CO5190697A1 - Aminoalcoxicarbazoles para el tratamiento de enfermedades del snc - Google Patents

Aminoalcoxicarbazoles para el tratamiento de enfermedades del snc

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Publication number
CO5190697A1
CO5190697A1 CO00066777A CO00066777A CO5190697A1 CO 5190697 A1 CO5190697 A1 CO 5190697A1 CO 00066777 A CO00066777 A CO 00066777A CO 00066777 A CO00066777 A CO 00066777A CO 5190697 A1 CO5190697 A1 CO 5190697A1
Authority
CO
Colombia
Prior art keywords
alkyl
substituted
cycloalkyl
independently
optionally substituted
Prior art date
Application number
CO00066777A
Other languages
English (en)
Inventor
Ruth E Tenbrink
Original Assignee
Upjohn Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Upjohn Co filed Critical Upjohn Co
Publication of CO5190697A1 publication Critical patent/CO5190697A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P25/32—Alcohol-abuse
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/88—Carbazoles; Hydrogenated carbazoles 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 to carbon atoms of the ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Abstract

Un compuesto de la fórmula I<EMI FILE="00066777_1" ID="1" IMF=JPEG >o su sal farmacéuticamente aceptable, racemato, solvato, tautómero, isómero óptico o su derivado profármaco; en dondeR1 es(a) H,(b) halo, o(c) C1-6 aIquilo;cada R2 es independientemente(a) H,(b) halo,(c) -OH,(d) -CN,(e) -CF3,(f) -O(C1-6)aIquilo,(g) C1-6 aIquilo,(h) C3-6 cicloalquilo,(i) -NR5R6,U) -CONR5R6,(k) -SO2NR5R6,O) -COOR7,(m) -OCF3, o(n) fenilo, opcionalmente substituido con halo, OH, O(C1-4) alquilo, o C1-6 alquilo;cada R3 es independientemente(a) H,(b) C1-6 alquilo, o(c) C3-6 cicloalquilo;R4 es( a) arilo, o(b) heteroarilo;R5 y R6 son independientemente(a) H,(b) C1-6 alquilo, o(c) C3-6 cicloalquilo;R7 es(a) H,(b) C1-6 alquilo, o(c) (C1-3 alquil)-fenilo en donde el fenilo puede estar substituido con R3;R8 y R9 son independientemente(a) H,(b) C1-6 alquilo, opcionalmente substituido con arilo, heteroarilo, o C3-6 cicloalquilo,(c) C2-6 alqueno,(d) C3-6 cicloalquilo,- 2 -(e) C2-6 alquilo substituido con R10,(f) -CHO, siempre que solamente uno de R8 y R9 sea CHO, y el otro sea H,(g) arilo,(h) heterociclo, en donde el heterociclo está unido a través de un átomo de carbono al nitrógeno al cual está unido,o(i) R8 y R9 conjuntamente con el nitrógeno al cual están unidos forman un anillo heterocíclico en donde el anillo heterocíclico puede tener uno o dos heteroátomos seleccionados del grupo integrado por oxígeno, azufre y N(Y) y en donde los átomos de carbono del anillo heterocíclico están opcionalmente substituidos con uno o dos R14;R10 es (a) -OH,(b) -O(C1-4 alquilo) opcionalmente el alquilo está sustituido con OH,(c) -O(C1-4 alquil)-NR11R12,(d) heterociclo, o(e) -CO2R5,R11 y R12 son independientemente,(a) H, o(b) C1-4 alquilo;arilo es fenilo o naftilo, opcionalmente substituido con uno o más R13;heteroarilo es un radical que es un anillo aromático monocíclico de cinco o seis miembros,con uno o dos heteroátomos, cada uno seleccionado del grupo integrado por oxígeno,azufre, y N(X), o un radical que es un anillo aromático bicíclico ortofusionado de nueve o diez miembros, que tiene uno, dos o tres heteroátomos, cada uno seleccionado del grupo integrado por oxígeno, azufre, y N(X); en donde los átomos de carbono del heteroarilo pueden estar substituidos con R13; heterociclo es un radical que es un anillo heterocíclico parcialmente saturado o no saturado, de cinco, seis o siete miembros, con uno, dos o tres heteroátomos seleccionados del grupo integrado por oxígeno, azufre y N(Y), en donde los átomos de carbono del anillo heterocíclico pueden estar substituidos con R14;X esta ausente, o es H o C1-4 alquilo;Y es(a) H,(b) C1-6 alquilo, opcionalmente substituido con arilo o heteroarilo, (c) C3-6 cicloalquilo, o(d) C2-6 alquilo substituido con -OH, -O(C1-4 alquilo), -O(C1-4 alquil)-NR11R12,-CO2R5, o NHCHO, o(e) -OH;R13 es(a) halo,(b) -OH,(c) -CN,(d) -CF3,(e) -O(C1-6)alquilo,(f) C1-6 alquilo,(g) C3-6 cicloalquilo,(h) -NR5R6,(i) -CONR5R6,(j ) -SO2NR5R6,(k) -COOR7,(I) -OCF3, o(m) fenilo, opcionalmente substituido con halo, OH, O(C1 -4) alquilo, o C1-6 alquilo;R14 es(a) C1-6 alquilo,(b) C3-6 cicloalquilo,(c) C2-6 alquilo substituido con -OH, -O(C1-4 alquilo), -O(C1-4 alquil)-NR11R12, o -CO2R5,(d) -OH, o(e) oxo (=O);m es 1, 2, 3 ó 4;n es 1, 2, 3, ó 4;En el C3-6 cicloalquilo de cada una de las definiciones anteriores, cada uno puede estar substituido independientemente con -OH, C1-4 alquilo, u oxo (=O), y con las siguientes condiciones :(a) cuando R4 es 4-fluorofenilo, n es 1, m es 1, cada R3 es independientemente hidrógeno, R8 y R9 es independientemente -CH2CH3, entonces R2 no puede ser fluoro o cloro en la posición C-6 de la fórmula I;(b) cuando n es 1, m es 1, R2, R3, R8 o R9 son hidrógeno, R4 es 4-tiazolilo, entonces dicho 4-tiazolilo no puede estar substituido con 4-clorofenilo;(c) cuando n es 1, m es 1, R2, R3, R8 o R9 son hidrógeno, entonces R4 no es 4-piridilo;(d) cuando n es 1, m es 1, R2, R3, R8 o R9 son hidrógeno, entonces no es 2-bromofenilo o 4-bromofenilo.
CO00066777A 1999-09-07 2000-09-05 Aminoalcoxicarbazoles para el tratamiento de enfermedades del snc CO5190697A1 (es)

Applications Claiming Priority (2)

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US15263899P 1999-09-07 1999-09-07
US20377100P 2000-05-12 2000-05-12

Publications (1)

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CO5190697A1 true CO5190697A1 (es) 2002-08-29

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US (1) US6514968B1 (es)
EP (1) EP1210329A2 (es)
JP (1) JP2003508518A (es)
KR (1) KR20020027622A (es)
CN (1) CN1169789C (es)
AR (1) AR032592A1 (es)
AU (1) AU780190B2 (es)
BR (1) BR0013767A (es)
CA (1) CA2380763A1 (es)
CO (1) CO5190697A1 (es)
MX (1) MXPA02002496A (es)
MY (1) MY125942A (es)
NZ (1) NZ517661A (es)
PE (1) PE20010522A1 (es)
WO (1) WO2001017963A2 (es)

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CN107325143B (zh) * 2017-08-07 2019-09-10 连云港恒运药业有限公司 氟维司群中间体合成方法
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AR032592A1 (es) 2003-11-19
PE20010522A1 (es) 2001-04-28
CA2380763A1 (en) 2001-03-15
WO2001017963A3 (en) 2001-11-15
WO2001017963A2 (en) 2001-03-15
AU7053200A (en) 2001-04-10
MXPA02002496A (es) 2002-07-30
AU780190B2 (en) 2005-03-03
NZ517661A (en) 2004-02-27
CN1372547A (zh) 2002-10-02
EP1210329A2 (en) 2002-06-05
MY125942A (en) 2006-09-29
CN1169789C (zh) 2004-10-06
BR0013767A (pt) 2002-06-25
US6514968B1 (en) 2003-02-04
JP2003508518A (ja) 2003-03-04
KR20020027622A (ko) 2002-04-13

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