JP2018507226A5 - - Google Patents
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- JP2018507226A5 JP2018507226A5 JP2017545908A JP2017545908A JP2018507226A5 JP 2018507226 A5 JP2018507226 A5 JP 2018507226A5 JP 2017545908 A JP2017545908 A JP 2017545908A JP 2017545908 A JP2017545908 A JP 2017545908A JP 2018507226 A5 JP2018507226 A5 JP 2018507226A5
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- JP
- Japan
- Prior art keywords
- group
- alkyl
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- combination
- hydrogen
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 125000000217 alkyl group Chemical group 0.000 claims description 44
- 229910052739 hydrogen Inorganic materials 0.000 claims description 38
- 229940126013 glucocorticoid receptor antagonist Drugs 0.000 claims description 29
- 239000003850 glucocorticoid receptor antagonist Substances 0.000 claims description 29
- 239000001257 hydrogen Substances 0.000 claims description 28
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 26
- 229910052736 halogen Inorganic materials 0.000 claims description 22
- 150000002367 halogens Chemical class 0.000 claims description 22
- 239000000275 Adrenocorticotropic Hormone Substances 0.000 claims description 20
- 101800000414 Corticotropin Proteins 0.000 claims description 20
- 102100027467 Pro-opiomelanocortin Human genes 0.000 claims description 20
- IDLFZVILOHSSID-OVLDLUHVSA-N corticotropin Chemical compound C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)NC(=O)[C@@H](N)CO)C1=CC=C(O)C=C1 IDLFZVILOHSSID-OVLDLUHVSA-N 0.000 claims description 20
- 229960000258 corticotropin Drugs 0.000 claims description 20
- NHXLMOGPVYXJNR-ATOGVRKGSA-N somatostatin Chemical compound C([C@H]1C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N1)[C@@H](C)O)NC(=O)CNC(=O)[C@H](C)N)C(O)=O)=O)[C@H](O)C)C1=CC=CC=C1 NHXLMOGPVYXJNR-ATOGVRKGSA-N 0.000 claims description 19
- 125000003545 alkoxy group Chemical group 0.000 claims description 18
- 125000001072 heteroaryl group Chemical group 0.000 claims description 18
- 150000002431 hydrogen Chemical class 0.000 claims description 18
- 229910052760 oxygen Inorganic materials 0.000 claims description 16
- 229910052717 sulfur Inorganic materials 0.000 claims description 16
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 14
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 14
- 206010028980 Neoplasm Diseases 0.000 claims description 14
- 229910052799 carbon Inorganic materials 0.000 claims description 14
- 125000005842 heteroatom Chemical group 0.000 claims description 14
- 229910052757 nitrogen Inorganic materials 0.000 claims description 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 10
- 125000003118 aryl group Chemical group 0.000 claims description 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 10
- -1 dimethylaminophenyl moiety Chemical group 0.000 claims description 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 8
- 239000000203 mixture Substances 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 230000003248 secreting effect Effects 0.000 claims description 8
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 6
- 150000003431 steroids Chemical group 0.000 claims description 6
- 102000005157 Somatostatin Human genes 0.000 claims description 5
- 108010056088 Somatostatin Proteins 0.000 claims description 5
- 229960000553 somatostatin Drugs 0.000 claims description 5
- PUDHBTGHUJUUFI-SCTWWAJVSA-N (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-n-[(2s,3r)-1-amino-3-hydroxy-1-oxobutan-2-yl]-19-[[(2r)-2-amino-3-naphthalen-2-ylpropanoyl]amino]-16-[(4-hydroxyphenyl)methyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-propan-2-yl-1,2-dithia-5,8,11,14,17-p Chemical compound C([C@H]1C(=O)N[C@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(N[C@@H](CSSC[C@@H](C(=O)N1)NC(=O)[C@H](N)CC=1C=C2C=CC=CC2=CC=1)C(=O)N[C@@H]([C@@H](C)O)C(N)=O)=O)C(C)C)C1=CC=C(O)C=C1 PUDHBTGHUJUUFI-SCTWWAJVSA-N 0.000 claims description 4
- YJDDXMSIMBMMGY-UHFFFAOYSA-N 2-cyclohexylpyrimidine Chemical group C1CCCCC1C1=NC=CC=N1 YJDDXMSIMBMMGY-UHFFFAOYSA-N 0.000 claims description 4
- 150000001204 N-oxides Chemical class 0.000 claims description 4
- 229960002437 lanreotide Drugs 0.000 claims description 4
- 229960002700 octreotide Drugs 0.000 claims description 4
- 125000006413 ring segment Chemical group 0.000 claims description 4
- 230000028327 secretion Effects 0.000 claims description 4
- 230000001225 therapeutic effect Effects 0.000 claims description 4
- DEQANNDTNATYII-OULOTJBUSA-N (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-19-[[(2r)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-n-[(2r,3r)-1,3-dihydroxybutan-2-yl]-7-[(1r)-1-hydroxyethyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxa Chemical compound C([C@@H](N)C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC=2C3=CC=CC=C3NC=2)NC(=O)[C@H](CC=2C=CC=CC=2)NC1=O)C(=O)N[C@H](CO)[C@H](O)C)C1=CC=CC=C1 DEQANNDTNATYII-OULOTJBUSA-N 0.000 claims description 3
- 238000009472 formulation Methods 0.000 claims description 3
- 108010021336 lanreotide Proteins 0.000 claims description 3
- 238000013268 sustained release Methods 0.000 claims description 3
- 239000012730 sustained-release form Substances 0.000 claims description 3
- ZCAUIZYRNPHJJO-CAMMJAKZSA-N (8s,10s,13s,14s)-10,13-dimethyl-1,2,6,7,8,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-3-one Chemical compound C([C@H]12)CC3=CC(=O)CC[C@]3(C)C1=CC[C@@]1(C)[C@H]2CCC1 ZCAUIZYRNPHJJO-CAMMJAKZSA-N 0.000 claims description 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims description 2
- 125000000530 1-propynyl group Chemical group [H]C([H])([H])C#C* 0.000 claims description 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 208000007740 Ectopic ACTH Syndrome Diseases 0.000 claims description 2
- 102000003676 Glucocorticoid Receptors Human genes 0.000 claims description 2
- 108090000079 Glucocorticoid Receptors Proteins 0.000 claims description 2
- 206010052399 Neuroendocrine tumour Diseases 0.000 claims description 2
- 108010016076 Octreotide Proteins 0.000 claims description 2
- 208000010067 Pituitary ACTH Hypersecretion Diseases 0.000 claims description 2
- 208000020627 Pituitary-dependent Cushing syndrome Diseases 0.000 claims description 2
- 229940124639 Selective inhibitor Drugs 0.000 claims description 2
- 125000002947 alkylene group Chemical group 0.000 claims description 2
- 208000011590 ectopic ACTH secretion syndrome Diseases 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- VKHAHZOOUSRJNA-GCNJZUOMSA-N mifepristone Chemical group C1([C@@H]2C3=C4CCC(=O)C=C4CC[C@H]3[C@@H]3CC[C@@]([C@]3(C2)C)(O)C#CC)=CC=C(N(C)C)C=C1 VKHAHZOOUSRJNA-GCNJZUOMSA-N 0.000 claims description 2
- 229960003248 mifepristone Drugs 0.000 claims description 2
- 208000016065 neuroendocrine neoplasm Diseases 0.000 claims description 2
- 201000011519 neuroendocrine tumor Diseases 0.000 claims description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 2
- CFODQUSMSYDHBS-UHFFFAOYSA-N octreotate Chemical compound O=C1NC(CC=2C=CC=CC=2)C(=O)NC(CC=2[C]3C=CC=CC3=NC=2)C(=O)NC(CCCCN)C(=O)NC(C(C)O)C(=O)NC(C(=O)NC(C(O)C)C(O)=O)CSSCC1NC(=O)C(N)CC1=CC=CC=C1 CFODQUSMSYDHBS-UHFFFAOYSA-N 0.000 claims description 2
- 125000004043 oxo group Chemical group O=* 0.000 claims description 2
- VMZMNAABQBOLAK-DBILLSOUSA-N pasireotide Chemical compound C([C@H]1C(=O)N2C[C@@H](C[C@H]2C(=O)N[C@H](C(=O)N[C@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@H](C(N[C@@H](CC=2C=CC(OCC=3C=CC=CC=3)=CC=2)C(=O)N1)=O)CCCCN)C=1C=CC=CC=1)OC(=O)NCCN)C1=CC=CC=C1 VMZMNAABQBOLAK-DBILLSOUSA-N 0.000 claims description 2
- 108700017947 pasireotide Proteins 0.000 claims description 2
- 229960005415 pasireotide Drugs 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 230000003637 steroidlike Effects 0.000 claims description 2
- 125000003944 tolyl group Chemical group 0.000 claims description 2
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 238000000034 method Methods 0.000 description 29
- 0 CCc1cc(C[C@](**)(CN(C)CC2)C2=C2)c2[n]1* Chemical compound CCc1cc(C[C@](**)(CN(C)CC2)C2=C2)c2[n]1* 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562127153P | 2015-03-02 | 2015-03-02 | |
| US62/127,153 | 2015-03-02 | ||
| PCT/US2016/019646 WO2016140867A1 (en) | 2015-03-02 | 2016-02-25 | Use of glucocorticoid receptor antagonist and somatostatin analogues to treat acth-secreting tumors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018507226A JP2018507226A (ja) | 2018-03-15 |
| JP2018507226A5 true JP2018507226A5 (https=) | 2019-01-31 |
| JP6821582B2 JP6821582B2 (ja) | 2021-01-27 |
Family
ID=56849054
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017545908A Active JP6821582B2 (ja) | 2015-03-02 | 2016-02-25 | Ａｃｔｈ分泌腫瘍を処置するための糖質コルチコイドレセプターアンタゴニストおよびソマトスタチンアナログの使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20180125856A1 (https=) |
| EP (1) | EP3265127B1 (https=) |
| JP (1) | JP6821582B2 (https=) |
| CN (1) | CN107530435A (https=) |
| AU (1) | AU2016226451B2 (https=) |
| CA (1) | CA2977591C (https=) |
| WO (1) | WO2016140867A1 (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12226412B2 (en) | 2012-05-25 | 2025-02-18 | Corcept Therapeutics, Inc. | Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators |
| US8859774B2 (en) | 2012-05-25 | 2014-10-14 | Corcept Therapeutics, Inc. | Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators |
| AU2018230429B2 (en) * | 2017-03-09 | 2023-06-15 | Corcept Therapeutics, Inc. | Use of glucocorticoid receptor modulators in the treatment of catecholamine-secreting tumors |
| WO2018236749A2 (en) | 2017-06-20 | 2018-12-27 | Corcept Therapeutics, Inc. | Methods of treating neuroepithelial tumors using selective glucocorticoid receptor modulators |
| CN113272322A (zh) * | 2018-10-08 | 2021-08-17 | Uab 研究基金会 | 神经内分泌癌靶向治疗 |
| US10946005B2 (en) | 2018-11-09 | 2021-03-16 | Corcept Therapeutics Incorporated | Methods for shrinking pituitary tumors |
| US11464764B2 (en) | 2018-12-19 | 2022-10-11 | Corcept Therapeutics Incorporated | Pharmaceutical formulations containing relacorilant, a heteroaryl-ketone fused azadecalin compound |
| SG11202105746TA (en) * | 2018-12-20 | 2021-07-29 | Corcept Therapeutics Inc | Methods for imaging and treatment of somatostatin-receptor positive tumors |
| 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 |
| 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 |
| WO2021242912A1 (en) | 2020-05-27 | 2021-12-02 | Corcept Therapeutics Incorporated | Concomitant administration of glucocorticoid receptor modulator relacorilant and paclitaxel, a dual substrate of cyp2c8 and cyp3a4 |
| WO2022134033A1 (en) | 2020-12-25 | 2022-06-30 | Corcept Therapeutics Incorporated | Methods of preparing heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators |
| 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 |
| KR20250164785A (ko) * | 2023-04-05 | 2025-11-25 | 크리네틱스 파마슈티칼스, 인크. | Acth 의존성 쿠싱 증후군의 치료를 위한 멜라노코르틴 아형-2 수용체(mc2r) 길항제 |
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| FR2528434B1 (fr) | 1982-06-11 | 1985-07-19 | Roussel Uclaf | Nouveaux 19-nor steroides substitues en 11b et eventuellement en 2, leur procede de preparation et leur application comme medicament |
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| FR2522328B1 (fr) | 1982-03-01 | 1986-02-14 | Roussel Uclaf | Nouveaux produits derives de la structure 3-ceto 4,9 19-nor steroides, leur procede de preparation et leur application comme medicaments |
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2016
- 2016-02-25 AU AU2016226451A patent/AU2016226451B2/en active Active
- 2016-02-25 JP JP2017545908A patent/JP6821582B2/ja active Active
- 2016-02-25 WO PCT/US2016/019646 patent/WO2016140867A1/en not_active Ceased
- 2016-02-25 CA CA2977591A patent/CA2977591C/en active Active
- 2016-02-25 CN CN201680023180.2A patent/CN107530435A/zh active Pending
- 2016-02-25 EP EP16759295.5A patent/EP3265127B1/en active Active
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2017
- 2017-06-19 US US15/627,391 patent/US20180125856A1/en not_active Abandoned