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AR049139A1 - Compuestos derivados de benzamidas n - heterociclil - sustituidas como activadores de la glucoquinasa (glk), metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso como medicamento en el tratamiento de la diabetes tipo ii. - Google Patents

Compuestos derivados de benzamidas n - heterociclil - sustituidas como activadores de la glucoquinasa (glk), metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso como medicamento en el tratamiento de la diabetes tipo ii.

Info

Publication number
AR049139A1
AR049139A1 ARP050102265A ARP050102265A AR049139A1 AR 049139 A1 AR049139 A1 AR 049139A1 AR P050102265 A ARP050102265 A AR P050102265A AR P050102265 A ARP050102265 A AR P050102265A AR 049139 A1 AR049139 A1 AR 049139A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
alkoxy
group
substituted
Prior art date
Application number
ARP050102265A
Other languages
English (en)
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
Priority claimed from GBGB0412602.5A external-priority patent/GB0412602D0/en
Priority claimed from GB0423041A external-priority patent/GB0423041D0/en
Priority claimed from GB0502961A external-priority patent/GB0502961D0/en
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR049139A1 publication Critical patent/AR049139A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or 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
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or 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
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
    • 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

La presente se refiere a composiciones farmacéuticas que contienen tales compuestos y al uso de esos compuestos y composiciones para la prevencion y/o tratamiento de trastornos hiper-proliferativos y enfermedades asociadas con la angiogénesis. Reivindicacion 1: Un compuesto de formula (1) en la cual R1 se selecciona del grupo integrado por arilo, bencilo, y heteroarilo, donde arilo y heteroarilo pueden estar opcionalmente sustituidos con 0, 1, 2, 3 o 4 sustituyentes seleccionados independientemente del grupo integrado por alquilo C1-4, donde alquilo C1-4 puede estar sustituido con 0, 1, 2 o 3 halogenos, 0 o 1 heterociclilo, o 0 o 1 alcoxi C1-3, donde alcoxi C1-3 puede estar opcionalmente sustituido con alquilamino C1-3; alcoxi C1-3, donde alcoxi C1-3 puede estar opcionalmente sustituido con alquilamino C1-3; halogeno; trifluorometilo; trifluorometoxi; cicloalquilo C3-6; fenilo opcionalmente sustituido con 1 o 2 halogenos; un resto de formula (2), donde X es CH2, O, S o NR1-1, y donde R1-1 es H o alquilo C1-6; nitro; ciano; alquiltio C1-3; trifluorometiltio; alquil C1-3-carbonilo; alcoxi C1-6-carbonilo; y fenoxi, donde fenoxi puede estar opcionalmente sustituido con 0, 1 o 2 sustituyentes seleccionados independientemente del grupo integrado por alquilo C1-6, alcoxi C1-6, trifluorometoxi y halogeno, y donde bencilo puede estar sustituido con 0, 1, 2 o 3 grupos seleccionados de halogeno, alquilo C1-3 y alcoxi C1-3; R2 se selecciona del grupo integrado por H, halogeno, alquilo C1-4 y alcoxi C1-4; R3 se selecciona del grupo integrado por carboxilo; formilo; alquil C1-6-carbonilo opcionalmente sustituido con 0, 1, 2 o 3 grupos seleccionados de F, Cl, hidroxi, alcoxi C1-6, y heterociclo; cicloalquil C3-6-carbonilo; alcoxi C1-6-carbonilo opcionalmente sustituido con 0, 1, 2 o 3 grupos seleccionados de amino y alcoxi C1-6-carbonilo; aminocarbonilo; alquilamino C1-6-carbonilo, donde alquilamino C1-6-carbonilo puede estar opcionalmente sustituido con 0, 1, 2 o 3 sustituyentes seleccionados independientemente del grupo integrado por cicloalquilo C3-6, halogeno, amino, alquilamino C1-6, hidroxi, alcoxi C1-6, alcoxi C1-6-carbonilo, alquiltio C1-6, alcoxi C1-6- carbonilamino, y metilsulfonilo, y donde alquilamino C1-6-carbonilo puede estar opcionalmente sustituido con 0 o 1 heterociclilo, donde heterociclilo puede estar opcionalmente sustituido con 0 o 1 alquilo C1-6, y donde alquilamino C1-6-carbonilo puede estar opcionalmente sustituido con 0 o 1 fenilo, donde fenilo puede estar opcionalmente sustituido con 0 o 1 halogeno, alquilo C1-6, o alcoxi C1-6; heterociclilcarbonilo opcionalmente sustituido con 0 o 1 amino, alquilamino C1-6, cicloalquilo, o alquilo C1-6, donde alquilo C1-6 puede estar opcionalmente sustituido con 0 o 1 amino o alquilamino C1-6; alquilo C1-6 opcionalmente sustituido con 0, 1, 2 o 3 sustituyentes seleccionados independientemente del grupo integrado por: a) hidroxilo, b) amino, c) alquilamino C1-6, donde alquilamino C1-6 puede estar sustituido con 0, 1, 2, 3 o 4 sustituyentes seleccionados independientemente del grupo integrado por halogeno, amino, alquilamino, metoxi, metilito y metilsulfonilo, d) arilamino, donde arilamino puede estar sustituido con 0, 1 o 2 sustituyentes seleccionados independientemente del grupo integrado por alquilo C1-6, alcoxi C1-6, y trifluorometilo, e) heterociclilo, donde heterociclilo puede estar sustituido con 0, 1 o 2 alquilo C1-6, donde alquilo C1-6 puede estar sustituido con 0, 1 o 2 hidroxi, metoxi o piridilo; f) imidazolilo, g) piridilamino, h) alcoxi C1-3 opcionalmente sustituido con fluoro hasta el nivel de perfluoro, o con heterociclo, donde heterociclo puede estar opcionalmente sustituido con 0 o 1 alquilo C1-6, i) alcoxi C1-3-alcoxi C2-3, y j) alcoxi C1-6-carbonilo, k) cicloalquilo C3-6, l) ciano, alcoxi C1-6 opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente del grupo integrado por amino, alquilamino C1-6, y heterociclilo, donde heterociclilo puede estar sustituido con 0, 1, 2 o 3 alquilo C1-6, cicloalquilamino C3-6-carbonilo opcionalmente sustituido con alquilo C1-3, ciano, heteroarilo, donde heteroarilo puede estar sustituido con 0, 1, 2 o 3 grupos seleccionados independientemente del grupo integrado por k) alquilo C1-6, donde alquilo C1-6 puede estar sustituido con 0, 1, 2 o 3 halogeno, 0 o 1 heterociclilo, 0 o 1 alquilamino, o 0 o 1 hidroxi o metoxi, l) halogeno, m) amino, n) alquilamino, o) alcoxi C1-6-carbonilo, y p) cicloalquilo C3-6, heteroarilcarbonilo, el cual puede estar sustituido con 0, 1, 2 o 3 grupos seleccionados independientemente del grupo integrado por alquilo C1-6, cicloalquilo C3-6 y halogeno, heterociclilo, donde heterociclilo puede estar sustituido con 0, 1, 2, o 3 grupos seleccionados independientemente del grupo integrado por alquilo C1-6 y alcoxi C1-6-carbonilo; y R4 se selecciona del grupo integrado por H, alquilo C1-6, alcoxi C1-6 y halogeno; o su sal aceptable para uso farmacéutico.
ARP050102265A 2004-06-05 2005-06-02 Compuestos derivados de benzamidas n - heterociclil - sustituidas como activadores de la glucoquinasa (glk), metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso como medicamento en el tratamiento de la diabetes tipo ii. AR049139A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB0412602.5A GB0412602D0 (en) 2004-06-05 2004-06-05 Compounds
GB0423041A GB0423041D0 (en) 2004-10-16 2004-10-16 Chemical compounds
GB0502961A GB0502961D0 (en) 2005-02-12 2005-02-12 Chemical compounds

Publications (1)

Publication Number Publication Date
AR049139A1 true AR049139A1 (es) 2006-06-28

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ID=34969165

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ARP050102265A AR049139A1 (es) 2004-06-05 2005-06-02 Compuestos derivados de benzamidas n - heterociclil - sustituidas como activadores de la glucoquinasa (glk), metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso como medicamento en el tratamiento de la diabetes tipo ii.

Country Status (19)

Country Link
US (2) US7745475B2 (es)
EP (2) EP1756076B1 (es)
JP (1) JP4860606B2 (es)
KR (1) KR20070024650A (es)
AR (1) AR049139A1 (es)
AT (1) ATE477249T1 (es)
AU (1) AU2005251990B2 (es)
BR (1) BRPI0511808A (es)
CA (1) CA2566951A1 (es)
DE (1) DE602005022859D1 (es)
ES (1) ES2347451T3 (es)
IL (1) IL179389A0 (es)
MX (1) MXPA06014128A (es)
MY (1) MY144048A (es)
NO (1) NO20070032L (es)
NZ (1) NZ551623A (es)
TW (1) TW200600086A (es)
UY (1) UY28936A1 (es)
WO (1) WO2005121110A1 (es)

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