AR076850A1 - Derivados sustituidos de indazol y aza-indazol como moduladores de la gamma secretasa. - Google Patents

Derivados sustituidos de indazol y aza-indazol como moduladores de la gamma secretasa.

Info

Publication number
AR076850A1
AR076850A1 ARP100101549A ARP100101549A AR076850A1 AR 076850 A1 AR076850 A1 AR 076850A1 AR P100101549 A ARP100101549 A AR P100101549A AR P100101549 A ARP100101549 A AR P100101549A AR 076850 A1 AR076850 A1 AR 076850A1
Authority
AR
Argentina
Prior art keywords
halo
hydrogen
alkyl
alkyloxy
substituents
Prior art date
Application number
ARP100101549A
Other languages
English (en)
Original Assignee
Ortho Mcneil Janssen Pharm
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 Ortho Mcneil Janssen Pharm filed Critical Ortho Mcneil Janssen Pharm
Publication of AR076850A1 publication Critical patent/AR076850A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D471/04—Ortho-condensed systems

Landscapes

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

Abstract

Estos compuestos son utiles como moduladores de la gamma secretasa. Se proveen además composiciones farmacéuticas que comprenden dichos compuestos como ingrediente activo como así también con el uso de dichos compuestos como medicamento para el tratamiento de la enfermedad de Alzheimer y otras formas de demencia. Reivindicacion 1: Un compuesto de formula (1) y formas estereoisoméricas del mismo, en donde R1 es alquilo C1-6 opcionalmente sustituido con uno o más sustituyentes cada uno independientemente seleccionado del grupo que consiste de halo, alquiloxi C1-4, cicloalquilo C3-7, tetrahidropiranilo, tetrahidrofuranilo y fenilo; cicloalquilo C3-7; tetrahidropiranilo; tetrahidrofuranilo; 1,3-benzodioxolilo; o fenilo; en donde cada fenilo independientemente es opcionalmente sustituido con uno o más sustituyentes cada uno independientemente seleccionado del grupo que consiste de halo, ciano, alquilo C1-4 opcionalmente sustituido con uno o más sustituyentes halo, y alquiloxi C1-4 opcionalmente sustituido con uno o más sustituyentes halo; R2 es hidrogeno; ciano; o alquilo C1-4 opcionalmente sustituido con uno o más sustituyentes cada uno independientemente seleccionado del grupo que consiste de alquiloxi C1-4, halo y NR3R4; X1 es CH o N; X2 es CR5 o N; R5 es hidrogeno; halo; ciano; alquiloxi C1-4 o alquilo C1-4 opcionalmente sustituido con uno o más sustituyentes cada uno independientemente seleccionado del grupo que consiste de halo, alquiloxi C1-4 y NR3R4; X3 es CR6 o N; R6 es hidrogeno; halo; ciano; alquiloxi C1-4 o alquilo C1-4 opcionalmente sustituido con uno o más sustituyentes cada uno independientemente seleccionado del grupo que consiste de halo, alquiloxi C1-4 y NR3R4, en donde cada R3 es independientemente hidrogeno; alquilo C1-4; o acilo C1-4; en donde cada R4 es independientemente hidrogeno; alquilo C1-4, o acilo C1-4; con la condicion de que no más de dos de X1, X2 y X3 sean N; A1 es CR7 o N; en donde R7 es hidrogeno, halo o alquiloxi C1-4; A2, A3 y A4 cada uno independientemente son CH o N; con la condicion de que no más de dos de A1, A2, A3 y A4 sean N; Het1 es un heterociclo aromático de miembros, de formula (a-1), (a-2), (a-3) o (a-4), R8 es hidrogeno o alquilo C1-4; R9 es hidrogeno o alquilo C1-4; R10 es hidrogeno o alquilo C1-4; R11 es hidrogeno o alquilo C1-4; R12 es alquilo C1-4; G1 es O o S; G2 es CH o N; y sales de adicion, y los solvatos farmacéuticamente aceptables de los mismos.
ARP100101549A 2009-05-07 2010-05-06 Derivados sustituidos de indazol y aza-indazol como moduladores de la gamma secretasa. AR076850A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09159615 2009-05-07

Publications (1)

Publication Number Publication Date
AR076850A1 true AR076850A1 (es) 2011-07-13

Family

ID=40786448

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100101549A AR076850A1 (es) 2009-05-07 2010-05-06 Derivados sustituidos de indazol y aza-indazol como moduladores de la gamma secretasa.

Country Status (20)

Country Link
US (1) US8835482B2 (es)
EP (1) EP2427453B1 (es)
JP (1) JP5559309B2 (es)
KR (1) KR20120024555A (es)
CN (1) CN102439005B (es)
AR (1) AR076850A1 (es)
AU (1) AU2010262036B2 (es)
BR (1) BRPI1011190A8 (es)
CA (1) CA2755467A1 (es)
EA (1) EA019702B1 (es)
ES (1) ES2431619T3 (es)
IL (1) IL216113A (es)
MX (1) MX2011011753A (es)
MY (1) MY152998A (es)
NZ (1) NZ596843A (es)
SG (1) SG175317A1 (es)
TW (1) TWI461419B (es)
UA (1) UA105377C2 (es)
WO (1) WO2010145883A1 (es)
ZA (1) ZA201108117B (es)

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JP6072308B2 (ja) * 2013-02-21 2017-02-01 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ジヒドロプテリジノンｉｉ
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CN103880683B (zh) * 2014-02-26 2018-06-22 南通大学 一种3-溴-2-硝基苯甲醛的化学合成方法
JP6831372B2 (ja) * 2015-09-09 2021-02-17 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 架橋ピペリジン誘導体
CN105585547A (zh) * 2016-03-09 2016-05-18 中国科学院广州生物医药与健康研究院 一种4-五氟化硫苯酚类化合物及制备方法以及五氟化硫取代苯并吡喃类化合物的制备方法
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Also Published As

Publication number Publication date
BRPI1011190A8 (pt) 2016-11-16
ES2431619T3 (es) 2013-11-27
UA105377C2 (uk) 2014-05-12
ZA201108117B (en) 2015-06-24
EA019702B1 (ru) 2014-05-30
EP2427453B1 (en) 2013-07-17
EP2427453A1 (en) 2012-03-14
CN102439005A (zh) 2012-05-02
WO2010145883A1 (en) 2010-12-23
JP5559309B2 (ja) 2014-07-23
TW201105658A (en) 2011-02-16
IL216113A0 (en) 2012-01-31
AU2010262036B2 (en) 2014-10-30
CA2755467A1 (en) 2010-12-23
MY152998A (en) 2014-12-31
AU2010262036A1 (en) 2011-09-22
SG175317A1 (en) 2011-11-28
NZ596843A (en) 2012-12-21
TWI461419B (zh) 2014-11-21
US8835482B2 (en) 2014-09-16
EA201171363A1 (ru) 2012-04-30
JP2012526078A (ja) 2012-10-25
MX2011011753A (es) 2011-11-29
IL216113A (en) 2015-02-26
BRPI1011190A2 (pt) 2016-03-15
US20120095036A1 (en) 2012-04-19
CN102439005B (zh) 2015-07-22
KR20120024555A (ko) 2012-03-14

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