JP6419294B2 - シグマ受容体に仲介される障害を処置するための環状アミド誘導体の使用の方法 - Google Patents
シグマ受容体に仲介される障害を処置するための環状アミド誘導体の使用の方法 Download PDFInfo
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- A—HUMAN NECESSITIES
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- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- C—CHEMISTRY; METALLURGY
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- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
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- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
- A01N43/40—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
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- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
-
- 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
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- Animal Behavior & Ethology (AREA)
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- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
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- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Child & Adolescent Psychology (AREA)
- Obesity (AREA)
- Anesthesiology (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Agronomy & Crop Science (AREA)
- Pest Control & Pesticides (AREA)
- Plant Pathology (AREA)
- Dentistry (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Environmental Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
[0009]
[0010] “調節する”には、この用語が本明細書で用いられる際、(例えば同種親和性および/またはヘテロ親和性の)タンパク質−タンパク質相互作用を安定化する、促進する、増大させる、阻害する、または混乱させることが含まれるが、それらに限定されない。本明細書で用いられる際、“調節する”は、非タンパク質分子および受容体分子の間の相互作用に影響を及ぼすことも指す。
用語“対症的処置”は、その病気を治療することなく対象における病気の作用または強さを和らげる、または低減する処置をさす。用語“予防性処置”(および対応する用語“予防的処置”)は、対象における病気の発生を防ぐ処置を指す。用語“回復性処置”(“治療的”)は、対象における病気の進行を止める、病気の病的徴候を低減する、または病気を完全に排除する処置を指す。処置は、組織、系または対象の生物学的または医薬的応答を引き出す療法上有効量の化合物、塩または組成物を用いて行うことができ、研究者、医師、獣医、または臨床家のような人がそれを求めている。
[0016] “BACS”は統合失調症認知機能簡易評価(Brief Assessment of Cognition in Schizophrenia)試験を意味する。
[0018] “HAMA”はハミルトン不安尺度(Hamilton Anxiety Scale)を意味する。
[0021] “PSQI”はピッツバーグ睡眠質指数(Pittsburgh Sleep Quality Index)を意味する。
[0024] 別の態様において、式Iの化合物は統合失調症の1種類以上の症状を処置するのに有用であることが示されている。一観点において、その症状は陰性症状である。別の観点において、その症状は陽性症状である。さらに別の観点において、その症状は一般症状である。一態様において、本発明は、下記でより完全に述べるように、統合失調症および統合失調症の症状を処置するための方法および組成物を提供する。
[0028]
[0031]
[0036]
[0038] 本発明に従う療法的投与に関して、式Iの化合物はその遊離塩基の形で用いることができるが、好ましくは医薬的に許容できる塩、典型的には塩酸塩の形で用いられる。
[0045] 一態様において、式Iの化合物またはその医薬的に許容できる塩は、あらゆる他の薬物療法から独立して投与される。別の態様において、式Iの化合物またはその医薬的に許容できる塩は、1種類以上の他の薬物療法と合わせて投与される。
統合失調症および統合失調症の症状の処置への有効性を調べるため、式IIの化合物を用いて試験を実施した。その試験は、DSM−IV統合失調症を有する患者における、多施設での、入院患者および通院患者の、2相の、二重盲検の、ランダム化された、プラセボを対照とした式IIの化合物の概念実証試験であった。その試験は3つの異なる国にわたって21の施設を用いた。
その試験の目的には、以下のことが含まれていた:
本明細書にそのまま援用する米国特許第7,166,617号は、CYR−101のシグマ2受容体部位への優先的な結合を説明している。米国特許第7,166,617号の実施例1の試験化合物がCYR−101である。米国特許第7,166,617号の表3で説明されているように、CYR−101はシグマ2受容体に関して13nMの親和性を有する。このデータは、CYR−101はシグマ2に選択的な受容体結合を示すことを説明している。さらに、CYR−101は5−HT2A/シグマ2拮抗薬であり、ドーパミン結合特性を欠いていることが知られている。
Claims (8)
- 一日当たりの用量が16〜64mgである請求項1に記載の医薬組成物。
- 一日当たりの用量が32〜64mgである請求項1に記載の医薬組成物。
- 一日当たりの用量が16〜64mgである請求項4に記載の医薬組成物。
- 一日当たりの用量が32〜64mgである請求項4に記載の医薬組成物。
- 化合物が低いQT延長傾向を有する、請求項1〜3のいずれかに記載の医薬組成物。
- 治療の経過中に化合物が低いQT延長傾向を有する、請求項4〜6のいずれかに記載の医薬組成物。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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US36608010P | 2010-07-20 | 2010-07-20 | |
US61/366,080 | 2010-07-20 |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
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JP2016135208A Division JP2016199578A (ja) | 2010-07-20 | 2016-07-07 | シグマ受容体に仲介される障害を処置するための環状アミド誘導体の使用の方法 |
Publications (3)
Publication Number | Publication Date |
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JP2018065829A JP2018065829A (ja) | 2018-04-26 |
JP2018065829A5 JP2018065829A5 (ja) | 2018-07-05 |
JP6419294B2 true JP6419294B2 (ja) | 2018-11-07 |
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Family Applications (3)
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JP2013520841A Pending JP2013531073A (ja) | 2010-07-20 | 2011-07-20 | シグマ受容体に仲介される障害を処置するための環状アミド誘導体の使用の方法 |
JP2016135208A Pending JP2016199578A (ja) | 2010-07-20 | 2016-07-07 | シグマ受容体に仲介される障害を処置するための環状アミド誘導体の使用の方法 |
JP2017225061A Active JP6419294B2 (ja) | 2010-07-20 | 2017-11-22 | シグマ受容体に仲介される障害を処置するための環状アミド誘導体の使用の方法 |
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JP2013520841A Pending JP2013531073A (ja) | 2010-07-20 | 2011-07-20 | シグマ受容体に仲介される障害を処置するための環状アミド誘導体の使用の方法 |
JP2016135208A Pending JP2016199578A (ja) | 2010-07-20 | 2016-07-07 | シグマ受容体に仲介される障害を処置するための環状アミド誘導体の使用の方法 |
Country Status (15)
Country | Link |
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US (3) | US20130274290A1 (ja) |
EP (2) | EP4070794A3 (ja) |
JP (3) | JP2013531073A (ja) |
KR (1) | KR101867634B1 (ja) |
CN (2) | CN107007603A (ja) |
BR (1) | BR112013001302A2 (ja) |
CA (2) | CA2805904C (ja) |
DK (1) | DK2595485T3 (ja) |
ES (1) | ES2914120T3 (ja) |
HU (1) | HUE058736T2 (ja) |
PL (1) | PL2595485T3 (ja) |
PT (1) | PT2595485T (ja) |
RU (2) | RU2613201C2 (ja) |
TW (1) | TWI520949B (ja) |
WO (1) | WO2012012543A1 (ja) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8937900B2 (en) | 2010-07-20 | 2015-01-20 | Qualcomm Incorporated | Enhancing pilot channel transmission in TD-SCDMA multicarrier systems using secondary carrier frequencies |
WO2015191554A1 (en) * | 2014-06-09 | 2015-12-17 | Intra-Cellular Therapies, Inc. | Compounds and methods of use to treat schizophrenia |
EP3227273B1 (en) * | 2014-12-02 | 2022-02-09 | Minerva Neurosciences, Inc. | Compositions comprising 2-((1-(2(4-fluorophenyl)-2-oxoethyl)piperidin-4-yl)methyl)isoindolin-1-one for treating schizophrenia |
CN113694065A (zh) * | 2016-05-25 | 2021-11-26 | 田边三菱制药株式会社 | 用于治疗非精神分裂症患者中的阴性症状的组合物和方法 |
IL308650A (en) * | 2017-06-21 | 2024-01-01 | Minerva Neurosciences Inc | Stomach-resistant controlled-release oral dosage forms |
WO2020041504A1 (en) * | 2018-08-21 | 2020-02-27 | Minerva Neurosciences, Inc. | Use of roluperidone to treat negative symptoms and disorders, increase neuroplasticity, and promote neuroprotection |
IL298323B2 (en) | 2020-05-20 | 2023-10-01 | Univ Illinois | A method for treating lysosomal storage disease using histatin peptides |
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EP0497843A4 (en) * | 1989-10-27 | 1992-09-23 | The Du Pont Merck Pharmaceutical Company | (n-phthalimidoalkyl) piperidines |
NZ235841A (en) * | 1989-10-27 | 1993-03-26 | Du Pont | (n-phthalimidoalkyl) piperidine derivatives and pharmaceutical compositions |
KR100259107B1 (ko) * | 1992-04-23 | 2000-07-01 | 슈테펜 엘. 네스비트 | 세로토닌 5ht₂길항제로서의 4-이미도메틸-1-[2'-페닐-2'-옥소에틸]피페리딘, 이의 제조방법 및 이를 포함하는 약제학적 조성물 |
CN100384836C (zh) * | 2000-02-29 | 2008-04-30 | 三菱制药株式会社 | 新型环状酰胺衍生物 |
TW200817400A (en) * | 2006-05-30 | 2008-04-16 | Elbion Ag | Pyrido [3,2-e] pyrazines, their use as inhibitors of phosphodiesterase 10, and processes for preparing them |
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2011
- 2011-07-20 ES ES11810350T patent/ES2914120T3/es active Active
- 2011-07-20 HU HUE11810350A patent/HUE058736T2/hu unknown
- 2011-07-20 US US13/810,775 patent/US20130274290A1/en not_active Abandoned
- 2011-07-20 CN CN201611063838.0A patent/CN107007603A/zh active Pending
- 2011-07-20 CN CN2011800450188A patent/CN103108548A/zh active Pending
- 2011-07-20 WO PCT/US2011/044698 patent/WO2012012543A1/en active Application Filing
- 2011-07-20 BR BR112013001302A patent/BR112013001302A2/pt not_active Application Discontinuation
- 2011-07-20 RU RU2013107378A patent/RU2613201C2/ru active
- 2011-07-20 CA CA2805904A patent/CA2805904C/en active Active
- 2011-07-20 RU RU2017105262A patent/RU2746871C2/ru active
- 2011-07-20 EP EP22162273.1A patent/EP4070794A3/en active Pending
- 2011-07-20 EP EP11810350.6A patent/EP2595485B1/en active Active
- 2011-07-20 PT PT118103506T patent/PT2595485T/pt unknown
- 2011-07-20 DK DK11810350.6T patent/DK2595485T3/da active
- 2011-07-20 JP JP2013520841A patent/JP2013531073A/ja active Pending
- 2011-07-20 TW TW100125662A patent/TWI520949B/zh active
- 2011-07-20 KR KR1020137004218A patent/KR101867634B1/ko active IP Right Grant
- 2011-07-20 PL PL11810350T patent/PL2595485T3/pl unknown
- 2011-07-20 CA CA3154027A patent/CA3154027A1/en active Pending
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2016
- 2016-05-24 US US15/163,385 patent/US20160354357A1/en not_active Abandoned
- 2016-07-07 JP JP2016135208A patent/JP2016199578A/ja active Pending
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2017
- 2017-11-22 JP JP2017225061A patent/JP6419294B2/ja active Active
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2020
- 2020-06-29 US US16/914,862 patent/US20210106573A1/en active Pending
Also Published As
Publication number | Publication date |
---|---|
CN103108548A (zh) | 2013-05-15 |
RU2017105262A3 (ja) | 2019-01-18 |
JP2016199578A (ja) | 2016-12-01 |
HUE058736T2 (hu) | 2022-09-28 |
WO2012012543A1 (en) | 2012-01-26 |
PT2595485T (pt) | 2022-05-30 |
TWI520949B (zh) | 2016-02-11 |
EP4070794A2 (en) | 2022-10-12 |
RU2013107378A (ru) | 2014-08-27 |
EP4070794A3 (en) | 2023-01-18 |
RU2613201C2 (ru) | 2017-03-15 |
JP2018065829A (ja) | 2018-04-26 |
US20130274290A1 (en) | 2013-10-17 |
EP2595485A1 (en) | 2013-05-29 |
JP2013531073A (ja) | 2013-08-01 |
US20160354357A1 (en) | 2016-12-08 |
BR112013001302A2 (pt) | 2017-07-04 |
CA2805904C (en) | 2022-06-21 |
EP2595485A4 (en) | 2014-04-23 |
RU2017105262A (ru) | 2019-01-18 |
KR20130129906A (ko) | 2013-11-29 |
KR101867634B1 (ko) | 2018-06-15 |
US20210106573A1 (en) | 2021-04-15 |
ES2914120T3 (es) | 2022-06-07 |
RU2746871C2 (ru) | 2021-04-21 |
TW201211022A (en) | 2012-03-16 |
PL2595485T3 (pl) | 2022-06-20 |
DK2595485T3 (da) | 2022-05-30 |
EP2595485B1 (en) | 2022-03-16 |
CA2805904A1 (en) | 2012-01-26 |
CN107007603A (zh) | 2017-08-04 |
CA3154027A1 (en) | 2012-01-26 |
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