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AR042046A1 - Inhibidores de 17 beta-hidroxiesteroide deshidrogenasa de tipo 3 para el tratamiento de enfermedades que dependen de androgenos - Google Patents

Inhibidores de 17 beta-hidroxiesteroide deshidrogenasa de tipo 3 para el tratamiento de enfermedades que dependen de androgenos

Info

Publication number
AR042046A1
AR042046A1 ARP030104210A ARP030104210A AR042046A1 AR 042046 A1 AR042046 A1 AR 042046A1 AR P030104210 A ARP030104210 A AR P030104210A AR P030104210 A ARP030104210 A AR P030104210A AR 042046 A1 AR042046 A1 AR 042046A1
Authority
AR
Argentina
Prior art keywords
aryl
heteroaryl
heteroaralkyl
aralkyl
alkyl
Prior art date
Application number
ARP030104210A
Other languages
English (en)
Original Assignee
Schering Corp
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 Corp filed Critical Schering Corp
Publication of AR042046A1 publication Critical patent/AR042046A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/46Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/12Keratolytics, e.g. wart or anti-corn preparations
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • 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
    • A61P5/28Antiandrogens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56Nitrogen atoms
    • C07D211/58Nitrogen atoms attached in position 4

Landscapes

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

Abstract

Inhibidores de 17beta-hidroxiesteroide deshidrogenasa de tipo 3, métodos para preparar dichos compuestos, composiciones farmacéuticas que contienen uno o más de dichos compuestos, métodos de preparación de formulaciones farmacéuticas que comprende uno o más de dichos compuestos, y métodos de tratamiento , prevención, inhibición o mejoramiento de una o más enfermedades asociadas con 17beta-hidroxiesteroide deshidrogenasa de tipo 3, usando dichos compuestos o composiciones farmacéuticas. Reivindicación 1: Un compuesto representado por la fórmula estructural (1), en la cual: X es CH o N; Z es O o N(R6); R1 y R2 son iguales o diferentes, estando cada uno de ellos independientemente seleccionado del grupo que consiste en arilo, heteroarilo, aralquilo y heteroaralquilo, donde cada uno de dichos arilo, heteroarilo, aralquilo y heteroaralquilo pueden estar no sustituidos o pueden estar opcionalmente independientemente sustituidos con una o más porciones que pueden ser iguales o diferentes, estando cada uno de las porciones independientemente seleccionados del grupo que consiste en halógeno, alquilo, arilo, heteroarilo, aralquilo, heteroaralquilo, cicloalquilo, heterociclilo, CF3, CN, -OCF3, -OR6, -C(O)R7, -NR6R7, -C(O)OR6, -C(O)NR6R7, -SR6, -S(O2)R7, -S(O2)NR6R7, -N(R6)S(O2)R7, -N(R6)C(O)R7 y -N(R6)C(O)NR6R7; R3 es H o -OR6, con la condición de que cuando X es N, R3 no es -OR6; R4 está seleccionado del grupo que consiste en H, alquilo, arilo, cicloalquilo, aralquilo, heteroarilo, heteroaralquilo, y heterociclilo, m es un número de 0 a 4, y cuando m es más de 1, los grupos R4 pueden ser iguales o diferentes y están independientemente seleccionados; R5 es -C(O)R7 o -S(O2)R7; R6 está seleccionado del grupo que consiste en H, alquilo, arilo, heteroarilo, aralquilo, heteroaralquilo, cicloalquilo y heterociclilo, donde cada uno de dichos alquilo, arilo, heteroarilo, aralquilo, heteroaralquilo, cicloalquilo y heterociclilo, pueden estar no sustituidos o pueden estar opcionalmente independientemente sustituidos con una o más porciones que pueden ser iguales o diferentes, donde cada porción está independientemente seleccionados del grupo que consiste en halógeno, alquilo, arilo, cicloalquilo, CF3, OCF3, CN, -OR7, -NHR7, -N(R7)2, -CH2OR7, -C(O)R7, -C(O)OR7, -C(O)NHR7, -C(O)N(R7)2, -SR7, -S(O2)R7, -S(O2)NHR7, -S(O2)N(R7)2, -N(R7)S(O2)R7, -N(R7)C(O)R7, -N(R7)C(O)NHR7 y -N(R7)C(O)N(R7)2; y R7 está seleccionado del grupo que consiste en alquilo, arilo, heteroarilo, aralquilo,. Heteroaralquilo, -OR6, -NHR6, y -N(R6)2, donde cada uno de dichos alquilo, heteroaralquilo, arilo, heteroarilo, y aralquilo pueden estar no sustituidos y puede estar opcionalmente sustituidos con una o más porciones que pueden ser iguales o diferentes, estando cada porción independientemente seleccionada del grupo que consiste en halógeno, alquilo, arilo, cicloalquilo, CF3, OCF3, CN, -OR6, -NHR6, -N(R6)2, -CH2OR6, -C(O)OR6, -C(O)NHR6, -C(O)N(R6)2, -SR6, -S(O2)R6, -S(O2)NHR6, -S(O2)N(R6)2, -N(R6)S(O2)R6, -N(R6)C(O)R6, -N(R7)C(O)NHR6 y -N(R7)C(O)N(R7)2, en el cual los dos grupos R6 o los dos grupos R7 en las porciones -N(R6)2 y -(N(R7)2, pueden ser respectivamente iguales o diferentes y estar independientemente seleccionados, en los cuales además los sustituyentes cualquiera adyacentes en un arilo o heteroarilo pueden estar unidos conjuntamente para formar un grupo metilendioxi o etilendioxi.
ARP030104210A 2002-11-18 2003-11-14 Inhibidores de 17 beta-hidroxiesteroide deshidrogenasa de tipo 3 para el tratamiento de enfermedades que dependen de androgenos AR042046A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US42726302P 2002-11-18 2002-11-18

Publications (1)

Publication Number Publication Date
AR042046A1 true AR042046A1 (es) 2005-06-08

Family

ID=32326512

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030104210A AR042046A1 (es) 2002-11-18 2003-11-14 Inhibidores de 17 beta-hidroxiesteroide deshidrogenasa de tipo 3 para el tratamiento de enfermedades que dependen de androgenos

Country Status (16)

Country Link
US (2) US7074795B2 (es)
EP (1) EP1562901B1 (es)
JP (2) JP4614770B2 (es)
CN (1) CN100374421C (es)
AR (1) AR042046A1 (es)
AT (1) ATE469886T1 (es)
AU (1) AU2003290799A1 (es)
CA (1) CA2506290C (es)
CL (1) CL2003002356A1 (es)
DE (1) DE60332862D1 (es)
ES (1) ES2345146T3 (es)
MX (1) MXPA05005360A (es)
MY (1) MY130792A (es)
PE (1) PE20040750A1 (es)
TW (1) TW200412964A (es)
WO (1) WO2004046111A1 (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60323765D1 (de) 2002-12-17 2008-11-06 Schering Corp Inhibitoren der 17 beta-hydroxysteroiddehydrogenase des typs 3 zur behandlung androgenabhängiger krankheiten
GB0513702D0 (en) 2005-07-04 2005-08-10 Sterix Ltd Compound
CA2606004A1 (en) * 2005-08-02 2007-02-08 Neurogen Corporation Dipiperazinyl ketones and related analogues
US8080540B2 (en) 2006-09-19 2011-12-20 Abbott Products Gmbh Therapeutically active triazoles and their use
US8288367B2 (en) 2006-11-30 2012-10-16 Solvay Pharmaceuticals Gmbh Substituted estratriene derivatives as 17BETA HSD inhibitors
US8501940B2 (en) * 2008-07-15 2013-08-06 Hoffmann-La Roche Inc. Tetrahydrocinnoline derivatives
PL2702982T3 (pl) * 2011-04-25 2017-07-31 Jun-Hyoung Park Kompozycja do miejscowego stosowania do zapobiegania wypadaniu włosów i stymulowania porostu włosów
AU2014300894A1 (en) 2013-06-25 2016-01-28 Forendo Pharma Ltd Therapeutically active 17-nitrogen substituted estratrienthiazole derivatives as inhibitors of 17.beta.-hydroxysteroid dehydrogenase
US10377791B2 (en) 2013-06-25 2019-08-13 Forendo Pharma Ltd. Therapeutically active estratrienthiazole derivatives as inhibitors of 17 B-hydroxysteroid dehydrogenase, type 1
WO2014207311A1 (en) 2013-06-25 2014-12-31 Forendo Pharma Ltd Therapeutically active estratrienthiazole derivatives as inhibitors of 17.beta.-hydroxy-steroid dehydrogenase, type 1
CN107207561B (zh) 2014-12-23 2020-03-31 佛恩多制药有限公司 17β-HSD1–抑制剂的前药
EP3237430B1 (en) 2014-12-23 2019-03-20 Forendo Pharma Ltd PRODRUGS OF 17ß -HSD1 -INHIBITORS
UY36875A (es) 2015-09-02 2017-03-31 Glaxosmithkline Intellectual Property (No 2) Ltd Composiciones inhibidoras de bromodominios para el tratamiento de diversas enfermedades
AU2018279205B2 (en) 2017-06-08 2021-04-15 Forendo Pharma Ltd 15.beta.-(3-propanamido)-substituted estra-1,3,5(10)-trien-17-one compounds and their 17-oximes for use in inhibition of 17.beta.-hydroxysteroid dehydrogenases
IL275337B2 (en) 2017-12-15 2024-06-01 Inthera Bioscience AG 1-(piperidinocarbonylmethyl)-2-oxopyrazine derivatives for cancer therapy
US20220041647A1 (en) 2018-12-05 2022-02-10 Forendo Pharma Ltd Estra-1,3,5(10)-triene compounds condensed in position 16(17) with a pyrazole ring as inhibitors of 17-hsd1

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DE3590389T1 (de) 1984-08-02 1986-08-28 Schering Corp., Kenilworth, N.J. Pharmazeutische Zusammensetzung für eine Kombinationstherapie hormon-abhängiger Cancer
ES2077675T3 (es) 1989-03-10 1995-12-01 Endorecherche Inc Terapia combinada para el tratamiento de enfermedades sensibles a los estrogenos.
ES2222633T3 (es) 1989-07-07 2005-02-01 Endorecherche Inc. Terapia combinada para la profilaxis y/o el tratamiento de la hiperplasia prostatica benigna.
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BR9908592A (pt) * 1998-03-11 2001-04-24 Endorech Inc Processo para inibir a atividade de 17ß-hidroxiesteróide desidrogenase tipo 5, composição farmacêutica, inibidor de 17ß-hidroxiesteróide desidrogenase tipo 5, processo para inibir 17ß-hidroxiesteróide desidrogenase tipo 3, inibidor de 17ß-hidroxiesteróide desidrogenase tipo 3, processos para tratar, ou reduzir o risco de desenvolver, câncer da próstata, hiperplasia prostática benigna, acne, seborréia, hirsutismo ou alopécia androgênica, sìndrome de ovário policìstico, câncer de mama, endometriose ou leiomioma, para inibir as secreções hormonais testiculares, para tratar puberdade precoce, e, kit
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JP4309761B2 (ja) * 2001-10-17 2009-08-05 シェーリング コーポレイション アンドロゲン依存性疾患の治療を目的とする17βヒドロキシステロイドデヒドロゲナーゼ3型の阻害剤としてのピペリジンアセトアミンおよびピペラジンアセトアミン

Also Published As

Publication number Publication date
CL2003002356A1 (es) 2005-02-11
CA2506290C (en) 2012-04-24
MXPA05005360A (es) 2005-08-03
CA2506290A1 (en) 2004-06-03
TW200412964A (en) 2004-08-01
JP4614770B2 (ja) 2011-01-19
WO2004046111A1 (en) 2004-06-03
CN100374421C (zh) 2008-03-12
EP1562901A1 (en) 2005-08-17
US7476681B2 (en) 2009-01-13
US20040127503A1 (en) 2004-07-01
MY130792A (en) 2007-07-31
ES2345146T3 (es) 2010-09-16
ATE469886T1 (de) 2010-06-15
PE20040750A1 (es) 2004-11-06
AU2003290799A1 (en) 2004-06-15
US20060148816A1 (en) 2006-07-06
JP2010138204A (ja) 2010-06-24
HK1073313A1 (en) 2005-09-30
CN1738800A (zh) 2006-02-22
DE60332862D1 (de) 2010-07-15
EP1562901B1 (en) 2010-06-02
US7074795B2 (en) 2006-07-11
JP2006513169A (ja) 2006-04-20

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