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1. 发明申请

WO2019103915A1 COMPOSITIONS AND METHODS FOR TREATMENT OF EYE DISEASES 审中-公开
公开(公告)号：WO2019103915A1
公开(公告)日：2019-05-31
申请号：PCT/US2018/061357
申请日：2018-11-15
申请人： THE JOHNS HOPKINS UNIVERSITY , NACUITY PHARMACEUTICALS, INC.
发明人： CAMPOCHIARO, Peter, A. , WALL, G., Michael
IPC分类号： A61K31/16 , A61P27/02 , A61P39/06
摘要： The present invention includes compositions and methods for treating an eye disease caused by oxidative damage in a subject in need thereof, the method comprising: identifying that the subject has a compromised blood-retinal barrier; and providing an effective amount of an Nacetylcysteine amide (NACA) sufficient to afford or reach a concentration of NACA in a retina that is greater than the concentration in plasma over the same time period.

2. 发明申请

WO2020146660A1 N-ACETYLCYSTEINE AMIDE (NACA) AND (2R,2R')-3-3'-DISULFANEDIYL BIS (2-ACETAMIDOPROPANAMIDE) (DINACA) FOR PREVENTION AND TREATMENT OF RADIATION PNEUMONITIS AND TREATMENT OF PULMONARY FUNCTION IN CYSTIC FIBROSIS 审中-公开
公开(公告)号：WO2020146660A1
公开(公告)日：2020-07-16
申请号：PCT/US2020/012968
申请日：2020-01-09
申请人： NACUITY PHARMACEUTICALS, INC.
发明人： WALL, G., Michael
IPC分类号： A61K31/16 , A61P11/00 , A61P39/06
摘要： The present invention includes a method for the use of N-acetylcysteine amide (NACA) or (2R,2R')-3,3'-disulfanediyl bis(2-acetamidopropanamide) (diNACA) for prevention and treatment of radiation pneumonitis and treatment of pulmonary function in Cystic Fibrosis (CF), chronic obstructive pulmonary disease (COPD), or bronchitis in a human that comprises administering to the human a therapeutically effective amount of NACA or diNACA sufficient to treat, reduce the symptoms, or prevent radiation pneumonitis and treatment of pulmonary function in Cystic Fibrosis (CF), chronic obstructive pulmonary disease (COPD), bronchitis, or respiratory disorder due to oxidative stress, and diNACA for the reduction of mucus viscosity and/or elasticity.

3. 发明申请

WO2020146666A9 N-ACETYLCYSTEINE AMIDE (NACA) AND (2R,2R')-3,3'-DISULFANEDIYL BIS (2-ACETAMIDOPROPANAMIDE) (DINACA) FOR THE PREVENTION AND TREATMENT OF RADIATION DERMATITIS AND SKIN LIGHTENING, SKIN WHITENING AND SKIN IMPROVEMENT 审中-公开
公开(公告)号：WO2020146666A9
公开(公告)日：2020-07-16
申请号：PCT/US2020/012975
申请日：2020-01-09
申请人： NACUITY PHARMACEUTICALS, INC.
发明人： WALL, G., Michael
IPC分类号： A61K31/16 , A61P17/00 , A61P39/06
摘要： The present invention includes a method for the use of N-acetylcysteine (NAC), N-acetylcysteine amide (NAC A) or (2R,2R')-3,3'-disulfanediyl bis(2-acetamidopropanamide) (diNACA) for the prevention and treatment of radiation dermatitis, radiation damage to the skin, xeroderma pigmentosa or protect patients with xeroderma pigmentosa from skin damage caused by exposure to the sun or other radiation, bioweapons, chemical bums, heat bums, contact damage caused by friction, contact dermatitis, hypersensitivity reactions and skin wrinkles and dehydration, skin lightening, skin whitening, and/or skin improvement in a human that comprises administering to the human a therapeutically effective amount of NAC, NACA or diNACA.

4. 发明申请

WO2020146666A1 N-ACETYLCYSTEINE AMIDE (NACA) AND (2R,2R')-3,3'-DISULFANEDIYL BIS (2-ACETAMIDOPROPANAMIDE) (DINACA) FOR THE PREVENTION AND TREATMENT OF RADIATION DERMATITIS AND SKIN LIGHTENING, SKIN WHITENING AND SKIN IMPROVEMENT 审中-公开
公开(公告)号：WO2020146666A1
公开(公告)日：2020-07-16
申请号：PCT/US2020/012975
申请日：2020-01-09
申请人： NACUITY PHARMACEUTICALS, INC.
发明人： WALL, G., Michael
IPC分类号： A61K31/16 , A61P17/00 , A61P39/06
摘要： The present invention includes a method for the use of N-acetylcysteine (NAC), N-acetylcysteine amide (NAC A) or (2R,2R')-3,3'-disulfanediyl bis(2-acetamidopropanamide) (diNACA) for the prevention and treatment of radiation dermatitis, radiation damage to the skin, xeroderma pigmentosa or protect patients with xeroderma pigmentosa from skin damage caused by exposure to the sun or other radiation, bioweapons, chemical bums, heat bums, contact damage caused by friction, contact dermatitis, hypersensitivity reactions and skin wrinkles and dehydration, skin lightening, skin whitening, and/or skin improvement in a human that comprises administering to the human a therapeutically effective amount of NAC, NACA or diNACA.

5. 发明申请

WO2019060623A1 METHOD FOR PREPARATION OF N-ACETYL CYSTEINE AMIDE AND DERIVATIVES THEREOF 审中-公开
公开(公告)号：WO2019060623A1
公开(公告)日：2019-03-28
申请号：PCT/US2018/052065
申请日：2018-09-20
申请人： NACUITY PHARMACEUTICALS, INC.
发明人： WALL, G., Michael , JOHNSON, Doug , RUBENSTEIN, Anja , TUCKER, Rodney , BOLGER, Josh
IPC分类号： C07C319/06 , C07C323/59 , C07C323/60
摘要： The present invention includes methods for making and isolating N-acetylcysteine amide, intermediates and derivatives thereof comprising: contacting cystine with an alcohol and a chlorinating reagent to form an organic solution containing L-cystine dimethylester dihydrochloride; combining dried or undried L-cystine dimethylester dihydrochloride with a triethylamine, an acetic anhydride, and an acetonitrile to form a di-N-acetylcystine dimethylester; mixing dried di-N-acetylcystine dimethylester with ammonium hydroxide to form a di-N-acetylcystine amide; and separating dried di-N-acetylcystine dimethylester into N-acetylcysteine amide with dithiothreitol, triethylamine and an alcohol.

6. 发明申请

WO2022204221A1 TREATMENT OF FERROPTOSIS 审中-公开
公开(公告)号：WO2022204221A1
公开(公告)日：2022-09-29
申请号：PCT/US2022/021452
申请日：2022-03-23
申请人： NACUITY PHARMACEUTICALS, INC.
发明人： WALL, G., Michael , BUSH, Ashley , BUSH, Ashley , JENKINS, Nicole
IPC分类号： A61K31/05 , A61K31/145 , A61K31/198
摘要： The present invention relates in general to the field of compositions and methods for using N- acetylcysteine amide (NACA) or (2R,2R')-3,3'-disulfanediyl bis(2-acetamidopropanamide) (diNACA) for treating or alleviating a disorder or condition associated with ferroptosis, which can cause or contribute to diseases, disorders and conditions including aging associated with declining cognition, cognitive impairment, declining physical function, physical decline, elevated inflammation, endothelial dysfunction, insulin resistance, central obesity, loss of muscle mass (sarcopenia), neurological diseases and disorders, including neurodegeneration, stroke, including ischemic stroke and post-hemorrhagic stroke damage, and neurotrauma, including traumatic brain injury, Alzheimers disease, Huntington's disease, Niemann-Pick disease, Parkinson's disease, motor neuron disease, Amyotrophic Lateral Sclerosis, Sedaghatian-type spondylo-metaphyseal dysplasia, cancer, including breast cancer, kidney injuries including ischemia-reperfusion and oxalic acid-induced kidney damage, rhabdomyolosis and acute renal failure, mitochondrial dysfunction leading to osteoporosis, lysosomal storage diseases including cystinosis, Danon, Fabry, Krabbe, Gaucher, Niemann-Pick, Pompe and Salla diseases.

7. 发明申请

WO2020146674A1 TREATMENT OF AGE-RELATED MACULAR DEGENERATION, GLAUCOMA, AND DIABETIC RETINOPATHY WITH N-ACETYLICYSTEINE AMIDE (NACA) OR 2R,2R')-3-3'-DISULFANEDIYL BIS (2-ACETAMIDOPROPANAMIDE) (DINACA) 审中-公开
公开(公告)号：WO2020146674A1
公开(公告)日：2020-07-16
申请号：PCT/US2020/012983
申请日：2020-01-09
申请人： NACUITY PHARMACEUTICALS, INC.
发明人： WALL, G., Michael
IPC分类号： A61L31/16 , A61P27/02
摘要： The present invention includes a method for the treatment of age-related macular degeneration, glaucoma, or diabetic retinopathy in a human that comprises administering to the human a therapeutically effective amount of N-acetyl cysteine amide (NACA) or (2R,2R')-3,3'- disulfanediyl bis(2-acetamidopropanamide) (diNACA) sufficient to treat or reduce the symptoms of the age-related macular degeneration, glaucoma, or diabetic retinopathy.

8. 发明申请

WO2019094383A1 METHODS OF MAKING DEUTERIUM-ENRICHED N-ACETYLCYSTEINE AMIDE (D-NACA) AND (2R,2R')-3,3' -DISULFANEDIYL BIS(2-ACETAMIDOPROPANAMIDE) (DINACA) AND USING D-NACA AND DINACA TO TREAT DISEASES INVOLVING OXIDATIVE STRESS 审中-公开
公开(公告)号：WO2019094383A1
公开(公告)日：2019-05-16
申请号：PCT/US2018/059446
申请日：2018-11-06
申请人： NACUITY PHARMACEUTICALS, INC.
发明人： WALL, G., Michael
IPC分类号： A61K31/195 , C07C233/76 , C08K5/20 , A61K31/16 , A61P39/06
摘要： The present invention includes pharmaceutical composition comprising (2R,2R')- 3,3'-disulfanediyl bis(2-acetamidopropanamide)(diNACA) or D3-N-acetyl cysteine amide, or a physiologically acceptable salt thereof, having a deuterium enrichment above the natural abundance of deuterium, and derivatives or solids thereof, and methods of using diNACA to treat eye diseases and other diseases associated with oxidative damage including, e.g., antivenom, beta-thallassemia, cataract, chronic obstructive pulmonary disease, macular degeneration, contrast-induced nephropathy, asthma, lung contusion, methamphetamine- induced oxidative stress, multiple sclerosis, Parkinson's disease, platelet apoptosis, Tardive dyskinesia, Alzheimer disease, HIV- 1 -associated dementia, mitochondrial diseases, myocardial myopathy, neurodegenerative diseases, pulmonary fibrosis, skin pigmentation, skin in need of rejuventation, antimicrobial infection, Friedreich's ataxia.

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