AR021757A1 - Metodo para inhibir la conversion de 4-androstan-3,17-diona en testosterona o de 3alfa-androstan-3,17-diona en dihidrotestosterona, inhibir la actividadde la 3alfa-hidroxiesteroide deshidrogenasa de tipo 3 humana, para determinar la eficacia de un inhibidor putativo de la conversion de 4-androsten-3 - Google Patents

Metodo para inhibir la conversion de 4-androstan-3,17-diona en testosterona o de 3alfa-androstan-3,17-diona en dihidrotestosterona, inhibir la actividadde la 3alfa-hidroxiesteroide deshidrogenasa de tipo 3 humana, para determinar la eficacia de un inhibidor putativo de la conversion de 4-androsten-3

Info

Publication number
AR021757A1
AR021757A1 ARP990103961A ARP990103961A AR021757A1 AR 021757 A1 AR021757 A1 AR 021757A1 AR P990103961 A ARP990103961 A AR P990103961A AR P990103961 A ARP990103961 A AR P990103961A AR 021757 A1 AR021757 A1 AR 021757A1
Authority
AR
Argentina
Prior art keywords
group
type
hydrogen
androstan
alkyl
Prior art date
Application number
ARP990103961A
Other languages
English (en)
Original Assignee
Endorech 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 Endorech Inc filed Critical Endorech Inc
Publication of AR021757A1 publication Critical patent/AR021757A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/566—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol having an oxo group in position 17, e.g. estrone
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • A61K31/5685—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A61K31/585—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P17/08—Antiseborrheics
    • 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
    • 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
    • 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
    • A61P5/26—Androgens

Abstract

Método para inhibir la conversion de 4-androstan-3,17-diona en testosterona o de 3alfa-androstan-3,17-diona en dihidrotestosterona en un paciente quenecesita dicha inhibicion que comprende la administracion a dicho paciente de una cantidad terapéuticamente efectiva de un inhibidor de la 3 alfa-hidroxiesteroide deshidrogenasa de tipo 3 humana. El inhibidor de la 3alfa-hidoxiesteroide deshidrogenasa de tipo 3 humana que posee la siguiente estructura: 1donde la línea de puntos es un enlace pi optativo; donde R3 es una porcion seleccionada del grupo formado por C1-20-alquiloxi, C1-10-aciloxi,C1-20-alcoxicarboniloxi, C1-20-alquiloxialquiloxi, hidroxilo, (N-alquil o -H)-carbamato y un grupo transformado in vivo en hidroxilo; donde R2 y R4 seseleccionan independientemente del grupo formado por hidrogeno, ciano, fluoro, cloro, bromo y nitro (donde R2 y R4 no son hidrogeno simultáneamente); dondeR17alfa se selecciona del grupo formado por hidogeno, una porcion carbonada de C2-14 sustituida porun radical seleccionado del grupo formado por hidrogeno,halogeno, carboxilo, amida, C1-3-alcoxi, C1-3-alquilo y fenilo sustituido con R100, donde R100 se selecciona del grupo formado por hidrogeno, carboxilo, amida,C1-5-alquilo, halo, nitro, hidroxilo y C1-3-alcoxi; o R17alfa y R18beta forman juntos un anillo C5-7-lactona o es un oxígeno cetonico; donde R17beta eshidroxilo, aciloxi, alcoxi, alqueniloxi, (N-alquil o H); o R17alfa y R17beta forman juntos un anillo C5-7-lactona o es un oxígeno cetonico; donde R16alfa yR16beta se seleccionan independientemente del grupo formado por hidrogeno, alquilo inferior y bencilo; o R16alfa y R16beta forman juntos a C5-6-cicloalqueno.Método de tratamiento y/o inhibicion del desarrollo del cáncer de prostata, hiperplasia prostática benigna, prostatitis,a cné, seborrea, hirsutismo o alopecíaandrogénica en los que se utilizan inhibidores de la 3-alfa hidroxiesteroide deshidrogenasa de tipo 3, solos o en combinacion con otros fármacos activos talescomo los inhibidores de la 17beta-deshidrogenasa de tipo 5. Un inhibidor de la 3alfa-hidroxiesteroide deshidrogenasa de tipo 5. Un inhibidor de la 3alfa
ARP990103961A 1998-08-07 1999-08-06 Metodo para inhibir la conversion de 4-androstan-3,17-diona en testosterona o de 3alfa-androstan-3,17-diona en dihidrotestosterona, inhibir la actividadde la 3alfa-hidroxiesteroide deshidrogenasa de tipo 3 humana, para determinar la eficacia de un inhibidor putativo de la conversion de 4-androsten-3 AR021757A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US9562398P 1998-08-07 1998-08-07

Publications (1)

Publication Number Publication Date
AR021757A1 true AR021757A1 (es) 2002-08-07

Family

ID=22252842

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP990103961A AR021757A1 (es) 1998-08-07 1999-08-06 Metodo para inhibir la conversion de 4-androstan-3,17-diona en testosterona o de 3alfa-androstan-3,17-diona en dihidrotestosterona, inhibir la actividadde la 3alfa-hidroxiesteroide deshidrogenasa de tipo 3 humana, para determinar la eficacia de un inhibidor putativo de la conversion de 4-androsten-3

Country Status (9)

Country Link
EP (1) EP1102582A2 (es)
JP (1) JP2002522380A (es)
CN (1) CN1322130A (es)
AR (1) AR021757A1 (es)
AU (1) AU5144999A (es)
CA (1) CA2339368A1 (es)
ID (1) ID28791A (es)
NO (1) NO20010651L (es)
WO (1) WO2000007576A2 (es)

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US6908910B2 (en) 1993-08-06 2005-06-21 The Children's Medical Center Corporation Estrogenic compounds as anti-mitotic agents
US5504074A (en) 1993-08-06 1996-04-02 Children's Medical Center Corporation Estrogenic compounds as anti-angiogenic agents
EP1321146A3 (en) * 1998-03-11 2004-06-02 Endorecherche Inc. Inhibitors of type 5 and 3 17beta-hydroxysteroid dehydrogenase and methods for their use
US7087592B1 (en) 1999-08-23 2006-08-08 Entre Med, Inc. Compositions comprising purified 2-methoxyestradiol and methods of producing same
US6891953B1 (en) 2000-06-27 2005-05-10 Microsoft Corporation Method and system for binding enhanced software features to a persona
US7135581B2 (en) 2000-08-18 2006-11-14 Entremed, Inc. Antiangiogenic agents
US6995278B2 (en) * 2000-08-18 2006-02-07 Entre Med, Inc. Antiangiogenic agents
CA2430100A1 (en) * 2000-11-27 2002-05-30 Entremed, Inc. Antiangiogenic agents
US6710037B2 (en) * 2001-05-01 2004-03-23 Schering Corporation Method of treating androgen-dependent disorders
DE60239207D1 (de) * 2001-08-10 2011-03-31 Takeda Pharmaceutical Gnrh-agonistische kombinationsmittel
CN100548283C (zh) * 2001-11-29 2009-10-14 Gtx公司 雄激素剥夺引起的骨质疏松症的预防和治疗
US7524866B2 (en) 2001-11-29 2009-04-28 Gtx, Inc. Prevention and treatment of androgen—deprivation induced osteoporosis
CA2558014A1 (en) 2004-03-12 2005-09-29 Entremed, Inc. Antiangiogenic agents
US7419972B2 (en) 2004-07-02 2008-09-02 Schering Ag 2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of 17β-hydroxy steroid dehydrogenase type 1
DE102004032674A1 (de) * 2004-07-02 2006-01-26 Schering Ag Neue 2-substituierte Estra-1,3,5(10)-trien-17-one als Inhibitoren der 17β-Hydroxysteroiddehydrogenase Typ 1
US8399440B2 (en) 2006-03-20 2013-03-19 Entremed, Inc. Disease modifying anti-arthritic activity of 2-methoxyestradiol
US9284345B2 (en) * 2007-04-12 2016-03-15 Endorecherche, Inc. 17alpha-substituted steroids as systemic antiandrogens and selective androgen receptor modulators
WO2009028618A1 (ja) * 2007-08-31 2009-03-05 Astellas Pharma Inc. ピペリジン誘導体
CN101698834B (zh) * 2009-09-08 2012-05-23 北京利德曼生化股份有限公司 3α-羟基类固醇脱氢酶及其核苷酸序列、重组载体、重组宿主细胞和试剂盒
EA201500112A1 (ru) * 2012-07-10 2015-07-30 Байер Фарма Акциенгезельшафт 3-замещенные производные эстра-1,3,5(10),16-тетраена, способы их получения, фармацевтические средства, которые их содержат, и их использование для получения лекарственных средств
EP2958928B1 (de) * 2013-02-21 2018-03-28 Bayer Pharma Aktiengesellschaft Estra-1,3,5(10),16-tetraen-3-carboxamide zur inhibierung von 17.beta.-hydroxysteroid dehdrogenase (akr1c3)
CN104873520A (zh) * 2014-02-27 2015-09-02 天津药物研究院 一种11β-羟基类固醇脱氢酶抑制剂、药用组合物及其用途
CN104873525A (zh) * 2014-02-27 2015-09-02 天津药物研究院 一种11β-羟基类固醇脱氢酶抑制剂及其药用组合物和用途

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US3562260A (en) * 1965-08-23 1971-02-09 Ormonoterapia Richter Spa 2-carbonyl-estratrienes and method of their preparation
US4340602A (en) * 1978-10-18 1982-07-20 Wayne State University Compositions inhibiting estrogen sulfotransferase activity
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Also Published As

Publication number Publication date
JP2002522380A (ja) 2002-07-23
AU5144999A (en) 2000-02-28
NO20010651L (no) 2001-04-05
ID28791A (id) 2001-07-05
CN1322130A (zh) 2001-11-14
CA2339368A1 (en) 2000-02-17
WO2000007576A3 (en) 2000-03-30
WO2000007576A2 (en) 2000-02-17
EP1102582A2 (en) 2001-05-30
NO20010651D0 (no) 2001-02-07

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