HRP20230313T1 - Modulatori receptora cxcr7 piperidina - Google Patents
Modulatori receptora cxcr7 piperidina Download PDFInfo
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- HRP20230313T1 HRP20230313T1 HRP20230313TT HRP20230313T HRP20230313T1 HR P20230313 T1 HRP20230313 T1 HR P20230313T1 HR P20230313T T HRP20230313T T HR P20230313TT HR P20230313 T HRP20230313 T HR P20230313T HR P20230313 T1 HRP20230313 T1 HR P20230313T1
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- Croatia
- Prior art keywords
- alkyl
- membered heteroaryl
- monosubstituted
- phenyl
- unsubstituted
- Prior art date
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- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 title 2
- 125000000217 alkyl group Chemical group 0.000 claims 39
- 125000001072 heteroaryl group Chemical group 0.000 claims 35
- 125000002947 alkylene group Chemical group 0.000 claims 25
- 125000002993 cycloalkylene group Chemical group 0.000 claims 25
- 125000003545 alkoxy group Chemical group 0.000 claims 23
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 23
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 23
- 125000000753 cycloalkyl group Chemical group 0.000 claims 22
- 125000001424 substituent group Chemical group 0.000 claims 22
- 125000001153 fluoro group Chemical group F* 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 18
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 17
- 229910052736 halogen Inorganic materials 0.000 claims 16
- 125000004430 oxygen atom Chemical group O* 0.000 claims 16
- 125000004076 pyridyl group Chemical group 0.000 claims 16
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 16
- 150000002367 halogens Chemical class 0.000 claims 15
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 15
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 12
- -1 chloro, methyl Chemical group 0.000 claims 9
- 150000001204 N-oxides Chemical class 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 125000003386 piperidinyl group Chemical group 0.000 claims 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- BOTWGQIJRFXZDN-ICSRJNTNSA-N N-[(3S,4S)-1-(cyclopropylmethyl)-3-[(1-pyrimidin-2-ylcyclopropyl)carbamoyl]piperidin-4-yl]-5-(2,4-difluorophenyl)-1,3,4-thiadiazole-2-carboxamide Chemical compound N1=C(N=CC=C1)C1(CC1)NC(=O)[C@H]1CN(CC[C@@H]1NC(=O)C=1SC(=NN=1)C1=C(C=C(C=C1)F)F)CC1CC1 BOTWGQIJRFXZDN-ICSRJNTNSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000004761 fibrosis Effects 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- DFZSUXTYPCCZKJ-HKUYNNGSSA-N 5-(2,4-difluorophenyl)-N-[(3S,4S)-1-[(1-fluorocyclopropyl)methyl]-3-[(1-pyrimidin-2-ylcyclopropyl)carbamoyl]piperidin-4-yl]-1,3,4-thiadiazole-2-carboxamide Chemical compound N1=C(N=CC=C1)C1(CC1)NC(=O)[C@H]1CN(CC[C@@H]1NC(=O)C=1SC(=NN=1)C1=C(C=C(C=C1)F)F)CC1(CC1)F DFZSUXTYPCCZKJ-HKUYNNGSSA-N 0.000 claims 1
- JNKPVHQCPZHLJL-ICSRJNTNSA-N N-[(3S,4S)-1-cyclobutyl-3-[(1-pyrimidin-2-ylcyclopropyl)carbamoyl]piperidin-4-yl]-5-(2,4-difluorophenyl)-1,3,4-thiadiazole-2-carboxamide Chemical compound N1=C(N=CC=C1)C1(CC1)NC(=O)[C@H]1CN(CC[C@@H]1NC(=O)C=1SC(=NN=1)C1=C(C=C(C=C1)F)F)C1CCC1 JNKPVHQCPZHLJL-ICSRJNTNSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 239000012752 auxiliary agent Substances 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
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Claims (17)
1. Spoj, naznačen time, da je predstavljen formulom (I)
[image]
u kojoj
su dva supstituenta od piperidinskog prstena: R1-CO- i -NH-CO-Ar1-Ar2, u relativnoj trans-konfiguraciji;
Ar1 predstavlja nesupstituiranu 5-člani heteroarilen skupinu koja sadrži jedan sumporov atom u prstenu i jedan ili dva dušikova atoma u prstenu, pri čemu su -NH-CO- skupina i Ar2 vezani u meta rasporedu na atome u prstenu od Ar1;
Ar2 predstavlja fenil, ili 6-člani heteroaril; pri čemu je navedeni fenil ili 6-člani heteroaril neovisno monosupstituiran, disupstituiran ili trisupstituiran, pri čemu se supstituenti neovisno biraju od fluoro, kloro, metil, cijano, metoksi, ili (C1)fluoroalkil;
R1 predstavlja RN1RN2N, pri čemu
• RN1 predstavlja
‣ vodik;
‣ (C16)alkil;
‣ (C16)alkil koji je monosupstituiran s
▪ hidroksi;
▪ (C13)alkoksi;
▪ 2-hidroksi-etoksi;
▪ -CO-NH2;
▪ -SO2-(C13)alkil;
▪ cijano;
▪ (C13)fluoroalkoksi;
▪ -NRN3RN4, pri čemu RN3 i RN4 neovisno predstavljaju vodik ili (C14)alkil;
‣ (C26)alkinil;
‣ (C25)fluoroalkil;
‣ (C14)alkoksi;
‣ 2-(2-okso-pirolidin-1-il)-etil;
‣ skupinu -L1-Cy1; pri čemu
▪ L1 predstavlja izravnu vezu, (C13)alkilen, ili (C35)cikloalkilen; i
▪ Cy1 predstavlja (C36)cikloalkil, pri čemu navedeni (C36)cikloalkil opcionalno sadrži jedan kisikov atom u prstenu; gdje je navedeni (C36)cikloalkil neovisno nesupstituiran; ili je monosupstituiran s fluoro, metil, ili hidroksi, -CO-(C14)alkoksi, ili cijano; ili je disupstituiran s fluoro, ili je trisupstituiran s metilom i dva fluoro;
‣ skupinu -L2-Ar3, pri čemu
▪ L2 predstavlja izravnu vezu, (C14)alkilen;
*(C35)cikloalkilen(C02)alkilen pri čemu navedeni (C35)cikloalkilen opcionalno sadrži jedan kisikov atom u prstenu, gdje zvjezdica označava vezu s kojom je povezan Ar3; *(C12)alkilen(C35)cikloalkilen pri čemu navedeni (C35)cikloalkilen opcionalno sadrži jedan kisikov atom u prstenu, gdje zvjezdica označava vezu s kojom je povezan Ar3; ili (C13)alkilen koji je monosupstituiran s hidroksi, trifluorometil, ili -CO-(C14)alkoksi; i
▪ Ar3 predstavlja fenil, ili 5-člani ili 6-člani heteroaril; pri čemu je navedeni fenil ili 5-člani ili 6-člani heteroaril neovisno nesupstituiran, ili je monosupstituiran, ili disupstituiran; pri čemu se supstituenti neovisno biraju od (C14)alkil, (C14)alkoksi, halogen, hidroksi, (C13)fluoroalkil, ili (C13)fluoroalkoksi; pri čemu, u slučaju da Ar3 predstavlja 6-člani heteroaril koji je piridil ili pirimidinil, takav piridil ili pirimidinil se može dodatno nalaziti u obliku odgovarajućeg N-oksida;
i RN2 neovisno predstavlja vodik, (C14)alkil, ili (C23)fluoroalkil;
• ili se RN1 i RN2 zajedno s dušikovim atom na kojega su vezani za tvorbu 4-članog do 6-članog prstena, biraju od sljedećih:
‣ azetidinil, pirolidinil ili piperidinil; od kojih je svaki neovisno
▪ nesupstituiran;
▪ ili monosupstituiran s fluoro, metil, ili hidroksi;
▪ ili disupstituiran s fluoro;
▪ ili monosupstituiran s Ar4, pri čemu Ar4 predstavlja fenil, ili 5-člani ili 6-člani heteroaril; pri čemu je navedeni fenil ili 5-člani ili 6-člani heteroaril neovisno nesupstituiran, ili je monosupstituiran, ili disupstituiran; gdje se supstituenti neovisno biraju od (C14)alkil, (C14)alkoksi, halogen, (C13)fluoroalkil,ili(C13)fluoroalkoksi; ili
‣ morfolinil;
R2 predstavlja
• vodik;
• (C16)alkil;
• (C26)alkil koji je monosupstituiran sa (C13)alkoksi, ili hidroksi;
• (C35)alkenil;
• cijano-metil;
• (C23)fluoroalkil;
• (C38)cikloalkil-(C0-3)alkil; pri čemu je (C38)cikloalkil nesupstituiran, ili je monosupstituiran ili disupstituiran, gdje se supstituenti neovisno biraju od (C13)alkil, fluoro, hidroksi, hidroksi-(C13)alkil, (C13)alkoksi, ili (C13)fluoroalkil;
• tietan-3-il;
• (C38)cikloalkenil(C13)alkil; ili
• Ar5-CH2- pri čemu Ar5 predstavlja fenil, ili 5-člani ili 6-člani heteroaril, pri čemu je fenil ili 5-člani ili 6-člani heteroaril neovisno nesupstituiran, ili je monosupstituiran ili disupstituiran, gdje se supstituenti neovisno biraju od (C14)alkil, (C14)alkoksi, halogen, (C13)fluoroalkil, ili (C13)fluoroalkoksi; i
R3 predstavlja vodik, ili metil;
ili njegova farmaceutski prihvatljiva sol.
2. Spoj formule (I) kao što je definiran za patentni zahtjev 1, koji također predstavlja spojeve Formule (Is), naznačen time, da su dva supstituenta od piperidinskog prstena: R1-CO- i -NH-CO-Ar1-Ar2, u relativnoj trans-konfiguraciji, pri čemu apsolutna konfiguracija od dva kiralna atoma ugljika na poziciji 3 i 4 od piperidinskog prstena, je (3S,4S):
[image]
ili njegova farmaceutski prihvatljiva sol.
3. Spoj prema patentnom zahtjevu 1 ili 2; naznačen time, da R3 predstavlja vodik;
ili njegova farmaceutski prihvatljiva sol.
4. Spoj prema bilo kojem od patentnih zahtjeva 1 do 3; naznačen time, da Ar1 predstavlja [1,3,4]tiadiazol-2,5-diil ili izotiazol-3,5-diil;
ili njegova farmaceutski prihvatljiva sol.
5. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4; naznačen time, da Ar2 predstavlja fenil koji je monosupstituiran, disupstituiran ili trisupstituiran; gdje se jedan ili dva od navedenih supstituenata neovisno biraju od fluoro, kloro, i metil, i preostali, ako je prisutan, jest/jesu fluoro;
ili njegova farmaceutski prihvatljiva sol.
6. Spoj prema bilo kojem od patentnih zahtjeva 1 do 5; naznačen time, da R1 predstavlja RN1RN2N, pri čemu
• RN1 predstavlja
‣ (C16)alkil;
‣ (C16)alkil koji je monosupstituiran s
▪ hidroksi;
▪ (C13)alkoksi;
▪ 2-hidroksi-etoksi;
▪ -CO-NH2;
▪ -SO2-(C13)alkil;
▪ cijano;
▪ (C13)fluoroalkoksi;
▪ -NRN3RN4, pri čemu RN3 i RN4 neovisno predstavljaju vodik ili (C14)alkil;
‣ (C26)alkinil;
‣ (C25)fluoroalkil;
‣ 2-(2-okso-pirolidin-1-il)-etil;
‣ skupinu -L1-Cy1; pri čemu
▪ L1 predstavlja izravnu vezu, (C13)alkilen, ili (C35)cikloalkilen; i
▪ Cy1 predstavlja (C36)cikloalkil, pri čemu navedeni (C36)cikloalkil opcionalno sadrži jedan kisikov atom u prstenu; gdje je navedeni (C36)cikloalkil neovisno nesupstituiran; ili je monosupstituiran s fluoro, metil, hidroksi, CO-(C14)alkoksi, ili cijano; ili disupstituiran s fluoro, ili je trisupstituiran s metilom i dva fluoro;
‣ skupinu -L2-Ar3, pri čemu
▪ L2 predstavlja (C14)alkilen; (C35)cikloalkilen pri čemu navedeni (C35)cikloalkilen opcionalno sadrži jedan kisikov atom u prstenu; *(C35)cikloalkilen(C12)alkilen pri čemu navedeni (C35)cikloalkilen opcionalno sadrži jedan kisikov atom u prstenu, gdje zvjezdica označava vezu s kojom je povezan Ar3; *(C12)alkilen(C35)cikloalkilen pri čemu navedeni (C35)cikloalkilen opcionalno sadrži jedan kisikov atom u prstenu, pri čemu zvjezdica označava vezu s kojom je povezan Ar3; ili (C13)alkilen koji je monosupstituiran s hidroksi ili trifluorometilom; i
▪ Ar3 predstavlja fenil, ili 5-člani heteroaril koji sadrži jedan kisikov atom i jedan ili dva dušikova atoma, ili 6-člani heteroaril koji sadrži jedan ili dva dušikova atoma; pri čemu je navedeni fenil ili 5-člani ili 6-člani heteroaril neovisno nesupstituiran, ili je monosupstituiran, ili disupstituiran; pri čemu se supstituenti neovisno biraju od (C14)alkil, (C14)alkoksi, halogen, (C13)fluoroalkil, ili (C13)fluoroalkoksi; pri čemu, u slučaju da Ar3 predstavlja 6-člani heteroaril koji je piridil ili pirimidinil, takav piridil ili pirimidinil se može dodatno nalaziti u obliku odgovarajućeg N-oksida;
i RN2 neovisno predstavlja vodik, ili (C14)alkil;
ili njegova farmaceutski prihvatljiva sol.
7. Spoj prema bilo kojem od patentnih zahtjeva 1 do 5; naznačen time, da
R1 predstavlja RN1RN2N, pri čemu
• RN1 predstavlja
‣ (C36)cikloalkil, pri čemu navedeni (C36)cikloalkil opcionalno sadrži jedan kisikov atom u prstenu; pri čemu je navedeni (C36)cikloalkil neovisno nesupstituiran, ili je monosupstituiran s fluoro, metil, ili hidroksi, ili disupstituiran s fluoro, ili je trisupstituiran s metilom i dva fluoro;
‣ (C36)cikloalkil(C13)alkilen, pri čemu navedeni (C36)cikloalkil opcionalno sadrži jedan kisikov atom u prstenu;
‣ (C36)cikloalkil(C35)cikloalkilen;
‣ fenil(C14)alkilen pri čemu je navedeni fenil nesupstituiran, ili monosupstituiran, ili disupstituiran; pri čemu se supstituenti neovisno biraju od (C14)alkil, (C14)alkoksi, halogen, (C13)fluoroalkil, ili (C13)fluoroalkoksi;
‣ fenil(C13)alkilen pri čemu je navedeni (C13)alkilen monosupstituiran s hidroksi;
‣ fenil(C35)cikloalkilen; pri čemu navedeni (C35)cikloalkilen opcionalno sadrži jedan kisikov atom u prstenu, i pri čemu je navedeni fenil nesupstituiran, ili je monosupstituiran, ili disupstituiran; gdje se supstituenti neovisno biraju od (C14)alkil, (C14)alkoksi, halogen, hidroksi, (C13)fluoroalkil, ili (C13)fluoroalkoksi;
‣ fenil(C35)cikloalkilen(C12)alkilen pri čemu navedeni (C35)cikloalkilen opcionalno sadrži jedan kisikov atom u prstenu, i pri čemu je navedeni fenil nesupstituiran, ili je monosupstituiran s halogenom;
‣ fenil(C12)alkilen(C35)cikloalkilen pri čemu navedeni (C35)cikloalkilen opcionalno sadrži jedan kisikov atom u prstenu;
‣ 5-člani heteroaril(C13)alkilen, pri čemu navedeni 5-člani heteroaril sadrži jedan kisikov atom i jedan ili dva dušikova atoma; i pri čemu je navedeni 5-člani heteroaril nesupstituiran, ili je monosupstituiran, ili disupstituiran; gdje se supstituenti neovisno biraju od (C14)alkil, (C14)alkoksi, halogen, (C13)fluoroalkil, ili (C13)fluoroalkoksi;
‣ 6-člani heteroaril(C14)alkilen, pri čemu navedeni 6-člani heteroaril sadrži jedan ili dva dušikova atoma; i pri čemu je navedeni 6-člani heteroaril nesupstituiran, ili je monosupstituiran, ili disupstituiran; gdje se supstituenti neovisno biraju od (C14)alkil, (C14)alkoksi, halogen, (C13)fluoroalkil, ili (C13)fluoroalkoksi; pri čemu, u slučaju da Ar3 predstavlja piridil ili pirimidinil, takav piridil ili pirimidinil se može dodatno nalaziti u obliku odgovarajućeg N-oksida;
‣ 6-člani heteroaril(C13)alkilen, pri čemu je navedeni (C13)alkilen monosupstituiran s hidroksi ili trifluorometilom; gdje navedeni 6-člani heteroaril sadrži jedan ili dva dušikova atoma; ili
‣ 6-člani heteroaril(C35)cikloalkilen, pri čemu navedeni 6-člani heteroaril sadrži jedan ili dva dušikova atoma; i pri čemu je navedeni 6-člani heteroaril nesupstituiran, ili monosupstituiran, ili disupstituiran; pri čemu se supstituenti neovisno biraju od (C14)alkil, (C14)alkoksi, halogen, (C13)fluoroalkil, ili (C13)fluoroalkoksi; pri čemu, u slučaju da Ar3 predstavlja piridil ili pirimidinil, takav piridil ili pirimidinil se može dodatno nalaziti u obliku odgovarajućeg N-oksida;
‣ 6-člani heteroaril(C35)cikloalkilen(C12)alkilen pri čemu navedeni 6-člani heteroaril sadrži jedan ili dva dušikova atoma; i pri čemu je navedeni 6-člani heteroaril nesupstituiran;
i RN2 neovisno predstavlja vodik, ili (C14)alkil;
• ili RN1 predstavlja (C13)alkil; i RN2 predstavlja vodik, ili metil;
ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema bilo kojem od patentnih zahtjeva 1 do 5; naznačen time, da R1 predstavlja RN1RN2N, pri čemu
• RN1 predstavlja
‣ (C36)cikloalkil(C13)alkilen, pri čemu navedeni (C36)cikloalkil opcionalno sadrži jedan kisikov atom u prstenu;
‣ fenil(C14)alkilen pri čemu je navedeni fenil nesupstituiran, ili je monosupstituiran, ili disupstituiran; gdje se supstituenti neovisno biraju od (C14)alkil, (C14)alkoksi, halogen, (C13)fluoroalkil, ili (C13)fluoroalkoksi;
‣ fenil(C35)cikloalkilen pri čemu navedeni (C35)cikloalkilen opcionalno sadrži jedan kisikov atom u prstenu, i pri čemu je navedeni fenil nesupstituiran, ili je monosupstituiran, ili disupstituiran; gdje se supstituenti neovisno biraju od (C14)alkil, (C14)alkoksi, halogen, hidroksi, (C13)fluoroalkil, ili (C13)fluoroalkoksi;
‣ 6-člani heteroaril(C14)alkilen, pri čemu navedeni 6-člani heteroaril sadrži jedan ili dva dušikova atoma; i pri čemu je navedeni 6-člani heteroaril nesupstituiran, ili monosupstituiran, ili disupstituiran; gdje se supstituenti neovisno biraju od (C14)alkil, (C14)alkoksi, halogen, (C13)fluoroalkil, ili (C13)fluoroalkoksi; pri čemu, u slučaju da Ar3 predstavlja piridil ili pirimidinil, takav piridil ili pirimidinil se može dodatno nalaziti u obliku odgovarajućeg N-oksida;
‣ 6-člani heteroaril(C35)cikloalkilen, pri čemu navedeni 6-člani heteroaril sadrži jedan ili dva dušikova atoma; i pri čemu je navedeni 6-člani heteroaril nesupstituiran, ili je monosupstituiran, ili disupstituiran; gdje se supstituenti neovisno biraju od (C14)alkil, (C14)alkoksi, halogen, (C13)fluoroalkil, ili (C13)fluoroalkoksi; pri čemu, u slučaju da Ar3 predstavlja piridil ili pirimidinil, takav piridil ili pirimidinil se može dodatno nalaziti u obliku odgovarajućeg N-oksida;
i RN2 neovisno predstavlja vodik, ili (C14)alkil;
ili njegova farmaceutski prihvatljiva sol.
9. Spoj prema bilo kojem od patentnih zahtjeva 1 do 5; naznačen time, da R1 predstavlja RN1RN2N, pri čemu
• RN1 predstavlja
‣ 6-člani heteroaril(C14)alkilen, pri čemu navedeni 6-člani heteroaril sadrži jedan ili dva dušikova atoma; i pri čemu je navedeni 6-člani heteroaril nesupstituiran, ili monosupstituiran, ili disupstituiran; gdje se supstituenti neovisno biraju od (C14)alkil, (C14)alkoksi, halogen, (C13)fluoroalkil, ili (C13)fluoroalkoksi; pri čemu, u slučaju da Ar3 predstavlja piridil ili pirimidinil, takav piridil ili pirimidinil se može dodatno nalaziti u obliku odgovarajućeg N-oksida;
‣ 6-člani heteroaril(C35)cikloalkilen, pri čemu navedeni 6-člani heteroaril sadrži jedan ili dva dušikova atoma; i pri čemu je navedeni 6-člani heteroaril nesupstituiran, ili monosupstituiran, ili disupstituiran; gdje se supstituenti neovisno biraju od (C14)alkil, (C14)alkoksi, halogen, (C13)fluoroalkil, ili (C13)fluoroalkoksi; pri čemu, u slučaju da Ar3 predstavlja piridil ili pirimidinil, takav piridil ili pirimidinil se može dodatno nalaziti u obliku odgovarajućeg N-oksida;
i RN2 neovisno predstavlja vodik ili metil.
ili njegova farmaceutski prihvatljiva sol.
10. Spoj prema bilo kojem od patentnih zahtjeva 1 do 9; naznačen time, da R2 predstavlja
• (C38)cikloalkil-(C1-3)alkil, pri čemu je (C38)cikloalkil nesupstituiran; ili je monosupstituiran pri čemu supstituent je (C13)alkil, fluoro, ili (C13)fluoroalkil; ili je disupstituiran s fluoro; ili
• (C38)cikloalkil, pri čemu je (C38)cikloalkil nesupstituiran, ili monosupstituiran ili disupstituiran gdje se supstituenti neovisno biraju od (C13)alkil, ili fluoro;
ili njegova farmaceutski prihvatljiva sol.
11. Spoj prema bilo kojem od patentnih zahtjeva 1 do 9; naznačen time, da R2 predstavlja
• nesupstituirani (C38)cikloalkil-(C1-3)alkil; ili
• nesupstituirani (C36)cikloalkil; ili
• (C38)cikloalkil, pri čemu je (C38)cikloalkil disupstituiran s fluoro; ili
• (C38)cikloalkil-(C1-3)alkil; pri čemu je (C38)cikloalkil monosupstituiran s metilom, fluoro, ili (C1)fluoroalkil; ili je disupstituiran s fluoro;
ili njegova farmaceutski prihvatljiva sol.
12. Spoj prema patentnom zahtjevu 1, naznačen time, da je:
(3S,4S)-1-Ciklobutil-4-{[5-(2,4-difluoro-fenil)-[1,3,4]tiadiazol-2-karbonil]-amino}-piperidin-3-karboksilna kiselina (1-pirimidin-2-il-ciklopropil)-amid;
(3S,4S)-4-{[5-(2,4-difluoro-fenil)-[1,3,4]tiadiazol-2-karbonil]-amino}-1-(1-fluoro-ciklopropilmetil)-piperidin-3-karboksilna kiselina (1-pirimidin-2-il-ciklopropil)-amid;
ili
(3S,4S)-1-Ciklopropilmetil-4-{[5-(2,4-difluoro-fenil)-[1,3,4]tiadiazol-2-karbonil]-amino}-piperidin-3-karboksilna kiselina (1-pirimidin-2-il-ciklopropil)-amid;
ili njegova farmaceutski prihvatljiva sol.
13. Spoj prema patentnom zahtjevu 12, naznačen time, da je (3S,4S)-1-Ciklopropilmetil-4-{[5-(2,4-difluoro-fenil)-[1,3,4]tiadiazol-2-karbonil]-amino}-piperidin-3-karboksilna kiselina (1-pirimidin-2-il-ciklopropil)-amid;
ili njegova farmaceutski prihvatljiva sol.
14. Farmaceutski pripravak, naznačen time, da sadrži, kao aktivni sastojak, jedan ili više spojeva u skladu s bilo kojem od patentnih zahtjeva 1 do 13, ili njihovih farmaceutski prihvatljivih soli, i najmanje jedno terapijski inertno pomoćno sredstvo.
15. Spoj prema bilo kojem od patentnih zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time, da se upotrebljava kao lijek.
16. Spoj prema bilo kojem od patentnih zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu u prevenciji ili liječenju raka, autoimunih poremećaja, upalnih bolesti, odbacivanja transplantata, ili fibroze.
17. Uporaba spoja formule (I) prema definiciji u patentnom zahtjevu 1, ili njegove farmaceutski prihvatljive soli, naznačena time, da je za proizvodnju lijeka za prevenciju ili liječenje raka, autoimunih poremećaja, upalnih bolesti, odbacivanja transplantata, ili fibroze.
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| AU2020372647A1 (en) | 2019-10-31 | 2022-06-16 | Idorsia Pharmaceuticals Ltd | Combination of a CXCR7 antagonist with an S1P1 receptor modulator |
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