专利号:US-7576211-B2 优先权日:2004-09-30 标题 :Synthesis of thienopyridinone compounds and related intermediates 发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE 权利人:EPIX DELAWARE INC 摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
专利号:US-2008214827-A1 优先权日:2004-02-03 标 题:Synthesis of Cyanoimino-Benzoimidazoles 发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN 权利人:EURO CELTIQUE SA 摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.
专利号:US-7749985-B2 优先权日:2006-09-15 标 题 :Acyloxyalkyl carbamate prodrugs, methods of synthesis and use 发明人:GALLOP MARK A; XU FENG; PHAN THU; DILIP USHA; PENG GE 权利人:XENOPORT INC 摘要:Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of making acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of using acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, and pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs 3-aminopropylphosphinic acid and analogs thereof for treating diseases or disorders such as mild cognitive impairment, cognitive impairment associated with Alzheimer's disease Alzheimer's disease, depression, anxiety, and epilepsy are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, which are suitable for oral administration and sustained release oral dosage forms are also disclosed.
专利号:US-7354923-B2 优先权日:2001-08-10 标 题 :Piperazine melanocortin-specific compounds 发明人:SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH 权利人:PALATIN TECHNOLOGIES INC 摘要:Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure: n nand stereoisomer and pharmaceutically acceptable salts thereof, where X is CH 2 or Câ•?O, R 1 , R 2 , and R 3 are as described in the specification, preferably where R 3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R 3 optionally further includes an amine capping group, a second amino acid residue or a second amino acid residue with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.
专利号:US-2006084805-A1 优先权日:2004-09-30 标题:Synthesis of thienopyridinone compounds and related intermediates
专利号:WO-2005102340-A1 优先权日:2003-05-30 标题 :Piperazine melanocortin-specific compounds 发明人:SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH 权利人:PALATIN TECHNOLOGIES INC; SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH 摘要:Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure (I); and stereoisomer and pharmaceutically acceptable salts thereof, where X is CH2 or C=O, R1, R2, and R3 are as described in the specification, preferably where R3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R3 optionally further includes an amine capping group, a second amino acid residue or a second amino acid residue with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.
1: Moretti A, Caccia C, Martini A, Bonollo L, Amico A, Sega R, Nicolella V, Nicolis FB. Effect of caroxazone, a new antidepressant drug, on monoamine oxidases in healthy volunteers. Br J Clin Pharmacol. 1981 May;11(5):511-5. 2: Martini A, Bonollo L, Nicolis FB, Sega R, Palermo A. Effects of caroxazone, a reversible monoamine oxidase inhibitor, on the pressor response to oral tyramine in man. Br J Clin Pharmacol. 1981 Jun;11(6):611-5. 3: Martini A, Bonollo L, Nicolis FB, Sega R, Palermo A, Braibanti E. Effects of caroxazone, a reversible monoamine oxidase inhibitor, on the pressor response to intravenous tyramine in man. Br J Clin Pharmacol. 1981 Jun;11(6):605-10.
合成参考文献
摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749 摘要:Psychotropic Drugs and Related Compounds, 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972, -(231), 1972 摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003).