AR094412A1 - Carboxamidas basadas en pirazolilo i - Google Patents
Carboxamidas basadas en pirazolilo iInfo
- Publication number
- AR094412A1 AR094412A1 ARP140100092A ARP140100092A AR094412A1 AR 094412 A1 AR094412 A1 AR 094412A1 AR P140100092 A ARP140100092 A AR P140100092A AR P140100092 A ARP140100092 A AR P140100092A AR 094412 A1 AR094412 A1 AR 094412A1
- Authority
- AR
- Argentina
- Prior art keywords
- residue
- polysubstituted
- monosubstituted
- unsubstituted
- independently
- Prior art date
Links
- 229910052757 nitrogen Inorganic materials 0.000 abstract 41
- 125000001931 aliphatic group Chemical group 0.000 abstract 10
- 229910052760 oxygen Inorganic materials 0.000 abstract 5
- 229910052717 sulfur Inorganic materials 0.000 abstract 5
- 101100495923 Schizosaccharomyces pombe (strain 972 / ATCC 24843) chr2 gene Proteins 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 208000027866 inflammatory disease Diseases 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
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- C07D401/10—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 aromatic rings
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Abstract
Inhibidores de ICRAC, composiciones farmacéuticas que contienen a estos compuestos y su uso en el tratamiento y/o la profilaxis de enfermedades y/o trastornos, en particular enfermedades inflamatorias y/o trastornos inflamatorios. Reivindicación 1: Un compuesto caracterizado porque es de fórmula general (1), donde R¹ denota H; residuo alifático C₁₋₄, no sustituido o monosustituido o polisustituido; o residuo cicloalifático C₃₋₆ o un residuo heterocicloalifático de entre 3 y 7 miembros, en cada caso no sustituido o monosustituido o polisustituido y en cada caso opcionalmente conectado a través de un grupo alifático C₁₋₄, que a su vez puede no estar sustituido o estar monosustituido o polisustituido; con la condición de que si R¹ representa un residuo heterocicloalifático de entre 3 y 7 miembros, dicho residuo heterocicloalifático de entre 3 y 7 miembros se conecta a la parte restante de la estructura de acuerdo con la fórmula general (1) a través de un átomo de carbono del residuo heterocicloalifático de entre 3 y 7 miembros; R² denota H; F; Cl; Br; I; NO₂; CN; CF₃; CF₂H; CFH₂; R¹³; OH; O-R¹³; NH₂; N(H)R¹³; N(R¹³)₂; T representa C-R³ o N o N⁺-O⁻, U representa C-R⁴ o N o N⁺-O⁻, y representa C-R⁵ o N o N⁺-O⁻, W representa C-R⁶ o N o N⁺-O⁻, y X representa C-R⁷ o N o N⁺-O⁻, con la condición de que 0, 1, 2 ó 3 de las variables T, U, V, W y X en forma independiente entre sí representan N o N⁺-O⁻, donde 0 ó 1 de las variables T, U, V, W y X en forma independiente entre sí representan N⁺-O⁻ y con la condición de que al menos uno de U, V y W no representa N, donde al menos uno de R⁴, R⁵ y R⁶ se selecciona entre el grupo que consiste en residuo cicloalifático C₃₋₆, no sustituido o monosustituido o polisustituido; residuo heterocicloalifático de entre 3 y 7 miembros, no sustituido o monosustituido o polisustituido; arilo, no sustituido o monosustituido o polisustituido; y heteroarilo, no sustituido o monosustituido o polisustituido, y los sustituyentes restantes de R³, R⁴, R⁵, R⁶ y R⁷ se seleccionan en forma independiente entre sí entre el grupo que consiste en H; F; Cl, Br; I; NO₂; CN; CF₃; CF₂H; CFH₂; CF₂Cl; CFCl₂; R¹³; R¹⁴; C(=O)OH; C(=O)-R¹³; C(=O)R¹⁴; C(=O)-OR¹³; C(=O)-OR¹⁴; C(=O)-N(H)(OH); C(=NOH)-H; C(=N-OH)-R¹³; C(=N-OH)-R¹⁴; C(=N-O-R¹³)-H; C(=N-OR¹³)-R¹³; C(=N-O-R¹³)-R¹⁴; C(O)NH₂; C(=O)-N(H)R¹³; C(=O)-N(R¹³)₂; C(=O)-N(H)R¹⁴; C(=O)-N(R¹⁴)₂; C(=O)-N(R¹³)(R¹⁴); C(=O)-N(Rᵃ) (Rᵇ); OH; OR¹³; OCF₃; OCF₂H; OCFH₂; OCF₂Cl; OCFCl₂; OR¹⁴; O-C(=O)-R¹³; O-C(=O)-R¹⁴; O-C(=O)-N(H)R¹³; O-C(=O)-N(H)R¹⁴; OC(O)-N(R¹³)₂; O-C(=O)-N(R¹⁴)₂; O-C(=O)-N(R¹³)(R¹⁴); O-C(=O)-N(Rᵃ)(Rᵇ); NH₂; N(H)R¹³; N(R¹³)₂; N(H)R¹⁴; N(R¹⁴)₂; N(R¹³)(R¹⁴); N(Rᵃ)(Rᵇ); NH-C(=O)R¹⁴; NH-C(=O)-R¹³; N(R¹³)C(=O)-R¹³; N(R¹³)C(=O)-R¹⁴; NH-S(=O)₂-R¹³; N(R¹³)S(=O)₂-R¹³; NHS(=O)₂-R¹⁴; N(R¹³)-S(=O)₂-R¹⁴; N(H)C(=O)-OR¹³; N(H)-C(=O)-OR¹⁴; N(R¹³)-C(=O)-OR¹³; N(R¹³)C(=O)OR¹⁴; N(H)C(=O)-NH₂; N(H)C(=O)-N(H)R¹³; N(H)-C(=O)-N(H)R¹⁴; N(H)C(=O)-N(R¹³)₂; N(H)-C(=O)-N(R¹⁴)₂; N(H)-C(=O)-N(R¹³)(R¹⁴); N(H)-C(=O)N(Rᵃ)(Rᵇ); N(R¹³)-C(=O)-NH₂; N(R¹³)-C(=O)-N(H)R¹³; N(R¹³)-C(=O)-N(H)R¹⁴; N(R¹³)-C(=O)-N(R¹³)₂; N(R¹³)-C(=O)-N(R¹⁴)₂; N(R¹³)-C(=O)-N(R¹³)(R¹⁴); N(R¹³)-C(=O)-N(Rᵃ)(Rᵇ); SH; S-R¹³; SCF₃; S-R¹⁴; S(=O)₂OH; S(=O)₂-R¹³; S(=O)₂-R¹⁴; S(=O)-R¹³; S(=O)-R¹⁴; S(=O)₂-OR¹³; S(=O)₂-OR¹⁴; S(=O)₂-N(H)(R¹³); S(=O)₂-N(R¹³)₂; S(=O)₂-N(H)(R¹⁴); S(=O)₂-N(R¹³)(R¹⁴); S(=O)₂-N(Rᵃ)(Rᵇ); n representa 0 ó 1, donde, si n representa 1, luego J representa C-R⁸ o N o N⁺-O⁻, K representa C-R⁹ o N o N⁺-O⁻, M representa C-R¹⁰ o N o N⁺-O⁻, Q representa C-R¹¹ o N o N⁺-O⁻, y R representa C-R¹² o N o N⁺-O⁻, con la condición de que 0, 1, 2 ó 3 de las variables J, K, M, Q y R en forma independiente entre sí representan N o N⁺-O⁻, donde 0 ó 1 de las variables J, K, M, Q y R en forma independiente representa N⁺-O⁻, donde, si n representa 0, entonces J representa C-R⁸ o N o N⁺-O⁻ ó O ó S o NH o N(residuo alifático C₁₋₄), K representa C-R⁹ o N o N⁺-O⁻ ó O ó S o NH o N(residuo alifático C₁₋₄), M representa C-R¹⁰ o N o N⁺-O⁻ ó O ó S o NH o N(residuo alifático C₁₋₄) y Q representa C-R¹¹ o N o N⁺-O⁻ ó O ó S o NH o N(residuo alifático C₁₋₄), con la condición de que uno de J, K, M y Q representa O ó S o NH o N(residuo alifático C₁₋₄) y los restantes de J, K, M y Q en forma independiente representan C-R⁸, respectivamente C-R⁹, respectivamente C- R¹⁰, respectivamente C-R o N o N⁺-O⁻ y con la condición de que 0, 1, 2 ó 3 de J, K, M y Q en forma independiente entre sí representan N o N⁺-O⁻, donde 0 ó 1 de las variables J, K, M y Q representa N⁺-O⁻, donde R⁸, R⁹, R¹⁰, R¹¹ y R¹² se seleccionan en forma independiente entre sí entre el grupo que consiste en H; F; Cl; Br; I; NO₂; CN; CF₃ CF₂H; CFH₂ CF₂Cl; CFCl₂; R¹³; R¹⁴; C(=O)OH; C(=O)-R¹³; C(=O)R¹⁴; C(=O)-OR¹³; C(=O)-OR¹⁴; C(=O)-N(H)(OH); C(=N-OH)-H; C(=N-OH)-R¹³; C(=NOH)-R¹⁴; C(=N-O-R¹³)-H; C(=N-O-R¹³)-R¹³; C(=N-O-R¹³)-R¹⁴; C(=O)NH₂; C(=O)-N(H)R¹³; C(=O)-N(R¹³)₂; C(=O)-N(H)R¹⁴; C(=O)-N(R¹⁴)₂; C(=O)-N(R¹³)(R¹⁴); C(=O)-N(Rᵃ)(Rᵇ); OH; OR¹³; OCF₃; OCF₂H; OCFH₂ OCF₂Cl; OCFCl₂; OR¹⁴; OC(=O)R¹³; O-C(=O)R¹⁴; O-C(=O)-N(H)R¹³; O-C(=O)-N(H)R¹⁴; OC(=O)-N(R¹³)₂; OC(=O)-N(R¹⁴)₂; O-C(=O)-N(R¹³)(R¹⁴); O-C(=O)-N(Rᵃ)(Rᵇ); NH₂; N(H)R¹³; N(R¹³)₂; N(H)R¹⁴; N(R¹⁴)₂; N(R¹³)(R¹⁴); N(Rᵃ)(Rᵇ); NH-C(=O)-R¹⁴; NH-C(=O)-R¹³; N(R¹³)-C(=O)-R¹³; N(R¹³)-C(=O)-R¹⁴; NH-S(=O)₂-R¹³; N(R¹³)-S(=O)₂-R¹³; NH-S(=O)₂-R¹⁴; N(R¹³)-S(=O)₂-R¹⁴; N(H)-C(=O)OR¹³; N(H)-C(=O)-OR¹⁴; N(R¹³)-C(=O)-OR¹³; N(R¹³)-C(=O)-OR¹⁴; N(H)-C(=O)-NH₂; N(H)C(=O)-N(H)R¹³; N(H)-C(=O)N(H)R¹⁴; N(H)-C(=O)-N(R¹³)₂; N(H)-C(=O)-N(R¹⁴)₂; N(H)-C(=O)-N(R¹³)(R¹⁴); N(H)-C(=O)-N(Rᵃ)(Rᵇ); N(R¹³)-C(=O)-NH₂; N(R¹³)-C(=O)-N(H)R¹³, N(R¹³)-C(=O)-N(H)R¹⁴; N(R¹³)-C(=O)-N(R¹³)₂; N(R¹³)-C(=O)-N(R¹⁴)₂; N(R¹³)-C(=O)-N(R¹³)(R¹⁴); N(R¹³)-C(=O)-N(Rᵃ)(Rᵇ); SH; S-R¹³; SCF₃; SR¹⁴; S(=O)OH; S(=O)₂-R¹³; S(=O)₂-R¹⁴; S(=O)-R¹³; S(=O)R¹⁴; S(=O)₂-OR¹³; S(=O)₂-OR¹⁴; S(=O)₂-N(H)(R¹³); S(=O)₂-N(R¹³)₂; S(=O)₂-N(H)(R¹⁴); S(=O)₂-N(R¹³)(R¹⁴); S(=O)₂-N(Rᵃ)(Rᵇ); con la condición de que al menos uno de R⁸, R⁹, R¹⁰, R¹¹ y R¹² no denota H; cada R¹³ en forma independiente en cada caso denota residuo alifático C₁₋₈, no sustituido o monosustituido o polisustituido; o residuo cicloalifático C₃₋₆ o residuo heterocicloalifático de entre 3 y 7 miembros, en cada caso no sustituido o monosustituido o polisustituido; o residuo cicloalifático C₃₋₆ o residuo heterocicloalifático de entre 3 y 7 miembros, en cada caso no sustituido o monosustituido o polisustituido, y en cada caso conectado a través de un residuo alifático C₁₋₄, no sustituido o monosustituido o polisustituido; cada R¹⁴ en forma independiente en cada caso denota residuo arilo y heteroarilo, en cada caso en forma independiente entre sí no sustituido o monosustituido o polisustituido, o residuo arilo y heteroarilo, en cada caso en forma independiente entre sí no sustituido o monosustituido o polisustituido y en cada caso conectado a través de un grupo alifático C₁₋₄, no sustituido o monosustituido o polisustituido; Rᵃ y Rᵇ junto con el átomo de N que los conecta forman un residuo heterocíclico de entre 3 y 7 miembros, no sustituido o monosustituido o polisustituido; opcionalmente en forma de un único estereoisómero o una mezcla de estereoisómeros, en forma del compuesto libre y/o una sal fisiológicamente aceptable del mismo y/o un solvato fisiológicamente aceptable del mismo.
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| US (1) | US9206136B2 (es) |
| EP (1) | EP2943196A1 (es) |
| JP (1) | JP2016508152A (es) |
| KR (1) | KR20150103751A (es) |
| CN (1) | CN104994851A (es) |
| AR (1) | AR094412A1 (es) |
| AU (1) | AU2014204978A1 (es) |
| BR (1) | BR112015016391A2 (es) |
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| TWI795381B (zh) | 2016-12-21 | 2023-03-11 | 比利時商健生藥品公司 | 作為malt1抑制劑之吡唑衍生物 |
| WO2019081485A1 (de) | 2017-10-26 | 2019-05-02 | Bayer Cropscience Aktiengesellschaft | Substituierte pyrazole sowie deren salze und ihre verwendung als herbizide wirkstoffe |
| WO2019081477A1 (de) | 2017-10-26 | 2019-05-02 | Bayer Cropscience Aktiengesellschaft | Substituierte pyrazole sowie deren salze und ihre verwendung als herbizide wirkstoffe |
| CA3112907A1 (en) | 2018-09-14 | 2020-03-19 | Rhizen Pharmaceuticals Ag | Compositions comprising a crac inhibitor and a corticosteroid and methods of use thereof |
| EP3953345B1 (en) | 2019-04-11 | 2023-04-05 | Janssen Pharmaceutica NV | Pyridine rings containing derivatives as malt1 inhibitors |
| EP4243813A4 (en) * | 2020-11-13 | 2024-07-17 | Calcimedica, Inc. | IMPROVED SYNTHESIS OF CRAC CHANNEL INHIBITORS |
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| AU751139B2 (en) | 1997-10-13 | 2002-08-08 | Astellas Pharma Inc. | Amide derivative |
| MXPA01008142A (es) | 1999-02-10 | 2003-07-21 | Welfide Corp | Compuestos de amida, y uso medicinal de los mismos. |
| WO2001021160A2 (en) | 1999-09-23 | 2001-03-29 | Axxima Pharmaceuticals Aktiengesellschaft | Carboxymide and aniline derivatives as selective inhibitors of pathogens |
| US8084467B2 (en) | 1999-10-18 | 2011-12-27 | University Of Connecticut | Pyrazole derivatives as cannabinoid receptor antagonists |
| WO2003035602A1 (en) | 2001-10-25 | 2003-05-01 | Sankyo Company, Limited | Lipid modulators |
| ES2338539T3 (es) | 2001-11-01 | 2010-05-10 | Icagen, Inc. | Pirazolamidas para uso en el tratamiento del dolor. |
| CA2533598C (en) | 2003-07-23 | 2012-09-11 | Synta Pharmaceuticals, Corp. | Method for modulating calcium ion-release-activated calcium ion channels |
| WO2005016877A2 (en) | 2003-08-07 | 2005-02-24 | Merck & Co., Inc. | Pyrazole carboxamides as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1 |
| AT7990U1 (de) | 2004-12-22 | 2005-12-15 | Gottfried Steiner Ingenieurbue | Spritzgussform |
| AU2006205220B2 (en) | 2005-01-10 | 2012-09-13 | Exelixis, Inc. | Heterocyclic carboxamide compounds as steroid nuclear receptors ligands |
| ES2525217T3 (es) | 2005-06-27 | 2014-12-19 | Exelixis Patent Company Llc | Moduladores de LXR basados en imidazol |
| WO2007024744A2 (en) | 2005-08-21 | 2007-03-01 | Exelixis, Inc. | Heterocyclic carboxamide compounds as steroid nuclear receptor ligands |
| US7947707B2 (en) | 2005-10-07 | 2011-05-24 | Kissei Pharmaceutical Co., Ltd. | Nitrogenated heterocyclic compound and pharmaceutical composition comprising the same |
| WO2007087427A2 (en) | 2006-01-25 | 2007-08-02 | Synta Pharmaceuticals Corp. | Thiazole and thiadiazole compounds for inflammation and immune-related uses |
| WO2007087441A2 (en) | 2006-01-25 | 2007-08-02 | Synta Pharmaceuticals Corp. | Substituted aromatic compounds for inflammation and immune-related uses |
| US20090069288A1 (en) | 2007-07-16 | 2009-03-12 | Breinlinger Eric C | Novel therapeutic compounds |
| AU2008276063B2 (en) | 2007-07-17 | 2013-11-28 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| UA103006C2 (ru) | 2007-08-27 | 2013-09-10 | Басф Се | Пиразольные соединения для борьбы с бесхребетными вредителями |
| PT2212283E (pt) | 2007-10-17 | 2011-11-03 | Sanofi Sa | Carboxamidas de n-fenil-bipirrolidina substituídas e sua utilização terapêutica |
| WO2009076454A2 (en) | 2007-12-12 | 2009-06-18 | Calcimedica, Inc. | Compounds that modulate intracellular calcium |
| EP2240029A4 (en) | 2008-01-07 | 2012-08-22 | Synta Pharmaceuticals Corp | COMPOUNDS FOR USE AGAINST INFLAMMATORY AND IMMUNOMIC DISEASES |
| GB0813042D0 (en) | 2008-07-16 | 2008-08-20 | Syngenta Participations Ag | Insecticidal compounds |
| EP2350084B1 (en) | 2008-10-17 | 2015-06-24 | Boehringer Ingelheim International GmbH | Tetra-aza-heterocycles as phosphatidylinositol-3-kinases (pi3-kinases) inhibitor |
| AR076373A1 (es) * | 2009-04-24 | 2011-06-08 | Glaxo Group Ltd | N-pirazolil carboxamidas como inhibidores de canales de calcio |
| US8377970B2 (en) | 2009-10-08 | 2013-02-19 | Rhizen Pharmaceuticals Sa | Modulators of calcium release-activated calcium channel |
| CA2826059A1 (en) | 2011-02-09 | 2012-08-16 | Pierre Joseph Marcel Jung | Insecticidal compounds |
| JP5976778B2 (ja) | 2011-04-11 | 2016-08-24 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | キナーゼ阻害剤としてのピラゾリル−ピリミジン誘導体 |
| EP2532661A1 (en) | 2011-06-10 | 2012-12-12 | Syngenta Participations AG | Novel insecticides |
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- 2014-01-10 AR ARP140100092A patent/AR094412A1/es unknown
- 2014-01-10 CN CN201480004373.4A patent/CN104994851A/zh active Pending
- 2014-01-10 KR KR1020157021496A patent/KR20150103751A/ko not_active Withdrawn
- 2014-01-10 CA CA2897562A patent/CA2897562A1/en not_active Abandoned
- 2014-01-10 EP EP14701466.6A patent/EP2943196A1/en not_active Withdrawn
- 2014-01-10 EA EA201500736A patent/EA201500736A1/ru unknown
- 2014-01-10 AU AU2014204978A patent/AU2014204978A1/en not_active Abandoned
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- 2014-01-10 WO PCT/EP2014/000043 patent/WO2014108337A1/en not_active Ceased
- 2014-01-10 JP JP2015552030A patent/JP2016508152A/ja active Pending
- 2014-01-10 BR BR112015016391A patent/BR112015016391A2/pt not_active IP Right Cessation
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Also Published As
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| IL239790A0 (en) | 2015-08-31 |
| US9206136B2 (en) | 2015-12-08 |
| HK1216300A1 (zh) | 2016-11-04 |
| CN104994851A (zh) | 2015-10-21 |
| AU2014204978A1 (en) | 2015-08-20 |
| US20140194443A1 (en) | 2014-07-10 |
| KR20150103751A (ko) | 2015-09-11 |
| EP2943196A1 (en) | 2015-11-18 |
| WO2014108337A1 (en) | 2014-07-17 |
| BR112015016391A2 (pt) | 2017-07-11 |
| CA2897562A1 (en) | 2014-07-17 |
| EA201500736A1 (ru) | 2016-04-29 |
| JP2016508152A (ja) | 2016-03-17 |
| WO2014108337A8 (en) | 2015-07-23 |
| MX2015008919A (es) | 2015-10-22 |
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