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Application pharmaceuticals

Please find here a few examples of our nitriles mainly used as intermediates for pharmaceuticals for human and veterinary use:

Human medicine application:

NITRALZ® CAS No. application area examples end product examples

4-Aminobenzonitrile

873-74-5

anti-migrane

anti-atherosclerotic

anticoagulant

treatment of HIV

anti-cancer

anti-asthmatic

Dabigatran

Frovatriptan

Goxalapladib

Rilpivirine

2-Brombenzonitrile

2042-37-7

anti-hypertensive

anti-epileptic

Irbesartan

Perampanel

4-Brombenzonitrile

623-00-7

analgesic
ocular anti-inflammatory

Bromfenac

2-Chlorbenzonitrile

873-32-5

anti-hypertensive

analgesic

hypnotic

anesthetic

Sartanes

 

 

Ketamine  Hydrochloride

4-Chlorbenzonitrile

623-03-0

anti-allergic

aromatase inhibitor

Lodoxamide Tromethamine

2,3-Dichlorbenzonitrile

6574-97-6 anti-epileptic Lamotrigine

2,4-Dichlorbenzonitrile

6574-98-7

treatment of HIV

Dolutegravir

Pivalonitrile

630-18-2

bronchodilator Pirbuterol

4-Tolunitrile

104-85-8

anti-histaminic

hemostatic

anti-ulcerative

anti-neoplastic

Letrozole
3-Acetylpyridine 350-03-8 anti-leukemia drug Imatinib

 

Veterinary medicine application:

NITRALZ® CAS No. application area examples end product examples

Benzonitrile

100-47-0

antibacterial Florfenicol, Robenacoxib

n-Butyronitrile

109-74-0

anticoccidial

Amprolium

4-Chlorbenzonitrile

623-03-0

contraceptive

Lotrifen

3-Acetylpyridine

350-03-8

tyrosine-kinase inhibitor treatment of mast cell tumors

Masitinib

 

Special solvents:

NITRALZ® CAS No.

n-Butyronitrile

109-74-0

Pivalonitrile

630-18-2

4-Heptanone

123-19-3

Did you know that …

Over 30 nitrile-containing pharmaceuticals are prescribed for a diverse variety of medicinal indications with more than 20 additional nitrile-containing leads in clinical development.
The nitrile group is quite robust and, in most cases, is not readily metabolized but passes through the body unchanged. The types of pharmaceuticals containing nitriles are diverse, from vildagliptin, an antidiabetic drug, to anastrozole, which is the gold standard in treating breast cancer. In many instances the nitrile mimics functionality present in substrates for enzymes, whereas in other cases the nitrile increases water solubility or decreases susceptibility to oxidative metabolism in the liver. The nitrile functional group is found in several drugs. (Fleming et al. 2010: 7902)

 

Fleming, Fraser F.; Lao, Lihua; Ravikumar, P.C; Funk, Lee and Shook, Brian C. (2010): Nitrile-Containing Pharmaceuticals. Efficacious Roles of the Nitrile Pharmacophor, in: Journal of Medicinal Chemistry. 53 (22), pp 7902-7917.

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