Sanofi Aventis

A series of dioxane carbamate inhibitors has recently been disclosed by Sanofi-Aventis. No biological data are provided for specific compounds, although most compounds are described as having IC50 values for FAAH inhibition ranging from 0.005-1 Compound (59) is one of over 25 compounds specifically claimed [74]. 

Sanofi-Aventis has disclosed a series of piperidine- and piperazine-alkyl carbamates as cannabinoid and/or FAAH modulators. No compounds are specifically claimed in the patent. Compound (60) is reported to have an IC50 value of 85 and is active in a mouse pain model [75]. 

In recent years pre-clinical testing and, in particular, clinical data on SR141716A (Rimonabant, Acomplia) (382) from Sanofi-Aventis (previously... 

Several groups have published on structural analogues of (382), one of the earliest being the disclosure of CP 272871 (383) from Pfizer, which displays lower affinity for the CBi receptor than (382), in addition to reduced selectivity over the CB2 receptor subtype. Both (382) and (383) have been shown to act as inverse agonists rather than neutral antagonists in vitro [265]. A recently published patent application from Sanofi-Aventis claims a series of 4-cyanopyrazole analogues of (382), with 42 specific examples [266]. 

Six-membered heterocycles have also been extensively used to mimic the central pyrazole scaffold of limonabant (382). Merck and Co. has utilised pyiidines (510) [314], and pyrimidines (511) [315] in this capacity. Sanofi-Aventis has also claimed a series of pyridine-based analogues [316], as exemplified by (512) and additionally the non-heteroatom containing terphenyl (513) [317]. 

The search for an effective non-peptide oxytocin antagonist has become a major goal of a number of pharmaceutical companies because of the poor pharmacokinetic properties and especially the lack of oral bioavailability associated with peptidic antagonists. Early research in this field was dominated by Merck, but in recent years significant research efforts at GlaxoSmithKline and Serono have been published. A number of other companies, notably Sanofi-Aventis, Yamanouchi and Wyeth, have had a major presence in vasopressin receptor research and oxytocin is frequently included in patent claims for the molecules. Occasionally, oxytocin-selective compounds have been reported, usually derived by adaptation of the vasopressin antagonist template. 

From Taxotere (docetaxel) product information. Bridgewater, NJ Sanofi-aventis, November 2007. 

Earlier examples of pilot- and bench-scale processes are summarized in [14]. Several cases with high ee-values and medium activity using Rh-bpm ligands were reported by Hoechst (now Sanofi Aventis) [46] Ru-binap and Ru-biphep... 

Zolpidem MR Sanofi-Aventis Launched-Phase IV studies... 

Sanofi-Aventis Deutschland Industriepark Hochst G878 65926 Frankfurt Germany... 

Thomas.Klabunde sanofi-aventis.com Cover Illustration... 

Agut et al. (2011) assessed the different technology transfer options and reported that within Sanofi-Aventis that option 1 (comparative testing) is the approach of choice for critical methodologies, i.e. assay, degradation products, and in some cases water content and dissolution. Option 2 (co-validation) is reserved for less-critical methodologies, i.e. residual solvents by gas chromatography (GC), water content, dissolution and particle size methods whereas, option 4 (transfer waiver) is restricted to pharmacopoeial compendial methods, i.e. appearance, pH, particulate matter, etc. 

Ombrabulin Oncology Tubulin binding Phase 111 Sanofi-Aventis 644, 645,... 

Paclitaxel (96) Diterpene taxoid Cabazitaxel Oncology Tubulin binding Phase III Sanofi-Aventis 658-662... 

Larotaxel Oncology Tubulin binding Phase in Sanofi-Aventis 658, 659,... 

Rohitukine (112) Flavone Alvocidib (flavopiridol, HMR 1275) (113) Oncology Cyclin-dependent kinase inhibition Phase III (NSCLC) Phase Ilb (CLL) Sanofi-Aventis 700-702... 

Semi-synthetic Macrolide NXL-103 Antibacterial (CAP Inhibits bacterial Phase II Sanofi-Aventis 778-783... 

Telithromycin Antibacterial Inhibits bacterial Phase ll/in Sanofi-Aventis 802... 

Sanofi Aventis Further information available at http //www.ketek.com/ (accessed on 14.12.2010). 

Recent examples of successful peptide-ligand based discoveries of drug-like peptidomimetics include the discovery of SST antagonists, or the discovery of non-peptidic antagonists of the recently deorphanized urotensin II receptor at Sanofi-Aventis. ° As illustrated in Fig. 3, Flohr etal. used 3D models of the NMR solution structure of cyclic peptide derivatives of Urotensin II as a template for virtual 3D pharmacophore searches which resulted into non-peptidic candidates for lead optimization. 

Ramipril (5, HOE-498), discovered at Hoechst (now Sanofi-Aventis), was launched in the United States as Altace in 1991 and is currently marketed by King Pharmaceuticals. Upon administration, rapid hepatic cleavage of the ethyl ester results in ramiprilat (42), the... 

USAN Zolpidem tartrate Trade name Ambien Sanofi-Aventis Launched 1999 M.W. 307.39... 

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