HRP20171875T1 - C-19 steroidi, namijenjeni inhibiranju neovaskulariziranja - Google Patents
C-19 steroidi, namijenjeni inhibiranju neovaskulariziranja Download PDFInfo
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- HRP20171875T1 HRP20171875T1 HRP20171875TT HRP20171875T HRP20171875T1 HR P20171875 T1 HRP20171875 T1 HR P20171875T1 HR P20171875T T HRP20171875T T HR P20171875TT HR P20171875 T HRP20171875 T HR P20171875T HR P20171875 T1 HRP20171875 T1 HR P20171875T1
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- 206010029113 Neovascularisation Diseases 0.000 title claims 2
- 230000002401 inhibitory effect Effects 0.000 title claims 2
- -1 C-19 steroids Chemical class 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 239000001257 hydrogen Substances 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000000217 alkyl group Chemical group 0.000 claims 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
- 150000002431 hydrogen Chemical class 0.000 claims 9
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 150000002148 esters Chemical class 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 238000011282 treatment Methods 0.000 claims 6
- BQOIJSIMMIDHMO-FBPKJDBXSA-N 4-Hydroxytestosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1O BQOIJSIMMIDHMO-FBPKJDBXSA-N 0.000 claims 4
- 108091008605 VEGF receptors Proteins 0.000 claims 4
- 239000000126 substance Substances 0.000 claims 4
- KPPVNWGJXFMGAM-UUILKARUSA-N (e)-2-methyl-1-(6-methyl-3,4-dihydro-2h-quinolin-1-yl)but-2-en-1-one Chemical compound CC1=CC=C2N(C(=O)C(/C)=C/C)CCCC2=C1 KPPVNWGJXFMGAM-UUILKARUSA-N 0.000 claims 3
- 125000006539 C12 alkyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 3
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 claims 3
- 125000002252 acyl group Chemical group 0.000 claims 3
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 3
- 230000004663 cell proliferation Effects 0.000 claims 3
- 238000010511 deprotection reaction Methods 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- 238000011321 prophylaxis Methods 0.000 claims 3
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 2
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 206010027476 Metastases Diseases 0.000 claims 2
- 229910019142 PO4 Inorganic materials 0.000 claims 2
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 2
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- 230000003074 vasoproliferative effect Effects 0.000 claims 1
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- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
- A61K31/5685—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
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Claims (11)
1. Spoj definiran formulom 1
[image]
,
gdje
a, b i c, međusobno neovisno, odgovarajuće označuju jednostruku vezu ili dvostruku vezu, uz uvjet da najmanje jedan od a, b i c predstavlja dvostruku vezu, te uz uvjet da ako je a jednostruka veza, a b je dvostruka veza, R2 nije H;
R1 je bilo vodik ili C1 do C6 alkil;
R2 je bilo OR5 ili vodik, gdje je R5 vodik ili C1 do C12 nerazgranati ili razgranati alkil;
R3 je, u slučaju ako je c jednostruka veza, bilo vodik ili C1 do C6 alkil, ili u slučaju ako je c dvostruka veza, CHR5, gdje je R5 isti kao što je definirano ranije;
R4 je vodik, C1 do C12 alkil, fenil koji nije supstituiran ili je supstituiran s C1 do C12 alkilnom ili COR6 acilnom skupinom; R6 je vodik, C1 do C12 nerazgranati ili razgranati alkil, fenil ili benzoil, koji odgovarajuće nije supstituiran ili je supstituiran s C1 do C12 alkilnom, ili bilo kojom skupinom koja se pretvara u hidroksilnu biološkim metaboliziranjem ili kemijskim uklanjanjem zaštite, osobito estera, etera, acetala, karbonata, karbamata, fosfata, fosfonata, ketala, sulfata ili sulfonata; i njihovih soli,
naznačen time što je namijenjen upotrebi u medicinskom liječenju kao inhibitor angiogeneze, gdje je navedeni spoj 4-hidroksitestosteron, ili njegove soli ili esteri.
2. Spoj definiran formulom 1
[image]
,
gdje
a, b i c, međusobno neovisno, odgovarajuće označuju jednostruku vezu ili dvostruku vezu, uz uvjet da najmanje jedan od a, b i c predstavlja dvostruku vezu, te uz uvjet da ako je a jednostruka veza, a b je dvostruka veza, R2 nije H;
R1 je bilo vodik ili C1 do C6 alkil;
R2 je bilo OR5 ili vodik, gdje je R5 vodik ili C1 do C12 nerazgranati ili razgranati alkil;
R3 je, u slučaju ako je c jednostruka veza, bilo vodik ili C1 do C6 alkil, ili u slučaju ako je c dvostruka veza, CHR5, gdje je R5 isti kao što je definirano ranije;
R4 je vodik, C1 do C12 alkil, fenil koji nije supstituiran ili je supstituiran s C1 do C12 alkilnom ili COR6 acilnom skupinom; R6 je vodik, C1 do C12 nerazgranati ili razgranati alkil, fenil ili benzoil, koji odgovarajuće nije supstituiran ili je supstituiran s C1 do C12 alkilnom, ili bilo kojom skupinom koja se pretvara u hidroksilnu biološkim metaboliziranjem ili kemijskim uklanjanjem zaštite, osobito estera, etera, acetala, karbonata, karbamata, fosfata, fosfonata, ketala, sulfata ili sulfonata; i njihovih soli,
naznačen time što je namijenjen upotrebi u skladu s patentnim zahtjevom 1, u terapiji upale i/ili raka inhibiranjem proliferacije ili sinteze, bilo sam ili u kombinaciji: proliferacije stanica endotela, proliferacije stanica glatkih mišića, migracije stanica endotela, proliferacije stanica glatkih mišića, čimbenika rasta endotela krvnih žila, receptora čimbenika rasta endotela krvnih žila, receptora 13 čimbenika rasta fibroblasta, receptor α i/ili β čimbenika rasta iz trombocita, te receptora čimbenika rasta mastocita/matičnih stanica, gdje je navedeni spoj 4-hidroksitestosteron, ili njegove soli ili esteri.
3. Spoj namijenjen upotrebi u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što je namijenjen upotrebi kao inhibitor neovaskulariziranja kod patološkog stanja koje uključuje regenerativne procese.
4. Spoj namijenjen upotrebi u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što je namijenjen sprječavanju ili inhibiranju vaskulariziranja u upalnom stanju, osobito kada se upalno stanje bira iz skupine koju čine artritis, upalne bolesti crijeva, egzem, te neurodermatitis.
5. Spoj namijenjen upotrebi u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što je namijenjen sprječavanju ili inhibiranju vaskulariziranja potaknutog tumorom, osobito kada je potaknuto rakom dojke ili rakom prostate.
6. Spoj namijenjen upotrebi u skladu s bilo kojim od prethodnih patentnih zahtjeva 1 do 5, naznačen time što je namijenjen profilaksi ili liječenju čvrstog tumora, po mogućnosti koji se bira iz skupine koju čine rak bubrega, kolorektalni rak, rak pluća, rak na mozgu, rak jajnika, rak gušterače i limfom, te njihove metastaze; ili u profilaksi ili liječenju nečvrstog tumora, po mogućnosti multiplog mijeloma, ili njegovih metastaza.
7. Spoj namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što je namijenjen upotrebi u profilaksi ili liječenju bolesti ili stanja koje se bira između:
• vaskularnih ili vazoproliferativnih novotvorina, po mogućnosti tumor stanica endotela, a osobito hemangioma,
• bolesti povezanih s očima, osobito gdje se bolest povezanu s očima bira iz skupine koju čine retinopatija, degeneracija makule, upala oka, vaskulariziranje rožnice, vaskularna injekcija u staklasto tijelo, te vaskulariziranje očne leće,
• zacjeljivanja rana, ili kod pretvorbe običnog funkcionalnog tkiva u meko tkivo, osobito kako bi se smanjilo prekomjerno nastajanje ožiljaka,
• malformacije žila, osobito protiv hemangioma u koži ili čvrstim organima,
• kardiovaskularnih bolesti, osobito hipertenzije, stenoze ili restenoze krvnih žila, arterioskleroze,
• pretilosti,
• endometrioze.
8. Farmaceutski pripravak, naznačen time što sadrži spoj formule u skladu s bilo kojim od prethodnih patentnih zahtjeva, gdje je navedeni spoj 4-hidroksitestosteron, ili njegove soli ili esteri, kao i farmaceutski prihvatljivu podlogu i/ili pomoćnu tvar, namijenjen upotrebi u medicinskom liječenju u skladu s bilo kojim od prethodnih patentnih zahtjeva.
9. Farmaceutski pripravak namijenjen upotrebi u skladu s patentnim zahtjevom 8, naznačen time što farmaceutski pripravak se pripravlja za dermalnu, mukoznu, submukoznu, transdermalnu, i.m., i.v., s.c, intradermalnu, oralnu, nazalnu, intraokularnu ili supozitorijsku primjenu ili ukapavanje u šupljine.
10. Kombinacija, naznačena time što sadrži:
(i) aktivnu tvar koju se bira iz skupine koju čine protutijela usmjerena protiv VEGF-a, VEGFR-a ili topljivih hibrida VEGFR/VEGFR, te inhibitori tirozinskih kinaza, i
(ii) spoj definiran formulom 1
[image]
,
gdje
a, b i c, međusobno neovisno, odgovarajuće označuju jednostruku vezu ili dvostruku vezu, uz uvjet da najmanje jedan od a, b i c predstavlja dvostruku vezu, te uz uvjet da ako je a jednostruka veza, a b je dvostruka veza, R2 nije H;
R1 je bilo vodik ili C1 do C6 alkil;
R2 je bilo OR5 ili vodik, gdje je R5 vodik ili C1 do C12 nerazgranati ili razgranati alkil;
R3 je, u slučaju ako je c jednostruka veza, bilo vodik ili C1 do C6 alkil, ili u slučaju ako je c dvostruka veza, CHR5, gdje je R5 isti kao što je definirano ranije;
R4 je vodik, C1 do C12 alkil, fenil koji nije supstituiran ili je supstituiran s C1 do C12 alkilnom ili COR6 acilnom skupinom;
R6 je vodik, C1 do C12 nerazgranati ili razgranati alkil, fenil ili benzoil, koji odgovarajuće nije supstituiran ili je supstituiran s C1 do C12 alkilnom, ili bilo kojom skupinom koja se pretvara u hidroksilnu biološkim metaboliziranjem ili kemijskim uklanjanjem zaštite, gdje je navedeni spoj 4-hidroksitestosteron, ili njegove soli ili esteri.
11. Kombinacija u skladu s patentnim zahtjevom 10, naznačena time što je namijenjena upotrebi u medicinskom liječenju u skladu s bilo kojim od prethodnih patentnih zahtjeva.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14200543.8A EP3040075B1 (en) | 2014-12-30 | 2014-12-30 | C-19 steroids for inhibiting neovascularization |
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| Publication Number | Publication Date |
|---|---|
| HRP20171875T1 true HRP20171875T1 (hr) | 2018-01-26 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20171875TT HRP20171875T1 (hr) | 2014-12-30 | 2017-12-04 | C-19 steroidi, namijenjeni inhibiranju neovaskulariziranja |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US10426785B2 (hr) |
| EP (2) | EP3040075B1 (hr) |
| JP (1) | JP6788592B2 (hr) |
| KR (1) | KR102481553B1 (hr) |
| CN (2) | CN107206010B (hr) |
| CA (1) | CA2972324C (hr) |
| DK (1) | DK3040075T3 (hr) |
| EA (2) | EA202190993A3 (hr) |
| ES (1) | ES2651442T3 (hr) |
| HR (1) | HRP20171875T1 (hr) |
| HU (1) | HUE037698T2 (hr) |
| NO (1) | NO3040075T3 (hr) |
| PL (1) | PL3040075T3 (hr) |
| PT (1) | PT3040075T (hr) |
| RS (1) | RS56621B1 (hr) |
| SI (1) | SI3040075T1 (hr) |
| WO (1) | WO2016107778A1 (hr) |
Families Citing this family (2)
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| EP3632445A1 (en) * | 2018-10-04 | 2020-04-08 | Curadis GmbH | Combinations with a c-19 steroid for treating cancers |
| CN114149923B (zh) * | 2021-11-19 | 2024-03-08 | 大连理工大学 | 内皮细胞-平滑肌细胞共培养的单流道微芯片模型的构建方法 |
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| US5504074A (en) * | 1993-08-06 | 1996-04-02 | Children's Medical Center Corporation | Estrogenic compounds as anti-angiogenic agents |
| KR20110118738A (ko) * | 2003-05-30 | 2011-10-31 | 제넨테크, 인크. | 항-ｖｅｇｆ 항체를 사용한 치료 |
| EP1756139A4 (en) * | 2004-03-12 | 2009-07-29 | Entremed Inc | ANTI-ANGIOGENIC AGENTS |
| US20060264413A1 (en) * | 2005-04-18 | 2006-11-23 | Sri International | Method and composition for inhibiting cell proliferation and angiogenesis |
| EP1854465A1 (en) * | 2006-05-12 | 2007-11-14 | Alexander Tobias Teichmann | Use of 4,17 beta-dihydroxyandrost-4-ene-3-one for treating cancers |
| PT2060300E (pt) * | 2007-11-13 | 2015-07-17 | Curadis Gmbh | Esteroides c-19 para usos terapêuticos |
| CN101619089B (zh) * | 2009-07-28 | 2011-07-20 | 陈大刚 | 抗肿瘤药物cl168、其合成方法及应用 |
-
2014
- 2014-12-30 PT PT142005438T patent/PT3040075T/pt unknown
- 2014-12-30 HU HUE14200543A patent/HUE037698T2/hu unknown
- 2014-12-30 DK DK14200543.8T patent/DK3040075T3/en active
- 2014-12-30 NO NO14200543A patent/NO3040075T3/no unknown
- 2014-12-30 RS RS20171258A patent/RS56621B1/sr unknown
- 2014-12-30 ES ES14200543.8T patent/ES2651442T3/es active Active
- 2014-12-30 SI SI201430519T patent/SI3040075T1/en unknown
- 2014-12-30 EP EP14200543.8A patent/EP3040075B1/en active Active
- 2014-12-30 PL PL14200543T patent/PL3040075T3/pl unknown
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2015
- 2015-12-21 EA EA202190993A patent/EA202190993A3/ru unknown
- 2015-12-21 US US15/535,461 patent/US10426785B2/en active Active
- 2015-12-21 CN CN201580071870.0A patent/CN107206010B/zh active Active
- 2015-12-21 EP EP15817308.8A patent/EP3215161A1/en not_active Withdrawn
- 2015-12-21 WO PCT/EP2015/080762 patent/WO2016107778A1/en active Application Filing
- 2015-12-21 EA EA201791209A patent/EA039485B1/ru unknown
- 2015-12-21 KR KR1020177018043A patent/KR102481553B1/ko active IP Right Grant
- 2015-12-21 JP JP2017535799A patent/JP6788592B2/ja active Active
- 2015-12-21 CA CA2972324A patent/CA2972324C/en active Active
- 2015-12-21 CN CN202110416346.XA patent/CN113117089A/zh active Pending
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Also Published As
| Publication number | Publication date |
|---|---|
| CN107206010A (zh) | 2017-09-26 |
| JP6788592B2 (ja) | 2020-11-25 |
| CN107206010B (zh) | 2021-12-21 |
| WO2016107778A1 (en) | 2016-07-07 |
| EA039485B1 (ru) | 2022-02-01 |
| PT3040075T (pt) | 2017-12-20 |
| HUE037698T2 (hu) | 2018-09-28 |
| JP2018508474A (ja) | 2018-03-29 |
| ES2651442T3 (es) | 2018-01-26 |
| RS56621B1 (sr) | 2018-03-30 |
| SI3040075T1 (en) | 2018-04-30 |
| US10426785B2 (en) | 2019-10-01 |
| NO3040075T3 (hr) | 2018-02-10 |
| EP3215161A1 (en) | 2017-09-13 |
| CA2972324C (en) | 2023-09-26 |
| CN113117089A (zh) | 2021-07-16 |
| CA2972324A1 (en) | 2016-07-07 |
| EA202190993A2 (ru) | 2021-08-31 |
| EA202190993A3 (ru) | 2021-10-29 |
| EP3040075B1 (en) | 2017-09-13 |
| KR20170100539A (ko) | 2017-09-04 |
| DK3040075T3 (en) | 2017-12-18 |
| PL3040075T3 (pl) | 2018-03-30 |
| EA201791209A1 (ru) | 2017-11-30 |
| US20170360804A1 (en) | 2017-12-21 |
| EP3040075A1 (en) | 2016-07-06 |
| KR102481553B1 (ko) | 2022-12-26 |
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