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Title:
THTRAHYDROPYRAN DERIVATIVE
Document Type and Number:
Japanese Patent JP2713561
Kind Code:
B2
Abstract:

PROBLEM TO BE SOLVED: To obtain the subject new compound exhibiting an excellent antifungal activity and excellent stability, useful for the local and systemic treatments of human and animal mycosis, and especially useful for the therapy of mucosal mycotic infection, etc.
SOLUTION: A compound of formula I [R1 is a Y-a(ra)lkyl group of the formula (Y is CONH, etc.,), etc.; R2 is H, OH; R3 is amino, aminoacetoxy (R31), (aminoacetyl)amino (R32), etc.; R4, R5 are each H, a lower alkyl, an alkoxy, etc.; R6 is H, OH, a lower alkyl, etc.; R7 is HG, OH, etc.; R2 and R4 may be bound to each other to forma single bond], its salt, hydrate or solvate, or their salts. For example, (2S, 3R, 4S, 5S)-4-methoxy-5-methyl-2-[(Z)-1-nonenyl) tetrahydro-2H-pyran-3-yl glycinate. The compound of formula I wherein R2 is H, and R3 is R31 or R32 is obtained by acylating a compound of formula II (R31 is OH, amino) with an N-protected glycine and subsequently removing the protecting group.


Inventors:
Yuko Aoki
Hiromichi Kotaki
Ichinao Masubuchi
Toru Okuda
Nobuo Shinma
Takuo Tsukuda
Umeda Isao
Application Number:
JP23153296A
Publication Date:
February 16, 1998
Filing Date:
September 02, 1996
Export Citation:
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Assignee:
F. Hoffman-La Rochille Age
International Classes:
A61K31/075; A01N37/44; A01N43/16; A01N43/20; A01N43/40; A01N43/42; A01N43/50; A01N43/653; A01N43/90; A01N49/00; A01N57/20; A61K31/015; A61K31/13; A61K31/336; A61K31/35; A61K31/351; A61K31/41; A61K31/415; A61K31/665; A61K31/70; A61K31/7028; A61P31/04; A61P31/10; C07C35/17; C07C43/188; C07C43/196; C07C43/205; C07C43/235; C07C45/30; C07C45/40; C07C45/51; C07C47/47; C07C211/17; C07C215/20; C07C217/52; C07C225/10; C07C225/20; C07C233/06; C07C233/38; C07C233/54; C07C235/40; C07C237/04; C07C321/22; C07D233/60; C07D233/61; C07D249/08; C07D303/12; C07D309/02; C07D309/08; C07D309/10; C07D309/14; C07D405/06; C07D405/12; C07D413/06; C07D413/08; C07D413/14; C07D417/06; C07D493/04; C07D493/10; C07D493/20; C07D495/10; C07D521/00; C07F9/32; C07F9/655; C07F9/6558; C07H15/04; (IPC1-7): C07D309/10; A01N43/16; A01N43/20; A01N43/40; A01N43/42; A01N57/20; A61K31/35; A61K31/41; A61K31/415; A61K31/665; A61K31/70; C07D309/08; C07D309/14; C07D405/06; C07D405/12; C07D417/06; C07D493/04; C07D493/10; C07D493/20; C07D495/10; C07F9/32; C07F9/655
Domestic Patent References:
JP3200780A
JP4427893B1
Other References:
EUR.J.MED.CHEM.−CHIM.THER.,12〜4!(1977)P.317−324
J.ORG.CHEM.,47〜19!(1982)P.3643−3646
Attorney, Agent or Firm:
Hajime Tsukuni (1 person outside)