PL377501A1 - Adamantyloacetamidy jako inhibitory dehydrogenazy 11-beta hydroksysteroidowej - Google Patents
Adamantyloacetamidy jako inhibitory dehydrogenazy 11-beta hydroksysteroidowejInfo
- Publication number
- PL377501A1 PL377501A1 PL377501A PL37750103A PL377501A1 PL 377501 A1 PL377501 A1 PL 377501A1 PL 377501 A PL377501 A PL 377501A PL 37750103 A PL37750103 A PL 37750103A PL 377501 A1 PL377501 A1 PL 377501A1
- Authority
- PL
- Poland
- Prior art keywords
- 4alkyl
- independently hydrogen
- substituted
- het1
- 4alkyloxy
- Prior art date
Links
- -1 Adamantyl acetamides Chemical class 0.000 title abstract 2
- 102000004277 11-beta-hydroxysteroid dehydrogenases Human genes 0.000 title 1
- 108090000874 11-beta-hydroxysteroid dehydrogenases Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 9
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- 125000005871 1,3-benzodioxolyl group Chemical group 0.000 abstract 1
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 abstract 1
- 125000000815 N-oxide group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 abstract 1
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
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- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/24—Oxygen or sulfur atoms
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- C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
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- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
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Abstract
Formy N-tlenków, farmaceutycznie dopuszczalne sole addycyjne i ich stereochemiczne formy izomeryczne, w których n oznacza liczbę całkowitą 1 lub 2; każdy R1 i R2 niezależnie oznacza atom wodoru, C1-4alkil, NR9R10, C3-6-alkilooksy; lub R1 i R2 razem z atom węgla, z którym są połączone tworzą C3-6cykloalkil; i w którym n ma wartość 2, albo R1 lub R2 mogą nie występować dając wiązanie nienasycone; R3 oznacza C6-12cykloalkil, korzystnie wybrany spośród takich jak cylooctanyl i cykloheksyl lub R3 oznacza jednowartościowy rodnik o jednym z następujących wzorów, przy czym ten C6-12cykloalkil lub jednowartościowy rodnik może być ewentualnie podstawiony przez jeden, lub gdzie to możliwe dwa, trzy lub więcej podstawników wybranych z grupy obejmującej C1-4alkil, C1-4alkilooksy, atom fluorowca lub hydroksykl; Q oznacza Het1 lub Ar2 przy czym ten C3-8cykloalkil, Het1 lub Ar2 są ewentualnie podstawione przez jeden lub gdzie to możliwe dwa lub więcej podstawników wybranych spośród takich jak atom fluorowca, C1-4alkil, C1-4alkilooksy, hydroksyl, nitro, NR5R6, C1-4alkilooksy podstawiony przez jeden lub gdzie to możliwe dwa, trzy lub więcej podstawników, przy czym każdy jest niezależnie wybrany spośród takich jak hydroksykarbonyl, Het2 i NR7R8, i C1-4alkil podstawiony przez jeden lub gdzie to możliwe dwa lub trzy atomy fluorowca, korzystnie trifluorometyl; każdy R5 i R6 niezależnie oznacza atom wodoru, C1-4alkil, lub C1-4alkil podstawiony przez fenyl; każdy R1 i R8 niezależnie oznacza atom wodoru lub C1-4alkil; każdy R9 i R10 niezależnie oznacza atom wodoru, C1-4alkil lub C1-4alkilooksykarbonyl; L oznacza C1-4alkil; Het1 oznacza heterocykl wybrany spośród takich jak pirydynyl, tiofenyl, lub 1,3-benzodioksolil; Het2 oznacza piperydynyl, pirolidynyl lub morfolinyl; Ar2 oznacza fenyl, naftyl lub indenyl.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/EP2002/014832 WO2004056744A1 (en) | 2002-12-23 | 2002-12-23 | Adamantyl acetamides as hydroxysteroid dehydrogenase inhibitors |
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| PL210615B1 PL210615B1 (pl) | 2012-02-29 |
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| DE10164139A1 (de) | 2001-12-27 | 2003-07-10 | Bayer Ag | 2-Heteroarylcarbonsäureamide |
| WO2004056744A1 (en) * | 2002-12-23 | 2004-07-08 | Janssen Pharmaceutica N.V. | Adamantyl acetamides as hydroxysteroid dehydrogenase inhibitors |
| AU2004273610B2 (en) | 2003-09-22 | 2010-07-01 | Onepharm Research & Development Gmbh | Prevention and treatment of inflammation-induced and/or immune-mediated bone loss |
| MXPA06007077A (es) * | 2003-12-19 | 2006-08-23 | Pfizer | Derivados de bencenosulfonilamino-piridin-2-ilo y compuestos relacionados como inhibidores de 11-beta-hidroxi esteroide deshidrogenasa tipo 1 para el tratamiento de diabetes y obesidad. |
| JP4960708B2 (ja) * | 2004-01-30 | 2012-06-27 | バーテックス ファーマシューティカルズ インコーポレイテッド | Atp結合カセットトランスポーターのモジュレーター |
| US20100222316A1 (en) * | 2004-04-29 | 2010-09-02 | Abbott Laboratories | Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme |
| US7880001B2 (en) | 2004-04-29 | 2011-02-01 | Abbott Laboratories | Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme |
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