BR112017026159A2 - inibidores heterocíclicos de erk1 e erk2 e seu uso no tratamento de câncer - Google Patents
inibidores heterocíclicos de erk1 e erk2 e seu uso no tratamento de câncerInfo
- Publication number
- BR112017026159A2 BR112017026159A2 BR112017026159-6A BR112017026159A BR112017026159A2 BR 112017026159 A2 BR112017026159 A2 BR 112017026159A2 BR 112017026159 A BR112017026159 A BR 112017026159A BR 112017026159 A2 BR112017026159 A2 BR 112017026159A2
- Authority
- BR
- Brazil
- Prior art keywords
- compounds
- erk1
- heterocyclic
- cancer treatment
- erk2 inhibitors
- Prior art date
Links
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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
-
- 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
- A61K31/44—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
- A61K31/495—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
- 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
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (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)
- Plural Heterocyclic Compounds (AREA)
Abstract
a presente invenção refere-se a novos compostos heterocíclicos e sais farmaceuticamente aceitáveis dos mesmos. também são providos métodos para preparar esses compostos. esses compostos são úteis para inibir erk1/2. com a administração a um paciente que necessita de uma quantidade terapeuticamente eficaz de um ou mais dos compostos de fórmula (i), em que x, y, z, j, m e r1 a r8 são definidos no presente documento, esses compostos são eficazes no tratamento de condições associadas com a desregulação da via ras/raf/mek/erk. uma variedade de condições pode ser tratada usando esses compostos e inclui doenças que são caracterizadas por proliferação celular anormal. em uma modalidade, a doença é câncer.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562175756P | 2015-06-15 | 2015-06-15 | |
US62/175,756 | 2015-06-15 | ||
PCT/US2016/037697 WO2016205418A1 (en) | 2015-06-15 | 2016-06-15 | Heterocyclic inhibitors of erk1 and erk2 and their use in the treatment of cancer |
Publications (1)
Publication Number | Publication Date |
---|---|
BR112017026159A2 true BR112017026159A2 (pt) | 2018-08-14 |
Family
ID=56497830
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112017026159-6A BR112017026159A2 (pt) | 2015-06-15 | 2016-06-15 | inibidores heterocíclicos de erk1 e erk2 e seu uso no tratamento de câncer |
Country Status (18)
Country | Link |
---|---|
US (5) | US10751332B2 (pt) |
EP (2) | EP3842429B1 (pt) |
JP (2) | JP6909729B2 (pt) |
KR (2) | KR102644798B1 (pt) |
CN (2) | CN107922387A (pt) |
AU (2) | AU2016280717C1 (pt) |
BR (1) | BR112017026159A2 (pt) |
CA (1) | CA2986587C (pt) |
DK (2) | DK3842429T3 (pt) |
ES (2) | ES2968007T3 (pt) |
FI (1) | FI3307727T3 (pt) |
IL (1) | IL255613B (pt) |
MX (2) | MX2017014584A (pt) |
PL (1) | PL3842429T3 (pt) |
PT (2) | PT3842429T (pt) |
RU (1) | RU2017139727A (pt) |
WO (1) | WO2016205418A1 (pt) |
ZA (1) | ZA201707526B (pt) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP3842429B1 (en) | 2015-06-15 | 2022-09-07 | Asana BioSciences, LLC | Heterocyclic inhibitors of erk1 and erk2 and their use in the treatment of cancer |
MX2018004643A (es) | 2015-10-21 | 2018-08-01 | Otsuka Pharma Co Ltd | Compuestos de benzolactama como inhibidores de la proteina cinasa. |
GB201706327D0 (en) * | 2017-04-20 | 2017-06-07 | Otsuka Pharma Co Ltd | A pharmaceutical compound |
US20210085663A1 (en) * | 2017-05-16 | 2021-03-25 | Biomed Valley Discoveries, Inc. | Compositions and methods for treating cancer with atypical braf mutations |
JP2021525783A (ja) * | 2018-06-08 | 2021-09-27 | 貝達薬業股▲ふん▼有限公司Betta Pharmaceuticals Co.,Ltd | Erk阻害剤及びその使用 |
CN109608444B (zh) * | 2018-11-27 | 2022-02-11 | 中国药科大学 | 含异吲哚啉酮的erk抑制剂及其制备方法与用途 |
TW202102511A (zh) | 2019-03-28 | 2021-01-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 噻吩并雜環類衍生物、其製備方法及其在醫藥上的應用 |
JP2022528083A (ja) * | 2019-03-29 | 2022-06-08 | ジエンス ヘンルイ メデイシンカンパニー リミテッド | ピロロ複素環式誘導体、この誘導体のための調製方法及び医学におけるこの誘導体の用途 |
EP4051264A1 (en) * | 2019-10-28 | 2022-09-07 | Asana BioSciences, LLC | Improved methods, kits, compositions and dosing regimens for the use of heterocyclic inhibitors of erk1 and erk2 |
CN111620860B (zh) * | 2020-06-23 | 2023-02-03 | 济南健丰化工有限公司 | 一种福瑞塞替的制备方法 |
CN114315837B (zh) * | 2020-09-29 | 2023-06-16 | 江苏恒瑞医药股份有限公司 | 一种erk抑制剂的结晶形式及其制备方法 |
US20230331731A1 (en) * | 2020-09-29 | 2023-10-19 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Crystal form of pyrrolo heterocyclic derivative and preparation method therefor |
US20240207269A1 (en) * | 2021-04-16 | 2024-06-27 | Erasca, Inc. | Uses of heterocyclic inhibitors of erk1/2 |
TW202317122A (zh) * | 2021-06-24 | 2023-05-01 | 美商艾瑞斯卡公司 | Erk1/2及kras g12c抑制劑之組合療法 |
TW202317123A (zh) * | 2021-06-24 | 2023-05-01 | 美商艾瑞斯卡公司 | Erk1/2及cdk4/6抑制劑之組合療法 |
CA3222772A1 (en) * | 2021-06-24 | 2022-12-29 | Erasca, Inc. | Erk1/2 and shp2 inhibitors combination therapy |
WO2022271919A1 (en) * | 2021-06-24 | 2022-12-29 | Erasca, Inc. | Erk1/2 or shp2 inhibitors and flt3 inhibitors combination therapy |
TW202341999A (zh) * | 2022-03-28 | 2023-11-01 | 大陸商江蘇恒瑞醫藥股份有限公司 | 吡咯并雜環類衍生物的富馬酸鹽的晶型及其製備方法 |
WO2024064690A1 (en) * | 2022-09-20 | 2024-03-28 | Erasca, Inc. | Erk1/2 inhibitor polymorph forms |
Family Cites Families (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IT1319849B1 (it) | 2000-02-18 | 2003-11-03 | Angelo Dotta | Cerotto in confezione ad apertura rapida e mezzi per la realizzazionedella stessa. |
MY130778A (en) * | 2001-02-09 | 2007-07-31 | Vertex Pharma | Heterocyclic inhibitiors of erk2 and uses thereof |
US6743941B2 (en) | 2001-06-15 | 2004-06-01 | Aventis Pharma Deutschland Gmbh | Process for the production of piperidine derivatives |
US7279576B2 (en) | 2002-12-31 | 2007-10-09 | Deciphera Pharmaceuticals, Llc | Anti-cancer medicaments |
US7202257B2 (en) | 2003-12-24 | 2007-04-10 | Deciphera Pharmaceuticals, Llc | Anti-inflammatory medicaments |
AU2004313928A1 (en) * | 2003-12-02 | 2005-07-28 | Vertex Pharmaceuticals, Inc. | Heterocyclic protein kinase inhibitors and uses thereof |
US20070191336A1 (en) | 2003-12-24 | 2007-08-16 | Flynn Daniel L | Anti-inflammatory medicaments |
UA84929C2 (en) * | 2004-05-14 | 2008-12-10 | Вертекс Фармасьютикалс Инкорпорейтед | Prodrugs of pyrrolylpyrimidine erk protein kinase inhibitors |
US7501415B2 (en) * | 2004-12-23 | 2009-03-10 | Vertex Pharmaceuticals Incorporated | Selective inhibitors of ERK protein kinase and uses thereof |
US8546404B2 (en) | 2005-12-13 | 2013-10-01 | Merck Sharp & Dohme | Compounds that are ERK inhibitors |
EA024729B1 (ru) * | 2009-11-13 | 2016-10-31 | Джиноско | Киназные ингибиторы |
WO2012142308A1 (en) | 2011-04-13 | 2012-10-18 | Activesite Pharmaceuticals, Inc. | Prodrugs of inhibitors of plasma kallikrein |
US9227969B2 (en) * | 2013-08-14 | 2016-01-05 | Novartis Ag | Compounds and compositions as inhibitors of MEK |
EP3842429B1 (en) | 2015-06-15 | 2022-09-07 | Asana BioSciences, LLC | Heterocyclic inhibitors of erk1 and erk2 and their use in the treatment of cancer |
TW201805000A (zh) | 2016-06-20 | 2018-02-16 | 庫拉腫瘤技術股份有限公司 | 利用erk抑制劑之鱗狀細胞癌之治療 |
WO2020046966A1 (en) | 2018-08-27 | 2020-03-05 | Kura Oncology, Inc. | Treatment of adenocarcinomas with mapk pathway inhibitors |
EP4051264A1 (en) | 2019-10-28 | 2022-09-07 | Asana BioSciences, LLC | Improved methods, kits, compositions and dosing regimens for the use of heterocyclic inhibitors of erk1 and erk2 |
US20240207269A1 (en) | 2021-04-16 | 2024-06-27 | Erasca, Inc. | Uses of heterocyclic inhibitors of erk1/2 |
-
2016
- 2016-06-15 EP EP21156048.7A patent/EP3842429B1/en active Active
- 2016-06-15 BR BR112017026159-6A patent/BR112017026159A2/pt not_active Application Discontinuation
- 2016-06-15 FI FIEP16741411.9T patent/FI3307727T3/fi active
- 2016-06-15 JP JP2017559575A patent/JP6909729B2/ja active Active
- 2016-06-15 ES ES16741411T patent/ES2968007T3/es active Active
- 2016-06-15 RU RU2017139727A patent/RU2017139727A/ru not_active Application Discontinuation
- 2016-06-15 DK DK21156048.7T patent/DK3842429T3/da active
- 2016-06-15 US US15/183,504 patent/US10751332B2/en active Active
- 2016-06-15 CN CN201680031963.5A patent/CN107922387A/zh active Pending
- 2016-06-15 EP EP16741411.9A patent/EP3307727B1/en active Active
- 2016-06-15 PL PL21156048.7T patent/PL3842429T3/pl unknown
- 2016-06-15 US US15/183,486 patent/US9896445B2/en active Active
- 2016-06-15 KR KR1020217005104A patent/KR102644798B1/ko active IP Right Grant
- 2016-06-15 PT PT211560487T patent/PT3842429T/pt unknown
- 2016-06-15 WO PCT/US2016/037697 patent/WO2016205418A1/en active Application Filing
- 2016-06-15 ES ES21156048T patent/ES2930050T3/es active Active
- 2016-06-15 DK DK16741411.9T patent/DK3307727T3/da active
- 2016-06-15 AU AU2016280717A patent/AU2016280717C1/en active Active
- 2016-06-15 MX MX2017014584A patent/MX2017014584A/es unknown
- 2016-06-15 CA CA2986587A patent/CA2986587C/en active Active
- 2016-06-15 PT PT167414119T patent/PT3307727T/pt unknown
- 2016-06-15 CN CN202110399513.4A patent/CN113200961B/zh active Active
- 2016-06-15 KR KR1020177034157A patent/KR102644788B1/ko active IP Right Grant
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2017
- 2017-09-01 US US15/694,124 patent/US10471051B2/en active Active
- 2017-11-07 ZA ZA2017/07526A patent/ZA201707526B/en unknown
- 2017-11-12 IL IL255613A patent/IL255613B/en active IP Right Grant
- 2017-11-14 MX MX2021000148A patent/MX2021000148A/es unknown
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2020
- 2020-02-13 US US16/790,082 patent/US11103491B2/en active Active
- 2020-11-19 AU AU2020273302A patent/AU2020273302B2/en active Active
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2021
- 2021-03-16 JP JP2021042239A patent/JP7093438B2/ja active Active
- 2021-07-06 US US17/368,559 patent/US11925629B2/en active Active
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