AR071067A1 - Ciclohexildiaminas sustituidas - Google Patents

Ciclohexildiaminas sustituidas

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Publication number
AR071067A1
AR071067A1 ARP090101057A ARP090101057A AR071067A1 AR 071067 A1 AR071067 A1 AR 071067A1 AR P090101057 A ARP090101057 A AR P090101057A AR P090101057 A ARP090101057 A AR P090101057A AR 071067 A1 AR071067 A1 AR 071067A1
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AR
Argentina
Prior art keywords
nhc
nhr0
aliphatic
ring
so3h
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ARP090101057A
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English (en)
Inventor
Saskia Zemolka
Bert Nolte
Hans Schick
Klaus Linz
Derek John Saunders
Fritz Theil
Helmut Sonnenschein
Werner Englberger
Wolfgang Schroder
Jens Kaufmann
Gebauer Julian Dr
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Gruenenthal Chemie
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Publication of AR071067A1 publication Critical patent/AR071067A1/es

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    • 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
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/20—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
    • 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
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/22—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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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

Se refiere a compuestos, que poseen afinidad con el receptor de opioides m y con el receptor ORL-1, a medicamentos que contienen estos compuestos y al uso de estos compuestos para la fabricacion de medicamentos. Reivindicacion 1: Compuesto de la formula general (1) en la que Y1, Y1', Y2, Y2', Y3, Y3', Y4 e Y4' se eligen en cada caso con independencia entre sí entre el grupo formado por -H, -F, -Cl, -Br, -I, -CN, -NO2, -CHO, -R0, -C(=O)R0, -C(=O)H, -C(=O)-OH, -C(=O)OR0, -C(=O)NH2, -C(=O)NHR0, -C(=O)N(R0)2, -OH, -OR0, -OC(=O)H, -OC(=O)R0, -OC(=O)OR0, -OC(=O)NHR0, -OC(=O)N(R0)2, -SH, -SR0, -SO3H, -S(=O)1-2-R0, -S(=O)1-2NH2, -NH2, -NHR0, -N(R0)2, -N+(R0)3, -N+(R0)2O-, -NHC(=O)R0, -NHC(=O)OR0, -NHC(=O)NH2, -NHC(=O)NHR0, -NHC(=O)N(R0)2; o Y1 e Y1', o Y2 e Y2', o Y3 e Y3', o Y4 e Y4' significan juntos =O; Q significa -R0; X significa =O, =CR6R7 o =N-R6; R0 en cada caso con independencia significa -alifático C1-8, -cicloalifático C3-12, -arilo, -heteroarilo, -alifático C1-8-cicloalifático C3-12, -alifático C1-8-arilo, -alifático C1-8-heteroarilo, -cicloalifático C3-8-alifático C1-8, -cicloalifático C3-8-arilo o -cicloalifático C3-8-heteroarilo; R1 y R2, con independencia entre sí significan -H o -R0; o R1 y R2 juntos significan -CH2CH2OCH2CH2-, -(CH2)3-6- o -CH2CH2N-R'CH2CH2-, en el que R' significa -H, -R0 o -C(=O)R0; R3 significa -R0; R4 significa -H, -C(=O)R0- o R0; R5 significa -H, -F, -Cl, -Br, -I, -CN, -NO2, -CHO, -R0, -C(=O)H, -C(=O)R0, -C(=O)OH, -C(=O)OR0, -C(=O)NH2, -C(=O)NHR0, -C(=O)N(R0)2, -N(R0)2, -N+(R0)3, -N+(R0)2O-, -SH, -SR0, -SO3H, -S(=O)1-2-R0, -S(=O)1-2NH2, -NH2, -NHR0, -N(R0)2, -N+(R0)3, -N+(R0)2O-, -NHC(=O)R0, -NHC(=O)OR0, -NHC(=O)NH2, -NHC(=O)NHR0 o -NHC(=O)N(R0)2; R6 y R7 en cada caso con independencia entre sí significan -H, -F, -Cl, -Br, -I, -CN, -NO2, -CHO, -R0, -C(=O)H, -C(=O)R0, -C(=O)OH, -C(=O)OR0, -C(=O)NH2, -C(=O)NHR0, -C(=O)N(R0)2, -OH, -OR0, -OC(=O)H, -OC(=O)R0, -OC(=O)OR0, -OC(=O)NHR0, -OC(=O)N(R0)2, -SH, -SR0, -SO3H, -S(=O)1-2-R0, -S(=O)1-2NH2, -NH2, -NHR0, -N(R0)2, -N+(R0)3, -N+(R0)2O-, -NHC(=O)R0, -NHC(=O)OR0, -NHC(=O)NH2, -NHC(=O)-NHR0, o -NHC(=O)N(R0)2, o R5 y R6 juntos forman un anillo de cinco o seis eslabones, cuyos átomos restantes en cada caso con independencia entre sí son C, N, S u O, dicho anillo es aromático o no aromático, está sin sustituir o sustituido una o varias veces por sustituyentes elegidos con independencia entre sí entre el grupo formado por -F, -Cl, -Br, -I, -CN, -NO2, -CHO, =O, -R0, C(=O)R0, -C(=O)H, -C(=O)OH, -C(=O)OR0, -C(=O)NH2, -C(=O)NHR0, -C(=O)N(R0)2, -OH, -OR0, -OC(=O)H, -OC(=O)R0, -OC(=O)OR0, -OC(=O)NHR0, -OC(=O)N(R0)2, -SH, -SR0, -SO3H, -S(=O)1-2-R0, -S(=O)1-2NH2, -NH2, -NHR0, -N(R0)2, -N+(R0)3, -N+(R0)2O-, -NHC(=O)R0, -NHC(=O)OR0, -NHC(=O)NH2, -NHC(=O)-NHR0, y -NHC(=O)N(R0)2; en la que ôalifáticoö es en cada caso un resto hidrocarburo alifático ramificado o sin ramificar, saturado o mono- o poliinsaturado, sin sustituir o sustituido una o más veces; ôcicloalifáticoö es en cada caso un resto hidrocarburo alicíclico, mono- o policíclico, saturado o mono- o poliinsaturado, sin sustituir o sustituido una o varias veces; cuyo numero de átomos de C en el anillo se situa con preferencia en el intervalo indicado; en lo referente a ôalifáticoö y ôcicloalifáticoö se entiende por ôsustituido una o varias vecesö la sustitucion unica o multiple de uno o varios átomos de hidrogeno, p.ej. la sustitucion una vez, dos veces, tres veces o total por sustituyentes elegidos con independencia entre sí entre el grupo formado por -F, -Cl, -Br, -I, -CN, -NO2, -CHO, =O, -R0, -C(=O)R0, -C(=O)H, -C(=O)OH, -C(=O)OR0, -C(=O)NH2, -C(=O)NHR0, -C(=O)N(R0)2, -OH, -OR0, -OC(=O)H, -OC(=O)R0, -OC(=O)OR0, -OC(=O)NHR0, -OC(=O)N(R0)2, -SH, -SR0, -SO3H, -S(O)1-2-R0, -S(=O)1-2NH2, -NH2, -NHR0, -N(R0)2, -N+(R0)3, -N+(R0)2O-, -NHC(=O)R0, -NHC(=O)OR0, -NHC(=O)NH2, -NHC(=O)-NHR0, -NHC(=O)N(R0)2, -NHS(=O)1-2R0, -Si(R0)3 y -PO(OR0)2; ôariloö significa en cada caso con independencia un sistema carbocíclico que tiene por lo menos un anillo aromático, pero sin heteroátomos en este anillo, dichos restos arilo pueden estar eventualmente condensados con otros sistemas de anillo saturados, (parcialmente) insaturados o aromáticos y cada resto arilo puede estar sin sustituir o sustituido una o varias veces; los sustituyentes del arilo pueden ser iguales o distintos y pueden ocupar cualquier posicion posible de arilo; ôheteroariloö significa un resto aromático cíclico de 5, 6 o 7 eslabones, que contiene 1, 2, 3, 4 o 5 heteroátomos, los heteroátomos pueden ser iguales o distintos y elegirse entre nitrogeno, oxígeno y azufre, y el heterociclo puede estar sin sustituir o sustituido una o varias veces; en el caso de sustitucion del heterociclo, los sustituyentes serán iguales o distintos y podrán ocupar cualquier posicion posible del heteroarilo; y el heterociclo puede formar también parte de un sistema bi- o policíclico; en lo referente a ôariloö y ôheteroariloö se entiende por ôsustituido una o varias vecesö una sustitucion unica o multiple de uno o más átomos de hidrogeno del sistema de anillo por sustituyentes elegidos entre el grupo formado por -F, -Cl, -Br, -I, -CN, -NO2, -CHO, =O, -R0, -C(=O)R0, -C(=O)H, -C(=O)OH, -C(=O)OR0, -C(=O)NH2, -C(=O)NHR0, -C(=O)-N(R0)2, -OH, -O(CH2)1-2O-, -OR0, -OC(=O)H, -OC(=O)R0, -OC(=O)OR0, -OC(=O)NHR0, -OC(=O)N(R0)2, -SH, -SR0, -SO3H, -S(=O)1-2-R0, -S(=O)1-2NH2, -NH2, -NHR0, -N(R0)2, -N+(R0)3, -N+(R0)2O-, -NH-C(=O)R0, -NHC(=O)OR0, -NHC(=O)NH2, -NHC(=O)NHR0, -NHC(=O)-N(R0)2, -Si(R0)3, -PO(OR0)2, en los que los átomos de N eventualmente existentes en el anillo pueden estar en cada caso oxidados; en forma de un estereoisomero individual o de una mezcla, de los compuestos libres y/o sus sales fisiologicamente compatibles.
ARP090101057A 2008-03-27 2009-03-25 Ciclohexildiaminas sustituidas AR071067A1 (es)

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US (1) US8357705B2 (es)
EP (1) EP2260022B1 (es)
JP (1) JP5529843B2 (es)
CN (1) CN102046596B (es)
AR (1) AR071067A1 (es)
AU (1) AU2009228648B2 (es)
CA (1) CA2719743A1 (es)
CL (1) CL2009000735A1 (es)
ES (1) ES2621407T3 (es)
IL (1) IL208281A0 (es)
MX (1) MX2010010339A (es)
PE (1) PE20091823A1 (es)
RU (1) RU2526251C2 (es)
TW (1) TWI466866B (es)
WO (1) WO2009118174A1 (es)

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US7977370B2 (en) 2008-03-27 2011-07-12 Gruenenthal Gmbh (Hetero)aryl cyclohexane derivatives
US8288430B2 (en) 2008-03-27 2012-10-16 Grunenthal Gmbh Spiro(5.5)undecane derivatives
US8288406B2 (en) 2008-03-27 2012-10-16 Gruenenthal Gmbh Hydroxymethylcyclohexylamines
US8293758B2 (en) 2008-03-27 2012-10-23 Grunenthal Gmbh Substituted spirocyclic cyclohexane derivatives
US8357705B2 (en) 2008-03-27 2013-01-22 Gruenenthal Gmbh Substituted cyclohexyldiamines
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WO2009118174A1 (de) 2009-10-01
TW200944501A (en) 2009-11-01
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US8357705B2 (en) 2013-01-22
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PE20091823A1 (es) 2009-12-10
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US20090247591A1 (en) 2009-10-01
CA2719743A1 (en) 2009-10-01
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CN102046596B (zh) 2013-12-25
CL2009000735A1 (es) 2009-05-15
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AU2009228648A1 (en) 2009-10-01

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