RU2742938C2 - 4,6-ЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]ПИРАЗИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ - Google Patents
4,6-ЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]ПИРАЗИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ Download PDFInfo
- Publication number
- RU2742938C2 RU2742938C2 RU2017123387A RU2017123387A RU2742938C2 RU 2742938 C2 RU2742938 C2 RU 2742938C2 RU 2017123387 A RU2017123387 A RU 2017123387A RU 2017123387 A RU2017123387 A RU 2017123387A RU 2742938 C2 RU2742938 C2 RU 2742938C2
- Authority
- RU
- Russia
- Prior art keywords
- pyrazol
- pyrazolo
- pyrazin
- alkyl
- pentan
- Prior art date
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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
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- A—HUMAN NECESSITIES
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
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- 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
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- A61P31/04—Antibacterial agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
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- 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
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- 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
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Neurosurgery (AREA)
- Obesity (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pulmonology (AREA)
- Molecular Biology (AREA)
- Ophthalmology & Optometry (AREA)
- Child & Adolescent Psychology (AREA)
- Transplantation (AREA)
- Psychiatry (AREA)
- Biochemistry (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462088068P | 2014-12-05 | 2014-12-05 | |
| US62/088,068 | 2014-12-05 | ||
| PCT/US2015/064062 WO2016090285A1 (en) | 2014-12-05 | 2015-12-04 | 4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2021102805A Division RU2021102805A (ru) | 2014-12-05 | 2015-12-04 | 4,6-ЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]ПИРАЗИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| RU2017123387A RU2017123387A (ru) | 2019-01-11 |
| RU2017123387A3 RU2017123387A3 (OSRAM) | 2019-06-03 |
| RU2742938C2 true RU2742938C2 (ru) | 2021-02-11 |
Family
ID=55069089
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2021102805A RU2021102805A (ru) | 2014-12-05 | 2015-12-04 | 4,6-ЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]ПИРАЗИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ |
| RU2017123387A RU2742938C2 (ru) | 2014-12-05 | 2015-12-04 | 4,6-ЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]ПИРАЗИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2021102805A RU2021102805A (ru) | 2014-12-05 | 2015-12-04 | 4,6-ЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]ПИРАЗИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ |
Country Status (29)
| Country | Link |
|---|---|
| US (3) | US10189845B2 (OSRAM) |
| EP (2) | EP3227297B1 (OSRAM) |
| JP (2) | JP6641373B2 (OSRAM) |
| KR (1) | KR20170090476A (OSRAM) |
| CN (1) | CN107278203B (OSRAM) |
| AU (1) | AU2015357585B2 (OSRAM) |
| BR (1) | BR112017011798A2 (OSRAM) |
| CA (1) | CA2969709A1 (OSRAM) |
| CL (1) | CL2017001422A1 (OSRAM) |
| CO (1) | CO2017006674A2 (OSRAM) |
| CR (1) | CR20170309A (OSRAM) |
| DK (1) | DK3227297T3 (OSRAM) |
| ES (1) | ES2865483T3 (OSRAM) |
| HR (1) | HRP20210501T1 (OSRAM) |
| HU (1) | HUE054371T2 (OSRAM) |
| IL (1) | IL252656A0 (OSRAM) |
| MX (1) | MX386316B (OSRAM) |
| MY (1) | MY191016A (OSRAM) |
| PH (1) | PH12017501032A1 (OSRAM) |
| PL (1) | PL3227297T3 (OSRAM) |
| PT (1) | PT3227297T (OSRAM) |
| RS (1) | RS61693B1 (OSRAM) |
| RU (2) | RU2021102805A (OSRAM) |
| SG (1) | SG11201704542SA (OSRAM) |
| SI (1) | SI3227297T1 (OSRAM) |
| TW (1) | TWI725004B (OSRAM) |
| UA (1) | UA120065C2 (OSRAM) |
| WO (1) | WO2016090285A1 (OSRAM) |
| ZA (1) | ZA201704494B (OSRAM) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE054371T2 (hu) | 2014-12-05 | 2021-09-28 | Array Biopharma Inc | 4,6-szubsztituált pirazolo[l,5-A]pirazinok mint janus kináz inhibitorok |
| AU2017222417B2 (en) | 2016-02-24 | 2020-07-09 | Pfizer Inc. | Pyrazolo[1,5-a]pyrazin-4-yl derivatives as JAK-inhibitors |
| US11028080B2 (en) | 2016-03-11 | 2021-06-08 | Denali Therapeutics Inc. | Substituted pyrimidines as LRKK2 inhibitors |
| KR102705724B1 (ko) | 2016-06-16 | 2024-09-12 | 데날리 테라퓨틱스 인크. | 신경퇴행성 장애의 치료에서 사용하기 위한 lrrk2 저해제로서 피리미딘-2-일아미노-1h-피라졸 |
| GB201617758D0 (en) * | 2016-10-20 | 2016-12-07 | Almac Discovery Limited | Pharmaceutical compounds |
| EP3571203B1 (en) | 2017-01-18 | 2023-06-07 | Array BioPharma Inc. | Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors |
| WO2018217946A1 (en) * | 2017-05-24 | 2018-11-29 | Denali Therapeutics Inc. | Compounds, compositions and methods |
| EP3668858A1 (en) | 2017-08-14 | 2020-06-24 | Pfizer Inc | Pyrazolo[1,5-a]pyrazin-4-yl and related derivatives |
| EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| CA3087578C (en) | 2018-01-18 | 2023-08-08 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| CN111615514B (zh) | 2018-01-18 | 2022-10-11 | 奥瑞生物药品公司 | 作为ret激酶抑制剂的取代的吡唑并[4,3-c]吡啶化合物 |
| JP2022500383A (ja) | 2018-09-10 | 2022-01-04 | アレイ バイオファーマ インコーポレイテッド | Retキナーゼ阻害剤としての縮合複素環式化合物 |
| MX2021012487A (es) * | 2019-04-12 | 2021-11-12 | Primegene Beijing Co Ltd | Compuestos derivados de pirazolopirazina, composicion farmaceutica y uso de la misma. |
| IL322315A (en) | 2019-05-14 | 2025-09-01 | Provention Bio Inc | Methods and preparations for preventing type 1 diabetes |
| CN113150012B (zh) * | 2020-01-22 | 2023-03-24 | 浙江海正药业股份有限公司 | 吡唑并[1,5-a]吡嗪类衍生物及其制备方法和用途 |
| CN115715194A (zh) | 2020-04-04 | 2023-02-24 | 辉瑞公司 | 治疗冠状病毒疾病2019的方法 |
| MX2022015872A (es) | 2020-06-11 | 2023-05-16 | Provention Bio Inc | Metodos y composiciones para prevenir diabetes tipo 1. |
| CA3237632A1 (en) * | 2021-11-12 | 2023-05-19 | Changqing WEI | 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 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011120146A1 (en) * | 2010-04-01 | 2011-10-06 | Smart Technologies Ulc | Input system with anti-reflective bezel for locating active pointers |
| EA201201143A1 (ru) * | 2010-02-18 | 2013-03-29 | Альмираль, С.А. | Производные пиразола в качестве ингибиторов jak |
| WO2013055645A1 (en) * | 2011-10-12 | 2013-04-18 | Array Biopharma Inc. | 5,7-substituted-imidazo[1,2-c]pyrimidines |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1105378B1 (en) | 1998-08-21 | 2005-03-30 | Parker Hughes Institute | Quinazoline derivatives |
| DE102007032349A1 (de) * | 2007-07-11 | 2009-01-15 | Bayer Healthcare Ag | Imidazo-, Pyrazolopyrazine und Imidazotriazine und ihre Verwendung |
| US8440689B2 (en) | 2009-12-23 | 2013-05-14 | Takeda Pharmaceutical Company Limited | Fused heteroaromatic pyrrolidinones |
| CA2787714C (en) * | 2010-01-22 | 2019-04-09 | Joaquin Pastor Fernandez | Inhibitors of pi3 kinase |
| UA109131C2 (ru) * | 2010-04-14 | 2015-07-27 | Еррей Біофарма Інк. | 5,7-ЗАМЕЩЕННЫЕ ИМИДАЗО[1,2-c]ПИРИМИДИНЫ КАК ИНГИБИТОРЫ JAK-КИНАЗ |
| KR102070567B1 (ko) * | 2012-03-28 | 2020-01-29 | 메르크 파텐트 게엠베하 | 바이시클릭 피라지논 유도체 |
| HUE054371T2 (hu) | 2014-12-05 | 2021-09-28 | Array Biopharma Inc | 4,6-szubsztituált pirazolo[l,5-A]pirazinok mint janus kináz inhibitorok |
-
2015
- 2015-12-04 HU HUE15819933A patent/HUE054371T2/hu unknown
- 2015-12-04 RU RU2021102805A patent/RU2021102805A/ru unknown
- 2015-12-04 SI SI201531544T patent/SI3227297T1/sl unknown
- 2015-12-04 CA CA2969709A patent/CA2969709A1/en not_active Abandoned
- 2015-12-04 EP EP15819933.1A patent/EP3227297B1/en active Active
- 2015-12-04 TW TW104140878A patent/TWI725004B/zh not_active IP Right Cessation
- 2015-12-04 UA UAA201707008A patent/UA120065C2/uk unknown
- 2015-12-04 HR HRP20210501TT patent/HRP20210501T1/hr unknown
- 2015-12-04 CN CN201580066136.5A patent/CN107278203B/zh not_active Expired - Fee Related
- 2015-12-04 US US15/532,937 patent/US10189845B2/en active Active
- 2015-12-04 RS RS20210415A patent/RS61693B1/sr unknown
- 2015-12-04 CR CR20170309A patent/CR20170309A/es unknown
- 2015-12-04 WO PCT/US2015/064062 patent/WO2016090285A1/en not_active Ceased
- 2015-12-04 AU AU2015357585A patent/AU2015357585B2/en not_active Ceased
- 2015-12-04 BR BR112017011798A patent/BR112017011798A2/pt not_active IP Right Cessation
- 2015-12-04 RU RU2017123387A patent/RU2742938C2/ru active
- 2015-12-04 DK DK15819933.1T patent/DK3227297T3/da active
- 2015-12-04 SG SG11201704542SA patent/SG11201704542SA/en unknown
- 2015-12-04 MX MX2017007284A patent/MX386316B/es unknown
- 2015-12-04 KR KR1020177018122A patent/KR20170090476A/ko not_active Withdrawn
- 2015-12-04 PL PL15819933T patent/PL3227297T3/pl unknown
- 2015-12-04 ES ES15819933T patent/ES2865483T3/es active Active
- 2015-12-04 PT PT158199331T patent/PT3227297T/pt unknown
- 2015-12-04 EP EP21152373.3A patent/EP3878451A1/en not_active Withdrawn
- 2015-12-04 MY MYPI2017702034A patent/MY191016A/en unknown
- 2015-12-04 JP JP2017529681A patent/JP6641373B2/ja not_active Expired - Fee Related
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2017
- 2017-06-02 PH PH12017501032A patent/PH12017501032A1/en unknown
- 2017-06-04 IL IL252656A patent/IL252656A0/en active IP Right Grant
- 2017-06-05 CL CL2017001422A patent/CL2017001422A1/es unknown
- 2017-06-30 CO CONC2017/0006674A patent/CO2017006674A2/es unknown
- 2017-07-03 ZA ZA2017/04494A patent/ZA201704494B/en unknown
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2018
- 2018-12-06 US US16/212,493 patent/US10730880B2/en active Active
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2019
- 2019-12-11 JP JP2019223760A patent/JP2020055859A/ja active Pending
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2020
- 2020-06-02 US US16/890,663 patent/US11028093B2/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA201201143A1 (ru) * | 2010-02-18 | 2013-03-29 | Альмираль, С.А. | Производные пиразола в качестве ингибиторов jak |
| WO2011120146A1 (en) * | 2010-04-01 | 2011-10-06 | Smart Technologies Ulc | Input system with anti-reflective bezel for locating active pointers |
| WO2013055645A1 (en) * | 2011-10-12 | 2013-04-18 | Array Biopharma Inc. | 5,7-substituted-imidazo[1,2-c]pyrimidines |
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