US2003013748A1PendingUtilityA1
Pharmaceutical compositions comprising tyrphostins
Est. expiryAug 14, 2016(expired)· nominal 20-yr term from priority
A61P 39/00A61K 31/277A61K 31/427A61K 31/415A61K 31/4406
42
PatentIndex Score
0
Cited by
0
References
0
Claims
Abstract
Compounds useful for countering undesired toxic effects to cells, tissues or organs having formula (I) wherein: Ar is a group of formulae (i) or (ii), n is O or, when Ar has formula (i) above, then n may also be 1, R is CN, —GC(S)NH2, —C(O)NHR3 or, when R1 is 4—NO2 and R2 is H or 3—OH, then R may also be a group of formulae (iii), (iv), (v), (vi) where R3 is H, phenyl, phenyl(lower alkyl) or pyridylmethyl; R1 and R2 are each independently H, OH, NO2 or, when R is CN, also CH3, F, or CF3, provided that both R1 and R2 are simultaneously H.
Claims
exact text as granted — not AI-modified1 . Pharmaceutical compositions for countering damage to cells or tissue comprising an effective amount of a compound of the general formula
wherein:
Ar is a group of the formulae
n is 0 or, when Ar has the formula (i) above, then n may also be 1,
R is CN, —C(S)NH 2 , —C(O)NHR 3 or, when R 1 is 4-NO 2 and R 2 is H or 3-OH, then R may also be a group of the formula
where R 3 is H, phenyl, phenyl(lower alkyl) or pyridylmethyl;
R 1 and R 2 are each independently H, OH, NO 2 or, when R is CN, also CH 3 , F, or CF 3 , provided that both R 1 and R 2 arc not simultaneously H, together with a pharmaceutically acceptable carrier.
2 . Pharmaceutical compositions according to claim 1 , comprising a compound of formula I wherein R is CN, —C(S)NH 2 , —C(O)NHCH 2 C 6 H 5 or a group of the formula
and n is 0, R 1 is 4-NO 2 and R 2 is H.
3 . Pharmaceutical compositions according to claim 1 or 2 , for countering damage caused by a cytotoxic drug.
4 . Pharmaceutical compositions according, to claim 3 for countering damage caused by an anti-neoplastic drug.
5 . Pharmaceutical compositions according to claim 3 or 4 comprising, an effective amount of a compounds of formula I in claim 1 , in combination with a cytotoxic drug.
6 . Pharmaceutical compositions according to any one of claims 3 - 5 , wherein the drug is selected from the group consisting of cisplatin, doxorubicin, cyclophosphamide, mitomycin-C and 5-fluorouracil.
7 . A pharmaceutical composition according to any one of claims 1 - 6 , for countering, myelotoxicity and lymphotoxicity.
8 . Pharmaceutical compositions according to any of the preceding claims in a form suitable for intravenous administration.
9 . Pharmaceutical compositions according to any of the preceding claims in a form suitable for oral administration.
10 . Pharmaceutical compositions according to claim 1 or 2 , for use in ex vivo preservation of cells, tissue or organ.
11 . Pharmaceutical compositions according to claim 1 or 2 , for countering damage caused by an immune mediated or inflammatory response.
12 . A pharmaceutical composition according to any one of claims 1 - 10 , for countering undesired apoptosis.
13 . A method of treatment of an individual for countering damage to cells, tissue or organ, said method comprising administering to the individual an effective amount of a compound of the general formula
wherein:
Ar is a group of the formulae
n is 0 or, when Ar has the formula (i) above, then n may also be 1,
R is CN, —C(S)NH 2 , —C(O)NHR 3 or, when R 1 is 4-NO 2 and R 2 is H or 3-OH, then R may also be a group of the formula
where R 3 is H, phenyl, phenyl(lower alkyl) or pyridylmethyl;
R 1 and R 2 arc each independently H, OH, NO 2 or, when R is CN, also CH 3 , F, or CF 3 , provided that both R 1 and R 2 are not simultaneously H, together with a pharmaceutically acceptable carrier.
14 . A method according to claim 13 , wherein in the compound of formula I, R is CN, —C(S)NH 2 , —C(O)NHCH 2 C 6 H 5 or a group of the formula
and n is 0, R 1 is 4-NO 2 and R 2 is H.
15 . A method according to claim 13 or 14 , wherein the harmful agent is a cytotoxic drug.
16 . A method according to claim 15 , wherein the anti-cytotoxic drug is an anti-neoplastic drug.
17 . A method according to claim 16 , wherein the cytotoxic drug is selected from the group consisting of cisplatin, doxorubicin, cyclophosphamide, mitomycin-C and 5-fluorouracil.
18 . A method according to any one of claims 13 - 17 , for countering myelotoxicity and lymphotoxicity.
19 . A method according to claim 12 , for counting undesired harmful effects of irradiation treatment.
20 . A method according to any one of claims 13 to 19 , wherein the compound of formula I is administered in combination with the cytotoxic drug or irradiation treatment.
21 . A method according to any one of claims 1 to 20 , wherein the compound of formula I is administered prior to the administration of the cytotoxic drug or the irradiation treatment.
22 . A method according to any one of claims 13 to 21 , wherein the compound of formula I is administered intravenously.
23 . A method according to any one of claims 13 to 21 , wherein the compounds of formula I is administered orally.
24 . A method according to claim 13 or 14 , for countering damage caused by an immune mediated or inflammatory response.
25 . A method for ex vivo preservation of organ, tissue or cells comprising contacting the organ, tissue or cells en vivo with a compound of the general formula
wherein:
Ar is a group of the formulae
n is 0 or, when Ar has the formula (i) above, then n may also be 1,
R is CN, —C(S)NH 2 , —C(O)NHR 3 or, when R 1 is 4-NO 2 and R 2 is H or 3-OH, then R may also be a group of the formula
where R 3 is H, phenyl, phenyl(lower alkyl) or pyridylmethyl;
R 1 and R 2 are each independently H, OH, NO 2 or, when R is CN, also CH 3 , F, or CF 3 , provided that both R 1 and R 2 are not simultaneously H, together with a pharmaceutically acceptable carrier.
26 . Compound of the general formula
wherein
Ar is a group of the formula
n is 0, or, when Ar has the formula (i) above, then n may also be 1,
R is —CN, —C(S)NH 2 , —C(O)NHR 3 or, where R 1 is 4-NO 2 and R 2 is H, then R may also be a group of the formulae
R 1 and R 2 are each independently H, OH, NO 2 or, when R is CN, also CH 3 , F or CF 3 ; and
R 3 is H, phenyl, phenyl(lower alkyl) or pyridylmethyl; with the provisos that:
a) when R is CN and n is 0, then
(aa) if one of R 1 and R 2 is H or OH, then the other cannot represent NO 2 ;
(ab) if one of R 1 and R 2 is H or F, then the other cannot represent H or F; and
b) when R 1 is 4-NO 2 , R 2 is H and n is 0, then R cannot represent —C(O)NH 2 or —C(S)NH 2 .
27 . Compound according to claim 26 , wherein R is CN, —C(S)NH 2 , —C(O)NHCH 2 C 6 H 5 or a group of the formula
and n is O,R 1 is 4-NO 2 , R 2 is H and n is 0.Join the waitlist — get patent alerts
Track US2003013748A1 — get alerts on status changes and closely related new filings.
We store only your email — no account needed. See our privacy policy.