Other

Neuromolecular, Inc.

Panorama Research Inc.

Jinan University

Adamas Pharmaceuticals, Inc.

Guangzhou Magpie Pharmaceuticals Co., Ltd.

Guangzhou Magpie Pharmaceutical Co., Ltd.

Yuqiang Wang

Pei Yu

Yewei Sun

Zaijun Zhang

Gaoxiao Zhang

James W Larrick

Peng Yi

Luchen Shan

Stuart Arthur Lipton

Jonathan S Stemler

Wenqing Ye

Zheng Liu

Wei Liu

Peng Fei Yi

Ming Liang

Jie Jiang

Liang Tao

Haiyun Chen

Xiaojian Jiang

Lipeng Xu

Mei Jing

Linda Wang

Zhaoqi Yang

Jing Du

Ming Lang

Zaizun Zhang

Moussa B H Youdim

James Larrick

Moussa BH Youdim

A crystal form of tetramethylpyrazine nitrone (TBN), and a preparation method and use thereof is provided. A crystal form A of TBN has characteristic diffraction peaks in the XRPD pattern at 2θ°: 10.60±0.2, 11.03±0.2, 15.31±0.2, 15.55±0.2, 17.14±0.2, 17.93±0.2, and 23.81±0.2. The crystal form A has low risk of polymorphism transformation and good stability, which contribute to the stability of the preparations during the production and storage processes, and effectively guarantee the consistency of the content of the crystal form in the preparations. Therefore, the preparations are safe, effective, and controllable in quality. Also, the crystal form A has high biological activity, good druggability, and high bioavailability, fast onset of action.

Crystal form of tetramethylpyrazine nitrone, preparation method and use thereof

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-κB signaling pathway activation and COX-2 expression, activation of PPAR-γ 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.

Use of andrographolide derivatives in preparation of medicaments for preventing and treating inflammatory bowel diseases

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.

Use of ligustrazine nitrone derivatives in prevention and treatment of diabetic complication diseases

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.

Amantadine nitrate compounds for use as medicaments for the treatment of diseases

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.

Pyrazine derivative, and preparation method and medical use thereof

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.

Trifluoroacetyl hydrazide compounds and medical uses thereof

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.

Trifluoroacetyl hydrazide compounds and methods of preparation and uses thereof

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.

Amantadine nitrate compounds with neural protective effect, and preparation and medical use thereof

The invention generally relates to compounds of formula (I) with neural protective effect, and preparation and uses thereof.  The compounds have multiple mechanisms or functions, for example, inhibition of monoamine oxidase and cholinesterase, scavenging of free radicals, and protection of cells such as nerve cells. The compounds can be used for manufacture of medicaments of cell protection, for prevention and/or treatment of monoamine oxidase, cholinesterase and free radicals related diseases, for example, neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease and stroke, and free-radical related diseases such as heart disease, myocardial ischemia, diabetes and other cardiovascular and cerebrovascular diseases.

Compounds with neural protective effect, and preparation and use thereof

The present invention provides pyrazine derivatives of formula I and pharmaceutically acceptable salts thereof, wherein the designation of R, R, Rand Ris provided herein. The invention also provides syntheses for preparation of such compounds. The invention further provides methods of use of these compounds and pharmaceutical compositions containing them for treatment and/or prevention of diseases and for manufacture of medicaments. These compounds and pharmaceutical compositions have antioxidative and thrombolytic effects, and thus can be used for the treatment and/or prevention of cerebral stroke caused by ischemia, and used for manufacture of medicaments for the treatment and/or prevention of nervous system diseases caused by excessive amount of radicals and/or thrombosis, infectious diseases, metabolic system diseases, cardiovascular and cerebrovascular diseases, and age-related degenerative diseases.

Lighting device having at least one heat sink

The present invention provides novel nitrones, their preparation and use. The novel compounds have the following formula: I The compounds of the present invention have strong antioxidative activity, and are thrombolytic. These compounds can be used to treat and/or prevent diseases caused by overproduction of free radicals and/or formation of thrombus. 

Nitrone compounds, process of preparation thereof, and use thereof in medicament manufacture

The present invention relates to an andrographolide derivative of the formula (I), wherein R, Rand Rare same or different substituents selected from hydrogen, substituted or unsubstituted organic acid radicals, inorganic acid radicals, alkyl, aryl or heteroaryl, and at least one of R, Rand Ris R-lipoic acid, S-lipoic acid or a mixture thereof, or corresponding dihydrolipoic acids thereof, or N-acetylcysteine radical. The derivative has good antitumor effect, can induce apoptosis of tumor cells, can directly kill Gram-positive bacteria () and drug resistance bacteria (MRSA5676 and MRSA5677), can inhibit the QS-system of Gram-negative bacteria (), can inhibit and destroy the formation of biofilm of; and exhibits significant hypoglycemic effect, so that it can be used in manufacture of medicaments for treatment of cancers, inflammation, diabetes, and bacterial and viral infections. 

Andrographolide derivatives and use thereof in manufacture of medicaments

The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions There are a variety of neurological disorders that can be treated using the present invention, including, for example, the following: neurological disorders arising from trauma, ischemic or hypoxic conditions that can be treated include stroke, hypoglycemia, cerebral ischemia, cardiac arrest, spinal cord trauma, head trauma, perinatal hypoxia, cardiac arrest and hypoglycemic neuronal damage; neurodegenerative disorders such as epilepsy, Alzheimer's disease, Huntington's disease Parkinsonism, and amyotrophic lateral sclerosis; other diseases or disorders such as convulsion, pain, depression, anxiety, schizophrenia, muscle spasms, migraine headaches, urinary incontinence, nicotine withdrawal, opiate tolerance and withdrawal, emesis, brain edema, tardive dyskinesia, AIDS-induced dementia, ocular damage, retinopathy, cognitive disorders, and neuronal injury associated with HIV-infection such as dysfunction in cognition, movement and sensation.

Aminoadamantane derivatives as therapeutic agents

The invention provides novel adamantane compounds having one of the following formulas: The present invention also relates to compositions and methods for treating and/or preventing neurological and inflammatory disorders in a patient by administering a therapeutically effective amount of the compounds of formula (I), (II) or (III) and a pharmaceutically acceptable carrier.

Antioxidant nitroxides and nitrones as therapeutic agents

The present invention provides novel conjugates of camptothecin compounds and long-chain unsaturated fatty acid. The novel conjugates can be used to treat mammalian cell proliferative diseases such as cancer.

Growing community of inventors

Guangzhou, China

Yuqiang Wang