摘要:
The present invention concerns nucleotide analogs and their compositions and use. In particular it relates to novel (phosphonomethoxy) methoxy purine/pyrimidine derivatives.
摘要:
The present invention concerns nucleotide analogs and their compositions and use. In particular it relates to novel (phosphonomethoxy) methoxy purine/pyrimidine derivatives.
摘要:
Provided are compounds of the following formulae: A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl and B is a purine or pyrimidine base. A 4'-phosphonomethoxytetrahydrofuranyl-1'-purine-pyrimidine of the formula ##STR2## wherein X and X' are the same or different and are hydrogen or alkyl, Y and Z are the same or different and are hydrogen, hydroxyl or alkyl or Y+Z is an alkenyl, an epoxide or cyclopropyl, and B is a purine or pyrimidine base. A compound of the formula (V) ##STR3## wherein B is cytosine, 5-ethylcytosine, 5-methylcytosine, thymine, uracil, 5-chlorouracil, 5-bromouracil, 5-ethyluracil, 5-iodouracil, 5-propyluracil, 5-vinyluracil, hypoxanthine, xanthine, guanine, 8-bromoguanine, 8-chloroguanine, 8-methylguanine, 8-thioguanine, 3-deazaguanine, purine, 2-aminopurine, 2,6-diaminopurine, adenine, 3-deazaadenine, 8-aminoguanine, 8-hydrazinoguanine, 8-hydroxyguanine, or 2-acetamido-6-diphenylcarbamoylpurine; and the pharmaceutically acceptable salts thereof.
摘要翻译:本发明提供下式的化合物:下式的膦酰甲氧基甲氧基甲氧基甲基嘌呤/嘧啶衍生物,其中X和X'相同或不同,为氢或烷基。 R和R'相同或不同,为氢,烷基,羟基烷基或烷酰基,B为嘌呤或嘧啶碱基。 其中X和X'相同或不同且为氢或烷基,Y和Z相同或不同,为氢,羟基或烷基的4'-膦基甲氧基四氢呋喃基-1'-嘌呤嘧啶, Y + Z是烯基,环氧化物或环丙基,B是嘌呤或嘧啶碱基。 式(V)化合物其中B为胞嘧啶,5-乙基胞嘧啶,5-甲基胞嘧啶,胸腺嘧啶,尿嘧啶,5-氯尿嘧啶,5-溴尿嘧啶,5-乙基尿嘧啶,5-碘尿嘧啶,5-丙基尿嘧啶, 5-乙酰尿嘧啶,次黄嘌呤,黄嘌呤,鸟嘌呤,8-溴鸟嘌呤,8-氯鸟嘌呤,8-甲基鸟嘌呤,8-硫鸟嘌呤,3-脱氮鸟嘌呤,嘌呤,2-氨基嘌呤,2,6-二氨基嘌呤,腺嘌呤,3-脱氮腺嘌呤,8-氨基鸟嘌呤, 8-肼基鸟嘌呤,8-羟基鸟嘌呤或2-乙酰氨基-6-二苯基氨基甲酰基嘌呤; 及其药学上可接受的盐。
摘要:
Provided are compounds of the following formulae: A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl and B is a purine or pyrimidine base. A 4'-phosphonomethoxytetrahydrofuranyl-1'-purine-pyrimidine of the formula ##STR2## wherein X and X' are the same or different and are hydrogen or alkyl, Y and Z are the same or different and are hydrogen, hydroxyl or alkyl or Y+Z is an alkenyl, an epoxide or cyclopropyl, and B is a purine or pyrimidine base.
摘要翻译:本发明提供下式的化合物:下式的膦酰甲氧基甲氧基甲氧基甲基嘌呤/嘧啶衍生物,其中X和X'相同或不同,为氢或烷基。 R和R'相同或不同,为氢,烷基,羟基烷基或烷酰基,B为嘌呤或嘧啶碱基。 其中X和X'相同或不同且为氢或烷基,Y和Z相同或不同,为氢,羟基或烷基的4'-膦基甲氧基四氢呋喃基-1'-嘌呤 - 嘧啶, Y + Z是烯基,环氧化物或环丙基,B是嘌呤或嘧啶碱基。
摘要:
The present invention is directed to compositions of the formula: ##STR1## wherein: R.sub.2 is H, or an alkyl group having 1 to 3 carbon atoms and 0 to 2 hydroxyls;R.sub.3 is H, or hydroxyl;R.sub.4 is H, or forms a hydrolyzable ester or amide with --CO.sub.2 --;R.sub.5 are H, or are taken together to form .dbd.NH; andR.sub.6 comprises an amine, or a group having 1 to 12 carbon atoms and 1 to 3 amine groups. The invention is also directed to methods of inhibiting the activity of neuraminidase using the compounds of the invention.
摘要:
Provided are compounds of the following formulae: A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl; B is a purine or pyrimidine base. optionally R is taken together with X' to complete a cyclic phosphonate having the formula ##STR2## A 4'-phosphonomethoxytetrahydrofuranyl-1'-purine-pyrimidine of the formula ##STR3## wherein X and X' are the same or different and are hydrogen or alkyl, the dashed line is an optional bond, Y and Z are the same or different and are hydrogen, hydroxyl or alkyl or Y+Z are taken together to form an epoxide or cyclopropyl, and B is a purine or pyrimidine base.
摘要:
Provided are compounds of the following formulae: A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroyalkyl or alkanoyl and B is a purine or pyrimidine base. A compound of formula (II) or (VIII) ##STR2## wherein the broken line is an optional bond; X, R and X' are the same or different and are H or alkyl with 1 to 6 carbon atoms; and B is cytosine, 5-ethylcytosine, 5-methylcytosine, thymine, uracil, 5-chlorouracil, 5-bromouracil, 5-ethyluracil, 5-iodouracil, 5-propyluracil or 5-vinyluracil, any one of which is substituted at the 1-position; wherein in the compound of formula (II), Y and Z are the same or different and are H; OH; alkyl having 1 to 6 carbon atoms; alkyl having 1 to 6 carbon atoms which is substituted with halogen, hydroxy, amino or azido; or are taken together to form an oxygen atom or a methylene group; or are taken together with X' to complete a cyclic phosphonate having the structure of formula (III) ##STR3## wherein R.sup.b is H or OH; wherein in the compound of formula (VIII), Y is halogen, phenylthio or phenylseleno; and the pharmaceutically acceptable salts thereof. B is a purine or pyrimidine base.
摘要:
Provided are compounds of the following formulae: A phosphonomethoxymethyoxymethyl purine/pyridimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl and B is a purine or pyrimidine base. A compound of formula (II) or (VIII) ##STR2## wherein the broken line is an optional bond; X, R and X' are the same or different and are H or alkyl with 1 to 6 carbon atoms; wherein in the compound of formula (II), Y and Z are the same or different and are H; OH; alkyl having 1 to 6 carbon atoms; alkyl having 1 to 6 carbon atoms which is substituted with halogen, hydroxy, amino or azido; or Y and Z are taken together to form an oxygen atom or a methylene group; or Y is taken together with X' to complete a cyclic phosphonate having the structure of formula (III) ##STR3## wherein R.sup.b is H or OH; wherein in the compound of formula (VIII), Y is halogen, phenylthio or phenylseleno; wherein in the compound of formula (II), B is hypoxanthine, xanthine, guanine, 8-bromoguanine, 8-chloroguanine, 8-methylguanine, 8-thioguanine, 3-deazaguanine, purine, 2-aminopurine, 2,6-diaminopurine, adenine or 3-deazaadenine, any one of which is substituted at the 9-position; and, wherein in the compound of formula (III) or (VIII), B is hypoxanthine, xanthine, guanine, 8-bromoguanine, 8-chloroguanine, 8-methylguanine, 8-thioguanine, 3-deazaguanine, purine, 2-aminopurine, 2,6-diaminopurine, adenine, 3-deazaadenine, 8-aminoguanine, 8-hydrazinoguanine or 8-hydroxyguanine, any one of which is substituted at the 9-position; and the pharmaceutically acceptable salts thereof.
摘要:
Provided are compounds of the following formulae: A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl and B is a purine or pyrimidine base. A compound of formula (VI) ##STR2## wherein X is halogen, Y is S-phenyl, Se-phenyl or halogen and B is hypoxanthine, xanthine, guanine, 8-bromoguanine, 8-chloroguanine, 8-methylguanine, 8-thioguanine, 3-deazaguanine, purine, 2-aminopurine, 2,6-diaminopurine, adenine, 3-deazaadenine, 8-aminoguanine, 8-hydrazinoguanine, 8-hydroxyguanine, cytosine, 5-ethylcytosine, 5-methylcytosine, thymine, uracil, 5-chlorouracil, 5-bromouracil, 5-ethyluracil, 5-iodouracil, 5-propyluracil or 5-vinyluracil, 2-acetamido-6-diphenylcarbamoylpurine, 6-N-dimethylamino-methyladenine or 6-N-pivaloyladenine. A compound of formula (VII) ##STR3## wherein B is guanine, 8-guanine, 8-bromoguanine, 8-chloroguanine, 8-methylguanine, 8-thioguanine, 3-deazaguanine, 8-aminoguanine, 8-hydrazinoguanine, 8-hydroxyguanine, cytosine, 5-ethylcytosine, or 5-methylcytosine.
摘要:
An arrow having an arrowhead assembly attached thereto is provided for marking a remote location with a marking media. The marking media is preferably in the form of a paint ball or a scent ball. The arrowhead assembly includes a media reservoir defining a cavity and a plurality of supports extending outward from the media reservoir along a longitudinal axis. The supports secure the marking media within the cavity in a press-fit connection. In one embodiment, a cap and a resilient nose cone are attached to the media reservoir, surrounding the marking media, to prevent damage to a target upon impacting the target.