HRP20150715T1 - C-19 steroidi za terapijske uporabe - Google Patents
C-19 steroidi za terapijske uporabe Download PDFInfo
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- HRP20150715T1 HRP20150715T1 HRP20150715TT HRP20150715T HRP20150715T1 HR P20150715 T1 HRP20150715 T1 HR P20150715T1 HR P20150715T T HRP20150715T T HR P20150715TT HR P20150715 T HRP20150715 T HR P20150715T HR P20150715 T1 HRP20150715 T1 HR P20150715T1
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- 230000001225 therapeutic effect Effects 0.000 title claims 3
- -1 C-19 steroids Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 26
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 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
- 101100134925 Gallus gallus COR6 gene Proteins 0.000 claims 4
- 206010060862 Prostate cancer Diseases 0.000 claims 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 4
- 125000002252 acyl group Chemical group 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000002677 5-alpha reductase inhibitor Substances 0.000 claims 3
- 230000002280 anti-androgenic effect Effects 0.000 claims 3
- 239000000051 antiandrogen Substances 0.000 claims 3
- 229940030495 antiandrogen sex hormone and modulator of the genital system Drugs 0.000 claims 3
- 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 2
- 102000014654 Aromatase Human genes 0.000 claims 2
- 108010078554 Aromatase Proteins 0.000 claims 2
- 108010066551 Cholestenone 5 alpha-Reductase Proteins 0.000 claims 2
- 102000001307 androgen receptors Human genes 0.000 claims 2
- 108010080146 androgen receptors Proteins 0.000 claims 2
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 2
- 230000015556 catabolic process Effects 0.000 claims 2
- 238000006731 degradation reaction Methods 0.000 claims 2
- 238000010511 deprotection reaction Methods 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- 150000002431 hydrogen Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 230000003449 preventive effect Effects 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- MEJYDZQQVZJMPP-ULAWRXDQSA-N (3s,3ar,6r,6ar)-3,6-dimethoxy-2,3,3a,5,6,6a-hexahydrofuro[3,2-b]furan Chemical compound CO[C@H]1CO[C@@H]2[C@H](OC)CO[C@@H]21 MEJYDZQQVZJMPP-ULAWRXDQSA-N 0.000 claims 1
- 102000006771 Gonadotropins Human genes 0.000 claims 1
- 108010086677 Gonadotropins Proteins 0.000 claims 1
- 230000001195 anabolic effect Effects 0.000 claims 1
- 230000000903 blocking effect Effects 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 239000002622 gonadotropin Substances 0.000 claims 1
- 201000000079 gynecomastia Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 239000002207 metabolite Substances 0.000 claims 1
- 230000028327 secretion Effects 0.000 claims 1
- 230000000699 topical effect Effects 0.000 claims 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- 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
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- 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
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- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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Claims (13)
1. Spoj izabran između spojeva koji imaju sljedeću formulu:
[image]
gdje
a, b i c odgovarajuće označavaju, nezavisno jedan od drugoga, jednostruku vezu ili dvostruku vezu, uz uvjet da barem jedan od a, b i c predstavlja dvostruku vezu, i uz uvjet da ako je a jednostruka veza i b je dvostruka veza, tada R2 nije H;
R1 je vodik ili C1 do C6 alkil;
R2 je OR5, gdje R5 je vodik ili C1 do C6 ravnolančani ili razgranati alkil;
R3 je, u slučaju da je c jednostruka veza, vodik ili C1 do C6 alkil, ili u slučaju da je c dvostruka veza, CHR5, gdje je R5 jednak kako je definirano ranije;
R4 je vodik, C1 do C6 alkil, fenil nesupstituiran ili supstituiran s C1 do C6 alkilom, COR6 acilnom skupinom (R6 je vodik; C1 do C6 ravnolančani ili razgranati alkil; odnosno fenil ili benzoil nesupstituiran ili supstituiran s C1 do C6 alkilom), ili bilo kojom skupinom koja vodi do hidroksila nakon biološke razgradnje ili kemijskog uklanjanja zaštite;
i njegove soli;
za uporabu u prevenciji i/ili liječenju karcinoma prostate.
2. Spoj za uporabu prema zahtjevu 1, gdje je spoj definiran time što su a i c jednostruka veza, b je dvostruka veza.
3. Spoj za uporabu prema bilo kojem od prethodnih zahtjeva, gdje se spoj koristi topikalno.
4. Spoj za uporabu prema bilo kojem od prethodnih zahtjeva, gdje se preventivnom i/ili terapijskom uporabom dobivaju
(i) blokirajući učinak na AR (androgen receptor) i
(ii) poboljšana anabolička aktivnost.
5. Spoj za uporabu prema bilo kojem od prethodnih zahtjeva, gdje se preventivnom i/ili terapijskom uporabom dobivaju sljedeći učinci ili svojstva, sami ili u kombinaciji:
(iii) aromataza ne aromatizira spoj;
(iv) 5α-reduktaza ne reducira spoj;
(v) spoj inhibira 5α-reduktazu;
(vi) u obliku svojeg C-17 oksidiranog metabolita, spoj pokazuje pojačanu inhibiciju aromataze.
6. Spoj za uporabu prema bilo kojem od prethodnih zahtjeva, gdje je spoj 4-hidroksitestosteron ili njegove soli ili esteri 4-hidroksitestosterona u kojima je R4 prema zahtjevu 1 COR6 acilna skupina kako je definirano u zahtjevu 1.
7. Spoj za uporabu prema zahtjevu 6, gdje ta uporaba za rezultat daje negativni odgovor na sekreciju gonadotropina.
8. Spoj za uporabu prema bilo kojem od prethodnih zahtjeva, gdje se spoj koristi prije, zajedno ili nakon liječenja raka prostate s lijekom izabranim iz grupe koja obuhvaća inhibitore 5α-reduktaze koji nisu spojevi prema zahtjevu 1, i anti-androgene, za kontrolu ginekomastije povezane s takvim liječenjem raka prostate.
9. Spoj za uporabu prema bilo kojem od prethodnih zahtjeva, u kombinaciji sa spojem izabranim iz grupe koja obuhvaća inhibitore 5α-reduktaze koji nisu spojevi prema zahtjevu 1, i anti-androgene.
10. Farmaceutski oblik za uporabu u prevenciji i/ili liječenju karcinoma prostate, oblik sadrži kombinaciju dimetil izosorbida i spoj izabran između spojeva koji imaju sljedeću formulu:
[image]
gdje
a, b i c odgovarajuće označavaju, nezavisno jedan od drugoga, jednostruku vezu ili dvostruku vezu, uz uvjet da barem jedan od a, b i c predstavlja dvostruku vezu, i uz uvjet da ako je a jednostruka veza i b je dvostruka veza, tada R2 nije H;
R1 je vodik ili C1 do C6 alkil;
R2 je OR5, gdje R5 je vodik ili C1 do C6 ravnolančani ili razgranati alkil;
R3 je, u slučaju da je c jednostruka veza, vodik ili C1 do C6 alkil, ili u slučaju da je c dvostruka veza, CHR5, gdje je R5 jednak kako je definirano ranije;
R4 je vodik, C1 do C6 alkil, fenil nesupstituiran ili supstituiran s C1 do C6 alkilom, COR6 acilnom skupinom (R6 je vodik; C1 do C6 ravnolančani ili razgranati alkil; odnosno fenil ili benzoil nesupstituiran ili supstituiran s C1 do C6 alkilom), ili bilo kojom skupinom koja vodi do hidroksila nakon biološke razgradnje ili kemijskog uklanjanja zaštite;
i njegove soli.
11. Farmaceutski oblik za uporabu prema zahtjevu 10, gdje je spoj 4-hidroksitestosteron ili njegove soli ili esteri 4-hidroksitestosterona u kojima je R4 prema zahtjevu 1 COR6 acilna skupina kako je definirano u zahtjevu 1.
12. Farmaceutski oblik za uporabu prema zahtjevu 10 ili 11 u topikalnom obliku.
13. Farmaceutski oblik prema bilo kojem od zahtjeva 10 do 12, dalje sadrži spoj izabran iz grupe koja obuhvaća inhibitore 5α-reduktaze inhibitors koji nisu spojevi prema zahtjevu 1, i anti-androgene.
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| US281707P | 2007-11-13 | 2007-11-13 | |
| EP07022016.5A EP2060300B1 (en) | 2007-11-13 | 2007-11-13 | C-19 steroids for therapeutic uses |
| EP20120194964 EP2564900B1 (en) | 2007-11-13 | 2008-11-12 | C-19 steroids for therapeutic uses |
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|---|---|
| HRP20150715T1 true HRP20150715T1 (hr) | 2015-08-14 |
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| HRP20150715TT HRP20150715T1 (hr) | 2007-11-13 | 2015-07-01 | C-19 steroidi za terapijske uporabe |
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| US (1) | US10265328B2 (hr) |
| EP (5) | EP2060300B1 (hr) |
| JP (1) | JP6025301B2 (hr) |
| KR (2) | KR20160036100A (hr) |
| CN (1) | CN101854979B (hr) |
| AU (1) | AU2008323199B2 (hr) |
| CA (1) | CA2705533C (hr) |
| CY (1) | CY1116496T1 (hr) |
| DK (4) | DK2949361T3 (hr) |
| ES (4) | ES2539800T3 (hr) |
| HK (1) | HK1148704A1 (hr) |
| HR (1) | HRP20150715T1 (hr) |
| HU (2) | HUE027440T2 (hr) |
| PL (4) | PL2500062T3 (hr) |
| PT (3) | PT2500062E (hr) |
| SI (1) | SI2564900T1 (hr) |
| WO (1) | WO2009062683A1 (hr) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| FR2964323B1 (fr) * | 2010-09-08 | 2012-11-09 | Jean Pierre Raynaud | Utilisation de la testosterone chez un patient en deficit androgenique et atteint d'un cancer de la prostate |
| DK2714006T3 (da) * | 2011-05-15 | 2021-03-15 | Acerus Biopharma Inc | Intranasale bioadhæsive testosterongelformuleringer og anvendelse deraf til behandling af mandlig hypogonadisme |
| AU2014252652A1 (en) * | 2013-04-10 | 2015-11-26 | Glycobiosciences, Inc. | Topical nutraceutical composition |
| NO3040075T3 (hr) * | 2014-12-30 | 2018-02-10 | ||
| EP3632445A1 (en) * | 2018-10-04 | 2020-04-08 | Curadis GmbH | Combinations with a c-19 steroid for treating cancers |
| CN112972465B (zh) * | 2021-02-22 | 2022-09-13 | 复旦大学附属中山医院 | 一种雄激素受体拮抗剂在制备治疗心血管疾病药物中的应用 |
| KR102554865B1 (ko) | 2021-10-05 | 2023-07-12 | 경상북도(농업기술원) | 친환경 덩굴 절단 파쇄장치 |
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| DE3121152A1 (de) * | 1981-05-22 | 1982-12-09 | Schering Ag, 1000 Berlin Und 4619 Bergkamen | "verwendung der kombination eines aromatase-hemmers mit einem antiandrogen zur prophylaxe und therapie der prostatahyperplasie" |
| JPS62132810A (ja) | 1985-12-05 | 1987-06-16 | Shiseido Co Ltd | 化粧料 |
| GB8721384D0 (en) | 1987-09-11 | 1987-10-21 | Erba Farmitalia | 17-substituted andro-sta-1 4-dien-3-one derivatives |
| US4895715A (en) * | 1988-04-14 | 1990-01-23 | Schering Corporation | Method of treating gynecomastia |
| GB9021546D0 (en) | 1990-10-04 | 1990-11-21 | Beecham Group Plc | Novel composition |
| JPH06502161A (ja) | 1990-10-31 | 1994-03-10 | ビーチャム・グループ・パブリック・リミテッド・カンパニー | レチノイド浸透作用エンハンサーを含む局所用組成物 |
| DE4405898A1 (de) | 1994-02-18 | 1995-08-24 | Schering Ag | Transdermale therapeutische Systeme enthaltend Sexualsteroide |
| US5824326A (en) | 1997-06-27 | 1998-10-20 | Chesebrough-Pond's Usa Co., Division Of Conopco, Inc. | Activity enhancement of ferulic acid with dimethyl isosorbride in cosmetic compositions |
| ATE501722T1 (de) * | 1999-09-30 | 2011-04-15 | Harbor Biosciences Inc | Therapeutische behandlung androgenrezeptorbedingter leiden |
| GB9930839D0 (en) | 1999-12-30 | 2000-02-16 | Pharmacia & Upjohn Spa | Process for treating gynecomastia |
| GB0012293D0 (en) | 2000-05-23 | 2000-07-12 | Astrazeneca Ab | Pharmaceutical combination |
| US6242436B1 (en) * | 2000-06-15 | 2001-06-05 | William Charles Llewellyn | Use of 5alpha-androstanediol or 5alpha-androstanedione to increase dihydrotestosterone levels in humans |
| AU2002330031B2 (en) * | 2001-09-21 | 2007-07-05 | Merck & Co., Inc. | Androstanes as androgen receptor modulators |
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| US20030229063A1 (en) | 2002-06-05 | 2003-12-11 | Llewellyn William Charles | Use of 4-hydroxytestosterone to lower estrogen levels in humans |
| CA2502209A1 (en) * | 2002-10-15 | 2004-04-29 | University Of Tennessee Research Foundation | Methylene-bridged selective androgen receptor modulators and methods of use thereof |
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| EP1692317A4 (en) | 2003-12-12 | 2007-12-19 | Univ Rochester | NON-ANDROGENO-DEPENDENT ROLES FOR ANDROGEN RECEPTOR AND NON-ANDROGENIC ASSOCIATED INHIBITORS OF ANDROGEN RECEPTOR |
| JP2008007404A (ja) * | 2004-10-08 | 2008-01-17 | Nippon Kayaku Co Ltd | 新規ピリジン誘導体 |
| WO2006083005A1 (ja) * | 2005-02-03 | 2006-08-10 | Takeda Pharmaceutical Company Limited | 縮合ピリミジン誘導体およびその用途 |
| WO2006084312A1 (en) | 2005-02-09 | 2006-08-17 | Acrux Dds Pty Ltd | Method of promoting hair growth |
| JP4755845B2 (ja) | 2005-04-28 | 2011-08-24 | 共栄化学工業株式会社 | テストステロン−５α−リダクターゼ阻害剤及びテストステロン−５α−リダクターゼ阻害剤を含有する化粧料。 |
| EP1854465A1 (en) * | 2006-05-12 | 2007-11-14 | Alexander Tobias Teichmann | Use of 4,17 beta-dihydroxyandrost-4-ene-3-one for treating cancers |
| ES2574933T3 (es) * | 2007-11-13 | 2016-06-23 | Athenion Ag | Esteroides de C-19 para usos cosméticos |
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