AR061370A1 - Derivados de imidazopirimidina - Google Patents
Derivados de imidazopirimidinaInfo
- Publication number
- AR061370A1 AR061370A1 ARP070102595A ARP070102595A AR061370A1 AR 061370 A1 AR061370 A1 AR 061370A1 AR P070102595 A ARP070102595 A AR P070102595A AR P070102595 A ARP070102595 A AR P070102595A AR 061370 A1 AR061370 A1 AR 061370A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkynyl
- alkylheteroaryl
- alkenyl
- optionally substituted
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 abstract 43
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 10
- 125000005213 alkyl heteroaryl group Chemical group 0.000 abstract 8
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 7
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 7
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 7
- 125000000623 heterocyclic group Chemical group 0.000 abstract 5
- 101100134925 Gallus gallus COR6 gene Proteins 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 4
- 101100477978 Hypocrea jecorina (strain QM6a) sor6 gene Proteins 0.000 abstract 3
- -1 OR6 Chemical group 0.000 abstract 3
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 3
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 abstract 3
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000004122 cyclic group Chemical group 0.000 abstract 2
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004785 fluoromethoxy group Chemical group [H]C([H])(F)O* 0.000 abstract 1
- 239000012458 free base Substances 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Reivindicacion 1: Un compuesto de formula 1: donde A está independientemente seleccionado de un anillo heterocíclico de 5, 6 o 7 miembros opcionalmente sustituido con uno o más R1; B está independientemente seleccionado de fenilo o de un anillo heteroaromático de 5 o 6 miembros opcionalmente sustituido con uno o más R2, R1 está independientemente seleccionado de halogeno, ciano, nitro, OR6, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquilarilo C0-6, alquilheteroarilo C0-6, alquil C0-6- cicloalquilo C3-6, alquil C0-6-cicloalquenilo C3-6, alquil C0-6-cicloalquinilo C3-6, alquil C0-6-heterociclilo C3-6, NR6R7, CONR6R7, NR6(CO)R7, O(CO)R6, CO2R6, COR6, (SO2)NR6R7, NR6(SO2)R7, SO2R6, SOR6, OSO2R6 y SO3R6, donde dichos alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquilarilo C0-6, alquilheteroarilo C0-6, alquil C0-6-cicloalquilo C3-6, alquil C0-6-cicloalquenilo C3-6, alquil C0-6-cicloalquinilo C3-6 y alquil C0-6 heterociclilo C3-6 pueden estar opcionalmente sustituido con uno o más C; o dos sustituyentes R1 junto con el átomo al cual ellos están unidos, forman un anillo cíclico o heterocíclico opcionalmente sustituido con uno o más C; R2, R3 y R4 están independientemente seleccionados de halogeno, ciano, nitro, OR6, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquilarilo C0-6, alquilheteroarilo C0-6, alquil C0-6-cicloalquilo C3-6, alquil C0-6-cicloalquenilo C3-6, alquil C0-6-cicloalquinilo C3-6, alquil C0-6-heterociclilo C3-6, NR6R7, CONR6R7, NR6(CO)R7, O(CO)R6, CO2R6, COR6, (SO2)NR6R7, NR6(SO2)R7, SO2R6, SOR6, OSO2R6 y SO3R6, donde dichos alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquilarilo C0-6, alquilheteroarilo C0-6, alquil C0-6-cicloalquilo C3-6, alquil C0-6-cicloalquenilo C3-6, alquil C0- 6-cicloalquinilo C3-6 y alquil C0-6 heterociclilo C3-6 pueden estar opcionalmente sustituido con uno o más C; o dos sustituyentes R2, R3 o R4 pueden conjuntamente con los átomos a los cuales ellos están unidos, forman un anillo cíclico o heterocíclico opcionalmente sustituido con uno o más C; R5 está independientemente seleccionado de hidrogeno, ciano, OR6, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquilarilo C0-6, alquilheteroarilo C0-6, alquil C0-6-cicloalquilo C3-6, alquil C0-6-cicloalquenilo C3-6, alquil C0-6-cicloalquinilo C3-6, alquiI C0-6heterociclilo C3-6, CONR6R7, CO2R6, COR6, SO2R6 y SO3R6 donde dicho alquiIo C1-6, alquenilo C2-6, aIquinilo C2-6, alquilarilo C0-6, alquilheteroarilo C0-6, alquil C0-6- cicloalquilo C3-6, alquiI C0-6-cicloalquenilo C3-6, alquil C0-6-cicloalquinilo C3-6, alquil C0-6-heterociclilo C3-6 pueden estar opcionalmente sustituido con uno o más C; C está independientemente seleccionado de halogeno, nitro, CN, OR6, alquilo C1- 6, alquenilo C2-6, alquinilo C2-6, alquilarilo C0-6, alquilheteroarilo C0-6, alquil C0-6-cicloalquilo C3-6, alquil C0-6-cicloalquenilo C3-6, alquil C0-6-cicloalquinilo C3-6, alquilheterociclilo C0-6, fluormetilo, difluormetilo, trifluormetilo, fluorrnetoxi, difluormetoxi, trifluormetoxi, NR6R7, CONR6R7, NR6(CO)R7, O(CO)R6, CO2R6, COR6, (SO2)NR6R7, NR6SO2R7, SO2R6, SOR6, OSO2R6 y SO3R6, donde dichos alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquilarilo C0-6, alquilheteroarilo C0-6, alquil C0-6-cicloalquilo C3-6, alquil C0-6-cicloalquenilo C3-6, alquil C0-6-cicloalquinilo C3-6 o alquilheterociclilo C0-6 pueden estar opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halo, nitro, ciano, OR6, alquiIo C1-6, fluormetilo, difluormetilo, trifluormetilo, fluormetoxi, difluormetoxi y trifluormetoxi; R6 y R7 están independientemente seleccionados de hidrogeno, alquilo C1-6, alquilarilo C0-6, heteroarilo, alquil C0-6-cicloalquilo C3-6, alquil C0- 6cicloalquenilo C3-6, aIquil C0-6-cicloalquinilo C3-6, alquilheterociclilo C0-6, fluormetilo, difluormetilo y trifluormetilo; o R6 y R7 pueden formar conjuntamente un anillo heterocíclico de 5 o 6 miembros que contiene uno o más heteroátomos seleccionados entre N, O o S; m= 0,1, 2 o 3; n= 0,1, 2 o 3 p= 0,1, 2 o 3; q= 0,1, 2 o 3; como una base libre o una sal, solvato o solvato de una sal farmacéuticamente aceptable de los mismos.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US81376706P | 2006-06-14 | 2006-06-14 | |
| US89699207P | 2007-03-26 | 2007-03-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR061370A1 true AR061370A1 (es) | 2008-08-20 |
Family
ID=38831993
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070102595A AR061370A1 (es) | 2006-06-14 | 2007-06-13 | Derivados de imidazopirimidina |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20080058349A1 (es) |
| EP (1) | EP2035424A1 (es) |
| JP (1) | JP2009539974A (es) |
| AR (1) | AR061370A1 (es) |
| CL (1) | CL2007001734A1 (es) |
| TW (1) | TW200815449A (es) |
| UY (1) | UY30414A1 (es) |
| WO (1) | WO2007145569A1 (es) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7763609B2 (en) * | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| JP2008508289A (ja) | 2004-07-28 | 2008-03-21 | シェーリング コーポレイション | 大環状βセクレターゼ阻害剤 |
| AU2006259572A1 (en) * | 2005-06-14 | 2006-12-28 | Schering Corporation | Aspartyl protease inhibitors |
| ES2436795T3 (es) | 2005-06-14 | 2014-01-07 | Merck Sharp & Dohme Corp. | Inhibidores heterocíclicos de aspartil proteasa, preparación y uso de los mismos |
| WO2007146225A2 (en) * | 2006-06-12 | 2007-12-21 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| TW200815447A (en) * | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds IV |
| TW200815349A (en) | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
| WO2008063114A1 (en) * | 2006-11-20 | 2008-05-29 | Astrazeneca Ab | Amino- imidazolones and their use as medicament for treating cognitive impairment alzheimer disease, neurodegeneration and dementia |
| KR20110003347A (ko) * | 2008-04-22 | 2011-01-11 | 쉐링 코포레이션 | Ｂａｃｅ-1 억제제로서의 페닐-치환된 2-이미노-3-메틸 피롤로 피리미디논 화합물, 조성물 및 이의 용도 |
| TW201020244A (en) | 2008-11-14 | 2010-06-01 | Astrazeneca Ab | New compounds |
| EP2485590B1 (en) | 2009-10-08 | 2015-01-07 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| EP2485591B1 (en) | 2009-10-08 | 2016-03-23 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| US8569310B2 (en) | 2009-10-08 | 2013-10-29 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as BACE-1 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 |
| US9145426B2 (en) | 2011-04-07 | 2015-09-29 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
| CN103874496A (zh) | 2011-08-22 | 2014-06-18 | 默沙东公司 | 作为bace抑制剂的2-螺-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其用途 |
| CN104270945B (zh) | 2012-03-19 | 2017-03-29 | 巴克老龄化研究所 | App特异性bace抑制剂(asbi)及其用途 |
| EP2908825B1 (en) | 2012-10-17 | 2018-04-18 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2908824B1 (en) | 2012-10-17 | 2018-05-02 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| WO2014127042A1 (en) | 2013-02-12 | 2014-08-21 | Buck Institute For Research On Aging | Hydantoins that modulate bace-mediated app processing |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1997646A (zh) * | 2004-06-16 | 2007-07-11 | 惠氏公司 | 作为β－分泌酶抑制剂的二苯基咪唑并嘧啶胺和二苯基咪唑并咪唑胺 |
| CN101103034A (zh) * | 2005-01-14 | 2008-01-09 | 惠氏公司 | 抑制β-分泌酶的氨基-咪唑酮 |
-
2007
- 2007-06-07 TW TW096120552A patent/TW200815449A/zh unknown
- 2007-06-11 US US11/761,120 patent/US20080058349A1/en not_active Abandoned
- 2007-06-12 EP EP07748235A patent/EP2035424A1/en not_active Withdrawn
- 2007-06-12 JP JP2009515345A patent/JP2009539974A/ja active Pending
- 2007-06-12 WO PCT/SE2007/000572 patent/WO2007145569A1/en not_active Ceased
- 2007-06-13 AR ARP070102595A patent/AR061370A1/es unknown
- 2007-06-13 CL CL2007001734A patent/CL2007001734A1/es unknown
- 2007-06-14 UY UY30414A patent/UY30414A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| WO2007145569A9 (en) | 2008-12-11 |
| UY30414A1 (es) | 2008-01-31 |
| JP2009539974A (ja) | 2009-11-19 |
| TW200815449A (en) | 2008-04-01 |
| WO2007145569A1 (en) | 2007-12-21 |
| EP2035424A1 (en) | 2009-03-18 |
| US20080058349A1 (en) | 2008-03-06 |
| CL2007001734A1 (es) | 2008-01-18 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |