40105-95-1Relevant articles and documents
4,4-Diphenylpiperidine Compounds or Pharmaceutically Acceptable Salts Thereof, Pharmaceutical Compositions and Uses Thereof
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Paragraph 0086; 0087, (2019/12/06)
The invention belongs to the field of medicine and chemical industry and relates to a 4,4-diphenylpiperidine compound or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same and uses thereof. In particular, the invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, and to a pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt thereof. In the present invention, the compound or pharmaceutically acceptable salt thereof and the pharmaceutical composition have significant activity in blocking an N-type calcium channel, and have good pharmacokinetic properties, can effectively relieve pain, and have a potentialas a new medicament for prevention or treatment of pain, stroke, cerebral ischemia, alcohol addiction, alcoholism, kidney disease, addictive disorder caused by analgesic or tolerance disorder caused by analgesic.
Synthesis, physico-chemical properties and pharmacological screening results of budipine and related 1-alkyl-4,4-diphenylpiperidines
Schaefer,Hackmack,Eistetter,Krueger,Menge,Klosa
, p. 233 - 240 (2007/10/02)
1-Alkyl-4,4-diphenylpiperidines are accessible in a simple manner and with attractive yields by regioselective reaction of certain piperidine derivatives, particularly 3-aroyl-4-aryl-4-hydroxypiperidines, which can be varied widely at the nitrogen atom, with benzene under Friedel-Crafts conditions. The physico-chemical parameters, which are important for the transport and the distribution of a drug in a living system, are discussed for the 1-tert-butyl derivative (13) (budipine) (pK(a), partition coefficient P, saturation concentration c(s), surface activity, protein binding). Rapid absorption of this drug in man is indicated by the size of the permeability coefficient P(M) of the passive transport through artificial phospholipid collodium membranes as well as the invasion curves calculated from P(M). According to pharmacological screening tests, most of the compounds of this class show marked antagonistic activity against experimentally generated pathological states in mice (tremorine and reserpine antagonism) which suggest their potential use in the therapy of Parkinson's disease. 13 has been selected for detailed investigations. Structure-activity analyses did not readily demonstrate the presence of a relationship between the type of alkyl substituent at the piperidine nitrogen atom and the pharmacological screening results obtained.
4,4-Diarylpiperidine compositions and use
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, (2008/06/13)
4,4-Diarylpiperidine compounds, preferably 4,4-diphenylpiperidine which are substituted or unsubstituted in the 1-position of the piperidine nucleus, such as 1-(lower alkyl)-4,4-diphenylpiperidines, 1-(lower alkyl)-4-phenyl-4-tolylpiperidines, and their s