AR058022A1 - DERIVATIVES OF BENZOOXAZOLES, PHARMACEUTICAL COMPOSITIONS AND ITS USE FOR THE TREATMENT OF NERVOUS SYSTEM DISORDERS. - Google Patents
DERIVATIVES OF BENZOOXAZOLES, PHARMACEUTICAL COMPOSITIONS AND ITS USE FOR THE TREATMENT OF NERVOUS SYSTEM DISORDERS.Info
- Publication number
- AR058022A1 AR058022A1 ARP060103590A AR058022A1 AR 058022 A1 AR058022 A1 AR 058022A1 AR P060103590 A ARP060103590 A AR P060103590A AR 058022 A1 AR058022 A1 AR 058022A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- halogen
- treatment
- mono
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 208000012902 Nervous system disease Diseases 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 5
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 4
- -1 SCF3 Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 3
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 abstract 2
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 abstract 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000006594 (C1-C3) alkylsulfony group Chemical group 0.000 abstract 1
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 206010003805 Autism Diseases 0.000 abstract 1
- 208000020706 Autistic disease Diseases 0.000 abstract 1
- 206010012335 Dependence Diseases 0.000 abstract 1
- 208000011688 Generalised anxiety disease Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 208000020114 Schizophrenia and other psychotic disease Diseases 0.000 abstract 1
- 208000012886 Vertigo Diseases 0.000 abstract 1
- DGYIJVNZSDYBOE-UHFFFAOYSA-N [CH2]C1=CC=NC=C1 Chemical group [CH2]C1=CC=NC=C1 DGYIJVNZSDYBOE-UHFFFAOYSA-N 0.000 abstract 1
- 230000016571 aggressive behavior Effects 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 235000019788 craving Nutrition 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 208000029364 generalized anxiety disease Diseases 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 208000019906 panic disease Diseases 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003053 piperidines Chemical class 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
- 231100000889 vertigo Toxicity 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
- C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
En realizaciones de la misma, compuestos específicos descriptos en la presente son utilizados para la fabricacion de un medicamento util en el tratamiento de desordenes del SNC, en particular el tratamiento de desordenes de ansiedad, incluyendo desorden de ansiedad generalizada y desorden de pánico, desorden obsesivo compulsivo, agresion, adiccion (incluyendo ansia), depresion, autismo, vértigo, esquizofrenia y otros desordenes psicoticos, enfermedad de Parkinson y disturbios del conocimiento y memoria. Métodos para su preparacion y composiciones farmacéuticas que los comprenden. Reivindicacion 1: Derivados de piperazina y piperidina de la formula general (1) en donde R1 es hidrogeno, halogeno alquilo C1-3, CN, CF3, OCF3, SCF3, alcoxi C1-3, amino o mono- o dialquil C1-3 sustituido amino, o hidroxi; ---Z representa =C o -N; R2 es hidrogeno o alquilo C1-3; R3 y R4 independientemente representan H o alquilo C1-3, o R3 y R4 juntos puede formar un puente de 2 o 3 átomos de carbono; Q es metilo, etilo o ciclopropilmetilo los cuales grupos etilo o ciclopropilmetilo están opcionalmente sustituidos con uno o más átomos de fluor, o Q es bencilo o 2-, 3- o 4-piridilmetilo, los cuales grupos están opcionalmente sustituidos con uno o más sustituyentes del grupo halogeno, nitro, ciano, amino, mono- o dialquil C1-3amino, alcoxi C1-3, CF3, OCF3, SCF3, alquilo C1-3, alquil C1-3sulfonilo o hidroxilo, o Q es un grupo de la formula (2) en donde R5 es halogeno, hidroxi, alcoxi C1-3 o alquilo C1-3; y q es 0, 1, 2 o 3; Y es fenilo, furanilo o tienilo, los cuales pueden estar sustituidos con 1-3 sustituyentes del grupo hidroxi, halogeno, alcoxi C1-3, alquilo C1-3, ciano, aminocarbonilo, mono- o dialquil C1- 3aminocarbonilo; y tautomeros, estereoisomeros, sales, hidratos y solvatos de los mismos farmacologicamente aceptables.In embodiments thereof, specific compounds described herein are used for the manufacture of a medicament useful in the treatment of CNS disorders, in particular the treatment of anxiety disorders, including generalized anxiety disorder and panic disorder, obsessive disorder. compulsive, aggression, addiction (including craving), depression, autism, vertigo, schizophrenia and other psychotic disorders, Parkinson's disease and disturbances of knowledge and memory. Methods for their preparation and pharmaceutical compositions that comprise them. Claim 1: Piperazine and piperidine derivatives of the general formula (1) wherein R1 is hydrogen, halogen C1-3 alkyl, CN, CF3, OCF3, SCF3, C1-3 alkoxy, amino or mono- or substituted C1-3 dialkyl amino, or hydroxy; --- Z represents = C or -N; R2 is hydrogen or C1-3 alkyl; R3 and R4 independently represent H or C1-3 alkyl, or R3 and R4 together can form a bridge of 2 or 3 carbon atoms; Q is methyl, ethyl or cyclopropylmethyl which ethyl or cyclopropylmethyl groups are optionally substituted with one or more fluorine atoms, or Q is benzyl or 2-, 3- or 4-pyridylmethyl, which groups are optionally substituted with one or more substituents of the halogen, nitro, cyano, amino, mono- or dialkyl C1-3amino, C1-3 alkoxy, CF3, OCF3, SCF3, C1-3 alkyl, C1-3 alkyl sulfonyl or hydroxyl group, or Q is a group of the formula ( 2) wherein R5 is halogen, hydroxy, C1-3 alkoxy or C1-3 alkyl; and q is 0, 1, 2 or 3; Y is phenyl, furanyl or thienyl, which may be substituted with 1-3 substituents of the hydroxy, halogen, C1-3 alkoxy, C1-3 alkyl, cyano, aminocarbonyl, mono- or C1-3-dialkylcarbonyl group; and pharmacologically acceptable tautomers, stereoisomers, salts, hydrates and solvates thereof.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05107671 | 2005-08-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR058022A1 true AR058022A1 (en) | 2008-01-23 |
Family
ID=35502590
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060103590 AR058022A1 (en) | 2005-08-22 | 2006-08-17 | DERIVATIVES OF BENZOOXAZOLES, PHARMACEUTICAL COMPOSITIONS AND ITS USE FOR THE TREATMENT OF NERVOUS SYSTEM DISORDERS. |
Country Status (6)
| Country | Link |
|---|---|
| CN (1) | CN101248053B (en) |
| AR (1) | AR058022A1 (en) |
| BR (1) | BRPI0614843A2 (en) |
| TW (1) | TW200738656A (en) |
| UA (1) | UA94718C2 (en) |
| ZA (1) | ZA200800741B (en) |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE503170A (en) * | 1975-09-02 | |||
| US6225312B1 (en) * | 1996-03-29 | 2001-05-01 | Duphar International Research B.V. | Piperazine and piperidine compounds |
| UA71590C2 (en) * | 1998-11-13 | 2004-12-15 | Duphar Int Res | Piperazine and piperidine derivatives |
| CZ301464B6 (en) * | 2000-05-12 | 2010-03-10 | Solvay Pharmaceuticals B. V. | Piperazine and piperidine compounds, process of their preparation and pharmaceutical preparations in which the compounds are comprised |
| US20050085510A1 (en) * | 2002-01-16 | 2005-04-21 | Telefonaktiebolaget Lm Ericsson (Publ) | Prucalopride-n-oxide |
-
2006
- 2006-08-17 AR ARP060103590 patent/AR058022A1/en not_active Application Discontinuation
- 2006-08-18 TW TW095130407A patent/TW200738656A/en unknown
- 2006-08-21 BR BRPI0614843-3A patent/BRPI0614843A2/en not_active IP Right Cessation
- 2006-08-21 UA UAA200803586A patent/UA94718C2/en unknown
- 2006-08-21 CN CN2006800306608A patent/CN101248053B/en not_active Expired - Fee Related
-
2008
- 2008-01-24 ZA ZA200800741A patent/ZA200800741B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN101248053A (en) | 2008-08-20 |
| ZA200800741B (en) | 2009-01-28 |
| HK1120261A1 (en) | 2009-03-27 |
| TW200738656A (en) | 2007-10-16 |
| CN101248053B (en) | 2011-06-01 |
| BRPI0614843A2 (en) | 2012-12-04 |
| UA94718C2 (en) | 2011-06-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |