CN117355521A - 血浆激肽释放酶的杂芳基抑制剂 - Google Patents

血浆激肽释放酶的杂芳基抑制剂 Download PDF

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Publication number
CN117355521A
CN117355521A CN202280022472.XA CN202280022472A CN117355521A CN 117355521 A CN117355521 A CN 117355521A CN 202280022472 A CN202280022472 A CN 202280022472A CN 117355521 A CN117355521 A CN 117355521A
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CN
China
Prior art keywords
pyridin
methyl
carboxamide
cyclopropane
amino
Prior art date
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Pending
Application number
CN202280022472.XA
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English (en)
Chinese (zh)
Inventor
N·帕帕约安努
J·M·特拉文斯
S·J·芬克
J·M·埃拉德
A·雷
J·A·斯宾塞
S·S·兰金
R·S·L·查普曼
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Takeda Pharmaceutical Co Ltd
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Takeda Pharmaceutical Co Ltd
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Filing date
Publication date
Application filed by Takeda Pharmaceutical Co Ltd filed Critical Takeda Pharmaceutical Co Ltd
Publication of CN117355521A publication Critical patent/CN117355521A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • C07D487/08—Bridged systems
    • 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
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN202280022472.XA 2021-03-17 2022-03-16 血浆激肽释放酶的杂芳基抑制剂 Pending CN117355521A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202163162468P 2021-03-17 2021-03-17
US63/162,468 2021-03-17
PCT/US2022/020482 WO2022197758A1 (en) 2021-03-17 2022-03-16 Heteroaryl inhibitors of plasma kallikrein

Publications (1)

Publication Number Publication Date
CN117355521A true CN117355521A (zh) 2024-01-05

Family

ID=81328275

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202280022472.XA Pending CN117355521A (zh) 2021-03-17 2022-03-16 血浆激肽释放酶的杂芳基抑制剂

Country Status (10)

Country Link
US (1) US20240228488A1 (https=)
EP (2) EP4585265A3 (https=)
JP (1) JP2024516073A (https=)
KR (1) KR20240004296A (https=)
CN (1) CN117355521A (https=)
AU (1) AU2022240596A1 (https=)
BR (1) BR112023018619A2 (https=)
CA (1) CA3208243A1 (https=)
MX (1) MX2023011014A (https=)
WO (1) WO2022197758A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117396473A (zh) * 2021-03-17 2024-01-12 武田药品工业株式会社 血浆激肽释放酶的咪唑并吡啶基抑制剂

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20200143376A (ko) 2018-03-13 2020-12-23 샤이어 휴먼 지네틱 테라피즈 인크. 혈장 칼리크레인 억제제로서의 치환된 이미다조피리딘 및 이의 용도
CN114667289B (zh) 2019-09-18 2025-08-26 武田药品工业有限公司 杂芳基血浆激肽释放酶抑制剂
EP4031547B1 (en) 2019-09-18 2024-07-17 Takeda Pharmaceutical Company Limited Plasma kallikrein inhibitors and uses thereof
BR112023018619A2 (pt) 2021-03-17 2023-11-28 Takeda Pharmaceuticals Co Inibidores de heteroaril de calicreína plasmática
JP2025531158A (ja) * 2022-09-21 2025-09-19 武田薬品工業株式会社 シクロプロパンカルボン酸の合成
KR20260029377A (ko) * 2023-06-29 2026-03-04 테라닙 인코포레이티드 암 및 염증성 질환 치료에 사용하기 위한 이미다조[1,2-α]피리딘 화합물 및 그 화합물의 제조 방법
CN117069662A (zh) * 2023-10-17 2023-11-17 峰成医药科技(天津)有限公司 一种4,6-二氯-2-（二氟甲基）嘧啶的合成方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016083816A1 (en) * 2014-11-27 2016-06-02 Kalvista Pharmaceuticals Limited N-((heteroarylmethyl)-heteroaryl-carboxamide derivatives as plasma kallikrein inhibitors
US20180194780A1 (en) * 2015-06-12 2018-07-12 Global Blood Therapeutics, Inc. Bridged bicyclic kallikrein inhibitors
CN112135825A (zh) * 2018-03-13 2020-12-25 夏尔人类遗传性治疗公司 血浆激肽释放酶抑制剂及其用途

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4911920A (en) 1986-07-30 1990-03-27 Alcon Laboratories, Inc. Sustained release, comfort formulation for glaucoma therapy
FR2588189B1 (fr) 1985-10-03 1988-12-02 Merck Sharp & Dohme Composition pharmaceutique de type a transition de phase liquide-gel
ATE141502T1 (de) 1991-01-15 1996-09-15 Alcon Lab Inc Verwendung von karrageenan in topischen ophthalmologischen zusammensetzungen
US5212162A (en) 1991-03-27 1993-05-18 Alcon Laboratories, Inc. Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions
US6309853B1 (en) 1994-08-17 2001-10-30 The Rockfeller University Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof
BR112023018619A2 (pt) 2021-03-17 2023-11-28 Takeda Pharmaceuticals Co Inibidores de heteroaril de calicreína plasmática

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016083816A1 (en) * 2014-11-27 2016-06-02 Kalvista Pharmaceuticals Limited N-((heteroarylmethyl)-heteroaryl-carboxamide derivatives as plasma kallikrein inhibitors
US20180194780A1 (en) * 2015-06-12 2018-07-12 Global Blood Therapeutics, Inc. Bridged bicyclic kallikrein inhibitors
CN112135825A (zh) * 2018-03-13 2020-12-25 夏尔人类遗传性治疗公司 血浆激肽释放酶抑制剂及其用途

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117396473A (zh) * 2021-03-17 2024-01-12 武田药品工业株式会社 血浆激肽释放酶的咪唑并吡啶基抑制剂

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WO2022197758A1 (en) 2022-09-22
JP2024516073A (ja) 2024-04-12
AU2022240596A1 (en) 2023-10-19
KR20240004296A (ko) 2024-01-11
BR112023018619A2 (pt) 2023-11-28
EP4308230A1 (en) 2024-01-24
EP4585265A2 (en) 2025-07-16
EP4585265A3 (en) 2025-10-15
US20240228488A1 (en) 2024-07-11
CA3208243A1 (en) 2022-09-22
MX2023011014A (es) 2023-12-06

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