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AR077162A1 - C5ar antagonistas - Google Patents

C5ar antagonistas

Info

Publication number
AR077162A1
AR077162A1 ARP090105070A ARP090105070A AR077162A1 AR 077162 A1 AR077162 A1 AR 077162A1 AR P090105070 A ARP090105070 A AR P090105070A AR P090105070 A ARP090105070 A AR P090105070A AR 077162 A1 AR077162 A1 AR 077162A1
Authority
AR
Argentina
Prior art keywords
group
heteroaryl
alkyl
aryl
independently selected
Prior art date
Application number
ARP090105070A
Other languages
English (en)
Inventor
Ju Yang
Pingchen Fan
Kevin Lloyd Greenman
Manmohan Reddy Leleti
Yandong Li
Jay Powers
Hiroko Tanaka
Yibin Zeng
Original Assignee
Chemocentryx Inc
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=42267017&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR077162(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Chemocentryx Inc filed Critical Chemocentryx Inc
Publication of AR077162A1 publication Critical patent/AR077162A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
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    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/14—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
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    • C07D401/02—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 two hetero rings
    • C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D401/10—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 two hetero rings linked by a carbon chain containing aromatic rings
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Abstract

Composiciones farmacéuticas, métodos para el tratamiento de enfermedades y trastornos que comprenden una activacion patologica de receptores de C5a. Reivindicacion 1: Un compuesto, caracterizado porque es de formula (1) y sales aceptables farmacéuticamente, hidratos y rotámeros del mismo; donde C1 se selecciona del grupo que consiste de arilo y heteroarilo, donde el grupo heteroarilo tiene entre 1 y 3 heteroátomos como miembros del anillo seleccionados entre N, O y S; y donde dichos grupos arilo y heteroarilo se sustituyen opcionalmente con entre 1 y 3 sustituyentes R1; C2 se selecciona del grupo que consiste de arilo y heteroarilo, donde el grupo heteroarilo tiene entre 1 y 3 heteroátomos como miembros del anillo seleccionados entre N, O y S; y donde dichos grupos arilo y heteroarilo se sustituyen opcionalmente con entre 1 y 3 sustituyentes R2; C3 se selecciona del grupo que consiste de alquilo C1-8, cicloalquilo C3-8, cicloalquil C3-8-alquilo C1-4, arilo, aril-C1-4-alquilo, heteroarilo, heteroaril-C1-4 alquilo, heterocicloalquilo o heterocicloalquil-C1-4 alquilo, donde el grupo o porcion heterocicloalquilo tiene entre 1 y 3 heteroátomos seleccionados entre N, O y S, y donde el grupo heteroarilo tiene entre 1 y 3 heteroátomos como miembros del anillo seleccionados entre N, O y S, y cada C3 se sustituye opcionalmente con entre 1 y 3 sustituyentes R3; cada R1 se selecciona independientemente del grupo que consiste de halogeno, -CN, Rc, -CO2Ra, -CONRaRb, -C(O)Ra, -OC(O)NRaRb, -NRbC(O)Ra, - NRbC(O)2Rc, -Nra-C(O)NRaRb, -NRaC(O)NRaRb, -NRaRb, -ORa y -S(O)2NRaRb; donde cada Ra y Rb se selecciona independientemente entre hidrogeno, alquilo C1-8 y haloalquilo C1-8, o cuando se unen al mismo átomo de nitrogeno se pueden combinar con el átomo de nitrogeno para formar un anillo de cinco o seis miembros que tiene entre 0 y 2 heteroátomos adicionales como miembros del anillo seleccionados entre N, O o S; cada Rc se selecciona independientemente del grupo que consiste de alquilo C1-8, haloalquilo C1-8, cicloalquilo C3-6, heterocicloalquilo, arilo y heteroarilo, y donde las porciones alifáticas y cíclicas de Ra, Rb y Rc se sustituyen opcionalmente adicionalmente con entre uno y tres grupos halogeno, hidroxi, metilo, amino, alquilamino y dialquilamino; y opcionalmente cuando dos sustituyentes R1 se encuentran en átomos adyacentes, se combinan para formar un anillo carbocíclico fusionado de cinco o seis miembros; cada R2 se selecciona independientemente del grupo que consiste de halogeno, -CN, -Rf, -CO2Rd, -CONRdRe, -C(O)Rd, -OC(O)NRdRe, -NReC(O)Rd, -NReC(O)2Rf, -NRdC(O)NRdRe, -NRdC(O)NRdRe, -NRdRe, -ORd, y -S(O)2NRdRe; donde cada Rd y Re se selecciona independientemente entre hidrogeno, alquilo C1-8, y haloalquilo C1-8, o cuando se unen al mismo átomo de nitrogeno se pueden combinar con el átomo de nitrogeno para formar un anillo de cinco o seis miembros que tiene entre 0 y 2 heteroátomos adicionales como miembros del anillo seleccionados entre N, O o S; cada Rf se selecciona independientemente del grupo que consiste de alquilo C1-8, haloalquilo C1-8, cicloalquilo C3-6, heterocicloalquilo, arilo y heteroarilo, y donde las porciones alifáticas y cíclicas de Rd, Re y Rf se sustituyen opcionalmente adicionalmente con entre uno y tres grupos halogeno, hidroxi, metilo, amino, alquilamino y dialquilamino; cada R3 se selecciona independientemente del grupo que consiste de halogeno, -CN, -Ri, -CO2Rg, -CONRgRh, -C(O)Rg, -OC(O)NRgRh, -NRhC(O)Rg, -NRhC(O)2Ri, -NRgC(O)NRgRh, -NRgRh, -ORg, -S(O)2NRgRh, -X4-Rj, -X4-NRgRh -X4-CONRgRh, -X4-NRhC(O)Rg, -NHRj y -NHCH2Rj, donde X4 es un alquileno C1-4; cada Rg y Rh se selecciona independientemente entre hidrogeno, alquilo C1-8, cicloalquilo C3-6 y haloalquilo C1-8, o cuando se unen al mismo átomo de nitrogeno se pueden combinar con el átomo de nitrogeno para formar un anillo de cinco o seis miembros que tiene entre 0 y 2 heteroátomos adicionales como miembros del anillo seleccionados entre N, O o S y se sustituye opcionalmente con uno o dos oxo; cada Ri se selecciona independientemente del grupo que consiste de alquilo C1-8, haloalquilo C1-8, cicloalquilo C3-6, heterocicloalquilo, arilo y heteroarilo; y cada Rj se selecciona del grupo que consiste de cicloalquilo C3-6, pirrolinilo, piperidinilo, morfolinilo, tetrahidrofuranilo, y tetrahidropiranilo, y donde las porciones alifáticas y cíclicas de Rg, Rh, Ri y Rj se sustituyen opcionalmente adicionalmente con entre uno y tres grupos halogeno, metilo, CF3, hidroxi, amino, alquilamino y dialquilamino; y X es hidrogeno o CH3.
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