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    2.
    发明专利
    未知

    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.

    5.
    发明专利
    未知

    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.

    Pyrrolo[2,3-d]pyrimidine derivatives useful as tyrosine kinase inhibitors
    7.
    发明专利
    Pyrrolo[2,3-d]pyrimidine derivatives useful as tyrosine kinase inhibitors 未知

    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.

    9.
    发明专利
    未知

    公开(公告)号：ID24653A

    公开(公告)日：2000-07-27

    申请号：ID991048

    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.

    PYRROLO[2,3-D]PYRIMIDINES AND THEIR APPLICATION AS TYROSINE KINASE INHIBITORS
    10.
    发明专利
    PYRROLO[2,3-D]PYRIMIDINES AND THEIR APPLICATION AS TYROSINE KINASE INHIBITORS 未知

    公开(公告)号：BG103785A

    公开(公告)日：2000-06-30

    申请号：BG10378599

    申请日：1999-10-07

    Applicant: BASF AG

    Inventor： CALDERWOOD DAVID J ,  JOHNSTON DAVID N ,  RAFFERTY PAUL ,  TWIGGER HELEN L ,  MUNSCHAUER RAINER ,  ARNOLD LEE

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

    Abstract: The compounds are useful for the treatment of proliferative diseases and diseases of the immune system in mammals, including their pharmaceutically acceptable salts. The compounds have the formula where R1 means hydrogen, 2-phenyl-1,3-dioxan-5-yl, C1-6-alkyl group, C3-8-cycloalkyl group, C5-7-cycloalkenyl group or (optionally substituted phenyl) C1-6-alkyl where the alkyl, cycloalkyl and cycloalkenyl group are optionally substituted by one or more groups with the formula ORA where RA means hydrogen or C1-6-alkyl group provided that the group with formula ORA is not positioned at the carbon atom adjuncted to the nitrogen; R2 means hydrogen, C1-6-alkyl group, C3-8-cycloalkyl group, halogen, hydroxy (optionally substituted phenyl)-C1-6-alkyl, optionally substituted phenyl or R4; and R3 means a group with formula (a) where the phenyl ring is optionally additionally substituted and A means NH, O, NHSO2, SO2NH, C1-4-alkylen residue, NHCO, NHCO2, CONH, NHCONH, CO2 or S(O)p where p has the value of 0,1 or 2, or A is absent and R5 is adjuncted directly to the phenyl ring; and R5 optionally means substituted phenyl, and in addition when A is absent, then R5 means phthalimidogroup optionally substituted with halogen, or pyrazolylaminogroup where the pyrazol ring is optionally substituted with one or more of the following groups: hydroxy or optionally substituted phenyl; R4 is heterocyclic group. The invention also relates to methods for the preparation of these compounds and pharmaceutical compositions containing them. 30 claims

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