专利号:US-9693999-B2 优先权日:2011-01-26 标题:Small molecule RNase inhibitors and methods of use 发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE 权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education 摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.
专利号:US-9439423-B2 优先权日:2007-10-29 标 题 :Antiparasitic agent for fish and method of controlling proliferation of fish parasites 发明人:KAWANO FUMI; HIRAZAWA NORITAKA 权利人:KAWANO FUMI; HIRAZAWA NORITAKA; NIPPON SUISAN KAISHA LTD 摘要:An antiparasitic agent for fish includes an inhibitor of folate synthesis and/or an inhibitor of folate activation as the active substance(s). A combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is disclosed. Sulfonamide is disclosed as suitable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist are disclosed as suitable inhibitors of folate activation. The antiparasitic agent is able to exterminate fish parasites via oral administration. It is effective against fish parasites belonging to the ciliate group.
专利号:US-9265777-B2 优先权日:2009-04-27 标题 :Antiparasitic agent for fish and method of controlling proliferation of fish parasites 发明人:KAWANO FUMI; HIRAZAWA NORITAKA 权利人:KAWANO FUMI; HIRAZAWA NORITAKA; NIPPON SUISAN KAISHA LTD 摘要:A method of controlling proliferation of fish parasites comprising the administration of 1 to 50 mg/kg fish body weight/day of an inhibitor of folate synthesis and/or an inhibitor of folate activation to fish continuously for 1 to 2 weeks. Using a combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is preferable, and a sulfonamide is preferable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist, etc., can be used as the inhibitor of folate activation. The antiparasitic agent is able to exterminate fish parasites via oral administration. It is particularly effective against parasites belonging to the ciliate group among fish parasites.
专利号:US-2007203079-A1 优先权日:2005-11-21 标题:Methods of using small molecule compounds for neuroprotection 发明人:CALDWELL GUY A; CALDWELL KIM A; CAO SONGSONG 权利人:CALDWELL GUY A; CALDWELL KIM A; CAO SONGSONG 摘要:Methods are provided for preventing neurodegeneration and neuronal loss by administering compositions comprising small molecule compounds with the effect of preventing neurodegeneration and neuronal loss. In one aspect of the invention, the methods and compositions are also useful for treating neurodegenerative diseases. Small molecule compounds provide an important treatment option because of their stability, ease of use in both manufacture and formulation, ease of administration, and patient compliance. The small molecule compound compositions of the present invention may include topoisomerase II inhibitors, bacterial transpeptidase inhibitors, calcium channel antagonists, cyclooxygenase inhibitors, folic acid synthesis inhibitors, or sodium channel blockers and functional analogues thereof that have an effect on neurodegeneration. The compositions of the present invention may be administered prophylactically before the onset of clinical symptoms or after clinical symptoms of a neurodegenerative disease have manifested.
专利号:US-6103865-A 优先权日:1998-08-03 标 题 :PH-sensitive polymer containing sulfonamide and its synthesis method 发明人:BAE YOU HAN; PARK SANG YEOB 权利人:KWANGJU INST SCI & TECH 摘要:There are disclosed pH-sensitive polymers containing sulfonamide groups, which can be changed in physical properties, such as swellability and solubility, depending on pH and which can be applied for a drug-delivery system, bio-material, sensor, etc, and a preparation method therefor. The pH-sensitive polymers are prepared by introduction of sulfonamide groups, various in pKa, to hydrophilic groups of polymers either through coupling to the hydrophilic groups, such as acrylamide, N,N-dimethylacrylamide, acrylic acid, N-isopropylacrylamide, etc, of polymers or copolymerization with other polymerizable monomers. These pH-sensitive polymers may have a structure of linear polymer, grafted copolymer, hydrogel or interpenetrating network polymer.
专利号:WO-2009056955-A1 优先权日:2007-10-30 标题 :Amine-bearing phospholipids (abps), their synthesis and use 发明人:ZUMBUEHL ANDREAS 权利人:UNIV BASEL; ZUMBUEHL ANDREAS 摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.
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合成参考文献
摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664 参考文献:10.1002/bies.10114 摘要:Bermingham A, Derrick JP. The folic acid biosynthesis pathway in bacteria: evaluation of potential for antibacterial drug discovery. Bioessays. 2002 Jul;24(7):637–48. doi: 10.1002/bies.10114.