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
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Otolaryngology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (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)
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 |
WO2013070996A1 (en) | 2011-11-11 | 2013-05-16 | Novartis Ag | Method of treating a proliferative disease |
AU2012340759C1 (en) * | 2011-11-23 | 2019-11-28 | Array Biopharma Inc. | Pharmaceutical formulations |
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 |
ES2908078T3 (es) | 2012-03-28 | 2022-04-27 | Dana Farber Cancer Inst Inc | Usos médicos que implican mutantes C-RAF que confieren resistencia a los inhibidores de RAF |
AU2013292580B2 (en) | 2012-07-18 | 2017-07-20 | 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 |
IN2015DN00450A (enEXAMPLES) * | 2012-08-07 | 2015-06-26 | Novartis Ag | |
LT2884979T (lt) | 2012-08-17 | 2019-09-10 | F. Hoffmann-La Roche Ag | Kombinuoti melanomos gydymo būdai, apimantys kobimetinibo ir vemurafenibo skyrimą |
US20150232452A1 (en) * | 2012-09-19 | 2015-08-20 | Ruga Corporation | 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 |
BR112015028845A2 (pt) | 2013-05-30 | 2017-07-25 | Plexxikon Inc | compostos para a modulação da quinase e indicações da mesma |
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 |
ES2909910T3 (es) * | 2013-12-20 | 2022-05-10 | Biomed Valley Discoveries Inc | Tratamiento contra el cáncer usando combinaciones de inhibidores de ERK y RAF |
MX2016008362A (es) * | 2013-12-23 | 2016-09-08 | Novartis Ag | Combinaciones farmaceuticas. |
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 |
DK3116909T3 (da) | 2014-03-14 | 2020-01-20 | Novartis Ag | Antistofmolekyler til lag-3 og anvendelser deraf |
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 |
US10167279B2 (en) * | 2014-09-12 | 2019-01-01 | Novartis Ag | Compounds and compositions as RAF kinase inhibitors |
US11344620B2 (en) | 2014-09-13 | 2022-05-31 | Novartis Ag | Combination therapies |
EP3200775B1 (en) | 2014-10-03 | 2019-11-20 | Novartis AG | Combination therapies |
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 |
MX2017011597A (es) | 2015-03-10 | 2018-05-11 | Aduro Biotech Inc | Composiciones y metodos para activar la señalizacion dependiente del "estimulador del gen 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 |
WO2017019897A1 (en) | 2015-07-29 | 2017-02-02 | Novartis Ag | Combination therapies comprising antibody molecules to tim-3 |
DK3317301T3 (da) | 2015-07-29 | 2021-06-28 | Immutep Sas | Kombinationsterapier omfattende antistofmolekyler mod lag-3 |
MA43186B1 (fr) | 2015-11-03 | 2022-03-31 | Janssen Biotech Inc | Anticorps se liant spécifiquement à pd-1 et leurs utilisations |
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 |
EP3738953A1 (en) | 2015-12-30 | 2020-11-18 | Saint Louis University | Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists with improved pharmacokinetic properties and methods for their manufacture |
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 |
SI3463345T1 (sl) | 2016-06-03 | 2023-02-28 | Array Biopharma Inc. | Farmacevtski sestavki |
WO2018009466A1 (en) | 2016-07-05 | 2018-01-11 | Aduro Biotech, Inc. | Locked nucleic acid cyclic dinucleotide compounds and uses thereof |
JP7076741B2 (ja) | 2016-12-27 | 2022-05-30 | 国立研究開発法人理化学研究所 | Bmpシグナル阻害化合物 |
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 |
WO2019133810A1 (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 |
SG11202106635WA (en) | 2018-12-21 | 2021-07-29 | Daiichi Sankyo Co Ltd | Combination of antibody-drug conjugate and kinase inhibitor |
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 |
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 |
PE20231651A1 (es) | 2020-06-09 | 2023-10-17 | Array Biopharma Inc | Compuestos para el tratamiento de enfermedades y trastornos asociados a braf |
EP4196228A1 (en) | 2020-08-13 | 2023-06-21 | 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 |
WO2022258612A1 (en) | 2021-06-09 | 2022-12-15 | F. Hoffmann-La Roche Ag | Combination therapy for cancer treatment |
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 |
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 |
JPH11514979A (ja) | 1995-09-07 | 1999-12-21 | フイズ テクノロジーズ リミテッド | 実質的に非溶解性の生体作用薬剤をバイオ・アベイラブルにするシステム |
US5717100A (en) | 1995-10-06 | 1998-02-10 | Merck & Co., Inc. | Substituted imidazoles having anti-cancer and cytokine inhibitory activity |
WO1997044058A1 (en) | 1996-05-23 | 1997-11-27 | 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 |
EP1000055A1 (en) | 1997-05-22 | 2000-05-17 | 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 |
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 |
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) |
DK1441714T3 (da) | 2001-10-25 | 2008-03-31 | Novartis Ag | Kombinationer omfattende en selektiv cyclooxygenase-2-inhibitor |
AU2002356301A1 (en) | 2001-12-21 | 2003-07-15 | Cancer Research Technology Ltd. | 3,4-diarylpyrazoles and their use in the therapy of cancer |
PL401637A1 (pl) | 2002-03-13 | 2013-05-27 | Array Biopharma Inc. | N3 alkilowane pochodne benzimidazolu jako inhibitory MEK |
EA200600495A1 (ru) | 2003-09-23 | 2006-10-27 | Новартис Аг | Комбинация ингибитора vegf рецептора с химиотерапевтическим агентом |
DK1692113T3 (en) | 2003-11-14 | 2018-01-08 | Lorus Therapeutics Inc | ARYLIMIDAZOLES AND USE THEREOF AS ANTICANCES |
CN1906188A (zh) | 2004-01-09 | 2007-01-31 | 诺瓦提斯公司 | 作为igf-1r抑制剂的苯基-[4-(3-苯基-1h-吡唑-4-基)-嘧啶-2-基]-胺衍生物 |
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 |
BRPI0606281A2 (pt) | 2005-03-17 | 2009-06-09 | Novartis Ag | compostos orgánicos |
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 |
CA2619035A1 (en) | 2005-08-22 | 2007-03-01 | Novartis Ag | Pharmaceutical compositions |
US20080242667A1 (en) | 2005-08-26 | 2008-10-02 | 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 |
EP2024353A2 (en) * | 2006-03-16 | 2009-02-18 | Pfizer Products Inc. | Pyrazole compounds |
KR20080108516A (ko) | 2006-04-05 | 2008-12-15 | 노파르티스 아게 | 암을 치료하기 위한 치료제의 조합물 |
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 |
WO2008034776A1 (en) | 2006-09-18 | 2008-03-27 | Boehringer Ingelheim International Gmbh | Method for treating cancer harboring egfr mutations |
MX2009003456A (es) | 2006-10-02 | 2009-04-14 | Irm Llc | Compuestos y composiciones como inhibidores de proteina cinasa. |
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 |
WO2008100985A2 (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 |
EA201000113A1 (ru) * | 2007-08-01 | 2010-08-30 | Пфайзер Инк. | Пиразольные соединения |
EP2197425A2 (en) | 2007-10-19 | 2010-06-23 | 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 |
BRPI0908906A2 (pt) * | 2008-03-21 | 2019-09-24 | Novartis Ag | compostos heterocíclicos e usos dos mesmos |
UA103319C2 (en) * | 2008-05-06 | 2013-10-10 | Глаксосмитклайн Ллк | Thiazole- and oxazole-benzene sulfonamide compounds |
EA019722B1 (ru) * | 2008-07-24 | 2014-05-30 | НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. | 3,4-диарилпиразолы в качестве ингибиторов протеинкиназ |
KR20110038159A (ko) | 2008-07-28 | 2011-04-13 | 길리애드 사이언시즈, 인코포레이티드 | 사이클로알킬리덴 및 헤테로사이클로알킬리덴 히스톤 데아세틸라아제 억제제 화합물 |
AR073700A1 (es) | 2008-09-29 | 2010-11-24 | Boehringer Ingelheim Int | Heterociclos y composiciones farmaceuticas para usarse en el tratamiento de cancer, infecciones y enfermedades autoinmunitarias |
CA2737400C (en) | 2008-10-07 | 2016-11-22 | Astrazeneca Uk Limited | Pharmaceutical formulation 514 |
US20110293750A1 (en) * | 2008-11-11 | 2011-12-01 | Yale University | Activated wnt-beta-catenin signaling in melanoma |
WO2010070060A1 (en) | 2008-12-19 | 2010-06-24 | 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 |
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 |
EA023942B1 (ru) | 2010-01-27 | 2016-07-29 | НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. | Сульфонамидные производные 3,4-диарилпиразолов в качестве ингибиторов протеинкиназы |
SG10201502484SA (en) | 2010-03-30 | 2015-05-28 | Verseon Corp | Multisubstituted aromatic compounds as inhibitors of thrombin |
JP5938038B2 (ja) | 2010-08-03 | 2016-06-22 | 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 | ピラゾロフェニル−ベンゼンスルホンアミド化合物の誘導体及びその抗腫瘍薬としての使用 |
HUE032100T2 (en) | 2011-03-21 | 2017-08-28 | Valcuria Ab | A pharmaceutical composition comprising an HDAC inhibitor and a steroid and its use |
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 |
WO2013070996A1 (en) | 2011-11-11 | 2013-05-16 | Novartis Ag | Method of treating a proliferative disease |
AU2012340759C1 (en) | 2011-11-23 | 2019-11-28 | Array Biopharma Inc. | Pharmaceutical formulations |
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 |
-
2010
- 2010-08-26 AR ARP100103123A patent/AR077975A1/es active IP Right Grant
- 2010-08-26 JO JOP/2010/0297A patent/JO3002B1/ar active
- 2010-08-27 US US12/870,130 patent/US8501758B2/en not_active Ceased
- 2010-08-27 DK DK14152945.3T patent/DK2727918T3/da active
- 2010-08-27 SM SM20170036T patent/SMT201700036T1/it unknown
- 2010-08-27 WO PCT/US2010/046930 patent/WO2011025927A1/en active Application Filing
- 2010-08-27 SG SG10201405311TA patent/SG10201405311TA/en unknown
- 2010-08-27 PL PL14152945T patent/PL2727918T3/pl unknown
- 2010-08-27 HU HUE14152945A patent/HUE032847T2/hu unknown
- 2010-08-27 SG SG2012009304A patent/SG178351A1/en unknown
- 2010-08-27 ME MEP-2017-6A patent/ME02684B/me unknown
- 2010-08-27 LT LTEP14152945.3T patent/LT2727918T/lt unknown
- 2010-08-27 AU AU2010286569A patent/AU2010286569C1/en active Active
- 2010-08-27 EP EP14152945.3A patent/EP2727918B1/en active Active
- 2010-08-27 HR HRP20140799AT patent/HRP20140799T1/hr unknown
- 2010-08-27 UA UAA201203042A patent/UA112285C2/uk unknown
- 2010-08-27 UY UY0001032860A patent/UY32860A/es active IP Right Grant
- 2010-08-27 PL PL10748211T patent/PL2470526T3/pl unknown
- 2010-08-27 GE GEAP201012645A patent/GEP20146102B/en unknown
- 2010-08-27 SI SI201030711T patent/SI2470526T1/sl unknown
- 2010-08-27 EA EA201500175A patent/EA201500175A1/ru unknown
- 2010-08-27 CN CN201410040923.XA patent/CN103896921B/zh active Active
- 2010-08-27 DK DK10748211.9T patent/DK2470526T3/da active
- 2010-08-27 ES ES10748211.9T patent/ES2492499T3/es active Active
- 2010-08-27 CU CU2012000034A patent/CU24110B1/es active IP Right Grant
- 2010-08-27 ES ES14152945.3T patent/ES2610825T3/es active Active
- 2010-08-27 PT PT107482119T patent/PT2470526E/pt unknown
- 2010-08-27 PE PE2012000268A patent/PE20120861A1/es active IP Right Grant
- 2010-08-27 SI SI201031371A patent/SI2727918T1/sl unknown
- 2010-08-27 BR BR112012004453-2A patent/BR112012004453B1/pt active IP Right Grant
- 2010-08-27 KR KR1020127007860A patent/KR101413392B1/ko active Active
- 2010-08-27 RS RS20170017A patent/RS55568B1/sr unknown
- 2010-08-27 NZ NZ598924A patent/NZ598924A/xx unknown
- 2010-08-27 EA EA201200373A patent/EA025222B1/ru not_active IP Right Cessation
- 2010-08-27 RS RS20140430A patent/RS53489B1/en unknown
- 2010-08-27 CN CN201080038197.8A patent/CN102725283B/zh active Active
- 2010-08-27 JP JP2012527014A patent/JP5475888B2/ja active Active
- 2010-08-27 ME MEP-2014-94A patent/ME01860B/me unknown
- 2010-08-27 PT PT141529453T patent/PT2727918T/pt unknown
- 2010-08-27 EP EP10748211.9A patent/EP2470526B1/en active Active
- 2010-08-27 IN IN2469DEN2012 patent/IN2012DN02469A/en unknown
- 2010-08-27 CA CA2771775A patent/CA2771775C/en active Active
- 2010-08-27 MY MYPI2012000611A patent/MY156259A/en unknown
- 2010-08-27 MX MX2012002546A patent/MX2012002546A/es active IP Right Grant
-
2012
- 2012-02-09 CL CL2012000340A patent/CL2012000340A1/es unknown
- 2012-02-13 IL IL218084A patent/IL218084A/en active IP Right Grant
- 2012-02-17 TN TNP2012000081A patent/TN2012000081A1/en unknown
- 2012-02-24 CO CO12032570A patent/CO6612222A2/es active IP Right Grant
- 2012-02-24 DO DO2012000051A patent/DOP2012000051A/es unknown
- 2012-02-24 NI NI201200029A patent/NI201200029A/es unknown
- 2012-02-27 GT GT201200053A patent/GT201200053A/es unknown
- 2012-02-27 HN HN2012000441A patent/HN2012000441A/es unknown
- 2012-02-28 EC ECSP12011700 patent/ECSP12011700A/es unknown
- 2012-02-28 CR CR20120102A patent/CR20120102A/es unknown
- 2012-03-19 ZA ZA2012/02020A patent/ZA201202020B/en unknown
- 2012-03-23 MA MA34716A patent/MA33604B1/fr unknown
-
2013
- 2013-06-28 US US13/931,111 patent/US9314464B2/en active Active
-
2014
- 2014-02-06 JP JP2014021339A patent/JP6045519B2/ja active Active
- 2014-09-12 SM SM201400133T patent/SMT201400133B/xx unknown
-
2016
- 2016-01-13 US US14/994,710 patent/US9593099B2/en active Active
- 2016-01-13 US US14/994,827 patent/US9593100B2/en active Active
- 2016-03-15 US US15/070,905 patent/US10005761B2/en active Active
- 2016-06-10 US US15/179,385 patent/US9850229B2/en active Active
- 2016-06-10 US US15/179,644 patent/US9850230B2/en active Active
-
2017
- 2017-01-03 HR HRP20170005TT patent/HRP20170005T1/hr unknown
- 2017-01-10 CY CY20171100028T patent/CY1118452T1/el unknown
- 2017-01-19 SM SM201700036T patent/SMT201700036B/it unknown
- 2017-11-20 US US15/818,264 patent/US10568884B2/en active Active
- 2017-11-20 US US15/818,082 patent/US10576080B2/en active Active
-
2019
- 2019-02-12 LU LU00101C patent/LUC00101I2/fr unknown
- 2019-02-12 LU LU00102C patent/LUC00102I2/fr unknown
- 2019-03-01 HU HUS1900012C patent/HUS1900012I1/hu unknown
- 2019-03-01 HU HUS1900013C patent/HUS1900013I1/hu unknown
- 2019-03-05 NO NO2019012C patent/NO2019012I1/no unknown
- 2019-03-05 NO NO2019011C patent/NO2019011I1/no unknown
- 2019-03-07 LT LTPA2019005C patent/LTC2470526I2/lt unknown
- 2019-03-07 LT LTPA2019006C patent/LTPA2019006I1/lt unknown
- 2019-03-15 NL NL300973C patent/NL300973I2/nl unknown
- 2019-03-18 CY CY2019014C patent/CY2019014I1/el unknown
- 2019-03-18 CY CY2019013C patent/CY2019013I2/el unknown
-
2020
- 2020-01-14 US US16/741,937 patent/US20200323852A1/en not_active Abandoned
-
2021
- 2021-07-15 US US17/376,199 patent/USRE49556E1/en active Active
-
2022
- 2022-04-20 US US17/724,589 patent/US20230116233A1/en not_active Abandoned
-
2023
- 2023-01-27 EC ECSENADI20234573A patent/ECSP23004573A/es unknown
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
CL2012000340A1 (es) | 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. | |
CR20150368A (es) | Inhibidores de histona desmetilasa | |
GT200800202A (es) | Quinazolinas para la inhibicion de pdk1 | |
CR20110028A (es) | Derivados de pirimidina como inhibidores de cinasa | |
CL2012002189A1 (es) | Compuestos derivados de pirrolidina-2-carboxamidas sustituidas; inhibidores de la interaccion mdm2-p53; composicion farmaceutica; y su uso para el tratamiento del cancer, en particular de tumores solidos. | |
CL2010001637A1 (es) | Compuestos derivados de isoindolonas; composición farmacéutica que los comprende; y su uso como inhibidores de la quinasa mek para tratar enfermedades hiperproliferativas y/o inflamatorias tales como cáncer, artritis reumatoidea entre otras. | |
ECSP099445A (es) | Quinazolinas para la inhibición de pdk1 | |
CR11757A (es) | Compuestos de triazina como inhibidores mtor y quinasa pi3 | |
GT201000376A (es) | Compuestos organicos | |
UY33597A (es) | Compuestos y composiciones como inhibidores de la trk | |
CU20100170A7 (es) | Inhibidores heterocíclicos de estearoil-coa-desaturasa | |
CL2009000687A1 (es) | Compuestos derivados de heterociclos nitrogenados de imidazol, inhibidores de la actividad de cinasa raf; composicion farmaceutica; utiles para el tratamiento del cancer, tal como carcinoma de pulmon, pancreatico, de prostata, tiroides, entre otras. | |
ECSP088450A (es) | Derivados de pirimidina 4-(3-aminopirazol) para uso como inhibidores de tirosina quinasa en el tratamiento de cáncer | |
JO3366B1 (ar) | مثبطات بيرازوليل كوينوكزالين كاينيز | |
CO6761389A2 (es) | Inhibidores de nampt y rock | |
BR112012033253A2 (pt) | novos derivados de pirimidina fundidos para inibição da atividade de tirosina quinase | |
EA201100425A1 (ru) | Производные пиколинамида в качестве ингибиторов киназы | |
EA201170531A1 (ru) | Соединения на основе пиридина и пиримидина в качестве ингибиторов сигнального пути wnt для лечения рака | |
CL2011000691A1 (es) | Compuestos derivados de nicotinamida sustituida; composicion farmaceutica que los comprende; uso para el tratamiento y/o prevencion de cancer, infecciones, enfermedades inflamatorias y autoinmunitarias. | |
GT201200171A (es) | Derivados de fenilimidazol heteroaromáticos como inhibidores de enzima pde10a | |
CU20110113A7 (es) | Lactamas como inhibidores beta secretasa | |
CR20120502A (es) | Uso de nuevos inhibidores de pan-cdk para tratar tumores | |
ECSP12011837A (es) | Derivados de pirazol que modulan la estearoil-coa-desaturasa | |
CL2009000949A1 (es) | Compuestos derivados de 1,2,3,5-tetrahidro-indolizina, 6,7,8,9-tetrahidro-4h-quinolizina sustituidos, inhibidores de la actividad de cinasa de mek; su composicion farmaceutica; su uso para el tratamiento de enfermedades hiperproliferativas, tal como cancer e inflamaciones. | |
CL2011001850A1 (es) | Uso de un compuesto nitrogenado heterociclico sustituido para el tratamiento de cánceres tales como cáncer de colon o mieloma múltiple;composición farmacéutica que comprende al compuesto. |