JP6906525B2 - 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
JP6906525B2
JP6906525B2 JP2018533649A JP2018533649A JP6906525B2 JP 6906525 B2 JP6906525 B2 JP 6906525B2 JP 2018533649 A JP2018533649 A JP 2018533649A JP 2018533649 A JP2018533649 A JP 2018533649A JP 6906525 B2 JP6906525 B2 JP 6906525B2
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JP
Japan
Prior art keywords
optionally substituted
alkyl
carbocyclyl
heterocyclyl
substituted
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Expired - Fee Related
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JP2018533649A
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English (en)
Japanese (ja)
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JP2019500374A (ja
JP2019500374A5 (enExample
Inventor
サン，ダーチン
アール． マギー，ローレンス
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
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
デララエ バルバス，ミナ
アール． ファンティン，ヴァレリア
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．
オリック ファーマシューティカルズ，インク．
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Publication of JP2019500374A publication Critical patent/JP2019500374A/ja
Publication of JP2019500374A5 publication Critical patent/JP2019500374A5/ja
Priority to JP2021103372A priority Critical patent/JP2021167323A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • 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
    • 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
    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • 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
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/567—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
    • 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
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
    • 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
    • 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
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • 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
    • 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
    • C07J41/0088—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing unsubstituted amino radicals
    • 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
    • C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Toxicology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
JP2018533649A 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 JP6906525B2 (ja)

Priority Applications (1)

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JP2021103372A JP2021167323A (ja) 2015-12-23 2021-06-22 グルココルチコイド受容体の阻害剤

Applications Claiming Priority (3)

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US201562387282P 2015-12-23 2015-12-23
US62/387,282 2015-12-23
PCT/US2016/068431 WO2017112902A1 (en) 2015-12-23 2016-12-22 Inhibitors of glucocorticoid receptor

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JP2021103372A Division JP2021167323A (ja) 2015-12-23 2021-06-22 グルココルチコイド受容体の阻害剤

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JP2019500374A JP2019500374A (ja) 2019-01-10
JP2019500374A5 JP2019500374A5 (enExample) 2020-01-30
JP6906525B2 true JP6906525B2 (ja) 2021-07-21

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JP2021103372A Ceased JP2021167323A (ja) 2015-12-23 2021-06-22 グルココルチコイド受容体の阻害剤

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US (2) US11124537B2 (enExample)
EP (1) EP3394078A4 (enExample)
JP (2) JP6906525B2 (enExample)
CN (1) CN108699102A (enExample)
AU (2) AU2016377702B2 (enExample)
CA (1) CA3009522A1 (enExample)
WO (1) WO2017112902A1 (enExample)

Families Citing this family (8)

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US11124537B2 (en) 2015-12-23 2021-09-21 Oric Pharmaceuticals, Inc. Inhibitors of glucocorticoid receptor
WO2017112909A1 (en) 2015-12-23 2017-06-29 Oric Pharmaceuticals, Inc. Inhibitors of glucocorticoid receptor
WO2017112904A1 (en) 2015-12-23 2017-06-29 Oric Pharmaceuticals, Inc. Inhibitors of glucocorticoid receptor
KR20210039001A (ko) 2016-10-07 2021-04-08 오릭 파마슈티칼스, 인크. 글루코코르티코이드 수용체의 억제제
US11998606B2 (en) 2018-04-13 2024-06-04 Board Of Regents, The University Of Texas System Compounds and methods for selective proteolysis of glucocorticoid receptors
US20230302014A1 (en) * 2020-08-04 2023-09-28 Oric Pharmaceuticals, Inc. Uses of glucocorticoid receptor (gr) antagonist and androgen receptor (ar) degrader combinations
KR20230061485A (ko) * 2020-08-31 2023-05-08 더 트러스티즈 오브 인디애나 유니버시티 항프로게스틴을 투여하여 고등급 장액성 난소암 및 유방암을 예방하는 방법
WO2023000135A1 (en) * 2021-07-19 2023-01-26 Context Biopharma Inc. Processes of making onapristone and intermediates thereof

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WO2017112909A1 (en) 2015-12-23 2017-06-29 Oric Pharmaceuticals, Inc. Inhibitors of glucocorticoid receptor
WO2017112904A1 (en) 2015-12-23 2017-06-29 Oric Pharmaceuticals, Inc. Inhibitors of glucocorticoid receptor
US11124537B2 (en) * 2015-12-23 2021-09-21 Oric Pharmaceuticals, Inc. Inhibitors of glucocorticoid receptor
KR20210039001A (ko) 2016-10-07 2021-04-08 오릭 파마슈티칼스, 인크. 글루코코르티코이드 수용체의 억제제
US12233073B2 (en) 2017-06-09 2025-02-25 Regents Of The University Of Minnesota Skin care formulations and skin cancer treatment
JP2021518842A (ja) 2018-04-11 2021-08-05 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アンタゴニストを含む固体の形態と製剤、およびその使用

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WO2017112902A1 (en) 2017-06-29
US20210395295A1 (en) 2021-12-23
AU2016377702B2 (en) 2021-03-11
EP3394078A1 (en) 2018-10-31
US11124537B2 (en) 2021-09-21
JP2019500374A (ja) 2019-01-10
JP2021167323A (ja) 2021-10-21
AU2016377702A1 (en) 2018-07-19
AU2021202019A1 (en) 2021-04-29
EP3394078A4 (en) 2019-11-27
CA3009522A1 (en) 2017-06-29
AU2021202019B2 (en) 2022-01-27
US20210017220A1 (en) 2021-01-21
CN108699102A (zh) 2018-10-23

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