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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 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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Reference:
Piperidine – Wikipedia,
Piperidine | C5H20152N – PubChem

 

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Further optimization of the biaryl amide series via extensively exploring structure-activity relationships resulted in potent and subtype selective M 1 agonists exemplified by compounds 9a and 9j with good rat PK properties including CNS penetration. Synthesis, structure-activity relationships, subtype selectivity for M1 over M2-5, and DMPK properties of these novel compounds are described.

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Compounds of Formula I and the pharmaceutically acceptable salts thereof are provided as 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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An efficient, one-pot procedure for the Hofmann rearrangement of aromatic and aliphatic amides has been developed. Methyl and benzyl carbamates are produced with N-bromoacetamide in the presence of lithium hydroxide or lithium methoxide, in high yields. beta-Phenylamino amides gave five-membered cyclic ureas stereospecifically. Side products of aryl or benzyl bromination were minimized. This procedure offers an easy access to various protected amines or diamines, which represent important synthetic precursors.

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This invention relates to compounds of formula 1 their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1 , R2 , R3 have meanings given in the description.

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Piperidine – Wikipedia,
Piperidine | C5H20122N – PubChem

 

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The intramolecular nitrile oxide cycloaddition (INOC) reaction is applied to the synthesis of novel isoxazolooxazepinoindazole, benzoisoxazolodiazepinoindazolone, and spiro[isoxazoloazepine]piperidine heterocycles. Each of these targets incorporates a unique trinitrogen-containing triheterocyclic framework. Georg Thieme Verlag Stuttgart · New York.

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Piperidine – Wikipedia,
Piperidine | C5H20180N – PubChem

 

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Urea derivatives which comprise piperidine or piperazine rings and further substitution are effective in ameliorating conditions characterized by unwanted calcium ion channel activity.

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Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III. These compounds are useful for the treatment of HIV and AIDS

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The disclosure generally relates to compounds of formula (I), including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.

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Compounds of formula (I) or (II) can modulate the activity of SIP receptors.

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