JP2020520910A5 - - Google Patents
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- Publication number
- JP2020520910A5 JP2020520910A5 JP2019563379A JP2019563379A JP2020520910A5 JP 2020520910 A5 JP2020520910 A5 JP 2020520910A5 JP 2019563379 A JP2019563379 A JP 2019563379A JP 2019563379 A JP2019563379 A JP 2019563379A JP 2020520910 A5 JP2020520910 A5 JP 2020520910A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- naphthylidine
- pharmaceutical composition
- ethoxy
- ethyl
- 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.)
- Withdrawn
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims description 86
- -1 4- (2- (3,3-difluoro-3-phosphonopropoxy) ethoxy) -2-methylphenethyl Chemical group 0.000 claims description 52
- 239000002245 particle Substances 0.000 claims description 42
- 125000005605 benzo group Chemical group 0.000 claims description 40
- 108091006082 receptor inhibitors Proteins 0.000 claims description 38
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 36
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 claims description 35
- 229910052782 aluminium Inorganic materials 0.000 claims description 35
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims description 34
- ABLZXFCXXLZCGV-UHFFFAOYSA-N Phosphorous acid Chemical compound OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims description 28
- 235000019260 propionic acid Nutrition 0.000 claims description 28
- 239000000725 suspension Substances 0.000 claims description 28
- 229940000425 combination drug Drugs 0.000 claims description 24
- 150000001875 compounds Chemical class 0.000 claims description 23
- DUWWHGPELOTTOE-UHFFFAOYSA-N n-(5-chloro-2,4-dimethoxyphenyl)-3-oxobutanamide Chemical compound COC1=CC(OC)=C(NC(=O)CC(C)=O)C=C1Cl DUWWHGPELOTTOE-UHFFFAOYSA-N 0.000 claims description 23
- 150000003839 salts Chemical class 0.000 claims description 22
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 claims description 21
- 239000003112 inhibitor Substances 0.000 claims description 19
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 17
- 229930195725 Mannitol Natural products 0.000 claims description 17
- 239000000594 mannitol Substances 0.000 claims description 17
- 235000010355 mannitol Nutrition 0.000 claims description 17
- 239000007983 Tris buffer Substances 0.000 claims description 16
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical group OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 claims description 16
- 229940045513 CTLA4 antagonist Drugs 0.000 claims description 14
- 229940076838 Immune checkpoint inhibitor Drugs 0.000 claims description 14
- 206010028980 Neoplasm Diseases 0.000 claims description 14
- 239000012274 immune-checkpoint protein inhibitor Substances 0.000 claims description 14
- 239000003814 drug Substances 0.000 claims description 13
- 125000001153 fluoro group Chemical group F* 0.000 claims description 12
- 108010021064 CTLA-4 Antigen Proteins 0.000 claims description 11
- 102000008203 CTLA-4 Antigen Human genes 0.000 claims description 11
- 239000012271 PD-L1 inhibitor Substances 0.000 claims description 10
- 102100040678 Programmed cell death protein 1 Human genes 0.000 claims description 10
- 101710089372 Programmed cell death protein 1 Proteins 0.000 claims description 10
- 229940121656 pd-l1 inhibitor Drugs 0.000 claims description 10
- 102100029822 B- and T-lymphocyte attenuator Human genes 0.000 claims description 9
- 101000864344 Homo sapiens B- and T-lymphocyte attenuator Proteins 0.000 claims description 9
- 102000002698 KIR Receptors Human genes 0.000 claims description 9
- 108010043610 KIR Receptors Proteins 0.000 claims description 9
- 102000017578 LAG3 Human genes 0.000 claims description 9
- 101150030213 Lag3 gene Proteins 0.000 claims description 9
- 239000012272 PD-L2 inhibitor Substances 0.000 claims description 9
- 229940121654 pd-l2 inhibitor Drugs 0.000 claims description 9
- 102100034458 Hepatitis A virus cellular receptor 2 Human genes 0.000 claims description 8
- 101710083479 Hepatitis A virus cellular receptor 2 homolog Proteins 0.000 claims description 8
- 229940126547 T-cell immunoglobulin mucin-3 Drugs 0.000 claims description 8
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 8
- 239000000203 mixture Substances 0.000 claims description 8
- 239000003795 chemical substances by application Substances 0.000 claims description 7
- 239000000872 buffer Substances 0.000 claims description 5
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 5
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 claims description 5
- 201000001441 melanoma Diseases 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- UEZVMMHDMIWARA-UHFFFAOYSA-M phosphonate Chemical compound [O-]P(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-M 0.000 claims description 4
- 230000009278 visceral effect Effects 0.000 claims description 4
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 2
- 229930006000 Sucrose Natural products 0.000 claims description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-M dihydrogenphosphate Chemical compound OP(O)([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-M 0.000 claims description 2
- GATNOFPXSDHULC-UHFFFAOYSA-N ethylphosphonic acid Chemical compound CCP(O)(O)=O GATNOFPXSDHULC-UHFFFAOYSA-N 0.000 claims description 2
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims description 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 239000005720 sucrose Substances 0.000 claims description 2
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims description 2
- 229920002554 vinyl polymer Polymers 0.000 claims description 2
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims 2
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims 2
- 108010074708 B7-H1 Antigen Proteins 0.000 claims 1
- 102100024216 Programmed cell death 1 ligand 1 Human genes 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 description 12
- 125000004450 alkenylene group Chemical group 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- 201000009030 Carcinoma Diseases 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 125000004957 naphthylene group Chemical group 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- WCZVZNOTHYJIEI-UHFFFAOYSA-N cinnoline Chemical compound N1=NC=CC2=CC=CC=C21 WCZVZNOTHYJIEI-UHFFFAOYSA-N 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 description 2
- 238000001802 infusion Methods 0.000 description 2
- 230000010412 perfusion Effects 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 0 Cc1cc(C)c(CCc2cnc3C(N)=Ic(cc(*I)cc4)c4-c3c2)cc1 Chemical compound Cc1cc(C)c(CCc2cnc3C(N)=Ic(cc(*I)cc4)c4-c3c2)cc1 0.000 description 1
- 239000012270 PD-1 inhibitor Substances 0.000 description 1
- 239000012668 PD-1-inhibitor Substances 0.000 description 1
- 229940044665 STING agonist Drugs 0.000 description 1
- 229940124614 TLR 8 agonist Drugs 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 229940047712 aluminum hydroxyphosphate Drugs 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- 229940127089 cytotoxic agent Drugs 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 239000007928 intraperitoneal injection Substances 0.000 description 1
- 230000002601 intratumoral effect Effects 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 229940121655 pd-1 inhibitor Drugs 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 229940044616 toll-like receptor 7 agonist Drugs 0.000 description 1
- 229940044655 toll-like receptor 9 agonist Drugs 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023060740A JP2023093524A (ja) | 2017-05-19 | 2023-04-04 | 固形腫瘍の治療において使用するための、ナフチリジン誘導体及びアルミニウムアジュバントを含む組成物 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762508474P | 2017-05-19 | 2017-05-19 | |
| US62/508,474 | 2017-05-19 | ||
| PCT/IB2018/053481 WO2018211453A1 (en) | 2017-05-19 | 2018-05-17 | Compositions comprising naphthyridine derivatives and aluminium adjuvant for use in treating solid tumors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023060740A Division JP2023093524A (ja) | 2017-05-19 | 2023-04-04 | 固形腫瘍の治療において使用するための、ナフチリジン誘導体及びアルミニウムアジュバントを含む組成物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020520910A JP2020520910A (ja) | 2020-07-16 |
| JP2020520910A5 true JP2020520910A5 (enExample) | 2021-07-26 |
Family
ID=62597814
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019563379A Withdrawn JP2020520910A (ja) | 2017-05-19 | 2018-05-17 | 固形腫瘍の治療において使用するための、ナフチリジン誘導体及びアルミニウムアジュバントを含む組成物 |
| JP2023060740A Pending JP2023093524A (ja) | 2017-05-19 | 2023-04-04 | 固形腫瘍の治療において使用するための、ナフチリジン誘導体及びアルミニウムアジュバントを含む組成物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023060740A Pending JP2023093524A (ja) | 2017-05-19 | 2023-04-04 | 固形腫瘍の治療において使用するための、ナフチリジン誘導体及びアルミニウムアジュバントを含む組成物 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US11752162B2 (enExample) |
| EP (1) | EP3624806A1 (enExample) |
| JP (2) | JP2020520910A (enExample) |
| KR (1) | KR20200007040A (enExample) |
| CN (2) | CN110636848A (enExample) |
| AR (1) | AR111760A1 (enExample) |
| AU (2) | AU2018268420B2 (enExample) |
| BR (1) | BR112019024260A2 (enExample) |
| CA (1) | CA3062609A1 (enExample) |
| CL (1) | CL2019003293A1 (enExample) |
| MX (2) | MX2019013720A (enExample) |
| TW (1) | TW201900166A (enExample) |
| WO (1) | WO2018211453A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3029902A1 (en) | 2016-07-07 | 2018-01-11 | The Board Of Trustees Of The Leland Stanford Junior University | Antibody adjuvant conjugates |
| US11364304B2 (en) | 2016-08-25 | 2022-06-21 | Northwestern University | Crosslinked micellar spherical nucleic acids |
| AR111760A1 (es) * | 2017-05-19 | 2019-08-14 | Novartis Ag | Compuestos y composiciones para el tratamiento de tumores sólidos mediante administración intratumoral |
| JP2022525594A (ja) | 2019-03-15 | 2022-05-18 | ボルト バイオセラピューティクス、インコーポレーテッド | Ｈｅｒ２を標的とする免疫結合体 |
| WO2022009157A1 (en) | 2020-07-10 | 2022-01-13 | Novartis Ag | Lhc165 and spartalizumab combinations for treating solid tumors |
Family Cites Families (46)
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| IL73534A (en) | 1983-11-18 | 1990-12-23 | Riker Laboratories Inc | 1h-imidazo(4,5-c)quinoline-4-amines,their preparation and pharmaceutical compositions containing certain such compounds |
| CZ288182B6 (en) | 1993-07-15 | 2001-05-16 | Minnesota Mining & Mfg | Imidazo[4,5-c]pyridine-4-amines and pharmaceutical preparations based thereon |
| UA67760C2 (uk) | 1997-12-11 | 2004-07-15 | Міннесота Майнінг Енд Мануфакчурінг Компані | Імідазонафтиридин та тетрагідроімідазонафтиридин, фармацевтична композиція, спосіб індукування біосинтезу цитокінів та спосіб лікування вірусної інфекції, проміжні сполуки |
| US6110929A (en) | 1998-07-28 | 2000-08-29 | 3M Innovative Properties Company | Oxazolo, thiazolo and selenazolo [4,5-c]-quinolin-4-amines and analogs thereof |
| IL129299A0 (en) | 1999-03-31 | 2000-02-17 | Mor Research Applic Ltd | Monoclonal antibodies antigens and diagnosis of malignant diseases |
| IL149820A0 (en) | 2002-05-23 | 2002-11-10 | Curetech Ltd | Humanized immunomodulatory monoclonal antibodies for the treatment of neoplastic disease or immunodeficiency |
| WO2004056875A1 (en) | 2002-12-23 | 2004-07-08 | Wyeth | Antibodies against pd-1 and uses therefor |
| US20040265351A1 (en) | 2003-04-10 | 2004-12-30 | Miller Richard L. | Methods and compositions for enhancing immune response |
| GB0321710D0 (en) | 2003-09-16 | 2003-10-15 | Novartis Ag | Organic compounds |
| EP1696912B1 (en) | 2003-10-03 | 2016-05-11 | 3M Innovative Properties Company | Pyrazolopyridines and analogs thereof |
| DK2161336T4 (en) | 2005-05-09 | 2017-04-24 | Ono Pharmaceutical Co | Human monoclonal antibodies for programmed death 1 (PD-1) and methods for treating cancer using anti-PD-1 antibodies alone or in combination with other immunotherapies |
| NZ582150A (en) | 2007-06-18 | 2012-08-31 | Msd Oss Bv | Antibodies to human programmed death receptor pd-1 |
| KR101208778B1 (ko) | 2008-03-03 | 2012-12-05 | 노파르티스 아게 | Ｔｌｒ 활성 조정제로서의 화합물 및 조성물 |
| WO2009114335A2 (en) | 2008-03-12 | 2009-09-17 | Merck & Co., Inc. | Pd-1 binding proteins |
| CN102203125A (zh) | 2008-08-25 | 2011-09-28 | 安普利穆尼股份有限公司 | Pd-1拮抗剂及其使用方法 |
| EP2342229A1 (en) | 2008-09-12 | 2011-07-13 | ISIS Innovation Limited | Pd-1 specific antibodies and uses thereof |
| MX2011003195A (es) | 2008-09-26 | 2011-08-12 | Dana Farber Cancer Inst Inc | Anticuerpos anti-pd-1, pd-l1 y pd-l2 humanos y usos de los mismos. |
| TR201802380T4 (tr) | 2009-06-10 | 2018-03-21 | Glaxosmithkline Biologicals Sa | Benzonaftiridin içeren aşılar. |
| JO3257B1 (ar) | 2009-09-02 | 2018-09-16 | Novartis Ag | مركبات وتركيبات كمعدلات لفاعلية tlr |
| NZ598654A (en) | 2009-09-02 | 2014-05-30 | Novartis Ag | Immunogenic compositions including tlr activity modulators |
| JP2013512251A (ja) | 2009-11-24 | 2013-04-11 | アンプリミューン、インコーポレーテッド | Ｐｄ−ｌ１／ｐｄ−ｌ２の同時阻害 |
| EP2545078A1 (en) | 2010-03-11 | 2013-01-16 | UCB Pharma, S.A. | Pd-1 antibody |
| JP6023696B2 (ja) * | 2010-03-31 | 2016-11-09 | スタビリテック リミテッド | ミョウバンアジュバントおよびミョウバンアジュバント化ワクチンの保存方法 |
| US9597326B2 (en) | 2010-04-13 | 2017-03-21 | Glaxosmithkline Biologicals Sa | Benzonapthyridine compositions and uses thereof |
| US8907053B2 (en) | 2010-06-25 | 2014-12-09 | Aurigene Discovery Technologies Limited | Immunosuppression modulating compounds |
| CN105999275A (zh) | 2010-09-01 | 2016-10-12 | 诺华有限公司 | 免疫增强剂吸附不溶性金属离子 |
| CA2833636A1 (en) | 2011-04-20 | 2012-10-26 | Amplimmune, Inc. | Antibodies and other molecules that bind b7-h1 and pd-1 |
| EP2532359A1 (en) | 2011-06-10 | 2012-12-12 | Affiris AG | CETP fragments |
| EP2734551B1 (en) | 2011-07-24 | 2018-01-10 | Cure Tech Ltd. | Variants of humanized immunomodulatory monoclonal antibodies |
| KR20140066212A (ko) * | 2011-09-01 | 2014-05-30 | 노파르티스 아게 | 스타필로코쿠스 아우레우스 항원의 보조제 첨가된 조제물 |
| US9827190B2 (en) | 2013-02-01 | 2017-11-28 | Glaxosmithkline Biologicals Sa | Intradermal delivery of immunological compositions comprising toll-like receptor 7 agonists |
| HRP20210122T1 (hr) | 2013-05-02 | 2021-04-16 | Anaptysbio, Inc. | Protutijela usmjerena protiv programirane smrti-1 (pd-1) |
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| TWI681969B (zh) | 2014-01-23 | 2020-01-11 | 美商再生元醫藥公司 | 針對ｐｄ-１的人類抗體 |
| JOP20200094A1 (ar) | 2014-01-24 | 2017-06-16 | Dana Farber Cancer Inst Inc | جزيئات جسم مضاد لـ pd-1 واستخداماتها |
| BE1022875B1 (fr) | 2014-03-26 | 2016-09-30 | Glaxosmithkline Biologicals S.A. | Compositions pour une immunisation contre staphylococcus aureus |
| TWI693232B (zh) | 2014-06-26 | 2020-05-11 | 美商宏觀基因股份有限公司 | 與pd-1和lag-3具有免疫反應性的共價結合的雙抗體和其使用方法 |
| WO2016019232A1 (en) | 2014-08-01 | 2016-02-04 | John Vasilakos | Methods and therapeutic combinations for treating tumors |
| CN105296433B (zh) | 2014-08-01 | 2018-02-09 | 中山康方生物医药有限公司 | 一种ctla4抗体、其药物组合物及其用途 |
| EP3206711B1 (en) | 2014-10-14 | 2023-05-31 | Novartis AG | Antibody molecules to pd-l1 and uses thereof |
| TWI595006B (zh) | 2014-12-09 | 2017-08-11 | 禮納特神經系統科學公司 | 抗ｐｄ－１抗體類和使用彼等之方法 |
| JP7378931B2 (ja) * | 2015-11-03 | 2023-11-14 | エイシー イミューン ソシエテ アノニム | ヒト患者における自己抗原に対するワクチン接種法 |
| AR111760A1 (es) * | 2017-05-19 | 2019-08-14 | Novartis Ag | Compuestos y composiciones para el tratamiento de tumores sólidos mediante administración intratumoral |
-
2018
- 2018-05-15 AR ARP180101267A patent/AR111760A1/es not_active Application Discontinuation
- 2018-05-17 MX MX2019013720A patent/MX2019013720A/es unknown
- 2018-05-17 EP EP18730857.2A patent/EP3624806A1/en active Pending
- 2018-05-17 CA CA3062609A patent/CA3062609A1/en active Pending
- 2018-05-17 CN CN201880032524.5A patent/CN110636848A/zh active Pending
- 2018-05-17 WO PCT/IB2018/053481 patent/WO2018211453A1/en not_active Ceased
- 2018-05-17 AU AU2018268420A patent/AU2018268420B2/en not_active Ceased
- 2018-05-17 US US16/614,280 patent/US11752162B2/en active Active
- 2018-05-17 BR BR112019024260A patent/BR112019024260A2/pt not_active IP Right Cessation
- 2018-05-17 KR KR1020197037113A patent/KR20200007040A/ko not_active Ceased
- 2018-05-17 JP JP2019563379A patent/JP2020520910A/ja not_active Withdrawn
- 2018-05-17 CN CN202310419489.5A patent/CN116473981A/zh active Pending
- 2018-05-17 TW TW107116758A patent/TW201900166A/zh unknown
-
2019
- 2019-11-15 MX MX2023004381A patent/MX2023004381A/es unknown
- 2019-11-15 CL CL2019003293A patent/CL2019003293A1/es unknown
-
2021
- 2021-06-01 AU AU2021203564A patent/AU2021203564B2/en not_active Ceased
-
2023
- 2023-04-04 JP JP2023060740A patent/JP2023093524A/ja active Pending
- 2023-07-28 US US18/360,909 patent/US20240009215A1/en not_active Abandoned
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