EA201071089A1 - Производные хиназолина как модуляторы raf-киназы и способы их применения - Google Patents

Производные хиназолина как модуляторы raf-киназы и способы их применения

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Publication number
EA201071089A1
EA201071089A1 EA201071089A EA201071089A EA201071089A1 EA 201071089 A1 EA201071089 A1 EA 201071089A1 EA 201071089 A EA201071089 A EA 201071089A EA 201071089 A EA201071089 A EA 201071089A EA 201071089 A1 EA201071089 A1 EA 201071089A1
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EA
Eurasian Patent Office
Prior art keywords
methods
raf
hinazolin
derivatives
application
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EA201071089A
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English (en)
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EA019350B1 (ru
Inventor
Санни Абрахам
Шрипад С. Бхагват
Брайан Т. Кэмпбелл
Ци Чао
Раффаэлла Фараони
Марк У. Холладэй
Эндилий Г. Лай
Мартин У. Роуботтом
Эдуардо Сетти
Келли Г. Спрэнкл
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Эмбит Байосайенсиз Корпорейшн
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Publication of EA201071089A1 publication Critical patent/EA201071089A1/ru
Publication of EA019350B1 publication Critical patent/EA019350B1/ru

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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88Oxygen atoms
    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/93Sulfur atoms
    • CCHEMISTRY; METALLURGY
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    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
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    • C07D261/10Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/14Nitrogen atoms
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    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

Обеспечиваются соединения, композиции и способы для модулирования активности RAF-киназ, включая BRAF-киназу, и для лечения, предупреждения или уменьшения одного или большего числа симптомов болезней или нарушений, опосредованных RAF-киназами.
EA201071089A 2008-03-17 2009-03-17 Производные хиназолина как модуляторы raf-киназы и способы их применения EA019350B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US6976308P 2008-03-17 2008-03-17
US11050808P 2008-10-31 2008-10-31
PCT/US2009/001659 WO2009117080A1 (en) 2008-03-17 2009-03-17 Quinazoline derivatives as raf kinase modulators and methods of use thereof

Publications (2)

Publication Number Publication Date
EA201071089A1 true EA201071089A1 (ru) 2011-04-29
EA019350B1 EA019350B1 (ru) 2014-03-31

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US (5) US8618289B2 (ru)
EP (3) EP2947072B1 (ru)
JP (1) JP5542793B2 (ru)
KR (2) KR101601997B1 (ru)
CN (2) CN106146484A (ru)
AU (1) AU2009226136B2 (ru)
BR (1) BRPI0906186A2 (ru)
CA (2) CA2718123C (ru)
DK (2) DK2947072T3 (ru)
EA (1) EA019350B1 (ru)
ES (2) ES2547406T3 (ru)
HK (2) HK1151525A1 (ru)
HU (2) HUE032873T2 (ru)
IL (1) IL207793A (ru)
MX (1) MX2010010172A (ru)
MY (1) MY161576A (ru)
NZ (1) NZ587907A (ru)
PL (2) PL2268623T3 (ru)
PT (2) PT2268623E (ru)
SG (2) SG10201608813PA (ru)
SI (2) SI2947072T1 (ru)
WO (1) WO2009117080A1 (ru)
ZA (1) ZA201006524B (ru)

Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2716952A1 (en) * 2008-02-29 2009-09-11 Array Biopharma Inc. Pyrazole [3,4-b] pyridine raf inhibitors
ES2392482T3 (es) * 2008-02-29 2012-12-11 Array Biopharma, Inc. Derivados de imidazo[4,5-b] piridina usados como inhibidores de RAF
WO2009111280A1 (en) * 2008-02-29 2009-09-11 Array Biopharma Inc. N- (6-aminopyridin-3-yl) -3- (sulfonamido) benzamide derivatives as b-raf inhibitors for the treatment of cancer
TW200940540A (en) * 2008-02-29 2009-10-01 Array Biopharma Inc RAF inhibitor compounds and methods of use thereof
PL2268623T3 (pl) 2008-03-17 2015-10-30 Ambit Biosciences Corp Pochodne chinazoliny jako modulatory kinazy RAF oraz sposoby ich zastosowania
WO2010094695A1 (en) * 2009-02-17 2010-08-26 Boehringer Ingelheim International Gmbh Pyrimido [5,4-d] pyrimidine derivatives for the inhibition of tyrosine kinases
GB0905955D0 (en) 2009-04-06 2009-05-20 Respivert Ltd Novel compounds
WO2011056939A1 (en) * 2009-11-05 2011-05-12 Ambit Biosciences Corp. Process for the preparation of imidazo[2,1-b][1,3]benzothiazole derivatives
US9024041B2 (en) 2010-04-08 2015-05-05 Respivert Ltd. P38 MAP kinase inhibitors
WO2011158044A2 (en) 2010-06-17 2011-12-22 Respivert Limited Respiratory formulations and compounds for use therein
PL2712358T3 (pl) 2011-05-13 2017-05-31 Array Biopharma, Inc. Związki mocznika pirolidynowego, tiomocznika pirolidynowego oraz guanidyny pirolidynowej jako inhibitory kinazy trka
WO2013032951A1 (en) 2011-08-26 2013-03-07 Neupharma, Inc. Certain chemical entities, compositions, and methods
CN115403531A (zh) 2011-09-14 2022-11-29 润新生物公司 作为激酶抑制剂的化学实体、组合物及方法
EP2763984B1 (en) 2011-10-03 2016-04-20 Respivert Limited 1-pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 map kinase inhibitors
EP2578582A1 (en) 2011-10-03 2013-04-10 Respivert Limited 1-Pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 MAP kinase inhibitors
AR088872A1 (es) 2011-11-14 2014-07-16 Cephalon Inc Derivados de uracilo como inhibidores de la quinasa axl y c-met
WO2013112950A2 (en) 2012-01-25 2013-08-01 Neupharma, Inc. Certain chemical entities, compositions, and methods
EP2626073A1 (en) * 2012-02-13 2013-08-14 Harmonic Pharma Compound for use in the prevention and/or treatment of a neurogenerative disease or a disease involving an activation of phosphodiesterase-4 (PDE4)
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
AU2013307688A1 (en) * 2012-08-29 2015-04-09 Merck Patent Gmbh Ddr2 inhibitors for the treatment of osteoarthritis
CN104812389B (zh) 2012-09-24 2020-07-17 润新生物公司 某些化学实体、组合物及方法
CN103102315B (zh) * 2012-11-01 2016-01-20 云南大学 一种喹唑啉类芳基脲及其制备方法和用途
WO2014075077A1 (en) 2012-11-12 2014-05-15 Neupharma, Inc. Certain chemical entities, compositions, and methods
WO2014076484A1 (en) 2012-11-16 2014-05-22 Respivert Limited Kinase inhibitors
WO2014127214A1 (en) * 2013-02-15 2014-08-21 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
WO2014127335A1 (en) * 2013-02-15 2014-08-21 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
TW201512192A (zh) * 2013-03-11 2015-04-01 Cephalon Inc 喹唑啉衍生物之固態形式及其作爲braf抑制劑之用途
EP2970190A1 (en) 2013-03-14 2016-01-20 Respivert Limited Kinase inhibitors
WO2014162121A1 (en) * 2013-04-02 2014-10-09 Topivert Pharma Limited Kinase inhibitors based upon n-alkyl pyrazoles
CN103159685A (zh) * 2013-04-11 2013-06-19 苏州立新制药有限公司 4-氯-6,7-二(2-甲氧基乙氧基)喹唑啉的制备方法
EP3071204B1 (en) * 2013-11-20 2019-02-20 SignalChem Lifesciences Corp. Quinazoline derivatives as tam family kinase inhibitors
TWI664967B (zh) 2014-02-14 2019-07-11 英商瑞斯比維特有限公司 新穎化合物(一)
CA2946538A1 (en) 2014-04-04 2015-10-08 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
WO2015171833A1 (en) * 2014-05-06 2015-11-12 The Regents Of The University Of California Wound healing using braf inhibitors
CN104892530A (zh) * 2015-05-27 2015-09-09 烟台大学 一种含喹唑啉结构的二芳基脲类化合物及其制备方法和应用
CN104892529A (zh) * 2015-05-27 2015-09-09 烟台大学 一种含喹唑啉结构的硫脲类化合物及其制备方法和应用
AU2016291676B2 (en) * 2015-07-16 2020-04-30 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as RET kinase inhibitors
KR20180086187A (ko) 2015-10-05 2018-07-30 더 트러스티이스 오브 콜롬비아 유니버시티 인 더 시티 오브 뉴욕 자가포식 유동의 활성체 및 포스포리파제 d 및 타우를 포함하는 단백질 응집물의 클리어런스 및 단백질질환의 치료
US10799503B2 (en) 2016-12-01 2020-10-13 Ignyta, Inc. Methods for the treatment of cancer
US11168090B2 (en) 2017-01-18 2021-11-09 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors
CN108530455B (zh) * 2017-03-01 2021-01-12 北京赛特明强医药科技有限公司 脲取代的芳环连二噁烷并喹唑啉类化合物或药用盐或水合物及作为酪氨酸激酶抑制剂的应用
CN106928069B (zh) * 2017-03-21 2019-03-19 上海玉函化工有限公司 一种4,5-二(2-甲氧基乙氧基)-2-硝基苯甲酸乙酯的制备方法
US11124509B2 (en) * 2017-03-23 2021-09-21 Clavius Pharmaceuticals, LLC. Tri-substituted imidazoles for the inhibition of TGF beta and methods of treatment
CN107501283B (zh) * 2017-09-13 2020-06-02 北京师范大学 取代芳甲杂基取代苯胺基缩乙二醇醚环代喹唑啉的制备及肿瘤治疗药物应用
CN109721552B (zh) * 2017-10-30 2022-09-20 上海北卡医药技术有限公司 一种吉非替尼的制备方法
CN109721551B (zh) * 2017-10-30 2022-09-20 上海北卡医药技术有限公司 一种3,4-二氢-7-甲氧基-4-氧代喹唑啉-6-醇乙酸酯的制备方法
CN111630054B (zh) 2018-01-18 2023-05-09 奥瑞生物药品公司 作为RET激酶抑制剂的取代的吡唑并[3,4-d]嘧啶化合物
CA3087972C (en) 2018-01-18 2023-01-10 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
US11603374B2 (en) 2018-01-18 2023-03-14 Array Biopharma Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
EP3750894B1 (en) 2018-02-11 2024-04-03 Beijing Scitech-MQ Pharmaceuticals Limited Urea-substituted aromatic ring-linked dioxazoline compound, preparation method therefor, and uses thereof
CN108358798A (zh) * 2018-02-12 2018-08-03 黑龙江鑫创生物科技开发有限公司 一种微通道反应器合成厄洛替尼中间体的方法
WO2019241787A1 (en) * 2018-06-15 2019-12-19 The Regents Of The University Of Colorado A Body Corporate Novel cyclic gmp-amp synthase (cgas) inhibitors and their method of use
CN110862398B (zh) * 2018-08-27 2021-04-06 北京赛特明强医药科技有限公司 脲取代的芳环连二噁烷并喹唑啉或喹啉类化合物、组合物及其应用
JP2022500385A (ja) 2018-09-10 2022-01-04 ミラティ セラピューティクス, インコーポレイテッド 組み合わせ療法
CN109553581B (zh) * 2018-09-25 2022-01-25 广州六顺生物科技股份有限公司 取代脲化合物、其药学上可接受的盐或其溶剂合物、其应用、药物及药物组合物
TW202043225A (zh) * 2019-01-25 2020-12-01 英屬開曼群島商百濟神州有限公司 B-raf激酶二聚體抑制劑之穩定固體分散體、製備方法及其用途
JP2022519675A (ja) * 2019-02-12 2022-03-24 ルトリス ファーマ エル ティー ディー. 放射線皮膚炎の治療のための局所用braf阻害剤組成物の使用
PE20221027A1 (es) * 2019-12-10 2022-06-16 Hoffmann La Roche Nuevos inhibidores de braf como rompedores de la paradoja
WO2022159835A1 (en) 2021-01-25 2022-07-28 Halia Therapeutics, Inc. Nek7 inhibitors
CN113254860B (zh) * 2021-06-04 2022-03-22 南京航空航天大学 一种堆芯栅元中子通量的计算方法

Family Cites Families (81)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3536809A (en) 1969-02-17 1970-10-27 Alza Corp Medication method
US3598123A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US3916899A (en) 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
US4008719A (en) 1976-02-02 1977-02-22 Alza Corporation Osmotic system having laminar arrangement for programming delivery of active agent
US4328245A (en) 1981-02-13 1982-05-04 Syntex (U.S.A.) Inc. Carbonate diester solutions of PGE-type compounds
US4410545A (en) 1981-02-13 1983-10-18 Syntex (U.S.A.) Inc. Carbonate diester solutions of PGE-type compounds
US4409239A (en) 1982-01-21 1983-10-11 Syntex (U.S.A.) Inc. Propylene glycol diester solutions of PGE-type compounds
DE3209472C2 (de) 1982-03-16 1984-05-17 Degussa Ag, 6000 Frankfurt Verfahren zur Herstellung von 3-Oxonitrilen sowie neue 3-Oxonitrile
KR890002631B1 (ko) 1984-10-04 1989-07-21 몬산토 캄파니 생물학적으로 활성인 소마토트로핀을 지속적으로 유리하는 조성물
IE58110B1 (en) 1984-10-30 1993-07-14 Elan Corp Plc Controlled release powder and process for its preparation
JPS6296479A (ja) 1985-10-23 1987-05-02 Shionogi & Co Ltd ポリフルオロアルキルイソオキサゾリルアミン類
US5073543A (en) 1988-07-21 1991-12-17 G. D. Searle & Co. Controlled release formulations of trophic factors in ganglioside-lipsome vehicle
US5612059A (en) 1988-08-30 1997-03-18 Pfizer Inc. Use of asymmetric membranes in delivery devices
IT1229203B (it) 1989-03-22 1991-07-25 Bioresearch Spa Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative.
PH30995A (en) 1989-07-07 1997-12-23 Novartis Inc Sustained release formulations of water soluble peptides.
US5120548A (en) 1989-11-07 1992-06-09 Merck & Co., Inc. Swelling modulated polymeric drug delivery device
US5585112A (en) 1989-12-22 1996-12-17 Imarx Pharmaceutical Corp. Method of preparing gas and gaseous precursor-filled microspheres
IT1246382B (it) 1990-04-17 1994-11-18 Eurand Int Metodo per la cessione mirata e controllata di farmaci nell'intestino e particolarmente nel colon
US5733566A (en) 1990-05-15 1998-03-31 Alkermes Controlled Therapeutics Inc. Ii Controlled release of antiparasitic agents in animals
US5543390A (en) 1990-11-01 1996-08-06 State Of Oregon, Acting By And Through The Oregon State Board Of Higher Education, Acting For And On Behalf Of The Oregon Health Sciences University Covalent microparticle-drug conjugates for biological targeting
US5580578A (en) 1992-01-27 1996-12-03 Euro-Celtique, S.A. Controlled release formulations coated with aqueous dispersions of acrylic polymers
TW333456B (en) 1992-12-07 1998-06-11 Takeda Pharm Ind Co Ltd A pharmaceutical composition of sustained-release preparation the invention relates to a pharmaceutical composition of sustained-release preparation which comprises a physiologically active peptide.
US5591767A (en) 1993-01-25 1997-01-07 Pharmetrix Corporation Liquid reservoir transdermal patch for the administration of ketorolac
US6274552B1 (en) 1993-03-18 2001-08-14 Cytimmune Sciences, Inc. Composition and method for delivery of biologically-active factors
US5985307A (en) 1993-04-14 1999-11-16 Emory University Device and method for non-occlusive localized drug delivery
US5523092A (en) 1993-04-14 1996-06-04 Emory University Device for local drug delivery and methods for using the same
US6087324A (en) 1993-06-24 2000-07-11 Takeda Chemical Industries, Ltd. Sustained-release preparation
US6004534A (en) 1993-07-23 1999-12-21 Massachusetts Institute Of Technology Targeted polymerized liposomes for improved drug delivery
IT1270594B (it) 1994-07-07 1997-05-07 Recordati Chem Pharm Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida
US5759542A (en) 1994-08-05 1998-06-02 New England Deaconess Hospital Corporation Compositions and methods for the delivery of drugs by platelets for the treatment of cardiovascular and other diseases
US5660854A (en) 1994-11-28 1997-08-26 Haynes; Duncan H Drug releasing surgical implant or dressing material
US6316652B1 (en) 1995-06-06 2001-11-13 Kosta Steliou Drug mitochondrial targeting agents
US5798119A (en) 1995-06-13 1998-08-25 S. C. Johnson & Son, Inc. Osmotic-delivery devices having vapor-permeable coatings
DE69632684T2 (de) 1995-06-27 2005-06-09 Takeda Pharmaceutical Co. Ltd. Verfahren zur herstellung von zubereitungen mit verzögerter freisetzung
TW448055B (en) 1995-09-04 2001-08-01 Takeda Chemical Industries Ltd Method of production of sustained-release preparation
JP2909418B2 (ja) 1995-09-18 1999-06-23 株式会社資生堂 薬物の遅延放出型マイクロスフイア
US6039975A (en) 1995-10-17 2000-03-21 Hoffman-La Roche Inc. Colon targeted delivery system
US6143764A (en) 1995-11-07 2000-11-07 Kirin Beer Kabushiki Kaisha Quinoline and quinazoline derivatives inhibiting platelet-derived growth factor receptor autophosphorylation and pharmaceutical compositions containing the same
US5980945A (en) 1996-01-16 1999-11-09 Societe De Conseils De Recherches Et D'applications Scientifique S.A. Sustained release drug formulations
TW345603B (en) 1996-05-29 1998-11-21 Gmundner Fertigteile Gmbh A noise control device for tracks
US6264970B1 (en) 1996-06-26 2001-07-24 Takeda Chemical Industries, Ltd. Sustained-release preparation
US6419961B1 (en) 1996-08-29 2002-07-16 Takeda Chemical Industries, Ltd. Sustained release microcapsules of a bioactive substance and a biodegradable polymer
IL129242A0 (en) 1996-10-01 2000-02-17 Cima Labs Inc Taste-masked microcapsule compositions and methods of manufacture
CA2217134A1 (en) 1996-10-09 1998-04-09 Sumitomo Pharmaceuticals Co., Ltd. Sustained release formulation
ES2221019T3 (es) 1996-10-31 2004-12-16 Takeda Chemical Industries, Ltd. Preparacion de liberacion mantenida.
US6131570A (en) 1998-06-30 2000-10-17 Aradigm Corporation Temperature controlling device for aerosol drug delivery
KR20000057693A (ko) 1996-12-20 2000-09-25 다케다 야쿠힌 고교 가부시키가이샤 지효성 제제의 제조 방법
US5891474A (en) 1997-01-29 1999-04-06 Poli Industria Chimica, S.P.A. Time-specific controlled release dosage formulations and method of preparing same
US6120751A (en) 1997-03-21 2000-09-19 Imarx Pharmaceutical Corp. Charged lipids and uses for the same
US6060082A (en) 1997-04-18 2000-05-09 Massachusetts Institute Of Technology Polymerized liposomes targeted to M cells and useful for oral or mucosal drug delivery
US20070244120A1 (en) * 2000-08-18 2007-10-18 Jacques Dumas Inhibition of raf kinase using substituted heterocyclic ureas
US6350458B1 (en) 1998-02-10 2002-02-26 Generex Pharmaceuticals Incorporated Mixed micellar drug deliver system and method of preparation
US6613358B2 (en) 1998-03-18 2003-09-02 Theodore W. Randolph Sustained-release composition including amorphous polymer
US6048736A (en) 1998-04-29 2000-04-11 Kosak; Kenneth M. Cyclodextrin polymers for carrying and releasing drugs
KR19990085365A (ko) 1998-05-16 1999-12-06 허영섭 지속적으로 약물 조절방출이 가능한 생분해성 고분자 미립구 및그 제조방법
EP1119567B1 (en) 1998-10-08 2005-05-04 AstraZeneca AB Quinazoline derivatives
DE60033857T2 (de) 1999-01-22 2007-10-25 Kirin Beer K.K. Derivate des N-((Chinolinyl)oxy)-phenyl)-Harnstoffs und des N-((Chinazolinyl)oxy)-phenyl)-Harnstoffs mit Antitumor Aktivität
US6248363B1 (en) 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
US6271359B1 (en) 1999-04-14 2001-08-07 Musc Foundation For Research Development Tissue-specific and pathogen-specific toxic agents and ribozymes
WO2001047890A1 (fr) 1999-12-24 2001-07-05 Kirin Beer Kabushiki Kaisha Quinoline, derives de la quinazoline et medicaments contenant ces substances
BR0113626A (pt) 2000-08-30 2003-06-17 Pfizer Prod Inc Formulações de liberação sustentada para secretores de hormÈnio do crescimento
DE60126997T2 (de) 2000-10-20 2007-10-25 Eisai R&D Management Co., Ltd. Stickstoff-enthaltende aromatische ringverbindungen zur behandlung von tumorerkrankungen
TWI324154B (ru) 2001-04-27 2010-05-01 Kyowa Hakko Kirin Co Ltd
EP2258366B1 (en) 2001-06-22 2013-04-03 Kirin Pharma Kabushiki Kaisha Quinoline derivatives capable of inhibiting autophosphorylation of hepatocyte growth factor receptors, and pharmaceutical composition comprising the same
US7576074B2 (en) 2002-07-15 2009-08-18 Rice Kenneth D Receptor-type kinase modulators and methods of use
EP2392564B1 (en) 2003-09-26 2013-10-23 Exelixis, Inc. c-Met modulators and methods of use
KR20070029110A (ko) 2003-10-16 2007-03-13 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 암의 치료를 위한 raf 키나아제의 저해제로서2,6-디치환 퀴나졸린, 퀴녹살린, 퀴놀린 및 아이소퀴놀린
US20050197371A1 (en) 2003-11-13 2005-09-08 Ambit Biosciences Corporation Urea derivatives as PDGFR modulators
EP1835934A4 (en) 2004-12-23 2010-07-28 Deciphera Pharmaceuticals Llc ENZYME MODULATORS AND TREATMENTS
US7576090B2 (en) 2004-12-27 2009-08-18 4Sc Ag Benzazole analogues and uses thereof
EP1746096A1 (en) 2005-07-15 2007-01-24 4Sc Ag 2-Arylbenzothiazole analogues and uses thereof in the treatment of cancer
JP2009520784A (ja) 2005-12-22 2009-05-28 アストラゼネカ アクチボラグ キナゾリン誘導体、その製造方法および抗癌剤としてのその使用
US7989461B2 (en) 2005-12-23 2011-08-02 Amgen Inc. Substituted quinazolinamine compounds for the treatment of cancer
US20070265258A1 (en) 2006-03-06 2007-11-15 Ruiping Liu Quinazoline derivatives as phosphodiesterase 10 inhibitors
JP2009532450A (ja) 2006-04-05 2009-09-10 アストラゼネカ アクチボラグ 化合物
EP2007736A1 (en) 2006-04-05 2008-12-31 AstraZeneca AB Substituted quinazolines with anti-cancer activity
AU2007269786A1 (en) 2006-06-30 2008-01-10 Discoverx Corporation Detectable nucleic acid tag
RU2478635C2 (ru) 2006-10-19 2013-04-10 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Гетероарильные соединения, содержащие их композиции и способы лечения с применением этих соединений
MX2009004019A (es) 2006-10-19 2009-06-19 Signal Pharm Llc Compuestos heteroarilo, composiciones de los mismos, y uso de los mismos como inhibidores de proteina cinasa.
PL2268623T3 (pl) * 2008-03-17 2015-10-30 Ambit Biosciences Corp Pochodne chinazoliny jako modulatory kinazy RAF oraz sposoby ich zastosowania

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