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AR074306A1 - Aminotetrahidropiranos como inhibidores de dipeptidil peptidasa-iv para el tratamiento o prevencion de diabetes - Google Patents

Aminotetrahidropiranos como inhibidores de dipeptidil peptidasa-iv para el tratamiento o prevencion de diabetes

Info

Publication number
AR074306A1
AR074306A1 ARP090104318A AR074306A1 AR 074306 A1 AR074306 A1 AR 074306A1 AR P090104318 A ARP090104318 A AR P090104318A AR 074306 A1 AR074306 A1 AR 074306A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
alkoxy
independently selected
hydroxy
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English (en)
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Merck Sharp & Dohme
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41559521&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR074306(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of AR074306A1 publication Critical patent/AR074306A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/16—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D309/28—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D309/30—Oxygen atoms, e.g. delta-lactones
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/1703—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • A61K38/1709—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/26—Glucagons
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61P3/06—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Endocrinology (AREA)
  • Marine Sciences & Fisheries (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

También se refiere a composiciones farmacéuticas que comprenden estos compuestos y al uso de estos compuestos. Reivindicación1: Un compuesto de fórmula estructural 1, o una sal farmacéuticamente aceptable del mismo; en el que V se selecciona entre el grupo que consiste en el grupo de fórmulas (2); Ar es fenilo opcionalmente sustituido por uno a cinco sustituyentes R1; cada R1 se selecciona independientemente entre el grupo que consiste en: halógeno, ciano, hidroxi, alquilo C1-6, opcionalmente sustituido por uno a cinco átomos de flúor; y alcoxi C1-4, opcionalmente sustituido por uno a cinco átomos de flúor; cada R2 se selecciona independientemente entre el grupo que consiste en hidrógeno, halógeno, ciano, alcoxi C1-10, donde el alcoxi está opcionalmente sustituido por uno a cinco sustituyentes seleccionados independientemente entre flúor e hidroxi, alquilo C1-10, donde el alquilo está opcionalmente sustituido por uno a cinco sustituyentes seleccionados independientemente entre flúor e hidroxi, alquenilo C2-10, donde el alquenilo está opcionalmente sustituido por uno a cinco sustituyentes seleccionados independientemente entre flúor e hidroxi, (CH2)n-arilo, donde el arilo está opcionalmente sustituido por uno a cinco sustituyentes seleccionados independientemente entre hidroxi, halógeno, cieno, nitro, CO2H, alquiloxi C1-6-carbonilo, alquilo C1-6 y alcoxi C1-6, donde el alquilo y el alcoxi están opcionalmente sustituidos por uno a cinco átomos de flúor, (CH2)n-heteroarilo, donde el heteroarilo está opcionalmente sustituido por uno a tres sustituyentes seleccionados independientemente entre hidroxi, halógeno, ciano, nitro, CO2H, alquiloxi C1-6-carbonilo, alquilo C1-6 y alcoxi C1-6, donde el alquilo y el alcoxi están opcionalmente sustituidos por uno a cinco átomos de flúor, (CH2)n-heterociclilo, donde el heterociclilo está opcionalmente sustituido por uno a tres sustituyentes seleccionados independientemente entre oxo, hidroxi, halógeno, ciano, nitro, COH, alquiloxi C1-6-carbonilo, alquilo C1-6 y alcoxi C1-6, donde el alquilo y el alcoxi están opcionalmente sustituidos por uno a cinco átomos de flúor, (CH2)n-cicloalquilo C3-6, donde el cicloalquilo está opcionalmente sustituido por uno a tres sustituyentes seleccionados independientemente entre halógeno, hidroxi, ciano, nitro, CO2H, alquiloxi C1-6-carbonilo, alquilo C1-6 y alcoxi C1-6, donde el alquilo y el alcoxi están opcionalmente sustituidos por uno a cinco átomos de flúor, (CH2)n-COOH, (CH2)n-COOalquilo C1-6, (CH2)n-NR4R5, (CH2)n-CONR4R5, (CH2)n-OCONR4R5, (CH2)n-SO2NR4R5, (CH2)n-SO2R6, (CH2)n-NR7SO2R6, (CH2)n-NR7CONR4R5, (CH2)n-NR7COR7, y (CH2)n-NR7CO2R6, donde cualquier átomo de carbono de metileno individual (CH2) en (CH2)n está opcionalmente sustituido por uno a dos sustituyentes seleccionados independientemente entre flúor, hidroxi. alquilo C1-4, y alcoxi C1-4, donde el alquilo y el alcoxi están opcionalmente sustituidos por uno a cinco átomos de flúor; cada uno de R3a y R3b es independientemente hidrógeno o alquilo C1-4 opcionalmente sustituido por uno a cinco átomos de flúor; cada uno de R4 y R5 se selecciona independientemente entre el grupo que consiste en hidrógeno, (CH2)m-fenilo, (CH2)m-cicloalquilo C3-6, y alquilo C1-6, donde el alquilo está opcionalmente sustituido por uno a cinco sustituyentes seleccionados independientemente entre flúor e hidroxi y donde el fenilo y el cicloalquilo están opcionalmente sustituidos por uno a cinco sustituyentes seleccionados independientemente entre halógeno, hidroxi, alquilo C1-6 y alcoxi C1-6, donde el alquilo y el alcoxi están opcionalmente sustituidos por uno a cinco átomos de flúor; o R4 y R5 junto con el átomo de nitrógeno al que están unidos forman un anillo heterocíclico seleccionado entre azetidina, pirrolidina, piperidina, piperazina, y morfolina donde dicho anillo heterocíclico está opcionalmente sustituido por uno a tres sustituyentes seleccionados independientemente entre halógeno, hidroxi, alquilo C1-6 y alcoxi C1-6, donde el alquilo y el alcoxi están opcionalmente sustituidos por uno a cinco átomos de flúor; cada R6 es independientemente alquilo C1-6, donde el alquilo está opcionalmente sustituido por uno a cinco sustituyentes seleccionados independientemente entre flúor e hidroxilo; R7 es hidrógeno o R6; R8 se selecciona entre el grupo que consiste en: -SO2aIquiIo C1-6, -SO2cicloalquilo C3-6, SO2-ariIo, -SO2-heteroarilo, -C(O)alquilo C1-6, -C(O)cicloalquilo C3-6, -C(O)-arilo, -C(O)-heteroarilo, -C(O)Oalquilo C1-6, -C(O)Ocicloalquilo C3-6, -C(O)O-arilo, -C(O)O-heteroarilo, -C(O)NHalquilo C1-6, -C(O)NHcicloalquilo C3-6, -C(O)NH-arilo, y -C(O)NHheteroarilo; donde el alquilo y el cicloalquilo están opcionalmente sustituidos por uno a cinco átomos de flúor y donde el arilo y el heteroarilo están opcionalmente sustituidos por uno a cinco sustituyentes seleccionados independientemente entre el grupo que consiste en hidroxi, halógeno, ciano, nitro, CO2H, alquiloxi C1-6-carbonilo, alquilo C1-6 y alcoxi C1-6, donde el aIquilo y el alcoxi están opcionalmente sustituidos por uno a cinco átomos de flúor; cada n es independientemente 0, 1, 2, o 3; y cada m es independientemente 0, 1, o 2.
ARP090104318 2008-11-13 2009-11-09 Aminotetrahidropiranos como inhibidores de dipeptidil peptidasa-iv para el tratamiento o prevencion de diabetes AR074306A1 (es)

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US19917908P 2008-11-13 2008-11-13

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AR074306A1 true AR074306A1 (es) 2011-01-05

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US (8) US8143289B2 (es)
EP (4) EP2358717B1 (es)
JP (2) JP4854825B1 (es)
KR (2) KR101260162B1 (es)
CN (1) CN102272136B (es)
AR (1) AR074306A1 (es)
AU (1) AU2009314191B2 (es)
BR (1) BRPI0921375B8 (es)
CA (1) CA2742783C (es)
CL (1) CL2011001082A1 (es)
CO (1) CO6382129A2 (es)
CR (1) CR20110257A (es)
CY (1) CY1114617T1 (es)
DK (1) DK2358717T3 (es)
DO (1) DOP2011000128A (es)
EA (1) EA018613B1 (es)
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ES (1) ES2432191T3 (es)
GE (1) GEP20135724B (es)
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NI (1) NI201100081A (es)
NZ (1) NZ592826A (es)
PA (1) PA8848201A1 (es)
PE (1) PE20120027A1 (es)
PL (1) PL2358717T3 (es)
PT (1) PT2358717E (es)
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SI (1) SI2358717T1 (es)
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