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CO5180570A1 - A NEW CRYSTALLINE FORM OF 6-HYDROXI- 3- (4- [2- (PIPERIDIN-1-IL) ETOXI] PHENOXI CHLORIDE HYDROXYIDE BENZO [B] THIOPHEN - Google Patents

A NEW CRYSTALLINE FORM OF 6-HYDROXI- 3- (4- [2- (PIPERIDIN-1-IL) ETOXI] PHENOXI CHLORIDE HYDROXYIDE BENZO [B] THIOPHEN

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Publication number
CO5180570A1
CO5180570A1 CO00056521A CO00056521A CO5180570A1 CO 5180570 A1 CO5180570 A1 CO 5180570A1 CO 00056521 A CO00056521 A CO 00056521A CO 00056521 A CO00056521 A CO 00056521A CO 5180570 A1 CO5180570 A1 CO 5180570A1
Authority
CO
Colombia
Prior art keywords
piperidin
benzo
phenoxi
hydroxyide
etoxi
Prior art date
Application number
CO00056521A
Other languages
Spanish (es)
Inventor
Julie Kay Bush
Charles Conrad Preston
Gerard Flom Merlyn
Wayne Douglas Luke
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of CO5180570A1 publication Critical patent/CO5180570A1/en

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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
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
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    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
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    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32—Antioestrogens
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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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  • Health & Medical Sciences (AREA)
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  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

El hidrato cristalino del clorhidrato de 6-hidroxi-3-(4-[2-(piperidin-1-il)etoxi]fenoxi)-2-(4-metoxifenil)benzo(b]tiofeno (F-I) de fórmula :<EMI FILE="00056521_1" ID="1" IMF=JPEG >que tiene un modelo de difracción de rayos X 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 ± 0,2° en 2T; cuando se obtiene a partir de una fuente de radiación de cobre.Crystalline hydrate of 6-hydroxy-3- (4- [2- (piperidin-1-yl) ethoxy] phenoxy) -2- (4-methoxyphenyl) benzo (b] thiophene (FI) hydrochloride of formula: <EMI FILE = "00056521_1" ID = "1" MFI = JPEG> which has an X-ray diffraction model comprising the following peaks: 7.9 ± 0.2, 10.7 ± 0.2, 14.9 ± 0 , 2, 15.9 ± 0.2, 18.3 ± 0.2, and 20.6 ± 0.2 ° in 2T; when obtained from a source of copper radiation.

CO00056521A 1999-07-29 2000-07-27 A NEW CRYSTALLINE FORM OF 6-HYDROXI- 3- (4- [2- (PIPERIDIN-1-IL) ETOXI] PHENOXI CHLORIDE HYDROXYIDE BENZO [B] THIOPHEN CO5180570A1 (en)

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
CO5180570A1 true CO5180570A1 (en) 2002-07-30

Family

ID=27386379

Family Applications (1)

Application Number Title Priority Date Filing Date
CO00056521A CO5180570A1 (en) 1999-07-29 2000-07-27 A NEW CRYSTALLINE FORM OF 6-HYDROXI- 3- (4- [2- (PIPERIDIN-1-IL) ETOXI] PHENOXI CHLORIDE HYDROXYIDE BENZO [B] THIOPHEN

Country Status (44)

Country Link
EP (1) EP1204656A2 (en)
JP (1) JP2001064277A (en)
KR (1) KR100697177B1 (en)
CN (1) CN1138770C (en)
AR (1) AR031073A1 (en)
AT (1) AT502318A1 (en)
AU (1) AU6335600A (en)
BE (1) BE1013411A3 (en)
BR (1) BR0003209A (en)
CA (1) CA2314682A1 (en)
CO (1) CO5180570A1 (en)
CZ (1) CZ299311B6 (en)
DE (1) DE10036854A1 (en)
DK (1) DK200001151A (en)
DZ (1) DZ3060A1 (en)
FI (1) FI20001722A7 (en)
FR (1) FR2796944B1 (en)
GB (1) GB2352717A (en)
GR (1) GR1004084B (en)
HR (1) HRP20000503B1 (en)
HU (1) HUP0003001A2 (en)
ID (1) ID27078A (en)
IL (1) IL137553A (en)
IT (1) IT1318660B1 (en)
LT (1) LT4790B (en)
LU (1) LU90617B1 (en)
LV (1) LV12623B (en)
MD (1) MD2336G2 (en)
MX (1) MXPA00007461A (en)
MY (1) MY128764A (en)
NL (1) NL1015821C2 (en)
NO (1) NO20003879L (en)
PE (1) PE20010385A1 (en)
PL (1) PL341749A1 (en)
PT (1) PT102502A (en)
RO (1) RO121851B1 (en)
SE (1) SE0002792L (en)
SG (1) SG91296A1 (en)
SI (1) SI20426A (en)
SV (1) SV2002000132A (en)
TR (1) TR200002206A2 (en)
TW (1) TWI276437B (en)
UA (1) UA72885C2 (en)
WO (1) WO2001009116A2 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU6335500A (en) * 1999-07-29 2001-02-19 Eli Lilly And Company A novel crystalline form of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-metho yphenyl)benzo[b]thiophene hydrochloride
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
IL152699A0 (en) * 2000-05-08 2003-06-24 Lilly Co Eli 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 &amp; Company Stabilized formulations of 6-hydroxy-3-(4-[2-(piperidin-1-YL)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene and salts thereof
EP1157996A1 (en) * 2000-05-23 2001-11-28 JENAPHARM GmbH New solid forms of mesoprogestin 11beta-(4E-(hydroxyiminomethyl)-phenyl)-17alpha-methoxymethyl-17beta-methoxy-estra-4,9-dien-3-on
UA76124C2 (en) * 2000-10-20 2006-07-17 Lilly Co Eli A crystal form of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]-phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene hydrochloride, pharmaceutical composition and a method for producing
US6921827B2 (en) 2000-11-27 2005-07-26 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
WO2006019835A1 (en) * 2004-07-22 2006-02-23 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-pyridinicarbox amide hemisuccinate salt

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR003930A1 (en) * 1995-02-28 1998-09-30 Lilly Co Eli PROCEDURE FOR PREPARING COMPOUNDS OF 2-PHENYL-3-PHENOXY OR PHENYLTIO-BENZOTIOFEN AND PHARMACEUTICALLY ACCEPTABLE SALTS, INTERMEDIATE COMPOUNDS OF EXCLUSIVE APPLICATION IN SUCH PROCEDURE AND METHOD FOR PREPARING INTERMEDIATE COMPOUNDS
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.

Also Published As

Publication number Publication date
HU0003001D0 (en) 2000-10-28
BR0003209A (en) 2001-03-20
LT2000076A (en) 2001-02-26
IL137553A (en) 2005-09-25
RO121851B1 (en) 2008-06-30
EP1204656A2 (en) 2002-05-15
HRP20000503A2 (en) 2001-06-30
IE20000605A1 (en) 2001-04-04
WO2001009116A2 (en) 2001-02-08
CN1288007A (en) 2001-03-21
WO2001009116A3 (en) 2001-05-17
SE0002792D0 (en) 2000-07-28
DZ3060A1 (en) 2004-05-22
TWI276437B (en) 2007-03-21
NO20003879D0 (en) 2000-07-28
ITMI20001759A0 (en) 2000-07-28
JP2001064277A (en) 2001-03-13
UA72885C2 (en) 2005-05-16
DK200001151A (en) 2001-01-30
HUP0003001A2 (en) 2002-04-29
GR20000100265A (en) 2001-03-30
CZ20002716A3 (en) 2001-05-16
FI20001722A0 (en) 2000-07-28
ITMI20001759A1 (en) 2002-01-28
LT4790B (en) 2001-05-25
CA2314682A1 (en) 2001-01-29
SE0002792L (en) 2001-01-30
IL137553A0 (en) 2001-07-24
FI20001722L (en) 2001-01-30
CN1138770C (en) 2004-02-18
LV12623B (en) 2001-07-20
MD2336G2 (en) 2004-06-30
MD2336F2 (en) 2003-12-31
NL1015821C2 (en) 2002-01-03
HK1035370A1 (en) 2001-11-23
LV12623A (en) 2001-03-20
NO20003879L (en) 2001-01-30
BE1013411A3 (en) 2001-12-04
ID27078A (en) 2001-02-22
MXPA00007461A (en) 2004-07-16
KR100697177B1 (en) 2007-03-21
MY128764A (en) 2007-02-28
FR2796944A1 (en) 2001-02-02
PT102502A (en) 2001-01-31
TR200002206A2 (en) 2001-03-21
IT1318660B1 (en) 2003-08-27
MD20000162A (en) 2001-04-30
SI20426A (en) 2001-06-30
LU90617B1 (en) 2001-06-15
AT502318A1 (en) 2007-02-15
FI20001722A7 (en) 2001-01-30
FR2796944B1 (en) 2003-01-31
AU6335600A (en) 2001-02-19
DE10036854A1 (en) 2001-03-01
HRP20000503B1 (en) 2008-04-30
SG91296A1 (en) 2002-09-17
KR20010049916A (en) 2001-06-15
PE20010385A1 (en) 2001-04-06
NL1015821A1 (en) 2001-01-30
SV2002000132A (en) 2002-06-07
GB2352717A (en) 2001-02-07
CZ299311B6 (en) 2008-06-18
PL341749A1 (en) 2001-02-12
GR1004084B (en) 2002-12-11
AR031073A1 (en) 2003-09-10
GB0018641D0 (en) 2000-09-13

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