RU2000102669A - POLYMORPHIC FORMS 8-CHLORO-6,11-DIHYDRO-11- (4-PIPERIDYLIDENE) -5H-BENZO [5,6] CYCLOGEPT [1,2-B] PIR IDINA - Google Patents
POLYMORPHIC FORMS 8-CHLORO-6,11-DIHYDRO-11- (4-PIPERIDYLIDENE) -5H-BENZO [5,6] CYCLOGEPT [1,2-B] PIR IDINAInfo
- Publication number
- RU2000102669A RU2000102669A RU2000102669/04A RU2000102669A RU2000102669A RU 2000102669 A RU2000102669 A RU 2000102669A RU 2000102669/04 A RU2000102669/04 A RU 2000102669/04A RU 2000102669 A RU2000102669 A RU 2000102669A RU 2000102669 A RU2000102669 A RU 2000102669A
- Authority
- RU
- Russia
- Prior art keywords
- polymorphic form
- vwd
- crystalline polymorphic
- approximately
- expressed
- Prior art date
Links
- -1 4-PIPERIDYLIDENE Chemical class 0.000 title claims 7
- 239000013078 crystal Substances 0.000 claims 8
- 238000002329 infrared spectrum Methods 0.000 claims 8
- 239000002480 mineral oil Substances 0.000 claims 8
- 235000010446 mineral oil Nutrition 0.000 claims 8
- 230000003266 anti-allergic effect Effects 0.000 claims 6
- 241000124008 Mammalia Species 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 4
- 229960003088 loratadine Drugs 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 206010020751 Hypersensitivity Diseases 0.000 claims 2
- 238000002441 X-ray diffraction Methods 0.000 claims 2
- 238000004458 analytical method Methods 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 2
Claims (1)
Параметр d (±0,04) - ОИ
9,04 - Слабая
6,42 - Слабая
5,67 - Слабая
5,02 - Слабая
3,58 - Слабая
2. Кристаллическая полиморфная форма 1 дезкарбонилэтоксилоратадина, в значительной мере свободная от полиморфной формы 2 и охарактеризованная с помощью рентгеноструктурного анализа по порошковому методу следующей кристаллической решеткой, имеющей характеристические максимумы, выраженные в терминах параметр кристаллической решетки "d" и относительная интенсивность (ОИ) [S - сильная, М - средняя, W - слабая, V - очень и D - размытая (диффузная)] примерно при:
Параметр d - ОИ
9,04 - W
7,24 - М
7,11 - VWD
6,69 - М
6,42 - W
6,02 - W
5,84 - VW
5,67 - W
5,02 - W
4,73 - М
4,54 - W
4,48 - W
4,40 - М
4,29 - WD
4,25 - W
4,18 - VS
3,72 - W
3,68 - W
3,63 - W
3,58 - W
3,52 - M
3,45 - W
3,37 - S
3,23 - W
3,19 - M
3,14 - VWD
3,10 - VWD
3,04 - M
2,99 - VWD
2,93 - VWD
2,87 - VWD
2,84 - W
2,79 - VWD
2,73 - VWD
2,70 - VWD
2,65 - W
2,57 - VWD
2,56 - VWD
2,55 - VWD
2,51 - VWD
2,48 - VWD
2,47 - VWD
2,44 - VWD
2,42 - WD
2,37 - VWD
2,34 - WD
2,32 - WD
2,29 - VWD
2,27 - W
3. Кристаллическая полиморфная форма 1 дезкарбонилэтоксилоратадина по п. 1, дополнительно охарактеризованная инфракрасным спектром полиморфной формы 1 в виде пленки в минеральном масле, содержащим характеристические максимумы, выраженные в обратных сантиметрах, примерно при:
Частота (см-1): 3303, 1290, 803, 780.1. Crystalline polymorphic form 1 of descarbonylethoxyloratadine, substantially free of polymorphic form 2 and characterized by X-ray powder diffraction analysis of the following crystal lattice having characteristic maxima expressed in terms of the crystal lattice parameter “d” and relative intensity (OR) at approximately :
Parameter d (± 0.04) - OI
9.04 - Weak
6.42 - Weak
5.67 - Weak
5.02 - Weak
3.58 - Weak
2. Crystalline polymorphic form 1 of descarbonylethoxyloratadine, substantially free of polymorphic form 2 and characterized by powder X-ray diffraction analysis of the following crystal lattice having characteristic maxima expressed in terms of the crystal lattice parameter “d” and relative intensity (OI) [S] - strong, M - medium, W - weak, V - very, and D - blurry (diffuse)] at about:
Parameter d - OI
9.04 - W
7.24 - M
7.11 - VWD
6.69 - M
6.42 - W
6.02 - W
5.84 - VW
5.67 - W
5.02 - W
4.73 - M
4.54 - W
4.48 - W
4.40 - M
4.29 - WD
4.25 - W
4.18 - VS
3.72 - W
3.68 - W
3.63 - W
3.58 - W
3.52 - M
3.45 - W
3.37 - S
3.23 - W
3.19 - M
3.14 - VWD
3.10 - VWD
3.04 - M
2.99 - VWD
2.93 - VWD
2.87 - VWD
2.84 - W
2.79 - VWD
2.73 - VWD
2.70 - VWD
2.65 - W
2.57 - VWD
2.56 - VWD
2.55 - VWD
2.51 - VWD
2.48 - VWD
2.47 - VWD
2.44 - VWD
2.42 - WD
2,37 - VWD
2,34 - WD
2.32 - WD
2.29 - VWD
2.27 - W
3. The crystalline polymorphic form 1 of descarbonylethoxyloratadine according to claim 1, further characterized by the infrared spectrum of polymorphic form 1 in the form of a film in mineral oil, containing characteristic maxima expressed in inverse centimeters, approximately:
Frequency (cm -1 ): 3303, 1290, 803, 780.
Частота (см-1): 3303, 3052, 3012, 1636, 1586, 1566, 1357, 1331, 1290, 1273, 1249, 1231, 1219, 1201, 1190, 1177, 1142, 1119, 1100, 1086, 1057, 1029, 1008, 987, 946, 934, 906, 882, 873, 847, 816, 803, 780, 767, 726, 703, 681, 642, 572, 549, 530, 520, 498, 490, 449.4. The crystalline polymorphic form 1 of descarbonylethoxyloratadine according to claim 1, further characterized by the infrared spectrum of polymorphic form 1 in the form of a film in mineral oil containing characteristic maxima expressed in inverse centimeters, approximately:
Frequency (cm -1 ): 3303, 3052, 3012, 1636, 1586, 1566, 1357, 1331, 1290, 1273, 1249, 1231, 1219, 1201, 1190, 1177, 1142, 1119, 1100, 1086, 1057, 1029 , 1008, 987, 946, 934, 906, 882, 873, 847, 816, 803, 780, 767, 726, 703, 681, 642, 572, 549, 530, 520, 498, 490, 449.
Частота (см-1): 3303, 1290, 803, 780.5. The crystalline polymorphic form 1 of descarboxyloratadine according to claim 2, further characterized by the infrared spectrum obtained for the film of said polymorphic form 1 in mineral oil and containing the following characteristic maxima in inverse centimeters at approximately:
Frequency (cm -1 ): 3303, 1290, 803, 780.
Частота (см-1): 3303, 3052, 3012, 1636, 1586, 1566, 1357, 1331, 1290, 1273, 1249, 1231, 1219, 1201, 1190, 1177, 1142, 1119, 1100, 1086, 1057, 1029, 1008, 987, 946, 934, 906, 882, 873, 847, 816, 803, 780, 767, 726, 703, 681, 642, 572, 549, 530, 520, 498, 490, 449.6. The crystalline polymorphic form 1 of descarbonylethoxyloratadine according to claim 2, further characterized by the infrared spectrum of polymorphic form 1, obtained for the film of the said polymorphic form in mineral oil and containing characteristic maxima expressed in inverse centimeters, approximately:
Frequency (cm -1 ): 3303, 3052, 3012, 1636, 1586, 1566, 1357, 1331, 1290, 1273, 1249, 1231, 1219, 1201, 1190, 1177, 1142, 1119, 1100, 1086, 1057, 1029 , 1008, 987, 946, 934, 906, 882, 873, 847, 816, 803, 780, 767, 726, 703, 681, 642, 572, 549, 530, 520, 498, 490, 449.
Параметр d (±0,04) - ОИ
8,34 - Слабая
6,87 - Средняя
6,20 - Средняя
4,90 - Средняя
9. Кристаллическая полиморфная форма 2 дезкарбонилэтоксилоратадина, в значительной мере свободная от полиморфной формы 1 и охарактеризованная с помощью рентгеноструктурного анализа следующей кристаллической решеткой, имеющей характеристические максимумы, выраженные в терминах параметр кристаллической решетки "d" и относительная интенсивность (ОИ) [S - сильная, М - средняя, W - слабая, V - очень и D - размытая (диффузная)] примерно при:
Параметр d - ОИ
8,34 - W
7,21 - W
6,87 - М
6,75 - М
6,20 - М
6,04 - М
5,91 - VW
4,90 - М
4,71 - М
4,64 - М
4,50 - WD
4,39 - VS
4,34 - S
4,19 - VWD
4,08 - W
3,95 - S
3,84 - М
3,66 - S
3,52 - W
3,46 - W
3,45 - WD
3,39 - W
3,25 - S
3,18 - W
3,11 - W
3,07 - M
2,95 - W
2,88 - WD
2,81 - WD
2,79 - WD
2,72 - VW
2,59 - VW
2,51 - WD
2,45 - VWD
2,40 - VWD
2,38 - VWD
2,32 - VWD
2,30 - VWD
10. Кристаллическая полиморфная форма 2 дезкарбоксилоратадина по п.8, охарактеризованная дополнительно инфракрасным спектром, полученным для пленки упомянутой полиморфной формы 2 в минеральном масле и имеющим следующие характеристические максимумы, выраженные в обратных сантиметрах, примерно при:
Частота (см-1): 3326, 1153, 1133, 795, 771, 655.8. Crystalline polymorphic form 2 of descarbonyl ethoxyloratadine, substantially free of polymorphic form 1 and characterized by X-ray diffraction analysis of the following crystal lattice, having characteristic maxima expressed in terms of the crystal lattice parameter "d" and relative intensity (OR) approximately at:
Parameter d (± 0.04) - OI
8.34 - Weak
6.87 - Average
6.20 - Average
4.90 - Average
9. Crystalline polymorphic form 2 of descarbonylethoxyloratadine, substantially free of polymorphic form 1 and characterized by x-ray diffraction analysis of the following crystal lattice having characteristic maxima expressed in terms of the crystal lattice parameter “d” and relative intensity (OI) [S - strong, M - medium, W - weak, V - very and D - blurred (diffuse)] approximately at:
Parameter d - OI
8.34 - W
7.21 - W
6.87 - M
6.75 - M
6.20 - M
6.04 - M
5.91 - VW
4.90 - M
4.71 - M
4.64 - M
4,50 - WD
4.39 - VS
4.34 - S
4.19 - VWD
4.08 - W
3.95 - S
3.84 - M
3.66 - S
3.52 - W
3.46 - W
3.45 - WD
3.39 - W
3.25 - S
3.18 - W
3.11 - W
3.07 - M
2.95 - W
2.88 - WD
2.81 - WD
2.79 - WD
2.72 - VW
2.59 - VW
2.51 - WD
2.45 - VWD
2.40 - VWD
2.38 - VWD
2.32 - VWD
2.30 - VWD
10. The crystalline polymorphic form 2 of descarboxyloratadine according to claim 8, further characterized by an infrared spectrum obtained for the film of said polymorphic form 2 in mineral oil and having the following characteristic maxima, expressed in inverse centimeters, approximately:
Frequency (cm -1 ): 3326, 1153, 1133, 795, 771, 655.
Частота (см-1): 3326, 3304, 3052, 3015, 1635, 1586, 1569, 1558, 1479, 1456, 1437, 1420, 1398, 1383, 1328, 1301, 1282, 1265, 1250, 1199, 1174, 1153, 1133, 1118, 1089, 1010, 977, 951, 915, 887, 868, 846, 816, 795, 781, 771, 730, 707, 688, 655, 623, 570, 550, 528, 515, 493, 476, 447.11. The crystalline polymorphic form 2 of descarbonylethoxyloratadine according to claim 8, further characterized by an infrared spectrum obtained for the film of said polymorphic form 2 in mineral oil and having the following characteristic maxima expressed in inverse centimeters, approximately:
Frequency (cm -1 ): 3326, 3304, 3052, 3015, 1635, 1586, 1569, 1558, 1479, 1456, 1437, 1420, 1398, 1383, 1328, 1301, 1282, 1265, 1250, 1199, 1174, 1153 , 1133, 1118, 1089, 1010, 977, 951, 915, 887, 868, 846, 816, 795, 781, 771, 730, 707, 688, 655, 623, 570, 550, 528, 515, 493, 476 , 447.
Частота (см-1):, 3326, 1153, 1133, 795, 771, 655.12. The crystalline polymorphic form 2 of descarbonylethoxyloratadine according to claim 9, further characterized by an infrared spectrum obtained for the film of said polymorphic form 2 in mineral oil and having the following characteristic maxima, expressed in inverse centimeters, approximately:
Frequency (cm -1 ) :, 3326, 1153, 1133, 795, 771, 655.
Частота (см-1): 3326, 3304, 3052, 3015, 1635, 1586, 1569, 1558, 1479, 1456, 1437, 1420, 1398, 1383, 1328, 1301, 1282, 1265, 1250, 1199, 1174, 1153, 1133, 1118, 1089, 1010, 977, 951, 915, 887, 868, 846, 816, 795, 781, 771, 730, 707, 688, 655, 623, 570, 550, 528, 515, 493, 476, 447.13. The crystalline polymorphic form 2 of descarboxyloratadine according to claim 9, further characterized by an infrared spectrum obtained for the film of said polymorphic form 2 in mineral oil and having the following characteristic maxima, expressed in inverse centimeters, at about:
Frequency (cm -1 ): 3326, 3304, 3052, 3015, 1635, 1586, 1569, 1558, 1479, 1456, 1437, 1420, 1398, 1383, 1328, 1301, 1282, 1265, 1250, 1199, 1174, 1153 , 1133, 1118, 1089, 1010, 977, 951, 915, 887, 868, 846, 816, 795, 781, 771, 730, 707, 688, 655, 623, 570, 550, 528, 515, 493, 476 , 447.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US88676697A | 1997-07-02 | 1997-07-02 | |
| US08/886,766 | 1997-07-02 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2000102669A true RU2000102669A (en) | 2001-10-27 |
| RU2197485C2 RU2197485C2 (en) | 2003-01-27 |
Family
ID=25389724
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2000102669/04A RU2197485C2 (en) | 1997-07-02 | 1998-07-01 | Polymorphic forms of 8-chloro-6,11-dihydro-11-(4-piperidylidene)-5h-benzo[5,6]cyclohepta[1,2-b]-pyridine |
Country Status (25)
| Country | Link |
|---|---|
| EP (1) | EP0993455B1 (en) |
| JP (2) | JP2002507991A (en) |
| KR (1) | KR20010014316A (en) |
| CN (1) | CN1261886A (en) |
| AR (1) | AR013161A1 (en) |
| AT (1) | ATE239010T1 (en) |
| AU (1) | AU734487B2 (en) |
| BR (1) | BR9811658A (en) |
| CA (1) | CA2294352C (en) |
| CO (1) | CO4940423A1 (en) |
| DE (1) | DE69814076T2 (en) |
| ES (1) | ES2197480T3 (en) |
| HU (1) | HUP0004308A3 (en) |
| IL (1) | IL133387A (en) |
| MY (1) | MY132943A (en) |
| NO (1) | NO996547L (en) |
| NZ (1) | NZ501417A (en) |
| PE (1) | PE86399A1 (en) |
| PL (1) | PL337712A1 (en) |
| RU (1) | RU2197485C2 (en) |
| SK (1) | SK185299A3 (en) |
| TR (1) | TR199903308T2 (en) |
| UA (1) | UA62976C2 (en) |
| WO (1) | WO1999001450A1 (en) |
| ZA (1) | ZA985783B (en) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7405223B2 (en) | 2000-02-03 | 2008-07-29 | Schering Corporation | Treating allergic and inflammatory conditions |
| WO2003086275A2 (en) * | 2002-04-15 | 2003-10-23 | Sun Pharmaceutical Industries Limited | Preperation of desloratatine |
| HRP20050110A2 (en) * | 2002-08-05 | 2006-02-28 | Sandoz Ag | Novel salt and polymorphs of desloratadine hemifumarate |
| US20060135547A1 (en) * | 2003-03-12 | 2006-06-22 | Toth Zoltan G | Stable pharmaceutical compositions of desloratadine and processes for preparation of polymorphic forms of desloratadine |
| US20040229896A1 (en) * | 2003-03-12 | 2004-11-18 | Toth Zoltan G. | Stable pharmaceutical compositions of desloratadine |
| EA011894B1 (en) * | 2004-07-07 | 2009-06-30 | Эгиш Дьёдьсердьяр Нирт. | New pseudopolymorph of desloratadine formed with carbon dioxide |
| CA2641668A1 (en) * | 2005-11-17 | 2008-05-15 | Teva Pharmaceutical Industries Ltd. | Desloratadine crystalline forms mixtures having a low level of residual solvents |
| HU230417B1 (en) * | 2006-10-26 | 2016-05-30 | Egis Gyógyszergyár Zrt | Process for producing adduct comprising desloratadine and carbon dioxide |
| US20100303908A1 (en) * | 2007-05-11 | 2010-12-02 | Balamurugan Jeganathan | Pharmaceutical composition comprising desloratadine |
| ATE525064T1 (en) | 2009-07-01 | 2011-10-15 | Tiefenbacher Alfred E Gmbh & Co Kg | PHARMACEUTICAL COMPOSITION CONTAINING DESLORATADINE |
| WO2011141483A2 (en) | 2010-05-10 | 2011-11-17 | Laboratorios Lesvi, S.L. | Stable pharmaceutical formulations containing an antihistaminic |
| EP2727592A1 (en) | 2012-11-05 | 2014-05-07 | Kücükgüzel, Sükriye Güniz | A combination of desloratadine and paracetamol |
| CN103755682A (en) * | 2013-12-30 | 2014-04-30 | 山东达因海洋生物制药股份有限公司 | Novel crystal form for desloratadine and preparation method thereof |
| CN108358892A (en) * | 2018-04-11 | 2018-08-03 | 常州方圆制药有限公司 | A kind of method of purification of Desloratadine crude product |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1985003707A1 (en) * | 1984-02-15 | 1985-08-29 | Schering Corporation | 8-CHLORO-6,11-DIHYDRO-11-(4-PIPERIDYLIDENE)-5H-BENZO AD5,6 BDCYCLOHEPTA AD1,2-b BDPYRIDINE AND ITS SALTS, PROCESSES FOR THE PRODUCTION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS |
| EP0208855B1 (en) * | 1985-05-13 | 1991-03-06 | Schering Corporation | process for preparing piperidylidene dihydrodibenzo(a,d)cycloheptenes and aza derivatives thereof, compounds obtained by such process and the use of such compounds for preparing useful pharmaceutical compositions |
| IE68935B1 (en) * | 1990-06-22 | 1996-07-24 | Schering Corp | Bis-benzo or benzopyrido cyclohepta piperidene piperidylidene and piperazine compounds compositions and methods of use |
-
1998
- 1998-01-07 UA UA2000010519A patent/UA62976C2/en unknown
- 1998-07-01 WO PCT/US1998/013433 patent/WO1999001450A1/en not_active Ceased
- 1998-07-01 KR KR1019997012456A patent/KR20010014316A/en not_active Ceased
- 1998-07-01 PL PL98337712A patent/PL337712A1/en unknown
- 1998-07-01 ZA ZA985783A patent/ZA985783B/en unknown
- 1998-07-01 AT AT98932930T patent/ATE239010T1/en not_active IP Right Cessation
- 1998-07-01 BR BR9811658-4A patent/BR9811658A/en not_active IP Right Cessation
- 1998-07-01 CO CO98037139A patent/CO4940423A1/en unknown
- 1998-07-01 IL IL13338798A patent/IL133387A/en not_active IP Right Cessation
- 1998-07-01 DE DE69814076T patent/DE69814076T2/en not_active Expired - Lifetime
- 1998-07-01 JP JP50726599A patent/JP2002507991A/en active Pending
- 1998-07-01 CA CA002294352A patent/CA2294352C/en not_active Expired - Fee Related
- 1998-07-01 TR TR1999/03308T patent/TR199903308T2/en unknown
- 1998-07-01 SK SK1852-99A patent/SK185299A3/en unknown
- 1998-07-01 EP EP98932930A patent/EP0993455B1/en not_active Expired - Lifetime
- 1998-07-01 NZ NZ501417A patent/NZ501417A/en unknown
- 1998-07-01 AU AU82710/98A patent/AU734487B2/en not_active Ceased
- 1998-07-01 CN CN98806712A patent/CN1261886A/en active Pending
- 1998-07-01 RU RU2000102669/04A patent/RU2197485C2/en not_active IP Right Cessation
- 1998-07-01 HU HU0004308A patent/HUP0004308A3/en unknown
- 1998-07-01 ES ES98932930T patent/ES2197480T3/en not_active Expired - Lifetime
- 1998-07-01 AR ARP980103203A patent/AR013161A1/en unknown
- 1998-07-02 PE PE1998000594A patent/PE86399A1/en not_active Application Discontinuation
- 1998-07-02 MY MYPI98003024A patent/MY132943A/en unknown
-
1999
- 1999-12-29 NO NO996547A patent/NO996547L/en not_active Application Discontinuation
-
2009
- 2009-07-27 JP JP2009174701A patent/JP2009242436A/en not_active Withdrawn
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