AR044371A1 - Derivados de 6,7 dimetoxi isoquinolinas, inhibidores de gfta, compuestos, procedimiento, composicion farmaceutica y usos - Google Patents

Derivados de 6,7 dimetoxi isoquinolinas, inhibidores de gfta, compuestos, procedimiento, composicion farmaceutica y usos

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Publication number
AR044371A1
AR044371A1 ARP040101698A ARP040101698A AR044371A1 AR 044371 A1 AR044371 A1 AR 044371A1 AR P040101698 A ARP040101698 A AR P040101698A AR P040101698 A ARP040101698 A AR P040101698A AR 044371 A1 AR044371 A1 AR 044371A1
Authority
AR
Argentina
Prior art keywords
alkyl
substituted
heterocyclic ring
heteroatoms
alkoxide
Prior art date
Application number
ARP040101698A
Other languages
English (en)
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR044371A1 publication Critical patent/AR044371A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C07D217/18Aralkyl radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/10Heterocyclic 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 linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/10Heterocyclic 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 carbon chain containing aromatic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

Abstract

Los compuestos tienen utilidad para el tratamiento de la diabetes tipo II. Reivindicación 1: Compuestos de fórmula (1), donde: R1 es -alquilo inferior, -CH2-arilo, -cicloalquilo, -(CH2)3 -OC(=O)CH3, -alcohol inferior, -alquilo inferior-R10, - CH2COOH, o -CH2CH2OCH2CH3; R2 es -alquilo inferior, -CH2-arilo, -alcohol inferior, -CH2C(=O)NH2, o -alquilo inferior-R10, donde al menos uno de R1 o R2 es -CH3; R3 es -COOH, -alquilo inferior-COOH, -alcohol inferior, -CH2OCH3, -CH2NH2, -CH2NHSO2R11, -C(=O)R12, -CNHCH2CH2-R12, -C(=NH)-R12, -(CH2)nNHC(=O)R13, -(CH2)mC(=O)N(R15)(R16), -C(=NH)-R17, o -(CH2)n-R18; R4 es -H, -alcóxido inferior, -O-C(R7R8)C(=O)R19, -halógeno, -SCH3, -C=CHC(=O)-R10, -CH2CH2C(=O)-R10, -O-alcohol inferior, - OCH2CH(OH)CH2N=N+=N-, -OCH2CH2OCH2CH2Cl, -NHC(=O)CH2-R10, -NHC(=O)CH2-alquilo inferior, -O(CH2)n-cicloalquilo, -O-alqueno inferior, o un anillo heterocíclico insaturado de 5 miembros que contiene un heteroátomo que es S o O; R5 y R6 son cada uno independientemente -H, -halógeno o -alcóxido inferior; R7 y R8 son cada uno independientemente -H o -CH3; R10 es un heterociclilo saturado de 5 ó 6 miembros que contiene 1 ó 2 heteroátomos, donde cada heteroátomo se selecciona entre N y O y el grupo se une al resto de la molécula a un N del anillo; R11 es -CF3, -alquilo inferior, -CH2Cl, -CH2CF3, o -R12; R12 es un anillo heterocíclico de 5 ó 6 miembros saturado sustituido o no sustituido que contiene un heteroátomo que se selecciona entre N, O y S donde el anillo sustituido es el anillo heterocíclico sustituido con -OH o -fenilo; R13 es -alquilo inferior, -alcóxido inferior, o -(CH2)nR14; R14 es un anillo heterocíclico de 5 ó 6 miembros saturado o insaturado que contiene uno o dos heteroátomos que son seleccionados entre N y O; R15 es -H o -CH3; R16 es -H, -alquilo inferior, -CºN, -OH, -alcóxido inferior, o -CH2COOCH2CH3; R17 es -alcóxido inferior -NH2 o -N-alquilo inferior; R18 es un anillo heterocíclico saturado o insaturado de 5 miembros sustituido o no sustituido que contiene de 1 a 4 heteroátomos donde los heteroátomos se seleccionan entre N, O y S, donde el anillo sustituido es el anillo heterocíclico que está sustituido en uno o dos carbonos del anillo con =O, o sustituido en un N del anillo con -alcohol inferior o -alquilo inferior; R19 es -OH, -NHCH(CH3)2, -N(CH3)CH2-arilo, -N(CH3)-alquilo inferior, o la fórmula (2), o un heterociclilo de 5 ó 6 miembros saturado sustituido o no sustituido que contiene 1 ó 2 heteroátomos donde cada heteroátomo es independientemente seleccionado entre N, O y S, donde dicho heterociclilo sustituido es el heterociclilo sustituido con alquilo inferior; m es 0, 1 ó 2; n es 0 ó 1; y sus sales y ésteres farmacéuticamente aceptables.
ARP040101698A 2003-05-19 2004-05-17 Derivados de 6,7 dimetoxi isoquinolinas, inhibidores de gfta, compuestos, procedimiento, composicion farmaceutica y usos AR044371A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US47169003P 2003-05-19 2003-05-19

Publications (1)

Publication Number Publication Date
AR044371A1 true AR044371A1 (es) 2005-09-07

Family

ID=33452454

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Application Number Title Priority Date Filing Date
ARP040101698A AR044371A1 (es) 2003-05-19 2004-05-17 Derivados de 6,7 dimetoxi isoquinolinas, inhibidores de gfta, compuestos, procedimiento, composicion farmaceutica y usos

Country Status (19)

Country Link
US (1) US7067529B2 (es)
EP (1) EP1631551A2 (es)
JP (1) JP2006528218A (es)
KR (1) KR100785571B1 (es)
CN (1) CN100540537C (es)
AR (1) AR044371A1 (es)
AU (1) AU2004238521B2 (es)
BR (1) BRPI0410760A (es)
CA (1) CA2524958A1 (es)
CL (1) CL2004001069A1 (es)
CO (1) CO5630035A2 (es)
MX (1) MXPA05012415A (es)
MY (1) MY142768A (es)
NO (1) NO20054852L (es)
NZ (1) NZ543065A (es)
RU (1) RU2320648C2 (es)
TW (1) TW200426144A (es)
WO (1) WO2004101528A2 (es)
ZA (1) ZA200509290B (es)

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Also Published As

Publication number Publication date
CO5630035A2 (es) 2006-04-28
KR100785571B1 (ko) 2007-12-13
WO2004101528A3 (en) 2005-01-06
WO2004101528A2 (en) 2004-11-25
JP2006528218A (ja) 2006-12-14
ZA200509290B (en) 2007-04-25
TW200426144A (en) 2004-12-01
US20040259910A1 (en) 2004-12-23
CN100540537C (zh) 2009-09-16
CN1791581A (zh) 2006-06-21
MXPA05012415A (es) 2006-02-13
CL2004001069A1 (es) 2005-04-01
CA2524958A1 (en) 2004-11-25
RU2005139524A (ru) 2007-06-27
HK1091838A1 (zh) 2007-01-26
NZ543065A (en) 2009-07-31
AU2004238521A1 (en) 2004-11-25
RU2320648C2 (ru) 2008-03-27
MY142768A (en) 2010-12-31
US7067529B2 (en) 2006-06-27
NO20054852L (no) 2005-12-13
EP1631551A2 (en) 2006-03-08
BRPI0410760A (pt) 2006-06-27
NO20054852D0 (no) 2005-10-20
KR20060015267A (ko) 2006-02-16
AU2004238521B2 (en) 2007-07-26

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