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1. (WO2017018752) BUSPIRONE DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Pub. No.: WO/2017/018752 International Application No.: PCT/KR2016/008072
Publication Date: 02.02.2017 International Filing Date: 25.07.2016
IPC:
C07D 401/12 (2006.01) ,C07D 401/14 (2006.01) ,C07D 401/06 (2006.01) ,A61K 31/444 (2006.01) ,A61K 31/506 (2006.01) ,A61K 31/497 (2006.01) ,A61K 9/20 (2006.01) ,A61K 9/48 (2006.01) ,A61K 9/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon 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
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
444
containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
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
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506
not condensed and containing further heterocyclic rings
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
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4965
Non-condensed pyrazines
497
containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
20
Pills, lozenges or tablets
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
48
Preparations in capsules, e.g. of gelatin, of chocolate
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
Applicants:
고려대학교 산학협력단 KOREA UNIVERSITY RESEARCH AND BUSINESS FOUNDATION [KR/KR]; 서울시 성북구 안암로 145 145, Anam-ro Seongbuk-gu Seoul 02841, KR
한국과학기술연구원 KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY [KR/KR]; 서울시 성북구 화랑로14길 5 5, Hwarang-ro 14-gil Seongbuk-gu Seoul 02792, KR
Inventors:
서홍석 SEO, Hong Seog; KR
심태보 SIM, Tae Bo; KR
이용직 LEE, Yong Jik; KR
윤호종 YOON, Hojong; KR
Agent:
특허법인 충현 CHUNG HYUN PATENT & LAW FIRM; 서울시 서초구 동산로 23 베델회관 8층 Bethel Bldg. 8F., 23, Dongsan-ro Seocho-gu Seoul 06779, KR
Priority Data:
10-2015-010698129.07.2015KR
10-2015-010698229.07.2015KR
Title (EN) BUSPIRONE DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
(FR) DÉRIVÉ BUSPIRONE ET COMPOSITION PHARMACEUTIQUE LE COMPRENANT
(KO) 부스피론 유도체 및 이를 함유하는 약학 조성물
Abstract:
(EN) The present invention relates to a buspirone derivative and a pharmaceutical composition comprising the same and, more particularly, to a novel buspirone derivative and a pharmaceutical composition for treating or preventing a hypertensive disease. The buspirone derivative according to the present invention falls under a novel buspirone derivative which is, in relation to buspirone which has been known to have a therapeutic effect on stress-related diseases, effective for the treatment of other pathologies. In addition, a composition for treating and preventing blood pressure-related diseases according to the present invention can treat or prevent blood pressure-related diseases such as hypertension by utilizing the buspirone derivative and thus is an invention which newly broadens the scope of utilization of buspirone. In particular, such buspirone derivative enables buspirone, which has been used only for the treatment of stress-related diseases, to be utilized for a new use for hypertension treatment. A blood pressure lowering effect, regardless of a mental stabilization effect, restores the intracellular AMPK and normalizes metabolic actions without artificially restraining the contraction-relaxation control mechanism of vascular cells, thereby fundamentally correcting causes of essential hypertension or primary hypertension, and thus having an effect of treating or preventing hypertension.
(FR) La présente invention concerne un dérivé buspirone et une composition pharmaceutique le comprenant, et plus particulièrement, un nouveau dérivé buspirone et une composition pharmaceutique de traitement ou de prévention d'une maladie hypertensive. Le dérivé buspirone selon la présente invention est un nouveau dérivé buspirone qui est, en relation à la buspirone qui est connue comme ayant un effet thérapeutique sur les maladies liées au stress, efficace pour le traitement d'autres pathologies. De plus, une composition de traitement et de prévention de maladies liées à la pression sanguine selon la présente invention peut traiter ou prévenir les maladies liées à la pression sanguine telles que l'hypertension en utilisant le dérivé buspirone et est ainsi une invention qui élargit d'une manière nouvelle la portée d'utilisation de la buspirone. En particulier, un tel dérivé buspirone permet à la buspirone, qui a été utilisée uniquement pour le traitement des maladies liées au stress, d'être utilisée pour un nouvel emploi du traitement de l'hypertension. Un effet de réduction de la pression sanguine, quel que soit l'effet de stabilisation mentale, restaure l'AMPK intracellulaire et normalise les actions métaboliques sans restreindre artificiellement le mécanisme de commande de la contraction-relaxation des cellules vasculaires, corrigeant fondamentalement de là les causes de l'hypertension essentielle ou de l'hypertension primaire, et ayant ainsi un effet de traitement ou de prévention de l'hypertension.
(KO) 본 발명은 부스피린 유도체와 이를 함유하는 약학 조성물에 관한 것으로서, 보다 구체적으로는 신규 부스피린 유도체 및 고혈압 질환을 치료하거나 예방하는 약학 조성물에 관한 것이다. 본 발명에 따른 부스피론 유도체는 기존에 스트레스성 질환에 치료 효과가 있는 것으로 알려진 부스피론에 관해, 다른 병증의 치료에도 효과가 있는 신규한 부스피론 유도체에 해당하는 것이다. 또한 본 발명에 따른 혈압질환의 치료 및 예방용 조성물은 상기 부스피론 유도체를 활용하여 고혈압 등의 혈압질환을 치료하거나 예방하는 것이 가능한 것으로서 부스피론의 활용폭을 새롭게 넓힌 발명이다. 특히 이러한 부스피론 유도체는 스트레스성 질환의 치료에만 이용되던 부스피론을 고혈압 치료라는 새로운 용도에 활용하도록 하였다. 혈압 하강효과는 정신적 안정효과와 무관하게, 인위적으로 혈관세포의 수축-이완조절 기전을 억제하지 않고, 세포내 AMPK를 회복하여 대사적작용을 정상화시킴으로써 본태성 고혈압이나 원발성 고혈압의 원인을 근본적으로 수정하여 고혈압을 치료하거나 예방하는 효과가 있다.
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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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, 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: Korean (KO)
Filing Language: Korean (KO)