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    Novel carboxylic acid derivatives, their preparation and use in treating cancer
    41.
    发明专利
    Novel carboxylic acid derivatives, their preparation and use in treating cancer 未知

    公开(公告)号：NZ337557A

    公开(公告)日：2001-08-31

    申请号：NZ33755798

    申请日：1998-03-09

    Applicant: BASF AG

    Inventor： ROMERDAHL CYNTHIA A

    IPC: C07D251/30 ,  A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61P35/00 ,  C07D239/60 ,  C07D405/12 ,  C07D409/12

    Abstract: 6-substituted 1,2,4a,5a,8a,8b-hexahydro- and 1,2,3,4,4a,5a,8a,8b-octahydro-6H-pyrrolo[3',4':4,5]furo[3,2-b]pyrid-8 7H -one derivatives of general formula (I) and their salts, in which: R1 is hydrogen or optionally substituted alkyl, cycloalkyl, arylalkyl, aryl, heteroaryl or herarylalkyl; R2 is hydrogen or optionally substituted alkyl, cycloalkyl or alkoxycarbonyl; Or R1 and R2 together with the atoms to which they are attached represent an optionally substituted 5- or 6-membered ring, which may be optionally interrupted by oxygen, sulphur, sulphoxyl or sulphonyl; R3 represents hydrogen or optionally substituted alkyl, cycloalkyl or alkoxycarbonyl; R4 represents hydrogen or optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heraryl, hetarylalkyl, amino, alkylamino, di-alkylamino or cycloalkylamino; A represents hydroxy, alkoxy, alkenyloxy, alkinyloxy, arylalkyloxy, formyloxy, azido, halogen, aryloxy, hetarylalkyloxy, hetaryloxy, mercapto, alkylthio, alkylsulphonyl, alkenylthio, arylalkylsulphonyl, hetarylalkylthio, hetarylalkylsulphonyl, arylthio, arylsulphonyl, alkyl, alkenyl, alkinyl, aryl, arylalkyl, hetaryl, hetarylalkyl, alkoxycarbonyl, -X-G(=Y)-Q, CHR6=C(=O)-R7 OR, -O-B1; X represents oxygen or sulphur; -G(=Y)- represents carbonyl, thiocarbonyl, sulphoxyl, sulphonyl, -P(O)-O-R5 OR -P(S)-O-R5; Q represents alkyl, alkenyl, alkinyl, cycloalkyl, alkoxy, alkenyloxy, alkinyloxy, aryl arylalkyl, cycloalkyoxy, hetaryl, hetarylalkyl, an optionally substituted cyclic amino group which is attached via the nitrogen atom; R5 represents alkyl; R6 represents hydrogen alkyl, alkoxy, arylalkoxy, alkylthio, cycloalkylthio, arylthio, hetarylaIkylthio; R7 represents optionally substituted alkyl, alkenyl, cycloalkyl, alkylthio, arylthio, aryl, arylalkyl, hetaryl or hetarylalkyl; Or R6 and R 7 together with the atoms to which they are attached represent a 5-, 6- or 7-membered carbocyclic ring, which may optionally be substituted, B represents hydrogen or optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, hetaryl, hetarylalkyl, formyl, alkoxydicarbonyl or a radical from the group consisting of B I, B2, B3 and B4 R8 represents hydrogen or optionally substituted, alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl; R8 and R9 together with the atoms to which they are attached represent an optionally substituted 5- or 6-membered ring, which is optionally interrupted by oxygen, sulphur, sulphoxyl or sulphonyl; R9 and R10 each represent hydrogen, alkyl, alkenyl, cycloalkyl or optionally substituted aryl, arylalkyl, hetaryl or hetarylalkyl; Or R9 and R10 together represent an optionally substituted spirocyclic ring; -G1(=Y1)- represents carboxyl, thiocarboxyl, -C=CH-NO2, -C=CH-CN, -C=N-R11, sulphoxyl, sulphonyl, -P(O)-O-R5 or -P(S)-O-R5, R11 represents hydrogen, hydroxyl, alkoxy, alkylcarbonyl, alkoxycarbonyl, halogenoalkylcarbonyl, alkylsulphonyl, nitro or cyano; Q represents optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, aryl, arylalkyl, hetaryl or hetarylalkyl, or a radical selected from the group consisting of G1 and G2; -G2(=Y2)- may represent carboxyl, thiocarboxyl or sulphonyl; Z represents oxygen, sulphur or -NR13; R12 may, if Z is nitrogen, represent a cyclic amino group, which is attached via a nitrogen atom; R12 and R13 independently of one another represent hydrogen or optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, alkoxycarbonyl, aryl, arylalkyl, hetaryl or hetarylalkyl; R12 and R13 together with the adjacent N atom represent an optionally substituted carbocyclic 5-, 6- or 7-membered ring system or represent a 7- to 10-membered bicyclic ring system, which may optionally be interrupted by oxygen, sulphur, sulphoxyl, sulphonyl, carbonyl, -N-O, -N=, -NR15- or by quarternized nitrogen; R14 represents hydrogen or alkyl; R15 represents hydrogen or optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, alkoxycar, alkylcarbonyl, cycloalkylcarbonyl, cyano, aryl, arylalkyl, hetaryl, hetarylalkyl; The dotted line is absent or represents a single bond. The compounds are useful in combatting endoparasites.

    42.
    发明专利
    未知

    公开(公告)号：BR9808263A

    公开(公告)日：2000-05-16

    申请号：BR9808263

    申请日：1998-03-09

    Applicant: BASF AG

    Inventor： ROMERDAHL CYNTHIA A

    IPC: C07D251/30 ,  A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61P35/00 ,  C07D239/60 ,  C07D405/12 ,  C07D409/12

    Abstract: This invention provides a method for treating cancer in an individual, wherein the cancer is a tumor in which endothelin is upregulated (e.g. tumors of the prostate, lung, liver, breast, brain, stomach, colon, endometrium, testicle, thyroid, pituatary, bladder, kidney, pancreas and meninges) by administering to the individual an effective amount of a compound of Formula I or Formula Ia, as describe herein.

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