TWI900486B - 3,6-二胺基-嗒-3基衍生物、含其之醫藥組成物及其作為促進細胞凋亡劑之用途 - Google Patents

3,6-二胺基-嗒-3基衍生物、含其之醫藥組成物及其作為促進細胞凋亡劑之用途

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Publication number
TWI900486B
TWI900486B TW109125418A TW109125418A TWI900486B TW I900486 B TWI900486 B TW I900486B TW 109125418 A TW109125418 A TW 109125418A TW 109125418 A TW109125418 A TW 109125418A TW I900486 B TWI900486 B TW I900486B
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TW
Taiwan
Prior art keywords
methyl
amino
group
propyl
thiazole
Prior art date
Application number
TW109125418A
Other languages
English (en)
Chinese (zh)
Other versions
TW202118761A (zh
Inventor
詹母士 愛德華 保羅 德維森
蒂博爾 諾娃克
阿提拉 帕克薩爾
安德拉斯 科奇
傑若姆 畢諾特 史塔克
詹母士 布魯基 莫瑞
賽門 貝多弗
瑪雅 泉琳恩
弗雷德里克 科蘭
派翠絲 德索斯
馬克 菲利普 達資沃司
佩特拉 丹凱爾
安德拉斯 赫納
佐爾坦 默德拉茲
安娜 萊蒂西亞 莫雷葛諾
馬克 莫爾納
米克羅司 倪兒祺
瑞秋 珍 帕森斯
莫妮卡 魯達索瓦
安格妮絲 史卓費課
瑪麗安娜 西蓋蒂
馬諦亞斯 帕爾 蒂馬里
保羅 韋伯
Original Assignee
法商施維雅藥廠
英商佛納利斯(R&D)股份有限公司
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Application filed by 法商施維雅藥廠, 英商佛納利斯(R&D)股份有限公司 filed Critical 法商施維雅藥廠
Publication of TW202118761A publication Critical patent/TW202118761A/zh
Application granted granted Critical
Publication of TWI900486B publication Critical patent/TWI900486B/zh

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Classifications

    • 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

Landscapes

  • 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)
TW109125418A 2019-07-29 2020-07-28 3,6-二胺基-嗒-3基衍生物、含其之醫藥組成物及其作為促進細胞凋亡劑之用途 TWI900486B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP19188747.0 2019-07-29
EP19188747 2019-07-29

Publications (2)

Publication Number Publication Date
TW202118761A TW202118761A (zh) 2021-05-16
TWI900486B true TWI900486B (zh) 2025-10-11

Family

ID=67514281

Family Applications (1)

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TW109125418A TWI900486B (zh) 2019-07-29 2020-07-28 3,6-二胺基-嗒-3基衍生物、含其之醫藥組成物及其作為促進細胞凋亡劑之用途

Country Status (30)

Country Link
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
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

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
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

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
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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