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WO 2014/170793 Al 23 October 2014 (23.10.2014) P O P C T

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WO 2014/170793 Al 23 October 2014 (23.10.2014) P O P C T (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2014/170793 Al 23 October 2014 (23.10.2014) P O P C T (51) International Patent Classification: DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, C07D 231/42 (2006.01) C07D 285/08 (2006.01) HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, C07D 417/12 (2006.01) C07D 285/135 (2006.01) KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, C07D 261/14 (2006.01) A61K 31/433 (2006.01) MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, C07D 277/52 (2006.01) A61P 19/06 (2006.01) OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, (21) International Application Number: TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, PCT/IB20 14/060503 ZW. (22) International Filing Date: (84) Designated States (unless otherwise indicated, for every 7 April 2014 (07.04.2014) kind of regional protection available): ARIPO (BW, GH, (25) Filing Language: English GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, (26) Publication Language: English TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, (30) Priority Data: EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, 61/813,796 19 April 2013 (19.04.2013) MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, 61/930,025 22 January 2014 (22.01.2014) TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). (71) Applicant: PFIZER LIMITED [GB/GB]; Ramsgate Road, Sandwich Kent, England CT13 9NJ (GB). Declarations under Rule 4.17 : — as to the identity of the inventor (Rule 4.1 7(Ϊ)) (72) Inventors: OWEN, Robert, McKenzie; c/o Neusentis, Portway Building, Granta Park, Great Abington Cam — as to applicant's entitlement to apply for and be granted a bridge, England CB21 6GS (GB). STORER, Robert, Ian; patent (Rule 4.1 7(H)) c/o Neusentis, Portway Building, Granta Park, Great — as to the applicant's entitlement to claim the priority of the Abington Cambridge, England CB21 6GS (GB). earlier application (Rule 4.1 7(in)) (74) Agents: LANE, Graham M. et al; Pfizer Limited, Ram s Published: gate Road, Sandwich Kent, England CT13 9NJ (GB). — with international search report (Art. 21(3)) (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, — with sequence listing part of description (Rule 5.2(a)) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, (54) Title: SULFONAMIDES FOR THE TREATMENT OF GOUT o (I) (57) Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to pro - o cesses for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide URAT-1 inhibitors of formula (I): (I) or pharmaceutically acceptable salts thereof, wherein R 1, R2, R3, R4, R5 and R6 are as defined in the description. URAT-1 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly gout. Chemical Compounds The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. Uric acid is the final product of purine metabolism in humans. In humans, unlike many other animals, uric acid is not further broken down, but is predominantly (70%) excreted into the urine with the remaining 30% excreted in faeces. Hyperuricemia is defined as an excessive production or decreased excretion of uric acid and can occur as an overproduction or under excretion of serum uric acid (sUA), or a combination of the both. Renal under excretion of uric acid is the primary cause of hyperuricemia in about 90% of cases, while overproduction is the cause in less than 10%. Increased sUA concentration above 6.8mg/dl_ results in crystallisation of uric acid in the form of salts, such as monosodium urate, and to precipitation of these crystals in joints, on tendons and in the surrounding tissues. These crystals (known as tophi) trigger a local immune- mediated inflammatory reaction, leading to gout. The risk of gout increases with increased sUA levels. Gout is a painful condition that can present in a number of ways, although the most usual is a recurrent attack of acute inflammatory arthritis (a red, tender, hot, swollen joint) often occurring in big toes, heels, knees, wrists and fingers. Gout is treated by agents to both decrease the cause and effects of uric acid crystal inflammation and pain. The pain associated with gout is commonly treated with pain and anti-inflammatory drugs such as nonsteroidal anti-inflammatory drugs (NSAIDs), colchicine and steroids. Agents that decrease sUA levels may be used to treat the cause of gout. These include agents that: inhibit the enzymes that result in uric acid production, such as xanthine oxidase inhibitors (e.g. allopurinol, febuxostat or tisopurine), or purine nucleoside phosphorylase (PNP) inhibitors (e.g. ulodesine); metabolise uric acid, such as urate oxidases - also known as uricases (e.g. pegloticase); or increase the excretion of uric acid in the urine (uricosurics), Uricosurics include agents that inhibit the transporters responsible for renal reabsorption of uric acid back into the blood, such as benziodarone, isobromindione, probenecid and sulphinpyrazone, and URAT-1 inhibitors (e.g. benzbromarone). URAT-1 is also known as solute carrier family 22 (organic anion/cation transporter), member 12, and is encoded by the gene SLC22A12. Human genetic analysis has demonstrated that polymorphisms in the SLC22A12 gene are directly associated with changes in serum uric acid. Inhibitors of uric acid transport, such as URAT-1 , are therefore effective in the treatment of gout. There is a continuing need to provide new treatments for gout that are more effective and/or are better tolerated. Certain URAT-1 inhibitors for the treatment of gout are known. WO201 1/1 59840 discloses phenylthioacetate URAT-1 inhibitors. Additionally, WO2008/1 18758, WO2009/0 12242, WO201 0/079443, WO201 2/004706, WO20 12/0047 14 and WO201 2/004743 disclose sulphonamides. There is, however, an ongoing need to provide new URAT-1 inhibitors that are good drug candidates. Furthermore, preferred compounds should have one or more of the following properties: be well absorbed from the gastrointestinal tract; be metabolically stable; have a good metabolic profile, in particular with respect to the toxicity or allergenicity of any metabolites formed; or possess favourable pharmacokinetic properties whilst still retaining their activity profile as URAT-1 inhibitors. They should be non-toxic and demonstrate few side-effects. Ideal drug candidates should exist in a physical form that is stable, non-hygroscopic and easily formulated. We have now found new sulphonamide URAT-1 inhibitors. According to a first aspect of the invention there is provided a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein: R is a 'C-linked' 5-membered heteroaryl containing one, two or three heteroatoms selected from: (a) one to three nitrogen atoms, (b) one or two nitrogen atoms and one sulphur atom and (c) one or two nitrogen atoms and one oxygen atom, wherein said heteroaryl is optionally substituted on a ring carbon atom by, valency permitting, one, two or three X1; 1 each X is independently selected from: F ; CI; CN; (Ci-C4)alkyl optionally substituted by one, two or three F ; and (Ci-C4)alkyloxy optionally substituted by one two or three F ; 2 3 5 R , R and R are independently selected from: H ; halogen; CN; (Ci-C4)alkyl optionally substituted by one, two or three F ; and (Ci-C4)alkyloxy optionally substituted by one, two or three F ; 4 R is selected from: halogen; CN; (Ci-C4)alkyl optionally substituted by one, two or three F ; and (Ci-C4)alkyloxy optionally substituted by one, two or three F ; R6 is phenyl substituted by one, two or three X2; or a 'C-linked' 6-membered heteroaryl containing one or two nitrogen atoms wherein said heteroaryl is optionally substituted by one, two or three X2; 2 7 8 each X is independently selected from: F, CI; CN; -S(C C4)alkyl; -NR R ; (CrC 6)alkyloxy optionally substituted by one, two or three F ; (C3-C6)cycloalkyloxy; (Ci-Ce)alkyl optionally substituted by one, two or three F ; and (Ci-Ce)alkyl substituted by OH; and 7 8 each R and R is independently H or (Ci-C4)alkyl or, together with the nitrogen atom to which they are attached, form a saturated 4- to 6-membered nitrogen containing monocycle. Described below are a number of embodiments (E) of this first aspect of the invention, where for convenience E 1 is identical thereto. E 1 A compound of formula (I) as defined above or a pharmaceutically acceptable salt thereof. E2 A compound according to E 1 wherein R is a 'C-linked' 5-membered heteroaryl containing one or two nitrogen atoms and one sulphur atom, wherein said heteroaryl is optionally substituted by one or two X1. E3 A compound according to E2 wherein R is a 'C-linked' 5-membered heteroaryl containing one or two nitrogen atoms and one sulphur atom, wherein said heteroaryl is optionally substituted by X1.
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