摘要:
The invention relates to poly(ADP-ribose)polymerase (PARP) homologs which have an amino acid sequence which has a) a functional NAD+ binding domain and b) no zinc finger sequence motif of the general formula CX2CXmHX2C in which m is an integral value from 28 or 30, and the X radicals are, independently of one another, any amino acid; and the functional equivalents thereof; nucleic acids coding therefor; antibodies with specificity for the novel protein; pharmaceutical and gene therapy compositions which comprise products according to the invention; methods for the analytical determination of the proteins and nucleic acids according to the invention; methods for identifying effectors or binding partners of the proteins according to the invention; novel PARP effectors; and methods for determining the activity of such effectors.
摘要:
The invention relates to poly(ADP-ribose)polymerase (PARP) homologs which have an amino acid sequence which has a) a functional NAD binding domain and b) no zinc finger sequence motif of the general formula CX2CXmHX2C in which m is an integral value from 28 or 30, and the X radicals are, independently of one another, any amino acid; and the functional equivalents thereof; nucleic acids coding therefor; antibodies with specificity for the novel protein; pharmaceutical and gene therapy compositions which comprise products according to the invention; methods for the analytical determination of the proteins and nucleic acids according to the invention; methods for identifying effectors or binding partners of the proteins according to the invention; novel PARP effectors; and methods for determining the activity of such effectors.
摘要:
The invention relates to novel 2-phenylbenzimidazoles of general formula (I) or (II), wherein the radicals have the meanings cited in the description, and to their tautomeric forms, possible enantiomeric and diastereomeric forms, to their prodrugs, and to possible physiologically compatible salts. The invention also relates to the production of said compounds and to their use.
摘要:
2-Phenylbenzimidazoles and 2-phenylindoles of formula I wherein A is N or CH, R1 is hydrogen or alkyl which optionally carries an OR11 group, R11 is hydrogen or alkyl, R2 is hydrogen, chlorine, fluorine, bromine, iodine, alkyl, nitro, CF3, CN, NR21R22, NH—CO—R23, OR21, R21 and R22 are each hydrogen or alkyl, R23 is hydrogen, alkyl or phenyl, R3 is —(CH2)q—NR31R32, q is 0, 1, 2 or 3, R31 is hydrogen, alkyl, (CH2)rNR33R34, R32 is (CH2)rNR33R34, r is 2, 3, 4, 5 or 6, R33 and R34 are each hydrogen, alkyl or phenylalkyl wherein the phenyl ring is optionally substituted, or R33 and R34 and the nitrogen atom form a 3- to 8-membered ring, R4 is hydrogen, alkyl, chlorine, bromine, fluorine, nitro, cyano, NR41R42, NH—CO—R43, OR41, R41 and R42 are each hydrogen or alkyl, and R43 is alkyl or phenyl, are useful as inhibitors of poly(ADP-ribose)polymerase and for the production of drugs.
摘要:
Compounds of the formula Ia or IB where A is a saturated or monounsaturated heterocyclic, 4 - to 8-membered ring which contains one or two nitrogen atoms, and their tautomeric forms, possible enantiomeric and diastereomeric forms, their prodrugs and possible physiologically tolerated salts are useful as inhibitors of the enzyme poly(ADP-ribose)polymerase.
摘要:
The present invention relates to the use of phthalazine derivatives as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30), to the use as inhibitors of PARP-homologous enzymes and, in particular, these phthalazine derivatives also show a selective inhibition of PARP-homologous enzymes.
摘要:
Compounds of the formula Ia or IB where A is a saturated or monounsaturated heterocyclic, 4- to 8-membered ring which contains one or two nitrogen atoms, and their tautomeric forms, possible enantiomeric and diastereomeric forms, their prodrugs and possible physiologically tolerated salts are useful as inhibitors of the enzyme poly(ADP-ribose)polymerase.
摘要:
The present invention relates to novel indole derivatives, to their preparation and to their use, as inhibitors of the enzyme poly(ADP-ribose)polymerase or PARP (EC 2.4.2.30), for producing drugs.
摘要:
The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs.
摘要:
The invention relates to compounds of the formula I and the tautomeric forms, possible enantiomeric and diasteromeric forms thereof, and prodrugs thereof, and use thereof as PARP inhibitors.