MX339584B - Inhibidores de pi3 cinasa y usos de los mismos. - Google Patents

Inhibidores de pi3 cinasa y usos de los mismos.

Info

Publication number
MX339584B
MX339584B MX2012002972A MX2012002972A MX339584B MX 339584 B MX339584 B MX 339584B MX 2012002972 A MX2012002972 A MX 2012002972A MX 2012002972 A MX2012002972 A MX 2012002972A MX 339584 B MX339584 B MX 339584B
Authority
MX
Mexico
Prior art keywords
kinase inhibitors
compositions
methods
same
present
Prior art date
Application number
MX2012002972A
Other languages
English (en)
Other versions
MX2012002972A (es
Inventor
F Kluge Arthur
Niu Deqiang
Singh Juswinder
Mazdiyasni Hormoz
Qiao Lixin
C Petter Russell
Zhu Zhendong
Kuntz Kevin
Original Assignee
Avila Therapeutics Inc
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 Avila Therapeutics Inc filed Critical Avila Therapeutics Inc
Publication of MX2012002972A publication Critical patent/MX2012002972A/es
Publication of MX339584B publication Critical patent/MX339584B/es

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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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • C12N9/1205—Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases
    • A—HUMAN NECESSITIES
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    • 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
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

La presente invención se refiere a un conjugado caracterizado porque comprende una o más PI3 cinasas que tienen un residuo de cisteína, CysX, en donde el CysX se une covalente e irreversiblemente a un inhibidor, de tal manera que la inhibición de la PI3 cinasa es mantenida, en donde el inhibidor comprende, antes de la unión, un grupo funcional den forma de ojiva -L-Y capaz de unir covalentemente a Cysx. El compuesto para usarse en un método para inhibir una o más PI3 cinasas, o un mutante de las mismas, actividad en una muestra biológica. El compuesto para usarse en un método in vitro para inhibir una o más PI3 cinasas, o un mutante de las mismas.
MX2012002972A 2009-09-09 2010-09-09 Inhibidores de pi3 cinasa y usos de los mismos. MX339584B (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US24094709P 2009-09-09 2009-09-09
US37139610P 2010-08-06 2010-08-06
PCT/US2010/048317 WO2011031896A2 (en) 2009-09-09 2010-09-09 Pi3 kinase inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
MX2012002972A MX2012002972A (es) 2012-06-25
MX339584B true MX339584B (es) 2016-06-01

Family

ID=43733099

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2012002972A MX339584B (es) 2009-09-09 2010-09-09 Inhibidores de pi3 cinasa y usos de los mismos.

Country Status (15)

Country Link
US (1) US20110230476A1 (es)
EP (1) EP2475375A4 (es)
JP (1) JP2013504325A (es)
KR (1) KR20120063515A (es)
CN (1) CN102625708A (es)
AU (1) AU2010292198A1 (es)
BR (1) BR112012008385A2 (es)
CA (1) CA2773848A1 (es)
IL (1) IL218555A0 (es)
MX (1) MX339584B (es)
NZ (2) NZ626650A (es)
RU (1) RU2595718C2 (es)
SG (2) SG179085A1 (es)
TW (2) TW201609747A (es)
WO (1) WO2011031896A2 (es)

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