JP2012508734A - Bace阻害剤としての置換イソインドール類及びそれらの使用 - Google Patents
Bace阻害剤としての置換イソインドール類及びそれらの使用 Download PDFInfo
- Publication number
- JP2012508734A JP2012508734A JP2011536289A JP2011536289A JP2012508734A JP 2012508734 A JP2012508734 A JP 2012508734A JP 2011536289 A JP2011536289 A JP 2011536289A JP 2011536289 A JP2011536289 A JP 2011536289A JP 2012508734 A JP2012508734 A JP 2012508734A
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- phenyl
- fluoro
- pyridyl
- pyrimidin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 0 *c1nccc(C(c2cccc(F)c22)(N=C2N)I)c1 Chemical compound *c1nccc(C(c2cccc(F)c22)(N=C2N)I)c1 0.000 description 1
- SYQQPPJAZKTFNJ-RELWKKBWSA-N CC(C)(C)S(/N=C(\c1cccc(Br)c1)/c1cccc(F)c1C#C)=O Chemical compound CC(C)(C)S(/N=C(\c1cccc(Br)c1)/c1cccc(F)c1C#C)=O SYQQPPJAZKTFNJ-RELWKKBWSA-N 0.000 description 1
- KZVSSVXPEVRMJY-UHFFFAOYSA-N CC(c(c1ccc2)c2F)=NC1(C1=CC=NCC1)c1cccc(-c2cncc(F)c2)c1 Chemical compound CC(c(c1ccc2)c2F)=NC1(C1=CC=NCC1)c1cccc(-c2cncc(F)c2)c1 KZVSSVXPEVRMJY-UHFFFAOYSA-N 0.000 description 1
- NPFILZKBYLIOSV-UHFFFAOYSA-N CC1(C)OB(c2cc(Cl)cc(F)c2C#N)OC1(C)C Chemical compound CC1(C)OB(c2cc(Cl)cc(F)c2C#N)OC1(C)C NPFILZKBYLIOSV-UHFFFAOYSA-N 0.000 description 1
- LCLBYJCQVLLEOK-UHFFFAOYSA-N Cc1cc(C(C(CC=C2)C3=C2F)(c2cc([Br]=C)ccc2)N=C3N)nc(C)n1 Chemical compound Cc1cc(C(C(CC=C2)C3=C2F)(c2cc([Br]=C)ccc2)N=C3N)nc(C)n1 LCLBYJCQVLLEOK-UHFFFAOYSA-N 0.000 description 1
- AUBWOOMBEPBCKT-UHFFFAOYSA-N Cc1cc(C(c2cccc(F)c22)(c3ccnc(-c4cncnc4)c3)N=C2N)cc(C)c1OC Chemical compound Cc1cc(C(c2cccc(F)c22)(c3ccnc(-c4cncnc4)c3)N=C2N)cc(C)c1OC AUBWOOMBEPBCKT-UHFFFAOYSA-N 0.000 description 1
- OSHCTQXVTOPUFG-UHFFFAOYSA-N NC(c(c1ccc2)c2F)=NC1(c(cc1-c2cnccn2)ccc1O)c1ccnc(C(F)(F)F)c1 Chemical compound NC(c(c1ccc2)c2F)=NC1(c(cc1-c2cnccn2)ccc1O)c1ccnc(C(F)(F)F)c1 OSHCTQXVTOPUFG-UHFFFAOYSA-N 0.000 description 1
- JTYGZAPMRYLRCN-UHFFFAOYSA-N NC(c(c1ccc2)c2F)=NC1(c1ccncc1)c1cccc(-c2cncnc2)c1 Chemical compound NC(c(c1ccc2)c2F)=NC1(c1ccncc1)c1cccc(-c2cncnc2)c1 JTYGZAPMRYLRCN-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11463408P | 2008-11-14 | 2008-11-14 | |
| US61/114,634 | 2008-11-14 | ||
| US13976708P | 2008-12-22 | 2008-12-22 | |
| US61/139,767 | 2008-12-22 | ||
| US22165309P | 2009-06-30 | 2009-06-30 | |
| US61/221,653 | 2009-06-30 | ||
| PCT/SE2009/051295 WO2010056196A1 (en) | 2008-11-14 | 2009-11-13 | New compounds 578 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012508734A true JP2012508734A (ja) | 2012-04-12 |
| JP2012508734A5 JP2012508734A5 (https=) | 2012-12-20 |
Family
ID=42170158
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011536289A Pending JP2012508734A (ja) | 2008-11-14 | 2009-11-13 | Bace阻害剤としての置換イソインドール類及びそれらの使用 |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US8030500B2 (https=) |
| EP (1) | EP2367814A4 (https=) |
| JP (1) | JP2012508734A (https=) |
| KR (1) | KR20110091540A (https=) |
| CN (1) | CN102282140A (https=) |
| AR (1) | AR074341A1 (https=) |
| AU (1) | AU2009314664A1 (https=) |
| BR (1) | BRPI0921879A2 (https=) |
| CA (1) | CA2743938A1 (https=) |
| CL (1) | CL2011001098A1 (https=) |
| CO (1) | CO6362004A2 (https=) |
| CR (1) | CR20110255A (https=) |
| CU (1) | CU20110106A7 (https=) |
| DO (1) | DOP2011000138A (https=) |
| EA (1) | EA201190020A1 (https=) |
| EC (1) | ECSP11011051A (https=) |
| IL (1) | IL212590A0 (https=) |
| MX (1) | MX2011004918A (https=) |
| NI (1) | NI201100099A (https=) |
| PE (1) | PE20110875A1 (https=) |
| TW (1) | TW201020244A (https=) |
| UY (1) | UY32241A (https=) |
| WO (1) | WO2010056196A1 (https=) |
| ZA (1) | ZA201104396B (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2416603C9 (ru) | 2005-10-25 | 2012-06-20 | Сионоги Энд Ко., Лтд. | Производные аминодигидротиазина |
| 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 |
| EP2147914B1 (en) | 2007-04-24 | 2014-06-04 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivatives substituted with cyclic groups |
| WO2009151098A1 (ja) | 2008-06-13 | 2009-12-17 | 塩野義製薬株式会社 | βセクレターゼ阻害作用を有する含硫黄複素環誘導体 |
| CN102186841A (zh) | 2008-10-22 | 2011-09-14 | 盐野义制药株式会社 | 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物 |
| 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 |
| TWI488852B (zh) | 2009-12-11 | 2015-06-21 | Shionogi & Co | 衍生物 |
| WO2011142716A1 (en) * | 2010-05-12 | 2011-11-17 | Astrazeneca Ab | Novel hemifumarate salt of isoindole compound acting as bace inhibitor |
| 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 |
| JP5766198B2 (ja) | 2010-10-29 | 2015-08-19 | 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 |
| TW201247635A (en) | 2011-04-26 | 2012-12-01 | Shionogi & Co | Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| WO2016160703A1 (en) | 2015-03-27 | 2016-10-06 | Harrup Mason K | 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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| WO2007149033A1 (en) * | 2006-06-22 | 2007-12-27 | Astrazeneca Ab | Substituted isoindoles as bace inhibitors and their use |
| JP2008526966A (ja) * | 2005-01-14 | 2008-07-24 | ワイス | β−セクレターゼの阻害のためのアミノ−イミダゾロン |
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| KR20090015967A (ko) | 2006-06-12 | 2009-02-12 | 쉐링 코포레이션 | 헤테로사이클릭 아스파르틸 프로테아제 억제제 |
| 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 |
| TW200808796A (en) | 2006-06-14 | 2008-02-16 | Astrazeneca Ab | New compounds III |
| TW200815447A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds IV |
| 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 |
| TW200831484A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
| TW200831091A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
| WO2008076044A1 (en) | 2006-12-20 | 2008-06-26 | Astrazeneca Ab | Novel 2-amino-5, 5-diaryl-imidazol-4-ones |
| 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 |
| US20100125087A1 (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 |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| EP2485920B1 (en) | 2009-10-08 | 2016-04-27 | 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 |
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2009
- 2009-11-12 TW TW098138485A patent/TW201020244A/zh unknown
- 2009-11-13 CN CN2009801545281A patent/CN102282140A/zh active Pending
- 2009-11-13 MX MX2011004918A patent/MX2011004918A/es not_active Application Discontinuation
- 2009-11-13 WO PCT/SE2009/051295 patent/WO2010056196A1/en not_active Ceased
- 2009-11-13 EP EP09826375A patent/EP2367814A4/en not_active Withdrawn
- 2009-11-13 JP JP2011536289A patent/JP2012508734A/ja active Pending
- 2009-11-13 CA CA2743938A patent/CA2743938A1/en not_active Abandoned
- 2009-11-13 AU AU2009314664A patent/AU2009314664A1/en not_active Abandoned
- 2009-11-13 KR KR1020117013516A patent/KR20110091540A/ko not_active Withdrawn
- 2009-11-13 US US12/618,212 patent/US8030500B2/en not_active Expired - Fee Related
- 2009-11-13 EA EA201190020A patent/EA201190020A1/ru unknown
- 2009-11-13 PE PE2011001034A patent/PE20110875A1/es not_active Application Discontinuation
- 2009-11-13 AR ARP090104400A patent/AR074341A1/es unknown
- 2009-11-13 UY UY0001032241A patent/UY32241A/es not_active Application Discontinuation
- 2009-11-13 BR BRPI0921879A patent/BRPI0921879A2/pt 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 DO DO2011000138A patent/DOP2011000138A/es unknown
- 2011-05-13 CR CR20110255A patent/CR20110255A/es unknown
- 2011-05-13 CU CU20110106A patent/CU20110106A7/es unknown
- 2011-05-13 CL CL2011001098A patent/CL2011001098A1/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
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| JP2008526966A (ja) * | 2005-01-14 | 2008-07-24 | ワイス | β−セクレターゼの阻害のためのアミノ−イミダゾロン |
| WO2007149033A1 (en) * | 2006-06-22 | 2007-12-27 | Astrazeneca Ab | Substituted isoindoles as bace inhibitors and their use |
Also Published As
| Publication number | Publication date |
|---|---|
| CA2743938A1 (en) | 2010-05-20 |
| US20100125082A1 (en) | 2010-05-20 |
| BRPI0921879A2 (pt) | 2018-10-16 |
| CR20110255A (es) | 2011-07-04 |
| EA201190020A1 (ru) | 2012-02-28 |
| CL2011001098A1 (es) | 2012-02-24 |
| AR074341A1 (es) | 2011-01-12 |
| CO6362004A2 (es) | 2012-01-20 |
| CN102282140A (zh) | 2011-12-14 |
| DOP2011000138A (es) | 2011-06-30 |
| AU2009314664A1 (en) | 2011-06-23 |
| US8030500B2 (en) | 2011-10-04 |
| WO2010056196A1 (en) | 2010-05-20 |
| US20110319426A1 (en) | 2011-12-29 |
| UY32241A (es) | 2010-06-30 |
| EP2367814A1 (en) | 2011-09-28 |
| IL212590A0 (en) | 2011-07-31 |
| ZA201104396B (en) | 2012-03-28 |
| CU20110106A7 (es) | 2012-01-31 |
| TW201020244A (en) | 2010-06-01 |
| KR20110091540A (ko) | 2011-08-11 |
| ECSP11011051A (es) | 2011-06-30 |
| PE20110875A1 (es) | 2012-01-11 |
| NI201100099A (es) | 2012-03-19 |
| MX2011004918A (es) | 2011-05-30 |
| EP2367814A4 (en) | 2012-07-04 |
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