SI9520091B - Soli anti-migrenskega derivata indola - Google Patents
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Claims (16)
1 EP O 776 323 Bi SI 9520091 IE-1/967 PATENTNI ZAHTEVKI 1 Spojina, značilna po tem, da ima formulo (I): CH,
: HBr (I)
2. Kristalna α-polimorfna oblika spojine po zahtevku 1, značilna po tem, da infra-rdeči spekter pokaže znatne absorpcijske pasove pri v=3371, 3293, 2713, 2524, 1419, 1343, 1307, 1264, 1151, 1086, 1020, 1008, 999, 922, 900, 805, 758, 740, 728, 689, 672, 652, 640, 598, 581, 573, 531, 498, 465, 457, 443, 428, 422, 414 in 399 cm"1.
3. Spojina po zahtevku 2, značilna po tem, da je nadalje karakterizirana z rentgenskim difrakcijskim vzorcem praška, ki smo ga dobili z uporabo bakrene radiacije filtrirane z grafitnim monokromatorjem (λ=0.15405 nm) , ki je pokazala glavne vrhove pri 9.7, 10.7, 15.9, 16.5, 17.8, 18.3, 19.3, 19.8, 20.1, 21.2, 24.4, 25.5, 25.8, 26.7, 27.6 in 29.4 stopinjah 2Θ.
4. Kristalna β-polimorfna oblika spojine po zahtevku 1, značilna po tem, da ima infra-rdeči sprekter, ki je pokazal večje absorpcijske pasove pri v=3239, 2672, 2656, 2632, 1409, 1366, 1351, 1334, 1303, 1293, 1152, 1138, 1122, 1098, 1086, 791, 771, 746, 688, 634, 557, 528, 484, 476, 469, 463, 455, 432, 424, 413 in 401 cm"1. 2 .
5. Spojina po zahtevku 4, značilna po tem, da ima vzorec rentgenske analize praška, ki smo ga opravili z uporabo bakrene radiacije filtrirane z grafitnim monokromatorjem (λ=0.15405 nm), ki kaže glavne vrhove pri 11.0, 17.2, 19.2, 20.1, 21.6, 22.6, 23.6 in 24.8 stopinj 2Θ.
6. Farmacevtski sestavek, značilen po tem, da vključuje spojino po kateremkoli izmed zahtevkov 2 in 3, skupaj z farmacevtsko aktivnim topilom ali nosilcem.
7. Farmacevtski sestavek, po zahtevku 6, značilen po tem, da je v trdni dozirni obliki.
8. Spojina po kateremkoli izmed zahtevkov 2 in 3, ali farmacevtski sestavek po kateremkoli izmed zahtevkov 6 in 7, značilen po tem, da sta uporabna kot zdravilo.
9. Uporaba spojine po kateremkoli izmed zahtevkov 2 in 3, ali farmacevtskega sestavka po kateremkoli izmed zahtevkov 6 in 7, značilna po tem, da gre za izdelavo zdravila za kurativno ali profilaktično zdravljenje zdravstvenih stanj za katerega je indiciran selektivni agonist 5-HTi receptorjev.
10. Uporaba po zahtevku 9, značilna po tem, da je zdravstveno stanje migrena ali s to boleznijo povezano stanje kakršna so pogosti glavoboli, kronična paroksimalna hemikranija, glavoboli povezani s krvožilnimi nemiri ali depresija, tesnoba, hranilne motnje, debelost, zloraba zdravil, hipertenzija ali emeza. 3
11. Postopek za pripravo kristalne α-polimorfne oblike spojine s formulo (I):
značilen po tem, da ima infra rdeči spekter, ki kaže večje absorpcijske pasove pri v=3371, 3293, 2713, 2524, 1419, 1343, 1307, 1264, 1151, 1086, 1020, 1008, 999, 922, 900, 805, 758, 740, 728, 689, 672, 652, 640, 598, 581, 573, 531, 498, 465, 457, 443, 428, 422, 414 in 399 cm-1, ter vključuje: a) obdelavo raztopine spojine po formuli (II):
v prvem ustreznem topilu z vodno raztopino vodikovega bromida, čemur sledi kristalizacija izoliranega neprečiščenega olja iz drugega ustreznega topila; b) kristalizacija β-polimorfe oblike spojine po formuli (I), karakterizirane z infra rdečim spektrom, ki kaže glavne absorpcijske vrhove pri v=3239, 2672, 2656, 2632, 1409, 1366, 1351, 1334, 1303, 1293, 1152, 1138, 1122, 1098, 1086, 791, 771, 746, 688, 634, 557, 528, 484, 476, 469, 463, 455, 432, 424, 413 in 401 cm'1, iz ustreznega topila, čemur sledi ublatenje dobljene mešanice; ali 4 c) obdelava raztopine spojine po formuli (II) v ustreznem topilu z vodno mešanico vodikovega bromida ter nadaljnje ublatenje reakcijske mešanice, čemur neobvezno sledi segrevanje do obarjanja, hlajenje ter nadaljnje ublatenje.
12. Postopek po zahtevku 11, značilen po tem, da je a) prvo ustrezno topilo aceton, drugo ustrezno topilo 2-propanol, vodna raztopina vodikovega bromida pa je 49% utežnih odstotkgv, obravnavanje pa se izvaja pri 20-25°C; b) ustrezno topilo je vodni aceton; ter c) ustrezno topilo je aceton, vodna raztopina vodikovega bromida pa je 62% utežnih odstotkov, obravnavanje tega pa se izvaja pri 0 do 5°C.
13. Postopek po enem izmed zahtevkov 11 ali 12 značilen po tem, da je α-polimorfna oblika spojine po formuli (I) nadalje karakterizirana z vzorcem rentgenske difrakcije, kjer smo uporabili bakreno radiacijo filtrirano z grafitnim monokromatorjem (λ=0.15405 nm), ki je pokazala glavne vrhove pri 9.7, 10.7, 15.9, 16.5, 17.8, 18.3, 19.3, 19.8, 20.1, 21.2, 24.4, 25.5, 25.8, 26.7, 27.6 in 29.4 stopinjah 2Θ, β-polimorfna oblika spojine po formuli (I) pa je nadalje karakterizirana z vzorcem rentgenske difrakcije ki smo jo opravili z uporabo bakrene radiacije filtrirane preko grafitnega monokromatorj a (λ=0.15405 nm), ki kaže glavne vrhove pri 11.0, 17.2, 19.2, 20.1, 21.6, 22.6, 23.6 in 24.8 stopinjah 2Θ.
14. Postopek za pripravo kristalne β-polimorfične oblike spojine po formuli (I) po zahtevku 11 ali 13, značilen po tem, da vključuje obravnavanje raztopine spojine po 5 formuli (II) v ustreznem topilu z vodno raztopino vodikovega bromide.
15. Postopek po zahtevku 14, značilen po tem, da je ustrezno topilo aceton ali etersko topilo, kakršen je tetrahidrofuran ali 1,2-dimetoksietan, vodna raztopina vodikovega bromida je 49 utežnih odstotkov, obravnavanje pa se odvija pri 0 do 10°C.
16. Postopek po zahtevku 14 ali 15, značilen po tem, da je ustrezno topilo 1,2-dimetoksietan. za Pfizer Research and Development Company, N.V./S. A. Alexandra House, Earlsfort Centre Earlsfort Terrace, DUBLIN, IRSKA
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9417310A GB9417310D0 (en) | 1994-08-27 | 1994-08-27 | Therapeutic agents |
| PCT/EP1995/001914 WO1996006842A1 (en) | 1994-08-27 | 1995-05-17 | Salts of an anti-migraine indole derivative |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| SI9520091A SI9520091A (sl) | 1998-02-28 |
| SI9520091B true SI9520091B (sl) | 2004-10-31 |
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| Application Number | Title | Priority Date | Filing Date |
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| SI9520091A SI9520091B (sl) | 1994-08-27 | 1995-05-17 | Soli anti-migrenskega derivata indola |
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Families Citing this family (37)
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| GB9420529D0 (en) | 1994-10-12 | 1994-11-30 | Pfizer Ltd | Indoles |
| GB9706089D0 (en) * | 1997-03-24 | 1997-05-14 | Scherer Ltd R P | Pharmaceutical composition |
| CA2292673C (en) * | 1997-07-03 | 2003-04-22 | Pfizer Inc. | Pharmaceutical compositions containing eletriptan hemisulphate |
| GB9714081D0 (en) * | 1997-07-03 | 1997-09-10 | Pfizer Ltd | Pharmaceutical compositions |
| GB9816556D0 (en) * | 1998-07-30 | 1998-09-30 | Pfizer Ltd | Therapy |
| GB9825988D0 (en) * | 1998-11-27 | 1999-01-20 | Pfizer Ltd | Indole derivatives |
| GB9922963D0 (en) * | 1999-09-28 | 1999-12-01 | Pfizer Ltd | Polymorphic salt |
| GB9915231D0 (en) | 1999-06-29 | 1999-09-01 | Pfizer Ltd | Pharmaceutical complex |
| GB9923314D0 (en) | 1999-10-01 | 1999-12-08 | Pfizer Ltd | Acylation process |
| CA2324116A1 (en) * | 1999-10-25 | 2001-04-25 | Susan Beth Sobolov-Jaynes | Nk-1 receptor antagonists and eletriptan for the treatment of migraine |
| US7108970B2 (en) | 2000-01-07 | 2006-09-19 | Transform Pharmaceuticals, Inc. | Rapid identification of conditions, compounds, or compositions that inhibit, prevent, induce, modify, or reverse transitions of physical state |
| US6977723B2 (en) | 2000-01-07 | 2005-12-20 | Transform Pharmaceuticals, Inc. | Apparatus and method for high-throughput preparation and spectroscopic classification and characterization of compositions |
| GB0008563D0 (en) | 2000-04-07 | 2000-05-24 | Cambridge Discovery Chemistry | Investigating different physical and/or chemical forms of materials |
| GB0018968D0 (en) * | 2000-08-02 | 2000-09-20 | Pfizer Ltd | Particulate composition |
| US20030166704A1 (en) * | 2000-12-20 | 2003-09-04 | Pfizer Inc. | New process |
| US6579898B2 (en) | 2001-03-01 | 2003-06-17 | Pfizer Inc. | Compositions having improved bioavailability |
| MXPA05010070A (es) | 2003-04-11 | 2005-11-23 | Pfizer | Combinacion farmaceutica. |
| US7132549B2 (en) | 2003-05-30 | 2006-11-07 | Pfizer Inc. | Process |
| GB0312478D0 (en) * | 2003-05-30 | 2003-07-09 | Pfizer Ltd | Improved process |
| US6927296B2 (en) | 2003-07-23 | 2005-08-09 | Pfizer Inc. | Process |
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| US20080139510A1 (en) * | 2006-12-07 | 2008-06-12 | Abe Rose | Treatment of migraine headaches with sublingual amino acids |
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| US20100285075A1 (en) * | 2007-12-17 | 2010-11-11 | Actavis Group Ptc Ehf | Novel Hemioxalate Salt of Eletriptan |
| US20090299077A1 (en) * | 2008-05-22 | 2009-12-03 | Vinod Kumar Kansal | Salts of (R)-5-(2phenylsulphonylethenyl)-3-(N-methylpyrrolidin-2-ylmethyl)-1H-indole, 5-bromo-3-[(R)-1-methyl-pyrrolidin-2-ylmethyl]-1H-indole and of eletriptan |
| US8349900B2 (en) | 2008-08-07 | 2013-01-08 | Valeant International Bermuda | Bupropion hydrobromide polymorphs |
| US20120027816A1 (en) * | 2009-02-25 | 2012-02-02 | Actavis Group Ptc Ehf | Highly pure eletriptan or a pharmaceutically acceptable salt thereof substantially free of eletriptan n-oxide impurity |
| WO2010116386A2 (en) * | 2009-04-08 | 2010-10-14 | Biophore India Pharmaceuticals Pvt. Ltd. | Novel polymorph of eletriptan hydrobromide and process for the preparation thereof |
| IT1393700B1 (it) | 2009-04-22 | 2012-05-08 | F S I Fabbrica Italiana Sint | Sintesi di 3-{[(2r)-1-metilpirrolidin-2-il]metil}-5-[2-(fenilsulfonil)etil]-1h-indolo |
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| WO2014063752A1 (en) | 2012-10-26 | 2014-05-01 | Synthon Bv | Process for making crystalline form alpha of eletriptan hydrobromide |
| JP2019502761A (ja) | 2016-01-21 | 2019-01-31 | ラボラトリオス レヴィ エセエレ | （（ｒ）−３−［（−１−メチルピロリジン−２−イル）メチル］−５−（２−フェニルスルホニルエチル）−１ｈ−インドールを作製する方法 |
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| GB9210400D0 (en) * | 1992-05-15 | 1992-07-01 | Merck Sharp & Dohme | Therapeutic agents |
| FR2701026B1 (fr) * | 1993-02-02 | 1995-03-31 | Adir | Nouveaux dérivés de l'indole, de l'indazole et du benzisoxazole, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent. |
| EP0695301B1 (en) * | 1993-04-22 | 1996-10-30 | Pfizer Limited | Indole derivatives as 5-ht1-like agonists for use in migraine |
| AP486A (en) * | 1993-04-27 | 1996-04-16 | Pfizer | Indole derivatives. |
| CZ59996A3 (en) * | 1993-08-31 | 1996-06-12 | Pfizer | 5-arylindole derivatives per se and for treating diseases, intermediates for their preparation and pharmaceutical compositions based thereon |
-
1994
- 1994-08-27 GB GB9417310A patent/GB9417310D0/en active Pending
-
1995
- 1995-05-17 AU AU27352/95A patent/AU691005B2/en not_active Expired
- 1995-05-17 PL PL95318319A patent/PL180867B1/pl unknown
- 1995-05-17 KR KR1019970701281A patent/KR100228952B1/ko not_active IP Right Cessation
- 1995-05-17 WO PCT/EP1995/001914 patent/WO1996006842A1/en active IP Right Grant
- 1995-05-17 JP JP8508431A patent/JP2904588B2/ja not_active Expired - Lifetime
- 1995-05-17 RO RO97-00375A patent/RO116400B1/ro unknown
- 1995-05-17 DK DK95922465.0T patent/DK0776323T3/da active
- 1995-05-17 RU RU97104885/04A patent/RU2159241C2/ru active
- 1995-05-17 MX MX9701538A patent/MX9701538A/es active IP Right Grant
- 1995-05-17 US US08/776,680 patent/US6110940A/en not_active Expired - Lifetime
- 1995-05-17 CZ CZ1997563A patent/CZ287693B6/cs not_active IP Right Cessation
- 1995-05-17 DE DE69501620T patent/DE69501620T2/de not_active Expired - Lifetime
- 1995-05-17 SK SK248-97A patent/SK282922B6/sk not_active IP Right Cessation
- 1995-05-17 UA UA97031432A patent/UA45980C2/uk unknown
- 1995-05-17 CA CA002198599A patent/CA2198599C/en not_active Expired - Lifetime
- 1995-05-17 AT AT95922465T patent/ATE163182T1/de active
- 1995-05-17 NZ NZ288210A patent/NZ288210A/en not_active IP Right Cessation
- 1995-05-17 HU HU9701704A patent/HU227822B1/hu unknown
- 1995-05-17 SI SI9520091A patent/SI9520091B/sl unknown
- 1995-05-17 ES ES95922465T patent/ES2112650T3/es not_active Expired - Lifetime
- 1995-05-17 CN CN95194697A patent/CN1066727C/zh not_active Expired - Lifetime
- 1995-05-17 EP EP95922465A patent/EP0776323B1/en not_active Expired - Lifetime
- 1995-07-27 AP APAP/P/1995/000754A patent/AP576A/en active
- 1995-08-14 SA SA95160156A patent/SA95160156B1/ar unknown
- 1995-08-16 TN TNTNSN95092A patent/TNSN95092A1/fr unknown
- 1995-08-21 MA MA23992A patent/MA23650A1/fr unknown
- 1995-08-21 IL IL11501395A patent/IL115013A/xx not_active IP Right Cessation
- 1995-08-23 DZ DZ950104A patent/DZ1923A1/fr active
- 1995-08-23 PE PE1995277098A patent/PE41596A1/es not_active IP Right Cessation
- 1995-08-23 CO CO95037815A patent/CO4410334A1/es unknown
- 1995-08-25 HR HR9417310.1A patent/HRP950460B1/xx not_active IP Right Cessation
- 1995-08-25 BR BRPI9503812A patent/BRPI9503812B1/pt not_active IP Right Cessation
- 1995-08-25 MY MYPI95002536A patent/MY113733A/en unknown
- 1995-08-25 YU YU56995A patent/YU49287B/sh unknown
- 1995-08-25 TR TR95/01061A patent/TR199501061A2/xx unknown
- 1995-08-25 ZA ZA9507142A patent/ZA957142B/xx unknown
- 1995-08-26 EG EG71195A patent/EG23822A/xx active
-
1996
- 1996-12-19 IS IS4401A patent/IS1850B/is unknown
-
1997
- 1997-02-20 BG BG101250A patent/BG61840B1/bg unknown
- 1997-02-26 LV LVP-97-34A patent/LV11800B/en unknown
- 1997-02-26 NO NO19970861A patent/NO311297B1/no not_active IP Right Cessation
- 1997-02-26 FI FI970800A patent/FI113768B/fi not_active IP Right Cessation
- 1997-02-27 OA OA60969A patent/OA10600A/en unknown
-
1998
- 1998-03-27 GR GR980400660T patent/GR3026475T3/el unknown
-
2000
- 2000-06-15 US US09/596,017 patent/US6380226B1/en not_active Expired - Lifetime
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