EA201291469A1 - Новые ингибиторы протеазы - катепсина s, предназначенные для лечения, в частности, аутоиммунных расстройств, аллергии и состояний хронической боли - Google Patents
Новые ингибиторы протеазы - катепсина s, предназначенные для лечения, в частности, аутоиммунных расстройств, аллергии и состояний хронической болиInfo
- Publication number
- EA201291469A1 EA201291469A1 EA201291469A EA201291469A EA201291469A1 EA 201291469 A1 EA201291469 A1 EA 201291469A1 EA 201291469 A EA201291469 A EA 201291469A EA 201291469 A EA201291469 A EA 201291469A EA 201291469 A1 EA201291469 A1 EA 201291469A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- alkoxy
- alkyl
- haloalkyl
- katepsin
- allergy
- Prior art date
Links
- 208000023275 Autoimmune disease Diseases 0.000 title 1
- 208000000094 Chronic Pain Diseases 0.000 title 1
- 206010020751 Hypersensitivity Diseases 0.000 title 1
- 208000002193 Pain Diseases 0.000 title 1
- 208000026935 allergic disease Diseases 0.000 title 1
- 230000007815 allergy Effects 0.000 title 1
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 8
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 108090000613 Cathepsin S Proteins 0.000 abstract 1
- 102100035654 Cathepsin S Human genes 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
Classifications
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
- C07D233/61—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
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- C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
- C07C237/14—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being saturated and containing rings
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
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- A61K38/00—Medicinal preparations containing peptides
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- C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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Abstract
Соединение формулы (I), где Rи Rнезависимо обозначают Н, атом галогена, С-Салкил, С-Сгалогеналкил или С-Салкокси или же Rи Rвместе с атомом углерода, к которому они присоединены, образуют С-Сциклоалкил; Rобозначает С-Салкил, необязательно замещенный 1-3 заместителями, независимо выбранными из атома галогена, С-Сгалогеналкила, С-Салкокси, С-Сгалогеналкокси; или Rобозначает C-Салкильную цепь, содержащую в качестве заместителей по меньшей мере 2 атома хлора или 3 атома фтора; или Rобозначает С-Сциклоалкилметил, необязательно замещенный 1-3 заместителями, независимо выбранными из C-Салкила, атома галогена, С-Сгалогеналкила, С-Салкокси, C-Сгалогеналкокси; Rобозначает С-Салкил, C-Сгалогеналкил, С-Салкокси, С-Сгалогеналкокси, C-Салкиламино, С-Сциалкиламино; или Rобозначает Het или карбоциклил, любой из которых необязательно замещен 1-3 заместителями; n принимает значение 1, 2 или 3; для применения для профилактики или лечения расстройства, которое характеризуется отклоняющейся от нормы экспрессией или активацией катепсина S.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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SE1050618 | 2010-06-16 | ||
PCT/IB2011/052613 WO2011158197A1 (en) | 2010-06-16 | 2011-06-16 | New cathepsin s protease inhibitors, useful in the treatment of e.g. autoimmune disorders, allergy and chronic pain conditions |
Publications (1)
Publication Number | Publication Date |
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EA201291469A1 true EA201291469A1 (ru) | 2013-05-30 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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EA201291469A EA201291469A1 (ru) | 2010-06-16 | 2011-06-16 | Новые ингибиторы протеазы - катепсина s, предназначенные для лечения, в частности, аутоиммунных расстройств, аллергии и состояний хронической боли |
Country Status (13)
Country | Link |
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US (2) | US8859505B2 (ru) |
EP (2) | EP2752404A1 (ru) |
JP (1) | JP2013534917A (ru) |
KR (1) | KR20130087504A (ru) |
CN (1) | CN102971286B (ru) |
AU (1) | AU2011266626B2 (ru) |
BR (1) | BR112012028804A2 (ru) |
CA (1) | CA2798150A1 (ru) |
EA (1) | EA201291469A1 (ru) |
IL (1) | IL223065A (ru) |
MX (1) | MX2012014830A (ru) |
PH (1) | PH12014501958A1 (ru) |
WO (1) | WO2011158197A1 (ru) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2358692A4 (en) * | 2008-12-19 | 2012-06-27 | Medivir Uk Ltd | CYSTEINE PROTEASE INHIBITORS |
WO2012172473A1 (en) * | 2011-06-13 | 2012-12-20 | Medivir Uk Ltd | Cysteine protease inhibitors |
Family Cites Families (15)
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US5650508A (en) * | 1991-12-27 | 1997-07-22 | Georgia Tech Research Corporation | Peptide ketoamides |
CA2251714A1 (en) | 1996-04-22 | 1997-10-30 | Massachusetts Institute Of Technology | Suppression of immune response via inhibition of cathepsin s |
GB9809664D0 (en) * | 1998-05-06 | 1998-07-01 | Hoffmann La Roche | a-Ketoamide derivatives |
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 |
US20030144234A1 (en) | 2001-08-30 | 2003-07-31 | Buxton Francis Paul | Methods for the treatment of chronic pain and compositions therefor |
EP1829179B1 (en) | 2004-12-13 | 2009-03-25 | Novar ED&S Ltd | Fitting for joining cable trunking units |
WO2006064286A1 (en) | 2004-12-13 | 2006-06-22 | Medivir Uk Ltd | Cathepsin s inhibitors |
SI1865940T1 (sl) * | 2005-03-21 | 2013-03-29 | Virobay, Inc. | Alfa ketoamidne spojine kot inhibitorji cistein proteaze |
EP1866276A1 (en) * | 2005-03-21 | 2007-12-19 | Celera Genomics | Alpha ketoamide compounds as cysteine protease inhibitors |
CA2602175C (en) * | 2005-03-21 | 2012-11-27 | Applera Corporation | Alpha ketoamide compounds as cysteine protease inhibitors |
US20100074867A1 (en) * | 2007-03-23 | 2010-03-25 | Schering Corporation Patent Department, K-6-1; 1990 | P1-nonepimerizable ketoamide inhibitors of hcv ns3 protease |
WO2009055467A2 (en) * | 2007-10-24 | 2009-04-30 | Virobay, Inc. | Compounds that inhibit protease cathepsin s and hcv replication |
EP2358692A4 (en) * | 2008-12-19 | 2012-06-27 | Medivir Uk Ltd | CYSTEINE PROTEASE INHIBITORS |
KR20120093423A (ko) * | 2009-12-10 | 2012-08-22 | 메디버 유케이 리미티드 | 시스테인 프로테아제 억제제 |
WO2012168852A1 (en) * | 2011-06-08 | 2012-12-13 | Medivir Uk Ltd | Cysteine protease inhibitors |
-
2011
- 2011-06-16 BR BR112012028804A patent/BR112012028804A2/pt not_active IP Right Cessation
- 2011-06-16 CN CN201180027599.2A patent/CN102971286B/zh not_active Expired - Fee Related
- 2011-06-16 CA CA2798150A patent/CA2798150A1/en not_active Abandoned
- 2011-06-16 AU AU2011266626A patent/AU2011266626B2/en not_active Ceased
- 2011-06-16 US US13/704,441 patent/US8859505B2/en not_active Expired - Fee Related
- 2011-06-16 JP JP2013514827A patent/JP2013534917A/ja not_active Ceased
- 2011-06-16 KR KR1020137001100A patent/KR20130087504A/ko not_active Application Discontinuation
- 2011-06-16 EP EP14162956.8A patent/EP2752404A1/en not_active Withdrawn
- 2011-06-16 EA EA201291469A patent/EA201291469A1/ru unknown
- 2011-06-16 MX MX2012014830A patent/MX2012014830A/es active IP Right Grant
- 2011-06-16 WO PCT/IB2011/052613 patent/WO2011158197A1/en active Application Filing
- 2011-06-16 EP EP11795278.8A patent/EP2582660B1/en active Active
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2012
- 2012-11-15 IL IL223065A patent/IL223065A/en not_active IP Right Cessation
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2014
- 2014-09-01 PH PH12014501958A patent/PH12014501958A1/en unknown
- 2014-10-02 US US14/504,419 patent/US20150025250A1/en not_active Abandoned
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EP2752404A1 (en) | 2014-07-09 |
US20130172232A1 (en) | 2013-07-04 |
CN102971286A (zh) | 2013-03-13 |
MX2012014830A (es) | 2013-01-29 |
EP2582660A1 (en) | 2013-04-24 |
US8859505B2 (en) | 2014-10-14 |
US20150025250A1 (en) | 2015-01-22 |
BR112012028804A2 (pt) | 2016-07-26 |
CN102971286B (zh) | 2015-08-26 |
PH12014501958A1 (en) | 2015-09-21 |
EP2582660B1 (en) | 2015-07-22 |
IL223065A (en) | 2015-05-31 |
WO2011158197A1 (en) | 2011-12-22 |
JP2013534917A (ja) | 2013-09-09 |
KR20130087504A (ko) | 2013-08-06 |
EP2582660A4 (en) | 2013-11-27 |
CA2798150A1 (en) | 2011-12-22 |
AU2011266626B2 (en) | 2014-10-23 |
IL223065A0 (en) | 2013-02-03 |
AU2011266626A1 (en) | 2013-01-31 |
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