XenoPort begins phase II trial of XP-23829 in patients with psoriasis

New Drug Approvals

XP 23829  from Xenoport is an interesting molecule and as on 27 July 2014, I did not find conclusive evidence

See some structures below

Not sure about the structure of XP 23829

OR

Figure US08148414-20120403-C00019Best fit

OR

Figure US08148414-20120403-C00027Not sure?

(N,N-dimethylcarbamoyl)methyl methyl(2E)but-2-ene-1,4-dioate.

OR

Figure imgf000032_0002

I AM NOT SURE ABOUT THIS ONE ALSO????????

As Football worldcup2014 goes on in Brazil

A thought for it is due…………

……………………………………………………

Best fit is probably is as shown below, and there are reasons

(N,N- Diethylcarbamoyl)methyl methyl (2E)but-2-ene-l,4-dioate 

Introduction

(N,​N-​Diethylcarbamoyl)​methyl methyl (2E)​-​but-​2-​ene-​1,​4-​dioate

Figure imgf000024_0002

C11 H17 N O5, mw 243.13

M.p.: 53-56 °C.

1 H NMR (CDCI3, 400 MHz): δ 6.99-6.90 (m, 2H), 4.83 (s, 2H), 3.80 (s, 3H), 3.39 (q, J = 1.1 Hz, 2H), 3.26 (q, J = 7.2 Hz, 2H), 1 .24 (t, J = 7.2 Hz, 3H), 1 .14 (t, J = 7.2 Hz, 3H). MS (ESI): m/z…

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Cocrystals

New Drug Approvals

Abstract Image

Active pharmaceutical ingredients (APIs) are frequently delivered to the patient in the solid state as part of such dosage forms as tablets, capsules, etc.In this context the ability to deliver the drug to the patient in a safe, efficacious and cost-effective way depends largely on the physicochemical properties of the APIs in the solid state, and ……..read more

http://www.allfordrugs.com/cocrystals/

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How to Handle Drug Polymorphs… Case Study of Trelagliptin Succinate

New Drug Approvals

Pharmaceutical API Polymorphs… case study of Trelagliptin
CASE STUDY WITH..Compound I having the formula
Figure imgf000073_0001
Links
WO2008067465A1 OR US8084605  IS THE PATENT USED AND WITH FORM “A” AND AMORPHOUS FORM
Active pharmaceutical ingredients (APIs), frequently delivered to the patient in the solid-state as part of an approved dosage form, can exist in such diverse solid forms as polymorphs, pseudopolymorphs, salts, co-crystals and amorphous solids. Various solid forms often display different mechanical, thermal, physical and chemical properties that can remarkably influence the bioavailability, hygroscopicity, stability and other performance characteristics of the drug.
Hence, a thorough understanding of the relationship between the particular solid form of an active pharmaceutical ingredient (API) and its functional properties is important in selecting the most suitable form of the API for development into a drug product. In past decades, there have been significant efforts on the discovery, selection and control…

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Idrabiotaparinux for anticoagulant therapy.

New Drug Approvals

Figure imgf000003_0002

Idrabiotaparinux

  •  抗血栓治療中の出血率を低下させるためのイドラビオタパリナックスの使用

(biotinylated idraparinux, SSR-126517, SSR-126517E)

405159-59-3              9 x Na salt
774531-07-6 (free acid)

Idrabiotaparinux has an attached biotin moiety at the non-reducing end unit, which allows its neutralisation with avidin, an egg-derived protein with low antigenicity. This compound is currently investigated in clinical trials for prevention of recurrent VTE in patients with acute pulmonary embolism. The future of idrabiotaparinux depends also on the safety and efficacy of avidin.
Symptomatic deep vein thrombosis (DVT) and/or pulmonary embolism (PE) – treatment and secondary prevention of recurrent venous thromboembolism (VTE).

SSR-126517, a biotinylated idraparinux, had been in phase III clinical trials at Sanofi (formerly known as sanofi-aventis) for the treatment of pulmonary embolism, deep venous thrombosis (DVT) and atrial fibrillation. However, in 2009, development of the compound was discontinued.


Idrabiotaparinux (biotinylated idraparinux, SSR-126517, SSR-126517E) is a long-acting selective pentasaccharide indirect factor Xa coagulation inhibitor, administered by…

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