RU2019120401A - Композиции для модулирования сигнальной трансдукции pd-1 - Google Patents
Композиции для модулирования сигнальной трансдукции pd-1 Download PDFInfo
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- RU2019120401A RU2019120401A RU2019120401A RU2019120401A RU2019120401A RU 2019120401 A RU2019120401 A RU 2019120401A RU 2019120401 A RU2019120401 A RU 2019120401A RU 2019120401 A RU2019120401 A RU 2019120401A RU 2019120401 A RU2019120401 A RU 2019120401A
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- 230000019491 signal transduction Effects 0.000 title claims 2
- 239000000203 mixture Substances 0.000 title 1
- 102100040678 Programmed cell death protein 1 Human genes 0.000 claims 10
- 101710089372 Programmed cell death protein 1 Proteins 0.000 claims 10
- 238000000034 method Methods 0.000 claims 8
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- ITFBYYCNYVFPKD-FMIDTUQUSA-N (4ar,6ar,6as,6br,8as,12as,14bs)-8a-(imidazole-1-carbonyl)-4,4,6a,6b,11,11,14b-heptamethyl-3,13-dioxo-4a,5,6,6a,7,8,9,10,12,12a-decahydropicene-2-carbonitrile Chemical compound O=C([C@]12CCC(C[C@H]1[C@@H]1[C@@]([C@@]3(CC[C@H]4C(C)(C)C(=O)C(C#N)=C[C@]4(C)C3=CC1=O)C)(C)CC2)(C)C)N1C=CN=C1 ITFBYYCNYVFPKD-FMIDTUQUSA-N 0.000 claims 1
- AKHFOJODMTWXAB-UHFFFAOYSA-N 1,2-bis[4-propan-2-yl-6-(trifluoromethyl)pyrimidin-2-yl]hydrazine Chemical compound CC(C)C1=CC(C(F)(F)F)=NC(NNC=2N=C(C=C(N=2)C(C)C)C(F)(F)F)=N1 AKHFOJODMTWXAB-UHFFFAOYSA-N 0.000 claims 1
- CNRPDCKHCGUKDK-UHFFFAOYSA-N 1,8-bis(phenylsulfanyl)anthracene-9,10-dione Chemical compound C=12C(=O)C3=C(SC=4C=CC=CC=4)C=CC=C3C(=O)C2=CC=CC=1SC1=CC=CC=C1 CNRPDCKHCGUKDK-UHFFFAOYSA-N 0.000 claims 1
- YIOOFDZGTGOZSB-UHFFFAOYSA-N 1-(2-chlorophenyl)-3-[4-[4-[(2-chlorophenyl)carbamoylamino]phenoxy]phenyl]urea Chemical compound ClC1=CC=CC=C1NC(=O)NC(C=C1)=CC=C1OC(C=C1)=CC=C1NC(=O)NC1=CC=CC=C1Cl YIOOFDZGTGOZSB-UHFFFAOYSA-N 0.000 claims 1
- ZRQAKHIGSFKUOK-UHFFFAOYSA-N 1-(benzotriazol-1-yl)anthracene-9,10-dione Chemical compound N1=NC2=CC=CC=C2N1C1=CC=CC2=C1C(=O)C1=CC=CC=C1C2=O ZRQAKHIGSFKUOK-UHFFFAOYSA-N 0.000 claims 1
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- MWPPELUBOBZLKD-UHFFFAOYSA-N 2-[2-[(6-oxo-5h-phenanthridin-3-yl)carbamoyl]phenyl]benzoic acid Chemical compound OC(=O)C1=CC=CC=C1C1=CC=CC=C1C(=O)NC1=CC=C2C3=CC=CC=C3C(=O)NC2=C1 MWPPELUBOBZLKD-UHFFFAOYSA-N 0.000 claims 1
- RUQGZBWIPGWOJG-UHFFFAOYSA-N 2-[2-[(6-oxobenzo[c]chromen-2-yl)carbamoyl]phenyl]benzoic acid Chemical compound OC(=O)C1=CC=CC=C1C1=CC=CC=C1C(=O)NC1=CC=C(OC(=O)C=2C3=CC=CC=2)C3=C1 RUQGZBWIPGWOJG-UHFFFAOYSA-N 0.000 claims 1
- IQZIRNIZQHVBMB-UHFFFAOYSA-N 2-[4-[4-(2-carboxyanilino)-3-methoxyphenyl]-2-methoxyanilino]benzoic acid Chemical compound COC1=CC(C=2C=C(OC)C(NC=3C(=CC=CC=3)C(O)=O)=CC=2)=CC=C1NC1=CC=CC=C1C(O)=O IQZIRNIZQHVBMB-UHFFFAOYSA-N 0.000 claims 1
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Claims (11)
1. Фармацевтическая композиция, содержащая эффективное количество одного или более соединений, модулирующих PD-1, выбранных из группы, состоящей из 1-(1H-бензо[d][1,2,3]триазол-1-ил)антрацен-9,10-диона; 1,1'-(оксибис(4,1-фенилен))бис(3-(2-хлорфенил)мочевины); 5,5'-дифенил-2,2',3,3'-тетрагидро-2,2'-бибензо[d]оксазола; 2-(изохинолин-1-ил)-5-фенил-4-(п-толил)оксазола; 2'-((6-оксо-5,6-дигидрофенантридин-3-ил)карбамоил)-[1,1'-бифенил]-2-карбоновой кислоты; 2'-((6-оксо-6H-бензо[c]хромен-2-ил)карбамоил)-[1,1'-бифенил]-2-карбоновой кислоты; 3-(4-хлор-6-фенокси-1,3,5-триазин-2-ил)-1-фенил-1H-индола; 1,8-бис(фенилтио)антрацен-9,10-диона; 4-хлор-2-(3-(фенилтио)фенил)хинолин-6-сульфонилфторида; бис(2,2,4-триметил-1,2-дигидрохинолин-6-ил)метана; 2-нитро-4-((6-нитрохинолин-4-ил)амино)-N-(4-(пиридин-4-иламино)фенил)бензамида; 1,2-бис(4-изопропил-6-(трифторметил)пиримидин-2-ил)гидразина; 3-(бензилтио)фенантро[9,10-e][1,2,4]триазина; (4aR,6aS,6bR,8aS,12aS,12bR,14bS)-8a-(1H-имидазол-1-карбонил)-4,4,6a,6b,11,11,14b-гептаметил-3,13-диоксо-3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,13,14b-октадекагидропицен-2-карбонитрила (CDDO-Im); 2-(1H-фенантро[9,10-d]имидазол-2-ил)фенола; 3-(4,5-диметилбензо[h][1,6]нафтиридин-2-ил)-2-метилхинолин-4-амина; N-(4-бромнафталин-1-ил)-1-гидрокси-2-нафтамида; N-(3-(пиридин-2-ил)изохинолин-1-ил)пиколинимидамида; 2-(изохинолин-1-ил)-4,5-дифенилоксазола; 2,2'-((3,3'-диметокси-[1,1'-бифенил]-4,4'-диил)бис(азандиил))дибензойной кислоты; или их энантиомера, сольвата, фармацевтически приемлемой соли или производного в количестве, эффективном для модулирования сигнальной трансдукции через рецептор PD-1 при введении субъекту, нуждающемуся в этом.
2. Фармацевтическая композиция по п. 1, отличающаяся тем, что одно или более соединений, модулирующих PD-1, связываются с PD-1 в физиологических условиях и ускоряют или индуцируют активирующий сигнал через PD-1, который активирует T-клетку, экспрессирующую PD-1.
3. Фармацевтическая композиция по п. 1 или 2, отличающаяся тем, что одно или более соединений, модулирующих PD-1, связываются с PD-1 в физиологических условиях и ингибируют, снижают или предотвращают связывание лигандов PD-1 с PD-1 и тем самым ингибируют, снижают или предотвращают передачу отрицательного сигнала через рецептор PD-1.
4. Способ индуцирования или ускорения активации T-клетки у субъекта, нуждающегося в этом, включающий введение указанному субъекту одного или более соединений по п. 1 в количестве, эффективном для увеличения антиген-специфической пролиферации T-клеток, увеличения или усиления выработки цитокинов T-клетками, стимуляции дифференцировки и эффекторных функций T-клеток и/или улучшения выживания T-клеток, или преодоления исчерпания и/или анергии T-клеток.
5. Способ индуцирования или ускорения иммунного ответа у субъекта, нуждающегося в этом, включающий введение субъекту эффективного количества одного или более соединений по п. 1 для индуцирования или ускорения активации T-клеток.
6. Способ лечения рака, включающий введение субъекту эффективного количества одного или более соединений по п. 1 для индуцирования или ускорения активации T-клеток.
7. Способ по п. 6, отличающийся тем, что рак выбран из группы, состоящей из рака мочевого пузыря, головного мозга, молочной железы, шейки матки, толстой и прямой кишок, пищевода, почки, печени, легкого, носоглотки, поджелудочной железы, предстательной железы, кожи, желудка, матки, яичника, яичек, гематологического рака, меланомы, рака почек, миеломы, рака щитовидной железы, лимфомы, лейкоза или метастатического рака.
8. Способ лечения инфекции у субъекта, нуждающегося в этом, включающий введение субъекту эффективного количества одного или более соединений по п. 1 для ускорения или индуцирования активации T-клеток у субъекта.
9. Способ по п. 8, отличающийся тем, что инфекция представляет собой микробную инфекцию.
10. Способ по п. 9, отличающийся тем, что инфекция представляет собой бактериальную, грибковую или вирусную инфекцию.
11. Способ по п. 8, отличающийся тем, что инфекция является паразитарной.
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US201662429126P | 2016-12-02 | 2016-12-02 | |
US62/429,126 | 2016-12-02 | ||
PCT/IB2017/057586 WO2018100556A1 (en) | 2016-12-02 | 2017-12-01 | Compositions for modulating pd-1 signal transduction |
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RU2022116451A Division RU2022116451A (ru) | 2016-12-02 | 2017-12-01 | Композиции для модулирования сигнальной трансдукции pd-1 |
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RU2019120401A true RU2019120401A (ru) | 2021-01-14 |
RU2019120401A3 RU2019120401A3 (ru) | 2021-03-25 |
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AU2017370002A1 (en) | 2019-07-04 |
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