US 6,982,334 B2
Crystalline form of (3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperindine-3-carboxylic acid
Jacques Bourget, Vitry sur Seine (France); Marc Antoine Perrin, Jouy en Josas (France); Serge Mignani, Chatenay Malabry (France); Bernd Janocha, Wiesbaden (Germany); Michel Cheve, Soisy sur Seine (France); Carole Neves, Paris (France); Pascal Billot, Montreuil (France); Michel Tabart, La Novrille (France); and Sylvaine Lafont, Trevoux (France)
Assigned to Aventis Pharma S.A., Antony (France)
Filed on Dec. 18, 2003, as Appl. No. 10/739,700.
Claims priority of provisional application 60/480412, filed on Jun. 20, 2003.
Claims priority of application No. 02 16415 (FR), filed on Dec. 20, 2002.
Prior Publication US 2004/0147751 A1, Jul. 29, 2004
Int. Cl. C07D 409/14 (2006.01); C07D 215/20 (2006.01); A61K 31/4709 (2006.01); A61P 31/04 (2006.01)
U.S. Cl. 546—174 4 Claims
 
1. A crystalline form A of (3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperidine-3-carboxylic acid having a powder X-ray diffraction pattern
   
          Lattice 2+74
        Multiplicity spacing +37 mean +80 Cu K+60 +38
  h k l factor J (+521 ) 1.54184 +521
   
 
  1 0 0 2 14.4954 6.0971
  0 0 1 2 10.9797 8.0523
  +31 1 0 1 2 10.0030 8.8400
  1 0 1 2 7.8775 11.2320
  2 0 0 2 7.2477 12.2116
  +31 2 0 1 2 6.8662 12.8930
  1 1 0 4 6.7356 13.1440
  0 1 1 4 6.2527 14.1640
  +31 1 1 1 4 6.0549 14.6294
  +31 1 0 2 2 5.6060 15.8078
  0 0 2 2 5.4898 16.1447
  1 1 1 4 5.4720 16.1977
  2 0 1 2 5.4674 16.2112
  2 1 0 4 5.2472 16.8964
  +31 2 1 1 4 5.0969 17.3987
  +31 2 0 2 2 5.0015 17.7331
  +31 3 0 1 2 4.8826 18.1687
  3 0 0 2 4.8318 18.3612
  1 0 2 2 4.7641 18.6246
  +31 1 1 2 4 4.5129 19.6713
  0 1 2 4 4.4516 19.9449
  2 1 1 4 4.4396 19.9992
  +31 2 1 2 4 4.1791 21.2601
  +31 3 0 2 2 4.1648 21.3338
  +31 3 1 1 4 4.1089 21.6273
  3 1 0 4 4.0786 21.7904
  3 0 1 2 4.0720 21.8259
  1 1 2 4 4.0376 22.0144
  2 0 2 2 3.9388 22.5737
   
at 295 K expressed in terms of h, k, l, multiplicity factor J, lattice spacing in Å and 2θ.