CR8264A - Derivados de malonamida bloqueadores de la actividad gamma-secretase - Google Patents

Derivados de malonamida bloqueadores de la actividad gamma-secretase

Info

Publication number
CR8264A
CR8264A CR8264A CR8264A CR8264A CR 8264 A CR8264 A CR 8264A CR 8264 A CR8264 A CR 8264A CR 8264 A CR8264 A CR 8264A CR 8264 A CR8264 A CR 8264A
Authority
CR
Costa Rica
Prior art keywords
lower alkyl
blockers
gamma
halogen
secretase activity
Prior art date
Application number
CR8264A
Other languages
English (en)
Inventor
Flohr Alexander
Galley Guido
Jacob-Roetne Roland
A Kitas Eric
Peters Jens-Uwe
Wostl Wolfang
Original Assignee
Hoffmann La Roche
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of CR8264A publication Critical patent/CR8264A/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16Benzazepines; Hydrogenated benzazepines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/557Eicosanoids, e.g. leukotrienes or prostaglandins
    • A61K31/558Eicosanoids, e.g. leukotrienes or prostaglandins having heterocyclic rings containing oxygen as the only ring hetero atom, e.g. thromboxanes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/18Dibenzazepines; Hydrogenated dibenzazepines
    • C07D223/20Dibenz [b, e] azepines; Hydrogenated dibenz [b, e] azepines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/161,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/181,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D273/00Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D313/00Heterocyclic compounds containing rings of more than six members having one oxygen atom as the only ring hetero atom
    • C07D313/02Seven-membered rings
    • C07D313/06Seven-membered rings condensed with carbocyclic rings or ring systems
    • C07D313/10Seven-membered rings condensed with carbocyclic rings or ring systems condensed with two six-membered rings
    • C07D313/14[b,f]-condensed

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

La invencion se refire a derivados de malonamida de la formula I en la que R1 es uno de los grupos siguientes a), b), c), d) R2 es alquilo inferior, alquinilo inferior, -(CH2) n- O -alquilo inferior, -(CH2) n-S-alquilo inferior, -(CH2) n -CN, -(CR'R") n -CF3, -(CR'R") n -CHF2, -(CR'R") n-CH2F,-(CH2)n-C (O) O-alquilo inferior, (CH2) n- halogeno, o es - (CH2) n- cicloalquilo, opcionalmente sustituido por uno o varios sustituyentes elegidos entre el grupo formado por fenilo, halogeno y CF3; R',R" con independencia de n y con independencia entre si son hidrogeno, alquilo inferior, alcoxi inferior, halogeno o hidroxi; R3, R4 con independencia entre si son hidrogeno, alquilo inferior, alcoxi inferior, fenilo o halogeno; R5 es hidrogeno, alquilo inferior, -(CH2) n -CF3 o - (CH2) n- cicloalquilo.
CR8264A 2003-09-09 2006-03-01 Derivados de malonamida bloqueadores de la actividad gamma-secretase CR8264A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP03019683 2003-09-09

Publications (1)

Publication Number Publication Date
CR8264A true CR8264A (es) 2008-09-22

Family

ID=34224068

Family Applications (1)

Application Number Title Priority Date Filing Date
CR8264A CR8264A (es) 2003-09-09 2006-03-01 Derivados de malonamida bloqueadores de la actividad gamma-secretase

Country Status (34)

Country Link
US (1) US7160875B2 (es)
EP (1) EP1711470B1 (es)
JP (2) JP4571639B2 (es)
KR (3) KR20070087233A (es)
CN (1) CN100593539C (es)
AR (1) AR045609A1 (es)
AT (1) ATE428698T1 (es)
AU (1) AU2004270361B2 (es)
BR (1) BRPI0413533A (es)
CA (1) CA2537440C (es)
CO (1) CO5660268A2 (es)
CR (1) CR8264A (es)
CY (1) CY1109225T1 (es)
DE (1) DE602004020680D1 (es)
DK (1) DK1711470T3 (es)
EA (1) EA009940B1 (es)
EC (1) ECSP066414A (es)
ES (1) ES2322652T3 (es)
HR (1) HRP20090266T1 (es)
IL (1) IL173905A (es)
MA (1) MA28034A1 (es)
MX (1) MXPA06002562A (es)
MY (1) MY141308A (es)
NO (1) NO20061047L (es)
NZ (1) NZ545538A (es)
PL (1) PL1711470T3 (es)
PT (1) PT1711470E (es)
RS (1) RS20060146A (es)
SI (1) SI1711470T1 (es)
TN (1) TNSN06077A1 (es)
TW (1) TW200519092A (es)
UA (1) UA83501C2 (es)
WO (1) WO2005023772A1 (es)
ZA (1) ZA200601989B (es)

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ATE402934T1 (de) * 2003-02-04 2008-08-15 Hoffmann La Roche Malonamidderivate als gamma-secretaseinhibitoren
AU2004270361B2 (en) * 2003-09-09 2009-06-25 F. Hoffmann-La Roche Ag Malonamide derivatives blocking the activity of gama-secretase
PT1673347E (pt) * 2003-10-06 2015-11-02 Hoffmann La Roche Derivados de dibenzo-azepina e benzo-diazepina substituídos, úteis como inibidores de secretase gama
US7211573B2 (en) 2004-12-08 2007-05-01 Hoffmann-La Roche Inc. Malonamide derivatives
KR101169628B1 (ko) * 2006-03-27 2012-07-30 에프. 호프만-라 로슈 아게 감마 세크레테아제 저해제로서의 말론아미드 유도체
CN101516859B (zh) * 2006-09-20 2012-07-04 霍夫曼-拉罗奇有限公司 4-氧代-2,3,4,5-四氢-苯并[b][1,4]二氮杂*衍生物
AU2008209861B2 (en) * 2007-02-02 2012-08-09 F. Hoffmann-La Roche Ag 6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl derivatives
DE602008006368D1 (de) * 2007-03-15 2011-06-01 Hoffmann La Roche Malonamide als orexin-antagonisten
US7579464B2 (en) 2007-05-25 2009-08-25 Hoffmann-La Roche Inc. Process for preparation of enantiomerically pure compounds
US8741889B2 (en) 2008-01-11 2014-06-03 Hoffmann-La Roche Inc Method of treating non-small cell lung cancer and colon cancer with gamma-secretase inhibitor
MA33076B1 (fr) * 2008-01-11 2012-03-01 Hoffmann La Roche Utilisation d'un inhibiteur de la gamma-secretase pour le traitement du cancer
US8309299B2 (en) * 2010-05-19 2012-11-13 Hoffmann-La Roche Inc. Combination therapy and method for assessing resistance to treatment
WO2012040444A2 (en) * 2010-09-24 2012-03-29 Bristol-Myers Squibb Company Treatment of patients with incipient alzheimer's disease
WO2012050370A2 (ko) * 2010-10-15 2012-04-19 성균관대학교산학협력단 감마-세크레타제 저해제를 유효성분으로 함유하는 류마티스성 관절염의 예방 또는 치료용 조성물
KR101330184B1 (ko) 2010-10-15 2013-11-15 성균관대학교산학협력단 감마-세크레타제 저해제를 유효성분으로 함유하는 류마티스성 관절염의 예방 또는 치료용 조성물
US20120114638A1 (en) 2010-11-08 2012-05-10 John Boylan Combination therapy
US20120184529A1 (en) 2011-01-14 2012-07-19 Demario Mark D Combination therapy
US20120225860A1 (en) 2011-03-02 2012-09-06 John Frederick Boylan Method for administration of a gamma secretase inhibitor
TWI530489B (zh) 2011-03-22 2016-04-21 必治妥美雅史谷比公司 雙(氟烷基)-1,4-苯二氮呯酮化合物
AR087107A1 (es) 2011-07-27 2014-02-12 Lilly Co Eli Compuesto inhibidor de la señalizacion de la trayectoria notch
CN104968648A (zh) 2012-09-21 2015-10-07 百时美施贵宝公司 1,4-苯并二氮杂*酮化合物的前药
CN105308030A (zh) 2012-09-21 2016-02-03 百时美施贵宝公司 烷基、氟烷基-1,4-苯并二氮杂*酮化合物
US9242940B2 (en) 2012-09-21 2016-01-26 Bristol-Myers Squibb Company N-substituted bis(fluoroalkyl)-1,4-benzodiazepinone compounds
TWI614238B (zh) 2012-09-21 2018-02-11 必治妥美雅史谷比公司 雙(氟烷基)-1,4-苯并二氮呯酮化合物及其前藥
JP2015529250A (ja) 2012-09-21 2015-10-05 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company フルオロアルキルジベンゾジアゼピノン化合物
CN104822677A (zh) 2012-09-21 2015-08-05 百时美施贵宝公司 氟烷基-1,4-苯并二氮杂*酮化合物
EP2897944B1 (en) 2012-09-21 2016-10-26 Bristol-Myers Squibb Company Substituted 1,5-benzodiazepinone compounds
WO2014047390A1 (en) 2012-09-21 2014-03-27 Bristol-Myers Squibb Company Tricyclic heterocyclic compounds as notch inhibitors
WO2014047397A1 (en) 2012-09-21 2014-03-27 Bristol-Myers Squibb Company Fluoroalkyl and fluorocycloalkyl 1,4-benzodiazepinone compounds as notch|inhibitors
JP2016515625A (ja) 2013-04-04 2016-05-30 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 増殖性疾患を治療するための併用療法
EP2932966A1 (en) 2014-04-16 2015-10-21 Novartis AG Gamma secretase inhibitors for treating respiratory diseases
AU2016344138B2 (en) * 2015-10-30 2019-06-06 Pipeline Therapeutics, Inc. Dibenzo azepine compounds and their use in the treatment of otic diseases and disorders
CN110337291A (zh) * 2016-12-16 2019-10-15 帕珀莱恩医疗公司 治疗耳蜗突触病变的方法
US20200179511A1 (en) 2017-04-28 2020-06-11 Novartis Ag Bcma-targeting agent, and combination therapy with a gamma secretase inhibitor
US20200055948A1 (en) 2017-04-28 2020-02-20 Novartis Ag Cells expressing a bcma-targeting chimeric antigen receptor, and combination therapy with a gamma secretase inhibitor
EP3668844A1 (en) * 2017-08-15 2020-06-24 Bayer Aktiengesellschaft 4-oxo-2,3,4,5-tetrahydro-1h-1,5-benzodiazepine-7-carboxamides
AU2019277029C1 (en) 2018-06-01 2024-01-04 Novartis Ag Binding molecules against BCMA and uses thereof
CN114286828A (zh) 2019-06-24 2022-04-05 诺华股份有限公司 针对靶向b细胞成熟抗原的多特异性抗体的给药方案和组合疗法
CN116234898A (zh) * 2020-07-23 2023-06-06 普渡研究基金会 用于治疗肥胖症和代谢紊乱的Notch信号传导抑制剂
KR20240054320A (ko) * 2021-08-31 2024-04-25 바스프 에스이 축합된 고리계를 함유하는 제초성 말론아미드
CN119095890A (zh) 2022-11-04 2024-12-06 株式会社Lg化学 全息图记录介质和包括其的光学元件
CN116621721B (zh) * 2023-04-12 2025-03-18 珠海市柏瑞医药科技有限公司 一种壬二酰胺的制备方法

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AU2004270361B2 (en) * 2003-09-09 2009-06-25 F. Hoffmann-La Roche Ag Malonamide derivatives blocking the activity of gama-secretase

Also Published As

Publication number Publication date
ATE428698T1 (de) 2009-05-15
DK1711470T3 (da) 2009-06-08
EP1711470B1 (en) 2009-04-15
KR20060054455A (ko) 2006-05-22
PT1711470E (pt) 2009-05-21
MXPA06002562A (es) 2006-06-20
UA83501C2 (uk) 2008-07-25
HK1099014A1 (zh) 2007-08-03
AR045609A1 (es) 2005-11-02
BRPI0413533A (pt) 2006-10-10
SI1711470T1 (sl) 2009-08-31
US20050054633A1 (en) 2005-03-10
CO5660268A2 (es) 2006-07-31
EP1711470A1 (en) 2006-10-18
HRP20090266T1 (en) 2009-06-30
JP2010229153A (ja) 2010-10-14
MA28034A1 (fr) 2006-07-03
DE602004020680D1 (de) 2009-05-28
AU2004270361A1 (en) 2005-03-17
TNSN06077A1 (fr) 2007-10-03
CA2537440A1 (en) 2005-03-17
RS20060146A (sr) 2008-06-05
CN100593539C (zh) 2010-03-10
KR20070087233A (ko) 2007-08-27
KR100838852B1 (ko) 2008-06-16
IL173905A (en) 2011-05-31
CY1109225T1 (el) 2014-07-02
NZ545538A (en) 2008-12-24
CN1875005A (zh) 2006-12-06
AU2004270361B2 (en) 2009-06-25
JP4571639B2 (ja) 2010-10-27
KR20070087690A (ko) 2007-08-28
MY141308A (en) 2010-04-16
CA2537440C (en) 2012-07-10
TW200519092A (en) 2005-06-16
EA009940B1 (ru) 2008-04-28
IL173905A0 (en) 2006-07-05
JP2007505063A (ja) 2007-03-08
WO2005023772A1 (en) 2005-03-17
KR100834177B1 (ko) 2008-05-30
US7160875B2 (en) 2007-01-09
PL1711470T3 (pl) 2009-09-30
NO20061047L (no) 2006-04-04
ES2322652T3 (es) 2009-06-24
ZA200601989B (en) 2007-05-30
ECSP066414A (es) 2006-09-18
EA200600503A1 (ru) 2006-08-25

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