BR112012014486A2 - derivados de aril triazol heteroaromático como inibidaores de enzima pde10a - Google Patents
derivados de aril triazol heteroaromático como inibidaores de enzima pde10aInfo
- Publication number
- BR112012014486A2 BR112012014486A2 BR112012014486A BR112012014486A BR112012014486A2 BR 112012014486 A2 BR112012014486 A2 BR 112012014486A2 BR 112012014486 A BR112012014486 A BR 112012014486A BR 112012014486 A BR112012014486 A BR 112012014486A BR 112012014486 A2 BR112012014486 A2 BR 112012014486A2
- Authority
- BR
- Brazil
- Prior art keywords
- formula
- enzyme inhibitors
- subject
- compound
- effective amount
- Prior art date
Links
Classifications
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- 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
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
-
- 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
-
- 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
- A61P25/36—Opioid-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
- C07D403/12—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
-
- 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
Abstract
derivados de aril triazol heteroaromático como inibidores de enzima pde10a esta invenção é dirigida aos compostos (fórmula 1), que são inibidores de enzima pde10a. a invenção fornece uma composição farmacêutica compreendendo uma quantidade terapeuticamente eficaz de um composto da invenção e um portador farmaceuticamente aceitável. a presente invenção também fornece processos para a perparação dos compostos da fórmula (i). a presente invenção fornece ainda um método de tratar um indivíduo que sofre de um transtorno neurodegenerativo compreendendo administrar ao indivíduo uma quantidade terapeuticamente eficaz de um composto da fórmula (i). a presente invenção também fornece um método de tratar um indivíduo que sofre de um vício compreendendo administrar ao invidíduo uma quantidade terapeuticamente eficaz de um composto da fórmula (i). a presente invenção fornece ainda um método de tratar um indivíduo que sofre de um transtorno psiquiátrico compreendendo administrar ao indivíduo uma quantidade terapeuticamente eficaz de um composto da fórmula (i).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA200901340 | 2009-12-17 | ||
| PCT/DK2010/050344 WO2011072697A1 (en) | 2009-12-17 | 2010-12-15 | Heteroaromatic aryl triazole derivatives as pde10a enzyme inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112012014486A2 true BR112012014486A2 (pt) | 2017-04-04 |
Family
ID=44246811
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112012014486A BR112012014486A2 (pt) | 2009-12-17 | 2010-12-15 | derivados de aril triazol heteroaromático como inibidaores de enzima pde10a |
Country Status (36)
| Country | Link |
|---|---|
| US (2) | US8501795B2 (pt) |
| EP (1) | EP2513106B1 (pt) |
| JP (1) | JP6035149B2 (pt) |
| KR (1) | KR101779629B1 (pt) |
| CN (1) | CN102753550B (pt) |
| AR (1) | AR079496A1 (pt) |
| AU (1) | AU2010333438B2 (pt) |
| BR (1) | BR112012014486A2 (pt) |
| CA (1) | CA2783728C (pt) |
| CO (1) | CO6602117A2 (pt) |
| CR (1) | CR20120318A (pt) |
| CY (1) | CY1116361T1 (pt) |
| DK (1) | DK2513106T3 (pt) |
| DO (1) | DOP2012000169A (pt) |
| EA (1) | EA021606B1 (pt) |
| ES (1) | ES2442179T3 (pt) |
| GE (1) | GEP20146201B (pt) |
| GT (1) | GT201200193A (pt) |
| HK (1) | HK1177745A1 (pt) |
| HR (1) | HRP20131210T1 (pt) |
| IL (1) | IL220328A (pt) |
| MA (1) | MA33923B1 (pt) |
| MX (1) | MX2012006715A (pt) |
| MY (1) | MY156520A (pt) |
| NZ (1) | NZ600365A (pt) |
| PL (1) | PL2513106T3 (pt) |
| PT (1) | PT2513106E (pt) |
| RS (1) | RS53101B (pt) |
| SG (1) | SG181672A1 (pt) |
| SI (1) | SI2513106T1 (pt) |
| SM (1) | SMT201400009B (pt) |
| TN (1) | TN2012000278A1 (pt) |
| TW (1) | TWI487705B (pt) |
| UA (1) | UA107950C2 (pt) |
| WO (1) | WO2011072697A1 (pt) |
| ZA (1) | ZA201204420B (pt) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| TWI487705B (zh) * | 2009-12-17 | 2015-06-11 | Lundbeck & Co As H | 作為ｐｄｅ１０ａ酵素抑制劑之雜芳香族芳基三唑衍生物 |
| 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 |
| US8765760B2 (en) | 2011-01-11 | 2014-07-01 | Sunovion Pharmaceuticals, Inc. | [1,2,4] triazol [1,5-a] pyrazines useful as inhibitors of phosphodiesterases |
| SG192839A1 (en) | 2011-02-18 | 2013-09-30 | Allergan Inc | Substituted 6,7-dialkoxy-3-isoquinolinol derivatives as inhibitors of phosphodiesterase 10 (pde10a) |
| KR101584925B1 (ko) * | 2011-09-19 | 2016-01-12 | 에프. 호프만-라 로슈 아게 | Pde10a 억제제로서의 트라이아졸로피리딘 화합물 |
| WO2013127817A1 (en) | 2012-02-27 | 2013-09-06 | H. Lundbeck A/S | Imidazole derivatives as pde10a enzyme inhibitors |
| EA201492069A1 (ru) | 2012-05-30 | 2015-03-31 | Ф.Хоффманн-Ля Рош Аг | Соединения триазола в качестве ингибиторов фосфодиэстеразы 10 (pde10) |
| AU2013277258B2 (en) * | 2012-06-19 | 2017-12-07 | Sunovion Pharmaceuticals Inc. | Heteroaryl compounds and methods of use thereof |
| WO2014071044A1 (en) | 2012-11-01 | 2014-05-08 | Allergan, Inc. | Substituted 6,7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde10a) |
| EP2919781B1 (en) | 2012-11-15 | 2017-06-28 | Merck Sharp & Dohme Corp. | Cyclobutyl benzimidazoles as pde10 inhibitors |
| JP2017501135A (ja) * | 2013-11-28 | 2017-01-12 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | イミダゾール誘導体 |
| US9200016B2 (en) | 2013-12-05 | 2015-12-01 | Allergan, Inc. | Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A) |
| CN114671874B (zh) * | 2021-08-30 | 2024-02-02 | 济南爱思医药科技有限公司 | 一种具有抗肿瘤活性的茶碱乙酸衍生物及其制备方法与应用 |
| WO2023064458A1 (en) * | 2021-10-13 | 2023-04-20 | Yale University | Selective jak2 inhibitors and methods of use |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1462521A (en) | 1974-02-11 | 1977-01-26 | Wyeth John & Brother Ltd | Triazole derivatives |
| GB8307865D0 (en) | 1983-03-22 | 1983-04-27 | Fujisawa Pharmaceutical Co | Benzimidazole derivatives |
| US5571775A (en) | 1994-07-11 | 1996-11-05 | Dowelanco | N-aryl[1,2,4]triazolo[1,5-a]pyridine-2-sulfonamide herbicides |
| US6699853B2 (en) | 1997-06-16 | 2004-03-02 | Hoechst Schering Agrevo Gmbh | 4-haloalkyl-3-heterocyclylpyridines, 4-haloalkyl-5-heterocyclyl-pyrimidines and 4-trifluoromethyl-3-oxadiazolylpyridines, processes for their preparation, compositions comprising them, and their use as pesticides |
| SE9802937D0 (sv) | 1998-09-01 | 1998-09-01 | Astra Pharma Prod | Novel compounds |
| 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 (fr) | 2001-04-26 | 2002-10-31 | Neuro3D | Composes inhibiteurs des phosphodiesterases des nucleotides cycliques, preparation et utilisations |
| ES2315546T3 (es) | 2002-10-30 | 2009-04-01 | Via Pharmaceuticals, Inc. | Inhibidores delas fosfodiesterasas de los nucleotidos ciclicos, que presentan una estructura de benzodiazepina, y su uso en terapia. |
| AU2004253690B2 (en) | 2003-06-30 | 2010-03-25 | Nycomed Gmbh | Pyrrolodihydroisoquinolines as PDE10 inhibitors |
| ES2331519T3 (es) | 2003-06-30 | 2010-01-07 | Nycomed Gmbh | Derivados de pirrolo-dihidroisoquinolina como inhibidores de pde10. |
| WO2005012485A2 (en) | 2003-07-31 | 2005-02-10 | Bayer Pharmaceuticals Corporation | Methods for treating diabetes and related disorders using pde10a inhibitors |
| BRPI0507839A (pt) | 2004-02-18 | 2007-05-08 | Pfizer Prod Inc | derivados tetraidroisoquinolinil de quinazolina e isoquinolina |
| FR2870539B1 (fr) | 2004-05-19 | 2006-08-04 | Greenpharma Sa Sa | Nouvelles methodes et medicaments |
| 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 |
| CA2578996A1 (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 |
| NL2000397C2 (nl) * | 2006-01-05 | 2007-10-30 | Pfizer Prod Inc | Bicyclische heteroarylverbindingen als PDE10 inhibitoren. |
| US20080090834A1 (en) * | 2006-07-06 | 2008-04-17 | Pfizer Inc | Selective azole pde10a inhibitor compounds |
| EP2057153B1 (en) * | 2006-07-10 | 2012-09-12 | H. Lundbeck A/S | (3-aryl-piperazin-1-yl) derivatives of 6,7-dialkoxyquinazoline, 6,7- dialkoxyphtalazine and 6,7-dialkoxyisoquinoline |
| AU2008276521B2 (en) | 2007-07-17 | 2011-11-03 | Amgen Inc. | Heterocyclic modulators of PKB |
| GB0800411D0 (en) | 2008-01-10 | 2008-02-20 | Glaxo Group Ltd | Novel compounds |
| TWI487705B (zh) | 2009-12-17 | 2015-06-11 | Lundbeck & Co As H | 作為ｐｄｅ１０ａ酵素抑制劑之雜芳香族芳基三唑衍生物 |
| 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 |
| AU2011258217B2 (en) * | 2010-05-26 | 2016-12-15 | Sunovion Pharmaceuticals Inc. | Heteroaryl compounds and methods of use thereof |
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2010
- 2010-12-13 TW TW099143441A patent/TWI487705B/zh not_active IP Right Cessation
- 2010-12-15 MY MYPI2012002595A patent/MY156520A/en unknown
- 2010-12-15 US US13/515,351 patent/US8501795B2/en not_active Expired - Fee Related
- 2010-12-15 MX MX2012006715A patent/MX2012006715A/es active IP Right Grant
- 2010-12-15 PT PT107979916T patent/PT2513106E/pt unknown
- 2010-12-15 NZ NZ600365A patent/NZ600365A/xx not_active IP Right Cessation
- 2010-12-15 EA EA201290517A patent/EA021606B1/ru not_active IP Right Cessation
- 2010-12-15 CA CA2783728A patent/CA2783728C/en not_active Expired - Fee Related
- 2010-12-15 MA MA35064A patent/MA33923B1/fr unknown
- 2010-12-15 SG SG2012043493A patent/SG181672A1/en unknown
- 2010-12-15 PL PL10797991T patent/PL2513106T3/pl unknown
- 2010-12-15 AU AU2010333438A patent/AU2010333438B2/en not_active Ceased
- 2010-12-15 EP EP10797991.6A patent/EP2513106B1/en active Active
- 2010-12-15 DK DK10797991.6T patent/DK2513106T3/da active
- 2010-12-15 WO PCT/DK2010/050344 patent/WO2011072697A1/en active Application Filing
- 2010-12-15 BR BR112012014486A patent/BR112012014486A2/pt not_active Application Discontinuation
- 2010-12-15 ES ES10797991.6T patent/ES2442179T3/es active Active
- 2010-12-15 GE GEAP201012784A patent/GEP20146201B/en unknown
- 2010-12-15 CN CN201080064069.0A patent/CN102753550B/zh not_active Expired - Fee Related
- 2010-12-15 KR KR1020127015379A patent/KR101779629B1/ko active IP Right Grant
- 2010-12-15 SI SI201030474T patent/SI2513106T1/sl unknown
- 2010-12-15 RS RS20130588A patent/RS53101B/en unknown
- 2010-12-15 UA UAA201207980A patent/UA107950C2/uk unknown
- 2010-12-15 JP JP2012543477A patent/JP6035149B2/ja not_active Expired - Fee Related
- 2010-12-16 AR ARP100104669A patent/AR079496A1/es unknown
-
2012
- 2012-05-31 TN TNP2012000278A patent/TN2012000278A1/en unknown
- 2012-06-12 IL IL220328A patent/IL220328A/en not_active IP Right Cessation
- 2012-06-12 CR CR20120318A patent/CR20120318A/es unknown
- 2012-06-13 GT GT201200193A patent/GT201200193A/es unknown
- 2012-06-15 DO DO2012000169A patent/DOP2012000169A/es unknown
- 2012-06-15 CO CO12101114A patent/CO6602117A2/es active IP Right Grant
- 2012-06-15 ZA ZA2012/04420A patent/ZA201204420B/en unknown
-
2013
- 2013-04-23 HK HK13104921.1A patent/HK1177745A1/xx not_active IP Right Cessation
- 2013-06-20 US US13/922,371 patent/US8785653B2/en not_active Expired - Fee Related
- 2013-12-19 HR HRP20131210AT patent/HRP20131210T1/hr unknown
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2014
- 2014-01-07 CY CY20141100012T patent/CY1116361T1/el unknown
- 2014-01-22 SM SM201400009T patent/SMT201400009B/xx unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] |
Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI |
|
| B06T | Formal requirements before examination [chapter 6.20 patent gazette] | ||
| B11E | Dismissal acc. art. 34 of ipl - requirements for examination incomplete | ||
| B11T | Dismissal of application maintained [chapter 11.20 patent gazette] |