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

Info

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
Authority
CN
China
Prior art keywords
mmol
compound
pyridin
compounds
reaction mixture
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.)
Expired - Fee Related
Application number
CN201180029735.1A
Other languages
English (en)
Chinese (zh)
Other versions
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
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.)
Methylgene Inc
Original Assignee
Methylgene 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 Methylgene Inc filed Critical Methylgene Inc
Publication of CN103025740A publication Critical patent/CN103025740A/zh
Application granted granted Critical
Publication of CN103025740B publication Critical patent/CN103025740B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/4365—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/005—Enzyme inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides

Landscapes

  • 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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Ophthalmology & Optometry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (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)
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)

Application Number Title Priority Date Filing Date
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)

Application Number Title Priority Date Filing Date
CN2011800297313A Pending CN102947315A (zh) 2010-04-16 2011-04-08 蛋白酪氨酸激酶活性抑制剂

Country Status (19)

Country Link
US (3) US8455484B2 (enExample)
EP (2) EP2563794A4 (enExample)
JP (2) JP2013523846A (enExample)
KR (2) KR20130100234A (enExample)
CN (2) CN103025740B (enExample)
AR (2) AR080871A1 (enExample)
AU (2) AU2011241420B2 (enExample)
CA (2) CA2796008A1 (enExample)
CO (2) CO6630193A2 (enExample)
EA (2) EA201291055A1 (enExample)
MX (2) MX2012012032A (enExample)
MY (1) MY157319A (enExample)
NZ (2) NZ602948A (enExample)
PH (2) PH12012502073A1 (enExample)
SG (2) SG184882A1 (enExample)
TW (2) TW201204735A (enExample)
UA (1) UA108878C2 (enExample)
WO (2) WO2011127567A1 (enExample)
ZA (2) ZA201207482B (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2635131T3 (es) * 2007-08-29 2017-10-02 Methylgene Inc. Inhibidores de la actividad de la proteína tirosina cinasa
BRPI0923670A2 (pt) * 2008-03-05 2013-07-30 Methylgene Inc inibidores da atividade de proteÍna tirosina quinase e seu uso, bem como composiÇço compreendendo os mesmos
MY157319A (en) * 2010-04-16 2016-05-31 Methylgene Inc Inhibitors of protein tyrosine kinase activity
US20130090327A1 (en) * 2011-09-30 2013-04-11 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
WO2013044361A1 (en) * 2011-09-30 2013-04-04 Methylgene Inc. Inhibitors of protein tyrosine kinase activity
EP2791108B1 (en) 2011-12-15 2016-07-27 Pfizer Limited Sulfonamide derivatives
WO2016040554A1 (en) 2014-09-10 2016-03-17 Temple University-Of The Commonwealth System Of Higher Education Novel 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
JP6664170B2 (ja) * 2015-08-31 2020-03-13 広栄化学工業株式会社 アミノヒドロキシピリジン化合物の製造方法
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
WO2006010264A1 (en) * 2004-07-30 2006-02-02 Methylgene, Inc. Inhibitors of vegf receptor and hgf receptor signaling
WO2009026720A1 (en) * 2007-08-29 2009-03-05 Methylgene Inc. Processes and intermediates for preparing fused heterocyclic kinase inhibitors
MY157319A (en) * 2010-04-16 2016-05-31 Methylgene Inc Inhibitors of protein tyrosine kinase activity
WO2013044361A1 (en) * 2011-09-30 2013-04-04 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
EA201291052A1 (ru) 2013-04-30
EA201291055A1 (ru) 2013-09-30
AR080875A1 (es) 2012-05-16
EP2563794A1 (en) 2013-03-06
PH12012502073A1 (en) 2013-02-11
ZA201207557B (en) 2013-06-26
JP2013525286A (ja) 2013-06-20
US8455484B2 (en) 2013-06-04
PH12012502070A1 (en) 2015-05-08
ZA201207482B (en) 2013-09-25
EP2563794A4 (en) 2013-12-04
NZ602954A (en) 2014-11-28
NZ602948A (en) 2014-09-26
AR080871A1 (es) 2012-05-16
UA108878C2 (ru) 2015-06-25
MX2012012032A (es) 2012-12-17
US20140315801A1 (en) 2014-10-23
TW201204735A (en) 2012-02-01
CO6630193A2 (es) 2013-03-01
WO2011127565A1 (en) 2011-10-20
US8906852B2 (en) 2014-12-09
CO6640224A2 (es) 2013-03-22
US20110257100A1 (en) 2011-10-20
CN102947315A (zh) 2013-02-27
MY157319A (en) 2016-05-31
SG184883A1 (en) 2012-11-29
EP2563795A4 (en) 2013-10-23
AU2011241422A1 (en) 2012-11-01
TW201204734A (en) 2012-02-01
KR20130058006A (ko) 2013-06-03
AU2011241420B2 (en) 2015-04-16
CN103025740A (zh) 2013-04-03
MX2012012031A (es) 2012-12-17
WO2011127567A1 (en) 2011-10-20
SG184882A1 (en) 2012-11-29
JP2013523846A (ja) 2013-06-17
CA2796008A1 (en) 2011-10-20
KR20130100234A (ko) 2013-09-10
AU2011241422B2 (en) 2015-05-07
CA2796054A1 (en) 2011-10-20
EP2563795A1 (en) 2013-03-06
US20110257175A1 (en) 2011-10-20

Similar Documents

Publication Publication Date Title
CN103025740B (zh) 蛋白酪氨酸激酶活性的抑制剂及其治疗眼科疾病的用途
CN102015723B (zh) 蛋白酪氨酸激酶活性的抑制剂
TWI571468B (zh) 蛋白質酪胺酸激酶活性抑制劑
AU2011241420A1 (en) Inhibitors of protein tyrosine kinase activity and use thereof to treat ophthalmic disorders
JP6944442B2 (ja) 疾患を治療するためのｍｃｔ４阻害剤
KR20160118368A (ko) 보체 매개된 장애의 치료를 위한 에터 화합물
JP2008523072A (ja) タンパク質キナーゼの阻害剤
CN112292374B (zh) 一种新型磷酸肌醇3-激酶抑制剂及其制备方法和用途
EA008501B1 (ru) 2-(1н-индазол-6-иламино)бензамидные соединения как ингибиторы протеинкиназ, полезные для лечения офтальмологических заболеваний
WO2019034153A1 (zh) 一种化合物，其药物组合物及其用途及应用
TW201329085A (zh) 蛋白酪氨酸激酶活性抑制劑
TW201718548A (zh) 哌嗪（ｐｉｐｅｒａｚｉｎｅ）衍生物
TW201329086A (zh) 蛋白酪氨酸激酶活性抑制劑
TW201329084A (zh) 蛋白酪氨酸激酶活性選擇的抑制劑
AU2021362678A1 (en) SUBSTITUTED 4-([1,2,4]TRIAZOLO[1,5-a]PYRIDIN-6-YL)THIOPHENE-2-CARBOXAMIDE DERIVATIVES AND USE THEREOF
HK1182379A (en) Inhibitors of protein tyrosine kinase activity

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20150701

Termination date: 20160408

CF01 Termination of patent right due to non-payment of annual fee