MD3237423T2 - Derivați ai tieno[2,3-c]pirol-4-onei în calitate de inhibitori ai ERK - Google Patents

Derivați ai tieno[2,3-c]pirol-4-onei în calitate de inhibitori ai ERK

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Publication number
MD3237423T2
MD3237423T2 MDE20170231T MD3237423T2 MD 3237423 T2 MD3237423 T2 MD 3237423T2 MD E20170231 T MDE20170231 T MD E20170231T MD 3237423 T2 MD3237423 T2 MD 3237423T2
Authority
MD
Moldova
Prior art keywords
pyrrol
thieno
derivatives
erk inhibitors
erk
Prior art date
Application number
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English (en)
Inventor
Guillermo S Cortez
Sajan Joseph
Johnathan Alexander Mclean
William T Mcmillen
Michael John Rodriguez
Gaiying Zhao
Original Assignee
Lilly Co Eli
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of MD3237423T2 publication Critical patent/MD3237423T2/ro

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    • 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
    • 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
    • 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

Prezenta invenţie furnizează compuşi ai tieno[2,3-c]pirol-4-onei care inhibă activitatea kinazei reglate de semnalul extracelular (ERK) şi pot fi utili pentru tratarea cancerului.
MDE20170231 2014-12-22 2015-12-16 Derivați ai tieno[2,3-c]pirol-4-onei în calitate de inhibitori ai ERK MD3237423T2 (ro)

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 (1)

Publication Number Publication Date
MD3237423T2 true MD3237423T2 (ro) 2019-11-30

Family

ID=55135525

Family Applications (1)

Application Number Title Priority Date Filing Date
MDE20170231 MD3237423T2 (ro) 2014-12-22 2015-12-16 Derivați ai tieno[2,3-c]pirol-4-onei în calitate de inhibitori ai ERK

Country Status (44)

Country Link
US (3) US9469652B2 (ro)
EP (1) EP3237423B1 (ro)
JP (1) JP6445701B2 (ro)
KR (1) KR101917972B1 (ro)
CN (1) CN107108648B (ro)
AR (1) AR102977A1 (ro)
AU (1) AU2015369983C1 (ro)
BR (1) BR112017011130A2 (ro)
CA (1) CA2966559C (ro)
CL (1) CL2017001514A1 (ro)
CO (1) CO2017005217A2 (ro)
CR (1) CR20170182A (ro)
CY (1) CY1121831T1 (ro)
DK (1) DK3237423T3 (ro)
DO (1) DOP2017000122A (ro)
EA (1) EA031659B1 (ro)
EC (1) ECSP17038500A (ro)
ES (1) ES2738406T3 (ro)
GT (1) GT201700134A (ro)
HR (1) HRP20191268T1 (ro)
HU (1) HUE045933T2 (ro)
IL (1) IL252065B (ro)
JO (1) JO3596B1 (ro)
LT (1) LT3237423T (ro)
MA (1) MA41251B1 (ro)
MD (1) MD3237423T2 (ro)
ME (1) ME03490B (ro)
MX (1) MX371206B (ro)
MY (1) MY178426A (ro)
NZ (1) NZ731531A (ro)
PE (1) PE20171043A1 (ro)
PH (1) PH12017501155B1 (ro)
PL (1) PL3237423T3 (ro)
PT (1) PT3237423T (ro)
RS (1) RS59015B1 (ro)
SG (1) SG11201704521SA (ro)
SI (1) SI3237423T1 (ro)
SV (1) SV2017005443A (ro)
TN (1) TN2017000233A1 (ro)
TR (1) TR201909887T4 (ro)
TW (1) TWI704151B (ro)
UA (1) UA119686C2 (ro)
WO (1) WO2016106029A1 (ro)
ZA (1) ZA201702786B (ro)

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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
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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

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Also Published As

Publication number Publication date
RS59015B1 (sr) 2019-08-30
JP6445701B2 (ja) 2018-12-26
AU2015369983A1 (en) 2017-05-25
EP3237423B1 (en) 2019-06-05
IL252065A0 (en) 2017-07-31
HUE045933T2 (hu) 2020-01-28
GT201700134A (es) 2018-11-23
US9469652B2 (en) 2016-10-18
CN107108648A (zh) 2017-08-29
TR201909887T4 (tr) 2019-07-22
TWI704151B (zh) 2020-09-11
US9526733B1 (en) 2016-12-27
IL252065B (en) 2020-08-31
US20160176896A1 (en) 2016-06-23
LT3237423T (lt) 2019-08-26
MA41251B1 (fr) 2019-09-30
AU2015369983C1 (en) 2019-02-21
EA201791133A1 (ru) 2017-10-31
SV2017005443A (es) 2018-08-27
SI3237423T1 (sl) 2019-08-30
HRP20191268T1 (hr) 2019-11-01
BR112017011130A2 (pt) 2017-12-26
JP2017538768A (ja) 2017-12-28
MX371206B (es) 2020-01-22
UA119686C2 (uk) 2019-07-25
PH12017501155A1 (en) 2017-11-27
EP3237423A1 (en) 2017-11-01
CR20170182A (es) 2017-06-21
CN107108648B (zh) 2019-07-12
KR20170083145A (ko) 2017-07-17
DK3237423T3 (da) 2019-07-22
PL3237423T3 (pl) 2020-01-31
CA2966559A1 (en) 2016-06-30
WO2016106029A1 (en) 2016-06-30
CY1121831T1 (el) 2020-07-31
EA031659B1 (ru) 2019-02-28
CA2966559C (en) 2019-06-18
TW201632530A (zh) 2016-09-16
TN2017000233A1 (en) 2018-10-19
PE20171043A1 (es) 2017-07-19
ECSP17038500A (es) 2017-12-01
SG11201704521SA (en) 2017-07-28
MX2017008242A (es) 2017-10-06
AU2015369983B2 (en) 2018-08-23
NZ731531A (en) 2018-12-21
ZA201702786B (en) 2019-02-27
KR101917972B1 (ko) 2018-11-12
MY178426A (en) 2020-10-13
ES2738406T3 (es) 2020-01-22
ME03490B (me) 2020-01-20
AR102977A1 (es) 2017-04-05
PH12017501155B1 (en) 2017-11-27
JO3596B1 (ar) 2020-07-05
CO2017005217A2 (es) 2017-09-20
MA41251A (fr) 2017-11-01
US20160375030A1 (en) 2016-12-29
CL2017001514A1 (es) 2018-02-09
DOP2017000122A (es) 2017-06-15
PT3237423T (pt) 2019-08-21
USRE48635E1 (en) 2021-07-13

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