JP2013516479A - 標的薬物を開発する方法および組成物 - Google Patents

標的薬物を開発する方法および組成物 Download PDF

Info

Publication number
JP2013516479A
JP2013516479A JP2012548125A JP2012548125A JP2013516479A JP 2013516479 A JP2013516479 A JP 2013516479A JP 2012548125 A JP2012548125 A JP 2012548125A JP 2012548125 A JP2012548125 A JP 2012548125A JP 2013516479 A JP2013516479 A JP 2013516479A
Authority
JP
Japan
Prior art keywords
unsaturated bond
contain
branched
lower alkyl
group
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.)
Pending
Application number
JP2012548125A
Other languages
English (en)
Japanese (ja)
Other versions
JP2013516479A5 (https=
Inventor
ジョゼフ・ピー・エリコ
ベンジャミン・マグレージ
イグナティウス・ターチ
マシュー・シルス
ジェーン・オング
ジョン・アロッコ
パム・ワインズ
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.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of JP2013516479A publication Critical patent/JP2013516479A/ja
Publication of JP2013516479A5 publication Critical patent/JP2013516479A5/ja
Pending legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20Oxygen atoms
    • C07D215/24Oxygen atoms attached in position 8
    • C07D215/26Alcohols; Ethers thereof
    • 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
    • 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
    • A61K31/4709Non-condensed quinolines 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/08Antiseborrheics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/12Keratolytics, e.g. wart or anti-corn preparations
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C335/00Thioureas, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C335/04Derivatives of thiourea
    • C07C335/24Derivatives of thiourea containing any of the groups, X being a hetero atom, Y being any atom
    • C07C335/26Y being a hydrogen or a carbon atom, e.g. benzoylthioureas
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/46Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
    • C07D207/48Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/08Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/121,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/1251,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C07D285/135Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/22Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/54Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • GPHYSICS
    • G16INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16BBIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B15/00ICT specially adapted for analysing two-dimensional [2D] or three-dimensional [3D] molecular structures, e.g. structural or functional relations or structure alignment
    • GPHYSICS
    • G16INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16BBIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B15/00ICT specially adapted for analysing two-dimensional [2D] or three-dimensional [3D] molecular structures, e.g. structural or functional relations or structure alignment
    • G16B15/30Drug targeting using structural data; Docking or binding prediction

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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Spectroscopy & Molecular Physics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Physics & Mathematics (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Evolutionary Biology (AREA)
  • Theoretical Computer Science (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Computational Biology (AREA)
  • Biotechnology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Medical Informatics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Peptides Or Proteins (AREA)
JP2012548125A 2010-01-06 2011-01-06 標的薬物を開発する方法および組成物 Pending JP2013516479A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US29277610P 2010-01-06 2010-01-06
US61/292,776 2010-01-06
PCT/US2011/020414 WO2011085126A2 (en) 2010-01-06 2011-01-06 Methods and compositions of targeted drug development

Publications (2)

Publication Number Publication Date
JP2013516479A true JP2013516479A (ja) 2013-05-13
JP2013516479A5 JP2013516479A5 (https=) 2014-11-06

Family

ID=44306150

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2012548125A Pending JP2013516479A (ja) 2010-01-06 2011-01-06 標的薬物を開発する方法および組成物

Country Status (10)

Country Link
US (4) US8618302B2 (https=)
EP (2) EP2521551A4 (https=)
JP (1) JP2013516479A (https=)
KR (1) KR20130027080A (https=)
CN (1) CN102811723A (https=)
AU (1) AU2011204368B2 (https=)
CA (2) CA2786289A1 (https=)
MX (1) MX2012007872A (https=)
SG (1) SG182343A1 (https=)
WO (2) WO2011085129A2 (https=)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8658170B2 (en) 2010-01-06 2014-02-25 Joseph P. Errico Combination therapy with MDM2 and EFGR inhibitors
AU2011204368B2 (en) * 2010-01-06 2014-11-27 Joseph P. Errico Methods and compositions of targeted drug development
EP2536709A4 (en) * 2010-02-17 2013-11-27 Univ Cornell PROLYL HYDROXYLASE HEMMER AND USE METHOD THEREFOR
HUP1000243A2 (en) * 2010-05-06 2012-01-30 Avidin Kft 8-hidroxy-quinoline derivatives
AU2011255627A1 (en) * 2010-05-18 2012-12-06 Eastern Virginia Medical School Inhibitors of human 12-lipoxygenase
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
EP2596366A4 (en) * 2010-07-21 2014-04-16 Joseph P Errico COMBINATION THERAPY WITH MDM2 AND EFGR INHIBITORS
EP2716292B1 (en) * 2011-05-23 2017-09-06 ONCO Biomedical Technology (Suzhou) Co., Ltd Cdc42 inhibitor and uses thereof
US8710043B2 (en) 2011-06-24 2014-04-29 Amgen Inc. TRPM8 antagonists and their use in treatments
EP2723718A1 (en) 2011-06-24 2014-04-30 Amgen Inc. Trpm8 antagonists and their use in treatments
CN102503945A (zh) * 2011-11-28 2012-06-20 华东理工大学 能够抑制表皮生长因子受体的化合物及其应用
CA2873902A1 (en) * 2012-05-18 2013-11-21 Georgetown University Methods and systems for populating and searching a drug informatics database
US20150150869A1 (en) * 2012-06-20 2015-06-04 Eutropics Pharmaceuticals, Inc. Methods and compositions useful for treating diseases involving bcl-2 family proteins with quinoline derivatives
US8952009B2 (en) 2012-08-06 2015-02-10 Amgen Inc. Chroman derivatives as TRPM8 inhibitors
EP2922544B1 (en) 2012-11-21 2018-08-01 Eutropics Pharmaceuticals, Inc. Methods and compositions useful for treating diseases involving bcl-2 family proteins with quinoline derivatives
CA2912313A1 (en) 2013-05-14 2014-11-20 Active Biotech Ab N-(heteroaryl)-sulfonamide derivatives useful as s100-inhibitors
WO2015017788A1 (en) 2013-08-01 2015-02-05 Eutropics Pharmaceuticals, Inc. Method for predicting cancer sensitivity
KR20160128288A (ko) * 2013-10-07 2016-11-07 리서치 파운데이션 오브 더 시티 유니버시티 오브 뉴욕 수계 약리작용단을 이용하는 방법
WO2015066305A1 (en) 2013-10-30 2015-05-07 Eutropics Pharmaceuticals, Inc. Methods for determining chemosensitivity and chemotoxicity
CN104016908B (zh) * 2014-04-03 2016-04-20 定陶县友帮化工有限公司 一种2-氨基-3,5-二氯吡啶的合成方法
CN104402831B (zh) * 2014-10-24 2016-08-17 郑州大学 含酰脲结构单元的-5-氰基嘧啶衍生物及其制备方法和用途
CN104744439A (zh) * 2015-02-10 2015-07-01 南开大学 8-羟基喹啉类ntr1小分子拮抗剂及应用
HUP1500098A2 (hu) * 2015-03-09 2016-09-28 Avidin Kft 8-hidroxikinolin származékok új enantiomerjei és szintézisük
WO2017066245A1 (en) * 2015-10-12 2017-04-20 Health Research, Inc. Methods for inducing apoptosis in cancer cells
EP3388419A1 (en) * 2017-04-12 2018-10-17 Leadiant Biosciences SA Gli1 inhibitors and uses thereof
WO2019043635A1 (en) 2017-09-01 2019-03-07 Richter Gedeon Nyrt. COMPOUNDS INHIBITING THE ACTIVITY OF D-AMINO ACID OXIDASE
CN113226323B (zh) * 2018-11-15 2024-12-31 法国古士塔柏罗斯学院 马德辛衍生化合物、组合物及其用于治疗癌症的用途
TW202218665A (zh) 2020-09-21 2022-05-16 德國阿爾伯特路德維希弗萊堡大學 用於治療或預防造血細胞移植後血液科贅瘤(neoplasm)復發之mdm2抑制劑
CN112250637A (zh) * 2020-10-30 2021-01-22 中山大学 虚拟筛选的化合物在制备抗肿瘤药物中的应用及其药物
CN114195691B (zh) * 2021-12-16 2023-10-20 贵州大学 一种含酰胺的阿魏酸衍生物及其制备方法和应用
WO2024073624A2 (en) * 2022-09-28 2024-04-04 The Research Foundation For The State University Of New York Antiproliferative betti bases and prodrugs thereof
CN115572266B (zh) * 2022-10-24 2023-10-03 南方医科大学 一种蛋白抑制剂、一种试剂组及其应用
CN120463779B (zh) * 2025-07-10 2025-09-19 南京农业大学三亚研究院 真菌效应子药靶Nep1及基于该药靶的高通量药物分子筛选和应用

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008116092A1 (en) * 2007-03-20 2008-09-25 Brandeis University Compositions and methods for the diagnosis, treatment, and prevention of amyotrophic lateral sclerosis and related neurological diseases
US20080269213A1 (en) * 2006-08-23 2008-10-30 Wyeth 8-Hydroxyquinoline compounds and methods thereof
WO2009051801A2 (en) * 2007-10-16 2009-04-23 Angiogenex Chemical inhibitors of inhibitors of differentiation
WO2009117484A2 (en) * 2008-03-18 2009-09-24 University Of South Florida Small molecule e2f inhibitor
WO2009137597A1 (en) * 2008-05-06 2009-11-12 The Trustees Of Columbia University In The City Of New York COMPOUNDS THAT INHIBIT PRODUCTION OF sAPPβ AND Aβ AND USES THEREOF
WO2009151972A1 (en) * 2008-05-28 2009-12-17 , The United States Of America, As Represented By The Secretary Of The Army, On Behalf Of U.S. Army Medical Research And Materiel Command Small molecule inhibitors of botulinum neurotoxins
JP2009544631A (ja) * 2006-07-25 2009-12-17 エンビボ ファーマシューティカルズ インコーポレイテッド キノリン誘導体
WO2011020886A1 (de) * 2009-08-20 2011-02-24 Vifor (International) Ag Neue chinolin-hepcidin-antagonisten

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3641474A (en) 1970-05-11 1972-02-08 Rca Corp Semiconductor mounting structure
US6664288B1 (en) 1999-04-14 2003-12-16 Dana Farber Cancer Institute, Inc. Method and composition for the treatment of cancer
US6465448B1 (en) 1999-08-13 2002-10-15 Case Western Reserve University Methoxyamine potentiation of temozolomide anti-cancer activity
US6931325B2 (en) 2001-02-07 2005-08-16 Regents Of The University Of Michigan Three dimensional protein mapping
EP1479693A4 (en) 2002-02-05 2005-07-27 Japan Science & Tech Agency EGF / EGFR COMPLEX
US6916455B2 (en) 2002-08-14 2005-07-12 The Regents Of The University Of California Protein crystallography prescreen kit
US20080305041A1 (en) 2004-11-19 2008-12-11 Bioquanta Corp. Pf4 Pharmacophores and Their Uses
CN102206216B (zh) * 2005-06-22 2014-11-12 普莱希科公司 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物
US7754724B2 (en) * 2005-06-30 2010-07-13 Dow Agrosciences Llc N-substituted piperazines
EP2606890A1 (en) 2006-04-05 2013-06-26 Novartis AG Combinations comprising BCR-ABL/C-KIT/PDGF-R TK inhibitors for treating cancer
WO2007139946A2 (en) 2006-05-25 2007-12-06 University Of Tennessee Research Foundation Gpcr ligands identified by computational modeling
US8183236B2 (en) * 2007-04-12 2012-05-22 University Of Southern California Compounds with HIV-1 integrase inhibitory activity and use thereof as anti-HIV/AIDS therapeutics
US8119656B2 (en) * 2007-12-07 2012-02-21 The Board Of Regents Of The University Of Texas System Inhibitors of the influenza virus non-structural 1 protein
CA2709784A1 (en) * 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
US8563580B2 (en) * 2008-09-23 2013-10-22 Georgetown University Flavivirus inhibitors and methods for their use
AU2011204368B2 (en) * 2010-01-06 2014-11-27 Joseph P. Errico Methods and compositions of targeted drug development

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009544631A (ja) * 2006-07-25 2009-12-17 エンビボ ファーマシューティカルズ インコーポレイテッド キノリン誘導体
US20080269213A1 (en) * 2006-08-23 2008-10-30 Wyeth 8-Hydroxyquinoline compounds and methods thereof
WO2008116092A1 (en) * 2007-03-20 2008-09-25 Brandeis University Compositions and methods for the diagnosis, treatment, and prevention of amyotrophic lateral sclerosis and related neurological diseases
WO2009051801A2 (en) * 2007-10-16 2009-04-23 Angiogenex Chemical inhibitors of inhibitors of differentiation
WO2009117484A2 (en) * 2008-03-18 2009-09-24 University Of South Florida Small molecule e2f inhibitor
WO2009137597A1 (en) * 2008-05-06 2009-11-12 The Trustees Of Columbia University In The City Of New York COMPOUNDS THAT INHIBIT PRODUCTION OF sAPPβ AND Aβ AND USES THEREOF
WO2009151972A1 (en) * 2008-05-28 2009-12-17 , The United States Of America, As Represented By The Secretary Of The Army, On Behalf Of U.S. Army Medical Research And Materiel Command Small molecule inhibitors of botulinum neurotoxins
WO2011020886A1 (de) * 2009-08-20 2011-02-24 Vifor (International) Ag Neue chinolin-hepcidin-antagonisten

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
JPN5012015632; ROXAS-DUNCAN, VIRGINIA: 'IDENTIFICATION AND BIOCHEMICAL CHARACTERIZATION OF SMALL-MOLECULE INHIBITORS 以下備考' ANTIMICROBIAL AGENTS AND CHEMOTHERAPY V53 N8, 20090615, P3478-3486 *
JPN5013002563; TOMLINSON: 'A CHEMICAL GENOMIC APPROACH IDENTIFIES MATRIX METALLOPROTEINASES AS PLAYING AN ESSENTIAL 以下備考' CHEMISTRY & BIOLOGY V16, 20090130, P93-104 *
JPN6014052603; Galam, Lakshmi et al.: 'High-throughput assay for the identification of Hsp90 inhibitors based on Hsp90-dependent refolding' Bioorganic & Medicinal Chemistry 15(5), 2007, p. 1939-1946 *
JPN6014052604; Moy, Terence I. et al.: 'High-Throughput Screen for Novel Antimicrobials using a Whole Animal Infection Model' ACS Chemical Biology 4(7), 2009, p. 527-533及びSupporting Infomation *
JPN6014052605; Cournia, Zoe et al.: 'Discovery of Human Macrophage Migration Inhibitory Factor (MIF)-CD74 Antagonists via Virtual Screeni' Journal of Medicinal Chemistry 52(2), 2009, p. 416-424 *
JPN7014003556; Sergiev, I. et al.: 'Plant growth regulating activity of some novel N-(6-methylpyrid-2-yl)-alpha-(8-hydroxy-quinolin-7-yl)-s' Dokladi na Bulgarskata Akademiya na Naukite 51(5-6), 1998, p. 67-70 *

Also Published As

Publication number Publication date
US20140163069A1 (en) 2014-06-12
EP2521551A2 (en) 2012-11-14
AU2011204368A1 (en) 2012-07-19
EP2521553A4 (en) 2013-08-28
US9073858B2 (en) 2015-07-07
EP2521551A4 (en) 2013-08-21
EP2521553A2 (en) 2012-11-14
WO2011085126A2 (en) 2011-07-14
KR20130027080A (ko) 2013-03-14
US20140179681A1 (en) 2014-06-26
US8618302B2 (en) 2013-12-31
WO2011085129A3 (en) 2011-09-01
US20140194439A1 (en) 2014-07-10
SG182343A1 (en) 2012-08-30
US20110301193A1 (en) 2011-12-08
MX2012007872A (es) 2012-10-03
CN102811723A (zh) 2012-12-05
CA2786277A1 (en) 2011-07-14
CA2786289A1 (en) 2011-07-14
WO2011085126A3 (en) 2012-02-23
AU2011204368B2 (en) 2014-11-27
WO2011085129A2 (en) 2011-07-14

Similar Documents

Publication Publication Date Title
US9073858B2 (en) Methods of targeted drug development
Tan et al. Development of dual inhibitors targeting epidermal growth factor receptor in cancer therapy
Xu et al. Chemical probes that competitively and selectively inhibit Stat3 activation
Zhang et al. Discovery of novel potent VEGFR-2 inhibitors exerting significant antiproliferative activity against cancer cell lines
JP7191828B2 (ja) がん治療のための組成物および方法
Eissa et al. New theobromine derivative as apoptotic anti-triple-negative breast cancer targeting EGFR protein: CADD story
Nawaz et al. 3′‐(4‐(Benzyloxy) phenyl)‐1′‐phenyl‐5‐(heteroaryl/aryl)‐3, 4‐dihydro‐1′ H, 2H‐[3, 4′‐bipyrazole]‐2‐carboxamides as EGFR kinase inhibitors: Synthesis, anticancer evaluation, and molecular docking studies
KR20230028371A (ko) 돌연변이 p53 재활성화 화합물에 대한 동반 진단 도구
US20120156197A1 (en) Combination therapy with mdm2 and efgr inhibitors
CA2726987A1 (en) Stat3 inhibitors
BR112021014977A2 (pt) Derivados de acetamido como inibidores de dna polimerase teta
JP2019508496A (ja) 癌の治療法のためのtaf1阻害剤
CN101801401A (zh) 激酶蛋白质结合抑制剂
Bhanushali et al. Design, Synthesis and Evaluation of 5-pyridin-4-yl-2-thioxo-[1, 3, 4] oxadiazol-3-yl Derivatives as Anti-angiogenic Agents Targeting VEGFR-2
Wu et al. Discovery of a promising CBP/p300 degrader XYD129 for the treatment of acute myeloid leukemia
Ali et al. Direct synthesis of diamides from dicarboxylic acids with amines using Nb2O5 as a Lewis acid catalyst and molecular docking studies as anticancer agents
Radwan et al. Synthesis, and docking studies of some fused-quinazolines and quinazolines carrying biological active isatin moiety as cell-cycle inhibitors of breast cancer cell lines
Eni et al. Design, synthesis, and biochemical and computational screening of novel oxindole derivatives as inhibitors of Aurora A kinase and SARS-CoV-2 spike/host ACE2 interaction
Marlhoux et al. Discovery of KDX1381, a bivalent CK2α inhibitor for the treatment of solid tumors as a single agent or in combination
EP2596366A1 (en) Combination therapy with mdm2 and efgr inhibitors
El-Hema et al. Design and Multi-Level Biological Evaluation of Naphthyridine-Based Derivatives as Topoisomerase I/II-Targeted Anticancer Agents with Anti-Fowlpox Virus Activity Supported by In Silico Analysis
Vyas et al. Unlocking potential topoisomerase-II inhibitors: ligand-based drug design pipeline integrating pharmacophore mapping, virtual screening, molecular docking, and ADMET profiling
Hamdy et al. Design, synthesis, and cytotoxicity evaluation of novel griseofulvin analogues with improved water solubility
AU2015200632A1 (en) Methods and compositions of targeted drug development
Kuthe et al. Cytotoxic Potential of Newly Synthesized Quinoline–Bearing Dihydropyridine Hybrids on A549 Lung Cancer Cells

Legal Events

Date Code Title Description
A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20131226

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140912

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20141211

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20141215

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20141216

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20150311

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20150415

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20150515

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150615

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20160105