35985-34-3

Upstream product

• 34273-01-3 4,4-diphenylpiperidine 
• 627-18-9 1-bromo-3-propanol 
• 71-43-2 benzene 
• 41661-47-6 piperidin-4-one 
• 40105-95-1 4,4-diphenyl-N-benzylpiperidine 
• 40105-98-4 1-Ethoxycarbonyl-4,4-diphenylpiperidin 
• 71-36-3 butan-1-ol 
• 14554-17-7 N-benzyl-3-benzoyl-4-hydroxy-4-phenylpiperidine 
• 63843-83-4 1-benzyl-4-hydroxy-4-phenylpiperidine 
• 3612-20-2 1-phenylmethyl-4-piperidone 
• 10338-69-9 1,2,3,6-tetrahydro-4-phenylpyridine 
• 40064-34-4 piperidine-4,4-diol hydrochloride 

Downstream Products

• 116395-62-1 acetoacetic acid 3-(4,4-diphenylpiperidin-1-yl)propyl ester 
• 157066-79-0 2,6-dimethyl-4-(4-nitrophenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid [3-(4,4-diphenylpiperidine-1-yl)-propyl] ester methyl ester 
• 119934-51-9 Niguldipine hydrochloride 

Relevant academic research and scientific papers

Use of alpha-1C specific compounds to treat benign prostatic hyperplasia

PCT No. PCT/US93/10950 Sec. 371 Date Apr. 1, 1997 Sec. 102(e) Date Apr. 1, 1997 PCT Filed Nov. 12, 1993 PCT Pub. No. WO94/10989 PCT Pub. Date May 26, 1994A method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound which binds to a human alpha 1C adrenergic receptor with a binding affinity greater than ten-fold higher than the binding affinity with which the compound binds to a human alpha 1A adrenergic receptor, a human alpha 1B adrenergic receptor, and a human histamine H1 receptor, and, binds to a human alpha 2 adrenergic receptor with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to such alpha 1C adrenergic receptor. Compounds meeting these criteria are provided.

ALPHA1C SPECIFIC COMPOUNDS TO TREAT BENIGN PROSTATIC HYPERPLASIA

This invention provides a method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of an α 1C antagonist which (a) binds to a human α 1C adrenergic receptor with a binding affinity greater than 100-fold higher than the binding affinity with which the α 1C antagonist binds to a human α 1A adrenergic receptor, a human α 1B adrenergic receptor, and a human histamine H 1 receptor; and (b) binds to a human α 2 adrenergic receptor with a binding affinity which is greater than 100-fold lower than the binding affinity with which the α 1C antagonist binds to such α 1C adrenergic receptor.The invention further provides a method of inhibiting contraction of a prostate tissue which comprises contacting the prostate tissue with an effective contraction-inhibiting amount of an α 1C antagonist which (a) binds to a human α 1C adrenergic receptor with a binding affinity greater than 100-fold higher than the binding affinity with which the α 1C antagonist binds to a human α 1A adrenergic receptor, a human α 1B adrenergic receptor, and a human histamine H 1 receptor; and (b) binds to a human α 2 adrenergic receptor with a binding affinity which is greater than 100-fold lower than the binding affinity with which the α 1C antagonist binds to such α 1C adrenergic receptor.

Aromatic amine derivatives

This invention relates to novel aromatic amine compounds having the structure: STR1 where each W, Z1 and Z2 is independently H, C1 -C6 alkyl, C1 -C6 alkoxy, OH, F, Cl, Br, I, NO2, CN, SO2 NHR3, NR42, CONR32, COR5 ; where each R1 and R2 is independently H, C1 -C6 straight or branched chain alkyl or phenyl; where each X and Y is independently CH2, NR4, S, S=O, SO2 ; where n is 0, 1 or 2; where each p and q is independently 1 or 2; where R3 is H, C1 -C6 straight or branched chain alkyl or phenyl; where R4 is H, C1 -C6 straight or branched chain alkyl or COR3 ; and where R5 is H, C1 -C6 straight or branched chain alkyl or phenyl, C1 -C6 straight or branched chain alkoxy or OH. In addition the invention includes using such compounds for the treatment of benign prostatic hyperplasia, lowering intraocular pressure and inhibiting cholesterol synthesis.

USE OF ALPHA-1C SPECIFIC COMPOUNDS TO TREAT BENIGN PROSTATIC HYPERPLASIA

The subject invention provides a method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound which binds to a human . alpha. 1C adrenergic receptor with a binding affinity greater than ten-fold higher than the binding affinity with which the compound binds to a human α 1A adrenergic receptor, a human α 1B adrenergic receptor, a human histamine H 1 receptor and α 2 adrenergic receptor. The subject invention also provides a method of inhibiting contraction of prostate tissue which comprises contacting the prostate tissue with an effective contraction-inhibiting amount of such compound.

Use of α1C specific compounds to treat benign prostatic hyperlasia

A method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound which binds to a human α1C adrenergic receptor with a binding affinity greater than ten-fold higher than the binding affinity with which the compound binds to a human α1A adrenergic receptor, a human α1B adrenergic receptor, and a human histamine H1 receptor, and, binds to a human α2 adrenergic receptor with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to such α1C adrenergic receptor. Compounds meeting these criteria are provided.

Optically-active 1,4-dihydropyridine

The invention relates to 3-methyl-5-[3-(4,4-diphenylpiperid-1-yl)-propyl] (+)-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-piperidine-3,5-dicarboxylate and its salts and to their preparation and use.

Diaryl piperidine containing esters of 1,4-dihydropyridines and coronary therapeutic use

Diaryl compounds of formula I STR1 wherein Ar represents a ring of the formula STR2 in which Y denotes oxygen (O), sulfur (S), vinylene (--CH=CH--), azomethine (--CH=N--) or a group of the formula STR3 R1, R2 and R3 are identical or different and denote h

Synthesis, physico-chemical properties and pharmacological screening results of budipine and related 1-alkyl-4,4-diphenylpiperidines

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-Diarylpiperidines and process of making the same

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