CN116096719B - 作为alk5抑制剂的哒嗪基氨基衍生物 - Google Patents
作为alk5抑制剂的哒嗪基氨基衍生物Info
- Publication number
- CN116096719B CN116096719B CN202180061803.6A CN202180061803A CN116096719B CN 116096719 B CN116096719 B CN 116096719B CN 202180061803 A CN202180061803 A CN 202180061803A CN 116096719 B CN116096719 B CN 116096719B
- Authority
- CN
- China
- Prior art keywords
- chloro
- fluorophenyl
- amino
- pyridazin
- pyridin
- Prior art date
- Legal status (The legal status 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 status listed.)
- Active
Links
Classifications
-
- 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
- A61K31/50—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
- A61K31/535—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D401/02—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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
-
- 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
- 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
-
- 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
- C07D471/10—Spiro-condensed 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
- C07D487/04—Ortho-condensed 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
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (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)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP20185890.9 | 2020-07-15 | ||
| EP20185890 | 2020-07-15 | ||
| PCT/EP2021/069649 WO2022013307A1 (en) | 2020-07-15 | 2021-07-14 | Pyridazinyl amino derivatives as alk5 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN116096719A CN116096719A (zh) | 2023-05-09 |
| CN116096719B true CN116096719B (zh) | 2025-09-30 |
Family
ID=71620257
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202180061803.6A Active CN116096719B (zh) | 2020-07-15 | 2021-07-14 | 作为alk5抑制剂的哒嗪基氨基衍生物 |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US12479826B2 (https=) |
| EP (1) | EP4182308B1 (https=) |
| JP (1) | JP7686741B2 (https=) |
| KR (1) | KR20230051500A (https=) |
| CN (1) | CN116096719B (https=) |
| AR (1) | AR122986A1 (https=) |
| AU (1) | AU2021307559A1 (https=) |
| BR (1) | BR112023000588A8 (https=) |
| CA (1) | CA3184990A1 (https=) |
| DK (1) | DK4182308T3 (https=) |
| ES (1) | ES2997111T3 (https=) |
| FI (1) | FI4182308T3 (https=) |
| HR (1) | HRP20241617T1 (https=) |
| HU (1) | HUE069150T2 (https=) |
| MX (1) | MX2023000521A (https=) |
| PL (1) | PL4182308T3 (https=) |
| PT (1) | PT4182308T (https=) |
| SI (1) | SI4182308T1 (https=) |
| WO (1) | WO2022013307A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7702205B2 (ja) * | 2021-09-15 | 2025-07-03 | 株式会社東芝 | 新規アミン化合物、酸性ガス吸収剤、酸性ガスの除去方法及び酸性ガス除去 |
| CN114957331A (zh) * | 2022-04-22 | 2022-08-30 | 北京康辰药业股份有限公司 | 磷酸酯取代的环丙酰胺衍生喹唑啉类化合物的制备方法 |
| WO2024180206A1 (en) | 2023-03-02 | 2024-09-06 | Chiesi Farmaceutici S.P.A. | Pyridazinyl amino derivatives as alk5 inhibitors |
| WO2024180207A1 (en) | 2023-03-02 | 2024-09-06 | Chiesi Farmaceutici S.P.A. | Pyridazinyl amino derivatives as alk5 inhibitors |
| KR20240159754A (ko) * | 2023-04-28 | 2024-11-06 | 한국원자력의학원 | N-메틸피페라진 에탄올 카바메이트(N-methylpiperazine ethanol carbamate) 구조를 포함하는 신규 화합물 및 이의 용도 |
| WO2025132458A1 (en) | 2023-12-18 | 2025-06-26 | Chiesi Farmaceutici S.P.A. | Pyridazinyl amino derivatives as alk5 inhibitors |
| WO2025132460A1 (en) | 2023-12-18 | 2025-06-26 | Chiesi Farmaceutici S.P.A. | Pyridazinyl amino derivatives as alk5 inhibitors |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009087212A2 (en) * | 2008-01-11 | 2009-07-16 | Novartis Ag | Pyridine derivatives |
| WO2020012357A1 (en) * | 2018-07-10 | 2020-01-16 | Integral Biosciences Pvt. Ltd. | Heterocyclic compounds and methods of use |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60001229T2 (de) | 1999-04-09 | 2003-10-30 | Smithkline Beecham Corp., Philadelphia | Triarylimidazole |
| AR029803A1 (es) | 2000-02-21 | 2003-07-16 | Smithkline Beecham Plc | Imidazoles sustituidos con piridilo y composiciones farmaceuticas que las comprenden |
| GB0007405D0 (en) | 2000-03-27 | 2000-05-17 | Smithkline Beecham Corp | Compounds |
| EP1317450B1 (en) * | 2000-09-15 | 2006-11-22 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| CA2423050A1 (en) | 2000-09-20 | 2002-03-28 | Ortho-Mcneil Pharmaceutical, Inc. | Pyrazine derivatives as modulators of tyrosine kinases |
| AR039241A1 (es) | 2002-04-04 | 2005-02-16 | Biogen Inc | Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos |
| JP2006503043A (ja) * | 2002-09-10 | 2006-01-26 | サイオス インク． | ＴＧＦβ阻害剤 |
| AU2004278382B2 (en) * | 2003-09-30 | 2008-09-18 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments |
| BRPI0714409A2 (pt) | 2006-07-14 | 2013-03-12 | Novartis Ag | derivados de pirimidina como inibidores de alk-5 |
| ES2375425T3 (es) | 2007-07-26 | 2012-02-29 | Novartis Ag | Compuestos org�?nicos. |
| BRPI0817434A2 (pt) | 2007-10-17 | 2015-06-16 | Novartis Ag | Composto orgânicos |
| AR070127A1 (es) | 2008-01-11 | 2010-03-17 | Novartis Ag | Pirrolo - pirimidinas y pirrolo -piridinas |
| MX2010007604A (es) | 2008-01-11 | 2010-08-02 | Novartis Ag | Pirimidinas como inhibidores de cinasa. |
| EA201001687A1 (ru) | 2008-04-29 | 2011-06-30 | Новартис Аг | Производные имидазопиридина в качестве ингибиторов активиноподобной рецепторной киназы ( alk-4 или alk-5 ) |
| CN102596200A (zh) * | 2009-11-07 | 2012-07-18 | 默克专利有限公司 | 作为TGF-β受体激酶抑制剂的杂芳基氨基喹啉类 |
| DK2731949T3 (en) | 2011-07-13 | 2018-06-14 | Tiumbio Co Ltd | 2-PYRIDYL-SUBSTITUTED IMIDAZOLS AS ALK5 AND / OR ALK4 INHIBITORS |
| HRP20201384T1 (hr) * | 2014-01-01 | 2020-11-27 | Medivation Technologies Llc | Spojevi i postupci njihove upotrebe |
-
2021
- 2021-07-14 PT PT217431865T patent/PT4182308T/pt unknown
- 2021-07-14 CN CN202180061803.6A patent/CN116096719B/zh active Active
- 2021-07-14 FI FIEP21743186.5T patent/FI4182308T3/fi active
- 2021-07-14 WO PCT/EP2021/069649 patent/WO2022013307A1/en not_active Ceased
- 2021-07-14 MX MX2023000521A patent/MX2023000521A/es unknown
- 2021-07-14 PL PL21743186.5T patent/PL4182308T3/pl unknown
- 2021-07-14 ES ES21743186T patent/ES2997111T3/es active Active
- 2021-07-14 US US18/014,764 patent/US12479826B2/en active Active
- 2021-07-14 AU AU2021307559A patent/AU2021307559A1/en active Pending
- 2021-07-14 HU HUE21743186A patent/HUE069150T2/hu unknown
- 2021-07-14 SI SI202130217T patent/SI4182308T1/sl unknown
- 2021-07-14 CA CA3184990A patent/CA3184990A1/en active Pending
- 2021-07-14 EP EP21743186.5A patent/EP4182308B1/en active Active
- 2021-07-14 BR BR112023000588A patent/BR112023000588A8/pt unknown
- 2021-07-14 HR HRP20241617TT patent/HRP20241617T1/hr unknown
- 2021-07-14 DK DK21743186.5T patent/DK4182308T3/da active
- 2021-07-14 KR KR1020237005127A patent/KR20230051500A/ko not_active Withdrawn
- 2021-07-14 JP JP2023502861A patent/JP7686741B2/ja active Active
- 2021-07-15 AR ARP210101996A patent/AR122986A1/es unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009087212A2 (en) * | 2008-01-11 | 2009-07-16 | Novartis Ag | Pyridine derivatives |
| WO2020012357A1 (en) * | 2018-07-10 | 2020-01-16 | Integral Biosciences Pvt. Ltd. | Heterocyclic compounds and methods of use |
Also Published As
| Publication number | Publication date |
|---|---|
| DK4182308T3 (da) | 2024-10-21 |
| BR112023000588A2 (pt) | 2023-01-31 |
| ES2997111T3 (en) | 2025-03-19 |
| AR122986A1 (es) | 2022-10-19 |
| TW202216677A (zh) | 2022-05-01 |
| HRP20241617T1 (hr) | 2025-01-31 |
| CA3184990A1 (en) | 2022-01-20 |
| WO2022013307A1 (en) | 2022-01-20 |
| PT4182308T (pt) | 2024-12-04 |
| AU2021307559A1 (en) | 2023-02-16 |
| JP2023533849A (ja) | 2023-08-04 |
| KR20230051500A (ko) | 2023-04-18 |
| US12479826B2 (en) | 2025-11-25 |
| BR112023000588A8 (pt) | 2023-05-09 |
| JP7686741B2 (ja) | 2025-06-02 |
| EP4182308A1 (en) | 2023-05-24 |
| US20240018122A1 (en) | 2024-01-18 |
| CN116096719A (zh) | 2023-05-09 |
| SI4182308T1 (sl) | 2025-04-30 |
| FI4182308T3 (fi) | 2024-12-07 |
| HUE069150T2 (hu) | 2025-02-28 |
| PL4182308T3 (pl) | 2025-01-07 |
| EP4182308B1 (en) | 2024-09-04 |
| MX2023000521A (es) | 2023-02-13 |
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