CN103025740B - 蛋白酪氨酸激酶活性的抑制剂及其治疗眼科疾病的用途 - Google Patents

蛋白酪氨酸激酶活性的抑制剂及其治疗眼科疾病的用途 Download PDF

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Publication number
CN103025740B
CN103025740B CN201180029735.1A CN201180029735A CN103025740B CN 103025740 B CN103025740 B CN 103025740B CN 201180029735 A CN201180029735 A CN 201180029735A CN 103025740 B CN103025740 B CN 103025740B
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compound
acid
base
reaction mixture
methyl
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Expired - Fee Related
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Chinese (zh)
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CN103025740A (zh
Inventor
S.雷佩尔
战莉洁
S.W.克拉里奇
F.雷佩尔
F.高德特
A.韦斯伯格
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Methylgene Inc
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Methylgene Inc
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    • 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
    • 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/005Enzyme inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • 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
    • 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
    • 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
    • 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
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201180029735.1A 2010-04-16 2011-04-08 蛋白酪氨酸激酶活性的抑制剂及其治疗眼科疾病的用途 Expired - Fee Related CN103025740B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US32480310P 2010-04-16 2010-04-16
US61/324,803 2010-04-16
PCT/CA2011/000390 WO2011127565A1 (en) 2010-04-16 2011-04-08 Inhibitors of protein tyrosine kinase activity and use thereof to treat ophthalmic disorders

Publications (2)

Publication Number Publication Date
CN103025740A CN103025740A (zh) 2013-04-03
CN103025740B true CN103025740B (zh) 2015-07-01

Family

ID=44788641

Family Applications (2)

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CN201180029735.1A Expired - Fee Related CN103025740B (zh) 2010-04-16 2011-04-08 蛋白酪氨酸激酶活性的抑制剂及其治疗眼科疾病的用途
CN2011800297313A Pending CN102947315A (zh) 2010-04-16 2011-04-08 蛋白酪氨酸激酶活性抑制剂

Family Applications After (1)

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CN2011800297313A Pending CN102947315A (zh) 2010-04-16 2011-04-08 蛋白酪氨酸激酶活性抑制剂

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US (3) US8455484B2 (US07846941-20101207-C00217.png)
EP (2) EP2563794A4 (US07846941-20101207-C00217.png)
JP (2) JP2013525286A (US07846941-20101207-C00217.png)
KR (2) KR20130100234A (US07846941-20101207-C00217.png)
CN (2) CN103025740B (US07846941-20101207-C00217.png)
AR (2) AR080871A1 (US07846941-20101207-C00217.png)
AU (2) AU2011241422B2 (US07846941-20101207-C00217.png)
CA (2) CA2796008A1 (US07846941-20101207-C00217.png)
CO (2) CO6630193A2 (US07846941-20101207-C00217.png)
EA (2) EA201291055A1 (US07846941-20101207-C00217.png)
MX (2) MX2012012031A (US07846941-20101207-C00217.png)
MY (1) MY157319A (US07846941-20101207-C00217.png)
NZ (2) NZ602948A (US07846941-20101207-C00217.png)
SG (2) SG184883A1 (US07846941-20101207-C00217.png)
TW (2) TW201204734A (US07846941-20101207-C00217.png)
UA (1) UA108878C2 (US07846941-20101207-C00217.png)
WO (2) WO2011127565A1 (US07846941-20101207-C00217.png)
ZA (2) ZA201207482B (US07846941-20101207-C00217.png)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2495044C2 (ru) * 2007-08-29 2013-10-10 Метилджен Инк. Ингибиторы активности протеинтирозинкиназы
EP2262815A4 (en) * 2008-03-05 2012-04-11 Methylgene Inc Inhibitors of protein intolerance activity
JP2013525286A (ja) * 2010-04-16 2013-06-20 メチルジーン・インコーポレイテッド タンパク質チロシンキナーゼ活性の阻害剤
US20130090327A1 (en) * 2011-09-30 2013-04-11 Methylgene Inc. Inhibitors of Protein Tyrosine Kinase Activity
US20130096088A1 (en) * 2011-09-30 2013-04-18 Methylgene Inc. Inhibitors of Protein Tyrosine Kinase Activity
US20130096135A1 (en) * 2011-09-30 2013-04-18 Methylgene Inc. Selected Inhibitors of Protein Tyrosine Kinase Activity
ES2593533T3 (es) 2011-12-15 2016-12-09 Pfizer Limited Derivados de sulfonamida
US10544117B2 (en) 2014-09-10 2020-01-28 Temple University—Of the Commonwealth System of Higher Education 5-hydroxytryptamine receptor 7 activity modulators and their method of use
US20180221365A1 (en) * 2015-05-12 2018-08-09 Temple University-Of The Commonwealth System Of Higher Education Novel sigma-2 receptor binders and their method of use
CN108530464B (zh) * 2017-03-02 2020-10-27 深圳海王医药科技研究院有限公司 一种多靶点激酶抑制剂

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2603125A1 (en) * 2005-03-28 2006-10-05 Kirin Pharma Kabushiki Kaisha Thienopyridine derivative, quinoline derivatives,and quinazoline derivatives, having c-met autophosphorylation inhibiting activity
CN1856498A (zh) * 2003-07-24 2006-11-01 艾博特公司 噻吩并吡啶和呋喃并吡啶激酶抑制剂
CA2605680A1 (en) * 2005-04-27 2006-11-02 Amgen Inc. Substituted amide derivatives as protein kinase inhibitors
US20070004675A1 (en) * 2005-05-20 2007-01-04 Methylgene, Inc. Inhibitors of VEGF receptor and HGF receptor signaling
CA2608726A1 (en) * 2005-05-20 2007-05-18 Methylgene Inc. Inhibitors of vegf receptor and hgf receptor signaling
WO2009026717A1 (en) * 2007-08-29 2009-03-05 Methylgene Inc. Inhibitors of protein tyrosine kinase activity
WO2009109035A1 (en) * 2008-03-05 2009-09-11 Methylgene Inc. Inhibitors of protein tyrosine kinase activity

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2438017T3 (es) * 2004-07-30 2014-01-15 Methylgene Inc. Inhibidores de la señalización del receptor del VEGF y del receptor del HGF
US8907091B2 (en) 2007-08-29 2014-12-09 Methylgene Inc. Processes and intermediates for preparing fused heterocyclic kinase inhibitors
JP2013525286A (ja) * 2010-04-16 2013-06-20 メチルジーン・インコーポレイテッド タンパク質チロシンキナーゼ活性の阻害剤
US20130096088A1 (en) * 2011-09-30 2013-04-18 Methylgene Inc. Inhibitors of Protein Tyrosine Kinase Activity

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1856498A (zh) * 2003-07-24 2006-11-01 艾博特公司 噻吩并吡啶和呋喃并吡啶激酶抑制剂
CA2603125A1 (en) * 2005-03-28 2006-10-05 Kirin Pharma Kabushiki Kaisha Thienopyridine derivative, quinoline derivatives,and quinazoline derivatives, having c-met autophosphorylation inhibiting activity
CA2605680A1 (en) * 2005-04-27 2006-11-02 Amgen Inc. Substituted amide derivatives as protein kinase inhibitors
US20070004675A1 (en) * 2005-05-20 2007-01-04 Methylgene, Inc. Inhibitors of VEGF receptor and HGF receptor signaling
CA2608726A1 (en) * 2005-05-20 2007-05-18 Methylgene Inc. Inhibitors of vegf receptor and hgf receptor signaling
WO2009026717A1 (en) * 2007-08-29 2009-03-05 Methylgene Inc. Inhibitors of protein tyrosine kinase activity
WO2009109035A1 (en) * 2008-03-05 2009-09-11 Methylgene Inc. Inhibitors of protein tyrosine kinase activity

Also Published As

Publication number Publication date
CO6630193A2 (es) 2013-03-01
AU2011241422B2 (en) 2015-05-07
AU2011241420B2 (en) 2015-04-16
TW201204735A (en) 2012-02-01
ZA201207557B (en) 2013-06-26
NZ602948A (en) 2014-09-26
ZA201207482B (en) 2013-09-25
EP2563795A4 (en) 2013-10-23
MY157319A (en) 2016-05-31
MX2012012031A (es) 2012-12-17
WO2011127565A1 (en) 2011-10-20
US20110257100A1 (en) 2011-10-20
US8455484B2 (en) 2013-06-04
JP2013523846A (ja) 2013-06-17
NZ602954A (en) 2014-11-28
CA2796054A1 (en) 2011-10-20
JP2013525286A (ja) 2013-06-20
CO6640224A2 (es) 2013-03-22
AU2011241422A1 (en) 2012-11-01
AR080871A1 (es) 2012-05-16
KR20130058006A (ko) 2013-06-03
EA201291055A1 (ru) 2013-09-30
AR080875A1 (es) 2012-05-16
US20110257175A1 (en) 2011-10-20
EA201291052A1 (ru) 2013-04-30
KR20130100234A (ko) 2013-09-10
EP2563795A1 (en) 2013-03-06
EP2563794A1 (en) 2013-03-06
MX2012012032A (es) 2012-12-17
US20140315801A1 (en) 2014-10-23
CN103025740A (zh) 2013-04-03
SG184883A1 (en) 2012-11-29
UA108878C2 (ru) 2015-06-25
SG184882A1 (en) 2012-11-29
CA2796008A1 (en) 2011-10-20
EP2563794A4 (en) 2013-12-04
CN102947315A (zh) 2013-02-27
US8906852B2 (en) 2014-12-09
WO2011127567A1 (en) 2011-10-20
TW201204734A (en) 2012-02-01

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