Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/16—Amides, e.g. hydroxamic acids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/16—Amides, e.g. hydroxamic acids
  • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P27/00—Drugs for disorders of the senses
  • A61P27/02—Ophthalmic agents
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

• Age-related macular degeneration is the leading cause of blindness in the elderly, with an incidence of about 20% in adults 65 years of age increasing to 37% in individuals 75 years or older.
• Non-exudative AMD is characterized by drusen accumulation and atrophy of rod and cone photoreceptors in the outer retina, retinal pigment epithelium (RPE), Bruch's membrane and choriocapillaris; while exudative AMD leads to choroidal neovascularization (Green and Enger, Ophthalmol, 100:1519-35, 1993; Green et al., Ophthalmol, 92:615-27, 1985; Green and Key, Trans Am Ophthalmol Soc, 75:180-254, 1977; Bressler et al., Retina, 14:130-42, 1994; Schneider et al., Retina, 18:242-50, 1998; Green and Kuchle (1997).
• MAO inhibitors have been described for other disorders.
• the MAO inhibitors selegiline and desmethylselegiline have been shown to protect ganglion cells from NMDA-induced excitotoxicity (Takahata et al., Eur J Pharmacol, 458(l-2):81-9, 2003).
• Deprenyl has also been shown to protect ganglion cells following optic nerve crush (Buys et al., Cur Eye Res, 14(2): 119-126, 1995) or serum deprivation (Ragaiey et al., J Ocul Pharmacol Ther, 13(5):479-88, 1997).
• Preferred compounds of formula I are compounds wherein:
• R 4 , R 5 are independently H, CH 3 R 6 is H, CH 3
• Retinal diseases are often disruptive to the tissue and can result in a loss of visual function for millions of patients.
• retinal tissues can be damaged by environmental factors, such as light exposure, which is known to contribute to the progression of retinal degenerative disorders such as AMD (Young 1988; Taylor et al. 1992; Cruickshank et al. 1993).
• AMD retinal degenerative disorders
• Early stages of macular degeneration are typically treated by combinations of antioxidants or anti-inflammatory agents whose efficacy has not been demonstrated in the clinic.
• Advanced stages of macular degeneration that lead to severe vision loss are treated either by surgical removal of membranes from the subretinal space, laser photocoagulation, photodynamic therapy, and most recently with VEGF blockers in patients with exudative AMD.
• the efficacy of Safmamide, a short acting MAO-B inhibitor, to protect retinal cells against the induction of photochemical lesions by blue-light exposure was assessed by measuring light-induced changes in retinal functioning (electroretinogram (ERG)) and evaluating retinal morphology changes.
• ERG electroretinogram
• Significant dose-dependent protection of retinal function was measured in light exposed rats after a 5-day recovery period in rats dosed with Safinamide (5-60 mg/kg).
• ERGs were not significantly different from normal after a 1 -month recovery period in Safinamide dosed rats (15 to 60 mg/kg).

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• Health & Medical Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• Veterinary Medicine (AREA)
• Chemical & Material Sciences (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Medicinal Chemistry (AREA)
• Animal Behavior & Ethology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Epidemiology (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Engineering & Computer Science (AREA)
• Ophthalmology & Optometry (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicinal Preparation (AREA)

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• 2007
  • 2007-07-27 AU AU2007278837A patent/AU2007278837A1/en not_active Abandoned
  • 2007-07-27 EP EP07813482A patent/EP2046451A1/en not_active Ceased
  • 2007-07-27 WO PCT/US2007/074603 patent/WO2008014457A1/en not_active Ceased
  • 2007-07-27 CN CNA2007800283812A patent/CN101495185A/zh active Pending
  • 2007-07-27 BR BRPI0714985-9A patent/BRPI0714985A2/pt not_active IP Right Cessation
  • 2007-07-27 ZA ZA200900234A patent/ZA200900234B/xx unknown
  • 2007-07-27 MX MX2009000792A patent/MX2009000792A/es not_active Application Discontinuation
  • 2007-07-27 JP JP2009522019A patent/JP2009544740A/ja active Pending
  • 2007-07-27 US US12/375,247 patent/US20110160308A1/en not_active Abandoned
  • 2007-07-27 KR KR1020097002001A patent/KR20090034365A/ko not_active Withdrawn
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