MD2336G2 - Кристаллический гидрат 6-гидрокси-3-(4-[2-(пиперидин-1-ил) этокси]фенокси)-2-(4-метоксифенил)бензо[b]тиофен гидрохлорида, способ получения, фармацевтическая композиция его содержащая и применение для ингибирования паталогических состояний и активирования холинацетилтрансферазы - Google Patents

Кристаллический гидрат 6-гидрокси-3-(4-[2-(пиперидин-1-ил) этокси]фенокси)-2-(4-метоксифенил)бензо[b]тиофен гидрохлорида, способ получения, фармацевтическая композиция его содержащая и применение для ингибирования паталогических состояний и активирования холинацетилтрансферазы

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Publication number
MD2336G2
MD2336G2 MDA20000162A MD20000162A MD2336G2 MD 2336 G2 MD2336 G2 MD 2336G2 MD A20000162 A MDA20000162 A MD A20000162A MD 20000162 A MD20000162 A MD 20000162A MD 2336 G2 MD2336 G2 MD 2336G2
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MD
Moldova
Prior art keywords
benzo
piperidine
phenoxy
ethoxy
hydroxy
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Application number
MDA20000162A
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English (en)
Romanian (ro)
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MD2336F2 (en
MD20000162A (en
Inventor
Джули Кей Буш
Престон Чарлз КОНРАД
Мерлин Джерард ФЛОМ
Вэйн Дуглас ЛЮК
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Ели Лилли Энд Кампэни
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Application filed by Ели Лилли Энд Кампэни filed Critical Ели Лилли Энд Кампэни
Publication of MD20000162A publication Critical patent/MD20000162A/xx
Publication of MD2336F2 publication Critical patent/MD2336F2/xx
Publication of MD2336G2 publication Critical patent/MD2336G2/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D333/64—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
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    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/567—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
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    • A61K38/08—Peptides having 5 to 11 amino acids
    • A61K38/09—Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A—HUMAN NECESSITIES
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Abstract

Изобретение относится к фармацевтической технологии, в частности к новой кристаллической форме 6-гидрокси-3-(4-[2-(пиперидин-1-ил) этокси]фенокси)-2-(4-метоксифенил)бензо[b]тиофен гидрохлорида, способу получения и композиции его содержащей.Кристаллический гидрат 6-гидрокси-3-(4-[2-(пиперидин-1-ил) этокси]фенокси)-2-(4-метоксифенил)бензо[b]тиофен гидрохлорида (арзофен), F-1, представляет собой вещество с высокой степенью кристаллизации. Фармацевтическая композиция на его основе содержит один или больше носителей, растворители или заменители и при необходимости эстроген, прогестин, ингибитор ароматазы, аналог гормона, который освобождает лютеинизирующий гормон (LHRH) и ингибитор ацетилхолинэстэразы. Способ получения упомянутого вещества предусматривает кристаллизацию 6-гидрокси-3-(4-[2-(пиперидин-1-ил)этокси]фенокси)-2-(4-метоксифенил)бензо[b]тиофен гидрохлорида из тетрагидрофурана.Заявленное соединение можно использовать для ингибирования патологических состояний, связанных с дефицитом эстрогена, таких, как фиброз матки, эндометриоз, пролиферацию гладких мышечных клеток в аорте, рестеноз, эстроген-зависимый рак (включая рак молочной железы и рак матки), рак простаты, доброкачественная гиперплазия простаты, остеопороз, сердечно-сосудистые заболевания, гиперлипидемия, расстройства ЦНС и болезнь Альцгеймера, предупреждения рака молочной железы и активирования холинацетилтрансферазы.
MDA20000162A 1999-07-29 2000-07-28 Кристаллический гидрат 6-гидрокси-3-(4-[2-(пиперидин-1-ил) этокси]фенокси)-2-(4-метоксифенил)бензо[b]тиофен гидрохлорида, способ получения, фармацевтическая композиция его содержащая и применение для ингибирования паталогических состояний и активирования холинацетилтрансферазы MD2336G2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US14628699P 1999-07-29 1999-07-29
US14757099P 1999-08-06 1999-08-06
US14977399P 1999-08-19 1999-08-19

Publications (3)

Publication Number Publication Date
MD20000162A MD20000162A (en) 2001-04-30
MD2336F2 MD2336F2 (en) 2003-12-31
MD2336G2 true MD2336G2 (ru) 2004-06-30

Family

ID=27386379

Family Applications (1)

Application Number Title Priority Date Filing Date
MDA20000162A MD2336G2 (ru) 1999-07-29 2000-07-28 Кристаллический гидрат 6-гидрокси-3-(4-[2-(пиперидин-1-ил) этокси]фенокси)-2-(4-метоксифенил)бензо[b]тиофен гидрохлорида, способ получения, фармацевтическая композиция его содержащая и применение для ингибирования паталогических состояний и активирования холинацетилтрансферазы

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EP (1) EP1204656A2 (ru)
JP (1) JP2001064277A (ru)
KR (1) KR100697177B1 (ru)
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Families Citing this family (9)

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Publication number Priority date Publication date Assignee Title
ATE251151T1 (de) * 1999-07-29 2003-10-15 Lilly Co Eli Eine kristalline form von 6-hydroxy-3-(4-(2- (piperidin-1-yl)ethoxy)phenoxy)-2-(4- methoxyphenyl)benzo(b)thiophen-hydrochlorid
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
DE60125416T2 (de) * 2000-05-08 2007-09-27 Eli Lilly And Co., Indianapolis Stabilisierte formulierungen von 6-hydroxy-3-(4-(2-(piperidin-1-yl)ethoxy)phenoxy)-2-(4-methoxyphenyl)benzo(b)thiophen und deren salze
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
EP1157996A1 (de) * 2000-05-23 2001-11-28 JENAPHARM GmbH Neue Festkörperformen des Mesoprogestins 11Beta-[4E-(Hydroxyiminomethyl)-phenyl]-17Alpha-methoxymethyl-17Beta-methoxy-estra-4,9-dien-3-on
IL155487A0 (en) * 2000-10-20 2003-11-23 Lilly Co Eli A 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
CA2393720C (en) * 2002-07-12 2010-09-14 Eli Lilly And Company Crystalline 2,5-dione-3-(1-methyl-1h-indol-3-yl)-4-[1-(pyridin-2-ylmethyl)piperidin-4-yl]-1h-indol-3-yl]-1h-pyrrole mono-hydrochloride
EP1773811B1 (en) * 2004-07-22 2010-09-08 Eli Lilly And Company A crystalline variable hydrate of (s)-6-(4-(2-((3-(9h-carbazol-4-yloxy)-2-hydroxypropyl)amino)-2-methylpropyl)phenoxy)-3-pyridinecarbox amide hemisuccinate salt

Citations (2)

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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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ZA9710262B (en) * 1996-11-19 1999-05-13 Lilly Co Eli Process for the synthesis of benzothiophenes
ZA982877B (en) * 1997-04-09 1999-10-04 Lilly Co Eli Treatment of central nervous system disorders with selective estrogen receptor modulators.

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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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DZ3060A1 (fr) 2004-05-22
MD2336F2 (en) 2003-12-31
UA72885C2 (ru) 2005-05-16
SE0002792D0 (sv) 2000-07-28
SG91296A1 (en) 2002-09-17
AR031073A1 (es) 2003-09-10
BR0003209A (pt) 2001-03-20
AU6335600A (en) 2001-02-19
DK200001151A (da) 2001-01-30
WO2001009116A2 (en) 2001-02-08
BE1013411A3 (fr) 2001-12-04
FI20001722A (fi) 2001-01-30
SE0002792L (sv) 2001-01-30
GR1004084B (el) 2002-12-11
EP1204656A2 (en) 2002-05-15
FI20001722A0 (fi) 2000-07-28
HRP20000503A2 (en) 2001-06-30
GR20000100265A (el) 2001-03-30
LT2000076A (lt) 2001-02-26
TR200002206A2 (tr) 2001-03-21
CA2314682A1 (en) 2001-01-29
IT1318660B1 (it) 2003-08-27
CO5180570A1 (es) 2002-07-30
NL1015821A1 (nl) 2001-01-30
MXPA00007461A (es) 2004-07-16
SV2002000132A (es) 2002-06-07
LV12623B (en) 2001-07-20
PL341749A1 (en) 2001-02-12
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MY128764A (en) 2007-02-28
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HK1035370A1 (en) 2001-11-23
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HUP0003001A2 (hu) 2002-04-29
ITMI20001759A0 (it) 2000-07-28
KR100697177B1 (ko) 2007-03-21
FR2796944B1 (fr) 2003-01-31
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ID27078A (id) 2001-02-22
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JP2001064277A (ja) 2001-03-13
WO2001009116A3 (en) 2001-05-17
FR2796944A1 (fr) 2001-02-02
LT4790B (lt) 2001-05-25

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