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
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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
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- 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
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- 229940125670 thienopyridine Drugs 0.000 description 1
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- WZMPOCLULGAHJR-UHFFFAOYSA-N thiophen-2-ol Chemical compound OC1=CC=CS1 WZMPOCLULGAHJR-UHFFFAOYSA-N 0.000 description 1
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- 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
- 238000001665 trituration Methods 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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Landscapes
- Health & Medical Sciences (AREA)
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- Pulmonology (AREA)
- Hematology (AREA)
- Pregnancy & Childbirth (AREA)
- Cardiology (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)
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| PCT/US2007/078352 WO2008036541A1 (en) | 2006-09-20 | 2007-09-13 | Thiophene pyrazolopyrimidine compounds |
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| EA200970302A1 EA200970302A1 (ru) | 2009-10-30 |
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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 |
| US9029411B2 (en) | 2008-01-25 | 2015-05-12 | Millennium Pharmaceuticals, Inc. | Thiophenes and uses thereof |
| WO2010090716A1 (en) | 2009-01-30 | 2010-08-12 | Millennium Pharmaceuticals, Inc. | Heteroaryls and their use as 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 |
| WO2012021611A1 (en) | 2010-08-11 | 2012-02-16 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| US8859768B2 (en) | 2010-08-11 | 2014-10-14 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| TW201217365A (en) | 2010-08-11 | 2012-05-01 | Millennium Pharm Inc | Heteroaryls and uses thereof |
| TW201307309A (zh) | 2010-10-13 | 2013-02-16 | Millennium Pharm Inc | 雜芳基化合物及其用途 |
| EP2729455B1 (en) | 2011-07-05 | 2016-09-14 | Lupin Limited | Biaryl derivatives as nachr modulators |
| 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 |
| RS65839B1 (sr) | 2014-01-21 | 2024-09-30 | Neurocrine Biosciences Inc | Crf1 receptor antagonisti za tretman kongenitalne adrenalne hiperplazije |
| 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 |
| WO2019036503A1 (en) | 2017-08-14 | 2019-02-21 | Spruce Biosciences, Inc. | CORTICOTROPIN RELEASE FACTOR RECEPTOR ANTAGONISTS |
| JP7285222B2 (ja) * | 2017-08-14 | 2023-06-01 | スプルース バイオサイエンシズ インコーポレイテッド | 副腎皮質刺激ホルモン放出因子受容体拮抗薬 |
| EP4643950A3 (en) | 2018-04-27 | 2026-01-14 | Spruce Biosciences, Inc. | Methods for treating testicular and ovarian adrenal rest tumors |
| US20220023266A1 (en) | 2018-12-07 | 2022-01-27 | Neurocrine Biosciences, Inc. | Crf1 receptor antagonist, pharmaceutical formulations and solid forms thereof for the treatment of congenital adrenal hyperplasia |
| JP7623365B2 (ja) | 2019-09-27 | 2025-01-28 | ニューロクライン バイオサイエンシーズ，インコーポレイテッド | Ｃｒｆ受容体アンタゴニストおよび使用方法 |
| TW202134241A (zh) * | 2019-12-04 | 2021-09-16 | 美商紐羅克里生物科學有限公司 | Ｃｒｆ受體拮抗劑及使用方法 |
| KR20240023691A (ko) | 2020-08-12 | 2024-02-22 | 스프루스 바이오사이언시스 인코포레이티드 | 다낭성 난소 증후군을 치료하기 위한 방법 및 조성물 |
| 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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| KR19990067704A (ko) | 1992-12-17 | 1999-08-25 | 디. 제이. 우드, 스피겔 알렌 제이 | 부신피질자극호르몬 유리인자 길항제로서의 피롤로피리미딘을함유하는 약학 조성물 |
| HU229024B1 (en) | 1996-07-24 | 2013-07-29 | Bristol Myers Squibb Pharma Co | Azolo-pyridimidines, pharmaceutical compositions containing the same and use thereof |
| JP3621706B2 (ja) | 1996-08-28 | 2005-02-16 | ファイザー・インク | 置換された６，５―ヘテロ―二環式誘導体 |
| EP1869049B1 (en) * | 2005-03-21 | 2009-03-04 | Eli Lilly And Company | Imidazopyridazine compounds |
-
2007
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- 2007-09-13 EP EP07814842.6A patent/EP2076515B1/en not_active Not-in-force
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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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|---|---|
| JP2010504343A (ja) | 2010-02-12 |
| CN101516886B (zh) | 2012-02-29 |
| MX2009003098A (es) | 2009-04-01 |
| US8110580B2 (en) | 2012-02-07 |
| ES2428543T3 (es) | 2013-11-08 |
| CN101516886A (zh) | 2009-08-26 |
| AU2007297481A1 (en) | 2008-03-27 |
| KR101088196B1 (ko) | 2011-11-30 |
| EA200970302A1 (ru) | 2009-10-30 |
| CA2662000C (en) | 2013-01-08 |
| CA2662000A1 (en) | 2008-03-27 |
| KR20090053921A (ko) | 2009-05-28 |
| EP2076515A1 (en) | 2009-07-08 |
| JP5184536B2 (ja) | 2013-04-17 |
| BRPI0717070A2 (pt) | 2013-09-24 |
| WO2008036541A1 (en) | 2008-03-27 |
| AU2007297481B2 (en) | 2012-03-08 |
| EP2076515B1 (en) | 2013-07-17 |
| US20100022560A1 (en) | 2010-01-28 |
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