GB2352717A - Crystalline form of arzoxifene - Google Patents

Crystalline form of arzoxifene Download PDF

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Publication number
GB2352717A
GB2352717A GB0018641A GB0018641A GB2352717A GB 2352717 A GB2352717 A GB 2352717A GB 0018641 A GB0018641 A GB 0018641A GB 0018641 A GB0018641 A GB 0018641A GB 2352717 A GB2352717 A GB 2352717A
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GB
United Kingdom
Prior art keywords
formulation
estrogen
cancer
excipients
diluents
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
GB0018641A
Other languages
English (en)
Other versions
GB0018641D0 (en
Inventor
Julie Kay Bush
Preston Charles Conrad
Merlyn Gerard Flom
Wayne Douglas Luke
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of GB0018641D0 publication Critical patent/GB0018641D0/en
Publication of GB2352717A publication Critical patent/GB2352717A/en
Withdrawn legal-status Critical Current

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Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • 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)
GB0018641A 1999-07-29 2000-07-28 Crystalline form of arzoxifene Withdrawn GB2352717A (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 (2)

Publication Number Publication Date
GB0018641D0 GB0018641D0 (en) 2000-09-13
GB2352717A true GB2352717A (en) 2001-02-07

Family

ID=27386379

Family Applications (1)

Application Number Title Priority Date Filing Date
GB0018641A Withdrawn GB2352717A (en) 1999-07-29 2000-07-28 Crystalline form of arzoxifene

Country Status (45)

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

Families Citing this family (9)

* Cited by examiner, † Cited by third party
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
BR0110620A (pt) * 2000-05-08 2003-04-01 Lilly Co Eli Formulações estabilizadas de 6-hidróxi-3-(4-[2-(piperidin-1-il)etóxi]fenóxi)-2-(4-metoxi fenil)benzo[b]tiofeno e de sais do mesmo
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
KR20030037690A (ko) * 2000-10-20 2003-05-14 일라이 릴리 앤드 캄파니 6-히드록시-3-(4-[2-(피페리딘-1-일)에톡시]페녹시)-2-(4-메톡시페닐)벤조[ｂ]티오펜 히드로클로라이드의 신규 결정형
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
PL1773811T3 (pl) * 2004-07-22 2011-02-28 Lilly Co Eli Krystaliczny zmienny hydrat soli hemibursztynianowej (s)-6-(4-(2-((3(9h-karbazol-4-iloksy)-2-hydroksypropylo)amino)-2-metylopropylo)fenoksy)-3-pirydynokarboksy amidu

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5723474A (en) * 1995-02-28 1998-03-03 Eli Lilly And Company Benzothiophene compounds, intermediates, compositions, and methods

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE44597A1 (es) * 1995-02-28 1997-10-13 Lilly Co Eli Compuestos de benzotiofeno, productos intermedios, composiciones y procedimientos
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.

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5723474A (en) * 1995-02-28 1998-03-03 Eli Lilly And Company Benzothiophene compounds, intermediates, compositions, and methods

Also Published As

Publication number Publication date
FI20001722A (fi) 2001-01-30
DE10036854A1 (de) 2001-03-01
AU6335600A (en) 2001-02-19
TWI276437B (en) 2007-03-21
DZ3060A1 (fr) 2004-05-22
NO20003879D0 (no) 2000-07-28
CN1288007A (zh) 2001-03-21
NL1015821C2 (nl) 2002-01-03
LV12623B (en) 2001-07-20
DK200001151A (da) 2001-01-30
NO20003879L (no) 2001-01-30
SE0002792L (sv) 2001-01-30
HRP20000503B1 (en) 2008-04-30
IT1318660B1 (it) 2003-08-27
ITMI20001759A0 (it) 2000-07-28
PL341749A1 (en) 2001-02-12
HK1035370A1 (en) 2001-11-23
CZ20002716A3 (en) 2001-05-16
CN1138770C (zh) 2004-02-18
AR031073A1 (es) 2003-09-10
IE20000605A1 (en) 2001-04-04
BR0003209A (pt) 2001-03-20
SI20426A (sl) 2001-06-30
GB0018641D0 (en) 2000-09-13
RO121851B1 (ro) 2008-06-30
CZ299311B6 (cs) 2008-06-18
FR2796944A1 (fr) 2001-02-02
ID27078A (id) 2001-02-22
UA72885C2 (uk) 2005-05-16
LT2000076A (lt) 2001-02-26
MY128764A (en) 2007-02-28
CA2314682A1 (en) 2001-01-29
HRP20000503A2 (en) 2001-06-30
JP2001064277A (ja) 2001-03-13
KR100697177B1 (ko) 2007-03-21
HUP0003001A2 (hu) 2002-04-29
IL137553A (en) 2005-09-25
IL137553A0 (en) 2001-07-24
PE20010385A1 (es) 2001-04-06
SE0002792D0 (sv) 2000-07-28
MD2336F2 (en) 2003-12-31
WO2001009116A2 (en) 2001-02-08
FR2796944B1 (fr) 2003-01-31
WO2001009116A3 (en) 2001-05-17
GR1004084B (el) 2002-12-11
EP1204656A2 (en) 2002-05-15
BE1013411A3 (fr) 2001-12-04
FI20001722A0 (fi) 2000-07-28
LT4790B (lt) 2001-05-25
LU90617B1 (fr) 2001-06-15
MD2336G2 (ro) 2004-06-30
MD20000162A (en) 2001-04-30
LV12623A (en) 2001-03-20
SG91296A1 (en) 2002-09-17
AT502318A1 (de) 2007-02-15
HU0003001D0 (en) 2000-10-28
KR20010049916A (ko) 2001-06-15
PT102502A (pt) 2001-01-31
ITMI20001759A1 (it) 2002-01-28
TR200002206A2 (tr) 2001-03-21
MXPA00007461A (es) 2004-07-16
GR20000100265A (el) 2001-03-30
NL1015821A1 (nl) 2001-01-30
CO5180570A1 (es) 2002-07-30
SV2002000132A (es) 2002-06-07

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