CA2924584A1 - Inhibitors of erk and methods of use - Google Patents

Inhibitors of erk and methods of use Download PDF

Info

Publication number
CA2924584A1
CA2924584A1 CA2924584A CA2924584A CA2924584A1 CA 2924584 A1 CA2924584 A1 CA 2924584A1 CA 2924584 A CA2924584 A CA 2924584A CA 2924584 A CA2924584 A CA 2924584A CA 2924584 A1 CA2924584 A1 CA 2924584A1
Authority
CA
Canada
Prior art keywords
alkyl
10hetaryl
10aryl
aryl
10alkenyl
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA2924584A
Other languages
English (en)
French (fr)
Inventor
Liansheng Li
Tao Wu
Jun Feng
Pingda Ren
Yi Liu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Kura Oncology Inc
Original Assignee
Kura Oncology Inc
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 Kura Oncology Inc filed Critical Kura Oncology Inc
Publication of CA2924584A1 publication Critical patent/CA2924584A1/en
Abandoned legal-status Critical Current

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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • 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
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/55171,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
CA2924584A 2013-10-03 2014-10-03 Inhibitors of erk and methods of use Abandoned CA2924584A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361886552P 2013-10-03 2013-10-03
US61/886,552 2013-10-03
US201462032446P 2014-08-01 2014-08-01
US62/032,446 2014-08-01
PCT/US2014/059197 WO2015051341A1 (en) 2013-10-03 2014-10-03 Inhibitors of erk and methods of use

Publications (1)

Publication Number Publication Date
CA2924584A1 true CA2924584A1 (en) 2015-04-09

Family

ID=52779215

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2924584A Abandoned CA2924584A1 (en) 2013-10-03 2014-10-03 Inhibitors of erk and methods of use

Country Status (28)

Country Link
US (4) US9624228B2 (https=)
EP (2) EP3363800A1 (https=)
JP (2) JP6427197B2 (https=)
KR (1) KR20160081908A (https=)
CN (2) CN105636586B (https=)
AU (2) AU2014331628B2 (https=)
BR (1) BR112016006994A8 (https=)
CA (1) CA2924584A1 (https=)
CY (1) CY1120095T1 (https=)
DK (1) DK3052096T3 (https=)
EA (1) EA032196B1 (https=)
ES (1) ES2664794T3 (https=)
HK (1) HK1255851A1 (https=)
HR (1) HRP20180538T1 (https=)
HU (1) HUE036600T2 (https=)
IL (1) IL244488A0 (https=)
LT (1) LT3052096T (https=)
ME (1) ME02991B (https=)
MX (1) MX2016004163A (https=)
PH (1) PH12016500432A1 (https=)
PL (1) PL3052096T3 (https=)
PT (1) PT3052096T (https=)
RS (1) RS57058B1 (https=)
SG (1) SG11201602572YA (https=)
SI (1) SI3052096T1 (https=)
SM (1) SMT201800205T1 (https=)
WO (1) WO2015051341A1 (https=)
ZA (1) ZA201601701B (https=)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3363800A1 (en) 2013-10-03 2018-08-22 Kura Oncology, Inc. Heterocyclic inhibitors of erk and methods of use
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
CN110506038B (zh) 2017-03-28 2023-11-24 巴斯夫欧洲公司 杀害虫化合物
WO2018183762A1 (en) 2017-03-29 2018-10-04 United States Government As Represented By The Department Of Veterans Affairs Methods and compositions for treating cancer
US20200247815A1 (en) * 2017-10-19 2020-08-06 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Pyrazolyl-containing tricyclic derivative, preparation method therefor and use thereof
CN109761986B (zh) * 2017-11-10 2021-10-08 上海翰森生物医药科技有限公司 三并环类衍生物抑制剂、其制备方法和应用
CN107879989B (zh) * 2017-11-29 2020-01-03 重庆市中药研究院 具有生物活性的3,4,5-取代苯并二氮卓2-酮类药物分子及其制备方法
EP3643705A1 (en) 2018-10-24 2020-04-29 Basf Se Pesticidal compounds
MX2021005171A (es) 2018-11-16 2021-10-01 California Inst Of Techn Inhibidores de cinasas reguladas por señal extracelular (erk) y usos de los mismos.
CN112020357B (zh) * 2019-04-02 2023-08-29 上海翰森生物医药科技有限公司 含吲唑基的三并环类衍生物的盐及其晶型
EP3766879A1 (en) 2019-07-19 2021-01-20 Basf Se Pesticidal pyrazole derivatives
WO2022075445A1 (ja) * 2020-10-08 2022-04-14 株式会社Adeka ポリオレフィン系樹脂組成物、それを用いた成形品、及びポリオレフィン系樹脂組成物の製造方法
EP4198023A1 (en) 2021-12-16 2023-06-21 Basf Se Pesticidally active thiosemicarbazone compounds
US20250197358A1 (en) 2022-02-17 2025-06-19 Basf Se Pesticidally active thiosemicarbazone compounds
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2024240859A1 (en) 2023-05-25 2024-11-28 Basf Se Lactam pesticidal compounds
EP4467535A1 (en) 2023-05-25 2024-11-27 Basf Se Lactam pesticidal compounds
IL326136A (en) 2023-08-07 2026-03-01 Revolution Medicines Inc RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein
TW202529768A (zh) 2023-09-29 2025-08-01 大陸商德昇濟醫藥(無錫)有限公司 癌症治療的療法
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
US20250375445A1 (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
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
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
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

Family Cites Families (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3657744A (en) 1970-05-08 1972-04-25 Univ Minnesota Method for fixing prosthetic implants in a living body
BE791816R (fr) 1971-11-24 1973-05-23 Sandoz Sa Derives de la quinazolinone, leur preparation et medicaments contenant ces
US3984556A (en) * 1973-01-19 1976-10-05 Sandoz, Inc. Alkyl-substituted-tricyclic quinazolinones for lowering blood pressure
US4042704A (en) 1976-03-18 1977-08-16 Sandoz, Inc. Benzindazoles
US4352931A (en) 1980-05-22 1982-10-05 Siegfried Aktiengesellschaft Lin-benzoaminopurinols
US4733665C2 (en) 1985-11-07 2002-01-29 Expandable Grafts Partnership Expandable intraluminal graft and method and apparatus for implanting an expandable intraluminal graft
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US5061273A (en) 1989-06-01 1991-10-29 Yock Paul G Angioplasty apparatus facilitating rapid exchanges
US5350395A (en) 1986-04-15 1994-09-27 Yock Paul G Angioplasty apparatus facilitating rapid exchanges
US5040548A (en) 1989-06-01 1991-08-20 Yock Paul G Angioplasty mehtod
US4748982A (en) 1987-01-06 1988-06-07 Advanced Cardiovascular Systems, Inc. Reinforced balloon dilatation catheter with slitted exchange sleeve and method
DE3701277A1 (de) * 1987-01-17 1988-07-28 Boehringer Mannheim Gmbh Neue tricyclische benzimidazole, verfahren zu ihrer herstellung und verwendung als arzneimittel
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
CA1322628C (en) 1988-10-04 1993-10-05 Richard A. Schatz Expandable intraluminal graft
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
US6344053B1 (en) 1993-12-22 2002-02-05 Medtronic Ave, Inc. Endovascular support device and method
US5674278A (en) 1989-08-24 1997-10-07 Arterial Vascular Engineering, Inc. Endovascular support device
US5292331A (en) 1989-08-24 1994-03-08 Applied Vascular Engineering, Inc. Endovascular support device
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
IL112248A0 (en) * 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
DK0821671T3 (da) 1995-04-20 2001-04-23 Pfizer Arylsulfonylhydroxamsyrederivater som MMP- og TNF-inhibitorer
DE69624081T2 (de) 1995-12-20 2003-06-12 Agouron Pharmaceuticals, Inc. Matrix-metalloprotease Inhibitoren
EP0923585B1 (en) 1996-07-18 2002-05-08 Pfizer Inc. Phosphinate based inhibitors of matrix metalloproteases
WO1998007697A1 (en) 1996-08-23 1998-02-26 Pfizer Inc. Arylsulfonylamino hydroxamic acid derivatives
WO1998030566A1 (en) 1997-01-06 1998-07-16 Pfizer Inc. Cyclic sulfone derivatives
EP0977733B1 (en) 1997-02-03 2003-09-03 Pfizer Products Inc. Arylsulfonylamino hydroxamic acid derivatives
JP2000507975A (ja) 1997-02-07 2000-06-27 ファイザー・インク N−ヒドロキシ−β−スルホニルプロピオンアミド誘導体類及びそれらのマトリックスメタロプロテイナーゼ阻害薬としての使用
EA002546B1 (ru) 1997-02-11 2002-06-27 Пфайзер Инк. Производные арилсульфонилгидроксамовой кислоты
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
US6087368A (en) 1998-06-08 2000-07-11 Bristol-Myers Squibb Company Quinazolinone inhibitors of cGMP phosphodiesterase
US6562836B1 (en) * 1999-05-24 2003-05-13 Queen's University Of Kingston Methods and compounds for inhibiting amyloid deposits
EP1317450B1 (en) 2000-09-15 2006-11-22 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
JP3896309B2 (ja) * 2001-07-09 2007-03-22 ファイザー株式会社 プロテインキナーゼc阻害物質としてのピラゾロキノリノン誘導体
US7119111B2 (en) 2002-05-29 2006-10-10 Amgen, Inc. 2-oxo-1,3,4-trihydroquinazolinyl derivatives and methods of use
AR045595A1 (es) 2003-09-04 2005-11-02 Vertex Pharma Composiciones utiles como inhibidores de proteinas quinasas
US20050203063A1 (en) * 2003-09-12 2005-09-15 Raymond Deshaies Proteasome pathway inhibitors and related methods
US7244757B2 (en) 2004-04-01 2007-07-17 Pfizer Inc Pyrazole-amine compounds for the treatment of neurodegenerative disorders
US7384930B2 (en) 2004-11-03 2008-06-10 Bristol-Myers Squibb Company Constrained compounds as CGRP-receptor antagonists
MX2008010635A (es) 2006-02-16 2008-10-28 Schering Corp Derivados de pirrolidina como inhibidores de cinasa regulada por señales extracelulares.
AR068046A1 (es) 2007-06-05 2009-11-04 Schering Corp Derivados policiclicos de indazol y su uso como inhibidores de erk para el tratamiento del cancer
WO2008156739A1 (en) 2007-06-18 2008-12-24 Schering Corporation Heterocyclic compounds and use thereof as erk inhibitors
DK2217597T3 (da) 2007-10-01 2011-06-20 Comentis Inc Quinuclidin-4-ylmethyl-1h-indol-3-carboxylatderivater som alpha-7-nicotin-acetylcholin-receptor-ligander til behandling af Alzheimers sygdom
WO2009105500A1 (en) 2008-02-21 2009-08-27 Schering Corporation Compounds that are erk inhibitors
US8022227B2 (en) 2008-08-27 2011-09-20 The Ohio State University Method of synthesizing 1H-indazole compounds
EP2408448A4 (en) 2009-03-18 2012-09-19 Univ Leland Stanford Junior METHODS AND COMPOSITIONS FOR TREATING INFECTION WITH A FLAVIVIRIDAE FAMILY VIRUS
SI2455381T1 (sl) * 2009-07-17 2014-08-29 Japan Tobacco Inc. Triazolopiridinova spojina in njeno delovanje kot zaviralec prolil-hidroksilaze in induktor produkcije eritropoietina
JP2013506669A (ja) 2009-09-30 2013-02-28 メルク・シャープ・アンド・ドーム・コーポレーション Erk阻害剤である新規化合物
WO2012030685A2 (en) 2010-09-01 2012-03-08 Schering Corporation Indazole derivatives useful as erk inhibitors
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
EP3536319A1 (en) 2010-10-29 2019-09-11 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
EP2654748B1 (en) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
WO2012170845A2 (en) * 2011-06-08 2012-12-13 Heffernan Michele L R Metabotropic glutamate receptor 5 modulators and methods of use thereof
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
WO2014052566A1 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
WO2014052563A2 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
WO2014134772A1 (en) 2013-03-04 2014-09-12 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
US9745307B2 (en) 2013-04-30 2017-08-29 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
EP3363800A1 (en) 2013-10-03 2018-08-22 Kura Oncology, Inc. Heterocyclic inhibitors of erk and methods of use
WO2016095089A1 (en) 2014-12-15 2016-06-23 Merck Sharp & Dohme Corp. Erk inhibitors
WO2016095088A1 (en) 2014-12-15 2016-06-23 Merck Sharp & Dohme Corp. Erk inhibitors
CN107001322B (zh) 2014-12-18 2020-07-28 默沙东公司 用于药物制剂的组合物
MX2017008078A (es) 2014-12-19 2017-09-28 Merck Sharp & Dohme Composiciones de (s)-n-(3-(6-isopropoxipiridin-3-il)-1h-indazol-5- il)-1-(2-(4-(4-(1-metil-1h-1,2,4-triazol-3-il)fenil)-3,6-dihidrop iridin-1(2h)-il)-2-oxoetil)-3-(metiltio)pirrolidin-3-carboxamida para preparaciones farmaceuticas.
TWI704151B (zh) 2014-12-22 2020-09-11 美商美國禮來大藥廠 Erk抑制劑

Also Published As

Publication number Publication date
ME02991B (me) 2018-10-20
JP2019031549A (ja) 2019-02-28
EP3363800A1 (en) 2018-08-22
EA201690708A1 (ru) 2016-12-30
IL244488A0 (en) 2016-04-21
EP3052096A4 (en) 2017-03-15
PL3052096T3 (pl) 2018-07-31
SG11201602572YA (en) 2016-04-28
JP2016531952A (ja) 2016-10-13
CN105636586B (zh) 2018-05-29
MX2016004163A (es) 2016-09-07
ZA201601701B (en) 2019-09-25
AU2018250439A1 (en) 2018-11-15
BR112016006994A8 (pt) 2020-02-27
SMT201800205T1 (it) 2018-05-02
US20170226110A1 (en) 2017-08-10
EP3052096B1 (en) 2018-01-17
EP3052096B8 (en) 2018-03-07
US9624228B2 (en) 2017-04-18
HK1255851A1 (en) 2019-08-30
AU2014331628A1 (en) 2016-03-24
US9951078B2 (en) 2018-04-24
PH12016500432B1 (en) 2016-05-16
EP3052096A1 (en) 2016-08-10
SI3052096T1 (en) 2018-04-30
AU2014331628B2 (en) 2018-08-30
DK3052096T3 (en) 2018-03-12
PT3052096T (pt) 2018-04-04
CY1120095T1 (el) 2018-12-12
EA032196B1 (ru) 2019-04-30
KR20160081908A (ko) 2016-07-08
ES2664794T3 (es) 2018-04-23
CN108864102A (zh) 2018-11-23
BR112016006994A2 (pt) 2017-08-01
LT3052096T (lt) 2018-04-10
WO2015051341A1 (en) 2015-04-09
JP6427197B2 (ja) 2018-11-21
CN105636586A (zh) 2016-06-01
HRP20180538T1 (hr) 2018-05-04
US10301317B2 (en) 2019-05-28
HUE036600T2 (hu) 2018-07-30
US20190292194A1 (en) 2019-09-26
US20180237444A1 (en) 2018-08-23
RS57058B1 (sr) 2018-05-31
PH12016500432A1 (en) 2016-05-16
US20160237091A1 (en) 2016-08-18

Similar Documents

Publication Publication Date Title
CA2924584A1 (en) Inhibitors of erk and methods of use
JP7586834B2 (ja) Shp2拮抗薬としてのピリミジノン誘導体
ES2900184T3 (es) Combinaciones terapéuticas de un inhibidor de BTK y un inhibidor de BCL-2
JP6404717B2 (ja) アミドスピロ環状アミド及びスルホンアミド誘導体
IL293962B2 (en) Mutant KRAS protein inhibitors
AU2014327235B2 (en) New 3-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-c]pyridine derivatives as NIK inhibitors
CN114163457A (zh) 嘧啶并五元氮杂环化合物及其用途
CA3103385A1 (en) 3-(5-hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and their use in the treatment of ikaros family zinc finger 2 (ikzf2)-dependent diseases
BRPI0920500B1 (pt) Inibidores de quinase benzoxazola e métodos de uso
BR112021018704B1 (pt) Derivado de heteroarila, método para produção do mesmo, e composição farmacêutica compreendendo a mesma como componente eficaz
AU2018380132B2 (en) Tubulin inhibitors
WO2012007926A1 (en) Substituted imidazoquinoline derivatives as kinase inhibitors
KR20150005645A (ko) Dna-pk 억제제
WO2012125544A2 (en) Necroptosis inhibitors and methods of use therefor
KR20170066447A (ko) Nik 억제제로서의 신규 티에노피리미딘 유도체
JP2021121599A (ja) ヒストンデメチラーゼ阻害剤
CN113968856B (zh) 一类具有激酶抑制活性的化合物
CN118055933A (zh) 选择性parp1抑制剂及其应用
KR20250054814A (ko) Cdk4 키나아제 억제제로 사용되는 화합물 및 이의 용도
JP2023527204A (ja) 3,4-ジヒドロイソキノリン系化合物及びその使用
CN106366085A (zh) 异喹啉酮类化合物或其盐及其制备方法和用途
BR112017004035B1 (pt) Inibidores macrocíclicos de rip2 quinase e composições farmacêuticas
JP2008521855A (ja) 新規ピリドチエノピリミジン誘導体
CN110003171B (zh) 治疗类风湿性关节炎的小分子可逆性btk抑制剂
CN118994200A (zh) 三并环类PI3Kα抑制剂及其制备方法和医药用途

Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20220406