HRP20231681T1 - Inhibitori za ret - Google Patents
Inhibitori za ret Download PDFInfo
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- HRP20231681T1 HRP20231681T1 HRP20231681TT HRP20231681T HRP20231681T1 HR P20231681 T1 HRP20231681 T1 HR P20231681T1 HR P20231681T T HRP20231681T T HR P20231681TT HR P20231681 T HRP20231681 T HR P20231681T HR P20231681 T1 HRP20231681 T1 HR P20231681T1
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- Croatia
- Prior art keywords
- hydrogen
- pharmaceutically acceptable
- alkyl
- acceptable salt
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- 239000003112 inhibitor Substances 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 27
- 239000001257 hydrogen Substances 0.000 claims 27
- 150000001875 compounds Chemical class 0.000 claims 24
- 150000003839 salts Chemical class 0.000 claims 20
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 13
- 239000000825 pharmaceutical preparation Substances 0.000 claims 13
- 238000000034 method Methods 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 150000002367 halogens Chemical class 0.000 claims 11
- 150000002431 hydrogen Chemical class 0.000 claims 11
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 9
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 7
- 125000004404 heteroalkyl group Chemical group 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- -1 heteroalkylalkyl Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010033701 Papillary thyroid cancer Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000004927 fusion Effects 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 206010051747 multiple endocrine neoplasia Diseases 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 125000004353 pyrazol-1-yl group Chemical group [H]C1=NN(*)C([H])=C1[H] 0.000 claims 1
- 125000004001 thioalkyl group Chemical group 0.000 claims 1
- 150000003573 thiols Chemical class 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 208000030045 thyroid gland papillary carcinoma Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero 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
- A61K31/435—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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- 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
- C07D239/30—Halogen atoms or nitro radicals
-
- C—CHEMISTRY; METALLURGY
- 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
- C07D239/34—One oxygen atom
-
- C—CHEMISTRY; METALLURGY
- 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
- C07D239/34—One oxygen atom
- C07D239/36—One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
-
- C—CHEMISTRY; METALLURGY
- 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
- C07D239/38—One sulfur atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Claims (15)
1. Spoj, naznačen time, da ima Formulu (A):
[image]
ili njegova farmaceutski prihvatljiva sol, u kojoj:
prsten A je 6-člani monociklički heteroaril koji sadrži najmanje jedan dušikov atom u prstenu;
svaki od X1 i X2 se neovisno bira od N i C(R6);
svaki od Y1 i Y2 se neovisno bira od -CH2- i -O-, pri čemu samo jedan od Y1 ili Y2 jest -O-;
svaki R1 se neovisno bira od sljedećih: C1-C6alkil, C2-C6alkenil, C2-C6alkinil, C1-C6alkoksi, halogen, C1-C6 heteroalkil, cikloalkil, aril, heteroaril, ariloksi, aralkil, heterociklil, heterociklilalkil, nitro, cijano, -C(O)R, -OC(O)R, -C(O)OR, -(C1-C6alkilen)-C(O)R, -SR, -S(O)2R, -S(O)2-N(R)(R), -(C1-C6alkilen)-S(O)2R, -(C1-C6alkilen)-S(O)2-N(R)(R), -N(R)(R), -C(O)-N(R)(R), -N(R)-C(O)R, -N(R)-C(O)OR, -(C1-C6alkilen)-N(R)-C(O)R, -N(R)-S(O)2R, i -P(O)(R)(R), gdje je svaki alkil, alkenil, alkinil, alkoksi, heteroalkil, cikloalkil, aril, heteroaril, ariloksi, aralkil, heterociklil, i heterociklilalkil neovisno supstituiran s 0-5 pojavljivanja od Ra,
ili se dva R1 uzimaju zajedno s atomima ugljika s kojima su vezani, za tvorbu cikloalkilnog ili heterociklilnog prstena neovisno supstituiranog s 0-5 pojavljivanja od Rb;
R7 je pirazol-1-il supstituiran s 0-3 pojavljivanja od Rb;
svaki od R2, R3a, R3b, R4, R8a i R8b se neovisno bira od sljedećih: vodik, C1-C6alkil, C1-C6alkoksi, halogen, hidroksil, C1-C6heteroalkil, i -N(R)(R), gdje je svaki alkil, alkoksi, i heteroalkil neovisno supstituiran s 0-5 pojavljivanja od Ra;
svaki od R5 i R9 se neovisno bira od sljedećih: vodik, C1-C6alkil, i C1-C6heteroalkil, gdje je svaki alkil i heteroalkil neovisno supstituiran s 0-5 pojavljivanja od Ra;
svaki R6 se neovisno bira od sljedećih: vodik, C1-C6alkil, C1-C6alkoksi, halogen, C1-C6heteroalkil, i -N(R)(R), gdje je svaki alkil, alkoksi, i heteroalkil neovisno supstituiran s 0-5 pojavljivanja od Ra;
svaki R se neovisno bira od sljedećih: vodik, hidroksil, halogen, tiol, C1-C6alkil, C1-C6tioalkil, C1-C6alkoksi, C1-C6heteroalkil, cikloalkil, cikloalkilalkil, heteroalkilalkil, heterociklil, i heterociklilalkil, gdje je svaki alkil, tioalkil, alkoksi, heteroalkil, cikloalkil, cikloalkilalkil, heteroalkilalkil, heterociklil, i heterociklilalkil neovisno supstituiran s 0-5 pojavljivanja od Ra, ili
dva R zajedno s atomom/atomima s kojim/a su vezani, tvore cikloalkilni ili heterociklilni prsten neovisno supstituiran s 0-5 pojavljivanja od Rb;
svaki Ra i svaki Rb se neovisno bira od sljedećih: C1-C6alkil, halogen, hidroksil, C1-C6heteroalkil, C1-C6alkoksi, cikloalkil, heterociklil, i cijano, gdje je svaki alkil, heteroalkil, alkoksi, cikloalkil, i heterociklil neovisno supstituiran s 0-5 pojavljivanja od R';
svaki R' se neovisno bira od sljedećih: C1-C6alkil, C1-C6heteroalkil, halogen, hidroksil, cikloalkil, i cijano, ili
dva R' zajedno s atomom/atomima s kojim/a su vezani, tvore cikloalkilni ili heterociklilni prsten;
___
- - - predstavlja jednostruku ili dvostruku vezu;
m je 0, 1 ili 2;
n je 1;
svaki o je 0 kada je
___
- - - dvostruka veza; i
svaki o je 1 kada je
___
- - - jednostruka veza.
2. Spoj prema patentnom zahtjevu 1, naznačen time, da ima formulu (I):
[image]
ili njegova farmaceutski prihvatljiva sol, u kojoj:
___
- - - predstavlja jednostruku ili dvostruku vezu; i
svaki od prstena A, X1, X2, R1, R2, R3a, R3b, R4, R5, R6, R7, R8a, R8b, R9, R, Ra, Rb, R’, m, n, i o jest kao što je definiran u patentnom zahtjevu 1.
3. Spoj prema patentnom zahtjevu 1 ili 2, ili njegova farmaceutski prihvatljiva sol, naznačen time, da:
m je 1, R1 se nalazi na poziciji 5, i R1 je C1-C4alkil supstituiran s 0-3 pojavljivanja od Ra; i/ili
R2 se bira od vodika, hidroksila, halogena, i C1-C4alkoksi; i/ili
svaki od R3a, R3b, R8a, i R8b se neovisno bira od vodika i C1-C4alkila koji je supstituiran s 0-3 pojavljivanja od Ra (i/ili gdje je najmanje jedan par od R3a i R3b, ili R8a i R8b, istovremeno vodik);
i/ili
R4 se bira od sljedećih: vodik, C1-C4alkil, i C1-C4alkoksi; pri čemu je svaki alkilni dio od R4 supstituiran s 0-3 pojavljivanja od Ra; i/ili
R5 se neovisno bira od vodika i C1-C4alkila koji je supstituiran s 0-3 pojavljivanja od Ra; i/ili
svaki R6 se neovisno bira od vodika, halogena, i C1-C4alkila koji je supstituiran s 0-3 pojavljivanja od Ra; i/ili
prsten A se bira od
[image]
i
[image]
i/ili
R9 je vodik.
4. Spoj, naznačen time, da ima formulu (II):
[image]
ili njegova farmaceutski prihvatljiva sol, u kojoj:
X1 se bira od N, CH, i C(halogena);
X2 se bira od N i CH;
X3 se bira od N i CH;
R12 se bira od vodika, hidroksila, halogena, i C1-C4 alkoksi;
svaki od R13a, R13b, R18a, i R18b se neovisno bira od vodika i C1-C4 alkila;
R14 se bira od vodika, -C1-C4 alkila, i C1-C4 alkoksi;
R15 se bira od vodika i -C1-C4 alkila;
R16 se bira od vodika i -C1-C4 alkila;
R17b se bira od vodika i halogena; i
svaki od R17a, i R17c, se neovisno bira od vodika i -C1-C4 alkila.
5. Spoj prema patentnom zahtjevu 4, ili njegova farmaceutski prihvatljiva sol, naznačen time, da:
X1 se bira od N, CH, i C(Cl);
R12 se bira od vodika, hidroksila, fluora, i -O-CH3;
svaki od R13a, R13b, R18a, i R18b se neovisno bira od vodika, metila, i etila, pri čemu je najmanje jedan par od R13a i R13b, ili R18a i R18b, istovremeno vodik;
R14 se bira od vodika, -CH3, -CH2CH3, -OCH3, i -OCH2CH3;
R15 se bira od vodika i -CH3;
R16 se bira od vodika i -CH3;
R17b se bira od vodika, klora i fluora; i
R17a i R17c su istovremeno vodik ili -CH3, pri čemu kada su R17a i R17c istovremeno -CH3, tada R17b je vodik.
6. Spoj prema patentnom zahtjevu 1, naznačen time, da se spoj bira od sljedećih:
[image]
(nastavak)
[image]
(nastavak)
[image]
(nastavak)
[image]
(nastavak)
[image]
(nastavak)
[image]
(nastavak)
[image]
(nastavak)
[image]
(nastavak)
[image]
(nastavak)
[image]
(nastavak)
[image]
ili njegova farmaceutski prihvatljiva sol.
7. Spoj prema patentnom zahtjevu 6, naznačen time, da spoj ima strukturnu formulu:
[image]
ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema patentnom zahtjevu 6, naznačen time, da spoj ima sljedeću strukturu:
[image]
9. Farmaceutski pripravak, naznačen time, da sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 8, ili njegovu farmaceutski prihvatljivu sol; i farmaceutski prihvatljiv nosač.
10. Spoj prema bilo kojem od patentnih zahtjeva 1 do 8, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak prema patentnom zahtjevu 9, naznačen time, da je za uporabu u postupku za liječenje pojedinca koji boluje od raka pluća ne-malih stanica, pri čemu postupak obuhvaća davanje pojedincu terapeutski učinkovite količine navedenog spoja, navedene farmaceutski prihvatljive soli, ili navedenog farmaceutskog pripravka.
11. Spoj prema bilo kojem od patentnih zahtjeva 1 do 8, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak prema patentnom zahtjevu 9, naznačen time, da je za uporabu u postupku za liječenje pojedinca koji boluje od papilarnog raka tiroidne žlijezde, pri čemu postupak obuhvaća davanje pojedincu terapeutski učinkovite količine navedenog spoja, navedene farmaceutski prihvatljive soli, ili navedenog farmaceutskog pripravka.
12. Spoj prema bilo kojem od patentnih zahtjeva 1 do 8, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak prema patentnom zahtjevu 9, naznačen time, da je za uporabu u postupku za liječenje pojedinca koji boluje od medularnog raka tiroidne žlijezde, pri čemu postupak obuhvaća davanje pojedincu terapeutski učinkovite količine navedenog spoja, navedene farmaceutski prihvatljive soli, ili navedenog farmaceutskog pripravka.
13. Spoj prema bilo kojem od patentnih zahtjeva 1 do 8, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak prema patentnom zahtjevu 9, naznačen time, da je za uporabu u postupku za liječenje pojedinca koji boluje od kolorektalnog raka, pri čemu postupak obuhvaća davanje pojedincu terapeutski učinkovite količine navedenog spoja, navedene farmaceutski prihvatljive soli, ili navedenog farmaceutskog pripravka.
14. Spoj prema bilo kojem od patentnih zahtjeva 1 do 8, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak prema patentnom zahtjevu 9, naznačen time, da je za uporabu u postupku za liječenje pojedinca koji boluje od multiple endokrine neoplazije, pri čemu postupak obuhvaća davanje pojedincu terapeutski učinkovite količine navedenog spoja, navedene farmaceutski prihvatljive soli, ili navedenog farmaceutskog pripravka.
15. Spoj prema bilo kojem od patentnih zahtjeva 1 do 8, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak prema patentnom zahtjevu 9, naznačen time, da je za uporabu u postupku za liječenje raka koji je posredovan s RET fuzijom ili RET mutacijom kod pojedinca kojemu je to potrebno, pri čemu postupak obuhvaća davanje pojedincu terapeutski učinkovite količine navedenog spoja, navedene farmaceutski prihvatljive soli, ili navedenog farmaceutskog pripravka.
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| PCT/US2016/059879 WO2017079140A1 (en) | 2015-11-02 | 2016-11-01 | Inhibitors of ret |
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