ES2628365T3 - Moduladores de quinolinilo unidos a fenilo de ROR-GAMA-T - Google Patents
Moduladores de quinolinilo unidos a fenilo de ROR-GAMA-T Download PDFInfo
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- ES2628365T3 ES2628365T3 ES13818857T ES13818857T ES2628365T3 ES 2628365 T3 ES2628365 T3 ES 2628365T3 ES 13818857 T ES13818857 T ES 13818857T ES 13818857 T ES13818857 T ES 13818857T ES 2628365 T3 ES2628365 T3 ES 2628365T3
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- alkyl
- optionally substituted
- pyridyl
- och3
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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
- C07D401/02—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
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- 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
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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
- 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
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D413/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
-
- 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
Abstract
Los compuestos de Fórmula 1: **Fórmula** en donde: R1 es pirrolilo, pirazolilo, imidazolilo, triazolilo, tiazolilo, piridilo, piridilo N-óxido, pirazinilo, pirimidinilo, piridazilo, piperidinailo, quinazolinilo, cinolinilo, benzotiazolilo, indazolilo, tetrahidropiranilo, tetrahidrofuranilo, furanilo, fenilo, oxazolilo, isoxazolilo, tiofenilo, benzoxazolilo, bencimidazolilo, indolilo, tiadiazolilo, oxadiazolilo o quinolinilo; en el que dicho piridilo, piridilo N-óxido, pirazinilo, pirimidinilo, piridazilo, piperidinailo, quinazolinilo, cinolinilo, benzotiazolilo, indazolilo, imidazolilo, fenilo, tiofenilo, benzoxazolilo, bencimidazolilo, indolilo, quinolinilo, y pirazolilo están opcionalmente sustituidos con C(O)C(1-4)alquilo, C(O)NH2, C(O)NHC(1-2)alquilo, C(O)N(C(1-2)alquilo)2, NHC(O)C(1-4)alilo, NHSO2C(1-4)alquilo, C(1-4)alquilo, CF3, CH2CF3, Cl, F, -CN, OC(1-4)alquilo, N(C(1-4)alquilo)2, (CH2)3OCH3, SC(1-4)alquilo, OH, CO2H, CO2C(1-4)alquilo, C(O)CF3, SO2CF3, OCF3, OCHF2, SO2CH3, SO2NH2, SO2NHC(1-2)alquilo, SO2N(C(1-2)alquilo)2, C(O)NHSO2CH3, o OCH2OCH3; y opcionalmente sustituidos con hasta dos sustituyentes adicionales seleccionados independientemente del grupo que consiste en Cl, C(1-2)alquilo, SCH3, OC(1-2)alquilo, CF3, -CN, y F; y en los que dichos triazolilo, oxazolilo, isoxazolilo, pirrolilo, y tiazolilo están opcionalmente sustituidos con hasta dos sustituyentes seleccionados independientemente del grupo que consiste en SO2CH3, SO2NH2, alquilo C(O)NH2, -CN, OC(1-2), (CH2)(2-3)OCH3, SCH3, CF3, F, Cl, y C(1-2)alquilo; y dicho tiadiazolilo y oxadiazolilo están opcionalmente sustituidos con C(1-2)alquilo; y dichos piridilo, piridiloóxido, pirimidinilo, piridazilo, y pirazinilo están opcionalmente sustituidos con hasta tres sustituyentes adicionales seleccionados independientemente del grupo que consiste en C(O)NHC(1-2)alquilo, C(O)N(C(1-2)alquilo)2, NHC(O)C(1-4)alquilo, NHSO2C(1-4)alquilo, C(O)CF3, SO2CF3, SO2NHC(1-2)alquilo, SO2N(C(1-2)alquilo)2, C(O)NHSO2CH3, SO2CH3, SO2NH2, C(O)NH2, -35 CN, OC(1-4)alquilo, (CH2)(2-3)OCH3, SC(1-4)alquilo, CF3, F, Cl, y C(1-4)alquilo; R2es triazolilo, piridilo, piridiloóxido, pirazolilo, pirimidinilo, oxazolilo, isoxazolilo, piperidinilo de N-acetilo, 1-H-piperidinilo, N-Boc-piperidinilo, N-C(1-3)alquilpiperidinilo, tiazolilo, piridazilo, pirazinilo, 1-(3-metoxipropilo)-imidazolilo, tiadiazolilo, oxadiazolilo, o imidazolilo; en el que dicho imidazolilo está opcionalmente sustituido con hasta tres sustituyentes adicionales seleccionados independientemente del grupo que consiste en C(1-2)alquilo, SCH3, OC(1-2)alquilo, CF3, -CN, F, y Cl; y dicho piridilo, piridiloóxido, pirimidinilo, piridazilo, y pirazinilo, están opcionalmente sustituidos con hasta tres sustituyentes adicionales seleccionados independientemente del grupo que consiste en SO2CH3, SO2NH2, C(O)NH2, -CN, OC(1-2)alquilo, (CH2)(2-3)OCH3, SCH3, CF3, F, Cl, o C(1-2)alquilo; y dichos triazolilo, tiazolilo, oxazolilo e isoxazolilo están opcionalmente sustituidos con hasta dos sustituyentes seleccionados independientemente del grupo que consiste en SO2CH3, SO2NH2, C(O)NH2, -CN, OC(1-2)alquilo, (CH2)(2-3)OCH3, SCH3, CF3, F, Cl, y C(1-2)alquilo; y dicho tiadiazolilo y oxadiazolilo están opcionalmente sustituidos con C(1-2)alquilo; y dicho pirazolilo está opcionalmente sustituido con hasta tres grupos CH3; R3es H, OH, OCH3, o NH2; R4es H o F; R5es H, Cl, -CN, CF3, SC(1-4)alquilo, OC(1-4)alquilo, OH, C(1-4)alquilo, N(CH3)OCH3, NH(C(1-4)alquilo), N(C(1-4)alquilo)2, o 4-hidroxi-piperidinilo;
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261714433P | 2012-10-16 | 2012-10-16 | |
US201261725537P | 2012-11-13 | 2012-11-13 | |
PCT/US2013/065026 WO2014062667A1 (en) | 2012-10-16 | 2013-10-15 | Phenyl linked quinolinyl modulators of ror-gamma-t |
Publications (1)
Publication Number | Publication Date |
---|---|
ES2628365T3 true ES2628365T3 (es) | 2017-08-02 |
Family
ID=49943493
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES13818857T Active ES2628365T3 (es) | 2012-10-16 | 2013-10-15 | Moduladores de quinolinilo unidos a fenilo de ROR-GAMA-T |
Country Status (21)
Country | Link |
---|---|
US (1) | US9309222B2 (es) |
EP (1) | EP2909193B1 (es) |
JP (1) | JP6251277B2 (es) |
KR (1) | KR20150070350A (es) |
CN (1) | CN105073729A (es) |
AU (1) | AU2013331505A1 (es) |
CA (1) | CA2888485C (es) |
CL (1) | CL2015000946A1 (es) |
CO (1) | CO7350658A2 (es) |
CR (1) | CR20150192A (es) |
EA (1) | EA201590750A1 (es) |
EC (1) | ECSP15015155A (es) |
ES (1) | ES2628365T3 (es) |
GT (1) | GT201500092A (es) |
HK (1) | HK1213887A1 (es) |
IL (1) | IL238122A0 (es) |
MX (1) | MX2015004784A (es) |
PE (1) | PE20151203A1 (es) |
PH (1) | PH12015500776A1 (es) |
SG (1) | SG11201502935VA (es) |
WO (1) | WO2014062667A1 (es) |
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CA2926339A1 (en) * | 2013-10-15 | 2015-04-23 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of roryt |
US10555941B2 (en) | 2013-10-15 | 2020-02-11 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of RORγt |
US9403816B2 (en) | 2013-10-15 | 2016-08-02 | Janssen Pharmaceutica Nv | Phenyl linked quinolinyl modulators of RORγt |
BR112016008183A2 (pt) * | 2013-10-15 | 2017-10-03 | Janssen Pharmaceutica Nv | Moduladores de ror-gama-t de quinolinila ligados à fenila |
WO2015057626A1 (en) | 2013-10-15 | 2015-04-23 | Janssen Pharmaceutica Nv | QUINOLINYL MODULATORS OF RORyT |
CA2926313A1 (en) * | 2013-10-15 | 2015-04-23 | Kristi A. Leonard | Secondary alcohol quinolinyl modulators of roryt |
AU2015301891B2 (en) | 2014-08-11 | 2019-12-05 | Angion Biomedica Corporation | Cytochrome P450 inhibitors and uses thereof |
JOP20200117A1 (ar) * | 2014-10-30 | 2017-06-16 | Janssen Pharmaceutica Nv | كحولات ثلاثي فلوروميثيل كمُعدلات للمستقبل النووي جاما تي المرتبط بحمض الريتيونَويك ROR?t |
US10287282B2 (en) | 2014-12-31 | 2019-05-14 | Angion Biomedica Corp. | Methods and agents for treating disease |
WO2016110821A1 (en) | 2015-01-08 | 2016-07-14 | Advinus Therapeutics Limited | Bicyclic compounds, compositions and medicinal applications thereof |
WO2016128908A1 (en) | 2015-02-12 | 2016-08-18 | Advinus Therapeutics Limited | Bicyclic compounds, compositions and medicinal applications thereof |
TW202220968A (zh) * | 2016-01-29 | 2022-06-01 | 美商維它藥物有限責任公司 | ROR-γ調節劑 |
CA3030423A1 (en) * | 2016-07-14 | 2018-01-18 | Crinetics Pharmaceuticals, Inc. | Somatostatin modulators and uses thereof |
WO2018112842A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | 6,6-fused heteroaryl piperidine ether allosteric modulators of m4 muscarinic acetylcholine receptor |
WO2019023278A1 (en) | 2017-07-25 | 2019-01-31 | Crinetics Pharmaceuticals, Inc. | MODULATORS OF SOMATOSTATIN AND USES THEREOF |
BR112020014462A2 (pt) | 2018-01-17 | 2020-12-01 | Crinetics Pharmaceuticals, Inc. | processo de produção de moduladores de somatostatina |
CN108503581A (zh) * | 2018-04-12 | 2018-09-07 | 苏州康润医药有限公司 | 一种3-溴-6-氟-2-吡啶乙酮的合成方法 |
WO2022055880A1 (en) | 2020-09-09 | 2022-03-17 | Crinetics Pharmaceuticals, Inc. | Formulations of a somatostatin modulator |
CN117682980A (zh) * | 2024-02-02 | 2024-03-12 | 济南悟通生物科技有限公司 | 一种2-乙酰基四氢吡啶的制备方法 |
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- 2013-10-15 JP JP2015537770A patent/JP6251277B2/ja not_active Expired - Fee Related
- 2013-10-15 EP EP13818857.8A patent/EP2909193B1/en active Active
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- 2013-10-15 ES ES13818857T patent/ES2628365T3/es active Active
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- 2013-10-15 PE PE2015000492A patent/PE20151203A1/es not_active Application Discontinuation
- 2013-10-15 SG SG11201502935VA patent/SG11201502935VA/en unknown
- 2013-10-15 US US14/053,707 patent/US9309222B2/en active Active
- 2013-10-15 CN CN201380065774.6A patent/CN105073729A/zh active Pending
- 2013-10-15 AU AU2013331505A patent/AU2013331505A1/en not_active Abandoned
- 2013-10-15 WO PCT/US2013/065026 patent/WO2014062667A1/en active Application Filing
- 2013-10-15 MX MX2015004784A patent/MX2015004784A/es unknown
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Also Published As
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MX2015004784A (es) | 2015-08-14 |
CN105073729A (zh) | 2015-11-18 |
GT201500092A (es) | 2015-12-31 |
CA2888485A1 (en) | 2014-04-24 |
IL238122A0 (en) | 2015-05-31 |
KR20150070350A (ko) | 2015-06-24 |
CO7350658A2 (es) | 2015-08-10 |
US20140107097A1 (en) | 2014-04-17 |
CL2015000946A1 (es) | 2015-10-02 |
EA201590750A1 (ru) | 2015-09-30 |
HK1213887A1 (zh) | 2016-07-15 |
SG11201502935VA (en) | 2015-09-29 |
EP2909193B1 (en) | 2017-04-19 |
WO2014062667A1 (en) | 2014-04-24 |
US9309222B2 (en) | 2016-04-12 |
AU2013331505A1 (en) | 2015-04-30 |
PE20151203A1 (es) | 2015-08-31 |
CR20150192A (es) | 2015-05-18 |
JP6251277B2 (ja) | 2017-12-20 |
CA2888485C (en) | 2021-01-26 |
PH12015500776A1 (en) | 2015-06-22 |
EP2909193A1 (en) | 2015-08-26 |
ECSP15015155A (es) | 2016-01-29 |
JP2015536321A (ja) | 2015-12-21 |
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