CN115052873A - 作为血浆激肽释放酶抑制剂的杂芳族甲酰胺衍生物 - Google Patents

作为血浆激肽释放酶抑制剂的杂芳族甲酰胺衍生物 Download PDF

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Publication number
CN115052873A
CN115052873A CN202180011395.3A CN202180011395A CN115052873A CN 115052873 A CN115052873 A CN 115052873A CN 202180011395 A CN202180011395 A CN 202180011395A CN 115052873 A CN115052873 A CN 115052873A
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China
Prior art keywords
mixture
azabicyclo
group
hex
methyl
Prior art date
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Pending
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CN202180011395.3A
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English (en)
Chinese (zh)
Inventor
M·埃克哈特
M·吉鲁
E·朗科普夫
C·迈尔
H·瓦格纳
D·威登迈尔
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Boehringer Ingelheim International GmbH
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Boehringer Ingelheim International GmbH
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Priority to CN202310088017.6A priority Critical patent/CN116120287B/zh
Publication of CN115052873A publication Critical patent/CN115052873A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (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)
  • Pyridine Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN202180011395.3A 2020-02-13 2021-02-11 作为血浆激肽释放酶抑制剂的杂芳族甲酰胺衍生物 Pending CN115052873A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202310088017.6A CN116120287B (zh) 2020-02-13 2021-02-11 作为血浆激肽释放酶抑制剂的杂芳族甲酰胺衍生物

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP20157259 2020-02-13
EP20157259.1 2020-02-13
PCT/EP2021/053286 WO2021160718A1 (en) 2020-02-13 2021-02-11 Heteroaromatic carboxamide derivatives as plasma kallikrein inhibitors

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CN202310088017.6A Division CN116120287B (zh) 2020-02-13 2021-02-11 作为血浆激肽释放酶抑制剂的杂芳族甲酰胺衍生物

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Publication Number Publication Date
CN115052873A true CN115052873A (zh) 2022-09-13

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CN202180011395.3A Pending CN115052873A (zh) 2020-02-13 2021-02-11 作为血浆激肽释放酶抑制剂的杂芳族甲酰胺衍生物
CN202310088017.6A Active CN116120287B (zh) 2020-02-13 2021-02-11 作为血浆激肽释放酶抑制剂的杂芳族甲酰胺衍生物

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Country Status (21)

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US (3) US11760745B2 (https=)
EP (1) EP4103562A1 (https=)
JP (3) JP7230277B2 (https=)
KR (1) KR20220141333A (https=)
CN (2) CN115052873A (https=)
AR (2) AR121341A1 (https=)
AU (1) AU2021218952A1 (https=)
BR (1) BR112022013979A2 (https=)
CA (1) CA3168690A1 (https=)
CL (2) CL2022002101A1 (https=)
CO (1) CO2022011254A2 (https=)
CR (2) CR20250167A (https=)
DO (2) DOP2022000157A (https=)
EC (1) ECSP22062410A (https=)
IL (2) IL320007A (https=)
JO (1) JOP20220186A1 (https=)
MX (3) MX2022009941A (https=)
PE (2) PE20221591A1 (https=)
SA (1) SA522440127B1 (https=)
TW (2) TWI873290B (https=)
WO (1) WO2021160718A1 (https=)

Cited By (1)

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Publication number Priority date Publication date Assignee Title
WO2025001956A1 (zh) * 2023-06-30 2025-01-02 远森制药（杭州）有限公司 杂芳族甲酰胺类化合物及其在医药上的应用

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CN112839711A (zh) 2018-10-10 2021-05-25 勃林格殷格翰国际有限公司 作为血浆激肽释放酶抑制剂的苯基四唑衍生物
TW202144331A (zh) * 2020-02-13 2021-12-01 德商百靈佳殷格翰國際股份有限公司 作為血漿激肽釋放酶抑制劑之雜芳族甲醯胺衍生物
TWI873290B (zh) * 2020-02-13 2025-02-21 德商百靈佳殷格翰國際股份有限公司 作為血漿激肽釋放酶抑制劑之雜芳族甲醯胺衍生物

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TW202144331A (zh) 2020-02-13 2021-12-01 德商百靈佳殷格翰國際股份有限公司 作為血漿激肽釋放酶抑制劑之雜芳族甲醯胺衍生物

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025001956A1 (zh) * 2023-06-30 2025-01-02 远森制药（杭州）有限公司 杂芳族甲酰胺类化合物及其在医药上的应用

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JP2022543494A (ja) 2022-10-12
AU2021218952A1 (en) 2022-07-28
WO2021160718A1 (en) 2021-08-19
IL295125B2 (en) 2025-09-01
US20240076286A1 (en) 2024-03-07
CO2022011254A2 (es) 2022-08-19
IL295125A (en) 2022-09-01
EP4103562A1 (en) 2022-12-21
JP7703587B2 (ja) 2025-07-07
AR121341A1 (es) 2022-05-11
DOP2023000195A (es) 2023-10-31
IL295125B1 (en) 2025-05-01
JP2023067881A (ja) 2023-05-16
TW202144330A (zh) 2021-12-01
MX2025013435A (es) 2025-12-01
TW202535863A (zh) 2025-09-16
JP7230277B2 (ja) 2023-02-28
TWI873290B (zh) 2025-02-21
PE20231985A1 (es) 2023-12-12
CN116120287A (zh) 2023-05-16
DOP2022000157A (es) 2022-09-15
CN116120287B (zh) 2025-01-28
CL2022002101A1 (es) 2023-01-27
CR20250167A (es) 2025-05-23
IL320007A (en) 2025-06-01
US20210292301A1 (en) 2021-09-23
AR131110A2 (es) 2025-02-19
US20240002363A1 (en) 2024-01-04
PE20221591A1 (es) 2022-10-10
US12479827B2 (en) 2025-11-25
US11760745B2 (en) 2023-09-19
SA522440127B1 (ar) 2025-04-06
BR112022013979A2 (pt) 2022-10-11
CR20220382A (es) 2022-09-16
CL2023001244A1 (es) 2023-11-03
MX2025013436A (es) 2025-12-01
CA3168690A1 (en) 2021-08-19
KR20220141333A (ko) 2022-10-19
JP2025148369A (ja) 2025-10-07
ECSP22062410A (es) 2022-09-30
JOP20220186A1 (ar) 2023-01-30

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