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161. (WO2012176804) GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVE
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Pub. No.:    WO/2012/176804    International Application No.:    PCT/JP2012/065744
Publication Date: 27.12.2012 International Filing Date: 20.06.2012
IPC:
C07H 17/02 (2006.01), A61K 31/155 (2006.01), A61K 31/426 (2006.01), A61K 31/64 (2006.01), A61K 31/7056 (2006.01), A61K 45/00 (2006.01), A61P 3/10 (2006.01), A61P 43/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
17
Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
02
Heterocyclic radicals containing only nitrogen as ring hetero atoms
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
13
Amines, e.g. amantadine
155
Amidines (), e.g. guanidine (H2N-C(NH)-NH2), isourea (HNC(OH)NH2), isothiourea (HNC(SH)-NH2)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425
Thiazoles
426
1,3-Thiazoles
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
64
Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
70
Carbohydrates; Sugars; Derivatives thereof
7042
Compounds having saccharide radicals and heterocyclic rings
7052
having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
7056
containing five-membered rings with nitrogen as a ring hetero atom
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45
Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
08
for glucose homeostasis
10
for hyperglycaemia, e.g. antidiabetics
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43
Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108
Applicants: KISSEI PHARMACEUTICAL CO., LTD. [JP/JP]; 19-48, Yoshino, Matsumoto-shi, Nagano 3998710 (JP) (For All Designated States Except US).
FUJIKURA, Hideki [JP/JP]; (JP) (For US Only).
FUJIOKA, Minoru [JP/JP]; (JP) (For US Only)
Inventors: FUJIKURA, Hideki; (JP).
FUJIOKA, Minoru; (JP)
Priority Data:
2011-136554 20.06.2011 JP
Title (EN) GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVE
(FR) DÉRIVÉ DE GLUCOPYRANOSYLOXYPYRAZOLE
(JA) グルコピラノシルオキシピラゾール誘導体
Abstract: front page image
(EN)The present invention addresses the problem of providing a compound having human SGLT2 inhibitory activity, a prodrug of the compound, a pharmacologically acceptable salt of the compound, and a pharmaceutical use of the compound. The present invention provides a compound which is represented by general formula (1) (wherein RA represents a hydrogen atom, a C1-6 alkyl group or the like; RB represents a C1-6 alkoxy group or the like; each of RC and RD independently represents a hydrogen atom, a halogen atom or the like; and n represents a number of 1-3) and has human SGLT2 inhibitory activity, a prodrug of the compound, or a pharmacologically acceptable salt of the compound. In addition, the compound of the present invention can be utilized as a therapeutic or prophylactic agent for diseases associated with high blood sugar.
(FR)La présente invention aborde le problème de fournir un composé ayant une activité inhibitrice de SGLT2 humain, un promédicament du composé, un sel pharmacologiquement acceptable du composé et une utilisation pharmaceutique du composé. La présente invention concerne un composé qui est représenté par la formule générale (1) (où RA représente un atome d'hydrogène, un groupe alkyle en C1-6 ou similaire ; RB représente un groupe alcoxy en C1-6 ou similaire ; chacun de RC et RD indépendamment représente un atome d'hydrogène, un atome d'halogène ou similaire ; et n représente un nombre de 1-3) et présente une activité inhibitrice de SGLT2 humain, un promédicament du composé ou un sel pharmacologiquement acceptable du composé. De plus, le composé de la présente invention peut être utilisé en tant qu'agent thérapeutique ou prophylactique pour des maladies associées à une hyperglycémie.
(JA)本発明は、ヒトSGLT2阻害活性を有する化合物もしくはそのプロドラッグ、またはその薬理学的に許容される塩、およびその医薬用途を提供することを課題とする。本発明は、ヒトSGLT2阻害活性を有する、一般式(1)〔式中、Rは水素原子またはC1-6アルキル基等、RはC1-6アルコキシ基等、RおよびRは独立して、水素原子、ハロゲン原子等、nは1~3を表す〕で表される化合物もしくはそのプロドラッグ、またはその薬理学的に許容される塩を提供するものである。更に、本発明の化合物は、高血糖に起因する疾患の治療薬または予防薬として利用できる。
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 Org. (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (EAPO) (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (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 (OAPI) (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)