RU2462454C2 - Новое сульфонамидное производное малоновой кислоты и его фармацевтическое применение - Google Patents

Новое сульфонамидное производное малоновой кислоты и его фармацевтическое применение Download PDF

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RU2462454C2
RU2462454C2 RU2010101633/04A RU2010101633A RU2462454C2 RU 2462454 C2 RU2462454 C2 RU 2462454C2 RU 2010101633/04 A RU2010101633/04 A RU 2010101633/04A RU 2010101633 A RU2010101633 A RU 2010101633A RU 2462454 C2 RU2462454 C2 RU 2462454C2
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Russia
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amino
malonamide
atom
benzyl
naphthylsulfonyl
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RU2010101633/04A
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RU2010101633A (ru
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Томохиро ЙОСИДА (JP)
Томохиро Йосида
Хироси САКАСИТА (JP)
Хироси Сакасита
Ацуси НУМАТА (JP)
Ацуси НУМАТА
Саори ТАХАРА (JP)
Саори ТАХАРА
Хисаси КАВАСУМИ (JP)
Хисаси КАВАСУМИ
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Мицубиси Танабе Фарма Корпорейшн
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    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/26—Radicals substituted by sulfur atoms
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    • A61P13/00—Drugs for disorders of the urinary system
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    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
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Abstract

Настоящее изобретение относится к новым производным сульфонилмалонамида формулы (II) или к их фармакологически приемлемым солям, обладающим агонистической активностью в отношении АТ2 рецептора, к фармацевтическим композициям на их основе и к агонисту АТ2 рецептора.
Figure 00000611
где R12 представляет собой 2-нафтил, транс-β-стирил, фенетил, 3-феноксипропил или 4-фенилбутил, a R13, R14 и R15 имеют значения, указанные в формуле изобретения. 4 н. и 9 з.п. ф-лы, 591 пр., 14 схем, 5 табл.

Description

Текст описания приведен в факсимильном виде.
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Claims (13)

1. Производное сульфонилмалонамида, которое представлено следующей формулой (II)
Figure 00000599

где R12 представляет собой 2-нафтил, транс-β-стирил, фенетил, 3-феноксипропил или 4-фенилбутил;
один из R13 и R14 представляет собой атом водорода, а другой представляет собой изопропил, изобутил, неопентил, аллил, -CH2-R16, {где R16 представляет собой необязательно замещенный С3-10циклоалкил, необязательно замещенный гетероцикл или -CO-NR5R6, (где R5 и R6 являются одинаковыми или разными, и каждый представляет собой атом водорода, С1-6алкил, или R5 и R6 вместе с соединенным с ними атомом азота необязательно образуют необязательно замещенный циклический амино)}, -(CH2)2-R16′, (где R16′ представляет собой циано или C1-6 алкокси) или -(СН2)n-Ar2, (где n представляет собой целое число от 1 до 3, и Ar2 представляет собой замещенный фенил или необязательно замещенный гетероарил), или R13 и R14 вместе с соединенным с ними атомом углерода необязательно образуют следующую формулу
Figure 00000600

R15 представляет собой ди(С1-6алкил)амино или следующую формулу
Figure 00000601

(где Z представляет собой атом водорода, атом галогена или трифторметил, Y представляет собой атом азота или СН, R17 представляет собой этил, изопропил или 3-пентил, при условии, что, когда Y представляет собой атом азота, то Z представляет собой атом водорода),
при этом в указанных выше группах заместитель необязательно замещенного С3-10циклоалкила в качестве R16 представляет собой метил; заместитель необязательно замещенного гетероцикла в качестве R16 представляет собой бензоил, бензил, бензилкарбонил, нафтилкарбонил, феноксикарбонил, пиридинкарбонил, фениламинокарбонил, бензолсульфонил, бензилсульфонил или бензотиазолил; необязательно замещенный циклический амино в качестве R5 и R6 представляет собой азетидинил, пирролидинил, пиперидинил, пиперазинил, морфолино, 1,4-диазепанил, 1,2,5,6-тетрагидропиридил, циклопентанспиро-4′-пиперидинил, индолинил, изоиндолинил, 1,2,3,4-тетрагидрохинолил, 1,2,3,4-тетрагидроизохинолил или спиро[индан-1,4′-пиперидин]-1′-ил; необязательно замещенный гетероарил в качестве Ar2 представляет собой пиридин, который может быть замещен C1-6алкокси; бензоксазол, который может быть замещен фенилом; пиразол, который может быть замещен C1-6алкилом, изопентенилом, хлорфенилом, бензилом, аминобензилом, фторбензилом, пиридилметилом, хлорпиридилметилом, фенилэтилом, фенилпропаном или фенилпропеном; тиазол, который может быть замещен С1-6алкилом, изопентенилом, хлорбензилом, аминобензилом, фторбензилом, пиридилметилом, хлорпиридилметилом, фенилэтилом, фенилпропаном или фенилпропеном; оксазол, который может быть замещен фторфенилом; триазол, который может быть замещен бензилом; или тетразол, который может быть замещен C1-6алкилом, С3-10циклоалкилом, фенилом или бензилом;
заместитель замещенного фенила в качестве Ar2 представляет собой атом фтора, атом хлора, атом брома, циано, нитро, гуанидино, амино (исключая замещение в орто-положении), -NHCOAr3, -NHSO2Ar3, (где Ar3 представляет собой С6-14арил, который может быть замещен одним или более заместителями, выбранными из атома водорода, атома фтора, атома хлора, атома брома, метокси, метила, гидроксила, амино, диметиламино, ацетиламино, трифторметила или циано; или гетероарил, который может быть замещен атомом хлора, атомом брома, амино, метилом, этилом или нитро), -NHCOR18, (где R18 представляет собой C1-6алкил или С3-10циклоалкил, который может быть замещен С1-6алкилом), ди(С1-6алкил)амино, C1-6алкокси, метилендиокси, трифторметокси, карбоксил, C1-6алкоксикарбонил, имидазолил, имидазолилметил, метилбензимидазолилметил, нитрофенилметил, аминофенилэтил, фторфенилокси, бензилокси, пиридилокси, хлорпиридилокси или следующую формулу
Figure 00000602
;
гетероарил в качестве Ar3 представляет собой пиридин, пиримидин, пиразин, пиразол, оксазол, фуран, тиофен, изоксазол или тиазол;
или его фармакологически приемлемая соль.
2. Производное сульфонилмалонамида по п.1, где необязательно замещенный циклический амино в качестве R5 и R6 представляет собой пирролидино, 1,2,3,4-тетрагидрохинолил или пиперазино, который может быть замещен нитрофенилом, аминофенилом или цианопиридином.
3. Производное сульфонилмалонамида по п.1, где Ar2 для R13 или R14 представляет собой замещенный фенил, представленный следующей формулой
Figure 00000603

где X представляет собой атом фтора, атом хлора, атом брома, циано, нитро, амино (исключая замещение в орто-положении), NHCOAr3, - NHSO2Ar3, (где Ar3 представляет собой C6-14арил, который может быть замещен одним или более заместителями, выбранными из атома фтора, атома хлора, метокси, метила, гидроксила, амино или диметиламино; или гетероарил, который может быть замещен одним или более заместителями, выбранными из атома хлора, атома брома, метила, этила или нитро), - NHCOR18, (где R18 представляет собой С1-6алкил или С3-10циклоалкил, который может быть замещен C1-6алкилом), С1-6алкоксикарбонил, ди(С1-6алкил) амино, С1-6алкокси, метилендиокси, трифторметокси, карбоксил, имидазолил, имидазолилметил, метилбензимидазолилметил, нитрофенилэтил, аминофенилэтил, фторфенилокси, бензилокси, пиридилокси или хлорпиридилокси,
при этом в указанных выше группах необязательно замещенный гетероарил в качестве Ar3 представляет собой пиридин, пиримидин, пиразин, пиразол, оксазол, фуран, тиофен, изоксазол или тиазол,
или его фармакологически приемлемая соль.
4. Производное сульфонилмалонамида по п.1, которое представлено следующей формулой (III)
Figure 00000604

где R12, R17, Y и Z - такие, как определено в п.1, один из R19 и R20 представляет собой атом водорода, а другой представляет собой изопропил, изобутил, неопентил, аллил, циклопропилметил или -СН2-Ar2, где Ar2 - такой, как определено в п.1,
или его фармакологически приемлемая соль.
5. Производное сульфонилмалонамида по п.1, которое представлено следующей формулой (IV)
Figure 00000605

где n представляет собой целое число от 1 до 3, Ar2 - такой, как определено в п.1,
или его фармакологически приемлемая соль.
6. Производное сульфонилмалонамида по п.5, где Ar2 представляет собой замещенный фенил, представленный следующей формулой
Figure 00000606

где R21 представляет собой атом фтора, атом хлора, нитро, циано, амино (исключая замещение в орто-положении), диметиламино, метокси, трифторметокси, метоксикарбонил, фенил, 2-пиридилокси, 1-имидазолил или следующую формулу
Figure 00000607

Figure 00000608

(где Ar3 представляет собой С6-14арил, который может быть замещен одним или более заместителями, выбранными из атома фтора, атома хлора, метокси, метила, гидроксила, амино или диметиламино; или гетероарил, который может быть замещен одним или более заместителями, выбранными из атома хлора, атома брома, метила, этила или нитро; необязательно замещенный гетероарил в качестве Ar3 представляет собой пиридин, пиримидин, пиразин, пиразол, оксазол, фуран, тиофен, изоксазол или тиазол),
или его фармакологически приемлемая соль.
7. Производное сульфонилмалонамида по п.5, где Ar2 представляет собой замещенный фенил, представленный следующей формулой
Figure 00000609

где Ar4 представляет собой 2-тиенил, 2-фурил, 4-пиридил, 3-пиридил, 2-пиридил или следующую формулу
Figure 00000610

где R22 и R25 являются одинаковыми или разными, и каждый представляет собой атом водорода, амино, атом фтора, гидрокси, метокси, метил или атом хлора, R23 представляет собой атом водорода или атом фтора, R24 представляет собой атом водорода, атом фтора, атом хлора, метил, амино, метокси или циано, и n представляет собой 1,
или его фармакологически приемлемая соль.
8. Производное сульфонилмалонамида по п.1, которое представляет собой следующее соединение:
N,N-диэтил-2-{4-[(2,6-дифторбензоил)амино]бензил}-N′-(2-нафтилсульфонил)малонамид,
(2S)-2-[4-(бензоиламино)бензил]-N,N-диэтил-N′-(2-нафтилсульфонил)малонамид,
(2S)-N,N-диэтил-2-{4-[(2-фторбензоил)амино]бензил}-N′-(2-нафтилсульфонил)малонамид,
(2S)-N,N-диэтил-2-{4-[(3-фторбензоил)амино]бензил}-N′-(2-нафтилсульфонил)малонамид,
(2S)-N,N-диэтил-2-{4-[(2,4-дифторбензоил)амино]бензил}-N′-(2-нафтилсульфонил)малонамид,
(2S)-N,N-диэтил-2-{4-[(4-метилбензоил)амино]бензил}-N′-(2-нафтилсульфонил)малонамид,
(2S)-N,N-диэтил-N′-(2-нафтилсульфонил)-2-{4-[(2-тиеноил)амино]бензил}малонамид,
(2S)-N,N-диэтил-2-{4-[(2-фуроил)амино]бензил}-N′-(2-нафтилсульфонил)малонамид,
(2S)-2-{4-[(2-амино-5-фторбензоил)амино]бензил}-N,N-диэтил-N′-(2-нафтилсульфонил)малонамид,
(2S)-2-{4-[(2-амино-6-фторбензоил)амино]бензил}-N,N-диэтил-N′-(2-нафтилсульфонил)малонамид,
(2S)-N,N-диэтил-N′-(2-нафтилсульфонил)-2-{4-[(2-пиридилкарбонил)амино]бензил}малонамид,
(2S)-2-{4-[(2-амино-4-хлорбензоил)амино]бензил}-N,N-диэтил-N′-(2-нафтилсульфонил)малонамид,
(2S)-2-{4-[(2-аминобензоил)амино]бензил}-N,N-диэтил-N′-(2-нафтилсульфонил)малонамид,
(2S)-2-{4-[(2-амино-5-хлорбензоил)амино]бензил}-N,N-диэтил-N′-(2-нафтилсульфонил)малонамид,
(2S)-2-{4-[(2-амино-4,5-дифторбензоил)амино]бензил}-N,N-диэтил-N′-(2-нафтилсульфонил)малонамид,
(2S)-2-{4-[(2-амино-4-фторбензоил)амино]бензил}-N,N-диэтил-N′-(2-нафтилсульфонил)малонамид,
(2S)-2-{4-[(2-амино-5-метилбензоил)амино]бензил}-N,N-диэтил-N′-(2-нафтилсульфонил)малонамид,
2-(4-фторбензил)-N-изопропил-N-(3-пиридил)-N′-((Е)-стирилсульфонил)малонамид,
2-аллил-N-(4-фторфенил)-N-изопропил-N′-((Е)-стирилсульфонил)малонамид,
N-(4-фторфенил)-2-изобутил-N-изопропил-N′-((Е)-стирилсульфонил)малонамид,
N-(4-фторфенил)-2-изобутил-N-изопропил-N′-фенетилсульфонилмалонамид,
N-(4-фторфенил)-2-изобутил-N-изопропил-N′-(2-нафтилсульфонил)малонамид,
(2S или 2R)-2-циклопропилметил-N-(4-фторфенил)-N-изопропил-N′-((Е)-2-стирилсульфонил)малонамид,
2-циклопропилметил-N-(4-фторфенил)-N-изопропил-N′-фенетилсульфонилмалонамид или
2-циклопропилметил-N-(4-фторфенил)-N-изопропил-N′-(2-нафтилсульфонил)малонамид,
или его фармакологически приемлемая соль.
9. Фармацевтическая композиция, обладающая агонистической активностью в отношении АТ2 рецептора, содержащая производное сульфонилмалонамида по любому из пп.1-8 или его фармакологически приемлемую соль, в качестве активного компонента.
10. Фармацевтическая композиция для лечения или профилактики нарушения, в котором участвует ренин-ангиотензин-альдостероновая система, выбранного из удара, заболевания почек, заболевания сердца, гипертензии, диабета, диабетических осложнений, гиперлипидемии и метаболического синдрома, содержащая производное сульфонилмалонамида по любому из пп.1-8 или его фармакологически приемлемую соль, в качестве активного компонента.
11. Агонист АТ2 рецептора, содержащий производное сульфонилмалонамида по любому из пп.1-8 или его фармакологически приемлемую соль.
12. Агонист АТ2 рецептора по п.11, содержащий производное сульфонилмалонамида по п.8 или его фармакологически приемлемую соль.
13. Агонист АТ2 рецептора по п.12, который является селективным к АТ2 рецептору.
RU2010101633/04A 2007-06-20 2008-06-19 Новое сульфонамидное производное малоновой кислоты и его фармацевтическое применение RU2462454C2 (ru)

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