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AR042001A1 - Compuestos androgenos no esteroidales; composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento de trastornos relacionados con el receptor de androgeno. - Google Patents

Compuestos androgenos no esteroidales; composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento de trastornos relacionados con el receptor de androgeno.

Info

Publication number
AR042001A1
AR042001A1 ARP030104099A ARP030104099A AR042001A1 AR 042001 A1 AR042001 A1 AR 042001A1 AR P030104099 A ARP030104099 A AR P030104099A AR P030104099 A ARP030104099 A AR P030104099A AR 042001 A1 AR042001 A1 AR 042001A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
halogen
optionally substituted
androgen receptor
Prior art date
Application number
ARP030104099A
Other languages
English (en)
Inventor
Pedro Harold Han Hermkens
Herman Thijs Stock
Der Louw Jaap Van
Neeltje Miranda Teerhuis
Johannes Petrus Maria Lommerse
Original Assignee
Akzo Nobel 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
Application filed by Akzo Nobel Nv filed Critical Akzo Nobel Nv
Publication of AR042001A1 publication Critical patent/AR042001A1/es

Links

Classifications

    • 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
    • C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • 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
    • 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
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D409/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

Compuestos no esteroidales con afinidad por el receptor de andrógeno y de utilidad para tratamientos relacionados con el receptor de andrógeno que tienen una estructura de acuerdo con la fórmula (1) en que X es S, SO o SO2; R1 es una estructura de anillo de 5 o 6 miembros, monocíclico, hétero u homocíclico, saturado o no saturado, sustituidos opcionalmente con uno o más sustituyentes seleccionados del grupo que consiste en halógeno, CN, fluoroalquilo (C1-4), nitro, alquilo C1-4, alcoxi C1-4, fluoroalcoxi C1-4; R2 es 2-nitrofenilo, 2-cianofenilo, 2-hidroximetil-fenilo, 2-piridin-2-ilo, piridin-2-il-N-óxido, 2-benzamida, éster metílico de ácido 2-benzoico o 2-metoxifenilo; R3 es H, halógeno o alquilo C1-4; R4 es H, OH, alcoxi C1-4, o halógeno; R5 es H, OH, alcoxi C1-4, NH2, CN, halógeno, fluoroalquilo C1-4, NO2, hidroxialquilo C1-4, CO2H, CO2 alquilo C1-6, o R5 es NHR6, en que R6 es acilo C1-6, sustituido opcionalmente con uno o más halógenos, S(O)2 alquilo C1-4 o S(O)2arilo sustituido opcionalmente con alquilo C1-4 o uno o más halógenos, o R5 es C(O)N(R8,R9), en que R8 y R9 cada uno es independientemente H. cicloalquilo C3-6, o CH2R10 en que R10 es H, alquilo C1-5, alquenilo C1-5, hidroxialquilo C1-3, alquil C1-4, éster de carboxialquilo C1-4, alcoxi (C1-3)alquilo C1-3, (mono- o di alquil(C1-4))aminometilo, (mono o di alquil(C1-4))aminocarbonilo, o un anillo de 3, 4, 5 o 6 miembros, monocíclico, homo o heterocíclico, aromático o no aromático, o R8 y R9 forman junto con el N un anillo heterocíclico de 5 o 6 miembros, saturado o no saturado sustituido opcionalmente con alquilo C1-4, o una sal o un hidrato de éstos, composiciones farmacéuticas que los contienen y uso de estos compuestos para preparar medicamentos.
ARP030104099A 2002-11-07 2003-11-07 Compuestos androgenos no esteroidales; composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento de trastornos relacionados con el receptor de androgeno. AR042001A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US42457902P 2002-11-07 2002-11-07
EP02079648 2002-11-07

Publications (1)

Publication Number Publication Date
AR042001A1 true AR042001A1 (es) 2005-06-08

Family

ID=32313841

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030104099A AR042001A1 (es) 2002-11-07 2003-11-07 Compuestos androgenos no esteroidales; composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento de trastornos relacionados con el receptor de androgeno.

Country Status (15)

Country Link
US (2) US7795280B2 (es)
KR (1) KR20050072812A (es)
AR (1) AR042001A1 (es)
CL (1) CL2003002243A1 (es)
CO (1) CO5580758A2 (es)
DE (1) DE60332769D1 (es)
EC (1) ECSP055782A (es)
EG (1) EG24959A (es)
HR (1) HRP20050396A2 (es)
IS (1) IS2700B (es)
LV (1) LV13359B (es)
MX (1) MXPA05004929A (es)
NO (1) NO329778B1 (es)
PE (1) PE20040788A1 (es)
ZA (1) ZA200503559B (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200602317A (en) * 2004-04-23 2006-01-16 Akzo Nobel Nv Novel androgens
RU2008127501A (ru) * 2006-01-13 2010-02-20 Вайет (Us) Сульфонилзамещенные 1н-индолы в качастве лигандов 5-гидрокситриптаминовых рецепторов
DE102006014324B4 (de) * 2006-03-23 2009-01-08 Bayer Schering Pharma Aktiengesellschaft Inhibitoren der löslichen Adenylatzyklase
ES2981967T3 (es) 2017-01-05 2024-10-14 Radius Pharmaceuticals Inc Formas polimórficas de RAD1901-2HCl
WO2020010216A1 (en) 2018-07-04 2020-01-09 Radius Pharmaceuticals, Inc. Polymorphic forms of rad 1901-2hcl
PH12021551950A1 (en) 2019-02-12 2022-05-23 Radius Pharmaceuticals Inc Processes and compounds

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NZ179580A (en) 1974-12-30 1978-04-03 Mcneilab Inc 2-or 3-(w-tertiaryaminoalkyl)-thioindoles and the corresponding sulfinyl and sulfonyl analogs
US4059583A (en) * 1975-11-13 1977-11-22 Mcneil Laboratories, Incorporated Substituted indoles
JPS63313770A (ja) 1987-06-16 1988-12-21 Sumitomo Chem Co Ltd イサチン誘導体、その製造法およびそれを有効成分とする除草剤
ES2054784T3 (es) 1987-08-08 1994-08-16 Akzo Nv Un metodo para la fabricacion de un implante.
DE3924052A1 (de) 1989-07-21 1991-01-24 Bayer Ag N- (indol-6-yl)-heterocyclen
EP0490996A4 (en) 1989-09-08 1992-08-05 Institute Of Textile Technology Method and apparatus for modifying spun textile yarn
FR2662713B1 (fr) * 1990-05-29 1994-04-08 Oreal Procede de teinture de fibres keratiniques avec un aminoindole associe a un derive quinonique.
US5938792A (en) * 1991-04-18 1999-08-17 L'oreal Process for dyeing keratinous fibers with aminoindoles and oxidation dye precursors at basic Ph's and dyeing agents
FR2675380A1 (fr) 1991-04-18 1992-10-23 Oreal Procede de teinture des fibres keratiniques avec des aminoindoles, a ph basique, compositions mises en óoeuvre et nouveaux composes.
GB9204365D0 (en) * 1992-02-28 1992-04-08 Pfizer Ltd Indoles
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CZ180599A3 (cs) 1996-11-25 1999-11-17 The Procter & Gamble Company 2-Imidazolinylaminoindolová sloučenina, farmaceutický prostředek ji obsahující a její použití
US5969155A (en) * 1997-04-11 1999-10-19 The United States Of America As Represented By The Secretary Of The Army Conversion of trinitrotoluene into high value compounds
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TW200602317A (en) 2004-04-23 2006-01-16 Akzo Nobel Nv Novel androgens

Also Published As

Publication number Publication date
ECSP055782A (es) 2005-08-11
NO20052012L (no) 2005-05-26
CO5580758A2 (es) 2005-11-30
LV13359B (en) 2006-03-20
CL2003002243A1 (es) 2005-01-14
PE20040788A1 (es) 2004-12-10
HK1078875A1 (en) 2006-03-24
US20060128722A1 (en) 2006-06-15
EG24959A (en) 2011-02-18
IS7804A (is) 2005-04-18
US7795280B2 (en) 2010-09-14
ZA200503559B (en) 2006-08-30
IS2700B (is) 2010-11-15
US8124647B2 (en) 2012-02-28
MXPA05004929A (es) 2005-08-18
KR20050072812A (ko) 2005-07-12
NO329778B1 (no) 2010-12-13
US20110065768A1 (en) 2011-03-17
DE60332769D1 (de) 2010-07-08
HRP20050396A2 (en) 2005-06-30

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