AR029989A1 - Compuestos esteroides 16 alfa-sustituidos para el uso en tratamientos relacionados con los receptores de estrogenos - Google Patents

Compuestos esteroides 16 alfa-sustituidos para el uso en tratamientos relacionados con los receptores de estrogenos

Info

Publication number
AR029989A1
AR029989A1 ARP010103558A ARP010103558A AR029989A1 AR 029989 A1 AR029989 A1 AR 029989A1 AR P010103558 A ARP010103558 A AR P010103558A AR P010103558 A ARP010103558 A AR P010103558A AR 029989 A1 AR029989 A1 AR 029989A1
Authority
AR
Argentina
Prior art keywords
strogen
alfa
substitutes
receivers
substituted
Prior art date
Application number
ARP010103558A
Other languages
English (en)
Inventor
Jordi Mestres
Hubert Jan Jozef Loozen
Gerrit Herman Veeneman
Original Assignee
Adam Worrall Julia
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 Adam Worrall Julia filed Critical Adam Worrall Julia
Publication of AR029989A1 publication Critical patent/AR029989A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0081—Substituted in position 17 alfa and 17 beta
    • C07J1/0088—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being an unsaturated hydrocarbon group
    • C07J1/0096—Alkynyl derivatives
    • 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
    • A61P15/18—Feminine contraceptives
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005—Oxygen-containing hetero ring
    • C07J71/001—Oxiranes

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Compuesto esteroide 16alfa-sustituidos que tiene la formula (1), donde el anillo de líneas de puntos es un anillo totalmente saturado, un anillo totalmente aromático o un anillo saturado con un doble enlace delta5-10; R1 es alquilo C1-3 o alquenilo C2-3, y cada uno de estos grupos puede estar sustituido con uno o más halogenos; R2 es alquilo C1-4, alquenilo C2-4, o metileno, y cada uno de estos grupos puede estar sustituido con uno o más halogenos; R3 es metilo o etilo; o un profármaco del mismo, cuyo compuesto puede usarse para un tratamiento selectivo para los receptores de estrogenos alfa.
ARP010103558A 2000-07-28 2001-07-26 Compuestos esteroides 16 alfa-sustituidos para el uso en tratamientos relacionados con los receptores de estrogenos AR029989A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP00202697 2000-07-28

Publications (1)

Publication Number Publication Date
AR029989A1 true AR029989A1 (es) 2003-07-23

Family

ID=8171866

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP010103558A AR029989A1 (es) 2000-07-28 2001-07-26 Compuestos esteroides 16 alfa-sustituidos para el uso en tratamientos relacionados con los receptores de estrogenos

Country Status (25)

Country Link
US (2) US7696190B2 (es)
EP (1) EP1307471B1 (es)
JP (1) JP2004505093A (es)
KR (1) KR20030029640A (es)
CN (1) CN1220696C (es)
AR (1) AR029989A1 (es)
AT (1) ATE294812T1 (es)
AU (2) AU2001282016B2 (es)
BR (1) BR0112791A (es)
CA (1) CA2416311C (es)
CZ (1) CZ2003270A3 (es)
DE (1) DE60110606T2 (es)
EC (1) ECSP034448A (es)
ES (1) ES2241854T3 (es)
HR (1) HRP20030060A2 (es)
HU (1) HUP0301592A2 (es)
IL (2) IL153934A0 (es)
IS (1) IS6692A (es)
MX (1) MXPA03000845A (es)
NO (1) NO20030419L (es)
PE (1) PE20020331A1 (es)
PL (1) PL366235A1 (es)
SK (1) SK882003A3 (es)
WO (1) WO2002010188A1 (es)
ZA (1) ZA200300417B (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS51490B (sr) * 2002-01-21 2011-04-30 N.V. Organon POSTUPAK ZA IZRADU 7α-METILSTEROIDA
DE10213371C1 (de) * 2002-03-21 2003-12-24 Schering Ag Verfahren zur Herstellung von 7alpha-Methylsteroiden
CN101014610B (zh) * 2004-09-08 2012-08-22 Msd欧斯股份有限公司 具有选择性雌激素活性的15β-取代的类固醇
UA89964C2 (ru) * 2004-09-08 2010-03-25 Н.В. Органон 15β-ЗАМЕЩЕННЫЕ СТЕРОИДЫ, КОТОРЫЕ ИМЕЮТ СЕЛЕКТИВНУЮ ЭСТРОГЕННУЮ АКТИВНОСТЬ
CN114409717B (zh) * 2021-12-17 2023-03-17 湖南科益新生物医药有限公司 替勃龙中间体醚化物和替勃龙的制备方法

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1084261B (de) * 1957-04-11 1960-06-30 Syntex Sa Verfahren zur Herstellung neuer Cyclopentanophenanthrenderivate
NL226738A (es) * 1957-04-11
US3257429A (en) * 1957-11-12 1966-06-21 Syntex Corp 16-methylene derivatives of estrone and estradiol
US3007946A (en) * 1958-11-06 1961-11-07 Searle & Co 3-alkoxy-16-methylene-1, 3, 5(10)-estratrien-17-ones
US3049555A (en) * 1959-12-22 1962-08-14 Searle & Co 3-alkoxy-16-methyl-1, 3, 5 (10)-estratrien-17-ones
US3092645A (en) * 1961-12-28 1963-06-04 Searle & Co Esters of 17alpha-alkynylester-5(10)-ene-3beta, 17beta-diols
GB1112840A (en) 1964-04-07 1968-05-08 Res Inst Medicine Chem Steroids having pro-oestrogenic activity
US3299108A (en) * 1965-10-18 1967-01-17 Searle & Co 17alpha-alkynyl/alkenyl-13beta-alkyl-11-alkylgona-1, 3, 5 (10)-triene-3, 17beta-diols, ethers and esters thereof and intermediates thereto
US3465010A (en) 1966-11-22 1969-09-02 Searle & Co 17 - (unsaturated hydrocarbon - substituted) 11,13beta - dialkylgon -4 - ene - 3,17beta-diols and esters thereof
US3377366A (en) * 1966-12-02 1968-04-09 Searle & Co 17alpha-alkynyl/alkenyl-11, 13beta-dialkylgon-5(10)-en-3-ones and esters thereof
ZA712312B (en) 1970-04-28 1972-01-26 Ochsner Med Found Alton 4,14-estradiene compounds
US3652606A (en) 1970-08-07 1972-03-28 Searle & Co 3-oxygenated 11beta-methylestr-4-en-17beta-ol and esters thereof
US3704253A (en) * 1970-09-23 1972-11-28 American Home Prod 13 - polycarbonalkyl - 16 - methylgona-1,3,5(10)-trienes and 13-polycarbonalkyl-16-methylgon - 4 - en-3-ones and intermediates for their production
FR2377419A1 (fr) * 1977-01-13 1978-08-11 Roussel Uclaf Nouveaux derives steroides 11b-substitues 1,3,5 (10) trieniques, leur procede de preparation et leur application comme medicament
DE2757157C3 (de) 1977-12-19 1980-10-09 Schering Ag, 1000 Berlin Und 4619 Bergkamen Verfahren zur Herstellung von 16 a -alkylierten Steroiden
AU572589B2 (en) 1983-12-14 1988-05-12 Upjohn Company, The 11(alpha)-difluoromethyl and (e)-and (z)-11-fluoromethylene steroids
US5116830A (en) * 1984-08-17 1992-05-26 Sri International Stereoisomerically pure 17α-ethynyl-estra-2-en-17β-ol and the 17β esters thereof, methods of preparation and uses
DE3822770A1 (de) * 1988-07-01 1990-01-04 Schering Ag 13-alkyl-11ss-phenylgonane
ZA94715B (en) 1993-02-08 1994-10-24 Akzo Nv Steroids for treating menopausal complaints
ATE180669T1 (de) 1993-03-05 1999-06-15 Akzo Nobel Nv Verwendung von pregnanderivaten zur behandlung von tumoren
TR200002593T2 (tr) 1998-03-09 2000-12-21 Akzo Nobel N.V. Yeni bir gebelik önleme kiti
TR200003743T2 (tr) * 1998-06-19 2001-07-23 Akzo Nobel N.V. Testosteron türevi.
EP1131336B1 (en) 1998-11-20 2002-08-28 Akzo Nobel N.V. Estrogenic estra-1,3,5(10)-trienes with differential effects on the alpha and beta estrogen receptors, having a linear hydrocarbon chain of from 5-9 carbon atoms in position 11
TW548277B (en) * 1999-07-16 2003-08-21 Akzo Nobel Nv Orally active androgens
TR200200575T2 (tr) * 1999-09-06 2002-06-21 Akzo Nobel N. V. 11 Konumunda bir hidrokarbon ikame ediciye sahip, aromatik olmayan östrojenik steroidler.

Also Published As

Publication number Publication date
US7696190B2 (en) 2010-04-13
SK882003A3 (en) 2003-07-01
US20040043976A1 (en) 2004-03-04
ATE294812T1 (de) 2005-05-15
AU2001282016B2 (en) 2005-11-10
US20100029603A1 (en) 2010-02-04
EP1307471B1 (en) 2005-05-04
MXPA03000845A (es) 2004-04-05
JP2004505093A (ja) 2004-02-19
PE20020331A1 (es) 2002-04-30
DE60110606D1 (de) 2005-06-09
CZ2003270A3 (cs) 2003-06-18
CN1220696C (zh) 2005-09-28
IS6692A (is) 2003-01-20
PL366235A1 (en) 2005-01-24
HUP0301592A2 (hu) 2003-09-29
ECSP034448A (es) 2003-03-10
CA2416311A1 (en) 2002-02-07
HRP20030060A2 (en) 2004-06-30
IL153934A0 (en) 2003-07-31
NO20030419D0 (no) 2003-01-27
CN1444596A (zh) 2003-09-24
BR0112791A (pt) 2003-06-24
CA2416311C (en) 2009-04-28
AU8201601A (en) 2002-02-13
EP1307471A1 (en) 2003-05-07
DE60110606T2 (de) 2005-12-01
ES2241854T3 (es) 2005-11-01
KR20030029640A (ko) 2003-04-14
ZA200300417B (en) 2004-04-15
WO2002010188A1 (en) 2002-02-07
IL153934A (en) 2007-07-24
NO20030419L (no) 2003-01-27

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