PE20050018A1 - Compuesto pentaciclico heteroaromatico como inhibidor de la proteina tirosina fosfatasa 1b (ptb1b) - Google Patents

Compuesto pentaciclico heteroaromatico como inhibidor de la proteina tirosina fosfatasa 1b (ptb1b)

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Publication number
PE20050018A1
PE20050018A1 PE2004000360A PE2004000360A PE20050018A1 PE 20050018 A1 PE20050018 A1 PE 20050018A1 PE 2004000360 A PE2004000360 A PE 2004000360A PE 2004000360 A PE2004000360 A PE 2004000360A PE 20050018 A1 PE20050018 A1 PE 20050018A1
Authority
PE
Peru
Prior art keywords
phenyl
alkyl
ptb1b
thiazo
ethylpropyl
Prior art date
Application number
PE2004000360A
Other languages
English (en)
Inventor
Tomoyuki Ikemoto
Masahiro Tanaka
Takeo Yuno
Johei Sakamoto
Hiroyuki Nakanishi
Yuichi Nakagawa
Takeshi Ohta
Shohei Sakata
Hisayo Morinaga
Original Assignee
Japan Tobacco 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 Japan Tobacco Inc filed Critical Japan Tobacco Inc
Publication of PE20050018A1 publication Critical patent/PE20050018A1/es

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    • 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
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
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    • 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
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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    • 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
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
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    • 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
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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    • 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
    • A61K31/428—Thiazoles condensed with carbocyclic rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
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    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
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    • C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Engineering & Computer Science (AREA)
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  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
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  • Neurosurgery (AREA)
  • Neurology (AREA)
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  • Pain & Pain Management (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Indole Compounds (AREA)

Abstract

SE REFIERE A UN ANILLO HETEROAROMATICO DE 5 ELEMENTOS REPRESENTADO POR LA FORMULA I, EN DONDE V ES =N o =CH; W ES S o O; m ES 0, 1 o 2; R1 Y R2 SON H o ALQUILO C1-C4; X ES N(R4), N(R5)CO-O, SO2-N(R5), ENTRE OTROS; R4 Y R5 SON H, ALQUILO C1-C6, ENTRE OTROS; n ES 0 a 4; p ES 0 o 1; L ES C(R20)(R21), ENTRE OTROS; R20 ES H, ALQUILO C1-C6, ENTRE OTROS; R21 ES H, ALQUILO C1-C6, ENTRE OTROS; R ES COO(R19), A1-COO(R19) o O-A1-COO(R19); R19 ES H o ALQUILO C1-C4; A1 ES ALQUILENO C1*-C4; B ES UN GRUPO ARILO O ANILLO HETEROAROMATICO; R3 ES H, HALOGENO, ALQUILO C1-C8, ALCOXI C1-C6; ENTRE OTROS; Y ES O, S, SO, SO2, CO, ENTRE OTROS; s ES 0 o 1; A ES ALQUILENO C1-C4 OPCIONALMENTE SUSTITUIDO POR CICLOALQUILO C3-C7; Z ES CICLOALQUILO C3-C7, ARILO, ANILLO HETEROAROMATICO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ACIDO 5-{4-[4-({[4-(1-ETILPROPIL)FENIL]ISOPROPILAMINO}METIL)FENIL]TIAZO-2-LILMETOXI}NICOTINICO; ACIDO 4-{4-[4-({[4-(1-ETILPROPIL)FENIL]ISOPROPILAMINO}METIL)FENIL]TIAZO-2-LILMETOXI}BENZOICO; ACIDO 6-{4-[4-({[4-(1-ETILPROPIL)FENIL]ISOPROPILAMINO}METIL)FENIL]TIAZO-2-LILMETOXI}NICOTINICO; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA QUE OPCIONALMENTE PUEDE CONTENER OTRAS SUSTANCIAS FARMACOLOGICAMENTE ACTIVAS. ESTOS COMPUESTOS SON INHIBIDORES DE LA PROTEINA TIROSINA FOSFATASA 1B (PTB1B) Y SON UTILES COMO AGENTES TERAPEUTICOS PARA LA DIABETES, COMPLICACIONES DIABETICAS, HIPERLIPIDEMIA, OBESIDAD Y SIMILARES
PE2004000360A 2003-04-09 2004-04-12 Compuesto pentaciclico heteroaromatico como inhibidor de la proteina tirosina fosfatasa 1b (ptb1b) PE20050018A1 (es)

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JP2003105267 2003-04-09
JP2003157590 2003-06-03

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US (1) US20060122181A1 (es)
EP (1) EP1553091A4 (es)
JP (1) JP3819415B2 (es)
KR (1) KR20050119201A (es)
AR (1) AR043860A1 (es)
AU (1) AU2004228565A1 (es)
BR (1) BRPI0409136A (es)
CA (1) CA2521830A1 (es)
CL (1) CL2004000778A1 (es)
CO (1) CO5700817A2 (es)
HK (1) HK1078086A1 (es)
MX (1) MXPA05010945A (es)
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PE (1) PE20050018A1 (es)
RU (1) RU2005134659A (es)
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WO (1) WO2004089918A1 (es)

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US8022058B2 (en) 2000-05-10 2011-09-20 The Trustees Of Columbia University In The City Of New York Agents for preventing and treating disorders involving modulation of the RyR receptors
ATE502928T1 (de) 2000-11-01 2011-04-15 Millennium Pharm Inc Stickstoffhaltige heterozyklische verbindungen und verfahren zu deren herstellung
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