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© Publication number : 0 4 6 4
009
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PATENT A P P L I C A T I O N
(2j) Application number: 91830284.5
© int. ci.5: C07K 5/00, A61K 3 7 / 0 2
(22) Date of filing : 26.06.91
(§) Priority : 28.06.90 IT 4810290
(43) Date of publication of application :
02.01.92 Bulletin 92/01
@ Designated Contracting States :
AT BE CH DE DK ES FR GB GR LI LU NL SE
(88) Date of deferred publication of search report :
17.06.92 Bulletin 92/25
(R) Applicant : Sigma-Tau Industrie
Farmaceutiche Riunite S.p.A.
47, Viale Shakespeare
1-00144 Rome (IT)
(72) Inventor : Marzi, Mauro
Via Antonio Ciamarra, 158
1-00169 Roma RM (IT)
Inventor : Foresta, Piero
Via L. Sturzo, 46
I-00040 Pomezia RM (IT)
Inventor : Minetti, Patrizia
Via Nanchino, 28
1-00144 Roma RM (IT)
Inventor : Tinti, Maria Ornella
Via Ernesto Basile, 81
1-00182 Roma RM (IT)
(74) Representative : Cavattoni, Fabio et al
Cavattoni & Raimondi Viale dei Parioli, 160
1-00197 Roma (IT)
(54) Oligopeptide derivatives of ipoxantine endowed with immunomodulating activity and
pharmaceutical compositions containingsame.
(57)
Ipoxantine derivatives of general formula (I) :
OH
O
D
(CH^n- O - C - A
CO
^
O
©
both as racemate and chiral forms and the salts thereof with pharmacologically acceptable cations,
wherein n is an integer comprised between 2 and 6, and A is the residue of a dipeptide, tripeptide,
tetrapeptide and pentapeptide selected, respectively, from the groups consisting of :
(a) glycyl-aspartate, alanyl-glycine, glycyl-glycine, aspartyl-arginine, leucyl-arginine ;
(b) arginyl-lysyl-aspartate, aspartyl-lysyl-arginine, lysyl-prolyl-arginine, prolyl-prolyl-arginine, lysylhistidyl-glycinamide, prolyl-phenilalanyl-arginine, phenylalanyl-prolyl-arginine ;
(c) arginyl-lysyl-aspartyl-valine, valyl-aspartyl-lysyl-arginine, threonylvalyl-leucyl-histidyne ; and
(d) arginyl-lysyl-aspartyl-valyl-tyrosine ; are endowed with immunomodulating activity and can be
formulated in orally or parenterally administrable pharmaceutical compositions.
CO
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DOCUMENTS CONSIDERED TO BE RELEVANT
Relevant
Citation of document with indication, where appropriate,
Category
to claim
of relevant passages
1-1U
EP-A-0 077 460 (CO PHARMA CORPORATION) Z7 April
1983
* page 1, line 1 - page 2, line 9 *
* page 3, line 24 - page 4, line 15 *
* examples 9-10 *
* claims 14-15 *
IL FARMAC0
vol. 45, no. 1. 1990. ROME
pages 39 - 47;
STRADI ET AL: 'Synthetic biological response
modifiers; Part 1. Synthesis and
Immunomodulatory properties of some N2-(w-(hypox
ant1n-9-yl)al koxycarbonyl )-l-arg1 nines '
* The whole document ( esp. p. 40 1. 12 ) *
i-10
EP-A-0 260 588 (SIGMA-TAU INDUSTRIE
FARMACEUTICHE RI UNITE) 23 March 1988
* page 2 - page 3 *
L-10
APPUCATION qnt. CI.S )
LU/K5/UU
A61K37/02
SEARCHED (Int. CI.S )
CU/K
C07D
The present search report has been drawn up for all claims
Dateof cunpMioa oftae tearta
Place of learca
16 APRIL 1992
THE HAGUE
KUKSNfcK
t.
T : theory or principle underlying toe invention
E : earlier patent document, but published on, or
after the filing date
D : document died in the application
L : document cited for other reasons
&: member of the same patent family, corresponding
document
CATEGORY OF CITED DOCUIVUfNla
X: particularly relevant if taken alone
Y: particularly relevant if combined with another
document of the same category
A: technological background
O : non-written disclosure
P : intermediate document
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