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
Links
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 4
- 208000035475 disorder Diseases 0.000 title abstract 3
- 206010005003 Bladder cancer Diseases 0.000 title abstract 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 title abstract 2
- 206010028980 Neoplasm Diseases 0.000 title abstract 2
- 206010060862 Prostate cancer Diseases 0.000 title abstract 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 title abstract 2
- 208000024770 Thyroid neoplasm Diseases 0.000 title abstract 2
- 201000001531 bladder carcinoma Diseases 0.000 title abstract 2
- 201000011510 cancer Diseases 0.000 title abstract 2
- 208000021045 exocrine pancreatic carcinoma Diseases 0.000 title abstract 2
- 201000001441 melanoma Diseases 0.000 title abstract 2
- 208000008443 pancreatic carcinoma Diseases 0.000 title abstract 2
- 239000008194 pharmaceutical composition Chemical class 0.000 title abstract 2
- 201000002510 thyroid cancer Diseases 0.000 title abstract 2
- 208000010570 urinary bladder carcinoma Diseases 0.000 title abstract 2
- 208000003200 Adenoma Diseases 0.000 title 1
- 206010009944 Colon cancer Diseases 0.000 title 1
- 150000002391 heterocyclic compounds Chemical class 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 201000007270 liver cancer Diseases 0.000 title 1
- 208000014018 liver neoplasm Diseases 0.000 title 1
- 201000005296 lung carcinoma Diseases 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 150000003230 pyrimidines Chemical class 0.000 title 1
- 230000002159 abnormal effect Effects 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 2
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 102000018471 Proto-Oncogene Proteins B-raf Human genes 0.000 abstract 1
- 108010091528 Proto-Oncogene Proteins B-raf Proteins 0.000 abstract 1
- 210000001072 colon Anatomy 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 230000001105 regulatory effect Effects 0.000 abstract 1
Classifications
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- 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)
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)
Families Citing this family (67)
| 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 |
| 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 |
| MX354725B (es) | 2011-11-11 | 2018-03-16 | Novartis Ag | Metodo de tratamiento de una enfermedad proliferativa. |
| UA115039C2 (uk) * | 2011-11-23 | 2017-09-11 | Еррей Біофарма Інк. | Фармацевтичні композиції |
| 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 |
| EP3333575B1 (en) | 2012-03-28 | 2020-02-26 | Dana Farber Cancer Institute, Inc. | C-raf mutants that confer resistance to raf inhibitors |
| US8716226B2 (en) | 2012-07-18 | 2014-05-06 | Saint Louis University | 3,5 phenyl-substituted beta amino acid derivatives as integrin antagonists |
| CA2878469A1 (en) | 2012-07-18 | 2014-01-23 | Saint Louis University | 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 |
| US11087354B2 (en) | 2012-08-17 | 2021-08-10 | Genentech, Inc. | Combination therapies |
| WO2014047330A1 (en) * | 2012-09-19 | 2014-03-27 | Jean-Michel Vernier | Novel raf kinase inhibitors |
| EP2916834A1 (en) | 2012-11-08 | 2015-09-16 | Novartis AG | Pharmaceutical combination comprising a b-raf inhibitor and a histone deacetylase inhibitor and their use in the treatment of proliferative diseases |
| 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 |
| US9873700B2 (en) | 2013-05-30 | 2018-01-23 | Plexxikon Inc. | Compounds for kinase modulation, and indications therefor |
| EP3757130A1 (en) | 2013-09-26 | 2020-12-30 | 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 |
| BR112016012506A8 (pt) * | 2013-12-23 | 2018-01-30 | Novartis Ag | combinações farmacêuticas, seus usos, e uso de um portador de dados |
| 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 |
| JP6576962B2 (ja) | 2014-03-14 | 2019-09-18 | ノバルティス アーゲー | Ｌａｇ−３に対する抗体分子およびその使用 |
| WO2015145388A2 (en) | 2014-03-27 | 2015-10-01 | Novartis Ag | Methods of treating colorectal cancers harboring upstream wnt pathway mutations |
| WO2015175846A2 (en) * | 2014-05-16 | 2015-11-19 | University Of Massachusetts | Treating chronic myelogenous leukemia (cml) |
| US20170114323A1 (en) | 2014-06-19 | 2017-04-27 | 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 |
| US9993551B2 (en) | 2014-09-13 | 2018-06-12 | Novartis Ag | Combination therapies of EGFR inhibitors |
| CN107106687A (zh) | 2014-10-03 | 2017-08-29 | 诺华股份有限公司 | 组合治疗 |
| 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 |
| US9988452B2 (en) | 2014-10-14 | 2018-06-05 | Novartis Ag | Antibody molecules to PD-L1 and uses thereof |
| BR112017018908A2 (pt) | 2015-03-10 | 2018-04-17 | Aduro Biotech, Inc. | composições e métodos para ativar a sinalização dependente do "estimulador do gene de interferon |
| CN108025051B (zh) | 2015-07-29 | 2021-12-24 | 诺华股份有限公司 | 包含抗pd-1抗体分子的联合疗法 |
| US20180207273A1 (en) | 2015-07-29 | 2018-07-26 | 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 |
| SI3370768T1 (sl) | 2015-11-03 | 2022-04-29 | Janssen Biotech, Inc. | Protitelesa, ki se specifično vežejo na PD-1, in njihove uporabe |
| WO2017106656A1 (en) | 2015-12-17 | 2017-06-22 | Novartis Ag | Antibody molecules to pd-1 and uses thereof |
| JP2019500355A (ja) | 2015-12-30 | 2019-01-10 | セントルイス ユニバーシティ | 汎インテグリンアンタゴニストとしてのメタ−アザ環式アミノ安息香酸誘導体 |
| 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 |
| CA3026361A1 (en) * | 2016-06-03 | 2017-12-07 | Giordano Caponigro | Pharmaceutical combinations |
| WO2018009466A1 (en) | 2016-07-05 | 2018-01-11 | Aduro Biotech, Inc. | Locked nucleic acid cyclic dinucleotide compounds and uses thereof |
| CA3048376A1 (en) * | 2016-12-27 | 2018-07-05 | 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 |
| CA3086765A1 (en) | 2017-12-28 | 2019-07-04 | Tract Pharmaceuticals, Inc. | 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 |
| JP7262843B2 (ja) * | 2018-07-12 | 2023-04-24 | 深▲チェン▼市塔吉瑞生物医薬有限公司 | ジアリールピラゾール化合物、該化合物を含む組成物およびその使用 |
| WO2020124397A1 (en) * | 2018-12-19 | 2020-06-25 | Inventisbio Shanghai Ltd. | C-terminal src kinase inhibitors |
| KR20210107069A (ko) | 2018-12-21 | 2021-08-31 | 다이이찌 산쿄 가부시키가이샤 | 항체-약물 컨쥬게이트와 키나아제 저해제의 조합 |
| US20220168250A1 (en) | 2019-05-16 | 2022-06-02 | 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 BRAFv6ooE COLORECTAL CANCER |
| EP4069692A1 (en) | 2019-12-05 | 2022-10-12 | Institut National de la Santé et de la Recherche Médicale (INSERM) | N-(3-(5-(pyrimidin-4-yl)thiazol-4-yl)phenyl)sulfonamide compounds and their uses as braf inhibitors |
| TW202426436A (zh) | 2020-06-09 | 2024-07-01 | 美商艾瑞生藥股份有限公司 | 用於治療ｂｒａｆ相關的疾病和病症之化合物 |
| US20230303551A1 (en) | 2020-08-13 | 2023-09-28 | 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 |
| WO2022195551A1 (en) | 2021-03-18 | 2022-09-22 | Novartis Ag | Biomarkers for cancer and methods of use thereof |
| 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 |
| CN114181197B (zh) * | 2022-02-16 | 2022-05-06 | 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 |
| 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)
| 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 |
| 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 |
| AU728701B2 (en) | 1996-05-23 | 2001-01-18 | Applied Research Systems Ars Holding N.V. | Compounds that inhibit the binding of Raf-1 or 14-3-3 proteins to the beta chain of IL-2 receptor, and pharmaceutical compositions containing same |
| 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 |
| AU754830C (en) | 1997-05-22 | 2004-02-12 | G.D. Searle Llc | 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 |
| AU782469B2 (en) | 1999-12-23 | 2005-08-04 | Mayne Pharma International Pty Ltd | Improved pharmaceutical compositions for poorly soluble drugs |
| 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) |
| RU2333754C2 (ru) | 2001-10-25 | 2008-09-20 | Новартис Аг | Композиции, содержащие избирательный ингибитор циклооксигеназы-2 |
| EP1456180B1 (en) | 2001-12-21 | 2007-10-03 | Vernalis (Cambridge) Limited | 3-(2,4)dihydroxyphenyl-4-phenylpyrazoles and their medical use |
| TWI338685B (en) | 2002-03-13 | 2011-03-11 | Array Biopharma Inc | N3 alkylated benzimid azole 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 |
| EP1706400A1 (en) | 2004-01-09 | 2006-10-04 | Novartis AG | Phenyl- 4-(3-phenyl-1h-pyrazol-4-yl)-pyrimidin-2-yl -amine derivatives as igf-ir inhibitors |
| CA2567662C (en) | 2004-06-10 | 2012-11-27 | 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 |
| AU2006279794B2 (en) | 2005-08-12 | 2011-04-07 | Synta Pharmaceuticals Corp. | Pyrazole compounds that modulate HSP90 activity |
| BRPI0614870A2 (pt) | 2005-08-22 | 2011-04-19 | Novartis Ag | composições farmacêuticas |
| US20080242667A1 (en) | 2005-08-26 | 2008-10-02 | Smithkline Beecham Corporation | Pyrimidinyl-Pyrazole Inhibitors of Aurora Kinases |
| TW200804345A (en) | 2005-08-30 | 2008-01-16 | Novartis Ag | Substituted benzimidazoles and methods of preparation |
| WO2007105058A2 (en) * | 2006-03-16 | 2007-09-20 | Pfizer Products Inc. | Pyrazole compounds |
| MX2008012716A (es) | 2006-04-05 | 2008-10-14 | Novartis Ag | Combinaciones de agentes terapeuticos para el tratamiento de cancer. |
| WO2007123892A2 (en) * | 2006-04-17 | 2007-11-01 | Arqule Inc. | Raf inhibitors and their uses |
| AU2007296744A1 (en) | 2006-09-11 | 2008-03-20 | Curis, Inc. | Multi-functional small molecules as anti-proliferative agents |
| US8877764B2 (en) | 2006-09-18 | 2014-11-04 | 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 |
| AR065335A1 (es) | 2007-02-15 | 2009-06-03 | Novartis Ag | Combinaciones de agentes terapeuticos para el tratamiento de cancer |
| US20090022789A1 (en) | 2007-07-18 | 2009-01-22 | Supernus Pharmaceuticals, Inc. | Enhanced formulations of lamotrigine |
| BRPI0815042A2 (pt) * | 2007-08-01 | 2015-02-10 | Pfizer | Compostos de pirazol |
| KR20100087170A (ko) | 2007-10-19 | 2010-08-03 | 애보트 게엠베하 운트 콤파니 카게 | Ｎ-아릴 우레아계 약물의 고체 분산액 생성물 |
| 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 |
| JP5384611B2 (ja) | 2008-03-21 | 2014-01-08 | ノバルティス アーゲー | 新規ヘテロ環式化合物およびそれらの使用 |
| 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 |
| CN102123987A (zh) | 2008-07-28 | 2011-07-13 | 吉里德科学公司 | 亚环烷基和亚杂环烷基组蛋白脱乙酰酶抑制剂化合物 |
| TW201018670A (en) | 2008-09-29 | 2010-05-16 | Boehringer Ingelheim Int | New chemical compounds |
| EA020783B1 (ru) | 2008-10-07 | 2015-01-30 | Астразенека Юк Лимитед | Фармацевтическая композиция, содержащая 4-[3-(4-циклопропанкарбонилпиперазин-1-карбонил)-4-фторбензил]-2н-фталазин-1-он и коповидон |
| 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 |
| CN102947290B (zh) | 2010-01-27 | 2015-05-27 | 内尔维安诺医学科学有限公司 | 作为蛋白激酶抑制剂的3,4-二芳基吡唑的亚磺酰氨基衍生物 |
| SG10201502484SA (en) | 2010-03-30 | 2015-05-28 | Verseon Corp | Multisubstituted aromatic compounds as inhibitors of thrombin |
| EP2601185B1 (en) | 2010-08-03 | 2015-10-07 | 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 |
| JP6200884B2 (ja) | 2011-06-14 | 2017-09-20 | ノバルティス アーゲー | 骨髄増殖性腫瘍などの癌の治療におけるパノビノスタットおよびルキソリチニブの組合せ |
| MX354725B (es) | 2011-11-11 | 2018-03-16 | Novartis Ag | Metodo de tratamiento de una enfermedad proliferativa. |
| UA115039C2 (uk) | 2011-11-23 | 2017-09-11 | Еррей Біофарма Інк. | Фармацевтичні композиції |
| EP2916834A1 (en) | 2012-11-08 | 2015-09-16 | Novartis AG | Pharmaceutical combination comprising a b-raf inhibitor and a histone deacetylase inhibitor and their use in the treatment of proliferative diseases |
| US10576680B2 (en) | 2015-11-19 | 2020-03-03 | The Boeing Company | Modular thermoforming system |
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