JP2011515398A5 - - Google Patents
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- Publication number
- JP2011515398A5 JP2011515398A5 JP2011500805A JP2011500805A JP2011515398A5 JP 2011515398 A5 JP2011515398 A5 JP 2011515398A5 JP 2011500805 A JP2011500805 A JP 2011500805A JP 2011500805 A JP2011500805 A JP 2011500805A JP 2011515398 A5 JP2011515398 A5 JP 2011515398A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- halo
- alkoxy
- cycloalkyl
- alkylamino
- 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
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- 125000005843 halogen group Chemical group 0.000 claims 96
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 41
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 34
- 125000003545 alkoxy group Chemical group 0.000 claims 32
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 26
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 24
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 23
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 22
- 125000004750 (C1-C6) alkylaminosulfonyl group Chemical group 0.000 claims 20
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 19
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 16
- 125000001072 heteroaryl group Chemical group 0.000 claims 15
- 125000004043 oxo group Chemical group O=* 0.000 claims 14
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 13
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 125000005148 cycloalkylalkanesulfinyl group Chemical group 0.000 claims 13
- 125000005366 cycloalkylthio group Chemical group 0.000 claims 13
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 12
- 229910052731 fluorine Inorganic materials 0.000 claims 12
- 239000011737 fluorine Substances 0.000 claims 12
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 11
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 10
- 125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 claims 10
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 10
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 10
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 10
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 10
- 229910052794 bromium Inorganic materials 0.000 claims 10
- 229910052801 chlorine Inorganic materials 0.000 claims 10
- 239000000460 chlorine Substances 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 125000006517 heterocyclyl carbonyl group Chemical group 0.000 claims 10
- -1 CO 2 H Chemical group 0.000 claims 9
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 9
- 125000000623 heterocyclic group Chemical group 0.000 claims 9
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 8
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 8
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 7
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 7
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 claims 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 6
- 150000001408 amides Chemical class 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 5
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 4
- 125000005167 cycloalkylaminocarbonyl group Chemical group 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 3
- 125000006528 (C2-C6) alkyl group Chemical group 0.000 claims 2
- 102000008645 11-beta-Hydroxysteroid Dehydrogenase Type 1 Human genes 0.000 claims 2
- 108010088011 11-beta-Hydroxysteroid Dehydrogenase Type 1 Proteins 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 125000004414 alkyl thio group Chemical group 0.000 claims 2
- 125000001769 aryl amino group Chemical group 0.000 claims 2
- 125000004663 dialkyl amino group Chemical group 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000005241 heteroarylamino group Chemical group 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000005529 alkyleneoxy group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 150000001924 cycloalkanes Chemical class 0.000 claims 1
- VILAVOFMIJHSJA-UHFFFAOYSA-N dicarbon monoxide Chemical compound [C]=C=O VILAVOFMIJHSJA-UHFFFAOYSA-N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 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
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US3764608P | 2008-03-18 | 2008-03-18 | |
| US61/037,646 | 2008-03-18 | ||
| PCT/US2009/001712 WO2009117109A1 (en) | 2008-03-18 | 2009-03-18 | Inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011515398A JP2011515398A (ja) | 2011-05-19 |
| JP2011515398A5 true JP2011515398A5 (enExample) | 2012-05-10 |
| JP5538356B2 JP5538356B2 (ja) | 2014-07-02 |
Family
ID=40757022
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011500805A Expired - Fee Related JP5538356B2 (ja) | 2008-03-18 | 2009-03-18 | 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) | US20110105504A1 (enExample) |
| EP (1) | EP2274287B1 (enExample) |
| JP (1) | JP5538356B2 (enExample) |
| CA (1) | CA2718264A1 (enExample) |
| WO (1) | WO2009117109A1 (enExample) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2125750B1 (en) | 2007-02-26 | 2014-05-21 | Vitae Pharmaceuticals, Inc. | Cyclic urea and carbamate inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| WO2009017671A1 (en) | 2007-07-26 | 2009-02-05 | Vitae Pharmaceuticals, Inc. | Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 |
| AR069207A1 (es) | 2007-11-07 | 2010-01-06 | Vitae Pharmaceuticals Inc | Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1 |
| EP2220048B1 (en) | 2007-11-16 | 2017-01-25 | Boehringer Ingelheim International GmbH | Aryl- and heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use |
| US8440658B2 (en) | 2007-12-11 | 2013-05-14 | Vitae Pharmaceuticals, 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 |
| US8592409B2 (en) * | 2008-01-24 | 2013-11-26 | Vitae Pharmaceuticals, Inc. | Cyclic carbazate and semicarbazide inhibitors of 11β-hydroxysteroid dehydrogenase 1 |
| JP5734666B2 (ja) * | 2008-02-11 | 2015-06-17 | 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１，３−オキサアゼパン−２−オン及び１，３−ジアゼパン−２−オン阻害剤 |
| CA2715290A1 (en) | 2008-02-15 | 2009-08-20 | Vitae Pharmaceuticals, Inc. | Inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| EP2291373B1 (en) * | 2008-05-01 | 2013-09-11 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| JP5301563B2 (ja) * | 2008-05-01 | 2013-09-25 | 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の環状インヒビター |
| EP2291371B1 (en) | 2008-05-01 | 2015-06-10 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| CA2723034A1 (en) | 2008-05-01 | 2009-11-05 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| EP2288596B1 (en) | 2008-05-13 | 2016-11-30 | Boehringer Ingelheim International GmbH | Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use |
| WO2010010150A1 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 |
| PL2324018T3 (pl) | 2008-07-25 | 2014-02-28 | Boehringer Ingelheim Int | Cykliczne inhibitory dehydrogenazy 11 beta-hydroksysteroidowej typu 1 |
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| WO2010046445A2 (en) | 2008-10-23 | 2010-04-29 | Boehringer Ingelheim International Gmbh | Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use |
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| MA33216B1 (fr) | 2009-04-30 | 2012-04-02 | Boehringer Ingelheim Int | Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1 |
| WO2010139673A1 (en) * | 2009-06-02 | 2010-12-09 | Boehringer Ingelheim International Gmbh | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 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 |
| EP2448928B1 (en) | 2009-07-01 | 2014-08-13 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
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| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
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2009
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