EA016056B1 - Тиофенпиразолопиримидиновые соединения - Google Patents
Тиофенпиразолопиримидиновые соединения Download PDFInfo
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- EA016056B1 EA016056B1 EA200970302A EA200970302A EA016056B1 EA 016056 B1 EA016056 B1 EA 016056B1 EA 200970302 A EA200970302 A EA 200970302A EA 200970302 A EA200970302 A EA 200970302A EA 016056 B1 EA016056 B1 EA 016056B1
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- EA
- Eurasian Patent Office
- Prior art keywords
- mmol
- hexane
- reaction
- formula
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- HDZGCSFEDULWCS-UHFFFAOYSA-N monomethylhydrazine Chemical compound CNN HDZGCSFEDULWCS-UHFFFAOYSA-N 0.000 description 1
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- UXCDUFKZSUBXGM-UHFFFAOYSA-N phosphoric tribromide Chemical compound BrP(Br)(Br)=O UXCDUFKZSUBXGM-UHFFFAOYSA-N 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
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- 230000003449 preventive effect Effects 0.000 description 1
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- JUXWUYWPUDKPSD-UHFFFAOYSA-N pyrazolo[1,5-a][1,3,5]triazine Chemical class N1=CN=CN2N=CC=C21 JUXWUYWPUDKPSD-UHFFFAOYSA-N 0.000 description 1
- LDIJKUBTLZTFRG-UHFFFAOYSA-N pyrazolo[1,5-a]pyrimidine Chemical class N1=CC=CN2N=CC=C21 LDIJKUBTLZTFRG-UHFFFAOYSA-N 0.000 description 1
- 238000010791 quenching Methods 0.000 description 1
- 230000000171 quenching effect Effects 0.000 description 1
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- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical compound C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 229940125670 thienopyridine Drugs 0.000 description 1
- 239000002175 thienopyridine Substances 0.000 description 1
- WZMPOCLULGAHJR-UHFFFAOYSA-N thiophen-2-ol Chemical compound OC1=CC=CS1 WZMPOCLULGAHJR-UHFFFAOYSA-N 0.000 description 1
- ARYHTUPFQTUBBG-UHFFFAOYSA-N thiophen-2-ylboronic acid Chemical compound OB(O)C1=CC=CS1 ARYHTUPFQTUBBG-UHFFFAOYSA-N 0.000 description 1
- CUPOOAWTRIURFT-UHFFFAOYSA-N thiophene-2-carbonitrile Chemical compound N#CC1=CC=CS1 CUPOOAWTRIURFT-UHFFFAOYSA-N 0.000 description 1
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- NHDIQVFFNDKAQU-UHFFFAOYSA-N tripropan-2-yl borate Chemical compound CC(C)OB(OC(C)C)OC(C)C NHDIQVFFNDKAQU-UHFFFAOYSA-N 0.000 description 1
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- QOEYTZPVSXRHCY-UHFFFAOYSA-M zinc;3-methyl-2h-thiophen-2-ide;bromide Chemical compound Br[Zn+].CC=1C=CS[C-]=1 QOEYTZPVSXRHCY-UHFFFAOYSA-M 0.000 description 1
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Classifications
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
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- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
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- Heart & Thoracic Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Pregnancy & Childbirth (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (2)
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| US82627306P | 2006-09-20 | 2006-09-20 | |
| PCT/US2007/078352 WO2008036541A1 (en) | 2006-09-20 | 2007-09-13 | Thiophene pyrazolopyrimidine compounds |
Publications (2)
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| EA200970302A1 EA200970302A1 (ru) | 2009-10-30 |
| EA016056B1 true EA016056B1 (ru) | 2012-01-30 |
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| EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| WO2009094224A1 (en) | 2008-01-25 | 2009-07-30 | Millennium Pharmaceuticals, Inc. | Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors |
| US8796314B2 (en) | 2009-01-30 | 2014-08-05 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| US9090601B2 (en) | 2009-01-30 | 2015-07-28 | Millennium Pharmaceuticals, Inc. | Thiazole derivatives |
| JP2012516329A (ja) | 2009-01-30 | 2012-07-19 | ミレニアム ファーマシューティカルズ， インコーポレイテッド | Ｐｉ３ｋ阻害剤としてのヘテロアリールおよびその使用 |
| EP2603214A4 (en) | 2010-08-11 | 2013-12-18 | Millennium Pharm Inc | HETEROARYLE AND USES THEREOF |
| US8859768B2 (en) | 2010-08-11 | 2014-10-14 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| US9062038B2 (en) | 2010-08-11 | 2015-06-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| MX2013004003A (es) | 2010-10-13 | 2013-10-01 | Millenium Pharmaceuticals Inc | Heteroarilos y usos de los mismos. |
| ES2606043T3 (es) | 2011-07-05 | 2017-03-17 | Lupin Limited | Derivados de biarilo como moduladores de nAChR |
| EP2567959B1 (en) | 2011-09-12 | 2014-04-16 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| KR20210064407A (ko) | 2014-01-21 | 2021-06-02 | 뉴로크린 바이오사이언시즈 인코퍼레이티드 | 선천성 부신 과형성 치료를 위한 ｃｒｆ1 수용체 길항제 |
| JP6364967B2 (ja) * | 2014-05-30 | 2018-08-01 | 東ソー株式会社 | ジチエノベンゾジチオフェンの製造方法 |
| EP3238676B1 (en) | 2016-04-29 | 2019-01-02 | The Procter and Gamble Company | Absorbent core with profiled distribution of absorbent material |
| BR112020002967A2 (pt) | 2017-08-14 | 2020-08-11 | Spruce Biosciences, Inc. | antagonistas de receptor de fator de liberação de corticotropina |
| TWI803504B (zh) * | 2017-08-14 | 2023-06-01 | 美商雲杉生物科技股份有限公司 | 促皮質素釋放因子受體拮抗劑 |
| MX2020011344A (es) | 2018-04-27 | 2021-02-09 | Spruce Biosciences Inc | Métodos para tratar tumores en reposo suprarrenales testiculares y de ovarios. |
| PL3984523T3 (pl) | 2018-12-07 | 2026-02-02 | Neurocrine Biosciences, Inc. | Antagonista receptora crf1, jego formulacje farmaceutyczne i postacie stałe do leczenia wrodzonego przerostu nadnerczy |
| US12383536B2 (en) | 2019-09-27 | 2025-08-12 | Neurocrine Biosciences, Inc. | CRF receptor antagonists and methods of use |
| ES3039926T3 (en) * | 2019-12-04 | 2025-10-27 | Neurocrine Biosciences Inc | Crf receptor antagonists and methods of use |
| JP2023537598A (ja) | 2020-08-12 | 2023-09-04 | スプルース バイオサイエンシーズ，インク． | 多嚢胞性卵巣症候群を処置するための方法および組成物 |
| US11708372B2 (en) | 2021-11-19 | 2023-07-25 | Spruce Biosciences, Inc. | Crystalline composition of tildacerfont and methods of use and preparation thereof |
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| WO1997029109A1 (en) * | 1996-02-07 | 1997-08-14 | Janssen Pharmaceutica N.V. | Pyrazolopyrimidines as crf receptor antagonists |
| WO2001023388A2 (en) * | 1999-09-30 | 2001-04-05 | Neurogen Corporation | AMINO SUBSTITUTED PYRAZOLO[1,5,-a]-1,5-PYRIMIDINES AND PYRAZOLO[1,5-a]-1,3,5-TRIAZINES |
| WO2005063755A1 (en) * | 2003-12-22 | 2005-07-14 | Sb Pharmco Puerto Rico Inc | Crf receptor antagonists and methods relating thereto |
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|---|---|---|---|---|
| BR9307646A (pt) | 1992-12-17 | 1999-05-25 | Pfizer | Pirrolopirimidinas como antagonistas de crf |
| AU747708B2 (en) | 1996-07-24 | 2002-05-23 | Du Pont Pharmaceuticals Company | Azolo triazines and pyrimidines |
| PL332040A1 (en) | 1996-08-28 | 1999-08-16 | Pfizer | Substitution 6,5-heterobicyclic derivatives |
| CN101142217B (zh) * | 2005-03-21 | 2010-12-08 | 伊莱利利公司 | 咪唑并哒嗪化合物 |
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| WO1997029109A1 (en) * | 1996-02-07 | 1997-08-14 | Janssen Pharmaceutica N.V. | Pyrazolopyrimidines as crf receptor antagonists |
| WO2001023388A2 (en) * | 1999-09-30 | 2001-04-05 | Neurogen Corporation | AMINO SUBSTITUTED PYRAZOLO[1,5,-a]-1,5-PYRIMIDINES AND PYRAZOLO[1,5-a]-1,3,5-TRIAZINES |
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Also Published As
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| BRPI0717070A2 (pt) | 2013-09-24 |
| CA2662000A1 (en) | 2008-03-27 |
| CN101516886B (zh) | 2012-02-29 |
| JP5184536B2 (ja) | 2013-04-17 |
| KR101088196B1 (ko) | 2011-11-30 |
| AU2007297481A1 (en) | 2008-03-27 |
| EA200970302A1 (ru) | 2009-10-30 |
| AU2007297481B2 (en) | 2012-03-08 |
| ES2428543T3 (es) | 2013-11-08 |
| WO2008036541A1 (en) | 2008-03-27 |
| US20100022560A1 (en) | 2010-01-28 |
| MX2009003098A (es) | 2009-04-01 |
| JP2010504343A (ja) | 2010-02-12 |
| CN101516886A (zh) | 2009-08-26 |
| KR20090053921A (ko) | 2009-05-28 |
| EP2076515A1 (en) | 2009-07-08 |
| US8110580B2 (en) | 2012-02-07 |
| CA2662000C (en) | 2013-01-08 |
| EP2076515B1 (en) | 2013-07-17 |
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