AR123543A1 - DERIVADOS DE 2-(3-PIRIDIN-2-IL-4-QUINOLIN-4-IL-PIRAZOL-1-IL)-ACETAMIDA COMO INHIBIDORES DEL RECEPTOR DEL FACTOR DE CRECIMIENTO TRANSFORMANTE b-1 / ALK5 - Google Patents
DERIVADOS DE 2-(3-PIRIDIN-2-IL-4-QUINOLIN-4-IL-PIRAZOL-1-IL)-ACETAMIDA COMO INHIBIDORES DEL RECEPTOR DEL FACTOR DE CRECIMIENTO TRANSFORMANTE b-1 / ALK5Info
- Publication number
- AR123543A1 AR123543A1 ARP210102591A ARP210102591A AR123543A1 AR 123543 A1 AR123543 A1 AR 123543A1 AR P210102591 A ARP210102591 A AR P210102591A AR P210102591 A ARP210102591 A AR P210102591A AR 123543 A1 AR123543 A1 AR 123543A1
- Authority
- AR
- Argentina
- Prior art keywords
- branched
- linear
- group
- alkyl
- group selected
- Prior art date
Links
- 102000009618 Transforming Growth Factors Human genes 0.000 title abstract 3
- 108010009583 Transforming Growth Factors Proteins 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 7
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- 102000005962 receptors Human genes 0.000 abstract 2
- 108020003175 receptors Proteins 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 abstract 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 abstract 1
- TUWGMOZGLKKBJJ-UHFFFAOYSA-N NC(CN(C=C1C2=CC=NC3=CC=CC=C23)N=C1C1=NC=CC=C1)=O Chemical class NC(CN(C=C1C2=CC=NC3=CC=CC=C23)N=C1C1=NC=CC=C1)=O TUWGMOZGLKKBJJ-UHFFFAOYSA-N 0.000 abstract 1
- 102000014172 Transforming Growth Factor-beta Type I Receptor Human genes 0.000 abstract 1
- 108010011702 Transforming Growth Factor-beta Type I Receptor Proteins 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 230000001668 ameliorated effect Effects 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- -1 carbon atom hydrogen Chemical class 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000002500 effect on skin Effects 0.000 abstract 1
- 230000003176 fibrotic effect Effects 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 208000036971 interstitial lung disease 2 Diseases 0.000 abstract 1
- 201000005202 lung cancer Diseases 0.000 abstract 1
- 208000020816 lung neoplasm Diseases 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Chemical group 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 230000003389 potentiating effect Effects 0.000 abstract 1
- 208000023504 respiratory system disease Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
Classifications
-
- 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
- A61K31/47—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
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- 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
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pulmonology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP20382861.1A EP3978487A1 (en) | 2020-09-30 | 2020-09-30 | 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-acetamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR123543A1 true AR123543A1 (es) | 2022-12-14 |
Family
ID=72744716
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP210102591A AR123543A1 (es) | 2020-09-30 | 2021-09-17 | DERIVADOS DE 2-(3-PIRIDIN-2-IL-4-QUINOLIN-4-IL-PIRAZOL-1-IL)-ACETAMIDA COMO INHIBIDORES DEL RECEPTOR DEL FACTOR DE CRECIMIENTO TRANSFORMANTE b-1 / ALK5 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US12577230B2 (https=) |
| EP (2) | EP3978487A1 (https=) |
| JP (1) | JP7752684B2 (https=) |
| KR (1) | KR20230079027A (https=) |
| CN (1) | CN116323601A (https=) |
| AR (1) | AR123543A1 (https=) |
| AU (1) | AU2021353965A1 (https=) |
| BR (1) | BR112023004612A2 (https=) |
| CA (1) | CA3196108A1 (https=) |
| ES (1) | ES3029607T1 (https=) |
| IL (1) | IL301663B1 (https=) |
| MX (1) | MX2023002900A (https=) |
| PH (1) | PH12023550777A1 (https=) |
| WO (1) | WO2022069509A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4065572A1 (en) | 2019-11-28 | 2022-10-05 | Origo Biopharma, S.L. | Benzylamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5 |
| WO2026017797A1 (en) | 2024-07-17 | 2026-01-22 | Agomab Spain S.L.U. | Crystalline forms |
| 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 (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6514977B1 (en) * | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| PL337020A1 (en) * | 1997-05-22 | 2000-07-31 | Searle & Co | Substituted pyrazoles as kinase p38 inhibitors |
| JP2004521915A (ja) * | 2001-02-02 | 2004-07-22 | グラクソ グループ リミテッド | Ｔｇｆ過剰発現に対するピラゾール誘導体 |
| HRP20050247A2 (en) | 2002-09-18 | 2005-10-31 | Pfizer Products Inc. | Pyrazole derivatives as transforming growth factor (tgf) inhibitors |
| WO2004026302A1 (en) | 2002-09-19 | 2004-04-01 | Eli Lilly And Company | Methods of inhibiting tgf beta with substituted pyrazoles |
| CL2004000234A1 (es) | 2003-02-12 | 2005-04-15 | Biogen Idec Inc | Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid |
| WO2007005951A2 (en) * | 2005-07-05 | 2007-01-11 | Aryx Therapeutics, Inc. | Stereoisomeric pyridyl and pyridonyl compounds and methods for the treatment of gastrointestinal and central nervous system disorders |
| CN102056907B (zh) * | 2008-04-04 | 2014-12-31 | 武田药品工业株式会社 | 杂环衍生物及其用途 |
| US8937150B2 (en) | 2009-06-11 | 2015-01-20 | Abbvie Inc. | Anti-viral compounds |
| AR079545A1 (es) | 2009-12-21 | 2012-02-01 | Bayer Cropscience Ag | Tienilpiri(mi)dinilazol |
| DK2731949T3 (en) * | 2011-07-13 | 2018-06-14 | Tiumbio Co Ltd | 2-PYRIDYL-SUBSTITUTED IMIDAZOLS AS ALK5 AND / OR ALK4 INHIBITORS |
| ES2579832T3 (es) | 2011-10-14 | 2016-08-17 | Bristol-Myers Squibb Company | Compuestos de tetrahidroisoquinolina sustituida como inhibidores del factor XIa |
| WO2016172631A2 (en) | 2015-04-24 | 2016-10-27 | President And Fellows Of Harvard College | Substrate selective inhibitors of insulin-degrading enzyme (ide) and uses thereof |
| JP2021518855A (ja) | 2018-03-02 | 2021-08-05 | ユニヴェルシテ ド ローザンヌ | Ｗｎｔシグナル伝達経路阻害剤としてのピラゾール誘導体 |
| US11945803B2 (en) | 2018-08-07 | 2024-04-02 | Tosk, Inc. | Modulators of RAS GTPase |
| CN110433164A (zh) | 2019-08-15 | 2019-11-12 | 南开大学 | TGF-beta受体分子抑制剂在治疗小鼠动物模型中急性髓系白血病的应用 |
| EP4065572A1 (en) | 2019-11-28 | 2022-10-05 | Origo Biopharma, S.L. | Benzylamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5 |
-
2020
- 2020-09-30 EP EP20382861.1A patent/EP3978487A1/en not_active Withdrawn
-
2021
- 2021-09-17 AR ARP210102591A patent/AR123543A1/es unknown
- 2021-09-29 KR KR1020237008242A patent/KR20230079027A/ko active Pending
- 2021-09-29 ES ES21786169T patent/ES3029607T1/es active Pending
- 2021-09-29 MX MX2023002900A patent/MX2023002900A/es unknown
- 2021-09-29 IL IL301663A patent/IL301663B1/en unknown
- 2021-09-29 AU AU2021353965A patent/AU2021353965A1/en active Pending
- 2021-09-29 CA CA3196108A patent/CA3196108A1/en active Pending
- 2021-09-29 BR BR112023004612A patent/BR112023004612A2/pt unknown
- 2021-09-29 CN CN202180066883.4A patent/CN116323601A/zh active Pending
- 2021-09-29 PH PH1/2023/550777A patent/PH12023550777A1/en unknown
- 2021-09-29 US US18/246,903 patent/US12577230B2/en active Active
- 2021-09-29 JP JP2023519608A patent/JP7752684B2/ja active Active
- 2021-09-29 EP EP21786169.9A patent/EP4222149A1/en active Pending
- 2021-09-29 WO PCT/EP2021/076730 patent/WO2022069509A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| PH12023550777A1 (en) | 2023-11-20 |
| IL301663B1 (en) | 2026-01-01 |
| ES3029607T1 (en) | 2025-06-24 |
| CN116323601A (zh) | 2023-06-23 |
| BR112023004612A2 (pt) | 2023-04-11 |
| MX2023002900A (es) | 2023-05-25 |
| EP3978487A1 (en) | 2022-04-06 |
| AU2021353965A1 (en) | 2023-04-27 |
| US12577230B2 (en) | 2026-03-17 |
| JP2023544716A (ja) | 2023-10-25 |
| IL301663A (en) | 2023-05-01 |
| JP7752684B2 (ja) | 2025-10-10 |
| AU2021353965A9 (en) | 2024-08-01 |
| US20230373966A1 (en) | 2023-11-23 |
| CA3196108A1 (en) | 2022-04-07 |
| WO2022069509A1 (en) | 2022-04-07 |
| EP4222149A1 (en) | 2023-08-09 |
| KR20230079027A (ko) | 2023-06-05 |
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