UY24362A1 - D-tartrato de (-)-cis-6(s)-fenil-5(r)-(4-(2-pirrolidin-1-il etoxi)fenil)-5,6,7,8-tetrahidronaftalen-2-ol - Google Patents

D-tartrato de (-)-cis-6(s)-fenil-5(r)-(4-(2-pirrolidin-1-il etoxi)fenil)-5,6,7,8-tetrahidronaftalen-2-ol

Info

Publication number
UY24362A1
UY24362A1 UY24362A UY24362A UY24362A1 UY 24362 A1 UY24362 A1 UY 24362A1 UY 24362 A UY24362 A UY 24362A UY 24362 A UY24362 A UY 24362A UY 24362 A1 UY24362 A1 UY 24362A1
Authority
UY
Uruguay
Prior art keywords
phenyl
solution
pyrrolidin
cis
tartrate
Prior art date
Application number
UY24362A
Other languages
English (en)
Inventor
K Chiu Charles
Morgan Meltz
Original Assignee
Pfizer
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 Pfizer filed Critical Pfizer
Publication of UY24362A1 publication Critical patent/UY24362A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/06—Antiabortive agents; Labour repressants
    • 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
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • A61P15/18—Feminine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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

Abstract

Un procedimiento ventajoso de preparación de D-tartrato de (-)-cis-6(S)-fenil-5(R)-[4-(2-pirrolidin-1-iletoxi)fenil]-5, 6, 7, 8-tetrahidronaftalen-2-ol, que es útil como agonista de estrógenos. También aporta procedimientos para tratar o prevenir enfermedades o estados que son susceptibles de ser tratados o prevenidos por agonistas de estrógenos, los cuales comprenden administrar a un mamífero que necesite tal tratamiento o prevención, una cantidad eficaz del compuesto. Dicho procedimiento comprende: a- disolver cis-6-fenil-5-[4-(2-pirrolidin-1-iletoxi)fenil]-5, 6, 7, 8-tetrahidronaftalen-2-ol racémico, o enriquecido ópticamente de forma parcial, en etanol acuoso en ebullición para formar una disolución, b- añadir a dicha disolución una cantidad molar igual de ácido D-tartárico disuelto en etanol acuoso para formar una segunda disolución; c- enfriar dicha segunda disolución; y d- recoger el producto formado en el paso c. Este procedimiento es útil para tratar osteoporosis, enfermedades cardiovascular o hiperlipidemia, para disminuir los niveles séricos de colesterol, obesidad cáncer de mama, endometriosis.
UY24362A 1995-11-02 1996-11-04 D-tartrato de (-)-cis-6(s)-fenil-5(r)-(4-(2-pirrolidin-1-il etoxi)fenil)-5,6,7,8-tetrahidronaftalen-2-ol UY24362A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US612595P 1995-11-02 1995-11-02

Publications (1)

Publication Number Publication Date
UY24362A1 true UY24362A1 (es) 1997-04-24

Family

ID=21719433

Family Applications (1)

Application Number Title Priority Date Filing Date
UY24362A UY24362A1 (es) 1995-11-02 1996-11-04 D-tartrato de (-)-cis-6(s)-fenil-5(r)-(4-(2-pirrolidin-1-il etoxi)fenil)-5,6,7,8-tetrahidronaftalen-2-ol

Country Status (43)

Country Link
US (1) US5948809A (es)
EP (1) EP0876359B1 (es)
JP (1) JP3088020B2 (es)
KR (1) KR19990067280A (es)
CN (1) CN1067065C (es)
AP (1) AP713A (es)
AR (1) AR004078A1 (es)
AT (1) ATE248827T1 (es)
AU (1) AU708841B2 (es)
BG (1) BG63943B1 (es)
BR (1) BR9611436A (es)
CA (1) CA2236673C (es)
CO (1) CO4770967A1 (es)
CZ (1) CZ287341B6 (es)
DE (1) DE69629837T2 (es)
DK (1) DK0876359T3 (es)
DZ (1) DZ2114A1 (es)
EG (1) EG21095A (es)
ES (1) ES2203713T3 (es)
GT (1) GT199600085A (es)
HR (1) HRP960503B1 (es)
HU (1) HU227521B1 (es)
IL (1) IL124027A (es)
IS (1) IS1855B (es)
MA (1) MA23998A1 (es)
NO (1) NO310358B1 (es)
NZ (1) NZ318498A (es)
OA (1) OA11009A (es)
PE (1) PE17698A1 (es)
PL (1) PL188633B1 (es)
PT (1) PT876359E (es)
RO (1) RO119829B1 (es)
RU (1) RU2162465C2 (es)
SI (1) SI0876359T1 (es)
SK (1) SK282172B6 (es)
TN (1) TNSN96134A1 (es)
TR (1) TR199800783T2 (es)
TW (2) TW581766B (es)
UA (1) UA51676C2 (es)
UY (1) UY24362A1 (es)
WO (1) WO1997016434A1 (es)
YU (1) YU49123B (es)
ZA (1) ZA969212B (es)

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PE20000646A1 (es) * 1998-06-16 2000-08-05 Pfizer Prod Inc Terapia de combinacion para la fragilidad musculoesqueletica
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CO5271697A1 (es) 2000-01-12 2003-04-30 Pfizer Prod Inc Composiciones y procedimientos para el tratamiento de afecciones que responden a un aumento de testosterona
CO5271696A1 (es) * 2000-01-12 2003-04-30 Pfizer Prod Inc Procedimiento para reducir la morbilidad y el riesgo de mortalidad
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HUP0300419A3 (en) 2000-04-07 2005-07-28 Pfizer Prod Inc Estrogen agonist/antagonist metabolites, pharmaceutical compositions containing them and their use
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EP1765461A1 (en) * 2004-06-21 2007-03-28 Pharmacia & Upjohn Company LLC Pyk2 inhibitors for stimulation of osteoblast function
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EP1899310B1 (en) 2005-06-22 2010-09-29 Pfizer Products Inc. Stereoselective hydrogenation process for preparing cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-2-methoxy-5,6,7,8-tetrahydronaphthalene hydrochloride
CZ2007373A3 (cs) * 2007-05-29 2008-12-10 Zentiva, A. S Zpusob prípravy lasofoxifenu
EP2424839A4 (en) 2009-04-29 2012-10-17 Glenmark Generics Ltd PROCESS FOR THE PREPARATION OF LASOFOXIFEN TARTRATE
KR101149529B1 (ko) 2009-09-11 2012-05-25 한국화학연구원 인덴온 유도체 및 이를 포함하는 약학적 조성물
CN103113323B (zh) * 2013-02-05 2015-11-11 南京华威医药科技开发有限公司 酒石酸拉索昔芬中间体的制备方法
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Also Published As

Publication number Publication date
IL124027A (en) 2001-10-31
DE69629837T2 (de) 2004-05-06
BR9611436A (pt) 1999-03-23
BG102474A (en) 1999-06-30
CN1067065C (zh) 2001-06-13
TR199800783T2 (xx) 1998-08-21
JPH11502866A (ja) 1999-03-09
TW518327B (en) 2003-01-21
EP0876359A1 (en) 1998-11-11
AU708841B2 (en) 1999-08-12
DZ2114A1 (fr) 2002-07-22
HU227521B1 (en) 2011-07-28
ATE248827T1 (de) 2003-09-15
UA51676C2 (uk) 2002-12-16
DK0876359T3 (da) 2003-11-24
JP3088020B2 (ja) 2000-09-18
PE17698A1 (es) 1998-04-18
CZ132098A3 (cs) 1999-03-17
PL326498A1 (en) 1998-09-28
NZ318498A (en) 1999-06-29
NO310358B1 (no) 2001-06-25
CZ287341B6 (en) 2000-10-11
SK54298A3 (en) 1999-07-12
CA2236673C (en) 2002-03-19
EP0876359B1 (en) 2003-09-03
AU6998496A (en) 1997-05-22
TW581766B (en) 2004-04-01
GT199600085A (es) 1998-04-04
SI0876359T1 (en) 2003-12-31
HUP9900087A3 (en) 1999-11-29
KR19990067280A (ko) 1999-08-16
HRP960503A2 (en) 1998-04-30
US5948809A (en) 1999-09-07
DE69629837D1 (de) 2003-10-09
YU57896A (sh) 1998-12-23
AP713A (en) 1998-12-28
AR004078A1 (es) 1998-09-30
YU49123B (sh) 2004-03-12
ZA969212B (en) 1998-05-04
AP9600880A0 (en) 1997-01-31
HRP960503B1 (en) 2001-12-31
RU2162465C2 (ru) 2001-01-27
IS4718A (is) 1998-04-16
CA2236673A1 (en) 1997-05-09
HUP9900087A2 (hu) 1999-05-28
RO119829B1 (ro) 2005-04-29
NO981962L (no) 1998-04-30
ES2203713T3 (es) 2004-04-16
WO1997016434A1 (en) 1997-05-09
IS1855B (is) 2003-02-21
CN1201458A (zh) 1998-12-09
BG63943B1 (bg) 2003-07-31
CO4770967A1 (es) 1999-04-30
PT876359E (pt) 2003-12-31
EG21095A (en) 2000-10-31
TNSN96134A1 (fr) 1998-12-31
SK282172B6 (sk) 2001-11-06
OA11009A (en) 2003-03-03
PL188633B1 (pl) 2005-03-31
NO981962D0 (no) 1998-04-30
MA23998A1 (fr) 1997-07-01
MX9803544A (es) 1998-09-30

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