Plural Ring Oxygens In The Additional Hetero Ring Patents (Class 546/283.7)
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Publication number: 20130245063Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: April 26, 2013Publication date: September 19, 2013Applicant: CalciMedica, Inc.Inventors: Jeffrey P. Whitten, Jonathan Grey, Jianguo Cao, Zhijun Wang, Evan Rogers
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Publication number: 20130245011Abstract: 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 (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: May 6, 2013Publication date: September 19, 2013Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
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Publication number: 20130245010Abstract: 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 (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: April 26, 2013Publication date: September 19, 2013Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
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Patent number: 8524910Abstract: The present invention relates to modulators of Formula I and the accompanying definitions herein of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases such as cystic fibrosis using such modulators.Type: GrantFiled: June 26, 2012Date of Patent: September 3, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
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Patent number: 8519142Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: September 14, 2012Date of Patent: August 27, 2013Assignee: Novartis AGInventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
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Patent number: 8507534Abstract: The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.Type: GrantFiled: December 4, 2008Date of Patent: August 13, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
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Patent number: 8507687Abstract: The present invention relates to a substantially a solid form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 1, Solvate Form A and Compound 1, HCl Salt Form A), processes for making such forms, pharmaceutical compositions thereof, and methods of treatment therewith.Type: GrantFiled: April 7, 2011Date of Patent: August 13, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
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Publication number: 20130203747Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.Type: ApplicationFiled: November 21, 2012Publication date: August 8, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Publication number: 20130202573Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: June 15, 2011Publication date: August 8, 2013Applicant: Ardea Biosciences, Inc.Inventors: Samedy Ouk, Esmir Gunic, Jean-Michel Vernier, Chixu Chen
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Patent number: 8470834Abstract: The present invention provides compounds of Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19, and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.Type: GrantFiled: August 19, 2009Date of Patent: June 25, 2013Assignees: Merck Sharp & Dohme Corp., Southern Research InstituteInventors: Cecil D. Kwong, F. George Njoroge, Subramaniam Ananthan, Feng Geng, Hollis S. Kezar, III, Joseph A. Maddry, John J. Piwinski, Robert C. Reynolds, John A. Secrist, III, Neng-Yang Shih
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Publication number: 20130158261Abstract: The present invention provides HIV protease inhibitors of formulas I, IA, IB, Ib or II, or pharmaceutically acceptable salts thereof, wherein R2 may be, for example, 2-pyridyl-CH2—, 3-pyridyl-CH2—, 4-pyridyl-CH2—, a sulfonyl group as described in the formulas herein including benzenesulfonyl or thiophenesulfonyl groups, R2a—CO)—, R2a being selected from the group consisting of piperonyl, 2-pyranzinyl (unsubstituted or substituted with H, or an alkyl of 1 to 4 carbon atoms) or a picolylamine group as described herein, wherein R3 may be, for example, a phenyl group or diphenylmethyl group as described herein, and wherein Cx may be, for example, COOH, CONR5R6, CH2OH or CH2OR7.Type: ApplicationFiled: February 15, 2013Publication date: June 20, 2013Applicant: TaiMed Biologics, Inc.Inventor: TaiMed Biologics, Inc.
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Patent number: 8461342Abstract: The present invention relates to a process of providing the 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in substantially free form (Compound 1).Type: GrantFiled: April 19, 2012Date of Patent: June 11, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventor: David Andrew Siesel
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Patent number: 8455497Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: February 12, 2009Date of Patent: June 4, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
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Publication number: 20130085158Abstract: The present invention relates to a substantially a solid form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 1, Solvate Form A and Compound 1, HCl Salt Form A), processes for making such forms, pharmaceutical compositions thereof, and methods of treatment therewith.Type: ApplicationFiled: October 5, 2012Publication date: April 4, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventor: VERTEX PHARMACEUTICALS INCORPORATED
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Publication number: 20130035358Abstract: There is provided compounds of formula I, wherein E1, E2a, E2b, E2c, E4, D1, D2, D3, L1, Y1, L2 and Y2 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.Type: ApplicationFiled: March 14, 2011Publication date: February 7, 2013Inventors: Peter Nilsson, Benjamin Pelcman, Martins Katkevics, Robert Ronn, Christian Krog-Jensen
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Publication number: 20130035354Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: September 14, 2012Publication date: February 7, 2013Applicant: NOVARTIS AGInventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
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Publication number: 20130023538Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: September 26, 2012Publication date: January 24, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
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Publication number: 20130023567Abstract: A compound for use in the treatment of proliferative disorders, such as cancer, having the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the specification.Type: ApplicationFiled: July 25, 2012Publication date: January 24, 2013Applicant: Spear Therapeutics LimitedInventors: Gerard A. Potter, Philip Huxley, Kenneth J. Beresford
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Patent number: 8354435Abstract: The present invention provides compounds that function as modulators of aldehyde dehydrogenase activity; and pharmaceutical compositions comprising the compounds. The present invention provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: GrantFiled: September 3, 2009Date of Patent: January 15, 2013Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Che-Hong Chen, Daria Mochly-Rosen, Wenjin Yang
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Publication number: 20130005574Abstract: 3-alkoxy, thioalkyl and amino-4-amino-6-(substituted)picolinic acids having a halogen, alkyl or mono-, di- tri- and tetra-substituted aryl substituents in the 6-position, and their acid derivatives, are herbicides demonstrating a broad spectrum of weed control.Type: ApplicationFiled: June 29, 2012Publication date: January 3, 2013Inventors: Jeffrey B. Epp, Christian T. Lowe, James M. Renga, Paul R. Schmitzer, Joseph D. Eckelbarger, Katherine A. Guenthenspberger, Thomas L. Siddall, Carla N. Yerkes, Lindsey G. Fischer, Natalie C. Giampietro, Jeremy Kister, Joshua Roth
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Publication number: 20120322801Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.Type: ApplicationFiled: March 4, 2011Publication date: December 20, 2012Applicant: Amakem NVInventors: Dirk Leysen, Olivier Defert, Nadzeya Kaval, Petra Blom, Sandro Boland
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Publication number: 20120316182Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: June 8, 2012Publication date: December 13, 2012Applicant: CalciMedica, Inc.Inventors: Jeffrey P. WHITTEN, Jonathan Grey, Jianguo Cao, Zhijun Wang, Evan Rogers
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Publication number: 20120309977Abstract: Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]aminolacetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, [(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibitors or for treating conditions wherein prolyl hydroxylase inhibition is desired.Type: ApplicationFiled: June 5, 2012Publication date: December 6, 2012Applicant: Akebia Therapeutics Inc.Inventors: Christopher M. Lanthier, Boris Gorin, Jan Oudenes, Craig Edward Dixon, Alan Quigbo Lu, James Densmore Copp, John Michael Janusz
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Publication number: 20120295889Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: May 16, 2012Publication date: November 22, 2012Applicant: Merck Serono S.A.Inventors: Ulrich Abel, Holger Deppe, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
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Publication number: 20120277232Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: July 9, 2012Publication date: November 1, 2012Inventors: Urs BAETTIG, Kamlesh Jagdis BALA, Emma BUDD, Lee EDWARDS, Catherine Howsham, Glyn HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
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Publication number: 20120277252Abstract: The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use. For example, the present invention provides chalcone and cyanopyridine compounds, and derivatives thereof, exhibiting high antibacterial activities having multiple electron withdrawing group substituents, such as halogens and fluorinated alkyl groups, and optionally having hydroxyl and/or alkoxyl groups substituents.Type: ApplicationFiled: July 6, 2012Publication date: November 1, 2012Inventors: Helen E. Blackwell, Matthew D. Bowman, Jennifer C. O'Neill, Joseph R. Stringer
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Publication number: 20120277268Abstract: The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.Type: ApplicationFiled: May 9, 2012Publication date: November 1, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
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Publication number: 20120270869Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: June 26, 2012Publication date: October 25, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
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Publication number: 20120263659Abstract: The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.Type: ApplicationFiled: November 22, 2010Publication date: October 18, 2012Applicants: BASF SE, SYMRISE AGInventors: Thomas Subkowski, Michael Backes, Heiko Oertling, Arnold Machinek, Hubert Loges, Ulrike Simchen, Horst Surburg, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel
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Publication number: 20120220634Abstract: The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation.Type: ApplicationFiled: April 25, 2012Publication date: August 30, 2012Applicant: Genta IncorporatedInventors: John K. Thottathil, Raymond P. Warrell
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Patent number: 8247437Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: June 8, 2011Date of Patent: August 21, 2012Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Publication number: 20120203006Abstract: The present invention relates to a process of providing the 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in substantially free form (Compound 1).Type: ApplicationFiled: April 19, 2012Publication date: August 9, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: David Siesel
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Publication number: 20120201763Abstract: 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: ApplicationFiled: December 23, 2011Publication date: August 9, 2012Applicant: SENOMYX, INC.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, Daivd Wallace, Amy Xing, Klaus Gubernator
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Patent number: 8236827Abstract: A compound for use in the treatment of proliferative disorders, such as cancer, having the following formula: wherein: R1, R2 and R3 are independently H or lower alkyl; R4, R5, R6, R7 and R8 are independently H, halo, lower alkyl or —O-lower alkyl, provided that at least one is —O-lower alkyl; or at least one pair of R4 to R8, the members of which pair are adjacent to one another on the ring, are conjoined to form —O—(CR14R15)n—O—, where n is 1 or 2 and R14 and R15 are independently H or lower alkyl, and the remainder of R4 to R8 are independently H, halo, lower alkyl or —O-lower alkyl; and R9, R10, R11, R12 and R13 are independently H, halo, lower alkyl or —O— lower alkyl, provided that at least one is —O-lower alkyl; or at least one pair of R9 to R13, the members of which pair are adjacent to one another on the ring, are conjoined to form —O—(CR16R17)m—O—, where m is 1 or 2 and R16 and R17 are independently H or lower alkyl, and the remainder of R9 to R13 are independently H, halo, lower alkyl or —O-Type: GrantFiled: June 4, 2009Date of Patent: August 7, 2012Assignee: Spear Therapeutics LimitedInventors: Gerard Andrew Potter, Philip Huxley, Kenneth James Beresford
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Publication number: 20120190551Abstract: Arylalkyl esters of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are herbicides for control of weeds especially those species common to rice and wheat cropping systems and in pasture management programs.Type: ApplicationFiled: January 24, 2012Publication date: July 26, 2012Applicant: DOW AGROSCIENCES LLCInventors: Carla N. Yerkes, Christian T. Lowe, Joseph D. Eckelbarger, Jeffrey B. Epp, Katherine A. Guenthenspberger, Thomas L. Siddall, Paul R. Schmitzer
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Publication number: 20120190856Abstract: The present invention relates to a process of providing the 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in substantially free form (Compound 1).Type: ApplicationFiled: January 17, 2012Publication date: July 26, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: David Siesel
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Patent number: 8227615Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: March 25, 2009Date of Patent: July 24, 2012Assignee: Vertex Pharmaceutical IncorporatedInventors: Sara Hadida-Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
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NOVEL SUBSTITUTED PICOLINIC ACIDS, SALTS AND ACID DERIVATIVES THEREOF, AND USE THEREOF AS HERBICIDES
Publication number: 20120157314Abstract: The present invention relates to novel, herbicidally active picolinic acid derivatives of the formula (I) and to processes for preparation thereof. The present invention further provides for the use thereof as a herbicide, especially as a herbicide for selective control of weed plants in useful plant crops, and as a plant growth regulator alone or in combination with safeners and/or in a mixture with other herbicides.Type: ApplicationFiled: October 21, 2011Publication date: June 21, 2012Applicant: BAYER CROPSCIENCE AGInventors: Hartmut AHRENS, Marco BRÜNJES, Hansjörg DIETRICH, Elmar GATZWEILER, Isolde HÄUSER-HAHN, Stefan LEHR, Dirk SCHMUTZLER -
Publication number: 20120129818Abstract: 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: ApplicationFiled: April 23, 2010Publication date: May 24, 2012Inventor: Desikan Rajagopal
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Publication number: 20120121783Abstract: A compound (including salts thereof) according to Formula I in which R1 is H, methyl or ethyl; R2 is H, OH, fluorine, C1-C4 linear or branched alkyl, C1-C6 alkoxy wherein the alkyl group is linear or branched, or a C3-C5 cycloalkyl moiety; R3 is H, methoxy, methyl or ethyl; or R2 and R3 together form a bridging moiety —O—CH2—O— between the phenyl carbon atoms to which they are connected; R4 is OH or methoxy; and R5 and R6 are independently H or methyl; R1, R2, R3, R4, R5 and R6 are such that, (i) when R2 and R3 together form a bridging moiety —O—CH2—O— between the phenyl carbon atoms to which they are connected, R1, R5, R6 are H, and R4 is OH; and (ii) when R4 is OH and R1—R3 are H, at least one of R5, R6 is methyl.Type: ApplicationFiled: July 9, 2010Publication date: May 17, 2012Inventors: Yili Wang, Andrew Daniher, Adri De Klerk, Cornelis Winkel
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Publication number: 20120101097Abstract: The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases.Type: ApplicationFiled: March 10, 2011Publication date: April 26, 2012Inventors: Solomon Ungashe, John Jessen Wright, Andrew Pennell
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Publication number: 20120100990Abstract: The present invention relates to substituted 4-aminopicolinates as well as N-oxides and agriculturally acceptable salts thereof, and their use in controlling plant growth, particularly undesirable plant growth, in crops of useful plants. The invention extends to herbicidal compositions comprising such compounds, N-oxides and/or salts as well as mixtures of the same with one or more further active ingredients and/or a safener.Type: ApplicationFiled: June 21, 2010Publication date: April 26, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: William Guy Whittingham, Shuji Hachisu, Matthew Brian Hotson
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Publication number: 20120088741Abstract: Certain aryl-substituted heterocyclic urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis).Type: ApplicationFiled: June 4, 2010Publication date: April 12, 2012Inventors: J. Guy Breitenbucher, Mark S. Tichenor, Jeffrey E. Merit, John M. Keith, Natallie A. Hawryluk, Alison L. Chambers
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Publication number: 20120071661Abstract: A chiral ionic compound comprising an alkyl substituted imidazolium or pyridinium cationic core having an alkyl ester side chain (-alkyl-C(O)O—) directly linked to the core and an associated counter anion, characterized in that the —O— atom of the ester side chain is linked to an alpha, a beta or a gamma hydroxycarboxylic acid functionality via the alpha, beta or gamma hydroxy of the acid functionality and the hydroxycarboxylic acid functionality has at least one asymmetric carbon, or characterized in that an —N? atom of the alkyl substituted imidazolium or pyridinium cationic core is substituted with an alpha, a beta or a gamma hydroxy group of a alpha, a beta or a gamma hydroxycarboxylic acid functionality and the hydroxycarboxylic acid functionality has at least one asymmetric carbon. The chiral ionic liquids (CILs) may be used as novel solvents, in particular for organic synthesis. The CILs have the potential to induce asymmetry into substrates or catalysts in a variety of organic transformations.Type: ApplicationFiled: February 24, 2010Publication date: March 22, 2012Inventors: Nicholas Gathergood, Bruce Pegot, Ian Beadham, Monika Gurbisz, Mukund D. Ghavre, Saibh Morrissey
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Patent number: 8124781Abstract: The present invention relates to a process of providing the 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in substantially free form (Compound 1).Type: GrantFiled: December 4, 2008Date of Patent: February 28, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventor: David Siesel
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Publication number: 20120022251Abstract: The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.Type: ApplicationFiled: March 26, 2010Publication date: January 26, 2012Inventors: Yukihito Sumino, Kazuya Okamoto, Moriyasu Masui, Toshiyuki Akiyama
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Publication number: 20120022255Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: March 23, 2010Publication date: January 26, 2012Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
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Publication number: 20120010248Abstract: The present invention provides compounds that function as modulators of mitochondrial aldehyde dehydrogenase-2 (ALDH2) activity; and pharmaceutical compositions comprising the compounds. The present invention provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition. The present invention further provides assays for identifying agonists of ALDH2.Type: ApplicationFiled: August 22, 2011Publication date: January 12, 2012Inventors: Daria Mochly-Rosen, Che-Hong Chen, Xiaohu Ouyang
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Publication number: 20120004244Abstract: There is provided compounds of formula I, wherein E1, E2a, E2b, E2c, E4, D1, D2, D3, L1, Y1, L2 and Y2 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.Type: ApplicationFiled: March 12, 2010Publication date: January 5, 2012Applicant: BIOLIPOX ABInventors: Peter Nilsson, Benjamin Pelcman, Martins Katkevics
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Publication number: 20110275650Abstract: This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties.Type: ApplicationFiled: November 10, 2009Publication date: November 10, 2011Applicant: THE SCRIPPS RESEARCH INSTITUTEInventors: Benjamin F. Cravatt, Jonathan Z. Long, Weiwei Li, Daniel K. Nomura