ES2661510T3 - Uso de inhibidores de la actividad o función de PI3K - Google Patents
Uso de inhibidores de la actividad o función de PI3K Download PDFInfo
- Publication number
- ES2661510T3 ES2661510T3 ES12818825.7T ES12818825T ES2661510T3 ES 2661510 T3 ES2661510 T3 ES 2661510T3 ES 12818825 T ES12818825 T ES 12818825T ES 2661510 T3 ES2661510 T3 ES 2661510T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- amino
- alkoxy
- hydroxy
- halo
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 108091007960 PI3Ks Proteins 0.000 title abstract description 12
- 239000003112 inhibitor Substances 0.000 title abstract description 9
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 title abstract 2
- 230000000694 effects Effects 0.000 title description 2
- -1 C1-alkoxy C8 Chemical group 0.000 abstract description 33
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract description 10
- 229910052757 nitrogen Inorganic materials 0.000 abstract description 10
- 125000001424 substituent group Chemical group 0.000 abstract description 10
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract description 9
- 229910052736 halogen Inorganic materials 0.000 abstract description 9
- 125000000623 heterocyclic group Chemical group 0.000 abstract description 9
- 239000012828 PI3K inhibitor Substances 0.000 abstract description 8
- 125000005842 heteroatom Chemical group 0.000 abstract description 8
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 abstract description 8
- 102000001708 Protein Isoforms Human genes 0.000 abstract description 7
- 108010029485 Protein Isoforms Proteins 0.000 abstract description 7
- 150000002367 halogens Chemical group 0.000 abstract description 7
- 230000002401 inhibitory effect Effects 0.000 abstract description 7
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract description 7
- 125000003545 alkoxy group Chemical group 0.000 abstract description 6
- 150000003839 salts Chemical class 0.000 abstract description 6
- 229910052799 carbon Inorganic materials 0.000 abstract description 5
- 125000004432 carbon atom Chemical group C* 0.000 abstract description 4
- 230000003647 oxidation Effects 0.000 abstract description 4
- 238000007254 oxidation reaction Methods 0.000 abstract description 4
- 125000004043 oxo group Chemical group O=* 0.000 abstract description 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract description 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract description 3
- 125000002757 morpholinyl group Chemical group 0.000 abstract description 3
- 125000004193 piperazinyl group Chemical group 0.000 abstract description 3
- 125000003386 piperidinyl group Chemical group 0.000 abstract description 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract description 3
- 125000001412 tetrahydropyranyl group Chemical group 0.000 abstract description 3
- 125000004632 tetrahydrothiopyranyl group Chemical group S1C(CCCC1)* 0.000 abstract description 3
- 102000008235 Toll-Like Receptor 9 Human genes 0.000 abstract description 2
- 108010060818 Toll-Like Receptor 9 Proteins 0.000 abstract description 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 3
- 125000002098 pyridazinyl group Chemical group 0.000 abstract 3
- 125000004076 pyridyl group Chemical group 0.000 abstract 3
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 3
- 125000004529 1,2,3-triazinyl group Chemical group N1=NN=C(C=C1)* 0.000 abstract 2
- 125000004530 1,2,4-triazinyl group Chemical group N1=NC(=NC=C1)* 0.000 abstract 2
- 125000003363 1,3,5-triazinyl group Chemical group N1=C(N=CN=C1)* 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000001544 thienyl group Chemical group 0.000 abstract 2
- NFKMPKOGCRBAJF-UHFFFAOYSA-N $l^{1}-azanylformonitrile Chemical compound [N]C#N NFKMPKOGCRBAJF-UHFFFAOYSA-N 0.000 abstract 1
- FHLXQXCQSUICIN-UHFFFAOYSA-N 1,2,3,4-tetrahydropyrido[3,2-d]pyrimidine Chemical group C1=CC=C2NCNCC2=N1 FHLXQXCQSUICIN-UHFFFAOYSA-N 0.000 abstract 1
- 125000004502 1,2,3-oxadiazolyl group Chemical group 0.000 abstract 1
- 125000004511 1,2,3-thiadiazolyl group Chemical group 0.000 abstract 1
- 125000001399 1,2,3-triazolyl group Chemical group N1N=NC(=C1)* 0.000 abstract 1
- 125000004504 1,2,4-oxadiazolyl group Chemical group 0.000 abstract 1
- 125000004514 1,2,4-thiadiazolyl group Chemical group 0.000 abstract 1
- 125000001376 1,2,4-triazolyl group Chemical group N1N=C(N=C1)* 0.000 abstract 1
- 125000004506 1,2,5-oxadiazolyl group Chemical group 0.000 abstract 1
- 125000004517 1,2,5-thiadiazolyl group Chemical group 0.000 abstract 1
- 125000001781 1,3,4-oxadiazolyl group Chemical group 0.000 abstract 1
- 125000004520 1,3,4-thiadiazolyl group Chemical group 0.000 abstract 1
- 125000004364 3-pyrrolinyl group Chemical group [H]C1=C([H])C([H])([H])N(*)C1([H])[H] 0.000 abstract 1
- 206010063094 Cerebral malaria Diseases 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 230000001154 acute effect Effects 0.000 abstract 1
- 125000003725 azepanyl group Chemical group 0.000 abstract 1
- 125000004069 aziridinyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000009454 functional inhibition Effects 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 125000005553 heteroaryloxy group Chemical group 0.000 abstract 1
- 125000005844 heterocyclyloxy group Chemical group 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 abstract 1
- 125000001786 isothiazolyl group Chemical group 0.000 abstract 1
- 125000000842 isoxazolyl group Chemical group 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 125000003551 oxepanyl group Chemical group 0.000 abstract 1
- 125000003566 oxetanyl group Chemical group 0.000 abstract 1
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 1
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 1
- 125000003507 tetrahydrothiofenyl group Chemical group 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 description 30
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 15
- 210000004027 cell Anatomy 0.000 description 15
- 239000012634 fragment Substances 0.000 description 12
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 description 10
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 description 10
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 description 8
- 238000010790 dilution Methods 0.000 description 5
- 239000012895 dilution Substances 0.000 description 5
- 239000012453 solvate Substances 0.000 description 5
- 210000000952 spleen Anatomy 0.000 description 5
- 210000004988 splenocyte Anatomy 0.000 description 5
- 238000003016 alphascreen Methods 0.000 description 4
- 238000006243 chemical reaction Methods 0.000 description 4
- 239000013598 vector Substances 0.000 description 4
- 238000010367 cloning Methods 0.000 description 3
- 238000001514 detection method Methods 0.000 description 3
- CQZXDIHVSPZIGF-UHFFFAOYSA-N 1-methylimidazole-4-carbaldehyde Chemical compound CN1C=NC(C=O)=C1 CQZXDIHVSPZIGF-UHFFFAOYSA-N 0.000 description 2
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 description 2
- LRGBDJBDJXZTTD-UHFFFAOYSA-N 1h-pyrazole-4-carbaldehyde Chemical compound O=CC=1C=NNC=1 LRGBDJBDJXZTTD-UHFFFAOYSA-N 0.000 description 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 description 2
- YRJNUIQFTSGXGK-UHFFFAOYSA-N 5-methyl-1,3,4-oxadiazole-2-carbaldehyde Chemical compound CC1=NN=C(C=O)O1 YRJNUIQFTSGXGK-UHFFFAOYSA-N 0.000 description 2
- 102000004889 Interleukin-6 Human genes 0.000 description 2
- 108090001005 Interleukin-6 Proteins 0.000 description 2
- 241001529936 Murinae Species 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 description 2
- 239000011324 bead Substances 0.000 description 2
- 238000004113 cell culture Methods 0.000 description 2
- 239000013592 cell lysate Substances 0.000 description 2
- 239000006285 cell suspension Substances 0.000 description 2
- 239000013599 cloning vector Substances 0.000 description 2
- 230000006862 enzymatic digestion Effects 0.000 description 2
- 239000012091 fetal bovine serum Substances 0.000 description 2
- 125000001153 fluoro group Chemical group F* 0.000 description 2
- 239000001963 growth medium Substances 0.000 description 2
- 125000005843 halogen group Chemical group 0.000 description 2
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 description 2
- 125000002140 imidazol-4-yl group Chemical group [H]N1C([H])=NC([*])=C1[H] 0.000 description 2
- 238000011534 incubation Methods 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 2
- 239000013612 plasmid Substances 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- DXBWJLDFSICTIH-UHFFFAOYSA-N pyrazine-2-carbaldehyde Chemical compound O=CC1=CN=CC=N1 DXBWJLDFSICTIH-UHFFFAOYSA-N 0.000 description 2
- QJZUKDFHGGYHMC-UHFFFAOYSA-N pyridine-3-carbaldehyde Chemical compound O=CC1=CC=CN=C1 QJZUKDFHGGYHMC-UHFFFAOYSA-N 0.000 description 2
- BGUWFUQJCDRPTL-UHFFFAOYSA-N pyridine-4-carbaldehyde Chemical compound O=CC1=CC=NC=C1 BGUWFUQJCDRPTL-UHFFFAOYSA-N 0.000 description 2
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 description 2
- DAEPDZWVDSPTHF-UHFFFAOYSA-M sodium pyruvate Chemical compound [Na+].CC(=O)C([O-])=O DAEPDZWVDSPTHF-UHFFFAOYSA-M 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- UCSJYZPVAKXKNQ-HZYVHMACSA-N streptomycin Chemical compound CN[C@H]1[C@H](O)[C@@H](O)[C@H](CO)O[C@H]1O[C@@H]1[C@](C=O)(O)[C@H](C)O[C@H]1O[C@@H]1[C@@H](NC(N)=N)[C@H](O)[C@@H](NC(N)=N)[C@H](O)[C@H]1O UCSJYZPVAKXKNQ-HZYVHMACSA-N 0.000 description 2
- 239000006228 supernatant Substances 0.000 description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 2
- 241000701447 unidentified baculovirus Species 0.000 description 2
- 108091003079 Bovine Serum Albumin Proteins 0.000 description 1
- 238000011740 C57BL/6 mouse Methods 0.000 description 1
- 101100322915 Caenorhabditis elegans akt-1 gene Proteins 0.000 description 1
- 108091026890 Coding region Proteins 0.000 description 1
- 238000002965 ELISA Methods 0.000 description 1
- 206010015548 Euthanasia Diseases 0.000 description 1
- 241000699666 Mus <mouse, genus> Species 0.000 description 1
- 229930182555 Penicillin Natural products 0.000 description 1
- JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 description 1
- 239000004743 Polypropylene Substances 0.000 description 1
- 239000006146 Roswell Park Memorial Institute medium Substances 0.000 description 1
- 102000002689 Toll-like receptor Human genes 0.000 description 1
- 108020000411 Toll-like receptor Proteins 0.000 description 1
- DHDIBUUKHMDGSQ-INIZCTEOSA-N [(3s)-3-[[6-[6-methoxy-5-(trifluoromethyl)pyridin-3-yl]-7,8-dihydro-5h-pyrido[4,3-d]pyrimidin-4-yl]oxy]pyrrolidin-1-yl]-(1-methylpyrazol-4-yl)methanone Chemical compound C1=C(C(F)(F)F)C(OC)=NC=C1N1CC2=C(O[C@@H]3CN(CC3)C(=O)C3=CN(C)N=C3)N=CN=C2CC1 DHDIBUUKHMDGSQ-INIZCTEOSA-N 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000008004 cell lysis buffer Substances 0.000 description 1
- 238000005119 centrifugation Methods 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 239000002299 complementary DNA Substances 0.000 description 1
- 239000013024 dilution buffer Substances 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 210000003743 erythrocyte Anatomy 0.000 description 1
- 239000013604 expression vector Substances 0.000 description 1
- 238000013213 extrapolation Methods 0.000 description 1
- 239000012467 final product Substances 0.000 description 1
- 108020001507 fusion proteins Proteins 0.000 description 1
- 102000037865 fusion proteins Human genes 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 229940100601 interleukin-6 Drugs 0.000 description 1
- 239000003446 ligand Substances 0.000 description 1
- 239000012139 lysis buffer Substances 0.000 description 1
- 238000002803 maceration Methods 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 229940049954 penicillin Drugs 0.000 description 1
- 230000026731 phosphorylation Effects 0.000 description 1
- 238000006366 phosphorylation reaction Methods 0.000 description 1
- 229920001155 polypropylene Polymers 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000011535 reaction buffer Substances 0.000 description 1
- 230000006798 recombination Effects 0.000 description 1
- 238000005215 recombination Methods 0.000 description 1
- 238000012163 sequencing technique Methods 0.000 description 1
- 238000013207 serial dilution Methods 0.000 description 1
- 229940054269 sodium pyruvate Drugs 0.000 description 1
- 210000004989 spleen cell Anatomy 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 239000011550 stock solution Substances 0.000 description 1
- 229960005322 streptomycin Drugs 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- DGVVWUTYPXICAM-UHFFFAOYSA-N β‐Mercaptoethanol Chemical compound OCCS DGVVWUTYPXICAM-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines 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
- A61K31/55—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/06—Antimalarials
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/10—Anthelmintics
-
- 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
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/74—Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161576194P | 2011-12-15 | 2011-12-15 | |
| US201161576194P | 2011-12-15 | ||
| PCT/IB2012/057332 WO2013088404A1 (en) | 2011-12-15 | 2012-12-14 | Use of inhibitors of the activity or function of PI3K |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2661510T3 true ES2661510T3 (es) | 2018-04-02 |
Family
ID=47603895
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES12818825.7T Active ES2661510T3 (es) | 2011-12-15 | 2012-12-14 | Uso de inhibidores de la actividad o función de PI3K |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US9949979B2 (https=) |
| EP (1) | EP2790705B1 (https=) |
| JP (1) | JP6117235B2 (https=) |
| KR (1) | KR102038462B1 (https=) |
| CN (1) | CN103998042B (https=) |
| AP (1) | AP3849A (https=) |
| AU (1) | AU2012354094C1 (https=) |
| BR (1) | BR112014014327A2 (https=) |
| CA (1) | CA2857302C (https=) |
| DK (1) | DK2790705T3 (https=) |
| EA (1) | EA029473B1 (https=) |
| ES (1) | ES2661510T3 (https=) |
| GT (1) | GT201400114A (https=) |
| HU (1) | HUE036052T2 (https=) |
| MA (1) | MA35857B1 (https=) |
| MX (1) | MX351530B (https=) |
| NI (1) | NI201400056A (https=) |
| NO (1) | NO2896266T3 (https=) |
| PH (1) | PH12014501348A1 (https=) |
| PL (1) | PL2790705T3 (https=) |
| PT (1) | PT2790705T (https=) |
| SI (1) | SI2790705T1 (https=) |
| TN (1) | TN2014000230A1 (https=) |
| WO (1) | WO2013088404A1 (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA112517C2 (uk) | 2010-07-06 | 2016-09-26 | Новартіс Аг | Тетрагідропіридопіримідинові похідні |
| EP2790705B1 (en) | 2011-12-15 | 2017-12-06 | Novartis AG | Use of inhibitors of the activity or function of pi3k |
| IN2015DN03235A (https=) | 2012-11-07 | 2015-10-02 | Karus Therapeutics Ltd | |
| PT2994465T (pt) | 2013-05-10 | 2018-10-25 | Karus Therapeutics Ltd | Novos inibidores de histona desacetilase |
| ES2818933T3 (es) * | 2013-10-10 | 2021-04-14 | Acetylon Pharmaceuticals Inc | Inhibidores de la HDAC en combinación con los inhibidores de la pi3k, para el tratamiento del linfoma no Hodgkin |
| EP3079683A4 (en) | 2013-12-13 | 2017-12-20 | Dana-Farber Cancer Institute, Inc. | Methods to treat lymphoplasmacytic lymphoma |
| CA2932353A1 (en) | 2013-12-13 | 2015-06-18 | Steven P. Treon | Methods to treat lymphoplasmacytic lymphoma |
| WO2015162584A1 (en) | 2014-04-24 | 2015-10-29 | Novartis Ag | Crystalline forms of the sulfate salt of n-[5-(3-imidazol-1-yl-4-methanesulfonyl-phenyl)-4-methyl-thiazol-2-yl]-acetamide |
| EP3715346B1 (en) | 2014-10-22 | 2024-01-03 | Dana-Farber Cancer Institute, Inc. | Thiazolyl-containing compounds for treating proliferative diseases |
| GB201419264D0 (en) | 2014-10-29 | 2014-12-10 | Karus Therapeutics Ltd | Compounds |
| GB201419228D0 (en) | 2014-10-29 | 2014-12-10 | Karus Therapeutics Ltd | Compounds |
| BR112020018094A2 (pt) | 2018-03-08 | 2020-12-22 | Incyte Corporation | Compostos de aminopirazina diol como inibidores de pi3k-¿ |
| BR112020025538A2 (pt) * | 2018-06-19 | 2021-03-16 | Novartis Ag | Compostos de cianotriazol e usos dos mesmos |
| US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
| US20220363667A1 (en) | 2018-07-17 | 2022-11-17 | Nippon Chemiphar Co., Ltd. | T-type calcium channel blocker |
| AU2020250468A1 (en) | 2019-03-29 | 2021-11-04 | Kinki University | Use of T-type calcium channel blocker for treating pruritus |
| CN119173446A (zh) | 2022-03-08 | 2024-12-20 | 赤盾医疗有限公司 | 机器人药物制备系统中的流体转移站 |
| CN114957676B (zh) * | 2022-06-22 | 2023-05-16 | 安徽工程大学 | 一种利用反溶剂沉积快速调控水分活度制备美拉德反应产物的方法 |
| CN117534672A (zh) * | 2023-11-10 | 2024-02-09 | 北京康立生医药技术开发有限公司 | 一种apds治疗药物新的制备方法 |
Family Cites Families (117)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5300645A (en) | 1993-04-14 | 1994-04-05 | Eli Lilly And Company | Tetrahydro-pyrido-indole |
| US5858753A (en) | 1996-11-25 | 1999-01-12 | Icos Corporation | Lipid kinase |
| US5939421A (en) | 1997-07-01 | 1999-08-17 | Signal Pharmaceuticals, Inc. | Quinazoline analogs and related compounds and methods for treating inflammatory conditions |
| US6667300B2 (en) | 2000-04-25 | 2003-12-23 | Icos Corporation | Inhibitors of human phosphatidylinositol 3-kinase delta |
| AU2001257571A1 (en) | 2000-05-10 | 2001-11-20 | Icos Corporation | Phosphatidyl inositol 3-kinase delta binding partner |
| DE10043667A1 (de) | 2000-09-05 | 2002-03-14 | Merck Patent Gmbh | 2-Guanidino-4-aryl-chinazoline |
| EP2070921A1 (en) | 2000-11-07 | 2009-06-17 | Novartis Ag | Indolylmaleimide derivatives as protein kinase c inhibitors |
| DE60217322T2 (de) | 2001-04-27 | 2007-10-04 | Zenyaku Kogyo K.K. | Heterocyclische verbindung und antitumormittel, das diese als wirkstoff enthält |
| TW200918046A (en) | 2002-04-03 | 2009-05-01 | Novartis Ag | Indolylmaleimide derivatives |
| CA2506432A1 (en) | 2002-12-09 | 2004-06-24 | Robert A. Kirken | Methods for selectively inhibiting janus tyrosine kinase 3 (jak3) |
| NZ540729A (en) | 2002-12-27 | 2008-03-28 | Angeletti P Ist Richerche Bio | Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds useful as HIV integrase inhibitors |
| US20050054614A1 (en) | 2003-08-14 | 2005-03-10 | Diacovo Thomas G. | Methods of inhibiting leukocyte accumulation |
| WO2005016348A1 (en) | 2003-08-14 | 2005-02-24 | Icos Corporation | Method of inhibiting immune responses stimulated by an endogenous factor |
| DK1704145T3 (da) | 2004-01-12 | 2012-09-24 | Ym Biosciences Australia Pty | Selektive kinaseinhibitorer |
| CA2553969A1 (en) | 2004-01-23 | 2005-08-04 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments |
| WO2005086814A2 (en) * | 2004-03-09 | 2005-09-22 | The Uab Research Foundation | Methods and compositions related to regulation of cytokine production by glycogen synthase kinase 3 (gsk-3) |
| CA2566436C (en) | 2004-05-13 | 2011-05-10 | Vanderbilt University | Phosphoinositide 3-kinase delta selective inhibitors for inhibiting angiogenesis |
| WO2005113556A1 (en) | 2004-05-13 | 2005-12-01 | Icos Corporation | Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta |
| SI1761528T1 (sl) | 2004-06-11 | 2008-06-30 | Japan Tobacco Inc | 5-amino-2,4,7-triokso-3,4,7,8-tetrahidro-2H-pirido(2,3-D)pirimidinski derivati in sorodne spojine za zdravljenje raka |
| GB0423653D0 (en) | 2004-10-25 | 2004-11-24 | Piramed Ltd | Pharmaceutical compounds |
| US20060128710A1 (en) | 2004-12-09 | 2006-06-15 | Chih-Hung Lee | Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof |
| KR20060079121A (ko) | 2004-12-31 | 2006-07-05 | 에스케이케미칼주식회사 | 당뇨 및 비만 치료예방에 유효한 퀴나졸린 유도체 |
| MX2007013595A (es) | 2005-05-04 | 2008-01-24 | Renovis Inc | Compuestos heterociclicos fusionados y composiciones y usos de estos. |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| US8071597B2 (en) | 2005-08-26 | 2011-12-06 | Merck Serono Sa | Pyrazine compounds and uses as PI3K inhibitors |
| GB0520657D0 (en) | 2005-10-11 | 2005-11-16 | Ludwig Inst Cancer Res | Pharmaceutical compounds |
| KR20080089416A (ko) | 2005-12-21 | 2008-10-06 | 페인셉터 파마 코포레이션 | 개폐 이온 통로를 조절하기 위한 조성물 및 방법 |
| GB0612630D0 (en) | 2006-06-26 | 2006-08-02 | Novartis Ag | Organic compounds |
| WO2008009077A2 (en) | 2006-07-20 | 2008-01-24 | Gilead Sciences, Inc. | 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives and pharmaceutical compositions useful for treating viral infections |
| RU2009106722A (ru) * | 2006-07-28 | 2010-09-10 | Новартис АГ (CH) | 2,4-замещенные хиназолины в качестве ингибиторов липидной киназы |
| EP1891958A1 (en) * | 2006-08-03 | 2008-02-27 | Universite Pierre Et Marie Curie (Paris Vi) | Rho/Rock/PI3/Akt kinase inhibitors for the treatment of diseases associated with protozoan parasites. |
| KR20090087027A (ko) | 2006-11-13 | 2009-08-14 | 일라이 릴리 앤드 캄파니 | 염증 질환 및 암의 치료를 위한 티에노피리미디논 |
| EP2139882B1 (en) | 2007-03-23 | 2013-12-25 | Amgen Inc. | 3- substituted quinoline or quinoxaline derivatives and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors |
| DK2137186T3 (en) | 2007-03-23 | 2016-04-18 | Amgen Inc | Heterocyclic compounds and their uses |
| EP2132207A2 (en) | 2007-03-23 | 2009-12-16 | Amgen Inc. | Heterocyclic compounds and their uses |
| EP2136639B1 (en) | 2007-04-02 | 2016-03-09 | Evotec AG | Pyrid-2-yl fused heterocyclic compounds, and compositions and uses thereof |
| JP2010523639A (ja) | 2007-04-12 | 2010-07-15 | エフ．ホフマン−ラ ロシュ アーゲー | 医薬化合物 |
| EP2146981A1 (en) | 2007-04-12 | 2010-01-27 | F. Hoffmann-Roche AG | Pharmaceutical compounds |
| GB0707087D0 (en) | 2007-04-12 | 2007-05-23 | Piramed Ltd | Pharmaceutical compounds |
| PT2139334E (pt) | 2007-04-17 | 2013-10-02 | Evotec Ag | Compostos heterocíclicos fusionados de 2-cianofenilo, e composições e utilizações dos mesmos |
| PE20090717A1 (es) | 2007-05-18 | 2009-07-18 | Smithkline Beecham Corp | Derivados de quinolina como inhibidores de la pi3 quinasa |
| WO2008150827A1 (en) | 2007-05-29 | 2008-12-11 | Smithkline Beecham Corporation | Naphthyridine, derivatives as p13 kinase inhibitors |
| US7893060B2 (en) | 2007-06-12 | 2011-02-22 | F. Hoffmann-La Roche Ag | Thiazolopyrimidines and their use as inhibitors of phosphatidylinositol-3 kinase |
| WO2008152394A1 (en) | 2007-06-12 | 2008-12-18 | F.Hoffmann-La Roche Ag | Pharmaceutical compounds |
| WO2008152387A1 (en) | 2007-06-12 | 2008-12-18 | F.Hoffmann-La Roche Ag | Quinazoline derivatives as pi3 kinase inhibitors |
| UY31137A1 (es) * | 2007-06-14 | 2009-01-05 | Smithkline Beecham Corp | Derivados de quinazolina como inhibidores de la pi3 quinasa |
| RU2341527C1 (ru) | 2007-07-17 | 2008-12-20 | Общество С Ограниченной Ответственностью "Исследовательский Институт Химического Разнообразия" | Аннелированные азагетероциклы, включающие пиримидиновый фрагмент, способ их получения и ингибиторы pi3k киназ |
| TW200908984A (en) | 2007-08-07 | 2009-03-01 | Piramal Life Sciences Ltd | Pyridyl derivatives, their preparation and use |
| WO2009036768A2 (en) | 2007-09-19 | 2009-03-26 | H. Lundbeck A/S | Diagnosing potential weight gain in a subject |
| GB2467670B (en) | 2007-10-04 | 2012-08-01 | Intellikine Inc | Chemical entities and therapeutic uses thereof |
| US20100298289A1 (en) | 2007-10-09 | 2010-11-25 | Ucb Pharma, S.A. | Heterobicyclic compounds as histamine h4-receptor antagonists |
| WO2009058361A1 (en) * | 2007-10-31 | 2009-05-07 | Dynavax Technologies Corp. | Inhibition of type i ifn production |
| CN101952292A (zh) | 2007-11-13 | 2011-01-19 | 艾科斯有限公司 | 人磷脂酰肌醇3-激酶δ的抑制剂 |
| MX2010007419A (es) | 2008-01-04 | 2010-11-12 | Intellikine Inc | Ciertas entidades quimicas, composiciones y metodos. |
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| JP2011515462A (ja) | 2008-03-27 | 2011-05-19 | アウククランド ウニセルビセス リミテッド | 置換されたピリミジン、及びトリアジン、並びに癌療法におけるこれらの使用 |
| US8436005B2 (en) | 2008-04-03 | 2013-05-07 | Abbott Laboratories | Macrocyclic pyrimidine derivatives |
| WO2009147189A1 (en) | 2008-06-05 | 2009-12-10 | Glaxo Group Limited | Novel compounds |
| ES2383246T3 (es) | 2008-06-05 | 2012-06-19 | Glaxo Group Limited | 4-amino-indazoles |
| WO2009147188A1 (en) | 2008-06-05 | 2009-12-10 | Glaxo Group Limited | Benzpyrazol derivatives as inhibitors of pi3 kinases |
| ES2491522T3 (es) | 2008-06-19 | 2014-09-08 | Millennium Pharmaceuticals, Inc. | Derivados de tiofeno o tiazol y su uso como inhibidores de PI3K |
| US8513221B2 (en) | 2008-07-07 | 2013-08-20 | Xcovery Holding, LLC | PI3K isoform selective inhibitors |
| BRPI0915231A2 (pt) | 2008-07-08 | 2018-06-12 | Intellikine Inc | compostos inibidores de quinase e métodos de uso |
| BRPI0919816A2 (pt) * | 2008-09-26 | 2019-09-24 | Eisai R&D Man Co Ltd | uso compostos benzoxazólicos no tratamento de malária |
| CA2738429C (en) | 2008-09-26 | 2016-10-25 | Intellikine, Inc. | Heterocyclic kinase inhibitors |
| KR20160091440A (ko) | 2008-11-13 | 2016-08-02 | 길리아드 칼리스토가 엘엘씨 | 혈액 종양에 대한 요법 |
| WO2010059593A1 (en) | 2008-11-18 | 2010-05-27 | Intellikine, Inc. | Methods and compositions for treatment of ophthalmic conditions |
| WO2010065923A2 (en) | 2008-12-04 | 2010-06-10 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Phosphatidylinositol-3-kinase p110 delta-targeted drugs in the treatment of cns disorders |
| JP5656880B2 (ja) | 2009-03-09 | 2015-01-21 | グラクソ グループ リミテッドＧｌａｘｏ Ｇｒｏｕｐ Ｌｉｍｉｔｅｄ | Ｐｉ３キナーゼの阻害剤としての４−オキサジアゾール−２−イル−インダゾール |
| BRPI1012333A2 (pt) | 2009-03-24 | 2016-03-29 | Gilead Calistoga Llc | atropisômeros de derivados de 2-purinil-3-tolil-quinazolinonas e métodos de uso |
| SG174483A1 (en) | 2009-03-24 | 2011-10-28 | Univ Singapore | Use of artemisinin derivatives for the treatment of asthma and chronic obstructive pulmonary disease (copd) |
| WO2010120991A1 (en) * | 2009-04-17 | 2010-10-21 | Wyeth Llc | 5, 6, 7, 8-tetrahydropyrido[4,3-d]pyrimidine compounds, their use as mtor, pi3, and hsmg-1 kinase inhibitors, and their syntheses |
| AP2011005956A0 (en) | 2009-04-20 | 2011-10-31 | Gilead Calistoga Llc | Methods of treatment for solid tumors. |
| LT2899191T (lt) | 2009-04-30 | 2017-10-25 | Glaxo Group Limited | Oksazolo pakeistieji indazolai kaip pi3-kinazės inhibitoriai |
| JP5789252B2 (ja) | 2009-05-07 | 2015-10-07 | インテリカイン， エルエルシー | 複素環式化合物およびその使用 |
| BRPI1009022A2 (pt) | 2009-05-27 | 2016-03-08 | Hoffmann La Roche | "composto, composição farmacêutica, processo para produzir uma composição farmacêutica, uso de um composto, método para tratamento de uma doença ou transtorno e kit" |
| US8158625B2 (en) | 2009-05-27 | 2012-04-17 | Genentech, Inc. | Bicyclic indole-pyrimidine PI3K inhibitor compounds selective for P110 delta, and methods of use |
| AU2010265971B2 (en) | 2009-06-25 | 2014-08-14 | Amgen Inc. | Heterocyclic compounds and their uses as inhibitors of PI3 K activity |
| CN102625799A (zh) | 2009-06-25 | 2012-08-01 | 安姆根有限公司 | 杂环化合物及其用途 |
| CA2765817A1 (en) | 2009-06-25 | 2010-12-29 | Amgen Inc. | 4h-pyrido[1,2-a]pyrimidin-4-one derivatives as pi3k inhibitors |
| SG176986A1 (en) | 2009-06-25 | 2012-02-28 | Amgen Inc | Polycyclic derivatives of pyridine and their use in the treatment of (inter alia) rheumatoid arthritis and similar diseases |
| KR101763656B1 (ko) | 2009-06-29 | 2017-08-01 | 인사이트 홀딩스 코포레이션 | Ｐｉ3ｋ 저해물질로서의 피리미디논 |
| HUE034503T2 (en) | 2009-07-02 | 2018-02-28 | Sanofi Sa | 2,3-Dihydro-1-imidazo [1,2-a] pyrimidin-5-one derivatives, their preparation process and their use in medicine |
| CN102482286B (zh) | 2009-07-02 | 2015-07-15 | 赛诺菲 | 新型1,2,3,4-四氢嘧啶并{1,2-a}嘧啶-6-酮衍生物、其制备以及其医药用途 |
| CA2768843A1 (en) | 2009-07-21 | 2011-01-27 | Gilead Calistoga Llc | Treatment of liver disorders with pi3k inhibitors |
| MX2012002059A (es) | 2009-08-20 | 2012-04-19 | Karus Therapeutics Ltd | Compestos heterociclicos triciclicos como inhibidores de fosfoionositida 3-quinasa. |
| JP2013505965A (ja) | 2009-09-29 | 2013-02-21 | エックスカバリー ホールディング カンパニー エルエルシー | Ｐｉ３ｋ（デルタ）選択的阻害剤 |
| GB0918249D0 (en) | 2009-10-19 | 2009-12-02 | Respivert Ltd | Compounds |
| NZ599830A (en) | 2009-11-05 | 2014-08-29 | Rhizen Pharmaceuticals Sa | Novel kinase modulators |
| US8741932B2 (en) | 2009-11-06 | 2014-06-03 | Piramal Enterprises Limited | Imidazopyridine derivatives |
| EA201290305A1 (ru) | 2009-11-13 | 2012-12-28 | Мерк Сероно С.А. | Производные трициклического пиразоламина |
| WO2011067364A1 (en) | 2009-12-03 | 2011-06-09 | Glaxo Group Limited | Novel compounds |
| JP2013512880A (ja) | 2009-12-03 | 2013-04-18 | グラクソ グループ リミテッド | Ｐｉ３−キナーゼ阻害剤としてのインダゾール誘導体 |
| WO2011067365A1 (en) | 2009-12-03 | 2011-06-09 | Glaxo Group Limited | Benzpyrazole derivatives as inhibitors of p13 kinases |
| MX2012006953A (es) | 2009-12-18 | 2012-10-09 | Amgen Inc | Compuestos heterociclicos y sus usos. |
| TW201130842A (en) | 2009-12-18 | 2011-09-16 | Incyte Corp | Substituted fused aryl and heteroaryl derivatives as PI3K inhibitors |
| US8759359B2 (en) | 2009-12-18 | 2014-06-24 | Incyte Corporation | Substituted heteroaryl fused derivatives as PI3K inhibitors |
| EP2539337A1 (en) | 2010-02-22 | 2013-01-02 | F. Hoffmann-La Roche AG | Pyrido[3,2-d]pyrimidine pi3k delta inhibitor compounds and methods of use |
| UY33304A (es) | 2010-04-02 | 2011-10-31 | Amgen Inc | Compuestos heterocíclicos y sus usos |
| EP2558463A1 (en) | 2010-04-14 | 2013-02-20 | Incyte Corporation | Fused derivatives as i3 inhibitors |
| GB201007347D0 (en) | 2010-04-30 | 2010-06-16 | Karus Therapeutics Ltd | Compounds |
| CA2799579A1 (en) | 2010-05-21 | 2011-11-24 | Intellikine, Inc. | Chemical compounds, compositions and methods for kinase modulation |
| WO2011163195A1 (en) | 2010-06-21 | 2011-12-29 | Incyte Corporation | Fused pyrrole derivatives as pi3k inhibitors |
| UA112517C2 (uk) * | 2010-07-06 | 2016-09-26 | Новартіс Аг | Тетрагідропіридопіримідинові похідні |
| ES2536780T3 (es) | 2010-07-14 | 2015-05-28 | F. Hoffmann-La Roche Ag | Compuestos de purina selectivos para I3 p110 delta, y métodos de uso |
| CA2812091C (en) | 2010-09-14 | 2020-03-24 | Exelixis, Inc. | Inhibitors of pi3k-delta and methods of their use and manufacture |
| EP2616442B8 (en) | 2010-09-14 | 2018-10-17 | Exelixis, Inc. | Inhibitors of pi3k-delta and methods of their use and manufacture |
| ES2637113T3 (es) | 2011-01-10 | 2017-10-10 | Infinity Pharmaceuticals, Inc. | Procedimientos para preparar isoquinolinonas y formas sólidas de isoquinolinonas |
| US9108984B2 (en) | 2011-03-14 | 2015-08-18 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors |
| US9090628B2 (en) | 2011-03-21 | 2015-07-28 | Genentech, Inc. | Benzoxazepin compounds selective for PI3K P110 delta and methods of use |
| WO2012135009A1 (en) | 2011-03-25 | 2012-10-04 | Incyte Corporation | Pyrimidine-4,6-diamine derivatives as pi3k inhibitors |
| AU2012236722A1 (en) | 2011-03-28 | 2013-10-17 | Mei Pharma, Inc. | (alpha-substituted cycloalkylamino and heterocyclylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, pharmaceutical compositions thereof, and their use in treating proliferative diseases |
| UY34013A (es) | 2011-04-13 | 2012-11-30 | Astrazeneca Ab | ?compuestos de cromenona con actividad anti-tumoral?. |
| EP2518071A1 (en) | 2011-04-29 | 2012-10-31 | Almirall, S.A. | Imidazopyridine derivatives as PI3K inhibitors |
| EP2518070A1 (en) | 2011-04-29 | 2012-10-31 | Almirall, S.A. | Pyrrolotriazinone derivatives as PI3K inhibitors |
| CN103987699A (zh) * | 2011-10-21 | 2014-08-13 | 诺华股份有限公司 | 作为pi3k调节剂的喹唑啉衍生物 |
| EP2790705B1 (en) | 2011-12-15 | 2017-12-06 | Novartis AG | Use of inhibitors of the activity or function of pi3k |
-
2012
- 2012-12-14 EP EP12818825.7A patent/EP2790705B1/en active Active
- 2012-12-14 MX MX2014007164A patent/MX351530B/es active IP Right Grant
- 2012-12-14 BR BR112014014327A patent/BR112014014327A2/pt not_active IP Right Cessation
- 2012-12-14 ES ES12818825.7T patent/ES2661510T3/es active Active
- 2012-12-14 EA EA201491182A patent/EA029473B1/ru not_active IP Right Cessation
- 2012-12-14 CA CA2857302A patent/CA2857302C/en active Active
- 2012-12-14 WO PCT/IB2012/057332 patent/WO2013088404A1/en not_active Ceased
- 2012-12-14 JP JP2014546719A patent/JP6117235B2/ja active Active
- 2012-12-14 CN CN201280062139.8A patent/CN103998042B/zh active Active
- 2012-12-14 HU HUE12818825A patent/HUE036052T2/hu unknown
- 2012-12-14 AU AU2012354094A patent/AU2012354094C1/en active Active
- 2012-12-14 PT PT128188257T patent/PT2790705T/pt unknown
- 2012-12-14 US US14/365,512 patent/US9949979B2/en active Active
- 2012-12-14 KR KR1020147019204A patent/KR102038462B1/ko active Active
- 2012-12-14 DK DK12818825.7T patent/DK2790705T3/en active
- 2012-12-14 SI SI201231220T patent/SI2790705T1/en unknown
- 2012-12-14 PL PL12818825T patent/PL2790705T3/pl unknown
- 2012-12-14 AP AP2014007679A patent/AP3849A/en active
-
2013
- 2013-07-04 NO NO13741876A patent/NO2896266T3/no unknown
-
2014
- 2014-05-23 TN TNP2014000230A patent/TN2014000230A1/en unknown
- 2014-06-13 GT GT201400114A patent/GT201400114A/es unknown
- 2014-06-13 PH PH12014501348A patent/PH12014501348A1/en unknown
- 2014-06-13 NI NI201400056A patent/NI201400056A/es unknown
- 2014-07-11 MA MA37198A patent/MA35857B1/fr unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ES2661510T3 (es) | Uso de inhibidores de la actividad o función de PI3K | |
| ES3013568T3 (en) | Substituted heteroaryl compounds useful as t cell activators | |
| ES2948194T3 (es) | Compuestos de pirazolo[1,5-a]pirazina sustituida como inhibidores de la cinasa RET | |
| KR102571130B1 (ko) | Alk 저해제 및 shp2 저해제를 포함하는 약제학적 조합 | |
| ES2872555T3 (es) | Inhibidores de HPK1 y métodos de uso de los mismos | |
| AU2025260019A1 (en) | Cyclin-dependent kinase 2 biomarkers and uses thereof | |
| Law et al. | Cyclin-dependent kinase inhibitors as anticancer therapeutics | |
| KR102652052B1 (ko) | 이미다졸로닐 퀴놀린 및 atm 키나아제 저해제로서의 이의 용도 | |
| ES2292130T3 (es) | Pirido(2,3-d)pirimidin-7-onas pirrolil-sustituidas y derivados de las mismas como agentes terapeuticos. | |
| ES2826448T3 (es) | Inhibidor de quinasa Aurora A | |
| KR102196424B1 (ko) | Hsp90 병용요법 | |
| ES2867505T3 (es) | Derivados de pirrolo[2,3-d]pirimidina como inhibidores de Janus quinasas | |
| ES2584331T3 (es) | Inhibidores de tirosina cinasa de Bruton | |
| JP6291132B2 (ja) | ブルートンチロシンキナーゼ阻害剤 | |
| TWI726017B (zh) | 做為布魯頓式酪胺酸激酶（ｂｔｋ）抑制劑之雜芳族化合物 | |
| US10130629B2 (en) | Pharmaceutical combinations | |
| BR112016007467B1 (pt) | Compostos heterocíclicos e usos dos mesmos | |
| Wang et al. | Pharmacokinetics-driven optimization of 4 (3 H)-pyrimidinones as phosphodiesterase type 5 inhibitors leading to TPN171, a clinical candidate for the treatment of pulmonary arterial hypertension | |
| KR20200015604A (ko) | C5a 억제제로서의 6-5 융합 고리 | |
| Faber et al. | Review of rationale and progress toward targeting cyclin-dependent kinase 2 (CDK2) for male contraception | |
| JP2020514361A (ja) | ９，１０，１１，１２−テトラヒドロ−８ｈ−［１，４］ジアゼピノ［５’，６’：４，５］チエノ［３，２−ｆ］キノリン−８−オン化合物およびその使用 | |
| UA77002C2 (en) | Combined therapy in cancer treatment | |
| ES3009460T3 (en) | Compounds for use in regulating follicle maturation | |
| Deng et al. | Modulating the interaction between CDK2 and cyclin A with a quinoline-based inhibitor | |
| CN109476669A (zh) | Lim激酶抑制剂 |