Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid

a technology of cyclopropanecarboxamido and cyclopropanecarboxamido, which is applied in the field of solid state forms, can solve the problems of imbalance in ion and fluid transport, debilitating and fatal effects of cf, and individual with two copies of the cf associated gene suffer from the debilitating and fatal effects of cf, and achieve the effect of lessening the severity of cftr-mediated diseases

a technology of cyclopropanecarboxamido and cyclopropanecarboxamido, which is applied in the field of solid state forms, can solve the problems of imbalance in ion and fluid transport, debilitating and fatal effects of cf, and individual with two copies of the cf associated gene suffer from the debilitating and fatal effects of cf, and achieve the effect of lessening the severity of cftr-mediated diseases

US20130085158A1Inactive Publication Date: 2013-04-04VERTEX PHARMA INC
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  • Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
  • Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
  • Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid

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Methods & Materials

[0206]Differential Scanning Calorimetry (DSC)

[0207]The Differential scanning calorimetry (DSC) data for Compound 1, Solvate Form A were collected using a DSC Q100 V9.6 Build 290 (TA Instruments, New Castle, Del.). Temperature was calibrated with indium, and heat capacity was calibrated with sapphire. Samples of 3-6 mg were weighed into aluminum pans that were crimped using lids with 1 pin hole. The samples were scanned from 25° C. to 350° C. at a heating rate of 1.0° C. / min and with a nitrogen gas purge of 50 ml / min. Data were collected by Thermal Advantage Q Series™ version 2.2.0.248 software and analyzed by Universal Analysis software version 4.1D (TA Instruments, New Castle, Del.). The reported numbers represent single analyses.

[0208]Jet Milling Description

[0209]Unmicronized Compound 1, Solvate Form A or Compound 1, HCl Salt Form A is sieved to de-lump it prior to placing it into the jet mill hopper. All sieves are disposable and received a wipe prior to use. U...

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Abstract

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.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]The present application claims the benefit of priority under 35 U.S.C. §119 to U.S. Provisional Application Ser. No. 61 / 321,729, filed Apr. 7, 2010, and entitled “Solid Forms of 3-(6-(1-(2,2-Difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid,” the entire contents of which is incorporated herein by reference.TECHNICAL FIELD OF THE INVENTION[0002]The present invention relates to solid state forms, for example, crystalline forms, of the compound 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid, pharmaceutical compositions thereof, and methods therewith.BACKGROUND OF THE INVENTION[0003]CFTR is a cAMP / ATP-mediated anion channel that is expressed in a variety of cell types, including absorptive and secretory epithelia cells, where it regulates anion flux across the membrane, as well as the activity of other ion channels and proteins. In epithelia ce...

Claims

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Application Information

Patent Timeline
04 Apr 2013
Publication
US20130085158A1
IPC
C07D405/12; A61K31/47; A61K45/06; A61K31/443
CPC
C07D213/75; C07D405/12; C07D405/14; Y10T428/2982; A61K31/47; A61K45/06; C07D407/12; A61K31/443
Inventors
KESHAVARZ-SHOKRI, ALI; ZHANG, BEILI