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公开(公告)号：AU2011230508B2
公开(公告)日：2016-04-28
申请号：AU2011230508
申请日：2011-03-25
Applicant: VERTEX PHARMA
Inventor： KESHAVARZ-SHOKRI ALI , ZHANG BEILI , ALCACIO TIM EDWARD , LEE ELAINE CHUNGMIN , ZHANG YUEGANG , KRAWIEC MARIUSZ
IPC: C07D405/12 , A61K31/404 , A61P11/00
Abstract: The present invention relates to solid forms of (
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公开(公告)号：NZ603043A
公开(公告)日：2015-02-27
申请号：NZ60304311
申请日：2011-04-22
Applicant: VERTEX PHARMA
Inventor： SHETH URVI JAGDISHBHAI , BOTFIELD MARTYN CURTIS , ALCACIO TIM EDWARD , YANG XIAOQING , SULLIVAN MARK JEFFREY , HURLEY DENNIS JAMES , AREKAR SNEHA G , KESHAVARZ-SHOKRI ALI , ZHANG BEILI , ZLOKARNIK GREGOR , KRAWIEC MARIUSZ , ALARGOVA ROSSITZA GUEORGUIEVA , ZHANG YUEGANG , BINCH HAYLEY MARIE , FANNING LEV TYLER DEWEY , JOHNSTON STEVEN C , YOUNG CHRISTOPHER RYAN , NUMA MEHDI , SILINA ALINA , GROOTENHUIS PETER DIEDERIK JAN , VAN GOOR FREDRICK F , ZAMAN NOREEN TASNEEM , MUDUNURI PRAVEEN , KAUSHIK RITU ROHIT , MEDEK ALES , KADIYALA IRINA NIKOLAEVNA , LEE ELAINE CHUNGMIN , LUISI BRIAN , VERWIJS MARINUS JACOBUS
IPC: A61K31/443 , A61K31/36 , A61K31/47 , C07D213/75 , C07D215/233 , C07D215/56 , C07D317/46
Abstract: Disclosed is a pharmaceutical composition comprising: Compound 1 SDD Formulation and Compound 3 Form I Tablet Formulation wherein: Compound 1 SDD Formulation is a spray dried dispersion of ivacaftor (VX-770), which comprises from about 45 wt% to about 85 wt% of substantially amorphous ivacaftor by weight of the dispersion, from about 14.45 wt% to about 55.55 wt% of hydroxypropylmethylcellulose acetate succinate (HPMCAS) by weight of the dispersion, and from about 0.45 wt% to about 0.55 wt% sodium lauryl sulfate (SLS) by weight of the dispersion; Compound 3 Form I Tablet Formulation comprises: crystalline form I of lumacaftor (VX-809) (characterized by one or more peaks at 15.2 to 15.6 degrees, 16.1 to 16.5 degrees, and 14.3 to 14.7 degrees in an X-ray powder diffraction obtained using Cu K alpha radiation) in an amount ranging from about 20 wt% to about 80 wt% by weight of the composition; a filler comprising microcrystalline cellulose in an amount ranging from about 20 wt% to about 50 wt% by weight of the composition; a disintegrant comprising sodium croscarmellose sodium in an amount ranging from about 1 wt% to about 5 wt% by weight of the composition; a surfactant comprising sodium lauryl sulfate in an amount ranging from about 2 wt% to about 0.3 wt% by weight of the composition; a diluent comprising mannitol in an amount ranging from about 1 wt% to about 30 wt% by weight of the composition; a lubricant comprising magnesium stearate in an amount ranging from about 0.3 wt% to about 5 wt% by weight of the composition; and at least one of: a binder comprising polyvinylpyrrolidone in an amount ranging from about 0.1 wt% to about 5 wt% by weight of the composition and a glidant comprising colloidal silica in an amount ranging from about 0.05 wt% to about 2 wt% by weight of the composition. Also disclosed is the use of the pharmaceutical composition as defined above in the manufacture of a medicament for treating a CFTR mediated disease in a human, wherein the CFTR mediated disease is selected from cystic fibrosis, COPD, emphysema, dry-eye disease or osteoporosis.
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公开(公告)号：AU2011242452A1
公开(公告)日：2012-11-08
申请号：AU2011242452
申请日：2011-04-22
Applicant: VERTEX PHARMA
Inventor： VAN GOOR FREDRICK F , ALARGOVA ROSSITZA GUEORGUIEVA , ALCACIO TIM EDWARD , AREKAR SNEHA G , JOHNSTON STEVEN C , KADIYALA IRINA NIKOLAEVNA , KESHAVARZ-SHOKRI ALI , KRAWIEC MARIUSZ , LEE ELAINE CHUNGMIN , MEDEK ALES , MUDUNURI PRAVEEN , SULLIVAN MARK JEFFREY , ZAMAN NOREEN TASNEEM , ZHANG BEILI , ZHANG YUEGANG , ZLOKARNIK GREGOR
IPC: A61K31/4704 , A61K31/404 , A61K31/443
Abstract: The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis.
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公开(公告)号：HRP20210165T1
公开(公告)日：2021-03-19
申请号：HRP20210165
申请日：2021-02-01
Applicant: VERTEX PHARMA
Inventor： KESHAVARZ-SHOKRI ALI , ZHANG BEILI , ALCACIO TIM EDWARD , LEE ELAINE CHUNGMIN , ZHANG YUEGANG , KRAWIEC MARIUSZ
IPC: A61K9/10 , A61K31/404 , A61P11/00 , C07D405/12
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公开(公告)号：SI2826776T1
公开(公告)日：2021-02-26
申请号：SI201131935
申请日：2011-03-25
Applicant: VERTEX PHARMA
Inventor： KESHAVARZ-SHOKRI ALI , ZHANG BEILI , ALCACIO TIM EDWARD , LEE ELAINE CHUNGMIN , ZHANG YUEGANG , KRAWIEC MARIUSZ
IPC: A61K9/00 , A61K31/00 , A61P11/00 , C07D405/00
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Patent Agency Ranking
公开(公告)号：CA2794559C
公开(公告)日：2019-07-23
申请号：CA2794559
申请日：2011-03-25
Applicant: VERTEX PHARMA
Inventor： KESHAVARZ-SHOKRI ALI , ZHANG BEILI , ALCACIO TIM EDWARD , LEE ELAINE CHUNGMIN , ZHANG YUEGANG , KRAWIEC MARIUSZ
IPC: C07D405/12 , A61K31/404 , A61P11/00
Abstract: The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2- methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith.
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公开(公告)号：RS57700B1
公开(公告)日：2018-12-31
申请号：RSP20181154
申请日：2014-12-12
Applicant: VERTEX PHARMA
Inventor： ANDERSON COREY , HADIDA-RUAH SARA SABINA , GOLEC JULIAN MARIAN CHARLES , ZHANG BEILI , LITTLER BENJAMIN JOSEPH , KESHAVARZ-SHOKRI ALI , ALCACIO TIM EDWARD , BELMONT DANIEL T
IPC: C07F9/576 , A61K31/675 , A61P19/02
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公开(公告)号：SI3080134T1
公开(公告)日：2018-11-30
申请号：SI201430873
申请日：2014-12-12
Applicant: VERTEX PHARMA
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公开(公告)号：HRP20181563T1
公开(公告)日：2018-11-30
申请号：HRP20181563
申请日：2018-10-01
Applicant: VERTEX PHARMA
Inventor： ANDERSON COREY , HADIDA-RUAH SARA SABINA , GOLEC JULIAN MARIAN CHARLES , ZHANG BEILI , LITTLER BENJAMIN JOSEPH , KESHAVARZ-SHOKRI ALI , ALCACIO TIM EDWARD , BELMONT DANIEL T
IPC: C07F9/576 , A61K31/675 , A61P19/02
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公开(公告)号：AU2018203149A1
公开(公告)日：2018-05-24
申请号：AU2018203149
申请日：2018-05-07
Applicant: VERTEX PHARMA
Inventor： ZHANG BEILI , ALCACIO TIM EDWARD , LEE ELAINE CHUNGMIN , ZHANG YUEGANG , KRAWIEC MARIUSZ , KESHAVARZ-SHOKRI ALI
IPC: C07D405/12 , A61K31/404 , A61P11/00
Abstract: The present invention relates to solid forms of (R)-I-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5 yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith. -98-
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