Abstract: The present invention provides a pharmaceutical composition of tetramethylpyrazine nitrone for injection and a method of manufacture thereof, wherein the pharmaceutical composition has good stability. The pharmaceutical composition of tetramethylpyrazine nitrone for injection is a freeze-dried powder injection, the characteristics thereof on appearance, acidity, moisture content, related substances, insoluble particles, content detection, sterility, and visible foreign objects are all in compliance with relevant regulations. The method of manufacture of the pharmaceutical composition is simple, and the prepared tetramethylpyrazine nitrone freeze-dried powder injection has good formability. The freeze-drying process of the present invention has good stability and short freeze-drying time, and the process can be performed for effectively saving energy and labor, and is suitable for industrial production.

Abstract: The present invention provides a combination therapy of a nitrone compound or a pharmaceutically acceptable salt thereof with a SGLT-2 inhibitor. Research found that the nitrone compounds TBN and TN-2, when used in combination with a SGLT-2 inhibitor, can synergistically lower blood sugar and also reduce the 24-hour urinary microalbumin and urinary albumin creatinine ratio in db/db mice, demonstrating a protective effect on the kidneys. The inventor also unexpectedly discovered that the combination of the nitrone compound with the SGLT-2 inhibitor can reduce the risk of urinary and reproductive tract infections caused by SGLT-2 inhibitors.

Abstract: The present invention provides the use of an amantadine mononitrate compound in the manufacture of a medicament for the prevention and treatment of hypertension. The amantadine mononitrate compound can be administered to reduce the systolic and/or diastolic pressure of subjects. The amantadine mononitrate compound has a long half-life and long drug action time in subjects and can reduce the number of administration times and improve patient compliance as compared to existing hypertensive drugs. The medicament of the amantadine mononitrate compound of the present invention has no adverse reactions of orthostatic hypotension, and thus has improved the safety of the drug use.

Abstract: The present invention relates to the use of ligustrazine nitrone derivatives and pharmaceutical composition thereof for the treatment and prevention of diseases of diabetic complications, which include renal anemia. The ligustrazine nitrone derivatives have the structure of the general formula (I). Experimental results indicated that the ligustrazine nitrone derivatives can significantly increase the levels of serum iron and erythropoietin in STZ induced SD rats and spontaneously hypertensive rats, and can be used for treating and preventing renal anemia caused by decrease in renal EPO production and/or concomitant iron deficiency. Therefore, the ligustrazine nitrone derivatives can be made into various dosage forms with a drug carrier. The derivatives can be prepared into various dose forms together with drug carriers.

Abstract: The present invention provides uses of an andrographolide derivative in preparation of a medicament for preventing and treating inflammatory bowel disease. The andrographolide derivative AL-1 has the mechanisms, for the treatment of ulcerative colitis, of scavenging of free radicals, inhibition of NF-?B signaling pathway activation and COX-2 expression, activation of PPAR-? expression, and thus can prevent the transcription and expression of inflammatory-related genes to improve the conditions of inflammation. AL-1 can be used as a medicine for the treatment of inflammatory bowel disease and can be formulated to various dosage forms with a pharmaceutically acceptable carrier.

Abstract: The present invention provided a process for manufacture of amantadine nitrate derivatives, and the process comprises using adamantane as the raw material to prepare amantadine nitrate derivatives via the following steps: (1) synthesis of adamantanol; (2) carboxylation of adamantanol; (3) acetylation of adamantanoic acid; (4) reduction; (5) hydrolysis of amido adamantanol and Boc protection of amino group; (6) crystallization of Boc protected amantadinol; (7) nitrate esterification of Boc protected amantadinol; (8) refining of the product of nitrate esterification; (9) Boc deprotection and salt formation; and (10) refining of amantadine nitrate hydrochloride. The amantadine nitrate derivatives have the struction of: wherein, R1 and R2 are each independently hydrogen, straight-chain or branched-chain alkyl, or substituted or unsubstituted aryl or heteroaryl. The process of this invention is efficient, cost effective, environmentally friendly, safe, reliable, and suitable for industrial production.

Abstract: The present invention relates to the use of ligustrazine nitrone derivatives and pharmaceutical composition thereof for the treatment and prevention of diseases of diabetic complications, which include renal anemia. The ligustrazine nitrone derivatives have the structure of the general formula (I). Experimental results indicated that the ligustrazine nitrone derivatives can significantly increase the levels of serum iron and erythropoietin in STZ induced SD rats and spontaneously hypertensive rats, and can be used for treating and preventing renal anemia caused by decrease in renal EPO production and/or concomitant iron deficiency. Therefore, the ligustrazine nitrone derivatives can be made into various dosage forms with a drug carrier. The derivatives can be prepared into various dose forms together with drug carriers.

Abstract: A use of of ligustrazine nitrone derivatives and a pharmaceutical composition thereof in the preparation of medicine for preventing and treating diabetic complication diseases. The ligustrazine nitrone derivatives can be prepared into various dose forms together with drug carriers.

Abstract: The present invention relates to amantadine nitrate compounds having neural protective effect, and preparation method and medical use thereof. The compounds have the structure of the general formula (II). The compounds have multifunctional mechanisms, including inhibiting NMDA receptors, releasing NO, inhibiting calcium influxes, and having protective effects on cells particularly neurocytes. The compounds can be used in the preparation of medicaments having a cellular protective effect, for prevention or treatment of the diseases related to such as NMDA receptors and elevation of calcium anions in cells, including the diseases related to neurodegeneration such as Alzheimer's disease, Parkinson's disease, cerebral paralysis and glaucoma, and the diseases related to cardio-cerebral-vascular system such as Parkinson's syndrome combined with cerebral arteriosclerosis, as well as respiratory tract infections caused by influenza virus.

Abstract: The present invention relates to trifluoroacetyl hydrazide compounds and medical uses thereof. The compounds have a structure of the following formula: The compounds showed multifunctional mechanisms, including inhibition of glutamate excitotoxicity, activation of MEF2 transcriptional activity, clearance of free radicals, and promotion of nerve differentiation, and has a better protective effect on cells especially nerve cells. The compound can be used to prepare prophylactic or therapeutic medicaments with cytoprotective effects, for the prevention or treatment of diseases related to glutamate receptor activation, MEF2 disorders or excessive free radicals generation. The diseases include, for example, neurodegenerative diseases such as Alzheimer's disease, Parkinson and stroke, and the free radicals related diseases such as heart disease, myocardial ischemia, diabetes and other cardiovascular and cerebrovascular diseases.

Abstract: The present invention relates to a pyrazine derivative, and preparation method and medical use thereof. The pyrazine derivative can remove free radicals and suppress calcium overload and has cytoprotective effects, and can be used for the prevention and treatment of cardiovascular and cerebrovascular diseases, neurodegenerative diseases and other related diseases.

Abstract: A use of of ligustrazine nitrone derivatives and a pharmaceutical composition thereof in the preparation of medicine for preventing and treating diabetic complication diseases. The ligustrazine nitrone derivatives can be prepared into various dose forms together with drug carriers.

Abstract: The present invention relates to a pyrazine derivative, and preparation method and medical use thereof. The pyrazine derivative can remove free radicals and suppress calcium overload and has cytoprotective effects, and can be used for the prevention and treatment of cardiovascular and cerebrovascular diseases, neurodegenerative diseases and other related diseases.

Abstract: The present invention relates to trifluoroacetyl hydrazide compounds and medical uses thereof. The compounds have a structure of the following formula: The compounds showed multifunctional mechanisms, including inhibition of glutamate excitotoxicity, activation of MEF2 transcriptional activity, clearance of free radicals, and promotion of nerve differentiation, and has a better protective effect on cells especially nerve cells. The compound can be used to prepare prophylactic or therapeutic medicaments with cytoprotective effects, for the prevention or treatment of diseases related to glutamate receptor activation, MEF2 disorders or excessive free radicals generation. The diseases include, for example, neurodegenerative diseases such as Alzheimer's disease, Parkinson and stroke, and the free radicals related diseases such as heart disease, myocardial ischemia, diabetes and other cardiovascular and cerebrovascular diseases.

Abstract: The present invention relates to amantadine nitrate compounds having neural protective effect, and preparation method and medical use thereof. The compounds have the structure of the general formula (II). The compounds have multifunctional mechanisms, including inhibiting NMDA receptors, releasing NO, inhibiting calcium influxes, and having protective effects on cells particularly neurocytes. The compounds can be used in the preparation of medicaments having a cellular protective effect, for prevention or treatment of the diseases related to such as NMDA receptors and elevation of calcium anions in cells, including the diseases related to neurodegeneration such as Alzheimer's disease, Parkinson's disease, cerebral paralysis and glaucoma, and the diseases related to cardio-cerebral-vascular system such as Parkinson's syndrome combined with cerebral arteriosclerosis, as well as respiratory tract infections caused by influenza virus.

Abstract: The present invention relates to trifluoroacetyl hydrazide compounds and methods of preparation and uses thereof. The compounds have a structure of the following formula: The compounds showed multifunctional mechanisms, including inhibition of glutamate excitotoxicity, activation of MEF2 transcriptional activity, clearance of free radicals, and promotion of nerve differentiation, and has a better protective effect on cells especially nerve cells. The compound can be used to prepare prophylactic or therapeutic medicaments with cytoprotective effects, for the prevention or treatment of diseases related to glutamate receptor activation, MEF2 disorders or excessive free radicals generation. The diseases include, for example, neurodegenerative diseases such as Alzheimer's disease, Parkinson and stroke, and the free radicals related diseases such as heart disease, myocardial ischemia, diabetes and other cardiovascular and cerebrovascular diseases.

Abstract: The present invention relates to amantadine nitrate compounds having neural protective effect, and preparation method and medical use thereof. The compounds have the structure of the general formula (I). The compounds have multifunctional mechanisms, including inhibiting NMDA receptors, releasing NO, inhibiting calcium influxes, and having protective effects on cells particularly neurocytes. The compounds can be used in the preparation of medicaments having a cellular protective effect, for prevention or treatment of the diseases related to such as NMDA receptors and elevation of calcium anions in cells, including the diseases related to neurodegeneration such as Alzheimer's disease, Parkinson's disease, cerebral paralysis and glaucoma, and the diseases related to cardio-cerebral-vascular system such as Parkinson's syndrome combined with cerebral arteriosclerosis, as well as respiratory tract infections caused by influenza virus.

Abstract: The present invention relates to trifluoroacetyl hydrazide compounds and methods of preparation and uses thereof. The compounds have a structure of the following formula: The compounds showed multifunctional mechanisms, including inhibition of glutamate excitotoxicity, activation of MEF2 transcriptional activity, clearance of free radicals, and promotion of nerve differentiation, and has a better protective effect on cells especially nerve cells. The compound can be used to prepare prophylactic or therapeutic medicaments with cytoprotective effects, for the prevention or treatment of diseases related to glutamate receptor activation, MEF2 disorders or excessive free radicals generation. The diseases include, for example, neurodegenerative diseases such as Alzheimer's disease, Parkinson and stroke, and the free radicals related diseases such as heart disease, myocardial ischemia, diabetes and other cardiovascular and cerebrovascular diseases.

Abstract: This invention is directed to novel compounds isolated or derived from Alpiniae oxyphyllae fructus, chemically synthesized novel compounds, methods of preparing the novel compounds and uses thereof as neuroprotectants or drugs for treating neurodegenerative diseases such as Parkinson's disease.

Abstract: The present invention provides uses of an andrographolide derivative in preparation of a medicament for preventing and treating inflammatory bowel disease. The andrographolide derivative AL-1 has the mechanisms, for the treatment of ulcerative colitis, of scavenging of free radicals, inhibition of NF-?B signaling pathway activation and COX-2 expression, activation of PPAR-? expression, and thus can prevent the transcription and expression of inflammatory-related genes to improve the conditions of inflammation. AL-1 can be used as a medicine for the treatment of inflammatory bowel disease and can be formulated to various dosage forms with a pharmaceutically acceptable carrier.