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AR031073A1 - A NEW CRYSTALLINE SHAPE OF 6-HYDROXI-3- (4- [2- (PIPERIDIN-1-IL) ETOXI) PHENOXI CHLORIDE HYDROXYIDE BENZO (B) THIOPHEN; PHARMACEUTICAL FORMULATIONS THAT INCLUDE SUCH CRYSTAL FORM; PROCEDURE TO PREPARE THE MENTIONED CRYSTAL FORM AND THE CRYSTAL FORM THAT IS OBTAINED WITH THE PRO - Google Patents

A NEW CRYSTALLINE SHAPE OF 6-HYDROXI-3- (4- [2- (PIPERIDIN-1-IL) ETOXI) PHENOXI CHLORIDE HYDROXYIDE BENZO (B) THIOPHEN; PHARMACEUTICAL FORMULATIONS THAT INCLUDE SUCH CRYSTAL FORM; PROCEDURE TO PREPARE THE MENTIONED CRYSTAL FORM AND THE CRYSTAL FORM THAT IS OBTAINED WITH THE PRO

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Publication number
AR031073A1
AR031073A1 ARP000103928A ARP000103928A AR031073A1 AR 031073 A1 AR031073 A1 AR 031073A1 AR P000103928 A ARP000103928 A AR P000103928A AR P000103928 A ARP000103928 A AR P000103928A AR 031073 A1 AR031073 A1 AR 031073A1
Authority
AR
Argentina
Prior art keywords
crystal form
piperidin
benzo
cancer
phenoxi
Prior art date
Application number
ARP000103928A
Other languages
Spanish (es)
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
Publication of AR031073A1 publication Critical patent/AR031073A1/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
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    • AHUMAN NECESSITIES
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    • 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
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Abstract

La presente invencion se refiere a un nuevo hidrato cristalino del clorhidrato de 6- hidroxi-3-(4-[2-(piperidin-1-il)etoxil]-fenoxi]-2-(4-metoxifenil)benzo[b]tiofeno que posee el siguiente diagrama de difraccion en Rx. que comprende los siguientes picos: 7,9 +- 0,2, 10,7 +- 0,2, 14,9 +- 0,2, 15,9 +- 0,2, 18,3 +- 0,2, y 20,6 +- 0,2s en 2c; cuando se obtiene a partir de una fuente de radiacion de cobre. La invencion comprende el uso de dicho compuesto, 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), el cáncer de prostata, la hiperplasia prostática benigna, trastornos del SNC que incluyen la enfermedad de Alzheimer, prevencion del cáncer mama y regulacion positiva de la ChAT. También se describen y reivindican los objetos restantes mencionados en el título.The present invention relates to a novel crystalline hydrate of 6- hydroxy-3- (4- [2- (piperidin-1-yl) ethoxy] -phenoxy] -2- (4-methoxyphenyl) benzo [b] thiophene hydrochloride which has the following diffraction diagram in Rx. comprising the following peaks: 7.9 + - 0.2, 10.7 + - 0.2, 14.9 + - 0.2, 15.9 + - 0, 2, 18.3 + - 0.2, and 20.6 + - 0.2s in 2c; when obtained from a source of copper radiation The invention comprises the use of said compound, including the inhibition of states of disease associated with estrogen deprivation that include cardiovascular disease, hyperlipidemia and osteoporosis; and the inhibition of other pathological disorders such as endometriosis, uterine fibrosis, estrogen-dependent cancer (including breast and uterine cancer), cancer of prostate, benign prostatic hyperplasia, CNS disorders that include Alzheimer's disease, prevention of breast cancer and positive regulation of ChAT. in and claim the remaining objects mentioned in the title.

ARP000103928A 1999-07-29 2000-07-28 A NEW CRYSTALLINE SHAPE OF 6-HYDROXI-3- (4- [2- (PIPERIDIN-1-IL) ETOXI) PHENOXI CHLORIDE HYDROXYIDE BENZO (B) THIOPHEN; PHARMACEUTICAL FORMULATIONS THAT INCLUDE SUCH CRYSTAL FORM; PROCEDURE TO PREPARE THE MENTIONED CRYSTAL FORM AND THE CRYSTAL FORM THAT IS OBTAINED WITH THE PRO AR031073A1 (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
AR031073A1 true AR031073A1 (en) 2003-09-10

Family

ID=27386379

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP000103928A AR031073A1 (en) 1999-07-29 2000-07-28 A NEW CRYSTALLINE SHAPE OF 6-HYDROXI-3- (4- [2- (PIPERIDIN-1-IL) ETOXI) PHENOXI CHLORIDE HYDROXYIDE BENZO (B) THIOPHEN; PHARMACEUTICAL FORMULATIONS THAT INCLUDE SUCH CRYSTAL FORM; PROCEDURE TO PREPARE THE MENTIONED CRYSTAL FORM AND THE CRYSTAL FORM THAT IS OBTAINED WITH THE PRO

Country Status (44)

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) FI20001722A7 (en)
FR (1) FR2796944B1 (en)
GB (1) GB2352717A (en)
GR (1) GR1004084B (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
AU6335500A (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
CA2408563A1 (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
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
CA2426007A1 (en) * 2000-10-20 2002-05-02 Eli Lilly And Company A 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
PT1773811E (en) * 2004-07-22 2010-10-19 Lilly Co Eli 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

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
JP3989569B2 (en) * 1995-02-28 2007-10-10 イーライ リリー アンド カンパニー 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.

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HUP0003001A2 (en) 2002-04-29
MD2336F2 (en) 2003-12-31
CA2314682A1 (en) 2001-01-29
ID27078A (en) 2001-02-22
SG91296A1 (en) 2002-09-17
FR2796944B1 (en) 2003-01-31
GR20000100265A (en) 2001-03-30
UA72885C2 (en) 2005-05-16
DE10036854A1 (en) 2001-03-01
PE20010385A1 (en) 2001-04-06
HK1035370A1 (en) 2001-11-23
NO20003879L (en) 2001-01-30
FI20001722A0 (en) 2000-07-28
NL1015821C2 (en) 2002-01-03
SV2002000132A (en) 2002-06-07
SE0002792L (en) 2001-01-30
IL137553A0 (en) 2001-07-24
AU6335600A (en) 2001-02-19
KR20010049916A (en) 2001-06-15
GR1004084B (en) 2002-12-11
MD2336G2 (en) 2004-06-30
JP2001064277A (en) 2001-03-13
LV12623B (en) 2001-07-20
CN1138770C (en) 2004-02-18
NO20003879D0 (en) 2000-07-28
CN1288007A (en) 2001-03-21
RO121851B1 (en) 2008-06-30
DK200001151A (en) 2001-01-30
MY128764A (en) 2007-02-28
HU0003001D0 (en) 2000-10-28
FI20001722L (en) 2001-01-30
PL341749A1 (en) 2001-02-12
AT502318A1 (en) 2007-02-15
EP1204656A2 (en) 2002-05-15
LT4790B (en) 2001-05-25
LV12623A (en) 2001-03-20
WO2001009116A3 (en) 2001-05-17
CZ299311B6 (en) 2008-06-18
HRP20000503B1 (en) 2008-04-30
ITMI20001759A0 (en) 2000-07-28
IE20000605A1 (en) 2001-04-04
BR0003209A (en) 2001-03-20
BE1013411A3 (en) 2001-12-04
GB2352717A (en) 2001-02-07
CO5180570A1 (en) 2002-07-30
FI20001722A7 (en) 2001-01-30
LU90617B1 (en) 2001-06-15
GB0018641D0 (en) 2000-09-13
SI20426A (en) 2001-06-30
TR200002206A2 (en) 2001-03-21
NL1015821A1 (en) 2001-01-30
IL137553A (en) 2005-09-25
KR100697177B1 (en) 2007-03-21
WO2001009116A2 (en) 2001-02-08
IT1318660B1 (en) 2003-08-27
TWI276437B (en) 2007-03-21
FR2796944A1 (en) 2001-02-02
MXPA00007461A (en) 2004-07-16
LT2000076A (en) 2001-02-26
ITMI20001759A1 (en) 2002-01-28
PT102502A (en) 2001-01-31
MD20000162A (en) 2001-04-30
DZ3060A1 (en) 2004-05-22
HRP20000503A2 (en) 2001-06-30
SE0002792D0 (en) 2000-07-28
CZ20002716A3 (en) 2001-05-16

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