HRP20231681T1 - Inhibitori za ret - Google Patents
Inhibitori za ret Download PDFInfo
- Publication number
- 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
- Authority
- HR
- Croatia
- Prior art keywords
- hydrogen
- pharmaceutically acceptable
- alkyl
- acceptable salt
- image
- Prior art date
Links
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (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.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562249784P | 2015-11-02 | 2015-11-02 | |
US201662367960P | 2016-07-28 | 2016-07-28 | |
PCT/US2016/059879 WO2017079140A1 (en) | 2015-11-02 | 2016-11-01 | Inhibitors of ret |
EP16794885.0A EP3371171B1 (en) | 2015-11-02 | 2016-11-01 | Inhibitors of ret |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20231681T1 true HRP20231681T1 (hr) | 2024-04-12 |
Family
ID=57286889
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20231681TT HRP20231681T1 (hr) | 2015-11-02 | 2016-11-01 | Inhibitori za ret |
Country Status (31)
Country | Link |
---|---|
US (4) | US10030005B2 (hr) |
EP (3) | EP4292594A3 (hr) |
JP (3) | JP6807385B2 (hr) |
KR (1) | KR20180073689A (hr) |
CN (2) | CN108473468B (hr) |
AU (1) | AU2016348402B2 (hr) |
BR (1) | BR112018008877B1 (hr) |
CA (1) | CA3003721C (hr) |
CL (1) | CL2018001181A1 (hr) |
DK (1) | DK3371171T3 (hr) |
EA (1) | EA038890B1 (hr) |
ES (1) | ES2969185T3 (hr) |
FI (1) | FI3371171T3 (hr) |
HK (1) | HK1259287A1 (hr) |
HR (1) | HRP20231681T1 (hr) |
HU (1) | HUE064659T2 (hr) |
IL (3) | IL302209B2 (hr) |
LT (1) | LT3371171T (hr) |
MX (1) | MX2018005528A (hr) |
MY (1) | MY194262A (hr) |
NZ (1) | NZ742351A (hr) |
PH (1) | PH12018500907A1 (hr) |
PL (1) | PL3371171T3 (hr) |
PT (1) | PT3371171T (hr) |
RS (1) | RS65069B1 (hr) |
SA (1) | SA518391496B1 (hr) |
SG (1) | SG11201803653QA (hr) |
SI (1) | SI3371171T1 (hr) |
TW (2) | TWI757256B (hr) |
WO (1) | WO2017079140A1 (hr) |
ZA (1) | ZA201803050B (hr) |
Families Citing this family (61)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
MX2012013467A (es) | 2010-05-20 | 2013-04-29 | Array Biopharma Inc | Compuestos macrociclicos como inhibidores de trk cinasa. |
KR102163776B1 (ko) | 2012-07-11 | 2020-10-12 | 블루프린트 메디신즈 코포레이션 | 섬유아세포 성장인자 수용체의 저해제 |
EP2970231A1 (en) | 2013-03-15 | 2016-01-20 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
PT3057969T (pt) | 2013-10-17 | 2018-07-11 | Blueprint Medicines Corp | Composições úteis para tratar distúrbios relacionados com kit |
CN105658642B (zh) | 2013-10-25 | 2019-05-03 | 蓝图药品公司 | 纤维母细胞生长因子受体抑制剂 |
WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
US10202365B2 (en) | 2015-02-06 | 2019-02-12 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors |
CA2992586A1 (en) | 2015-07-16 | 2017-01-19 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
BR112018001190A2 (pt) | 2015-07-24 | 2018-09-11 | Blueprint Medicines Corp | composições úteis para tratar distúrbios relacionados a kit e pdfgr |
AU2016311426B2 (en) | 2015-08-26 | 2021-05-20 | Blueprint Medicines Corporation | Compounds and compositions useful for treating disorders related to NTRK |
TWI757256B (zh) | 2015-11-02 | 2022-03-11 | 美商纜圖藥品公司 | 轉染過程重排之抑制劑 |
AR106756A1 (es) | 2015-11-19 | 2018-02-14 | Blueprint Medicines Corp | Compuestos y composiciones útiles para el tratamiento de trastornos relacionados con ntrk |
TW201738228A (zh) | 2016-03-17 | 2017-11-01 | 藍圖醫藥公司 | Ret之抑制劑 |
PT3442977T (pt) | 2016-04-15 | 2023-10-04 | Blueprint Medicines Corp | Inibidores do recetor de activina de tipo quinase |
US20190142868A1 (en) | 2016-05-13 | 2019-05-16 | Instituto de Medicina Moleccular | Methods of treating diseases associated with ilc3 cells |
US10227329B2 (en) | 2016-07-22 | 2019-03-12 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
US10035789B2 (en) * | 2016-07-27 | 2018-07-31 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
US11168090B2 (en) | 2017-01-18 | 2021-11-09 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors |
JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
US11040979B2 (en) | 2017-03-31 | 2021-06-22 | Blueprint Medicines Corporation | Substituted pyrrolo[1,2-b]pyridazines for treating disorders related to KIT and PDGFR |
WO2018213329A1 (en) | 2017-05-15 | 2018-11-22 | Blueprint Medicines Corporation | Combinations of ret inhibitors and mtorc1 inhibitors and uses thereof for the treatment of cancer mediated by aberrant ret activity |
TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
TW202410896A (zh) | 2017-10-10 | 2024-03-16 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
WO2019079649A1 (en) | 2017-10-18 | 2019-04-25 | Blueprint Medicines Corporation | SUBSTITUTED PYRROLOPYRIDINES AS INHIBITORS OF ACTIVIN RECEPTOR-RELATED KINASE |
JP6997876B2 (ja) | 2018-01-18 | 2022-02-04 | アレイ バイオファーマ インコーポレイテッド | Retキナーゼ阻害剤としての置換ピラゾリル[4,3-c]ピリジン化合物 |
US11524963B2 (en) | 2018-01-18 | 2022-12-13 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidines as RET kinase inhibitors |
TWI802635B (zh) | 2018-01-18 | 2023-05-21 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡咯并[2,3-d]嘧啶化合物 |
JP7422084B2 (ja) | 2018-04-03 | 2024-01-25 | ブループリント メディシンズ コーポレイション | Ret変化を有する癌の処置において使用するためのret阻害剤 |
US20210308134A1 (en) | 2018-08-10 | 2021-10-07 | Blueprint Medicines Corporation | Treatment of egfr-mutant cancer |
CN112566907A (zh) * | 2018-08-17 | 2021-03-26 | 南京明德新药研发有限公司 | 作为ret抑制剂的吡唑衍生物 |
EP3849986B1 (en) | 2018-09-10 | 2022-06-08 | Array Biopharma, Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
CN111285875B (zh) * | 2018-12-06 | 2023-02-03 | 苏州信诺维医药科技股份有限公司 | 一种杂环化合物、其应用及含其的药物组合物 |
CN111285882B (zh) * | 2018-12-07 | 2022-12-02 | 四川科伦博泰生物医药股份有限公司 | 稠环化合物、包含其的药物组合物及其制备方法和用途 |
CN111484479B (zh) * | 2019-01-25 | 2023-06-13 | 四川科伦博泰生物医药股份有限公司 | 氮杂环化合物、包含其的药物组合物及其制备方法和用途 |
CN111499613B (zh) * | 2019-01-31 | 2023-05-12 | 浙江海正药业股份有限公司 | N-甲酰胺衍生物、其制备方法及其在医药上的用途 |
CN117327078A (zh) | 2019-02-19 | 2024-01-02 | 四川科伦博泰生物医药股份有限公司 | 杂环化合物、包含其的药物组合物及其制备方法和用途 |
JP7198386B2 (ja) * | 2019-04-03 | 2022-12-28 | 広州白雲山医薬集団股分有限公司白雲山制薬総廠 | Ret阻害剤としての窒素含有スピロ環誘導体 |
JP2022526438A (ja) | 2019-04-12 | 2022-05-24 | ブループリント メディシンズ コーポレイション | (s)-1-(4-フルオロフェニル)-1-(2-(4-(6-(1-メチル-1h-ピラゾール-4-イル)ピロロ[2,1-f][1、2,4]トリアジン-4-イル)ピペラジニル)-ピリミジン-5-イル)エタン-1-アミンの結晶形態及び製造方法 |
CN111808077B (zh) * | 2019-04-12 | 2023-05-02 | 浙江海正药业股份有限公司 | 哌嗪酰胺衍生物,其制备方法及其在医药上的用途 |
CN111961034A (zh) * | 2019-05-20 | 2020-11-20 | 浙江同源康医药股份有限公司 | 用作ret激酶抑制剂的化合物及其应用 |
US11666570B2 (en) * | 2019-07-11 | 2023-06-06 | The Board Of Trustees Of The Leland Stanford Junior University | Diagnosis and regulation of epidermal differentiation and cancer cell activity |
CN113121524B (zh) | 2019-12-31 | 2023-04-25 | 南京创济生物医药有限公司 | 杂环亚砜亚胺化合物及其中间体、制备方法和应用 |
CN113135896A (zh) * | 2020-01-18 | 2021-07-20 | 正大天晴药业集团股份有限公司 | 作为ret抑制剂的甲基吡唑类衍生物 |
CN111362923A (zh) * | 2020-03-25 | 2020-07-03 | 魏威 | 制备ret抑制剂普拉塞替尼的方法、以及普拉塞替尼的中间体及其制备方法 |
CN111440151A (zh) * | 2020-03-25 | 2020-07-24 | 魏威 | 制备抗肿瘤药普拉赛替尼的方法 |
CN111269229B (zh) * | 2020-03-27 | 2021-02-12 | 苏州信诺维医药科技有限公司 | 一种治疗癌症的化合物 |
CA3179612A1 (en) * | 2020-05-20 | 2021-11-25 | Tyk Medicines, Inc. | Compound used as ret kinase inhibitor and application thereof |
JP2023527412A (ja) | 2020-05-29 | 2023-06-28 | ブループリント メディシンズ コーポレイション | プラルセチニブの固体形態 |
MX2022015022A (es) * | 2020-05-29 | 2023-03-08 | Blueprint Medicines Corp | Composiciones farmaceuticas de pralsetinib. |
CN111777595A (zh) * | 2020-07-22 | 2020-10-16 | 上海希迈医药科技有限公司 | 一种环己烷甲酰胺类化合物的新晶型及其制备方法 |
US20230391746A1 (en) | 2020-10-19 | 2023-12-07 | Teva Pharmaceuticals International Gmbh | Solid state forms of pralsetinib and process for preparation thereof |
WO2022117448A1 (en) | 2020-12-03 | 2022-06-09 | Sandoz Ag | Crystalline forms of pralsetinib |
US20240059672A1 (en) | 2020-12-04 | 2024-02-22 | Blueprint Medicines Corporation | Method of preparing pralsetinib |
CN113072541B (zh) * | 2021-04-02 | 2022-07-08 | 山东四环药业股份有限公司 | 一种靶向药物blu-667的制备方法 |
EP4347645A1 (en) | 2021-06-03 | 2024-04-10 | Fundação D. Anna de Sommer Champalimaud e Dr. Carlos Montez Champalimaud Foundation | Neuro-mesenchyme units control ilc2 and obesity via a brain-adipose circuit |
TW202345806A (zh) | 2022-03-31 | 2023-12-01 | 美商艾伯維有限公司 | 噻唑并〔5,4-b〕吡啶malt-1抑制劑 |
CN115057822B (zh) * | 2022-07-14 | 2023-05-02 | 上海优合贝德医药科技有限公司 | 一种普拉替尼中间体2097133-31-6的新合成方法 |
CN117466901A (zh) * | 2022-07-23 | 2024-01-30 | 浙江海正药业股份有限公司 | 哌嗪酰胺衍生物的晶型及其制备方法和用途 |
Family Cites Families (84)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU3704101A (en) | 2000-02-17 | 2001-08-27 | Amgen Inc | Kinase inhibitors |
BR0312873A (pt) * | 2002-07-24 | 2005-06-28 | Univ Cincinnati | 4-(4-metilpiperazin-1-ilmetil)-n-[4-metil-3-(4-piridin-3-il) pirimidin-2-ilamino)fenil] benzamida para tratamento de doenças associadas com ret cinase mutante |
ES2527118T3 (es) | 2003-12-19 | 2015-01-20 | Plexxikon Inc. | Compuestos y procedimientos de desarrollo de moduladores de Ret |
US8227455B2 (en) * | 2005-04-18 | 2012-07-24 | Rigel Pharmaceuticals, Inc. | Methods of treating cell proliferative disorders |
WO2006128042A2 (en) | 2005-05-26 | 2006-11-30 | The Johns Hopkins University | Methods of identifying mutations in nucleic acid |
WO2007023382A2 (en) | 2005-08-25 | 2007-03-01 | Pfizer Inc. | Pyrimidine amino pyrazole compounds, potent kinase inhibitors |
EP1978958A4 (en) | 2006-01-24 | 2009-12-02 | Merck & Co Inc | INHIBITION OF TYROSINE KINASE RET |
US20090048214A1 (en) * | 2006-11-15 | 2009-02-19 | Rigel Pharmaceuticals, Inc | Methods for Treating Renal Tumors Using 2, 4-Pyrimidinediamine Drug and Prodrug Compounds |
WO2009003136A1 (en) * | 2007-06-26 | 2008-12-31 | Rigel Pharmaceuticals, Inc. | Substituted pyrimidine-2, 4 -diamines for treating cell proliferative disorders |
BRPI0814818A2 (pt) | 2007-07-09 | 2019-09-10 | Astrazeneca Ab | composto, uso de um composto, métodos para produzir um efeito anti-proliferativo e um efeito inibitório de mtor quinase em uma animal de sangue quente, método para tratar doenças, e, composição farmacêutica |
MY150032A (en) | 2007-07-19 | 2013-11-29 | Merck Sharp & Dohme | Heterocyclic amide compounds as protein kinase inhibitors |
JP5553751B2 (ja) * | 2007-07-31 | 2014-07-16 | バーテックス ファーマシューティカルズ インコーポレイテッド | 5−フルオロ−1H−ピラゾロ[3,4−b]ピリジン−3−アミンおよびその誘導体を調製するためのプロセス |
WO2009100536A1 (en) | 2008-02-15 | 2009-08-20 | Methylgene Inc. | Inhibitors of kinase activity with 1,2-di-cyclyl substituted alkyne structures |
EP2313091A4 (en) | 2008-07-14 | 2012-04-04 | Univ Kingston | PHARMACEUTICAL COMPOSITIONS WITH RET-HEMMERN AND METHOD FOR THE TREATMENT OF CANCER |
AU2010229140A1 (en) | 2009-03-24 | 2011-11-10 | Msd K.K. | Novel aminopyridine derivatives having Aurora A selective inhibitory action |
KR20120026612A (ko) | 2009-06-09 | 2012-03-19 | 아브락시스 바이오사이언스, 엘엘씨 | 벤질 치환 트리아진 유도체와 이들의 치료적 용도 |
EA201290255A1 (ru) | 2009-10-30 | 2013-04-30 | Ариад Фармасьютикалз, Инк. | Способы и композиции для лечения рака |
MY160820A (en) | 2009-11-13 | 2017-03-31 | Genosco | Kinase inhibitors |
IN2014DN01605A (hr) | 2011-08-04 | 2015-05-15 | Nat Cancer Ct | |
WO2013028817A1 (en) | 2011-08-23 | 2013-02-28 | Foundation Medicine , Inc. | Novel kif5b-ret fusion molecules and uses thereof |
WO2013077921A2 (en) | 2011-09-02 | 2013-05-30 | The Regents Of The University Of California | Substituted pyrazolo[3,4-d]pyrimidines and uses thereof |
US20130096136A1 (en) | 2011-09-30 | 2013-04-18 | Methylgene Inc. | Inhibitors of Protein Tyrosine Kinase Activity |
US10023855B2 (en) | 2011-10-31 | 2018-07-17 | Macrogen, Inc. | Fusion protein comprising C-terminal domain of RET protein and use thereof as a diagnosing marker |
EP2776420A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
JP2015109806A (ja) | 2012-03-22 | 2015-06-18 | アステラス製薬株式会社 | 新規ret融合体の検出法 |
RU2646754C2 (ru) * | 2012-04-25 | 2018-03-07 | Раквалиа Фарма Инк. | Производные пирролопиридинона в качестве ttx-s блокаторов |
US20150099721A1 (en) | 2012-05-10 | 2015-04-09 | Synta Pharmaceuticals Corp. | Treating cancer with hsp90 inhibitory compounds |
KR102163776B1 (ko) | 2012-07-11 | 2020-10-12 | 블루프린트 메디신즈 코포레이션 | 섬유아세포 성장인자 수용체의 저해제 |
JPWO2014017491A1 (ja) | 2012-07-26 | 2016-07-11 | 国立研究開発法人国立がん研究センター | Cep55遺伝子とret遺伝子との融合遺伝子 |
JP6513567B2 (ja) | 2012-09-07 | 2019-05-15 | エクセリクシス, インク. | 肺腺癌の治療で使用するためのmet、vegfr、およびretの阻害剤 |
CN111388478A (zh) * | 2012-09-25 | 2020-07-10 | 中外制药株式会社 | Ret抑制剂 |
ES2755772T3 (es) | 2012-11-07 | 2020-04-23 | Nerviano Medical Sciences Srl | Pirimidinil y piridinilpirrolopiridinonas sustituidas, proceso para su preparación y su uso como inhibidores de cinasas |
TWI629266B (zh) | 2012-12-28 | 2018-07-11 | 藍印藥品公司 | 纖維母細胞生長因子受體之抑制劑 |
EA027861B1 (ru) | 2013-02-25 | 2017-09-29 | Бристол-Майерс Сквибб Компани | C-3 алкил- и алкенилмодифицированные производные бетулиновой кислоты или их фармацевтические соли, противовирусная фармацевтическая композиция и фармацевтическая композиция для лечения вич на их основе |
EP2970231A1 (en) | 2013-03-15 | 2016-01-20 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
NZ628388A (en) * | 2013-03-15 | 2016-09-30 | Glaxosmithkline Ip Dev Ltd | Pyridine derivatives as rearranged during transfection (ret) kinase inhibitors |
WO2015006875A1 (en) | 2013-07-18 | 2015-01-22 | Methylgene Inc. | Process for the preparation of substituted pyrimidines |
TW201542825A (zh) | 2013-08-20 | 2015-11-16 | Nat Cancer Ct | 在肺癌辨識出的新穎融合基因 |
WO2015058129A1 (en) | 2013-10-17 | 2015-04-23 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
PT3057969T (pt) | 2013-10-17 | 2018-07-11 | Blueprint Medicines Corp | Composições úteis para tratar distúrbios relacionados com kit |
CN105658642B (zh) | 2013-10-25 | 2019-05-03 | 蓝图药品公司 | 纤维母细胞生长因子受体抑制剂 |
GB201321146D0 (en) | 2013-11-29 | 2014-01-15 | Cancer Rec Tech Ltd | Quinazoline compounds |
WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
WO2016022569A1 (en) | 2014-08-04 | 2016-02-11 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
WO2016038552A1 (en) | 2014-09-10 | 2016-03-17 | Glaxosmithkline Intellectual Property Development Limited | Pyridone derivatives as rearranged during transfection (ret) kinase inhibitors |
US9879021B2 (en) | 2014-09-10 | 2018-01-30 | Glaxosmithkline Intellectual Property Development Limited | Compounds as rearranged during transfection (RET) inhibitors |
ES2792036T3 (es) | 2014-11-14 | 2020-11-06 | Nerviano Medical Sciences Srl | Derivados de 6-amino-7-biciclo-7-deaza-purina como inhibidores de cinasa |
US10202365B2 (en) | 2015-02-06 | 2019-02-12 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors |
CA2992586A1 (en) | 2015-07-16 | 2017-01-19 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
BR112018001190A2 (pt) | 2015-07-24 | 2018-09-11 | Blueprint Medicines Corp | composições úteis para tratar distúrbios relacionados a kit e pdfgr |
AU2016311426B2 (en) | 2015-08-26 | 2021-05-20 | Blueprint Medicines Corporation | Compounds and compositions useful for treating disorders related to NTRK |
CN105255927B (zh) | 2015-09-30 | 2018-07-27 | 温州医科大学附属第一医院 | 一种kiaa1217-ret融合基因 |
MX2018005545A (es) | 2015-11-02 | 2019-02-20 | Janssen Pharmaceutica Nv | Anticuerpos anti-il1rap, moleculas de union a antigenos biespecificas que se unen a il1rap y cd3, y usos de estas. |
TWI757256B (zh) | 2015-11-02 | 2022-03-11 | 美商纜圖藥品公司 | 轉染過程重排之抑制劑 |
PE20181300A1 (es) | 2015-11-02 | 2018-08-09 | Five Prime Therapeutics Inc | Polipeptidos del dominio extracelular de cd80 y su uso en el tratamiento del cancer |
AR106756A1 (es) | 2015-11-19 | 2018-02-14 | Blueprint Medicines Corp | Compuestos y composiciones útiles para el tratamiento de trastornos relacionados con ntrk |
WO2017145050A1 (en) | 2016-02-23 | 2017-08-31 | Glaxosmithkline Intellectual Property Development Limited | Pyridylpyridone derivative useful as a ret kinase inhibitor in the treatment of ibs and cancer |
TW201738228A (zh) | 2016-03-17 | 2017-11-01 | 藍圖醫藥公司 | Ret之抑制劑 |
SG11201808388QA (en) | 2016-04-01 | 2018-10-30 | Signal Pharm Llc | Substituted aminopurine compounds, compositions thereof, and methods of treatment therewith |
DK3442980T3 (da) | 2016-04-15 | 2021-08-30 | Cancer Research Tech Ltd | Heterocykliske forbindelser som ret-kinase-hæmmere |
HRP20221051T8 (hr) | 2016-04-15 | 2023-07-21 | Cancer Research Technology Limited | Heterociklički spojevi kao inhibitori ret kinaze |
PT3442977T (pt) | 2016-04-15 | 2023-10-04 | Blueprint Medicines Corp | Inibidores do recetor de activina de tipo quinase |
US10227329B2 (en) | 2016-07-22 | 2019-03-12 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
US10035789B2 (en) | 2016-07-27 | 2018-07-31 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
US20190192522A1 (en) | 2016-09-08 | 2019-06-27 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor 4 in combination with cyclin-dependent kinase inhibitors |
JP2018052878A (ja) | 2016-09-29 | 2018-04-05 | 第一三共株式会社 | ピリジン化合物 |
CN106749231B (zh) | 2016-10-09 | 2019-03-01 | 南京纳丁菲医药科技有限公司 | 萘啶化合物和药物组合物及它们的应用 |
JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
US10799503B2 (en) | 2016-12-01 | 2020-10-13 | Ignyta, Inc. | Methods for the treatment of cancer |
US11168090B2 (en) | 2017-01-18 | 2021-11-09 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors |
WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
US11040979B2 (en) | 2017-03-31 | 2021-06-22 | Blueprint Medicines Corporation | Substituted pyrrolo[1,2-b]pyridazines for treating disorders related to KIT and PDGFR |
GB201705971D0 (en) | 2017-04-13 | 2017-05-31 | Cancer Res Tech Ltd | Inhibitor compounds |
WO2018213329A1 (en) | 2017-05-15 | 2018-11-22 | Blueprint Medicines Corporation | Combinations of ret inhibitors and mtorc1 inhibitors and uses thereof for the treatment of cancer mediated by aberrant ret activity |
EP3641776B1 (en) | 2017-06-23 | 2023-10-18 | San Diego State University Research Foundation | Atropisomerism for enhanced kinase inhibitor selectivity |
CN109180677A (zh) | 2017-06-30 | 2019-01-11 | 厦门大学 | 取代芳基醚类化合物、其制备方法、药用组合物及其应用 |
PT3649260T (pt) | 2017-07-07 | 2022-05-30 | Nipd Genetics Public Company Ltd | Análise paralela multiplexada enriquecida com alvo para avaliação de biomarcadores tumorais |
EP3728271B1 (en) | 2017-12-19 | 2022-09-28 | Turning Point Therapeutics, Inc. | Macrocyclic compounds for treating diseases |
TWI802635B (zh) | 2018-01-18 | 2023-05-21 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡咯并[2,3-d]嘧啶化合物 |
JP6997876B2 (ja) | 2018-01-18 | 2022-02-04 | アレイ バイオファーマ インコーポレイテッド | Retキナーゼ阻害剤としての置換ピラゾリル[4,3-c]ピリジン化合物 |
US11524963B2 (en) | 2018-01-18 | 2022-12-13 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidines as RET kinase inhibitors |
JP7422084B2 (ja) | 2018-04-03 | 2024-01-25 | ブループリント メディシンズ コーポレイション | Ret変化を有する癌の処置において使用するためのret阻害剤 |
US20210308134A1 (en) | 2018-08-10 | 2021-10-07 | Blueprint Medicines Corporation | Treatment of egfr-mutant cancer |
-
2016
- 2016-11-01 TW TW105135376A patent/TWI757256B/zh active
- 2016-11-01 IL IL302209A patent/IL302209B2/en unknown
- 2016-11-01 NZ NZ742351A patent/NZ742351A/en unknown
- 2016-11-01 HU HUE16794885A patent/HUE064659T2/hu unknown
- 2016-11-01 SG SG11201803653QA patent/SG11201803653QA/en unknown
- 2016-11-01 US US15/340,428 patent/US10030005B2/en active Active
- 2016-11-01 HR HRP20231681TT patent/HRP20231681T1/hr unknown
- 2016-11-01 CA CA3003721A patent/CA3003721C/en active Active
- 2016-11-01 CN CN201680076816.XA patent/CN108473468B/zh active Active
- 2016-11-01 PT PT167948850T patent/PT3371171T/pt unknown
- 2016-11-01 JP JP2018521916A patent/JP6807385B2/ja active Active
- 2016-11-01 LT LTEPPCT/US2016/059879T patent/LT3371171T/lt unknown
- 2016-11-01 RS RS20240044A patent/RS65069B1/sr unknown
- 2016-11-01 TW TW110148980A patent/TWI787018B/zh active
- 2016-11-01 FI FIEP16794885.0T patent/FI3371171T3/fi active
- 2016-11-01 KR KR1020187015706A patent/KR20180073689A/ko not_active Application Discontinuation
- 2016-11-01 PL PL16794885.0T patent/PL3371171T3/pl unknown
- 2016-11-01 BR BR112018008877-3A patent/BR112018008877B1/pt active IP Right Grant
- 2016-11-01 MY MYPI2018701728A patent/MY194262A/en unknown
- 2016-11-01 AU AU2016348402A patent/AU2016348402B2/en active Active
- 2016-11-01 IL IL288519A patent/IL288519B2/en unknown
- 2016-11-01 EP EP23201915.8A patent/EP4292594A3/en active Pending
- 2016-11-01 ES ES16794885T patent/ES2969185T3/es active Active
- 2016-11-01 EP EP23201930.7A patent/EP4331585A3/en active Pending
- 2016-11-01 WO PCT/US2016/059879 patent/WO2017079140A1/en active Application Filing
- 2016-11-01 EA EA201891087A patent/EA038890B1/ru unknown
- 2016-11-01 CN CN202010391097.9A patent/CN111423416B/zh active Active
- 2016-11-01 DK DK16794885.0T patent/DK3371171T3/da active
- 2016-11-01 MX MX2018005528A patent/MX2018005528A/es unknown
- 2016-11-01 SI SI201631796T patent/SI3371171T1/sl unknown
- 2016-11-01 EP EP16794885.0A patent/EP3371171B1/en active Active
-
2018
- 2018-04-24 IL IL258902A patent/IL258902B/en unknown
- 2018-04-27 PH PH12018500907A patent/PH12018500907A1/en unknown
- 2018-05-02 SA SA518391496A patent/SA518391496B1/ar unknown
- 2018-05-02 CL CL2018001181A patent/CL2018001181A1/es unknown
- 2018-05-09 ZA ZA2018/03050A patent/ZA201803050B/en unknown
- 2018-07-20 US US16/041,719 patent/US10584114B2/en active Active
-
2019
- 2019-01-30 HK HK19101648.3A patent/HK1259287A1/zh unknown
-
2020
- 2020-01-29 US US16/775,646 patent/US11279688B2/en active Active
- 2020-12-07 JP JP2020202520A patent/JP7026196B2/ja active Active
-
2022
- 2022-02-11 US US17/669,785 patent/US20220315560A1/en not_active Abandoned
- 2022-02-14 JP JP2022020355A patent/JP2022058976A/ja active Pending
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20231681T1 (hr) | Inhibitori za ret | |
HRP20192336T1 (hr) | Derivati imidazotiadiazola i imidazopirazina kao inhibitori proteazom aktiviranog receptora 4 (par4) za liječenje agregacije trombocita | |
HRP20160533T1 (hr) | Indoli kao antivirusna sredstva respiratornog sincicijskog virusa | |
HRP20221112T1 (hr) | Derivati benzodiazepina kao inhibitori rsv | |
HRP20160852T1 (hr) | Biciklični heterociklični spojevi kao inhibitori protein tirozin kinaze | |
SI3024819T1 (en) | Glyoxamide-substituted pyrrolamide derivatives and their use as medicines for the treatment of hepatitis B | |
HRP20160002T1 (hr) | Bicikliäśki heterocikliäśki spojevi kao inhibitori protein tirozin kinaze | |
PE20170127A1 (es) | Indazol-3-carboxamidas 5-sustituidas y preparacion y uso de las mismas | |
MX2022005839A (es) | Compuestos utiles como inhibidores de la proteina helios. | |
HRP20220899T1 (hr) | Spojevi policikličkog karbamoilpiridona i njihova farmaceutska uporaba | |
HRP20180444T1 (hr) | 9-aminometil-supstituirani tetraciklinski spojevi | |
DE602007008550D1 (de) | 3,7-diamino-10h-phenothiazinsalze und ihre verwendung | |
HRP20120202T1 (hr) | AMIDOFENOKSIINDAZOLI, KORISNI KAO INHIBITORI c-MET | |
EA201290260A1 (ru) | Бензимидазол-имидазольные производные | |
HRP20090151T3 (hr) | Derivati indozolona kao inhibitori 11b-hsd1 | |
JP2009532486A5 (hr) | ||
HRP20211973T1 (hr) | Kinazolini kao inhibitori ionskih kalijskih kanala | |
JP2015512435A5 (hr) | ||
RS51795B (en) | 2-AMINO-7,8-DIHYDRO-6H-PIRIDO [4,3-D] PYRIMIDINE-5-ONE, A PROCEDURE FOR THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM | |
PE20131304A1 (es) | Heteroarilos y sus usos | |
AR062110A1 (es) | Derivado de anillo fusionado de espiroquetas y su uso como farmaco antidiabetico | |
TW200640879A (en) | Amide derivatives | |
AR065927A1 (es) | Derivados de 5,6-dihidro-1h-piridin-2-ona | |
CL2022000125A1 (es) | Derivados de 2,4-diaminoquinazolina y usos médicos de los mismos. (divisional de solicitud 202002253) | |
HRP20201789T1 (hr) | Antiproliferativni spojevi, te njihovi farmaceutski pripravci i uporabe |