Publication number: 20030055246
Abstract: The invention relates to serine protease inhibitor compounds of formula (I) where R1 is hydrogen, halo, cyano, nitro or hydroxyl, amino, alkoxy, alkyl, aminoalkyl, hydroxyalkyl, thiol, alkylthio, aminosulphonyl, alkoxyalkyl, alkoxycarbonyl, acyloxymethoxycarbonyl 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; wherein 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 bicycloalkylalkenyl, aralkyl, heteroaryl-alkyl
Type:
Application
Filed:
February 4, 2002
Publication date:
March 20, 2003
Inventors:
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
Patent number: 6420438
Abstract: The invention relates to serine protease inhibitor compounds of formula (I)
where R1 is hydrogen, halo, cyano, nitro or hydroxyl, amino, alkoxy, alkyl, aminoalkyl, hydroxyalkyl, thiol, alkylthio, aminosulphonyl, alkoxyalkyl, alkoxycarbonyl, acyloxymethoxycarbonyl 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; wherein each X independently is 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 bicycloalkylalkenyl, aralkyl,
Type:
Grant
Filed:
May 29, 2001
Date of Patent:
July 16, 2002
Assignee:
Tularik Limited
Inventors:
John Walter Liebeschuetz, William Alexander Wylie, Bohdan Waszkowycz, Christopher William Murray, Andrew David Rimmer, Pauline Mary Welsh, Stuart Donald Jones, Jonathan Michael Ernest Roscoe, Stephen Clinton Young, Phillip John Morgan, Nicholas Paul Camp, Andrew Philip Austin Crew
Patent number: 6262069
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, heter
Type:
Grant
Filed:
February 25, 2000
Date of Patent:
July 17, 2001
Assignee:
Protherics Molecular Design Limited
Inventors:
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
