JP2011513305A5 - - Google Patents
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- Publication number
- JP2011513305A5 JP2011513305A5 JP2010548719A JP2010548719A JP2011513305A5 JP 2011513305 A5 JP2011513305 A5 JP 2011513305A5 JP 2010548719 A JP2010548719 A JP 2010548719A JP 2010548719 A JP2010548719 A JP 2010548719A JP 2011513305 A5 JP2011513305 A5 JP 2011513305A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- pharmaceutically acceptable
- halo
- compound
- acceptable salt
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims 38
- 150000001875 compounds Chemical class 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 18
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 17
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 239000001257 hydrogen Substances 0.000 claims 11
- 125000005843 halogen group Chemical group 0.000 claims 9
- 125000006559 (C1-C3) alkylamino group Chemical group 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 5
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 3
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 3
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000006677 (C1-C3) haloalkoxy group Chemical group 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 2
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 2
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- 125000004434 sulfur atom Chemical group 0.000 claims 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 1
- 102000008645 11-beta-Hydroxysteroid Dehydrogenase Type 1 Human genes 0.000 claims 1
- 108010088011 11-beta-Hydroxysteroid Dehydrogenase Type 1 Proteins 0.000 claims 1
- 125000001963 4 membered heterocyclic group Chemical group 0.000 claims 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000006413 ring segment Chemical group 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 0 *c1c(C=CC(N(CC2)CCC22N(*)CCc3ccccc23)=O)cccc1 Chemical compound *c1c(C=CC(N(CC2)CCC22N(*)CCc3ccccc23)=O)cccc1 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US3197508P | 2008-02-27 | 2008-02-27 | |
| US61/031,975 | 2008-02-27 | ||
| PCT/US2009/001215 WO2009108332A1 (en) | 2008-02-27 | 2009-02-26 | INHIBITORS OF 11β -HYDROXYSTEROID DEHYDROGENASE TYPE 1 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011513305A JP2011513305A (ja) | 2011-04-28 |
| JP2011513305A5 true JP2011513305A5 (enExample) | 2012-04-05 |
| JP5451646B2 JP5451646B2 (ja) | 2014-03-26 |
Family
ID=40638089
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010548719A Expired - Fee Related JP5451646B2 (ja) | 2008-02-27 | 2009-02-26 | １１β−ヒドロキシステロイドデヒドロゲナーゼ１型の阻害剤 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8383629B2 (enExample) |
| EP (1) | EP2265588B1 (enExample) |
| JP (1) | JP5451646B2 (enExample) |
| CA (1) | CA2716128A1 (enExample) |
| WO (1) | WO2009108332A1 (enExample) |
Families Citing this family (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8575156B2 (en) | 2007-07-26 | 2013-11-05 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1 |
| AR069207A1 (es) | 2007-11-07 | 2010-01-06 | Vitae Pharmaceuticals Inc | Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1 |
| WO2009075835A1 (en) | 2007-12-11 | 2009-06-18 | Vitae Pharmaceutical, Inc | CYCLIC UREA INHIBITORS OF 11β-HYDROXYSTEROID DEHYDROGENASE 1 |
| TW200934490A (en) | 2008-01-07 | 2009-08-16 | Vitae Pharmaceuticals Inc | Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1 |
| JP5490020B2 (ja) | 2008-01-24 | 2014-05-14 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状カルバゼート及びセミカルバジドインヒビター |
| US8598160B2 (en) | 2008-02-15 | 2013-12-03 | Vitae Pharmaceuticals, Inc. | Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
| US8383629B2 (en) | 2008-02-27 | 2013-02-26 | Vitae Pharmaceuticals, Inc. | Inhibitors of 11β-hydroxysteroid dehydrogenase type 1 |
| NZ588954A (en) | 2008-05-01 | 2012-08-31 | Vitae Pharmaceuticals Inc | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| WO2009134387A1 (en) | 2008-05-01 | 2009-11-05 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| TW201016691A (en) | 2008-07-25 | 2010-05-01 | Boehringer Ingelheim Int | Inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| CA2729993A1 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 |
| CN104327062A (zh) | 2008-07-25 | 2015-02-04 | 贝林格尔·英格海姆国际有限公司 | 11β-羟基类固醇脱氢酶1的环状抑制剂 |
| EP2393807B1 (en) | 2009-02-04 | 2013-08-14 | Boehringer Ingelheim International GmbH | Cyclic inhibitors of 11 -hydroxysteroid dehydrogenase 1 |
| MA33216B1 (fr) | 2009-04-30 | 2012-04-02 | Boehringer Ingelheim Int | Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1 |
| WO2011011123A1 (en) | 2009-06-11 | 2011-01-27 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure |
| EP2496589B1 (en) | 2009-11-05 | 2014-03-05 | Boehringer Ingelheim International GmbH | Novel chiral phosphorus ligands |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| WO2011149822A1 (en) | 2010-05-26 | 2011-12-01 | Boehringer Ingelheim International Gmbh | 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives |
| JP5860042B2 (ja) | 2010-06-16 | 2016-02-16 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | 置換５、６及び７員複素環、そのような化合物を含有する医薬及びそれらの使用 |
| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
| EP2585444B1 (en) | 2010-06-25 | 2014-10-22 | Boehringer Ingelheim International GmbH | Azaspirohexanones as inhibitors of 11-beta-hsd1 for the treatment of metabolic disorders |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| EA201300522A1 (ru) | 2010-11-02 | 2013-11-29 | Бёрингер Ингельхайм Интернациональ Гмбх | Фармацевтические комбинации для лечения метаболических нарушений |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| US9532984B2 (en) | 2011-06-10 | 2017-01-03 | The Translational Genomics Research Institute | Therapeutic combination for cancer treatment |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| US9611267B2 (en) | 2012-06-13 | 2017-04-04 | Incyte Holdings Corporation | Substituted tricyclic compounds as FGFR inhibitors |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| TWI649318B (zh) | 2013-04-19 | 2019-02-01 | 英塞特控股公司 | 作為ｆｇｆｒ抑制劑之雙環雜環 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| AU2016219822B2 (en) | 2015-02-20 | 2020-07-09 | Incyte Holdings Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| SMT202200201T1 (it) * | 2016-02-12 | 2022-07-21 | Cytokinetics Inc | Derivati di tetraidroisochinolina |
| EP3235813A1 (en) | 2016-04-19 | 2017-10-25 | Cidqo 2012, S.L. | Aza-tetra-cyclo derivatives |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| CN107417519A (zh) * | 2017-08-03 | 2017-12-01 | 江苏万隆化学有限公司 | 一种高收率的2,3,4,5‑四氯苯甲酰氯制备方法 |
| TW201946630A (zh) | 2018-05-04 | 2019-12-16 | 美商英塞特公司 | Fgfr抑制劑之鹽 |
| ES2991427T3 (es) | 2018-05-04 | 2024-12-03 | Incyte Corp | Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| GEAP202415945A (en) | 2019-10-14 | 2024-04-25 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| AU2020395185A1 (en) | 2019-12-04 | 2022-06-02 | Incyte Corporation | Derivatives of an FGFR inhibitor |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| AR126101A1 (es) | 2021-06-09 | 2023-09-13 | Incyte Corp | Heterociclos tricíclicos como inhibidores de fgfr |
| CA3220274A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| MX2024008868A (es) | 2022-01-18 | 2024-09-23 | Maze Therapeutics Inc | Inhibidores de la apolipoproteína l1 (apol1) y métodos de uso. |
| EP4539838A1 (en) * | 2022-06-16 | 2025-04-23 | Lieber Institute, Inc. | Non-acid inhibitors of inositol hexakisphosphate kinase (ip6k) and methods of use thereof |
| WO2025201444A1 (en) * | 2024-03-28 | 2025-10-02 | Pyrotech (Beijing) Biotechnology Co., Ltd. | Novel gsdme inhibitors |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5206240A (en) | 1989-12-08 | 1993-04-27 | Merck & Co., Inc. | Nitrogen-containing spirocycles |
| CA2037357A1 (en) | 1990-03-02 | 1991-09-03 | Ben E. Evans | Methods for using spirocyclic oxytocin antagonists |
| DE69412067T2 (de) | 1993-01-28 | 1999-03-25 | Merck & Co., Inc., Rahway, N.J. | Substituierte spiro-azaringen als tachykinine rezeptor antagonisten |
| US5962462A (en) | 1996-12-13 | 1999-10-05 | Merck & Co., Inc. | Spiro-substituted azacycles as modulators of chemokine receptor activity |
| AU5803398A (en) | 1996-12-13 | 1998-07-03 | Merck & Co., Inc. | Spiro-substituted azacycles as modulators of chemokine receptor activity |
| US6013652A (en) | 1997-12-04 | 2000-01-11 | Merck & Co., Inc. | Spiro-substituted azacycles as neurokinin antagonists |
| US6566367B2 (en) | 2000-12-12 | 2003-05-20 | Pfizer Inc. | Spiro[isobenzofuran-1,4′-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4′-piperidines |
| US6828440B2 (en) | 2001-04-18 | 2004-12-07 | Euro-Celtique, S.A. | Spiroindene and spiroindane compounds |
| MXPA04001144A (es) | 2001-08-07 | 2004-07-08 | Banyu Pharma Co Ltd | Compuestos espiro. |
| JP2007516298A (ja) * | 2003-12-23 | 2007-06-21 | アリーナ ファーマシューティカルズ， インコーポレイテッド | 新規なスピロインドリンまたはスピロイソキノリン化合物、それらの使用方法および組成物 |
| CA2566094A1 (en) * | 2004-05-26 | 2005-12-08 | Eisai R & D Management Co., Ltd. | Cinnamide compound |
| JP2008504278A (ja) | 2004-06-24 | 2008-02-14 | インサイト・コーポレイション | アミド化合物およびその医薬としての使用 |
| WO2006058303A2 (en) | 2004-11-29 | 2006-06-01 | Vertex Pharmaceuticals Incorporated | Modulators of muscarinic receptors |
| DE102005023784A1 (de) | 2005-05-19 | 2006-11-30 | Grünenthal GmbH | Substituierte Spiro-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln |
| JP2009507800A (ja) | 2005-09-09 | 2009-02-26 | ユーロ−セルティーク エス．エイ． | 縮合およびスピロ環化合物ならびにその使用 |
| TW200804382A (en) | 2005-12-05 | 2008-01-16 | Incyte Corp | Lactam compounds and methods of using the same |
| US7998959B2 (en) | 2006-01-12 | 2011-08-16 | Incyte Corporation | Modulators of 11-β hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same |
| WO2007101270A1 (en) * | 2006-03-02 | 2007-09-07 | Incyte Corporation | MODULATORS OF 11-β HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME |
| TWI314400B (en) | 2006-03-13 | 2009-09-01 | Realtek Semiconductor Corp | Sigma-delta modulator |
| MX2008015906A (es) * | 2006-06-13 | 2009-03-06 | Vertex Pharma | Antagonistas del receptor del peptido relacionado con el gen de calcitonina. |
| US8383629B2 (en) * | 2008-02-27 | 2013-02-26 | Vitae Pharmaceuticals, Inc. | Inhibitors of 11β-hydroxysteroid dehydrogenase type 1 |
-
2009
- 2009-02-26 US US12/919,370 patent/US8383629B2/en not_active Expired - Fee Related
- 2009-02-26 EP EP09714767.2A patent/EP2265588B1/en not_active Not-in-force
- 2009-02-26 WO PCT/US2009/001215 patent/WO2009108332A1/en not_active Ceased
- 2009-02-26 CA CA2716128A patent/CA2716128A1/en not_active Abandoned
- 2009-02-26 JP JP2010548719A patent/JP5451646B2/ja not_active Expired - Fee Related
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