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CO5150220A1 - 4-carboxiamino-2- metil-1,2,3,4-tetrahidroquinolinas - Google Patents

4-carboxiamino-2- metil-1,2,3,4-tetrahidroquinolinas

Info

Publication number
CO5150220A1
CO5150220A1 CO99057639A CO99057639A CO5150220A1 CO 5150220 A1 CO5150220 A1 CO 5150220A1 CO 99057639 A CO99057639 A CO 99057639A CO 99057639 A CO99057639 A CO 99057639A CO 5150220 A1 CO5150220 A1 CO 5150220A1
Authority
CO
Colombia
Prior art keywords
substituted
optionally
mono
carbon
oxo
Prior art date
Application number
CO99057639A
Other languages
English (en)
Inventor
Michael Paul Deninno
Christian James Mularski
Roger Benjamin Ruggeri
Ronald Thure Wester
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 CO5150220A1 publication Critical patent/CO5150220A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom 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
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/38—Nitrogen atoms
    • C07D215/42—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Un compuesto de la fórmula I<EMI FILE="99057639_1" ID="1" IMF=JPEG >uno de sus profármacos, una sal farmacéuticamente aceptable de dicho compuesto o de dicho profármaco;en la que R1 es hidrógeno, Y, W-X, W-Y;en el que W es un carbonilo, tiocarbonilo, sulfinilo o sulfonilo;X es -a-Y, -S-Y, -N(H)-Y o -N-(Y)2;Y en cada caso es independientemente Z o una cadena de carbonos, lineal o ramificada, de uno a diez miembros, totalmente saturada, parcialmente insaturada o totalmente insaturada, en la que los carbonos, distintos del carbono de unión, pueden estar reemplazados opcionalmente por uno o dos heteroátomos seleccionados independientemente de oxígeno, azufre y nitrógeno, y dicho carbono está opcionalmente mono-, di- o tri-sustituido independientemente con halógeno, dicho carbono está opcionalmente mono- sustituido con hidroxi, dicho carbono está opcionalmente mono-sustituido con oxo, dicho azufre está opcionalmente mono- o di-sustituido con oxo, dicho nitrógeno está opcionalmente mono- o di-sustituido con oxo y dicha cadena de carbonos está opcionalmente mono-sustituida con Z; en el que Z es un anillo, de tres a doce miembros, parcialmente saturado, totalmente saturado o totalmente insaturado, que tiene opcionalmente uno a cuatro heteroátomos seleccionados independientemente de oxígeno, azufre y nitrógeno, o un anillo bicíclico que consiste en dos anillos, de tres a seis miembros, fusionados, parcialmente saturados, totalmente saturados o totalmente insaturados, considerados independientemente, teniendo opcionalmente de uno a cuatro heteroátomos seleccionados independientemente de nitrógeno, azufre y oxígeno;en el que dicho sustituyente Z está opcionalmente mono-, di- o tri-sustituido independientemente con halógeno, alquenilo(C2-C6), alquilo(C1-C6), hidroxi, alcoxi(C1-C6), alquiltio(C1-C4), amino, nitro, ciano, oxo, carboxi, alquiloxi (C1-C6)-carbonilo, mono-N- o di-N,N-alquilamino(C1-C6) en el que dicho sustituyente alquilo(C1-C6) está opcionalmente mono-, di- o tri-sustituido independientemente con halógeno, hidroxi, alcoxi(C1-C6), alquiltio(C1-C4), amino, nitro, ciano, oxo, carboxi, alquiloxi(C1-C6)-carbonilo, mono-N- o di-N,N-alquilamino(C1-C6), estando dicho alquilo(C1-6) opcionalmente sustituido con uno a nueve átomos de flúor; R3 es hidrógeno o Q; en el que Q es una cadena de carbonos, lineal o ramificada, de uno a seis miembros, totalmente saturada, parcialmente insaturada o totalmente insaturada, en la que los carbonos, distintos del carbono de unión, pueden estar reemplazados opcionalmente por un heteroátomo- 2 - seleccionado de oxígeno, azufre y nitrógeno, y dicho carbono está opcionalmente mono-, di- o tri-sustituido independientemente con halógeno, dicho carbono está opcionalmente mono-sustituido con hidroxi, dicho carbono está opcionalmente mono-sustituido con oxo, dicho azufre está opcionalmente mono- o di-sustituido con oxo, dicho nitrógeno está opcionalmente mono- o di-sustituido con oxo y dicha cadena de carbonos está opcionalmente mono-sustituida con V; en el que V es un anillo, de tres a doce miembros parcialmente saturado, totalmente saturado o totalmente insaturado, que tiene opcionalmente de uno a cuatro heteroátomos seleccionados independientemente de oxígeno, azufre y nitrógeno, o un anillo bicíclico que consiste en dos anillos, de tres a seis miembros, fusionados, parcialmente saturados, totalmente saturados o totalmente insaturados, considerados independientemente, que tienen opcionalmente de uno a cuatro heteroátomos seleccionados independientemente de nitrógeno, azufre y oxígeno; en el que dicho sustituyente V está opcionalmente mono-, di-, tri o tetra-sustituido independientemente con halógeno, alquilo(C1-C6), alquenilo(C2-C6), hidroxi, alcoxi(C1-C6), alquiltio(C1-C4), amino, nitro, ciano, oxo, carboxamoilo, mono-N- o di-N,N-alquil(C1-C6)-carboxamoilo, carboxi, alquiloxi(C1-C6)-carbonilo, mono-N- o di-N,N-alquilamino(C1-C6), en el que dicho sustituyente alquilo(C1-C6) o alquenilo(C2-C6) está opcionalmente mono-, di- o tri-sustituido independientemente con hidroxi, alcoxi(C1-C6), alquiltio(C1-C4), amino, nitro, ciano, oxo, carboxi, alquiloxi(C1-C6)-carbonilo, mono-N- o di-N,N- alquilamillo(C1-C6), estando dicho alquilo(C1-C6) o alquenilo(C2-C6) opcionalmente sustituido con uno a nueve átomos de flúor; R4 esQ1 oV1; en el que Q1 es una cadena de carbonos, lineal o ramificada, de uno a seis miembros, totalmente saturada, parcialmente insaturada o totalmente insaturada, en la que los carbonos, distintos del carbono de unión, pueden estar reemplazados opcionalmente por un heteroátomo seleccionado de oxígeno, azufre y nitrógeno, y dicho carbono está opcionalmente mono-, di- o tri-sustituido independientemente con halógeno, dicho carbono está opcionalmente mono-sustituido con hidroxi, dicho carbono está opcionalmente mono-sustituido con oxo, dicho azufre está opcionalmente mono- o di-sustituido con oxo, dicho nitrógeno está opcionalmentc mono- o di-sustituido con oxo, y dicha cadena de carbonos está opcionalmente mono- sustituida con V1; en el que V1 es un anillo, de tres a seis miembros, parcialmente saturado, totalmente saturado o totalmente insaturado, que tiene uno a dos heteroátomos seleccionados independientemente de oxígeno, azufre y nitrógeno; en el que dicho sustituyente V1 está opcionalmente mono-, di-, tri- o tetra-sustituido independientemente con halógeno, alquilo(C1-C6), alcoxi(C1-C6), amino, nitro, ciano, alquiloxi(C1-C6)-carbonilo, mono-N- o di-N,N-alquilamino(C1-C6), en el que dicho sustituyente alquilo(C1-C6) está opcionalmente mono-sustituido con oxo, teniendo opcionalmente dicho sustituyente alquilo(C1-C6) de uno a nueve átomos de flúor; en la que R3 debe contener V o R4 debe contener V1; y R5, R6, R7, y R8 son cada uno independientemente hidrógeno, un enlace, nitro o halo, en el que dicho enlace está sustituido con T o una cadena de carbonos lineal o ramificada de (C1-C12) parcial o completamente saturada, o completamente insaturada, reemplazándose opcionalmente dicho carbono con uno o dos heteroátomos seleccionados independientemente de oxígeno, azufre y nitrógeno, en el que dichos átomos de carbono están mono-, di- o tri-sustituidos independientemente con halo, dicho carbono está mono-sustituido con hidroxi, dicho carbono está mono-sustituido con oxo, dicho azufre está opcionalmente mono- o di-sustituido con oxo, dicho nitrógeno está opcionalmente mono- o di-sustituido con oxo, y dicho carbono está mono-sustituido con T; en el que T es un anillo de tres a doce miembros parcial o completamente saturado o completamente insaturado, que tiene opcionalmente uno a cuatro heteroátomos seleccionados independientemente de oxígeno, azufre y nitrógeno; o un anillo bicíclico que comprende dos anillos condensados de tres a seis miembros parcial o completamente saturado, o completamente insaturado, tomados independientemente, teniendo opcionalmente uno a cuatro heteroátomos seleccionados independientemente de nitrógeno, azufre y oxígeno; en la que dicho sustituyente T está opcionalmente mono-, di- o tri-sustituido independientemente con halógeno, alquilo(C1-C6), alquenilo(C2-C6), hidroxi, alcoxi(C1-C6), alquiltio(C1-C4), amino, nitro, ciano, oxo, carboxi, alquiloxi(C1-C6)-carbonilo, mono-N- o di-N,N-alquilamino(C1-C6) en el que dicho sustituyente alquilo(C1-C6) está opcionalmente mono-, di- o tri-sustituido independientemente con hidroxi, alcoxi(C1-C6), alquiltio(C1-C4), amino, nitro, ciano, oxo, carboxi, alquiloxi(C1-C6)-carbonilo, mono-N- o di-N,N-alquilamino(C1-C6), o teniendo dicho alquilo(C1-C6) opcionalmente uno a nueve átomos de flúor; con la condición de que R5, R6, R7 y R8 no sea hidrógeno y no esté enlazado al resto de quinolina a través de oxi.
CO99057639A 1998-09-17 1999-09-10 4-carboxiamino-2- metil-1,2,3,4-tetrahidroquinolinas CO5150220A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US10092998P 1998-09-17 1998-09-17

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CO5150220A1 true CO5150220A1 (es) 2002-04-29

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Country Status (25)

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US (2) US6147090A (es)
EP (1) EP1114033B1 (es)
JP (1) JP3655193B2 (es)
AR (1) AR021482A1 (es)
AT (1) ATE277906T1 (es)
AU (1) AU5439899A (es)
BR (1) BR9913842A (es)
CA (1) CA2344556A1 (es)
CO (1) CO5150220A1 (es)
DE (1) DE69920727T2 (es)
DK (1) DK1114033T3 (es)
DZ (1) DZ2889A1 (es)
ES (1) ES2228086T3 (es)
GT (1) GT199900149A (es)
HN (1) HN1999000155A (es)
MA (1) MA26687A1 (es)
MY (1) MY121838A (es)
PA (1) PA8481501A1 (es)
PE (1) PE20001048A1 (es)
PT (1) PT1114033E (es)
SI (1) SI1114033T1 (es)
SV (1) SV1999000149A (es)
TN (1) TNSN99172A1 (es)
TW (1) TWI232859B (es)
WO (1) WO2000017166A1 (es)

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US6147090A (en) 2000-11-14
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