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RU2018145296A - Простое эфирное производное никотинилового спирта, получение и фармацевтическая композиция и применения - Google Patents

Простое эфирное производное никотинилового спирта, получение и фармацевтическая композиция и применения Download PDF

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RU2018145296A
RU2018145296A RU2018145296A RU2018145296A RU2018145296A RU 2018145296 A RU2018145296 A RU 2018145296A RU 2018145296 A RU2018145296 A RU 2018145296A RU 2018145296 A RU2018145296 A RU 2018145296A RU 2018145296 A RU2018145296 A RU 2018145296A
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pyridin
bromo
phenylbenzyloxy
chloro
ylmethyleneoxy
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RU2018145296A
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RU2018145296A3 (ru
RU2735541C2 (ru
Inventor
Чжицян ФЫН
Сяогуан Чэнь
Ян Ян
И Чжэн
Фанфан ЛАЙ
Мин ЦЗИ
Чуань ЧЖОУ
Лицзин ЧЖАН
Кэ Ван
Нина СЮЭ
Лин Ли
Original Assignee
Инститьют Оф Материя Медика, Чайниз Экедеми Оф Медикал Сайенсез
Тяньцзинь Чейз Сан Фармасьютикал Ко., Лтд
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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Claims (92)

1. Простое эфирное производное никотинилового спирта формулы (I):
Figure 00000001
или его стереоизомер или фармацевтически приемлемая соль,
где:
R1 выбран из
Figure 00000002
и
Figure 00000003
;
R3 выбран из замещенного C1-C8 насыщенного алкиламино, замещенного C2-C6 ненасыщенного алкиламино, замещенного N-содержащего C2-C6 гетероцикл-1-ила, где каждый является моно-, ди-, три- или тетразамещенным заместителем(ми), выбранным из атома водорода, фтора, хлора, брома, йода, гидрокси, C1-C5 алкила, C1-C5 алкокси, амино, C1-C6 алкиламино, ацетиламино, циано, уреидо (-NH(C=O)NH2), гуанидино (-NH(C=NH)NH2), уреидоамино (-NH-NH(C=O)NH2), гуанидиноамино (-NH-NH(C=NH)NH2), сульфониламино (-NHSO3H), сульфамоила (-SO2NH2), метансульфониламино (-NH-SO2CH3), гидроксиформила (-COOH), C1-C8 алкоксилкарбонила, сульфгидрила, имидазолила, тиазолила, оксазолила, тетразолила,
Figure 00000004
,
Figure 00000005
и
Figure 00000006
;
Х выбран из атома водорода, фтора, хлора, брома, йода, С1-С4 алкила, этенила, трифторметила, метокси.
2. Простое эфирное производное никотинилового спирта по п. 1, представленное формулой (IA), или его фармацевтически приемлемая соль или стереоизомер;
Figure 00000007
где:
R1 выбран из
Figure 00000008
и
Figure 00000009
;
R3 выбран из замещенного C1-C8 насыщенного алкиламино, замещенного C2-C6 ненасыщенного алкиламино, замещенного N-содержащего C2-C6 гетероцикл-1-ила, где каждый является моно-, ди-, три- или тетразамещенным заместителем(ми), выбранным из атома водорода, фтора, хлора, брома, йода, гидрокси, C1-C5 алкила, C1-C5 алкокси, амино, C1-C6 алкиламино, ацетиламино, циано, уреидо (-NH(C=O)NH2), гуанидино (-NH(C=NH)NH2), уреидоамино (-NH-NH(C=O)NH2), гуанидиноамино (-NH-NH(C=NH)NH2), сульфониламино (-NHSO3H), сульфамоила (-SO2NH2), метансульфониламино (-NH-SO2CH3), гидроксиформила (-COOH), C1-C8 алкоксилкарбонила, сульфгидрила, имидазолила, тиазолила, оксазолила, тетразолила,
Figure 00000010
,
Figure 00000011
и
Figure 00000012
;
Х выбран из атома водорода, фтора, хлора, брома, йода, С1-С4 алкила, этенила, трифторметила и метокси.
3. Простое эфирное производное никотинилового спирта по п. 2, представленное формулой (IA-1), или его фармацевтически приемлемая соль или стереоизомер;
Figure 00000013
где:
R3 выбран из замещенного C1-C8 насыщенного алкиламино, замещенного C2-C6 ненасыщенного алкиламино, замещенного N-содержащего C2-C6 гетероцикл-1-ила, где каждый является моно-, ди-, три- или тетразамещенным заместителем(ми), выбранным из атома водорода, фтора, хлора, брома, йода, гидрокси, C1-C5 алкила, C1-C5 алкокси, амино, C1-C6 алкиламино, ацетиламино, циано, уреидо (-NH(C=O)NH2), гуанидино (-NH(C=NH)NH2), уреидоамино (-NH-NH(C=O)NH2), гуанидиноамино (-NH-NH(C=NH)NH2), сульфониламино (-NHSO3H), сульфамоила (-SO2NH2), метансульфониламино (-NH-SO2CH3), гидроксиформила (-COOH), C1-C8 алкоксилкарбонила, сульфгидрила, имидазолила, тиазолила, оксазолила, тетразолила,
Figure 00000014
,
Figure 00000015
и
Figure 00000016
;
Х выбран из атома водорода, фтора, хлора, брома, йода, С1-С4 алкила, этенила, трифторметила и метокси.
4. Простое эфирное производное никотинилового спирта по п. 2, представленное формулой (IA-2), или его фармацевтически приемлемая соль или стереоизомер:
Figure 00000017
где:
R3 выбран из замещенного C1-C8 насыщенного алкиламино, замещенного C2-C6 ненасыщенного алкиламино, замещенного N-содержащего C2-C6 гетероцикл-1-ила, где каждый является моно-, ди-, три- или тетразамещенным заместителем(ми), выбранным из атома водорода, фтора, хлора, брома, йода, гидрокси, C1-C5 алкила, C1-C5 алкокси, амино, C1-C6 алкиламино, ацетиламино, циано, уреидо (-NH(C=O)NH2), гуанидино (-NH(C=NH)NH2), уреидоамино (-NH-NH(C=O)NH2), гуанидиноамино (-NH-NH(C=NH)NH2), сульфониламино (-NHSO3H), сульфамоила (-SO2NH2), метансульфониламино (-NH-SO2CH3), гидроксиформила (-COOH), C1-C8 алкоксилкарбонила, сульфгидрила, имидазолила, тиазолила, оксазолила, тетразолила,
Figure 00000018
,
Figure 00000019
и
Figure 00000020
;
Х выбран из атома водорода, фтора, хлора, брома, йода, С1-С4 алкила, этенила, трифторметила и метокси.
5. Простое эфирное производное никотинилового спирта по любому из пп. 1-4, или его фармацевтически приемлемая соль или стереоизомер, где R3 выбран из:
Figure 00000021
где R выбран из метила, этила, пропила, изопропила, бутила, пентила, гексила, гептила, октила; и
Х выбран из атома водорода, фтора, хлора, брома, метила, этенила и трифторметила.
6. Простое эфирное производное никотинилового спирта по п. 1 или его фармацевтически приемлемая соль или стереоизомер, где соединение выбрано из:
этил N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)серината дигидрохлорида
Figure 00000022
N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)серина
Figure 00000023
(S)-этил N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)серината
Figure 00000024
(S)-N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)серина
Figure 00000025
(S)-этил N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)серината дигидрохлорида
Figure 00000026
(S)-изопропил N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)серината дигидрохлорида
Figure 00000027
(R)-этил N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)серината
Figure 00000028
(R)-N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)серина
Figure 00000029
N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)глицина
Figure 00000030
N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)валина
Figure 00000031
(E)-3-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензиламино)бут-2-еннитрила
Figure 00000032
N,N-бис(гидроксиэтил)-4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензиламина
Figure 00000033
N-(2-метансульфонаминоэтил)-4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензиламина
Figure 00000034
N-(2-ацетиламиноэтил)-4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензиламина
Figure 00000035
(E)-3-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензиламино)бут-2-еноевой кислоты
Figure 00000036
2-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензиламино)этансульфоновой кислоты
Figure 00000037
N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)лейцина
Figure 00000038
N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)тирозина
Figure 00000039
N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)изолейцина
Figure 00000040
N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)аспарагина
Figure 00000041
N-(гидроксиэтил)-4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензиламина
Figure 00000042
N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)аланина
Figure 00000043
N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)пролина
Figure 00000044
(S)-N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)серината натрия
Figure 00000045
(S)-(N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-илметиленокси)бензил)серината кальция
Figure 00000046
(S)-(5-метил-2-оксо-1,3-диоксол-4-ил)метил N-(4-(2-бром-3-фенилбензилокси)-5-хлор-2-(пиридин-3-ил-метиленокси)бензил)серината
Figure 00000047
7. Простое эфирное производное никотинилового спирта по п. 1 или его стереоизомер и его фармацевтически приемлемая соль, где фармацевтически приемлемая соль включает соль, образованную неорганической кислотой, соль, образованную органической кислотой, соль иона щелочного металла, соль иона щелочноземельного металла или соль, образованную органическим основанием, которое обеспечивает физиологически приемлемый катион, и соль аммония.
8. Простое эфирное производное никотинилового спирта по п. 7 или его стереоизомер и его фармацевтически приемлемая соль, где неорганическая кислота выбрана из хлористоводородной кислоты, бромистоводородной кислоты, фосфорной кислоты или серной кислоты; органическая кислота выбрана из метансульфоновой кислоты, п-толуолсульфоновой кислоты, трифторуксусной кислоты, лимонной кислоты, малеиновой кислоты, винной кислоты, фумаровой кислоты, лимонной кислоты или молочной кислоты; ион щелочного металла выбран из иона лития, иона натрия, иона калия; ион щелочноземельного металла выбран из иона кальция и иона магния; органическое основание, которое обеспечивает физиологически приемлемый катион, выбрано из метиламина, диметиламина, триметиламина, пиперидина, морфолина или трис(2-гидроксиэтил)амина.
9. Способ получения простого эфирного производного никотинилового спирта по любому из пп. 1-8 или его стереоизомера или его фармацевтически приемлемой соли:
Figure 00000048
для получения соединений формулы (I), согласно их структуре, способ получения разделяется на две стадии:
(а) 2-гидрокси-4-(2-бром-3-R1-бензилокси)-Х-замещенный бензальдегид 1 в качестве исходного соединения подвергают взаимодействию с пиридин-3-илметиленгалогенидом в щелочных условиях с получением альдегидсодержащего промежуточного соединения 2;
(b) альдегидсодержащее промежуточное соединение 2 в качестве исходного соединения конденсируют с HR3, содержащим аминогруппу или иминогруппу, и полученный продукт восстанавливают с получением целевого соединения I;
где R1, R3 и X каждый имеет значения, определенные в любом из пп. 1-8.
10. Фармацевтическая композиция, отличающаяся тем, что она содержит простое эфирное производное никотинилового спирта по любому из пп. 1-8, или его стереоизомер или фармацевтически приемлемую соль в качестве активного ингредиента и один или более фармацевтически приемлемых носителей или эксципиентов.
11. Применение простого эфирного производного никотинилового спирта по любому из пп. 1-8 или его стереоизомера или его фармацевтически приемлемой соли в производстве лекарственного средства для профилактики и/или лечения заболевания, ассоциированного с сигнальным путем PD-1/PD-L1.
12. Применение по п. 11, где заболевание, ассоциированное с сигнальным путем PD-1/PD-L1, выбрано из рака, инфекционного заболевания и аутоиммунного заболевания.
13. Применение по п. 12, где рак выбран из рака кожи, рака легкого, опухоли органов мочевой системы, гематологической опухоли, рака молочной железы, глиомы, опухоли органов пищеварительной системы, опухоли органов репродуктивной системы, лимфомы, опухоли нервной системы, опухоли головного мозга, рака головы и шеи; инфекционное заболевание выбрано из бактериальной инфекции и вирусной инфекции; аутоиммунное заболевание выбрано из органоспецифического аутоиммунного заболевания и системного аутоиммунного заболевания; где органоспецифическое аутоиммунное заболевание включает хронический лимфоцитарный тиреоидит, гипертиреоз, инсулинозависимый сахарный диабет, миастению, язвенный колит, злокачественную анемию с хроническим атрофическим гастритом, геморрагический легочно-почечный синдром, первичный билиарный цирроз, рассеянный цереброспинальный склероз и острый идиопатический полиневрит; системные аутоиммунные заболевания включают ревматоидный артрит, системную красную волчанку, системный васкулит, склеродермию, пемфигус, дерматомиозит, смешанное заболевание соединительной ткани и аутоиммунную гемолитическую анемию.
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