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(12) United States Patent (10) Patent No.: US 8,080,562 B2

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(12) United States Patent (10) Patent No.: US 8,080,562 B2 US008080562B2 (12) UnitedO States Patent (10) Patent No.: US 8,080,562 B2 Burnier et al. (45) Date of Patent: Dec. 20, 2011 (54) CRYSTALLINE PHARMACEUTICAL AND 5,922,356 A 7/1999 Koseki et al. METHODS OF PREPARATION AND USE 5,968,895 A 10/1999 Gefter et al. 5,973, 188 A 10/1999 Alig et al. THEREOF 5,980,945. A 1 1/1999 Ruiz 6,180,608 B1 1/2001 Gefter et al. (75) Inventors: John Burnier, Pacifica, CA (US); 6,204.280 B1 3/2001 Gante et al. Thomas Gadek, Oakland, CA (US); 6,294.522 B1 9, 2001 Zablocki et al. car s s 6,331,640 B1 12/2001 Fotouhi et al. Frederic Naud, Binningen (CH) 6,340,679 B1 1/2002 Peyman et al. 6,358,976 B1 3/2002 Wityak et al. (73) Assignee: Sarcode Bioscience Inc., Brisbane, CA 6,515,124 B2 2/2003 Fotouhi et al. (US) 6,524,581 B1 2/2003 Adamis 6,605,597 B1 8, 2003 Zablocki et al. (*) Notice: Subject to any disclaimer, the term of this 32. R 3. MSE patent is extended or adjusted under 35 6,667,060w - - B1 12/2003 VandecruysaSK ea. et al. U.S.C. 154(b) by 449 days. 6,667,318 B2 12/2003 Burdick et al. 6,670,321 B1 12/2003 Adamis (21) Appl. No.: 12/386,361 6,803,384 B2 10/2004 Fotouhi et al. 6,872,382 B1 3/2005 Gamache et al. 22) Filed: Apr. 15, 2009 6,872,735 B2 3/2005 Burdick et al. (22) 1. pr. 15, 7,097,851 B1 8, 2006 Takada (65) Prior Publication Data (Continued) US 2009/O298869 A1 Dec. 3, 2009 FOREIGN PATENT DOCUMENTS Related U.S. Application Data EP 0314863 A2 5, 1989 (Continued) (60) Provisional application No. 61/045,142, filed on Apr. 15, 2008. OTHER PUBLICATIONS U.S. Appl. No. 12/909,241, filed Oct. 21, 2010, Burnier et al. (51) Int. Cl. Wermuch. The practice of medicinal chemistry-molecular variations A6K 3/47 (2006.01) based on isosteric replacements. Academic Press Limited. 1996; C07D 217/02 (2006.01) 226-228. (52) U.S. Cl. ........................................ 514/307: 546/146 Park, et al. Effects of fluorine substitution on drug metabolism: (58) Field of Classification Search .................. 514/307 pharmacological and toxicological implications. Drug Metab Rev. 546/146 1994:26(3):605-43. S lication file f let h hist Park, et al. Metabolism of fluorine-containing drugs. Annu Rev ee appl1cauon Ille Ior complete searcn n1Story. Pharmacol Toxicol. 2001:41:443-70. Kunert, et al. Analysis of Topical Cyclosporine Treatment of Patients (56) References Cited with Dry Eye Syndrome. Arch Ophthalmol, vol. 118, Nov. 2000, 1489-1496. U.S. PATENT DOCUMENTS 3,773.919 A 1 1/1973 Boswell et al. (Continued) is: A 38 Ey. Primary Examiner — Raymond Henley, III 4,767.62s A 8, 1988 Hutchinson (74) Attorney, Agent, or Firm — Wilson Sonsini Goodrich & 4,908,202 A 3, 1990 Schulz Rosati 4,931,279 A 6, 1990 Bawa et al. 4,992.445 A 2/1991 Lawter et al. (57) ABSTRACT 5,001,139 A 3/1991 Lawter et al. Novel crystalline polymorphic forms. Forms A, B, C, D, and 5,023,252 A 6, 1991 Hseih E of a compound of Formula I, which has been found to be a 5,149.7805,134,122 A 9,7, 1992 OrsoliniPOW et al. potent inhibitor- - - - - of LFA-1, are disclosed. Methods of prepa 5, 192,741 A 3, 1993 Orsolini et al. ration and uses thereof in the treatment of LFA-1 mediated 5,236,704 A 8/1993 Fujioka et al. diseases are also disclosed in this invention. 5,288,854 A 2f1994 Diamond et al. 5,298.492 A 3, 1994 Neustadt et al. 5,340,800 A 8, 1994 Liu et al. Formula I 5,397,791 A 3, 1995 Hartman et al. 5,424,289 A 6/1995 Yang et al. 5,424,399 A 6, 1995 Arnaout 5,445,832 A 8, 1995 Orsolini et al. 5,470,953 A 11/1995 Gallatin et al. C O SOMe 5,585,359 A 12/1996 Breslin et al. 5,597,567 A 1/1997 Whitcup et al. N OH 5,612,052 A 3/1997 Shalaby 7 H 5,622,700 A 4/1997 Jardieu et al. N O 5,672,659 A 9/1997 Shalaby et al. O C 5,747,035 A 5, 1998 Presta et al. 5,840,332 A 11/1998 Lerner et al. O 5,849,327 A 12/1998 Berliner et al. 5,877,224. A 3, 1999 Brocchini et al. 5,893,985 A 4/1999 Luo et al. 21 Claims, 48 Drawing Sheets US 8,080,562 B2 Page 2 U.S. PATENT DOCUMENTS WO WOO1? 49311 A1 T 2001 7,211,586 B2 5/2007 Fenton et al. W. W. S. A 398: 7,217,728 B2 5, 2007 Fotouhi et al. WO WOO1,8784.0 A1 11, 2001 7,314.938 B2 1/2008 Shen et al. WO WOO1/49249 A3 1, 2002 2001/0031260 A1 10, 2001 Lee et al. WO WOO2,30398 A2 4/2002 2002fOO19446 A1 2, 2002 Brocchini et al. WO WOO2,381.29 A2 5, 2002 2002fO115692 A1 8, 2002 Archibald et al. WO WOO2,5008O A1 6, 2002 2002/01 19994 A1 8, 2002 Burdick et al. WO WO O2/O58672 A2 8, 2002 2002/0132807 A1 9/2002 Wang et al. WO WO O2/O59114 A1 8, 2002 2002/0176841 A1 11/2002 Barker et al. WO WO O2/O74247 A2 9, 2002 2002/0177591 A1 11, 2002 O'Donnell et al. WO WO O2/O58672 A3 12/2002 2003/00444.06 A1 3/2003 Dingivan WO WO O2/O74247 A3 12/2002 2003/0064105 A1 4/2003 Kim et al. WO WO O2/O98426 A1 12/2002 2003.0068320 A1 4/2003 Dingivan WO WOO2,381.29 A3 2, 2003 2003.0068384 A1 4/2003 Brocchini et al. WO WOO2,30398 A3 3, 2003 2003. O138488 A1 7/2003 Kohnet al. WO WOO3,0534O1 A2 T 2003 2003. O166630 A1 9, 2003 Auvin et al. WO WOO3,O75887 A1 9, 2003 2003/0171296 A1 9, 2003 Gefter et al. WO WO 2003/0534O1 A3 1, 2004 2003/0216307 A1 11/2003 Kohn et al. WO WO 2004/0264.06 A1 4/2004 2004.0006236 A1 1/2004 Fotouhi et al. WO WO 2005/O14532 A1 2, 2005 2004/0028648 A1 2, 2004 Adamis WO WO 2005/014.533 A2 2, 2005 2004/0058968 A1 3, 2004 Burdick et al. WO WO 2005/014.533 A3 4/2005 2004/O120960 A1 6/2004 Jardieu et al. WO WO 2005/044817 A1 5, 2005 2005, 0080119 A1 4/2005 Fotouhi et al. WO WO 2005,123706 A1 12/2005 2005. O148588 A1 7/2005 Burdick et al. WO WO 2006/1251.19 A1 11, 2006 2006/0281739 A1 12/2006 Gadek et al. WO WO 2009/139817 A3 1, 2010 2007/0O25990 A1 2/2007 Dingivan 2007/O1556.71 A1 7/2007 Fotouhi et al. 2008, OO19977 A1 1/2008 Adams OTHER PUBLICATIONS 2008. O176896 A1 7/2008 Shen et al. Fox. Systemic diseases associated with dry eye. Int Ophthalmol Clin, 2008. O182839 A1 7/2008 Shen et al. 1994 Winter, 34(1):71-87. 2009. O1551.76 A1 6/2009 Burnier et al. Stern, et al. Conjunctival T-cell Subpopulations in Sjögren's and 2010/0092541 Al 4, 2010 Burnier et al. non-Sjögren's patients with dry eye. Invest OphthalmolVis Sci. Aug. 2010/0092542 A1 4/2010 Burnier et al. 2002:43(8):2609-14 2011/O165228 A1 7/2011 Burnier et al. s 2011/O165229 A1 7, 2011 Burnier et al. Legarreta Eye Center, Dry Eye, Jan. 2002, printed from http://www. legarretaeyecenter.com/dry-eye.html with Google date entry, 3 FOREIGN PATENT DOCUMENTS pageS. EP 0314863 A3 4f1990 The Eye Digest, Eye Exam for Dry Eyes, Mar. 2003, printed from EP O362526 A2 4f1990 http://www.agingeye.net/dryeyes/dryeeyeseyeexam.php and google EP O362531 A1 4f1990 date entry, 4 pages. EP O362526 A3 7, 1990 International search report dated Sep. 19, 2006 for PCT Application EP O326151 B1 6, 1993 EP O656789 B1 12/1997 No. PCT/US 2006, 19327. EP O467389 B1 10, 1999 European search report dated May 20, 2009 for Application No. EP 1392306 B1 1, 2008 O677O6O7.7. JP 4193895 7, 1992 International search report and written opinion dated Sep. 24, 2009 WO WO 90,03400 A1 4, 1990 for PCT Application No. US2009/02391. W W 2. A. 28 International search report and written opinion dated Dec. 22, 2010 WO WO91, 19511 A1 12, 1991 for PCT Application No. US 1053571. WO WO92fO3473 A1 3, 1992 Coleman, et al. Chemoselective Cleavage of Benzyl Ethers, Esters, WO WO93, 16702 A1 9, 1993 and Carbamates in the Presence of Other Easily Reducible Groups. WO WO 93.24150 A1 12, 1993 Synthesis. 1999; 1399-1400. WO WO 94,03481 A1 2, 1994 European Office Action dated Nov. 9, 2010 for Application No. WO WO94/11400 A1 5, 1994 677O6O7.7. W. W. 23, A. 3.E. Murphy, et al. The Pharmacologic Assessment of A Novel Lympho WO WO95/04531 A1 2, 1995 cyte Function-Associated Antigen-1 Antagonist (SAR 1118) for the WO WO95/2817O A1 10, 1995 Treatment of Keratoconjunctivitis Sicca in Dogs. Invest Ophthalmol WO WO96,09836 A1 4f1996 Vis Sci. May 16, 2011:52(6):3174-80.
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