- Preparation of novel azabicyclic amines and α7 nicotinic acetylcholine receptor activity of derived aryl amides
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(Chemical Equation Presented) Three new azabicyclic amines, namely exo-3-amino-1-azabicyclo[3.2.1]octane, 3-amino-1-azabicyclo-[3.2.2]nonane and exo-6-amino-8-azabicyclo[3.2.1]octane, have been designed and prepared as isosteres of 3-aminoquinuclidine. Ar
- Walker, Daniel P.,Acker, Brad A.,Jacobsen, E. Jon,Wishka, Donn G.
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p. 247 - 257
(2008/09/18)
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- SPIRO CONDENSED PIPERIDNES AS MODULATORS OF MUSCARINIC RECEPTORS
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The present invention relates to modulators of muscarnic receptors of formula (I). The present invention also provides impositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
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Page/Page column 50
(2008/06/13)
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- 1H-PYRAZOLE AND 1H-PYRROLE-AZABICYCLIC COMPOUNDS WITH ALFA-7 NACHR ACTIVITY
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The invention provides compounds of Formula (I), wherein Azabicyclo is Formula (I, II, III, IV, V, VI, VII); W is Formula (m); where the variables have the definitions discussed herein. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat a disease or condition in which α7 is known to be involved.
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- COMPOUNDS HAVING BOTH α7 NICOTINIC AGONIST ACTIVITY AND 5HT3 ANTAGONIST ACTIVITY FOR TREATMENT OF CNS DISEASES
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The invention discloses compounds that are selective α7 nAChR agonists and 5-HT3 antagonists. The compounds are useful for treating many CNS diseases.
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- COMPOUNDS AS RADIOLIGANDS FOR THE DIAGNOSIS OF DISEASE
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Radiolabeled ligands useful as probes for determining the relative abundance, receptor occupancy, and/or function of nicotinic acetylcholine receptors. The compounds of Formula I as described herein are labeled with a radioactive isotopic moiety such as 11C, 18F, 76Br, 123I or 125I. Disorders are diagnosed by administering to a mammal a detectably labeled compound and detecting the binding of that compound to the nAChR. The compounds that have been administered are detected using methods including, but not limited to, position emission topography and single-photon to emission computed tomography. The present invention is useful in diagnosing a wide variety of diseases and disorders as discussed herein.
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- Substituted-aryl compounds for treatment of disease
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The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals to treat diseases or conditions in which α7 is known to be involved.
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- Azabicyclic compounds for the treatment of disease
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The invention provides compounds of Formula I: 1wherein Azabicyclo is 2These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals in which α7 is known to be involved.
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- Fused bicyclic-N-bridged-heteroaromatic carboxamides for the treatment of disease
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The invention provides compounds of Formula I: 1These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat conditions or diseases in which α7 is known to be involved.
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- Azabicyclic compounds for the treatment of disease
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The invention provides compounds of Formula I: wherein Azabicyclo is W is a six-membered heterocyclic ring system having 1-2 nitrogen atoms or a 10-membered bicyclic-six-six-fused-ring system having up to two nitrogen atoms within either or both rings, provided that no nitrogen is at a bridge of the bicyclic-six-six-fused-ring system, and further having 1-2 substitutents independently selected from R3. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat diseases or conditions in which α7 is known to be involved.
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- BENZOIC ACID COMPOUNDS AND USE THEREOF AS MEDICAMENTS
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Benzoic acid compounds of the formula STR1 wherein each symbol is as defined in the specification, optical isomers thereof and pharmaceutically acceptable salts thereof; pharmaceutical composition comprising this compound and pharmaceutically acceptable additive; and serotonin 4 receptor agonists, gastrointestinal prokinetic agents and therapeutic agents for various gastrointestinal diseases, which comprise this compound as active ingredient. The compounds of the present invention have high and selective affinity for serotonin 4 receptor, and show agonistic effects thereon. Accordingly, they are useful medications for the prophylaxis and treatment of various gastrointestinal diseases, central nervous disorders, cardiac function disorders, urinary diseases, and the like, as well as useful anti-nociceptors for analgesic use which increase threshold of pain.
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- Enantioselective synthesis of (S)-2-(aminomethyl)butanedioic acid using chiral β-alanine α-enolate equivalents
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(S)-2-(Aminomethyl)butanedioic acid (6) can been synthesised by stereoselective alkylation of the Na enolates of acyloxazolidinones 1a and 1b with methyl bromoacetate, then oxidation of the vinyl or dimethoxyphenyl substituent to a carboxyl group, followed by Curtius rearrangement and deprotection. The absolute configuration of 6 has been correlated with that of (S)-1-phenylethylamine by a combination of crystallographic and chemical means.
- Arvanitis, Elena,Motevalli, Majid,Wyatt, Peter B.
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p. 4277 - 4280
(2007/10/03)
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