165893-99-2Relevant academic research and scientific papers
Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists
Rotstein, David M.,Melville, Chris R.,Padilla, Fernando,Cournoyer, Dick,Lee, Eun K.,Lemoine, Remy,Petersen, Ann C.,Setti, Lina Q.,Wanner, Jutta,Chen, Lijing,Filonova, Lubov,Loughhead, David G.,Manka, Jason,Lin, Xiao-Fa,Gleason, Shelley,Sankuratri, Surya,Ji, Changhua,deRosier, Andre,Dioszegi, Marianna,Heilek, Gabrielle,Jekle, Andreas,Berry, Pamela,Mau, Cheng-I,Weller, Paul
scheme or table, p. 3116 - 3119 (2010/10/02)
Starting with a high-throughput screening lead, a novel series of CCR5 antagonists was developed utilizing an information-based approach. Improvement of pharmacokinetic properties for the series was pursued by SAR exploration of the lead template. The synthesis, SAR and biological profiles of the series are described.
Novel pyrrolo (2,3-b)pyridine derivatives, the preparation and the pharmaceutical use thereof in the form of kinase inhibitors
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Page/Page column 50, (2008/06/13)
Novel compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R, R1, R2, R3, R4, R5, and R6 have the meanings given in the description, pharmaceutical compositions comprising said compounds and use thereof as protein kinase inhibit
Rifamycin derivatives
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Page/Page column 25, (2008/06/13)
Novel rifamycin derivatives of formula I (both hydroquinone and corresponding quinone (C1-C4) forms): or their salts, hydrates or prodrugs thereof, wherein: a preferred R comprises hydrogen, acetyl; L is a linker, a preferred linker group elements selected from any combination of 1 to 5 groups shown FIG. 1, provided L is not wherein R1 is H, methyl or alkyl. The inventive compounds exhibit valuable antibiotic properties. Formulations having these compounds can be used in the control or prevention of infectious diseases in mammals, both humans and non-humans. In particular, the compounds exhibit a pronounced antibacterial activity, even against multiresistant strains of microbes.
ANTIBACTERIAL AGENTS
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Page/Page column 21; 33, (2010/10/19)
Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment bacterial infections in mammals, particularly humans, are disclosed herein.
BICYCLIC AND BRIDGED NITROGEN HETEROCYCLES
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Page/Page column 71, (2008/06/13)
Compounds are provided that act as potent modulators of one or more of the CCR1, CCR2 and CCR3 receptors. The compounds are generally fused-, spiro-or bridged-nitrogen heterocycles having an aryl and heteroaryl component and are useful in pharmaceutical compositions, methods for the treatment of CCR1-, CCR2-and/or CCR3-mediated diseases, and as controls in assays for the identification of competitive receptor antagonists for the above chemokine receptors.
PHENYLAMINOPYRIMIDINES AND THEIR USE AS RHO-KINASE INHIBITORS
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Page column 53, (2010/02/06)
The invention relates to the phenylaminopyrimidines of formula (I), wherein A, D, R1, R2, R3 and R4 are defined as in the description. The invention also relates to methods for producing said phenylaminopyrimidines and to their use for producing drugs for the treatment and/or the prophylaxis of diseases, especially cardiovascular diseases.
