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PE20130239A1 - Compuestos heteroaril-aril-ureas como inhibidores de la quinasa - Google Patents

Compuestos heteroaril-aril-ureas como inhibidores de la quinasa

Info

Publication number
PE20130239A1
PE20130239A1 PE2012002442A PE2012002442A PE20130239A1 PE 20130239 A1 PE20130239 A1 PE 20130239A1 PE 2012002442 A PE2012002442 A PE 2012002442A PE 2012002442 A PE2012002442 A PE 2012002442A PE 20130239 A1 PE20130239 A1 PE 20130239A1
Authority
PE
Peru
Prior art keywords
heteroaryl
aryl
kinase inhibitors
compounds
ureas compounds
Prior art date
Application number
PE2012002442A
Other languages
English (en)
Inventor
Qiang Ding
Bing Li
Yi Liu
Taebo Sim
Tetsuo Uno
Guobao Zhang
Soldermann Carole Pissot
Werner Breitenstein
Guido Bold
Giorgio Caravatti
Pascal Furet
Vito Guagnano
Marc Lang
Paul W Manley
Joseph Schoepfer
Carsten Spanka
Original Assignee
Irm Llc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34855683&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20130239(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Irm Llc, Novartis Ag filed Critical Irm Llc
Publication of PE20130239A1 publication Critical patent/PE20130239A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/26—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
    • C07D251/40—Nitrogen atoms
    • C07D251/48—Two nitrogen atoms
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Reproductive Health (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Cephalosporin Compounds (AREA)

Abstract

SE REFIERE A UNA SAL DE ADICION DE ACIDO FARMACEUTICAMENTE ACEPTABLE DE LOS COMPUESTOS 3-(2,6-DICLORO-3,5-DIMETOXI-FENIL)-1-{6-[4-(4-ETIL-PIPERAZIN-1-IL)-FENILAMINO]-PIRIMIDIN-4-IL}-1-METIL-UREA Y 1-(2,6-DICLORO-3,5-DIMETOXI-FENIL)-3-{6-[4-(4-ETIL-PIPERAZIN-1-IL)-FENILAMINO]-PIRIMIDIN-4-IL}-1-METIL-UREA. SE REFIERE TAMBIEN A COMPOSICIONES FARMACEUTICAS
PE2012002442A 2004-06-24 2005-06-24 Compuestos heteroaril-aril-ureas como inhibidores de la quinasa PE20130239A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US58242504P 2004-06-24 2004-06-24
GBGB0512324.5A GB0512324D0 (en) 2005-06-16 2005-06-16 Organic compounds

Publications (1)

Publication Number Publication Date
PE20130239A1 true PE20130239A1 (es) 2013-03-18

Family

ID=34855683

Family Applications (3)

Application Number Title Priority Date Filing Date
PE2005000736A PE20060479A1 (es) 2004-06-24 2005-06-24 Compuestos heteroaril-aril-ureas como inhibidores de la quinasa
PE2011001630A PE20120252A1 (es) 2004-06-24 2005-06-24 Compuestos heteroaril-aril-ureas como inhibidores de la quinasa
PE2012002442A PE20130239A1 (es) 2004-06-24 2005-06-24 Compuestos heteroaril-aril-ureas como inhibidores de la quinasa

Family Applications Before (2)

Application Number Title Priority Date Filing Date
PE2005000736A PE20060479A1 (es) 2004-06-24 2005-06-24 Compuestos heteroaril-aril-ureas como inhibidores de la quinasa
PE2011001630A PE20120252A1 (es) 2004-06-24 2005-06-24 Compuestos heteroaril-aril-ureas como inhibidores de la quinasa

Country Status (30)

Country Link
US (3) US8552002B2 (es)
EP (3) EP2418205B1 (es)
JP (1) JP4944776B2 (es)
KR (1) KR101238591B1 (es)
CN (3) CN101035769A (es)
AR (1) AR050343A1 (es)
AT (1) ATE520671T1 (es)
AU (2) AU2005256491C1 (es)
BR (1) BRPI0512588B1 (es)
CA (1) CA2570873C (es)
DK (1) DK1761505T3 (es)
EC (1) ECSP067076A (es)
ES (1) ES2432646T3 (es)
GB (1) GB0512324D0 (es)
HR (1) HRP20110822T1 (es)
IL (1) IL179743A0 (es)
MA (1) MA28695B1 (es)
MX (1) MXPA06014746A (es)
MY (1) MY144655A (es)
NO (1) NO338287B1 (es)
NZ (1) NZ551438A (es)
PE (3) PE20060479A1 (es)
PL (1) PL1761505T3 (es)
PT (1) PT1761505E (es)
RU (1) RU2430093C2 (es)
SG (1) SG153875A1 (es)
SI (1) SI1761505T1 (es)
TN (1) TNSN06411A1 (es)
TW (1) TWI361187B (es)
WO (1) WO2006000420A1 (es)

Families Citing this family (185)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0512324D0 (en) * 2005-06-16 2005-07-27 Novartis Ag Organic compounds
JP4641839B2 (ja) * 2005-03-23 2011-03-02 セントラル硝子株式会社 ４−メチル−３−トリフルオロメチル安息香酸の製造方法
GT200600197A (es) * 2005-05-13 2007-03-28 Compuestos y composiciones como inhibidores de proteina quinasa
US20070049592A1 (en) * 2005-08-22 2007-03-01 Geuns-Meyer Stephanie D Bis-aryl urea compounds and methods of use
BRPI0620408B8 (pt) 2005-12-21 2021-05-25 Novartis Ag derivados de pirimidinil aril uréia sendo inibidores de fgf, seus usos, e preparação farmacêutica
JP2009532449A (ja) * 2006-04-05 2009-09-10 アストラゼネカ アクチボラグ 抗癌活性のある置換キナゾリン
US7722898B2 (en) * 2006-04-26 2010-05-25 Supernus Pharmaceuticals, Inc. Modified-release preparations containing oxcarbazepine and derivatives thereof
EP1882475A1 (en) * 2006-07-26 2008-01-30 Novartis AG Method of treating disorders mediated by the fibroblast growth factor receptor
CA2672213C (en) 2006-12-22 2016-02-16 Astex Therapeutics Limited Bicyclic amine derivatives as protein tyrosine kinase inhibitors
US8131527B1 (en) 2006-12-22 2012-03-06 Astex Therapeutics Ltd. FGFR pharmacophore compounds
MX2009006706A (es) 2006-12-22 2009-07-02 Astex Therapeutics Ltd Compuestos heterociclicos biciclicos como inhibidores del receptor del factor de crecimiento de fibroblastos.
AU2007345526B2 (en) 2007-02-01 2013-02-28 Resverlogix Corp. Compounds for the prevention and treatment of cardiovascular diseases
GB0720038D0 (en) 2007-10-12 2007-11-21 Astex Therapeutics Ltd New compounds
GB0720041D0 (en) 2007-10-12 2007-11-21 Astex Therapeutics Ltd New Compounds
KR101660544B1 (ko) * 2008-04-29 2016-09-27 노파르티스 아게 섬유모세포 성장 인자 수용체의 키나제 활성에 대한 조정을 모니터링하는 방법 및 상기 방법의 용도
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
EA029131B1 (ru) 2008-05-21 2018-02-28 Ариад Фармасьютикалз, Инк. Фосфорсодержащие производные в качестве ингибиторов киназы
EA020317B1 (ru) * 2008-05-23 2014-10-30 УАЙТ ЭлЭлСи ТРИАЗИНЫ КАК ИНГИБИТОРЫ КИНАЗЫ PI3 И mTOR
GB0810902D0 (en) 2008-06-13 2008-07-23 Astex Therapeutics Ltd New compounds
CA2952692C (en) 2008-09-22 2020-04-28 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds
HRP20140265T1 (hr) * 2009-02-06 2014-04-25 Nippon Shinyaku Co., Ltd. Derivat aminopirazina i odgovarajuä†i lijek
MX392179B (es) 2009-03-18 2025-03-21 Resverlogix Corp Nuevos agentes anti-inflamatorios.
GB0906472D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
GB0906470D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
TR201818390T4 (tr) 2009-04-22 2019-01-21 Resverlogix Corp Yeni̇ anti̇-i̇nflamatuvar ajanlar
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
AU2010313152A1 (en) * 2009-10-30 2012-04-19 Ariad Pharmaceuticals, Inc. Methods and compositions for treating cancer
CN102596916B (zh) * 2009-10-30 2015-06-17 诺瓦提斯公司 3-(2,6-二氯-3,5-二甲氧基-苯基)-1-{6-[4-(4-乙基-哌嗪-1-基)-苯基氨基]-嘧啶-4-基}-1-甲基-脲的n-氧化物
AR079257A1 (es) * 2009-12-07 2012-01-04 Novartis Ag Formas cristalinas de 3-(2,6-dicloro-3-5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperazin-1-il)-fenil-amino]-pirimidin-4-il}-1-metil-urea y sales de las mismas
WO2011075620A1 (en) 2009-12-18 2011-06-23 Novartis Ag Method for treating haematological cancers
AT509266B1 (de) * 2009-12-28 2014-07-15 Univ Wien Tech Substituierte pyridine und pyrimidine
JPWO2012005299A1 (ja) * 2010-07-07 2013-09-05 日本新薬株式会社 Ｒｏｓチロシンキナーゼ阻害剤
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
CZ305457B6 (cs) 2011-02-28 2015-09-30 Ústav organické chemie a biochemie, Akademie věd ČR v. v. i. Pyrimidinové sloučeniny inhibující tvorbu oxidu dusnatého a prostaglandinu E2, způsob výroby a použití
CA2832504C (en) 2011-05-04 2019-10-01 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
CN102250065B (zh) * 2011-05-20 2015-05-13 浙江海正药业股份有限公司 取代的三嗪苯脲衍生物及其用途
KR20140040769A (ko) * 2011-07-01 2014-04-03 노파르티스 아게 조합 요법
EP2755944B1 (en) 2011-09-16 2017-06-14 Sanofi Biarylderivatives,their preparation and their therapeutic application
AT511441B1 (de) 2011-09-21 2012-12-15 Univ Wien Tech Triazin-derivate als differenzierungsbeschleuniger
JP2014532647A (ja) 2011-10-28 2014-12-08 ノバルティス アーゲー 消化管間質腫瘍を治療する方法
WO2013063003A1 (en) 2011-10-28 2013-05-02 Novartis Ag Method of treating gastrointestinal stromal tumors
AR089489A1 (es) 2011-12-30 2014-08-27 27 Derivados de tieno[3,2-d]pirimidina que tienen actividad inhibidora por las quinasas de las proteinas
GB201204384D0 (en) 2012-03-13 2012-04-25 Univ Dundee Anti-flammatory agents
WO2013144339A1 (en) * 2012-03-30 2013-10-03 Novartis Ag Fgfr inhibitor for use in the treatment of hypophosphatemic disorders
US20150051210A1 (en) 2012-04-03 2015-02-19 Novartis Ag Tyrosine Kinase Inhibitor Combinations and their Use
AU2013204563B2 (en) 2012-05-05 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
US9254288B2 (en) * 2012-05-07 2016-02-09 The Translational Genomics Research Institute Susceptibility of tumors to tyrosine kinase inhibitors and treatment thereof
CN107652289B (zh) 2012-06-13 2020-07-21 因塞特控股公司 作为fgfr抑制剂的取代的三环化合物
JP2015522070A (ja) 2012-07-11 2015-08-03 ノバルティス アーゲー 消化管間質腫瘍を治療する方法
EP2880448B1 (en) 2012-08-03 2022-06-29 Foundation Medicine, Inc. Human papilloma virus as predictor of cancer prognosis
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
CN104884427B (zh) * 2012-10-15 2016-09-07 雷斯韦洛吉克斯公司 可用于合成苯甲酰胺化合物的化合物
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
WO2014138364A2 (en) 2013-03-06 2014-09-12 Genentech, Inc. Methods of treating and preventing cancer drug resistance
TWI647220B (zh) 2013-03-15 2019-01-11 美商西建卡爾有限責任公司 雜芳基化合物及其用途
CN111793068A (zh) 2013-03-15 2020-10-20 西建卡尔有限责任公司 杂芳基化合物和其用途
KR102350704B1 (ko) 2013-03-15 2022-01-13 셀젠 카르 엘엘씨 헤테로아릴 화합물 및 이의 용도
WO2014147573A2 (en) * 2013-03-21 2014-09-25 Novartis Ag Combination therapy
WO2014155268A2 (en) 2013-03-25 2014-10-02 Novartis Ag Fgf-r tyrosine kinase activity inhibitors - use in diseases associated with lack of or reduced snf5 activity
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
KR102269032B1 (ko) 2013-04-19 2021-06-24 인사이트 홀딩스 코포레이션 Fgfr 저해제로서 이환식 헤테로사이클
EP3003377A1 (en) 2013-05-31 2016-04-13 Novartis AG Combination therapy containing a pi3k-alpha inhibitor and fgfr kinase inhibitor for treating cancer
CA2917667A1 (en) * 2013-07-09 2015-01-15 Dana-Farber Cancer Institute, Inc. Kinase inhibitors for the treatment of disease
WO2015048312A1 (en) 2013-09-26 2015-04-02 Costim Pharmaceuticals Inc. Methods for treating hematologic cancers
KR101826015B1 (ko) * 2013-10-18 2018-02-06 에자이 알앤드디 매니지먼트 가부시키가이샤 피리미딘 fgfr4 억제제
SI3079667T1 (sl) * 2013-12-13 2019-10-30 Novartis Ag Farmacevtske dozirne oblike
JOP20200094A1 (ar) 2014-01-24 2017-06-16 Dana Farber Cancer Inst Inc جزيئات جسم مضاد لـ pd-1 واستخداماتها
JOP20200096A1 (ar) 2014-01-31 2017-06-16 Children’S Medical Center Corp جزيئات جسم مضاد لـ tim-3 واستخداماتها
CN104860891B (zh) * 2014-02-25 2017-06-30 上海海雁医药科技有限公司 芳氨基嘧啶类化合物及其应用以及由其制备的药物组合物和药用组合物
LT3116909T (lt) 2014-03-14 2020-02-10 Novartis Ag Antikūno molekulės prieš lag-3 ir jų panaudojimas
US20230190750A1 (en) 2014-06-13 2023-06-22 Genentech, Inc. Methods of treating and preventing cancer drug resistance
US9782727B2 (en) 2014-07-14 2017-10-10 International Business Machines Corporation Filtration membranes with functionalized star polymers
US10287268B2 (en) 2014-07-21 2019-05-14 Dana-Farber Cancer Institute, Inc. Imidazolyl kinase inhibitors and uses thereof
US10457691B2 (en) 2014-07-21 2019-10-29 Dana-Farber Cancer Institute, Inc. Macrocyclic kinase inhibitors and uses thereof
EP3177295A4 (en) * 2014-08-08 2018-06-13 Dana Farber Cancer Institute, Inc. Uses of salt-inducible kinase (sik) inhibitors
ES2914072T3 (es) 2014-08-18 2022-06-07 Eisai R&D Man Co Ltd Sal de derivado de piridina monocíclico y su cristal
CA2960824A1 (en) 2014-09-13 2016-03-17 Novartis Ag Combination therapies of alk inhibitors
WO2016048833A2 (en) 2014-09-26 2016-03-31 Janssen Pharmaceutica Nv Use of fgfr mutant gene panels in identifying cancer patients that will be responsive to treatment with an fgfr inhibitor
ES2774448T3 (es) 2014-10-03 2020-07-21 Novartis Ag Terapias de combinación
US20170304313A1 (en) 2014-10-06 2017-10-26 Novartis Ag Therapeutic Combination For The Treatment Of Cancer
MA41044A (fr) 2014-10-08 2017-08-15 Novartis Ag Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer
JP6877339B2 (ja) 2014-10-14 2021-05-26 ノバルティス アーゲー Ｐｄ−ｌ１に対する抗体分子およびその使用
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US9931598B2 (en) 2015-02-16 2018-04-03 International Business Machines Corporation Anti-fouling coatings with star polymers for filtration membranes
PE20171514A1 (es) 2015-02-20 2017-10-20 Incyte Corp Heterociclos biciclicos como inhibidores de fgfr
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
CN107530304A (zh) * 2015-02-27 2018-01-02 科泰纳制药公司 Olig2活性的抑制
JP6692826B2 (ja) 2015-03-10 2020-05-13 アドゥロ バイオテック，インク． 「インターフェロン遺伝子刺激因子」依存性シグナル伝達の活性化のための組成物及び方法
KR102662814B1 (ko) 2015-03-13 2024-05-03 리스버로직스 코퍼레이션 보체 관련 질환을 치료하기 위한 조성물 및 치료 방법
JP6503450B2 (ja) 2015-03-25 2019-04-17 国立研究開発法人国立がん研究センター 胆管癌治療剤
KR20170129757A (ko) 2015-03-25 2017-11-27 노파르티스 아게 Fgfr4 억제제로서의 포르밀화 n-헤테로시클릭 유도체
US10130629B2 (en) 2015-03-25 2018-11-20 Novartis Ag Pharmaceutical combinations
CN107660200B (zh) * 2015-04-14 2022-01-11 卫材R&D管理有限公司 结晶fgfr4抑制剂化合物和其用途
WO2016189472A1 (en) 2015-05-28 2016-12-01 Novartis Ag Fgfr inhibitor for use in the treatment of the phosphaturic mesenchymal tumor
SI3322706T1 (sl) 2015-07-16 2021-04-30 Array Biopharma, Inc. Substituirane pirazolo(1,5-A)piridinske spojine kot zaviralci ret-kinaze
JP2018527321A (ja) * 2015-07-20 2018-09-20 タイペイ・メディカル・ユニバーシティＴａｉｐｅｉ Ｍｅｄｉｃａｌ Ｕｎｉｖｅｒｓｉｔｙ クロロベンゼン置換されたアザアリール化合物
WO2017019896A1 (en) 2015-07-29 2017-02-02 Novartis Ag Combination therapies comprising antibody molecules to pd-1
EP3878465A1 (en) 2015-07-29 2021-09-15 Novartis AG Combination therapies comprising antibody molecules to tim-3
EP3964528A1 (en) 2015-07-29 2022-03-09 Novartis AG Combination therapies comprising antibody molecules to lag-3
JP6549311B2 (ja) 2015-08-20 2019-07-24 浙江海正薬業股▲ふん▼有限公司Ｚｈｅｊｉａｎｇ Ｈｉｓｕｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌ ＣＯ．，ＬＴＤ． インドール誘導体、その調製方法および医薬におけるその使用
CA3003153A1 (en) 2015-10-26 2017-05-04 Loxo Oncology, Inc. Point mutations in trk inhibitor-resistant cancer and methods relating to the same
LT3370768T (lt) 2015-11-03 2022-05-25 Janssen Biotech, Inc. Antikūnai, specifiškai surišantys pd-1, ir jų panaudojimas
EP4424322A3 (en) 2015-12-17 2025-04-16 Novartis AG Antibody molecules to pd-1 and uses thereof
MX384034B (es) 2015-12-17 2025-03-14 Eisai R&D Man Co Ltd Agente terapeutico para cancer de mama.
CN109195593A (zh) 2016-03-15 2019-01-11 奥莱松基因组股份有限公司 用于治疗实体瘤的lsd1抑制剂的组合
PH12018502124B1 (en) 2016-04-04 2024-04-12 Loxo Oncology Inc Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
JP7057343B2 (ja) 2016-04-04 2022-04-19 ロクソ オンコロジー， インコーポレイテッド 小児癌の処置方法
US11357769B2 (en) 2016-05-10 2022-06-14 Eisai R&D Management Co., Ltd. Drug combinations for reducing cell viability and/or cell proliferation
PT3458456T (pt) 2016-05-18 2020-12-07 Array Biopharma Inc Preparação de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidino-1-carboxamida
EP3459952B1 (en) * 2016-05-20 2022-01-05 Zhejiang Hisun Pharmaceutical Co., Ltd. Pyrimidine derivative, method for preparing same and use thereof in medicine
CN107459519A (zh) 2016-06-06 2017-12-12 上海艾力斯医药科技有限公司 稠合嘧啶哌啶环衍生物及其制备方法和应用
WO2018009466A1 (en) 2016-07-05 2018-01-11 Aduro Biotech, Inc. Locked nucleic acid cyclic dinucleotide compounds and uses thereof
CN110225914A (zh) 2016-07-05 2019-09-10 布罗德研究所股份有限公司 双环脲激酶抑制剂及其用途
CN107619388A (zh) * 2016-07-13 2018-01-23 南京天印健华医药科技有限公司 作为fgfr抑制剂的杂环化合物
WO2018053373A1 (en) 2016-09-16 2018-03-22 The General Hospital Corporation Uses of satl-inducible kinase (sik) inhibitors for treating osteoporosis
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
CN108239069B (zh) * 2016-12-26 2021-01-05 南京药捷安康生物科技有限公司 一种用于成纤维细胞生长因子受体的抑制剂及其用途
AU2018206372B2 (en) 2017-01-06 2020-10-08 Lemonex Inc. Composition for preventing or treating metastatic ovarian cancer, endometrial cancer or breast cancer
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
CA3049136C (en) 2017-01-18 2022-06-14 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors
BR112019017741A2 (pt) 2017-02-28 2020-04-07 Dana Farber Cancer Inst Inc usos de pirimidopirimidinonas como inibidores de sik
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
JP2020517618A (ja) 2017-04-21 2020-06-18 エピザイム，インコーポレイティド Ｅｈｍｔ２阻害剤との併用療法
UY37695A (es) 2017-04-28 2018-11-30 Novartis Ag Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
JOP20190280A1 (ar) 2017-06-02 2019-12-02 Janssen Pharmaceutica Nv مثبطات fgfr2 لعلاج سرطان الأوعية الصفراوية
EP3642240A1 (en) 2017-06-22 2020-04-29 Novartis AG Antibody molecules to cd73 and uses thereof
JP7202350B2 (ja) * 2017-07-13 2023-01-11 サンシャイン・レイク・ファーマ・カンパニー・リミテッド 置換尿素誘導体の塩及び薬におけるその使用
US11236094B2 (en) 2017-08-15 2022-02-01 Cspc Zhongqi Pharmaceuticall Technology (Shijiazhuang) Co., Ltd. Substituted pyrrolo[2,1-f][1,2,4]triazines as FGFR inhibitors
CN109467538A (zh) * 2017-09-07 2019-03-15 和记黄埔医药（上海）有限公司 环烯烃取代的杂芳环类化合物及其用途
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
TWI876442B (zh) 2017-10-10 2025-03-11 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
JP6997876B2 (ja) 2018-01-18 2022-02-04 アレイ バイオファーマ インコーポレイテッド Ｒｅｔキナーゼ阻害剤としての置換ピラゾリル［４，３－ｃ］ピリジン化合物
US11524963B2 (en) 2018-01-18 2022-12-13 Array Biopharma Inc. Substituted pyrazolo[3,4-d]pyrimidines as RET kinase inhibitors
EP3740491A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
US12398209B2 (en) 2018-01-22 2025-08-26 Janssen Biotech, Inc. Methods of treating cancers with antagonistic anti-PD-1 antibodies
BR112020017922A2 (pt) 2018-03-28 2020-12-22 Eisai R&D Management Co., Ltd. Agente terapêutico para carcinoma hepatocelular
SG11202010636VA (en) 2018-05-04 2020-11-27 Incyte Corp Solid forms of an fgfr inhibitor and processes for preparing the same
BR112020022373A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation sais de um inibidor de fgfr
TWI869346B (zh) 2018-05-30 2025-01-11 瑞士商諾華公司 Ｅｎｔｐｄ２抗體、組合療法、及使用該等抗體和組合療法之方法
US12109193B2 (en) 2018-07-31 2024-10-08 Loxo Oncology Inc. Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1H-pyrazole-4-carboxamide
CN109053592B (zh) * 2018-08-07 2020-12-04 温州医科大学 1-(2,5-二甲氧基苯基)-3-(取代嘧啶-4-基)脲类化合物及其制备和应用
CN109053593B (zh) * 2018-08-07 2020-12-04 温州医科大学 1-(2,6-氯苯基)-3-(取代嘧啶-4-基)脲类化合物及其制备和应用
CN109053594B (zh) * 2018-08-07 2020-12-18 温州医科大学 1-(3,5-二甲氧基苯基)-3-(取代嘧啶-4-基)脲类化合物及其制备和应用
ES2922314T3 (es) 2018-09-10 2022-09-13 Array Biopharma Inc Compuestos heterocíclicos condensados como inhibidores de cinasa RET
CA3111866A1 (en) 2018-09-21 2020-03-26 Janssen Pharmaceutica Nv Treatment of cholangiocarcinoma
US12351571B2 (en) 2018-12-19 2025-07-08 Array Biopharma Inc. Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases
JP2022515198A (ja) 2018-12-19 2022-02-17 アレイ バイオファーマ インコーポレイテッド ＦＧＦＲチロシンキナーゼの阻害剤としての置換ピラゾロ［１，５－ａ］ピリジン化合物
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
WO2020205493A1 (en) 2019-03-29 2020-10-08 Janssen Pharmaceutica Nv Fgfr tyrosine kinase inhibitors for the treatment of urothelial carcinoma
WO2020201138A1 (en) 2019-03-29 2020-10-08 Janssen Pharmaceutica Nv Fgfr tyrosine kinase inhibitors for the treatment of urothelial carcinoma
CN114127057B (zh) 2019-05-10 2024-07-12 德西费拉制药有限责任公司 苯基氨基嘧啶酰胺自噬抑制剂及其使用方法
EP4295846A3 (en) 2019-05-10 2024-02-28 Deciphera Pharmaceuticals, LLC Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
US11590134B2 (en) 2019-06-17 2023-02-28 Deciphera Pharmaceuticals, Llc Aminopyrimidine amide autophagy inhibitors and methods of use thereof
CN110283130B (zh) * 2019-07-05 2023-12-19 温州医科大学 一种1-(2,5-二甲氧基苯基)-3-取代脲类结肠癌抑制剂及其制备和应用
CN110396066B (zh) * 2019-07-05 2023-12-19 温州医科大学 一种1-(3,5-二甲氧基苯基)-3-取代脲类结肠癌抑制剂及其制备和应用
CN110563657B (zh) * 2019-07-05 2024-05-03 温州医科大学 一种1-(2,6-二氯苯基)-3-取代脲类结肠癌抑制剂及其制备和应用
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN114502590A (zh) 2019-09-18 2022-05-13 诺华股份有限公司 Entpd2抗体、组合疗法、以及使用这些抗体和组合疗法的方法
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076602A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN115151539A (zh) 2019-12-04 2022-10-04 因赛特公司 Fgfr抑制剂的衍生物
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
KR20220123023A (ko) 2019-12-27 2022-09-05 슈뢰딩거, 인크. 시클릭 화합물 및 이의 사용 방법
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
TWI900527B (zh) 2020-02-12 2025-10-11 比利時商健生藥品公司 用於治療尿路上皮癌的ｆｇｆｒ酪胺酸激酶抑制劑和抗ｐｄ１藥劑
US20230110113A1 (en) 2020-02-12 2023-04-13 Janssen Pharmaceutica Nv Fgfr tyrosine kinase inhibitors for the treatment of high-risk non-muscle invasive bladder cancer
WO2022055963A1 (en) 2020-09-10 2022-03-17 Schrödinger, Inc. Heterocyclic pericondensed cdc7 kinase inhibitors for the treatment of cancer
JP2023542296A (ja) 2020-09-14 2023-10-06 ヤンセン ファーマシューティカ エヌ．ベー． Ｆｇｆｒ阻害剤の併用療法
US20240148732A1 (en) 2021-01-26 2024-05-09 Schrödinger, Inc. Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders
TW202300150A (zh) 2021-03-18 2023-01-01 美商薛定諤公司 環狀化合物及其使用方法
US12065494B2 (en) 2021-04-12 2024-08-20 Incyte Corporation Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent
IL298474A (en) 2021-05-17 2023-01-01 Voronoibio Inc Compounds of heteroaryl derivatives and uses thereof
MX2023013802A (es) 2021-05-19 2023-12-06 Janssen Pharmaceutica Nv Inhibidores de tirosina quinasa de fgfr para el tratamiento de tumores solidos avanzados.
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN115785001B (zh) * 2022-11-23 2023-09-15 斯坦德药典标准物质研发(湖北)有限公司 一种英菲格拉替尼的制备方法
IL322665A (en) 2023-02-13 2025-10-01 Janssen Pharmaceutica Nv FGFR tyrosine kinase inhibitors for the treatment of high-risk non-muscle invasive bladder cancer
WO2025059027A1 (en) 2023-09-11 2025-03-20 Schrödinger, Inc. Cyclopenta[e]pyrazolo[1,5-a]pyrimidine derivatives as malt1 inhibitors

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3759921A (en) 1969-10-16 1973-09-18 Lilly Co Eli Method of suppressing immuneresponse with 1 substituted-3-(2 pyrimidyl)ureas
CA961855A (en) * 1969-10-16 1975-01-28 Eli Lilly And Company Immunosuppressants and anti-viral agents
GB1524747A (en) 1976-05-11 1978-09-13 Ici Ltd Polypeptide
EP0100172B1 (en) 1982-07-23 1987-08-12 Imperial Chemical Industries Plc Amide derivatives
GB8327256D0 (en) 1983-10-12 1983-11-16 Ici Plc Steroid derivatives
IL86632A0 (en) 1987-06-15 1988-11-30 Ciba Geigy Ag Derivatives substituted at methyl-amino nitrogen
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
TW225528B (es) 1992-04-03 1994-06-21 Ciba Geigy Ag
DE69233803D1 (de) 1992-10-28 2011-03-31 Genentech Inc Verwendung von vaskulären Endothelwachstumsfaktor-Antagonisten
NZ264063A (en) * 1993-08-13 1995-11-27 Nihon Nohyaku Co Ltd N-(2-phenylpyrid-3-yl)- and n-(4-phenylpyrimidin-5-yl)-n'-phenylurea derivatives and pharmaceutical compositions
CN1046731C (zh) 1994-09-29 1999-11-24 诺瓦蒂斯有限公司 吡咯并[2,3-d]嘧啶类化合物及其应用
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5843901A (en) 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
TR199800012T1 (xx) 1995-07-06 1998-04-21 Novartis Ag Piroloprimidinler ve preparasyon i�in tatbikler.
GB9517060D0 (en) 1995-08-17 1995-10-25 Ciba Geigy Ag Acylated oligopeptide derivatives
GB9516842D0 (en) 1995-08-17 1995-10-18 Ciba Geigy Ag Various acylated oligopeptides
CH690773A5 (de) 1996-02-01 2001-01-15 Novartis Ag Pyrrolo(2,3-d)pyrimide und ihre Verwendung.
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
AU1794697A (en) 1996-03-06 1997-09-22 Novartis Ag 7-alkyl-pyrrolo{2,3-d}pyrimidines
DE69710712T3 (de) 1996-04-12 2010-12-23 Warner-Lambert Co. Llc Umkehrbare inhibitoren von tyrosin kinasen
CA2258548C (en) 1996-06-24 2005-07-26 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
AU3176297A (en) 1996-06-25 1998-01-14 Novartis Ag Substituted 7-amino-pyrrolo{3,2-d}pyrimidines and the use thereof
DE19638745C2 (de) 1996-09-11 2001-05-10 Schering Ag Monoklonale Antikörper gegen die extrazelluläre Domäne des menschlichen VEGF - Rezeptorproteins (KDR)
AU4342997A (en) 1996-09-13 1998-04-02 Sugen, Inc. Use of quinazoline derivatives for the manufacture of a medicament in the reatment of hyperproliferative skin disorders
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
CO4940418A1 (es) 1997-07-18 2000-07-24 Novartis Ag Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso
GB9721069D0 (en) 1997-10-03 1997-12-03 Pharmacia & Upjohn Spa Polymeric derivatives of camptothecin
ES2342240T3 (es) 1998-08-11 2010-07-02 Novartis Ag Derivados de isoquinolina con actividad que inhibe la angiogenia.
GB9824579D0 (en) 1998-11-10 1999-01-06 Novartis Ag Organic compounds
UA71587C2 (uk) 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Аміди антранілової кислоти та їхнє застосування як лікарських засобів
US20030087854A1 (en) 2001-09-10 2003-05-08 Isis Pharmaceuticals Inc. Antisense modulation of fibroblast growth factor receptor 3 expression
EP1140173B2 (en) 1998-12-22 2013-04-03 Genentech, Inc. Vascular endothelial cell growth factor antagonists and uses thereof
GB9903547D0 (en) 1999-02-16 1999-04-07 Novartis Ag Organic compounds
DE60028740T2 (de) 1999-03-30 2007-05-24 Novartis Ag Phthalazinderivate zur behandlung von entzündlichen erkrankungen
AU770600B2 (en) * 1999-10-07 2004-02-26 Amgen, Inc. Triazine kinase inhibitors
GB0001930D0 (en) 2000-01-27 2000-03-22 Novartis Ag Organic compounds
ES2241781T3 (es) 2000-02-09 2005-11-01 Novartis Ag Derivados de piridina inhibidores de la angiogenesis y/o del receptor tirosina quinasa de vegf.
UA76977C2 (en) 2001-03-02 2006-10-16 Icos Corp Aryl- and heteroaryl substituted chk1 inhibitors and their use as radiosensitizers and chemosensitizers
AU2002329540A1 (en) 2001-06-20 2003-01-02 Morphosys Ag Antibodies that block receptor protein tyrosine kinase activation, methods of screening for and uses thereof
PT1478358E (pt) 2002-02-11 2013-09-11 Bayer Healthcare Llc Tosilato de sorafenib para o tratamento de doenças caracterizadas por angiogénese anormal
PE20040522A1 (es) * 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
AU2003243318A1 (en) 2002-05-29 2003-12-19 Millennium Pharmaceuticals, Inc. Diarylurea compounds and derivatives as chk-1 inhibitors for the treatment of cancer
US20040034038A1 (en) 2002-08-13 2004-02-19 Goaquan Li Urea kinase inhibitors
WO2004058713A1 (en) * 2002-12-20 2004-07-15 Irm Llc Differential tumor cytotoxocity compounds and compositions
US8124331B2 (en) 2003-03-26 2012-02-28 Progenika Biopharma, S.A. In vitro method to detect bladder transitional cell carcinoma
DK1636585T3 (da) 2003-05-20 2008-05-26 Bayer Pharmaceuticals Corp Diarylurinstoffer med kinasehæmmende aktivitet
IL156495A0 (en) 2003-06-17 2004-01-04 Prochon Biotech Ltd Use of fgfr3 antagonists for treating t cell mediated diseases
WO2005030735A1 (en) 2003-09-25 2005-04-07 Ranbaxy Laboratories Limited Triazines derivatives as cell adhesion inhibitors
RU2006122853A (ru) * 2003-11-28 2008-01-10 Новартис АГ (CH) Производные диарилмочевины для лечения заболеваний, зависимых от протеинкиназы
RU2006131045A (ru) 2004-01-30 2008-03-10 Мерк Патент ГмбХ (DE) Производные бисарилмочевины
MXPA06013338A (es) * 2004-05-20 2007-02-22 Sugen Inc Tiofen-heteroaril-aminas.
UY28931A1 (es) 2004-06-03 2005-12-30 Bayer Pharmaceuticals Corp Derivados de pirrolotriazina utiles para tratar trastornos hiper-proliferativos y enfermedades asociadas con angiogenesis
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
WO2006049941A2 (en) 2004-10-27 2006-05-11 Neurogen Corporation Diaryl ureas as cb1 antagonists
TW200628159A (en) 2004-11-10 2006-08-16 Synta Pharmaceuticals Corp IL-12 modulatory compounds
US20070032493A1 (en) 2005-05-26 2007-02-08 Synta Pharmaceuticals Corp. Method for treating B cell regulated autoimmune disorders
WO2006128129A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating cancer
US20070049592A1 (en) 2005-08-22 2007-03-01 Geuns-Meyer Stephanie D Bis-aryl urea compounds and methods of use
BRPI0620408B8 (pt) 2005-12-21 2021-05-25 Novartis Ag derivados de pirimidinil aril uréia sendo inibidores de fgf, seus usos, e preparação farmacêutica
US20090062320A1 (en) 2007-08-28 2009-03-05 Vito Guagnano Method of Treating Disorders Mediated by the Fibroblast Growth Factor Receptor
CN102596916B (zh) 2009-10-30 2015-06-17 诺瓦提斯公司 3-(2,6-二氯-3,5-二甲氧基-苯基)-1-{6-[4-(4-乙基-哌嗪-1-基)-苯基氨基]-嘧啶-4-基}-1-甲基-脲的n-氧化物
AR079257A1 (es) 2009-12-07 2012-01-04 Novartis Ag Formas cristalinas de 3-(2,6-dicloro-3-5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperazin-1-il)-fenil-amino]-pirimidin-4-il}-1-metil-urea y sales de las mismas
WO2011075620A1 (en) 2009-12-18 2011-06-23 Novartis Ag Method for treating haematological cancers

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