AR047517A1 - DERIVATIVES OF 3- (DIARILMETILEN) -8-AZABICICLO (3,2,1) OCTANO - Google Patents
DERIVATIVES OF 3- (DIARILMETILEN) -8-AZABICICLO (3,2,1) OCTANOInfo
- Publication number
- AR047517A1 AR047517A1 ARP050100322A ARP050100322A AR047517A1 AR 047517 A1 AR047517 A1 AR 047517A1 AR P050100322 A ARP050100322 A AR P050100322A AR P050100322 A ARP050100322 A AR P050100322A AR 047517 A1 AR047517 A1 AR 047517A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- aryl
- agents
- amino
- hydrogen
- Prior art date
Links
- TVMXDCGIABBOFY-UHFFFAOYSA-N octane Chemical compound CCCCCCCC TVMXDCGIABBOFY-UHFFFAOYSA-N 0.000 title 1
- 125000001424 substituent group Chemical group 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 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
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 3
- -1 [1,3] -benzodioxolyl Chemical group 0.000 abstract 3
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 3
- 239000003795 chemical substances by application Substances 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 2
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 229940079593 drug Drugs 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000003831 tetrazolyl group Chemical group 0.000 abstract 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000006624 (C1-C6) alkoxycarbonylamino group Chemical group 0.000 abstract 1
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 1
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 abstract 1
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 abstract 1
- 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 abstract 1
- 208000007848 Alcoholism Diseases 0.000 abstract 1
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 abstract 1
- 206010012735 Diarrhoea Diseases 0.000 abstract 1
- 206010013654 Drug abuse Diseases 0.000 abstract 1
- 208000007882 Gastritis Diseases 0.000 abstract 1
- 101100244562 Pseudomonas aeruginosa (strain ATCC 15692 / DSM 22644 / CIP 104116 / JCM 14847 / LMG 12228 / 1C / PRS 101 / PAO1) oprD gene Proteins 0.000 abstract 1
- 206010001584 alcohol abuse Diseases 0.000 abstract 1
- 208000025746 alcohol use disease Diseases 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 abstract 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 1
- 229940035676 analgesics Drugs 0.000 abstract 1
- 239000000730 antalgic agent Substances 0.000 abstract 1
- 239000002260 anti-inflammatory agent Substances 0.000 abstract 1
- 229940121363 anti-inflammatory agent Drugs 0.000 abstract 1
- 239000002327 cardiovascular agent Substances 0.000 abstract 1
- 229940125692 cardiovascular agent Drugs 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 108700023159 delta Opioid Receptors Proteins 0.000 abstract 1
- 102000048124 delta Opioid Receptors Human genes 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 229960003444 immunosuppressant agent Drugs 0.000 abstract 1
- 239000003018 immunosuppressive agent Substances 0.000 abstract 1
- 230000000926 neurological effect Effects 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 1
- 208000023504 respiratory system disease Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 208000011117 substance-related disease Diseases 0.000 abstract 1
- IMCGHZIGRANKHV-AJNGGQMLSA-N tert-butyl (3s,5s)-2-oxo-5-[(2s,4s)-5-oxo-4-propan-2-yloxolan-2-yl]-3-propan-2-ylpyrrolidine-1-carboxylate Chemical compound O1C(=O)[C@H](C(C)C)C[C@H]1[C@H]1N(C(=O)OC(C)(C)C)C(=O)[C@H](C(C)C)C1 IMCGHZIGRANKHV-AJNGGQMLSA-N 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Son utiles como moduladores del receptor delta opioide o mu opioide. Como analgésicos, inmunosupresores, agentes antiinflamatorios, agentes para el tratamiento de afecciones neurologicas y psiquiátricas, medicamentos para abuso de fármacos y de alcohol, agentes para tratar la gastritis y la diarrea, agentes cardiovasculares y agentes para el tratamiento de enfermedades respiratorias. Reivindicacion 1: Un compuesto de formula (1), en la cual R1a es un sustituyente seleccionado del grupo formado por hidrogeno, alquilo(C1-6)-CH-(alquenilo C2-8), cicloalquil alquilo(C1-4), heterocilil alquilo (C1-8), aril alquilo (C1-8), arilo alquinilo(C2-8), heteroaril alquilo(C1-8), (R11)2-N-alquilo(C1-8), R11-O-alquilo(C1-8), -R11-S-alquilo(C1-8), R11-SO-alquilo(C1-8), y R11-SO2-alquilo(C1-8); en el cual el heterociclilo está sustituido en forma opcional con uno a tres sustituyentes seleccionado en forma independiente del grupo formado por alquilo(C1-6) alcoxi(C1-6), alcoxicarbonilo C1-6, alquilcarbonilamino C1-6, alquiltio C1-6, alquilsulfonilo C1-6, halogeno, y oxo; y en el cual el arilo y el heteroarilo están sustituidos en forma opcional con uno a tres sustituyentes seleccionados en forma independiente del grupo formado por alquil(C1-6) alquenilo(C2-6), alcoxi C1-6, amino, alquilamino C1-6, di(alquil C1-6)amino, alquilcarbonilo C1-6, alcoxicarbonilamino C1-6, alquiltio C1-6, alquilsulfonilo C1-6, heterociclilo, ciano, halogeno, hidroxi, trifluorometilo y trifluorometoxi; en los que R11 es hidrogeno, alquilo C1-8 o arilo; R2a es un sustituyente seleccionado de hidrogeno, halogeno, ciano, [1,3]-benzodioxolilo, quinolinilo, tetrazolilo, o arilo; en el cual el arilo está sustituido con uno a tres sustituyentes seleccionados en forma independiente del grupo formado por alquilo C-14, carboxi, amino y carboxi, nitro, di(alquil C1-6)aminocarbonilo, (alquil C1-6)aminocarbonilo, aminocarbonilo, aminosulfonilo, o tetrazolilo; y en el cual el alquilo está sustituido con uno a tres sustituyentes seleccionados de amino, hidroxi, o carboxi; X se selecciona de O, o S; R5 y R6 se seleccionan en forma independiente de hidrogeno o alquilo C1-8; y sus enantiomeros, diastereomeros y sales aceptables desde el punto de vista farmacéutico.They are useful as modulators of the opioid delta receptor or mu opioid. As analgesics, immunosuppressants, anti-inflammatory agents, agents for the treatment of neurological and psychiatric conditions, drugs for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases. Claim 1: A compound of formula (1), wherein R1a is a substituent selected from the group consisting of hydrogen, (C1-6) alkyl -CH- (C2-8 alkenyl), cycloalkyl (C1-4) alkyl, heterocylyl (C1-8) alkyl, aryl (C1-8) alkyl, aryl (C2-8) alkynyl, heteroaryl (C1-8) alkyl, (R11) 2-N-(C1-8) alkyl, R11-O-alkyl (C1-8), -R11-S-(C1-8) alkyl, R11-SO-C1-8 alkyl, and R11-SO2-(C1-8) alkyl; wherein the heterocyclyl is optionally substituted with one to three substituents independently selected from the group consisting of (C1-6) alkyl (C1-6) alkoxy, C1-6 alkoxycarbonyl, C1-6 alkylcarbonylamino, C1-6 alkylthio , C1-6 alkylsulfonyl, halogen, and oxo; and in which the aryl and the heteroaryl are optionally substituted with one to three substituents independently selected from the group consisting of (C 1-6) alkyl (C 2-6) alkenyl, C 1-6 alkoxy, amino, C 1-6 alkylamino 6, di (C1-6 alkyl) amino, C1-6 alkylcarbonyl, C1-6 alkoxycarbonylamino, C1-6 alkylthio, C1-6 alkylsulfonyl, heterocyclyl, cyano, halogen, hydroxy, trifluoromethyl and trifluoromethoxy; wherein R11 is hydrogen, C1-8 alkyl or aryl; R2a is a substituent selected from hydrogen, halogen, cyano, [1,3] -benzodioxolyl, quinolinyl, tetrazolyl, or aryl; in which the aryl is substituted with one to three substituents independently selected from the group consisting of C-14 alkyl, carboxy, amino and carboxy, nitro, di (C1-6 alkyl) aminocarbonyl, (C1-6 alkyl) aminocarbonyl, aminocarbonyl, aminosulfonyl, or tetrazolyl; and in which the alkyl is substituted with one to three substituents selected from amino, hydroxy, or carboxy; X is selected from O, or S; R5 and R6 are independently selected from hydrogen or C1-8 alkyl; and its enantiomers, diastereomers and pharmaceutically acceptable salts.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10/767,712 US20050004163A1 (en) | 2000-03-03 | 2004-01-29 | 3-(diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR047517A1 true AR047517A1 (en) | 2006-01-25 |
Family
ID=36609371
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050100322A AR047517A1 (en) | 2004-01-29 | 2005-01-28 | DERIVATIVES OF 3- (DIARILMETILEN) -8-AZABICICLO (3,2,1) OCTANO |
Country Status (2)
| Country | Link |
|---|---|
| AR (1) | AR047517A1 (en) |
| TW (1) | TW200536852A (en) |
-
2005
- 2005-01-28 AR ARP050100322A patent/AR047517A1/en unknown
- 2005-01-28 TW TW94102558A patent/TW200536852A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| TW200536852A (en) | 2005-11-16 |
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| FB | Suspension of granting procedure |