CY1105774T1 - Μεθοδος παρασκευης ξανθινικων αναστολεων φωσφοδιεστepασης v και προδρομων αυτων - Google Patents
Μεθοδος παρασκευης ξανθινικων αναστολεων φωσφοδιεστepασης v και προδρομων αυτωνInfo
- Publication number
- CY1105774T1 CY1105774T1 CY20061101635T CY061101635T CY1105774T1 CY 1105774 T1 CY1105774 T1 CY 1105774T1 CY 20061101635 T CY20061101635 T CY 20061101635T CY 061101635 T CY061101635 T CY 061101635T CY 1105774 T1 CY1105774 T1 CY 1105774T1
- Authority
- CY
- Cyprus
- Prior art keywords
- inhibitors
- phosphodidespase
- xanthine
- precursors
- preparation
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 5
- LRFVTYWOQMYALW-UHFFFAOYSA-N 9H-xanthine Chemical compound O=C1NC(=O)NC2=C1NC=N2 LRFVTYWOQMYALW-UHFFFAOYSA-N 0.000 title abstract 4
- 229940075420 xanthine Drugs 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 239000002243 precursor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 230000015572 biosynthetic process Effects 0.000 abstract 2
- 238000003786 synthesis reaction Methods 0.000 abstract 2
- 238000005859 coupling reaction Methods 0.000 abstract 1
- 238000005695 dehalogenation reaction Methods 0.000 abstract 1
- 239000002590 phosphodiesterase V inhibitor Substances 0.000 abstract 1
- 238000000746 purification Methods 0.000 abstract 1
- 238000000926 separation method Methods 0.000 abstract 1
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
Abstract
Μέθοδος παρασκευής ξανθινικών αναστολέων φωσφοδιεστεράσης V, και ενώσεων που χρησιμοποιούνται σε αυτή τη μέθοδο. Η μέθοδος περιλαμβάνει μια μεθοδολογία 5 βαθμίδων για την αποτελεσματική σύνθεση της ένωσης (5) χωρίς ενδιάμεσους καθαρισμούς ή διαχωρισμούς, μια βαθμίδα διαλογόνωσης για τη σύνθεση της ένωσης (7) και μια αντίδραση σύζευξης για την παραγωγή της ένωσης (9).
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US38447802P | 2002-05-31 | 2002-05-31 | |
PCT/US2003/017042 WO2003101992A1 (en) | 2002-05-31 | 2003-05-30 | Process for preparing xanthine phosphodiesterase v inhibitors and precursors thereof |
Publications (1)
Publication Number | Publication Date |
---|---|
CY1105774T1 true CY1105774T1 (el) | 2011-02-02 |
Family
ID=29712039
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CY20061101635T CY1105774T1 (el) | 2002-05-31 | 2006-11-13 | Μεθοδος παρασκευης ξανθινικων αναστολεων φωσφοδιεστepασης v και προδρομων αυτων |
Country Status (17)
Country | Link |
---|---|
US (2) | US7074923B2 (el) |
EP (1) | EP1509525B9 (el) |
JP (1) | JP2005529934A (el) |
CN (2) | CN100497336C (el) |
AR (1) | AR040232A1 (el) |
AT (1) | ATE336494T1 (el) |
AU (1) | AU2003238822A1 (el) |
CA (1) | CA2483923A1 (el) |
CY (1) | CY1105774T1 (el) |
DE (1) | DE60307628T2 (el) |
DK (1) | DK1509525T5 (el) |
ES (1) | ES2270047T3 (el) |
HK (1) | HK1068139A1 (el) |
MX (1) | MXPA04011862A (el) |
PT (1) | PT1509525E (el) |
WO (1) | WO2003101992A1 (el) |
ZA (1) | ZA200408719B (el) |
Families Citing this family (47)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
CA2533715A1 (en) | 2003-07-31 | 2005-02-10 | Schering Corporation | Metabolite of xanthine phosphodiesterase 5 inhibitor and derivatives thereof useful for treatment of erectile dysfunction |
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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CA2030112A1 (en) * | 1989-11-24 | 1991-05-25 | Yasuo Ito | Xanthine compound, method for preparing thereof, and a pharmaceutical composition comprising the same |
IL98559A0 (en) * | 1990-06-21 | 1992-07-15 | Schering Corp | Polycyclic guanine derivatives |
JPH04128285A (ja) * | 1990-06-27 | 1992-04-28 | Hokuriku Seiyaku Co Ltd | キサンチン誘導体 |
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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 |
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HUP0301622A3 (en) * | 2000-07-04 | 2006-05-29 | Novo Nordisk As | Purine derivatives inhibiting the enzyme dipeptidyl petidase iv (dpp-iv) and pharmaceutical compositions containing them |
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 |
US6869947B2 (en) * | 2001-07-03 | 2005-03-22 | Novo Nordisk A/S | Heterocyclic compounds that are inhibitors of the enzyme DPP-IV |
EP1421084B1 (en) | 2001-08-28 | 2008-05-14 | Schering Corporation | Polycyclic guanine phosphodiesterase v inhibitors |
EP1463727A2 (en) * | 2001-09-19 | 2004-10-06 | Novo Nordisk A/S | Heterocyclic compounds that are inhibitors of the enzyme dpp-iv |
EP1442042A1 (en) | 2001-11-09 | 2004-08-04 | Schering Corporation | Polycyclic guanine derivative phosphodiesterase v inhibitors |
ATE409466T1 (de) * | 2002-01-11 | 2008-10-15 | Novo Nordisk As | Verfahren und zusammensetzung zur behandlung von diabetes, hypertonie, chronischer herzinsuffizienz und mit flüssigkeitsretention einhergehenden zuständen |
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 |
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 |
KR101150449B1 (ko) * | 2002-08-21 | 2012-06-01 | 베링거 잉겔하임 파르마 게엠베하 운트 코 카게 | 8-[3-아미노-피페리딘-1-일]-크산틴, 이의 제조방법 및 이를 포함하는 약제학적 조성물 |
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 |
CA2533715A1 (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 |
-
2003
- 2003-05-30 CA CA002483923A patent/CA2483923A1/en not_active Abandoned
- 2003-05-30 MX MXPA04011862A patent/MXPA04011862A/es active IP Right Grant
- 2003-05-30 WO PCT/US2003/017042 patent/WO2003101992A1/en active IP Right Grant
- 2003-05-30 CN CNB038124971A patent/CN100497336C/zh not_active Expired - Fee Related
- 2003-05-30 DE DE60307628T patent/DE60307628T2/de not_active Expired - Lifetime
- 2003-05-30 AR ARP030101921A patent/AR040232A1/es unknown
- 2003-05-30 PT PT03734281T patent/PT1509525E/pt unknown
- 2003-05-30 AU AU2003238822A patent/AU2003238822A1/en not_active Abandoned
- 2003-05-30 EP EP03734281A patent/EP1509525B9/en not_active Expired - Lifetime
- 2003-05-30 AT AT03734281T patent/ATE336494T1/de not_active IP Right Cessation
- 2003-05-30 DK DK03734281T patent/DK1509525T5/da active
- 2003-05-30 ES ES03734281T patent/ES2270047T3/es not_active Expired - Lifetime
- 2003-05-30 CN CNA2009101321189A patent/CN101538224A/zh active Pending
- 2003-05-30 US US10/449,526 patent/US7074923B2/en not_active Expired - Fee Related
- 2003-05-30 JP JP2004509683A patent/JP2005529934A/ja active Pending
-
2004
- 2004-10-27 ZA ZA200408719A patent/ZA200408719B/en unknown
-
2005
- 2005-03-03 HK HK05101860A patent/HK1068139A1/xx not_active IP Right Cessation
-
2006
- 2006-05-08 US US11/429,719 patent/US7786301B2/en not_active Expired - Fee Related
- 2006-11-13 CY CY20061101635T patent/CY1105774T1/el unknown
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 |
WO2003101992A1 (en) | 2003-12-11 |
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 |
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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