FR2796944B1 - NOUVELLE FORME CRISTALLINE DU CHLORHYDRATE DE 6-HYDROXY-3- (4-[2-(PIPERIDIN-1-YL)ETHOXY]PHENOXY)-2-(4-METHOXYPHENYL) BENZO[b]THIOPHENE - Google Patents

NOUVELLE FORME CRISTALLINE DU CHLORHYDRATE DE 6-HYDROXY-3- (4-[2-(PIPERIDIN-1-YL)ETHOXY]PHENOXY)-2-(4-METHOXYPHENYL) BENZO[b]THIOPHENE

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Publication number
FR2796944B1
FR2796944B1 FR0009969A FR0009969A FR2796944B1 FR 2796944 B1 FR2796944 B1 FR 2796944B1 FR 0009969 A FR0009969 A FR 0009969A FR 0009969 A FR0009969 A FR 0009969A FR 2796944 B1 FR2796944 B1 FR 2796944B1
Authority
FR
France
Prior art keywords
chlorhydrate
piperidin
thiophene
benzo
methoxyphenyl
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.)
Expired - Fee Related
Application number
FR0009969A
Other languages
English (en)
Other versions
FR2796944A1 (fr
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 FR2796944A1 publication Critical patent/FR2796944A1/fr
Application granted granted Critical
Publication of FR2796944B1 publication Critical patent/FR2796944B1/fr
Anticipated expiration legal-status Critical
Expired - Fee Related 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Reproductive Health (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (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)
FR0009969A 1999-07-29 2000-07-28 NOUVELLE FORME CRISTALLINE DU CHLORHYDRATE DE 6-HYDROXY-3- (4-[2-(PIPERIDIN-1-YL)ETHOXY]PHENOXY)-2-(4-METHOXYPHENYL) BENZO[b]THIOPHENE Expired - Fee Related FR2796944B1 (fr)

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
FR2796944A1 FR2796944A1 (fr) 2001-02-02
FR2796944B1 true FR2796944B1 (fr) 2003-01-31

Family

ID=27386379

Family Applications (1)

Application Number Title Priority Date Filing Date
FR0009969A Expired - Fee Related FR2796944B1 (fr) 1999-07-29 2000-07-28 NOUVELLE FORME CRISTALLINE DU CHLORHYDRATE DE 6-HYDROXY-3- (4-[2-(PIPERIDIN-1-YL)ETHOXY]PHENOXY)-2-(4-METHOXYPHENYL) BENZO[b]THIOPHENE

Country Status (45)

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

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 (fr) * 2000-05-08 2009-07-15 Eli Lilly & Company Formulations stabilisées de 6-hydroxy-3-(4- 2-(pipéridin-1-yl)éthoxyphénoxy)-2-(4-methoxyphényl) benzo(b)thiophène et sels de ces composés
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 (fr) * 2000-05-23 2001-11-28 JENAPHARM GmbH Nouveaux formes solides du mesoprogestin 11beta-(4E-(hxdroxyiminomethyl)-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 (fr) * 2002-07-12 2010-09-14 Eli Lilly And Company Monochlorhydrate de 3-(1-methyl-1h-indol-3-yl)-4-[[1-(pyridin-2-ylmethyl)piperidin-4-yl]-1h-indol-3-yl]-1h-pyrrole-2,5-dione cristallin
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.

Family Cites Families (4)

* 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
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
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
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 (fr) 2001-01-29
MXPA00007461A (es) 2004-07-16
HUP0003001A2 (hu) 2002-04-29
NL1015821C2 (nl) 2002-01-03
LV12623B (en) 2001-07-20
AR031073A1 (es) 2003-09-10
WO2001009116A2 (fr) 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
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 (fr) 2001-05-17
TWI276437B (en) 2007-03-21
HU0003001D0 (en) 2000-10-28
DZ3060A1 (fr) 2004-05-22
GR1004084B (el) 2002-12-11
EP1204656A2 (fr) 2002-05-15
RO121851B1 (ro) 2008-06-30

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