JP2021119136A5 - - Google Patents
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- JP2021119136A5 JP2021119136A5 JP2021060013A JP2021060013A JP2021119136A5 JP 2021119136 A5 JP2021119136 A5 JP 2021119136A5 JP 2021060013 A JP2021060013 A JP 2021060013A JP 2021060013 A JP2021060013 A JP 2021060013A JP 2021119136 A5 JP2021119136 A5 JP 2021119136A5
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- Prior art keywords
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- disease
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- Prior art date
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- 201000010099 disease Diseases 0.000 claims 6
- 238000000634 powder X-ray diffraction Methods 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 5
- 101700018814 KDM1A Proteins 0.000 claims 4
- 102100000513 KDM1A Human genes 0.000 claims 4
- 101700047494 LDL1 Proteins 0.000 claims 4
- 101700032951 SWM1 Proteins 0.000 claims 4
- 101710006827 Su(var)3-3 Proteins 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000011780 sodium chloride Substances 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 239000002904 solvent Substances 0.000 claims 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N HCl Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 229910000041 hydrogen chloride Inorganic materials 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- BDERNNFJNOPAEC-UHFFFAOYSA-N propanol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims 2
- 230000001105 regulatory Effects 0.000 claims 2
- 239000000243 solution Substances 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 238000001237 Raman spectrum Methods 0.000 claims 1
- 239000007864 aqueous solution Substances 0.000 claims 1
- 238000002425 crystallisation Methods 0.000 claims 1
- 230000005712 crystallization Effects 0.000 claims 1
- 238000004090 dissolution Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
Claims (12)
- ２４．８°及び１４．９°（±０．１°）の回折角２シータにＸＲＰＤピークを含むＸＲＰＤ回折パターンによって特徴付けられる、式（Ｉ）
の化合物又はその塩の結晶。
- １４．９°、１６．０°、２０．６°、及び２４．８°（±０．１°）の回折角２シータにＸＲＰＤピークを含むＸＲＰＤ回折パターンによって特徴付けられる、式（Ｉ）の化合物の二塩酸塩の結晶である、請求項１に記載の結晶。
- １４．９°、１６．０°、及び２４．８°（±０．２°）の回折角２シータにＸＲＰＤピークを含むＸＲＰＤ回折パターンによって特徴付けられる、式（Ｉ）
の化合物又はその塩の結晶。 - ラマンスペクトルにおける１２２５ｃｍ−１（±１ｃｍ−１）のバンドによって特徴付けられる、式（Ｉ）
の化合物又はその塩の結晶。 - 請求項１から４の何れか一項に記載の結晶の調製のための方法であって、反応工程：
ａ）式ＢＯＣ−（Ｉ）
の化合物の溶媒への溶解；
ｂ）ＨＣｌの溶液の添加；
ｃ）高温における水の添加；
ｄ）温度の漸減による生成物の結晶化
を含む方法。 - 工程ａ）における溶媒がＣ１−７アルコールである；及び／又は
工程ａ）における溶媒が１−プロパノールである；及び／又は
工程ｂ）における溶液が水溶液である；及び／又は
工程ｂ）において２〜２０当量のＨＣｌが添加される；及び／又は
工程ｃ）において少なくとも５当量の水が添加される；及び／又は
工程ｃ）が５０℃を超える温度で行なわれる；及び／又は
工程ｄ）における温度が−２０℃〜周囲温度の間の最終温度に下げられる；及び／又は
工程ｄ）における温度が１〜１００℃／時間の速度で下げられる、請求項５に記載の方法。 - 請求項１から４の何れか一項に記載の結晶並びに薬学的に許容される賦形剤を含む薬学的組成物。
- 請求項１から４の何れか一項に記載の結晶を含む治療活性物質。
- ＬＳＤ１に関連する疾患又はＬＳＤ１阻害剤によって調節される疾患の治療又は予防における使用のための、請求項７に記載の薬学的組成物。
- ＬＳＤ１に関連する疾患又はＬＳＤ１阻害剤によって調節される疾患の治療又は予防に有用な医薬の調製のための、請求項１から４の何れか一項に記載の結晶の使用。
- 前記疾患ががんである、請求項９に記載の薬学的組成物。
- 前記疾患ががんである、請求項１０に記載の使用。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15166641.9 | 2015-05-06 | ||
| EP15166641.9A EP3090998A1 (en) | 2015-05-06 | 2015-05-06 | Solid forms |
| JP2017557899A JP7005007B2 (ja) | 2015-05-06 | 2016-05-02 | 固体形態 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017557899A Division JP7005007B2 (ja) | 2015-05-06 | 2016-05-02 | 固体形態 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2021119136A JP2021119136A (ja) | 2021-08-12 |
| JP2021119136A5 true JP2021119136A5 (ja) | 2021-11-25 |
Family
ID=53039825
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017557899A Active JP7005007B2 (ja) | 2015-05-06 | 2016-05-02 | 固体形態 |
| JP2021060013A Pending JP2021119136A (ja) | 2015-05-06 | 2021-03-31 | 固体形態 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017557899A Active JP7005007B2 (ja) | 2015-05-06 | 2016-05-02 | 固体形態 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US10221125B2 (ja) |
| EP (2) | EP3090998A1 (ja) |
| JP (2) | JP7005007B2 (ja) |
| KR (1) | KR20180022660A (ja) |
| CN (1) | CN107735394B (ja) |
| AR (1) | AR104505A1 (ja) |
| AU (1) | AU2016259054B2 (ja) |
| BR (1) | BR112017023740B1 (ja) |
| CA (1) | CA2984203A1 (ja) |
| HK (2) | HK1245235A1 (ja) |
| IL (1) | IL255194B (ja) |
| MX (1) | MX2017014035A (ja) |
| PL (1) | PL3292100T3 (ja) |
| WO (1) | WO2016177656A1 (ja) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112014009306B1 (pt) | 2011-10-20 | 2021-07-20 | Oryzon Genomics S.A. | Compostos de (hetero)aril ciclopropilamina como inibidores de lsd1 |
| EP3090998A1 (en) | 2015-05-06 | 2016-11-09 | F. Hoffmann-La Roche AG | Solid forms |
| SG10201913331VA (en) | 2016-03-15 | 2020-03-30 | Oryzon Genomics Sa | Combinations of lsd1 inhibitors for use in the treatment of solid tumors |
| WO2017157813A1 (en) | 2016-03-15 | 2017-09-21 | F. Hoffmann-La Roche Ag | Combinations of lsd1 inhibitors for the treatment of hematological malignancies |
| EP3430015A1 (en) | 2016-03-16 | 2019-01-23 | Oryzon Genomics, S.A. | Methods to determine kdm1a target engagement and chemoprobes useful therefor |
| RS58951B1 (sr) | 2016-06-10 | 2019-08-30 | Oryzon Genomics Sa | Lečenje multiple skleroze |
| JP2020529995A (ja) | 2017-08-03 | 2020-10-15 | オリゾン ジェノミックス ソシエダッド アノニマ | 行動の変化の治療方法 |
| AU2019264231A1 (en) * | 2018-05-04 | 2020-10-22 | Oryzon Genomics, S.A. | Stable pharmaceutical formulation |
| SG11202109159VA (en) | 2019-03-20 | 2021-10-28 | Oryzon Genomics Sa | Methods of treating borderline personality disorder |
| CN113631164A (zh) | 2019-03-20 | 2021-11-09 | 奥莱松基因组股份有限公司 | 使用kdm1a抑制剂如化合物伐菲德司他治疗注意缺陷多动症的方法 |
| JP2022546908A (ja) | 2019-07-05 | 2022-11-10 | オリゾン・ゲノミクス・ソシエダッド・アノニマ | Ｋｄｍ１ａ阻害剤を使用した小細胞肺がんの個別化された処置のためのバイオマーカーおよび方法 |
| AU2022254484A1 (en) | 2021-04-08 | 2023-11-09 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors for treating myeloid cancers |
| WO2023217758A1 (en) | 2022-05-09 | 2023-11-16 | Oryzon Genomics, S.A. | Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors |
| WO2023217784A1 (en) | 2022-05-09 | 2023-11-16 | Oryzon Genomics, S.A. | Methods of treating nf1-mutant tumors using lsd1 inhibitors |
Family Cites Families (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2591717A1 (en) | 2004-12-16 | 2006-07-06 | President And Fellows Of Harvard College | Histone demethylation mediated by the nuclear amine oxidase homolog lsd1 |
| EP1704859B1 (en) | 2005-02-18 | 2010-08-11 | Universitätsklinikum Freiburg | Androgen receptor-dependent gene expression control by inhibiting the amine oxidase activity of lysine-specific demethylase (LSD1) |
| CA2619005A1 (en) | 2005-08-10 | 2007-02-22 | Johns Hopkins University | Polyamines useful as anti-parasitic and anti-cancer therapeutics and as lysine-specific demethylase inhibitors |
| JP2010523685A (ja) | 2007-04-13 | 2010-07-15 | ザ・ジョンズ・ホプキンス・ユニバーシティー | リジン特異的デメチラーゼ阻害剤 |
| US8916596B2 (en) | 2008-07-24 | 2014-12-23 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Preventing or treating viral infection using an inhibitor of the LSD1 protein, a MAO inhibitor or an inhibitor of LSD1 and a MAO inhibitor |
| EP2361242B1 (en) | 2008-10-17 | 2018-08-01 | Oryzon Genomics, S.A. | Oxidase inhibitors and their use |
| EP2389362B1 (en) | 2009-01-21 | 2019-12-11 | Oryzon Genomics, S.A. | Phenylcyclopropylamine derivatives and their medical use |
| US8389580B2 (en) | 2009-06-02 | 2013-03-05 | Duke University | Arylcyclopropylamines and methods of use |
| EP2258865A1 (en) | 2009-06-05 | 2010-12-08 | Universitätsklinikum Freiburg | Lysine-specific demethylase 1 (LSD1) is a biomarker for breast cancer |
| JPWO2010143582A1 (ja) | 2009-06-11 | 2012-11-22 | 公立大学法人名古屋市立大学 | フェニルシクロプロピルアミン誘導体及びｌｓｄ１阻害剤 |
| US9708255B2 (en) | 2009-08-18 | 2017-07-18 | Robert A. Casero | (bis)urea and (bis)thiourea compounds as epigenic modulators of lysine-specific demethylase 1 and methods of treating disorders |
| CN102639496B (zh) | 2009-09-25 | 2014-10-29 | 奥瑞泽恩基因组学股份有限公司 | 赖氨酸特异性脱甲基酶-1抑制剂及其应用 |
| US8946296B2 (en) | 2009-10-09 | 2015-02-03 | Oryzon Genomics S.A. | Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use |
| US9186337B2 (en) | 2010-02-24 | 2015-11-17 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for diseases and disorders associated with Hepadnaviridae |
| US9616058B2 (en) | 2010-02-24 | 2017-04-11 | Oryzon Genomics, S.A. | Potent selective LSD1 inhibitors and dual LSD1/MAO-B inhibitors for antiviral use |
| US20130197088A1 (en) | 2010-03-12 | 2013-08-01 | Robert A. Casero, JR. | Compositions and Methods for Combinations of Oligoamines with 2-Difluoromethylornithine (DFMO) |
| EP2560947B1 (en) | 2010-04-19 | 2016-10-12 | Oryzon Genomics, S.A. | Lysine specific demethylase-1 inhibitors and their use |
| JP5934184B2 (ja) | 2010-04-20 | 2016-06-15 | ウニヴェルシタ・デグリ・ストゥディ・ディ・ローマ・ラ・サピエンツァ | ヒストンデメチラーゼｌｓｄ１及び／又はｌｓｄ２の阻害剤としてのトラニルシプロミン誘導体 |
| AU2011284688B2 (en) | 2010-07-29 | 2015-07-16 | Oryzon Genomics S.A. | Arylcyclopropylamine based demethylase inhibitors of LSD1 and their medical use |
| EP2598480B1 (en) | 2010-07-29 | 2019-04-24 | Oryzon Genomics, S.A. | Cyclopropylamine derivatives useful as lsd1 inhibitors |
| WO2012034116A2 (en) | 2010-09-10 | 2012-03-15 | The Johns Hopkins University | Small molecules as epigenetic modulators of lysine-specific demethylase 1 and methods of treating disorders |
| US20130303545A1 (en) | 2010-09-30 | 2013-11-14 | Tamara Maes | Cyclopropylamine derivatives useful as lsd1 inhibitors |
| WO2012045883A1 (en) | 2010-10-08 | 2012-04-12 | Oryzon Genomics S.A. | Cyclopropylamine inhibitors of oxidases |
| WO2012072713A2 (en) | 2010-11-30 | 2012-06-07 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae |
| WO2012107498A1 (en) | 2011-02-08 | 2012-08-16 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
| US20140163041A1 (en) | 2011-02-08 | 2014-06-12 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders |
| ES2742805T3 (es) | 2011-03-25 | 2020-02-17 | Glaxosmithkline Ip No 2 Ltd | Ciclopropilaminas como inhibidores de LSD1 |
| EP2750671A2 (en) | 2011-05-19 | 2014-07-09 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for thrombosis and cardiovascular diseases |
| WO2012156531A2 (en) | 2011-05-19 | 2012-11-22 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for inflammatory diseases or conditions |
| CN107417549A (zh) | 2011-10-20 | 2017-12-01 | 奥莱松基因组股份有限公司 | 作为lsd1抑制剂的（杂）芳基环丙基胺化合物 |
| BR112014009306B1 (pt) | 2011-10-20 | 2021-07-20 | Oryzon Genomics S.A. | Compostos de (hetero)aril ciclopropilamina como inibidores de lsd1 |
| EP3090998A1 (en) | 2015-05-06 | 2016-11-09 | F. Hoffmann-La Roche AG | Solid forms |
| WO2016198649A1 (en) | 2015-06-12 | 2016-12-15 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| WO2017013061A1 (en) | 2015-07-17 | 2017-01-26 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| WO2017060319A1 (en) | 2015-10-09 | 2017-04-13 | F. Hoffmann-La Roche Ag | Gene expression biomarkers for personalized cancer care to epigenetic modifying agents |
| SG10201913331VA (en) | 2016-03-15 | 2020-03-30 | Oryzon Genomics Sa | Combinations of lsd1 inhibitors for use in the treatment of solid tumors |
| WO2017157813A1 (en) | 2016-03-15 | 2017-09-21 | F. Hoffmann-La Roche Ag | Combinations of lsd1 inhibitors for the treatment of hematological malignancies |
| EP3430015A1 (en) | 2016-03-16 | 2019-01-23 | Oryzon Genomics, S.A. | Methods to determine kdm1a target engagement and chemoprobes useful therefor |
| EP3535414A1 (en) | 2016-11-03 | 2019-09-11 | Oryzon Genomics, S.A. | Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents |
| EP3535420A1 (en) | 2016-11-03 | 2019-09-11 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
-
2015
- 2015-05-06 EP EP15166641.9A patent/EP3090998A1/en not_active Ceased
-
2016
- 2016-05-02 WO PCT/EP2016/059726 patent/WO2016177656A1/en active Application Filing
- 2016-05-02 US US15/571,945 patent/US10221125B2/en active Active
- 2016-05-02 CA CA2984203A patent/CA2984203A1/en active Pending
- 2016-05-02 EP EP16719864.7A patent/EP3292100B1/en active Active
- 2016-05-02 CN CN201680025229.8A patent/CN107735394B/zh active Active
- 2016-05-02 PL PL16719864.7T patent/PL3292100T3/pl unknown
- 2016-05-02 BR BR112017023740-7A patent/BR112017023740B1/pt active IP Right Grant
- 2016-05-02 AU AU2016259054A patent/AU2016259054B2/en active Active
- 2016-05-02 KR KR1020177035160A patent/KR20180022660A/ko active IP Right Grant
- 2016-05-02 MX MX2017014035A patent/MX2017014035A/es unknown
- 2016-05-02 JP JP2017557899A patent/JP7005007B2/ja active Active
- 2016-05-03 AR ARP160101249A patent/AR104505A1/es unknown
-
2017
- 2017-10-22 IL IL255194A patent/IL255194B/en active IP Right Grant
-
2018
- 2018-04-03 HK HK18104438.2A patent/HK1245235A1/zh unknown
- 2018-09-05 HK HK18111399.4A patent/HK1252089A1/zh unknown
-
2021
- 2021-03-31 JP JP2021060013A patent/JP2021119136A/ja active Pending
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