AR007742A1 - FUSIONED PYROLCARBOXANILIDES; A NEW KIND OF LIGAND GABA BRAIN RECEPTORS. - Google Patents
FUSIONED PYROLCARBOXANILIDES; A NEW KIND OF LIGAND GABA BRAIN RECEPTORS.Info
- Publication number
- AR007742A1 AR007742A1 ARP970103190A ARP970103190A AR007742A1 AR 007742 A1 AR007742 A1 AR 007742A1 AR P970103190 A ARP970103190 A AR P970103190A AR P970103190 A ARP970103190 A AR P970103190A AR 007742 A1 AR007742 A1 AR 007742A1
- Authority
- AR
- Argentina
- Prior art keywords
- hydrogen
- substituted
- pyrolcarboxanilides
- fusioned
- hydroxy
- Prior art date
Links
- 210000004556 brain Anatomy 0.000 title abstract 3
- 229960003692 gamma aminobutyric acid Drugs 0.000 title 1
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 title 1
- 239000003446 ligand Substances 0.000 title 1
- 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
- 239000000556 agonist Substances 0.000 abstract 3
- 102000005915 GABA Receptors Human genes 0.000 abstract 2
- 108010005551 GABA Receptors Proteins 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 239000005557 antagonist Substances 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 229940049706 benzodiazepine Drugs 0.000 abstract 1
- 150000001557 benzodiazepines Chemical class 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 238000003745 diagnosis Methods 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- -1 hydroxy, nitro, amino Chemical group 0.000 abstract 1
- 230000006993 memory improvement Effects 0.000 abstract 1
- 231100000252 nontoxic Toxicity 0.000 abstract 1
- 230000003000 nontoxic effect Effects 0.000 abstract 1
- 125000000962 organic group Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 208000019116 sleep disease Diseases 0.000 abstract 1
- 208000023516 stroke disease Diseases 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente invención comprende estructuras de la fórmula: I o las sales no tóxicas farmacéuticamente aceptables de la misma donde la porción cíclica C esde fórmulas (II), (III), (IV) o (V), y donde: W representa fenilo sustituido o nosustituido; X es hidrógeno, hidroxi o alquilo inferior; Y representa N-R7o un átomo de carbono sustituido; T es hidrógeno, halógeno, hidroxi, nitro, amino o alquilo; R3 es hidrógeno o un grupo órganico; R4 es hidrógeno o un sustituyente orgánicosustituido o no sustituido; R5 y R6 representan sustituyentes orgánicos, inorgánicos; y n es 1, 2, 3 o 4, cuyos compuestos son agonistasaltamente selectivos, antagonistas o agonistas inversos para receptores GABA del cerebro o prodrogas deagonistas, antag onistas o agonistas inversos parareceptores GABA del cerebro. Estos compuestos son útiles en el diagnóstico y tratamiento de la ansiedad, sueno y desórdenes de apoplejía, sobredosis condrogas, benzodiazepinas y para elmejoramiento de la memoria.The present invention comprises structures of the formula: I or the pharmaceutically acceptable non-toxic salts thereof where the cyclic portion C is from formulas (II), (III), (IV) or (V), and where: W represents substituted phenyl or not substituted; X is hydrogen, hydroxy, or lower alkyl; Y represents N-R7 or a substituted carbon atom; T is hydrogen, halogen, hydroxy, nitro, amino or alkyl; R3 is hydrogen or an organic group; R4 is hydrogen or an substituted or unsubstituted organic substituent; R5 and R6 represent organic, inorganic substituents; and n is 1, 2, 3 or 4, the compounds of which are highly selective agonists, antagonists or inverse agonists for brain GABA receptors or deagonist, antagonist or inverse agonists prodrugs for brain GABA receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and stroke disorders, overdose of chondrogens, benzodiazepines, and for memory enhancement.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US68306693A | 1993-05-25 | 1993-05-25 | |
| US08/683,066 US5750702A (en) | 1993-10-27 | 1996-07-16 | Certain pyrrolo pyridine-3-carboxamides; a new class of GABA brain receptor ligands |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR007742A1 true AR007742A1 (en) | 1999-11-10 |
Family
ID=51929774
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP970103190A AR007742A1 (en) | 1993-05-25 | 1997-07-16 | FUSIONED PYROLCARBOXANILIDES; A NEW KIND OF LIGAND GABA BRAIN RECEPTORS. |
Country Status (1)
| Country | Link |
|---|---|
| AR (1) | AR007742A1 (en) |
-
1997
- 1997-07-16 AR ARP970103190A patent/AR007742A1/en not_active Application Discontinuation
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |