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51.
公开(公告)号:JOP20190042A1
公开(公告)日:2017-06-16
申请号:JOP20190042
申请日:2019-03-11
Applicant: VERTEX PHARMA
Inventor: ABELA ALEXANDER RUSSELL , BAEK MINSON , ZHANG BEILI , UY JOHNNY , ZHOU JINGLAN , JOSHI PRAMOD VIRUPAX , SIESEL DAVID ANDREW , BUSCH BRETT BRADLEY , GROOTENHUIS PETER , VAN GOOR FREDRICK , KESHAVARZ-SHOKRI ALI , MELILLO VITO , HUGHES ROBERT M , ANDERSON COREY , ALCACIO TIMOTHY , PARASELLI PRASUNA , KHATUYA HARIPADA , FRIEMAN BRYAN A , CLEVELAND THOMAS , PIERRE FABRICE JEAN DENIS , KRENITSKY PAUL JOHN , MCCARTNEY JASON , TERMIN ANDREAS P , MCAULEY-AOKI RACHEL , MILLER MARK THOMAS , HADIDA RUAH SARA SABINA
Abstract: ( I )، يتمالكشفعنمركباتلهاالصيغة ( I )،أملاحمقبولةصيدليًامنها،مشتقاتمعالجةبالديوتيريوممنأيٍمماسبق،ونواتجأيضلأيٍمماسبق. كمايتمالكشفعنتركيباتصيدليةتشتملعليها،طرقلعلاجالتليفالكيسيباستخدامها،وطرقلتصنيعها.
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公开(公告)号:AU2009313198B2
公开(公告)日:2016-03-24
申请号:AU2009313198
申请日:2009-11-10
Applicant: VERTEX PHARMA
Inventor: CHARRIER JEAN-DAMIEN , DURRANT STEVEN , KAY DAVID , O'DONNELL MICHAEL , KNEGTEL RONALD , MACCORMICK SOMHAIRLE , PINDER JOANNE , VIRANI ANISA , YOUNG STEPHEN , BINCH HAYLEY , CLEVELAND THOMAS , FANNING LEV T D , HURLEY DENNIS , JOSHI PRAMOD , SHETH URVI , SILINA ALINA , REAPER PHILIP MICHAEL
IPC: C07D401/04 , A61K31/4965 , A61P35/00 , C07D403/04 , C07D413/04
Abstract: The present disclosure relates to pyrazine compounds of formula (I) wherein L, n, R
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公开(公告)号:NZ593316A
公开(公告)日:2013-06-28
申请号:NZ59331609
申请日:2009-11-10
Applicant: VERTEX PHARMA
Inventor: CHARRIER JEAN-DAMIEN , DURRANT STEVEN , KAY DAVID , O DONNELL MICHAEL , KNEGTEL RONALD , MACCORMICK SOMHAIRLE , PINDER JOANNE , VIRANI ANISA , YOUNG STEPHEN , BINCH HAYLEY , CLEVELAND THOMAS , FANNING LEV T
IPC: C07D413/04 , A61K31/4965 , A61P35/00 , C07D401/04 , C07D403/04
Abstract: 593316 The present disclosure relates to pyrazine compounds of formula (Ia) wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. Compounds of the present disclosure include: 2-[5-Amino-6-[5-[4-(methylaminomethyl)phenyl]-1,3,4-oxadiazol-2-yl]pyrazin-2-yl]-N-ethyl-cyclopropanecarboxamide, 1-(4-(5-Amino-6-(5-( 4-((methylamino)methyl)phenyl)-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)piperidin-1-yl)propan-1-one, 1-(7-(5-Amino-6-(5-( 4-CCmethylamino)methy])phenyl)-I,3A-oxadiazol-2-y])pyrazin-2-y])-2,7-diazaspiro[4,4]nonan-2-y])propan-1-one, 1-{ 7-(5-Amino-6-(5-(4-((methylamino)methyllphenyl)-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-2,7-diazaspiro[4,4]nonan-2-yl} propan-1-one, 1-[S-amino-6-(S-phenyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yI]-3 ,6-dihydro-2H-pyridine-4-carboxylic acid, 3-{ [1,2,4(triazolo[1,S-alpyridin-2-y])-S-(1-(ethylsulfony])-1,2,3,6-tetrahydropyridin-4-y])pyrazin-2-amine, 3-amino-N-(pyridin-2-yl)-6-(4-(thiophen-3-ylsulfonyl)piperazin-1-yl)pyrazine-2-carboxamide, 3-amino-6-(4-(phenylcarbonyl)piperazin-1-yl)-N-(pyridin-2-yl)pyrazine-2-carboxamide, 3-(1H-benzo[d]imidazol-2-yl)-5-(1-(thiophen-2-ylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl)pyrazin-2-amine and 4-(5-amino-6-(3H-imidazo[4,5-b]pyridin-2-yl)pyrazin-2-yl)-N,N-dimethyl-5,6-dihydropyridine-1(2H)-sulfonamide
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公开(公告)号:NO20061543L
公开(公告)日:2006-06-06
申请号:NO20061543
申请日:2006-04-05
Applicant: VERTEX PHARMA
Inventor: MILLER MARK T , RUAH SARA S HADIDA , SINGH ASHAVINI K , CLEVELAND THOMAS , MAKINGS LEWIS R , HAMILTON MATTHEW , GROOTENHUIS PETER D J
IPC: C07D263/48 , A61K31/426 , A61K31/427 , A61P43/00 , C07D277/46 , C07D277/82 , C07D417/02 , C07D417/04 , C07D417/06 , C07D417/12
Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
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公开(公告)号:CA2537841A1
公开(公告)日:2005-03-24
申请号:CA2537841
申请日:2004-09-07
Applicant: VERTEX PHARMA
Inventor: GROOTENHUIS PETER D J , MAKINGS LEWIS R , CLEVELAND THOMAS , HAMILTON MATTHEW , SINGH ASHAVINI K , HADIDA RUAH SARA S , MILLER MARK T
IPC: C07D277/82 , A61K31/426 , A61K31/427 , A61P43/00 , C07D263/48 , C07D277/46 , C07D417/02 , C07D417/04 , C07D417/06 , C07D417/12
Abstract: The present invention relates to modulators of ATP-Binding Cassette ("ABC") transporters or fragments thereof, including CF Transmembrane Regulator ("CFTR"), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
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公开(公告)号:AU2020252367B2
公开(公告)日:2025-04-17
申请号:AU2020252367
申请日:2020-04-02
Applicant: VERTEX PHARMA
Inventor: ABELA ALEXANDER RUSSELL , ABRAHAM SUNNY , ANDERSON COREY DON , ARUMUGAM VIJAYALAKSMI , CHAU JACLYN , CLEMENS JEREMY , CLEVELAND THOMAS , DWIGHT TIMOTHY A , FRIEMAN BRYAN A , GROOTENHUIS PETER , HADIDA RUAH SARA SABINA , ISHIHARA YOSHIHIRO , KRENITSKY PAUL , MCCARTNEY JASON , MELILLO VITO , MILLER MARK THOMAS , SILINA ALINA , UY JOHNNY , ZHOU JINGLAN
IPC: C07D239/69 , A61P11/00 , C07D515/08
Abstract: Compound (I), deuterated derivatives, and pharmaceutically acceptable salts of any of the foregoing are disclosed. Methods of treating cystic fibrosis using these compounds are also disclosed.
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公开(公告)号:PE20250606A1
公开(公告)日:2025-02-26
申请号:PE2024002167
申请日:2023-04-05
Applicant: VERTEX PHARMA
Inventor: ABELA ALEXANDER RUSSELL , CLEMENS JEREMY J , CLEVELAND THOMAS , COON TIMOTHY RICHARD , HADIDA RUAH SARA SABINA , KHATUYA HARIPADA , MCCARTNEY JASON , MILLER MARK THOMAS , PIERRE FABRICE JEAN DENIS , UY JOHNNY , ZHOU JINGLAN , COOK CHRISTOPHER
IPC: C07D515/08 , A61P11/00 , C07D519/00
Abstract: La presente invencion se refiere a moduladores del regulador de la conductancia transmembrana de la fibrosis quistica (CFTR) de formula I, o sus tautomeros, derivados deuterados, y sales farmaceuticamente. Dichos moduladores comprenden al anillo A, en donde Q es -C- y -N-; W es -CH-, -C(F)-, -C(CF3)- y -N-; X2 y X3 son -CH- y -N-; R6 es un heterociclilo de 4 a 6 miembros, cicloalquilo C3-C8 sustituidos con haloalquilo C1-C8, entre otros; Y es -N-, -N(Ry)-, -C(Ry)- y -O-, en donde Ry es haloalquilo C1-C8, cicloalquilo C3- C6, entre otros; y Z es -NRz, en donde Rz es hidrogeno y alquilo C1-C8, entre otros. Asimismo, X1 es -CH- y -N-; R1 y R2 son alcoxi C1-C8, alquilo C1-C8, entre otros; R3a, R3b, R5a y R5b es hidrogeno, halogeno, entre otros; R4 es cicloalquilo C3-C6 o alquilo C1-C9, entre otros; y R7 es O y NR, donde R es hidrogeno o alquilo C1-C8. Tambien, refiere al uso de los moduladores en la fabricacion de un medicamento para tratar la fibrosis quistica; composiciones farmaceuticas combinadas que comprenden al menos a uno de los moduladores, o sus tautomeros, derivados deuterados y sales, junto a un portador farmaceutico; terapias combinadas que emplean esos moduladores; y metodos para el tratamiento de la fibrosis quistica.
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公开(公告)号:CO2022002634A2
公开(公告)日:2022-06-21
申请号:CO2022002634
申请日:2022-03-04
Applicant: VERTEX PHARMA
Inventor: SHI YI , MEDEK ALES , WALDO MICHAEL , ANDERSON COREY DON , CLEMENS JEREMY J , CLEVELAND THOMAS , COON TIMOTHY RICHARD , FRIEMAN BRYAN , GROOTENHUIS PETER (DECEASED) , HADIDA RUAH SARA SABINA , MCCARTNEY JASON , MILLER MARK THOMAS , PARASELLI PRASUNA , PIERRE FABRICE , SWIFT SARA E , ZHOU JINGLAN , SHRESTHA MUNA , GAGNON KEVIN J , LI JICONG , LU JENNIFER , ZHANG BEILI , ZWICKER CARL L
IPC: C07D513/22 , A61K31/435 , A61P11/00
Abstract: Se describen formas cristalinas del Compuesto I: I, sales farmacéuticamente aceptables de este, y solvatos e hidratos de estas. También se describen composiciones farmacéuticas que comprenden las mismas, métodos para tratar la fibrosis quística mediante el uso de las mismas y métodos para fabricar las mismas.
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公开(公告)号:UY39458A
公开(公告)日:2022-05-31
申请号:UY39458
申请日:2021-10-07
Applicant: VERTEX PHARMA
Inventor: GROOTENHUIS PETER , SARA SABINA HADIDA RUAH , CLEVELAND THOMAS , BRYAN A FRIEMAN , KHATUYA HARIPADA , ZHOU JINGLAN , ALEXANDER RUSSELL ABELA , MARK THOMAS MILLER , MCCARTNEY JASON , ABRAHAM SUNNY , COREY DON ANDERSON , ARUMUGAM VIJAYALAKSMI , CHAU JACLYN , CLEMENS JEREMY , TIMOTHY A DWIGHT , ISHIHARA YOSHIHIRO , KRENITSKY PAUL , PIERRE FABRICE , SILINA ALINA , TIMOTHY RICHARD COON , JOE A TRAN , PARASELLI PRASUNA
IPC: A61K31/36 , A61K31/404 , A61K31/443 , A61K31/47 , A61K31/519 , A61P11/00 , C07D515/04 , C07D515/14
Abstract: Esta descripción proporciona moduladores del regulador de conductancia transmembranario de la fibrosis quística (CFTR), composiciones farmacéuticas que contienen al menos uno de tales moduladores, métodos de tratamiento de la fibrosis quística mediante el uso de tales moduladores y composiciones farmacéuticas, y procesos para producir tales moduladores
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公开(公告)号:UY39455A
公开(公告)日:2022-05-31
申请号:UY39455
申请日:2021-10-07
Applicant: VERTEX PHARMA
Inventor: GROOTENHUIS PETER , SARA SABINA HADIDA RUAH , CLEVELAND THOMAS , BRYAN A FRIEMAN , ZHOU JINGLAN , ALEXANDER RUSSELL ABELA , MARK THOMAS MILLER , MCCARTNEY JASON , ABRAHAM SUNNY , COREY DON ANDERSON , ARUMUGAM VIJAYALAKSMI , CHAU JACLYN , CLEMENS JEREMY , TIMOTHY A DWIGHT , ISHIHARA YOSHIHIRO , KRENITSKY PAUL , PIERRE FABRICE , SILINA ALINA
IPC: A61K31/36 , A61K31/404 , A61K31/443 , A61K31/47 , A61K31/519 , A61P11/00 , C07D513/04 , C07D515/04
Abstract: Esta descripción proporciona moduladores del regulador de conductancia transmembranario de la fibrosis quística (CFTR), composiciones farmacéuticas que contienen al menos uno de tales moduladores, métodos de tratamiento de la fibrosis quística mediante el uso de tales moduladores y composiciones farmacéuticas, y procesos para producir tales moduladores
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