PE20080689A1 - KINASE INHIBITORS AMINE DERIVATIVES - Google Patents
KINASE INHIBITORS AMINE DERIVATIVESInfo
- Publication number
- PE20080689A1 PE20080689A1 PE2007000962A PE2007000962A PE20080689A1 PE 20080689 A1 PE20080689 A1 PE 20080689A1 PE 2007000962 A PE2007000962 A PE 2007000962A PE 2007000962 A PE2007000962 A PE 2007000962A PE 20080689 A1 PE20080689 A1 PE 20080689A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- methyl
- amine
- pyrrolo
- pyrrolidin
- Prior art date
Links
- 150000001412 amines Chemical class 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- NGXSWUFDCSEIOO-UHFFFAOYSA-N pyrrolidin-3-amine Chemical compound NC1CCNC1 NGXSWUFDCSEIOO-UHFFFAOYSA-N 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102100024908 Ribosomal protein S6 kinase beta-1 Human genes 0.000 abstract 1
- 101710108924 Ribosomal protein S6 kinase beta-1 Proteins 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 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
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
REFERIDA A UN DERIVADO DE AMINA DE FORMULA (I), DONDE A ES UN BICICLO FUSIONADO; u ES UN ENTERO DE 0 A 3; V ES N O CR7; W Y X SON N O CR8; Y ES CH, N O NH; Z ES CH O N; D Y E SON C O N; L ES -(CR3R4)m- O C(O); m ES UN ENTERO DE 1 A 6; R1 Y R2 SON H, ALQUILO C1-C6, CICLOALQUILO C3-C10, CICLOALQUENILO C5-C10, ENTRE OTROS; R3 Y R4 SON H, ALQUILO C1-C6, CF3; R5 ES OR13, NR14R15, NR11C(O)R10, ENTRE OTROS; R6 ES ALQUILO C1-C6 O CICLOALQUILO C3-C10; R7 ES HALOGENO, OH, CF3, ENTRE OTROS; R8 ES H, HALO, CN, OH O ALQUILO C1-C6; R10 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, ENTRE OTROS; R11 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, ENTRE OTROS; R13 ES ALQUILO C1-C6, CICLOALQUILO C3-C10, CICLOALQUENILO C5-C10, ENTRE OTROS; R14 ES H, CF3, ALQUILO C1-C6, ENTRE OTROS; R15 ES ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (3S)-3-{[(4-CLOROFENIL9AMINO]METIL}-1-(5-METIL-7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)PIRROLIDIN-3-AMINA, 3-({[2-FLUORO-3-(TRIFLUOROMETIL)FENIL]AMINO}METIL)-1-(5-METIL-7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)PIRROLIDIN-3-AMINA, (3S)-1-(5-METIL-7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-3-{[3-(TRIFLUOROMETIL)FENIL]AMINO}METIL)PIRROLIDIN-3-AMINA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE QUINASA AKT Y/O P70S6K1 Y SON UTILES EN EL TRATAMIENTO DE CELULAS CANCEROSASREFERRED TO AN AMINE DERIVATIVE OF FORMULA (I), WHERE A IS A FUSED BIKE; u IS AN INTEGER FROM 0 TO 3; V IS NO CR7; W AND X ARE NO CR8; Y IS CH, N O NH; Z IS CH O N; D AND E ARE C O N; L ES - (CR3R4) m- O C (O); m IS AN INTEGER FROM 1 TO 6; R1 AND R2 ARE H, C1-C6 ALKYL, C3-C10 CYCLOALKYL, C5-C10 CYCLOALKENYL, AMONG OTHERS; R3 AND R4 ARE H, C1-C6 ALKYL, CF3; R5 IS OR13, NR14R15, NR11C (O) R10, AMONG OTHERS; R6 IS C1-C6 ALKYL OR C3-C10 CYCLOALKYL; R7 IS HALOGEN, OH, CF3, AMONG OTHERS; R8 IS H, HALO, CN, OH OR C1-C6 ALKYL; R10 IS H, C1-C6 ALKYL, C2-C6 ALKYL, AMONG OTHERS; R11 IS H, C1-C6 ALKYL, C2-C6 ALKYL, AMONG OTHERS; R13 IS C1-C6 ALKYL, C3-C10 CYCLOALKYL, C5-C10 CYCLOALKENYL, AMONG OTHERS; R14 IS H, CF3, C1-C6 ALKYL, AMONG OTHERS; R15 IS C1-C6 ALKYL, C2-C6 ALKYL, C2-C6 ALKYL, AMONG OTHERS. PREFERRED COMPOUNDS ARE: (3S) -3 - {[(4-CHLOROPHENYL9AMINE] METHYL} -1- (5-METHYL-7H-PYRROLO [2,3-d] PYRIMIDIN-4-IL) PYRROLIDIN-3-AMINE, 3 - ({[2-FLUORO-3- (TRIFLUOROMETIL) PHENYL] AMINO} METHYL) -1- (5-METHYL-7H-PYRROLO [2,3-d] PYRIMIDIN-4-IL) PYRROLIDIN-3-AMINE, ( 3S) -1- (5-METHYL-7H-PYRROLO [2,3-d] PYRIMIDIN-4-IL) -3 - {[3- (TRIFLUOROMETHYL) PHENYL] AMINO} METHYL) PYRROLIDIN-3-AMINE, AMONG OTHERS . IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SAID COMPOUNDS ARE INHIBITORS OF KINASE AKT AND / OR P70S6K1 AND ARE USEFUL IN THE TREATMENT OF CANCER CELLS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US82044106P | 2006-07-26 | 2006-07-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20080689A1 true PE20080689A1 (en) | 2008-06-14 |
Family
ID=38963178
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2007000962A PE20080689A1 (en) | 2006-07-26 | 2007-07-25 | KINASE INHIBITORS AMINE DERIVATIVES |
Country Status (7)
| Country | Link |
|---|---|
| AR (1) | AR062050A1 (en) |
| CL (1) | CL2007002188A1 (en) |
| GT (1) | GT200700062A (en) |
| PE (1) | PE20080689A1 (en) |
| TW (1) | TW200817408A (en) |
| UY (1) | UY30499A1 (en) |
| WO (1) | WO2008012635A2 (en) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE532789T1 (en) | 2006-07-06 | 2011-11-15 | Array Biopharma Inc | DIHYDROTHIENOPYRIMIDINES AS ACT PROTEIN KINASE INHIBITORS |
| KR20150041164A (en) | 2006-07-06 | 2015-04-15 | 어레이 바이오파마 인크. | Cyclopenta〔d〕pyrimidines as akt protein kinase inhibitors |
| US8063050B2 (en) | 2006-07-06 | 2011-11-22 | Array Biopharma Inc. | Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| US8329701B2 (en) | 2006-07-06 | 2012-12-11 | Array Biopharma Inc. | Dihydrofuro pyrimidines as AKT protein kinase inhibitors |
| UA99284C2 (en) | 2007-05-11 | 2012-08-10 | Елі Ліллі Енд Компані | P70 s6 kinase inhibitors |
| US9409886B2 (en) | 2007-07-05 | 2016-08-09 | Array Biopharma Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| AR067413A1 (en) | 2007-07-05 | 2009-10-07 | Genentech Inc | HETEROCICLICAL COMPOUNDS CONTAINING CYCLOPENTA [D] PYRIMIDINE INHIBITORS OF AKT PROTEINQUINASES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, METHOD OF PREPARATION AND USE OF THE SAME FOR THE TREATMENT OF HYPER-TROLIFERATIVE TIPERIFERATIVE AS-ISSUES |
| KR101624361B1 (en) | 2007-07-05 | 2016-05-25 | 어레이 바이오파마 인크. | Pyrimidyl cyclopentanes as akt protein kinase inhibitors |
| US8846683B2 (en) | 2007-07-05 | 2014-09-30 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as Akt protein kinase inhibitors |
| JP5608097B2 (en) | 2008-01-08 | 2014-10-15 | アレイ バイオファーマ、インコーポレイテッド | Pyrrolopyridine as a kinase inhibitor |
| CN101965347B (en) | 2008-01-09 | 2013-01-02 | 阵列生物制药公司 | Pyrazolopyridines as kinase inhibitors |
| US8853216B2 (en) | 2008-01-09 | 2014-10-07 | Array Biopharma, Inc. | Hydroxylated pyrimidyl cyclopentane as AKT protein kinase inhibitor |
| AU2009204025B2 (en) | 2008-01-09 | 2014-02-20 | Array Biopharma Inc. | Hydroxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| AU2013218743B2 (en) * | 2008-05-13 | 2016-04-28 | Array Biopharma Inc. | Pyrrolopyridines as kinase inhibitors |
| CL2009001152A1 (en) | 2008-05-13 | 2009-10-16 | Array Biopharma Inc | Compounds derived from n- (4- (nitrogen cycloalkyl-1-yl) -1h-pyrrolo [2,3-b] pyridin-3-yl) amide, kinase inhibitors; Preparation process; pharmaceutical composition; and its use for the treatment of a proliferative disease. |
| AR074072A1 (en) | 2008-11-11 | 2010-12-22 | Lilly Co Eli | COMPOSITE OF IMIDAZOL -PIPERIDIN -PIRROL-PIRIMIDIN-6-ONA, PHARMACEUTICAL COMPOSITION THAT INCLUDES IT AND ITS USE TO PREPARE A USEFUL MEDICINAL PRODUCT TO TREAT MULTIFORM GLIOBLASTOMA |
| AR074830A1 (en) | 2008-12-19 | 2011-02-16 | Cephalon Inc | PIRROLOTRIAZINAS AS ALK AND JAK2 INHIBITORS |
| DE102009005193A1 (en) * | 2009-01-20 | 2010-07-22 | Merck Patent Gmbh | Novel heterocyclic compounds as MetAP-2 inhibitors |
| US8481557B2 (en) | 2009-04-11 | 2013-07-09 | Array Biopharma Inc. | Method of treatment using checkpoint kinase 1 inhibitors |
| WO2011019780A1 (en) | 2009-08-11 | 2011-02-17 | Bristol-Myers Squibb Company | Azaindazoles as btk kinase modulators and use thereof |
| PL2473049T3 (en) | 2009-09-04 | 2019-07-31 | Biogen Ma Inc. | Bruton's tyrosine kinase inhibitors |
| WO2011082271A2 (en) | 2009-12-30 | 2011-07-07 | Arqule, Inc. | Substituted triazolo-pyrimidine compounds |
| ES2621857T3 (en) | 2010-11-16 | 2017-07-05 | Array Biopharma, Inc. | Combination of control point kinase 1 inhibitors and WEE1 kinase inhibitors |
| ES2617339T3 (en) | 2010-12-16 | 2017-06-16 | Calchan Limited | ASK1 inhibitor pyrrolopyrimidine derivatives |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| EP2694072B2 (en) | 2011-04-01 | 2024-08-07 | Genentech, Inc. | Combination of akt inhibitor compound and abiraterone for use in therapeutic treatments |
| CN103841976A (en) | 2011-04-01 | 2014-06-04 | 基因泰克公司 | Combinations of AKT and MEK inhibitor compounds and methods of use thereof |
| CN103930407B (en) * | 2011-09-12 | 2019-02-26 | 默克专利有限公司 | Aminopyrimidine derivatives useful as modulators of kinase activity |
| AR091273A1 (en) | 2012-06-08 | 2015-01-21 | Biogen Idec Inc | PYRIMIDINYL TIROSINE KINASE INHIBITORS |
| CN107652289B (en) | 2012-06-13 | 2020-07-21 | 因塞特控股公司 | Substituted tricyclic compounds as FGFR inhibitors |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| JP6449244B2 (en) | 2013-04-19 | 2019-01-09 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Bicyclic heterocycles as FGFR inhibitors |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (en) | 2015-02-20 | 2017-12-26 | Incyte Corp | BICYCLIC HETEROCYCLES USED AS FGFR4 INHIBITORS |
| ES2751669T3 (en) | 2015-02-20 | 2020-04-01 | Incyte Corp | Bicyclic heterocycles as FGFR inhibitors |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| WO2017004134A1 (en) * | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| HUE064656T2 (en) | 2016-03-28 | 2024-04-28 | Incyte Corp | Pyrrolotriazine compounds as TAM inhibitors |
| WO2018017153A1 (en) | 2016-07-21 | 2018-01-25 | Biogen Ma Inc. | Succinate forms and compositions of bruton's tyrosine kinase inhibitors |
| AR111960A1 (en) | 2017-05-26 | 2019-09-04 | Incyte Corp | CRYSTALLINE FORMS OF A FGFR INHIBITOR AND PROCESSES FOR ITS PREPARATION |
| EP3461480A1 (en) | 2017-09-27 | 2019-04-03 | Onxeo | Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer |
| CN119241541A (en) | 2018-05-04 | 2025-01-03 | 因赛特公司 | Solid forms of FGFR inhibitors and methods for preparing the same |
| PE20210919A1 (en) | 2018-05-04 | 2021-05-19 | Incyte Corp | SALTS FROM A FGFR INHIBITOR |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| GEP20247679B (en) | 2019-10-14 | 2024-10-10 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| IL293001A (en) | 2019-12-04 | 2022-07-01 | Incyte Corp | Derivatives of an fgfr inhibitor |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| JP2024513575A (en) | 2021-04-12 | 2024-03-26 | インサイト・コーポレイション | Combination therapy including FGFR inhibitor and Nectin-4 targeting agent |
| WO2022261160A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| AR126101A1 (en) | 2021-06-09 | 2023-09-13 | Incyte Corp | TRICYCLIC HETEROCYCLES AS FGFR INHIBITORS |
| WO2022272062A1 (en) * | 2021-06-24 | 2022-12-29 | Reservoir Neuroscience, Inc. | Ep2 antagonist compounds |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PA8474101A1 (en) * | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | PYROLEUM [2,3-D] PIRIMIDINE COMPOUNDS |
| MY179032A (en) * | 2004-10-25 | 2020-10-26 | Cancer Research Tech Ltd | Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors |
-
2007
- 2007-07-13 WO PCT/IB2007/002065 patent/WO2008012635A2/en not_active Ceased
- 2007-07-24 UY UY30499A patent/UY30499A1/en not_active Application Discontinuation
- 2007-07-24 GT GT200700062A patent/GT200700062A/en unknown
- 2007-07-24 AR ARP070103290A patent/AR062050A1/en unknown
- 2007-07-25 PE PE2007000962A patent/PE20080689A1/en not_active Application Discontinuation
- 2007-07-25 TW TW096127409A patent/TW200817408A/en unknown
- 2007-07-26 CL CL200702188A patent/CL2007002188A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2008012635A2 (en) | 2008-01-31 |
| CL2007002188A1 (en) | 2008-02-01 |
| TW200817408A (en) | 2008-04-16 |
| AR062050A1 (en) | 2008-08-10 |
| UY30499A1 (en) | 2008-02-29 |
| GT200700062A (en) | 2008-08-08 |
| WO2008012635A3 (en) | 2008-05-08 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD | Application declared void or lapsed |