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RU2004120784A - Замещенные 2-аминоциклоалканкарбоксамиды и их применение в качестве ингибиторов цистеиновой протеазы - Google Patents

Замещенные 2-аминоциклоалканкарбоксамиды и их применение в качестве ингибиторов цистеиновой протеазы Download PDF

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RU2004120784A
RU2004120784A RU2004120784/04A RU2004120784A RU2004120784A RU 2004120784 A RU2004120784 A RU 2004120784A RU 2004120784/04 A RU2004120784/04 A RU 2004120784/04A RU 2004120784 A RU2004120784 A RU 2004120784A RU 2004120784 A RU2004120784 A RU 2004120784A
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ГАБРИЕЛЬ Томас (US)
ГАБРИЕЛЬ Томас
Элизабет КРАУСС Нэнси (US)
Элизабет КРАУСС Нэнси
МИРЗАДЕГАН Таранех (US)
МИРЗАДЕГАН Таранех
Соланг ПАЛМЕР Уайли (US)
Соланг ПАЛМЕР Уайли
Бернард СМИТ Дейвид (US)
Бернард Смит Дейвид
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Ф.Хоффманн-Ля Рош Аг (Ch)
Ф.Хоффманн-Ля Рош Аг
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Claims (22)

1. Соединения формулы (I)
Figure 00000001
где R1 означает гетероарил, (CR'R")m-CO-Ra или -S(O)p-Ra, где
R' и R" независимо означают водород или (низш.)алкил,
m равно 0 или 1,
р равно 1 или 2,
Ra означает гетероарил, гетероарил(низш.)алкил или гетероарил(низш.)алкокси, где гетероарил в каждом случае выбирают из группы, включающей индолил, пиридил, хинолинил, изохинолинил, N-оксохинолинил, N-оксоизохинолинил, нафтиридинил, пиразолил, индазолил, фуро[2,3-b]пиридинил, фуро[2,3-с]пиридинил, фуро[3,2-с]пиридинил, фуро[3,2-b]пиридинил, 1Н-пирроло[3,2-b]пиридинил, 1Н-пирроло[2,3-b]пиридинил, 1Н-пирроло[3,2-с]пиридинил, 1Н-пирроло[2,3-с]пиридинил, 1Н-пиразоло[3,4-b]пиридин, 1Н-пиразоло[3,4-с]пиридин, 1Н-пиразоло[4,3-b]пиридин, 1Н-пиразоло[4,3-с]пиридин, бензотиазолил, азаиндолил, имидазо[2,1-b]бензотиазолил и индолизинил, каждый необязательно замещенный, R2 означает водород или (низш.)алкил, R3 означает водород или (низш.)алкил, R4 означает водород или (низш.)алкил, R5 означает водород, (низш.)алкил, гетероалкил, циклоалкил, циклоалкил(низш.)алкил, (низш.)алкоксикарбонил(низш.)алкил, арил, аралкил, гетероарил или гетероарил(низш.)алкил, R6 означает водород или алкил, n означает целое число от 1 до 3, и их фармацевтически приемлемые соли и/или фармацевтически приемлемые сложные эфиры.
2. Соединения по п.1, где R1 означает (CR'R")m-CO-Ra, m равно нулю, а Ra имеет значения, указанные в п.1.
3. Соединения по п.2, где Ra означает индолил, пиридил, хинолинил, изохинолинил, N-оксохинолинил, N-оксоизохинолинил, пиразолил, индазолил, хиноксалинил, бензотиазолил, пирролопиридинил, бензоимидазотиазолил или индолизинил, каждый необязательно замещенный одним или более заместителями, выбранными из группы, включающей галоген, гидрокси, (низш.)алкил, гидрокси(низш.)алкил, (низш.)алкокси, алкилтио, NH2, NH-COO-(низш.)алкил, NH-СОО-(низш.)алкенил, NH-SO2-(низш.)алкил, SO2NH2, арил, гетероциклилокси, гетероциклилалкокси и гетероарилалкокси.
4. Соединения по п.3, где Ra означает 1Н-индол-2-ил, 1-метил-1H-индол-2-ил, 1Н-индол-5-ил, хинолин-2-ил, 6-[2-(4-метилпиперазин-1-ил)этокси]-1Н-индол-2-ил, 1-метил-6-(2-пиридин-2-илэтокси)-1Н-индол-2-ил или 1-(2-гидроксиэтил)-1Н-индол-2-ил.
5. Соединения по п.1, где R1 означает хинолин-8-ил.
6. Соединения по п.1, где R2 означает водород.
7. Соединения по п.1, где R3 означает водород.
8. Соединения по п.1, где R4 означает водород.
9. Соединения по п.1, где R5 означает водород, (низш.)алкил, гидрокси(низш.)алкил, (низш.)алкоксикарбонил(низш.)алкил, (низш.)алкилтио(низш.)алкил, циклоалкил, гетероарил(низш.)алкил или арил(низш.)алкил.
10. Соединения по п.1, где R5 означает водород, (низш.)алкил или циклоалкил.
11. Соединения по п.1, где R5 означает водород, изобутил или циклопропил.
12. Соединения по п.1, где R6 означает водород.
13. Соединения по любому из пп.1-12, где n равно двум.
14. Соединения по п.1, выбранные из группы, включающей
N-[(1S,2R)-2-({[(1S)-1-циано-3-метилбутил]амино}карбонил)пиклогексил]-1-метил-1Н-индол-2-карбоксамид,
N-((1S,2R)-2-{[(цианометил)амино]карбонил}циклогексил)-1Н-индол-2-карбоксамид,
N-[(1S,2R)-2-({[циано(циклопропил)метил]амино}карбонил)циклогексил]-1-метил-1Н-индол-2-карбоксамид,
N-[(1S,2R)-2-({[циано(циклопропил)метил]амино}карбонил)циклогексил]-1Н-индол-5-карбоксамид, N-[(1S,2R)-2-({[(S)-циано(циклопропил)метил]амино}карбонил)циклогексил]-1-метил-1H-индол-2-карбоксамид,
N-[(1S,2R)-2-({[циано(циклопропил)метил]амино}карбонил)циклогексил]хинолин-2-карбоксамид,
N-((1S,2R)-2-{[(цианометил)амино]карбонил}циклогексил)-6-[2-(4-метилпиперазин-1-ил)этокси]-1 Н-индол-2-карбоксамид,
[(1S,2R)-2-(1-(S)-циано-3-метилбутилкарбамоил)циклогексил]амид1-метил-6-(2-пиридин-2-илэтокси)-1Н-индол-2-карбоновой кислоты и
[(1S,2R)-2-(1-(S)-циано-3-метилбутилкарбамоил)циклогексил]амид1-(2-гидроксиэтил)-1Н-индол-2-карбоновой кислоты.
15. Способ получения соединения по любому из пп.1-14, включающий
а) взаимодействие соединения формулы (II)
Figure 00000002
с соединением формулы (III)
Figure 00000003
где R1, R2, R3, R4, R5, R6 и n имеют значения, указанные в любом из пп.1-14, или
б) взаимодействие соединения формулы (IV)
Figure 00000004
с соединением формулы (V) или (VI)
Figure 00000005
где R2, R3, R4, R5, R6, Ra и n имеют значения, указанные в любом из пп.1-14, или
в) обработку соединения формулы (XI)
Figure 00000006
дегидратирующим агентом, где R2, R3, R4, R5, R6 и n имеют значения, указанные в любом из пп.1-14.
16. Соединения по п.1, полученные способом по п.15.
17. Фармацевтические композиции, включающая соединение по любому из пп.1-14 и фармацевтически приемлемый носитель и/или адъювант.
18. Соединения по п.1 для применения в качестве терапевтически активного соединения.
19. Соединения по п.1 для применения в качестве терапевтически активного соединения при лечении и/или профилактике заболеваний, ассоциированных с цистеиновыми протеазами.
20. Способ лечения и/или профилактики заболеваний, ассоциированных с цистеиновыми протеазами, включающий введение соединений по любому из пп.1-14 человеку или животному.
21. Применение соединений по любому из пп.1-14 для лечения и/или профилактики заболеваний, ассоциированных с цистеиновыми протеазами.
22. Применение соединений по любому из пп.1-14 для получения лекарственных средств, предназначенных для лечения и/или профилактики заболеваний, ассоциированных с цистеиновыми протеазами.
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2676328C2 (ru) * 2014-02-14 2018-12-28 Тоа Эйо Лтд. Циклическое углеводородное соединение

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000042213A1 (en) * 1999-01-13 2000-07-20 The Research Foundation Of State University Of New York A novel method for designing protein kinase inhibitors
US7005445B2 (en) * 2001-10-22 2006-02-28 The Research Foundation Of State University Of New York Protein kinase and phosphatase inhibitors and methods for designing them
GB0128996D0 (en) 2001-12-04 2002-01-23 Novartis Ag Organic compounds
AU2003235741B8 (en) * 2002-01-07 2009-01-15 Eisai R&D Management Co., Ltd. Deazapurines and uses thereof
SE0203712D0 (sv) 2002-12-13 2002-12-13 Astrazeneca Ab Novel compounds
GB0403038D0 (en) 2004-02-11 2004-03-17 Novartis Ag Organic compounds
WO2006007664A1 (en) * 2004-07-22 2006-01-26 Genomics Research Partners Pty Ltd Agents and methods for diagnosing osteoarthritis
WO2007002481A2 (en) * 2005-06-28 2007-01-04 Merck & Co., Inc. Non-nucleoside reverse transcriptase inhibitors
RU2424234C2 (ru) * 2005-08-05 2011-07-20 Ибриженикс Са Новые ингибиторы цистеиновых протеаз и их терапевтическое применение
DE602005010421D1 (de) * 2005-08-05 2008-11-27 Hybrigenics Sa Neue Cysteine Protease Hemmers und ihre therapeutische Anwendungen
WO2007041775A1 (en) * 2005-10-10 2007-04-19 The University Of Queensland Cysteine protease inhibitors incorporating azide groups
WO2007081530A2 (en) * 2006-01-03 2007-07-19 Med Institute, Inc. Endoluminal medical device for local delivery of cathepsin inhibitors
JP4012239B2 (ja) 2006-01-11 2007-11-21 生化学工業株式会社 オキサゾロン誘導体
US7838542B2 (en) * 2006-06-29 2010-11-23 Kinex Pharmaceuticals, Llc Bicyclic compositions and methods for modulating a kinase cascade
CN101687864A (zh) * 2007-06-26 2010-03-31 阿斯利康(瑞典)有限公司 作为组织蛋白酶k抑制剂的1-氰基环丙基-衍生物
CN101591327B (zh) * 2008-05-26 2012-07-25 华东理工大学 苯烷酰胺类化合物及其用途
DK2736888T3 (da) * 2011-07-26 2016-02-01 Sanofi Sa 3-heteroaroylaminopropionsyrederivater og deres anvendelse som farmaceutika
ES2660210T3 (es) 2012-09-07 2018-03-21 Novartis Ag Derivados de indolcarboxamida y usos de los mismos
NO2699580T3 (ru) 2014-01-24 2018-02-24
CA3066711A1 (en) 2017-07-31 2019-02-07 Novartis Ag Use of mavoglurant in the reduction of cocaine use or in preventing relapse into cocaine use
CN112055593B (zh) 2018-03-01 2024-04-09 阿斯利康(瑞典)有限公司 药物组合物
EP3823627A4 (en) 2018-07-17 2022-04-20 Insmed Incorporated CERTAIN (2S)-N-[(1S)-1-CYANO-2-PHENYLETHYL]-1,4-OXAZEPANE-2-CARBOXAMIDES FOR THE TREATMENT OF LUPUS ENEHROPATHY
EP4497473A3 (en) 2020-08-26 2025-04-23 Haisco Pharmaceuticals Pte. Ltd. Nitrile derivative that acts as inhibitor of dipeptidyl peptidase 1 and use thereof
EP4257588A4 (en) 2020-12-04 2024-10-16 Reistone Biopharma Company Limited SMALL MOLECULE INHIBITOR OF CATHEPSIN C AND ITS MEDICINAL USE
AU2023285191A1 (en) 2022-06-07 2024-12-12 Reistone Biopharma Company Limited Pharmaceutically acceptable salt of benzo[c]chroman compound and polymorphic form and use of pharmaceutically acceptable salt
EP4538271A4 (en) 2022-06-07 2025-10-08 Reistone Biopharma Company Ltd POLYMORPH OF BENZO[C]CHROMANE COMPOUND, ITS PREPARATION METHOD AND ITS USE
AU2024206233A1 (en) 2023-01-06 2025-08-21 Insmed Incorporated Novel, reversible dpp1 inhibitors and uses thereof

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU177576B (en) 1975-06-02 1981-11-28 Chinoin Gyogyszer Es Vegyeszet Process for preparing 2-amino-cyclohexane carboxylic acid,its amides and similar compounds
DE4417163A1 (de) 1994-05-17 1995-11-23 Hoechst Schering Agrevo Gmbh Heterocyclylamino- und Heterocyclyloxy-cycloalkyl-Derivate, ihre Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel und Fungizide
IT1283467B1 (it) 1996-07-19 1998-04-21 Menarini Farma Ind Derivati di cicloalcani 1,2 sostituiti come inibitori della trombina, procedimento per la loro preparazione e loro impiego in formulazioni
SK6572000A3 (en) 1997-11-05 2000-10-09 Novartis Ag Dipeptide nitriles, process for the preparation thereof, their use as medicaments and pharmaceutical composition comprising them
CA2395179A1 (en) * 1999-12-24 2001-07-05 F. Hoffmann-La Roche Ag Nitrile derivatives as cathepsin k inhibitors
JP2003525874A (ja) 2000-01-06 2003-09-02 メルク フロスト カナダ アンド カンパニー プロテアーゼ阻害剤としての新規化合物および組成物
US6462076B2 (en) * 2000-06-14 2002-10-08 Hoffmann-La Roche Inc. Beta-amino acid nitrile derivatives as cathepsin K inhibitors
JP4343690B2 (ja) 2001-11-13 2009-10-14 メルク フロスト カナダ リミテツド プロテアーゼ阻害薬としてのシアノアルキルアミノ誘導体

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2676328C2 (ru) * 2014-02-14 2018-12-28 Тоа Эйо Лтд. Циклическое углеводородное соединение

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