ES2009486A6 - Procedimiento para prepara la forma de hidrocloruro de 2-(4-(2-furoil)-(2-piperazin)-1-il)-4-amin-6,7-dimetoxiquinazolina - Google Patents

Procedimiento para prepara la forma de hidrocloruro de 2-(4-(2-furoil)-(2-piperazin)-1-il)-4-amin-6,7-dimetoxiquinazolina

Info

Publication number
ES2009486A6
ES2009486A6 ES8700500A ES8700500A ES2009486A6 ES 2009486 A6 ES2009486 A6 ES 2009486A6 ES 8700500 A ES8700500 A ES 8700500A ES 8700500 A ES8700500 A ES 8700500A ES 2009486 A6 ES2009486 A6 ES 2009486A6
Authority
ES
Spain
Prior art keywords
furoyl
piperazin
amino
preparation
crystalline anhydrous
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.)
Expired
Application number
ES8700500A
Other languages
English (en)
Inventor
Helmut Schickaneder
Ingomar Grafe
Kurt Henning Arhens
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.)
Heumann Pharma GmbH and Co
Original Assignee
Heumann Pharma GmbH and 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 Heumann Pharma GmbH and Co filed Critical Heumann Pharma GmbH and Co
Publication of ES2009486A6 publication Critical patent/ES2009486A6/es
Expired legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

PROCEDIMIENTO PARA PREPARAR LA FORMA DE HIDROCLORURO DE 2-4-(2-FUROIL) -(2-PIPERAZIN)-1-IL -4-AMIN-6,7-DIMETOXIQUINAZOLINA. EL PROCEDIMIENTO OBJETO DEL INVENTO SE CARACTERIZA PORQUE SE HACE REACCIONAR 2-4-(2-FUROIL)-(2-PIPERAZIN)-1-IL -4-AMINO-6,7-DIMETOXIQUINAZOLINA, ESCALONADAMENTE, EN UNA REACCION DE ACIDO-BASE, EN MEDIO ACUOSO Y A CONTINUACION SE SECA, LA FORMA SECADA, OBTENIDA, DE HIDRATO DE HIDROCLORURO DE 2-4-(2-FUROIL)-(2-PIPERAZIN)-1-IL -4-AMINO-6,7-DIMETOXIQUINAZOLINA SE HACE REACCIONAR EN EL SENO DE METANOL, Y LA RESULTANTE FORMA DE METANOLATO DE HIDROCLORURO DE 2-4-(2- FUROIL)-(2-PIPERAZIN)-1-IL -4-AMINO-6,7-DIMETOXIQUINAZOLINA SE SECA, CON ELIMINACION DE LA PORCION DE METANOL DE CRISTALIZACION. ESTA NUEVA FORMA SE DISTINGUE POR UNA SORPRENDENTE ESTABILIDAD EN ALMACENAMIENTO FRENTE A LAS FORMAS POLIMORFAS CONOCIDAS DEL PRAZOSIN.
ES8700500A 1986-03-21 1987-02-25 Procedimiento para prepara la forma de hidrocloruro de 2-(4-(2-furoil)-(2-piperazin)-1-il)-4-amin-6,7-dimetoxiquinazolina Expired ES2009486A6 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP86103925A EP0237608B1 (de) 1986-03-21 1986-03-21 Kristalline, wasserfreie Sigma -Form von 2-[4-(2-Furoyl-(2-piperazin)-1-yl]-4-amino-6,7-dimethoxychinazolinhydrochlorid und Verfahren zu ihrer Herstellung

Publications (1)

Publication Number Publication Date
ES2009486A6 true ES2009486A6 (es) 1989-10-01

Family

ID=8194990

Family Applications (1)

Application Number Title Priority Date Filing Date
ES8700500A Expired ES2009486A6 (es) 1986-03-21 1987-02-25 Procedimiento para prepara la forma de hidrocloruro de 2-(4-(2-furoil)-(2-piperazin)-1-il)-4-amin-6,7-dimetoxiquinazolina

Country Status (19)

Country Link
US (1) US4816455B1 (es)
EP (1) EP0237608B1 (es)
JP (1) JPH0662615B2 (es)
KR (1) KR870008875A (es)
AR (1) AR242384A1 (es)
AT (1) ATE72244T1 (es)
AU (1) AU586318B2 (es)
CA (1) CA1240999A (es)
DE (1) DE3683760D1 (es)
DK (1) DK173283B1 (es)
ES (1) ES2009486A6 (es)
GR (1) GR870429B (es)
HU (1) HU200176B (es)
ID (1) ID810B (es)
IE (1) IE59913B1 (es)
IL (1) IL81841A (es)
NZ (1) NZ219644A (es)
PT (1) PT84496B (es)
ZA (1) ZA87966B (es)

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US5587377A (en) * 1995-10-24 1996-12-24 Invamed, Inc. Terazosin crystalline polymorph and pharmaceutical compositions thereof
DE59611417D1 (de) * 1996-12-20 2007-03-29 Heumann Pharma Gmbh & Co Neue polymorphe Form von Doxazosinmesylat (Form III)
EP0849265A1 (de) * 1996-12-20 1998-06-24 HEUMANN PHARMA GmbH Neue polymorphe Form von Doxazosin-Mesylat (Form II)
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CA2566652C (en) 1998-06-19 2008-10-21 Teijin Limited Polymorphic modifications of 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazole-carboxylic acid and processes for the preparation thereof
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
CL2004001034A1 (es) 2003-05-14 2005-03-28 Teijin Pharma Ltd Formas cristalinas de acido 4-(1-((,etilbenzotiofen-3-il)me til)benzimidazol-2-iltio)butanoico; procedimiento de preparacion de las formas cristalinas; composicion farmaceutica; y su uso para el tratamiento de enfermedades inflamatorias, alergicas, r
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
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
JPWO2006052026A1 (ja) * 2004-11-12 2008-05-29 帝人ファーマ株式会社 ベンズイミダゾール誘導体の酸性塩及びその結晶
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
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
PE20080251A1 (es) 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
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
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
BRPI0916997A2 (pt) 2008-08-06 2020-12-15 Boehringer Ingelheim International Gmbh Inibidor de dpp-4 e seu uso
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
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
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
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

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US3511836A (en) 1967-12-13 1970-05-12 Pfizer & Co C 2,4,6,7-tetra substituted quinazolines
US4026894A (en) * 1975-10-14 1977-05-31 Abbott Laboratories Antihypertensive agents
US4092315A (en) * 1976-03-01 1978-05-30 Pfizer Inc. Novel crystalline forms of prazosin hydrochloride
GB1591490A (en) * 1977-08-04 1981-06-24 Abbott Lab 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine hydrochloride dihydrate
DE3375395D1 (en) * 1983-11-22 1988-02-25 Heumann Ludwig & Co Gmbh Process for the preparation of 4-amino-6,7-dimethoxy-2-(4-(furoyl-2)-piperazin-1-yl)-quinazoline and its physiologically acceptable salt
FI79107C (fi) * 1984-06-25 1989-11-10 Orion Yhtymae Oy Foerfarande foer framstaellning av stabil -form av prazosinhydroklorid.

Also Published As

Publication number Publication date
US4816455A (en) 1989-03-28
IL81841A (en) 1991-06-10
ZA87966B (en) 1987-08-04
DK139887D0 (da) 1987-03-18
DK173283B1 (da) 2000-06-13
DK139887A (da) 1987-09-22
EP0237608B1 (de) 1992-01-29
ID810B (id) 1996-07-15
PT84496A (de) 1987-04-01
DE3683760D1 (de) 1992-03-12
IE870705L (en) 1987-09-21
HUT47101A (en) 1989-01-30
AR242384A1 (es) 1993-03-31
AU6870787A (en) 1987-09-24
IL81841A0 (en) 1987-10-20
HU200176B (en) 1990-04-28
NZ219644A (en) 1989-04-26
US4816455B1 (en) 1992-11-24
EP0237608A1 (de) 1987-09-23
JPS62226980A (ja) 1987-10-05
GR870429B (en) 1987-07-13
KR870008875A (ko) 1987-10-21
IE59913B1 (en) 1994-04-20
CA1240999A (en) 1988-08-23
AU586318B2 (en) 1989-07-06
JPH0662615B2 (ja) 1994-08-17
PT84496B (pt) 1989-11-10
ATE72244T1 (de) 1992-02-15

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Effective date: 20110301