JP2012532874A5 - - Google Patents

Download PDF

Info

Publication number
JP2012532874A5
JP2012532874A5 JP2012519660A JP2012519660A JP2012532874A5 JP 2012532874 A5 JP2012532874 A5 JP 2012532874A5 JP 2012519660 A JP2012519660 A JP 2012519660A JP 2012519660 A JP2012519660 A JP 2012519660A JP 2012532874 A5 JP2012532874 A5 JP 2012532874A5
Authority
JP
Japan
Prior art keywords
pharmaceutically acceptable
pharmaceutical formulation
acceptable salt
compound according
fluoropicolinamide
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.)
Granted
Application number
JP2012519660A
Other languages
English (en)
Japanese (ja)
Other versions
JP5666578B2 (ja
JP2012532874A (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2010/041034 external-priority patent/WO2011005738A1/en
Publication of JP2012532874A publication Critical patent/JP2012532874A/ja
Publication of JP2012532874A5 publication Critical patent/JP2012532874A5/ja
Application granted granted Critical
Publication of JP5666578B2 publication Critical patent/JP5666578B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

JP2012519660A 2009-07-09 2010-07-06 Bace阻害剤 Expired - Fee Related JP5666578B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22424109P 2009-07-09 2009-07-09
US61/224,241 2009-07-09
PCT/US2010/041034 WO2011005738A1 (en) 2009-07-09 2010-07-06 Bace inhibitors

Publications (3)

Publication Number Publication Date
JP2012532874A JP2012532874A (ja) 2012-12-20
JP2012532874A5 true JP2012532874A5 (cg-RX-API-DMAC10.html) 2013-08-15
JP5666578B2 JP5666578B2 (ja) 2015-02-12

Family

ID=42985394

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2012519660A Expired - Fee Related JP5666578B2 (ja) 2009-07-09 2010-07-06 Bace阻害剤

Country Status (26)

Country Link
US (2) US8278441B2 (cg-RX-API-DMAC10.html)
EP (1) EP2451793B1 (cg-RX-API-DMAC10.html)
JP (1) JP5666578B2 (cg-RX-API-DMAC10.html)
KR (1) KR101362557B1 (cg-RX-API-DMAC10.html)
CN (1) CN102471296B (cg-RX-API-DMAC10.html)
AR (1) AR077277A1 (cg-RX-API-DMAC10.html)
AU (1) AU2010270691B8 (cg-RX-API-DMAC10.html)
BR (1) BR112012000525A2 (cg-RX-API-DMAC10.html)
CA (1) CA2764429C (cg-RX-API-DMAC10.html)
CL (1) CL2012000033A1 (cg-RX-API-DMAC10.html)
CO (1) CO6480979A2 (cg-RX-API-DMAC10.html)
CR (1) CR20120011A (cg-RX-API-DMAC10.html)
DO (1) DOP2012000004A (cg-RX-API-DMAC10.html)
EA (1) EA019892B1 (cg-RX-API-DMAC10.html)
EC (1) ECSP12011581A (cg-RX-API-DMAC10.html)
HN (1) HN2012000012A (cg-RX-API-DMAC10.html)
IL (1) IL216742A0 (cg-RX-API-DMAC10.html)
MA (1) MA33492B1 (cg-RX-API-DMAC10.html)
MX (1) MX2012000510A (cg-RX-API-DMAC10.html)
NZ (1) NZ596579A (cg-RX-API-DMAC10.html)
PE (1) PE20120632A1 (cg-RX-API-DMAC10.html)
SG (1) SG177594A1 (cg-RX-API-DMAC10.html)
TN (1) TN2011000673A1 (cg-RX-API-DMAC10.html)
TW (1) TWI405765B (cg-RX-API-DMAC10.html)
WO (1) WO2011005738A1 (cg-RX-API-DMAC10.html)
ZA (1) ZA201109385B (cg-RX-API-DMAC10.html)

Families Citing this family (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
ES2537898T3 (es) * 2005-10-25 2015-06-15 Shionogi & Co., Ltd. Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
KR20100017255A (ko) * 2007-04-24 2010-02-16 시오노기 앤드 컴파니, 리미티드 환식기로 치환된 아미노다이하이드로싸이아진 유도체
SI2233474T1 (sl) * 2008-01-18 2015-11-30 Eisai R&D Management Co., Ltd. Kondenziran derivat aminodihidrotiazina
EP2305672B1 (en) 2008-06-13 2019-03-27 Shionogi & Co., Ltd. SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY
WO2010013794A1 (en) * 2008-07-28 2010-02-04 Eisai R&D Management Co., Ltd. Spiroaminodihydrothiazine derivatives
ES2539859T3 (es) * 2008-09-30 2015-07-06 Eisai R&D Management Co., Ltd. Nuevo derivado de aminodihidrotiazina condensado
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
GB0912777D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydropyrimidone derivatives
GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
WO2011044184A1 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2485920B1 (en) 2009-10-08 2016-04-27 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
RU2012129168A (ru) 2009-12-11 2014-01-20 Сионоги Энд Ко. Лтд. Производные оксазина
WO2011071109A1 (ja) * 2009-12-11 2011-06-16 塩野義製薬株式会社 アミノ基を有する縮合ヘテロ環化合物
CN102933564B (zh) 2010-06-09 2015-07-22 詹森药业有限公司 用作β-分泌酶(BACE)抑制剂的5,6-二氢-2H-[1,4]噁嗪-3-基-胺衍生物
CN103261199A (zh) 2010-10-29 2013-08-21 盐野义制药株式会社 萘啶衍生物
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
WO2012085038A1 (en) 2010-12-22 2012-06-28 Janssen Pharmaceutica Nv 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
GB201100181D0 (en) * 2011-01-06 2011-02-23 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101140D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
ES2624288T3 (es) * 2011-01-21 2017-07-13 Eisai R&D Management Co., Ltd. Métodos y compuestos útiles en la síntesis de derivados de aminodihidrotiazina condensados
JP5853035B2 (ja) 2011-03-09 2016-02-09 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap β−セクレターゼ(BACE)の阻害剤として有用な3,4−ジヒドロ−ピロロ[1,2−a]ピラジン−1−イルアミン誘導体
WO2012138590A1 (en) 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2012138734A1 (en) 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2012147763A1 (ja) 2011-04-26 2012-11-01 塩野義製薬株式会社 オキサジン誘導体およびそれを含有するbace1阻害剤
US8604024B2 (en) 2011-05-24 2013-12-10 Bristol-Myers Squibb Company Compounds for the reduction of beta-amyloid production
TW201302763A (zh) 2011-05-24 2013-01-16 必治妥美雅史谷比公司 用於減少β-類澱粉產生之化合物
US8927535B2 (en) * 2011-07-06 2015-01-06 Hoffman-La Roche Inc. Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors
EP2747769B1 (en) 2011-08-22 2017-08-02 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
EP2751116B1 (en) 2011-08-31 2016-10-12 Pfizer Inc Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds
JO3143B1 (ar) 2012-04-03 2017-09-20 Lilly Co Eli مركبات تتراهيدرو بيرولو ثيازين
US9227942B2 (en) 2012-04-27 2016-01-05 Eisai R&D Management Co., Ltd. Method for producing 5-(difluoromethyl)pyrazine-2-carboxylic acid and production intermediate thereof
CA2872154C (en) 2012-05-04 2016-08-23 Pfizer Inc. Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin-2-amine compounds as inhibitors of app, bace1 and bace2
GB201212871D0 (en) 2012-07-20 2012-09-05 Eisai Ltd Novel compounds
US9260455B2 (en) 2012-09-20 2016-02-16 Pfizer Inc. Alkyl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
PL2912041T3 (pl) 2012-10-26 2017-06-30 Eli Lilly And Company Pochodne tetrahydropirolotiazyny stanowiące inhibitory BACE
EP2931731A1 (en) 2012-12-11 2015-10-21 Pfizer Inc. Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds as inhibitors of bace1
WO2014098831A1 (en) 2012-12-19 2014-06-26 Bristol-Myers Squibb Company 4,6-diarylaminothiazines as bace1 inhibitors and their use for the reduction of beta-amyloid production
US9403846B2 (en) 2012-12-19 2016-08-02 Pfizer Inc. Carbocyclic- and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
WO2014120658A1 (en) 2013-01-29 2014-08-07 Amgen Inc. Fused multicyclic 3-amino-5,6-dihydro-2h-1,4-thiazine derivatives and their use as beta-secretase inhibitors
US10202355B2 (en) 2013-02-12 2019-02-12 Buck Institute For Research On Aging Hydantoins that modulate bace-mediated app processing
CA2897678A1 (en) 2013-02-13 2014-08-21 Pfizer Inc. Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
US9233981B1 (en) 2013-02-15 2016-01-12 Pfizer Inc. Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
AU2014223334C1 (en) * 2013-03-01 2018-10-18 Amgen Inc. Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
AP2015008716A0 (en) 2013-03-08 2015-09-30 Amgen Inc Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
TWI593692B (zh) 2013-03-12 2017-08-01 美國禮來大藥廠 四氫吡咯并噻嗪化合物
ES2627633T3 (es) 2013-06-12 2017-07-28 Janssen Pharmaceutica N.V. Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5-a]piracin-3(2H)-ona como inhibidores de beta-secretasa (BACE)
CN105324383B (zh) 2013-06-12 2017-10-31 詹森药业有限公司 作为β‑分泌酶(BACE)抑制剂的4‑氨基‑6‑苯基‑6,7‑二氢[1,2,3]三唑并[1,5‑A]吡嗪衍生物
JO3318B1 (ar) * 2013-06-18 2019-03-13 Lilly Co Eli مثبطات bace
US9096615B2 (en) 2013-07-30 2015-08-04 Amgen Inc. Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta-secretase and methods of use thereof
CN106459088A (zh) 2014-04-10 2017-02-22 辉瑞公司 2‑氨基‑6‑甲基‑4,4a,5,6‑四氢吡喃并[3,4‑d][1,3]噻嗪‑8a(8H)‑基‑1,3‑噻唑‑4‑基酰胺
US9550762B2 (en) 2014-08-08 2017-01-24 Amgen, Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
MA40941A (fr) 2014-11-10 2017-09-19 H Lundbeck As 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
CR20170187A (es) 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer
JO3458B1 (ar) 2014-11-10 2020-07-05 H Lundbeck As 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1
KR20170095881A (ko) 2014-12-18 2017-08-23 얀센 파마슈티카 엔.브이. 베타―세크레타제의 2,3,4,5―테트라히드로피리딘―6―아민 및 3,4―디히드로―2h―피롤―5―아민 화합물 억제제
AR103680A1 (es) 2015-02-23 2017-05-24 Lilly Co Eli Inhibidores selectivos de bace1
CN107257795A (zh) * 2015-03-19 2017-10-17 伊莱利利公司 选择性bace1抑制剂
AR104241A1 (es) 2015-04-29 2017-07-05 Lilly Co Eli Derivados de tetrahidrofuro tiazina como inhibidores de bace1 selectivos
WO2017024180A1 (en) 2015-08-06 2017-02-09 Amgen Inc. Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
TW201717948A (zh) 2015-08-10 2017-06-01 H 朗德貝克公司 包括給予2-胺基-3,5,5-三氟-3,4,5,6-四氫吡啶的聯合治療
HK1253372A1 (zh) 2015-08-12 2019-06-14 H‧隆德贝克有限公司 作为bace1抑制剂的2-氨基-3-氟-3-(氟甲基)-6-甲基-6-苯基-3,4,5,6-四氢吡啶
CN107849056A (zh) * 2015-08-12 2018-03-27 H.隆德贝克有限公司 Bace1抑制剂2‑氨基‑7a‑苯基‑3,4,4a,5,7,7a‑六氢呋喃并[3,4‑b]吡啶
WO2017051303A1 (en) 2015-09-24 2017-03-30 Pfizer Inc. Tetrahydropyrano[3,4-d][1,3]oxazin derivatives and their use as bace inhibitors
WO2017051294A1 (en) 2015-09-24 2017-03-30 Pfizer Inc. N-[2-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2h-1,2,4-thiadiazin-5-yl)-1,3-thiazol-4-yl] amides useful as bace inhibitors
EP3353183A1 (en) * 2015-09-24 2018-08-01 Pfizer Inc N-[2-(2-amino-6,6-disubstituted-4, 4a, 5, 6-tetrahydropyrano [3,4-d][1,3]thiazin-8a (8h)-yl) -1, 3-thiazol-4-yl]amides
TWI675034B (zh) * 2016-05-20 2019-10-21 美商美國禮來大藥廠 四氫呋喃并<img align="absmiddle" height="18px" width="27px" file="d10999.TIF" alt="其他非圖式 ed10999.png" img-content="tif" orientation="portrait" inline="yes" giffile="ed10999.png"></img>化合物及其作為選擇性BACE1抑制劑之用途
MX2019005247A (es) * 2016-11-04 2019-06-24 Janssen Pharmaceutica Nv Compuestos 4,4a,5,7-tetrahidro-3h-furo[3,4-b]piridinilicos.
WO2018112086A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
WO2018112084A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
CA3047290A1 (en) 2016-12-15 2018-06-21 Amgen Inc. 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
MX388697B (es) 2016-12-15 2025-03-20 Amgen Inc Derivados de tiazina como inhibidores de beta-secretasa y metodos de uso.
WO2018112081A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Oxazine derivatives as beta-secretase inhibitors and methods of use
MX2019010649A (es) * 2017-03-07 2019-10-21 Janssen Pharmaceutica Nv Inhibidores de beta secretasa.
CA3051779A1 (en) * 2017-03-07 2018-09-13 Janssen Pharmaceutica Nv Inhibitors of beta secretase
EP3592751A1 (en) * 2017-03-07 2020-01-15 Janssen Pharmaceutica NV Inhibitors of beta secretase
EA201992055A1 (ru) * 2017-09-07 2020-01-30 Янссен Фармацевтика Нв Ингибиторы бета-секретазы
EA201992076A1 (ru) * 2017-09-07 2020-03-19 Янссен Фармацевтика Нв Ингибиторы бета-секретазы
EA201992108A1 (ru) * 2017-09-07 2020-01-27 Янссен Фармацевтика Нв Ингибиторы бета-секретазы
CN110590517A (zh) * 2019-09-24 2019-12-20 武汉嘉诺康医药技术有限公司 一种3,4-二羟基-2′-氯苯乙酮的制备方法

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101061113A (zh) * 2004-11-23 2007-10-24 默克公司 作为β-内分泌抑制剂用于治疗阿耳茨海默氏病的2,3,4,6-四取代吡啶衍生物
ES2537898T3 (es) * 2005-10-25 2015-06-15 Shionogi & Co., Ltd. Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1
CN101360722A (zh) * 2005-11-15 2009-02-04 阿斯利康(瑞典)有限公司 新颖的2-氨基嘧啶衍生物及其用途
EP2151435A4 (en) * 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
KR20100017255A (ko) 2007-04-24 2010-02-16 시오노기 앤드 컴파니, 리미티드 환식기로 치환된 아미노다이하이드로싸이아진 유도체
ITTO20070665A1 (it) * 2007-09-24 2009-03-25 Rottapharm Spa Derivati amidinici, tioureici e guanidinici di 2-amminobenzotiazoli e amminobenzotiazine, nuovi agenti farmacologici per il trattamento delle patologie neurodegenerative.
SI2233474T1 (sl) 2008-01-18 2015-11-30 Eisai R&D Management Co., Ltd. Kondenziran derivat aminodihidrotiazina
EP2305672B1 (en) 2008-06-13 2019-03-27 Shionogi & Co., Ltd. SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY
ES2539859T3 (es) * 2008-09-30 2015-07-06 Eisai R&D Management Co., Ltd. Nuevo derivado de aminodihidrotiazina condensado

Similar Documents

Publication Publication Date Title
JP2012532874A5 (cg-RX-API-DMAC10.html)
JP2009502743A5 (cg-RX-API-DMAC10.html)
JP2012255026A5 (cg-RX-API-DMAC10.html)
JP2010529118A5 (cg-RX-API-DMAC10.html)
JP2013543896A5 (cg-RX-API-DMAC10.html)
JP2014521735A5 (cg-RX-API-DMAC10.html)
JP2013518107A5 (cg-RX-API-DMAC10.html)
JP2013534248A5 (cg-RX-API-DMAC10.html)
JP2014530220A5 (cg-RX-API-DMAC10.html)
JP2013509429A5 (cg-RX-API-DMAC10.html)
JP2017520613A5 (cg-RX-API-DMAC10.html)
JP2009535352A5 (cg-RX-API-DMAC10.html)
JP2013519645A5 (cg-RX-API-DMAC10.html)
JP2013520405A5 (cg-RX-API-DMAC10.html)
JP2010536849A5 (cg-RX-API-DMAC10.html)
RU2009133262A (ru) Нападизилатная соль антагониста мускаринового мз-рецептора
JP2015516419A5 (cg-RX-API-DMAC10.html)
JP2016539156A5 (cg-RX-API-DMAC10.html)
JP2017501140A5 (cg-RX-API-DMAC10.html)
JP2012519182A5 (cg-RX-API-DMAC10.html)
JP2008513510A5 (cg-RX-API-DMAC10.html)
JP2010500284A5 (cg-RX-API-DMAC10.html)
JP2012508256A5 (cg-RX-API-DMAC10.html)
WO2017182873A3 (en) Peptide-oligourea foldamer compounds and methods of their use
JP2009539874A5 (cg-RX-API-DMAC10.html)