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[미국특허] 4″-Keto-and 4″-amino-4″-deoxy avermectin compounds and substituted amino derivatives thereof 원문보기

IPC분류정보
국가/구분 United States(US) Patent 등록
국제특허분류(IPC7판)
  • A61K-031/71
  • C07H-015/22
출원번호 US-0358736 (1982-03-16)
발명자 / 주소
  • Mrozik Helmut H. (Matawan NJ)
출원인 / 주소
  • Merck & Co., Inc. (Rahway NJ 02)
인용정보 피인용 횟수 : 47  인용 특허 : 9

초록 ▼

There are disclosed novel avermectin compounds wherein the 4″hydroxy group is oxidized to a keto group or replaced with an amino or substituted amino group. The keto compounds are prepared by oxidation with reagents such as oxalyl chloride in dimethylsulfoxide. The amino compounds are prepared from

대표청구항 ▼

A compound having the formula: [Figure] wherein R1 is 〓O, －NR5R6 or [Figure] wherein R1′is 〓O or －NR5R6: R5 and R6 are independently hydrogen, loweralkyl, loweralkanoyl, substituted benzenesulfonyl wherein the substituent is halogen; or loweralkyl sulfonyl; R2 is hydrogen or hydroxy; R3 is sec-butyl

이 특허에 인용된 특허 (9) 인용/피인용 타임라인 분석

  1. Sciavolino ; Frank C., 4-Deoxy-4-substituted amino derivatives of oleandomycin.
    상세보기
  2. Myers ; Robert F., 4-Substituted amino derivatives of oleandomycin.
    상세보기
  3. Myers Robert F. (East Lyme CT), 4″-Deoxy-4″-carbamate and dithiocarbamate derivatives of oleandomycin and its esters.
    상세보기
  4. Daniels Peter J. L. (Cedar Grove NJ) Turner William N. (Bloomfield NJ), 6′-N-alkyl-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols, methods for their use as antibacterial agents and composition.
    상세보기
  5. Mrozik Helmut H. (Matawan NJ) Albers-Schonberg George (Princeton NJ), Monosaccharide and aglycone derivatives of C-076.
    상세보기
  6. Albers-Schonberg George (Princeton NJ) Wallick Hyman (Springfield NJ) Ormond Robert E. (Edison NJ) Miller Thomas W. (Carteret NJ) Burg Richard W. (Murray Hill NJ), Novel substances and process for their production.
    상세보기
  7. Ross ; Barry C., Process for .omega.-amino-2-hydroxyalkyl derivatives of aminoglycoside antibiotics.
    상세보기
  8. Chabala John C. (Westfield NJ) Fisher Michael H. (Bridgewater NJ), Selective hydrogenation products of C-076 compounds and derivatives thereof.
    상세보기
  9. Bright ; Gene M., Semi-synthetic 4-ureido-oleandomycin derivatives.
    상세보기

이 특허를 인용한 특허 (47) 인용/피인용 타임라인 분석

  1. Asato Goro (Titusville NJ) France Donald J. (Pennington NJ), 13-deoxy-23-imino derivatives of 13-deoxy C-076-aglycone compounds.
    상세보기
  2. Asato Goro (Titusville NJ) France Donald J. (Pennington NJ), 23-Imino derivatives of LL-F28249 compounds.
    상세보기
  3. Mrozik Helmut ; Shih Thomas L., 24-and 25-substituted avermectin and milbemycin derivatives.
    상세보기
  4. Tobler, Hans, 4"-Deoxy-4"-(s)-amino avermectin derivatives.
    상세보기
  5. Tobler, Hans; Kessabi, Fiona Murphy, 4"-deoxy-4"-(S)-amido avermectin derivatives.
    상세보기
  6. Mrozik Helmut (Matawan NJ), 4″-Deoxy-4-N-methylamino avermectin Bla/Blb.
    상세보기
  7. Fisher Michael H. (Ringoes NJ) Mrozik Helmut (Matawan NJ), 5-oxime avermectin derivatives.
    상세보기
  8. Masurekar Prakash S. (Warren NJ) Shoop Wesley L. (Somerville NJ) Wallace Michael A. (Lebanon NJ) Monaghan Richard L. (Somerset NJ), Active avermectin analogue.
    상세보기
  9. Brück, Ernst; Erdelen, Christoph; Fischer, Reiner, Active ingredient combination having insecticidal and acaricidal characteristics.
    상세보기
  10. Bruck, Ernst; Erdelen, Christoph; Fischer, Reiner, Active ingredient combination having insecticidal and acaricidal characteristics.
    상세보기
  11. Fischer,Reiner; Erdelen,Christoph, Active ingredient combinations with insecticidal and acaricidal properties.
    상세보기
  12. Konze,J철rg; Andersch,Wolfram; St체bler,Dietrich; Fischer,R체diger, Active substance combinations having insecticidal and acaricidal properties.
    상세보기
  13. Konze,J철rg; Andersch,Wolfram; St체bler,Dietrich; Fischer,R체diger, Active substance combinations having insecticidal and acaricidal properties.
    상세보기
  14. Fischer, Reiner; Erdelen, Christoph; Bretschneider, Thomas, Active substance combinations with insecticidal and acaricidal properties.
    상세보기
  15. Eskola Philip (Wall NJ) Shih Thomas L. (Edison NJ) Mrozik Helmut (Matawan NJ), Alkyl avermectin derivatives.
    상세보기
  16. Goegelman Robert T. (Linden NJ), Anthelmintic fermentation products of microorganisms.
    상세보기
  17. Freehauf, Keith; Moaddeb, Maryam, Anthelmintic oral homogeneous veterinary pastes.
    상세보기
  18. Freehauf,Keith; Moaddeb,Maryam, Anthelmintic oral homogeneous veterinary pastes.
    상세보기
  19. Albright, Robert Bruce, Antiparasitic composition.
    상세보기
  20. Wyvratt ; Jr. Matthew J. (Mountainside NJ), Avermectin 8,9-cyclopropyl compounds, pharmaceutical composition and therapeutic methods of use.
    상세보기
  21. Cassayre, J?r?me, Avermectin B1 derivatives having an aminosulfonyloxy substituent in the 4′-position.
    상세보기
  22. Pitterna, Thomas; Maienfisch, Peter; Murphy Kessabi, Fiona; Cassayre, Jerome; Quaranta, Laura; Jung, Pierre, Avermectin and avemectin monosaccharide derivatives substituted in the 4"-or 4'-position having pesticidal properties.
    상세보기
  23. Pitterna, Thomas; Kessabi, Fiona Murphy; Maienfisch, Peter; Cassayre, Jerome; Quaranta, Laura; Jung, Pierre, Avermectin and avermectin monosaccharide derivatives substituted in the 4″-or 4′-position having pesticidal properties.
    상세보기
  24. Meinke Peter T. (New York NY), Avermectin compounds with a 6,5-spiroketal ring system ad a 23-acyl substituent.
    상세보기
  25. Linn Bruce O. (Bridgewater NJ) Mrozik Helmut (Matawan NJ), Avermectin derivatives.
    상세보기
  26. Omura, Satoshi; Sunazuka, Toshiaki; Turberg, Andreas; von Samson-Himmelstjerna, Georg; Hansen, Olaf; Harder, Achim, Avermectin derivatives.
    상세보기
  27. Omura,Satoshi; Nagai,Kenichiro; Sunazuka,Toshiaki, Avermectin derivatives.
    상세보기
  28. Omura,Satoshi; Nagai,Kenichiro; Sunazuka,Toshiaki, Avermectin derivatives.
    상세보기
  29. Murphy Kessabi, Fiona; Pitterna, Thomas; Maienfisch, Peter; Cassayre, Jérôme; Quaranta, Laura; Jung, Pierre; Hueter, Ottmar Franz, Avermectins and avermectin monosacharides substituted in the 4′-and 4″ position having pesticidal properties.
    상세보기
  30. Pitterna, Thomas; O'Sullivan, Anthony Cornelius; Lutz, William, Avermectins substituted in the 4″-position having pesticidal properties.
    상세보기
  31. Mrozik, Helmut H.; Waksmunski, Frank S., C-8A-Oxo-avermectin and milbemycin derivatives, pharmaceutical compositions and method of use.
    상세보기
  32. Soll, Mark David; Cramer, Luiz Gustavo; Pate, James; Shub, Natalya; Le Hir de Fallois, Loic Patrick; Timmons, Philip Reid, Compositions comprising an aryl pyrazole and/or a formamidine, methods and uses thereof.
    상세보기
  33. Soll, Mark David; Cramer, Luiz Gustavo; Wurtz, Patrice; Pate, James; Shub, Natalya; Le Hir de Fallois, Loic Patrick; Timmons, Philip Reid, Compositions comprising an aryl pyrazole and/or a formamidine, methods and uses thereof.
    상세보기
  34. Egerton John R. (Neshanic Station NJ), Increased litter size in monogastric domestic animals after treatment in mid-gestation of gravid female with avermectin.
    상세보기
  35. Chern, Rey T.; Zingerman, Joel R., Liquid polymeric compositions for controlled release of bioactive substances.
    상세보기
  36. Ramsay Michael V. J. (South Harrow) Evans Derek N. (South Ruislip) Sutherland Derek R. (Chalfont St Giles) Tiley Edward P. (Pinner) Ward John B. (Chorleywood) Porter Neil (Pinner) Noble Hazel M. (Ayl, Macrolide compounds.
    상세보기
  37. Wurtz, Patrice, Multi-cavity container having offset indentures for dispensing fluids.
    상세보기
  38. Putter Irving (Martinsville NJ) Stout Daniel M. (Kirkwood MO), Novel synergistic compositions.
    상세보기
  39. Pachlatko, Johannes Paul; Pitterna, Thomas; Jungmann, Volker, Preparation of a macrocyclic lactone.
    상세보기
  40. Pitterna, Thomas, Salts of avermectins substituted in the 4″-position and having pesticidal properties.
    상세보기
  41. Andersch,Wolfram; Lubos Erdelen, legal representative,Angelika; Jeschke,Peter; Erdelen, deceased,Christoph, Synergistic insecticidal mixtures.
    상세보기
  42. Andersch, Wolfram; Jeschke, Peter; Bretschneider, Thomas; Lubos-Erdelen, Angelika, Synergistic insecticide mixtures.
    상세보기
  43. Yin, Mingxing; Wu, Jianchao; Chai, Jian, Synthesis process of antiparasitic drug selamectin.
    상세보기
  44. Boeckh, Albert; Cramer, Luiz Gustavo; Soll, Mark D., Topical formulations comprising 1-N-arylpyrazole derivatives and amitraz.
    상세보기
  45. Boeckh, Albert; Cramer, Luiz Gustavo; Soll, Mark D., Topical formulations comprising 1-N-arylpyrazole derivatives and amitraz.
    상세보기
  46. Boeckh, Albert; Cramer, Luiz Gustavo; Soll, Mark David, Topical formulations comprising 1-N-arylpyrazole derivatives and amitraz.
    상세보기
  47. Wallace Dennis H. (Columbia MO), Treatment for fescue toxicosis in grazing animals.
    상세보기

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