EA201200866A1 - Ингибиторы цистеиновых протеаз - Google Patents

Ингибиторы цистеиновых протеаз

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Publication number
EA201200866A1
EA201200866A1 EA201200866A EA201200866A EA201200866A1 EA 201200866 A1 EA201200866 A1 EA 201200866A1 EA 201200866 A EA201200866 A EA 201200866A EA 201200866 A EA201200866 A EA 201200866A EA 201200866 A1 EA201200866 A1 EA 201200866A1
Authority
EA
Eurasian Patent Office
Prior art keywords
cysteen
haloalkyl
alkyl
proteas
inhibitors
Prior art date
Application number
EA201200866A
Other languages
English (en)
Inventor
Сусана Айеса
Каролина Эрсмарк
Урсула Грабовска
Эллен Хьюитт
Даниель Йенссон
Пиа Канберг
Бьерн Классон
Петер Линд
Стина Лундгрен
Лурдес Оден
Кевин Паркес
Даниель Виктелиус
Original Assignee
МЕДИВИР ЮКей ЛИМИТЕД
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GBGB1010084.0A external-priority patent/GB201010084D0/en
Application filed by МЕДИВИР ЮКей ЛИМИТЕД filed Critical МЕДИВИР ЮКей ЛИМИТЕД
Publication of EA201200866A1 publication Critical patent/EA201200866A1/ru

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    • CCHEMISTRY; METALLURGY
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    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05Dipeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
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    • A61P11/02Nasal agents, e.g. decongestants
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • C07C271/10Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/20Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
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    • C07C271/10Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
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    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D277/32Heterocyclic 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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/0606Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
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    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic

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Abstract

Соединения формулы (II), где Rпредставляет собой Н; и Rпредставляет собой C-Салкил, карбоциклил или Het; или Rи Rвместе образуют насыщенный циклический амин с 3-6 кольцевыми атомами; Rи Rнезависимо представляют собой Н, галоген, C-Салкил, C-Сгалогеналкил или C-Салкоксигруппу, или Rи Rвместе с атомом углерода, к которому они присоединены, образуют С-Сциклоалкил; Rпредставляет собой разветвленную С-Салкильную цепь, С-Сгалоалкил или -СНС-Сциклоалкил; Rпредставляет собой C-Салкил, C-Сгалоалкил или оксетан-3-ил, для применения в профилактике или лечении нарушения, характеризующегося неадекватной экспрессией или активацией катепсина S.
EA201200866A 2009-12-10 2010-12-10 Ингибиторы цистеиновых протеаз EA201200866A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
SE0950951 2009-12-10
GBGB1010084.0A GB201010084D0 (en) 2010-06-16 2010-06-16 Cysteine protease inhibitors
PCT/IB2010/055732 WO2011070539A1 (en) 2009-12-10 2010-12-10 Cysteine protease inhibitors

Publications (1)

Publication Number Publication Date
EA201200866A1 true EA201200866A1 (ru) 2012-12-28

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA201200866A EA201200866A1 (ru) 2009-12-10 2010-12-10 Ингибиторы цистеиновых протеаз

Country Status (13)

Country Link
US (2) US8815809B2 (ru)
EP (2) EP2509956B1 (ru)
JP (2) JP2013513597A (ru)
KR (2) KR20120093423A (ru)
CN (2) CN102834383A (ru)
AU (1) AU2010329468B2 (ru)
BR (2) BR112012013861A2 (ru)
CA (2) CA2782294A1 (ru)
EA (1) EA201200866A1 (ru)
IN (2) IN2012DN04914A (ru)
MX (2) MX2012006652A (ru)
RU (1) RU2012128859A (ru)
WO (2) WO2011070539A1 (ru)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010070615A1 (en) * 2008-12-19 2010-06-24 Medivir Uk Ltd Cysteine protease inhibitors
CA2782294A1 (en) * 2009-12-10 2011-06-16 Medivir Uk Limited Cysteine protease inhibitors
JP2013534917A (ja) * 2010-06-16 2013-09-09 メディヴィル・ユーケイ・リミテッド 自己免疫障害、アレルギー、及び慢性疼痛状態、等の治療に有用な新規カテプシンsプロテアーゼ阻害剤
WO2012168852A1 (en) * 2011-06-08 2012-12-13 Medivir Uk Ltd Cysteine protease inhibitors
WO2012172473A1 (en) * 2011-06-13 2012-12-20 Medivir Uk Ltd Cysteine protease inhibitors
GB201314503D0 (en) * 2013-08-13 2013-09-25 Medivir Ab Cysteine protease inhibitor salt
CN113332420B (zh) * 2021-06-30 2023-07-28 蚌埠医学院 日本血吸虫半胱氨酸蛋白酶抑制剂在动脉粥样硬化方面的应用

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2098702A1 (en) * 1990-12-28 1992-06-29 James C. Powers Peptide ketoamides, ketoacids, and ketoesters
JP3892187B2 (ja) * 1998-11-12 2007-03-14 生化学工業株式会社 環状アミド誘導体
KR20040015725A (ko) * 2001-06-01 2004-02-19 액시스 파마슈티컬스 인코포레이티드 카텝신 s 억제제로서의 화합물 및 약제학적 조성물
MXPA04002282A (es) 2001-09-14 2005-03-07 Axis Pharmaceutical Inc Nuevos compuestos y preparaciones como inhibidores de la catepsina.
WO2003091202A1 (fr) 2002-04-25 2003-11-06 Ono Pharmaceutical Co., Ltd. Composes derives de dicetohydrazine et medicaments contenant ces composes comme ingredient actif
ZA200708602B (en) * 2005-03-21 2009-02-25 Applera Corp Alpha ketoamide compounds as cysteine protease inhibitors
JP2008533205A (ja) * 2005-03-21 2008-08-21 セレーラ ジェノミックス システインプロテアーゼインヒビターとしてのαケトアミド化合物
EA017874B1 (ru) * 2005-03-21 2013-03-29 Вайробей, Инк. Производные альфа-кетоамидов в качестве ингибиторов цистеинпротеаз
WO2010070615A1 (en) 2008-12-19 2010-06-24 Medivir Uk Ltd Cysteine protease inhibitors
CA2782294A1 (en) * 2009-12-10 2011-06-16 Medivir Uk Limited Cysteine protease inhibitors

Also Published As

Publication number Publication date
JP2013513597A (ja) 2013-04-22
EP2509956A4 (en) 2013-06-19
JP2013513598A (ja) 2013-04-22
EP2509956A1 (en) 2012-10-17
IN2012DN04915A (ru) 2015-09-25
CA2782294A1 (en) 2011-06-16
MX2012006653A (es) 2012-11-30
US8859605B2 (en) 2014-10-14
EP2509956B1 (en) 2014-07-23
EP2509957A4 (en) 2013-05-22
AU2010329468B2 (en) 2013-08-22
EP2509957A1 (en) 2012-10-17
CN102834383A (zh) 2012-12-19
AU2010329470A1 (en) 2012-06-14
US20120309673A1 (en) 2012-12-06
WO2011070541A1 (en) 2011-06-16
IN2012DN04914A (ru) 2015-09-25
BR112012013861A2 (pt) 2017-09-26
KR20120110173A (ko) 2012-10-09
AU2010329468A1 (en) 2012-06-14
MX2012006652A (es) 2012-11-30
BR112012014091A2 (pt) 2017-04-04
AU2010329470B2 (en) 2013-08-22
RU2012128859A (ru) 2014-01-20
CA2782292A1 (en) 2011-06-16
US8815809B2 (en) 2014-08-26
WO2011070539A1 (en) 2011-06-16
US20120283305A1 (en) 2012-11-08
CN102858751A (zh) 2013-01-02
KR20120093423A (ko) 2012-08-22

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