HRP20131224T1 - Male molekule modulatori aktivnosti trp-p8 - Google Patents

Male molekule modulatori aktivnosti trp-p8 Download PDF

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HRP20131224T1
HRP20131224T1 HRP20131224TT HRP20131224T HRP20131224T1 HR P20131224 T1 HRP20131224 T1 HR P20131224T1 HR P20131224T T HRP20131224T T HR P20131224TT HR P20131224 T HRP20131224 T HR P20131224T HR P20131224 T1 HRP20131224 T1 HR P20131224T1
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Croatia
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ethyl
dihydro
amino
benzoimidazol
oxo
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HRP20131224TT
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Ofir Moreno
Sateesh Natarajan
David F. Duncan
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Dendreon Corporation
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    • C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
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    • C07C237/10—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
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    • C07C237/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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    • C07C237/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having carbon atoms of carboxamide groups, amino groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
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    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
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Claims (18)

1. Spoj formule I-E: [image] gdje su A, B, C i D nezavisno izabrani od CR1 i N; gdje je najmanje jedan od A, B, C i D jednak CR1; gdje je R1 izabran od H, alkil, heteroalkil, aril, arilalkil, halogen grupe; i gdje kada su dva susjedna od A, B, C i D jednaka CR1, dva R1 mogu se spojiti tako da formiraju jednu aril, cikloalkil ili heterocikloalkil grupu; R2 je izabran od alkil, heteroalkil i arilalkil grupe; R3 je izabran od H, alkil, heteroalkil i arilalkil grupe; i R2 i R3 uzeti zajedno sa dušikovom grupom formiraju alifatični amin.
2. Spoj prema patentnom zahtjevu 1 naznačen time što je R1 jednako -ORi, -SRii, -S (O) Riii, -S (O)2Riv, -C (O) NRvRvi, CF3, halogen ili metoksi, pri čemu su Ri, Rii, Riii i Riv nezavisno izabrani iz grupe koju čine metil, hidroksimetil, etil, hidroksietil, propil, hidroksipropil, butil, hidroksibutil, acetonitril, fenil, fenilmetoksi, feniletoksi, fenilpropoksi, fenilbutoksi i benzil, pri čemu su Rv i Rvi nezavisno izabrani iz grupe koju čine H, metil, hidroksimetil, etil, hidroksietil, propil, hidroksipropil, butil, hidroksibutil, dietilaminoetil, fenil, piridinil, metoksietil, hidroksietoksietil, benzil, metilfenil, feniletil, hidroksihidroksimetilfeniletil, karbamoilmetil i hidroksimetil hidroksietil, ili Rv i Rvi zajedno formiraju morfolin, piperazin, piperazin etil ester.
3. Spoj prema patentnom zahtjevu 1, naznačen time što je navedeni spoj 3- (2- aminoetil)- 1- (2- izopropil- 5- metil- cikloheksankarbonil)-5- metoksi- 1, 3- dihidro- benzoimidazol- 2- on.
4. Spoj prema patentnom zahtjevu 1 naznačen time što je R1 jednako H.
5. Spoj prema patentnom zahtjevu 1 naznačen time što je R1 jednako metoksi.
6. Spoj prema patentnom zahtjevu 1 naznačen time što je R2 izabran od metilena, etilena, propilena ili butilena.
7. Spoj prema patentnom zahtjevu 1 naznačen time što je R3 jednako H.
8. Spoj prema patentnom zahtjevu 1 naznačen time što je grupa: [image] izabrana iz grupe koju čine 3- (2- amino- etil)- 5- metoksi- 1, 3- dihidro- benzoimidazol- 2- on, 3-(2- amino- etil)- 5- (3- hidroksi- propoksi)- 1, 3- dihidro- benzoimidazol- 2- on, 3- (2- amino- etil)- 5- etoksi- 1,3- dihidro- benzoimidazol- 2- on, 3- (2- amino- etil)- 5- metansulfonil- 1, 3- dihidro- benzoimidazol- 2- on, 3- (2- amino- etil)- 5- (2- hidroksi- etoksi)- 1, 3- dihidro- benzoimidazol- 2- on, amid 3- (2- amino- etil)- 2- okso- 2,3- dihidro- 1H- benzoimidazol- 5- karboksilne kiseline, 3- (2- amino- etil)- 5- metilsulfanil- 1, 3- dihidrobenzoimidazol-2- on, 3- (2- amino- etil)- 5- metansulfinil- 1, 3- dihidro- benzoimidazol- 2- on, (2- dietilamino- etil)- amid 3- (2- aminoetil)-2- okso- 2, 3- dihidro- 1H- benzoimidazol- 5- karboksilne kiseline, 3- (2- aminopropil)-2, 3- dihidro- benzoimidazol- 2- on, [3- (2- amino- etil)- 2- okso- 2, 3- dihidro- 1H- benzoimidazol- 5-iloksi]- acetonitril, etilamid 3- (2- amino- etil)- 2- okso- 2, 3- dihidro- 1H- benzoimidazol- 5- karboksilne kiseline, piridin-3-ilamid 3- (2- amino- etil)- 2- okso- 2, 3- dihidro- 1H- benzoimidazol- 5- karboksilne kiseline, (2-metoksi-etil)-amid 3- (2- aminoetil)-2- okso- 2, 3- dihidro- 1H- benzoimidazol- 5- karboksilne kiseline, 1- (2- amino- etil)-1, 3- dihidro- benzoimidazol- 2- on, 1- (2- amino- etil)- 1, 3- dihidro- nafto [2, 3- d] imidazol- 2- on, (2-hidroksi-etil)-amid 3- (2-amino- etil)- 2- okso- 2, 3- dihidro- 1H- benzoimidazol- 5- karboksilne kiseline, 3- (2- aminoetil)-5- propoksi- 1, 3- dihidro- benzoimidazol- 2- on, 3- (2- amino- etil)- 1, 3- dihidro- imidazo [4, 5- c] piridin-2- on, (2-dietilamino-etil)-amid 3- (2- amino- etil)- 2- okso- 2, 3- dihidro- 1H- benzoimidazol- 4- karboksilne kiseline, piridin-4-ilamid 3- (2- amino- etil)- 2- okso- 2, 3- dihidro- 1H- benzoimidazol- 5- karboksilne kiseline, 3- (2-amino- etil)- 1, 3- dihidro- imidazo [4, 5- b] piridin- 2- on, 1- (3- amino- propil)- 1, 3- dihidro- benzoimidazol-2- on, fenilamid 3- (2- amino- etil)- 2- okso- 2, 3- dihidro- 1H- benzoimidazol- 5- karboksilne kiseline, [2- (2- hidroksi- etoksi)- etil]- amid 3- (2- aminoetil)-2- okso- 2, 3- dihidro- 1H- benzoimidazol- 5- karboksilne kiseline, 1- (2-amino- etil)- 5- trifluorometil- 1, 3- dihidro- benzoimidazol- 2- on, 1- (2- amino- etil)- 1, 3- dihidro- imidazo[4, 5- c] piridin- 2- on, benzilamid 3- (2- amino- etil)- 2- okso- 2, 3- dihidro- 1H- benzoimidazol- 5- karboksilne kiseline, 3- (2- amino- etil)- 5- (morfolin- 4- karbonil)- 1, 3- dihidro- benzoimidazol- 2- on, 3- (2- amino- etil)- 5- (2-okso- 2- fenil- etoksi)- 1, 3- dihidro- benzoimidazol- 2- on, 3- (2- metilamino- etil)- 1, 3- dihidro- benzoimidazol-2- on, 3- (2- amino- etil)- 5- butoksi- 1, 3- dihidro- benzoimidazol- 2- on, metil-fenil-amid 3- (2- amino- etil)- 2- okso- 2, 3-dihidro- 1H- benzoimidazol- 5- karboksilne kiseline, etil ester 4- [3- (2- amino- etil)- 2- okso- 2, 3- dihidro-1H- benzoimidazol- 5- karbonil]- piperazin- 1- karboksilne kiseline, dietilamid 3- (2- amino- etil)- 2- okso- 2, 3-dihidro- 1H- benzoimidazol- 5- karboksilne kiseline, fenetil-amid 3- (2- amino- etil)- 2- okso- 2, 3- dihidro- 1H- benzoimidazol-5- karboksilne kiseline, (2- hidroksi- 1- hidroksimetil- 2- fenil- etil)- amid 3- (2- amino- etil)- 2- okso- 2, 3- dihidro- 1H- benzoimidazol-5- karboksilne kiseline, karbamoilmetil-amid 3- (2- amino- etil)- 2- okso- 2, 3- dihidro-1H- benzoimidazol- 5- karboksilne kiseline, (2- hidroksi- 1- hidroksimetil- etil)- amid 3- (2- amino- etil)- 2- okso- 2, 3- dihidro- 1H-benzoimidazol-5- karboksilne kiseline, N- {2- [2- okso- 2, 3- dihidrobenzoimidazol-1- il]- etil}- guanidin, 3- (2- amino- etil)- 5- benziloksi- 1, 3- dihidro- benzoimidazol- 2- on i 1- (4- amino- butil)- 1, 3- dihidro- benzoimidazol- 2- on.
9. Spoj prema patentnom zahtjevu 1 naznačen time što je navedeni spoj 1- (2- aminoetil)- 3- (2- izopropil- 5- metil- cikloheksankarbonil)-1, 3- dihidro- benzoimidazol- 2- on.
10. Spoj prema bilo kojem od patentnih zahtjeva 1 do 9 u izoliranom i pročišćenom obliku.
11. Spoj prema bilo kojem od patentnih zahtjeva 1 do 10 ili njegova farmaceutski prihvatljiva sol za uporabu u smanjenju stanične vijabilnosti i/ili inhibiciji staničnog rasta, indukciji apoptoze i/ili nekroze u stanici koja eksprimira Trp-p8, modulaciji receptorne funkcije Trp-p8 ili medicinskoj dijagnozi ili terapiji.
12. Spoj za uporabu prema patentnom zahtjevu 11, naznačen time što je medicinska terapija izabrana iz grupe koju čine liječenje bolesti ili stanja kod sisavaca kod kojih je indiciran Trp-p8 receptor i poželjna je modulacija receptorne funkcije, liječenje bolesti povezane sa ekspresijom Trp-p8 i liječenje kancera.
13. Spoj za uporabu prema patentnom zahtjevu 12, naznačen time što je navedeni sisavac čovjek.
14. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 11 do 13, naznačen time što je medicinska terapija - liječenje kancera.
15. Spoj za uporabu prema patentnom zahtjevu 14, naznačen time što je kancer – kancer prostate, pluća, dojke i debelog crijeva.
16. Farmaceutska kompozicija koja sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 10 ili njegove kombinacije, ili njegovu farmaceutski prihvatljivu sol, i farmaceutski prihvatljiv inertni punitelj.
17. Farmaceutska kompozicija prema patentnom zahtjevu 16 naznačena time što dalje sadrži farmaceutski prihvatljiv nosač ili sredstvo.
18. Postupak za identifikaciju agonista Trp-p8, naznačen time što navedeni postupak sadrži korak dovođenja u kontakt stanice koja eksprimira Trp-p8 i stanice koja ne eksprimira Trp-p8 sa spojem prema bilo kojem od patentnih zahtjeva 1 do 10 in vitro tokom vremena i u količini koji su dovoljni da se smanji vijabilnost navedene stanice koja eksprimira Trp-p8, ali ne i navedene stanice koja ne eksprimira Trp-p8.
HRP20131224TT 2006-02-15 2013-12-23 Male molekule modulatori aktivnosti trp-p8 HRP20131224T1 (hr)

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