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Quinoline derivatives as inhibitors of pde10a Enzyme
专利权人:
H. LUNDBECK A/S
发明人:
申请号:
ARP120104861
公开号:
AR089361A1
申请日:
2012.12.20
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
This provides quinoline Derivatives of formula (1) are pde10a Enzyme inhibitors and, as such, are useful for treating neurodegenerative and Psychiatric Disorders. In particular, this provides compounds that are highly Selective PDE10 on other subtypes of PDE.This also provides Pharmaceutical compositions comprising the compounds and Methods of using the compounds to treat disorders of the Mind.Claim 1: a compound having the structure of formula (1) where r u00b9, R u00b2, r u00b3, r u2074, r u2075 and r u2076 individually selected in the group consisting of hydrogen, hydroxyl alkyl, cyano, c u2081 u208b u2086 c u2081 u208b u2086, alkoxy, halogen, methylenedioxy, difluorometilendioxi and ethylenedioxy, Where l is a Connector between ch u2082 ch u2082 - - - selected and - ch = CH - Where Het is selected from the group of formulas (2),Where one or more of the Hydrogen Atoms attached to carbon in the het can be optionally replaced with up to three r u2077 r u2078 substituents, and r u2079 selected individually c u2081 u208b u2086 Halogen, alkyl, cyano, haloalquilo c u2081 u208b u2086, aryl alkoxy, and hidroxialquilo c u2081 u208b u2086 and Gift * marks the point of Union; and pharmaceutically acceptable Salts and their taut u00f3meros and its polymorphic forms.La presente proporciona derivados de quinolina de fórmula (1) que son inhibidores de la enzima PDE10A y, como tales, son útiles para tratar trastornos psiquiátricos y neurodegenerativos. En especial, la presente proporciona compuestos que son altamente selectivos para PDE10 respecto de otros subtipos de PDE. La presente proporciona además composiciones farmacéuticas que comprenden compuestos de la presente y métodos para tratar trastornos empleando los compuestos de la presente. Reivindicación 1: Un compuesto que tiene la estructura de fórmula (1) donde R¹, R², R³, R⁴, R⁵ y R⁶ se seleccionan en forma individual del grupo integrado por hidrógeno, hidroxilo, ciano, alquilo C₁₋₆, alcoxi C₁₋₆, halógeno, metilendioxi,
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