AR074341A1 - Derivados heterociclicos de isoindol, inhibidores de proteinasas bace, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento y/o prevencion de patologias relacionadas a deficiencias cognitivas, tales como alzheimer. - Google Patents
Derivados heterociclicos de isoindol, inhibidores de proteinasas bace, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento y/o prevencion de patologias relacionadas a deficiencias cognitivas, tales como alzheimer.Info
- Publication number
- AR074341A1 AR074341A1 ARP090104400A ARP090104400A AR074341A1 AR 074341 A1 AR074341 A1 AR 074341A1 AR P090104400 A ARP090104400 A AR P090104400A AR P090104400 A ARP090104400 A AR P090104400A AR 074341 A1 AR074341 A1 AR 074341A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- heteroaryl
- alkenyl
- aryl
- alkynyl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D403/10—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 carbon chain containing aromatic rings
Abstract
etiles para el tratamiento y/o prevención de patologías relacionadas con Ab tales como síndrome de Down, angiopatía b-amiloide tal como, a modo no taxativo, angiopatía amiloide cerebral o hemorragia cerebral hereditaria, trastornos asociados con deficiencia cognitiva tales como, a modo no taxativo, deterioro cognitivo leve, enfermedad de Alzheimer, pérdida de memoria, síntomas de déficit atencional asociados con la enfermedad de Alzheimer, neurodegeneración asociada con enfermedades tales como enfermedad de Alzheimer o demencia, incluyendo demencia de origen mixto vascular y degenerativo, demencia presenil, demencia senil y demencia asociada con la enfermedad de Parkinson, parálisis supranuclear progresiva o degeneración córtico-basal. Reivindicación 1: Un compuesto de acuerdo con la fórmula (1) en donde R1 se selecciona de halógeno, ciano, NO2, SO2R2, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, NR3R4, OR2, C(O)R2, C(O)NR3R4 y COOR2, en donde dicho alquilo C1-6, alquenilo C2-6 o alquinilo C2-6 está opcionalmente sustituido por uno o más R7; R2 es alquilo C1-6, alquenilo C2-6 o alquinilo C2-6, en donde dicho alquilo C1-6, alquenilo C2-6 o alquinilo C2-6 está opcionalmente sustituido por uno o más R7; R3 y R4 se seleccionan independientemente de hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, heterociclilo y carbociclilo, en donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, heterociclilo o carbociclilo está opcionalmente sustituido por uno o más R7; o R3 y R4 junto con el átomo al que están unidos, forman un anillo de 4 a 7 miembros; A se selecciona de arilo y heteroarilo, en donde dicho arilo o heteroarilo está opcionalmente sustituido por uno o más R5; B es arilo o heteroarilo, en donde dicho arilo o heteroarilo está opcionalmente sustituido por uno o más R6; C se selecciona de hidrógeno, halógeno, ciano, arilo, heteroarilo, heterociclilo, cicloalquilo C3-6, cicloalquenilo C3-6, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquil C1-6-cicloalquilo C3-6, alquil C1-6-heterociclilo C3-6, alquil C1-6-arilo, alquil C1-6-heteroarilo y alquenil C2-6-cicloalquilo C3-6, en donde dicho arilo, heteroarilo heterociclilo, cicloalquilo C3-6, cicloalquenilo C3-6, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquil C1-6-cicloalquilo C3-6, alquil C1-6-heterociclilo C3-6, alquil C1-6-arilo, alquil C1-6-heteroarilo o alquenil C2-6-cicloalquilo C3-6, está opcionalmente sustituido por uno a tres R7; R5 se selecciona de halógeno, ciano, alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-6, O-alquilo C1-6 y O-alquil C1-6-arilo, en donde dicho alquilo C1-6, cicloalquilo C3-6, O-alquilo C1-6 u O-alquil C1-6-arilo, está opcionalmente sustituido por uno a tres R7; R6 es halógeno, hidroxi o ciano; R7 se selecciona de halógeno, alquilo C1-6, SO2-alquilo C1-3, O-alquilo C1-3, O-haloalquilo C1-3, alquil C1-3OH, alquil C1-3NR8R9, OH, ciano, C(O)O-alquilo C1-3 y NR8R9, en donde dicho alquilo C1-6, SO2-alquilo C1-3, O-alquilo C1-3, O-haloalquilo C1-3, alquil C1-3OH, alquil C1-3-NR8R9 o C(O)O-alquilo C1-3 está opcionalmente sustituido por uno o más R10; R8 y R9 se seleccionan independientemente de hidrógeno, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquil C1-3-NR11R12, alquil C1-3Oarilo, heteroarilo, heterociclilo y carbociclilo, en donde dicho alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquil C1-3-NR11R12, alquil C1-3Oarilo, heteroarilo, heterociclilo o carbociclilo, está opcionalmente sustituido por uno o más R10; o R8 y R9 junto con el átomo al que están unidos forman un anillo de 4 a 6 miembros; R10 se selecciona de halo, alquilo C1-3, O-alquilo C1-3 y O-haloalquilo C1-3; R11 y R12 se seleccionan independientemente de hidrógeno, alquilo C1-3 y haloalquilo C1-3; m es 0, 1 ó 2; con la condición de que cuando C es alquilo C1-6 entonces R7 no es O-alquilo C1-3 u O-haloalquilo C1-3; como una base libre o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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US11463408P | 2008-11-14 | 2008-11-14 | |
US13976708P | 2008-12-22 | 2008-12-22 | |
US22165309P | 2009-06-30 | 2009-06-30 |
Publications (1)
Publication Number | Publication Date |
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AR074341A1 true AR074341A1 (es) | 2011-01-12 |
Family
ID=42170158
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ARP090104400A AR074341A1 (es) | 2008-11-14 | 2009-11-13 | Derivados heterociclicos de isoindol, inhibidores de proteinasas bace, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento y/o prevencion de patologias relacionadas a deficiencias cognitivas, tales como alzheimer. |
Country Status (24)
Country | Link |
---|---|
US (2) | US8030500B2 (es) |
EP (1) | EP2367814A4 (es) |
JP (1) | JP2012508734A (es) |
KR (1) | KR20110091540A (es) |
CN (1) | CN102282140A (es) |
AR (1) | AR074341A1 (es) |
AU (1) | AU2009314664A1 (es) |
BR (1) | BRPI0921879A2 (es) |
CA (1) | CA2743938A1 (es) |
CL (1) | CL2011001098A1 (es) |
CO (1) | CO6362004A2 (es) |
CR (1) | CR20110255A (es) |
CU (1) | CU20110106A7 (es) |
DO (1) | DOP2011000138A (es) |
EA (1) | EA201190020A1 (es) |
EC (1) | ECSP11011051A (es) |
IL (1) | IL212590A0 (es) |
MX (1) | MX2011004918A (es) |
NI (1) | NI201100099A (es) |
PE (1) | PE20110875A1 (es) |
TW (1) | TW201020244A (es) |
UY (1) | UY32241A (es) |
WO (1) | WO2010056196A1 (es) |
ZA (1) | ZA201104396B (es) |
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JP2009520686A (ja) | 2005-11-21 | 2009-05-28 | アストラゼネカ・アクチエボラーグ | 新規な2−アミノ−イミダゾール−4−オン化合物並びに認知障害、アルツハイマー病、神経変性及び認知症の治療に使用する医薬の製造におけるその使用 |
AR058381A1 (es) | 2005-12-19 | 2008-01-30 | Astrazeneca Ab | Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica |
EP2004630A4 (en) | 2006-04-05 | 2010-05-19 | Astrazeneca Ab | 2-AMINOPYRIMIDIN-4-ONES AND THEIR USE FOR THE TREATMENT OR PREVENTION OF PATHOLOGIES RELATED TO PROTEIN A |
TW200808751A (en) | 2006-04-13 | 2008-02-16 | Astrazeneca Ab | New compounds |
US8168641B2 (en) | 2006-06-12 | 2012-05-01 | Schering Corporation | Aspartyl protease inhibitors |
TW200808796A (en) | 2006-06-14 | 2008-02-16 | Astrazeneca Ab | New compounds III |
TW200815443A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds I |
TW200815449A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds II |
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 |
WO2008076044A1 (en) | 2006-12-20 | 2008-06-26 | Astrazeneca Ab | Novel 2-amino-5, 5-diaryl-imidazol-4-ones |
TW200831091A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
TW200831484A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
TW200902503A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
WO2009005470A1 (en) * | 2007-07-05 | 2009-01-08 | Astrazeneca Ab | Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors |
WO2009005471A1 (en) * | 2007-07-05 | 2009-01-08 | Astrazeneca Ab | Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors |
US20100125081A1 (en) | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | New compounds 574 |
WO2010056195A1 (en) | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | New compounds 575 |
EP2485590B1 (en) | 2009-10-08 | 2015-01-07 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
US8563543B2 (en) | 2009-10-08 | 2013-10-22 | 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 |
UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування |
-
2009
- 2009-11-12 TW TW098138485A patent/TW201020244A/zh unknown
- 2009-11-13 CA CA2743938A patent/CA2743938A1/en not_active Abandoned
- 2009-11-13 US US12/618,212 patent/US8030500B2/en not_active Expired - Fee Related
- 2009-11-13 UY UY0001032241A patent/UY32241A/es not_active Application Discontinuation
- 2009-11-13 AR ARP090104400A patent/AR074341A1/es unknown
- 2009-11-13 CN CN2009801545281A patent/CN102282140A/zh active Pending
- 2009-11-13 EA EA201190020A patent/EA201190020A1/ru unknown
- 2009-11-13 JP JP2011536289A patent/JP2012508734A/ja active Pending
- 2009-11-13 EP EP09826375A patent/EP2367814A4/en not_active Withdrawn
- 2009-11-13 BR BRPI0921879A patent/BRPI0921879A2/pt not_active Application Discontinuation
- 2009-11-13 AU AU2009314664A patent/AU2009314664A1/en not_active Abandoned
- 2009-11-13 WO PCT/SE2009/051295 patent/WO2010056196A1/en active Application Filing
- 2009-11-13 KR KR1020117013516A patent/KR20110091540A/ko not_active Application Discontinuation
- 2009-11-13 PE PE2011001034A patent/PE20110875A1/es not_active Application Discontinuation
- 2009-11-13 MX MX2011004918A patent/MX2011004918A/es not_active Application Discontinuation
-
2011
- 2011-04-28 IL IL212590A patent/IL212590A0/en unknown
- 2011-04-28 CO CO11052264A patent/CO6362004A2/es not_active Application Discontinuation
- 2011-05-13 CU CU20110106A patent/CU20110106A7/es unknown
- 2011-05-13 CL CL2011001098A patent/CL2011001098A1/es unknown
- 2011-05-13 DO DO2011000138A patent/DOP2011000138A/es unknown
- 2011-05-13 CR CR20110255A patent/CR20110255A/es unknown
- 2011-05-13 NI NI201100099A patent/NI201100099A/es unknown
- 2011-05-13 EC EC2011011051A patent/ECSP11011051A/es unknown
- 2011-06-13 ZA ZA2011/04396A patent/ZA201104396B/en unknown
- 2011-09-06 US US13/225,707 patent/US20110319426A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
UY32241A (es) | 2010-06-30 |
ECSP11011051A (es) | 2011-06-30 |
JP2012508734A (ja) | 2012-04-12 |
CL2011001098A1 (es) | 2012-02-24 |
EA201190020A1 (ru) | 2012-02-28 |
CN102282140A (zh) | 2011-12-14 |
IL212590A0 (en) | 2011-07-31 |
US20110319426A1 (en) | 2011-12-29 |
KR20110091540A (ko) | 2011-08-11 |
DOP2011000138A (es) | 2011-06-30 |
PE20110875A1 (es) | 2012-01-11 |
CR20110255A (es) | 2011-07-04 |
NI201100099A (es) | 2012-03-19 |
EP2367814A1 (en) | 2011-09-28 |
AU2009314664A1 (en) | 2011-06-23 |
US8030500B2 (en) | 2011-10-04 |
US20100125082A1 (en) | 2010-05-20 |
CU20110106A7 (es) | 2012-01-31 |
CO6362004A2 (es) | 2012-01-20 |
WO2010056196A1 (en) | 2010-05-20 |
BRPI0921879A2 (pt) | 2018-10-16 |
TW201020244A (en) | 2010-06-01 |
ZA201104396B (en) | 2012-03-28 |
EP2367814A4 (en) | 2012-07-04 |
CA2743938A1 (en) | 2010-05-20 |
MX2011004918A (es) | 2011-05-30 |
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