HRP20201008T1 - SUPSTITUIRANI SPOJEVI PIRAZOLO[1,5-a]PIRIDINA KAO INHIBITORI RET-KINAZE - Google Patents

SUPSTITUIRANI SPOJEVI PIRAZOLO[1,5-a]PIRIDINA KAO INHIBITORI RET-KINAZE Download PDF

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HRP20201008T1
HRP20201008T1 HRP20201008TT HRP20201008T HRP20201008T1 HR P20201008 T1 HRP20201008 T1 HR P20201008T1 HR P20201008T T HRP20201008T T HR P20201008TT HR P20201008 T HRP20201008 T HR P20201008T HR P20201008 T1 HRP20201008 T1 HR P20201008T1
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alkyl
substituted
ring
fluorines
cancer
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Steven W. Andrews
Sean ARONOW
James F. Blake
Barbara J. Brandhuber
Adam Cook
Julia Haas
Yutong Jiang
Gabrielle R. KOLAKOWSKI
Elizabeth A. MCFADDIN
Megan L. MCKENNEY
Oren T. MCNULTY
Andrew T. Metcalf
David A. Moreno
Tony P. Tang
Li Ren
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Array Biopharma Inc.
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    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/495—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K31/495—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
    • A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
    • 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
    • A61K31/495—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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Claims (22)

1. Spoj Formule I: [image] i njegove farmaceutski prihvatljive soli i solvati, naznačen time što: X1, X2, X3 i X4 su neovisno CH, CF, CCH3 ili N, gdje su nula, jedan ili dva od X1, X2, X3 i X4 N; A je H, CN, Cl, CH3-, CH3CH2-, ciklopropil, -CH2CN ili -CH(CN)CH3; B je (a) vodik, (b) C1-C6 alkil, koji može biti supstituiran s 1-3 fluora, (c) hidroksiC2-C6 alkil-, gdje alkilni dio može biti supstituiran s 1-3 fluora ili C3-C6 cikloalkilidenskim prstenom, (d) dihidroksiC3-C6 alkil-, gdje alkilni dio može biti supstituiran s C3-C6 cikloalkilidenskim prstenom, (e) (C1-C6 alkoksi)C1-C6 alkil-, koji može biti supstituiran s 1-3 fluora, (f) (R1R2N)C1-C6 alkil-, gdje navedeni alkilni dio može biti supstituiran s OH, te gdje su R1 i R2 neovisno H ili C1-C6 alkil (koji može biti supstituiran s 1-3 fluora); (g) hetAr1C1-C3 alkil-, gdje je hetAr1 5-6-eročlani heteroarilni prsten s 1-3 heteroatoma u prstenu, koje se neovisno bira između N, O i S i može biti supstituiran s jednim ili više neovisno biranih C1-C6 alkilnih supstituenata; (h) (C3-C6 cikloalkil)C1-C3 alkil-, gdje navedeni cikloalkil može biti supstituiran s OH, (i) (hetCyca)C1-C3 alkil-, (j) hetCyca-; (k) C3-C6 cikloalkil-, gdje navedeni cikloalkil može biti supstituiran s OH, (l) (C1-C4 alkil)C(=O)O-C1-C6 alkil-, gdje svaki od C1-C4 alkilnog i C1-C6 alkilnog dijela može biti i neovisno supstituiran s 1-3 fluora, ili (m) (R1R2N)C(=O)C1-C6 alkil-, gdje su R1 i R2 neovisno H ili C1-C6 alkil (koji može biti supstituiran s 1-3 fluora); hetCyca- je 4-6-eročlani heterociklički prsten s 1-2 heteroatoma u prstenu, koje se neovisno bira između N i O, koji može biti supstituiran s jednim ili više supstituenata, koje se neovisno bira između OH, C1-C6 alkil (koji može biti supstituiran s 1-3 fluora), hidroksiC1-C6 alkil-, C1-C6 alkoksi, (C1-C6 alkil)C(=O)-, (C1-C6 alkoksi)C1-C6 alkil- i fluora, ili, gdje je hetCyca supstituiran s okso; Prsten D je (i) zasićeni 4-7-eročlani heterociklički prsten s dva atoma dušika u prstenu, (ii) zasićeni 7-9-eročlani premošteni heterociklički prsten s dva atoma dušika u prstenu, koji može imati treći heteroatom u prstenu koji je kisik, (iii) zasićeni 7-11-eročlani heterospirociklički prsten s dva atoma dušika u prstenu, ili (iv) zasićeni 9-10-eročlani biciklički kondenzirani heterociklički prsten s dva atoma dušika u prstenu, gdje svaki od navedenih prstena može biti supstituiran s (a) jednom do četiri skupine, koje se neovisno bira između halogena, OH, C1-C3 alkila, koji može biti supstituiran s 1-3 fluora, ili C1-C3 alkoksi, koji može biti supstituiran s 1-3 fluora, (b) C3-C6 cikloalkilidenskim prstenom, ili (c) okso skupinom; E je (a) vodik, (b) C1-C6 alkil, koji može biti supstituiran s 1-3 fluora, (c) (C1-C6 alkoksi)C1-C6 alkil-, koji može biti supstituiran s 1-3 fluora, (d) (C1-C6 alkil)C(=O)-, gdje navedeni alkilni dio može biti supstituiran s 1-3 fluora ili s RgRhN-supstituent, gdje su Rg i Rh neovisno H ili C1-C6 alkil, (e) (hidroksiC2-C6 alkil)C(=O)-, koji može biti supstituiran s 1-3 fluora, (f) (C1-C6 alkoksi)C(=O)-, (g) (C3-C6 cikloalkil)C(=O)-, gdje navedeni cikloalkil može biti supstituiran s jednim ili više supstituenata, koje se neovisno bira između C1-C6 alkil, C1-C6 alkoksi, OH, te (C1-C6 alkoksi)C1-C6 alkil-, ili je navedeni cikloalkil supstituiran s 5-6-eročlanim heteroarilni prsten s 1-3 heteroatoma u prstenu, koje se neovisno bira između N i O, (h) Ar1C1-C6 alkil-, (i) Ar1(C1-C6 alkil)C(=O)-, gdje navedeni alkilni dio može biti supstituiran s OH, hidroksiC1-C6 alkil-, C1-C6 alkoksi, RmRnN- ili RmRnN-CH2-, gdje je svaki Rm i Rn neovisno H ili C1-C6 alkil, (j) hetAr2C1-C6 alkil-, gdje alkilni dio može biti supstituiran s 1-3 fluora, (k) hetAr2(C1-C6 alkil)C(=O)-, gdje navedeni alkilni dio može biti supstituiran s OH, hidroksiC1-C6 alkil- ili C1-C6 alkoksi, (l) hetAr2C(=O)-, (m) hetCyc1C(=O)-, (n) hetCyc1C1-C6 alkil-, (o) R3R4NC(=O)-, (p) Ar1N(R3)C(=O)-, (q) hetAr2N(R3)C(=O)-, (r) (C1-C6 alkil)SO2-, gdje alkilni dio može biti supstituiran s 1-3 fluora, (s) Ar1SO2-, (t) hetAr2SO2-, (u) N-(C1-C6 alkil)piridinonil, (v) Ar1C(=O)-, (w) Ar1O-C(=O)-, (x) (C3-C6 cikloalkil)(C1-C6 alkil)C(=O)-, (y) (C3-C6 cikloalkil)(C1-C6 alkil)SO2-, gdje alkilni dio može biti supstituiran s 1-3 fluora, (z) Ar1(C1-C6 alkil)SO2-, (aa) hetCyc1-O-C(=O)-, (bb) hetCyc1CH2C(=O)-, (cc) hetAr2, ili (dd) C3-C6 cikloalkil; Ar1 je fenil, koji može biti supstituiran s jednim ili više supstituenata, koje se neovisno bira iz skupine koju čine halogen, CN, C1-C6 alkil (koji može biti supstituiran s 1-3 fluora), C1-C6 alkoksi (koji može biti supstituiran s 1-3 fluora), ReRfN-, gdje su Re i Rf neovisno H ili C1-C6 alkil, (RpRqN)C1-C6 alkoksi-, gdje su Rp i Rq neovisno H ili C1-C6 alkil, te (hetAra)C1-C6 alkil-, gdje je hetAra 5-6-eročlani heteroarilni prsten s 1-2 atoma dušika u prstenu, ili je Ar1 fenilni prsten kondenziran s 5-6-eročlanim heterocikličkim prstenom s 1-2 heteroatoma u prstenu, koje se neovisno bira između N i O; hetAr2 je 5-6-eročlani heteroarilni prsten s 1-3 heteroatoma u prstenu, koje se neovisno bira između N, O i S, ili 9-10-eročlani biciklički heteroarilni prsten s 1-3 atoma dušika u prstenu, gdje hetAr2 može biti supstituiran s jednim ili više supstituenata, koje se neovisno bira iz skupine koju čine halogen, CN, C1-C6 alkil (koji može biti supstituiran s 1-3 fluora), C1-C6 alkoksi (koji može biti supstituiran s 1-3 fluora), (C1-C6 alkoksi)C1-C6 alkil-(koji može biti supstituiran s 1-3 fluora), ReRfN-, gdje su Re i Rf neovisno H ili C1-C6 alkil, OH, (C1-C6 alkoksi)C1-C6 alkoksi- i C3-C6 cikloalkil; hetCyc1 je 4-6-eročlani zasićeni heterociklički prsten s 1-2 heteroatoma u prstenu, koje se neovisno bira između N, O i S, gdje navedeni heterociklički prsten može biti supstituiran s jednim ili više supstituenata, koje se neovisno bira između C1-C6 alkoksi i halogena; R3 je H ili C1-C6 alkil; i R4 je C1-C6 alkil.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je Prsten D zasićeni 7-8-eročlani premošteni heterociklički prsten s dva atoma dušika u prstenu, koji može imati treći heteroatom u prstenu koji je kisik, gdje navedeni prsten može biti supstituiran s (a) jednom do četiri skupine, koje se neovisno bira između halogena, OH, C1-C3 alkila, koji može biti supstituiran s 1-3 fluora, ili C1-C3 alkoksi, koji može biti supstituiran s 1-3 fluora, (b) C3-C6 cikloalkilidenskim prstenom, ili (c) okso skupinom.
3. Spoj u skladu s patentnim zahtjevom 2, naznačen time što je Prsten D [image] gdje valovita linija označuje mjesto vezanja Prstena D na prsten koji sadrži X1, X2, X3 i X4, a zvjezdica označuje mjesto vezanja na E.
4. Spoj u skladu s patentnim zahtjevom 3, naznačen time što je Prsten D [image] .
5. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-4, naznačen time što je B hidroksiC2-C6 alkil-, gdje alkilni dio može biti supstituiran s C3-C6 cikloalkilidenskim prstenom.
6. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-4, naznačen time što je B (hetCyca)C1-C3 alkil-.
7. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-6, naznačen time što je X1 N, a X2, X3 i X4 su CH.
8. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-7, naznačen time što je A CN.
9. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je [image] , ili njegova farmaceutski prihvatljiva sol.
10. Spoj u skladu s patentnim zahtjevom 9, naznačen time što je [image] .
11. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je [image] , ili njegova farmaceutski prihvatljiva sol.
12. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je ili njegova farmaceutski prihvatljiva sol.
13. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je [image] , ili njegova farmaceutski prihvatljiva sol.
14. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je [image] , ili njegova farmaceutski prihvatljiva sol.
15. Farmaceutski pripravak, naznačen time što sadrži spoj, ili njegovu farmaceutski prihvatljivu sol, u skladu s bilo kojim od patentnih zahtjeva 1-14, u smjesi s farmaceutski prihvatljivim razrjeđivačem ili nosačem.
16. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s bilo kojim od patentnih zahtjeva 1-14, naznačen time što je namijenjen upotrebi u liječenju raka.
17. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 16, naznačen time što je rak rak povezan s RET.
18. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 17, naznačen time što je rak povezan s RET rak s disreguliranim RET genom, proteinom RET-kinaze ili ekspresijom ili aktivnošću ili razinom bilo kojeg od navedenog.
19. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 17-18, naznačen time što rak povezan s RET se bira iz skupine koju čine: rak pluća, papilarni rak štitnjače, rak jezgre štitnjače, diferencirani rak štitnjače, recidivirajući rak štitnjače, rezistentan diferencirani rak štitnjače, multiple endokrine novotvorine tipa 2A ili 2B (MEN2A odnosno MEN2B), feokromocitom, hiperplazija nusštitnjače, rak dojke, kolorektalni rak, karcinom papilarnih bubrežnih stanica, ganglioneuromatoza želučanocrijevne sluznice, te rak vrata maternice.
20. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 19, naznačen time što je rak pluća RET-fuzijski rak pluća, ili je rak rak jezgre štitnjače.
21. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s patentnim zahtjevom 19, naznačen time što je rak pluća karcinom malih stanica pluća, rak velikih stanica pluća, karcinom stanica bronhiola pluća ili adenokarcinom pluća.
22. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 16-21, naznačen time što je formuliran za oralnu primjenu.
HRP20201008TT 2016-10-10 2020-06-25 SUPSTITUIRANI SPOJEVI PIRAZOLO[1,5-a]PIRIDINA KAO INHIBITORI RET-KINAZE HRP20201008T1 (hr)

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US201662406252P 2016-10-10 2016-10-10
US201762447850P 2017-01-18 2017-01-18
US201762491164P 2017-04-27 2017-04-27
US201762554817P 2017-09-06 2017-09-06
US201762566093P 2017-09-29 2017-09-29
PCT/US2017/055983 WO2018071447A1 (en) 2016-10-10 2017-10-10 Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
EP17787843.6A EP3523301B1 (en) 2016-10-10 2017-10-10 Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors

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