44results about How to "Good pharmacokinetic parameters" patented technology

Transdermal therapeutic systems for administering analgesics, preferably buprenorphine or one of its pharmaceutically acceptable salts or pro-drugs, and processes for the production of such systems.

The invention provides a diaminopyrimidine compound and a composition containing the same and discloses the diaminopyrimidine compound shown as in a formula (I) and a drug combination containing the compound or salt thereof acceptable in crystal form and pharmacy, hydrate or solvent complex, stereoisomer, pro-drug or isotope variant. The diaminopyrimidine compound and the composition containing the same have excellent inhibition effect on protein kinase and have better pharmacokinetic parameter characteristics, and drug concentration of the compound in animal bodies can be increased to improve drug efficacy and safety.

The invention provides substituted diaminopyrimidine compound, a composition comprising the compound and application of the compound. The substituted diaminopyrimidine compound is diaminopyrimidine compound shown as in formula (I) or its crystal-form pharmaceutically acceptable salts and prodrugs, and stereoisomer, hydrate or solvent compound. The substituted diaminopyrimidine compound disclosed herein and the composition comprising the compound have excellent inhibitory action on EGFR (epidermal growth factor receptor) kinase, have better pharmacokinetics parameter characteristics, and can increase the drug concentration of the compound in an animal body to provide improved drug therapeutic effect and safety.

The invention relates to an indazole compound for inhibiting kinase activity and relates to preparation and application of the indazole compound. Specifically, the invention discloses the indazole compound shown as a formula (I), or crystal forms, prodrugs, pharmaceutically acceptable salts, stereoisomers, tautomers, solvates or pharmaceutical compositions of hydrates of the indazole compound. Thecompound and the composition containing the compound, provided by the invention, have excellent inhibition performance on kinase protein, and also have better pharmacokinetics parameter characteristics at the same time; the medicine concentration of the compound in animals can be improved and the curative effect and safety of the medicine are improved. The formula (I) is shown in the description.

The invention provides a substituted pyridazinone compound and application thereof. The substituted pyridazinone compound is a compound shown in a general formula I, or a pharmaceutically acceptable salt, a prodrug, a hydrate or a solvent compound, a polymorphic form, a stereoisomer or an isotope variant of the substituted pyridazinone compound. The compound disclosed by the invention can be applied to preparation of medicines for preventing and / or treating diseases related to abnormal thyroid hormone functions. The compound has higher THbeta selectivity; the compound has better pharmacokinetic parameters and ideal compound stability; and while the selectivity is improved, the activation activity on THbeta is also obviously enhanced.

The invention relates to a double-targeting recombinant protein based on an antibody and targeting macropinocytosis and an application of a coupling chemotherapeutic drug composition in the preparation of anti-tumor drugs. A research shows that a double-targeting action of an anti-EGFR single-chain antibody scFv and a macropinocytosis recombinant protein mediated by LDP and albumin D III is utilized to realize the coupling of chemotherapeutic drugs, and chemotherapeutic drugs such as lidamycin and the like can be conveyed targetedly to tumor cells, so that a more effective anti-tumor effect isexerted. The invention discloses a preparation method and application of the anti-tumor drugs based on the double-targeting action the antibody and the macropinocytosis, and no relevant reports havebeen found at home and abroad so far.

The invention discloses applications of turmeric rhizome oil. The applications include an application of the turmeric rhizome oil in preparation of drugs for treating or preventing brain dysfunction,and an application of the turmeric rhizome oil in preparation of health products for relieving the brain dysfunction. The invention discovers for the first time a new use of the turmeric rhizome oil in drugs or massive health products displaying activity in the brain dysfunction of experimental animals, and discovers for the first time that the turmeric rhizome oil or any compound containing the turmeric rhizome oil can relieve animals' symptoms of the brain dysfunction such as Alzheimer's Disease and depression in an in-vivo model of the animals. Compared with existing drugs for treating thebrain dysfunction, the turmeric rhizome oil or any combination thereof has the advantages that the turmeric rhizome oil or any combination thereof has the mechanism of inhibiting cholinesterase and regulating the polymolecular synergistic effect of neurotransmitters on multiple targets, has good pharmacological parameters, and easily penetrates blood brain barriers, thereby having toxicological safety, metabolic stability, long half-life and / or small side effect.

The present invention discloses amide compound represented by a formula (I), preparation and uses thereof, specifically an amide compound represented by the formula (I), or a polymorph, a pharmaceutically acceptable salt, a prodrug, a stereoisomer, an isotope variant, a hydrate or a solvate thereof, a pharmaceutical composition containing the compound, and uses of the compound. According to the present invention, the amide compound and the composition containing the compound can well inhibit protein kinase, have good pharmacokinetic parameter characteristics, and can improve the drug concentration of the compound in the animal so as to improve the treatment effect and the safety of the drug. The formulas I is defined in the specification.

The invention discloses application of bighead atractylodes rhizome essential oil. The bighead atractylodes rhizome essential oil can be applied to preparation of medicines for treating or preventingbrain function and disorder diseases as well as healthy products for improving the brain function and disorder diseases. The invention discovers the new application of the bighead atractylodes rhizomeessential oil to preparation of medicine or large health products which show activity in the experiment animal brain function and disorder diseases for the first time; and the invention discovers that the bighead atractylodes rhizome essential oil or the composition containing the bighead atractylodes rhizome essential oil can improve the brain function and disorder animal symptoms such as seniledementia, depression and anxiety in an animal in vivo model for the first time. Compared with the medicines for treating the brain function and disorder thereof at present, the bighead atractylodes rhizome essential oil or the any composition has mechanism of performing multimolecular synergistic effect of inhibiting cholinesterase and regulating neurotransmitter on a multi-target point, has goodpharmacokinetic parameters and can penetrate through a blood brain barrier easily, so the characteristics of toxicological safety, metabolic stability, long half-life period and small side effect areachieved.

The invention relates to a substituted condensed imidazole ring compound, a composition containing the compound and applications thereof. Specifically, the invention discloses a fused imidazole ring compound represented by formula (), or a pharmaceutical composition of its crystal form, pharmaceutically acceptable salt, prodrug, stereoisomer, hydrate or solvate. The compound of the present invention can be used as a histamine H1-receptor antagonist and a mast cell stabilizer, which can inhibit the release of histamine from mast cells and prevent the action of histamine, thereby alleviating allergic reactions. Formula (I).

The invention discloses application of cedarwood essential oil. The application of the cedarwood essential oil comprises application of the cedarwood essential oil to preparing brain function and disorder disease treating or preventing medicines and healthcare products. According to the application of the cedarwood essential oil, novel application of the cedarwood essential oil, which is highly active in treating brain function and disorder diseases in experimental animals, to preparing medicines and healthcare products is discovered for the first time; that the cedarwood essential oil or cedarwood essential oil-containing compositions can improve the symptoms of animals with brain function and disorder diseases such as senile dementia and depression and anxiety is also discovered for thefirst time. Compared with existing brain function and disorder treating medicines, the cedarwood essential oil or the cedarwood essential oil-containing compositions can have a mechanism of polymolecular synergistic effects on targets by inhibiting cholinesterase, regulating neurotransmitters and the like, achieve good pharmacokinetic parameters and easily penetrate through blood brain barriers, thereby having the advantages of toxicological safety, stable metabolism, a relatively long half-life period and relatively low side effects.

Provided are a substituted naphthalene ring compound, a pharmaceutical composition, and applications thereof. The naphthalene ring compound is a compound represented by formula (I), or its polymorph, pharmaceutically acceptable salt, prodrug, stereo Isomers, isotopic variations, hydrates or solvates. The naphthalene ring compound can be used as a hepatitis C virus inhibitor, has better hepatitis C virus protein NS5B inhibitory activity, and better pharmacodynamics / pharmacokinetic performance, so it is more suitable for preparing and treating hepatitis C virus infection medicine. Formula (I).

It relates to a substituted boronic acid compound, a pharmaceutical composition containing the compound and its use. The substituted boronic acid compound is, for example, a compound represented by formula (I), or its crystal form, pharmaceutically acceptable salt, or prodrug , stereoisomers, hydrates or solvates. The boronic acid compound has proteasome inhibitory activity, has better pharmacodynamics / pharmacokinetic properties, has good applicability and high safety, and can be used for preparing medicines for treating diseases related to proteasomes. Formula 1)

The invention discloses application of ligusticum chuanxiong hort essential oil, including application of ligusticum chuanxiong hort essential oil in preparation of drugs for treating or preventing brain dysfunctions and disorder diseases, and application of ligusticum chuanxiong hort essential oil in preparation of healthy products for improving brain dysfunctions and treating disorder diseases.According to the application, the novel application of the ligusticum chuanxiong hort essential oil in drugs or large healthy products showing activity in brain dysfunctions and disorder diseases of experimental animals is found for the first time, and it is found for the first time that the ligusticum chuanxiong hort essential oil or a composition containing the ligusticum chuanxiong hort essential oil or any ligusticum chuanxiong hort essential oil composition can alleviate or treat the symptoms of the brain dysfunctions and disorder diseases such as alzheimer's disease, depression and anxiety in in-vivo models of the animals. Compared with current drugs for treating brain dysfunctions and disorders, the ligusticum chuanxiong hort essential oil or any composition thereof has the mechanism of making polymolecular synergistic effects on multiple targets, for example, cholinesterase inhibiting and neurotransmitter regulating, has good pharmacokinetic parameters and easily permeates through the blood-brain barrier, so that the ligusticum chuanxiong hort essential oil has the advantages of improving toxicological safety and having stable metabolism, longer half-life and / or smaller side effects.

The invention discloses application of Fructus Amomi Rotundus essential oil. The Fructus Amomi Rotundus essential oil can be used for preparing drugs for treating or preventing brain functions and disorders and health products for improving brain functions and disorders. The invention discloses new application of Fructus Amomi Rotundus essential oil in medicines or health products showing activity in brain functions and disorder diseases of experimental animals for the first time; for the first time, it discovers that the Fructus Amomi Rotundus essential oil or a composition containing the Fructus Amomi Rotundus essential oil or any combination of the Fructus Amomi Rotundus essential oil can be used for improving brain functions such as senile dementia, depression and anxiety and symptoms of animals suffering from the brain functions and the like in animal in-vivo models. Compared with an existing medicine for treating brain functions and disorders, the Fructus Amomi Rotundus essential oil or any composition thereof has a mechanism of inhibiting cholinesterase, regulating neurotransmitters and other multi-molecular synergistic effects on multiple targets, has good pharmacokinetic parameters and is easy to permeate a blood-brain barrier, and therefore has the characteristics of toxicological safety, stable metabolism, longer half-life and smaller side effects.

A 1,2,4-triazole compound shown in formula (I) and pharmaceutically acceptable salts thereof. The compound has the activity of an apoptosis signal-regulating kinase 1 ("ASK1") inhibitor; thus, the compound can be used for treating ASK1 mediated diseases including chronic liver disease, cardiovascular disease, metabolic disturbance, respiratory system disorder, gastrointestinal disorder, and neurodegenerative diseases. A pharmaceutical composition comprising the compound of formula (I) and uses thereof.

Disclosed are a substituted adenine compound and a pharmaceutical composition thereof, the substituted adenine compound being a compound of a formula (I), or a crystalline form, pharmaceutically acceptable salt, prodrug, stereoisomer, hydrate, or solvate thereof. The compound of the present invention can inhibit activity of a nucleoside reverse transcriptase and also has improved pharmacodynamic / pharmacokinetic properties; the compound has high applicability, is safe to use, and can be used for the preparation of a pharmaceutical composition for the treatment of viral infection-associated diseases, thereby having great market potential.

The invention discloses a liposome glucose fluorescent probe with good biocompatibility and a preparation method thereof. The nanoliposome probe was developed by using an amphiphilic molecule (DSPE‑PEG 2000 ) encapsulating organoboronic acid glucose molecular probes together to form nanovesicles with lipid bilayer membranes. The diboronic acid recognition site in the organoboronic acid molecule can specifically bind to the cis-adjacent diol in the glucose molecule, so that the nanoprobe has high affinity and selectivity for glucose. The construction of liposome nanoprobes enables molecular probes to have the good properties of liposomes. Compared with organoboronic acid molecules, the liposome nanoprobe has better biocompatibility, faster response time and good fluorescence stability, thus enabling rapid and accurate identification and detection of glucose in vitro and in vivo. Meanwhile, the liposome nanoprobe has the advantages of simple preparation method, stability and high efficiency.

The invention relates to a 1,2,4-triazole compound shown as formula (I) and pharmaceutically acceptable salts thereof. The compound has the activities of apoptosis signal-regulating kinase 1 ('ASK1')inhibitors, so that the compound can be used for treating ASK1-induced symptoms, including chronic liver diseases, cardiovascular diseases, metabolic disturbance, respiratory system disorder, intestines and stomach disorder and neurodegenerative diseases. The invention also provides a drug compound containing the compound disclosed by the invention and an application thereof.

The present invention discloses substituted quinoline compounds represented by formula (I) and compounds containing the compounds, or polymorphs, pharmaceutically acceptable salts, prodrugs, stereoisomers, isotopic variants, hydrates or Pharmaceutical compositions of solvates and uses thereof. The quinoline compound disclosed in the present invention and the composition comprising the compound can be used as 5-HT 6 The receptor antagonist has better properties of pharmacokinetic parameters and can be used to prepare a drug for treating Alzheimer's disease. (I).

The present invention discloses a fused pyrimidine compound as shown in formula (I), and preparation and use of same. In particular, the present invention discloses a fused pyrimidine compound as shown in formula (I), or a crystal form, a pharmaceutically acceptable salt, a prodrug, a stereoisomer, an isotopic variant, a hydrate or solvate thereof, and a pharmaceutical composition comprising same and use of same. The fused pyrimidine compound and the composition comprising the compound disclosed in the present invention exhibit an excellent inhibitory effect against protein kinases, and have improved pharmacokinetic parameter characteristics, which allow increased drug concentration of the compounds in an animal body and enhance drug efficacy and safety.

A substituted pyridine amide compound and its application. Specifically disclosed are deuterated pyridine amide compounds represented by formula (I) and compounds containing the compound, or its crystal form, pharmaceutically acceptable salt, prodrug, stereoisomer, hydrate or solvate pharmaceutical composition. The compound can be used as a JAK inhibitor, and is further applicable to the preparation of medicines for treating JAK-related diseases (such as autoimmune diseases, etc.).

An oxazolidone compound represented by formula (I), or a crystalline form, pharmaceutically acceptable salt, prodrug, metabolite, stereoisomer, isotopic isomer, hydrate, or solvate thereof, and a pharmaceutical composition comprising the compound. The compound has demonstrated inhibitory activity against a broad spectrum of bacteria and low toxicity, and can be used to prepare an antibiotic.