MX2012000763A - Derivados sustituidos de triazol e imidazol como moduladores de la gamma secretasa. - Google Patents
Derivados sustituidos de triazol e imidazol como moduladores de la gamma secretasa.Info
- Publication number
- MX2012000763A MX2012000763A MX2012000763A MX2012000763A MX2012000763A MX 2012000763 A MX2012000763 A MX 2012000763A MX 2012000763 A MX2012000763 A MX 2012000763A MX 2012000763 A MX2012000763 A MX 2012000763A MX 2012000763 A MX2012000763 A MX 2012000763A
- Authority
- MX
- Mexico
- Prior art keywords
- sup
- imidazole derivatives
- gamma secretase
- substituted triazole
- secretase modulators
- Prior art date
Links
- VHNYOQKVZQVBLC-RTCGXNAVSA-N (4r,7e,9as)-7-[[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]methylidene]-4-(3,4,5-trifluorophenyl)-1,3,4,8,9,9a-hexahydropyrido[2,1-c][1,4]oxazin-6-one Chemical compound C1([C@@H]2COC[C@@H]3CC\C(C(N32)=O)=C/C=2C=C(C(=CC=2)N2C=C(C)N=C2)OC)=CC(F)=C(F)C(F)=C1 VHNYOQKVZQVBLC-RTCGXNAVSA-N 0.000 title abstract 2
- 150000002460 imidazoles Chemical class 0.000 title abstract 2
- 229940079865 intestinal antiinfectives imidazole derivative Drugs 0.000 title abstract 2
- 229940042055 systemic antimycotics triazole derivative Drugs 0.000 title abstract 2
- 150000003852 triazoles Chemical class 0.000 title abstract 2
- 229940124648 γ-Secretase Modulator Drugs 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 4
- 239000004480 active ingredient Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
- C07D233/60—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
-
- 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
- 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
- A61P25/28—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D403/02—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
- C07D403/10—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 aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Biomedical Technology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La presente invención se refiere a novedosos derivados de triazol e imidazol de la Fórmula (I) (ver fórmula (I)) donde R1, R2, A1, A2, A3, A4, X y Het1 tienen el significado que se define en las reivindicaciones; los compuestos según la presente invención resultan de utilidad como moduladores de la gamma secretasa; la invención también se refiere a los procedimientos para elaborar tales compuestos novedosos, a composiciones farmacéuticas que comprenden dichos compuestos a modo de ingrediente activo, así como al uso de dichos compuestos como medicamento.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09165585 | 2009-07-15 | ||
| EP10164625 | 2010-06-01 | ||
| PCT/EP2010/060083 WO2011006903A1 (en) | 2009-07-15 | 2010-07-13 | Substituted triazole and imidazole derivatives as gamma secretase modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2012000763A true MX2012000763A (es) | 2012-02-08 |
Family
ID=42542935
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2012000763A MX2012000763A (es) | 2009-07-15 | 2010-07-13 | Derivados sustituidos de triazol e imidazol como moduladores de la gamma secretasa. |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US8946266B2 (es) |
| EP (1) | EP2454239B1 (es) |
| JP (2) | JP2012532912A (es) |
| KR (1) | KR20120050450A (es) |
| CN (1) | CN102482227A (es) |
| AP (1) | AP2011006034A0 (es) |
| AU (1) | AU2010272578B2 (es) |
| BR (1) | BR112012000915A2 (es) |
| CA (1) | CA2778517A1 (es) |
| EA (1) | EA021047B1 (es) |
| ES (1) | ES2519565T3 (es) |
| IL (1) | IL217491A (es) |
| MX (1) | MX2012000763A (es) |
| NZ (1) | NZ597505A (es) |
| SG (1) | SG177644A1 (es) |
| TW (1) | TW201109316A (es) |
| WO (1) | WO2011006903A1 (es) |
| ZA (1) | ZA201200285B (es) |
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| US7935815B2 (en) * | 2007-08-31 | 2011-05-03 | Eisai R&D Management Co., Ltd. | Imidazoyl pyridine compounds and salts thereof |
| CA2694401C (en) * | 2007-08-31 | 2012-12-04 | Eisai R&D Management Co., Ltd. | Polycyclic compound |
| PA8854101A1 (es) | 2008-12-18 | 2010-07-27 | Ortho Mcneil Janssen Pharm | Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa |
| WO2010089292A1 (en) | 2009-02-06 | 2010-08-12 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc | Novel substituted bicyclic heterocyclic compounds as gamma secretase modulators |
| TWI461425B (zh) | 2009-02-19 | 2014-11-21 | Janssen Pharmaceuticals Inc | 作為伽瑪分泌酶調節劑之新穎經取代的苯并唑、苯并咪唑、唑并吡啶及咪唑并吡啶衍生物類 |
| KR20110118626A (ko) | 2009-02-26 | 2011-10-31 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 테트라하이드로트리아졸로피리딘 유도체의 염과 이의 결정 |
| AU2010218714A1 (en) | 2009-02-26 | 2011-09-08 | Eisai R&D Management Co., Ltd. | Nitrogen-containing fused heterocyclic compounds and their use as beta amyloid production inhibitors |
| EP2427453B1 (en) | 2009-05-07 | 2013-07-17 | Janssen Pharmaceuticals, Inc. | Substituted indazole and aza-indazole derivatives as gamma secretase modulators |
| EA021047B1 (ru) | 2009-07-15 | 2015-03-31 | Янссен Фармасьютикалз, Инк. | Замещенные производные триазола и имидазола в качестве модуляторов гамма-секретазы |
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| CA2827969A1 (en) * | 2011-03-24 | 2012-09-27 | Janssen Pharmaceuticals, Inc. | Novel substituted triazolyl piperazine and triazolyl piperidine derivatives as gamma secretase modulators |
| CN102690194B (zh) * | 2011-03-24 | 2014-06-25 | 上海通远生物科技有限公司 | 3-环丙基甲氧基-4-二氟甲氧基苯甲酸的制备方法 |
| WO2013005354A1 (ja) * | 2011-07-01 | 2013-01-10 | 武田薬品工業株式会社 | 複素環化合物 |
| AU2012286021A1 (en) | 2011-07-15 | 2014-01-16 | Janssen Pharmaceutica Nv | Monoclonal antibodies specific for beta-amyloid x-37 and uses thereof |
| EA023045B1 (ru) | 2011-07-15 | 2016-04-29 | Янссен Фармасьютикалз, Инк. | Новые замещенные производные индола в качестве модуляторов гамма-секретазы |
| ES2674451T3 (es) | 2012-02-21 | 2018-06-29 | Merck Patent Gmbh | 2-amino-[1,2,4]triazolo[1,5-a] pirazinas 8-sustituidos como inhibidores de la SYK tirosina quinasa e inhibidores de la serina quinasa GCN2 |
| JP6106745B2 (ja) | 2012-05-16 | 2017-04-05 | ヤンセン ファーマシューティカルズ,インコーポレーテッド | (特に)アルツハイマー病の治療に有用な置換3,4−ジヒドロ−2H−ピリド[1,2−a]ピラジン−1,6−ジオン誘導体 |
| JP6453218B2 (ja) | 2012-08-24 | 2019-01-16 | ボード・オブ・リージエンツ,ザ・ユニバーシテイ・オブ・テキサス・システム | 疾患を治療するためのhif活性の複素環式修飾物質 |
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| EP3004080B1 (en) | 2013-06-04 | 2018-10-10 | Acturum Real Estate AB | Triazole compounds and their use as gamma secretase modulators |
| ES2665421T3 (es) | 2013-06-04 | 2018-04-25 | Acturum Real Estate Ab | Compuestos de pirimidina y su uso como moduladores de la gamma secretasa |
| WO2014195321A1 (en) | 2013-06-04 | 2014-12-11 | Acturum Life Science AB | Triazole compounds and their use as gamma secretase modulators |
| US10562897B2 (en) | 2014-01-16 | 2020-02-18 | Janssen Pharmaceutica Nv | Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators |
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| JP6672296B2 (ja) | 2014-10-31 | 2020-03-25 | ザ ジェネラル ホスピタル コーポレイション | 強力なγ−セクレターゼモジュレータ |
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| CN109311877B (zh) * | 2016-07-14 | 2021-05-28 | 豪夫迈·罗氏有限公司 | 稠合嘧啶衍生物 |
| CN109790149B (zh) | 2016-11-08 | 2022-05-17 | 豪夫迈·罗氏有限公司 | 苯氧基三唑类化合物 |
| CN111201229B (zh) | 2017-10-11 | 2024-08-23 | 豪夫迈·罗氏有限公司 | 用作rip1激酶抑制剂的二环化合物 |
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2010
- 2010-07-13 EA EA201270166A patent/EA021047B1/ru not_active IP Right Cessation
- 2010-07-13 MX MX2012000763A patent/MX2012000763A/es active IP Right Grant
- 2010-07-13 EP EP10734963.1A patent/EP2454239B1/en active Active
- 2010-07-13 NZ NZ597505A patent/NZ597505A/xx not_active IP Right Cessation
- 2010-07-13 AU AU2010272578A patent/AU2010272578B2/en not_active Ceased
- 2010-07-13 US US13/382,659 patent/US8946266B2/en not_active Expired - Fee Related
- 2010-07-13 KR KR1020127003902A patent/KR20120050450A/ko not_active Ceased
- 2010-07-13 CN CN2010800332416A patent/CN102482227A/zh active Pending
- 2010-07-13 ES ES10734963.1T patent/ES2519565T3/es active Active
- 2010-07-13 CA CA2778517A patent/CA2778517A1/en not_active Abandoned
- 2010-07-13 AP AP2011006034A patent/AP2011006034A0/xx unknown
- 2010-07-13 SG SG2012002473A patent/SG177644A1/en unknown
- 2010-07-13 WO PCT/EP2010/060083 patent/WO2011006903A1/en not_active Ceased
- 2010-07-13 BR BR112012000915A patent/BR112012000915A2/pt not_active IP Right Cessation
- 2010-07-13 JP JP2012520010A patent/JP2012532912A/ja active Pending
- 2010-07-14 TW TW099123059A patent/TW201109316A/zh unknown
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2012
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- 2012-01-13 ZA ZA2012/00285A patent/ZA201200285B/en unknown
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2015
- 2015-02-06 JP JP2015022061A patent/JP2015129147A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| ES2519565T3 (es) | 2014-11-07 |
| IL217491A (en) | 2015-08-31 |
| JP2015129147A (ja) | 2015-07-16 |
| ZA201200285B (en) | 2014-06-25 |
| EP2454239A1 (en) | 2012-05-23 |
| BR112012000915A2 (pt) | 2019-09-24 |
| SG177644A1 (en) | 2012-03-29 |
| EP2454239B1 (en) | 2014-08-13 |
| KR20120050450A (ko) | 2012-05-18 |
| IL217491A0 (en) | 2012-02-29 |
| JP2012532912A (ja) | 2012-12-20 |
| CN102482227A (zh) | 2012-05-30 |
| US8946266B2 (en) | 2015-02-03 |
| AP2011006034A0 (en) | 2011-12-31 |
| EA021047B1 (ru) | 2015-03-31 |
| EA201270166A1 (ru) | 2012-06-29 |
| AU2010272578A1 (en) | 2012-01-19 |
| NZ597505A (en) | 2013-05-31 |
| AU2010272578B2 (en) | 2015-03-05 |
| US20120135981A1 (en) | 2012-05-31 |
| CA2778517A1 (en) | 2011-01-20 |
| TW201109316A (en) | 2011-03-16 |
| WO2011006903A1 (en) | 2011-01-20 |
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