公开(公告)号：ZA200901784B

公开(公告)日：2011-01-26

申请号：ZA200901784

申请日：2009-03-12

Applicant: PHARMACYCLICS INC

Inventor： PAN ZHENGYING ,  HONIGBERG LEE ,  VERNER ERIC J

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.

公开(公告)号：BRPI0622054A2

公开(公告)日：2010-11-09

申请号：BRPI0622054

申请日：2006-12-28

Applicant: PHARMACYCLICS INC

Inventor： HONIGBERG LEE ,  VERNER ERIK ,  PAN ZHENGYING

IPC: A01N43/90 ,  A61K31/519

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.

公开(公告)号：CA2874756A1

公开(公告)日：2008-10-09

申请号：CA2874756

申请日：2008-03-27

Applicant: PHARMACYCLICS INC

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

IPC: C07D487/04 ,  A61K31/519 ,  A61P19/02 ,  A61P29/00 ,  A61P37/06 ,  C12N9/12 ,  C12Q1/48 ,  G01N33/53

Abstract: Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.

公开(公告)号：CA2668286A1

公开(公告)日：2008-05-08

申请号：CA2668286

申请日：2007-11-05

Applicant: PHARMACYCLICS INC

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

IPC: C07D487/00

Abstract: Described herein are probes for Bruton's tyrosine kinase (Btk). Such prob es are used to characterize and develop Btk-selective inhibitors intended fo r therapeutic use.

公开(公告)号：AU2006348662A1

公开(公告)日：2008-04-03

申请号：AU2006348662

申请日：2006-12-28

Applicant: PHARMACYCLICS INC

Inventor： HONIGBERG LEE ,  PAN ZHENGYING ,  VERNER ERIK

IPC: A01N43/90 ,  A61K31/519 ,  A61K31/52 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02

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.

公开(公告)号：CA2636696A1

公开(公告)日：2007-08-02

申请号：CA2636696

申请日：2006-12-28

Applicant: PHARMACYCLICS INC

Inventor： JANKOWSKI ORION D ,  PALMER JAMES T ,  HONIGBERG LEE

IPC: C07D471/06 ,  A61K31/416 ,  A61K31/4375 ,  A61K31/675

Abstract: Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided.

公开(公告)号：CY1112513T1

公开(公告)日：2015-12-09

申请号：CY121100100

申请日：2012-01-27

Applicant: PHARMACYCLICS INC

Inventor： HONIGBERG LEE ,  VERNER ERIK ,  PAN ZHENGYING

IPC: A01N43/90 ,  A61K31/519 ,  A61P35/00 ,  C07D487/04

Abstract: Αποκαλύπτονταιεδώενώσεις, οιοποίεςσχηματίζουνομοιοπολικούςδεσμούςμεκινάσεςτυροσίνηςτουΒruton (Βtk). ΕπίσηςπεριγράφονταιμηαναστρέψιμοιαναστολείςτηςΒtk. Αποκαλύπτονταιμέθοδοιγιατηνπαρασκευήτωνενώσεων. Επίσηςαποκαλύπτονταιφαρμακευτικέςσυνθέσειςπουπεριλαμβάνουντιςενώσεις. ΑποκαλύπτονταιμέθοδοιχρήσηςτωναναστολέωντηςΒtk μόνωνή σεσυνδυασμόμεάλλουςθεραπευτικούςπαράγοντεςγιατηνθεραπευτικήαγωγήαυτοάνοσωνασθενειώνή καταστάσεων, ετεροάνοσωνασθενειώνή καταστάσεων, καρκίνου, συμπεριλαμβανομένουλεμφώματοςκαιφλεγμονωδώνασθενειώνή καταστάσεων.

公开(公告)号：SG10201503235VA

公开(公告)日：2015-06-29

申请号：SG10201503235V

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.

公开(公告)号：EA020001B1

公开(公告)日：2014-07-30

申请号：EA201000599

申请日：2006-12-28

Applicant: PHARMACYCLICS INC

Inventor： HONIGBERG LEE ,  VERNER ERIK ,  PAN ZHENGYING

IPC: C07D487/04 ,  A61K31/519 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  A61P37/08

Abstract: Визобретенииприведеноописаниесоединений, образующихковалентныесвязис тирозинкиназойБрутона (Btk), инеобратимыхингибиторов Btk. Описаныспособыполучениятакихсоединений, атакжефармацевтическиекомпозиции, содержащиетакиесоединения. Крометого, приведеноописаниеспособовпримененияингибиторов Btk отдельноилив комбинациис другимитерапевтическимиагентамидлялеченияаутоиммунныхзаболеванийилисостояний, гетероиммунныхзаболеванийилисостояний, рака, включаялимфому, ивоспалительныхзаболеванийилисостояний.

公开(公告)号：EA017865B1

公开(公告)日：2013-03-29

申请号：EA200901313

申请日：2008-03-27

Applicant: PHARMACYCLICS INC

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

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

Abstract: Впатентеописанынеобратимыеингибиторыкиназ, способысинтезатакихнеобратимыхингибиторови способыприменениятакихнеобратимыхингибиторовдлялеченияболезней. Описанытакжеметодыанализаи системыдляопределениясоответствующегонеобратимогоингибиторабелка, включаякиназу.