Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-06-09
1999-02-02
Chang, Ceila
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514370, 514321, 514322, 514323, 514324, 514326, 546193, 546196, 546197, 546198, 546199, 546201, 546202, 546208, 546210, A61K 31445, C07D40112, C07D40114
Patent
active
058665897
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
1. Field of the Invention
The Anti-AIDS Amines (I) are useful in treating individuals who have AIDS as well as those individuals who are HIV positive but do not as yet have AIDS.
2. Description of the Related Art
An estimated one to one and one-half million people in the United States are infected with a human retrovirus, the human immunodeficiency virus type I (HIV-1) which is the etiological agent of acquired immunodeficiency syndrome, AIDS, see Science, 661-662 (1986). Of those infected, an estimated two hundred and fifty thousands people will develop AIDS in the next five years, see Science, 1352-1357 (1985). On Mar. 20, 1987, the FDA approved the use of the compound, AZT (zidovudine), to treat AIDS patients with a recent initial episode of pneumocystis carinii pneumonia, AIDS patients with conditions other than pneumocystis carinii pneumonia or patients infected with the virus with an absolute CD4 lymphocyte count of less than 200/mm.sup.3 in the peripheral blood. AZT is a known inhibitor of viral reverse transcriptase, an enzyme necessary for human immunodeficiency virus replication.
U.S. Pat. No. 4,724,232 claims a method of treating humans having acquired immunodeficiency syndrome utilizing 3'-azido-3'-deoxy-thymidine (azidothymidine, AZT).
Following the discovery of the anti-HIV activity of AZT, much effort has been focused on a wide variety of other dideoxynucleoside analogues in the search for superior agents. In the case of the 2',3'-dideoxy series, ddC and ddI have shown potent activity against HIV in vitro and have been evaluated in clinical trials, see Drug News & Perspectives, 5(3) 153-169 (1992) in particular page 160. The FDA has approved ddI for the treatment of HIV-1 infections in adults and pediatrics patients who are intolerant to, or whose health has significantly deteriorated while on, AZT treatment, see AIDS Research and Human Retroviruses, 8(6), 963-990, 1992 (1992) in particular page 966.
It is known in the art that certain antibiotics and polyanionic dyes inhibit retrovirus reverse transcriptase.
International Publication No. WO 88/08424 (U.S. Pat. No. 5,120,843) disclosed compounds which can be represented as see the compounds of formulas (I) and (III). None of those compounds were disclosed as having the utility set forth in this invention. In U.S. Pat. No. 5,120,843 it was disclosed that the compounds of formula (I) of International Publication No. WO 88/08424 were useful against AIDS.
Many publications have reported the ability of various sulfated compounds to inhibit virus replication, including HIV.
Nature 343, 470 (1990) and Science 250, 1411 (1990) discloses potent benzodiazepin type reverse transcriptase inhibitors. The compounds of the present invention are not benzodiazepin type compounds.
U.S. Pat. Nos. 3,146,234 and 3,188,313 disclose a number of compounds which can be represented as: substituted or not) attached to the piperazinyl moiety. Further, the compounds of the present invention require that the heteroaryl group must be substituted.
VINITI, 3979-82 (1982) in Russian and Chem. Abst. 100(7) 51549b (1984) discloses a compound which can be represented as compounds have quinoline structure or any bicyclic structure attached to the piperazinyl, piperidinyl or aminopiperidinyl moiety.
JP 01132579 (1987) discloses compounds which can be represented as where n is 1-5 which differs from the claimed compounds in that the claimed compounds do not permit any linking group between the piperazinyl moiety and the heteroaryl group.
Indian J. Chem. Sect. B, 17B(3), 246-9 (1979) and Indian J. Med. Res., 63(10), 1418-25 (1975) disclose compounds which can be represented as: phenyl) none of the compounds showed any noteworthy (CNS) biological activity. The Indian J. Med. Res., 63(10), 1418-25 (1975) reported some of the compounds they prepared had anti-viral activity against Semliki forest virus (SFV) in mice. One compound, a dihydroisoquinolin was tested and found to be inactive against new castle disease virus in chick embryo. These compounds diffe
REFERENCES:
patent: 3686188 (1972-08-01), Huebner
patent: 5489593 (1996-02-01), Palmer et al.
patent: 5688610 (1997-11-01), Palmer et al.
May Paul D.
Poel Toni-Jo
Romero Donna L.
Thomas Richard C.
Chang Ceila
Pharmacia & Upjohn Company
Stein Bruce
LandOfFree
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