MX2021007738A - Derivados de (piridin-2-il)amina como inhibidores de tgf-beta r1 (alk5) para el tratamiento de cancer. - Google Patents
Derivados de (piridin-2-il)amina como inhibidores de tgf-beta r1 (alk5) para el tratamiento de cancer.Info
- Publication number
- MX2021007738A MX2021007738A MX2021007738A MX2021007738A MX2021007738A MX 2021007738 A MX2021007738 A MX 2021007738A MX 2021007738 A MX2021007738 A MX 2021007738A MX 2021007738 A MX2021007738 A MX 2021007738A MX 2021007738 A MX2021007738 A MX 2021007738A
- Authority
- MX
- Mexico
- Prior art keywords
- cancer
- treatment
- alk5
- tgf
- pyridin
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title abstract 3
- 201000011510 cancer Diseases 0.000 title abstract 3
- ICSNLGPSRYBMBD-UHFFFAOYSA-N 2-aminopyridine Chemical class NC1=CC=CC=N1 ICSNLGPSRYBMBD-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 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
- 206010016654 Fibrosis 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
- 230000035755 proliferation 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
-
- 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
- A61K31/435—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
- 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
Abstract
La presente invención está relacionada con compuestos, composiciones y métodos farmacéuticos, especialmente debido a que están relacionados con composiciones y métodos para el tratamiento y/o la prevención de un trastorno de proliferación relacionado con la actividad de TGFßR1, tal como el cáncer o la fibrosis. La invención proporciona compuestos de la Fórmula (I) y de la Fórmula (II) como se describe con más detalle en la presente que tienen una fracción ácida que realza la especificidad del tejido para los tejidos y los órganos objetivo. (ver Fórmulas) Fórmula (I) Fórmula (II) La invención incluye composiciones farmacéuticas, combinaciones farmacéuticas y métodos de uso de estos compuestos para tratar afecciones que incluyen el cáncer o la fibrosis.
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 |
|---|---|
| MX2021007738A true MX2021007738A (es) | 2021-08-05 |
Family
ID=69185691
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2021007738A MX2021007738A (es) | 2018-12-27 | 2019-12-17 | Derivados de (piridin-2-il)amina como inhibidores de tgf-beta r1 (alk5) para el tratamiento de cancer. |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US20220054465A1 (es) |
| EP (1) | EP3902796B1 (es) |
| JP (2) | JP2022517730A (es) |
| KR (1) | KR20210110316A (es) |
| CN (1) | CN113348167A (es) |
| AR (1) | AR117539A1 (es) |
| AU (1) | AU2019417418A1 (es) |
| BR (1) | BR112021007006A2 (es) |
| CA (1) | CA3117838A1 (es) |
| EA (1) | EA202191619A1 (es) |
| IL (1) | IL284266B1 (es) |
| MX (1) | MX2021007738A (es) |
| SG (1) | SG11202103457PA (es) |
| TW (1) | TW202039436A (es) |
| WO (1) | WO2020139636A1 (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2023522689A (ja) | 2020-04-21 | 2023-05-31 | レクシコン ファーマシューティカルズ インコーポレイテッド | ＣｏＶ－２２９Ｅ又はＣｏＶ－ＯＣ４３コロナウイルス感染症の治療において使用される４－（３－（ピリジン－３－イル）ピラゾロ［１，５－ａ］ピリミジン－５－イル）ピペラジン |
| CA3175970A1 (en) | 2020-04-21 | 2021-10-28 | Suma GOPINATHAN | Aak1 inhibitors for use in treating 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 |
| US20230054602A1 (en) | 2021-08-19 | 2023-02-23 | Hyundai Mobis Co., Ltd. | Robot system for automated assembly of modular component |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1951939A (zh) | 2001-05-24 | 2007-04-25 | 伊莱利利公司 | 作为药物的新的吡唑衍生物 |
| UA80571C2 (en) | 2002-11-22 | 2007-10-10 | Lilly Co Eli | Quinolinyl-pyrrolopyrazoles |
| TW200538120A (en) | 2004-02-20 | 2005-12-01 | Kirin Brewery | Compound having TGF-beta inhibitory activity and pharmaceutical composition containing same |
| 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 |
| AU2012240240A1 (en) | 2011-04-04 | 2013-05-09 | Netherlands Cancer Institute | Methods and compositions for predicting resistance to anticancer treatment with protein kinase inhibitors |
| RU2612217C2 (ru) * | 2011-05-04 | 2017-03-03 | Мерк Шарп И Доум Корп. | Аминопиридинсодержащие ингибиторы тирозинкиназы селезенки (syk) |
| US9586931B2 (en) * | 2012-09-28 | 2017-03-07 | 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 |
| TWI582083B (zh) * | 2014-10-07 | 2017-05-11 | 美國禮來大藥廠 | 胺基吡啶基氧基吡唑化合物 |
| WO2016201370A1 (en) * | 2015-06-12 | 2016-12-15 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
-
2019
- 2019-12-17 US US17/299,696 patent/US20220054465A1/en active Pending
- 2019-12-17 WO PCT/US2019/066993 patent/WO2020139636A1/en active Application Filing
- 2019-12-17 KR KR1020217021785A patent/KR20210110316A/ko unknown
- 2019-12-17 CN CN201980086920.0A patent/CN113348167A/zh active Pending
- 2019-12-17 CA CA3117838A patent/CA3117838A1/en active Pending
- 2019-12-17 IL IL284266A patent/IL284266B1/en unknown
- 2019-12-17 SG SG11202103457PA patent/SG11202103457PA/en unknown
- 2019-12-17 EP EP19839715.0A patent/EP3902796B1/en active Active
- 2019-12-17 JP JP2021536757A patent/JP2022517730A/ja active Pending
- 2019-12-17 BR BR112021007006-0A patent/BR112021007006A2/pt unknown
- 2019-12-17 MX MX2021007738A patent/MX2021007738A/es unknown
- 2019-12-17 AU AU2019417418A patent/AU2019417418A1/en active Pending
- 2019-12-17 EA EA202191619A patent/EA202191619A1/ru unknown
- 2019-12-25 TW TW108147526A patent/TW202039436A/zh unknown
- 2019-12-27 AR ARP190103894A patent/AR117539A1/es unknown
-
2023
- 2023-01-17 JP JP2023005014A patent/JP2023052437A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| IL284266A (en) | 2021-08-31 |
| IL284266B1 (en) | 2024-02-01 |
| JP2022517730A (ja) | 2022-03-10 |
| SG11202103457PA (en) | 2021-05-28 |
| KR20210110316A (ko) | 2021-09-07 |
| EP3902796C0 (en) | 2024-02-07 |
| TW202039436A (zh) | 2020-11-01 |
| AU2019417418A1 (en) | 2021-04-15 |
| EA202191619A1 (ru) | 2021-09-28 |
| AR117539A1 (es) | 2021-08-11 |
| BR112021007006A2 (pt) | 2021-08-10 |
| CA3117838A1 (en) | 2020-07-02 |
| WO2020139636A1 (en) | 2020-07-02 |
| CN113348167A (zh) | 2021-09-03 |
| EP3902796B1 (en) | 2024-02-07 |
| JP2023052437A (ja) | 2023-04-11 |
| EP3902796A1 (en) | 2021-11-03 |
| US20220054465A1 (en) | 2022-02-24 |
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