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1. (WO2018101762) PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING ISCHEMIC ACUTE KIDNEY INJURY, CONTAINING TRICYCLIC DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
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Pub. No.: WO/2018/101762 International Application No.: PCT/KR2017/013891
Publication Date: 07.06.2018 International Filing Date: 30.11.2017
IPC:
A61K 31/4375 (2006.01) ,A61K 31/5377 (2006.01)
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
4353
ortho- or peri-condensed with heterocyclic ring systems
4375
the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
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
535
having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5375
1,4-Oxazines, e.g. morpholine
5377
not condensed and containing further heterocyclic rings, e.g. timolol
Applicants:
사회복지법인 삼성생명공익재단 SAMSUNG LIFE PUBLIC WELFARE FOUNDATION [KR/KR]; 서울시 용산구 이태원로55길 48 48, Itaewon-ro 55-gil Yongsan-gu Seoul 04348, KR
제일약품주식회사 JEIL PHARMACEUTICAL CO.,LTD. [KR/KR]; 서울시 서초구 사평대로 343 343, Sapyeong-daero Seocho-gu Seoul 06543, KR
Inventors:
허우성 HUH, Woo Seong; KR
장혜련 JANG, Hye Ryoun; KR
고재욱 KO, Jae Wook; KR
김정렬 KIM, Jung Ryul; KR
Agent:
김순웅 KIM, Soon Woong; KR
Priority Data:
10-2016-016290001.12.2016KR
Title (EN) PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING ISCHEMIC ACUTE KIDNEY INJURY, CONTAINING TRICYCLIC DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
(FR) COMPOSITION PHARMACEUTIQUE DE PRÉVENTION OU DE TRAITEMENT D'UNE LÉSION RÉNALE AIGUË ISCHÉMIQUE, COMPRENANT UN DÉRIVÉ TRICYCLIQUE OU UN SEL PHARMACEUTIQUEMENT ACCEPTABLE DE CE DERNIER
(KO) 트리시클릭 유도체 또는 이의 약학적으로 허용 가능한 염을 포함하는 허혈성 급성 신 손상 예방 또는 치료용 약학적 조성물
Abstract:
(EN) The present invention relates to: a pharmaceutical composition for preventing or treating ischemic acute kidney injury and delayed graft function (DGF), containing a tricyclic derivative or a pharmaceutically acceptable salt thereof; or a method for treating the ischemic acute kidney injury and DGF. The tricyclic derivative of the present invention, preferably, 10-ethoxy-8-(morpholinomethyl)-1,2,3,4-tetrahydrobenzo[h][1,6]naphthyridin-5(6H)-one dihydrochloride or a pharmaceutically acceptable salt thereof specifically inhibits, as a PARP inhibitor, PARP, thereby enabling the progress of kidney injury caused by the immune inflammatory response promotion of renal tubule cells themselves, which have been damaged by reperfusion injury, to be fundamentally inhibited without direct immunosuppression, having an excellent oral administration absorption rate, and being administrable even when renal function has deteriorated by being mainly metabolized in the liver, and thus can be more clinically useful.
(FR) La présente invention concerne : une composition pharmaceutique de prévention ou de traitement d'une lésion rénale aiguë ischémique et d'une fonction de greffe retardée (DGF), comprenant un dérivé tricyclique ou un sel pharmaceutiquement acceptable de ce dernier ; ou un procédé de traitement de la lésion rénale aiguë ischémique et du DGF. Le dérivé tricyclique de la présente invention, de préférence un dichlorhydrate de 10-éthoxy-8-(morpholinométhyl)-1,2,3,4-tétrahydrobenzo[h][1,6]naphtyridin-5(6H)-one ou un sel pharmaceutiquement acceptable de ce dernier, inhibe plus particulièrement, en tant qu'inhibiteur de PARP, la PARP, permettant ainsi l'inhibition essentielle, sans immunosuppression directe, de la progression d'une lésion rénale provoquée par la promotion de réponse inflammatoire immunitaire de cellules tubulaires rénales elles-mêmes, qui ont été endommagées par une lésion de reperfusion, possédant un excellent taux d'absorption d'administration orale, et étant apte à être administré même en cas de détérioration de la fonction rénale du fait qu'il est principalement métabolisé dans le foie, et peut donc être cliniquement avantageux.
(KO) 본 발명은 트리시클릭 유도체 또는 이의 약학적으로 허용 가능한 염을 포함하는 허혈성 급성 신 손상, 이식신 기능 지연 (delayed graft function, DGF)의 예방 또는 치료용 약학적 조성물 또는 이의 치료 방법에 관한 것이다. 본 발명의 트리시클릭 유도체, 바람직하게는 10-에톡시-8-(모르폴리노메틸)-1,2,3,4-테트라히드로벤조[h][1,6]나프티리딘-5(6H)-온 디히드로클로라이드 또는 이의 약학적으로 허용 가능한 염은 PARP의 저해제로 PARP를 특이적으로 저해함으로써, 재관류 손상에 의해 손상된 신세관 세포 자체가 면역학적 염증 반응을 촉진하여 신 손상을 진행시키는 것을 직접적인 면역억제작용 (immunosuppression) 없이 원천적으로 억제할 수 있으며, 경구 투여 흡수율이 좋을 뿐만 아니라, 주로 간으로 대사되어 신기능이 저하된 상태에서도 투여 가능하므로, 임상에서 더욱 유용하게 사용될 수 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, 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: Korean (KO)
Filing Language: Korean (KO)