CN109311843B - 作为PI3Kβ抑制剂的氮杂苯并咪唑衍生物 - Google Patents

作为PI3Kβ抑制剂的氮杂苯并咪唑衍生物 Download PDF

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Publication number
CN109311843B
CN109311843B CN201780037153.5A CN201780037153A CN109311843B CN 109311843 B CN109311843 B CN 109311843B CN 201780037153 A CN201780037153 A CN 201780037153A CN 109311843 B CN109311843 B CN 109311843B
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Chinese (zh)
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CN109311843A (zh
Inventor
I.N.C.皮拉特
O.A.G.克罗勒
P.R.安吉鲍
D.J-C.贝特洛
S.库帕
C.G.M.德梅斯特雷
L.米尔佩尔
G.J.M.梅塞
L.A.梅维勒
C.梅耶
E.T.J.帕基尔
V.S.蓬斯莱
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201780037153.5A 2016-06-16 2017-06-15 作为PI3Kβ抑制剂的氮杂苯并咪唑衍生物 Active CN109311843B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP16174712 2016-06-16
EP16174712.6 2016-06-16
PCT/EP2017/064672 WO2017216293A1 (en) 2016-06-16 2017-06-15 Azabenzimidazole derivatives as pi3k beta inhibitors

Publications (2)

Publication Number Publication Date
CN109311843A CN109311843A (zh) 2019-02-05
CN109311843B true CN109311843B (zh) 2021-10-08

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CN201780037153.5A Active CN109311843B (zh) 2016-06-16 2017-06-15 作为PI3Kβ抑制剂的氮杂苯并咪唑衍生物

Country Status (13)

Country Link
US (1) US20190263804A1 (https=)
EP (1) EP3472147B1 (https=)
JP (1) JP7158286B2 (https=)
KR (1) KR102472198B1 (https=)
CN (1) CN109311843B (https=)
AU (1) AU2017286380B2 (https=)
BR (1) BR112018076169A2 (https=)
CA (1) CA3025746A1 (https=)
EA (1) EA037871B1 (https=)
ES (1) ES2818620T3 (https=)
IL (1) IL263653A (https=)
MX (1) MX375484B (https=)
WO (1) WO2017216293A1 (https=)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK3904350T3 (da) 2018-04-12 2023-11-13 Bayer Ag N-(cyclopropylmethyl)-5-(methylsulfonyl)-n-{1-[1-(pyrimidin-2-yl)-1h-1,2,4-triazol-5-yl]ethyl}benzamidderivater og de tilsvarende pyridincarboxamidderivater som pesticider
WO2019209811A1 (en) 2018-04-24 2019-10-31 Bristol-Myers Squibb Company Macrocyclic toll-like receptor 7 (tlr7) agonists
MX2020011275A (es) 2018-04-25 2020-11-13 Bayer Ag Novedosos compuestos de heteroaril-triazol y hetroaril[-]tetrazol como plaguicidas.
US11554120B2 (en) 2018-08-03 2023-01-17 Bristol-Myers Squibb Company 1H-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (TLR7) agonists and methods and uses therefor
US20220274947A1 (en) 2019-07-23 2022-09-01 Bayer Aktiengesellschaft Novel heteroaryl-triazole compounds as pesticides
CN110551101B (zh) * 2019-08-28 2020-11-24 沈阳药科大学 1、6-二取代-苯并五元杂环类衍生物及其用途
TW202128664A (zh) 2019-10-09 2021-08-01 德商拜耳廠股份有限公司 作為除害劑之新穎雜芳基三唑化合物
JP2023512204A (ja) 2020-01-27 2023-03-24 ブリストル－マイヤーズ スクイブ カンパニー トール様受容体７（ＴＬＲ７）アゴニストとしての１Ｈ－ピラゾロ［４，３－ｄ］ピリミジン化合物
US20230131192A1 (en) 2020-01-27 2023-04-27 Bristol-Myers Squibb Company 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS
US12485123B2 (en) 2020-01-27 2025-12-02 Bristol-Myers Squibb Company 1H-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (TLR7) agonists
KR20220132601A (ko) 2020-01-27 2022-09-30 브리스톨-마이어스 스큅 컴퍼니 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물
CN115151546A (zh) 2020-01-27 2022-10-04 百时美施贵宝公司 作为Toll样受体7(TLR7)激动剂的C3-取代的1H-吡唑并[4,3-d]嘧啶化合物
US20230348468A1 (en) 2020-01-27 2023-11-02 Bristol-Myers Squibb Company 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS
KR20220132589A (ko) 2020-01-27 2022-09-30 브리스톨-마이어스 스큅 컴퍼니 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물
WO2021154663A1 (en) 2020-01-27 2021-08-05 Bristol-Myers Squibb Company 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS
US20230144824A1 (en) 2020-01-27 2023-05-11 Bristol-Myers Squibb Company 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS
US20250382289A1 (en) * 2022-02-18 2025-12-18 Xizang Haisco Pharmaceutical Co., Ltd. Pyrazolopyridine derivative and application thereof in medicine
WO2024222880A1 (zh) * 2023-04-27 2024-10-31 西藏海思科制药有限公司 一种吡啶并吡唑衍生物的药物组合物及其在医药上的应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009045175A1 (en) * 2007-10-05 2009-04-09 S*Bio Pte Ltd Pyrimidine substituted purine derivatives
WO2013095761A1 (en) * 2011-12-20 2013-06-27 Glaxosmithkline Llc Imidazopyridine derivatives as pi3 kinase inhibitors

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5177074A (en) * 1991-03-26 1993-01-05 Merck & Co., Inc. Angiotensin ii antagonists incorporating a substituted thiophene or furan
EP1993537A4 (en) 2006-03-02 2010-05-19 Glaxosmithkline Llc THIAZOLONES AS INHIBITORS OF P13-KINASES
WO2008014219A2 (en) 2006-07-24 2008-01-31 Smithkline Beecham Corporation Thiozolidinedione derivatives as p13 kinase inhibitors
WO2009021083A1 (en) 2007-08-09 2009-02-12 Smithkline Beecham Corporation Quinoxaline derivatives as pi3 kinase inhibitors
EP3613743B1 (en) 2008-01-04 2022-03-16 Intellikine, LLC Processes for the preparation of 1h-pyrazolo[3,4-d]pyrimidin-4-amine derivatives
PE20121148A1 (es) 2009-08-17 2012-09-07 Intellikine Llc Compuestos heterociclicos y usos de los mismos
KR20120081164A (ko) 2009-09-29 2012-07-18 엑스커버리 홀딩 컴퍼니 엘엘씨 Ｐｉ3ｋ(델타) 선택적 억제제
UY33304A (es) 2010-04-02 2011-10-31 Amgen Inc Compuestos heterocíclicos y sus usos
JP5719028B2 (ja) 2010-10-06 2015-05-13 グラクソスミスクライン エルエルシー Ｐｉ３キナーゼ阻害剤としてのベンズイミダゾール誘導体
WO2012116237A2 (en) 2011-02-23 2012-08-30 Intellikine, Llc Heterocyclic compounds and uses thereof
WO2013028263A1 (en) * 2011-08-24 2013-02-28 Glaxosmithkline Llc Pyrazolopyrimidine derivatives as pi3 kinase inhibitors
US8778937B2 (en) 2011-12-20 2014-07-15 Glaxosmithkline Llc Benzimidazole boronic acid derivatives as PI3 kinase inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009045175A1 (en) * 2007-10-05 2009-04-09 S*Bio Pte Ltd Pyrimidine substituted purine derivatives
WO2013095761A1 (en) * 2011-12-20 2013-06-27 Glaxosmithkline Llc Imidazopyridine derivatives as pi3 kinase inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Structure–activity relationships in Toll-like receptor 7 agonistic 1H-imidazo[4,5-c]pyridines;Euna Yoo, et al.;《Org. Biomol. Chem》;20130815;6526–6545 *

Also Published As

Publication number Publication date
CN109311843A (zh) 2019-02-05
MX2018015709A (es) 2019-03-21
JP2019518059A (ja) 2019-06-27
KR102472198B1 (ko) 2022-11-28
AU2017286380A1 (en) 2018-12-06
EA037871B1 (ru) 2021-05-28
MX375484B (es) 2025-03-06
KR20190016976A (ko) 2019-02-19
EA201892734A1 (ru) 2019-05-31
IL263653A (en) 2019-01-31
AU2017286380B2 (en) 2021-02-04
BR112018076169A2 (pt) 2019-03-26
EP3472147B1 (en) 2020-06-17
JP7158286B2 (ja) 2022-10-21
ES2818620T3 (es) 2021-04-13
CA3025746A1 (en) 2017-12-21
EP3472147A1 (en) 2019-04-24
US20190263804A1 (en) 2019-08-29
WO2017216293A1 (en) 2017-12-21

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