AR079496A1 - Derivados de aril triazol heteroaromaticos como inhibidores de enzima pde10a - Google Patents

Derivados de aril triazol heteroaromaticos como inhibidores de enzima pde10a

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Publication number
AR079496A1
AR079496A1 ARP100104669A ARP100104669A AR079496A1 AR 079496 A1 AR079496 A1 AR 079496A1 AR P100104669 A ARP100104669 A AR P100104669A AR P100104669 A ARP100104669 A AR P100104669A AR 079496 A1 AR079496 A1 AR 079496A1
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AR
Argentina
Prior art keywords
compound
formula
provides
subject
effective amount
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ARP100104669A
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English (en)
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Lundbeck & Co As H
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Application filed by Lundbeck & Co As H filed Critical Lundbeck & Co As H
Publication of AR079496A1 publication Critical patent/AR079496A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41961,2,4-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Neurology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente se dirige a compuestos, que son inhibidores de la enzima PDE10A. Proporciona una composicion farmacéutica que comprende una cantidad terapéuticamente efectiva de un compuesto y un portador farmacéuticamente aceptable. La presente también proporciona procesos para la preparacion de los compuestos de la formula 1. La presente además proporciona un método de tratar un sujeto que padece de un trastorno neurodegenerativo que comprende la administracion al sujeto de una cantidad terapéuticamente efectiva de un compuesto de la formula 1. La presente también proporciona un método para tratar a un sujeto que padece de adiccion a las drogas que comprende la administracion a un sujeto de una cantidad terapéuticamente efectiva de un compuesto de la formula 1. La presente además proporciona un método para tratar a un sujeto que padece de un trastorno psiquiátrico que comprende la administracion al sujeto de una cantidad terapéuticamente efectiva de un compuesto de la formula 1. Reivindicacion 1: Un compuesto que tiene la estructura 1 en donde HET-1 es un grupo heteroaromático de la formula 2 que contiene de 2 a 4 átomos de nitrogeno: en donde Y puede ser N o CH, Z puede ser N o C, y en donde HET-1 puede sustituirse opcionalmente con hasta tres sustituyentes R2-R4 individualmente seleccionados de hidrogeno, alquilo C1-6 halogeno; ciano, haloalquilo C1-6; arilo, alcoxi e hidroxialquilo C1-6, y en donde * denota el punto de union, Q es un fenilo, opcionalmente sustituido con uno a cinco sustituyentes, o un grupo heteroaromático de 5 o 6 miembros monocíclico que contiene 1 o 2 heteroátomos. -L- es un enlazante seleccionado de -S-CH2-, -CH2-S-, -CH2-CH2- -CH=CH-, , -C=C R1 se selecciona de H, alquilo C1-6 alquil C1-6 cicloalquilo C3-8; hidroxialquilo C1-6, CH2CN, CH2C(O)NH2, arilalquilo C1-6, y alquil C1-6 heterocicloalquilo, y tautomeros y sales farmacéuticamente aceptables de los mismos, y formas polimorficas de los mismos, con la condicion de que cuando el enlazante (L) es -CH2-S- entonces HET-1 no es ni imidazol[1,2-a]piridina ni imidazol[1,2-a]pirimidina.
ARP100104669A 2009-12-17 2010-12-16 Derivados de aril triazol heteroaromaticos como inhibidores de enzima pde10a AR079496A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DKPA200901340 2009-12-17

Publications (1)

Publication Number Publication Date
AR079496A1 true AR079496A1 (es) 2012-02-01

Family

ID=44246811

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100104669A AR079496A1 (es) 2009-12-17 2010-12-16 Derivados de aril triazol heteroaromaticos como inhibidores de enzima pde10a

Country Status (36)

Country Link
US (2) US8501795B2 (es)
EP (1) EP2513106B1 (es)
JP (1) JP6035149B2 (es)
KR (1) KR101779629B1 (es)
CN (1) CN102753550B (es)
AR (1) AR079496A1 (es)
AU (1) AU2010333438B2 (es)
BR (1) BR112012014486A2 (es)
CA (1) CA2783728C (es)
CO (1) CO6602117A2 (es)
CR (1) CR20120318A (es)
CY (1) CY1116361T1 (es)
DK (1) DK2513106T3 (es)
DO (1) DOP2012000169A (es)
EA (1) EA021606B1 (es)
ES (1) ES2442179T3 (es)
GE (1) GEP20146201B (es)
GT (1) GT201200193A (es)
HK (1) HK1177745A1 (es)
HR (1) HRP20131210T1 (es)
IL (1) IL220328A (es)
MA (1) MA33923B1 (es)
MX (1) MX2012006715A (es)
MY (1) MY156520A (es)
NZ (1) NZ600365A (es)
PL (1) PL2513106T3 (es)
PT (1) PT2513106E (es)
RS (1) RS53101B (es)
SG (1) SG181672A1 (es)
SI (1) SI2513106T1 (es)
SM (1) SMT201400009B (es)
TN (1) TN2012000278A1 (es)
TW (1) TWI487705B (es)
UA (1) UA107950C2 (es)
WO (1) WO2011072697A1 (es)
ZA (1) ZA201204420B (es)

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TWI481607B (zh) * 2009-12-17 2015-04-21 Lundbeck & Co As H 作為pde10a酵素抑制劑的2-芳基咪唑衍生物
TWI487705B (zh) 2009-12-17 2015-06-11 Lundbeck & Co As H 作為pde10a酵素抑制劑之雜芳香族芳基***衍生物
TWI485151B (zh) 2009-12-17 2015-05-21 Lundbeck & Co As H 作為pde10a酵素抑制劑之雜芳香族苯基咪唑衍生物
EP3210984B1 (en) 2011-01-11 2019-06-19 Sunovion Pharmaceuticals Inc. Heteroaryl compounds and methods of use thereof
CN103476757A (zh) 2011-02-18 2013-12-25 阿勒根公司 作为磷酸二酯酶10(pde10a)的抑制剂的取代的6,7-二烷氧基-3-异喹啉醇衍生物
WO2013041472A1 (en) * 2011-09-19 2013-03-28 F. Hoffmann-La Roche Ag Triazolopyridine compounds as pde10a inhibitors
WO2013127817A1 (en) 2012-02-27 2013-09-06 H. Lundbeck A/S Imidazole derivatives as pde10a enzyme inhibitors
MX2014014468A (es) 2012-05-30 2015-02-12 Hoffmann La Roche Compuestos triazolo como inhibidores de fosfodiesterasa 10 (pde10).
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WO2014071044A1 (en) 2012-11-01 2014-05-08 Allergan, Inc. Substituted 6,7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde10a)
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KR20160089474A (ko) * 2013-11-28 2016-07-27 에프. 호프만-라 로슈 아게 이미다졸 유도체
US9200016B2 (en) 2013-12-05 2015-12-01 Allergan, Inc. Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A)
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TWI481607B (zh) 2009-12-17 2015-04-21 Lundbeck & Co As H 作為pde10a酵素抑制劑的2-芳基咪唑衍生物
TWI487705B (zh) 2009-12-17 2015-06-11 Lundbeck & Co As H 作為pde10a酵素抑制劑之雜芳香族芳基***衍生物
CN103038229B (zh) * 2010-05-26 2016-05-11 桑诺维恩药品公司 杂芳基化合物及其使用方法

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Publication number Publication date
TW201130834A (en) 2011-09-16
EA201290517A1 (ru) 2012-12-28
KR101779629B1 (ko) 2017-09-18
US20120309764A1 (en) 2012-12-06
GEP20146201B (en) 2014-11-25
MY156520A (en) 2016-02-26
HK1177745A1 (en) 2013-08-30
UA107950C2 (en) 2015-03-10
DOP2012000169A (es) 2012-12-15
DK2513106T3 (da) 2014-01-13
PL2513106T3 (pl) 2014-09-30
JP2013514286A (ja) 2013-04-25
CY1116361T1 (el) 2017-02-08
SMT201400009B (it) 2014-03-07
ES2442179T3 (es) 2014-02-10
TN2012000278A1 (en) 2013-12-12
EA021606B1 (ru) 2015-07-30
MX2012006715A (es) 2012-07-03
CA2783728C (en) 2018-06-12
KR20120113215A (ko) 2012-10-12
RS53101B (en) 2014-06-30
CN102753550B (zh) 2015-03-25
MA33923B1 (fr) 2013-01-02
US20130281459A1 (en) 2013-10-24
EP2513106B1 (en) 2013-11-06
CO6602117A2 (es) 2013-01-18
HRP20131210T1 (hr) 2014-01-17
BR112012014486A2 (pt) 2017-04-04
SG181672A1 (en) 2012-07-30
ZA201204420B (en) 2013-09-25
IL220328A0 (en) 2012-08-30
NZ600365A (en) 2013-10-25
GT201200193A (es) 2013-09-26
JP6035149B2 (ja) 2016-11-30
AU2010333438A1 (en) 2012-06-21
CA2783728A1 (en) 2011-06-23
WO2011072697A1 (en) 2011-06-23
AU2010333438B2 (en) 2016-03-10
TWI487705B (zh) 2015-06-11
CN102753550A (zh) 2012-10-24
IL220328A (en) 2014-12-31
PT2513106E (pt) 2014-01-20
CR20120318A (es) 2012-08-16
US8785653B2 (en) 2014-07-22
SI2513106T1 (sl) 2014-01-31
US8501795B2 (en) 2013-08-06
EP2513106A1 (en) 2012-10-24

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