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(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 17 June 2010 (17.06.2010) WO 2010/068601 Al (51) International Patent Classification: Hoechst, Building K801, D-65926 Frankfurt am Main C07H 17/00 (2006.01) A61K 31/70 (2006.01) (DE). BYARD, Stephen [GB/GB]; c/o Sanofi-aventis C07H 17/02 (2006.01) U.K., Willowburn Avenue, Alnwick, Northumberland NE66 2JH (GB). DONEGAN, Timothy [US/US]; c/o (21) International Application Number: Sanofi-aventis, 104 1 Route 202-206, Mail Code: PCT/US2009/067046 BWD-3O3A, Bridgewater, New Jersey 08807 (US). (22) International Filing Date: GILL, Harpal S . [US/US]; c/o Sanofi-aventis, 1041 8 December 2009 (08.12.2009) Route 202-206, Mail Code: BWD-3O3A, Bridgewater, New Jersey 08807 (US). LIEBERMAN, Harvey English (25) Filing Language: [GB/US]; c/o Sanofi-aventis, 1041 Route 202-206, Mail (26) Publication Language: English Code: BWD-3O3A, Bridgewater, New Jersey 08807 (US). NAGEL, Norbert [DE/DE]; c/o Sanofi-aventis Deutsch¬ (30) Priority Data: land GmbH, Industriepark Hoechst, Building K801, 61/120,771 8 December 2008 (08.12.2008) U S D-65926 Frankfurt am Main (DE). PLETTENBURG, 61/120,755 8 December 2008 (08.12.2008) U S Oliver [DE/DE]; c/o Sanofi-aventis Deutschland GmbH, 0955430 3 1 July 2009 (3 1.07.2009) F R Industriepark Hoechst, Building K801, D-65926 Frank¬ 0904040 2 5 August 2009 (25.08.2009) F R furt am Main (DE). SECORD, Elizabeth [US/US]; c/o (71) Applicant (for all designated States except US): Sanofi-aventis, 104 1 Route 202-206, Mail Code: BWD-3O3A, Bridgewater, New Jersey 08807 (US). SANOFI-AVENTIS [PR/PR]; 174 avenue d e France, F-75013 Paris (FR). WEIBERTH, Franz J . [US/US]; c/o Sanofi-aventis, 1041 Route 202-206, Mail Code: BWD-3O3A, Bridgewa¬ (71) Applicant (for US only): GORDONOV, Natalia (ex¬ ter, New Jersey 08807 (US). YU, Yong [CN/US]; c/o ecutrix for the deceased inventor) [US/US]; c/o Sanofi- Sanofi-aventis, 104 1 Route 202-206, Mail Code: aventis, 1041 Route 202-206, Mail Code: BWD-3O3A, BWD-3O3A, Bridgewater, New Jersey 08807 (US). Bridgewater, New Jersey 08807 (US). (74) Agents: KURYS, Barbara, E . et al; Sanofi-aventis U.S. (72) Inventor: GORDONOV, Boris (deceased). Inc., 1041 Route 202-206, Mail Code: BWD-3O3A, Bridgewater, N J 08807 (US). (72) Inventors; and (75) Inventors/Applicants (for US only): BAUMGARTNER, (81) Designated States (unless otherwise indicated, for every Bruno [DE/DE]; c/o Sanofi-aventis Deutschland GmbH, kind of national protection available): AE, AG, AL, AM, Industriepark Hoechst, Building K801, D-65926 Frank¬ AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, furt am Main (DE). BERCHTOLD, Harald [DE/DE]; c/ CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, o Sanofi-aventis Deutschland GmbH, Industriepark DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, [Continued on next page] (54) Title: A CRYSTALLINE HETEROAROMATIC FLUOROGL YCOSIDE HYDRATE, PROCESSES FOR MAKING, METHODS O F USE AND PHARMACEUTICAL COMPOSITIONS THEREOF (57) Abstract: A novel crystalline heteroaromatic fluoro glycoside hydrate, processes for making, methods o f use and pharmaceu- ttiiccaall ccoommppoossiittiioonnss tthheerreeooff.. TThhee iinnvveennttiioonn rreellaatteess ttoo a ccrryyssttaalllliinne hydrate o f the formula (I) in which n has a value o f from 0.9 to 1. 1. The compound is suitable, for example, as an antidiabetic. HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, MC, MK, MT, NL, NO, PL, PT, RO, SE, SI, SK, SM, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, ML, MR, NE, SN, TD, TG). SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. Declarations under Rule 4.17: — of inventorship (Rule 4.1 7(iv)) (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, Published: GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, — with international search report (Art. 21(3)) ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM), European (AT, BE, BG, CH, CY, CZ, DE, DK, EE, A CRYSTALLINE HETEROAROMATIC FLUOROGLYCOSIDE HYDRATE, PROCESSES FOR MAKING, METHODS OF USE AND PHARMACEUTICAL COMPOSITIONS THEREOF Field of the Invention The invention relates to a crystalline hydrate of a heteroaromatic fluoroglycoside known as 4-[(4-methoxyphenyl)methyl]-5-(thfluoromethyl)-1 H-pyrazole-3-yl]-4-deoxy- 4-fluoro-beta-D-glucopyranoside. Background of the Invention Heteroaromatic fluoroglycosides have been described in EP1 572708 B 1 and Published United States Patent Application US 2004/0259819. The aforementioned patent and/or application makes no mention as to the particular physical form of 4-[(4- methoxyphenyl)methyl]-5-(trifluoromethyl)-1 H-pyrazole-3-yl]-4-deoxy-4-fluoro-beta-D- glucopyranoside provided from the procedure disclosed therein or the hydration state or physical purity of the compound provided from the procedure. Furthermore, there is no physical chemical data reported for 4-[(4-methoxyphenyl)methyl]-5- (thfluoromethyl)-1 H-pyrazole-3-yl]-4-deoxy-4-fluoro-beta-D-glucopyranoside in said published patent/application that suggests the physical form of the product obtained. It is an object of the invention to provide a stable hydrate of said compound. It is an object of the invention to provide a heteroaromatic fluoroglycoside which, compared to that described in EP1 572708 B 1 and Published United States Patent Application US 2004/025981 9, has improved properties. Another object is to increase the storage stability of the amorphous heteroaromatic fluoroglycoside from EP1 572708 B 1 which is a crucial parameter for formulating pharmaceuticals. Another object is to provide processes for the preparation of a stable monohydrate form of 4-[(4-methoxyphenyl)methyl]-5-(thfluoromethyl)-1 H-pyrazole-3-yl]-4-deoxy-4- fluoro-beta-D-glucopyranoside or a tautomer thereof (henceforth referred to as "Form A"). The object is achieved by providing a stable crystalline hydrate of the formula I in which n has a value of from 0.9 to 1. 1 or a tautomer thereof. Although widespread, not all pharmaceutically active compounds form hydrates or solvates. The existence of hydrates, their crystal structure and properties are unpredictable. Preference is given to the crystalline hydrate of the compound of the formula I or a tautomer thereof in which n has a value of 1. Detailed Description of the Drawings Figure 1: Form A exhibits the XRPD shown. The XRPD was measured in transmission with Cu-K α1 radiation at room temperature. Figure 2 shows the Raman spectrum of Form A . Figure 3 shows the DSC thermogram of Form A . Figure 4 shows the TG analysis of Form A . Detailed Description of the Invention By providing a crystalline hydrate of formula I (or more specifically, Form A) according to the invention, the active ingredient - is easier to purify (for example by recrystallization) - can have a defined purity required for the approval of a pharmaceutical - is readily detectable and identifiable by customary methods such as XRPD (X- ray powder diffraction), melting point, IR (infrared spectrum), and it has - has a reproducible and stable physical quality. Crystalline active ingredients are generally more stable than amorphous active ingredients. Problems with the degradation of the active ingredients and the degradation products formed are thus avoided. The amorphous form of an active ingredient may also comprise an unwanted content of solvents. These are generally difficult to remove, since recrystallization is not possible. The amorphous form is a more energetic state than a crystalline form and, as such, is more difficult to stabilize. Molecules of an amorphous material may spontaneously rearrange to a lower energy crystalline one leading to a change in activity of the active ingredient. As a consequence there may be significant effect on the reliability of the active ingredient and thus a risk for the patient. It is also difficult to prove that different batches of amorphous active ingredient are identical. A further embodiment of the invention comprises Form A wherein the XRPD, measured with CuKa radiation, has a main peak of 20.27 degrees 2 theta ± 0.2 degrees 2 theta. A further embodiment of the invention comprises Form A wherein the XRPD, measured with CuKa radiation, has at least peaks of the following 2 theta values: 14.88, 20.27, 22.98 ± 0.2 degrees 2 theta. A further embodiment of the invention comprises Form A wherein the XRPD, measured with CuKa radiation, has at least peaks of the following 2 theta values: 5.98, 14.88, 20.27, 22.98, 26.52 ± 0.2 degrees 2 theta. A further embodiment of the invention comprises Form A wherein the XRPD, measured with CuKa radiation, has at least peaks of the following 2 theta values: 5.98, 7.48, 12.09, 14.88, 14.99, 20.27, 20.75, 22.81 , 22.98, 26.52, 27.60, 3 1 .01 ± 0.2 degrees 2 theta. Formulations The amount of a compound of formula I necessary to achieve the desired biological effect depends on a number of factors, for example the specific compound chosen, the intended use, the mode of administration and the clinical condition of the patient.
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  • Lipoprotein Lipase and Obesity

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    Vol.4, No.12A, 1405-1412 (2012) Health http://dx.doi.org/10.4236/health.2012.412A203 Lipoprotein lipase and obesity Masataka Kusunoki1*, Kazuhiko Tsutsumi2, Daisuke Sato3, Takao Nakamura3 1Department of Internal Medicine, Medical Clinic, Aichi Medical University, Nagoya, Japan; *Corresponding Author: [email protected] 2Okinaka Memorial Institute for Medical Research, Tokyo, Japan 3Department of Biomedical Information Engineering, Graduate School of Medical Science, Yamagata University, Yamagata, Japan Received 11 October 2012; revised 11 November 2012; accepted 24 November 2012 ABSTRACT stored in adipose tissue. The balance between these competing effects could determine whether increased Obesity is one of the fast-growing major dis- LPL activity will lead to a reduced rate of weight gain or eases in developed and developing countries. to increased adiposity through increased rates of adipose As has been persuasively argued, long-term tissue storage of TG. An imbalance of LPL activity may imbalance between intake and expenditure of fat alter the partitions of plasma TG between muscle and is a central factor in the etiology of obesity. adipose tissue, and thus influence insulin resistance and Obesity aggravates insulin resistance and pro- obesity. motes cardiovascular diseases and atheroscle- Institute of Otsuka Pharmaceutical Factory, Inc. syn- rosis. We hypothesized that elevating lipopro- thesized the LPL activator NO-1886 ([4-(4-bromo-2- tein lipase (LPL) activity in skeletal muscle cyano-phenylcarbamoyl)-benzyl]-phosphonic acid diethyl would cause an improvement of obesity. To test ester, CAS no.: 133208-93-2, generic name: ibrolipim). this hypothesis, we studied the effects of the Hara et al. reported that LPL activator NO-1886 LPL activator NO-1886 in obese animals.
  • 1 Lipid Lowering Agents, Cognitive Decline, and Dementia

    1 Lipid Lowering Agents, Cognitive Decline, and Dementia

    Lipid Lowering Agents, Cognitive Decline, and Dementia: The Three-City Study Marie-Laure Ancelin, PhD.a,b,§,*, Isabelle Carrière, PhD.a,b,§, Pascale Barberger-Gateau PhD.c, Sophie Auriacombe, MDc, Olivier Rouaud, MDd, Spiros Fourlanos, MD, PhD.e, Claudine Berr, PhD.a,b, Anne-Marie Dupuy, PhD.a,b,f, Karen Ritchie, PhD.a,b,g Running title: Lipid Lowering Agents and Cognitive Decline a Inserm, U1061, Montpellier, F-34093 France b Université Montpellier 1, Montpellier, France c Inserm, U897, Bordeaux, F-33076 France d Centre Mémoire Ressources et Recherche, Centre Hospitalier Universitaire, Dijon, France e Department of Diabetes & Endocrinology, Royal Melbourne Hospital, Melbourne, Australia f CHU Montpellier, Laboratoire de Biochimie, Hopital Lapeyronie, Montpellier, France g Faculty of Medicine, Imperial College, London, W12 0NN, U.K. *Corresponding author: Inserm U1061, Hopital La Colombiere, 39, avenue C. Flahault, BP 34493, 34093 Montpellier Cedex 5, France Tel: +33 499 614 562; Fax: +33 499 614 579; E-mail address: [email protected] § Joint first authors Declaration of interest: No conflict of interest. Paper length: 2863 words Title character count: 67 Abstract: 231 words 3 Tables 1 Abstract The aim of this prospective cohort study was to evaluate the effects of lipid lowering agent (LLA) intake on cognitive function in 6830 community-dwelling elderly persons. Cognitive performance (global cognitive functioning, visual memory, verbal fluency, psychomotor speed and executive function), clinical diagnosis of dementia, and fibrate and statin use, were evaluated at baseline, and 2, 4, and 7 year follow-up. Multivariate Cox models were stratified by gender and adjusted for sociodemographic characteristics, mental and physical health including vascular risk factors, and genetic vulnerability (apolipoprotein E and cholesteryl ester transfer protein).