EA028984B1 - Применение (s)-пирролидин-1,2-дикарбоновой кислоты 2-амид 1-({4-метил-5-[2-(2,2,2-трифтор-1,1-диметилэтил)пиридин-4-ил]тиазол-2-ил}амида) для лечения рака - Google Patents
Применение (s)-пирролидин-1,2-дикарбоновой кислоты 2-амид 1-({4-метил-5-[2-(2,2,2-трифтор-1,1-диметилэтил)пиридин-4-ил]тиазол-2-ил}амида) для лечения рака Download PDFInfo
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- EA028984B1 EA028984B1 EA201491787A EA201491787A EA028984B1 EA 028984 B1 EA028984 B1 EA 028984B1 EA 201491787 A EA201491787 A EA 201491787A EA 201491787 A EA201491787 A EA 201491787A EA 028984 B1 EA028984 B1 EA 028984B1
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- Prior art keywords
- cancer
- amide
- bei
- agde
- thiazol
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- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
- C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
- C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
- C12Q1/6886—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q2600/00—Oligonucleotides characterized by their use
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q2600/00—Oligonucleotides characterized by their use
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| EP3140427B1 (en) * | 2014-05-09 | 2020-10-14 | Memorial Sloan Kettering Cancer Center | Biomarkers for response to pi3k inhibitors |
| KR102486126B1 (ko) * | 2014-10-03 | 2023-01-09 | 노파르티스 아게 | 알펠리십을 포함하는 제약 조성물 |
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| WO2019199860A1 (en) * | 2018-04-09 | 2019-10-17 | The Research Foundation For The State University Of New York | Genetically modified t-cells and pi3k/akt inhibitors for cancer treatment |
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| WO2012016970A1 (en) * | 2010-08-02 | 2012-02-09 | Novartis Ag | A crystalline form of (s)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-(4 -methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl)-amide and its use as pi3k inhibitor |
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| EP0359789B1 (en) | 1988-01-21 | 1993-08-04 | Genentech, Inc. | Amplification and detection of nucleic acid sequences |
| CA1340807C (en) | 1988-02-24 | 1999-11-02 | Lawrence T. Malek | Nucleic acid amplification process |
| US5130238A (en) | 1988-06-24 | 1992-07-14 | Cangene Corporation | Enhanced nucleic acid amplification process |
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| US5169766A (en) | 1991-06-14 | 1992-12-08 | Life Technologies, Inc. | Amplification of nucleic acid molecules |
| US5846717A (en) | 1996-01-24 | 1998-12-08 | Third Wave Technologies, Inc. | Detection of nucleic acid sequences by invader-directed cleavage |
| US5605798A (en) | 1993-01-07 | 1997-02-25 | Sequenom, Inc. | DNA diagnostic based on mass spectrometry |
| GB2453173A (en) | 2007-09-28 | 2009-04-01 | Dxs Ltd | Polynucleotide primers |
| EP2307414A4 (en) | 2008-07-07 | 2011-10-26 | Xcovery Holding Co Llc | SELECTIVE INHIBITORS OF PI3 KINASE ISOFORMS |
| UA104147C2 (uk) | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
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Patent Citations (2)
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|---|---|---|---|---|
| EP2377933A1 (en) * | 2008-12-23 | 2011-10-19 | Guangzhou Surexam Bio-Tech Co., Ltd. | Probes, liquid phase chips and methods for detecting pik3ca gene mutations |
| WO2012016970A1 (en) * | 2010-08-02 | 2012-02-09 | Novartis Ag | A crystalline form of (s)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-(4 -methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl)-amide and its use as pi3k inhibitor |
Non-Patent Citations (2)
| Title |
|---|
| FRAZZETTO MARK ET AL.: "Dissecting isoform selectivity of PI3K inhibitors: the role of non-conserved residues in the catalytic pocket", BIOCHEMICAL JOURNAL, vol. 414, no. Part 3, September 2008 (2008-09), pages 383-390, XP002697246, table 2 page 387 under the headmark: "The influence of p110alpha mutations on inhibitor potency" * |
| SABBAH DIMA A. ET AL.: "Biological evaluation and docking studies of recently identified inhibitors of phosphoinositide-3-kinases", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 22, no. 2, January 2012 (2012-01), pages 876-880, XP002697245, table 3 * |
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| EP2830621B1 (en) | 2020-10-21 |
| IL234658B (en) | 2018-02-28 |
| IN2014DN08970A (enExample) | 2015-05-22 |
| CL2014002576A1 (es) | 2015-01-23 |
| US9795596B2 (en) | 2017-10-24 |
| GT201400206A (es) | 2017-09-28 |
| HK1200723A1 (en) | 2015-08-14 |
| EA201491787A1 (ru) | 2015-01-30 |
| KR20140138771A (ko) | 2014-12-04 |
| PH12014502168A1 (en) | 2014-12-10 |
| JP6224067B2 (ja) | 2017-11-01 |
| CO7091176A2 (es) | 2014-10-21 |
| TW201345525A (zh) | 2013-11-16 |
| JP2015514080A (ja) | 2015-05-18 |
| WO2013144249A1 (en) | 2013-10-03 |
| NZ628596A (en) | 2015-10-30 |
| CA2866127A1 (en) | 2013-10-03 |
| SG11201405169SA (en) | 2014-10-30 |
| MX2014011682A (es) | 2015-01-22 |
| ECSP14025016A (es) | 2015-09-30 |
| EP2830621A1 (en) | 2015-02-04 |
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