REGJISTRI I OBJEKTEVE TE PRONESISE INDUSTRIALE

Lloji i Aplikimit
EPO patents
Nënlloji i Aplikimit
EPO Patent
(10) Numri dhe Data e Regjistrimit
6775 2017.09.29
Status
Regjistruar
(180) Data e mbarimit të afatit
2031.02.04
(20) Numri dhe Data e Depozitimit
AL/P/2017/352 2017.06.20
(40) Numri dhe Data e Publikimit
2017.10.24
(86) Data dhe Numri Ndërkombëtar i Depozitimit
11702449.7 2011.02.04
Status
Regjistruar
Data dhe Numri Ndërkombëtar i Publikimit
EP2534132 2017.04.26
(30) Detajet e Prioritetit
Kodi ID e prioritetit
CH 20100702402
(51) Klasat e KNP-së (IPC)
(71/73) Aplikanti
Aplikanti Adresa
F. Hoffmann-La Roche AG Grenzacherstrasse 124, 4070 Basel
(72) Shpikës
Emri Adresa
BARTKOVITZ, David Joseph 21 Povershon Road, Nutley, New Jersey 07110 , US
CHU, Xin-Jie 21 Riker Hill Road, Livingston, New Jersey 07039 , US
DING, Qingjie 23 Sterling Drive, Bridgewater, New Jersey 08807 , US
JIANG, Nan 12 Flanders Drive, Pine Brook, New Jersey 07058 , US
LIU, Jin-Jun 50 Highmount Avenue, Warren, New Jersey 07059 , US
ROSS, Tina Morgan 101 Rosemont Lane, Royersford, Pennsylvania 19468 , US
ZHANG, Jing 161 Carlton Drive, Parsippany, New Jersey 07054 , US
ZHANG, Zhuming 59 Wesley Road, Hillsborough, New Jersey 08844 , US
(74) Emri i Përfaqësuesit
Emri Adresa
Eno DODBIBA Rr. Naim FRASHERI, 60/3, Shk.1, Ap.16, Tirane, Shqiperi, AL , AL
Eno DODBIBA Rr. Naim FRASHERI, 60/3, Shk.1, Ap.16, Tirane, Shqiperi, AL , AL
(54) Titull
Pirrolidine-2-karboksamidat e zevendesuara
(57) Abstrakt
(58) Pretendime
Pretendim Përshkrim
1 Një përbërje e zgjedhur nga grupi i chiral [2-(4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-phenyl)-ethyl]-carbamic acid tert-butyl ester, rac-(4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-benzyl)-carbamic acid tert-butyl ester, 1-(4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-phenyl)-piperidine-4-carboxylic acid ethyl ester, 1-(4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-phenyl)-piperidine-4-carboxylic acid, rac-4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-4-methyl-piperidine-1-carboxylic acid tert-butyl ester, 4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-trifluoromethoxy-benzoic acid methyl ester, 4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-trifluoromethoxy-benzoic acid, 4-{[(2R,3S,4R,5S)-4-(4-chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid methyl ester, 4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-fluoro-benzoic acid methyl ester, 4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-chloro-benzoic acid methyl ester, 4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-trifluoromethoxy-benzoic acid, 4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-2,5-difluoro-benzoic acid methyl ester, 4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-2,5-difluoro-benzoic acid, 4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-2,6-difluoro-benzoic acid, 4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-hydroxy-benzoic acid, 4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-2-fluoro-5-methoxy-benzoic acid methyl ester, 4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-2-fluoro-5-methoxy-benzoic acid, rac-4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-2-ethoxy-benzoic acid, 5-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-pyrazine-2-carboxylic acid, 4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid dhe kripëra të pranueshme farmaceutikisht.
2 Përbërja sipas pretendimit 1, rac-4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-2-ethoxy-benzoic acid.
3 Përbërja sipas pretendimit 1, 5-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-pyrazine-2-carboxylic acid.
4 Përbërja sipas pretendimit 1, 4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid.
5 Një përgatitje farmaceutike që përfshin një përbërje sipas njërës prej pretendimeve 1 deri në 4 bashkë me mbushësit ose mbartësit e pranueshëm farmaceutikisht.
6 Një përbërje sipas pretendimeve 1 deri në 4 për përdorimin e saj si ilaç.
7 Një përbërje sipas njërit prej pretendimeve 1 deri në 4 për përdorimin e saj si ilaç për trajtimin e kancerit, në veçanti tumoreve solide, sidomos tumorit të gjoksit, zorrës së trashë, mushkërisë dhe prostatës.
8 Përdorimi i një përbërjeje sipas një prej pretendimeve nga 1 te 4 për prodhimin e një ilaçi për trajtimin e kancerit, në veçanti të tumoreve solidë.