AR107556A1 - DERIVATIVES OF HALOALILAMINE INDOL AND AZAINDOL AS INHIBITORS OF LISIL OXIDASES AND USES OF THE SAME - Google Patents

DERIVATIVES OF HALOALILAMINE INDOL AND AZAINDOL AS INHIBITORS OF LISIL OXIDASES AND USES OF THE SAME

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Publication number
AR107556A1
AR107556A1 ARP170100307A ARP170100307A AR107556A1 AR 107556 A1 AR107556 A1 AR 107556A1 AR P170100307 A ARP170100307 A AR P170100307A AR P170100307 A ARP170100307 A AR P170100307A AR 107556 A1 AR107556 A1 AR 107556A1
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AR
Argentina
Prior art keywords
6alkyl
3alkyl
group
halogen
optionally substituted
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ARP170100307A
Other languages
Spanish (es)
Inventor
Alan Duncan Robertson
Wenbin Zhou
Wolfgang Jarolimek
Jonathan Stuart Foot
Mandar Deodhar
Craig Ivan Turner
Alison Dorothy Findlay
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Pharmaxis Ltd
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Publication date
Priority claimed from AU2016900478A external-priority patent/AU2016900478A0/en
Application filed by Pharmaxis Ltd filed Critical Pharmaxis Ltd
Publication of AR107556A1 publication Critical patent/AR107556A1/en

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Abstract

Compuestos capaces de inhibir determinadas enzimas amina oxidasas. Estos compuestos son útiles para el tratamiento de una variedad de indicaciones, por ejemplo, de la fibrosis, el cáncer y/o la angiogénesis en sujetos humanos, en animales domésticos y ganado. Además, se describen composiciones farmacéuticas que contienen estos compuestos y distintos usos de las mismas. Reivindicación 1: Un compuesto de fórmula (1), o un estereoisómero, sal farmacéuticamente aceptable, forma polimórfica, solvato, forma tautomérica o profármaco del mismo; donde: a es N o CR³; b es N o CR⁴; c es N o CR⁵; d es N o CR⁶; y entre 0 y 2 de a, b, c y d son N; R¹ se selecciona entre el grupo que consiste en hidrógeno, halógeno, C₁₋₆alquilo, C₃₋₇cicloalquilo, -O-C₁₋₆alquilo, -O-C₃₋₇cicloalquilo, -C(O)OR⁸, -C(O)NR⁹R¹⁰ y -NR⁹C(O)R¹¹; donde cada C₁₋₆alquilo es un alquilo de cadena lineal o ramificada; y donde cada C₁₋₆alquilo y C₃₋₇cicloalquilo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halógeno, -OH, -SH, -C₁₋₃alquilo, -O-C₁₋₃alquilo, -CF₃, CH₂CF₃, y -O-CF₃; R² es arilo o heteroarilo; donde cada R² está opcionalmente sustituido con uno o más R¹²; R³, R⁴, R⁵ y R⁶ se seleccionan en forma independiente entre sí entre el grupo que consiste en hidrógeno, halógeno, hidroxilo, C₁₋₆alquilo, C₃₋₇cicloalquilo, -O-C₁₋₆alquilo, -O-C₃₋₇cicloalquilo, -CN, -NO₂, -NR⁹R¹⁰, -C(O)OR⁸, -C(O)NR⁹R¹⁰, -NR⁹C(O)R¹¹, -S(O₂)NR⁹R¹⁰, -NR⁹S(O₂)R¹¹, -S(O)R¹¹, -S(O₂)R¹¹, tetrazol y oxadiazol; donde cada C₁₋₆alquilo es un alquilo de cadena lineal o ramificada; y donde cada C₁₋₆alquilo y C₃₋₇cicloalquilo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halógeno, -OH, -SH, -C₁₋₃alquilo, -O-C₁₋₃alquilo, -CF₃, -CH₂CF₃, y -O-CF₃; R⁸ se selecciona entre el grupo que consiste en hidrógeno, C₁₋₆alquilo, y C₃₋₇cicloalquilo; donde cada C₁₋₆alquilo es un alquilo de cadena lineal o ramificada; y donde cada C₁₋₆alquilo y C₃₋₇cicloalquilo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halógeno, -OH, -SH, -C₁₋₃alquilo, -O-C₁₋₃alquilo, -CF₃, -CH₂CF₃, y -O-CF₃; R⁹ y R¹⁰ se seleccionan en forma independiente entre el grupo que consiste en hidrógeno, C₁₋₆alquilo y C₃₋₇cicloalquilo; donde cada C₁₋₆alquilo es un alquilo de cadena lineal o ramificada; y donde cada C₁₋₆alquilo y C₃₋₇cicloalquilo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halógeno, -OH, -SH, -C₁₋₃alquilo, -O-C₁₋₃alquilo, -CF₃, CH₂CF₃, y -O-CF₃; o R⁹ y R¹⁰ cuando se unen al mismo átomo de nitrógeno se combinan para formar un anillo de entre 3 y 7 miembros que tiene entre 0 y 2 heteroátomos adicionales como miembros del anillo; R¹¹ se selecciona entre el grupo que consiste en C₁₋₆alquilo y C₃₋₇cicloalquilo; donde cada C₁₋₆alquilo es un alquilo de cadena lineal o ramificada; y donde cada C₁₋₆alquilo y C₃₋₇cicloalquilo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halógeno, -OH, -SH, -C₁₋₃alquilo, -O-C₁₋₃alquilo, -CF₃, -CH₂CF₃, y -O-CF₃; y R¹² se selecciona entre el grupo que consiste en halógeno, C₁₋₆alquilo, -O-C₁₋₆alquilo, -S-C₁₋₆alquilo, C₃₋₇cicloalquilo, -O-C₃₋₇cicloalquilo, -C(O)OR⁸, -C(O)NR⁹R¹⁰, -NR⁹C(O)R¹¹, -S(O₂)NR⁹R¹⁰, -NR⁹S(O₂)R¹¹, -S(O)R¹¹ y -S(O₂)R¹¹; donde cada C₁₋₆alquilo es un alquilo de cadena lineal o ramificada; y donde cada C₁₋₆alquilo y C₃₋₇cicloalquilo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halógeno, -OH, -C₁₋₃alquilo, -O-C₁₋₃alquilo, -CF₃, -CH₂CF₃, y -O-CF₃.Compounds capable of inhibiting certain amine oxidases enzymes. These compounds are useful for the treatment of a variety of indications, for example, of fibrosis, cancer and / or angiogenesis in human subjects, in domestic animals and livestock. In addition, pharmaceutical compositions containing these compounds and different uses thereof are described. Claim 1: A compound of formula (1), or a stereoisomer, pharmaceutically acceptable salt, polymorphic form, solvate, tautomeric form or prodrug thereof; where: a is N or CR³; b is N or CR⁴; c is N or CR⁵; d is N or CR⁶; and between 0 and 2 of a, b, c and d are N; R¹ is selected from the group consisting of hydrogen, halogen, C₁₋₆alkyl, C₃₋₇cycloalkyl, -O-C₁₋₆alkyl, -O-C₃₋₇cycloalkyl, -C (O) OR⁸, -C (O) NR⁹R¹⁰ and - NR⁹C (O) R¹¹; where each C₁₋₆alkyl is a straight or branched chain alkyl; and wherein each C₁₋₆alkyl and C₃₋₇cycloalkyl is optionally substituted with one or more substituents selected from the group consisting of halogen, -OH, -SH, -C₁₋₃alkyl, -O-C₁₋₃alkyl, -CF₃, CH₂CF₃, and -O-CF₃; R² is aryl or heteroaryl; where each R² is optionally substituted with one or more R¹²; R³, R⁴, R⁵ and R⁶ are independently selected from each other from the group consisting of hydrogen, halogen, hydroxyl, C₁₋₆alkyl, C₃₋₇cycloalkyl, -O-C₁₋₆alkyl, -O-C₃₋₇cycloalkyl, -CN , -NO₂, -NR⁹R¹⁰, -C (O) OR⁸, -C (O) NR⁹R¹⁰, -NR⁹C (O) R¹¹, -S (O₂) NR⁹R¹⁰, -NR⁹S (O₂) R¹¹, -S (O) R¹¹, - S (O₂) R¹¹, tetrazol and oxadiazole; where each C₁₋₆alkyl is a straight or branched chain alkyl; and wherein each C₁₋₆alkyl and C₃₋₇cycloalkyl is optionally substituted with one or more substituents selected from the group consisting of halogen, -OH, -SH, -C₁₋₃alkyl, -O-C₁₋₃alkyl, -CF₃, -CH₂CF₃ , and -O-CF₃; R⁸ is selected from the group consisting of hydrogen, C₁₋₆alkyl, and C₃₋₇cycloalkyl; where each C₁₋₆alkyl is a straight or branched chain alkyl; and wherein each C₁₋₆alkyl and C₃₋₇cycloalkyl is optionally substituted with one or more substituents selected from the group consisting of halogen, -OH, -SH, -C₁₋₃alkyl, -O-C₁₋₃alkyl, -CF₃, -CH₂CF₃ , and -O-CF₃; R⁹ and R¹⁰ are independently selected from the group consisting of hydrogen, C₁₋₆alkyl and C₃₋₇cycloalkyl; where each C₁₋₆alkyl is a straight or branched chain alkyl; and wherein each C₁₋₆alkyl and C₃₋₇cycloalkyl is optionally substituted with one or more substituents selected from the group consisting of halogen, -OH, -SH, -C₁₋₃alkyl, -O-C₁₋₃alkyl, -CF₃, CH₂CF₃, and -O-CF₃; or R⁹ and R¹⁰ when attached to the same nitrogen atom combine to form a ring of between 3 and 7 members that has between 0 and 2 additional heteroatoms as ring members; R¹¹ is selected from the group consisting of C₁₋₆alkyl and C₃₋₇cycloalkyl; where each C₁₋₆alkyl is a straight or branched chain alkyl; and wherein each C₁₋₆alkyl and C₃₋₇cycloalkyl is optionally substituted with one or more substituents selected from the group consisting of halogen, -OH, -SH, -C₁₋₃alkyl, -O-C₁₋₃alkyl, -CF₃, -CH₂CF₃ , and -O-CF₃; and R¹² is selected from the group consisting of halogen, C₁₋₆alkyl, -O-C₁₋₆alkyl, -S-C₁₋₆alkyl, C₃₋₇cycloalkyl, -O-C₃₋₇cycloalkyl, -C (O) OR⁸, -C (O) NR⁹R¹⁰, -NR⁹C (O) R¹¹, -S (O₂) NR⁹R¹⁰, -NR⁹S (O₂) R¹¹, -S (O) R¹¹ and -S (O₂) R¹¹; where each C₁₋₆alkyl is a straight or branched chain alkyl; and wherein each C₁₋₆alkyl and C₃₋₇cycloalkyl is optionally substituted with one or more substituents selected from the group consisting of halogen, -OH, -C₁₋₃alkyl, -O-C₁₋₃alkyl, -CF₃, -CH₂CF₃, and - O-CF₃.

ARP170100307A 2016-02-12 2017-02-07 DERIVATIVES OF HALOALILAMINE INDOL AND AZAINDOL AS INHIBITORS OF LISIL OXIDASES AND USES OF THE SAME AR107556A1 (en)

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AU2016900478A AU2016900478A0 (en) 2016-02-12 Haloallylamine indole and azaindole derivative inhibitors of lysyl oxidases and uses thereof

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AR107556A1 true AR107556A1 (en) 2018-05-09

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ARP170100307A AR107556A1 (en) 2016-02-12 2017-02-07 DERIVATIVES OF HALOALILAMINE INDOL AND AZAINDOL AS INHIBITORS OF LISIL OXIDASES AND USES OF THE SAME

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