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    Amino acid derivatives as endothelin antagonists
    122.
    发明专利
    Amino acid derivatives as endothelin antagonists 未知

    公开(公告)号：NZ319595A

    公开(公告)日：2001-03-30

    申请号：NZ31959596

    申请日：1996-09-26

    Applicant: BASF AG

    Inventor： KLINGE DAGMAR ,  AMBERG WILHELM ,  KLING ANDREAS ,  RIECHERS HARTMUT ,  UNGER LILIANE ,  RASCHACK MANFRED

    IPC: A61K31/00 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/444 ,  A61K31/505 ,  A61K31/53 ,  A61P5/24 ,  A61P5/36 ,  A61P5/42 ,  A61P9/12 ,  C07D213/74 ,  C07D239/10 ,  C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50 ,  C07D239/52 ,  C07D239/58 ,  C07D251/46 ,  C07D401/04 ,  C07D405/12 ,  C07D405/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052 ,  C07D491/056 ,  C07D251/12 ,  C07D403/06

    Abstract: The amino acid derivatives of formula (I) are endothelin antagonists. The compounds may be used in medicaments to treat hypertension, myocardial infarct, angina pectoris, acute kidney failure, renal insufficiency, cerebral vasospasms, cerebral ischemia, subarachnoid hemorrhages, migraine, asthma, atherosclerosis, endotoxic shock, intravascular coagulation, restenosis following angioplasty, benign prostate hyperplasia and ischemic kidney failure. In formula (I); R is COOH or a radical which can be hydrolyzed to COOH; W is nitrogen; R2 is hydrogen, halogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 haloalkoxy, hydroxyl, mercapto, C1-C4-alkylthio, nitro, amino, C1-C4-alkylamino or C1-C4-dialkylamino, cyano, optionally substituted phenyl, or an optionally substituted five-or six-membered heteroaromatic ring which contains from one to three N atoms and/or one S or O; or R2 can furthermore form with the adjacent carbon atom and X, a 5- or 6-membered alkylene or alkylidene ring in which, in each case, one or two carbon atoms can be replaced by a N, S or O hetero atom and which can be mono- to trisubstituted by the following radicals: halogen, nitro, cyano, hydroxyl, mercapto, C1-C3 alkyl, C1-C3 haloalkyl, C1-C3 alkoxy, C1-C3 alkylthio, amino, C1-C3 alkylamino, C1-C3 dialkylamino; R3 can have the same meaning as R2, or furthermore form together with the adjacent carbon atom and Y, an optionally substituted 5- or 6-embered alkylene or alkylidene ring in which, in each case, one or two carbon atoms can be replaced by N, O or S; X is nitrogen or CR15, where R15 is hydrogen or C1-C5-alkyl, C1-C5-alkoxy, C1-C5-alkylthio, nitro, phenyl, hydroxyl, mercapto, halogen, amino, C1-C4-alkylamino, C1-C4-dialkylamino or cyano, or CR15 is linked to R2 to form a 5- or 6-membered ring as described above, or CR15 can form together with R3 and its adjacent carbon atom a 5- or 6-membered ring as described above; Y is nitrogen or CR16, where R16 is the same as R15, or CR16 forms together with R3 and its adjacent carbon atom a 5- or 6-membered ring as described above; R4 is hydrogen, C1-C7-alkyl, C3-C7-cycloalkyl, or optionally substituted phenyl or naphthyl; or R4 can be an optionally substituted 5- or 6-membered heteroaromatic ring which contains one N, O or S atom, or R4 and R5 can be phenyl groups which are connected to each other in the ortho positions by a direct linkage, a methylene, ethylene or ethenylene group, an O or S atom or an SO2, NH or N-alkyl group; R5 is C1-C7-alkyl, C3-C7-cycloalkyl or phenyl or naphthyl which can be substituted by 1 to 3 of the following radicals; halogen, nitro, cyano, hydroxyl, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, phenoxy, phenyl, C1-C4-alkylthio, amino, C1-C4-alkylamino or C1-C4-dialkylamino, or the radicals depicted above; or R5 can be an optionally substituted 5- or 6-membered hetero aromatic ring with one N, S or O heteroatoms; or R5 can form together with R4 a tricyclic system, or R5 can be an optionally substituted phenyl or heteroaromatic radical as described above, which is linked in the ortho position to R8 to form a 6-membered ring where Q must be a single bond and R8 must be a CH-R17 group; R6 is hydrogen or C1-C4-alkyl or C1-C4 haloalkyl; Z is a single bond, O, S, sulfinyl or sulfonyl; R7 is hydrogen, or C1-C4 alkyl, C2-C4-alkenyl, C2-C4-alkynyl; Q is a single bond, a C=O, or C(=O)O group; and R8 is hydrogen, C1-C4-alkyl, C2-C4-alkenyl, phenyl or benzyl, and R8 can furthermore be directly connected to R5 as described above, in which case R8 is a CH-R17 group, where R17 is hydrogen, C1-C4-alkyl, phenyl or phenyl which is mono- to trisubstituted by methoxy, or R8 is a radical as depicted above.

    124.
    发明专利
    未知

    公开(公告)号：NO20010046D0

    公开(公告)日：2001-01-04

    申请号：NO20010046

    申请日：2001-01-04

    Applicant: BASF AG ,  BASF BIORES CORP

    Inventor： RITTER KURT ,  JANSSEN BERND ,  HAUPT ANDREAS ,  KLING ANDREAS ,  BARLOZZARI TERESA ,  AMBERG WILHELM

    IPC: A61K38/00 ,  A61K35/56 ,  A61P35/00 ,  C07K5/103 ,  C07K5/117 ,  C07K7/02 ,  C07K

    Abstract: Compounds of the present invention include cell growth inhibitors which are peptides of Formula IA-B-D-E-F-G(I)and acid salts thereof, wherein A, D, and E are alpha -amino acid residues, B is an alpha -amino acid residue or an alpha -hydroxy acid residue, F is an aminobenzoic acid residue or an aminocycloalkanecarboxylic acid residue, and G is a monovalent radical, such as, for example, a hydrogen atom, an amino group, an alkyl group, an alkylene alkyl ether, an alkylene alkyl thioether, an alkylene aldehyde, an alkylene amide, a beta -hydroxylamino group, a hydrazido group, an alkoxy group, a thioalkoxy group, an aminoxy group, an oximato group, an alkylene aryl group, an alkylene ester, an alkylene sulfoxide or an alkylene sulfone. Another aspect of the present invention includes pharmaceutical compositions comprising a compound of Formula I and a pharmaceutically acceptable carrier. An additional embodiment of the present invention is a method for treating cancer in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound of Formula I in a pharmaceutically acceptable composition.

    DOLASTATINE 15 DERIVATIVES
    125.
    发明专利
    DOLASTATINE 15 DERIVATIVES 未知

    公开(公告)号：BG104089A

    公开(公告)日：2000-12-29

    申请号：BG10408900

    申请日：2000-01-17

    Applicant: BASF AG

    Inventor： JANSSEN BERND ,  BARLOZZARI TEREZA ,  HAUPT ANDREAS ,  ZIERKE THOMAS ,  KLING ANDREAS

    IPC: A61K38/00 ,  A61K38/08 ,  A61P35/00 ,  C07K7/06 ,  C12P19/34

    Abstract: The invention relates to inhibitors of the cellular growth and to their adjunctive to acid salts which are peptides with the formula A - B - D - E - F - (G)r - (K)s - L (I) where A, B, D, E, F, G. and K are -aminoacid residues and s and r are, individually, 0 or 1. L is univalent radical, such as aminogroup, N-substituted aminogroup, beta-hydroxyaminogroup, beta-hydroxyaminogroup, hydrasidogroup, alkoxygroup, thioalkoxygroup, aminooxygroup or oximatogroup. The invention also relates to a method for the treatment of cancer in mammals, including humans which includes the administration of an effective quantity of the above compound in a pharmaceutically acceptable composition. 6 claims

    129.
    发明专利
    未知

    公开(公告)号：NO20004075L

    公开(公告)日：2000-08-15

    申请号：NO20004075

    申请日：2000-08-15

    Applicant: BASF AG

    Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  HERGENROEDER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

    IPC: A61K31/505 ,  A61K31/506 ,  A61P5/14 ,  A61P9/02 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/46 ,  C07D239/52 ,  C07D239/60 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

    Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein the substituents have the following meanings; R = tetrazole or a group (1); R = a radical OR (2), (3), a 5-membe red heteroaromatic bonded by a nitrogen atom such a pyrrolyl, pyrazolyl, imidazolyl and trizolyl; R , R = hydrogen, hydroxy, NH2, NH(C1-C4-alkyl), N(C1-C4-alkyl)2, halogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkinyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy, C1-C4-halogen alkyl, C1-C4-alkoxy, C1-C4-halogen alkoxy or C1-C4-alkythio; X = halogen, C1-C4-halogen alkyl, hydroxy; R and R = phenyl or naphthyl, C3-C7-cycloalkyl, phenyl or naphthyl which are bonded in ortho position by a direct bond, a methylene, ethylene or ethenylene group, an oxygen or sulfur atom or an SO2-NH or an N-alkyl group or a 5-membered or 6-membered heteroaromatic; R = hydrogen, phenyl or naphthyl, a five or six-membered heteroaromatic, C1-C8-alkyl, C3-C6-alkenyl, C3-C6-alkinyl or C3-C8-cycloalkyl, whereby said radicals can be substituted once or many times, with the proviso that R can only stand for hydrogen if Z does not represent a single bond; Z = sulfur, oxygen or a single bond, in addition to the physiologically compatible salts and the enantiomeric-pure and diastereomeric-pure forms. The novel compounds are suitable for combating diseases, especially as endothelin antagonists.

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