JP7646626B2 - ３，６－ジアミノ－ピリダジン－３－イル誘導体、それを含有する医薬組成物及びアポトーシス促進剤としてのその使用 - Google Patents

３，６－ジアミノ－ピリダジン－３－イル誘導体、それを含有する医薬組成物及びアポトーシス促進剤としてのその使用 Download PDF

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Publication number
JP7646626B2
JP7646626B2 JP2022505602A JP2022505602A JP7646626B2 JP 7646626 B2 JP7646626 B2 JP 7646626B2 JP 2022505602 A JP2022505602 A JP 2022505602A JP 2022505602 A JP2022505602 A JP 2022505602A JP 7646626 B2 JP7646626 B2 JP 7646626B2
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Japan
Prior art keywords
methyl
amino
propyl
mmol
thiazole
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JP2022505602A
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English (en)
Japanese (ja)
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JP2022542937A (ja
JP2022542937A5 (enExample
Inventor
デービッドソン，ジェームス・エドワード・ポール
ノヴァーク，ティボール
パッツァル，アッティラ
コッチャイ，アンドラーシュ
スタルク，ジェローム－ブノワ
マレー，ジェームズ・ブルック
ベッドフォード，サイモン
シャンリオン，マイア
コラン，フレデリク
デソ，パトリス
ドッズワース，マーク・フィリップ
ドゥンケル，ペトラ
ヘルナー，アンドラーシュ
マダラシュ，ゾルターン
マラグノ，アナ・レティシア
モルナール，マーク
ニェルゲシュ，ミクロス
パーソンズ，レイチェル・ジェーン
ルダソヴァ，モニカ
シュトロフェク，アーグネシュ
シゲティ，マリアンナ
ティマリ，マティアス・パル
ウェッブ，ポール
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Les Laboratoires Servier SAS
Vernalis R&D Ltd
Original Assignee
Les Laboratoires Servier SAS
Vernalis R&D Ltd
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Publication of JP2022542937A publication Critical patent/JP2022542937A/ja
Publication of JP2022542937A5 publication Critical patent/JP2022542937A5/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • 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
    • A61K31/535—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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Hydrogenated Pyridines (AREA)
JP2022505602A 2019-07-29 2020-07-28 ３，６－ジアミノ－ピリダジン－３－イル誘導体、それを含有する医薬組成物及びアポトーシス促進剤としてのその使用 Active JP7646626B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP19188747.0 2019-07-29
EP19188747 2019-07-29
PCT/EP2020/071179 WO2021018857A1 (en) 2019-07-29 2020-07-28 3,6-diamino-pyridazin-3-yl derivatives, pharmaceutical compositions containing them and their uses as pro-apoptotic agents

Publications (3)

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JP2022542937A JP2022542937A (ja) 2022-10-07
JP2022542937A5 JP2022542937A5 (enExample) 2023-07-14
JP7646626B2 true JP7646626B2 (ja) 2025-03-17

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JP2022505602A Active JP7646626B2 (ja) 2019-07-29 2020-07-28 ３，６－ジアミノ－ピリダジン－３－イル誘導体、それを含有する医薬組成物及びアポトーシス促進剤としてのその使用

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US (1) US12649733B2 (enExample)
EP (1) EP4003988B1 (enExample)
JP (1) JP7646626B2 (enExample)
KR (1) KR102987770B1 (enExample)
CN (1) CN114450283B (enExample)
AR (1) AR119493A1 (enExample)
AU (1) AU2020322072B2 (enExample)
BR (1) BR112022001330A2 (enExample)
CL (1) CL2021003594A1 (enExample)
CO (1) CO2022000700A2 (enExample)
CR (1) CR20220014A (enExample)
DK (1) DK4003988T3 (enExample)
DO (1) DOP2022000015A (enExample)
ES (1) ES3074241T3 (enExample)
FI (1) FI4003988T3 (enExample)
GE (2) GEP20247670B (enExample)
IL (1) IL289932B2 (enExample)
JO (1) JOP20220006A1 (enExample)
LT (1) LT4003988T (enExample)
MA (1) MA56644B1 (enExample)
MX (1) MX2022001161A (enExample)
PE (1) PE20220704A1 (enExample)
PH (1) PH12022550018A1 (enExample)
PT (1) PT4003988T (enExample)
PY (1) PY2039849A (enExample)
SA (1) SA522431498B1 (enExample)
TW (1) TWI900486B (enExample)
UA (1) UA130870C2 (enExample)
UY (1) UY38809A (enExample)
WO (1) WO2021018857A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116761635A (zh) * 2020-11-24 2023-09-15 诺华股份有限公司 Bcl-xl抑制剂抗体药物缀合物及其使用方法
JP2024505562A (ja) * 2021-02-02 2024-02-06 レス ラボラトイレス セルビエル 選択的ｂｃｌ－ｘｌ ｐｒｏｔａｃ化合物及び使用の方法
EP4525925A1 (en) 2022-05-20 2025-03-26 Novartis AG Epha2 bcl-xl inhibitor antibody-drug conjugates and methods of use thereof
CN119562832A (zh) 2022-05-20 2025-03-04 诺华股份有限公司 Met bcl-xl抑制剂抗体-药物缀合物及其使用方法
IL317101A (en) 2022-05-20 2025-01-01 Novartis Ag Antibody-drug conjugates of anticancer compounds and methods of using them
AR134424A1 (es) 2023-11-22 2026-01-14 Novartis Ag Conjugados de anticuerpo anti-cd7-fármaco y métodos de uso de los mismos
UY40985A (es) 2023-11-22 2025-06-30 Servier Lab Conjugados de anticuerpo anti-cd74-fármaco y métodos de uso de los mismos

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006503796A (ja) 2001-12-21 2006-02-02 バイエル・フアーマシユーチカルズ・コーポレーシヨン ピリダジンまたはピリジン誘導体を含んでなる抗−脈管形成組み合わせ療法
WO2009020603A2 (en) 2007-08-08 2009-02-12 The Scripps Research Institute Upp amphiphilic alpha-helix mimetics

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2008343932B2 (en) * 2007-12-19 2013-08-15 Amgen Inc. Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors
FR3015483B1 (fr) 2013-12-23 2016-01-01 Servier Lab Nouveaux derives de thienopyrimidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
EP3229844B1 (en) 2014-12-09 2020-03-04 AbbVie Inc. Antibody drug conjugates with cell permeable bcl-xl inhibitors
JP2018502839A (ja) 2014-12-09 2018-02-01 アッヴィ・インコーポレイテッド Ｂｃｌ−ｘＬ阻害性化合物およびこれを含む抗体薬物コンジュゲート
RU2017123942A (ru) 2014-12-09 2019-01-11 Эббви Инк. Ингибирующие bcl-xl соединения, обладающие низкой клеточной проницаемостью, и коньюгаты антитело-лекарственное средство, включающие их
US10124004B2 (en) * 2015-05-29 2018-11-13 Teijin Pharma Limited Pyrido[3,4-d]pyrimidine derivative and pharmaceutically acceptable salt thereof
MX2018015284A (es) 2016-06-08 2019-09-18 Abbvie Inc Conjugados de anticuerpo anti-egfr y fármaco.

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006503796A (ja) 2001-12-21 2006-02-02 バイエル・フアーマシユーチカルズ・コーポレーシヨン ピリダジンまたはピリジン誘導体を含んでなる抗−脈管形成組み合わせ療法
WO2009020603A2 (en) 2007-08-08 2009-02-12 The Scripps Research Institute Upp amphiphilic alpha-helix mimetics

Also Published As

Publication number Publication date
IL289932B1 (en) 2025-10-01
KR102987770B1 (ko) 2026-07-07
ES3074241T3 (en) 2026-07-20
WO2021018857A1 (en) 2021-02-04
PE20220704A1 (es) 2022-05-04
SA522431498B1 (ar) 2025-04-13
MA56644B1 (fr) 2026-06-30
EP4003988A1 (en) 2022-06-01
PY2039849A (es) 2021-05-06
FI4003988T3 (fi) 2026-07-10
JOP20220006A1 (ar) 2023-01-30
NZ784583A (en) 2025-02-28
PH12022550018A1 (en) 2022-10-17
GEAP202415866A (en) 2024-06-10
CO2022000700A2 (es) 2022-02-07
UA130870C2 (uk) 2026-06-03
KR20220042182A (ko) 2022-04-04
DOP2022000015A (es) 2022-05-15
IL289932A (en) 2022-03-01
CA3148502A1 (en) 2021-02-04
CN114450283B (zh) 2024-05-07
CR20220014A (es) 2022-03-02
AR119493A1 (es) 2021-12-22
JP2022542937A (ja) 2022-10-07
US20220289734A1 (en) 2022-09-15
UY38809A (es) 2021-02-26
MX2022001161A (es) 2022-02-22
PT4003988T (pt) 2026-07-20
LT4003988T (lt) 2026-07-10
CN114450283A (zh) 2022-05-06
AU2020322072A1 (en) 2022-02-10
AU2020322072B2 (en) 2026-06-25
GEP20247670B (en) 2024-09-25
US12649733B2 (en) 2026-06-09
IL289932B2 (en) 2026-02-01
TWI900486B (zh) 2025-10-11
CL2021003594A1 (es) 2022-11-18
DK4003988T3 (da) 2026-06-15
TW202118761A (zh) 2021-05-16
EP4003988B1 (en) 2026-05-20
BR112022001330A2 (pt) 2022-05-17

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