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    4.
    发明专利
    未知

    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.

    8.
    发明专利
    未知

    公开(公告)号：NO20012218L

    公开(公告)日：2001-06-18

    申请号：NO20012218

    申请日：2001-05-04

    Applicant: BASF AG

    Inventor： ARNOLD LEE DANIEL ,  BOUSQUET PETER F

    IPC: A61K45/00 ,  A61K31/7105 ,  A61K38/00 ,  A61K38/17 ,  A61K38/19 ,  A61K39/395 ,  A61K48/00 ,  A61P1/04 ,  A61P1/16 ,  A61P3/10 ,  A61P7/10 ,  A61P9/00 ,  A61P9/02 ,  A61P9/10 ,  A61P11/06 ,  A61P11/16 ,  A61P13/00 ,  A61P13/02 ,  A61P15/00 ,  A61P17/02 ,  A61P19/00 ,  A61P27/00 ,  A61P27/06 ,  A61P27/12 ,  A61P29/00 ,  A61P35/00 ,  A61P37/08 ,  A61P43/00 ,  C07K14/71

    Abstract: Vascular hyperpermeability and the subsequent events such as macular edema, retinoblastoma, ocular ischemia, ocular inflammatory disease or infection, choroidal melanoma, edematous side-effects induced by iron chelation therapy, pulmonary edema, myocardial infarction, rheumatoid diseases, anaphylaxis, allergies, hypersensitive reactions, cerebral edema, brain tumor fluid-filled cysts, communicating hydrocephalus, carpal tunnel syndrome, organ damage resulting from a burn, irritation or infection, erythema multiforme, edematous macules and other disorders, brain tumors, tumor effusions, lung or breast carcinomas, ascites, pleural effusions, pericardial effusions, high altitude "sickness", radioanaphylaxis, radiodermatitis, glaucoma, conjunctivitis, choroidal melanoma, adult respiratory distress syndrome, asthma, bronchitis, ovarian hyperstimulation syndrome, polycystic ovary syndrome, menstrual swelling, menstrual cramps, stroke, head trauma, cerebral infarct or occlusion, hyotension, ulcerations, sprains, fractures, effusions associated with synovitis, diabetic complications, hyperviscosity syndrome, liver cirrhosis, microalbuminuria, proteinuria, oliguria, electrolyte imbalance, nephrotic syndrome, exudates, fibroses, keloid, can be inhibited by the administration of a compound that inhibits the enzyme activity of the VEGF tyrosine kinase receptor known as KDR tyrosine kinase. The preferred compound 4,5-dihydro-3-pyridin-4-yl-1(2)H-benzo[g]indazole selectively inhibits the function of KDR tyrosine kinase but do not block the activity of Flt-1 tyrosine kinase which is another VEGE tyrosine kinase receptor.

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