CL2010001467A1 - Compuestos derivados de fenil-imidazol sustituido con un heteroaromatico biciclico; composicion farmaceutica que los comprende; y su uso como inhibidores de la pde10a para tratar trastornos neurodegenerativos o psiquiatricos como alzheimer, demencia alcoholica, trastorno del aprendizaje, esquizofrenia, adiccion a las drogas. - Google Patents
Compuestos derivados de fenil-imidazol sustituido con un heteroaromatico biciclico; composicion farmaceutica que los comprende; y su uso como inhibidores de la pde10a para tratar trastornos neurodegenerativos o psiquiatricos como alzheimer, demencia alcoholica, trastorno del aprendizaje, esquizofrenia, adiccion a las drogas.Info
- Publication number
- CL2010001467A1 CL2010001467A1 CL2010001467A CL2010001467A CL2010001467A1 CL 2010001467 A1 CL2010001467 A1 CL 2010001467A1 CL 2010001467 A CL2010001467 A CL 2010001467A CL 2010001467 A CL2010001467 A CL 2010001467A CL 2010001467 A1 CL2010001467 A1 CL 2010001467A1
- Authority
- CL
- Chile
- Prior art keywords
- subject
- schizophrenia
- alzheimer
- inhibitors
- pharmaceutical composition
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 208000015122 neurodegenerative disease Diseases 0.000 title abstract 3
- 206010012289 Dementia Diseases 0.000 title abstract 2
- 208000020358 Learning disease Diseases 0.000 title abstract 2
- 230000001476 alcoholic effect Effects 0.000 title abstract 2
- 206010013663 drug dependence Diseases 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 201000003723 learning disability Diseases 0.000 title abstract 2
- 230000000626 neurodegenerative effect Effects 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 208000020016 psychiatric disease Diseases 0.000 title abstract 2
- 201000000980 schizophrenia Diseases 0.000 title abstract 2
- 208000011117 substance-related disease Diseases 0.000 title abstract 2
- SEULWJSKCVACTH-UHFFFAOYSA-N 1-phenylimidazole Chemical group C1=NC=CN1C1=CC=CC=C1 SEULWJSKCVACTH-UHFFFAOYSA-N 0.000 title 1
- 238000000034 method Methods 0.000 abstract 2
- 101001072037 Homo sapiens cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A Proteins 0.000 abstract 1
- 230000002860 competitive effect Effects 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/28—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
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Addiction (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
SE DESCRIBE COMPUESTOS DE FÓRMULA (I), COMPOSICIÓN FARMACÉUTICA QUE COMPRENDE UNA CANTIDAD TERAPÉUTICAMENTE EFECTIVA DE UN COMPUESTO DE LA INVENCIÓN Y UN PORTADOR FARMACÉUTICAMENTE ACEPTABLE. LA PRESENTE INVENCIÓN PROPORCIONA ADEMÁS UN MÉTODO PARA TRATAR UN SUJETO QUE SUFRE UN TRASTORNO NEURODEGENERATIVO, QUE COMPRENDE ADMINISTRAR AL SUJETO UNA CANTIDAD TERAPÉUTICAMENTE EFECTIVA DE UN COMPUESTO DE FÓRMULA 1. LA PRESENTE INVENCIÓN ASIMISMO PROPORCIONA UN MÉTODO PARA TRATAR UN SUJETO QUE SUFRE UNA ADICCIÓN A LAS DROGAS, QUE COMPRENDE ADMINISTRAR AL SUJETO UNA CANTIDAD TERAPÉUTICAMENTE EFECTIVA DE UN COMPUESTO DE FÓRMULA 1. LA PRESENTE INVENCIÓN TAMBIÉN PROPORCIONA UN MÉTODO PARA TRATAR UN SUJETO QUE SUFRE UN TRASTORNO PSIQUIÁTRICO, QUE COMPRENDE ADMINISTRAR AL SUJETO UNA CANTIDAD TERAPÉUTICAMENTE EFECTIVA DE UN COMPUESTO DE FÓRMULA I; Y EL USO DE DICHOS COMO INHIBIDORES DE LA ENZIMA PDE10A PARA EL TRATAMIENTO DE TRASTORNOS NEURODEGENERATIVOS O PSIQUIÁTRICOS COMO ALZHEIMER, DEMENCIA ALCOHÓLICA, TRASTORNO DEL APRENDIZAJE, ESQUIZOFRENIA, ADICCIÓN A IAS DROGAS.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA200800855 | 2008-06-20 | ||
| DKPA200900402 | 2009-03-24 | ||
| DKPA200900519 | 2009-04-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CL2010001467A1 true CL2010001467A1 (es) | 2011-08-05 |
Family
ID=40902594
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2010001467A CL2010001467A1 (es) | 2008-06-20 | 2010-12-17 | Compuestos derivados de fenil-imidazol sustituido con un heteroaromatico biciclico; composicion farmaceutica que los comprende; y su uso como inhibidores de la pde10a para tratar trastornos neurodegenerativos o psiquiatricos como alzheimer, demencia alcoholica, trastorno del aprendizaje, esquizofrenia, adiccion a las drogas. |
| CL2011003205A CL2011003205A1 (es) | 2008-06-20 | 2011-12-16 | Compuesto 5,8-dimetil-2-[2-(1-metil-4-fenil-1h-imidazol-2-il)-etil]-[1,2,4]triazolo[1,5-a]pirazina; composicion farmaceutica; y su uso para el tratamiento de un trastorno neurodegenerativo, tales como alzheimer y demencias. |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2011003205A CL2011003205A1 (es) | 2008-06-20 | 2011-12-16 | Compuesto 5,8-dimetil-2-[2-(1-metil-4-fenil-1h-imidazol-2-il)-etil]-[1,2,4]triazolo[1,5-a]pirazina; composicion farmaceutica; y su uso para el tratamiento de un trastorno neurodegenerativo, tales como alzheimer y demencias. |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US8841297B2 (es) |
| EP (1) | EP2318394B1 (es) |
| JP (1) | JP5930714B2 (es) |
| KR (3) | KR20170016523A (es) |
| CN (2) | CN102124002B (es) |
| AR (1) | AR072199A1 (es) |
| AU (1) | AU2009259209B2 (es) |
| BR (1) | BRPI0915383B8 (es) |
| CA (1) | CA2728335C (es) |
| CL (2) | CL2010001467A1 (es) |
| CO (1) | CO6321263A2 (es) |
| CY (1) | CY1115001T1 (es) |
| DK (1) | DK2318394T3 (es) |
| EA (2) | EA018880B1 (es) |
| ES (1) | ES2456349T3 (es) |
| HR (1) | HRP20140232T1 (es) |
| IL (1) | IL209834A (es) |
| MX (1) | MX2010014136A (es) |
| MY (1) | MY152949A (es) |
| NZ (1) | NZ589926A (es) |
| PL (1) | PL2318394T3 (es) |
| PT (1) | PT2318394E (es) |
| RS (2) | RS53226B (es) |
| SI (1) | SI2318394T1 (es) |
| TW (1) | TWI501965B (es) |
| WO (1) | WO2009152825A1 (es) |
| ZA (1) | ZA201100109B (es) |
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| UA102693C2 (ru) | 2008-06-20 | 2013-08-12 | Х. Луннбек А/С | Производные фенилимидазола как ингибиторы фермента pde10a |
| US8133897B2 (en) | 2008-06-20 | 2012-03-13 | H. Lundbeck A/S | Phenylimidazole derivatives as PDE10A enzyme inhibitors |
| TWI501965B (zh) * | 2008-06-20 | 2015-10-01 | Lundbeck & Co As H | 作為ｐｄｅ１０ａ酵素抑制劑之新穎苯基咪唑衍生物 |
| TWI481607B (zh) * | 2009-12-17 | 2015-04-21 | Lundbeck & Co As H | 作為ｐｄｅ１０ａ酵素抑制劑的２－芳基咪唑衍生物 |
| TWI485151B (zh) * | 2009-12-17 | 2015-05-21 | Lundbeck & Co As H | 作為ｐｄｅ１０ａ酵素抑制劑之雜芳香族苯基咪唑衍生物 |
| KR101713453B1 (ko) * | 2010-03-12 | 2017-03-07 | 오메로스 코포레이션 | Pde10 억제제 및 관련 조성물 및 방법 |
| US8410117B2 (en) * | 2010-03-26 | 2013-04-02 | Hoffmann-La Roche Inc. | Imidazopyrimidine derivatives |
| NZ603789A (en) | 2010-05-26 | 2015-03-27 | Sunovion Pharmaceuticals Inc | Heteroaryl compounds and methods of use thereof |
| TW201215607A (en) | 2010-07-02 | 2012-04-16 | Lundbeck & Co As H | Aryl-and heteroarylamid derivatives as PDE10A enzyme inhibitor |
| TW201206935A (en) | 2010-07-16 | 2012-02-16 | Lundbeck & Co As H | Triazolo-and pyrazoloquinazoline derivatives as PDE10A enzyme inhibitor |
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| US8883788B2 (en) | 2010-08-04 | 2014-11-11 | Takeda Pharmaceutical Company Limited | Fused heterocyclic ring compound |
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| JO3089B1 (ar) | 2010-11-19 | 2017-03-15 | H Lundbeck As | مشتقات ايميدازول كمثبطات لانزيمات pde10a |
| US8552045B2 (en) | 2010-11-19 | 2013-10-08 | H. Lundbeck A/S | Tricyclic imidazole compounds as PDE10 inhibitors |
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| MX2013009575A (es) | 2011-02-18 | 2014-10-14 | Exonhit Therapeutics Sa | Derivados de 6, 7-dialcoxi-3-isoquinolinol sustituidos como inhibidores de fosfodiesterasa 10 (pdei0a). |
| WO2013005798A1 (ja) * | 2011-07-06 | 2013-01-10 | 持田製薬株式会社 | 新規含窒素複素環誘導体 |
| WO2013045607A1 (en) | 2011-09-30 | 2013-04-04 | H. Lundbeck A/S | Quinazoline linked heteroaromatic tricycle derivatives as pde10a enzyme inhibitors |
| WO2013050527A1 (en) | 2011-10-05 | 2013-04-11 | H. Lundbeck A/S | Quinazoline derivatives as pde10a enzyme inhibitors |
| AR089361A1 (es) * | 2011-12-21 | 2014-08-20 | Lundbeck & Co As H | Derivados de quinolina como inhibidores de la enzima pde10a |
| WO2013127817A1 (en) | 2012-02-27 | 2013-09-06 | H. Lundbeck A/S | Imidazole derivatives as pde10a enzyme inhibitors |
| MX2014014468A (es) | 2012-05-30 | 2015-02-12 | Hoffmann La Roche | Compuestos triazolo como inhibidores de fosfodiesterasa 10 (pde10). |
| NZ702239A (en) * | 2012-06-19 | 2017-01-27 | Sunovion Pharmaceuticals Inc | Heteroaryl compounds and methods of use thereof |
| US20140045856A1 (en) | 2012-07-31 | 2014-02-13 | Boehringer Ingelheim International Gmbh | 4-Methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalenes |
| WO2014071044A1 (en) | 2012-11-01 | 2014-05-08 | Allergan, Inc. | Substituted 6,7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde10a) |
| WO2014100533A1 (en) | 2012-12-21 | 2014-06-26 | Bristol-Myers Squibb Company | NOVEL SUBSTITUTED IMIDAZOLES AS CASEIN KINASE 1 δ/ε INHIBITORS |
| CN106957317B (zh) * | 2013-02-27 | 2019-12-31 | 持田制药株式会社 | 新型吡唑衍生物 |
| US9200016B2 (en) | 2013-12-05 | 2015-12-01 | Allergan, Inc. | Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A) |
| RU2659070C9 (ru) | 2014-04-23 | 2018-08-24 | Дарт Нейросайенс (Кайман) Лтд. | ЗАМЕЩЕННЫЕ [1,2,4]ТРИАЗОЛО[1,5-a]ПИРИМИДИН-7-ИЛЬНЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE2 |
| NZ630810A (en) | 2014-04-28 | 2016-03-31 | Omeros Corp | Processes and intermediates for the preparation of a pde10 inhibitor |
| NZ630803A (en) | 2014-04-28 | 2016-03-31 | Omeros Corp | Optically active pde10 inhibitor |
| PL408251A1 (pl) * | 2014-05-19 | 2015-11-23 | Celon Pharma Spółka Z Ograniczoną Odpowiedzialnością | Skondensowane pochodne triazolu jako inhibitory fosfodiesterazy 10A |
| US10239882B2 (en) | 2014-11-05 | 2019-03-26 | Dart Neuroscience (Cayman) Ltd. | Substituted 5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-amine compounds as PDE2 inhibitors |
| JP2018513153A (ja) | 2015-04-24 | 2018-05-24 | オメロス コーポレーション | Ｐｄｅ１０インヒビターならびに関連する組成物および方法 |
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| WO2020094591A1 (en) | 2018-11-06 | 2020-05-14 | H. Lundbeck A/S | Pde10a inhibitors for treating negative symptoms and cognitive impairments in a patient suffering from schizophrenia |
| BR112020013743A2 (pt) | 2018-11-06 | 2020-12-01 | H. Lundbeck A/S | hemiadipato de 5,8-dimetil-2-[2-(1-metil-4-fenil-1h-imidazol-2-il)-etil]-[1,2,4]triazolo[1,5-a]pirazina |
| BR112020013697A2 (pt) | 2018-11-06 | 2020-12-01 | H. Lundbeck A/S | compostos para tratamento de sintomas negativos e comprometimentos cognitivos |
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| TWI501965B (zh) * | 2008-06-20 | 2015-10-01 | Lundbeck & Co As H | 作為ｐｄｅ１０ａ酵素抑制劑之新穎苯基咪唑衍生物 |
| US8133897B2 (en) | 2008-06-20 | 2012-03-13 | H. Lundbeck A/S | Phenylimidazole derivatives as PDE10A enzyme inhibitors |
| UA102693C2 (ru) | 2008-06-20 | 2013-08-12 | Х. Луннбек А/С | Производные фенилимидазола как ингибиторы фермента pde10a |
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