CN101538224A - 制备黄嘌呤磷酸二酯酶v抑制剂及其前体的方法 - Google Patents

制备黄嘌呤磷酸二酯酶v抑制剂及其前体的方法 Download PDF

Info

Publication number
CN101538224A
CN101538224A CNA2009101321189A CN200910132118A CN101538224A CN 101538224 A CN101538224 A CN 101538224A CN A2009101321189 A CNA2009101321189 A CN A2009101321189A CN 200910132118 A CN200910132118 A CN 200910132118A CN 101538224 A CN101538224 A CN 101538224A
Authority
CN
China
Prior art keywords
compound
alkyl
group
reaction
cycloalkyl
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.)
Pending
Application number
CNA2009101321189A
Other languages
English (en)
Chinese (zh)
Inventor
V·H·达哈努卡
H·N·阮
C·A·奥尔
F·张
I·A·扎维亚洛夫
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.)
Merck Sharp and Dohme LLC
Original Assignee
Schering Corp
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 Corp filed Critical Schering Corp
Publication of CN101538224A publication Critical patent/CN101538224A/zh
Pending legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00Compounds 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
    • C07C257/10Compounds 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
    • C07C257/12Compounds 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic 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
    • C07D233/66Heterocyclic 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
    • C07D233/90Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
CNA2009101321189A 2002-05-31 2003-05-30 制备黄嘌呤磷酸二酯酶v抑制剂及其前体的方法 Pending CN101538224A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US38447802P 2002-05-31 2002-05-31
US60/384478 2002-05-31

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CNB038124971A Division CN100497336C (zh) 2002-05-31 2003-05-30 制备黄嘌呤磷酸二酯酶v抑制剂及其前体的方法

Publications (1)

Publication Number Publication Date
CN101538224A true CN101538224A (zh) 2009-09-23

Family

ID=29712039

Family Applications (2)

Application Number Title Priority Date Filing Date
CNA2009101321189A Pending CN101538224A (zh) 2002-05-31 2003-05-30 制备黄嘌呤磷酸二酯酶v抑制剂及其前体的方法
CNB038124971A Expired - Fee Related CN100497336C (zh) 2002-05-31 2003-05-30 制备黄嘌呤磷酸二酯酶v抑制剂及其前体的方法

Family Applications After (1)

Application Number Title Priority Date Filing Date
CNB038124971A Expired - Fee Related CN100497336C (zh) 2002-05-31 2003-05-30 制备黄嘌呤磷酸二酯酶v抑制剂及其前体的方法

Country Status (16)

Country Link
US (2) US7074923B2 (https=)
EP (1) EP1509525B9 (https=)
JP (1) JP2005529934A (https=)
CN (2) CN101538224A (https=)
AR (1) AR040232A1 (https=)
AT (1) ATE336494T1 (https=)
AU (1) AU2003238822A1 (https=)
CA (1) CA2483923A1 (https=)
CY (1) CY1105774T1 (https=)
DE (1) DE60307628T2 (https=)
DK (1) DK1509525T5 (https=)
ES (1) ES2270047T3 (https=)
MX (1) MXPA04011862A (https=)
PT (1) PT1509525E (https=)
WO (1) WO2003101992A1 (https=)
ZA (1) ZA200408719B (https=)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6821978B2 (en) * 2000-09-19 2004-11-23 Schering Corporation Xanthine phosphodiesterase V inhibitors
EP1368349B1 (de) * 2001-02-24 2007-02-14 Boehringer Ingelheim Pharma GmbH & Co.KG Xanthinderivate, deren herstellung und deren verwendung als arzneimittel
JP2005529933A (ja) * 2002-05-31 2005-10-06 シェーリング コーポレイション キサンチンホスホジエステラーゼvインヒビター多形体
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
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
KR20060101762A (ko) * 2003-11-21 2006-09-26 쉐링 코포레이션 포스포디에스테라제 v 억제제 제형
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
EP2540725A1 (de) 2006-05-04 2013-01-02 Boehringer Ingelheim International GmbH Polymorphe von 1-((4-Methyl-chinazolin-2-yl)methyl)-3-methyl-7-(2-butin-1-yl)-8-(3-(R)-amino-piperidin-1-yl)xanthin
PE20080251A1 (es) 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
EP1852108A1 (en) * 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
JP2010500326A (ja) * 2006-08-08 2010-01-07 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 糖尿病の治療のためのdpp−iv阻害剤としてのピロロ[3,2−d]ピリミジン
WO2009024542A2 (en) * 2007-08-17 2009-02-26 Boehringer Ingelheim International Gmbh Purin derivatives for use in the treatment of fab-related diseases
PE20091730A1 (es) 2008-04-03 2009-12-10 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"
NZ604091A (en) * 2008-08-15 2014-08-29 Boehringer Ingelheim Int Purin derivatives for use in the treatment of fab-related diseases
CN102149407A (zh) 2008-09-10 2011-08-10 贝林格尔.英格海姆国际有限公司 治疗糖尿病和相关病症的组合疗法
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
CN102256976A (zh) 2008-12-23 2011-11-23 贝林格尔.英格海姆国际有限公司 有机化合物的盐形式
AR074990A1 (es) 2009-01-07 2011-03-02 Boehringer Ingelheim Int Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina
KR20240090632A (ko) 2009-11-27 2024-06-21 베링거 인겔하임 인터내셔날 게엠베하 리나글립틴과 같은 dpp-iv 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료
CN102946875A (zh) 2010-05-05 2013-02-27 贝林格尔.英格海姆国际有限公司 组合疗法
WO2011161161A1 (en) 2010-06-24 2011-12-29 Boehringer Ingelheim International Gmbh Diabetes therapy
AR083878A1 (es) 2010-11-15 2013-03-27 Boehringer Ingelheim Int Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento
US8883800B2 (en) 2011-07-15 2014-11-11 Boehringer Ingelheim International Gmbh Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
JP6224084B2 (ja) 2012-05-14 2017-11-01 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 糸球体上皮細胞関連障害及び/又はネフローゼ症候群の治療に用いるdpp−4阻害薬としてのキサンチン誘導体
JP6218811B2 (ja) 2012-05-14 2017-10-25 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 Sirs及び/又は敗血症の治療に用いるdpp−4阻害薬としてのキサンチン誘導体
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
EP3110449B1 (en) 2014-02-28 2023-06-28 Boehringer Ingelheim International GmbH Medical use of a dpp-4 inhibitor
CN109310697A (zh) 2016-06-10 2019-02-05 勃林格殷格翰国际有限公司 利格列汀和二甲双胍的组合

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6903224B2 (en) * 1988-04-11 2005-06-07 Biochem Pharma Inc. Substituted 1,3-oxathiolanes
US5064825A (en) * 1989-06-01 1991-11-12 Merck & Co., Inc. Angiotensin ii antagonists
JPH0372480A (ja) * 1989-08-10 1991-03-27 Hokuriku Seiyaku Co Ltd キサンチン誘導体及びそれらを有効成分とする気管支拡張剤
CA2030112A1 (en) * 1989-11-24 1991-05-25 Yasuo Ito Xanthine compound, method for preparing thereof, and a pharmaceutical composition comprising the same
NZ238609A (en) * 1990-06-21 1993-12-23 Schering Corp Polycyclic guanine derivatives; preparation, pharmaceutical compositions,
JPH04128285A (ja) * 1990-06-27 1992-04-28 Hokuriku Seiyaku Co Ltd キサンチン誘導体
JPH04279586A (ja) * 1991-03-05 1992-10-05 Hokuriku Seiyaku Co Ltd キサンチン誘導体
JPH051065A (ja) * 1991-06-20 1993-01-08 Hokuriku Seiyaku Co Ltd キサンチン誘導体
EP0538194B1 (de) * 1991-10-17 1997-06-04 Novartis AG Bicyclische Nukleoside, Oligonukleotide, Verfahren zu deren Herstellung und Zwischenprodukte
DE4411660A1 (de) * 1994-04-05 1995-10-12 Hoechst Ag Verwendung von Xanthinderivaten zur Reduktion der pathologischen Hyperreagibilität eosinophiler Granulozyten, neue Xanthinverbindungen und Verfahren zu deren Herstellung
DE19540798A1 (de) 1995-11-02 1997-05-07 Hoechst Ag Alkylxanthinphosphonate und Alkylxanthinphosphinoxide und deren Verwendung als Arzneimittel
ES2185837T3 (es) * 1996-06-07 2003-05-01 Hoechst Ag Utilizacion de derivados de teofilina para el tratamiento y la profilaxis de las enfermedades de choque, nuevos compuestos de xantina y procedimientos para su produccion.
AU2001268958B2 (en) * 2000-07-04 2006-03-09 Novo Nordisk A/S Heterocyclic compounds, which are inhibitors of the enzyme dpp-iv
US6821978B2 (en) * 2000-09-19 2004-11-23 Schering Corporation Xanthine phosphodiesterase V inhibitors
EP1368349B1 (de) * 2001-02-24 2007-02-14 Boehringer Ingelheim Pharma GmbH & Co.KG Xanthinderivate, deren herstellung und deren verwendung als arzneimittel
US6869947B2 (en) * 2001-07-03 2005-03-22 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme DPP-IV
ATE395349T1 (de) * 2001-08-28 2008-05-15 Schering Corp Polycyclische guanin phosphodiesterase inhibitoren
AU2002331311A1 (en) * 2001-09-19 2003-04-01 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme dpp-iv
CA2465893A1 (en) 2001-11-09 2003-05-22 Schering Corporation Polycyclic guanine derivative phosphodiesterase v inhibitors
AU2003201274A1 (en) * 2002-01-11 2003-07-24 Novo Nordisk A/S Compositions comprising inhibitors of dpp-iv and nep enzymes for the treatment of diabetes
JP2004043429A (ja) * 2002-02-25 2004-02-12 Eisai Co Ltd 新規キサンチン誘導体およびdppiv阻害剤
JP2005529933A (ja) * 2002-05-31 2005-10-06 シェーリング コーポレイション キサンチンホスホジエステラーゼvインヒビター多形体
WO2004009091A1 (en) * 2002-06-17 2004-01-29 Glaxo Group Limited Purine derivatives as liver x receptor agonists
ES2339112T3 (es) * 2002-08-21 2010-05-17 BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG 8-(3-amino-piperidin-1-il)-xantinas,su preparacion y su uso como medicamentos.
AU2003269850A1 (en) * 2002-10-08 2004-05-04 Novo Nordisk A/S Hemisuccinate salts of heterocyclic dpp-iv inhibitors
AU2003280680A1 (en) * 2002-11-01 2004-06-18 Sumitomo Pharmaceuticals Co., Ltd. Xanthine compound
US7247639B2 (en) * 2003-06-06 2007-07-24 Endacea, Inc. A1 adenosine receptor antagonists
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
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

Also Published As

Publication number Publication date
CA2483923A1 (en) 2003-12-11
CN100497336C (zh) 2009-06-10
AR040232A1 (es) 2005-03-23
MXPA04011862A (es) 2005-03-31
ES2270047T3 (es) 2007-04-01
PT1509525E (pt) 2006-12-29
ZA200408719B (en) 2005-11-15
EP1509525A1 (en) 2005-03-02
DE60307628D1 (de) 2006-09-28
US7786301B2 (en) 2010-08-31
WO2003101992A1 (en) 2003-12-11
EP1509525B9 (en) 2007-10-31
DK1509525T3 (da) 2006-12-11
US7074923B2 (en) 2006-07-11
HK1068139A1 (en) 2005-04-22
JP2005529934A (ja) 2005-10-06
AU2003238822A1 (en) 2003-12-19
DK1509525T5 (da) 2007-07-30
US20060205943A1 (en) 2006-09-14
EP1509525B1 (en) 2006-08-16
ATE336494T1 (de) 2006-09-15
DE60307628T2 (de) 2007-08-09
CN1668618A (zh) 2005-09-14
US20030232987A1 (en) 2003-12-18
CY1105774T1 (el) 2011-02-02

Similar Documents

Publication Publication Date Title
CN100497336C (zh) 制备黄嘌呤磷酸二酯酶v抑制剂及其前体的方法
CN110698461B (zh) 第三代egfr抑制剂的制备方法
KR20210127961A (ko) 방법 및 화합물
KR20130004393A (ko) 인테그라제 억제제의 제조를 위한 방법 및 중간체
CA2752045A1 (en) Process for the preparation of bosentan
EP2170840A1 (en) An improved process for preparing purine derivative
AU2005273430B2 (en) Methods for producing isoindole derivatives
EP0556720B1 (en) 5-Aminoflavone derivatives
AU2008313425B2 (en) Improved process for preparing 2-(substituted phenyl)-2-hydroxy-ethyl carbamates
WO2000024742A1 (en) Pyrazolopyridine as adenosine antagonists
JP7689076B2 (ja) 1,5-ベンゾチアゼピン化合物を製造するための方法
US20100298580A1 (en) Process for the Preparation of 2H-Chromene-3-Carbamate Derivatives
EP1719772A1 (en) Process for preparing xanthine phosphodiesterase v inhibitors and precursors thereof
KR102748251B1 (ko) 리나글립틴 및 이의 염의 제조를 위한 중간체 및 방법
HK1097547A (en) Process for preparing xanthine phosphodiesterase v inhibitors and precursors thereof
HK1068139B (en) Process for preparing xanthine phosphodiesterase v inhibitors and precursors thereof
EP0273321A1 (en) 7-Bromo-beta-carboline compound and method for producing same
JP2022529000A (ja) 置換2-[2-(フェニル)エチルアミノ]アルカンアミド誘導体の製造方法
FR2769912A1 (fr) Nouveaux derives de la 3-oxo- (2h)-1,2,4 triazine leur preparation et leur application en therapeutique humaine
CH670090A5 (https=)
EP2897937B1 (en) Process for the preparation of indacaterol and intermediates thereof
KR100377578B1 (ko) 온단세트론 및 그의 염의 제조방법
JPH0339072B2 (https=)

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Open date: 20090923