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-4216319-A 优先权日:1976-06-09 标题:Synthesis of 2,4-diamino-5-benzylpyrimidines using benzyl cyanoacetal intermediates 发明人:SWARINGEN ROY A JR; YEOWELL DAVID A 权利人:BURROUGHS WELLCOME CO 摘要:Benzyl cyanoacetals of formula: ##STR1## wherein R 1 , R 2 and R 3 are the same or different and each is a halogen or a hydrogen atom, an alkoxy group, an alkyl group, or a dialkylamino group; R 4 is an alkoxycarbonyl group, or an aldehyde group; and R 5 is an alkyl group; the alkyl or alkoxy groups each having from 1 to 4 carbon atoms, and their use as intermediates in the preparation of antibacterial 2,4-diamino-5-benzylpyrimidines. They are prepared from a reaction between an orthoester and an α-substituted-β-benzylpropionitrile and then the resulting cyanoacetal is converted to the benzylpyrimidine by reaction with guanidine.
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-4151196-A 优先权日:1975-06-26 标题 :Cyano-enol ethers 发明人:ROSEN PERRY 权利人:HOFFMANN LA ROCHE 摘要:The present invention relates to a new synthesis for the preparation of 5-(substituted benzyl)-2,4-diamino-pyrimidines, including new pyrimidine derivatives. More particularly, a new synthesis of ormetoprin, diaveridine and related compounds, including novel derivatives, is disclosed. The synthesis involves the condensation of a substituted benzene and an acrylonitrile derivative to directly give enol ether intermediates, which upon subsequent reaction by known techniques with guanidine, provides the desired 5-(substituted benzyl)-2,4-diamino-pyrimidines, including novel compounds. The pyrimidine end products are useful as potentiators of sulfonamides and as antibacterial agents.
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.
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合成参考文献
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