151409-82-4Relevant articles and documents
3, 4 - SUBSTITUTED PIPERIDINE DERIVATIVES AS RENIN INHIBITORS
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Page/Page column 55, (2009/12/27)
The present invention relates to 3,4-substituted piperidinyl - based renin inhibitor compounds bearing at 4-position lsoqumolone and having the Formula (I) : The invention further relates to pharmaceutical compositions containing said compounds, as well a
3, 4 - SUBSTITUTED PIPERIDINE DERIVATIVES AS RENIN INHIBITORS
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Page/Page column 75-76, (2010/01/29)
The present invention relates to 3,4-substituted piperidinyl-based renin inhibitor compounds bearing at 4-position oxopyridine and having the formula (I). The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency.
3,4,(5)-SUBSTITUTED TETRAHVDROPYRIDINES
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Page/Page column 136, (2008/06/13)
Organic Compounds 3,4(,5)-substituted tetrahydropyridine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4(,5)- substituted tetrahydropyridine compound, and/or a method of treatment comprising administering a 3,4(,5)-substituted tetrahydropyridine compound, a method for the manufacture of a 3,4(,5)- substituted tetrahydropyridine compound, and novel intermediates and partial steps for its synthesis. The 3,4(,5)- substituted tetrahydropyridine compounds have the formula I wherein the substituents and symbols are as described in the specification.
N6-Substituted Adenosine Receptor Agonists. Synthesis and Pharmacological Activity as Potent Antinociceptive Agents
Guengoer, Timur,Malabre, Patrice,Teulon, Jean-Marie,Camborde, Francoise,Meignen, Joelle,et al.
, p. 4307 - 4316 (2007/10/02)
Novel N6-(indol-3-yl)alkyl derivatives of adenosine were synthesized.The adenosine receptor affinity and the antinociceptive activity of these compounds were assessed in binding studies and the phenylbenzoquinone-induced writhing test.Most of these analogues exhibited a potent analgesic activity without side effects.Among them, compound 3c (UP 202-32) bound to A1 (Ki = 110 nM) and A2 (Ki = 350 nM) adenosine receptors in a specific manner since it did not interact with many other receptors, especially opioid binding sites.The antinociceptive activity in the phenylbenzoquinone assay (ED50 = 3.3 mg/kg po) was antagonized by 8-cyclopentyltheophylline, suggesting that an adenosinergic mechanism underlies the analgesic activity observed with this compound.The data obtained with these new N6-substituted adenosine receptor agonists emphasize the interest of such compounds in the treatment of pain.