JP2002516865A5 - - Google Patents
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- Publication number
- JP2002516865A5 JP2002516865A5 JP2000551779A JP2000551779A JP2002516865A5 JP 2002516865 A5 JP2002516865 A5 JP 2002516865A5 JP 2000551779 A JP2000551779 A JP 2000551779A JP 2000551779 A JP2000551779 A JP 2000551779A JP 2002516865 A5 JP2002516865 A5 JP 2002516865A5
- Authority
- JP
- Japan
- Prior art keywords
- carbons
- group
- alkyl
- compound
- substituted
- 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
- 125000000217 alkyl group Chemical group 0.000 description 28
- 125000003118 aryl group Chemical group 0.000 description 13
- 229910052739 hydrogen Inorganic materials 0.000 description 13
- 125000001072 heteroaryl group Chemical group 0.000 description 10
- 125000003342 alkenyl group Chemical group 0.000 description 9
- 125000003545 alkoxy group Chemical group 0.000 description 9
- 125000000304 alkynyl group Chemical group 0.000 description 9
- 238000000034 method Methods 0.000 description 8
- 239000008194 pharmaceutical composition Substances 0.000 description 8
- 150000001875 compounds Chemical class 0.000 description 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 6
- 229910052794 bromium Inorganic materials 0.000 description 6
- 229910052731 fluorine Inorganic materials 0.000 description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 6
- 150000002772 monosaccharides Chemical group 0.000 description 6
- 229910052760 oxygen Inorganic materials 0.000 description 6
- 239000000825 pharmaceutical preparation Substances 0.000 description 6
- 125000003710 aryl alkyl group Chemical group 0.000 description 5
- 229910052801 chlorine Inorganic materials 0.000 description 5
- 239000003937 drug carrier Substances 0.000 description 5
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 5
- 229910052740 iodine Inorganic materials 0.000 description 5
- 229910052717 sulfur Inorganic materials 0.000 description 5
- 206010028980 Neoplasm Diseases 0.000 description 4
- 230000002491 angiogenic effect Effects 0.000 description 4
- 201000010099 disease Diseases 0.000 description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 229910052757 nitrogen Inorganic materials 0.000 description 4
- 230000002265 prevention Effects 0.000 description 4
- 230000002159 abnormal effect Effects 0.000 description 3
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 description 3
- 125000002102 aryl alkyloxo group Chemical group 0.000 description 3
- 229910052799 carbon Inorganic materials 0.000 description 3
- 125000004432 carbon atom Chemical group C* 0.000 description 3
- -1 heterocycloalkoxy Chemical group 0.000 description 3
- 125000005113 hydroxyalkoxy group Chemical group 0.000 description 3
- 125000005647 linker group Chemical group 0.000 description 3
- 125000004433 nitrogen atom Chemical group N* 0.000 description 3
- 208000017497 prostate disease Diseases 0.000 description 3
- 125000001054 5 membered carbocyclic group Chemical group 0.000 description 2
- 208000030507 AIDS Diseases 0.000 description 2
- 201000001320 Atherosclerosis Diseases 0.000 description 2
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 description 2
- 208000005623 Carcinogenesis Diseases 0.000 description 2
- 206010012289 Dementia Diseases 0.000 description 2
- 206010012689 Diabetic retinopathy Diseases 0.000 description 2
- 201000009273 Endometriosis Diseases 0.000 description 2
- 208000023105 Huntington disease Diseases 0.000 description 2
- 208000018737 Parkinson disease Diseases 0.000 description 2
- 206010060862 Prostate cancer Diseases 0.000 description 2
- 208000004403 Prostatic Hyperplasia Diseases 0.000 description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 2
- 201000004681 Psoriasis Diseases 0.000 description 2
- 208000006011 Stroke Diseases 0.000 description 2
- 150000001413 amino acids Chemical class 0.000 description 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 description 2
- 210000004556 brain Anatomy 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 230000036952 cancer formation Effects 0.000 description 2
- 150000001721 carbon Chemical group 0.000 description 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 2
- 231100000504 carcinogenesis Toxicity 0.000 description 2
- 230000006806 disease prevention Effects 0.000 description 2
- 206010015037 epilepsy Diseases 0.000 description 2
- 208000030533 eye disease Diseases 0.000 description 2
- 201000002222 hemangioblastoma Diseases 0.000 description 2
- 208000028867 ischemia Diseases 0.000 description 2
- 208000002780 macular degeneration Diseases 0.000 description 2
- 201000006417 multiple sclerosis Diseases 0.000 description 2
- 206010028537 myelofibrosis Diseases 0.000 description 2
- 239000001301 oxygen Substances 0.000 description 2
- 208000033808 peripheral neuropathy Diseases 0.000 description 2
- 208000005069 pulmonary fibrosis Diseases 0.000 description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 description 2
- 230000029663 wound healing Effects 0.000 description 2
- 208000024827 Alzheimer disease Diseases 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 description 1
- 108091000080 Phosphotransferase Proteins 0.000 description 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 208000029028 brain injury Diseases 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229910052736 halogen Inorganic materials 0.000 description 1
- 150000002367 halogens Chemical class 0.000 description 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 210000002307 prostate Anatomy 0.000 description 1
- 208000037803 restenosis Diseases 0.000 description 1
- 210000000278 spinal cord Anatomy 0.000 description 1
- 208000020431 spinal cord injury Diseases 0.000 description 1
- 125000000547 substituted alkyl group Chemical group 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 125000004434 sulfur atom Chemical group 0.000 description 1
- 230000001228 trophic effect Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8811498P | 1998-06-05 | 1998-06-05 | |
| US60/088,114 | 1998-06-05 | ||
| US09/325,140 US6127401A (en) | 1998-06-05 | 1999-06-03 | Bridged indenopyrrolocarbazoles |
| US09/325,140 | 1999-06-03 | ||
| PCT/US1999/012531 WO1999062523A1 (en) | 1998-06-05 | 1999-06-04 | Bridged indenopyrrolocarbazoles |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2002516865A JP2002516865A (ja) | 2002-06-11 |
| JP2002516865A5 true JP2002516865A5 (enExample) | 2006-08-03 |
| JP4481493B2 JP4481493B2 (ja) | 2010-06-16 |
Family
ID=26778288
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000551779A Expired - Fee Related JP4481493B2 (ja) | 1998-06-05 | 1999-06-04 | 架橋インデノピロロカルバゾール |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US6127401A (enExample) |
| EP (1) | EP1083903B1 (enExample) |
| JP (1) | JP4481493B2 (enExample) |
| KR (1) | KR100647753B1 (enExample) |
| CN (1) | CN1304311A (enExample) |
| AT (1) | ATE274348T1 (enExample) |
| AU (1) | AU744900B2 (enExample) |
| BG (1) | BG65447B1 (enExample) |
| BR (1) | BR9910908A (enExample) |
| CA (1) | CA2334189C (enExample) |
| CZ (1) | CZ301754B6 (enExample) |
| DE (1) | DE69919700T2 (enExample) |
| DK (1) | DK1083903T3 (enExample) |
| EA (1) | EA004066B1 (enExample) |
| ES (1) | ES2228056T3 (enExample) |
| HU (1) | HUP0102512A3 (enExample) |
| NO (1) | NO20006166L (enExample) |
| NZ (1) | NZ508306A (enExample) |
| PL (1) | PL198434B1 (enExample) |
| PT (1) | PT1083903E (enExample) |
| SK (1) | SK285368B6 (enExample) |
| TR (1) | TR200003623T2 (enExample) |
| UA (1) | UA66865C2 (enExample) |
| WO (1) | WO1999062523A1 (enExample) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6811992B1 (en) * | 1998-05-14 | 2004-11-02 | Ya Fang Liu | Method for identifying MLK inhibitors for the treatment of neurological conditions |
| US6127401A (en) * | 1998-06-05 | 2000-10-03 | Cephalon, Inc. | Bridged indenopyrrolocarbazoles |
| EP1126855B1 (en) | 1998-09-25 | 2007-05-09 | Cephalon, Inc. | Use of fused pyrrolocarbazoles for preventing/treating damage to sensory hair cells and cochlear neurons |
| US6841567B1 (en) | 1999-02-12 | 2005-01-11 | Cephalon, Inc. | Cyclic substituted fused pyrrolocarbazoles and isoindolones |
| US6630500B2 (en) | 2000-08-25 | 2003-10-07 | Cephalon, Inc. | Selected fused pyrrolocarbazoles |
| US20020169154A1 (en) * | 2001-04-04 | 2002-11-14 | Cephalon, Inc. | Novel methods and compositions involving trk tyrosine kinase inhibitors and antineoplastic agents |
| US7018999B2 (en) | 2001-05-16 | 2006-03-28 | Cephalon, Inc. | Methods for the treatment and prevention of pain |
| CA2398828A1 (en) * | 2002-08-09 | 2004-02-09 | Merck & Co., Inc. | A pharmaceutical composition containing an indolopyrrolocarbazole derivative |
| AU2003259846A1 (en) * | 2002-08-16 | 2004-03-03 | The General Hospital Corporation | Non-invasive functional imaging of peripheral nervous system activation in humans and animals |
| CA2500901A1 (en) * | 2002-10-04 | 2004-04-22 | Rinat Neuroscience Corp. | Methods for treating cardiac arrhythmia and preventing death due to cardiac arrhythmia using ngf antagonists |
| ZA200502612B (en) | 2002-10-08 | 2007-07-25 | Rinat Neuroscience Corp | Methods for treating post-surgical pain by administering a nerve crowth factor antagonist and compositions containing the same |
| UA80447C2 (en) | 2002-10-08 | 2007-09-25 | Methods for treating pain by administering nerve growth factor antagonist and opioid analgesic | |
| WO2005000194A2 (en) * | 2002-10-08 | 2005-01-06 | Rinat Neuroscience Corp. | Methods for treating post-surgical pain by administering an anti-nerve growth factor antagonist antibody and compositions containing the same |
| US9498530B2 (en) | 2002-12-24 | 2016-11-22 | Rinat Neuroscience Corp. | Methods for treating osteoarthritis pain by administering a nerve growth factor antagonist and compositions containing the same |
| DK2270048T3 (en) | 2002-12-24 | 2016-01-18 | Rinat Neuroscience Corp | Anti-NGF antibodies and methods for their use |
| US7569364B2 (en) | 2002-12-24 | 2009-08-04 | Pfizer Inc. | Anti-NGF antibodies and methods using same |
| BRPI0407375A (pt) * | 2003-02-19 | 2006-02-07 | Rinat Neuroscience Corp | Métodos para tratar dor por meio da administração de um antagonista do fator de crescimento neural e u nsaid e composições contendo os mesmos |
| US7241779B2 (en) * | 2003-12-23 | 2007-07-10 | Cephalon, Inc. | Fused pyrrolocarbazoles |
| EP3372614B1 (en) | 2004-04-07 | 2022-06-08 | Rinat Neuroscience Corp. | Methods for treating bone cancer pain by administering a nerve growth factor antagonist |
| US7419972B2 (en) * | 2004-07-02 | 2008-09-02 | Schering Ag | 2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of 17β-hydroxy steroid dehydrogenase type 1 |
| US20060058250A1 (en) * | 2004-09-10 | 2006-03-16 | Cephalon, Inc. | Methods of treating proliferative skin diseases using carbazole derivatives |
| US20080021013A1 (en) * | 2006-07-21 | 2008-01-24 | Cephalon, Inc. | JAK inhibitors for treatment of myeloproliferative disorders |
| EP1952813A1 (en) * | 2007-02-01 | 2008-08-06 | Ferring International Center S.A. | Medicament for the treatment of endometriosis |
| SA08290041B1 (ar) * | 2007-02-01 | 2012-06-05 | فيرينج انترناشونال سنتر اس آيه | أدوية من أجل معالجة بطانة الرحم |
| KR101160225B1 (ko) | 2007-02-01 | 2012-07-11 | 페링 인터내셔널 센터 에스 에이 | 자궁 내막증 치료용 약제 |
| EP4514998A1 (en) | 2022-04-27 | 2025-03-05 | Regeneron Pharmaceuticals, Inc. | Treatment of arthropathy based upon stratification of osteoarthritis polygenic risk score |
| EP4680973A1 (en) | 2023-03-17 | 2026-01-21 | Regeneron Pharmaceuticals, Inc. | Proteomic risk score for osteoarthritis (oa) |
| WO2026054762A1 (en) | 2024-09-05 | 2026-03-12 | Regeneron Pharmaceuticals, Inc. | Proteomic risk score for adjudicated arthropathy (aa) |
Family Cites Families (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS62220196A (ja) * | 1986-03-20 | 1987-09-28 | Kyowa Hakko Kogyo Co Ltd | 新規物質ｕｃｎ―０１ |
| US4816450A (en) * | 1986-09-15 | 1989-03-28 | Duke University | Inhibition of protein kinase C by long-chain bases |
| US4735939A (en) * | 1987-02-27 | 1988-04-05 | The Dow Chemical Company | Insecticidal activity of staurosporine |
| US4923986A (en) * | 1987-03-09 | 1990-05-08 | Kyowa Hakko Kogyo Co., Ltd. | Derivatives of physiologically active substance K-252 |
| JPH07113027B2 (ja) * | 1987-12-24 | 1995-12-06 | 協和醗酵工業株式会社 | Ｋ−２５２誘導体 |
| FR2631199B1 (fr) * | 1988-05-09 | 1991-03-15 | Centre Nat Rech Scient | Reacteur a plasma |
| US5668271A (en) * | 1991-11-29 | 1997-09-16 | Banyu Pharmaceutical Co., Ltd. | Indolopyrrolocarbazole derivatives |
| US5591842A (en) * | 1991-11-29 | 1997-01-07 | Banyu Pharmaceutical Co., Ltd. | Indolopyrrolocarbazole derivatives |
| US5437996A (en) * | 1992-11-24 | 1995-08-01 | Banyu Pharmaceutical Co., Ltd. | Microtetraspora strain for preparation of indolopyrrolocarbazole derivatives |
| US5589365A (en) * | 1991-11-29 | 1996-12-31 | Banyu Pharmaceutical Co., Ltd. | Process for producing glycosylated indolopyrrolocarbazole derivatives by culturing certain microorganisms |
| US5344926A (en) * | 1992-06-22 | 1994-09-06 | Kyowa Hakko Kogyo Co., Ltd. | Process for producing staurosporine derivatives |
| US5756494A (en) * | 1992-07-24 | 1998-05-26 | Cephalon, Inc. | Protein kinase inhibitors for treatment of neurological disorders |
| US5621100A (en) * | 1992-07-24 | 1997-04-15 | Cephalon, Inc. | K-252a derivatives for treatment of neurological disorders |
| US5461146A (en) * | 1992-07-24 | 1995-10-24 | Cephalon, Inc. | Selected protein kinase inhibitors for the treatment of neurological disorders |
| US5621101A (en) * | 1992-07-24 | 1997-04-15 | Cephalon, Inc. | Protein kinase inhibitors for treatment of neurological disorders |
| CA2123895A1 (en) * | 1992-09-21 | 1994-03-31 | Tatsuya Tamaoki | A therapeutic agent for thrombocytopenia |
| WO1994007895A1 (en) * | 1992-09-25 | 1994-04-14 | Schering Corporation | Diindolo compounds and pharmaceutical compositions containing them |
| US5721230A (en) * | 1993-05-10 | 1998-02-24 | Hoffmann-La Roche Inc. | Substituted pyrroles |
| AU679752B2 (en) * | 1993-05-28 | 1997-07-10 | Cephalon, Inc. | Use of indolocarbazole derivatives to treat a pathological condition of the prostate |
| US5468872A (en) * | 1993-09-16 | 1995-11-21 | Cephalon, Inc. | K-252a functional derivatives potentiate neurotrophin-3 for the treatment of neurological disorders |
| JPH07112987A (ja) * | 1993-10-14 | 1995-05-02 | Asahi Chem Ind Co Ltd | スタウロスポリン糖部分変換誘導体 |
| PT657458E (pt) * | 1993-12-07 | 2002-02-28 | Lilly Co Eli | Inibidores de proteina cinase c |
| US5624949A (en) * | 1993-12-07 | 1997-04-29 | Eli Lilly And Company | Protein kinase C inhibitors |
| US5723456A (en) * | 1993-12-07 | 1998-03-03 | Eli Lilly & Company | Therapeutic treatment for cardiovascular diseases |
| CA2179650C (en) * | 1993-12-23 | 2007-10-30 | William Francis Heath, Jr. | Bisindolemaleimides and their use as protein kinase c inhibitors |
| US5545636A (en) * | 1993-12-23 | 1996-08-13 | Eli Lilly And Company | Protein kinase C inhibitors |
| WO1995032975A1 (en) * | 1994-06-01 | 1995-12-07 | Ciba-Geigy Ag | Indolocarbazole derivatives for sensitizing multidrug-resistant cells to antitumor agents |
| US5475110A (en) * | 1994-10-14 | 1995-12-12 | Cephalon, Inc. | Fused Pyrrolocarbazoles |
| US5594009A (en) * | 1994-10-14 | 1997-01-14 | Cephalon, Inc. | Fused pyrrolocarbazoles |
| US5591855A (en) * | 1994-10-14 | 1997-01-07 | Cephalon, Inc. | Fused pyrrolocarbazoles |
| US5705511A (en) * | 1994-10-14 | 1998-01-06 | Cephalon, Inc. | Fused pyrrolocarbazoles |
| EP0768311B1 (en) * | 1995-03-09 | 2003-08-06 | Kyowa Hakko Kogyo Co., Ltd. | Pyrrolocarbazole derivatives |
| WO1997007081A2 (en) * | 1995-08-11 | 1997-02-27 | Yale University | Glycosylated indolocarbazole synthesis |
| PL184728B1 (pl) * | 1995-11-20 | 2002-12-31 | Lilly Co Eli | Nowe pochodne bisindolilomaleimidu z mostkiem N,N'i środek farmaceutyczny |
| SI0776895T1 (en) * | 1995-11-20 | 1999-04-30 | Eli Lilly And Company | Protein kinase C inhibitor |
| US5808060A (en) * | 1995-12-11 | 1998-09-15 | Cephalon, Inc. | Fused isoindolones |
| US5616724A (en) * | 1996-02-21 | 1997-04-01 | Cephalon, Inc. | Fused pyrrolo[2,3-c]carbazole-6-ones |
| EA001450B1 (ru) * | 1996-05-01 | 2001-04-23 | Эли Лилли Энд Компани | Галогензамещенные ингибиторы протеинкиназы с |
| DK0912184T3 (da) * | 1996-06-25 | 2002-11-25 | Cephalon Inc | Anvendelse af K-252a-derivat til behandlingen af perifere eller centrale nervelidelser og cytokinoverproduktion |
| NZ333536A (en) * | 1996-08-22 | 1999-10-28 | Bristol Myers Squibb Co | Cytotoxic amino sugar and related sugar derivatives of indolopyrrolocarbazoles, and use as antitumour agents |
| US5721272A (en) * | 1996-11-18 | 1998-02-24 | Eli Lilly And Company | Intermediates and their use to prepare N,N'-bridged bisindolylmaleimides |
| US6127401A (en) * | 1998-06-05 | 2000-10-03 | Cephalon, Inc. | Bridged indenopyrrolocarbazoles |
-
1999
- 1999-06-03 US US09/325,140 patent/US6127401A/en not_active Expired - Lifetime
- 1999-06-04 ES ES99927234T patent/ES2228056T3/es not_active Expired - Lifetime
- 1999-06-04 CN CN99807036A patent/CN1304311A/zh active Pending
- 1999-06-04 HU HU0102512A patent/HUP0102512A3/hu unknown
- 1999-06-04 DK DK99927234T patent/DK1083903T3/da active
- 1999-06-04 EA EA200100012A patent/EA004066B1/ru not_active IP Right Cessation
- 1999-06-04 KR KR1020007013686A patent/KR100647753B1/ko not_active Expired - Fee Related
- 1999-06-04 JP JP2000551779A patent/JP4481493B2/ja not_active Expired - Fee Related
- 1999-06-04 AT AT99927234T patent/ATE274348T1/de active
- 1999-06-04 BR BR9910908-5A patent/BR9910908A/pt not_active Application Discontinuation
- 1999-06-04 PL PL344475A patent/PL198434B1/pl not_active IP Right Cessation
- 1999-06-04 WO PCT/US1999/012531 patent/WO1999062523A1/en not_active Ceased
- 1999-06-04 TR TR2000/03623T patent/TR200003623T2/xx unknown
- 1999-06-04 NZ NZ508306A patent/NZ508306A/en unknown
- 1999-06-04 DE DE69919700T patent/DE69919700T2/de not_active Expired - Lifetime
- 1999-06-04 CA CA002334189A patent/CA2334189C/en not_active Expired - Fee Related
- 1999-06-04 EP EP99927234A patent/EP1083903B1/en not_active Expired - Lifetime
- 1999-06-04 UA UA2001010125A patent/UA66865C2/uk unknown
- 1999-06-04 PT PT99927234T patent/PT1083903E/pt unknown
- 1999-06-04 SK SK1799-2000A patent/SK285368B6/sk not_active IP Right Cessation
- 1999-06-04 AU AU44188/99A patent/AU744900B2/en not_active Ceased
- 1999-06-04 CZ CZ20004522A patent/CZ301754B6/cs not_active IP Right Cessation
-
2000
- 2000-05-17 US US09/572,160 patent/US6359130B1/en not_active Expired - Fee Related
- 2000-12-04 NO NO20006166A patent/NO20006166L/no not_active Application Discontinuation
- 2000-12-07 BG BG105028A patent/BG65447B1/bg unknown
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