AR065811A1 - Derivados de 2-amino-4h-imidazol-4-ona,composiciones farmaceuticas que los contienen y usos para el tratamiento de la enfermedad de alzheimer y otros trastornos neurodegenerativos. - Google Patents
Derivados de 2-amino-4h-imidazol-4-ona,composiciones farmaceuticas que los contienen y usos para el tratamiento de la enfermedad de alzheimer y otros trastornos neurodegenerativos.Info
- Publication number
- AR065811A1 AR065811A1 ARP080101180A ARP080101180A AR065811A1 AR 065811 A1 AR065811 A1 AR 065811A1 AR P080101180 A ARP080101180 A AR P080101180A AR P080101180 A ARP080101180 A AR P080101180A AR 065811 A1 AR065811 A1 AR 065811A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- alkyl
- independently
- group
- cycloalkyl
- Prior art date
Links
- 208000024827 Alzheimer disease Diseases 0.000 title 1
- 208000015122 neurodegenerative disease Diseases 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 8
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 8
- 125000003342 alkenyl group Chemical group 0.000 abstract 4
- 125000000304 alkynyl group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000004429 atom Chemical group 0.000 abstract 4
- 125000005842 heteroatom Chemical group 0.000 abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- 229910052760 oxygen Inorganic materials 0.000 abstract 4
- 229910052717 sulfur Inorganic materials 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000001188 haloalkyl group Chemical group 0.000 abstract 3
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 2
- -1 cycloheteroalkyl Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 101100134929 Gallus gallus COR9 gene Proteins 0.000 abstract 1
- 125000003302 alkenyloxy group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000262 haloalkenyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 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
- C07D233/66—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)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicacion 1: Un compuesto de la formula (1) caracterizado porque 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 contiene opcionalmente 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, halogeno, 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, halogeno, NR20R21 o un grupo alquilo, cicloalquilo o alcoxi cada grupo se sustituye opcionalmente, con la condicion que uno de R7 o R8 puede ser diferente de 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 grupo un 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 tornar 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; y R22 es un grupo alquilo opcionalmente sustituido; o un tautomero de éstos, un estereoisomero de éstos o una sal farmacéuticamente aceptable de éstos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91908707P | 2007-03-20 | 2007-03-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR065811A1 true AR065811A1 (es) | 2009-07-01 |
Family
ID=39564223
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080101180A AR065811A1 (es) | 2007-03-20 | 2008-03-19 | Derivados de 2-amino-4h-imidazol-4-ona,composiciones farmaceuticas que los contienen y usos para el tratamiento de la enfermedad de alzheimer y otros trastornos neurodegenerativos. |
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 |
| JP2008543849A (ja) | 2005-06-14 | 2008-12-04 | シェーリング コーポレイション | アスパルチルプロテアーゼ阻害剤 |
| 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 |
| US8633212B2 (en) | 2009-03-13 | 2014-01-21 | 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 | |
| US8889703B2 (en) | 2010-02-24 | 2014-11-18 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| 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 |
| US9145426B2 (en) | 2011-04-07 | 2015-09-29 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
| BR112014004181A2 (pt) | 2011-08-22 | 2017-06-13 | Merck Sharp & Dohme | composto, composição farmacêutica, e, método de tratamento, prevenção, e / ou retardo do início de uma doença ou patologia |
| 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 |
| WO2014052398A1 (en) | 2012-09-28 | 2014-04-03 | Vitae Pharmaceuticals, Inc. | Inhibitor of beta-secretase |
| JP6471100B2 (ja) * | 2013-02-12 | 2019-02-13 | バック・インスティテュート・フォー・リサーチ・オン・エイジング | Ｂａｃｅ仲介性ａｐｐプロセシングを調節するヒダントイン |
| 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 |
| CN112423756B (zh) | 2018-04-23 | 2024-08-13 | 默沙东有限责任公司 | 用于合成苯氧基二氨基嘧啶化合物的新方法 |
| 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 |
| AU2003229024A1 (en) * | 2002-05-07 | 2003-11-11 | Elan Pharmaceuticals, Inc. | Succinoyl aminopyrazoles and related compounds |
| US7700603B2 (en) * | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| JP2008503459A (ja) * | 2004-06-16 | 2008-02-07 | ワイス | β−セクレターゼを阻害するためのアミノ−５，５−ジフェニルイミダゾロン誘導体 |
| KR20070026811A (ko) * | 2004-06-16 | 2007-03-08 | 와이어쓰 | 베타-세크리타제 억제제로서의 디페닐이미다조피리미딘 및디페닐이미다졸 아민 |
| EP2264036A1 (en) * | 2005-01-14 | 2010-12-22 | Wyeth LLC (Formerly Known As Wyeth) | Amino-imidazolones for the inhibition of beta-secretase |
| AU2006211159A1 (en) * | 2005-02-01 | 2006-08-10 | Wyeth | Amino-pyridines as inhibitors of beta-secretase |
| WO2006088705A1 (en) * | 2005-02-14 | 2006-08-24 | Wyeth | Terphenyl guanidines as [beta symbol] -secretase inhibitors |
| WO2006088711A1 (en) * | 2005-02-14 | 2006-08-24 | Wyeth | AZOLYLACYLGUANIDINES AS β-SECRETASE INHIBITORS |
| WO2006088694A1 (en) * | 2005-02-14 | 2006-08-24 | Wyeth | SUBSTITUTED THIENYL AND FURYL ACYLGUANIDINES AS β-SECRETASE MODULATORS |
| CA2613435A1 (en) * | 2005-06-30 | 2007-01-11 | Wyeth | Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for .beta.-secretase modulation |
| TW200738683A (en) * | 2005-06-30 | 2007-10-16 | Wyeth Corp | Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation |
| TW200730523A (en) * | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
| BRPI0616757A2 (pt) * | 2005-09-26 | 2011-06-28 | Wyeth Corp | composto da fórmula i; processo para o tratamento de uma doença ou de um distúrbio associado com a atividade excessiva de bace; processo para a modulação da atividade de bace; processo para o tratamento da doença de alzheimer; e composição farmacêutica |
| BRPI0620025A2 (pt) * | 2005-12-19 | 2011-10-25 | Wyeth Corp | composto, método para o tratamento de uma doença ou transtorno associado a atividade excessiva de bace, método para modular a atividade de bace, composição farmacêutica e uso do composto |
| 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 |
| MX2009003102A (es) * | 2006-09-21 | 2009-04-01 | Wyeth Corp | INDOLILALQUILPIRIDIN-2-AMINAS PARA LA INHIBICION DE ß-SECRETASA. |
-
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 AR ARP080101180A patent/AR065811A1/es unknown
- 2008-03-19 PA PA20088772701A patent/PA8772701A1/es unknown
- 2008-03-20 EP EP08727031A patent/EP2137161A1/en not_active Withdrawn
- 2008-03-20 JP JP2010500934A patent/JP2010522235A/ja not_active Withdrawn
- 2008-03-20 CN CN200880008871A patent/CN101641335A/zh active Pending
- 2008-03-20 US US12/052,098 patent/US20090042964A1/en not_active Abandoned
- 2008-03-20 BR BRPI0808944-2A patent/BRPI0808944A2/pt not_active Application Discontinuation
- 2008-03-20 RU RU2009133807/04A patent/RU2009133807A/ru not_active Application Discontinuation
- 2008-03-20 AU AU2008229327A patent/AU2008229327A1/en not_active Abandoned
- 2008-03-20 WO PCT/US2008/003681 patent/WO2008115552A1/en not_active Ceased
- 2008-03-20 MX MX2009009699A patent/MX2009009699A/es not_active Application Discontinuation
- 2008-03-20 KR KR1020097020772A patent/KR20100015376A/ko not_active Withdrawn
- 2008-03-20 TW TW097109933A patent/TW200845965A/zh unknown
- 2008-03-20 CA CA002681243A patent/CA2681243A1/en not_active Abandoned
-
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 ZA ZA200906542A patent/ZA200906542B/xx unknown
- 2009-09-18 EC EC2009009639A patent/ECSP099639A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PA8772701A1 (es) | 2008-11-19 |
| SV2009003373A (es) | 2010-08-10 |
| AU2008229327A8 (en) | 2009-10-15 |
| MX2009009699A (es) | 2009-09-24 |
| NI200900164A (es) | 2010-07-29 |
| CR11020A (es) | 2009-10-06 |
| WO2008115552A1 (en) | 2008-09-25 |
| PE20090160A1 (es) | 2009-02-11 |
| CA2681243A1 (en) | 2008-09-25 |
| ZA200906542B (en) | 2010-06-30 |
| US20090042964A1 (en) | 2009-02-12 |
| EP2137161A1 (en) | 2009-12-30 |
| AU2008229327A1 (en) | 2008-09-25 |
| ECSP099639A (es) | 2009-10-30 |
| JP2010522235A (ja) | 2010-07-01 |
| BRPI0808944A2 (pt) | 2014-09-02 |
| IL200961A0 (en) | 2010-05-17 |
| KR20100015376A (ko) | 2010-02-12 |
| TW200845965A (en) | 2008-12-01 |
| CO6140056A2 (es) | 2010-03-19 |
| RU2009133807A (ru) | 2011-04-27 |
| CN101641335A (zh) | 2010-02-03 |
| GT200900241A (es) | 2010-05-07 |
| CL2008000784A1 (es) | 2008-05-30 |
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