CL2012000340A1 - Compuestos heterociclicos derivados de pirimidina sustituida; composicion farmaceutica y su uso como inhibidores de quinasas para tratar el cancer tal como carcinoma pulmonar, carcinoma pancreatico, carcinoma de vejiga, carcinoma de colon, trastornos mieloides, cancer de prostata, de tiroides, melanomas, adenomas, cancer de higado. - Google Patents

Compuestos heterociclicos derivados de pirimidina sustituida; composicion farmaceutica y su uso como inhibidores de quinasas para tratar el cancer tal como carcinoma pulmonar, carcinoma pancreatico, carcinoma de vejiga, carcinoma de colon, trastornos mieloides, cancer de prostata, de tiroides, melanomas, adenomas, cancer de higado.

Info

Publication number
CL2012000340A1
CL2012000340A1 CL2012000340A CL2012000340A CL2012000340A1 CL 2012000340 A1 CL2012000340 A1 CL 2012000340A1 CL 2012000340 A CL2012000340 A CL 2012000340A CL 2012000340 A CL2012000340 A CL 2012000340A CL 2012000340 A1 CL2012000340 A1 CL 2012000340A1
Authority
CL
Chile
Prior art keywords
carcinoma
cancer
melanomas
adenomas
pharmaceutical composition
Prior art date
Application number
CL2012000340A
Other languages
English (en)
Inventor
Huang Shenlin
Liu Zuosheng
E Tellew John
Wan Yongqin
Wang Xing
Xie Yongping
Jin Xianming
Poon Daniel
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=CL2012000340(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 CL2012000340A1 publication Critical patent/CL2012000340A1/es

Links

Classifications

    • 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
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/14—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 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)

Abstract

LA INVENCIÓN PROPORCIONA UNA CLASE NOVEDOSA DE COMPUESTOS, COMPOSICIONES FARMACÉUTICAS QUE COMPRENDEN ESTOS COMPUESTOS, Y SU USO PARA TRATAR PREVENIR LAS ENFERMEDADES O LOS TRASTORNOS<br /> ASOCIADOS CON UNA ACTIVIDAD DE CINASA ANORMAL O MAL REGULADA, EN PARTICULAR LAS ENFERMEDADES O LOS TRASTORNOS QUE INVOLUCREN UNA ACTIVIDAD ANORMAL DE B-RAF, COMO CÁNCER, CARCINOMA<br /> PULMONAR, CARCINOMA PANCREÁTICO, CARCINOMA DE VEJIGA, DE COLON, TRASTORNOS MIELOIDES, CÁNCER DE PROSTATA, DE TIROIDES, MELANOMAS, ADENOMAS, CÁNCER DE HÍGADO.<br />  
CL2012000340A 2009-08-28 2012-02-09 Compuestos heterociclicos derivados de pirimidina sustituida; composicion farmaceutica y su uso como inhibidores de quinasas para tratar el cancer tal como carcinoma pulmonar, carcinoma pancreatico, carcinoma de vejiga, carcinoma de colon, trastornos mieloides, cancer de prostata, de tiroides, melanomas, adenomas, cancer de higado. CL2012000340A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US23807309P 2009-08-28 2009-08-28
US31303910P 2010-03-11 2010-03-11

Publications (1)

Publication Number Publication Date
CL2012000340A1 true CL2012000340A1 (es) 2012-08-17

Family

ID=42782253

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2012000340A CL2012000340A1 (es) 2009-08-28 2012-02-09 Compuestos heterociclicos derivados de pirimidina sustituida; composicion farmaceutica y su uso como inhibidores de quinasas para tratar el cancer tal como carcinoma pulmonar, carcinoma pancreatico, carcinoma de vejiga, carcinoma de colon, trastornos mieloides, cancer de prostata, de tiroides, melanomas, adenomas, cancer de higado.

Country Status (50)

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US (12) US8501758B2 (es)
EP (2) EP2470526B1 (es)
JP (2) JP5475888B2 (es)
KR (1) KR101413392B1 (es)
CN (2) CN102725283B (es)
AR (1) AR077975A1 (es)
AU (1) AU2010286569C1 (es)
BR (1) BR112012004453B1 (es)
CA (1) CA2771775C (es)
CL (1) CL2012000340A1 (es)
CO (1) CO6612222A2 (es)
CR (1) CR20120102A (es)
CU (1) CU24110B1 (es)
CY (3) CY1118452T1 (es)
DK (2) DK2727918T3 (es)
DO (1) DOP2012000051A (es)
EA (2) EA201500175A1 (es)
EC (2) ECSP12011700A (es)
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GE (1) GEP20146102B (es)
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IN (1) IN2012DN02469A (es)
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LT (3) LT2727918T (es)
LU (2) LUC00102I2 (es)
MA (1) MA33604B1 (es)
ME (2) ME01860B (es)
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MY (1) MY156259A (es)
NI (1) NI201200029A (es)
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PE (1) PE20120861A1 (es)
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SG (2) SG10201405311TA (es)
SI (2) SI2727918T1 (es)
SM (2) SMT201400133B (es)
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UA (1) UA112285C2 (es)
UY (1) UY32860A (es)
WO (1) WO2011025927A1 (es)
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Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO3002B1 (ar) 2009-08-28 2016-09-05 Irm Llc مركبات و تركيبات كمثبطات كيناز بروتين
CA2789696C (en) 2010-02-25 2017-11-07 Dana-Farber Cancer Institute, Inc. Braf mutations conferring resistance to braf inhibitors
US8907270B2 (en) 2010-06-30 2014-12-09 Schlumberger Technology Corporation Method and apparatus for gain regulation in a gamma detector
CA2855243C (en) * 2011-11-11 2020-04-14 Novartis Ag Method of treating a proliferative disease
JP6216325B2 (ja) 2011-11-23 2017-10-18 ノバルティス アーゲー 医薬製剤
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
UY34540A (es) * 2011-12-23 2013-06-28 Millennium Pharm Inc Heteroarilos y usos de los mismos
ES2673070T3 (es) 2012-03-28 2018-06-19 Dana-Farber Cancer Institute, Inc. Mutantes C-RAF que confieren resistencia a los inhibidores de RAF
US9085606B2 (en) 2012-07-18 2015-07-21 Saint Louis University Beta amino acid derivatives as integrin antagonists
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
PT2882440T (pt) * 2012-08-07 2019-04-23 Array Biopharma Inc Combinações farmacêuticas compreendendo um inibidor de braf, um inibidor de egfr e opcionalmente um inibidor de pi3k-alfa
PL2884979T3 (pl) 2012-08-17 2019-11-29 Hoffmann La Roche Terapie skojarzone czerniaka obejmujące podawanie kobimetynibu i wemurafinibu
WO2014047330A1 (en) * 2012-09-19 2014-03-27 Jean-Michel Vernier Novel raf kinase inhibitors
JP2015536964A (ja) 2012-11-08 2015-12-24 ノバルティス アーゲー Ｂ−ｒａｆ阻害剤とヒストン脱アセチル化酵素阻害剤を含む医薬組合せおよび増殖性疾患の治療におけるそれらの使用
CN112641787A (zh) 2013-03-21 2021-04-13 诺华股份有限公司 包含B-Raf抑制剂和第二抑制剂的组合疗法
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
RU2015149937A (ru) 2013-05-30 2017-07-06 Плексксикон Инк. Соединения для модулирования киназы и показания к их применению
EP3049442A4 (en) 2013-09-26 2017-06-28 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
AU2014368906B2 (en) * 2013-12-20 2020-04-30 Biomed Valley Discoveries, Inc. Cancer treatment using combinations of ERK and RAF inhibitors
AU2014372166B2 (en) * 2013-12-23 2017-10-26 Novartis Ag 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
ES2770684T3 (es) 2014-03-14 2020-07-02 Novartis Ag Moléculas de anticuerpos contra LAG-3 y usos de los mismos
WO2015145388A2 (en) 2014-03-27 2015-10-01 Novartis Ag Methods of treating colorectal cancers harboring upstream wnt pathway mutations
US10428387B2 (en) 2014-05-16 2019-10-01 University Of Massachusetts Treating chronic myelogenous leukemia (CML)
WO2016038582A1 (en) * 2014-09-12 2016-03-17 Novartis Ag Compounds and compositions as raf kinase inhibitors
KR20170060042A (ko) 2014-09-13 2017-05-31 노파르티스 아게 Alk 억제제의 조합 요법
JP2017535528A (ja) 2014-10-03 2017-11-30 ノバルティス アーゲー 組み合わせ治療
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
MX2017004810A (es) 2014-10-14 2017-10-16 Novartis Ag Moleculas de anticuerpo que se unen a pd-l1 y usos de las mismas.
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
EP3964528A1 (en) 2015-07-29 2022-03-09 Novartis AG Combination therapies comprising antibody molecules to 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
MX2018005550A (es) 2015-11-03 2019-07-18 Janssen Biotech Inc Anticuerpos que se unen especificamente a tim-3 y sus usos.
JP2019503349A (ja) 2015-12-17 2019-02-07 ノバルティス アーゲー Ｐｄ−１に対する抗体分子およびその使用
ES2806276T3 (es) 2015-12-30 2021-02-17 Univ Saint Louis Derivados de ácido aminobenzoico meta-azaciclicos como antagonistas pan-integrina
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
RU2759669C2 (ru) 2016-06-03 2021-11-16 Аррэй Байофарма Инк. Фармацевтические комбинации
US11098077B2 (en) 2016-07-05 2021-08-24 Chinook Therapeutics, Inc. Locked nucleic acid cyclic dinucleotide compounds and uses thereof
CA3048376A1 (en) * 2016-12-27 2018-07-05 Riken Bmp-signal-inhibiting compound
US11471538B2 (en) 2017-02-10 2022-10-18 INSERM (Institut National de la Santéet de la Recherche Medicale) 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
WO2019133810A1 (en) 2017-12-28 2019-07-04 Tract Pharmaceuticals, Inc. Stem cell culture systems for columnar epithelial stem cells, and uses related thereto
US20210283132A1 (en) * 2018-07-12 2021-09-16 Shenzhen Targetrx, Inc. Diarylpyrazole compound, composition comprising same, and use thereof
WO2020124397A1 (en) * 2018-12-19 2020-06-25 Inventisbio Shanghai Ltd. C-terminal src kinase inhibitors
EP3903828A4 (en) 2018-12-21 2022-10-05 Daiichi Sankyo Company, Limited COMBINATION OF AN ANTIBODY-DRUG CONJUGATE AND A KINASE INHIBITOR
EP3968995A1 (en) 2019-05-16 2022-03-23 Eli Lilly and Company Triple combination of an erk1/2 inhibitor with a braf inhibitor and an egfr inhibitor for use in the treatment of brafv600e colorectal cancer
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
EP4196228A1 (en) 2020-08-13 2023-06-21 Albert Einstein College of Medicine N-cyclyl-sulfonamides useful for inhibiting raf
EP4225307A1 (en) 2020-10-05 2023-08-16 Pierre Fabre Medicament Combination of encorafenib and binimetinib as adjuvant treatment for resected stage ii melanoma
JP2024511373A (ja) 2021-03-18 2024-03-13 ノバルティス アーゲー がんのためのバイオマーカーおよびその使用
KR20240005899A (ko) 2021-06-09 2024-01-12 에프. 호프만-라 로슈 아게 암 치료를 위한 병용요법
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

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
EP0184384B1 (en) 1984-12-06 1989-08-02 Pfizer Inc. 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
AU7106996A (en) 1995-09-07 1997-03-27 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
CA2291115A1 (en) 1997-05-22 1998-11-26 G.D. Searle & Co. Substituted pyrazoles as p38 kinase inhibitors
US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company 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
US7351834B1 (en) 1999-01-13 2008-04-01 Bayer Pharmaceuticals Corporation ω-Carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US6316435B2 (en) 1999-02-24 2001-11-13 Supergen, Inc. Combination therapy for lymphoproliferative diseases
AU782469B2 (en) 1999-12-23 2005-08-04 Mayne Pharma International Pty Ltd Improved pharmaceutical compositions for poorly soluble drugs
AU2001285349A1 (en) 2000-08-30 2002-03-13 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)
ES2295428T3 (es) 2001-10-25 2008-04-16 Novartis Ag Combinaciones que comprenden un inhibidor selectivo de ciclooxigenasa-2.
US7247734B2 (en) 2001-12-21 2007-07-24 Vernalis (Cambridge) Limited 3,4-diarylpyrazoles and their use in the therapy of cancer
IL163995A0 (en) 2002-03-13 2005-12-18 Array Biopharma Inc N3 alkylated benzimidazole derivatives as mek inhibitors
BRPI0414698A (pt) 2003-09-23 2006-11-28 Novartis Ag combinação de um inibidor receptor de vegf com um agente quimioterapêutico
CA2545942C (en) 2003-11-14 2012-07-10 Lorus Therapeutics Inc. Aryl imidazoles and their use as anti-cancer agents
RU2006128788A (ru) 2004-01-09 2008-02-20 Новартис АГ (CH) Производные фенил[4-(3-фенил-1н-пиразол-4-ил)пиримидин-2-ил] амина в качестве igf-1r ингибиторов
AR049511A1 (es) 2004-06-10 2006-08-09 Irm Llc Compuestos y composiciones como inhibidores de quinasa de proteina
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
AU2006284053B2 (en) 2005-08-22 2010-04-22 Novartis Ag Pharmaceutical compositions comprising a pH-dependent drug, a pH modifier and a retarding agent
WO2007024843A2 (en) 2005-08-26 2007-03-01 Smithkline Beecham Corporation Pyrimidinyl-pyrazole inhibitors of aurora kinases
PE20070427A1 (es) 2005-08-30 2007-04-21 Novartis Ag Compuestos derivados de benzimidazoles sustituidos como inhibidores de tirosina quinasas
CA2643066A1 (en) * 2006-03-16 2007-09-20 Pfizer Products Inc. Pyrazole compounds
BRPI0710291A2 (pt) 2006-04-05 2011-08-09 Novartis Ag combinações de agente terapêuticos para tratamento de cáncer
WO2007123892A2 (en) * 2006-04-17 2007-11-01 Arqule Inc. Raf inhibitors and their uses
EP2061772A4 (en) 2006-09-11 2011-06-29 Curis Inc MULTIFUNCTIONAL SMALL MOLECULES AS PROLIFERATION-ACTIVE ACTIVE SUBSTANCES
PT2068880E (pt) 2006-09-18 2012-07-12 Boehringer Ingelheim Int Método para tratamento do cancro apresentando mutações no egfr
CA2663366C (en) 2006-10-02 2012-02-07 Irm Llc Compounds and compositions as protein kinase inhibitors
MX2009003649A (es) 2006-10-06 2009-04-22 Irm Llc Inhibidores de cinasa de proteina y metodos para utilizarlos.
PE20090519A1 (es) 2007-02-15 2009-05-29 Novartis Ag Composicion farmaceutica que contiene n-hidroxi-3-[4-[[[2-(2-metil-1h-indol-3-il)-etil]-amino]-metil]-fenil]-2e-2-propenamida
US20090022789A1 (en) 2007-07-18 2009-01-22 Supernus Pharmaceuticals, Inc. Enhanced formulations of lamotrigine
EA201000113A1 (ru) * 2007-08-01 2010-08-30 Пфайзер Инк. Пиразольные соединения
WO2009050291A2 (en) 2007-10-19 2009-04-23 Abbott Gmbh & Co. Kg Solid dispersion product of n-aryl urea-based drugs
WO2009062676A2 (en) * 2007-11-14 2009-05-22 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. Imidazo[1,2-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
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
CA2731146C (en) 2008-07-24 2016-05-03 Nerviano Medical Sciences S.R.L. 3,4-diarylpyrazoles as protein kinase inhibitors
CA2731323A1 (en) 2008-07-28 2010-02-04 Gilead Sciences, Inc. Cycloalkylidene and heterocycloalkylidene histone deacetylase inhibitor compounds
AU2009295855A1 (en) 2008-09-29 2010-04-01 Boehringer Ingelheim International Gmbh Antiproliferative compounds
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
JP5789602B2 (ja) * 2009-06-15 2015-10-07 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 置換ピリミジニルピロロピリジノン誘導体、これらの製造のための方法およびキナーゼ阻害剤としてのこれらの使用
KR101256018B1 (ko) * 2009-08-20 2013-04-18 한국과학기술연구원 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물
JO3002B1 (ar) 2009-08-28 2016-09-05 Irm Llc مركبات و تركيبات كمثبطات كيناز بروتين
US8242260B2 (en) * 2009-08-28 2012-08-14 Novartis Ag Compounds and compositions as protein kinase inhibitors
MX341728B (es) 2010-01-27 2016-08-30 Nerviano Medical Sciences S R L * Derivados sulfonamido de 3, 4/diarilpirazoles como inhibidores de proteina quinasa.
WO2011126903A2 (en) 2010-03-30 2011-10-13 Verseon, Inc. Multisubstituted aromatic compounds as inhibitors of thrombin
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
BR112013023970B1 (pt) 2011-03-21 2021-11-16 Valcuria Ab Uso de uma combinação de ácido valproico ou um sal farmaceuticamente aceitável deste e prednisona ou dexametasona ou um sal farmaceuticamente aceitável deste
AU2012271814A1 (en) 2011-06-14 2013-12-12 Novartis Ag Combination of panobinostat and ruxolitinib in the treatment of cancer such as a myeloproliferative neoplasm
CA2855243C (en) 2011-11-11 2020-04-14 Novartis Ag Method of treating a proliferative disease
JP6216325B2 (ja) 2011-11-23 2017-10-18 ノバルティス アーゲー 医薬製剤
JP2015536964A (ja) 2012-11-08 2015-12-24 ノバルティス アーゲー Ｂ−ｒａｆ阻害剤とヒストン脱アセチル化酵素阻害剤を含む医薬組合せおよび増殖性疾患の治療におけるそれらの使用
US10576680B2 (en) 2015-11-19 2020-03-03 The Boeing Company Modular thermoforming system

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