AR052458A1 - Amino-imidazolonas para la inhibicion de beta-secretasa - Google Patents
Amino-imidazolonas para la inhibicion de beta-secretasaInfo
- Publication number
- AR052458A1 AR052458A1 ARP060100150A ARP060100150A AR052458A1 AR 052458 A1 AR052458 A1 AR 052458A1 AR P060100150 A ARP060100150 A AR P060100150A AR P060100150 A ARP060100150 A AR P060100150A AR 052458 A1 AR052458 A1 AR 052458A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- independently
- alkyl
- attached
- cycloalkyl
- Prior art date
Links
- 230000005764 inhibitory process Effects 0.000 title 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 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
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000004429 atom Chemical group 0.000 abstract 3
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 abstract 2
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 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
- 208000037259 Amyloid Plaque Diseases 0.000 abstract 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 abstract 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 abstract 1
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
- A61P25/28—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)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Además se proveen composiciones y métodos para su uso, a fin de inhibir beta-secretasa (BACE) y tratar depositos beta- amiloideos y enredos neurofibrilares. Reivindicacion 1: Un compuesto de formula (1) donde. R1 y R2 son de manera independiente H o un grupo alquilo C1-4 opcionalmente sustituido, R3 y R4 son de manera independiente H o un grupo alquilo C1-4 opcionalmente sustituido; o R3 y R4 pueden tomarse juntos para formar un anillo de 4 a 7 miembros que, en forma opcional, contiene 1 o 2 heteroátomos seleccionados de O, N o S; R5, R6 y R7 son de manera independiente H, halogeno, NO2, CN, OR11, NR12R13 o un grupo alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloheteroalquilo, arilo o aril- alquilo C1-4, donde cada uno está opcionalmente sustituido; o cuando están unidos a átomos de C adyacentes, R5 y R6 pueden tomarse junto con los átomos a los que están unidos para formar un anillo de 5 a 7 miembros opcionalmente sustituido, que en forma opcional, contiene 1 o 2 heteroátomos seleccionados de O, N o S; R8, R9 y R10 son de manera independiente H, halogeno, NO2, CN, OR14, NR15R16 o un grupo alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloheteroalquilo, arilo o aril-alquilo C1-4, donde cada uno está opcionalmente sustituido; o cuando están unidos a átomos de C adyacentes, R8 y R9 pueden tomarse junto con los átomos a los que están unidos para formar un anillo de 5 a 7 miembros opcionalmente sustituido, que en forma opcional, contiene 1 o 2 heteroátomos seleccionados de O, N o S; n es 0, 1 o 2; R11 y R14 son de manera independiente H o un grupo alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3- 8 o arilo, donde cada uno está opcionalmente sustituido; y R12, R13, R15 y r16 son de manera independiente H, alquilo C1-4, cicloalquilo C3-8, o R12 y R13, o R15 y R16, pueden tomarse junto con el átomo al que están unidos para formar un anillo de 5 a 7 miembros, que en forma opcional, contiene un heteroátomo adicional seleccionado de O, N o S; o un tautomero de dicho compuesto, un estereoisomero de dicho compuesto o una sal farmacéuticamente aceptable de dicho compuesto.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US64380505P | 2005-01-14 | 2005-01-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR052458A1 true AR052458A1 (es) | 2007-03-21 |
Family
ID=36581776
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060100150A AR052458A1 (es) | 2005-01-14 | 2006-01-13 | Amino-imidazolonas para la inhibicion de beta-secretasa |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US7563796B2 (es) |
| EP (2) | EP2264036A1 (es) |
| JP (1) | JP2008526966A (es) |
| KR (1) | KR20070095948A (es) |
| CN (1) | CN101103034A (es) |
| AR (1) | AR052458A1 (es) |
| AU (1) | AU2006205127A1 (es) |
| BR (1) | BRPI0606690A2 (es) |
| CA (1) | CA2593515A1 (es) |
| CR (1) | CR9244A (es) |
| GT (1) | GT200600009A (es) |
| IL (1) | IL183938A0 (es) |
| MX (1) | MX2007008555A (es) |
| NO (1) | NO20073099L (es) |
| PA (1) | PA8660001A1 (es) |
| PE (1) | PE20060842A1 (es) |
| RU (1) | RU2007126570A (es) |
| TW (1) | TW200637866A (es) |
| WO (1) | WO2006076284A2 (es) |
| ZA (1) | ZA200705783B (es) |
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| KR20070026811A (ko) * | 2004-06-16 | 2007-03-08 | 와이어쓰 | 베타-세크리타제 억제제로서의 디페닐이미다조피리미딘 및디페닐이미다졸 아민 |
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| WO2006088711A1 (en) | 2005-02-14 | 2006-08-24 | Wyeth | AZOLYLACYLGUANIDINES AS β-SECRETASE 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 |
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| TW200738683A (en) * | 2005-06-30 | 2007-10-16 | Wyeth Corp | Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation |
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| 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 |
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| TW200815447A (en) * | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds IV |
| TW200815443A (en) * | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds I |
| TW200808796A (en) * | 2006-06-14 | 2008-02-16 | Astrazeneca Ab | New compounds III |
| TW200815449A (en) * | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds II |
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| EP1644354A1 (en) | 2003-07-01 | 2006-04-12 | Bayer CropScience GmbH | 3-pyridylcarboxamide derivatives as pesticidal agents |
| SG163508A1 (en) | 2003-12-15 | 2010-08-30 | Schering Corp | Heterocyclic aspartyl protease inhibitors |
| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| KR20070026811A (ko) | 2004-06-16 | 2007-03-08 | 와이어쓰 | 베타-세크리타제 억제제로서의 디페닐이미다조피리미딘 및디페닐이미다졸 아민 |
| 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 |
| AU2006211159A1 (en) | 2005-02-01 | 2006-08-10 | Wyeth | Amino-pyridines as inhibitors of beta-secretase |
| WO2006088711A1 (en) | 2005-02-14 | 2006-08-24 | Wyeth | AZOLYLACYLGUANIDINES AS β-SECRETASE INHIBITORS |
| WO2006088705A1 (en) | 2005-02-14 | 2006-08-24 | Wyeth | Terphenyl guanidines as [beta symbol] -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 |
-
2006
- 2006-01-09 EP EP10173563A patent/EP2264036A1/en not_active Withdrawn
- 2006-01-09 BR BRPI0606690-9A patent/BRPI0606690A2/pt not_active IP Right Cessation
- 2006-01-09 CN CNA2006800021783A patent/CN101103034A/zh active Pending
- 2006-01-09 JP JP2007551307A patent/JP2008526966A/ja not_active Withdrawn
- 2006-01-09 AU AU2006205127A patent/AU2006205127A1/en not_active Abandoned
- 2006-01-09 WO PCT/US2006/000656 patent/WO2006076284A2/en not_active Ceased
- 2006-01-09 MX MX2007008555A patent/MX2007008555A/es unknown
- 2006-01-09 CA CA002593515A patent/CA2593515A1/en not_active Abandoned
- 2006-01-09 KR KR1020077016053A patent/KR20070095948A/ko not_active Withdrawn
- 2006-01-09 EP EP06717815A patent/EP1836208A2/en not_active Withdrawn
- 2006-01-09 RU RU2007126570/04A patent/RU2007126570A/ru unknown
- 2006-01-10 PE PE2006000052A patent/PE20060842A1/es not_active Application Discontinuation
- 2006-01-11 GT GT200600009A patent/GT200600009A/es unknown
- 2006-01-13 US US11/332,732 patent/US7563796B2/en not_active Expired - Fee Related
- 2006-01-13 AR ARP060100150A patent/AR052458A1/es not_active Application Discontinuation
- 2006-01-13 PA PA20068660001A patent/PA8660001A1/es unknown
- 2006-01-13 TW TW095101509A patent/TW200637866A/zh unknown
-
2007
- 2007-06-14 IL IL183938A patent/IL183938A0/en unknown
- 2007-06-18 NO NO20073099A patent/NO20073099L/no not_active Application Discontinuation
- 2007-07-12 CR CR9244A patent/CR9244A/es not_active Application Discontinuation
- 2007-07-13 ZA ZA200705783A patent/ZA200705783B/xx unknown
-
2009
- 2009-06-18 US US12/487,395 patent/US20090253716A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| JP2008526966A (ja) | 2008-07-24 |
| CR9244A (es) | 2007-09-07 |
| CN101103034A (zh) | 2008-01-09 |
| GT200600009A (es) | 2006-08-17 |
| WO2006076284A3 (en) | 2007-04-19 |
| WO2006076284A2 (en) | 2006-07-20 |
| US7563796B2 (en) | 2009-07-21 |
| EP1836208A2 (en) | 2007-09-26 |
| TW200637866A (en) | 2006-11-01 |
| NO20073099L (no) | 2007-07-31 |
| PA8660001A1 (es) | 2006-09-08 |
| ZA200705783B (en) | 2008-09-25 |
| US20090253716A1 (en) | 2009-10-08 |
| US20060160828A1 (en) | 2006-07-20 |
| IL183938A0 (en) | 2007-10-31 |
| MX2007008555A (es) | 2007-11-21 |
| CA2593515A1 (en) | 2006-07-20 |
| EP2264036A1 (en) | 2010-12-22 |
| KR20070095948A (ko) | 2007-10-01 |
| PE20060842A1 (es) | 2006-10-12 |
| RU2007126570A (ru) | 2009-02-20 |
| AU2006205127A1 (en) | 2006-07-20 |
| BRPI0606690A2 (pt) | 2009-07-14 |
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| Date | Code | Title | Description |
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| FA | Abandonment or withdrawal |