BRPI1011838B8 - compostos de carboxamida heterocíclica de diamino, seu uso, composição farmacêutica que os compreende e inibidor contra a atividade de cinase de proteína de fusão eml4-alk - Google Patents
compostos de carboxamida heterocíclica de diamino, seu uso, composição farmacêutica que os compreende e inibidor contra a atividade de cinase de proteína de fusão eml4-alkInfo
- Publication number
- BRPI1011838B8 BRPI1011838B8 BRPI1011838A BRPI1011838A BRPI1011838B8 BR PI1011838 B8 BRPI1011838 B8 BR PI1011838B8 BR PI1011838 A BRPI1011838 A BR PI1011838A BR PI1011838 A BRPI1011838 A BR PI1011838A BR PI1011838 B8 BRPI1011838 B8 BR PI1011838B8
- Authority
- BR
- Brazil
- Prior art keywords
- fusion protein
- protein kinase
- alk fusion
- pharmaceutical composition
- kinase activity
- Prior art date
Links
- 108091000080 Phosphotransferase Proteins 0.000 title abstract 4
- 230000000694 effects Effects 0.000 title abstract 4
- 108020001507 fusion proteins Proteins 0.000 title abstract 4
- 102000037865 fusion proteins Human genes 0.000 title abstract 4
- 102000020233 phosphotransferase Human genes 0.000 title abstract 4
- -1 heterocyclic diamino carboxamide compounds Chemical class 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 3
- 230000002401 inhibitory effect Effects 0.000 abstract 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 206010041067 Small cell lung cancer Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 201000005202 lung cancer Diseases 0.000 abstract 1
- 208000020816 lung neoplasm Diseases 0.000 abstract 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 208000000587 small cell lung carcinoma Diseases 0.000 abstract 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
- C07D241/28—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
composto de carboxamida heterocíclica de diamino. a presente invenção refere-se a um composto útil como um inibidor contra a atividade de cinase de proteína de fusão eml4-alk. como um resultado de estudos intensivos e extensivos sobre compostos tendo atividade inibidora com relação à atividade de cinase de proteína de fusão eml4-alk, os presentes inventores descobriram que os compostos de carboxamida heterocíclica de diamino da presente invenção tinham atividade inibidora com relação à atividade de cinase de proteína de fusão eml4-alk. por esta descoberta, a presente invenção foi concluída.os compos-tos da presente invenção podem ser usados como uma composição farmacêutica para prevenção e/ou trata-mento de câncer, tal como câncer de pulmão, câncer de pulmão de célula não pequena, e câncer de pulmão de célula pequena.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2009-113936 | 2009-05-08 | ||
| JP2009113936 | 2009-05-08 | ||
| PCT/JP2010/057751 WO2010128659A1 (ja) | 2009-05-08 | 2010-05-06 | ジアミノへテロ環カルボキサミド化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BRPI1011838A2 BRPI1011838A2 (pt) | 2018-02-06 |
| BRPI1011838B1 BRPI1011838B1 (pt) | 2021-03-16 |
| BRPI1011838B8 true BRPI1011838B8 (pt) | 2021-05-25 |
Family
ID=43050157
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI1011838A BRPI1011838B8 (pt) | 2009-05-08 | 2010-05-06 | compostos de carboxamida heterocíclica de diamino, seu uso, composição farmacêutica que os compreende e inibidor contra a atividade de cinase de proteína de fusão eml4-alk |
Country Status (28)
| Country | Link |
|---|---|
| US (2) | US8969336B2 (pt) |
| EP (2) | EP2428508B9 (pt) |
| JP (1) | JP5364159B2 (pt) |
| KR (1) | KR101614572B1 (pt) |
| CN (1) | CN102421761B (pt) |
| AU (1) | AU2010245545B2 (pt) |
| BR (1) | BRPI1011838B8 (pt) |
| CA (1) | CA2760061C (pt) |
| CY (3) | CY1117546T1 (pt) |
| DK (2) | DK2428508T3 (pt) |
| ES (2) | ES2667706T3 (pt) |
| FR (1) | FR20C1003I2 (pt) |
| HR (2) | HRP20151435T8 (pt) |
| HU (3) | HUE038515T2 (pt) |
| IL (1) | IL216132A (pt) |
| LT (2) | LT3009428T (pt) |
| LU (1) | LUC00147I2 (pt) |
| MX (1) | MX2011011875A (pt) |
| NL (1) | NL301028I2 (pt) |
| NO (2) | NO3009428T3 (pt) |
| PL (2) | PL2428508T3 (pt) |
| PT (2) | PT2428508E (pt) |
| RS (2) | RS54552B1 (pt) |
| SI (2) | SI3009428T1 (pt) |
| SM (2) | SMT201800237T1 (pt) |
| TW (1) | TWI484961B (pt) |
| WO (1) | WO2010128659A1 (pt) |
| ZA (1) | ZA201108642B (pt) |
Families Citing this family (73)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120208824A1 (en) * | 2006-01-20 | 2012-08-16 | Cell Signaling Technology, Inc. | ROS Kinase in Lung Cancer |
| US8138339B2 (en) | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| NZ589315A (en) | 2008-04-16 | 2012-11-30 | Portola Pharm Inc | 2,6-diamino-pyrimidin-5-yl-carboxamides as Spleen tryosine kinase (syk) or Janus kinase (JAK) inhibitors |
| US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| TWI458721B (zh) | 2008-06-27 | 2014-11-01 | Celgene Avilomics Res Inc | 雜芳基化合物及其用途 |
| CN105693720B (zh) | 2010-05-20 | 2019-01-18 | 阵列生物制药公司 | 作为trk激酶抑制剂的大环化合物 |
| RU2013109393A (ru) | 2010-08-10 | 2014-09-20 | Сэлджин Авиаломикс Ресеарч, Инк. | Безилатная соль ингибитора втк |
| JP2014005206A (ja) * | 2010-10-22 | 2014-01-16 | Astellas Pharma Inc | アリールアミノヘテロ環カルボキサミド化合物 |
| CA2815858C (en) | 2010-11-01 | 2018-10-16 | Celgene Avilomics Research, Inc. | Heterocyclic compounds and uses thereof |
| US20130317029A1 (en) * | 2010-11-01 | 2013-11-28 | Portola Pharmaceuticals, Inc. | Oxypyrimidines as syk modulators |
| EP2635285B1 (en) | 2010-11-01 | 2017-05-03 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| EP2637502B1 (en) | 2010-11-10 | 2018-01-10 | Celgene CAR LLC | Mutant-selective egfr inhibitors and uses thereof |
| CN102285969B (zh) * | 2011-06-28 | 2013-06-19 | 山东大学 | N-1-取代哌啶-4-芳胺类衍生物及其制备方法与应用 |
| CA2846197C (en) | 2011-08-23 | 2024-01-16 | Foundation Medicine, Inc. | Kif5b-ret fusion molecules and uses thereof |
| CA2853498A1 (en) | 2011-10-28 | 2013-05-02 | Celgene Avilomics Research, Inc. | Methods of treating a bruton's tyrosine kinase disease or disorder |
| EP2782579B1 (en) * | 2011-11-23 | 2019-01-02 | Portola Pharmaceuticals, Inc. | Pyrazine kinase inhibitors |
| UA111010C2 (uk) | 2012-01-17 | 2016-03-10 | Астеллас Фарма Інк. | Сполука піразинкарбоксаміду |
| BR112014022789B1 (pt) | 2012-03-15 | 2022-04-19 | Celgene Car Llc | Formas sólidas de um inibidor de quinase de receptor do fator de crescimento epidérmico, composição farmacêutica e usos do mesmo |
| RU2711077C9 (ru) | 2012-03-15 | 2020-08-11 | Селджен Кар Ллс | Соли ингибитора киназы рецептора эпидермального фактора роста |
| JP6359020B6 (ja) * | 2012-11-06 | 2018-08-15 | シャンハイ フォチョン ファーマシューティカル カンパニー リミテッド | Alkキナーゼ阻害剤 |
| WO2014100748A1 (en) | 2012-12-21 | 2014-06-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| EP2953457B1 (en) | 2013-02-08 | 2020-04-08 | Celgene CAR LLC | Erk inhibitors and uses thereof |
| US9492471B2 (en) | 2013-08-27 | 2016-11-15 | Celgene Avilomics Research, Inc. | Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase |
| CN104262328B (zh) * | 2013-09-18 | 2016-09-07 | 北京韩美药品有限公司 | 抑制btk和/或jak3激酶活性的化合物 |
| WO2015054465A1 (en) | 2013-10-11 | 2015-04-16 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| HUE044683T2 (hu) * | 2013-10-21 | 2019-11-28 | Merck Patent Gmbh | Heteroaril vegyületek mint BTK inhibitorok és alkalmazásuk |
| AU2014360446A1 (en) | 2013-12-05 | 2016-06-09 | Pharmacyclics, Llc | Inhibitors of Bruton's tyrosine kinase |
| US9415049B2 (en) | 2013-12-20 | 2016-08-16 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| CA2935944A1 (en) | 2014-01-09 | 2015-07-16 | The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone | Substituted benzoxazine and related compounds |
| NZ715903A (en) | 2014-01-30 | 2017-06-30 | Signal Pharm Llc | Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use |
| HRP20200662T1 (hr) * | 2014-02-04 | 2020-10-02 | Astellas Pharma Inc. | Ljekoviti pripravak koji sadrži spoj diamino heterocikličkog karboksamida kao aktivni sastojak |
| CN104016977B (zh) * | 2014-06-13 | 2016-06-22 | 山东大学 | 一种取代噻二嗪二酮类衍生物及其制备方法与应用 |
| EP3179858B1 (en) | 2014-08-13 | 2019-05-15 | Celgene Car Llc | Forms and compositions of an erk inhibitor |
| SG11201704827UA (en) | 2014-12-16 | 2017-07-28 | Signal Pharm Llc | Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide |
| WO2016100308A1 (en) | 2014-12-16 | 2016-06-23 | Signal Pharmaceuticals, Llc | Methods for measurement of inhibition of c-jun n-terminal kinase in skin |
| EP3250557B1 (en) | 2015-01-29 | 2024-11-20 | Signal Pharmaceuticals, LLC | Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide |
| DK3318259T3 (en) | 2015-07-03 | 2023-03-06 | Astellas Pharma Inc | Stabil farmaceutisk sammensætning til oral indgivelse |
| EP3322706B1 (en) | 2015-07-16 | 2020-11-11 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
| CN105001096B (zh) * | 2015-07-21 | 2017-07-21 | 沈阳化工研究院有限公司 | 一种制备4‑氨基‑n‑烷基苄胺的方法 |
| CN107922287B (zh) | 2015-07-24 | 2021-04-09 | 细胞基因公司 | 合成(1r,2r,5r)-5-氨基-2-甲基环己醇盐酸盐的方法和其中可用的中间体 |
| EP3372231B1 (en) * | 2015-11-04 | 2021-09-15 | Astellas Pharma Inc. | Pharmaceutical composition for cancer immunotherapy purposes and/or immunostimulation purposes which contains diamino heterocyclic carboxamide compound as active ingredient |
| US20190099413A1 (en) | 2016-02-26 | 2019-04-04 | Ono Pharmaceutical Co., Ltd. | Drug for cancer therapy characterized in that axl inhibitor and immune checkpoint inhibitor are administered in combination |
| CN106083821B (zh) * | 2016-06-22 | 2019-01-11 | 上海皓元生物医药科技有限公司 | 一种3,5-二取代-吡嗪-2-甲酰胺化合物的合成方法 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| CN110267960B (zh) | 2017-01-18 | 2022-04-26 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡嗪化合物 |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| WO2018211018A1 (en) | 2017-05-17 | 2018-11-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Flt3 inhibitors for improving pain treatments by opioids |
| CN109384774B (zh) * | 2017-08-11 | 2023-02-17 | 中国科学院上海药物研究所 | 一类多取代的吡嗪/三嗪酰胺类化合物及其制备方法和应用 |
| EP3673907A4 (en) | 2017-08-23 | 2020-08-19 | ONO Pharmaceutical Co., Ltd. | CANCER TREATMENT PHARMACEUTICAL INCLUDING AX1 INHIBITOR AS AN EFFECTIVE INGREDIENT |
| JP7223998B2 (ja) | 2017-10-13 | 2023-02-17 | 小野薬品工業株式会社 | Axl阻害剤を有効成分として含む固形がん治療剤 |
| TW201938169A (zh) | 2018-01-18 | 2019-10-01 | 美商亞雷生物製藥股份有限公司 | 作為RET激酶抑制劑之經取代吡唑并[3,4-d]嘧啶化合物 |
| WO2019143994A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| CN111971286B (zh) | 2018-01-18 | 2023-04-14 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物 |
| JP7492742B2 (ja) * | 2018-03-28 | 2024-05-30 | 深▲チェン▼市塔吉瑞生物医薬有限公司 | 置換ジアミノ複素環式カルボキサミド化合物、該化合物を含む組成物およびその使用 |
| ES2922314T3 (es) | 2018-09-10 | 2022-09-13 | Array Biopharma Inc | Compuestos heterocíclicos condensados como inhibidores de cinasa RET |
| CN112839930B (zh) | 2018-09-30 | 2022-03-15 | 南京明德新药研发有限公司 | 作为flt3和axl抑制剂的3,9-二氮杂螺[5,5]十一烷类化合物 |
| KR102850357B1 (ko) * | 2018-10-22 | 2025-08-27 | 알루미스 인크. | Tyk2 억제제 및 이의 용도 |
| EP3939954B1 (en) | 2019-03-13 | 2025-07-23 | Otsuka Pharmaceutical Co., Ltd. | Method for introducing deuterated lower alkyl into amine moiety of compound containing secondary amine |
| PL3949952T3 (pl) | 2019-04-03 | 2024-10-14 | Astellas Pharma Inc. | Kompozycja farmaceutyczna |
| CN115380024B (zh) * | 2020-03-30 | 2024-03-15 | 南京明德新药研发有限公司 | 二氮杂螺吡喃化合物的晶型 |
| CN111423387B (zh) * | 2020-05-11 | 2022-03-08 | 苏州康纯医药科技有限公司 | 一种Gilteritinib关键中间体的制备方法 |
| US20230167099A1 (en) * | 2020-06-01 | 2023-06-01 | Wigen Biomedicine Technology (shanghai) Co., Ltd. | New pyrazine compound |
| WO2022009235A1 (en) * | 2020-07-10 | 2022-01-13 | Msn Laboratories Private Limited, R&D Center | Process for the preparation of gilteritinib fumarate |
| CN113943288A (zh) * | 2020-07-17 | 2022-01-18 | 微境生物医药科技(上海)有限公司 | 5,6-二氢吡嗪并[2,3-c]异喹啉化合物 |
| CN112225703B (zh) * | 2020-09-28 | 2022-03-11 | 广州智睿医药科技有限公司 | 一种治疗或预防与lrrk2激酶或异常lrrk2突变激酶活性相关疾病的药物 |
| WO2022078305A1 (zh) * | 2020-10-12 | 2022-04-21 | 四川海思科制药有限公司 | 一种杂环衍生物及其在医药上的应用 |
| WO2023027966A1 (en) * | 2021-08-24 | 2023-03-02 | Biomea Fusion, Inc. | Pyrazine compounds as irreversible inhibitors of flt3 |
| IL313670A (en) | 2021-12-30 | 2024-08-01 | Biomea Fusion Inc | Pyrazine compounds as inhibitors of FLT3 |
| WO2023178094A2 (en) * | 2022-03-14 | 2023-09-21 | Purdue Research Foundation | Spleen tyrosine kinase inhibitor, composition, and methods of use |
| EP4525873A1 (en) * | 2022-05-17 | 2025-03-26 | Biomea Fusion, Inc. | Flt3 combination therapy for cancer and compositions therefor |
| CN115124590B (zh) * | 2022-07-05 | 2024-10-22 | 武汉大学中南医院 | 一种靶向降解flt3-itd突变蛋白的protac类化合物及其制备方法与应用 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1184376B1 (en) * | 1999-06-09 | 2005-02-02 | Yamanouchi Pharmaceutical Co. Ltd. | Novel heterocyclic carboxamide derivatives |
| WO2000076980A1 (en) | 1999-06-10 | 2000-12-21 | Yamanouchi Pharmaceutical Co., Ltd. | Novel nitrogen-contaiing heterocyclic derivatives or salts thereof |
| CN1665789A (zh) | 2002-06-28 | 2005-09-07 | 山之内制药株式会社 | 二氨基嘧啶酰胺衍生物 |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| JP2008013499A (ja) | 2006-07-06 | 2008-01-24 | Sankyo Co Ltd | 5−シアノニコチンアミド誘導体 |
| WO2008016660A2 (en) * | 2006-08-02 | 2008-02-07 | Xanthus Pharmaceuticals, Inc. | Imidazoacridine compounds for treating leukemias |
| US20080070930A1 (en) | 2006-08-24 | 2008-03-20 | Huang Kenneth H | Pyrimidine and Pyrazine Derivatives |
| EP1914240B1 (en) | 2006-10-11 | 2009-12-02 | Astellas Pharma Inc. | EML4-ALK fusion gene |
| AU2007309427B2 (en) | 2006-10-23 | 2013-02-28 | Cephalon, Inc. | Fused bicyclic derivatives of 2,4-diaminopyrimidine as ALK and c-Met inhibitors |
| KR101149295B1 (ko) | 2006-12-08 | 2012-07-05 | 아이알엠 엘엘씨 | 단백질 키나제 억제제로서의 화합물 |
| WO2008077885A2 (en) | 2006-12-22 | 2008-07-03 | Boehringer Ingelheim International Gmbh | 2- [(phenylamino) -pyrimidin-4ylamin0] -cyclopentane carboxamide derivatives and related compounds as inhibitors of kinases of the cell cycle for the treatment of cancer |
| TWI389893B (zh) * | 2007-07-06 | 2013-03-21 | Astellas Pharma Inc | 二(芳胺基)芳基化合物 |
| WO2009012421A1 (en) | 2007-07-17 | 2009-01-22 | Rigel Pharmaceuticals, Inc. | Cyclic amine substituted pyrimidinediamines as pkc inhibitors |
| CN101827848B (zh) | 2007-08-08 | 2012-11-07 | 葛兰素史密丝克莱恩有限责任公司 | 作为IGF-1R抑制剂用于治疗癌症的2-[(2-{苯基氨基}-1H-吡咯并[2,3-d]嘧啶-4-基)氨基]苯甲酰胺衍生物 |
| WO2009032703A1 (en) | 2007-08-28 | 2009-03-12 | Irm Llc | 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma kinase inhibitors |
| WO2009040399A1 (en) | 2007-09-28 | 2009-04-02 | Nerviano Medical Sciences S.R.L. | Substituted pyrrolo-pyrimidine derivatives, process for their preparation and their use as kinase inhibitors |
| US20090270418A1 (en) | 2008-01-09 | 2009-10-29 | Marianne Sloss | Pyrazole pyrazine amine compounds as kinase inhibitors, compositions thereof and methods of treatment therewith |
| JP5298187B2 (ja) | 2008-04-07 | 2013-09-25 | アイアールエム・リミテッド・ライアビリティ・カンパニー | タンパク質キナーゼ阻害剤としての化合物および組成物 |
| JP5214799B2 (ja) | 2008-04-07 | 2013-06-19 | アイアールエム・リミテッド・ライアビリティ・カンパニー | キナーゼ阻害剤としての化合物および組成物 |
| CN102066339B (zh) * | 2008-04-16 | 2014-09-24 | 波托拉医药品公司 | 作为syk或jak蛋白激酶抑制剂的2,6-二氨基-嘧啶-5-基甲酰胺类化合物 |
| CA2960692C (en) * | 2008-04-16 | 2019-09-24 | Portola Pharmaceuticals, Inc. | 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinase inhibitors |
| PL2300013T5 (pl) | 2008-05-21 | 2025-04-28 | Takeda Pharmaceutical Company Limited | Pochodne fosforu jako inhibitor kinazy |
-
2010
- 2010-05-06 DK DK10772177.1T patent/DK2428508T3/en active
- 2010-05-06 PL PL10772177T patent/PL2428508T3/pl unknown
- 2010-05-06 ES ES15189570.3T patent/ES2667706T3/es active Active
- 2010-05-06 MX MX2011011875A patent/MX2011011875A/es active IP Right Grant
- 2010-05-06 RS RS20160032A patent/RS54552B1/sr unknown
- 2010-05-06 TW TW099114522A patent/TWI484961B/zh active
- 2010-05-06 JP JP2011512353A patent/JP5364159B2/ja active Active
- 2010-05-06 HU HUE15189570A patent/HUE038515T2/hu unknown
- 2010-05-06 NO NO15189570A patent/NO3009428T3/no unknown
- 2010-05-06 DK DK15189570.3T patent/DK3009428T3/en active
- 2010-05-06 ES ES10772177.1T patent/ES2559230T3/es active Active
- 2010-05-06 PT PT107721771T patent/PT2428508E/pt unknown
- 2010-05-06 HU HUE10772177A patent/HUE026647T2/en unknown
- 2010-05-06 RS RS20180358A patent/RS57045B1/sr unknown
- 2010-05-06 CN CN201080020181.4A patent/CN102421761B/zh active Active
- 2010-05-06 BR BRPI1011838A patent/BRPI1011838B8/pt active IP Right Grant
- 2010-05-06 PL PL15189570T patent/PL3009428T3/pl unknown
- 2010-05-06 SM SM20180237T patent/SMT201800237T1/it unknown
- 2010-05-06 CA CA2760061A patent/CA2760061C/en active Active
- 2010-05-06 HR HRP20151435TT patent/HRP20151435T8/hr unknown
- 2010-05-06 KR KR1020117026122A patent/KR101614572B1/ko active Active
- 2010-05-06 EP EP10772177.1A patent/EP2428508B9/en active Active
- 2010-05-06 PT PT151895703T patent/PT3009428T/pt unknown
- 2010-05-06 WO PCT/JP2010/057751 patent/WO2010128659A1/ja not_active Ceased
- 2010-05-06 LT LTEP15189570.3T patent/LT3009428T/lt unknown
- 2010-05-06 US US13/266,164 patent/US8969336B2/en active Active
- 2010-05-06 EP EP15189570.3A patent/EP3009428B1/en active Active
- 2010-05-06 SI SI201031651T patent/SI3009428T1/en unknown
- 2010-05-06 AU AU2010245545A patent/AU2010245545B2/en active Active
- 2010-05-06 SI SI201031107T patent/SI2428508T1/sl unknown
-
2011
- 2011-11-03 IL IL216132A patent/IL216132A/en active Protection Beyond IP Right Term
- 2011-11-24 ZA ZA2011/08642A patent/ZA201108642B/en unknown
-
2014
- 2014-08-29 US US14/472,959 patent/US9487491B2/en active Active
-
2016
- 2016-01-27 CY CY20161100072T patent/CY1117546T1/el unknown
- 2016-03-16 SM SM201600075T patent/SMT201600075B/xx unknown
-
2018
- 2018-03-01 HR HRP20180368TT patent/HRP20180368T1/hr unknown
- 2018-03-27 CY CY20181100350T patent/CY1120367T1/el unknown
-
2020
- 2020-01-16 NO NO2020001C patent/NO2020001I1/no unknown
- 2020-01-17 NL NL301028C patent/NL301028I2/nl unknown
- 2020-01-21 LT LTPA2020002C patent/LTC2428508I2/lt unknown
- 2020-01-22 CY CY2020004C patent/CY2020004I2/el unknown
- 2020-02-04 FR FR20C1003C patent/FR20C1003I2/fr active Active
- 2020-02-06 LU LU00147C patent/LUC00147I2/fr unknown
- 2020-02-20 HU HUS2000005C patent/HUS000511I2/hu unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| BRPI1011838B8 (pt) | compostos de carboxamida heterocíclica de diamino, seu uso, composição farmacêutica que os compreende e inibidor contra a atividade de cinase de proteína de fusão eml4-alk | |
| AR065721A1 (es) | Derivados de piridazinona utiles como inhibidores de glucano sintasa. composiciones farmaceuticas. | |
| BR112014004504A2 (pt) | "composto como inibidor de c-kit cinase, seu uso, composição farmacêutica, e medicamento para o tratamento de uma doença mediada por uma cinase" | |
| DOP2013000192A (es) | Compuestos y composiciones como inhibidores de la trk | |
| CL2015002608A1 (es) | Compuesto de amino-pirazol y usos medicinales relacionados. | |
| DOP2011000279A (es) | Derivados de benzofuranilo usados como inhibidores de glucoquinasa | |
| CL2009000316A1 (es) | Compuestos derivados de urea de benzomorfanos y sus sales, inhibidores de la enzima 11-beta-hidroxiesteroide deshidrogenasa; procedimiento de preparacion; composicion farmaceutica; y uso para el tratamiento o prevencion de trastornos metabolicos. | |
| BR112014009415A2 (pt) | inibidores de arginase e suas aplicações terapêuticas | |
| UY33597A (es) | Compuestos y composiciones como inhibidores de la trk | |
| BR112017005531A2 (pt) | derivados de diaril ureia como inibidores de quinase p38 | |
| CL2009000483A1 (es) | Compuestos derivados de n-(piridin-3-il)-1,3-tiazol-5-amino-4-carboxamida, inhibidores de cinasa pim; composicion farmaceutica; y uso para el tratamiento del cancer. | |
| CL2010001415A1 (es) | Compuestos derivados de diazacarbazol, con actividad inhibidora de quinasa; composición farmacéutica que comprende a uno de los compuestos; y uso de la composición farmacéutica en la preparación de medicamentos para la inhibición del crecimiento celular o el tratamiento de un trastorno hiperproliferativo | |
| BR112012002134B8 (pt) | compostos inibidores de apaf-1 | |
| BR112017003054A2 (pt) | compostos de aminopirimidinila como inibidores de jak | |
| MX377802B (es) | Metodos y composiciones para trastornos del sueño y otros trastornos. | |
| BR112016020199A8 (pt) | composto inibidor de calicreína plasmática de humano, composição farmacêutica compreendendo o referido composto, kit e seu uso | |
| CL2007003520A1 (es) | Compuestos derivados de heterociclos sustituidos con morfolina, inhibidores de la actividad pi3 quinasa; composicion farmaceutica que comprende a dichos compuestos; kit farmaceutico; y su uso para el tratamiento profilactico o terapeutico del cancer. | |
| BR112014015720A8 (pt) | derivados de tieno[3,2-d]pirimidina que têm atividade inibidora de proteinas quinases | |
| BR112016015818A2 (pt) | Compostos e respectivos usos para tratar pacientes com células cancerosas mutantes em relação a ros1 | |
| BR112015028501A2 (pt) | derivados de bipirazol como inibidores de jak | |
| BR112014003963A2 (pt) | compostos e composições como inibidores de quinase c-kit | |
| CL2011000489A1 (es) | Compuestos derivados de pirimido[5,4-d]pirimidina, los cuales actuan como inhibidores de tirosina-quinasas; y composiciones farmaceuticas que los comprenden, utiles en el tratamiento de enfermedades que se caracterizan por una proliferacion celular excesiva o anomala | |
| ECSP088828A (es) | 4-anilinoquinolina-3-carboxamidas como inhibidores de la quinasa csf-1r | |
| UY30846A1 (es) | Derivados de oxindol sustituidos, medicamentos que los comprenden y uso de los mismos | |
| BR112015020350A2 (pt) | derivados de 6-(5-hidroxi-1h-pirazol-1-il)nicotinamida e seu uso como inibidores de phd |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B65X | Notification of requirement for priority examination of patent application | ||
| B65Y | Grant of priority examination of the patent application (request complies with dec. 132/06 of 20061117) | ||
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] |
Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI |
|
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] |
Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI |
|
| B07B | Technical examination (opinion): publication cancelled [chapter 7.2 patent gazette] |
Free format text: ANULADA A PUBLICACAO CODIGO 7.5 NA RPI NO 2516 DE 26/03/2019 POR TER SIDO INDEVIDA. |
|
| B09B | Patent application refused [chapter 9.2 patent gazette] | ||
| B12B | Appeal against refusal [chapter 12.2 patent gazette] | ||
| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 16/03/2021, OBSERVADAS AS CONDICOES LEGAIS. |
|
| B16C | Correction of notification of the grant [chapter 16.3 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 06/05/2010 OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF |