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Pub. No.:    WO/2012/116349    International Application No.:    PCT/US2012/026658
Publication Date: 30.08.2012 International Filing Date: 24.02.2012
C07D 205/08 (2006.01), C07D 205/02 (2006.01), A61K 31/397 (2006.01), A61P 3/10 (2006.01), A61P 9/12 (2006.01)
Applicants: AMPLIO PHARMA, LLC [US/US]; 240 Grand Avenue Suite 5 Leonia, NJ 07605 (US) (For All Designated States Except US).
CHILDS, Scott, L. [US/US]; (US) (For US Only).
BARISHANSKY, Nathan [US/US]; (US) (For US Only).
LINGIREDDY, Shreenivas, Reddy [IN/US]; (US) (For US Only)
Inventors: CHILDS, Scott, L.; (US).
LINGIREDDY, Shreenivas, Reddy; (US)
Agent: O'BRIEN, Michelle; O'Brien Jones, PLLC 1951 Kidwell Drive Suite 740 Tysons Corner, VA 22182 (US)
Priority Data:
61/447,049 26.02.2011 US
Abstract: front page image
(EN)The invention relates to a novel L-proline cocrystal of l-(4-fluorophenyl)-3(R)-[3-(4- fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone. The invention further relates to a novel imidazole cocrystal of l-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)- 3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone. The preparation and characterization of the novel cocrystals according to various embodiments of the invention are described. The invention also relates to pharmaceutical compositions containing the novel L- proline and/or novel imidazole cocrystal, and the therapeutic use of the novel cocrystals to treat and/or prevent various disorders and/or conditions, including primary hypercholesterolemia, mixed hyperlipidemia and homozygous familial sitosterolemia.
(FR)La présente invention concerne un nouveau cocristal de L-proline de 1-(4-fluorophényl)-3(R)-[3-(4-fluorophényl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphényl)-2-azétidinone. L'invention concerne en outre un nouveau cocristal d'imidazole de 1-(4-fluorophényl)-3(R)-[3-(4-fluorophényl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphényl)-2-azétidinone. La préparation et la caractérisation des nouveaux cocristaux selon différents modes de réalisation de l'invention sont décrites. L'invention concerne en outre des compositions pharmaceutiques contenant le nouveau cocristal de L-proline et/ou le nouveau cocristal d'imidazole, et l'utilisation thérapeutique des nouveaux cocristaux pour traiter et/ou prévenir différents troubles et/ou différentes affections, comprenant l'hypercholestérolémie primaire, l'hyperlipidémie mixte et la sitostérolémie familiale homozygote.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, 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, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)