JP7434281B2 - Pad酵素のベンズイミダゾール阻害剤 - Google Patents

Pad酵素のベンズイミダゾール阻害剤 Download PDF

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JP7434281B2
JP7434281B2 JP2021506660A JP2021506660A JP7434281B2 JP 7434281 B2 JP7434281 B2 JP 7434281B2 JP 2021506660 A JP2021506660 A JP 2021506660A JP 2021506660 A JP2021506660 A JP 2021506660A JP 7434281 B2 JP7434281 B2 JP 7434281B2
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substituted
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heterocyclyl
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ケヒョン・グー
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Bristol Myers Squibb Co
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
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    • 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
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41921,2,3-Triazoles
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    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
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    • A61K31/435Heterocyclic 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
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • 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
    • A61K31/4965Non-condensed pyrazines
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    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • 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
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P35/00Antineoplastic agents
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    • A61P35/02Antineoplastic agents specific for leukemia
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    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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)
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  • Health & Medical Sciences (AREA)
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  • Medicinal Chemistry (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
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  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2021506660A 2018-08-08 2019-08-07 Pad酵素のベンズイミダゾール阻害剤 Active JP7434281B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862715845P 2018-08-08 2018-08-08
US62/715,845 2018-08-08
PCT/US2019/045459 WO2020033514A1 (en) 2018-08-08 2019-08-07 Benzimidazole inhibitors of pad enzymes

Publications (4)

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JP2021534104A JP2021534104A (ja) 2021-12-09
JP2021534104A5 JP2021534104A5 (https=) 2022-08-16
JPWO2020033514A5 JPWO2020033514A5 (https=) 2022-08-16
JP7434281B2 true JP7434281B2 (ja) 2024-02-20

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US (1) US20220348562A1 (https=)
EP (1) EP3833439B1 (https=)
JP (1) JP7434281B2 (https=)
KR (1) KR20210042933A (https=)
CN (1) CN112789087B (https=)
ES (1) ES2956090T3 (https=)
WO (1) WO2020033514A1 (https=)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3833671B1 (en) 2018-08-08 2022-08-24 Bristol-Myers Squibb Company Substituted thienopyrroles as pad4 inhibitors
AU2019319835A1 (en) 2018-08-08 2021-03-25 Bristol-Myers Squibb Company Indole and azaindole inhibitors of PAD enzymes
EP4100405A1 (en) 2020-02-06 2022-12-14 Bristol-Myers Squibb Company Macrocyclic pad4 inhibitors useful as immunosuppressant
TW202140477A (zh) 2020-02-12 2021-11-01 美商必治妥美雅史谷比公司 雜環pad4抑制劑
EP4143189A1 (en) * 2020-04-30 2023-03-08 Gilead Sciences, Inc. Macrocyclic inhibitors of peptidylarginine deiminases
TW202241884A (zh) 2020-12-22 2022-11-01 美商基利科學股份有限公司 肽基精胺酸去亞胺酶之抑制劑
WO2022140428A2 (en) 2020-12-22 2022-06-30 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases
WO2025024265A1 (en) 2023-07-21 2025-01-30 Bristol-Myers Squibb Company Methods of assessing citrullination and activity of pad4 modulators
WO2026020127A2 (en) 2024-07-19 2026-01-22 Bristol-Myers Squibb Company Methods of assessing citrullination and activity of pad2 modulators

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001021634A1 (en) 1999-09-21 2001-03-29 Lion Bioscience Ag Benzimidazole derivatives and combinatorial libraries thereof
WO2010051245A1 (en) 2008-11-03 2010-05-06 Merck Sharp & Dohme Corp. Benzimidazole and aza-benzimidazole carboxamides
JP2015522628A (ja) 2012-07-26 2015-08-06 グラクソ グループ リミテッドGlaxo Group L Pad4阻害剤としての2−(アザインドール−2−イル)ベンズイミダゾール
WO2017100594A1 (en) 2015-12-09 2017-06-15 Padlock Therapeutics, Inc. Bicyclic inhibitors of pad4
WO2017147102A1 (en) 2016-02-23 2017-08-31 Padlock Therapeutics, Inc. Heteroaryl inhibitors of pad4
CN107311933A (zh) 2017-06-28 2017-11-03 中国人民解放军军事医学科学院毒物药物研究所 一类苯并咪唑衍生物,及其制备方法和用途
WO2018022897A1 (en) 2016-07-27 2018-02-01 Padlock Therapeutics, Inc. Covalent inhibitors of pad4
JP2018520105A (ja) 2015-05-21 2018-07-26 グラクソスミスクライン、インテレクチュアル、プロパテ Pad4阻害剤としてのベンゾイミダゾール誘導体

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR107030A1 (es) * 2015-12-09 2018-03-14 Padlock Therapeutics Inc Inhibidores aza-bencimidazol de pad4

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001021634A1 (en) 1999-09-21 2001-03-29 Lion Bioscience Ag Benzimidazole derivatives and combinatorial libraries thereof
WO2010051245A1 (en) 2008-11-03 2010-05-06 Merck Sharp & Dohme Corp. Benzimidazole and aza-benzimidazole carboxamides
JP2015522628A (ja) 2012-07-26 2015-08-06 グラクソ グループ リミテッドGlaxo Group L Pad4阻害剤としての2−(アザインドール−2−イル)ベンズイミダゾール
JP2018520105A (ja) 2015-05-21 2018-07-26 グラクソスミスクライン、インテレクチュアル、プロパテ Pad4阻害剤としてのベンゾイミダゾール誘導体
WO2017100594A1 (en) 2015-12-09 2017-06-15 Padlock Therapeutics, Inc. Bicyclic inhibitors of pad4
WO2017147102A1 (en) 2016-02-23 2017-08-31 Padlock Therapeutics, Inc. Heteroaryl inhibitors of pad4
WO2018022897A1 (en) 2016-07-27 2018-02-01 Padlock Therapeutics, Inc. Covalent inhibitors of pad4
CN107311933A (zh) 2017-06-28 2017-11-03 中国人民解放军军事医学科学院毒物药物研究所 一类苯并咪唑衍生物,及其制备方法和用途

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Future Medicinal Chemistry,2013年,5(15),pp.1-14
Il Farmaco,1998年,53(6),pp.415-420

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Publication number Publication date
KR20210042933A (ko) 2021-04-20
EP3833439B1 (en) 2023-07-12
ES2956090T3 (es) 2023-12-13
CN112789087A (zh) 2021-05-11
CN112789087B (zh) 2024-08-13
JP2021534104A (ja) 2021-12-09
WO2020033514A1 (en) 2020-02-13
US20220348562A1 (en) 2022-11-03
EP3833439A1 (en) 2021-06-16

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