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AR021757A1 - METHOD FOR INHIBITING THE CONVERSION OF 4-ANDROSTAN-3,17-DIONA IN TESTOSTERONE OR 3ALFA-ANDROSTAN-3,17-DIONA IN DIHYDROTESTOSTERONE, INHIBIT THE ACTIVITY OF 3ALFA-HYDROXYSTEROID DEHYDROGENASE OF TYPE 3 OF HIFTIVA OF TYPE 3 PUTATIVE INHIBITOR OF THE CONVERSION OF 4-ANDROSTEN-3 - Google Patents

METHOD FOR INHIBITING THE CONVERSION OF 4-ANDROSTAN-3,17-DIONA IN TESTOSTERONE OR 3ALFA-ANDROSTAN-3,17-DIONA IN DIHYDROTESTOSTERONE, INHIBIT THE ACTIVITY OF 3ALFA-HYDROXYSTEROID DEHYDROGENASE OF TYPE 3 OF HIFTIVA OF TYPE 3 PUTATIVE INHIBITOR OF THE CONVERSION OF 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
Spanish (es)
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/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • A61K31/566Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • A61K31/568Compounds 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
    • A61K31/5685Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A61K31/585Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/08Antiseborrheics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P5/26Androgens

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

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 3alfaMethod for inhibiting the conversion of 4-androstan-3,17-dione in testosterone or 3alpha-androstan-3,17-dione in dihydrotestosterone in a patient who needs said inhibition comprising the administration to said patient of a therapeutically effective amount of a human type 3 alpha-hydroxysteroid dehydrogenase inhibitor. The human type 3 3-alpha-hidoxysteroid dehydrogenase inhibitor that has the following structure: 1 where the dotted line is an optional pi bond; where R3 is a portion selected from the group consisting of C1-20-alkyloxy, C1-10-acyloxy, C1-20-alkoxycarbonyloxy, C1-20-alkyloxyalkyloxy, hydroxy, (N-alkyl or -H) -carbamate and a transformed group in vivo in hydroxyl; where R2 and R4 are independently selected from the group consisting of hydrogen, cyano, fluoro, chloro, bromo and nitro (where R2 and R4 are not hydrogen simultaneously); where R17alpha is selected from the group consisting of hydrogen, a carbonized portion of C2-14 substituted by a radical selected from the group consisting of hydrogen, halogen, carboxyl, amide, C1-3-alkoxy, C1-3-alkyl and phenyl substituted with R100, where R100 is selected from the group consisting of hydrogen, carboxyl, amide, C1-5-alkyl, halo, nitro, hydroxyl and C1-3-alkoxy; or R17alfa and R18beta together form a C5-7-lactone ring or is a ketone oxygen; where R17beta is hydroxy, acyloxy, alkoxy, alkenyloxy, (N-alkyl or H); or R17alfa and R17beta together form a C5-7-lactone ring or is a ketone oxygen; where R16alfa and R16beta are independently selected from the group consisting of hydrogen, lower alkyl and benzyl; or R16alfa and R16beta together form C5-6-cycloalkene. Method of treatment and / or inhibition of the development of prostate cancer, benign prostatic hyperplasia, prostatitis, cne, seborrhea, hirsutism or androgenic alopecia in which inhibitors of 3 -alpha hydroxysteroid dehydrogenase type 3, alone or in combination with other active drugs such as inhibitors of 17beta-dehydrogenase type 5. An inhibitor of 3alpha-hydroxysteroid dehydrogenase type 5. An inhibitor of 3alpha

ARP990103961A 1998-08-07 1999-08-06 METHOD FOR INHIBITING THE CONVERSION OF 4-ANDROSTAN-3,17-DIONA IN TESTOSTERONE OR 3ALFA-ANDROSTAN-3,17-DIONA IN DIHYDROTESTOSTERONE, INHIBIT THE ACTIVITY OF 3ALFA-HYDROXYSTEROID DEHYDROGENASE OF TYPE 3 OF HIFTIVA OF TYPE 3 PUTATIVE INHIBITOR OF THE CONVERSION OF 4-ANDROSTEN-3 AR021757A1 (en)

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 (en) 2002-08-07

Family

ID=22252842

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP990103961A AR021757A1 (en) 1998-08-07 1999-08-06 METHOD FOR INHIBITING THE CONVERSION OF 4-ANDROSTAN-3,17-DIONA IN TESTOSTERONE OR 3ALFA-ANDROSTAN-3,17-DIONA IN DIHYDROTESTOSTERONE, INHIBIT THE ACTIVITY OF 3ALFA-HYDROXYSTEROID DEHYDROGENASE OF TYPE 3 OF HIFTIVA OF TYPE 3 PUTATIVE INHIBITOR OF THE CONVERSION OF 4-ANDROSTEN-3

Country Status (9)

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

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* Cited by examiner, † Cited by third party
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US5504074A (en) 1993-08-06 1996-04-02 Children's Medical Center Corporation Estrogenic compounds as anti-angiogenic agents
US6908910B2 (en) 1993-08-06 2005-06-21 The Children's Medical Center Corporation Estrogenic compounds as anti-mitotic 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
US6995278B2 (en) 2000-08-18 2006-02-07 Entre Med, Inc. Antiangiogenic agents
US7135581B2 (en) 2000-08-18 2006-11-14 Entremed, Inc. Antiangiogenic agents
AU8838601A (en) * 2000-11-27 2002-06-03 Entremed Inc Antiangiogenic agents
US6710037B2 (en) * 2001-05-01 2004-03-23 Schering Corporation Method of treating androgen-dependent disorders
JP2003137814A (en) * 2001-08-10 2003-05-14 Takeda Chem Ind Ltd COMBINED PHARMACEUTICAL OF GnRH AGONIST
DK1666033T3 (en) * 2001-11-29 2009-04-06 Gtx Inc Prevention and treatment of osteoporosis caused by androgen deficiency
US7524866B2 (en) 2001-11-29 2009-04-28 Gtx, Inc. Prevention and treatment of androgen—deprivation induced osteoporosis
WO2005030120A2 (en) 2003-05-28 2005-04-07 Entremed, Inc. Antiangiogenic agents
EP1756139A4 (en) 2004-03-12 2009-07-29 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 (en) * 2004-07-02 2006-01-26 Schering Ag New 2-substituted Estra-1,3,5 (10) -triene-17-ones as inhibitors of 17β-hydroxysteroid dehydrogenase type 1
CA2646065C (en) 2006-03-20 2014-01-14 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
DK2181990T3 (en) * 2007-08-31 2012-09-10 Astellas Pharma Inc piperidine
CN101698834B (en) * 2009-09-08 2012-05-23 北京利德曼生化股份有限公司 3 alpha-hydroxysteroid dehydrogenase and nucleotide sequence, recombinant vector, recombinant host cell and kit thereof
KR20150036319A (en) * 2012-07-10 2015-04-07 바이엘 파마 악티엔게젤샤프트 3-substituted estra-1,3,5(10),16-tetraene derivatives, methods for the production thereof, pharmaceutical preparations containing same, and use thereof for the production of medicaments
HK1211592A1 (en) 2013-02-21 2016-05-27 拜耳医药股份公司 Estra-1,3,5(10),16-tetraene-3-carboxamides for inhibition of 17.beta.-hydroxysteroid dehydrogenase (akr1 c3)
CN104873525A (en) * 2014-02-27 2015-09-02 天津药物研究院 11 beta-hydroxysteroid dehydrogenase inhibitor and its pharmaceutical composition and use
CN104873520A (en) * 2014-02-27 2015-09-02 天津药物研究院 11 beta-hydroxysteroid dehydrogenase inhibitor and its pharmaceutical composition and use

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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
AU556749B2 (en) * 1983-02-22 1986-11-20 Liehr, J.G. Pharmaceutical compositions of 2-fluoroestradiol
US4568673A (en) * 1984-03-20 1986-02-04 Wayne State University Compositions inhibiting murine MXT ductal carcinoma
US5504074A (en) * 1993-08-06 1996-04-02 Children's Medical Center Corporation Estrogenic compounds as anti-angiogenic agents
TR200002784T2 (en) * 1998-03-11 2000-12-21 Endorecherche, Inc Type 5 and type 3 17beta-Hydroxysteroid dehydrogenase inhibitors and methods for their use

Also Published As

Publication number Publication date
CA2339368A1 (en) 2000-02-17
AU5144999A (en) 2000-02-28
CN1322130A (en) 2001-11-14
EP1102582A2 (en) 2001-05-30
JP2002522380A (en) 2002-07-23
WO2000007576A3 (en) 2000-03-30
NO20010651L (en) 2001-04-05
WO2000007576A2 (en) 2000-02-17
ID28791A (en) 2001-07-05
NO20010651D0 (en) 2001-02-07

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