- PYRROLIDINE GPR40 MODULATORS FOR THE TREATMENT OF DISEASES SUCH AS DIABETES
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The present invention provides compounds of Formula (I) or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.
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Page/Page column 67
(2015/11/27)
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- NICOTINIC RECEPTOR COMPOUNDS
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Provided herein are compounds and methods of preparation of compounds that are capable of functioning as agonists or antagonists of a nicotinic receptor. Also provided are pharmaceutical compositions comprising one or more of these compounds, which may further comprise one or more additional therapeutic agents. Further provided are methods of treatment of various conditions that may be responsive to such activity at the nicotinic receptors, such as nicotine dependence.
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Page/Page column 56
(2012/03/11)
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- 2-ARYLBENZOTHIOPHENE DERIVATIVES OR PHARCEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARCEUTICAL COMPOSITION FOR THE DIAGNOSIS OR TREATMENT OF DEGENERATIVE BRAIN DISEASE CONTAINING THE SAME AS ACTIVE INGREDIENT
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2-arylbenzothiophene derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition for the diagnosis or treatment of degenerative brain disease containing the same as an active ingredient. Since the 2-arylbenzothiophene derivatives of Formula 1 have a relatively high binding affinity for β-amyloid, they can be used as diagnostic reagents for diagnosing Alzheimer's disease at an early stage by non-invasive techniques when they are labeled with radioisotopes: wherein R1-R4, V, W, X, Y and Z are as defined in the Detailed Descript of the specification. Further, when the pharmaceutical composition containing the 2-arylbenzothiophene derivative binds with a low-molecular weight β-amyloid peptide binding compound, generation of malignant high-molecular weight β-amyloid deposits is minimized. Accordingly, the pharmaceutical composition can be used as a therapeutic agent of degenerative brain disease such as Alzheimer's disease.
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Page/Page column 26
(2010/11/03)
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- Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics.
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We have introduced solubilizing functionality to a 3,6-disubstituted pyrazolo[1,5-a]pyrimidine series of KDR kinase inhibitors to improve the physical properties of these compounds. The addition of a basic side-chain to the 6-aryl ring, introduction of 3-pyridyl groups, and most significantly, incorporation of a 4-pyridinonyl substituent at the 6-position of the core are modifications that maintain and often enhance the intrinsic potency of this class of inhibitors. Moreover, the improvements in physical properties result in marked increases in cellular activity and more favorable pharmacokinetics in rats. The synthesis and SAR of these compounds are described.
- Fraley, Mark E,Rubino, Robert S,Hoffman, William F,Hambaugh, Scott R,Arrington, Kenneth L,Hungate, Randall W,Bilodeau, Mark T,Tebben, Andrew J,Rutledge, Ruth Z,Kendall, Richard L,McFall, Rosemary C,Huckle, William R,Coll, Kathleen E,Thomas, Kenneth A
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p. 3537 - 3541
(2007/10/03)
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- Catalyzed Metalation Applied to 2-Methoxypyridine
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Directed ortho lithiation of 2-methoxypyridine (1) has been regioselectively achieved at position 3 by using methyllithium catalyzed by a small amount of diisopropylamine.This metalation methodology, called "catalyzed metalation", gave good results whereas other metalation routes failed.This allowed the convenient synthesis of various 3-substituted 2-methoxypyridines of general interest.
- Trecourt, F.,Mallet, M.,Marsais, F.,Queguiner, G.
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p. 1367 - 1371
(2007/10/02)
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