公开(公告)号：LT3057953T

公开(公告)日：2018-11-26

申请号：LT14799578

申请日：2014-10-17

Applicant: VERTEX PHARMA

Inventor： NTI-ADDAE KWAME ,  O`NEIL SIMON ,  ZHANG YUEGANG ,  MUDUNURI PRAVEEN ,  VAN ALSTEN JOHN GREGG ,  SONG BIN ,  STAVROPOULOS KATHY ,  STROHMEIER MARK ,  WALDO MICHAEL ,  NAVAMAL METTACHIT ,  KADIYALA IRINA NIKOLAEVNA

IPC: C07D401/14 ,  A61K31/506 ,  A61P35/00

公开(公告)号：UY37513A

公开(公告)日：2018-07-31

申请号：UY37513

申请日：2017-12-08

Applicant: VERTEX PHARMA

Inventor： ALCACIO TIMOTHY ,  BAEK MINSON ,  SARA SABINA HADIDA RUAH ,  ALI KESHAVARZ-SHOKRI ,  MCCARTNEY JASON ,  ANDERSON COREY ,  CLEVELAND THOMAS ,  KHATUYA HARIPADA ,  PRAMOD VIRUPAX JOSHI ,  PAUL JOHN KRENITSKY ,  FABRICE JEAN DENIS PIERRE ,  ANDREAS P TERMIN ,  ZHOU JINGLAN ,  ALEXANDER RUSSELL ABELA ,  PAUL TIMOTHY ANGELL ,  JEREMY J CLEMENS ,  LORI ANN FERRIS ,  PETER DIEDERIK JAN GROOTENHUIS ,  RAYMOND STANLEY GROSS ,  GULEVICH ANTON ,  CLARA KUANG-JU HSIA ,  ROBERT M HUGHES ,  KANG PING ,  MARK THOMAS MILLER ,  SHI YI ,  SHRESTHA MUNA ,  DAVID ANDREW SIESEL ,  STAVROPOULOS KATHY ,  UY JOHNNY ,  FREDRICK F VAN GOOR ,  TIMOTHY JOHN YOUNG ,  PARASELLI PRASUNA

IPC: A61K31/44

Abstract: Se describen compuestos de Fórmula (I): sales farmacéuticamente aceptables de este, derivados deuterados de cualquiera de los que anteceden y metabolitos de cualquiera de los anteceden. También se describen composiciones farmacéuticas que los comprenden, métodos para el tratamiento de la fibrosis quística mediante el uso de estos y métodos para confeccionarlos. Se describen además las formas en estado sólido del Compuesto 1 y sales y solvatos de este.

公开(公告)号：CA3046086A1

公开(公告)日：2018-06-14

申请号：CA3046086

申请日：2017-12-08

Applicant: VERTEX PHARMA

Inventor： ABELA ALEXANDER RUSSELL ,  ALCACIO TIMOTHY ,  ANDERSON COREY ,  ANGELL PAUL TIMOTHY ,  BAEK MINSON ,  CLEMENS JEREMY J ,  CLEVELAND THOMAS ,  FERRIS LORI ANN ,  GROOTENHUIS PETER DIEDERIK JAN ,  GROSS RAYMOND STANLEY ,  GULEVICH ANTON ,  HADIDA RUAH SARA SABINA ,  HSIA CLARA KUANG-JU ,  HUGHES ROBERT M ,  JOSHI PRAMOD VIRUPAX ,  KANG PING ,  KESHAVARZ-SHOKRI ALI ,  KHATUYA HARIPADA ,  KRENITSKY PAUL JOHN ,  MCCARTNEY JASON ,  MILLER MARK THOMAS ,  PARASELLI PRASUNA ,  PIERRE FABRICE JEAN DENIS ,  SHI YI ,  SHRESTHA MUNA ,  SIESEL DAVID ANDREW ,  STAVROPOULOS KATHY ,  TERMIN ANDREAS P ,  UY JOHNNY ,  VAN GOOR FREDRICK F ,  YOUNG TOMOTHY JOHN ,  ZHOU JINGLAN

IPC: C07D401/14 ,  A61K31/455 ,  A61P11/00 ,  C07D231/20 ,  C07D401/04

Abstract: Compounds of Formula (I) pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed. Also disclosed are solid state forms of Compound 1 and salts and solvates thereof.

公开(公告)号：SG11201705924RA

公开(公告)日：2017-08-30

申请号：SG11201705924R

申请日：2016-01-29

Applicant: BIOMED VALLEY DISCOVERIES INC ,  VERTEX PHARMA

Inventor： DECRESCENZO GARY ,  WELSCH DEAN ,  VLAHOVA PETINKA I ,  BOERRIGTER STEPHAN X M ,  ARONOV ALEXANDER ,  KESHAVARZ-SHOKRI ALI ,  SCANGAS ALEXANDER N ,  STAVROPOULOS KATHY ,  LITTLER BENJAMIN ,  KADIYALA IRINA NIKOLAEVNA ,  ALARGOVA ROSSITZA GUEORGUIEVA

IPC: C07D401/04

Abstract: The present invention provides crystalline forms of a compound of formula (I):Also provided are pharmaceutical compositions that include the provided crystalline forms and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.

公开(公告)号：PE20161022A1

公开(公告)日：2016-11-12

申请号：PE2016000512

申请日：2014-10-17

Applicant: VERTEX PHARMA

Inventor： KADIYALA IRINA NIKOLAEVNA ,  MUDUNURI PRAVEEN ,  NAVAMAL METTACHIT ,  NTI-ADDAE KWAME WIREDU ,  O'NEIL SIMON ADAM ,  ZHANG YUEGANG ,  STAVROPOULOS KATHY ,  STROHMEIER MARK ,  VAN ALSTEN JOHN GREGG ,  WALDO MICHAEL ,  SONG BIN

IPC: A61K31/506 ,  A61P35/00 ,  C07D401/14

Abstract: Se refiere a un cocristal que comprende un compuesto de formula I, donde R1 y R2 son hidrogeno o deuterio; y un formador de cocristales tales como acido adipico, acido citrico, acido fumarico, acido maleico, acido succinico o acido benzoico. Son compuestos preferidos: (S)-N-4-metil-2-(8-((1´-metil-[2’-bipirimidin]-4,5-il)amino)propan-6-il)quinolina-2-carboxamida y (S)-N-metil-8-(1-((2’-metil-4’,6’-dideuterio-[4,5’-bipirimidin]-4,5-il)amino)propan-6-il)quinolina-2-carboxamida. Dichos cocristales tienen picos de difraccion de rayos X aproximadamente a 6,46, 7,91, 11,92, 12,26, 12,99, 14,19, 18,68 y 19,07-Theta. Tambien se refiere a una composicion farmaceutica y a un metodo de preparacion. Dichos cocristales inhiben la proteina quinasa dependiente de ADN (DNA-PK) y son utiles en el tratamiento del cancer

公开(公告)号：CA2975048A1

公开(公告)日：2016-08-04

申请号：CA2975048

申请日：2016-01-29

Applicant: BIOMED VALLEY DISCOVERIES INC ,  VERTEX PHARMA

Inventor： DECRESCENZO GARY ,  WELSCH DEAN ,  VLAHOVA PETINKA I ,  BOERRIGTER STEPHAN X M ,  ARONOV ALEXANDER ,  KESHAVARZ-SHOKRI ALI ,  SCANGAS ALEXANDER N ,  STAVROPOULOS KATHY ,  LITTLER BENJAMIN ,  KADIYALA IRINA NIKOLAEVNA ,  ALARGOVA ROSSITZA GUEORGUIEVA

IPC: C07D401/04

Abstract: The present invention provides crystalline forms of a compound of formula (I). Also provided are pharmaceutical compositions that include the provided crystalline forms and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer. It has been discovered that crystalline forms of 4-(5-Chloro-2- isopropylaminopyridin-4-yl)-1 H-pyrrole-2-carboxylic acid [1 -(3-chlorophenyl)-2- hydroxyethyl]amide can be prepared which exhibit improved properties, e.g. surprisingly improved stability and improved solubility characteristics. Thus, the present invention provides crystalline 4-(5-Chloro-2- isopropylaminopyridin-4-yl)-1H-pyrrole-2-carboxylic acid [1 -(3-chlorophenyl)-2- hydroxyethyljamide.

公开(公告)号：SG11201602962PA

公开(公告)日：2016-05-30

申请号：SG11201602962P

申请日：2014-10-17

Applicant: VERTEX PHARMA

Inventor： NTI-ADDAE KWAME WIREDU ,  O'NEIL SIMON ADAM ,  ZHANG YUEGANG ,  WALDO MICHAEL ,  MUDUNURI PRAVEEN ,  SONG BIN ,  VAN ALSTEN JOHN GREGG ,  STROHMEIER MARK ,  STAVROPOULOS KATHY ,  KADIYALA IRINA NIKOLAEVNA ,  NAVAMAL METTACHIT

IPC: C07D401/14 ,  A61K31/506 ,  A61P35/00

Abstract: The present invention relates to compositions and co-crystals each comprising a compound of formula I having the structure: wherein each of R 1 and R 2 is H or 2 H and a co-crystal former selected from adipic acid, citric acid, fumaric acid, maleic acid, succinic acid, or benzoic acid. Also within the scope of this invention are methods of making and using the same.