JP6516743B2 - オクタヒドロ縮合アザデカリン糖質コルチコイドレセプター調節因子 - Google Patents

オクタヒドロ縮合アザデカリン糖質コルチコイドレセプター調節因子 Download PDF

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JP6516743B2
JP6516743B2 JP2016533614A JP2016533614A JP6516743B2 JP 6516743 B2 JP6516743 B2 JP 6516743B2 JP 2016533614 A JP2016533614 A JP 2016533614A JP 2016533614 A JP2016533614 A JP 2016533614A JP 6516743 B2 JP6516743 B2 JP 6516743B2
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fluorophenyl
sulfonyl
pyrazolo
octahydro
isoquinolin
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JP2016537394A5 (https=
JP2016537394A (ja
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ヘイゼル ハント，
ヘイゼル ハント，
イアン ウォルターズ，
イアン ウォルターズ，
ブノワ グールデット，
ブノワ グールデット，
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コーセプト セラピューティクス， インコーポレイテッド
コーセプト セラピューティクス， インコーポレイテッド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Virology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2016533614A 2013-11-25 2014-11-21 オクタヒドロ縮合アザデカリン糖質コルチコイドレセプター調節因子 Active JP6516743B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361908333P 2013-11-25 2013-11-25
US61/908,333 2013-11-25
US201461985035P 2014-04-28 2014-04-28
US61/985,035 2014-04-28
PCT/US2014/066759 WO2015077530A1 (en) 2013-11-25 2014-11-21 Octahydro fused azadecalin glucocorticoid receptor modulators

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JP2017206081A Division JP2018012734A (ja) 2013-11-25 2017-10-25 オクタヒドロ縮合アザデカリン糖質コルチコイドレセプター調節因子
JP2019063279A Division JP2019094355A (ja) 2013-11-25 2019-03-28 オクタヒドロ縮合アザデカリン糖質コルチコイドレセプター調節因子

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JP2016537394A JP2016537394A (ja) 2016-12-01
JP2016537394A5 JP2016537394A5 (https=) 2017-12-07
JP6516743B2 true JP6516743B2 (ja) 2019-05-22

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JP2017206081A Pending JP2018012734A (ja) 2013-11-25 2017-10-25 オクタヒドロ縮合アザデカリン糖質コルチコイドレセプター調節因子
JP2019063279A Withdrawn JP2019094355A (ja) 2013-11-25 2019-03-28 オクタヒドロ縮合アザデカリン糖質コルチコイドレセプター調節因子
JP2021021630A Withdrawn JP2021073315A (ja) 2013-11-25 2021-02-15 オクタヒドロ縮合アザデカリン糖質コルチコイドレセプター調節因子
JP2022189246A Withdrawn JP2023011052A (ja) 2013-11-25 2022-11-28 オクタヒドロ縮合アザデカリン糖質コルチコイドレセプター調節因子
JP2024148322A Withdrawn JP2024170470A (ja) 2013-11-25 2024-08-30 オクタヒドロ縮合アザデカリン糖質コルチコイドレセプター調節因子

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JP2019063279A Withdrawn JP2019094355A (ja) 2013-11-25 2019-03-28 オクタヒドロ縮合アザデカリン糖質コルチコイドレセプター調節因子
JP2021021630A Withdrawn JP2021073315A (ja) 2013-11-25 2021-02-15 オクタヒドロ縮合アザデカリン糖質コルチコイドレセプター調節因子
JP2022189246A Withdrawn JP2023011052A (ja) 2013-11-25 2022-11-28 オクタヒドロ縮合アザデカリン糖質コルチコイドレセプター調節因子
JP2024148322A Withdrawn JP2024170470A (ja) 2013-11-25 2024-08-30 オクタヒドロ縮合アザデカリン糖質コルチコイドレセプター調節因子

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US (8) US10047082B2 (https=)
EP (5) EP3848027B1 (https=)
JP (6) JP6516743B2 (https=)
KR (1) KR102352737B1 (https=)
CN (2) CN106029066B (https=)
AU (1) AU2014352915B2 (https=)
BR (1) BR112016011826B1 (https=)
CA (1) CA2931302C (https=)
DK (2) DK3848027T3 (https=)
ES (3) ES2869172T3 (https=)
FI (1) FI3848027T3 (https=)
IL (1) IL245848B (https=)
MX (1) MX368167B (https=)
MY (1) MY180141A (https=)
PH (1) PH12016500968B1 (https=)
PL (3) PL3848027T3 (https=)
PT (2) PT3848027T (https=)
RU (1) RU2674983C1 (https=)
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US12514849B2 (en) 2018-12-19 2026-01-06 Corcept Therapeutics Incorporated Pharmaceutical formulations containing relacorilant, a heteroaryl-ketone fused azadecalin compound
US12589094B2 (en) 2020-05-27 2026-03-31 Corcept Therapeutics Incorporated Concomitant administration of glucocorticoid receptor modulator relacorilant and paclitaxel, a dual substrate of CYP2C8 and CYP3A4

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US8859774B2 (en) 2012-05-25 2014-10-14 Corcept Therapeutics, Inc. Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
PL3848027T3 (pl) 2013-11-25 2023-07-24 Corcept Therapeutics Incorporated Skondensowane oktahydrozwiązki azadekaliny jako modulatory receptora glukokortykoidowego
US10610534B2 (en) 2015-03-30 2020-04-07 Corcept Therapeutics, Inc. Use of glucocorticoid receptor antagonists in combination with glucocorticoids to treat adrenal insufficiency
WO2017151613A1 (en) 2016-03-01 2017-09-08 Corcept Therapeutics, Inc. The use of glucocorticoid receptor modulators to potentiate checkpoint inhibitors
CN106478464B (zh) * 2016-08-30 2018-06-05 黄河三角洲京博化工研究院有限公司 一种2-氟-6-三氟甲基苯磺酰氯的制备方法
US9943505B2 (en) 2016-09-09 2018-04-17 Corcept Therapeutics, Inc. Glucocorticoid receptor modulators to treat pancreatic cancer
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MX2019011543A (es) * 2017-03-31 2019-12-16 Corcept Therapeutics Inc Moduladores del receptor de glucocorticoides para el tratamiento de cancer cervical.
WO2018209142A2 (en) * 2017-05-10 2018-11-15 Corcept Therapeutics, Inc. Octahydro azadecalin formulations
WO2018236749A2 (en) 2017-06-20 2018-12-27 Corcept Therapeutics, Inc. Methods of treating neuroepithelial tumors using selective glucocorticoid receptor modulators
CN117771239A (zh) * 2018-04-10 2024-03-29 杜克大学 乳腺癌的拉索昔芬治疗
ES3038908T3 (en) 2018-04-23 2025-10-15 Corcept Therapeutics Inc Methods of preparing regioselective n-alkyl triazoles
TWI811400B (zh) 2018-07-20 2023-08-11 德商歌林達有限公司 經進一步取代之三唑并喹噁啉衍生物
IL263184A (en) 2018-11-21 2020-05-31 Yarden Yosef Method of treating cancer and compositions for same
US11389432B2 (en) 2018-12-19 2022-07-19 Corcept Therapeutics Incorporated Methods of treating cancer comprising administration of a glucocorticoid receptor modulator and a cancer chemotherapy agent
US11234971B2 (en) 2018-12-19 2022-02-01 Corcept Therapeutics Incorporated Methods of treating cancer comprising administration of a glucocorticoid receptor modulator and a cancer chemotherapy agent
JP7789561B2 (ja) 2019-02-22 2025-12-22 コーセプト セラピューティクス， インコーポレイテッド レラコリラント、ヘテロアリール－ケトン縮合アザデカリングルココルチコイド受容体調節物質の治療用途
AU2020367769B2 (en) 2019-10-16 2023-10-12 Corcept Therapeutics Incorporated Method of normalizing the neutrophil to lymphocyte ratio in cancer patients with a selective glucocorticoid receptor antagonist
JP7569492B2 (ja) 2019-12-11 2024-10-18 コーセプト セラピューティクス， インコーポレイテッド 抗精神病薬誘発性体重増加のミリコリラントによる治療方法
ES3060361T3 (en) 2019-12-21 2026-03-26 Corcept Therapeutics Inc Treatment of, and differential diagnosis between, acth-dependent cushing's syndrome and acth-independent cushing's syndrome
BR112022015011A2 (pt) 2020-01-29 2022-09-20 Corcept Therapeutics Inc Método para tratar um sujeito que sofre de tumor de carcinoma adrenocortical e tendo excesso de cortisol, e, composição farmacêutica para tratar carcinoma adrenocortical
AU2021220763B2 (en) * 2020-02-10 2024-01-18 Corcept Therapeutics Incorporated Methods of stimulating an anti-tumor response using a selective glucocorticoid receptor modulator
CN116113627B (zh) 2020-06-22 2025-06-03 科赛普特治疗公司 季吲哚糖皮质激素受体拮抗剂
WO2022134033A1 (en) 2020-12-25 2022-06-30 Corcept Therapeutics Incorporated Methods of preparing heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
WO2022166810A1 (zh) * 2021-02-03 2022-08-11 江苏恒瑞医药股份有限公司 稠合的氮杂三环类衍生物、其制备方法及其在医药上的应用
IL313667A (en) 2021-12-21 2024-08-01 Corcept Therapeutics Inc Glucocorticoid receptor antagonists INDAZOL CYCLES
CA3243549A1 (en) 2021-12-21 2023-06-29 Corcept Therapeutics Incorporated INDAZOLE PIPERAZINE-BASED GLUCOCORTICOID RECEPTOR ANTAGONISTS
CN117510490A (zh) * 2022-08-03 2024-02-06 江苏恒瑞医药股份有限公司 一种稠合氮杂萘烷类衍生物的晶型及其制备方法
KR20250073629A (ko) 2022-10-06 2025-05-27 코어셉트 쎄라퓨틱스 인코포레이티드 글루코코르티코이드 수용체 조절제의 제형
US12433882B2 (en) 2022-10-28 2025-10-07 Corcept Therapeutics Incorporated Treatments for amyotrophic lateral sclerosis using dazucorilant
CN120752040A (zh) * 2023-02-17 2025-10-03 科赛普特治疗学股份有限公司 用于治疗亨廷顿舞蹈症及其症状的方法和组合物
EP4716536A1 (en) * 2023-05-22 2026-04-01 Corcept Therapeutics Incorporated Methods for treating adrenal gland tumors
TW202539687A (zh) * 2024-01-15 2025-10-16 香港商英矽智能科技知識產權有限公司 作為糖皮質激素受體調節劑的新化合物及其用途

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