JP2011524336A5 - - Google Patents
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- Publication number
- JP2011524336A5 JP2011524336A5 JP2011507441A JP2011507441A JP2011524336A5 JP 2011524336 A5 JP2011524336 A5 JP 2011524336A5 JP 2011507441 A JP2011507441 A JP 2011507441A JP 2011507441 A JP2011507441 A JP 2011507441A JP 2011524336 A5 JP2011524336 A5 JP 2011524336A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cycloalkyl
- halo
- alkoxy
- hydroxy
- 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 93
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 60
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 48
- 125000003545 alkoxy group Chemical group 0.000 claims 38
- -1 cycloalkyl alkanes Chemical class 0.000 claims 38
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 36
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 31
- 125000004043 oxo group Chemical group O=* 0.000 claims 31
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 27
- 125000004093 cyano group Chemical group *C#N 0.000 claims 24
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 23
- 150000001875 compounds Chemical class 0.000 claims 22
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 22
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 21
- 125000000217 alkyl group Chemical group 0.000 claims 20
- 125000004750 (C1-C6) alkylaminosulfonyl group Chemical group 0.000 claims 18
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims 18
- 150000001408 amides Chemical class 0.000 claims 18
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 claims 18
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 17
- 229910052731 fluorine Inorganic materials 0.000 claims 17
- 239000011737 fluorine Substances 0.000 claims 17
- 229910052736 halogen Inorganic materials 0.000 claims 17
- 150000002367 halogens Chemical group 0.000 claims 17
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 15
- 125000001072 heteroaryl group Chemical group 0.000 claims 15
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 14
- 229910052801 chlorine Inorganic materials 0.000 claims 14
- 239000000460 chlorine Substances 0.000 claims 14
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 14
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 12
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 12
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 12
- 229910052757 nitrogen Inorganic materials 0.000 claims 12
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 12
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 12
- 125000005167 cycloalkylaminocarbonyl group Chemical group 0.000 claims 11
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 10
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 10
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 10
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 10
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 10
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 10
- 125000005366 cycloalkylthio group Chemical group 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 9
- 125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 claims 9
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 9
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 9
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 9
- 125000004414 alkyl thio group Chemical group 0.000 claims 9
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 9
- 229910052794 bromium Inorganic materials 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 125000004663 dialkyl amino group Chemical group 0.000 claims 9
- 125000001188 haloalkyl group Chemical group 0.000 claims 9
- 125000006517 heterocyclyl carbonyl group Chemical group 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 claims 8
- 125000005145 cycloalkylaminosulfonyl group Chemical group 0.000 claims 7
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 6
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 5
- 125000003830 C1- C4 alkylcarbonylamino group Chemical group 0.000 claims 5
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- QOXOZONBQWIKDA-UHFFFAOYSA-N 3-hydroxypropyl Chemical group [CH2]CCO QOXOZONBQWIKDA-UHFFFAOYSA-N 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 125000001207 fluorophenyl group Chemical group 0.000 claims 4
- 125000006526 (C1-C2) alkyl group Chemical group 0.000 claims 3
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 3
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical group C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 125000003725 azepanyl group Chemical group 0.000 claims 3
- 125000005241 heteroarylamino group Chemical group 0.000 claims 3
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 3
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 2
- 125000001769 aryl amino group Chemical group 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000004458 methylaminocarbonyl group Chemical group [H]N(C(*)=O)C([H])([H])[H] 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 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
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 125000004965 chloroalkyl group Chemical group 0.000 claims 1
- 125000005148 cycloalkylalkanesulfinyl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 0 *C(*)(CCN1[C@@](C*I)(CCC2)CN2c2nc(*)c(*#*)[s]2)OC1=O Chemical compound *C(*)(CCN1[C@@](C*I)(CCC2)CN2c2nc(*)c(*#*)[s]2)OC1=O 0.000 description 1
- UHOVQNZJYSORNB-UHFFFAOYSA-N c1ccccc1 Chemical compound c1ccccc1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4965008P | 2008-05-01 | 2008-05-01 | |
| US61/049,650 | 2008-05-01 | ||
| US13714808P | 2008-07-25 | 2008-07-25 | |
| US61/137,148 | 2008-07-25 | ||
| PCT/US2008/009017 WO2009017664A1 (en) | 2007-07-26 | 2008-07-25 | CYCLIC INHIBITORS OF 11β-HYDROXYSTERIOD DEHYDROGENASE 1 |
| USPCT/US2008/009017 | 2008-07-25 | ||
| US20682509P | 2009-02-04 | 2009-02-04 | |
| US61/206,825 | 2009-02-04 | ||
| PCT/US2009/002629 WO2009134384A1 (en) | 2008-05-01 | 2009-04-30 | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011524336A JP2011524336A (ja) | 2011-09-01 |
| JP2011524336A5 true JP2011524336A5 (https=) | 2012-06-14 |
| JP5451752B2 JP5451752B2 (ja) | 2014-03-26 |
Family
ID=40765565
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011507441A Expired - Fee Related JP5451752B2 (ja) | 2008-05-01 | 2009-04-30 | 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 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8242111B2 (https=) |
| EP (1) | EP2291373B1 (https=) |
| JP (1) | JP5451752B2 (https=) |
| CA (1) | CA2723032A1 (https=) |
| WO (1) | WO2009134384A1 (https=) |
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2678577A1 (en) | 2007-02-26 | 2008-09-04 | Vitae Pharmaceuticals, Inc. | Cyclic urea and carbamate inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
| JP5470557B2 (ja) | 2007-07-26 | 2014-04-16 | 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 | １１β−ヒドロキシステロイドデヒドロゲナーゼ１型の阻害剤の合成 |
| AR069207A1 (es) | 2007-11-07 | 2010-01-06 | Vitae Pharmaceuticals Inc | Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1 |
| 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 |
| WO2009094169A1 (en) * | 2008-01-24 | 2009-07-30 | Vitae Pharmaceuticals, Inc. | Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| CA2714532A1 (en) * | 2008-02-11 | 2009-08-20 | Vitae Pharmaceuticals, Inc. | 1,3-oxazepan-2-one and 1,3-diazepan-2-one inhibitors of 11.beta.-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 |
| WO2009117109A1 (en) * | 2008-03-18 | 2009-09-24 | Vitae Pharmaceuticals, Inc. | Inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 |
| EP2291370B1 (en) | 2008-05-01 | 2013-11-27 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| RU2531272C2 (ru) | 2008-05-01 | 2014-10-20 | Вайтаи Фармасьютиклз, Инк. | Циклические ингибиторы 11бета-гидроксистероид-дегидрогеназы 1 |
| US8242111B2 (en) | 2008-05-01 | 2012-08-14 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1 |
| JP5696037B2 (ja) | 2008-05-01 | 2015-04-08 | 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 |
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| CA2750517A1 (en) | 2009-02-04 | 2010-08-12 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 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 |
| JP5656880B2 (ja) | 2009-03-09 | 2015-01-21 | グラクソ グループ リミテッドＧｌａｘｏ Ｇｒｏｕｐ Ｌｉｍｉｔｅｄ | Ｐｉ３キナーゼの阻害剤としての４−オキサジアゾール−２−イル−インダゾール |
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| EP2448928B1 (en) | 2009-07-01 | 2014-08-13 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
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| WO2013097052A1 (en) | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
| CR20170077A (es) | 2014-08-04 | 2017-06-26 | Nuevolution As | Derivados de heterociclilo opcionalmente condensados de pirimidina útiles para el tratamiento de enfermedades inflamatorias, metabólicas, oncológicas y autoinmunitarias |
| PT3442972T (pt) | 2016-04-15 | 2020-05-29 | Abbvie Inc | Inibidores de bromodomínio |
| UY38994A (es) | 2019-12-20 | 2021-07-30 | Nuevolution As | Compuestos activos frente a receptores nucleares |
| MX2022007265A (es) | 2019-12-20 | 2022-09-09 | Nuevolution As | Compuestos activos frente a receptores nucleares. |
| AU2021245397A1 (en) | 2020-03-31 | 2022-10-20 | Nuevolution A/S | Compounds active towards nuclear receptors |
| WO2021198956A1 (en) | 2020-03-31 | 2021-10-07 | Nuevolution A/S | Compounds active towards nuclear receptors |
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-
2009
- 2009-04-30 US US12/990,309 patent/US8242111B2/en not_active Expired - Fee Related
- 2009-04-30 CA CA2723032A patent/CA2723032A1/en not_active Abandoned
- 2009-04-30 JP JP2011507441A patent/JP5451752B2/ja not_active Expired - Fee Related
- 2009-04-30 EP EP09739187.4A patent/EP2291373B1/en not_active Not-in-force
- 2009-04-30 WO PCT/US2009/002629 patent/WO2009134384A1/en not_active Ceased
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