KR20160107361A - Dpp-iv 억제제의 용도 - Google Patents
Dpp-iv 억제제의 용도 Download PDFInfo
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- KR20160107361A KR20160107361A KR1020167024324A KR20167024324A KR20160107361A KR 20160107361 A KR20160107361 A KR 20160107361A KR 1020167024324 A KR1020167024324 A KR 1020167024324A KR 20167024324 A KR20167024324 A KR 20167024324A KR 20160107361 A KR20160107361 A KR 20160107361A
- Authority
- KR
- South Korea
- Prior art keywords
- diabetic
- methyl
- dpp
- inhibitor
- diabetes
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
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- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
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Abstract
Description
Claims (19)
- 당뇨병전기, 글루코스 불내성, 병리학적 공복 글루코스, 당뇨발, 당뇨병-관련 궤양, 당뇨병성 고지혈증, 당뇨병성 이상지혈증, 새롭게 진단된 1형 당뇨병, 임신당뇨병, 고혈당증, 식후 아드레날린증후군 및 심부전증으로부터 선택되는 생리 기능장애로 진단되는 환자의 치료용, 또는 이식된 랑게르한스 섬 또는 베타 세포를 갖는 환자의 치료용 약제를 제조하기 위한, 화학식 I 또는 화학식 II의 DPP-IV 억제제 또는 이들의 염들 중 하나의 용도.
화학식 I
화학식 II
상기 화학식 I 및 화학식 II에서,
R1은 ([1,5]나프티리딘-2-일)메틸, (퀴나졸린-2-일)메틸, (퀴녹살린-6-일)메틸, (4-메틸-퀴나졸린-2-일)메틸, 2-시아노-벤질, (3-시아노-퀴놀린-2-일)메틸, (3-시아노-피리딘-2-일)메틸, (4-메틸-피리미딘-2-일)메틸, 또는 (4,6-디메틸-피리미딘-2-일)메틸이고,
R2는 3-(R)-아미노-피페리딘-1-일, (2-아미노-2-메틸-프로필)-메틸아미노 또는 (2-(S)-아미노-프로필)-메틸아미노이다. - 당뇨병전기 또는 발현 2형 당뇨병(manifest type 2 diabetes)으로 진단받은 환자의 치료용 약제를 제조하기 위한, 화학식 I 또는 화학식 II의 DPP-IV 억제제 또는 이들의 염들 중 하나의 용도로서, 당해 약제학적 조성물을 사용함으로써, 치료에도 불구하고 발생하는 글루코스 대사장애, 치료에도 불구하고 발생하는 HbA1c 수치 상승, 치료에도 불구하고 발생하는 공복 글루코스 수치 장애, 인슐린 치료의 필요성, 발현 2형 당뇨병, 당뇨발, 당뇨병-관련 궤양, 당뇨병성 고지혈증, 당뇨병성 이상지혈증 또는 대혈관 합병증의 위험이 감소되는 것을 특징으로 하는, 화학식 I 또는 화학식 II의 DPP-IV 억제제 또는 이들의 염들 중 하나의 용도.
화학식 I
화학식 II
상기 화학식 I 및 화학식 II에서,
R1은 ([1,5]나프티리딘-2-일)메틸, (퀴나졸린-2-일)메틸, (퀴녹살린-6-일)메틸, (4-메틸-퀴나졸린-2-일)메틸, 2-시아노-벤질, (3-시아노-퀴놀린-2-일)메틸, (3-시아노-피리딘-2-일)메틸, (4-메틸-피리미딘-2-일)메틸, 또는 (4,6-디메틸-피리미딘-2-일)메틸이고,
R2는 3-(R)-아미노-피페리딘-1-일, (2-아미노-2-메틸-프로필)-메틸아미노 또는 (2-(S)-아미노-프로필)-메틸아미노이다. - 제2항에 있어서, 대혈관 합병증이 심근 경색, 급성 관상동맥 증후군, 불안정형 협심증, 안정형 협심증, 출혈성 또는 허혈성 뇌졸중, 말초동맥 폐쇄성 질환, 심근병증, 좌심부전증, 우심부전증, 심부전증(global heart failure), 심박장애 및 혈관 재협착 중에서 선택되는 것을 특징으로 하는, 용도.
- 제1항에 있어서, 약제학적 조성물이 당뇨병전기, 글루코스 불내성 또는 병리학적 공복 글루코스로 진단된 환자를 치료하기 위해 사용되는 것을 특징으로 하는, 용도.
- 제1항에 있어서, 약제학적 조성물이 당뇨병성 고지혈증 또는 당뇨병성 이상지혈증으로 진단된 환자를 치료하기 위해 사용되는 것을 특징으로 하는, 용도.
- 제1항에 있어서, 약제학적 조성물이 임신당뇨병을 치료하기 위해 사용되는 것을 특징으로 하는, 용도.
- 제1항에 있어서, 약제학적 조성물이 고혈당증 또는 식후 아드레날린증후군을 치료하기 위해 사용되는 것을 특징으로 하는, 용도.
- 제1항에 있어서, 약제학적 조성물이 심부전증을 치료하기 위해 사용되는 것을 특징으로 하는, 용도.
- 제2항에 있어서, 약제학적 조성물을 사용함으로써, HbA1c 수치의 추가 상승의 위험, 공복 글루코스의 저하의 위험, 및 인슐린 치료의 필요성이 감소되는 것을 특징으로 하는, 용도.
- 화학식 I 또는 화학식 II의 DPP-IV 억제제 또는 이들의 염들 중 하나 이외의 다른 항당뇨병 성분들 중에서 선택된 활성 성분; 혈당 수준을 낮추는 활성 성분; 혈중 지질 수준을 낮추는 활성 성분; 혈중 HDL 수준을 높이는 활성 성분; 혈압을 낮추는 활성 성분; 또는 아테롬성동맥경화증 또는 비만을 치료하는 활성 성분과의 약제 병용물을 제조하기 위한, 화학식 I 또는 화학식 II의 DPP-IV 억제제 또는 이들의 염들 중 하나의 용도.
화학식 I
화학식 II
상기 화학식 I 및 화학식 II에서,
R1은 ([1,5]나프티리딘-2-일)메틸, (퀴나졸린-2-일)메틸, (퀴녹살린-6-일)메틸, (4-메틸-퀴나졸린-2-일)메틸, 2-시아노-벤질, (3-시아노-퀴놀린-2-일)메틸, (3-시아노-피리딘-2-일)메틸, (4-메틸-피리미딘-2-일)메틸, 또는 (4,6-디메틸-피리미딘-2-일)메틸이고,
R2는 3-(R)-아미노-피페리딘-1-일, (2-아미노-2-메틸-프로필)-메틸아미노 또는 (2-(S)-아미노-프로필)-메틸아미노이다. - 제10항에 있어서, DPP-IV 억제제와 다른 항당뇨병 활성 성분 또는 혈압을-낮추는 활성 성분과의 약제 병용물이 제조되는 것을 특징으로 하는, 용도.
- 제10항에 있어서, DPP-IV 억제제와 메트포르민, 미글리톨, 아토르바스타틴, 발사르탄 또는 텔미사르탄과의 약제 병용물이 제조되는 것을 특징으로 하는, 용도.
- 제10항에 있어서, 약제 병용물이 당뇨병전기, 글루코스 불내성, 병리학적 공복 글루코스, 당뇨발, 당뇨병-관련 궤양, 당뇨병성 고지혈증, 당뇨병성 이상지혈증, 새롭게 진단된 1형 당뇨병, 임신당뇨병, 심부전증, 고혈당증 및 식후 아드레날린증후군으로부터 선택되는 생리 기능장애로 진단되는 환자를 치료하기 위해 사용되는 것을 특징으로 하는, 용도.
- 랑게르한스 섬 또는 베타 세포의 분리 또는 저장 매질로서, 세포의 생명력과 분비 용량을 향상시키기 위해 DPP-IV 억제제 1nmol/ℓ 내지 1μmol/ℓ를 함유하는 것을 특징으로 하는, 랑게르한스 섬 또는 베타 세포의 분리 또는 저장 매질.
- 제14항에 있어서, DPP-IV 억제제가 화학식 I 또는 화학식 II의 구조를 갖는 화합물 또는 이들의 염들 중 하나임을 특징으로 하는, 랑게르한스 섬 또는 베타 세포의 분리 또는 저장 매질.
화학식 I
화학식 II
상기 화학식 I 및 화학식 II에서,
R1은 ([1,5]나프티리딘-2-일)메틸, (퀴나졸린-2-일)메틸, (퀴녹살린-6-일)메틸, (4-메틸-퀴나졸린-2-일)메틸, 2-시아노-벤질, (3-시아노-퀴놀린-2-일)메틸, (3-시아노-피리딘-2-일)메틸, (4-메틸-피리미딘-2-일)메틸, 또는 (4,6-디메틸-피리미딘-2-일)메틸이고,
R2는 3-(R)-아미노-피페리딘-1-일, (2-아미노-2-메틸-프로필)-메틸아미노 또는 (2-(S)-아미노-프로필)-메틸아미노이다. - 랑게르한스 섬 또는 베타 세포의 생명력과 분비 용량을 향상시키는 방법으로서, DPP-IV 억제제가 랑게르한스 섬 또는 베타 세포의 분리 및 이식 기(phase) 동안 1nmol/ℓ 내지 1μmol/ℓ의 농도로 분리 및 저장 매질에 첨가됨을 특징으로 하는, 랑게르한스 섬 또는 베타 세포의 생명력과 분비 용량을 향상시키는 방법.
- DPP-IV 억제제로 환자를 치료하는 방법에 있어서, 환자가 당뇨병전기, 글루코스 불내성, 병리학적 공복 글루코스, 당뇨발, 당뇨병-관련 궤양, 당뇨병성 고지혈증, 당뇨병성 이상지혈증, 새롭게 진단된 1형 당뇨병, 임신당뇨병, 심부전증, 고혈당증 및 식후 아드레날린증후군으로부터 선택되는 생리 기능장애로 진단되는 환자, 또는 이식된 랑게르한스 섬 또는 베타 세포를 갖는 환자인 것을 특징으로 하는, DPP-IV 억제제로 환자를 치료하는 방법.
- DPP-IV 억제제로 당뇨병전기 또는 2형 당뇨병 환자를 치료하는 방법에 있어서, 치료에도 불구하고 발생하는 글루코스 대사장애, 치료에도 불구하고 발생하는 HbA1c 수치 상승, 치료에도 불구하고 발생하는 공복 글루코스 대사장애, 인슐린 치료의 필요성, 발현 2형 당뇨병, 당뇨발, 당뇨병-관련 궤양, 당뇨병성 고지혈증, 당뇨병성 이상지혈증 또는 대혈관 합병증의 위험이 상기 치료에 의해 감소되는 것을 특징으로 하는, DPP-IV 억제제로 당뇨병전기 또는 2형 당뇨병 환자를 치료하는 방법.
- DPP-IV 억제제로 환자를 치료하는 방법에 있어서, 환자가 심부전증을 앓는 것을 특징으로 하는, DPP-IV 억제제로 환자를 치료하는 방법.
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