公开(公告)号：WO2013142124A1

公开(公告)日：2013-09-26

申请号：PCT/US2013030267

申请日：2013-03-11

Applicant: VERTEX PHARMA

Inventor： KULDIPKUMAR ANUJ K ,  MEDEK ALES ,  FERRIS LORI ANN ,  MUDUNURI PRAVEEN ,  JUNG YOUNG CHUN ,  WILLCOX DAVID RICHARD ,  WALDO MICHAEL ,  NUGENT WILLIAM ALOYSIUS

IPC: C07H19/06 ,  A61K31/7072 ,  A61P31/14

CPC classification number: C07H19/10 ,  A61K31/7056 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K38/00 ,  A61K45/06 ,  C07B2200/13 ,  C07H19/06 ,  A61K2300/00

Abstract: The present application relates to solid state forms, for example, crystalline forms of 2'- C-methyluridine-5 '-(O-phenyl-N-(S)- 1 -(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2'-C-methyluridine-5'- (0-phenyl-N-(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2'-C-methyluridine-5'- (O-phenyl-N-(S)- 1 -(isopropoxy carbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2'-C- methyluridine-5 '-(O-phenyl-N-(S)- 1 -(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.

Abstract translation: 本申请涉及固体形式，例如2'-C-甲基尿苷-5' - （O-苯基-N-（S）-1-（异丙氧基羰基）乙基）硫代磷酰胺的结晶形式，可以包括 一种或多种固体形式的2'-C-甲基尿苷-5'-（O-苯基-N-（S）-1-（异丙氧基羰基）乙基）硫代氨基磷酸酯，以及用一种或多种硫代磷酸酰胺酯治疗或改善疾病和/或病症的方法 更多固体形式的2'-C-甲基尿苷-5'-（O-苯基-N-（S）-1-（异丙氧基羰基）乙基）硫代磷酰胺。 本文还公开的是使用一种或多种固体形式的2'-C-甲基尿苷-5' - （O-苯基-N-（S）-1-（异丙氧基羰基）乙基）硫代磷酰胺的组合治疗疾病和/或病症的方法 与一个或多个其他代理。

公开(公告)号：CA2824403C

公开(公告)日：2019-09-24

申请号：CA2824403

申请日：2012-01-13

Applicant: VERTEX PHARMA

Inventor： SHANNON DEAN ,  LUISI BRIAN ,  KRAWIEC MARIUSZ ,  KULDIPKUMAR ANUJ K

IPC: C07D413/14 ,  A61K31/4184 ,  A61P31/00

Abstract: The present application is directed to solid forms of compounds of formula (I) and pharmaceutically acceptable salts thereof, that inhibit bacterial gyrase and/or Topo IV and pharmaceutical compositions comprising said compounds and salts. These compounds and salts are useful in treating bacterial infections.

公开(公告)号：NZ612918A

公开(公告)日：2015-10-30

申请号：NZ61291812

申请日：2012-01-13

Applicant: VERTEX PHARMA

Inventor： KRAWIEC MARIUSZ ,  SHANNON DEAN ,  LUISI BRIAN ,  KULDIPKUMAR ANUJ K

IPC: C07D413/14 ,  A61K31/4184 ,  A61P31/00

Abstract: The disclosure relates to crystalline forms of 8(R)-1-ethyl-3-[6-fluoro-5-[2-(1-hydroxy-1-methyl-ethyl) pyrimidin-5-yl]-7-(tetrahydrofuran-2-yl)-1H-benzimidazol-2-yl]urea represented by formula (I) and hydrochloride and mesylate salts thereof, which inhibit bacterial enzymes gyrase and/or topoisomerase IV. Also disclosed are pharmaceutical compositions comprising said compound of formula (I) or its salts and their use for treating bacterial infection caused by Mycobacterium tuberculosis, Streptococcus pneumoniae, Staphylococcus epidermidis, Enterococcus faecalis, Staphylococcus aureus, Clostridium difficile, Moraxella catarrhalis, Neisseria gonorrhoeae, Neisseria meningitidis, Mycobacterium avium complex, Mycobacterium abscessus, Mycobacterium kansasii, Mycobacterium ulcerans, Chlamydophila pneumoniae, Chlamydia trachomatis, Haemophilus injluenzae, Streptococcus pyogenes or &bgr;-haemolytic streptococci.

公开(公告)号：ZA201305231B

公开(公告)日：2014-11-26

申请号：ZA201305231

申请日：2013-07-11

Applicant: VERTEX PHARMA

Inventor： SHANNON DEAN ,  LUISI BRIAN ,  KRAWIEC MARUISZ ,  KULDIPKUMAR ANUJ K

IPC: C07D20060101 ,  A61K20060101 ,  A61P20060101

Abstract: The present application is directed to solid forms of compounds of formula I: and pharmaceutically acceptable salts thereof, that inhibit bacterial gyrase and/or Topo IV and pharmaceutical compositions comprising said compounds and salts. These compounds and salts are useful in treating bacterial infections.

公开(公告)号：MX2013008161A

公开(公告)日：2013-08-27

申请号：MX2013008161

申请日：2012-01-13

Applicant: VERTEX PHARMA

Inventor： KRAWIEC MARIUSZ ,  LUISI BRIAN ,  SHANNON DEAN ,  KULDIPKUMAR ANUJ K

IPC: C07D413/14 ,  A61K31/4184 ,  A61P31/00

Abstract: La presente solicitud se dirige a formas sólidas de compuestos de la fórmula (I) y sales farmacéuticamente aceptables de la misma, que inhiben la girasa y/o Topo IV bacterianas y composiciones farmacéuticas que comprende los compuestos y sales. Estos compuestos y sales son útiles en el tratamiento de infecciones bacterianas.

公开(公告)号：CA2824403A1

公开(公告)日：2012-07-19

申请号：CA2824403

申请日：2012-01-13

Applicant: VERTEX PHARMA

Inventor： SHANNON DEAN ,  LUISI BRIAN ,  KRAWIEC MARIUSZ ,  KULDIPKUMAR ANUJ K

IPC: C07D413/14 ,  A61K31/4184 ,  A61P31/00

Abstract: The present application is directed to solid forms of compounds of formula (I) and pharmaceutically acceptable salts thereof, that inhibit bacterial gyrase and/or Topo IV and pharmaceutical compositions comprising said compounds and salts. These compounds and salts are useful in treating bacterial infections.

公开(公告)号：CL2013002027A1

公开(公告)日：2013-12-13

申请号：CL2013002027

申请日：2013-07-12

Applicant: VERTEX PHARMA

Inventor： SHANNON DEAN ,  LUISI BRAIN ,  KRAWIEC MARIUSZ ,  KULDIPKUMAR ANUJ K

IPC: C07D239/26 ,  A61K31/506 ,  A61P31/04

公开(公告)号：UY34701A

公开(公告)日：2014-10-31

申请号：UY34701

申请日：2013-03-21

Applicant: VERTEX PHARMA

Inventor： MUDUNURI PRAVEEN ,  CHUN JUNG YOUNG ,  KULDIPKUMAR ANUJ K ,  MEDEK ALES ,  ANN FERRIS LORI ,  RICHARD WILLCOX DAVID ,  WALDO MICHAEL ,  ALOYSIUS NUGENT WILLIAM

IPC: C12N15/00

Abstract: La presente solicitud se refiere a formas de estado sólido, por ejemplo, a formas cristalinas de 2?C?metiluridin?5??(O?fenil?N?(S)?1?(isopropoxicarbonil)etil)tiofosforamidato, a composiciones farmacéuticas que pueden incluir una o mas formas sólidas de 2??C?metiluridin?5?(O?fenil?N?(S)?1?(isopropoxicarbonil)etil)tiofosforamidato, y a métodos para tratar o mejorar enfermedades y/o condiciones con una o mas formas sólidas de 2??C?metiluridin?5?(O?fenil?N?(S)?1?(isopropoxicarbonil)etil) tiofosforamidato. En la presente se revelan también métodos para tratar una o mas formas sólidas de 2??C?metiluridin?5??(O?fenil?N?(S)?1?(isopropoxicarbonil)etil) tiofosforamidato en combinación uno o más otros agentes.

公开(公告)号：SG191927A1

公开(公告)日：2013-08-30

申请号：SG2013053186

申请日：2012-01-13

Applicant: VERTEX PHARMA

Inventor： SHANNON DEAN ,  LUISI BRIAN ,  KRAWIEC MARIUSZ ,  KULDIPKUMAR ANUJ K

Abstract: The present application is directed to solid forms of compounds of formula (I) and pharmaceutically acceptable salts thereof, that inhibit bacterial gyrase and/or Topo IV and pharmaceutical compositions comprising said compounds and salts. These compounds and salts are useful in treating bacterial infections.

公开(公告)号：AU2012205419A1

公开(公告)日：2013-08-01

申请号：AU2012205419

申请日：2012-01-13

Applicant: VERTEX PHARMA

Inventor： SHANNON DEAN ,  LUISI BRIAN ,  KRAWIEC MARIUSZ ,  KULDIPKUMAR ANUJ K

IPC: C07D413/14 ,  A61K31/4184 ,  A61P31/00

Abstract: The present application is directed to solid forms of compounds of formula (I) and pharmaceutically acceptable salts thereof, that inhibit bacterial gyrase and/or Topo IV and pharmaceutical compositions comprising said compounds and salts. These compounds and salts are useful in treating bacterial infections.