ES2620531T3 - Inhibidores de la fosfodiesterasa tipo 10A - Google Patents

Inhibidores de la fosfodiesterasa tipo 10A Download PDF

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ES2620531T3
ES2620531T3 ES12784578T ES12784578T ES2620531T3 ES 2620531 T3 ES2620531 T3 ES 2620531T3 ES 12784578 T ES12784578 T ES 12784578T ES 12784578 T ES12784578 T ES 12784578T ES 2620531 T3 ES2620531 T3 ES 2620531T3
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Hervé Geneste
Michael Ochse
Karla Drescher
Sean Turner
Berthold Behl
Loic LAPLANCHE
Jürgen DINGES
Clarissa Jakob
Lawrence A. Black
Katja. JANTOS
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AbbVie Deutschland GmbH and Co KG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D401/06—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
    • C—CHEMISTRY; METALLURGY
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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
    • C07D401/08—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 alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D401/14—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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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D405/14—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 three or more hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more 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
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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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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    • C07—ORGANIC CHEMISTRY
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    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
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  • Child & Adolescent Psychology (AREA)
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  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Compuesto de fórmula I **Fórmula** en el que Q es O o S; X1 es N o CH; X2 es N o C-R7; X3 es O, S, -X4>=C(R8)-, donde C(R8) está unido al átomo de carbono que lleva a R2, o -X5>=C(R9)-, donde X5 está unido al átomo de carbono que lleva a R2; X4 es N o C-R9; X5 es N; Het se elige entre i. hetarilo monocíclico de 6 integrantes unido por C con 1 o 2 átomos de nitrógeno como integrantes del anillo, que no está sustituido o puede llevar 1, 2, 3 o 4 sustituyentes Rx idénticos o diferentes, ii. hetarilo bicíclico fusionado con 1 o 2 átomos de nitrógeno y opcionalmente otro heteroátomo elegido entre O, S y N como integrantes del anillo, benzotienilo o benzofurilo, donde el hetarilo bicíclico, benzotienilo y benzofurilo, independientemente unos de otros, no están sustituidos o pueden llevar 1, 2, 3 o 4 sustituyentes Rx idénticos o diferentes, y fenilo, que lleva un radical hetarilo monocíclico con 1 o 2 átomos de nitrógeno y opcionalmente otro heteroátomo elegido entre O, S y N como integrantes del anillo, el cual además del hetarilo monocíclico, puede llevar 1, 2 o 3 sustituyentes Rx iguales o diferentes, donde Rx se elige del grupo que consiste en H, halógeno, C1-C4-alquilo, C1-C4-alcoxi, C1-C4-fluoroalquilo, C1-C4- fluoroalcoxi, C3-C6-cicloalquilo, C1-C4-alcoxi-C1-C4-alcoxi, C1-C4-alcoxi-C1-C4-alquilo, OH, hidroxi-C1-C4- 30 alquilo, O-C3-C6-cicloalquilo, benciloxi, C(O)O-(C1-C4-alquilo), O-(C1-C4-alquilo)-CO2H, N(Rx1)(Rx2), C(O)N(Rx1)(Rx2), C1-C4-alquil-N(Rx1)(Rx2), -NRx3-C(O)-N(Rx1)(Rx2),NRx3-C(O)O-(C1-C4-alquil), -N(Rx3)-SO2- Rx4, fenilo, CN, -SF5, -OSF5, -SO2Rx4, -SRx4 y trimetilsililo, donde Rx1, Rx2, Rx3 y Rx4, se eligen independientemente unos de otros del grupo que consiste en hidrógeno, C1-C4-alquilo, C1-C4-fluoroalquilo y C3-C6-cicloalquilo o Rx1 y Rx2 junto con el átomo de N al cual están unidos forman un heterociclo de nitrógeno de 3 a 7 integrantes, que puede tener 1, 2 o 3 heteroátomos idénticos o diferentes o grupos que contienen heteroátomos elegidos del grupo de O, N, S, SO y SO2 como integrantes del anillo y puede llevar 1, 2, 3, 4, 5 o 6 sustituyentes elegidos entre C1-C4-alquilo, o dos radicales Rx que están unidos a átomos de carbono adyacentes pueden formar un radical carbocíclico saturado fusionado de 5 o 6 integrantes o un radical heterocíclico fusionado de 5 o 6 integrantes con 1, 2 o 3 heteroátomos como integrantes del anillo, que se eligen entre O, S y N; R1 es una fracción de Y1-Cyc1; R2 se elige del grupo que consiste en hidrógeno, halógeno, OH, C1-C4-alquilo, trimetilsililo, C1-C4-alcoxi-C1-C4- alquilo, C1-C4-alcoxi, C1-C4-alcoxi-C1-C4-alcoxi, C2-C4-alqueniloxi, C1-C4-fluoroalquilo, C1-C4-fluoroalcoxi, ciclopropilo, opcionalmente sustituido con 1, 2 o 3 grupos metilo, ciclopropilo fluorado, CN y NRx1Rx2; A representa uno de los grupos siguientes A1, A2, A3, A4 o A5: **Fórmula** donde * indica los puntos de unión a Het y al átomo de nitrógeno, respectivamente; R3, R4, R5, R6 independientemente unos de otros se eligen del grupo que consiste en hidrógeno, halógeno, C1- C4-alquilo, trimetilsililo, C1-C4-fluoroalquilo, C1-C4-fluoroalcoxi, C3-C6-cicloalquilo, o los radicales junto con los átomos de carbono a los cuales están unidos forman un carbociclo saturado de 3 a 6 integrantes o un heterociclo saturado de 3 a 6 integrantes con 1 o 2 heteroátomos que no son adyacentes como integrantes del anillo, donde el carbociclo y el heterociclo no están sustituidos o pueden llevar 1, 2, 3 o 4 sustituyentes elegidos entre flúor y metilo o bien los radicales R3, R4 o los radicales R5, R6 junto con el átomo de carbono al cual están unidos forman un carbociclo saturado de 3 a 6 integrantes o un heterociclo saturado de 3 a 6 integrantes con 1 o 2 heteroátomos que no son adyacentes como integrantes del anillo, donde el carbociclo y el heterociclo no están sustituidos o pueden llevar 1, 2, 3 o 4 sustituyentes elegidos entre flúor y metilo; A' es un O, NR3a, CR3bR3c o un C2-C3-alcanodiilo lineal, donde una de las porciones CH2 del C2-C3-alcanodiilo puede ser reemplazada por oxígeno o NR3a, y donde 1, 2, 3 o 4 de los átomos de hidrógeno de C2-C3- alcanodiilo pueden ser reemplazados por un radical R3d, donde R3a es hidrógeno o C1-C4-alquilo, R3b, R3c independientemente unos de otros se eligen del grupo que consiste en hidrógeno, halógeno, C1-C4- alquilo o R3b y R3c forman juntos C2-C3-alcanodiilo; R3d se elige del grupo que consiste en halógeno y C1-C4-alquilo.
ES12784578T 2011-11-09 2012-11-08 Inhibidores de la fosfodiesterasa tipo 10A Active ES2620531T3 (es)

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US201161557874P 2011-11-09 2011-11-09
PCT/EP2012/072150 WO2013068470A1 (en) 2011-11-09 2012-11-08 Inhibitors of phosphodiesterase type 10a

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US (3) US20130116241A1 (es)
EP (1) EP2776418B1 (es)
JP (1) JP2014534976A (es)
KR (1) KR20140097318A (es)
CN (1) CN104053654A (es)
AR (1) AR088801A1 (es)
AU (1) AU2012334074A1 (es)
BR (1) BR112014011284A2 (es)
CA (1) CA2852604A1 (es)
CL (1) CL2014001212A1 (es)
CO (1) CO7030959A2 (es)
CR (1) CR20140223A (es)
DO (1) DOP2014000097A (es)
ES (1) ES2620531T3 (es)
GT (1) GT201400089A (es)
HK (1) HK1201519A1 (es)
IL (1) IL232358A0 (es)
MX (1) MX2014005714A (es)
PE (1) PE20141938A1 (es)
RU (1) RU2014123316A (es)
SG (1) SG11201402142VA (es)
TW (1) TW201326153A (es)
UY (1) UY34445A (es)
WO (1) WO2013068470A1 (es)
ZA (1) ZA201402966B (es)

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