CN102947295B - 作为11β-HSD1抑制剂的3,3-二取代的-(8-氮杂双环[3.2.1]辛烷-8-基)-[5-(1H-吡唑-4基)-噻吩-3-基]-甲酮 - Google Patents
作为11β-HSD1抑制剂的3,3-二取代的-(8-氮杂双环[3.2.1]辛烷-8-基)-[5-(1H-吡唑-4基)-噻吩-3-基]-甲酮 Download PDFInfo
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- 0 CN1C2CC(*)(*)CC1CC2 Chemical compound CN1C2CC(*)(*)CC1CC2 0.000 description 6
- FPUWZCRNPFGOPF-DEUQGVHJSA-N CCC(/C=C\C/C(/NC(OC(C)(C)C)=O)=C\C)O Chemical compound CCC(/C=C\C/C(/NC(OC(C)(C)C)=O)=C\C)O FPUWZCRNPFGOPF-DEUQGVHJSA-N 0.000 description 1
- WQDGWDUYAKPQCZ-ZLYUWLSTSA-N CCC(C(C1)C2CC1(/C(/C(CC)=C)=N/C=C\C)O)N2C(OC(C)(C)C)=O Chemical compound CCC(C(C1)C2CC1(/C(/C(CC)=C)=N/C=C\C)O)N2C(OC(C)(C)C)=O WQDGWDUYAKPQCZ-ZLYUWLSTSA-N 0.000 description 1
- NMUYMJWEFIXNCH-UHFFFAOYSA-N CCC(C(C1)C2CC1(c1c[s]cn1)O)N2C(OC(C)(C)I)=O Chemical compound CCC(C(C1)C2CC1(c1c[s]cn1)O)N2C(OC(C)(C)I)=O NMUYMJWEFIXNCH-UHFFFAOYSA-N 0.000 description 1
- YJBJHKKREAOVRX-UHFFFAOYSA-N CCC1N(Cc2ccccc2)C(CO)CC1 Chemical compound CCC1N(Cc2ccccc2)C(CO)CC1 YJBJHKKREAOVRX-UHFFFAOYSA-N 0.000 description 1
- FKGXSLVMPDNWQV-VOMCLLRMSA-N CCCC(CC)(C1N(C)C[C@@H](C)N1)[O]=C Chemical compound CCCC(CC)(C1N(C)C[C@@H](C)N1)[O]=C FKGXSLVMPDNWQV-VOMCLLRMSA-N 0.000 description 1
- KJUJJBXVDKYAND-UHNVWZDZSA-N C[C@H]1N=CC=N[C@@H]1I Chemical compound C[C@H]1N=CC=N[C@@H]1I KJUJJBXVDKYAND-UHNVWZDZSA-N 0.000 description 1
- NJFLAHOWIWGYFO-UHFFFAOYSA-N OC(C1)(CC23C1N(CC1=CC=CCC1)C2CC3)c1nccnc1 Chemical compound OC(C1)(CC23C1N(CC1=CC=CCC1)C2CC3)c1nccnc1 NJFLAHOWIWGYFO-UHFFFAOYSA-N 0.000 description 1
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32945310P | 2010-04-29 | 2010-04-29 | |
| US61/329,453 | 2010-04-29 | ||
| PCT/GB2011/000345 WO2011135276A1 (en) | 2010-04-29 | 2011-03-10 | 3, 3 -disubstituted- ( 8 - aza - bicyclo [3.2.1] oct- 8 - yl) -[5- (1h - pyrazol - 4 -yl) -thiophen-3 -yl] methanones as inhibitors of 11 (beta) -hsd1 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102947295A CN102947295A (zh) | 2013-02-27 |
| CN102947295B true CN102947295B (zh) | 2016-01-20 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201180031564.6A Active CN102947295B (zh) | 2010-04-29 | 2011-03-10 | 作为11β-HSD1抑制剂的3,3-二取代的-(8-氮杂双环[3.2.1]辛烷-8-基)-[5-(1H-吡唑-4基)-噻吩-3-基]-甲酮 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US9365564B2 (https=) |
| EP (1) | EP2563780B1 (https=) |
| JP (1) | JP5899202B2 (https=) |
| KR (1) | KR101714820B1 (https=) |
| CN (1) | CN102947295B (https=) |
| AU (1) | AU2011247116B2 (https=) |
| BR (1) | BR112012027640B1 (https=) |
| CA (1) | CA2796297C (https=) |
| DK (1) | DK2563780T3 (https=) |
| ES (1) | ES2543692T3 (https=) |
| IL (1) | IL222417A (https=) |
| MX (1) | MX344142B (https=) |
| RU (1) | RU2593753C2 (https=) |
| WO (1) | WO2011135276A1 (https=) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0724251D0 (en) | 2007-12-12 | 2008-02-06 | Univ Edinburgh | Therapeutic compounds and their use |
| GB0804685D0 (en) | 2008-03-13 | 2008-04-16 | Univ Edinburgh | Therapeutic compounds and their use |
| EP2477983B1 (en) | 2009-09-16 | 2015-04-15 | The University Of Edinburgh | (4-phenyl-piperidin-1-yl)-[5-1h-pyrazol-4yl)-thiophen-3-yl]-methanone compounds and their use |
| WO2011135276A1 (en) | 2010-04-29 | 2011-11-03 | The University Of Edinburgh | 3, 3 -disubstituted- ( 8 - aza - bicyclo [3.2.1] oct- 8 - yl) -[5- (1h - pyrazol - 4 -yl) -thiophen-3 -yl] methanones as inhibitors of 11 (beta) -hsd1 |
| FR2993563B1 (fr) * | 2012-07-20 | 2015-12-18 | Metabrain Res | Derives de thiophenes utiles dans le traitement du diabete |
| WO2015131773A1 (zh) * | 2014-03-06 | 2015-09-11 | 上海海雁医药科技有限公司 | 作为食欲素受体拮抗剂的哌啶衍生物 |
| FR3035326B1 (fr) * | 2015-04-21 | 2017-05-12 | Pf Medicament | Utilisation de la (4-hydroxy-2-methyl-1,1-dioxido-2h-benzo[e][1,2]thiazin-3-yl)(naphtalen-2-yl)methanone dans la prevention et/ou le traitement de la steatohepatite non-alcoolique |
| CN104961698A (zh) * | 2015-07-13 | 2015-10-07 | 佛山市赛维斯医药科技有限公司 | 末端硝基取代的三氮唑亚砜类化合物、其制备方法及其用途 |
| CN104974080A (zh) * | 2015-07-19 | 2015-10-14 | 佛山市赛维斯医药科技有限公司 | 二吡啶叔醇结构的11β-HSD1抑制剂、制备方法及其用途 |
| CN104945315A (zh) * | 2015-07-19 | 2015-09-30 | 佛山市赛维斯医药科技有限公司 | 一类硝基二吡啶叔醇结构的11β-HSD1抑制剂及其用途 |
| CN104961677A (zh) * | 2015-07-19 | 2015-10-07 | 佛山市赛维斯医药科技有限公司 | 一类腈基二吡啶叔醇结构的11β-HSD1抑制剂及其用途 |
| EP3373920A4 (en) | 2015-11-13 | 2019-07-17 | Pietro Paolo Sanna | METHOD AND COMPOSITIONS FOR TREATING ALCOHOL CONSUMPTION MALFUNCTIONS |
| EA202092441A1 (ru) | 2016-06-07 | 2021-05-21 | Джакобио Фармасьютикалс Ко., Лтд. | Новые гетероциклические производные, применимые в качестве ингибиторов shp2 |
| KR20240026521A (ko) | 2017-03-23 | 2024-02-28 | 자코바이오 파마슈티칼스 컴퍼니 리미티드 | Shp2 억제제로서 유용한 신규한 헤테로환형 유도체 |
| CN112839935A (zh) | 2018-09-26 | 2021-05-25 | 北京加科思新药研发有限公司 | 可用作shp2抑制剂的新型杂环衍生物 |
| TW202523658A (zh) * | 2019-05-24 | 2025-06-16 | 美商賽吉醫療公司 | 化合物、組合物及使用方法 |
| MX2022003845A (es) * | 2019-09-30 | 2022-06-22 | Actinogen Medical Ltd | Tratamientos cognitivos medicinales. |
| WO2022051565A1 (en) * | 2020-09-04 | 2022-03-10 | Ikena Oncology, Inc. | Substituted 4-piperidinyl-quinazolines, 4-piperidinyl-pyrimidine-2-amines, and related compounds and their use in treating medical conditions |
| US12029718B2 (en) | 2021-11-09 | 2024-07-09 | Cct Sciences, Llc | Process for production of essentially pure delta-9-tetrahydrocannabinol |
| WO2022094668A1 (en) * | 2020-11-06 | 2022-05-12 | Actinogen Medical Limited | Process for preparing heterocyclic methanone compounds and aza-bicyclo intermediates thereof |
| JP2023550654A (ja) * | 2020-11-25 | 2023-12-04 | セージ セラピューティクス, インコーポレイテッド | 神経変性障害の治療のためのcyp46a1阻害剤としての4-フルオロ-(4-(4-ベンジル)ピペリジン-1-イル)(2-(ピリミジン-4-イル)ピリジン-3-イル)メタノン誘導体および類似化合物 |
| JP2025519558A (ja) * | 2022-06-10 | 2025-06-26 | アクチノゲン メディカル リミテッド | 抗うつ薬抵抗性対象の治療 |
| CN115073422A (zh) * | 2022-07-28 | 2022-09-20 | 成都普瑞熙药业有限公司 | 一种制备4-(1-甲基-1h-吡唑-5-基)哌啶及其盐的方法 |
| CN120153257A (zh) * | 2022-10-07 | 2025-06-13 | 射线质医疗有限公司 | 用于11β-HSD1抑制剂治疗的受试者选择 |
| CN120957989A (zh) * | 2023-03-02 | 2025-11-14 | 射线质医疗有限公司 | 用于制备氮杂双环杂芳基化合物的流动化学工艺 |
| WO2025073002A1 (en) * | 2023-10-03 | 2025-04-10 | Actinogen Medical Limited | Tablet formulation |
| GB202408335D0 (en) | 2024-06-11 | 2024-07-24 | Astrazeneca Ab | Therapies for wound treatment |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101243074A (zh) * | 2005-06-08 | 2008-08-13 | 日本烟草产业株式会社 | 杂环化合物 |
| WO2009074789A1 (en) * | 2007-12-12 | 2009-06-18 | The University Of Edinburgh | Amido-thiophene compounds and their use as 11-beta-hsd1 inhibitors |
| WO2009112845A1 (en) * | 2008-03-13 | 2009-09-17 | The University Of Edinburgh | Amido-thiophene compounds and their use |
| WO2010023161A1 (en) * | 2008-08-25 | 2010-03-04 | Boehringer Ingelheim International Gmbh | Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use |
| CN101848910A (zh) * | 2007-11-05 | 2010-09-29 | 默克专利股份公司 | 作为选择性11-β-羟基类固醇脱氢酶1型抑制剂的7-氮杂吲哚衍生物 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5087631A (en) | 1990-12-18 | 1992-02-11 | Glaxo Inc. | Oxathi(SIV)azol-5-one compounds |
| AR011913A1 (es) | 1997-03-06 | 2000-09-13 | Yamano Masaki | Derivados de 4,4-difluoro-2,3,4,5-tetrahidro-1h-1-benzoazepina y composiciones farmaceuticas de los mismos. |
| US6303593B1 (en) | 1999-03-02 | 2001-10-16 | Merck & Co., Inc. | 3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity |
| AU2002353716A1 (en) | 2001-11-22 | 2003-06-10 | Biovitrum Ab | Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1 |
| SE0202430D0 (sv) | 2002-08-14 | 2002-08-14 | Astrazeneca Ab | New Compounds |
| US7700583B2 (en) | 2003-04-11 | 2010-04-20 | High Point Pharmaceuticals, Llc | 11β-hydroxysteroid dehydrogenase type 1 active compounds |
| GB0325745D0 (en) | 2003-11-05 | 2003-12-10 | Astrazeneca Ab | Chemical compounds |
| GB0326029D0 (en) | 2003-11-07 | 2003-12-10 | Astrazeneca Ab | Chemical compounds |
| RU2006146608A (ru) | 2004-06-09 | 2008-07-20 | Ф.Хоффманн-Ля Рош Аг (Ch) | ОКТАГИДРОПИРРОЛО[3,4-с]-ПРОИЗВОДНЫЕ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ПРОТИВОВИРУСНЫХ АГЕНТОВ |
| EP1894919B1 (en) | 2005-06-07 | 2012-03-28 | Shionogi & Co., Ltd. | Heterocyclic compound having type i 11 beta hydroxysteroid dehydrogenase inhibitory activity |
| EP1889842A4 (en) | 2005-06-08 | 2009-07-29 | Japan Tobacco Inc | HETEROCYCLIC CONNECTION |
| US7803806B2 (en) | 2005-11-03 | 2010-09-28 | Sgx Pharmaceuticals, Inc. | Pyrimidinyl-thiophene kinase modulators |
| BRPI0710479A2 (pt) | 2006-01-18 | 2012-08-14 | Hoffmann La Roche | composto, processo para sua preparaÇço, composiÇço farmacÊutica, uso de um composto e mÉtodo de tratamento de doenÇa ou desosrdem metabàlica. |
| CN101484424B (zh) | 2006-02-28 | 2014-05-14 | 达特神经科学(开曼)有限公司 | 治疗化合物 |
| UA95480C2 (uk) | 2006-06-08 | 2011-08-10 | Елі Ліллі Енд Компані | Заміщені карбоксаміди |
| TW200811170A (en) * | 2006-06-27 | 2008-03-01 | Sanofi Aventis | Urea derivatives of tropane, their preparation and their therapeutic application |
| US7666888B2 (en) | 2006-07-20 | 2010-02-23 | Amgen Inc. | Substituted azole aromatic heterocycles as inhibitors of 11β-HSD-1 |
| US20100022590A1 (en) | 2008-01-17 | 2010-01-28 | Biovitrum Ab (Publ.) | Novel compounds |
| EP2443113A1 (en) | 2009-06-15 | 2012-04-25 | The University Of Edinburgh | Amido-isothiazole compounds and their use as inhibitors of 11beta-hsd1 for the treatment of metabolic syndrome and related disorders |
| EP2477983B1 (en) | 2009-09-16 | 2015-04-15 | The University Of Edinburgh | (4-phenyl-piperidin-1-yl)-[5-1h-pyrazol-4yl)-thiophen-3-yl]-methanone compounds and their use |
| WO2011135276A1 (en) | 2010-04-29 | 2011-11-03 | The University Of Edinburgh | 3, 3 -disubstituted- ( 8 - aza - bicyclo [3.2.1] oct- 8 - yl) -[5- (1h - pyrazol - 4 -yl) -thiophen-3 -yl] methanones as inhibitors of 11 (beta) -hsd1 |
-
2011
- 2011-03-10 WO PCT/GB2011/000345 patent/WO2011135276A1/en not_active Ceased
- 2011-03-10 MX MX2012012413A patent/MX344142B/es active IP Right Grant
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- 2012-10-14 IL IL222417A patent/IL222417A/en active IP Right Grant
-
2016
- 2016-05-13 US US15/154,254 patent/US9834549B2/en active Active
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101243074A (zh) * | 2005-06-08 | 2008-08-13 | 日本烟草产业株式会社 | 杂环化合物 |
| CN101848910A (zh) * | 2007-11-05 | 2010-09-29 | 默克专利股份公司 | 作为选择性11-β-羟基类固醇脱氢酶1型抑制剂的7-氮杂吲哚衍生物 |
| WO2009074789A1 (en) * | 2007-12-12 | 2009-06-18 | The University Of Edinburgh | Amido-thiophene compounds and their use as 11-beta-hsd1 inhibitors |
| WO2009112845A1 (en) * | 2008-03-13 | 2009-09-17 | The University Of Edinburgh | Amido-thiophene compounds and their use |
| WO2010023161A1 (en) * | 2008-08-25 | 2010-03-04 | Boehringer Ingelheim International Gmbh | Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use |
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| JP5899202B2 (ja) | 2016-04-06 |
| JP2013527162A (ja) | 2013-06-27 |
| CA2796297C (en) | 2017-09-05 |
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| US20160251346A1 (en) | 2016-09-01 |
| AU2011247116B2 (en) | 2015-12-03 |
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| US9834549B2 (en) | 2017-12-05 |
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| AU2011247116A1 (en) | 2012-11-22 |
| DK2563780T3 (en) | 2015-07-27 |
| CA2796297A1 (en) | 2011-11-03 |
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