CA2969709A1 - 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 Download PDF

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Publication number
CA2969709A1
CA2969709A1 CA2969709A CA2969709A CA2969709A1 CA 2969709 A1 CA2969709 A1 CA 2969709A1 CA 2969709 A CA2969709 A CA 2969709A CA 2969709 A CA2969709 A CA 2969709A CA 2969709 A1 CA2969709 A1 CA 2969709A1
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CA
Canada
Prior art keywords
alkyl
pyrazol
formula
mmol
compound
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA2969709A
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English (en)
French (fr)
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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Celgene Corp
Array Biopharma Inc
Original Assignee
Celgene Corp
Array Biopharma Inc
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 Celgene Corp, Array Biopharma Inc filed Critical Celgene Corp
Publication of CA2969709A1 publication Critical patent/CA2969709A1/en
Abandoned legal-status Critical Current

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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
    • 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
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • A61P17/00—Drugs for dermatological disorders
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61P19/00—Drugs for skeletal disorders
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    • A—HUMAN NECESSITIES
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
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    • A61P19/00—Drugs for skeletal disorders
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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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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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

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  • 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)
CA2969709A 2014-12-05 2015-12-04 4,6-substituted-pyrazolo[1,5-a]pyrazines as janus kinase inhibitors Abandoned CA2969709A1 (en)

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

Publications (1)

Publication Number Publication Date
CA2969709A1 true CA2969709A1 (en) 2016-06-09

Family

ID=55069089

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2969709A Abandoned CA2969709A1 (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 (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)

* Cited by examiner, † Cited by third party
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

Family Cites Families (10)

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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
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
UA109131C2 (ru) * 2010-04-14 2015-07-27 Еррей Біофарма Інк. 5,7-ЗАМЕЩЕННЫЕ ИМИДАЗО[1,2-c]ПИРИМИДИНЫ КАК ИНГИБИТОРЫ JAK-КИНАЗ
BR112014008865A2 (pt) * 2011-10-12 2017-04-25 Array Biopharma Inc imidazo[1,2-c]pirimidinas 5,7-substituídas
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

Also Published As

Publication number Publication date
HRP20210501T1 (hr) 2021-05-14
CL2017001422A1 (es) 2018-01-05
MX386316B (es) 2025-03-18
EP3878451A1 (en) 2021-09-15
US10730880B2 (en) 2020-08-04
UA120065C2 (uk) 2019-09-25
AU2015357585B2 (en) 2020-07-02
RU2021102805A (ru) 2021-02-12
RU2017123387A (ru) 2019-01-11
US20190177328A1 (en) 2019-06-13
DK3227297T3 (da) 2021-04-06
PT3227297T (pt) 2021-04-09
AU2015357585A1 (en) 2017-07-13
PH12017501032A1 (en) 2017-11-27
US20200291039A1 (en) 2020-09-17
US20170362240A1 (en) 2017-12-21
HUE054371T2 (hu) 2021-09-28
JP2020055859A (ja) 2020-04-09
SG11201704542SA (en) 2017-07-28
WO2016090285A1 (en) 2016-06-09
MX2017007284A (es) 2017-08-25
TW201632523A (zh) 2016-09-16
JP2018507167A (ja) 2018-03-15
ZA201704494B (en) 2022-03-30
SI3227297T1 (sl) 2021-04-30
BR112017011798A2 (pt) 2017-12-26
RU2017123387A3 (OSRAM) 2019-06-03
KR20170090476A (ko) 2017-08-07
MY191016A (en) 2022-05-28
CN107278203B (zh) 2020-05-19
CN107278203A (zh) 2017-10-20
JP6641373B2 (ja) 2020-02-05
US10189845B2 (en) 2019-01-29
IL252656A0 (en) 2017-07-31
US11028093B2 (en) 2021-06-08
PL3227297T3 (pl) 2021-10-25
CR20170309A (es) 2018-02-02
EP3227297A1 (en) 2017-10-11
EP3227297B1 (en) 2021-01-20
CO2017006674A2 (es) 2017-10-20
ES2865483T3 (es) 2021-10-15
RU2742938C2 (ru) 2021-02-11
RS61693B1 (sr) 2021-05-31
TWI725004B (zh) 2021-04-21

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