CA2608419A1 - Substituted n-arylpyrrolidines as selective androgen receptor modulators - Google Patents

Substituted n-arylpyrrolidines as selective androgen receptor modulators Download PDF

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Publication number
CA2608419A1
CA2608419A1 CA002608419A CA2608419A CA2608419A1 CA 2608419 A1 CA2608419 A1 CA 2608419A1 CA 002608419 A CA002608419 A CA 002608419A CA 2608419 A CA2608419 A CA 2608419A CA 2608419 A1 CA2608419 A1 CA 2608419A1
Authority
CA
Canada
Prior art keywords
methyl
halo
compound according
group
alkyl
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA002608419A
Other languages
English (en)
French (fr)
Inventor
Konstantinos Gavardinas
Prabhakar Kondaji Jadhav
Douglas Richard Stack
Ian Roger Clemens
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2608419A1 publication Critical patent/CA2608419A1/en
Abandoned legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • 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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • 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
    • 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
    • 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
    • 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)
  • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Reproductive Health (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA002608419A 2005-05-13 2006-05-10 Substituted n-arylpyrrolidines as selective androgen receptor modulators Abandoned CA2608419A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US68091105P 2005-05-13 2005-05-13
US60/680,911 2005-05-13
PCT/US2006/018061 WO2006124447A2 (en) 2005-05-13 2006-05-10 Substituted n-arylpyrrolidines as selective androgen receptor modulators

Publications (1)

Publication Number Publication Date
CA2608419A1 true CA2608419A1 (en) 2006-11-23

Family

ID=37057376

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002608419A Abandoned CA2608419A1 (en) 2005-05-13 2006-05-10 Substituted n-arylpyrrolidines as selective androgen receptor modulators

Country Status (17)

Country Link
US (1) US7807691B2 (enExample)
EP (1) EP1891038B1 (enExample)
JP (1) JP5089578B2 (enExample)
CN (1) CN101175747B (enExample)
AT (1) ATE412647T1 (enExample)
AU (1) AU2006247738A1 (enExample)
BR (1) BRPI0610183A2 (enExample)
CA (1) CA2608419A1 (enExample)
CY (1) CY1108690T1 (enExample)
DE (1) DE602006003432D1 (enExample)
DK (1) DK1891038T3 (enExample)
ES (1) ES2314922T3 (enExample)
MX (1) MX2007014053A (enExample)
PL (1) PL1891038T3 (enExample)
PT (1) PT1891038E (enExample)
SI (1) SI1891038T1 (enExample)
WO (1) WO2006124447A2 (enExample)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007015567A1 (ja) * 2005-08-01 2007-02-08 Takeda Pharmaceutical Company Limited 環状アミン化合物
CA2670976C (en) 2006-11-30 2015-01-27 Atsushi Hasuoka Cyclic amine compound
TW200831080A (en) 2006-12-15 2008-08-01 Irm Llc Compounds and compositions as inhibitors of cannabinoid receptor 1 activity
MY159910A (en) 2007-08-07 2017-02-15 Takeda Pharmaceuticals Co Pyrrolidin-2-one derivatives as androgen receptor modulator
CN101945853B (zh) 2007-12-21 2014-08-20 配体药物公司 选择性雄激素受体调节剂(sarm)及其应用
BRPI0907844B8 (pt) 2008-02-22 2021-05-25 Radius Health Inc compostos e método para modular um receptor de andrógeno, processos de preparação e composição farmacêutica dos mesmos e seus usos
US8268872B2 (en) 2008-02-22 2012-09-18 Radius Health, Inc. Selective androgen receptor modulators
WO2009131196A1 (ja) * 2008-04-24 2009-10-29 武田薬品工業株式会社 置換ピロリジン誘導体およびその用途
WO2009133861A1 (ja) * 2008-04-28 2009-11-05 武田薬品工業株式会社 環状アミン化合物
JP5964756B2 (ja) 2010-02-04 2016-08-03 ラジウス ヘルス,インコーポレイテッド 選択的アンドロゲン受容体モジュレーター
PL2568806T3 (pl) 2010-05-12 2017-03-31 Radius Health, Inc. Schematy lecznicze
US8642632B2 (en) 2010-07-02 2014-02-04 Radius Health, Inc. Selective androgen receptor modulators
AU2011312490B2 (en) 2010-09-28 2015-06-25 Radius Pharmaceuticals, Inc. Selective androgen receptor modulators
BR112013021638A2 (pt) * 2011-02-25 2016-08-02 Irm Llc "compostos inibidores de trk, seu uso e composições que os compreendem"
AR088082A1 (es) 2011-10-13 2014-05-07 Lilly Co Eli Moduladores selectivos del receptor androgeno
MX2015005949A (es) * 2012-11-16 2015-09-08 Biocryst Pharm Inc Nucleosidos que contienen aza-azucar antiviral.
ES2939940T3 (es) 2014-03-28 2023-04-28 Univ Duke Tratamiento del cáncer de mama utilizando moduladores selectivos de los receptores de estrógenos
US9421264B2 (en) 2014-03-28 2016-08-23 Duke University Method of treating cancer using selective estrogen receptor modulators
WO2017223115A1 (en) 2016-06-22 2017-12-28 Radius Health, Inc. Ar+ breast cancer treatment methods
EP3565542B1 (en) 2017-01-05 2024-04-10 Radius Pharmaceuticals, Inc. Polymorphic forms of rad1901-2hcl
AU2018346597B2 (en) 2017-10-06 2023-07-13 Forma Therapeutics, Inc. Inhibiting Ubiquitin Specific Peptidase 30
BR112020023136A2 (pt) 2018-05-14 2021-02-09 Nuvation Bio Inc. compostos de alvo de receptor de hormônio nuclear anticâncer
IL278291B2 (en) 2018-05-17 2023-10-01 Forma Therapeutics Inc Condensed bicyclic compounds are useful as ubiquitin-specific peptidase 30 inhibitors
SG11202013177WA (en) 2018-07-04 2021-01-28 Radius Pharmaceuticals Inc Polymorphic forms of rad 1901-2hcl
EP4218934B1 (en) 2018-10-05 2025-06-18 Forma Therapeutics, Inc. Inhibiting ubiquitin-specific protease 30 (usp30)
US12441745B2 (en) 2019-02-12 2025-10-14 Radius Pharmaceuticals, Inc. Processes and compounds
AU2020257397B2 (en) 2019-04-19 2026-02-26 Ligand Pharmaceuticals Inc. Crystalline forms and methods of producing crystalline forms of a compound
CN113811333B (zh) 2019-05-14 2024-03-12 诺维逊生物股份有限公司 靶向抗癌核激素受体的化合物
EP4058464A1 (en) 2019-11-13 2022-09-21 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
WO2021098810A1 (zh) * 2019-11-20 2021-05-27 南京明德新药研发有限公司 用作选择性雄激素受体调节剂的化合物
EP4313991A1 (en) 2021-03-23 2024-02-07 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
WO2022235585A1 (en) 2021-05-03 2022-11-10 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
AU2025211735A1 (en) * 2024-01-24 2026-07-16 Siteone Therapeutics, Inc. 2-aryl cycloalkyl and heterocycloalkyl inhibitors of nav1.8 for the treatment of pain

Family Cites Families (7)

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US5411981A (en) 1991-01-09 1995-05-02 Roussel Uclaf Phenylimidazolidines having antiandrogenic activity
FR2671348B1 (fr) * 1991-01-09 1993-03-26 Roussel Uclaf Nouvelles phenylimidazolidines, leur procede de preparation, leur application comme medicaments et les compositions pharmaceutiques les renfermant.
FR2693461B1 (fr) * 1992-07-08 1994-09-02 Roussel Uclaf Nouvelles phénylimidazolidines substituées, leur procédé de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant.
US6887870B1 (en) 1999-10-12 2005-05-03 Bristol-Myers Squibb Company Heterocyclic sodium/proton exchange inhibitors and method
NZ538713A (en) * 2002-08-12 2007-01-26 Takeda Chemical Industries Ltd Fused benzene derivative and use
AU2003285952A1 (en) * 2002-10-21 2004-05-13 Irm Llc Pyrrolidones with anti-hiv activity
WO2005000795A2 (en) * 2003-06-10 2005-01-06 Smithkline Beecham Corporation Aniline derivatived androgen-, glucocorticoid-, mineralcorticoid- and progesterone- receptor modulators

Also Published As

Publication number Publication date
JP2008540554A (ja) 2008-11-20
CN101175747A (zh) 2008-05-07
ES2314922T3 (es) 2009-03-16
DK1891038T3 (da) 2009-01-19
CN101175747B (zh) 2011-06-22
CY1108690T1 (el) 2014-04-09
PL1891038T3 (pl) 2009-04-30
ATE412647T1 (de) 2008-11-15
WO2006124447A2 (en) 2006-11-23
US20080176864A1 (en) 2008-07-24
EP1891038B1 (en) 2008-10-29
AU2006247738A1 (en) 2006-11-23
WO2006124447A3 (en) 2007-03-29
JP5089578B2 (ja) 2012-12-05
MX2007014053A (es) 2008-02-05
SI1891038T1 (sl) 2009-04-30
DE602006003432D1 (de) 2008-12-11
PT1891038E (pt) 2008-12-02
EP1891038A2 (en) 2008-02-27
BRPI0610183A2 (pt) 2012-12-04
US7807691B2 (en) 2010-10-05

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued

Effective date: 20140716