- A flupirtin derivative and its inorganic acid salt preparation method (by machine translation)
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The invention relates to a kind of flupirtine derivative and its inorganic acid salt of the preparation method, the [...] derivatives by the following chemical formula 1 that: The [...] derivative is maleic acid flupirtin synthesis process and/or storage of produced in the process of an important impurity. The preparation method according to this application, and may be the above-mentioned yield of flupirtine derivative and its inorganic acid salt, each step of the reaction yield can be up to 55% or more. (by machine translation)
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- Discovery of Aromatic Carbamates that Confer Neuroprotective Activity by Enhancing Autophagy and Inducing the Anti-Apoptotic Protein B-Cell Lymphoma 2 (Bcl-2)
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Neurodegenerative diseases share certain pathophysiological hallmarks that represent common targets for drug discovery. In particular, dysfunction of proteostasis and the resultant apoptotic death of neurons represent common pathways for pharmacological intervention. A library of aromatic carbamate derivatives based on the clinically available drug flupirtine was synthesized to determine a structure-activity relationship for neuroprotective activity. Several derivatives were identified that possess greater protective effect in human induced pluripotent stem cell-derived neurons, protecting up to 80% of neurons against etoposide-induced apoptosis at concentrations as low as 100 nM. The developed aromatic carbamates possess physicochemical properties desirable for CNS therapeutics. The primary known mechanisms of action of the parent scaffold are not responsible for the observed neuroprotective activity. Herein, we demonstrate that neuroprotective aromatic carbamates function to increase the Bcl-2/Bax ratio to an antiapoptotic state and activate autophagy through induction of beclin 1.
- Kinarivala, Nihar,Patel, Ronak,Boustany, Rose-Mary,Al-Ahmad, Abraham,Trippier, Paul C.
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p. 9739 - 9756
(2017/12/26)
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- Use of a combination of active substances containing bioquinones for the production of cosmetic or dermatological preparations
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The invention relates to the use of a compound or several compounds from the group of bioquinones a) in combination with a compound or several compounds from the group of potassium channel openers and/or b) in combination with a compound or several compounds from the group of 5-alpha-reductase inhibitors, for the production of cosmetic or dermatological preparations for treatment of the scalp and for hair in order to prolong the anagenic phase and/or for the treatment and prophylaxis of seborrhoeic symptoms, optionally by additionally using one or several compounds from the group formed from carnitine, arginine, succinic acid, folic acid, conjugated fatty acids and respectively the derivatives thereof, in addition to antioxidants.
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- 2,3-Dihydrospiro[1H-4- and 5-azabenzimidazole-2,1'-cyclohexane] (= spiro[cyclohexane-1,2'(3'H)-1'H-imidazo[4,5-b]pyridine] and spiro[cyclohexane-1,2'(3'H)-1'H-imidazo[4,5-c]pyridine]): Reactions with nucleophiles
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The readily available title compounds 4a and 24 react with N-, O-, S-, and C-nucleophiles in presence of MnO2 to give the corresponding mono- or disubstituted 2H-azabenzimidazoles (= azaisobenzimidazoles), e.g., 11-18 and 26a-h, respectively, or 2,3-dihydro-1H-azabenzimidazoles (= dihydro-azabenzimidazoles) such as 9 and 10 and 27 and 28, respectively, by a 1,4- or 1,6-Michael addition (Schemes 2 and 4). The bromo-dihydro-1H-azabenzimidazole 4b lost the Br-atom when treated with piperidine or morpholine yielding the corresponding disubstituted 2H-azabenzimidazole 21 (Scheme 3). Reductive ring opening of the substituted spiro compounds leads to mono- and disubstituted diaminopyridines which are intermediates for fused pyridine ring systems with substituents often not available by conventional routes and of potential pharmaceutical interest (see 32-37). E.g., starting from 4a, a three-step synthesis of the analgesic flupirtine maleate (= ethyl {2-amino-6-[(4-fluorobenzyl)amino]pyridin-3-yl}carbamate maleate = Katadolon; 39) and of its non-fluorinated derivative D-7195 is described. Its analogue 40 was similarly made from the spiro compound 24.
- Schwoch,Kramer,Neidlein,Suschitzky
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p. 2175 - 2190
(2007/10/02)
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- 2-Amino-3-acylamino-6-benzylamino-pyridine-derivative having antiepileptic action
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Compounds of the formula STR1 where R is a C1 -C4 alkyl group, a C1 -C4 alkoxy group, a phenoxy group or a phenyl-C1 -C2 -alkoxy group, R1 is hydrogen or a C1 -C4 -alkyl group and R5 is hydrogen or a C1 -C4 -alkyl group and the groups R2, R3, and R4 are the same or different and are hydrogen, halogen atoms, C1 -C4 alkyl groups, C1 -C4 -alkylcarbonyl group, the aminosulfonyl group, the trifluoromethyl group and their acid addition salts are effective as antiepileptics.
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