EA202191619A1 - Производные (пиридин-2-ил)амина в качестве ингибиторов tgfбета r1 (alk5) для лечения злокачественных новообразований - Google Patents
Производные (пиридин-2-ил)амина в качестве ингибиторов tgfбета r1 (alk5) для лечения злокачественных новообразованийInfo
- Publication number
- EA202191619A1 EA202191619A1 EA202191619A EA202191619A EA202191619A1 EA 202191619 A1 EA202191619 A1 EA 202191619A1 EA 202191619 A EA202191619 A EA 202191619A EA 202191619 A EA202191619 A EA 202191619A EA 202191619 A1 EA202191619 A1 EA 202191619A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- treatment
- alk5
- tgf
- pyridin
- inhibitors
- Prior art date
Links
- -1 PYRIDIN-2-YL Chemical class 0.000 title 1
- 150000001412 amines Chemical class 0.000 title 1
- 230000015572 biosynthetic process Effects 0.000 title 1
- 238000005755 formation reaction Methods 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 230000003211 malignant effect Effects 0.000 title 1
- ZRKFYGHZFMAOKI-QMGMOQQFSA-N tgfbeta Chemical compound C([C@H](NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)C(C)C)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(O)=O)C1=CC=C(O)C=C1 ZRKFYGHZFMAOKI-QMGMOQQFSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 238000000034 method Methods 0.000 abstract 3
- 206010016654 Fibrosis Diseases 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 201000011510 cancer Diseases 0.000 abstract 2
- 230000004761 fibrosis Effects 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 230000002378 acidificating effect Effects 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 210000000056 organ Anatomy 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
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
- A61K31/435—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
- A61K31/435—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
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862785616P | 2018-12-27 | 2018-12-27 | |
| PCT/US2019/066993 WO2020139636A1 (en) | 2018-12-27 | 2019-12-17 | (pyridin-2-yl)amine derivatives as tgf-beta r1 (alk5) inhibitors for the treatment of cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA202191619A1 true EA202191619A1 (ru) | 2021-09-28 |
Family
ID=69185691
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA202191619A EA202191619A1 (ru) | 2018-12-27 | 2019-12-17 | Производные (пиридин-2-ил)амина в качестве ингибиторов tgfбета r1 (alk5) для лечения злокачественных новообразований |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US12102626B2 (https=) |
| EP (1) | EP3902796B1 (https=) |
| JP (2) | JP7515049B2 (https=) |
| KR (1) | KR102832376B1 (https=) |
| CN (1) | CN113348167B (https=) |
| AR (1) | AR117539A1 (https=) |
| AU (1) | AU2019417418B2 (https=) |
| BR (1) | BR112021007006A2 (https=) |
| CA (1) | CA3117838A1 (https=) |
| EA (1) | EA202191619A1 (https=) |
| ES (1) | ES2972516T3 (https=) |
| IL (1) | IL284266B2 (https=) |
| MX (1) | MX2021007738A (https=) |
| SG (1) | SG11202103457PA (https=) |
| TW (1) | TWI884934B (https=) |
| WO (1) | WO2020139636A1 (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2021259419A1 (en) | 2020-04-21 | 2022-11-10 | Lexicon Pharmaceuticals, Inc. | AAK1 inhibitors for use in treating viral infections |
| US11666575B2 (en) | 2020-04-21 | 2023-06-06 | Lexicon Pharmaceuticals, Inc. | Pyrazolo[1,5]pyrimidine-based compounds and methods of their use to treat viral infections |
| CN113214111A (zh) * | 2021-04-30 | 2021-08-06 | 上海立科化学科技有限公司 | 3-（2-氰基苯基）丙酸及4-氰基-1-茚满酮的制备方法 |
| US12263576B2 (en) | 2021-08-19 | 2025-04-01 | Hyundai Mobis Co., Ltd. | Robot system for automated assembly of modular component |
| MX2024008704A (es) * | 2022-01-14 | 2024-07-22 | Shanghai Hansoh Biomedical Co Ltd | Derivado policiclico que contiene piridina, y metodo de preparacion de este y uso de este. |
| CN121554469B (zh) * | 2026-01-23 | 2026-04-17 | 四川大学华西医院 | 一种alk5 protac化合物及其应用 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1397364B1 (en) | 2001-05-24 | 2007-07-25 | Eli Lilly And Company | Novel pyrrole derivatives as pharmaceutical agents |
| UA80571C2 (en) | 2002-11-22 | 2007-10-10 | Lilly Co Eli | Quinolinyl-pyrrolopyrazoles |
| WO2005080377A1 (ja) | 2004-02-20 | 2005-09-01 | Kirin Beer Kabushiki Kaisha | TGFβ阻害活性を有する化合物およびそれを含んでなる医薬組成物 |
| WO2009022171A1 (en) * | 2007-08-13 | 2009-02-19 | Astrazeneca Ab | Pyridinyiioxy pyridines as alk5 inhibitors |
| US8080568B1 (en) | 2010-06-29 | 2011-12-20 | Ewha University - Industry Collaboration Foundation | 2-pyridyl substituted imidazoles as therapeutic ALK5 and/or ALK4 inhibitors |
| US20140296248A1 (en) | 2011-04-04 | 2014-10-02 | Stichting het Nederlands Kanker Instiuut-Antoni van Leeuwenhoek ziekenhuis | Methods and compositions for predicting resistance to anticancer treatment |
| BR112013028430A2 (pt) * | 2011-05-04 | 2017-08-01 | Merck Sharp & Dohme | composto, composição farmacêutica, método para tratar uma doença ou condição mediada por tirosina quinase do baço (syk), e, uso de uma quantidade terapeuticamente eficiente do composto |
| EP2900665B1 (en) * | 2012-09-28 | 2018-01-03 | Merck Sharp & Dohme Corp. | Triazolyl derivatives as syk inhibitors |
| EP2934525B1 (en) * | 2012-12-21 | 2019-05-08 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors |
| WO2014155300A2 (en) * | 2013-03-28 | 2014-10-02 | Aurigene Discovery Technologies Limited | Substitued pyrimidine amine derivatives as tak-1 inhibitors |
| HRP20201384T1 (hr) | 2014-01-01 | 2020-11-27 | Medivation Technologies Llc | Spojevi i postupci njihove upotrebe |
| CN106536507B (zh) | 2014-04-08 | 2020-04-07 | 里格尔药品股份有限公司 | 作为TGF-β抑制剂的2,3-二取代的吡啶化合物及其使用方法 |
| JO3336B1 (ar) | 2014-10-07 | 2019-03-13 | Lilly Co Eli | مركبات أمينو بيريديلوكسي بيرازول |
| US10702527B2 (en) * | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| KR20180032611A (ko) | 2015-07-23 | 2018-03-30 | 브리스톨-마이어스 스큅 컴퍼니 | Tgf 베타 수용체 길항제 |
| WO2020103817A1 (zh) | 2018-11-20 | 2020-05-28 | 南京圣和药业股份有限公司 | TGF-βR1抑制剂及其应用 |
| EP3990445A4 (en) | 2019-06-25 | 2023-07-05 | InventisBio Co., Ltd. | HETEROCYCLIC COMPOUNDS, METHODS FOR THEIR PREPARATION AND THEIR METHODS OF USE |
| CN112707902B (zh) | 2020-03-23 | 2022-04-15 | 杭州阿诺生物医药科技有限公司 | TGF-β受体抑制剂 |
-
2019
- 2019-12-17 CA CA3117838A patent/CA3117838A1/en active Pending
- 2019-12-17 JP JP2021536757A patent/JP7515049B2/ja active Active
- 2019-12-17 KR KR1020217021785A patent/KR102832376B1/ko active Active
- 2019-12-17 EA EA202191619A patent/EA202191619A1/ru unknown
- 2019-12-17 IL IL284266A patent/IL284266B2/en unknown
- 2019-12-17 AU AU2019417418A patent/AU2019417418B2/en active Active
- 2019-12-17 WO PCT/US2019/066993 patent/WO2020139636A1/en not_active Ceased
- 2019-12-17 MX MX2021007738A patent/MX2021007738A/es unknown
- 2019-12-17 BR BR112021007006-0A patent/BR112021007006A2/pt unknown
- 2019-12-17 ES ES19839715T patent/ES2972516T3/es active Active
- 2019-12-17 CN CN201980086920.0A patent/CN113348167B/zh active Active
- 2019-12-17 EP EP19839715.0A patent/EP3902796B1/en active Active
- 2019-12-17 SG SG11202103457PA patent/SG11202103457PA/en unknown
- 2019-12-17 US US17/299,696 patent/US12102626B2/en active Active
- 2019-12-25 TW TW108147526A patent/TWI884934B/zh active
- 2019-12-27 AR ARP190103894A patent/AR117539A1/es unknown
-
2023
- 2023-01-17 JP JP2023005014A patent/JP2023052437A/ja active Pending
-
2024
- 2024-08-05 US US18/795,000 patent/US20240398776A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| US20220054465A1 (en) | 2022-02-24 |
| EP3902796B1 (en) | 2024-02-07 |
| EP3902796C0 (en) | 2024-02-07 |
| KR20210110316A (ko) | 2021-09-07 |
| JP7515049B2 (ja) | 2024-07-12 |
| WO2020139636A1 (en) | 2020-07-02 |
| CN113348167B (zh) | 2026-01-09 |
| SG11202103457PA (en) | 2021-05-28 |
| US20240398776A1 (en) | 2024-12-05 |
| AR117539A1 (es) | 2021-08-11 |
| MX2021007738A (es) | 2021-08-05 |
| EP3902796A1 (en) | 2021-11-03 |
| AU2019417418A1 (en) | 2021-04-15 |
| CA3117838A1 (en) | 2020-07-02 |
| CN113348167A (zh) | 2021-09-03 |
| AU2019417418B2 (en) | 2025-02-27 |
| TWI884934B (zh) | 2025-06-01 |
| JP2023052437A (ja) | 2023-04-11 |
| JP2022517730A (ja) | 2022-03-10 |
| NZ775362A (en) | 2025-02-28 |
| TW202039436A (zh) | 2020-11-01 |
| IL284266B2 (en) | 2024-06-01 |
| BR112021007006A2 (pt) | 2021-08-10 |
| ES2972516T3 (es) | 2024-06-13 |
| KR102832376B1 (ko) | 2025-07-09 |
| US12102626B2 (en) | 2024-10-01 |
| IL284266A (en) | 2021-08-31 |
| IL284266B1 (en) | 2024-02-01 |
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