Patent classifications
C07C281/16
PROCESS FOR THE PREPARATION OF (9S)-2-BROMO-9-(2,3,4-TRIFLUOROPHENYL)-6,7,8,9-TETRAHYDRO-5H-[1,2,4]TRIAZOLO[1,5-A]AZEPINE
The present invention relates to a process for synthesizing large scale a compound of formula (I), or pharmacuetically acceptable salt thereof, which is useful as the key intermediate for the synthesis of compounds for prophylaxis and treatment of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
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PROCESS FOR THE PREPARATION OF (9S)-2-BROMO-9-(2,3,4-TRIFLUOROPHENYL)-6,7,8,9-TETRAHYDRO-5H-[1,2,4]TRIAZOLO[1,5-A]AZEPINE
The present invention relates to a process for synthesizing large scale a compound of formula (I), or pharmacuetically acceptable salt thereof, which is useful as the key intermediate for the synthesis of compounds for prophylaxis and treatment of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
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IGF2BP2 INHIBITORS AND USES THEREOF
Described herein, inter alia, are IGF2BP2 inhibitor compounds and methods of using the same.
Method for measuring blood coagulation
A method for measuring blood coagulation, including: preparing a reaction solution including a plasma specimen, a blood coagulation activator, and at least one of amino-guanidine and an acid addition salt thereof; and measuring blood coagulation time by detecting a turbidity change in the reaction solution.
Method for measuring blood coagulation
A method for measuring blood coagulation, including: preparing a reaction solution including a plasma specimen, a blood coagulation activator, and at least one of amino-guanidine and an acid addition salt thereof; and measuring blood coagulation time by detecting a turbidity change in the reaction solution.
NEW METAL N-AMINOGUANIDINATE COMPLEXES FOR USE IN THIN FILM FABRICATION AND CATALYSIS
The present patent application relates to new metal complexes having at least one N-aminoguanidinate ligand. The patent application further relates to the preparation of the new metal complexes and also to their use. The new metal complexes are especially suitable as precursors for the preparation of functional layers by means of gas-phase thin-film processes such as CVD, MO-CVD, MOVPE and ALD. Additionally, they are also suitable as catalysts for olefin hydroamination and for olefm polymerization.
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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).
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.