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Title:
12の環原子を有する環状デプシペプチドの内部寄生虫の防除のための利用、12の環原子を有する新規環状デプシペプチド及びそれらの製造法
Document Type and Number:
Japanese Patent JP3626233
Kind Code:
B2
Abstract:
Control of endoparasites in human beings and animals comprises admin. of cyclic depsipeptide of formula (I); R<1>,R<4> = H or opt. substd. alkyl, cycloalkyl, aralkyl, aryl, heteroaryl or heteroarylalkyl; R<2>,R<3>,R<5>,R<6> = H; 1-8C alkyl; haloalkyl; HO-alkyl; alkanoylalkyl; alkoxyalkyl; aryloxyalkyl; HS-alkyl; alkylthioalkyl; alkylsulphinylalkyl; alkylsulphonylalkyl; COOH-alkyl; alkoxycarbonylalkyl; arylalkoxycarbonylalkyl; carbamoylalkyl; H2N-alkyl opt. N-mono- or N,N-di-substd. by alkyl; guanidinoalkyl opt. mono- or di-substd. by BzO-CO- or mono- to tetra-substd. by alkyl; alkoxycarbonylaminoalkyl; Fmoc-aminoalkyl; alkenyl; cycloalkyl; cycloalkylalkyl; or opt. substd. aryl, aralkyl, heteroaryl or heteroarylalkyl. Known cpds. (I) are described in J.A.C.S. 91(1969), p. 4888; Biorg. Khim. 1 (1975), 375; Biofizica 16 (1971) p. 407; and lav. Akad. Nark. SCSR, Set Khim, 1970, p. 991. (I) have good mammalian toxicity and can be used to control pathogenic endoparasites such as cestodes, trematodes, nematodes and acantocephales, e.g. Taenia, Dactylogyrus, Schistosoma, Fasciola, Trichomosoides, Strondyloides, Filaroides, Enterobius and Toxocara spp. (I) are pref. used in veterinary medicine to treat e.g. domestic pets, farm, zoo and laboratory animals, poultry, fish and insects such as honey bees and silkworms. (I) can also be used therapeutically or prophylactically in the form of conventional formulations, e.g. powders, tablets or medicated feed, and may be administered by the enteral, parenteral, nasal or transdermal route. (I) are more active in controlling worm diseases than prior art cpds.

Inventors:
Jürgen Cielkenbeck
Peter Yesuke
Andrew Plant
Achim Halder
Norbert Menke
Application Number:
JP2132595A
Publication Date:
March 02, 2005
Filing Date:
January 13, 1995
Export Citation:
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Assignee:
Bayer Aktiengesellschaft
International Classes:
A61K31/33; A61K31/365; A61K31/38; A61K31/41; A61K38/00; A61P33/00; A61P33/10; C07D273/00; C07D273/08; C07D413/06; C07K11/02; (IPC1-7): C07K11/02; A61K31/41; A61K38/00; A61P33/00; C07D273/08
Attorney, Agent or Firm:
Heikichi Odashima