BRPI0919290A2 - composto de imidazoldina com moduladores de receptor de androgênio, e composição farmacêutica - Google Patents

composto de imidazoldina com moduladores de receptor de androgênio, e composição farmacêutica

Info

Publication number
BRPI0919290A2
BRPI0919290A2 BRPI0919290-5A BRPI0919290A BRPI0919290A2 BR PI0919290 A2 BRPI0919290 A2 BR PI0919290A2 BR PI0919290 A BRPI0919290 A BR PI0919290A BR PI0919290 A2 BRPI0919290 A2 BR PI0919290A2
Authority
BR
Brazil
Prior art keywords
pharmaceutical composition
androgen receptor
receptor modulators
imidazoldine
compound
Prior art date
Application number
BRPI0919290-5A
Other languages
English (en)
Inventor
Nique François
Jagerschmidt Catherine
Blanqué Roland
Lefrançois Jean-Michel
Peixoto Christophe
Deprez Pierre
Triballeau Nicolas
Tom Bert Paul Wigerinck Piet
Sylvie Namour Florence
Original Assignee
Galapagos N.V.
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 N.V. filed Critical Galapagos N.V.
Publication of BRPI0919290A2 publication Critical patent/BRPI0919290A2/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic 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
    • C07D233/56—Heterocyclic 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
    • C07D233/60—Heterocyclic 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
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • 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
    • 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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • 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
    • 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
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic 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
    • C07D233/66—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic 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
    • C07D233/66—Heterocyclic 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
    • C07D233/72—Two oxygen atoms, e.g. hydantoin
    • C07D233/74—Two oxygen atoms, e.g. hydantoin with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to other ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic 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
    • C07D233/66—Heterocyclic 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
    • C07D233/72—Two oxygen atoms, e.g. hydantoin
    • C07D233/76—Two oxygen atoms, e.g. hydantoin with substituted hydrocarbon radicals attached to the third ring carbon atom
    • C07D233/78—Radicals substituted by oxygen atoms

Landscapes

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

Abstract

compostos de imidazolidina como moduladores de receptor de androgénio, e composição farmacêutica. a presente invenção refere-se a novos compostos que têm a fórmula representada pela seguinte em que x, r1, r2a, r2b r2c r3a r3b, r4a r4b r4c e m1 são como descritos aqui. os compostos podem ser preparados como composições farmacêuticas, e podem ser usados para a prevenção e tratamento de uma variedade de condições em mamíferos incluindo humanos, incluindo por meio de exemplo não limitante, caquexia, osteoporose, sarcopenia, um declínio em libido e/ou disfunção sexual.
BRPI0919290-5A 2008-09-11 2009-09-10 composto de imidazoldina com moduladores de receptor de androgênio, e composição farmacêutica BRPI0919290A2 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US19191808P 2008-09-11 2008-09-11
US61/191,918 2008-09-11
GB0900333.6A GB2463514C (en) 2008-09-11 2009-01-09 Imidazolidine compounds and uses therefor
GB0900333.6 2009-01-09
PCT/EP2009/061733 WO2010029119A1 (en) 2008-09-11 2009-09-10 Novel imidazolidine compounds as androgen receptor modulators

Publications (1)

Publication Number Publication Date
BRPI0919290A2 true BRPI0919290A2 (pt) 2019-04-30

Family

ID=40379370

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0919290-5A BRPI0919290A2 (pt) 2008-09-11 2009-09-10 composto de imidazoldina com moduladores de receptor de androgênio, e composição farmacêutica

Country Status (20)

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

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BR112013023028B1 (pt) 2011-03-10 2021-09-21 Suzhou Kintor Pharmaceuticals, Inc Composto de fórmula (i) ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica e formulação farmacêutica tópica
GB201311107D0 (en) * 2013-06-21 2013-08-07 Univ Edinburgh Bioorthogonal methods and compounds
EP3021841B1 (en) * 2013-07-18 2022-11-16 Baylor College Of Medicine Methods and compositions for treatment of muscle wasting, muscle weakness, and/or cachexia
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
CN106573921B (zh) * 2013-12-31 2019-05-07 博福-益普生（天津）制药有限公司 咪唑烷-2,4-二酮衍生物
US11662606B2 (en) * 2017-12-06 2023-05-30 Eyebright Medical Technology (Beijing) Co., Ltd. Orthokeratology lens and method for making orthokeratology lenses
EP3773537B1 (en) 2018-04-19 2022-03-23 Tvardi Therapeutics, Inc. Stat3 inhibitors
US11026905B2 (en) 2018-04-19 2021-06-08 Tvardi Therapeutics, Inc. STAT3 inhibitors
EP4093377A1 (en) 2020-01-24 2022-11-30 Tvardi Therapeutics, Inc. Therapeutic compounds, formulations, and uses thereof
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

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Also Published As

Publication number Publication date
RU2488584C2 (ru) 2013-07-27
EP2344460B1 (en) 2015-08-12
JP5595402B2 (ja) 2014-09-24
CO6382130A2 (es) 2012-02-15
GB0900333D0 (en) 2009-02-11
KR20110067029A (ko) 2011-06-20
CN102149687A (zh) 2011-08-10
CA2736364C (en) 2018-06-26
GB2463514B (en) 2010-07-28
WO2010029119A1 (en) 2010-03-18
GB2463514A (en) 2010-03-17
AU2009290849A1 (en) 2010-03-18
US20100113547A1 (en) 2010-05-06
EP2344460A1 (en) 2011-07-20
CN102149687B (zh) 2014-08-13
CA2736364A1 (en) 2010-03-18
TWI449698B (zh) 2014-08-21
NZ591374A (en) 2012-07-27
ES2552684T3 (es) 2015-12-01
MX2011002374A (es) 2011-04-11
US20120178718A1 (en) 2012-07-12
ZA201101707B (en) 2012-01-25
IL211277A (en) 2014-12-31
JP2012524708A (ja) 2012-10-18
US8383608B2 (en) 2013-02-26
KR101705157B1 (ko) 2017-02-09
TW201016671A (en) 2010-05-01
US7968581B2 (en) 2011-06-28
GB2463514C (en) 2018-09-26
AU2009290849B2 (en) 2015-04-02
HK1141015A1 (en) 2010-10-29
RU2011113749A (ru) 2012-10-20
AR073282A1 (es) 2010-10-28
IL211277A0 (en) 2011-04-28

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Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B25C Requirement related to requested transfer of rights

Owner name: GALAPAGOS N.V. (BE)

Free format text: A FIM DE ATENDER A TRANSFERENCIA, REQUERIDA ATRAVES DA PETICAO NO 20130032114 DE 15/04/2013, E NECESSARIO APRESENTAR O DOCUMENTO DE CESSAO NOTARIZADO E COM APOSTILAMENTO OU LEGALIZACAO CONSULAR, ALEM DA GUIA DE CUMPRIMENTO DE EXIGENCIA.

B25A Requested transfer of rights approved

Owner name: DART THERAPEUTICS, LLC (US)

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B11B Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements