SG11201704521SA - Thieno[2,3-c]pyrrol-4-one derivatives as erk inhibitors - Google Patents

Thieno[2,3-c]pyrrol-4-one derivatives as erk inhibitors

Info

Publication number
SG11201704521SA
SG11201704521SA SG11201704521SA SG11201704521SA SG11201704521SA SG 11201704521S A SG11201704521S A SG 11201704521SA SG 11201704521S A SG11201704521S A SG 11201704521SA SG 11201704521S A SG11201704521S A SG 11201704521SA SG 11201704521S A SG11201704521S A SG 11201704521SA
Authority
SG
Singapore
Prior art keywords
thieno
pyrrol
derivatives
erk inhibitors
erk
Prior art date
Application number
SG11201704521SA
Other languages
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 SG11201704521SA publication Critical patent/SG11201704521SA/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2863Immunoglobulins [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)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Mycology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Microbiology (AREA)
  • Proteomics, Peptides & Aminoacids (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)
SG11201704521SA 2014-12-22 2015-12-16 Thieno[2,3-c]pyrrol-4-one derivatives as erk inhibitors SG11201704521SA (en)

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
SG11201704521SA true SG11201704521SA (en) 2017-07-28

Family

ID=55135525

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201704521SA SG11201704521SA (en) 2014-12-22 2015-12-16 Thieno[2,3-c]pyrrol-4-one derivatives as erk inhibitors

Country Status (44)

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

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SG11201602572YA (en) 2013-10-03 2016-04-28 Kura Oncology Inc Inhibitors of erk and methods of use
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
EP3365334B1 (de) 2015-10-21 2024-07-17 Otsuka Pharmaceutical Co., Ltd. Benzolactam-verbindungen als proteinkinasehemmer
JP2019523778A (ja) * 2016-06-29 2019-08-29 イーライ リリー アンド カンパニー 膵癌の治療に使用するための、erk1/2阻害剤化合物と、ゲムシタビン、またはゲムシタビンおよびnab−パクリタキセルとの併用
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
AU2019253706A1 (en) * 2018-04-09 2020-11-26 G1 Therapeutics, Inc. Treatment of cancers having driving oncogenic mutations
CA3101117A1 (en) * 2018-05-22 2019-11-28 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 (de) * 2019-03-27 2023-04-26 Eli Lilly and Company Salze der 5,6-dihydro-4h-thieno[2,3-c]pyrrol-4-on-verbindung als erk-inhibitoren
BR112021017957A2 (pt) * 2019-03-28 2021-11-23 Jiangsu Hengrui Medicine Co Derivado tienoeterocíclico, método de preparação do mesmo e uso médico do mesmo
CA3135070A1 (en) * 2019-03-29 2020-10-08 Jiangsu Hengrui Medicine Co., Ltd. Pyrroloheterocyclic derivative, preparation method therefor, and application thereof in medicine
US20220168250A1 (en) * 2019-05-16 2022-06-02 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 BRAFv6ooE 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
TWI765451B (zh) * 2019-12-06 2022-05-21 大陸商南京明德新藥研發有限公司 作為erk抑制劑的螺環類化合物及其應用
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
TWI825811B (zh) * 2021-06-28 2023-12-11 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
WO2023087027A1 (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
PT3237423T (pt) 2019-08-21
SI3237423T1 (sl) 2019-08-30
US20160375030A1 (en) 2016-12-29
KR20170083145A (ko) 2017-07-17
DK3237423T3 (da) 2019-07-22
TW201632530A (zh) 2016-09-16
IL252065A0 (en) 2017-07-31
MY178426A (en) 2020-10-13
KR101917972B1 (ko) 2018-11-12
ZA201702786B (en) 2019-02-27
ES2738406T3 (es) 2020-01-22
USRE48635E1 (en) 2021-07-13
JP6445701B2 (ja) 2018-12-26
HUE045933T2 (hu) 2020-01-28
SV2017005443A (es) 2018-08-27
US9469652B2 (en) 2016-10-18
PE20171043A1 (es) 2017-07-19
CR20170182A (es) 2017-06-21
JO3596B1 (ar) 2020-07-05
NZ731531A (en) 2018-12-21
DOP2017000122A (es) 2017-06-15
AU2015369983C1 (en) 2019-02-21
TWI704151B (zh) 2020-09-11
ME03490B (de) 2020-01-20
CN107108648A (zh) 2017-08-29
TR201909887T4 (tr) 2019-07-22
UA119686C2 (uk) 2019-07-25
CY1121831T1 (el) 2020-07-31
GT201700134A (es) 2018-11-23
EA201791133A1 (ru) 2017-10-31
AU2015369983A1 (en) 2017-05-25
ECSP17038500A (es) 2017-12-01
JP2017538768A (ja) 2017-12-28
PH12017501155A1 (en) 2017-11-27
US9526733B1 (en) 2016-12-27
CA2966559C (en) 2019-06-18
BR112017011130A2 (pt) 2017-12-26
CO2017005217A2 (es) 2017-09-20
HRP20191268T1 (hr) 2019-11-01
EA031659B1 (ru) 2019-02-28
RS59015B1 (sr) 2019-08-30
PH12017501155B1 (en) 2017-11-27
IL252065B (en) 2020-08-31
US20160176896A1 (en) 2016-06-23
AU2015369983B2 (en) 2018-08-23
CL2017001514A1 (es) 2018-02-09
AR102977A1 (es) 2017-04-05
MX371206B (es) 2020-01-22
MD3237423T2 (ro) 2019-11-30
MA41251A (fr) 2017-11-01
PL3237423T3 (pl) 2020-01-31
EP3237423A1 (de) 2017-11-01
MA41251B1 (fr) 2019-09-30
MX2017008242A (es) 2017-10-06
LT3237423T (lt) 2019-08-26
EP3237423B1 (de) 2019-06-05
CN107108648B (zh) 2019-07-12
TN2017000233A1 (en) 2018-10-19
WO2016106029A1 (en) 2016-06-30
CA2966559A1 (en) 2016-06-30

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