ZA200609975B - Pyrrole compounds as inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto - Google Patents

Pyrrole compounds as inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto Download PDF

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Publication number
ZA200609975B
ZA200609975B ZA200609975A ZA200609975A ZA200609975B ZA 200609975 B ZA200609975 B ZA 200609975B ZA 200609975 A ZA200609975 A ZA 200609975A ZA 200609975 A ZA200609975 A ZA 200609975A ZA 200609975 B ZA200609975 B ZA 200609975B
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ZA
South Africa
Prior art keywords
compound
aliphatic
optionally substituted
compound according
chloro
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ZA200609975A
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English (en)
Inventor
Martinez-Botella Gabriel
Michael R Hale
Maltais Fran Ois
Tang Qing
Straub Judith
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Vertex Pharma
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Publication of ZA200609975B publication Critical patent/ZA200609975B/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Cardiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Vascular Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
ZA200609975A 2004-05-14 2005-05-13 Pyrrole compounds as inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto ZA200609975B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US57130904P 2004-05-14 2004-05-14

Publications (1)

Publication Number Publication Date
ZA200609975B true ZA200609975B (en) 2008-02-27

Family

ID=35106760

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA200609975A ZA200609975B (en) 2004-05-14 2005-05-13 Pyrrole compounds as inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto

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US (6) US7354939B2 (ja)
EP (5) EP3305776B1 (ja)
JP (1) JP5132305B2 (ja)
CN (1) CN1976919A (ja)
AR (2) AR051735A1 (ja)
AU (1) AU2005245885B2 (ja)
BR (1) BRPI0511111A (ja)
CA (1) CA2566461C (ja)
CY (1) CY1122336T1 (ja)
DK (1) DK3305776T3 (ja)
ES (4) ES2897422T3 (ja)
HK (2) HK1203505A1 (ja)
HU (1) HUE047130T2 (ja)
IL (1) IL179207A0 (ja)
LT (1) LT3305776T (ja)
MX (1) MXPA06013209A (ja)
NO (1) NO20065727L (ja)
NZ (1) NZ551582A (ja)
PL (1) PL3305776T3 (ja)
PT (1) PT3305776T (ja)
RU (1) RU2376299C2 (ja)
SI (1) SI3305776T1 (ja)
TW (1) TW200607803A (ja)
UA (1) UA84930C2 (ja)
WO (1) WO2005113541A1 (ja)
ZA (1) ZA200609975B (ja)

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AU2004221881A1 (en) * 2003-03-13 2004-09-30 Vertex Pharmaceuticals Incorporated Compositions useful as protein kinase inhibitors
WO2005100342A1 (en) * 2004-03-26 2005-10-27 Vertex Pharmaceuticals, Incorporated Pyridine inhibitors of erk2 and uses thereof
AU2005245885B2 (en) * 2004-05-14 2011-01-20 Vertex Pharmaceuticals, Incorporated Pyrrole compounds as inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto
US8546404B2 (en) 2005-12-13 2013-10-01 Merck Sharp & Dohme Compounds that are ERK inhibitors
EP1984331B1 (en) 2006-02-16 2010-10-20 Schering Corporation Pyrrolidine derivatives as erk inhibitors
WO2008153858A1 (en) * 2007-06-05 2008-12-18 Schering Corporation Polycyclic indazole derivatives and their use as erk inhibitors for the treatment of cancer
ES2556353T3 (es) 2008-02-21 2016-01-15 Merck Sharp & Dohme Corp. Compuestos que son inhibidores de las ERK
CN102146074B (zh) * 2011-01-26 2013-02-06 江苏先声药物研究有限公司 吡咯衍生物的制备方法及应用
WO2012172093A1 (en) 2011-06-17 2012-12-20 Merz Pharma Gmbh & Co. Kgaa Dihydroindolizine derivate as metabotropic glutamate receptor modulators
CA2926645C (en) 2013-10-14 2022-10-25 Indiana University Research And Technology Corporation Use of acamprosate to modulate erk 1/2 activation in animal models for fxs and asd and individuals diagnosed with fxs and asd
JPWO2015060368A1 (ja) 2013-10-23 2017-03-09 武田薬品工業株式会社 複素環化合物
US10668055B2 (en) 2013-12-20 2020-06-02 Biomed Valley Discoveries, Inc. Cancer treatment using combinations of ERK and RAF inhibitors
WO2015095835A1 (en) * 2013-12-20 2015-06-25 Biomed Valley Discoveries, Inc. Methods of modulating radioiodine uptake for the treatment of radioiodine-refractory cancers
WO2015095840A1 (en) 2013-12-20 2015-06-25 Biomed Valley Discoveries, Inc. Cancer treatments using combinations of cdk and erk inhibitors
WO2015095807A1 (en) * 2013-12-20 2015-06-25 Biomed Valley Discoveries, Inc. Cancer treatments using combinations of egfr and erk inhibitors
WO2015095831A1 (en) * 2013-12-20 2015-06-25 Biomed Valley Discoveries, Inc. Cancer treatments using combinations of mtor and erk inhibitors
WO2015095833A1 (en) * 2013-12-20 2015-06-25 Biomed Valley Discoveries, Inc. Treatment of hematologic cancers
WO2015095842A2 (en) * 2013-12-20 2015-06-25 Biomed Valley Discoveries, Inc. Methods and compositions for treating non-erk mapk pathway inhibitor-resistant cancers
ES2918375T3 (es) 2013-12-20 2022-07-15 Biomed Valley Discoveries Inc Tratamientos contra el cáncer usando combinaciones de inhibidores de la ruta de PI3K/Akt y ERK
EP3082779B1 (en) * 2013-12-20 2023-06-07 Biomed Valley Discoveries, Inc. Cancer treatments using combinations of type 2 mek and erk inhibitors
AU2014368925A1 (en) * 2013-12-20 2016-07-21 Biomed Valley Discoveries, Inc. Cancer treatments using combinations of MEK type I and ERK inhibitors
AU2016211246B2 (en) * 2015-01-30 2020-08-27 Biomed Valley Discoveries, Inc. Crystalline forms of C21H22CI2N4O2
WO2016123581A1 (en) * 2015-01-30 2016-08-04 Biomed Valley Discoveries, Inc. Crystalline c21h22c12n4o2 malonate
WO2016187028A1 (en) * 2015-05-15 2016-11-24 Celgene Avilomics Research, Inc. Heteroaryl compounds, synthesis thereof, and intermediates thereto
WO2016192063A1 (en) * 2015-06-03 2016-12-08 Changzhou Jiekai Pharmatech Co. Ltd Heterocyclic compounds as erk inhibitors
CN106536522B (zh) * 2015-06-03 2020-08-28 捷思英达医药技术(上海)有限公司 用于治疗银屑病的杂环化合物
EP3365334B1 (en) 2015-10-21 2024-07-17 Otsuka Pharmaceutical Co., Ltd. Benzolactam compounds as protein kinase inhibitors
EP3170822A1 (en) 2015-11-18 2017-05-24 AGV Discovery Azaindole derivatives and their use as erk kinase inhibitors
CN109890827A (zh) * 2016-10-05 2019-06-14 芝诺罗耶尔蒂里程碑有限责任公司 螺环化合物
GB201706327D0 (en) 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound
US11406627B2 (en) * 2017-10-12 2022-08-09 Novartis Ag Combinations of MDM2 inhibitors with inhibitors of ERK for treating cancers
WO2019180141A1 (en) 2018-03-23 2019-09-26 Bayer Aktiengesellschaft Combinations of rogaratinib
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WO2023169480A1 (zh) * 2022-03-08 2023-09-14 甘李药业股份有限公司 氘代化合物,及其制备方法和应用
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US7304061B2 (en) * 2002-04-26 2007-12-04 Vertex Pharmaceuticals Incorporated Heterocyclic inhibitors of ERK2 and uses thereof
EP1554269A1 (en) * 2002-07-09 2005-07-20 Vertex Pharmaceuticals Incorporated Imidazoles, oxazoles and thiazoles with protein kinase inhibiting activities
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AU2005245885B2 (en) * 2004-05-14 2011-01-20 Vertex Pharmaceuticals, Incorporated Pyrrole compounds as inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto

Also Published As

Publication number Publication date
ES2751761T3 (es) 2020-04-01
EP3608315B1 (en) 2021-08-11
HK1203505A1 (en) 2015-10-30
USRE47318E1 (en) 2019-03-26
HUE047130T2 (hu) 2020-04-28
CN1976919A (zh) 2007-06-06
US20060106069A1 (en) 2006-05-18
EP2799434A1 (en) 2014-11-05
EP1753738A1 (en) 2007-02-21
JP2007537295A (ja) 2007-12-20
US20230183276A1 (en) 2023-06-15
USRE49500E1 (en) 2023-04-25
UA84930C2 (ru) 2008-12-10
NO20065727L (no) 2006-12-12
EP3305776B1 (en) 2019-09-25
RU2006144445A (ru) 2008-06-20
ES2513965T3 (es) 2014-10-27
AR051735A1 (es) 2007-02-07
US7354939B2 (en) 2008-04-08
USRE48266E1 (en) 2020-10-20
CA2566461C (en) 2012-07-10
AU2005245885B2 (en) 2011-01-20
BRPI0511111A (pt) 2007-11-27
WO2005113541A1 (en) 2005-12-01
ES2897422T3 (es) 2022-03-01
JP5132305B2 (ja) 2013-01-30
EP3943489A1 (en) 2022-01-26
MXPA06013209A (es) 2007-01-16
RU2376299C2 (ru) 2009-12-20
NZ551582A (en) 2011-01-28
CA2566461A1 (en) 2005-12-01
DK3305776T3 (da) 2019-12-09
IL179207A0 (en) 2007-03-08
LT3305776T (lt) 2020-01-10
CY1122336T1 (el) 2021-01-27
USRE46097E1 (en) 2016-08-09
EP3608315A1 (en) 2020-02-12
ES2651439T3 (es) 2018-01-26
PT3305776T (pt) 2019-12-17
TW200607803A (en) 2006-03-01
EP2799434B1 (en) 2017-08-02
EP1753738B1 (en) 2014-07-09
EP3305776A1 (en) 2018-04-11
HK1247910A1 (zh) 2018-10-05
AU2005245885A1 (en) 2005-12-01
AR106755A2 (es) 2018-02-14
PL3305776T3 (pl) 2020-03-31
SI3305776T1 (sl) 2020-01-31

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