SG11201704542SA - 4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS - Google Patents

4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS

Info

Publication number: SG11201704542SA
Authority: SG; Singapore
Prior art keywords: pyrazines; pyrazolo; substituted; kinase inhibitors; janus kinase
Prior art date: 2014-12-05

Application number

SG11201704542SA

Other languages

English (en)

Inventor

Shelley Allen

Mark Laurence Boys

Mark J Chicarelli

Jay Bradford Fell

John P Fischer

John Gaudino

Erik James Hicken

Ronald Jay Hinklin

Christopher F Kraser

Ellen Laird

John E Robinson

Tony P Tang

Laurence E Burgess

Robert Andrew Rieger

Jed Pheneger

Yoshitaka Satoh

Katerina Leftheris

Raj K Raheja

Brydon L Bennett

Original Assignee

Array Biopharma Inc

Celgene Corp

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2014-12-05

Filing date

2015-12-04

Publication date

2017-07-28

2015-12-04 Application filed by Array Biopharma Inc, Celgene Corp filed Critical Array Biopharma Inc

2017-07-28 Publication of SG11201704542SA publication Critical patent/SG11201704542SA/en

Classifications

- 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
- 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
- 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
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- 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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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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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- A—HUMAN NECESSITIES
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- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A—HUMAN NECESSITIES
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- A61P37/00—Drugs for immunological or allergic disorders
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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
- 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
- A61P37/08—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
- 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)
General Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Medicinal Chemistry (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
Animal Behavior & Ethology (AREA)
Pharmacology & Pharmacy (AREA)
Chemical Kinetics & Catalysis (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Epidemiology (AREA)
Immunology (AREA)
Diabetes (AREA)
Rheumatology (AREA)
Hematology (AREA)
Physical Education & Sports Medicine (AREA)
Pain & Pain Management (AREA)
Neurosurgery (AREA)
Obesity (AREA)
Neurology (AREA)
Biomedical Technology (AREA)
Orthopedic Medicine & Surgery (AREA)
Pulmonology (AREA)
Dermatology (AREA)
Molecular Biology (AREA)
Communicable Diseases (AREA)
Psychiatry (AREA)
Emergency Medicine (AREA)
Child & Adolescent Psychology (AREA)
Biochemistry (AREA)
Oncology (AREA)
Endocrinology (AREA)
Hospice & Palliative Care (AREA)
Transplantation (AREA)
Ophthalmology & Optometry (AREA)

SG11201704542SA 2014-12-05 2015-12-04 4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS SG11201704542SA (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US201462088068P	2014-12-05	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

Publications (1)

Publication Number	Publication Date
SG11201704542SA true SG11201704542SA (en)	2017-07-28

Family

ID=55069089

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
SG11201704542SA SG11201704542SA (en)	2014-12-05	2015-12-04	4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS

Country Status (29)

Country	Link
US (3)	US10189845B2 (da)
EP (2)	EP3878451A1 (da)
JP (2)	JP6641373B2 (da)
KR (1)	KR20170090476A (da)
CN (1)	CN107278203B (da)
AU (1)	AU2015357585B2 (da)
BR (1)	BR112017011798A2 (da)
CA (1)	CA2969709A1 (da)
CL (1)	CL2017001422A1 (da)
CO (1)	CO2017006674A2 (da)
CR (1)	CR20170309A (da)
DK (1)	DK3227297T3 (da)
ES (1)	ES2865483T3 (da)
HR (1)	HRP20210501T1 (da)
HU (1)	HUE054371T2 (da)
IL (1)	IL252656A0 (da)
MX (1)	MX386316B (da)
MY (1)	MY191016A (da)
PH (1)	PH12017501032A1 (da)
PL (1)	PL3227297T3 (da)
PT (1)	PT3227297T (da)
RS (1)	RS61693B1 (da)
RU (2)	RU2021102805A (da)
SG (1)	SG11201704542SA (da)
SI (1)	SI3227297T1 (da)
TW (1)	TWI725004B (da)
UA (1)	UA120065C2 (da)
WO (1)	WO2016090285A1 (da)
ZA (1)	ZA201704494B (da)

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DK3227297T3 (da)	2014-12-05	2021-04-06	Array Biopharma Inc	4,6-substitueret-pyrazolo[1,5-a]pyraziner som janus kinase-inhibitorer
DK3419978T3 (da) *	2016-02-24	2020-06-02	Pfizer	Pyrazolo[1,5-A]pyrazin-4-yl-derivater som JAK-hæmmere
US11028080B2 (en)	2016-03-11	2021-06-08	Denali Therapeutics Inc.	Substituted pyrimidines as LRKK2 inhibitors
CR20220182A (es)	2016-06-16	2022-06-15	Denali Therapeutics Inc	Pirimidin-2-ilamino-1h-pirazoles como inhibidores de lrrk2 para el uso en el tratamiento de trastornos neurodegenerativos (divisional 2018-592)
GB201617758D0 (en) *	2016-10-20	2016-12-07	Almac Discovery Limited	Pharmaceutical compounds
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
WO2018217946A1 (en) *	2017-05-24	2018-11-29	Denali Therapeutics Inc.	Compounds, compositions and methods
US11254668B2 (en)	2017-08-14	2022-02-22	Pfizer Inc.	Pyrazolo[1,5-A]pyrazin-4-yl and related derivatives
WO2019143977A1 (en)	2018-01-18	2019-07-25	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
EP3740486A1 (en)	2018-01-18	2020-11-25	Array Biopharma, Inc.	Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
EP3849986B1 (en)	2018-09-10	2022-06-08	Array Biopharma, Inc.	Fused heterocyclic compounds as ret kinase inhibitors
AU2020256720B2 (en) *	2019-04-12	2022-09-01	PrimeGene (Beijing) Co. Ltd.	Pyrazolopyrazine derived compounds, pharmaceutical composition and use thereof
JOP20210298A1 (ar)	2019-05-14	2023-01-30	Provention Bio Inc	طرق وتركيبات للوقاية من مرض السكري من النوع الأول
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
US20230149407A1 (en)	2020-04-04	2023-05-18	Pfizer Inc.	Methods of Treating Coronavirus Disease 2019
WO2021252917A2 (en)	2020-06-11	2021-12-16	Provention Bio, Inc.	Methods and compositions for preventing type 1 diabetes
CN118317960A (zh) *	2021-11-12	2024-07-09	海南康哲美丽科技有限公司	吡唑并环化合物及其应用
KR20260009361A (ko) *	2023-05-12	2026-01-19	씨엠에스 리서치 앤드 디벨롭먼트 피티이. 리미티드	피라졸로피라진 화합물 및 이의 결정형의 제조 방법

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IL141434A0 (en)	1998-08-21	2002-03-10	Parker Hughes Inst	Quinazoline derivatives
DE102007032349A1 (de) *	2007-07-11	2009-01-15	Bayer Healthcare Ag	Imidazo-, Pyrazolopyrazine und Imidazotriazine und ihre Verwendung
SI2516434T1 (sl) *	2009-12-23	2015-10-30	Takeda Pharmaceutical Company Limited	Zliti heteroaromatski pirolidinoni kot inhibitorji SYK
CA2787714C (en) *	2010-01-22	2019-04-09	Joaquin Pastor Fernandez	Inhibitors of pi3 kinase
UY33213A (es)	2010-02-18	2011-09-30	Almirall Sa	Derivados de pirazol como inhibidores de jak
US20110241987A1 (en) *	2010-04-01	2011-10-06	Smart Technologies Ulc	Interactive input system and information input method therefor
EP2558468B1 (en) *	2010-04-14	2015-04-01	Array Biopharma, Inc.	5, 7-substituted-imidazo [1,2-c] pyrimidines as inhibitors of jak kinases
JP2014528475A (ja) *	2011-10-12	2014-10-27	アレイバイオファーマ、インコーポレイテッド	５，７置換イミダゾ［１，２−ｃ］ピリミジン
JP6096879B2 (ja) *	2012-03-28	2017-03-15	メルクパテントゲゼルシャフトミットベシュレンクテルハフツングＭｅｒｃｋＰａｔｅｎｔＧｅｓｅｌｌｓｃｈａｆｔｍｉｔｂｅｓｃｈｒａｅｎｋｔｅｒＨａｆｔｕｎｇ	二環式ピラジノン誘導体
DK3227297T3 (da)	2014-12-05	2021-04-06	Array Biopharma Inc	4,6-substitueret-pyrazolo[1,5-a]pyraziner som janus kinase-inhibitorer

2015
- 2015-12-04 DK DK15819933.1T patent/DK3227297T3/da active
- 2015-12-04 MX MX2017007284A patent/MX386316B/es unknown
- 2015-12-04 SG SG11201704542SA patent/SG11201704542SA/en unknown
- 2015-12-04 HR HRP20210501TT patent/HRP20210501T1/hr unknown
- 2015-12-04 WO PCT/US2015/064062 patent/WO2016090285A1/en not_active Ceased
- 2015-12-04 PT PT158199331T patent/PT3227297T/pt unknown
- 2015-12-04 PL PL15819933T patent/PL3227297T3/pl unknown
- 2015-12-04 RU RU2021102805A patent/RU2021102805A/ru unknown
- 2015-12-04 CR CR20170309A patent/CR20170309A/es unknown
- 2015-12-04 RU RU2017123387A patent/RU2742938C2/ru active
- 2015-12-04 EP EP21152373.3A patent/EP3878451A1/en not_active Withdrawn
- 2015-12-04 AU AU2015357585A patent/AU2015357585B2/en not_active Ceased
- 2015-12-04 JP JP2017529681A patent/JP6641373B2/ja not_active Expired - Fee Related
- 2015-12-04 HU HUE15819933A patent/HUE054371T2/hu unknown
- 2015-12-04 MY MYPI2017702034A patent/MY191016A/en unknown
- 2015-12-04 ES ES15819933T patent/ES2865483T3/es active Active
- 2015-12-04 US US15/532,937 patent/US10189845B2/en active Active
- 2015-12-04 UA UAA201707008A patent/UA120065C2/uk unknown
- 2015-12-04 TW TW104140878A patent/TWI725004B/zh not_active IP Right Cessation
- 2015-12-04 KR KR1020177018122A patent/KR20170090476A/ko not_active Withdrawn
- 2015-12-04 EP EP15819933.1A patent/EP3227297B1/en active Active
- 2015-12-04 RS RS20210415A patent/RS61693B1/sr unknown
- 2015-12-04 SI SI201531544T patent/SI3227297T1/sl unknown
- 2015-12-04 CN CN201580066136.5A patent/CN107278203B/zh not_active Expired - Fee Related
- 2015-12-04 BR BR112017011798A patent/BR112017011798A2/pt not_active IP Right Cessation
- 2015-12-04 CA CA2969709A patent/CA2969709A1/en not_active Abandoned
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
2018
- 2018-12-06 US US16/212,493 patent/US10730880B2/en active Active
2019
- 2019-12-11 JP JP2019223760A patent/JP2020055859A/ja active Pending
2020
- 2020-06-02 US US16/890,663 patent/US11028093B2/en active Active

Also Published As

Publication number	Publication date
RU2017123387A3 (da)	2019-06-03
MX2017007284A (es)	2017-08-25
IL252656A0 (en)	2017-07-31
MX386316B (es)	2025-03-18
WO2016090285A1 (en)	2016-06-09
TW201632523A (zh)	2016-09-16
BR112017011798A2 (pt)	2017-12-26
UA120065C2 (uk)	2019-09-25
CO2017006674A2 (es)	2017-10-20
US10730880B2 (en)	2020-08-04
US20170362240A1 (en)	2017-12-21
ZA201704494B (en)	2022-03-30
US10189845B2 (en)	2019-01-29
US20190177328A1 (en)	2019-06-13
RU2017123387A (ru)	2019-01-11
US11028093B2 (en)	2021-06-08
EP3878451A1 (en)	2021-09-15
JP2018507167A (ja)	2018-03-15
SI3227297T1 (sl)	2021-04-30
AU2015357585A1 (en)	2017-07-13
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DK3227297T3 (da)	2021-04-06
RU2021102805A (ru)	2021-02-12
CR20170309A (es)	2018-02-02
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US20200291039A1 (en)	2020-09-17
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AU2015357585B2 (en)	2020-07-02
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EP3227297A1 (en)	2017-10-11
PL3227297T3 (pl)	2021-10-25
PH12017501032A1 (en)	2017-11-27
CN107278203B (zh)	2020-05-19
JP2020055859A (ja)	2020-04-09
CN107278203A (zh)	2017-10-20
EP3227297B1 (en)	2021-01-20
RS61693B1 (sr)	2021-05-31
HRP20210501T1 (hr)	2021-05-14
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ES2865483T3 (es)	2021-10-15

Publication	Publication Date	Title
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IL277576A (en)	2020-11-30	Mutated pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors
IL265918B (en)	2021-01-31	Converted pyrazolo[1,5–a]pyridine compounds as ret kinase inhibitors
ZA201800771B (en)	2021-05-26	Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
ZA201901034B (en)	2021-06-30	Macrocycle kinase inhibitors
ZA201808431B (en)	2020-05-27	Pyrazolopyrimidine derivatives as kinase inhibitor
IL254224A0 (en)	2017-10-31	7-substituted 5-alkyl-[4,2,1]triazolo[5,1-a]pyrimidine derivatives as pde2 inhibitors
IL252053A0 (en)	2017-07-31	Substituted pyrazolo(1,5-a)pyrimidines and their use in the treatment of medical disorders
PL3305788T3 (pl)	2021-03-08	Inhibitor kinazy janusowej
EP3209296A4 (en)	2018-04-11	Ethyl n-boc piperidinyl pyrazolo pyridones as janus kinase inhibitors
IL290419B (en)	2022-10-01	Imidazo[a-1,5]pyrazine derivatives as inhibitors of pi3k delta
IL252986B (en)	2019-11-28	5,3-diaminopyrazole kinase inhibitors
HK1238236A1 (en)	2018-04-27	4,6-substituted-pyrazolo[1,5-a]pyrazines as janus kinase inhibitors
HK40009742A (en)	2020-06-26	Macrocycle kinase inhibitors
GB201613945D0 (en)	2016-09-28	Compounds useful as kinase inhibitors