NL1015821C2 - Een nieuwe kristallijne vorm van 6-hydroxy-3-(4-[2-(piperidin-1-yl) ethoxy]fenoxy)-2-(4-methoxyfenyl)benzo[b]thiofeen hydrochloride. - Google Patents

Een nieuwe kristallijne vorm van 6-hydroxy-3-(4-[2-(piperidin-1-yl) ethoxy]fenoxy)-2-(4-methoxyfenyl)benzo[b]thiofeen hydrochloride. Download PDF

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Publication number
NL1015821C2
NL1015821C2 NL1015821A NL1015821A NL1015821C2 NL 1015821 C2 NL1015821 C2 NL 1015821C2 NL 1015821 A NL1015821 A NL 1015821A NL 1015821 A NL1015821 A NL 1015821A NL 1015821 C2 NL1015821 C2 NL 1015821C2
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Netherlands
Prior art keywords
formulation
estrogen
compound
excipients
optionally
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NL1015821A
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English (en)
Dutch (nl)
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NL1015821A1 (nl
Inventor
Preston Charles Conrad
Wayne Douglas Luke
Julie Kay Bush
Merlyn Gerard Flom
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Lilly Co Eli
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Publication of NL1015821A1 publication Critical patent/NL1015821A1/xx
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Publication of NL1015821C2 publication Critical patent/NL1015821C2/nl

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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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • 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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • Diabetes (AREA)
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  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
NL1015821A 1999-07-29 2000-07-27 Een nieuwe kristallijne vorm van 6-hydroxy-3-(4-[2-(piperidin-1-yl) ethoxy]fenoxy)-2-(4-methoxyfenyl)benzo[b]thiofeen hydrochloride. NL1015821C2 (nl)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US14628699P 1999-07-29 1999-07-29
US14628699 1999-07-29
US14757099P 1999-08-06 1999-08-06
US14757099 1999-08-06
US14977399P 1999-08-19 1999-08-19
US14977399 1999-08-19

Publications (2)

Publication Number Publication Date
NL1015821A1 NL1015821A1 (nl) 2001-01-30
NL1015821C2 true NL1015821C2 (nl) 2002-01-03

Family

ID=27386379

Family Applications (1)

Application Number Title Priority Date Filing Date
NL1015821A NL1015821C2 (nl) 1999-07-29 2000-07-27 Een nieuwe kristallijne vorm van 6-hydroxy-3-(4-[2-(piperidin-1-yl) ethoxy]fenoxy)-2-(4-methoxyfenyl)benzo[b]thiofeen hydrochloride.

Country Status (45)

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

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.
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
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
DZ3376A1 (fr) * 2000-05-08 2001-11-15 Lilly Co Eli Formulations stabilisees de 6-hydroxy-3-(4-[2-(piperidin-1-yl) ethoxy]phenoxy)-2-(4-methoxyphenyl) benzo[b]thiophene et sels de ces composes
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
BR0114792A (pt) * 2000-10-20 2003-08-12 Lilly Co Eli Composto cristalino, anidro, não solvatado, de cloridreto de 6-hidróxi-3-(-4-[2-piperidin-1-il)-etóxi]-fenóxi)-2-(4-metóx i-fenil)-benzol[b]tiofeno (f-v), formulação farmacêutica, processo para preparar um composto, e uso de um composto
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
ES2349798T3 (es) * 2004-07-22 2011-01-11 Eli Lilly And Company Hidrato variable cristalino de la sal hemisuccinato de (s)-6-(4-(2-((3-(9h-carbazol-4-iloxi)-2-hidroxipropil)amino)-2-metilpropil)fenoxi)-3-piridinocarboxamida.

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0729956A1 (en) * 1995-02-28 1996-09-04 Eli Lilly And Company Benzothiophene compounds, intermediates, compositions, and methods
WO1998045287A1 (en) * 1997-04-09 1998-10-15 Eli Lilly And Company Treatment of central nervous system disorders with selective estrogen receptor modulators

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0729956A1 (en) * 1995-02-28 1996-09-04 Eli Lilly And Company Benzothiophene compounds, intermediates, compositions, and methods
WO1998045287A1 (en) * 1997-04-09 1998-10-15 Eli Lilly And Company Treatment of central nervous system disorders with selective estrogen receptor modulators

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
RABASSEDA X ET AL: "ARZOXIFENE HYDROCHLORIDE ESTROGEN RECEPTOR MODULATOR TREATMENT OF POSTMENOPAUSAL SYNDROME ANTINEOPLASTIC", DRUGS OF THE FUTURE, BARCELONA, ES, vol. 24, no. 6, June 1999 (1999-06-01), pages 599 - 604, XP000982097, ISSN: 0377-8282 *

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Publication number Publication date
MD20000162A (en) 2001-04-30
SE0002792D0 (sv) 2000-07-28
GB0018641D0 (en) 2000-09-13
HK1035370A1 (en) 2001-11-23
FR2796944A1 (fr) 2001-02-02
CN1288007A (zh) 2001-03-21
MD2336F2 (en) 2003-12-31
CA2314682A1 (en) 2001-01-29
MXPA00007461A (es) 2004-07-16
HUP0003001A2 (hu) 2002-04-29
LV12623B (en) 2001-07-20
AR031073A1 (es) 2003-09-10
WO2001009116A2 (en) 2001-02-08
ITMI20001759A0 (it) 2000-07-28
BE1013411A3 (fr) 2001-12-04
AU6335600A (en) 2001-02-19
IL137553A0 (en) 2001-07-24
SI20426A (sl) 2001-06-30
BR0003209A (pt) 2001-03-20
TR200002206A2 (tr) 2001-03-21
CO5180570A1 (es) 2002-07-30
MD2336G2 (ro) 2004-06-30
IT1318660B1 (it) 2003-08-27
CN1138770C (zh) 2004-02-18
PT102502A (pt) 2001-01-31
DE10036854A1 (de) 2001-03-01
FI20001722A0 (fi) 2000-07-28
NO20003879L (no) 2001-01-30
HRP20000503A2 (en) 2001-06-30
ITMI20001759A1 (it) 2002-01-28
LV12623A (en) 2001-03-20
AT502318A1 (de) 2007-02-15
KR20010049916A (ko) 2001-06-15
FI20001722A (fi) 2001-01-30
JP2001064277A (ja) 2001-03-13
GB2352717A (en) 2001-02-07
IL137553A (en) 2005-09-25
SE0002792L (sv) 2001-01-30
KR100697177B1 (ko) 2007-03-21
LU90617B1 (fr) 2001-06-15
SG91296A1 (en) 2002-09-17
LT2000076A (lt) 2001-02-26
GR20000100265A (el) 2001-03-30
ID27078A (id) 2001-02-22
NL1015821A1 (nl) 2001-01-30
IE20000605A1 (en) 2001-04-04
LT4790B (lt) 2001-05-25
FR2796944B1 (fr) 2003-01-31
DK200001151A (da) 2001-01-30
HRP20000503B1 (en) 2008-04-30
UA72885C2 (uk) 2005-05-16
SV2002000132A (es) 2002-06-07
CZ20002716A3 (en) 2001-05-16
MY128764A (en) 2007-02-28
CZ299311B6 (cs) 2008-06-18
PE20010385A1 (es) 2001-04-06
PL341749A1 (en) 2001-02-12
NO20003879D0 (no) 2000-07-28
WO2001009116A3 (en) 2001-05-17
TWI276437B (en) 2007-03-21
HU0003001D0 (en) 2000-10-28
DZ3060A1 (fr) 2004-05-22
GR1004084B (el) 2002-12-11
EP1204656A2 (en) 2002-05-15
RO121851B1 (ro) 2008-06-30

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