- Immunomodulatory peptides
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The invention relates to peptides derivatized with a hydrophilic polymer which, in some embodiments, bind to human FcRn and inhibit binding of the Fc portion of an IgG to an FcRn, thereby modulating serum IgG levels. The disclosed compositions and methods may be used in some embodiments, for example, in treating autoimmune diseases and inflammatory disorders. The invention also relates, in further embodiments, to methods of using and methods of making the peptides of the invention.
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- Bisoxazoline and bioxazoline chiral ligands bearing 4-diphenylmethyl shielding substituents. Diels-Alder reaction of cyclopentadiene with 3-acryloyl-2-oxazolidinone catalyzed by the aqua nickel(II) complex
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Enantiopure 2-amino-3,3-diphenyl-1-propanol was synthesized by the hidantoin route starting from diphenyl-acetaldehyde followed by subsequent functional group transformations and optical resolution by a chiral HPLC. The amino alcohol can be converted into two new chiral ligands: 4,4'-bis(diphenylmethyl)-2,2'-bioxazoline and 2,2'-isopropylidenebis(4-diphenylmethyloxazoline), and further to complexes with copper(II) trifluoromethanesulfonate and nickel(II) perchlorate hexahydrate. The nickel(II) aqua complex obtained from the bisoxazoline effectively catalyzed the Diels-Alder reactions of cyclopentadiene with 3-acryloyl-2-oxazolidinone in high endo-selectivities and moderate enantioselectivities via a square planar transition structure.
- Kanemasa,Adachi,Yamamoto,Wada
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p. 681 - 687
(2007/10/03)
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- Substituted quinoxaline-2-ones as glutamate receptor antagonists
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A novel series of substituted quinoxaline 2-ones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the compounds are also taught. The compounds are glutamate receptor antagonists and are useful in the treatment of stroke, cerebral ischemia, or cerebral infarction resulting from thromboembolic or hemorrhagic stroke, cerebral vasospasms, hypoglycemia, cardiac arrest, status epilepticus, perinatal asphyxia, anoxia, seizure disorders, pain, Alzheimer's, Parkinson's, and Huntington's Diseases.
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- Process for the preparation of D(-) and L(+)-3,3-diphenylalanine and D(-) and L(+)-substituted 3,3-diphenylalanines and derivatives thereof
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A process for the preparation of D(-) and L(+)-3,3-diphenylalanine and D(-) and L(+)-substituted 3,3-diphenylalanines is described where N-protected DL-3,3-diphenylalanine or N-protected-DL-substituted 3,3-diphenylalanine are treated with (-)cinchonidine and the resulting salt resolved into the desired enantiomers, as well as derivatives thereof and valuable intermediates used in the process.
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- Hydrophobic peptides
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Hydrophobic peptides having antihypertensive activity are disclosed. Also disclosed are pharmaceutical compositions comprising a hydrophobic peptide and a method of treatment of mammalian hypertension comprising administering a hydrophobic peptide to a hy
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