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(12) United States Patent (10) Patent No.: US 9,139,517 B2 Raillard Et Al

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(12) United States Patent (10) Patent No.: US 9,139,517 B2 Raillard Et Al US009139517B2 (12) United States Patent (10) Patent No.: US 9,139,517 B2 Raillard et al. (45) Date of Patent: Sep. 22, 2015 (54) ANHYDROUSAND HEMIHYDRATE WO WO 2008/086492 A1 T 2008 CRYSTALLINE FORMS OF AN WO 2009,096.985 8, 2009 (R)-BACLOFEN PRODRUG, METHODS OF WO WO 2009,096.985 A1 8/2009 SYNTHESIS AND METHODS OF USE OTHER PUBLICATIONS (71) Applicant: XenoPort, Inc., Santa Clara, CA (US) Caira, “Crystalline Polymorphism of Organic Compounds.” Topics (72) Inventors: Stephen P. Raillard, Mountain View, in Current Chemistry, vol. 198, 1998, pp. 163-208. CA (US): Suresh K. Manthati, Lal et al., “Arbaclofen Placarbil, A Novel R-Baclofen Prodrug: Sunnyvale, CA (US); Sudhir Joshi, Visp Improved Absorption, Distribution, Metabolism, and Elimination (CH) Properties Compared with R-Baclofen.” The Journal of Pharmacol ogy and Experimental Therapeutics, The American Society for Phar (73) Assignee: XenoPort, Inc., Santa Clara, CA (US) macology and Experimental Therapeutics, vol. 330, No. 3, Sep. 1, (*) Notice: Subject to any disclaimer, the term of this 2009, pp. 911-921. patent is extended or adjusted under 35 Addolorato et al., “Baclofen efficacy in reducing alcohol craving and U.S.C. 154(b) by 0 days. intake: a preliminary double-blind randomized controlled study.” Alcohol & Alcoholism (2002)37(5):504-508. (21) Appl. No.: 14/076,406 Ahmadi-Abhari et al., “Baclofen versus clonidine in the treatment of (22) Filed: Nov. 11, 2013 opiates withdrawal, side-effects aspect: a double-blind randomized controlled trial.”J Clin Pharm Ther: (2001) 26:67-71. (65) Prior Publication Data Aley et al., “Vincristine hyperalgesia in the rat: a model of painful US 2014/OO665O1 A1 Mar. 6, 2014 vincristine neuropathy in humans.” Neurosci. (1996), 73(1): 259 265. Related U.S. Application Data Anghinah et al., “Effect of baclofen on pain in diabetic neuropathy.” Muscle & Nerve (1994) 17(8):958-9. (63) Continuation of application No. 13/572.367, filed on Argoff, “Pharmacologic management of chronic pain.” JAOA Supp. 3 Aug. 10, 2012, now Pat. No. 8,580,850. (2002), 102(9): S21-S26. (60) Provisional application No. 61/508,286, filed on Aug. ASSadi et al., “Baclofen for maintenance treatment of opioid depen 11, 2011. dence: a randomized double-blind placebo-controlled clinical trial.” BMC Psychiatry (2003), 3(16) (10 pages). (51) Int. C. Authier et al., “Assessment of allodynia and hyperalgesia after C07C 27L/22 (2006.01) cisplatin administration to rats.” Neurosci. Lett. (2000), 291: 73-76. U.S. C. Backonja et al., “Gabapentin dosing for neuropathic pain: evidence (52) from randomaized, placebo-controlled clinical trials.” Clin. Ther. CPC ........... C07C271/22 (2013.01); C07B 2.200/07 (2003), 25: 81-104. (2013.01); C07B 2.200/13 (2013.01) Balerio et al., “Baclofen analgesia: involvement of the GABAergic (58) Field of Classification Search system.” Pharm. Res. (2002) 46(3):281-286. USPC ............................................. 514/487; 560/30 Baron, “Mechanisms of disease: neuropathic pain—a clinical per See application file for complete search history. spective.” Nat. Clin. Pract. Neurol. (2006), 2(2): 95-106. Becker et al., “Intrathecal baclofen alleviates autonomic dysfunction (56) References Cited in severe brain injury.”J Clin. Neurosci. (2000) 7(4):316-319. Beggs et al., “Neuropathic pain: Symptoms, models and mecha U.S. PATENT DOCUMENTS nisms,” Drug Dev. Res. (2006), 67: 289-301. 4,126,684 A 11, 1978 Robson et al. Bennett et al., “A peripheral mononeuropathy in rat that produces 5,006,560 A 4, 1991 Kreutner et al. disorders of pain sensation like those seen in man.” Pain (1988), 33: 5,719, 185 A 2f1998 Bountra et al. 87-107. 6,117,908 A 9, 2000 Andrews et al. Blackshaw et al., “Inhibition of transient LES relaxations and reflux 7,109,239 B2 9/2006 Gallop et al. in ferrets by GABA receptor agonists.” Am. J. Physiol. (1999), 277: 7,227,028 B2 6/2007 Gallop et al. G867-G874. 2002/0151529 A1 10/2002 Cundy et al. 2003. O133951 A1 7/2003 Coe et al. (Continued) 2003/0171303 A1 9/2003 Gallop et al. 2003/0176398 A1 9/2003 Gallop et al. 2004.0006132 A1 1/2004 Gallop et al. Primary Examiner — San-Ming Hui 2004, OO1494.0 A1 1/2004 Raillard et al. Assistant Examiner — Kathrien Cruz 2004/O138305 A1 7/2004 Dooley et al. 2004/O180959 A1 9/2004 Dooley et al. (74) Attorney, Agent, or Firm — Polsinelli PC 2007/0O32500 A1 2/2007 Sun et al. 2007/0O82939 A1 4/2007 Lippa et al. (57) ABSTRACT Crystalline (3R)-4-(1S)-2-methyl-1-(2-methylpropanoy FOREIGN PATENT DOCUMENTS loxy)propoxycarbonylamino-3-(4-chlorophenyl)butanoic EP 1178O34 2, 2002 acid anhydrate and crystalline (3R)-4-(1S)-2-methyl-1-(2- WO 91.0874O 6, 1991 methylpropanoyloxy)propoxycarbonylamino-3-(4-chlo WO O1,08675 2, 2001 rophenyl)butanoic acid hemihydrate, pharmaceutical compo WO O1,26638 4/2001 WO O1,900.52 11, 2001 sitions comprising Such compounds, methods of making and WO 02/0964.04 12/2002 methods of using the same are disclosed. WO 2005/019 163 3, 2005 WO 2008/086492 T 2008 16 Claims, 4 Drawing Sheets US 9,139,517 B2 Page 2 (56) References Cited Flannery et al., “Baclofen for alcohol dependence: a preliminary open-label study.” Alcohol Clin. Exp. Res. (2004) 28(10): 1517-1523. OTHER PUBLICATIONS Fox et al., “Critical evaluation of the streptozotocin model of painful diabetic neuropathy in the rat.” Pain (1999), 81: 307-316. 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Heinzerling et al., “Randomized, placebo-controlled trial ofbaclofen Cousins et al., "GABA receptor agonists for the treatment of drug and gabapentin for the treatment of methamphetamine dependence.” addiction: a review of recent findings.” Drug and Alcohol Depend. Drug Alcohol Depend. (2006) 85:177-184. (2002) 65:209-220. Hering-Hanit et al., “Baclofen in cluster headache.” Headache Crofford et al., “Pregabalin for the treatment of fibromyalgia syn (2000) 40:48-51. drome.” Arth. Rheum. (2005), 52(4): 1264-1273. Hering-Hanit, “Baclofen for prevention of migraine.” Cephalalgia Dapas et al., “Baclofen for the treatment of acute low-back syn (1999) 19:589-591. drome—a double-blind comparison with placebo.” Spine (1985) Herman et al., “Intrathecal baclofen Suppresses central pain in 10(4):345-349.
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