ECSP099639A - Compuestos amino-5-[-4-(difluorometoxi)fenil sustituido]-5-fenilimidazolona como inhibidores de ?-secretasa - Google Patents
Compuestos amino-5-[-4-(difluorometoxi)fenil sustituido]-5-fenilimidazolona como inhibidores de ?-secretasaInfo
- Publication number
- ECSP099639A ECSP099639A EC2009009639A ECSP099639A ECSP099639A EC SP099639 A ECSP099639 A EC SP099639A EC 2009009639 A EC2009009639 A EC 2009009639A EC SP099639 A ECSP099639 A EC SP099639A EC SP099639 A ECSP099639 A EC SP099639A
- Authority
- EC
- Ecuador
- Prior art keywords
- optionally substituted
- alkyl
- group
- independently
- cycloalkyl
- Prior art date
Links
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
- C07D233/66—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/88—Nitrogen atoms, e.g. allantoin
-
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4168—1,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
-
- 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
- A61P25/28—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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención proporciona un compuesto de la Fórmula I. en donde R1 y R2 son cada uno independientemente H o un grupo alquilo, cicloalquilo, cicloheteroalquilo, arilo o heteroarilo cada uno se sustituye opcionalmente o R1 y R2 se pueden tomar junto con el átomo al cual ellos se adhieren para formar un anillo de 5 a 7 miembros opcionalmente sustituido que se interrumpe opcionalmente por un heteroátomo adicional seleccionado de O, N o S; R3 es H o un grupo alquilo, cicloalquilo, cicloheteroalquilo, arilo o heteroarilo cada uno se sustituye opcionalmente;R4, R5 y R6 son cada uno independientemente H, halógeno, NO2, CN, COR9, NR10CO2R11, NR12R13, OR14, NR15COR16, SOnR17 o un grupo alquilo, haloalquilo, alquenilo, haloalquenilo, alquinilo, cicloalquilo, alcoxi, alqueniloxi, alquiniloxi o cicloheteroalquilo cada uno se sustituye opcionalmente o cuando se adhieren a los átomos de carbono adyacentes R4 y R5 se pueden tomar junto con los átomos a los cuales ellos se adhieren para formar un anillo de 5 a 7 miembros opcionalmente sustituido que contiene opcionalmente uno o dos heteroátomos seleccionados de O, N o S;n es 0, 1 o 2;R7 y R8 son cada uno independientemente H, halógeno, NR20R21 o un grupo alquilo, cicloalquilo o alcoxi cada grupo se sustituye opcionalmente con la condición que uno de R7 o R8 puede ser diferente a H;R9 y R17 son cada uno independientemente H, NR18R19 o un grupo alquilo, haloalquilo, alcoxialquilo, alquenilo, alquinilo, cicloalquilo o arilo cada uno se sustituye opcionalmente;R10 y R15 son cada uno independientemente H o un grupo alquilo opcionalmente sustituido; R11, R14 y R16 son cada uno independientemente H o un grupo alquilo, haloalquilo, alcoxialquilo, alquenilo, alquinilo, cicloalquilo o arilo cada uno se sustituye opcionalmente;R12 y R13 son cada uno independientemente H o un grupo alquilo o cicloalquilo cada uno se sustituye opcionalmente o R12 y R13 se pueden tomar junto con el átomo al cual ellos se adhieren para formar un anillo de 5 a 7 miembros opcionalmente sustituido que contiene opcionalmente un heteroátomo adicional seleccionado de O, N o S; R18 y R19 son cada uno independientemente H o un grupo alquilo, alquenilo, alquinilo o cicloalquilo cada uno se sustituye opcionalmente o R18 y R19 se pueden tomar junto con el átomo al cual ellos se adhieren para formar un anillo de 5 a 7 miembros opcionalmente sustituido que contiene opcionalmente un heteroátomo adicional seleccionado de O, N o S; R20 y R21 son cada uno independientemente H, COR22 o un grupo alquilo opcionalmente sustituido; yR22 es un grupo alquilo opcionalmente sustituido; oun tautómero de estos, un estereoisómero de estos o una sal farmacéuticamente aceptable de estos.La presente invención también se relaciona con el uso de tales compuestos para el tratamiento de los depósitos -amiloides y ovillos neurofibrilares. Los compuestos de la Fórmula I son particularmente útiles en el tratamiento de la Enfermedad de Alzheimer, deterioro cognitivo, Síndrome de Down, HCHWA-D, disminución cognitiva, demencia senil, angiopatía amiloide cerebral, demencia degenerativa, o otros trastornos neurodegenerativos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91908707P | 2007-03-20 | 2007-03-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP099639A true ECSP099639A (es) | 2009-10-30 |
Family
ID=39564223
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2009009639A ECSP099639A (es) | 2007-03-20 | 2009-09-18 | Compuestos amino-5-[-4-(difluorometoxi)fenil sustituido]-5-fenilimidazolona como inhibidores de ?-secretasa |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US20090042964A1 (es) |
| EP (1) | EP2137161A1 (es) |
| JP (1) | JP2010522235A (es) |
| KR (1) | KR20100015376A (es) |
| CN (1) | CN101641335A (es) |
| AR (1) | AR065811A1 (es) |
| AU (1) | AU2008229327A1 (es) |
| BR (1) | BRPI0808944A2 (es) |
| CA (1) | CA2681243A1 (es) |
| CL (1) | CL2008000784A1 (es) |
| CO (1) | CO6140056A2 (es) |
| CR (1) | CR11020A (es) |
| EC (1) | ECSP099639A (es) |
| GT (1) | GT200900241A (es) |
| IL (1) | IL200961A0 (es) |
| MX (1) | MX2009009699A (es) |
| NI (1) | NI200900164A (es) |
| PA (1) | PA8772701A1 (es) |
| PE (1) | PE20090160A1 (es) |
| RU (1) | RU2009133807A (es) |
| SV (1) | SV2009003373A (es) |
| TW (1) | TW200845965A (es) |
| WO (1) | WO2008115552A1 (es) |
| ZA (1) | ZA200906542B (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| PE20070135A1 (es) | 2005-06-14 | 2007-03-09 | Schering Corp | Compuestos heterociclicos como inhibidores de aspartil proteasas |
| US8450308B2 (en) | 2008-08-19 | 2013-05-28 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| EP2184276A1 (en) * | 2008-11-07 | 2010-05-12 | Universite Paul Cezanne Aix-Marseille Iii | Process to prepare new substituted 1H-Benzo(d) imidazol-2(3h)-Ones, New intermediates and their use as bace 1 inhibitors |
| AP2866A (en) | 2009-03-13 | 2014-03-31 | Vitae Pharmaceuticals Inc | Inhibitors of beta-secretase |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| JP5828848B2 (ja) | 2010-02-24 | 2015-12-09 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | ベータセクレターゼインヒビター |
| WO2012138590A1 (en) | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| US9221839B2 (en) | 2011-04-07 | 2015-12-29 | Merck Sharp & Dohme Corp. | C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
| RU2014111055A (ru) | 2011-08-22 | 2015-09-27 | Мерк Шарп И Доум Корп. | 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение |
| TWI557112B (zh) | 2012-03-05 | 2016-11-11 | 百靈佳殷格翰國際股份有限公司 | β－分泌酶抑制劑 |
| TW201422592A (zh) | 2012-08-27 | 2014-06-16 | Boehringer Ingelheim Int | β－分泌酶抑制劑 |
| EP2900650A1 (en) | 2012-09-28 | 2015-08-05 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| CN104995176B (zh) | 2013-02-12 | 2019-02-22 | 巴克老龄化研究所 | 调节bace所介导的app加工的乙内酰脲 |
| US20160298151A1 (en) | 2015-04-09 | 2016-10-13 | Sher Ali Butt | Novel Method for the cheap, efficient, and effective production of pharmaceutical and therapeutic api's intermediates, and final products |
| BR112020020549A8 (pt) | 2018-04-23 | 2023-02-07 | Msd Werthenstein Biopharma Gmbh | Novo processo para síntese de um composto fenoxi diaminopirimidina |
| CN109289696B (zh) * | 2018-10-29 | 2022-03-22 | 天津先光化工有限公司 | 一种咪唑啉两性表面活性剂的制备方法 |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IE45198B1 (en) * | 1976-06-05 | 1982-07-14 | Wyeth John & Brother Ltd | Guanidine derivatives |
| GB1588096A (en) * | 1978-05-20 | 1981-04-15 | Wyeth & Bros Ltd John | Pyrrole derivatives |
| GB9511694D0 (en) * | 1995-06-09 | 1995-08-02 | Fujisawa Pharmaceutical Co | Benzamide derivatives |
| TW544448B (en) * | 1997-07-11 | 2003-08-01 | Novartis Ag | Pyridine derivatives |
| US6492408B1 (en) * | 1999-07-21 | 2002-12-10 | Boehringer Ingelheim Pharmaceuticals, Inc. | Small molecules useful in the treatment of inflammatory disease |
| DE10046993A1 (de) * | 2000-09-22 | 2002-04-11 | Aventis Pharma Gmbh | Substituierte Zimtsäureguanidide, Verfahren zur ihrer Herstellung, ihre Verwendung als Medikament sowie sie enthaltendes Medikament |
| WO2003094854A2 (en) * | 2002-05-07 | 2003-11-20 | Elan Pharmaceuticals, Inc. | Succinoyl aminopyrazoles and related compounds |
| US7700603B2 (en) * | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| WO2006009653A1 (en) * | 2004-06-16 | 2006-01-26 | Wyeth | Amino-5,5-diphenylimidazolone derivatives for the inhibition of beta-secretase |
| JP2008503460A (ja) * | 2004-06-16 | 2008-02-07 | ワイス | β−セクレターゼのインヒビターとしてのジフェニルイミダゾピリミジンおよびイミダゾールアミン |
| AU2006205127A1 (en) * | 2005-01-14 | 2006-07-20 | Wyeth | Amino-imidazolones for the inhibition of beta-secretase |
| MX2007009313A (es) * | 2005-02-01 | 2007-09-12 | Wyeth Corp | Amino-piridinas como inhibidores de ????-secretasa. |
| WO2006088694A1 (en) * | 2005-02-14 | 2006-08-24 | Wyeth | SUBSTITUTED THIENYL AND FURYL ACYLGUANIDINES AS β-SECRETASE MODULATORS |
| EP1848692A1 (en) * | 2005-02-14 | 2007-10-31 | Wyeth | AZOLYLACYLGUANIDINES AS ß-SECRETASE INHIBITORS |
| WO2006088705A1 (en) * | 2005-02-14 | 2006-08-24 | Wyeth | Terphenyl guanidines as [beta symbol] -secretase inhibitors |
| TW200738683A (en) * | 2005-06-30 | 2007-10-16 | Wyeth Corp | Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation |
| CA2613435A1 (en) * | 2005-06-30 | 2007-01-11 | Wyeth | Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for .beta.-secretase modulation |
| TW200730523A (en) * | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
| EP1928841A1 (en) * | 2005-09-26 | 2008-06-11 | Wyeth a Corporation of the State of Delaware | Amino-5- ý4- (difluoromethoxy) phenyl¨-5-phenylimidazolone compounds as inhibitors of the beta-secretase (bace) |
| CA2634037A1 (en) * | 2005-12-19 | 2007-07-12 | Wyeth | 2-amino-5-piperidinylimidazolone compounds and use thereof for .beta.-secretase modulation |
| WO2007100536A1 (en) * | 2006-02-24 | 2007-09-07 | Wyeth | DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE |
| US7700606B2 (en) * | 2006-08-17 | 2010-04-20 | Wyeth Llc | Imidazole amines as inhibitors of β-secretase |
| WO2008036196A2 (en) * | 2006-09-21 | 2008-03-27 | Wyeth | Indolylalkylpyridin-2-amines for the inhibition of beta-secretase |
-
2008
- 2008-03-18 CL CL200800784A patent/CL2008000784A1/es unknown
- 2008-03-18 PE PE2008000494A patent/PE20090160A1/es not_active Application Discontinuation
- 2008-03-19 PA PA20088772701A patent/PA8772701A1/es unknown
- 2008-03-19 AR ARP080101180A patent/AR065811A1/es unknown
- 2008-03-20 AU AU2008229327A patent/AU2008229327A1/en not_active Abandoned
- 2008-03-20 JP JP2010500934A patent/JP2010522235A/ja not_active Withdrawn
- 2008-03-20 EP EP08727031A patent/EP2137161A1/en not_active Withdrawn
- 2008-03-20 CA CA002681243A patent/CA2681243A1/en not_active Abandoned
- 2008-03-20 WO PCT/US2008/003681 patent/WO2008115552A1/en active Application Filing
- 2008-03-20 US US12/052,098 patent/US20090042964A1/en not_active Abandoned
- 2008-03-20 CN CN200880008871A patent/CN101641335A/zh active Pending
- 2008-03-20 RU RU2009133807/04A patent/RU2009133807A/ru not_active Application Discontinuation
- 2008-03-20 KR KR1020097020772A patent/KR20100015376A/ko not_active Application Discontinuation
- 2008-03-20 MX MX2009009699A patent/MX2009009699A/es not_active Application Discontinuation
- 2008-03-20 TW TW097109933A patent/TW200845965A/zh unknown
- 2008-03-20 BR BRPI0808944-2A patent/BRPI0808944A2/pt not_active Application Discontinuation
-
2009
- 2009-09-04 NI NI200900164A patent/NI200900164A/es unknown
- 2009-09-09 CR CR11020A patent/CR11020A/es unknown
- 2009-09-10 GT GT200900241A patent/GT200900241A/es unknown
- 2009-09-15 IL IL200961A patent/IL200961A0/en unknown
- 2009-09-16 CO CO09100417A patent/CO6140056A2/es unknown
- 2009-09-18 SV SV2009003373A patent/SV2009003373A/es not_active Application Discontinuation
- 2009-09-18 EC EC2009009639A patent/ECSP099639A/es unknown
- 2009-09-18 ZA ZA200906542A patent/ZA200906542B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL200961A0 (en) | 2010-05-17 |
| WO2008115552A1 (en) | 2008-09-25 |
| AU2008229327A1 (en) | 2008-09-25 |
| KR20100015376A (ko) | 2010-02-12 |
| AU2008229327A8 (en) | 2009-10-15 |
| US20090042964A1 (en) | 2009-02-12 |
| AR065811A1 (es) | 2009-07-01 |
| GT200900241A (es) | 2010-05-07 |
| JP2010522235A (ja) | 2010-07-01 |
| NI200900164A (es) | 2010-07-29 |
| ZA200906542B (en) | 2010-06-30 |
| CN101641335A (zh) | 2010-02-03 |
| CA2681243A1 (en) | 2008-09-25 |
| EP2137161A1 (en) | 2009-12-30 |
| BRPI0808944A2 (pt) | 2014-09-02 |
| CR11020A (es) | 2009-10-06 |
| PE20090160A1 (es) | 2009-02-11 |
| SV2009003373A (es) | 2010-08-10 |
| TW200845965A (en) | 2008-12-01 |
| PA8772701A1 (es) | 2008-11-19 |
| CL2008000784A1 (es) | 2008-05-30 |
| CO6140056A2 (es) | 2010-03-19 |
| RU2009133807A (ru) | 2011-04-27 |
| MX2009009699A (es) | 2009-09-24 |
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