57368-81-7

Upstream product

• 33953-37-6 N-(piperidin-4-yl)benzamide 
• 584-08-7 potassium carbonate 

Downstream Products

• 57368-82-8 4-Amino-1-(4-phenyl-4-oxobutyl)piperidine 
• 57479-67-1 4-(4-benzoylamino-piperidin-1-yl)-1-phenyl-butan-1-ol 

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.

DNA ENDODING HUMAN ALPHA 1 ADRENERGIC RECEPTORS

This invention provides an isolated nucleic acid, vectors, transformed mammalian cells and non-human transgenic animals that encode and express normal or mutant alpha 1a, alpha 1b and alpha 1c adrenergic receptor genes. This invention also provides a protein, and an antibody directed to the protein and pharmaceutical compounds related to alpha 1a, alpha 1b and alpha 1c adrenergic receptors. This invention provides nucleic acid probes, and antisense oligonucleotides complementary to alpha 1a, alpha 1b and alpha 1c adrenergic receptor genes. This invention further provides methods for determining ligand binding, detecting expression, drug screening, and treatments for alleviating abnormalities associated with human alpha 1a, alpha 1b and alpha 1c adrenergic receptors.

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.

Pharmaceutical compositions and methods of treating hypertension

Pharmaceutical compositions containing a group of heterocyclic compounds and their use in treatment of disorders and diseases of the cardiovascular system and/or in the treatment of superficial and deep allergic phenomena is described. These compounds used in the composition and/or methods are piperidine compounds linked by the nitrogen atom to a substituted or unsubstituted cycloalkyl, aryl or heterocyclic radical through the intermediary of a group selected from a lower-alkylene radical, a monoketo lower-alkylene radical or a hydroxy-lower-alkylene radical, or a bivalent radical of the formula --NH.CO.(CH2)n -- where n is 1, 2 or 3, STR1 or --0-(lower-alkylene)--. The piperidine ring is further substituted by an acylamino residue.

HETEROCYCLIC COMPOUNDS

A group of heterocyclic compounds useful in the treatment of disorders and diseases of the cardiovascular system and/or in the treatment of superficial and deep allergic phenomena is described. These compounds are piperidine compounds linked by the nitrogen atom to a substituted or unsubstituted phenyl radical through the intermediary of a group selected from a lower-alkylene radical, a mono-keto lower alkylene radical or a hydroxy-lower-alkylene radical, or a bivalent radical of the formula EQU1 or--O--(lower-alkylene)-. The piperidine rings are further substituted by a benzamido, substituted benzamido or cyclohexylcarboxamido residue.