TWI347940B - Methods for synthesizing quinolinone compounds - Google Patents

Methods for synthesizing quinolinone compounds

Info

Publication number
TWI347940B
TWI347940B TW093133800A TW93133800A TWI347940B TW I347940 B TWI347940 B TW I347940B TW 093133800 A TW093133800 A TW 093133800A TW 93133800 A TW93133800 A TW 93133800A TW I347940 B TWI347940 B TW I347940B
Authority
TW
Taiwan
Prior art keywords
methods
quinolinone compounds
synthesizing
synthesizing quinolinone
compounds
Prior art date
Application number
TW093133800A
Other languages
English (en)
Chinese (zh)
Other versions
TW200526604A (en
Inventor
Shaopei Cai
Eric Harwood
David Ryckman
Xiao Shang
Shuguang Zhu
Joyce Chou
Timothy Machajewski
Augustus O Okhamafe
Marc S Tesconi
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of TW200526604A publication Critical patent/TW200526604A/zh
Application granted granted Critical
Publication of TWI347940B publication Critical patent/TWI347940B/zh

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 or sparfloxacin
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
TW093133800A 2003-11-07 2004-11-05 Methods for synthesizing quinolinone compounds TWI347940B (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US51791503P 2003-11-07 2003-11-07
US52642603P 2003-12-02 2003-12-02
US52642503P 2003-12-02 2003-12-02
US54601704P 2004-02-19 2004-02-19

Publications (2)

Publication Number Publication Date
TW200526604A TW200526604A (en) 2005-08-16
TWI347940B true TWI347940B (en) 2011-09-01

Family

ID=34596121

Family Applications (1)

Application Number Title Priority Date Filing Date
TW093133800A TWI347940B (en) 2003-11-07 2004-11-05 Methods for synthesizing quinolinone compounds

Country Status (14)

Country Link
US (7) US20050209247A1 (https=)
EP (4) EP2762475A1 (https=)
JP (5) JP4724665B2 (https=)
KR (3) KR20060111520A (https=)
CN (1) CN102225926A (https=)
AU (3) AU2004288709B2 (https=)
BR (1) BRPI0416143A (https=)
CA (3) CA2544186A1 (https=)
EA (1) EA012621B1 (https=)
ES (1) ES2486240T3 (https=)
IL (5) IL174471A (https=)
MX (1) MXPA06004194A (https=)
TW (1) TWI347940B (https=)
WO (3) WO2005046589A2 (https=)

Families Citing this family (96)

* 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
CZ304344B6 (cs) 2000-09-11 2014-03-19 Novartis Vaccines & Diagnostics, Inc. Chinolinonový derivát a jeho použití a farmaceutický prostředek s obsahem tohoto derivátu
US7825132B2 (en) * 2002-08-23 2010-11-02 Novartis Vaccines And Diagnostics, Inc. Inhibition of FGFR3 and treatment of multiple myeloma
CA2496164C (en) 2002-08-23 2010-11-09 Chiron Corporation Benzimidazole quinolinones and uses thereof
AU2003290699B2 (en) * 2002-11-13 2009-08-27 Novartis Vaccines And Diagnostics, Inc. Methods of treating cancer and related methods
CN102225926A (zh) * 2003-11-07 2011-10-26 诺华疫苗和诊断公司 具有改进药物特性的喹啉酮类化合物的药学上可接受的盐
US7875624B2 (en) * 2004-02-20 2011-01-25 Novartis Vaccines And Diagnostics, Inc. Modulating and measuring cellular adhesion
KR101387985B1 (ko) * 2005-01-27 2014-04-25 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 전이 종양의 치료
US8034823B2 (en) * 2005-02-22 2011-10-11 Savvipharm Inc Method of increasing drug oral bioavailability and compositions of less toxic orotate salts
ES2732251T3 (es) * 2005-04-25 2019-11-21 Enterin Inc Dilactato de escualamina cristalino
CA2608171C (en) * 2005-05-13 2014-02-04 Novartis Ag Use of quinolinone compounds for treating drug resistant cancers
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
MX2007014782A (es) * 2005-05-23 2008-02-19 Novartis Ag Formas cristalinas y otras formas de las sales de acido lactico de 4-amino-5-fluoro-3-[6-(4-metilpiperazin-1-il)-1h-bencimidazol-2 -il]-1h quinolin-2-ona.
EP1904065A2 (en) * 2005-07-14 2008-04-02 AB Science Use of dual c-kit/fgfr3 inhibitors for treating multiple myeloma
RU2433826C2 (ru) * 2005-11-29 2011-11-20 Новартис Аг Композиции хинолинонов
CN101316593B (zh) * 2005-11-29 2012-05-02 诺瓦提斯公司 喹啉酮类的制剂
JP2009523410A (ja) 2005-12-08 2009-06-25 ノバルティス アクチエンゲゼルシャフト 遺伝子転写に対するｆｇｆｒ３の阻害剤の効果
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
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
WO2008044041A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
CA2679268A1 (en) * 2007-03-09 2008-09-18 Novartis Ag Treatment of melanoma
EP2170859A1 (en) 2007-06-25 2010-04-07 F. Hoffmann-Roche AG Benzimidazole amido derivatives as kinase inhibitors
GB0800855D0 (en) 2008-01-17 2008-02-27 Syngenta Ltd Herbicidal compounds
JPWO2009113436A1 (ja) * 2008-03-14 2011-07-21 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
PE20091628A1 (es) * 2008-03-19 2009-11-19 Novartis Ag Formas cristalinas y dos formas solvatadas de sales de acido lactico de 4-amino-5-fluoro-3-[5-(4-metilpiperazin-1-il)-1h-benzimidazol-2-il]quinolin-2(1h)-ona
EP2370417A2 (en) * 2008-11-21 2011-10-05 Millennium Pharmaceuticals, 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
WO2010075443A1 (en) * 2008-12-22 2010-07-01 Burnham Institute For Medical Research Selective inhibitors of akt and methods of using same
SG173014A1 (en) 2009-01-16 2011-08-29 Exelixis Inc Malate salt of n- (4- { [ 6, 7-bis (methyloxy) quin0lin-4-yl] oxy}phenyl)-n' - (4 -fluorophenyl) cyclopropane-1,1-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
MX2012011090A (es) * 2010-03-26 2012-10-10 Novartis Ag Preparacion de polimorfos hidratados de sal de acido lactico de la 4-amino-5-fluoro-3-[6-(4-metil-piperazin-1-il)-1h-bencimidazol- 2-il]-1h-quinolin-2-ona.
NZ602807A (en) * 2010-04-16 2014-02-28 Novartis Ag 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1h-benzimidazol-2-yl]-1h-quinolin-2-one and an mtor inhibitor
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
EP2593090B1 (en) 2010-07-16 2021-10-13 Exelixis, Inc. C-met modulator pharmaceutical compositions
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
JP2014505109A (ja) 2011-02-10 2014-02-27 エクセリクシス， インク． キノリン化合物およびそのような化合物を含有する医薬組成物の調製方法
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
GB201118654D0 (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
WO2013063003A1 (en) 2011-10-28 2013-05-02 Novartis Ag Method of treating gastrointestinal stromal tumors
GB201118652D0 (en) * 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118675D0 (en) 2011-10-28 2011-12-14 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
JP2015505562A (ja) 2012-01-31 2015-02-23 ノバルティス アーゲー Ｒｔｋ阻害剤と抗エストロゲン剤との組合せ、およびがん治療のためのその使用
HK1205528A1 (en) 2012-03-08 2015-12-18 Astellas Pharma Inc. Novel fgfr3 fusion product
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
US20150202203A1 (en) 2012-07-11 2015-07-23 Novartis Ag Method of Treating Gastrointestinal Stromal Tumors
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
CA2886002C (en) * 2012-09-27 2020-06-09 Chugai Seiyaku Kabushiki Kaisha Fgfr3 fusion gene and pharmaceutical drug targeting same
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
DK2950649T3 (da) 2013-02-01 2020-05-04 Wellstat Therapeutics Corp Aminforbindelser med antiinflammations-, antisvampe-, antiparasit- og anticanceraktivitet
JP6669499B2 (ja) 2013-02-15 2020-03-18 カラ ファーマシューティカルズ インコーポレイテッド 治療用化合物
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
JP2016510000A (ja) 2013-02-20 2016-04-04 カラ ファーマシューティカルズ インコーポレイテッド 治療用化合物およびその使用
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
US9925184B2 (en) 2013-10-11 2018-03-27 Pulmokine, Inc. Spray-dry formulations
JP6223563B2 (ja) 2013-10-14 2017-11-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 選択的に置換されたキノリン化合物
CN105636945B (zh) 2013-10-14 2017-11-17 卫材R&D管理有限公司 选择性取代的喹啉化合物
US9890173B2 (en) 2013-11-01 2018-02-13 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
NZ719185A (en) 2013-11-01 2017-11-24 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
JP6752715B2 (ja) 2014-03-26 2020-09-09 アステックス、セラピューティックス、リミテッドＡｓｔｅｘ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｌｉｍｉｔｅｄ 組合せ
MX373150B (es) 2014-03-26 2020-04-21 Astex Therapeutics Ltd Combinaciones de un inhibidor del factor de crecimiento de fibroblasto (fgfr) y un inhibidor del receptor del factor de crecimiento 1 similar a insulina (igf1r).
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
EP2977374A1 (en) * 2014-07-21 2016-01-27 Université de Strasbourg Molecules presenting dual emission properties
RU2743074C2 (ru) 2014-08-01 2021-02-15 Нуэволюшон А/С Соединения, активные по отношению к бромодоменам
TWI719960B (zh) 2015-02-10 2021-03-01 英商阿斯迪克治療公司 新穎組成物
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
GB201506660D0 (en) 2015-04-20 2015-06-03 Cellcentric Ltd Pharmaceutical compounds
GB201506658D0 (en) 2015-04-20 2015-06-03 Cellcentric Ltd Pharmaceutical compounds
AU2016328693B2 (en) 2015-09-23 2021-03-11 Janssen Pharmaceutica Nv Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer
DK3353177T3 (da) 2015-09-23 2020-08-24 Janssen Pharmaceutica Nv Tricykliske heterocykler til behandling af cancer
ME03636B (me) * 2015-10-23 2020-07-20 Esteve Pharmaceuticals Sa Oksa-diazaspiro jedinjenja која imaju aktivnost protiv bola
CN109369656B (zh) * 2015-12-31 2021-05-07 上海医药集团股份有限公司 喹啉类化合物硫酸盐的晶型、制备方法、组合物与应用
SG11201805869XA (en) * 2016-01-11 2018-08-30 Merck Patent Gmbh Quinolin-2-one derivatives
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
AU2017324713B2 (en) 2016-09-08 2020-08-13 KALA BIO, Inc. Crystalline forms of therapeutic compounds and uses thereof
EP3509423A4 (en) 2016-09-08 2020-05-13 Kala Pharmaceuticals, Inc. CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
KR20190051010A (ko) 2016-09-08 2019-05-14 칼라 파마슈티컬스, 인크. 치료 화합물의 결정형 및 그의 용도
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
RU2763525C2 (ru) 2016-10-27 2021-12-30 Пульмокин, Инк. Комбинированная терапия для лечения легочной гипертензии
EP3645526B1 (en) * 2017-06-27 2024-09-04 Janssen Pharmaceutica NV New quinolinone compounds
EP3461480A1 (en) 2017-09-27 2019-04-03 Onxeo Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer
KR102723359B1 (ko) 2017-11-24 2024-10-28 얀센 파마슈티카 엔브이 피라졸로피리디논 화합물
EP3713941B1 (en) 2017-11-24 2022-06-22 Janssen Pharmaceutica NV Pyrazolopyridinone compounds
CN112638881B (zh) 2018-07-31 2025-01-07 普林斯顿大学托管委员会 用于治疗转移性和化疗耐受性癌症的四氢喹啉衍生物
MX2021007853A (es) * 2018-12-26 2021-08-11 Janssen Pharmaceutica Nv Compuestos de tienopiridinona.
EP4069696A1 (en) * 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
KR102925139B1 (ko) 2021-04-22 2026-02-10 카요테라 인코포레이티드 헤테로시클릭 화합물 및 이의 용도
WO2022261159A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US20250144110A1 (en) * 2022-01-28 2025-05-08 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
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
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
US5856115A (en) * 1991-05-24 1999-01-05 Fred Hutchinson Cancer Research Center Assay for identification therapeutic agents
EP1306095A3 (en) * 1992-03-05 2003-06-25 Board Of Regents, The University Of Texas System Methods and compositions for targeting the vasculature of solid tumors
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
US5763441A (en) * 1992-11-13 1998-06-09 Sugen, Inc. Compounds for the treatment of disorders related to vasculogenesis and/or angiogenesis
US5792771A (en) * 1992-11-13 1998-08-11 Sugen, Inc. Quinazoline compounds and compositions thereof for the treatment of disease
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
EP0686625B1 (en) 1993-12-27 1999-05-26 Eisai Co., Ltd. Anthranilic acid derivative
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
EP0888310B1 (en) 1996-03-15 2005-09-07 AstraZeneca AB Cinnoline derivatives and use as medicine
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
CA2258728C (en) * 1996-06-19 2011-09-27 Rhone Poulenc Rorer Limited Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase
HUP9904567A3 (en) 1996-06-20 2001-10-29 Univ Texas Use of azo, thioalkyl, thiocarbonyl derivatives substituted by fused heterocycles and/or phenyl group for the preparation of pharmaceutical compositions stimulating bone growth
KR100567649B1 (ko) 1996-09-25 2006-04-05 아스트라제네카 유케이 리미티드 혈관 내피 성장 인자와 같은 성장 인자의 효과를 억제하는 퀴놀린 유도체
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
WO1999010349A1 (en) 1997-08-22 1999-03-04 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
CA2328893A1 (en) 1998-05-20 1999-11-25 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
EP1133474B1 (en) * 1998-12-04 2007-02-21 Bristol-Myers Squibb Company 3-substituted-4-arylquinolin-2-one derivatives as potassium channel modulators
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
AU778042B2 (en) * 1999-10-19 2004-11-11 Merck & Co., Inc. Tyrosine kinase inhibitors
HRP20020349A2 (en) * 1999-10-19 2004-02-29 Merck & Co Inc Tyrosine kinase inhibitors
EP1248642A4 (en) 2000-01-18 2005-05-18 Ludwig Inst Cancer Res PEPTIDOMIMETIC INHIBITOR OF VEGF-D / VEGF-C / VEGF
YU54202A (sh) 2000-01-18 2006-01-16 Agouron Pharmaceuticals Inc. Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije
CN1307303C (zh) 2000-01-19 2007-03-28 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
SI1255752T1 (sl) 2000-02-15 2007-12-31 Pharmacia & Upjohn Co Llc S pirolom substituirani zaviralci 2-indolinon protein kinaza
US6420382B2 (en) 2000-02-25 2002-07-16 Merck & Co., Inc. Tyrosine kinase inhibitors
AU778417B2 (en) 2000-02-25 2004-12-02 Merck & Co., Inc. Tyrosine kinase inhibitors
US6313138B1 (en) * 2000-02-25 2001-11-06 Merck & Co., Inc. Tyrosine kinase inhibitors
WO2001066084A2 (en) * 2000-03-07 2001-09-13 Rush-Presbyterian-St. Luke's Medical Center 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
WO2002020500A2 (en) * 2000-09-01 2002-03-14 Icos Corporation Materials and methods to potentiate cancer treatment
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
CZ304344B6 (cs) * 2000-09-11 2014-03-19 Novartis Vaccines & Diagnostics, Inc. Chinolinonový derivát a jeho použití a farmaceutický prostředek s obsahem tohoto derivátu
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
EP1447405A4 (en) * 2001-10-17 2005-01-12 Kirin Brewery CHINOLIN OR CHINAZOLINE DERIVATIVES THAT PREVENT THE AUTOPHOSPHORYLATION OF RECEPTORS FOR THE FIBROBLAST GROWTH FACTOR
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
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
CA2496164C (en) * 2002-08-23 2010-11-09 Chiron Corporation Benzimidazole quinolinones and uses thereof
EP1545529A4 (en) * 2002-09-30 2010-03-03 Bristol Myers Squibb Co NEW TYROSINE KINASE HEMMER
AU2003290699B2 (en) 2002-11-13 2009-08-27 Novartis Vaccines And Diagnostics, Inc. Methods of treating cancer and related methods
US6774327B1 (en) * 2003-09-24 2004-08-10 Agilent Technologies, Inc. Hermetic seals for electronic components
WO2005037235A2 (en) * 2003-10-16 2005-04-28 Imclone Systems Incorporated Fibroblast growth factor receptor-1 inhibitors and methods of treatment thereof
CN102225926A (zh) * 2003-11-07 2011-10-26 诺华疫苗和诊断公司 具有改进药物特性的喹啉酮类化合物的药学上可接受的盐
US7875624B2 (en) * 2004-02-20 2011-01-25 Novartis Vaccines And Diagnostics, Inc. Modulating and measuring cellular adhesion
BRPI0613200A2 (pt) * 2005-05-18 2012-01-03 M & G Polimeri Italia Spa composiÇço de poliÉster

Also Published As

Publication number Publication date
JP2011042687A (ja) 2011-03-03
IL174471A (en) 2013-06-27
TW200526604A (en) 2005-08-16
JP2007510665A (ja) 2007-04-26
WO2005046589A3 (en) 2007-11-22
CA2544492A1 (en) 2005-05-26
EP1699421B1 (en) 2014-05-21
ES2486240T3 (es) 2014-08-18
IL175385A (en) 2012-06-28
KR20060111520A (ko) 2006-10-27
US20140303182A1 (en) 2014-10-09
IL174767A0 (en) 2006-08-20
EP1692085A2 (en) 2006-08-23
MXPA06004194A (es) 2006-06-28
JP5214768B2 (ja) 2013-06-19
KR101224410B1 (ko) 2013-01-23
AU2004288692A1 (en) 2005-05-26
EP1699421A4 (en) 2010-02-17
EP1682529A2 (en) 2006-07-26
WO2005046590A2 (en) 2005-05-26
IL175385A0 (en) 2008-04-13
KR101167573B1 (ko) 2012-07-30
IL217114A0 (en) 2012-01-31
EP1682529A4 (en) 2010-06-30
US20120277434A1 (en) 2012-11-01
US20050137399A1 (en) 2005-06-23
US20090181979A1 (en) 2009-07-16
EP1699421A2 (en) 2006-09-13
CA2544492C (en) 2013-01-29
KR20070011231A (ko) 2007-01-24
BRPI0416143A (pt) 2007-01-02
US20130018058A1 (en) 2013-01-17
AU2011202249B2 (en) 2013-02-21
EP1692085A4 (en) 2010-10-13
JP4823914B2 (ja) 2011-11-24
CA2543820A1 (en) 2005-05-26
AU2011202249A1 (en) 2011-06-02
JP4724665B2 (ja) 2011-07-13
HK1097444A1 (en) 2007-06-29
CN102225926A (zh) 2011-10-26
AU2004288709B2 (en) 2011-01-06
WO2005046590A3 (en) 2005-10-20
AU2004289672B2 (en) 2010-06-24
WO2005047244A2 (en) 2005-05-26
US20050209247A1 (en) 2005-09-22
EP2762475A1 (en) 2014-08-06
US20130338171A1 (en) 2013-12-19
JP2007510668A (ja) 2007-04-26
JP2011162563A (ja) 2011-08-25
JP4890255B2 (ja) 2012-03-07
IL219818A0 (en) 2012-06-28
IL174471A0 (en) 2006-08-01
CA2543820C (en) 2012-07-10
EA200600928A1 (ru) 2007-10-26
CA2544186A1 (en) 2005-05-26
WO2005046589A2 (en) 2005-05-26
JP2007522098A (ja) 2007-08-09
AU2004289672A1 (en) 2005-05-26
AU2004289672C1 (en) 2010-12-02
EA012621B1 (ru) 2009-10-30
IL217114A (en) 2015-04-30
AU2004288709A1 (en) 2005-05-26
KR20070011241A (ko) 2007-01-24
WO2005047244A3 (en) 2006-12-21

Similar Documents

Publication Publication Date Title
TWI347940B (en) Methods for synthesizing quinolinone compounds
GB0308114D0 (en) Novel compounds
EP1613322A4 (en) AMINOQUINOLINE COMPOUNDS
GB0305918D0 (en) Novel compounds
GB0308186D0 (en) Novel compounds
GB0308185D0 (en) Novel compounds
GB0304424D0 (en) Novel compounds
GB0309221D0 (en) Novel compounds
EP1596860A4 (en) NEW CONNECTIONS
GB0305426D0 (en) Novel compounds
GB0314980D0 (en) Methods for identifying compounds
GB0302431D0 (en) Novel compounds
GB0304809D0 (en) Novel compounds
GB0302546D0 (en) Novel compounds
HK1086575A (en) Methods for synthesizing quinolinone compounds
GB0309222D0 (en) Novel compounds
HU0300167D0 (en) Process for alginat obtaining from alginit
GB0301589D0 (en) Novel compounds
GB0301592D0 (en) Novel compounds
GB0301872D0 (en) Novel compounds
GB0302988D0 (en) Novel compounds
GB0303464D0 (en) Novel compounds
GB0304408D0 (en) Novel compounds
GB0301608D0 (en) Novel compounds
GB0301593D0 (en) Novel compounds

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees