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US 2011/0034438 A1Published application
Structural mimetics of proline-rich peptides and the pharmaceutical use thereof
AssigneeForschungsverbund Berlin E.V.
InventorsRonald Kuehne, Hartmut Oschkinat, Christoph Brockmann, Hans-Guenther Schmalz
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Abstract
The invention relates to compounds of general formula (I), which can be used particularly as structural mimetics of proline-rich peptides and are therefore capable of binding PRM binding domains (proline-rich motif binding domains) of proteins. The invention also relates to the use of said compounds as pharmaceutical active agents and the use of these pharmaceutical active agents for treating bacterial diseases, neurodegenerative diseases and tumours.
Claims26
Compounds according to general formula 1
- with a saturated or unsaturated central seven-membered ring, wherein
- X is O and/or S;
- A, B are ring bridges;
- Y1, Y2 are H, alkyl, fluoroalkyl, aryl and/or heteroaryl;
- Z1, Z2 are H, carbonyl, OH, O-alkyl, O-acyl, NR1R2 with R1 and/or R2=H, alkyl, acyl, sulfonyl, alkyl, acyl, fluoroalkyl, aryl and/or heteroaryl;
- R1 is alkyl, acyl, alkoxycarbonyl, aryloxycarbonyl and/or aminocarbonyl (CONH2, CONHR, CONH peptidyl, (with R));
- R2 is H, alkyl, aryl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aminocarbonyl, aryloxycarbonyl, alkylsulfonyl, arylsulfonyl, aminoacyl and/or peptidyl.
4 more elements
The method of claim 20,
- wherein
- the bacterial diseases are induced by bacteria selected from the group comprising legionellas, streptococci, staphylococci, klebsiellas, Haemophilis influenzae, rickettsiae (typhoid fever), mycobacteria, mycoplasmas, ureaplasmas, neisseriae (meningitis, Waterhouse-Friedrichsen syndrome, gonorrhea), pseudomonads, bordetellas (pertussis), corynebacteria (diphtheria), chlamydiae, campylobacteria (diarrhea), Escherichia coli, proteus, salmonellas, shigellas, yersiniae, vibrions, enterococci, clostridiae, borreliae, Treponema pallidum, brucellas, francisellas and/or Leptospira, particularly listeriae.
The method of claim 20,
- wherein
- the neurodegenerative disease is selected from the group comprising Alzheimer's disease, Parkinson's disease, Huntington's disease and/or amyotrophic lateral sclerosis (ALS).
The method of claim 20,
- wherein
- the viral infectious disease is a hepatitis and/or an HIV disease.
The method of claim 20,
- wherein
- the tumor disease is a carcinoma, a sarcoma, a neuroendocrine tumor, a hemooncologic tumor, a dysontogenetic tumor and/or a mixed tumor.
The method of claim 20,
- wherein
- the tumor disease is selected from the group comprising tumors of the ear-nose-throat region, comprising tumors of the inner nose, nasal sinus, nasopharynx, lips, oral cavity, oropharynx, larynx, hypopharynx, ear, salivary glands, and paragangliomas, tumors of the lungs comprising non-parvicellular bronchial carcinomas, parvicellular bronchial carcinomas, tumors of the mediastinum, tumors of the gastrointestinal tract, comprising tumors of the esophagus, stomach, pancreas, liver, gallbladder and biliary tract, small intestine, colon and rectal carcinomas and anal carcinomas, urogenital tumors comprising tumors of the kidneys, ureter, bladder, prostate gland, urethra, penis and testicles, gynecological tumors comprising tumors of the cervix, vagina, vulva, uterine cancer, malignant trophoblast disease, ovarial carcinoma, tumors of the uterine tube (Tuba Faloppii), tumors of the abdominal cavity, mammary carcinomas, tumors of the endocrine organs, comprising tumors of the thyroid, parathyroid, adrenal cortex, endocrine pancreas tumors, carcinoid tumors and carcinoid syndrome, multiple endocrine neoplasias, bone and soft-tissue sarcomas, mesotheliomas, skin tumors, melanomas comprising cutaneous and intraocular melanomas, tumors of the central nervous system, tumors during infancy, comprising retinoblastoma, Wilms tumor, neurofibromatosis, neuroblastoma, Ewing sarcoma tumor family, rhabdomyosarcoma, lymphomas comprising non-Hodgkin lymphomas, cutaneous T cell lymphomas, primary lymphomas of the central nervous system, Hodgkin's disease, leukemias comprising acute leukemias, chronic myeloid and lymphatic leukemias, plasma cell neoplasms, myelodysplasia syndromes, paraneoplastic syndromes, metastases with unknown primary tumor (CUP syndrome), peritoneal carcinomatosis, immunosuppression-related malignancy comprising AIDS-related malignancy such as Kaposi sarcoma, AIDS-associated lymphomas, AIDS-associated lymphomas of the central nervous system, AIDS-associated Hodgkin's disease and AIDS-associated anogenital tumors, transplantation-related malignancy, metastasized tumors comprising brain metastases, lung metastases, liver metastases, bone metastases, pleural and pericardial metastases, and malignant ascites.
Dependencies are inferred from the claim text.