The -c(=x)- Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 546/147)
  • Patent number: 9045458
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Grant
    Filed: May 12, 2014
    Date of Patent: June 2, 2015
    Assignee: SARcode Bioscience Inc.
    Inventors: Min Zhong, Wang Shen, Johan D. Oslob, Kenneth Barr
  • Publication number: 20150105422
    Abstract: (S)-2-(Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Applicant: SPINIFEX PHARMACEUTICALS PTY LTD
    Inventors: Thomas David McCarthy, Craig James Stewart Boyle, Alexander Redvers Eberlin, Peter Michael Kelly
  • Patent number: 9000010
    Abstract: The invention relates to compounds corresponding to the general formula (I): in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or —NR8R9; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C1-6-alkylene or —O—C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4-(4-chlorophenyl)piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: April 7, 2015
    Assignee: Sanofi
    Inventors: Ahmed Abouabdellah, Antoine Ravet
  • Publication number: 20150045387
    Abstract: Bi- and tri-aromatic compounds of the formula (I) wherein R1 to RIO and X are as defined, are Nox2 inhibitors that are useful as medicaments for the treatment of a disease or condition selected from: cardiovascular diseases, respiratory diseases, inflammatory diseases, cancers, ageing and age related disorders, kidney diseases, neurodegenerative diseases, diabetes and conditions associated with diabetes. The compounds, their preparation and pharmaceutical compositions comprising them are disclosed.
    Type: Application
    Filed: September 17, 2012
    Publication date: February 12, 2015
    Inventors: Jian-Mei Li, Brendan Howlin, Daniel Nathan Meijles
  • 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: 8927575
    Abstract: (S)-2-(Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: January 6, 2015
    Assignee: Spinifex Pharmaceuticals Pty Ltd
    Inventors: Thomas David McCarthy, Craig James Stewart Boyle, Alexander Redvers Eberlin, Peter Michael Kelly
  • Publication number: 20140378459
    Abstract: [Problem] Provided is a compound which is useful as an agent for preventing and/or treating renal diseases. [Means for Solution] The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.
    Type: Application
    Filed: September 14, 2012
    Publication date: December 25, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Jiro Fujiyasu, Kazuhiko Ohne, Susumu Yamaki, Tomoyoshi Imaizumi, Takeshi Hondo, Keisuke Matsuura, Tomohki Satou, Satoshi Sasamura
  • Publication number: 20140371265
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: May 12, 2014
    Publication date: December 18, 2014
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier, Min Zhong, Wang Shen, Johan D. Oslob, Kenneth Barr
  • Publication number: 20140323482
    Abstract: The present invention provides a compound of Formula I (The formula should be inserted here) as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
    Type: Application
    Filed: December 17, 2012
    Publication date: October 30, 2014
    Inventors: Yao Ma, Manami Shizuka, Timothy J. Guzi, Yuan Liu, Yuan Tian, Brian R. Lahue, Craig R. Gibeau, Gerald W. Shipps, JR., Yaolin Wang, Stephane L. Bogen, Latha G. Nair, Weidong Pan, Mark A. McCoy, Matthew E. Voss, Margarita Kirova-Snover, W. Bent Clayton
  • Patent number: 8871770
    Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: February 3, 2014
    Date of Patent: October 28, 2014
    Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
  • Publication number: 20140309174
    Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.
    Type: Application
    Filed: November 12, 2013
    Publication date: October 16, 2014
    Applicant: Eisai Co., Ltd
    Inventors: James J. Kowalczyk, Galina Kuznetsov, Shawn Schiller, Boris M. Seletsky, Mark Spyvee, Hu Yang
  • Publication number: 20140303150
    Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
    Type: Application
    Filed: December 22, 2011
    Publication date: October 9, 2014
    Applicant: LEO Laboratories Limited
    Inventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø, Thomas Vifian
  • Publication number: 20140303143
    Abstract: Disclosed are compounds of Formula (A) or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (A) or their salts, and methods of treating neuropathic pain disorders using the same.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 9, 2014
    Inventors: Mark E. Layton, Joseph E. Pero, Hannah Fiji, Michael J. Kelly, III, Pablo de Leon, Michael A. Rossi, Kevin F. Gilbert, Anthony J. Roecker, Zhijian Zhao, Swati I P. Mercer, Scott Wolkenberg, James Mulhearn, Lianyun Zhao, Dansu Li
  • Publication number: 20140288084
    Abstract: In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: October 28, 2012
    Publication date: September 25, 2014
    Applicant: VANDERBILT UNIVERSITY
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Woods, Corey R. Hopkins, Bruce J. Melancon, Michael S. Poslusney, Darren W. Engers
  • Publication number: 20140275028
    Abstract: The present invention relates to compounds of Formula (I), and solvates, hydrates, and pharmaceutically acceptable salts thereof, wherein ring A, R1, R5 and R6 are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Wenying Chai, Charlotte Deckhut, Curt A. Dvorak, Wendy Eccles, James P. Edwards, Steven D. Goldberg, Paul J. Krawczuk, Alec D. Lebsack, Jing Liu, Virginia M. Tanis, Kyle T. Tarantino
  • Publication number: 20140274960
    Abstract: The present invention provides compounds of Formula (I) or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 18, 2014
    Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, Shefali Srivastava
  • Patent number: 8809381
    Abstract: A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula I in which R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle such as, for example, radicals of optionally substituted piperidines, optionally substituted piperazines, optionally substituted tetrahydropyridines, optionally substituted azepanes, tertiary amines (cyclic or acyclic), isoindoline-1,3-dione, or optionally substituted tetrahydroisoquinolones (aromatically substituted): R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.
    Type: Grant
    Filed: August 18, 2008
    Date of Patent: August 19, 2014
    Assignees: The University of Mississippi, L'Universite Catholique de Louvain
    Inventors: Christopher R. McCurdy, Christophe Mesangeau, Sanju Narayanan, Rae Reiko Matsumoto, Jacques Henri Poupaert
  • Publication number: 20140148467
    Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Application
    Filed: February 3, 2014
    Publication date: May 29, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
  • Publication number: 20140135327
    Abstract: This invention relates to the discovery of novel compounds, or pharmaceutically acceptable salts thereof, which possess HDAC inhibitory activity. In particular, the compounds of the invention demonstrate selectivity towards Class I HDAC enzymes, and are accordingly expected to be useful for their anti-proliferative activity and in methods of treatment of the human or animal body, for example in preventing or inhibiting tumour growth and metastasis in cancers. The invention also relates to processes for the manufacture of the compounds defined herein, or pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-proliferative effect in a warm-blooded animal such as man.
    Type: Application
    Filed: July 6, 2012
    Publication date: May 15, 2014
    Applicant: CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Ronald Ernest Grigg, Martyn Inman, Graham Packham
  • Patent number: 8716492
    Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: May 6, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
  • Patent number: 8703955
    Abstract: A process for the resolution of racemic tetrahydropapaverine with optically active arylpropionic acids is described.
    Type: Grant
    Filed: February 25, 2009
    Date of Patent: April 22, 2014
    Assignee: Recordati Industria Chimica e Farmaceutica S.p.A.
    Inventors: Franca Segnalini, Angela Tuozzi, Angelo Gentile
  • Publication number: 20140088069
    Abstract: An antibacterial composition is provided including a combination of a ?-lactam antibiotic that has a binding affinity for bacterial penicillin-binding protein 2; and a non-antibiotic compound which may be a thienopyridine or a non-thienopyridine compound. A method of treatment using the composition is also provided.
    Type: Application
    Filed: November 29, 2013
    Publication date: March 27, 2014
    Inventors: Eric D. Brown, Maya Farha, Alexander Leung, Gerry Wright, Kalinka Koteva, Ted Sewell, Linda Ejim
  • Publication number: 20140080865
    Abstract: (S)-2-(Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described.
    Type: Application
    Filed: November 18, 2013
    Publication date: March 20, 2014
    Applicant: SPINIFEX PHARMACEUTICALS PTY LTD
    Inventors: Thomas David McCarthy, Craig James Stewart Boyle, Alexander Redvers Eberlin, Peter Michael Kelly
  • Patent number: 8633182
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n 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. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: January 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dieter Hamprecht, Sara Frattini, Iain Lingard, Stefan Peters
  • Publication number: 20140005177
    Abstract: A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory diseases and/or allergic conditions, in cancer therapy, specifically heme malignancies, and autoimmune conditions.
    Type: Application
    Filed: March 8, 2012
    Publication date: January 2, 2014
    Applicant: GLAXO GROUP LIMITED
    Inventors: Francis Louis Atkinson, Michael David Barker, John Liddle, David Matthew Wilson
  • Publication number: 20140005382
    Abstract: There are provided compounds represented by the following general formula (I) or pharmaceutically acceptable salts of thereof, which have a superior monoacylglycerol acyltransferase 2 inhibitory action: wherein Ring A represents a partially saturated heteroaryl group, an aryl group or a heteroaryl group, RB represents a C4-18 alkyl group, a C3-8 cycloalkyl group, a partially saturated aryl group, an aryl group, or the following formula (II): wherein V represents the formula —CR11R12—, —CO—, —CO—O—, or —CO—NH—, W represents a single bond or a C1-3 alkylene group, and Ring B represents a C3-8 cycloalkyl group, a C3-8 cycloalkenyl group, a partially saturated heteroaryl group, a saturated heterocyclyl group, an aryl group, or a heteroaryl group, Y represents a nitrogen atom or the formula N+(RF), RF represents a C1-4 alkyl group, and m and n, which may be the same or different, each represent an integer of 0 or 1.
    Type: Application
    Filed: March 14, 2012
    Publication date: January 2, 2014
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Tsuyoshi Busujima, Takahiro Oi, Hiroaki Tanaka, Yoshihisa Shirasaki, Kanako Iwakiri, Nagaaki Sato, Shigeru Tokita
  • Patent number: 8614227
    Abstract: (S)-2-(Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described.
    Type: Grant
    Filed: July 21, 2011
    Date of Patent: December 24, 2013
    Assignee: Spinifex Pharmaceuticals Pty Ltd
    Inventors: Thomas David McCarthy, Craig James Stewart Boyle, Alexander Redvers Eberlin, Peter Michael Kelly
  • Publication number: 20130338132
    Abstract: Compounds represented by the following formula (I), are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.
    Type: Application
    Filed: June 14, 2012
    Publication date: December 19, 2013
    Applicant: Ajinomoto Co., Inc.
    Inventors: Takahiro Koshiba, Munetaka Tokumasu, Taisuke Ichimaru, Koji Ohsumi, Tadakiyo Nakagawa, Tatsuhiro Yamada, Kayo Matsumoto, Tamotsu Suzuki
  • Patent number: 8592451
    Abstract: The invention provides neuromuscular blockade agents of the non-depolarizing type with few if any circulatory effects. Compounds of the invention include bis(isoquinolylalkanol) diesters of fumaric, maleic, succinic, and acetylenedicarboxylic acids; compositions suitable for parenteral administration of these compounds as a surgical adjunct to anesthesia, and methods of preparation of the compounds. Compounds of the invention can produce neuromuscular blockade of short or intermediate duration, which for various compounds can be reversed by administration of a thiol compound such as L-cysteine, D-cysteine or glutathione. For various compounds of the invention, the neuromuscular blockade effect can be reversed quickly, efficiently, and without notable side-effects.
    Type: Grant
    Filed: March 17, 2010
    Date of Patent: November 26, 2013
    Assignee: Cornell University
    Inventor: John J. Savarese
  • Publication number: 20130310559
    Abstract: Among other things, the present invention provides novel isoprenyl compounds capable of effectively modulating inflammatory responses and pharmaceutical, cosmetic, cosmeceutical and topical compositions comprising these isoprenyl compounds. Anti-inflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with inflammation. Proinflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with suppression of inflammatory responses. Thus, the present invention also provides methods useful in the treatment or prevention of diseases or conditions associated with inflammation as well as methods useful in the treatment or prevention of diseases or conditions associated with suppression of inflammatory responses.
    Type: Application
    Filed: February 6, 2013
    Publication date: November 21, 2013
    Applicant: SIGNUM BIOSCIENCES, INC.
    Inventors: Jeffry B. Stock, Maxwell Stock, Keshava Rapole, Seung-Yub Lee, Michael Voronkov, Eduardo Perez, Joel Gordon, Shuyi Chen, Jinglong Chen
  • Publication number: 20130274256
    Abstract: Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms.
    Type: Application
    Filed: October 11, 2012
    Publication date: October 17, 2013
    Applicant: SEQUOIA SCIENCES, INC.
    Inventor: Sequoia Sciences, Inc.
  • Patent number: 8507523
    Abstract: Disclosed are therapeutic tetrahydroisoquinoline compositions for the treatment of cancer, these compositions having selectivity for cancer cells while demonstrating few, if any, deleterious side effects on normal cells.
    Type: Grant
    Filed: November 21, 2007
    Date of Patent: August 13, 2013
    Inventors: Renukadevi Patil, Charles Ryan Yates, Duane D. Miller, Eldon E. Geisert
  • Publication number: 20130184263
    Abstract: The present invention relates to compounds characterized by having a structure according to the following Formula I: or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.
    Type: Application
    Filed: December 14, 2012
    Publication date: July 18, 2013
    Applicant: GlaxoSmithKline LLC
    Inventor: GlaxoSmithKline LLC
  • Patent number: 8461329
    Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.
    Type: Grant
    Filed: December 25, 2009
    Date of Patent: June 11, 2013
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Tetsuo Takayama, Hajime Asanuma, Daisuke Wakasugi, Rie Nishikawa, Yoshinori Sekiguchi, Madoka Kawamura, Naoya Ono, Tetsuya Yabuuchi, Takahiro Oi, Yusuke Oka, Shoichi Kuroda, Fumito Uneuchi, Takeshi Koami
  • Publication number: 20130144063
    Abstract: Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention.
    Type: Application
    Filed: December 11, 2012
    Publication date: June 6, 2013
    Applicant: SARCODE BIOSCIENCE INC.
    Inventor: SARcode Bioscience Inc.
  • Publication number: 20130137874
    Abstract: The present invention provides an efficient process for the preparation of hexahydroisoquinolines from amides. In particular, the invention provides a good yielding, one-pot process for the synthesis of hexahydroisoquinolines.
    Type: Application
    Filed: January 25, 2013
    Publication date: May 30, 2013
    Applicant: Mallinckrodt LLC
    Inventors: Christopher W. Grote, Frank W. Moser, Peter X. Wang, Gary L. Cantrell, David W. Berberich
  • Patent number: 8435984
    Abstract: The present invention provides tertiary amine substituted peptides of Formula (I) useful as inhibitors of HCV replication. The variables R and R1-R12 in Formula I are described herein. The invention also includes methods for preparing such compounds. The present invention further includes pharmaceutical compositions containing tertiary amine substituted peptides and methods for using such compounds, including methods for using the compounds to treat hepatitis C infection.
    Type: Grant
    Filed: February 26, 2008
    Date of Patent: May 7, 2013
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Atul Agarwal, Xiangzhu Wang, Dawei Chen, Suoming Zhang, Avinash Phadke
  • Patent number: 8435983
    Abstract: A method for synthesizing anti-leukemic epothilone analogues includes rigidifying a region between the macrolactone ring and the aromatic side-chain. The anti-leukemic compositions are non-naturally occurring epothilone analogue that are rigidified between the macrolactone ring and the aromatic side-chain.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: May 7, 2013
    Assignee: The University of Toledo
    Inventors: Viranga Tillekeratne, Richard A. Hudson, Mamoun Alhamadsheh
  • Publication number: 20130096310
    Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a pharmaceutical.
    Type: Application
    Filed: June 22, 2011
    Publication date: April 18, 2013
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Tetsuo Takayama, Madoka Kawamura, Daisuke Wakasugi, Rie Nishikawa, Yoshinori Sekiguchi
  • Patent number: 8357807
    Abstract: The present invention provides novel isoquinolinium compounds, methods of producing the isoquinolinium compounds, and methods for converting them into cisatracurium, e.g., cisatracurium besylate. The isoquinolinium compounds of the present invention can be obtained in the form of solids, which can be purified using simple techniques and can be used to afford pure cisatracurium besylate without HPLC purification.
    Type: Grant
    Filed: May 1, 2008
    Date of Patent: January 22, 2013
    Assignee: CHEMAGIS Ltd.
    Inventors: Vladimir Naddaka, Shen Jingshan, Oded Arad, Guo Hongli, Ofer Sharon, Eyal Klopfer, Shady Saeed
  • Publication number: 20120316337
    Abstract: Method for preparing carboxylic acid derivatives by aromatic nucleophilic substitution, in which a carboxylic acid derivative having a single carboxyl functional group, or one of the salts thereof, the carboxylic acid derivative having, in the ortho position of the carboxyl functional group, a leaving group, which is preferably an atom of fluorine or of chlorine or an alkoxy group, chiral or not, preferably a methoxy group, the carboxylic acid derivative not being substituted by an electro attractive group other than the leaving group if any; is reacted with a reactant MNu, where M is a metal and Nu is a nucleophile, chiral or not, the aromatic nucleophilic substitution reaction being carried out without a catalyst and without a step of protecting/deprotecting the acid functional group of the starting compound.
    Type: Application
    Filed: February 17, 2011
    Publication date: December 13, 2012
    Applicants: UNIVERSITE DU MAINE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Jacques Mortier, Anne-Sophie Castanet, Mickael Belaud-Rotureau
  • Publication number: 20120295909
    Abstract: The invention relates to compounds corresponding to the general formula (I): in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or —NR8R9; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C1-6-alkylene or —O—C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4-(4-chlorophenyl)piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.
    Type: Application
    Filed: January 19, 2011
    Publication date: November 22, 2012
    Applicant: SANOFI
    Inventors: Ahmed Abouabdellah, Antoine Ravet
  • Publication number: 20120295906
    Abstract: The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R2, R3, R4, R5 and R6 are as defined in the specification. Further objects of the invention are processes and intermediates for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
    Type: Application
    Filed: July 27, 2012
    Publication date: November 22, 2012
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Ermes Vanotti, Marina Caldarelli, Alessandra Cirla, Barbara Forte, Antonella Ermoli, Maria Menichincheri, Antonio Pillan, Alessandra Scolaro
  • Patent number: 8293912
    Abstract: The present invention provides processes for producing isoquinolinium compounds, and for converting them into cisatracurium salts, e.g.
    Type: Grant
    Filed: May 1, 2008
    Date of Patent: October 23, 2012
    Assignee: Chemagis Ltd.
    Inventors: Vladimir Naddaka, Shen Jingshan, Oded Arad, Guo Hongli, Ofer Sharon, Eyal Klopfer, Shady Saeed
  • Publication number: 20120258929
    Abstract: The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect peptidyl-dipeptidase A; a method for assaying pesticidal activity of a test substance, which comprises a step of measuring the activity of a peptidyl-dipeptidase A in a reaction system in which the peptidyl-dipeptidase A contacts with a test substance, and the like.
    Type: Application
    Filed: June 23, 2006
    Publication date: October 11, 2012
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Yasutaka Shimokawatoko, Marc Van De Craen, Irene Nooren, Sandra Turconi, Yann Naudet, Guy Nys, Jurgen Debaveye
  • Patent number: 8263620
    Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: September 11, 2012
    Assignee: Glaxo Group Limited
    Inventors: Jag Paul Heer, Thomas Daniel Heightman
  • Patent number: 8188115
    Abstract: The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders.
    Type: Grant
    Filed: August 18, 2005
    Date of Patent: May 29, 2012
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Antoni Torrens Jover, Josep Mas Prio, Susana Yenes Minguez, Mónica Garcia Lopez, Alberto Dordal Zueras, Luz Romero Alonso, Helmut Henrich Buschmann
  • Publication number: 20120129818
    Abstract: Ortho methoxy phenolic compounds are provided that include methylenedioxyphenyl ferulate and ferulylproline and derivatives thereof. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating cardiovascular diseases, including hypertension, atherosclerosis, coronary heart disease, angina, stroke, and myocardial infarction, are further provided. The compounds are also useful in reducing low-density lipoprotein oxidation, improving or increasing vasodilation, and reducing plaque destabilization in a subject.
    Type: Application
    Filed: April 23, 2010
    Publication date: May 24, 2012
    Inventor: Desikan Rajagopal
  • Publication number: 20120108529
    Abstract: Compounds useful as protease inhibitors are provided, as are methods of use and preparation of such compounds and compositions containing such compounds. In one embodiment, the compounds are useful for inhibiting HIV protease enzymes, and are therefore useful in slowing the proliferation of HIV.
    Type: Application
    Filed: May 14, 2010
    Publication date: May 3, 2012
    Inventors: Robert R. Webb, II, Mitchell W. Mutz, Kenneth J. Barr
  • Publication number: 20120095040
    Abstract: The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m, n, o and p independently are a number from 0 to 3; A is a covalent bond, an oxygen atom, a C1-6-alkylene group or a —O—C1-6-alkylene group in which the end that is an oxygen atom is bonded to the R1 group while the end that is an alkylene group is bonded to the carbon of the bicyclic compound; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl or trifluoromethyl group; R4 is an optionally substituted 5-membered heterocyclic compound; wherein the compounds can be in the state of a base or an acid addition salt. The invention can be used in therapeutics.
    Type: Application
    Filed: May 11, 2010
    Publication date: April 19, 2012
    Applicant: SANOFI
    Inventors: Ahmed Abouabdellah, Luc Even, Aude Fayol, Julien Vache, Philippe Yauche