Aureobasidins

Assignee: Takara Shuzo Co Ltd

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Filing: 1994-12-26

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Granted: 1997-12-16

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Expires: 2014-12-26

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Abstract

Abstract This invention relates to Aureobasidins useful as an antifungal agent having broader spectrum. The compound according to this invention includes a cyclic depsipeptide consisting of one hydroxy acid residue having A 1 , 3 amino acid residues having C 1 , F 1 and H 1 , respectively, 4 N-methylamino acid residues having B 1 , D 1 , G 1 and I 1 , respectively, and 1 cyclic amino acid residue having E 1 . The typical compound includes one wherein A 1 is CH 3 CH 2 CH(CH 3 )--, B 1 is (CH 3 ) 2 CH--, C 1 is benzyl, cyclohexylmethyl, p-fluorobenzyl, benzyloxymethyl, benzyloxybenzyl, methoxybenzyl, cyclohexylmethyloxybenzyl or the like, D 1 is methyl, benzyl, hydroxymethyl or the like, E 1 is --(CH 2 ) 3 --, F 1 is CH 3 CH 2 CH(CH 3 )--, G 1 is (CH 3 ) 2 CH--, H 1 is (CH 3 ) 2 CHCH 2 -- and I 1 is (CH 3 ) 2 C(OH)--. The compound according to this invention has an excellent activity against not only Candida but also Cryptococcus and Aspergillus.

Inventors

👤 Toru Kurome
👤 Tetsuya Inoue
👤 Kazutoh Takesako
👤 Kaoru Inami
👤 Ikunoshin Kato

Bibliographic Details

Application Number —

Jurisdiction US

Data Source google_patents

Last Synchronized 2026-10-29 05:08

CPC Classifications

C; C07; C07K; C07K11/00; C07K11/02; A; A61; A61P; A61P31/00; A61P31/04; A61K; A61K38/00

Claims Analysis

Total Claims: 4

Claim 1

Independent Claim 181 words

An Aureobasidin compound of general formula (1): ##STR10## wherein A 1 , B 1 , F 1 , G 1 and H 1 are the same or different from each other and each represents a straight-chain or branched lower alkyl having 1 to 6 carbon atoms; C 1 represents a straight-chain or branched lower alkyl having 1 to 6 carbon atoms, a cycloalkyl group having 3 to 7 carbon atoms, benzyloxymethyl, benzyl, a substituted benzyl, phenyl or a substituted phenyl (said substituted benzyl or substituted phenyl means benzyl or phenyl substituted by at least one substituent selected from a straight-chain or branched lower alkoxy having 1 to 6 carbon atoms, cycloalkoxy having 3 to 7 carbon atoms, benzyloxy and halogen); D 1 represents a straight-chain or branched lower alkyl having 1 to 6 carbon atoms, hydroxymethyl or benzyl (where C 1 is benzyl, ortho-fluorobenzyl, or meta-fluorobenzyl, D 1 is a group other than benzyl and hydroxymethyl); E 1 represents a straight-chain alkylene having 1 to 5 carbon atoms; I 1 represents a hydroxy-substituted lower alkyl having 1 to 6 carbon atoms.

Claim 2

Dependent Claim 181 words

Claim 3

Dependent Claim 219 words

The Aureobasidin compound according to claim 1, wherein; said A 1 is (CH 3 ) 2 CH-- or CH 3 CH 2 CH(CH 3 )--, said B 1 is (CH 3 ) 2 CH--, said C 1 is a straight-chain or branched lower alkyl having 1 to 6 carbon atoms, a cycloalkyl having 3 to 7 carbon atoms, benzyloxymethyl, benzyl, a substituted benzyl, phenyl or a substituted phenyl (said substituted benzyl or substituted phenyl means benzyl or phenyl substituted by at least one substituent selected from a straight-chain or branched lower alkoxy having 1 to 6 carbon atoms, cycloalkoxy having 3 to 7 carbon atoms, benzyloxy and halogen), said D 1 is a straight-chain or branched lower alkyl group having 1 to 6 carbon atoms, hydroxymethyl or benzyl (where C 1 is benzyl, ortho-fluorobenzyl, or meta-fluorobenzyl, D 1 is not benzyl and hydroxymethyl), said E 1 is --(CH 2 ) 3 --, said F 1 is (CH 3 ) 2 CH--, (CH 3 ) 2 CHCH 2 -- or CH 3 CH 2 CH(CH 3 )--, said G 1 is (CH 3 ) 2 CH--, said H 1 is (CH 3 ) 2 CH--, (CH 3 ) 2 CHCH 2 -- or CH 3 CH 2 CH(CH 3 )--, and, said I 1 is (CH 3 ) 2 C(OH)--.

Claim 4

Dependent Claim 224 words

The Aureobasidin compound according to claim 2, wherein; said A 1 is (CH 3 ) 2 CH-- or CH 3 CH 2 CH(CH 3 )--, said B 1 is (CH 3 ) 2 CH--, said C 1 is CH 3 --, (CH 3 ) 2 CH--, (CH 3 ) 2 CHCH 2 --, CH 3 CH 2 CH(CH 3 )--, cyclohexylmethyl, benzyloxymethyl, benzyl or a substituted benzyl (said substituted benzyl means benzyl or phenyl substituted by at least one substituent selected from a straight-chain or branched lower alkoxy having 1 to 6 carbon atoms, cycloalkoxy having 3 to 7 carbon atoms, benzyloxy and halogen), said D 1 is CH 3 --, (CH 3 ) 2 CH--, (CH 3 ) 2 CHCH 2 --, CH 3 CH 2 CH(CH 3 )--, hydroxymethyl or benzyl (where C 1 is benzyl, ortho-fluorobenzyl, or meta-fluorobenzyl, D 1 is not benzyl and hydroxymethyl), said E 1 is --(CH 2 ) 3 --, said F 1 is (CH 3 ) 2 CH--, (CH 3 ) 2 CHCH 2 -- or CH 3 CH 2 CH(CH 3 )--, said G 1 is (CH 3 ) 2 CH--, said H 1 is (CH 3 ) 2 CH--, (CH 3 ) 2 CHCH 2 -- or CH 3 CH 2 CH(CH 3 )--, and, said I 1 is (CH 3 ) 2 C(OH)--.

References Cited (Backward Citations)

EP0352092A2 Cited

JPH02138296A Cited

JPH0322995A Cited

JPH0344398A Cited

EP0443719A1 Cited

JPH03220199A Cited

EP0500264A1 Cited

JPH0539204A Cited

EP0507484A1 Cited

JPH05279384A Cited

EP0581429A2 Cited

JPH0665291A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage	Window Opens	Payment Deadline	Surcharge Period Until	Estimated Fee	Status
3.5 Years (Year 4)	2000-12-15	2001-06-16	2001-12-16	$2000.00	Window Closed / Lapsed
7.5 Years (Year 8)	2004-12-15	2005-06-16	2005-12-16	$3760.00	Window Closed / Lapsed
11.5 Years (Year 12)	2008-12-15	2009-06-16	2009-12-16	$7700.00	Window Closed / Lapsed

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