PE20110581A1 - Compuestos pirazina como inhibidores de fosfodiesterasa 10 - Google Patents
Compuestos pirazina como inhibidores de fosfodiesterasa 10Info
- Publication number
- PE20110581A1 PE20110581A1 PE2011001035A PE2011001035A PE20110581A1 PE 20110581 A1 PE20110581 A1 PE 20110581A1 PE 2011001035 A PE2011001035 A PE 2011001035A PE 2011001035 A PE2011001035 A PE 2011001035A PE 20110581 A1 PE20110581 A1 PE 20110581A1
- Authority
- PE
- Peru
- Prior art keywords
- compounds
- pirazine
- iloxi
- methanone
- imidazol
- Prior art date
Links
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
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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
- A61K31/495—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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/36—Opioid-abuse
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Addiction (AREA)
- Psychology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
REFERIDA A UN COMPUESTO DERIVADO DE PIRAZINA DE FORMULA (I), DONDE X1, X2, X3, X4 Y X5 SON N O C, EN DONDE NO MAS DE DOS X1, X2, X3, Y X4 SON N; X6, X7, X9 Y X10 SON N O C, EN DONDE NO MAS DE TRES DE X6, X7, X9, Y X10 SON N; X8 Y X11 SON C; Y ES NH, CH(OH), C(=O), ENTRE OTROS; Z ES NH, S, SO, ENTRE OTROS; m ES UN ENTERO DE 0 A 4; n ES 0, 1 O 2; p ES 0, 1 O 2; R1 ES H, F, Cl, ENTRE OTROS; R2 ES F, Cl, OH, ENTRE OTROS; R3 ES F, Cl, CN, ENTRE OTROS; R4 ES F, Cl, CH3, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (1H-BENZO[d]IMIDAZOL-2-IL)(4-(3-MORFOLINOPIRAZIN-2-ILOXI)FENIL)-METANONA, (S)-(1H-BENZO[d]IMIDAZOL-2-IL)(4-(3-(4-(1,1,1-TRIFLUORO-2-HIDROXIPROPAN-2-IL)PIPERIDIN-1-IL)PIRAZIN-2-ILOXI)FENIL)METANONA, (1H-BENZO[d]IMIDAZOL-2-IL)(4-(3-CLOROPIRAZIN-2-ILOXI)FENIL)-METANONA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA FOSFODIESTERASA 10 (PDE 10) Y SON UTILES EN EL TRATAMIENTO DE LA OBESIDAD, ESQUIZOFEENIA, DIABETES NO DEPENDIENTE DE INSULINA, ENTRE OTROS
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11456708P | 2008-11-14 | 2008-11-14 | |
| US16621209P | 2009-04-02 | 2009-04-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20110581A1 true PE20110581A1 (es) | 2011-09-03 |
Family
ID=41478512
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2011001035A PE20110581A1 (es) | 2008-11-14 | 2009-11-16 | Compuestos pirazina como inhibidores de fosfodiesterasa 10 |
Country Status (31)
| Country | Link |
|---|---|
| US (4) | US8053438B2 (es) |
| EP (1) | EP2364308B1 (es) |
| JP (1) | JP5746972B2 (es) |
| KR (1) | KR20110083746A (es) |
| CN (1) | CN102300860B (es) |
| AR (1) | AR074358A1 (es) |
| AU (1) | AU2009313768B2 (es) |
| BR (1) | BRPI0922095A2 (es) |
| CA (1) | CA2742993C (es) |
| CL (1) | CL2011001094A1 (es) |
| CO (1) | CO6382157A2 (es) |
| CR (1) | CR20110326A (es) |
| CY (1) | CY1113680T1 (es) |
| DK (1) | DK2364308T3 (es) |
| EA (1) | EA019206B1 (es) |
| ES (1) | ES2397218T3 (es) |
| HK (1) | HK1161251A1 (es) |
| HR (1) | HRP20130054T1 (es) |
| IL (1) | IL212687A0 (es) |
| MA (1) | MA32889B1 (es) |
| MX (1) | MX2011005100A (es) |
| NZ (1) | NZ592508A (es) |
| PE (1) | PE20110581A1 (es) |
| PL (1) | PL2364308T3 (es) |
| PT (1) | PT2364308E (es) |
| RS (1) | RS52598B (es) |
| SI (1) | SI2364308T1 (es) |
| SM (1) | SMT201200061B (es) |
| TN (1) | TN2011000221A1 (es) |
| TW (1) | TWI396689B (es) |
| WO (1) | WO2010057121A1 (es) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9156812B2 (en) | 2008-06-04 | 2015-10-13 | Bristol-Myers Squibb Company | Crystalline form of 6-[(4S)-2-methyl-4-(2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine |
| CA2746307C (en) * | 2008-12-17 | 2013-11-19 | Amgen Inc. | Aminopyridine and carboxypyridine compounds as phosphodiesterase 10 inhibitors |
| AU2010211050B2 (en) | 2009-02-05 | 2016-05-12 | Takeda Pharmaceutical Company Limited | Pyridazinone compounds |
| JP5764553B2 (ja) * | 2009-05-12 | 2015-08-19 | アルバニー モレキュラー リサーチ， インコーポレイテッド | ７−（［１，２，４］トリアゾロ［１，５−ａ］ピリジン−６−イル）−４−（３，４−ジクロロフェニル）−１，２，３，４−テトラヒドロイソキノリンおよびその使用 |
| JP5739415B2 (ja) | 2009-05-12 | 2015-06-24 | ブリストル−マイヤーズ スクウィブ カンパニー | （Ｓ）−７−（［１，２，４］トリアゾロ［１，５−ａ］ピリジン−６−イル）−４−（３，４−ジクロロフェニル）−１，２，３，４−テトラヒドロイソキノリンの結晶形態およびその使用 |
| WO2011101424A1 (en) | 2010-02-19 | 2011-08-25 | Boehringer Ingelheim International Gmbh | Tricyclic pyridine derivatives, medicaments containing such compounds, their use and process for their preparation |
| JP5739526B2 (ja) | 2010-06-24 | 2015-06-24 | 武田薬品工業株式会社 | ホスホジエステラーゼ（ＰＤＥｓ）阻害薬としての縮合複素環化合物 |
| US8883788B2 (en) | 2010-08-04 | 2014-11-11 | Takeda Pharmaceutical Company Limited | Fused heterocyclic ring compound |
| WO2012018909A1 (en) | 2010-08-04 | 2012-02-09 | Takeda Pharmaceutical Company Limited | Fused heterocyclic compounds |
| US9150588B2 (en) | 2010-08-10 | 2015-10-06 | Takeda Pharmaceutical Company Limited | Substituted pyridazin-4(1H)-ones as phosphodiesterase 10A inhibitors |
| KR101903204B1 (ko) * | 2010-11-19 | 2018-11-22 | 리간드 파마슈티칼스 인코포레이티드 | 복소환 아민 및 이의 용도 |
| CN103619841B (zh) | 2011-01-11 | 2017-03-29 | 桑诺维恩药品公司 | 杂芳基化合物及其使用方法 |
| US9029388B2 (en) | 2011-03-16 | 2015-05-12 | Takeda Pharmaceutical Company Limited | Condensed heterocyclic compound |
| TWI570122B (zh) | 2011-06-22 | 2017-02-11 | 武田藥品工業股份有限公司 | 稠合雜環化合物之結晶 |
| CA2922849A1 (en) * | 2012-08-31 | 2014-03-06 | Ixchel Pharma, Llc | Agents useful for treating obesity, diabetes and related disorders |
| CN102911135B (zh) * | 2012-10-18 | 2016-01-13 | 内蒙古工业大学 | 2-巯基苯并噻唑类衍生物的合成方法 |
| KR101840526B1 (ko) | 2013-02-05 | 2018-03-20 | 퍼듀 퍼머 엘피 | 내변조성 제약 제제 |
| WO2014142322A1 (ja) | 2013-03-15 | 2014-09-18 | 第一三共株式会社 | ベンゾチオフェン誘導体 |
| WO2015006689A1 (en) | 2013-07-12 | 2015-01-15 | University Of South Alabama | Treatment and diagnosis of cancer and precancerous conditions using pde10a inhibitors and methods to measure pde10a expression |
| MX2016003843A (es) | 2013-09-27 | 2017-02-15 | Nimbus Iris Inc | Inhibidores de cinasas asociadas al receptor de interleucina 1 (irak) y usos de los mismos. |
| US9657015B2 (en) | 2014-07-31 | 2017-05-23 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| CN104649882A (zh) * | 2015-02-11 | 2015-05-27 | 南通恒盛精细化工有限公司 | 一种磷酸二酯酶抑制剂的中间体制备工艺 |
| US10807983B2 (en) | 2015-03-16 | 2020-10-20 | Ligand Pharmaceuticals, Inc. | Imidazo-fused heterocycles and uses thereof |
| MY195201A (en) * | 2015-09-18 | 2023-01-11 | Kaken Pharma Co Ltd | Biaryl Derivative and Medicine Containing Same |
| US11453674B2 (en) | 2018-01-19 | 2022-09-27 | Evopoint Biosciences Co., Ltd. | Heterocyclic compound, preparation method and use thereof in medicine |
| CN109020977B (zh) * | 2018-10-26 | 2020-11-13 | 安庆奇创药业有限公司 | 一种Acalabrutinib的制备方法 |
| JP2023553699A (ja) | 2020-12-17 | 2023-12-25 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | ヘテロ芳香族イソチオシアネート類 |
| CN113929598A (zh) * | 2021-11-24 | 2022-01-14 | 上海吉奉生物科技有限公司 | 一种（s）-2-叔丁氧羰基氨基-3-（4,4-二氟环己基）丙酸的合成方法 |
| EP4524134A1 (en) * | 2022-05-09 | 2025-03-19 | TYK Medicines Inc. | Polycyclic compound and use thereof |
| CN115894181A (zh) * | 2022-09-30 | 2023-04-04 | 渭南高新区海泰新型电子材料有限责任公司 | 一种环己烯基环己基二氟苯类液晶化合物的合成方法 |
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| US4198417A (en) | 1979-01-10 | 1980-04-15 | American Hoechst Corporation | Phenoxyphenylpiperidines |
| US20060293360A1 (en) | 2003-04-04 | 2006-12-28 | H. Lundbeck A/S | 4-(2-Phenyloxyphenyl)-piperidine or-1,2,3,6-tetrahydropyridine derivatives as serotonin reuptake inhibitors |
| DE10337942A1 (de) | 2003-08-18 | 2005-03-17 | Merck Patent Gmbh | Aminobenzimidazolderivate |
| DE10344223A1 (de) | 2003-09-24 | 2005-04-21 | Merck Patent Gmbh | 1,3-Benzoxazolylderivate als Kinase-Inhibitoren |
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| CA2703653A1 (en) | 2007-10-25 | 2009-04-30 | Astrazeneca Ab | Pyridine and pyrazine derivatives -083 |
| WO2009081259A1 (en) | 2007-12-21 | 2009-07-02 | Pfizer Inc. | Phenoxy-pyridyl derivatives |
| KR20110026481A (ko) | 2008-06-20 | 2011-03-15 | 메타볼렉스, 인코포레이티드 | 아릴 ｇｐｒ１１９ 작동약 및 이의 용도 |
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2009
- 2009-11-13 TW TW098138718A patent/TWI396689B/zh not_active IP Right Cessation
- 2009-11-16 MX MX2011005100A patent/MX2011005100A/es active IP Right Grant
- 2009-11-16 US US12/619,574 patent/US8053438B2/en not_active Expired - Fee Related
- 2009-11-16 CA CA2742993A patent/CA2742993C/en not_active Expired - Fee Related
- 2009-11-16 PE PE2011001035A patent/PE20110581A1/es not_active Application Discontinuation
- 2009-11-16 DK DK09752705.5T patent/DK2364308T3/da active
- 2009-11-16 KR KR1020117013506A patent/KR20110083746A/ko not_active Application Discontinuation
- 2009-11-16 CN CN200980154871.6A patent/CN102300860B/zh not_active Expired - Fee Related
- 2009-11-16 AU AU2009313768A patent/AU2009313768B2/en not_active Ceased
- 2009-11-16 ES ES09752705T patent/ES2397218T3/es active Active
- 2009-11-16 PL PL09752705T patent/PL2364308T3/pl unknown
- 2009-11-16 BR BRPI0922095A patent/BRPI0922095A2/pt not_active IP Right Cessation
- 2009-11-16 EP EP09752705A patent/EP2364308B1/en active Active
- 2009-11-16 RS RS20120569A patent/RS52598B/en unknown
- 2009-11-16 SI SI200930429T patent/SI2364308T1/sl unknown
- 2009-11-16 WO PCT/US2009/064637 patent/WO2010057121A1/en active Application Filing
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- 2009-11-16 AR ARP090104436A patent/AR074358A1/es not_active Application Discontinuation
- 2009-11-16 JP JP2011536567A patent/JP5746972B2/ja not_active Expired - Fee Related
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2011
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2012
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