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JOP20190193A1 - ممركبات 2-أريل غير متجانس-3-أكسو-2، 3-ثنائي هيدرو بيريدازين-4-كربوكساميد لمعالجة السرطان - Google Patents

ممركبات 2-أريل غير متجانس-3-أكسو-2، 3-ثنائي هيدرو بيريدازين-4-كربوكساميد لمعالجة السرطان

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Publication number
JOP20190193A1
JOP20190193A1 JOP/2019/0193A JOP20190193A JOP20190193A1 JO P20190193 A1 JOP20190193 A1 JO P20190193A1 JO P20190193 A JOP20190193 A JO P20190193A JO P20190193 A1 JOP20190193 A1 JO P20190193A1
Authority
JO
Jordan
Prior art keywords
compounds
dihydropyridazine
heteroaryl
oxo
cancer
Prior art date
Application number
JOP/2019/0193A
Other languages
English (en)
Inventor
Horst Irlbacher
Ilona Gutcher
Christina Kober
Lars R?Se
Ulrike R?Hn
Benjamin Bader
Detlef St?Ckigt
Ludwig Zorn
Michael Platten
Rafael Carretero
Norbert Schmees
Original Assignee
Bayer Pharma AG
Bayer Ag
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.)
Filing date
Publication date
Application filed by Bayer Pharma AG, Bayer Ag filed Critical Bayer Pharma AG
Publication of JOP20190193A1 publication Critical patent/JOP20190193A1/ar

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/04—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having less than three double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/14—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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    • 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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    • 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
    • C07D401/14—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 three or more hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

يتعلق الاختراع الحالي بمركبات 2-اريل غير متجانس-3-أكسو-2، 3-ثنائي هيدرو بيريدازين-4-كربوكساميد بالصيغة العامة (I): (I) حيث X، R1، R2، R3، R4، وR5 كما هي موضحة ومحددة في هذه الوثيقة، بطرق لتحضير المركبات المذكورة، بمركبات وسيطة مفيدة في تحضير المركبات المذكورة، بتراكيب وتوليفات صيدلانية تشتمل على المركبات المذكورة، وباستخدام المركبات المذكورة في تصنيع تراكيب صيدلانية مستخدمة في العلاج أو الوقاية من الأمراض، ولا سيما السرطان أو حالات مرضية مقترنة باختلال الاستجابات المناعية وغيرها من الاضطرابات المصاحبة لتأشير AHR الشاذ، كعامل وحيد أو بشكل مؤتلف مع مكونات نشطة أخرى.
JOP/2019/0193A 2017-02-09 2017-06-16 ممركبات 2-أريل غير متجانس-3-أكسو-2، 3-ثنائي هيدرو بيريدازين-4-كربوكساميد لمعالجة السرطان JOP20190193A1 (ar)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP17155406 2017-02-09
EP17202882 2017-11-21

Publications (1)

Publication Number Publication Date
JOP20190193A1 true JOP20190193A1 (ar) 2019-08-08

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JOP/2019/0193A JOP20190193A1 (ar) 2017-02-09 2017-06-16 ممركبات 2-أريل غير متجانس-3-أكسو-2، 3-ثنائي هيدرو بيريدازين-4-كربوكساميد لمعالجة السرطان

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US (2) US20240294505A1 (ar)
EP (1) EP3580211B1 (ar)
JP (1) JP7128826B2 (ar)
KR (1) KR102627266B1 (ar)
CN (3) CN116554152A (ar)
AU (1) AU2018217860B2 (ar)
BR (1) BR112019016497A2 (ar)
CA (1) CA3052718A1 (ar)
CL (1) CL2019002255A1 (ar)
CO (1) CO2019008684A2 (ar)
CR (1) CR20190364A (ar)
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CY (1) CY1124484T1 (ar)
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DO (1) DOP2019000206A (ar)
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HR (1) HRP20210143T1 (ar)
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MA (1) MA47447B1 (ar)
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PE (1) PE20191496A1 (ar)
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CN114685426A (zh) * 2020-12-28 2022-07-01 苏州泽璟生物制药股份有限公司 磺酰胺类抑制剂及其制备方法和应用
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TW202320777A (zh) * 2021-09-14 2023-06-01 中國大陸商元啟（蘇州）生物製藥股份有限公司 芳基烴受體調節劑及其用於治療疾病及病症之用途
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CY1124484T1 (el) 2022-07-22
BR112019016497A2 (pt) 2022-05-10
AU2018217860A1 (en) 2019-08-22
MX2019009571A (es) 2020-01-20
JP2020506946A (ja) 2020-03-05
EP3580211B1 (en) 2020-12-02
TW201840549A (zh) 2018-11-16
CU20190073A7 (es) 2020-03-04
IL268469A (en) 2019-09-26
ES2847162T3 (es) 2021-08-02
MA47447B1 (fr) 2021-02-26
CL2019002255A1 (es) 2020-01-03
KR102627266B1 (ko) 2024-01-24
PE20191496A1 (es) 2019-10-21
PL3580211T3 (pl) 2021-04-19
SG11201907232XA (en) 2019-09-27
CO2019008684A2 (es) 2019-08-20
IL268469B (en) 2022-04-01
CA3052718A1 (en) 2018-08-16
HUE053191T2 (hu) 2021-06-28
GEP20217281B (en) 2021-08-10
SI3580211T1 (sl) 2021-06-30
TWI770113B (zh) 2022-07-11
UY37606A (es) 2018-09-28
RS61401B1 (sr) 2021-02-26
AU2018217860B2 (en) 2021-07-08
US11795164B2 (en) 2023-10-24
CR20190364A (es) 2019-09-27
UA124507C2 (uk) 2021-09-29
CN110678459A (zh) 2020-01-10
NI201900085A (es) 2019-11-15
CN116531380A (zh) 2023-08-04
ZA201905902B (en) 2021-05-26
EP3580211A1 (en) 2019-12-18
KR20190115460A (ko) 2019-10-11
DK3580211T3 (da) 2021-01-25
WO2018146010A1 (en) 2018-08-16
JP7128826B2 (ja) 2022-08-31
CN110678459B (zh) 2023-04-04
DOP2019000206A (es) 2019-09-30
PH12019501846A1 (en) 2020-03-09
US20230121195A1 (en) 2023-04-20
US20240294505A1 (en) 2024-09-05
LT3580211T (lt) 2021-02-25
HRP20210143T1 (hr) 2021-03-19
MA47447A (fr) 2019-12-18
CU24564B1 (es) 2022-01-13
ECSP19057713A (es) 2019-08-30
CN116554152A (zh) 2023-08-08
SA519402422B1 (ar) 2021-11-14

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