JP5490014B2 - １１β−ヒドロキシステロイドデヒドロゲナーゼ１型の環状尿素阻害剤 - Google Patents
１１β−ヒドロキシステロイドデヒドロゲナーゼ１型の環状尿素阻害剤 Download PDFInfo
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- JP5490014B2 JP5490014B2 JP2010537950A JP2010537950A JP5490014B2 JP 5490014 B2 JP5490014 B2 JP 5490014B2 JP 2010537950 A JP2010537950 A JP 2010537950A JP 2010537950 A JP2010537950 A JP 2010537950A JP 5490014 B2 JP5490014 B2 JP 5490014B2
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- 108010088011 11-beta-Hydroxysteroid Dehydrogenase Type 1 Proteins 0.000 title claims description 59
- 102000008645 11-beta-Hydroxysteroid Dehydrogenase Type 1 Human genes 0.000 title claims description 59
- 239000003112 inhibitor Substances 0.000 title description 23
- ZMGMDXCADSRNCX-UHFFFAOYSA-N 5,6-dihydroxy-1,3-diazepan-2-one Chemical compound OC1CNC(=O)NCC1O ZMGMDXCADSRNCX-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims description 167
- 125000000217 alkyl group Chemical group 0.000 claims description 109
- -1 CO 2 H Chemical group 0.000 claims description 94
- 125000004043 oxo group Chemical group O=* 0.000 claims description 82
- 125000003545 alkoxy group Chemical group 0.000 claims description 77
- 125000005843 halogen group Chemical group 0.000 claims description 77
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- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 58
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- 150000002367 halogens Chemical class 0.000 claims description 43
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 40
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 40
- 125000004414 alkyl thio group Chemical group 0.000 claims description 35
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 35
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 35
- 125000001072 heteroaryl group Chemical group 0.000 claims description 35
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims description 34
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- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 34
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 23
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- FBXGQDUVJBKEAJ-UHFFFAOYSA-N 4h-oxazin-3-one Chemical group O=C1CC=CON1 FBXGQDUVJBKEAJ-UHFFFAOYSA-N 0.000 claims description 3
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- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 3
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 3
- 125000003107 substituted aryl group Chemical group 0.000 claims description 3
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 3
- 125000006536 (C1-C2)alkoxy group Chemical group 0.000 claims description 2
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- 125000006532 (C3-C5) alkyl group Chemical group 0.000 claims description 2
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- 125000005148 cycloalkylalkanesulfinyl group Chemical group 0.000 claims 3
- 125000005145 cycloalkylaminosulfonyl group Chemical group 0.000 claims 2
- 241001553014 Myrsine salicina Species 0.000 claims 1
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
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- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical group C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 72
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- 238000000034 method Methods 0.000 description 53
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- 239000003862 glucocorticoid Substances 0.000 description 31
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 description 31
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- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 18
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US706007P | 2007-12-11 | 2007-12-11 | |
| US61/007,060 | 2007-12-11 | ||
| PCT/US2008/013539 WO2009075835A1 (en) | 2007-12-11 | 2008-12-10 | CYCLIC UREA INHIBITORS OF 11β-HYDROXYSTEROID DEHYDROGENASE 1 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011506438A JP2011506438A (ja) | 2011-03-03 |
| JP2011506438A5 JP2011506438A5 (cg-RX-API-DMAC7.html) | 2012-01-05 |
| JP5490014B2 true JP5490014B2 (ja) | 2014-05-14 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010537950A Expired - Fee Related JP5490014B2 (ja) | 2007-12-11 | 2008-12-10 | １１β−ヒドロキシステロイドデヒドロゲナーゼ１型の環状尿素阻害剤 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US8440658B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2229368A1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP5490014B2 (cg-RX-API-DMAC7.html) |
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-
2008
- 2008-12-10 EP EP08859146A patent/EP2229368A1/en not_active Withdrawn
- 2008-12-10 CA CA2708303A patent/CA2708303A1/en not_active Abandoned
- 2008-12-10 WO PCT/US2008/013539 patent/WO2009075835A1/en not_active Ceased
- 2008-12-10 US US12/747,391 patent/US8440658B2/en not_active Expired - Fee Related
- 2008-12-10 JP JP2010537950A patent/JP5490014B2/ja not_active Expired - Fee Related
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2013
- 2013-04-30 US US13/873,574 patent/US8748444B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US20130245051A1 (en) | 2013-09-19 |
| US8440658B2 (en) | 2013-05-14 |
| WO2009075835A8 (en) | 2009-08-27 |
| EP2229368A1 (en) | 2010-09-22 |
| WO2009075835A1 (en) | 2009-06-18 |
| JP2011506438A (ja) | 2011-03-03 |
| US20110263582A1 (en) | 2011-10-27 |
| CA2708303A1 (en) | 2009-06-18 |
| US8748444B2 (en) | 2014-06-10 |
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