BR0014901A - Derivados de trifenil-alquenos e seu uso como moduladores de receptores seletivos de estrogênios - Google Patents

Derivados de trifenil-alquenos e seu uso como moduladores de receptores seletivos de estrogênios

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Publication number
BR0014901A
BR0014901A BR0014901-2A BR0014901A BR0014901A BR 0014901 A BR0014901 A BR 0014901A BR 0014901 A BR0014901 A BR 0014901A BR 0014901 A BR0014901 A BR 0014901A
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BR
Brazil
Prior art keywords
ethoxy
alken
modulators
derivatives
different
Prior art date
Application number
BR0014901-2A
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English (en)
Other versions
BRPI0014901B1 (pt
BRPI0014901B8 (pt
Inventor
Marja-Liisa Soedervall
Arja Kalapudas
Risto Lammintausta
Kalervo Vaeaenaenen
Lauri Kangas
Pirkko Haerkoenen
Original Assignee
Hormos Medical Corp
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Publication date
Application filed by Hormos Medical Corp filed Critical Hormos Medical Corp
Publication of BR0014901A publication Critical patent/BR0014901A/pt
Publication of BRPI0014901B1 publication Critical patent/BRPI0014901B1/pt
Publication of BRPI0014901B8 publication Critical patent/BRPI0014901B8/pt

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    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/24—Antidepressants
    • 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
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/02—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C211/09—Diamines
    • C07C211/10—Diaminoethanes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
    • C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
    • C07C215/16—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic the nitrogen atom of the amino group being further bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/02—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C217/04—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C217/06—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted
    • C07C217/14—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring
    • C07C217/18—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted
    • C07C217/20—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted by halogen atoms, by trihalomethyl, nitro or nitroso groups, or by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/10—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C323/11—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/12—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C43/00—Ethers; Compounds having groups, groups or groups
    • C07C43/02—Ethers
    • C07C43/20—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
    • C07C43/225—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C43/00—Ethers; Compounds having groups, groups or groups
    • C07C43/02—Ethers
    • C07C43/20—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
    • C07C43/23—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing hydroxy or O-metal groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/58—Unsaturated compounds containing ether groups, groups, groups, or groups
    • C07C59/64—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings
    • C07C59/66—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings the non-carboxylic part of the ether containing six-membered aromatic rings
    • C07C59/68—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings the non-carboxylic part of the ether containing six-membered aromatic rings the oxygen atom of the ether group being bound to a non-condensed six-membered aromatic ring
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    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Anesthesiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hospice & Palliative Care (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Steroid Compounds (AREA)

Abstract

"DERIVADOS DE TRIFENIL-ALQUENOS E SEU USO COMO MODULADORES DE RECEPTORES SELETIVOS DE ESTROGêNIOS". A invenção fornece compostos moduladores de receptores seletivos de estrogênios, inovadores, da fórmula genérica: onde R1 and R2, que são iguais ou diferentes, são a) H, halogênio, OCH3, OH; ou b) onde X é O, NH ou S; e n é um número inteiro entre 1 e 4; e R4 e R5, que são iguais ou diferentes, são uma alquila com 1 a 4 carbonos, H, -CH2C<154>CH ou -CH2CH2OH; ou R4 e R5 formam um anel com cinco ou seis membros contendo N ou um anel heteroaromático; ou c) -Y-(CH2)nCH2-O-R6 onde Y é O, NH ou S e n é um número inteiro entre 1 e 4; e R6 é H, -CH2CH2OH, ou -CH2CH2C1; ou d) 2,3-diidróxi-propóxi, 2-metil-sulfamil-etóxi, 2-cloro-etóxy, 1-etil-2-hidróxi-etóxi, 2,2-dietil-2-hidróxi-etóxi ou carbóxi-metóxi; e em que R1 e R2, sendo os mesmos ou diferentes são R3 é H, halogênio, OH ou -OCH3; e seus sais e ésteres atóxicos de uso farmacêutico, e suas misturas, compostos estes que apresentam propriedades farmacológicas valiosas.
BRPI0014901A 1999-11-16 2000-11-01 composto derivado de trifenil-alquenos e composição farmacêutica para uso como moduladores de receptores seletivos de estrogênios BRPI0014901B8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US16582899P 1999-11-16 1999-11-16
PCT/FI2000/000946 WO2001036360A1 (en) 1999-11-16 2000-11-01 Triphenylalkene derivatives and their use as selective estrogen receptor modulators

Publications (3)

Publication Number Publication Date
BR0014901A true BR0014901A (pt) 2002-06-11
BRPI0014901B1 BRPI0014901B1 (pt) 2016-08-02
BRPI0014901B8 BRPI0014901B8 (pt) 2021-05-25

Family

ID=22600649

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0014901A BRPI0014901B8 (pt) 1999-11-16 2000-11-01 composto derivado de trifenil-alquenos e composição farmacêutica para uso como moduladores de receptores seletivos de estrogênios

Country Status (29)

Country Link
US (2) US6576645B1 (pt)
EP (1) EP1235776B1 (pt)
JP (1) JP4202647B2 (pt)
KR (2) KR100877487B1 (pt)
CN (2) CN1263720C (pt)
AT (1) ATE317378T1 (pt)
AU (1) AU778296B2 (pt)
BG (1) BG65853B1 (pt)
BR (1) BRPI0014901B8 (pt)
CA (1) CA2390116C (pt)
CZ (1) CZ304738B6 (pt)
DE (1) DE60025938T2 (pt)
DK (1) DK1235776T3 (pt)
EE (1) EE05126B1 (pt)
ES (1) ES2253268T3 (pt)
HR (1) HRP20020223C1 (pt)
HU (1) HU228512B1 (pt)
IL (2) IL148198A0 (pt)
MX (1) MXPA02002154A (pt)
NO (2) NO328010B1 (pt)
NZ (1) NZ518542A (pt)
PL (1) PL201512B1 (pt)
PT (1) PT1235776E (pt)
RU (1) RU2247715C2 (pt)
SK (1) SK287752B6 (pt)
TW (1) TW593256B (pt)
UA (1) UA76409C2 (pt)
WO (1) WO2001036360A1 (pt)
ZA (1) ZA200201433B (pt)

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW593256B (en) * 1999-11-16 2004-06-21 Hormos Medical Oy Ltd Triphenylalkene derivatives and their use as selective estrogen receptor modulators
FI111710B (fi) 2001-05-04 2003-09-15 Hormos Medical Oy Ltd Menetelmä terapeuttisesti aktiivisen yhdisteen valmistamiseksi
US20040248989A1 (en) * 2003-06-05 2004-12-09 Risto Santti Method for the treatment or prevention of lower urinary tract symptoms
MXPA06001094A (es) 2003-07-28 2006-04-11 Smithkline Beecham Corp Compuestos quimicos.
US7196119B2 (en) 2003-10-21 2007-03-27 The Regents Of The University Of California Development of new selective estrogen receptor modulators
KR20070059110A (ko) * 2004-09-03 2007-06-11 호르모스 메디칼 리미티드 안드로겐 결핍의 치료 또는 예방에 사용하는 제제의 제조를위한 선택적 에스트로겐 수용체 조절자의 용도
BRPI0618510A2 (pt) * 2005-11-09 2011-09-06 Hormos Medical Ltd formulação medicamentosa lìquida ou semi-sólida
JP2009516694A (ja) * 2005-11-22 2009-04-23 スミスクライン ビーチャム コーポレーション 化合物
CN101484000A (zh) * 2005-11-22 2009-07-15 史密丝克莱恩比彻姆公司 化合物
EP1951250A4 (en) * 2005-11-22 2009-12-16 Smithkline Beecham Corp CHEMICAL COMPOUNDS
JP2009516746A (ja) * 2005-11-22 2009-04-23 スミスクライン ビーチャム コーポレーション 化合物
US7825107B2 (en) 2006-05-22 2010-11-02 Hormos Medical Ltd. Method of treating men suffering from chronic nonbacterial prostatitis with SERM compounds or aromatase inhibitors
EP2121553B1 (en) 2007-02-14 2012-06-27 Hormos Medical Ltd. Method for the preparation of therapeutically valuable triphenylbutene derivatives
WO2008099060A2 (en) 2007-02-14 2008-08-21 Hormos Medical Ltd Methods for the preparation of fispemifene from ospemifene
WO2008157335A2 (en) * 2007-06-13 2008-12-24 Quatrx Pharmaceuticals Company Methods for the treatment of erectile dysfunction using fispemifene
SG185311A1 (en) 2007-10-16 2012-11-29 Repros Therapeutics Inc Trans-clomiphene for metabolic syndrome
WO2009120999A2 (en) * 2008-03-28 2009-10-01 Olema Pharmaceuticals, Inc. Use of an endoxifen prodrug for treatment of breast cancer
US8318667B2 (en) 2009-02-25 2012-11-27 Merck Sharp & Dohme Corp. Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
RS53353B (sr) 2010-01-19 2014-10-31 Cambrex Karlskoga Ab Novi postupci za proizvodnju derivata benzofenona
ES2532536T3 (es) * 2010-05-20 2015-03-27 Basf Se Derivados de tris(2-hidroxifenil)metano, su preparación y su uso
DE102010027016A1 (de) 2010-07-09 2012-01-12 Universitätsklinikum Jena Steroid-Styrylfarbstoff-Konjugate zur Simulation und direkten lichtoptischen Detektion des Verhaltens von Steroiden im lebenden biologischen Gewebe und in Gegenwart von steroidbindenden Proteinen
GB2483736B (en) 2010-09-16 2012-08-29 Aragon Pharmaceuticals Inc Estrogen receptor modulators and uses thereof
KR101308258B1 (ko) * 2010-10-15 2013-09-13 씨제이제일제당 (주) 엔독시펜의 신규한 제조 방법
KR20150039705A (ko) * 2011-12-30 2015-04-13 켄타우루스 바이오파마 컴퍼니 리미티드 신규 아릴알켄 유도체 및 이의 선택성 에스트로겐 수용체 조절제에 있어서의 응용
CN102584687A (zh) * 2011-12-30 2012-07-18 北京赛林泰医药技术有限公司 作为选择性雌激素受体调节剂的乙烯衍生物
CN102532073A (zh) * 2011-12-30 2012-07-04 北京赛林泰医药技术有限公司 作为选择性雌激素受体调节剂的乙烯衍生物
US20150031656A1 (en) 2012-02-29 2015-01-29 Repros Therapeutics Inc. Combination therapy for treating androgen deficiency
MX2014011217A (es) 2012-03-20 2015-03-10 Seragon Pharmaceuticals Inc Moduladores del receptor de estrogeno y sus usos.
US9321712B2 (en) 2012-10-19 2016-04-26 Fermion Oy Process for the preparation of ospemifene
US20150321983A1 (en) 2012-10-19 2015-11-12 Fermion Oy A process for the preparation of ospemifene
WO2014141292A2 (en) * 2013-03-04 2014-09-18 Intas Pharmaceuticals Limited Endoxifen citrate polymorph and process for preparing the same
US9744177B2 (en) 2014-03-10 2017-08-29 Endorecherche, Inc. Treatment of male androgen deficiency symptoms or diseases with sex steroid precursor combined with SERM
MX2017003290A (es) * 2014-09-16 2017-06-21 Shionogi & Co Proceso para la preparacion de derivados de trifenilbuteno.
CA2971216A1 (en) 2014-12-23 2016-06-30 The Regents Of The University Of California Methods for immunomodulation of cancer and infectious disease therapy
EP3373967B9 (en) 2015-11-10 2023-10-04 Paracrine Therapeutics AB Treatment of er-negative breast cancer with an pdgf-cc inhibitor and an anti estrogen
EA039048B1 (ru) 2016-03-15 2021-11-26 Сионоги Энд Ко., Лтд. Способ получения производных феноксиэтанола
US20190167820A1 (en) 2016-06-27 2019-06-06 Sung Yeoun HWANG Novel aryl ethene derivative and pharmaceutical composition containing same as active ingredient
KR101819639B1 (ko) * 2016-06-27 2018-01-17 주식회사 케미메디 신규한 아릴에텐 유도체 및 이를 유효성분으로 함유하는 약제학적 조성물
KR102052133B1 (ko) * 2017-08-10 2019-12-05 고려대학교 산학협력단 당 부가된 오스페미펜, 이의 제조방법 및 이를 유효성분으로 함유하는 약학적 조성물
WO2019103989A1 (en) * 2017-11-22 2019-05-31 Temple University-Of The Commonwealth System Of Higher Education Novel functionalized n,n-dialkylamino phenyl ethers and their method of use
AU2019384807A1 (en) * 2018-11-21 2021-05-20 Accutar Biotechnology Inc. Novel compounds having estrogen receptor alpha degradation activity and uses thereof
WO2021133886A1 (en) 2019-12-23 2021-07-01 Accutar Biotechnology Combinations of estrogen receptor degraders and cyclin-dependent kinase inhibitors for treating cancer
US12496309B2 (en) 2020-06-22 2025-12-16 Novmetapharma Co., Ltd. Method for treatment of pancreatitis
US11413270B2 (en) * 2020-06-22 2022-08-16 Novmetapharma Co., Ltd. Method for the treatment of pancreatitis
CN116113409B (zh) 2020-08-04 2026-02-03 诺麦塔制药有限公司 细胞因子释放综合征的治疗方法

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE637389A (pt) 1962-09-13
GB2042519B (en) * 1979-01-17 1983-03-23 Biorex Laboratories Ltd 1,1,2-triphenylethane and -ehylene derivatives
US4656187A (en) 1981-08-03 1987-04-07 Eli Lilly And Company Treatment of mammary cancer
FI67538C (fi) * 1982-05-27 1985-04-10 Farmos Oy Foerfarande foer framstaellning av (z)-1,2-difenyl-1-(4-(2-(n n-dimetylamino)etoxi)fenyl)-1-buten
FI77839C (fi) * 1982-05-27 1989-05-10 Farmos Oy Foerfarande foer framstaellning av nya terapeutiskt effektiva trifenylalkan- och alkenderivat.
GB2126576B (en) * 1982-06-25 1985-06-19 Farmos Group Limited Alkane and alkene derivatives
US5491173A (en) 1982-06-25 1996-02-13 Orion-Yhtyma Oy Tri-phenyl alkene derivatives and their preparation and use
US4729999A (en) 1984-10-12 1988-03-08 Bcm Technologies Antiestrogen therapy for symptoms of estrogen deficiency
GB2196003A (en) 1986-09-11 1988-04-20 Nat Res Dev Iodo-and bromo-tamoxifen derivatives
US5189212A (en) 1990-09-07 1993-02-23 University Of Georgia Research Foundation, Inc. Triarylethylene carboxylic acids with estrogenic activity
US6096874A (en) 1990-10-01 2000-08-01 Board Of Regents, The University Of Texas System High affinity tamoxifen derivatives
EP0551434B1 (en) 1990-10-01 1995-11-15 The Board Of Regents, The University Of Texas System High affinity tamoxifen derivatives and uses thereof
US5219548A (en) 1990-10-01 1993-06-15 Board Of Regents, The University Of Texas System High affinity halogenated-tamoxifen derivatives and uses thereof
US5118667A (en) 1991-05-03 1992-06-02 Celtrix Pharmaceuticals, Inc. Bone growth factors and inhibitors of bone resorption for promoting bone formation
US5196435A (en) 1991-11-21 1993-03-23 Eli Lilly And Company Melatonin derivatives and combinations with antiestrogen compounds for treating mammalian breast carcinoma
GB9207437D0 (en) 1992-04-03 1992-05-20 Orion Yhtymae Oy Topical administration of toremifene and its metabolites
US5446203A (en) 1992-08-25 1995-08-29 New York University Synthesis of haloenones and aryl or alkyl substituted enones or alkenes
DE4335876A1 (de) 1993-10-17 1995-04-20 Schering Ag Kombination von Progesteronantagonisten und Antiöstrogenen mit partialer agonistischer Wirkung für die Hormonsubstitutions-Therapie für peri- und postmenopausale Frauen
US5650425A (en) 1994-04-04 1997-07-22 Pharmos Corporation Permanently ionic derivatives of steroid hormones and their antagonists
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
US5604248A (en) 1994-05-05 1997-02-18 Eli Lilly And Company Method for minimizing the uterotrophic effect of tamoxifen and tamoxifen analogs
US5470883A (en) 1994-05-23 1995-11-28 Stromberg; Brent V. Method of treating peripheral vasoconstriction with tamoxifen citrate
US5441986A (en) 1994-07-19 1995-08-15 Pfizer Inc. Estrogen agonists as remedies for prostate and cardiovascular diseases
GB9418067D0 (en) * 1994-09-07 1994-10-26 Orion Yhtymae Oy Triphenylethylenes for the prevention and treatment of osteoporosis
US5629425A (en) * 1994-09-19 1997-05-13 Eli Lilly And Company Haloalkyl hemisolvates of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-piperidinoethoxy)-benzoyl]benzo[b]thiophene
US5658931A (en) 1994-09-20 1997-08-19 Eli Lilly And Company Method for inhibiting mammalian breast carcinoma with tamoxifen, and analogs thereof, and certain naphthyl compounds
WO1996016646A1 (en) 1994-11-29 1996-06-06 Hoechst Marion Roussel, Inc. Method of using triaryl-ethylene derivatives in the treatment and prevention of osteoporosis
US5821254A (en) 1995-02-17 1998-10-13 The United States Of America As Represented By The Department Of Health And Human Services Uses of 9-cis-retinoic acids and derivatives thereof alone or in combination with antineoplastic agents in the prevention or treatment of cancer
GB9509572D0 (en) * 1995-05-11 1995-07-05 Cancer Res Campaign Tech Cancer therapy
DE19526146A1 (de) 1995-07-07 1997-01-09 Schering Ag Triphenylethylene, Verfahren zu deren Herstellung, diese Triphenylethylene enthaltene pharmazeutische Präparate sowie deren Verwendung zur Herstellung von Arzneimitteln
GB9604577D0 (en) 1996-03-04 1996-05-01 Orion Yhtymae Oy Serum cholesterol lowering agent
GB9803521D0 (en) * 1998-02-19 1998-04-15 Orion Yhtymo Oy New compounds and pharmaceutical compositions thereof
US6465445B1 (en) * 1998-06-11 2002-10-15 Endorecherche, Inc. Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
TW593256B (en) * 1999-11-16 2004-06-21 Hormos Medical Oy Ltd Triphenylalkene derivatives and their use as selective estrogen receptor modulators

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