384337-90-0

Upstream product

• 384338-23-2 (1-benzyl-4-methyl-piperidin-3-yl)-methyl-amine 
• 3680-69-1 4-chloro-1H-pyrrolo[2,3-d]pyrimidine 
• 1228879-37-5 N,4-dimethyl-1-(phenylmethyl)-3-piperidineamine bishydrochloride 
• 1252883-87-6 N-(1-benzyl-4-methylpiperidin-3-yl)-N-methyl-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine 
• 1354621-59-2 cis-N-benzyl-3-methoxycarbonylamino-4-methylpiperidine 

Downstream Products

• 384336-73-6 (3R,4R)-methyl-(4-methyl-piperidin-3-yl)-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amine 
• 1252883-90-1 N-((3S,4S)-1-benzyl-4-methylpiperidin-3-yl)-N-methyl-7H-pyrrolo[2,3-d] pyrimidin-4-amine 
• 477600-74-1 tert-butyl (3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidine-1-carboxylate 
• 540737-29-9 Tofacitinib citrate 
• 1259404-17-5 tasocitinib 

Relevant academic research and scientific papers

EFFICIENT METHOD FOR THE PREPARATION OF TOFACITINIB CITRATE

Disclosed is a novel process for the synthesis of tofacitinib citrate on an industrial scale with high yields and purity starting with cis-(1-benzyl-4-methyl-piperidin-3-yl)methylamine bis-hydrochloride racemate (intermediate VIII), which comprises: 1. Condensation between intermediates VII and VIII to give intermediate VI 2. Hydrogenation of intermediate VI to give intermediate V 3. Resolution of intermediate V to give intermediate IV with enantiomeric purity >99% 4. Release of intermediate IV in a basic medium to give intermediate III 5. N-acylation reaction of intermediate III to give II (tofacitinib) 6. Salification of intermediate II to give tofacitinib monocitrate (I)

PHARMACEUTICAL COMPOSITIONS AND METHODS OF TREATING DRY EYE DISORDERS

Ophthalmic compositions comprising Inhibitors of Janus kinase-3 (“Jak3”) are useful for treating dry eye disorders and other disorders requiring the wetting of the eye.

PIPERIDINE INHIBITORS OF JANUS KINASE 3

The present invention relates to a new piperidine inhibitors of Janus Kinase 3 activity, pharmaceutical compositions thereof, and methods of use there-of.

COMBINATION THERAPIES FOR RHEUMATOID ARTHRITIS

This disclosure relates to pharmaceutical combination therapies for the treatment or prevention of arthritis, such as rheumatoid arthritis, in a human comprising a Janus Kinase inhibitor or a pharmaceutically acceptable salt thereof and at least one anti-arthritic agent or a pharmaceutically acceptable salt thereof. This disclosure also relates to certain methods for treating or preventing arthritis, such as rheumatoid arthritis, in a human comprising co-administering to a human a Janus Kinase inhibitor or a pharmaceutically acceptable salt thereof and at least one anti-arthritic agent or a pharmaceutically acceptable salt thereof.

METHOD OF TREATMENT OF TRANSPLANT REJECTION

A method of treating or preventing chronic organ transplant rejection comprising administering a compound of the formula (I) wherein R1, R2 and R3 are as defined above.

Method of treatment of atherosclerosis

A method of treating or preventing atherosclerosis comprising administering a compound of the formula wherein R1, R2 and R3 are as defined above.

Chiral salt resolution

A method for resolving enantiomers of a compound containing the structure of the formula: 1wherein R4or R5 may contain one or more asymmetric centers, by mixing a racemic mixture of enantiomers of a compound, containing the structure of said formula; in a solvent, with a resolving compound having a defined stereospecificity, to form a solution and with said resolving agent being capable of binding with at least one but not all of said enantiomers to form a precipitate, containing said at least one of said enantiomers in stereospecific form and collecting either the precipitate and purifying it or collecting the solution with contained other of said enantiomers and recrystallizing the enantiomer contained in said solution.