| 摘要 |
#CMT# #/CMT# Use of at least a compound (I) for preparing a pharmaceutical composition for preventing and/or treating viral infection, is claimed. #CMT# : #/CMT# Use of at least a compound of formula (A-B1-C1) (I) for preparing a pharmaceutical composition for prophylaxis and/or treatment of viral infection, is claimed. A : quinoline or quinoline-type group; B1 : single amino acid (preferably aspartic acid), peptide or polypeptide (preferably aspartic acid and valine) with a sequence of amino acids (preferably valine-aspartic acid sequence or valine-alanine-aspartic acid), preferably peptide with di-, tri- or tetra- polypeptide sequence; and C1 : O-phenoxy. Independent claims are included for: (1) an antiviral composition comprising (I), and another antiviral agent, preferably antiretroviral agent; and (2) a combination comprising (I) and another antiviral agent, preferably other antiretroviral agent, in which the compounds (I) and other antiretroviral agent are separated from one another. . #CMT#ACTIVITY : #/CMT# Virucide; Antiinflammatory; Hepatotropic; Respiratory-Gen.; Anti-HIV. #CMT#MECHANISM OF ACTION : #/CMT# Transcriptase inhibitor. #CMT#USE : #/CMT# (I) is useful for preparing the pharmaceutical composition for preventing and/or treating viral infection caused by a DNA virus or a RNA virus, to prevent and/or inhibit viral replication in an animal or human infected by the virus, for preventing and/or inhibiting the synthesis of viral proteins in an animal or a human infected by the virus, to prevent and/ or inhibit the increased cell death in an animal infected with the virus, and for preventing and/or inhibiting increased death of T lymphocytes, preferably increased T cell cluster of differentiation (CD)4 +>death, where the virus is: flaviviridae (flavivirus genus such as dengue virus and yellow fever virus), orthomyxovirus represented by influenza virus, paramyxoviridae (morbillivirus genus, measles virus and pneumovirus genus of human respiratory syncytial virus and metapneumovirus), reoviridae (rotavirus genus), picornaviridae (enterovirus genus represented by poliovirus and responsible virus of viral meningitis, aphthovirus genus of virus of the foot-and-mouth disease and rhinovirus genus), filoviridae (Ebola virus), arenaviridae (Lassa virus), rhabdoviridae (rhabdovirus genus comprising rabies virus and vesiculovirus genus, and vesicular stomatitis virus), togaviridae (Rubivirus genus including rubella virus), poxviridae (vaccinia virus and smallpox), herpesviridae (herpes virus, and varicella zoster virus), hepatitis viruses A, B, C, D and E, coronaviridae (coronavirus genus e.g. severe acute respiratory syndrome virus), retrovirus (lentivirus genus and oncovirus genus e.g. human T-lymphotropic virus type I and HIV-1 or HIV-2), and simian retrovirus (preferably lentivirus simian), which is simian immunodeficiency virus (SIV); the viral infection is viral encephalitis, viral meningitis, foot and mouth disease, influenza, yellow fever, viral respiratory infections, infantile diarrhea, hemorrhagic fever, polio, rabies, measles, rubella, chickenpox, smallpox, herpes zoster, genital herpes, hepatitis A, B, C, D and E, severe acute respiratory syndrome, leukemia and paralysis caused by human T-cell lymphotropic virus type 1 (HTLV-1), and infections caused by HIV virus, preferably AIDS; the viral infection is correlated with an increase in cell death in an animal, preferably an increase in T cell death, and an increase in CD4 +>T-cell death, from a human infected by the virus; and the animal is a non-human mammal, preferably monkey or cat. The antiviral combination or composition is useful: as medicine as antiviral agent, preferably antiretroviral agent; to prevent and/or treat viral infection, preferably to prevent or inhibit viral replication in animal or human; prevent and/or inhibit the increased cell death, preferably the increased CD4 +>T-cell death, in an animal or a human infected by a virus (all claimed). Tests details are described but no results given. #CMT#ADVANTAGE : #/CMT# (I) exhibits synergistic effect with antiretroviral agent, and is non-toxic. #CMT#ORGANIC CHEMISTRY : #/CMT# Preferred Components: (I) is quinoline compound of formula (II). R1-R4 : H, alkyl, alkoxy, F, Cl, carbonyl, aryl carbonyl or amino. #CMT#[Image]#/CMT# #CMT#PHARMACEUTICALS : #/CMT# Preferred Components: The other antiviral agent is: transcriptase inhibitors; viral protease inhibitors (or antiproteases); inhibitors of the fusion of viral envelope with the cell membrane; inhibitors of receptor or co-receptor; anti-sense oligonucleotides; integrase inhibitors, and molecules targeting other steps of viral multiplication, preferably at least a transcriptase inhibitor: and/or at least a viral protease inhibitor, preferably transcriptase inhibitors; viral protease inhibitors. The transcriptase inhibitor is reverse transcriptase inhibitor, preferably reverse transcriptase inhibitor of HIV virus. The reverse transcriptase inhibitor is azidothymidine (preferred) or zidovudine, didanosine or ddI, zalcitabine or ddC, stavudine or d4T, lamivudine or 3TC, abacavir or ABC, and territricitabine or FTC, nevirapine, efavirenz, delavirdine and tenofovir or bis-POC-PMPA. The viral protease inhibitor is: HIV virus protease inhibitor; and indinavir (preferred) or IDV, Nelfinavir or NLFN, saquinavir or SQN, ritonavir or RTN, amprenavir and lopinavir. (I) and another antiretroviral agent are present in two separate compositions. (I) and another antiretroviral agent are formulated for a simultaneous administration at one time. (I) is formulated for sequential administration before and/or after administration of another antiretroviral agent. (I) and/or another antiretroviral agent further comprise excipients, diluents and/or adjuvants. Preferred Composition: The pharmaceutical composition further comprises: excipients, diluents and/or adjuvants; and other antiviral agent, preferably other antiretroviral agent. The antiviral composition further comprises excipients, diluents and/or adjuvants. The pharmaceutical composition is administered to the animal or human before the human or animal not exposed to the virus and/or during exposure to the virus and/or after exposure to virus, preferably within 48 hours after the animal or human is exposed to virus. #CMT#ADMINISTRATION : #/CMT# Administration of (I) is enteral, parenteral (intravenous, intramuscular or subcutaneous), transcutaneous, cutaneous, oral, mucosal, preferably oral-transmucosal, nasal, ophthalmic, otologic, vaginal, rectal, intragastric, intracardiac, intraperitoneal, intratracheal or intrapulmonary (claimed). Administration of (I) is 15-50 mg/kg. |
