Plural Ring Oxygens In The Additional Hetero Ring Patents (Class 546/283.7)
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Publication number: 20110263612Abstract: 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 12, 2011Publication date: October 27, 2011Applicant: CalciMedica, Inc.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20110263654Abstract: 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: April 7, 2011Publication date: October 27, 2011Applicant: Vertex Phamaceuticals IncorporatedInventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
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Publication number: 20110263564Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: October 29, 2009Publication date: October 27, 2011Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Radha Narayan, Jeremy S. Disch, Robert B. Perni, Chi B. Vu
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Publication number: 20110224260Abstract: The present invention provides a catechol-based derivative and a pharmaceutical acceptable salt therefrom and a solvate therefrom. A pharmaceutical composition for preventing or treating diabetes and ischemia, comprising a catechol-based derivative of formula (I) and at least one selected from the group consisting of a pharmaceutical excipient, a diluent and a carrier.Type: ApplicationFiled: May 24, 2011Publication date: September 15, 2011Applicant: NATIONAL TAIWAN UNIVERSITYInventors: Yueh-Hsiung Kuo, Ming-Jai Su
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Patent number: 8008302Abstract: 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: July 25, 2005Date of Patent: August 30, 2011Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Publication number: 20110201610Abstract: 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: August 18, 2011Inventors: Solomon Ungashe, John Jessen Wright, Andrew Pennell
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Publication number: 20110178120Abstract: The present invention relates to pyridoxine (vitamin B6) derived compounds of formula (I), pharmaceutically acceptable salts, or solvates thereof, wherein R1, R2, R4, A, L B1 and B2 are as defined in the specification, and pharmaceutical compositions comprising the compounds. Compounds of formula (I) inhibit Human Immunodeficiency Virus (HIV)-integrase enzyme and are useful for preventing and treating HIV infection and AIDS.Type: ApplicationFiled: June 4, 2009Publication date: July 21, 2011Applicant: AMBRILIA BIOPHARMA, INC.Inventors: Brent Stranix, Francis Beaulieu, Jean-Emmanuel Bouchard, Guy Milot, Wang Zhigang, Réjean Ruel
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Publication number: 20110145970Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.Type: ApplicationFiled: August 26, 2009Publication date: June 23, 2011Applicant: BASF SEInventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
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Publication number: 20110112140Abstract: The present invention relates to a novel compound having plasminogen activator inhibitor-1 (PAI-1) inhibitory activity, and a PAI-1 inhibitor comprising the compound as an active ingredient. The present invention further relates to a pharmaceutical composition that has an inhibitory action on PAI-1 activity and is useful in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. The novel compound is represented by the following general formula. Each symbol is defined as those in the specification.Type: ApplicationFiled: March 31, 2009Publication date: May 12, 2011Applicant: RENASCIENCE CO., LTD.Inventors: Toshio Miyata, Nagahisa Yamaoka, Hidehiko Kodama, Kenji Murano
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Publication number: 20110071142Abstract: The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor. The present invention also relates to various compounds described herein (e.g.Type: ApplicationFiled: March 19, 2010Publication date: March 24, 2011Applicant: BETH ISRAEL DEACONESS MEDICAL CENTERInventors: Peter Oettgen, Alan C. Rigby, Towia Libermann
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Publication number: 20110059968Abstract: The present invention relates to novel carboxamide compounds of the formula I and their use for the manufacture of a medicament. The carboxamide compounds are prodrugs of inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.Type: ApplicationFiled: December 29, 2008Publication date: March 10, 2011Applicant: Abbott GmbH & Co. KGInventors: Wilfried Hornberger, Helmut Mack, Andreas Kling, Achim Moeller, Barbara Vogg, Jürgen Delzer, Gisela Backfisch, Armin Beyerbach
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Publication number: 20110009407Abstract: The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R1, R2, R3, R4, R5 and R6 are defined in the specification. The invention further provides pharmaceutical compositions including the compounds of the invention as well as methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various conditions and disorders, such as Crohn's disease and ulcerative colitis.Type: ApplicationFiled: April 27, 2010Publication date: January 13, 2011Inventors: Ying-Zi Xu, Shendong Yuan, David Wone, Andrei Konradi
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Publication number: 20110009426Abstract: The present invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists.Type: ApplicationFiled: August 6, 2010Publication date: January 13, 2011Applicant: SANOFI-AVENTISInventors: Jean-Michel Altenburger, Valérie Fossey, Daniel Galtier, Frédéric Petit
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Publication number: 20110009454Abstract: Disclosed is a composition for agricultural use, which is used for controlling or preventing plant diseases caused by plant pathogens. The composition for agricultural use contains a compound represented by formula (1), a salt thereof or a hydrate of the compound or the salt. (1) [In the formula, Z represents an oxygen atom, a sulfur atom or NRZ; and E represents a furyl group, a thienyl group, a pyrrolyl group, a tetrazolyl group, a thiazolyl group, a pyrazolyl group, a phenyl group or the like.Type: ApplicationFiled: February 27, 2009Publication date: January 13, 2011Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yuichi Matsuzaki, Takashi Komori, Tohru Inoue
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Patent number: 7855219Abstract: This invention relates to compounds of formula (I) in which the variable groups are as defined in the text and claims. A pharmaceutical composition and methods of using these materials in treatment of various conditions are also disclosed and claimed.Type: GrantFiled: February 20, 2002Date of Patent: December 21, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Ulrich Rosentreter, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes-Peter Stasch
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Publication number: 20100311582Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6, independently of each other, are for example, selected from the group consisting of H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C3-C8-cycloalkyl, R7C(?O), and a ring system; provided that at least one of R1 and R6 is a —C2-C6-alkenylthio-C1-C6-alkyl, —C1-C6-alkoxy-C(?O)NRx-C1-C6-alkyl, —partially or fully unsaturated ring system containing in at least one ring in the ring system at least one hetero atom selected from N, O and S, which ring system is bound (i.e. through the N bonded to R1 and R6 in formula I) either directly or via a a C1-C6-alkylene group to the remainder of the compound, —partially or fully unsaturated ring system containing a ring that is bound to the remainder of the compound (i.e.Type: ApplicationFiled: January 23, 2009Publication date: December 9, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Thomas Pitterna, Peter Renold, Ottmar Franz Hueter, Peter Maienfisch, Werner Zambach
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Publication number: 20100305097Abstract: Compounds of Formula (I) are effective in the treatment of a microbial infection.Type: ApplicationFiled: July 28, 2010Publication date: December 2, 2010Inventors: Namal Chithranga Warshakoon, Rodney Dean Bush
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Publication number: 20100292225Abstract: 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: May 14, 2010Publication date: November 18, 2010Inventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
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Publication number: 20100222337Abstract: Conventional fungicidal compositions have had practical problems such that either a preventive effect or a curative effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired. The present invention provides a fungicidal composition containing a carboxylic acid amide derivative of the formula (I) or a salt thereof, as an active ingredient: wherein A is phenyl which may be substituted, benzodioxolanyl which may be substituted, or benzodioxanyl which may be substituted; B is 2- or 3-pyridyl which may be substituted; each of R1 and R2 is alkyl, or R1 and R2 may together form a 3- to 6-membered saturated carbon ring, provided that when B is 3-pyridyl which may be substituted, A is phenyl substituted by at least two substituents.Type: ApplicationFiled: December 13, 2006Publication date: September 2, 2010Applicant: Ishihara Sangyo Kaisha, Ltd.Inventors: Yuji Nakamura, Shigeru Mitani, Shintaro Tsukuda
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Patent number: 7781591Abstract: The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.Type: GrantFiled: June 13, 2007Date of Patent: August 24, 2010Assignee: Wyeth LLCInventors: Derek Cecil Cole, Diane Harris Boschelli, Yanong Daniel Wang, Magda Asselin, Diane Marie Joseph-McCarthy, Amarnauth Shastrie Prashad, Allan Wissner, Russell Dushin, Biqi Wu, Lawrence Nathan Tumey, Chuan S. Niu, Joan Chen
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Patent number: 7772233Abstract: The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.Type: GrantFiled: April 18, 2007Date of Patent: August 10, 2010Assignee: Merck Serono, S.A.Inventors: Andreas Goutopoulos, Benny C. Askew, Jr., Nhut Kiet Diep, Srinivasa Karra, Matthias Schwarz, Henry Yu
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Publication number: 20100184977Abstract: Organozinc compounds of the type R1—Ar1—ZnY (1) can be reacted with different functionalized aryl halides R2—Ar2—X (2) in the presence of catalytic amounts of Ni or Fe in a polar solvent or solvent mixture to form polyfunctional biaryles of the type R1—Ar1—Ar2—R2 (3). Organozinc compounds of the type (1) can be represented by the transmetallation reaction of functionalized aryl magnesium halides or lithium aryl compounds with e.g. ZnBr2.Type: ApplicationFiled: September 12, 2006Publication date: July 22, 2010Inventors: Paul knochel, Andrei Gavriushin, Christiane Charlotte Kofink, Georg Manolikakes
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Publication number: 20100179141Abstract: Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR5. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.Type: ApplicationFiled: December 17, 2007Publication date: July 15, 2010Inventors: David B. Belanger, M. Arshad Siddiqui, Patrick J. Curran, Blake Hamann, Lianyun Zhao, Panduranga Adulla P. Reddy, Praveen K. Tadikonda, Gerald W. Shipps, JR., Umar Faruk Mansoor
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Publication number: 20100168180Abstract: 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-lType: ApplicationFiled: June 4, 2009Publication date: July 1, 2010Inventors: Gerard Andrew Potter, Philip Huxley
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Publication number: 20100168175Abstract: The present invention relates to processes for preparing certain 2-pyridones and 2-pyridinols, to novel compounds of these two types and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection, in the medicinal field and in the protection of materials.Type: ApplicationFiled: December 10, 2009Publication date: July 1, 2010Applicant: BAYER CROPSCIENCE AGInventors: Isabelle ADELT, Robert VELTEN, Welf Burkhard WIESE, Ulrike WACHENDORFF-NEUMANN, Karl-Heinz KUCK, Peter DAHMEN, Arnd VOERSTE, Ronald EBBERT, Franz von NUSSBAUM
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Publication number: 20100166839Abstract: Non-peptidic renin inhibitors nitroderivatives of general formula (I): A1-(Xa—ONO2)j ??(I) having wider pharmacological activity and enhanced tolerability. They can be employed for treating or preventing cardiovascular, renal and chronic liver diseases, inflammatory processes and metabolic syndrome.Type: ApplicationFiled: March 1, 2007Publication date: July 1, 2010Applicant: Nicox S.AInventors: Nicoletta Almirante, Stefano Biondi, Ennio Ongini
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Publication number: 20100168136Abstract: A compound having activity to inhibit production and/or secretion of ?-amyloid protein, and is useful for prevention and/or treatment of various diseases associated with abnormal production and/or secretion of ?-amyloid protein, the compound represented by the general formula (I): [wherein, R1 represents a C1-C6 alkyl group which may have 1 to 6 halogen atoms as substituent groups, a C2-C6 alkenyl group which may have 1 to 6 halogen atoms as substituent groups, or a C3-C7 cycloalkyl group which may have 1 to 6 halogen atoms as substituent groups; R2 represents a 6-membered nitrogen-containing monocyclic aromatic heterocyclic group having 1 to 3 substituent groups, or a 9- or 10-membered nitrogen-containing bicyclic heterocyclic group having 1 to 4 substituent groups; Z1, Z2 and Z3 each independently represent a hydrogen atom, a halogen atom or a cyano group; and n represents 0, 1 or 2], salts thereof, or solvates thereof.Type: ApplicationFiled: March 11, 2010Publication date: July 1, 2010Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Hitoshi Iimori, Hideki Kubota, Satoru Miyauchi, Kayoko Motoki
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Patent number: 7741345Abstract: The invention is related to compounds of Formula I: or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: GrantFiled: July 19, 2007Date of Patent: June 22, 2010Assignee: Gilead Sciences, Inc.Inventors: Carina E. Cannizzaro, James M. Chen, Manoj C. Desai, Michael L. Mitchell, Sundaramoorthi Swaminathan, Lianhong Xu
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Publication number: 20100105739Abstract: 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: ApplicationFiled: January 7, 2010Publication date: April 29, 2010Inventors: Sara S. Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D.J. Grootenhuis
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Publication number: 20100087490Abstract: The present invention relates to formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in Form I, pharmaceutical packs or kits thereof, and methods of treatment therewith.Type: ApplicationFiled: September 29, 2009Publication date: April 8, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Christopher Young
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Publication number: 20100075971Abstract: This invention relates to novel diaryl ureas, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.Type: ApplicationFiled: December 1, 2009Publication date: March 25, 2010Inventors: Jacques DUMAS, Wendy Lee, Yuanwei Chen, Lila Adnane, William J. Scott, Sharad Verma, Jianqing Chen, Zhi Chen, Lin Yi
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Patent number: 7678919Abstract: Taxan derivatives are produced efficiently and inexpensively, which are useful as oral-administrable antitumor compounds. A compound of formula (1) (wherein R1 is an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group; R2 is a hydroxyl group optionally having a protective group) is processed with an alkali metal permanganate to produce a compound of formula (2), which may be a starting material for oral-administrable antitumor compounds.Type: GrantFiled: September 25, 2008Date of Patent: March 16, 2010Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Akihiro Imura, Tatsuya Yamaguchi, Yoshihiro Takayanagi, Seishiro Uchida
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Publication number: 20100063100Abstract: 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: ApplicationFiled: September 3, 2009Publication date: March 11, 2010Inventors: CHE-HONG CHEN, Daria Mochly-Rosen, Wenjin Yang
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Publication number: 20100063045Abstract: Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represented by the formula (1) or a salt thereof.Type: ApplicationFiled: March 28, 2008Publication date: March 11, 2010Applicant: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyuki Mogi, Hasashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
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Patent number: 7671221Abstract: 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: GrantFiled: June 29, 2007Date of Patent: March 2, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D. J. Grootenhuis
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Patent number: 7659268Abstract: 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: GrantFiled: May 18, 2007Date of Patent: February 9, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Matthew Hamilton, Mark Miller, Peter D. J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Frederick van Goor
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Publication number: 20090264660Abstract: An alkyl aryl sulfide of Chemical Formula (III) is prepared by substituting an aryl halogen compound of Chemical Formula (I) with an alkyl lithium organometallic reagent. The sulfide is subsequently reacted with a compound of Chemical Formula (II). Alternatively an aryl halogen compound of Chemical Formula (I) is reacted with Grignard reagent to protect the hydrogen-donating substituent, and then reacted with an alkyl lithium organometallic reagent, and subsequently with sulfur and a compound of Chemical Formula (II). An alkyl aryl sulfide of Chemical Formula (III) is prepared via a one-step reaction without separation or purification of an intermediate compound from various aryl halogen compounds.Type: ApplicationFiled: October 21, 2005Publication date: October 22, 2009Inventors: Heonjoong Kang, Jungyeob Ham, Jaeyoung Ko
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Publication number: 20090253684Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, COPD.Type: ApplicationFiled: December 2, 2008Publication date: October 8, 2009Inventors: Romyr Dominique, Robert Alan Goodnow, JR., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
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Publication number: 20090246137Abstract: 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: March 25, 2009Publication date: October 1, 2009Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
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Publication number: 20090196912Abstract: Described are pyridinylamines and pharmaceutically acceptable salts thereof, the use of these pyridinylamines for the prophylaxis and/or treatment of various diseases such as infectious diseases, including opportunistic infections, prion diseases immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as pharmaceutical compositions containing at least one pyridinylamine and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the pyridinylamines are disclosed.Type: ApplicationFiled: August 1, 2005Publication date: August 6, 2009Applicant: GPC Botech AGInventors: Jan Elke Eickhoff, Doris Hafenbradl, Wilfried Schwab, Matthew Cotton, Bert Matthias Kiebl, Birgit Zech, Stefan Muller, John Harris, Vladimir Savic, Jackie MacRitchie
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Publication number: 20090186868Abstract: A compound represented by the general formula (1) [X1 and X2 represent hydrogen atom, a halogen atom, hydroxyl group and the like, R1 represents a phenyl group, R2 represents an alkyl group, an alkenyl group, or an alkoxy group, R3 represents hydrogen atom, a halogen atom, hydroxyl group, or an alkoxy group, R4 represents hydrogen atom, or an alkyl group, Z1 and Z2 represent hydrogen atom, a halogen atom, hydroxyl group and the like, Z3 represents cyano group, an alkyl group, an alkenyl group and the like, Z4 represents an alkyl group, an alkenyl group, an alkynyl group and the like, and represents a single bond or a double bond], which shows high antitumor effect against cancer cells including drug resistant cells.Type: ApplicationFiled: October 24, 2006Publication date: July 23, 2009Applicant: Daiichi Sankyo Company LimitedInventors: Kouichi Uoto, Yasuyuki Takeda, Atsunobu Sakamoto, Yoshihiro Takayanagi
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Publication number: 20090176989Abstract: 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: December 4, 2008Publication date: July 9, 2009Inventor: David Siesel
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Patent number: 7557129Abstract: This invention relates to novel diaryl ureas, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.Type: GrantFiled: February 27, 2004Date of Patent: July 7, 2009Assignee: Bayer Healthcare LLCInventors: William J. Scott, Jacques Dumas, Stephen Boyer, Wendy Lee, Yuanwei Chen, Barton Phillips, Sharad Verma, Jianqing Chen, Zhi Chen, Jianmei Fan, Brian Raudenbush, Aniko Redman, Lin Yi, Qingming Zhu, Lila Adnane
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Publication number: 20090170905Abstract: 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: December 4, 2008Publication date: July 2, 2009Inventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
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Publication number: 20090093462Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds (I) 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: October 19, 2005Publication date: April 9, 2009Inventors: Ulricn Abel, Holger Deppe, Achim Feurer, Ulrich Gradler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
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Publication number: 20090030209Abstract: Taxan derivatives are produced efficiently and inexpensively, which are useful as oral-administrable antitumor compounds. A compound of formula (1) (wherein R1 is an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group; R2 is a hydroxyl group optionally having a protective group) is processed with an alkali metal permanganate to produce a compound of formula (2), which may be a starting material for oral-administrable antitumor compounds.Type: ApplicationFiled: September 25, 2008Publication date: January 29, 2009Applicant: DAIICHI PHARMACEUTICAL CO., LTD.Inventors: Akihiro IMURA, Tatsuya YAMAGUCHI, Yoshihiro TAKAYANAGI, Seishiro UCHIDA
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Publication number: 20090018157Abstract: Compounds of Formula (I) wherein: R1—X— is selected from: methyl, methoxymethyl and Formula (X); R2 is selected from hydrogen, methyl, chloro and fluoro; n is 1 or 2; or a salt, pro-drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.Type: ApplicationFiled: November 25, 2004Publication date: January 15, 2009Inventors: Craig Johnstone, Darren McKerrecher, Kurt Gordon Pike
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Publication number: 20080306062Abstract: 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: ApplicationFiled: May 5, 2008Publication date: December 11, 2008Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
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Publication number: 20080300243Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: February 24, 2006Publication date: December 4, 2008Inventors: Michael G. Kelly, John Kincaid, Matthew Duncton, Kiran Sahasrabudhe, Satyanarayana Janagani, Ravindra B. Upasani, Guoxian Wu, YunFeng Fang, Zhi-Liang Wei, Carl Kaub, Jianhua He
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Patent number: 7410980Abstract: A crystal of (1S,2S,3R,4S,5R,8R,9S,10R,13S)-4-acetoxy-2-benzoyloxy-9,10-[(1S)-2-(dimethylamino)ethylidenedioxy]-5,20-epoxy-1-hydroxytax-11-en-13-yl (2R,3S)-3-(tert-butoxycarbonylamino)-3-(3-fluoro-2-pyridyl)-2-hydroxypropionate, which has characteristic peaks at diffraction angles (2?) of 6.2°, 10.3°, 10.7°, 11.4°, and 12.0° in a powder X-ray diffraction pattern, and a method for preparing the aforementioned crystal, which comprises the step of performing crystallization by using an organic solvent selected from the group consisting of a ketone type solvent, a nitrile type solvent, and a mixture thereof, or a mixture of said organic solvent and water.Type: GrantFiled: November 29, 2002Date of Patent: August 12, 2008Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Seishiro Uchida, Yoshihiro Takayanagi, Makoto Ono