AR067413A1 - Compuestos heterociclicos que contienen ciclopenta[d]pirimidina inhibidores de proteinquinasas akt, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de las mismas para el tratamiento de enfermedades hiperproliferativas, tales como cancer - Google Patents
Compuestos heterociclicos que contienen ciclopenta[d]pirimidina inhibidores de proteinquinasas akt, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de las mismas para el tratamiento de enfermedades hiperproliferativas, tales como cancerInfo
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- AR067413A1 AR067413A1 ARP080102885A ARP080102885A AR067413A1 AR 067413 A1 AR067413 A1 AR 067413A1 AR P080102885 A ARP080102885 A AR P080102885A AR P080102885 A ARP080102885 A AR P080102885A AR 067413 A1 AR067413 A1 AR 067413A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- phenyl
- membered
- troliferative
- tiperiferative
- Prior art date
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- 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
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- A61P3/00—Drugs for disorders of the metabolism
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- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- 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
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Abstract
Reivindicacion 1: Un compuesto de la formula (1) y sus enantiomeros y sales, donde: G es fenilo, naftaleno, un heteroarilo de 5-6 miembros o un heteroarilo bicíclico de 9-10 miembros, donde el fenilo, naftaleno, o heteroarilo de 5-6 miembros o heteroarilo bicíclico de 9-10 miembros están opcionalmente sustituidos con uno a cuatro grupos Ra; R1 y R1a se seleccionan, de manera independiente, de H, Me, Et, -CH=CH2, -CH2OH, CF3, CHF2 o CH2F; R2 es H, -OH, -OMe o F; R2a es H, Me o F, o R2 y R2a son oxo; R3es H, Me, Et, o CF3; R4 es H, heterociclo de 4-6 miembros, ciclopropilmetilo o alquilo C1-4 opcionalmente sustituido con F, -OH o -Oalquilo C1-3; R5 y R5a se seleccionan, de manera independiente, de H y alquilo C1-4; o R5 y R5a junto con el átomo al cual están unidos forman un grupo carbonilo, un cicloalquilo de 5-6 miembros o un heterociclo de 5-6 miembros, donde el heterociclo tiene un heteroátomo de oxigeno; cada Ra es, de manera independiente, halogeno, alquilo C1-6, cicloalquilo C3-6, -O-alquilo C1-6, CF3, -OCF3, Salquilo C1-6, CN, fenilo, -OCH2-fenilo, NH2, -NO2, -NH-alquilo C1-6, -N-(alquilo C1-6)2, piperidina, pirrolidina, pirazol piridina, 2-aminopiridina, CH2F, CHF2, -OCH2F, -OCHF2, -OH, -SO2alquilo C1-6, C(O)NH2, C(O)NHalquilo C1-6 y C(O)N(alquilo C1-6)2 y j es 1 o 2; y cuando j es 2, el carbono de anillo de j opuesto a NR4 puede ser reemplazado con un heteroátomo O.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US94813807P | 2007-07-05 | 2007-07-05 | |
US2008808P | 2008-01-09 | 2008-01-09 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR067413A1 true AR067413A1 (es) | 2009-10-07 |
Family
ID=40076864
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP080102885A AR067413A1 (es) | 2007-07-05 | 2008-07-03 | Compuestos heterociclicos que contienen ciclopenta[d]pirimidina inhibidores de proteinquinasas akt, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de las mismas para el tratamiento de enfermedades hiperproliferativas, tales como cancer |
Country Status (20)
Country | Link |
---|---|
US (1) | US8618097B2 (es) |
EP (1) | EP2170863B1 (es) |
JP (2) | JP5628028B2 (es) |
KR (2) | KR101650956B1 (es) |
CN (2) | CN103396409B (es) |
AR (1) | AR067413A1 (es) |
AU (1) | AU2008272830B8 (es) |
BR (1) | BRPI0813999A2 (es) |
CA (1) | CA2692502C (es) |
CO (1) | CO6251283A2 (es) |
CR (1) | CR11229A (es) |
EC (1) | ECSP109937A (es) |
ES (1) | ES2551352T3 (es) |
HK (1) | HK1147255A1 (es) |
MA (1) | MA31679B1 (es) |
NZ (1) | NZ582692A (es) |
RU (1) | RU2486181C2 (es) |
SG (1) | SG185274A1 (es) |
TW (1) | TWI450720B (es) |
WO (1) | WO2009006567A2 (es) |
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US8846683B2 (en) | 2007-07-05 | 2014-09-30 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as Akt protein kinase inhibitors |
CN101959887B (zh) | 2008-01-08 | 2013-07-31 | 阵列生物制药公司 | 作为激酶抑制剂的吡咯并吡啶 |
EP2240483B8 (en) * | 2008-01-09 | 2013-04-03 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as akt protein kinase inhibitors |
ES2392014T3 (es) | 2008-01-09 | 2012-12-03 | Array Biopharma, Inc. | Pirazolopiridinas como inhibidores de la cinasa |
ES2401685T3 (es) * | 2008-01-09 | 2013-04-23 | Array Biopharma, Inc. | Pirimidil ciclopentano hidroxilado como inhibidor de la proteína quinasa AKT |
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JP6293655B2 (ja) | 2011-04-01 | 2018-03-14 | ジェネンテック, インコーポレイテッド | 癌治療に対する感受性を予測するためのバイオマーカー |
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CN104662015B (zh) | 2012-06-20 | 2017-03-29 | 诺华股份有限公司 | 补体途径调节剂及其用途 |
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JP6907319B2 (ja) | 2016-08-31 | 2021-07-21 | アエリエ ファーマシューティカルズ インコーポレイテッド | 眼科用組成物 |
EP3609871A4 (en) | 2017-03-31 | 2021-01-06 | Aerie Pharmaceuticals, Inc. | ARYL CYCLOPROPYL-AMINO-ISOQUINOLINYL AMIDE COMPOUNDS |
US11472799B2 (en) * | 2018-03-06 | 2022-10-18 | Icahn School Of Medicine At Mount Sinai | Serine threonine kinase (AKT) degradation / disruption compounds and methods of use |
KR20240095318A (ko) * | 2018-04-04 | 2024-06-25 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해 조절제 및 연관된 사용 방법 |
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