AR078120A1 - Antagonistas de ccr3 de arilsulfonamida 2,5-disustituida y composiciones farmaceuticas - Google Patents

Antagonistas de ccr3 de arilsulfonamida 2,5-disustituida y composiciones farmaceuticas

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Publication number
AR078120A1
AR078120A1 ARP100101320A ARP100101320A AR078120A1 AR 078120 A1 AR078120 A1 AR 078120A1 AR P100101320 A ARP100101320 A AR P100101320A AR P100101320 A ARP100101320 A AR P100101320A AR 078120 A1 AR078120 A1 AR 078120A1
Authority
AR
Argentina
Prior art keywords
nr1br1c
nr1ac
nr1as
alkyl
independently
Prior art date
Application number
ARP100101320A
Other languages
English (en)
Original Assignee
Axikin Pharmaceuticals 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.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42344061&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR078120(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Axikin Pharmaceuticals Inc filed Critical Axikin Pharmaceuticals Inc
Publication of AR078120A1 publication Critical patent/AR078120A1/es

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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
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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
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
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    • C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07D295/04—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
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    • C07D295/13—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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  • Psychiatry (AREA)

Abstract

Arilsulfonamidas 2,5-disustituidas utiles para modular la actividad de CCR3 y composiciones farmacéuticas de éstas. También métodos de uso para el tratamiento, la prevencion o la mejora de uno o más síntomas de un trastorno, enfermedad o afeccion mediados por CCR3. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula (1) o un enantiomero, una mezcla de enantiomeros, una mezcla de dos o más diastereomeros, un tautomero o una mezcla de dos o más tautomeros de éste; o una sal, solvato, hidrato o profármaco farmacéuticamente aceptable de éste; en donde R1 y R2 son cada uno, independientemente, (a) halo, ciano, nitro, hidroxilo o guanidina; (b) alquilo C1-6, alcoxi C1-6 o alquiltio C1-6, en donde cada uno de alquilo, alcoxi y alquiltio se sustituyen, de manera independiente y opcional, con uno, dos o tres halo; (c) alquenilo C2-6, alquinilo C2-6, fenilo, bencilo, fenoxi, benzoxi o heterociclilo; o (d) -C(O)R1a, -C(O)OR1a, -C(O)NR1bR1c, -C(NR1a)NR1bR1c, -OC(O)R1a, -OC(O)OR1a, -OC(O)NR1bR1c, -OC(=NR1a)NR1bR1c, -OS(O)R1a, -OS(O)2R1a, -OS(O)NR1bR1c, -OS(O)2NR1bR1c, -NR1bR1c, -NR1aC(O)R1d, -NR1aC(O)OR1d, -NR1aC(O)NR1bR1c, -NR1aC(=NR1d)NR1bR1c, - NR1aS(O)R1d, -NR1aS(O)2R1d, -NR1aS(O)NR1bR1c, -NR1aS(O)2NR1bR1c, -S(O)R1a, -S(O)2R1a, -S(O)NR1bR1c, o -S(O)2NR1bR1c; R3 es (a) hidrogeno, halo, ciano, nitro o hidroxilo; (b) alquilo C1-6, alcoxi C1-6 o alquiltio C1-6, en donde cada uno de alquilo, alcoxi y alquiltio se sustituyen, de manera independiente y opcional, con uno, dos o tres halo; (c) alquenilo C2-6, alquinilo C2-6 o tetrazolilo; o (d) -C(O)R1a, -C(O)OR1a, -C(O)NR1bR1c, -C(NR1a)NR1bR1c, -OC(O)R1a, -OC(O)OR1a, -OC(O)NR1bR1c, -OC(=NR1a)NR1bR1c, -OS(O)R1a, -OS(O)2R1a, -OS(O)NR1bR1c, -OS(O)2NR1bR1c, -NR1bR1c, -NR1aC(O)R1d, -NR1aC(O)OR1d, -NR1aC(O)NR1bR1c, -NR1aC(=NR1d)NR1bR1c, -NR1aS(O)R1d, -NR1aS(O)2R1d, -S(O)R1a, -S(O)2R1a, -S(O)NR1bR1c, o -S(O)2NR1bR1c, R4 es como en formulas (2); R5 es (a) halo, ciano, nitro, hidroxilo, oxo o guanidina; (b) alquilo C1-6, alcoxi C1-6 o alquiltio C1-6, en donde cada uno de alquilo, alcoxi y alquiltio se selecciona, de manera independiente y opcional, con uno, dos o tres halo; (c) alquenilo C2-6, alquinilo C2-6, fenilo, bencilo, fenoxi, benzoxi o heterociclilo; o (d) -C(O)R1a, -C(O)OR1a, -C(O)NR1bR1c, -C(NR1a)NR1bR1c, -OC(O)R1a, -OC(O)OR1a, -OC(O)NR1bR1c, -OC(=NR1a)NR1bR1c, -OS(O)R1a, -OS(O)2R1a, -OS(O)NR1bR1c, -OS(O)2NR1bR1c, -NR1bR1c, -NR1aC(O)R1d, -NR1aC(O)OR1d, -NR1aC(O)NR1bR1c, -NR1aC(=NR1d)NR1bR1c, -NR1aS(O)R1d, -NR1aS(O)2R1d, -NR1aS(O)NR1d, -NR1aS(O)2R1d, -S(O)R1a, -S(O)2R1a, -S(O)NR1bR1c, o -S(O)2NR1bR1c; X es O o S; Y es -O-, -S-, -S(O)-, -S(O)2-, -N(R1a)-, -C(R1a)(R1d)- o -C(R1a)(NR1bR1c)-; m es un entero de 0 a 3; n es un entero de 1 a 3; p es un entero de 0 a 4; r es un entero de 1 a 6; y cada R1a, R1b, R1c y R1d es, independientemente, (a) hidrogeno, fenilo o bencilo; (b) cicloalquilo C3-7, heteroarilo o heterociclilo, cada uno opcionalmente sustituido; o (c) alquilo C1-6, opcionalmente sustituido con uno, dos o tres sustituyentes, en donde cada uno se selecciona, independientemente, de halo, hidroxilo, carboxi, alcoxi, carbamoílo, arilo C6-14, alquilcarbamoílo C1-6, di(alquil C1-6)carbamoílo, cicloalquilcarbamoílo C3-7 y heterociclilcarbamoílo C3-7; o cada par de R1b y R1c, junto con el átomo N al cual están unidos, forman independientemente heteroarilo o heterociclilo; siempre que cuando X sea O; Y sea -N(R1a)-; m y n sean 1; R1 y R2 sean cada uno, independientemente cloro, nitro, metilo o isopropilo; R3 sea nitro; y p sea 0; entonces R1a no es hidrogeno. Reivindicacion 35: Una composicion farmacéutica caracterizada porque comprende un compuesto de acuerdo con cualquiera de las reivindicaciones 1 a 34, o una sal, solvato, hidrato, estereoisomero o tautomero farmacéuticamente aceptable de éste; y uno o más portadores o excipientes farmacéuticamente aceptables.
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