SI9520091B - Soli anti-migrenskega derivata indola - Google Patents
Soli anti-migrenskega derivata indola Download PDFInfo
- Publication number
- SI9520091B SI9520091B SI9520091A SI9520091A SI9520091B SI 9520091 B SI9520091 B SI 9520091B SI 9520091 A SI9520091 A SI 9520091A SI 9520091 A SI9520091 A SI 9520091A SI 9520091 B SI9520091 B SI 9520091B
- Authority
- SI
- Slovenia
- Prior art keywords
- compound
- formula
- polymorphic form
- solvent
- suitable solvent
- Prior art date
Links
- 230000002460 anti-migrenic effect Effects 0.000 title 1
- 150000002475 indoles Chemical class 0.000 title 1
- 150000003839 salts Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 17
- 238000000034 method Methods 0.000 claims abstract 6
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 5
- 238000002360 preparation method Methods 0.000 claims abstract 2
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 claims 14
- 239000002904 solvent Substances 0.000 claims 13
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical group CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 8
- 229910000042 hydrogen bromide Inorganic materials 0.000 claims 7
- 239000007864 aqueous solution Substances 0.000 claims 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 4
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 claims 4
- XTHFKEDIFFGKHM-UHFFFAOYSA-N Dimethoxyethane Chemical compound COCCOC XTHFKEDIFFGKHM-UHFFFAOYSA-N 0.000 claims 4
- 238000010521 absorption reaction Methods 0.000 claims 4
- 229910052802 copper Inorganic materials 0.000 claims 4
- 239000010949 copper Substances 0.000 claims 4
- 229910002804 graphite Inorganic materials 0.000 claims 4
- 239000010439 graphite Substances 0.000 claims 4
- 238000002329 infrared spectrum Methods 0.000 claims 4
- 230000005855 radiation Effects 0.000 claims 4
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical group CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 3
- 239000000243 solution Substances 0.000 claims 3
- 238000011282 treatment Methods 0.000 claims 3
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
- 206010019233 Headaches Diseases 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- 238000002441 X-ray diffraction Methods 0.000 claims 2
- 238000002425 crystallisation Methods 0.000 claims 2
- 230000008025 crystallization Effects 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 238000010791 quenching Methods 0.000 claims 2
- 230000000171 quenching effect Effects 0.000 claims 2
- 102000035038 5-HT1 receptors Human genes 0.000 claims 1
- 108091005478 5-HT1 receptors Proteins 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 206010009094 Chronic paroxysmal hemicrania Diseases 0.000 claims 1
- 206010013654 Drug abuse Diseases 0.000 claims 1
- 208000030814 Eating disease Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010047700 Vomiting Diseases 0.000 claims 1
- 238000004458 analytical method Methods 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 239000010779 crude oil Substances 0.000 claims 1
- 238000009109 curative therapy Methods 0.000 claims 1
- 238000013016 damping Methods 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 231100000869 headache Toxicity 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 208000007777 paroxysmal Hemicrania Diseases 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 238000001556 precipitation Methods 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 239000011541 reaction mixture Substances 0.000 claims 1
- 239000000018 receptor agonist Substances 0.000 claims 1
- 229940044601 receptor agonist Drugs 0.000 claims 1
- 238000012827 research and development Methods 0.000 claims 1
- 239000007909 solid dosage form Substances 0.000 claims 1
- 208000011117 substance-related disease Diseases 0.000 claims 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Anesthesiology (AREA)
- Diabetes (AREA)
- Child & Adolescent Psychology (AREA)
- Nutrition Science (AREA)
- Toxicology (AREA)
- Otolaryngology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Crystals, And After-Treatments Of Crystals (AREA)
- Reciprocating, Oscillating Or Vibrating Motors (AREA)
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 |
Family
ID=10760474
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SI9520091A SI9520091B (sl) | 1994-08-27 | 1995-05-17 | Soli anti-migrenskega derivata indola |
Country Status (45)
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| GB9714081D0 (en) * | 1997-07-03 | 1997-09-10 | Pfizer Ltd | Pharmaceutical compositions |
| CN1145486C (zh) * | 1997-07-03 | 2004-04-14 | 美国辉瑞有限公司 | 含eletriptan半硫酸盐和咖啡因的药用组合物 |
| 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 |
| US20040252299A9 (en) | 2000-01-07 | 2004-12-16 | Lemmo Anthony V. | Apparatus and method for high-throughput preparation and spectroscopic classification and characterization of compositions |
| 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 |
| 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 |
| GB0031094D0 (en) * | 2000-12-20 | 2001-01-31 | Pfizer Ltd | New Process |
| 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 |
| WO2004089365A1 (en) | 2003-04-11 | 2004-10-21 | Pfizer Limited | Pharmaceutical combination comprising eletriptan and sodium bicarbonate |
| GB0312478D0 (en) * | 2003-05-30 | 2003-07-09 | Pfizer Ltd | Improved process |
| US7132549B2 (en) | 2003-05-30 | 2006-11-07 | Pfizer Inc. | Process |
| GB0317229D0 (en) * | 2003-07-23 | 2003-08-27 | Pfizer Ltd | Improved process |
| US6927296B2 (en) | 2003-07-23 | 2005-08-09 | Pfizer Inc. | Process |
| US7884136B2 (en) * | 2005-06-27 | 2011-02-08 | Biovail Laboratories International S.R.L. | Modified-release formulations of a bupropion salt |
| RU2313340C1 (ru) * | 2006-02-20 | 2007-12-27 | Дмитрий Владимирович Зимин | Лекарственное средство, обладающее противомигренозным действием, и способ его изготовления |
| ATE502921T1 (de) * | 2006-10-19 | 2011-04-15 | Auspex Pharmaceuticals Inc | Substituierte indole |
| US20080139510A1 (en) * | 2006-12-07 | 2008-06-12 | Abe Rose | Treatment of migraine headaches with sublingual amino acids |
| EP1956018A1 (de) * | 2007-02-06 | 2008-08-13 | Boehringer Ingelheim Pharma GmbH & Co. KG | Verfahren zur Herstellung eines Benzimidazolderivats |
| EP2093225A1 (en) | 2007-05-01 | 2009-08-26 | Plus Chemicals B.V. | Process for preparing crystalline eletriptan hydrobromide form ß |
| EP2038273A1 (en) * | 2007-05-29 | 2009-03-25 | Plus Chemicals B.V. | A process for preparing 5-bromo-3-[(r)-1-methyl-pyrrolidin-2-ylmethyl]-1h-indole |
| 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 |
| WO2010097703A1 (en) * | 2009-02-25 | 2010-09-02 | 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 |
| WO2011004391A2 (en) | 2009-06-25 | 2011-01-13 | Matrix Laboratories Ltd | An improved process for the preparation of eletriptan and its salt thereof |
| WO2011089614A1 (en) * | 2010-01-19 | 2011-07-28 | Sms Pharmaceuticals Limited | PROCESS FOR PREPARING ELETRIPTAN HYDROBROMIDE HAVING α-FORM |
| WO2014063752A1 (en) | 2012-10-26 | 2014-05-01 | Synthon Bv | Process for making crystalline form alpha of eletriptan hydrobromide |
| WO2017125351A1 (en) | 2016-01-21 | 2017-07-27 | Laboratorios Lesvi Sl | Process for preparing (( r)-3-[(-1-methylpyrrolidin-2-yl)methyl]-5-(2-phenylsulfonylethyl)-1h-indole |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2773875A (en) * | 1952-03-28 | 1956-12-11 | Hoffmann La Roche | Indole derivatives and method for producing same |
| GB886684A (en) * | 1957-09-17 | 1962-01-10 | Upjohn Co | Improvements in or relating to heterocyclic compounds and the manufacture thereof |
| GB851780A (en) * | 1958-02-25 | 1960-10-19 | Rhone Poulenc Sa | New indole derivatives |
| US3037031A (en) * | 1959-08-04 | 1962-05-29 | Warner Lambert Pharmaceutical | Derivatives of 3-(2-aminoalkyl)-5-indolol and process therefor |
| GB893707A (en) * | 1960-03-01 | 1962-04-11 | Roche Products Ltd | Novel tryptamine derivatives and a process for the manufacture thereof |
| GB966562A (en) * | 1961-04-06 | 1964-08-12 | Parke Davis & Co | Amine compounds and means of producing the same |
| US4092315A (en) * | 1976-03-01 | 1978-05-30 | Pfizer Inc. | Novel crystalline forms of prazosin hydrochloride |
| ZA795239B (en) * | 1978-10-12 | 1980-11-26 | Glaxo Group Ltd | Heterocyclic compounds |
| ZW19381A1 (en) * | 1980-08-12 | 1983-03-09 | Glaxo Group Ltd | Heterocyclic compounds |
| US4803218A (en) * | 1982-09-29 | 1989-02-07 | Mcneilab, Inc. | 3-aminoalkyl-1H-indole-5-urea and amide derivatives |
| GB8600397D0 (en) * | 1986-01-08 | 1986-02-12 | Glaxo Group Ltd | Chemical compounds |
| DK158590D0 (da) * | 1990-07-02 | 1990-07-02 | Lundbeck & Co As H | Indolderivater |
| US5559246A (en) * | 1990-10-15 | 1996-09-24 | Pfizer Inc. | Indole derivatives |
| US5545644A (en) * | 1990-10-15 | 1996-08-13 | Pfizer Inc. | Indole derivatives |
| US5559129A (en) * | 1990-10-15 | 1996-09-24 | Pfizer Inc | Indole derivatives |
| HU225055B1 (en) * | 1990-10-15 | 2006-05-29 | Pfizer | Indole derivatives, their intermediates, process for production them and pharmaceutical compositions containing the compounds |
| US5578612A (en) * | 1990-10-15 | 1996-11-26 | Pfizer Inc. | Indole derivatives |
| US5208248A (en) * | 1991-01-11 | 1993-05-04 | Merck Sharpe & Dohme, Ltd. | Indazole-substituted five-membered heteroaromatic compounds |
| SK278998B6 (sk) * | 1991-02-01 | 1998-05-06 | Merck Sharp & Dohme Limited | Deriváty imidazolu, triazolu a tetrazolu, spôsob i |
| EP0619805B1 (en) * | 1991-11-25 | 2000-03-15 | Pfizer Inc. | 5-(hetero- or carbocyclylamino)-indole derivatives, their preparation and their use as 5-ht1 agonists |
| GB9201038D0 (en) * | 1992-01-16 | 1992-03-11 | Glaxo Group Ltd | Chemical compounds |
| US5409941A (en) * | 1992-02-03 | 1995-04-25 | Pfizer Inc. | 5-heteroyl indole derivatives |
| TW288010B (sl) * | 1992-03-05 | 1996-10-11 | Pfizer | |
| JP2644088B2 (ja) * | 1992-04-07 | 1997-08-25 | フアイザー・インコーポレイテツド | 5−ht1作動薬としてのインドール誘導体 |
| DK0635015T3 (da) * | 1992-04-10 | 1997-03-17 | Pfizer | Acylaminoindolderivater som 5-Htl agonister |
| GB9207930D0 (en) * | 1992-04-10 | 1992-05-27 | Pfizer Ltd | Indoles |
| GB9208161D0 (en) * | 1992-04-14 | 1992-05-27 | Pfizer Ltd | Indoles |
| 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. |
| HUT73807A (en) * | 1993-04-22 | 1996-09-30 | Pfizer Res & Dev | 5-ht1-like indole derivatives and pharmaceutical compositions containing them |
| AP486A (en) * | 1993-04-27 | 1996-04-16 | Pfizer | Indole derivatives. |
| KR100191973B1 (ko) * | 1993-08-31 | 1999-06-15 | 디. 제이. 우드, 스피겔 알렌 제이 | 5-아릴인돌 유도체 |
-
1994
- 1994-08-27 GB GB9417310A patent/GB9417310D0/en active Pending
-
1995
- 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 CA CA002198599A patent/CA2198599C/en not_active Expired - Lifetime
- 1995-05-17 DE DE69501620T patent/DE69501620T2/de not_active Expired - Lifetime
- 1995-05-17 AU AU27352/95A patent/AU691005B2/en not_active Expired
- 1995-05-17 PL PL95318319A patent/PL180867B1/pl unknown
- 1995-05-17 NZ NZ288210A patent/NZ288210A/en not_active IP Right Cessation
- 1995-05-17 EP EP95922465A patent/EP0776323B1/en not_active Expired - Lifetime
- 1995-05-17 UA UA97031432A patent/UA45980C2/uk unknown
- 1995-05-17 HU HU9701704A patent/HU227822B1/hu unknown
- 1995-05-17 SI SI9520091A patent/SI9520091B/sl unknown
- 1995-05-17 MX MX9701538A patent/MX9701538A/es active IP Right Grant
- 1995-05-17 RO RO97-00375A patent/RO116400B1/ro unknown
- 1995-05-17 SK SK248-97A patent/SK282922B6/sk not_active IP Right Cessation
- 1995-05-17 ES ES95922465T patent/ES2112650T3/es not_active Expired - Lifetime
- 1995-05-17 RU RU97104885/04A patent/RU2159241C2/ru active
- 1995-05-17 JP JP8508431A patent/JP2904588B2/ja not_active Expired - Lifetime
- 1995-05-17 AT AT95922465T patent/ATE163182T1/de active
- 1995-05-17 CN CN95194697A patent/CN1066727C/zh not_active Expired - Lifetime
- 1995-05-17 KR KR1019970701281A patent/KR100228952B1/ko not_active Expired - Lifetime
- 1995-05-17 WO PCT/EP1995/001914 patent/WO1996006842A1/en not_active Ceased
- 1995-05-17 DK DK95922465.0T patent/DK0776323T3/da active
- 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 IL IL11501395A patent/IL115013A/xx not_active IP Right Cessation
- 1995-08-21 MA MA23992A patent/MA23650A1/fr unknown
- 1995-08-23 CO CO95037815A patent/CO4410334A1/es unknown
- 1995-08-23 DZ DZ950104A patent/DZ1923A1/fr active
- 1995-08-23 PE PE1995277098A patent/PE41596A1/es not_active IP Right Cessation
- 1995-08-25 ZA ZA9507142A patent/ZA957142B/xx unknown
- 1995-08-25 MY MYPI95002536A patent/MY113733A/en unknown
- 1995-08-25 BR BRPI9503812A patent/BRPI9503812B1/pt not_active IP Right Cessation
- 1995-08-25 HR HR9417310.1A patent/HRP950460B1/xx not_active IP Right Cessation
- 1995-08-25 YU YU56995A patent/YU49287B/sh unknown
- 1995-08-25 TR TR95/01061A patent/TR199501061A2/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
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| SI9520091B (sl) | Soli anti-migrenskega derivata indola | |
| Martín et al. | Synthesis and conformational study of acridine derivatives related to 1, 4‐dihydropyridines | |
| JPS61191683A (ja) | 新規な酸性インド−ル化合物 | |
| JPH0216315B2 (sl) | ||
| PT2262505E (pt) | Sólidos de gama-carbolinas fusionadas a heterociclos substituídos | |
| PT88669B (pt) | Processo para a preparacao de compostos aromaticos e hetero-aromaticos alfa,alfa-di-substituidos utilizados para aumentar a percepcao | |
| IE58102B1 (en) | Active compounds | |
| CN112457308A (zh) | 新型三环芳香杂环化合物,及其制备方法、药物组合物和应用 | |
| PT70921A (de) | Neue indolderivate deren herstellung und deren verwendung als arzneimittel | |
| Sturm et al. | (H+-K+)-ATPase inhibiting 2-[(2-pyridylmethyl) sulfinyl] benzimidazoles. 1. Their reaction with thiols under acidic conditions. Disulfide containing 2-pyridiniobenzimidazolides as mimics for the inhibited enzyme | |
| WO2001023377A3 (en) | Polymorphic salt | |
| EP4043457A1 (en) | Aromatic heterocyclic compound having tricyclic structure, and preparation method therefor and application thereof | |
| WO2000078729A1 (en) | Crystalline forms of lansoprazole | |
| Agrawal et al. | Potential antitumor agents. 12. 2-Formyl-4-aminophenylpyridine thiosemicarbazones | |
| KR900008814B1 (ko) | 살균성 폴리시클릭 화합물의 제조방법 | |
| WO2003037903A1 (en) | Olanzapine dihydrate-ii a process for its preparation and use thereof | |
| KR101589910B1 (ko) | 결정형 α 탈티레린의 제조방법 및 결정형의 변환방법 | |
| MX9706339A (es) | Piretanida amorfa, polimorfos de piretanida, proceso para su preparacion y su uso. | |
| JPS6116272B2 (sl) | ||
| CN107344955A (zh) | 一种地塞米松水合物化合物 | |
| Bahrin et al. | Synthesis and Structural Characterization of a New Iodine-containing Phenacyl N, N-Diethylamino Carbodithioate | |
| WO2002030902A1 (en) | Crystal forms of 1-[6-chloro-5-(trifluoromethyl)-2-pyridinyl]piperazine.hydrochloride | |
| JPH0346468B2 (sl) | ||
| JPS6353984B2 (sl) | ||
| CN112759580B (zh) | 一种苯并二氢吡喃-4-酮及其派生物的制备方法 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| IF | Valid on the event date | ||
| SP73 | Change of data on owner |
Owner name: PFIZER IRELAND PHARMACEUTICALS; IE Effective date: 20050406 |
|
| SP73 | Change of data on owner |
Owner name: PFIZER IRELAND PHARMACEUTICALS; IE Effective date: 20110826 |