公开(公告)号：NZ337529A

公开(公告)日：2000-10-27

申请号：NZ33752998

申请日：1998-03-09

Applicant: BASF AG

Inventor： CALDERWOOD DAVID JOHN ,  JOHNSTON DAVID NORMAN ,  RAFFERTY PAUL ,  TWIGGER HELEN LOUISE ,  MUNSCHAUER RAINER ,  ARNOLD LEE

IPC: A61K31/519 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/04 ,  A61K31/505

Abstract: The pyrrolo[2,3-d]pyrimidin-4-ylamine derivatives or pharmaceutically acceptable salts have the formula I wherein: R1 is H, 2-phenyl-1,3-dioxan-5-yl, optionally substituted phenylalkyl or ORA substituted alkyl, cycloalkyl or cycloalkenyl; R2 is H, alkyl, cycloalkyl, halo, hydroxy, R4 or optionally substituted phenylalkyl or phenyl; R3 is an AR5 substituted phenyl that can be further substituted; A is NH, O, NHSO2, SO2NH, alkylene, NHCO, NHCO2, CONH, NHCONH, CO2 or S(O)p or A is absent and R5 is attached directly to the phenyl ring; p is 0 to 2; R5 is optionally substituted phenyl or when A is absent R5 is optionally substituted phthalimido, pyrazolyl or phenyl; R4 is optionally substituted thienyl, benzo(b)thienyl, pyridyl, pyrazolyl, isoxazolyl, thiadiazolyl, indazolyl or oxadiazolyl. A pharmaceutical composition thereof is useful for treating benign and neoplastic proliferative diseases and disorders and disorders of the immune system.

公开(公告)号：TR199902301T2

公开(公告)日：1999-12-21

申请号：TR9902301

申请日：1998-03-09

Applicant: BASF AG

Inventor： CALDERWOOD DAVID JOHN ,  JOHNSTON DAVID NORMAN ,  RAFFERTY PAUL ,  TWIGGER HELEN LOUISE ,  MUNSCHAUER DR RAINER ,  ARNOLD LEE

IPC: A61K31/519 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/04

Abstract: Compounds of formula I including pharmaceutically acceptable salts thereof in which R1 represents hydrogen, 2-phenyl-1,3-dioxan-5-yl, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C5-7 cycloalkenyl group or an (optionally substituted phenyl)C1-6 alkyl group wherein the alkyl, cycloalkyl and cycloalkenyl groups are optionally substituted by one or more groups of formula ORA in which RA represents H or a C1-6 alkyl group provided that a group of formula ORA is not located on the carbon attached to nitrogen; R2 represents hydrogen, a C1-6 alkyl group, a C3-8 cycloalkyl group, halo, hydroxy, an (optionally substituted phenyl)C1-6 alkyl group, optionally substituted phenyl or R4; and R3 represents a group of formula (a) in which the phenyl ring is additionally optionally substituted and A represents NH, O, NHSO2, SO2NH, a C1-4 alkylene chain, NHCO, NHCO2, CONH, NHCONH, CO2 or S(O)p in which p is 0, 1 or 2, or A is absent and R5 is attached directly to the phenyl ring; and R5 represents optionally substituted phenyl and, additionally, when A is absent R5 represents a) a phthalimido group optionally substituted by halo or b) a pyrazolylamino group in which the pyrazole ring is optionally substituted by one or more of the following: hydroxy or optionally substituted phenyl; R4 represents a heterocyclic group; are described which are useful in treating proliferative diseases and disorders of the immune system in mammals. Processes to prepare these compounds and pharmaceutical compositions containing these compound are also described.

公开(公告)号：AU748884B2

公开(公告)日：2002-06-13

申请号：AU6829398

申请日：1998-03-09

Applicant: BASF AG

Inventor： CALDERWOOD DAVID JOHN ,  JOHNSTON DAVID NORMAN ,  RAFFERTY PAUL ,  TWIGGER HELEN LOUISE ,  MUNSCHAUER RAINER ,  ARNOLD LEE

IPC: A61K31/519 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/04 ,  A61K31/505

Abstract: Compounds of formula I including pharmaceutically acceptable salts thereof in which R1 represents hydrogen, 2-phenyl-1,3-dioxan-5-yl, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C5-7 cycloalkenyl group or an (optionally substituted phenyl)C1-6 alkyl group wherein the alkyl, cycloalkyl and cycloalkenyl groups are optionally substituted by one or more groups of formula ORA in which RA represents H or a C1-6 alkyl group provided that a group of formula ORA is not located on the carbon attached to nitrogen; R2 represents hydrogen, a C1-6 alkyl group, a C3-8 cycloalkyl group, halo, hydroxy, an (optionally substituted phenyl)C1-6 alkyl group, optionally substituted phenyl or R4; and R3 represents a group of formula (a) in which the phenyl ring is additionally optionally substituted and A represents NH, O, NHSO2, SO2NH, a C1-4 alkylene chain, NHCO, NHCO2, CONH, NHCONH, CO2 or S(O)p in which p is 0, 1 or 2, or A is absent and R5 is attached directly to the phenyl ring; and R5 represents optionally substituted phenyl and, additionally, when A is absent R5 represents a) a phthalimido group optionally substituted by halo or b) a pyrazolylamino group in which the pyrazole ring is optionally substituted by one or more of the following: hydroxy or optionally substituted phenyl; R4 represents a heterocyclic group; are described which are useful in treating proliferative diseases and disorders of the immune system in mammals. Processes to prepare these compounds and pharmaceutical compositions containing these compound are also described.

公开(公告)号：BR9808281A

公开(公告)日：2000-05-16

申请号：BR9808281

申请日：1998-03-09

Applicant: BASF AG

Inventor： CALDERWOOD DAVID JOHN ,  JOHNSTON DAVID NORMAN ,  RAFFERTY PAUL ,  TWIGGER HELEN LOUISE ,  MUNSCHAUER RAINER ,  ARNOLD LEE

IPC: A61K31/519 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/04

Abstract: Compounds of formula I including pharmaceutically acceptable salts thereof in which R1 represents hydrogen, 2-phenyl-1,3-dioxan-5-yl, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C5-7 cycloalkenyl group or an (optionally substituted phenyl)C1-6 alkyl group wherein the alkyl, cycloalkyl and cycloalkenyl groups are optionally substituted by one or more groups of formula ORA in which RA represents H or a C1-6 alkyl group provided that a group of formula ORA is not located on the carbon attached to nitrogen; R2 represents hydrogen, a C1-6 alkyl group, a C3-8 cycloalkyl group, halo, hydroxy, an (optionally substituted phenyl)C1-6 alkyl group, optionally substituted phenyl or R4; and R3 represents a group of formula (a) in which the phenyl ring is additionally optionally substituted and A represents NH, O, NHSO2, SO2NH, a C1-4 alkylene chain, NHCO, NHCO2, CONH, NHCONH, CO2 or S(O)p in which p is 0, 1 or 2, or A is absent and R5 is attached directly to the phenyl ring; and R5 represents optionally substituted phenyl and, additionally, when A is absent R5 represents a) a phthalimido group optionally substituted by halo or b) a pyrazolylamino group in which the pyrazole ring is optionally substituted by one or more of the following: hydroxy or optionally substituted phenyl; R4 represents a heterocyclic group; are described which are useful in treating proliferative diseases and disorders of the immune system in mammals. Processes to prepare these compounds and pharmaceutical compositions containing these compound are also described.

公开(公告)号：PL335685A1

公开(公告)日：2000-05-08

申请号：PL33568598

申请日：1998-03-09

Applicant: BASF AG

Inventor： CALDERWOOD DAVID JOHN ,  JOHNSTON DAVID NORMAN ,  RAFFERTY PAUL ,  TWIGGER HELEN LOUISE ,  MUNSCHAUER RAINER ,  ARNOLD LEE

IPC: A61K31/519 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/04 ,  A61K31/505

Abstract: Compounds of formula I including pharmaceutically acceptable salts thereof in which R1 represents hydrogen, 2-phenyl-1,3-dioxan-5-yl, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C5-7 cycloalkenyl group or an (optionally substituted phenyl)C1-6 alkyl group wherein the alkyl, cycloalkyl and cycloalkenyl groups are optionally substituted by one or more groups of formula ORA in which RA represents H or a C1-6 alkyl group provided that a group of formula ORA is not located on the carbon attached to nitrogen; R2 represents hydrogen, a C1-6 alkyl group, a C3-8 cycloalkyl group, halo, hydroxy, an (optionally substituted phenyl)C1-6 alkyl group, optionally substituted phenyl or R4; and R3 represents a group of formula (a) in which the phenyl ring is additionally optionally substituted and A represents NH, O, NHSO2, SO2NH, a C1-4 alkylene chain, NHCO, NHCO2, CONH, NHCONH, CO2 or S(O)p in which p is 0, 1 or 2, or A is absent and R5 is attached directly to the phenyl ring; and R5 represents optionally substituted phenyl and, additionally, when A is absent R5 represents a) a phthalimido group optionally substituted by halo or b) a pyrazolylamino group in which the pyrazole ring is optionally substituted by one or more of the following: hydroxy or optionally substituted phenyl; R4 represents a heterocyclic group; are described which are useful in treating proliferative diseases and disorders of the immune system in mammals. Processes to prepare these compounds and pharmaceutical compositions containing these compound are also described.

公开(公告)号：CA2283961A1

公开(公告)日：1998-09-24

申请号：CA2283961

申请日：1998-03-09

Applicant: BASF AG

Inventor： JOHNSTON DAVID NORMAN ,  CALDERWOOD DAVID JOHN ,  MUNSCHAUER RAINER ,  ARNOLD LEE ,  TWIGGER HELEN LOUISE ,  RAFFERTY PAUL

IPC: A61K31/519 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/04 ,  A61K31/505

Abstract: Compounds of formula (I) including pharmaceutically acceptable salts thereof in which R1 represents hydrogen, 2-phenyl-1,3-dioxan-5-yl, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C5-7 cycloalkenyl group or an (optionally substituted phenyl) C1-6 alkyl group wherein the alkyl, cycloalkyl and cycloalkenyl groups are optionally substitued by one or more groups of the formula ORA in which RA represents H or a C1-6 alkyl group provided that a group of the formula ORA is not located on the carbon attached to nitrogen; R2 represents hydrogen, a C1-6 alkyl group, a C3-8 cycloalkyl group, halo, hydroxy, an (optionally substituted phenyl) C1-6 alkyl group, optionally substituted phenyl or R4; and R3 represents a group of formula (a) in which the phenyl ring is additionally optionally substituted and A represents NH, O, NHSO2, SO2NH, a C1-4 alkylene chain, NHCO, NHCO2, CONH, NHCONH, CO2 or S(O)p in which p is 0, 1 or 2, or A is absent and R5 is attached directly to the phenyl ring; and R5 represents optionally substituted phenyl and, additionally, when A is absent R 5 represents a) a phthalimido group optionally substituted by halo or b) a pyrazolylamino group in which the pyrazole ring is optionally substituted by one or more of the following: hydroxy or optionally substituted phenyl; R4 represents a heterocyclic group; are described which are useful in treating proliferative diseases and disorders of the immune system in mammals. Processes to prepare these compounds and pharmaceutical compositions containing these compounds are also described.

公开(公告)号：AT242245T

公开(公告)日：2003-06-15

申请号：AT98913690

申请日：1998-03-09

Applicant: BASF AG

Inventor： CALDERWOOD DAVID JOHN ,  JOHNSTON DAVID NORMAN ,  RAFFERTY PAUL ,  TWIGGER HELEN LOUISE ,  MUNSCHAUER RAINER ,  ARNOLD LEE

IPC: A61K31/519 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/04 ,  A61K31/505 ,  C07D239/00 ,  C07D209/00

Abstract: Compounds of formula I including pharmaceutically acceptable salts thereof in which R1 represents hydrogen, 2-phenyl-1,3-dioxan-5-yl, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C5-7 cycloalkenyl group or an (optionally substituted phenyl)C1-6 alkyl group wherein the alkyl, cycloalkyl and cycloalkenyl groups are optionally substituted by one or more groups of formula ORA in which RA represents H or a C1-6 alkyl group provided that a group of formula ORA is not located on the carbon attached to nitrogen; R2 represents hydrogen, a C1-6 alkyl group, a C3-8 cycloalkyl group, halo, hydroxy, an (optionally substituted phenyl)C1-6 alkyl group, optionally substituted phenyl or R4; and R3 represents a group of formula (a) in which the phenyl ring is additionally optionally substituted and A represents NH, O, NHSO2, SO2NH, a C1-4 alkylene chain, NHCO, NHCO2, CONH, NHCONH, CO2 or S(O)p in which p is 0, 1 or 2, or A is absent and R5 is attached directly to the phenyl ring; and R5 represents optionally substituted phenyl and, additionally, when A is absent R5 represents a) a phthalimido group optionally substituted by halo or b) a pyrazolylamino group in which the pyrazole ring is optionally substituted by one or more of the following: hydroxy or optionally substituted phenyl; R4 represents a heterocyclic group; are described which are useful in treating proliferative diseases and disorders of the immune system in mammals. Processes to prepare these compounds and pharmaceutical compositions containing these compound are also described.

公开(公告)号：NO313962B1

公开(公告)日：2003-01-06

申请号：NO994509

申请日：1999-09-17

Applicant: BASF AG

Inventor： CALDERWOOD DAVID JOHN ,  JOHNSTON DAVID NORMAN ,  RAFFERTY PAUL ,  TWIGGER HELEN LOUISE ,  MUNSCHAUER RAINER ,  ARNOLD LEE DANIEL

IPC: A61K31/519 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/04 ,  A61K31/505

Abstract: Compounds of formula I including pharmaceutically acceptable salts thereof in which R1 represents hydrogen, 2-phenyl-1,3-dioxan-5-yl, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C5-7 cycloalkenyl group or an (optionally substituted phenyl)C1-6 alkyl group wherein the alkyl, cycloalkyl and cycloalkenyl groups are optionally substituted by one or more groups of formula ORA in which RA represents H or a C1-6 alkyl group provided that a group of formula ORA is not located on the carbon attached to nitrogen; R2 represents hydrogen, a C1-6 alkyl group, a C3-8 cycloalkyl group, halo, hydroxy, an (optionally substituted phenyl)C1-6 alkyl group, optionally substituted phenyl or R4; and R3 represents a group of formula (a) in which the phenyl ring is additionally optionally substituted and A represents NH, O, NHSO2, SO2NH, a C1-4 alkylene chain, NHCO, NHCO2, CONH, NHCONH, CO2 or S(O)p in which p is 0, 1 or 2, or A is absent and R5 is attached directly to the phenyl ring; and R5 represents optionally substituted phenyl and, additionally, when A is absent R5 represents a) a phthalimido group optionally substituted by halo or b) a pyrazolylamino group in which the pyrazole ring is optionally substituted by one or more of the following: hydroxy or optionally substituted phenyl; R4 represents a heterocyclic group; are described which are useful in treating proliferative diseases and disorders of the immune system in mammals. Processes to prepare these compounds and pharmaceutical compositions containing these compound are also described.

公开(公告)号：NO994509L

公开(公告)日：1999-09-17

申请号：NO994509

申请日：1999-09-17

Applicant: BASF AG

Inventor： CALDERWOOD DAVID JOHN ,  JOHNSTON DAVID NORMAN ,  RAFFERTY PAUL ,  TWIGGER HELEN LOUISE ,  MUNSCHAUER RAINER ,  ARNOLD LEO

IPC: A61K31/519 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/04 ,  A61K31/505

Abstract: Compounds of formula I including pharmaceutically acceptable salts thereof in which R1 represents hydrogen, 2-phenyl-1,3-dioxan-5-yl, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C5-7 cycloalkenyl group or an (optionally substituted phenyl)C1-6 alkyl group wherein the alkyl, cycloalkyl and cycloalkenyl groups are optionally substituted by one or more groups of formula ORA in which RA represents H or a C1-6 alkyl group provided that a group of formula ORA is not located on the carbon attached to nitrogen; R2 represents hydrogen, a C1-6 alkyl group, a C3-8 cycloalkyl group, halo, hydroxy, an (optionally substituted phenyl)C1-6 alkyl group, optionally substituted phenyl or R4; and R3 represents a group of formula (a) in which the phenyl ring is additionally optionally substituted and A represents NH, O, NHSO2, SO2NH, a C1-4 alkylene chain, NHCO, NHCO2, CONH, NHCONH, CO2 or S(O)p in which p is 0, 1 or 2, or A is absent and R5 is attached directly to the phenyl ring; and R5 represents optionally substituted phenyl and, additionally, when A is absent R5 represents a) a phthalimido group optionally substituted by halo or b) a pyrazolylamino group in which the pyrazole ring is optionally substituted by one or more of the following: hydroxy or optionally substituted phenyl; R4 represents a heterocyclic group; are described which are useful in treating proliferative diseases and disorders of the immune system in mammals. Processes to prepare these compounds and pharmaceutical compositions containing these compound are also described.

公开(公告)号：NO994509A

公开(公告)日：1999-09-17

申请号：NO994509

申请日：1999-09-17

Applicant: BASF AG

Inventor： CALDERWOOD DAVID JOHN ,  JOHNSTON DAVID NORMAN ,  RAFFERTY PAUL ,  TWIGGER HELEN LOUISE ,  MUNSCHAUER RAINER ,  ARNOLD LEO

IPC: A61K31/519 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/04 ,  A61K31/505

CPC classification number: C07D487/04