ATE251151T1 - Eine kristalline form von 6-hydroxy-3-(4-(2- (piperidin-1-yl)ethoxy)phenoxy)-2-(4- methoxyphenyl)benzo(b)thiophen-hydrochlorid - Google Patents

Eine kristalline form von 6-hydroxy-3-(4-(2- (piperidin-1-yl)ethoxy)phenoxy)-2-(4- methoxyphenyl)benzo(b)thiophen-hydrochlorid

Info

Publication number
ATE251151T1
ATE251151T1 AT00950222T AT00950222T ATE251151T1 AT E251151 T1 ATE251151 T1 AT E251151T1 AT 00950222 T AT00950222 T AT 00950222T AT 00950222 T AT00950222 T AT 00950222T AT E251151 T1 ATE251151 T1 AT E251151T1
Authority
AT
Austria
Prior art keywords
piperidin
benzo
methoxyphenyl
phenoxy
ethoxy
Prior art date
Application number
AT00950222T
Other languages
English (en)
Inventor
Julie Kay Bush
Preston Charles Conrad
Merlyn Gerard Flom
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
Application granted granted Critical
Publication of ATE251151T1 publication Critical patent/ATE251151T1/de

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Classifications

    • 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
    • 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
    • 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
AT00950222T 1999-07-29 2000-07-17 Eine kristalline form von 6-hydroxy-3-(4-(2- (piperidin-1-yl)ethoxy)phenoxy)-2-(4- methoxyphenyl)benzo(b)thiophen-hydrochlorid ATE251151T1 (de)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US14618499P 1999-07-29 1999-07-29
US14764299P 1999-08-06 1999-08-06
US14982099P 1999-08-19 1999-08-19
PCT/US2000/016332 WO2001009115A2 (en) 1999-07-29 2000-07-17 A NOVEL CRYSTALLINE FORM OF 6-HYDROXY-3- (4-[2-(PIPERIDIN-1- YL)ETHOXY] PHENOXY)-2- (4-METHOXYPHENYL) BENZO[b]THIOPHENE HYDROCHLORIDE

Publications (1)

Publication Number Publication Date
ATE251151T1 true ATE251151T1 (de) 2003-10-15

Family

ID=27386367

Family Applications (2)

Application Number Title Priority Date Filing Date
AT00950222T ATE251151T1 (de) 1999-07-29 2000-07-17 Eine kristalline form von 6-hydroxy-3-(4-(2- (piperidin-1-yl)ethoxy)phenoxy)-2-(4- methoxyphenyl)benzo(b)thiophen-hydrochlorid
AT0132300A AT502317A1 (de) 1999-07-29 2000-07-28 Neue kristalline form von 6-hydroxy-3-(4-(2-(piperidin-l-yl) ethoxy)phenoxy)-2-(4-methoxyphenyl) benzo(b)thiophen-hydrochlorid, verfahren zu deren herstellung, deren verwendung und pharmazeutische mittel

Family Applications After (1)

Application Number Title Priority Date Filing Date
AT0132300A AT502317A1 (de) 1999-07-29 2000-07-28 Neue kristalline form von 6-hydroxy-3-(4-(2-(piperidin-l-yl) ethoxy)phenoxy)-2-(4-methoxyphenyl) benzo(b)thiophen-hydrochlorid, verfahren zu deren herstellung, deren verwendung und pharmazeutische mittel

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
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
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
UA77941C2 (en) * 2000-05-08 2007-02-15 Lilly Co Eli Stabilized pharmaceutical formulations containing 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo(?)thiophene or a salt 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
JP2004512333A (ja) * 2000-10-20 2004-04-22 イーライ・リリー・アンド・カンパニー 新規な結晶形の６−ヒドロキシ−３−（４−［２−（ピペリジン−１−イル）エトキシ］フェノキシ）−２−（４−メトキシフェニル）ベンゾ［ｂ］チオフェン塩酸塩
US6921827B2 (en) 2000-11-27 2005-07-26 Eli Lilly And Company Process for preparing 3-aryl-benzo{b} thiophenes
AU2005275185B2 (en) * 2004-07-22 2011-06-23 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-pyridinecarbox amide hemisuccinate salt
EP2425846A1 (de) * 2004-12-23 2012-03-07 Voyager Pharmaceutical Corporation Acetylcholinesterasehemmer und Leuprolidacetat zur Behandlung von Alzheimer-Krankheit
US20090137632A1 (en) * 2005-02-11 2009-05-28 Erwin M Johnston 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
PT729956E (pt) * 1995-02-28 2002-03-28 Lilly Co Eli Compostos intermediarios formulacoes e metodos de benzotiofeno
ZA982877B (en) * 1997-04-09 1999-10-04 Lilly Co Eli Treatment of central nervous system disorders with selective estrogen receptor modulators.
AU6335600A (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

Also Published As

Publication number Publication date
BE1013410A3 (fr) 2001-12-04
HU0003005D0 (en) 2000-10-28
EP1204655A2 (de) 2002-05-15
CA2314685A1 (en) 2001-01-29
EG24196A (en) 2008-10-14
AU6335500A (en) 2001-02-19
CZ20002717A3 (en) 2001-05-16
FI20001721A (fi) 2001-01-30
SI20427A (sl) 2001-06-30
GB0018636D0 (en) 2000-09-13
DK200001150A (da) 2001-01-30
LT2000075A (lt) 2001-02-26
EP1204655B1 (de) 2003-10-01
MXPA00007462A (es) 2002-06-04
AR029176A1 (es) 2003-06-18
SI20427B (sl) 2009-04-30
PL341748A1 (en) 2001-02-12
ITMI20001758A1 (it) 2002-01-28
SE0002793L (sv) 2001-01-30
HRP20000502B1 (en) 2008-04-30
CN1138771C (zh) 2004-02-18
DK176771B1 (da) 2009-08-03
PT102501A (pt) 2001-01-31
JP2001048880A (ja) 2001-02-20
SE0002793D0 (sv) 2000-07-28
NL1015822C2 (nl) 2004-08-04
KR20010049911A (ko) 2001-06-15
CN1283622A (zh) 2001-02-14
HK1034962A1 (en) 2001-11-09
GR20000100264A (el) 2001-03-30
DE10036855A1 (de) 2001-03-22
LV12733B (lv) 2002-02-20
WO2001009115A2 (en) 2001-02-08
SV2002000134A (es) 2002-06-07
IE20000604A1 (en) 2001-04-04
ID26679A (id) 2001-02-01
ITMI20001758A0 (it) 2000-07-28
HUP0003005A2 (hu) 2002-04-29
MD2335G2 (ro) 2004-06-30
NL1015822A1 (nl) 2001-01-30
HRP20000502A2 (en) 2001-06-30
KR100733094B1 (ko) 2007-06-27
MD2335F2 (en) 2003-12-31
LU90616B1 (fr) 2007-06-08
TR200002205A2 (tr) 2001-03-21
CA2314685C (en) 2009-10-20
MY120393A (en) 2005-10-31
IT1318659B1 (it) 2003-08-27
MD20000161A (en) 2001-04-30
LV12733A (lv) 2001-10-20
AU4891100A (en) 2001-02-01
FR2798384A1 (fr) 2001-03-16
NO20003876D0 (no) 2000-07-28
FI20001721A0 (fi) 2000-07-28
NO325594B1 (no) 2008-06-23
SG90737A1 (en) 2002-08-20
FR2798384B1 (fr) 2004-09-24
DE60005693T2 (de) 2004-07-29
CO5180572A1 (es) 2002-07-30
AU779559B2 (en) 2005-01-27
GB2352716A (en) 2001-02-07
LT4789B (lt) 2001-05-25
AT502317A1 (de) 2007-02-15
BR0003211A (pt) 2001-03-13
DE60005693D1 (de) 2003-11-06
CZ300356B6 (cs) 2009-04-29
TWI271403B (en) 2007-01-21
NO20003876L (no) 2001-01-30
IL137552A (en) 2009-06-15
ES2208384T3 (es) 2004-06-16
IL137552A0 (en) 2001-07-24
PE20010383A1 (es) 2001-04-05
WO2001009115A3 (en) 2001-08-16
NZ506045A (en) 2002-02-01

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