AR031073A1 - Una nueva forma cristalina de clorhidrato de 6-hidroxi-3-(4-[2-(piperidin-1-il)etoxi)fenoxi]-2-(4-metoxifenil)benzo(b)tiofeno; formulaciones farmaceuticas que comprenden dicha forma cristalina; procedimiento para preparar la forma cristalina mencionada y la forma cristalina que se obtiene con el pro - Google Patents

Una nueva forma cristalina de clorhidrato de 6-hidroxi-3-(4-[2-(piperidin-1-il)etoxi)fenoxi]-2-(4-metoxifenil)benzo(b)tiofeno; formulaciones farmaceuticas que comprenden dicha forma cristalina; procedimiento para preparar la forma cristalina mencionada y la forma cristalina que se obtiene con el pro

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Publication number
AR031073A1
AR031073A1 ARP000103928A ARP000103928A AR031073A1 AR 031073 A1 AR031073 A1 AR 031073A1 AR P000103928 A ARP000103928 A AR P000103928A AR P000103928 A ARP000103928 A AR P000103928A AR 031073 A1 AR031073 A1 AR 031073A1
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AR
Argentina
Prior art keywords
crystal form
piperidin
benzo
cancer
phenoxi
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ARP000103928A
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English (en)
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Lilly Co Eli
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Publication date
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Publication of AR031073A1 publication Critical patent/AR031073A1/es

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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
    • 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
    • A61K31/435—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
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • A61K38/09—Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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Abstract

La presente invencion se refiere a un nuevo hidrato cristalino del clorhidrato de 6- hidroxi-3-(4-[2-(piperidin-1-il)etoxil]-fenoxi]-2-(4-metoxifenil)benzo[b]tiofeno que posee el siguiente diagrama de difraccion en Rx. que comprende los siguientes picos: 7,9 +- 0,2, 10,7 +- 0,2, 14,9 +- 0,2, 15,9 +- 0,2, 18,3 +- 0,2, y 20,6 +- 0,2s en 2c; cuando se obtiene a partir de una fuente de radiacion de cobre. La invencion comprende el uso de dicho compuesto, incluyendo la inhibicion de estados de enfermedad asociados con la privacion de estrogenos que incluyen enfermedades cardiovasculares, hiperlipidemia y osteoporosis; y la inhibicion de otros trastornos patologicos tales como la endometriosis, la fibrosis uterina, el cáncer dependiente de estrogenos (incluyendo el cáncer de mama y uterino), el cáncer de prostata, la hiperplasia prostática benigna, trastornos del SNC que incluyen la enfermedad de Alzheimer, prevencion del cáncer mama y regulacion positiva de la ChAT. También se describen y reivindican los objetos restantes mencionados en el título.
ARP000103928A 1999-07-29 2000-07-28 Una nueva forma cristalina de clorhidrato de 6-hidroxi-3-(4-[2-(piperidin-1-il)etoxi)fenoxi]-2-(4-metoxifenil)benzo(b)tiofeno; formulaciones farmaceuticas que comprenden dicha forma cristalina; procedimiento para preparar la forma cristalina mencionada y la forma cristalina que se obtiene con el pro AR031073A1 (es)

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 (1)

Publication Number Publication Date
AR031073A1 true AR031073A1 (es) 2003-09-10

Family

ID=27386379

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP000103928A AR031073A1 (es) 1999-07-29 2000-07-28 Una nueva forma cristalina de clorhidrato de 6-hidroxi-3-(4-[2-(piperidin-1-il)etoxi)fenoxi]-2-(4-metoxifenil)benzo(b)tiofeno; formulaciones farmaceuticas que comprenden dicha forma cristalina; procedimiento para preparar la forma cristalina mencionada y la forma cristalina que se obtiene con el pro

Country Status (45)

Country Link
EP (1) EP1204656A2 (es)
JP (1) JP2001064277A (es)
KR (1) KR100697177B1 (es)
CN (1) CN1138770C (es)
AR (1) AR031073A1 (es)
AT (1) AT502318A1 (es)
AU (1) AU6335600A (es)
BE (1) BE1013411A3 (es)
BR (1) BR0003209A (es)
CA (1) CA2314682A1 (es)
CO (1) CO5180570A1 (es)
CZ (1) CZ299311B6 (es)
DE (1) DE10036854A1 (es)
DK (1) DK200001151A (es)
DZ (1) DZ3060A1 (es)
FI (1) FI20001722A (es)
FR (1) FR2796944B1 (es)
GB (1) GB2352717A (es)
GR (1) GR1004084B (es)
HK (1) HK1035370A1 (es)
HR (1) HRP20000503B1 (es)
HU (1) HUP0003001A2 (es)
ID (1) ID27078A (es)
IL (1) IL137553A (es)
IT (1) IT1318660B1 (es)
LT (1) LT4790B (es)
LU (1) LU90617B1 (es)
LV (1) LV12623B (es)
MD (1) MD2336G2 (es)
MX (1) MXPA00007461A (es)
MY (1) MY128764A (es)
NL (1) NL1015821C2 (es)
NO (1) NO20003879L (es)
PE (1) PE20010385A1 (es)
PL (1) PL341749A1 (es)
PT (1) PT102502A (es)
RO (1) RO121851B1 (es)
SE (1) SE0002792L (es)
SG (1) SG91296A1 (es)
SI (1) SI20426A (es)
SV (1) SV2002000132A (es)
TR (1) TR200002206A2 (es)
TW (1) TWI276437B (es)
UA (1) UA72885C2 (es)
WO (1) WO2001009116A2 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2208384T3 (es) * 1999-07-29 2004-06-16 Eli Lilly And Company Forma cristalina de clorhidrato de 6 hidroxi-3-(4-(2-(piperidin-1-il)-etoxi)-fenoxi)2--(4-metoxifenil)-benzo(b)tiofeno.
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
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
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
PL360946A1 (en) * 2000-10-20 2004-09-20 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
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
PT1773811E (pt) * 2004-07-22 2010-10-19 Lilly Co Eli Um hidrato cristalino variável de sal de hemissuccinato de (s)-6-(4-(2-((3-(9h-carbazol-4-iloxi)-2- hidroxipropil)amino)-2-metilpropil)fenoxi)-3-piridinicarbox amida

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3989569B2 (ja) * 1995-02-28 2007-10-10 イーライ リリー アンド カンパニー ベンゾチオフェン化合物、中間体、組成物および方法
US5510357A (en) 1995-02-28 1996-04-23 Eli Lilly And Company Benzothiophene compounds as anti-estrogenic agents
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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MY128764A (en) 2007-02-28
ITMI20001759A0 (it) 2000-07-28
KR100697177B1 (ko) 2007-03-21
AU6335600A (en) 2001-02-19
CN1138770C (zh) 2004-02-18
NL1015821C2 (nl) 2002-01-03
LT4790B (lt) 2001-05-25
GB0018641D0 (en) 2000-09-13
HU0003001D0 (en) 2000-10-28
DK200001151A (da) 2001-01-30
CZ299311B6 (cs) 2008-06-18
LT2000076A (lt) 2001-02-26
FI20001722A (fi) 2001-01-30
LU90617B1 (fr) 2001-06-15
JP2001064277A (ja) 2001-03-13
HRP20000503B1 (en) 2008-04-30
FR2796944B1 (fr) 2003-01-31
GB2352717A (en) 2001-02-07
NO20003879L (no) 2001-01-30
IL137553A (en) 2005-09-25
UA72885C2 (uk) 2005-05-16
BR0003209A (pt) 2001-03-20
HRP20000503A2 (en) 2001-06-30
GR1004084B (el) 2002-12-11
BE1013411A3 (fr) 2001-12-04
RO121851B1 (ro) 2008-06-30
CA2314682A1 (en) 2001-01-29
PL341749A1 (en) 2001-02-12
TWI276437B (en) 2007-03-21
LV12623A (en) 2001-03-20
ITMI20001759A1 (it) 2002-01-28
LV12623B (en) 2001-07-20
PE20010385A1 (es) 2001-04-06
SE0002792L (sv) 2001-01-30
IL137553A0 (en) 2001-07-24
CO5180570A1 (es) 2002-07-30
MD2336F2 (en) 2003-12-31
NL1015821A1 (nl) 2001-01-30
KR20010049916A (ko) 2001-06-15
MXPA00007461A (es) 2004-07-16
MD20000162A (en) 2001-04-30
ID27078A (id) 2001-02-22
SI20426A (sl) 2001-06-30
TR200002206A2 (tr) 2001-03-21
CN1288007A (zh) 2001-03-21
FR2796944A1 (fr) 2001-02-02
SV2002000132A (es) 2002-06-07
HK1035370A1 (en) 2001-11-23
DZ3060A1 (fr) 2004-05-22
EP1204656A2 (en) 2002-05-15
SE0002792D0 (sv) 2000-07-28
FI20001722A0 (fi) 2000-07-28
CZ20002716A3 (en) 2001-05-16
DE10036854A1 (de) 2001-03-01
PT102502A (pt) 2001-01-31
NO20003879D0 (no) 2000-07-28
IT1318660B1 (it) 2003-08-27
WO2001009116A2 (en) 2001-02-08
WO2001009116A3 (en) 2001-05-17
IE20000605A1 (en) 2001-04-04
SG91296A1 (en) 2002-09-17
HUP0003001A2 (hu) 2002-04-29
GR20000100265A (el) 2001-03-30
AT502318A1 (de) 2007-02-15
MD2336G2 (ro) 2004-06-30

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