DK176771B1 - Ny krystallinsk form af 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophen hydrochlorid, anvendelse heraf i lægemiddelformuleringer, samt fremgangsmåde til fremstilling heraf - Google Patents

Ny krystallinsk form af 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophen hydrochlorid, anvendelse heraf i lægemiddelformuleringer, samt fremgangsmåde til fremstilling heraf Download PDF

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Publication number
DK176771B1
DK176771B1 DK200001150A DKPA200001150A DK176771B1 DK 176771 B1 DK176771 B1 DK 176771B1 DK 200001150 A DK200001150 A DK 200001150A DK PA200001150 A DKPA200001150 A DK PA200001150A DK 176771 B1 DK176771 B1 DK 176771B1
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iii
compound
formulation
estrogen
water
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DK200001150A
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Danish (da)
English (en)
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Preston Charles Conrad
Julie Kay Bush
Merlyn Gerard Flom
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Lilly Co Eli
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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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/12—Materials from mammals; Compositions comprising non-specified tissues or cells; Compositions comprising non-embryonic stem cells; Genetically modified cells
    • A61K35/22—Urine; Urinary tract, e.g. kidney or bladder; Intraglomerular mesangial cells; Renal mesenchymal cells; Adrenal gland
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • 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
    • 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
    • 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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  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
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  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Reproductive Health (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biotechnology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
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  • Developmental Biology & Embryology (AREA)
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DK200001150A 1999-07-29 2000-07-28 Ny krystallinsk form af 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophen hydrochlorid, anvendelse heraf i lægemiddelformuleringer, samt fremgangsmåde til fremstilling heraf DK176771B1 (da)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US14618499P 1999-07-29 1999-07-29
US14618499 1999-07-29
US14764299P 1999-08-06 1999-08-06
US14764299 1999-08-06
US14982099P 1999-08-19 1999-08-19
US14982099 1999-08-19

Publications (2)

Publication Number Publication Date
DK200001150A DK200001150A (da) 2001-01-30
DK176771B1 true DK176771B1 (da) 2009-08-03

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DK200001150A DK176771B1 (da) 1999-07-29 2000-07-28 Ny krystallinsk form af 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophen hydrochlorid, anvendelse heraf i lægemiddelformuleringer, samt fremgangsmåde til fremstilling heraf

Country Status (45)

Country Link
EP (1) EP1204655B1 (de)
JP (1) JP2001048880A (de)
KR (1) KR100733094B1 (de)
CN (1) CN1138771C (de)
AR (1) AR029176A1 (de)
AT (2) ATE251151T1 (de)
AU (2) AU6335500A (de)
BE (1) BE1013410A3 (de)
BR (1) BR0003211A (de)
CA (1) CA2314685C (de)
CO (1) CO5180572A1 (de)
CZ (1) CZ300356B6 (de)
DE (2) DE60005693T2 (de)
DK (1) DK176771B1 (de)
EG (1) EG24196A (de)
ES (1) ES2208384T3 (de)
FI (1) FI20001721A (de)
FR (1) FR2798384B1 (de)
GB (1) GB2352716A (de)
GR (1) GR20000100264A (de)
HK (1) HK1034962A1 (de)
HR (1) HRP20000502B1 (de)
HU (1) HUP0003005A2 (de)
ID (1) ID26679A (de)
IL (1) IL137552A (de)
IT (1) IT1318659B1 (de)
LT (1) LT4789B (de)
LU (1) LU90616B1 (de)
LV (1) LV12733B (de)
MD (1) MD2335G2 (de)
MX (1) MXPA00007462A (de)
MY (1) MY120393A (de)
NL (1) NL1015822C2 (de)
NO (1) NO325594B1 (de)
NZ (1) NZ506045A (de)
PE (1) PE20010383A1 (de)
PL (1) PL341748A1 (de)
PT (1) PT102501A (de)
SE (1) SE0002793L (de)
SG (1) SG90737A1 (de)
SI (1) SI20427B (de)
SV (1) SV2002000134A (de)
TR (1) TR200002205A2 (de)
TW (1) TWI271403B (de)
WO (1) WO2001009115A2 (de)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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 (de) * 2000-05-08 2009-07-15 Eli Lilly & Company Stabilisierte Formulierungen von 6-Hydroxy-3-(4-[2-(Piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophen und deren Salze
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
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
MXPA03003432A (es) * 2000-10-20 2003-08-07 Lilly Co Eli Nueva forma cristalina de clorhidrato de 6-hidroxi -3-(4 -(2 -(piperidin-1- il)etoxi)fenoxi) -2-(4-metoxifenil) benzo (b) tiofeno.
WO2002042289A2 (en) 2000-11-27 2002-05-30 Eli Lilly And Company Process for preparing 3-aryl-benzo[b]thiophenes
US7834187B2 (en) * 2004-07-22 2010-11-16 Eli Lilly And Company Crystalline variable hydrate of (S)-6-(4-(2-((3-9H-carbazol-4-yloxy)-2-hydroxypropyl)amino)-2-methylpropyl)phenoxy)-3-pyridinecarbox amide hemisuccinate salt
EP2425846A1 (de) * 2004-12-23 2012-03-07 Voyager Pharmaceutical Corporation Acetylcholinesterasehemmer und Leuprolidacetat zur Behandlung von Alzheimer-Krankheit
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

Family Cites Families (4)

* 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
IL132952A (en) * 1995-02-28 2002-02-10 Lilly Co Eli Derivatives of benzothiophene
ZA982877B (en) * 1997-04-09 1999-10-04 Lilly Co Eli Treatment of central nervous system disorders with selective estrogen receptor modulators.
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

Also Published As

Publication number Publication date
EP1204655A2 (de) 2002-05-15
LV12733A (lv) 2001-10-20
IL137552A (en) 2009-06-15
LV12733B (lv) 2002-02-20
ITMI20001758A0 (it) 2000-07-28
AU4891100A (en) 2001-02-01
IT1318659B1 (it) 2003-08-27
MY120393A (en) 2005-10-31
FR2798384A1 (fr) 2001-03-16
ITMI20001758A1 (it) 2002-01-28
HRP20000502B1 (en) 2008-04-30
SG90737A1 (en) 2002-08-20
NL1015822C2 (nl) 2004-08-04
AU6335500A (en) 2001-02-19
PE20010383A1 (es) 2001-04-05
ES2208384T3 (es) 2004-06-16
FR2798384B1 (fr) 2004-09-24
IE20000604A1 (en) 2001-04-04
DK200001150A (da) 2001-01-30
AR029176A1 (es) 2003-06-18
SV2002000134A (es) 2002-06-07
MD2335F2 (en) 2003-12-31
LT2000075A (lt) 2001-02-26
FI20001721A0 (fi) 2000-07-28
SI20427B (sl) 2009-04-30
CZ20002717A3 (en) 2001-05-16
NO325594B1 (no) 2008-06-23
PT102501A (pt) 2001-01-31
WO2001009115A2 (en) 2001-02-08
FI20001721A (fi) 2001-01-30
SI20427A (sl) 2001-06-30
HUP0003005A2 (hu) 2002-04-29
PL341748A1 (en) 2001-02-12
DE60005693D1 (de) 2003-11-06
LT4789B (lt) 2001-05-25
CN1138771C (zh) 2004-02-18
MD2335G2 (ro) 2004-06-30
ATE251151T1 (de) 2003-10-15
KR100733094B1 (ko) 2007-06-27
NO20003876D0 (no) 2000-07-28
GR20000100264A (el) 2001-03-30
MD20000161A (en) 2001-04-30
WO2001009115A3 (en) 2001-08-16
BR0003211A (pt) 2001-03-13
TWI271403B (en) 2007-01-21
IL137552A0 (en) 2001-07-24
CA2314685A1 (en) 2001-01-29
DE60005693T2 (de) 2004-07-29
SE0002793L (sv) 2001-01-30
EP1204655B1 (de) 2003-10-01
HK1034962A1 (en) 2001-11-09
MXPA00007462A (es) 2002-06-04
KR20010049911A (ko) 2001-06-15
CA2314685C (en) 2009-10-20
CO5180572A1 (es) 2002-07-30
NL1015822A1 (nl) 2001-01-30
NZ506045A (en) 2002-02-01
SE0002793D0 (sv) 2000-07-28
DE10036855A1 (de) 2001-03-22
NO20003876L (no) 2001-01-30
LU90616B1 (fr) 2007-06-08
GB0018636D0 (en) 2000-09-13
AT502317A1 (de) 2007-02-15
AU779559B2 (en) 2005-01-27
CZ300356B6 (cs) 2009-04-29
HRP20000502A2 (en) 2001-06-30
TR200002205A2 (tr) 2001-03-21
GB2352716A (en) 2001-02-07
CN1283622A (zh) 2001-02-14
BE1013410A3 (fr) 2001-12-04
HU0003005D0 (en) 2000-10-28
EG24196A (en) 2008-10-14
JP2001048880A (ja) 2001-02-20
ID26679A (id) 2001-02-01

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