http://rdf.ncbi.nlm.nih.gov/pubchem/patent/KR-20100040808-A
Outgoing Links
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| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D209-32 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-44 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P3-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D231-12 |
| filingDate | 2007-06-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_75ca94e33a7e7ee91d66ac01be808b46 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_61650f9ef7d51318a9fbdfe409071ab6 |
| publicationDate | 2010-04-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | KR-20100040808-A |
| titleOfInvention | NASA Precursors with Very High Skin and Membrane Penetration Rate and Their New Pharmaceutical Uses |
| abstract | New positively charged NSAIA drug precursors of structure (1, 2a, 2b, 2c, or 2d) structures 1, 2a, 2b, 2c or 2d have been designed and synthesized.n n n n n n n n Structure 1n n n The above general formula (1, 2a, 2b, 2c, or 2d) "structure 1, 2a, 2b, 2c, or 2d" compounds are prepared by reaction with metal salts, organic base or immobilized base salts of NSAIA and suitable halide compounds. Can be. Positively charged amino groups greatly increase the water solubility of the drug. The positive charge of these drug precursor amino groups will be combined with the negative conversion of the phosphate head group of the membrane. Thus, the local concentration outside the membrane or skin is so high that these drug precursors will easily pass from the high concentration region to the low concentration region. This binding will slightly disrupt the membrane and create some space for the lipophilic portion of the drug precursor. When membrane molecules move, the membrane is weakly cracked by drug precursor binding. The drug precursor is then inserted into the membrane. At pH 7.4, only about 99% of the amino groups are protonated. When the amino group is not protonated, the bond between the amino group of the drug precursor and the phosphate head group of the membrane will break and the drug precursor will enter the membrane completely. The amino group of the drug precursor enters the other side of the membrane and is thus protonated, after which the drug is drawn into the cytoplasm, which is a semi-liquid concentrated aqueous solution or suspension. These drug precursors include diabetes (type I and / or II), abnormal blood glucose and blood lipid levels, stroke, myocardial infarction, and other cardiovascular diseases, Alzheimer's disease, Parkinson's disease, and other neurodegenerative diseases, psoriasis, disc erythema Lupus, systemic lupus erythematosus (SLE), autoimmune hepatitis, scleroderma, Sjogren's syndrome, rheumatoid arthritis, polymyositis, scleroderma, Hashimoto's thyroiditis, juvenile diabetes, Addison's disease, vitiligo, pernicious anemia, glomerulonephritis, and pulmonary fibrosis, multiple Sclerosis (MS), Crohn's disease, and other autoimmune diseases, muscular dystrophy (ALS), ocular pharyngeal muscular dystrophy (OPMS), myotonic dystrophy (MD), Duchenne muscular dystrophy (DMD), polymyositis ( PM), dermatitis (DM), inclusion body myositis (IBM), and other muscular diseases, hemorrhoids, inflammatory hemorrhoids, post-irradiation (artificial) proctitis, chronic ulcerative colitis, adenitis, other inflammatory anal rectal conditions, and anal pruritus, prostate Salt, Prostate cystitis, varicose veins, autoimmune hepatitis, autoimmune nephritis, colon-colitis, enteritis, phlebitis, vasculitis, and other inflammations, skin cancer, breast cancer, colon-rectal cancer, oral cancer, lung and other respiratory system cancers, uterine cancer, reproductive organ cancer, In treating and preventing urinary tract cancer, leukemia, and other blood and lymphoid cancers and other cancers, scars, vascular skin lesions, birthmarks, spots (nevus), ductile fibroids, aging spots (liver spots), and other skin disorders useful. These drug precursors can be administered transdermally without dermal penetration agent assistance. |
| priorityDate | 2007-06-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 174.