JP2017036314A5 - - Google Patents
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- JP2017036314A5 JP2017036314A5 JP2016201383A JP2016201383A JP2017036314A5 JP 2017036314 A5 JP2017036314 A5 JP 2017036314A5 JP 2016201383 A JP2016201383 A JP 2016201383A JP 2016201383 A JP2016201383 A JP 2016201383A JP 2017036314 A5 JP2017036314 A5 JP 2017036314A5
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- JP
- Japan
- Prior art keywords
- cancer
- compound
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- pharmaceutical composition
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- 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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- 150000001875 compounds Chemical class 0.000 claims 11
- 206010028980 Neoplasm Diseases 0.000 claims 10
- 201000011510 cancer Diseases 0.000 claims 10
- 239000003795 chemical substances by application Substances 0.000 claims 10
- 239000003112 inhibitor Substances 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 239000003814 drug Substances 0.000 claims 7
- 206010006187 Breast cancer Diseases 0.000 claims 4
- 208000026310 Breast neoplasm Diseases 0.000 claims 4
- 206010009944 Colon cancer Diseases 0.000 claims 4
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 4
- 102000004190 Enzymes Human genes 0.000 claims 4
- 108090000790 Enzymes Proteins 0.000 claims 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 4
- 206010029260 Neuroblastoma Diseases 0.000 claims 4
- 206010033128 Ovarian cancer Diseases 0.000 claims 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 4
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 4
- 108010022394 Threonine synthase Proteins 0.000 claims 4
- 102000005497 Thymidylate Synthase Human genes 0.000 claims 4
- 238000010914 gene-directed enzyme pro-drug therapy Methods 0.000 claims 4
- 208000014829 head and neck neoplasm Diseases 0.000 claims 4
- 201000005202 lung cancer Diseases 0.000 claims 4
- 208000020816 lung neoplasm Diseases 0.000 claims 4
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 4
- 201000001441 melanoma Diseases 0.000 claims 4
- 201000002528 pancreatic cancer Diseases 0.000 claims 4
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 4
- 230000002062 proliferating effect Effects 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- -1 9-fluorenylmethyloxycarbonyl Chemical group 0.000 claims 3
- 125000000524 functional group Chemical group 0.000 claims 3
- 102000052567 Anaphase-Promoting Complex-Cyclosome Apc1 Subunit Human genes 0.000 claims 2
- 108700004581 Anaphase-Promoting Complex-Cyclosome Apc1 Subunit Proteins 0.000 claims 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims 2
- 102000003915 DNA Topoisomerases Human genes 0.000 claims 2
- 108090000323 DNA Topoisomerases Proteins 0.000 claims 2
- 230000005778 DNA damage Effects 0.000 claims 2
- 231100000277 DNA damage Toxicity 0.000 claims 2
- 230000005971 DNA damage repair Effects 0.000 claims 2
- 239000012623 DNA damaging agent Substances 0.000 claims 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 2
- 208000032612 Glial tumor Diseases 0.000 claims 2
- 206010018338 Glioma Diseases 0.000 claims 2
- 208000017604 Hodgkin disease Diseases 0.000 claims 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 2
- 208000005410 Mediastinal Neoplasms Diseases 0.000 claims 2
- 206010027476 Metastases Diseases 0.000 claims 2
- 102000029749 Microtubule Human genes 0.000 claims 2
- 108091022875 Microtubule Proteins 0.000 claims 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 2
- 102000007537 Type II DNA Topoisomerases Human genes 0.000 claims 2
- 108010046308 Type II DNA Topoisomerases Proteins 0.000 claims 2
- 208000008385 Urogenital Neoplasms Diseases 0.000 claims 2
- 201000005188 adrenal gland cancer Diseases 0.000 claims 2
- 208000024447 adrenal gland neoplasm Diseases 0.000 claims 2
- 230000000340 anti-metabolite Effects 0.000 claims 2
- 229940100197 antimetabolite Drugs 0.000 claims 2
- 239000002256 antimetabolite Substances 0.000 claims 2
- 201000009036 biliary tract cancer Diseases 0.000 claims 2
- 208000020790 biliary tract neoplasm Diseases 0.000 claims 2
- 238000002512 chemotherapy Methods 0.000 claims 2
- 235000005911 diet Nutrition 0.000 claims 2
- 230000037213 diet Effects 0.000 claims 2
- 235000020805 dietary restrictions Nutrition 0.000 claims 2
- 201000004101 esophageal cancer Diseases 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 229960005277 gemcitabine Drugs 0.000 claims 2
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims 2
- 238000001415 gene therapy Methods 0.000 claims 2
- 230000005865 ionizing radiation Effects 0.000 claims 2
- 201000011061 large intestine cancer Diseases 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 208000014018 liver neoplasm Diseases 0.000 claims 2
- 210000004072 lung Anatomy 0.000 claims 2
- 230000036210 malignancy Effects 0.000 claims 2
- 208000026037 malignant tumor of neck Diseases 0.000 claims 2
- 201000000349 mediastinal cancer Diseases 0.000 claims 2
- 230000009401 metastasis Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 210000004688 microtubule Anatomy 0.000 claims 2
- 230000000394 mitotic effect Effects 0.000 claims 2
- 201000000050 myeloid neoplasm Diseases 0.000 claims 2
- 201000011682 nervous system cancer Diseases 0.000 claims 2
- 201000008968 osteosarcoma Diseases 0.000 claims 2
- 238000002428 photodynamic therapy Methods 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- 238000001959 radiotherapy Methods 0.000 claims 2
- 230000011664 signaling Effects 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 201000002314 small intestine cancer Diseases 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 230000008685 targeting Effects 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 201000002510 thyroid cancer Diseases 0.000 claims 2
- 208000037964 urogenital cancer Diseases 0.000 claims 2
- XYFCBTPGUUZFHI-UHFFFAOYSA-N Phosphine Natural products P XYFCBTPGUUZFHI-UHFFFAOYSA-N 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims 1
- FJDQFPXHSGXQBY-UHFFFAOYSA-L caesium carbonate Chemical compound [Cs+].[Cs+].[O-]C([O-])=O FJDQFPXHSGXQBY-UHFFFAOYSA-L 0.000 claims 1
- 229910000024 caesium carbonate Inorganic materials 0.000 claims 1
- 230000008878 coupling Effects 0.000 claims 1
- 238000010168 coupling process Methods 0.000 claims 1
- 238000005859 coupling reaction Methods 0.000 claims 1
- 238000006880 cross-coupling reaction Methods 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 239000003960 organic solvent Substances 0.000 claims 1
- UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 claims 1
- 229910000073 phosphorus hydride Inorganic materials 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261647200P | 2012-05-15 | 2012-05-15 | |
| US61/647,200 | 2012-05-15 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015512120A Division JP6027230B2 (ja) | 2012-05-15 | 2013-05-14 | ５−［［４−［［モルホリン−２−イル］メチルアミノ］−５−（トリフルオロメチル）−２−ピリジル］アミノ］ピラジン−２−カルボニトリルおよびその治療上の使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017036314A JP2017036314A (ja) | 2017-02-16 |
| JP2017036314A5 true JP2017036314A5 (enExample) | 2017-06-01 |
| JP6362652B2 JP6362652B2 (ja) | 2018-07-25 |
Family
ID=48468659
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015512120A Active JP6027230B2 (ja) | 2012-05-15 | 2013-05-14 | ５−［［４−［［モルホリン−２−イル］メチルアミノ］−５−（トリフルオロメチル）−２−ピリジル］アミノ］ピラジン−２−カルボニトリルおよびその治療上の使用 |
| JP2016201383A Active JP6362652B2 (ja) | 2012-05-15 | 2016-10-13 | ５−［［４−［［モルホリン−２−イル］メチルアミノ］−５−（トリフルオロメチル）−２−ピリジル］アミノ］ピラジン−２−カルボニトリルおよびその治療上の使用 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015512120A Active JP6027230B2 (ja) | 2012-05-15 | 2013-05-14 | ５−［［４−［［モルホリン−２−イル］メチルアミノ］−５−（トリフルオロメチル）−２−ピリジル］アミノ］ピラジン−２−カルボニトリルおよびその治療上の使用 |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US9663503B2 (enExample) |
| EP (2) | EP2855448B1 (enExample) |
| JP (2) | JP6027230B2 (enExample) |
| KR (6) | KR20240023685A (enExample) |
| CN (2) | CN104302635B (enExample) |
| AU (2) | AU2013261605B2 (enExample) |
| BR (1) | BR112014026801B1 (enExample) |
| CA (1) | CA2870837C (enExample) |
| DK (1) | DK2855448T3 (enExample) |
| ES (2) | ES2981584T3 (enExample) |
| IL (1) | IL235133A (enExample) |
| IN (1) | IN2014DN09221A (enExample) |
| MX (1) | MX358819B (enExample) |
| NZ (1) | NZ702050A (enExample) |
| PL (1) | PL2855448T3 (enExample) |
| RU (1) | RU2659786C2 (enExample) |
| SG (1) | SG11201407238VA (enExample) |
| WO (1) | WO2013171470A1 (enExample) |
| ZA (1) | ZA201408452B (enExample) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6073910B2 (ja) | 2011-11-09 | 2017-02-01 | キャンサー・リサーチ・テクノロジー・リミテッド | ５−（ピリジン−２−イル−アミノ）−ピラジン−２−カルボニトリル化合物及びその治療使用 |
| JP6027230B2 (ja) * | 2012-05-15 | 2016-11-16 | キャンサー・リサーチ・テクノロジー・リミテッド | ５−［［４−［［モルホリン−２−イル］メチルアミノ］−５−（トリフルオロメチル）−２−ピリジル］アミノ］ピラジン−２−カルボニトリルおよびその治療上の使用 |
| SMT202000713T1 (it) | 2012-12-07 | 2021-03-15 | Vertex Pharma | Pirazolo [1,5-a] pirimidine utili come inibitori dell'atr chinasi per il trattamento di malattie del cancro |
| JP2016512815A (ja) | 2013-03-15 | 2016-05-09 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | Ａｔｒキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体 |
| HUE046727T2 (hu) | 2013-12-06 | 2020-03-30 | Vertex Pharma | Az ATR-kináz inhibitoraként használható vegyület, 2-amino-6-fluoro-N-[5-fluoro-piridin-3-IL]-pirazolo-[1,5-A]-pirimidin-3-karboxamid, ennek elõállítása, különbözõ szilárd formái és ezek radioaktív nyomjelzett származékai |
| CN107074863B (zh) | 2014-06-05 | 2019-12-03 | 沃泰克斯药物股份有限公司 | Atr激酶抑制剂的制备方法及其不同的固体形式 |
| PL3157566T3 (pl) * | 2014-06-17 | 2019-10-31 | Vertex Pharma | Metoda leczenia nowotworu przy użyciu kombinacji inhibitorów chk1 i atr |
| KR102678021B1 (ko) | 2015-09-30 | 2024-06-26 | 버텍스 파마슈티칼스 인코포레이티드 | Dna 손상제와 병용되는, atr 저해제를 포함하는 암 치료용 약제학적 조성물 |
| WO2018094325A1 (en) * | 2016-11-18 | 2018-05-24 | The Trustees Of Columbia University In The City Of New York | Therapeutic modulation of oncogenes by pharmacologic top2 targeting for cancer |
| US20200108074A1 (en) * | 2017-03-31 | 2020-04-09 | Seattle Genetics, Inc. | Combinations of chk1- and wee1- inhibitors |
| KR102645511B1 (ko) * | 2017-04-10 | 2024-03-08 | 시에라 온코로지 엘엘씨 | 종양 성장을 저해하는 CHK1(SRA737)/PARPi 조합 방법 |
| WO2018191299A1 (en) * | 2017-04-10 | 2018-10-18 | Sierra Oncology, Inc. | Chk1(sra737)wee1 inhibitor combination methods of inhibiting tumor growth |
| AU2018278336A1 (en) * | 2017-06-01 | 2020-01-16 | Crt Pioneer Fund Lp | Biomarkers and patient selection strategies |
| CN107266897B (zh) * | 2017-08-04 | 2019-05-14 | 上海跃贝新材料科技股份有限公司 | 一种低粘度矿物增强pc/pet合金材料及其制备方法 |
| AU2019224164A1 (en) * | 2018-02-26 | 2020-10-01 | Crt Pioneer Fund Lp | Methods of treatment of cancer comprising Chk1 inhibitors |
| JP2022523028A (ja) * | 2019-01-25 | 2022-04-21 | ヌメディー， インコーポレイテッド | 特発性肺線維症を処置するための方法 |
| CA3135165A1 (en) * | 2019-03-28 | 2020-10-01 | Sierra Oncology, Inc. | Methods of treating cancer with chk1 inhibitors |
| WO2020232154A2 (en) * | 2019-05-14 | 2020-11-19 | Sierra Oncology, Inc. | Methods of treating cancer using chk1 inhibitors |
| CN110872277B (zh) * | 2019-11-14 | 2021-06-04 | 浙江大学 | N-取代芳环-2-氨基嘧啶类化合物及用途 |
| CN110680928B (zh) * | 2019-12-06 | 2020-04-28 | 深圳前海港影生物科技有限公司 | 抑制黑色素合成的偶联物及其在药品和化妆品中的应用 |
| CN110684083B (zh) * | 2019-12-06 | 2020-05-15 | 北京诺赛启研再生医学研究院有限公司 | 抑制黑色素合成的偶联物ii及其在药品和化妆品中的应用 |
| TW202204348A (zh) * | 2020-04-07 | 2022-02-01 | 美商西爾拉癌症醫學公司 | Ｃｈｋ１抑制劑之合成方法 |
| US20240351992A1 (en) * | 2021-08-17 | 2024-10-24 | Glaxosmithkline Intellectual Property (No.3) Limited | Preparation of p2x3 antagonist |
| WO2025101691A1 (en) | 2023-11-08 | 2025-05-15 | Exelixis, Inc. | Methods for treating cancer using compounds that inhibit pkmyt1 |
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| US3773778A (en) | 1972-01-24 | 1973-11-20 | Squibb & Sons Inc | Sulfur derivatives of pyrazolo (3,4-b)pyridines |
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| EP0836605B1 (en) | 1995-07-06 | 2002-02-06 | Novartis AG | Pyrrolopyrimidines and processes for the preparation thereof |
| DE60221866T2 (de) | 2001-10-19 | 2008-05-29 | Ortho-Mcneil Pharmaceutical, Inc. | 2-PHENYL BENZIMIDAZOLE UND IMIDAZO-i4,5ö-PYRIDINE ALS CDS1/CHK2-INHIBITOREN UND ADJUVANTIEN IN DER CHEMOTHERAPIE ODER STRAHLUNGSTHERAPIE ZUR BEHANDLUNG VON KREBS |
| JP5039268B2 (ja) | 2001-10-26 | 2012-10-03 | アベンティス・ファーマスーティカルズ・インコーポレイテツド | ベンゾイミダゾールおよび類縁体および蛋白キナーゼ阻害剤としてのその使用 |
| CA2464934A1 (en) | 2001-10-31 | 2003-05-08 | Bayer Healthcare Ag | Pyrimido [4,5-b] indole derivatives |
| CA2484209C (en) * | 2002-05-03 | 2013-06-11 | Exelixis, Inc. | Protein kinase modulators and methods of use |
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| ES2344007T3 (es) | 2003-10-14 | 2010-08-16 | The Arizona Board Of Regents On Behalf Of The University Of Arizona | Inhibidores proteina quinasa. |
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| GB0719644D0 (en) | 2007-10-05 | 2007-11-14 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| GB0803018D0 (en) * | 2008-02-19 | 2008-03-26 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| JP6073910B2 (ja) | 2011-11-09 | 2017-02-01 | キャンサー・リサーチ・テクノロジー・リミテッド | ５−（ピリジン−２−イル−アミノ）−ピラジン−２−カルボニトリル化合物及びその治療使用 |
| JP6027230B2 (ja) * | 2012-05-15 | 2016-11-16 | キャンサー・リサーチ・テクノロジー・リミテッド | ５−［［４−［［モルホリン−２−イル］メチルアミノ］−５−（トリフルオロメチル）−２−ピリジル］アミノ］ピラジン−２−カルボニトリルおよびその治療上の使用 |
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2013
- 2013-05-14 JP JP2015512120A patent/JP6027230B2/ja active Active
- 2013-05-14 EP EP13723910.9A patent/EP2855448B1/en active Active
- 2013-05-14 ES ES17152400T patent/ES2981584T3/es active Active
- 2013-05-14 ES ES13723910.9T patent/ES2624307T3/es active Active
- 2013-05-14 CA CA2870837A patent/CA2870837C/en active Active
- 2013-05-14 AU AU2013261605A patent/AU2013261605B2/en active Active
- 2013-05-14 MX MX2014012881A patent/MX358819B/es active IP Right Grant
- 2013-05-14 PL PL13723910T patent/PL2855448T3/pl unknown
- 2013-05-14 KR KR1020247004407A patent/KR20240023685A/ko not_active Withdrawn
- 2013-05-14 NZ NZ702050A patent/NZ702050A/en unknown
- 2013-05-14 CN CN201380025541.3A patent/CN104302635B/zh active Active
- 2013-05-14 US US14/396,338 patent/US9663503B2/en active Active
- 2013-05-14 KR KR1020227037439A patent/KR102635954B1/ko active Active
- 2013-05-14 KR KR1020147031572A patent/KR102090792B1/ko active Active
- 2013-05-14 KR KR1020217012299A patent/KR102341637B1/ko active Active
- 2013-05-14 KR KR1020217041302A patent/KR20210156333A/ko not_active Ceased
- 2013-05-14 CN CN201610652725.8A patent/CN106279142B/zh active Active
- 2013-05-14 EP EP17152400.2A patent/EP3210980B1/en active Active
- 2013-05-14 DK DK13723910.9T patent/DK2855448T3/en active
- 2013-05-14 BR BR112014026801-0A patent/BR112014026801B1/pt active IP Right Grant
- 2013-05-14 KR KR1020207007411A patent/KR102246265B1/ko active Active
- 2013-05-14 WO PCT/GB2013/051233 patent/WO2013171470A1/en not_active Ceased
- 2013-05-14 SG SG11201407238VA patent/SG11201407238VA/en unknown
- 2013-05-14 RU RU2014147105A patent/RU2659786C2/ru active
- 2013-05-14 IN IN9221DEN2014 patent/IN2014DN09221A/en unknown
-
2014
- 2014-10-19 IL IL235133A patent/IL235133A/en active IP Right Grant
- 2014-11-18 ZA ZA2014/08452A patent/ZA201408452B/en unknown
-
2016
- 2016-10-13 JP JP2016201383A patent/JP6362652B2/ja active Active
-
2017
- 2017-05-04 US US15/587,270 patent/US10259806B2/en active Active
- 2017-11-28 AU AU2017268508A patent/AU2017268508C1/en active Active
-
2020
- 2020-12-17 US US17/124,606 patent/US11787792B2/en active Active
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