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ME02218B - Jedinjenja piruvamida kao inhibitori peptidaza alergena grinja grupe 1 - Google Patents

Jedinjenja piruvamida kao inhibitori peptidaza alergena grinja grupe 1

Info

Publication number
ME02218B
ME02218B MEP-2015-115A MEP11515A ME02218B ME 02218 B ME02218 B ME 02218B ME P11515 A MEP11515 A ME P11515A ME 02218 B ME02218 B ME 02218B
Authority
ME
Montenegro
Prior art keywords
asthma
piperizino
compound according
4alkyl
independently
Prior art date
Application number
MEP-2015-115A
Other languages
English (en)
Inventor
Clive Robinson
Jihui Zhang
David Ronald Garrod
Trevor Robert Perrior
Gary Karl Newton
Kerry Jenkins
Rebekah Elisabeth Beevers
Meriel Ruth Mayor
Mark Richard Stewart
Original Assignee
St Georges Hospital Medical School
Univ Manchester
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
Application filed by St Georges Hospital Medical School, Univ Manchester filed Critical St Georges Hospital Medical School
Priority claimed from PCT/GB2011/000097 external-priority patent/WO2011092461A2/en
Publication of ME02218B publication Critical patent/ME02218B/me

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
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    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
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    • A01N37/44—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a nitrogen atom attached to the same carbon skeleton by a single or double bond, this nitrogen atom not being a member of a derivative or of a thio analogue of a carboxylic group, e.g. amino-carboxylic acids
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Claims (31)

1.Jedinjenje odabrano od jedinjenja naredne formule, i njegove farmaceutski prihvatljive soli, hidrati i solvati: gde:-R1 je nezavisno -H ili -R1A;-R1A je saturisan alifatični C1-6alkil, i opciono je supstituisan sa jednim ili više supstituenata -RX1;-R2 je -H;-R3 je nezavisno -H ili -R3A;-R3A je saturisan alifatični C1-3alkil;-R4 je -R4A;-R4A je -Me;-R5 je -H;-R6 je -H ili -R6A;-R6A je saturisan alifatični C1-3alkil;-R7 je -H, -R7A, ili -R7B;-R7A je saturisan alifatični C1-6alkil;-R7B je nezavisno -L7B1-R7BB ili -R7BB;-L7B1- je saturisan alifatični C1-3alkilen;-R7BB je nezavisno -R7BB1, -R7BB2, -R7BB3, ili -R7BB4;-R7BB1 je nezavisno fenil ili naftil, i opciono je supstituisan sa jednim ili više supstituenata -RX3; -R7BB2 je C5-10 heteroaril, i opciono je supstituisan sa jednim ili više supstituenata -RX3;-R7BB3 je C3-7cikloalkil, i opciono je supstituisan sa jednim ili više supstituenata -RX2, ili je opciono fuzionisan na benzenski prsten koji je opciono supstituisan sa jednim ili više supstituenata -RX3;-R7BB4 je saturisan premošćen C5-10cikloalkil, i opciono je supstituisan sa jednim ili više supstituenata -RX2;-R8 je -H;-R9 je nezavisno -H ili -R9A;-R9A je saturisan alifatični C1-4alkil;-R10 je nezavisno -R10A, -R10B, -R10C, ili -R10D;-R10A je nezavisno fenil ili naftil, i opciono je supstituisan sa jednim ili više supstituenata -RX3;-R10B je C5-10heteroaril, i opciono je supstituisan sa jednim ili više supstituenata -RX3;-R10C je saturisan C3-7cikloalkil, i opciono je supstituisan sa jednim ili više supstituenata -RX2;-R10D je nearomatični C3-10heterociklil, i opciono je supstituisan sa jednim ili više supstituenata -RX2; ili -R9 i -R10, uzeti zajedno sa atomom azota i atomom ugljenika na koje su respektivno povezan, obrazuju nearomatični C5-7heterociklični laktamski prsten, koji je opciono supstituisan sa jednim ili više supstituenata -RX2, ili koji je opciono fuzionisan za benzenski prsten koji je opciono supstituisan sa jednim ili više supstituenata -RX3;-R11 je nezavisno -H, -R11A, ili -R11B;-R11A je nezavisno -RZ1, -RZ2, -RZ3, -RZ4, -RZ5, -LZ-RZ2, -LZ-RZ3, -LZ-RZ4, ili -LZ-RZ5;-RZ1 je saturisan alifatični C1-6alkil, i opciono je supstituisan sa jednim ili više supstituenata -RX1;svaki -RZ2 je saturisan C3-7cikloalkil, i opciono je supstituisan sa jednim ili više supstituenata -RX2;svaki -RZ3 je nezavisno -RZ3A ili -RZ3B;svaki -RZ3A je nearomatični C3-7heterociklil, i opciono je supstituisan sa jednim ili više supstituenata -RX2;svaki -RZ3B je saturisan premošćen C5-10heterociklil, i opciono je supstituisan sa jednim ili više supstituenata -RX2;svaki -RZ4 je nezavisno fenil ili naftil, i opciono je supstituisan sa jednim ili više supstituenata -RX3;svaki -RZ5 je C5-10heteroaril, i opciono je supstituisan sa jednim ili više supstituenata -RX3;svaki -LZ- je saturisan alifatični C1-4alkilen;-R11B je -CRJ1RJ2-C(=O)-NRJ3RJ4;-RJ1 je nezavisno -H ili saturisan alifatični C1-4alkil;-RJ2 je nezavisno -H ili saturisan alifatični C1-4alkil;-RJ3 je nezavisno -H, saturisan alifatični C1-4alkil, fenil, ili benzil;-RJ4 je nezavisno -H, saturisan alifatični C1-4alkil, fenil, ili benzil; ili -NRJ3RJ4 je a C3-10heterociklil grupa, i opciono je supstituisan sa jednim ili više supstituenata -RX2;-R12 je nezavisno -H ili -R12A;-R12A je saturisan alifatični C1-4alkil;gde je svaki -RX1 nezavisno izabran od:-F, -Cl, -Br, -I, fenil, -CF3, -OH, -ORS, -OCF3, -NH2, -NHRS, -NRS2, pirolidino, piperidino, morfolino, piperizino, N-(C1-4alkil)-piperizino, -NHC(=O)RS, -NRSC(=O)RS, -C(=O)RS, -C(=O)OH, -C(=O)ORS, -C(=O)NH2, -C(=O)NHRS, -C(=O)NRS2, -C(=O)-pirolidino, -C(=O)-piperidino, -C(=O)-morfolino, -C(=O)-piperizino, -C(=O)-{N-(C1-4alkil)-piperizino}-, -SRS, -S(=O)RS, i -S(=O)2RS;gde je svaki -RS nezavisno saturisan alifatični C1-6alkil, fenil, ili -CH2-fenil;gde je svaki fenil opciono supstituisan sa jednom ili više grupa izabranih od: -F, -Cl, -Br, -I, -RSS, -CF3, -OH, -ORSS, ili -OCF3, gde je svaki -RSS saturisan alifatični C1-4alkil;i gde je svaki -RX2 je nezavisno izabran od:-F, -Cl, -Br, -I, -RT, fenil, -OH, -ORT, -C(=O)RT, -NH2, -NHRT, -NRT2, pirolidino, piperidino, morfolino, piperizino, N-(C1-4alkil)-piperizino, -NHC(=O)RT, i -NRTC(=O)RT;gde je svaki -RT nezavisno saturisan alifatični C1-6alkil, fenil, ili -CH2-fenil;gde je svaki fenil opciono supstituisan sa jednom ili više grupa izabranih od: -F, -Cl, -Br, -I, -RTT, -CF3, -OH, -ORTT, ili -OCF3, gde je svaki -RTT saturisan alifatični C1-4alkil;i gde je svaki -RX3 nezavisno izabran od:-F, -Cl, -Br, -I,-RV,-CH=CH2, -C=CH, ciklopropil,-CF3, -CHF2, -OCF3, -OCHF2,-CN,-NO2,-OH, -ORV,-LV-OH, -LV-ORV,-O-LV-OH, -O-LV-ORV,-NH2, -NHRV, -NRV2,pirolidino, piperidino, morfolino,piperizino, N-(C1-4alkil)-piperizino,-LV-NH2, -LV-NHRV, -LV-NRV2,-LV-pirolidino, -LV-piperidino, -LV-morfolino,-LV-piperizino, -LV-{N-(C1-4alkil)-piperizino},-LV-imidazol-2-il, -LV-{N-(C1-4alkil)-imidazol-2-il},-O-LV-NH2, -O-LV-NHRV, -O-LV-NRV2,-O-LV-pirolidino, -O-LV-piperidino, -O-LV-morfolino,-O-LV-piperizino, -O-LV-{N-(C1-4alkil)-piperizino},-O-LV-imidazol-2-il, -O-LV-{N-(C1-4alkil)-imidazol-2-il},-NHC(=O)RV, -NRVC(=O)RV,-C(=O)RV,-C(=O)OH, -C(=O)ORV,-C(=O)NH2, -C(=O)NHRV, -C(=O)NRV2,-C(=O)-pirolidino, -C(=O)-piperidino, -C(=O)-morfolino,-C(=O)-piperizino, -C(=O)-{N-(C1-4alkil)-piperizino}-,-NHC(=O)NH2, -NHC(=O)NHRV, -NHC(=O)NRV2,-NHC(=O)-pirolidino, -NHC(=O)-piperidino, -NHC(=O)-morfolino,-NHC(=O)-piperizino, -NHC(=O)-{N-(C1-4alkil)-piperizino}-,-S(=O)2RV,-S(=O)2NH2, -S(=O)2NHRV, -S(=O)2NRV2, i=O;gde je svaki -LV-je saturisan alifatični C1-4alkilen;gde je svaki -RV je nezavisno saturisan alifatični C1-6alkil, fenil, -CH2-fenil, C5-6heteroaril, or-CH2-C5-6heteroaril;gde je svaki fenil je opciono supstituisan sa jednom ili više grupa izabranih od: -F, -Cl, -Br, -I, -RVV, -CF3, -OH, -ORVV, ili -OCF3;gde je svaki C5-6heteroaril je opciono supstituisan sa jednom ili više grupa izabranih od: -F, -Cl, -Br, -I, -RVV, -CF3, -OH, -ORVV, ili -OCF3;gde je svaki -RVV je saturisan alifatični C1-4alkil;i dodatno, dve susedne grupe -RX3 mogu zajedno obrazovati -OCH2O-, -OCH2CH2O-, -CH2OCH2- ili -OCH2CH2-;i dodatno, dve susedne grupe -RX3 mogu, zajedno sa prstenovima atoma za koje su vezani, da obrazuju C5-7karbociklični prsten ili a C5-7heterociklični prsten.
2.Jedinjenje prema patentnom zahtevu 1, gde -R1 je -R1A, gde -R1A je -iPr.
3.Jedinjenje prema patentnom zahtevu 1 ili 2, gde -R3 je -H i -R6 je -H.
4.Jedinjenje prema bilo kom patentnom zahtevu od 1 do 3, gde -R7 je -R7A, i -R7A je -tBu.
5.Jedinjenje prema bilo kom patentnom zahtevu od 1 do 3, gde -R7 je -R7B; -R7B je -L7B1-R7BB; -L7B1- je -CH2-; -R7BB je -R7BB1; i -R7BB1 je fenil.
6.Jedinjenje prema bilo kom patentnom zahtevu od 1 do 5, gde -R9 je -H; -R10 je -R10A; i -R10A je fenil, i opciono je supstituisan sa jednim ili više supstituenata -RX3.
7.Jedinjenje prema bilo kom patentnom zahtevu od 1 do 5, gde -R9 je -H; -R10 je -R10B; i -R10B je piridil, i opciono je supstituisan sa jednim ili više supstituenata -RX3.
8.Jedinjenje prema bilo kom patentnom zahtevu od 1 do 5, gde -R9 je -H; -R10 je -R10B; i -R10B je nezavisno indazolil, benzimidazolil, benzotiazolil, kvinolinil, ili isokvinolinil, i opciono je supstituisan sa jednim ili više supstituenata -RX3.
9.Jedinjenje prema bilo kom patentnom zahtevu od 1 do 5, gde -R9 je -H; -R10 je -R10D; i -R10D je nezavisno:
10.Jedinjenje prema bilo kom patentnom zahtevu od 1 do 5, gde je grupa -N(R9)-C(=O)-R10 naredna grupa:
11.Jedinjenje prema bilo kom patentnom zahtevu od 1 do 10, gde: -R11 je -R11A; -R11A je -LZ-RZ4; -LZ- je -CH2- ili -CH(Me)-; i -RZ4 je nezavisno izabran od: i -R12 je -H.
12.Jedinjenje prema bilo kom patentnom zahtevu od 1 do 10, gde: -R11 je -R11B; -RJ1 je nezavisno -H, -Me, -Et, -npr., ili -iPr; -RJ2 je -H; -NRJ3RJ4 je nezavisno izabran od: 1,2,3,4-tetrahidro-isokvinolin-2-il, i 2,3-dihidro-1H-indol-1-il; i -R12 je -H.
13.Jedinjenje prema bilo kom patentnom zahtevu od 1 do 12, gde je svaki -RX1, ako je prisutan, nezavisno izabran od: -F, -Cl, -Br, -I, -OH, -ORS, -NH2, -NHRS, -NRS2, pirolidino, piperidino, morfolino, piperizino, N-(C1-4alkil)-piperizino, -NHC(=O)RS, -NRSC(=O)RS, -C(=O)NH2, -C(=O)NHRS, -C(=O)NRS2, -C(=O)-pirolidino, -C(=O)-piperidino, -C(=O)-morfolino, -C(=O)-piperizino, i -C(=O)-{N-(C1-4alkil)-piperizino}-; i svaki -RX2, ako je prisutan, nezavisno izabran od: -RT, -OH, -ORT, -C(=O)RT, -NH2, -NHRT, -NRT2, pirolidino, piperidino, morfolino, piperizino, N-(C1-4alkil)-piperizino, -NHC(=O)RT, i -NRTC(=O)RT.
14.Jedinjenje prema bilo kom patentnom zahtevu od 1 do 13, gde je svaki -RX3, ako je prisutan, nezavisno izabran od: -F, -Cl, -Br, -I, -RV, -CN, -OH, -ORV, -NH2, -NHRV, -NRV2, pirolidino, piperidino, morfolino, piperizino, N-(C1-4alkil)-piperizino, -LV-NH2, -LV-NHRV, -LV-NRV2, -LV-pirolidino, -LV-piperidino, -LV-morfolino, -LV-piperizino, -LV-{N-(C1-4alkil)-piperizino}, -C(=O)OH, -C(=O)ORV, -C(=O)NH2, -C(=O)NHRV, -C(=O)NRV2, -NHC(=O)NH2, -S(=O)2NH2, -S(=O)2NHRV, -S(=O)2NRV2, i =O.
15.Jedinjenje prema bilo kom patentnom zahtevu od 1 do 13, gde je svaki -RX3, ako je prisutan, nezavisno izabran od: -F, -Cl, -Br, -I, -RV, -OH, -ORV, -NH2, -NHRV, -NRV2, pirolidino, piperidino, morfolino, piperizino, i N-(C1-4alkil)-piperizino.
16.Jedinjenje prema patentnom zahtevu 1, izabrano od narednih jedinjenja i njegovih farmaceutski prihvatljivih soli, hidrata i solvata: PVA-001 do PVA-005, PVA-008 do PVA-013, PVA-015 do PVA-017, PVA-019 do PVA-086, PVA-089, PVA-092 do PVA-099, PVA-102 do PVA-122, PVA-124 do PVA-138, PVA-141-PVA-144, i PVA-146-PVA-216.
17.Sastav koji obuhvata jedinjenje prema bilo kom patentnom zahtevu od 1 do 16, i njegovih farmaceutski prihvatljivih nosača, rastvarača, ili ekscipijenasa.
18.Postupak pripreme sastava koji obuhvata mešanje jedinjenje prema bilo kom patentnom zahtevu od 1 do 16 i njegovih farmaceutski prihvatljivih nosača, rastvarača, ili ekscipijenasa.
19.Jedinjenje prema bilo kom patentnom zahtevu od 1 do 16 za primenu u postupku tretmana ljudskog ili životinjskog tela terapijom
20.Jedinjenje prema bilo kom patentnom zahtevu od 1 do 16 za primenu u postupku tretmana: astme, na primer, lokalne astme; alergijske astme; atopijske bronhijalne IgE posredovane astme; bronhijalne astme; spoljašnje astme; astme izazvane alergenima; alergijska astma pogoršane virusom infekcije disajnih puteva; infektivne astme; infektivne astme uzrokovane bakterijskom infekcijom; infektivne astme uzrokovane gljivičneom infekcijom; infektivne astme uzrokovane protozojskom infekcijom; ili infektivne astme uzrokovane virusnom infekcijom; bronhijalne preosetljivosti povezane sa astmom; ili bronhijalne preosetljivosti povezane sa astmom; preobilikovanje disajnih puteva povezano sa alergijskim bolestima pluća, npr. preoblikovanje disajnih puteva povezano sa astmom; astme zajedno prisutne sa hroničnom opstruktivnom bolesti pluća, na primer, astme zajedno pristune sa emfizemom; ili astme zajedno prisutne sa hroničnim bronhitisom; rinitisa, na primer, alergijskog rinitisa; višegodišnji rinitisa; upornog rinitisa; ili IgE-posredovanog rinitisa; alergijskog konjuktivitisa, na primer IgE-posredovanog konjunktivitisa; atopijskog dermatitisa; alergijskih stanja koja pokreću grinje; alergijskih stanja koje pokreće peptidaza alergen grinja Grupe 1; ili pseće atopije.
21.Jedinjenje prema patentnom zahtevu 20, gde tretman dalje obuhvata tretman sa jednim ili više dodatnih terapijskih agenasa izabranih od agenasa koji se koriste, ili će se verovatno koristiti, za tretman respiratornih bolesti.
22.Korišćenje jedinjenja prema bilo kom patentnom zahtevu od 1 do 16 u proizvodnji leka za tretman: astme, na primer, lokalne astme; alergijske astme; atopijske bronhijalne IgE posredovane astme; bronhijalne astme; spoljašnje astme; astme izazvane alergenima; alergijska astma pogoršane virusom infekcije disajnih puteva; infektivne astme; infektivne astme uzrokovane bakterijskom infekcijom; infektivne astme uzrokovane gljivičnom infekcijom; infektivne astme uzrokovane protozojskom infekcijom; ili infektivne astme uzrokovane virusnom infekcijom; bronhijalne preosetljivosti povezane sa astmom; ili bronhijalne preosetljivosti povezane sa astmom; preobilikovanje disajnih puteva povezano sa alergijskim bolestima pluća, npr. preoblikovanje disajnih puteva povezano sa astmom; astme zajedno prisutne sa hroničnom opstruktivnom bolesti pluća, na primer, astme zajedno prisutne sa emfizemom; ili astme zajedno prisutne sa hroničnim bronhitisom; rinitisa, na primer, alergijskog rinitisa; višegodišnji rinitisa; upornog rinitisa; ili IgE-posredovanog rinitisa; alergijskog konjuktivitisa, na primer IgE-posredovanog konjunktivitisa; atopijskog dermatitisa; alergijskih stanja koja pokreću grinje; alergijskih stanja koje pokreće peptidaza alergen grinja Grupe 1; ili pseće atopije.
23.Primena prema patentnom zahtevu 22, gde tretman dalje obuhvata tretman sa jednim ili više dodatnih terapijskih agenasa izabranih od agenasa koji se koriste, ili će se verovatno koristiti, za tretman respiratornih bolesti.
24.Postupak inhibiranja peptidaza alergena grinja Grupe 1, in vitro, koji obuhvata dovođenje u dodir navedenog peptidaza alergena grinja Grupa 1 sa delotvornom količinom jedinjenja prema bilo kom patentnom zahtevu od 1 do 16.
25.Postupak inhibiranja peptidaza alergena grinja Grupe 1 u ćeliji, in vitro, koji obuhvata dovođenje u dodir navedenog ćelije sa delotvornom količinom jedinjenja prema bilo kom patentnom zahtevu od 1 do 16.
26.Jedinjenje prema bilo kom patentnom zahtevu od 1 do 16, za primenu kao akaricid.
27.Sastav koji obuhvata jedinjenje prema bilo kom patentnom zahtevu od 1 do 16, za primenu kao akaricid.
28.Sastav akaricida koji obuhvata jedinjenje prema bilo kom patentnom zahtevu od 1 do 16.
29.Primena jedinjenja prema bilo kom patentnom zahtevu od 1 do 16 kao akaricid.
30.Postupak ubijanja grinja, koji obuhvata izlaganje navedenih grinja delotvornoj količini jedinjenja prema bilo kom patentnom zahtevu od 1 do 16.
31.Postupak kontrolisanja populacije grinja koji obuhvata izlaganje grinja delotvornoj količini jedinjenja prema bilo kom patentnom zahtevu od 1 do 16.
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