HUE045192T2 - 6-morfolinil-2-pirazolil-9H-purin származékok és felhasználásuk PI3K inhibitorokként - Google Patents

6-morfolinil-2-pirazolil-9H-purin származékok és felhasználásuk PI3K inhibitorokként

Info

Publication number
HUE045192T2
HUE045192T2 HUE16718910A HUE16718910A HUE045192T2 HU E045192 T2 HUE045192 T2 HU E045192T2 HU E16718910 A HUE16718910 A HU E16718910A HU E16718910 A HUE16718910 A HU E16718910A HU E045192 T2 HUE045192 T2 HU E045192T2
Authority
HU
Hungary
Prior art keywords
morpholinyl
pyrazolyl
purine derivatives
pi3k inhibitors
pi3k
Prior art date
Application number
HUE16718910A
Other languages
English (en)
Inventor
Kirandeep Samby
Yogesh Surase
Sagar Amale
Suresh Gorla
Priyanka Patel
Ashwani Verma
Original Assignee
Daiichi Sankyo Co 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 Daiichi Sankyo Co Ltd filed Critical Daiichi Sankyo Co Ltd
Publication of HUE045192T2 publication Critical patent/HUE045192T2/hu

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • 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
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • 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
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • 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
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
HUE16718910A 2015-03-30 2016-03-29 6-morfolinil-2-pirazolil-9H-purin származékok és felhasználásuk PI3K inhibitorokként HUE045192T2 (hu)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IN878DE2015 2015-03-30

Publications (1)

Publication Number Publication Date
HUE045192T2 true HUE045192T2 (hu) 2019-12-30

Family

ID=55854760

Family Applications (1)

Application Number Title Priority Date Filing Date
HUE16718910A HUE045192T2 (hu) 2015-03-30 2016-03-29 6-morfolinil-2-pirazolil-9H-purin származékok és felhasználásuk PI3K inhibitorokként

Country Status (31)

Country Link
US (1) US10174035B2 (hu)
EP (1) EP3277682B1 (hu)
JP (1) JP6669417B2 (hu)
KR (1) KR20170131444A (hu)
CN (1) CN107428756B (hu)
AU (1) AU2016242080B2 (hu)
BR (1) BR112017020818A2 (hu)
CA (1) CA2980517C (hu)
CO (1) CO2017011020A2 (hu)
CY (1) CY1122018T1 (hu)
DK (1) DK3277682T3 (hu)
ES (1) ES2733505T3 (hu)
HK (1) HK1250161B (hu)
HR (1) HRP20190998T1 (hu)
HU (1) HUE045192T2 (hu)
IL (1) IL254688B (hu)
LT (1) LT3277682T (hu)
MX (1) MX2017012390A (hu)
MY (1) MY185268A (hu)
PH (1) PH12017501750A1 (hu)
PL (1) PL3277682T3 (hu)
PT (1) PT3277682T (hu)
RS (1) RS59213B1 (hu)
RU (1) RU2710549C2 (hu)
SG (1) SG11201706509QA (hu)
SI (1) SI3277682T1 (hu)
SM (1) SMT201900405T1 (hu)
TR (1) TR201910941T4 (hu)
TW (1) TWI689508B (hu)
WO (1) WO2016157074A1 (hu)
ZA (1) ZA201705530B (hu)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10822336B2 (en) * 2016-09-29 2020-11-03 Daiichi Sankyo Company, Limited Crystals of [2-(1-methyl-1H-pyrazol-4-yl)-6(morpholin-4-yl)-9H-purin-8-yl][4-(morpholin-4-yl)piperidin-1-yl]methanone and pharmaceutically acceptable salt thereof
CN107163061A (zh) * 2017-04-14 2017-09-15 江西科技师范大学 含吡唑啉结构的噻吩并嘧啶类化合物的制备及应用
CN110963955A (zh) * 2018-09-30 2020-04-07 南京富润凯德生物医药有限公司 一种单氟代螺环化合物的合成方法及其中间体
CN111087336A (zh) * 2018-10-24 2020-05-01 南京富润凯德生物医药有限公司 一种双氟代螺环化合物的合成方法及其中间体
CN110577515B (zh) * 2019-09-02 2022-05-17 南通大学 一种4-(氮杂环丁烷-3-基)-1-甲基哌嗪-2-酮二盐酸盐的合成方法

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4768265B2 (ja) 2002-10-15 2011-09-07 シンタ ファーマシューティカルズ コーポレーション 新規化合物
WO2005000404A2 (en) 2003-05-29 2005-01-06 Synta Pharmaceuticals, Corp. Heterocyclic compounds for preventing and treating disorders associated with excessive bone loss
GB2431156A (en) 2005-10-11 2007-04-18 Piramed Ltd 1-cyclyl-3-substituted- -benzenes and -azines as inhibitors of phosphatidylinositol 3-kinase
TW200801012A (en) * 2006-04-26 2008-01-01 Piramed Ltd Phosphoinositide 3-kinase inhibitor compounds and methods of use
TWI498332B (zh) * 2006-04-26 2015-09-01 Hoffmann La Roche 作為pi3k抑制劑之嘧啶衍生物及相關製備方法、醫藥組合物、用途、套組及產物
US20080233127A1 (en) 2007-03-21 2008-09-25 Wyeth Imidazolopyrimidine analogs and their use as pi3 kinase and mtor inhibitors
WO2009034386A1 (en) 2007-09-13 2009-03-19 Astrazeneca Ab Derivatives of adenine and 8-aza-adenine and uses thereof-796
EP2209786B1 (en) 2007-10-05 2013-02-27 Verastem, Inc. Pyrimidine substituted purine derivatives
WO2009045174A1 (en) 2007-10-05 2009-04-09 S*Bio Pte Ltd 2-morpholinylpurines as inhibitors of pi3k
US20110230464A1 (en) 2007-10-26 2011-09-22 Paul Goldsmith Purine derivatives useful as p13 kinase inhibitors
WO2009100406A2 (en) 2008-02-07 2009-08-13 Synta Pharmaceuticals Corp. Topical formulations for the treatment of psoriasis
CA2721851A1 (en) 2008-05-30 2009-12-03 Genentech, Inc. Purine pi3k inhibitor compounds and methods of use
US8513221B2 (en) 2008-07-07 2013-08-20 Xcovery Holding, LLC PI3K isoform selective inhibitors
TWI378933B (en) 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
WO2010114494A1 (en) 2009-04-03 2010-10-07 S*Bio Pte Ltd 8-substituted-2-morpholino purines for use as pi3k and/or mtor inhibitors in the treatment of proliferative disorders
US8158625B2 (en) 2009-05-27 2012-04-17 Genentech, Inc. Bicyclic indole-pyrimidine PI3K inhibitor compounds selective for P110 delta, and methods of use
BRPI1009022A2 (pt) * 2009-05-27 2016-03-08 Hoffmann La Roche "composto, composição farmacêutica, processo para produzir uma composição farmacêutica, uso de um composto, método para tratamento de uma doença ou transtorno e kit"
JP5579864B2 (ja) 2009-11-12 2014-08-27 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト N−9−置換プリン化合物、組成物及び使用の方法
ES2536780T3 (es) 2010-07-14 2015-05-28 F. Hoffmann-La Roche Ag Compuestos de purina selectivos para I3 p110 delta, y métodos de uso
CA2812091C (en) 2010-09-14 2020-03-24 Exelixis, Inc. Inhibitors of pi3k-delta and methods of their use and manufacture
TW201500358A (zh) 2010-12-16 2015-01-01 赫夫門羅氏藥廠股份有限公司 三環pi3k抑制劑化合物及其使用方法
MX343706B (es) 2011-01-31 2016-11-18 Novartis Ag Derivados heterocíclicos novedosos.
RU2013138835A (ru) 2011-02-09 2015-03-20 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения в качестве ингибиторов pi3 киназы

Also Published As

Publication number Publication date
PT3277682T (pt) 2019-07-09
JP6669417B2 (ja) 2020-03-18
US20180072732A1 (en) 2018-03-15
MX2017012390A (es) 2018-01-26
IL254688A0 (en) 2017-11-30
LT3277682T (lt) 2019-06-25
PL3277682T3 (pl) 2019-09-30
CA2980517C (en) 2020-02-25
WO2016157074A1 (en) 2016-10-06
TWI689508B (zh) 2020-04-01
IL254688B (en) 2021-03-25
SG11201706509QA (en) 2017-09-28
ZA201705530B (en) 2018-05-30
AU2016242080B2 (en) 2019-09-19
EP3277682A1 (en) 2018-02-07
TR201910941T4 (tr) 2019-08-21
RU2017134110A (ru) 2019-04-03
RU2710549C2 (ru) 2019-12-27
HRP20190998T1 (hr) 2019-10-18
RS59213B1 (sr) 2019-10-31
MY185268A (en) 2021-04-30
DK3277682T3 (da) 2019-07-29
ES2733505T3 (es) 2019-11-29
EP3277682B1 (en) 2019-04-24
CO2017011020A2 (es) 2018-01-16
CA2980517A1 (en) 2016-10-06
PH12017501750A1 (en) 2018-04-02
BR112017020818A2 (pt) 2018-07-03
CN107428756A (zh) 2017-12-01
RU2017134110A3 (hu) 2019-06-11
SMT201900405T1 (it) 2019-09-09
AU2016242080A1 (en) 2017-08-24
HK1250161B (en) 2020-05-15
KR20170131444A (ko) 2017-11-29
US10174035B2 (en) 2019-01-08
SI3277682T1 (sl) 2019-06-28
TW201643162A (zh) 2016-12-16
JP2018510146A (ja) 2018-04-12
CY1122018T1 (el) 2020-10-14
CN107428756B (zh) 2019-07-23

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