Publication date: August 5, 2010
    Applicant: Gilead Palo Alto, Inc.
    Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki
  • Publication number: 20100179191
    Abstract: Glucopyranosyl-substituted cyclopropyl-benzene derivatives defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.
    Type: Application
    Filed: August 14, 2007
    Publication date: July 15, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank Himmelsbach, Matthias Eckhardt, Peter Eickelmann
  • Patent number: 7635782
    Abstract: This invention relates to a new method for the stereospecific thiocarboxylation of organic compounds for the preparation of compounds according to formula (I): wherein a compound of formula (II): is reacted with a compound of formula (IIIa) or (IIIb): then treating the obtained product with a thiocarboxylic acid or a salt thereof, and subsequently carrying out a nitration reaction.
    Type: Grant
    Filed: February 17, 2009
    Date of Patent: December 22, 2009
    Assignee: Lacer, S.A.
    Inventors: Francisco Pubill Coy, Anna Modolell Saladrigas, Jose Repolles Moliner
  • Patent number: 7619102
    Abstract: A method for purification of the antibiotic mupirocin (pseudomonic acid A) which comprises: a) Causing or allowing precipitation of mupirocin from an aqueous solution thereof; b) Recovering the precipitate; c) Dissolving the recovered precipitate in an organic solvent.
    Type: Grant
    Filed: February 21, 2006
    Date of Patent: November 17, 2009
    Assignee: Axellia Pharmaceuticals ApS
    Inventors: Marc Antonius Theodorus Bisschops, Tiemen Geert Pieter Reijns, Anita Mathiesen, Lene Aassveen
  • Publication number: 20090281175
    Abstract: Compounds of the avermectin family or derivatives thereof, notably latidectin, are formulated into pharmaceutical compositions useful for the treatment of dermatological conditions in humans, in particular rosacea.
    Type: Application
    Filed: March 26, 2009
    Publication date: November 12, 2009
    Applicant: GALDERMA S.A.
    Inventors: Alexandre Kaoukhov, Cecile Cousin
  • Publication number: 20090240071
    Abstract: The present invention relates to methods for the preparation and purification of mupirocin calcium. The process comprises adsorbing mupirocin to a hydrophobic adsorbent resin, exposing the bound mupirocin to a calcium-containing solution, washing impurities from the resin and eluting purified mupirocin calcium from the resin.
    Type: Application
    Filed: August 29, 2007
    Publication date: September 24, 2009
    Applicant: Axellia Pharmaceuticals ApS
    Inventor: Lene Aassveen
  • Patent number: 7569604
    Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.
    Type: Grant
    Filed: June 22, 2005
    Date of Patent: August 4, 2009
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Andreas Termin, Esther Martinborough, Nicole Zimmerman, Charles Cohen, Corey Gutierrez
  • Patent number: 7479502
    Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
    Type: Grant
    Filed: December 3, 2003
    Date of Patent: January 20, 2009
    Assignee: Pharmacyclics, Inc.
    Inventors: Aleksandr Kolesnikov, Roopa Rai, William Dvorak Shrader, Steven M. Torkelson, Kieron E. Wesson, Wendy B. Young
  • Patent number: 7470720
    Abstract: The invention provides methods and compositions for use in treating diseases associated with excessive cellular proliferation, such as cancer.
    Type: Grant
    Filed: October 16, 2003
    Date of Patent: December 30, 2008
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Bruce A. Littlefield, Murray J. Towle
  • Patent number: 7442793
    Abstract: Novel PDF inhibitors and novel methods for their use are provided.
    Type: Grant
    Filed: December 11, 2003
    Date of Patent: October 28, 2008
    Assignee: SmithKline Beecham Corporation
    Inventors: Jinhwa Lee, Siegfried B. Christensen, IV
  • Publication number: 20080249165
    Abstract: The invention relates to new polysulfated glycosides of formula (I), the salts thereof formed with alkali metals or alkaline-earth metals, as well as the pharmaceutical compositions containing these compounds as active ingredients. Furthermore the invention provides a method of preventing, treating or alleviating the symptoms of acute and chronic inflammatory disorders of the airways of mammals—including asthma and asthma-related pathologies.
    Type: Application
    Filed: August 5, 2005
    Publication date: October 9, 2008
    Applicant: Ivax Drug Research Institute Ltd.
    Inventors: Janos Kuszmann, Istvan Kurucz, Gabor Medgyes, Nicholas Bodor