AR079496A1 - Derivados de aril triazol heteroaromaticos como inhibidores de enzima pde10a - Google Patents
Derivados de aril triazol heteroaromaticos como inhibidores de enzima pde10aInfo
- Publication number
- AR079496A1 AR079496A1 ARP100104669A ARP100104669A AR079496A1 AR 079496 A1 AR079496 A1 AR 079496A1 AR P100104669 A ARP100104669 A AR P100104669A AR P100104669 A ARP100104669 A AR P100104669A AR 079496 A1 AR079496 A1 AR 079496A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- formula
- provides
- subject
- 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
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- 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
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- 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
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- 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
La presente se dirige a compuestos, que son inhibidores de la enzima PDE10A. Proporciona una composicion farmacéutica que comprende una cantidad terapéuticamente efectiva de un compuesto y un portador farmacéuticamente aceptable. La presente también proporciona procesos para la preparacion de los compuestos de la formula 1. La presente además proporciona un método de tratar un sujeto que padece de un trastorno neurodegenerativo que comprende la administracion al sujeto de una cantidad terapéuticamente efectiva de un compuesto de la formula 1. La presente también proporciona un método para tratar a un sujeto que padece de adiccion a las drogas que comprende la administracion a un sujeto de una cantidad terapéuticamente efectiva de un compuesto de la formula 1. La presente además proporciona un método para tratar a un sujeto que padece de un trastorno psiquiátrico que comprende la administracion al sujeto de una cantidad terapéuticamente efectiva de un compuesto de la formula 1. Reivindicacion 1: Un compuesto que tiene la estructura 1 en donde HET-1 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-1 puede sustituirse opcionalmente con hasta tres sustituyentes R2-R4 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, Q es un fenilo, opcionalmente sustituido con uno a cinco sustituyentes, o un grupo heteroaromático de 5 o 6 miembros monocíclico que contiene 1 o 2 heteroátomos. -L- es un enlazante seleccionado de -S-CH2-, -CH2-S-, -CH2-CH2- -CH=CH-, , -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, y tautomeros y sales farmacéuticamente aceptables de los mismos, y formas polimorficas de los mismos, con la condicion de que cuando el enlazante (L) es -CH2-S- entonces HET-1 no es ni imidazol[1,2-a]piridina ni imidazol[1,2-a]pirimidina.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA200901340 | 2009-12-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR079496A1 true AR079496A1 (es) | 2012-02-01 |
Family
ID=44246811
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100104669A AR079496A1 (es) | 2009-12-17 | 2010-12-16 | Derivados de aril triazol heteroaromaticos como inhibidores de enzima pde10a |
Country Status (36)
| Country | Link |
|---|---|
| US (2) | US8501795B2 (es) |
| EP (1) | EP2513106B1 (es) |
| JP (1) | JP6035149B2 (es) |
| KR (1) | KR101779629B1 (es) |
| CN (1) | CN102753550B (es) |
| AR (1) | AR079496A1 (es) |
| AU (1) | AU2010333438B2 (es) |
| BR (1) | BR112012014486A2 (es) |
| CA (1) | CA2783728C (es) |
| CO (1) | CO6602117A2 (es) |
| CR (1) | CR20120318A (es) |
| CY (1) | CY1116361T1 (es) |
| DK (1) | DK2513106T3 (es) |
| DO (1) | DOP2012000169A (es) |
| EA (1) | EA021606B1 (es) |
| ES (1) | ES2442179T3 (es) |
| GE (1) | GEP20146201B (es) |
| GT (1) | GT201200193A (es) |
| HK (1) | HK1177745A1 (es) |
| HR (1) | HRP20131210T1 (es) |
| IL (1) | IL220328A (es) |
| MA (1) | MA33923B1 (es) |
| MX (1) | MX2012006715A (es) |
| MY (1) | MY156520A (es) |
| NZ (1) | NZ600365A (es) |
| PL (1) | PL2513106T3 (es) |
| PT (1) | PT2513106E (es) |
| RS (1) | RS53101B (es) |
| SG (1) | SG181672A1 (es) |
| SI (1) | SI2513106T1 (es) |
| SM (1) | SMT201400009B (es) |
| TN (1) | TN2012000278A1 (es) |
| TW (1) | TWI487705B (es) |
| UA (1) | UA107950C2 (es) |
| WO (1) | WO2011072697A1 (es) |
| ZA (1) | ZA201204420B (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| EP3210984B1 (en) | 2011-01-11 | 2019-06-19 | Sunovion Pharmaceuticals Inc. | Heteroaryl compounds and methods of use thereof |
| WO2012112946A1 (en) | 2011-02-18 | 2012-08-23 | Allergan, Inc. | Substituted 6,7-dialkoxy-3-isoquinolinol derivatives as inhibitors of phosphodiesterase 10 (pde10a) |
| AU2012311713A1 (en) * | 2011-09-19 | 2014-03-13 | F. Hoffmann-La Roche Ag | Triazolopyridine compounds as PDE10A inhibitors |
| 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). |
| CA2874180A1 (en) * | 2012-06-19 | 2013-12-27 | 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) |
| US9284302B2 (en) | 2012-11-15 | 2016-03-15 | Merck Sharp & Dohme Corp. | Cyclobutyl benzimidazoles as PDE 10 inhibitors |
| RU2016123329A (ru) * | 2013-11-28 | 2018-01-10 | Ф. Хоффманн-Ля Рош Аг | Производные имидазола |
| 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 |
| 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 (fr) | 2001-04-26 | 2002-10-31 | Neuro3D | Composes inhibiteurs des phosphodiesterases des nucleotides cycliques, preparation et utilisations |
| WO2004041258A2 (fr) | 2002-10-30 | 2004-05-21 | Neuro3D | Utilisation d’inhibiteurs des phosphodiesterases des nucleotides cycliques, ayant une structure benzodiazepinique en therapie |
| ES2331519T3 (es) | 2003-06-30 | 2010-01-07 | Nycomed Gmbh | Derivados de pirrolo-dihidroisoquinolina como inhibidores de pde10. |
| EP1641794A1 (en) | 2003-06-30 | 2006-04-05 | ALTANA Pharma AG | Novel pyrrolodihydroisoquinolines useful in the treatment of cancer |
| US20070032404A1 (en) | 2003-07-31 | 2007-02-08 | Bayer Pharmaceuticals Corporation | Methods for treating diabetes and related disorders using pde10a inhibitors |
| JP2007523152A (ja) | 2004-02-18 | 2007-08-16 | ファイザー・プロダクツ・インク | キナゾリンおよびイソキノリンのテトラヒドロイソキノリニル誘導体 |
| FR2870539B1 (fr) | 2004-05-19 | 2006-08-04 | Greenpharma Sa Sa | Nouvelles methodes et medicaments |
| CA2568929A1 (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 |
| 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 |
| 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 |
| ES2392553T3 (es) * | 2006-07-10 | 2012-12-11 | H. Lundbeck A/S | Derivados (3-aril-piperazina-1-ilo) de 6,7-dialcoxiquinazolina, 6,7-dialcoxiftalazina y 6,7-dialcoxiisoquinolina |
| JP2010533715A (ja) | 2007-07-17 | 2010-10-28 | アムジエン・インコーポレーテツド | 複素環系ｐｋｂ調節剤 |
| GB0800411D0 (en) | 2008-01-10 | 2008-02-20 | Glaxo Group Ltd | Novel compounds |
| 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 |
| NZ603789A (en) * | 2010-05-26 | 2015-03-27 | 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 NZ NZ600365A patent/NZ600365A/xx not_active IP Right Cessation
- 2010-12-15 AU AU2010333438A patent/AU2010333438B2/en not_active Ceased
- 2010-12-15 BR BR112012014486A patent/BR112012014486A2/pt not_active Application Discontinuation
- 2010-12-15 CA CA2783728A patent/CA2783728C/en not_active Expired - Fee Related
- 2010-12-15 ES ES10797991.6T patent/ES2442179T3/es active Active
- 2010-12-15 CN CN201080064069.0A patent/CN102753550B/zh not_active Expired - Fee Related
- 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 RS RS20130588A patent/RS53101B/en unknown
- 2010-12-15 WO PCT/DK2010/050344 patent/WO2011072697A1/en active Application Filing
- 2010-12-15 MA MA35064A patent/MA33923B1/fr unknown
- 2010-12-15 EP EP10797991.6A patent/EP2513106B1/en active Active
- 2010-12-15 KR KR1020127015379A patent/KR101779629B1/ko active IP Right Grant
- 2010-12-15 SI SI201030474T patent/SI2513106T1/sl unknown
- 2010-12-15 GE GEAP201012784A patent/GEP20146201B/en unknown
- 2010-12-15 DK DK10797991.6T patent/DK2513106T3/da active
- 2010-12-15 UA UAA201207980A patent/UA107950C2/uk unknown
- 2010-12-15 PT PT107979916T patent/PT2513106E/pt unknown
- 2010-12-15 JP JP2012543477A patent/JP6035149B2/ja not_active Expired - Fee Related
- 2010-12-15 SG SG2012043493A patent/SG181672A1/en unknown
- 2010-12-15 EA EA201290517A patent/EA021606B1/ru not_active IP Right Cessation
- 2010-12-15 PL PL10797991T patent/PL2513106T3/pl unknown
- 2010-12-15 MY MYPI2012002595A patent/MY156520A/en unknown
- 2010-12-16 AR ARP100104669A patent/AR079496A1/es unknown
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2012
- 2012-05-31 TN TNP2012000278A patent/TN2012000278A1/en unknown
- 2012-06-12 CR CR20120318A patent/CR20120318A/es unknown
- 2012-06-12 IL IL220328A patent/IL220328A/en not_active IP Right Cessation
- 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
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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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