ES2753816T3 - Moduladores del receptor de glucocorticoides de azadecalina condensada con heteroaril-cetona - Google Patents

Moduladores del receptor de glucocorticoides de azadecalina condensada con heteroaril-cetona Download PDF

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ES2753816T3
ES2753816T3 ES18154256T ES18154256T ES2753816T3 ES 2753816 T3 ES2753816 T3 ES 2753816T3 ES 18154256 T ES18154256 T ES 18154256T ES 18154256 T ES18154256 T ES 18154256T ES 2753816 T3 ES2753816 T3 ES 2753816T3
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Hazel Hunt
Tony Johnson
Nicholas Ray
Iain Walters
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Corcept Therapeutics Inc
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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
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    • 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
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • 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
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    • 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
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    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
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  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Electroluminescent Light Sources (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un compuesto para su uso en el tratamiento de un cáncer seleccionado del grupo que consiste en cáncer de mama, cáncer de próstata, cáncer de ovario, cáncer de piel, cáncer de cerebro, cáncer de vejiga, cáncer de cuello uterino, cáncer de hígado, cáncer de pulmón, leucemia, linfoma, neuroblastoma y cáncer de huesos, teniendo el compuesto la fórmula:**Fórmula** en la que R1 es un anillo heteroarilo que tiene de 5 a 6 miembros de anillo y de 1 a 4 heteroátomos cada uno seleccionado independientemente entre el grupo que consiste en N, O y S, opcionalmente sustituido con 1-4 grupos cada uno seleccionado independientemente entre R1a; cada R1a se selecciona independientemente entre el grupo que consiste en hidrógeno, alquilo C1-6, halógeno, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, -CN, N-óxido, cicloalquilo C3-8 y heterocicloalquilo C3-8; el anillo J se selecciona entre el grupo que consiste en un anillo cicloalquilo, un anillo heterocicloalquilo, un anillo arilo y un anillo heteroarilo, en el que los anillos heterocicloalquilo y heteroarilo tienen de 5 a 6 miembros de anillo y de 1 a 4 heteroátomos cada uno seleccionado independientemente entre el grupo que consiste en N, O y S; cada R2 se selecciona independientemente del grupo que consiste en hidrógeno, alquilo C1-6, halógeno, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, alquil C1-6-alcoxi C1-6, -CN, -OH, -NR2aR2b, -C(O)R2a, -C(O)OR2a, -C(O)NR2aR2b, - SR2a, -S(O)R2a, -S(O)2R2a, cicloalquilo C3-8 y heterocicloalquilo C3-8, en el que los grupos heterocicloalquilo están opcionalmente sustituidos con 1-4 grupos R2c; como alternativa, dos grupos R2 unidos al mismo carbono se combinan para formar un grupo oxo (=O); como alternativa, dos grupos R2 se combinan para formar un anillo heterocicloalquilo que tiene de 5 a 6 miembros de anillo y de 1 a 3 heteroátomos seleccionados cada uno de ellos independientemente entre el grupo que consiste en N, O y S, en el que el anillo heterocicloalquilo está opcionalmente sustituido con 1 a 3 grupos R2d; cada uno de R2a y R2b se selecciona independientemente entre el grupo que consiste en hidrógeno y alquilo C1-6; cada R2c se selecciona independientemente entre el grupo que consiste en hidrógeno, halógeno, hidroxi, alcoxi C1- 6, haloalcoxi C1-6, -CN y -NR2aR2b; cada R2d se selecciona independientemente entre el grupo que consiste en hidrógeno y alquilo C1-6, o dos grupos R2d unidos al mismo átomo del anillo se combinan para formar (=O); R3 se selecciona entre el grupo que consiste en fenilo y piridilo, cada uno opcionalmente sustituido con 1-4 grupos R3a; cada R3a se selecciona independientemente entre el grupo que consiste en hidrógeno, halógeno y haloalquilo C1- 6; el subíndice n es un número entero de 0 a 3; o sales de los mismos.
ES18154256T 2012-05-25 2013-05-24 Moduladores del receptor de glucocorticoides de azadecalina condensada con heteroaril-cetona Active ES2753816T3 (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261651669P 2012-05-25 2012-05-25
US201261691083P 2012-08-20 2012-08-20
US201261715907P 2012-10-19 2012-10-19
US201361759520P 2013-02-01 2013-02-01
US201361781629P 2013-03-14 2013-03-14

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ES2753816T3 true ES2753816T3 (es) 2020-04-14

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ES21154665T Active ES2930298T3 (es) 2012-05-25 2013-05-24 Moduladores del receptor de glucocorticoides de azadecalina condensada con heteroaril-cetona
ES19188885T Active ES2873949T3 (es) 2012-05-25 2013-05-24 Moduladores del receptor de glucocorticoides de azadecalina condensada con heteroaril-cetona
ES13793417.0T Active ES2665338T3 (es) 2012-05-25 2013-05-24 Moduladores del receptor de glucocorticoides de azadecalina condensada con heteroaril-cetona
ES18154256T Active ES2753816T3 (es) 2012-05-25 2013-05-24 Moduladores del receptor de glucocorticoides de azadecalina condensada con heteroaril-cetona

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ES21154665T Active ES2930298T3 (es) 2012-05-25 2013-05-24 Moduladores del receptor de glucocorticoides de azadecalina condensada con heteroaril-cetona
ES19188885T Active ES2873949T3 (es) 2012-05-25 2013-05-24 Moduladores del receptor de glucocorticoides de azadecalina condensada con heteroaril-cetona
ES13793417.0T Active ES2665338T3 (es) 2012-05-25 2013-05-24 Moduladores del receptor de glucocorticoides de azadecalina condensada con heteroaril-cetona

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EP (6) EP3851107B1 (es)
JP (1) JP6172871B2 (es)
KR (1) KR102062640B1 (es)
CN (1) CN104619328B (es)
AU (1) AU2013266110C1 (es)
BR (1) BR112014028857B1 (es)
CA (1) CA2872260C (es)
CL (1) CL2014003173A1 (es)
DK (5) DK2854814T3 (es)
ES (4) ES2930298T3 (es)
HK (2) HK1208818A1 (es)
IL (1) IL235868A (es)
MX (1) MX365423B (es)
MY (1) MY172739A (es)
NZ (1) NZ701469A (es)
PE (1) PE20150352A1 (es)
PH (1) PH12014502584B1 (es)
PL (4) PL3338781T3 (es)
PT (5) PT3338781T (es)
RU (1) RU2639867C2 (es)
SG (1) SG11201407682TA (es)
WO (1) WO2013177559A2 (es)
ZA (1) ZA201408182B (es)

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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.
CA3065555A1 (en) 2017-06-20 2018-12-27 Corcept Therapeutics, Inc. Methods of treating neuroepithelial tumors using selective glucocorticoid receptor modulators
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CN113015528A (zh) * 2018-11-09 2021-06-22 科塞普特治疗公司 缩小垂体肿瘤的方法
AU2019404026B2 (en) 2018-12-19 2023-06-08 Corcept Therapeutics Incorporated Pharmaceutical formulations containing relacorilant, a heteroaryl-ketone fused azadecalin compound
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
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JP7444889B2 (ja) * 2018-12-20 2024-03-06 コーセプト セラピューティクス, インコーポレイテッド ソマトスタチン受容体陽性腫瘍のイメージング及び治療のための方法
AU2020226863B2 (en) 2019-02-22 2023-04-06 Corcept Therapeutics Incorporated Therapeutic uses of relacorilant, a heteroaryl-ketone fused azadecalin glucocorticoid receptor modulator
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
UA128573C2 (uk) 2019-12-11 2024-08-14 Корсепт Терапьютікс Інкорпорейтед Способи лікування підвищення маси тіла, індукованого антипсихотичними засобами, за допомогою мірикориланту
WO2021127376A1 (en) 2019-12-21 2021-06-24 Corcept Therapeutics Incorporated Treatment of, and differential diagnosis between, acth-dependent cushing's syndrome and acth-independent cushing's syndrome
WO2022134033A1 (en) * 2020-12-25 2022-06-30 Corcept Therapeutics Incorporated Methods of preparing heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
CN116829556A (zh) * 2021-02-03 2023-09-29 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
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PL3851107T3 (pl) 2023-03-06
JP2015517580A (ja) 2015-06-22
AU2013266110B2 (en) 2017-04-20
ES2665338T3 (es) 2018-04-25
PL3590517T3 (pl) 2021-09-20
NZ701469A (en) 2017-06-30
EP3338781B1 (en) 2019-09-11
RU2639867C2 (ru) 2017-12-25
CA2872260A1 (en) 2013-11-28
IL235868A (en) 2017-12-31
PE20150352A1 (es) 2015-03-16
PT3338781T (pt) 2019-11-29
EP2854814A2 (en) 2015-04-08
PT3851107T (pt) 2022-10-28
HK1208818A1 (en) 2016-03-18
EP2854814B1 (en) 2018-01-31
ES2873949T3 (es) 2021-11-04
EP3590517A1 (en) 2020-01-08
DK4119561T3 (da) 2024-09-30
WO2013177559A3 (en) 2014-01-16
BR112014028857B1 (pt) 2021-09-28
EP2854814A4 (en) 2016-01-27
PT2854814T (pt) 2018-03-15
PH12014502584A1 (en) 2015-01-21
IL235868A0 (en) 2015-01-29
CA2872260C (en) 2020-12-22
PT4119561T (pt) 2024-09-30
DK3590517T3 (da) 2021-05-03
CL2014003173A1 (es) 2015-02-27
BR112014028857A2 (pt) 2017-08-15
PL3338781T3 (pl) 2020-03-31
HK1250014B (zh) 2020-06-12
DK3338781T3 (da) 2019-12-09
AU2013266110A1 (en) 2014-11-20
ES2930298T3 (es) 2022-12-09
ZA201408182B (en) 2017-09-27
MY172739A (en) 2019-12-11
PT3590517T (pt) 2021-04-07
PH12014502584B1 (en) 2015-01-21
KR102062640B1 (ko) 2020-01-06
DK3851107T3 (da) 2022-11-21
EP3851107B1 (en) 2022-10-19
JP6172871B2 (ja) 2017-08-02
EP4119561A1 (en) 2023-01-18
EP3338781A1 (en) 2018-06-27
EP3590517B1 (en) 2021-03-17
EP3851107A1 (en) 2021-07-21
EP4434584A2 (en) 2024-09-25
DK2854814T3 (en) 2018-03-12
KR20150021955A (ko) 2015-03-03
CN104619328B (zh) 2018-10-02
RU2014152625A (ru) 2016-07-20
SG11201407682TA (en) 2014-12-30
MX365423B (es) 2019-06-03
CN104619328A (zh) 2015-05-13
PL2854814T3 (pl) 2018-07-31
EP4119561B1 (en) 2024-09-11
MX2014014239A (es) 2015-08-05
AU2013266110C1 (en) 2018-07-12
WO2013177559A2 (en) 2013-11-28

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