EA201791684A1 - Селективные ингибиторы bace1 - Google Patents

Селективные ингибиторы bace1

Info

Publication number
EA201791684A1
EA201791684A1 EA201791684A EA201791684A EA201791684A1 EA 201791684 A1 EA201791684 A1 EA 201791684A1 EA 201791684 A EA201791684 A EA 201791684A EA 201791684 A EA201791684 A EA 201791684A EA 201791684 A1 EA201791684 A1 EA 201791684A1
Authority
EA
Eurasian Patent Office
Prior art keywords
bace1 inhibitors
selective bace1
selective
inhibitors
compound
Prior art date
Application number
EA201791684A
Other languages
English (en)
Other versions
EA031546B1 (ru
Inventor
Эрик Джеймс Хембр
Хосе Эдуардо Лопез
Дженнифер Энн Макмахон
Саймон Джеймс Ричардс
Леонард Лэрри Дж. Виннероски
Тимоти Эндрю Вудс
Original Assignee
Эли Лилли Энд Компани
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
Application filed by Эли Лилли Энд Компани filed Critical Эли Лилли Энд Компани
Publication of EA201791684A1 publication Critical patent/EA201791684A1/ru
Publication of EA031546B1 publication Critical patent/EA031546B1/ru

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/28Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02Dicarboxylic acids
    • C07C55/08Malonic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/16Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D309/28Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D309/30Oxygen atoms, e.g. delta-lactones

Abstract

В настоящем изобретении представлено соединение формулы IIили его фармацевтически приемлемая соль.
EA201791684A 2015-02-23 2016-02-17 Селективные ингибиторы bace1 EA031546B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562119391P 2015-02-23 2015-02-23
PCT/US2016/018160 WO2016137788A1 (en) 2015-02-23 2016-02-17 Selective bace1 inhibitors

Publications (2)

Publication Number Publication Date
EA201791684A1 true EA201791684A1 (ru) 2017-12-29
EA031546B1 EA031546B1 (ru) 2019-01-31

Family

ID=55442893

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201791684A EA031546B1 (ru) 2015-02-23 2016-02-17 Селективные ингибиторы bace1

Country Status (27)

Country Link
US (1) US9522923B2 (ru)
EP (1) EP3262051B1 (ru)
JP (1) JP6111001B1 (ru)
KR (1) KR101945139B1 (ru)
CN (1) CN107257801B (ru)
AR (1) AR103680A1 (ru)
AU (1) AU2016223072B2 (ru)
BR (1) BR112017013936A2 (ru)
CA (1) CA2972098A1 (ru)
CL (1) CL2017002090A1 (ru)
CO (1) CO2017008382A2 (ru)
CR (1) CR20170315A (ru)
DO (1) DOP2017000178A (ru)
EA (1) EA031546B1 (ru)
EC (1) ECSP17054980A (ru)
GT (1) GT201700185A (ru)
IL (1) IL252969A0 (ru)
MX (1) MX367940B (ru)
NZ (1) NZ732940A (ru)
PE (1) PE20171337A1 (ru)
PH (1) PH12017501523A1 (ru)
SG (1) SG11201705764SA (ru)
SI (1) SI3262051T1 (ru)
TN (1) TN2017000355A1 (ru)
TW (1) TWI627177B (ru)
WO (1) WO2016137788A1 (ru)
ZA (1) ZA201704293B (ru)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201116559D0 (en) 2011-09-26 2011-11-09 Univ Leuven Kath Novel viral replication inhibitors
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
JOP20160086B1 (ar) 2015-05-08 2021-08-17 2 Katholieke Univ Leuven Ku Leuven Research And Development مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
JO3633B1 (ar) 2015-09-16 2020-08-27 Katholieke Univ Leuven Ku Leuven Research & Development مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
JOP20160198B1 (ar) 2015-09-16 2022-03-14 Janssen Pharmaceuticals Inc مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
HUE054936T2 (hu) 2016-03-31 2021-10-28 Janssen Pharmaceuticals Inc Helyettesített indol-származékok mint a dengue-vírus replikációjának inhibitorai
EA201892216A1 (ru) 2016-03-31 2019-03-29 Янссен Фармасьютикалз, Инк. Замещенные производные индолина в качестве ингибиторов репликации вирусов денге
JOP20170069B1 (ar) 2016-04-01 2021-08-17 1 Janssen Pharmaceuticals Inc مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
EA201892200A1 (ru) 2016-04-01 2019-03-29 Янссен Фармасьютикалз, Инк. Замещенные производные соединений индола в качестве ингибиторов репликации вирусов денге
WO2018034977A1 (en) * 2016-08-18 2018-02-22 Eli Lilly And Company Combination therapy of bace-1 inhibitor and anti-n3pglu abeta antibody
JOP20180025B1 (ar) 2017-03-31 2021-08-17 Janssen Pharmaceuticals Inc مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
JOP20180026A1 (ar) 2017-03-31 2019-01-30 Univ Leuven Kath مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
CN110691773B (zh) 2017-05-22 2023-06-23 杨森制药公司 作为登革热病毒复制抑制剂的经取代的吲哚啉衍生物
EA039702B1 (ru) 2017-05-22 2022-03-01 Янссен Фармасьютикалз, Инк. Замещенные производные индолина в качестве ингибиторов репликации вирусов денге

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MX2007016180A (es) 2005-06-14 2008-03-07 Schering Corp Inhibidores de aspartil proteasas.
CN101910143B (zh) 2008-01-18 2013-08-21 卫材R&D管理有限公司 稠合的氨基二氢噻嗪衍生物
BRPI0915500A2 (pt) 2008-06-13 2019-08-27 Shionogi & Co derivado heterocíclico contendo enxofre tendo atividade inibitória de beta secretase
AR073406A1 (es) 2008-09-30 2010-11-03 Eisai R&D Man Co Ltd Aminodihidrotiazinas fusionadas con tetrahidropiranos,inhibidoras de bace1 y de la produccion de abeta amiloide, composiciones farmaceuticas que las contienen y usos de las mismas para el tratamiento de enfermedades neurodegenerativas,tales como alzheimer.
AR077277A1 (es) 2009-07-09 2011-08-17 Lilly Co Eli Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer
WO2011071057A1 (ja) 2009-12-09 2011-06-16 塩野義製薬株式会社 含硫黄複素環誘導体を含有するアルツハイマー症の治療用または予防用医薬組成物
EP2511269A4 (en) 2009-12-11 2013-04-24 Shionogi & Co FUSED HETEROCYCLIC COMPOUND HAVING AN AMINO GROUP
GB201100181D0 (en) 2011-01-06 2011-02-23 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101139D0 (en) * 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101140D0 (en) * 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
AR086539A1 (es) 2011-05-24 2014-01-08 Bristol Myers Squibb Co COMPUESTOS PARA LA REDUCCION DE LA PRODUCCION DE b-AMILOIDE
GB201212816D0 (en) * 2012-07-19 2012-09-05 Eisai Ltd Novel compounds
WO2014015125A1 (en) 2012-07-19 2014-01-23 Eisai R&D Management Co., Ltd. Fused aminodihydrothiazine derivative salts and uses thereof
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
TWI639607B (zh) * 2013-06-18 2018-11-01 美國禮來大藥廠 Bace抑制劑
AR104241A1 (es) * 2015-04-29 2017-07-05 Lilly Co Eli Derivados de tetrahidrofuro tiazina como inhibidores de bace1 selectivos

Also Published As

Publication number Publication date
TW201643170A (zh) 2016-12-16
PH12017501523A1 (en) 2018-02-05
SG11201705764SA (en) 2017-08-30
EP3262051B1 (en) 2019-10-02
AR103680A1 (es) 2017-05-24
PE20171337A1 (es) 2017-09-13
GT201700185A (es) 2018-11-23
TWI627177B (zh) 2018-06-21
AU2016223072A1 (en) 2017-07-13
DOP2017000178A (es) 2017-09-15
JP2017511806A (ja) 2017-04-27
EA031546B1 (ru) 2019-01-31
JP6111001B1 (ja) 2017-04-05
CR20170315A (es) 2017-08-14
TN2017000355A1 (en) 2019-01-16
NZ732940A (en) 2019-06-28
BR112017013936A2 (pt) 2018-01-02
US20160244465A1 (en) 2016-08-25
SI3262051T1 (sl) 2019-11-29
EP3262051A1 (en) 2018-01-03
WO2016137788A1 (en) 2016-09-01
US9522923B2 (en) 2016-12-20
IL252969A0 (en) 2017-08-31
CO2017008382A2 (es) 2017-11-30
ZA201704293B (en) 2019-01-30
AU2016223072B2 (en) 2018-11-15
CN107257801A (zh) 2017-10-17
CA2972098A1 (en) 2016-09-01
KR20170103971A (ko) 2017-09-13
KR101945139B1 (ko) 2019-02-01
MX367940B (es) 2019-09-12
CL2017002090A1 (es) 2018-04-13
CN107257801B (zh) 2019-08-13
ECSP17054980A (es) 2017-11-30
MX2017010861A (es) 2017-12-11

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Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU