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MXPA04003828A - Novedosos inhibidores de dipeptidil peptidasa iv (dp-iv) como agentes antiabeticos. - Google Patents

Novedosos inhibidores de dipeptidil peptidasa iv (dp-iv) como agentes antiabeticos.

Info

Publication number
MXPA04003828A
MXPA04003828A MXPA04003828A MXPA04003828A MXPA04003828A MX PA04003828 A MXPA04003828 A MX PA04003828A MX PA04003828 A MXPA04003828 A MX PA04003828A MX PA04003828 A MXPA04003828 A MX PA04003828A MX PA04003828 A MXPA04003828 A MX PA04003828A
Authority
MX
Mexico
Prior art keywords
lower alkyl
optionally substituted
inhibitors
phenyl
independently
Prior art date
Application number
MXPA04003828A
Other languages
English (en)
Inventor
Andre Tartar
Original Assignee
Ferring Bv
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 Ferring Bv filed Critical Ferring Bv
Publication of MXPA04003828A publication Critical patent/MXPA04003828A/es

Links

Classifications

    • 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
    • A61K31/426—1,3-Thiazoles
    • 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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
    • 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
    • C07D277/04—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • 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)
  • Animal Behavior & Ethology (AREA)
  • Diabetes (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)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Peptides Or Proteins (AREA)

Abstract

(ver formula 1)la presente invencion se refiere a una serie de profarmacos de inhibidores de la dipeptidil peptidasa IV (DP-IV) con propiedades mejoradas. Los compuestos pueden usarse ara el tratamiento de cierto numero de enfermedades humanas, incluyendo la tolerancia deteriorada a la glucosa y la diabetes tipo II. Los compuestos de la invencion estan descritos por la formula general (1); en donde R1 es H o CN; R2 se selecciona de CH2R5, CH2CH2R5 y C(R3) (R4) - X2 (CH2)aR5; R3 Y R4 se seleccionan, cada uno independientemente, de H y Me; R5 se selecciona de con (R6) (R7), N(R8) C (=O) R9, N(R8) C (=S) R9, N(R8) y N(R8)R10; R6 Y R7 son cada uno, independientemente, R11(CH2)b o en forma conjunta son -(CH2)2-Z-(CH2)2- O -CH2-O-C6H4-Z-CH2-; R8 es H o Me; R9 se selecciona de R11(CH2)b, R11(CH2)bO y N(R6) (R7); R10 es R11(CH2)b R11 se selecciona de H, alquilo, arilo opcionalmente substituido, aroilo opcionalmente substituido, arilsulfonilo opcionalmente substituido y heteroarilo opcionalmente substituido; R12 se selecciona de H2NCH(R13)CO, H2NCH(R14)CONHCH(R15)CO, C(R16)=C(R17)COR18 Y R19OCO; R13, R14 Y R15 se seleccionan de las cadenas laterales de los aminoacidos proteinicos; R16 se selecciona de H, alquilo inferior (C1 - C6) y fenilo; R17 se selecciona de H y alquilo inferior (C1 - C6); R18 se selecciona de H, alquilo inferior (C1 - C6), OH, O-(alquilo inferior (C1 - C6)) y fenilo; R19 se selecciona de alquilo inferior (C1 - C6), fenilo opcionalmente substituido y R20C(=O)OC(R21)(R22); R20, R21 y R22 se seleccionan, cada uno, independientemente, de H y alquilo inferior (C1 - C6); Z se selecciona de un enlace covalente, -(CH2)C, -O-, -SOd- Y -N(R10)-; X1 es S o CH2; X2 es O, S o Ch2; a es 1, 2 o 3; b es 0 - 3; c es 1 o 2; y d es 0, 1 o 2.
MXPA04003828A 2001-10-23 2002-10-23 Novedosos inhibidores de dipeptidil peptidasa iv (dp-iv) como agentes antiabeticos. MXPA04003828A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0125446.5A GB0125446D0 (en) 2001-10-23 2001-10-23 Novel anti-diabetic agents
PCT/GB2002/004787 WO2003035067A1 (en) 2001-10-23 2002-10-23 Novel dipeptidyl peptidase iv (dp-iv) inhibitors as anti-diabetic agents

Publications (1)

Publication Number Publication Date
MXPA04003828A true MXPA04003828A (es) 2004-07-16

Family

ID=9924376

Family Applications (1)

Application Number Title Priority Date Filing Date
MXPA04003828A MXPA04003828A (es) 2001-10-23 2002-10-23 Novedosos inhibidores de dipeptidil peptidasa iv (dp-iv) como agentes antiabeticos.

Country Status (18)

Country Link
US (1) US7144886B2 (es)
EP (1) EP1450794A1 (es)
JP (1) JP2005510499A (es)
KR (1) KR20040049321A (es)
CN (1) CN1329375C (es)
AR (1) AR037247A1 (es)
CA (1) CA2464256A1 (es)
GB (1) GB0125446D0 (es)
HU (1) HUP0402403A3 (es)
IL (1) IL161192A0 (es)
MX (1) MXPA04003828A (es)
NO (1) NO20042114L (es)
NZ (1) NZ532044A (es)
PL (1) PL370149A1 (es)
RU (1) RU2004110055A (es)
UY (1) UY27511A1 (es)
WO (1) WO2003035067A1 (es)
ZA (1) ZA200402500B (es)

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Also Published As

Publication number Publication date
PL370149A1 (en) 2005-05-16
US7144886B2 (en) 2006-12-05
CN1575171A (zh) 2005-02-02
AR037247A1 (es) 2004-11-03
GB0125446D0 (en) 2001-12-12
UY27511A1 (es) 2003-04-30
NZ532044A (en) 2005-03-24
HUP0402403A2 (hu) 2005-04-28
ZA200402500B (en) 2005-01-24
IL161192A0 (en) 2004-08-31
HUP0402403A3 (en) 2009-05-28
KR20040049321A (ko) 2004-06-11
JP2005510499A (ja) 2005-04-21
WO2003035067A1 (en) 2003-05-01
NO20042114L (no) 2004-07-21
CN1329375C (zh) 2007-08-01
EP1450794A1 (en) 2004-09-01
RU2004110055A (ru) 2005-10-20
CA2464256A1 (en) 2003-05-01
US20050004205A1 (en) 2005-01-06

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