PE20110875A1 - Derivados de isoindol como inhibidores de bace - Google Patents
Derivados de isoindol como inhibidores de baceInfo
- Publication number
- PE20110875A1 PE20110875A1 PE2011001034A PE2011001034A PE20110875A1 PE 20110875 A1 PE20110875 A1 PE 20110875A1 PE 2011001034 A PE2011001034 A PE 2011001034A PE 2011001034 A PE2011001034 A PE 2011001034A PE 20110875 A1 PE20110875 A1 PE 20110875A1
- Authority
- PE
- Peru
- Prior art keywords
- fluoro
- isoindol
- halogen
- amine
- derivatives
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- VHMICKWLTGFITH-UHFFFAOYSA-N 2H-isoindole Chemical class C1=CC=CC2=CNC=C21 VHMICKWLTGFITH-UHFFFAOYSA-N 0.000 title 1
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 208000024827 Alzheimer disease Diseases 0.000 abstract 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 2
- GZPHSAQLYPIAIN-UHFFFAOYSA-N 3-pyridinecarbonitrile Chemical compound N#CC1=CC=CN=C1 GZPHSAQLYPIAIN-UHFFFAOYSA-N 0.000 abstract 1
- ILADHFOYFBUJPH-UHFFFAOYSA-N 7-fluoro-3h-isoindol-1-amine Chemical compound C1=CC(F)=C2C(N)=NCC2=C1 ILADHFOYFBUJPH-UHFFFAOYSA-N 0.000 abstract 1
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract 1
- 201000010374 Down Syndrome Diseases 0.000 abstract 1
- WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical class F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 abstract 1
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 abstract 1
- 206010039966 Senile dementia Diseases 0.000 abstract 1
- 206010044688 Trisomy 21 Diseases 0.000 abstract 1
- 230000002490 cerebral effect Effects 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical group [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
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
-
- 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
-
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE 4-FLUORO-1H-ISOINDOL-3-AMINA DE FORMULA (I) DONDE R1 ES HALOGENO, CN, ALQUILO(C1-C6), ALQUENILO(C2-C6), ENTRE OTROS; A ES ARILO O HETEROARILO OPCIONALMENTE SUSTITUIDO CON R5, EN DONDE R5 ES HALOGENO, CN, CICLOALQUILO(C3-C6), ENTRE OTROS; B ES ARILO O HETEROARILO OPCIONALMENTE SUSTITUIDO CON R6, EN DONDE R6 ES HALOGENO, HIDROXI O CN; C ES H, HALOGENO, CICLOALQUILO(C3-C6), HETEROCICLILO, ENTRE OTROS; m ES DE 0 A 2. SON COMPUESTOS PREFERIDOS: 5-(3-(3-AMINO-4-FLUORO-1-(2-METILPIRIDIN-4-IL)-1H-ISOINDOL-1-IL)-4-FLUOROFENIL)NICOTINONITRILO; 4-FLUORO-1-(2-FLUORO-5-(5-FLUOROPIRIDIN-3-IL)FENIL)-1-(2-METILPIRIDIN-4-IL)-1H-ISOINDOL-3-AMINA; 4-FLUORO-1-(2-FLUORO-5-(PIRIMIDIN-5-IL)FENIL)-1-(2-(TRIFLUOROMETIL)PIRIDIN-4-IL)-1H-ISOINDOL-3-AMINA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA B-SECRETASA (BACE) SIENDO UTILES EN EL TRATAMIENTO DEL SINDROME DE DOWN, ENFERMEDAD DE ALZHEIMER, ANGIOPATIA AMILOIDE CEREBRAL, DEMENCIA SENIL
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 |
|---|---|
| PE20110875A1 true PE20110875A1 (es) | 2012-01-11 |
Family
ID=42170158
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2011001034A PE20110875A1 (es) | 2008-11-14 | 2009-11-13 | Derivados de isoindol como inhibidores de bace |
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) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2537898T3 (es) | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
| TW200815349A (en) | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
| EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| EP2689780A1 (en) | 2007-04-24 | 2014-01-29 | Shionogi & Co., Ltd. | Intermediates for aminodihydrothiazine derivatives substituted with a cyclic group |
| EP2305672B1 (en) | 2008-06-13 | 2019-03-27 | Shionogi & Co., Ltd. | SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY |
| EP2360155A4 (en) | 2008-10-22 | 2012-06-20 | Shionogi & Co | 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT |
| US8563543B2 (en) | 2009-10-08 | 2013-10-22 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace 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 | |
| CN102834384A (zh) | 2009-12-11 | 2012-12-19 | 盐野义制药株式会社 | *嗪衍生物 |
| UY33376A (es) * | 2010-05-12 | 2011-12-30 | Astrazeneca Ab | Sal de tipo hemifumarato |
| WO2012019056A1 (en) | 2010-08-05 | 2012-02-09 | Amgen Inc. | Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use |
| JP5816630B2 (ja) | 2010-10-29 | 2015-11-18 | 塩野義製薬株式会社 | ナフチリジン誘導体 |
| WO2012057247A1 (ja) | 2010-10-29 | 2012-05-03 | 塩野義製薬株式会社 | 縮合アミノジヒドロピリミジン誘導体 |
| US20120165346A1 (en) * | 2010-12-22 | 2012-06-28 | Astrazeneca Ab | Compounds and their use as BACE inhibitors |
| CN103608345A (zh) | 2011-04-26 | 2014-02-26 | 盐野义制药株式会社 | 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂 |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| US10707526B2 (en) | 2015-03-27 | 2020-07-07 | New Dominion Enterprises Inc. | All-inorganic solvents for electrolytes |
| CN105272884B (zh) * | 2015-11-02 | 2017-05-24 | 浙江大学 | 一种邻氰基二苯甲酮衍生物的制备方法 |
| US10707531B1 (en) | 2016-09-27 | 2020-07-07 | New Dominion Enterprises Inc. | All-inorganic solvents for electrolytes |
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| TW200831484A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
| TW200831091A (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 |
| WO2009005471A1 (en) * | 2007-07-05 | 2009-01-08 | Astrazeneca Ab | Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors |
| WO2009005470A1 (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 |
| US20100125087A1 (en) * | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | New compounds 575 |
| WO2011044185A2 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| WO2011044184A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | 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 | |
| US8563543B2 (en) | 2009-10-08 | 2013-10-22 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
-
2009
- 2009-11-12 TW TW098138485A patent/TW201020244A/zh unknown
- 2009-11-13 MX MX2011004918A patent/MX2011004918A/es not_active Application Discontinuation
- 2009-11-13 BR BRPI0921879A patent/BRPI0921879A2/pt not_active Application Discontinuation
- 2009-11-13 AR ARP090104400A patent/AR074341A1/es unknown
- 2009-11-13 EA EA201190020A patent/EA201190020A1/ru unknown
- 2009-11-13 EP EP09826375A patent/EP2367814A4/en not_active Withdrawn
- 2009-11-13 WO PCT/SE2009/051295 patent/WO2010056196A1/en not_active Ceased
- 2009-11-13 JP JP2011536289A patent/JP2012508734A/ja active Pending
- 2009-11-13 CN CN2009801545281A patent/CN102282140A/zh active Pending
- 2009-11-13 AU AU2009314664A patent/AU2009314664A1/en not_active Abandoned
- 2009-11-13 PE PE2011001034A patent/PE20110875A1/es not_active Application Discontinuation
- 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 KR KR1020117013516A patent/KR20110091540A/ko not_active Withdrawn
- 2009-11-13 CA CA2743938A patent/CA2743938A1/en not_active Abandoned
-
2011
- 2011-04-28 CO CO11052264A patent/CO6362004A2/es not_active Application Discontinuation
- 2011-04-28 IL IL212590A patent/IL212590A0/en unknown
- 2011-05-13 CL CL2011001098A patent/CL2011001098A1/es unknown
- 2011-05-13 NI NI201100099A patent/NI201100099A/es unknown
- 2011-05-13 CR CR20110255A patent/CR20110255A/es unknown
- 2011-05-13 CU CU20110106A patent/CU20110106A7/es unknown
- 2011-05-13 DO DO2011000138A patent/DOP2011000138A/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 |
|---|---|
| IL212590A0 (en) | 2011-07-31 |
| NI201100099A (es) | 2012-03-19 |
| ZA201104396B (en) | 2012-03-28 |
| EP2367814A1 (en) | 2011-09-28 |
| JP2012508734A (ja) | 2012-04-12 |
| EP2367814A4 (en) | 2012-07-04 |
| AR074341A1 (es) | 2011-01-12 |
| ECSP11011051A (es) | 2011-06-30 |
| CR20110255A (es) | 2011-07-04 |
| CA2743938A1 (en) | 2010-05-20 |
| TW201020244A (en) | 2010-06-01 |
| CN102282140A (zh) | 2011-12-14 |
| WO2010056196A1 (en) | 2010-05-20 |
| KR20110091540A (ko) | 2011-08-11 |
| UY32241A (es) | 2010-06-30 |
| EA201190020A1 (ru) | 2012-02-28 |
| BRPI0921879A2 (pt) | 2018-10-16 |
| US20110319426A1 (en) | 2011-12-29 |
| CL2011001098A1 (es) | 2012-02-24 |
| AU2009314664A1 (en) | 2011-06-23 |
| DOP2011000138A (es) | 2011-06-30 |
| US20100125082A1 (en) | 2010-05-20 |
| CO6362004A2 (es) | 2012-01-20 |
| CU20110106A7 (es) | 2012-01-31 |
| MX2011004918A (es) | 2011-05-30 |
| US8030500B2 (en) | 2011-10-04 |
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