Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Reexamination Certificate
2000-03-23
2002-09-17
Travers, Russell (Department: 1617)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
C514S508000, C514S229200
Reexamination Certificate
active
06451851
ABSTRACT:
The invention relates to an antivirally pharmaceutical composition exerting an enhanced antiviral action and/or decreased side effect(s).
Antivirally active agents used e.g. for the treatment of HIV viral infections induce a general cellular injury in addition to the primary virus-injuring effect. Consequently, in a number of cases the chance of survival of the organism weakened also by the viral infection is hardly improved.
The hydroximic acid derivatives of formula (I)
wherein
R
1
means hydrogen or C
1-5
alkyl group;
R
2
represents hydrogen; C
1-5
alkyl group; C
3-8
cycloalkyl group; or phenyl group optionally substituted by hydroxyl or phenyl group; or
R
1
and R
2
together with the adjacent nitrogen atom form a 5 to 8 membered ring optionally containing additional nitrogen, oxygen or sulfur atom(s); and said ring can be condensed with an other alicyclic or heterocyclic ring, preferably with benzene, naphthalene, quinoline, isoquinoline, pyridine or pyrazoline ring; furthermore if desired and possible, nitrogen and/or sulfur as heteroatom(s) are present in the form of an oxide or dioxide;
R
3
stands for hydrogen or phenyl, naphthyl or pyridyl group optionally substituted by one or more halogen(s) or C
1-4
alkoxy group(s);
Y means hydrogen; hydroxyl group; C
1-24
alkoxy group optionally substituted by amino group; C
2-24
polyalkenyloxy group containing 1 to 6 double bond(s);
C
1-25
alkanoyl group; C
3-9
alkenoyl group; or a group of formula R
7
—COO—, wherein R
7
is a C
2-30
polyalkenyl group containing 1 to 6 double bond(s);
X represents halogen; amino group; or C
1-4
alkoxy group;or
X and B together form an oxygen atom; or
X and Y together with the adjacent carbon atoms and the interjacent —NR—O—CH
2
— group form a ring of formula (a),
wherein
Z means oxygen or nitrogen;
R means hydrogen; or
R and B together represent a chemical bond;
A stands for C
1-4
alkylene group or a chemical bond; or a group of the formula (b),
wherein
R
4
means hydrogen; C
1-5
alkyl group; C
3-8
cycloalkyl group; or a phenyl group preferably substituted by halogen, C
1-4
alkoxy or C
1-5
alkyl group;
R
5
means hydrogen; C
1-4
alkyl group; or a phenyl group;
m is 0, 1 or 2; and
n is 0, 1 or 2,
The U.S. Pat. No. 4,308,399 discloses compounds belonging to the scope of hydroximic acid derivatives of formula (I), which are useful for treatment of the diabetic angiopathy.
The EP-PS No. 417,210 describes hydroximic acid halides, which also fall into the scope of compounds of formula (I), possess a selective &bgr;-blocking effect and are useful for treatment of the diabetic angiopathy.
The Hungarian published patent application No. T/66350 discloses a number of other hydroximic acid derivatives being within the scope of compounds of formula (I). These known substances are useful in the therapy of vascular complications, particularly of diabetes mellitus.
It is known from the PCT Application No. WO/9713504 that hydroximic acid derivatives of formula (I) are useful for the prevention and treatment of disorders of mitochondrial origin. According to an investigation discussed in the description rats were treated with zidovudine (AZT), an antiviral nucleoside analogue useful in the therapy of AIDS, in order to correct the “defect” of the mitochondrial genom. This method resulted in animals suffering from hereditary cardiomyopathy. It was concluded from this investigation that the studied compounds of formula (I) diminished or prevented the mitochondrial membrane-injuring effect of zidovudine. However, it cannot be concluded from this establishment in any way that compounds of formula (I) were useful to diminish or to eliminate the unfavourable side effect of all known antivirally active substances.
REFERENCES:
patent: WO 97/13504 (1997-04-01), None
patent: 97 13504 (1999-04-01), None
Westarp et al, 120CA:153741, Sep. 23, 1993.*
Malley S.D. et al, Proc. Natl. Acad. Sci. U.S.A., 1994, 91/3, (11017-11021), XP000572692 USA see p. 11020, col. 1, paragraph 3.
Birch & Stewart Kolasch & Birch, LLP
N-Gene Research Laboratories Inc.
Travers Russell
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