AR075835A1 - Compuestos bis-aromaticos para su uso como inhibvidores de ltc4 sintasa - Google Patents
Compuestos bis-aromaticos para su uso como inhibvidores de ltc4 sintasaInfo
- Publication number
- AR075835A1 AR075835A1 ARP100100797A ARP100100797A AR075835A1 AR 075835 A1 AR075835 A1 AR 075835A1 AR P100100797 A ARP100100797 A AR P100100797A AR P100100797 A ARP100100797 A AR P100100797A AR 075835 A1 AR075835 A1 AR 075835A1
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- Argentina
- Prior art keywords
- optionally substituted
- substituents selected
- alkyl
- independently represent
- hydrogen
- Prior art date
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- 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
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Abstract
Dichos compuestos son de utilidad en el tratamiento de enfermedades en donde se desea, y/o requiere inhibir la leucotrieno C4 sintasa y, en particular, en el tratamiento de un trastorno respiratorio y/o de una inflamacion. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula 1, donde uno de E2a, E2b y E2c representa -C(-L3-Y3)= y los otros dos respectivamente representan E2 y E3; Y representa -C(O)- o -C(=N-OR28)-; R28 representa hidrogeno o C1-6 alquilo opcionalmente sustituido con uno o más átomos de fluor; uno o dos de D1, D2 y D3 representa(n) -N=; y/o uno o dos de E1, E2, E3 y E4 representa(n) -N=; y los demás grupos D1, D2 y D3 representan cada uno en forma independiente -C(R1)=; y los demás grupos E1, E2, E3 y E4 representan cada uno en forma independiente -C(R2)=; cada R1 representa en forma independiente, en cada ocasion en que se lo usa en la presente, hidrogeno o un sustituyente seleccionado entre X1; cada R2 representa en forma independiente, en cada ocasion en que se lo usa en la presente, hidrogeno o un sustituyente seleccionado entre X2; Y1 representa -C(O)OR9a o 5-tetrazolilo; R9a representa: (i) hidrogeno; o (ii) C1-8 alquilo o un grupo heterocicloalquilo, de los cuales ambos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre G1 y/o Z1; uno de Y2 e Y3 representa un grupo arilo o un grupo heteroarilo (de los cuales ambos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre A) y el otro representa: (a) un grupo arilo o un grupo heteroarilo (de los cuales ambos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre A); o (b) C1-12 alquilo o un grupo heterocicloalquilo, de los cuales ambos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre G1 y/o Z1; A representa, en cada ocasion en que se lo usa en la presente: I) un grupo arilo o un grupo heteroarilo, de los cuales ambos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre B; II) C1-8 alquilo o un grupo heterocicloalquilo, de los cuales ambos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre G1 y/o Z1; o III) un grupo G1; X1, X2, G1 y B representan en forma independiente halo, -R5a, -C(O)R5b, -CN, -NO2, -C(O)N(R6a)R7a, -N(R6b)R7b, -N(R5c)C(O)R6c, -N(R5b)C(O)OR6d, -OR5e, -OS(O)2R5f, -S(O)mR5g, -OC(O)R5h o -S(O)2N(R6e)R7e; R5b a R5e, R5g, R5h, R6a a R6c, R6e, R7a, R7b y R7e representan en forma independiente, en cada ocasion en que se lo usa en la presente, H o R5a; o cualquiera de los pares R6a y R7a, R6b y R7b, o R6e y R7e se pueden unir para formar, junto con el o los átomos a los cuales se encuentran unidos, un anillo de 3 a 6 miembros, cuyo anillo contiene opcionalmente un heteroátomo adicional (como por ejemplo nitrogeno u oxigeno) además del átomo de nitrogeno al cual estos sustituyentes se encuentran necesariamente unidos, y cuyo anillo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre fluoro, =O, -OR y/o R5a; R5f y R6d representan en forma independiente R5a; R5a representa, en cada ocasion en que se lo usa en la presente: (i) C1-6 alquilo opcionalmente sustituido con uno o más sustituyentes seleccionados entre fluoro, -CN, =O, -OR8a, -N(R8b)R8c, -S(O)nR8d y/o -S(O)2N(R8e)R8f; o (ii) arilo o heteroarilo, de los cuales ambos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre halo, -CN, -OR8a, -N(R8b)R8C, -S(O)nR8d y/o -S(O)2N(R8e)R8f; n representa 0, 1 o 2; cada R8a, R8b, R8d y R8d representa en forma independiente H o C1-6 alquilo opcionalmente sustituido con uno o más sustituyentes seleccionados entre fluoro, =O, -OR11a y/o -N(R12a)R12b; cada R8c y R8f representa en forma independiente H o C1-3 alquilo opcionalmente sustituido con uno o más sustituyentes seleccionados entre F, =O, -OR13a, -N(R14a)R14b, -S(O)2CH3, -S(O)-2CHF2 y/o -S(O)2CF3; o R8b y R8c y/o R8e y R8f se pueden unir para formar, junto con el o los átomos a los cuales se encuentran unidos, un anillo de 3 a 6 miembros, opcionalmente sustituido con uno o más sustituyentes seleccionados entre fluoro y C1-2 alquilo; R11a y R13a representan en forma independiente H o C1-3 alquilo opcionalmente sustituido con uno o más átomos de fluor; R12a, R12b, R14a y R14b representan en forma independiente H, -CH3 o -CH2CH3; Z1 representa, en cada ocasion en que se lo usa en la presente, =O o =NOR16b; representa hidrogeno o C1-6 alquilo opcionalmente sustituido con uno o más átomos de fluor; L1 representa una union simple o -(CH2)p-Q-(CH2)q-; Q representa -C(Ry1)(Ry2)-, -C(O)-, -N(Ry3)- o -O-; p y q representan en forma independiente 0, 1 o 2, pero donde la suma de p y q no excede 2; L2 y L3 representan en forma independiente una union simple o un grupo separador seleccionado entre -S(O)n1-, -C(Ry4)(Ry5)-, -N(R17a)-A16-, -OA17- y -C(O)-A17; n1 representa 0, 1 o 2; A16 representa una union directa, -C(Ry6)(Ry7)-, -C(O)-, C(O)N(R17b), -C(O)C(Ry6)(Ry7)- o -S(O)2-; A17 representa una union directa o -C(Ry8)(Ry9)-; cada Ry1, Ry2, Ry4, Ry5, Ry6, Ry7, Ry8 y Ry9 representa en forma independiente H, fluoro o C1-3 alquilo opcionalmente sustituido con uno o más átomos de fluor; o Ry1, Ry2, Ry4, Ry5, Ry6, Ry7, Ry8 y Ry9 pueden estar unidos para formar un anillo de 3 a 6 miembros opcionalmente sustituido con uno o más sustituyentes seleccionados entre fluoro y C1-2 alquilo; Ry3 representa hidrogeno o C1-3 alquilo; R17a y R17b representan en forma independiente hidrogeno, C1-6 alquilo (opcionalmente sustituido con uno o más sustituyentes seleccionados entre heterocicloalquilo, arilo, fluoro, -CN, -OR19 y/o =O), arilo o heteroarilo (de los cuales ambos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre halo, -R18a, -C(O)R18b, -CN, -C(O)N(R18c)R18d, -N(R18e)R18f, -N(R18g)C(O)R18h, -N(R18i)C(O)OR18j, -OR18k, -OS(O)2R18m, -S(O)mR18n, -OC(O)R18p y/o -S(O)2N(R18q)(R18r); m representa 0, 1 o 2; R18a, R18b, R18C, R18d, R18e, R18f, R18g, R18h, R18i, R18k, R18n, R18p, R18q y R18r representan en forma independiente hidrogeno o C1-3 alquilo opcionalmente sustituido con uno o más átomos de fluor; R18j y R18m representan en forma independiente C1-3 alquilo opcionalmente sustituido con uno o más átomos de fluor; R19 representa hidrogeno o C1-6 alquilo opcionalmente sustituido con uno o más átomos de fluor; o una sal aceptable farmacéuticamente del mismo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US20254909P | 2009-03-12 | 2009-03-12 |
Publications (1)
Publication Number | Publication Date |
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AR075835A1 true AR075835A1 (es) | 2011-04-27 |
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ID=42133546
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100100797A AR075835A1 (es) | 2009-03-12 | 2010-03-12 | Compuestos bis-aromaticos para su uso como inhibvidores de ltc4 sintasa |
Country Status (8)
Country | Link |
---|---|
US (2) | US20120004244A1 (es) |
EP (1) | EP2406219A1 (es) |
JP (1) | JP2012520275A (es) |
CN (1) | CN102348686A (es) |
AR (1) | AR075835A1 (es) |
CA (1) | CA2754781A1 (es) |
TW (1) | TW201035050A (es) |
WO (1) | WO2010103278A1 (es) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2545036A1 (en) | 2010-03-12 | 2013-01-16 | Biolipox AB | Bis aromatic compounds for use as ltc4 synthase inhibitors |
JP6261340B2 (ja) * | 2010-11-18 | 2018-01-17 | リガンド ファーマシューティカルズ インコーポレイテッド | 造血成長因子模倣体の使用 |
WO2015129859A1 (ja) * | 2014-02-28 | 2015-09-03 | キッセイ薬品工業株式会社 | 新規なアニリン誘導体、それを含有する医薬組成物およびそれらの用途 |
GB201507753D0 (en) | 2015-05-06 | 2015-06-17 | Biolipox Ab | New compounds and uses |
EP3833352A4 (en) * | 2018-08-10 | 2022-04-06 | University of Central Florida Research Foundation, Inc. | NON-POLYAMINE BASED TRANSPORT INHIBITORS AND THEIR USE IN THE TREATMENT OF HUMAN CANCER |
WO2020234103A1 (en) | 2019-05-21 | 2020-11-26 | Bayer Aktiengesellschaft | Identification and use of kras inhibitors |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1771450B9 (en) | 2004-05-14 | 2008-12-24 | Millennium Pharmaceuticals, Inc. | Compounds and methods for inhibiting mitotic progression by inhibition of aurora kinase |
US8097623B2 (en) | 2005-01-19 | 2012-01-17 | Biolipox Ab | Indoles useful in the treatment of inflammation |
WO2008107661A1 (en) * | 2007-03-05 | 2008-09-12 | Biolipox Ab | New methylenebisphenyl compounds useful in the treatment of inflammation |
AU2008294535A1 (en) | 2007-09-04 | 2009-03-12 | Biolipox Ab | BIS-aromatic compounds useful in the treatment of inflammation |
-
2010
- 2010-03-12 US US13/256,003 patent/US20120004244A1/en not_active Abandoned
- 2010-03-12 CN CN2010800110410A patent/CN102348686A/zh active Pending
- 2010-03-12 WO PCT/GB2010/000438 patent/WO2010103278A1/en active Application Filing
- 2010-03-12 AR ARP100100797A patent/AR075835A1/es unknown
- 2010-03-12 JP JP2011553512A patent/JP2012520275A/ja active Pending
- 2010-03-12 CA CA2754781A patent/CA2754781A1/en not_active Abandoned
- 2010-03-12 TW TW099107187A patent/TW201035050A/zh unknown
- 2010-03-12 EP EP10709919A patent/EP2406219A1/en not_active Withdrawn
-
2011
- 2011-03-14 US US13/634,221 patent/US20130035358A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
US20130035358A1 (en) | 2013-02-07 |
EP2406219A1 (en) | 2012-01-18 |
JP2012520275A (ja) | 2012-09-06 |
CA2754781A1 (en) | 2010-09-16 |
CN102348686A (zh) | 2012-02-08 |
WO2010103278A1 (en) | 2010-09-16 |
TW201035050A (en) | 2010-10-01 |
US20120004244A1 (en) | 2012-01-05 |
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