AR079497A1 - PHENYLIMIDAZOL DERIVATIVES UNDERSTANDING AN ETHYLLENE BINDER AS ENZYME PDE10A INHIBITORS - Google Patents

PHENYLIMIDAZOL DERIVATIVES UNDERSTANDING AN ETHYLLENE BINDER AS ENZYME PDE10A INHIBITORS

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Publication number
AR079497A1
AR079497A1 ARP100104670A ARP100104670A AR079497A1 AR 079497 A1 AR079497 A1 AR 079497A1 AR P100104670 A ARP100104670 A AR P100104670A AR P100104670 A ARP100104670 A AR P100104670A AR 079497 A1 AR079497 A1 AR 079497A1
Authority
AR
Argentina
Prior art keywords
alkyl
ethyllene
phenylimidazol
binder
derivatives
Prior art date
Application number
ARP100104670A
Other languages
Spanish (es)
Original Assignee
Lundbeck & Co As H
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 Lundbeck & Co As H filed Critical Lundbeck & Co As H
Publication of AR079497A1 publication Critical patent/AR079497A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • 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
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • 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

Abstract

Compuestos, que son inhibidores de la enzima PDE10A. Se proporciona una composicion farmacéutica que comprende una cantidad terapéuticamente efectiva de un de estos compuestos y un portador farmacéuticamente aceptable. Su utilizacion para tratar trastornos neurodegenerativos el uso de los mismos en el tratamiento de adiccion a las drogas. Reivindicacion 1: Un compuesto que tiene la estructura 1 en donde HET es un grupo heteroaromático de la formula 2 que contiene de 2 a 4 átomos de nitrogeno: en donde Y puede ser N o CH, Z puede ser N o C, y en donde HET puede sustituirse opcionalmente con hasta tres sustituyentes R7-R9 individualmente seleccionados de hidrogeno, alquilo C1-6 halogeno; ciano, haloalquilo C1-6; arilo, alcoxi e hidroxialquilo C1-6, y en donde * denota el punto de union, -L- es el enlazante -C=C-, R1 se selecciona de H, alquilo C1-6 alquil C1-6 cicloalquilo C3-8; hidroxialquilo C1-6, CH2CN, CH2C(O)NH2, arilalquilo C1-6, y alquil C1-6- heterocicloalquilo, R2-R6 son individualmente seleccionados de H, alcoxi C1-6 y halogeno, y tautomeros y sales farmacéuticamente aceptables de los mismos, y formas polimorficas de los mismos, siempre que el compuesto no sea 2-(5-fenil-1H-imidazol-2-ilmetilsulfanil)-1H-benzoimidazol o 2-(5-fenil-1H-imidazol-2-il-sulfanil-metil)-1H-benzoimidazol.Compounds, which are inhibitors of the PDE10A enzyme. A pharmaceutical composition is provided comprising a therapeutically effective amount of one of these compounds and a pharmaceutically acceptable carrier. Its use to treat neurodegenerative disorders use them in the treatment of drug addiction. Claim 1: A compound having structure 1 wherein HET is a heteroaromatic group of formula 2 containing from 2 to 4 nitrogen atoms: wherein Y can be N or CH, Z can be N or C, and wherein HET may optionally be substituted with up to three individually selected R7-R9 substituents of hydrogen, C1-6 alkyl halogen; cyano, C1-6 haloalkyl; aryl, C1-6 alkoxy and hydroxyalkyl, and where * denotes the point of attachment, -L- is the linker -C = C-, R1 is selected from H, C1-6 alkyl C1-6 alkyl C3-8 cycloalkyl; C1-6 hydroxyalkyl, CH2CN, CH2C (O) NH2, C1-6 arylalkyl, and C1-6-alkylcycloalkyl, R2-R6 are individually selected from H, C1-6 alkoxy and halogen, and pharmaceutically acceptable tautomers and salts of the same, and polymorphic forms thereof, provided that the compound is not 2- (5-phenyl-1H-imidazol-2-ylmethylsulfanyl) -1H-benzoimidazole or 2- (5-phenyl-1H-imidazol-2-yl- sulfanyl-methyl) -1H-benzoimidazole.

ARP100104670A 2009-12-17 2010-12-16 PHENYLIMIDAZOL DERIVATIVES UNDERSTANDING AN ETHYLLENE BINDER AS ENZYME PDE10A INHIBITORS AR079497A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DKPA200901342 2009-12-17

Publications (1)

Publication Number Publication Date
AR079497A1 true AR079497A1 (en) 2012-02-01

Family

ID=44246809

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100104670A AR079497A1 (en) 2009-12-17 2010-12-16 PHENYLIMIDAZOL DERIVATIVES UNDERSTANDING AN ETHYLLENE BINDER AS ENZYME PDE10A INHIBITORS

Country Status (3)

Country Link
AR (1) AR079497A1 (en)
TW (1) TW201200516A (en)
WO (1) WO2011072695A1 (en)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI485151B (en) 2009-12-17 2015-05-21 Lundbeck & Co As H Heteroaromatic phenylimidazole derivatives as pde 10a enzyme inhibitors
US8552045B2 (en) 2010-11-19 2013-10-08 H. Lundbeck A/S Tricyclic imidazole compounds as PDE10 inhibitors
JO3089B1 (en) * 2010-11-19 2017-03-15 H Lundbeck As Imidazole derivatives as PDE10A enzyme inhibitors
ES2627788T3 (en) 2011-01-11 2017-07-31 Sunovion Pharmaceuticals Inc. Heteroaryl compounds and methods of use thereof
MX2013009575A (en) 2011-02-18 2014-10-14 Exonhit Therapeutics Sa Substituted 6,7-dialkoxy-3-isoquinolinol derivatives as inhibitors of phosphodiesterase 10 (pde10a).
US8592423B2 (en) * 2011-06-21 2013-11-26 Bristol-Myers Squibb Company Inhibitors of PDE10
US8975276B2 (en) 2011-06-29 2015-03-10 Bristol-Myers Squibb Company Inhibitors of PDE10
ES2626801T3 (en) * 2011-09-19 2017-07-26 F. Hoffmann-La Roche Ag Triazolopyridine compounds as pde10a inhibitors
WO2014071044A1 (en) 2012-11-01 2014-05-08 Allergan, Inc. Substituted 6,7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde10a)
US9200016B2 (en) 2013-12-05 2015-12-01 Allergan, Inc. Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A)
CA2935065A1 (en) * 2014-01-31 2015-08-06 F. Hoffmann-La Roche Ag (hetero)aryl imidazoles/pyrazoles for treatment of neurological disorders
AU2015357596A1 (en) 2014-12-05 2017-06-29 Southern Research Institute Heterocyclic compounds as biogenic amine transport modulators
JP2018509378A (en) 2014-12-05 2018-04-05 サウザーン リサーチ インスチチュート Novel quinazolines as biogenic amine transport modulators

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IL149106A0 (en) 2001-04-20 2002-11-10 Pfizer Prod Inc Therapeutic use of selective pde10 inhibitors
US20030032579A1 (en) 2001-04-20 2003-02-13 Pfizer Inc. Therapeutic use of selective PDE10 inhibitors
FR2824065A1 (en) 2001-04-26 2002-10-31 Neuro3D COMPOUNDS INHIBITORS OF CYCLIC NUCLEOTIDE PHOSPHODIESTERASES, PREPARATION AND USES
AU2003288352A1 (en) 2002-10-30 2004-06-07 Centre National De La Recherche Scientifique (Cnrs) Cyclic nucleotide phosphodiesterase inhibitors, preparation and uses
UA86591C2 (en) 2003-06-30 2009-05-12 Алтана Фарма Аг Pyrrolodihydroisoquinolines as pde10 inhibitors, pharmaceutical composition based thereon
ATE438398T1 (en) 2003-06-30 2009-08-15 Nycomed Gmbh PYRROLO-DIHYDROISOCINOLINE DERIVATIVES AS PDE10 INHIBITORS
US20070032404A1 (en) 2003-07-31 2007-02-08 Bayer Pharmaceuticals Corporation Methods for treating diabetes and related disorders using pde10a inhibitors
WO2005082883A2 (en) 2004-02-18 2005-09-09 Pfizer Products Inc. Tetrahydroisoquinolinyl derivatives of quinazoline and isoquinoline
FR2870539B1 (en) 2004-05-19 2006-08-04 Greenpharma Sa Sa NEW METHODS AND MEDICINES
WO2005120514A1 (en) 2004-06-07 2005-12-22 Pfizer Products Inc. Phosphodiesterase 10 inhibition as treatment for obesity-related and metabolic syndrome-related conditions
US20060019975A1 (en) 2004-07-23 2006-01-26 Pfizer Inc Novel piperidyl derivatives of quinazoline and isoquinoline
EP1802585A1 (en) 2004-09-03 2007-07-04 Memory Pharmaceuticals Corporation 4-substituted 4,6-dialkoxy-cinnoline derivatives as phospodiesterase 10 inhibitors for the treatment of psychiatric or neurological syndroms

Also Published As

Publication number Publication date
WO2011072695A1 (en) 2011-06-23
TW201200516A (en) 2012-01-01

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