WO2009008009A4 - Novel crystalline form b of carvedilol dihydrogen phosphate - Google Patents

Novel crystalline form b of carvedilol dihydrogen phosphate Download PDF

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Publication number
WO2009008009A4
WO2009008009A4 PCT/IN2008/000441 IN2008000441W WO2009008009A4 WO 2009008009 A4 WO2009008009 A4 WO 2009008009A4 IN 2008000441 W IN2008000441 W IN 2008000441W WO 2009008009 A4 WO2009008009 A4 WO 2009008009A4
Authority
WO
WIPO (PCT)
Prior art keywords
process according
crystalline form
dihydrogen phosphate
carvedilol dihydrogen
range
Prior art date
Application number
PCT/IN2008/000441
Other languages
French (fr)
Other versions
WO2009008009A1 (en
Inventor
Rajesh Kumar Thaper
Manoj Devilalji Prabhavat
A V Mounishwarachar
Yogesh Dadaji Pawar
Pritesh R Upadhay
Original Assignee
Lupin Ltd
Rajesh Kumar Thaper
Manoj Devilalji Prabhavat
A V Mounishwarachar
Yogesh Dadaji Pawar
Pritesh R Upadhay
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Lupin Ltd, Rajesh Kumar Thaper, Manoj Devilalji Prabhavat, A V Mounishwarachar, Yogesh Dadaji Pawar, Pritesh R Upadhay filed Critical Lupin Ltd
Publication of WO2009008009A1 publication Critical patent/WO2009008009A1/en
Publication of WO2009008009A4 publication Critical patent/WO2009008009A4/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56Ring systems containing three or more rings
    • C07D209/80[b, c]- or [b, d]-condensed
    • C07D209/82Carbazoles; Hydrogenated carbazoles
    • C07D209/88Carbazoles; Hydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

Abstract

A novel crystalline form B of carvedilol dihydrogen phosphate having X-ray diffraction pattern as shown in figure 1. A process for the preparation of crystalline form B of carvedilol dihydrogen phosphate according to claim 1 that comprises dissolving carvedilol base in aprotic polar solvent, addition of phosphoric acid, heating the solution, adding water to hot solution, cooling, and isolation of solid.

Claims

AMENDED CLAIMS received by the International Bureau on 19 December 2008 (19.12.08).
1, A process for the preparation of crystalline form B of oarvedilol dihydrogen phosphate having X~ray diffraction pattern as shown in figure 1, said process comprises of:
(i) dissolving carvedilol base in aprotic polar solvent, (ii) addition of phosphoric acid, (iii) heating the solution, (iv) adding water to hot solution,
(v) cooling, and (vi) isolation of solid.
2, A process according to claim 1 wherein the aprotie solvent is selected from formamide, N,N-dimethyl formamide, N-mcthylpyrrolidine and mixtures thereof, preferably N5N-dimethy1 formamide.
3, A process according to claim 1 wherein heating is carried out at temperature in the range of 40-100 0C, preferably at 50-70 0C and most preferably at 55-60 0C.
4, A process according to claim 1 wherein water is added at temperature in the range of 40-100 °C, preferably at 50-70 0C and most preferably at 55-60 0C.
5. A process according to claim 1 wherein cooling is carried out at temperature in the range of -5 to 3O0C, preferably to 0-100C.
6. A process according to claim 1 wherein the solid is isolated by filtration.
PCT/IN2008/000441 2007-07-11 2008-07-09 Novel crystalline form b of carvedilol dihydrogen phosphate WO2009008009A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN980/KOL/2007 2007-07-11
IN980KO2007 2007-07-11

Publications (2)

Publication Number Publication Date
WO2009008009A1 WO2009008009A1 (en) 2009-01-15
WO2009008009A4 true WO2009008009A4 (en) 2009-03-05

Family

ID=39827949

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2008/000441 WO2009008009A1 (en) 2007-07-11 2008-07-09 Novel crystalline form b of carvedilol dihydrogen phosphate

Country Status (1)

Country Link
WO (1) WO2009008009A1 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106892858A (en) * 2015-12-21 2017-06-27 上海科胜药物研发有限公司 A kind of carvidilol dihydric phosphate novel crystal forms

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004002419A2 (en) * 2002-06-27 2004-01-08 Sb Pharmco Puerto Rico Inc. Carvedilol phosphate salts and/or solvates thereof, correspondinq compositions, and/or methods of treatment
EP1991527A2 (en) * 2006-06-28 2008-11-19 Teva Pharmaceutical Industries Ltd Polymorphous forms of carvedilol phosphate

Also Published As

Publication number Publication date
WO2009008009A1 (en) 2009-01-15

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