AR075730A1 - 3-amino-2-mercaptoquinolina sustituida como moduladores de kcnq2/3 - Google Patents

3-amino-2-mercaptoquinolina sustituida como moduladores de kcnq2/3

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Publication number
AR075730A1
AR075730A1 ARP100100719A ARP100100719A AR075730A1 AR 075730 A1 AR075730 A1 AR 075730A1 AR P100100719 A ARP100100719 A AR P100100719A AR P100100719 A ARP100100719 A AR P100100719A AR 075730 A1 AR075730 A1 AR 075730A1
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substituted
alkyl
unsubstituted
saturated
unsaturated
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ARP100100719A
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Gruenenthal Gmbh
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D215/38—Nitrogen atoms
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P25/14—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
    • A61P25/22—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
    • A61P25/28—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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D215/36—Sulfur atoms
    • 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
    • C07D409/12—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 chain containing hetero atoms as chain links

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  • Physical Education & Sports Medicine (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)

Abstract

Se refiere a las 3-amino-2-mercaptoquinolinas sustituidas, al procedimiento para producirlas, a los medicamentos que contienen estos compuestos, así como el uso de estos compuestos para la elaboracion de medicamentos para el dolor, epilepsia, ansiedad, dependencias, manías, enfermedades cognitivas. Reivindicacion 1: 1,3-amino-2-mercaptoquinolina sustituida de la formula general (1) en donde, m representa 0 o 1 y n representa un numero entero de 0 a 4, R1, R2, R3, R4, R5, R6a, R6b son, en forma independiente entre sí, H; F; CI; Br; I; NO2; C3; CN; OH; OCF3; SH; SCF3; NH2; alquilo C1-10, O-alquilo C1-10, O-C(=O)-alquilo C1-10, S-alquilo C1-10, NH(alquilo C1-10), N(alquilo C1-10)2, NH-C(=O)-alquilo C1-10, N(C(=O)-alquilo C1-10)2 o C(=O)-alquilo C1-10, saturado o no saturado, ramificado o no ramificado, no sustituido o sustituido en forma simple o multiple; cicloalquilo C3-8 o heterociclilo, saturado o no saturado, no sustituido o sustituido en forma simple o multiple Y es O o NR9, en donde R9 es H o alquilo C1-4 saturado o no saturado, ramificado o no ramificado sustituido o en forma simple o multiple, R7 es alquilo C1-10, o heteroalquilo C2-10, saturado o no saturado, ramificado o no ramificado, no sustituido o sustituido en forma simple o multiple; cicloalquilo C3-10 o heterociclilo, saturado o no saturado, no sustituido o sustituido en forma simple o multiple; arilo o heteroarilo, no sustituido o sustituido en forma simple o multiple; a condicion de que cuando R7 signifique heterociclilo, el enlace del heteroarilo o heterociclilo a una estructura general superior se puede realizar sobre un átomo de carbono del heterociclilo; y a condicion de que cuando R7 sea arilo o heteroarilo, la suma de n más m sea mayor o igual a 1; R8 se selecciona del grupo compuesto de alquilo C1-10 o heteroalquilo C2-10, saturado o no saturado, ramificado o no ramificado, no sustituido o sustituido en forma simple o multiple; cicloalquilo C3-10 o heterociclilo, saturado o no saturado, no sustituido o sustituido en forma simple o multiple; arilo o heteroarilo, no sustituido o sustituido en forma simple o multiple; cicloalquilo C3-10 o heterociclilo con enlace por puente sobre alquilo C1-8 o heteroalquilo C2-8, saturado o no saturado, no sustituido o sustituido en forma simple o multiple, arilo o heteroarilo con enlace por puente sobre alquilo C1-8 o heteroalquilo C2-8, no sustituido o sustituido en forma simple o multiple, en donde la cadena de alquilo o heteroalquilo puede estar ramificada o no ramificada, saturada o no saturada, no sustituida; donde el ôalquilo sustituidoö, el ôheteroalquilo sustituidoö, el ôheterociclilo sustituidoö y el ôcicloalquilo sustituidoö representan la sustitucion de uno o más átomos de hidrogeno, independientes entre sí, por medio de F; CI; Br; I; CN; CF3 =O; =NH; =C(NH2)2; NO2; R0; C(=O)H; C(=O)R0; CO2H; C(=O)OR0; CONH2; C(=O)NHR0; C(=O)N(R0)2; OH; OR0; -O-(alquilo C1-8)-O-; O-C(=O)-R0; O-C(=O)-O-R0; O-(C=O)NH-R0; O-C(=O)-N(R0)2; O-S(=O)2-R0; O-S(=O)2OH; O-S(=O)2OR0; O-S(=O)2NH2; O-S(=O)2NHR0; O-S(=O)2N(R0)2; NH2; NH-R0; N(R0)2; NH-C(=O)-R0; NH-C(=O)-O-R0; NH-C(=O)-NH2; NH-C(=O)-NH-R0; NH-C(=O)-N(R0)2; NR0-C(=O)-R0; NR0-C(=O)-O-R0; NR0-C(=O)-NH2; NR0-C(=O)-NH-R0; NR0-C(=O)-N(R0)2; NH-S(=O)2OH; NH-S(=O)2R0; NH-S(=O)2OR0; NH-S(=O)2NH2; NH-S(=O)2NHR0; NH-S(=O)2N(R0)2; NR0-S(=O)2OH; NR0-S(=O)2R0; NR0-S(=O)2OR0; NR0-S(=O)2NH2; NR0-S(=O)2NHR0; NR0-S(=O)2N(R0)2; SH; SR0; S(=O)R0; S(=O)2R0; S(=O)2H; S(=O)2OH; S(=O)2OR0; S(=O)2NH2; S(=O)2NHR0; S(=O)2N(R0)2; donde el ôarilo sustituidoö y el ôheteroarilo sustituidoö representan la sustitucion de uno o más átomos de hidrogeno, independientes entre sí, por medio de F; CI; Br; I; NO2; CF3; CN; R0; C(=O)H; C(=O)R0; CO2H; C(=O)OR0; CONH2; C(=O)NHR0; C(=O)N(R0)2; OH; OR0; -O-(alquilo C1-8)-O-; O-C(=O)-R0; O-C(=O)-O-R0; O-(C=O)NH-R0; O-C(=O)-N(R0)2; O-S(=O)2-R0; O-S(=O)2OH; O-S(=O)2OR0; O-S(=O)2NH2; O-S(=O)2NHR0; O-S(=O)2N(R0)2; NH2; NH-R0; N(R0)2; NH-C(=O)-R0; NH-C(=O)-O-R0; NH-C(=O)-NH2; NH-C(=O)-NH-R0; NH-C(=O)-N(R0)2; NR0-C(=O)-R0; NR0-C(=O)-O-R0; NR0-C(=O)-NH2; NR0-C(=O)-NH-R0; NR0-C(=O)-N(R0)2; NH-S(=O)2OH; NH-S(=O)2R0; NH-S(=O)2OR0; NH-S(=O)2NH2; NH-S(=O)2NHR0; NH-S(=O)2N(R0)2; NR0-S(=O)2OH; NR0-S(=O)2R0; NR0-S(=O)2OR0; NR0-S(=O)2NH2; NR0-S(=O)2NHR0; NR0-S(=O)2N(R0)2; SH; SR0; S(=O)R0; S(=O)2R0; S(=O)2OH; S(=O)2OR0; S(=O)2NH2; S(=O)2NHR0; S(=O)2N(R0)2; R0 representa alquilo C1-10 o heteroalquilo C2-10, saturado o no saturado, ramificado o no ramificado, no sustituido o sustituido en forma simple o multiple; cicloalquilo C3-10 o heterociclilo, saturado o no saturado, no sustituido o sustituido en forma simple o multiple; arilo o heteroarilo, no sustituido o sustituido en forma simple o multiple; cicloalquilo C3-10 o heterociclilo con enlace por puente sobre alquilo C1-8 o heteroalquilo C2-8, saturado o no saturado, no sustituido o sustituido en forma simple o multiple, en donde la cadena de alquilo o heteroalquilo puede estar ramificada o no ramificada, saturada o no saturada, no sustituida o sustituida en forma simple o multiple; o bien, el arilo o heteroarilo con enlace por puente sobre alquilo C1-8 o heteroalquilo C2-8, no sustituido o sustituido en forma simple o multiple, en donde la cadena de alquilo o heteroalquilo puede estar ramificada o no ramificada, saturada o no saturada, no sustituida o sustituida en forma simple o multiple; en forma de compuestos o sales libres fisiologicamente compatibles con ácidos o bases.
ARP100100719A 2009-03-10 2010-03-10 3-amino-2-mercaptoquinolina sustituida como moduladores de kcnq2/3 AR075730A1 (es)

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EP (1) EP2406228B1 (es)
JP (1) JP5727945B2 (es)
KR (1) KR20110130461A (es)
CN (1) CN102341374A (es)
AR (1) AR075730A1 (es)
AU (1) AU2010223556B2 (es)
BR (1) BRPI1009519A2 (es)
CA (1) CA2754943A1 (es)
CL (1) CL2011002160A1 (es)
CO (1) CO6410291A2 (es)
EC (1) ECSP11011346A (es)
ES (1) ES2436365T3 (es)
IL (1) IL214944A0 (es)
MX (1) MX2011009338A (es)
NZ (1) NZ595569A (es)
PE (1) PE20120535A1 (es)
PL (1) PL2406228T3 (es)
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CL2011002160A1 (es) 2012-08-17
JP5727945B2 (ja) 2015-06-03
ZA201107370B (en) 2012-07-25
JP2012521966A (ja) 2012-09-20
MX2011009338A (es) 2011-09-27
CO6410291A2 (es) 2012-03-30
IL214944A0 (en) 2011-11-30
PE20120535A1 (es) 2012-05-09
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US20100234421A1 (en) 2010-09-16
ES2436365T3 (es) 2013-12-30
AU2010223556A1 (en) 2011-11-03
BRPI1009519A2 (pt) 2016-03-15
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US8207342B2 (en) 2012-06-26
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EP2406228A1 (de) 2012-01-18
ECSP11011346A (es) 2011-10-31
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AU2010223556B2 (en) 2015-01-29
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