摘要:
Disclosed are (N)-methanocarba adenine nucleosides of the formula: [Formula] as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias. The invention also provides compounds that are agonists of both A1 and A3 adenosine receptors for use in cardioprotection.
摘要翻译:公开了具有下式的(N) - 甲烷卡巴腺嘌呤核苷:作为高效A 3 N 3腺苷受体激动剂,包含这种核苷的药物组合物,以及这些核苷的使用方法,其中R < SUB> 1 SUB> 6 SUB>如说明书中所定义。 这些核苷被考虑用于治疗许多疾病,例如炎症,心脏缺血,中风,哮喘,糖尿病和心律失常。 本发明还提供了用于心脏保护的作为Aβ1 N和A 3 N 3腺苷受体的激动剂的化合物。
摘要:
Compounds of the formulae I and Ia and their racemates ##STR1## in which A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --, R.sub.1 is hydrogen or a protective group, R.sub.2 is hydrogen or a protective group or a radical forming a phosphorus-containing nucleotide bridge group and B is a purine or pyrimidine radical or an analogue thereof, can be used as antiviral active ingredients or for the preparation of biologically active oligonucleotides.
摘要:
Alpha-morpholino subunits and polymer compositions composed of alpha-morpholino subunits are disclosed. These subunits can be linked together by uncharged linkages, one to three atoms in length, joining the morpholino nitrogen of one subunit to the 5' exocyclic carbon of an adjacent subunit. Each subunit contains a purine or pyrimidine base-pairing moiety effective to bind by hydrogen bonding to a specific base or base-pair in a target polynucleotide. The polymers of the instant invention can be used in place of standard RNA or DNA oligomers. For example, the target-specific polymers of the invention can be used in a variety of diagnostic assays for detection of RNA or DNA having a given target sequence. Further, the polymers of the invention also have potential use as therapeutic agents.
摘要:
6-(3-Thienylmethylamino)-purine of the formula ##STR1## a process for its manufacture, and agents for regulating plant growth containing a compound of the formula I.
摘要:
The invention provides a new convergent approach for the synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′-methylene-carbocyclic guanosine (FMCG) from a readily available starting material in eight steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, (1S,3R,4R)-3-tert-butoxy-4-(tert-butoxymethyl)-2-fluoro-5-methylenecyclopentanol (compound 8 of scheme 1A or a) in only six (6) steps is also provided. Prodrugs of these compounds are also prepared.
摘要:
A cyclopentenecarboxamide derivative represented by the formula (I): ##STR1## and a method for preparing the cyclopentencarboxamide derivative. A bicycloamide derivative represented by the formula (II): ##STR2## and a method for preparing the bicycloamide derivative.
摘要:
A method of treating susceptible neoplasms in mammals comprising administering to a mammal in need of such treatment a pharmaceutically effective amount of a compound of the formula ##STR1## wherein: R.sup.1 is hydrogen;R.sup.2 is a base defined by one of the formulae ##STR2## X is C-R.sup.4 ; R.sup.3 is hydrogen;R.sup.4 is hydrogen, C.sub.1 -C.sub.4 alkyl, bromo, fluoro, chloro or iodo;and the pharmaceutically-acceptable salts thereof.
摘要:
Stable salts of S-adenosyl-L-methionine with water-soluble polyanions, such as polyphosphates, polyvinylsulfonates -sulfates or -phosphates, polyacrylates, polystyrene sulfonates, are described.The salts according to the invention, prepared by precipitation from aqueous solutions of pH not exceeding 3.5, possess peculiar stability, solubility, nonhygroscopicity and are valuable for use as active constituents in pharmaceutical compositions.
摘要:
Compounds of the general formula ##STR1## (wherein X represents an oxygen or sulphur atom, R.sup.1 represents a hydroxy or amino group, R.sup.2 represents a hydrogen atom or a group of formula --CH.sub.2 OR.sup.3.sub.a and R.sup.3 and R.sup.3.sub.a which may be the same or different, each represents an amino acid acyl radical) and physiologically acceptable salts thereof are useful for the treatment of viral infections and have been found to have a surprisingly high water-solubility which renders them of value in the formulation of aqueous pharmaceutical preparations. Processes for preparing the compounds are described.
摘要:
The invention provides a new convergent approach for the synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′-methylene-carbocyclic guanosine (FMCG) from a readily available starting material in eight steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, (1S,3R, 4R)-3-tert-butoxy -4-(tert-butoxymethyl)-2-fluoro-5-methylenecyclopentanol (compound 8 of scheme 1A or a) in only six (6) steps is also provided. Prodrugs of these compounds are also prepared.