ES2688395T3 - Derivados de bencimidazol novedosos como inhibidores de cinasa - Google Patents

Derivados de bencimidazol novedosos como inhibidores de cinasa Download PDF

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Publication number
ES2688395T3
ES2688395T3 ES13811246.1T ES13811246T ES2688395T3 ES 2688395 T3 ES2688395 T3 ES 2688395T3 ES 13811246 T ES13811246 T ES 13811246T ES 2688395 T3 ES2688395 T3 ES 2688395T3
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Prior art keywords
nitro
heterocycle
independently selected
optionally substituted
dibromo
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Spanish (es)
Inventor
Wojciech Czardybon
Krzysztof Brzózka
Michal GALEZOWSKI
Renata Windak
Mariusz Milik
Magdalena ZAWADZKA
Pawel GUZIK
Ewelina WINCZA
Marta PROKOP
Katarzyna WIKLIK
Aleksandra Sabiniarz
Wieslaw Marek Cholody
Raymond Horvath
Tomasz RZYMSKI
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Selvita Sp zoo
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Selvita Sp zoo
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/14—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Epidemiology (AREA)
ES13811246.1T 2012-12-21 2013-12-20 Derivados de bencimidazol novedosos como inhibidores de cinasa Active ES2688395T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1223265.8A GB201223265D0 (en) 2012-12-21 2012-12-21 Novel benzimidazole derivatives as kinase inhibitors
GB201223265 2012-12-21
PCT/EP2013/077754 WO2014096388A2 (en) 2012-12-21 2013-12-20 Novel benzimidazole derivatives as kinase inhibitors

Publications (1)

Publication Number Publication Date
ES2688395T3 true ES2688395T3 (es) 2018-11-02

Family

ID=47682482

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ES13811246.1T Active ES2688395T3 (es) 2012-12-21 2013-12-20 Derivados de bencimidazol novedosos como inhibidores de cinasa

Country Status (23)

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US (2) US9388192B2 (Direct)
EP (1) EP2935244B1 (Direct)
JP (1) JP6169185B2 (Direct)
KR (1) KR101779272B1 (Direct)
CN (1) CN104936951B (Direct)
AU (1) AU2013366513B2 (Direct)
BR (1) BR112015014701B8 (Direct)
CA (1) CA2896156C (Direct)
CY (1) CY1120692T1 (Direct)
DK (1) DK2935244T3 (Direct)
ES (1) ES2688395T3 (Direct)
GB (1) GB201223265D0 (Direct)
HR (1) HRP20181429T8 (Direct)
HU (1) HUE039376T2 (Direct)
IL (1) IL239193A0 (Direct)
LT (1) LT2935244T (Direct)
MX (1) MX369589B (Direct)
PL (1) PL2935244T3 (Direct)
PT (1) PT2935244T (Direct)
RS (1) RS57658B1 (Direct)
SI (1) SI2935244T1 (Direct)
SM (1) SMT201800473T1 (Direct)
WO (1) WO2014096388A2 (Direct)

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CR20160363A (es) 2014-01-14 2016-10-12 Millennium Pharm Inc Heteroarilos y usos de estos
MX2017004543A (es) 2014-10-06 2017-10-04 Vertex Pharma Moduladores de regulador de conductancia transmembranal de fibrosis quística.
MX2018002631A (es) 2015-09-03 2019-02-07 Univ Arizona Inhibidores de molecula pequeña de dyrkia y usos de los mismos.
PL3436446T3 (pl) 2016-03-31 2023-09-11 Vertex Pharmaceuticals Incorporated Modulatory mukowiscydozowego przezbłonowego regulatora przewodnictwa
PT3519401T (pt) 2016-09-30 2021-12-27 Vertex Pharma Modulador de regulador de condutância transmembranar de fibrose quística, composições farmacêuticas, métodos de tratamento e processo para fazer o modulador
WO2018107100A1 (en) 2016-12-09 2018-06-14 Vertex Pharmaceuticals Incorporated Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
US9855255B1 (en) 2017-05-26 2018-01-02 King Saud University Substituted naphthyridinyl hydrazines as anti-liver cancer agents
US11253509B2 (en) 2017-06-08 2022-02-22 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
AU2018304168B2 (en) 2017-07-17 2023-05-04 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
AR112467A1 (es) 2017-08-02 2019-10-30 Vertex Pharma Procesos para preparar compuestos
IL273831B2 (en) 2017-10-19 2024-10-01 Vertex Pharma Crystalline forms and compositions of cftr modulators
WO2019079578A1 (en) 2017-10-19 2019-04-25 Amgen Inc. BENZIMIDAZOLE DERIVATIVES AND USES THEREOF
EP3720849A2 (en) 2017-12-08 2020-10-14 Vertex Pharmaceuticals Incorporated Processes for making modulators of cystic fibrosis transmembrane conductance regulator
TWI810243B (zh) 2018-02-05 2023-08-01 美商維泰克斯製藥公司 用於治療囊腫纖化症之醫藥組合物
US12528810B2 (en) 2018-03-01 2026-01-20 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of DYRK/CLK and uses thereof
WO2019200246A1 (en) 2018-04-13 2019-10-17 Alexander Russell Abela Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
KR20210059663A (ko) * 2019-11-15 2021-05-25 가천대학교 산학협력단 신규한 벤즈이미다졸 유도체 및 이의 용도
CN113491691B (zh) * 2020-04-02 2023-04-14 深圳贝瑞生物医药科技有限公司 一种用于制备抗肿瘤药物或14-3-3η蛋白抑制剂的化合物
KR102854745B1 (ko) * 2020-04-23 2025-09-04 진크래프트 주식회사 R-point 조절 단백질 복합체를 유효성분으로 포함하는 폐암 치료용 약학적 조성물, 상기 복합체의 형성 여부를 이용한 폐암 치료제 스크리닝 방법 및 폐암 진단 방법
WO2023241627A1 (en) * 2022-06-15 2023-12-21 Insilico Medicine Ip Limited Cdk8/19 dual inhibitors and methods of use thereof
IL318614A (en) 2022-07-29 2025-03-01 Ryvu Therapeutics S A Cancer treatment combination that includes a BCL-2 inhibitor
EP4561577A1 (en) 2022-07-29 2025-06-04 Ryvu Therapeutics S.A. Cancer combination therapy including a flt3-inhibitor
CN120826396A (zh) * 2023-03-06 2025-10-21 英矽智能科技(上海)有限公司 Cdk8/19双重抑制剂及其使用方法
CN120004808B (zh) * 2023-11-15 2025-11-25 宜昌人福药业有限责任公司 一种2-溴-5,6-二氯-1h-苯并咪唑的制备方法

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JP2012520884A (ja) * 2009-03-18 2012-09-10 ザ ボード オブ トラスティーズ オブ ザ リランド スタンフォード ジュニア ユニバーシティー フラビウイルス科ウイルス感染症を治療する方法および組成物
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GB201223265D0 (en) 2012-12-21 2013-02-06 Selvita Sa Novel benzimidazole derivatives as kinase inhibitors

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RS57658B1 (sr) 2018-11-30
PT2935244T (pt) 2018-10-22
US20170152249A1 (en) 2017-06-01
KR101779272B1 (ko) 2017-09-18
HUE039376T2 (hu) 2018-12-28
DK2935244T3 (en) 2018-09-10
IL239193A0 (en) 2015-07-30
SI2935244T1 (sl) 2019-01-31
US10174013B2 (en) 2019-01-08
MX369589B (es) 2019-11-13
WO2014096388A2 (en) 2014-06-26
WO2014096388A3 (en) 2014-08-21
BR112015014701B8 (pt) 2022-12-13
SMT201800473T1 (it) 2018-11-09
LT2935244T (lt) 2018-10-25
CN104936951A (zh) 2015-09-23
BR112015014701B1 (pt) 2022-11-01
CY1120692T1 (el) 2019-12-11
BR112015014701A2 (pt) 2017-07-11
US9388192B2 (en) 2016-07-12
CA2896156C (en) 2018-05-22
KR20150095908A (ko) 2015-08-21
EP2935244B1 (en) 2018-06-27
HRP20181429T1 (hr) 2018-11-30
EP2935244A2 (en) 2015-10-28
AU2013366513B2 (en) 2016-09-01
CN104936951B (zh) 2018-02-06
JP2016503779A (ja) 2016-02-08
GB201223265D0 (en) 2013-02-06
AU2013366513A1 (en) 2015-06-11
US20150336967A1 (en) 2015-11-26
HRP20181429T8 (hr) 2018-12-28
PL2935244T3 (pl) 2019-02-28
CA2896156A1 (en) 2014-06-26
JP6169185B2 (ja) 2017-07-26
MX2015007057A (es) 2016-01-20

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