AR029176A1 - Una nueva forma cristalina del clorhidrato de 6-hidroxi-3-(4-[2-(piperidin-1-il) etoxi] fenoxi)-2-(4-metoxifenil) benzo [b] tiofeno aplicables en la inhibicion, entre otros, de estados patologicos asociados con la reduccion de los niveles plasmaticos de estrogenos y composicion farmaceutica que comp - Google Patents

Una nueva forma cristalina del clorhidrato de 6-hidroxi-3-(4-[2-(piperidin-1-il) etoxi] fenoxi)-2-(4-metoxifenil) benzo [b] tiofeno aplicables en la inhibicion, entre otros, de estados patologicos asociados con la reduccion de los niveles plasmaticos de estrogenos y composicion farmaceutica que comp

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Publication number
AR029176A1
AR029176A1 ARP000103929A ARP000103929A AR029176A1 AR 029176 A1 AR029176 A1 AR 029176A1 AR P000103929 A ARP000103929 A AR P000103929A AR P000103929 A ARP000103929 A AR P000103929A AR 029176 A1 AR029176 A1 AR 029176A1
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AR
Argentina
Prior art keywords
inhibition
piperidin
states associated
strogens
phenoxi
Prior art date
Application number
ARP000103929A
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English (en)
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.)
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Publication date
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of AR029176A1 publication Critical patent/AR029176A1/es

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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
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    • 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
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    • 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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Abstract

Se describe y reivindica un nuevo hidrato cristalino del clorhidrato de 6-hidroxi-3-(4-[2-(piperidin-1-il) etoxi]-fenoxi)-2-(4-metoxifenil) benzo[b] tiofeno y a usos para el mismo, incluyendo la inhibicion de estados de enfermedad asociados con la privacion de estrogenos que incluyen enfermedades cardiovasculares, hiperlipidemia y osteoporosis; y la inhibicion de otros trastornos patologicos tales como la endometriosis, la fibrosis uterina, el cáncer dependiente de estrogenos (incluyendo el cáncer de mama y uterino), cáncer de prostata, la hiperplasia prostática benigna, trastornos del SNC que incluyen la enfermedad de Alzheimer, prevencion del cáncer de mama y regulacion positiva de la ChAT. Dicho hidrato cristalino posee un diagrama de difraccion RX que comprende los siguientes picos: 4,6 +- 0,2; 7,8 +- 0,2; 9,3 +- 0,2; 14,0 +- 0,2; 17,6 +- 0,2; 20,8 +- 0,2 y 24,3 +- 0,2 degree en 2 theta; cuando se obtiene a 25 +- 2 degree C y con una humedad relativa del 35 +- 10% (HR) a partir de una fuente de radiacion de cobre.
ARP000103929A 1999-07-29 2000-07-28 Una nueva forma cristalina del clorhidrato de 6-hidroxi-3-(4-[2-(piperidin-1-il) etoxi] fenoxi)-2-(4-metoxifenil) benzo [b] tiofeno aplicables en la inhibicion, entre otros, de estados patologicos asociados con la reduccion de los niveles plasmaticos de estrogenos y composicion farmaceutica que comp AR029176A1 (es)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
AR029176A1 true AR029176A1 (es) 2003-06-18

Family

ID=27386367

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Application Number Title Priority Date Filing Date
ARP000103929A AR029176A1 (es) 1999-07-29 2000-07-28 Una nueva forma cristalina del clorhidrato de 6-hidroxi-3-(4-[2-(piperidin-1-il) etoxi] fenoxi)-2-(4-metoxifenil) benzo [b] tiofeno aplicables en la inhibicion, entre otros, de estados patologicos asociados con la reduccion de los niveles plasmaticos de estrogenos y composicion farmaceutica que comp

Country Status (45)

Country Link
EP (1) EP1204655B1 (es)
JP (1) JP2001048880A (es)
KR (1) KR100733094B1 (es)
CN (1) CN1138771C (es)
AR (1) AR029176A1 (es)
AT (2) ATE251151T1 (es)
AU (2) AU6335500A (es)
BE (1) BE1013410A3 (es)
BR (1) BR0003211A (es)
CA (1) CA2314685C (es)
CO (1) CO5180572A1 (es)
CZ (1) CZ300356B6 (es)
DE (2) DE60005693T2 (es)
DK (1) DK176771B1 (es)
EG (1) EG24196A (es)
ES (1) ES2208384T3 (es)
FI (1) FI20001721A (es)
FR (1) FR2798384B1 (es)
GB (1) GB2352716A (es)
GR (1) GR20000100264A (es)
HK (1) HK1034962A1 (es)
HR (1) HRP20000502B1 (es)
HU (1) HUP0003005A2 (es)
ID (1) ID26679A (es)
IL (1) IL137552A (es)
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LU (1) LU90616B1 (es)
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MD (1) MD2335G2 (es)
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NO (1) NO325594B1 (es)
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PL (1) PL341748A1 (es)
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SE (1) SE0002793L (es)
SG (1) SG90737A1 (es)
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WO (1) WO2001009115A2 (es)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001085147A2 (en) * 2000-05-08 2001-11-15 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
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
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
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
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.
CA2590997A1 (en) * 2004-12-23 2006-07-06 Voyager Pharmaceutical Corporation Leuprolide acetate and acetylcholinesterase inhibitors or nmda receptor antagonists for the treatment of alzheimer`s disease
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
PL182493B1 (pl) * 1995-02-28 2002-01-31 Lilly Co Eli Nowe pochodne benzotiofenu, nowe związki pośrednie i sposób wytwarzania nowych pochodnych benzotiofenu oraz środek farmaceutyczny
US5510357A (en) * 1995-02-28 1996-04-23 Eli Lilly And Company Benzothiophene compounds as anti-estrogenic agents
ZA982877B (en) * 1997-04-09 1999-10-04 Lilly Co Eli Treatment of central nervous system disorders with selective estrogen receptor modulators.
EP1204656A2 (en) * 1999-07-29 2002-05-15 Eli Lilly And Company A crystalline form of 6-hydroxy-3-(4-[2-(piperidin-1-yl) ethoxy] phenoxy)-2-(4-methoxyphenyl) benzo[b]thiophene hydrochloride

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CO5180572A1 (es) 2002-07-30
NZ506045A (en) 2002-02-01
LV12733A (lv) 2001-10-20
DK176771B1 (da) 2009-08-03
IL137552A0 (en) 2001-07-24
SV2002000134A (es) 2002-06-07
WO2001009115A3 (en) 2001-08-16
SI20427A (sl) 2001-06-30
DE60005693D1 (de) 2003-11-06
PE20010383A1 (es) 2001-04-05
ATE251151T1 (de) 2003-10-15
MY120393A (en) 2005-10-31
KR20010049911A (ko) 2001-06-15
HU0003005D0 (en) 2000-10-28
NO20003876L (no) 2001-01-30
SE0002793L (sv) 2001-01-30
NO325594B1 (no) 2008-06-23
IE20000604A1 (en) 2001-04-04
CZ20002717A3 (en) 2001-05-16
FR2798384B1 (fr) 2004-09-24
ITMI20001758A0 (it) 2000-07-28
CN1283622A (zh) 2001-02-14
BR0003211A (pt) 2001-03-13
MD2335F2 (en) 2003-12-31
LT4789B (lt) 2001-05-25
HRP20000502B1 (en) 2008-04-30
ITMI20001758A1 (it) 2002-01-28
AU4891100A (en) 2001-02-01
NO20003876D0 (no) 2000-07-28
AT502317A1 (de) 2007-02-15
EP1204655B1 (en) 2003-10-01
SE0002793D0 (sv) 2000-07-28
CA2314685C (en) 2009-10-20
FR2798384A1 (fr) 2001-03-16
PL341748A1 (en) 2001-02-12
SI20427B (sl) 2009-04-30
GR20000100264A (el) 2001-03-30
FI20001721A (fi) 2001-01-30
HUP0003005A2 (hu) 2002-04-29
NL1015822C2 (nl) 2004-08-04
EP1204655A2 (en) 2002-05-15
MD20000161A (en) 2001-04-30
LV12733B (lv) 2002-02-20
LU90616B1 (fr) 2007-06-08
TWI271403B (en) 2007-01-21
WO2001009115A2 (en) 2001-02-08
CN1138771C (zh) 2004-02-18
ID26679A (id) 2001-02-01
MXPA00007462A (es) 2002-06-04
AU6335500A (en) 2001-02-19
TR200002205A2 (tr) 2001-03-21
JP2001048880A (ja) 2001-02-20
GB0018636D0 (en) 2000-09-13
KR100733094B1 (ko) 2007-06-27
CA2314685A1 (en) 2001-01-29
DE60005693T2 (de) 2004-07-29
DK200001150A (da) 2001-01-30
IT1318659B1 (it) 2003-08-27
MD2335G2 (ro) 2004-06-30
IL137552A (en) 2009-06-15
PT102501A (pt) 2001-01-31
ES2208384T3 (es) 2004-06-16
HRP20000502A2 (en) 2001-06-30
CZ300356B6 (cs) 2009-04-29
BE1013410A3 (fr) 2001-12-04
FI20001721A0 (fi) 2000-07-28
GB2352716A (en) 2001-02-07
HK1034962A1 (en) 2001-11-09
AU779559B2 (en) 2005-01-27
DE10036855A1 (de) 2001-03-22
NL1015822A1 (nl) 2001-01-30
LT2000075A (lt) 2001-02-26
EG24196A (en) 2008-10-14
SG90737A1 (en) 2002-08-20

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