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公开(公告)号:AU2016206309A1
公开(公告)日:2016-08-04
申请号:AU2016206309
申请日:2016-07-20
Applicant: PHARMACYCLICS LLC
Inventor: CHEN WEI , LOURY DAVID J , YAN SHUNQI , WANG LONGCHENG , FRYE LEAH LYNN
IPC: C07D473/32 , A61K31/52 , A61P35/00 , A61P37/00
Abstract: Abstract Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
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22.
公开(公告)号:PE20160560A1
公开(公告)日:2016-06-09
申请号:PE2016000427
申请日:2014-09-29
Applicant: PHARMACYCLICS LLC
Inventor: CHEN WEI , WANG LONGCHENG , LOURY DAVID J , JIA ZHAOZHONG J
IPC: A61K31/519 , A61P19/00 , A61P19/02 , C07D401/14 , C07D403/14
Abstract: La presente invencion se refiere a derivados de pirazolo[3,4-d]pirimidin de formula (I), en donde: L1 es –N(R2)C(O)- o –C(O)N(R2)-; R1 es arilo C6-C12, entre otros; R2 es H o alquilo C1-C4; R4 es H, alquilo C1-C6, entre otros; R5 es cicloalquilo C3-C8, entre otros; R10 es halogeno, entre otros; m es 1 o 2; n es 0 o 1 y p es 0, 1 o 2. Son compuestos preferidos: (R,E)-4-(4-amino-1-(1-(4-(ciclopropil(metil)amino)but-2-enoil)pirrolidin-3-il)- 1H-pirazolo[3,4-d]pirimidin-3-il)-N-(4-metilpiridin-2-il)benzamida; (R,E)-4-(4-amino-1-(1-(4-(ciclopropil(metil)amino)but-2-enoil)pirrolidin-3-il)- 1H-pirazolo[3,4-d]pirimidin-3-il)-N-(4-(trifluorometil)piridin-2-il)benzamida, entre otros. Estos derivados actuan como inhibidores irreversibles de la Tirosina Cinasa de Bruton (Btk) siendo utiles en el tratamiento de enfermedades autoinmunitarias, heteroinmunitarias, cancer, inclusive linfoma y enfermedades inflamatorias
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公开(公告)号:AU2014324532A1
公开(公告)日:2016-04-21
申请号:AU2014324532
申请日:2014-09-29
Applicant: PHARMACYCLICS LLC
Inventor: WANG LONGCHENG , CHEN WEI , JIA ZHAOZHONG J , LOURY DAVID J
IPC: C07D403/14 , A61K31/519 , A61P19/00 , A61P19/02 , C07D401/14
Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
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公开(公告)号:CA2917167A1
公开(公告)日:2015-01-08
申请号:CA2917167
申请日:2014-06-30
Applicant: PHARMACYCLICS LLC
Inventor: CHEN WEI , JIA ZHAOZHONG J , LOURY DAVID J
IPC: C07D473/34 , A61K31/52 , A61P19/02 , A61P37/00
Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
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公开(公告)号:CA3110966A1
公开(公告)日:2013-04-25
申请号:CA3110966
申请日:2012-10-19
Applicant: PHARMACYCLICS LLC
Inventor: BUGGY JOSEPH J , ELIAS LAURENCE , FYFE GWEN , HEDRICK ERIC , LOURY DAVID J , MODY TARAK D
IPC: G01N33/48 , A61K31/519 , A61P35/00
Abstract: Methods are provided for treating a hematologic cancer comprising administering an anticancer agent to a subject identified as having an increased mobilization of a subpopulation of lymphocytes from a malignancy following administration of an irreversible Btk inhibitor. Methods also are provided for identification of subjects for treatment and the analysis of cells mobilized from a hematologic malignancy following administration of an irreversible Btk inhibitor.
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公开(公告)号:CA3022256A1
公开(公告)日:2011-12-08
申请号:CA3022256
申请日:2011-06-03
Applicant: PHARMACYCLICS LLC
Inventor: BUGGY JOSEPH J , ELIAS LAURENCE , FYFE GWEN , HEDRICK ERIC , LOURY DAVID J , MODY TARAK D
IPC: A61K31/519 , A61K9/48 , A61K39/395 , A61P35/00
Abstract: Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.
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公开(公告)号:CA3007788A1
公开(公告)日:2011-12-08
申请号:CA3007788
申请日:2011-06-03
Applicant: PHARMACYCLICS LLC
Inventor: BUGGY JOSEPH J , ELIAS LAURENCE , FYFE GWEN , HEDRICK ERIC , LOURY DAVID J , MODY TARAK D
IPC: A61K39/395 , A61K31/519 , A61P35/00
Abstract: Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.
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公开(公告)号:CA3007787A1
公开(公告)日:2011-12-08
申请号:CA3007787
申请日:2011-06-03
Applicant: PHARMACYCLICS LLC
Inventor: BUGGY JOSEPH J , ELIAS LAURENCE , FYFE GWEN , HEDRICK ERIC , LOURY DAVID J , MODY TARAK D
IPC: A61K31/519 , A61P35/00
Abstract: Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.
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公开(公告)号:MX391121B
公开(公告)日:2025-03-19
申请号:MX2017014058
申请日:2014-04-16
Applicant: PHARMACYCLICS LLC
Inventor: LOURY DAVID J , HEDRICK ERIC , FYFE GWEN , BUGGY JOSEPH J , ELIAS LAURENCE , MODY TARAK D
IPC: A61P35/00 , A61K31/519 , A61K39/395
Abstract: La presente invención se refiere a procedimientos de tratamiento de un cáncer hematológico que comprenden administrar un agente antineoplásico a un sujeto identificado por tener una elevada movilización de una subpoblación de linfocitos de un tumor maligno tras la administración de un inhibidor de Btk irreversible. También se proporcionan procedimientos de identificación de sujetos para el tratamiento y el análisis de células movilizadas de un tumor maligno hematológico tras la administración de un inhibidor de Btk irreversible.
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公开(公告)号:MX380899B
公开(公告)日:2025-03-12
申请号:MX2020004438
申请日:2012-12-03
Applicant: PHARMACYCLICS LLC
Inventor: LOURY DAVID J , HEDRICK ERIC , FYFE GWEN , BUGGY JOSEPH J , ELIAS LAURENCE , MODY TARAK D
IPC: A61K31/519 , A61K31/496 , A61P35/00
Abstract: Se divulgan aquí métodos para tratar un cáncer que comprenden: a. administrar un inhibidor de Btk a un sujeto suficiente para dar como resultado un incremento o aparición en la sangre de una subpoblación de linfocitos definida por inmunofenotipificación; b. determinar el perfil de expresión de uno o más biomarcadores a partir de una o más subpoblaciones de linfocitos; y c. administrar un segundo agente con base en el perfil de expresión determinado.
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