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AR060605A1 - Derivados de diazepano como antagonistas del receptor ccr2 - Google Patents

Derivados de diazepano como antagonistas del receptor ccr2

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Publication number
AR060605A1
AR060605A1 ARP070101679A ARP070101679A AR060605A1 AR 060605 A1 AR060605 A1 AR 060605A1 AR P070101679 A ARP070101679 A AR P070101679A AR P070101679 A ARP070101679 A AR P070101679A AR 060605 A1 AR060605 A1 AR 060605A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
heterocyclyl
heteroaryl
phenyl
Prior art date
Application number
ARP070101679A
Other languages
English (en)
Inventor
Patrizi Mattei
Olivier Roche
Johannes Aebi
Luke Green
Fabienne Ricklin
Peter Zahm
Original Assignee
Hoffmann La Roche
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Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR060605A1 publication Critical patent/AR060605A1/es

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    • C07D405/00—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
    • 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
    • C07D405/06—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 carbon chain containing only aliphatic carbon atoms
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    • 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
    • A61K31/55—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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    • A61P25/00—Drugs for disorders of the nervous system
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/14—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 three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • 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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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
    • C07D471/10—Spiro-condensed systems

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Abstract

Así como las sales farmacéuticamente aceptables de los mismos. Estos compuestos son antagonistas del receptor CCR-2, del receptor CCR-5 y/o del receptor CCR-3 y pueden utilizarse como medicamentos. Reivindicacion 1: Compuestos de la formula (1) en la que A es arilo o heteroarilo, dicho arilo y dicho heteroarilo están opcionalmente sustituidos de 1 a 3 veces por sustituyentes elegidos con independencia entre el grupo formado por halogeno, benciloxi, heteroaril-alcoxi C1-6, alquilo C1-6, alcoxi C1-6 y halo-alcoxi C1-6, o dicho arilo y dicho heteroarilo están opcionalmente sustituidos por alquilenodioxi C1-6; X es -N(R1)(R2) o -N+(R1)(R2)(R7); i) R1 y R2 son con independencia entre sí H, alquilo C1-6, alquenilo C3-6, alquinilo C3-6, hidroxialquilo C2-6, alcoxi C1-6-alquilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-6, bicicloalquilo C7-10, fenil-alquilo C1-3, heteroaril-alquilo C1-3, heterociclilo o heterociclil-alquilo C1-6, en el que el cicloalquilo de dicho cicloalquilo C3-7 y dicho cicloalquil C3-7-alquilo C1-6, el fenilo de dicho fenil-alquilo C1-3, el heteroarilo de dicho heteroaril-alquilo C1-3 y el heterociclilo de dicho heterociclilo y dicho heterociclil-alquilo C1-6 están opcionalmente sustituidos de una a tres veces por sustituyentes elegidos con independencia entre el grupo formado por Rd; o R1 y R2, junto con el átomo de nitrogeno al que están unidos, forman un heterociclilo opcionalmente sustituido de una a tres veces por sustituyentes elegidos entre el grupo formado por Rd, y uno de los átomos de carbono del anillo de dicho heterociclilo formado por R1 y R2 está opcionalmente sustituido por un grupo carbonilo; y/o uno de los átomos de carbono del anillo del heterociclilo formado por R1 y R2 puede ser un átomo de carbono de otro anillo, que sea cicloalquilo C3-7, o heterociclilo, uno o dos átomos de carbono de dicho otro anillo están opcionalmente reemplazados por un grupo carbonilo, y dicho otro anillo está opcionalmente sustituido por alquilo C1-6; R3 y R4 son con independencia entre si hidrogeno, hidroxi, alquilo C1-6, alcoxi C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-6, alcoxi C1-6-carbonilo, carboxilo, hidroxialquilo C1-6, alcoxi C1- 6-alquilo C1-6, halogeno o halo-alquilo C1-6; o R3 y R4, junto con el átomo de carbono al que están unidos, forman un cicloalquilo C3-7 o heterociclilo opcionalmente sustituido de una a tres veces por sustituyentes elegidos entre el grupo formado por alquilo C1-4 alquilo, haloalquilo C1-4 y halogeno; o bien ii) R1 es H, alquilo C1-6, alquenilo C3-6, alquinilo C3-6, hidroxi-alquilo C1-6, alcoxi C1-6-alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-6, bicicloalquilo C7-10, fenil- alquilo C1-3, heteroaril-alquilo C1-3; heterociclilo o heterociclil-alquilo C1-6, en el que el cicloalquilo de dicho cicloalquilo C3-7 y dicho cicloalquil C3-7-alquilo C1-6, el fenilo de dicho fenil-alquilo C1-3, el heteroarilo de dicho heteroaril- alquilo C1-3 y el heterociclilo de dicho heterociclilo y dicho heterociclil-alquilo C1-6 están opcionalmente sustituidos de 1 a 3 veces por sustituyentes elegidos con independencia entre el grupo formado por Rd; R3 es H, alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-6, halogeno o halo-alquilo C1-6; R2 y R4, junto con el átomo de N al que está unido R2, el átomo de C al que está unido R4 y el alquileno C1-2 entre dicho átomo de N y dicho átomo de C, si lo hubiera, forman un heterociclilo opcionalmente sustituido de 1 a 3 veces por sustituyentes elegidos entre el grupo formado por alquilo C1-6 y F; R5 y R6 con independencia entre sí son H, F, alquilo C1-6 o cicloalquilo C3-7; R7 es alquilo C1-6; R8, R9, R10, R11, R12 y R13 son con independencia entre sí H, alquilo C1-6 o cicloalquilo C3-7; Rd es hidroxi, ciano, NRaRb, halogeno, alquilo C1-6, halo-alquilo C1-6, hidroxi-alquilo C1-6, alcoxi C1-6, alcoxi C1-6- alquilo C1-6, cicloalquilo C3-7, alcoxi C1-6-carbonilo, acilo, -C(O)NRaRb, -NRa-C(O)-Rb, -NRa-C(O)-ORb, -NRa-C(O)-NRb, -NRa-SO2-Rb, -NRa-SO2-NRbRc, -OC(O)NRaRb, -OC(O)ORa, alquilsulfonilo C1-6, alquilsulfinilo C1-6, alquiltio C1-6, fenilo, fenil-alquilo C1-3, heteroarilo, heteroaril-alquilo C1-3 y heterociclilo, y el fenilo de dicho fenilo y dicho fenil-alquilo C1-3, el heteroarilo de dicho heteroarilo y dicho heteroaril-alquilo C1-3 y el heterociclilo están opcionalmente sustituidos de una a tres veces por sustituyentes elegidos con independencia entre el grupo formado por hidroxi, ciano, NRaRb, halogeno, alquilo C1-6, halo-alquilo C1-6, hidroxi-alquilo C1-6, alcoxi C1-6-carbonilo, acilo, -C(O)NRaRb, --NRa-C(O)-Rb, -NRa-C(O)-ORb, -NRa-C(O)-NRb, -NRa-SO2-Rb, -NRa-SO2-NRbRc, - OC(O)NRaRb, -OC(O)ORa, alquilsulfonilo C1-6, alquilsulfinilo C1-6, alquiltio C1-6, y uno o dos átomos de carbono del anillo del heterociclilo están opcionalmente sustituidos por un grupo carbonilo; Ra, Rb y Rc son con independencia hidrogeno o alquilo C1-6; n es un numero entero de 0 a 3; m es un numero entero de 0 a 3; m+n es un numero entero de 1 a 5; o profármacos o sales farmacéuticamente aceptables de los mismos; en los que, a menos que se indique lo contrario, el término ôariloö significa fenilo o naftilo; el término ôheterocicliloö significa restos no aromáticos, mono- o bicíclicos, de cuatro a nueve átomos en el anillo, de los cuales de 1 a 3 son heteroátomos, elegidos con independencia entre N, O y S(O)n (en el que n es un numero entero de 0 a 2), los demás átomos del anillo son C; el término ôheteroariloö significa un resto monocíclico o bicíclico de 5 a 10 átomos en el anillo, que tiene de 1 a 3 heteroátomos en el anillo, elegidos con independencia entre N, O y S, los demás átomos del anillo son C; el término ôaciloö significa R-C(O)-, en el que R es alquilo C1-6, halo-alquilo C1-6, cicloalquilo C3-7 o cicloalquil C3-7-alquilo C1-6.
ARP070101679A 2006-04-20 2007-04-19 Derivados de diazepano como antagonistas del receptor ccr2 AR060605A1 (es)

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US (1) US7632829B2 (es)
EP (1) EP2010506B1 (es)
JP (1) JP5016666B2 (es)
KR (1) KR101176697B1 (es)
CN (1) CN101472904B (es)
AR (1) AR060605A1 (es)
AT (1) ATE476424T1 (es)
AU (1) AU2007242883B2 (es)
BR (1) BRPI0710512A2 (es)
CA (1) CA2649636A1 (es)
CL (1) CL2007001090A1 (es)
DE (1) DE602007008222D1 (es)
ES (1) ES2348122T3 (es)
IL (1) IL194556A0 (es)
MX (1) MX2008013468A (es)
NO (1) NO20084332L (es)
RU (1) RU2439065C2 (es)
TW (1) TWI337181B (es)
WO (1) WO2007122103A1 (es)

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WO2009133778A1 (ja) * 2008-04-30 2009-11-05 住友化学株式会社 ｔｅｒｔ－ブチル ３－アミノピペリジン－１－カルボキシレートの製造方法およびその中間体
BRPI0915761A2 (pt) 2008-07-16 2015-11-03 Hoffmann La Roche composto de heterociclila para tratamento de doença cardiovascular
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