AR073282A1 - Compuestos de imidazolidina como moduladores del receptor de androgenos - Google Patents

Compuestos de imidazolidina como moduladores del receptor de androgenos

Info

Publication number
AR073282A1
AR073282A1 ARP090103461A ARP090103461A AR073282A1 AR 073282 A1 AR073282 A1 AR 073282A1 AR P090103461 A ARP090103461 A AR P090103461A AR P090103461 A ARP090103461 A AR P090103461A AR 073282 A1 AR073282 A1 AR 073282A1
Authority
AR
Argentina
Prior art keywords
halo
cyano
optionally substituted
alkyl
nitro
Prior art date
Application number
ARP090103461A
Other languages
English (en)
Original Assignee
Galapagos 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 Galapagos Nv filed Critical Galapagos Nv
Publication of AR073282A1 publication Critical patent/AR073282A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C07D233/60Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41661,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/72Two oxygen atoms, e.g. hydantoin
    • C07D233/74Two oxygen atoms, e.g. hydantoin with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to other ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/72Two oxygen atoms, e.g. hydantoin
    • C07D233/76Two oxygen atoms, e.g. hydantoin with substituted hydrocarbon radicals attached to the third ring carbon atom
    • C07D233/78Radicals substituted by oxygen atoms

Abstract

Composiciones farmacéuticas, para la prevencion y el tratamiento de una variedad de afecciones en mamíferos, incluido el ser humano, que incluyen, a modo de ejemplos no Iimitativos, caquexia, osteoporosis, sarcopenia, disminucion de la líbido y/o disfuncion sexual. Reivindicacion 1: Un compuesto de acuerdo con la formula (1) en donde X es O o s; R1 es H; o R1 se selecciona de alquilo C1-6, cicloalquilo C3-7, alquenilo C3-6, alquinilo C3-6 y acilo C1-6, cada uno de los cuales puede estar opcionalmente sustituido con ciano, uno o varios halo, hidroxilo o aIcoxi C1-6; R2a se selecciona de H, P(O)(OH)2 y C(O)(CH2)n1C(O)OH; o R2a se selecciona de acilo C1-6 y alqueniIo C3-6; cada uno de los cuales puede estar opcionalmente sustituido con arilo, amino o carboxi; n1 es 0, 1, 2, 3 o 4; cada R2b y R2c se selecciona independientemente de H y aIquilo C1-6, o R2b y R2c se pueden unir para formar un cicloalquilo C3-7; R3a es H, halo, ciano o nitro; o R3a es alquilo C1-6 opciorialmente sustituido con halo, ciano, nitro, hidroxilo o alcoxi C1-4; o R3a es amido opcionalmente sustituido con alquino C1-6; cada R3b es independientemente halo, ciano o nitro; o cada R3b es independientemente alquilo C1-6 opcionalmerte sustituido con ciano o halo; o cada R3b es amido opcionalmente sustituido con alquilo C1-6; cada R4a y R4b es independientemente H, halo. ciano, carboxi o nitro; a cada R4a y R4b se selecciona de alquilo C1-6 y alcoxi C1-6; cada uno de los cuales puede estar opcionalmente sustituido por uno o varios halo o alcoxi C1-6; o R4a y R4b se unen para formar un cicloalquilo de 5 o 6 miembros, heterocicloalquilo de 5 o 6 miembros, arilo de 5 o 6 miembros, o heteroarilo de 5 o 6 miembros; R4c es halo, ciano o nitro; y m1 es 0, 1 o 2; o sales farmacéuticamente aceptables, y los solvatos de los compuestos o los solvatos de sus sales farmacéuticamente aceptables; o sus estereoisomeros.
ARP090103461A 2008-09-11 2009-09-09 Compuestos de imidazolidina como moduladores del receptor de androgenos AR073282A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US19191808P 2008-09-11 2008-09-11
GB0900333.6A GB2463514C (en) 2008-09-11 2009-01-09 Imidazolidine compounds and uses therefor

Publications (1)

Publication Number Publication Date
AR073282A1 true AR073282A1 (es) 2010-10-28

Family

ID=40379370

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090103461A AR073282A1 (es) 2008-09-11 2009-09-09 Compuestos de imidazolidina como moduladores del receptor de androgenos

Country Status (20)

Country Link
US (2) US7968581B2 (es)
EP (1) EP2344460B1 (es)
JP (1) JP5595402B2 (es)
KR (1) KR101705157B1 (es)
CN (1) CN102149687B (es)
AR (1) AR073282A1 (es)
AU (1) AU2009290849B2 (es)
BR (1) BRPI0919290A2 (es)
CA (1) CA2736364C (es)
CO (1) CO6382130A2 (es)
ES (1) ES2552684T3 (es)
GB (1) GB2463514C (es)
HK (1) HK1141015A1 (es)
IL (1) IL211277A (es)
MX (1) MX2011002374A (es)
NZ (1) NZ591374A (es)
RU (1) RU2488584C2 (es)
TW (1) TWI449698B (es)
WO (1) WO2010029119A1 (es)
ZA (1) ZA201101707B (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8168667B2 (en) * 2006-05-31 2012-05-01 Galapagos Nv Imidazolidine derivatives, uses therefor, preparation thereof and compositions comprising such
CN103608333B (zh) 2011-03-10 2016-01-06 苏州开拓药业有限公司 雄激素受体拮抗剂及其用途
GB201311107D0 (en) * 2013-06-21 2013-08-07 Univ Edinburgh Bioorthogonal methods and compounds
ES2934319T3 (es) * 2013-07-18 2023-02-21 Baylor College Medicine Métodos y composiciones para el tratamiento de la atrofia muscular, la debilidad muscular y/o la caquexia
CN105979943A (zh) * 2013-10-25 2016-09-28 厄恩斯特.D.布什 肌营养不良的治疗方法
EP3089975B1 (en) * 2013-12-31 2018-06-06 Ipsen Pharma S.A.S. Novel imidazolidine-2, 4-dione derivatives
JP7028987B2 (ja) * 2017-12-06 2022-03-02 アイブライト メディカル テクノロジー (ペキン) カンパニー リミテッド オルソケラトロジーレンズおよびその製造方法
HUE059318T2 (hu) 2018-04-19 2022-11-28 Tvardi Therapeutics Inc STAT3 inhibitorok
US11026905B2 (en) 2018-04-19 2021-06-08 Tvardi Therapeutics, Inc. STAT3 inhibitors
CN115052584A (zh) 2020-01-24 2022-09-13 特维迪疗法公司 治疗性化合物及其制剂和用途
CN113024513A (zh) * 2021-03-22 2021-06-25 中国药科大学 新型雄激素受体降解剂、制备方法和医药用途
CN113801064A (zh) * 2021-09-26 2021-12-17 甘肃省化工研究院有限责任公司 一种[3+2]环加成反应构建苯基乙内酰脲的方法

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5136332B1 (es) * 1970-12-09 1976-10-07
GB1601310A (en) * 1978-05-23 1981-10-28 Lilly Industries Ltd Aryl hydantoins
DE2855770A1 (de) 1978-12-22 1980-07-10 Bayer Ag Hydantoine
US4753957A (en) 1981-09-28 1988-06-28 Rohm And Haas Company Substituted 2,4-imidazolidinediones and fungicidal compositions
EP0091596B1 (de) 1982-04-08 1991-09-11 Shell Internationale Researchmaatschappij B.V. Neue Hydantoine, ihre Herstellung und Verwendung
FR2619381B1 (fr) * 1987-08-13 1989-12-08 Roussel Uclaf Nouvelles imidazolidines substituees par un radical hydroxymethyle et un radical phenyl substitue, leur procede de preparation, leur application comme medicaments, les compositions pharmaceutiques les renfermant et un intermediaire pour leur preparation
JP2566792B2 (ja) 1987-09-30 1996-12-25 株式会社資生堂 発毛、養毛促進剤
JPH0219363A (ja) 1988-07-06 1990-01-23 Fujisawa Pharmaceut Co Ltd イミダゾリジン誘導体
US4992443A (en) 1990-03-12 1991-02-12 William Chelen Method of treating motion sickness
US5346913A (en) 1992-05-26 1994-09-13 Rohm And Haas Company N-iodopropargyl hydantoin compounds, compositions, preparation, and use as antimicrobial agents
JP3137430B2 (ja) 1992-06-10 2001-02-19 鐘淵化学工業株式会社 5,5−二置換ヒダントインの製造法
US6846525B2 (en) 1993-03-19 2005-01-25 Xerox Corporation Recording sheets containing purine, pyrimidine, benzimidazole, imidazolidine, urazole, pyrazole, triazole, benzotriazole, tetrazole, and pyrazine compounds
TW521073B (en) * 1994-01-05 2003-02-21 Hoechst Marion Roussel Inc New optionally substituted phenylimidazolidines, their preparation process, their use as anti-androgenic agent and the pharmaceutical compositions containing them
FR2715402B1 (fr) * 1994-01-05 1996-10-04 Roussel Uclaf Nouvelles phénylimidazolines éventuellement substituées, leur procédé et des intermédiaires de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant.
AU1884595A (en) 1994-04-29 1995-11-29 Pfizer Inc. Novel acyclic and cyclic amides as neurotransmitter release enhancers
EP0760239A3 (en) 1995-09-01 1999-04-14 Pfizer Inc. Therapeutic agents for use in cancer therapy
FR2741342B1 (fr) * 1995-11-22 1998-02-06 Roussel Uclaf Nouvelles phenylimidazolidines fluorees ou hydroxylees, procede, intermediaires de preparation, application comme medicaments, nouvelle utilisation et compositions pharmaceutiques
DE69811867T2 (de) 1997-03-03 2003-11-20 Boehringer Ingelheim Pharma Kleine moleküle anwendbar in der behandlung von entzündgskrankheiten
US6355664B1 (en) 1997-03-03 2002-03-12 Boehringer Ingelheim Pharmaceuticals, Inc. Phenylpyrrolidines, phenylimidazolidines, 3-phenyl-1,3-oxizolidines and 3-phenyl-1,3-thiazolidines and their use in the treatment of inflammatory disease
UA57081C2 (uk) 1997-06-16 2003-06-16 Пфайзер Продактс Інк. Фармацевтична композиція для лікування раку або доброякісних проліферативних хвороб у ссавців, спосіб лікування, фармацевтична композиція для інгібування ненормального росту клітин у ссавців та спосіб інгібування
US6492553B1 (en) 1998-01-29 2002-12-10 Aventis Pharamaceuticals Inc. Methods for preparing N-[(aliphatic or aromatic)carbonyl)]-2-aminoaetamide compounds and for cyclizing such compounds
DE19912383A1 (de) 1998-03-27 1999-09-30 Degussa Verfahren zur Herstellung von cyclischen 4-Oxoamidinen
DE60129222T2 (de) 2000-05-11 2008-03-06 Consejo Superior de Investigaciónes Científicas Heterocyclischen inhibitoren von glycogen synthase kinase gsk-3
US6846643B2 (en) 2000-08-14 2005-01-25 Boehringer Ingelheim Pharmaceuticals, Inc. Methods and molecules useful for identifying molecules that bind LFA-1 and for determining receptor occupancy
CN101056862B (zh) * 2004-09-10 2013-03-13 詹森药业有限公司 作为选择性雄激素受体调节剂(sarms)的咪唑烷-2-酮衍生物
WO2007047146A2 (en) 2005-10-11 2007-04-26 Intermune, Inc. Inhibitors of viral replication
GB0610765D0 (en) * 2006-05-31 2006-07-12 Proskelia Sas Imidazolidine derivatives, uses therefor, preparation thereof and compositions comprising such

Also Published As

Publication number Publication date
ZA201101707B (en) 2012-01-25
NZ591374A (en) 2012-07-27
US20120178718A1 (en) 2012-07-12
BRPI0919290A2 (pt) 2019-04-30
KR101705157B1 (ko) 2017-02-09
IL211277A (en) 2014-12-31
RU2011113749A (ru) 2012-10-20
HK1141015A1 (en) 2010-10-29
CA2736364A1 (en) 2010-03-18
CO6382130A2 (es) 2012-02-15
US20100113547A1 (en) 2010-05-06
MX2011002374A (es) 2011-04-11
AU2009290849B2 (en) 2015-04-02
GB2463514B (en) 2010-07-28
CN102149687A (zh) 2011-08-10
JP2012524708A (ja) 2012-10-18
GB0900333D0 (en) 2009-02-11
TW201016671A (en) 2010-05-01
WO2010029119A1 (en) 2010-03-18
EP2344460B1 (en) 2015-08-12
CN102149687B (zh) 2014-08-13
IL211277A0 (en) 2011-04-28
GB2463514A (en) 2010-03-17
AU2009290849A1 (en) 2010-03-18
KR20110067029A (ko) 2011-06-20
CA2736364C (en) 2018-06-26
EP2344460A1 (en) 2011-07-20
GB2463514C (en) 2018-09-26
TWI449698B (zh) 2014-08-21
ES2552684T3 (es) 2015-12-01
US8383608B2 (en) 2013-02-26
JP5595402B2 (ja) 2014-09-24
US7968581B2 (en) 2011-06-28
RU2488584C2 (ru) 2013-07-27

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