PE20210398A1 - Benzofurano, benzopirrol, benzotiofeno sustituidos y otros inhibidores del complemento estructuralmente relacionados - Google Patents

Benzofurano, benzopirrol, benzotiofeno sustituidos y otros inhibidores del complemento estructuralmente relacionados

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Publication number
PE20210398A1
PE20210398A1 PE2020001534A PE2020001534A PE20210398A1 PE 20210398 A1 PE20210398 A1 PE 20210398A1 PE 2020001534 A PE2020001534 A PE 2020001534A PE 2020001534 A PE2020001534 A PE 2020001534A PE 20210398 A1 PE20210398 A1 PE 20210398A1
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PE
Peru
Prior art keywords
alkyl
cycloalkyl
heterocycloalkyl
aryl
halogen
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PE2020001534A
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English (en)
Inventor
Pravin L Kotian
Yarlagadda Babu
Weihe Zhang
Pen-Cheng Lu
Minwan Wu
Wei Lv
Trung Xuan Nguyen
zhao Dang
Venkat R Chintareddy
V Satish Kumar
Krishnan Raman
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Biocryst Pharm Inc
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Publication of PE20210398A1 publication Critical patent/PE20210398A1/es

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    • A61K31/4164—1,3-Diazoles
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    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • C07D495/04—Ortho-condensed systems

Abstract

Se describen compuestos de formulas I y II, donde: el anillo A es arilo, heteroarilo, cicloalquilo, o heterocicloalquilo; el anillo B es arilo, heteroarilo, heterocicloalquilo, o cicloalquilo; el anillo C es arilo o heteroarilo; Ra es halogeno, ciano, hidroxi, -NH2, -NH(Ac), -NH(alquilo), -NH(cicloalquilo), -NH(heterocicloalquilo), entre otros; Rb es halogeno, ciano, -alquilen-(polietilenglicol ramificado o no ramificado), -alquilen-O-(polietilenglicol ramificado o no ramificado), alquilo sustituido o no sustituido, haloalquilo, hidroxialquilo, entre otros; Rc es halogeno, -OH, -NRjRk, alcoxi, alquilo, cicloalquilo, y heterocicloalquilo; R1 es -NH2, -COOH, -CH2COOH, -CH(NH(CO)(alquil))COOH, -CH(NH(CO)(arilalquil))COOH, -CH(NH(CO)(cicloalquil))COOH, entre otros; n, m y p son 0, 1, 2, 3, o 4; J es -C(O)-, -NH-, -CH2-, -O-, -S-, -S(O)-, -SO2-, entre otros; K es -C(O)-, -NH-, -CH2-, -O-, -S-, -S(O)-, -SO2-, -N(alquilo)-, -CH(alquilo)-, entre otros; L es una union, -CH2-, -CH2CH2-, -CHR2-, -CF2-, -CFR2-, -C(O)-, -C(=NRL)-, entre otros; RL es H o alquilo; R2 es alquilo, cicloalquilo, hidroxialquilo, o haloalquilo; Rj y Rk son H, alquilo sustituido o no sustituido, aminoalquilo, (heterocicloalquil)alquilo, heterocicloalquilo, arilo, entre otros; U es N o CR3; R3 es H, halogeno, alquilo, cicloalquilo, arilo, heteroarilo, alcoxi, entre otros; V es N, CH, C(halogeno), o C(alquilo); T1 es N, CH, NRT1, o CRT1; T2 es NRT2 o CRT2; T3 es N, CH, NRT3, o CRT3; donde: (a) T1 es CRT1 o NRT1, donde RT1 y RT2, tomados junto con los atomos participantes, forman un anillo cicloalquilo, arilo, o heteroarilo opcionalmente sustituido; y T3 es N o CH; o (b) T3 es CRT3 o NRT3; donde RT3 y RT2, tomados junto con los atomos participantes, forman un anillo heteroarilo opcionalmente sustituido; y T1 es N o CH; y al menos uno de (a) T2 es NRT2, (b) T3 es N, o (c) T1 es NRT1; W es N, CH, o CRc; X es N, CH, o CRc; Y es N, CH, o CRc; Z es N, CH, o CRc; Rc es halogeno, -OH, -NRjRk, alcoxi o alquilo. Tambien esta referida a una composicion farmaceutica. Dichos compuestos son inhibidores del sistema del complemento. Tambien se proveen composiciones farmaceuticas que comprenden dicho compuesto, y metodos para usar los compuestos y composiciones en el tratamiento o prevencion de una enfermedad o condicion que se caracteriza por una actividad aberrante del sistema del complemento tales como trastornos inmunologicos, enfermedades renales, entre otras
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