HRP20120377T1 - Alkiltiopirimidini kao antagonisti crth2 - Google Patents
Alkiltiopirimidini kao antagonisti crth2 Download PDFInfo
- Publication number
- HRP20120377T1 HRP20120377T1 HRP20120377AT HRP20120377T HRP20120377T1 HR P20120377 T1 HRP20120377 T1 HR P20120377T1 HR P20120377A T HRP20120377A T HR P20120377AT HR P20120377 T HRP20120377 T HR P20120377T HR P20120377 T1 HRP20120377 T1 HR P20120377T1
- Authority
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- Croatia
- Prior art keywords
- alkyl
- trihalogen
- mono
- substituted
- optionally substituted
- Prior art date
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- -1 Alkylthio pyrimidines Chemical class 0.000 title claims abstract 24
- 239000005557 antagonist Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims abstract 72
- 125000003118 aryl group Chemical group 0.000 claims abstract 30
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 29
- 239000001257 hydrogen Substances 0.000 claims abstract 29
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 26
- 125000004750 (C1-C6) alkylaminosulfonyl group Chemical group 0.000 claims abstract 24
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 24
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims abstract 19
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 18
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims abstract 17
- 229910052736 halogen Inorganic materials 0.000 claims abstract 16
- 150000002367 halogens Chemical class 0.000 claims abstract 16
- 150000001875 compounds Chemical class 0.000 claims abstract 15
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims abstract 14
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims abstract 12
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims abstract 12
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract 12
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims abstract 12
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims abstract 12
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 12
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims abstract 12
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 11
- 150000003839 salts Chemical class 0.000 claims abstract 11
- 239000012453 solvate Substances 0.000 claims abstract 11
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims abstract 9
- 125000003545 alkoxy group Chemical group 0.000 claims abstract 8
- 125000004399 C1-C4 alkenyl group Chemical group 0.000 claims abstract 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims abstract 6
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims abstract 6
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 claims abstract 6
- 125000001424 substituent group Chemical group 0.000 claims abstract 6
- 238000006467 substitution reaction Methods 0.000 claims abstract 6
- 150000002825 nitriles Chemical class 0.000 claims abstract 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims abstract 2
- 201000010099 disease Diseases 0.000 claims 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 13
- 208000024891 symptom Diseases 0.000 claims 10
- 208000006673 asthma Diseases 0.000 claims 6
- 208000016557 Acute basophilic leukemia Diseases 0.000 claims 3
- 208000032671 Allergic granulomatous angiitis Diseases 0.000 claims 3
- 208000006344 Churg-Strauss Syndrome Diseases 0.000 claims 3
- 206010009900 Colitis ulcerative Diseases 0.000 claims 3
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims 3
- 208000011231 Crohn disease Diseases 0.000 claims 3
- 201000004624 Dermatitis Diseases 0.000 claims 3
- 206010012438 Dermatitis atopic Diseases 0.000 claims 3
- 208000018428 Eosinophilic granulomatosis with polyangiitis Diseases 0.000 claims 3
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 3
- 208000019693 Lung disease Diseases 0.000 claims 3
- 201000004681 Psoriasis Diseases 0.000 claims 3
- 206010039085 Rhinitis allergic Diseases 0.000 claims 3
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 3
- 206010052568 Urticaria chronic Diseases 0.000 claims 3
- 208000002205 allergic conjunctivitis Diseases 0.000 claims 3
- 201000010105 allergic rhinitis Diseases 0.000 claims 3
- 206010003246 arthritis Diseases 0.000 claims 3
- 208000024998 atopic conjunctivitis Diseases 0.000 claims 3
- 201000008937 atopic dermatitis Diseases 0.000 claims 3
- 208000010668 atopic eczema Diseases 0.000 claims 3
- 230000001684 chronic effect Effects 0.000 claims 3
- 208000024376 chronic urticaria Diseases 0.000 claims 3
- 206010024378 leukocytosis Diseases 0.000 claims 3
- 230000000414 obstructive effect Effects 0.000 claims 3
- 201000009890 sinusitis Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 150000002431 hydrogen Chemical group 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- 230000037081 physical activity Effects 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 125000004434 sulfur atom Chemical group 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 238000011282 treatment Methods 0.000 claims 2
- 206010003557 Asthma exercise induced Diseases 0.000 claims 1
- 208000004657 Exercise-Induced Asthma Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 210000003651 basophil Anatomy 0.000 claims 1
- 125000005841 biaryl group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 210000003979 eosinophil Anatomy 0.000 claims 1
- 208000024695 exercise-induced bronchoconstriction Diseases 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 238000007911 parenteral administration Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
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- 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
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- Emergency Medicine (AREA)
Abstract
Spoj, naznačen time što ima formulu I:ili njegova farmaceutski prihvatljiva sol, solvat, hidrat, stereoizomer ili tautomer, gdjeW je jednostruka veza, -(CH2)m-, -O-, -S(O)n-, -NR7-, -C(O)-, -C(O)O-, -C(O)NR7-, -NR7C(O)NR7- ili -NR7C(O)O-;R1 je -CO2R9-C(O)NR8aR8b, nitril ili tetrazolil; R2 je (a) vodik; (b) halogen; (c) (C1-C6)alkil; (d) (C1-C6)alkil, supstituiran s arilom, hidroksi, karboksi, alkoksi, karbamoilom, (C1-C6)alkilkarbamoilom, di((C1-C6)alkil)karbamoilom, (C3-C7)cikloalkilkarbamoilom ili (C3-C7)heterociklilkarbamoilom; (e) (C1-C6)alkil, supstituiran s mono-, di- ili trihalogenom; (f) (C3-C7)cikloalkil; (g) -NR8aR8b; (h) -SR3; ili (i) (C1-C6)alkoksi, izborno supstituiran s mono-, di- ili trihalogenom; svaki R3 je neovisno (a) vodik; (b) (C1-C6)alkil, izborno supstituiran s mono-, di- ili trihalogenom; (c) (C3-C7)cikloalkil; ili (d) -C(O)R9;svakog od R4a i R4b se neovisno bira između vodika ili (C1-C6)alkila; svaki R5 je neovisno (a) vodik; (b) halogen; (c) cijano; (d) nitro; (e) hidroksi; (f) fenil; (g) feniloksi; (h) benzil; (i) benziloksi; (j) gvanidino; (k) heterociklil; (l) -NR8aR8b; (m) sulfamoil; (n) (C1-C6)alkilsulfonil; (o) (C1-C6)alkilaminosulfonil; (p) di(C1-C6)alkilaminosulfonil; (q) -C(O)R9; (r) -C(O)OR9; (s) -C(O)NR8aR8b; (t) -OC(O)NR8aR8b; (u) -NR7C(O)OR9; (v) -NR7C(O)R9; (w) (C2-C6)alkenil; (x) (C1-C6)alkil, izborno supstituiran s mono-, di- ili trihalogenom; (y) (C1-C6)alkoksi, izborno supstituiran s mono-, di- ili trihalogenom; ili (z) (C1-C6)alkiltio, izborno supstituiran s mono-, di- ili trihalogenom; R6 je (a) vodik; (b) (C1-C6)alkil; (c) (C2-C6)alkenil; (d) (C2-C6)alkinil; (e) (C3-C7)cikloalkil; (f) (C1-C6)alkil supstituiran byaril ili heteroaril; (g) (C2-C4)alkenil, supstituiran s arilom ili heteroarilom; (h) (C1-C6)alkil, supstituiran s mono-, di- ili trihalogenom; (i) (C1-C6)alkil, supstituiran s -C(O)R6a; (j) (C1-C6)alkoksi, supstituiran s mono-, di- ili trihalogenom; (k) (C1-C6)alkiltio, supstituiran s mono-, di- ili trihalogenom; (l) aril; ili (m) heteroaril, gdje su navedeni aril i heteroaril na položaju gdje je moguća supstitucija izborno supstituirani s jednim ili više supstituenata koje se bira iz skupine koju čine (a) halogen; (b) cijano; (c) nitro; (d) hidroksi; (e)gvanidino;(f) heterociklil; (g) fenil; (h) feniloksi; (i) benzil; (j) benziloksi; (k) -NR8aR8b; (l) -C(O)R9; (m) -C(O)NR8aR8b; (n) -OC(O)NR8aR8b; (o) -C(O)OR9; (p) -NR7C(O)OR9; (q) -NR7C(O)R9; (r) sulfamoil; (s) (C1-C6)alkilsulfonil; (t) (C1-C6)alkilaminosulfonil; (u) di(C1-C6)alkilaminosulfonil; (v) (C1-C6)alkil, izborno supstituiran s mono-, di- ili trihalogenom; (w) (C1-C6)alkoksi, izborno supstituiran s mono-, di- ili trihalogenom; i (x) (C1-C6)alkiltio, izborno supstituiran s mono-, di- ili trihalogenom; R6a je (a) vodik; (b) (C1-C6)alkil; (c) (C2-C6)alkenil; (d) (C2-C6)alkinil; (e) (C3-C7)cikloalkil; (f) (C1-C6)alkil, supstituiran s arilom ili heteroarilom; (g) (C2-C4)alkenil, supstituiran s arilom ili heteroarilom; (h) (C1-C6)alkil, su
Claims (12)
1. Spoj, naznačen time što ima formulu I:
[image]
ili njegova farmaceutski prihvatljiva sol, solvat, hidrat, stereoizomer ili tautomer, gdje
W je jednostruka veza, -(CH2)m-, -O-, -S(O)n-, -NR7-, -C(O)-, -C(O)O-, -C(O)NR7-, -NR7C(O)NR7- ili -NR7C(O)O-;
R1 je -CO2R9-C(O)NR8aR8b, nitril ili tetrazolil;
R2 je (a) vodik; (b) halogen; (c) (C1-C6)alkil; (d) (C1-C6)alkil, supstituiran s arilom, hidroksi, karboksi, alkoksi, karbamoilom, (C1-C6)alkilkarbamoilom, di((C1-C6)alkil)karbamoilom, (C3-C7)cikloalkilkarbamoilom ili (C3-C7)heterociklilkarbamoilom; (e) (C1-C6)alkil, supstituiran s mono-, di- ili trihalogenom; (f) (C3-C7)cikloalkil; (g) -NR8aR8b; (h) -SR3; ili (i) (C1-C6)alkoksi, izborno supstituiran s mono-, di- ili trihalogenom;
svaki R3 je neovisno (a) vodik; (b) (C1-C6)alkil, izborno supstituiran s mono-, di- ili trihalogenom; (c) (C3-C7)cikloalkil; ili (d) -C(O)R9;
svakog od R4a i R4b se neovisno bira između vodika ili (C1-C6)alkila;
svaki R5 je neovisno (a) vodik; (b) halogen; (c) cijano; (d) nitro; (e) hidroksi; (f) fenil; (g) feniloksi; (h) benzil; (i) benziloksi; (j) gvanidino; (k) heterociklil; (l) -NR8aR8b; (m) sulfamoil; (n) (C1-C6)alkilsulfonil; (o) (C1-C6)alkilaminosulfonil; (p) di(C1-C6)alkilaminosulfonil; (q) -C(O)R9; (r) -C(O)OR9; (s) -C(O)NR8aR8b; (t) -OC(O)NR8aR8b; (u) -NR7C(O)OR9; (v) -NR7C(O)R9; (w) (C2-C6)alkenil; (x) (C1-C6)alkil, izborno supstituiran s mono-, di- ili trihalogenom; (y) (C1-C6)alkoksi, izborno supstituiran s mono-, di- ili trihalogenom; ili (z) (C1-C6)alkiltio, izborno supstituiran s mono-, di- ili trihalogenom;
R6 je (a) vodik; (b) (C1-C6)alkil; (c) (C2-C6)alkenil; (d) (C2-C6)alkinil; (e) (C3-C7)cikloalkil; (f) (C1-C6)alkil supstituiran byaril ili heteroaril; (g) (C2-C4)alkenil, supstituiran s arilom ili heteroarilom; (h) (C1-C6)alkil, supstituiran s mono-, di- ili trihalogenom; (i) (C1-C6)alkil, supstituiran s -C(O)R6a; (j) (C1-C6)alkoksi, supstituiran s mono-, di- ili trihalogenom; (k) (C1-C6)alkiltio, supstituiran s mono-, di- ili trihalogenom; (l) aril; ili (m) heteroaril, gdje su navedeni aril i heteroaril na položaju gdje je moguća supstitucija izborno supstituirani s jednim ili više supstituenata koje se bira iz skupine koju čine (a) halogen; (b) cijano; (c) nitro; (d) hidroksi; (e)gvanidino;(f) heterociklil; (g) fenil; (h) feniloksi; (i) benzil; (j) benziloksi; (k) -NR8aR8b; (l) -C(O)R9; (m) -C(O)NR8aR8b; (n) -OC(O)NR8aR8b; (o) -C(O)OR9; (p) -NR7C(O)OR9; (q) -NR7C(O)R9; (r) sulfamoil; (s) (C1-C6)alkilsulfonil; (t) (C1-C6)alkilaminosulfonil; (u) di(C1-C6)alkilaminosulfonil; (v) (C1-C6)alkil, izborno supstituiran s mono-, di- ili trihalogenom; (w) (C1-C6)alkoksi, izborno supstituiran s mono-, di- ili trihalogenom; i (x) (C1-C6)alkiltio, izborno supstituiran s mono-, di- ili trihalogenom;
R6a je (a) vodik; (b) (C1-C6)alkil; (c) (C2-C6)alkenil; (d) (C2-C6)alkinil; (e) (C3-C7)cikloalkil; (f) (C1-C6)alkil, supstituiran s arilom ili heteroarilom; (g) (C2-C4)alkenil, supstituiran s arilom ili heteroarilom; (h) (C1-C6)alkil, supstituiran s mono-, di- ili trihalogenom; (i) (C1-C6)alkoksi, supstituiran s mono-, di- ili trihalogenom; (j) (C1-C6)alkiltio, supstituiran s mono-, di- ili trihalogenom; (k) aril; ili (l) heteroaril, gdje su navedeni aril i heteroaril na položaju gdje je moguća supstitucija izborno supstituirani s jednim ili više supstituenata koje se bira iz skupine koju čine (a) halogen; (b) cijano; (c) nitro; (d) hidroksi; (e) gvanidino; (f) heterociklil; (g) fenil; (h) feniloksi; (i) benzil; (j) benziloksi; (k) -NR8aR8b; (l) -C(O)R9; (m) -C(O)NR8aR8b; (n) -OC(O)NR8aR8b; (o) -C(O)OR9; (p) -NR7C(O)OR9; (q) -NR7C(O)R9; (r) sulfamoil; (s) (C1-C6)alkilsulfonil; (t) (C1-C6)alkilaminosulfonil; (u) di (C1-C6)alkilaminosulfonil; (v) (C1-C6)alkil, izborno supstituiran s mono-, di-, ili trihalogen; (w) (C1-C6)alkoksi, izborno supstituiran s mono-, di- ili trihalogenom; i (x) (C1-C6)alkiltio, izborno supstituiran s mono-, di- ili trihalogenom;
R7 je (a) vodik; (b) (C1-C6)alkil; (c) fenil; (d) (C1-C6)alkil, supstituiran s arilom, hidroksi, karboksi, alkoksi, karbamoilom, (C1-C6)alkilkarbamoilom, di((C1-C6)alkil)karbamoilom, (C3-C7)cikloalkilkarbamoilom ili (C3-C7)heterociklilkarbamoilom; (e) (C1-C6)alkil, supstituiran s mono-, di- ili trihalogenom; ili (f) (C3-C7)cikloalkil;
R8a i R8b se u svakom slučaju neovisno bira između (i) ili (ii), kao što slijedi:
(i) svakog od R8a i R8b se neovisno bira između (a) vodika; (b) (C1-C6)alkila; (c) fenila; (d) (C1-C6)alkila, supstituiranog s arilom, hidroksi, karboksi, alkoksi, karbamoilom, (C1-C6)alkilkarbamoilom, di((C1-C6)alkil)karbamoilom, (C3-C7)cikloalkilkarbamoilom ili (C3-C7)heterociklilkarbamoilom; (e) (C1-C6)alkila, supstituiranog s mono-, di- ili trihalogenom; ili (f) (C3-C7)cikloalkila; ili
(ii) svaki R8a i R8b, zajedno s N na kojeg su vezani, neovisno mogu tvoriti 3- do 8-eročlani zasićeni ili nezasićeni prsten, koji izborno sadrži jedan ili više O ili S atoma, ili jedan ili više dodatnih N atoma, u prstenu;
svaki R9 je neovisno (a) vodik; (b) (C1-C6)alkil; (c) fenil; ili (d) (C1-C6)alkil, supstituiran s arilom, alkoksi ili mono-, di- ili trihalogenom;
k je 0, 1 ili 2;
m je 1, 2, 3 ili 4; i
n je 0, 1 ili 2.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što
R1 je -CO2H; i/ili
R2 je -SR3; i/ili
svaki R3 je neovisno (C1-C6)alkil; i/ili
svaki od R4a i R4b je neovisno vodik, metil ili etil.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima formulu II:
[image]
ili njegova farmaceutski prihvatljiva sol, solvat, hidrat, stereoizomer ili tautomer, gdje
W je jednostruka veza, -(CH2)m-, -O-, -S(O)n-, -NR7-, -C(O)-, -C(O)O-, -C(O)NR7-, -NR7C(O)NR7- ili -NR7C(O)O-;
svaki R3 je neovisno (C1-C6)alkil;
svakog od R4a i R4b se neovisno bira između vodika, metila ili etila;
svaki R5 je neovisno (a) vodik; (b) halogen; (c) cijano; (d) nitro; (e) hidroksi; (f) fenil; (g) feniloksi; (h) benzil; (i) benziloksi; (j) gvanidino; (k) heterociklil; (l) -NR8aR8b; (m) sulfamoil; (n) (C1-C6)alkilsulfonil; (o) (C1-C6)alkilaminosulfonil; (p) di(C1-C6)alkilaminosulfonil; (q) -C(O)R9; (r) -C(O)OR9; (s) -C(O)NR8aR8b; (t) -OC(O)NR8aR8b; (u) -NR7C (O)OR9; (v) -NR7C(O)R9; (w) (C2-C6)alkenil; (x) (C1-C6)alkil, izborno supstituiran s mono-, di- ili trihalogenom; (y) (C1-C6)alkoksi, izborno supstituiran s mono-, di- ili trihalogenom; ili (z) (C1-C6)alkiltio, izborno supstituiran s mono-, di- ili trihalogenom;
R6 je (a) vodik; (b) (C1-C6)alkil; (c) (C2-C6)alkenil; (d) (C2-C6)alkinil; (e) (C3-C7)cikloalkil; (f) (C1-C6)alkil, supstituiran s arilom ili heteroarilom; (g) (C2-C4)alkenil, supstituiran s arilom ili heteroarilom; (h) (C1-C6)alkil, supstituiran s mono-, di- ili trihalogenom; (i) (C1-C6)alkil, supstituiran s -C(O)R6a; (j) (C1-C6)alkoksi, supstituiran s mono-, di- ili trihalogenom; (k) (C1-C6)alkiltio, supstituiran s mono-, di- ili trihalogenom; (l) aril; ili (m) heteroaril, gdje su navedeni aril i heteroaril na položaju gdje je moguća supstitucija izborno supstituirani s jednim ili više supstituenata koje se bira iz skupine koju čine (a) halogen; (b) cijano; (c) nitro; (d) hidroksi; (e) gvanidino; (f) heterociklil; (g) fenil; (h) feniloksi; (i) benzil; (j) benziloksi; (k) -NR8aR8b; (l) -C(O)R9; (m) -C(O)NR8aR8b; (n) -OC(0)NR8aR8b; (o) -C(O)OR9; (p) -NR7C(O)OR9; (q) -NR7C(O)R9; (r) sulfamoil; (s) (C1-C6)alkilsulfonil; (t) (C1-C6)alkilaminosulfonil; (u) di(C1-C6)alkilaminosulfonil; (v) (C1-C6)alkil, izborno supstituiran s mono-, di- ili trihalogenom; (w) (C1-C6)alkoksi, izborno supstituiran s mono-, di- ili trihalogenom; i (x) (C1-C6)alkiltio, izborno supstituiran s mono-, di- ili trihalogenom;
R6a je (a) vodik; (b) (C1-C6)alkil; (c) (C2-C6)alkenil; (d) (C2-C6)alkinil; (e) (C3-C7)cikloalkil; (f) (C1-C6)alkil, supstituiran s arilom ili heteroarilom; (g) (C2-C4)alkenil, supstituiran s arilom ili heteroarilom; (h) (C1-C6)alkil, supstituiran s mono-, di- ili trihalogenom; (i) (C1-C6)alkoksi, supstituiran s mono-, di- ili trihalogenom; (j) (C1-C6)alkiltio, supstituiran s mono-, di- ili trihalogenom; (k) aril; ili (l) heteroaril, gdje su navedeni aril i heteroaril na položaju gdje je moguća supstitucija izborno supstituirani s jednim ili više supstituenata koje se bira iz skupine koju čine (a) halogen; (b) cijano; (c) nitro; (d) hidroksi; (e) gvanidino; (f) heterociklil; (g) fenil; (h) feniloksi; (i) benzil; (j) benziloksi; (k) -NR8aR8b; (l) -C(O)R9; (m) -C(O)NR8aR8b; (n) -OC(O)NR8aR8b; (o) -C(O)OR9; (p) -NR7C(O)OR9; (q) -NR7C(O)R9; (r) sulfamoil; (s) (C1-C6)alkilsulfonil; (t) (C1-C6)alkilaminosulfonil; (u) di (C1-C6)alkilaminosulfonil; (v) (C1-C6)alkil, izborno supstituiran s mono-, di- ili trihalogenom; (w) (C1-C6)alkoksi, izborno supstituiran s mono-, di- ili trihalogenom; i (x) (C1-C6)alkiltio, izborno supstituiran s mono-, di- ili trihalogenom;
R7 je (a) vodik; (b) (C1-C6)alkil; (c) fenil; (d) (C1-C6)alkil, supstituiran s arilom, hidroksi, karboksi, alkoksi, karbamoilom, (C1-C6)alkilkarbamoilom, di((C1-C6)alkil)karbamoilom, (C3-C7)cikloalkilkarbamoilom ili (C3-C7)heterociklilkarbamoilom; (e) (C1-C6)alkil, supstituiran s mono-, di- ili trihalogenom; ili (f) (C3-C7)cikloalkil;
R8a i R8b se u svakom slučaju neovisno bira između (i) ili (ii), kao što slijedi:
(i) svakog od R8a i R8b se neovisno bira između (a) vodika; (b) (C1-C6)alkila; (c) fenila; (d) (C1-C6)alkila, supstituiranog s arilom, hidroksi, karboksi, alkoksi, karbamoilom, (C1-C6)alkilkarbamoilom, di((C1-C6)alkil)karbamoilom, (C3-C7)cikloalkilkarbamoilom ili (C3-C7)heterociklilkarbamoilom; (e) (C1-C6)alkila, supstituiranog s mono-, di- ili trihalogenom; ili (f) (C3-C7)cikloalkila; ili
(ii) svaki R8a i R8b, zajedno s N na kojeg su vezani, neovisno mogu tvoriti 3- do 8-eročlani zasićeni ili nezasićeni prsten, koji izborno sadrži jedan ili više O ili S atoma, ili jedan ili više dodatnih N atoma, u prstenu;
svaki R9 je neovisno (a) vodik; (b) (C1-C6)alkil; (c) fenil; ili (d) (C1-C6)alkil, supstituiran s arilom, alkoksi ili mono-, di- ili trihalogenom;
k je 0, 1 ili 2;
m je 1, 2, 3 ili 4; i
n je 0, 1 ili 2.
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima formulu III:
[image]
ili njegova farmaceutski prihvatljiva sol, solvat, hidrat, stereoizomer ili tautomer, gdje
X je jednostruka veza, -O(CH2)p- ili -NR9(CH2)p-;
R7 je vodik ili (C1-C6)alkil; i
p je 1, 2, 3, 4, 5 ili 6.
5. Spoj u skladu s patentnim zahtjevom 4, naznačen time što svaki
R3 je neovisno (C1-C6)alkil; i/ili
svaki od R4a i R4b je neovisno vodik; i/ili
R2 je -S(C1-C6)alkil, a svaki od R7 i R9 je neovisno vodik; i/ili
R6 je aril ili heteroaril, gdje su navedeni aril i heteroaril na položaju gdje je moguća supstitucija izborno supstituirani s jednim ili više supstituenata koje se bira iz skupine koju čine (a) halogen; (b) cijano; (c) nitro; (d) hidroksi; (e) -NR8aR8b; (f) -C(O)R9; (g) -C (O)NR8aR8b; (h) -OC(O)NR8aR8b; (i) -NR7C(O)OR9; (j) -NR7C(O)R9; (k) -C(O)OR9; (l) gvanidino; (m) heterociklil; (n) fenil; (o) feniloksi; (p) benzil; (q) benziloksi; (r) sulfamoil; (s) (C1-C6)alkilsulfonil; (t) (C1-C6)alkilaminosul-fonil; (u)di(C1-C6)alkilaminosulfonil; (v) (C1-C6)alkil, izborno supstituiran s mono-, di- ili trihalogenom; (w) (C1-C6) alkoksi, izborno supstituiran s mono-, di- ili trihalogenom; i (x) (C1-C6)alkiltio, izborno supstituiran s mono-, di- ili trihalogenom; i
svaki od R7 i R8 je neovisno vodik ili (C1-C6)alkil.
6. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima formulu IV:
[image]
ili njegova farmaceutski prihvatljiva sol, solvat, hidrat, stereoizomer ili tautomer, gdje
svaki R3 je neovisno (C1-C6)alkil;
svaki R10 je neovisno (a) halogen; (b) cijano; (c) nitro; (d) hidroksi; (e) -NR8aR8b; (f) -C(O)R9; (g) -C(O)NR8aR8b; (h) -OC(O)NR8aR8b; (i) -NR7C(O)OR9; (j) -NR7C(O)R9; (k) -C(O)OR9; (l) gvanidino; (m) heterociklil; (n) fenil; (o) feniloksi; (p) benzil; (q) benziloksi; (r) sulfamoil; (s) (C1-C6)alkilsulfonil; (t) (C1-C6)alkilaminosulfonil; (u) di(C1-C6)alkilaminosulfonil; (v) (C1-C6)alkil, izborno supstituiran s mono-, di- ili trihalogenom; (w) (C1-C6)alkoksi, izborno supstituiran s mono-, di- ili trihalogenom; ili (x) (C1-C6)alkiltio, izborno supstituiran s mono-, di- ili trihalogenom; i
q je 0, 1, 2, 3, 4 ili 5; ili
što ima formulu V:
[image]
ili njegova farmaceutski prihvatljiva sol, solvat, hidrat, stereoizomer ili tautomer, gdje
R2 je vodik ili halogen;
R3 je (C1-C6)alkil;
svaki R10 je neovisno (a) halogen; (b) cijano; (c) nitro; (d) hidroksi; (e) -NR8aR8b; (f) -C(O)R9; (g) -C(O)NR8aR8b; (h) -OC(O)NR8aR8b; (i) -NR7C(O)OR9; (j) -NR7C(O)R9; (k) -C(O)OR9; (l) gvanidino; (m) heterociklil; (n) fenil; (o) feniloksi; (p) benzil; (q) benziloksi; (r) sulfamoil; (s) (C1-C6)alkilsulfonil; (t) (C1-C6)alkilaminosulfonil; (u) di(C1-C6)alkilaminosulfonil; (v) (C1-C6)alkil, izborno supstituiran s mono-, di- ili trihalogenom; (w) (C1-C6)alkoksi, izborno supstituiran s mono-, di- ili trihalogenom; i (x) (C1-C6)alkiltio, izborno supstituiran s mono-, di- ili trihalogenom; i
q je 0, 1, 2, 3, 4 ili 5; ili
što ima formulu VI:
[image]
ili njegova farmaceutski prihvatljiva sol, solvat, hidrat, stereoizomer ili tautomer; ili
što ima formulu VII:
[image]
ili njegova farmaceutski prihvatljiva sol, solvat, hidrat, stereoizomer ili tautomer.
7. Spoj u skladu s patentnim zahtjevom 6, naznačen time što
svaki R10 je neovisno (a) halogen; (b) cijano; (c) nitro; (d) hidroksi; (e) -NH2; (f) -NH(C1-C6)alkil; (g) -N((C1-C6)alkil)2; (h) -C(O)(C1-C6)alkil; (i) -CO2H; (j) -NHC(O)(C1-C6)alkil; (k) -C(O)O(C1-C6)alkil; (l) fenil; (m) feniloksi; (n) benzil; (o) benziloksi; (p) sulfamoil; (q) (C1-C6)alkilsulfonil; (r) (C1-C6)alkilaminosulfonil; (s) di(C1-C6)alkilaminosulfonil; (t) (C1-C6)alkil, izborno supstituiran s mono-, di- ili trihalogenom; (u) (C1-C6)alkoksi, izborno supstituiran s mono-, di- ili trihalogenom; ili (v) (C1-C6)alkiltio, izborno supstituiran s mono-, di- ili trihalogenom.
8. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima formulu VIII:
[image]
ili njegova farmaceutski prihvatljiva sol, solvat, hidrat, stereoizomer ili tautomer, gdje
X je jednostruka veza, -O- ili -NH; ili
što ima formulu IX:
[image]
ili njegova farmaceutski prihvatljiva sol, solvat, hidrat, stereoizomer ili tautomer, gdje
R2 je vodik ili halogen; i
X je jednostruka veza, -O- ili -NH.
9. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima formulu koju se bira između:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
ili njegova farmaceutski prihvatljiva sol, solvat, hidrat, stereoizomer ili tautomer.
10. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1-9 i jednu ili više farmaceutski prihvatljivih podloga ili pomoćnih tvari.
11. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-9, naznačen time što je namijenjen upotrebi u liječenju ili profilaksi alergijske bolesti, ili jednog ili više njenih simptoma;
bolesti povezane s eozinofilima, ili jednog ili više njenih simptoma;
bolesti povezane s bazofilima, ili jednog ili više njenih simptoma;
upalne bolesti, ili jednog ili više njenih simptoma;
bolesti ili stanja, ili jednog ili više njenih simptoma, gdje se bolest ili stanje bira iz skupine koju čine astma, astma uzrokovana fizičkom aktivnošću, alergijski rinitis, atopični dermatitis, alergijski konjunktivitis, Churg-Straussov sindrom, sinusitis, bazofilna leukemija, kronična koprivnjača, bazofilna leukocitoza, psorijaza, ekzem, upalna bolest crijeva, ulcerozni kolitis, Crohnova bolest, COPD (kronični opstruktivni plućni poremećaj) i artritis;
bolesti ili stanja, ili jednog ili više njenih simptoma, gdje se bolest ili stanje bira iz skupine koju čine astma, astma uzrokovana fizičkom aktivnošću, alergijski rinitis, atopični dermatitis i alergijski konjunktivitis;
bolesti ili stanja, ili jednog ili više njenih simptoma, gdje se bolest ili stanje bira iz skupine koju čine Churg-Straussov sindrom i sinusitis;
bolesti ili stanja, ili jednog ili više njenih simptoma, gdje se bolest ili stanje bira iz skupine koju čine bazofilna leukemija, kronična koprivnjača i bazofilna leukocitoza;
bolesti ili stanja, ili jednog ili više njenih simptoma, gdje se bolest ili stanje bira iz skupine koju čine psorijaza, ekzem, upalna bolest crijeva, ulcerozni kolitis, Crohnova bolest, COPD (kronični opstruktivni plućni poremećaj) i artritis.
12. Spoj u skladu s patentnim zahtjevima 1-9, namijenjen upotrebi u terapiji bilo koje od bolesti u skladu s patentnim zahtjevom 11, naznačen time što spoj se pripravlja za oralnu, parenteralnu ili topikalnu primjenu; i/ili
kada se spoj pripravlja za primjenu u kombinaciji ili naizmjece s drugim terapijskim sredstvom;
izborno kada je drugo terapijsko sredstvo korisno za liječenje astme, astme uzrokovane fizičkom aktivnošću, alergijskog rinitisa, atopičnog dermatitisa, alergijskog konjunktivitisa, Churg-Straussovog sindroma, sinusitisa, bazofilne leukemije, kronične koprivnjače, bazofilne leukocitoze, psorijaze, ekzema, upalne bolesti crijeva, ulceroznog kolitisa, Crohnove bolesti, COPD (kronični opstruktivni plućni poremećaj), artritisa, ili njihovih simptoma.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US99538607P | 2007-09-25 | 2007-09-25 | |
| PCT/US2008/011053 WO2009042138A1 (en) | 2007-09-25 | 2008-09-24 | Alkylthio pyrimidines as crth2 antagonists |
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| Publication Number | Publication Date |
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| HRP20120377T1 true HRP20120377T1 (hr) | 2012-05-31 |
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| HRP20120377AT HRP20120377T1 (hr) | 2007-09-25 | 2012-05-03 | Alkiltiopirimidini kao antagonisti crth2 |
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| Country | Link |
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| US (1) | US8324229B2 (hr) |
| EP (1) | EP2205569B1 (hr) |
| JP (1) | JP5524847B2 (hr) |
| KR (1) | KR20100061747A (hr) |
| CN (1) | CN101874023A (hr) |
| AR (1) | AR068632A1 (hr) |
| AT (1) | ATE547407T1 (hr) |
| AU (1) | AU2008305632B2 (hr) |
| BR (1) | BRPI0817319A2 (hr) |
| CA (1) | CA2700524C (hr) |
| CL (1) | CL2008002826A1 (hr) |
| CY (1) | CY1112720T1 (hr) |
| DK (1) | DK2205569T3 (hr) |
| ES (1) | ES2383249T3 (hr) |
| HR (1) | HRP20120377T1 (hr) |
| IL (1) | IL205647A0 (hr) |
| MX (1) | MX2010003182A (hr) |
| NZ (1) | NZ584352A (hr) |
| PL (1) | PL2205569T3 (hr) |
| PT (1) | PT2205569E (hr) |
| RU (1) | RU2491280C2 (hr) |
| SI (1) | SI2205569T1 (hr) |
| TW (1) | TW200922587A (hr) |
| WO (1) | WO2009042138A1 (hr) |
| ZA (1) | ZA201002173B (hr) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| AR068633A1 (es) | 2007-09-25 | 2009-11-25 | Actimis Pharmaceuticals Inc | Pirimidinas sustituidas con 2-s- bencilo como antagonistas de crth2 |
| CN101903394B (zh) * | 2007-10-18 | 2013-12-25 | 贝林格尔.英格海姆国际有限公司 | 二氢噻吩并[3,2-d]嘧啶的制备及其中使用的中间体 |
| EP2393492A1 (en) * | 2009-02-09 | 2011-12-14 | Boehringer Ingelheim International GmbH | New pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders |
| HUE025318T2 (en) * | 2010-01-27 | 2016-02-29 | Boehringer Ingelheim Int | Pyrazole Compounds as CRTH2 antagonists |
| JP2013535457A (ja) * | 2010-07-28 | 2013-09-12 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 呼吸器系及び炎症性疾患の治療用医薬組成物 |
| EP2457900A1 (en) | 2010-11-25 | 2012-05-30 | Almirall, S.A. | New pyrazole derivatives having CRTh2 antagonistic behaviour |
| US8759386B2 (en) | 2011-01-24 | 2014-06-24 | Boehringer Ingelheim International Gmbh | Pyrazole compounds as CRTH2 antagonists |
| WO2012130633A1 (en) | 2011-03-25 | 2012-10-04 | Boehringer Ingelheim International Gmbh | Pyrazole compounds as crth2 antagonists |
| GB2494277A (en) | 2011-08-29 | 2013-03-06 | Univ Heriot Watt | Electro-spinning nanofibres onto a moving wire card |
| CA2856100C (en) * | 2011-11-17 | 2016-09-27 | Kbp Biosciences Co., Ltd. | Nitrogen-containing fused ring compounds as crth2 antagonists |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| BE790679A (fr) | 1971-11-03 | 1973-04-27 | Ici Ltd | Derives de l'indole |
| GB9125842D0 (en) | 1991-12-04 | 1992-02-05 | Ici Plc | Heterocyclic derivatives |
| CA2147275A1 (en) * | 1992-10-16 | 1994-04-28 | Hirokazu Yamada | Pyrimidine derivative |
| GB2359078A (en) | 2000-02-11 | 2001-08-15 | Astrazeneca Uk Ltd | Pharmaceutically active pyrimidine derivatives |
| JP2001302667A (ja) | 2000-04-28 | 2001-10-31 | Bayer Ag | イミダゾピリミジン誘導体およびトリアゾロピリミジン誘導体 |
| US6878522B2 (en) | 2000-07-07 | 2005-04-12 | Baiyong Li | Methods for the identification of compounds useful for the treatment of disease states mediated by prostaglandin D2 |
| EP1413306A1 (en) | 2002-10-21 | 2004-04-28 | Warner-Lambert Company LLC | Tetrahydroquinoline derivatives as CRTH2 antagonists |
| ES2401079T3 (es) | 2002-12-20 | 2013-04-16 | Amgen Inc. | Moduladores del asma y de la inflamación alérgica |
| DE60303238T2 (de) * | 2003-04-25 | 2006-09-14 | Actimis Pharmaceuticals, Inc., La Jolla | Pyrimidin-Essigsäure Derivate geeignet zur Behandlung von CRTH2-bedingten Krankheiten |
| RU2373208C2 (ru) * | 2004-01-31 | 2009-11-20 | Актимис Фармасьютикалз, Инк. | Производные имидазо[1,2-c]пиримидинилуксусной кислоты |
| WO2007062677A1 (en) * | 2005-11-30 | 2007-06-07 | 7Tm Pharma A/S | Thiazolyl- and pyrimidinyl-acetic acids and their use as crth2 receptor ligands |
| AR068633A1 (es) | 2007-09-25 | 2009-11-25 | Actimis Pharmaceuticals Inc | Pirimidinas sustituidas con 2-s- bencilo como antagonistas de crth2 |
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- 2008-09-24 EP EP08833849A patent/EP2205569B1/en not_active Not-in-force
- 2008-09-24 KR KR1020107008867A patent/KR20100061747A/ko not_active Application Discontinuation
- 2008-09-24 CN CN200880117669A patent/CN101874023A/zh active Pending
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- 2008-09-24 WO PCT/US2008/011053 patent/WO2009042138A1/en active Application Filing
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- 2008-09-24 NZ NZ584352A patent/NZ584352A/en not_active IP Right Cessation
- 2008-09-24 PT PT08833849T patent/PT2205569E/pt unknown
- 2008-09-24 CL CL2008002826A patent/CL2008002826A1/es unknown
- 2008-09-24 TW TW097136691A patent/TW200922587A/zh unknown
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- 2008-09-24 MX MX2010003182A patent/MX2010003182A/es active IP Right Grant
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- 2010-03-26 ZA ZA2010/02173A patent/ZA201002173B/en unknown
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Also Published As
| Publication number | Publication date |
|---|---|
| PL2205569T3 (pl) | 2012-08-31 |
| AU2008305632A1 (en) | 2009-04-02 |
| IL205647A0 (en) | 2011-07-31 |
| JP5524847B2 (ja) | 2014-06-18 |
| AU2008305632B2 (en) | 2014-01-30 |
| CL2008002826A1 (es) | 2009-08-07 |
| EP2205569B1 (en) | 2012-02-29 |
| BRPI0817319A2 (pt) | 2015-03-17 |
| RU2010116293A (ru) | 2011-11-10 |
| WO2009042138A1 (en) | 2009-04-02 |
| KR20100061747A (ko) | 2010-06-08 |
| DK2205569T3 (da) | 2012-05-21 |
| US20100298361A1 (en) | 2010-11-25 |
| ZA201002173B (en) | 2011-05-25 |
| ES2383249T3 (es) | 2012-06-19 |
| EP2205569A1 (en) | 2010-07-14 |
| CA2700524A1 (en) | 2009-04-02 |
| RU2491280C2 (ru) | 2013-08-27 |
| JP2010540520A (ja) | 2010-12-24 |
| AR068632A1 (es) | 2009-11-25 |
| US8324229B2 (en) | 2012-12-04 |
| TW200922587A (en) | 2009-06-01 |
| CN101874023A (zh) | 2010-10-27 |
| ATE547407T1 (de) | 2012-03-15 |
| CY1112720T1 (el) | 2016-02-10 |
| CA2700524C (en) | 2017-08-01 |
| WO2009042138A9 (en) | 2009-10-15 |
| MX2010003182A (es) | 2010-06-02 |
| PT2205569E (pt) | 2012-05-25 |
| SI2205569T1 (sl) | 2012-06-29 |
| NZ584352A (en) | 2012-03-30 |
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