EA201791133A1 - Ингибиторы erk - Google Patents
Ингибиторы erkInfo
- Publication number
- EA201791133A1 EA201791133A1 EA201791133A EA201791133A EA201791133A1 EA 201791133 A1 EA201791133 A1 EA 201791133A1 EA 201791133 A EA201791133 A EA 201791133A EA 201791133 A EA201791133 A EA 201791133A EA 201791133 A1 EA201791133 A1 EA 201791133A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- erk inhibitors
- erk
- pyrrol
- cancer
- inhibit
- Prior art date
Links
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
- A61K31/535—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
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
- A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
-
- 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
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
- C07K16/2863—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against receptors for growth factors, growth regulators
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Molecular Biology (AREA)
- Endocrinology (AREA)
- Mycology (AREA)
- Engineering & Computer Science (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Microbiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
В настоящем изобретении предложены тиено[2,3-с]пиррол-4-оновые соединения, ингибирующие активность внеклеточной сигнал-регулируемой киназы (ERK), которые могут быть эффективными при лечении рака.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462095185P | 2014-12-22 | 2014-12-22 | |
| PCT/US2015/065940 WO2016106029A1 (en) | 2014-12-22 | 2015-12-16 | Thieno[2,3-c]pyrrol-4-one derivatives as erk inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201791133A1 true EA201791133A1 (ru) | 2017-10-31 |
| EA031659B1 EA031659B1 (ru) | 2019-02-28 |
Family
ID=55135525
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201791133A EA031659B1 (ru) | 2014-12-22 | 2015-12-16 | Ингибиторы erk |
Country Status (44)
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA032196B1 (ru) | 2013-10-03 | 2019-04-30 | Кура Онколоджи, Инк. | Ингибиторы erk и способы применения |
| TWI704151B (zh) * | 2014-12-22 | 2020-09-11 | 美商美國禮來大藥廠 | Ｅｒｋ抑制劑 |
| ES2700200T3 (es) | 2014-12-22 | 2019-02-14 | Lilly Co Eli | Inhibidores de ERK |
| WO2017068412A1 (en) | 2015-10-21 | 2017-04-27 | Otsuka Pharmaceutical Co., Ltd. | Benzolactam compounds as protein kinase inhibitors |
| EP3478292A1 (en) * | 2016-06-29 | 2019-05-08 | Eli Lilly and Company | Combination of erk1/2 inhibitor compound with gemcitabine or with gemcitabine and nab-paclitaxel for use in treatment of pancreatic cancer |
| WO2018081204A1 (en) * | 2016-10-26 | 2018-05-03 | Li George Y | DEUTERATED N-(5-((4-ETHYLPIPERAZIN-1-YL)METHYL) PYRIDIN-2-YL)-5-FLUORO-4-(4-FLUORO-1-ISOPROPYL-2-METHYL-1H-BENZO[d]IMIDAZOL-6-YL)PYRIMIDIN-2-AMINE |
| GB201706327D0 (en) | 2017-04-20 | 2017-06-07 | Otsuka Pharma Co Ltd | A pharmaceutical compound |
| JP7312171B2 (ja) | 2017-11-24 | 2023-07-20 | ヤンセン ファーマシューティカ エヌ．ベー． | ピラゾロピリジノン化合物 |
| CN114366743A (zh) * | 2018-04-09 | 2022-04-19 | G1治疗公司 | 具有驱动致癌突变的癌症的治疗 |
| KR20210013145A (ko) * | 2018-05-22 | 2021-02-03 | 제이에스 이노메드 홀딩스 엘티디. | 키나아제 억제제로서 헤테로시클릭 화합물, 헤테로시클릭 화합물을 포함하는 조성물 및 그 사용 방법 |
| SG11202106635WA (en) | 2018-12-21 | 2021-07-29 | Daiichi Sankyo Co Ltd | Combination of antibody-drug conjugate and kinase inhibitor |
| ES2944857T3 (es) * | 2019-03-27 | 2023-06-26 | Lilly Co Eli | Sales del compuesto 5,6-dihidro-4H-tieno[2,3-c]pirrol-4-ona como inhibidores de ERK |
| US20220213119A1 (en) * | 2019-03-28 | 2022-07-07 | Jiangsu Hengrui Medicine Ca, Lid. | Thienoheterocyclic derivative, preparation method therefor and medical use thereof |
| EP3950690A4 (en) * | 2019-03-29 | 2022-12-07 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | PYRROLOHETEROCYCLIC DERIVATIVE, PROCESS FOR PRODUCTION THEREOF AND APPLICATION THEREOF IN MEDICINE |
| EP3968995A1 (en) * | 2019-05-16 | 2022-03-23 | Eli Lilly and Company | Triple combination of an erk1/2 inhibitor with a braf inhibitor and an egfr inhibitor for use in the treatment of brafv600e colorectal cancer |
| CN112457326B (zh) * | 2019-09-06 | 2022-02-15 | 上海凌达生物医药有限公司 | 一类芳香杂环并内酰胺类化合物、制备方法和用途 |
| EP4071152A4 (en) * | 2019-12-06 | 2024-01-17 | D3 Bio Wuxi Co Ltd | SPIRO COMPOUND SERVING AS AN ERK INHIBITOR AND THEIR USE |
| CN110950876B (zh) * | 2019-12-10 | 2021-08-17 | 上海凌达生物医药有限公司 | 一类呋喃并内酰胺类化合物、制备方法和用途 |
| WO2021216777A1 (en) * | 2020-04-21 | 2021-10-28 | The Trustees Of The Stevens Institute Of Technology | Erk inhibitors for cancer therapy |
| 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 |
| CN116437915A (zh) * | 2020-09-29 | 2023-07-14 | 江苏恒瑞医药股份有限公司 | 一种吡咯并杂环类衍生物的晶型及其制备方法 |
| EP4345103A1 (en) * | 2021-06-28 | 2024-04-03 | D3 Bio (Wuxi) Co., Ltd. | Thiazole-lactam-spiroheterocyclic compounds and applications thereof |
| CA3238655A1 (en) * | 2021-11-15 | 2023-05-19 | Erasca, Inc. | Thiophene ulk1/2 inhibitors and their use thereof |
| WO2023137297A2 (en) * | 2022-01-11 | 2023-07-20 | Suvalent Therapeutics, Inc. | 5,6-dihydro-4h-thieno[2,3-c]pyrrole sumo inhibitors and uses thereof |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4023048A1 (de) * | 1990-07-20 | 1992-01-23 | Basf Ag | Dicarbonsaeureimide, verfahren zu ihrer herstellung und ihre verwendung als herbizide |
| US7473691B2 (en) * | 2000-09-15 | 2009-01-06 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| MXPA03002299A (es) * | 2000-09-15 | 2003-06-06 | Vertex Pharma | Compuestos de pirazol utiles como inhibidores de proteina cinasa. |
| ES2362931T3 (es) | 2002-03-04 | 2011-07-15 | Imclone Llc | Anticuerpos humanos específicos contra kdr y usos de los mismos. |
| AU2003295396B2 (en) * | 2002-11-04 | 2009-02-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl-pyramidine derivatives as JAK inhibitors |
| UA80571C2 (en) | 2002-11-22 | 2007-10-10 | Lilly Co Eli | Quinolinyl-pyrrolopyrazoles |
| JP2009519218A (ja) * | 2005-11-03 | 2009-05-14 | エスジーエックス ファーマシューティカルズ、インコーポレイテッド | ピリミジニル−チオフェンキナーゼモジュレータ |
| CA2734486A1 (en) | 2008-08-20 | 2010-02-25 | Southern Research Institute | Substituted pyridine and pyrimidine derivatives and their use in treating viral infections |
| US8344160B2 (en) * | 2008-10-08 | 2013-01-01 | Bristol-Myers Squibb Company | Pyrrolone melanin concentrating hormone receptor-1 antagonists |
| JO2885B1 (en) * | 2008-12-22 | 2015-03-15 | ايلي ليلي اند كومباني | Protein kinase inhibitors |
| CN103201277B (zh) * | 2010-09-01 | 2015-11-25 | 吉利德康涅狄格有限公司 | 哒嗪酮、其制备方法及使用方法 |
| AR087107A1 (es) | 2011-07-27 | 2014-02-12 | Lilly Co Eli | Compuesto inhibidor de la señalizacion de la trayectoria notch |
| CN106349217B (zh) * | 2012-03-01 | 2020-08-28 | 阵列生物制药公司 | 丝氨酸/苏氨酸激酶抑制剂 |
| AR090151A1 (es) | 2012-03-07 | 2014-10-22 | Lilly Co Eli | Compuestos inhibidores de raf |
| WO2014049099A1 (en) * | 2012-09-28 | 2014-04-03 | Boehringer Ingelheim International Gmbh | Pharmaceutical combinations comprising dual angiopoietin-2 / dll4 binders and anti-vegf-r agents |
| ES2700200T3 (es) * | 2014-12-22 | 2019-02-14 | Lilly Co Eli | Inhibidores de ERK |
| TWI704151B (zh) * | 2014-12-22 | 2020-09-11 | 美商美國禮來大藥廠 | Ｅｒｋ抑制劑 |
-
2015
- 2015-12-09 TW TW104141368A patent/TWI704151B/zh active
- 2015-12-10 JO JOP/2015/0310A patent/JO3596B1/ar active
- 2015-12-11 AR ARP150104045A patent/AR102977A1/es unknown
- 2015-12-16 ME MEP-2019-201A patent/ME03490B/me unknown
- 2015-12-16 PE PE2017001109A patent/PE20171043A1/es unknown
- 2015-12-16 CA CA2966559A patent/CA2966559C/en active Active
- 2015-12-16 ES ES15823869T patent/ES2738406T3/es active Active
- 2015-12-16 MD MDE20170231 patent/MD3237423T2/ro unknown
- 2015-12-16 MA MA41251A patent/MA41251B1/fr unknown
- 2015-12-16 CN CN201580070315.6A patent/CN107108648B/zh active Active
- 2015-12-16 PL PL15823869T patent/PL3237423T3/pl unknown
- 2015-12-16 HU HUE15823869A patent/HUE045933T2/hu unknown
- 2015-12-16 EA EA201791133A patent/EA031659B1/ru not_active IP Right Cessation
- 2015-12-16 AU AU2015369983A patent/AU2015369983C1/en not_active Ceased
- 2015-12-16 BR BR112017011130A patent/BR112017011130A2/pt active Search and Examination
- 2015-12-16 US US14/970,588 patent/US9469652B2/en not_active Ceased
- 2015-12-16 LT LTEP15823869.1T patent/LT3237423T/lt unknown
- 2015-12-16 MY MYPI2017702263A patent/MY178426A/en unknown
- 2015-12-16 JP JP2017533381A patent/JP6445701B2/ja active Active
- 2015-12-16 NZ NZ731531A patent/NZ731531A/en not_active IP Right Cessation
- 2015-12-16 MX MX2017008242A patent/MX371206B/es active IP Right Grant
- 2015-12-16 RS RS20190906A patent/RS59015B1/sr unknown
- 2015-12-16 PT PT15823869T patent/PT3237423T/pt unknown
- 2015-12-16 TN TN2017000233A patent/TN2017000233A1/en unknown
- 2015-12-16 UA UAA201706046A patent/UA119686C2/uk unknown
- 2015-12-16 TR TR2019/09887T patent/TR201909887T4/tr unknown
- 2015-12-16 KR KR1020177016748A patent/KR101917972B1/ko active IP Right Grant
- 2015-12-16 CR CR20170182A patent/CR20170182A/es unknown
- 2015-12-16 SG SG11201704521SA patent/SG11201704521SA/en unknown
- 2015-12-16 DK DK15823869.1T patent/DK3237423T3/da active
- 2015-12-16 WO PCT/US2015/065940 patent/WO2016106029A1/en active Application Filing
- 2015-12-16 EP EP15823869.1A patent/EP3237423B1/en active Active
- 2015-12-16 SI SI201530773T patent/SI3237423T1/sl unknown
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2016
- 2016-09-08 US US15/259,381 patent/US9526733B1/en active Active
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2017
- 2017-04-20 ZA ZA2017/02786A patent/ZA201702786B/en unknown
- 2017-05-01 IL IL252065A patent/IL252065B/en active IP Right Grant
- 2017-05-15 SV SV2017005443A patent/SV2017005443A/es unknown
- 2017-05-16 DO DO2017000122A patent/DOP2017000122A/es unknown
- 2017-05-25 CO CONC2017/0005217A patent/CO2017005217A2/es unknown
- 2017-06-13 CL CL2017001514A patent/CL2017001514A1/es unknown
- 2017-06-19 GT GT201700134A patent/GT201700134A/es unknown
- 2017-06-20 PH PH12017501155A patent/PH12017501155B1/en unknown
- 2017-06-22 EC ECIEPI201738500A patent/ECSP17038500A/es unknown
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2019
- 2019-05-22 US US16/419,141 patent/USRE48635E1/en active Active
- 2019-07-15 HR HRP20191268 patent/HRP20191268T1/hr unknown
- 2019-07-23 CY CY20191100777T patent/CY1121831T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AZ BY KG TJ TM |