JP5451646B2 - 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 - Google Patents
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 Download PDFInfo
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- JP5451646B2 JP5451646B2 JP2010548719A JP2010548719A JP5451646B2 JP 5451646 B2 JP5451646 B2 JP 5451646B2 JP 2010548719 A JP2010548719 A JP 2010548719A JP 2010548719 A JP2010548719 A JP 2010548719A JP 5451646 B2 JP5451646 B2 JP 5451646B2
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- PLWMBYBVKVUTBR-UHFFFAOYSA-N spiro[2,3-dihydro-1h-naphthalene-4,4'-piperidine] Chemical compound C1CCC2=CC=CC=C2C21CCNCC2 PLWMBYBVKVUTBR-UHFFFAOYSA-N 0.000 description 1
- HEOQEWRIMCDLFB-UHFFFAOYSA-N spiro[2h-1-benzofuran-3,4'-piperidine] Chemical compound C1OC2=CC=CC=C2C11CCNCC1 HEOQEWRIMCDLFB-UHFFFAOYSA-N 0.000 description 1
- BFBDISABSUDHBW-UHFFFAOYSA-N spiro[piperidine-4,3'-pyrrolo[2,3-b]pyridine] Chemical compound C1CNCCC21C1=CC=CN=C1N=C2 BFBDISABSUDHBW-UHFFFAOYSA-N 0.000 description 1
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- GFYHSKONPJXCDE-UHFFFAOYSA-N sym-collidine Natural products CC1=CN=C(C)C(C)=C1 GFYHSKONPJXCDE-UHFFFAOYSA-N 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
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- VLDXMVBQRZLZEO-OUKQBFOZSA-N tert-butyl 1'-[(e)-3-[2-(trifluoromethyl)phenyl]prop-2-enoyl]spiro[1,3-dihydroisoquinoline-4,4'-piperidine]-2-carboxylate Chemical compound C1N(C(=O)OC(C)(C)C)CC2=CC=CC=C2C1(CC1)CCN1C(=O)\C=C\C1=CC=CC=C1C(F)(F)F VLDXMVBQRZLZEO-OUKQBFOZSA-N 0.000 description 1
- LSAZPKBLNMNLGH-UHFFFAOYSA-N tert-butyl 1'-[3-[2-(trifluoromethyl)phenyl]propanoyl]spiro[1,3-dihydroisoquinoline-4,4'-piperidine]-2-carboxylate Chemical compound C1N(C(=O)OC(C)(C)C)CC2=CC=CC=C2C1(CC1)CCN1C(=O)CCC1=CC=CC=C1C(F)(F)F LSAZPKBLNMNLGH-UHFFFAOYSA-N 0.000 description 1
- OWYHAYAJHNQBGG-UHFFFAOYSA-N tert-butyl 3-oxospiro[2h-indene-1,4'-piperidine]-1'-carboxylate Chemical compound C1CN(C(=O)OC(C)(C)C)CCC11C2=CC=CC=C2C(=O)C1 OWYHAYAJHNQBGG-UHFFFAOYSA-N 0.000 description 1
- PVNSZDHDIOZJEQ-UHFFFAOYSA-N tert-butyl 4-[(3,5-dichloro-2-iodobenzoyl)-[(4-methoxyphenyl)methyl]amino]-3,6-dihydro-2h-pyridine-1-carboxylate Chemical compound C1=CC(OC)=CC=C1CN(C=1CCN(CC=1)C(=O)OC(C)(C)C)C(=O)C1=CC(Cl)=CC(Cl)=C1I PVNSZDHDIOZJEQ-UHFFFAOYSA-N 0.000 description 1
- LQZQWYQPRPUIBB-UHFFFAOYSA-N tert-butyl 4-bromo-1-(2-trimethylsilylethoxycarbonylamino)spiro[1,2-dihydroindene-3,4'-piperidine]-1'-carboxylate Chemical compound C1CN(C(=O)OC(C)(C)C)CCC11C2=C(Br)C=CC=C2C(NC(=O)OCC[Si](C)(C)C)C1 LQZQWYQPRPUIBB-UHFFFAOYSA-N 0.000 description 1
- XKVSTTHNVBKSHX-UHFFFAOYSA-N tert-butyl 5-fluoro-2-oxospiro[1h-indole-3,4'-piperidine]-1'-carboxylate Chemical compound C1CN(C(=O)OC(C)(C)C)CCC21C1=CC(F)=CC=C1NC2=O XKVSTTHNVBKSHX-UHFFFAOYSA-N 0.000 description 1
- MYONTCLFEPBNGF-UHFFFAOYSA-N tert-butyl 7'-bromo-2'-[(4-methoxyphenyl)methyl]-3'-oxospiro[2,3-dihydropyridine-4,1'-isoindole]-1-carboxylate Chemical compound C1=CC(OC)=CC=C1CN1C2(C=CN(CC2)C(=O)OC(C)(C)C)C2=C(Br)C=CC=C2C1=O MYONTCLFEPBNGF-UHFFFAOYSA-N 0.000 description 1
- 210000001550 testis Anatomy 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- RAOIDOHSFRTOEL-UHFFFAOYSA-N tetrahydrothiophene Chemical compound C1CCSC1 RAOIDOHSFRTOEL-UHFFFAOYSA-N 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
- DNGMYXZLJGHHOM-UHFFFAOYSA-N thiazinane 1,1-dioxide Chemical compound O=S1(=O)CCCCN1 DNGMYXZLJGHHOM-UHFFFAOYSA-N 0.000 description 1
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- 150000003573 thiols Chemical class 0.000 description 1
- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
- C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
- C07D221/20—Spiro-condensed ring systems
Landscapes
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
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 JP2011513305A5 (enExample) | 2012-04-05 |
| JP5451646B2 true JP5451646B2 (ja) | 2014-03-26 |
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| 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) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| JP5451611B2 (ja) | 2007-07-26 | 2014-03-26 | 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のサイクリックインヒビター |
| AR069207A1 (es) | 2007-11-07 | 2010-01-06 | Vitae Pharmaceuticals Inc | Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1 |
| CA2708303A1 (en) | 2007-12-11 | 2009-06-18 | Vitae Pharmaceuticals, Inc. | Cyclic urea inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
| TW200934490A (en) | 2008-01-07 | 2009-08-16 | Vitae Pharmaceuticals Inc | Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1 |
| WO2009094169A1 (en) | 2008-01-24 | 2009-07-30 | Vitae Pharmaceuticals, Inc. | Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| US8598160B2 (en) | 2008-02-15 | 2013-12-03 | Vitae Pharmaceuticals, Inc. | Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
| EP2265588B1 (en) | 2008-02-27 | 2013-06-26 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF 11ß -HYDROXYSTEROID DEHYDROGENASE TYPE 1 |
| KR20110002492A (ko) | 2008-05-01 | 2011-01-07 | 비타이 파마슈티컬즈, 인코포레이티드 | 11베타-하이드록시스테로이드 탈수소효소 1의 고리형 억제제 |
| EP2291370B1 (en) | 2008-05-01 | 2013-11-27 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| US8846668B2 (en) | 2008-07-25 | 2014-09-30 | Vitae Pharmaceuticals, Inc. | Inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| WO2010011314A1 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | Cyclic inhibitors of 11 beta-hydroxysteroid dehydrogenase 1 |
| CA2729993A1 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 |
| JP5679997B2 (ja) | 2009-02-04 | 2015-03-04 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状阻害剤 |
| UA109255C2 (ru) | 2009-04-30 | 2015-08-10 | Берінгер Інгельхайм Інтернешнл Гмбх | Циклические ингибиторы 11бета-гидроксистероиддегидрогеназы 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 |
| EP2576570A1 (en) | 2010-05-26 | 2013-04-10 | Boehringer Ingelheim International GmbH | 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives |
| EP2582698B1 (en) | 2010-06-16 | 2016-09-14 | Vitae Pharmaceuticals, Inc. | Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use |
| 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 |
| WO2011161128A1 (en) | 2010-06-25 | 2011-12-29 | 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 |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| 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 |
| CA2813671A1 (en) | 2010-11-02 | 2012-05-10 | Boehringer Ingelheim International Gmbh | Pharmaceutical combinations for the treatment of metabolic disorders |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
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| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| PH12015502383B1 (en) | 2013-04-19 | 2023-02-03 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
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| CA2976790C (en) | 2015-02-20 | 2024-02-27 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
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| KR102956194B1 (ko) | 2018-05-04 | 2026-04-23 | 인사이트 코포레이션 | Fgfr 억제제의 염 |
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| 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 |
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| WO1998025605A1 (en) | 1996-12-13 | 1998-06-18 | 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 |
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| EP2033644A1 (en) | 2001-04-18 | 2009-03-11 | Euro-Celtique S.A. | Spiroindene and spiroindane compounds |
| ATE427935T1 (de) | 2001-08-07 | 2009-04-15 | Banyu Pharma Co Ltd | Spiro isobenzofurane als neuropeptid y rezeptor antagonisten |
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| DE102005023784A1 (de) | 2005-05-19 | 2006-11-30 | Grünenthal GmbH | Substituierte Spiro-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln |
| WO2007028638A1 (en) | 2005-09-09 | 2007-03-15 | Euro-Celtique S.A. | Fused and spirocycle compounds and the use thereof |
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| 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 |
| EP2027106A2 (en) * | 2006-06-13 | 2009-02-25 | Vertex Pharmaceuticals Incorporated | Cgrp receptor antagonists |
| EP2265588B1 (en) * | 2008-02-27 | 2013-06-26 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF 11ß -HYDROXYSTEROID DEHYDROGENASE TYPE 1 |
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- 2009-02-26 CA CA2716128A patent/CA2716128A1/en not_active Abandoned
- 2009-02-26 JP JP2010548719A patent/JP5451646B2/ja not_active Expired - Fee Related
- 2009-02-26 US US12/919,370 patent/US8383629B2/en not_active Expired - Fee Related
- 2009-02-26 WO PCT/US2009/001215 patent/WO2009108332A1/en not_active Ceased
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| WO2009108332A1 (en) | 2009-09-03 |
| JP2011513305A (ja) | 2011-04-28 |
| CA2716128A1 (en) | 2009-09-03 |
| US20110136821A1 (en) | 2011-06-09 |
| EP2265588A1 (en) | 2010-12-29 |
| EP2265588B1 (en) | 2013-06-26 |
| US8383629B2 (en) | 2013-02-26 |
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