US2004152751A1PendingUtilityA1
Pyrazolidinol compounds
Priority: Jun 29, 1999Filed: Nov 6, 2003Published: Aug 5, 2004
Est. expiryJun 29, 2019(expired)· nominal 20-yr term from priority
A61P 37/06A61P 31/08A61P 5/38A61P 31/12A61P 31/18A61P 7/06A61P 3/10A61P 7/00A61P 37/02A61P 25/28A61P 29/00A61P 15/08A61K 31/415A61K 31/4152A61K 31/522A61K 31/495A61K 45/06A61K 31/70A61K 31/7076C07D 231/30C07D 231/32A61P 21/00A61K 31/55A61K 31/551A61P 21/04A61P 1/04
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Claims
Abstract
The invention provides the use of an optionally hydroxyl-protected 4-hydroxy or hydroperoxy-3,5-dioxopyrazolidine or an equivalent wherein a pyrazolidine ring attached oxygen is replaced by a sulphur, or a physiologically acceptable salt thereof, for the manufacture of a medicament for use in drug therapy or prophylaxis. Additionally, the invention provides a method of combating HIV infection which comprises administering to an HIV-infected patient a T-lymphocyte growth suppressing agent, preferably a pyrazolidinol, in an amount sufficient to suppress T-lymphocyte growth in said patient for a period sufficient to reduce the T-lymphocyte concentration in lymph nodes in said patient.
Claims
exact text as granted — not AI-modified1 . The use of an optionally hydroxy-protected 4-hydroxy or hydroperoxy-3,5-dioxo-pyrazolidine or an equivalent wherein a pyrazolidine ring attached oxygen is replaced by a sulphur, or a physiologically acceptable salt thereof, for the manufacture of a medicament for use in therapy or prophylaxis.
2 . A method of treatment of the human or non-human body to combat an inflammatory or viral disease, which method comprises administering to said body an optionally hydroxy-protected 4-hydroxy or hydroperoxy-3,5-dioxo-pyrazolidine or an equivalent wherein a pyrazolidine ring attached oxygen is replaced by a sulphur, or a physiologically acceptable salt thereof.
3 . A method as claimed in claim 2 comprising administering said optionally hydroxy-protected 4-hydroxy or hydroperoxy-3,5-dioxo-pyrazolidine or an equivalent wherein a pyrazolidine ring attached oxygen is replaced by a sulphur, or a physiologically acceptable salt thereof in combination with another antiviral agent.
4 . A method as claimed in claim 3 wherein said additional antiviral agent is at least one antiviral agent selected from a reverse transcriptase inhibitor and a protease inhibitor.
5 . A method as claimed in claim 3 wherein said additional antiviral agent is an agent selected from the group of AZT, indinavir, nevirapine and 2′,3′-dideoxyinosine (daI).
6 . A method as claimed in any of claims 2 to 5 wherein said disease is a disease caused by a pathogen from the group of togaviridea, reoviridea, picornaviridea, hantaviridea, orthomyxoviridea, paramyxoviridea, mononegaviralis, viral hepatitis, haemorrhagic fevers, flaviviridea, viral encephalitis, coronaviridea, calciviridea, adenoviridea, papovaviridea, arboviridea, pox virus, rhabdoviridea, arenaviridea HIV-1, HIV-2, HTLV-I, HTLV-II and herpes viruses.
7 . A method of combatting HIV infection which comprises administering to an HIV-infected patient a T-lymphocyte growth suppressing agent in an amount sufficient to suppress T-lymphocyte growth in said patient for a period sufficient to reduce the T-lymphocyte concentration in the lymphatic system in said patient by at least 25% said administration being repeated at intervals of at least 3 months.
8 . A method of combatting HIV infection as claimed in claim 6 wherein said T-lymphocyte growth suppressing agent is a pyrazolidinol.
9 . A method as claimed in claim 7 or claim 8 wherein said interval is at least 9 months.
10 . A method as claimed in any of claims 7 to 9 wherein a 4-hydroxy or hydroperoxy-3,5-dioxo-pyrazolidine or an equivalent wherein a pyrazolidine ring attached oxygen is replaced by a sulphur, or a physiologically acceptable salt thereof is administered in a daily dose of 0.1 to 10 μmol/kg bodyweight.
11 . A pharmaceutical composition comprising an optionally hydroxy-protected 4-hydroxy or hydroperoxy-3,5-dioxo-pyrazolidine or an equivalent wherein a pyrazolidine ring attached oxygen is replaced by a sulphur, or a physiologically acceptable salt thereof, together with at least one pharmaceutically acceptable carrier or excipient.
12 . A pharmaceutical composition as claimed in claim 11 additionally comprising another antiviral agent.
13 . An optionally hydroxy-protected 4-hydroxy or hydroperoxy-3,5-dioxo-pyrazolidine or an equivalent wherein a pyrazolidine ring attached oxygen is replaced by a sulphur, or a physiologically acceptable salt thereof.
14 . A compound of formula I
(where each X 2 , which may be the same or different is O or S,
X 1 is 0, 00 or S,
R 1 is hydrogen or a hydroxyl or thiol protecting group,
R 2 is hydrogen or a carbon attached organic group containing up to 10 carbons, and each of
Ar 1 and Ar 2 , which may be the same or different, is a homo or heterocyclic aromatic group) or a salt thereof.
15 . A compound of claim 14 wherein R 1 , R 2 , X 1 , X 2 , Ar 1 and Ar 2 are as defined in claim 14 , providing that if X 1 and each X 2 is 0, the remaining groups do not correspond to the following table:
R 2
R 1
Ar 1
Ar 2
H
H
H
C 6 H 5
H
H
C 6 H 5
C 6 H 5
CH 3
H
H
C 6 H 5
CH 3
H
H
—CH 2 —C 6 H 5
CH 3
H
H
p-CH 3 O—C 6 H 4
CH 3
H
H
p-Cl—C 6 H 4
C 2 H 5
H
H
C 6 H 5
C 2 H 5
H
C 6 H 5
C 6 H 5
C 2 H 5
H
H
N-methyl-piperidin-4-yl
iC 3 H 7
H
H
C 6 H 5
nC 3 H 7
H
H
C 6 H 5
nC 3 H 7
H
C 6 H 5
C 6 H 5
nC 3 H 7
H
H
5-phenyl-triazol-1-yl
C 4 H 9
H
H
C 6 H 5
C 4 H 9
H
C 6 H 5
C 6 H 5
C 4 H 9
H
C 6 H 5
p-OH—C 6 H 4
C 4 H 9
OH
C 6 H 5
C 6 H 5
C 4 H 9
OH
C 6 H 5
p-OH—C 6 H 4
C 4 H 9
H
H
N-methyl-piperidin-4-yl
C 5 H 11
H
H
C 6 H 5
C 5 H 11
H
C 6 H 5
C 6 H 5
C 5 H 11
H
H
5-phenyl-triazol-1-yl
Cyclohexyl
H
H
C 6 H 5
Phenyl
H
H
C 6 H 5
Phenyl
H
C 6 H 5
C 6 H 5
Benzyl
H
H
C 6 H 5
Benzyl
H
C 6 H 5
C 6 H 5
CH 3 CO(CH 2 ) 2
H
C 6 H 5
C 6 H 5
(CH 3 ) 2 C═CH—
H
C 6 H 5
C 6 H 5
(CH 2 ) 2 C═CHCH 2
H
C 6 H 5
C 6 H 5
C 6 H 5 SCH 2 CH 2
H
C 6 H 5
C 6 H 5
Pyrrolidin-1-yl
H
C 6 H 5
C 6 H 5
Piperidin-1-yl
H
C 6 H 5
C 6 H 5
Morpholin-4-yl
H
C 6 H 5
C 6 H 5
16 . A compound as claimed in claim 14 or claim 15 wherein one X 2 group is S.
17 . A compound as claimed in any of claims 14 to 16 wherein X 1 is 0.
18 . A compound as claimed in any of claims 14 to 17 wherein R 1 is acyl.
19 . A compound as claimed in any of claims 14 to 18 wherein R 1 is hydrogen.
20 . A compound as claimed in any of claims 14 to 19 wherein one of Ar 1 and Ar 2 is Ph and the other is 4-hydroxyphenyl.
21 . A compound as claimed in claim 14 wherein each X 2 is oxygen, R 1 X 1 is HO or CH 3 CO.O, each of Ar 1 and AR 2 , which may be the same or different is optionally halo or hydroxy substituted phenyl, and R 2 is C 1-6 alkyl or alkenyl, or a salt thereof.
22 . A compound as claimed in any of claims 14 to 21 for use as a medicament.
23 . 4-Butyl-4-hydroxy-2(p-hydroxyphenyl)-1-phenyl-3,5-pyrazolidinedione for use as a medicament.
24 . A method of treatment of the human or non-human body to combat an autoimmune disease or tissue rejection, which method comprises administering to said body an optionally hydroxy-protected 4-hydroxy or hydroperoxy-3,5-dioxo-pyrazolidine or an equivalent wherein a pyrazolidine ring attached oxygen is replaced by a sulphur, or a physiologically acceptable salt thereof.
25 . A method of claim 24 wherein said disease is selected from Addison's disease, Behcet's syndrome, diabetes mellitus, haemolytic anaemia, lupus erythematosus, multiple sclerosis, myasthenia gravis, pernicious anaemia, polyglandular deficiency, polymyositis, dermatomyositis, testicular failure, thrombocytopenic purpura, Crohns disease, ulcerative colitis and rheumatoid arthritis.
26 . A method of claim 24 wherein said tissue rejection is tissue rejection following transplant.Join the waitlist — get patent alerts
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