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AR074325A1 - Compuesto de 1-(arilsulfonil)-4-(piperazin-1-il)-1h-benzimidazole, composicion y medicamento que lo comprende y uso y metodo de sintesis del compuesto - Google Patents

Compuesto de 1-(arilsulfonil)-4-(piperazin-1-il)-1h-benzimidazole, composicion y medicamento que lo comprende y uso y metodo de sintesis del compuesto

Info

Publication number
AR074325A1
AR074325A1 ARP090104372A ARP090104372A AR074325A1 AR 074325 A1 AR074325 A1 AR 074325A1 AR P090104372 A ARP090104372 A AR P090104372A AR P090104372 A ARP090104372 A AR P090104372A AR 074325 A1 AR074325 A1 AR 074325A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkenyl
halo
cycloalkyl
hydroxy
Prior art date
Application number
ARP090104372A
Other languages
English (en)
Inventor
Simon Nicolas Haydar
Patrick Andrae
Albert Jean Robichaud
Heedong Yun
Original Assignee
Wyeth Corp
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41404503&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR074325(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Wyeth Corp filed Critical Wyeth Corp
Publication of AR074325A1 publication Critical patent/AR074325A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/22Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms directly attached to ring nitrogen atoms
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P25/06Antimigraine agents
    • 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
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D487/08Bridged systems

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

Abstract

Compuestos para tratar desórdenes del SNC Reivindicación 1: Un compuesto 1-(arilsulfonil)-4-(piperazin-1-il)-1H-benzimidazol de la fórmula 1 caracterizado porque: R1a y R1b son, cada uno independientemente entre sí, H o alquilo C1-6, alquenilo C2-6 o alquinilo C2-6, cada uno sustituido con 0-4 sustituyentes seleccionados independientemente del grupo que consiste de alquilo C1-4, cicloalquilo C3-6, cicloalquenilo C3-6, alquenilo C2-6, alquinilo C2-6, halo, nitro, ciano, hidroxi, N(Ra)2, -C(O)Rb, -ORc y -S(O)pRd; corno alternativa, R1a y R1b se toman juntos para formar -(CH2)n-; R2 es H, alquilo C1-4, -CHO o -C(O)(alquilo C1-4; R3 es, independientemente cada vez que aparece, halo, nitro, ciano, hidroxi, -N(Ra)2, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, acilo C1-6 o alcoxi C1-6, en donde cada alquilo C1-6, alquenilo C2-6, acilo C1-6 o alcoxi C1-6 está sustituido con 0-4 sustituyentes seleccionados independientemente del grupo que consiste de alquilo C1-4, cicloalquilo C3-6, cicloalquenilo C3-6, alquenilo C2-6, alquinilo C2-6, halo, nitro, ciano, hidroxi, -N(Ra)2, C(O)Rb, -ORc y -S(O)pRd; R4 es H, hidroxi, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, acilo C1-6, cicloalquilo C3-6, o cicloalquenilo C3-6, en donde cada alquilo C1-6, alquenilo C2-6, alquinilo C2-6, acilo C1-6, cicloalquilo C3-6, o cicloalquenilo C3-6, está sustituido con 0-4 sustituyentes seleccionados independientemente del grupo que consiste de alquilo C1-4, cicloalquilo C3-6, cicloalquenilo C3-6, halo, nitro, ciano, hidroxi, -N(Ra)2, C(O)Rb, -ORc y -S(O)pRd; R5, R6, R7, R8, y R9 son, cada uno independientemente entre sí, H, halo, nitro, ciano, hidroxi, S(O)pRd, -N(Ra)2, alquilo C1-6, acilo C1-6, alcoxi C1-6, cicloalquilo C3-6 o cicloalquenilo C3-6, en donde cada alquilo C1-6, acilo C1-6, alcoxi C1-6, cicloalquilo C3-6 o cicloalquenilo C3-6 está sustituido con 0-4 sustituyentes seleccionados independientemente del grupo que consiste de alquilo C1-4, cicloalquilo C3-6, cicloalquenilo C3-6, alquenilo C2-6, alquinilo C2-6, halo, nitro, ciano, hidroxi, -N(Ra)2, C(O)Rb, -ORc y -S(O)pRd; como alternativa, uno de R5 y R6 o R6 y R7 se toman junto con los átomos de carbono a los cuales están unidos para formar un anillo fusionado de fenilo, cicloalquilo C3-6 o cicloalquenilo C3-6sustituido con 0-3 grupos R10; R10 es halo, nitro, ciano, hidroxi, S(O)pRd, -N(Ra)2, alquilo C1-6, acilo C1-6, alcoxi C1-6, cicloalquilo C3-6 o cicloalquenilo C3-6, en donde cada alquilo C1-6, acilo C1-6, alcoxi C1-6, cicloalquilo C3-6 o cicloalquenilo C3-6 está sustituido con 0-4 sustituyentes seleccionados independientemente del grupo que consiste de alquilo C1-4, cicloalquilo C3-6, cicloalquenilo C3-6, alquenilo C2-6, alquinilo C2-6, halo, nitro, ciano, hidroxi, fenilo, -N(Ra)2, C(O)Rb, -ORc y -S(O)pRd; cada Ra es, independientemente, H, -CHO, -C(O)(alquilo C1-4), -CO2(alquilo C1-4) o alquil C1-4 sustituido opcionalmente con halo; cada Rb es, independientemente, H, -OH, alcoxi C1-4, -NH2, -NH(alquilo C1-4), -N(alquilo C1-4)2 o alquilo C1-4 sustituido opcionalmente con halo; cada Rc es independientemente, H, -C(O)(alquilo C1-4) o alquilo C1-4 sustituido opcionalmente con halo; cada Rd es, independientemente, hidroxi o alquilo C1-4 sustituido opcionalmente con halo; cada p es, independientemente, 0, 1 o 2, m es 0,1 o 2; y n es 1 o 2, o un tautómero, estereoisómero o una sal farmacéuticamente aceptable del mismo.
ARP090104372A 2008-11-11 2009-11-11 Compuesto de 1-(arilsulfonil)-4-(piperazin-1-il)-1h-benzimidazole, composicion y medicamento que lo comprende y uso y metodo de sintesis del compuesto AR074325A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US11329608P 2008-11-11 2008-11-11

Publications (1)

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AR074325A1 true AR074325A1 (es) 2011-01-05

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ID=41404503

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ARP090104372A AR074325A1 (es) 2008-11-11 2009-11-11 Compuesto de 1-(arilsulfonil)-4-(piperazin-1-il)-1h-benzimidazole, composicion y medicamento que lo comprende y uso y metodo de sintesis del compuesto

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US (1) US8063053B2 (es)
EP (1) EP2285784B1 (es)
JP (1) JP5087171B2 (es)
KR (1) KR101323417B1 (es)
CN (1) CN102209713B (es)
AP (1) AP2814A (es)
AR (1) AR074325A1 (es)
AU (1) AU2009314221B2 (es)
BR (1) BRPI0920682A2 (es)
CA (1) CA2740262C (es)
CL (1) CL2011001050A1 (es)
CO (1) CO6440548A2 (es)
CR (1) CR20110247A (es)
CU (1) CU24020B1 (es)
CY (1) CY1113025T1 (es)
DK (1) DK2285784T3 (es)
DO (1) DOP2011000130A (es)
EA (1) EA018369B1 (es)
EC (1) ECSP11011045A (es)
ES (1) ES2389694T3 (es)
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PE (1) PE20120026A1 (es)
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UA100192C2 (en) 2012-11-26
CR20110247A (es) 2011-06-24
DK2285784T3 (da) 2012-07-23
TWI481605B (zh) 2015-04-21
CO6440548A2 (es) 2012-05-15
KR101323417B1 (ko) 2013-10-29
NI201100093A (es) 2011-10-31
AP2011005664A0 (en) 2011-04-30
EP2285784A1 (en) 2011-02-23
NZ592563A (en) 2012-10-26
CN102209713B (zh) 2014-07-02
CN102209713A (zh) 2011-10-05
KR20110075013A (ko) 2011-07-05
AP2814A (en) 2013-12-31
ME01129B (me) 2013-03-20
ES2389694T3 (es) 2012-10-30
CA2740262C (en) 2013-05-28
CU20110101A7 (es) 2012-01-31
WO2010056644A8 (en) 2010-11-18
AU2009314221B2 (en) 2012-08-30
ZA201103283B (en) 2012-01-25
WO2010056644A1 (en) 2010-05-20
MX2011004996A (es) 2011-05-25
AU2009314221A1 (en) 2010-05-20
CY1113025T1 (el) 2016-04-13
CU24020B1 (es) 2014-07-30
SA109300673B1 (ar) 2013-05-25
EP2285784B1 (en) 2012-07-04
DOP2011000130A (es) 2017-04-30
PT2285784E (pt) 2012-09-19
RS52381B (sr) 2012-12-31
MA32788B1 (fr) 2011-11-01
HK1158647A1 (en) 2012-07-20
MY156324A (en) 2016-02-15
JP2012508275A (ja) 2012-04-05
US20100120779A1 (en) 2010-05-13
TN2011000203A1 (fr) 2012-12-17
GEP20135805B (en) 2013-04-10
HRP20120561T1 (hr) 2012-07-31
EA018369B1 (ru) 2013-07-30
US8063053B2 (en) 2011-11-22
SI2285784T1 (sl) 2012-08-31
BRPI0920682A2 (pt) 2016-09-27
TW201022247A (en) 2010-06-16
CL2011001050A1 (es) 2011-08-19
SV2011003902A (es) 2011-07-05
PE20120026A1 (es) 2012-02-12
ECSP11011045A (es) 2011-06-30
CA2740262A1 (en) 2010-05-20
IL212213A0 (en) 2011-06-30
EA201100696A1 (ru) 2011-10-31
JP5087171B2 (ja) 2012-11-28
PL2285784T3 (pl) 2012-12-31

Similar Documents

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