AR038564A1 - THIOIBOTENIC ACID AND DERIVATIVES OF THE SAME - Google Patents
THIOIBOTENIC ACID AND DERIVATIVES OF THE SAMEInfo
- Publication number
- AR038564A1 AR038564A1 ARP030100528A ARP030100528A AR038564A1 AR 038564 A1 AR038564 A1 AR 038564A1 AR P030100528 A ARP030100528 A AR P030100528A AR P030100528 A ARP030100528 A AR P030100528A AR 038564 A1 AR038564 A1 AR 038564A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- aryl
- heteroaryl
- hydrogen
- Prior art date
Links
- AMHAYEWLPAREES-UHFFFAOYSA-N 2-amino-2-(3-oxo-1,2-thiazol-5-yl)acetic acid Chemical compound OC(=O)C(N)C1=CC(=O)NS1 AMHAYEWLPAREES-UHFFFAOYSA-N 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 abstract 8
- 229910052739 hydrogen Inorganic materials 0.000 abstract 8
- 239000001257 hydrogen Substances 0.000 abstract 8
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 7
- 125000001072 heteroaryl group Chemical group 0.000 abstract 7
- 150000002431 hydrogen Chemical group 0.000 abstract 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 5
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 5
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 4
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 abstract 4
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- -1 aryl (C1-6) alkyl Chemical group 0.000 abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 2
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 2
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 abstract 2
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 abstract 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000006621 (C3-C8) cycloalkyl-(C1-C6) alkyl group Chemical group 0.000 abstract 1
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 235000013922 glutamic acid Nutrition 0.000 abstract 1
- 239000004220 glutamic acid Substances 0.000 abstract 1
- 150000003854 isothiazoles Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Reivindicación 1: Un derivado isotiazol de fórmula 1 ó 2; en las cuales R1 es hidrógeno, alquilo C1-18, alquenilo C2-18, alquinilo C2-18, cicloalquilo C3-8, cicloalquilo(C3-8)-alquilo(C1-6), o aril-alquilo(C1-6); R2 es hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquilo(C3-8)-alquilo(C1-6), arilo, aril-alquilo(C1-6), heteroarilo, heteroaril-alquilo(C1-6); R3 y R4, independientemente están seleccionados entre hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquilo(C3-8)-alquilo(C1-6), arilo, aril-alquilo(C1-6), heteroarilo, heteroaril-alquilo(C1-6), alquilcarbonilo, trifluormetilsulfonilo y alquilsulfonilo C1-6; R5 es hidrógeno, halógeno, ciano, nitro, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquilo(C3-8)-alquilo(C1-6), arilo, aril-alquilo(C1-6), heteroarilo, heteroaril-alquilo(C1-6), amino, alquilamino C1-6, di-(alquilo C1-6)amino, alquilcarbonilo C1-6, aminocarbonilo, alquilaminocarbonilo C1-6, di-(alquiloC1-6)aminocarbonilo, alcoxi C1-6, alquiltio C1-6, hidroxi, trifluormetilo, trifluormetilsulfonilo o alquilsulfonilo C1-6; ó R2 y R5 conjuntamente son -CR7=CR8- ó CR7CR7'-CR8R8'-, donde R7, R7', R8 y R8'-, independientemente están seleccionados entre hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquilo(C3-8)-alquilo(C1-6), arilo, aril-alquilo(C1-6), heteroarilo y heteroaril-alquilo(C1-6); y R6 es hidrógeno, alquilo-hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquilo(C3-8)-alquilo(C1-6), arilo, aril-alquilo(C1-6), heteroarilo, heteroaril-alquilo(C1-6); alquilcarbonilo C1-6, trifluormetilsulfonilo o alquilsulfonilo C1-6, cada arilo y heteroarilo presentes en la molécula puede estar sustituidos con uno o más sustituyentes independientemente seleccionados del grupo que comprende hidrógeno, halógeno, ciano, nitro, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquilo(C3-8)-alquilo(C1-6), arilo, aril-alquilo(C1-6), heteroarilo, heteroaril-alquilo(C1-6), amino, alquilamino C1-6, di-(alquiloC1-6)amino, alquilcarbonilo C1-6, aminocarbonilo, alquilaminocarbonilo C1-6, di-(alquiloC1-6)aminocarbonilo, alcoxi C1-6, alquiltio C1-6, hidroxi, trifluormetilo, trifluormetilsulfonilo o alquilsulfonilo C1-6; o sus sales de adición farmacéuticamente aceptables. Los compuestos de la presente son agonistas en los receptores metabotrópicos de ácido glutámico del grupo II y III.Claim 1: An isothiazole derivative of formula 1 or 2; wherein R1 is hydrogen, C1-18 alkyl, C2-18 alkenyl, C2-18 alkynyl, C3-8 cycloalkyl, (C3-8) cycloalkyl (C1-6) alkyl, or aryl (C1-6) alkyl ; R2 is hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, (C3-8) cycloalkyl (C1-6) alkyl, aryl, aryl (C1-6) alkyl, heteroaryl , heteroaryl (C1-6) alkyl; R3 and R4, independently are selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, (C3-8) cycloalkyl-(C1-6) alkyl, aryl, aryl-alkyl ( C1-6), heteroaryl, heteroaryl (C1-6) alkyl, alkylcarbonyl, trifluoromethylsulfonyl and C1-6 alkylsulfonyl; R5 is hydrogen, halogen, cyano, nitro, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, (C3-8) cycloalkyl (C1-6) alkyl, aryl, aryl-alkyl ( C1-6), heteroaryl, heteroaryl (C1-6) alkyl, amino, C1-6 alkylamino, di- (C1-6 alkyl) amino, C1-6 alkylcarbonyl, aminocarbonyl, C1-6 alkylaminocarbonyl, di- (C1- alkyl 6) aminocarbonyl, C1-6 alkoxy, C1-6 alkylthio, hydroxy, trifluoromethyl, trifluoromethylsulfonyl or C1-6 alkylsulfonyl; or R2 and R5 together are -CR7 = CR8- or CR7CR7'-CR8R8'-, where R7, R7 ', R8 and R8'-, independently are selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2- alkynyl 6, C3-8 cycloalkyl, (C3-8) cycloalkyl (C1-6) alkyl, aryl, aryl (C1-6) alkyl, heteroaryl and heteroaryl (C1-6) alkyl; and R 6 is hydrogen, alkyl-hydrogen, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-6 alkyl, aryl, aryl C 1-6 alkyl -6), heteroaryl, heteroaryl (C1-6) alkyl; C1-6 alkylcarbonyl, trifluoromethylsulfonyl or C1-6 alkylsulfonyl, each aryl and heteroaryl present in the molecule may be substituted with one or more substituents independently selected from the group comprising hydrogen, halogen, cyano, nitro, C1-6 alkyl, C2- alkenyl 6, C2-6 alkynyl, C3-8 cycloalkyl, (C3-8) cycloalkyl (C1-6) alkyl, aryl, aryl (C1-6) alkyl, heteroaryl, heteroaryl (C1-6) alkyl, amino, C1-6 alkylamino, di- (C1-6 alkyl) amino, C1-6 alkylcarbonyl, aminocarbonyl, C1-6 alkylaminocarbonyl, di- (C1-6 alkyl) aminocarbonyl, C1-6 alkoxy, C1-6 alkylthio, hydroxy, trifluoromethyl, trifluoromethylsulfonyl or C1-6 alkylsulfonyl; or its pharmaceutically acceptable addition salts. The compounds herein are agonists in the metabotropic glutamic acid receptors of group II and III.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA200200258 | 2002-02-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR038564A1 true AR038564A1 (en) | 2005-01-19 |
Family
ID=42777114
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030100528A AR038564A1 (en) | 2002-02-19 | 2003-02-18 | THIOIBOTENIC ACID AND DERIVATIVES OF THE SAME |
Country Status (1)
| Country | Link |
|---|---|
| AR (1) | AR038564A1 (en) |
-
2003
- 2003-02-18 AR ARP030100528A patent/AR038564A1/en not_active Application Discontinuation
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