BRPI0516187A - processo para preparação de [3, 4-c]pirid-2-onas de 4, 5-diidro-pirazolo - Google Patents

processo para preparação de [3, 4-c]pirid-2-onas de 4, 5-diidro-pirazolo

Info

Publication number
BRPI0516187A
BRPI0516187A BRPI0516187-8A BRPI0516187A BRPI0516187A BR PI0516187 A BRPI0516187 A BR PI0516187A BR PI0516187 A BRPI0516187 A BR PI0516187A BR PI0516187 A BRPI0516187 A BR PI0516187A
Authority
BR
Brazil
Prior art keywords
dihydro
ones
preparing
pyrid
pyrazolo
Prior art date
Application number
BRPI0516187-8A
Other languages
English (en)
Inventor
Rafael Shapiro
Lucius T Rossano
Boguslaw M Mudryk
Nicolas Cuniere
Matthew Oberholzer
Huiping Zhang
Bang-Chi Chen
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of BRPI0516187A publication Critical patent/BRPI0516187A/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/80Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D211/84Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen directly attached to ring carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

PROCESSO PARA PREPARAçãO DE ¢3,4 c!PIRID-2-ONAS DE 4,5-DIIDRO-PIRAZOLO. Um novo processo e intermediários deste para preparação de 4,5-diidro-pirazolo¢3,4-c!pirid-2-onas do tipo mostrado abaixo a partir de hidrazinas de fenila apropriada é descrito. Estes compostos podem ser úteis como inibidores de fator Xa.
BRPI0516187-8A 2004-09-28 2005-09-27 processo para preparação de [3, 4-c]pirid-2-onas de 4, 5-diidro-pirazolo BRPI0516187A (pt)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US61393804P 2004-09-28 2004-09-28
US68899905P 2005-06-09 2005-06-09
US11/235,510 US7396932B2 (en) 2004-09-28 2005-09-26 Process for preparing 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones
PCT/US2005/034548 WO2007001385A2 (en) 2004-09-28 2005-09-27 Process for preparing 4,5-dihydro-pyrazolo [3,4-c] pyrid-2-ones

Publications (1)

Publication Number Publication Date
BRPI0516187A true BRPI0516187A (pt) 2008-08-26

Family

ID=36100191

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0516187-8A BRPI0516187A (pt) 2004-09-28 2005-09-27 processo para preparação de [3, 4-c]pirid-2-onas de 4, 5-diidro-pirazolo

Country Status (12)

Country Link
US (1) US7396932B2 (pt)
EP (1) EP1805178A2 (pt)
JP (1) JP2008514712A (pt)
KR (1) KR20070067177A (pt)
AR (1) AR051304A1 (pt)
AU (1) AU2005333566A1 (pt)
BR (1) BRPI0516187A (pt)
CA (1) CA2582233A1 (pt)
IL (1) IL182177A0 (pt)
MX (1) MX2007003702A (pt)
NO (1) NO20071702L (pt)
WO (1) WO2007001385A2 (pt)

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TWI320039B (en) * 2001-09-21 2010-02-01 Lactam-containing compounds and derivatives thereof as factor xa inhibitors
TW200303201A (en) * 2001-12-10 2003-09-01 Bristol Myers Squibb Co Synthesis of 4,5-dihydro-pyrazolo [3,4-c] pyrid-2-ones
US20070203178A1 (en) * 2004-09-28 2007-08-30 Malley Mary F Crystalline solvates of apixaban
US7304157B2 (en) * 2004-09-28 2007-12-04 Bristol-Myers Squibb Company Efficient synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones
US20060069085A1 (en) * 2004-09-28 2006-03-30 Rulin Zhao Preparation of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones
US20060069260A1 (en) * 2004-09-28 2006-03-30 Huiping Zhang Preparation of N-aryl pyridones
US20060160841A1 (en) * 2005-01-19 2006-07-20 Chenkou Wei Crystallization via high-shear transformation
SMT202000093T1 (it) 2009-06-16 2020-03-13 Pfizer Forme di dosaggio di apixaban
SI2538925T1 (sl) 2010-02-25 2016-04-29 Bristol-Myers Squibb Company Apiksaban formulacije
ITMI20111047A1 (it) * 2011-06-10 2012-12-11 Dipharma Francis Srl Forma cristallina di apixaban
ITMI20111135A1 (it) * 2011-06-22 2012-12-23 Dipharma Francis Srl Procedimento per la preparazione di apixaban
JP2014516072A (ja) 2011-06-10 2014-07-07 ディフアルマ フランチス ソシエタ ア レスポンサビリタ リミタータ アピキサバン製造方法
EP2554159A1 (en) 2011-08-04 2013-02-06 ratiopharm GmbH Dosage forms comprising apixaban and content uniformity enhancer
WO2013119328A1 (en) * 2012-02-07 2013-08-15 Assia Chemical Industries Ltd. Solid state forms of apixaban
US9045473B2 (en) * 2012-03-14 2015-06-02 Dr. Reddy's Laboratories Ltd. Forms of Apixaban
CA2873949A1 (en) 2012-05-24 2013-11-28 Ratiopharm Gmbh Dosage forms comprising apixaban and matrix former
WO2014072884A1 (en) 2012-11-12 2014-05-15 Alembic Pharmaceuticals Limited Process for the synthesis of apixaban
CZ304846B6 (cs) * 2012-11-13 2014-12-03 Zentiva, K.S. Způsob přípravy APIXABANU
EP2752414A1 (en) 2013-01-04 2014-07-09 Sandoz AG Crystalline form of apixaban
WO2014108919A2 (en) * 2013-01-09 2014-07-17 Msn Laboratories Limited NOVEL INTERMEDIATE AND POLYMORPHS OF 1-(4-METHOXYPHENYL)-7-OXO-6-[4-(2-OXOPIPERIDIN-1-YL)PHENYL]-4,5,6,7-TETRAHYDRO-1H-PYRAZOLO[3,4-c] PYRIDINE-3-CARBOXAMIDE AND PROCESS THEREOF
CZ2013305A3 (cs) 2013-04-23 2014-11-05 Zentiva, K.S. Nové krystalické formy APIXABANU a způsob jejich přípravy
WO2014203275A2 (en) 2013-06-18 2014-12-24 Cadila Healthcare Limited An improved process for the preparation of apixaban and intermediates thereof
CN103360391B (zh) * 2013-08-06 2015-03-25 齐鲁制药有限公司 阿哌沙班新晶型及其制备方法
CN104370902A (zh) * 2013-08-12 2015-02-25 药源药物化学(上海)有限公司 一种阿哌沙班新晶型及其制备方法
CN103923080B (zh) * 2014-04-04 2016-06-22 苏州景泓生物技术有限公司 一种制备抗血栓药物阿哌沙班的方法
WO2015177801A1 (en) * 2014-05-23 2015-11-26 Symed Labs Limited Novel process for the preparation of a lactam-containing compound
WO2016005560A1 (en) * 2014-07-11 2016-01-14 Laboratorios Lesvi, S.L. Process for prepararing apixaban
HU231122B1 (hu) 2014-08-06 2020-11-30 Egis Gyógyszergyár Zrt Eljárás apixaban előállítására
EP3189053B1 (en) 2014-09-05 2021-05-05 Unichem Laboratories Limited An improved process for the preparation of apixaban and intermediates thereof
EP3098221B1 (en) * 2014-10-15 2017-12-06 F.I.S.- Fabbrica Italiana Sintetici S.p.A. Process for preparing apixaban form n-1
US9932336B2 (en) 2014-10-28 2018-04-03 Jubilant Generics Limited Process for the preparation of apixaban and intermediates thereof
HU230991B1 (hu) 2014-11-19 2019-08-28 Egis Gyógyszergyár Zrt. Eljárás és köztitermék apixaban előállítására
US9603846B2 (en) 2014-11-25 2017-03-28 Cadila Healthcare Limited Process for the preparation of apixaban
CN104892601B (zh) * 2015-06-09 2017-09-19 江苏中邦制药有限公司 一种抗血栓药物阿哌沙班的制备方法
EP3064497A1 (en) 2015-07-20 2016-09-07 F.I.S.- Fabbrica Italiana Sintetici S.p.A. Dimer impurities of apixaban and method to remove them
WO2017088841A1 (en) 2015-11-26 2017-06-01 Zentiva, K.S. Preparation of a drug form containing amorphous apixaban
WO2017221209A1 (en) 2016-06-23 2017-12-28 Lupin Limited Pharmaceutical formulations of apixaban
KR102188341B1 (ko) 2018-10-24 2020-12-08 하나제약 주식회사 아픽사반의 제조방법
EP3666773A1 (en) 2018-12-11 2020-06-17 KRKA, D.D., Novo Mesto Process for preparing apixaban
AR122679A1 (es) 2020-06-23 2022-09-28 Guilherme Savoi Cocristales derivados de apixabán
JP2022022550A (ja) * 2020-06-26 2022-02-07 ダイト株式会社 アピキサバンの新規製造方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2078447T3 (es) * 1990-06-15 1995-12-16 Merck & Co Inc Un procedimiento de cristalizacion para mejorar la estructura y el tamaño de los cristales.
YU34501A (sh) * 2000-05-26 2003-10-31 Pfizer Products Inc. Postupak reaktivne kristalizacije radi povećanja veličine čestica
TWI320039B (en) 2001-09-21 2010-02-01 Lactam-containing compounds and derivatives thereof as factor xa inhibitors
CN104744461A (zh) 2001-09-21 2015-07-01 百时美施贵宝公司 含有内酰胺的化合物及其衍生物作为Xa因子的抑制剂
WO2003048081A2 (en) 2001-12-04 2003-06-12 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
TW200303201A (en) 2001-12-10 2003-09-01 Bristol Myers Squibb Co Synthesis of 4,5-dihydro-pyrazolo [3,4-c] pyrid-2-ones
WO2006045756A1 (en) 2004-10-25 2006-05-04 Boehringer Ingelheim International Gmbh Use of dipyridamole in combination with antithrombotics for treatment and prevention of thromboembolic diseases
US20060160841A1 (en) 2005-01-19 2006-07-20 Chenkou Wei Crystallization via high-shear transformation

Also Published As

Publication number Publication date
EP1805178A2 (en) 2007-07-11
US7396932B2 (en) 2008-07-08
AU2005333566A1 (en) 2007-01-04
NO20071702L (no) 2007-05-25
WO2007001385B1 (en) 2007-07-12
MX2007003702A (es) 2007-04-20
CA2582233A1 (en) 2007-01-04
JP2008514712A (ja) 2008-05-08
WO2007001385A3 (en) 2007-05-31
KR20070067177A (ko) 2007-06-27
US20060069258A1 (en) 2006-03-30
IL182177A0 (en) 2007-07-24
AR051304A1 (es) 2007-01-03
WO2007001385A2 (en) 2007-01-04

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Legal Events

Date Code Title Description
B11A Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing
B11Y Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette]