- METHODS OF TREATING COGNITIVE IMPAIRMENT ASSOCIATED WITH NEURODEGENERATIVE DISEASE
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Provided herein are methods of treating cognitive impairment associated with neurodegenerative disease in a patient by administering to the patient an effective amount of the Compound, or a pharmaceutically acceptable salt thereof.
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Page/Page column 21; 23
(2021/06/11)
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- SPIRO-LACTAM NMDA MODULATORS AND METHODS OF USING SAME
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Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
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Page/Page column 33; 35
(2018/03/28)
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- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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The present invention provides compounds of Formula I : (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 proph
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Page/Page column 34
(2016/05/19)
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- Cs2CO3-Promoted Direct N-Alkylation: Highly Chemoselective Synthesis of N-Alkylated Benzylamines and Anilines
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Herein is described an efficient and chemoselective method for the synthesis of diversely substituted secondary amines in yields up to 98 %. Direct mono-N-alkylation of primary benzylamines and anilines with a wide range of alkyl halides is promoted by a cesium base in the absence of any additive or catalyst. The basicity and solubility of cesium carbonate in anhydrous N,N-dimethylformamide not only enables mono-N-alkylation of primary amines but also suppresses undesired dialkylation of the desired amines.
- Castillo, Juan-Carlos,Orrego-Hernández, Jessica,Portilla, Jaime
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p. 3824 - 3835
(2016/08/20)
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- NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
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The present invention relates to compounds of the formula (I), the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof. In formula I the variables Het, A, X, Y, Z, R1, R2, R3, R4, R5 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
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Page/Page column 77
(2014/09/29)
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- SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
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Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
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Paragraph 0140
(2014/08/19)
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- AKT / PKB INHIBITORS
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The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
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Page/Page column 196
(2011/06/11)
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- Intramolecular Diels-Alder synthesis of 7-aza-α-carboline compounds
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An efficient, versatile, and scalable route for the synthesis of 7-aza-α-carboline compounds is described. The tricyclic system has been prepared from modified pyrazinones using a key intramolecular [4+2] Diels-Alder transformation.
- Wallace, Michael B.,Scorah, Nicholas,Vu, Phong H.,Brown, Jason W.,Stafford, Jeffrey A.,Dong, Qing
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supporting information; experimental part
p. 1739 - 1741
(2010/05/18)
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- A convenient new synthesis of 3-substituted β-lactams formally derived from 1-(aminomethyl)cyclopropanecarboxylic acids
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1,3-Dipolar cycloaddition of N-benzyl-C-(methoxycarbonyl)-nitrone (3a), N-benzyl-C-phenylnitrone (3b), N-benzyl-C-cyanonitrone (3c), N-(p-methoxybenzyl)-C-cyanonitrone (3d), N-phenyl- (3e) and N-(2-pyridyl)-C- methylnitrones (3f) to bicyclopropylidene (2)
- Zanobini, Alessandra,Gensini, Martina,Magull, Joerg,Vidovic, Denis,Kozhushkov, Sergei I.,Brandi, Alberto,De Meijere, Armin
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p. 4158 - 4166
(2007/10/03)
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- Design and synthesis of novel type VI-like β-turn mimetics. Diversity at the i+1 and the i+2 position
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In this paper, a synthetic approach for functionalised 5-aminopiperidinone- 2-carboxylate (APC) systems as non-pro cis-peptide bond containing external β-turn mimics is presented. The scope and limitations of the synthetic method are discussed and the pot
- De Borggraeve, Wim M.,Verbist, Bie M.P.,Rombouts, Frederik J.R.,Pawar, Vijaykumar G.,Smets, Wim J.,Kamoune, Laila,Alen, Jo,Van Der Eycken, Erik V.,Compernolle, Frans,Hoornaert, Georges J.
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p. 11597 - 11612
(2007/10/03)
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- Synthesis of a new series of 2,7-diazaspirononan-1-ones and study of their cholinergic properties
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A new series of substituted 2,7-diazaspirononan-1-ones (1a-l), structurally related to the muscarinic agonist RS-86, has been synthesized and tested for cholinergic properties both in vitro and in vivo.None of the compounds showed significant cholinergic properties at either the central or peripheral level.A possible explanation for the lack of activity is given.Alzheimer's disease / cholinergic system / RS-86 / muscarinic agonists
- Cignarella, G.,Villa, S.,Barlocco, D.
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p. 115 - 120
(2007/10/02)
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- Synthesis of a new series of N-substituted-3-[1-alkyl(aryl)-4- piperidyl]azetidin-2-ones as possible muscarinic agents
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A new series of N-substituted-3-[1-alkyl(aryl)-4-piperidyl]azetidin-2- ones 2a-j structurally related to the previously reported 2,7- diazaspiro[3,5]nonan-1-ones 1 have been synthesized and tested for their activity as muscarinic agents, both in vitro and in vivo. Preliminary pharmacological results showed that compounds 2 are devoid of significant cholinergic properties.
- Cignarella,Villa,Barlocco
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p. 1337 - 1340
(2007/10/02)
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- NEW SHORT STEP SYNTHESIS OF 3-HYDROXYETHYL-4-CYANOAZETIDIN-2-ONE DERIVATIVE: A POTENTIAL PRECURSOR OF THE PENEMS AND THE CARBAPENEMS
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3-Hydroxyethyl-4 cyanoazetidin-2-one derivative was synthesized from (2R,3R)-2,3-epoxybutyric acid in two steps.
- Shiozaki, Masao,Maruyama, Hiroshi,Ishida, Noboru
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p. 1725 - 1726
(2007/10/02)
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