AR107714A1 - Derivados de pirazolo[1,5-a]pirazin-4-ilo - Google Patents
Derivados de pirazolo[1,5-a]pirazin-4-iloInfo
- Publication number
- AR107714A1 AR107714A1 ARP170100462A ARP170100462A AR107714A1 AR 107714 A1 AR107714 A1 AR 107714A1 AR P170100462 A ARP170100462 A AR P170100462A AR P170100462 A ARP170100462 A AR P170100462A AR 107714 A1 AR107714 A1 AR 107714A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydroxy
- independently
- cycloalkyl
- halo
- Prior art date
Links
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 17
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 6
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000001475 halogen functional group Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- -1 cyano, hydroxy Chemical group 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 101100134925 Gallus gallus COR6 gene Proteins 0.000 abstract 1
- 229940122245 Janus kinase inhibitor Drugs 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
Classifications
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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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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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
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- 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
- 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
- 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
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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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
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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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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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
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Gastroenterology & Hepatology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Un compuesto que tiene la estructura de fórmula (1), o una sal de este aceptable desde el punto de vista farmacéutico, o un solvato aceptable desde el punto de vista farmacéutico de un compuesto o una sal aceptable desde el punto de vista farmacéutico, en donde A, A y A son independientemente O, C=O, C-R o N-R, en donde R y R pueden ser independientemente H, amino, -NR⁷COR⁶, COR⁶, -CONR⁷R⁸, C₁₋₆ alquilo o hidroxi(C₁₋₆ alquilo), y R puede estar presente o ausente, y está presente donde las reglas de valencia lo permiten, y en donde no más de uno de A, A y A es O ó C=O; R⁰ y R son independientemente H, Br, Cl, F o C₁₋₆ alquilo; R¹ es H, C₁₋₆ alquilo o hidroxi(C₁₋₆ alquilo); R² se selecciona del grupo que consiste en H, C₁₋₆ alquilo, C₁₋₆ alcoxi, hidroxi(C₁₋₆ alquilo), fenil(C₁₋₆ alquilo), formilo, heteroarilo, heterocíclico, -COR⁶, -OCOR⁶, -COOR⁶, -NR⁷COR⁶, -CONR⁷R⁸ y -(CH₂)ₙ-W, en donde W es ciano, hidroxi, C₃₋₈ cicloalquilo, -SO₂NR⁷R⁸ y -SO₂-R⁹, en donde R⁹ es C₁₋₆ alquilo, C₃₋₈ cicloalquilo, heteroarilo o heterocíclico; en donde cada uno de alquilo, cicloalquilo, heterocíclico o heteroarilo puede ser no sustituido o sustituido por halo, ciano, hidroxi o C₁₋₆ alquilo; X es C-R³ o N, en donde R³ puede ser H o C₁₋₆ alquilo; R⁴ y R⁵ son independientemente H, amino, C₁₋₆ alquilo o hidroxi(C₁₋₆ alquilo); R⁶, R⁷ y R⁸ son, cada uno independientemente, H, C₁₋₆ alquilo, C₁₋₄ alcoxi(C₁₋₆ alquilo) o C₃₋₈ cicloalquilo, dicho C₁₋₆ alquilo se sustituye opcionalmente con halo, CN o hidroxi; o R⁷ y R⁸, junto con el átomo unido a estos, forman un anillo de 5 ó 6 miembros, en donde el anillo se sustituye opcionalmente con halo, hidroxi, CN o C₁₋₆ alquilo; y n es 0, 1, 2 ó 3. También se proporcionan métodos de tratamiento tales como inhibidores de quinasas Janus y composiciones farmacéuticas que contienen los compuestos y combinaciones de estos con otros agentes terapéuticos.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201662299130P | 2016-02-24 | 2016-02-24 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR107714A1 true AR107714A1 (es) | 2018-05-23 |
Family
ID=58054385
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP170100462A AR107714A1 (es) | 2016-02-24 | 2017-02-23 | Derivados de pirazolo[1,5-a]pirazin-4-ilo |
Country Status (45)
Families Citing this family (22)
Publication number | Priority date | Publication date | Assignee | Title |
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DK3419978T3 (da) | 2016-02-24 | 2020-06-02 | Pfizer | Pyrazolo[1,5-A]pyrazin-4-yl-derivater som JAK-hæmmere |
WO2018119142A1 (en) | 2016-12-21 | 2018-06-28 | Amgen Inc. | Anti-tnf alpha antibody formulations |
AU2019227607C1 (en) | 2018-02-27 | 2023-07-20 | Incyte Corporation | Imidazopyrimidines and triazolopyrimidines as A2A / A2B inhibitors |
CA3090842A1 (en) | 2018-03-12 | 2019-09-19 | Abbvie Inc. | Inhibitors of tyrosine kinase 2 mediated signaling |
MX2020012201A (es) | 2018-05-17 | 2021-01-29 | Bayer Ag | Derivados sustituidos de la carboxamida dihidropirazolo pirazina. |
JP7391046B2 (ja) | 2018-05-18 | 2023-12-04 | インサイト・コーポレイション | A2a/a2b阻害剤としての縮合ピリミジン誘導体 |
SG11202013216RA (en) | 2018-07-05 | 2021-01-28 | Incyte Corp | Fused pyrazine derivatives as a2a / a2b inhibitors |
AR116592A1 (es) | 2018-10-17 | 2021-05-26 | Lilly Co Eli | Tratamiento de la colangitis biliar primaria y la colangitis esclerosante primaria con baricitinib |
TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
US20220204513A1 (en) * | 2019-04-12 | 2022-06-30 | Primegene (Beijing) Co., Ltd. | Pyrazolopyrazine derived compounds, pharmaceutical composition and use thereof |
IL287665A (en) | 2019-04-30 | 2022-07-01 | Celgene Corp | Combination therapies comprising apremilast and tyk2 inhibitors |
MX2022002995A (es) * | 2019-09-11 | 2022-06-02 | Pfizer | Tratamiento de hidradenitis con inhibidores de quinasa. |
WO2021124095A1 (en) * | 2019-12-18 | 2021-06-24 | Pfizer Inc. | Treatment of ulcerative colitis with kinase inhibitors |
US20230149407A1 (en) | 2020-04-04 | 2023-05-18 | Pfizer Inc. | Methods of Treating Coronavirus Disease 2019 |
EP4132931A1 (en) * | 2020-04-08 | 2023-02-15 | Pfizer Inc. | Crystalline forms of 3-cyano-1-[4-[6-(1-methyl-1h-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl]-1h-pyrazol-1-yl]cyclobutaneacetonitrile, and use thereof |
JP2023542298A (ja) * | 2020-09-11 | 2023-10-06 | プルモシム セラピューティクス リミテッド ライアビリティ カンパニー | 肺高血圧症を治療又は予防する組成物及び方法 |
CN112592345B (zh) * | 2020-12-07 | 2024-09-13 | 嘉兴特科罗生物科技有限公司 | 一种三氮唑并吡嗪类化合物及其用途 |
WO2022165530A1 (en) * | 2021-02-01 | 2022-08-04 | Janssen Biotech, Inc. | Small molecule inhibitors of salt inducible kinases |
CA3215278A1 (en) | 2021-03-30 | 2022-10-06 | Pfizer Inc. | Methods for treatment of vitiligo |
KR20240111312A (ko) | 2021-10-25 | 2024-07-16 | 카이메라 쎄라퓨틱스 인코포레이티드 | Tyk2 분해제 및 이의 용도 |
US20250011332A1 (en) * | 2021-11-12 | 2025-01-09 | Soter Biopharma Pte. Ltd. | Pyrazolo fused ring compound and use thereof |
WO2024235167A1 (zh) * | 2023-05-12 | 2024-11-21 | 海南康哲美丽科技有限公司 | 一种吡唑并吡嗪类化合物及其晶型的制备方法 |
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CN101679408B (zh) | 2006-12-22 | 2016-04-27 | Astex治疗学有限公司 | 作为fgfr抑制剂的双环杂环化合物 |
AR066879A1 (es) * | 2007-06-08 | 2009-09-16 | Novartis Ag | Derivados de quinoxalina como inhibidores de la actividad de cinasa de tirosina de las cinasas janus |
CL2008001709A1 (es) | 2007-06-13 | 2008-11-03 | Incyte Corp | Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras. |
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EP2832734A4 (en) * | 2012-03-28 | 2015-08-26 | Takeda Pharmaceutical | HETEROCYCLIC COMPOUND |
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GB201504565D0 (en) | 2015-03-18 | 2015-05-06 | Takeda Pharmaceutical | Novel compounds |
HUE044240T2 (hu) | 2015-04-29 | 2019-10-28 | Wuxi Fortune Pharmaceutical Co Ltd | Janus kináz (JAK) inhibitorok |
EP3394066A2 (en) | 2015-12-22 | 2018-10-31 | H. Hoffnabb-La Roche Ag | PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS |
DK3419978T3 (da) | 2016-02-24 | 2020-06-02 | Pfizer | Pyrazolo[1,5-A]pyrazin-4-yl-derivater som JAK-hæmmere |
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CN110267960B (zh) | 2017-01-18 | 2022-04-26 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡嗪化合物 |
WO2018234342A1 (en) | 2017-06-21 | 2018-12-27 | F. Hoffmann-La Roche Ag | ISOINDOLINONE DERIVATIVES AS MODULATORS OF IRAK4 |
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2017
- 2017-02-10 DK DK17705705.6T patent/DK3419978T3/da active
- 2017-02-10 JP JP2018544300A patent/JP6505956B2/ja active Active
- 2017-02-10 UA UAA201808148A patent/UA119835C2/uk unknown
- 2017-02-10 MD MDE20190031T patent/MD3419978T2/ro unknown
- 2017-02-10 GE GEAP201714864A patent/GEP20217242B/en unknown
- 2017-02-10 ME MEP-2020-97A patent/ME03743B/me unknown
- 2017-02-10 TN TNP/2018/000295A patent/TN2018000295A1/en unknown
- 2017-02-10 KR KR1020187024431A patent/KR102128671B1/ko active IP Right Grant
- 2017-02-10 MA MA052987A patent/MA52987A/fr unknown
- 2017-02-10 AU AU2017222417A patent/AU2017222417B2/en active Active
- 2017-02-10 MA MA43668A patent/MA43668B1/fr unknown
- 2017-02-10 SG SG11201806307YA patent/SG11201806307YA/en unknown
- 2017-02-10 RU RU2018130547A patent/RU2718902C2/ru active
- 2017-02-10 CO CONC2018/0008799A patent/CO2018008799A2/es unknown
- 2017-02-10 MY MYPI2018702937A patent/MY189118A/en unknown
- 2017-02-10 PL PL17705705T patent/PL3419978T3/pl unknown
- 2017-02-10 WO PCT/IB2017/050748 patent/WO2017144995A1/en active Application Filing
- 2017-02-10 MX MX2018010236A patent/MX2018010236A/es unknown
- 2017-02-10 CU CU2018000078A patent/CU24511B1/es unknown
- 2017-02-10 PT PT177057056T patent/PT3419978T/pt unknown
- 2017-02-10 HU HUE17705705A patent/HUE049305T2/hu unknown
- 2017-02-10 EA EA201891463A patent/EA035036B1/ru unknown
- 2017-02-10 SI SI201730289T patent/SI3419978T1/sl unknown
- 2017-02-10 NZ NZ744349A patent/NZ744349A/en unknown
- 2017-02-10 CR CR20180372A patent/CR20180372A/es unknown
- 2017-02-10 CN CN201780013165.4A patent/CN109071546B/zh active Active
- 2017-02-10 EP EP20168877.7A patent/EP3712153B1/en active Active
- 2017-02-10 RS RS20200584A patent/RS60261B1/sr unknown
- 2017-02-10 EP EP17705705.6A patent/EP3419978B1/en active Active
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