AR079497A1 - PHENYLIMIDAZOL DERIVATIVES UNDERSTANDING AN ETHYLLENE BINDER AS ENZYME PDE10A INHIBITORS - Google Patents
PHENYLIMIDAZOL DERIVATIVES UNDERSTANDING AN ETHYLLENE BINDER AS ENZYME PDE10A INHIBITORSInfo
- 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
Links
- ZCUJYXPAKHMBAZ-UHFFFAOYSA-N 2-phenyl-1h-imidazole Chemical class C1=CNC(C=2C=CC=CC=2)=N1 ZCUJYXPAKHMBAZ-UHFFFAOYSA-N 0.000 title 1
- 108090000790 Enzymes Proteins 0.000 title 1
- 102000004190 Enzymes Human genes 0.000 title 1
- 229940123773 Phosphodiesterase 10A inhibitor Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 1
- FNZTVMQDZXRQGK-UHFFFAOYSA-N 1h-benzimidazol-2-yl-(5-phenyl-1h-imidazol-2-yl)methanethiol Chemical compound N=1C2=CC=CC=C2NC=1C(S)C(N1)=NC=C1C1=CC=CC=C1 FNZTVMQDZXRQGK-UHFFFAOYSA-N 0.000 abstract 1
- AWDYUWHHJCNRJN-UHFFFAOYSA-N 2-[(5-phenyl-1h-imidazol-2-yl)methylsulfanyl]-1h-benzimidazole Chemical compound N=1C2=CC=CC=C2NC=1SCC(N1)=NC=C1C1=CC=CC=C1 AWDYUWHHJCNRJN-UHFFFAOYSA-N 0.000 abstract 1
- -1 C1-6 alkyl halogen Chemical class 0.000 abstract 1
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 1
- 101001072037 Homo sapiens cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A Proteins 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 206010013663 drug dependence Diseases 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 208000011117 substance-related disease Diseases 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Addiction (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
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.
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 (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI485151B (en) | 2009-12-17 | 2015-05-21 | Lundbeck & Co As H | Heteroaromatic phenylimidazole derivatives as PDE10A 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 inhibitors of PDE10A enzymes |
| CN107141309A (en) | 2011-01-11 | 2017-09-08 | 桑诺维恩药品公司 | Heteroaryl compound and its application method |
| CN103476757A (en) | 2011-02-18 | 2013-12-25 | 阿勒根公司 | 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 |
| SG11201400759RA (en) * | 2011-09-19 | 2014-07-30 | Hoffmann La Roche | 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) |
| HK1223932A1 (en) * | 2014-01-31 | 2017-08-11 | 豪夫迈‧罗氏有限公司 | (hetero)aryl imidazoles/pyrazoles for treatment of neurological disorders |
| CA2969839A1 (en) * | 2014-12-05 | 2016-06-09 | Subramaniam Ananthan | Heterocyclic compounds as biogenic amine transport modulators |
| EP3226868A4 (en) | 2014-12-05 | 2018-08-15 | Subramaniam Ananthan | Novel quinazolines as biogenic amine transport modulators |
| WO2022238816A1 (en) * | 2021-05-14 | 2022-11-17 | Bm Pharma Consulting Pty. Ltd | Bicyclic heterocyclic compounds for prophylaxis and treatment of viral infections |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030032579A1 (en) | 2001-04-20 | 2003-02-13 | Pfizer Inc. | Therapeutic use of selective PDE10 inhibitors |
| IL149106A0 (en) | 2001-04-20 | 2002-11-10 | Pfizer Prod 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 |
| US20060128695A1 (en) | 2002-10-30 | 2006-06-15 | Neuro3D | Cyclic nucleotide phosphodiesterase inhibitors, preparation and uses |
| DE602004022415D1 (en) | 2003-06-30 | 2009-09-17 | Nycomed Gmbh | PYRROLO DIHYDROISOCHINOLINE DERIVATIVES AS PDE10 INHIBITORS |
| CA2530316A1 (en) | 2003-06-30 | 2005-01-13 | Altana Pharma Ag | Pyrrolodihydroisoquinolines as pde10 inhibitors |
| US20070032404A1 (en) | 2003-07-31 | 2007-02-08 | Bayer Pharmaceuticals Corporation | Methods for treating diabetes and related disorders using pde10a inhibitors |
| CA2556413A1 (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 |
| JP2008501776A (en) | 2004-06-07 | 2008-01-24 | ファイザー・プロダクツ・インク | Inhibition of phosphodiesterase 10 as a treatment for conditions associated with obesity and associated with metabolic syndrome |
| US20060019975A1 (en) | 2004-07-23 | 2006-01-26 | Pfizer Inc | Novel piperidyl derivatives of quinazoline and isoquinoline |
| AU2005282721A1 (en) | 2004-09-03 | 2006-03-16 | Memory Pharmaceuticals Corporation | 4-substituted 4, 6-dialkoxy-cinnoline derivatives as phospodiesterase 10 inhibitors for the treatment of psychiatric or neurological syndroms |
-
2010
- 2010-12-10 TW TW099143188A patent/TW201200516A/en unknown
- 2010-12-15 WO PCT/DK2010/050342 patent/WO2011072695A1/en not_active Ceased
- 2010-12-16 AR ARP100104670A patent/AR079497A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| TW201200516A (en) | 2012-01-01 |
| WO2011072695A1 (en) | 2011-06-23 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |