AR082391A1 - Inhibidores biciclicos de acetil-coa y usos de los mismos - Google Patents
Inhibidores biciclicos de acetil-coa y usos de los mismosInfo
- Publication number
- AR082391A1 AR082391A1 ARP110102709A ARP110102709A AR082391A1 AR 082391 A1 AR082391 A1 AR 082391A1 AR P110102709 A ARP110102709 A AR P110102709A AR P110102709 A ARP110102709 A AR P110102709A AR 082391 A1 AR082391 A1 AR 082391A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- carbon atoms
- amino
- alkoxy
- independently
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 36
- 125000004432 carbon atom Chemical group C* 0.000 abstract 31
- 125000000623 heterocyclic group Chemical group 0.000 abstract 12
- 125000003545 alkoxy group Chemical group 0.000 abstract 11
- 229910052739 hydrogen Inorganic materials 0.000 abstract 10
- 239000001257 hydrogen Substances 0.000 abstract 10
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 9
- 229910052799 carbon Inorganic materials 0.000 abstract 9
- 229910052736 halogen Inorganic materials 0.000 abstract 9
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 8
- 150000002367 halogens Chemical class 0.000 abstract 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 7
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 7
- 229910052757 nitrogen Inorganic materials 0.000 abstract 7
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 7
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 abstract 6
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 abstract 6
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 4
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 4
- 125000004423 acyloxy group Chemical group 0.000 abstract 4
- 125000001589 carboacyl group Chemical group 0.000 abstract 4
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 abstract 3
- 125000004104 aryloxy group Chemical group 0.000 abstract 3
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 3
- -1 cyano, carboxyl Chemical group 0.000 abstract 3
- 229910052805 deuterium Inorganic materials 0.000 abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 150000002431 hydrogen Chemical class 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000005115 alkyl carbamoyl group Chemical group 0.000 abstract 2
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 239000013543 active substance Substances 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000005281 alkyl ureido group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 125000004001 thioalkyl group Chemical group 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
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- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
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- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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- A61K31/42—Oxazoles
- A61K31/423—Oxazoles condensed with carbocyclic rings
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Abstract
La presente proporciona un método para la elaboración de los compuestos de la fórmula (1), sus usos terapéuticos, combinaciones con otros de los agentes farmacológicamente activos, y composiciones farmacéuticas.Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en donde el anillo A es un sistema de anillo bicíclico seleccionado a partir del grupo de fórmulas (2) en donde la línea ondulada indica que el punto de unión de L1 está sobre el anillo A’; y en donde R1 puede reemplazar a un átomo de hidrógeno de cualquier enlace de CH en el anillo A; X1, por cada presentación, es independientemente CH o N; X2 es NR19, O, o S; X3, por cada presentación, es independientemente NR9, CH2, O, o S; r es 1 ó 2; el anillo B es ciclohexilo o fenilo; en el entendido de que, cuando el anillo B es fenilo, el anillo A es de fórmula (3) en donde R1a es hidrógeno, fenilo, fenil-amino, o un heteroarilo de 5 a 10 miembros, en donde R1a puede estar opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R13 independientemente seleccionados; y en donde, cuando R1a es un heteroarilo que comprende uno o más -NH-, el hidrógeno de cada grupo -NH- puede ser opcionalmente reemplazado con R22; Q se selecciona a partir del grupo de fórmulas (4) en donde la línea ondulada indica el punto de unión con el anillo B; X4 es -NR4- u -O-; q y n son cada uno independientemente 0, 1, 2, 3 ó 4; L1 es -NHSO2-, -SO2NH-, -NHSO2NH- o -NHC(O)NH-; R1 puede reemplazar a un átomo de hidrógeno de cualquier enlace de CH en el anillo A y, por cada presentación, es independientemente deuterio, hidroxilo, nitro, halógeno, ciano, carboxilo, formilo, alquilo C1-7, carbociclilo C3-8, alquenilo C2-7, alquinilo C2-7, alcoxilo C1-7, tioalquilo C1-7, cicloalcoxilo C3-8, arilo C6-10, arilo C6-10-alquilo C1-4, ariloxilo C6-10, amino, N-alquilo C1-7-amino, N,N-di-(alquilo C1-7)-amino, N-arilo C6-10-amino, heterociclilo de 3 a 10 miembros, N-(heterociclilo de 3 a 10 miembros)-amino, (heterociclilo de 3 a 10 miembros)-oxilo, heteroarilo de 5 a 10 miembros, (heteroarilo de 5 a 10 miembros)-alquilo C1-4, N-(heteroarilo de 5 a 10 miembros)-amino, (heteroarilo de 5 a 10 miembros)-oxilo, alcanoílo C1-7, alcoxilo C1-7-carbonilo, alcanoiloxilo C1-7, alquilo C1-7-amido, arilo C6-10-amido, (heterociclilo de 3 a 10 miembros)-amido, carbamoilo, N-alquilo C1-7-carbamoilo, N,N-di-(alquilo C1-7)-carbamoilo, alcoxilo C1-7-amido, alquilo C1-7-ureido, y arilo C6-10-ureido, en donde R1 está opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R13 independientemente seleccionados; y en donde, cuando R1 comprende un heterociclilo o un heteroarilo que comprende uno o más -NH-, el hidrógeno de cada grupo -NH- puede ser independientemente reemplazado opcionalmente con R22; o dos R1 sobre el mismo átomo de carbono, pueden formar juntos un oxo; o dos R1 sobre el mismo átomo de carbono, junto con el átomo de carbono con el que están unidos, forman un espiro-carbociclilo de 3 a 8 átomos de carbono; o dos R1 sobre átomos de carbono adyacentes, junto con los átomos de carbono con los que están unidos, pueden formar un carbociclilo de 3 a 8 átomos de carbono fusionado o fenilo, el cual puede estar opcionalmente sustituido con uno o más R13; y R2, por cada presentación, se selecciona independientemente a partir del grupo que consiste en hidroxilo, ciano, alquilo C1-7, alcoxilo C1-7, alquenilo C2-7, amino, alquilo C1-7-amino, di-(alquilo C1-7)-amino, alquilo C1-7-amido, alcoxilo C1-7-amido; en donde R2, por cada presentación, puede ser independientemente sustituido opcionalmente con uno o más halógenos; o dos o más grupos R2 sobre átomos de carbono no adyacentes forman juntos un puente de alquileno C1-4; o dos o más grupos R2 sobre átomos de carbono adyacentes, pueden formar un carbociclilo C3-8 fusionado; R3 se selecciona a partir del grupo que consiste en un alquilo C1-7, carbociclilo C3-8, carbociclilo C3-8-alquilo C1-4, arilo C6-10, arilo C6-10-alquilo C1-4, un heteroarilo de 5 a 10 miembros, un (heteroarilo de 5 a 10 miembros)-alquilo C1-4, un heterociclilo de 3 a 10 miembros, y un (heterociclilo de 3 a 10 miembros)-alquilo C1-4, en donde R3 está opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R14; y en donde, cuando R3 comprende un heteroarilo o heterociclilo, el cual comprende uno o más -NH-, el hidrógeno de cada grupo -NH- puede ser independientemente reemplazado opcionalmente con un alquilo C1-7; R4 es hidrógeno, alquilo C1-7, o alcoxilo C1-4-alquilo C1-4; o R3 y R4, junto con el átomo de nitrógeno con el que están unidos, forman un heterociclilo de 3 a 7 miembros, en donde el heterociclilo puede estar opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R15; y en donde, cuando el heterociclilo comprende uno o más -NH-, el hidrógeno de cada grupo -NH- puede ser independientemente reemplazado opcionalmente con R16; R13, por cada presentación, es independientemente deuterio, nitro, halógeno, ciano, hidroxilo, carboxilo, alquilo C1-7, cicloalquilo C3-8, alcoxilo C1-7, arilo C6-10, ariloxilo C6-10, heterociclilo de 3 a 10 miembros, heteroarilo de 5 a 10 miembros, amino, alquilo C1-7-amino, di-(alquilo C1-7)-amino, alcanoílo C1-7, alcoxilo C1-7-carbonilo, alcanoiloxilo C1-7, alquilo C1-7-amido, alcoxilo C1-7-amido, carbamoilo, N-alquilo C1-7-carbamoilo, N,N-di-(alquilo C1-7)-carbamoilo, alquilo C1-7-sulfonilo, alquilo C1-7-sulfoniloxilo, alquilo C1-7-sulfonamido, sulfamoilo, N-alquilo C1-7-sulfamoilo, o N,N-di-(alquilo C1-7)sulfamoilo, en donde R13 está opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R17 independientemente seleccionados; y en donde, cuando R13 es un heterociclilo o un heteroarilo que comprende uno o más -NH-, el hidrógeno de cada grupo -NH- puede ser independientemente reemplazado opcionalmente con R20; o dos R13 sobre el mismo átomo de carbono, pueden formar juntos un oxo o un espiro-carbociclilo C3-8; o dos R13 sobre átomos de carbono adyacentes, junto con los átomos de carbono con los que están unidos, pueden formar un heterociclilo de 3 a 7 miembros, el cual puede estar opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R17, y si el heterociclilo comprende uno o más grupos -NH-, el hidrógeno de cada grupo -NH- puede ser independientemente reemplazado opcionalmente con R20; R14, por cada presentación, es independientemente halógeno, hidroxilo, carboxilo, alcoxilo C1-7-carbonilo, alquilo C1-7, alcoxilo C1-7, cicloalquilo C3-8, arilo C6-10, o heteroarilo de 5 a 10 miembros, en donde R14 puede estar opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R24 independientemente seleccionados; o dos R14 sobre el mismo átomo de carbono, pueden formar juntos un oxo, un espiro-carbociclilo C3-8, o un espiro-heterociclilo de 3 a 7 miembros; o dos R14 sobre átomos de carbono adyacentes, junto con los átomos de carbono con los que están unidos, pueden formar un fenilo, el cual puede estar opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R24; R15, por cada presentación, se selecciona independientemente a partir del grupo que consiste en hidroxilo, carboxilo, alquilo C1-7, alcoxilo C1-7, carbociclilo C3-8, fenilo, y alcoxilo C1-7-carbonilo; en donde R15 puede estar opcionalmente sustituido sobre uno o más átomos de carbono con uno o más sustituyentes independientemente seleccionados a partir de halógeno, hidroxilo, alcoxilo C1-4; o dos R15 sobre el mismo átomo de carbono forman juntos un oxo, o junto con el átomo de carbono con el que están unidos, forman un cicloalquilo C2-8, o un heterociclilo de 3 a 10 miembros; o dos R15 sobre átomos de carbono adyacentes, junto con los átomos de carbono con los que están unidos, pueden formar un fenilo fusionado; R16, por cada presentación, se selecciona independientemente a partir del grupo que consiste en alquilo C1-7, carbociclilo C3-8, alcanoílo C1-7, alcoxilo C1-7-carbonilo, o heteroarilo de 5 a 10 miembros; R17, por cada presentación, se selecciona independientemente a partir de ciano, halógeno, hidroxilo, carboxilo, alquilo C1-7, alcoxilo C1-7, amino, alquilo C1-7-amino, di(alquilo C1-7)-amino, arilo C6-10-amino, arilo C6-10-alquilo C1-4-amino, alcoxilo C1-7-carbonilo, alcanoiloxilo C1-7, heterociclilo de 3 a 10 miembros, en donde R17 puede estar opcionalmente sustituido sobre uno o más átomos de carbono con uno o más de los siguientes independientemente seleccionados: halógeno, amino, alquilo C1-7, alcoxilo C1-7, halo-alquilo C1-7, carboxilo, o alcoxilo C1-7-carbonilo; y en donde, cuando R17 es un heterociclilo, el cual comprende uno o más -NH-, el hidrógeno de cada grupo -NH- puede ser independientemente reemplazado opcionalmente con R23; o dos R17 sobre el mismo átomo de carbono, pueden formar juntos un oxo; R18 es un alquilo C1-7, cicloalquilo C3-8, fenilo o un alcoxilo C1-7-alquilo C1-7; R19, por cada presentación, es independientemente hidrógeno, alquilo C1-7, alcanoílo C1-7, tri-(alquilo C1-7)-sililo, cicloalquilo C3-8, alcoxilo C1-7-carbonilo, cicloalcoxilo C3-8-carbonilo, carbamoilo, N-alquilo C1-7-carbamoilo, N,N-di-(alquilo C1-7)-carbamoilo, o arilo C6-10-alquilo C1-4; en donde R19 está opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R21; R20, R21, R22, y R23, por cada presentación, son independientemente deuterio, halógeno, carboxilo, alquilo C1-7, alcoxilo C1-7, ariloxilo C6-10, arilo C6-10-alcoxilo C1-4, o alcoxilo C1-7-carbonilo; y R24, por cada presentación, es independientemente hidroxilo, halógeno, carboxilo, alquilo C1-7, halo-alquilo C1-7, alcoxilo C1-7, amino, N-alquilo C1-7-amino, N,N-di(alquilo C1-7)-amino, alcoxilo C1-7-carbonilo, alcanoiloxilo C1-7, fosfono-oxilo, alcoxilo C1-7-(hidroxi)-fosforiloxilo o di-(alcoxilo C1-7)-fosforiloxilo; en donde R24 puede estar opcionalmente sustituido sobre uno o más átomos de carbono con un grupo independientemente seleccionado a partir de amino, N-al
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-
2011
- 2011-07-25 US US13/189,760 patent/US8697739B2/en not_active Expired - Fee Related
- 2011-07-27 ES ES11741554.7T patent/ES2641833T3/es active Active
- 2011-07-27 AR ARP110102709A patent/AR082391A1/es unknown
- 2011-07-27 EP EP11741554.7A patent/EP2598486B1/en not_active Not-in-force
- 2011-07-27 WO PCT/EP2011/062933 patent/WO2012013716A1/en active Application Filing
- 2011-07-27 JP JP2013521136A patent/JP5998133B2/ja not_active Expired - Fee Related
- 2011-07-27 CN CN201180035809.2A patent/CN103339111B/zh not_active Expired - Fee Related
- 2011-07-28 TW TW100126860A patent/TW201206907A/zh unknown
- 2011-07-28 UY UY0001033536A patent/UY33536A/es not_active Application Discontinuation
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2014
- 2014-02-24 US US14/188,647 patent/US9789118B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
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JP5998133B2 (ja) | 2016-09-28 |
CN103339111A (zh) | 2013-10-02 |
TW201206907A (en) | 2012-02-16 |
US8697739B2 (en) | 2014-04-15 |
US9789118B2 (en) | 2017-10-17 |
CN103339111B (zh) | 2015-12-16 |
EP2598486A1 (en) | 2013-06-05 |
JP2013533279A (ja) | 2013-08-22 |
US20120028969A1 (en) | 2012-02-02 |
ES2641833T3 (es) | 2017-11-14 |
WO2012013716A1 (en) | 2012-02-02 |
UY33536A (es) | 2012-02-29 |
US20140171363A1 (en) | 2014-06-19 |
EP2598486B1 (en) | 2017-06-28 |
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