JP2002523508A5 - - Google Patents
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- JP2002523508A5 JP2002523508A5 JP2000567532A JP2000567532A JP2002523508A5 JP 2002523508 A5 JP2002523508 A5 JP 2002523508A5 JP 2000567532 A JP2000567532 A JP 2000567532A JP 2000567532 A JP2000567532 A JP 2000567532A JP 2002523508 A5 JP2002523508 A5 JP 2002523508A5
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- JP
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- Prior art keywords
- compound
- hydrogen
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- formula
- compound according
- Prior art date
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- Pending
Links
- 150000001875 compounds Chemical class 0.000 description 29
- 229910052739 hydrogen Inorganic materials 0.000 description 12
- 239000001257 hydrogen Substances 0.000 description 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 10
- 125000000217 alkyl group Chemical group 0.000 description 6
- 201000010099 disease Diseases 0.000 description 5
- 229910052736 halogen Inorganic materials 0.000 description 5
- 150000002367 halogens Chemical class 0.000 description 5
- -1 arylsulfoxyl Chemical group 0.000 description 4
- 239000000203 mixture Substances 0.000 description 4
- 210000003169 Central Nervous System Anatomy 0.000 description 3
- 125000003545 alkoxy group Chemical group 0.000 description 3
- 125000004414 alkyl thio group Chemical group 0.000 description 3
- 201000008779 central nervous system disease Diseases 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 208000008787 Cardiovascular Disease Diseases 0.000 description 2
- 208000008665 Gastrointestinal Disease Diseases 0.000 description 2
- 208000008589 Obesity Diseases 0.000 description 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 description 2
- 125000003118 aryl group Chemical group 0.000 description 2
- 125000004104 aryloxy group Chemical group 0.000 description 2
- 230000003542 behavioural Effects 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 125000000623 heterocyclic group Chemical group 0.000 description 2
- 150000002431 hydrogen Chemical class 0.000 description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 2
- 230000002458 infectious Effects 0.000 description 2
- 235000020824 obesity Nutrition 0.000 description 2
- 239000000546 pharmaceutic aid Substances 0.000 description 2
- 230000002588 toxic Effects 0.000 description 2
- 231100000331 toxic Toxicity 0.000 description 2
- AYNAVHUTXWVDLR-UHFFFAOYSA-N 1-(6,7-difluoro-2,3-dihydro-1H-pyrrolo[1,2-a]indol-4-yl)propan-2-amine Chemical compound C12=CC(F)=C(F)C=C2C(CC(N)C)=C2N1CCC2 AYNAVHUTXWVDLR-UHFFFAOYSA-N 0.000 description 1
- VCCGTYYMZYICBO-UHFFFAOYSA-N 1-(6-bromo-2,3-dihydro-1H-pyrrolo[1,2-a]indol-4-yl)propan-2-amine Chemical compound C12=CC=C(Br)C=C2C(CC(N)C)=C2N1CCC2 VCCGTYYMZYICBO-UHFFFAOYSA-N 0.000 description 1
- XNFYXIJQNZVXAX-UHFFFAOYSA-N 1-(6-chloro-2,3-dihydro-1H-pyrrolo[1,2-a]indol-4-yl)propan-2-amine Chemical compound C12=CC=C(Cl)C=C2C(CC(N)C)=C2N1CCC2 XNFYXIJQNZVXAX-UHFFFAOYSA-N 0.000 description 1
- SPMDNODKUUODIS-UHFFFAOYSA-N 1-(6-methylsulfanyl-2,3-dihydro-1H-pyrrolo[1,2-a]indol-4-yl)propan-2-amine Chemical compound CSC1=CC=C2N(CCC3)C3=C(CC(C)N)C2=C1 SPMDNODKUUODIS-UHFFFAOYSA-N 0.000 description 1
- 102100017238 AVP Human genes 0.000 description 1
- 101700084127 AVP Proteins 0.000 description 1
- 208000007848 Alcoholism Diseases 0.000 description 1
- 208000000103 Anorexia Nervosa Diseases 0.000 description 1
- 206010057666 Anxiety disease Diseases 0.000 description 1
- 206010004938 Bipolar disease Diseases 0.000 description 1
- 206010006550 Bulimia nervosa Diseases 0.000 description 1
- 206010008874 Chronic fatigue syndrome Diseases 0.000 description 1
- 206010057668 Cognitive disease Diseases 0.000 description 1
- 206010012289 Dementia Diseases 0.000 description 1
- 206010013663 Drug dependence Diseases 0.000 description 1
- 206010014599 Encephalitis Diseases 0.000 description 1
- 206010015037 Epilepsy Diseases 0.000 description 1
- 206010019233 Headache Diseases 0.000 description 1
- 206010022114 Injury Diseases 0.000 description 1
- JJWLVOIRVHMVIS-UHFFFAOYSA-N Isopropylamine Chemical compound CC(C)N JJWLVOIRVHMVIS-UHFFFAOYSA-N 0.000 description 1
- 206010027175 Memory impairment Diseases 0.000 description 1
- 206010061284 Mental disease Diseases 0.000 description 1
- 206010027599 Migraine Diseases 0.000 description 1
- 208000008085 Migraine Disorders Diseases 0.000 description 1
- 206010053643 Neurodegenerative disease Diseases 0.000 description 1
- 208000002193 Pain Diseases 0.000 description 1
- 206010034721 Personality disease Diseases 0.000 description 1
- 206010061920 Psychotic disease Diseases 0.000 description 1
- 208000000927 Sleep Apnea Syndrome Diseases 0.000 description 1
- 206010040979 Sleep apnoea syndrome Diseases 0.000 description 1
- 206010040984 Sleep disease Diseases 0.000 description 1
- 206010041250 Social phobia Diseases 0.000 description 1
- 208000006011 Stroke Diseases 0.000 description 1
- 208000007536 Thrombosis Diseases 0.000 description 1
- 230000016571 aggressive behavior Effects 0.000 description 1
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 description 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 description 1
- 125000003710 aryl alkyl group Chemical group 0.000 description 1
- 125000005129 aryl carbonyl group Chemical group 0.000 description 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 description 1
- 125000005110 aryl thio group Chemical group 0.000 description 1
- 201000003084 atypical depressive disease Diseases 0.000 description 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 1
- 125000002837 carbocyclic group Chemical group 0.000 description 1
- 125000004093 cyano group Chemical group *C#N 0.000 description 1
- 201000010064 diabetes insipidus Diseases 0.000 description 1
- 125000004663 dialkyl amino group Chemical group 0.000 description 1
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 description 1
- 125000005202 dialkylaminocarbonyloxy group Chemical group 0.000 description 1
- 229940079593 drugs Drugs 0.000 description 1
- 230000004064 dysfunction Effects 0.000 description 1
- 230000005176 gastrointestinal motility Effects 0.000 description 1
- 201000002146 gastrointestinal system disease Diseases 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 125000005842 heteroatoms Chemical group 0.000 description 1
- 201000009941 intracranial hypertension Diseases 0.000 description 1
- 201000009906 meningitis Diseases 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 1
- 201000008430 obsessive-compulsive disease Diseases 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 229940002612 prodrugs Drugs 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 201000000980 schizophrenia Diseases 0.000 description 1
- 201000001880 sexual dysfunction Diseases 0.000 description 1
- 231100000872 sexual dysfunction Toxicity 0.000 description 1
- 201000002859 sleep apnea Diseases 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9819035.8 | 1998-09-01 | ||
| GBGB9819035.8A GB9819035D0 (en) | 1998-09-01 | 1998-09-01 | Chemical compounds VII |
| PCT/GB1999/002884 WO2000012510A1 (en) | 1998-09-01 | 1999-09-01 | Pyrroloindoles, pyridoindoles and azepinoindoles as 5-ht2c agonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2002523508A JP2002523508A (ja) | 2002-07-30 |
| JP2002523508A5 true JP2002523508A5 (pt-PT) | 2006-10-26 |
Family
ID=10838167
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000567532A Pending JP2002523508A (ja) | 1998-09-01 | 1999-09-01 | ５−ｈｔ２ｃアゴニストとしての、ピロロインドール、ピリドインドールおよびアゼピノインドール |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US6433175B1 (pt-PT) |
| EP (1) | EP1109813B1 (pt-PT) |
| JP (1) | JP2002523508A (pt-PT) |
| KR (2) | KR20070062609A (pt-PT) |
| CN (1) | CN1165537C (pt-PT) |
| AT (1) | ATE273308T1 (pt-PT) |
| AU (1) | AU758084B2 (pt-PT) |
| BR (1) | BR9913477A (pt-PT) |
| CA (1) | CA2341991C (pt-PT) |
| CZ (1) | CZ296275B6 (pt-PT) |
| DE (1) | DE69919364T2 (pt-PT) |
| DK (1) | DK1109813T3 (pt-PT) |
| ES (1) | ES2226430T3 (pt-PT) |
| GB (1) | GB9819035D0 (pt-PT) |
| HK (1) | HK1034967A1 (pt-PT) |
| HR (1) | HRP20010126B1 (pt-PT) |
| HU (1) | HUP0103333A3 (pt-PT) |
| ID (1) | ID28842A (pt-PT) |
| IL (2) | IL141659A0 (pt-PT) |
| MX (1) | MXPA01002101A (pt-PT) |
| NO (1) | NO321527B1 (pt-PT) |
| NZ (1) | NZ510097A (pt-PT) |
| PL (1) | PL346427A1 (pt-PT) |
| PT (1) | PT1109813E (pt-PT) |
| RU (1) | RU2232162C2 (pt-PT) |
| SI (1) | SI1109813T1 (pt-PT) |
| TR (2) | TR200501110T2 (pt-PT) |
| WO (1) | WO2000012510A1 (pt-PT) |
| YU (1) | YU16001A (pt-PT) |
| ZA (1) | ZA200101457B (pt-PT) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6960579B1 (en) | 1998-05-19 | 2005-11-01 | Alcon Manufacturing, Ltd. | Serotonergic 5HT7 receptor compounds for treating ocular and CNS disorders |
| GB9902047D0 (en) * | 1999-01-29 | 1999-03-17 | Cerebrus Ltd | Chemical compounds XI |
| US6465467B1 (en) | 1999-05-21 | 2002-10-15 | Biovitrum Ab | Certain aryl-aliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases |
| GB9918965D0 (en) * | 1999-08-11 | 1999-10-13 | Cerebrus Ltd | Chemical compounds xxi |
| US6818639B2 (en) | 2000-07-21 | 2004-11-16 | Biovitrum Ab | Pharmaceutical combination formulation and method of treatment with the combination |
| SE0002754D0 (sv) * | 2000-07-21 | 2000-07-21 | Pharmacia & Upjohn Ab | New pharmaceutical combination formulation and method of treatment with the combination |
| SE0004245D0 (sv) | 2000-11-20 | 2000-11-20 | Pharmacia Ab | Novel compounds and their use |
| AU1529402A (en) | 2000-11-20 | 2002-05-27 | Biovitrum Ab | Piperazinylpyrazines compounds as antagonists of serotonin 5-ht2 receptor |
| HUP0303316A2 (hu) | 2000-12-20 | 2004-01-28 | Bristol-Myers Squibb Pharma Company | Aril- és amino-aril-szubsztituált szerotoninreceptor agonista és antagonista ligandumok és ezeket tartalmazó gyógyszerkészítmények |
| WO2002051844A1 (en) | 2000-12-27 | 2002-07-04 | F. Hoffmann-La Roche Ag | Indole derivatives and their use as 5-ht2b and 5-ht2c receptor ligands |
| JP2004532887A (ja) | 2001-06-01 | 2004-10-28 | アルコン，インコーポレイテッド | 新規な融合インダゾールおよびインドールおよび緑内障治療へのこれらの使用 |
| EP1392269A1 (en) | 2001-06-01 | 2004-03-03 | Alcon, Inc. | Novel arylaminopropane analogues and their use for the treatment of glaucoma |
| DK1392292T3 (da) | 2001-06-01 | 2006-05-29 | Alcon Inc | Pyranoindazoler og deres anvendelse til behandling af glaukom |
| TW593302B (en) | 2001-12-20 | 2004-06-21 | Alcon Inc | Novel benzodifuranimidazoline and benzofuranimidazoline derivatives and their use for the treatment of glaucoma |
| BR0311970A (pt) | 2002-06-19 | 2005-03-29 | Biovitrum Ab | Novos compostos, seu uso e preparação |
| PL375564A1 (en) * | 2002-08-30 | 2005-11-28 | Alcon, Inc. | Substituted 5-chroman-5-yl-ethylamine compounds and their use for the treatment of glaucoma |
| JP2006511556A (ja) | 2002-12-13 | 2006-04-06 | アルコン，インコーポレイテッド | 新規のベンゾピラン類似体及び緑内障の治療のためのそれらの使用 |
| CL2004000826A1 (es) | 2003-04-25 | 2005-03-04 | Pfizer | Uso de un agonista para el receptor 5-ht2c para preparar un medicamento util en el tratamiento de la incontinencia urinaria provocada por estres, con la condicion de que el agonista no sea 1-[6-cloro-5-(trifluorometil)-2-piridinil]piperazina (org-129 |
| GB0314967D0 (en) | 2003-06-26 | 2003-07-30 | Hoffmann La Roche | Piperazine derivatives |
| US7435837B2 (en) * | 2003-10-24 | 2008-10-14 | Wyeth | Dihydrobenzofuranyl alkanamine derivatives and methods for using same |
| WO2005053688A1 (en) | 2003-11-26 | 2005-06-16 | Alcon, Inc. | Substituted furo[2,3-g] indazoles for the treatment of glaucoma |
| US7129257B1 (en) | 2003-12-15 | 2006-10-31 | Alcon, Inc. | Pyrazolo[3,4- e]benzoxazoles for the treatment of glaucoma |
| US7338972B1 (en) | 2003-12-15 | 2008-03-04 | Alcon, Inc. | Substituted 1-alkylamino-1H-indazoles for the treatment of glaucoma |
| WO2005058911A2 (en) | 2003-12-15 | 2005-06-30 | Alcon, Inc. | Substituted [1,4]oxazino[2,3-g]indazoles for the treatment of glaucoma |
| EP2400300A1 (en) | 2004-08-25 | 2011-12-28 | Takeda Pharmaceutical Company Limited | Method of screening preventives/remedies for stress urinary incontinence |
| AU2005302559A1 (en) | 2004-11-01 | 2006-05-11 | Wyeth | Substituted indolizines and derivatives as CNS agents |
| US7425572B2 (en) | 2004-12-08 | 2008-09-16 | Alcon, Inc. | Use of dioxindoindazoles and dioxoloindazoles for treating glaucoma |
| AU2006228378A1 (en) | 2005-03-31 | 2006-10-05 | Pfizer Products Inc. | Cyclopentapyridine and tetrahydroquinoline derivatives |
| US20060252825A1 (en) * | 2005-04-22 | 2006-11-09 | Wyeth | Crystal forms of {[(2r)-7-(2,6-dichlorophenyl)-5-fluoro-2,3-dihydro-1-benzofuran-2-yl]methyl}amine hydrochloride |
| ATE514698T1 (de) * | 2005-05-03 | 2011-07-15 | Hoffmann La Roche | Tetracyclische azapyrazinoindoline als 5-ht2- liganden |
| EP2018863B9 (en) | 2006-05-16 | 2015-02-18 | Takeda Pharmaceutical Company Limited | Fused heterocyclic compound and use thereof |
| CA2657640A1 (en) * | 2006-07-14 | 2008-01-24 | Pfizer Products Inc. | Tartrate salt of (7s)-7-[(5-fluoro-2-methyl-benzyl)oxy]-2-[(2r)-2-methylpiperazin-1-yl]-6,7-dihydro-5h-cyclopenta[b]pyridine |
| EP2216023A4 (en) | 2007-11-15 | 2013-03-13 | Takeda Pharmaceutical | CONDENSED PYRIDINE DERIVATIVE AND USE THEREOF |
| KR101062376B1 (ko) | 2008-04-10 | 2011-09-06 | 한국화학연구원 | 신규 인돌 카르복실산 비스피리딜 카르복사마이드 유도체,이의 제조방법 및 이를 유효성분으로 함유하는 조성물 |
| WO2011071136A1 (ja) | 2009-12-11 | 2011-06-16 | アステラス製薬株式会社 | 線維筋痛症治療剤 |
| WO2012030953A1 (en) | 2010-09-01 | 2012-03-08 | Arena Pharmaceuticals, Inc. | 5-ht2c receptor agonists in the treatment of disorders ameliorated by reduction of norepinephrine level |
| CN102964352B (zh) * | 2012-11-23 | 2015-04-08 | 华中师范大学 | 具有生物活性的手性2,3-二氢吡咯[1,2-a]吲哚衍生物及其不对称合成方法 |
| WO2015066344A1 (en) | 2013-11-01 | 2015-05-07 | Arena Pharmaceuticals, Inc. | 5-ht2c receptor agonists and compositions and methods of use |
| US20210052600A1 (en) | 2017-12-27 | 2021-02-25 | Takeda Pharmaceutical Company Limited | Therapeutic agents for stress urinary incontinence and incotinence of feces |
| WO2020072675A1 (en) | 2018-10-02 | 2020-04-09 | Northwestern University | Beta-carbolines as positive allosteric modulators of the human serotonin receptor 2c (5-ht2c) |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3250783A (en) | 1964-09-21 | 1966-05-10 | American Cyanamid Co | Novel pyrrolo (1, 2-alpha) indoles |
| US4134894A (en) * | 1978-05-04 | 1979-01-16 | Warner-Lambert Company | Pyrrolo[1,2-a]indole compounds |
| GB8416724D0 (en) * | 1984-06-30 | 1984-08-01 | Sorbio Sa Lab | Active compounds |
| US4778812A (en) * | 1987-06-12 | 1988-10-18 | American Home Products Corporation | 2,3-dihydro-9-methyl-1H-pyrrolo[1,2-a]indol-1-amines and derivatives thereof |
| GB8802127D0 (en) * | 1988-02-01 | 1988-03-02 | Glaxo Group Ltd | Chemical compounds |
| PT884319E (pt) * | 1992-03-12 | 2004-09-30 | Smithkline Beecham Plc | N-¬(1-n-butil-4-piperidil)metil|-3,4-di-hidro-2h-¬1,3|oxazino¬3,2-a|indole-10-carboxamida ou um seu sal farmaceuticamente aceitavel |
| EP0572863A1 (de) * | 1992-06-05 | 1993-12-08 | F. Hoffmann-La Roche Ag | ZNS Pyrazinoindole |
| WO1994020102A2 (en) * | 1993-03-08 | 1994-09-15 | Fujisawa Pharmaceutical Co., Ltd. | Medicament for treating or preventing cerebrovascular diseases |
| US5629427A (en) * | 1993-08-26 | 1997-05-13 | Peterson; Dwight M. | 2,7-diaminomitosene analogues |
-
1998
- 1998-09-01 GB GBGB9819035.8A patent/GB9819035D0/en not_active Ceased
-
1999
- 1999-09-01 JP JP2000567532A patent/JP2002523508A/ja active Pending
- 1999-09-01 KR KR1020077011961A patent/KR20070062609A/ko active IP Right Grant
- 1999-09-01 US US09/763,889 patent/US6433175B1/en not_active Expired - Fee Related
- 1999-09-01 AU AU56375/99A patent/AU758084B2/en not_active Ceased
- 1999-09-01 PL PL99346427A patent/PL346427A1/xx not_active IP Right Cessation
- 1999-09-01 NZ NZ510097A patent/NZ510097A/xx unknown
- 1999-09-01 DK DK99943091T patent/DK1109813T3/da active
- 1999-09-01 ES ES99943091T patent/ES2226430T3/es not_active Expired - Lifetime
- 1999-09-01 PT PT99943091T patent/PT1109813E/pt unknown
- 1999-09-01 IL IL14165999A patent/IL141659A0/xx active IP Right Grant
- 1999-09-01 KR KR1020017002608A patent/KR100768595B1/ko not_active IP Right Cessation
- 1999-09-01 ID IDW20010677A patent/ID28842A/id unknown
- 1999-09-01 EP EP99943091A patent/EP1109813B1/en not_active Expired - Lifetime
- 1999-09-01 SI SI9930677T patent/SI1109813T1/xx unknown
- 1999-09-01 TR TR2005/01110T patent/TR200501110T2/xx unknown
- 1999-09-01 AT AT99943091T patent/ATE273308T1/de not_active IP Right Cessation
- 1999-09-01 WO PCT/GB1999/002884 patent/WO2000012510A1/en not_active Application Discontinuation
- 1999-09-01 MX MXPA01002101A patent/MXPA01002101A/es not_active IP Right Cessation
- 1999-09-01 CA CA002341991A patent/CA2341991C/en not_active Expired - Fee Related
- 1999-09-01 CN CNB998128341A patent/CN1165537C/zh not_active Expired - Fee Related
- 1999-09-01 HU HU0103333A patent/HUP0103333A3/hu unknown
- 1999-09-01 BR BR9913477-2A patent/BR9913477A/pt not_active Application Discontinuation
- 1999-09-01 CZ CZ20010772A patent/CZ296275B6/cs not_active IP Right Cessation
- 1999-09-01 TR TR2001/00659T patent/TR200100659T2/xx unknown
- 1999-09-01 RU RU2001108570/04A patent/RU2232162C2/ru not_active IP Right Cessation
- 1999-09-01 DE DE69919364T patent/DE69919364T2/de not_active Expired - Fee Related
- 1999-09-01 YU YU16001A patent/YU16001A/sh unknown
-
2001
- 2001-02-21 ZA ZA200101457A patent/ZA200101457B/xx unknown
- 2001-02-21 HR HR20010126A patent/HRP20010126B1/xx not_active IP Right Cessation
- 2001-02-26 IL IL141659A patent/IL141659A/en not_active IP Right Cessation
- 2001-02-27 NO NO20010991A patent/NO321527B1/no not_active IP Right Cessation
- 2001-08-14 HK HK01105681A patent/HK1034967A1/xx not_active IP Right Cessation
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