Patent classifications
C07C281/16
Self-assembled active agents
A self-assembled active agent may be formed by a process including covalently bonding at least a first component molecule and a second component molecule, the two component molecules displaying synergy such that the effective amount of the self-assembled active agent is lower than the sum of the effective amounts of the first component molecule and the second component molecule. The component molecules may be chosen such that the covalent bonding is reversible, for example through a hydrazone bond between an amine and an aldehyde. The active agent may thus have controllable activity such as an antimicrobial agent, a biocide, an antiviral agent, a preservative, an antifouling agent, a disinfectant, or a sensor agent, such as for a particular molecule or for pH.
Self-assembled active agents
A self-assembled active agent may be formed by a process including covalently bonding at least a first component molecule and a second component molecule, the two component molecules displaying synergy such that the effective amount of the self-assembled active agent is lower than the sum of the effective amounts of the first component molecule and the second component molecule. The component molecules may be chosen such that the covalent bonding is reversible, for example through a hydrazone bond between an amine and an aldehyde. The active agent may thus have controllable activity such as an antimicrobial agent, a biocide, an antiviral agent, a preservative, an antifouling agent, a disinfectant, or a sensor agent, such as for a particular molecule or for pH.
Salts formed by 2-(1-acyloxy-n-pentyl) benzoic acid and basic amino acid or aminoguanidine, and preparation method and application thereof
The present disclosure discloses salts formed by 2-(1-acyloxy-n-pentyl)benzoic acid and basic amino acid or aminoguanidine, a preparation method thereof, pharmaceutical preparations containing these salts, and application thereof in preparation of drugs for preventing or treating ischemic cardiovascular and cerebrovascular diseases, resisting thrombosis and improving cardio-cerebral circulation disorders. The compound of the present disclosure has excellent water solubility, aqueous solution stability and pharmacokinetic properties, also has significant anti-platelet aggregation, anti-thrombosis, anti-cerebral ischemia and neuroprotective activity. The compound of the present disclosure has significantly better effects than those of (S)-butylphthalide and potassium (R/S)-2-(1-hydroxy-n-pentyl) benzoate (PHPB), has significantly lower acute toxicity to mice by intravenous injection than that of butylphthalide and PHPB, has a lower inhibition rate of the hERG potassium channel in CHO-hERG cells than that of (S)-butylphthalide, and has a negative result in Bacterial Reverse Mutation Test (Ames test).
Salts formed by 2-(1-acyloxy-n-pentyl) benzoic acid and basic amino acid or aminoguanidine, and preparation method and application thereof
The present disclosure discloses salts formed by 2-(1-acyloxy-n-pentyl)benzoic acid and basic amino acid or aminoguanidine, a preparation method thereof, pharmaceutical preparations containing these salts, and application thereof in preparation of drugs for preventing or treating ischemic cardiovascular and cerebrovascular diseases, resisting thrombosis and improving cardio-cerebral circulation disorders. The compound of the present disclosure has excellent water solubility, aqueous solution stability and pharmacokinetic properties, also has significant anti-platelet aggregation, anti-thrombosis, anti-cerebral ischemia and neuroprotective activity. The compound of the present disclosure has significantly better effects than those of (S)-butylphthalide and potassium (R/S)-2-(1-hydroxy-n-pentyl) benzoate (PHPB), has significantly lower acute toxicity to mice by intravenous injection than that of butylphthalide and PHPB, has a lower inhibition rate of the hERG potassium channel in CHO-hERG cells than that of (S)-butylphthalide, and has a negative result in Bacterial Reverse Mutation Test (Ames test).
Hydrogen sulfide donor in organic salt form and preparation method therefor
A hydrogen sulfide donor in an organic salt form and a preparation method thereof. The hydrogen sulfide donor exists as a salt formed by organic compounds with an alkaline motif and hydrogen sulfide with weak acidity. The hydrogen sulfide donor features with a simple structure, and an easy preparation method. Moreover, hydrogen sulfide donors in different forms can be prepared according to research and development needs. After the hydrogen sulfide donor enters an organism, the process of in vivo dissociation and hydrogen sulfide supply is simple, rapid, and effective, and there is no requirement for enzyme or any other complicated condition, and thus, the hydrogen sulfide donor has a great application prospect and value.
Gas generating agent, and method for producing foam using the same
The gas generating agent of the present invention comprises an oxalic acid salt of an aminoguanidine compound represented by general formula (1) below. ##STR00001##
Gas generating agent, and method for producing foam using the same
The gas generating agent of the present invention comprises an oxalic acid salt of an aminoguanidine compound represented by general formula (1) below. ##STR00001##
Lipophilic guanidinium compounds for removal of oxyanions from aqueous solutions
Methods for removing an oxyanion from an aqueous source containing said oxyanion, comprising contacting said aqueous source with an aqueous-insoluble hydrophobic solution containing an oxyanion extractant compound dissolved in an aqueous-insoluble hydrophobic solvent to result in formation of an oxyanion salt of said extractant compound and extraction of said oxyanion salt into said aqueous-insoluble hydrophobic solution, wherein said extraction results in an extraction affinity (D) of said oxyanion of at least 1, wherein D is the concentration ratio of said oxyanion in the organic phase divided by the concentration of said oxyanion in the aqueous phase; wherein said extractant compound has the following composition: ##STR00001##
wherein at least one of R.sup.1-R.sup.10 is or contains a hydrocarbon (R) group containing at least 4, 5, 6, 7, 8, 9, 10, 11, or 12 carbon atoms.
Lipophilic guanidinium compounds for removal of oxyanions from aqueous solutions
Methods for removing an oxyanion from an aqueous source containing said oxyanion, comprising contacting said aqueous source with an aqueous-insoluble hydrophobic solution containing an oxyanion extractant compound dissolved in an aqueous-insoluble hydrophobic solvent to result in formation of an oxyanion salt of said extractant compound and extraction of said oxyanion salt into said aqueous-insoluble hydrophobic solution, wherein said extraction results in an extraction affinity (D) of said oxyanion of at least 1, wherein D is the concentration ratio of said oxyanion in the organic phase divided by the concentration of said oxyanion in the aqueous phase; wherein said extractant compound has the following composition: ##STR00001##
wherein at least one of R.sup.1-R.sup.10 is or contains a hydrocarbon (R) group containing at least 4, 5, 6, 7, 8, 9, 10, 11, or 12 carbon atoms.
Benzylideneguanidine derivatives and therapeutic use for the treatment of protein misfolding diseases
The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein: R.sub.1 is alkyl, Cl, F or Br; R.sub.2 is H or F; R.sub.3 is selected from H and alkyl; R.sub.4 is selected from H and C(O)R.sub.6; R.sub.5 is H; or R.sub.4 and R.sub.5 are linked to form a heterocyclic group which is optionally substituted with one or more R.sub.10 groups; R.sub.6 is selected from R.sub.7, OR.sub.7 and NR.sub.8R.sub.9; R.sub.7, R.sub.8 and R.sub.9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocyclyl and aryl, each of which is optionally substituted with one or more R.sub.10 groups; each R.sub.10 is independently selected from halogen, OH, CN, NO.sub.2, COO-alkyl, aralkyl, SO.sub.2-alkyl, SO.sub.2-aryl, COOH, CO-alkyl, CO-aryl, NH.sub.2, NH-alkyl, N(alkyl).sub.2, CF.sub.3, alkyl and alkoxy; X and Z are each independently CR.sub.11, and Y is selected from CR.sub.11 and N; and R.sub.11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.