MX339584B - Inhibidores de pi3 cinasa y usos de los mismos. - Google Patents
Inhibidores de pi3 cinasa y usos de los mismos.Info
- Publication number
- MX339584B MX339584B MX2012002972A MX2012002972A MX339584B MX 339584 B MX339584 B MX 339584B MX 2012002972 A MX2012002972 A MX 2012002972A MX 2012002972 A MX2012002972 A MX 2012002972A MX 339584 B MX339584 B MX 339584B
- Authority
- MX
- Mexico
- Prior art keywords
- kinase inhibitors
- compositions
- methods
- same
- present
- Prior art date
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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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/10—Transferases (2.)
- C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
- C12N9/1205—Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases
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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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Genetics & Genomics (AREA)
- Neurosurgery (AREA)
- Molecular Biology (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Physical Education & Sports Medicine (AREA)
- Microbiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Oncology (AREA)
- Biotechnology (AREA)
- Diabetes (AREA)
- General Engineering & Computer Science (AREA)
- Hematology (AREA)
- Biochemistry (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
Abstract
La presente invención se refiere a un conjugado caracterizado porque comprende una o más PI3 cinasas que tienen un residuo de cisteína, CysX, en donde el CysX se une covalente e irreversiblemente a un inhibidor, de tal manera que la inhibición de la PI3 cinasa es mantenida, en donde el inhibidor comprende, antes de la unión, un grupo funcional den forma de ojiva -L-Y capaz de unir covalentemente a Cysx. El compuesto para usarse en un método para inhibir una o más PI3 cinasas, o un mutante de las mismas, actividad en una muestra biológica. El compuesto para usarse en un método in vitro para inhibir una o más PI3 cinasas, o un mutante de las mismas.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US24094709P | 2009-09-09 | 2009-09-09 | |
US37139610P | 2010-08-06 | 2010-08-06 | |
PCT/US2010/048317 WO2011031896A2 (en) | 2009-09-09 | 2010-09-09 | Pi3 kinase inhibitors and uses thereof |
Publications (2)
Publication Number | Publication Date |
---|---|
MX2012002972A MX2012002972A (es) | 2012-06-25 |
MX339584B true MX339584B (es) | 2016-06-01 |
Family
ID=43733099
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2012002972A MX339584B (es) | 2009-09-09 | 2010-09-09 | Inhibidores de pi3 cinasa y usos de los mismos. |
Country Status (15)
Country | Link |
---|---|
US (1) | US20110230476A1 (es) |
EP (1) | EP2475375A4 (es) |
JP (1) | JP2013504325A (es) |
KR (1) | KR20120063515A (es) |
CN (1) | CN102625708A (es) |
AU (1) | AU2010292198A1 (es) |
BR (1) | BR112012008385A2 (es) |
CA (1) | CA2773848A1 (es) |
IL (1) | IL218555A0 (es) |
MX (1) | MX339584B (es) |
NZ (2) | NZ626650A (es) |
RU (1) | RU2595718C2 (es) |
SG (2) | SG10201405598QA (es) |
TW (2) | TW201609747A (es) |
WO (1) | WO2011031896A2 (es) |
Families Citing this family (121)
Publication number | Priority date | Publication date | Assignee | Title |
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JP5291616B2 (ja) * | 2006-04-26 | 2013-09-18 | ジェネンテック, インコーポレイテッド | ホスホイノシチド3−キナーゼ抑制剤化合物およびその使用方法 |
US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
KR101860057B1 (ko) | 2008-05-21 | 2018-05-21 | 어리어드 파마슈티칼스, 인코포레이티드 | 키나아제 억제제로서 포스포러스 유도체 |
SG179172A1 (en) | 2009-09-16 | 2012-04-27 | Avila Therapeutics Inc | Protein kinase conjugates and inhibitors |
US8946197B2 (en) | 2009-11-16 | 2015-02-03 | Chdi Foundation, Inc. | Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof |
AU2010339456A1 (en) | 2009-12-30 | 2012-07-05 | Celgene Avilomics Research, Inc. | Ligand-directed covalent modification of protein |
US9295673B2 (en) | 2011-02-23 | 2016-03-29 | Intellikine Llc | Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof |
CA2829558A1 (en) * | 2011-03-09 | 2012-09-13 | Celgene Avilomics Research, Inc. | Pi3 kinase inhibitors and uses thereof |
US9834518B2 (en) | 2011-05-04 | 2017-12-05 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
WO2012154608A1 (en) * | 2011-05-06 | 2012-11-15 | Intellikine, Llc | Reactive mtor and pi3 kinase inhibitors and uses thereof |
WO2012154610A1 (en) * | 2011-05-06 | 2012-11-15 | Intellikine, Llc | Reactive pi3k kinase inhibitors and uses thereof |
US8889716B2 (en) | 2011-05-10 | 2014-11-18 | Chdi Foundation, Inc. | Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof |
AU2012283775A1 (en) | 2011-07-13 | 2014-01-23 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase |
CA2849995A1 (en) | 2011-09-27 | 2013-04-04 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
US8377946B1 (en) | 2011-12-30 | 2013-02-19 | Pharmacyclics, Inc. | Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors |
UY34632A (es) | 2012-02-24 | 2013-05-31 | Novartis Ag | Compuestos de oxazolidin- 2- ona y usos de los mismos |
AU2013241854B2 (en) * | 2012-03-28 | 2017-11-02 | Intervet International B.V. | Heteroaryl compounds with cyclic bridging unit for use in the treatment helminth infection |
WO2013155223A1 (en) | 2012-04-10 | 2013-10-17 | The Regents Of The University Of California | Compositions and methods for treating cancer |
US9879003B2 (en) | 2012-04-11 | 2018-01-30 | Dana-Farber Cancer Institute, Inc. | Host targeted inhibitors of dengue virus and other viruses |
EP2841075B1 (en) | 2012-04-26 | 2020-03-18 | The General Hospital Corporation | Agents and methods for treating and preventing seborrheic keratosis |
AU2013204563B2 (en) | 2012-05-05 | 2016-05-19 | Takeda Pharmaceutical Company Limited | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
WO2013173454A1 (en) * | 2012-05-15 | 2013-11-21 | New York University | Phosphatidylinositol-3-kinase c2 beta modulators and methods of use thereof |
WO2014012093A1 (en) * | 2012-07-13 | 2014-01-16 | Wake Forest University Health Sciences | Prostate cancer targeted prodrugs and methods of use thereof |
WO2014022569A1 (en) * | 2012-08-03 | 2014-02-06 | Principia Biopharma Inc. | Treatment of dry eye |
US11458199B2 (en) | 2012-08-21 | 2022-10-04 | Opko Pharmaceuticals, Llc | Liposome formulations |
MX363822B (es) * | 2012-08-21 | 2019-04-04 | Opko Pharmaceuticals Llc | Formulaciones de liposomas. |
WO2014039899A1 (en) | 2012-09-10 | 2014-03-13 | Principia Biopharma Inc. | Pyrazolopyrimidine compounds as kinase inhibitors |
WO2014063054A1 (en) | 2012-10-19 | 2014-04-24 | Dana-Farber Cancer Institute, Inc. | Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof |
US9296733B2 (en) | 2012-11-12 | 2016-03-29 | Novartis Ag | Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases |
CA2895782C (en) | 2012-12-21 | 2017-08-22 | Gilead Calistoga Llc | Substituted pyrimidine aminoalkyl-quinazolones as phosphatidylinositol 3-kinase inhibitors |
NZ708870A (en) | 2012-12-21 | 2016-09-30 | Gilead Calistoga Llc | Isoquinolinone or quinazolinone phosphatidylinositol 3-kinase inhibitors |
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RU2595718C2 (ru) | 2016-08-27 |
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EP2475375A2 (en) | 2012-07-18 |
BR112012008385A2 (pt) | 2019-09-24 |
KR20120063515A (ko) | 2012-06-15 |
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