KR20030077568A - 소수성 폴리아민 유사체들과 그 사용에 대한 방법들 - Google Patents
소수성 폴리아민 유사체들과 그 사용에 대한 방법들 Download PDFInfo
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Abstract
Description
Claims (28)
- 다음의 식으로 표현되는R-X-L-폴리아민여기서 R은 곧은 또는 가지달린 탄소 10 내지 50의 포화 또는 불포화된 지방족화합물, 카르복시알킬, 카르발콕시알킬, 또는 알콕시; 탄소1내지 8의 지방족고리화합물; 단일 또는 다중고리 아릴 치환된 또는 비치환된 지방족 화합물; 지방족-치환된 또는 비치환된 단일 또는 다중고리 방향족화합물; 단일 또는 다중고리의 헤테로고리화합물; 단일 또는 다중고리의 헤테로고리 지방족화합물; 아릴 술포닐;X는 -CO-,SO2- 또는 -CH2-;이고L은 공유성결합 또는 자연 발생적인 아미노산, 오르니틴, 2,4-다이아미노부티릭산, 또는 그들의 유도체들인 폴리아민 유사체 또는 유도체.
- 다음의 식Ⅱ에 의해 표시되는여기서 a, b, 와 c는 독립적으로 1 내지 10의 범위; d와 e는 독립적으로 0내지 30의 범위; 각 X는 독립적으로 탄소(C) 또는 황(S)원소이며, R1과 R2은 독립적으로 H, 또는 곧은 또는 가지달린 탄소 1 내지 50의 포화 또는 불포화된 지방족화합물, 카르복시알킬, 카르발콕시알킬, 또는 알콕시; 탄소 1 내지 8의 지방족고리화합물; 단일 또는 다중고리 아릴 치환된 또는 비치환된 지방족화합물; 지방족-치환된 또는 비치환된 단일 또는 다중고리의 방향족화합물; 단일 또는 다중고리의 헤테로고리형화합물; 단일 또는 다중고리의 헤테로고리형 지방족화합물; 탄소 1 내지 10의 알킬; 아릴 술포닐; 또는 시아노의 군으로부터 선택되고; 또는R1X{O}n-와 R2X{O}n-의 각각이 독립적으로 H에 의해 치환되며;*는 키럴 탄소위치를 나타내며;그리고 X가 C인 경우 n은 1이며; X가 S인 경우 n은 2; 그리고 X가 C인 경우 XO그룹은 n이 0인 CH2인 폴리아민 유사체 또는 유도체.
- 다음의 식Ⅲ에 의해 표시되는여기서, a, b, 와 c는 독립적으로 1 내지 10의 범위이고 d와 e는 독립적으로0내지 30의 범위; 그리고R1, R2, R3, 및 R4는 같거나 다르며, 독립적으로 H, 또는 곧은 또는 가지달린 탄소 1 내지 50의 포화 또는 불포화된 지방족화합물, 카르복시알킬, 카르발콕시알킬, 또는 알콕시; 탄소 1 내지 8의 지방족고리화합물; 단일 또는 다중고리 아릴 치환된 또는 비치환된 지방족화합물; 지방족-치환된 또는 비치환된 단일 또는 다중고리의 방향족화합물; 단일 또는 다중고리의 헤테로고리형화합물; 단일 또는 다중고리의 헤테로고리형 지방족화합물; 탄소1내지 10의 알킬; 아릴 술포닐; 또는 시아노군으로부터 선택되는 폴리아민 유사체 또는 유도체.
- 다음의 식Ⅳ로 표시되는여기서, a, b, 와 c는 독립적으로 1내지 10의 범위이고 d와 e는 독립적으로 0내지 30의 범위; 그리고R1, R2, R3, 및 R4는 같거나 다르며, 독립적으로 H, 또는 곧은 또는 가지달린 탄소 1 내지 50의 포화 또는 불포화된 지방족화합물, 카르복시알킬, 카르발콕시알킬, 또는 알콕시; 탄소 1 내지 8의 지방족고리화합물; 단일 또는 다중고리 아릴 치환된 또는 비치환된 지방족화합물; 지방족-치환된 또는 비치환된 단일 또는 다중고리의 방향족화합물; 단일 또는 다중고리의 헤테로고리형화합물; 단일 또는 다중고리의 헤테로고리형 지방족화합물; 탄소 1 내지 10의 알킬; 아릴 술포닐; 또는 시아노의 군으로부터 선택되는 폴리아민 유사체 또는 유도체.
- 다음의 식Ⅴ로 표시되는여기서, a, b, 와 c는 독립적으로 1 내지 10의 범위이고 d와 e는 독립적으로 0 내지 30의 범위; 그리고Z1은 NR1R3이고 Z2는 -R1, -CHR1R2또는 -CR1R2R3로부터 선택되어지거나, 또는 Z2는 NR2R4이고 Z1은 -R1, -CHR1R2또는 -CR1R2R3로부터 선택되어지며,R1, R2, 그리고 R3는 같거나 다르며, 독립적으로 H, 또는 곧은 또는 가지달린 탄소1내지 50의 포화 또는 불포화된 지방족화합물, 카르복시알킬, 카르발콕시알킬, 또는 알콕시; 탄소 1 내지 8의 지방족고리화합물; 단일 또는 다중고리 아릴 치환된 또는 비치환된 지방족화합물; 지방족-치환된 또는 비치환된 단일 또는 다중고리의방향족화합물; 단일 또는 다중고리의 헤테로고리형화합물; 단일 또는 다중고리의 헤테로고리형 지방족화합물; 탄소1내지 10의 알킬; 아릴 술포닐; 또는 시아노의 군으로부터 선택되는 폴리아민 유사체 또는 유도체.
- 제 1항 내지 5항중 어느 한 항에 있어서,상기 a, b, 와 c는 유사체 또는 유도체가 푸트레신, 스퍼민,또는 스퍼미딘에 근거한 유사체 또는 유도체.
- 제 1항 내지 5항중 어느 한 항에 있어서,R1, R2, R3, 그리고 R4의 각각은, 독립적으로 H, 또는 곧은 또는 가지달린 탄소 1 내지 50의 포화 또는 불포화된 지방족화합물, 카르복시알킬, 카르발콕시알킬, 또는 알콕시로 부터 선택된 유사체 또는 유도체.
- 제 1항에 있어서,L은 리신, 아스파틱산, 글루탐산, 오르니틴, 또는 2,4-다이아미노부틸산으로부터 선택된 아미노산인 유사체 또는 유도체.
- 도 2에 도시된 것과 같은 스퍼민에 기초한 화합물 IA4, IB4, IA7, IVB22, 또는 IVA22 로부터 선택된 폴리아민 유사체 또는 유도체.
- 도 12에 도시된 화합물로부터 선택된 폴리아민 유사체 또는 유도체.
- 제 1항 내지 5항중 어느 한 항에 있어서,d는 4이고 e는 0인 유사체 또는 유도체.
- 제 1항 내지 5항중 어느 한 항에 있어서,R1, R2, R3, 그리고 R4의 각각은, 독립적으로 H, 또는로부터 선택되고,각각의 g, h, i, j, 그리고 k는 독립적으로 0 내지 15이고, E는 "엔트게겐(entgegen)"을 의미하고 Z는 "쭈잠멘(zusammen)"을 의미하는 유사체 또는 유도체.
- 제 1항 내지 12항중 어느 한 항에 의한 폴리아민 유사체 또는 유도체와 첨가제, 희석제 또는 용액(vehicle)을 포함하는 조성물.
- 제 13항에 있어서,상기 첨가제, 희석제 또는 용액은 약리학적 또는 미용학적으로 수용가능한 조성물.
- 제 13항에 있어서,상기 첨가제, 희석제 또는 용액은 국부적으로나 귀 내부에 투여되는 조성물.
- 제 13항에 있어서,폴리아민 생합성 억제재를 더 포함하는 조성물.
- 제 16항에 있어서,상기 억제재는 DFMO인 조성물.
- 제 13항에 있어서,정맥주사, 피하주사, 근육내, 두개내의, 복강내주사, 국부적인, 피부를 통한, 질을 통한, 코를 통한, 기관지를 통한, 두개내의, 안구내의, 귀를 통한, 직장또는 비경구적인 투여를 위한 구성인 조성물.
- 암, 골다공증, 천식, 자가면역의 병, 류마티즘성 관절염, 조직적 낭창 에리서메토서스, 유형Ⅰ의 인슐린 의존 당뇨병, 건선, 레스테노시스, 피부의 원하지 않는 털의 성장 억제, 조직 이식, 아프리카 졸음병, 염증, 부갑상선기능항진증, 소화성 궤양 치료, 녹내장, 알쯔하이머 병, 심방 심계항진 억압, 창자의 운동서의 자극 또는 저해, 크론 병, 그리고 다른 염증의 창자병, 고혈압, 충격, 간질, 두려움, 신경쇄약증, 하이퍼럴제직 상태, 화학치료요법으로 유도된 청각손실로부터의 헤어세포의 보호, 코카인 중독과 과다복용을 처리하는데 코카인 강화와 갈망의 약리학적 촉진으로부터 선택된 하나 이상의 이상징후를, 제 1항 내지 12항중 어느 한 항에 의한 유사체 또는 유도체나, 또는 13항 내지 18항중 어느 한 항의 조성물을 상기한 하나이상의 이상징후로 고생하는 대상에 투여하여 치료하는 방법.
- 제 19항에 있어서,상기 투여는 조직계통투여(systemic)인 방법.
- 제 19항 또는 20항에 있어서,상기 투여는 구강투여인 방법.
- 제 19항 또는 20항에 있어서,상기투여는 시간 방출 용액(time release vehicle)을 통한 것인 방법.
- 제 1항 내지 12항중 어느 한 항에 의한 유사체 또는 유도체이거나 청구항 13항 내지 18항중 어느 한 항의 조성물을 균성, 박테리아성, 바이러스성, 또는 해충성 병으로 고생하는 대상에 투여하여 치료하는 방법.
- 제 1항 내지 12항중 어느 한 항에 의한 유사체 또는 유도체로 세포와 접촉시키는 것을 포함하는 핵산의 세포흡수를 촉진하는 방법.
- 제 1항 내지 12항중 어느 항 항에 의한 유사체 또는 유도체이거나 청구항 13항 내지 18항중 어느 한 항에 의한 조성물을 털 성장 억제가 필요한 대상에 국부적으로 투여하는 것을 포함하는 털 성장 억제 방법.
- 제 25항에 있어서,상기 유사체 또는 유도체는 화장용도로 구성되는 것인 방법.
- 제 1항 내지 12항중 어느 한 항에 의한 유사체 또는 유도체를 청각 손실을 억제할 필요가 있는 대상에 투여하는 청각 손실 억제 방법.
- 제 27항에 있어서,상기 대상은 암에 대한 화학치료에 의해 청각 손실을 일으키기 쉬운 대상인 방법.
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EP1373185B1 (en) * | 2001-01-08 | 2017-03-01 | Aminex Therapeutics, Inc. | Hydrophobic polyamine analogs and methods for their use |
-
2002
- 2002-01-08 EP EP02717293.1A patent/EP1373185B1/en not_active Expired - Lifetime
- 2002-01-08 US US10/296,259 patent/US6963010B2/en not_active Ceased
- 2002-01-08 RU RU2003124640/04A patent/RU2003124640A/ru not_active Application Discontinuation
- 2002-01-08 CA CA2433807A patent/CA2433807C/en not_active Expired - Lifetime
- 2002-01-08 KR KR1020037009149A patent/KR100859929B1/ko active IP Right Grant
- 2002-01-08 JP JP2002554639A patent/JP4253503B2/ja not_active Expired - Fee Related
- 2002-01-08 WO PCT/US2002/000347 patent/WO2002053519A2/en active Search and Examination
- 2002-01-08 CN CN02803508A patent/CN100582084C/zh not_active Expired - Fee Related
-
2005
- 2005-01-27 US US11/050,789 patent/US20050176828A1/en not_active Abandoned
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR100682326B1 (ko) * | 2005-01-14 | 2007-02-15 | 주식회사 엔젤금속 | 완충기능을 갖는 도어레버 |
KR100731122B1 (ko) * | 2005-12-28 | 2007-06-22 | 동부일렉트로닉스 주식회사 | 씨모스 이미지 센서 및 그 제조방법 |
Also Published As
Publication number | Publication date |
---|---|
CN100582084C (zh) | 2010-01-20 |
KR100859929B1 (ko) | 2008-09-23 |
JP4253503B2 (ja) | 2009-04-15 |
CA2433807A1 (en) | 2002-07-11 |
EP1373185A4 (en) | 2005-12-07 |
WO2002053519A2 (en) | 2002-07-11 |
US6963010B2 (en) | 2005-11-08 |
US20050176828A1 (en) | 2005-08-11 |
CN1511137A (zh) | 2004-07-07 |
EP1373185A2 (en) | 2004-01-02 |
RU2003124640A (ru) | 2005-02-27 |
US20030187276A1 (en) | 2003-10-02 |
JP2004529082A (ja) | 2004-09-24 |
CA2433807C (en) | 2012-04-24 |
EP1373185B1 (en) | 2017-03-01 |
WO2002053519A3 (en) | 2003-03-13 |
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