- COMPOUNDS AND THEIR USE IN THE TREATMENT OF BACTERIAL INFECTION
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The invention provides novel compounds having the general formula (I) wherein R1, R2, R3a, R3b, R4, A1, A2, A3, A4, A5, A6, B1/s
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- ALLOSTERIC CHROMENONE INHIBITORS OF PHOSPHOINOSITIDE 3-KINASE (PI3K) FOR THE TREATMENT OF DISEASES ASSOCIATED WITH P13K MODULATION
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The disclosure relates to compounds of Formula (I) as allosteric chromenone inhibitors of phosphoinositide 3-kinase (PI3K) useful in the treatment of diseases or disorders associated with PI3K modulation, Formula (I), or a prodrug, solvate, enantiomer, st
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- QUINAZOLINE COMPOUND FOR EGFR INHIBITION
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Disclosed is a novel quinazoline compound. Specifically, disclosed are a compound represented by the formula (I) and a pharmacologically acceptable salt.
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- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
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- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
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- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
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- AUTOTAXIN INHIBITOR COMPOUNDS
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Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with autotaxin activity.
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- Substituted 1-oxa-3,8-diazaspiro[4.5]-decan-2-one-Compounds and the Use Thereof for Producing Drugs
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The present invention relates to substituted 1-oxa-3,8-diazaspiro[4.5]-decan-2-one compounds, to methods for the production thereof, to medicaments containing these compounds and to the use of these compounds for producing medicaments.
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Page/Page column 31
(2009/05/29)
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- NOVEL SPIROPIPERIDINE COMPOUNDS AND METHODS FOR THE MODULATION OF CHEMOKINE RECEPTOR ACTIVITY
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The present invention relates to spiropiperidine compounds of formula (I) wherein W, X, Y, Z, R1, R2 and R3 are as defined herein, and pharmaceutically acceptable salts, hydrates and solvates thereof. These spiropiperidine
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Page/Page column 47-48
(2010/11/27)
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- Inhibitors of prenyl-protein transferase
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The present invention is directed to conformationally constrained compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
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- New Spiropiperidines as Potent and Selective Non-Peptide Tachykinin NK2 Receptor Antagonists
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The synthesis of a series of 2-(5-fluoro-1H-indol-3-yl)ethyl spiropiperidines is described together with their tachykinin NK2 receptor affinities measured in a rat colon binding assay.Equivalent NK2 receptor binding affinity was observed for the spirooxalidinone 3-benzyl-8--1-oxa-3,8-diazaspirodecan-2-one (3a), the imidazolidinone 3-benzyl-8--1,3,8-triazaspirodecan-2-one (3s), and the pyrrolidinone 2-benzyl-8--2,8-diazaspirodecan-3-one (3t).Substitution in the phenyl ring of compound 3a produced no significant enhancement in NK2 binding affinity.Replacement of the phenyl ring in 3a with other aromatic rings resulted in a significant loss in binding affinity.Compound 3a was shown to be a potent NK2 receptor antagonist in guinea pig trachea where it also demonstrated 1000-fold selectivity for NK2 receptors over NK1.In the anesthesized guinea pig, compound 3a administered by the intravenous or oral route displayed potent and long-lasting antagonist activity against NK2 receptor agonist induced bronchoconstriction.
- Smith, Paul W.,Cooper, Anthony W. J.,Bell, Richard,Beresford, Isabel J. M.,Gore, Paul M.,et al.
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p. 3772 - 3779
(2007/10/03)
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