RU2016151190A - Соединения, включающие саморасщепляющуюся группу - Google Patents
Соединения, включающие саморасщепляющуюся группу Download PDFInfo
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- RU2016151190A RU2016151190A RU2016151190A RU2016151190A RU2016151190A RU 2016151190 A RU2016151190 A RU 2016151190A RU 2016151190 A RU2016151190 A RU 2016151190A RU 2016151190 A RU2016151190 A RU 2016151190A RU 2016151190 A RU2016151190 A RU 2016151190A
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- 150000001875 compounds Chemical class 0.000 title claims 30
- 235000018102 proteins Nutrition 0.000 claims 12
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- 108090000623 proteins and genes Proteins 0.000 claims 12
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- 229910052739 hydrogen Inorganic materials 0.000 claims 10
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- 125000002947 alkylene group Chemical group 0.000 claims 9
- 125000005647 linker group Chemical group 0.000 claims 8
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- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
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- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 1
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Classifications
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Claims (92)
1. Соединение, включающее саморасщепляющуюся группу, представленную следующей химической формулой 1:
[Химическая формула 1]
G представляет собой группу глюкуроновой кислоты или ее производное;
A представляет собой (C1-C20)гидрокарбил, биоматериал или модифицированный биоматериал;
B представляет собой (C1-C100)гидрокарбил;
W представляет собой электроноакцепторную группу;
Z представляет собой водород, (C1-C8)алкил, галоген, циано или нитро;
n представляет собой целое число от 1 до 3, и, когда n представляет собой целое число 2 или более, каждый из заместителей Z являются одинаковыми или отличными друг от друга;
L представляет собой линкер, связывающий A и W саморасщепляющейся группы при помощи ковалентных связей; и
R1 и R2, каждый независимо, представляют собой водород, (C1-C8)алкил или (C3-C8)циклоалкил.
2. Соединение по п. 1, где G представляет собой
R3 представляет собой водород или защитную группу карбоксила, и R4(s), каждый независимо, представляют собой водород или защитную группу гидроксила.
3. Соединение по п. 1, где W представляет собой -C(O)-, -C(O)NRʹ-, -C(O)O-, -SO2NRʹ-, -P(O)RʹʹNRʹ-, -SONRʹ- или -PO2NRʹ-, и Rʹ и Rʺ, каждый независимо, представляют собой водород, (C1-C8)алкил, (C3-C8)циклоалкил, (C1-C8)алкокси, (C1-C8)алкилтио, моно- или ди-(C1-C8)алкиламино, (C3-C20)гетероарил или (C6-C20)арил.
4. Соединение по п. 1, где линкер L представляет собой алкилен, содержащий от 1 до 50 атомов углерода, и удовлетворяет по меньшей мере одному из следующих условий (i) - (iv):
(i) алкилен включает по меньшей мере одну ненасыщенную связь,
(ii) алкилен включает по меньшей мере один гетероарилен,
(iii) атом углерода алкилена замещен одним или несколькими гетероатомами, выбранными из азота (N), кислорода (О) и серы (S), и
(iv) алкилен дополнительно замещен одним или несколькими алкилами, содержащими от 1 до 20 атомов углерода.
5. Соединение по п. 1, где линкер L включает по меньшей мере одно звено, представляющее собой изопрениловое производное, представленное следующей химической формулой A, которое распознается изопреноид-трансферазой.
[Химическая формула A]
6. Соединение по п. 5, где линкер L дополнительно включает связывающее звено, образованное в результате реакций 1,3-диполярного циклоприсоединения, гетеро-реакций Дильса-Альдера, реакций нуклеофильного замещения, реакций карбонильных соединений не-альдольного типа, присоединений по месту кратных связей углерод-углерод, реакций окисления или клик-реакций.
7. Соединение по п. 6, где связывающее звено образовано путем реакции между ацетиленом и азидом или реакции между группой альдегида или кетона и гидразином или гидроксиламином.
8. Соединение по п. 7, где связывающее звено представлено следующей химической формулой B, C, D или E:
[Химическая формула B]
[Химическая формула C]
[Химическая формула D]
[Химическая формула E]
L1 представляет собой простую связь или алкилен, содержащий от 1 до 30 атомов углерода;
R11 представляет собой водород или алкил, содержащий от 1 до 10 атомов углерода; и
L2 представляет собой алкилен, содержащий от 1 до 30 атомов углерода.
9. Соединение по п. 6, где линкер L дополнительно включает соединительное звено, представленное следующей химической формулой F или G:
[Химическая формула F]
-(CH2)r(V(CH2)p)q-
[Химическая формула G]
-(CH2CH2X)w-
V представляет собой простую связь, -O-, -S-, -NR21-, -C(O)NR22-, -NR23C(O)-, -NR24SO2- или -SO2NR25-;
X представляет собой -O-, (C1-C8)алкилен или -NR21-;
R21 - R25, каждый независимо, представляют собой водород, (C1-C6)алкил, (C1-C6)алкил(C6-C20)арил или (C1-C6)алкил(C3-C20)гетероарил;
r представляет собой целое число от 1 до 10;
p представляет собой целое число от 0 до 10;
q представляет собой целое число от 1 до 10; и
w представляет собой целое число от 1 до 10.
10. Соединение по п. 1, где, когда A представляет собой гидрокарбил, содержащий от 1 до 20 атомов углерода, L представляет собой 
, 
или 
, V представляет собой простую связь, -O-, -S-, -NR21-, -C(O)NR22-, -NR23C(O)-, -NR24SO2- или -SO2NR25-, R21 - R25, каждый независимо, представляют собой водород, (C1-C6)алкил, (C1-C6)алкил(C6-C20)арил или (C1-C6)алкил(C3-C20)гетероарил, r представляет собой целое число от 1 до 10, p представляет собой целое число от 0 до 10, q представляет собой целое число от 1 до 10, и L1 представляет собой простую связь.
11. Соединение по п. 1, где биоматериал представляет собой белок.
12. Соединение по п. 11, где белок представляет собой олигопептид, полипептид, антитело, фрагмент антигенного полипептида или repebody.
13. Соединение по п. 12, где белок содержит аминокислотный мотив, который должен распознаваться изопреноид-трансферазой.
14. Соединение по п. 13, где белок дополнительно включает спейсерное звено, состоящее из аминокислоты, олигопептида или полипептида, между белком и аминокислотным мотивом.
15. Соединение по п. 13 или 14, где белок ковалентно связан с линкером L через аминокислотный мотив.
16. Соединение по п. 15, где аминокислотный мотив ковалентно связан с C-концом белка или ковалентно связан с по меньшей мере одним спейсерным звеном, ковалентно связанным с C-концом белка.
17. Соединение по п. 16, где C-конец белка представляет собой C-конец легкой цепи или тяжелой цепи антитела.
18. Соединение по п. 13, где изопреноид-трансфераза представляет собой фарнезилпротеинтрансферазу (FTаза) или геранилгеранилтрансферазу (GGTаза).
19. Соединение по п. 12, где антитело выбрано из группы, состоящей из интактных поликлональных антител, интактных моноклональных антител, фрагментов антител, одноцепочечных Fv-мутантов (scFv), мультиспецифичных антител, биспецифичных антител, химерных антител, гуманизированных антител, человеческих антител, гибридных белков, включающих антиген-определяющую часть антитела, и других модифицированных молекул иммуноглобулинов, включающих сайт распознавания антигена.
20. Соединение по п. 19, где антитело выбрано из группы, состоящей из муромонаба-CD3, абциксимаба, ритуксимаба, даклизумаба, паливизумаба, инфликсимаба, трастузумаба, этанерцепта, базиликсимаба, гемтузумаба озогамицина, алемтузумаба, ибритутомаба тиуксетана, адалимумаба, алефацепта, омализумаба, эфализумаба, тозитумомаба-I131, цетуксимаба, бевацизумаба, натализумаба, ранибизумаба, панитумумаба, экулизумаба, рилонацепта, цертолизумаба пегола, ромиплостима, AMG-531, CNTO-148, CNTO-1275, ABT-874, LEA-29Y, белимумаба, TACI-Ig, анти-CD20 второго поколения, ACZ-885, тоцилизумаба, атлизумаба, меполизумаба, пертузумаба, HuMax CD20, тремелимумаба (CP-675 206), тицилимумаба, MDX-010, IDEC-114, инотузумаба озогамицина, HuMax EGFR, афлиберцепта, VEGF Trap-Eye, HuMax-CD4, Ala-Ala, ChAglyCD3, TRX4, катумаксомаба, IGN101, MT-201, преговомаба, CH-14,18, WX-G250, AMG-162, AAB-001, мотавизумаба, MEDI-524, эфунгумаба, Aurograb®, раксибацумаба, анти-CD20 третьего поколения, LY2469298 и велтузумаба.
21. Соединение по п. 19, где белок представляет собой моноклональное антитело.
22. Соединение по п. 13 или 14, где аминокислотный мотив представляет собой CYYX, XXCC, XCXC или CXX, где C представляет собой цистеин, Y представляет собой алифатическую аминокислоту, и X представляет собой аминокислоту, которая определяет субстрат-специфичность изопреноид-трансферазы.
23. Соединение по п. 1, где B представляет собой активное вещество.
24. Соединение по п. 23, где активное вещество представляет собой лекарственное средство, токсин, аффинный лиганд, детекторный зонд или их комбинацию.
25. Соединение по п. 23, где активное вещество представляет собой иммуномодулирующее соединение, противораковое средство, противовирусное средство, антибактериальное средство, противогрибковое средство, противопаразитарное средство или их комбинацию.
26. Соединение по п. 22, где белок, содержащий аминокислотный мотив, выбран из группы, состоящей из A-HC-(G)zCVIM, A-HC-(G)zCVLL, A-LC-(G)zCVIM и A-LC-(G)zCVLL, где A представляет собой антитело, HC представляет собой тяжелую цепь, LC представляет собой легкую цепь, G представляет собой глициновое звено, и z представляет собой целое число от 0 до 20.
27. Соединение по п. 26, где оно выбрано из соединений, имеющих следующие структуры:
где
Z представляет собой водород, (C1-C8)алкил, галоген, циано или нитро;
X представляет собой -O-, (C1-C8)алкилен или -NR21-;
R21 представляет собой водород, (C1-C6)алкил, (C1-C6)алкил(C6-C20)арил или (C1-C6)алкил(C3-C20)гетероарил;
n представляет собой целое число от 1 до 3, и, когда n представляет собой целое число 2 или более, каждый из заместителей Z являются одинаковыми или отличными друг от друга;
r представляет собой целое число от 1 до 10;
q представляет собой целое число от 1 до 10;
w представляет собой целое число от 1 до 10;
x представляет собой целое число от 0 до 10;
g представляет собой целое число от 1 до 10;
-S-mAb представляет собой A-HC-(G)zCVIM-, A-HC-(G)zCVLL-, A-LC-(G)zCVIM- или A-LC-(G)zCVLL-, где A представляет собой антитело, HC представляет собой тяжелую цепь, LC представляет собой легкую цепь, G представляет собой глициновое звено, и z представляет собой целое число от 0 до 20;
B представляет собой лекарственное средство, имеющее структуру, выбранную из следующих структур; и
y представляет собой целое число от 1 до 10.
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| KR20140064360 | 2014-05-28 | ||
| KR10-2014-0064360 | 2014-05-28 | ||
| KR1020150073161A KR101628872B1 (ko) | 2014-05-28 | 2015-05-26 | 자가-희생 기를 포함하는 화합물 |
| KR10-2015-0073161 | 2015-05-26 | ||
| PCT/KR2015/005299 WO2015182984A1 (ko) | 2014-05-28 | 2015-05-27 | 자가-희생 기를 포함하는 화합물 |
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| JP (2) | JP6815201B2 (ru) |
| KR (1) | KR101628872B1 (ru) |
| CN (2) | CN105358579B (ru) |
| AU (2) | AU2015268300B2 (ru) |
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| CA (1) | CA2949943A1 (ru) |
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| MX (1) | MX2016015511A (ru) |
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| RU (2) | RU2020101906A (ru) |
| WO (1) | WO2015182984A1 (ru) |
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