CN107108634B - 作为PI3Kβ抑制剂的咪唑并哒嗪衍生物 - Google Patents

作为PI3Kβ抑制剂的咪唑并哒嗪衍生物 Download PDF

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Publication number
CN107108634B
CN107108634B CN201580069133.7A CN201580069133A CN107108634B CN 107108634 B CN107108634 B CN 107108634B CN 201580069133 A CN201580069133 A CN 201580069133A CN 107108634 B CN107108634 B CN 107108634B
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substituted
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CN107108634A (zh
Inventor
L.A.梅维勒
L.米波伊
S.考帕
V.S.邦塞勒特
I.N.C.皮拉特
E.T.J.帕斯奎尔
D.J-C.伯特洛特
O.A.G.奎伊罗勒
C.梅耶
P.R.安吉鲍德
C.G.M.德梅斯特雷
G.J.M.梅塞伊
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Janssen Pharmaceutica NV
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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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Psychiatry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Taps Or Cocks (AREA)
CN201580069133.7A 2014-12-19 2015-12-18 作为PI3Kβ抑制剂的咪唑并哒嗪衍生物 Expired - Fee Related CN107108634B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EPEP14199322.0 2014-12-19
EP14199322 2014-12-19
PCT/EP2015/080604 WO2016097347A1 (en) 2014-12-19 2015-12-18 IMIDAZOPYRIDAZINE DERIVATIVES AS ΡΙ3Κβ INHIBITORS

Publications (2)

Publication Number Publication Date
CN107108634A CN107108634A (zh) 2017-08-29
CN107108634B true CN107108634B (zh) 2020-09-15

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CN201580069133.7A Expired - Fee Related CN107108634B (zh) 2014-12-19 2015-12-18 作为PI3Kβ抑制剂的咪唑并哒嗪衍生物

Country Status (26)

Country Link
US (1) US10087187B2 (enExample)
EP (1) EP3233862B1 (enExample)
JP (1) JP6568588B2 (enExample)
KR (1) KR20170095239A (enExample)
CN (1) CN107108634B (enExample)
AU (1) AU2015366190B2 (enExample)
BR (1) BR112017012930A2 (enExample)
CA (1) CA2967551A1 (enExample)
CY (1) CY1122381T1 (enExample)
DK (1) DK3233862T3 (enExample)
EA (1) EA029789B1 (enExample)
ES (1) ES2761051T3 (enExample)
HR (1) HRP20191550T1 (enExample)
HU (1) HUE045220T2 (enExample)
IL (1) IL252866B (enExample)
LT (1) LT3233862T (enExample)
MA (1) MA41174B1 (enExample)
MD (1) MD3233862T2 (enExample)
ME (1) ME03517B (enExample)
MX (1) MX2017008074A (enExample)
PL (1) PL3233862T3 (enExample)
PT (1) PT3233862T (enExample)
RS (1) RS59301B1 (enExample)
SI (1) SI3233862T1 (enExample)
SM (1) SMT201900509T1 (enExample)
WO (1) WO2016097347A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA037401B1 (ru) 2015-10-09 2021-03-24 Янссен Фармацевтика Нв Производные хиноксалина и пиридопиразина в качестве ингибиторов pi3k
CA3025594C (en) 2016-06-16 2024-06-18 Janssen Pharmaceutica Nv Bicyclic pyridine, pyrazine, and pyrimidine derivatives as pi3k beta inhibitors
MX391942B (es) 2017-03-29 2025-03-21 Janssen Pharmaceutica Nv Derivados de quinoxalina y piridoprazina como inhibidores de pi3k-beta
EP3921320B1 (en) * 2019-02-07 2024-03-06 BeiGene, Ltd. Imidazo [2, 1-f] [1, 2, 4] triazin-4-amine derivatives as tlr7 agonist
CN110128505A (zh) * 2019-05-21 2019-08-16 梯尔希（南京）药物研发有限公司 一种戈舍瑞林杂质的合成方法

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008138834A1 (en) * 2007-05-09 2008-11-20 Novartis Ag Substituted imidazopyridazines as pi3k lipid kinase inhibitors
WO2009060197A1 (en) * 2007-11-08 2009-05-14 Centro Nacional De Investigaciones Oncologicas (Cnio) Imidazopyridazines for use as protein kinase inhibitors
WO2009106577A1 (en) * 2008-02-28 2009-09-03 Novartis Ag Imidazo [1,2-b] pyridazine derivatives for the treatment of c-met tyrosine kinase mediated disease
WO2010007099A1 (en) * 2008-07-15 2010-01-21 Cellzome Limited 2-aminoimidazo[1,2-b]pyridazine derivatives as pi3k inhibitors
WO2011047770A2 (de) * 2009-10-19 2011-04-28 Merck Patent Gmbh Pyrazolopyrimidinderivate
WO2013028263A1 (en) * 2011-08-24 2013-02-28 Glaxosmithkline Llc Pyrazolopyrimidine derivatives as pi3 kinase inhibitors
WO2013095761A1 (en) * 2011-12-20 2013-06-27 Glaxosmithkline Llc Imidazopyridine derivatives as pi3 kinase inhibitors
WO2014078211A1 (en) * 2012-11-14 2014-05-22 Calitor Sciences, Llc Heteroaromatic compounds as pi3 kinase modulators and methods of use

Family Cites Families (12)

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Publication number Priority date Publication date Assignee Title
US20070078136A1 (en) 2005-09-22 2007-04-05 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
PE20121506A1 (es) 2006-07-14 2012-11-26 Amgen Inc Compuestos triazolopiridinas como inhibidores de c-met
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
US20090215818A1 (en) 2006-07-24 2009-08-27 Smithkline Beecham Corporation Thiozolidinedione derivatives as pi3 kinase inhibitors
AU2007292924A1 (en) 2006-09-07 2008-03-13 Biogen Idec Ma Inc. IRAK modulators for treating an inflammatory condition, cell proliferative disorder, immune disorder
KR101721280B1 (ko) 2009-08-17 2017-03-29 인텔리카인, 엘엘씨 헤테로사이클릭 화합물 및 이의 용도
WO2011058109A1 (en) 2009-11-12 2011-05-19 Ucb Pharma S.A. Fused bicyclic pyrrole and imidazole derivatives as kinase inhibitors
UY33304A (es) 2010-04-02 2011-10-31 Amgen Inc Compuestos heterocíclicos y sus usos
PT2624696T (pt) * 2010-10-06 2017-03-21 Glaxosmithkline Llc Derivados de benzimidazole como inibidores da cinase pi3
US9127000B2 (en) 2011-02-23 2015-09-08 Intellikine, LLC. Heterocyclic compounds and uses thereof
US8778937B2 (en) 2011-12-20 2014-07-15 Glaxosmithkline Llc Benzimidazole boronic acid derivatives as PI3 kinase inhibitors
GB201321734D0 (en) * 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic Agents

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008138834A1 (en) * 2007-05-09 2008-11-20 Novartis Ag Substituted imidazopyridazines as pi3k lipid kinase inhibitors
WO2009060197A1 (en) * 2007-11-08 2009-05-14 Centro Nacional De Investigaciones Oncologicas (Cnio) Imidazopyridazines for use as protein kinase inhibitors
WO2009106577A1 (en) * 2008-02-28 2009-09-03 Novartis Ag Imidazo [1,2-b] pyridazine derivatives for the treatment of c-met tyrosine kinase mediated disease
WO2010007099A1 (en) * 2008-07-15 2010-01-21 Cellzome Limited 2-aminoimidazo[1,2-b]pyridazine derivatives as pi3k inhibitors
WO2011047770A2 (de) * 2009-10-19 2011-04-28 Merck Patent Gmbh Pyrazolopyrimidinderivate
WO2013028263A1 (en) * 2011-08-24 2013-02-28 Glaxosmithkline Llc Pyrazolopyrimidine derivatives as pi3 kinase inhibitors
WO2013095761A1 (en) * 2011-12-20 2013-06-27 Glaxosmithkline Llc Imidazopyridine derivatives as pi3 kinase inhibitors
WO2014078211A1 (en) * 2012-11-14 2014-05-22 Calitor Sciences, Llc Heteroaromatic compounds as pi3 kinase modulators and methods of use

Also Published As

Publication number Publication date
JP2017538734A (ja) 2017-12-28
RS59301B1 (sr) 2019-10-31
MD3233862T2 (ro) 2019-11-30
IL252866A0 (en) 2017-08-31
MA41174A (fr) 2017-10-25
HUE045220T2 (hu) 2019-12-30
KR20170095239A (ko) 2017-08-22
US10087187B2 (en) 2018-10-02
MX2017008074A (es) 2018-01-09
EA201791396A1 (ru) 2017-10-31
JP6568588B2 (ja) 2019-08-28
CA2967551A1 (en) 2016-06-23
BR112017012930A2 (pt) 2018-01-09
EA029789B1 (ru) 2018-05-31
PL3233862T3 (pl) 2020-01-31
ME03517B (me) 2020-04-20
AU2015366190A1 (en) 2017-05-25
EP3233862A1 (en) 2017-10-25
HRP20191550T1 (hr) 2019-11-29
US20180002336A1 (en) 2018-01-04
PT3233862T (pt) 2019-10-09
MA41174B1 (fr) 2019-09-30
SI3233862T1 (sl) 2019-09-30
ES2761051T3 (es) 2020-05-18
SMT201900509T1 (it) 2019-11-13
LT3233862T (lt) 2019-09-10
AU2015366190B2 (en) 2020-01-23
IL252866B (en) 2020-09-30
CN107108634A (zh) 2017-08-29
EP3233862B1 (en) 2019-07-03
WO2016097347A1 (en) 2016-06-23
CY1122381T1 (el) 2021-01-27
DK3233862T3 (da) 2019-10-07

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Granted publication date: 20200915