JP2015510933A5 - - Google Patents
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- Publication number
- JP2015510933A5 JP2015510933A5 JP2015501763A JP2015501763A JP2015510933A5 JP 2015510933 A5 JP2015510933 A5 JP 2015510933A5 JP 2015501763 A JP2015501763 A JP 2015501763A JP 2015501763 A JP2015501763 A JP 2015501763A JP 2015510933 A5 JP2015510933 A5 JP 2015510933A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- phenyl
- patient
- methylethyl
- cyclopentyl
- 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.)
- Granted
Links
- -1 2,6-bis (1-methylethyl) phenyl Chemical group 0.000 claims description 42
- VYWQTJWGWLKBQA-UHFFFAOYSA-N [amino(hydroxy)methylidene]azanium;chloride Chemical compound Cl.NC(N)=O VYWQTJWGWLKBQA-UHFFFAOYSA-N 0.000 claims description 23
- 239000003814 drug Substances 0.000 claims description 19
- 229940124597 therapeutic agent Drugs 0.000 claims description 19
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 claims description 16
- 230000001919 adrenal effect Effects 0.000 claims description 11
- 208000008448 Congenital adrenal hyperplasia Diseases 0.000 claims description 10
- 239000002246 antineoplastic agent Substances 0.000 claims description 10
- 229940127089 cytotoxic agent Drugs 0.000 claims description 10
- 208000014311 Cushing syndrome Diseases 0.000 claims description 8
- 229940088597 hormone Drugs 0.000 claims description 8
- 239000005556 hormone Substances 0.000 claims description 8
- 229960000890 hydrocortisone Drugs 0.000 claims description 8
- 208000005676 Adrenogenital syndrome Diseases 0.000 claims description 6
- 239000000055 Corticotropin-Releasing Hormone Substances 0.000 claims description 6
- 229960000258 corticotropin Drugs 0.000 claims description 6
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 6
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims description 5
- 230000015556 catabolic process Effects 0.000 claims description 5
- 238000006731 degradation reaction Methods 0.000 claims description 5
- 229960005167 everolimus Drugs 0.000 claims description 5
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims description 5
- 229960003105 metformin Drugs 0.000 claims description 5
- 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 5
- 229960003248 mifepristone Drugs 0.000 claims description 5
- 230000008685 targeting Effects 0.000 claims description 5
- SDOOGTHIDFZUNM-UHFFFAOYSA-N 1-[[1-[4-(dimethylamino)phenyl]cyclopentyl]methyl]-3-[2,6-di(propan-2-yl)phenyl]urea;hydrochloride Chemical compound Cl.CC(C)C1=CC=CC(C(C)C)=C1NC(=O)NCC1(C=2C=CC(=CC=2)N(C)C)CCCC1 SDOOGTHIDFZUNM-UHFFFAOYSA-N 0.000 claims description 4
- 206010000021 21-hydroxylase deficiency Diseases 0.000 claims description 4
- 101001034652 Homo sapiens Insulin-like growth factor 1 receptor Proteins 0.000 claims description 4
- 206010020571 Hyperaldosteronism Diseases 0.000 claims description 4
- 102100039688 Insulin-like growth factor 1 receptor Human genes 0.000 claims description 4
- 208000020990 adrenal cortex carcinoma Diseases 0.000 claims description 4
- 208000007128 adrenocortical carcinoma Diseases 0.000 claims description 4
- 239000003098 androgen Substances 0.000 claims description 4
- 239000005557 antagonist Substances 0.000 claims description 4
- 230000002146 bilateral effect Effects 0.000 claims description 4
- 239000003862 glucocorticoid Substances 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 239000002395 mineralocorticoid Substances 0.000 claims description 4
- 201000009395 primary hyperaldosteronism Diseases 0.000 claims description 4
- RZRPTBIGEANTGU-UHFFFAOYSA-N -Androst-4-ene-3,11,17-trione Natural products O=C1CCC2(C)C3C(=O)CC(C)(C(CC4)=O)C4C3CCC2=C1 RZRPTBIGEANTGU-UHFFFAOYSA-N 0.000 claims description 2
- 208000003200 Adenoma Diseases 0.000 claims description 2
- 208000006468 Adrenal Cortex Neoplasms Diseases 0.000 claims description 2
- PQSUYGKTWSAVDQ-ZVIOFETBSA-N Aldosterone Chemical compound C([C@@]1([C@@H](C(=O)CO)CC[C@H]1[C@@H]1CC2)C=O)[C@H](O)[C@@H]1[C@]1(C)C2=CC(=O)CC1 PQSUYGKTWSAVDQ-ZVIOFETBSA-N 0.000 claims description 2
- PQSUYGKTWSAVDQ-UHFFFAOYSA-N Aldosterone Natural products C1CC2C3CCC(C(=O)CO)C3(C=O)CC(O)C2C2(C)C1=CC(=O)CC2 PQSUYGKTWSAVDQ-UHFFFAOYSA-N 0.000 claims description 2
- JWBOIMRXGHLCPP-UHFFFAOYSA-N Chloditan Chemical group C=1C=CC=C(Cl)C=1C(C(Cl)Cl)C1=CC=C(Cl)C=C1 JWBOIMRXGHLCPP-UHFFFAOYSA-N 0.000 claims description 2
- FMGSKLZLMKYGDP-UHFFFAOYSA-N Dehydroepiandrosterone Natural products C1C(O)CCC2(C)C3CCC(C)(C(CC4)=O)C4C3CC=C21 FMGSKLZLMKYGDP-UHFFFAOYSA-N 0.000 claims description 2
- 208000007740 Ectopic ACTH Syndrome Diseases 0.000 claims description 2
- 102000008109 Mixed Function Oxygenases Human genes 0.000 claims description 2
- 108010074633 Mixed Function Oxygenases Proteins 0.000 claims description 2
- 208000010067 Pituitary ACTH Hypersecretion Diseases 0.000 claims description 2
- 230000002159 abnormal effect Effects 0.000 claims description 2
- RZRPTBIGEANTGU-IRIMSJTPSA-N adrenosterone Chemical compound O=C1CC[C@]2(C)[C@H]3C(=O)C[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 RZRPTBIGEANTGU-IRIMSJTPSA-N 0.000 claims description 2
- 229960002478 aldosterone Drugs 0.000 claims description 2
- AEMFNILZOJDQLW-QAGGRKNESA-N androst-4-ene-3,17-dione Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 AEMFNILZOJDQLW-QAGGRKNESA-N 0.000 claims description 2
- 229960005471 androstenedione Drugs 0.000 claims description 2
- AEMFNILZOJDQLW-UHFFFAOYSA-N androstenedione Natural products O=C1CCC2(C)C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 AEMFNILZOJDQLW-UHFFFAOYSA-N 0.000 claims description 2
- 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 2
- 230000007812 deficiency Effects 0.000 claims description 2
- FMGSKLZLMKYGDP-USOAJAOKSA-N dehydroepiandrosterone Chemical compound C1[C@@H](O)CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC=C21 FMGSKLZLMKYGDP-USOAJAOKSA-N 0.000 claims description 2
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims description 2
- 208000011590 ectopic ACTH secretion syndrome Diseases 0.000 claims description 2
- 230000001394 metastastic effect Effects 0.000 claims description 2
- 206010061289 metastatic neoplasm Diseases 0.000 claims description 2
- 229960000350 mitotane Drugs 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 229960002847 prasterone Drugs 0.000 claims description 2
- 208000024891 symptom Diseases 0.000 claims description 2
- 208000011580 syndromic disease Diseases 0.000 claims description 2
- BVHCJYWPHHHKRC-UHFFFAOYSA-N Cl.CN(C1=CC=C(C=C1)C1(CCCC1)CNC(=O)N)C Chemical compound Cl.CN(C1=CC=C(C=C1)C1(CCCC1)CNC(=O)N)C BVHCJYWPHHHKRC-UHFFFAOYSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 description 30
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261614269P | 2012-03-22 | 2012-03-22 | |
| US61/614,269 | 2012-03-22 | ||
| PCT/US2013/031068 WO2013142214A1 (en) | 2012-03-22 | 2013-03-13 | Compounds and methods for treating aberrant adrenocartical cell disorders |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017124186A Division JP6317016B2 (ja) | 2012-03-22 | 2017-06-26 | 異常な副腎皮質細胞障害を処置するための化合物および方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015510933A JP2015510933A (ja) | 2015-04-13 |
| JP2015510933A5 true JP2015510933A5 (https=) | 2016-05-12 |
| JP6234987B2 JP6234987B2 (ja) | 2017-11-22 |
Family
ID=48014328
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015501763A Active JP6234987B2 (ja) | 2012-03-22 | 2013-03-13 | 異常な副腎皮質細胞障害を処置するための化合物および方法 |
| JP2017124186A Active JP6317016B2 (ja) | 2012-03-22 | 2017-06-26 | 異常な副腎皮質細胞障害を処置するための化合物および方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017124186A Active JP6317016B2 (ja) | 2012-03-22 | 2017-06-26 | 異常な副腎皮質細胞障害を処置するための化合物および方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (5) | US9107883B2 (https=) |
| EP (1) | EP2838523A1 (https=) |
| JP (2) | JP6234987B2 (https=) |
| CN (2) | CN106236741A (https=) |
| AU (2) | AU2013235535B2 (https=) |
| BR (1) | BR112014023517B1 (https=) |
| CA (1) | CA2867668A1 (https=) |
| HK (1) | HK1206607A1 (https=) |
| IN (1) | IN2014DN08604A (https=) |
| MX (1) | MX355129B (https=) |
| NZ (1) | NZ630828A (https=) |
| WO (1) | WO2013142214A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2748238B2 (ja) | 1994-12-20 | 1998-05-06 | 新興機械工業株式会社 | ばね製造装置の足起こし装置 |
| CN106236741A (zh) * | 2012-03-22 | 2016-12-21 | 密歇根大学董事会 | 用于治疗异常肾上腺皮质细胞疾病的化合物和方法 |
| WO2015048543A1 (en) * | 2013-09-26 | 2015-04-02 | Atterocor, Inc. | Treating disorders associated with aberrant adrenocortical cell behavior |
| EP3197435A1 (en) * | 2014-09-26 | 2017-08-02 | Millendo Therapeutics, Inc. | Solid drug form of n-(2,6-bis(1-methylethyl)phenyl)-n'-((1-(4-(dimethylamino)phenyl)cyclopentyl) methyl)urea hydrochloride and compositions, methods and kits related thereto |
| US20160287565A1 (en) * | 2015-04-06 | 2016-10-06 | Millendo Therapeutics, Inc. | Combination therapy for treating disorders associated with excess cortisol production |
| WO2017011302A1 (en) * | 2015-07-10 | 2017-01-19 | Millendo Therapeutics, Inc. | Enhanced bioavailability of n-(2,6-bis(1-methylethyl) phenyl)-n'-((1-(4-(dimethylamino)-phenyl)cyclopentyl) methyl)urea hydrochloride |
| EP3461480A1 (en) | 2017-09-27 | 2019-04-03 | Onxeo | Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer |
| US11202787B2 (en) | 2018-07-02 | 2021-12-21 | Corcept Therapeutics, Inc. | Use of ACTH in assessment and prophylactic treatment of hypokalemia associated with glucocorticoid receptor modulator treatment of Cushing's syndrome patients |
| US10231983B1 (en) | 2018-08-22 | 2019-03-19 | Corcept Therapeutics, Inc. | Use of ACTH in assessment and prophylactic treatment of hypokalemia associated with glucocorticoid receptor modulator treatment of Cushing's syndrome patients |
| US10780097B2 (en) | 2018-07-02 | 2020-09-22 | Corcept Therapeutics, Inc. | Use of cortisol in assessment and prophylactic treatment of hypokalemia associated with glucocorticoid receptor modulator treatment of Cushing's syndrome patients |
| WO2020252054A1 (en) * | 2019-06-11 | 2020-12-17 | The Regents Of The University Of Michigan | Compositions and methods for treating cancer |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| US5015644A (en) | 1987-06-02 | 1991-05-14 | Warner-Lambert Company | Antihyperlipidemic and antiatherosclerotic urea and carbamate compounds |
| JP5330260B2 (ja) * | 2006-12-06 | 2013-10-30 | スミスクライン ビーチャム コーポレーション | 二環式化合物ならびに抗糖尿病薬としての使用 |
| US20090192220A1 (en) * | 2007-11-19 | 2009-07-30 | Ore Pharmaceuticals Inc. | Treatment for solid tumors |
| CN106236741A (zh) * | 2012-03-22 | 2016-12-21 | 密歇根大学董事会 | 用于治疗异常肾上腺皮质细胞疾病的化合物和方法 |
-
2013
- 2013-03-13 CN CN201610595176.5A patent/CN106236741A/zh active Pending
- 2013-03-13 CN CN201380015269.0A patent/CN104302283B/zh active Active
- 2013-03-13 WO PCT/US2013/031068 patent/WO2013142214A1/en not_active Ceased
- 2013-03-13 HK HK15107166.6A patent/HK1206607A1/xx unknown
- 2013-03-13 BR BR112014023517-1A patent/BR112014023517B1/pt active IP Right Grant
- 2013-03-13 JP JP2015501763A patent/JP6234987B2/ja active Active
- 2013-03-13 NZ NZ630828A patent/NZ630828A/en unknown
- 2013-03-13 CA CA2867668A patent/CA2867668A1/en not_active Abandoned
- 2013-03-13 AU AU2013235535A patent/AU2013235535B2/en active Active
- 2013-03-13 IN IN8604DEN2014 patent/IN2014DN08604A/en unknown
- 2013-03-13 EP EP13712998.7A patent/EP2838523A1/en not_active Withdrawn
- 2013-03-13 US US13/802,047 patent/US9107883B2/en active Active
- 2013-03-13 MX MX2014011188A patent/MX355129B/es active IP Right Grant
-
2015
- 2015-07-13 US US14/798,237 patent/US9446010B2/en active Active
-
2016
- 2016-06-01 US US15/170,682 patent/US9877937B2/en active Active
-
2017
- 2017-06-26 JP JP2017124186A patent/JP6317016B2/ja active Active
- 2017-11-17 AU AU2017261632A patent/AU2017261632A1/en not_active Abandoned
- 2017-12-12 US US15/839,647 patent/US20180256524A1/en not_active Abandoned
-
2021
- 2021-06-30 US US17/364,464 patent/US20220160662A1/en not_active Abandoned
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