专利号:US-9777034-B2 优先权日:2013-05-21 标题 :Modular synthesis of amphiphilic Janus glycodendrimers and their self-assembly into glycodendrimersomes 发明人:PERCEC VIRGIL 权利人:UNIV PENNSYLVANIA 摘要:The invention concerns compounds of the formula (I) wherein: Y 1 and Y 2 are independently a monosaccharide or disaccharide; X 1 and X 2 are independently —(R 9 —O) m —, —(R 10 ) p —, —O—(R 11 —O) q —, —R 16 —O—R 17 —O— or a covalent bond; Q 1 and Q 2 are independently a nitrogen-containing heterocycle moiety; Z 1 and Z 2 are independently —(O—R 7 )—, —(O—C(â•?O)—R 8 )a-, —O—C(â•?O)—R 12 —C(=0)-R 13 —, —O—C(â•?O)—R 14 —C(â•?O)—R 15 or a covalent bond; R 7 -R 17 are each independently C 1 -C 6 alkyl; R 1 -R 6 are each independently a linear or branched alkyl group; b, c, d, e, f, and g are 0 or 1, provided b+c+d equals at least 2 and e+f+g equals at least 2; and a, m, p, and q are each an integer from 1-6.
专利号:US-2008039473-A1 优先权日:2006-08-08 标题:Preparation and utility of substituted quinazoline compounds with alpha-adrenergic blocking effects 发明人:GANT THOMAS G; SARSHAR SEPEHR 权利人:AUSPEX PHARMACEUTICALS INC 摘要:The present disclosure is directed to modulators of alpha-adrenergic receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the use of such compounds for the treatment and/or management of hypertension, cardiac failure, prostatitis, and benign prostatic hyperplasia, and any other condition in which it is beneficial to modulate an alpha-adrenergic receptor.
专利号:US-7745490-B2 优先权日:2004-05-12 标题 :Substituted N-aryl benzamides and related compounds for treatment of amyloid diseases and synucleinopathies 发明人:SNOW ALAN D; NGUYEN BETH P; LAKE THOMAS P; CASTILLO GERARDO M; WEIGELE MANFRED 权利人:PROTEOTECH INC 摘要:Substituted n-aryl benzamides, related compounds and their pharmaceutically acceptable derivatives, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, including Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment are provided.
专利号:US-7872013-B2 优先权日:2006-08-16 标 题 :Preparation and utility of opioid analgesics 发明人:GANT THOMAS G; SARSHAR SEPEHR 权利人:AUSPEX PHARMACEUTICALS INC 摘要:The present disclosure is directed to modulators of opiate- and/or NMDA receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the use of such compounds for the treatment and/or management of pain, anxiety, neurodegeneration, drug dependence, coughing, muscular tension, and/or glaucoma and any other condition in which it is beneficial to modulate an opiate- and/or NMDA receptor.
专利号:US-2016108076-A1 优先权日:2013-05-21 标题:Modular synthesis of amphiphilic janus glycodendrimers and their self-assembly into glycodendrimersomes
专利号:US-2011015119-A1 优先权日:2009-06-24 标题:Novel semi-synthetic glycopeptides as antibacterial agents 发明人:CHU DANIEL; YE TAO; WANG BING 权利人:LEAD THERAPEUTICS INC 摘要:Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of a glycopeptide (Compound A, Compound B, Compound H or Compound C) or monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Key reaction is the treatment of properly protected intermediate compound with isocyanate. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.