AR077975A1 - Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina - Google Patents
Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteinaInfo
- Publication number
- AR077975A1 AR077975A1 ARP100103123A ARP100103123A AR077975A1 AR 077975 A1 AR077975 A1 AR 077975A1 AR P100103123 A ARP100103123 A AR P100103123A AR P100103123 A ARP100103123 A AR P100103123A AR 077975 A1 AR077975 A1 AR 077975A1
- Authority
- AR
- Argentina
- Prior art keywords
- carbon atoms
- alkyl
- halogen
- alkoxy
- hydrogen
- Prior art date
Links
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical class C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 239000003909 protein kinase inhibitor Substances 0.000 title 1
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 title 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 18
- 125000000217 alkyl group Chemical group 0.000 abstract 10
- 229910052736 halogen Inorganic materials 0.000 abstract 9
- 150000002367 halogens Chemical group 0.000 abstract 9
- 125000003545 alkoxy group Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 230000002159 abnormal effect Effects 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000035475 disorder Diseases 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- -1 cyano, hydroxyl Chemical group 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 230000001105 regulatory effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 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)
- 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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (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 |
|---|---|
| AR077975A1 true AR077975A1 (es) | 2011-10-05 |
Family
ID=42782253
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100103123A AR077975A1 (es) | 2009-08-28 | 2010-08-26 | Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina |
Country Status (49)
Families Citing this family (68)
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| JO3002B1 (ar) | 2009-08-28 | 2016-09-05 | Irm Llc | مركبات و تركيبات كمثبطات كيناز بروتين |
| CA2789696C (en) | 2010-02-25 | 2017-11-07 | Dana-Farber Cancer Institute, Inc. | Braf mutations conferring resistance to braf inhibitors |
| US8907270B2 (en) | 2010-06-30 | 2014-12-09 | Schlumberger Technology Corporation | Method and apparatus for gain regulation in a gamma detector |
| CN103917236A (zh) * | 2011-11-11 | 2014-07-09 | 诺华股份有限公司 | 治疗增生性疾病的方法 |
| BR112014011981B8 (pt) * | 2011-11-23 | 2022-07-19 | Novartis Ag | Formulações farmacêuticas sólidas orais, seus processos de preparação e usos |
| 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 |
| EP2793879A4 (en) * | 2011-12-23 | 2015-07-01 | Millennium Pharm Inc | HETEROARYLE AND USES THEREOF |
| EA028135B1 (ru) | 2012-03-28 | 2017-10-31 | Дана-Фарбер Кэнсер Инститьют, Инк. | Мутанты c-raf, придающие резистентность к ингибиторам raf |
| CA2878469A1 (en) | 2012-07-18 | 2014-01-23 | 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 |
| JP6342396B2 (ja) * | 2012-08-07 | 2018-06-13 | ノバルティス アーゲー | Ｂ−Ｒａｆ阻害薬、ＥＧＦＲ阻害薬及び場合によってはＰＩ３Ｋ−α阻害薬を含む組合せ医薬 |
| EP2884979B1 (en) | 2012-08-17 | 2019-06-26 | F.Hoffmann-La Roche Ag | Combination therapies for melanoma comprising administering cobimetinib and vemurafinib |
| WO2014047330A1 (en) * | 2012-09-19 | 2014-03-27 | Jean-Michel Vernier | Novel raf kinase inhibitors |
| BR112015010477A2 (pt) * | 2012-11-08 | 2017-07-11 | Novartis Ag | combinação farmacêutica que compreende um inibidor b-raf e um inibidor de histona desacetilase e o uso dos mesmos no tratamento de doenças proliferativas |
| AU2014233805B2 (en) * | 2013-03-21 | 2018-10-18 | Array Biopharma Inc. | Combination therapy comprising a B-Raf inhibitor and a second inhibitor |
| 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 |
| KR20160013028A (ko) | 2013-05-30 | 2016-02-03 | 플렉시콘, 인코퍼레이티드 | 키나제 조정을 위한 화합물 및 그에 대한 적응증 |
| 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 |
| JP6678585B2 (ja) * | 2013-12-20 | 2020-04-22 | バイオメッド バレー ディスカバリーズ，インコーポレイティド | Ｅｒｋ阻害剤およびｒａｆ阻害剤の組み合わせを使用するがん処置 |
| CA2934866A1 (en) * | 2013-12-23 | 2015-07-02 | Novartis Ag | Pharmaceutical combinations |
| JOP20200094A1 (ar) | 2014-01-24 | 2017-06-16 | Dana Farber Cancer Inst Inc | جزيئات جسم مضاد لـ pd-1 واستخداماتها |
| JOP20200096A1 (ar) | 2014-01-31 | 2017-06-16 | Children’S Medical Center Corp | جزيئات جسم مضاد لـ tim-3 واستخداماتها |
| DE102015103158A1 (de) | 2014-03-04 | 2015-09-10 | Bergische Universität Wuppertal | Verbindungen für die Behandlung des Melanoms |
| US20150259420A1 (en) | 2014-03-14 | 2015-09-17 | Novartis Ag | Antibody molecules to lag-3 and uses thereof |
| WO2015145388A2 (en) | 2014-03-27 | 2015-10-01 | Novartis Ag | Methods of treating colorectal cancers harboring upstream wnt pathway mutations |
| EP3143166A4 (en) * | 2014-05-16 | 2018-04-18 | University of Massachusetts | Treating chronic myelogenous leukemia (cml) |
| WO2015196072A2 (en) | 2014-06-19 | 2015-12-23 | Whitehead Institute For Biomedical Research | Uses of kinase inhibitors for inducing and maintaining pluripotency |
| US10167279B2 (en) * | 2014-09-12 | 2019-01-01 | Novartis Ag | Compounds and compositions as RAF kinase inhibitors |
| US20170281624A1 (en) | 2014-09-13 | 2017-10-05 | Novartis Ag | Combination therapies of alk inhibitors |
| EP3662903A3 (en) | 2014-10-03 | 2020-10-14 | Novartis AG | Combination therapies |
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| JP6805336B2 (ja) | 2016-06-03 | 2020-12-23 | アレイ バイオファーマ、インコーポレイテッド | 薬学的組み合わせ |
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| US10954216B2 (en) | 2016-12-27 | 2021-03-23 | Riken | BMP-signal-inhibiting compound |
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