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

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Publication number
SG11201704542SA
SG11201704542SA SG11201704542SA SG11201704542SA SG11201704542SA SG 11201704542S A SG11201704542S A SG 11201704542SA SG 11201704542S A SG11201704542S A SG 11201704542SA SG 11201704542S A SG11201704542S A SG 11201704542SA SG 11201704542S A SG11201704542S A SG 11201704542SA
Authority
SG
Singapore
Prior art keywords
pyrazines
pyrazolo
substituted
kinase inhibitors
janus kinase
Prior art date
Application number
SG11201704542SA
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.)
Filing date
Publication date
Application filed by Array Biopharma Inc, Celgene Corp filed Critical Array Biopharma Inc
Publication of SG11201704542SA publication Critical patent/SG11201704542SA/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic 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
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)

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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 (en)
EP (2) EP3878451A1 (en)
JP (2) JP6641373B2 (en)
KR (1) KR20170090476A (en)
CN (1) CN107278203B (en)
AU (1) AU2015357585B2 (en)
BR (1) BR112017011798A2 (en)
CA (1) CA2969709A1 (en)
CL (1) CL2017001422A1 (en)
CO (1) CO2017006674A2 (en)
CR (1) CR20170309A (en)
DK (1) DK3227297T3 (en)
ES (1) ES2865483T3 (en)
HR (1) HRP20210501T1 (en)
HU (1) HUE054371T2 (en)
IL (1) IL252656A0 (en)
MX (1) MX2017007284A (en)
MY (1) MY191016A (en)
PH (1) PH12017501032A1 (en)
PL (1) PL3227297T3 (en)
PT (1) PT3227297T (en)
RS (1) RS61693B1 (en)
RU (2) RU2021102805A (en)
SG (1) SG11201704542SA (en)
SI (1) SI3227297T1 (en)
TW (1) TWI725004B (en)
UA (1) UA120065C2 (en)
WO (1) WO2016090285A1 (en)
ZA (1) ZA201704494B (en)

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Publication number Priority date Publication date Assignee Title
WO2017156493A1 (en) 2016-03-11 2017-09-14 Denali Therapeutics Inc. Compounds, compositions, and methods
SG11201704542SA (en) 2014-12-05 2017-07-28 Array Biopharma Inc 4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS
EP3712153B1 (en) * 2016-02-24 2021-12-01 Pfizer Inc. Pyrazolo[1,5-a]pyrazin-4-yl derivatives as jak-inhibitors
RS62868B1 (en) 2016-06-16 2022-02-28 Denali Therapeutics Inc Pyrimidin-2-ylamino-1h-pyrazols as lrrk2 inhibitors for use in the treatment of neurodegenerative disorders
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
US11254668B2 (en) 2017-08-14 2022-02-22 Pfizer Inc. Pyrazolo[1,5-A]pyrazin-4-yl and related derivatives
US11472802B2 (en) 2018-01-18 2022-10-18 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors
JP7061195B2 (en) 2018-01-18 2022-04-27 アレイ バイオファーマ インコーポレイテッド Substituted pyrazolo [3,4-d] pyrimidine compound as a RET kinase inhibitor
CN111971286B (en) 2018-01-18 2023-04-14 阿雷生物药品公司 Substituted pyrrolo [2,3-d ] pyrimidine compounds as RET kinase inhibitors
WO2020055672A1 (en) 2018-09-10 2020-03-19 Array Biopharma Inc. Fused heterocyclic compounds as ret kinase inhibitors
EP3954689B1 (en) * 2019-04-12 2024-04-24 Primegene (Beijing) Co., Ltd. Pyrazolopyrazine derived compounds, pharmaceutical composition and use thereof
JP7137696B2 (en) 2019-05-14 2022-09-14 プロヴェンション・バイオ・インコーポレイテッド Methods and compositions for preventing type 1 diabetes
CN113150012B (en) * 2020-01-22 2023-03-24 浙江海正药业股份有限公司 Pyrazolo [1,5-a ] pyrazine derivative and preparation method and application thereof
KR20220164008A (en) 2020-04-04 2022-12-12 화이자 인코포레이티드 how to treat coronavirus disease 2019
WO2023083200A1 (en) * 2021-11-12 2023-05-19 南京明德新药研发有限公司 Pyrazolo fused ring compound and use thereof

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US6313129B1 (en) 1998-08-21 2001-11-06 Hughes Institute Therapeutic compounds
DE102007032349A1 (en) 2007-07-11 2009-01-15 Bayer Healthcare Ag Imidazo, pyrazolopyrazines and imidazotriazines and their use
SI2516434T1 (en) 2009-12-23 2015-10-30 Takeda Pharmaceutical Company Limited Fused heteroaromatic pyrrolidinones as syk inhibitors
CA2787714C (en) * 2010-01-22 2019-04-09 Joaquin Pastor Fernandez Inhibitors of pi3 kinase
UY33213A (en) * 2010-02-18 2011-09-30 Almirall Sa PIRAZOL DERIVATIVES AS JAK INHIBITORS
US20110241987A1 (en) * 2010-04-01 2011-10-06 Smart Technologies Ulc Interactive input system and information input method therefor
AU2011240808B2 (en) * 2010-04-14 2015-01-22 Array Biopharma Inc. 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of JAK kinases
MX2014004473A (en) * 2011-10-12 2015-04-14 Array Biopharma Inc 5,7-substituted-imidazo[1,2-c]pyrimidines.
ES2585044T3 (en) * 2012-03-28 2016-10-03 Merck Patent Gmbh Bicyclic Pyrazinone Derivatives
SG11201704542SA (en) 2014-12-05 2017-07-28 Array Biopharma Inc 4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS

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AU2015357585B2 (en) 2020-07-02
US10730880B2 (en) 2020-08-04
DK3227297T3 (en) 2021-04-06
US10189845B2 (en) 2019-01-29
WO2016090285A1 (en) 2016-06-09
US20190177328A1 (en) 2019-06-13
EP3878451A1 (en) 2021-09-15
CR20170309A (en) 2018-02-02
PH12017501032A1 (en) 2017-11-27
HUE054371T2 (en) 2021-09-28
RU2017123387A (en) 2019-01-11
MX2017007284A (en) 2017-08-25
KR20170090476A (en) 2017-08-07
RU2017123387A3 (en) 2019-06-03
TWI725004B (en) 2021-04-21
JP6641373B2 (en) 2020-02-05
JP2020055859A (en) 2020-04-09
US11028093B2 (en) 2021-06-08
ES2865483T3 (en) 2021-10-15
US20200291039A1 (en) 2020-09-17
UA120065C2 (en) 2019-09-25
TW201632523A (en) 2016-09-16
SI3227297T1 (en) 2021-04-30
HRP20210501T1 (en) 2021-05-14
EP3227297B1 (en) 2021-01-20
EP3227297A1 (en) 2017-10-11
MY191016A (en) 2022-05-28
IL252656A0 (en) 2017-07-31
CO2017006674A2 (en) 2017-10-20
ZA201704494B (en) 2022-03-30
CN107278203B (en) 2020-05-19
AU2015357585A1 (en) 2017-07-13
CA2969709A1 (en) 2016-06-09
US20170362240A1 (en) 2017-12-21
JP2018507167A (en) 2018-03-15
PL3227297T3 (en) 2021-10-25
CN107278203A (en) 2017-10-20
PT3227297T (en) 2021-04-09
RU2742938C2 (en) 2021-02-11
CL2017001422A1 (en) 2018-01-05
BR112017011798A2 (en) 2017-12-26
RS61693B1 (en) 2021-05-31
RU2021102805A (en) 2021-02-12

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