AR068748A1 - Derivados de piridina activadores de glucoquinasa - Google Patents

Derivados de piridina activadores de glucoquinasa

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Publication number
AR068748A1
AR068748A1 ARP080104388A ARP080104388A AR068748A1 AR 068748 A1 AR068748 A1 AR 068748A1 AR P080104388 A ARP080104388 A AR P080104388A AR P080104388 A ARP080104388 A AR P080104388A AR 068748 A1 AR068748 A1 AR 068748A1
Authority
AR
Argentina
Prior art keywords
denotes
mhet
mar
alk
atoms
Prior art date
Application number
ARP080104388A
Other languages
English (en)
Inventor
Christine Charon
Lars Thore Burgdorf
Daniel Cravo
Johannes Gleitz
Norbert Beier
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR068748A1 publication Critical patent/AR068748A1/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
    • C07D417/12—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
    • 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
    • A61K31/435—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • 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
    • C07D401/14—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 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
    • C07D417/14—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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Compuestos heterocíclicos de la formula (1) en donde R1, R2, R3, R4 denotan cada uno, de modo independiente entre sí, H, A, Hal, [C(R12)2]mAr, [C(R12)2]mHet, [C(R12)2]mO[C(R12)2]mR12, S(O)nR12, NR10R11, NO2, CN, COOR10, CONR10R11, NR10COR11, NR10CONR10R11, NR10SOnR11, COR10, SO3H, SOnNR10R11, O-Alk-NR10R11, O-Alk-O-Alk-NR10R11, O-Alk-O-R12, O[C(R12)2]mCONR10R11, O-Alk-NR10COR11, O[C(R12)2]mHet, O[C(R12)2]mAr, S(O)n[C(R12)2]mHet o S(O)n[C(R12)2]mAr; D denota un resto del grupo de formulas (2); R5, R6, R7, R8 denotan cada uno, de modo independiente entre sí, H, A, [C(R12)2]mAr, [C(R12)2]mHet, [C(R12)2]mOCOA, [C(R12)2]mO[C(R12)2]mR12, S(O)nR12, NR10R11, CN, COOR10, CONR10R11, NR10COR11, NR10CONR10R11, NR10SOnR11, COR10, SO3H, SOnNR10R11, O-Alk-NR10R11, O[C(R12)2]mCONR10R11, O-Alk-NR10COR11, O[C(R12)2]mHet, O[C(R12)2]mAr, S(O)n[C(R12)2]mHet o S(O)n[C(R12)2]mAr; R9 denota H, A, S(O)n[C(R12)2]mR10, CONR10R11, COR10, SOnNR10R11, [C(R12)2]mAr o [C(R12)2]mHet; R10, R11 denotan cada uno, de modo independiente entre sí, H, A, Ar o Het; A denota alquilo no ramificado o ramificado que tiene 1-10 átomos de C, en donde uno o varios grupos CH2 no adyacentes pueden estar reemplazados por O, S, SO, SO2, NH, NA', NAr, NHet y/o por grupos -CH=CH- y/o además 1-7 átomos de H pueden estar reemplazados por F, Cl, Br, =S, NR12 y/u =O o denota cicloalquilo que tiene 3-7 átomos de C, que no está sustituido o que está mono-, di- o trisustituido con =O, F, Cl, OH, OA', OAr', OHet', SOnA', SOnAr', SOnHet', NH2, NHA', NA'2, NHAr' y/o NHHet'; A' denota alquilo no ramificado o ramificado que tiene 1-6 átomos de C, en donde 1-7 átomos de H pueden estar reemplazados por F y/o Cl; Alk denota alquileno ramificado o no ramificado que tiene 1, 2, 3 o 4 átomos de C; Ar denota fenilo, naftilo o bifenilo, cada uno de los cuales no está sustituido o está mono-, di-, tri-, tetra o pentasustituido con A, Hal, [C(R12)2]mAr', [C(R12)2]mHet', O[C(R12)2]mR12, S(O)nR12, NH2, NHA', NA'2, NHAr', NHHet', NO2, CN, COOR12, CON(R12)2, NR12COR12, NR12CON(R12)2, NR12SOnR12, COR12, SO3H, SOnN(R12)2, O-Alk-N(R12)2, O[C(R12)2]mCON(R12)2, O-Alk-NR12COR12, O[C(R12)2]mHet', O[C(R12)2]mAr', S(O)n[C(R12)2]mHet' y/o S(O)n[C(R12)2]mAr'; Het denota un heterociclo saturado, insaturado o aromático mono- o bicíclico que tiene 1 a 4 átomos de N, O y/o S, que puede estar mono-, di- o trisustituido con Hal, A, [C(R12)2]mAr', [C(R12)2]mHet', O[C(R12)2]mAr', O[C(R12)2]mHet', [C(R12)2]m-cicloalquilo, [C(R12)2]mOR12, [C(R12)2]mN(R12)2, NO2, CN, [C(R12)2]mCOOR12, O[C(R12)2]mCOOR12, [C(R12)2]mCON(R12)2, [C(R12)2]mCONR12N(R12)2, O[C(R12)2]mCON(R12)2, O[C(R12)2]mCONR12N(R12)2, [C(R12)2]mNR12COA, NR12CON(R12)2, [C(R12)2]mNR12SO2A, COR12, SO2N(R12)2, S(O)mA, =S, =NR2 y/u =O (oxígeno del carbonilo); Ar' denota fenilo, naftilo o bifenilo, cada uno de los cuales no está sustituido o está mono-, di- o trisustituido con Hal, A, OR12, N(R12)2, NO2, CN, COOR12, CON(R12)2, NR12COA, NR12CON(R12)2, NR12SO2A, COR12, SO2N(R12)2, S(O)nA, [C(R12)2]mCOOR12 y/u O[C(R12)2]mCOOR12; Het' denota un heterociclo saturado, insaturado o aromático mono- o bicíclico que tiene 1 a 4 átomos de N, O y/o S, que puede estar mono-, di- o trisustituido con Hal, A, OR12, N(R12)2, NO2, CN, COOR12, CON(R12)2, NR12COA, NR12SO2A, COR12, SO2N(R12)2, S(O)nA, =S, =NR12 y/u =O (oxígeno de carbonilo); R12 denota H o alquilo no ramificado o ramificado que tiene 1, 2, 3, 4, 5 o 6 átomos de C o denota cicloalquilo que tiene 3-7 átomos de C, no sustituido o monosustituido con =O; Hal denota F, Cl, Br o I; m denota 0, 1, 2, 3 o 4; n denota 0, 1 o 2; con la condicion de que, cuando D denota tiazol, entonces R1 no sea igual a OCH2Ar u OCH2Het; y sus sales y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Son activadores de la glucoquinasa y se pueden usar para la prevencion y/o el tratamiento de diabetes de tipo 1 y 2, obesidad, neuropatía y/o nefropatía.
ARP080104388A 2007-10-09 2008-10-08 Derivados de piridina activadores de glucoquinasa AR068748A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP07019691 2007-10-09
EP08001168 2008-01-23

Publications (1)

Publication Number Publication Date
AR068748A1 true AR068748A1 (es) 2009-12-02

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US (1) US8420642B2 (es)
EP (1) EP2195312B1 (es)
JP (1) JP5567481B2 (es)
KR (1) KR20100090250A (es)
CN (1) CN101821264A (es)
AR (1) AR068748A1 (es)
AU (1) AU2008310097B2 (es)
BR (1) BRPI0818658A2 (es)
CA (1) CA2701806A1 (es)
CY (1) CY1113767T1 (es)
DK (1) DK2195312T3 (es)
EA (1) EA201000561A1 (es)
EC (1) ECSP10010158A (es)
ES (1) ES2399469T3 (es)
HR (1) HRP20120948T1 (es)
IL (1) IL204746A0 (es)
MX (1) MX2010003759A (es)
NZ (1) NZ585236A (es)
PL (1) PL2195312T3 (es)
PT (1) PT2195312E (es)
SI (1) SI2195312T1 (es)
WO (1) WO2009046784A1 (es)

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AU2008310097A1 (en) 2009-04-16
EA201000561A1 (ru) 2010-10-29
PT2195312E (pt) 2013-02-20
EP2195312A1 (en) 2010-06-16
NZ585236A (en) 2012-03-30
CN101821264A (zh) 2010-09-01
CY1113767T1 (el) 2016-07-27
ES2399469T3 (es) 2013-04-01
JP2010540667A (ja) 2010-12-24
AU2008310097B2 (en) 2013-05-16
US20100216794A1 (en) 2010-08-26
DK2195312T3 (da) 2013-01-02
IL204746A0 (en) 2010-11-30
US8420642B2 (en) 2013-04-16
WO2009046784A1 (en) 2009-04-16
EP2195312B1 (en) 2012-11-21
JP5567481B2 (ja) 2014-08-06
CA2701806A1 (en) 2009-04-16
PL2195312T3 (pl) 2013-04-30
MX2010003759A (es) 2010-04-21
BRPI0818658A2 (pt) 2015-04-14
ECSP10010158A (es) 2010-06-29
HRP20120948T1 (hr) 2012-12-31
KR20100090250A (ko) 2010-08-13

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