AR031852A1 - Compuestos para tratar enfermedad de alzheimer - Google Patents

Compuestos para tratar enfermedad de alzheimer

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Publication number
AR031852A1
AR031852A1 ARP010103113A ARP010103113A AR031852A1 AR 031852 A1 AR031852 A1 AR 031852A1 AR P010103113 A ARP010103113 A AR P010103113A AR P010103113 A ARP010103113 A AR P010103113A AR 031852 A1 AR031852 A1 AR 031852A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
optionally substituted
alkoxy
csn
Prior art date
Application number
ARP010103113A
Other languages
English (en)
Original Assignee
Elan Pharm Inc
Upjohn Co
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
Application filed by Elan Pharm Inc, Upjohn Co filed Critical Elan Pharm Inc
Publication of AR031852A1 publication Critical patent/AR031852A1/es

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    • C07D295/22—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 hetero atoms directly attached to ring nitrogen atoms
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
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    • C07C311/08—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)

Abstract

La invencion comprende una amina sustituida de la formula (1)en donde R1 es (I) C1-6alquilo, opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste de C1-3alquilo, C1-7 alquilo (opcionalmente sustituido con C1-3 alquilo y C1-3 alcoxi), -F, -Cl, -Br, -I, -OH, -SH, -CsN, -CF3, C1-3 alcoxi, -NR1-aR1-b en donde R1-a y R1-b son ûH o C1-6 alquilo, -OC=O NR1-aR1-b en donde R1-a y R1b son como se ha definido anteriormente, (II) ûCH2-S(O)0-2(C1-6 alquilo), (III) ûCH2-CH2-S(O)0-2-(C1-6alquilo), (IV) C2-6 alquenilo con uno o dos enlaces dobles, opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste de ûF, -Cl, -OH, -SH, -CsN, CF3, C1-3 alcoxi, -NR1-aR1-b en donde R1-a y R1-b son ûH o C1-6 alquilo, (V) C2-6 alquinilo con uno o dos enlaces triples, opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste de ûF, -Cl, -OH, -SH, -CsN, -CF3, C1-3alcoxi, -NR1-aR1-b en donde R1-a y R1-b son ûH o C1-6 alquilo, (VI) û(CH2)n1-(R1-arilo) en donde n1 es cero o uno y en donde R1-arilo es fenilo, 1-naftilo, 2-naftilo e indanilo, indenilo, dihidronaftalilo, tetralinilo, opcionalmente sustituido con uno, dos, tres o cuatro de los siguientes sustituyentes en el anillo arilo: (A) C1-6 alquilo opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste de C1-3 alquilo, -F, Cl, -Br, -I, -OH, -SH, -NR1-aR1-b en donde R1-a y R1-b son como se definio anteriormente, -CsN, -CF3, C1-3 alcoxi, (B) C2-6 alquenilo con uno o dos enlaces dobles opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste de ûF, Cl, -OH, -SH, -CsN, -CF3, C1-3 alcoxi, -NR1-aR1-b en donde R1-a y R1-b son ûH o C1-6 alquilo, (C)C2-6 alquinilo con uno o dos enlaces triples, opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste de ûF, -Cl, -OH, -SH, -CsN, -CF3, C1-3 alcoxi, -NR1-aR1-b en donde R1-a y R1-b son ûH o C1-6 alquilo, (D) ûF, -Cl, -Br y ûI, (F)-C1-6 alcoxi opcionalmente sustituido con uno, dos o tres de ûF, (G) ûNRN-2RN-3 donde RN-2 y RN-3 son como se ha definido anteriormente, (H) ûOH (I) ûCsN, (J) C3-7 cicloalquilo, opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste de ûF, Cl, -OH, -SH, -CsN, -CF3, C1-3 alcoxi, -NR1-aR1-b en donde R1-a y R1-b son -H o C1-6 alquilo, (K) ûCO-(C1-4 alquilo) , (L) ûSO2NR1-aR1-b en donde R1-a y R1-b son como se ha definido anteriormente, (M) ûCO-NR1-aR1-b en donde R1-a y R1-b son como se ha definido anteriormente, (N) ûSO2-(C1-4 alquilo), (VII)-(CH2)n1-(R1-heteroarilo) en donde n1 es como se definio anteriormente y en donde R1-heteroarilo está seleccionado del grupo que consiste de: (A) piridinilo, (B) pirimidinilo, (C) quinolinilo, (F) benzotienilo, (G) indolilo, (H) indolinilo, (I) piridazinilo, (J) pirazinilo, (K) isoindolilo, (L) isoquinolilo, (M) quinazolinilo, (N) quinoxalinilo, (O) ftalazinilo, (P) imidazolilo, (Q) isoxazolilo, (R) pirazolilo, (S) oxazolilo, (T) tiazolilo, (U) indolizinilo, (V) indazolilo, (W) benzotiazolilo, (X) bencimidazolilo, (Y) benzofuranilo, (Z) furanilo, (AA) tienilo, (BB) pirrolilo, (CC) oxadiazolilo, (DD) tiadiazolilo, (EE) triazolilo, (FF) tetrazolilo, (II) oxazolopiridinilo, (JJ) imidazopiridinilo, (KK) isotiazolilo, (LL) naftiridinilo, (MM) cinnolinilo, (NN) carbazolilo, (OO) beta-carbolinilo, (PP) isocromanilo, (QQ) cromanilo, (SS) tetrahidroisoquinolinilo, (TT) isoindolinilo, (UU) isobenzotetrahidrofuranilo, (VV) isobenzotetrahidrotienilo, (WW) isobenzotienilo, (XX) benzoxazolilo, (YY) piridopiridinilo, (ZZ) benzotetrahidrofuranilo, (AAA) benzotetrahidrotienilo, (BBB) purinilo, (CCC) benzodioxolilo, triazinilo, fenoxazinilo, fenotiazinilo, pteridinilo, benzotiazolilo, imidazopiridinilo, imidazotiazolilo, dihidrobencisoxazinilo, bencisoxazinilo, benzoxazinilo, dihidrobencisotiazinilo, benzopiranilo, benzotiopiranilo, cumarinilo, isocumarinilo, cromonilo, cromanonilo, piridinil-N-oxido donde el grupo R1-heteroarilo está ligado al û(CH2)n1-mediante cualquier átomo del anillo del grupo madre RN-heteroarilo sustituido por hidrogeno de modo que el nuevo enlace al grupo R1-heteroarilo reemplaza el átomo de hidrogeno y su enlace, en donde el heteroarilo está opcionalmente sustituido con uno, dos tres o cuatro: (1) C1-6 alquilo opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste de C1-3 alquilo, -F, -Cl, -Br, -I, -OH, -SH, -NR1-aR1-b en donde R1-a y R1-b son como se definio anteriormente, -CsN, CF3, C1-3 alcoxi, (2) C2-6 alquenilo con uno o dos enlaces dobles opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste de ûF, -Cl, -OH, -SH, CsN, -CF3, C1-3 alcoxi, -NR1-aR1-b en donde R1-a y R1-b son ûH o C1-6 alquilo, (3) C2-6 alquinilo con uno o dos enlaces triples, opcionalmente sustituidos con uno, dos o tres sustituyentes seleccionados del grupo que consiste de ûF, -Cl, -OH, -SH, -CsN, -CF3, C1-3 alcoxi, -NR1-aR1-b en donde R1-a y R1-b son ûH o C1-6 alquilo, (4) ûF, -Cl, -Br y ûI, (6)-C1-6 alcoxi opcionalmente sustituido con uno, dos o tres de ûF, (7) ûNRN-2RN-3 donde RN-2 y RN-3 son como se define más adelante, (8) ûOH, (9) ûCsN, (10) C3-3 cicloalquilo, opcionalmente sustituido con uno dos o tres sustituyentes seleccionados del grupo que consiste de ûF, -Cl, -OH, -SH, -CsN, -CF3, C1-3 alcoxi, -NR1-aR1-b en donde NR1-aR1-b son ûH o C1-6 alquilo, (11) ûCO-(C1-4 alquilo), (12)-SO2-NR-NR1-aR1-b donde R1-a y R1-b son como se definio anteriormente, (13)-CO-NR1-aR1-b donde R1-a y R1-b son como se definio anteriormente, (14) ûSO2-(C1-4 alquilo), con la condicion de que cuando n1 es cero, R1-heteroarilo no está ligado a la cadena de carbonos mediante el nitrogeno, (VIII) û(CH2)n1-(R1-heterociclo) donde n1 es como se definio anteriormente y R1-heterociclo está seleccionado del grupo que consiste de: (A) morfolinilo, (B) tiomorfolinilo, (C) tiomorfolinil S-oxido, (D) tiomorfilinil S,S-dioxido, (E) piperazinilo, (F) homopiperazinilo, (G) pirrolidinilo, (H) pirrolinilo, (I) tetrahidropiranilo, (J) piperidinilo, (K) tetrahidrofuranilo, (L) tetrahidrotienilo, (M) homopiperidinilo, homomorfolinilo, homotiomorfolinilo, homotiomorfolinil S-oxido, homotiomorfolinil S,S-dioxido, y oxazolidinonilo, donde el grupo R1-heterociclo está ligado mediante cualquier átomo del grupo madre R1-heterociclo sustituido por hidrogeno de modo tal que el nuevo enlace al grupo R1-heterociclo reemplaza el átomo de hidrogeno y su enlace, en donde el heterociclo está opcionalmente sustituido con uno, dos tres o cuatro: (1) C1-6 alquilo opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste de C1-3 alquilo, -F, -Cl, -Br, -I, -OH, -SH, -NR1-aR1-b en donde R1-a y R1-b son como se definio anteriormente, -CsN, -CF3, C1-3 alcoxi (2) C2-6 alquenilo con uno o dos enlaces dobles, opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste de ûF, -Cl, -OH, -SH, -CsN, -CF3, C1-3 alcoxi, -NR1-aR1-b en donde R1-a y R1-b son ûH o C1-6 alquilo, (3) C2-6 alquinilo con uno o dos enlaces triples, opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste de ûF, -Cl, -OH, -SH, -CsN, -CF3, C1-3 alcoxi, -NR1-aR1-b en donde R1-a y R1-b son ûH o C1-6 alquilo, (4) ûF, -Cl, -Br y ûI, (5) C1-6 alcoxi, (6) ûC1-6 alcoxi opcionalmente sustituido con uno, dos o tres ûF, (7) ûNRN-2RN-3 en donde RN-2 y RN-3 son como se define más adelante, (8) ûOH, (9) ûCsN, (10) C3-7 cicloalquilo, opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste de ûF, -Cl, -OH, -SH, CsN, -CF3, C1-3 alcoxi, -NR1-aR1-b en donde R1-a y R1-b son ûH, o C1-6 alquilo, (11) ûCO(C1-4 alquilo), (12) ûSO2-NR1-aR1-b en donde R1-a y R1-b son como se definio anteriormente, (13) ûCO-NR1-aR1-b en donde R1-a y R1-b son como se definio anteriormente, (14) ûSO2-(C1-4alquilo), (15) =O, con la condicion de que cuando n1 es cero R1-heterociclo no está ligado a la cadena de carbono mediante nitrogeno; en donde R2 está seleccionado del grupo consistente de (I) ûH, (II) C1-6 alquilo, opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste de C1-3 alquilo, -F, -Cl, Br, -I, -OH, -SH, -CsN, -CF3, C1-3 alcoxi, -NR1-aR1-b en donde R1-a y R1-b son como se definio anteriormente; (III) û(CH2)0-4-R2-1 en donde R2-1 es R1-arilo o R1-heteroarilo en donde R1-arilo y R1-heteroarilo son como se definio anteriormente ; (IV) C2-6 alquenilo con uno o dos enlaces, opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste de ûF, -Cl, -OH, -SH, -CsN, -CF3, C1-3 alcoxi, -NR1-aR1-b en donde R1-a y R1-b son ûH o C1-6 alquilo, (V) C2-6 alquinilo con uno o dos enlaces triples, opcionalmente sustituido con uno, dos o tres sustituyentes del grupo que consiste de ûF, -Cl, -OH, -SH, -CsN, -CF3, C1-3 alcoxi, -NR1-aR1-b en donde R1-a y R1-b son ûH o C1-6 alquilo, (VI) û(CH2)0-4-C3-7 cicloalquilo, opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste de ûF, -Cl, -OH, -SH, -CsN, -CF3, C1-3 alcoxi, -NR1-aR1-b en donde R1-a y R1-b son ûH o C1-6 alquilo, donde R3 está seleccionado del grupo que consiste de: (I) ûH, (II) C1-6 alquilo, opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste de C1-3 alquilo, -F, -Cl, -Br, -I, -OH, -SH, -CsN, -CF3, C1-3 alcoxi, -NR1-aR1-b en donde R1-aR1-b en donde R1-a y R1-b son como se define anteriormente, (III) û(CH2)0-4-R2-1 en donde R2-1 es R1-arilo o R1-heteroarilo en donde R1-arilo y R1-heteroarilo son como se definio anteriormente; (IV) C2-6 alquenilo con uno o dos enlaces dobles, (V) C2-6 alquinilo con uno o dos enlaces triples, (VI) û(CH2)0-4-C3-7 cicloalquilo, opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste d
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