8-bromo-1,3-dimethyl-3,7-dihydro-purine-2,6-dione; compound with 2-amino-2-methyl-propan-1-ol；8-Brom-1,3-dimethyl-3,7-dihydro-purin-2,6-dion; Verbindung mit 2-Amino-2-methyl-propan-1-ol；8-bromo-3,7-dihydro-1,3-dimethyl-1H-purine-2,6-dione, compd. with 2-amino-2-methyl-1-propanol (1:1)；2-amino-2-methylpropanol 8-bromotheophyllinate；2-amino-2-methylpropan-1-ol;8-bromo-1,3-dimethyl-7H-purine-2,6-dione
参考文献：M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. 美国食品药品监督管理局批准的药物标签用于研究药物诱导的肝损伤，《药物发现今日》，16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007
M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank：按人类发展药物诱导肝损伤风险排名的最大参考药物清单。《药物发现今日》2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015
References:M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. FDA-Approved Drug Labeling for the Study of Drug-Induced Liver Injury, Drug Discovery Today, 16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007
M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. Drug Discov Today 2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015
Section 1. Chemical Product and Company Identification Pamabrom Common Name/ Trade Name Pamabrom Section 4. First Aid Measures Eye Contact Check for and remove any contact lenses. In case of contact, immediately flush eyes with plenty of water for at least 15 minutes. Get medical attention if irritation occurs. Skin Contact Wash with soap and water. Cover the irritated skin with an emollient. Get medical attention if irritation develops. Serious Skin Contact Not available. Inhalation If inhaled, remove to fresh air. If not breathing, give artificial respiration. If breathing is difficult, give oxygen. Get medical attention. Serious Inhalation Not available. Ingestion Do NOT induce vomiting unless directed to do so by medical personnel. Never give anything by mouth to an unconscious person. If large quantities of this material are swallowed, call a physician immediately. Loosen tight clothing such as a collar, tie, belt or waistband. Serious Ingestion Not available. Section 5. Fire and Explosion Data Flammability of the Product May be combustible at high temperature. Auto-Ignition Temperature Not available. Flash Points Not available. Flammable Limits Not available. Products of Combustion These products are carbon oxides (CO, CO2), nitrogen oxides (NO, NO2...), halogenated compounds. Fire Hazards in Presence of Slightly flammable to flammable in presence of heat. Various Substances Non-flammable in presence of shocks. Explosion Hazards in Presence Slightly explosive in presence of open flames and sparks. Non-explosive in presence of shocks. of Various Substances SMALL FIRE: Use DRY chemical powder. Fire Fighting Media and Instructions LARGE FIRE: Use water spray, fog or foam. Do not use water jet. As with most organic solids, fire is possible at elevated temperatures Special Remarks on Fire Hazards Special Remarks on Explosion Fine dust dispersed in air in sufficient concentrations, and in the presences of an ignition source is a potential dust Hazards explosion hazard. Section 6. Accidental Release Measures Small Spill Use appropriate tools to put the spilled solid in a convenient waste disposal container. Finish cleaning by spreading water on the contaminated surface and dispose of according to local and regional authority requirements. Large Spill Use a shovel to put the material into a convenient waste disposal container. Finish cleaning by spreading water on the contaminated surface and allow to evacuate through the sanitary system. Pamabrom Section 7. Handling and Storage Precautions Keep away from heat. Keep away from sources of ignition. Do not breathe dust. Storage Keep container tightly closed. Keep container in a cool, well-ventilated area. Section 8. Exposure Controls/Personal Protection Engineering Controls Use process enclosures, local exhaust ventilation, or other engineering controls to keep airborne levels below recommended exposure limits. If user operations generate dust, fume or mist, use ventilation to keep exposure to airborne contaminants below the exposure limit. Personal Protection Safety glasses. Lab coat. Dust respirator. Be sure to use an approved/certified respirator or equivalent. Gloves. Personal Protection in Case of Splash goggles. Full suit. Dust respirator. Boots. Gloves. A self contained breathing apparatus should be used a Large Spill to avoid inhalation of the product. Suggested protective clothing might not be sufficient; consult a specialist BEFORE handling this product. Exposure Limits Not available. Section 9. Physical and Chemical Properties Physical state and appearance Solid. (Crystalline powder.) Odor Amine like. (Slight.) Taste Not available. Molecular Weight 348.2 g/mole White. Color Not available. pH (1% soln/water) Boiling Point Not available. Melting point: 295 -316 deg. C. Melting Point Decomposition temperature: 300°C (572°F) Not available. Critical Temperature Specific Gravity Not available. Not applicable. Vapor Pressure Vapor Density Not available. Volatility Not available. Odor Threshold Not available. Water/Oil Dist. Coeff. Not available. Ionicity (in Water) Not available. Dispersion Properties Not available. Solubility Soluble in cold water. Solubility in water: 30 g/100 ml @ 25 deg. C Section 10. Stability and Reactivity Data Stability The product is stable. Not available. Instability Temperature Conditions of Instability Excess heat, incompatible materials Incompatibility with various Not available. substances Corrosivity Not available. Pamabrom Not available. Special Remarks on Reactivity Not available. Special Remarks on Corrosivity Polymerization Will not occur. Section 11. Toxicological Information Routes of Entry Inhalation. Ingestion. Toxicity to Animals Acute oral toxicity (LD50): 940 mg/kg [Rat]. Chronic Effects on Humans Not available. Other Toxic Effects on Slightly hazardous in case of skin contact (irritant), of ingestion, of inhalation. Humans Special Remarks on Not available. Toxicity to Animals Special Remarks on Not available. Chronic Effects on Humans Special Remarks on other Potential Health Effects Toxic Effects on Humans Skin: May cause skin irritation. Eyes: Dust may cause eye irritation. Inhalation: Dust may cause respiratory tract irritation. Ingestion: It may cause gastrointestinal tract irritation with nausea or vomiting, and diarrhea. It is a Theophylline analog and is used as an over-the-counter diuretic. Therefore, it can affect the urinary system. Since it is a Theophylline analog, it may have similar effects as Theophylline. Theophylline may affect the cardiovascular system(cardiac arrhythmias, hypotension, pericardial pain), and behavior/Central Nervous System(headache, insomnia, dizziness, restlessness, agitation, excitement, incoordination, somnolence, coma), respiration, metabolism (metabolic acidosis, weight loss), liver, blood (changes in white blood cell count). Section 12. Ecological Information Ecotoxicity Not available. BOD5 and COD Not available. Products of Biodegradation Possibly hazardous short term degradation products are not likely. However, long term degradation products may arise. Toxicity of the Products The products of degradation are more toxic than the product itself. of Biodegradation Special Remarks on the Not available. Products of Biodegradation Section 13. Disposal Considerations Waste Disposal Waste must be disposed of in accordance with federal, state and local environmental control regulations. Pamabrom Section 14. Transport Information DOT Classification Not a DOT controlled material (United States). Identification Not applicable. Not applicable. Special Provisions for Transport DOT (Pictograms) Section 15. Other Regulatory Information and Pictograms TSCA 8(b) inventory: No products were found. Federal and State Regulations California California prop. 65: This product contains the following ingredients for which the State of California has found to cause cancer which would require a warning under the statute: No products were found. Proposition 65 Warnings California prop. 65: This product contains the following ingredients for which the State of California has found to cause birth defects which would require a warning under the statute: No products were found. Other Regulations EINECS: This product is on the European Inventory of Existing Commercial Chemical Substances. Other Classifications WHMIS (Canada) Not controlled under WHMIS (Canada). DSCL (EEC) This product is not classified according S24/25- Avoid contact with skin and eyes. to the EU regulations. Health Hazard HMIS (U.S.A.) 1 National Fire Protection 1 Flammability 1 Association (U.S.A.) Fire Hazard 1 0 Reactivity Health Reactivity 0 Specific hazard Personal Protection E WHMIS (Canada) (Pictograms) DSCL (Europe) (Pictograms) TDG (Canada) (Pictograms) ADR (Europe) (Pictograms) Pamabrom Protective Equipment Gloves. Lab coat. Dust respirator. Be sure to use an approved/certified respirator or equivalent.
SUBSTITUTED 2,4 DIAMINO-QUINOLINE AS NEW MEDICAMENT FOR FIBROSIS, AUTOPHAGY AND CATHEPSINS B (CTSB), L (CTSL) AND D (CTSD) RELATED DISEASES
申请人：Genoscience Pharma SAS
公开号：EP3620164A1
公开（公告）日：2020-03-11
The present invention relates to novel 2-primary amino-4-secondary amino-quinoline derivatives, their manufacture, pharmaceutical compositions comprising them and their use as medicaments. The active compounds of the present invention can be useful as a medicament in the treatment and/or the decreasing and/or the prevention of fibrosis and/or fibrosis related diseases, or for use as a medicament in the treatment and/or the decreasing and/or the prevention of the autophagy and/or autophagy related diseases and for the inhibition of the autophagy flux, or for use in the inhibition of cathepsins B (CTSB), L (CTSL) and/or D (CTSD) and/or cathepsins B (CTSB), L (CTSL) and/or D (CTSD) related diseases; with the proviso that said compounds are not to be used for the treatment of any forms of cancers.
Hydroxylated nebivolol metabolites increase NO release from human endothelial cell preparations in a concentration dependent fashion following acute administration. In addition, hydroxylated nebivolol metabolites, including but not limited to 4-hydroxy-6,6′difluoro-, 4-hydroxy-5-phenol-6,6′difluoro-, and 4-hydroxy-8-pheno-6,6′difluoro-, have the ability to increase the capacity for NO release in human endothelial cells following chronic administration. This invention provides hydroxylated nebivolol metabolites and compositions comprising nebivolol and/or at least one hydroxylated metabolite of nebivolol and/or at least one additional compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof. In addition, this invention provides methods of treating and/or preventing vascular diseases by administering at least one hydroxylated metabolite of nebivolol that is capable of releasing a therapeutically effective amount of nitric oxide to a targeted site affected by the vascular disease. Also, this invention is directed to the treatment and/or prevention of migraine headaches administering at least one hydroxylated metabolite of nebivolol. This invention may also be used in conjunction with or as a single treatment of metabolic syndrome disorders.
[EN] CARBONATE PRODRUGS AND METHODS OF USING THE SAME<br/>[FR] PROMÉDICAMENTS CARBONATÉS ET LEURS MÉTHODES D'UTILISATION
申请人：NEUROGESX INC
公开号：WO2009143297A1
公开（公告）日：2009-11-26
The present invention provides carbonate prodrugs which comprise a carbonic phosphoric anhydride prodrug moiety attached to the hydroxyl or carboxyl group of a parent drug moiety. The prodrugs may provide improved physicochemical properties over the parent drug. Also provided are methods of treating a disease or condition that is responsive to the parent drug using the carbonate prodrugs, as well as kits and unit dosages.
Nitrosated and nitrosylated diuretic compounds, compositions and methods of use
申请人：Garvey S. David
公开号：US20050059655A1
公开（公告）日：2005-03-17
The invention describes novel nitrosated and/or nitrosylated diuretic compounds or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated diuretic compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one diuretic compound of the invention, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; and (l) treating nephropathy.
Nitric Oxide Releasing Prodrugs of Therapeutic Agents
申请人：SATYAM Apparao
公开号：US20110263526A1
公开（公告）日：2011-10-27
The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.
