SI2668184T1 - Derivati vrste azaindazol ali diazaindazol kot zdravilo - Google Patents
Derivati vrste azaindazol ali diazaindazol kot zdravilo Download PDFInfo
- Publication number
- SI2668184T1 SI2668184T1 SI201231273T SI201231273T SI2668184T1 SI 2668184 T1 SI2668184 T1 SI 2668184T1 SI 201231273 T SI201231273 T SI 201231273T SI 201231273 T SI201231273 T SI 201231273T SI 2668184 T1 SI2668184 T1 SI 2668184T1
- Authority
- SI
- Slovenia
- Prior art keywords
- group
- compound
- compound according
- atom
- optionally substituted
- Prior art date
Links
- 239000003814 drug Substances 0.000 title claims abstract 5
- VQNDBXJTIJKJPV-UHFFFAOYSA-N 2h-triazolo[4,5-b]pyridine Chemical compound C1=CC=NC2=NNN=C21 VQNDBXJTIJKJPV-UHFFFAOYSA-N 0.000 title claims 2
- QRUDEWIWKLJBPS-UHFFFAOYSA-N benzotriazole Chemical class C1=CC=C2N[N][N]C2=C1 QRUDEWIWKLJBPS-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 24
- 239000000203 mixture Substances 0.000 claims abstract 6
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 4
- 150000003839 salts Chemical class 0.000 claims abstract 4
- 206010028980 Neoplasm Diseases 0.000 claims abstract 3
- 201000011510 cancer Diseases 0.000 claims abstract 3
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 claims abstract 2
- 206010061218 Inflammation Diseases 0.000 claims abstract 2
- 230000004054 inflammatory process Effects 0.000 claims abstract 2
- 229940043355 kinase inhibitor Drugs 0.000 claims abstract 2
- 238000000034 method Methods 0.000 claims abstract 2
- 230000004770 neurodegeneration Effects 0.000 claims abstract 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims abstract 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims abstract 2
- 239000012453 solvate Substances 0.000 claims abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 5
- DBTDEFJAFBUGPP-UHFFFAOYSA-N Methanethial Chemical compound S=C DBTDEFJAFBUGPP-UHFFFAOYSA-N 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 2
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 claims 2
- 102000001332 SRC Human genes 0.000 claims 2
- 108060006706 SRC Proteins 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- -1 (C 1 -C 6 alkyl Chemical group 0.000 claims 1
- 102000001253 Protein Kinase Human genes 0.000 claims 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 1
- 101100212791 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) YBL068W-A gene Proteins 0.000 claims 1
- 101100073357 Streptomyces halstedii sch2 gene Proteins 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 230000008878 coupling Effects 0.000 claims 1
- 238000010168 coupling process Methods 0.000 claims 1
- 238000005859 coupling reaction Methods 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 229940126601 medicinal product Drugs 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 229940079593 drug Drugs 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- 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
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (18)
- DERIVATI VRSTE AZAINDAZOL ALI DIAZAINDAZOL KOT ZDRAVILO Patentni zahtevki1. Spojina s sledečo splošno formulo (I):ali farmacevtsko sprejemljiva sol ali solvat le-te, tavtomer le-te ali steroizomer ali zmes stereoizomerov le-te v kakršnem koli razmerju, kot na primer zmes enantiomerov, predvsem racemna zmes, pri čemer: Yi in Y4 vsak predstavlja, neodvisno drug od drugega, CH skupino ali dušikov atom, Y2 predstavlja C-X-Ar skupino in Υ3 predstavlja dušikov atom ali C-W skupino, ali Υ2 predstavlja dušikov atom ali CH skupino in Υ3 predstavlja C-X-Ar skupino, pod pogojem, da: vsaj ena in največ dve Υι, Y2, Υ3 in Y4 skupini predstavljata dušikov atom, in Y2 in Y4 ne moreta sočasno predstavljati dušikov atom, Ar predstavlja aril ali heteroaril skupino, ki je izbirama substituirana z eno ali več skupinami, izbranimi med atomom halogena, (Ci-Cejalkilom, (Ci-Cejhaloalkilom, (Ci-C6)haloalkoksijem, (Ci-C6)halotioalkoksijem, CN, N02, ORu, SRi2, NR13R14, CO2R15, CONRieRiv, SOzRie, SO2NR19R20, COR21, NR22COR23, NR24S02R25 in R26NR27R28 in/ali je izbiroma spojena na heterocikel, X predstavlja divalentno skupino, ki je izbrana med O, S, S(O), S(0)2, NR4, S(NR4), S(0)(NR4), S(0)2(NR4), NR4S, NR4S(0), NR4S(0)2, CH2j CH2S, CH2S(0), CH2S(0)2, SCH2j S(0)CH2, S(0)2CH2, ch2ch2, ch=ch, oc, ch2o, och2, NR^CHz in CH2NR4, W predstavlja R5, SR5, ORs ali NR5R6 skupino, U predstavlja CH2 ali NH skupino, V predstavlja C(O), n predstavlja 0, Ri predstavlja atom vodika ali NR7Ra skupino,R2 predstavlja eno izmed naslednjih skupin: NH2, NH(CH2)3NMe2, NMe(CH2)3NMe2, N02, aliR3 predstavlja H, R4, R11 do R25 in R27 do R28 vsak predstavlja, neodvisno drug od drugega, atom vodika ali (Ci-C6)alkil skupino, Rs in R« vsak predstavlja, neodvisno drug od drugega, atom vodika ali (Ci-Ce)alkil, izbiroma substituirano aril ali izbiroma substituirano benzil skupino, - R7 in Ra vsak predstavlja, neodvisno drug od drugega, atom vodika ali izbiroma substituirano (Ci-C6)alkil ali (C3-Ci2)cikloalkil skupino ali izbiroma substituiran heterocikel, in Rae predstavlja (Ci-Csjalkil skupino.
- 2. Spojina po zahtevku 1, značilna po tem, da: Yi in/ali Y4 = N, Y2=CH ali C-X-Ar, in Y3=C-W ali C-X-Ar.
- 3. Spojina po bodisi zahtevku 1 bodisi zahtevku 2, značilna po tem, da X predstavlja divalentno skupino, izbrano med S, S(O), S(0)2, NR4, CH2, CH2S, CH2S(0), CH2S(0)2, CH20, CH2NR4, NHS(0)2, SCH2j S(0)CH2, S(0)2CH2, S(0)2NH, OCH2j NR4CH2, CH2CH2> CH=CH in OC; predvsem med S, S(0), S(0)2, Nil«, CH2, SCH2, S(0)CH2, S(0)2CH2, S(0)2NH, CH2CH2j C=C, OCH2 in NR4CH2, pri Čemer je prvi atom teh skupin vezan na C atom verige C-X-Ar.
- 4. Spojina po zahtevku 3, značilna po tem, da X predstavlja divalentno skupino, izbrano med S, S(0)2, CH2, SCH2, S(0)2CH2, S(0)2NH, CH2CH2 in C=C, pri čemer je prvi atom teh skupin vezan na C atom verige C-X-Ar.
- 5. Spojina po katerem koli od zahtevkov 1 do 4, značilna po tem, da Ar predstavlja aril skupino, kot je fenil, izbiroma substituirano z eno ali več skupinami, izbranimi med atomom halogena, (Ci-C6)alkilom, (Ci-C6)haloalkilom, (Ci-C6)haloalkoksijem, (Ci-C6)halotioalkoksijem, CN, N02, ORu, SR12, NR13Ri4, C02R1S, CONR16R17, S02R18, SO2NRi9R20, COR2i, NR22COR23 in NR24S02R2s; ali piridin skupino.
- 6. Spojina po zahtevku 5, značilna po tem, da Ar predstavlja skupino, izbrano med naslednjimi skupinami:
- 7. Spojina po katerem koli od zahtevkov 1 do 6, značilna po tem, da W predstavlja Rs, SRs, OR5 ali NR5Re skupino, kjer Rs in Re predstavljata, neodvisno drug od drugega, atom vodika ali (Ci-Cejalkil skupino.
- 8. Spojina po katerem koli od zahtevkov 1 do 7, značilna po tem, da R7 predstavlja atom halogena in Ra predstavlja izbiroma substituirano (C3-Ci2)cikloalkil skupino ali izbiroma substituiran heterocikel.
- 9. Spojina po katerem koli od zahtevkov 1 do 8, značilna po tem, da Ri predstavlja eno izmed naslednjih skupin:
- 10. Spojina po katerem koli od zahtevkov 1 do 9, značilna po tem, da je izbrana med naslednjimi spojinami:
- 11. Spojina po katerem koli od zahtevkov 1 do 10 za uporabo kot zdravilo.
- 12. Spojina po katerem koli od zahtevkov 1 do 10 za uporabo kot zdravilo, namenjeno zdravljenju raka, vnetja in nevrodegenerativnih bolezni, kot je Alzheimerjeva bolezen, zlasti raka.
- 13. Spojina po katerem koli od zahtevkov 1 do 10 za uporabo kot zaviralec kinaz, kot je ALK, Abl in/ali c-Src.
- 14. Spojina po katerem koli od zahtevkov 1 do 10 za uporabo kot zdravilo, namenjeno zdravljenju bolezni, povezanih s kinazo, kot so ALK, Abl in/ali c-Src.
- 15. Farmacevtska sestava, ki obsega vsaj eno spojino s formulo (I) po katerem koli od zahtevkov 1 do 10, in vsaj eno farmacevtsko sprejemljivo pomožno snov.
- 16. Farmacevtska sestava po zahtevku 15, ki dalje obsega vsaj eno drugo aktivno sestavino, kot je sredstvo proti raku.
- 17. Farmacevtska sestava, ki obsega: (i) vsaj eno spojino s formulo (I) po katerem koli od zahtevkov 1 do 10, (ii) vsaj eno drugo aktivno sestavino, kot je sredstvo proti raku, kot kombinirani izdelek za hkratno, ločeno ali zaporedno uporabo.
- 18. Postopek za pripravo spojine s formulo (I) po katerem koli od zahtevkov 1 do 10, ki obsega naslednje zaporedne korake: (al) vezanje med spojino z naslednjo formulo (Α):pri čemer so Υι, Υ2, Υ3 in Y4> kot so definirani v zahtevku 1, in R29 predstavlja atom vodika ali N-zaščitno skupino, s spojino z naslednjo formulo (Β):pri čemer so Ri, Ra, U, V in n, kot so definirani v zahtevku 1, in Rao=OH ali odhodna skupina, kot je Cl, da dobimo spojino z naslednjo formulo (C):pri čemer so Υι, Υ2, Υ3, Y4, Ri, R2, U, V in n, kot so definirani v zahtevku 1, in R29 je tak, kot je definiran zgoraj, (bi) izbiroma odstranitev zaščite atoma dušika, ki nosi R» skupino, ki predstavlja N-zaščitno skupino, da dobimo spojino s formulo (I), (cl) izbiroma tvorjenje soli spojine s formulo (I), pridobljene v predhodnem koraku, da dobimo farmacevtsko sprejemljivo sol le-te.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR1150651A FR2970967B1 (fr) | 2011-01-27 | 2011-01-27 | Derives de type azaindazole ou diazaindazole comme medicament |
| PCT/EP2012/051283 WO2012101239A1 (en) | 2011-01-27 | 2012-01-27 | Derivatives of azaindazole or diazaindazole type as medicament |
| EP12701884.4A EP2668184B1 (en) | 2011-01-27 | 2012-01-27 | Derivatives of azaindazole or diazaindazole type as medicament |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SI2668184T1 true SI2668184T1 (sl) | 2018-06-29 |
Family
ID=44318089
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SI201231273T SI2668184T1 (sl) | 2011-01-27 | 2012-01-27 | Derivati vrste azaindazol ali diazaindazol kot zdravilo |
Country Status (30)
| Country | Link |
|---|---|
| US (2) | US20130172360A1 (sl) |
| EP (1) | EP2668184B1 (sl) |
| JP (1) | JP5931926B2 (sl) |
| KR (2) | KR101923751B1 (sl) |
| CN (1) | CN103339129B (sl) |
| AR (1) | AR084935A1 (sl) |
| AU (1) | AU2012210467B2 (sl) |
| BR (1) | BR112013018852B1 (sl) |
| CA (1) | CA2823824C (sl) |
| CY (1) | CY1120088T1 (sl) |
| DK (1) | DK2668184T3 (sl) |
| ES (1) | ES2661695T3 (sl) |
| FR (1) | FR2970967B1 (sl) |
| HR (1) | HRP20180524T1 (sl) |
| HU (1) | HUE037153T2 (sl) |
| IL (2) | IL227496B (sl) |
| LT (1) | LT2668184T (sl) |
| MA (1) | MA34903B1 (sl) |
| MX (1) | MX356411B (sl) |
| MY (1) | MY180666A (sl) |
| PL (1) | PL2668184T3 (sl) |
| PT (1) | PT2668184T (sl) |
| RS (1) | RS57101B1 (sl) |
| RU (1) | RU2600976C2 (sl) |
| SI (1) | SI2668184T1 (sl) |
| TN (1) | TN2013000293A1 (sl) |
| TR (1) | TR201802944T4 (sl) |
| TW (1) | TWI546303B (sl) |
| UA (1) | UA109698C2 (sl) |
| WO (1) | WO2012101239A1 (sl) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| FR2970967B1 (fr) * | 2011-01-27 | 2013-02-15 | Pf Medicament | Derives de type azaindazole ou diazaindazole comme medicament |
| CA2865071C (en) * | 2012-02-22 | 2020-06-23 | Sanford-Burnham Medical Research Institute | Sulfonamide compounds and uses as tnap inhibitors |
| SMT201700146T1 (it) | 2012-06-13 | 2017-05-08 | Incyte Holdings Corp | Composti triciclici sostituiti come inibitori di fgfr |
| EP2689779A1 (en) * | 2012-07-27 | 2014-01-29 | Pierre Fabre Medicament | Derivatives of azaindazole or diazaindazole type for treating a cancer overexpressing trk |
| EP2689778A1 (en) * | 2012-07-27 | 2014-01-29 | Pierre Fabre Medicament | Derivatives of azaindoles or diazaindoles for treating pain |
| WO2014026125A1 (en) * | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| CA2909207C (en) | 2013-04-19 | 2021-11-02 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| US10336707B2 (en) | 2014-12-16 | 2019-07-02 | Eudendron S.R.L. | Heterocyclic derivatives modulating activity of certain protein kinases |
| UA121669C2 (uk) | 2015-02-20 | 2020-07-10 | Інсайт Корпорейшн | Біциклічні гетероцикли як інгібітори fgfr |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| US10211205B2 (en) * | 2016-04-27 | 2019-02-19 | International Business Machines Corporation | Field effect transistor structure for reducing contact resistance |
| CN108570052A (zh) * | 2017-03-13 | 2018-09-25 | 中国科学院上海药物研究所 | 五元杂环并吡嗪化合物、制备方法、中间体、组合和应用 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| CA3098988A1 (en) * | 2018-05-02 | 2019-11-07 | Jw Pharmaceutical Corporation | Heterocycle derivative |
| SMT202400507T1 (it) | 2018-05-04 | 2025-01-14 | Incyte Corp | Forme solide di un inibitore di fgfr e procedimenti per preparare le stesse |
| SG11202010882XA (en) | 2018-05-04 | 2020-11-27 | Incyte Corp | Salts of an fgfr inhibitor |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| EP3725777A1 (en) * | 2019-04-17 | 2020-10-21 | Rottapharm Biotech S.r.l. | Benzo- and pyrido-pyrazoles as protein kinase inhibitors |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CA3157361A1 (en) | 2019-10-14 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021113462A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Derivatives of an fgfr inhibitor |
| US11897891B2 (en) | 2019-12-04 | 2024-02-13 | Incyte Corporation | Tricyclic heterocycles as FGFR inhibitors |
| EP4085061A1 (en) * | 2019-12-31 | 2022-11-09 | IFM Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021197467A1 (zh) * | 2020-04-02 | 2021-10-07 | 上海华汇拓医药科技有限公司 | 多靶点的抗肿瘤化合物及其制备方法和应用 |
| CN116745268A (zh) * | 2020-11-20 | 2023-09-12 | 2692372安大略公司 | 苯磺酰胺衍生物及其用途 |
| CA3215903A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| EP4352060A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261160A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUP0001507A3 (en) * | 1997-03-19 | 2002-01-28 | Abbott Gmbh & Co Kg | Pyrrolo [2,3-d] pyrimidine derivatives, process for their preparation, their use and pharmaceutical compositions containing them |
| EP1215208B1 (en) | 1997-10-27 | 2006-07-12 | Agouron Pharmaceuticals, Inc. | 4-Aminothiazole derivatives, their preparation and their use as inhibitors of cyclin-dependent kinases |
| YU93902A (sh) | 2000-06-22 | 2005-11-28 | Pfizer Products Inc. | Postupak za pripremanje pirazolopirimidinona |
| WO2003068773A1 (en) * | 2002-02-12 | 2003-08-21 | Glaxo Group Limited | Pyrazolopyridine derivatives |
| DE102004061288A1 (de) * | 2004-12-14 | 2006-06-29 | Schering Ag | 3-Amino-Pyrazolo[3,4b]pyridine als Inhibitoren von Proteintyrosinkinasen, deren Herstellung und Verwendung als Arzneimittel |
| JP2009506006A (ja) * | 2005-08-25 | 2009-02-12 | エフ.ホフマン−ラ ロシュ アーゲー | p38MAPキナーゼ阻害剤およびその使用方法 |
| EP2044068A4 (en) | 2006-07-17 | 2010-07-21 | Merck Sharp & Dohme | 1-HYDROXY Naphthyridine Compounds as Anti- HIV Drugs |
| CA2673095C (en) | 2006-12-20 | 2016-03-15 | Nerviano Medical Sciences S.R.L. | Indazole derivatives as kinase inhibitors for the treatment of cancer |
| CA2693901C (en) | 2007-07-20 | 2015-12-29 | Nerviano Medical Sciences S.R.L. | Substituted indazole derivatives active as kinase inhibitors |
| ES2630026T3 (es) | 2008-12-18 | 2017-08-17 | Nerviano Medical Sciences S.R.L. | Derivados indazólicos sustituidos activos como inhibidores de cinasa |
| FR2970967B1 (fr) * | 2011-01-27 | 2013-02-15 | Pf Medicament | Derives de type azaindazole ou diazaindazole comme medicament |
-
2011
- 2011-01-27 FR FR1150651A patent/FR2970967B1/fr active Active
-
2012
- 2012-01-20 TW TW101102531A patent/TWI546303B/zh active
- 2012-01-27 US US13/823,658 patent/US20130172360A1/en not_active Abandoned
- 2012-01-27 EP EP12701884.4A patent/EP2668184B1/en active Active
- 2012-01-27 ES ES12701884.4T patent/ES2661695T3/es active Active
- 2012-01-27 KR KR1020137022330A patent/KR101923751B1/ko not_active Expired - Fee Related
- 2012-01-27 TR TR2018/02944T patent/TR201802944T4/tr unknown
- 2012-01-27 BR BR112013018852-9A patent/BR112013018852B1/pt not_active IP Right Cessation
- 2012-01-27 PL PL12701884T patent/PL2668184T3/pl unknown
- 2012-01-27 RU RU2013138624/04A patent/RU2600976C2/ru active
- 2012-01-27 PT PT127018844T patent/PT2668184T/pt unknown
- 2012-01-27 RS RS20180418A patent/RS57101B1/sr unknown
- 2012-01-27 UA UAA201310425A patent/UA109698C2/ru unknown
- 2012-01-27 MY MYPI2013002799A patent/MY180666A/en unknown
- 2012-01-27 CA CA2823824A patent/CA2823824C/en active Active
- 2012-01-27 AU AU2012210467A patent/AU2012210467B2/en not_active Ceased
- 2012-01-27 SI SI201231273T patent/SI2668184T1/sl unknown
- 2012-01-27 LT LTEP12701884.4T patent/LT2668184T/lt unknown
- 2012-01-27 DK DK12701884.4T patent/DK2668184T3/en active
- 2012-01-27 MA MA36177A patent/MA34903B1/fr unknown
- 2012-01-27 CN CN201280006671.8A patent/CN103339129B/zh active Active
- 2012-01-27 KR KR1020187031264A patent/KR20180122028A/ko not_active Ceased
- 2012-01-27 HU HUE12701884A patent/HUE037153T2/hu unknown
- 2012-01-27 HR HRP20180524TT patent/HRP20180524T1/hr unknown
- 2012-01-27 AR ARP120100272A patent/AR084935A1/es active IP Right Grant
- 2012-01-27 WO PCT/EP2012/051283 patent/WO2012101239A1/en not_active Ceased
- 2012-01-27 JP JP2013550886A patent/JP5931926B2/ja active Active
- 2012-01-27 MX MX2013008673A patent/MX356411B/es active IP Right Grant
- 2012-11-27 US US13/686,334 patent/US8883821B2/en active Active
-
2013
- 2013-07-11 TN TNP2013000293A patent/TN2013000293A1/fr unknown
- 2013-07-16 IL IL227496A patent/IL227496B/en active IP Right Grant
-
2018
- 2018-02-26 IL IL257748A patent/IL257748B/en active IP Right Grant
- 2018-03-26 CY CY20181100338T patent/CY1120088T1/el unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| SI2668184T1 (sl) | Derivati vrste azaindazol ali diazaindazol kot zdravilo | |
| HRP20170104T1 (hr) | Derivati tipa azaindazola ili diazaindazola za liječenje boli | |
| RU2403258C2 (ru) | Тиазолилдигидроиндазолы | |
| HRP20160967T1 (hr) | Heterociklički spojevi korisni kao pdk1 inhibitori | |
| RU2013148922A (ru) | Три- и тетрациклические пиразоло[3,4-в]пиридины в качестве антинеопластического средства | |
| RU2014141579A (ru) | Гетероциклические соединения в качестве ингибиторов бета-лактамаз | |
| JP2014503574A5 (sl) | ||
| RU2397168C2 (ru) | Производные тиофена в качестве ингибиторов снк 1 | |
| HRP20200538T1 (hr) | Derivati pirimidina za liječenje virusnih infekcija | |
| HRP20180212T1 (hr) | Derivati 1-fenil-2-piridinilalkil-alkohola kao inhibitori fosfodiesteraze | |
| JP2017511360A5 (sl) | ||
| JP2013523614A5 (sl) | ||
| RU2010121763A (ru) | Производные пиридазинона и ингибиторы р2х7 рецептора | |
| DE69925141D1 (de) | Chinazolin derivate | |
| RS51861B2 (sr) | Heterociklični inhibitori mek-a | |
| CA2572208A1 (en) | 3-carbamoyl-2-pyridone derivative | |
| JP2014510774A5 (sl) | ||
| SI3024819T1 (sl) | Glioksamid substituirani derivati pirolamida in njihova uporaba kot zdravila za zdravljenje hepatitisa B | |
| HRP20161786T1 (hr) | Pirolidinil urea, pirolidinil tiourea i pirolidinil gvanidin spojevi kao inhibitori trka kinaze | |
| RU2012142730A (ru) | Соединения, композиции и способы для снижения или устранения горького вкуса | |
| HRP20110156T1 (hr) | Monociklički heterocikli kao inhibitori kinaze | |
| RU2013149174A (ru) | Новое имидазооксазиновое соединение или его соль | |
| UY39032A (es) | Compuestos heterocíclicos como agentes antivirales | |
| HRP20171638T1 (hr) | Derivati pirazolin diona kao inhibitori nadph oksidaze | |
| PH12021552201A1 (en) | Benzodiazepine derivatives as rsv inhibitors |