公开(公告)号：US07074934B2

公开(公告)日：2006-07-11

申请号：US10296245

申请日：2001-06-12

Applicant: Sarah Elizabeth Lively ,  Bohdan Waszkowycz ,  Martin James Harrison ,  Christopher Neil Farthing ,  Keith Michael Johnson

Inventor： Sarah Elizabeth Lively ,  Bohdan Waszkowycz ,  Martin James Harrison ,  Christopher Neil Farthing ,  Keith Michael Johnson

IPC: C07D211/08 ,  C07D211/20 ,  C07D333/56 ,  C07C233/00 ,  A61K31/445

CPC classification number: C07D417/12 ,  A61K31/165 ,  A61K31/277 ,  A61K31/381 ,  A61K31/426 ,  C07C237/22 ,  C07C255/58 ,  C07C271/22 ,  C07C271/66 ,  C07C2601/08 ,  C07D209/08 ,  C07D209/12 ,  C07D211/26 ,  C07D211/34 ,  C07D211/46 ,  C07D211/60 ,  C07D213/55 ,  C07D215/38 ,  C07D233/24 ,  C07D277/30 ,  C07D277/40 ,  C07D277/46 ,  C07D277/54 ,  C07D277/82 ,  C07D295/135 ,  C07D295/185 ,  C07D307/54 ,  C07D307/81 ,  C07D317/46 ,  C07D317/60 ,  C07D333/38 ,  C07D333/60 ,  C07D333/66 ,  C07D333/68 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D409/06 ,  C07D417/06

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R 2，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。

公开(公告)号：US06262069B1

公开(公告)日：2001-07-17

申请号：US09485677

申请日：2000-02-25

Applicant: John Walter Liebeschuetz ,  William Alexander Wylie ,  Bohdan Waszkowycz ,  Christopher William Murray ,  Andrew David Rimmer ,  Pauline Mary Welsh ,  Stuart Donald Jones ,  Jonathan Michael Ernest Roscoe ,  Stephan Clinton Young ,  Phillip John Morgan ,  Nicholas Paul Camp ,  Andrew Philip Austin Crew

Inventor： John Walter Liebeschuetz ,  William Alexander Wylie ,  Bohdan Waszkowycz ,  Christopher William Murray ,  Andrew David Rimmer ,  Pauline Mary Welsh ,  Stuart Donald Jones ,  Jonathan Michael Ernest Roscoe ,  Stephan Clinton Young ,  Phillip John Morgan ,  Nicholas Paul Camp ,  Andrew Philip Austin Crew

IPC: A61K3147

CPC classification number: C07D401/12 ,  A61K38/00 ,  C07D217/22 ,  C07D217/24 ,  C07D401/14 ,  C07D405/12 ,  C07D409/14 ,  C07K5/0207

Abstract: The invention relates to serine protease inhibitor compounds of fornula (I) where R1 is hydrogen, halo, cyano, nitro or hydroxyl, amino, alkoxy, alkyl amminoalkyl, hydroxyalkyl, thiol, alkylthio, aminosulphonyl alkoxyalkyl, alkoxycarbonyl, acyloxymethoxycabonyl or alkylamino optionally substituted by hydroxy, alkylamino, alkoxy, oxo, aryl, cycloalkyl, amino, halo, cyano, nitro, thiol, alkylthio, alkylsulphonyl, alkylsulphenyl, alkylsulphonamido, alkylaminosulphonyl, haloalkoxy and haloalkyl; R2 is hydrogen, halo, methyl amino, hydroxy, or oxo; and R is X—X—Y(R7)—L—Lp(D)n; wheren each X independently is a C, N, O or S atom or a CO, CR1, C(R1)2 or NR1 group, at least one X being C, CO, CR1 or a C(R1)2 group; Y (the &agr;-atom) is a nitrogen atom or a CR1 group or Y and L taken together form a cyclic group; R7 is a lipophilic group selected from alkyl, alkenyl, mono- or bi-cycloalkyl, aryl, heteroaryl, mono- or bicycloalkylalkyl, mono- or bicycloalkylakenyl, aralkyl, heteroaryl-alkyl, arylalkenyl, heteroarylalkenyl all optionally substituted by a group R1; L is an organic linker group containing 1 to 5 backbone atoms selected from C, N, O and S, or a branched alkyl or cyclic group; Lp is a lipophilic organic group selected from alkyl, heterocyclic, alkenyl, alkaryl cycloalkyl, polycycloalkyl, cycloalkenyl, aryl, aralkyl or haloalkyl group or a combination of two or more such groups optionally substituted by one or more of oxa, thia, aza or R1 groups; D is a hydrogen bond donor group; and n is 0, 1 or 2 and salts thereof.