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1. (WO2019065532) T-TYPE CALCIUM CHANNEL INHIBITOR
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Pub. No.: WO/2019/065532 International Application No.: PCT/JP2018/035170
Publication Date: 04.04.2019 International Filing Date: 21.09.2018
IPC:
C07D 311/32 (2006.01) ,A61K 31/353 (2006.01) ,A61P 25/00 (2006.01) ,A61P 29/00 (2006.01) ,A61P 43/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
311
Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02
ortho- or peri-condensed with carbocyclic rings or ring systems
04
Benzo [b] pyrans, not hydrogenated in the carbocyclic ring
22
with oxygen or sulfur atoms directly attached in position 4
26
with aromatic rings attached in position 2 or 3
28
with aromatic rings attached in position 2 only
32
2, 3-Dihydro derivatives, e.g. flavanones
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
335
having oxygen as the only ring hetero atom, e.g. fungichromin
35
having six-membered rings with one oxygen as the only ring hetero atom
352
condensed with carbocyclic rings, e.g. cannabinols, methantheline
353
3,4-Dihydrobenzopyrans, e.g. chroman, catechin
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29
Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
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:
学校法人近畿大学 KINKI UNIVERSITY [JP/JP]; 大阪府東大阪市小若江3丁目4番1号 4-1, Kowakae 3-chome, Higashiosaka-shi, Osaka 5778502, JP
国立大学法人富山大学 NATIONAL UNIVERSITY CORPORATION UNIVERSITY OF TOYAMA [JP/JP]; 富山県富山市五福3190 3190, Gofuku, Toyama-shi, Toyama 9308555, JP
扶桑薬品工業株式会社 FUSO PHARMACEUTICAL INDUSTRIES, LTD. [JP/JP]; 大阪府大阪市中央区道修町1丁目7番10号 7-10, Dosho-machi 1-chome, Chuo-ku, Osaka-shi, Osaka 5410045, JP
Inventors:
川畑 篤史 KAWABATA, Atsufumi; JP
関口 富美子 SEKIGUCHI, Fumiko; JP
坪田 真帆 TSUBOTA, Maho; JP
豊岡 尚樹 TOYOOKA, Naoki; JP
西川 裕之 NISHIKAWA, Hiroyuki; JP
Agent:
山尾 憲人 YAMAO, Norihito; JP
江間 晴彦 EMA, Haruhiko; JP
Priority Data:
2017-18871728.09.2017JP
Title (EN) T-TYPE CALCIUM CHANNEL INHIBITOR
(FR) INHIBITEUR DU CANAL CALCIQUE DE TYPE T
(JA) T型カルシウムチャネル阻害剤
Abstract:
(EN) Developed is a novel analgesic, the therapeutic targets of which are T-type calcium channels. The present invention provides a T-type calcium channel inhibitor which is a compound represented by formula (1), a pharmaceutically acceptable salt of this compound, or a solvate of this compound. The present invention also provides: this T-type calcium channel inhibitor; a pharmaceutical product which contains this T-type calcium channel inhibitor; and a therapeutic agent or prophylactic agent for diseases, the effective action of which is T-type calcium channel inhibitory activity. (In the formula, each of R1 and R2 independently represents H or -OH; R3 represents -OH; R4 represents -OH or -H; and R5 represents a linear or branched alkyl or cycloalkyl alkyl group having 1-10 carbon atoms, or a linear or branched alkenyl or cycloalkyl alkenyl group having 2-10 carbon atoms.)
(FR) La présente invention concerne un nouvel analgésique dont les cibles thérapeutiques sont des canaux calciques de type T. La présente invention concerne un inhibiteur du canal calcique de type T, qui est un composé représenté par la formule (1), un sel pharmaceutiquement acceptable de ce composé, ou un solvate de celui-ci. La présente invention concerne également : ledit inhibiteur du canal calcique de type T; un produit pharmaceutique contenant ledit inhibiteur du canal calcique de type T; et un agent thérapeutique ou un agent prophylactique pour des maladies, dont l'action efficace est une activité d'inhibition du canal calcique de type T. (Dans la formule, chacun des R1 et R2 représente indépendamment H ou -OH; R3 représente -OH; R4 représente -OH ou -H; et R5 représente un groupe alkyle ou cycloalkyle linéaire ou ramifié ayant de 1 à 10 atomes de carbone, ou un groupe alcényle ou cycloalkyle alcényle linéaire ou ramifié ayant de 2 à 10 atomes de carbone.)
(JA) T型カルシウムチャネルを治療標的として新しい鎮痛薬を開発する。 本発明は、下記式(1)で表される化合物、この化合物の医薬的に許容され得る塩またはこの化合物の溶媒和物である、T型カルシウムチャネル阻害剤を提供する。本発明はまた、このT型カルシウムチャネル阻害剤、T型カルシウムチャネル阻害剤を含む医薬、T型カルシウムチャネル阻害作用を有効作用とする疾患の治療薬または予防薬も提供する。 [式中、 RおよびRは、それぞれ独立して、Hまたは-OHであり、 Rは、-OHであり、 Rは-OHまたは-Hであり、 Rは、炭素数1~10の直鎖もしくは分枝鎖状のアルキル基もしくはシクロアルキル-アルキル基、または炭素数2~10の直鎖もしくは分枝鎖状のアルケニル基もしくはシクロアルキル-アルケニル基である]。
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, 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, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (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 (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)