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PE20021083A1 - MODULATORS OF THE ESTROGEN RECEPTORS - Google Patents

MODULATORS OF THE ESTROGEN RECEPTORS

Info

Publication number
PE20021083A1
PE20021083A1 PE2002000308A PE2002000308A PE20021083A1 PE 20021083 A1 PE20021083 A1 PE 20021083A1 PE 2002000308 A PE2002000308 A PE 2002000308A PE 2002000308 A PE2002000308 A PE 2002000308A PE 20021083 A1 PE20021083 A1 PE 20021083A1
Authority
PE
Peru
Prior art keywords
alkyl
cycloalkyl
alkenyl
modulators
acetophenone
Prior art date
Application number
PE2002000308A
Other languages
Spanish (es)
Inventor
Helen Y Chen
Jane Y Wu
Seongkon Kim
Frank P Dininno
Original Assignee
Merck & Co Inc
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 Merck & Co Inc filed Critical Merck & Co Inc
Publication of PE20021083A1 publication Critical patent/PE20021083A1/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D411/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/04Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D411/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/12Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and 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
    • 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
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32Antioestrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D327/00Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D327/02Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms one oxygen atom and one sulfur atom
    • C07D327/06Six-membered rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D339/00Heterocyclic compounds containing rings having two sulfur atoms as the only ring hetero atoms
    • C07D339/08Six-membered rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Reproductive Health (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA I DONDE R1 ES H, ALQUILO C1-C5, CICLOALQUILO C3-C8, ALQUENILO C2-C5, ALQUINILO C2-C5, OR6, ENTRE OTROS; R2 ES H, ALQUILO C1-C5, CICLOALQUILO C3-C8, ALQUENILO C2-C5, ALQUINILO C2-C5, ENTRE OTROS; R3 ES H, ALQUILO C1-C5, CICLOALQUILO C3-C8, ALQUENILO C2-C5, ALQUINILO C2-C5, ENTRE OTROS; R4 ES H, ALQUILO C1-C5, CICLOALQUILO C3-C8, ALQUENILO C2-C5, ALQUINILO C2-C5, ENTRE OTROS; R5 ES ALQUILO C1-C5, CICLOALQUILO C3-C8, ALQUENILO C2-C5, ENTRE OTROS; X E Y SON O, S, SULFOXIDO, SULFONA; R6 ES H, ALQUILO C1-C5, BENCILO, METOXIMETILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS 2-TIOFENO-4-METOXI-ACETOFENONA, 2-TIOFENO-4-HIDROXI-ACETOFENONA, 2-TIOFENO-4-METOXI-ACETOFENONA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS MENCIONADOS SON MODULADORES DE LOS RECEPTORES ESTROGENOS Y SON UTILES PARA EL TRATAMIENTO DE OSTEOPOROSIS, DEGENERACION DE CARTILAGO, ENDOMETRIOSISREFERS TO COMPOUNDS OF FORMULA I WHERE R1 IS H, C1-C5 ALKYL, C3-C8 CYCLOALKYL, C2-C5 ALKENYL, C2-C5 ALKYNYL, OR6, AMONG OTHERS; R2 IS H, C1-C5 ALKYL, C3-C8 CYCLOALKYL, C2-C5 ALKENYL, C2-C5 ALKYL, AMONG OTHERS; R3 IS H, C1-C5 ALKYL, C3-C8 CYCLOALKYL, C2-C5 ALKENYL, C2-C5 ALKYL, AMONG OTHERS; R4 IS H, C1-C5 ALKYL, C3-C8 CYCLOALKYL, C2-C5 ALKENYL, C2-C5 ALKYL, AMONG OTHERS; R5 IS C1-C5 ALKYL, C3-C8 CYCLOALKYL, C2-C5 ALKYL, AMONG OTHERS; X AND Y ARE O, S, SULFOXIDE, SULFONE; R6 IS H, C1-C5 ALKYL, BENZYL, METOXIMETHYL, AMONG OTHERS. PREFERRED COMPOUNDS ARE 2-THIOPHENE-4-METOXY-ACETOPHENONE, 2-THIOPHENE-4-HYDROXY-ACETOPHENONE, 2-THIOPHENE-4-METOXY-ACETOPHENONE, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION AND A PROCEDURE FOR THE PREPARATION. THE MENTIONED COMPOUNDS ARE MODULATORS OF THE ESTROGEN RECEPTORS AND ARE USEFUL FOR THE TREATMENT OF OSTEOPOROSIS, CARTILAGE DEGENERATION, ENDOMETRIOSIS

PE2002000308A 2000-10-19 2002-04-15 MODULATORS OF THE ESTROGEN RECEPTORS PE20021083A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24158200P 2000-10-19 2000-10-19
PCT/US2001/042735 WO2002032377A2 (en) 2000-10-19 2001-10-15 Estrogen receptor modulators

Publications (1)

Publication Number Publication Date
PE20021083A1 true PE20021083A1 (en) 2002-12-16

Family

ID=22911282

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2002000308A PE20021083A1 (en) 2000-10-19 2002-04-15 MODULATORS OF THE ESTROGEN RECEPTORS

Country Status (20)

Country Link
EP (1) EP1333827A2 (en)
JP (1) JP2004511502A (en)
KR (1) KR20030042020A (en)
CN (1) CN1469743A (en)
AU (2) AU3238102A (en)
BG (1) BG107676A (en)
BR (1) BR0114689A (en)
CA (1) CA2424729A1 (en)
EA (1) EA200300474A1 (en)
EC (1) ECSP034558A (en)
EE (1) EE200300153A (en)
HU (1) HUP0303563A2 (en)
IL (1) IL154984A0 (en)
IS (1) IS6761A (en)
MX (1) MXPA03003485A (en)
NO (1) NO20031737L (en)
PE (1) PE20021083A1 (en)
PL (1) PL361053A1 (en)
SK (1) SK4772003A3 (en)
WO (1) WO2002032377A2 (en)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030225132A1 (en) * 2002-04-11 2003-12-04 Dininno Frank P. Estrogen receptor modulators
US7138426B2 (en) * 2002-04-24 2006-11-21 Merck & Co., Inc. Estrogen receptor modulators
RU2387451C2 (en) 2002-05-10 2010-04-27 Ф.Хоффманн-Ля Рош Аг Bisphosphonic acids intended for treatment and prevention of osteoporosis
CA2512000C (en) * 2002-12-26 2011-08-09 Eisai Co., Ltd. Selective estrogen receptor modulator
EP2314295B1 (en) * 2005-07-29 2015-01-28 Resverlogix, Inc Pharmaceutical compositions for the prevention and treatment of complex diseases and their delivery by insertable medical devices
WO2007049798A1 (en) 2005-10-27 2007-05-03 Banyu Pharmaceutical Co., Ltd. Novel benzoxathiin derivative
CN101641339B (en) 2007-02-01 2013-07-17 雷斯韦洛吉克斯公司 Compounds for the prevention and treatment of cardiovascular diseases
US8952021B2 (en) 2009-01-08 2015-02-10 Resverlogix Corp. Compounds for the prevention and treatment of cardiovascular disease
AU2010224523B2 (en) 2009-03-18 2014-05-08 Resverlogix Corp. Novel anti-inflammatory agents
MX374414B (en) 2009-04-22 2025-03-06 Resverlogix Corp NEW ANTI-INFLAMMATORY AGENTS.
EP2580210B1 (en) 2010-06-10 2017-03-01 Seragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
US8853423B2 (en) 2010-06-17 2014-10-07 Seragon Pharmaceuticals, Inc. Indane estrogen receptor modulators and uses thereof
SI2773354T1 (en) 2011-11-01 2019-08-30 Resverlogix Corp. Oral immediate release formulations for substituted quinazolinones
EP2791132A4 (en) 2011-12-14 2015-08-05 Seragon Pharmaceuticals Inc MODULATORS OF STROGEN RECEPTORS AND USES THEREOF
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
CN105073744B (en) 2012-12-21 2019-11-08 齐尼思表观遗传学有限公司 Novel heterocyclic compounds as bromodomain inhibitors
CN107530356A (en) 2015-03-13 2018-01-02 雷斯韦洛吉克斯公司 Compositions and methods of treatment for treating complement-associated diseases

Also Published As

Publication number Publication date
ECSP034558A (en) 2003-06-25
EA200300474A1 (en) 2003-10-30
SK4772003A3 (en) 2003-08-05
JP2004511502A (en) 2004-04-15
EE200300153A (en) 2003-06-16
KR20030042020A (en) 2003-05-27
WO2002032377A3 (en) 2002-08-22
CN1469743A (en) 2004-01-21
IS6761A (en) 2003-03-27
WO2002032377A2 (en) 2002-04-25
BR0114689A (en) 2003-07-01
AU3238102A (en) 2002-04-29
PL361053A1 (en) 2004-09-20
HUP0303563A2 (en) 2004-03-01
BG107676A (en) 2003-11-28
EP1333827A2 (en) 2003-08-13
IL154984A0 (en) 2003-10-31
NO20031737D0 (en) 2003-04-15
CA2424729A1 (en) 2002-04-25
AU2002232381B2 (en) 2004-11-18
MXPA03003485A (en) 2003-07-14
NO20031737L (en) 2003-06-19

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