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Usage

Uses

Used in Neurology:
Siponimod is used as a disease-modifying therapy for relapsing forms of multiple sclerosis. It functions by targeting specific receptors in the central nervous system, leading to a reduction in inflammation and the migration of immune cells into the brain and spinal cord. This results in a decreased frequency of relapses and a slowed progression of disability in patients with relapsing multiple sclerosis.
Used in Pharmaceutical Industry:
In the pharmaceutical industry, Siponimod is utilized as a novel treatment option for patients suffering from multiple sclerosis. Its unique mechanism of action, which involves the modulation of immune responses through the targeting of specific receptors, positions it as a valuable addition to the current treatment landscape for this condition.
It is crucial for patients taking Siponimod to be closely monitored by their healthcare providers to ensure appropriate dosing and to detect any potential side effects, such as headaches, high blood pressure, and liver enzyme elevations. Regular monitoring helps maintain the safety and efficacy of Siponimod as a treatment for relapsing multiple sclerosis.

Upstream product

• 1034188-32-3 4-cyclohexyl-3-(trifluoromethyl)benzamide 
• 13376-27-7 1-cyclohexyl-2-(trifluoromethyl)benzene 
• 161622-14-6 4-bromo-3-(trifluoromethyl)benzoic acid 
• 89490-05-1 cyclohex-1-enylboronic acid 
• 1034188-31-2 2-(trifluoromethyl)-2',3',4',5'-tetrahydro-[1,1'-biphenyl]-4-carboxylic acid 
• 261952-20-9 1-bromo-4-methyl-2-(trifluoromethyl)benzene 
• 1449293-47-3 1-cyclohex-1-enyl-4-methyl-2-trifluoromethylbenzene 
• 1449293-48-4 1-cyclohexyl-4-methyl-2-trifluoromethylbenzene 
• 13376-26-6 1-cyclohex-1-enyl-2-trifluoromethylbenzene 
• 392-83-6 o-trifluoromethylphenyl bromide 
• 108-94-1 cyclohexanone 
• 1131594-38-1 C₁₄H₁₇BrO₂ 
• 18594-05-3 4-cyclohexylacetophenone 
• 827-52-1 1-phenyl-1-cyclohexane 

Downstream Products

• 957205-23-1 [4-cyclohexyl-3-(trifluoromethyl)phenyl]methanol 
• 800381-60-6 4-(bromomethyl)-1-cyclohexyl-2-(trifluoromethyl)benzene 
• 1418144-65-6 N-(4-cyclohexyl-3-trifluoromethylbenzyloxy)acetimidic acid ethyl ester 
• 1418144-66-7 (E)-1-(3-ethyl-4-(hydroxymethyl)phenyl)ethan-1-one-O-(4-cyclohexyl-3-(trifluoromethyl)benzyl)-oxime 
• 1230487-01-0 4-[(1E)-1-([[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]imino)ethyl]-2-ethylbenzaldehyde 
• 1230487-00-9 Siponimod 

Relevant academic research and scientific papers

Preparation method of siponimod intermediate

The invention relates to a preparation method of a siponimod intermediate, belonging to the field of medicinal chemistry. The preparation method comprises the following steps: with cyclohexylbenzene as a starting material, carrying out reactions such as Friedel-Crafts acylation, bromination, oxidation, esterification, trifluoromethylation and hydrolysis to obtain 4-cyclohexyl-3-trifluoromethyl benzoic acid. Such a technical scheme provided by the invention is simple and convenient to operate, easy to implement, mild in reaction conditions, high in yield, high in purity, low in cost and suitable for industrial production.

PROCESS FOR PREPARATION OF SIPONIMOD, ITS SALTS AND SOLID STATE FORMS THEREOF

The present application provides process for preparation of siponimod, intermediates of siponimod, salts of siponimod, polymorphic forms and solid dispersions of siponimod and its salts thereof. The present application specifically provides crystalline polymorphic forms of siponimod base, siponimod hemifumarate and other salts and pharmaceutical compositions thereof. Also provided are solid dispersions of siponimod hemifumarate and pharmaceutical compositions containing them.

AZETIDINE MODULATORS OF THE SPHINGOSINE 1-PHOSPHATE RECEPTOR

Described are deuterium-substituted azetidine compounds of Formula (I), which are modulators of sphingosine 1 -phosphate receptor. Also described are pharmaceutical compositions comprising the deuterium-substituted azetidine compounds, and methods of use thereof.

PROCESS FOR PREPARING N-(4-CYCLOHEXYL-3-TRIFLUOROMETHYL-BENZYLOXY)-ACETIMIDIC ACID ETHYL ESTER

This invention relates to novel processes for synthesizing N-(4-cyclohexyl-3-trifluoromethyl-benzyloxy)-acetimidic acid ethyl ester and to the compound of formula I and other intermediates that are used in such processes.

OXADIAZOLE DERIVATIVES AS S1P1 RECEPTOR AGONISTS

The present invention relates to novel oxadiazole compounds of formula (I) having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.

INDOLE DERIVATIVES AS S1P1 RECEPTOR AGONISTS

The invention relates to compounds of formula (I) wherein one of R5 and R6 is hydrogen or R2 and the other is (a) processes for their preparation, pharmaceutical compositions containing them and their use in the treatment

OXADIAZOLE SUBSTITUTED INDAZOLE DERIVATIVES FOR USE AS SPHINGOSINE 1-PHOSPHATE (S1P) AGONISTS

The present invention provides compounds of formula (I) or salts thereof, having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders mediated by S1P1 receptors.