BRPI1011190A8 - Derivados de indazol e aza-indazol substituídos como moduladores de gama secretase - Google Patents
Derivados de indazol e aza-indazol substituídos como moduladores de gama secretaseInfo
- Publication number
- BRPI1011190A8 BRPI1011190A8 BRPI1011190A BRPI1011190A BRPI1011190A8 BR PI1011190 A8 BRPI1011190 A8 BR PI1011190A8 BR PI1011190 A BRPI1011190 A BR PI1011190A BR PI1011190 A BRPI1011190 A BR PI1011190A BR PI1011190 A8 BRPI1011190 A8 BR PI1011190A8
- Authority
- BR
- Brazil
- Prior art keywords
- indazole
- aza
- gamma secretase
- secretase modulators
- substituted
- 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 3
- QRUDEWIWKLJBPS-UHFFFAOYSA-N benzotriazole Chemical class C1=CC=C2N[N][N]C2=C1 QRUDEWIWKLJBPS-UHFFFAOYSA-N 0.000 title abstract 3
- 229940124648 γ-Secretase Modulator Drugs 0.000 title abstract 3
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical class C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 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
- 150000002473 indoazoles Chemical class 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- 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
- 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
- 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
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/12—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 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
DERIVADOS DE INDAZOL E AZA-INDAZOL SUBSTITUÍDOS COMO MODULADORES DE GAMA SECRETASE A presente invenção refere-se aos novos derivados de indazol e aza-indazol substituídos da Fórmula (I), em que R1, R2 , R3 , R4, Y, A1, A2 , A3 , A4, x1, X2 , X3 e Het1 têm o significado definido nas reivindicações. Os compostos de acordo com a presente invenção são úteis como moduladores de gama secretase. A invenção ainda diz respeito aos processos para preparar tais novos compostos, composições farmacêuticas compreendendo os ditos compostos como um ingrediente ativo como também o uso dos ditos compostos como um medicamento.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09159615 | 2009-05-07 | ||
| PCT/EP2010/056074 WO2010145883A1 (en) | 2009-05-07 | 2010-05-05 | Novel substituted indazole and aza-indazole derivatives as gamma secretase modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BRPI1011190A2 BRPI1011190A2 (pt) | 2016-03-15 |
| BRPI1011190A8 true BRPI1011190A8 (pt) | 2016-11-16 |
Family
ID=40786448
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI1011190A BRPI1011190A8 (pt) | 2009-05-07 | 2010-05-05 | Derivados de indazol e aza-indazol substituídos como moduladores de gama secretase |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US8835482B2 (pt) |
| EP (1) | EP2427453B1 (pt) |
| JP (1) | JP5559309B2 (pt) |
| KR (1) | KR20120024555A (pt) |
| CN (1) | CN102439005B (pt) |
| AR (1) | AR076850A1 (pt) |
| AU (1) | AU2010262036B2 (pt) |
| BR (1) | BRPI1011190A8 (pt) |
| CA (1) | CA2755467A1 (pt) |
| EA (1) | EA019702B1 (pt) |
| ES (1) | ES2431619T3 (pt) |
| IL (1) | IL216113A (pt) |
| MX (1) | MX2011011753A (pt) |
| MY (1) | MY152998A (pt) |
| NZ (1) | NZ596843A (pt) |
| SG (1) | SG175317A1 (pt) |
| TW (1) | TWI461419B (pt) |
| UA (1) | UA105377C2 (pt) |
| WO (1) | WO2010145883A1 (pt) |
| ZA (1) | ZA201108117B (pt) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PA8854101A1 (es) | 2008-12-18 | 2010-07-27 | Ortho Mcneil Janssen Pharm | Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa |
| EA019685B1 (ru) | 2009-02-06 | 2014-05-30 | Янссен Фармасьютикалз, Инк. | Новые замещенные бициклические гетероциклические соединения в качестве модуляторов гамма-секретазы |
| 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 |
| BRPI1011190A8 (pt) | 2009-05-07 | 2016-11-16 | Janssen Pharmaceuticals Inc | Derivados de indazol e aza-indazol substituídos como moduladores de gama secretase |
| ES2519565T3 (es) | 2009-07-15 | 2014-11-07 | Janssen Pharmaceuticals Inc. | Derivados de triazol e imidazol sustituidos como moduladores de gamma secretasa |
| EP2523949B1 (en) | 2010-01-15 | 2014-08-20 | Janssen Pharmaceuticals Inc. | Novel substituted triazole derivatives as gamma secretase modulators |
| CA2827969A1 (en) | 2011-03-24 | 2012-09-27 | Janssen Pharmaceuticals, Inc. | Novel substituted triazolyl piperazine and triazolyl piperidine derivatives as gamma secretase modulators |
| TWI567079B (zh) | 2011-07-15 | 2017-01-21 | 健生醫藥公司 | 作為伽瑪分泌酶調節劑之新穎的經取代的吲哚衍生物 |
| NZ702611A (en) | 2012-05-16 | 2016-10-28 | Cellzome Ltd | Substituted 3, 4 - dihydro - 2h - pyrido [1, 2 -a] pyrazine - 1, 6 - dione derivatives useful for the treatment of (inter alia) alzheimer’s disease |
| AU2013366668B2 (en) | 2012-12-20 | 2017-07-20 | Janssen Pharmaceutica Nv | Novel tricyclic 3,4-dihydro-2H-pyrido[1,2-alpha]pyrazine -1,6-dione derivatives as gamma secretase modulators |
| ES2612215T3 (es) | 2013-01-17 | 2017-05-12 | Janssen Pharmaceutica, N.V. | Novedosos derivados de pirido-piperazinona sustituidos como moduladores de gamma secretasa |
| WO2014127816A1 (en) * | 2013-02-21 | 2014-08-28 | Boehringer Ingelheim International Gmbh | Dihydropteridinones ii |
| 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 |
| CN103880683B (zh) * | 2014-02-26 | 2018-06-22 | 南通大学 | 一种3-溴-2-硝基苯甲醛的化学合成方法 |
| EP3347363B1 (en) * | 2015-09-09 | 2020-01-01 | H. Hoffnabb-La Roche Ag | N-(3-azabicyclo[3.2.1]octan-8-yl)-8-(4-phenyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[l,5-a]pyridin-2-amine derivatives as gamma-secretase modulators for treating alzheimer's disease |
| CN105585547A (zh) * | 2016-03-09 | 2016-05-18 | 中国科学院广州生物医药与健康研究院 | 一种4-五氟化硫苯酚类化合物及制备方法以及五氟化硫取代苯并吡喃类化合物的制备方法 |
| CN114195702A (zh) * | 2020-09-18 | 2022-03-18 | 瑞博(杭州)医药科技有限公司 | 一种用于合成抗肿瘤药物尼拉帕利的中间体及其制备方法 |
| CN121405704A (zh) * | 2024-07-25 | 2026-01-27 | 浙江养生堂天然药物研究所有限公司 | 氮杂芳基类化合物及其用途 |
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| 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 |
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| ES2519565T3 (es) | 2009-07-15 | 2014-11-07 | Janssen Pharmaceuticals Inc. | Derivados de triazol e imidazol sustituidos como moduladores de gamma secretasa |
| EP2523949B1 (en) | 2010-01-15 | 2014-08-20 | Janssen Pharmaceuticals Inc. | Novel substituted triazole derivatives as gamma secretase modulators |
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-
2010
- 2010-05-05 BR BRPI1011190A patent/BRPI1011190A8/pt not_active IP Right Cessation
- 2010-05-05 SG SG2011077518A patent/SG175317A1/en unknown
- 2010-05-05 KR KR1020117024948A patent/KR20120024555A/ko not_active Ceased
- 2010-05-05 ES ES10719325T patent/ES2431619T3/es active Active
- 2010-05-05 JP JP2012509024A patent/JP5559309B2/ja not_active Expired - Fee Related
- 2010-05-05 WO PCT/EP2010/056074 patent/WO2010145883A1/en not_active Ceased
- 2010-05-05 EA EA201171363A patent/EA019702B1/ru not_active IP Right Cessation
- 2010-05-05 EP EP10719325.2A patent/EP2427453B1/en active Active
- 2010-05-05 MY MYPI2011005324 patent/MY152998A/en unknown
- 2010-05-05 UA UAA201110540A patent/UA105377C2/uk unknown
- 2010-05-05 US US13/263,860 patent/US8835482B2/en active Active
- 2010-05-05 AU AU2010262036A patent/AU2010262036B2/en not_active Ceased
- 2010-05-05 CA CA2755467A patent/CA2755467A1/en not_active Abandoned
- 2010-05-05 NZ NZ596843A patent/NZ596843A/xx not_active IP Right Cessation
- 2010-05-05 CN CN201080020131.6A patent/CN102439005B/zh not_active Expired - Fee Related
- 2010-05-05 MX MX2011011753A patent/MX2011011753A/es active IP Right Grant
- 2010-05-06 TW TW099114456A patent/TWI461419B/zh not_active IP Right Cessation
- 2010-05-06 AR ARP100101549A patent/AR076850A1/es not_active Application Discontinuation
-
2011
- 2011-11-03 IL IL216113A patent/IL216113A/en not_active IP Right Cessation
- 2011-11-04 ZA ZA2011/08117A patent/ZA201108117B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2755467A1 (en) | 2010-12-23 |
| EA201171363A1 (ru) | 2012-04-30 |
| EA019702B1 (ru) | 2014-05-30 |
| AU2010262036A1 (en) | 2011-09-22 |
| AR076850A1 (es) | 2011-07-13 |
| KR20120024555A (ko) | 2012-03-14 |
| EP2427453B1 (en) | 2013-07-17 |
| TW201105658A (en) | 2011-02-16 |
| CN102439005A (zh) | 2012-05-02 |
| BRPI1011190A2 (pt) | 2016-03-15 |
| JP5559309B2 (ja) | 2014-07-23 |
| JP2012526078A (ja) | 2012-10-25 |
| ES2431619T3 (es) | 2013-11-27 |
| IL216113A (en) | 2015-02-26 |
| ZA201108117B (en) | 2015-06-24 |
| WO2010145883A1 (en) | 2010-12-23 |
| EP2427453A1 (en) | 2012-03-14 |
| SG175317A1 (en) | 2011-11-28 |
| IL216113A0 (en) | 2012-01-31 |
| NZ596843A (en) | 2012-12-21 |
| MY152998A (en) | 2014-12-31 |
| TWI461419B (zh) | 2014-11-21 |
| US8835482B2 (en) | 2014-09-16 |
| AU2010262036B2 (en) | 2014-10-30 |
| US20120095036A1 (en) | 2012-04-19 |
| CN102439005B (zh) | 2015-07-22 |
| UA105377C2 (uk) | 2014-05-12 |
| MX2011011753A (es) | 2011-11-29 |
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| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
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| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |