MX2017008242A - Derivados de tieno [2,3c] pirrol-4-ona como inhibidores de erk. - Google Patents
Derivados de tieno [2,3c] pirrol-4-ona como inhibidores de erk.Info
- Publication number
- MX2017008242A MX2017008242A MX2017008242A MX2017008242A MX2017008242A MX 2017008242 A MX2017008242 A MX 2017008242A MX 2017008242 A MX2017008242 A MX 2017008242A MX 2017008242 A MX2017008242 A MX 2017008242A MX 2017008242 A MX2017008242 A MX 2017008242A
- Authority
- MX
- Mexico
- Prior art keywords
- pyrrol
- thieno
- derivatives
- erk inhibitors
- erk
- Prior art date
Links
- KHVSDEGLMIURSH-UHFFFAOYSA-N thieno[2,3-c]pyrrol-4-one Chemical class S1C=CC2=C1C=NC2=O KHVSDEGLMIURSH-UHFFFAOYSA-N 0.000 title abstract 2
- 239000012824 ERK inhibitor Substances 0.000 title 1
- 102000007665 Extracellular Signal-Regulated MAP Kinases Human genes 0.000 abstract 2
- 108010007457 Extracellular Signal-Regulated MAP Kinases Proteins 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
Classifications
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- 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
- 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
- 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)
- Proteomics, Peptides & Aminoacids (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Microbiology (AREA)
- Mycology (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
La presente invención proporciona compuestos de tieno[2,3-c]pirrol-4-ona que inhiben la actividad de la cinasa de señal extracelular regulada (ERK) y pueden ser útiles en el tratamiento de cáncer.
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 |
|---|---|
| MX2017008242A true MX2017008242A (es) | 2017-10-06 |
| MX371206B MX371206B (es) | 2020-01-22 |
Family
ID=55135525
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2017008242A MX371206B (es) | 2014-12-22 | 2015-12-16 | Derivados de tieno [2,3c] pirrol-4-ona como inhibidores de erk. |
Country Status (44)
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL3052096T3 (pl) | 2013-10-03 | 2018-07-31 | Kura Oncology Inc | Inhibitory ERK i sposoby ich zastosowania |
| TWI704151B (zh) * | 2014-12-22 | 2020-09-11 | 美商美國禮來大藥廠 | Ｅｒｋ抑制劑 |
| CN107074874B (zh) | 2014-12-22 | 2019-04-23 | 伊莱利利公司 | Erk抑制剂 |
| HUE068392T2 (hu) | 2015-10-21 | 2024-12-28 | Otsuka Pharma Co Ltd | Benzolaktám vegyületek mint fehérje kináz gátlók |
| 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 |
| KR20210006365A (ko) * | 2018-04-09 | 2021-01-18 | 쥐원 쎄라퓨틱스, 인크. | 구동 종양원성 돌연변이를 갖는 암의 치료 |
| AU2019272303B2 (en) * | 2018-05-22 | 2024-11-07 | Js Innomed Holdings Ltd. | Heterocyclic compounds as kinase inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof |
| US20220040324A1 (en) | 2018-12-21 | 2022-02-10 | Daiichi Sankyo Company, Limited | Combination of antibody-drug conjugate and kinase inhibitor |
| EP3946620B1 (en) * | 2019-03-27 | 2023-04-26 | Eli Lilly and Company | Salts of 5,6-dihydro-4h-thieno[2,3-c]pyrrol-4-one compound as erk inhibitors |
| WO2020192750A1 (zh) * | 2019-03-28 | 2020-10-01 | 江苏恒瑞医药股份有限公司 | 噻吩并杂环类衍生物、其制备方法及其在医药上的应用 |
| CA3135070A1 (en) * | 2019-03-29 | 2020-10-08 | Jiangsu Hengrui Medicine Co., Ltd. | Pyrroloheterocyclic derivative, preparation method therefor, and application thereof in medicine |
| JP7234418B2 (ja) * | 2019-05-16 | 2023-03-07 | イーライ リリー アンド カンパニー | Ｂｒａｆｖ６００ｅ大腸癌の治療に使用するためのｅｒｋ１／２阻害剤と、ｂｒａｆ阻害剤およびｅｇｆｒ阻害剤との三重組み合わせ |
| 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 |
| US12398153B2 (en) | 2019-12-06 | 2025-08-26 | D3 Bio (Wuxi) Co., Ltd. | Spiro compound serving as ERK inhibitor, and application thereof |
| 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 |
| WO2022068860A1 (zh) * | 2020-09-29 | 2022-04-07 | 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 |
| TW202409052A (zh) * | 2021-06-28 | 2024-03-01 | 大陸商德昇濟醫藥（無錫）有限公司 | 噻唑並內醯胺並螺雜環類化合物及其應用 |
| JP7716127B2 (ja) * | 2021-06-28 | 2025-07-31 | 徳昇済医薬（無錫）有限公司 | ジメチル置換チアゾロラクタム化合物及びその使用 |
| TW202332448A (zh) * | 2021-11-15 | 2023-08-16 | 美商艾瑞斯卡公司 | 噻吩ulk1/2抑制劑及其用途 |
| 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 |
| US20240352029A1 (en) * | 2023-04-14 | 2024-10-24 | Prelude Therapeutics Incorporated | CDK Inhibitors And Their Use As Pharmaceuticals |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
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| DE4023048A1 (de) * | 1990-07-20 | 1992-01-23 | Basf Ag | Dicarbonsaeureimide, verfahren zu ihrer herstellung und ihre verwendung als herbizide |
| WO2002022607A1 (en) * | 2000-09-15 | 2002-03-21 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US7473691B2 (en) * | 2000-09-15 | 2009-01-06 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| ATE510561T1 (de) | 2002-03-04 | 2011-06-15 | Imclone Llc | Kdr-spezifische menschliche antikörper und ihre verwendung |
| EP1562938B1 (en) * | 2002-11-04 | 2007-08-29 | Vertex Pharmaceuticals Incorporated | Heteroaryl-pyrimidine derivatives as jak inhibitors |
| UA80571C2 (en) | 2002-11-22 | 2007-10-10 | Lilly Co Eli | Quinolinyl-pyrrolopyrazoles |
| EP1948647A1 (en) * | 2005-11-03 | 2008-07-30 | SGX Pharmaceuticals, Inc. | Pyrimidinyl-thiophene kinase modulators |
| AR072937A1 (es) | 2008-08-20 | 2010-09-29 | Schering Corp | Derivados de piridina y pirimidina sustituida y su uso en el tratamiento de infecciones virales |
| EP2346860B1 (en) * | 2008-10-08 | 2012-09-19 | Bristol-Myers Squibb Company | Pyrrolone melanin concentrating hormone receptor-1 antagonists |
| PA8852901A1 (es) * | 2008-12-22 | 2010-07-27 | Lilly Co Eli | Inhibidores de proteina cinasa |
| US8975260B2 (en) * | 2010-09-01 | 2015-03-10 | Genetech, Inc | Pyridazinones, method of making, and method of use thereof |
| JO3148B1 (ar) | 2011-07-27 | 2017-09-20 | Lilly Co Eli | مركب مثبط لإشارات مسار notch |
| MY191936A (en) * | 2012-03-01 | 2022-07-19 | Genentech Inc | Serine/threonine kinase inhibitors |
| AR090151A1 (es) | 2012-03-07 | 2014-10-22 | Lilly Co Eli | Compuestos inhibidores de raf |
| EP2900261A1 (en) * | 2012-09-28 | 2015-08-05 | Boehringer Ingelheim International GmbH | Pharmaceutical combinations comprising dual angiopoietin-2 / dll4 binders and anti-vegf-r agents |
| TWI704151B (zh) * | 2014-12-22 | 2020-09-11 | 美商美國禮來大藥廠 | Ｅｒｋ抑制劑 |
| CN107074874B (zh) * | 2014-12-22 | 2019-04-23 | 伊莱利利公司 | Erk抑制剂 |
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2015
- 2015-12-09 TW TW104141368A patent/TWI704151B/zh not_active IP Right Cessation
- 2015-12-10 JO JOP/2015/0310A patent/JO3596B1/ar active
- 2015-12-11 AR ARP150104045A patent/AR102977A1/es unknown
- 2015-12-16 BR BR112017011130A patent/BR112017011130A2/pt active Search and Examination
- 2015-12-16 MY MYPI2017702263A patent/MY178426A/en unknown
- 2015-12-16 ME MEP-2019-201A patent/ME03490B/me unknown
- 2015-12-16 NZ NZ731531A patent/NZ731531A/en not_active IP Right Cessation
- 2015-12-16 MA MA41251A patent/MA41251B1/fr unknown
- 2015-12-16 WO PCT/US2015/065940 patent/WO2016106029A1/en not_active Ceased
- 2015-12-16 CA CA2966559A patent/CA2966559C/en active Active
- 2015-12-16 RS RS20190906A patent/RS59015B1/sr unknown
- 2015-12-16 JP JP2017533381A patent/JP6445701B2/ja not_active Expired - Fee Related
- 2015-12-16 AU AU2015369983A patent/AU2015369983C1/en not_active Ceased
- 2015-12-16 PT PT15823869T patent/PT3237423T/pt unknown
- 2015-12-16 US US14/970,588 patent/US9469652B2/en not_active Ceased
- 2015-12-16 DK DK15823869.1T patent/DK3237423T3/da active
- 2015-12-16 HR HRP20191268 patent/HRP20191268T1/hr unknown
- 2015-12-16 EP EP15823869.1A patent/EP3237423B1/en active Active
- 2015-12-16 PL PL15823869T patent/PL3237423T3/pl unknown
- 2015-12-16 CN CN201580070315.6A patent/CN107108648B/zh not_active Expired - Fee Related
- 2015-12-16 MD MDE20170231 patent/MD3237423T2/ro not_active IP Right Cessation
- 2015-12-16 MX MX2017008242A patent/MX371206B/es active IP Right Grant
- 2015-12-16 TN TN2017000233A patent/TN2017000233A1/en unknown
- 2015-12-16 KR KR1020177016748A patent/KR101917972B1/ko not_active Expired - Fee Related
- 2015-12-16 UA UAA201706046A patent/UA119686C2/uk unknown
- 2015-12-16 TR TR2019/09887T patent/TR201909887T4/tr unknown
- 2015-12-16 LT LTEP15823869.1T patent/LT3237423T/lt unknown
- 2015-12-16 EA EA201791133A patent/EA031659B1/ru not_active IP Right Cessation
- 2015-12-16 CR CR20170182A patent/CR20170182A/es unknown
- 2015-12-16 ES ES15823869T patent/ES2738406T3/es active Active
- 2015-12-16 SG SG11201704521SA patent/SG11201704521SA/en unknown
- 2015-12-16 PE PE2017001109A patent/PE20171043A1/es unknown
- 2015-12-16 SI SI201530773T patent/SI3237423T1/sl unknown
- 2015-12-16 HU HUE15823869A patent/HUE045933T2/hu 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
- 2019-07-23 CY CY20191100777T patent/CY1121831T1/el unknown
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