CU20150149A7 - Un modulador de la gmp-amp cíclico sintasa (cgas), composiciones farmacéuticas del mismo, y métodos para diseñar o caracterizar un modulador de cgas - Google Patents

Un modulador de la gmp-amp cíclico sintasa (cgas), composiciones farmacéuticas del mismo, y métodos para diseñar o caracterizar un modulador de cgas

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Publication number
CU20150149A7
CU20150149A7 CUP2015000149A CU20150149A CU20150149A7 CU 20150149 A7 CU20150149 A7 CU 20150149A7 CU P2015000149 A CUP2015000149 A CU P2015000149A CU 20150149 A CU20150149 A CU 20150149A CU 20150149 A7 CU20150149 A7 CU 20150149A7
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CU
Cuba
Prior art keywords
cgas
modulator
characterizing
designing
pharmaceutical compositions
Prior art date
Application number
CUP2015000149A
Other languages
English (en)
Other versions
CU24376B1 (es
Inventor
Dinshaw J Patel
Thomas Tuschl
Manuel Ascano
Yang Wu
Yizhou Liu
Winfried Barchet
Gunther Hartmann
Thomas Zillinger
Roger Jones
Barbara L Gaffney
Pu Gao
Original Assignee
Sloan Kettering Inst Cancer
Univ Rockefeller
Rutgers
Univ Bonn
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Publication date
Application filed by Sloan Kettering Inst Cancer, Univ Rockefeller, Rutgers, Univ Bonn filed Critical Sloan Kettering Inst Cancer
Publication of CU20150149A7 publication Critical patent/CU20150149A7/es
Publication of CU24376B1 publication Critical patent/CU24376B1/es

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
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    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
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Abstract

La invención se refiere a nuevos análogos de GMP-AMP cíclico (cGAMP), moduladores de cGAS, y composiciones farmacéuticas de los mismos. Adicionalmente, la invención se refiere a un método para diseñar o caracterizar un modulador de cGAS; un método para diseñar y/o caracterizar un modulador de cGAS usando un sistema que comprende un computador o un medio legible en computador en el que una estructura cristalina de cGAS, o las coordinadas de la misma, está(n) incluida(s) y/o presentadas; un inhibidor de cGAS; y un inhibidor de cGAS diseñado. La invención también se refiere a una composición cristalina o cristalizable que comprende o contiene un polipéptido cGAS y un kit que comprende uno o más compuestos cGMPA y opcionalmente uno o más moléculas de cGAS.
CU2015000149A 2013-04-29 2014-04-29 ANÁLOGOS DE LA GMP-AMP CÍCLICO (cGAMP) ACTIVOS COMO MODULADORES DE LA GMP-AMP CÍCLICO SINTASA (cGAS) Y COMPOSICIONES FARMACÉUTICAS DEL MISMO CU24376B1 (es)

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