公开(公告)号：US06716839B2

公开(公告)日：2004-04-06

申请号：US10378108

申请日：2003-02-26

申请人： Douglas Wade Beight ,  Trelia Joyce Craft ,  Jeffry Bernard Franciskovich ,  Theodore Goodson, Jr. ,  Steven Edward Hall ,  David Kent Herron ,  Sajan Joseph ,  Valentine Joseph Klimkowski ,  Jeffrey Alan Kyle ,  John Joseph Masters ,  David Mendel ,  Guy Milot ,  Marta Maria Piñeiro-Núñez ,  Jason Scott Sawyer ,  Robert Theodore Shuman ,  Gerald Floyd Smith ,  Anne Louise Tebbe ,  Jennifer Marie Tinsley ,  Leonard Crayton Weir ,  James Howard Wikel ,  Michael Robert Wiley ,  Ying Kwong Yee

发明人： Douglas Wade Beight ,  Trelia Joyce Craft ,  Jeffry Bernard Franciskovich ,  Theodore Goodson, Jr. ,  Steven Edward Hall ,  David Kent Herron ,  Sajan Joseph ,  Valentine Joseph Klimkowski ,  Jeffrey Alan Kyle ,  John Joseph Masters ,  David Mendel ,  Guy Milot ,  Marta Maria Piñeiro-Núñez ,  Jason Scott Sawyer ,  Robert Theodore Shuman ,  Gerald Floyd Smith ,  Anne Louise Tebbe ,  Jennifer Marie Tinsley ,  Leonard Crayton Weir ,  James Howard Wikel ,  Michael Robert Wiley ,  Ying Kwong Yee

IPC分类号： A61K315377

CPC分类号： C07D295/135 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14

摘要： This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

公开(公告)号：US06635657B1

公开(公告)日：2003-10-21

申请号：US09857751

申请日：2001-06-08

申请人： Douglas Wade Beight ,  Trelia Joyce Craft ,  Carl Penman Denny ,  Jeffry Bernard Franciskovich ,  Theodore Goodson ,  Steven Edward Hall ,  David Kent Herron ,  Sajan Joseph ,  Valentine Joseph Klimkowski ,  Jeffrey Alan Kyle ,  John Joseph Masters ,  David Mendel ,  Guy Milot ,  Marta Maria Piñeiro-Núñez ,  Jason Scott Sawyer ,  Robert Theodore Shuman ,  Gerald Floyd Smith ,  Anne Louise Tebbe ,  Jennifer Marie Tinsley ,  Leonard Crayton Weir ,  James Howard Wikel ,  Michael Robert Wiley ,  Ying Kwong Yee

发明人： Douglas Wade Beight ,  Trelia Joyce Craft ,  Carl Penman Denny ,  Jeffry Bernard Franciskovich ,  Theodore Goodson ,  Steven Edward Hall ,  David Kent Herron ,  Sajan Joseph ,  Valentine Joseph Klimkowski ,  Jeffrey Alan Kyle ,  John Joseph Masters ,  David Mendel ,  Guy Milot ,  Marta Maria Piñeiro-Núñez ,  Jason Scott Sawyer ,  Robert Theodore Shuman ,  Gerald Floyd Smith ,  Anne Louise Tebbe ,  Jennifer Marie Tinsley ,  Leonard Crayton Weir ,  James Howard Wikel ,  Michael Robert Wiley ,  Ying Kwong Yee

IPC分类号： A61K314545

CPC分类号： C07D213/75 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

摘要： This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

摘要翻译： 本申请涉及如本文所定义的式I化合物（或其药学上可接受的盐），其药物组合物及其作为因子Xa抑制剂的用途，以及其制备方法及其中间体。

公开(公告)号：US06605626B2

公开(公告)日：2003-08-12

申请号：US09961164

申请日：2001-09-21

申请人： Douglas Wade Beight ,  Trelia Joyce Craft ,  Jeffry Bernard Franciskovich ,  Theodore Goodson Jr. ,  Steven Edward Hall ,  David Kent Herron ,  Valentine Joseph Klimkowski ,  Jeffrey Alan Kyle ,  John Joseph Masters ,  David Mendel ,  Guy Milot ,  Jason Scott Sawyer ,  Robert Theodore Shuman ,  Gerald Floyd Smith ,  Anne Louise Tebbe ,  Jennifer Marie Tinsley ,  Leonard Crayton Weir ,  James Howard Wikel ,  Michael Robert Wiley ,  Ying Kwong Yee

发明人： Douglas Wade Beight ,  Trelia Joyce Craft ,  Jeffry Bernard Franciskovich ,  Theodore Goodson Jr. ,  Steven Edward Hall ,  David Kent Herron ,  Valentine Joseph Klimkowski ,  Jeffrey Alan Kyle ,  John Joseph Masters ,  David Mendel ,  Guy Milot ,  Jason Scott Sawyer ,  Robert Theodore Shuman ,  Gerald Floyd Smith ,  Anne Louise Tebbe ,  Jennifer Marie Tinsley ,  Leonard Crayton Weir ,  James Howard Wikel ,  Michael Robert Wiley ,  Ying Kwong Yee

IPC分类号： A61K3144

CPC分类号： C07D209/48 ,  C07C233/75 ,  C07C235/56 ,  C07C237/40 ,  C07C237/42 ,  C07C237/44 ,  C07C257/18 ,  C07C259/18 ,  C07C307/10 ,  C07C311/08 ,  C07C311/09 ,  C07C311/16 ,  C07C311/21 ,  C07C317/44 ,  C07C317/50 ,  C07C2603/18 ,  C07D209/58 ,  C07D209/64 ,  C07D211/22 ,  C07D211/34 ,  C07D211/46 ,  C07D211/62 ,  C07D211/78 ,  C07D211/96 ,  C07D213/30 ,  C07D213/56 ,  C07D213/70 ,  C07D213/75 ,  C07D261/10 ,  C07D277/56 ,  C07D295/185 ,  C07D307/85 ,  C07D317/58 ,  C07D333/70 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D417/06

摘要： This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

公开(公告)号：US06313122B1

公开(公告)日：2001-11-06

申请号：US09445972

申请日：2000-03-20

申请人： Douglas Wade Beight ,  Trelia Joyce Craft ,  Jeffry Bernard Franciskovich ,  Theodore Goodson, Jr. ,  Steven Edward Hall ,  David Kent Herron ,  Valentine Joseph Klimkowski ,  Jeffrey Alan Kyle ,  John Joseph Masters ,  David Mendel ,  Guy Milot ,  Jason Scott Sawyer ,  Robert Theodore Shuman ,  Gerald Floyd Smith ,  Anne Louise Tebbe ,  Jennifer Marie Tinsley ,  Leonard Crayton Weir ,  James Howard Wikel ,  Michael Robert Wiley ,  Ying Kwong Yee

发明人： Douglas Wade Beight ,  Trelia Joyce Craft ,  Jeffry Bernard Franciskovich ,  Theodore Goodson, Jr. ,  Steven Edward Hall ,  David Kent Herron ,  Valentine Joseph Klimkowski ,  Jeffrey Alan Kyle ,  John Joseph Masters ,  David Mendel ,  Guy Milot ,  Jason Scott Sawyer ,  Robert Theodore Shuman ,  Gerald Floyd Smith ,  Anne Louise Tebbe ,  Jennifer Marie Tinsley ,  Leonard Crayton Weir ,  James Howard Wikel ,  Michael Robert Wiley ,  Ying Kwong Yee

IPC分类号： A61K314545

CPC分类号： C07D209/48 ,  C07C233/75 ,  C07C235/56 ,  C07C237/40 ,  C07C237/42 ,  C07C237/44 ,  C07C257/18 ,  C07C259/18 ,  C07C307/10 ,  C07C311/08 ,  C07C311/09 ,  C07C311/16 ,  C07C311/21 ,  C07C317/44 ,  C07C317/50 ,  C07C2603/18 ,  C07D209/58 ,  C07D209/64 ,  C07D211/22 ,  C07D211/34 ,  C07D211/46 ,  C07D211/62 ,  C07D211/78 ,  C07D211/96 ,  C07D213/30 ,  C07D213/56 ,  C07D213/70 ,  C07D213/75 ,  C07D261/10 ,  C07D277/56 ,  C07D295/185 ,  C07D307/85 ,  C07D317/58 ,  C07D333/70 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D417/06

摘要： This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

公开(公告)号：US06417200B1

公开(公告)日：2002-07-09

申请号：US09445970

申请日：2000-05-09

申请人： Douglas Wade Beight ,  Trelia Joyce Craft ,  Jeffry Bernard Franciskovich ,  Theodore Goodson, Jr. ,  Steven Edward Hall ,  David Kent Herron ,  Valentine Joseph Klimkowski ,  John Joseph Masters ,  David Mendel ,  Guy Milot ,  Jason Scott Sawyer ,  Robert Theodore Shuman ,  Gerald Floyd Smith ,  Anne Louise Tebbe ,  Jennifer Marie Tinsley ,  Leonard Crayton Weir ,  James Howard Wikel ,  Michael Robert Wiley ,  Ying Kwong Yee

发明人： Douglas Wade Beight ,  Trelia Joyce Craft ,  Jeffry Bernard Franciskovich ,  Theodore Goodson, Jr. ,  Steven Edward Hall ,  David Kent Herron ,  Valentine Joseph Klimkowski ,  John Joseph Masters ,  David Mendel ,  Guy Milot ,  Jason Scott Sawyer ,  Robert Theodore Shuman ,  Gerald Floyd Smith ,  Anne Louise Tebbe ,  Jennifer Marie Tinsley ,  Leonard Crayton Weir ,  James Howard Wikel ,  Michael Robert Wiley ,  Ying Kwong Yee

IPC分类号： A61K31445

CPC分类号： C07C271/66 ,  A61K31/00 ,  C07C257/18 ,  C07C259/18 ,  C07C271/64 ,  C07D209/44 ,  C07D211/60 ,  C07D261/20 ,  C07D333/38

摘要： This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

公开(公告)号：US06677369B2

公开(公告)日：2004-01-13

申请号：US10133907

申请日：2002-04-25

申请人： Douglas Wade Beight ,  Trelia Joyce Craft ,  Jeffry Bernard Franciskovich ,  Theodore Goodson, Jr. ,  Steven Edward Hall ,  David Kent Herron ,  Valentine Joseph Klimkowski ,  John Joseph Masters ,  David Mendel ,  Guy Milot ,  Jason Scott Sawyer ,  Robert Theodore Shuman ,  Gerald Floyd Smith ,  Anne Louise Tebbe ,  Jennifer Marie Tinsley ,  Leonard Crayton Weir ,  James Howard Wikel ,  Michael Robert Wiley ,  Ying Kwong Yee

发明人： Douglas Wade Beight ,  Trelia Joyce Craft ,  Jeffry Bernard Franciskovich ,  Theodore Goodson, Jr. ,  Steven Edward Hall ,  David Kent Herron ,  Valentine Joseph Klimkowski ,  John Joseph Masters ,  David Mendel ,  Guy Milot ,  Jason Scott Sawyer ,  Robert Theodore Shuman ,  Gerald Floyd Smith ,  Anne Louise Tebbe ,  Jennifer Marie Tinsley ,  Leonard Crayton Weir ,  James Howard Wikel ,  Michael Robert Wiley ,  Ying Kwong Yee

IPC分类号： A61K31381

CPC分类号： C07C271/66 ,  A61K31/00 ,  C07C257/18 ,  C07C259/18 ,  C07C271/64 ,  C07D209/44 ,  C07D211/60 ,  C07D261/20 ,  C07D333/38

摘要： This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

公开(公告)号：US06759414B2

公开(公告)日：2004-07-06

申请号：US10629760

申请日：2003-07-29

申请人： Douglas Wade Beight ,  Trelia Joyce Craft ,  Carl Penman Denny ,  Jeffry Bernard Franciskovich ,  Theodore Goodson, Jr. ,  Steven Edward Hall ,  David Kent Herron ,  Sajan Joseph ,  Valentine Joseph Klimkowski ,  Jeffrey Alan Kyle ,  John Joseph Masters ,  David Mendel ,  Guy Milet ,  Marta Maria Piñeiro-Nuñez ,  Jason Scott Sawyer ,  Robert Theodore Shuman ,  Gerald Floyd Smith ,  Anne Louise Tebbe ,  Jennifer Marie Tinsley ,  Leonard Crayton Weir ,  James Howard Wikel ,  Michael Robert Wiley ,  Ying Kwong Yee

发明人： Douglas Wade Beight ,  Trelia Joyce Craft ,  Carl Penman Denny ,  Jeffry Bernard Franciskovich ,  Theodore Goodson, Jr. ,  Steven Edward Hall ,  David Kent Herron ,  Sajan Joseph ,  Valentine Joseph Klimkowski ,  Jeffrey Alan Kyle ,  John Joseph Masters ,  David Mendel ,  Guy Milet ,  Marta Maria Piñeiro-Nuñez ,  Jason Scott Sawyer ,  Robert Theodore Shuman ,  Gerald Floyd Smith ,  Anne Louise Tebbe ,  Jennifer Marie Tinsley ,  Leonard Crayton Weir ,  James Howard Wikel ,  Michael Robert Wiley ,  Ying Kwong Yee

IPC分类号： A61K315501

CPC分类号： C07D213/75 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

摘要： This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

公开(公告)号：US06583173B2

公开(公告)日：2003-06-24

申请号：US09967054

申请日：2001-09-28

申请人： Douglas Wade Beight ,  Trelia Joyce Craft ,  Jeffrey Bernard Franciskovich ,  Theodore Goodson, Junior ,  Steven Edward Hall ,  David Kent Herron ,  Valentine Joseph Klimkowski ,  Jeffrey Alan Kyle ,  John Joseph Masters ,  David Mendel ,  Guy Milot ,  Jason Scott Sawyer ,  Robert Theodore Shuman ,  Gerald Floyd Smith ,  Anne Louise Tebbe ,  Jennifer Marie Tinsley ,  Leonard Crayton Weir ,  James Howard Wikel ,  Michael Robert Wiley ,  Ying Kwong Yee

发明人： Douglas Wade Beight ,  Trelia Joyce Craft ,  Jeffrey Bernard Franciskovich ,  Theodore Goodson, Junior ,  Steven Edward Hall ,  David Kent Herron ,  Valentine Joseph Klimkowski ,  Jeffrey Alan Kyle ,  John Joseph Masters ,  David Mendel ,  Guy Milot ,  Jason Scott Sawyer ,  Robert Theodore Shuman ,  Gerald Floyd Smith ,  Anne Louise Tebbe ,  Jennifer Marie Tinsley ,  Leonard Crayton Weir ,  James Howard Wikel ,  Michael Robert Wiley ,  Ying Kwong Yee

IPC分类号： A61K31381

CPC分类号： C07D213/75 ,  A61K31/44 ,  C07D209/42 ,  C07D333/38

摘要： This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

公开(公告)号：US07320995B2

公开(公告)日：2008-01-22

申请号：US10522227

申请日：2003-07-31

申请人： Rosanne Bonjouklian ,  Jose Eugenio De Diego Gomez ,  Alfonso De Dios ,  Chafiq Hamdouchi Hamdouchi ,  Tiecho Li ,  Beatriz Lopez De Uralde Garmendia ,  Michal Vieth ,  Jeremy Schulenberg York ,  Robert Dean Dally ,  Miriam Filadelfa Del Prado Catalina ,  Carlos Jaramillo Aguado ,  Luisa Maria Martin-Cabrejas ,  Carlos Montero Salgado ,  Sheila Pleite Selgas ,  Concepcion Sanchez-Martinez ,  Timothy Alan Shepherd ,  James Howard Wikel

发明人： Rosanne Bonjouklian ,  Jose Eugenio De Diego Gomez ,  Alfonso De Dios ,  Chafiq Hamdouchi Hamdouchi ,  Tiecho Li ,  Beatriz Lopez De Uralde Garmendia ,  Michal Vieth ,  Jeremy Schulenberg York ,  Robert Dean Dally ,  Miriam Filadelfa Del Prado Catalina ,  Carlos Jaramillo Aguado ,  Luisa Maria Martin-Cabrejas ,  Carlos Montero Salgado ,  Sheila Pleite Selgas ,  Concepcion Sanchez-Martinez ,  Timothy Alan Shepherd ,  James Howard Wikel

IPC分类号： A61K31/4184 ,  A61K31/428 ,  C07D277/68 ,  C07D235/10

CPC分类号： C07D403/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D513/04

摘要： The present invention provides kinase inhibitors of Formula I: wherein W represents inter alia imidazol, oxazol, pyrazol, thiazol as triazol, which are substituted by phenyl or thienyl. The disclosed compounds inhibit p-38 kinase and are useful in the treatment of metastasis or rheumatoid arthritis

摘要翻译： 本发明提供式I的激酶抑制剂：其中W代表由苯基或噻吩取代的咪唑，恶唑，吡唑，噻唑三唑。 所公开的化合物抑制p-38激酶，并且可用于治疗转移或类风湿性关节炎