- Substituted ring compound and its method and use thereof
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The invention provides a substituted cyclic compound as well as a use method and application thereof. The compound is a compound as shown in a formula (I) or stereoisomers, stereomers, tautomers, nitric oxides, solvates, metabolites and pharmaceutically acceptable salts or prodrugs of the compound as shown in the formula (I). The invention further provides a medicament composition containing the compound. The compound and the medicament composition are capable of regulating the activity of protein kinase in a biological sample body and are used for protecting, treating or relieving proliferative diseases of patients. The formula (I) is as shown in the specification.
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- ALDOSTERONE SYNTHASE INHIBITORS
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The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2. R3, R4, R5, R6, R7, W, Y, m and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
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- SUBSTITUTED CYCLIC COMPOUNDS AND METHODS OF USE
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The present invention provides novel substituted alkynyl compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
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- Heterocyclic derivatives as metabotropic glutamate receptor modulators
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The invention relates to heterocyclic derivatives of formula I as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are mGluR5 modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders.
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Paragraph 0230
(2013/11/05)
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- METABOTROPIC GLUTAMATE RECEPTOR MODULATORS
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The invention relates to heterocyclic derivatives of formula (I) as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are mGluR5 modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders wherein Y, W, R1, R2 and R3 are as defined in claim 1.
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Page/Page column 51
(2012/05/05)
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- Synthesis and β-blocking activity of (R,S)-(E)-oximeethers of 2,3-dihydro-1,8-naphthyridine and 2,3-dihydrothiopyrano[2,3-b]pyridine: Identification of β3-antagonists
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Drugs acting on β1- and β2-adrenergic receptors are widely used for the clinical management of a large number of cardiovascular and respiratory pathologies. In the last decade, the discovery of the third subtype of β receptors, the β3-adrenoceptor, gave a further pharmacological target for the development of new selective drugs. Initially, a potential therapeutic use of β3-selective agents seemed to be restricted to agonists, for the treatment of metabolic diseases, such as obesity, non-insulin-dependent diabetes, urinary frequency and incontinence. More recently, some interesting theories about a negative role played by the cardio-depressant activity of myocardial β 3-adrenoceptors in heart failure, seemed to justify a clinical use of β3-antagonists in the last phases of this cardiac disease. Following the indications deriving from previous experimental work, the β-antagonist properties of newly-synthesised (R,S)-(E)-oximeethers of 2,3-dihydro-1,8-naphthyridine and of 2,3-dihydrothiopyrano[2,3-b]pyridine were evaluated, in order to identify some useful structure-activity relationships, which might account for selectivity towards the three β-subtypes and, in particular, the β3-adrenoceptor. Among the various observations regarding possible structure-activity relationships, able to explain the pharmacodynamic patterns of the synthesised compounds on the three subtypes of β-adrenoceptors, the most significant data derived from the evaluation of the β3-blocking properties of some oximeethers of 1,8-naphthyridine derivatives. In these molecules, although the presence of the large substituents in position 7, such as 4-chloro-phenoxy- or 4-t-butyl-phenoxy groups determined a dramatic decline in both the β 1- and β2-activities, this structural characteristic had a modest influence on the β3-affinity, which was only slightly lower. Hence, this last structural requirement of oximeethers of 1,8-naphthyridine derivatives seems to represent a useful expedient to induce an appreciable selectivity towards the β3-receptor, through a markedly negative effect on the β1- and β 2-activities rather than an increase in the β 3-affinity.
- Saccomanni, Giuseppe,Badawneh, Muwaffag,Adinolfi, Barbara,Calderone, Vincenzo,Cavallini, Tiziana,Ferrarini, Pier Luigi,Greco, Rosamiria,Manera, Clementina,Testai, Lara
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p. 4921 - 4931
(2007/10/03)
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