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USP14(ubiquitin-specific protease 14) 억제제 및 프로탁(proteolysis-targeting chimera, PROTAC)을 포함하는, 암의 예방 또는 치료용 약학적 조성물
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제1항에 있어서,상기 USP14 억제제는 IU1 계열 화합물인 것을 특징으로 하는, 조성물
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제2항에 있어서,상기 IU1 계열 화합물은 1-[1-(4-fluorophenyl)-2,5-dimethylpyrrol-3-yl]-2-pyrrolidin-1-ylethanone; 1-[1-(4-Chlorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]-2-(1-piperidinyl)ethanone; 1-(1-(4-chlorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl)-2-(pyrrolidin-1-yl)ethan-1-one; 4-(3-(2-(4-hydroxypiperidin-1-yl)acetyl)-2,5-dimethyl-1H-pyrrol-1-yl)benzonitrile; 1-(1-(4-chlorophenyl)-5-methyl-1H-pyrazol-4-yl)-2-(piperidin-1-yl)ethan-1-one; 4-(2-methyl-3-(2-(piperidin-1-yl)acetyl)-1H-pyrrolo[3,2-b]pyridin-1-yl)benzonitrile; 1-(4-cyanophenyl)-2-methyl-3-(2-(piperidin-1-yl)acetyl)-1H-pyrrolo[3,2-b]pyridine-5-carbonitrile; 4-(3-(2-((2R)-2-hydroxy-7-azabicyclo[2
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제1항에 있어서,상기 암은 뇌종양, 두경부암, 유방암, 폐암, 식도암, 위암, 십이지장암, 충수암, 대장암, 직장암, 간암, 췌장암, 담낭암, 담관암, 항문암, 신암, 수뇨관암, 방광암, 전립선암, 음경암, 정소암, 자궁암, 난소암, 외음암, 질암 또는 피부암인 것을 특징으로 하는, 조성물
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제1항에 있어서,상기 프로탁은 CDK9(Cyclin-dependent kinase 9)/CDK family, BRD4(Bromodomain-containing protein 4)/BET(Bromodomain and extra-terminal) family, SHP-2(Src homology region 2 domain-containing phosphatase-2), AR(Androgen receptor), ER(Estrogen receptor), RAR(Retinoic acid receptor), ERRα(Estrogen-related receptor alpha), BTK(Bruton's tyrosine kinase), ALK(Anaplastic lymphoma kinase), RIPK(Receptor-interacting serine/threonine-protein kinase), c-Met(MET proto-oncogene/receptor tyrosine kinase), FAK(Focal adhesion kinase), IRAK4(Interleukin-1 receptor-associated kinase 4), p38 MAPK(p38 mitogen-activated protein kinases), SGK(Serum and glucocorticoid-regulated kinase), TBK1(TANK-binding kinase 1), KRAS(Kirsten rat sarcoma virus protein), B-Raf(B-Raf proto-oncogene serine/threonine kinase), β-catenin, FKBP(FK506 binding protein), IDO(Indoleamine 2,3-dioxygenase), PD-1/PD-L1(Programmed death protein 1/programmed death-ligand 1), PARP1(Poly [ADP-ribose] polymerase 1), PRC2(Polycomb repressive complex 2), EGFR(Epidermal growth factor receptor), Sirt2(NAD-dependent deacetylase sirtuin 2), HER2/ERBB2(Human epidermal growth factor receptor 2), FRS2(Fibroblast growth factor receptor substrate 2), BCL-XL(B-cell lymphoma-extra large), SMARCA(SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A), HDM2(Human double minute 2 homolog), HDAC(Histone deacetylase) family, BCR-ABL(Breakpoint cluster region protein- Tyrosine-protein kinase ABL1), MCL1(Modulator Of VRAC Current 1), FLT-3(Fms Related Receptor Tyrosine Kinase 3), STAT3(Transcription factor STAT3), Myc family 및 BAF complex(Brg/Brahma-associated factors)로 구성되는 군에서 선택되는 단백질을 타겟으로 하는 것을 특징으로 하는, 조성물
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제1항에 있어서,상기 USP14 억제제는 프로탁의 단백질 분해 효과를 증진시키는 것을 특징으로 하는, 조성물
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프로탁과 병용되는 암의 예방 또는 치료 효과 증진용 약학적 조성물로서, 상기 조성물은 USP14 억제제를 유효성분으로 포함하는 것을 특징으로 하는, 약학적 조성물
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제7항에 있어서,상기 USP14 억제제는 IU1 계열 화합물인 것을 특징으로 하는, 조성물
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제7항에 있어서,상기 IU1 계열 화합물은 1-[1-(4-fluorophenyl)-2,5-dimethylpyrrol-3-yl]-2-pyrrolidin-1-ylethanone; 1-[1-(4-Chlorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]-2-(1-piperidinyl)ethanone; 1-(1-(4-chlorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl)-2-(pyrrolidin-1-yl)ethan-1-one; 4-(3-(2-(4-hydroxypiperidin-1-yl)acetyl)-2,5-dimethyl-1H-pyrrol-1-yl)benzonitrile; 1-(1-(4-chlorophenyl)-5-methyl-1H-pyrazol-4-yl)-2-(piperidin-1-yl)ethan-1-one; 4-(2-methyl-3-(2-(piperidin-1-yl)acetyl)-1H-pyrrolo[3,2-b]pyridin-1-yl)benzonitrile; 1-(4-cyanophenyl)-2-methyl-3-(2-(piperidin-1-yl)acetyl)-1H-pyrrolo[3,2-b]pyridine-5-carbonitrile; 4-(3-(2-((2R)-2-hydroxy-7-azabicyclo[2
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제7항에 있어서,상기 암은 뇌종양, 두경부암, 유방암, 폐암, 식도암, 위암, 십이지장암, 충수암, 대장암, 직장암, 간암, 췌장암, 담낭암, 담관암, 항문암, 신암, 수뇨관암, 방광암, 전립선암, 음경암, 정소암, 자궁암, 난소암, 외음암, 질암 또는 피부암인 것을 특징으로 하는, 조성물
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제7항에 있어서,상기 프로탁은 CDK9(Cyclin-dependent kinase 9)/CDK family, BRD4(Bromodomain-containing protein 4)/BET(Bromodomain and extra-terminal) family, SHP-2(Src homology region 2 domain-containing phosphatase-2), AR(Androgen receptor), ER(Estrogen receptor), RAR(Retinoic acid receptor), ERRα(Estrogen-related receptor alpha), BTK(Bruton's tyrosine kinase), ALK(Anaplastic lymphoma kinase), RIPK(Receptor-interacting serine/threonine-protein kinase), c-Met(MET proto-oncogene/receptor tyrosine kinase), FAK(Focal adhesion kinase), IRAK4(Interleukin-1 receptor-associated kinase 4), p38 MAPK(p38 mitogen-activated protein kinases), SGK(Serum and glucocorticoid-regulated kinase), TBK1(TANK-binding kinase 1), KRAS(Kirsten rat sarcoma virus protein), B-Raf(B-Raf proto-oncogene serine/threonine kinase), β-catenin, FKBP(FK506 binding protein), IDO(Indoleamine 2,3-dioxygenase), PD-1/PD-L1(Programmed death protein 1/programmed death-ligand 1), PARP1(Poly [ADP-ribose] polymerase 1), PRC2(Polycomb repressive complex 2), EGFR(Epidermal growth factor receptor), Sirt2(NAD-dependent deacetylase sirtuin 2), HER2/ERBB2(Human epidermal growth factor receptor 2), FRS2(Fibroblast growth factor receptor substrate 2), BCL-XL(B-cell lymphoma-extra large), SMARCA(SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A), HDM2(Human double minute 2 homolog), HDAC(Histone deacetylase) family, BCR-ABL(Breakpoint cluster region protein- Tyrosine-protein kinase ABL1), MCL1(Modulator Of VRAC Current 1), FLT-3(Fms Related Receptor Tyrosine Kinase 3), STAT3(Transcription factor STAT3), Myc family 및 BAF complex(Brg/Brahma-associated factors)로 구성되는 군에서 선택되는 단백질을 타겟으로 하는 것을 특징으로 하는, 조성물
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제7항에 있어서,상기 USP14 억제제는 프로탁의 단백질 분해 효과를 증진시키는 것을 특징으로 하는, 조성물
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제7항에 있어서,상기 병용은 프로탁과 동시에(simultaneous), 별도로(separate) 또는 순차적(sequential)으로 투여되는 것을 특징으로 하는, 조성물
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USP14 억제제 및 프로탁을 포함하는 암의 예방 또는 개선용 건강기능식품
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