1005397-62-5Relevant articles and documents
4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-3,6-DIHYDROPYRIDINE-1-(2H)-CARBOXAMIDE DERIVATIVES AS LIMK AND/OR ROCK KINASES INHIBITORS FOR USE IN THE TREATMENT OF CANCER
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Paragraph 0157; 0159, (2021/12/07)
The present invention concerns a compound of formula (I), in particular as LIMK and/or ROCK kinases inhibitors. The present invention also concerns these new inhibitors for use for the treatment of a condition selected in the group consisting of: cancers, virion infections, ocular hypertension and glaucoma formation, Neurofibromatosis type 1 and 2, psoriatic lesions, inflammatory diseases and hyperalgesia, central sensitization and chronic pain, reproduction erectile dysfunction, and neuronal diseases. The present description discloses the syntheses and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 32 to 127; examples 1 to 96; families 1 to 8; compounds; biological studies; tables). An exemplary compound is e.g. 4-(5-m ethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-N-phenyl-3,6-dihydropyridine-1-(2H)-carboxamide (example 1; compound 5).
Piperidone derivatives and medical uses thereof
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Page/Page column 12, (2009/04/23)
The present invention relates to compositions comprising 4-Oxo-piperidine-carboxylates and derivatives thereof, for example derivatives substituted with phenyl, nitrophenyl or benzyl groups. It also teaches the medical use of these and related compounds for treatment of retroviral diseases, in particular, HIV and HTLV, proliferative diseases, in particular CML and Trypanosomiasis.
UROTENSIN II RECEPTOR ANTAGONISTS
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Page/Page column 61, (2008/06/13)
The invention is directed to Urotensin II receptor antagonists. More specifically, the present invention relates to certain novel compounds and methods for preparing compounds, compositions, intermediates and derivatives thereof. Pharmaceutical compositio
In search of novel agents for therapy of tropical diseases and human immunodeficiency virus
Goebel, Tim,Ulmer, Daniela,Projahn, Holger,Kloeckner, Jessica,Heller, Eberhard,Glaser, Melanie,Ponte-Sucre, Alicia,Specht, Sabine,Sarite, Salem Ramadan,Hoerauf, Achim,Kaiser, Annette,Hauber, Ilona,Hauber, Joachim,Holzgrabe, Ulrike
, p. 238 - 250 (2008/09/18)
Malaria, sleeping sickness, Chagas' disease, Aleppo boil, and AIDS are among the tropical diseases causing millions of infections and cases of deaths per year because only inefficient chemotherapy is available. Since the targeting of the enzymes of the polyamine pathway may provide novel therapy options, we aimed to inhibit the deoxyhypusine hydroxylase, which is an important step in the biosynthesis of the eukaryotic initiation factor 5A. In order to identify new lead compounds, piperidines were produced and biologically evaluated. The 3,5-diethyl piperidone-3,5-dicarboxylates 11 and 13 substituted with 4-nitrophenyl rings in the 2 and 6 positions were found to be active against Trypanosoma brucei brucei and Plasmodium falciparum combined with low cytotoxicity against macrophages. The corresponding monocarboxylates are only highly active against the T. brucei brucei. The piperidine oximether 53 demonstrated the highest plasmodicidal activity. Moreover, compounds 11 and 53 were also able to inhibit replication of HIV-1.