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    12.
    发明专利
    未知

    公开(公告)号：ES2164259T3

    公开(公告)日：2002-02-16

    申请号：ES96925746

    申请日：1996-07-12

    Applicant: BASF AG

    Inventor： BUSCHMANN ERNST ,  ZIERKE THOMAS

    IPC: C07C231/02 ,  C07C237/02 ,  C07K1/06 ,  C07K1/08 ,  C07K7/06

    Abstract: PCT No. PCT/EP96/03075 Sec. 371 Date Jan. 20, 1998 Sec. 102(e) Date Jan. 20, 1998 PCT Filed Jul. 12, 1996 PCT Pub. No. WO97/05096 PCT Pub. Date Feb. 13, 1997A process for preparing alpha -(N,N-dialkylamino) carboxamides of the formula I where the substituents have the stated meanings, comprises reacting the corresponding free acids with primary or secondary amines in the presence of anhydrides of an alkanephosphonic acid.

    Dolastatin 15 derivatives
    13.
    发明专利
    Dolastatin 15 derivatives 未知

    公开(公告)号：NZ502296A

    公开(公告)日：2002-02-01

    申请号：NZ50229698

    申请日：1998-07-07

    Applicant: BASF AG

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

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

    Abstract: Compound of formula: A-B-D-E-F-(G)r-(K)s-L wherein: A is a proline derivative of formula IIa, wherein na is O to 3; Ra I hydrogen, or unsubstituted or fluorine-substituted normal, branched or cyclic C1-3-alkyl; R1a is hydrogen, C1-3 -alkyl, phenyl, or substituted phenyl; or Ra and R1a together form a propylene bridge; and R2a, R3a, R4a and R5a are each, independently, hydrogen or alkyl; or an alpha-amino acid derivative of Formula IIIa, Formula IVa, Formula Va, Formula VIa, Formula VIIa, Formula VIIIa, a 2-azabicyclo heptane-3-carboxylic acid derivative of Formula IXa, an amino acid derivative of Formula Xa; B is a valyl, isoleucyl, allo-isoleucyl, norvalyl, 2-tert-butylglycyl or 2-ethylglycyl residue; or an alpha-amino acid residue of Formula IIb; D is an N-alkylvalyl, N-alkyl-2-ethylglycyl, N-alkyl-2-tert-butylglycyl, N-alkylnorleucyl, N-alkylisoleucyl, N-alkyl-allo-isoleucyl or N-alkylnorvalyl residue; or an alpha-amino acid residue of Formula IId, Formula IIId; E is a prolyl, thiazolidinyl-4-carbonyl, homoprolyl, or hydroxyprolyl residue; or an alpha-amino acid residue of Formula IIe; or an aminocyclopentanecarboxylic acid residue of Formula IIIe, wherein Re is alkyl and R1e is hydrogen, or unsubstituted or fluorine-substituted alkyl; F is a prolyl, thiazolidinyl-4-carbonyl, homoprolyl or hydroxyprolyl residue; or an alpha-amino acid residue of Formula IIf; or a 2- or 3-aminocyclopentanecarboxylic acid residue of Formula IIIf; G is an alpha-amino acid residue of Formula IIg; K is an alpha-amino acid of Formula IIk; and L is a substituted or unsubstituted amino, hydrazido, aminoxy or oximato group; and r and s are independently, 0 or 1; provided that when s and r are 0 and A is of formula IIa where na is 0 or 1 and R1a, R2a, R3a, R4a and R5a are each hydrogen, L is a substituted or unsubstituted amino or hydrazido group .

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