AR091654A1 - COMPOUNDS CONTAINING BIARILO AS INVESTED AGONISTS OF ROR-g RECEIVERS - Google Patents

COMPOUNDS CONTAINING BIARILO AS INVESTED AGONISTS OF ROR-g RECEIVERS

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Publication number
AR091654A1
AR091654A1 ARP130102358A AR091654A1 AR 091654 A1 AR091654 A1 AR 091654A1 AR P130102358 A ARP130102358 A AR P130102358A AR 091654 A1 AR091654 A1 AR 091654A1
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AR
Argentina
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optionally substituted
alkyl
independently
cycloalkyl
heterocycloalkyl
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Spanish (es)
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Biogen Idec Inc
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Publication of AR091654A1 publication Critical patent/AR091654A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/04—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
    • C07D215/08—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
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    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
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    • C07B59/002—Heterocyclic compounds
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/88—Carboxylic acid amides having nitrogen atoms of carboxamide groups bound to an acyclic carbon atom and to a carbon atom of a six-membered aromatic ring wherein at least one ortho-hydrogen atom has been replaced
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/30—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C07C255/60—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
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    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
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    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
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    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
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    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16—Benzazepines; Hydrogenated benzazepines
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    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/42—Benzopyrazines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • C07D257/06—Five-membered rings with nitrogen atoms directly attached to the ring carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
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    • C07D305/00—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
    • C07D305/02—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D305/04—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D305/08—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings 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 atoms
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    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans 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 carbon atoms of the hetero ring
    • C07D307/84—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
    • C07D333/30—Hetero atoms other than halogen
    • C07D333/36—Nitrogen atoms
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D401/00—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
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
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    • C07D401/00—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
    • C07D401/14—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 three or more hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
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    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems

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Abstract

Composiciones farmacéuticas que comprenden estos agonistas inversos que contienen biarilo y método para modular y usar receptores ROR-g usando estos agonistas inversos. Reivindicación 1: Un compuesto de fórmula (1) o sales farmacéuticamente aceptables de los mismos, en donde: R¹ᵃ y R¹ᵇ son cada uno independientemente H, alquilo opcionalmente sustituido, alcoxi opcionalmente sustituido, cicloalquilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, aralquilo opcionalmente heteroaralquilo opcionalmente sustituido, heterocicloalquil-alquilo opcionalmente sustituido, cicloalquil-alquilo opcionalmente sustituido, o R¹ᵃ y R¹ᵇ tomados juntos forman un anillo heterocíclico de 4 a 7 miembros opcionalmente sustituido; R²ᵃ, R²ᵇ, R²ᶜ y R²ᵈ son cada uno independientemente H, halógeno, alquilo C₁₋₄, O-alquilo C₁₋₄ o CF₃; R³ es H, alquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, OR⁴, halógeno, SR⁴, S(O)₂R⁴, NR⁵R⁶, un heteroarilo opcionalmente sustituido o un heterocicloalquilo opcionalmente sustituido; R⁴, R⁵ y R⁶ son cada uno independientemente alquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido o heterocicloalquilo opcionalmente sustituido; R⁷ es alquilo C₁₋₄ o R³ y R⁷ pueden tomarse juntos para formar un anillo heterocíclico de 4 a 7 miembros opcionalmente sustituido; R⁸ᵃ, R⁸ᵇ, R⁸ᶜ, R⁸ᵈ y R⁸ᵉ son cada uno independientemente H, halógeno, alquilo C₁₋₄, OR⁴, NR⁵R⁶, CF₃ o CN; X es CH o N; y J es un enlace o alquileno C₁₋₄. Reivindicación 5: Un compuesto de fórmula (2) o sales farmacéuticamente aceptables del mismo, en donde J es un enlace o alquileno C₁₋₄: A es un resto de formula (3) ó (4); B es seleccionado del los compuestos de formula (5) - (10); siempre y cuando J es alquileno C₁₋₄ y B es el resto de formula (5), R¹⁰ no es hidroxilo; X¹ es CH o N; X² es C-R²ᵃ o N; X³ es C-R²ᵇ o N; X⁴ es C-R²ᵈ o N; X⁵ es S u O; R²ᵃ, R²ᵇ, R²ᶜ y R²ᵈ son cada uno independientemente H, halógeno, alquilo C₁₋₄, O-alquilo C₁₋₄ o CF₃; R³ es H, alquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, OR⁴, halógeno, SR⁴, S(O)₂R⁴, NR⁵R⁶, un heteroarilo opcionalmente sustituido o un heterocicloalquilo opcionalmente sustituido; cada R⁴ es independientemente alquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido o heterocicloalquilo opcionalmente sustituido; R⁵ y R⁶ son cada uno independientemente hidrógeno, alquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido o heterocicloalquilo opcionalmente sustituido; R⁷ es alquilo C₁₋₄ o R³ y R⁷ pueden tomarse juntos para formar un anillo heterocíclico de 5 a 7 miembros opcionalmente sustituido; R⁸ᵃ, R⁸ᵇ, R⁸ᶜ, R⁸ᵈ, son cada uno independientemente H, halógeno, alquilo C₁₋₄, OR⁴, NR⁵R⁶, CF₃ o CN; R⁹ es un enlace, alquileno opcionalmente sustituido o cicloalquileno opcionalmente sustituido; R¹⁰ es NR¹ᵃR¹ᵇ, hidroxilo o alquilo opcionalmente sustituido; y R¹²ᵃ y R¹²ᵇ son cada uno independientemente alquilo opcionalmente sustituido, o R¹²ᵃ y R¹²ᵇ pueden tomarse juntos para formar un anillo heterocíclico de 4 a 7 miembros, y R¹ᵃ y R¹ᵇ son cada uno independientemente H, alquilo opcionalmente sustituido, alcoxi opcionalmente sustituido, cicloalquilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, aralquilo opcionalmente sustituido, heteroaralquilo opcionalmente sustituido, heterocicloalquil-alquilo opcionalmente sustituido, cicloalquil-alquilo opcionalmente sustituido, o R¹ᵃ y R¹ᵇ tomados juntos forman un anillo heterocíclico de 4 a 7 miembros opcionalmente sustituido.Pharmaceutical compositions comprising these inverse agonists containing biaryl and method for modulating and using ROR-g receptors using these inverse agonists. Claim 1: A compound of formula (1) or pharmaceutically acceptable salts thereof, wherein: R¹ᵃ and R¹ᵇ are each independently H, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted heteroaryl, optionally substituted heteroaralkyl optionally substituted, optionally substituted heterocycloalkyl-alkyl, optionally substituted cycloalkyl-alkyl, or R¹ᵃ and R¹ᵇ taken together form an optionally substituted 4- to 7-membered heterocyclic ring; R²ᵃ, R²ᵇ, R²ᶜ and R²ᵈ are each independently H, halogen, C₁₋₄ alkyl, O-C₁₋₄ alkyl or CF₃; R³ is H, optionally substituted alkyl, optionally substituted cycloalkyl, OR⁴, halogen, SR⁴, S (O) ₂R⁴, NR⁵R⁶, an optionally substituted heteroaryl or an optionally substituted heterocycloalkyl; R⁴, R⁵ and R⁶ are each independently optionally substituted alkyl, optionally substituted cycloalkyl or optionally substituted heterocycloalkyl; R⁷ is C₁₋₄ or R³ alkyl and R⁷ can be taken together to form an optionally substituted 4- to 7-membered heterocyclic ring; R⁸ᵃ, R⁸ᵇ, R⁸ᶜ, R⁸ᵈ and R⁸ᵉ are each independently H, halogen, C₁₋₄ alkyl, OR⁴, NR⁵R⁶, CF₃ or CN; X is CH or N; and J is a C₁₋₄ bond or alkylene. Claim 5: A compound of formula (2) or pharmaceutically acceptable salts thereof, wherein J is a bond or C₁₋₄ alkylene: A is a moiety of formula (3) or (4); B is selected from the compounds of formula (5) - (10); as long as J is C₁₋₄ alkylene and B is the remainder of formula (5), R¹⁰ is not hydroxyl; X¹ is CH or N; X² is C-R²ᵃ or N; X³ is C-R²ᵇ or N; X⁴ is C-R²ᵈ or N; X⁵ is S or O; R²ᵃ, R²ᵇ, R²ᶜ and R²ᵈ are each independently H, halogen, C₁₋₄ alkyl, O-C₁₋₄ alkyl or CF₃; R³ is H, optionally substituted alkyl, optionally substituted cycloalkyl, OR⁴, halogen, SR⁴, S (O) ₂R⁴, NR⁵R⁶, an optionally substituted heteroaryl or an optionally substituted heterocycloalkyl; each R⁴ is independently optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heteroaryl or optionally substituted heterocycloalkyl; R⁵ and R⁶ are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl or optionally substituted heterocycloalkyl; R⁷ is C₁₋₄ or R³ alkyl and R⁷ can be taken together to form an optionally substituted 5- to 7-membered heterocyclic ring; R⁸ᵃ, R⁸ᵇ, R⁸ᶜ, R⁸ᵈ, are each independently H, halogen, C₁₋₄ alkyl, OR⁴, NR⁵R⁶, CF₃ or CN; R⁹ is a bond, optionally substituted alkylene or optionally substituted cycloalkylene; R¹⁰ is NR¹ᵃR¹ᵇ, hydroxy or optionally substituted alkyl; and R¹²ᵃ and R¹²ᵇ are each independently optionally substituted alkyl, or R¹²ᵃ and R¹²ᵇ can be taken together to form a 4- to 7-membered heterocyclic ring, and R¹ᵃ and R¹ᵇ are each independently H, optionally substituted alkyl, optionally substituted alkoxy, optionally cycloalkyl substituted, optionally substituted heterocycloalkyl, optionally substituted heteroaryl, optionally substituted aralkyl, optionally substituted heteroaralkyl, optionally substituted heterocycloalkyl-alkyl, optionally substituted cycloalkyl-alkyl, or R¹ᵃ and R¹ᵇ taken together form an optionally substituted 4- to 7-membered heterocyclic ring.

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