KR102062640B1 - 헤테로아릴-케톤 융합된 아자데칼린 글루코코르티코이드 수용체 조절제 - Google Patents

헤테로아릴-케톤 융합된 아자데칼린 글루코코르티코이드 수용체 조절제 Download PDF

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KR102062640B1
KR102062640B1 KR1020147036405A KR20147036405A KR102062640B1 KR 102062640 B1 KR102062640 B1 KR 102062640B1 KR 1020147036405 A KR1020147036405 A KR 1020147036405A KR 20147036405 A KR20147036405 A KR 20147036405A KR 102062640 B1 KR102062640 B1 KR 102062640B1
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fluorophenyl
isoquinolin
sulfonyl
pyrazolo
methanone
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KR20150021955A (ko
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헤젤 헌트
토니 존슨
니콜라스 레이
이언 왈터스
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코어셉트 쎄라퓨틱스 인코포레이티드
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems

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  • 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)
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  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
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  • Child & Adolescent Psychology (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Electroluminescent Light Sources (AREA)
KR1020147036405A 2012-05-25 2013-05-24 헤테로아릴-케톤 융합된 아자데칼린 글루코코르티코이드 수용체 조절제 Active KR102062640B1 (ko)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US201261651669P 2012-05-25 2012-05-25
US61/651,669 2012-05-25
US201261691083P 2012-08-20 2012-08-20
US61/691,083 2012-08-20
US201261715907P 2012-10-19 2012-10-19
US61/715,907 2012-10-19
US201361759520P 2013-02-01 2013-02-01
US61/759,520 2013-02-01
US201361781629P 2013-03-14 2013-03-14
US61/781,629 2013-03-14
PCT/US2013/042732 WO2013177559A2 (en) 2012-05-25 2013-05-24 Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators

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KR20150021955A KR20150021955A (ko) 2015-03-03
KR102062640B1 true KR102062640B1 (ko) 2020-01-06

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JP (1) JP6172871B2 (enExample)
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AU (1) AU2013266110C1 (enExample)
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SG (1) SG11201407682TA (enExample)
WO (1) WO2013177559A2 (enExample)
ZA (1) ZA201408182B (enExample)

Cited By (3)

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US11648245B2 (en) 2012-05-25 2023-05-16 Corcept Therapeutics, Inc. Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
US11925626B2 (en) 2018-12-19 2024-03-12 Corcept Therapeutics Incorporated Pharmaceutical formulations containing relacorilant, a heteroaryl-ketone fused azadecalin compound
US12226412B2 (en) 2012-05-25 2025-02-18 Corcept Therapeutics, Inc. Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators

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US10047082B2 (en) 2013-11-25 2018-08-14 Corcept Therapeutics, Inc. Octahydro fused azadecalin glucocorticoid receptor modulators
AU2016226451B2 (en) * 2015-03-02 2019-12-19 Corcept Therapeutics, Inc. Use of glucocorticoid receptor antagonist and somatostatin analogues to treat ACTH-secreting tumors
KR102495223B1 (ko) * 2015-03-30 2023-02-01 코어셉트 쎄라퓨틱스 인코포레이티드 부신기능부전을 치료하기 위한 글루코코르티코이드와 조합된 글루코코르티코이드 수용체 길항제의 용도
JP6755264B2 (ja) 2015-05-18 2020-09-16 コーセプト セラピューティクス, インコーポレイテッド クッシング症候群についての処置を診断および評価するための方法
WO2017027851A1 (en) * 2015-08-13 2017-02-16 Corcept Therapeutics, Inc. Method for differentially diagnosing acth-dependent cushing's syndrome
AU2017228329B2 (en) * 2016-03-01 2021-03-11 Corcept Therapeutics, Inc. The use of glucocorticoid receptor modulators to potentiate checkpoint inhibitors
US9943505B2 (en) 2016-09-09 2018-04-17 Corcept Therapeutics, Inc. Glucocorticoid receptor modulators to treat pancreatic cancer
PT3600282T (pt) 2017-03-31 2025-11-05 Corcept Therapeutics Inc Moduladores de recetores de glucocorticoides para tratar cancro cervical
AU2018289307B2 (en) 2017-06-20 2024-02-01 Corcept Therapeutics, Inc. Methods of treating neuroepithelial tumors using selective glucocorticoid receptor modulators
US10494349B2 (en) * 2018-04-23 2019-12-03 Corcept Therapeutics, Inc. Methods of preparing regioselective N-alkyl triazoles
SG11202104732UA (en) 2018-11-09 2021-06-29 Corcept Therapeutics Inc Methods for shrinking pituitary tumors
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
WO2020132046A1 (en) 2018-12-19 2020-06-25 Corcept Therapeutics Incorporated Methods of treating cancer comprising administration of a glucocorticoid receptor modulator and a cancer chemotherapy agent
CN113194944A (zh) * 2018-12-20 2021-07-30 科塞普特治疗公司 用于对生长抑素受体阳性肿瘤进行成像和治疗的方法
CN113490496A (zh) 2019-02-22 2021-10-08 科赛普特治疗学股份有限公司 一种杂芳基-酮稠合氮杂萘烷糖皮质激素受体调节剂瑞拉可兰的治疗用途
US12440487B2 (en) 2019-10-16 2025-10-14 Corcept Therapeutics Incorporated Method of normalizing the neutrophil to lymphocyte ratio in cancer patients with a selective glucocorticoid receptor antagonist
WO2021119432A1 (en) 2019-12-11 2021-06-17 Corcept Therapeutics Incorporated Methods of treating antipsychotic-induced weight gain with miricorilant
EP4076470B1 (en) 2019-12-21 2025-12-03 Corcept Therapeutics Incorporated Treatment of, and differential diagnosis between, acth-dependent cushing's syndrome and acth-independent cushing's syndrome
WO2021163058A1 (en) * 2020-02-10 2021-08-19 Corcept Therapeutics Incorporated Methods of stimulating an anti-tumor response using a selective glucocorticoid receptor modulator
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
WO2024077169A1 (en) * 2022-10-06 2024-04-11 Corcept Therapeutics Incorporated Formulations of glucocorticoid receptor modulators
EP4608402A1 (en) 2022-10-28 2025-09-03 Corcept Therapeutics Incorporated Treatments for amyotrophic lateral sclerosis using dazucorilant
US20250360125A1 (en) * 2023-02-17 2025-11-27 Corcept Therapeutics Incorporated Methods and compositions for treating huntington's disease and its symptoms

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US4963558A (en) 1988-12-08 1990-10-16 Lilly Industries Limited Pyrazolo-[3,4-g]isoquinoline derivatives useful to treat CNS disorders
WO2005087769A1 (en) 2004-03-09 2005-09-22 Corcept Therapeutics, Inc. Fused ring azadecalin glucocorticoid receptor modulators
US20100179115A1 (en) 2006-02-28 2010-07-15 Corcept Therapeutics, Inc. Use of a glucocorticoid receptor ii antagonist to treat depression in patients taking il-2
WO2012027702A1 (en) 2010-08-27 2012-03-01 Corcept Therapeutics, Inc. Pyridyl-amine fused azadecalin modulators

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US4963558A (en) 1988-12-08 1990-10-16 Lilly Industries Limited Pyrazolo-[3,4-g]isoquinoline derivatives useful to treat CNS disorders
WO2005087769A1 (en) 2004-03-09 2005-09-22 Corcept Therapeutics, Inc. Fused ring azadecalin glucocorticoid receptor modulators
US20070281928A1 (en) 2004-03-09 2007-12-06 Clark Robin D Fused Ring Azadecalin Glucocorticoid Receptor Modulators
US20110166110A1 (en) 2004-03-09 2011-07-07 Corcept Therapeutics, Inc. Fused Ring Azadecalin Glucocorticoid Receptor Modulators
US20100179115A1 (en) 2006-02-28 2010-07-15 Corcept Therapeutics, Inc. Use of a glucocorticoid receptor ii antagonist to treat depression in patients taking il-2
WO2012027702A1 (en) 2010-08-27 2012-03-01 Corcept Therapeutics, Inc. Pyridyl-amine fused azadecalin modulators

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11648245B2 (en) 2012-05-25 2023-05-16 Corcept Therapeutics, Inc. Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
US12226412B2 (en) 2012-05-25 2025-02-18 Corcept Therapeutics, Inc. Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
US11925626B2 (en) 2018-12-19 2024-03-12 Corcept Therapeutics Incorporated Pharmaceutical formulations containing relacorilant, a heteroaryl-ketone fused azadecalin compound

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PT3590517T (pt) 2021-04-07
CA2872260C (en) 2020-12-22
AU2013266110C1 (en) 2018-07-12
PL3851107T3 (pl) 2023-03-06
MX365423B (es) 2019-06-03
PT4119561T (pt) 2024-09-30
MX2014014239A (es) 2015-08-05
PE20150352A1 (es) 2015-03-16
ES2665338T3 (es) 2018-04-25
DK2854814T3 (en) 2018-03-12
EP3851107B1 (en) 2022-10-19
EP4119561A1 (en) 2023-01-18
CL2014003173A1 (es) 2015-02-27
KR20150021955A (ko) 2015-03-03
EP3590517A1 (en) 2020-01-08
WO2013177559A3 (en) 2014-01-16
BR112014028857B1 (pt) 2021-09-28
DK3851107T3 (da) 2022-11-21
EP2854814A4 (en) 2016-01-27
DK4119561T3 (da) 2024-09-30
PH12014502584B1 (en) 2015-01-21
HK1250014B (en) 2020-06-12
WO2013177559A2 (en) 2013-11-28
EP2854814B1 (en) 2018-01-31
ES2873949T3 (es) 2021-11-04
HK1208818A1 (en) 2016-03-18
IL235868A0 (en) 2015-01-29
CN104619328B (zh) 2018-10-02
PL4119561T3 (pl) 2024-11-25
PL3338781T3 (pl) 2020-03-31
BR112014028857A2 (pt) 2017-08-15
SG11201407682TA (en) 2014-12-30
RU2639867C2 (ru) 2017-12-25
AU2013266110B2 (en) 2017-04-20
EP3338781B1 (en) 2019-09-11
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ES2995026T3 (en) 2025-02-05
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JP6172871B2 (ja) 2017-08-02
NZ701469A (en) 2017-06-30
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EP2854814A2 (en) 2015-04-08
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ES2930298T3 (es) 2022-12-09
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ZA201408182B (en) 2017-09-27
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EP4119561B1 (en) 2024-09-11
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DK3338781T3 (da) 2019-12-09
RU2014152625A (ru) 2016-07-20
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AU2013266110A1 (en) 2014-11-20
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