AR071387A1 - Pirimidin-5-carboxamidas sustituidas - Google Patents

Pirimidin-5-carboxamidas sustituidas

Info

Publication number
AR071387A1
AR071387A1 ARP090101395A ARP090101395A AR071387A1 AR 071387 A1 AR071387 A1 AR 071387A1 AR P090101395 A ARP090101395 A AR P090101395A AR P090101395 A ARP090101395 A AR P090101395A AR 071387 A1 AR071387 A1 AR 071387A1
Authority
AR
Argentina
Prior art keywords
independently selected
optionally substituted
alkyl
halo
cyano
Prior art date
Application number
ARP090101395A
Other languages
English (en)
Original Assignee
Astrazeneca Ab
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40810517&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR071387(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR071387A1 publication Critical patent/AR071387A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P3/06—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
    • 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
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/38—One sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/557—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms, e.g. orotic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/58—Two sulfur 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
    • C07D401/14—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
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

También se describen su uso en la inhibicion de 11bHSD1, procedimientos para prepararlos y composiciones farmacéuticas que los comprenden. Reivindicacion 1: Un compuesto de formula (1) en el que: Q es O, S, N(R8) o un enlace sencillo; R8 se selecciona entre hidrogeno, alquilo C1-4, cicloalquilo C3-5 y cicloalquilmetilo C3-5 (estando cada uno opcionalmente sustituido con 1, 2 o 3 átomos de fluor); R1 se selecciona entre alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, heterociclilo, heteroarilo, arilo, arilalquilo C1-3, heteroarilalquilo C1-3, cicloalquil C3-7-alquilo C1-3, heterociclilalquilo C1-3, cicloalquil C3-7-alquenilo C2-3 y cicloalquil C3-7-alquinilo C2-3, [estando cada uno opcionalmente sustituido, en átomos de carbono disponibles, con 1, 2 o 3 sustituyentes seleccionados independientemente entre alquilo C1-3, hidroxi, halo, oxo, ciano, trifluorometilo, alcoxi C1-3, alquil C1-3-S(O)n- (donde n es 0, 1, 2 o 3), R5CON(R5')-, (R5')(R5'')N-, (R5')(R5'')NC(O)-, R5'C(O)O-, R5'OC(O)-, (R5')(R5'')NC(O)N(R5''')-, R5SO2N(R5'')-, (R5')(R5'')NSO2- y alquilo C1-2 opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente entre hidroxi, halo, carboxi y alcoxi C1-3 (donde R5 es alquilo C1-3 opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente entre hidroxilo, halo y ciano; y R5', R5'' y R5''' se seleccionan independientemente entre hidrogeno y alquilo C1-3 opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente entre hidroxilo, halo, alcoxi C1-3, carboxi y ciano, o R5' y R5'' junto con el átomo de nitrogeno al que están unidos forman un anillo saturado de 4-7 miembros) y opcionalmente sustituido, en un nitrogeno disponible, con un sustituyente seleccionado independientemente entre alquilo C1-4, alcanoilo C2-4, y alcanosulfonilo C1-4, estando cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente entre hidroxilo, halo, alcoxi C1-4, carboxi y ciano]; o R1 y R8 junto con el átomo de nitrogeno al que están unidos forman un sistema de anillos saturados, mono, bicíclicos o enlazados, que contiene opcionalmente 1 o 2 heteroátomos adicionales en el anillo seleccionados independientemente entre nitrogeno, oxígeno y azufre y opcionalmente condensado con un anillo monocíclico saturado, parcialmente saturado o insaturado, donde el sistema de anillos resultante está opcionalmente sustituido, en átomos de carbono disponibles, con 1, 2 o 3 sustituyentes seleccionados independientemente entre R9 y opcionalmente sustituido, en un nitrogeno disponible, con un sustituyente seleccionado independientemente entre alquilo C1-4, alcanoilo C2-4 y alcanosulfonilo C1-4, estando cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente entre hidroxilo, halo, alcoxi C1-4, carboxi y ciano; R2 se selecciona entre cicloalquil C3-7-(CH2)m- y policicloalquil C6-12-(CH2)m- (donde m es 0, 1 o 2 y los anillos contienen opcionalmente 1 o 2 átomos en el anillo seleccionados independientemente entre nitrogeno, oxígeno y azufre y están opcionalmente sustituidos, en átomos de carbono disponibles, con 1, 2 o 3 sustituyentes seleccionados independientemente entre R6 y opcionalmente sustituidos, en un nitrogeno disponible, con un sustituyente seleccionado independientemente entre alquilo C1-4, alcanoílo C2-4 y alcanosulfonilo C1-4, estando cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente entre hidroxilo, halo, alcoxi C1-4, carboxi y ciano); R3 se selecciona entre hidrogeno, alquilo C1-4, cicloalquilo C3-5 y cicloalquilmetilo C3-5 (estando cada uno opcionalmente sustituido con 1, 2 o 3 átomos de fluor); R2 y R3 junto con el átomo de nitrogeno al que están unidos forman un sistema de anillos saturados, mono, bicíclicos o enlazados, que contiene opcionalmente 1 o 2 heteroátomos adicionales en el anillo seleccionados independientemente entre nitrogeno, oxígeno y azufre y opcionalmente condensado con un anillo monocíclico saturado, parcialmente saturado o insaturado, donde el sistema de anillos resultante está opcionalmente sustituido, en átomos de carbono disponibles, con 1, 2 o 3 sustituyentes seleccionados independientemente entre R7 y opcionalmente sustituido, en un nitrogeno disponible, con un sustituyente seleccionado independientemente entre alquilo C1-4, alcanoílo C2-4 y alcanosulfonilo C1-4, estando cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente entre hidroxilo, halo, alcoxi C1-4, carboxi y ciano; R4 se selecciona entre hidrogeno, R10, -OR10, -SR10 y-NR11R12; R10 se selecciona entre alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, heterociclilo, arilalquilo C1-3, heteroarilalquilo C1-3, heterociclilalquilo C1-3, cicloalquil C3-7-alquilo C1-3, cicloalquil C3-7-alquenilo C2-3 y cicloalquil C3-7-alquinilo C2-3, [estando cada uno opcionalmente sustituido, en átomos de carbono disponibles, con 1, 2 o 3 sustituyentes seleccionados independientemente entre alquilo C1-3, hidroxi, halo, oxo, ciano, trifluorometilo, alcoxi C1-3, alquil C1-3-S(O)p- (donde p es 0, 1, 2 o 3), R13CON(R13')-, (R13')(R13'')N-, (R13')(R13'')NC(O)-, R13'C(O)O-, R13'OC(O)-, (R13')(R13'')NC(O)N(R13''')-, R13SO2N(R13'')-, (R13')(R13'')NSO2- y alquilo C1-2 opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente entre hidroxi, halo, carboxi y alcoxi C1-3 (donde R13 es alquilo C1-3 opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados entre hidroxilo, halo y ciano; y R13', R13'' y R13''' se seleccionan independientemente entre hidrogeno y alquilo C1-3 opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente entre hidroxilo, halo, alcoxi C1-3, carboxi y ciano, o R13' y R13'' junto con el átomo de nitrogeno al que están unidos forman un anillo saturado de 4-7 miembros) y opcionalmente sustituido, en un nitrogeno disponible, con un sustituyente seleccionado independientemente entre alquilo C1-4, alcanoílo C2-4 y alcanosulfonilo C1-4, estando cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente entre hidroxilo, halo, alcoxi C1-4, carboxi y ciano]; R11 se selecciona entre hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, heterociclilo, arilalquilo C1-3, heteroarilalquilo C1-3, heterociclilalquilo C1-3, cicloalquil C3-7-alquilo C1-3, cicloalquil C3-7-alquenilo C2-3 y cicloalquil C3-7-alquinilo C2-3, [estando cada uno opcionalmente sustituido, en átomos de carbono disponibles, con 1, 2 o 3 sustituyentes seleccionados independientemente entre alquilo C1-3, hidroxi, halo, oxo, ciano, trifluorometilo, alcoxi C1-3, alquil C1-3-S(O)q- (donde q es 0, 1, 2 o 3), R14CON(R14')-, (R14')(R14'')NC(O)-, R14'C(O)O-, R14'OC(O)-, (R14')(R14'')NC(O)N(R14''')-, R14SO2N(R14'')-, (R14')(R14'')NSO2- y alquilo C1-2 opcionalmente sustituido con 1, 2 o 3, sustituyentes seleccionados independientemente entre hidroxi, halo, carboxi y alcoxi C1-3 (donde R14 es alquilo C1-3 opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente entre hidroxilo, halo y ciano; y R14', R14'' y R14''' se seleccionan independientemente entre hidrogeno y alquilo C1-3 opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente entre hidroxilo, halo, alcoxi C1-3, carboxi y ciano, o R14' y R14'' junto con el átomo de nitrogeno al que están unidos forman un anillo saturado de 4-7 miembros) y opcionalmente sustituido, en un nitrogeno disponible, con un sustituyente seleccionado independientemente entre alquilo C1-4, alcanoílo C1-4 y alcanosulfonilo C1-4, estando cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente entre hidroxilo, halo, alcoxi C1-4, carboxi y ciano]; y R12 se selecciona entre hidrogeno, alquilo C1-4, cicloalquilo C3-5 y cicloalquilmetilo C3-5 (estando cada uno opcionalmente sustituido con 1, 2 o 3 átomos de fluor); o R11 y R12 junto con el átomo de nitrogeno al que están unidos forman un sistema de anillos saturados, mono, bicíclicos o enlazados, que contiene opcionalmente 1 o 2 heteroátomos adicionales en el anillo seleccionados independientemente entre nitrogeno, oxígeno y azufre y opcionalmente condensado con un anillo monocíclico saturado, parcialmente saturado o insaturado (que contiene opcionalmente 1 o 2 heteroátomos adicionales en el anillo seleccionados independientemente entre nitrogeno, oxígeno y azufre), donde el sistema de anillos resultante está opcionalmente sustituido, en átomos de carbono disponibles, con 1, 2 o 3 sustituyentes seleccionados independientemente entre R15 y opcionalmente sustituido en un nitrogeno disponible con un sustituyente seleccionado independientemente entre alquilo C1-4, alcanoílo C2-4 y alcanosulfonilo C1-4, estando cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente entre hidroxilo, halo, alcoxi C1-4, carboxi y ciano; R6, R7, R9 y R15 se seleccionan independientemente entre hidroxilo, halo, oxo, carboxi, ciano, trifluorometilo, R16, R16O-, R16CO-, R16C(O)O-, R16CON(R16')-, (R16')(R16'')NC(O), (R16')(R16'')N, R16S(O)a- donde a es de 0 a 2, R16'OC(O)-, (R16')(R16'')NSO2-, R16SO2N(R16'')-, (R16')(R16'')NC(O)N(R16''')-, fenilo y heteroarilo [donde los grupos fenilo y heteroarilo están opcionalmente condensados con un fenilo, heteroarilo o un anillo de 5 o 6 miembros, saturado o parcialmente saturado, que contiene opcionalmente 1, 2 o 3 heteroátomos seleccionados independientemente entre nitrogeno, oxígeno y azufre y el sistema de anillos resultante está opcionalmente sustituido, en átomos de carbono disponibles, con 1, 2 o 3 sustituyentes seleccionados independientemente entre alquilo C1-4, hidroxilo, ciano, trifluorometilo, trifluorometoxi, halo, alcoxi C1-4, alcoxi C1-4-alquilo C1-4, amino, N-alquilamino C1-4, di-N,N-(alquil C1-4)amino, N-alquilcarbamo
ARP090101395A 2008-04-22 2009-04-21 Pirimidin-5-carboxamidas sustituidas AR071387A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US4683608P 2008-04-22 2008-04-22
US14020108P 2008-12-23 2008-12-23

Publications (1)

Publication Number Publication Date
AR071387A1 true AR071387A1 (es) 2010-06-16

Family

ID=40810517

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090101395A AR071387A1 (es) 2008-04-22 2009-04-21 Pirimidin-5-carboxamidas sustituidas

Country Status (24)

Country Link
US (1) US20090264401A1 (es)
EP (1) EP2271629A1 (es)
JP (1) JP2011518216A (es)
KR (1) KR20110002475A (es)
CN (1) CN102066335A (es)
AR (1) AR071387A1 (es)
AU (1) AU2009239794A1 (es)
BR (1) BRPI0910734A2 (es)
CA (1) CA2719936A1 (es)
CL (1) CL2009000967A1 (es)
CO (1) CO6321254A2 (es)
CR (1) CR11750A (es)
DO (1) DOP2010000323A (es)
EA (1) EA201001669A1 (es)
EC (1) ECSP10010561A (es)
IL (1) IL208405A0 (es)
MX (1) MX2010011591A (es)
NI (1) NI201000179A (es)
PE (1) PE20091810A1 (es)
SV (1) SV2010003713A (es)
TW (1) TW200948789A (es)
UY (1) UY31774A (es)
WO (1) WO2009130496A1 (es)
ZA (1) ZA201006993B (es)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007058346A1 (ja) 2005-11-21 2007-05-24 Shionogi & Co., Ltd. I型11βヒドロキシステロイド脱水素酵素阻害活性を有するヘテロ環化合物
TW200827346A (en) 2006-11-03 2008-07-01 Astrazeneca Ab Chemical compounds
TW200836719A (en) 2007-02-12 2008-09-16 Astrazeneca Ab Chemical compounds
KR101376432B1 (ko) 2007-05-18 2014-05-16 시오노기세이야쿠가부시키가이샤 １１β-하이드록시스테로이드 탈수소효소 유형 １ 저해 활성을 갖는 질소-함유 헤테로환형 유도체
US7951833B2 (en) * 2008-02-04 2011-05-31 Astrazeneca Ab Crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]Benzoic acid 471
TW201118085A (en) * 2009-10-20 2011-06-01 Astrazeneca Ab Adamantyl iminocarbonyl-substituted pyrimidines as inhibitors of 11-β-HSD1
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
CN105001165B (zh) 2011-04-22 2020-06-23 西格诺药品有限公司 取代的二氨基嘧啶其组合物，和用其治疗的方法
EP2735567B1 (en) * 2011-07-21 2016-10-26 Xuanzhu Pharma Co., Ltd. Heterocyclic substituted pyrimidine compound
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
EP2760862B1 (en) 2011-09-27 2015-10-21 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013113716A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
CN104302620A (zh) 2012-04-26 2015-01-21 弗朗西斯·泽维尔·塔瓦雷斯 内酰胺的合成
US10093631B2 (en) 2014-02-14 2018-10-09 Acquist Llc Bifunctional compounds and use for reducing uric acid levels
TWI744723B (zh) * 2014-06-20 2021-11-01 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
WO2016118611A1 (en) 2015-01-22 2016-07-28 Warrell Raymond P Jr Bifunctional compounds and use for reducing uric acid levels
CN104592131A (zh) * 2015-02-11 2015-05-06 佛山市赛维斯医药科技有限公司 含嘧啶结构的对称环己烷羧酸苄基酰胺类化合物及用途
CN104649980A (zh) * 2015-02-11 2015-05-27 佛山市赛维斯医药科技有限公司 含嘧啶结构的对称环己烷羧酸酰胺类sglt2/sglt1双靶点抑制剂、制备方法及用途
CN104649981A (zh) * 2015-02-11 2015-05-27 佛山市赛维斯医药科技有限公司 一种含嘧啶结构的对称环己烷羧酸苄基酰胺类双靶点抑制剂、制备方法及用途
CN104628656A (zh) * 2015-02-11 2015-05-20 佛山市赛维斯医药科技有限公司 一类含嘧啶结构的对称环己烷羧酸酰胺类双靶点抑制剂及用途
EP3235813A1 (en) 2016-04-19 2017-10-25 Cidqo 2012, S.L. Aza-tetra-cyclo derivatives
TWI771303B (zh) 2016-06-30 2022-07-21 美商艾克奎斯特有限責任公司 化合物及其於降低尿酸位準之用途(一)
BR112018077155A2 (pt) 2016-07-01 2019-04-02 G1 Therapeutics, Inc. processo para preparar um composto, e, composto
EP3481819B1 (en) 2016-07-06 2022-06-01 Acquist LLC Compounds and their use for reducing uric acid levels
US11548893B2 (en) 2017-07-15 2023-01-10 Arisan Therapeutics Inc. Enantiomerically pure adamantane carboxamides for the treatment of filovirus infection
CN112839657A (zh) 2018-08-24 2021-05-25 G1治疗公司 1,4-二氮杂螺[5.5]十一烷-3-酮改进的合成
TW202130623A (zh) * 2019-12-02 2021-08-16 美商富曼西公司 用於合成2-硫烷嘧啶的製程
MX2023003446A (es) * 2020-09-25 2023-06-22 Shanghai Meiyue Biotech Dev Co Ltd Compuesto de pirimidina carboxamida y aplicación del mismo.
CN115141147B (zh) * 2022-08-24 2023-09-12 绍兴上虞新银邦生化有限公司 一种n-甲基-3-取代甲基-4-吡唑甲酰胺衍生物的合成方法

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GR66581B (es) * 1978-02-21 1981-03-27 Delalande Sa
FR2631028B1 (fr) * 1988-05-09 1990-07-13 Cird Adamantyl-2 isothiazoline-4 ones-3, leur procede de preparation et leur utilisation comme agents bactericides et fongicides
DE69304453T2 (de) * 1992-07-07 1997-02-06 Kyowa Hakko Kogyo Kk Pyridin-Derivate und diese enthaltende pharmazeutische Zubereitungen
EP1223170B1 (en) * 1999-10-12 2005-12-28 Takeda Pharmaceutical Company Limited Pyrimidine-5-carboxamide compounds, process for producing the same and use thereof
US7273868B2 (en) * 2000-04-28 2007-09-25 Tanabe Seiyaku Co., Ltd. Pyrazine derivatives
DE10023492A1 (de) * 2000-05-09 2001-11-22 Schering Ag Aza- und Polyazanthranylamide und deren Verwendung als Arzneimittel
JP4178816B2 (ja) * 2001-03-15 2008-11-12 田辺三菱製薬株式会社 医薬組成物
US20040067985A1 (en) * 2002-10-04 2004-04-08 Fortuna Haviv Method of inhibiting angiogenesis
ATE467616T1 (de) * 2003-04-11 2010-05-15 High Point Pharmaceuticals Llc Verbindungen mit aktivität an der 11beta- hydroxasteroiddehydrogenase
US7459460B2 (en) * 2003-05-28 2008-12-02 Bristol-Myers Squibb Company Trisubstituted heteroaromatic compounds as calcium sensing receptor modulators
JP2008519034A (ja) * 2004-11-03 2008-06-05 バーテックス ファーマシューティカルズ インコーポレイテッド イオンチャネル調節剤としてのピリミジン誘導体および使用方法
EP1879881A2 (en) * 2005-04-14 2008-01-23 Bristol-Myers Squibb Company Inhibitors of 11-beta hydroxysteroid dehydrogenase type i
US20100022589A1 (en) * 2006-07-27 2010-01-28 Mccoull William Pyridine-3-carboxamide compounds and their use for inhibiting 11-beta-hydroxysteroid dehydrogenase
TW200827346A (en) * 2006-11-03 2008-07-01 Astrazeneca Ab Chemical compounds
TW200836719A (en) * 2007-02-12 2008-09-16 Astrazeneca Ab Chemical compounds
EP2202228B1 (en) * 2007-10-15 2014-12-10 Takeda Pharmaceutical Company Limited Amide compounds and use of the same
AU2008326226B2 (en) * 2007-11-06 2011-10-20 Astrazeneca Ab 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid - 465
US7951833B2 (en) * 2008-02-04 2011-05-31 Astrazeneca Ab Crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]Benzoic acid 471
TW201118085A (en) * 2009-10-20 2011-06-01 Astrazeneca Ab Adamantyl iminocarbonyl-substituted pyrimidines as inhibitors of 11-β-HSD1

Also Published As

Publication number Publication date
CL2009000967A1 (es) 2010-06-11
DOP2010000323A (es) 2010-12-15
CR11750A (es) 2010-12-15
WO2009130496A1 (en) 2009-10-29
BRPI0910734A2 (pt) 2015-09-29
NI201000179A (es) 2011-12-15
ZA201006993B (en) 2012-03-28
CO6321254A2 (es) 2011-09-20
EA201001669A1 (ru) 2011-06-30
US20090264401A1 (en) 2009-10-22
AU2009239794A1 (en) 2009-10-29
MX2010011591A (es) 2010-11-09
TW200948789A (en) 2009-12-01
UY31774A (es) 2009-12-14
JP2011518216A (ja) 2011-06-23
SV2010003713A (es) 2011-02-17
ECSP10010561A (es) 2010-11-30
CN102066335A (zh) 2011-05-18
IL208405A0 (en) 2010-12-30
CA2719936A1 (en) 2009-10-29
PE20091810A1 (es) 2009-12-23
EP2271629A1 (en) 2011-01-12
KR20110002475A (ko) 2011-01-07

Similar Documents

Publication Publication Date Title
AR071387A1 (es) Pirimidin-5-carboxamidas sustituidas
AR065300A1 (es) Compuestos quimicos derivados de 1,2-pirazol
BRPI0619255B8 (pt) composto de peptídeo, composição farmacêutica, uso do composto e medicamento para imunoterapia de câncer
CO6321130A2 (es) Piridinas carboxamidas como inhibidores de la 11 beta-hsd1
AR059687A1 (es) Derivados de pirazol inhibidores de la enzima mao-b,utiles para mejorar la funcion cognitiva, composiciones farmaceuticas que los contienen,y metodo de preparacion.
AR061923A1 (es) Compuestos derivados de benzofuran-piperidina
BRPI0707491B8 (pt) compostos úteis como agentes moduladores de receptores de mineralocorticóides, os referidos agentes compreendendo os mesmos e composições farmacêuticas
RU2010102229A (ru) Производные бензазепина, пригодные для использования в качестве антагонистов вазопрессина
AR057769A1 (es) Pirazolo pirimidinas como inhibidores de map quinasa p38, metodos para utilizarlos y composiciones farmaceuticas
AR069509A1 (es) Pirido (3,2-e) pirazinas, su procedimiento de preparacion y uso como inhibidores de fosfodiesterasa 10
AR011093A1 (es) Compuestos derivados de sulfonil urea, composicion farmaceutica que los contiene y procedimiento para su uso.
AR057987A1 (es) Compuestos agonistas de cb1 (receptor cannabinoide)
AR044134A1 (es) Derivados de quinuclidina, metodo de preparacion y composiciones farmaceuticas.
WO2008007113A3 (en) Pharmaceutical combinations
BRPI0818193B8 (pt) composto, composição farmacêutica, e, uso de um composto
AR060050A1 (es) Compuestos moduladores del receptor de s1p y uso de los mismos
AR057072A1 (es) Compuestos quimicos derivados de 2-azetidinona, formulacion farmaceutica y un proceso de preparacion del compuesto
AR060623A1 (es) Compuestos derivados de 2-azetidinona y un metodo de preparacion
BRPI0506858A (pt) composto, métodos de preparação de monoidrato de gaboxadol cristalino e de anidrato de gaboxadol cristalino, composição farmacêutica, e, uso de um composto
AR071300A1 (es) Compuestos; composiciones farmaceuticas en base al compuesto y uso del mismo para la manufactura de un medicamento
RS51462B (en) TRIAZOLOPYRIDINE CARBOXAMID DERIVATIVES, THEIR PREPARATION AND THERAPEUTIC APPLICATION
AR070345A1 (es) (dihidro ) pirrolo (2,1-a) isoquinolinas
AR070801A1 (es) Derivados pirimidin -piridina
AR045979A1 (es) Amidas heterociclicas
MX2008016558A (es) Preparacion y aplicacion terapéutica de derivados de 2-benzoil-imidazopiridinas.

Legal Events

Date Code Title Description
FA Abandonment or withdrawal