MX370017B - Compuestos de [1,2,4]triazolo[1,5-c]quinazolin-5-amina heterobiciclo-sustituidos con propiedades antagonistas para a2a. - Google Patents

Compuestos de [1,2,4]triazolo[1,5-c]quinazolin-5-amina heterobiciclo-sustituidos con propiedades antagonistas para a2a.

Info

Publication number
MX370017B
MX370017B MX2015008481A MX2015008481A MX370017B MX 370017 B MX370017 B MX 370017B MX 2015008481 A MX2015008481 A MX 2015008481A MX 2015008481 A MX2015008481 A MX 2015008481A MX 370017 B MX370017 B MX 370017B
Authority
MX
Mexico
Prior art keywords
compounds
heterobicyclo
quinazolin
triazolo
ami
Prior art date
Application number
MX2015008481A
Other languages
English (en)
Other versions
MX2015008481A (es
Inventor
Dong Xiao
Andrew Stamford
Paul Tempest
Xianhai Huang
Rongze Kuang
Jae-Hun Kim
Yeon-Hee Lim
Junying Zheng
Walter Won
Amjad Ali
Edward Metzger
Timothy J Henderson
Younong Yu
Heping Wu
Nicolas Zorn
Christopher Boyce
Michael Man-Chu Lo
Pauline Ting
Gioconda V Gallo
Qiaolin Deng
Original Assignee
Merck Sharp & Dohme
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 Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of MX2015008481A publication Critical patent/MX2015008481A/es
Publication of MX370017B publication Critical patent/MX370017B/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems

Abstract

Se describen compuestos de fórmula GI: (ver Fórmula) en donde "RG3" "Rd1", a "Rd4","n","m","p", "W","X", "Y" y "Z" son como se definen en la presente, cuyos compuestos son antagonistas del receptor A2A; también se describen en la presente usos de los compuestos descritos en la presente como antagonistas del receptor A2A en el tratamiento potencial o prevención de trastornos y enfermedades neurológicas en las cuales están involucrados los receptores A2A; en la presente también se describen composiciones farmacéuticas que comprenden estos compuestos y usos de estas composiciones farmacéuticas.
MX2015008481A 2012-12-28 2013-12-20 Compuestos de [1,2,4]triazolo[1,5-c]quinazolin-5-amina heterobiciclo-sustituidos con propiedades antagonistas para a2a. MX370017B (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/CN2012/087865 WO2014101120A1 (en) 2012-12-28 2012-12-28 Heterobicyclo-substituted-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties
PCT/CN2013/076853 WO2014101373A1 (en) 2012-12-28 2013-06-06 Heterobicyclo-substituted-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds for treatment of central nervous system disorder
PCT/US2013/076781 WO2014105666A1 (en) 2012-12-28 2013-12-20 Heterobicyclo-substituted-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties

Publications (2)

Publication Number Publication Date
MX2015008481A MX2015008481A (es) 2015-09-23
MX370017B true MX370017B (es) 2019-11-28

Family

ID=51019745

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2015008481A MX370017B (es) 2012-12-28 2013-12-20 Compuestos de [1,2,4]triazolo[1,5-c]quinazolin-5-amina heterobiciclo-sustituidos con propiedades antagonistas para a2a.

Country Status (22)

Country Link
US (2) US9708347B2 (es)
EP (1) EP2945632B1 (es)
JP (1) JP6306049B2 (es)
KR (1) KR102165113B1 (es)
AU (1) AU2013370977B2 (es)
BR (1) BR112015015468B8 (es)
CA (1) CA2896056C (es)
CY (1) CY1120258T1 (es)
DK (1) DK2945632T3 (es)
ES (1) ES2667477T3 (es)
HR (1) HRP20180678T1 (es)
HU (1) HUE037950T2 (es)
LT (1) LT2945632T (es)
ME (1) ME03034B (es)
MX (1) MX370017B (es)
NO (1) NO2945632T3 (es)
PL (1) PL2945632T3 (es)
PT (1) PT2945632T (es)
RS (1) RS57162B1 (es)
RU (2) RU2671628C2 (es)
SI (1) SI2945632T1 (es)
WO (3) WO2014101120A1 (es)

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WO2017008205A1 (en) 2015-07-10 2017-01-19 Merck Sharp & Dohme Corp. Substituted aminoquinazoline compounds as a2a antagonist
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US10821106B2 (en) 2015-08-21 2020-11-03 Srx Cardio, Llc Composition and methods of use of novel phenylalanine small organic compounds to directly modulate PCSK9 protein activity
US10865185B2 (en) 2015-08-21 2020-12-15 Srx Cardio, Llc Composition and methods of use of tetrahydroisoquinoline small molecules to bind and modulate PCSK9 protein activity
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ES2789756T3 (es) 2015-12-23 2020-10-26 Merck Sharp & Dohme Moduladores alostéricos de 6,7-dihidro-5H-pirrolo[3,4-b]piridin-5-ona del receptor de acetilcolina muscarínico M4
WO2017107089A1 (en) 2015-12-23 2017-06-29 Merck Sharp & Dohme Corp. 3- (1h-pyrazol-4-yl) pyridineallosteric modulators of the m4 muscarinic acetylcholine receptor
WO2017147328A1 (en) 2016-02-23 2017-08-31 Portola Pharmaceuticals, Inc. Compounds for binding proprotein convertase subtilisin/kexin type 9 (pcsk9)
WO2018112843A1 (en) 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor
WO2018112842A1 (en) 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. 6,6-fused heteroaryl piperidine ether allosteric modulators of m4 muscarinic acetylcholine receptor
WO2018130184A1 (zh) 2017-01-13 2018-07-19 江苏恒瑞医药股份有限公司 1,2,4-三嗪-3-胺类衍生物、其制备方法及其在医药上的应用
RU2745035C1 (ru) 2017-02-27 2021-03-18 Бетта Фармасьютикалз Ко., Лтд. Ингибитор fgfr и его применение
UA125592C2 (uk) 2017-03-16 2022-04-27 Джянгсу Хенгруй Медісін Ко., Лтд. ПОХІДНА ГЕТЕРОАРИЛ[4,3-c]ПІРИМІДИН-5-АМІНУ, СПОСІБ ЇЇ ОТРИМАННЯ ТА ЇЇ МЕДИЧНІ ЗАСТОСУВАННЯ
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US11498923B2 (en) 2017-12-13 2022-11-15 Merck Sharp & Dohme Llc Substituted imidazo[1,2-c]quinazolines as A2A antagonists
WO2019154294A1 (zh) 2018-02-06 2019-08-15 江苏恒瑞医药股份有限公司 吡唑并[1,5-a][1,3,5]三嗪-2-胺类衍生物、其制备方法及其在医药上的应用
MA54298A (fr) 2018-11-30 2022-03-09 Merck Sharp & Dohme Dérivés amino triazolo quinazoline 9-substitués utiles en tant qu'antagonistes du récepteur de l'adénosine, compositions pharmaceutiques et leur utilisation
CN115698003A (zh) 2020-02-07 2023-02-03 加舒布鲁姆生物公司 杂环glp-1激动剂
CN112159411A (zh) * 2020-10-15 2021-01-01 南京工业大学 一种三氟甲基取代嘧啶并[1,3]二氮杂*化合物及其制备方法
WO2023201267A1 (en) 2022-04-13 2023-10-19 Gilead Sciences, Inc. Combination therapy for treating trop-2 expressing cancers

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Also Published As

Publication number Publication date
AU2013370977B2 (en) 2017-12-14
BR112015015468B8 (pt) 2023-04-25
US20170197991A1 (en) 2017-07-13
JP6306049B2 (ja) 2018-04-04
KR102165113B1 (ko) 2020-10-13
NO2945632T3 (es) 2018-08-04
LT2945632T (lt) 2018-05-25
WO2014105666A1 (en) 2014-07-03
PT2945632T (pt) 2018-05-22
US9708347B2 (en) 2017-07-18
CA2896056C (en) 2020-11-10
RU2671628C2 (ru) 2018-11-06
AU2013370977A1 (en) 2015-07-09
EP2945632B1 (en) 2018-03-07
WO2014101373A1 (en) 2014-07-03
JP2016504363A (ja) 2016-02-12
ES2667477T3 (es) 2018-05-11
RU2018136104A (ru) 2018-11-21
RS57162B1 (sr) 2018-07-31
CA2896056A1 (en) 2014-07-03
HRP20180678T1 (hr) 2018-06-01
SI2945632T1 (en) 2018-05-31
US10011615B2 (en) 2018-07-03
ME03034B (me) 2018-10-20
MX2015008481A (es) 2015-09-23
RU2018136104A3 (es) 2022-04-05
PL2945632T3 (pl) 2018-07-31
DK2945632T3 (en) 2018-05-22
US20150361098A1 (en) 2015-12-17
EP2945632A4 (en) 2016-09-14
RU2015131148A (ru) 2017-02-03
KR20150100879A (ko) 2015-09-02
HUE037950T2 (hu) 2018-09-28
BR112015015468B1 (pt) 2021-10-26
BR112015015468A2 (pt) 2017-07-11
EP2945632A1 (en) 2015-11-25
CY1120258T1 (el) 2019-07-10
WO2014101120A1 (en) 2014-07-03

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