- Development and scale up of a route to cyclohexylhydrazine dimethanesulfonate
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A mild, high-yielding synthesis of cyclohexylhydrazine dimethane-sulfonate has been developed that is suitable for further scale up. The process consists of three chemical steps: condensation of cyclohexanone with tert-butyl carbazate, reduction of the hy
- Connolly, Terrence J.,Crittall, Andrew J.,Ebrahim, Alkarim S.,Ji, Guijun
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- PYRAZOLOPYRIMIDINES AS INHIBITORS OF GLUCOCORTICOID RECEPTOR TRANSLOCATION
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Provided herein are compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of Glucocorticoid Receptor (GR) translocation. Furthermore, the subject compounds and compositions are useful for the treatment of diseases involved in the hypothalamic-pituitary-adrenal (HPA) axis.
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Paragraph 00475
(2016/08/23)
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- INHIBITORS OF BRUTON'S TYROSINE KINASE
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The invention provides novel poly-substituted 5-membered heterocyclic compounds represented by Formula (IV), or a pharmaceutically acceptable salt, solvate, metabolites, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as selective irreversible bruton's tyrosine kinase (Btk) inhibitors and is further useful to treat inflammatory, auto immune diseases associated with aberrant B-cell proliferation such as RA (rheumatoid arthritis) and cancers. This invention also provided the preparation of a medicament using of Formula (IV), and methods of preventing or treating diseases associated with excessive Btk activity in mammals, especially humans. Formula (IV)
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Paragraph 0417
(2014/06/23)
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- Solvent-free synthesis of hydrazones and their subsequent N-alkylation in a Ball-mill
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A large variety of Boc-, Bz-, Ts-, and Fmoc- protected hydrazones were prepared via condensation of an equimolar amount of carbonyl-compound and the corresponding hydrazine using a ball-mill. Hydrazones were always obtained in a quantitative yield and no solvents were used at any step. In a second step, we realized the first solvent-free N-allylation and N-benzylation of these hydrazones.
- Nun, Pierrick,Martin, Charlotte,Martinez, Jean,Lamaty, Frédéric
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supporting information; experimental part
p. 8187 - 8194
(2011/10/31)
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- Catalytic hydrophosphorylation of alkyl- and acylhydrazones
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N-Boc- and N-acylhydrazino phosphonates were obtained for the first time by hydrophos- phorylation of the appropriate hydrazones of aliphatic and aromatic aldehydes and heterocyclic and aliphatic ketones in the presence of [tetra(tert-butyl)phthalocyanine
- Matveeva,Podrugina,Kolesnikova,Prisyazhnoi,Karateev,Zefirov
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experimental part
p. 418 - 424
(2011/02/17)
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- Stereoselective synthesis of cis- or trans-3,5-disubstituted pyrazolidines via pd-catalyzed carboamination reactions: Use of allylic strain to control product stereochemistry through N-substituent manipulation
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The stereoselective synthesis of either trans- or cis-3,5-disubstituted pyrazolidines is accomplished via Pd-catalyzed carboamination reactions of unsaturated hydrazine derivatives. The products are obtained in good yield with up to >20:1 diastereoselectivity. Stereocontrol is achieved by modulating the degree of allylic strain in the transition state for syn-aminopalladation through a simple modification of the substrate N2-substituent. The pyrazolidine products can be further transformed to 3,5-disubstituted pyrazolines via deprotection/oxidation, or to substituted 1,3-diamines via N-N bond cleavage.
- Giampietro, Natalie C.,Wolfe, John P.
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supporting information; experimental part
p. 12907 - 12911
(2009/03/12)
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- Hydrazinopyrimidines as cysteine protease inhibitors
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Substituted heteroaryl nitrile derivatives of Formula I, processes for their preparation, pharmaceutical compositions comprising such compounds and use of the compounds as cysteine protease inhibitors are provided.
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Page/Page column 25
(2008/12/04)
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- Substituted pyrazolopyrimidines
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The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted heterobicyclic pyrimidines of Formula (I): wherein R1, R2, R3, R4, R5, X, W, and ring A are as defined herein; pharmaceutical compositions of substituted heterobicyclic pyrimidines of Formula (I); and their use in the treatment of chronic neurodegenerative diseases, neurotraumatic diseases, depression and/or diabetes. More particularly, the present invention relates to substituted pyrazolopyrimidines of Formula (I).
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Page/Page column 17
(2008/06/13)
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- FUSED HETEROCYCLIC COMPOUNDS
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Certain fused pyrrole- and pyrazole-containing heterocyclic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.
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Page/Page column 150
(2008/06/13)
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- Synthesis, biological evaluation, and structural studies on N1 and C5 substituted cycloalkyl analogues of the pyrazole class of CB1 and CB2 ligands
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A series of N1 and C5 substituted cycloalkyl and C5 4-methylphenyl analogues of the N-(piperidin-1-yl)-4-methyl-1H-pyrazole-3-carboxamide class of cannabinoid ligands were synthesized. The analogues were evaluated for CB1 and CB2 receptor binding affinities and receptor subtype selectivity. The effects of pyrazole substitution on ligand conformation and as such receptor affinities was not readily apparent; therefore, the geometries of the N1 and C5 substituents relative to the pyrazole ring were studied using high field NMR spectroscopy and systematic molecular mechanics geometry searches. An analysis of the relative ring geometries and functional group orientations provides new insight into the structural requirements of the CB1 and CB2 ligand binding pocket.
- Krishnamurthy, Mathangi,Li, Wei,Moore II, Bob M.
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p. 393 - 404
(2007/10/03)
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