EA200600928A1 - Фармацевтически приемлемые соли хинолиноновых соединений с улучшенными фармацевтическими свойствами - Google Patents

Фармацевтически приемлемые соли хинолиноновых соединений с улучшенными фармацевтическими свойствами

Info

Publication number
EA200600928A1
EA200600928A1 EA200600928A EA200600928A EA200600928A1 EA 200600928 A1 EA200600928 A1 EA 200600928A1 EA 200600928 A EA200600928 A EA 200600928A EA 200600928 A EA200600928 A EA 200600928A EA 200600928 A1 EA200600928 A1 EA 200600928A1
Authority
EA
Eurasian Patent Office
Prior art keywords
quinolineum
compounds
pharmaceutically acceptable
acceptable salts
pharmaceutical properties
Prior art date
Application number
EA200600928A
Other languages
English (en)
Other versions
EA012621B1 (ru
Inventor
Щаопэй Цай
Джойс Чоу
Эрик Харвуд
Тимоти Д. Мачаевски
Дэвид Рикман
Сяо Шан
Шугуан Чжу
Марк С. Тескони
Аугустус О. Окхамафе
Original Assignee
Чирон Корпорейшн
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 Чирон Корпорейшн filed Critical Чирон Корпорейшн
Publication of EA200600928A1 publication Critical patent/EA200600928A1/ru
Publication of EA012621B1 publication Critical patent/EA012621B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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
    • 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
    • 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
    • A61K31/4375—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 containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41—Preparation of salts of carboxylic acids
    • C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/01—Saturated compounds having only one carboxyl group and containing hydroxy or O-metal groups
    • C07C59/08—Lactic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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

Abstract

Лактатная соль соединения формулы (I) или таутомера соединения, где формула (I) имеет следующую структуру, и значения R-Rи R-Rопределены в настоящем описании.
EA200600928A 2003-11-07 2004-11-05 Фармацевтически приемлемые соли хинолиноновых соединений с улучшенными фармацевтическими свойствами EA012621B1 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US51791503P 2003-11-07 2003-11-07
US52642503P 2003-12-02 2003-12-02
US52642603P 2003-12-02 2003-12-02
US54601704P 2004-02-19 2004-02-19
PCT/US2004/036941 WO2005046589A2 (en) 2003-11-07 2004-11-05 Pharmaceutically acceptable salts of quinolinone compounds having improved pharmaceutical properties

Publications (2)

Publication Number Publication Date
EA200600928A1 true EA200600928A1 (ru) 2007-10-26
EA012621B1 EA012621B1 (ru) 2009-10-30

Family

ID=34596121

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200600928A EA012621B1 (ru) 2003-11-07 2004-11-05 Фармацевтически приемлемые соли хинолиноновых соединений с улучшенными фармацевтическими свойствами

Country Status (15)

Country Link
US (7) US20050209247A1 (ru)
EP (4) EP1682529A4 (ru)
JP (5) JP4890255B2 (ru)
KR (3) KR20060111520A (ru)
CN (1) CN102225926A (ru)
AU (3) AU2004288709B2 (ru)
BR (1) BRPI0416143A (ru)
CA (3) CA2544186A1 (ru)
EA (1) EA012621B1 (ru)
ES (1) ES2486240T3 (ru)
HK (1) HK1097444A1 (ru)
IL (5) IL174471A (ru)
MX (1) MXPA06004194A (ru)
TW (1) TWI347940B (ru)
WO (3) WO2005046590A2 (ru)

Families Citing this family (93)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1313734B1 (en) 2000-09-01 2009-11-11 Novartis Vaccines and Diagnostics, Inc. Aza heterocyclic derivatives and their therapeutic use
US20030028018A1 (en) * 2000-09-11 2003-02-06 Chiron Coporation Quinolinone derivatives
AP1666A (en) * 2000-09-11 2006-09-29 Chiron Corp Quinolinone derivatives as tyrosine kinase inhibitors.
WO2004018419A2 (en) 2002-08-23 2004-03-04 Chiron Corporation Benzimidazole quinolinones and uses thereof
US7825132B2 (en) * 2002-08-23 2010-11-02 Novartis Vaccines And Diagnostics, Inc. Inhibition of FGFR3 and treatment of multiple myeloma
BR0316229A (pt) * 2002-11-13 2005-10-04 Chiron Corp Métodos de tratamento de câncer e métodos relacionados
EP1682529A4 (en) * 2003-11-07 2010-06-30 Novartis Vaccines & Diagnostic METHODS FOR SYNTHESIS OF QUINOLINONE COMPOUNDS
EP1718306A2 (en) * 2004-02-20 2006-11-08 Chiron Corporation Modulation of inflammatory and metastatic processes
WO2006081445A2 (en) * 2005-01-27 2006-08-03 Novartis Vaccines And Diagnostics Inc. Treatment of metastasized tumors
US8034823B2 (en) * 2005-02-22 2011-10-11 Savvipharm Inc Method of increasing drug oral bioavailability and compositions of less toxic orotate salts
EP2527355B1 (en) * 2005-04-25 2019-02-20 Enterin, Inc. Polymorphic and amorphous salt forms of squalamine dilactate
DK1885187T3 (da) 2005-05-13 2013-12-09 Novartis Ag Fremgangsmåde til behandling af lægemiddelresistent cancer
JP5545925B2 (ja) * 2005-05-17 2014-07-09 ノバルティス アーゲー ヘテロ環化合物の合成方法
AU2012258324B2 (en) * 2005-05-17 2014-07-24 Novartis Ag Methods for synthesizing heterocyclic compounds
EP2270000B1 (en) * 2005-05-23 2015-07-29 Novartis AG Crystalline and other forms of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one lactic acid salts
EP1904065A2 (en) * 2005-07-14 2008-04-02 AB Science Use of dual c-kit/fgfr3 inhibitors for treating multiple myeloma
AR062545A1 (es) * 2005-11-29 2008-11-19 Novartis Ag Formulaciones estables de quinolinonas
CN101316593B (zh) * 2005-11-29 2012-05-02 诺瓦提斯公司 喹啉酮类的制剂
EP2546359A1 (en) 2005-12-08 2013-01-16 Novartis AG Effects of inhibitors of FGFR3 on gene transcription
CN100488960C (zh) * 2006-03-09 2009-05-20 中国药科大学 2-位取代的喹诺酮类化合物及其在制药中的应用
WO2008044041A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
JP5528807B2 (ja) 2006-10-12 2014-06-25 アステックス、セラピューティックス、リミテッド 複合薬剤
MX2009009574A (es) * 2007-03-09 2009-09-16 Novartis Ag Tratamiento de melanoma.
JP2010531316A (ja) 2007-06-25 2010-09-24 エフ．ホフマン−ラ ロシュ アーゲー キナーゼ阻害剤としてのベンズイミダゾールアミド誘導体
GB0800855D0 (en) * 2008-01-17 2008-02-27 Syngenta Ltd Herbicidal compounds
WO2009113436A1 (ja) * 2008-03-14 2009-09-17 国立大学法人千葉大学 Ｆｇｆｒ３遺伝子阻害剤の放射線照射併用による放射線の抗癌作用増強法および副作用軽減法
AR070924A1 (es) * 2008-03-19 2010-05-12 Novartis Ag Formas cristalinas y dos formas solvatadas de sales del acido lactico de 4- amino -5- fluoro-3-(5-(4-metilpiperazin-1-il ) -1h- bencimidazol-2-il) quinolin -2-(1h) - ona
US20100168162A1 (en) * 2008-04-25 2010-07-01 The Burnham Institute For Medical Research Selective inhibitors of akt and methods of using same
US20100273808A1 (en) * 2008-11-21 2010-10-28 Millennium Pharmaceticals, Inc. Lactate salt of 4-[6-methoxy-7-(3-piperidin-1-yl-propoxy)quinazolin-4-yl]piperazine-1-carboxylic acid(4-isopropoxyphenyl)-amide and pharmaceutical compositions thereof for the treatment of cancer and other diseases or disorders
WO2010083414A1 (en) 2009-01-16 2010-07-22 Exelixis, Inc. Malate salt of n- (4- { [ 6, 7-bis (methyloxy) quin0lin-4-yl] oxy}phenyl-n' - (4 -fluorophenyl) cyclopropane-1-dicarboxamide, and crystalline forms therof for the treatment of cancer
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
WO2011117380A1 (en) * 2010-03-26 2011-09-29 Novartis Ag Preparation of hydrated polymorphs of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1h-benzimidazol-2-yl]-1h-quinolin-2-one lactic acid salt
JP2013525292A (ja) * 2010-04-16 2013-06-20 ノバルティス アーゲー 有機化合物の組合せ
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
NZ607118A (en) 2010-07-16 2015-05-29 Exelixis Inc C-met modulator pharmaceutical compositions
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
EP4019498A1 (en) 2011-02-10 2022-06-29 Exelixis, Inc. Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds
EP2524915A1 (en) * 2011-05-20 2012-11-21 Sanofi 2-Amino-3-(imidazol-2-yl)-pyridin-4-one derivatives and their use as VEGF receptor kinase inhibitors
WO2013063003A1 (en) 2011-10-28 2013-05-02 Novartis Ag Method of treating gastrointestinal stromal tumors
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) * 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
WO2013088191A1 (en) 2011-12-12 2013-06-20 Institut National De La Sante Et De La Recherche Medicale (Inserm) Antagonist of the fibroblast growth factor receptor 3 (fgfr3) for use in the treatment or the prevention of skeletal disorders linked with abnormal activation of fgfr3
BR112014017985A8 (pt) 2012-01-31 2017-07-11 Novartis Ag Combinação de um inibidor de rtk com um antiestrogênio e uso da mesma para o tratamento de cancer
PL2824181T3 (pl) 2012-03-08 2019-02-28 Astellas Pharma Inc. Nowa fuzja fgfr3
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
BR112015000349A2 (pt) 2012-07-11 2017-06-27 Novartis Ag método de tratamento de tumores estromais gastrointestinais
JP6226981B2 (ja) * 2012-07-17 2017-11-08 サノフイ 肝細胞癌を処置するためのｖｅｇｆｒ−３阻害剤の使用
TWI606066B (zh) * 2012-09-27 2017-11-21 中外製藥股份有限公司 FGFR3 Fusion Gene and Its Targeted Medicine
WO2014058785A1 (en) 2012-10-10 2014-04-17 Novartis Ag Combination therapy
CN103804305A (zh) * 2012-11-05 2014-05-21 韩文毅 一类治疗湿疹的化合物及其用途
EP3007689B1 (en) 2013-01-10 2018-03-07 Pulmokine, Inc. Non-selective kinase inhibitors
BR112015018282B1 (pt) 2013-02-01 2021-08-24 Wellstat Therapeutics Corporation Compostos de amina, composição compreendendo os referidos compostos e usos dos mesmos
WO2014127214A1 (en) 2013-02-15 2014-08-21 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
EP2958895B1 (en) 2013-02-20 2020-08-19 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
US9688688B2 (en) 2013-02-20 2017-06-27 Kala Pharmaceuticals, Inc. Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
ES2959419T3 (es) 2013-10-11 2024-02-26 Pulmokine Inc Formulaciones secas por aspersión
MX363708B (es) 2013-10-14 2019-03-29 Eisai R&D Man Co Ltd Compuestos de quinolina selectivamente sustituidos.
AU2014334554B2 (en) 2013-10-14 2018-12-06 Eisai R&D Management Co., Ltd. Selectively substituted quinoline compounds
CN106061261B (zh) 2013-11-01 2018-04-24 卡拉制药公司 治疗化合物的结晶形式及其用途
US9890173B2 (en) 2013-11-01 2018-02-13 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
TWI541022B (zh) * 2013-12-18 2016-07-11 應克隆公司 針對纖維母細胞生長因子受體－３（ｆｇｆｒ３）之化合物及治療方法
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
LT3122358T (lt) 2014-03-26 2021-04-12 Astex Therapeutics Ltd. Egfr ir cmet inhibitorių deriniai, skirti vėžio gydymui
HUE053653T2 (hu) 2014-03-26 2021-07-28 Astex Therapeutics Ltd FGFR inhibitor és IGF1R inhibitor kombinációi
EP2977374A1 (en) * 2014-07-21 2016-01-27 Université de Strasbourg Molecules presenting dual emission properties
US10752640B2 (en) 2014-08-01 2020-08-25 Nuevolution A/S Compounds active towards bromodomains
JOP20200201A1 (ar) 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
EP3265462A1 (en) 2015-03-03 2018-01-10 INSERM - Institut National de la Santé et de la Recherche Médicale Fgfr3 antagonists
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
GB201506658D0 (en) 2015-04-20 2015-06-03 Cellcentric Ltd Pharmaceutical compounds
GB201506660D0 (en) 2015-04-20 2015-06-03 Cellcentric Ltd Pharmaceutical compounds
HRP20220012T1 (hr) 2015-09-23 2022-04-01 Janssen Pharmaceutica Nv Bi-heteroaril supstituirani 1,4-benzodiazepini i njihova upotreba za liječenje raka
CN108026095B (zh) 2015-09-23 2021-07-27 詹森药业有限公司 新化合物
ES2775522T3 (es) * 2015-10-23 2020-07-27 Esteve Pharmaceuticals Sa Compuestos oxa-diazaspiro que tienen actividad contra el dolor
US10344035B2 (en) * 2015-12-31 2019-07-09 Shanghai Phaarmaceuticals Holding Co., Ltd. Salt of quinolone compound, polymorphs thereof, preparation method therefor, composition, and applications
PL3402792T3 (pl) * 2016-01-11 2022-01-17 Merck Patent Gmbh Pochodne chinolino-2-onowe
TWI590475B (zh) * 2016-06-17 2017-07-01 財團法人工業技術研究院 堆疊型太陽能電池模組
EP3509423A4 (en) 2016-09-08 2020-05-13 Kala Pharmaceuticals, Inc. CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
WO2018048747A1 (en) 2016-09-08 2018-03-15 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
MX2019002629A (es) 2016-09-08 2019-10-07 Kala Pharmaceuticals Inc Formas cristalinas de compuestos terapéuticos y usos de los mismos.
CN107935858B (zh) * 2016-10-12 2020-09-08 利尔化学股份有限公司 5-氟-2-硝基苯酚的制备方法
CN110087653A (zh) 2016-10-27 2019-08-02 普尔莫凯恩股份有限公司 用于治疗肺高血压的组合疗法
KR20200020888A (ko) 2017-06-27 2020-02-26 얀센 파마슈티카 엔.브이. 신규 퀴놀리논 화합물
EP3461480A1 (en) 2017-09-27 2019-04-03 Onxeo Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer
CA3082509A1 (en) 2017-11-24 2019-05-31 Janssen Pharmaceutica Nv Pyrazolopyridinone compounds
MX2020005342A (es) 2017-11-24 2020-10-14 Janssen Pharmaceutica Nv Compuestos de pirazolopiridinona.
JP2021532158A (ja) * 2018-07-31 2021-11-25 ザ、トラスティーズ オブ プリンストン ユニバーシティ 転移性癌および化学療法抵抗性癌の治療のためのテトラヒドロキノリノ誘導体
WO2020135483A1 (en) * 2018-12-26 2020-07-02 Janssen Pharmaceutica Nv Thienopyridinone compounds
WO2023147513A2 (en) * 2022-01-28 2023-08-03 Washington University Compositions of autophagy modulating agents and uses thereof

Family Cites Families (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3663606A (en) * 1966-06-21 1972-05-16 Mitsui Toatsu Chemicals Organic imino-compounds
DE2363459A1 (de) 1973-12-20 1975-06-26 Basf Ag Neue fluoreszierende chinolinverbindungen
US4287341A (en) 1979-11-01 1981-09-01 Pfizer Inc. Alkoxy-substituted-6-chloro-quinazoline-2,4-diones
US4659657A (en) * 1982-12-24 1987-04-21 Bayer Aktiengesellschaft Chromogenic and fluorogenic esters for photometric or fluorimetric determination of phosphatases or sulphatases
DE3634066A1 (de) * 1986-10-07 1988-04-21 Boehringer Mannheim Gmbh Neue 5-alkylbenzimidazole, verfahren zu ihrer herstellung sowie arzneimittel
US5073492A (en) * 1987-01-09 1991-12-17 The Johns Hopkins University Synergistic composition for endothelial cell growth
JPH0699497B2 (ja) 1987-04-16 1994-12-07 富士写真フイルム株式会社 光重合性組成物
DE3932953A1 (de) * 1989-10-03 1991-04-11 Boehringer Mannheim Gmbh Neue 2-bicyclo-benzimidazole, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
US5151360A (en) * 1990-12-31 1992-09-29 Biomembrane Institute Effect of n,n,n-trimethylsphingosine on protein kinase-c activity, melanoma cell growth in vitro, metastatic potential in vivo and human platelet aggregation
GB9108547D0 (en) 1991-04-22 1991-06-05 Fujisawa Pharmaceutical Co Quinoline derivatives
US5710158A (en) * 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5480883A (en) * 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
USRE37650E1 (en) * 1991-05-10 2002-04-09 Aventis Pharmacetical Products, Inc. Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
US5856115A (en) * 1991-05-24 1999-01-05 Fred Hutchinson Cancer Research Center Assay for identification therapeutic agents
DE69332948T2 (de) * 1992-03-05 2003-11-27 Univ Texas Verwendung von Immunokonjugate zur Diagnose und/oder Therapie der vaskularisierten Tumoren
JP3142378B2 (ja) 1992-06-22 2001-03-07 ティーディーケイ株式会社 有機ｅｌ素子
US5330992A (en) * 1992-10-23 1994-07-19 Sterling Winthrop Inc. 1-cyclopropyl-4-pyridyl-quinolinones
US5792771A (en) * 1992-11-13 1998-08-11 Sugen, Inc. Quinazoline compounds and compositions thereof for the treatment of disease
US5763441A (en) * 1992-11-13 1998-06-09 Sugen, Inc. Compounds for the treatment of disorders related to vasculogenesis and/or angiogenesis
US5981569A (en) * 1992-11-13 1999-11-09 Yissum Research Development Company Of The Hebrew University Of Jerusalem Substituted phenylacrylonitrile compounds and compositions thereof for the treatment of disease
JPH0743896A (ja) 1993-07-28 1995-02-14 Toyobo Co Ltd 光重合性組成物
US5716993A (en) 1993-12-27 1998-02-10 Eisai Co., Ltd. Anthranilic acid derivatives
JPH0829973A (ja) 1994-07-11 1996-02-02 Toyobo Co Ltd 光重合性組成物
JP3441246B2 (ja) 1995-06-07 2003-08-25 富士写真フイルム株式会社 光重合性組成物
GB9624482D0 (en) * 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
US6010711A (en) * 1996-01-26 2000-01-04 University Of Rochester Methods, articles and compositions for the pharmacologic inhibition of bone resorption with phosphodiesterase inhibitors
DE69734149T2 (de) 1996-03-15 2006-07-06 Astrazeneca Ab Cinoline derivate und verwendung als heilmittel
DE19610723A1 (de) 1996-03-19 1997-09-25 Bayer Ag Elektrolumineszierende Anordnungen unter Verwendung von Blendsystemen
US5942385A (en) * 1996-03-21 1999-08-24 Sugen, Inc. Method for molecular diagnosis of tumor angiogenesis and metastasis
EP0934307B1 (en) * 1996-06-19 2011-04-27 Aventis Pharma Limited Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase
CN1226245A (zh) 1996-06-20 1999-08-18 德克萨斯州大学系统董事会 具有药理活性的化合物,其制备方法及其用途
AU733551B2 (en) 1996-09-25 2001-05-17 Astrazeneca Ab Qinoline derivatives inhibiting the effect of growth factors such as VEGF
US6111110A (en) * 1996-10-30 2000-08-29 Eli Lilly And Company Synthesis of benzo[f]quinolinones
GB9716557D0 (en) * 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
US6294532B1 (en) 1997-08-22 2001-09-25 Zeneca Limited Oxindolylquinazoline derivatives as angiogenesis inhibitors
DE19756235A1 (de) * 1997-12-17 1999-07-01 Klinge Co Chem Pharm Fab Neue piperidinylsubstituierte Pyridylalkan- alken- und -alkincarbonsäureamide
AU3850299A (en) 1998-05-20 1999-12-06 Kyowa Hakko Kogyo Co. Ltd. Vegf activity inhibitors
US6174912B1 (en) * 1998-08-21 2001-01-16 Dupont Pharmaceuticals Company Nitrogen substituted imidazo[4,5-C]pyrazoles as corticotropin releasing hormone antagonists
DE19841985A1 (de) 1998-09-03 2000-03-09 Schering Ag Dialkylsulfonsäure- und Dialkylcarbonsäure-Derivate
IL126953A0 (en) 1998-11-08 1999-09-22 Yeda Res & Dev Pharmaceutical compositions comprising porphyrins and some novel porphyrin derivatives
US20030087854A1 (en) * 2001-09-10 2003-05-08 Isis Pharmaceuticals Inc. Antisense modulation of fibroblast growth factor receptor 3 expression
CN1129582C (zh) * 1998-12-04 2003-12-03 布里斯托尔-迈尔斯斯奎布公司 作为钾通道调节剂的3－取代－4－芳基喹啉－2－酮衍生物
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
KR100298572B1 (ko) * 1999-08-19 2001-09-22 박찬구 카바아닐라이드로부터 4-니트로디페닐아민과 4-니트로소디페닐아민의 제조방법
DZ3223A1 (fr) * 1999-10-19 2001-04-26 Merck & Co Inc Inhibiteurs de tyrosine kinases
ATE290865T1 (de) * 1999-10-19 2005-04-15 Merck & Co Inc Tyrosin kinase inhibitoren
YU54202A (sh) 2000-01-18 2006-01-16 Agouron Pharmaceuticals Inc. Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije
US7045133B2 (en) 2000-01-18 2006-05-16 Ludwig Institute For Cancer Research VEGF-D/VEGF-C/VEGF peptidomimetic inhibitor
CN101053573A (zh) 2000-01-19 2007-10-17 帕卡什·S·吉尔 针对反义vegf寡核苷酸的方法和组合物
GB0001930D0 (en) 2000-01-27 2000-03-22 Novartis Ag Organic compounds
WO2001060814A2 (en) 2000-02-15 2001-08-23 Sugen, Inc. Pyrrole substituted 2-indolinone protein kinase inhibitors
US6420382B2 (en) * 2000-02-25 2002-07-16 Merck & Co., Inc. Tyrosine kinase inhibitors
US6313138B1 (en) * 2000-02-25 2001-11-06 Merck & Co., Inc. Tyrosine kinase inhibitors
EP1259236A4 (en) 2000-02-25 2004-11-03 Merck & Co Inc Tyrosine kinase inhibitors
CA2402589C (en) * 2000-03-07 2011-02-01 Sanjay Garg Compositions and methods for trapping and inactivating pathogenic microbes and spermatozoa
US6257320B1 (en) * 2000-03-28 2001-07-10 Alec Wargo Heat sink device for power semiconductors
EP1313734B1 (en) * 2000-09-01 2009-11-11 Novartis Vaccines and Diagnostics, Inc. Aza heterocyclic derivatives and their therapeutic use
WO2002020500A2 (en) * 2000-09-01 2002-03-14 Icos Corporation Materials and methods to potentiate cancer treatment
AP1666A (en) * 2000-09-11 2006-09-29 Chiron Corp Quinolinone derivatives as tyrosine kinase inhibitors.
US20030028018A1 (en) * 2000-09-11 2003-02-06 Chiron Coporation Quinolinone derivatives
EP1188751A1 (en) * 2000-09-13 2002-03-20 Casale Chemicals SA Process for the production of high purity melamine from urea
US7064215B2 (en) * 2001-07-03 2006-06-20 Chiron Corporation Indazole benzimidazole compounds
US7495104B2 (en) * 2001-10-17 2009-02-24 Kirin Beer Kabushiki Kaisha Quinoline or quinazoline derivatives inhibiting auto-phosphorylation of fibroblast growth factor receptors
US6476068B1 (en) * 2001-12-06 2002-11-05 Pharmacia Italia, S.P.A. Platinum derivative pharmaceutical formulations
US20030159702A1 (en) * 2002-01-21 2003-08-28 Lindell Katarina E.A. Formulation and use manufacture thereof
US6822097B1 (en) * 2002-02-07 2004-11-23 Amgen, Inc. Compounds and methods of uses
WO2004018419A2 (en) * 2002-08-23 2004-03-04 Chiron Corporation Benzimidazole quinolinones and uses thereof
US7825132B2 (en) * 2002-08-23 2010-11-02 Novartis Vaccines And Diagnostics, Inc. Inhibition of FGFR3 and treatment of multiple myeloma
US20050256157A1 (en) * 2002-08-23 2005-11-17 Chiron Corporation Combination therapy with CHK1 inhibitors
AU2003275282A1 (en) * 2002-09-30 2004-04-23 Bristol-Myers Squibb Company Novel tyrosine kinase inhibitors
BR0316229A (pt) * 2002-11-13 2005-10-04 Chiron Corp Métodos de tratamento de câncer e métodos relacionados
US6774327B1 (en) * 2003-09-24 2004-08-10 Agilent Technologies, Inc. Hermetic seals for electronic components
SI1680140T1 (sl) * 2003-10-16 2011-08-31 Imclone Llc Inhibitorji receptorja-1 za fibroblastni rastni faktor in metode za zdravljenje z le-temi
EP1682529A4 (en) * 2003-11-07 2010-06-30 Novartis Vaccines & Diagnostic METHODS FOR SYNTHESIS OF QUINOLINONE COMPOUNDS
EP1718306A2 (en) * 2004-02-20 2006-11-08 Chiron Corporation Modulation of inflammatory and metastatic processes
MX2007014612A (es) * 2005-05-18 2008-01-17 M & G Polimeri Italia Spa Composicion de poliester.

Also Published As

Publication number Publication date
IL174767A0 (en) 2006-08-20
US20130018058A1 (en) 2013-01-17
EA012621B1 (ru) 2009-10-30
WO2005046589A3 (en) 2007-11-22
WO2005046589A2 (en) 2005-05-26
AU2004289672C1 (en) 2010-12-02
EP1699421A2 (en) 2006-09-13
CA2544492A1 (en) 2005-05-26
KR20070011231A (ko) 2007-01-24
WO2005046590A2 (en) 2005-05-26
CA2543820C (en) 2012-07-10
AU2004288709A1 (en) 2005-05-26
KR101224410B1 (ko) 2013-01-23
EP1692085A4 (en) 2010-10-13
JP4724665B2 (ja) 2011-07-13
JP4823914B2 (ja) 2011-11-24
EP1699421B1 (en) 2014-05-21
CA2543820A1 (en) 2005-05-26
IL174471A (en) 2013-06-27
HK1097444A1 (en) 2007-06-29
US20050137399A1 (en) 2005-06-23
CA2544492C (en) 2013-01-29
IL217114A0 (en) 2012-01-31
BRPI0416143A (pt) 2007-01-02
JP4890255B2 (ja) 2012-03-07
IL217114A (en) 2015-04-30
AU2011202249B2 (en) 2013-02-21
IL174471A0 (en) 2006-08-01
WO2005047244A2 (en) 2005-05-26
CN102225926A (zh) 2011-10-26
WO2005047244A3 (en) 2006-12-21
TW200526604A (en) 2005-08-16
JP2007510668A (ja) 2007-04-26
JP2011162563A (ja) 2011-08-25
EP2762475A1 (en) 2014-08-06
AU2004289672A1 (en) 2005-05-26
MXPA06004194A (es) 2006-06-28
TWI347940B (en) 2011-09-01
ES2486240T3 (es) 2014-08-18
EP1682529A4 (en) 2010-06-30
JP2007522098A (ja) 2007-08-09
CA2544186A1 (en) 2005-05-26
AU2004288692A1 (en) 2005-05-26
US20090181979A1 (en) 2009-07-16
EP1682529A2 (en) 2006-07-26
KR101167573B1 (ko) 2012-07-30
EP1692085A2 (en) 2006-08-23
IL219818A0 (en) 2012-06-28
US20050209247A1 (en) 2005-09-22
US20140303182A1 (en) 2014-10-09
AU2004289672B2 (en) 2010-06-24
KR20060111520A (ko) 2006-10-27
US20120277434A1 (en) 2012-11-01
AU2004288709B2 (en) 2011-01-06
IL175385A0 (en) 2008-04-13
IL175385A (en) 2012-06-28
KR20070011241A (ko) 2007-01-24
AU2011202249A1 (en) 2011-06-02
JP2011042687A (ja) 2011-03-03
US20130338171A1 (en) 2013-12-19
JP2007510665A (ja) 2007-04-26
EP1699421A4 (en) 2010-02-17
JP5214768B2 (ja) 2013-06-19
WO2005046590A3 (en) 2005-10-20

Similar Documents

Publication Publication Date Title
EA200600928A1 (ru) Фармацевтически приемлемые соли хинолиноновых соединений с улучшенными фармацевтическими свойствами
EA200501009A1 (ru) Замещённые пирролопиразольные производные в качестве ингибиторов киназы
EA200501936A1 (ru) Производные пиридо[2,1-a]изохинолина в качестве ингибиторов dpp-iv
CY1119381T1 (el) Παραγωγα 2-μεθυλομορφολινο πυριδο-, πυραζο- και πυριμιδο-πυριμιδινης ως αναστολεις mtor
EA200400480A1 (ru) N-замещённые производные пирролидина в качестве ингибиторов дипептидилпептидазы
EA200800172A1 (ru) 2,4-диаминопиримидины как ингибиторы aurora
DE60328010D1 (de) Heterocyclische verbindungen
EA201001368A1 (ru) Гетероциклические производные мочевины и способы их применения-211
EA200601747A1 (ru) Три(цикло)замещённые амидные соединения
EA200801287A1 (ru) Пиримидиновые производные для лечения аномального клеточного роста
MY136761A (en) Oxazol derivatives
ATE484508T1 (de) Furylverbindungen
EA200901241A1 (ru) Соединения для лечения гепатита с
ATE307810T1 (de) Imidazol-2-carbonsäureamid derivate als raf- kinase-inhibitoren
SE0402762D0 (sv) Indazole sulphonamide derivatives
EA200700901A1 (ru) Производные 2-амидо-4-фенилтиазола, их получение и применение в терапии
DE60333746D1 (de) Thienylverbindungen
DE602006010738D1 (de) Pyrroloä2,3-cüpyridinderivate
EA201001858A1 (ru) Гетероциклические производные мочевины для лечения бактериальных инфекций
SE0302573D0 (sv) Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof
EA201001859A1 (ru) Гетероциклические производные мочевины и способы их применеия
WO2006051314A3 (en) Guanidine derivatives as inhibitors of ddah
UA83832C2 (ru) Производные бензимидазола, фармацевтическая композиция, которая их содержит, способ их получения и их применение
SE0302570D0 (sv) Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof
EA200601176A1 (ru) 3-цианохинолиновые производные с антипролиферативной активностью

Legal Events

Date Code Title Description
PD4A Registration of transfer of a eurasian patent in accordance with the succession in title
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ MD

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): BY KZ KG TJ TM RU