Abstract:
PROBLEM TO BE SOLVED: To provide a method for identifying anti-HIV therapeutic compounds substituted with carboxyl ester or phosphonate ester groups. SOLUTION: Libraries of such compounds are screened optionally using the novel enzyme GS-7340 Ester Hydrolase. Compositions and methods relating to GS-7430 Ester Hydrolase also are provided. In one embodiment, this invention comprises following steps: (a) identifying a non-nucleotide prototype compound, (b) substituting the prototype compound with phosphonate-containing group to form a candidate compound, and (c) determining the anti-HIV activity of the candidate compound. COPYRIGHT: (C)2009,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a new method for screening prodrugs of methoxyphosphonate nucleotide analogues to identify prodrugs selectively targeting desired tissues with antiviral or antitumor activity. SOLUTION: The method leads to the identification of new mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, and the ester-amidates of PMPA includes compounds of structure (5a) having specified substituent groups. Compositions of these new compounds in pharmaceutically acceptable excipients and their use in therapy and prophylaxis are provided. An improved method for the use of magnesium alkoxide for the preparation of starting materials and compounds for specific use is also provided. COPYRIGHT: (C)2010,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a compound useful as an antiproliferative agent, an apoptotic agent, an anti-HPV agent and a topical anti-HPV agent. SOLUTION: This compound is represented by formula (I). Pharmaceutical compositions containing an effective amount of the compound described in formula (I) or its pharmaceutically acceptable salts and pharmaceutically acceptable carriers are also included therein. COPYRIGHT: (C)2011,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a form of compound, which can facilitate manufacturing processes for therapeutic dosage forms.SOLUTION: This invention relates to: an organic acid salt of compound (1) and/or its tautomers and solvates thereof; composition comprising a carbohydrate in which storage stability of the salt is enhanced; and a method for the treatment of a patient having a hematological malignancy, comprising administering to the patient a therapeutically effective amount of the compound 1 and/or its salt, tautomers, and solvates.
Abstract:
PROBLEM TO BE SOLVED: To provide a new method for screening prodrugs of methoxyphosphonate nucleotide analogues to identify prodrugs selectively targeting desired tissues having antiviral activity or antitumor activity. SOLUTION: The method has led to the identification of new mixed ester-amidates of PMPA for retroviral therapy or hepadnaviral therapy, and the ester-amidates of PMPA includes compounds of a structure (5a) having substituent groups as defined herein. Compositions of the new compounds in pharmaceutically acceptable excipients and their use in therapy and prophylaxis are provided. Also provided is an improved method for the use of magnesium alkoxide for the preparation of starting materials and compounds for use herein. COPYRIGHT: (C)2009,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a compound of formula I, wherein L 1 and L 2 are each independently an amino acid or polypeptide residue bound to the phosphorus atom of the compound through an amidate bond, or an oxyester, a thioester, a substituted or un-substituted amine, or OH, but one or both of L 1 and L 2 are amino acids or polypeptide residues; and a carboxyl group bound to amidate N with five or less atoms is esterified or amidated, and the stereoisomer or salt of the compound, to provide their production method, and to provide their uses. SOLUTION: The compound of formula I, and the stereoisomer or salt of the compound, their production methods, and their uses are provided. COPYRIGHT: (C)2007,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a new method for screening the prodrugs of methoxyphosphonate nucleotide analogs for identifying the prodrugs selectively targeting desired tissues with antiviral activity or antitumor activity. SOLUTION: This method for selecting and producing the prodrugs is provided by inducing identification of the new mixed ester amidates of PMPA ä9-[2-(phosphonomethoxy)propyl]adenine} for treating retrovirus or hepadnavirus, and the ester amidates of the PMPA contain a compound of a structure (5a) having substituent groups prescribed in this specification. The composition of these new compounds in a pharmaceutically acceptable excipient and use of them in treatment and prophylaxis are provided. Further, the improved method for using a magnesium alkoxide for preparing a starting material and the compounds for the uses described in the specification is provided. COPYRIGHT: (C)2011,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a therapeutic antiviral preparation having improved pharmacological characteristics, a dosing regimen for a new antiviral compound not more troublesome than the conventional regimen, or an assay method determining the presence or absence of, or the amount of virus-inhibition. SOLUTION: The invention relates not only to a phosphorus-substituted compound having antiviral activity, a composition containing such compound and a therapeutic method including a process for dosing such compound, but also to a useful process and an intermediate for preparing such compound. The invention provides new phosphonate-containing analogues of the antiviral compounds. These analogues have all of usefulness of these parent compounds, and provide accumulation of them in cells described below, at need. The compounds of the invention can inhibit RNA-dependent RNA polymerase of retro virus or reverse transcriptase, and therefore, can inhibit duplication of virus. COPYRIGHT: (C)2007,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a new nucleotide analog exhibiting an antitumor/antineoplastic activity, an antimicrobial activity of a wide spectrum and other desired activities. SOLUTION: The invention provides a compound of formula: B-Z-PO(-L 1 )-L 2 wherein -Z- is exemplified by -CH 2 -O-CH 2 -CH 2 -; B is exemplified by adenin-9-yl; and L 1 and L 2 are each exemplified by -NHCH(CH 3 )-CO(O)OCH 2 C 6 H 5 , and a stereoisomer and salt of the compound, a method for producing the compound, etc., and use of the compound, etc. COPYRIGHT: (C)2007,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a nucleotide analog compound having antiviral activity. SOLUTION: A compound represented by formula Ib, its stereoisomer and salt have antiviral activity (wherein, X 1 indicates O or S; # indicates a carbon having optical activity; B indicates a residue of a nucleic acid base; and L 1 indicates a group such as alkoxycarbonylmethoxy and acylmethoxy). COPYRIGHT: (C)2006,JPO&NCIPI