Boehringer Ingelheim

Fine chemical companies are generally either small and privately held or divisions of larger companies, such as Eastman Fine Chemicals (United States) and Lonza (Switzerland). Examples of large public fife science companies, which market fine chemicals as a subsidiary activity to their production for captive use, are Hoffmann-La Roche, Sandoz, and Boehringer Ingelheim, which produce and market bulk vitamins and liquid crystal intermediates, dyestuff intermediates, and bulk active ingredients, respectively. Table 3 fists some representative companies having an important fine chemical business. 

Total sales of prescription bronchodHators and antiasthma products in 1989 were approximately 1.2 and 3.3 bHHon in the North American and world markets, respectively (166). The three largest shares of the world market were held by Glaxo Holdings pic, Schering-Plough Corporation, and Boehringer Ingelheim Corporation. 

Hauptmann, K.H., Weber, K.-H., Zeile, K., Danneberg, P. and Giesemann, R. South African Patent 68/0803 February 7, 1968 assigned to Boehringer Ingelheim GmbH, Germany... 

Muller, E. and Hasspacher, K. U.S. Patent 3,275,625 September 27,1966 assigned to Boehringer Ingelheim GmbH,Germany... 

Heike Zimdahl Boehringer Ingelheim Pharma GmbH Co KG Biberach Germany... 

After the discovery of weak inhibition by the N-terminal products of substrate peptides, researchers at Boehringer Ingelheim reported potent and specific hexapeptides providing up to a 10 -fold increase in potency (Figure 2.3) [89]. 

Another series of non-covalent competitive inhibitors reaching toward the F side has been reported by Boehringer Ingelheim researchers. Bailey, et al. [116]... 

Following these announcements, the first wave of publications addressing the use of SMB for the manufacture of pharmaceutical products of interest was published. The separation of a chiral hetrazepine [26], WEB 2170 6-(2-chlorophenyl)-8-9-di-hydro-l-methyl-8-[(morpholinyl)-carbonyl]-4H,7H-cyclopenta[4,5]-thieno[3,2-f][l,2,4]triazolo[4,3-a][l,4]diazepine. WEB 2170 is a chiral hetrazepine from Boehringer-Ingelheim. The enantioseparation of WEB 2170 was performed using cellulose triacetate (CTA) from Merck (Darmstadt) as the CSP and with pure methanol as eluent. 

Biolnvent Production AB Boehringer Ingelheim DSM Biologies Genentech IDEC... 

J. Conners, Boehringer Ingelheim Pharmaceuticals, Inc., personal communication, 1991. 

Tenecteplase (also marketed as Metalyse) (TNK-tPA, modified rtPA) Boehringer Ingelheim... 

Oxamic acid 26 and AT-hydroxyoxamic acid 27 derivatives were disclosed by the Boehringer Ingelheim group as moderately active Lck SH2 domain antagonists [119,130]. 

A structurally rather dissimilar pTyr mimic was developed by the Boehringer Ingelheim group, namely a triazole-dicarboxylic acid derivative 31 [130], which was shown to yield highly active Lck SH2 domain antagonists. 

The Boehringer Ingelheim group chose a pyridone-based core structure to replace the -Glu-Glu-Ile- tripeptide of the generic SH2 domain recognition sequence [130]. From a series of more than 200 analogues, pyridones with mutually different decoration patterns were identified to result in pTyr derivatives with submicromolar affinities (e.g., 55,56) for the Lck SH2 domain [130]. 

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