ME02728B - Jedinjenja i njihova upotreba kao bace inhibitori - Google Patents

Jedinjenja i njihova upotreba kao bace inhibitori

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Publication number
ME02728B
ME02728B MEP-2017-115A MEP11517A ME02728B ME 02728 B ME02728 B ME 02728B ME P11517 A MEP11517 A ME P11517A ME 02728 B ME02728 B ME 02728B
Authority
ME
Montenegro
Prior art keywords
pharmaceutically acceptable
compound
disease
acceptable salt
alzheimer
Prior art date
Application number
MEP-2017-115A
Other languages
German (de)
English (en)
French (fr)
Inventor
Gabor Csjernyik
Sofia Karlström
Annika Kers
Karin Kolmodin
Martin Nylöf
Liselotte Öhberg
Laszlo Rakos
Lars Sandberg
Fernando Sehgelmeble
Peter Söderman
Britt-Marie Swahn
Berg Stefan Von
Original Assignee
Astrazeneca Ab
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46314249&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ME02728(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of ME02728B publication Critical patent/ME02728B/me

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    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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    • 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
    • C07D401/10—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 linked by a carbon chain containing aromatic rings
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • A—HUMAN NECESSITIES
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • 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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    • 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
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    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
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    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
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  • Engineering & Computer Science (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Furan Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Claims (6)

1.Jedinjenje koje je (1r,1'R,4R)-4-metoksi-5"-metil-6'-[5-(prop-1-in-1-il)piridin-3-il]-3'H-dispiro[cikloheksan-1,2'-inden-1',2"-imidazol]-4"-amin: ili njegova farmaceutski prihvatljiva so.
2.Farmaceutski sastav koji se sastoji od aktivnih sastojaka terapeutski efektivnih količina jedinjenja prema patentnom zahtevu 1, ili njegova farmaceutski prihvatljiva so, u vezi sa bar jednim farmaceutski prihvatljivim ekscipijentom, nosiocem ili razblaživačem.
3.Jedinjenje prema patentnom zahtevu 1, ili njegova farmaceutski prihvatljiva so za upotrebu kao lek.
4.Jedinjenje ili njegova farmaceutski prihvatljiva so prema patentnom zahtevu 1 za upotrebu kao metod lečenja ili sprečavanja Aβ-povezanih patologija, gde je navedena Aβ-povezana patologija Daunov sindrom, β-amiloidna angiopatija, cerebralna amiloidna angiopatija, nasledno cerebralno krvarenje, poremećaji povezani sa kognitivnim oštećenjem, MCI ("blago kognitivno oštećenje"), Alchajmerova bolest, gubitak pamćenja, simptomi nedostatka pažnje povezani sa Alchajmerovom bolešću, neurodegeneracija povezana sa Alchajmerovom bolešću, demencija mešovitog vaskularnog porekla, demencija degenerativnog porekla, presenilna demencija, senilna demencija, demencije povezane sa Parkinsonovom bolešću, progresivna supranuklearna paraliza ili kortikalna bazalna degeneracija.
5.Jedinjenje ili njegova farmaceutski prihvatljiva so za upotrebu prema patentnom zahtevu 4, gde je navedena β-povezana patologija Alchajmerova bolest.
6.Jedinjenje ili njegova farmaceutski prihvatljiva za upotrebu prema patentnim zahtevima 4 ili 5, gde je navedena upotreba u kombinaciji sa bar jednim kongitivnim poboljšavajućim agensom, agensom za poboljšavanje memorije ili inhibitorom holinesteraze.
MEP-2017-115A 2010-12-22 2011-12-21 Jedinjenja i njihova upotreba kao bace inhibitori ME02728B (me)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201061425852P 2010-12-22 2010-12-22
US201161529620P 2011-08-31 2011-08-31
PCT/SE2011/051555 WO2012087237A1 (en) 2010-12-22 2011-12-21 Compounds and their use as bace inhibitors
EP11850232.7A EP2655378B1 (en) 2010-12-22 2011-12-21 Compounds and their use as bace inhibitors

Publications (1)

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ME02728B true ME02728B (me) 2017-10-20

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EP (2) EP2655378B1 (me)
JP (3) JP6180325B2 (me)
KR (1) KR101916975B1 (me)
CN (2) CN103380133B (me)
AR (1) AR084553A1 (me)
AU (3) AU2011345389B2 (me)
BR (1) BR112013016030B1 (me)
CA (1) CA2822378C (me)
CL (1) CL2013001849A1 (me)
CO (1) CO6781485A2 (me)
CR (1) CR20130308A (me)
CY (1) CY1119211T1 (me)
DK (1) DK2655378T3 (me)
DO (3) DOP2013000147A (me)
EA (2) EA032687B1 (me)
EC (1) ECSP13012708A (me)
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GT (1) GT201300165A (me)
HR (1) HRP20170723T1 (me)
HU (1) HUE033274T2 (me)
LT (1) LT2655378T (me)
ME (1) ME02728B (me)
MX (1) MX342477B (me)
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NI (1) NI201300055A (me)
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PE (2) PE20141191A1 (me)
PH (2) PH12017500851A1 (me)
PL (1) PL2655378T3 (me)
PT (1) PT2655378T (me)
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SA (2) SA114360153B1 (me)
SG (2) SG10201602241SA (me)
SI (1) SI2655378T1 (me)
SM (1) SMT201700243T1 (me)
TW (2) TWI618700B (me)
UY (1) UY33829A (me)
WO (1) WO2012087237A1 (me)
ZA (1) ZA201305495B (me)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011106414A1 (en) 2010-02-24 2011-09-01 Dillard Lawrence W Inhibitors of beta-secretase
US8415483B2 (en) * 2010-12-22 2013-04-09 Astrazeneca Ab Compounds and their use as BACE inhibitors
WO2013054108A1 (en) 2011-10-10 2013-04-18 Astrazeneca Ab Mono-fluoro beta-secretase inhibitors
US8779355B2 (en) 2011-12-28 2014-07-15 Quest Diagnostics Investments, Inc. Methods for detecting lacosamide by mass spectrometry
JP5869151B2 (ja) 2012-01-26 2016-02-24 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ フルオロメチル−５，６−ジヒドロ−４ｈ−［１，３］オキサジン
TWI557112B (zh) * 2012-03-05 2016-11-11 百靈佳殷格翰國際股份有限公司 β－分泌酶抑制劑
EP2854797A4 (en) 2012-05-30 2016-01-13 Comentis Inc CHROMANE COMPOUNDS
US9000182B2 (en) * 2012-06-20 2015-04-07 Astrazeneca Ab 2H-imidazol-4-amine compounds and their use as BACE inhibitors
US9000185B2 (en) * 2012-06-20 2015-04-07 Astrazeneca Ab Cycloalkyl ether compounds and their use as BACE inhibitors
US9000183B2 (en) * 2012-06-20 2015-04-07 Astrazeneca Ab Cyclohexane-1,2′-indene-1′,2″-imidazol compounds and their use as BACE inhibitors
US9000184B2 (en) * 2012-06-20 2015-04-07 Astrazeneca Ab Cyclohexane-1,2′-naphthalene-1′,2″-imidazol compounds and their use as BACE inhibitors
US10548882B2 (en) * 2012-06-21 2020-02-04 Astrazeneca Ab Camsylate salt
TW201422592A (zh) 2012-08-27 2014-06-16 Boehringer Ingelheim Int β－分泌酶抑制劑
JP2015532282A (ja) * 2012-09-28 2015-11-09 ヴァイティー ファーマシューティカルズ，インコーポレイテッド β−セクレターゼの阻害剤
CA2899938C (en) 2013-02-12 2021-10-19 Buck Institute For Research On Aging Hydantoins that modulate bace-mediated app processing
US10053453B2 (en) 2014-10-07 2018-08-21 Astrazeneca Ab Compounds and their use as BACE inhibitors
TW201742625A (zh) 2016-03-15 2017-12-16 阿斯特捷利康公司 組合療法
TW201740944A (zh) 2016-03-15 2017-12-01 美國禮來大藥廠 組合療法
WO2017169503A1 (ja) * 2016-04-01 2017-10-05 国立大学法人 千葉大学 含窒素芳香族アミドの製造方法、ピロール・イミダゾールポリアミドの製造方法、及び化合物
CN107892697B (zh) 2016-12-26 2020-11-03 郑州泰基鸿诺医药股份有限公司 一种[1,3]噻嗪-2-胺类化合物及应用，药物组合物
CN107954927A (zh) * 2017-10-30 2018-04-24 广东莱佛士制药技术有限公司 一种3-溴-5-(丙炔-1-基)吡啶的制备方法
WO2019122268A1 (en) 2017-12-21 2019-06-27 Astrazeneca Ab Processes for the stereoselective preparation of bace inhibitors
WO2019122421A1 (en) 2017-12-22 2019-06-27 Astrazeneca Ab Stereoselective ketone reduction using a ketoreductase enzyme
WO2019129755A1 (en) 2017-12-29 2019-07-04 Astrazeneca Ab Ketal hydrogenation
WO2019129750A1 (en) 2017-12-29 2019-07-04 Astrazeneca Ab Processes for the racemization of dihydroimidazole ring systems
CN110615751B (zh) * 2018-06-19 2021-08-17 上海医药工业研究院 一种2-氧代硫代丙酰胺的制备方法
WO2020183021A1 (en) 2019-03-14 2020-09-17 Astrazeneca Ab Lanabecestat for weight loss
CN111253427A (zh) * 2020-03-13 2020-06-09 苏州大学 正丁基锂在催化醛和硅烷的氰硅化反应中的应用
CN114989103B (zh) * 2022-06-09 2024-07-09 杭州科巢生物科技有限公司 一种2-甲氧基-3-(1-甲基-1h-1,2,4-三唑-3-基)苯胺的制备方法

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100452491B1 (ko) 2001-03-29 2004-10-12 한미약품 주식회사 신규한 결정형 암로디핀 캠실레이트 염 및 그의 제조방법
JP4273406B2 (ja) * 2001-06-01 2009-06-03 小野薬品工業株式会社 アルドース還元酵素阻害剤を有効成分とする脱髄性疾患または脱髄を伴う疾患治療剤
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
ES2332184T3 (es) 2004-03-22 2010-01-28 ELI LILLY & COMPANY Derivados de piridilo y su uso como antagonistas del receptor mglu5.
PE20070135A1 (es) 2005-06-14 2007-03-09 Schering Corp Compuestos heterociclicos como inhibidores de aspartil proteasas
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
JP2009521488A (ja) 2005-12-21 2009-06-04 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｐｋｃ−シータのインヒビターとして有益なピリミジン誘導体
WO2007100536A1 (en) 2006-02-24 2007-09-07 Wyeth DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE
SA07280338B1 (ar) * 2006-06-22 2010-11-02 استكس ثيرابيوتكس ليمتد مشتقات أيزوإندول جديدة
WO2008076044A1 (en) * 2006-12-20 2008-06-26 Astrazeneca Ab Novel 2-amino-5, 5-diaryl-imidazol-4-ones
EP2108018A2 (en) * 2007-02-01 2009-10-14 Glaxo Group Limited 8-oxa-1,4-diazaspiro [4,5] dec-3-en-1-yl and 1,4,8-triazaspiro [4,5] dec-3-en-1-yl acetamides as glyti transporter inhibitors in treatment of neurological and neuropsychiatric disorders
MX2009012177A (es) * 2007-05-07 2009-11-23 Schering Corp Moduladores de gamma-secretasa.
WO2009100169A1 (en) 2008-02-06 2009-08-13 Glaxo Group Limited Dual pharmacophores - pde4-muscarinic antagonistics
FR2929943B1 (fr) 2008-04-15 2010-09-24 Inst Rech Developpement Ird Sels de quinoleines 2-substituees
AU2009277485B2 (en) 2008-07-28 2013-05-02 Eisai R&D Management Co., Ltd. Spiroaminodihydrothiazine derivatives
WO2010021680A2 (en) 2008-08-19 2010-02-25 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
CN102209721A (zh) 2008-09-11 2011-10-05 安姆根有限公司 作为β-分泌酶调节剂的螺四环化合物及其使用方法
MX2011009571A (es) 2009-03-13 2011-10-19 Boehringer Ingelheim Int Inhibidores de beta-secretasa.
TW201105650A (en) 2009-07-02 2011-02-16 Astrazeneca Ab New compounds
UY32750A (es) 2009-07-02 2011-01-31 Astrazeneca Ab Imidazoles sustituidos y uso de los mismos
WO2011106414A1 (en) 2010-02-24 2011-09-01 Dillard Lawrence W Inhibitors of beta-secretase
AR080865A1 (es) 2010-03-31 2012-05-16 Array Biopharma Inc Derivados de espirotetrahidronaftaleno, composiciones farmaceuticas que los contienen, proceso de preparacion y uso de los mismos para tratar enfermedades neurodegenerativas,tal como alzheimer.
WO2011130741A1 (en) 2010-04-16 2011-10-20 Array Biopharma Inc. Compounds for treating neurodegenerative diseases
US8921363B2 (en) 2010-08-05 2014-12-30 Amgen Inc. Derivatives of 1 H-isoindol-3-amine, 1 H-iso-aza-indol-3amine, 3,4-dihydroisoquinolin-1-amine, and 1,4-dihydroisoquinolin-3-amine as beta-secretase inhibitors
WO2012040641A2 (en) 2010-09-24 2012-03-29 Array Biopharma Inc. Compounds for treating neurodegenerative diseases
WO2012071458A1 (en) 2010-11-22 2012-05-31 Array Biopharma Inc. Heterocyclic inhibitors of beta - secretase for the treatment of neurodegenerative diseases
US8415483B2 (en) * 2010-12-22 2013-04-09 Astrazeneca Ab Compounds and their use as BACE inhibitors
WO2013054108A1 (en) 2011-10-10 2013-04-18 Astrazeneca Ab Mono-fluoro beta-secretase inhibitors
US9000184B2 (en) * 2012-06-20 2015-04-07 Astrazeneca Ab Cyclohexane-1,2′-naphthalene-1′,2″-imidazol compounds and their use as BACE inhibitors
US9000183B2 (en) * 2012-06-20 2015-04-07 Astrazeneca Ab Cyclohexane-1,2′-indene-1′,2″-imidazol compounds and their use as BACE inhibitors
US9000185B2 (en) 2012-06-20 2015-04-07 Astrazeneca Ab Cycloalkyl ether compounds and their use as BACE inhibitors
US9000182B2 (en) * 2012-06-20 2015-04-07 Astrazeneca Ab 2H-imidazol-4-amine compounds and their use as BACE inhibitors
US10548882B2 (en) 2012-06-21 2020-02-04 Astrazeneca Ab Camsylate salt

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