Plural Ring Chalcogens In The Polycyclo Ring Sytem (e.g., Methylenedioxyphenyl Containing, Etc.) Patents (Class 548/526)
  • Patent number: 9908846
    Abstract: This invention relates to novel isonitriles, including arylsulfonyl isonitriles, and methods for their synthesis. The isonitriles include a conjugated ring system. The structure is designed with the flexibility to have multiple substitution patterns. The isonitriles may be used in applications including, but not limited to, pharmaceutical compositions.
    Type: Grant
    Filed: February 20, 2015
    Date of Patent: March 6, 2018
    Assignee: Duquesne University of the Holy Spirit
    Inventors: Fraser Fergusson Fleming, Jesus Armando Lujan-Montelongo
  • Publication number: 20150148534
    Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.
    Type: Application
    Filed: June 26, 2014
    Publication date: May 28, 2015
    Inventors: Bradford H. Hirth, Craig Siegel
  • Publication number: 20150133444
    Abstract: The present disclosure provides derivatives of melampomagnolide B (MMB), including carbonates, carbamates, and thiocarbamates. The derivatives may be synthesized via an MMB triazole intermediate. These derivatives are useful for treating cancer in humans.
    Type: Application
    Filed: November 10, 2014
    Publication date: May 14, 2015
    Inventors: Venumadhav Janganati, Narsimha Reddy Penthala, Peter A. Crooks, Craig T. Jordan
  • Publication number: 20150126574
    Abstract: The present disclosure relates to: (a) mandelate salts of atrasentan, (b) pharmaceutical compositions comprising an atrasentan mandelate salt, and, optionally, one or more additional therapeutic agents; (b) methods of using an atrasentan mandelate salt to treat nephropathy, chronic kidney disease, and/or other conditions; (c) kits comprising a first pharmaceutical composition comprising an atrasentan mandelate salt, and, optionally, a second pharmaceutical composition comprising one or more additional therapeutic agents; (d) methods for the preparation of an atrasentan mandelate salt; and (e) atrasentan mandelate salts prepared by such method.
    Type: Application
    Filed: January 12, 2015
    Publication date: May 7, 2015
    Inventors: Yuchuan Gong, Geoff G. Zhang
  • Publication number: 20150126518
    Abstract: The present invention relates to biguanide compounds and use thereof, more particularly, to biguanide derivatives exhibiting excellent effects for inhibition of cancer cell proliferation and inhibition of cancer metastasis and recurrence, a method for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and a method of prevention or treatment of cancer comprising the step of administering an effective amount of the composition to a subject in need thereof.
    Type: Application
    Filed: October 30, 2014
    Publication date: May 7, 2015
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Hong Woo KIM, Ji Sun LEE, Hye Jin HEO, Hong Bum LEE, Jae Kap JEONG, Ji Hyun PARK, Seo-il KIM, Young Woo LEE
  • Publication number: 20150111889
    Abstract: The present invention relates to compounds of the formula (I), wherein the residues A, R1 to R5, Z1 and Z2 have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: May 16, 2013
    Publication date: April 23, 2015
    Applicant: SANOFI
    Inventors: Marc Nazare, Detlef Kozian, Martin Bossart, Werngard Czechtizky, Andreas Evers
  • Patent number: 9012494
    Abstract: The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo,
    Type: Grant
    Filed: April 29, 2005
    Date of Patent: April 21, 2015
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Libuse Jaroskova, Joannes Theodorus Maria Linders, Christophe Francis Robert Nestor Buyck, Louis Jozef Elisabeth Van Der Veken, Vladimir Dimtchev Dimitrov, Theo Teofanov Nikiforov
  • Publication number: 20150093339
    Abstract: The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers,—savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.
    Type: Application
    Filed: October 8, 2014
    Publication date: April 2, 2015
    Inventors: Catherine TACHDJIAN, Andrew P. PATRON, Sara L. ADAMSKI-WERNER, Farid BAKIR, Qing CHEN, Vincent DARMOHUSODO, Stephen Terrence HOBSON, Xiaodong LI, Ming QI, Daniel H. ROGERS, Marketa RINNOVA, Guy SERVANT, Xiao-Qing TANG, Mark ZOLLER, David WALLACE, Amy XING, Klaus GUBERNATOR
  • Patent number: 8993584
    Abstract: Providing a novel control agent for soft rot and a novel control method for the same. A compound having no antibacterial activity against Erwinia carotovora but having a control activity against fungi on soil surface, specifically containing, as the active ingredient, a fungicide comprising any of a strobilurin compound such as azoxystrobin and kresoxim-methyl, an azole compound such as triflumizol, cyazofamid, amisulbrom, and thiophanate-methyl, a carboxamide compound such as penthiopyrad and boscalid, a sulfonamide compound such as flusulfamide, an organic chlorine compound such as chlorothalonil, a dicarboximide compound such as procymidone and iprodione, a phenylpyrrole compound such as fludioxonil, an anilinopyrimidine compound such as mepanipyrim, and a guanidine compound such as iminoctadine is the control agent for plant soft rot, which is applied to plant cultivation soil.
    Type: Grant
    Filed: July 21, 2011
    Date of Patent: March 31, 2015
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Koji Sugimoto, Hiroyuki Hayashi
  • Patent number: 8961959
    Abstract: Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.
    Type: Grant
    Filed: October 15, 2012
    Date of Patent: February 24, 2015
    Assignee: The Regents of the University of Michigan
    Inventors: Scott Larsen, Akira Abe, Liming Shu, Michael William Wilson, Richard F. Keep, James A. Shayman
  • Publication number: 20150045327
    Abstract: The present invention discloses compounds according to Formula I: wherein R1 is as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment cystic fibrosis by administering a compound of the invention.
    Type: Application
    Filed: August 5, 2014
    Publication date: February 12, 2015
    Inventors: Steven Emiel VAN DER PLAS, Hans KELGTERMANS, Sébastien Jean Jacques Cédric DROPSIT MONTOVER, Sébastien Laurent Xavier MARTINA, Martin James Inglis ANDREWS
  • Patent number: 8952050
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: September 25, 2013
    Date of Patent: February 10, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Sabina Hadida Ruah, Peter Diederik Jan Grootenhuis, Fredrick F. Van Goor, Jinglan Zhou, Brian Richard Bear, Mark Thomas Miller, Jason McCartney, Mehdi Numa, Xiaoqing Yang
  • Patent number: 8952049
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: February 28, 2013
    Date of Patent: February 10, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Sabina Hadida Ruah, Peter Diederik Jan Grootenhuis, Fredrick F. Van Goor, Jinglan Zhou, Brian Richard Bear, Mark Thomas Miller, Jason McCartney, Mehdi Michel Djamel Numa
  • Patent number: 8940776
    Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 27, 2012
    Date of Patent: January 27, 2015
    Assignee: Genzyme Corporation
    Inventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
  • Publication number: 20150014607
    Abstract: There is provided an organic nonlinear optical material including a polymer binder and a compound represented by the following Formula (I): wherein, in Formula (I), R1 and R2 each independently represent a substituted or unsubstituted alkyl group or a substituted or unsubstituted aryl group; R3 represents a hydrogen atom, a substituted or unsubstituted alkyl group, or a substituted or unsubstituted aryl group; and L represents a divalent linking group connecting a nitrogen atom and an oxopyrroline ring having a dicyanomethylidene group in a ?-conjugated system containing an azo group (—N?N—).
    Type: Application
    Filed: September 26, 2014
    Publication date: January 15, 2015
    Applicant: FUJIFILM CORPORATION
    Inventors: Akihiro KANEKO, Masaaki TSUKASE, Masataka SATOU
  • Publication number: 20140359951
    Abstract: An agent for oxidative coloring of keratin-containing fibers, in particular human hair, includes as oxidation dye precursor of the developer type at least one compound of formula (I).
    Type: Application
    Filed: August 22, 2014
    Publication date: December 11, 2014
    Inventors: Antje Gebert, Annika Koenen
  • Publication number: 20140343283
    Abstract: The present invention relates to the technical field of medicine, and specifically provides methods for preparing Icotinib, Icotinib hydrochloride, and intermediates thereof. These methods avoid the use of phosphorus oxychloride, thereby greatly reducing the emission of pollutants, which is of major benefits to the economy and environment.
    Type: Application
    Filed: December 28, 2012
    Publication date: November 20, 2014
    Applicant: BETTA PHARMACEUTICALS CO., LTD.
    Inventors: Shaojing Hu, Wei Long, Fei Wang, Zongquan Li
  • Publication number: 20140343070
    Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof, or a prodrug the
    Type: Application
    Filed: August 1, 2014
    Publication date: November 20, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
  • Patent number: 8884027
    Abstract: Melampomagnolide B is disclosed as a new antileukemic sesquiterpene. A biotin-conjugated derivative of melampomagnolide B was prepared to elucidate its mechanism of action. Prodrugs of Melampomagnolide B are disclosed.
    Type: Grant
    Filed: October 21, 2011
    Date of Patent: November 11, 2014
    Assignees: University of Rochester, University of Kentucky Research Foundation
    Inventors: Peter A. Crooks, Craig T. Jordan, Shanshan Pei, Shama Nasim
  • Publication number: 20140309418
    Abstract: Gambogenic acid derivatives having a structure shown as Formula (I) or (II), salts, preparation method and application thereof in the treatment of tumor. Compared with gambogenic acid, the gambogenic acid derivatives exhibit more potent anti-tumor activities.
    Type: Application
    Filed: September 28, 2012
    Publication date: October 16, 2014
    Inventors: Wantao Chen, Xu Wang, Zhiyuan Zhang, Chenping Zhang, Li Mao, Ping Zhang, Qin Xu, Ming Yan, Jianjun Zhang, Jinsong Pan, Yan Lv, Rongxin Deng, Weiliu Qiu
  • Publication number: 20140288065
    Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
    Type: Application
    Filed: June 10, 2014
    Publication date: September 25, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Muneaki KURIMURA, Shinichi TAIRA, Takahiro TOMOYASU, Nobuaki ITO, Kuninori TAI, Noriaki TAKEMURA, Takayuki MATSUZAKI, Yasuhiro MENJO, Shin MIYAMURA, Yohji SAKURAI, Akihito WATANABE, Yasuyo SAKATA, Takumi MASUMOTO, Kohei AKAZAWA, Haruhiko SUGINO, Naoki AMADA, Satoshi OHASHI, Tomoichi SHINOHARA, Hirofumi SASAKI, Chisako MORITA, Junko YAMASHITA, Satoko NAKAJIMA
  • Publication number: 20140273252
    Abstract: Compound tags and shifting agents are provided that find use in ion mobility spectrometry (IMS), mass spectrometry (MS), or a combination of IMS and MS, and which can substantially increase separation of multiple components in complex samples and facilitate quantitative and multiplexed analyses. In some cases, the compounds include a linker and a normalizing group, each including a structural unit and separated by a cleaveable group, and a crown ether. Also provided are methods for analyzing peptides in a sample. In some cases, the method includes coupling the compound to peptides which include a terminal guanidinium moiety capable of forming an intra-molecular complex with the crown ether.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: Agilent Technologies, Inc.
    Inventors: Brian Phillip Smart, Joel Myerson, Craig Daniel Wenger, Javier E. Satulovsky
  • Publication number: 20140256712
    Abstract: Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 11, 2014
    Applicants: Psychogenics Inc., Sunovion Pharmaceuticals Inc.
    Inventors: Liming SHAO, John Emmerson CAMPBELL, Michael Charles HEWITT, Una CAMPBELL, Taleen G. HANANIA
  • Publication number: 20140249319
    Abstract: Chemical crosslinkers and methods of their synthesis are disclosed.
    Type: Application
    Filed: March 1, 2013
    Publication date: September 4, 2014
    Inventor: Mark Quang Nguyen
  • Patent number: 8779163
    Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.
    Type: Grant
    Filed: March 14, 2012
    Date of Patent: July 15, 2014
    Assignee: Genzyme Corporation
    Inventors: Bradford H. Hirth, Craig Siegel
  • Patent number: 8729063
    Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: May 20, 2014
    Assignee: Incyte Corporation
    Inventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taishing Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
  • Publication number: 20140135310
    Abstract: Sulphonamide derivatives of alicyclic amines of formula (I), wherein A represents naphthyl or 9- or 10-membered bicyclic group, consisting of benzene ring fused with 5- or 6-membered heterocyclic ring; D represents phenyl, naphthyl, 5-membered aromatic heterocyclic group, bicyclic group consisting of a ring selected from benzene and pyridine, fused with aromatic or non-aromatic 5-membered heterocyclic ring; p, r independently represent 0 or 1; x, z independently represent 1 or 2; n is 2 or 3; and enancjomers, pharmaceutically acceptable salts and solvates thereof. The compounds may be useful for the treatment and/or prevention of the central nervous system disorders.
    Type: Application
    Filed: June 29, 2012
    Publication date: May 15, 2014
    Applicant: Adamed Sp. z o.o.
    Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Maciej Pawlowski, Andrzej Krukowski, Rafal Rusiecki, Agata Magdalena Siwek, Malgorzata Anna Wolak
  • Publication number: 20140135373
    Abstract: Compound with formula (I), wherein R? and R? represent a hydrogen atom, a monovalent radical with formula (IIa), or a monovalent radical with formula (IIb), it being understood that at least one of the R? or R? radicals does not represent a hydrogen atom and that when the R? and R? radicals do not represent a hydrogen atom, R? and R? are identical; method for preparing and using in cosmetics and as a drug.
    Type: Application
    Filed: May 24, 2012
    Publication date: May 15, 2014
    Applicant: SOCIETE D'EXPLOITATION DE PROUITS POUR LES INDUSTRIES CHMIQUES SEPPIC
    Inventors: Andre Benattar, Laetitia Cattuzzato, Sandy Dumont, Stephanie Garcel, Jerome Guilbot, Sebastien Kkerverdo, Herve Rolland
  • Publication number: 20140128436
    Abstract: The present invention provides prodrugs of compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating plasma kallikrein dependent diseases or conditions, for example, diabetic macular edema, with the prodrugs having the formula:
    Type: Application
    Filed: November 8, 2013
    Publication date: May 8, 2014
    Applicant: ActiveSite Pharmaceuticals, Inc.
    Inventors: Sukanto Sinha, Tamie Jo Chilcote
  • Patent number: 8716329
    Abstract: The present invention provides compounds of the formula (I) wherein: X1, X2 and X3 are heteroatoms; R4, R5, R6, R7, R8, R9 and R10 are independently selected from H, halo, —OH, —NO2, —CN and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and Z is optionally substituted C1-8 straight-chained or branched aliphatic, optionally containing 1 or more double or triple bonds, wherein one or more carbons are optionally replaced by R* wherein R* is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; an amino acid residue, H, —CN, —C(O)—, —C(O)C(O)—, —C(O)NR1—, —C(O)NR1NR2—, —C(O)O—, —OC(O)—, —NR1CO2—, —O—, —NR1C(O)NR2—, —OC(O)NR1—, —NR1NR2—, —NR1C(O)—, —S—, —SO—, —SO2—, —NR1—, —SO2NR1—, —NR1R2, or —NR1SO2—, wherein R1 and R2 are independently selected from H and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or where R* is NR1R2, R1 and R2 optionally together with the nitrogen atom form an optionally substituted 5-12 me
    Type: Grant
    Filed: June 24, 2013
    Date of Patent: May 6, 2014
    Assignee: University of Kentucky
    Inventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
  • Publication number: 20140100211
    Abstract: Pyrrolidine derivatives of the formula and their use as medicaments for the treatment of obesity and type 2 diabetes.
    Type: Application
    Filed: October 1, 2013
    Publication date: April 10, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
  • Publication number: 20140088078
    Abstract: The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Application
    Filed: May 7, 2012
    Publication date: March 27, 2014
    Applicant: ZAFGEN, Inc.
    Inventors: Susan Mary Cramp, Hazel Joan Dyke, Thomas David Pallin, Robert Zahler
  • Publication number: 20140024647
    Abstract: A compound having TRPV4 inhibitory activity or a pharmaceutically acceptable salt thereof is provided. The present invention is related to a compound represented by the formula (I), wherein R1a is substituted or unsubstituted alkyl or the like; R1b is hydrogen or substituted or unsubstituted alkyl; R1c is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted nonaromatic heterocyclic group or the like; -L- is —C(=0)—NR2? or the like; X is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or the like, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 18, 2012
    Publication date: January 23, 2014
    Inventor: Akira Yukimasa
  • Publication number: 20140018342
    Abstract: Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
    Type: Application
    Filed: April 4, 2012
    Publication date: January 16, 2014
    Inventors: Wen-Lian Wu, Duane A. Burnett, William J. Greenlee
  • Patent number: 8623905
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFFR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: April 26, 2010
    Date of Patent: January 7, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick F. van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Djamel Numa
  • Publication number: 20130345195
    Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Application
    Filed: August 23, 2013
    Publication date: December 26, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Asitha ABEYWARDANE, Michael J. BURKE, Thomas Martin KIRRANE, Matthew Russell NETHERTON, Anil Kumar PADYANA, Lana Louise SMITH KEENAN, Hidenori TAKAHASHI, Michael Robert TURNER, QIANG ZHANG, Qing ZHANG
  • Publication number: 20130338095
    Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.
    Type: Application
    Filed: October 18, 2011
    Publication date: December 19, 2013
    Applicant: ELCELYX THERAPEUTICS, INC.
    Inventors: Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley
  • Publication number: 20130323203
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: August 2, 2013
    Publication date: December 5, 2013
    Applicant: Gilead Sciences, Inc.
    Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Michael Mertzman Belmont, Philip Anthony Morganelli, William J. Watkins
  • Publication number: 20130310419
    Abstract: The present invention is related to pyrrole derivatives of formula I as the modulators of nicotinic acetylcholine receptors particularly the ?7 subtype. The invention includes pyrrole derivatives, analogues, their prodrugs, their isotopes, their metabolites, pharmaceutically acceptable salts, polymorphs, solvates, optical isomers, clathrates, co-crystals, combinations with suitable medicament and pharmaceutical compositions thereof. The present invention also includes process of preparation of the said compounds and intended use in therapy of them. Owing to the modulatory activity of the pyrrole derivatives on the nicotinic acetylcholine receptors, the invention finds application in the prophylaxis and therapy of disorders encompassing the involvement of cholinergic transmission in the central and peripheral nervous system.
    Type: Application
    Filed: January 31, 2012
    Publication date: November 21, 2013
    Applicant: LUPIN LIMITED
    Inventors: Neelima Sinha, Gourhari Jana, Navnath Popat Karche, Shridhar Keshav Adurkar, Girish Dhanraj Hatnapure, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20130295261
    Abstract: The present invention provides isosorbide derivatives having the formula shown below and certain subgenera or species thereof, as flavor or taste modifiers, particularly, savory (“umami”) taste modifiers, savory flavoring agents and savory flavor enhancers in foods, beverages, and other comestible compositions,
    Type: Application
    Filed: March 13, 2013
    Publication date: November 7, 2013
    Applicant: SENOMYX, INC.
    Inventors: Catherine TACHDJIAN, Donald S. Karanewsky, Sara L. Adamski-Werner, Jeffrey M. Yamamoto, Guy Servant
  • Patent number: 8575209
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: November 17, 2010
    Date of Patent: November 5, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick F. Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Numa, Xiaoqing Yang
  • Publication number: 20130289067
    Abstract: Inhibitors of HIV-1 protease and compositions containing them are described. Use of the inhibitors and compositions containing them to treat HIV, AIDS, and AIDS-related diseases is described.
    Type: Application
    Filed: June 27, 2013
    Publication date: October 31, 2013
    Inventors: Arun K. GHOSH, Bruno D. Chapsal, Hiroaki Mitsuya
  • Publication number: 20130281453
    Abstract: Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar IC50 values. An exemplary compound of the invention was shown to be an effective inhibitor of prostate cancer pathogenesis. Other inhibitory compounds of the invention comprising fluorophore groups are shown to be effective in spatial and temporal localization of the serine hydrolase in cells and tissues.
    Type: Application
    Filed: October 21, 2011
    Publication date: October 24, 2013
    Applicant: The Scripps Research Institute
    Inventors: Benjamin Cravatt, Daniel Nomura, Jae W. Chang, Raymond E. Moellering, Dan Bachovehin, Weiwei Li
  • Patent number: 8563593
    Abstract: The present invention relates to formulations of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), pharmaceutical packs or kits thereof, and methods of treatment therewith.
    Type: Grant
    Filed: June 8, 2011
    Date of Patent: October 22, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Rossitza Gueorguieva Alargova, Irina Nikolaevna Kadiyala, Noreen Tasneem Zaman
  • Patent number: 8551364
    Abstract: A process for inhibiting polymerization of an aromatic vinyl compound during the stage of producing, purifying, storing or transporting the aromatic vinyl compound which not only inhibits an initial polymerization but also inhibits polymerization efficiently over a long period of time and which is excellent in handleability. The process involves the step of adding a nitrogenous aromatic compound in combination with a sulfonic acid compound to the aromatic vinyl compound during the production, purification, storage of transportation thereof.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: October 8, 2013
    Assignee: Hakuto Co., Ltd.
    Inventors: Junichi Nakajima, Seiji Tanizaki
  • Patent number: 8551982
    Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Grant
    Filed: March 13, 2012
    Date of Patent: October 8, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
  • Patent number: 8518874
    Abstract: The present invention is directed to compounds that are antiviral agents. Specifically the compounds of the present invention inhibit replication of HCV and are therefore useful in treating hepatitis C infections. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
    Type: Grant
    Filed: October 23, 2009
    Date of Patent: August 27, 2013
    Assignee: Virobay, Inc.
    Inventors: Michael Graupe, John O. Link, Chandrasekar Venkataramani
  • Publication number: 20130210167
    Abstract: The invention describes antibodies that bind molecules of the pyrrolidinophenone class of synthetic drugs. The antibodies are derived from novel chemical intermediates, haptens and immunogens and are used in methods and kits to detect and quantify pyrrolidinophenones.
    Type: Application
    Filed: February 8, 2013
    Publication date: August 15, 2013
    Applicant: RANDOX LABORATORIES LIMITED
    Inventor: Randox Laboratories Limited
  • Publication number: 20130196973
    Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Application
    Filed: March 13, 2012
    Publication date: August 1, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
  • Patent number: 8492372
    Abstract: The present invention relates to novel 1-(4H-1,3-benzodioxin-2-yl)methanamine derivatives, useful as modulators of dopamine neurotransmission, and more specifically asdopaminergic stabilizers. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: April 28, 2009
    Date of Patent: July 23, 2013
    Assignee: Integrated Research Laboratories Sweden AB
    Inventors: Clas Sonesson, Peder Svensson, Mikael Andersson