HRP20161324T1 - Pripravci i postupci za povećavanje telomerazne aktivnosti - Google Patents

Pripravci i postupci za povećavanje telomerazne aktivnosti Download PDF

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HRP20161324T1
HRP20161324T1 HRP20161324TT HRP20161324T HRP20161324T1 HR P20161324 T1 HRP20161324 T1 HR P20161324T1 HR P20161324T T HRP20161324T T HR P20161324TT HR P20161324 T HRP20161324 T HR P20161324T HR P20161324 T1 HRP20161324 T1 HR P20161324T1
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image
compound according
hydroxy
amino
methyltetrahydrofuran
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HRP20161324TT
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Calvin B. Harley
Soo-Peang Khor
Mahesh Ramaseshan
Premchandran H. Ramiya
Zhu Zhen Pirot
Steven Fauce
Tong Lin
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Telomerase Activation Sciences, Inc.
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Publication of HRP20161324T1 publication Critical patent/HRP20161324T1/hr

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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
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    • C12N9/10—Transferases (2.)
    • C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • C12N9/1241—Nucleotidyltransferases (2.7.7)
    • C12N9/1276—RNA-directed DNA polymerase (2.7.7.49), i.e. reverse transcriptase or telomerase

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Claims (18)

1. Spoj formule I: [image] , naznačen time što se X1 bira između keto, hidroksi i [image] ; gdje se X2 bira između keto, hidroksi i [image] ; gdje se X3 bira između keto, hidroksi i [image] ; gdje je najmanje jedan od X1, X2 i X3 [image] , [image] odnosno [image] ; gdje se R1 ili R2 neovisno bira između -CH(CH3)2 i -CH(CH3)CH2CH3; i njegove farmaceutski prihvatljive soli.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je X1 -OC(O)CH(NH2)CH(CH3)2, a X2 i X3 su OH.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je X1 [image] , gdje se R1 bira iz skupine koju čine -CH(CH3)2 ili -CH(CH3)CH2CH3.
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je X2 [image] , gdje se R2 bira iz skupine koju čine -CH(CH3)2 ili -CH(CH3)CH2CH3.
5. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je X3 [image] .
6. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je najmanje jedan od X1, X2 ili X3 [image] .
7. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je najmanje jedan od X1 ili X2 -OC(O)CH(NH2)CH(CH3)CH2CH3-.
8. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je X1 -OC(O)CH(NH2)CH(CH3)CH2CH3, a X2 i X3 su -OH, X2 je -OC(O)CH(NH2)CH(CH3)2, a X1 i X3 su OH ili je X2 -OC(O)CH(NH2)CH(CH3)CH2CH3, a X1 i X3 su OH.
9. Spoj u skladu s patentnim zahtjevom 1, naznačen time što se bira iz skupine koju čine: [image] [image] [image] i [image] ; i njihove farmaceutski prihvatljive soli.
10. Spoj u skladu s patentnim zahtjevom 1, naznačen time što se bira iz skupine koju čine: 6α,16β-dihidroksi-17-[5-(1-hidroksi-1-metiletil)-2-metiltetrahidrofuran-2-il]-4,4,13,14-tetrametiltetradekahidrociklopropa[9,10]ciklopenta[a]fenantren-3β-ilni ester 2-(l)-amino-3-metilmaslačne kiseline; 6α-(2-amino-3-metilbutiriloksi)-16β-hidroksi-17-[5-(1-hidroksi-1-metiletil)-2-metiltetrahidrofuran-2-il]-4,4,13,14-tetrametiltetradekahidrociklopropa[9,10]ciklopenta[a]fenantren-3β-ilni ester 2-(l)-amino-3-metilmaslačne kiseline; 3β,16β-dihidroksi-17-[5-(1-hidroksi-1-metiletil)-2-metiltetrahidrofuran-2-il]-4,4,13,14-tetrametiltetradekahidrociklopropa[9,10]ciklopenta[a]fenantren-6α-ilni ester 2-(l)-amino-3-metilmaslačne kiseline; 6α,16β-dihidroksi-17-[5-(1-hidroksi-1-metiletil)-2-metiltetrahidrofuran-2-il]-4,4,13,14-tetrametiltetradekahidrociklopropa[9,10]ciklopenta[a]fenantren-3β-ilni ester 2-(l)-amino-3-metilpentanske kiseline; 16β-hidroksi-17-[5-(1-hidroksi-1-metiletil)-2-metiltetrahidrofuran-2-il]-4,4,13,14-tetrametil-3-okso-tetradekahidrociklopropa[9,10]ciklopenta[a]fenantren-6α-ilni ester 2-(l)-amino-3-metilmaslačne kiseline; 6α-(2-amino-3-metilpentanoiloksi)-16β-hidroksi-17-[5-(1-hidroksi-1-metiletil)-2-metiltetrahidrofuran-2-il]-4,4,13,14-tetrametiltetradekahidrociklopropa[9,10]ciklopenta[a]fenantren-3β-ilni ester 2-(l)-amino-3-metil pentanske kiseline; 3β,6α-dihidroksi-17-[5-(1-hidroksi-1-metiletil)-2-metiltetrahidrofuran-2-il]-4,4,13,14-tetrametiltetradekahidrociklopropa[9,10]ciklopenta[a]fenantren-16β-ilni ester 2-(l)-amino-3-metilmaslačne kiseline; i njihove farmaceutski prihvatljive soli.
11. Spoj u skladu s patentnim zahtjevima 1-10, naznačen time što je namijenjen upotrebi u povećavanju telomerazne aktivnosti u stanici ili tkivu.
12. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 11, naznačen time što se stanicu ili tkivo identificira prema potrebi za povećanom telomeraznom aktivnošću.
13. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s patentnim zahtjevima 1-10, u farmaceutski prihvatljivom vehikulumu.
14. Farmaceutski pripravak, naznačen time što sadrži topikalnu formulaciju spoja u skladu s patentnim zahtjevima 1-10.
15. Postupak povećavanja replikativne sposobnosti stanica ex vivo, naznačen time što se sastoji u stavljanju navedenih stanica u kontakt sa spojem u skladu s patentnim zahtjevima 1-10, u količini koja djelotvorno povećava telomeraznu aktivnost u navedenim stanicama.
16. Postupak u skladu s patentnim zahtjevom 15, naznačen time što su navedene stanice eksplantirane stanice dobivene iz pacijenta.
17. Spoj u skladu s patentnim zahtjevima 1-10, naznačen time što je namijenjen upotrebi u povećavanju replikativne sposobnosti stanica.
18. Spoj u skladu s patentnim zahtjevima 1-10, naznačen time što je namijenjen upotrebi u liječenju bolesti.
HRP20161324TT 2009-05-18 2016-10-11 Pripravci i postupci za povećavanje telomerazne aktivnosti HRP20161324T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US17930509P 2009-05-18 2009-05-18
PCT/US2010/035119 WO2010135247A1 (en) 2009-05-18 2010-05-17 Compositions and methods for increasing telomerase activity
EP10778210.4A EP2437606B1 (en) 2009-05-18 2010-05-17 Compositions and methods for increasing telomerase activity

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HRP20161324T1 true HRP20161324T1 (hr) 2016-11-18

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US (4) US8481721B2 (hr)
EP (1) EP2437606B1 (hr)
JP (1) JP5830013B2 (hr)
CN (2) CN104447936A (hr)
CA (1) CA2795981C (hr)
CY (1) CY1118073T1 (hr)
DK (1) DK2437606T3 (hr)
ES (1) ES2596631T3 (hr)
HR (1) HRP20161324T1 (hr)
HU (1) HUE030253T2 (hr)
LT (1) LT2437606T (hr)
PL (1) PL2437606T3 (hr)
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CN117247339B (zh) * 2023-11-16 2024-03-12 潍坊富邦药业有限公司 一种烷基胺衍生物的制备方法

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US20160318973A1 (en) 2016-11-03
US9403866B2 (en) 2016-08-02
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