- Practical and scalable synthesis of ethyl (R)-piperidine-3-acetate
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A practical and scalable synthesis of ethyl (R)-piperidine-3-acetate was achieved from commercially available 3-pyridylacetic acid in 76% overall yield. The practical synthesis was demonstrated on 100-g scale. One-pot reductive N-ethylation of the pyridinium salt with acetonitrile gave an N-ethyl piperidine derivative. Copyright Taylor & Francis Group, LLC.
- Zhu, Ying-Guang,Kan, Hong-Zhu,Jiang, Li-Qin,Hu, Wen-Hao
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p. 1137 - 1145
(2012/05/05)
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- A SUBSTITUTED PYRIMIDINE AS A PROSTAGLANDIN D2 RECEPTOR ANTAGONIST
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The present invention is directed to a 2,6-substituted-4-monosubstitutedamino-pyrinudine compound of formula (I) as set forth herein, or an enantiomer thereof, or an ester prodrug or a pharmaceutically acceptable salt thereof, or a pharmaceutical composit
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Page/Page column 31; 32
(2011/10/10)
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- Microwave-assisted hydrogenation of pyridines
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Using a commercially available device for controlled introduction of hydrogen in a vial for reactions under microwave dielectric heating, we developed a protocol for the transformation of substituted pyridines into the corresponding piperidines. Complete reduction occurred in 40 minutes, or even less, on substrates that require 24-48 hours to be reduced under standard conditions. Moreover, the reduction proved to be as stereoselective as the corresponding reaction carried out at room temperature. Georg Thieme Verlag Stuttgart.
- Piras, Leonarda,Genesio, Eva,Ghiron, Chiara,Taddei, Maurizio
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body text
p. 1125 - 1128
(2009/04/04)
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- 3-Mercaptopropionic acids as efficacious inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa)
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A novel series of cyclic potent, selective, small molecule, thiol-based inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa) and the crystal structures of TAFIa inhibitors bound to porcine pancreatic carboxypeptidase B are described. Three series of cyclic arginine and lysine mimetic inhibitors vary significantly in their selectivity against other human basic carboxypeptidases, carboxypeptidase N and carboxypeptidase B. (-)2a displays TAFIa IC50 = 3 nM and 600-fold selectivity against CPN. Inhibition of TAFIa with (rac)2a resulted in dose dependent acceleration of human plasma clot lysis in vitro and was efficacious as an adjunct to tPA in an in vivo rabbit jugular vein thrombolysis model.
- Islam, Imadul,Bryant, Judi,May, Karen,Mohan, Raju,Yuan, Shendong,Kent, Lorraine,Morser, John,Zhao, Lei,Vergona, Ron,White, Kathy,Adler, Marc,Whitlow, Marc,Buckman, Brad O.
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p. 1349 - 1354
(2007/10/03)
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- 2,6-SUBSTITUTED-4-MONOSUBSTITUTED AMINO-PYRIMIDINE AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS
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The present invention is directed to a compound of formula (I) wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, a pharmaceutically acceptable prodrug thereof, or a pharmaceutically acceptable salt, hydrate or solvate of the prodrug, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds of the invention in admixture with a pharmaceutically acceptable carrier, a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which are generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like by administering to said patient a pharmaceutically effective amount of a compound of the invention.
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Page/Page column 24
(2008/06/13)
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- Immunopotentiator agents
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Novel compounds and methods for preparing same, immunopotentiating compositions, and a method for potentiating the immune system of a host animal. The method comprises administering to the animal an effective amount of an immunopotentiating compound of Formula I or Formula II, or a physiologically acceptable salt.
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Page column 13
(2010/02/05)
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- Beta lactam compounds and their use as inhibitors of tryptase
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Compounds of the formulas: are disclosed. These compounds inhibit tryptase as well as other enzyme systems or are selective tryptase inhibitors and are useful as antiinflammatory agents particularly in the treatment of chronic asthma.
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Page column 257
(2010/11/29)
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