AU2004289672C1 - Inhibition of FGFR3 and treatment of multiple myeloma - Google Patents

Inhibition of FGFR3 and treatment of multiple myeloma Download PDF

Info

Publication number
AU2004289672C1
AU2004289672C1 AU2004289672A AU2004289672A AU2004289672C1 AU 2004289672 C1 AU2004289672 C1 AU 2004289672C1 AU 2004289672 A AU2004289672 A AU 2004289672A AU 2004289672 A AU2004289672 A AU 2004289672A AU 2004289672 C1 AU2004289672 C1 AU 2004289672C1
Authority
AU
Australia
Prior art keywords
substituted
unsubstituted
groups
alkyl
heterocyclyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
AU2004289672A
Other languages
English (en)
Other versions
AU2004289672A1 (en
AU2004289672B2 (en
Inventor
Shaopei Cai
Joyce Chou
Eric Harwood
Carla C. Heise
Timothy D. Machajewski
David Ryckman
Xiao Shang
Marion Wiesmann
Shuguang Zhu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis Vaccines and Diagnostics Inc
Original Assignee
Novartis Vaccines and Diagnostics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis Vaccines and Diagnostics Inc filed Critical Novartis Vaccines and Diagnostics Inc
Publication of AU2004289672A1 publication Critical patent/AU2004289672A1/en
Assigned to NOVARTIS VACCINES AND DIAGNOSTICS, INC. reassignment NOVARTIS VACCINES AND DIAGNOSTICS, INC. Alteration of Name(s) of Applicant(s) under S113 Assignors: CHIRON CORPORATION
Assigned to NOVARTIS VACCINES AND DIAGNOSTICS, INC. reassignment NOVARTIS VACCINES AND DIAGNOSTICS, INC. Alteration of Name(s) of Applicant(s) under S113 Assignors: CHIRON CORPORATION
Application granted granted Critical
Publication of AU2004289672B2 publication Critical patent/AU2004289672B2/en
Publication of AU2004289672C1 publication Critical patent/AU2004289672C1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic 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
    • A61K31/4375Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54Heterocyclic 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
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41Preparation of salts of carboxylic acids
    • C07C51/412Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/01Saturated compounds having only one carboxyl group and containing hydroxy or O-metal groups
    • C07C59/08Lactic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Obesity (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)
AU2004289672A 2003-11-07 2004-11-05 Inhibition of FGFR3 and treatment of multiple myeloma Ceased AU2004289672C1 (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US51791503P 2003-11-07 2003-11-07
US60/517,915 2003-11-07
US52642603P 2003-12-02 2003-12-02
US52642503P 2003-12-02 2003-12-02
US60/526,425 2003-12-02
US60/526,426 2003-12-02
US54601704P 2004-02-19 2004-02-19
US60/546,017 2004-02-19
PCT/US2004/036956 WO2005047244A2 (en) 2003-11-07 2004-11-05 Inhibition of fgfr3 and treatment of multiple myeloma

Publications (3)

Publication Number Publication Date
AU2004289672A1 AU2004289672A1 (en) 2005-05-26
AU2004289672B2 AU2004289672B2 (en) 2010-06-24
AU2004289672C1 true AU2004289672C1 (en) 2010-12-02

Family

ID=34596121

Family Applications (3)

Application Number Title Priority Date Filing Date
AU2004289672A Ceased AU2004289672C1 (en) 2003-11-07 2004-11-05 Inhibition of FGFR3 and treatment of multiple myeloma
AU2004288709A Ceased AU2004288709B2 (en) 2003-11-07 2004-11-05 Methods for synthesizing quinolinone compounds
AU2011202249A Ceased AU2011202249B2 (en) 2003-11-07 2011-05-16 Pharmaceutically acceptable salts of quinolinone compounds having improved pharmaceutical properties

Family Applications After (2)

Application Number Title Priority Date Filing Date
AU2004288709A Ceased AU2004288709B2 (en) 2003-11-07 2004-11-05 Methods for synthesizing quinolinone compounds
AU2011202249A Ceased AU2011202249B2 (en) 2003-11-07 2011-05-16 Pharmaceutically acceptable salts of quinolinone compounds having improved pharmaceutical properties

Country Status (14)

Country Link
US (7) US20050209247A1 (enExample)
EP (4) EP1692085A4 (enExample)
JP (5) JP4724665B2 (enExample)
KR (3) KR101224410B1 (enExample)
CN (1) CN102225926A (enExample)
AU (3) AU2004289672C1 (enExample)
BR (1) BRPI0416143A (enExample)
CA (3) CA2544492C (enExample)
EA (1) EA012621B1 (enExample)
ES (1) ES2486240T3 (enExample)
IL (5) IL174471A (enExample)
MX (1) MXPA06004194A (enExample)
TW (1) TWI347940B (enExample)
WO (3) WO2005046590A2 (enExample)

Families Citing this family (96)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2334641T3 (es) 2000-09-01 2010-03-15 Novartis Vaccines And Diagnostics, Inc. Derivados aza heterociclicos y su uso terapeutico.
US20030028018A1 (en) * 2000-09-11 2003-02-06 Chiron Coporation Quinolinone derivatives
NZ524717A (en) 2000-09-11 2004-09-24 Chiron Corp Quinolinone derivatives
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
US7838527B2 (en) * 2002-11-13 2010-11-23 Novartis Vaccines And Diagnostics, Inc. Methods of treating cancer and related methods
KR101224410B1 (ko) * 2003-11-07 2013-01-23 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 퀴놀리논 화합물을 합성하는 방법
RU2377988C2 (ru) * 2004-02-20 2010-01-10 Новартис Вэксинес Энд Дайэгностикс, Инк. Модуляция воспалительных и метастатических процессов
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
CA2606077C (en) * 2005-04-25 2013-07-09 Genaera Corporation Polymorphic and amorphous salt forms of squalamine dilactate
PT1885187E (pt) 2005-05-13 2013-12-16 Novartis Ag Métodos para o tratamento de cancro resistente a fármacos
PL1888556T3 (pl) * 2005-05-17 2012-03-30 Novartis Ag Metody syntetyzowania związków heterocyklicznych
AU2012258324B2 (en) * 2005-05-17 2014-07-24 Novartis Ag Methods for synthesizing heterocyclic compounds
RU2425041C2 (ru) * 2005-05-23 2011-07-27 Новартис Аг Кристаллические и другие формы солей, образованных из молочной кислоты и 4-амино-5-фтор-3-[6-(4-метилпиперазин-1-ил)-1н-бензимидазол-2-ил]-1н-хинолин-2-она
EP1904065A2 (en) * 2005-07-14 2008-04-02 AB Science Use of dual c-kit/fgfr3 inhibitors for treating multiple myeloma
CN101316593B (zh) * 2005-11-29 2012-05-02 诺瓦提斯公司 喹啉酮类的制剂
AR062545A1 (es) 2005-11-29 2008-11-19 Novartis Ag Formulaciones estables de quinolinonas
RU2008127252A (ru) 2005-12-08 2010-01-20 Новартис АГ (CH) Эффекты ингибиторов fgfr3 на транскрипцию генов
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
US8916552B2 (en) 2006-10-12 2014-12-23 Astex Therapeutics Limited Pharmaceutical combinations
MX2009009574A (es) * 2007-03-09 2009-09-16 Novartis Ag Tratamiento de melanoma.
CN101687840A (zh) 2007-06-25 2010-03-31 霍夫曼-拉罗奇有限公司 作为激酶抑制剂的苯并咪唑酰胺基衍生物
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
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
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
WO2010075443A1 (en) * 2008-12-22 2010-07-01 Burnham Institute For Medical Research Selective inhibitors of akt and methods of using same
CA2995880C (en) 2009-01-16 2021-01-05 Exelixis, Inc. Processes for preparing n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
KR20130018275A (ko) 2010-03-26 2013-02-20 노파르티스 아게 4-아미노-5-플루오로-3-[6-(4-메틸피페라진-1-일)-1h-벤즈이미다졸-2-일]-1h-퀴놀린-2-온 락트산 염의 수화된 다형체의 제조
SG184311A1 (en) * 2010-04-16 2012-11-29 Novartis Ag Combination of organic compounds
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
IL224189A (en) 2010-07-16 2017-07-31 Exelixis Inc C-met modulator pharmaceutical compositions
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
KR20210147117A (ko) 2011-02-10 2021-12-06 엑셀리시스, 인코포레이티드 퀴놀린 화합물들의 제조 방법들 및 상기 화합물들을 함유하는 약학 조성물들
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
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
GB201118656D0 (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
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
MX2014009303A (es) 2012-01-31 2014-10-14 Novartis Ag Combinacion de un inhibidor de rtk con un anti-estrogeno y uso del mismo para el tratamiento de cancer.
JP6107812B2 (ja) 2012-03-08 2017-04-05 アステラス製薬株式会社 新規fgfr3融合体
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
IN2014DN10801A (enExample) 2012-07-11 2015-09-04 Novartis Ag
KR102068860B1 (ko) * 2012-07-17 2020-01-21 사노피 Vegfr-3 저해제의 간세포암 치료를 위한 용도
US10689705B2 (en) 2012-09-27 2020-06-23 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
WO2014110200A1 (en) 2013-01-10 2014-07-17 Zisman Lawrence S Non-selective kinase inhibitors
EP2950649B1 (en) 2013-02-01 2020-03-04 Wellstat Therapeutics Corporation Amine compounds having anti-inflammatory, antifungal, antiparasitic and anticancer activity
HK1217092A1 (zh) 2013-02-15 2016-12-23 Kala Pharmaceuticals, Inc. 治疗性化合物及其用途
CN105189462B (zh) 2013-02-20 2017-11-10 卡拉制药公司 治疗性化合物和其用途
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
SG10201704327RA (en) 2013-10-14 2017-06-29 Eisai R&D Man Co Ltd Selectively substituted quinoline compounds
MX363708B (es) 2013-10-14 2019-03-29 Eisai R&D Man Co Ltd Compuestos de quinolina selectivamente sustituidos.
AU2014342042B2 (en) 2013-11-01 2017-08-17 KALA BIO, Inc. Crystalline forms of therapeutic compounds and uses thereof
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
BR112016022062B1 (pt) 2014-03-26 2023-04-11 Astex Therapeutics Limited Combinação, composição farmacêutica, uso de uma combinação ou de uma composição farmacêutica, e, produto farmacêutico
PL3122358T3 (pl) 2014-03-26 2021-06-14 Astex Therapeutics Ltd. Połączenia inhibitorów fgfr i cmet w leczeniu nowotworu
EP2977374A1 (en) * 2014-07-21 2016-01-27 Université de Strasbourg Molecules presenting dual emission properties
KR102633122B1 (ko) 2014-08-01 2024-02-05 누에볼루션 에이/에스 브로모도메인에 대하여 활성을 갖는 화합물
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
US20180237424A1 (en) 2015-03-03 2018-08-23 Inserm (Institut National De La Sante Et De La Recherche Medicale) 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
BR112018005637B1 (pt) 2015-09-23 2023-11-28 Janssen Pharmaceutica Nv Compostos derivados de quinoxalina, quinolina e quinazolinona,composições farmacêuticas que os compreende, e uso dos referidos compostos
SI3365346T1 (sl) * 2015-10-23 2020-04-30 Esteve Pharmaceuticals, S.A. Spojine oksa diazaspiro s protibolečinskim delovanjem
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
LT3402792T (lt) * 2016-01-11 2021-12-10 Merck Patent Gmbh Chinolin-2-ono dariniai
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
CA3036340A1 (en) 2016-09-08 2018-03-15 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
CA3036336A1 (en) 2016-09-08 2018-03-15 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
WO2018048746A1 (en) 2016-09-08 2018-03-15 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
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
MX389551B (es) 2016-10-27 2025-03-20 Pulmokine Inc Politerapia para tratar hipertension pulmonar.
MX2020000135A (es) * 2017-06-27 2020-07-22 Janssen Pharmaceutica Nv Nuevos compuestos de quinolinona.
EP3461480A1 (en) 2017-09-27 2019-04-03 Onxeo Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer
JP7329510B2 (ja) 2017-11-24 2023-08-18 ヤンセン ファーマシューティカ エヌ.ベー. ピラゾロピリジノン化合物
WO2019101182A1 (en) 2017-11-24 2019-05-31 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
CN113227100B (zh) * 2018-12-26 2023-05-05 詹森药业有限公司 噻吩并吡啶酮化合物
JP7720840B2 (ja) * 2019-12-04 2025-08-08 インサイト・コーポレイション Fgfr阻害剤としての三環式複素環
MX2023012435A (es) 2021-04-22 2024-02-08 Kayothera Inc Compuestos heterociclicos y usos de los mismos.
WO2022261159A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2023147513A2 (en) * 2022-01-28 2023-08-03 Washington University Compositions of autophagy modulating agents and uses thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002022598A1 (en) * 2000-09-11 2002-03-21 Chiron Corporation Quinolinone derivatives as tyrosine kinase inhibitors

Family Cites Families (75)

* 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
EP0627940B1 (en) * 1992-03-05 2003-05-07 Board of Regents, The University of Texas System Use of immunoconjugates for the diagnosis and/or therapy of vascularized 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
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
US5792771A (en) * 1992-11-13 1998-08-11 Sugen, Inc. Quinazoline 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
NZ277556A (en) 1993-12-27 1997-06-24 Eisai Co Ltd N-phenyl(alkyl)- and n-pyridyl(alkyl)anthranilic acid derivatives; intermediates
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
WO1997034876A1 (en) 1996-03-15 1997-09-25 Zeneca Limited 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
WO1997048697A1 (en) * 1996-06-19 1997-12-24 Rhone-Poulenc Rorer Limited Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase
BR9711805A (pt) 1996-06-20 2002-01-15 Regents The Univesity Of Texas Compostos e métodos para providenciar preparações farmacologicamente ativas e uso dos mesmos
JP2001500890A (ja) * 1996-09-25 2001-01-23 ゼネカ リミテッド Vegfのような成長因子の作用を阻害するキノリン誘導体
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
EP1086705A4 (en) 1998-05-20 2002-02-06 Kyowa Hakko Kogyo Kk INHIBITORS OF VASCULAR ENDOTHELIAL GROWTH FACTOR (VEGF) ACTIVITY
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
DK1133474T3 (da) * 1998-12-04 2007-04-10 Bristol Myers Squibb Co 3-Substituerede 4-arylquinolin-2-onderivater som kaliumkanal-modulatorer
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
WO2001028993A2 (en) 1999-10-19 2001-04-26 Merck & Co. Inc. Tyrosine kinase inhibitors
EP1226136B1 (en) 1999-10-19 2004-12-29 Merck & Co., Inc. Tyrosine kinase inhibitors
YU54202A (sh) 2000-01-18 2006-01-16 Agouron Pharmaceuticals Inc. Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije
EP1248642A4 (en) 2000-01-18 2005-05-18 Ludwig Inst Cancer Res PEPTIDOMIMETIC INHIBITOR OF VEGF-D / VEGF-C / VEGF
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
BRPI0117360B8 (pt) 2000-02-15 2021-07-06 Upjohn Co inibidores de proteína de quinase de 2-indolinona de pirrol substituído, seus sais e composições farmacêuticas compreendendo os mesmos
JP2003523390A (ja) 2000-02-25 2003-08-05 メルク エンド カムパニー インコーポレーテッド チロシンキナーゼ阻害薬
US6313138B1 (en) * 2000-02-25 2001-11-06 Merck & Co., Inc. Tyrosine kinase inhibitors
US6420382B2 (en) 2000-02-25 2002-07-16 Merck & Co., Inc. Tyrosine kinase inhibitors
AU2001243431B2 (en) * 2000-03-07 2006-05-25 Rush University 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
ES2334641T3 (es) * 2000-09-01 2010-03-15 Novartis Vaccines And Diagnostics, Inc. Derivados aza heterociclicos y su uso terapeutico.
EP1351946A2 (en) * 2000-09-01 2003-10-15 Icos Corporation Materials and methods to potentiate cancer treatment
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
JP2004536113A (ja) * 2001-07-03 2004-12-02 カイロン コーポレイション チロシンキナーゼおよびセリン/スレオニンキナーゼのインヒビターとしてのインダゾールベンズイミダゾール化合物
WO2003033472A1 (en) * 2001-10-17 2003-04-24 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
CA2496164C (en) * 2002-08-23 2010-11-09 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
EP1545529A4 (en) * 2002-09-30 2010-03-03 Bristol Myers Squibb Co NEW TYROSINE KINASE HEMMER
US7838527B2 (en) * 2002-11-13 2010-11-23 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
EP1680140B1 (en) * 2003-10-16 2011-04-20 Imclone LLC Fibroblast growth factor receptor-1 inhibitors and methods of treatment thereof
KR101224410B1 (ko) * 2003-11-07 2013-01-23 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 퀴놀리논 화합물을 합성하는 방법
RU2377988C2 (ru) * 2004-02-20 2010-01-10 Новартис Вэксинес Энд Дайэгностикс, Инк. Модуляция воспалительных и метастатических процессов
US20060261307A1 (en) * 2005-05-18 2006-11-23 Black D J Water Activated Organic Scavenger

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002022598A1 (en) * 2000-09-11 2002-03-21 Chiron Corporation Quinolinone derivatives as tyrosine kinase inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
William S Dalton et al in Multiple Myeloma, Hematology, American Society of Hematology Educ. Program, 2001, pages 157 - 177 *

Also Published As

Publication number Publication date
AU2004288692A1 (en) 2005-05-26
CA2544492A1 (en) 2005-05-26
CA2543820A1 (en) 2005-05-26
EP1699421B1 (en) 2014-05-21
HK1097444A1 (en) 2007-06-29
CN102225926A (zh) 2011-10-26
CA2544186A1 (en) 2005-05-26
KR20070011241A (ko) 2007-01-24
IL175385A (en) 2012-06-28
US20130018058A1 (en) 2013-01-17
US20050137399A1 (en) 2005-06-23
EP2762475A1 (en) 2014-08-06
EP1699421A2 (en) 2006-09-13
US20130338171A1 (en) 2013-12-19
KR101167573B1 (ko) 2012-07-30
KR101224410B1 (ko) 2013-01-23
EP1682529A2 (en) 2006-07-26
IL174471A0 (en) 2006-08-01
WO2005047244A3 (en) 2006-12-21
US20050209247A1 (en) 2005-09-22
IL174767A0 (en) 2006-08-20
JP4724665B2 (ja) 2011-07-13
US20120277434A1 (en) 2012-11-01
JP2007510665A (ja) 2007-04-26
JP2007522098A (ja) 2007-08-09
CA2544492C (en) 2013-01-29
CA2543820C (en) 2012-07-10
WO2005046589A3 (en) 2007-11-22
AU2004289672A1 (en) 2005-05-26
AU2011202249A1 (en) 2011-06-02
EP1699421A4 (en) 2010-02-17
WO2005046589A2 (en) 2005-05-26
KR20060111520A (ko) 2006-10-27
US20140303182A1 (en) 2014-10-09
JP2007510668A (ja) 2007-04-26
JP4823914B2 (ja) 2011-11-24
EP1682529A4 (en) 2010-06-30
AU2011202249B2 (en) 2013-02-21
IL217114A0 (en) 2012-01-31
JP5214768B2 (ja) 2013-06-19
IL174471A (en) 2013-06-27
IL217114A (en) 2015-04-30
AU2004288709B2 (en) 2011-01-06
EP1692085A2 (en) 2006-08-23
IL175385A0 (en) 2008-04-13
WO2005046590A3 (en) 2005-10-20
WO2005047244A2 (en) 2005-05-26
BRPI0416143A (pt) 2007-01-02
KR20070011231A (ko) 2007-01-24
JP2011162563A (ja) 2011-08-25
EA200600928A1 (ru) 2007-10-26
ES2486240T3 (es) 2014-08-18
MXPA06004194A (es) 2006-06-28
TWI347940B (en) 2011-09-01
IL219818A0 (en) 2012-06-28
TW200526604A (en) 2005-08-16
JP4890255B2 (ja) 2012-03-07
JP2011042687A (ja) 2011-03-03
EA012621B1 (ru) 2009-10-30
AU2004288709A1 (en) 2005-05-26
AU2004289672B2 (en) 2010-06-24
US20090181979A1 (en) 2009-07-16
EP1692085A4 (en) 2010-10-13
WO2005046590A2 (en) 2005-05-26

Similar Documents

Publication Publication Date Title
AU2004289672C1 (en) Inhibition of FGFR3 and treatment of multiple myeloma
US7825132B2 (en) Inhibition of FGFR3 and treatment of multiple myeloma
AU2003288899B2 (en) Benzimidazole quinolinones and uses thereof
US20050256157A1 (en) Combination therapy with CHK1 inhibitors
SK287181B6 (sk) Chinolinónový derivát a jeho použitie a farmaceutický prostriedok s obsahom tohto derivátu
CA2556872A1 (en) Modulation of inflammatory and metastatic processes
ZA200503598B (en) Bicomponent monofilament
CN1976706B (zh) 抑制fgfr3及治疗多发性骨髓瘤
CN100526312C (zh) 苯并咪唑喹啉酮及其应用
HK1085205B (en) Benzimidazole quinolinones and uses thereof

Legal Events

Date Code Title Description
DA2 Applications for amendment section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT(S) FILED 20 JUL 2010.

DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT(S) FILED 20 JUL 2010

FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired