BR112015001801A2 - métodos e composições para determinar a resistência à terapia de receptor de androgênio - Google Patents

métodos e composições para determinar a resistência à terapia de receptor de androgênio

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Publication number
BR112015001801A2
BR112015001801A2 BR112015001801A BR112015001801A BR112015001801A2 BR 112015001801 A2 BR112015001801 A2 BR 112015001801A2 BR 112015001801 A BR112015001801 A BR 112015001801A BR 112015001801 A BR112015001801 A BR 112015001801A BR 112015001801 A2 BR112015001801 A2 BR 112015001801A2
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BR
Brazil
Prior art keywords
androgen receptor
methods
modified
compositions
polypeptides
Prior art date
Application number
BR112015001801A
Other languages
English (en)
Inventor
David Joseph James
H Hager Jeffrey
Qian Jing
Lee Sensintaffar John
Lu Nhin
D Smith Nicholas
Original Assignee
Aragon Pharmaceuticals 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 Aragon Pharmaceuticals Inc filed Critical Aragon Pharmaceuticals Inc
Priority to BR122017017921A priority Critical patent/BR122017017921A2/pt
Publication of BR112015001801A2 publication Critical patent/BR112015001801A2/pt

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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
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
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    • 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
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    • A—HUMAN NECESSITIES
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/72—Receptors; Cell surface antigens; Cell surface determinants for hormones
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Abstract

methods and compositions for determining resistance to androgen receptor therapy abstract described herein are modified androgen receptor polypeptides that are resistant to inhibition by an androgen receptor inhibitor. described herein are compositions, combinations, and kits containing the modified androgen receptor polypeptides and methods of using the modified androgen receptor polypeptides. also described herein are methods of using the modified androgen receptor polypeptides as screening agents for the identification and design of third-generation androgen receptor modulators. also described herein are third-generation androgen receptor modulators that inhibit the activity of the modified androgen receptor polypeptides. also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such androgen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions, including cancers, such as castration resistant prostate cancers, that are mediated or dependent upon androgen receptors. tradução do resumo resumo patente de invenção "métodos e composições para determinar a resistência à terapia de receptor de androgênio" são descritos no presente documento polipeptídeos de receptor de androgênio modificados que são resistentes à inibição por um inibidor de receptor de androgênio. são descritas no presente documento composições, combinações e kits que contêm os polipeptídeos de receptor de androgênio modificados e métodos do uso dos polipeptídeos de receptor de androgênio modificados. são também descritos no presente documento métodos de uso dos polipeptídeos de receptor de androgênio modificados como agentes de triagem para a identificação e o design de moduladores de receptor de androgênio de terceira geração. são também descritos no presente documento moduladores de receptor de androgênio de terceira geração que inibem a atividade dos polipeptídeos de receptor de androgênio modificados. são também descritas composições farmacêuticas e medicamentos que incluem os compostos descritos no presente documento, bem como métodos de uso desses moduladores de receptor de androgênio, sozinhos e em combinação com outros compostos, para tratar doenças ou condições, incluindo cânceres, como cânceres de próstata resistentes à castração, que são mediados ou dependentes de receptores de androgênio.
BR112015001801A 2012-07-27 2013-07-26 métodos e composições para determinar a resistência à terapia de receptor de androgênio BR112015001801A2 (pt)

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BR122017017921A BR122017017921A2 (pt) 2012-07-27 2013-07-26 métodos e sistema para determinar a resistência à terapia de receptor de androgênio

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US201261676842P 2012-07-27 2012-07-27
US201361783763P 2013-03-14 2013-03-14
US201361829123P 2013-05-30 2013-05-30
PCT/US2013/052395 WO2014018926A1 (en) 2012-07-27 2013-07-26 Methods and compositions for determining resistance to androgen receptor therapy

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