公开(公告)号：ES2532433T3

公开(公告)日：2015-03-26

申请号：ES11178128

申请日：2005-03-11

Applicant: VERTEX PHARMA

Inventor： TANOURY GERALD J ,  CHEN MINZHANG ,  JONES ANDREW D ,  NYCE PHILIP L ,  TRUDEAU MARTIN ,  GUERIN DAVID J ,  SNOONIAN JOHN R

IPC: C07D405/12 ,  C07B43/04 ,  C07B57/00

Abstract: Un proceso de producción de un compuesto de**Fórmula** que comprende purificar una mezcla de**Fórmula** en la que R8 es un grupo protector y R9 es alquilo C1-C5, y purificar incluye cristalizar selectivamente o cristalizar dinámicamente la mezcla.

公开(公告)号：DK2399915T3

公开(公告)日：2015-03-09

申请号：DK11178126

申请日：2005-03-11

Applicant: VERTEX PHARMA

Inventor： TANOURY GERALD J ,  CHEN MINZHANG ,  JONES ANDREW D ,  NYCE PHILIP L ,  TRUDEAU MARTIN ,  GUERIN DAVID J ,  SNOONIAN JOHN R

IPC: C07D405/12 ,  C07B43/04 ,  C07B57/00

公开(公告)号：DK2399916T3

公开(公告)日：2015-03-02

申请号：DK11178128

申请日：2005-03-11

Applicant: VERTEX PHARMA

Inventor： TANOURY GERALD J ,  CHEN MINZHANG ,  JONES ANDREW D ,  NYCE PHILIP L ,  TRUDEAU MARTIN ,  GUERIN DAVID J ,  SNOONIAN JOHN R

IPC: C07D405/12 ,  C07B43/04 ,  C07B57/00

公开(公告)号：ES2331250T3

公开(公告)日：2009-12-28

申请号：ES05008137

申请日：2001-12-12

Applicant: VERTEX PHARMA

Inventor： GRILLOT ANNE-LAURE ,  CHARIFSON PAUL ,  STAMOS DEAN ,  LIAO YUSHENG ,  TRUDEAU MARTIN

IPC: C07D235/30 ,  C07D235/32 ,  A61K31/00 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/437 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  A61P31/00 ,  A61P31/04 ,  A61P43/00 ,  C07D213/00 ,  C07D221/00 ,  C07D235/00 ,  C07D263/58 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D471/04 ,  C07D471/14 ,  C07D491/04 ,  C07D491/056 ,  C07D498/04 ,  C07D521/00 ,  C07F9/6558 ,  C07F9/6561

Abstract: Un procedimiento ex vivo para disminuir la cantidad de bacterias en una muestra biológica ex vivo que comprende el paso de poner en contacto dicha muestra biológica con un compuesto de la fórmula I: **(Ver fórmula)** o una sal farmacéuticamente aceptable del mismo, en la que Z es N-R4 u O W es CRa Ra es hidrógeno R4 es hidrógeno R2 es hidrógeno, en la que, cuando Z es O, R1 es fenilo, R3 es hidrógeno y R5 es CO2CH2CH3, cuando Z es N-R4, R3 es hidrógeno, R5 es CO2CH2CH3 y R1 es un grupo seleccionado entre fenilo y 2-, 3- o 4-piridina, **(Ver fórmula)** cuando Z es N-R4 y R3 es bromuro o C3H7, R5 es CO2CH2CH3 y R1 es fenilo; cuando Z es N-R4 y R3 es bromuro, R5 es CO2CH2CH3 y R1 es 3-piridina; cuando Z es N-R4, R3 es hidrógeno, R1 es fenilo, R5 es CO2CH3 o CO2CH2-CCH.

公开(公告)号：MY138797A

公开(公告)日：2009-07-31

申请号：MYPI20015634

申请日：2001-12-12

Applicant: VERTEX PHARMA

Inventor： GRILLOT ANNE-LAURE ,  CHARIFSON PAUL ,  STAMOS DEAN ,  LIAO YUSHENG ,  BADIA MICHAEL ,  TRUDEAU MARTIN

IPC: C07D235/32 ,  C07D403/04 ,  A61K31/00 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/437 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  A61P31/00 ,  A61P31/04 ,  A61P43/00 ,  C07D213/00 ,  C07D221/00 ,  C07D235/00 ,  C07D235/30 ,  C07D263/58 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D471/04 ,  C07D471/14 ,  C07D491/04 ,  C07D491/056 ,  C07D498/04 ,  C07D521/00 ,  C07F9/6558 ,  C07F9/6561

Abstract: THE PRESENT INVENTION RELATES TO COMPOUNDS OF THE FORMULA I:I OR A PHARMACEUTICALLY ACCEPTABLE DERIVATIVE OR PRODRUG THEREOF. THE COMPOUNDS ARE USEFUL AS INHIBITORS OF BACTERIAL GYRASE ACTIVITY. THE PRESENT INVENTION ALSO RELATES TO METHODDS FOR TREATING BACTERIAL INFECTIONS IN MAMMALA. THE PRESENT INVENTION ALSO RELATES TO METHODS FOR DECREASING BACTERIAL QUANTITY IN A BIOLOGICAL SAMPLE.

公开(公告)号：SG150547A1

公开(公告)日：2009-03-30

申请号：SG2009013095

申请日：2005-03-11

Applicant: VERTEX PHARMA

Inventor： TANOURY GERALD J ,  CHEN MINZHANG ,  JONES ANDREW D ,  NYCE PHILIP L ,  TRUDEAU MARTIN ,  GUERIN DAVID J ,  SNOONIAN JOHN R

IPC: C07B43/04 ,  C07B57/00 ,  C07D405/12

Abstract: The invention relates to a process of producing a compound of comprising purifying a mixture of wherein R 8 is a protecting group, and purifying includes chromatographing, selectively crystallizing, or dynamically crystallizing the mixture.

公开(公告)号：BRPI0508102A

公开(公告)日：2007-07-17

申请号：BRPI0508102

申请日：2005-02-28

Applicant: VERTEX PHARMA

Inventor： CHARRIER JEAN-DAMIEN ,  DURRANT STEVEN ,  MORTIMORE MICHAEL ,  O'DONNELL MICHAEL ,  RUTHERFORD ALISTAIR ,  RAMAYA SHARN ,  STUDLEY JOHN R ,  TRUDEAU MARTIN ,  LOOKER ADAM

IPC: C07D405/12 ,  A61K31/401 ,  A61K31/4025 ,  A61K31/403 ,  A61K31/443 ,  A61K38/04 ,  A61K38/06 ,  C07D207/16 ,  C07D209/52 ,  C07D401/12 ,  C07D401/14 ,  C07D417/06 ,  C07D417/12 ,  C07K5/02 ,  C07K5/04

Abstract: The present invention provides a compound of formula (I): wherein the variables are as defined herein. The present invention also provides processes for preparing the compounds of formula (I), and intermediates thereof, pharmaceutical compositions comprising those compounds, and methods of using the compounds and compositions.

公开(公告)号：NO20064344L

公开(公告)日：2006-10-19

申请号：NO20064344

申请日：2006-09-26

Applicant: VERTEX PHARMA

Inventor： CHARRIER JEAN-DAMIEN ,  MORTIMORE MICHAEL ,  DURRANT STEVEN ,  STUDLEY JOHN R ,  O'DONNELL MICHAEL ,  RUTHERFORD ALISTAIR ,  RAMAYA SHARN ,  TRUDEAU MARTIN ,  LOOKER ADAM

IPC: C07D207/16 ,  A61K38/04 ,  A61K38/06 ,  C07D209/52 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D417/06 ,  C07D417/12 ,  C07K5/02 ,  C07K5/04

Abstract: The present invention provides a compound of formula (I): wherein the variables are as defined herein. The present invention also provides processes for preparing the compounds of formula (I), and intermediates thereof, pharmaceutical compositions comprising those compounds, and methods of using the compounds and compositions.

公开(公告)号：AP1498A

公开(公告)日：2005-11-21

申请号：AP2001002298

申请日：2000-03-17

Applicant: VERTEX PHARMA

Inventor： STAMOS DEAN ,  TRUDEAU MARTIN ,  BETHIEL SCOTT ,  BADIA MICHAEL C ,  SAUNDERS JEFFREY

IPC: C07D307/20 ,  A61K31/27 ,  A61K31/275 ,  A61K31/341 ,  A61K31/421 ,  A61K31/422 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/00 ,  A61P1/18 ,  A61P9/10 ,  A61P11/06 ,  A61P19/02 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07C275/40 ,  C07C275/42 ,  C07D263/32 ,  C07D413/12 ,  C07D417/12 ,  C07F9/653 ,  A61K31/277 ,  C07C275/34

Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

公开(公告)号：SI1251848T1

公开(公告)日：2004-12-31

申请号：SI200130127

申请日：2001-01-16

Applicant: VERTEX PHARMA

Inventor： CHARIFSON PAUL ,  STAMOS DEAN ,  BADIA MICHAEL ,  GRILLOT ANNE-LAURE ,  RONKIN STEVEN ,  TRUDEAU MARTIN

IPC: C07D231/38 ,  A61K31/4155 ,  A61K31/421 ,  A61K31/422 ,  A61K31/427 ,  A61K31/454 ,  A61K31/5377 ,  A61P1/00 ,  A61P11/00 ,  A61P13/02 ,  A61P13/08 ,  A61P17/00 ,  A61P17/02 ,  A61P19/02 ,  A61P19/08 ,  A61P25/00 ,  A61P31/04 ,  A61P31/06 ,  A61P43/00 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14

Abstract: The present invention relates to compounds of the formula I: where Ring A is a thiazole, oxazole, imidazole or pyrazole and the substituents are as described in the specification, and pharmaceutically acceptable salts thereof. The compounds inhibit bacterial gyrase activity and therefore are useful for treating bacterial infections in mammals.