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WO 2013/085849 A2 13 June 2013 (13.06.2013) P O P C T

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WO 2013/085849 A2 13 June 2013 (13.06.2013) P O P C T (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization I International Bureau (10) International Publication Number (43) International Publication Date WO 2013/085849 A2 13 June 2013 (13.06.2013) P O P C T (51) International Patent Classification: AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, C07D 487/22 (2006.01) BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (21) International Application Number: HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, PCT/US20 12/067627 KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, (22) International Filing Date: ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, 3 December 2012 (03.12.2012) NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, (25) Filing Language: English TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, (26) Publication Language: English ZM, ZW. (30) Priority Data: (84) Designated States (unless otherwise indicated, for every 61/569,144 9 December 201 1 (09. 12.201 1) US kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, (71) Applicant: DEMERX, INC. [US/US]; 4400 Biscayne UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, Boulevard, Suite 580, Miami, Florida 33 137 (US). TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, (72) Inventors; and MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, (71) Applicants : GLESS, Richard D. [US/US]; c/o Demerx, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, Inc., 4400 Biscayne Boulevard, Suite 580, Miami, Florida ML, MR, NE, SN, TD, TG). 33 137 (US). MORIARTY, Robert M. [US/US]; 3739 Michiana Drive, Michiana Shores, Indiana 46360-1 126 Declarations under Rule 4.17 : (US). — as to the applicant's entitlement to claim the priority of the (74) Agent: SWISS, Gerald F.; Foley & Lardner LLP, 3579 earlier application (Rule 4.1 7(in)) Valley Centre Drive, Suite 300, San Diego, California Published: 92130 (US). — without international search report and to be republished (81) Designated States (unless otherwise indicated, for every upon receipt of that report (Rule 48.2(g)) kind of national protection available): AE, AG, AL, AM, < 00 ©00 (54) Title: SULFATE ESTERS OF NORIBOGAINE (57) Abstract: Disclosed herein arc sulfate esters of nonbogaine or 9, 17 dihydronoribogaine, and pharmaceutically acceptable salts of each thereof, pharmaceutical compositions comprising such compounds, and methods of their use, including in treating addiction and/or pain. SULFATE ESTERS OF NORIBOGAINE FIELD OF THE INVENTION [0001] This invention is directed to sulfate esters of noribogaine. STATE OF THE ART [0002J Noribogaine is a metabolite of ibogaine and is sometimes referred to as 12- hydroxyibogaine. U.S. Patent No. 2,813,873 claims noribogaine albeit as "12-0- demethyli oga e" while providing an incorrect structural formula for ibogaine. Noribogaine can be depicted by the following formula: [0003] Noribogaine and its pharmaceutically acceptable salts have recently received significant attention as a non-addictive alkaloid useful in treating drug dependency (U.S. Patent No. 6,348,456) and as a potent analgesic (U.S. Patent No. 7,220,737). [0004] Noribogaine is typically administered orally or intravenously and becomes systemically available to the treated patient. SUMMARY OF THE INVENTION [0005] This invention is directed to sulfate esters of noribogaine and a vicinal dihydro derivative of noribogaine, and compositions comprising each of them. As used herein, the sulfate esters include pharmaceutically acceptable salts and esters (esterifying the OH group attached to the sulfur atom) thereof. [0006] n one aspect of this invention is provided a compound of formula I: I wherein: refers to a single or a double bond provided that when is a single bond. Formula I refers to the corresponding 9,17 dihydro compound; R is hydrogen or S0 2OR ; R 1 is hydrogen or S0 OR ; R2 is hydrogen or - C alkyl; provided that at least one of R and R1 is not hydrogen; or a salt thereof. 0007] As used herein, the 9,1 dihydro noribogaine sulfate ester derivatives include the 9a, β; 9a, 1 a ; 9β, 17a; and the 9β, 17β stereoisomers. [0008] In one of its composition aspects, this invention provides for a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I and at least a pharmaceutically acceptable excipient. [0009] In one of its method aspects, this invention is directed to a method for treating pain in a patient, which method comprises administering to said patient a therapeutically effective amount of a compound of Formula I above optionally in the presence of at least a pharmaceutically acceptable excipient. [0010] In another of its method aspects, this invention is directed to a method for treating addiction in a patient, which method comprises administering to said patient a therapeutically effective amount of a compound of Formula I above optionally in the presence of at least a pharmaceutically acceptable excipient. DETAILED DESCRIPTION OF THE INVENTION [001 ] It is to be understood that this invention is not limited to particular embodiments described, as such may, of course, vary. It is also to be understood that the terminology used herein is for the purpose of describing particular embodiments only, and is not intended to be limiting, since the scope of this invention will be limited only by the appended claims. [0012] It must be noted that as used herein and in the appended claims, the singular forms "a", "an", and "the" include plural referents unless the context clearly dictates otherwise. Thus, for example, reference to "a compound of Formula I" includes a plurality of compounds of Formula 1 such as a mixture of two or more of such compounds. Definitions [0013] Unless defined otherwise all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. As used herein, the following terms have the following meanings. [0014] As used herein, the term "comprising" or comprises" shall mean that the compositions and methods include the recited elements, but not excluding others. ' Consisting essentially of when used to define compositions and methods, shall mean excluding other elements of any essential significance to the combination for the stated purpose. Thus, a composition or method consisting essentially of the elements as defmed herein would not exclude other materials or steps that do not materially affect the basic and novel characteristic(s) of the claimed invention. ' Consisting of shall mean excluding more than trace elements of other ingredients and substantial method steps. Embodiments defmed by each of these transition terms are within the scope of this invention. [0015] The term "about" when used before a numerical designation, e.g., temperature, time, amount, and concentration, including range, indicates approximations which may vary by ( + ) or (- ) 10 %, 5 % or 1 %. [0016] As stated above, the invention is directed to the sulfate ester of noribogaine or a pharmaceutically acceptable salt thereof. [0017] As used herein, the ter "noribogaine" refers to the compound: as well as its pharmaceutically acceptable salts thereof. Conventionally, noribogaine is prepared by demethylation of naturally occurring ibogaine: which is isolated from Tabernanthe iboga, a shrub of West Africa. Demethylation may be accomplished by conventional techniques such as by reaction with boron tribromide/methylenc chloride at room temperature followed by conventional purification. (See, for example, Huffman, et al, J. Org. Chem. 50:1460 (1985)). This invention is not limited to any particular chemical form of noribogaine and the drug may be given to patients either as a free base or as a pharmaceutically acceptable addition salt. [0 18] As used herein, the term "alkyl" refers to a yl groups having from 1 to 1 carbon atoms, preferably 1 to 6 carbon atoms and more preferably 1 to 3 carbon atoms. The alkyl group may contain linear or branched carbon chains. This term is exemplified by groups such as methyl, ethyl, n-propyl, iso-propyl, n-butyl, t-butyl, n-pentyl and the like. The term C alkyl" refers to an alkyl group having x carbon atoms, wherein x is an integer for example, C3 refers to an alkyl group having 3 carbon atoms. [0019] As used herein, the term "cycloalkyl" refers to cyclic hydrocarbyl groups of from 3 to 10 carbon atoms having single or multiple cyclic rings including, by way of example, adamantyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclooctyl and the like [0020] As used herein, the term "aryl" refers to an aromatic carbocyclic group of from 6 to 4 carbon atoms having a single ring (e.g., phenyl) or multiple condensed rings (e.g., naphthyl or anthryl) which condensed rings may or may not be aromatic (e.g., 2- benzoxazolinone, 2H- 1,4-benzoxazin-3(4H)-one-7-yl, and the like) provided that the point of attachment is at an aromatic carbon atom. [0021] As used herein, the term "heteroaryl" refers to an aromatic group of from 1 to 10 carbon atoms and 1 to 4 heteroatoms selected from the group consisting of oxygen, nitrogen, sulfur within the ring, wherein the nitrogen and/or sulfur atom(s) of the heteroaryl are optionally oxidized (e.g., N-oxide, -S(O)- or -S(0)2-). Such heteroaryl groups can have a single ring (e.g., pyridyl or furyl) or multiple condensed rings (e.g., indolizinyl or benzothienyl) wherein the condensed rings may or may not be aromatic and/or contain a heteroatom provided that the point of attachment is through an atom of the aromatic heteroaryl group.
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