Crystalline freebase forms of a biphenyl compound
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Publication Number
US-11858898-B2
Publication Date
2024-01-02
Expiration Date
Abstract
The invention provides two crystalline freebase forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester. The invention also provides pharmaceutical compositions comprising the crystalline freebase or prepared using the crystalline freebases; processes and intermediates for preparing the crystalline freebases; and methods of using the crystalline freebases to treat a pulmonary disorder.
Core Innovation
The invention discloses anhydrous crystalline freebase Forms III and IV of the specified biphenyl ester. The forms are distinguished by powder X-ray diffraction patterns and thermal behavior, and the claims cover both treatment using a composition containing the crystalline freebase and the crystalline forms themselves. The partial content describes inhaled pharmaceutical compositions as intended for pulmonary-disorder treatment.
The background section is not included in the partial content, so the problem being solved is not explicitly described. The provided summary states that the crystalline forms are non-deliquescent and have acceptable hygroscopicity. It also describes isotonic nebulizer solutions and micronized dry-powder products, without providing further background on the need those forms or products address.
Claims Coverage
The partial content identifies three inventive features across three independent claims, comprising one method claim and two crystalline form claims.
Treatment of chronic obstructive pulmonary disease using the crystalline freebase
A method for treating chronic obstructive pulmonary disease in a human patient by administering a pharmaceutical composition comprising a pharmaceutically acceptable carrier and the specified crystalline freebase, characterized by a powder X-ray diffraction pattern.
Crystalline form characterized by powder X-ray diffraction
A crystalline form of the specified biphenyl ester characterized by a powder X-ray diffraction pattern comprising diffraction peaks.
Crystalline form characterized by differential scanning calorimetry
A crystalline form of the specified biphenyl ester characterized by a differential scanning calorimetry thermograph showing an onset of endothermic heat flow.
The claims cover treatment of chronic obstructive pulmonary disease using the specified crystalline freebase and two crystalline-form characterizations based on powder X-ray diffraction or differential scanning calorimetry.
Stated Advantages
The crystalline forms are described as non-deliquescent and having acceptable hygroscopicity.
Documented Applications
Inhaled treatment of chronic obstructive pulmonary disease in a human patient is covered by the claims; the partial content also identifies asthma as an intended pulmonary-disorder application.
The partial content describes inhaled pharmaceutical compositions in nebulizer-solution and micronized dry-powder forms.
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