WO2003101992A1 - Process for preparing xanthine phosphodiesterase v inhibitors and precursors thereof - Google Patents

Process for preparing xanthine phosphodiesterase v inhibitors and precursors thereof Download PDF

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Publication number
WO2003101992A1
WO2003101992A1 PCT/US2003/017042 US0317042W WO03101992A1 WO 2003101992 A1 WO2003101992 A1 WO 2003101992A1 US 0317042 W US0317042 W US 0317042W WO 03101992 A1 WO03101992 A1 WO 03101992A1
Authority
WO
WIPO (PCT)
Prior art keywords
compound
alkyl
group
reacting
cycloalkyl
Prior art date
Application number
PCT/US2003/017042
Other languages
English (en)
French (fr)
Inventor
Vilas H. Dahanukar
Hoa N. Nguyen
Cecilia A. Orr
Fucheng Zhang
Ilia A. Zavialov
Original Assignee
Schering Corporation
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 Schering Corporation filed Critical Schering Corporation
Priority to DK03734281T priority Critical patent/DK1509525T5/da
Priority to AU2003238822A priority patent/AU2003238822A1/en
Priority to DE60307628T priority patent/DE60307628T2/de
Priority to MXPA04011862A priority patent/MXPA04011862A/es
Priority to JP2004509683A priority patent/JP2005529934A/ja
Priority to CA002483923A priority patent/CA2483923A1/en
Priority to EP03734281A priority patent/EP1509525B9/en
Priority to SI200330476T priority patent/SI1509525T1/sl
Publication of WO2003101992A1 publication Critical patent/WO2003101992A1/en
Priority to HK05101860A priority patent/HK1068139A1/xx
Priority to CY20061101635T priority patent/CY1105774T1/el

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/12—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to hydrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
PCT/US2003/017042 2002-05-31 2003-05-30 Process for preparing xanthine phosphodiesterase v inhibitors and precursors thereof WO2003101992A1 (en)

Priority Applications (10)

Application Number Priority Date Filing Date Title
DK03734281T DK1509525T5 (da) 2002-05-31 2003-05-30 Fremgangsmåde til fremstilling af xanthin-phosphodiesterase V-inhibitorer og præcursorer derfor
AU2003238822A AU2003238822A1 (en) 2002-05-31 2003-05-30 Process for preparing xanthine phosphodiesterase v inhibitors and precursors thereof
DE60307628T DE60307628T2 (de) 2002-05-31 2003-05-30 Verfahren zur herstellung von xanthin phosphodiesterase v inhibitoren und deren vorstufen
MXPA04011862A MXPA04011862A (es) 2002-05-31 2003-05-30 Procedimiento para preparar inhibidores xantina de la fosfodiesterasa v, y precursores de los mismos.
JP2004509683A JP2005529934A (ja) 2002-05-31 2003-05-30 キサンチンホスホジエステラーゼｖインヒビターおよびその前駆物質を調製するプロセス
CA002483923A CA2483923A1 (en) 2002-05-31 2003-05-30 Process for preparing xanthine phosphodiesterase v inhibitors and precursors thereof
EP03734281A EP1509525B9 (en) 2002-05-31 2003-05-30 Process for preparing xanthine phosphodiesterase v inhibitors and precursors thereof
SI200330476T SI1509525T1 (sl) 2002-05-31 2003-05-30 Postopek priprave inhibitorjev ksantinske fosfodiesteraze V in njihovih prekurzorjev
HK05101860A HK1068139A1 (en) 2002-05-31 2005-03-03 Process for preparing xanthine phosphodiesterase vinhibitors and precursors thereof
CY20061101635T CY1105774T1 (el) 2002-05-31 2006-11-13 Μεθοδος παρασκευης ξανθινικων αναστολεων φωσφοδιεστepασης v και προδρομων αυτων

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US38447802P 2002-05-31 2002-05-31
US60/384,478 2002-05-31

Publications (1)

Publication Number Publication Date
WO2003101992A1 true WO2003101992A1 (en) 2003-12-11

Family

ID=29712039

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/017042 WO2003101992A1 (en) 2002-05-31 2003-05-30 Process for preparing xanthine phosphodiesterase v inhibitors and precursors thereof

Country Status (17)

Country Link
US (2) US7074923B2 (US07786301-20100831-C00010.png)
EP (1) EP1509525B9 (US07786301-20100831-C00010.png)
JP (1) JP2005529934A (US07786301-20100831-C00010.png)
CN (2) CN100497336C (US07786301-20100831-C00010.png)
AR (1) AR040232A1 (US07786301-20100831-C00010.png)
AT (1) ATE336494T1 (US07786301-20100831-C00010.png)
AU (1) AU2003238822A1 (US07786301-20100831-C00010.png)
CA (1) CA2483923A1 (US07786301-20100831-C00010.png)
CY (1) CY1105774T1 (US07786301-20100831-C00010.png)
DE (1) DE60307628T2 (US07786301-20100831-C00010.png)
DK (1) DK1509525T5 (US07786301-20100831-C00010.png)
ES (1) ES2270047T3 (US07786301-20100831-C00010.png)
HK (1) HK1068139A1 (US07786301-20100831-C00010.png)
MX (1) MXPA04011862A (US07786301-20100831-C00010.png)
PT (1) PT1509525E (US07786301-20100831-C00010.png)
WO (1) WO2003101992A1 (US07786301-20100831-C00010.png)
ZA (1) ZA200408719B (US07786301-20100831-C00010.png)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005012303A1 (en) * 2003-07-31 2005-02-10 Schering Corporation Metabolite of xanthine phosphodiesterase 5 inhibitor and derivatives thereof useful for treatment of erectile dysfunction

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US6821978B2 (en) * 2000-09-19 2004-11-23 Schering Corporation Xanthine phosphodiesterase V inhibitors
NZ528216A (en) * 2001-02-24 2006-12-22 Boehringer Ingelheim Pharma Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
TW200404802A (en) * 2002-05-31 2004-04-01 Schering Corp Xanthine phosphodiesterase V inhibitor polymorphs
WO2004009091A1 (en) * 2002-06-17 2004-01-29 Glaxo Group Limited Purine derivatives as liver x receptor agonists
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
US7495005B2 (en) * 2002-08-22 2009-02-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, their preparation and their use in pharmaceutical compositions
US7569574B2 (en) 2002-08-22 2009-08-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Purine derivatives, the preparation thereof and their use as pharmaceutical compositions
US7482337B2 (en) 2002-11-08 2009-01-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
DE10254304A1 (de) * 2002-11-21 2004-06-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
US7566707B2 (en) * 2003-06-18 2009-07-28 Boehringer Ingelheim International Gmbh Imidazopyridazinone and imidazopyridone derivatives, the preparation thereof and their use as pharmaceutical compositions
AR047948A1 (es) * 2003-11-21 2006-03-15 Schering Corp Formulaciuones de inhibidores de la fosfodiesterasa v
DE10355304A1 (de) 2003-11-27 2005-06-23 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 8-(Piperazin-1-yl)-und 8-([1,4]Diazepan-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
US7501426B2 (en) * 2004-02-18 2009-03-10 Boehringer Ingelheim International Gmbh 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
DE102004009039A1 (de) * 2004-02-23 2005-09-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-[3-Amino-piperidin-1-yl]-xanthine, deren Herstellung und Verwendung als Arzneimittel
US7393847B2 (en) 2004-03-13 2008-07-01 Boehringer Ingleheim International Gmbh Imidazopyridazinediones, their preparation and their use as pharmaceutical compositions
US7179809B2 (en) * 2004-04-10 2007-02-20 Boehringer Ingelheim International Gmbh 2-Amino-imidazo[4,5-d]pyridazin-4-ones, their preparation and their use as pharmaceutical compositions
US7439370B2 (en) * 2004-05-10 2008-10-21 Boehringer Ingelheim International Gmbh Imidazole derivatives, their preparation and their use as intermediates for the preparation of pharmaceutical compositions and pesticides
DE102004030502A1 (de) * 2004-06-24 2006-01-12 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Imidazole und Triazole, deren Herstellung und Verwendung als Arzneimittel
DE102004043944A1 (de) * 2004-09-11 2006-03-30 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 8-(3-Amino-piperidin-1-yl)-7-(but-2-inyl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
DE102004044221A1 (de) * 2004-09-14 2006-03-16 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 3-Methyl-7-butinyl-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
DE102004054054A1 (de) * 2004-11-05 2006-05-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine
DE102005035891A1 (de) * 2005-07-30 2007-02-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
EA030606B1 (ru) 2006-05-04 2018-08-31 Бёрингер Ингельхайм Интернациональ Гмбх Способы приготовления лекарственного средства, содержащего полиморфы
PE20080251A1 (es) 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
EP2057160A1 (en) 2006-08-08 2009-05-13 Boehringer Ingelheim International GmbH Pyrrolo [3, 2 -d]pyrimidines as dpp-iv inhibitors for the treatment of diabetes mellitus
KR101610005B1 (ko) * 2007-08-17 2016-04-08 베링거 인겔하임 인터내셔날 게엠베하 Ｆａｂ 관련 질환의 치료에 사용하기 위한 푸린 유도체
PE20140960A1 (es) 2008-04-03 2014-08-15 Boehringer Ingelheim Int Formulaciones que comprenden un inhibidor de dpp4
PE20100156A1 (es) * 2008-06-03 2010-02-23 Boehringer Ingelheim Int Tratamiento de nafld
BRPI0916997A2 (pt) 2008-08-06 2020-12-15 Boehringer Ingelheim International Gmbh Inibidor de dpp-4 e seu uso
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
EA031225B1 (ru) * 2008-08-15 2018-12-28 Бёрингер Ингельхайм Интернациональ Гмбх Ингибиторы дпп-4 для заживления ран
EP2344195A2 (en) 2008-09-10 2011-07-20 Boehringer Ingelheim International GmbH Combination therapy for the treatment of diabetes and related conditions
US20200155558A1 (en) 2018-11-20 2020-05-21 Boehringer Ingelheim International Gmbh Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug
BRPI0923121A2 (pt) 2008-12-23 2015-08-11 Boehringer Ingelheim Int Formas salinas de compostos orgânico
TW201036975A (en) 2009-01-07 2010-10-16 Boehringer Ingelheim Int Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy
ES2760917T3 (es) 2009-11-27 2020-05-18 Boehringer Ingelheim Int Tratamiento de pacientes diabéticos genotipificados con inhibidores DPP-IV como la linagliptina
JP6034781B2 (ja) 2010-05-05 2016-11-30 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 併用療法
EA201991014A1 (ru) 2010-06-24 2019-09-30 Бёрингер Ингельхайм Интернациональ Гмбх Лечение диабета
US9034883B2 (en) 2010-11-15 2015-05-19 Boehringer Ingelheim International Gmbh Vasoprotective and cardioprotective antidiabetic therapy
MX366629B (es) 2011-07-15 2019-07-17 Boehringer Ingelheim Int Quinazolinas sustituidas, su preparación y su uso en composiciones farmacéuticas.
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
EP3685839A1 (en) 2012-05-14 2020-07-29 Boehringer Ingelheim International GmbH Linagliptin for use in the treatment of albuminuria and kidney related diseases
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
US9526728B2 (en) 2014-02-28 2016-12-27 Boehringer Ingelheim International Gmbh Medical use of a DPP-4 inhibitor
JP2019517542A (ja) 2016-06-10 2019-06-24 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング リナグリプチンおよびメトホルミンの組合せ

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005012303A1 (en) * 2003-07-31 2005-02-10 Schering Corporation Metabolite of xanthine phosphodiesterase 5 inhibitor and derivatives thereof useful for treatment of erectile dysfunction
US7312223B2 (en) 2003-07-31 2007-12-25 Schering Corporation Metabolite of xanthine Phosphodiesterase 5 inhibitor and derivatives thereof useful for treatment of erectile dysfunction

Also Published As

Publication number Publication date
US7074923B2 (en) 2006-07-11
CN100497336C (zh) 2009-06-10
CN1668618A (zh) 2005-09-14
DE60307628D1 (de) 2006-09-28
US20030232987A1 (en) 2003-12-18
CN101538224A (zh) 2009-09-23
EP1509525B1 (en) 2006-08-16
DK1509525T5 (da) 2007-07-30
AR040232A1 (es) 2005-03-23
EP1509525B9 (en) 2007-10-31
PT1509525E (pt) 2006-12-29
HK1068139A1 (en) 2005-04-22
JP2005529934A (ja) 2005-10-06
MXPA04011862A (es) 2005-03-31
ZA200408719B (en) 2005-11-15
CY1105774T1 (el) 2011-02-02
CA2483923A1 (en) 2003-12-11
EP1509525A1 (en) 2005-03-02
ES2270047T3 (es) 2007-04-01
DK1509525T3 (da) 2006-12-11
DE60307628T2 (de) 2007-08-09
US20060205943A1 (en) 2006-09-14
ATE336494T1 (de) 2006-09-15
US7786301B2 (en) 2010-08-31
AU2003238822A1 (en) 2003-12-19

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