US2015038744A1PendingUtilityA1

Crystalline Solid Rasagiline Base

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Assignee: FRENKEL ANTONPriority: Dec 14, 2006Filed: Aug 14, 2014Published: Feb 5, 2015
Est. expiryDec 14, 2026(~0.4 yrs left)· nominal 20-yr term from priority
C07C 209/82C07C 2602/08C07C 211/42C07B 2200/13A61P 25/16A61K 31/135A61K 9/70
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Claims

Abstract

The subject invention provides crystalline R(+)-N-propargyl-1-aminoindan, pharmaceutical compositions and methods of manufacture thereof.

Claims

exact text as granted — not AI-modified
1 - 18 . (canceled) 
     
     
         19 . A process for manufacturing a rasagiline salt comprising reacting crystalline R(+)-N-propargyl-1-aminoindan characterized by an X-ray powder diffraction pattern having peaks at 8.5, 12.6, 16.1 and 16.9 in degrees two theta ±0.2, with an acid, so as to form the rasagiline salt. 
     
     
         20 . The process of  claim 19 , wherein the crystalline R(+)-N-propargyl-1-aminoindan is further characterized by a melting point of 38-39° C. when determined in an open capillary or 41° C. when determined by differential scanning calorimetry. 
     
     
         21 . The process of  claim 19 , wherein the crystalline R(+)-N-propargyl-1-aminoindan is further characterized by an X-ray powder diffraction pattern having peaks at 20.3, 20.9, 25.4, 26.4 and 28.3 in degrees two theta ±0.2. 
     
     
         22 . A process for manufacturing a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a rasagiline salt which process comprises contacting crystalline R(+)-N-propargyl-1-aminoindan characterized by an X-ray powder diffraction pattern having peaks at 8.5, 12.6, 16.1 and 16.9 in degrees two theta ±0.2, with an acid, so as to form the pharmaceutical composition. 
     
     
         23 . The process of  claim 22 , wherein the crystalline R(+)-N-propargyl-1-aminoindan is further characterized by a melting point of 38-39° C. when determined in an open capillary or 41° C. when determined by differential scanning calorimetry. 
     
     
         24 . The process of  claim 22 , wherein the crystalline R(+)-N-propargyl-1-aminoindan is further characterized by an X-ray powder diffraction pattern having peaks at 20.3, 20.9, 25.4, 26.4 and 28.3 in degrees two theta ±0.2. 
     
     
         25 . The process of  claim 22 , wherein the pharmaceutical composition further comprises levodopa, L-carbidopa, beserazide, ladostigil, pentahydric alcohol, hexahydric alcohol, or riluzole.

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