TWI562992B - Indazole derivative, pharmaceutical composition thereof, and use thereof as inhibitors of kinase activity - Google Patents

Indazole derivative, pharmaceutical composition thereof, and use thereof as inhibitors of kinase activity

Info

Publication number
TWI562992B
TWI562992B TW104135940A TW104135940A TWI562992B TW I562992 B TWI562992 B TW I562992B TW 104135940 A TW104135940 A TW 104135940A TW 104135940 A TW104135940 A TW 104135940A TW I562992 B TWI562992 B TW I562992B
Authority
TW
Taiwan
Prior art keywords
inhibitors
pharmaceutical composition
kinase activity
indazole derivative
indazole
Prior art date
Application number
TW104135940A
Other languages
English (en)
Chinese (zh)
Other versions
TW201604192A (zh
Inventor
Julie Nicole Hamblin
Paul Spencer Jones
Suzanne Elaine Keeling
Joelle Le
Charlotte Jane Mitchell
Nigel James Parr
Original Assignee
Glaxo Group Ltd
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 Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of TW201604192A publication Critical patent/TW201604192A/zh
Application granted granted Critical
Publication of TWI562992B publication Critical patent/TWI562992B/zh

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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    • 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
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    • 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
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    • A—HUMAN NECESSITIES
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
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  • Oncology (AREA)
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  • Hematology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
TW104135940A 2009-04-30 2010-04-28 Indazole derivative, pharmaceutical composition thereof, and use thereof as inhibitors of kinase activity TWI562992B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US17403309P 2009-04-30 2009-04-30

Publications (2)

Publication Number Publication Date
TW201604192A TW201604192A (zh) 2016-02-01
TWI562992B true TWI562992B (en) 2016-12-21

Family

ID=42225106

Family Applications (3)

Application Number Title Priority Date Filing Date
TW104135940A TWI562992B (en) 2009-04-30 2010-04-28 Indazole derivative, pharmaceutical composition thereof, and use thereof as inhibitors of kinase activity
TW99113559A TWI466884B (zh) 2009-04-30 2010-04-28 6-(1h-吲哚-4-基)-4-(5-{[4-(1-甲基乙基)-1-哌嗪基]甲基}-1,3-噁唑-2-基)-1h-吲唑、其醫藥組合物及作為激酶活性抑制劑之用途
TW103127990A TWI516487B (zh) 2009-04-30 2010-04-28 新穎化合物、其醫藥組合物及作為激酶活性抑制劑之用途

Family Applications After (2)

Application Number Title Priority Date Filing Date
TW99113559A TWI466884B (zh) 2009-04-30 2010-04-28 6-(1h-吲哚-4-基)-4-(5-{[4-(1-甲基乙基)-1-哌嗪基]甲基}-1,3-噁唑-2-基)-1h-吲唑、其醫藥組合物及作為激酶活性抑制劑之用途
TW103127990A TWI516487B (zh) 2009-04-30 2010-04-28 新穎化合物、其醫藥組合物及作為激酶活性抑制劑之用途

Country Status (39)

Country Link
US (14) US8580797B2 (OSRAM)
EP (3) EP2899191B1 (OSRAM)
JP (1) JP5570589B2 (OSRAM)
KR (2) KR101679642B1 (OSRAM)
CN (1) CN102459253B (OSRAM)
AR (2) AR076435A1 (OSRAM)
AU (1) AU2010243613B2 (OSRAM)
BR (1) BRPI1016219B8 (OSRAM)
CA (1) CA2759476C (OSRAM)
CL (1) CL2011002706A1 (OSRAM)
CO (1) CO6390057A2 (OSRAM)
CR (1) CR20110603A (OSRAM)
CY (1) CY1119515T1 (OSRAM)
DK (2) DK2424864T3 (OSRAM)
DO (1) DOP2011000328A (OSRAM)
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HR (2) HRP20150173T1 (OSRAM)
HU (1) HUE034724T2 (OSRAM)
IL (1) IL215803A (OSRAM)
JO (1) JO3025B1 (OSRAM)
LT (1) LT2899191T (OSRAM)
MA (1) MA33304B1 (OSRAM)
ME (2) ME02053B (OSRAM)
MX (1) MX2011011534A (OSRAM)
MY (1) MY160454A (OSRAM)
NZ (1) NZ596071A (OSRAM)
PE (1) PE20120321A1 (OSRAM)
PL (2) PL2424864T3 (OSRAM)
PT (2) PT2424864E (OSRAM)
RS (2) RS56433B1 (OSRAM)
SG (2) SG10201401881QA (OSRAM)
SI (2) SI2899191T1 (OSRAM)
SM (2) SMT201700481T1 (OSRAM)
TW (3) TWI562992B (OSRAM)
UA (1) UA101098C2 (OSRAM)
UY (1) UY32585A (OSRAM)
WO (1) WO2010125082A1 (OSRAM)
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JP5502076B2 (ja) 2008-06-05 2014-05-28 グラクソ グループ リミテッド 新規化合物
ES2383246T3 (es) 2008-06-05 2012-06-19 Glaxo Group Limited 4-amino-indazoles
WO2009147188A1 (en) 2008-06-05 2009-12-10 Glaxo Group Limited Benzpyrazol derivatives as inhibitors of pi3 kinases
JP5656880B2 (ja) 2009-03-09 2015-01-21 グラクソ グループ リミテッドＧｌａｘｏ Ｇｒｏｕｐ Ｌｉｍｉｔｅｄ Ｐｉ３キナーゼの阻害剤としての４−オキサジアゾール−２−イル−インダゾール
MY160454A (en) 2009-04-30 2017-03-15 Glaxo Group Ltd Oxazole substituted indazoles as pi3-kinase inhibitors
CN102372675B (zh) * 2010-08-14 2013-12-18 王娜 6-氯-4-碘吲唑及其制备方法与应用
US9102668B2 (en) * 2010-09-08 2015-08-11 Glaxo Group Limited Polymorphs and salts
US9326987B2 (en) 2010-09-08 2016-05-03 Glaxo Group Limited Indazole derivatives for use in the treatment of influenza virus infection
DK2614058T3 (en) 2010-09-08 2015-09-28 Glaxosmithkline Ip Dev Ltd Polymorphs, and the salts of N- [5- [4- (5 - {[(2R, 6S) -2,6-dimethyl-4-morpholinyl] methyl} -1,3-oxazol-2-yl) -1H-indazole -6-yl] -2- (methyloxy) -3-pyridinyl] methanesulfonamide.
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
CA2816753A1 (en) * 2010-11-08 2012-05-18 Lycera Corporation N- sulfonylated tetrahydroquinolines and related bicyclic compounds inhibition of rory activity and the treatment of diseases
CA2857302C (en) 2011-12-15 2020-08-25 Novartis Ag Use of inhibitors of the activity or function of pi3k
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