218450-03-4

Upstream product

• 218450-02-3 1-(3,4-difluorophenyl)-2-hydroxy-propan-1-one-oxime 
• 60-29-7 diethyl ether 
• 218450-01-2 1-(3,4-difluorophenyl)-2-hydroxy-propan-1-one 
• 72235-53-1 3,4-difluorobenzylamine 
• 218451-54-8 benzhydrylidene-(3,4-difluoro-benzyl)-amine 
• 289673-35-4 1-(benzhydryliden-amino)-1-(3,4-difluoro-phenyl)-propan-2-ol 

Downstream Products

• 218450-04-5 [1-(3,4-difluorophenyl)-2-hydroxypropyl]carbamic acid tert-butyl ester 
• 218450-16-9 trans(+)-4-(3,4-Difluorophenyl)-5-methyl-2-oxo-oxazolidine-3-carboxylic acid {3-[4-(4-fluorophenyl)-piperidin-1-yl]propyl}amide 
• 218450-10-3 4(S)-(3,4-difluorophenyl)-5(S)-methyloxazolidin-2-one 

Relevant academic research and scientific papers

SUBSTITUTED ANILINIC PIPERIDINES AS MCH SELECTIVE ANTAGONISTS

This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therepeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.

DNA encoding a human melanin concentrating hormone receptor (MCH1) and uses thereof

This invention provides an isolated nucleic acid encoding a human MCH1 receptor, a purified human MCH1 receptor, vectors comprising isolated nucleic acid encoding a human MCH1 receptor, cells comprising such vectors, antibodies directed to a human MCH1 receptor, nucleic acid probes useful for detecting nucleic acid encoding human MCH1 receptors, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding human MCH1 receptors, transgenic, nonhuman animals which express DNA encoding a normal or mutant human MCH1 receptor, methods of isolating a human MCH1 receptor, methods of treating an abnormality that is linked to the activity of a human MCH1 receptor, as well as methods of determining binding of compounds to mammalian MCH1 receptors. This invention provides a method of modifying the feeding behavior of a subject which comprises administering to the subject an amount of an MCH1 antagonist effective to decrease the body mass of the subject and/or decrease the consumption of food by the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of an MCH1 antagonist effective to treat the subject's depression and/or anxiety.

Combination therapy for the treatment of benign prostatic hyperplasia

This invention relates to combination therapy for the treatment of benign prostatic hyperplasia comprising an alpha-1a antagonist and an endothelin antagonist. More specifically, the use of a selective alpha-1a adrenergic receptor antagonist in combination with a subtype non-selective endothelin antagonist provides relief of lower urinary tract symptoms in patients with symptomatic prostatism or benign prostatic hyperplasia. This combination therapy improves lower urinary tract symptoms including increasing urine flow rate, decreasing residual urine volume and improving overall obstructive and irritative symptoms in patients with benign prostatic hyperplasia or symptomatic prostatism.

MORPHOLINONE AND MORPHOLINE DERIVATIVES AND USES THEREOF

This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human α 1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the α 1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Oxazolidinones as alpha 1A receptor antagonists

This invention is directed to oxazolidinone compounds which are selective antagonists for human alpha 1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the alpha 1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Determination of the relative and absolute stereochemistry of a potent and α(1A)-selective adrenoceptor antagonist

The binding affinities and selectivities of antagonists 1-4 for the α(1A)-adrenoceptor are dependent on the stereochemical orientation of the groups at the C-4 and C-5 positions of the oxazolidinone ring. The unambiguous assignment of the relative and abs