MD2335G2 - Hidrat cristalin de hidroclorură de 6-hidroxi-3-(4-[2-(piperidin-1-il)etoxi]fenoxi)-2-(4-metoxifenil)benzo[b]tiofen, procedeu de obţinere, compoziţie farmaceutică care îl conţine şi utilizarea pentru inhibarea stărilor patologice şi activarea colinacetiltransferazei - Google Patents

Hidrat cristalin de hidroclorură de 6-hidroxi-3-(4-[2-(piperidin-1-il)etoxi]fenoxi)-2-(4-metoxifenil)benzo[b]tiofen, procedeu de obţinere, compoziţie farmaceutică care îl conţine şi utilizarea pentru inhibarea stărilor patologice şi activarea colinacetiltransferazei Download PDF

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MD2335G2
MD2335G2 MDA20000161A MD20000161A MD2335G2 MD 2335 G2 MD2335 G2 MD 2335G2 MD A20000161 A MDA20000161 A MD A20000161A MD 20000161 A MD20000161 A MD 20000161A MD 2335 G2 MD2335 G2 MD 2335G2
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Moldova
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benzo
ethoxy
hydroxy
piperidine
phenoxy
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MDA20000161A
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Russian (ru)
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MD20000161A (ro
MD2335F2 (ro
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Джули Кей Буш
Престон Чарлз КОНРАД
Мерлин Джерард ФЛОМ
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Ели Лилли Энд Кампэни
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Publication of MD20000161A publication Critical patent/MD20000161A/ro
Publication of MD2335F2 publication Critical patent/MD2335F2/ro
Publication of MD2335G2 publication Critical patent/MD2335G2/ro

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    • C—CHEMISTRY; METALLURGY
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    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
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Abstract

Invenţia se referă la tehnologiile farmaceutice, în special la o formă cristalină nouă de hidroclorură de 6-hidroxi-3-(4-[2-(piperidin-1-il)etoxi]fenoxi)-2-(4-metoxifenil)benzo[b]tiofen, la un procedeu de obţinere şi la o compoziţie care o conţine.Hidratul cristalin de hidroclorură de 6-hidroxi-3-(4-[2-(piperidin-1-il)etoxi]fenoxi)-2-(4-metoxifenil)benzo[b]tiofen (arzofen), F-III, reprezintă un compus cu un grad înalt de cristalizare. Compoziţia farmaceutică pe baza lui conţine unul sau mai mulţi purtători, diluanţi sau excipienţi, estrogen, progestină, un inhibitor al aromatazei, un analog al hormonului, care eliberează hormonul luteinizant (LHRH) şi un inhibitor al acetilcolinesterazei. Procedeul de obţinere a compusului menţionat prevede cristalizarea hidroclorurii de 6-hidroxi-3-(4-[2-(piperidin-1-il)etoxi]fenoxi)-2-(4-metoxifenil)benzo[b]tiofen din amestecul de izopropanol şi apă, luate în raportul de (1...9):1, optimal fiind de (3...5,6):l.Compusul declarat se poate utiliza pentru inhibarea stărilor patologice asociate cu deficienţă de estrogen, cum ar fi fibroza uterină, endometrioza, restenoza, cancerul estrogen-dependent (inclusiv cancerul mamar şi cancerul uterin), cancerul de prostată, hiperplazia benignă a prostatei, osteoporoza, afecţiunile cardiovasculare, hiperlipidemia, tulburări ale SNC şi boala Alzheimer, prevenirea cancerului mamar şi activarea colinacetiltransferazei
MDA20000161A 1999-07-29 2000-07-28 Hidrat cristalin de hidroclorură de 6-hidroxi-3-(4-[2-(piperidin-1-il)etoxi]fenoxi)-2-(4-metoxifenil)benzo[b]tiofen, procedeu de obţinere, compoziţie farmaceutică care îl conţine şi utilizarea pentru inhibarea stărilor patologice şi activarea colinacetiltransferazei MD2335G2 (ro)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US14618499P 1999-07-29 1999-07-29
US14764299P 1999-08-06 1999-08-06
US14982099P 1999-08-19 1999-08-19

Publications (3)

Publication Number Publication Date
MD20000161A MD20000161A (ro) 2001-04-30
MD2335F2 MD2335F2 (ro) 2003-12-31
MD2335G2 true MD2335G2 (ro) 2004-06-30

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ID=27386367

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MDA20000161A MD2335G2 (ro) 1999-07-29 2000-07-28 Hidrat cristalin de hidroclorură de 6-hidroxi-3-(4-[2-(piperidin-1-il)etoxi]fenoxi)-2-(4-metoxifenil)benzo[b]tiofen, procedeu de obţinere, compoziţie farmaceutică care îl conţine şi utilizarea pentru inhibarea stărilor patologice şi activarea colinacetiltransferazei

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Families Citing this family (11)

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US7122203B2 (en) 2000-05-08 2006-10-17 Eli Lilly And Company Stabilized formulations of 6-hydroxy-3-(-4-[2-(piperidin-1-yl) ethoxy]phenoxy)-2-(4-methoxyphenyl) benzo[b]thiophene and salts thereof
EP1757291A3 (en) * 2000-05-08 2009-07-15 Eli Lilly & Company Stabilized formulations of 6-hydroxy-3-(4-[2-(piperidin-1-YL)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene and salts thereof
CZ20023651A3 (cs) * 2000-05-08 2003-02-12 Eli Lilly And Company Stabilizované přípravky 6-hydroxy-3-(4-[2-(piperidin-1-yl)-ethoxy]fenoxy)-2-(4-methoxyfenyl)benzo[b]thiofen a jejich sole
AU2005200809B2 (en) * 2000-05-08 2006-05-11 Eli Lilly And Company Stabilized Formulations of 6-hydroxy-3-(4-[2-(piperidin-1-yl) Ethoxy]phenoxy)-2-(4-methoxyphenyl) Benzo[b]thiophene and Salts Thereof
US20040014672A1 (en) * 2000-10-20 2004-01-22 Luke Wayne Douglas Novel crystalline form of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene hydrochloride
WO2002042289A2 (en) 2000-11-27 2002-05-30 Eli Lilly And Company Process for preparing 3-aryl-benzo[b]thiophenes
ATE480534T1 (de) * 2004-07-22 2010-09-15 Lilly Co Eli Kristallines variables hydrat von (s)-6-(4-(2-((3-(9h-carbazol-4-yloxy)-2-hydroxy ropyl)amino)-2- methylpropyl)phenoxy)-3-pyridincarbonsäureamid- hemisuccinatsalz
JP2008525439A (ja) * 2004-12-23 2008-07-17 ボイジャー・ファーマシューティカル・コーポレーション アルツハイマー病の治療のための酢酸ロイプロリド及びアセチルコリンエステラーゼインヒビターまたはｎｍｄａレセプターアゴニスト
WO2006088648A1 (en) * 2005-02-11 2006-08-24 Eli Lilly And Company Compositions and methods for treating dyslipidemia
DE102008057230A1 (de) * 2008-11-11 2010-05-12 Bayer Schering Pharma Aktiengesellschaft Synergistische pharmazeutische Kombination mit einem Estrogenrezeptorantagonisten und einem Progestin
CN113325183B (zh) * 2021-06-01 2022-11-15 中国医学科学院北京协和医院 一种用于鉴别诊断em/fem的试剂盒

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US5510357A (en) * 1995-02-28 1996-04-23 Eli Lilly And Company Benzothiophene compounds as anti-estrogenic agents
EP0729956A1 (en) * 1995-02-28 1996-09-04 Eli Lilly And Company Benzothiophene compounds, intermediates, compositions, and methods

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WO2001009116A2 (en) * 1999-07-29 2001-02-08 Eli Lilly And Company A NOVEL CRYSTALLINE FORM OF 6-HYDROXY-3- (4-[2-(PIPERIDIN-1-YL) ETHOXY]PHENOXY)- 2-(4-METHOXYPHENYL)BENZO[b]THIOPHENE HYDROCHLORIDE

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US5510357A (en) * 1995-02-28 1996-04-23 Eli Lilly And Company Benzothiophene compounds as anti-estrogenic agents
EP0729956A1 (en) * 1995-02-28 1996-09-04 Eli Lilly And Company Benzothiophene compounds, intermediates, compositions, and methods
US5723474A (en) * 1995-02-28 1998-03-03 Eli Lilly And Company Benzothiophene compounds, intermediates, compositions, and methods

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CA2314685A1 (en) 2001-01-29
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AU6335500A (en) 2001-02-19
AU4891100A (en) 2001-02-01
SI20427B (sl) 2009-04-30
MD2335F2 (ro) 2003-12-31
AR029176A1 (es) 2003-06-18
SV2002000134A (es) 2002-06-07
SE0002793D0 (sv) 2000-07-28
PL341748A1 (en) 2001-02-12
WO2001009115A2 (en) 2001-02-08
NL1015822A1 (nl) 2001-01-30
LU90616B1 (fr) 2007-06-08
HK1034962A1 (en) 2001-11-09
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HRP20000502B1 (en) 2008-04-30
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FR2798384B1 (fr) 2004-09-24
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TR200002205A2 (tr) 2001-03-21
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FR2798384A1 (fr) 2001-03-16
TWI271403B (en) 2007-01-21
BE1013410A3 (fr) 2001-12-04
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IE20000604A1 (en) 2001-04-04
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DK176771B1 (da) 2009-08-03
AU779559B2 (en) 2005-01-27
JP2001048880A (ja) 2001-02-20
FI20001721L (fi) 2001-01-30

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