AR099997A1 - 2-AMINO-6-METHYL-4,4a, 5,6-TETRAHYDROPIRANE [3,4-d] [1,3] TIAZIN-8a (8H) -IL-1,3-TIAZOL-4-ILAMIDAS - Google Patents

2-AMINO-6-METHYL-4,4a, 5,6-TETRAHYDROPIRANE [3,4-d] [1,3] TIAZIN-8a (8H) -IL-1,3-TIAZOL-4-ILAMIDAS

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Publication number
AR099997A1
AR099997A1 ARP150101077A ARP150101077A AR099997A1 AR 099997 A1 AR099997 A1 AR 099997A1 AR P150101077 A ARP150101077 A AR P150101077A AR P150101077 A ARP150101077 A AR P150101077A AR 099997 A1 AR099997 A1 AR 099997A1
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Argentina
Prior art keywords
alkyl
cycloalkyl
alkoxy
alkynyl
alkenyl
Prior art date
Application number
ARP150101077A
Other languages
Spanish (es)
Inventor
Alphie Lchapelle Erik
Thomas Oneill Brian
Aaron Brodney Michael
Barreiro Gabriela
Nelsen Rogers Bruce
Ryan Butler Christopher
Mary Beck Elizabeth
Zhang Lei
Original Assignee
Pfizer
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Application filed by Pfizer filed Critical Pfizer
Publication of AR099997A1 publication Critical patent/AR099997A1/en

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Abstract

También composiciones farmacéuticas, métodos de tratamiento, métodos de síntesis e intermediarios. Reivindicación 1: Un compuesto, caracterizado porque tiene la fórmula (1) en donde R¹ se selecciona del grupo que consiste en: fenilo opcionalmente sustituido con uno a tres R²; cicloalquilo C₃₋₉ opcionalmente sustituido con uno a tres R²; y un heteroarilo de 5 a 10 miembros, que tiene uno a cuatro heteroátomos seleccionados, de modo independiente, de N, O ó S, en donde al menos uno de los heteroátomos es N y en donde dicho N está opcionalmente sustituido con R³; y en donde dicho heteroarilo de 5 a 10 miembros está opcionalmente sustituido en el carbono con uno a tres R²; R² en cada aparición está seleccionado, de modo independiente, del grupo que consiste en halógeno, hidroxi, ciano, alquilo C₁₋₆, alcoxi C₁₋₆, alquenilo C₃₋₆, alquenil C₃₋₆-oxi, alquinilo C₃₋₆, alquinil C₃₋₆-oxi, alcoxi C₁₋₆-alquilo C₁₋₆, cicloalcoxi C₃₋₆, cicloalquilo C₃₋₆, cicloalquil C₃₋₆-alquilo C₁₋₆, cicloalquil C₃₋₆-alcoxi C₁₋₆, heterocicloalquilo de 4 a 6 miembros y heterocicloalquil-alquilo C₁₋₆ de 4 a 6 miembros; en donde dicho alquilo C₁₋₆, alcoxi C₁₋₆, alquenilo C₃₋₆, alquenil C₃₋₆-oxi, alquinilo C₃₋₆, alquinil C₃₋₆-oxi, alcoxi C₁₋₆-alquilo C₁₋₆, cicloalcoxi C₃₋₆, cicloalquilo C₃₋₆, cicloalquil C₃₋₆-alquilo C₁₋₆, cicloalquil C₃₋₆-alcoxi C₁₋₆, heterocicloalquilo de 4 a 6 miembros y heterocicloalquil-alquilo C₁₋₆ de 4 a 6 miembros están opcionalmente sustituidos cada uno con uno a tres sustituyentes seleccionados, de modo independiente, de flúor, cloro, hidroxi, ciano, metilo, fluorometilo, difluorometilo, trifluorometilo, metoxi, fluorometoxi, difluorometoxi y trifluorometoxi; o dos R² grupos tomados juntos pueden ser un alquileno C₃₋₅; R³ es hidrógeno, alquilo C₁₋₆, alquenilo C₃₋₆, alquinilo C₃₋₆, alcoxi C₁₋₆-alquilo C₁₋₆, cicloalquilo C₃₋₆, cicloalquil C₃₋₆-alquilo C₁₋₆, heterocicloalquilo de 4 a 6 miembros y heterocicloalquil-alquilo C₁₋₆ de 4 a 6 miembros; en donde dicho alquilo C₁₋₆, alquenilo C₁₋₆, alquinilo C₃₋₆, alcoxi C₁₋₆-alquilo C₁₋₆, cicloalquilo C₁₋₆, cicloalquil C₃₋₆-alquilo C₁₋₆, heterocicloalquilo de 4 a 6 miembros y heterocicloalquil-alquilo C₁₋₆ de 4 a 6 miembros están opcionalmente sustituidos cada uno con uno a tres sustituyentes seleccionados, de modo independiente, de flúor, cloro, hidroxi, ciano, metilo, fluorometilo, difluorometilo, trifluorometilo, metoxi, fluorometoxi, difluorometoxi y trifluorometoxi; o R³ y R² tomados juntos pueden ser un alquileno C₃₋₅; o uno de sus tautómeros o una sal farmacéuticamente aceptable de dicho compuesto o tautómero.Also pharmaceutical compositions, treatment methods, synthesis methods and intermediaries. Claim 1: A compound, characterized in that it has the formula (1) wherein R¹ is selected from the group consisting of: phenyl optionally substituted with one to three R²; C₃₋₉ cycloalkyl optionally substituted with one to three R²; and a 5 to 10 membered heteroaryl, having one to four heteroatoms independently selected from N, O or S, wherein at least one of the heteroatoms is N and wherein said N is optionally substituted with R³; and wherein said 5 to 10 membered heteroaryl is optionally substituted on the carbon with one to three R²; R² at each occurrence is independently selected from the group consisting of halogen, hydroxy, cyano, C₁₋₆ alkyl, C₁₋₆ alkoxy, C₃₋₆ alkenyl, C₃₋₆-oxy alkenyl, C₃₋₆ alkynyl, alkynyl C₃₋₆-oxy, C₁₋₆ alkoxy-Cxi alkyl, C₃₋₆ cycloalkoxy, C₃₋₆ cycloalkyl, C₃₋₆ cycloalkyl, C₃₋₆ cycloalkyl-C₁₋₆ alkoxy, 4 to heterocycloalkyl 6 members and heterocycloalkyl C₁₋₆ alkyl of 4 to 6 members; wherein said C₁₋₆ alkyl, C₁₋₆ alkoxy, C₃₋₆ alkenyl, C₃₋₆-oxy alkenyl, C₃₋₆ alkynyl, C₃₋₆-oxy alkynyl, C₁₋₆ alkoxy-C₁₋₆ alkyl, C₃₋ cycloalkoxy ₆, C₃₋₆ cycloalkyl, C₃₋₆ cycloalkyl-C₁₋₆ alkyl, C₃₋₆ cycloalkyl-C₁₋₆-alkoxy, 4 to 6-membered heterocycloalkyl and C a-4-6-membered heterocycloalkyl are each optionally substituted with one to three substituents independently selected from fluorine, chlorine, hydroxy, cyano, methyl, fluoromethyl, difluoromethyl, trifluoromethyl, methoxy, fluoromethoxy, difluoromethoxy and trifluoromethoxy; or two R² groups taken together may be a C₃₋₅ alkylene; R³ is hydrogen, C₁₋₆ alkyl, C₃₋₆ alkenyl, C₃₋₆ alkynyl, C₁₋₆ alkoxy-C₁₋₆ alkyl, C₃₋₆ cycloalkyl, C₃₋₆ cycloalkyl-C₁₋₆ alkyl, 4-6 membered heterocycloalkyl and 4 to 6-membered heterocycloalkyl-alkyl; wherein said C₁₋₆ alkyl, C₁₋₆ alkenyl, C₃₋₆ alkynyl, C₁₋₆ alkoxy-C₁₋₆ alkyl, C₁₋₆ cycloalkyl, C₃₋₆ cycloalkyl-C₁₋₆ alkyl, 4-6 membered heterocycloalkyl and 4 to 6-membered heterocycloalkyl-alkyl are each optionally substituted with one to three substituents independently selected from fluorine, chloro, hydroxy, cyano, methyl, fluoromethyl, difluoromethyl, trifluoromethyl, methoxy, fluoromethoxy, difluoromethoxy and trifluoromethoxy; or R³ and R² taken together can be a C₃₋₅ alkylene; or one of its tautomers or a pharmaceutically acceptable salt of said compound or tautomer.

ARP150101077A 2014-04-10 2015-04-09 2-AMINO-6-METHYL-4,4a, 5,6-TETRAHYDROPIRANE [3,4-d] [1,3] TIAZIN-8a (8H) -IL-1,3-TIAZOL-4-ILAMIDAS AR099997A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201461977774P 2014-04-10 2014-04-10

Publications (1)

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AR099997A1 true AR099997A1 (en) 2016-08-31

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ARP150101077A AR099997A1 (en) 2014-04-10 2015-04-09 2-AMINO-6-METHYL-4,4a, 5,6-TETRAHYDROPIRANE [3,4-d] [1,3] TIAZIN-8a (8H) -IL-1,3-TIAZOL-4-ILAMIDAS

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AR (1) AR099997A1 (en)

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