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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- 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
- 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
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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)
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- Medicinal Chemistry (AREA)
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- Pregnancy & Childbirth (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
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Applications Claiming Priority (2)
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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 |
| 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 |
| EP2250160B1 (en) | 2008-01-25 | 2015-11-11 | Millennium Pharmaceuticals, Inc. | Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors |
| 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 |
| US9062038B2 (en) | 2010-08-11 | 2015-06-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| UY33554A (es) | 2010-08-11 | 2012-02-29 | Millennium Pharm Inc | Heteroarilos y usos de los mismos |
| WO2012021615A1 (en) | 2010-08-11 | 2012-02-16 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| BR112013009166A2 (pt) | 2010-10-13 | 2016-07-26 | Millennium Pharm Inc | heteroarilas e uso das mesmas. |
| US8946432B2 (en) | 2011-07-05 | 2015-02-03 | 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 |
| CN106102740A (zh) | 2014-01-21 | 2016-11-09 | 纽罗克里生物科学有限公司 | 治疗先天性肾上腺增生的crf1受体拮抗剂 |
| 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 |
| CA3064445A1 (en) * | 2017-08-14 | 2019-02-21 | Spruce Biosciences, Inc. | Corticotropin releasing factor receptor antagonists |
| EP3984523B1 (en) | 2018-12-07 | 2025-09-03 | Neurocrine Biosciences, Inc. | Crf1 receptor antagonist, pharmaceutical formulations and solid forms thereof for the treatment of congenital adrenal hyperplasia |
| WO2021062246A1 (en) | 2019-09-27 | 2021-04-01 | Neurocrine Biosciences, Inc. | Crf receptor antagonists and methods of use |
| AR120649A1 (es) * | 2019-12-04 | 2022-03-09 | Neurocrine Biosciences Inc | Antagonistas del receptor de crf y métodos de uso |
| EP4175572A4 (en) | 2020-08-12 | 2024-03-27 | Spruce Biosciences, Inc. | Methods and compositions for treating polycystic ovary syndrome |
| US11708372B2 (en) | 2021-11-19 | 2023-07-25 | Spruce Biosciences, Inc. | Crystalline composition of tildacerfont and methods of use and preparation thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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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| ES2128544T3 (es) | 1992-12-17 | 1999-05-16 | Pfizer | Pirrolopirimidinas como antagonistas del crf. |
| ES2294800T3 (es) | 1996-07-24 | 2008-04-01 | Bristol-Myers Squibb Pharma Company | Azolo triazinas y pirimidinas. |
| BR9711970A (pt) | 1996-08-28 | 1999-08-24 | Pfizer | Derivados 6,5-substitu¡do-heterobic¡clicos |
| DK1869049T3 (da) * | 2005-03-21 | 2009-05-18 | Lilly Co Eli | Imidazopyridazinforbindelser |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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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| MX2009003098A (es) | 2009-04-01 |
| BRPI0717070A2 (pt) | 2013-09-24 |
| JP5184536B2 (ja) | 2013-04-17 |
| KR20090053921A (ko) | 2009-05-28 |
| EP2076515B1 (en) | 2013-07-17 |
| CN101516886A (zh) | 2009-08-26 |
| JP2010504343A (ja) | 2010-02-12 |
| AU2007297481A1 (en) | 2008-03-27 |
| EP2076515A1 (en) | 2009-07-08 |
| AU2007297481B2 (en) | 2012-03-08 |
| KR101088196B1 (ko) | 2011-11-30 |
| US20100022560A1 (en) | 2010-01-28 |
| EA200970302A1 (ru) | 2009-10-30 |
| ES2428543T3 (es) | 2013-11-08 |
| CN101516886B (zh) | 2012-02-29 |
| CA2662000C (en) | 2013-01-08 |
| US8110580B2 (en) | 2012-02-07 |
| CA2662000A1 (en) | 2008-03-27 |
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