公开(公告)号：PL192628B1

公开(公告)日：2006-11-30

申请号：PL32963997

申请日：1997-04-21

Applicant: VERTEX PHARMA

Inventor： ARMISTEAD DAVID M ,  BADIA MICHAEL C ,  BEMIS GUY W ,  BETHIEL RANDY S ,  FRANK CATHARINE A ,  NOVAK PERRY M ,  RONKIN STEVEN M ,  SAUNDERS JEFFREY O

IPC: C07D263/32 ,  A61K31/17 ,  A61K31/18 ,  A61K31/404 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61P9/14 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07C275/42 ,  C07D263/18 ,  C07D277/18 ,  C07D413/12

公开(公告)号：CL2004000139A1

公开(公告)日：2005-04-15

申请号：CL2004000139

申请日：2004-01-29

Applicant: VERTEX PHARMA

Inventor： CHARIFSON PAUL S ,  DEININGER DAVID D ,  GRILLOT ANNE-LAURE ,  LIAO YUSHENG ,  RONKIN STEVEN M ,  STAMOS DEAN

IPC: A61K31/4184 ,  A61P31/04 ,  C07D20090101 ,  C07D231/12 ,  C07D231/20 ,  C07D235/30 ,  C07D239/34 ,  C07D317/50 ,  C07D401/14 ,  C07D411/14 ,  C07D413/14 ,  C07D

公开(公告)号：PT966465E

公开(公告)日：2003-11-28

申请号：PT98909165

申请日：1998-03-13

Applicant: VERTEX PHARMA

Inventor： ARMISTEAD DAVID M ,  SAUNDERS JEFFREY O ,  BADIA MICHAEL C ,  BETHIEL RANDY S ,  FRANK CATHARINE A ,  NOVAK PERRY M ,  RONKIN STEVEN M ,  NAEGELE DOUG ,  PEARLMAN DAVID A

IPC: A61K31/4184 ,  A61K31/422 ,  A61K31/423 ,  A61K31/427 ,  A61K31/428 ,  A61P9/00 ,  C07D277/82 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D235/30 ,  C07D263/58 ,  C07D413/12 ,  C07D417/12 ,  A61K31/42

Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. 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：AT244717T

公开(公告)日：2003-07-15

申请号：AT98909165

申请日：1998-03-13

Applicant: VERTEX PHARMA

Inventor： SAUNDERS JEFFREY O ,  ARMISTEAD DAVID M ,  BADIA MICHAEL C ,  BETHIEL RANDY S ,  FRANK CATHARINE A ,  NAEGELE DOUG ,  NOVAK PERRY M ,  PEARLMAN DAVID A ,  RONKIN STEVEN M

IPC: C07D277/82 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/423 ,  A61K31/427 ,  A61K31/428 ,  A61P9/00 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D235/30 ,  C07D263/58 ,  C07D413/12 ,  C07D417/12 ,  A61K31/42

Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. 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：NZ332405A

公开(公告)日：2000-06-23

申请号：NZ33240597

申请日：1997-04-21

Applicant: VERTEX PHARMA

Inventor： ARMISTEAD DAVID M ,  BADIA MICHAEL C ,  BETHIEL RANDY S ,  FRANK CATHERINE A ,  BEMIS GUY W ,  NOVAK PERRY M ,  RONKIN STEVEN M ,  SAUNDERS JEFFREY O

IPC: A61K31/17 ,  A61K31/18 ,  A61K31/404 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61P9/14 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07C275/42 ,  C07D263/18 ,  C07D263/32 ,  C07D277/18 ,  C07D413/12 ,  C07C275/28 ,  C07C275/34

Abstract: The oxazolyl, thiazolyl or phenyl urea derivatives have the formula I, II, III or IV wherein: A is an optionally substituted alkyl, alkenyl or alkynyl; B and B' are independently an optionally saturated optionally substituted mono or bicyclic ring system optionally having up to 4 heteroatoms selected from N, O or S; D is -C(O)-, -C(S)- or -S(O)2-; G and G' are independently R1 or H; R1 is 1,2-methylenedioxy, 1,2-ethylenedioxy, -(CH2)n-Y or R6; R6 is H or optionally substituted alkyl or alkenyl; K and J are independently R1 or are as defined in the specification; n is 0 to 2; Y is halo, CN, nitro, CF3, OCF3, OR6, S(O)nR6, N(R6)2, NR6R8 or COOR6; R8 is an amino protecting group; E is O or S and any carbon atom in A, R2 and R6 is optionally replaced by -O-, -S(O)n-, -NH- or -N(alkyl)-. A pharmaceutical composition thereof is useful for treating or preventing IMPDH mediated diseases. The compound of formula V and VI A-NH-D-NH-A (V) B-NH-D-NH-B (VI) are used in a manufacture of a medicament for inhibiting IMPDH activity. In formulae V and VI A, D and B are as defined above.

公开(公告)号：AP813A

公开(公告)日：2000-02-28

申请号：AP9700973

申请日：1997-04-23

Applicant: VERTEX PHARMA

Inventor： ARMISTEAD DAVID ,  BADIA MICHAEL C ,  BEMIS GUY ,  BETHIEL RANDY S ,  FRANK CATHRINE A ,  NOVAK PERRY M ,  RONKIN STEVEN M ,  SAUNDERS JEFFREY

IPC: A61K31/17 ,  A61K31/18 ,  A61K31/404 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61P9/14 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07C275/42 ,  C07D263/18 ,  C07D263/32 ,  C07D277/18 ,  C07D413/12 ,  C07C275/00 ,  A61

Abstract: A class of compounds which are IMPDH inhibitors, and pharmaceutical compositions comprising these compounds, of the formula: A is selected from (Ci-C6) alkyl, or (C2-C6)- alkenyl or alkynyl; B is a monocyclic or bicyclic ring system, D is selected from C(O), C(S), or S(0)2.

公开(公告)号：SK146198A3

公开(公告)日：1999-07-12

申请号：SK146198

申请日：1997-04-21

Applicant: VERTEX PHARMA

Inventor： ARMISTEAD DAVID M ,  BADIA MICHAEL C ,  BEMIS GUY W ,  BETHIEL RANDY S ,  FRANK CATHARINE A ,  NOVAK PERRY M ,  RONKIN STEVEN M ,  SAUNDERS JEFFREY O

IPC: A61K31/17 ,  A61K31/18 ,  A61K31/404 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61P9/14 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07C275/42 ,  C07D263/18 ,  C07D263/32 ,  C07D277/18 ,  C07D413/12 ,  C07C275/28 ,  C07C275/34

Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. 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：CZ338098A3

公开(公告)日：1999-02-17

申请号：CZ338098

申请日：1997-04-21

Applicant: VERTEX PHARMA

Inventor： ARMISTEAD DAVID M ,  BADIA MICHAEL C ,  BEMIS GUY W ,  BETHIEL RANDY S ,  FRANK CATHARINE A ,  NOVAK PERRY M ,  RONKIN STEVEN M ,  SAUNDERS JEFFREY O

IPC: A61K31/17 ,  A61K31/18 ,  A61K31/404 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61P9/14 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07C275/42 ,  C07D263/18 ,  C07D263/32 ,  C07D277/18 ,  C07D413/12 ,  C07C275/28 ,  C07C275/34

Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. 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：NO984917D0

公开(公告)日：1998-10-22

申请号：NO984917

申请日：1998-10-22

Applicant: VERTEX PHARMA

Inventor： ARMISTEAD DAVID M ,  BADIA MICHAEL C ,  BEMIS GUY W ,  BETHIEL RADNY S ,  FRANK CATHARINE A ,  NOVAK PERRY M ,  RONKIN STEVEN M ,  SAUNDERS JEFFREY O

IPC: A61K31/17 ,  A61K31/18 ,  A61K31/404 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61P9/14 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07C275/42 ,  C07D263/18 ,  C07D263/32 ,  C07D277/18 ,  C07D413/12 ,  C07D

Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. 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：JOP20210301A1

公开(公告)日：2023-01-30

申请号：JOP20210301

申请日：2020-05-14

Applicant: VERTEX PHARMA

Inventor： SHI YI ,  TAPLEY TIMOTHY LEWIS ,  SWETT REBECCA JANE ,  XU JINWANG ,  MAXWELL JOHN PATRICK ,  SHRESTHA MUNA ,  OVERHOFF KIRK ALAN ,  BANDARAGE UPUL KEERTHI ,  BRODNEY MICHAEL AARON ,  BLIGH CAVAN MCKEON ,  BOUCHER DIANE ,  BOYD MICHAEL JOHN ,  TANG QING ,  THOMSON STEPHEN ,  GAGNON KEVIN JAMES ,  GREY JR RONALD LEE ,  JONES PETER ,  JOHNSON JR MAC ARTHUR ,  GUIDO SAMANTHA ,  GIACOMETTI ROBERT DANIEL ,  GIROUX SIMON ,  DAMAGNEZ VERONIQUE ,  RODAY SETU ,  RONKIN STEVEN M ,  ROEPER STEFANIE ,  ZAKY MARIAM ,  SAWANT RUPA ,  SPOSATO MARISA ,  STAVROPOULOS KATHY ,  GARCIA BARRANTES PEDRO MANUEL ,  FANNING LEV TYLER DEWEY ,  FLEMING GABRIELLE SIMONE ,  FIMOGNARI ROBERT FRANCIS ,  CLARK MICHAEL PHILIP ,  COTTRELL KEVIN MICHAEL ,  KESAVAN SARATHY ,  LAI MEI-HSIU ,  LOOKER ADAM ,  LIU SIYING ,  MAXWELL BRAD ,  MEDEK ALES ,  NUHANT PHILIPPE MARCEL ,  HOOD SARAH CAROL ,  HALL AMY BETH ,  HURLEY DENNIS JAMES

Abstract: يوفرالكشفالحاليمركباتمُفيدةلعلاجنقصمضادتريبسينألفا-1 (AATD)،وفقًاللصيغة (I): (I)،ومماثلاتكيميائيةمنها،وأملاحمقبولةصيدليًامنالمركبات،وأملاحمقبولةصيدليًامنالمماثلاتالكيميائية،ومشتقاتمُعالجةبالديوتريوممنالمركبات،ومشتقاتمعالجةبالديوتريوممنالمماثلاتالكيميائية،ومشتقاتمُعالجةبالديوتريوممنالأملاح،والصورالصلبةمنتلكالمركباتوعملياتتحضيرتلكالمركبات.