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)
Spanish (es)
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

    • 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)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
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 (49)

Country Link
US (12) US8501758B2 (enEXAMPLES)
EP (2) EP2727918B1 (enEXAMPLES)
JP (2) JP5475888B2 (enEXAMPLES)
KR (1) KR101413392B1 (enEXAMPLES)
CN (2) CN103896921B (enEXAMPLES)
AR (1) AR077975A1 (enEXAMPLES)
AU (1) AU2010286569C1 (enEXAMPLES)
BR (1) BR112012004453B1 (enEXAMPLES)
CA (1) CA2771775C (enEXAMPLES)
CL (1) CL2012000340A1 (enEXAMPLES)
CO (1) CO6612222A2 (enEXAMPLES)
CR (1) CR20120102A (enEXAMPLES)
CU (1) CU24110B1 (enEXAMPLES)
CY (3) CY1118452T1 (enEXAMPLES)
DK (2) DK2470526T3 (enEXAMPLES)
DO (1) DOP2012000051A (enEXAMPLES)
EA (2) EA201500175A1 (enEXAMPLES)
EC (2) ECSP12011700A (enEXAMPLES)
ES (2) ES2610825T3 (enEXAMPLES)
GE (1) GEP20146102B (enEXAMPLES)
GT (1) GT201200053A (enEXAMPLES)
HN (1) HN2012000441A (enEXAMPLES)
HR (2) HRP20140799T1 (enEXAMPLES)
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IL (1) IL218084A (enEXAMPLES)
IN (1) IN2012DN02469A (enEXAMPLES)
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NI (1) NI201200029A (enEXAMPLES)
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NZ (1) NZ598924A (enEXAMPLES)
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PL (2) PL2470526T3 (enEXAMPLES)
PT (2) PT2727918T (enEXAMPLES)
RS (2) RS53489B1 (enEXAMPLES)
SG (2) SG178351A1 (enEXAMPLES)
SI (2) SI2727918T1 (enEXAMPLES)
SM (3) SMT201700036T1 (enEXAMPLES)
TN (1) TN2012000081A1 (enEXAMPLES)
UA (1) UA112285C2 (enEXAMPLES)
UY (1) UY32860A (enEXAMPLES)
WO (1) WO2011025927A1 (enEXAMPLES)
ZA (1) ZA201202020B (enEXAMPLES)

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
EP2538943B1 (en) 2010-02-25 2016-03-30 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
PT2782557T (pt) 2011-11-23 2018-11-26 Array Biopharma Inc Formulações farmacêuticas
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
WO2013096630A1 (en) * 2011-12-23 2013-06-27 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
ES2790896T3 (es) 2012-03-28 2020-10-29 Dana Farber Cancer Inst Inc Mutantes C-RAF que confieren resistencia a los inhibidores de RAF
JP6215324B2 (ja) 2012-07-18 2017-10-18 セントルイス ユニバーシティ インテグリンアンタゴニストとしてのβアミノ酸誘導体
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
DK2882440T3 (da) * 2012-08-07 2019-05-06 Novartis Ag Farmaceutiske kombinationer, der omfatter en b-raf-inhibitor, en egfr-inhibitor og eventuelt en pi3k-alfa-inhibitor
HK1206605A1 (en) 2012-08-17 2016-01-15 霍夫曼-拉罗奇有限公司 Combination therapies for melanoma comprising administering cobimetinib and vemurafinib
WO2014047330A1 (en) * 2012-09-19 2014-03-27 Jean-Michel Vernier Novel raf kinase inhibitors
RU2015121367A (ru) * 2012-11-08 2017-01-10 Новартис Аг Фармацевтическая комбинация, содержащая ингибитор b-raf и ингибитор деацетилазы гистонов, и ее применение при лечении пролиферативных заболеваний
UA118846C2 (uk) 2013-03-21 2019-03-25 Новартіс Аг Комбінована терапія
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
US10570204B2 (en) 2013-09-26 2020-02-25 The Medical College Of Wisconsin, 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
MX384721B (es) * 2013-12-20 2025-03-14 Biomed Valley Discoveries Inc Tratamiento del cáncer usando combinaciones de inhibidores de erk y raf.
CN105848682A (zh) * 2013-12-23 2016-08-10 诺华股份有限公司 药物组合
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
KR20220126813A (ko) 2014-03-14 2022-09-16 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
US10428387B2 (en) 2014-05-16 2019-10-01 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
WO2016038582A1 (en) * 2014-09-12 2016-03-17 Novartis Ag Compounds and compositions as raf kinase inhibitors
EP3925622A1 (en) 2014-09-13 2021-12-22 Novartis AG Combination therapies
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
EP3206711B1 (en) 2014-10-14 2023-05-31 Novartis AG Antibody molecules to pd-l1 and uses thereof
AR103894A1 (es) 2015-03-10 2017-06-14 Aduro Biotech Inc Composiciones y métodos para activar la señalización dependiente del estimulador del gen interferón
US20180207273A1 (en) 2015-07-29 2018-07-26 Novartis Ag Combination therapies comprising antibody molecules to tim-3
WO2017019894A1 (en) 2015-07-29 2017-02-02 Novartis Ag Combination therapies comprising antibody molecules to lag-3
EP3328418A1 (en) 2015-07-29 2018-06-06 Novartis AG Combination therapies comprising antibody molecules to pd-1
EA201891093A1 (ru) 2015-11-03 2018-10-31 Янссен Байотек, Инк. Антитела, специфически связывающие pd-1, и их применение
EP3389712B1 (en) 2015-12-17 2024-04-10 Novartis AG Antibody molecules to pd-1 and uses thereof
RU2729518C2 (ru) 2015-12-30 2020-08-07 Сент-Луис Юниверсити Мета-азациклические производные аминобензойной кислоты в качестве антагонистов пан-интегрина
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
PL3463345T3 (pl) 2016-06-03 2023-02-06 Array Biopharma Inc. Kombinacje farmaceutyczne
WO2018009466A1 (en) 2016-07-05 2018-01-11 Aduro Biotech, Inc. Locked nucleic acid cyclic dinucleotide compounds and uses thereof
WO2018124001A1 (ja) 2016-12-27 2018-07-05 国立研究開発法人理化学研究所 Bmpシグナル阻害化合物
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
US11725185B2 (en) 2017-12-28 2023-08-15 University Of Houston System Stem cell culture systems for columnar epithelial stem cells, and uses related thereto
US12398209B2 (en) 2018-01-22 2025-08-26 Janssen Biotech, Inc. Methods of treating cancers with antagonistic anti-PD-1 antibodies
EP3816162A4 (en) * 2018-07-12 2021-08-11 Shenzhen TargetRx, Inc. DIARYL PYRAZOLE COMPOUND, COMPOSITION THEREOF, AND USE THEREOF
WO2020124397A1 (en) * 2018-12-19 2020-06-25 Inventisbio Shanghai Ltd. C-terminal src kinase inhibitors
JPWO2020130125A1 (ja) 2018-12-21 2021-11-04 第一三共株式会社 抗体−薬物コンジュゲートとキナーゼ阻害剤の組み合わせ
WO2020231976A1 (en) 2019-05-16 2020-11-19 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
KR20220131229A (ko) 2019-12-05 2022-09-27 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) N-(3-(5-(피리미딘-4-일)티아졸-4-일)페닐)설폰아미드 화합물 및 이의 용도
JP7312335B2 (ja) 2020-06-09 2023-07-20 アレイ バイオファーマ インコーポレイテッド Braf関連疾患および障害を処置するための4-オキソ-3,4-ジヒドロキナゾリノン化合物
EP4196228A1 (en) 2020-08-13 2023-06-21 Albert Einstein College of Medicine N-cyclyl-sulfonamides useful for inhibiting raf
MX2023003867A (es) 2020-10-05 2023-04-18 Pf Medicament Combinacion de encorafenib y binimetinib a manera de tratamiento adyuvante contra melanoma resecado en etapa ii.
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
KR20240008410A (ko) 2021-06-09 2024-01-18 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
WO2024163166A1 (en) * 2023-01-30 2024-08-08 5Metis, Inc. Boron containing compounds and their uses
AU2023439518A1 (en) 2023-04-06 2025-08-28 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
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
JP2000511419A (ja) 1996-05-23 2000-09-05 アプライド・リサーチ・システムズ・エイアールエス・ホールディング・ナムローゼ・フェンノートシャップ Raf―1または14―3―3タンパク質のIL―2受容体β鎖への結合を阻害する化合物およびそれを含有する医薬組成物
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
CA2291115A1 (en) 1997-05-22 1998-11-26 G.D. Searle & Co. 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
RU2319693C9 (ru) 1999-01-13 2008-08-20 Байер Копэрейшн Производные мочевины (варианты), фармацевтическая композиция (варианты) и способ лечения заболевания, связанного с ростом раковых клеток (варианты)
US6316435B2 (en) 1999-02-24 2001-11-13 Supergen, Inc. Combination therapy for lymphoproliferative diseases
EP2415462A1 (en) 1999-12-23 2012-02-08 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)
PT1441714E (pt) 2001-10-25 2008-03-10 Novartis Ag Combinações compreendendo um inibidor selectivo da ciclo-oxigenase 2
DE60222804T2 (de) 2001-12-21 2008-07-03 Vernalis (Cambridge) Ltd., Abington 3-(2,4)dihydroxyphenyl-4-phenylpyrazole und deren medizinische verwendung
IL163995A0 (en) 2002-03-13 2005-12-18 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
EP1692113B1 (en) 2003-11-14 2017-09-27 Lorus Therapeutics Inc. Aryl imidazoles and their use as anti-cancer agents
CA2551948A1 (en) 2004-01-09 2005-07-28 Novartis Ag Phenyl-[4-(3-phenyl-1h-pyrazol-4-yl)-pyrimidin-2-yl]-amine derivatives as igf-ir inhibitors
BRPI0511978A (pt) 2004-06-10 2008-01-22 Irm Llc compostos e composições como inibidores de proteìnas quinases
US20060058311A1 (en) 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
JP2008533172A (ja) 2005-03-17 2008-08-21 ノバルティス アクチエンゲゼルシャフト チロシン/スレオニンキナーゼ阻害剤、特にB−RAFキナーゼ阻害剤としての、N−[3−(1−アミノ−5,6,7,8−テトラヒドロ−2,4,4b−トリアザフルオレン−9−イル)−フェニル]ベンズアミド
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
CA2618377A1 (en) 2005-08-12 2007-02-22 Synta Pharmaceuticals Corp. 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
EP1917258A2 (en) 2005-08-26 2008-05-07 SmithKline Beecham Corporation Pyrimidinyl-pyrazole inhibitors of aurora kinases
PE20070335A1 (es) 2005-08-30 2007-04-21 Novartis Ag Benzimidazoles sustituidos y metodos para su preparacion
WO2007105058A2 (en) * 2006-03-16 2007-09-20 Pfizer Products Inc. Pyrazole compounds
RU2008143554A (ru) 2006-04-05 2010-05-10 Новартис АГ (CH) Комбинации терапевтических агентов для лечения рака
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
JP2010503717A (ja) 2006-09-18 2010-02-04 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 Egfr変異を有する腫瘍を治療するための方法
KR101101675B1 (ko) 2006-10-02 2011-12-30 노파르티스 아게 단백질 키나제 억제제로서의 화합물 및 조성물
CA2664147A1 (en) * 2006-10-06 2008-04-17 Irm Llc Protein kinase inhibitors and methods for using thereof
MX2009008584A (es) 2007-02-15 2009-08-18 Novartis Ag Combinacion de lbh589 con otros agentes terapeuticos para el tratamiento de cancer.
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
PA8800101A1 (es) 2007-10-19 2009-05-15 Abbott Gmbh & Co Kg Producto de dispersion sólida que contiene un compuesto a base de n-aril urea
ES2637794T3 (es) * 2007-11-14 2017-10-17 Janssen Pharmaceuticals, Inc. Derivados de imidazo[1,2-A]piridina y su uso como moduladores alostéricos positivos de receptores MGLUR2
AU2009227013B2 (en) * 2008-03-21 2013-01-10 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
US8088771B2 (en) 2008-07-28 2012-01-03 Gilead Sciences, Inc. Cycloalkylidene and heterocycloalkylidene inhibitor compounds
MX2011003292A (es) 2008-09-29 2011-04-21 Boehringer Ingelheim Int Compuestos antiproliferativos.
HUE030800T2 (en) 2008-10-07 2017-05-29 Astrazeneca Uk Ltd Pharmaceutical Form No. 514
WO2010056662A1 (en) * 2008-11-11 2010-05-20 University Of Washington 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
AR077975A1 (es) 2009-08-28 2011-10-05 Irm Llc Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina
US8242260B2 (en) 2009-08-28 2012-08-14 Novartis Ag Compounds and compositions as protein kinase inhibitors
JP5806239B2 (ja) 2010-01-27 2015-11-10 ネルヴィアーノ・メディカル・サイエンシズ・ソチエタ・ア・レスポンサビリタ・リミタータ プロテインキナーゼ阻害剤としての3,4−ジアリールピラゾールのスルホンアミド誘導体
RU2639876C2 (ru) 2010-03-30 2017-12-25 Версеон Корпорейшн Мультизамещенные ароматические соединения в качестве ингибиторов тромбина
US9114137B2 (en) 2010-08-03 2015-08-25 Nerviano Medical Sciences S.R.L. Derivatives of pyrazolophenyl-benzenesulfonamide compounds and use thereof as antitumor agents
US20140093565A1 (en) 2011-03-21 2014-04-03 Valcuria Ab A pharmaceutical composition comprising a hdac inhibitor and a steroid and the use thereof
SG195141A1 (en) 2011-06-14 2013-12-30 Novartis Ag Combination of panobinostat and ruxolitinib in the treatment of cancer suchas a myeloproliferative neoplasm
CA2855243C (en) 2011-11-11 2020-04-14 Novartis Ag Method of treating a proliferative disease
PT2782557T (pt) 2011-11-23 2018-11-26 Array Biopharma Inc Formulações farmacêuticas
RU2015121367A (ru) 2012-11-08 2017-01-10 Новартис Аг Фармацевтическая комбинация, содержащая ингибитор b-raf и ингибитор деацетилазы гистонов, и ее применение при лечении пролиферативных заболеваний
US10576680B2 (en) 2015-11-19 2020-03-03 The Boeing Company Modular thermoforming system

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