Crystalline pharmaceutical and methods of preparation and...

Details Crystalline pharmaceutical and methods of preparation and... Crystalline pharmaceutical and methods of preparation and...

2009-04-15

2011-12-20

Henley, III, Raymond (Department: 1629)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C546S146000

Reexamination Certificate

active

08080562

ABSTRACT:
Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention.

REFERENCES:
patent: 3773919 (1973-11-01), Boswell et al.
patent: 4668506 (1987-05-01), Bawa
patent: 4713244 (1987-12-01), Bawa
patent: 4767628 (1988-08-01), Hutchinson
patent: 4908202 (1990-03-01), Schulz
patent: 4931279 (1990-06-01), Bawa et al.
patent: 4992445 (1991-02-01), Lawter et al.
patent: 5001139 (1991-03-01), Lawter et al.
patent: 5023252 (1991-06-01), Hseih
patent: 5134122 (1992-07-01), Orsolini
patent: 5149780 (1992-09-01), Plow et al.
patent: 5192741 (1993-03-01), Orsolini et al.
patent: 5236704 (1993-08-01), Fujioka et al.
patent: 5288854 (1994-02-01), Diamond et al.
patent: 5298492 (1994-03-01), Neustadt et al.
patent: 5340800 (1994-08-01), Liu et al.
patent: 5397791 (1995-03-01), Hartman et al.
patent: 5424289 (1995-06-01), Yang et al.
patent: 5424399 (1995-06-01), Arnaout
patent: 5445832 (1995-08-01), Orsolini et al.
patent: 5470953 (1995-11-01), Gallatin et al.
patent: 5585359 (1996-12-01), Breslin et al.
patent: 5597567 (1997-01-01), Whitcup et al.
patent: 5612052 (1997-03-01), Shalaby
patent: 5622700 (1997-04-01), Jardieu et al.
patent: 5672659 (1997-09-01), Shalaby et al.
patent: 5747035 (1998-05-01), Presta et al.
patent: 5840332 (1998-11-01), Lerner et al.
patent: 5849327 (1998-12-01), Berliner et al.
patent: 5877224 (1999-03-01), Brocchini et al.
patent: 5893985 (1999-04-01), Luo et al.
patent: 5922356 (1999-07-01), Koseki et al.
patent: 5968895 (1999-10-01), Gefter et al.
patent: 5973188 (1999-10-01), Alig et al.
patent: 5980945 (1999-11-01), Ruiz
patent: 6180608 (2001-01-01), Gefter et al.
patent: 6204280 (2001-03-01), Gante et al.
patent: 6294522 (2001-09-01), Zablocki et al.
patent: 6331640 (2001-12-01), Fotouhi et al.
patent: 6340679 (2002-01-01), Peyman et al.
patent: 6358976 (2002-03-01), Wityak et al.
patent: 6515124 (2003-02-01), Fotouhi et al.
patent: 6524581 (2003-02-01), Adamis
patent: 6605597 (2003-08-01), Zablocki et al.
patent: 6620422 (2003-09-01), Maquin et al.
patent: 6653478 (2003-11-01), Urbanski et al.
patent: 6667060 (2003-12-01), Vandecruys et al.
patent: 6667318 (2003-12-01), Burdick et al.
patent: 6670321 (2003-12-01), Adamis
patent: 6803384 (2004-10-01), Fotouhi et al.
patent: 6872382 (2005-03-01), Gamache et al.
patent: 6872735 (2005-03-01), Burdick et al.
patent: 7097851 (2006-08-01), Takada
patent: 7211586 (2007-05-01), Fenton et al.
patent: 7217728 (2007-05-01), Fotouhi et al.
patent: 7314938 (2008-01-01), Shen et al.
patent: 2001/0031260 (2001-10-01), Lee et al.
patent: 2002/0019446 (2002-02-01), Brocchini et al.
patent: 2002/0115692 (2002-08-01), Archibald et al.
patent: 2002/0119994 (2002-08-01), Burdick et al.
patent: 2002/0132807 (2002-09-01), Wang et al.
patent: 2002/0176841 (2002-11-01), Barker et al.
patent: 2002/0177591 (2002-11-01), O'Donnell et al.
patent: 2003/0044406 (2003-03-01), Dingivan
patent: 2003/0064105 (2003-04-01), Kim et al.
patent: 2003/0068320 (2003-04-01), Dingivan
patent: 2003/0068384 (2003-04-01), Brocchini et al.
patent: 2003/0138488 (2003-07-01), Kohn et al.
patent: 2003/0166630 (2003-09-01), Auvin et al.
patent: 2003/0171296 (2003-09-01), Gefter et al.
patent: 2003/0216307 (2003-11-01), Kohn et al.
patent: 2004/0006236 (2004-01-01), Fotouhi et al.
patent: 2004/0028648 (2004-02-01), Adamis
patent: 2004/0058968 (2004-03-01), Burdick et al.
patent: 2004/0120960 (2004-06-01), Jardieu et al.
patent: 2005/0080119 (2005-04-01), Fotouhi et al.
patent: 2005/0148588 (2005-07-01), Burdick et al.
patent: 2005/0267098 (2005-12-01), Shen et al.
patent: 2006/0281739 (2006-12-01), Gadek et al.
patent: 2007/0025990 (2007-02-01), Dingivan
patent: 2007/0155671 (2007-07-01), Fotouhi et al.
patent: 2008/0019977 (2008-01-01), Adamis
patent: 2008/0176896 (2008-07-01), Shen et al.
patent: 2008/0182839 (2008-07-01), Shen et al.
patent: 2009/0155176 (2009-06-01), Burnier et al.
patent: 2010/0092541 (2010-04-01), Burnier et al.
patent: 2010/0092542 (2010-04-01), Burnier et al.
patent: 2011/0165228 (2011-07-01), Burnier et al.
patent: 2011/0165229 (2011-07-01), Burnier et al.
patent: 0314863 (1989-05-01), None
patent: 0314863 (1990-04-01), None
patent: 0362526 (1990-04-01), None
patent: 0362531 (1990-04-01), None
patent: 0362526 (1990-07-01), None
patent: 0326151 (1993-06-01), None
patent: 0656789 (1997-12-01), None
patent: 0467389 (1999-10-01), None
patent: 1392306 (2008-01-01), None
patent: 4193895 (1992-07-01), None
patent: WO 90/03400 (1990-04-01), None
patent: WO 90/10652 (1990-09-01), None
patent: WO 90/13316 (1990-11-01), None
patent: WO 91/19511 (1991-12-01), None
patent: WO 92/03473 (1992-03-01), None
patent: WO 93/16702 (1993-09-01), None
patent: WO 93/24150 (1993-12-01), None
patent: WO 94/03481 (1994-02-01), None
patent: WO 94/11400 (1994-05-01), None
patent: WO 94/15587 (1994-07-01), None
patent: WO 94/15587 (1994-09-01), None
patent: WO 95/04531 (1995-02-01), None
patent: WO 95/28170 (1995-10-01), None
patent: WO 96/09836 (1996-04-01), None
patent: WO 97/04744 (1997-02-01), None
patent: WO 97/26015 (1997-07-01), None
patent: WO 97/40085 (1997-10-01), None
patent: WO 98/13029 (1998-04-01), None
patent: WO 98/25642 (1998-06-01), None
patent: WO 98/46599 (1998-10-01), None
patent: WO 99/49856 (1999-10-01), None
patent: WO 99/49856 (1999-11-01), None
patent: WO 00/21920 (2000-04-01), None
patent: WO 00/38714 (2000-07-01), None
patent: WO 00/44731 (2000-08-01), None
patent: WO 01/01964 (2001-01-01), None
patent: WO 01/12233 (2001-02-01), None
patent: WO 01/27102 (2001-04-01), None
patent: WO 01/01964 (2001-06-01), None
patent: WO 01/49249 (2001-07-01), None
patent: WO 01/49311 (2001-07-01), None
patent: WO 01/58853 (2001-08-01), None
patent: WO 01/12233 (2001-11-01), None
patent: WO 01/87840 (2001-11-01), None
patent: WO 01/49249 (2002-01-01), None
patent: WO 02/30398 (2002-04-01), None
patent: WO 02/38129 (2002-05-01), None
patent: WO 02/50080 (2002-06-01), None
patent: WO 02/058672 (2002-08-01), None
patent: WO 02/059114 (2002-08-01), None
patent: WO 02/074247 (2002-09-01), None
patent: WO 02/058672 (2002-12-01), None
patent: WO 02/074247 (2002-12-01), None
patent: WO 02/098426 (2002-12-01), None
patent: WO 02/38129 (2003-02-01), None
patent: WO 02/30398 (2003-03-01), None
patent: WO 03/053401 (2003-07-01), None
patent: WO 03/075887 (2003-09-01), None
patent: WO 2003/053401 (2004-01-01), None
patent: WO 2004/026406 (2004-04-01), None
patent: WO 2005/014532 (2005-02-01), None
patent: WO 2005/014533 (2005-02-01), None
patent: WO 2005/014533 (2005-04-01), None
patent: WO 2005/044817 (2005-05-01), None
patent: WO 2005/123706 (2005-12-01), None
patent: WO 2006/125119 (2006-11-01), None
patent: WO 2009/139817 (2009-11-01), None
patent: WO 2009/139817 (2010-01-01), None
U.S. Appl. No. 12/909,241, filed Oct. 21, 2010, Burnier et al.
Wermuch. The practice of medicinal chemistry-molecular variations based on isosteric replacements. Academic Press Limited. 1996; 226-228.
Park, et al. Effects of fluorine substitution on drug metabolism: pharmacological and toxicological implications. Drug Metab Rev. 1994;26(3):605-43.
Park, et al. Metabolism of fluorine-containing drugs. Annu Rev Pharmacol Toxicol. 2001;41:443-70.
Kunert, et al. Analysis of Topical Cyclosporine Treatment of Patients with Dry Eye Syndrome. Arch Ophthalmol, vol. 118, Nov. 2000, 1489-1496.
Fox. Systemic diseases associated with dry eye. Int Ophthalmol Clin, 1994 Winter, 34(1):71-87.
Stern, et al. Conjunctival T-cell subpopulations in Sjögren's and non-Sjögren's patients with dry eye. Invest Ophthalmol Vis Sci. Aug. 2002;43(8):2609-14.
Legarreta Eye Center, Dry Eye, Jan. 2002, printed from http://www.legarretaeyecenter.com/dry-eye.html with Google date entry, 3 pages.
The Eye Digest, Eye Exam for Dry Eyes, Mar. 2003, printed from http://www.agingeye.net/dryeyes/dryeeyeseyeexam.php and google date entry, 4 pages.
International search report dated Sep. 19, 2006 for PCT Appl

Affiliated with

Also associated with

Rating

Crystalline pharmaceutical and methods of preparation and... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Crystalline pharmaceutical and methods of preparation and..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Crystalline pharmaceutical and methods of preparation and... will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-4295913