HRP20211180T1 - Spojevi koji moduliraju androgeni receptor - Google Patents
Spojevi koji moduliraju androgeni receptor Download PDFInfo
- Publication number
- HRP20211180T1 HRP20211180T1 HRP20211180TT HRP20211180T HRP20211180T1 HR P20211180 T1 HRP20211180 T1 HR P20211180T1 HR P20211180T T HRP20211180T T HR P20211180TT HR P20211180 T HRP20211180 T HR P20211180T HR P20211180 T1 HRP20211180 T1 HR P20211180T1
- Authority
- HR
- Croatia
- Prior art keywords
- alkyl
- hydrogen
- compound
- image
- hydroxy
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims 15
- 102000001307 androgen receptors Human genes 0.000 title claims 5
- 108010080146 androgen receptors Proteins 0.000 title claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 35
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- 150000002431 hydrogen Chemical class 0.000 claims 9
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 9
- 125000003282 alkyl amino group Chemical group 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 238000000034 method Methods 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 230000001419 dependent effect Effects 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- -1 nitro, amino Chemical group 0.000 claims 3
- GMBPVBVTPBWIKC-NSHDSACASA-N 3-acetyl-n-[(2s)-1-[3-(3-chloro-4-cyanophenyl)pyrazol-1-yl]propan-2-yl]-1h-pyrazole-5-carboxamide Chemical compound C([C@H](C)NC(=O)C=1NN=C(C=1)C(C)=O)N(N=1)C=CC=1C1=CC=C(C#N)C(Cl)=C1 GMBPVBVTPBWIKC-NSHDSACASA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000001054 5 membered carbocyclic group Chemical group 0.000 claims 1
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims 1
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 claims 1
- 125000005189 alkyl hydroxy group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- BLIJXOOIHRSQRB-PXYINDEMSA-N n-[(2s)-1-[3-(3-chloro-4-cyanophenyl)pyrazol-1-yl]propan-2-yl]-5-(1-hydroxyethyl)-1h-pyrazole-3-carboxamide Chemical compound C([C@H](C)NC(=O)C=1NN=C(C=1)C(C)O)N(N=1)C=CC=1C1=CC=C(C#N)C(Cl)=C1 BLIJXOOIHRSQRB-PXYINDEMSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non 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
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D403/12—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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Claims (11)
1. Spoj koji je formule (VI)
[image]
pri čemu R1 je halogen, metil, cijano, nitro ili trifluorometil; R2 je cijano, halogen ili nitro; R3 je vodik, halogen ili metil; R4 je vodik ili metil; R5 je vodik ili C1-3 alkil,
R8 je vodik, hidroksi, halogen, nitro, amino, cijano, okso, C1-7 alkil, C1-7 alkoksi, halo C1-7 alkil, hidroksi C1-7 alkil, cijano C1-7 alkil, amino C1-7 alkil, okso C1-7 alkil, C1-7 alkoksi C1-7 alkil, metilsulfonamido C1-7 alkil, oksiran C1-7 alkil, C1-7 alkilamino, hidroksi C1-7 alkilamino, C1-7 alkoksi C1-7 alkilamino, C1-7 alkilamino C1-7 alkil, hidroksi C1-7 alkilamino C1-7 alkil, hidroksiimino C1-7 alkil, halo C1-7 alkilhidroksi C1-7 alkil, -C(O)R10, -OC(O)R17, -NH-C(O)R18 ili po potrebi supstituirani 5 - 12 člani karbociklični ili heterociklični prsten, svaka grupa po potrebi vezana za A-prsten preko C1-7 alkilenske spone;
R9 je vodik, halogen, C1-7 alkil, okso, hidroksi C1-7 alkil, okso C1-7 alkil ili po potrebi supstituiran 5 ili 6 člani karbociklični ili heterociklični prsten, svaka grupa po potrebi vezana za A-prsten preko C1-7 alkilen prstena;
R10 je vodik, hidroksi, C1-7 alkil, hidroksi C1-7 alkil, halo C1-7 alkil, C1-7 alkoksi, NR11R12, ili po potrebi supstituirani 5 - 12 člani karbociklični ili heterociklični prsten;
R11 je vodik, C1-7 alkil, hidroksi C1-7 alkil, amino C1-7 alkil, C1-7 alkil amino C1-7 alkil,
R12 je vodik ili C1-7 alkil;
R17 je C1-7 alkil, C1-7 alkoksi, amino C1-7 alkil ili C1-7 alkilamino C1-7 alkil;
R18 je C1-7 alkil, amino C1-7 alkil ili C1-7 alkilamino C1-7 alkil; ili je njegova farmaceutski prihvatljiva sol;
i pri čemu A je bilo koja od sljedećih grupa ili njihovih tautomera:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
2. Spoj prema zahtjevu 1, pri čemu je A jedna od grupa (5’), (6’), (7’), (8’), (12’), (20’), (21’), (27’) i (28’) ili njihovi tautomeri,
R8 je vodik, C1-7 alkil, hidroksi C1-7 alkil, halogen, piridinil, pirazolil, imidazolil, furanil, -C(O)R10 ili -OC(O)R17, pri čemu R10 je C1-7 alkil, R17 je C1-7 alkil, i R9 je vodik, halogen ili C1-7 alkil, i pri čemu piridinil, pirazolil, imidazolil, furanil, -C(O)R10, ili -OC(O)R17 grupe mogu biti vezane za A-prsten preko C1-7 alkilenske spone.
3. Spoj prema zahtjevu 2, pri čemu R1 je halogen, R2 je cijano; R3 je vodik, halogen ili metil; R4 je vodik, R5 je metil.
4. Farmaceutski sastav koji sadrži spoj prema bilo kojem od zahtjeva 1 do 3 zajedno sa farmaceutski prihvatljivim nosačem.
5. Spoj kao što je zahtjevano u bilo kojem od zahtjeva 1 do 3 za upotrebu u postupku za liječenje ili prevenciju poremećaja koji zavisi od androgenog receptora (AR), koji obuhvaća davanje subjektu kojem je potrebno terapeutski efikasne količine spomenutog spoja.
6. Spoj za upotrebu prema zahtjevu 5, gdje je stanje koje ovisi o androgenom receptoru karcinoma prostate.
7. Spoj za upotrebu prema zahtjevu 6, gdje je stanje koje ovisi od androgenog receptora karcinoma prostate rezistentan na kastraciju.
8. Postupak za dobivanje spoja prema bilo kojem od zahtjeva 1 do 3 koji obuhvaća reagiranje spojeva formule (16’)
[image]
gdje su R1, R2, R3, R4 i R5 kao što je definirano u zahtjevu 1, sa spojem formule (4)
[image]
pri čemu su R8, R9 i prsten A kao što je definirano u zahtjevu 1.
9. Postupak prema zahtjevu 8, gdje je dobiven optički aktivni enantiomer spoja prema bilo kojem od zahtjeva 1 do 3, koji obuhvaća reagiranje optički aktivnog enantiomera spoja formule (16’) sa spojem formule (4).
10. Postupak prema zahtjevu 9 za dobivanje (S)-3-acetil-N-(1-(3-(3-kloro-4-cijanofenil)-1H-pirazol-1-il)propan-2-il)-1H-pirazol-5-karboksamida ili njegovog tautomera.
11. Postupak prema zahtjevu 10, koji dalje obuhvaća konverziju (S)-3-acetil-N-(1-(3-(3-kloro-4-cijanofenil)-1H-pirazol-1-il)propan-2-il)-1H-pirazol-5-karboksamida ili njegovog tautomera u N-((S)-1-(3-(3-kloro-4-cijanofenil)-1H-pirazol-1-il)-propan-2-il)-3-(1-hidroksietil)-1H-pirazol-5-karboksamid ili njegov tautomer.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US25515909P | 2009-10-27 | 2009-10-27 | |
EP18163765.3A EP3369732B1 (en) | 2009-10-27 | 2010-10-27 | Androgen receptor modulating compounds |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20211180T1 true HRP20211180T1 (hr) | 2021-10-15 |
Family
ID=43383475
Family Applications (3)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20140919AT HRP20140919T1 (hr) | 2009-10-27 | 2014-09-26 | Spojevi koji moduliraju androgene receptore |
HRP20181229TT HRP20181229T1 (hr) | 2009-10-27 | 2018-07-31 | Spojevi koji moduliraju androgene receptore |
HRP20211180TT HRP20211180T1 (hr) | 2009-10-27 | 2021-07-22 | Spojevi koji moduliraju androgeni receptor |
Family Applications Before (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20140919AT HRP20140919T1 (hr) | 2009-10-27 | 2014-09-26 | Spojevi koji moduliraju androgene receptore |
HRP20181229TT HRP20181229T1 (hr) | 2009-10-27 | 2018-07-31 | Spojevi koji moduliraju androgene receptore |
Country Status (36)
Country | Link |
---|---|
US (5) | US8975254B2 (hr) |
EP (5) | EP2493858B1 (hr) |
JP (1) | JP5763083B2 (hr) |
KR (2) | KR101654529B1 (hr) |
CN (2) | CN102596910B (hr) |
AR (1) | AR078793A1 (hr) |
AU (1) | AU2010311299C1 (hr) |
BR (1) | BR112012008823B8 (hr) |
CA (1) | CA2777896C (hr) |
CL (1) | CL2012000772A1 (hr) |
CO (1) | CO6531494A2 (hr) |
CY (2) | CY2020010I1 (hr) |
DK (3) | DK2493858T3 (hr) |
EA (1) | EA021170B1 (hr) |
ES (3) | ES2486263T3 (hr) |
GE (1) | GEP20166472B (hr) |
HK (1) | HK1173442A1 (hr) |
HR (3) | HRP20140919T1 (hr) |
HU (2) | HUE039390T2 (hr) |
IL (2) | IL218586A (hr) |
LT (3) | LT3056485T (hr) |
LU (1) | LUC00154I2 (hr) |
MX (1) | MX2012004867A (hr) |
MY (1) | MY159924A (hr) |
NL (1) | NL301041I2 (hr) |
NO (1) | NO2020018I1 (hr) |
NZ (1) | NZ598747A (hr) |
PE (1) | PE20121058A1 (hr) |
PL (3) | PL3369732T3 (hr) |
PT (3) | PT2493858E (hr) |
RS (3) | RS53469B (hr) |
SI (3) | SI3369732T1 (hr) |
SM (1) | SMT201400138B (hr) |
UA (1) | UA109535C2 (hr) |
WO (1) | WO2011051540A1 (hr) |
ZA (1) | ZA201202655B (hr) |
Families Citing this family (42)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2012007500A2 (de) * | 2010-07-15 | 2012-01-19 | Bayer Cropscience Ag | Neue heterocyclische verbindungen als schädlingsbekämpfungsmittel |
EP2699561B1 (en) * | 2011-04-21 | 2015-06-03 | Orion Corporation | Androgen receptor modulating carboxamides |
EP2574607A1 (en) * | 2011-09-06 | 2013-04-03 | F. Hoffmann-La Roche AG | PDE10 modulators |
UA114194C2 (uk) * | 2012-03-15 | 2017-05-10 | Сігнал Фармасьютікалз, Елелсі | Лікування раку інгібітором тоr кінази |
TW201343644A (zh) * | 2012-03-23 | 2013-11-01 | Nihon Nohyaku Co Ltd | 噻唑羧醯胺衍生物及其使用方法 |
EP2862855A4 (en) | 2012-06-15 | 2015-11-18 | Taisho Pharmaceutical Co Ltd | HETERO-AROMATIC ALKYL RING DERIVATIVE WITH BRANCHED CHAINS |
ES2779748T3 (es) | 2012-08-23 | 2020-08-19 | Janssen Biopharma Inc | Compuestos para el tratamiento de infecciones víricas por paramixovirus |
CN102952095A (zh) * | 2012-10-19 | 2013-03-06 | 盛世泰科生物医药技术(苏州)有限公司 | 一种2-羧酸乙酯-5-溴甲基噻唑的合成方法 |
AU2014308991B2 (en) | 2013-08-21 | 2019-02-14 | Janssen Biopharma, Inc. | Antiviral compounds |
WO2015172196A1 (en) * | 2014-05-13 | 2015-11-19 | Monash University | Heterocyclic compounds and use of same |
US20170327469A1 (en) | 2015-01-20 | 2017-11-16 | Arvinas, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
WO2016118666A1 (en) | 2015-01-20 | 2016-07-28 | Arvinas, Inc. | Compounds and methods for the targeted degradation of the androgen receptor |
WO2016120530A1 (en) * | 2015-01-30 | 2016-08-04 | Orion Corporation | A carboxamide derivative and its diastereomers in stable crystalline form |
MA41614A (fr) * | 2015-02-25 | 2018-01-02 | Alios Biopharma Inc | Composés antiviraux |
RU2719590C2 (ru) * | 2015-04-09 | 2020-04-21 | Орион Корпорейшн | Способ получения антагонистов андрогенного рецептора и их промежуточных соединений |
US10392402B2 (en) * | 2015-05-18 | 2019-08-27 | Translational Drug Development, Llc | Heterocyclic compounds as kinase inhibitors |
EP3388428B1 (en) * | 2015-12-07 | 2021-08-04 | Suzhou Sinovent Pharmaceuticals Company | Five-membered heterocyclic amides wnt pathway inhibitor |
CN107286094A (zh) * | 2016-04-12 | 2017-10-24 | 常州爱诺新睿医药技术有限公司 | 一种bay-1841788与药用辅料的固体分散体及其制备方法 |
PT3495352T (pt) * | 2016-08-26 | 2021-05-03 | Crystal Pharmaceutical Suzhou Co Ltd | Formas de cristal de um antagonista de recetor de androgénio, método de preparação e utilização das mesmas |
KR102173463B1 (ko) | 2016-10-11 | 2020-11-04 | 아비나스 오퍼레이션스, 인코포레이티드 | 안드로겐 수용체의 표적 분해용 화합물 및 방법 |
WO2018162793A1 (en) * | 2017-03-07 | 2018-09-13 | Orion Corporation | Manufacture of a crystalline pharmaceutical product |
US11185549B2 (en) | 2017-06-28 | 2021-11-30 | Bayer Consumer Care Ag | Combination of a PI3K-inhibitor with an androgen receptor antagonist |
CN116396220A (zh) | 2017-08-09 | 2023-07-07 | 杭州领业医药科技有限公司 | Odm-201晶型及其制备方法和药物组合物 |
CN107602471B (zh) * | 2017-09-22 | 2021-04-27 | 成都恒汇化成医药科技有限公司 | 一种达罗鲁胺的晶型制备方法 |
WO2019166385A1 (en) | 2018-02-27 | 2019-09-06 | Sandoz Ag | Crystalline form ii of darolutamide |
WO2020035880A1 (en) * | 2018-08-13 | 2020-02-20 | National Centre For Biological Sciences-Tifr | Inhibitors to target hiv-1 nef-cd80/cd86 interactions for therapeutic intervention |
EP3876929A1 (en) | 2018-11-05 | 2021-09-15 | Pfizer Inc. | Combination for treating cancer |
EP3917519A1 (en) | 2019-01-30 | 2021-12-08 | Aragon Pharmaceuticals, Inc. | Anti-androgens for the treatment of metastatic castration-sensitive prostate cancer |
WO2020173457A1 (zh) * | 2019-02-27 | 2020-09-03 | 深圳市塔吉瑞生物医药有限公司 | 取代的吡唑类化合物及包含该化合物的组合物及其用途 |
CN114144168A (zh) | 2019-07-02 | 2022-03-04 | 奥赖恩公司 | 达鲁酰胺的药物组合物 |
CN110590668A (zh) * | 2019-07-17 | 2019-12-20 | 江苏君若医药有限公司 | N-[(1s)-2-[3-(3-氯-4-氰基苯基)-1h-吡唑-1-基]-1-甲基乙基]-5-(1-羟基乙基)- 1h-吡唑-3-甲酰胺的制备方法 |
KR20220047589A (ko) | 2019-08-08 | 2022-04-18 | 래크나 리미티드 | 암 치료 방법 |
CN111116476A (zh) * | 2019-12-27 | 2020-05-08 | 武汉九州钰民医药科技有限公司 | 制备抗肿瘤药物多拉米胺的方法 |
IL298047A (en) | 2020-05-11 | 2023-01-01 | Orion Corp | A method for the preparation of androgen receptor antagonists and their intermediates |
CA3188821A1 (en) | 2020-08-13 | 2022-02-17 | Lars ANDERS | Combination therapy |
CN111978534B (zh) * | 2020-09-07 | 2022-05-31 | 陕西师范大学 | 一种含苯并咪唑液晶基元的侧链型液晶离聚物及其制备方法 |
JP2024510666A (ja) | 2021-03-24 | 2024-03-08 | ファイザー・インク | Ddr遺伝子変異転移性去勢感受性前立腺がんを処置するためのタラゾパリブおよび抗アンドロゲンの組合せ |
CN113527208A (zh) * | 2021-08-31 | 2021-10-22 | 江西金丰药业有限公司 | 一步法制备2-氯-4-(1h-吡唑-3-基)苯甲腈的方法 |
CN113861115A (zh) * | 2021-09-10 | 2021-12-31 | 浙江师范大学 | 一种吡唑酰胺类衍生物及合成方法和应用 |
WO2023161458A1 (en) | 2022-02-28 | 2023-08-31 | Química Sintética, S.A. | Crystalline form of darolutamide |
WO2023194528A1 (en) | 2022-04-07 | 2023-10-12 | Astrazeneca Ab | Combination therapy for treating cancer |
WO2024074959A1 (en) | 2022-10-02 | 2024-04-11 | Pfizer Inc. | Combination of talazoparib and enzalutamide in the treatment of metastatic castration-resistant prostate cancer |
Family Cites Families (31)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
LU88769I2 (fr) | 1982-07-23 | 1996-11-05 | Zeneca Ltd | Bicalutamide et ses sels et esters pharmaceutiquement acceptables (Casodex (R)) |
FR2656609B1 (fr) | 1989-12-28 | 1992-03-27 | Synthelabo | Derives de 2-aminopyrimidine-4-carboxamide, leur preparation et leur application en therapeutique. |
US5578550A (en) | 1993-10-08 | 1996-11-26 | American Cyanamid Company | Herbicidal oxadiazole carbonamide compounds |
FR2741342B1 (fr) | 1995-11-22 | 1998-02-06 | Roussel Uclaf | Nouvelles phenylimidazolidines fluorees ou hydroxylees, procede, intermediaires de preparation, application comme medicaments, nouvelle utilisation et compositions pharmaceutiques |
AU754529B2 (en) | 1998-09-22 | 2002-11-21 | Yamanouchi Pharmaceutical Co., Ltd. | Cyanophenyl derivatives |
JP2005508978A (ja) | 2001-11-02 | 2005-04-07 | ファイザー・プロダクツ・インク | Pde9阻害薬によるインスリン抵抗性症候群及び2型糖尿病の治療 |
JP2005516964A (ja) * | 2001-12-28 | 2005-06-09 | バイエル・フアーマシユーチカルズ・コーポレーシヨン | 5−ht2cレセプターと関連する疾患における使用のための1h−ピラゾリル誘導体化合物 |
CA2471754A1 (en) | 2001-12-28 | 2003-07-17 | Takeda Chemical Industries, Ltd. | Androgen receptor antagonist |
AU2002364035A1 (en) * | 2001-12-28 | 2003-07-24 | Bayer Pharmaceuticals Corporation | 4-sulfide / sulfoxide / sulfonyl-1h-pyrazolyl derivative compounds, for use in diseases associated with the 5-ht2c receptor |
US20040180889A1 (en) | 2002-03-01 | 2004-09-16 | Pintex Pharmaceuticals, Inc. | Pin1-modulating compounds and methods of use thereof |
TW200406386A (en) * | 2002-06-07 | 2004-05-01 | Novartis Ag | Organic compounds |
KR20050034732A (ko) * | 2002-08-02 | 2005-04-14 | 아젠터 디스커버리 리미티드 | 히스톤 디아세틸라제 억제제로서의 치환된티에닐-히드록사믹산 |
DE10322108B4 (de) | 2003-05-09 | 2008-12-11 | Bayer Schering Pharma Aktiengesellschaft | Antiandrogene Pyrrolidine mit tumorhemmender Wirksamkeit |
US7271188B2 (en) | 2003-06-12 | 2007-09-18 | Chugai Seikayu Kabushiki Kaisha | Imidazolidine derivatives |
EP1663953A1 (en) | 2003-09-24 | 2006-06-07 | Methylgene, Inc. | Inhibitors of histone deacetylase |
EP1790640A4 (en) | 2004-09-09 | 2009-07-29 | Chugai Pharmaceutical Co Ltd | NEW IMIDAZOLIDINE DERIVATIVE AND APPLICATION THEREOF |
JP2008007405A (ja) * | 2004-12-07 | 2008-01-17 | Takeda Chem Ind Ltd | カルボキサミド誘導体 |
EP1710237A1 (en) * | 2005-04-08 | 2006-10-11 | Bayer CropScience S.A. | New heterocyclylethylbenzamide derivatives |
ES2535179T3 (es) | 2005-05-13 | 2015-05-06 | The Regents Of The University Of California | Compuesto de diarilhidantoína como antagonistas de los receptores de andrógenos para el tratamiento de cáncer |
US7709516B2 (en) | 2005-06-17 | 2010-05-04 | Endorecherche, Inc. | Helix 12 directed non-steroidal antiandrogens |
US20090227571A1 (en) | 2005-07-01 | 2009-09-10 | Ligand Pharmaceuticals Incorporated | Androgen Receptor Modulator Compounds and Methods |
GB0518237D0 (en) * | 2005-09-07 | 2005-10-19 | Angeletti P Ist Richerche Bio | Therapeutic compounds |
WO2007056155A1 (en) * | 2005-11-03 | 2007-05-18 | Chembridge Research Laboratories, Inc. | Heterocyclic compounds as tyrosine kinase modulators |
TW200800997A (en) | 2006-03-22 | 2008-01-01 | Astrazeneca Ab | Chemical compounds |
WO2008062878A1 (fr) | 2006-11-22 | 2008-05-29 | Nihon Nohyaku Co., Ltd. | Nouveau dérivé de pyrazole, agent de lutte contre des organismes nuisibles et utilisation de l'agent de lutte contre des organismes nuisibles |
WO2008124000A2 (en) * | 2007-04-02 | 2008-10-16 | Ligand Pharmaceuticals Incorporated | Thiazole derivatives as androgen receptor modulator compounds |
WO2009006404A2 (en) * | 2007-06-29 | 2009-01-08 | Sunesis Pharmaceuticals, Inc. | Heterocyclic compounds useful as raf kinase inhibitors |
EA201070323A1 (ru) | 2007-08-30 | 2010-10-29 | Такеда Фармасьютикал Компани Лимитед | Замещенное производное пиразола |
UY31432A1 (es) | 2007-10-26 | 2009-05-29 | Compuestos de diarilhidantoina | |
US20090270361A1 (en) | 2008-03-26 | 2009-10-29 | Takeda Pharmaceutical Company Limited | Substituted pyrazole derivatives and use thereof |
US20110306597A1 (en) * | 2008-06-18 | 2011-12-15 | James Michael Crawforth | Nicotinamide Derivatives |
-
2010
- 2010-10-26 AR ARP100103942A patent/AR078793A1/es active IP Right Grant
- 2010-10-27 PT PT107819187T patent/PT2493858E/pt unknown
- 2010-10-27 EP EP10781918.7A patent/EP2493858B1/en active Active
- 2010-10-27 PE PE2012000424A patent/PE20121058A1/es active IP Right Grant
- 2010-10-27 RS RS20140420A patent/RS53469B/en unknown
- 2010-10-27 SI SI201032078T patent/SI3369732T1/sl unknown
- 2010-10-27 HU HUE16157716A patent/HUE039390T2/hu unknown
- 2010-10-27 EP EP21169615.8A patent/EP3885340A1/en active Pending
- 2010-10-27 CN CN201080048340.1A patent/CN102596910B/zh active Active
- 2010-10-27 KR KR1020127013214A patent/KR101654529B1/ko active IP Right Grant
- 2010-10-27 PT PT181637653T patent/PT3369732T/pt unknown
- 2010-10-27 US US13/504,511 patent/US8975254B2/en active Active
- 2010-10-27 EP EP18163765.3A patent/EP3369732B1/en active Active
- 2010-10-27 HU HUE18163765A patent/HUE055528T2/hu unknown
- 2010-10-27 LT LTEP16157716.8T patent/LT3056485T/lt unknown
- 2010-10-27 PL PL18163765T patent/PL3369732T3/pl unknown
- 2010-10-27 RS RS20210903A patent/RS62123B1/sr unknown
- 2010-10-27 ES ES10781918.7T patent/ES2486263T3/es active Active
- 2010-10-27 ES ES18163765T patent/ES2877248T3/es active Active
- 2010-10-27 PL PL10781918T patent/PL2493858T3/pl unknown
- 2010-10-27 ES ES16157716.8T patent/ES2678073T3/es active Active
- 2010-10-27 DK DK10781918.7T patent/DK2493858T3/da active
- 2010-10-27 CA CA2777896A patent/CA2777896C/en active Active
- 2010-10-27 PT PT161577168T patent/PT3056485T/pt unknown
- 2010-10-27 SI SI201030739T patent/SI2493858T1/sl unknown
- 2010-10-27 NZ NZ598747A patent/NZ598747A/xx unknown
- 2010-10-27 BR BR112012008823A patent/BR112012008823B8/pt active IP Right Grant
- 2010-10-27 UA UAA201206302A patent/UA109535C2/ru unknown
- 2010-10-27 EA EA201270597A patent/EA021170B1/ru active Protection Beyond IP Right Term
- 2010-10-27 KR KR1020167023703A patent/KR101670299B1/ko active IP Right Grant
- 2010-10-27 EP EP16157716.8A patent/EP3056485B1/en active Active
- 2010-10-27 WO PCT/FI2010/000065 patent/WO2011051540A1/en active Application Filing
- 2010-10-27 DK DK18163765.3T patent/DK3369732T3/da active
- 2010-10-27 AU AU2010311299A patent/AU2010311299C1/en active Active
- 2010-10-27 PL PL16157716T patent/PL3056485T3/pl unknown
- 2010-10-27 EP EP14162075.7A patent/EP2754656A1/en not_active Withdrawn
- 2010-10-27 SI SI201031718T patent/SI3056485T1/en unknown
- 2010-10-27 GE GEAP201012722A patent/GEP20166472B/en unknown
- 2010-10-27 JP JP2012535889A patent/JP5763083B2/ja active Active
- 2010-10-27 MY MYPI2012001441A patent/MY159924A/en unknown
- 2010-10-27 RS RS20180913A patent/RS57592B1/sr unknown
- 2010-10-27 LT LTEP18163765.3T patent/LT3369732T/lt unknown
- 2010-10-27 MX MX2012004867A patent/MX2012004867A/es active IP Right Grant
- 2010-10-27 DK DK16157716.8T patent/DK3056485T3/en active
- 2010-10-27 CN CN201510501603.4A patent/CN105061313B/zh active Active
-
2012
- 2012-03-12 IL IL218586A patent/IL218586A/en active IP Right Grant
- 2012-03-28 CL CL2012000772A patent/CL2012000772A1/es unknown
- 2012-04-12 ZA ZA2012/02655A patent/ZA201202655B/en unknown
- 2012-04-27 CO CO12069611A patent/CO6531494A2/es active IP Right Grant
-
2013
- 2013-01-15 HK HK13100600.7A patent/HK1173442A1/zh unknown
-
2014
- 2014-09-23 SM SM201400138T patent/SMT201400138B/xx unknown
- 2014-09-26 HR HRP20140919AT patent/HRP20140919T1/hr unknown
-
2015
- 2015-01-16 US US14/598,973 patent/US9657003B2/en active Active
- 2015-03-30 IL IL238044A patent/IL238044A/en active IP Right Grant
-
2017
- 2017-04-13 US US15/486,995 patent/US10118933B2/en active Active
-
2018
- 2018-07-31 HR HRP20181229TT patent/HRP20181229T1/hr unknown
- 2018-09-25 US US16/140,716 patent/US10711013B2/en active Active
-
2020
- 2020-02-24 US US16/799,270 patent/US11046713B2/en active Active
- 2020-05-11 NL NL301041C patent/NL301041I2/nl unknown
- 2020-05-19 LU LU00154C patent/LUC00154I2/fr unknown
- 2020-06-05 CY CY2020010C patent/CY2020010I1/el unknown
- 2020-06-17 NO NO2020018C patent/NO2020018I1/no unknown
- 2020-06-26 LT LTPA2020514C patent/LTC2493858I2/lt unknown
-
2021
- 2021-07-22 HR HRP20211180TT patent/HRP20211180T1/hr unknown
- 2021-08-10 CY CY20211100717T patent/CY1124429T1/el unknown
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20211180T1 (hr) | Spojevi koji moduliraju androgeni receptor | |
RU2485131C2 (ru) | Производные пиридина, замещенные гетероциклическим кольцом и фосфоноксиметильной группой и содержащие их противогрибковые средства | |
JP2016538313A5 (hr) | ||
HRP20180382T1 (hr) | Inhibitori protein kinaze | |
RU2394031C2 (ru) | Соли четвертичного аммония в качестве антагонистов м3 | |
MX2009011487A (es) | Agentes antihipertensivos de doble accion. | |
HRP20211255T1 (hr) | Derivati pirana kao inhibitori cyp11a1 (citokrom p450 monooksigenaze 11a1) | |
MA31087B1 (fr) | Derives d'amide et d'ester d'indazolyle pour traiter des troubles medies par le recepteur de glucocorticoïde. | |
HRP20070505B1 (hr) | Spiro-oksindol spojevi i njihove upotrebe kao terapijska sredstva | |
ATE555099T1 (de) | Dual wirkende benzimidazol-derivate und deren verwendung als blutdrucksenkende mittel | |
TW200607504A (en) | Cinnamide compound | |
AR074426A1 (es) | Compuesto de n-(((1s,4s,6s)-3-(2-piridinilcarbonil)3-azabiciclo (4,1.0)hept-4-il) metil)-2-heteroarilamina, su uso para la prepracion de un medicamento para el tratamiento de una enfermedad que requiere un antagonista de un receptor de orexina humana y composicion farmaceutica que lo comprende | |
HRP20110938T1 (hr) | Spojevi koji sadrže gvanidin i koji se koriste kao agonisti muskarinskih receptora | |
CA2632771A1 (en) | Substituted imidazoles and their use as pesticides | |
MA28422B1 (fr) | Derives de n- (1,5-diphenyl-1h-pyrazol-3-yl) sulfonamide avec une affinite pour les recepteurs cb1 | |
HK1092152A1 (en) | Processes for preparing substituted n-aryl-n'-[3-(1h-pyrazol-5-yl)phenyl] ureas and intermediates thereof | |
MA37891B1 (fr) | Alcoxypyrazoles comme activateurs de guanylate cyclase soluble | |
MA31873B1 (fr) | Inhibiteurs de la peptide déformylase | |
MA35716B1 (fr) | Formulations pharmaceutiques | |
RU2017134379A (ru) | Формилированные n-гетероциклические производные в качестве ингибиторов fgfr4 | |
IL183373A0 (en) | 3-[2-(3-acylamino-2-oxo-2h-pyridin-1-yl)-acetylamino]-4-oxo-pentanoic acid derivatives, pharmaceutical compositions containing the same and methods for the preparation thereof | |
MA32150B1 (fr) | Inhibiteurs heterocycliques de la stearoyl-coa desaturase | |
NO20085271L (no) | Muscarin reseptoragonister som er effektive i behandling av smerte, Alzheimers sykdom og schizofreni | |
MA31742B1 (fr) | Derives de l'indol-2-one disubstitues en 3, leur preparation et leur application en therapeutique | |
MA46229B1 (fr) | Composés d'hétéroaryle carboxamide en tant qu'inhibiteurs de ripk2 |