AR066412A1 - Derivados de dibenzofurano y dibenzotiofeno, composiciones farmaceuticas que los contienen y usos en patologias tales como trastornos oseos, crecimiento de tumores, diabetes y obesidad. - Google Patents

Derivados de dibenzofurano y dibenzotiofeno, composiciones farmaceuticas que los contienen y usos en patologias tales como trastornos oseos, crecimiento de tumores, diabetes y obesidad.

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Publication number
AR066412A1
AR066412A1 ARP080101855A ARP080101855A AR066412A1 AR 066412 A1 AR066412 A1 AR 066412A1 AR P080101855 A ARP080101855 A AR P080101855A AR P080101855 A ARP080101855 A AR P080101855A AR 066412 A1 AR066412 A1 AR 066412A1
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Argentina
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alkyl
group
alkynyl
haloalkyl
cycloalkyl
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ARP080101855A
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English (en)
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Tarek S Mansour
Rajeev Hotchandani
Wei Li
Jianchang Li
Yuchuan Wu
Steve Tam
Jun Jun Wu
Joseph P Sypek
Iain Mcfadyen
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Wyeth Corp
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Publication of AR066412A1 publication Critical patent/AR066412A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/91—Dibenzofurans; Hydrogenated dibenzofurans
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
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    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/76—Dibenzothiophenes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/14—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 three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Furan Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicacion 1: Un compuesto de la formula (1), o una sal farmacéuticamente aceptable o éster de este, caracterizado porque: X es O, S, S(O), o S(O)2; R1-Y es un sustituyente en la posicion C2 o C3 de la formula 1; Y es S(O), o S(O)2; R1 es unaminoácido natural o no natural, carboxilo protegido o libre de carboxilo, ligado a N que contiene por lo menos un hidrogeno amino-alfa; R2 es un sustituyente en la posicion C7 o C8 de la formula 1, seleccionado de a) -C(O)OR6, b) -C(S)OR6, c) -C(S)R7, d) -C(S)NR7R8, e) -C(NR7)R7, f) -C(NR7)OR6, g) -C(NR7)NR7R8, h) un grupo alquenilo C2-10, i) alquinilo C2-10, j) haloalquilo C1-10, k) cicloalquilo C3-14, l) cicloheteroalquilo de 3 a 14 miembros y m) heteroarilo de 5 a 14 miembros, en dondeel grupo cicloheteroalquilo de 3 a 14 miembros, o el grupo heteroarilo de 5 a 14 miembros se liga al nucleo tricíclico por vía de un átomo de carbono en el anillo, y cada uno de h) -m) opcionalmente se sustituye con 1-4 grupos -Z-R9; R3 y R4independientemente son a) H, b) -CN, c) -NO2, d) halogeno, e) -OR6, f) -NR7R8, g) S(O)mR7, h) S(O)mOR6, i) C(O)R7, j) C(O)OR6, k) -C(O)NR7R8, l) -C(S)R7, m) -C(S)OR6, n) -C(S)NR7R8, o) -C(NR7)R7, p) -C(NR7)OR6, q) -C(NR7)NR7R8, r) un grupo alquiloC1-10, s) alquenilo C2-10, t) alquinilo C2-10, u) haloalquilo C1-10, v) cicloalquilo C3-14, w) arilo C6-14, x) cicloheteroalquilo de 3 a 14 miembros, o y) un grupo heteroarilo de 5 a 14 miembros, en donde cada uno de r) - y) opcionalmente sesustituye con 1- 4 grupos -Z-R9; R6 en cada ocurrencia, independientemente es a) H, b) -C(O)R7, c) -C(O)NR7R8, d) -C(S)R7, e) -C(S)NR7R8, f) -C(NR7)R7, g) -C(NR7)NR7R8, h) un grupo alquilo C1-10, i) alquenilo C2-10, j) alquinilo C2-10, k)haloalquilo C1-10, l) cicloalquilo C3-14, m) arilo C6-14, o) un grupo cicloheteroalquilo de 3 a 14 miembros, o p) un grupo heteroarilo de 5 a 14 miembros, en donde cada uno de h) - p) opcionalmente se sustituye con 1-4 grupos -Z-R9; R7 y R8, en cadaocurrencia, independientemente son a) H, b) -OH, c) -NH2, d) -S(O)mH, e) -S(O)mOH, f) -C(O)OH, g) -C(O)NH2, h) -C(S)NH2, i) -C(NH)NH2, j) -Oalquilo C1-10, k) -NH-alquilo C1-10, l) -N(alquilo C1-10)2, m) -S(O)m-alquilo C1-10, n) -S(O)m-Oalquilo C1-10, o) -C(O)-alquilo C1-10, p) -C(O)-Oalquilo C1-10, q) -C(O)NH-alquilo C1-10, r) -C(O)N(alquilo C1-10)2, s) -C(S)NH-alquilo C1-10, t) -C(S)N(alquilo C1-10)2, u) -C(NH)-alquilo C1-10, v) -C(NH)-Oalquilo C1-10, w) -C(NH)NH-alquilo C1-10, x) -C(NH)N(alquilo C1-10)2, y) -C(Nalquilo C1-10)-alquilo C1-10, z) -C(Nalquilo C1-10)-Oalquilo C1-10, aa) -C(Nalquilo C1-10)NH-alquilo C1-10, ab) -C(Nalquilo C1-10)N(alquilo C1-10)2, ac) un grupo alquilo C1-10, ad) alquenilo C2-10, ae) alquinilo C2-10,af) haloalquilo C1-10, ag) cicloalquilo C3-14, ah) arilo C6-14, ai) un grupo cicloheteroalquilo de 3 a 14 miembros, o aj) un grupo heteroarilo de 5 a 14 miembros, en donde cada uno del grupo alquilo C1-10, alquenilo C2-10, alquinilo C2-10,haloalquilo C1-10, cicloalquilo C3-14, arilo C6-14, el grupo cicloheteroalquilo de 3 a 14 miembros, y el grupo heteroarilo de 5 a 14 miembros opcionalmente se sustituye con 1-4 grupos -Z-R9; R9 en cada ocurrencia, independientemente es a) halogeno,b) -ON, c) -NO2, d) oxo, en donde dos R9 en un átomo de carbono unico se puede reemplazar, e) -O-Z-R10, f) -NR10-Z-R11, g) -N(O)R10-Z-R11, h) -S(O)mR10, i) -S(O)mO-Z-R10, j) -S(O)mNR10-Z-R11, k) -C(O)R10, l) -C(O)O-Z-R10, m) -C(O)NR10-Z-R11, n) -C(S)NR10-Z-R11, o) -C(NR10)R10, p) -C(NR10)O-Z-R10, q) -C(NR10)NR10-Z-R11, r) -Si(alquilo C1-10)3, s) un grupo alquilo C1-10, t) alquenilo C2-10, u) alquinilo C2-10, v) haloalquilo C1-10, w) cicloalquilo C3-14, x) arilo C6-14, y) un grupocicloheteroalquilo de 3 a 14 miembros, o z) un grupo heteroarilo de 5 a 14 miembros, en donde cada uno del grupo alquilo C1-10, alquenilo C2-10, alquinilo C2-10, haloalquilo C1-10, cicloalquilo C3-14, arilo C6-14, el grupo cicloheteroalquilo de 3 a14 miembros, y el grupo heteroarilo de 5 a 14 miembros opcionalmente se sustituye con 1- 4 grupos -Z-R12; R10 y R11, en cada ocurrencia, independientemente son a) H, b) -OH, c) -NH2, d) S(O)mH, e) S(O)mOH, f) -C(O)OH, g) -C(O)NH2, h) -C(S)NH2, i) -C(NH)NH2, j) -Oalquilo C1-10, k) -NH-alquilo C1-10, l) -N(alquilo C1-10)2, m) -S(O)m-alquilo C1-10, n) -S(O)m-Oalquilo C1-10, o) -C(O)-alquilo C1-10, p) -C(O)-Oalquilo C1-10, q) -C(O)NH-alquilo C1-10, r) -C(O)N(alquilo C1-10)2, s) -C(S)NH-alquilo C1-10, t) -C(S)N(alquilo C1-10)2, u) -C(NH)-alquilo C1-10, v) -C(NH)-Oalquilo C1-10, w) -C(NH)NH-alquiloC1-10, x) -C(NH)N(alquilo C1-10)2, y) -C(Nalquilo C1-10)-alquilo C1-10, z) -C(Nalquilo C1-10)-Oalquilo C1-10, aa) -C(Nalquilo C1-10)NH-alquilo C1-10, ab) -C(Nalquilo C1-10)N(alquilo C1-10)2, ac) un grupo alquilo C1-10, ad) alquenilo C2-10, ae) alquinilo C2-10, af) haloalquilo C1-10, ag) cicloalquilo C3-14, ah) arilo C6-14, ai) un grupo cicloheteroalquilo de 3 a 14 miembros, o aj) un grupoheteroarilo de 5 a 14 miembros, en donde cada uno del grupo alquilo C1-10, alquenilo C2-10, alquinilo C2-10, haloalquilo C1-10, cicloalquilo C3-14, arilo C6-14, el grupo cicloheteroalquilo de 3 a 14 miembros, y el grupo heteroarilo de 5 a 14miembros opcionalmente se sustituye con 1-4 grupos -Z-R12; R12 en cada ocurrencia, independientemente es a) halogeno, b) -CN, c) -NO2 d) oxo, en donde dos R12 en un carbono unico se puede reemplazar e) -OH, f) -NH2, g) -NH(alquilo C1-10), h) -N(alquilo C1-10)2, i) -S(O)mH, j) -S(O)m-alquilo C1-10, k) -S(O)mOH, l) -S(O)m-Oalquilo C1-10, m) -CHO, n) -C(O)-alquilo C1-10, o) -C(O)OH, p) -C(O)-Oalquilo C1-10, q) -C(O)NH2, r) -C(O)NH-alquilo C1-10, s) -C(O)N(alquilo C1-10)2, t) -C(NH)H, u) -C(NH)-alquilo C1-10, v) -C(NH)OH, w) -C(NH)-Oalquilo C1-10, x) -C(NH)NH2, y) -C(NH)NH-alquilo C1-10, z) -C(NH)N(alquilo C1-10)2, aa) -C(Nalquilo C1-10)H, ab) -C(Nalquilo C1-10)-alquilo C1-10, ac) -C(Nalquilo C1-10)OH, ad) -C(Nalquilo C1-10)-OalquiloC1-10, ae) -C(Nalquilo C1-10)NH2, af) -C(Nalquilo C1-10)NH-alquilo C1-10, ag) -C(Nalquilo C1-10)N(alquiIo C1-10)2, ah) -C(S)NH2, ai) -C(S)NH-alquilo C1-10, aj) -C(S)N(alquilo C1-10)2, ak) -S(O)mNH2, al) -S(O)mNH(alquilo C1-10), am) -S(O)mN(alquiloC1-10)2, an) -Si(alquilo C1-10)3, ap) un grupo alquilo C1-10, aq) alquenilo C2-10, ar) alquinilo C2-10, as) haloalquilo C1-10, at) cicloalquilo C3-14, au) arilo C6-14, ay) un grupo cicloheteroalquilo de 3 a 14 miembros, o aw) un grupo heteroarilo de5 a 14 miembros; en donde cada uno de ap) a av) se sustituye opcionalmente con 1-4 grupos seleccionados de halogeno, -CN, -NO2, -OH, -O(alquilo C1-10), -NH2, -NH(alquilo C1-10), y -N(alquilo C1-10)2; Z, en cada ocurrencia, independientemente es a)un grupo alquilo C1-10 divalente, b) un grupo alquenilo C2-10 divalente, c) un grupo alquinilo C2-10 divalente, d) un grupo haloalquilo C1-10 divalente, o e) -Z- es un enlace; y m, en cada ocurrencia, independientemente es 0, 1 o 2.
ARP080101855A 2007-05-04 2008-04-30 Derivados de dibenzofurano y dibenzotiofeno, composiciones farmaceuticas que los contienen y usos en patologias tales como trastornos oseos, crecimiento de tumores, diabetes y obesidad. AR066412A1 (es)

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US (1) US20100227859A1 (es)
EP (1) EP2144893A2 (es)
JP (1) JP2010526106A (es)
AR (1) AR066412A1 (es)
CA (1) CA2685389A1 (es)
CL (1) CL2008001257A1 (es)
MX (1) MX2009011749A (es)
PA (1) PA8779101A1 (es)
PE (1) PE20090223A1 (es)
TW (1) TW200900397A (es)
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US9273021B2 (en) 2009-02-05 2016-03-01 Trustees Of Boston College Dibenzofuran derivatives as inhibitors of fructose 1,6-bisphosphatase and methods of use thereof
MX2011010482A (es) * 2009-04-06 2012-01-30 Ptc Therapeutics Inc Compustos y métodos para tratamiento antiviral.
WO2014123032A1 (ja) 2013-02-08 2014-08-14 三菱瓦斯化学株式会社 レジスト組成物、レジストパターン形成方法及びそれに用いるポリフェノール誘導体
AU2014249192B2 (en) 2013-03-11 2017-12-21 The Regents Of The University Of Michigan BET bromodomain inhibitors and therapeutic methods using the same
EP2907512A1 (en) 2014-02-14 2015-08-19 Commissariat A L'energie Atomique Et Aux Energies Alternatives Inhibitors of MMP-12 as antiviral Agents
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