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公开(公告)号:US07417064B2
公开(公告)日:2008-08-26
申请号:US10532657
申请日:2003-10-24
Applicant: Serge Louis Boulet , Sandra Ann Filla , Peter Thaddeus Gallagher , Kevin John Hudziak , Anette Margareta Johansson , Rushad E. Karanjawala , John Joseph Masters , Victor Giulio Matassa , Brian Michael Mathes , Richard Edmund Rathmell , Maria Ann Whatton , Chad Nolan Wolfe
Inventor: Serge Louis Boulet , Sandra Ann Filla , Peter Thaddeus Gallagher , Kevin John Hudziak , Anette Margareta Johansson , Rushad E. Karanjawala , John Joseph Masters , Victor Giulio Matassa , Brian Michael Mathes , Richard Edmund Rathmell , Maria Ann Whatton , Chad Nolan Wolfe
IPC: A61K31/381 , C07D333/64
CPC classification number: C07C217/20 , C07C217/34 , C07D333/54
Abstract: There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from H, OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1-C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; with the proviso that, when Z is H, then Y may not be optionally substituted phenyl or optionally substituted naphthyl.
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公开(公告)号:US07163938B2
公开(公告)日:2007-01-16
申请号:US10415756
申请日:2001-11-14
Applicant: David Kent Herron , Sajan Joseph , Angela Lynn Marquart , John Joseph Masters , David Mendel , Gerald Floyd Smith , Philip Parker Waid , Michael Robert Wiley , Ying Kwong Yee
Inventor: David Kent Herron , Sajan Joseph , Angela Lynn Marquart , John Joseph Masters , David Mendel , Gerald Floyd Smith , Philip Parker Waid , Michael Robert Wiley , Ying Kwong Yee
IPC: A61P7/00 , A61K31/44 , A61K31/55 , C07D213/00 , C07D401/12
CPC classification number: C07D213/75 , C07D213/81 , C07D401/12 , C07D401/14
Abstract: 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.
Abstract translation: 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。
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公开(公告)号:US07160878B2
公开(公告)日:2007-01-09
申请号:US10332120
申请日:2001-07-18
Applicant: David Kent Herron , Sajan Joseph , Angela Lynn Marquart , John Joseph Masters , David Mendel , Gerald Floyd Smith , Philip Parker Waid , Michael Robert Wiley , Ying Kwong Yee
Inventor: David Kent Herron , Sajan Joseph , Angela Lynn Marquart , John Joseph Masters , David Mendel , Gerald Floyd Smith , Philip Parker Waid , Michael Robert Wiley , Ying Kwong Yee
IPC: A61P7/02 , A61K31/55 , C07D243/08
CPC classification number: C07D401/14 , C07D237/24 , C07D403/04
Abstract: 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.
Abstract translation: 本申请涉及本文所定义的式(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。
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公开(公告)号:US06946467B2
公开(公告)日:2005-09-20
申请号:US10030187
申请日:2001-12-06
Applicant: John Walter Liebeschuetz , Christopher William Murray , Stephen Clinton Young , Nicholas Paul Camp , Stuart Donald Jones , William Alexander Wylie , John Joseph Masters , Michael Robert Wiley , Scott Martin Sheehan , David Birenbaum Engel , Brian Morgan Watson , Peter Robert Guzzo , Michael John Mayer
Inventor: John Walter Liebeschuetz , Christopher William Murray , Stephen Clinton Young , Nicholas Paul Camp , Stuart Donald Jones , William Alexander Wylie , John Joseph Masters , Michael Robert Wiley , Scott Martin Sheehan , David Birenbaum Engel , Brian Morgan Watson , Peter Robert Guzzo , Michael John Mayer
IPC: C07D295/16 , A61K31/395 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/501 , A61P1/16 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/02 , A61P19/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D207/12 , C07D207/14 , C07D211/26 , C07D211/46 , C07D211/58 , C07D213/36 , C07D213/38 , C07D213/56 , C07D213/74 , C07D231/56 , C07D277/64 , C07D295/18 , C07D295/185 , C07D309/14 , C07D309/32 , C07D309/34 , C07D335/02 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D417/12 , C07D417/14 , C07D521/00
CPC classification number: C07D295/185 , C07D207/12 , C07D207/14 , C07D211/26 , C07D211/46 , C07D213/36 , C07D213/56 , C07D231/12 , C07D233/56 , C07D249/08 , C07D309/34 , C07D335/02 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D417/12 , C07D417/14
Abstract: The compound 1-(indole-6-carbonyl-D-phenylglycinyl)-4-(1-methylpiperidin-4-yl)piperazine and physiologically-tolerable salts thereof are factor Xa inhibitors useful for the treatment of thrombotic disorders.
Abstract translation: 化合物1-(吲哚-6-羰基-D-苯基甘氨酰基)-4-(1-甲基哌啶-4-基)哌嗪及其生理上可耐受的盐是可用于治疗血栓形成障碍的因子Xa抑制剂。
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公开(公告)号:US06855715B1
公开(公告)日:2005-02-15
申请号:US09926712
申请日:2000-06-13
Applicant: John Walter Liebeschuetz , Amanda Jane Lyons , Christopher William Murray , Andrew David Rimmer , Stephen Clinton Young , Nicholas Paul Camp , Stuart Donald Jones , Phillip John Morgan , Simon James Richards , William Alexander Wylie , John Joseph Masters , Michael Robert Wiley
Inventor: John Walter Liebeschuetz , Amanda Jane Lyons , Christopher William Murray , Andrew David Rimmer , Stephen Clinton Young , Nicholas Paul Camp , Stuart Donald Jones , Phillip John Morgan , Simon James Richards , William Alexander Wylie , John Joseph Masters , Michael Robert Wiley
IPC: C07D295/16 , A61K31/166 , A61K31/40 , A61K31/4025 , A61K31/433 , A61K31/4439 , A61K31/445 , A61K31/4525 , A61K31/454 , A61K31/4545 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/497 , A61P1/16 , A61P7/00 , A61P7/02 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/06 , A61P19/02 , A61P35/00 , A61P43/00 , C07C237/22 , C07C237/36 , C07C255/60 , C07D207/12 , C07D209/08 , C07D209/30 , C07D209/34 , C07D209/42 , C07D211/00 , C07D211/26 , C07D211/30 , C07D211/34 , C07D211/46 , C07D211/60 , C07D213/53 , C07D213/72 , C07D213/74 , C07D213/82 , C07D215/38 , C07D217/02 , C07D217/04 , C07D217/06 , C07D231/56 , C07D235/06 , C07D235/08 , C07D241/24 , C07D277/28 , C07D277/46 , C07D277/64 , C07D277/82 , C07D295/135 , C07D295/185 , C07D317/68 , C07D333/24 , C07D333/38 , C07D333/68 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D487/04 , C07D241/04
CPC classification number: C07D401/14 , C07C237/36 , C07C255/60 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07D209/08 , C07D209/30 , C07D209/34 , C07D209/42 , C07D211/26 , C07D211/34 , C07D211/46 , C07D211/60 , C07D213/53 , C07D213/74 , C07D213/82 , C07D215/38 , C07D217/04 , C07D217/06 , C07D231/56 , C07D235/06 , C07D241/24 , C07D277/28 , C07D277/46 , C07D277/64 , C07D277/82 , C07D295/135 , C07D295/185 , C07D317/68 , C07D333/38 , C07D333/68 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/14 , C07D413/14 , C07D417/06 , C07D487/04
Abstract: Compounds of formula (I) where R2, each X, L, Y, Cy, Lp, D and n are as defined in the specification, are serine protease inhibitors useful as antithrombotic agents.
Abstract translation: 其中R2,X,L,Y,Cy,Lp,D和n如说明书中所定义的式(I)化合物是用作抗血栓形成剂的丝氨酸蛋白酶抑制剂。
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公开(公告)号:US06583173B2
公开(公告)日:2003-06-24
申请号:US09967054
申请日:2001-09-28
Applicant: 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
Inventor: 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: A61K31381
CPC classification number: C07D213/75 , A61K31/44 , C07D209/42 , C07D333/38
Abstract: 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.
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公开(公告)号:US06372759B1
公开(公告)日:2002-04-16
申请号:US09445969
申请日:2000-03-20
Applicant: Douglas Wade Beight , Trelia Joyce Craft , Jeffry Bernard Franciskovich , Theodore Goodson , 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
Inventor: Douglas Wade Beight , Trelia Joyce Craft , Jeffry Bernard Franciskovich , Theodore Goodson , 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: A61K314545
CPC classification number: C07D401/14 , C07D209/08 , C07D209/30 , C07D231/56 , C07D235/06 , C07D401/12 , C07D403/12 , C07D409/12
Abstract: 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.
Abstract translation: 本申请涉及式(I)化合物,本文定义的化合物或其前药的药学上可接受的盐,其药物组合物及其作为因子Xa抑制剂的用途,以及其用于其 制剂及其中间体。
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公开(公告)号:US06924296B2
公开(公告)日:2005-08-02
申请号:US10333624
申请日:2001-08-06
Applicant: Douglas Wade Beight , John Joseph Masters , Jason Scott Sawyer , Robert Theodore Shuman , Michael Robert Wiley , Ying Kwong Yee
Inventor: Douglas Wade Beight , John Joseph Masters , Jason Scott Sawyer , Robert Theodore Shuman , Michael Robert Wiley , Ying Kwong Yee
IPC: A61P7/02 , A61P9/10 , C07D401/14 , C07D403/12 , A61K31/445
CPC classification number: C07D401/14 , C07D403/12
Abstract: 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.
Abstract translation: 本申请涉及如本文所定义的式I化合物(或其前体药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,以及用于 其制备方法及其中间体。
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公开(公告)号:US06780878B2
公开(公告)日:2004-08-24
申请号:US10382614
申请日:2003-03-05
Applicant: 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
Inventor: 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: C07D31202
CPC classification number: C07D295/135 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/14
Abstract: 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.
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公开(公告)号:US06716839B2
公开(公告)日:2004-04-06
申请号:US10378108
申请日:2003-02-26
Applicant: 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
Inventor: 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: A61K315377
CPC classification number: C07D295/135 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/14
Abstract: 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.
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