PE20011134A1 - 4-fluoralquil-2h-benzopiranos con efecto antiestrogenico, metodo para su obtencion, preparados farmaceuticos que los contienen y su utilizacion para obtener medicamentos - Google Patents

4-fluoralquil-2h-benzopiranos con efecto antiestrogenico, metodo para su obtencion, preparados farmaceuticos que los contienen y su utilizacion para obtener medicamentos

Info

Publication number
PE20011134A1
PE20011134A1 PE2001000249A PE2001000249A PE20011134A1 PE 20011134 A1 PE20011134 A1 PE 20011134A1 PE 2001000249 A PE2001000249 A PE 2001000249A PE 2001000249 A PE2001000249 A PE 2001000249A PE 20011134 A1 PE20011134 A1 PE 20011134A1
Authority
PE
Peru
Prior art keywords
alkyl
benzopyranes
fluoralkyl
obtaining
contain
Prior art date
Application number
PE2001000249A
Other languages
English (en)
Inventor
Karl-Heinrich Fritzemeir
Christa Hegele-Hartung
Ludwing Zorn
Uwe Kollenkirchen
Hermann Kunzer
Rolf Jautelat
Original Assignee
Schering Ag
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 Schering Ag filed Critical Schering Ag
Publication of PE20011134A1 publication Critical patent/PE20011134A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
    • C07D311/60—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4 with aryl radicals attached in position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P15/12—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
    • A61P15/16—Masculine 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
    • A61P15/18—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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/28—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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • 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
    • A61P9/12—Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Pulmonology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)

Abstract

SE REFIERE A 4-FLUORALQUIL-2H-BENZOPIRANOS DE FORMULA I, DONDE R1 Y R2 SON H, ALQUILO C1-C5, ALCANOILO C1-C5, BENZOIL; X ES O, S, METILENO; n ES 2-4; Y ES NR3R4; R3 Y R4 SON H, ALQUILO C1-C10, ALQUENILO C1-C10, ALQUINILO C1-C10; OPCIONALMENTE SUSTITUIDOS CON FLUOR INTERRUMPIDO CON O, S, NR5; R5 ES H, ALQUILO, ARILO, HETEROARILO, ENTRE OTROS; R3 Y R4 JUNTO A N FORMAN HETEROCICLO DE 5-7 MIEMBROS; Z ES ALQUILO C1-C5. SON COMPUESTOS PREFERIDOS (+)-7-HIDROXI-3-(4'-HIDROXIFENIL)-2-[4"-(2"'-PIPERIDIN-1-ILETOXI)-FENIL]-4-(TRIFLUOROMETIL)-2H-1-BENZOPIRANO; 2-[4"-[2"'-DIMETILAMINOETOXI)-FENIL]-7-HIDROXI-3-(4'-HIDROXIFENIL)-4-(TRIFLUOROMETIL)-2H-1-BENZOPIRANO, ENTRE OTROS. EL COMPUESTO I ES UN INHIBIDOR DE ESTROGENOS Y PUEDEN SER UTILES PARA TRATAMIENTO DE OSTEOPOROSIS
PE2001000249A 2000-03-15 2001-03-15 4-fluoralquil-2h-benzopiranos con efecto antiestrogenico, metodo para su obtencion, preparados farmaceuticos que los contienen y su utilizacion para obtener medicamentos PE20011134A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10013782A DE10013782A1 (de) 2000-03-15 2000-03-15 4-Fluoralkyl-2H-benzopyrane mit antiestrogener Wirksamkeit, Verfahren zu ihrer Herstellung, pharmazeutische Präparate, die diese enthalten sowie deren Verwendung zur Herstellung von Arzneimitteln

Publications (1)

Publication Number Publication Date
PE20011134A1 true PE20011134A1 (es) 2001-11-23

Family

ID=7635636

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2001000249A PE20011134A1 (es) 2000-03-15 2001-03-15 4-fluoralquil-2h-benzopiranos con efecto antiestrogenico, metodo para su obtencion, preparados farmaceuticos que los contienen y su utilizacion para obtener medicamentos

Country Status (13)

Country Link
US (1) US6844336B2 (es)
EP (1) EP1272481B1 (es)
JP (1) JP3954386B2 (es)
AT (1) ATE264851T1 (es)
AU (1) AU4246501A (es)
DE (2) DE10013782A1 (es)
DK (1) DK1272481T3 (es)
ES (1) ES2218400T3 (es)
PE (1) PE20011134A1 (es)
PT (1) PT1272481E (es)
TR (1) TR200401782T4 (es)
UY (1) UY26620A1 (es)
WO (1) WO2001068634A1 (es)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003267773A1 (en) * 2003-10-14 2005-04-27 Council Of Scientific And Industrial Research (3r, 4r)-trans-3,4-diarylchroman derivatives with estrogenic activity
DK1812417T3 (da) * 2004-11-18 2009-02-16 Janssen Pharmaceutica Nv Nye 2H-chromenderivater som selektive östrogenreceptormodulatorer
JP2008528496A (ja) * 2005-01-21 2008-07-31 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ エストロゲン受容体のモジュレーターとして有用な新規な複素環式ベンゾ［ｃ］クロメン誘導体
MY150082A (en) 2007-10-16 2013-11-29 Repros Therapeutics Inc Trans-clomiphene for metabolic syndrome
DE102008057230A1 (de) 2008-11-11 2010-05-12 Bayer Schering Pharma Aktiengesellschaft Synergistische pharmazeutische Kombination mit einem Estrogenrezeptorantagonisten und einem Progestin
JP5735967B2 (ja) * 2009-08-19 2015-06-17 ユニバーシティー オブ ザ フリーステートＵｎｉｖｅｒｓｉｔｙ Ｏｆ Ｔｈｅ Ｆｒｅｅ Ｓｔａｔｅ Ｃ環３位連結ビフラボノイド及びｃ環３位連結ビフラボノイドアナログの合成
WO2011092127A1 (en) 2010-01-26 2011-08-04 Bayer Schering Pharma Aktiengesellschaft 14,17-bridged estratriene derivatives comprising heterocyclic bioisosteres for the phenolic a-ring
HUE033581T2 (hu) * 2010-06-10 2017-12-28 Seragon Pharmaceuticals Inc Ösztrogén receptor modulátorok és alkalmazásaik
KR20200144591A (ko) 2010-06-16 2020-12-29 앙도르쉐르슈 인코포레이티드 에스트로겐-관련 질병의 치료 또는 예방 방법
CA2857057A1 (en) * 2011-12-14 2013-06-20 Seragon Pharmaceuticals, Inc. Fluorinated estrogen receptor modulators and uses thereof
CA2857061A1 (en) 2011-12-16 2013-06-20 Olema Pharmaceuticals, Inc. Novel benzopyran compounds, compositions and uses thereof
CA2865234A1 (en) 2012-02-29 2013-09-06 Repros Therapeutics Inc. Combination therapy for treating androgen deficiency
CA2915534A1 (en) * 2013-06-19 2014-12-24 Seragon Pharmaceuticals, Inc. Azetidine estrogen receptor modulators and uses thereof
SG11201509508YA (en) 2013-06-19 2015-12-30 Seragon Pharmaceuticals Inc Estrogen receptor modulator and uses thereof
WO2014203132A1 (en) * 2013-06-19 2014-12-24 Olema Pharmaceuticals, Inc. Substituted benzopyran compounds, compositions and uses thereof
WO2016189011A1 (en) 2015-05-26 2016-12-01 F. Hoffmann-La Roche Ag Heterocyclic estrogen receptor modulators and uses thereof
RS63217B1 (sr) * 2015-10-27 2022-06-30 Sun Pharma Advanced Res Co Ltd Novi heterociklični antiestrogeni
JP7048505B2 (ja) 2015-11-10 2022-04-05 パラクリン セラピューティクス エービー Ｐｄｇｆ－ｃｃ阻害剤および抗エストロゲン剤によるｅｒ陰性乳癌の処置
WO2019144132A1 (en) * 2018-01-22 2019-07-25 Radius Pharmaceuticals, Inc. Estrogen receptor-modulating compounds
JP2022541938A (ja) 2019-07-22 2022-09-28 サン・ファーマ・アドバンスド・リサーチ・カンパニー・リミテッド 選択的エストロゲン受容体分解剤

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0470310B1 (en) 1990-08-09 1995-11-29 Council of Scientific and Industrial Research Novel benzopyrans and process for their production
US5254568A (en) 1990-08-09 1993-10-19 Council Of Scientific & Industrial Research Benzopyrans as antiestrogenic agents
US6060503A (en) 1991-12-02 2000-05-09 Endorecherche, Inc. Benzopyran-containing compounds and method for their use
AU8102398A (en) 1997-07-09 1999-02-08 Central Drug Research Institute (dl)-2,3-diaryl-2h-1-benzopyrans

Also Published As

Publication number Publication date
US20040034017A1 (en) 2004-02-19
EP1272481A1 (de) 2003-01-08
PT1272481E (pt) 2004-08-31
JP2003528057A (ja) 2003-09-24
EP1272481B1 (de) 2004-04-21
ES2218400T3 (es) 2004-11-16
US6844336B2 (en) 2005-01-18
AU4246501A (en) 2001-09-24
TR200401782T4 (tr) 2004-09-21
DE50102058D1 (de) 2004-05-27
JP3954386B2 (ja) 2007-08-08
UY26620A1 (es) 2001-10-25
ATE264851T1 (de) 2004-05-15
DK1272481T3 (da) 2004-08-02
DE10013782A1 (de) 2001-10-18
WO2001068634A1 (de) 2001-09-20

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