AR052307A1 - Procedimientos para la preparacion de inhibidores de p2x7, composicion farmaceutica y un metodo de preparacion - Google Patents

Procedimientos para la preparacion de inhibidores de p2x7, composicion farmaceutica y un metodo de preparacion

Info

Publication number
AR052307A1
AR052307A1 ARP050102636A ARP050102636A AR052307A1 AR 052307 A1 AR052307 A1 AR 052307A1 AR P050102636 A ARP050102636 A AR P050102636A AR P050102636 A ARP050102636 A AR P050102636A AR 052307 A1 AR052307 A1 AR 052307A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
phenyl
naphthyl
optionally substituted
Prior art date
Application number
ARP050102636A
Other languages
English (en)
Original Assignee
Pfizer Prod 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 Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of AR052307A1 publication Critical patent/AR052307A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
    • C07D253/06—1,2,4-Triazines
    • C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
    • C07D253/06—1,2,4-Triazines
    • C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C07D253/07—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members 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
    • C07D253/075—Two hetero atoms, in positions 3 and 5
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
    • C07D253/06—1,2,4-Triazines
    • C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C07D253/07—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Los compuestos son utiles como agentes en el tratamiento de enfermedades, incluyendo enfermedades inflamatorias tales como artritis (de diversos tipos), enfermedad de Crohn, enfisema, osteoporosis y otras. Reivindicacion 1: Un procedimiento de preparacion de un compuesto de formula (1) o una sal farmacéuticamente aceptable del mismo, en la que R1 es alquilo C1-6, opcionalmente sustituido con cicloalquilo C3-8, fenilo, naftilo, heterocicloalquilo de 5 o 6 miembros, o un heteroarilo de 5 o 6 miembros, en el que cada uno de dichos alquilo C1-6, cicloalquilo C3-8, fenilo, naftilo, heterocicloalquilo de 5 o 6 miembros, o heteroarilo de 5 o 6 miembros están opcionalmente sustituidos con uno a tres restos seleccionados independientemente del grupo constituido por hidroxi, halo, CN, alquilo C1-6, HO-alquilo C1-6, alquil C1-6-NH-(C=O)-, NH2(C=O)-, alcoxi C1-6, o cicloalquilo C3-8; R2 es H, halo, -CN o alquilo C1-6, en el que dicho alquilo C1-6, está opcionalmente sustituido con uno a tres restos independientemente seleccionados entre el grupo constituido por halo, hidroxi, amino, -CN, alquilo C1-6, alcoxi C1-6, -CF3, CF3O-, alquil C1-6-NH-, [alquil C1-6]2-N-, alquil C1-6-S-, alquil C1-6-(S=O)-, alquil C1-6-(SO2)-, alquil C1-6-O- (C=O)-, formilo, alquil C1-6-(C=O)- y cicloalquilo C3-6; en la que R4 se selecciona independientemente entre el grupo constituido por H, halo, hidroxi, -CN, HO-alquilo c1-6,alquilo c1-6, opcionalmente sustituido con 1 a 3 fluoro, alcoxi C1-6 opcionalmente sustituido con uno a tres fluoro, HO2C-alquil C1-6-O-(C=O)-, R5R6N(O2S)-, alquil C1-6-(O2S)-NH-, alquil C1-6-O2S[alquil C1-6-N]-, R5R6N(C=O)-, R5R6N(CH2)m-, fenilo, naftilo, cicloalquilo C3-8, heteroarilo de 5 o 6 miembros, heterocicloalquilo de 5 o 6 miembros, fenil-O-, naftil-O-, cicloalquil C3-8-O-,heteroariloxi de 5 o 6 miembros y heterocicloalquil-O- de 5 o 6 miembros; y R7 es -CH2-C(R10R11)-OH, en la que R10 y R11 se seleccionan independientemente del grupo constituido por: H, fenilo y alquilo C1-6 sustituido opcionalmente con uno a tres halo, hidroxi, -CN, alcoxi C1-6, (alquil C1-6)n-N-, alquil C1-6-(C=O)-, cicloalquil C3-8-(C=O)-, heterocicloaquil-(C=O) de 5 o 6 miembros, fenil-(C=O)-, naftil-(C= O), heteroaril-(C=O)- de 5 o 6 miembros, alquil C1-6-(C=O)O-, alquil C1-6-O(C=O)-, cicloalquilo C3-8, fenilo, naftilo, heterocicloalquilo de 5 o 6 miembros y heteroarilo de 5 o 6 miembros; R5 y R6 se seleccionan cada uno independientemente del grupo constituido por H, alquilo C1-6, HO-alquilo C2-6, y cicloalquilo C3-8, o R5 y R6 se pueden tomar conjuntamente de forma opcional con el átomo de N al cual están unidos para formar un heterocicloalquilo de 5 o 6 miembros; n es 1 o 2; m es 1 o 2; en el que dicho procedimiento comprende hacer reaccionar un compuesto de formula (2) con un compuesto de formula (7) en la presencia de al menos un ácido de Lewis.
ARP050102636A 2004-06-29 2005-06-27 Procedimientos para la preparacion de inhibidores de p2x7, composicion farmaceutica y un metodo de preparacion AR052307A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US58381304P 2004-06-29 2004-06-29
US66975605P 2005-04-08 2005-04-08

Publications (1)

Publication Number Publication Date
AR052307A1 true AR052307A1 (es) 2007-03-14

Family

ID=35124636

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050102636A AR052307A1 (es) 2004-06-29 2005-06-27 Procedimientos para la preparacion de inhibidores de p2x7, composicion farmaceutica y un metodo de preparacion

Country Status (13)

Country Link
US (1) US20050288288A1 (es)
EP (1) EP1768965A1 (es)
JP (1) JP2008504362A (es)
KR (1) KR20070115583A (es)
AR (1) AR052307A1 (es)
AU (1) AU2005258924A1 (es)
BR (1) BRPI0512651A (es)
CA (1) CA2572118A1 (es)
IL (1) IL180239A0 (es)
MX (1) MXPA06015273A (es)
NO (1) NO20070528L (es)
TW (1) TW200612965A (es)
WO (1) WO2006003513A1 (es)

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ATE541832T1 (de) 2009-04-14 2012-02-15 Affectis Pharmaceuticals Ag Neuartige p2x7r-antagonisten und ihre verwendung
CN102858741A (zh) 2010-05-14 2013-01-02 阿费克蒂斯制药股份公司 制备p2x7r拮抗剂的新方法
WO2012110190A1 (en) 2011-02-17 2012-08-23 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use
WO2012163792A1 (en) 2011-05-27 2012-12-06 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use
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Also Published As

Publication number Publication date
MXPA06015273A (es) 2007-03-15
CA2572118A1 (en) 2006-01-12
WO2006003513A1 (en) 2006-01-12
EP1768965A1 (en) 2007-04-04
AU2005258924A1 (en) 2006-01-12
NO20070528L (no) 2007-03-29
IL180239A0 (en) 2007-07-04
JP2008504362A (ja) 2008-02-14
KR20070115583A (ko) 2007-12-06
US20050288288A1 (en) 2005-12-29
TW200612965A (en) 2006-05-01
BRPI0512651A (pt) 2008-03-25

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