HRP20221154T1 - Supstituirani pirazolo[1,5-a]piridinski spojevi kao inhibitori ret kinaze - Google Patents
Supstituirani pirazolo[1,5-a]piridinski spojevi kao inhibitori ret kinaze Download PDFInfo
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- HRP20221154T1 HRP20221154T1 HRP20221154TT HRP20221154T HRP20221154T1 HR P20221154 T1 HRP20221154 T1 HR P20221154T1 HR P20221154T T HRP20221154T T HR P20221154TT HR P20221154 T HRP20221154 T HR P20221154T HR P20221154 T1 HRP20221154 T1 HR P20221154T1
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- Croatia
- Prior art keywords
- alkyl
- substituted
- ring
- cancer
- independently selected
- Prior art date
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- 101150077555 Ret gene Proteins 0.000 title claims 3
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- DVUBDHRTVYLIPA-UHFFFAOYSA-N pyrazolo[1,5-a]pyridine Chemical class C1=CC=CN2N=CC=C21 DVUBDHRTVYLIPA-UHFFFAOYSA-N 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 16
- 235000019000 fluorine Nutrition 0.000 claims 16
- 125000001153 fluoro group Chemical group F* 0.000 claims 10
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 7
- 101000579425 Homo sapiens Proto-oncogene tyrosine-protein kinase receptor Ret Proteins 0.000 claims 6
- 102100028286 Proto-oncogene tyrosine-protein kinase receptor Ret Human genes 0.000 claims 6
- 229910052731 fluorine Inorganic materials 0.000 claims 6
- 239000011737 fluorine Substances 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000006876 Multiple Endocrine Neoplasia Type 2b Diseases 0.000 claims 2
- 206010073148 Multiple endocrine neoplasia type 2A Diseases 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 125000006519 CCH3 Chemical group 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000009018 Medullary thyroid cancer Diseases 0.000 claims 1
- 206010033701 Papillary thyroid cancer Diseases 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 208000015799 differentiated thyroid carcinoma Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000008482 dysregulation Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000002496 gastric effect Effects 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000023356 medullary thyroid gland carcinoma Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 210000004877 mucosa Anatomy 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 201000010279 papillary renal cell carcinoma Diseases 0.000 claims 1
- 208000025061 parathyroid hyperplasia Diseases 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 208000028591 pheochromocytoma Diseases 0.000 claims 1
- 230000000306 recurrent effect Effects 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 208000030045 thyroid gland papillary carcinoma Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4162—1,2-Diazoles condensed with heterocyclic 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
- A61K31/435—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
- A61K31/435—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
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines 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
- A61K31/495—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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines 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
- A61K31/495—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
- 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
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Claims (16)
1. Spoj Formule I:
[image]
,
i njegove farmaceutski prihvatljive soli, naznačen time što:
X1, X2, X3 i X4 su neovisno CH, CCH3, CF ili N, gdje su nula, jedan ili dva od X1, X2, X3 i X4 N;
A je H, CN, Cl, metil, etil ili ciklopropil;
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 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 se R1 i R2 neovisno bira između H, C1-C6 alkila (koji može biti supstituiran s 1-3 fluora), (C1-C6 alkoksi)C1-C6 alkil- i (C1-C6 alkoksi)C(=O)-;
(g) hetAr1C1-C3 alkil-, gdje je hetAr1 5-6-eročlani heteroarilni prsten koji ima 1-3 heteroatoma u prstenu koje se neovisno bira između N, O i S i može biti supstituiran s jednim ili više neovisno odabranih C1-C6 alkilnih supstituenata;
(h) (C3-C6 cikloalkil)C1-C3 alkil-;
(i) (hetCyca)C1-C3 alkil-;
(j) hetCyca;
(k) (R1R2N)C(=O)C1-C6 alkil-, gdje se R1 i R2 neovisno bira između H i C1-C6 alkila;
(l) (R1R2N)C(=O)-, gdje se R1 i R2 neovisno bira između H i C1-C6 alkila; ili
(m) hetCycaC(=O)C1-C6 alkil-;
hetCyca je 4-6-eročlani heterociklički prsten koji ima 1-2 heteroatoma u prstenu koje se neovisno bira između N i O i može biti supstituiran s jednim ili više supstituenata koje se neovisno bira između OH, C1-C6 alkila (koji može biti supstituiran s 1-3 fluora), hidroksiC1-C6 alkila, halogena, (C1-C6 alkil)C(=O)-, C1-C6 alkoksi, okso, te (C1-C6 alkoksi)C(=O)-;
Prsten D je
(i) zasićeni monociklički 4-7-eročlani heterociklički prsten koji ima jedan heteroatom u prstenu koji je dušik;
svaki Ra je neovisno C1-C6 alkil (koji može biti supstituiran s 1-3 fluora), hidroksiC1-C6 alkil ili (C1-C6 alkoksi)C1-C6 alkil-;
Rb je (a) hidroksi;
(c) hetCycbCH2-, gdje je hetCycb 4-6-eročlani heterociklički prsten koji ima 1-2 heteroatoma u prstenu koje se neovisno bira između N i O, te gdje hetCycb može biti supstituiran s C1-C6 alkilom (izborno supstituiranim s 1-3 fluora);
(e) RcRdN-; ili
(f) RcRdNCH2-;
Rc je vodik ili C1-C6 alkil; i
Rd je vodik ili C1-C6 alkil (koji može biti supstituiran s 1-3 fluora);
n je 0, ili 1;
m je 0 ili 1;
E je:
(d) Ar1C1-C6 alkil-, gdje navedeni alkilni dio može biti supstituiran s 1-3 fluora;
(e) hetAr2C1-C6 alkil-;
(g) Ar1O-;
(h) hetAr2O-;
(l) Ar1C(=O)NRg-, gdje je Rg H ili C1-C6 alkil; ili
(m) hetAr2C(=O)NRg(CH2)p-, gdje je p 0 ili 1;
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), (C1-C6 alkoksi)C1-C6 alkil- (koji može biti supstituiran s 1-3 fluora), C3-C6 cikloalkil, hidroksiC1-C6 alkil, (C1-C6 alkil)SO2-, ReRfN- i (ReRfN)C1-C6 alkil-, gdje je svaki Re i Rf neovisno H ili C1-C6 alkil;
hetAr2 je 5-6-eročlani heteroarilni prsten koji ima 1-3 heteroatoma u prstenu koje se neovisno bira između N, O i S, ili 9-10-eročlani biciklički heteroaril koji ima 1-2 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) i hidroksiC1-C6 alkoksi.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što svaki Ra je neovisno odabrana C1-C6 alkilna skupina.
3. Spoj u skladu s patentnim zahtjevom 2, naznačen time što je D
[image]
,
gdje valovita linija označuje mjesto vezanja Prstena D na prsten koji sadrži X1, X2, X3 i X4, a asterisk označuje mjesto vezanja Prstena D na skupinu E.
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je D
[image]
,
gdje valovita linija označuje mjesto vezanja Prstena D na prsten koji sadrži X1, X2, X3 i X4, a asterisk označuje mjesto vezanja na skupinu E.
5. Spoj u skladu s patentnim zahtjevom 4, naznačen time što je E (d) Ar1C1-C6 alkil-, gdje navedeni alkilni dio može biti supstituiran s 1-3 fluora, (e) hetAr2C1-C6 alkil-, (g) Ar1O-, (h) hetAr2O-, (1) Ar1C(=O)NRg-, gdje je Rg H ili C1-C6 alkil, ili (m) hetAr2C(=O)NRg(CH2)p-, gdje je p 0 ili 1.
6. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-5, naznačen time što B je C1-C6 alkil koji može biti supstituiran s 1-3 fluora.
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 1, naznačen time što je:
[image]
,
ili njegova farmaceutski prihvatljiva sol.
11. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1-10, ili njegova farmaceutski prihvatljiva sol, u smjesi s farmaceutski prihvatljivim razrjeđivačem ili nosačem.
12. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-10, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u liječenju raka.
13. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 12, naznačen time što rak je rak vezan uz RET.
14. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 13, naznačen time što je rak rak vezan uz RET koji ima disregulaciju u genu RET, proteina RET kinaze, ili ekspresije ili aktivnosti ili razine bilo kojeg od navedenog koje uzrokuje jedna ili više točkastih mutacija u genu RET.
15. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s bilo kojim patentnim zahtjevom 13 ili 14, naznačen time što se rak vezan uz RET bira iz skupine koju čine: rak pluća, papilarni rak štitnjače, medularni rak štitnjače, diferencirani rak štitnjače, recidivirajući rak štitnjače, refraktorni diferencirani rak štitnjače, multipla endokrina neoplazija tipa 2A ili 2B (MEN2A odnosno MEN2B), feokromocitom, hiperplazija nusštitnjače, rak dojke, kolorektalni rak, papilarni karcinom bubrežnih stanica, ganglioneuromatoza želučano-crijevne sluznice, te rak vrata maternice.
16. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 12-15, naznačen time što je medikament formuliran za oralnu primjenu.
Applications Claiming Priority (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201662406275P | 2016-10-10 | 2016-10-10 | |
US201762447849P | 2017-01-18 | 2017-01-18 | |
US201762491180P | 2017-04-27 | 2017-04-27 | |
US201762531690P | 2017-07-12 | 2017-07-12 | |
US201762566030P | 2017-09-29 | 2017-09-29 | |
PCT/US2017/055993 WO2018071454A1 (en) | 2016-10-10 | 2017-10-10 | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
EP17787844.4A EP3523302B1 (en) | 2016-10-10 | 2017-10-10 | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
Publications (1)
Publication Number | Publication Date |
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HRP20221154T1 true HRP20221154T1 (hr) | 2022-12-09 |
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