cas 91419-49-7, 1-N-Boc-piperidine-3-carboxamide

Articles about 91419-49-7Total 13 be found

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General Ser/Thr Kinases Pharmacophore Approach for Selective Kinase Inhibitors Search as Exemplified by Design of Potent and Selective Aurora A Inhibitors
A general pharmachophore model for various types of Ser/Thr kinases was developed. Search for the molecules fitting to this pharmacophore among ASINEX proprietary library revealed a number of compounds, which were tested and appeared to possess some activity against several Ser/Thr kinases such as Aurora A, Aurora B and Haspin. The possibility of performing the fine-tuning of the general Ser/Thr pharmacophore to desired types of kinase to get active and selective inhibitors was exemplified by Aurora A kinase. As a result, several hits in 3–5?nm range of activity against Aurora A kinase with rather good selectivity and ADME properties were obtained.
Vasilevich, Natalya I.,Aksenova, Elena A.,Kazyulkin, Denis N.,Afanasyev, Ilya I.
p. 54 - 65
(2016/07/09)

MK2 INHIBITORS AND USES THEREOF
The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 00605

(2014/10/03)

Carbazole inhibitors of histamine receptors for the treatment of disease
The present invention relates to carbazole compounds, pharmaceutical compositions comprising them, and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
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Page/Page column 37-38

(2012/01/04)

BRUTON'S TYROSINE KINASE INHIBITORS
The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
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Page/Page column 112; 113

(2011/04/14)

Substituted Oxadiazole Derivatives as Positive Allosteric Modulators of Metabotropic Glutamate Receptors
The present invention relates to new compounds which are Oxadiazole derivatives of formula (I) wherein B, P, Q, W, R1 and R2 are defined in the description. Invention compounds are useful in the prevention or treatment of central or peripheral nervous system disorders as well as other disorders modulated by mGluR5 receptors.(I).
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Page/Page column 11

(2009/09/07)

Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers
A series of 2-oxopiperazine, 4-aminomethyl-, 3-amino- and 3-aminomethylpiperidine analogues of DM235 (sunifiram) and MN19 (sapunifiram), two previously reported potent cognition-enhancers, have been synthesized and tested in the mouse passive-avoidance test. The compounds display minimal effective doses in the range 0.3-10 mg/kg. Although the new substances do not show improved activity when compared to the parent compounds, some useful information has been obtained to understand structure-activity relationships. In addition, the 3-aminopiperidine moiety appears to be a promising scaffold to synthesize new drugs endowed with cognition-enhancing activity.
Martini, Elisabetta,Ghelardini, Carla,Dei, Silvia,Guandalini, Luca,Manetti, Dina,Melchiorre, Michele,Norcini, Monica,Scapecchi, Serena,Teodori, Elisabetta,Romanelli, Maria Novella
p. 1431 - 1443
(2008/09/18)

Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors
Human immunodeficiency virus type-1 (HIV-1) integrase, one of the three constitutive viral enzymes required for replication, is a rational target for chemotherapeutic intervention in the treatment of AIDS that has also recently been confirmed in the clinical setting. We report here on the design and synthesis of N-benzyl-5,6-dihydroxypyrimidine-4-carboxamides as a class of agents which exhibits potent inhibition of the HIV-integrase-catalyzed strand transfer process. In the current study, structural modifications on these molecules were made in order to examine effects on HIV-integrase inhibitory potencies. One of the most interesting compounds for this series is 2-[1-(dimethylamino)-1-methylethyl]-N-(4-fluorobenzyl)-5,6-dihydroxypyrimidine- 4-carboxamide 38, with a CIC95 of 78 nM in the cell-based assay in the presence of serum proteins. The compound has favorable pharmacokinetic properties in preclinical species (rats, dogs, and monkeys) and shows no liabilities in several counterscreening assays, highlighting its potential as a clinically useful antiviral agent.
Pace, Paola,Di Francesco, M. Emilia,Gardelli, Cristina,Harper, Steven,Muraglia, Ester,Nizi, Emanuela,Orvieto, Federica,Petrocchi, Alessia,Poma, Marco,Rowley, Michael,Scarpelli, Rita,Laufer, Ralph,Paz, Odalys Gonzalez,Monteagudo, Edith,Bonelli, Fabio,Hazuda, Daria,Stillmock, Kara A.,Summa, Vincenzo
p. 2225 - 2239
(2007/10/03)

NEW COMPOUNDS
The present invention relates to new compounds of formula (I) wherein Y1 and Y2 selected from the group consisting of hydrogen, halogen atom; C1-4 alkyl, C1-4alkoxy, cyano and trifluoromethyl group, Q is -CH- gr
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Page/Page column 35-36

(2010/11/26)

PHENYL-3-{ (3- (1H- PYRROL- 2 -YL) - [1 , 2 , 4] 0XADIAZ0L-5-YL] PIPERIDIN-1-YL}-METHANONE DERIVATIVES AND RELATED COMPOUNDS AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
The present invention provides new compounds of formula (I) as positive allosteric modulators of metabotropic receptors - subtype 5 ("mGluR5") which are useful for the treatment or prevention of central nervous system disorders such as for example, cognitive decline, both positive and negative symptoms in schizophrenia as well as other central or peripheral nervous system disorders in which the mGluR5 subtype of glutamate metabotropic receptor is involved. The invention is also directed to pharmaceutical compounds and compositions in the prevention or treatment of such diseases in which mGluKi is involved. W represents (C4-C7)cycloalkyl, (C3-C7)heterocycloalkyl , (C3-C7)heterocycloalkyl-(C1-C3)alkyl or (C3-C7)heterocycloalkenyl ring; represents a (C5-C7)heteroeycloalkyl, (C5-C7)heterocycloalkeiiyl ring or a heteroaryl group of formula (a), (b), (c), (d), (e), (f), (g), (i). Q denotes a cycloalkyl, an aryl or heteroaryl group of formula (j), (k), (l), (m), (n). A is azo -N=N-, ethyl, ethenyl, ethynyl, -NR8C(=O)-, -NR8C(=O)-O-, -NR8C(=O)-NR9, NR8S(=O)2-, -C(=O)NR8-, -O-C(=O)NR8-, -S-, -S(=O)-, -S(=O)2-, -S(C=O)2NR8-, -C(=0)-0-, -0-C(=0)-, -C(=NR8)NR9-, C(C=NOR8)NR9- , -NR8C(=NOR9)-, =N-0-, -0-N=CH- or a group aryl or heteroaryl of formula, (o), (p), (q), (r), (s), (t), (u), (v), (w), (x). The other substituents are defined in the claims.
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Page/Page column 34

(2008/06/13)

SUBSTITUTED 3- AND 4- AMINOMETHYLPIPERIDINES FOR USE AS BETA-SECRETASE IN THE TREATMENT OF ALZHEIMER’S DISEASE
The invention relates to novel compounds, which are substituted chiral or achiral derivatives of 3- or 4- aminomethylpiperidine of the general formula (I). The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of general formula (I) and especially their use as inhibitors of beta-secretases for the treatment of Alzheimer’s disease.
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Page/Page column 23; 41

(2008/06/13)

Monocharged inhibitors of mast cell tryptase derived from potent and selective dibasic inhibitors
Truncation of potent and selective dibasic inhibitors afforded monocharged inhibitors of human mast-cell tryptase. Using two classes of analogues as lead structures, several monocharged derivatives were identified with Ki values ranging from 0.
Dener, Jeffrey M,Wang, Vivian R,Rice, Kenneth D,Gangloff, Anthony R,Kuo, Elaine Y.-L,Newcomb, William S,Putnam, Daun,Wong, Martin
p. 2325 - 2330
(2007/10/03)

A MILD EFFICIENT PROCEDURE FOR THE CONVERSION OF CARBOXYLIC ACID ESTERS TO PRIMARY AMIDES USING FORMAMIDE/METHANOLIC SODIUM METHOXIDE
An improved method for the preparation of primary carboxylic acid amides from the corresponding esters is described.This reaction was easily followed by GLC and was usually complete in less than one hour.
Jagdmann, G. Erik,Munson, H. Randall,Gero, Thomas W.
p. 1203 - 1208
(2007/10/02)

Tetrazole analogues of GABA-mimetic agents
Six tetrazole analogues of GABA-mimetic compounds were synthesized. In vitro only two compounds, analogues of GABA and isoguvacine, showed a weak affinity for GABA-A and GABA-B receptors. In vivo compounds were inactive in a psychopharmacological screening in mice. The results were interpreted in terms of intercharge distance, electronic delocalisation and ability of membrane crossing.
Schlewer,Wermuth,Chambon
p. 181 - 186
(2007/10/02)

Chemical Properties

Melting Point: 174.0 to 178.0 °C
Boiling Point: 384.4 °C at 760 mmHg
Flash Point:186.3 °C
Density: 1.123 g/cm³
Solubility:soluble in Methanol
Storage Temp.:Keep in dark place,Inert atmosphere,Room temperature
Vapor Pressure: 4.1E-06mmHg at 25°C
Refractive Index: 1.498
PKA: 16.41±0.20(Predicted)
PSA: 72.63000
LogP: 1.75700

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91419-49-7

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Chemical Properties

Melting Point: 174.0 to 178.0 °C

Boiling Point: 384.4 °C at 760 mmHg

Flash Point:186.3 °C

Density: 1.123 g/cm³

Solubility:soluble in Methanol

Storage Temp.:Keep in dark place,Inert atmosphere,Room temperature

Vapor Pressure: 4.1E-06mmHg at 25°C

Refractive Index: 1.498

PKA: 16.41±0.20(Predicted)

PSA: 72.63000

LogP: 1.75700

Global suppliers and manufacturers of 91419-49-7total 63 suppliers on LookChem

Article Database

91419-49-7

Articles about 91419-49-7Total 13 be found

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Chemical Properties

Melting Point: 174.0 to 178.0 °C

Boiling Point: 384.4 °C at 760 mmHg

Flash Point:186.3 °C

Density: 1.123 g/cm3

Solubility:soluble in Methanol

Storage Temp.:Keep in dark place,Inert atmosphere,Room temperature

Vapor Pressure: 4.1E-06mmHg at 25°C

Refractive Index: 1.498

PKA: 16.41±0.20(Predicted)

PSA: 72.63000

LogP: 1.75700

Global suppliers and manufacturers of 91419-49-7total 63 suppliers on LookChem

Density: 1.123 g/cm³