December 16, 2014 – All About Drugs

All About Drugs

Tout sur les médicaments הכל על תרופות كل شيئ عن الأدوية Все о наркотиках 关于药品的一切 డ్రగ్స్ గురించి అన్ని 마약에 관한 모든 것 Όλα για τα Ναρκωτικά Complete Tracking of Drugs Across the World by Dr Anthony Melvin Crasto, Worldpeacepeaker, worlddrugtracker, PH.D (ICT), MUMBAI, INDIA, Worlddrugtracker, Helping millions, 9 million hits on google on all websites, 2.5 lakh connections on all networks, “ALL FOR DRUGS” CATERS TO EDUCATION GLOBALLY, No commercial exploits are done or advertisements added by me. This is a compilation for educational purposes only. P.S. : The views expressed are my personal and in no-way suggest the views of the professional body or the company that I represent

Lexipafant

CAS : 139133-26-9

N-Methyl-N-[[4-[(2-methyl-1H-imidazo[4,5-c]pyridin-1-yl)methyl]phenyl]sulfonyl]-L-leucine ethyl ester

N-methyl-N-[[a-(2-methyl-1H-imidazo[4,5-c]pyridin-1-yl)-p-tolyl]sulfonyl]-L-leucine ethyl ester

N-Methyl-N-[4-(2-methyl-1H-imidazo[4,5-c]pyridin-1-ylmethyl)phenylsulfonyl]-L-leucine ethyl ester

Manufacturers’ Codes: BB-882

DO6
GR-167089
ISV-611

UNII-H14917M9YW

Trademarks: Zacutex (Brit. Biotech)

MF: C23H30N4O4S

M Wt: 458.57

Percent Composition: C 60.24%, H 6.59%, N 12.22%, O 13.96%, S 6.99%

Properties: White crystalline solid from ethyl acetate, mp 105°. [a]D20 -6.7° (c = 2.0 in CDCl3).

Melting point: mp 105°

Optical Rotation: [a]D20 -6.7° (c = 2.0 in CDCl3)

Therap-Cat: Anti-inflammatory. (Nonsteroidal); Platelet Activating Factor Antagonist.

Lexipafant is a platelet-activating factor (PAF) antagonist that was in early clinical development at DevCo for the oral treatment of dementia and motor function disorders in HIV patients, intravenous treatment of acute pancreatitis, as well as for the prevention of certain serious renal and neurological complications experienced by patients undergoing cardiac surgery, including stroke. However, no recent developments of the drug candidate have been reported by the company.

Lexipafant was also being studied at British Biotech (now Vernalis) for the intravenous treatment of pancreatitis, but development for this indication was discontinued. In 2002, DevCo obtained from British Biotech exclusive rights to develop, manufacture and sell lexipafant for the treatment of human disease, excluding the fields of oncology and ophthalmology.

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http://www.google.com.ar/patents/EP0543858B1?cl=en

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WO 1993016075

http://www.google.com/patents/WO1993016075A1?cl=en

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WO 1995013064

http://www.google.com/patents/EP0727995A1?cl=en

Literature References:

Platelet activating factor (PAF) antagonist. Prepn: M. Whittaker, A. Miller, WO 9203422; eidem, US5200412 (1992, 1993 both to British Bio-Technology).

Structure-activity report: M. Whittaker et al., J. Lipid Mediators Cell Signalling 10, 151 (1994).

Pharmacology: F. M. Abu-Zidan et al., Pharmacol. Toxicol. 78, 23 (1996).

Clinical evaluation in acute pancreatitis: A. N. Kingsnorth et al., Br. J. Surg. 82, 1414 (1995).

ANTHONY MELVIN CRASTO

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Dithiocarbamates: Reagents for the Removal of Transition Metals from Organic Reaction Media

Chemical Development, Bristol-Myers Squibb Co., 1 Squibb Drive, New Brunswick, New Jersey 08903,United States

Org. Process Res. Dev., Article ASAP

DOI: 10.1021/op500336h

Dithiocarbamates (DTCs) are ligands known to chelate with Cu and other transition metals to form insoluble complexes. Wastewater treatment protocols have utilized DTCs to remove trace (ppb) metals from waste streams. We have extended the applicability of DTCs to a protocol that readily enables control of the residual Cu in isolated material in a quick and cost-effective manner. Formation of the chelate complex typically results in purging of Cu and a variety of other metals in an array of reaction media to ≤10 ppm. Furthermore, the simplicity of the method makes it very attractive for large-scale applications late in a synthetic sequence because of the low toxicity and efficient removal of the metal complex by filtration.