AR076942A1 - Derivados de amidas del acido 6,7-dihidro-5h-imidazo(1,2-a)imidazol-3-carboxilico - Google Patents

Derivados de amidas del acido 6,7-dihidro-5h-imidazo(1,2-a)imidazol-3-carboxilico

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Publication number
AR076942A1
AR076942A1 ARP100101925A ARP100101925A AR076942A1 AR 076942 A1 AR076942 A1 AR 076942A1 AR P100101925 A ARP100101925 A AR P100101925A AR P100101925 A ARP100101925 A AR P100101925A AR 076942 A1 AR076942 A1 AR 076942A1
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AR
Argentina
Prior art keywords
optionally substituted
alkyl
nr9r10
halogen
cycloalkyl
Prior art date
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ARP100101925A
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English (en)
Inventor
Rene Marc Lemieux
Steven Richard Brunette
Joshua Courtney Horan
Jennifer A Kowalski
Michael David Lawlor
Bryan Mckibben
Craig Andrew Miller
Antonio Barbosa
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Boehringer Ingelheim Int
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Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR076942A1 publication Critical patent/AR076942A1/es

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    • 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
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • 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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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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Abstract

Derivados de amida del ácido 6,7-dihidro-5H-imidazo[1,2-a]imidazol-3-carboxílico exhiben efecto inhibidor tras la interaccion entre CAMs y Leucointegrinas y, por consiguiente, en el tratamiento de enfermedades inflamatorias. Composiciones farmacéuticas. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula (1) en donde R1 se selecciona de -CN, -OCF3, -CF3, halogeno, heteroarilo, opcionalmente sustituido con halogeno o alquilo C1-3, y fenilo, opcionalmente sustituido con halogeno; R2 es -Cl o -CF3; R3 es H o halogeno; X es un grupo de formula (2), en la que R4 se selecciona de (A) -H; (B) alquilo C1-3 opcionalmente sustituido con uno o dos grupos seleccionados de cicloalquilo C3-6, -OR9, -NR9R10, -SOR9, -SO2R9, -C(O)NR9R10, -C(O)OR9, heteroarilo opcionalmente sustituido con alquilo C1-3, heterociclilo, opcionalmente sustituido con alquilo C1-3; y fenilo, opcionalmente sustituido con alquilo C1-3; (C) cicloalquilo C3-6; (D) heteroarilo; y (E) fenilo, opcionalmente sustituido con halogeno, -OR9, -CN o -CF3; R5 es H o alquilo C1-3; o R4 y R5, junto con el carbono al que están unidos, forman un anillo hidrocarbonado saturado con 3 - 7 átomos de carbono y en donde un átomo de carbono en dicho anillo hidrocarbonado puede estar opcionalmente reemplazado por -O-, -S-, -S(O)-, -SO2-, NH-, -NCH3- o -NC(O)CH3-; Y es un grupo de formula (3) en la que R6 es H o alquilo C1-3; R7es H o alquilo C1-3; o R6 y R7, junto con el carbono al que están unidos, forman un anillo hidrocarbonado saturado con 3 - 7 átomos de carbono, en donde un átomo de carbono en dicho anillo hidrocarbonado puede estar opcionalmente reemplazado por -O-, -S-, -S(O)-, -SO2-, NH-, -NCH3- o -NC(O)CH3-; Z es arilo o heteroarilo; R8 se selecciona de (A) arilo, opcionalmente sustituido con uno o dos grupos seleccionados de alquilo C1-3, opcionalmente sustituido con -OR9, -NR9R10 o -NR9SO2R10; cicloalquilo C3-7, opcionalmente sustituido con -OR9 o -NR9R10; -OR9; halogeno; -C(O)NR9R10, -SO2NR9R10; -NR9(CO)R10, -SO2R9, -NR9R10, -CN; -C(O)OR9, -NR9SO2R10 y -C(O)R9; (B) heteroarilo, opcionalmente sustituido con uno o dos grupos seleccionados de alquilo C1-3, opcionalmente sustituido con -OR9, -NR9R10 o halogeno; cicloalquilo C3-7, opcionalmente sustituido con -OR9, -NR9R10; -OR9, halogeno; -C(O)NR9R10, -SO2NR9R10, -NR9(CO)R10, -SO2R9, -NR9R10; y -CN; R9 se selecciona de H, alquilo C1-5 o cicloalquilo C3-7; R10 se selecciona de H, alquilo C1-5 o cicloalquilo C3-7; o una de sus sales farmacéuticamente aceptable.
ARP100101925A 2009-06-02 2010-06-01 Derivados de amidas del acido 6,7-dihidro-5h-imidazo(1,2-a)imidazol-3-carboxilico AR076942A1 (es)

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US18309809P 2009-06-02 2009-06-02

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AR076942A1 true AR076942A1 (es) 2011-07-20

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US (1) US8575360B2 (es)
EP (1) EP2445909B1 (es)
JP (1) JP5384732B2 (es)
KR (1) KR20120024699A (es)
CN (1) CN102448960A (es)
AR (1) AR076942A1 (es)
AU (1) AU2010256994A1 (es)
BR (1) BRPI1012581A2 (es)
CA (1) CA2764296A1 (es)
CL (1) CL2011003076A1 (es)
DK (1) DK2445909T3 (es)
EA (1) EA019990B1 (es)
ES (1) ES2446352T3 (es)
IL (1) IL215521A0 (es)
MX (1) MX2011012717A (es)
NZ (1) NZ595622A (es)
PL (1) PL2445909T3 (es)
TW (1) TWI443099B (es)
WO (1) WO2010141273A1 (es)

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WO2018166855A1 (en) 2017-03-16 2018-09-20 Basf Se Heterobicyclic substituted dihydroisoxazoles
WO2018234488A1 (en) 2017-06-23 2018-12-27 Basf Se SUBSTITUTED CYCLOPROPYL DERIVATIVES

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JP5485164B2 (ja) * 2007-11-29 2014-05-07 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ６，７−ジヒドロ−５Ｈ−イミダゾ［１，２−ａ］イミダゾール−３−カルボン酸アミドの誘導体
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