EA201071288A1 - Тризамещенные пиразолы в качестве модуляторов рецепторов ацетилхолина - Google Patents
Тризамещенные пиразолы в качестве модуляторов рецепторов ацетилхолинаInfo
- Publication number
- EA201071288A1 EA201071288A1 EA201071288A EA201071288A EA201071288A1 EA 201071288 A1 EA201071288 A1 EA 201071288A1 EA 201071288 A EA201071288 A EA 201071288A EA 201071288 A EA201071288 A EA 201071288A EA 201071288 A1 EA201071288 A1 EA 201071288A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- acetylcholine receptors
- modulators
- pyrazoles
- triple
- relates
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic 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
- C07D231/14—Heterocyclic 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
- C07D231/38—Nitrogen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Abstract
Настоящее изобретение относится к производным 1-алкил-3-анилин-5-арилпиразола формулы (I) и к их фармацевтически приемлемым солям, способам их получения, фармацевтическим композициям, их содержащих, и к их применению в терапии. В особенности, изобретение относится к положительным аллостерическим модуляторам никотиновых рецепторов ацетилхолина, проявляющим способность повышать эффективность агонистов никотиновых рецепторов.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP08155991 | 2008-05-09 | ||
PCT/EP2009/055617 WO2009135944A1 (en) | 2008-05-09 | 2009-05-08 | Trisubstituted pyrazoles as acetylcholine receptor modulators |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201071288A1 true EA201071288A1 (ru) | 2011-04-29 |
EA018187B1 EA018187B1 (ru) | 2013-06-28 |
Family
ID=39800623
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201071288A EA018187B1 (ru) | 2008-05-09 | 2009-05-08 | Тризамещенные пиразолы в качестве модуляторов рецепторов ацетилхолина |
Country Status (14)
Country | Link |
---|---|
US (1) | US8779158B2 (ru) |
EP (1) | EP2280945B1 (ru) |
JP (1) | JP5486591B2 (ru) |
KR (1) | KR20110007234A (ru) |
CN (1) | CN102015655A (ru) |
AR (1) | AR071763A1 (ru) |
AU (1) | AU2009245715B2 (ru) |
BR (1) | BRPI0912196A2 (ru) |
CA (1) | CA2722805A1 (ru) |
CL (1) | CL2009001125A1 (ru) |
EA (1) | EA018187B1 (ru) |
ES (1) | ES2525132T3 (ru) |
TW (1) | TWI440634B (ru) |
WO (1) | WO2009135944A1 (ru) |
Families Citing this family (25)
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CN101827836B (zh) * | 2007-10-18 | 2014-02-19 | 詹森药业有限公司 | 三取代的1,2,4-三唑化合物 |
JO2784B1 (en) * | 2007-10-18 | 2014-03-15 | شركة جانسين فارماسوتيكا ان. في | 5,3,1 - Triazole substitute derivative |
MY152486A (en) * | 2008-03-19 | 2014-10-15 | Janssen Pharmaceutica Nv | Trisubstituted 1,2,4 - triazoles as nicotinic acetylcholine receptor modulators |
FR2931677B1 (fr) * | 2008-06-02 | 2010-08-20 | Sanofi Aventis | Association d'un agoniste partiel des recepteurs nicotiniques et d'un inhibiteur d'acetylcholinesterase, composition la contenant et son utilisation dans le traitement des troubles cognitifs |
KR101710197B1 (ko) * | 2009-09-17 | 2017-02-24 | 얀센 파마슈티카 엔.브이. | 치환된 n-페닐-1-(4-피리디닐)-1h-피라졸-3-아민 |
WO2012104782A1 (en) | 2011-02-03 | 2012-08-09 | Lupin Limited | Pyrrole derivatives used as modulators of alpha7 nachr |
PL2678327T3 (pl) | 2011-02-23 | 2017-02-28 | Lupin Limited | Pochodne heteroarylowe jako modulatory Alfa 7 NACHR |
WO2012113850A2 (en) * | 2011-02-25 | 2012-08-30 | Janssen Pharmaceutica Nv | (PYRIDIN-4-YL)BENZYLAMIDES AS ALLOSTERIC MODULATORS OF ALPHA 7 nAChR |
US9187420B2 (en) | 2011-03-31 | 2015-11-17 | Lupin Limited | Pyrrole derivatives as nicotinic acetylcholine receptor modulators for use in the treatment of neurodegenerative disorders such as alzheimer's and parkinson's disease |
WO2013005153A1 (en) | 2011-07-05 | 2013-01-10 | Lupin Limited | Biaryl derivatives as nachr modulators |
JP6042896B2 (ja) | 2011-10-06 | 2016-12-14 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH | 殺菌剤としての複素環ピリ(ミ)ジニルピラゾール |
WO2013132380A1 (en) | 2012-03-06 | 2013-09-12 | Lupin Limited | Thiazole derivatives as alpha 7 nachr modulators |
WO2014072957A1 (en) | 2012-11-12 | 2014-05-15 | Lupin Limited | Thiazole derivatives as alpha 7 nachr modulators |
WO2014111839A1 (en) | 2013-01-16 | 2014-07-24 | Lupin Limited | Pyrrole derivatives as alpha 7 nachr modulators |
AU2014229300A1 (en) | 2013-03-13 | 2015-06-11 | Lupin Limited | Pyrrole derivatives as alpha 7 nAChR modulators |
TW201446243A (zh) | 2013-06-03 | 2014-12-16 | Lupin Ltd | 4-(5-(4-氯苯基)-2-(2-環丙基乙醯基)-1,4-二甲基-1氫-吡咯-3-基)苯磺醯胺作為α7尼古丁乙醯膽鹼受體調節劑 |
AU2014282886A1 (en) | 2013-06-17 | 2015-12-17 | Lupin Limited | Pyrrole derivatives as alpha 7 nAChR modulators |
WO2017107089A1 (en) * | 2015-12-23 | 2017-06-29 | Merck Sharp & Dohme Corp. | 3- (1h-pyrazol-4-yl) pyridineallosteric modulators of the m4 muscarinic acetylcholine receptor |
WO2019000237A1 (en) * | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
WO2019000238A1 (en) * | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | 5- (PYRIDIN-3-YL) OXAZOLE ALLOSTERIC MODULATORS OF M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
WO2019000236A1 (en) * | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
CN107652204A (zh) * | 2017-09-30 | 2018-02-02 | 山东理工大学 | 一种环氧化物接枝肼还原制备及分散石墨烯的方法 |
HU231333B1 (hu) | 2018-07-13 | 2023-01-28 | Richter Gedeon Nyrt | Spirokromán származékok |
HU231478B1 (hu) | 2018-07-13 | 2024-02-28 | Richter Gedeon Nyrt. | Szubsztituált (aza)indol származékok |
HU231414B1 (hu) | 2018-07-13 | 2023-08-28 | Richter Gedeon Nyrt. | Tiadiazin származékok |
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MY152486A (en) | 2008-03-19 | 2014-10-15 | Janssen Pharmaceutica Nv | Trisubstituted 1,2,4 - triazoles as nicotinic acetylcholine receptor modulators |
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KR101710197B1 (ko) | 2009-09-17 | 2017-02-24 | 얀센 파마슈티카 엔.브이. | 치환된 n-페닐-1-(4-피리디닐)-1h-피라졸-3-아민 |
JO3078B1 (ar) | 2009-11-27 | 2017-03-15 | Janssen Pharmaceutica Nv | مورفولينوثيازولات بصفتها منظمات الوستيرية نوع الفا 7 موجبة |
WO2012113850A2 (en) | 2011-02-25 | 2012-08-30 | Janssen Pharmaceutica Nv | (PYRIDIN-4-YL)BENZYLAMIDES AS ALLOSTERIC MODULATORS OF ALPHA 7 nAChR |
-
2009
- 2009-05-08 WO PCT/EP2009/055617 patent/WO2009135944A1/en active Application Filing
- 2009-05-08 EP EP09742162.2A patent/EP2280945B1/en active Active
- 2009-05-08 CN CN2009801164538A patent/CN102015655A/zh active Pending
- 2009-05-08 CA CA2722805A patent/CA2722805A1/en not_active Abandoned
- 2009-05-08 TW TW098115214A patent/TWI440634B/zh not_active IP Right Cessation
- 2009-05-08 BR BRPI0912196A patent/BRPI0912196A2/pt not_active IP Right Cessation
- 2009-05-08 JP JP2011507940A patent/JP5486591B2/ja not_active Expired - Fee Related
- 2009-05-08 EA EA201071288A patent/EA018187B1/ru not_active IP Right Cessation
- 2009-05-08 KR KR1020107026864A patent/KR20110007234A/ko not_active Application Discontinuation
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- 2009-05-08 CL CL2009001125A patent/CL2009001125A1/es unknown
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Also Published As
Publication number | Publication date |
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EP2280945B1 (en) | 2014-09-03 |
CN102015655A (zh) | 2011-04-13 |
AU2009245715B2 (en) | 2014-01-09 |
TWI440634B (zh) | 2014-06-11 |
KR20110007234A (ko) | 2011-01-21 |
TW201006812A (en) | 2010-02-16 |
JP5486591B2 (ja) | 2014-05-07 |
BRPI0912196A2 (pt) | 2015-10-06 |
CL2009001125A1 (es) | 2011-02-11 |
AU2009245715A1 (en) | 2009-11-12 |
US8779158B2 (en) | 2014-07-15 |
EA018187B1 (ru) | 2013-06-28 |
WO2009135944A1 (en) | 2009-11-12 |
AR071763A1 (es) | 2010-07-14 |
US20110065683A1 (en) | 2011-03-17 |
ES2525132T3 (es) | 2014-12-17 |
JP2011519901A (ja) | 2011-07-14 |
EP2280945A1 (en) | 2011-02-09 |
CA2722805A1 (en) | 2009-11-12 |
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