UA72885C2 - CRYSTALLINE 6-HYDROXY-3-(4-[2-(PIPERIDINE-1-YL)ETHOXY]PHENOXY)-2-(4-METHOXYPHENYL)BENZO[b]THIOPHENE HYDROCHLORIDE AND METHOD FOR PRODUCING THE SAME, ACTIVE INGREDIENT AND PHARMACEUTICAL COMPOSITION - Google Patents

CRYSTALLINE 6-HYDROXY-3-(4-[2-(PIPERIDINE-1-YL)ETHOXY]PHENOXY)-2-(4-METHOXYPHENYL)BENZO[b]THIOPHENE HYDROCHLORIDE AND METHOD FOR PRODUCING THE SAME, ACTIVE INGREDIENT AND PHARMACEUTICAL COMPOSITION

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Publication number
UA72885C2
UA72885C2 UA2000074563A UA200074563A UA72885C2 UA 72885 C2 UA72885 C2 UA 72885C2 UA 2000074563 A UA2000074563 A UA 2000074563A UA 200074563 A UA200074563 A UA 200074563A UA 72885 C2 UA72885 C2 UA 72885C2
Authority
UA
Ukraine
Prior art keywords
benzo
methoxyphenyl
phenoxy
ethoxy
hydroxy
Prior art date
Application number
UA2000074563A
Other languages
Russian (ru)
Ukrainian (uk)
Inventor
Джулі Кей Буш
Джули Кей Буш
Престон Чарлз КОНРАД
Мерлін Джерард Флом
Уейн Дуглас ЛЮК
Уэйн Дуглас Люк
Original Assignee
Елі Ліллі Енд Компані
Эли Лилли Энд Компани
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 Елі Ліллі Енд Компані, Эли Лилли Энд Компани filed Critical Елі Ліллі Енд Компані
Publication of UA72885C2 publication Critical patent/UA72885C2/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62Benzo[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
    • C07D333/64Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • A61K31/567Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08Peptides having 5 to 11 amino acids
    • A61K38/09Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32Antioestrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (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)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Reproductive Health (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • 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

The present invention is directed to a novel crystalline hydrate of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene hydrochloride and uses for same, including inhibition of disease states associated with estrogen deprivation including cardiovascular disease, hyperlipidemia, and osteoporosis; and inhibition of other pathological conditions such as endometriosis, uterine fibrosis, estrogen-dependent cancer (including breast and uterine cancer), prostate cancer, benign prostatic hyperplasia, CNS disorders including Alzheimer's disease, prevention of breast cancer, and up-regulating ChAT.
UA2000074563A 1999-07-29 2000-07-28 CRYSTALLINE 6-HYDROXY-3-(4-[2-(PIPERIDINE-1-YL)ETHOXY]PHENOXY)-2-(4-METHOXYPHENYL)BENZO[b]THIOPHENE HYDROCHLORIDE AND METHOD FOR PRODUCING THE SAME, ACTIVE INGREDIENT AND PHARMACEUTICAL COMPOSITION UA72885C2 (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
UA72885C2 true UA72885C2 (en) 2005-05-16

Family

ID=27386379

Family Applications (1)

Application Number Title Priority Date Filing Date
UA2000074563A UA72885C2 (en) 1999-07-29 2000-07-28 CRYSTALLINE 6-HYDROXY-3-(4-[2-(PIPERIDINE-1-YL)ETHOXY]PHENOXY)-2-(4-METHOXYPHENYL)BENZO[b]THIOPHENE HYDROCHLORIDE AND METHOD FOR PRODUCING THE SAME, ACTIVE INGREDIENT AND PHARMACEUTICAL COMPOSITION

Country Status (45)

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) FI20001722A (en)
FR (1) FR2796944B1 (en)
GB (1) GB2352717A (en)
GR (1) GR1004084B (en)
HK (1) HK1035370A1 (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
DE60005693T2 (en) * 1999-07-29 2004-07-29 Eli Lilly And Co., Indianapolis A CRYSTALLINE FORM OF 6-HYDROXY-3- (4- [2- (PIPERIDIN-1-YL) ETHOXY] PHENOXY) -2- (4-METHOXYPHENYL) BENZO [B] THIOPHENE HYDROCHLORIDE
HUP0302190A3 (en) * 2000-05-08 2009-03-30 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 & 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
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
CZ20031098A3 (en) * 2000-10-20 2003-08-13 Eli Lilly And Company Novel crystalline form of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene hydrochloride
AU2002230409A1 (en) 2000-11-27 2002-06-03 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
DK1773811T3 (en) * 2004-07-22 2010-12-13 Lilly Co Eli Crystalline variable hydrate of (s) -6- (4- (2 - ((3- (9H-carbazol-4-yloxy) -2-hydroxypropyl) amine) -2-methylpropyl) phenoxy) -3-pyridinecarboxamide hemisuccinate salt

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
SG90193A1 (en) * 1995-02-28 2002-07-23 Lilly Co Eli Benzothiophene compounds, intermediates, compositions, and methods
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
AU6335600A (en) 2001-02-19
CZ20002716A3 (en) 2001-05-16
HK1035370A1 (en) 2001-11-23
DE10036854A1 (en) 2001-03-01
MXPA00007461A (en) 2004-07-16
ITMI20001759A0 (en) 2000-07-28
CN1288007A (en) 2001-03-21
IL137553A0 (en) 2001-07-24
MD2336G2 (en) 2004-06-30
CO5180570A1 (en) 2002-07-30
PT102502A (en) 2001-01-31
FR2796944A1 (en) 2001-02-02
HRP20000503A2 (en) 2001-06-30
HUP0003001A2 (en) 2002-04-29
MY128764A (en) 2007-02-28
WO2001009116A2 (en) 2001-02-08
SE0002792D0 (en) 2000-07-28
LV12623B (en) 2001-07-20
FI20001722A0 (en) 2000-07-28
NL1015821A1 (en) 2001-01-30
FR2796944B1 (en) 2003-01-31
NO20003879D0 (en) 2000-07-28
LV12623A (en) 2001-03-20
BR0003209A (en) 2001-03-20
SI20426A (en) 2001-06-30
HRP20000503B1 (en) 2008-04-30
BE1013411A3 (en) 2001-12-04
SE0002792L (en) 2001-01-30
LT4790B (en) 2001-05-25
CN1138770C (en) 2004-02-18
CZ299311B6 (en) 2008-06-18
DZ3060A1 (en) 2004-05-22
DK200001151A (en) 2001-01-30
TWI276437B (en) 2007-03-21
JP2001064277A (en) 2001-03-13
CA2314682A1 (en) 2001-01-29
RO121851B1 (en) 2008-06-30
FI20001722A (en) 2001-01-30
LT2000076A (en) 2001-02-26
ID27078A (en) 2001-02-22
IL137553A (en) 2005-09-25
MD20000162A (en) 2001-04-30
NO20003879L (en) 2001-01-30
TR200002206A2 (en) 2001-03-21
SG91296A1 (en) 2002-09-17
AT502318A1 (en) 2007-02-15
LU90617B1 (en) 2001-06-15
IE20000605A1 (en) 2001-04-04
SV2002000132A (en) 2002-06-07
AR031073A1 (en) 2003-09-10
GB2352717A (en) 2001-02-07
NL1015821C2 (en) 2002-01-03
ITMI20001759A1 (en) 2002-01-28
GR20000100265A (en) 2001-03-30
KR100697177B1 (en) 2007-03-21
EP1204656A2 (en) 2002-05-15
IT1318660B1 (en) 2003-08-27
MD2336F2 (en) 2003-12-31
WO2001009116A3 (en) 2001-05-17
GR1004084B (en) 2002-12-11
GB0018641D0 (en) 2000-09-13
KR20010049916A (en) 2001-06-15
HU0003001D0 (en) 2000-10-28
PL341749A1 (en) 2001-02-12
PE20010385A1 (en) 2001-04-06

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