AR075182A1 - 2-AZA-BICYCLE COMPOUNDS (2.2.2) OCTANO AND ITS USES - Google Patents

2-AZA-BICYCLE COMPOUNDS (2.2.2) OCTANO AND ITS USES

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Publication number
AR075182A1
AR075182A1 ARP100100196A ARP100100196A AR075182A1 AR 075182 A1 AR075182 A1 AR 075182A1 AR P100100196 A ARP100100196 A AR P100100196A AR P100100196 A ARP100100196 A AR P100100196A AR 075182 A1 AR075182 A1 AR 075182A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
optionally substituted
cycloalkyl
independently selected
Prior art date
Application number
ARP100100196A
Other languages
Spanish (es)
Original Assignee
Astrazeneca Ab
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 Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR075182A1 publication Critical patent/AR075182A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/08—Bridged systems
    • 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
    • A61P25/04—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
    • A61P25/18—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
    • A61P25/24—Antidepressants
    • 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]

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Además se refiere a composiciones farmacéuticas que comprenden este compuesto, usos de este tipo de compuesto (que incluye, por ejemplo, métodos de tratamiento y preparaciones de medicamentos), y procesos para producir este compuesto. Son utiles para el tratamiento de psicosis, trastorno cognitivo, ansiedad, dolor, esquizofrenia. Reivindicacion 1: Un compuesto o su sal aceptable para uso farmacéutico, donde el compuesto corresponde a la formula 1, A1 se selecciona de fenilo opcionalmente sustituido con 1, 2 o 3 grupos R5; y un heteroarilo de 5 o 6 miembros opcionalmente sustituido con 1, 2 o 3 grupos R7; A2 se selecciona de fenilo sustituido con 1, 2 o 3 grupos R2; y un heteroarilo opcionalmente sustituido con 1, 2 o 3 grupos R6; R1 se selecciona de hidrogeno, alquilo C1-6, cicloalquilo C3-6, heterocicloalquilo de 3 a 6 miembros, cicloalquil C3-8-alquilo C1-4, aril-alquilo C1-4, heterocicloalquil-alquilo C1-4, heteroaril-alquilo C1-4, y alquenilo C3-8, donde el cicloalquil C3-8-alquilo C1-4, el aril-alquilo C1-4 y el heteroaril-alquilo C1-4 están opcionalmente sustituidos con uno o más halogenos independientemente seleccionados; cada R2 se selecciona independientemente de halogeno, -CN, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, heterociclilo de 5 o 6 miembros, -SOR, -SO2R, -NH2, -SR, alcoxi C1-6, alquilo C1-6, y alcoxi C1-4-alquilo C1-4, donde el alquilo C1-6, el alcoxi C1-6, y el cicloalquilo C3-6 están opcionalmente sustituidos con uno o más halogenos independientemente seleccionados; y el heterociclilo está opcionalmente sustituido con 1, 2 o 3 grupos R6; cada R5 se selecciona independientemente de alquilo C1-6, cicloalquilo C3-8, alcoxi C1-6, -CN, halogeno, -SO2R, -SOR, -SR y heterociclilo, donde el alquilo C1-6, el cicloalquilo C3-8 y el alcoxi C1-6 están opcionalmente sustituidos con uno o más halogenos independientemente seleccionados; y el heterociclilo está opcionalmente sustituido con alquilo C1-4 o halogeno; cada R6 se selecciona independientemente de alquilo C1-6, alcoxi C1-6, halogeno, -SO2R, -SOR, -SR, fenilo, -CF3, -OCF3, -CN y heterociclilo, donde el heterociclilo está opcionalmente sustituido con alquilo C1-4; cada R7 se selecciona independientemente de alquilo C1-6, alcoxi C1-4, CF3, -OCF3, -CN, -SO2R, -SOR, -SR, fenilo, heterociclilo y alcoxi C1-4, donde el alquilo C1-6, el cicloalquilo C3-8 y el alcoxi C1-4 están opcionalmente sustituidos; cada R se selecciona independientemente de alquilo C1-6, cicloalquil C3-8-alquilo C1-6 y NR3R4; cada R3 y R4 se selecciona independientemente de H y alquilo C1-6; donde los compuestos (y sus sales aceptables para uso farmacéutico) que satisfacen las siguientes definiciones A1 y A2 se excluyen; A1 es fenilo y A2 es fenilo sustituido con 1, 2 o 3 grupos seleccionados de halogeno, -CN, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, -SO2NR3R4, -NH2, -S-alquilo C1-6, alcoxi C1-6, y alquilo C1-6, donde, el alquilo C1-6 y el alcoxi C1-6 están opcionalmente sustituidos con uno o más halogenos; y donde los compuestos (y sus sales aceptables para uso farmacéutico) que satisfacen cualesquiera de las siguientes estructuras 2 a 17 se excluyen.It also refers to pharmaceutical compositions comprising this compound, uses of this type of compound (which includes, for example, methods of treatment and drug preparations), and processes for producing this compound. They are useful for the treatment of psychosis, cognitive disorder, anxiety, pain, schizophrenia. Claim 1: A compound or its salt acceptable for pharmaceutical use, wherein the compound corresponds to formula 1, A1 is selected from phenyl optionally substituted with 1, 2 or 3 R5 groups; and a 5 or 6 membered heteroaryl optionally substituted with 1, 2 or 3 R7 groups; A2 is selected from phenyl substituted with 1, 2 or 3 R2 groups; and a heteroaryl optionally substituted with 1, 2 or 3 R6 groups; R 1 is selected from hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, 3-6 membered heterocycloalkyl, C 3-8 cycloalkyl-C 1-4 alkyl, arylC 1-4 alkyl, heterocycloalkylC 1-4 alkyl, heteroaryl-alkyl C1-4, and C3-8 alkenyl, wherein the C3-8 cycloalkyl-C1-4 alkyl, the aryl-C1-4 alkyl and the heteroaryl-C1-4 alkyl are optionally substituted with one or more independently selected halogens; each R2 is independently selected from halogen, -CN, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, 5- or 6-membered heterocyclyl, -SOR, -SO2R, -NH2, -SR, C1-6 alkoxy, C1-6 alkyl, and C1-4 alkoxy-C1-4 alkyl, wherein C1-6 alkyl, C1-6 alkoxy, and C3-6 cycloalkyl are optionally substituted with one or more independently selected halogens; and the heterocyclyl is optionally substituted with 1, 2 or 3 R6 groups; each R5 is independently selected from C1-6 alkyl, C3-8 cycloalkyl, C1-6 alkoxy, -CN, halogen, -SO2R, -SOR, -SR and heterocyclyl, wherein C1-6 alkyl, C3-8 cycloalkyl and C1-6 alkoxy are optionally substituted with one or more independently selected halogens; and the heterocyclyl is optionally substituted with C1-4 alkyl or halogen; each R6 is independently selected from C1-6 alkyl, C1-6 alkoxy, halogen, -SO2R, -SOR, -SR, phenyl, -CF3, -OCF3, -CN and heterocyclyl, where the heterocyclyl is optionally substituted with C1- alkyl 4; each R7 is independently selected from C1-6 alkyl, C1-4 alkoxy, CF3, -OCF3, -CN, -SO2R, -SOR, -SR, phenyl, heterocyclyl and C1-4 alkoxy, wherein C1-6 alkyl, the C3-8 cycloalkyl and C1-4 alkoxy are optionally substituted; each R is independently selected from C1-6 alkyl, C3-8 cycloalkyl-C1-6 alkyl and NR3R4; each R3 and R4 is independently selected from H and C1-6 alkyl; wherein compounds (and their salts acceptable for pharmaceutical use) that meet the following definitions A1 and A2 are excluded; A1 is phenyl and A2 is phenyl substituted with 1, 2 or 3 groups selected from halogen, -CN, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, -SO2NR3R4, -NH2, -S-C1-6 alkyl , C1-6 alkoxy, and C1-6 alkyl, where, C1-6 alkyl and C1-6 alkoxy are optionally substituted with one or more halogens; and where compounds (and their salts acceptable for pharmaceutical use) that satisfy any of the following structures 2 to 17 are excluded.

ARP100100196A 2009-01-28 2010-01-27 2-AZA-BICYCLE COMPOUNDS (2.2.2) OCTANO AND ITS USES AR075182A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US14801509P 2009-01-28 2009-01-28

Publications (1)

Publication Number Publication Date
AR075182A1 true AR075182A1 (en) 2011-03-16

Family

ID=42395831

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100100196A AR075182A1 (en) 2009-01-28 2010-01-27 2-AZA-BICYCLE COMPOUNDS (2.2.2) OCTANO AND ITS USES

Country Status (3)

Country Link
AR (1) AR075182A1 (en)
TW (1) TW201028416A (en)
WO (1) WO2010087761A1 (en)

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2838739B1 (en) * 2002-04-19 2004-05-28 Sanofi Synthelabo N- [PHENYL (PIPERIDIN-2-YL) METHYL) BENZAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
FR2842805A1 (en) * 2002-07-29 2004-01-30 Sanofi Synthelabo N- [PHENYL (PIPERIDIN-2-YL) METHYL] BENZAMIDE DERIVATIVES, THEIR PREPARATION AND APPLICATION THERAPEUTICS
FR2842804B1 (en) * 2002-07-29 2004-09-03 Sanofi Synthelabo N- [PHENYL (PIPERIDIN-2-YL) METHYL] BENZAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
FR2861073B1 (en) * 2003-10-17 2006-01-06 Sanofi Synthelabo N- [HETEROARYL (PIPERIDIN-2-YL) METHYL] BENZAMIDE DERIVATIVES, THEIR PREPARATION AND THERAPEUTIC USE THEREOF
FR2861076B1 (en) * 2003-10-17 2006-01-06 Sanofi Synthelabo N-HETEROCYCLYMETHYLBENZAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC USE
FR2861071B1 (en) * 2003-10-17 2006-01-06 Sanofi Synthelabo N- [PHENYL (ALKYLPIPERIDIN-2-YL) METHYL] BENZAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC USE
FR2861074B1 (en) * 2003-10-17 2006-04-07 Sanofi Synthelabo N- [PHENYL (PIPERIDIN-2-YL) METHYL] BENZAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC USE
EP1874721A2 (en) * 2004-12-23 2008-01-09 Glaxo Group Limited Glycine transport inhibitors
JP2009179562A (en) * 2006-08-11 2009-08-13 Taisho Pharmaceutical Co Ltd Glycine transporter inhibitor
FR2906251B1 (en) * 2006-09-22 2008-11-07 Sanofi Aventis Sa PYRROLIZINE, INDOLIZINE AND QUINOLIZINE DERIVATIVES, THEIR PREPARATION AND THERAPEUTIC USE THEREOF
WO2009013535A1 (en) * 2007-07-23 2009-01-29 Astrazeneca Ab 2-azabicyclo(2.2.2)octane derivatives as modulators of the glycine transporter i receptor

Also Published As

Publication number Publication date
TW201028416A (en) 2010-08-01
WO2010087761A1 (en) 2010-08-05

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