EA201690094A1 - Ингибиторы syk - Google Patents
Ингибиторы sykInfo
- Publication number
- EA201690094A1 EA201690094A1 EA201690094A EA201690094A EA201690094A1 EA 201690094 A1 EA201690094 A1 EA 201690094A1 EA 201690094 A EA201690094 A EA 201690094A EA 201690094 A EA201690094 A EA 201690094A EA 201690094 A1 EA201690094 A1 EA 201690094A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- compounds
- syk
- formula
- present
- syk inhibitors
- Prior art date
Links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- 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
- A61P11/06—Antiasthmatics
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- 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
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- 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
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- 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
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- 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
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- 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
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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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
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- 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]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
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- 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
- A61P37/08—Antiallergic 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
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- 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
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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
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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
- C07D403/14—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
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- 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
- C07D405/14—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 three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
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- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- 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
- C07D487/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/08—Bridged systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Abstract
Настоящее изобретение относится к соединениям, которые представляют собой ингибиторы Syk, и к их применению для лечения различных болезненных состояний, в том числе раковых заболеваний и воспалительных состояний. Согласно конкретным вариантам реализации структура соединений представлена формулой Iгде X, X, X, R, R, R, Rи Y такие, как описано в настоящем документе. В настоящем изобретении также предложены фармацевтические композиции, которые включают соединение формулы I или его фармацевтически приемлемые соли, и способы применения указанных соединений и композиций для лечения состояний, опосредованных Syk.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361860870P | 2013-07-31 | 2013-07-31 | |
US201462025304P | 2014-07-16 | 2014-07-16 | |
PCT/US2014/049032 WO2015017610A1 (en) | 2013-07-31 | 2014-07-31 | Syk inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201690094A1 true EA201690094A1 (ru) | 2016-08-31 |
EA031601B1 EA031601B1 (ru) | 2019-01-31 |
Family
ID=51359434
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201690094A EA031601B1 (ru) | 2013-07-31 | 2014-07-31 | Ингибиторы syk |
Country Status (16)
Country | Link |
---|---|
US (2) | US9376441B2 (ru) |
EP (1) | EP3027601B1 (ru) |
JP (1) | JP6159028B2 (ru) |
KR (1) | KR101750667B1 (ru) |
CN (1) | CN105555780B (ru) |
AU (1) | AU2014296184B2 (ru) |
BR (1) | BR112016001954A2 (ru) |
CA (1) | CA2919479C (ru) |
EA (1) | EA031601B1 (ru) |
ES (1) | ES2656192T3 (ru) |
IL (1) | IL243578A0 (ru) |
MX (1) | MX2016001427A (ru) |
NZ (1) | NZ715747A (ru) |
PT (1) | PT3027601T (ru) |
SG (1) | SG11201600373YA (ru) |
WO (1) | WO2015017610A1 (ru) |
Families Citing this family (39)
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NZ593460A (en) | 2008-12-08 | 2013-11-29 | Gilead Connecticut Inc | Imidazopyrazine syk inhibitors |
NZ602362A (en) | 2010-03-11 | 2014-11-28 | Gilead Connecticut Inc | Imidazopyridines syk inhibitors |
AP2016009007A0 (en) | 2013-07-30 | 2016-01-31 | Gilead Connecticut Inc | Formulation of syk inhibitors |
KR101810798B1 (ko) | 2013-07-30 | 2017-12-19 | 질레드 코네티컷 인코포레이티드 | Syk 억제제의 다형체 |
JP6159028B2 (ja) | 2013-07-31 | 2017-07-05 | ギリアード サイエンシーズ, インコーポレイテッド | Syk阻害剤 |
EA201690608A1 (ru) | 2013-12-04 | 2016-12-30 | Джилид Сайэнс, Инк. | Способы лечения раковых заболеваний |
US9290505B2 (en) | 2013-12-23 | 2016-03-22 | Gilead Sciences, Inc. | Substituted imidazo[1,2-a]pyrazines as Syk inhibitors |
UY35898A (es) | 2013-12-23 | 2015-07-31 | Gilead Sciences Inc | ?compuestos inhibidores de syk y composiciones que los comprenden?. |
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JP6177456B2 (ja) | 2014-04-04 | 2017-08-09 | ファイザー・インク | 二環式縮合ヘテロアリールまたはアリール化合物およびirak4阻害剤としてのそれらの使用 |
KR20170029580A (ko) | 2014-07-14 | 2017-03-15 | 길리애드 사이언시즈, 인코포레이티드 | 암을 치료하기 위한 조합물 |
CA2998250A1 (en) * | 2015-09-11 | 2017-03-16 | Boehringer Ingelheim International Gmbh | Pyrazolyl-substituted heteroaryls and their use as medicaments |
CO2018008799A2 (es) | 2016-02-24 | 2018-09-20 | Pfizer | Derivados de pirazolo[1,5-a]pirazin-4-ilo como inhibidores de jak |
CN105646476B (zh) * | 2016-03-07 | 2018-09-04 | 暨南大学 | 联苯并[1,2,5]硒二唑衍生物及其制备方法和应用 |
DK3500568T3 (da) | 2016-08-16 | 2020-12-14 | Bayer Cropscience Ag | Fremgangsmåde til fremstilling af 2-(3,6-dihalopyridin-2-yl)-3h-imidazol[4,5-c]pyridinderivater og beslægtede forbindelser ved hjælp af omsætning af 3h-imidazol[4,5-c]pyridinderivatet med en metalorganisk zink-amin base |
AU2017325844A1 (en) | 2016-09-14 | 2019-03-07 | Gilead Sciences, Inc. | SYK inhibitors |
KR102471278B1 (ko) | 2016-09-14 | 2022-11-25 | 바이엘 크롭사이언스 악티엔게젤샤프트 | 할로겐화 바이사이클릭 화합물의 제조 방법 |
TW201822764A (zh) | 2016-09-14 | 2018-07-01 | 美商基利科學股份有限公司 | Syk抑制劑 |
WO2018195471A1 (en) | 2017-04-21 | 2018-10-25 | Gilead Sciences, Inc. | Syk inhibitors in combination with hypomethylating agents |
EP3668858A1 (en) | 2017-08-14 | 2020-06-24 | Pfizer Inc | Pyrazolo[1,5-a]pyrazin-4-yl and related derivatives |
CA3073871A1 (en) | 2017-08-25 | 2019-02-28 | Gilead Sciences, Inc. | Polymorphs of syk inhibitors |
EP3636645A1 (de) | 2018-10-11 | 2020-04-15 | Bayer Aktiengesellschaft | Verfahren zur herstellung schwefel-substituierter pyridinderivate |
ES2951539T3 (es) | 2018-10-11 | 2023-10-23 | Bayer Ag | Procedimiento para la preparación de derivados de imidazol |
CA3116347A1 (en) * | 2018-10-31 | 2020-05-07 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity |
JP7460644B2 (ja) | 2018-10-31 | 2024-04-02 | ギリアード サイエンシーズ, インコーポレイテッド | Hpk1阻害剤としての置換6-アザベンゾイミダゾール化合物 |
KR20210131372A (ko) | 2019-02-22 | 2021-11-02 | 크로노스 바이오, 인코포레이티드 | Syk 억제제로서의 축합된 피라진의 고체 형태 |
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BR112014001898A2 (pt) * | 2011-07-26 | 2017-02-21 | Boehringer Ingelheim Int | quinolinas substituídas e seu uso como medicamentos |
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2014
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- 2014-07-31 WO PCT/US2014/049032 patent/WO2015017610A1/en active Application Filing
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- 2014-07-31 ES ES14752974.7T patent/ES2656192T3/es active Active
- 2014-07-31 US US14/448,160 patent/US9376441B2/en active Active
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- 2014-07-31 AU AU2014296184A patent/AU2014296184B2/en not_active Ceased
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- 2014-07-31 EA EA201690094A patent/EA031601B1/ru not_active IP Right Cessation
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EP3027601B1 (en) | 2017-10-25 |
JP2016529244A (ja) | 2016-09-23 |
AU2014296184A1 (en) | 2016-01-28 |
MX2016001427A (es) | 2016-08-03 |
US9376441B2 (en) | 2016-06-28 |
CN105555780A (zh) | 2016-05-04 |
SG11201600373YA (en) | 2016-02-26 |
US20150038488A1 (en) | 2015-02-05 |
ES2656192T3 (es) | 2018-02-26 |
US20160368918A1 (en) | 2016-12-22 |
WO2015017610A1 (en) | 2015-02-05 |
PT3027601T (pt) | 2018-01-08 |
KR101750667B1 (ko) | 2017-07-04 |
EA031601B1 (ru) | 2019-01-31 |
US10005774B2 (en) | 2018-06-26 |
AU2014296184B2 (en) | 2017-04-27 |
EP3027601A1 (en) | 2016-06-08 |
BR112016001954A2 (pt) | 2017-08-01 |
NZ715747A (en) | 2017-03-31 |
IL243578A0 (en) | 2016-02-29 |
CA2919479A1 (en) | 2015-02-05 |
KR20160037198A (ko) | 2016-04-05 |
CN105555780B (zh) | 2018-01-23 |
JP6159028B2 (ja) | 2017-07-05 |
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