专利号:WO-0005212-A1 优先权日:1998-07-21 标 题:3-substituted pyridine compounds and related synthesis 发明人:HOGLEN DEAN KENT 权利人:NOVARTIS AG; NOVARTIS ERFIND VERWALT GMBH; HOGLEN DEAN KENT 摘要:The present invention relates to 3-substituted and 2,3-disubstituted pyridine compounds of formula (I), wherein R1 is C1-C4 haloalkyl and R4 is H, halogen or C1-C4 alkylthio; and acid addition salts thereof which are useful as intermediates in the synthesis of pyridylsulfonylurea herbicides. The invention also relates to arylation of alcohols using a pyridinediazonium salt. More particularly the arylation process of the instant invention relates to the synthesis of 2,3-disubstituted pyridine compounds via anhydrous diazotization of 3-aminopyridines to form a diazonium salt intermediate that is then reacted with the appropriate alcohol to produce the desired product. The invention additionally relates to pyridine-3-diazonium salt intermediates.
专利号:US-6093739-A 优先权日:1997-11-21 标 题:Synthesis of long wavelength absorbing photosensitizers 发明人:JOHNSON CLAIRE K; DOLPHIN DAVID 权利人:UNIV BRITISH COLUMBIA 摘要:The present invention provides for novel therapeutic macrocycle compounds useful in photodynamic therapy that are based on the chlorin ring system. The macrocycle compounds have, in many cases, wavelengths of activation at about 670 nm, characteristics of chlorins, and are stabilized against oxidation by the attachment to the chlorin ring of a structure that comprises one or more exocyclic rings that contribute at least one nitrogen atom. Protonation or covalent modification of this nitrogen atom, or other covalent modification of the one or more exocyclic rings permits optimization of pharmacalogically relevant properties including, for example, solubility. Representative chlorins include the pyridochlorins depicted as follows ##STR1##
专利号:US-6710180-B2 优先权日:1998-07-21 标题 :Diazonium salts which are intermediates for 3-substituted pyridines 发明人:HOGLEN DEAN KENT 权利人:SYNGENTA PARTICIPATIONS AG 摘要:The present invention relates to 3-substituted and 2,3-disubstituted pyridine compounds which are useful as intermediates in the synthesis of pyridylsulfonylurea herbicides. The invention also relates to arylation of alcohols using a pyridinediazonium salt. More particularly the arylation process of the instant invention relates to the synthesis of 2,3-disubstituted pyridine compounds via anhydrous diazotization of 3-amninopyridines to form a diazonium salt intermediate that is then reacted with the appropriate alcohol to produce the desired product. The invention additionally relates to pyridine-3-diazonium salt intermediates.
专利号:US-7687487-B2 优先权日:2007-04-19 标题 :Camptothecin-analog with a novel, “flippedâ€? lactone-stable, E-ring and methods for making and using same 发明人:HAUSHEER FREDERICK H 权利人:BIONUMERIK PHARMACEUTICALS INC 摘要:The present invention discloses: (i) a novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (ii) methods of synthesis of said novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (iii) pharmaceutically-acceptable formulations comprising said novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents; (iv) methods of administration of said novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof; and (v) devices for the administration of said novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more chemotherapeutic aents, to subjects in need thereof.
专利号:US-7999090-B2 优先权日:2000-07-07 标 题:Fungal cell wall synthesis gene 发明人:TSUKAHARA KAPPEI; HATA KATSURA; SAGANE KOJI; NAKAMOTO KAZUTAKA; TSUCHIYA MAMIKO; WATANABE NAOAKI; OHBA FUMINORI; TSUKADA ITARU; UEDA NORIHIRO; TANAKA KEIGO; KAI JUNKO 权利人:EISAI R&D MAN CO LTD 摘要:The present invention provides isolated DNA encoding a GWT1 protein having activity to confer resistance of a fungus against a compound of formula Ia, and wherein a defect of a function of the GWT1 protein leads to a decrease in the amount of a glycosylphosphatidylinositol (GPI)-anchored protein in the cell wall of a fungus.
专利号:EP-2007386-B1 优先权日:2006-04-19 标题 :Camptothecin-analog with a novel, flipped lactone-stable, e-ring and methods for making and using same 发明人:HAUSHEER FREDERICK H 权利人:BIONUMERIK PHARMACEUTICALS INC 摘要:The present invention discloses: (i) a novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (ii) methods of synthesis of said novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (iii) pharmaceutically-acceptable formulations comprising said novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents; (iv) methods of administration of said novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof; and (v) devices for the administration of said novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more chemotherapeutic aents, to subjects in need thereof.
参考标题:Design And Synthesis Of Novel, Potent And Selective Hypoxanthine Analogs As Adenosine A 1 Receptor Antagonists And Their Biological Evaluation 作者:Summon Koul,Vidya Ramdas,Dinesh A. Barawkar,Yogesh B. Waman,Neela Prasad,Santosh Kumar Madadi,Yogesh D. Shejul,Rajesh Bonagiri,Sujay Basu,Suraj Menon,Srinivasa B. Reddy,Sandhya Chaturvedi,Srinivas Rao Chennamaneni,Gaurav Bedse,Rhishikesh Thakare,Jayasagar Gundu,Sumit Chaudhary,Siddhartha De,Ashwinkumar V. Meru,Venkata Palle,Anita Chugh,Kasim A. Mookhtiar |发布日期:2017.3 摘要:Multipronged Approach Was Used To Synthesize A Library Of Diverse C-8 Cyclopentyl Hypoxanthine Analogs From A Common Intermediate Iii. Several Potent And Selective Compounds Were Identified And Evaluated For Pharmacokinetic (Pk) Properties In Wistar Rats. One Of The Compounds 14 With Acceptable Pk Parameters Was Selected For Testing In In Vivo Primary Acute Diuresis Model. The Compound Demonstrated
合成参考文献
摘要:U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals., NX#04685 摘要:Keller, P. A., Science of Synthesis, (2005) 15, 380.