- QUINOLINE DERIVATIVES AS SMO INHIBITORS
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Disclosed are quinoline derivatives as hedgehog pathway inhibitors, especially as SMO inhibitors. Compounds of the present invention can be used in treating diseases relating to hedgehog pathway including cancer.
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- COMPOUNDS FOR REGULATING FAK AND/OR SRC PATHWAYS
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The present application provides novel optionally substituted fused pyridine and pyrimidine bicyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating FAK and/or Src activity by administering a therapeutically effective amount of one or more of the compounds to a subject. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the FAK and/or Src pathway. Advantageously, these compounds perform as dual FAK and/or Src inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.
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- Composition Comprising An NK-1 Receptor Antagonist And An SSRI For The Treatment Of Tinnitus And Hearing Loss
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The present invention relates to methods for treating a subject suffering from tinnitus, hearing loss, or tinnitus and hearing loss comprising administering to the subject an effective amount of an NK1 receptor antagonist alone, or in combination with an
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- Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs
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Structure-activity relationships on two novel potent cognition enhancing drugs, unifiram (DM232, 1) and sunifiram (DM235, 2), are reported. Although none of the compounds synthesised reached the potency of the parent drugs, some fairly active compounds have been identified that may represent new leads to develop other cognition enhancing drugs. An interesting result of this research is the identification of two compounds (13 and 14) that are endowed with amnesing activity (the opposite of the activity of the original molecules) and are nearly equipotent to scopolamine. Moreover, two compounds of the series (5 and 6) were found endowed with analgesic activity on a rat model of neuropathic pain at the dose of 1 mg/kg.
- Scapecchi, Serena,Martini, Elisabetta,Manetti, Dina,Ghelardini, Carla,Martelli, Cecilia,Dei, Silvia,Galeotti, Nicoletta,Guandalini, Luca,Romanelli, Maria Novella,Teodori, Elisabetta
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- Design, synthesis, and preliminary pharmacological evaluation of 1,4- diazabicyclo[4.3.0]nonan-9-ones as a new class of highly potent nootropic agents
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Several 4-substituted 1,4-diazabicyclo[4.3.0]nonan-9-ones have been synthesized and tested in vivo on mouse passive avoidance test, to evaluate their nootropic activity. The results show that they represent a new class of nootropic drugs with a pharmacolo
- Manetti, Dina,Ghelardini, Carla,Bartolini, Alessandro,Bellucci, Cristina,Dei, Silvia,Galeotti, Nicoletta,Gualtieri, Fulvio,Romanelli, Maria Novella,Scapecchi, Serena,Teodori, Elisabetta
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p. 1969 - 1974
(2007/10/03)
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- Dual antagonists of platelet activating factor and histamine. Part 3. Synthesis, biological activity and conformational implications of substituted N-acyl-bis-arylcycloheptapiperazines
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A series of N-acyl-4-(5,6-dihydro-11-H-benzo[5,6]cyclohepta[1,2- b]pyridin-11-ylidene)piperazines is described that are dual antagonists of PAF and histamine. The structural requirements for activity in this series parallel those of their previously reported piperidinylidene counterparts. Whereas their global minimum energy conformations are different for both series of compounds, computer assisted molecular modeling suggests that a common bioactive conformation is possible.
- Piwinski, John J.,Wong, Jesse K.,Green, Michael J.,Kaminski, James J.,Colizzo, Frank,Albanese, Margaret M.,Ganguly, Ashit K.,Billah, M. Motasim,Anthes, John C.,West Jr., Robert E.
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p. 3469 - 3474
(2007/10/03)
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