PE20110796A1 - (s)-1-({4-metil-5-[2-(2,2,2-trifluoro-1,1-dimetil-etil)-piridin-4-il]-tiazol-2-il}-amida) de 2-amida del acido pirrolidin-1,2-dicarboxilico como inhibidor de la cinasa de fosfatidilinositol (pi3k) - Google Patents
(s)-1-({4-metil-5-[2-(2,2,2-trifluoro-1,1-dimetil-etil)-piridin-4-il]-tiazol-2-il}-amida) de 2-amida del acido pirrolidin-1,2-dicarboxilico como inhibidor de la cinasa de fosfatidilinositol (pi3k)Info
- Publication number
- PE20110796A1 PE20110796A1 PE2011000591A PE2011000591A PE20110796A1 PE 20110796 A1 PE20110796 A1 PE 20110796A1 PE 2011000591 A PE2011000591 A PE 2011000591A PE 2011000591 A PE2011000591 A PE 2011000591A PE 20110796 A1 PE20110796 A1 PE 20110796A1
- Authority
- PE
- Peru
- Prior art keywords
- amide
- pyrrolidin
- methyl
- pyridin
- ethyl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- OAWXZFGKDDFTGS-UHFFFAOYSA-N pyrrolidine-1,2-dicarboxylic acid Chemical compound OC(=O)C1CCCN1C(O)=O OAWXZFGKDDFTGS-UHFFFAOYSA-N 0.000 title abstract 2
- 102000017343 Phosphatidylinositol kinases Human genes 0.000 title 2
- 108050005377 Phosphatidylinositol kinases Proteins 0.000 title 2
- -1 2,2,2-TRIFLUORO-1,1-DIMETHYL-ETHYL Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 108091007960 PI3Ks Proteins 0.000 abstract 2
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 abstract 2
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 2
- 125000004005 formimidoyl group Chemical group [H]\N=C(/[H])* 0.000 abstract 2
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 abstract 1
- RAHZWNYVWXNFOC-UHFFFAOYSA-N Sulphur dioxide Chemical class O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
Classifications
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- 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
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Abstract
SE REFIERE A UN COMPUESTO DE FORMULA (I) DONDE A ES PIRIDIN, PIRIMIDIN, PIRAZIN, BENZOIMIDAZOL; R1 ES ALQUILO C1-C7, CICLOALQUILO C3-C5, FENILO, SULFONILO, ENTRE OTROS; R2 ES H; R3 ES H, METILO, CH2CL, CH2N(CH3)3 ENTRE OTROS. SON COMPUESTOS PREFERIDOS (S)-1-{[5-(2-TERBUTIL-PIRIDIN-4-IL)-4-METIL-TIAZOL-2-IL]-AMIDA} DE 2-AMIDA DEL ACIDO PIRROLIDIN-1,2-DICARBOXILICO, (S)-1-{[5-(3-TERBUTIL-3H-BENZO-IMIDAZOL-5-IL)-TIAZOL-2-IL]-AMIDA} DE 2-AMIDA DEL ACIDO PIRROLIDIN-1,2-DICARBOXILICO; (S)-1-{[5-(2-ETIL-PIRIMIDIM-4-IL)-4-METIL-TIAZOL-2-IL]-AMIDA} DE 2-AMIDA DEL ACIDO PIRROLIDIN-1,2-DICARBOXILICO; ENTRE OTROS. REFERIDA TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCESO PARA LA OBTENCION DEL COMPUESTO DE FORMULA (I). DICHOS COMPUESTOS SON INHIBIDORES DE CINASA DE FOSFATIDIL-INOSITOL-3(PI-3) UTILES EN EL TRATAMIENTO DE ENFERMEDADES PROLIFERATIVAS
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08164104 | 2008-09-10 | ||
| US9667408P | 2008-09-12 | 2008-09-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20110796A1 true PE20110796A1 (es) | 2011-11-04 |
Family
ID=40350060
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2011000591A PE20110796A1 (es) | 2008-09-10 | 2009-09-08 | (s)-1-({4-metil-5-[2-(2,2,2-trifluoro-1,1-dimetil-etil)-piridin-4-il]-tiazol-2-il}-amida) de 2-amida del acido pirrolidin-1,2-dicarboxilico como inhibidor de la cinasa de fosfatidilinositol (pi3k) |
Country Status (50)
Families Citing this family (110)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR044519A1 (es) * | 2003-05-02 | 2005-09-14 | Novartis Ag | Derivados de piridin-tiazol amina y de pirimidin-tiazol amina |
| WO2010006225A1 (en) | 2008-07-11 | 2010-01-14 | Novartis Ag | Combination of (a) a phosphoinositide 3-kinase inhibitor and (b) a modulator of ras/raf/mek pathway |
| UA104147C2 (uk) * | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
| US8293753B2 (en) * | 2009-07-02 | 2012-10-23 | Novartis Ag | Substituted 2-carboxamide cycloamino ureas |
| AR082418A1 (es) | 2010-08-02 | 2012-12-05 | Novartis Ag | Formas cristalinas de 1-(4-metil-5-[2-(2,2,2-trifluoro-1,1-dimetil-etil)-piridin-4-il]-tiazol-2-il)-amida de 2-amida del acido (s)-pirrolidin-1,2-dicarboxilico |
| AU2015203865B2 (en) * | 2010-11-08 | 2016-11-03 | Novartis Ag | Use of 2-carboxamide cycloamino urea derivatives in the treatment of EGFR dependent diseases or diseases that have acquired resistance to agents that target EGFR family members |
| BR112013009624A2 (pt) * | 2010-11-08 | 2016-07-12 | Novartis Ag | uso de derivados de 2-carboxamida cicloamino ureia no tratamento de doenças dependemtes de egfr pu doenças que tenham adquirido resistência a agentes que tenham como alvo membros da família egfr |
| UA112539C2 (uk) * | 2011-03-03 | 2016-09-26 | Новартіс Аг | Спосіб одержання похідних 2-карбоксамідциклоаміносечовини |
| CA2833962A1 (en) | 2011-04-25 | 2012-11-01 | Novartis Ag | Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor |
| CA2839621A1 (en) * | 2011-06-21 | 2012-12-27 | Novartis Ag | Polymorphs 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 |
| PH12013502697A1 (en) * | 2011-07-01 | 2014-02-10 | Novartis Ag | Combination therapy comprising a cdk4/6 inhibitor and a pi3k inhibitor for use in the treatment of cancer |
| AU2012333092B2 (en) * | 2011-08-31 | 2016-04-21 | Novartis Ag | Synergistic combinations of PI3K- and MEK-inhibitors |
| US20140235630A1 (en) * | 2011-09-30 | 2014-08-21 | Beth Israel Deaconess Medical Center, Inc. | Compositions and methods for the treatment of proliferative diseases |
| CN106474127A (zh) * | 2011-10-14 | 2017-03-08 | 诺华股份有限公司 | 用于治疗增生性疾病的2‑甲酰胺环氨基尿素衍生物与Hsp90抑制剂的组合 |
| PH12014500897A1 (en) * | 2011-10-28 | 2019-10-07 | Novartis Ag | Method of treating gastrointestinal stromal tumors |
| KR20140088869A (ko) * | 2011-11-02 | 2014-07-11 | 노파르티스 아게 | Vegf-의존성 질환의 치료에 사용하기 위한 2-카르복스아미드 시클로아미노 우레아 유도체 |
| BR112014020773A2 (pt) | 2012-02-22 | 2020-10-27 | Sanford-Burnham Medical Research Institute | compostos de sulfonamida e seus usos como inibidores tnap |
| IN2014DN08970A (es) | 2012-03-29 | 2015-05-22 | Novartis Ag | |
| CA2865993A1 (en) * | 2012-03-30 | 2013-10-03 | Novartis Ag | Compounds for use in the treatment of neuroblastoma, ewing's sarcoma or rhabdomyosarcoma |
| BR112014028881A2 (pt) | 2012-05-23 | 2017-06-27 | Hoffmann La Roche | populações de células, banco de células, métodos de obtenção de uma população de células, métodos de identificação de um fator, métodos de seleção, métodos de fornecimento de terapia, populações de hepatócitos e método de obtenção de células |
| US8980259B2 (en) | 2012-07-20 | 2015-03-17 | Novartis Ag | Combination therapy |
| DK2882440T3 (da) * | 2012-08-07 | 2019-05-06 | Novartis Ag | Farmaceutiske kombinationer, der omfatter en b-raf-inhibitor, en egfr-inhibitor og eventuelt en pi3k-alfa-inhibitor |
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