KR102987770B1 - 3,6-디아미노-피리다진-3-일 유도체, 이를 함유하는 약학적 조성물 및 아폽토시스 유발제로서의 용도 - Google Patents

3,6-디아미노-피리다진-3-일 유도체, 이를 함유하는 약학적 조성물 및 아폽토시스 유발제로서의 용도

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Publication number
KR102987770B1
KR102987770B1 KR1020227006624A KR20227006624A KR102987770B1 KR 102987770 B1 KR102987770 B1 KR 102987770B1 KR 1020227006624 A KR1020227006624 A KR 1020227006624A KR 20227006624 A KR20227006624 A KR 20227006624A KR 102987770 B1 KR102987770 B1 KR 102987770B1
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South Korea
Prior art keywords
methyl
amino
propyl
thiazole
benzothiazole
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Active
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KR1020227006624A
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English (en)
Korean (ko)
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KR20220042182A (ko
Inventor
제임스 에드워드 폴 데이비슨
티보르 노박
아틸라 파찰
안드라스 코치
제롬-베누아 스타크
제임스 브룩 머레이
사이먼 베드포드
마이아 찬리온
프레데릭 콜랜드
파트리스 데소스
마크 필립 도즈워스
페트라 던켈
안드라스 헤르너
졸탄 마다라스
아나 레티샤 마라뇨
마크 몰나르
미클로스 니에르게스
레이첼 제인 파슨스
모니카 루다소바
아그네스 스트로펙
마리안나 시게티
마티아스 팔 티마리
폴 웹
Original Assignee
르 라보레또레 쎄르비에르
베르날리스 (알 앤드 디) 리미티드
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Application filed by 르 라보레또레 쎄르비에르, 베르날리스 (알 앤드 디) 리미티드 filed Critical 르 라보레또레 쎄르비에르
Publication of KR20220042182A publication Critical patent/KR20220042182A/ko
Application granted granted Critical
Publication of KR102987770B1 publication Critical patent/KR102987770B1/ko
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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)
KR1020227006624A 2019-07-29 2020-07-28 3,6-디아미노-피리다진-3-일 유도체, 이를 함유하는 약학적 조성물 및 아폽토시스 유발제로서의 용도 Active KR102987770B1 (ko)

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 (2)

Publication Number Publication Date
KR20220042182A KR20220042182A (ko) 2022-04-04
KR102987770B1 true KR102987770B1 (ko) 2026-07-07

Family

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KR1020227006624A Active KR102987770B1 (ko) 2019-07-29 2020-07-28 3,6-디아미노-피리다진-3-일 유도체, 이를 함유하는 약학적 조성물 및 아폽토시스 유발제로서의 용도

Country Status (30)

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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)
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DO (1) DOP2022000015A (enExample)
ES (1) ES3074241T3 (enExample)
FI (1) FI4003988T3 (enExample)
GE (2) GEP20247670B (enExample)
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JO (1) JOP20220006A1 (enExample)
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MA (1) MA56644B1 (enExample)
MX (1) MX2022001161A (enExample)
PE (1) PE20220704A1 (enExample)
PH (1) PH12022550018A1 (enExample)
PT (1) PT4003988T (enExample)
PY (1) PY2039849A (enExample)
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TW (1) TWI900486B (enExample)
UA (1) UA130870C2 (enExample)
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WO (1) WO2021018857A1 (enExample)

Families Citing this family (7)

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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)

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WO2003059354A2 (en) 2001-12-21 2003-07-24 Bayer Pharmaceuticals Corporation Anti-angiogenesis combination therapies comprising pyridazine or pyridine derivatives
WO2009020603A2 (en) 2007-08-08 2009-02-12 The Scripps Research Institute Upp amphiphilic alpha-helix mimetics

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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
WO2003059354A2 (en) 2001-12-21 2003-07-24 Bayer Pharmaceuticals Corporation Anti-angiogenesis combination therapies comprising pyridazine or pyridine derivatives
WO2009020603A2 (en) 2007-08-08 2009-02-12 The Scripps Research Institute Upp amphiphilic alpha-helix mimetics

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IL289932B1 (en) 2025-10-01
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
JP7646626B2 (ja) 2025-03-17
EP4003988B1 (en) 2026-05-20
BR112022001330A2 (pt) 2022-05-17

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