AR076687A1 - ISOXAZOLINS AS INHIBITORS OF THE AMIDAHIDROLASA OF FATTY ACIDS AND PHARMACEUTICAL COM-POSITIONS CONTAINING THEM - Google Patents

ISOXAZOLINS AS INHIBITORS OF THE AMIDAHIDROLASA OF FATTY ACIDS AND PHARMACEUTICAL COM-POSITIONS CONTAINING THEM

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Publication number
AR076687A1
AR076687A1 ARP100101710A ARP100101710A AR076687A1 AR 076687 A1 AR076687 A1 AR 076687A1 AR P100101710 A ARP100101710 A AR P100101710A AR P100101710 A ARP100101710 A AR P100101710A AR 076687 A1 AR076687 A1 AR 076687A1
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Argentina
Prior art keywords
nrf
alkyl
nrfre
ore
independently selected
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ARP100101710A
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Spanish (es)
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Infinity Pharmaceuticals Inc
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Publication of AR076687A1 publication Critical patent/AR076687A1/en

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    • 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
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Abstract

La presenten también provee composiciones farmacéuticas que comprenden un compuesto de la formula (1) y un excipiente farmacéuticamente aceptable. Reivindicacion 1: Un compuesto de la formula (1): o una de sus formas farmacéuticamente aceptables, donde: (i) cada uno de Ra, Rb y Rc está seleccionado, de modo independiente, de H, alquilo C1-10 y perhaloalquilo C1-10, Rd es el grupo -L-Z y Z está seleccionado de arilo C6-14: (ii) cada uno de Ra, Rb y Rc está seleccionado, de modo independiente, de -H, alquilo C1-10 y perhaloalquilo C1-10, Rd es el grupo -L-Z y Z está seleccionado de heterociclilo de 3-14 miembros y heteroarilo de 5-14 miembros; (iii) Ra y Rd se unen para formar un carbociclilo C3-10 o anillo fusionado con heterociclilo de 3-14 miembros y Rb y Rc están seleccionados, de modo independiente, de -H, alquilo C1-10 y perhaloalquilo C1-10; o (iv) Rc y Rd se unen para formar un carbociclilo C3-10 o anillo espirofusionado heterociclilo de 3-14 miembros y Ra y Rb están seleccionados, de modo independiente, de -H, alquilo C1-10 y perhaloalquilo C1-10; L es un enlace covalente o un grupo hidrocarbonado C1-6 divalente, donde una, dos o tres unidades de metileno de L están reemplazadas, de manera opcional e independiente, con uno o varios átomos de oxigeno nitrogeno; G está seleccionado de -CN, -NO2, -S(=O)Re, .-SO2Re, -SO2NRfRe, -PO2Re, -PO2ORe, -PO2NRfRe, -(C=O)Re, -(C=O)ORe, -(C=O)NRfRe, -Br, -I, -F, -CI, -ORe, -ONRfRe, -ONRf(C=O)Re, -ONRfSO2Re, -ONRfPO2Re, -ONRfPO2ORe, -SRe, -OSO2Re, -NRfSO2Re, -OPO2Re, -OPO2ORe, -NRfPO2Re, -NRfPO2ORe, -OPO2NRfRe, -O(C=O)Re, -O(C=O)ORe, -NRfRe, -NRf(C=O)Re,-NRf(C=O)ORe, -O(C=O)NRfRe, -NRf(C=NRf)NRfRe, -O(C=NRf)NRfRe, -NRf(C=NRf)ORe, -[N(Rf)2Re]+X- donde X- es un contraion; y cada Re está seleccionado de alquilo C1-10, alquenilo C2-10, alquinilo C2-10, carbociclo C3-10, arilo C6-14, heterociclilo de 3-14 miembros y heteroarilo de 5-14 miembros; cada Rf unido a un átomo de nitrogeno está seleccionado, de modo independiente, de -H, alquilo C1-10 o un grupo protector amino; o Re y Rf se unen para formar un anillo heterociclilo de 3-14 miembros o un anillo heteroarilo de 5-14 miembros.The present also provides pharmaceutical compositions comprising a compound of the formula (1) and a pharmaceutically acceptable excipient. Claim 1: A compound of the formula (1): or one of its pharmaceutically acceptable forms, wherein: (i) each of Ra, Rb and Rc is independently selected from H, C1-10 alkyl and C1 perhaloalkyl -10, Rd is the group -LZ and Z is selected from C6-14 aryl: (ii) each of Ra, Rb and Rc is independently selected from -H, C1-10 alkyl and C1-10 perhaloalkyl , Rd is the group -LZ and Z is selected from 3-14 membered heterocyclyl and 5-14 membered heteroaryl; (iii) Ra and Rd join to form a C3-10 carbocyclyl or 3-14 membered heterocyclyl ring and Rb and Rc are independently selected from -H, C1-10 alkyl and C1-10 perhaloalkyl; or (iv) Rc and Rd are joined to form a C3-10 carbocyclyl or 3-14 membered heterocyclyl spiro fused ring and Ra and Rb are independently selected from -H, C1-10 alkyl and C1-10 perhaloalkyl; L is a covalent bond or a divalent C1-6 hydrocarbon group, where one, two or three methylene units of L are optionally and independently replaced with one or more nitrogen oxygen atoms; G is selected from -CN, -NO2, -S (= O) Re,.-SO2Re, -SO2NRfRe, -PO2Re, -PO2ORe, -PO2NRfRe, - (C = O) Re, - (C = O) ORe, - (C = O) NRfRe, -Br, -I, -F, -CI, -ORe, -ONRfRe, -ONRf (C = O) Re, -ONRfSO2Re, -ONRfPO2Re, -ONRfPO2ORe, -SRe, -OSO2Re, -NRfSO2Re, -OPO2Re, -OPO2ORe, -NRfPO2Re, -NRfPO2ORe, -OPO2NRfRe, -O (C = O) Re, -O (C = O) ORe, -NRfRe, -NRf (C = O) Re, -NRf (C = O) ORe, -O (C = O) NRfRe, -NRf (C = NRf) NRfRe, -O (C = NRf) NRfRe, -NRf (C = NRf) ORe, - [N (Rf) 2Re ] + X- where X- is a counterion; and each Re is selected from C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 carbocycle, C6-14 aryl, 3-14 membered heterocyclyl and 5-14 membered heteroaryl; each Rf attached to a nitrogen atom is independently selected from -H, C1-10 alkyl or an amino protecting group; or Re and Rf join to form a 3-14 membered heterocyclyl ring or a 5-14 membered heteroaryl ring.

ARP100101710A 2009-05-18 2010-05-17 ISOXAZOLINS AS INHIBITORS OF THE AMIDAHIDROLASA OF FATTY ACIDS AND PHARMACEUTICAL COM-POSITIONS CONTAINING THEM AR076687A1 (en)

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US17928309P 2009-05-18 2009-05-18
US17928009P 2009-05-18 2009-05-18
US17928509P 2009-05-18 2009-05-18

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AR076687A1 true AR076687A1 (en) 2011-06-29

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EP (1) EP2432771A4 (en)
JP (1) JP2012527467A (en)
KR (1) KR20120042766A (en)
CN (1) CN102459202B (en)
AR (1) AR076687A1 (en)
AU (1) AU2010249674A1 (en)
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