HRP20140799T1 - Spojevi i sastavi kao inhibitori kinaze proteina - Google Patents

Spojevi i sastavi kao inhibitori kinaze proteina Download PDF

Info

Publication number
HRP20140799T1
HRP20140799T1 HRP20140799AT HRP20140799T HRP20140799T1 HR P20140799 T1 HRP20140799 T1 HR P20140799T1 HR P20140799A T HRP20140799A T HR P20140799AT HR P20140799 T HRP20140799 T HR P20140799T HR P20140799 T1 HRP20140799 T1 HR P20140799T1
Authority
HR
Croatia
Prior art keywords
propan
pyrimidin
amino
carbamate
methyl
Prior art date
Application number
HRP20140799AT
Other languages
English (en)
Croatian (hr)
Inventor
Shenlin Huang
Xianming Jin
Zuosheng Liu
Daniel Poon
John Tellew
Yongqin Wan
Xing Wang
Yongping Xie
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=42782253&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20140799(T1) "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 HRP20140799T1 publication Critical patent/HRP20140799T1/hr

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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 three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Hospice & Palliative Care (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Otolaryngology (AREA)
  • Psychiatry (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
HRP20140799AT 2009-08-28 2010-08-27 Spojevi i sastavi kao inhibitori kinaze proteina HRP20140799T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US23807309P 2009-08-28 2009-08-28
US31303910P 2010-03-11 2010-03-11
PCT/US2010/046930 WO2011025927A1 (en) 2009-08-28 2010-08-27 Compounds and compositions as protein kinase inhibitors

Publications (1)

Publication Number Publication Date
HRP20140799T1 true HRP20140799T1 (hr) 2014-11-07

Family

ID=42782253

Family Applications (2)

Application Number Title Priority Date Filing Date
HRP20140799AT HRP20140799T1 (hr) 2009-08-28 2010-08-27 Spojevi i sastavi kao inhibitori kinaze proteina
HRP20170005TT HRP20170005T1 (hr) 2009-08-28 2017-01-03 Spojevi i sastavi kao inhibitori kinaze proteina

Family Applications After (1)

Application Number Title Priority Date Filing Date
HRP20170005TT HRP20170005T1 (hr) 2009-08-28 2017-01-03 Spojevi i sastavi kao inhibitori kinaze proteina

Country Status (49)

Country Link
US (12) US8501758B2 (enExample)
EP (2) EP2727918B1 (enExample)
JP (2) JP5475888B2 (enExample)
KR (1) KR101413392B1 (enExample)
CN (2) CN103896921B (enExample)
AR (1) AR077975A1 (enExample)
AU (1) AU2010286569C1 (enExample)
BR (1) BR112012004453B1 (enExample)
CA (1) CA2771775C (enExample)
CL (1) CL2012000340A1 (enExample)
CO (1) CO6612222A2 (enExample)
CR (1) CR20120102A (enExample)
CU (1) CU24110B1 (enExample)
CY (3) CY1118452T1 (enExample)
DK (2) DK2470526T3 (enExample)
DO (1) DOP2012000051A (enExample)
EA (2) EA201500175A1 (enExample)
EC (2) ECSP12011700A (enExample)
ES (2) ES2610825T3 (enExample)
GE (1) GEP20146102B (enExample)
GT (1) GT201200053A (enExample)
HN (1) HN2012000441A (enExample)
HR (2) HRP20140799T1 (enExample)
HU (3) HUE032847T2 (enExample)
IL (1) IL218084A (enExample)
IN (1) IN2012DN02469A (enExample)
JO (1) JO3002B1 (enExample)
LT (3) LT2727918T (enExample)
LU (2) LUC00101I2 (enExample)
MA (1) MA33604B1 (enExample)
ME (2) ME01860B (enExample)
MX (1) MX2012002546A (enExample)
MY (1) MY156259A (enExample)
NI (1) NI201200029A (enExample)
NL (1) NL300973I2 (enExample)
NO (2) NO2019011I1 (enExample)
NZ (1) NZ598924A (enExample)
PE (1) PE20120861A1 (enExample)
PL (2) PL2727918T3 (enExample)
PT (2) PT2470526E (enExample)
RS (2) RS55568B1 (enExample)
SG (2) SG10201405311TA (enExample)
SI (2) SI2727918T1 (enExample)
SM (3) SMT201700036T1 (enExample)
TN (1) TN2012000081A1 (enExample)
UA (1) UA112285C2 (enExample)
UY (1) UY32860A (enExample)
WO (1) WO2011025927A1 (enExample)
ZA (1) ZA201202020B (enExample)

Families Citing this family (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR077975A1 (es) 2009-08-28 2011-10-05 Irm Llc Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina
ES2576061T3 (es) 2010-02-25 2016-07-05 Dana-Farber Cancer Institute, Inc. Mutaciones de BRAF que confieren resistencia a inhibidores de BRAF
US8907270B2 (en) 2010-06-30 2014-12-09 Schlumberger Technology Corporation Method and apparatus for gain regulation in a gamma detector
US11007194B2 (en) 2011-11-11 2021-05-18 Array Biopharma Inc. Method of treating a proliferative disease
CN105708819B (zh) 2011-11-23 2020-12-29 诺华股份有限公司 医药制剂
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
CN103159736B (zh) * 2011-12-10 2015-05-13 通化济达医药有限公司 取代的吡唑激酶抑制剂
UY34539A (es) * 2011-12-23 2013-06-28 Millennium Pharm Inc Heteroarilos y usos de los mismos
EA028135B1 (ru) 2012-03-28 2017-10-31 Дана-Фарбер Кэнсер Инститьют, Инк. Мутанты c-raf, придающие резистентность к ингибиторам raf
IN2015DN00099A (enExample) 2012-07-18 2015-05-29 Univ Saint Louis
US8716226B2 (en) 2012-07-18 2014-05-06 Saint Louis University 3,5 phenyl-substituted beta amino acid derivatives as integrin antagonists
AR091876A1 (es) * 2012-07-26 2015-03-04 Novartis Ag Combinaciones farmaceuticas para el tratamiento de enfermedades proliferativas
MX359403B (es) * 2012-08-07 2018-09-26 Novartis Ag Combinaciones farmacéuticas que comprenden un inhibidor de b-raf, un inhibidor de egfr, y opcionalmente un inhibidor de pi3k-alfa.
CA2928396A1 (en) 2012-08-17 2014-02-20 F. Hoffmann-La Roche Ag Combination therapies for melanoma comprising administering cobimetinib and vemurafinib
WO2014047330A1 (en) * 2012-09-19 2014-03-27 Jean-Michel Vernier Novel raf kinase inhibitors
UA115151C2 (uk) 2012-11-08 2017-09-25 Новартіс Аг Фармацевтична комбінація, що містить інгібітор b-raf та інгібітор деацетилази гістонів, та її застосування при лікуванні проліферативних захворювань
DK2976106T3 (da) * 2013-03-21 2021-06-14 Array Biopharma Inc Kombinationsterapi, som omfatter en b-raf-hæmmer og en anden hæmmer
TWI634114B (zh) 2013-05-08 2018-09-01 永恒生物科技公司 作為激酶抑制劑之呋喃酮化合物
WO2014194127A1 (en) 2013-05-30 2014-12-04 Plexxikon Inc. Compounds for kinase modulation, and indications therefor
WO2015048312A1 (en) 2013-09-26 2015-04-02 Costim Pharmaceuticals Inc. Methods for treating hematologic cancers
WO2015084804A1 (en) 2013-12-03 2015-06-11 Novartis Ag Combination of mdm2 inhibitor and braf inhibitor and their use
CA3168002C (en) * 2013-12-20 2024-10-22 Biomed Valley Discoveries Inc Cancer treatment using combinations of erk and raf inhibitors
US20160339023A1 (en) * 2013-12-23 2016-11-24 Fang Li Pharmaceutical Combinations
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
DE102015103158A1 (de) 2014-03-04 2015-09-10 Bergische Universität Wuppertal Verbindungen für die Behandlung des Melanoms
KR20240110004A (ko) 2014-03-14 2024-07-12 노파르티스 아게 Lag-3에 대한 항체 분자 및 그의 용도
WO2015145388A2 (en) 2014-03-27 2015-10-01 Novartis Ag Methods of treating colorectal cancers harboring upstream wnt pathway mutations
EP3143166A4 (en) 2014-05-16 2018-04-18 University of Massachusetts Treating chronic myelogenous leukemia (cml)
WO2015196072A2 (en) 2014-06-19 2015-12-23 Whitehead Institute For Biomedical Research Uses of kinase inhibitors for inducing and maintaining pluripotency
JP6636014B2 (ja) * 2014-09-12 2020-01-29 ノバルティス アーゲー Rafキナーゼ阻害剤としての化合物および組成物
EP3191127A1 (en) 2014-09-13 2017-07-19 Novartis AG Combination therapies of egfr inhibitors
BR112017006664A2 (pt) 2014-10-03 2017-12-26 Novartis Ag terapias de combinação
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
KR102513870B1 (ko) 2014-10-14 2023-03-23 노파르티스 아게 Pd-l1에 대한 항체 분자 및 그의 용도
CN107530415A (zh) 2015-03-10 2018-01-02 艾杜罗生物科技公司 用于活化“干扰素基因刺激物”依赖性信号传导的组合物和方法
PT3317301T (pt) 2015-07-29 2021-07-09 Novartis Ag Terapias de associação compreendendo moléculas de anticorpo contra lag-3
WO2017019897A1 (en) 2015-07-29 2017-02-02 Novartis Ag Combination therapies comprising antibody molecules to tim-3
US20180222982A1 (en) 2015-07-29 2018-08-09 Novartis Ag Combination therapies comprising antibody molecules to pd-1
RS63125B1 (sr) 2015-11-03 2022-05-31 Janssen Biotech Inc Antitela koja se specifično vezuju za pd-1 i njihova upotreba
US20180371093A1 (en) 2015-12-17 2018-12-27 Novartis Ag Antibody molecules to pd-1 and uses thereof
EP3294716B1 (en) 2015-12-30 2020-04-15 Saint Louis University Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
RU2615986C1 (ru) * 2016-02-25 2017-04-12 Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") Замещенные метил (2-{ 4-[3-(3-метансульфониламино-2-фтор-5-хлор-фенил)-1Н-пиразол-4-ил]пиримидин-2-иламино} -этил)карбаматы, способ их получения и применения
FI3463345T3 (fi) 2016-06-03 2023-01-31 Farmaseuttisia yhdistelmiä
EP3507367A4 (en) 2016-07-05 2020-03-25 Aduro BioTech, Inc. CYCLIC DINUCLEOTID COMPOUNDS WITH INCLUDED NUCLEIC ACIDS AND USES THEREOF
US10954216B2 (en) 2016-12-27 2021-03-23 Riken BMP-signal-inhibiting compound
WO2018146253A1 (en) 2017-02-10 2018-08-16 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the mapk pathway
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
CN107540699A (zh) * 2017-10-16 2018-01-05 康化(上海)新药研发有限公司 一种2‑氨基‑3‑氟吡啶‑4‑硼酸盐酸盐的合成方法
JP7416716B2 (ja) 2017-12-28 2024-01-17 トラクト ファーマシューティカルズ インコーポレイテッド 円柱上皮幹細胞のための幹細胞培養系およびそれに関連した使用法
US12398209B2 (en) 2018-01-22 2025-08-26 Janssen Biotech, Inc. Methods of treating cancers with antagonistic anti-PD-1 antibodies
WO2020011141A1 (zh) * 2018-07-12 2020-01-16 深圳市塔吉瑞生物医药有限公司 一种二芳基吡唑化合物及包含该化合物的组合物及其用途
WO2020124397A1 (en) * 2018-12-19 2020-06-25 Inventisbio Shanghai Ltd. C-terminal src kinase inhibitors
CN113195000A (zh) 2018-12-21 2021-07-30 第一三共株式会社 抗体-药物缀合物和激酶抑制剂的组合
CN113811303A (zh) 2019-05-16 2021-12-17 伊莱利利公司 用于治疗brafv600e结直肠癌的erk1/2抑制剂与braf抑制剂和egfr抑制剂的三药组合
JP2023504730A (ja) 2019-12-05 2023-02-06 アンセルム(アンスティチュート・ナシオナル・ドゥ・ラ・サンテ・エ・ドゥ・ラ・ルシェルシュ・メディカル) N-(3-(5-(ピリミジン-4-イル)チアゾール-4-イル)フェニル)スルホンアミド化合物及びbraf阻害剤としてのそれらの使用
EP4161907A1 (en) 2020-06-09 2023-04-12 Array BioPharma Inc. 4-oxo-3,4-dihydroquinazolinon compounds for the treatment of braf-associated diseases and disorders
US20230303551A1 (en) 2020-08-13 2023-09-28 Albert Einstein College Of Medicine N-cyclyl-sulfonamides useful for inhibiting raf
WO2022074011A1 (en) 2020-10-05 2022-04-14 Pierre Fabre Medicament Combination of encorafenib and binimetinib as adjuvant treatment for resected stage ii melanoma
CN117321418A (zh) 2021-03-18 2023-12-29 诺华股份有限公司 癌症生物标志物及其使用方法
US12371667B2 (en) 2021-05-13 2025-07-29 Washington University Enhanced methods for inducing and maintaining naive human pluripotent stem cells
TW202313046A (zh) 2021-06-09 2023-04-01 瑞士商赫孚孟拉羅股份公司 用於癌症治療之組合療法
CN114557977A (zh) * 2022-02-16 2022-05-31 北京康立生医药技术开发有限公司 一种治疗肠癌的药物的制备方法、制剂及纯度分析方法
WO2023230554A1 (en) 2022-05-25 2023-11-30 Pfizer Inc. Combination of a braf inhibitor, an egfr inhibitor, and a pd-1 antagonist for the treatment of braf v600e-mutant, msi-h/dmmr colorectal cancer
WO2024163166A1 (en) * 2023-01-30 2024-08-08 5Metis, Inc. Boron containing compounds and their uses
EP4656193A1 (en) 2023-04-06 2025-12-03 Eisai R&D Management Co., Ltd. Pharmaceutical composition for treating tumors
CN116396222A (zh) * 2023-04-10 2023-07-07 上海睿腾医药科技有限公司 一种康奈非尼中间体1-(3-氨基-1-异丙基-1h-吡唑-4-基)乙-1-酮的合成方法
WO2025003956A1 (en) 2023-06-30 2025-01-02 Pfizer Inc. High drug loading formulations of encorafenib

Family Cites Families (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4104250A (en) * 1976-08-11 1978-08-01 Borg-Warner Corporation Flame-retardant polymers with 1,3,5-triazines having halo- and halo-aryl substitutents
JPS5475888A (en) 1977-11-29 1979-06-18 Jiyasuko Kk Surgical laser
DE3571974D1 (en) 1984-12-06 1989-09-07 Pfizer Substituted dihydroquinolone carboxylic acids, anti-bacterial compositions containing them
US6358932B1 (en) 1994-05-31 2002-03-19 Isis Pharmaceticals, Inc. Antisense oligonucleotide inhibition of raf gene expression
US6391636B1 (en) 1994-05-31 2002-05-21 Isis Pharmaceuticals, Inc. Antisense oligonucleotide modulation of raf gene expression
US6037136A (en) 1994-10-24 2000-03-14 Cold Spring Harbor Laboratory Interactions between RaF proto-oncogenes and CDC25 phosphatases, and uses related thereto
WO1997008950A1 (en) 1995-09-07 1997-03-13 Fuisz Technologies, Ltd. System for rendering substantially non-dissoluble bio-affecting agents bio-available
US5717100A (en) 1995-10-06 1998-02-10 Merck & Co., Inc. Substituted imidazoles having anti-cancer and cytokine inhibitory activity
IL127210A0 (en) 1996-05-23 1999-09-22 Applied Research Systems Compounds inhibiting the binding of raf-1 or 13-3-3 proteins to the beta-chain of il-2 pharmaceutical compositions containing them and their use
AR012634A1 (es) 1997-05-02 2000-11-08 Sugen Inc Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion
US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
NZ501112A (en) 1997-05-22 2002-10-25 G Substituted pyrazoles as p38 kinase inhibitors
US6187799B1 (en) 1997-05-23 2001-02-13 Onyx Pharmaceuticals Inhibition of raf kinase activity using aryl ureas
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
US6022884A (en) 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
US6204467B1 (en) 1998-03-24 2001-03-20 Ford Global Technologies, Inc. Method and apparatus for resistive welding
ME00275B (me) 1999-01-13 2011-02-10 Bayer Corp ω-KARBOKSIARIL SUPSTITUISANI DIFENIL KARBAMIDI KAO INHIBITORI RAF KINAZE
US6316435B2 (en) 1999-02-24 2001-11-13 Supergen, Inc. Combination therapy for lymphoproliferative diseases
ES2398643T3 (es) 1999-12-23 2013-03-20 Mayne Pharma International Pty Ltd. Composiciones farmacéuticas mejoradas para fármacos escasamente solubles
WO2002018654A1 (en) 2000-08-30 2002-03-07 The Board Of Trustees Of The University Of Arkansas Induction of ldl receptor expression by extracellular-signal regulated kinase, erk-1/2
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
SI1441714T1 (sl) 2001-10-25 2008-06-30 Novartis Ag Kombinacije, ki obsegajo selektivni inhibitor ciklooksigenaze-2
US7247734B2 (en) 2001-12-21 2007-07-24 Vernalis (Cambridge) Limited 3,4-diarylpyrazoles and their use in the therapy of cancer
ZA200407220B (en) 2002-03-13 2007-05-30 Array Biopharma Inc N3 alkylated benzimidazole derivatives as MEK inhibitors
CA2537991A1 (en) 2003-09-23 2005-03-31 Novartis Ag Combination of a vegf receptor inhibitor with a chemotherapeutic agent
US8969372B2 (en) 2003-11-14 2015-03-03 Aptose Boisciences Inc. Aryl imidazoles and their use as anti-cancer agents
KR20060127032A (ko) 2004-01-09 2006-12-11 노파르티스 아게 Igf―ir 억제제로서의페닐-[4-(3-페닐-1h-피라졸-4-일)-피리미딘-2-일]-아민유도체
WO2005123719A1 (en) 2004-06-10 2005-12-29 Irm Llc Compounds and compositions as protein kinase inhibitors
US20060058311A1 (en) 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
CA2601766A1 (en) 2005-03-17 2006-09-28 Novartis Ag N- [3- (1-amin0-5, 6, 7, 8-tetrahydro-2 , 4, 4b-triazafluoren-9-yl)-phenyl] benzamides as tyrosine/threonine kinase inhibitors, in particular b-raf kinase
US20070099856A1 (en) 2005-05-13 2007-05-03 Gumerlock Paul H Combined treatment with docetaxel and an epidermal growth factor receptor kinase inhibitor using an intermittent dosing regimen
EP1934185A1 (en) 2005-08-12 2008-06-25 Synta Pharmaceuticals Corporation Pyrazole compounds that modulate hsp90 activity
MX2008002492A (es) 2005-08-22 2008-04-03 Novartis Ag Composiciones farmaceuticas que comprenden un farmaco dependiente del ph, un modificador del ph, y un agente retardante.
US20080242667A1 (en) 2005-08-26 2008-10-02 Smithkline Beecham Corporation Pyrimidinyl-Pyrazole Inhibitors of Aurora Kinases
TWI387592B (zh) 2005-08-30 2013-03-01 Novartis Ag 經取代之苯并咪唑及其作為與腫瘤形成相關激酶之抑制劑之方法
WO2007105058A2 (en) 2006-03-16 2007-09-20 Pfizer Products Inc. Pyrazole compounds
CN101415411A (zh) 2006-04-05 2009-04-22 诺瓦提斯公司 用于治疗癌症的治疗剂组合
WO2007123892A2 (en) * 2006-04-17 2007-11-01 Arqule Inc. Raf inhibitors and their uses
KR20090077914A (ko) 2006-09-11 2009-07-16 쿠리스 인코퍼레이션 항증식제로서의 다작용성 소분자
AU2007299080B2 (en) 2006-09-18 2013-04-18 Boehringer Ingelheim International Gmbh Method for treating cancer harboring EGFR mutations
AU2007305016B2 (en) 2006-10-02 2011-11-03 Novartis Ag Compounds and compositions as protein kinase inhibitors
CN101522026A (zh) * 2006-10-06 2009-09-02 Irm责任有限公司 蛋白激酶抑制剂及其应用方法
AU2008216327A1 (en) 2007-02-15 2008-08-21 Novartis Ag Combination of LBH589 with other therapeutic agents for treating cancer
US20090022789A1 (en) 2007-07-18 2009-01-22 Supernus Pharmaceuticals, Inc. Enhanced formulations of lamotrigine
AP2010005167A0 (en) * 2007-08-01 2010-02-28 Pfizer Pyrazole compounds and their use as RAF inhibitors
MX2010004291A (es) 2007-10-19 2010-08-02 Abbott Gmbh & Co Kg Producto de dispersion solida de farmacos basados en n-aril urea.
MX2010005110A (es) 2007-11-14 2010-09-09 Ortho Mcneil Janssen Pharm Derivados de imidazo[1,2-a]piridina y su uso como moduladores alostericos positivos de los receptores de glutamato metabotropico 2.
CA2718936A1 (en) 2008-03-21 2009-09-24 Novartis Ag Novel heterocyclic compounds and uses therof
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
PT2324008E (pt) * 2008-07-24 2012-06-25 Nerviano Medical Sciences Srl 3,4-diarilpirazoles como inibidores da proteína quinase
MX2011001090A (es) 2008-07-28 2011-03-15 Gilead Sciences Inc Compuestos de inhibidor de desacetilasa de histona de cicloalquilideno y heterocicloalquilideno.
JP5603869B2 (ja) 2008-09-29 2014-10-08 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規化合物
HUE030800T2 (en) 2008-10-07 2017-05-29 Astrazeneca Uk Ltd Pharmaceutical Form No. 514
US20110293750A1 (en) * 2008-11-11 2011-12-01 Yale University Activated wnt-beta-catenin signaling in melanoma
EP2373664B1 (en) 2008-12-19 2013-06-12 Nerviano Medical Sciences S.r.l. Bicyclic pyrazoles as protein kinase inhibitors
AR075180A1 (es) 2009-01-29 2011-03-16 Novartis Ag Formulaciones orales solidas de una pirido-pirimidinona
RU2402602C1 (ru) 2009-02-12 2010-10-27 Государственное учреждение Российский онкологический научный центр им. Н.Н. Блохина РАМН КЛЕТОЧНАЯ ЛИНИЯ МЕЛАНОМЫ ЧЕЛОВЕКА mel Rac, ИСПОЛЬЗУЕМАЯ ДЛЯ ПОЛУЧЕНИЯ ПРОТИВООПУХОЛЕВЫХ ВАКЦИН
WO2010100127A1 (en) 2009-03-04 2010-09-10 Novartis Ag Disubstituted imidazole derivatives as modulators of raf kinase
TWI532484B (zh) 2009-06-08 2016-05-11 艾伯維有限公司 包含凋亡促進劑之固態分散劑
US8546413B2 (en) * 2009-06-15 2013-10-01 Nerviano Medical Sciences S.R.L. Substituted pyrimidinylpyrrolopyridinone derivatives, process for their preparation and their use as kinase inhibitors
KR101256018B1 (ko) * 2009-08-20 2013-04-18 한국과학기술연구원 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물
US8242260B2 (en) * 2009-08-28 2012-08-14 Novartis Ag Compounds and compositions as protein kinase inhibitors
AR077975A1 (es) 2009-08-28 2011-10-05 Irm Llc Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina
CA2786509C (en) 2010-01-27 2016-01-05 Nerviano Medical Sciences S.R.L. Sulfonamido derivatives of 3,4-diarylpyrazoles as protein kinase inhibitors
KR102113960B1 (ko) 2010-03-30 2020-05-21 베르선 코포레이션 트롬빈 억제제로서의 다중치환된 방향족 화합물
WO2012016993A1 (en) 2010-08-03 2012-02-09 Nerviano Medical Sciences S.R.L. Derivatives of pyrazolophenyl-benzenesulfonamide compounds and use thereof as antitumor agents
PL2688572T3 (pl) 2011-03-21 2017-08-31 Valcuria Ab Kompozycja farmaceutyczna zawierająca inhibitor hdac i steroid oraz jej stosowanie
SG195141A1 (en) 2011-06-14 2013-12-30 Novartis Ag Combination of panobinostat and ruxolitinib in the treatment of cancer suchas a myeloproliferative neoplasm
US11007194B2 (en) 2011-11-11 2021-05-18 Array Biopharma Inc. Method of treating a proliferative disease
CN105708819B (zh) 2011-11-23 2020-12-29 诺华股份有限公司 医药制剂
UA115151C2 (uk) 2012-11-08 2017-09-25 Новартіс Аг Фармацевтична комбінація, що містить інгібітор b-raf та інгібітор деацетилази гістонів, та її застосування при лікуванні проліферативних захворювань
US10576680B2 (en) 2015-11-19 2020-03-03 The Boeing Company Modular thermoforming system

Also Published As

Publication number Publication date
LTPA2019005I1 (lt) 2019-03-25
CY2019014I2 (el) 2019-11-27
PT2470526E (pt) 2014-09-01
RS55568B1 (sr) 2017-05-31
US9593099B2 (en) 2017-03-14
CN102725283B (zh) 2014-02-26
CA2771775C (en) 2015-01-20
JO3002B1 (ar) 2016-09-05
AU2010286569C1 (en) 2019-11-28
JP6045519B2 (ja) 2016-12-14
US20160280686A1 (en) 2016-09-29
CL2012000340A1 (es) 2012-08-17
RS53489B1 (sr) 2015-02-27
US20160263113A1 (en) 2016-09-15
EP2727918B1 (en) 2016-10-12
NL300973I2 (nl) 2022-05-05
LUC00102I2 (enExample) 2024-05-21
NO2019012I1 (no) 2019-03-05
US20130296318A1 (en) 2013-11-07
DOP2012000051A (es) 2012-05-31
US20110306625A1 (en) 2011-12-15
KR20120062839A (ko) 2012-06-14
ZA201202020B (en) 2012-12-27
HUE032847T2 (hu) 2017-11-28
US20180297986A1 (en) 2018-10-18
MY156259A (en) 2016-01-29
CY2019013I2 (el) 2019-11-27
US20160120866A1 (en) 2016-05-05
MX2012002546A (es) 2012-04-11
ME01860B (me) 2014-12-20
SG10201405311TA (en) 2014-09-26
PL2470526T3 (pl) 2014-10-31
CU20120034A7 (es) 2012-06-21
SMT201700036B (it) 2017-03-08
CA2771775A1 (en) 2011-03-03
BR112012004453A8 (pt) 2021-06-08
US20160280687A1 (en) 2016-09-29
ECSP23004573A (es) 2023-04-28
SI2727918T1 (sl) 2017-02-28
PE20120861A1 (es) 2012-07-14
CY2019013I1 (el) 2019-11-27
ES2610825T3 (es) 2017-05-03
WO2011025927A1 (en) 2011-03-03
CN103896921A (zh) 2014-07-02
US20180297985A1 (en) 2018-10-18
EP2727918A1 (en) 2014-05-07
IL218084A (en) 2016-11-30
JP2014098022A (ja) 2014-05-29
HUS1900012I1 (hu) 2019-04-29
NZ598924A (en) 2013-07-26
AR077975A1 (es) 2011-10-05
LUC00101I1 (enExample) 2019-02-13
HUS1900013I1 (hu) 2019-04-29
US10576080B2 (en) 2020-03-03
JP2013503186A (ja) 2013-01-31
EP2470526B1 (en) 2014-05-28
US20230116233A1 (en) 2023-04-13
ME02684B (me) 2017-06-20
DK2727918T3 (da) 2017-01-23
CY2019014I1 (el) 2019-11-27
USRE49556E1 (en) 2023-06-20
HK1167390A1 (en) 2012-11-30
ECSP12011700A (es) 2012-03-30
AU2010286569A1 (en) 2012-04-12
BR112012004453A2 (pt) 2021-03-09
TN2012000081A1 (en) 2013-09-19
US9850229B2 (en) 2017-12-26
JP5475888B2 (ja) 2014-04-16
ES2492499T3 (es) 2014-09-09
US9314464B2 (en) 2016-04-19
US20160122324A1 (en) 2016-05-05
CN103896921B (zh) 2016-02-24
CN102725283A (zh) 2012-10-10
CU24110B1 (es) 2015-07-30
SMT201400133B (it) 2014-11-10
UA112285C2 (uk) 2016-08-25
KR101413392B1 (ko) 2014-06-27
SG178351A1 (en) 2012-03-29
EA201200373A1 (ru) 2012-09-28
UY32860A (es) 2011-03-31
EA201500175A1 (ru) 2015-05-29
LUC00101I2 (enExample) 2020-01-23
US10568884B2 (en) 2020-02-25
HN2012000441A (es) 2015-01-05
US9593100B2 (en) 2017-03-14
IL218084A0 (en) 2012-04-30
LT2727918T (lt) 2017-01-25
IN2012DN02469A (enExample) 2015-08-21
US8501758B2 (en) 2013-08-06
GT201200053A (es) 2014-03-27
PT2727918T (pt) 2017-01-20
CO6612222A2 (es) 2013-02-01
CR20120102A (es) 2012-05-02
EP2470526A1 (en) 2012-07-04
US20200323852A1 (en) 2020-10-15
EA025222B1 (ru) 2016-12-30
MA33604B1 (fr) 2012-09-01
NI201200029A (es) 2012-05-29
BR112012004453B1 (pt) 2022-04-26
SMT201700036T1 (it) 2017-03-08
US10005761B2 (en) 2018-06-26
NO2019011I1 (no) 2019-03-05
PL2727918T3 (pl) 2017-06-30
LTPA2019006I1 (lt) 2019-03-25
DK2470526T3 (da) 2014-08-25
US9850230B2 (en) 2017-12-26
LTC2470526I2 (lt) 2020-04-27
SI2470526T1 (sl) 2014-09-30
GEP20146102B (en) 2014-05-27
NL300973I1 (enExample) 2019-03-27
CY1118452T1 (el) 2017-07-12
HRP20170005T1 (hr) 2017-03-10
AU2010286569B2 (en) 2013-10-10

Similar Documents

Publication Publication Date Title
HRP20140799T1 (hr) Spojevi i sastavi kao inhibitori kinaze proteina
CN1151789C (zh) 芳基(或杂芳基)吡咯基甲醇的衍生物的应用
KR101855358B1 (ko) 골암통증에서의 시그마 리간드의 용도
MX2025001995A (es) Compuesto heterociclico, procedimiento para prepararlo y uso farmaceutico del mismo
SG10201407409WA (en) Inhibitors of jun n-terminal kinase
EA200900155A1 (ru) Модуляторы фармакокинетических свойств лекарственных средств
EA200970342A1 (ru) Антагонисты рецептора глюкагона, композиции, содержащие такие соединения, и способы применения
NZ593295A (en) Preparation method of dihydroindene amide compounds, their pharmaceutical compositions containing compounds thereof and use as protein kinase inhibitor
EA200901138A1 (ru) Производные дианилинопиримидина как ингибиторы киназы wee1, фармацевтическая композиция и применение
BR122013028005B8 (pt) compostos de ciclopentanos de pirimidila hidroxilados e metoxilados, composição farmacêutica, kit e forma de dosagem oral compreendendo os referidos compostos, uso das referidas composições, bem como processo de preparação dos referidos compostos
MA29432B1 (fr) Antagonistes du recepteur du glucagon, leur preparation et leurs utilisations therapeutiques
EA200700118A1 (ru) Амидосоединения и их применение в качестве лекарственных средств
TW200637874A (en) Peptides with neuropeptide-2 receptor (Y2R) agonist activity
JP2011524906A5 (enExample)
EA200901133A1 (ru) Производные дианилинопиримидина как ингибиторы киназы wee1, фармацевтическая композиция и применение
ZA200808816B (en) Pieridinyl substituted pyrrolidinones as inhibitors of 11-Beta-hydroxysteroid dehydrogenase 1
EA200800665A1 (ru) АГЕНТЫ ДЛЯ ПРЕДУПРЕЖДЕНИЯ И ЛЕЧЕНИЯ НАРУШЕНИЙ, ВКЛЮЧАЮЩИХ МОДУЛИРОВАНИЯ RyR РЕЦЕПТОРОВ
HRP20110219T1 (hr) Novi alfa-(n-sulfonamido)acetamidni spoj kao inhibitor proizvodnje beta amiloid peptida
ATE530544T1 (de) Benzyl-substituierte positive allosterische chinolon-m1-rezeptormodulatoren
AR077642A1 (es) Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
EA201000486A1 (ru) Ингибитор белка, активирующего 5-липоксигеназу (flap)
EA200700027A1 (ru) Антагонисты рецептора глюкагона, их получение и терапевтическое применение
ECSP088829A (es) Derivados de bencimidazol 5-sulfonamida como ligandos del receptor cannabinoide 1 (cb1)
HRP20120085T1 (hr) Pripravak zibotentana koji sadrži manitol i mikrokristalnu celulozu
GEP20115348B (en) Pharmaceutical composition for treating burns (variants) and methods for the production thereof (variants)