HRP20151378T1 - Derivati kromena korisni u liječenju bolesti posredovane međudjelovanjem trc-nck - Google Patents

Derivati kromena korisni u liječenju bolesti posredovane međudjelovanjem trc-nck Download PDF

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HRP20151378T1
HRP20151378T1 HRP20151378TT HRP20151378T HRP20151378T1 HR P20151378 T1 HRP20151378 T1 HR P20151378T1 HR P20151378T T HRP20151378T T HR P20151378TT HR P20151378 T HRP20151378 T HR P20151378T HR P20151378 T1 HRP20151378 T1 HR P20151378T1
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alkyl
substance
formula
independently represents
ring
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HRP20151378TT
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Balbino José ALARCÓN SÁNCHEZ
Ángel MESSEGUER PEYPOCH
Antonio MORREALE DE LEÓN
Aldo Jorge Borroto Revuelta
Irene Azahara Arellano Rojo
Almudena Perona Requena
Esther Carrasco Romero
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Consejo Superior De Investigaciones Científicas (Csic)
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/4025Heterocyclic 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D311/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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 three or more hetero rings

Claims (9)

1. Tvar formule I [image] ili njena sol, pri čemu svaki R1 nezavisno predstavlja vodik, C1-4 alkil, C2-4 alkenil, C2-4alkinil, hidroksil, C1-4alkoksil, C1-4alkoksiC1-4alkil, halo C1-4alkil, hidroksiC1-4alkil, cijanoC1-4alkil, halogen, -CN, NO2 ili Cy2; R2 predstavlja vodik; svaki R3 nezavisno predstavlja C1-4 alkil halo C1-4alkil ili halogen; Cy1 predstavlja monociklički heterocikl od 5 ili 6 članova, zasićen ili djelomično nezasićen koji je pričvršćen za ostatak molekule preko bilo kojeg dostupnog N atoma, pri čemu Cy1 može sadržavati 1 ili 2 heteroatoma odabrana između N, O i S, pri čemu jedan ili više C ili S atoma iz prstena može biti oksidirano tako da tvori grupe CO, SO ili SO2, i gdje je Cy1 opcionalno supstituiran s jednim ili više R4; svaki Cy2 nezavisno predstavlja aromatski prsten od 5-7 članova koji mogu biti pridruženi ostatku molekule preko bilo kojeg dostupnog C ili N atoma, gdje Cy2 može opcionalno biti udružen u prsten sa 5 ili 6 članova koji je karbociklički ili heterociklički zasićen, djelomično nezasićen ili aromatski, pri čemu Cy2 može ukupno sadržavati od 1 do 4 heteroatoma odabrana između N, O i S, pri čemu jedan ili više atoma C ili S iz prstena može biti oksidirano tako da tvori grupe CO, SO ili SO2, i gdje je Cy2 opcionalno supstituiran s jednim ili više R4; svaki R4 nezavisno predstavlja, C1-4 alkil, C2-4 alkenil, C2-4 alkinil, hidroksil, C1-4alkoksil, C1-4alkoksiC1-4alkil, halo C1-4alkil, hidroksiC1-4alkil, cijanoC1-4alkil, halogen, -CN ili NO2; n predstavlja od 0 do 4; i m predstavlja 1.
2. Tvar u skladu s patentnim zahtjevom 1 pri čemu svaki R1 nezavisno predstavlja vodik, C1-4alkoksil ili Cy2.
3. Tvar u skladu s bilo kojim od patentnih zahtjeva 1 ili 2 pri čemu Cy1 predstavlja grupu: [image]
4. Tvar u skladu s bilo kojim od patentnih zahtjeva 1 do 3 gdje svaki Cy2 nezavisno predstavlja fenil ili aromatski prsten od 5 ili 6 članova koji može biti pridružen ostatku molekule preko bilo kojeg dostupnog C ili N atomom, gdje Cy2 sadrži 1 ili 2 heteroatoma odabrana između N, O i S, gdje jedan ili više atoma C ili S iz prstena može biti oksidirano tako da tvori CO, SO ili SO2 grupe, i gdje je Cy2 opcionalno supstituiran s jednim ili više R4.
5. Tvar u skladu s bilo kojim od patentnih zahtjeva 1 do 4 gdje svaki R4 nezavisno predstavlja C1-4alkil, hidroksil, C1-4alkoksil, haloC1-4alkil, hidroksiC1-4alkil ili halogen.
6. Tvar u skladu s bilo kojim od patentnih zahtjeva 1 do 5 gdje n predstavlja 0 ili 1.
7. Farmaceutski sastav obuhvaća tvar formule I u skladu s bilo kojim od patentnih zahtjeva 1 do 6 ili njenu farmaceutski prihvatljivu sol i jedan ili više farmaceutski prihvatljivih ekscipijenasa.
8. Tvar formule I u skladu s bilo kojim od patentnih zahtjeva 1 do 6 ili njena farmaceutski prihvatljiva sol za uporabu u liječenju bolesti posredovane međudjelovanjem TRC-Nck u T-limfocitima, pri čemu je bolest odabrana između odbacivanja transplantata, reumatoidnog artritisa, psorijatičnog artritisa, psorijaze, dijabetesa tipa I, komplikacija dijabetesa, multiple skleroze, sustavnog eritemskog lupusa, atopijskog dermatitisa, alergijskih reakcija posredovanih mast stanicama, leukemija, limfoma i tromboembolijskih i alergijskih komplikacija povezanih s leukemijama i limfomima.
9. Postupak za pripremu tvari formule I u skladu s patentnim zahtjevom 1, obuhvaća: a) reagiranje tvari formule II s tvari formule III [image] gdje R1, R2, R3, Cy1, n i m imaju značenje opisano u patentnom zahtjevu 1; i/ili b) transformiranje, u jednom od nekoliko stupnjeva, tvari formule I u drugu tvar formule I.
HRP20151378TT 2010-09-28 2015-12-15 Derivati kromena korisni u liječenju bolesti posredovane međudjelovanjem trc-nck HRP20151378T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
ES201031437A ES2379242B1 (es) 2010-09-28 2010-09-28 Derivados de cromeno.
PCT/ES2011/070506 WO2012042078A1 (es) 2010-09-28 2011-07-08 Derivados de cromeno
EP11828172.4A EP2623503B1 (en) 2010-09-28 2011-07-08 Chromene derivatives useful in the treatment of a disease mediated by the tcr-nck interaction

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HRP20151378T1 true HRP20151378T1 (hr) 2016-01-15

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US (1) US9120764B2 (hr)
EP (1) EP2623503B1 (hr)
JP (1) JP5894164B2 (hr)
KR (1) KR101800919B1 (hr)
CN (1) CN103189367B (hr)
AU (1) AU2011310078B2 (hr)
BR (1) BR112013007073B1 (hr)
CA (1) CA2813144C (hr)
DK (1) DK2623503T3 (hr)
ES (1) ES2379242B1 (hr)
HK (1) HK1186727A1 (hr)
HR (1) HRP20151378T1 (hr)
HU (1) HUE025731T2 (hr)
MX (1) MX342960B (hr)
PL (1) PL2623503T3 (hr)
PT (1) PT2623503E (hr)
WO (1) WO2012042078A1 (hr)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201602982YA (en) * 2013-10-17 2016-05-30 Abbvie Deutschland Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy
ES2534336B1 (es) * 2013-10-18 2016-01-28 Artax Biopharma Inc. Derivados de cromeno como inhibidores de la interacción TCR-Nck
ES2534318B1 (es) * 2013-10-18 2016-01-28 Artax Biopharma Inc. Derivados de cromeno sustituidos por alcóxido como inhibidores de la interacción TCR-Nck
US9968604B2 (en) * 2015-04-16 2018-05-15 Chiesi Farmaceutici S.P.A. Chromene derivatives as phoshoinositide 3-kinases inhibitors
CN117304157A (zh) * 2018-02-27 2023-12-29 阿塔克斯生物制药有限公司 作为tcr-nck相互作用的抑制剂的色烯衍生物

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002008217A2 (en) * 2000-07-21 2002-01-31 Chugai Seiyaku Kabushiki Kaisha COUMARIN DERIVATIVES USEFUL AS TNFα INHIBITORS
BRPI0417543A (pt) * 2003-12-12 2007-03-27 Wyeth Corp quinolinas úteis no tratamento de doença cardiovascular
WO2008005572A2 (en) * 2006-07-06 2008-01-10 Cytovia, Inc. Substituted 4-aryl-chromene as activator of caspases and inducer of apoptosis and as antivascular agent and the use thereof
ES2331451B1 (es) 2008-06-30 2010-10-21 Consejo Superior De Investigaciones Cientificas (Csic) Inmunosupresor basado en la interrupcion de la interaccion tcr-nck.
BRPI0922135B1 (pt) * 2008-12-05 2021-07-13 Astellas Pharma Inc Composto de 2h-cromeno ou um sal do mesmo, composição farmacêutica compreendendo dito composto e uso do mesmo para prevenir ou tratar uma doença induzida por infiltração de linfócito indesejável associada com s1p1

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HUE025731T2 (en) 2016-05-30
HK1186727A1 (zh) 2014-07-04
AU2011310078A1 (en) 2013-04-11
CN103189367A (zh) 2013-07-03
RU2013117924A (ru) 2014-11-10
JP2013537899A (ja) 2013-10-07
US20140005247A1 (en) 2014-01-02
CA2813144C (en) 2018-10-30
CA2813144A1 (en) 2012-04-05
MX2013003498A (es) 2013-05-20
BR112013007073B1 (pt) 2021-11-16
PL2623503T3 (pl) 2016-04-29
BR112013007073A2 (pt) 2020-04-28
ES2379242B1 (es) 2013-03-04
AU2011310078B2 (en) 2016-12-15
ES2379242A1 (es) 2012-04-24
DK2623503T3 (en) 2016-01-11
KR101800919B1 (ko) 2017-11-23
JP5894164B2 (ja) 2016-03-23
EP2623503A4 (en) 2014-03-05
WO2012042078A1 (es) 2012-04-05
KR20130141481A (ko) 2013-12-26
EP2623503B1 (en) 2015-09-23
EP2623503A1 (en) 2013-08-07
CN103189367B (zh) 2016-06-08
PT2623503E (pt) 2016-01-26
US9120764B2 (en) 2015-09-01
MX342960B (es) 2016-10-18

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