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AR079840A2 - Receptor nicotinico de acetilcolina, subtipo selectivo de amidas de diazabicicloalcanos - Google Patents

Receptor nicotinico de acetilcolina, subtipo selectivo de amidas de diazabicicloalcanos

Info

Publication number
AR079840A2
AR079840A2 ARP110100026A ARP110100026A AR079840A2 AR 079840 A2 AR079840 A2 AR 079840A2 AR P110100026 A ARP110100026 A AR P110100026A AR P110100026 A ARP110100026 A AR P110100026A AR 079840 A2 AR079840 A2 AR 079840A2
Authority
AR
Argentina
Prior art keywords
alkyl
substituted
aryl
heteroaryl
compounds
Prior art date
Application number
ARP110100026A
Other languages
English (en)
Inventor
Regina Whitaker
Srinivisa Rao Akireddy
V Srinivasa Murthy
Anatoly A Mazurov
Lan Miao
Yun Xiao
Philip S Hammond
Craig H Miller
Scott R Breining
Matt S Melvin
Original Assignee
Targacept Inc
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 Targacept Inc filed Critical Targacept Inc
Publication of AR079840A2 publication Critical patent/AR079840A2/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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/08Antiepileptics; Anticonvulsants
    • 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
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D471/08Bridged systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Se revelan compuestos, composiciones farmacéuticas que incluyen los compuestos y métodos de preparacion y el uso de los mismos. Los compuestos son compuestos amida que pueden prepararse desde ciertos ácidos carboxílicos heteroarilos y ciertos diazabicicloalcanos. Los compuestos exhiben selectividad para los receptores nicotínicos neuronales del subtipo alfa4beta2 en el sistema nervioso central (SNC) y se unen con alta afinidad. Los compuestos y composiciones pueden ser utilizados para tratar y/o prevenir una gran variedad de males y enfermedades, particularmente del Sistema Nervioso Central. Los compuestos pueden: (i) alterar el numero de receptores colinérgicos nicotínicos del cerebro del paciente, (ii) exhibir efectos neuroprotectores, y (iii) cuando se utilizan en cantidades efectivas, no dan como resultado efectos colaterales adversos (por ejemplo, efectos colaterales como presion sanguínea y frecuencia cardiaca, efectos negativos importantes en el tracto gastrointestinal y efectos importantes en el musculo oseo). Reivindicacion 1: Un compuesto representado por formula (1) caracterizado porque n tiene el valor de 0 o 1, y Cy es un grupo heteroarilo elegido del grupo de 2-furanilo, 3-furanilo, 2-oxazolilo, 4-oxazolilo, 5-oxazolilo, 3-isoxazolilo, 4-isoxazolilo, 5-isoxazolilo, 1,3,4-oxadiazol-2-ilo, 1,2,4-oxadiazol-3-ilo, 1,2,4-oxadiazol-5-ilo, 2-tiazolilo, 4-tiazolilo, 5-tiazolilo, 3-isotiazolilo, 4-isotiazolilo, 5-isotiazolilo, 1,3,4-tiadiazol-2-ilo, 1,2,4-tiadiazol-3-ilo, 1,2,4-tiadiazol-5-ilo y 4-piridinilo, cuyos grupos heteroarilo son sustituidos opcionalmente con hasta tres sustituyentes no hidrogeno independientemente seleccionados de alquilo C1-6, alquilo C1-6 sustituido, alquenilo C2-6, alquenilo C2-6 sustituido, alquinilo C2-6, alquinilo C2-6 sustituido, heterociclilo de 3 a 8 miembros, heterociclilo de 3 a 8 miembros sustituido, cicloalquilo C3-8, cicloalquilo C3-8 sustituido, arilo C5-10, heteroarilo de 5 a 10 miembros, arilo C5-10 sustituido, heteroarilo de 5 a 10 miembros sustituido, alquilo C1-6-arilo C5-10, alquil C1-6-heteroarilo de 5 a 10 miembros, alquilo C1-6-arilo C5-10 sustituido, alquilo C1-6-heteroarilo de 5 a 10 miembros sustituido, arilo C5-10-alquilo C1-6, heteroarilo de 5 a 10 miembros-alquilo C1-6, arilo C5-10-alquilo C1-6 sustituido, heteroarilo de 5 a 10 miembros-alquilo C1-6 sustituido, halo, -OR', -NR'Rö, -CF3, -CN, -NO2, -C2R', -SR', -N3, -C(=O)NR'Rö, -NR'C(=O)Rö, -C(=O)R', -C(=O)OR', -OC(=O)R', -OC(=O)NR'Rö, -NR'C(=O)ORö, -SO2R', -SO2NR'Rö, y -NR'SO2Rö, donde R' y Rö se seleccionan independientemente del hidrogeno, alquilo C1-6, cicloalquilo C3-8, heterociclilo de 3 a 8 miembros, arilo C5-10, heteroarilo de 5 a 10 miembros y arilo C5-10-alquilo C1-6, o R' y Rö junto con los átomos a los cuales se unen pueden formar un anillo heterocíclico de 3 a 8 miembros, en donde el término ôsustituidoö aplicado a alquilo, alquenilo, alquinilo, heterociclilo, cicloalquilo, arilo, heteroarilo, alquilarilo, alquilheteroarilo, arilalquilo y heteroarilalquilo, se refiere a una sustitucion por uno o mas grupos alquilo, arilo, heteroarilo, halo, -OR' y -NR'Rö, o sales farmacéuticamente aceptables de los mismos.
ARP110100026A 2006-11-02 2011-01-05 Receptor nicotinico de acetilcolina, subtipo selectivo de amidas de diazabicicloalcanos AR079840A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US85607906P 2006-11-02 2006-11-02

Publications (1)

Publication Number Publication Date
AR079840A2 true AR079840A2 (es) 2012-02-22

Family

ID=39233054

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP070104876A AR063451A1 (es) 2006-11-02 2007-11-01 Diazabiciclo alcanos como receptores nicotinicos de acetilcolina. composiciones farmaceuticas.
ARP110100026A AR079840A2 (es) 2006-11-02 2011-01-05 Receptor nicotinico de acetilcolina, subtipo selectivo de amidas de diazabicicloalcanos

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP070104876A AR063451A1 (es) 2006-11-02 2007-11-01 Diazabiciclo alcanos como receptores nicotinicos de acetilcolina. composiciones farmaceuticas.

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US (6) US8114889B2 (es)
EP (2) EP2284171B1 (es)
JP (2) JP5539723B2 (es)
KR (2) KR20100124356A (es)
CN (4) CN102942569B (es)
AR (2) AR063451A1 (es)
AT (2) ATE509022T1 (es)
AU (2) AU2007317433B2 (es)
BR (2) BRPI0722387A2 (es)
CA (1) CA2663925C (es)
CL (1) CL2007003155A1 (es)
CO (1) CO6180435A2 (es)
CY (1) CY1112374T1 (es)
DK (1) DK2094703T3 (es)
ES (2) ES2395212T3 (es)
HR (1) HRP20110570T1 (es)
IL (2) IL197618A (es)
MX (1) MX2009004801A (es)
MY (2) MY156730A (es)
NO (1) NO20091251L (es)
NZ (2) NZ587847A (es)
PE (2) PE20110671A1 (es)
PL (1) PL2094703T3 (es)
PT (1) PT2094703E (es)
RS (1) RS51834B (es)
RU (2) RU2517693C2 (es)
SA (1) SA07280584B1 (es)
SI (1) SI2094703T1 (es)
TW (3) TWI404532B (es)
UA (2) UA98944C2 (es)
UY (1) UY30686A1 (es)
WO (1) WO2008057938A1 (es)

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CL2007003155A1 (es) 2008-05-16
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