AR048643A1 - Derivados de indol como moduladores selectivos de los receptores androgenicos (sarms) - Google Patents

Derivados de indol como moduladores selectivos de los receptores androgenicos (sarms)

Info

Publication number
AR048643A1
AR048643A1 ARP050101746A ARP050101746A AR048643A1 AR 048643 A1 AR048643 A1 AR 048643A1 AR P050101746 A ARP050101746 A AR P050101746A AR P050101746 A ARP050101746 A AR P050101746A AR 048643 A1 AR048643 A1 AR 048643A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
halogen
group
alkyl
amino
Prior art date
Application number
ARP050101746A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34965787&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR048643(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR048643A1 publication Critical patent/AR048643A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
    • 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
    • A61P15/16—Masculine 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
    • A61P17/10—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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • 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
    • A61P5/28—Antiandrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • AIDS & HIV (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Furan Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente se refiere a derivados de indol como moduladores selectivos de los receptores androgénicos (SARMS), composiciones farmacéuticas que los contienen y su uso en el tratamiento de trastornos y afecciones moduladas por el receptor de androgenos. Reivindicacion 1: Un compuesto de formula (1) donde X se selecciona del grupo integrado por O, S y NR1; R1 se selecciona del grupo integrado por H, alquilo inferior, alquilo inferior fluorado, -SO2-(alquilo inferior), -SO2-fenilo, -SO2- tolilo, -(CH2)-(alquilo inferior fluorado), -(alquilo inferior)-CN, -(alquilo inferior)-C(O)-O-(alquilo inferior), -(alquilo inferior)-O-(alquilo inferior) y -(alquilo inferior)-S(O)0-2-(alquilo inferior); R4 se selecciona del grupo integrado por H, halogeno, alquilo inferior, alquenilo inferior, alquinilo inferior y ciano; donde el alquilo inferior, alquenilo inferior o alquinilo inferior están opcionalmente sustituidos sobre el átomo de C termal con -Si(alquilo inferior)3; a es un entero de 0 a 4; R5 se selecciona del grupo integrado por halogeno, hidroxi, carboxi, alquilo inferior, alquilo inferior sustituido con halogeno, alcoxi inferior, alcoxi inferior sustituido con halogeno, ciano, nitro, amino, alquilamino inferior, di(alquilo inferior)amino, -C(O)-(alquilo inferior), -C(O)-(alcoxi inferior), -C(O)-N(RA)2, -S(O)0-2-(alquilo inferior), -SO2-N(RA)2, -N(RA)-C(O)-(alquilo inferior), -N(RA)-C(O)-(alquilo inferior sustituido con halogeno) y arilo; donde cada RA se selecciona independientemente de H o alquilo inferior; donde el arilo está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halogeno, hidroxi, carboxi, alquilo inferior, alquilo inferior sustituido con halogeno, alcoxi inferior, alcoxi inferior sustituido con halogeno, ciano, nitro, amino, alquilamino inferior o di(alquilo inferior)amino; b es un entero de 0 a 1; c es un entero de 0 a 1; R7 se selecciona del grupo integrado por H, alquilo inferior y -Si(alquilo inferior)3; El anillo (A) es una estructura de anillo saturado o parcialmente insaturado de 4 a 7 miembros, que contiene 1 a 2 heteroátomos seleccionados de O, N o S; donde la estructura de anillo saturado o parcialmente insaturado de 4 a 7 miembros está opcionalmente sustituida con un sustituyente seleccionado de -(L1)0-1-R8; donde L1 se selecciona del grupo integrado por -(CH2)1-4-, -C(O)-, -C(O)-(CH2)1-4-, -C(O)O- y -C(O)O-(CH2)1-4; donde R8 se selecciona del grupo integrado por arilo y heteroarilo, donde el arilo o heteroarilo están opcionalmente sustituidos con uno o más sustituyentes seleccionados independientemente del grupo integrado por halogeno, hidroxi, carboxi, alquilo inferior, alquilo inferior sustituido con halogeno, alcoxi inferior, ciano, nitro, amino, alquilamino inferior, di(alquilo inferior)amino, -S(O)0-2-(alquilo inferior) y -SO2-N(RA)2; siempre que cuando X es NH o N(CH3), R4 es H, b es 0, c es 0, R7 es H o metilo y a es 0, entonces el anillo (A) es diferente de piperidinilo, donde el piperidinilo está opcionalmente sustituido con alquilo inferior o aralquilo; o su sal aceptable para uso farmacéutico.
ARP050101746A 2004-05-03 2005-05-02 Derivados de indol como moduladores selectivos de los receptores androgenicos (sarms) AR048643A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US56776304P 2004-05-03 2004-05-03
US11/096,664 US7282507B2 (en) 2004-05-03 2005-04-01 Indole derivatives as selective androgen receptor modulators (SARMS)

Publications (1)

Publication Number Publication Date
AR048643A1 true AR048643A1 (es) 2006-05-10

Family

ID=34965787

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050101746A AR048643A1 (es) 2004-05-03 2005-05-02 Derivados de indol como moduladores selectivos de los receptores androgenicos (sarms)

Country Status (10)

Country Link
US (1) US7282507B2 (es)
EP (1) EP1753749B1 (es)
JP (1) JP5070042B2 (es)
CN (1) CN1980917B (es)
AR (1) AR048643A1 (es)
AU (1) AU2005243240B2 (es)
CA (1) CA2564952A1 (es)
MY (1) MY142850A (es)
TW (1) TW200606146A (es)
WO (1) WO2005111028A1 (es)

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HUE029852T2 (en) 2004-03-15 2017-04-28 Janssen Pharmaceutica Nv Opioid receptor modulators
ES2371170T3 (es) * 2004-05-03 2011-12-28 Janssen Pharmaceutica Nv Derivados de benzofurano comomoduladores selectivos de receptores de andrógenos (msra).
CN101374808B (zh) * 2006-01-24 2011-05-25 伊莱利利公司 孕酮受体的吲哚磺酰胺调节剂
US8238515B2 (en) * 2007-08-16 2012-08-07 Caldera Pharmaceuticals, Inc. Well plate
MX2010009162A (es) 2008-02-22 2010-12-21 Radius Health Inc Moduladores selectivos del receptor de androgeno.
US8268872B2 (en) 2008-02-22 2012-09-18 Radius Health, Inc. Selective androgen receptor modulators
CA2788907A1 (en) 2010-02-04 2011-08-11 Radius Health, Inc. Selective androgen receptor modulators
PT2568806T (pt) 2010-05-12 2016-08-05 Radius Health Inc Regimes terapêuticos
US8642632B2 (en) 2010-07-02 2014-02-04 Radius Health, Inc. Selective androgen receptor modulators
ES2550319T3 (es) 2010-09-28 2015-11-06 Radius Health, Inc Moduladores selectivos del receptor de andrógenos
JP2015508414A (ja) * 2012-01-12 2015-03-19 イエール ユニバーシティ E3ユビキチンリガーゼによる標的タンパク質および他のポリペプチドの分解増強のための化合物および方法
HRP20180061T1 (hr) 2012-07-17 2018-02-23 Glaxosmithkline Intellectual Property (No. 2) Limited Indolkarbonitrili kao selektivni modulatori androgenskih receptora
RS67458B1 (sr) 2014-03-28 2025-12-31 Univ Duke Lečenje kancera dojke pozitivnog na receptor estrogena upotrebom selektivnih modulatora receptora estrogena
US9421264B2 (en) 2014-03-28 2016-08-23 Duke University Method of treating cancer using selective estrogen receptor modulators
RS63311B1 (sr) 2016-06-22 2022-07-29 Ellipses Pharma Ltd Ar+ metode lečenja raka dojke
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CN112423844B (zh) 2018-07-04 2024-08-13 雷迪厄斯制药公司 Rad1901-2hcl的多晶型形式
JOP20210218A1 (ar) 2019-02-12 2023-01-30 Radius Pharmaceuticals Inc عمليات ومركبات
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Also Published As

Publication number Publication date
EP1753749A1 (en) 2007-02-21
CN1980917B (zh) 2014-02-12
AU2005243240A1 (en) 2005-11-24
JP5070042B2 (ja) 2012-11-07
CA2564952A1 (en) 2005-11-24
US20050245485A1 (en) 2005-11-03
US7282507B2 (en) 2007-10-16
AU2005243240B2 (en) 2012-03-15
MY142850A (en) 2011-01-14
TW200606146A (en) 2006-02-16
CN1980917A (zh) 2007-06-13
EP1753749B1 (en) 2014-07-30
WO2005111028A1 (en) 2005-11-24
JP2007536227A (ja) 2007-12-13

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