Plural Ring Oxygens In The Additional Hetero Ring Patents (Class 546/283.7)
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Patent number: 10512636Abstract: This disclosure relates to methods of treating or preventing cystic fibrosis transmembrane conductance regulator (CFTR) mediated diseases such as cystic fibrosis, chronic obstructive pulmonary disease, chronic pancreatitis, chronic bronchitis, asthma, mucus formation, comprising administering an effective amount of a 3-(phenyl)-N-(4-phenoxybenzyl)-1,2,4-oxa-diazole-5-carboxamide compound, salt, or derivative thereof to a subject in need thereof. In certain embodiments, the 2-amino-N-benzylidene-acetohydrazide compound is 3-(3,5-dibromo-4-hydroxyphenyl)-N-(4-phenoxybenzyl)-1,2,4-oxadiazole-5-carboxamide.Type: GrantFiled: May 27, 2016Date of Patent: December 24, 2019Assignees: Emory University, Children's Healthcare of Atlanta, Inc.Inventors: Nael McCarty, Guiying Cui
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Patent number: 10017500Abstract: The present invention provides a compound having a particular chemical structure or a pharmacologically acceptable salt thereof which has an excellent inhibitory effect on EZH1 and/or EZH2 activity. The present invention provides a compound having a 1,3-benzodioxole structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, or a pharmaceutical composition comprising the compound (wherein R1, R2, R3, R4, R5, R6, and V in the formula (I) are each as defined in the present specification).Type: GrantFiled: March 16, 2015Date of Patent: July 10, 2018Assignee: DAIICHI SANKYO COMPANY, LIMITEDInventors: Osamu Kanno, Jun Watanabe, Takao Horiuchi, Akira Nakao, Keisuke Suzuki, Tomonori Yamasaki, Nobuaki Adachi, Daisuke Honma, Yoshito Hamada
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Patent number: 9771361Abstract: Polymorphic forms of Compound (1) or a pharmaceutically acceptable salt thereof, wherein Compound (1) is represented by the following structural formula: are Form A of HCl salt of Compound (1).½H2O, Form F of HCl salt of Compound (1).3H2O, Form D of HCl salt of Compound (1), Form A of Compound (1), and Form A of tosylate salt of Compound (1). Such polymorphic forms are employed for treating influenza, inhibiting the replication of influenza viruses, or reducing the amount of influenza viruses in a biological sample or in a subject.Type: GrantFiled: May 10, 2016Date of Patent: September 26, 2017Assignee: Vertex Pharmaceuticals IncorporatedInventors: Kwame W. Nti-Addae, Michael Waldo, Simon Adam O'Neil, John Gregg Van Alsten, Dainius Macikenas, Praveen Mudunuri, Yi Shi, Mark Willem Ledeboer, Valdas Jurkauskas, Ales Medek, Steven Jones, Randal Byrn, Mohammed Asmal, Sarah Marie Robertson, Wanjung Tsai
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Patent number: 9434717Abstract: 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: August 31, 2015Date of Patent: September 6, 2016Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
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Publication number: 20150133301Abstract: 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: April 29, 2014Publication date: May 14, 2015Applicant: DOW AGROSCIENCES LLCInventors: 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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Patent number: 9012652Abstract: 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: July 16, 2014Date of Patent: April 21, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventor: David Andrew Siesel
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Patent number: 8993600Abstract: 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 5, 2008Date of Patent: March 31, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D. J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
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Publication number: 20150080578Abstract: 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: July 8, 2014Publication date: March 19, 2015Inventors: John K. Thottathil, Raymond P. Warrell
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Publication number: 20150080351Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: November 24, 2014Publication date: March 19, 2015Inventors: Solomon Ungashe, John J. Wright, Andrew Pennell, Zheng Wei
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Patent number: 8980629Abstract: 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: GrantFiled: August 23, 2013Date of Patent: March 17, 2015Assignee: CalciMedica, Inc.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20150065500Abstract: 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: September 11, 2014Publication date: March 5, 2015Applicant: 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: 20150065497Abstract: 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: August 5, 2014Publication date: March 5, 2015Inventors: Sara S. Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D.J. Grootenhuis
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Patent number: 8969574Abstract: 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 10, 2014Date of Patent: March 3, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
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Patent number: 8962529Abstract: 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: GrantFiled: October 21, 2011Date of Patent: February 24, 2015Assignee: Bayer Cropscience AGInventors: Harmut Ahrens, Marco Brünjes, Hansjörg Dietrich, Elmar Gatzweiler, Isolde Häuser-Hahn, Stefan Lehr, Dirk Schmutzler
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Publication number: 20150031876Abstract: 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: September 5, 2014Publication date: January 29, 2015Applicant: Shionogi & Co., Ltd.Inventors: Yukihito Sumino, Kazuya Okamoto, Moriyasu Masui, Toshiyuki Akiyama
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Publication number: 20140371230Abstract: 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 25, 2014Publication date: December 18, 2014Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
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Publication number: 20140371070Abstract: The present invention relates to novel non-steroidal brassinosteroid mimetic derivatives of formula (I), to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.Type: ApplicationFiled: December 13, 2012Publication date: December 18, 2014Applicant: Syngenta Participations AGInventors: Pierre Joseph Marcel Jung, Joerg Leipner, Mathilde Denise Lachia, Alain De Mesmaeker
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Patent number: 8906942Abstract: 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: December 17, 2012Date of Patent: December 9, 2014Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Che-Hong Chen, Daria Mochly-Rosen, Wenjin Yang
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Patent number: 8901111Abstract: 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: GrantFiled: June 4, 2010Date of Patent: December 2, 2014Assignee: Janssen Pharmaceutica NVInventors: J. Guy Breitenbucher, Mark S. Tichenor, Jeffrey E. Merit, Natalie A. Hawryluk, Alison L. Chambers, John M. Keith
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Publication number: 20140350056Abstract: The disclosure relates to Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein Ar1, Ar2, L1, L2, X, R3, R22, and m are as defined herein, compositions comprising an effective amount of a Compound of Formula (I), and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a Compound of Formula (I).Type: ApplicationFiled: August 9, 2012Publication date: November 27, 2014Inventor: Jianming Yu
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Patent number: 8889875Abstract: 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: August 2, 2013Date of Patent: November 18, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
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Publication number: 20140336193Abstract: The present invention relates to compounds that exhibit vasodilatory and anti-inflammatory effects by inhibiting the activity of soluble epoxide hydrolase (sEH). The present invention is also directed to methods of identifying such compounds, and use of such compounds for the treatment of diseases related to dysfunction of vasodilation, inflammation, and/or endothelial cells. In particular non-limiting embodiments, components of the invention may be used to treat hypertension.Type: ApplicationFiled: July 23, 2014Publication date: November 13, 2014Inventors: Donald W. Landry, Shi-Xian Deng, Stevan Pecic, Kirsten Alison Rinderspacher
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Publication number: 20140330023Abstract: 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: July 16, 2014Publication date: November 6, 2014Inventor: David Andrew Siesel
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Publication number: 20140309237Abstract: 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 26, 2014Publication date: October 16, 2014Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
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Publication number: 20140303232Abstract: This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, L and X are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.Type: ApplicationFiled: March 7, 2014Publication date: October 9, 2014Applicant: NOVARTIS AGInventors: Jeremy Lee BARYZA, Rohan Eric John BECKWITH, Keith BOWMAN, Crystal BYERS, Tanzina FAZAL, Gabriel Grant GAMBER, Cameron Chuck-munn LEE, Ritesh Bhanudasji TICHKULE, Chandra VARGEESE, Shuangxi WANG, Laura Ellen West, Thomas ZABAWA, Junping ZHAO
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Publication number: 20140295045Abstract: 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, which compound or salt thereof provides umami flavour.Type: ApplicationFiled: June 17, 2014Publication date: October 2, 2014Inventors: Yili WANG, Andrew DANIHER, Adri DE KLERK, Cornelis WINKEL
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Publication number: 20140274701Abstract: Novel 4-amino-6-(heterocyclic)picolinic acids and their derivatives and 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their derivatives are useful to control undesirable vegetation.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: Dow AgroSciences LLCInventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Lindsey G. Fischer, Christian T. Lowe, Jeff Petkus, Joshua Roth, Norbert M. Satchivi, Paul R. Schmitzer, Thomas L. Siddall
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Patent number: 8835461Abstract: 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: GrantFiled: March 23, 2010Date of Patent: September 16, 2014Assignee: Shionogi & Co., Ltd.Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
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Publication number: 20140249186Abstract: 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: March 6, 2014Publication date: September 4, 2014Applicant: GFV, LLCInventors: JOHN K. THOTTATHIL, RAYMOND P. WARRELL
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Publication number: 20140243366Abstract: 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: May 1, 2014Publication date: August 28, 2014Applicant: CalciMedica, Inc.Inventors: Jeffrey P. WHITTEN, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20140243349Abstract: The present disclosure provides ?-diketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.Type: ApplicationFiled: February 21, 2014Publication date: August 28, 2014Inventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
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Patent number: 8816093Abstract: 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: June 10, 2013Date of Patent: August 26, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventor: David Andrew Siesel
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Publication number: 20140235637Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.Type: ApplicationFiled: April 28, 2014Publication date: August 21, 2014Applicant: InterMune, Inc.Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid D. Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
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Publication number: 20140221430Abstract: 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 10, 2014Publication date: August 7, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Ali KESHAVARZ-SHOKRI, Beili ZHANG, Mariusz KRAWIEC
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Publication number: 20140194433Abstract: 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: March 12, 2014Publication date: July 10, 2014Applicant: BASF SEInventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
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Patent number: 8742122Abstract: 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: July 12, 2013Date of Patent: June 3, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
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Publication number: 20140142134Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Psendomonas spp., Yersinia spp., en tero pathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.Type: ApplicationFiled: July 13, 2012Publication date: May 22, 2014Applicant: MICROBIOTIX, INC.Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams, Matthew Torhan
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Publication number: 20140135329Abstract: 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: June 20, 2013Publication date: May 15, 2014Inventors: Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
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Patent number: 8716338Abstract: 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: GrantFiled: September 29, 2009Date of Patent: May 6, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventor: Christopher Young
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Publication number: 20140080768Abstract: The invention generally relates to Pro-Drugs of dihydroorotate dehydrogenase (DHODH) inhibitors and methods of use thereof. In certain embodiments, the invention provides a DHODH inhibitor compound including a cleavable functional group that increases bioavailability as compared to a form of the DHODH inhibitor without the functional group, rendering the former more suitable for therapeutic use.Type: ApplicationFiled: September 19, 2012Publication date: March 20, 2014Inventors: Alan Palmer, Michael J. Hudson, Richard Todd, Patrick Camilleri
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Publication number: 20130345193Abstract: 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: August 23, 2013Publication date: December 26, 2013Applicant: CALCIMEDICA, INC.Inventors: Jeffrey P. WHITTEN, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20130345240Abstract: 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: August 16, 2013Publication date: December 26, 2013Applicant: CALCIMEDICA, INC.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20130317020Abstract: 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: August 2, 2013Publication date: November 28, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
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Patent number: 8592602Abstract: 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: January 17, 2012Date of Patent: November 26, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventor: David Siesel
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Publication number: 20130296379Abstract: 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: July 12, 2013Publication date: November 7, 2013Inventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
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Publication number: 20130274477Abstract: 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: June 10, 2013Publication date: October 17, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventor: David Andrew Siesel
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Publication number: 20130267516Abstract: Compounds of general formula I, (formula [I)], their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.Type: ApplicationFiled: November 21, 2011Publication date: October 10, 2013Applicant: LEO PHARMA A/SInventors: Kristoffer Månsson, Lars Kristian Albert Blæhr
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Publication number: 20130267492Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: March 28, 2013Publication date: October 10, 2013Applicant: ChemoCentryx, Inc.Inventors: Solomon Ungashe, John J. Wright, Andrew Pennell, Zheng Wei
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Patent number: 8552034Abstract: A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a binder, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering an oral pharmaceutical formulation of Compound 1 to the patient.Type: GrantFiled: April 7, 2011Date of Patent: October 8, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Marinus Jacobus Verwijs, Rossitza Gueorguieva Alargova, Ritu Rohit Kaushik, Irina Nikolaevna Kadiyala, Christopher Young
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Patent number: 8546403Abstract: 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: GrantFiled: April 12, 2011Date of Patent: October 1, 2013Assignee: Calcimedica, Inc.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey