ES2575154T3 - Moduladores alostéricos positivos del receptor M1 de quinolina amida - Google Patents

Moduladores alostéricos positivos del receptor M1 de quinolina amida Download PDF

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ES2575154T3
ES2575154T3 ES10841821.1T ES10841821T ES2575154T3 ES 2575154 T3 ES2575154 T3 ES 2575154T3 ES 10841821 T ES10841821 T ES 10841821T ES 2575154 T3 ES2575154 T3 ES 2575154T3
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alkyl
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halogen
ring
ring atoms
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Scott D. Kuduk
Kelly-Ann Schlegel
Zhi-Qiang Yang
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Organon Pharma UK Ltd
Merck Sharp and Dohme LLC
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/58—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
    • C07D215/60—N-oxides
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4704—2-Quinolinones, e.g. carbostyril
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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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07D215/16—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 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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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
    • C07D401/04—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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    • C07D401/06—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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    • C07D401/02—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
    • C07D401/10—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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    • 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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    • 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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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Un compuesto de formula (I):**Fórmula** en la que X1 se selecciona entre el grupo que consiste en (1) N, y (2) NO; X2-X3 se seleccionan entre el grupo que consiste en (1) -CH2-CH2-, (2) -O-CH2-, (3) -CH2-O-, o (4) -CH2-; X4, X5, X6 y X7 se seleccionan cada uno entre el grupo que consiste en (1) N, (2) N→ O, (3) CH, (4) O con la condicion de que uno de X4, X5, X6 y X7 puede estar ausente, formando de ese modo un anillo de cinco miembros; R1 se selecciona entre el grupo que consiste en (1) hidrogeno, (2) halogeno, (3) -alquilo C1-6, (4) -alquinilo C2-6, (4) fenilo, (5) >=O, (6) >=CH2, (7) hidroxilo, en donde los grupos alquilo, alquinilo o fenilo de R1 estan opcionalmente sustituidos con uno o mas (a) hidroxilo, o (b) halogeno; R2A y R2B se seleccionan independientemente entre el grupo que consiste en (1) hidrogeno, (2) hidroxilo, y (3) halogeno, o R2A y R2B forman juntos >=O; R3 esta opcionalmente presente en uno o mas de los atomos de carbono del anillo y se selecciona independientemente entre el grupo que consiste en (1) halogeno, (2) -O-alquilo C1-6, (3) -S-alquilo C1-6, o (4) un grupo heteroarilo, que es un grupo ciclico aromatico, que tiene de cinco a doce atomos de anillo, dichos atomos de anillo se seleccionan entre C, O, N, N → O o S, al menos uno de los cuales es O, N, N → O o S, en donde el heteroarilo esta opcionalmente sustituido con alquilo C1-6; R4 esta opcionalmente presente en uno o mas de los atomos de anillo y se selecciona entre el grupo que consiste en (1) hidroxilo, (2) halogeno, (3) -alquilo C1-6, (4) -O-alquilo C1-6, (5) -S-alquilo C1-6, (6) -cicloalquilo C3-8, (7) -arilo C6-10, (8) -CN, (9) un grupo heteroarilo, que es un grupo ciclico aromatico, que tiene de cinco a doce atomos de anillo, dichos atomos de anillo se seleccionan entre C, O, N, NO o S, al menos uno de los cuales es O, N, N → O o S, (10) -O-heterociclilo, (11) -NRARB, en donde RA y RB se seleccionan entre el grupo que consiste en (a) hidrogeno, o (b) -alquilo C1-6, o RA y RB se unen junto con el nitrogeno al que estan unidos para formar un anillo carbociclico de 4 a 6 40 miembros, en el que uno o dos de los atomos de carbono de anillo estan opcionalmente reemplazados por un nitrogeno, un oxigeno o un azufre, y el anillo esta opcionalmente sustituido con uno o mas (a) halogeno, (b) hidroxilo, (c) alquilo C1-6, (d) -O-alquilo C1-6, (e) -C(>=O)-(O)n -alquilo C1-6; en donde n es 0-1; y el grupo alquilo, cicloalquilo, arilo o heteroarilo de R4 esta opcionalmente sustituido con uno o mas (a) halogeno, (b) hidroxi, (c) -O-alquilo C1-6, (d) -alquilo C1-6, (e) -S-alquilo C1-6, o (f) un grupo heteroarilo, que es un grupo ciclico aromatico, que tiene de cinco a doce atomos de anillo, dichos atomos de anillo se seleccionan entre C, O, N, N → O o S, al menos uno de los cuales es O, N, N → O o S, en donde los restos alquilo, arilo o heteroarilo estan opcionalmente sustituidos con uno o mas (i) halogeno, (ii) hidroxi, (iii) -O-alquilo C1-6, o (iv) -alquilo C1-6; o dos grupos R4 se unen conjuntamente para formar un grupo heteroarilo de anillo condensado de tres o cuatro atomos, dichos atomos de anillo se seleccionan entre C, O, N, N → O o S, al menos uno de los cuales es O, N, N → O o S, o una sal farmaceuticamente aceptable del mismo.

Description

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Claims (1)

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ES10841821.1T 2009-12-17 2010-12-13 Moduladores alostéricos positivos del receptor M1 de quinolina amida Active ES2575154T3 (es)

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US287535P 2001-04-30
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PCT/US2010/060007 WO2011084368A1 (en) 2009-12-17 2010-12-13 Quinoline amide m1 receptor positive allosteric modulators

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