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RU2010148740A - Высокоэффективные конъюгаты и гидрофильные сшивающие агенты (линкеры) - Google Patents

Высокоэффективные конъюгаты и гидрофильные сшивающие агенты (линкеры) Download PDF

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Publication number
RU2010148740A
RU2010148740A RU2010148740/04A RU2010148740A RU2010148740A RU 2010148740 A RU2010148740 A RU 2010148740A RU 2010148740/04 A RU2010148740/04 A RU 2010148740/04A RU 2010148740 A RU2010148740 A RU 2010148740A RU 2010148740 A RU2010148740 A RU 2010148740A
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RU
Russia
Prior art keywords
bond
cell
binds
agent
antibody
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RU2010148740/04A
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English (en)
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RU2487877C2 (ru
Inventor
Раджиева СИНГХ (US)
Раджиева Сингх
Елена КОВТУН (US)
Елена Ковтун
Шарон Д. ВИЛЬХЕЛЬМ (US)
Шарон Д. ВИЛЬХЕЛЬМ
Рави В. Дж. ЧАРИ (US)
Рави В. Дж. Чари
Original Assignee
Иммьюноджен, Инк. (Us)
Иммьюноджен, Инк.
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Publication of RU2010148740A publication Critical patent/RU2010148740A/ru
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Publication of RU2487877C2 publication Critical patent/RU2487877C2/ru

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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/537—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
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Abstract

1. Соединение формулы (1) или (1'): ! ! ! где: ! Z представляет собой реакционноспособную функциональную группу, которая может образовывать амидную или тиоэфирную связь с агентом, связывающимся с клеткой; ! D представляет собой лекарственное средство; ! Х представляет собой алифатическую, ароматическую или гетероциклическую структурную единицу, присоединенную к агенту, связывающемуся с клеткой через тиоэфирную связь, амидную связь, карбаматную связь или простую эфирную связь; ! Y представляет собой алифатическую, ароматическую или гетероциклическую структурную единицу, присоединенную к лекарственному средству через ковалентную связь, которую выбирают из группы, состоящей из тиоэфирной связи, амидной связи, карбаматной связи, простой эфирной связи, аминной связь, углерод-углеродной связи и гидразоновой связи; ! l представляет собой 0 или 1; ! р представляет собой 0 или 1; и ! n представляет собой целое число от 1 до 2000. ! 2. Конъюгат агента, связывающегося с клеткой, и цитотоксического лекарственного средства формулы (2) или (2'): ! ! ! где: ! СВ представляет собой агент, связывающийся с клеткой; ! D представляет собой лекарственное средство; ! Х представляет собой алифатическую, ароматическую или гетероциклическую структурную единицу, присоединенную к агенту, связывающемуся с клеткой через тиоэфирную связь, амидную связь, карбаматную связь или простую эфирную связь; ! Y представляет собой алифатическую, ароматическую или гетероциклическую структурную единицу, присоединенную к лекарственному средству через ковалентную связь, которую выбирают из группы, состоящей из тиоэфирной связи, амидной связи, карбаматной св

Claims (17)

1. Соединение формулы (1) или (1'):
Figure 00000001
Figure 00000002
где:
Z представляет собой реакционноспособную функциональную группу, которая может образовывать амидную или тиоэфирную связь с агентом, связывающимся с клеткой;
D представляет собой лекарственное средство;
Х представляет собой алифатическую, ароматическую или гетероциклическую структурную единицу, присоединенную к агенту, связывающемуся с клеткой через тиоэфирную связь, амидную связь, карбаматную связь или простую эфирную связь;
Y представляет собой алифатическую, ароматическую или гетероциклическую структурную единицу, присоединенную к лекарственному средству через ковалентную связь, которую выбирают из группы, состоящей из тиоэфирной связи, амидной связи, карбаматной связи, простой эфирной связи, аминной связь, углерод-углеродной связи и гидразоновой связи;
l представляет собой 0 или 1;
р представляет собой 0 или 1; и
n представляет собой целое число от 1 до 2000.
2. Конъюгат агента, связывающегося с клеткой, и цитотоксического лекарственного средства формулы (2) или (2'):
Figure 00000003
Figure 00000004
где:
СВ представляет собой агент, связывающийся с клеткой;
D представляет собой лекарственное средство;
Х представляет собой алифатическую, ароматическую или гетероциклическую структурную единицу, присоединенную к агенту, связывающемуся с клеткой через тиоэфирную связь, амидную связь, карбаматную связь или простую эфирную связь;
Y представляет собой алифатическую, ароматическую или гетероциклическую структурную единицу, присоединенную к лекарственному средству через ковалентную связь, которую выбирают из группы, состоящей из тиоэфирной связи, амидной связи, карбаматной связи, простой эфирной связи, аминной связь, углерод-углеродной связи и гидразоновой связи;
l представляет собой 0 или 1;
р представляет собой 0 или 1; и
m представляет собой целое число от 2 до 15; и
n представляет собой целое число от 1 до 2000.
3. Соединение формулы (3) или (3'):
Figure 00000005
Figure 00000006
в которой:
Z представляет собой реакционноспособную функциональную группу, которая может образовывать амидную или тиоэфирную связь с агентом, связывающимся с клеткой; D представляет собой лекарственное средство;
Х представляет собой алифатическую, ароматическую или гетероциклическую структурную единицу, присоединенную к агенту, связывающемуся с клеткой, через тиоэфирную связь, амидную связь, карбаматную связь или простую эфирную связь;
Y представляет собой алифатическую, неароматическую гетероциклическую или ароматическую гетероциклическую структурную единицу, присоединенную к лекарственному средству через дисульфидную связь;
l представляет собой 0 или 1; и
n представляет собой целое число от 1 до 14.
4. Конъюгат агента, связывающегося с клеткой, и цитотоксического лекарственного средства формулы (4) или (4'):
Figure 00000007
Figure 00000008
в которой:
СВ представляет собой агент, связывающийся с клеткой;
D представляет собой лекарственное средство;
Х представляет собой алифатическую, ароматическую или гетероциклическую структурную единицу, присоединенную к агенту, связывающемуся с клеткой через тиоэфирную связь, амидную связь, карбаматную связь или простую эфирную связь;
Y представляет собой алифатическую, ароматическую или гетероциклическую структурную единицу, присоединенную к лекарственному средству через дисульфидную связь;
l представляет собой 0 или 1; и
m представляет собой целое число от 3 до 8; и
n представляет собой целое число от 1 до 14.
5. Конъюгат по п.2 или 4, в котором указанный агент, связывающийся с клеткой, представляет собой антитело, одноцепочечное антитело, фрагмент антитела, который предпочтительно связывается с клеткой-мишенью, моноклональное антитело, одноцепочечное моноклональное антитело, моноклональное антитело, биспецифическое антитело, фрагмент, который специфически связывается с клеткой-мишенью, аднектины, имитирующие действие антител, белки DARPin, лимфокин, цитокин, гормон, фактор роста, фермент или молекулу, транспортирующую питательные вещества.
6. Конъюгат по п.2 или 4, в котором указанный агент, связывающийся с клеткой, представляет собой моноклональное антитело с измененной поверхностью, одноцепочечное моноклональное антитело с измененной поверхностью или фрагмент моноклонального антитела с измененной поверхностью, который предпочтительно связывается с клеткой-мишенью.
7. Конъюгат по п.2 или 4, в котором указанный агент, связывающийся, с клеткой, представляет собой гуманизированное моноклональное антитело, гуманизированное одноцепочечное моноклональное антитело, или фрагмент гуманизированного моноклонального антитела, который предпочтительно связывается с клеткой-мишенью.
8. Конъюгат по п.5, в котором указанное антитело представляет собой химерное антитело, фрагмент химерного антитела, домен этого антитела или фрагмент домена этого антитела.
9. Конъюгат по п.5, в котором указанное антитело представляет собой MY9, анти-В4, ЕрСАМ, CD2, CD3, CD4, CD5, CD6, CD11, CD19, CD20, CD22, CD26, CD30, CD33, CD37, CD3 8, CD40, CD44, CD56, CD79, CD 105, CD 13 8, рецепторы EphA, рецепторы EphB, EGFR, EGFRvIII, HER2, HER3, мезотелин, белок Cripto, интегрин альфаvбета3, альфаvбета5, альфаvбета6 или С242.
10. Конъюгат по п.5, в котором указанное антитело представляет собой гуманизированное, человеческое антитело или антитело с измененной поверхностью, которое выбирают из Му9-6, В4, С242, N901, DS6, рецептора EphA2, CD38, IGF-IR, CNTO 95, В-В4, трастузумаба, пертузумаба, биватузумаба, сибротузумаба или ритуксимаба.
11. Конъюгат по п.2 или 4, в котором указанный агент, связывающийся с клеткой, связывается с клеткой-мишенью, которую выбирают из опухолевых клеток; клеток, инфицированных вирусом, клеток, инфицированных микроорганизмами, клеток, инфицированных паразитами, аутоиммунных клеток, активированных клеток, миелоидных клеток, активированных Т-клеток, В-клеток или меланоцитов; клеток, экспрессирующих один или несколько из следующего: IGF-IR, CanAg, EGFR, MUC1, MUC16, VEGF, TF, MY9, анти-В4, EpCAM, CD2, CD3, CD4, CDS, CD6, CD11, CD11a, CD18, CD19, CD20, CD22, CD26, CD30. CD33, CD37, CD38, CD40, CD44, CD56, CD70, CD79, CD 105, CD 138, рецепторы EphA, рецепторы EphB, EGFRvIII, HER2/neu, HER3, мезотелин, белок Cripto, интегрин альфаvбета3, интегрин альфаvбета5, интегрин альфаvбетаβ, Аро2 и антигены С242; или клетки, экспрессирующие рецептор инсулиноподобного фактора роста, рецептор эпидермального фактора роста и рецептор фолата.
12. Конъюгат по п.11, в котором опухолевые клетки представляют собой клетки, которые выбирают из клеток рака молочной железы, из клеток рака предстательной железы, из клеток рака яичников, из клеток колоректального рака, из клеток рака желудка, из клеток плоскоклеточного рака, из клеток мелкоклеточного рака легкого и из клеток рака яичек.
13. Фармацевтическая композиция, содержащая эффективное количество конъюгата лекарственное средство-агент, связывающийся с клеткой, по п.2 или 4, фармацевтически приемлемую соль или ее сольват, и фармацевтически приемлемую основу, разбавитель или эксипиент.
14. Способ лечения заболевания, чувствительного к лечению указанным способом, указанный способ, включающий парентеральное введение нуждающемуся в этом пациенту эффективной дозы конъюгата по п.2 или 4.
15. Способ по п.14, в котором указанное заболевание выбирают из опухолей, аутоиммунных заболеваний, отторжений трансплантатов, реакции трансплантата против хозяина, вирусных инфекций и паразитарных инфекций.
16. Способ по п.15, в котором указанную опухоль выбирают из одного или нескольких раков легкого, крови, плазмы, молочной железы, толстой кишки, предстательной железы, почек, поджелудочной железы, мозга, костей, яичников, семенников и органов лимфатической системы.
17. Способ по п.15, в котором указанная опухоль экспрессирует одно или несколько из следующего: IGF-IR, FOLR1, CanAg, EGFR, EphA2, MUC1, MUC16, VEGF, TF, MY9, анти-В4, EpCAM, CD2, CDS, CD4, CD5, CD6, CD11, CD11a, CD18, CD19, CD20, CD22, CD26, CD30, CD33, CD37, CD38, CD40, CD44, CD56, CD70, CD79, CD105, CD138, EphA, EphB, EGFRvIII, HER2/neu, HER3, мезотелин, белок Cripto, интегрин альфаvбета3, интегрин альфаvбета5, интегрин альфаvбета6, Аро2 и антигены С242.
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AU2009243009A1 (en) 2009-11-05
RU2487877C2 (ru) 2013-07-20
US20100129314A1 (en) 2010-05-27
MX2010011808A (es) 2011-03-04
AU2009243009B2 (en) 2014-09-11
CN102083461B (zh) 2014-09-17
WO2009134952A2 (en) 2009-11-05
WO2009134952A3 (en) 2010-01-07
WO2009134976A1 (en) 2009-11-05
EP2276506A4 (en) 2014-05-07
IL208937A0 (en) 2011-01-31
CA2722109A1 (en) 2009-11-05
US9150649B2 (en) 2015-10-06
US20160114052A1 (en) 2016-04-28
KR20100137585A (ko) 2010-12-30
EP2276506A1 (en) 2011-01-26

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