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    INHIBITORS OF BRUTON'S TYROSINE KINASE
    41.
    发明专利
    INHIBITORS OF BRUTON'S TYROSINE KINASE 未知

    公开(公告)号：ZA201007561B

    公开(公告)日：2012-09-26

    申请号：ZA201007561

    申请日：2010-10-22

    Applicant: PHARMACYCLICS INC

    Inventor： HONIGBERG LEE ,  PAN ZHENGYING ,  VERNER ERIK

    IPC: A61K20060101 ,  A01N20060101 ,  A61P20060101

    Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. 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.

    INHIBITORS OF BRUTONÆS TYROSINE KINASE
    43.
    发明专利
    INHIBITORS OF BRUTONÆS TYROSINE KINASE 未知

    公开(公告)号：SG166093A1

    公开(公告)日：2010-11-29

    申请号：SG2010066017

    申请日：2006-12-28

    Applicant: PHARMACYCLICS INC

    Inventor： HONIGBERG LEE ,  VERNER ERIK ,  PAN ZHENGYING

    Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. 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. (no suitable figure)

    INHIBIDORES DE TIROSINA CINASA DE BRUTON.
    44.
    发明专利
    INHIBIDORES DE TIROSINA CINASA DE BRUTON. 未知

    公开(公告)号：MX2009003122A

    公开(公告)日：2009-08-07

    申请号：MX2009003122

    申请日：2006-12-28

    Applicant: PHARMACYCLICS INC

    Inventor： HONIGBERG LEE ,  VERNER ERIK ,  PAN ZHENGYING

    IPC: A61K31/519 ,  A01N43/90

    Abstract: En la presente invención de describen compuestos que forman enlaces covalentes con tirosina cinasa de Bruton (Btk); también se describen inhibidores irreversibles de Btk; se describen métodos para la preparación de los compuestos; también de escriben composiciones farmacéuticas que incluyen los compuestos; se describen métodos de uso de los inhibidores de Brk, solos o en combinación con otros agentes terapéuticos, para el tratamiento de enfermedades o condiciones autoinmunes, enfermedades o condiciones heteroinmunes, cáncer, incluyendo linfoma, y enfermedades o condiciones inflamatorias.

    BRUTON'S TYROSINE KINASE ACTIVITY PROBE AND METHOD OF USING
    46.
    发明专利
    BRUTON'S TYROSINE KINASE ACTIVITY PROBE AND METHOD OF USING 未知

    公开(公告)号：CA2668286C

    公开(公告)日：2014-09-16

    申请号：CA2668286

    申请日：2007-11-05

    Applicant: PHARMACYCLICS INC

    Inventor： PAN ZHENGYING ,  LI SHYR JIANN ,  SCHEREENS HELEEN ,  HONIGBERG LEE ,  VERNER ERIK

    IPC: C07F5/02 ,  C12N9/12 ,  C12Q1/48 ,  G01N33/52

    Abstract: Described herein are probes for Bruton's tyrosine kinase (Btk). Such probes are used to characterize and develop Btk-selective inhibitors intended for therapeutic use. The invention relates to a Btk activity probe comprising a Btk inhibitor moiety, a reporter moiety, and a linker moiety that links the inhibitor moiety to the reporter moiety. Specifically described are a Btk inhibitor moiety which covalently bonds to a cysteine residue of a Btk enzyme, a fluorophore and a linker moiety that links the inhibitor moiety to the fluorophore. In an embodiment, the Btk activity probe is: (see compound 3)

    Inhibitors of Bruton's tyrosine kinase
    47.
    发明专利
    Inhibitors of Bruton's tyrosine kinase 未知

    公开(公告)号：NZ601278A

    公开(公告)日：2013-09-27

    申请号：NZ60127806

    申请日：2006-12-28

    Applicant: PHARMACYCLICS INC

    Inventor： HONIGBERG LEE ,  VERNER ERIK ,  PAN ZHENGYING

    IPC: A01N43/90 ,  A61K31/4162 ,  A61K31/4985 ,  A61K31/519 ,  C07D487/04

    Abstract: 601278 Disclosed are pyrazolo-pyrimidin derivatives of formula (D) that form covalent bonds with Bruton's tyrosine kinase (Btk), wherein the variables shown in the structure of formula (D) are as defined in the specification. Also described are irreversible inhibitors of Btk; methods for the preparation of these compounds; and pharmaceutical compositions that include the compounds. These Btk inhibitors are suitable for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. Examples of compounds of formula (D) are: 1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-yn-1-one; N-((1s,4s)-4-(4-amino-3-(4-phenoxyphenyl)-1Hpyrazolo[3,4-d]pyrimidin-1-yl)cyclohexyl)propiolamide; 1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-yn-1-one;

    INHIBITORS OF BRUTON'S TYROSINE KINASE
    49.
    发明专利
    INHIBITORS OF BRUTON'S TYROSINE KINASE 未知

    公开(公告)号：NZ579911A

    公开(公告)日：2012-05-25

    申请号：NZ57991108

    申请日：2008-03-27

    Applicant: PHARMACYCLICS INC

    Inventor： HONIGBERG LEE ,  VERNER ERIK ,  BUGGY JOSEPH J ,  LOURY DAVID ,  CHEN WEI

    IPC: C07D473/34 ,  A61K31/519 ,  A61K31/52 ,  A61P29/00 ,  A61P35/00 ,  C07D253/06 ,  C07D487/04

    Abstract: Disclosed are irreversible tyrosine kinase inhibitor compounds of Formula (I) (1H-pyrazolo[3,4-d] pyrimidine), wherein the substituents are as described within the specification. Further disclosed is a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula (I), and the use of a compound of Formula (I) for the manufacture of a medicament for the treatment of an autoimmune disorder, a heteroimmune disorder, inflammation, rheumatoid arthritis, lupus, allergies, type I hypersensitivity, allergic conjunctivitis, allergic rhinitis, atopic dermatitis, B-cell lymphoma, diffuse large B cell lymphoma, follicular lymphoma, chronic lymphocytic leukemia, or a combination thereof.

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