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

DS 2330 by Daiichi Sankyo

phase 1

Apr 072016

DS 2330

4-[2-(4-{[2-({3-[(trans-4-carboxy-cyclohexyl)(ethyl)sulfocarbamoyl]benzoyl}amino)-5-(piperidin-1-yl)benzoyl]amino}phenyl)ethyl]benzoic acid,

4- [2- (4 – {[2 – ({3 – [(trans-4-carboxy-cyclohexyl) (ethyl) sulfur carbamoyl] benzoyl} amino) -5- (piperidin-1-yl) benzoyl] amino} phenyl) ethyl] benzoate

CAS 1634680-81-1

C₄₃ H₄₈ N₄ O₈ S, 780.9

Benzoic acid, 4-[2-[4-[[2-[[3-[[(trans-4-carboxycyclohexyl)ethylamino]sulfonyl]benzoyl]amino]-5-(1-piperidinyl)benzoyl]amino]phenyl]ethyl]-

CIS CAS 1634681-85-8

DISODIUM SALT 1634681-00-7

OriginatorDaiichi Sankyo Inc
ClassHyperphosphataemia therapies

useful for treating hyperphosphatemia, DS-2330, a phosphorous lowering agent, being developed by Daiichi Sankyo, for treating hyperphosphatemia in chronic kidney disease. In April 2016, DS-2330 was reported to be in phase 1 clinical development.

Phase IHyperphosphataemia

31 Oct 2015Phase-I clinical trials in Hyperphosphataemia in USA (unspecified route)

SEE WO2015108038,

PATENT

WO2014175317

http://www.google.com/patents/EP2990400A1?cl=en

PATENT

WO-2016047613

he problem is to provide a pharmaceutical for the prevention or treatment of hyperphosphatemia. The solution is a salt of a compound including formula (I), or a crystal of a hydrate thereof.

(Example 1)
disodium 4- [2- (4 – {[2 – ({3 – [(trans-4-carboxy-cyclohexyl) (ethyl) sulfur carbamoyl] benzoyl} amino) -5- (piperidin-1-yl ) benzoyl] amino} phenyl) ethyl] benzoic acid trihydrate
Disodium 4- [2- (4 – { [2 – ({3 – [(trans-4-carboxylatocyclohexyl) (ethyl) sulfamoyl] benzoyl} amino) – 5- (piperidin-1-yl) benzoyl] amino} phenyl) ethyl] benzoate trihydrate
of α crystal

[Formula 7] crystal of disodium salt trihydrate of (α crystal)

(1)
4- [2- (4 – {[2 – ({3 – [(trans-4-carboxy-cyclohexyl) (ethyl) sulfur carbamoyl] benzoyl} amino) -5- (piperidin-1-yl) benzoyl] amino} phenyl) ethyl] 1 mol / L NaOH aqueous solution to benzoic acid (1.2 g) (3.1 mL) was added and dissolved completely. After stirring at room temperature for 1 day was added acetonitrile (60 mL), at 40 ° C.
and stirred for further 1 day. The precipitated solid was collected by filtration, and 3 hours drying under reduced pressure at room temperature to give the title compound 1.1 g (85%).

(2)

　4- [2- (4 – {[2 – ({3 – [(trans-4-carboxy-cyclohexyl) (ethyl) sulfur carbamoyl] benzoyl} amino) -5- (piperidin-1-yl) benzoyl] amino} phenyl) ethyl] benzoate (40.0 g)
in water (46.4 mL), 1-PrOH (72 mL), 4 mol / L NaOH aqueous solution (25.54 mL) was added, then filtered after stirring insolubles at room temperature, water / 1-PrOH: was washed with (3 7, 80 mL). The filtrate was heated up to 40 ℃, 1-PrOH the (160 mL) was added, and further seed crystal (α crystals, 0.2g) was added. Then the temperature was raised to 50 ℃, 1-PrOH (96 ml) was added, and the mixture was stirred overnight.Thereafter, 1-PrOH (480 ml) was added and after overnight stirring, was collected by filtration the precipitated solid was cooled to room temperature.Thereafter, and vacuum dried overnight at 40 ° C., to give the title compound 39.4 g (96%).

REFERENCES

http://www.daiichisankyo.com/media_investors/investor_relations/ir_calendar/files/005280/Presentation%20Material.pdf

////////////DS 2330, DS-2330, DAIICHI SANKYO, phase 1

O=C(O)[C@@H]1CC[C@H](CC1)N(CC)S(=O)(=O)c2cccc(c2)C(=O)Nc5ccc(cc5C(=O)Nc4ccc(CCc3ccc(cc3)C(=O)O)cc4)N6CCCCC6

DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO …..FOR BLOG HOME CLICK HERE