JP6995757B2 - グルココルチコイド受容体の阻害剤 - Google Patents

グルココルチコイド受容体の阻害剤 Download PDF

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Publication number
JP6995757B2
JP6995757B2 JP2018533668A JP2018533668A JP6995757B2 JP 6995757 B2 JP6995757 B2 JP 6995757B2 JP 2018533668 A JP2018533668 A JP 2018533668A JP 2018533668 A JP2018533668 A JP 2018533668A JP 6995757 B2 JP6995757 B2 JP 6995757B2
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JP
Japan
Prior art keywords
optionally substituted
alkyl
carbocyclyl
heterocyclyl
hydroxy
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Expired - Fee Related
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JP2018533668A
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Japanese (ja)
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JP2019500376A5 (enExample
JP2019500376A (ja
Inventor
サン，ダーチン
アール． マギー，ローレンス
デュ，シャオフイ
ズー，リウシェン
ヤン，シュエレイ
リュー，ヨサプ
エクステロウィズ，ジョン
シー． メディナ，ジュリオ
チョウ，ハイイン
デララエ バルバス，ミナ
アール． ファンティン，ヴァレリア
Original Assignee
オリック ファーマシューティカルズ，インク．
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Priority to JP2021147955A priority Critical patent/JP2022003045A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0081—Substituted in position 17 alfa and 17 beta
    • C07J1/0088—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being an unsaturated hydrocarbon group
    • C07J1/0096—Alkynyl derivatives
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
    • 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
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003—Androstane derivatives
    • C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005—Ketals
    • C07J21/006—Ketals at position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005—Ketals
    • C07J21/008—Ketals at position 17
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005—Oxygen-containing hetero ring
    • C07J71/001—Oxiranes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2818—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2827—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against B7 molecules, e.g. CD80, CD86

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
JP2018533668A 2015-12-23 2016-12-22 グルココルチコイド受容体の阻害剤 Expired - Fee Related JP6995757B2 (ja)

Priority Applications (1)

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JP2021147955A JP2022003045A (ja) 2015-12-23 2021-09-10 グルココルチコイド受容体の阻害剤

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562387293P 2015-12-23 2015-12-23
US62/387,293 2015-12-23
PCT/US2016/068448 WO2017112909A1 (en) 2015-12-23 2016-12-22 Inhibitors of glucocorticoid receptor

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JP2021147955A Division JP2022003045A (ja) 2015-12-23 2021-09-10 グルココルチコイド受容体の阻害剤

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JP2019500376A JP2019500376A (ja) 2019-01-10
JP2019500376A5 JP2019500376A5 (enExample) 2020-01-30
JP6995757B2 true JP6995757B2 (ja) 2022-01-17

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JP2018533668A Expired - Fee Related JP6995757B2 (ja) 2015-12-23 2016-12-22 グルココルチコイド受容体の阻害剤
JP2021147955A Pending JP2022003045A (ja) 2015-12-23 2021-09-10 グルココルチコイド受容体の阻害剤

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US (1) US11208432B2 (enExample)
EP (1) EP3394079A4 (enExample)
JP (2) JP6995757B2 (enExample)
CN (1) CN108713023B (enExample)
AU (2) AU2016379417B2 (enExample)
CA (1) CA3009525A1 (enExample)
WO (1) WO2017112909A1 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021046409A (ja) * 2016-10-07 2021-03-25 オリック ファーマシューティカルズ，インク． グルココルチコイド受容体の阻害剤
JP2022003045A (ja) * 2015-12-23 2022-01-11 オリック ファーマシューティカルズ，インク． グルココルチコイド受容体の阻害剤

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017112904A1 (en) 2015-12-23 2017-06-29 Oric Pharmaceuticals, Inc. Inhibitors of glucocorticoid receptor
EP3394078A4 (en) 2015-12-23 2019-11-27 Oric Pharmaceuticals, Inc. INHIBITORS OF THE GLUCOCORTICIDE RECEPTOR
TW202010502A (zh) * 2018-04-11 2020-03-16 美商歐瑞克製藥公司 包含糖皮質激素受體拮抗劑之固體形式與調配物及其用途
CN118265717A (zh) * 2022-03-31 2024-06-28 成都赛璟生物医药科技有限公司 一种cdk8抑制剂及其制备方法和用途

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JP2003119154A (ja) 2001-08-16 2003-04-23 Jenapharm Gmbh & Co Kg 男性生殖器系疾病の予防及び治療におけるグルココルチコイド受容体アンタゴニストの使用方法
US20040180869A1 (en) 2002-12-16 2004-09-16 Ulrich Bothe New glucocorticoid receptor antagonists for prophylaxis and therapy of glucocorticoid-mediated hypogonadism, of sexual dysfunction and/or infertility

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022003045A (ja) * 2015-12-23 2022-01-11 オリック ファーマシューティカルズ，インク． グルココルチコイド受容体の阻害剤
JP2021046409A (ja) * 2016-10-07 2021-03-25 オリック ファーマシューティカルズ，インク． グルココルチコイド受容体の阻害剤

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Publication number Publication date
AU2016379417B2 (en) 2020-09-24
EP3394079A4 (en) 2019-08-21
AU2016379417A1 (en) 2018-07-19
AU2020256460A1 (en) 2020-11-12
JP2019500376A (ja) 2019-01-10
JP2022003045A (ja) 2022-01-11
CA3009525A1 (en) 2017-06-29
US20210002324A1 (en) 2021-01-07
CN108713023B (zh) 2021-10-26
CN108713023A (zh) 2018-10-26
EP3394079A1 (en) 2018-10-31
US11208432B2 (en) 2021-12-28
WO2017112909A1 (en) 2017-06-29

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