[go: up one dir, main page]

WO2009017813A1 - Saccharinate d'o-desméthyl-venlafaxine - Google Patents

Saccharinate d'o-desméthyl-venlafaxine Download PDF

Info

Publication number
WO2009017813A1
WO2009017813A1 PCT/US2008/009296 US2008009296W WO2009017813A1 WO 2009017813 A1 WO2009017813 A1 WO 2009017813A1 US 2008009296 W US2008009296 W US 2008009296W WO 2009017813 A1 WO2009017813 A1 WO 2009017813A1
Authority
WO
WIPO (PCT)
Prior art keywords
saccharinate
desmethyl venlafaxine
venlafaxine
desmethyl
odv
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2008/009296
Other languages
English (en)
Inventor
Uri Zadok
Eli Lancry
Sigal Blau
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Teva Pharmaceutical Industries Ltd
Teva Pharmaceuticals USA Inc
Original Assignee
Teva Pharmaceutical Industries Ltd
Teva Pharmaceuticals USA Inc
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 Teva Pharmaceutical Industries Ltd, Teva Pharmaceuticals USA Inc filed Critical Teva Pharmaceutical Industries Ltd
Publication of WO2009017813A1 publication Critical patent/WO2009017813A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/04—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/46—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C215/64—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Definitions

  • a solution of succinic acid in water is prepared in a water bath. More preferably, the water bath is at a temperature of about 40°C-80°C.
  • Flavoring agents and flavor enhancers make the dosage form more palatable to the patient.
  • Common flavoring agents and flavor enhancers for pharmaceutical products that may be included in the composition of the present invention include maltol, vanillin, ethyl vanillin, menthol, citric acid, fumaric acid, ethyl maltol, and tartaric acid.
  • Solid and liquid compositions may also be dyed using any pharmaceutically acceptable colorant to improve their appearance and/or facilitate patient identification of the product and unit dosage level.
  • Step 1 Succcinic acid (650.3 mg) was added to water (70 ml) and mixed in a water bath at 50°C. After a clear solution was obtained, ODV base (1449.9 mg) was added and mixed for 15 min, and the solution was filtered through a 0.2 ⁇ filter.

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne le sel de saccharine d'O-desméthyl-venlafaxine et l'un de ses polymorphes cristallins. L'invention a également pour objet des procédés de préparation du sel de saccharine, des formulations pharmaceutiques contenant ce sel et leurs procédés d'utilisation.
PCT/US2008/009296 2007-08-02 2008-08-01 Saccharinate d'o-desméthyl-venlafaxine Ceased WO2009017813A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US96324407P 2007-08-02 2007-08-02
US60/963,244 2007-08-02

Publications (1)

Publication Number Publication Date
WO2009017813A1 true WO2009017813A1 (fr) 2009-02-05

Family

ID=39930560

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2008/009296 Ceased WO2009017813A1 (fr) 2007-08-02 2008-08-01 Saccharinate d'o-desméthyl-venlafaxine

Country Status (1)

Country Link
WO (1) WO2009017813A1 (fr)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012140577A1 (fr) 2011-04-12 2012-10-18 Lupin Limited Compositions pharmaceutiques à libération modifiée de desvenlafaxine
WO2015011244A1 (fr) * 2013-07-25 2015-01-29 Almirall, S.A. Sels de dérivés 2-amino-1-hydroxyéthyl-8-hydroxyquinolin-2(1h)-one ayant à la fois l'activité d'un antagoniste du recepteur muscarinique et l'activite d'un agoniste du recepteur β2 adrenergique
US9233108B2 (en) 2011-11-11 2016-01-12 Almirall, S.A. Cyclohexylamine derivatives having β2 adrenergic agonist and M3 muscarinic antagonist activities
US9315463B2 (en) 2010-05-13 2016-04-19 Almirall, S.A. Cyclohexylamine derivatives having β2 adrenergic agonist and M3 muscarinic antagonist activities
US9518050B2 (en) 2012-12-18 2016-12-13 Almirall, S.A. Cyclohexyl and quinuclidinyl carbamate derivatives having β2 adrenergic agonist and M3 muscarinic antagonist activity
US9562039B2 (en) 2013-02-27 2017-02-07 Almirall, S.A. Salts of 2-amino-1-hydroxyethyl-8-hydroxyquinolin-2(1H)-one derivatives having both β2 adrenergic receptor agonist and M3 muscarinic receptor antagonist activities
US9643961B2 (en) 2010-05-13 2017-05-09 Almirall, S.A. Cyclohexylamine derivatives having β2 adrenergic antagonist and M3 muscarinic antagonist activities
US10005771B2 (en) 2014-09-26 2018-06-26 Almirall, S.A. Bicyclic derivatives having β2 adrenergic agonist and M3 muscarinic antagonist activities
US10456390B2 (en) 2013-07-25 2019-10-29 Almirall, S.A. Combinations comprising MABA compounds and corticosteroids

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2173787A (en) * 1982-12-13 1986-10-22 American Home Prod Derivatives of cycloalkanols and cycloalkenols
US4845098A (en) * 1986-11-22 1989-07-04 Bayer Aktiengesellschaft Saccharine salts of substituted hydroxypropylamines, compositions and use
US20030045583A1 (en) * 2001-02-12 2003-03-06 American Home Products Corporation Novel succinate salt of O-desmethyl-venlafaxine
US20060047125A1 (en) * 2004-08-24 2006-03-02 Recordati Ireland Limited Lercanidipine salts
WO2007005961A2 (fr) * 2005-07-06 2007-01-11 Sepracor Inc. Combinaisons d'un eszopiclone et d'un o-desmethylvenlafaxine, et methodes de traitement de la menopause et de l'humeur, de l'anxiete et des troubles cognitifs

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2173787A (en) * 1982-12-13 1986-10-22 American Home Prod Derivatives of cycloalkanols and cycloalkenols
US4845098A (en) * 1986-11-22 1989-07-04 Bayer Aktiengesellschaft Saccharine salts of substituted hydroxypropylamines, compositions and use
US20030045583A1 (en) * 2001-02-12 2003-03-06 American Home Products Corporation Novel succinate salt of O-desmethyl-venlafaxine
US20060047125A1 (en) * 2004-08-24 2006-03-02 Recordati Ireland Limited Lercanidipine salts
WO2007005961A2 (fr) * 2005-07-06 2007-01-11 Sepracor Inc. Combinaisons d'un eszopiclone et d'un o-desmethylvenlafaxine, et methodes de traitement de la menopause et de l'humeur, de l'anxiete et des troubles cognitifs

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
E. J. BARAN: "The saccharinate anion: a versatile and fascinating ligand in coordination chemistry", QUIMICA NOVA, vol. 28, no. 2, 2005, BRSOCIEDADE BRASILEIRA DE QUIMICA, SAO PAULO,, pages 326 - 328, XP002503521 *

Cited By (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9643961B2 (en) 2010-05-13 2017-05-09 Almirall, S.A. Cyclohexylamine derivatives having β2 adrenergic antagonist and M3 muscarinic antagonist activities
US9315463B2 (en) 2010-05-13 2016-04-19 Almirall, S.A. Cyclohexylamine derivatives having β2 adrenergic agonist and M3 muscarinic antagonist activities
WO2012140577A1 (fr) 2011-04-12 2012-10-18 Lupin Limited Compositions pharmaceutiques à libération modifiée de desvenlafaxine
US10300072B2 (en) 2011-11-11 2019-05-28 Almirall, S.A. Cyclohexylamine derivatives having β2 adrenergic agonist and M3 muscarinic antagonist activities
US9233108B2 (en) 2011-11-11 2016-01-12 Almirall, S.A. Cyclohexylamine derivatives having β2 adrenergic agonist and M3 muscarinic antagonist activities
US9757383B2 (en) 2011-11-11 2017-09-12 Almirall, S.A. Cyclohexylamine derivatives having β2 adrenergic agonist and M3 muscarinic antagonist activities
US9549934B2 (en) 2011-11-11 2017-01-24 Almirall, S.A. Cyclohexylamine derivatives having β2 adrenergic agonist and M3 muscarinic antagonist activities
US9518050B2 (en) 2012-12-18 2016-12-13 Almirall, S.A. Cyclohexyl and quinuclidinyl carbamate derivatives having β2 adrenergic agonist and M3 muscarinic antagonist activity
US9562039B2 (en) 2013-02-27 2017-02-07 Almirall, S.A. Salts of 2-amino-1-hydroxyethyl-8-hydroxyquinolin-2(1H)-one derivatives having both β2 adrenergic receptor agonist and M3 muscarinic receptor antagonist activities
US9579316B2 (en) 2013-07-25 2017-02-28 Almirall, S.A. Salts of 2-amino-1-hydroxyethyl-8-hydroxyquinolin-2(1H)-one derivatives having both muscarinic receptor antagonist and β2 adrenergic receptor agonist activities
CN105492027A (zh) * 2013-07-25 2016-04-13 阿尔米雷尔有限公司 具有毒蕈碱受体拮抗体和β2肾上腺素能受体激动剂两种活性的2-氨基-1-羟乙基-8-羟基喹啉-2(1H)-酮衍生物的盐
AU2014295028B2 (en) * 2013-07-25 2018-05-31 Almirall, S.A. Salts of 2-amino-1-hydroxyethyl-8-hydroxyquinolin-2(1H)-one derivatives having both muscarinic receptor antagonist and beta2 adrenergic receptor agonist activities
TWI641373B (zh) * 2013-07-25 2018-11-21 阿爾米雷爾有限公司 具有蕈毒鹼受體拮抗劑和β２腎上腺素受體促效劑二者之活性的２－胺基－１－羥乙基－８－羥基喹啉－２（１Ｈ）－酮衍生物之鹽
WO2015011244A1 (fr) * 2013-07-25 2015-01-29 Almirall, S.A. Sels de dérivés 2-amino-1-hydroxyéthyl-8-hydroxyquinolin-2(1h)-one ayant à la fois l'activité d'un antagoniste du recepteur muscarinique et l'activite d'un agoniste du recepteur β2 adrenergique
US10456390B2 (en) 2013-07-25 2019-10-29 Almirall, S.A. Combinations comprising MABA compounds and corticosteroids
EA035436B1 (ru) * 2013-07-25 2020-06-15 Альмираль, С.А. Кристаллическая соль присоединения транс-4-[{3-[5-({[(2r)-2-гидрокси-2-(8-гидрокси-2-оксо-1,2-дигидрохинолин-5-ил)этил]амино}метил)-1н-1,2,3-бензотриазол-1-ил]пропил}(метил)амино]циклогексилгидрокси(ди-2-тиенил)ацетатсахаринат, обладающая антагонистической активностью по отношению к мускариновому рецептору и агонистической активностью по отношению к 2 адренергическому рецептору
CN112321579A (zh) * 2013-07-25 2021-02-05 阿尔米雷尔有限公司 2-氨基-1-羟乙基-8-羟基喹啉-2(1h)-酮衍生物的盐
US10005771B2 (en) 2014-09-26 2018-06-26 Almirall, S.A. Bicyclic derivatives having β2 adrenergic agonist and M3 muscarinic antagonist activities

Similar Documents

Publication Publication Date Title
WO2009017813A1 (fr) Saccharinate d'o-desméthyl-venlafaxine
US7674935B2 (en) Crystal forms of O-desmethylvenlafaxine
US8207361B2 (en) Tigecycline crystalline forms and processes for preparation thereof
US6710184B2 (en) Crystalline solids of carvedilol and processes for their preparation
US20120122915A1 (en) Crystalline forms of palonosetron hydrochloride
AU2008247169A1 (en) Polymorphic forms of bosentan
US20070185211A1 (en) Crystal forms of cinacalcet HCI and processes for their preparation
US20040235904A1 (en) Crystalline and amorphous solids of pantoprazole and processes for their preparation
EP1866275A1 (fr) Formes cristallines de pregabaline
US20090012182A1 (en) Crystal forms of O-desmethylvenlafaxine succinate
EP4508035A1 (fr) Formes à l'état solide de mavacamten et leur procédé de préparation
JP2023506025A (ja) レンボレキサントの固体形態
US20080027128A1 (en) Duloxetine HCL polymorphs
WO2025141465A1 (fr) Formes à l'état solide de chlorhydrate de zipalertinib et leur procédé de préparation
WO2008105794A1 (fr) Procédé de purification du carvédilol ou de ses sels
MX2008000137A (en) Tigeycline crystalline forms and processes for preparation thereof

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 08780351

Country of ref document: EP

Kind code of ref document: A1

NENP Non-entry into the national phase

Ref country code: DE

122 Ep: pct application non-entry in european phase

Ref document number: 08780351

Country of ref document: EP

Kind code of ref document: A1