Avermectin derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

Reexamination Certificate

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C536S007100

Reexamination Certificate

active

10997869

ABSTRACT:
A compound represented by the general formula (I) or a salt thereof:whereinrepresents —CH═CH—, —CH2—CH2— or the like,between R1and the carbon atom at 4′-position represents a single bond or a double bond,between R2and the carbon atom at 5-position represents a single bond or a double bond, and for example, 1) whenrepresents —CH═CH— or —CH2—CH2—, andbetween R1and the carbon atom at 4′-position represents a double bond, R1represents ═C(R11)(R12) (wherein R11represents a lower alkyl group or the like and R12represents a hydrogen atom or the like) or the like, and R2represents a hydroxyl group or the like, or R2may be combined together with the carbon atom at 5-position to form a carbonyl group, and 2) whenrepresents —CH═CH— or —CH2—CH2—, andbetween R1and the carbon atom at 4′-position represents a single bond, R1represents —OCH(R1a)(R1b) (wherein R1arepresents a lower alkyl or the like and R1brepresents a hydrogen atom or the like) or the like, and R2represents a hydroxyl group or the like.

REFERENCES:
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patent: 4427663 (1984-01-01), Mrozik
patent: 4833168 (1989-05-01), Wyvratt
patent: 4895837 (1990-01-01), Mrozik et al.
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patent: 5723488 (1998-03-01), Walshe
patent: 5733887 (1998-03-01), Walshe
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patent: 6605595 (2003-08-01), Omura et al.
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patent: 0456509 (1991-11-01), None
patent: 0480693 (1992-04-01), None
patent: 0506331 (1992-09-01), None
patent: 3-74397 (1991-03-01), None
patent: 3-254678 (1991-11-01), None
patent: 6-33273 (1994-05-01), None
patent: WO-93/18778 (1993-09-01), None
patent: WO-94/29328 (1994-12-01), None
patent: WO-95/04746 (1995-02-01), None
patent: WO-95/22552 (1995-08-01), None
English Language Abstract of JP 3-254678 (provided by esp@cenet).
English Language Abstract of JP 3-74397 (provided by esp@cenet).
English Language Abstract corresponding to JP 6-33273 (provided by esp@cenet).
Chabala, J.C. et al., “Ivermectin, a New Broad-Spectrum Antiparasitic Agent,” J. Med. Chem., 1980, 23, pp. 1134-1136.
Mrozik, H. et al., “Avermectin Acyl Derivatives with Anthelmintic Activity,” J. Med. Chem. 1982, 25, pp. 658-663.
U.S. Appl. No. 10/343,980, filed Feb. 6, 2003 (National Stage of PCT/JP01/06802, filed Aug. 8, 2001) having the title “Avermectin Derivatives” (Applicants: Satoshi Omura et al.).
Shin, et al., “Cleavage of the Spiroketal Portion of Avermectin B2p” Tetrahedron Letters, 1990, pp. 3525-3528, vol. 31, No. 25, Pergamon Press.

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