PE20160204A1 - Compuestos y composiciones como inhibidores de la mek - Google Patents
Compuestos y composiciones como inhibidores de la mekInfo
- Publication number
- PE20160204A1 PE20160204A1 PE2016000238A PE2016000238A PE20160204A1 PE 20160204 A1 PE20160204 A1 PE 20160204A1 PE 2016000238 A PE2016000238 A PE 2016000238A PE 2016000238 A PE2016000238 A PE 2016000238A PE 20160204 A1 PE20160204 A1 PE 20160204A1
- Authority
- PE
- Peru
- Prior art keywords
- methyl
- compounds
- compositions
- mek inhibitors
- imidazo
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 239000001257 hydrogen Substances 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- WZZBNLYBHUDSHF-DHLKQENFSA-N 1-[(3s,4s)-4-[8-(2-chloro-4-pyrimidin-2-yloxyphenyl)-7-fluoro-2-methylimidazo[4,5-c]quinolin-1-yl]-3-fluoropiperidin-1-yl]-2-hydroxyethanone Chemical compound CC1=NC2=CN=C3C=C(F)C(C=4C(=CC(OC=5N=CC=CN=5)=CC=4)Cl)=CC3=C2N1[C@H]1CCN(C(=O)CO)C[C@@H]1F WZZBNLYBHUDSHF-DHLKQENFSA-N 0.000 abstract 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- -1 cyano-methyl Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
Classifications
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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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines 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
- A61K31/495—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
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente invencion se relaciona con compuestos de la formula I: Capaces de inhibir la actividad de MEK. Donde N es 0, 1, 2 o 3, R1 es i), ii), etc. R2 es cloro, metilo, etc. R3a es ciano-metilo, 2-hidroxi-etilo, etc. R4 es hidrogeno, halo, etc. R5 es hidrogeno y metilo. Son compuestos preferidos: 1-((3S,4S)- 4-(8-(2-cloro-4-(pirimidin-2-iloxi)fenil)-7-fluoro-2-metil-1H- imidazo[4,5-c]quinolin-1 il)-3-fluoropiperidin-1-il)-2Hidroxietanona; 8-(2-cloro-4-(pirimidim- 2- iloxi)fenil)- 7-fluoro-1-(1- (2-metoxietil)piperidin-4-il)-2-metil-1H-imidazo[4,5-c]quinolina. La invencion proporciona ademas un procedimiento para la preparacion de compuestos que son utiles en el manejo de enfermedades hiperproliferitivas similares al cancer
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN2418DE2013 | 2013-08-14 | ||
| IN1686DE2014 | 2014-06-24 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20160204A1 true PE20160204A1 (es) | 2016-04-27 |
Family
ID=51844790
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2016000238A PE20160204A1 (es) | 2013-08-14 | 2014-08-14 | Compuestos y composiciones como inhibidores de la mek |
Country Status (33)
| Country | Link |
|---|---|
| US (3) | US9227969B2 (es) |
| EP (1) | EP3033343B1 (es) |
| JP (1) | JP6473453B2 (es) |
| KR (1) | KR102354208B1 (es) |
| CN (1) | CN105473588B (es) |
| AP (1) | AP2016008981A0 (es) |
| AU (1) | AU2014307593C1 (es) |
| BR (1) | BR112016001783B1 (es) |
| CA (1) | CA2921300C (es) |
| CL (1) | CL2016000150A1 (es) |
| CR (1) | CR20160072A (es) |
| CU (1) | CU20160020A7 (es) |
| DO (1) | DOP2016000047A (es) |
| EA (1) | EA029093B1 (es) |
| ES (1) | ES2714718T3 (es) |
| GE (1) | GEP201706725B (es) |
| HK (1) | HK1219271A1 (es) |
| IL (1) | IL243349A0 (es) |
| MX (1) | MX359401B (es) |
| NI (1) | NI201600014A (es) |
| PE (1) | PE20160204A1 (es) |
| PH (1) | PH12016500003A1 (es) |
| PL (1) | PL3033343T3 (es) |
| PT (1) | PT3033343T (es) |
| SG (1) | SG11201510727VA (es) |
| SV (1) | SV2016005153A (es) |
| TN (1) | TN2015000574A1 (es) |
| TR (1) | TR201902709T4 (es) |
| TW (1) | TW201536782A (es) |
| UA (1) | UA116566C2 (es) |
| UY (1) | UY35704A (es) |
| WO (1) | WO2015022662A1 (es) |
| ZA (1) | ZA201509337B (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9227969B2 (en) * | 2013-08-14 | 2016-01-05 | Novartis Ag | Compounds and compositions as inhibitors of MEK |
| AU2015240465B2 (en) | 2014-04-04 | 2020-02-27 | Del Mar Pharmaceuticals | Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer |
| CA2975116C (en) | 2015-01-30 | 2022-10-11 | Biomed Valley Discoveries, Inc. | Crystalline c21h22c12n4o2 malonate |
| NZ772411A (en) * | 2015-01-30 | 2022-05-27 | Vertex Pharma | Crystalline forms of c21h22ci2n4o2 |
| CN113200961B (zh) * | 2015-06-15 | 2023-12-22 | 阿沙纳生物科学公司 | Erk1与erk2的杂环抑制剂及其在癌症治疗中的应用 |
| TWI674261B (zh) | 2017-02-17 | 2019-10-11 | 美商英能腫瘤免疫股份有限公司 | Nlrp3 調節劑 |
| US20210380683A1 (en) * | 2018-04-12 | 2021-12-09 | The Methodist Hospital System | Modulation of irf-4 and uses thereof |
| BR112021018168B1 (pt) | 2019-03-21 | 2023-11-28 | Onxeo | Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer |
| CN110141657B (zh) * | 2019-05-17 | 2023-01-17 | 温州医科大学附属第二医院、温州医科大学附属育英儿童医院 | 一种表皮生长因子脂质体及其制备方法 |
| PE20221417A1 (es) | 2019-09-16 | 2022-09-20 | Novartis Ag | Degradadores bifuncionales de brd9 y sus metodos de uso |
| CN114761006A (zh) | 2019-11-08 | 2022-07-15 | Inserm(法国国家健康医学研究院) | 对激酶抑制剂产生耐药性的癌症的治疗方法 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| US12280055B2 (en) | 2021-05-27 | 2025-04-22 | Mirati Therapeutics, Inc. | Combination therapies |
| JP2025509969A (ja) * | 2022-03-24 | 2025-04-11 | バイオメッド バレー ディスカバリーズ，インコーポレイティド | Ｅｒｋのピロール阻害剤の重水素化アナログ、その合成およびその中間体 |
| WO2024049929A2 (en) * | 2022-08-30 | 2024-03-07 | Pannex Therapeutics Inc. | Pannexin-1 modulators and methods of treating disorders in which pannexin-1 is implicated |
| CN117800964A (zh) * | 2022-09-30 | 2024-04-02 | 四川大学 | PI3K/m-TOR抑制剂及其应用 |
| WO2025073765A1 (en) | 2023-10-03 | 2025-04-10 | Institut National de la Santé et de la Recherche Médicale | Methods of prognosis and treatment of patients suffering from melanoma |
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