PE20150371A1 - Indolcarbonitrilos como moduladores selectivos del receptor de androgeno - Google Patents
Indolcarbonitrilos como moduladores selectivos del receptor de androgenoInfo
- Publication number
- PE20150371A1 PE20150371A1 PE2015000039A PE2015000039A PE20150371A1 PE 20150371 A1 PE20150371 A1 PE 20150371A1 PE 2015000039 A PE2015000039 A PE 2015000039A PE 2015000039 A PE2015000039 A PE 2015000039A PE 20150371 A1 PE20150371 A1 PE 20150371A1
- Authority
- PE
- Peru
- Prior art keywords
- androgen receptor
- indolcarbonitriles
- selective modulators
- development
- modulators
- Prior art date
Links
- 102000001307 androgen receptors Human genes 0.000 title abstract 2
- 108010080146 androgen receptors Proteins 0.000 title abstract 2
- CBTITARLOCZPDU-UHFFFAOYSA-N 1h-indole-2-carbonitrile Chemical class C1=CC=C2NC(C#N)=CC2=C1 CBTITARLOCZPDU-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D209/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an alkyl or cycloalkyl radical attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/06—Anabolic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/26—Androgens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261672455P | 2012-07-17 | 2012-07-17 | |
| US201361748874P | 2013-01-04 | 2013-01-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20150371A1 true PE20150371A1 (es) | 2015-03-27 |
Family
ID=49117887
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2015000039A PE20150371A1 (es) | 2012-07-17 | 2013-07-15 | Indolcarbonitrilos como moduladores selectivos del receptor de androgeno |
Country Status (39)
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10155099B2 (en) | 2009-09-21 | 2018-12-18 | Cook Regentec Llc | Method for infusing stem cells |
| BR112015000940B1 (pt) | 2012-07-17 | 2022-05-17 | Glaxosmithkline Intellectual Property (No. 2) Limited | Composto, composição farmacêutica, e, uso de um composto |
| EP3097077A1 (en) * | 2014-01-21 | 2016-11-30 | Glaxosmithkline Intellectual Property (No. 2) Limited | Crystalline forms of (r)-1 -(1-(methylsulfonyl)propan-2-yl)-4-(trifluoromethyl)indoline-5-carbonitrile |
| CA2964371A1 (en) * | 2014-10-16 | 2016-04-21 | Gtx, Inc. | Methods of treating urological disorders using sarms |
| CN105130872B (zh) * | 2015-08-25 | 2018-01-30 | 江西师范大学 | 一种3位三氟甲基取代吲哚的制备方法 |
| CN110437125B (zh) * | 2019-09-06 | 2021-03-12 | 苏州旺山旺水生物医药有限公司 | 一种Tezacaftor中间体II的制备方法 |
| US20220306609A1 (en) * | 2021-03-23 | 2022-09-29 | Nido Biosciences, Inc. | Bicyclic compounds as androgen receptor modulators |
| CN115010574B (zh) * | 2022-06-06 | 2024-01-05 | 爱斯特(成都)生物制药股份有限公司 | 1-溴-2-氯-4-氟-2碘苯的合成方法 |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20010041343A (ko) | 1998-02-25 | 2001-05-15 | 브루스 엠. 에이센, 토마스 제이 데스로저 | 포스포리파제 효소의 억제제 |
| EA005852B1 (ru) * | 1998-06-19 | 2005-06-30 | Пфайзер Продактс Инк. | ПИРРОЛО[2,3-d]ПИРИМИДИНЫ |
| US6576265B1 (en) | 1999-12-22 | 2003-06-10 | Acell, Inc. | Tissue regenerative composition, method of making, and method of use thereof |
| BR0311266A (pt) | 2002-05-24 | 2005-02-22 | Bayer Cropscience Ag | Processo para a preparação de derivados de tioalquilamina |
| CN1960973A (zh) * | 2004-03-30 | 2007-05-09 | 惠氏公司 | 作为去甲肾上腺素(ne)与血清素(5-h t)活性和单胺重摄取的调控剂以治疗血管舒缩症状(vms)的1-(1h-吲哚-1-基)-3-(4-甲基哌嗪-1-基)-1-苯基丙烷-2-醇衍生物和相关化合物 |
| US7517899B2 (en) | 2004-03-30 | 2009-04-14 | Wyeth | Phenylaminopropanol derivatives and methods of their use |
| EP2078712B1 (en) | 2004-05-03 | 2015-06-10 | Janssen Pharmaceutica N.V. | Indole derivatives as selective androgen receptor modulators (sarms) |
| US7282507B2 (en) | 2004-05-03 | 2007-10-16 | Janssen Pharmaceutica N.V. | Indole derivatives as selective androgen receptor modulators (SARMS) |
| US7427682B2 (en) | 2004-05-03 | 2008-09-23 | Janssen Pharmaceutica N.V. | Indole derivatives as selective androgen receptor modulators (SARMS) |
| AU2005250116B2 (en) * | 2004-06-01 | 2011-01-20 | F. Hoffmann-La Roche Ag | 3-amino-1-arylpropyl indoles as monoamine reuptake inhibitor |
| ES2377771T3 (es) * | 2005-07-29 | 2012-03-30 | Pfizer Products Inc. | Derivados de pirrolo [2,3-d]pirimidina, sus intermedios y síntesis |
| GB0526246D0 (en) * | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
| CN101426778A (zh) * | 2006-03-15 | 2009-05-06 | 惠氏公司 | 作为组胺-3拮抗剂的n-经取代-氮杂环基胺 |
| MX2008011791A (es) * | 2006-03-15 | 2008-09-25 | Wyeth Corp | Azaciclilaminas-n-sustituidas como antagonistas de histamina-3. |
| WO2008042571A2 (en) * | 2006-09-29 | 2008-04-10 | Smithkline Beecham Corporation | Substituted indole compounds |
| KR101335843B1 (ko) * | 2008-08-20 | 2013-12-02 | 조에티스 엘엘씨 | 피롤로[2,3-d]피리미딘 화합물 |
| WO2010118287A1 (en) | 2009-04-10 | 2010-10-14 | Radius Health, Inc. | Selective androgen receptor modulators |
| CN102574860A (zh) * | 2009-10-15 | 2012-07-11 | 辉瑞大药厂 | 吡咯并[2,3-d]嘧啶化合物 |
| EP2513114B1 (en) * | 2009-12-18 | 2014-04-02 | Pfizer Inc. | Pyrrolo[2,3-d]pyrimidine compounds |
| EP2590647B1 (en) | 2010-07-07 | 2017-11-08 | Board of Regents of the University of Texas System | Pro-neurogenic compounds |
| MX351305B (es) * | 2011-01-20 | 2017-10-09 | Merck Sharp & Dohme | Antagonistas del receptor de mineralocorticoides. |
| SI2796460T1 (sl) * | 2011-12-21 | 2018-10-30 | Jiangsu Hengrui Medicine Co. Ltd | Pirolni šestčlenski derivat heteroarilnega obroča, postopek priprave zanj in medicinske uporabe le-tega |
| BR112015000940B1 (pt) * | 2012-07-17 | 2022-05-17 | Glaxosmithkline Intellectual Property (No. 2) Limited | Composto, composição farmacêutica, e, uso de um composto |
| EP3097077A1 (en) * | 2014-01-21 | 2016-11-30 | Glaxosmithkline Intellectual Property (No. 2) Limited | Crystalline forms of (r)-1 -(1-(methylsulfonyl)propan-2-yl)-4-(trifluoromethyl)indoline-5-carbonitrile |
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2013
- 2013-07-15 BR BR112015000940-9A patent/BR112015000940B1/pt active IP Right Grant
- 2013-07-15 IN IN2993KON2014 patent/IN2014KN02993A/en unknown
- 2013-07-15 JP JP2015522180A patent/JP6106746B2/ja active Active
- 2013-07-15 CA CA2879104A patent/CA2879104C/en active Active
- 2013-07-15 MX MX2015000825A patent/MX349943B/es active IP Right Grant
- 2013-07-15 WO PCT/IB2013/001530 patent/WO2014013309A1/en not_active Ceased
- 2013-07-15 MY MYPI2018001949A patent/MY198512A/en unknown
- 2013-07-15 MY MYPI2015000121A patent/MY173845A/en unknown
- 2013-07-15 TW TW102125297A patent/TWI574946B/zh active
- 2013-07-15 LT LTEP13758975.0T patent/LT2875013T/lt unknown
- 2013-07-15 DK DK13758975.0T patent/DK2875013T3/en active
- 2013-07-15 PE PE2015000039A patent/PE20150371A1/es active IP Right Grant
- 2013-07-15 KR KR1020157003959A patent/KR102127939B1/ko active Active
- 2013-07-15 JO JOP/2013/0214A patent/JO3384B1/ar active
- 2013-07-15 SG SG11201408493WA patent/SG11201408493WA/en unknown
- 2013-07-15 EA EA201492237A patent/EA026371B8/ru not_active IP Right Cessation
- 2013-07-15 CN CN201380048232.8A patent/CN104619693B/zh active Active
- 2013-07-15 ME MEP-2018-16A patent/ME02996B/me unknown
- 2013-07-15 ES ES13758975.0T patent/ES2657912T3/es active Active
- 2013-07-15 NZ NZ703129A patent/NZ703129A/en unknown
- 2013-07-15 PT PT137589750T patent/PT2875013T/pt unknown
- 2013-07-15 RS RS20180119A patent/RS56810B1/sr unknown
- 2013-07-15 SI SI201330945T patent/SI2875013T1/en unknown
- 2013-07-15 AU AU2013291721A patent/AU2013291721B2/en active Active
- 2013-07-15 SM SM20180115T patent/SMT201800115T1/it unknown
- 2013-07-15 UY UY0001034911A patent/UY34911A/es not_active Application Discontinuation
- 2013-07-15 EP EP13758975.0A patent/EP2875013B1/en active Active
- 2013-07-15 HR HRP20180061TT patent/HRP20180061T1/hr unknown
- 2013-07-15 HU HUE13758975A patent/HUE036238T2/hu unknown
- 2013-07-15 US US13/941,911 patent/US8957104B2/en active Active
- 2013-07-15 AR ARP130102513A patent/AR091770A1/es active IP Right Grant
- 2013-07-15 PL PL13758975T patent/PL2875013T3/pl unknown
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2014
- 2014-11-20 US US14/549,034 patent/US9533948B2/en active Active
- 2014-12-23 CO CO14282153A patent/CO7240378A2/es unknown
- 2014-12-25 IL IL236448A patent/IL236448A/en active IP Right Grant
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2015
- 2015-01-07 ZA ZA2015/00096A patent/ZA201500096B/en unknown
- 2015-01-08 DO DO2015000004A patent/DOP2015000004A/es unknown
- 2015-01-09 CR CR20150008A patent/CR20150008A/es unknown
- 2015-01-14 PH PH12015500104A patent/PH12015500104A1/en unknown
- 2015-01-16 CL CL2015000119A patent/CL2015000119A1/es unknown
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2016
- 2016-11-22 US US15/358,458 patent/US10196353B2/en active Active
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2018
- 2018-02-13 CY CY20181100173T patent/CY1120064T1/el unknown
- 2018-12-20 US US16/226,763 patent/US10710963B2/en active Active
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2020
- 2020-05-12 US US16/872,949 patent/US11299457B2/en active Active
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Legal Events
| Date | Code | Title | Description |
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| FG | Grant, registration |