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AR052177A1 - Medicamentos para el tratamiento o la prevencion de enfermedades fibroticas - Google Patents

Medicamentos para el tratamiento o la prevencion de enfermedades fibroticas

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Publication number
AR052177A1
AR052177A1 ARP050105468A ARP050105468A AR052177A1 AR 052177 A1 AR052177 A1 AR 052177A1 AR P050105468 A ARP050105468 A AR P050105468A AR P050105468 A ARP050105468 A AR P050105468A AR 052177 A1 AR052177 A1 AR 052177A1
Authority
AR
Argentina
Prior art keywords
group
alkyl
amino
3alkyl
alkoxy
Prior art date
Application number
ARP050105468A
Other languages
English (en)
Inventor
John Edward Park
Gerald Juergen Roth
Armin Heckel
Nveed Chaudhary
Trixi Brandl
Georg Dahmann
Matthias Grauert
Original Assignee
Boehringer Ingelheim Int
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=36602118&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR052177(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR052177A1 publication Critical patent/AR052177A1/es

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • 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
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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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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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    • 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
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    • 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
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    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
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Abstract

La presente se refiere al uso de indolinonas de formula general (1) sustituidas en la posicion 6, en donde: X significa un átomo de oxígeno o azufre; R1 significa un átomo de hidrogeno o grupo profármaco; R2 significa grupo carboxi, grupo alcoxiC1-6- carbonilo de cadena lineal o ramificado, grupo cicloalcoxiC4-7-carbonilo o grupo ariloxicarbonilo; grupo alcoxiC1-6-carbonilo de cadena lineal o ramificado, que está sustituido en el extremo en el resto alquilo con grupo fenilo, heteroarilo, carboxi, alcoxiC13-carbonilo, aminocarbonilo, alquilC1-3-aminocarbonilo o di-(alquilC1-3)-aminocarbonilo; grupo alcoxiC2-6-carbonilo de cadena lineal o ramificado, que está sustituido en el extremo en el resto alquilo con un átomo de cloro o grupo hidroxi, alcoxi C1-3, amino, alquilC1-3-amino o di-(alquilC1-3)-amino; grupo aminocarbonilo o metilaminocarbonilo, grupo etilaminocarbonilo opcionalmente sustituido en la posicion 2 del grupo con un grupo hidroxi o alcoxi C1-3 o grupo di-(alquilC1- 2)-aminocarbonilo; R3 significa un átomo de hidrogeno, grupo alquilo C1-6, cicloalquilo C3-7, trifluorometilo o heteroarilo; grupo fenilo o naftilo, grupo fenilo o naftilo mono- o di-sustituido con un átomo de fluoro, cloro, bromo o yodo, con un grupo trifluorometilo, alquilo C1-3 o alcoxi C1-3, mientras que en el caso de disustitucion los sustituyentes pueden ser idénticos o diferentes y en donde los grupos fenilo y naftilo no sustituidos, así como mono- y di-sustituidos antes mencionados pueden estar adicionalmente sustituidos con grupo hidroxi, hidroxi-alquiloC1-3 o alcoxiC1-3-alquilo-C1-3, con grupo ciano, carboxi, carboxi-alquiloC1-3, alcoxiC1-3-carbonilo, aminocarbonilo, alquilC1-3-amino-carbonilo o di-alquilC1-3)- aminocarbonilo; con grupo nitro; con grupo amino, alquilC1-3-amino, di-(alquilC1-3)-amino o amino-alquiloC1-3; con grupo alquilC1-3-carbonilamino, N-(alquilC1-3)-alquil-C1-3-carbonilamino, alquilC1-3-carbonilamino-alquiloC1-3, N-(alquilC1-3)- alquilC1-3-carbonilamino-alquiloC1-3, alquilC1-3-sulfonilamino, alquilC1-3-sulfonilamino-alquiloC1-3, N-(alquilC1-3)-alquilC1-3-sulfonilamino-alquiloC1-3 o aril-alquiloC1-3- sulfonilamino; con grupo cicloalquilamino, cicloalquilenimino, cicloalquileniminocarbonilo, cicloalquilenimino-alquiloC1-3, cicloalquileniminocarbonilo-alquiloC1-3 o cicloalquileniminosulfonil-alquiloC1-3 con 4 a 7 miembros del anillo en cada caso, mientras que en cada caso el grupo metileno en la posicion 4 de grupo cicloalquilenimino de 6 o 7 miembros puede estar reemplazado por un átomo de oxígeno o azufre, por grupo sulfinilo, sulfonilo, -NH o -NalquiloC1-3; o con un grupo heteroarilo o heteroaril-alquiloC1-3; R4 significa grupo cicloalquilo C3-7; mientras que el grupo metileno en la posicion 4 de un grupo cicloalquilo de 6 o 7 miembros puede estar sustituido con grupo amino, alquilC1-3-amino o di-(alquilC1-3)-amino, o puede estar reemplazado por un grupo -NH o -NalquiloC1-3; o grupo fenilo sustituido con el grupo R6, que puede estar adicionalmente mono- o di-sustituido con átomo de fluoro, cloro, bromo o yodo, con grupos alquilo C1-5, trifluorometilo, hidroxi, alcoxi C1-3, carboxi, alcoxiC1-3-carbonilo, amino, acetilamino, alquilC1-3- sulfonilamino, aminocarbonilo, alquilC1-3-aminocarbonilo, di-(alquilC1-3)-aminocarbonilo, aminosulfonilo, alquilC1-3-aminosulfonilo, di-(alquilC1-3)- aminosulfonilo, nitro o ciano, en donde los sustituyentes pueden ser idénticos o diferentes y en donde: R6 significa un átomo de hidrogeno, fluoro, cloro, bromo o yodo; grupo ciano, nitro, amino, alquilo C1-5, cicloalquilo C3-7, trifluorometilo, fenilo, tetrazolilo o heteroarilo; el grupo de formula (2), en donde los átomos de hidrogeno unidos a un átomo de nitrogeno pueden estar reemplazados, en cada caso independientemente uno de otro, con grupo alquilo C1-3; grupo alcoxi C1-3, grupo alcoxiC1-3-alcoxiC1-3, fenil-alcoxi-C1-3, amino-alcoxiC2-3, alquilC1-3-amino-alcoxiC2-3, di-(alquilC1-3)- amino-alcoxiC2-3, fenil-alquilC1-3-amino-alcoxiC2-3, N-(alquilC1-3)-fenil- alquilC1-3-amino-alcoxiC2-3, cicloalquilenC5-7-imino-alcoxiC2-3 o alquilC1-3-mercapto; un grupo carboxi, alcoxiC1-4-carbonilo, aminocarbonilo, alquilC1-3aminocarbonlo, N- (alquilC1-5)-alquilC1-3-aminocarbonilo, fenil-alquilC1-3-aminocarbonilo, N-(alquilC1-3)- fenil-alquilC1-3-aminocarbonilo, piperazinocarbonilo o N-(alquilC1-3)-piperazinocarbonilo; grupo alquilC1-3-aminocarbonilo o N-(alquilC1-5)-alquilC1-3- aminocarbonilo, en donde un resto alquilo está sustituido con grupo carboxi o alcoxiC1-3-carbonilo, o en la posicion 2 o 3 está sustituido con grupo di-(alquilC1-3)-amino, piperazino, N-(alquilC1-3)-piperazino o un grupo cicloalquilenimino de 4 a 7 miembros; grupo cicloalquilC3-7-carbonilo; en donde el grupo metileno en la posicion 4 del resto cicloalquilo de 6 o 7 miembros puede estar sustituido con grupo amino, alquilC1-3-amino o di-(alquilC1-3)-amino, o puede estar reemplazado por un grupo - NH o - NalquiloC1-3; grupo cicloalquilenimino de 4 a 7 miembros, en donde grupo metileno enlazado al grupo imino puede estar reemplazado por grupo carbonilo o sulfonilo; o el resto cicloalquileno puede estar condensado a un anillo fenilo, o uno o los dos átomos de hidrogeno puede estar cada uno reemplazado por un grupo alquilo C1-3; y/o en cada caso el grupo metileno en la posicion 4 de grupo cicloalquilenimino de 6 o 7 miembros puede estar sustituido con grupo carboxi, alcoxiC1-3-carbonilo, aminocarbonilo, alquilC1-3- aminocarbonilo, di-(alquilC1-3)-aminocarbonilo, fenil-alquilC1-3-amino o N-(alquilC1-3)-fenil-alquilC1-3-amino; o puede estar reemplazado por un átomo de oxígeno o azufre, por grupo sulfinilo, sulfonilo, -NH, -NalquiloC1- 3, -Nfenilo, -NalquilC1-3-carbonilo o - Nbenzoilo; grupo alquilo C1-4 sustituido con el grupo R7, en donde R7 significa grupo cicloalquilo C3-7; mientras que el grupo metileno en la posicion 4 de grupo cicloalquilo de 6 o 7 miembros puede estar sustituido con grupo amino, alquilC1-3-amino o di-(alquilC1-3)- amino, o puede estar reemplazado por grupo -NH o -NalquiloC1-3; o en grupo cicloalquilo de 5 a 7 miembros, grupo -(CH2)2 puede estar reemplazado por grupo -CO-NH, grupo -(CH2)3 puede estar reemplazado por grupo -NH-CO-NH o -CO-NH-CO, o grupo -(CH2)4 puede estar reemplazado por grupo -NH-CO-NH-CO, mientras que en cada caso un átomo de hidrogeno unido a un átomo de nitrogeno puede estar reemplazado por grupo alquilo C1-3; grupo arilo o heteroarilo; grupo hidroxi o alcoxi C1-3; grupo amino, alquilC1-7-amino, di-(alquilC1-7)-amino, fenilamino, N-fenil-alquilC1-3-amino, fenil-alquilC1-3-amino, N-(alquilC1-3)-fenil-alquilC1-3-amino o di-(fenil- alquilC1-3)-amino; grupo omega- hidroxiC2-3-amino, N-(alquilC1-3)-omega-hidroxi-alquilC2-3-amino, di-(omega-hidroxi-alquilC2-3)- amino, di-(omega-(alcoxiC1-3)-alquilC2-3)-amino o N-(dioxolan-2-il)-alquilC1-3amino; grupo alquilC1-3-carbonilamino-alquilC2-3-amino o alquilC1-3- carbonilamino-alquilC2-3-N-(alquilC1-3)-amino; grupo alquilC1-3-sulfonilamino, N-(alquilC1-3)-alquilC1-3-sulfonilamino, alquilC1-3-sulfonilamino-alquilC2-3-amino o grupo alquilC1-3-sulfonilamino-alquilC2-3-N-(alquilC1-3)-amino; grupo hidroxicarbonil- alquilC1-3-amino o N-(alquilC1-3)-hidroxicarbonil-alquilC1-3-amino; grupo guanidino, en donde uno de o los dos átomos de hidrogeno puede estar cada uno reemplazado por grupo alquilo C1-3; grupo de formula: -N(R8)-CO-(CH2)n-R9, en la que: R8 significa un átomo de hidrogeno o grupo alquilo C1-3; n significa uno de los numero 0, 1, 2 o 3 y R9 significa un grupo amino, alquilC1-4-amino, di-(alquilC1-4)-amino, fenilamino, N-(alquilC1-4)-fenilamino, bencilamino, N-(alquilC1-4)-bencilamino o alcoxi C1-4, grupo cicloalquilenimino de 4 a 7 miembros, mientras que en cada caso el grupo metileno en la posicion 4 de grupo cicloalquilenimino de 6 o 7 miembros puede estar reemplazado por un átomo de oxígeno o azufre, por grupo sulfinilo, sulfonilo, -NH-, -NalquiloC1-3, -Nfenilo, - NalquilC1-3-carbonilo o -Nbenzoilo o, si n significa uno de los numeros 1, 2 o 3, también puede significar un átomo de hidrogeno; grupo de formula: -N(R10)-(CH2)m-C(O)o-R11, en la que: R10 significa un átomo de hidrogeno, grupo alquilo C1-3, grupo alquilC1-3-carbonilo, arilcarbonilo, fenil-alquilC1-3-carbonilo, alquilC1-3-sulfonilo, arilsulfonilo o fenil-alquilC1-3-sulfonilo; m significa uno de los numeros 1, 2, 3 o 4; o significa el numero 1 o, si m significa uno de los numeros 2, 3 o 4, o puede también significar el numero 0; y R11 significa grupo amino, alquilC1-4-amino, di-(alquilC1-4)-amino, fenilamino, N-(alquilC1-4)-fenilamino, bencilamino, N-(alquilC1-4)-bencilamino, alcoxi C1-4 o alcoxiC1-3-alcoxi-C1-3, grupo di-(alquilC1-4)-amino-alquilC1-3-amino, opcionalmente sustituido en la posicion 1 con grupo alquilo C1-3 o grupo cicloalquilenimino de 4 a 7 miembros, en donde el resto cicloalquileno puede estar condensado a un anillo de fenilo, o en cada caso el grupo metileno en la posicion 4 de un grupo cicloalquilenimino de 6 o 7 miembros puede estar reemplazados por un átomo de oxígeno o azufre, por un grupo sulfinilo, sulfonilo, -NH, -NalquiloC1-3, -Nfenilo, -NalquilC1-3- carbonilo o -Nbenzoilo; grupo cicloalquiloC4-7-amino cicloalquilC4-7-alquil-C1-3-amino o cicloalquenilC4-7-amino, en donde la posicion 1 del anillo no está implicada en el doble enlace y en donde los grupos antes mencionados puede estar, cada uno adicionalmente, sustituido en el átomo de nitrogeno del amino con un grupo cicloalquilo C5-7, alquenilo C2-4 o alquilo C1-4; grupo cicloalquilenimino de 4 a 7 miembros, en donde: el resto cicloalquileno puede estar condensado a grupo fenilo o a grupo oxazolo, imidazolo, tiazolo, piridino, pirazino o pirimidino, opcionalmente sustituido con un átomo de fluoro, cloro, bromo o yodo, con grupo nitro, alquilo C1-3, alcoxi C1-3 o amino; y/o uno o los dos átomos de hidrogeno puede estar cada uno reemplazado por grupo alquilo C1-3, cicloalquilo C5-7- o fenilo; y/o el grupo metileno en la posicion 3 de grupo cicloalquilenimi
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DE10042062A1 (de) 2000-08-26 2002-03-07 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Hertellung
DE10042059A1 (de) 2000-08-26 2002-03-07 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
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PE20060777A1 (es) 2004-12-24 2006-10-06 Boehringer Ingelheim Int Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas
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