AR035493A1 - Derivados de azepino (4,5b) indolina sustituidos, composicion farmaceutica y el uso de dichos derivados para preparar un medicamento - Google Patents
Derivados de azepino (4,5b) indolina sustituidos, composicion farmaceutica y el uso de dichos derivados para preparar un medicamentoInfo
- Publication number
- AR035493A1 AR035493A1 ARP010104449A ARP010104449A AR035493A1 AR 035493 A1 AR035493 A1 AR 035493A1 AR P010104449 A ARP010104449 A AR P010104449A AR P010104449 A ARP010104449 A AR P010104449A AR 035493 A1 AR035493 A1 AR 035493A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrocarbylene
- hydrogen
- independently
- het
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Diabetes (AREA)
- Addiction (AREA)
- Child & Adolescent Psychology (AREA)
- Anesthesiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Indole Compounds (AREA)
Abstract
Derivados de azepino[4,5b]indolina sustituidos, que comprenden un compuesto de Fórmula (1) en la cual R1 está seleccionado del grupo que consiste en hidrógeno, alquilo C1-8 y hidrocarbileno C1-8 Ar, cada R2 independientemente está seleccionado del grupo que consiste en alquilo C1-8, y OH; R3 es hidrógeno, alquilo C1-8, Ar, Het, R7C(=O)-, R7OC(=O)-, R5R6NC(=O)-, R7C(=S)-, R7SC(=O)-, R5R6NC(=S)-, R7SO2-, R5R6NSO2, R7S(=O)-, R5R6NS(=O)-, Rc hidrocarbileno C1-8, o Rc hidrocarbileno C1-8 C(=O)-; cada R4, independientemente , esta seleccionado del grupo que consiste en Ar, alquilo C1-8, ArO-, alcoxi C1-8, Het, halo, OH, CN, NO2, CF3, CF3O, NRaRb, N=CRaRb, R7S, hidrocarbileno C1-8 Ar, e hidrocarbileno C1-8 ORa; cada R5 y R6 es independientemente hidrógeno, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, haloalquilo C1-8, cicloalquenilo C3-8, Ar, o hidrocarbileno C1-8 Ar; o R5 y R6 conjuntamente con el nitrógeno al cual están unidos forman un anillo pirrolidino, piperidino, morfolino, o tiomorfolino, cada R7 es independientemente hidrógeno, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, haloalquilo C1-8, cicloalquenilo C3-8, Ar, o hidrocarbileno C1-8 Ar, Ra y Rb, independientemente, están seleccionados del grupo que consiste en hidrógeno, alquilo C1-8, Ar, hidrocarbileno C1-3 Ar, SO2Ar, SO2 alquilo C1-4, (cicloalquilo C3-8) alquilo C1-8, y Het; Rc es Ar, Het, R7CO2-, R7C(=O)-, R7OC(=O)-, R7O-, R7 alquileno C1-8 O-, R7S-, R7C(=S)-, R7S(=O)-, R7S(=O)2-, R7SC(=O)-, R7C(=O)N(R7)-, R7C(=S)N(R7)-, R5R6N-, R5R6NC(=O)-, R5R6NC(=S)-, R5R6NS(=O)-, R5R6NSO2-, R7S(=O)N(R7)-, R7SO2N(R7)-, o R7N(R7)C(=O)N(R7)-; cada Ar es independientemente arilo o heteroarilo; p es 0, 1, 2, 3, o 4; y q es 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 o 10; donde Ar de R1, R3- R7, Ra, Rb y Rc está opcionalmente sustituido con uno o más (por ejemplo 1, 2, 3, 4 o 5) sustituyentes independientemente seleccionados de halo, CN, NO2, ORe, metilendioxi, etilendioxi, CF3, OCF3, SRe, SO2Re, NRfRg, CONRfRg, CORe, Re e hidrocarbileno Rd C1-8, cada Rd es independientemente hidroxi, alcoxi C1-8, ciano, SRh o C(=O)Rh, cada Re está independientemente seleccionado del grupo que consiste en hidrógeno, alquilo C1-8, Ar, hidrocarbileno Ar C1-3, SO2Ar, SO2alquilo C1-4, (cicloalquilo C3-8) alquilo C1-8 y Het; donde cualquier Ar de Re está opcionalmente sustituido con uno o más (por ejemplo 1, 2, 3, 4 o 5) sustituyentes independientemente seleccionados de halo, CN, NO2, ORd, metilendioxi, etilendioxi, CF3, OCF3, SRf, SO2Rf, NRfRg, CONRfRg, CORf, Rf e hidrocarbileno Rd C1-8; cada Rf y Rg está independientemente seleccionado del grupo que consiste en hidrógeno, alquilo C1-8, Ar, hidrocarbileno Ar C1-3, SO2Ar, SO2 alquilo C1-4, (cicloalquilo C3-8) alquilo C1-8 y Het; y cada Rh es independientemente hidrógeno, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, halolaquilo C1-8, cicloalquenilo C3-8, fenilo o hidrocarbileno (fenilo) C1-8; o una sal farmacéuticamente aceptable del mismo; con la condición de que cuando (a) R1 es metilo; y (b) R3 hidrógeno o -(CH2)3NR5R6, donde, R5 y R6 son cada uno metilo; entonces p y q no son cada uno 0, y composiciones farmacéuticas que contienen dichos compuestos o sales. Los compuestos y sales son ligandos 5-HT y son útiles para tratar enfermedades, desórdenes, y/o condiciones de un mamífero en el cual está implicada la actividad de un receptor 5-HT. Los compuestos y sales son particularmente útiles para tratar enfermedades del sistema nervioso central. También se refiere al uso de dichos derivados para preparar medicamentos útiles para tratar una enfermedad del sistema nervioso central.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US23437600P | 2000-09-20 | 2000-09-20 | |
US26604701P | 2001-02-01 | 2001-02-01 | |
US30196401P | 2001-06-29 | 2001-06-29 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR035493A1 true AR035493A1 (es) | 2004-06-02 |
Family
ID=27398561
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP010104450A AR034264A1 (es) | 2000-09-20 | 2001-09-20 | Derivados azepino(4,5-b)indol sustituidos y composiciones farmaceuticas |
ARP010104449A AR035493A1 (es) | 2000-09-20 | 2001-09-20 | Derivados de azepino (4,5b) indolina sustituidos, composicion farmaceutica y el uso de dichos derivados para preparar un medicamento |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP010104450A AR034264A1 (es) | 2000-09-20 | 2001-09-20 | Derivados azepino(4,5-b)indol sustituidos y composiciones farmaceuticas |
Country Status (7)
Country | Link |
---|---|
US (4) | US6583135B2 (es) |
EP (2) | EP1319005A2 (es) |
JP (2) | JP2004509894A (es) |
AR (2) | AR034264A1 (es) |
AU (2) | AU2001292898A1 (es) |
PE (2) | PE20020443A1 (es) |
WO (2) | WO2002024701A2 (es) |
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FR2663935A1 (fr) | 1990-06-27 | 1992-01-03 | Adir | Nouveaux 1,2,3,4,5,6-hexahydroazepino [4,5-b] indoles et 1,2,3,4-tetrahydrobethacarbolines, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent. |
PE20010052A1 (es) | 1999-04-23 | 2001-01-27 | Upjohn Co | Compuestos de azepinindol tetraciclico como agonistas o antagonistas del receptor de 5-ht |
MXPA01012969A (es) * | 1999-06-15 | 2003-10-14 | Bristol Myers Squibb Pharma Co | Gamma-carbolinas fusionadas de heterociclo sustituido. |
DE19929076A1 (de) | 1999-06-25 | 2000-12-28 | Aventis Pharma Gmbh | Indanylsubstituierte Benzolcarbonamide, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament sowie sie enthaltende pharmazeutische Zubereitungen |
MY122278A (en) | 1999-07-19 | 2006-04-29 | Upjohn Co | 1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles containing arylsulfones at the 9-position |
AU2001269781A1 (en) * | 2000-07-06 | 2002-01-21 | Pharmacia And Upjohn Company | Substituted 2,3,7,8,9,10,11,12-octahydroazepino(4,5-b)pyrano(3,2-e) indoles |
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2001
- 2001-09-20 PE PE2001000945A patent/PE20020443A1/es not_active Application Discontinuation
- 2001-09-20 AU AU2001292898A patent/AU2001292898A1/en not_active Abandoned
- 2001-09-20 EP EP01975267A patent/EP1319005A2/en not_active Withdrawn
- 2001-09-20 AU AU2001294606A patent/AU2001294606A1/en not_active Abandoned
- 2001-09-20 EP EP01973304A patent/EP1319004A2/en not_active Withdrawn
- 2001-09-20 WO PCT/US2001/029535 patent/WO2002024701A2/en not_active Application Discontinuation
- 2001-09-20 JP JP2002529111A patent/JP2004509894A/ja not_active Withdrawn
- 2001-09-20 US US09/957,625 patent/US6583135B2/en not_active Expired - Fee Related
- 2001-09-20 AR ARP010104450A patent/AR034264A1/es unknown
- 2001-09-20 AR ARP010104449A patent/AR035493A1/es not_active Application Discontinuation
- 2001-09-20 WO PCT/US2001/029447 patent/WO2002024700A2/en not_active Application Discontinuation
- 2001-09-20 PE PE2001000944A patent/PE20020510A1/es not_active Application Discontinuation
- 2001-09-20 JP JP2002529110A patent/JP2004509893A/ja active Pending
- 2001-09-20 US US09/957,319 patent/US6586421B2/en not_active Expired - Fee Related
-
2003
- 2003-03-20 US US10/394,676 patent/US6828314B2/en not_active Expired - Fee Related
- 2003-03-20 US US10/393,968 patent/US6903090B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
JP2004509894A (ja) | 2004-04-02 |
PE20020510A1 (es) | 2002-06-12 |
AU2001294606A1 (en) | 2002-04-02 |
AR034264A1 (es) | 2004-02-18 |
EP1319004A2 (en) | 2003-06-18 |
US6828314B2 (en) | 2004-12-07 |
US6903090B2 (en) | 2005-06-07 |
US6586421B2 (en) | 2003-07-01 |
US20020107278A1 (en) | 2002-08-08 |
JP2004509893A (ja) | 2004-04-02 |
US20020077318A1 (en) | 2002-06-20 |
WO2002024700A3 (en) | 2002-06-13 |
US20030220321A1 (en) | 2003-11-27 |
EP1319005A2 (en) | 2003-06-18 |
AU2001292898A1 (en) | 2002-04-02 |
US20030225058A1 (en) | 2003-12-04 |
WO2002024700A2 (en) | 2002-03-28 |
US6583135B2 (en) | 2003-06-24 |
WO2002024701A3 (en) | 2002-06-13 |
PE20020443A1 (es) | 2002-05-16 |
WO2002024701A2 (en) | 2002-03-28 |
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