RU2004116311A - Сукцинатные соли 5,8,14-триазатетрацикло [10.3.1.02,11(04,9]гексадека- 2(11),3,5,7,9-пентаена и их фармацевтические композиции - Google Patents
Сукцинатные соли 5,8,14-триазатетрацикло [10.3.1.02,11(04,9]гексадека- 2(11),3,5,7,9-пентаена и их фармацевтические композиции Download PDFInfo
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- 150000003890 succinate salts Chemical class 0.000 title claims 2
- 150000001875 compounds Chemical class 0.000 claims 10
- 238000002441 X-ray diffraction Methods 0.000 claims 8
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 claims 4
- 229910052802 copper Inorganic materials 0.000 claims 4
- 239000010949 copper Substances 0.000 claims 4
- 206010012335 Dependence Diseases 0.000 claims 3
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims 2
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- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 claims 2
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- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
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- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
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Claims (11)
1. Сукцинатная соль 5,8,14-триазатетрацикло-[10.3.1.02,11.04,9]-гексадека-2(11),3,5,7,9-пентаена.
2. Соединение по п.1, где соль является безводной.
3. Соединение по п.2, имеющее рентгеновскую дифрактограмму, характеризуемую, главным образом, наличием пиков на рентгеновской дифрактограмме, как измерено с медным излучателем, при 2θ примерно 13,3 и 17,2.
4. Соединение по п.2, имеющее рентгеновскую дифрактограмму, характеризуемую, главным образом, следующими главными пиками на рентгеновской дифрактограмме, выраженными в терминах 2θ и D-интервалов, как измерено с медным излучателем:
5. Соединение по п.2, отличающееся остановкой перехода плавление/разложение при примерно 198оС.
6. Фармацевтическая композиция, включающая соединение по п.2 и фармацевтически приемлемый носитель.
7. Соединение по п.1, где соль представляет собой гидрат.
8. Соединение по п.7, имеющее рентгеновскую дифрактограмму, характеризуемую, главным образом, наличием пиков на рентгеновской дифрактограмме, как измерено с медным излучателем, при 2θ примерно 13,0, 16,5 и 19,0.
9. Соединение по п.7, имеющее рентгеновскую дифрактограмму, характеризуемую, главным образом, следующими главными пиками на рентгеновской дифрактограмме, выраженными в терминах 2θ и D-интервалов, как измерено с медным излучателем:
10. Способ лечения воспалительных заболеваний кишечника (включая, но не ограничиваясь этим, язвенный колит, гангренозную пиодермию и болезнь Крона), синдрома раздраженной толстой кишки, спастической дистонии, хронических болей, острых болей, нетропической спру (болезнью глютеновой недостаточности), воспаления брюшины, сужения сосудов, беспокойства, панического состояния, депрессии, биполярного расстройства, аутизма, расстройств сна, нарушения суточного ритма организма при перелете через несколько часовых поясов, бокового амиотрофического склероза (БАС), дисфункции познавательной способности, гипертонии, булимии, анорексии, тучности, сердечной аритмии, повышенной кислотности желудка, язвенных болезней, феохромоцитомы, прогрессивной надмышечной атрофии, зависимостей от химических веществ и пристрастия к ним (например, зависимости от или пристрастия к никотину (и/или табачным продуктам), алкоголю, бензодиазепинам, барбитуратам, опиоидам или кокаину), головной боли, мигрени, удара, травматического поражения мозга (ТПМ), обсессивно-компульсивного расстройства (ОКР), психоза, хореи Хантингтона, поздней дискинезии, гиперкинезии, дислексии, шизофрении, мультиинфарктного слабоумия, возрастного ухудшения познавательной способности, эпилепсии, включая эпилепсию кратковременной потери сознания, старческого слабоумия альцгеймеровского типа (болезнь Альцгеймера, БА), болезни Паркинсона (БП), расстройства дефицита внимания - гиперактивности (ADHD), и синдрома Туррета, включающий введение нуждающемуся в лечении субъекту терапевтически эффективного количества соединения по п.1.
11. Способ лечения никотиновой зависимости, пристрастия к никотину и синдрома абстиненции в отношении никотина у млекопитающих, включающий введение нуждающемуся в этом субъекту соединения по п.1.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33424501P | 2001-11-29 | 2001-11-29 | |
| US60/334,245 | 2001-11-29 |
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| Publication Number | Publication Date |
|---|---|
| RU2004116311A true RU2004116311A (ru) | 2005-03-27 |
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| RU2004116311/04A RU2004116311A (ru) | 2001-11-29 | 2002-10-21 | Сукцинатные соли 5,8,14-триазатетрацикло [10.3.1.02,11(04,9]гексадека- 2(11),3,5,7,9-пентаена и их фармацевтические композиции |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US6794388B2 (ru) |
| EP (1) | EP1461040B1 (ru) |
| JP (1) | JP4196829B2 (ru) |
| KR (1) | KR20040066140A (ru) |
| CN (1) | CN1589148A (ru) |
| AR (1) | AR037677A1 (ru) |
| AT (1) | ATE320256T1 (ru) |
| AU (1) | AU2002341327A1 (ru) |
| BR (1) | BR0214559A (ru) |
| CA (1) | CA2468705A1 (ru) |
| DE (1) | DE60209929T2 (ru) |
| DO (1) | DOP2002000512A (ru) |
| ES (1) | ES2258652T3 (ru) |
| GT (1) | GT200200236A (ru) |
| HN (1) | HN2002000332A (ru) |
| IL (1) | IL161326A0 (ru) |
| MX (1) | MXPA04003192A (ru) |
| PA (1) | PA8559401A1 (ru) |
| PE (1) | PE20030738A1 (ru) |
| PL (1) | PL374325A1 (ru) |
| RU (1) | RU2004116311A (ru) |
| SV (1) | SV2004001413A (ru) |
| TW (1) | TW200300345A (ru) |
| UY (1) | UY27548A1 (ru) |
| WO (1) | WO2003045394A1 (ru) |
| ZA (1) | ZA200402720B (ru) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2527970C2 (ru) * | 2008-12-11 | 2014-09-10 | Селл Терапьютикс,Инк. | Цитрат 11-(2-пирролидин-1-ил-этокси)-14,19-диокса-5,7,26-триазатетрацикло[19.3.1.1(2,6).1(8,12)]гептакоза-1(25),2(26),3,5,8,10,12(27),16,21,23-декаена |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1044189T4 (en) * | 1997-12-31 | 2015-03-30 | Pfizer Prod Inc | Aryl-fused fused azapolycyclic connections |
| US7429565B2 (en) | 2003-04-25 | 2008-09-30 | Gilead Sciences, Inc. | Antiviral phosphonate analogs |
| JP2006528237A (ja) * | 2003-05-20 | 2006-12-14 | ファイザー・プロダクツ・インク | バレニクリンの医薬組成物 |
| CA2543201C (en) * | 2003-10-27 | 2010-12-21 | Merck & Co., Inc. | ((ir, 3s)-3-isopropyl-3-{ [3-(trifluoromethyl)-7, 8-dihydro-1, 6-naphthyridin-6 (5h)-yl] carbonyl} cyclopentyl) [(3s, 4s)-3-methoxytetrahydro-2h-pyran-4-yl] amine succinate salt, composition thereof, and its use in the treatment of inflammatory diseases |
| HRP20070078A2 (hr) | 2004-07-27 | 2007-05-31 | Gilead Sciences | Fosfonatni analozi spojeva koji inhibiraju hiv |
| US20110086086A1 (en) * | 2005-07-26 | 2011-04-14 | Pfizer Inc | Transdermal system for varenicline |
| KR100734147B1 (ko) * | 2005-07-29 | 2007-07-02 | 주식회사 엘지데이콤 | 호 알림 지연을 통한 멀티미디어 통화연결음 서비스 시스템및 방법 |
| PT2020996E (pt) * | 2006-05-16 | 2012-02-20 | Gilead Sciences Inc | Método e composições para tratar neoplasias malignas hematológicas |
| AU2007319951A1 (en) * | 2006-11-09 | 2008-05-22 | Pfizer Products Inc. | Polymorphs of nicotinic intermediates |
| CN101611029B (zh) * | 2006-12-21 | 2014-09-10 | 辉瑞产品公司 | 2-((4-(1-甲基-4-(吡啶-4-基)-1h-吡唑-3-基)苯氧基)甲基)喹啉的琥珀酸盐 |
| US8440825B2 (en) | 2008-03-06 | 2013-05-14 | Medichem S.A. | Fumaric acid salt of varenicline |
| WO2009143347A2 (en) | 2008-05-22 | 2009-11-26 | Teva Pharmaceutical Industries Ltd. | Varenicline tosylate, an intermediate in the preparation process of varenicline l-tartrate |
| US20090318460A1 (en) * | 2008-05-26 | 2009-12-24 | Glenmark | Amorphous varenicline tartrate and process for the preparation thereof |
| PT2307435E (pt) * | 2008-07-08 | 2012-09-19 | Gilead Sciences Inc | Sais de compostos inibidores de vih |
| US20100010221A1 (en) * | 2008-07-10 | 2010-01-14 | Revital Lifshitz-Liron | Processes for purifying varenicline l-tartrate salt and preparing crystalline forms of varenicline l-tartrate salt |
| WO2010033045A1 (en) * | 2008-09-16 | 2010-03-25 | Igor Anatolievich Pomytkin | Compositions and methods for prevention or treatment of beta amyloid deposition |
| CA2801842A1 (en) | 2009-06-10 | 2010-12-16 | Actavis Group Ptc Ehf | Amorphous varenicline tartrate co-precipitates |
| WO2010151524A1 (en) | 2009-06-22 | 2010-12-29 | Teva Pharmaceutical Industries Ltd | Solid states forms of varenicline salts and processes for preparation thereof |
| WO2011140431A1 (en) | 2010-05-06 | 2011-11-10 | Teva Pharmaceutical Industries Ltd. | Varenicline salts and crystal forms thereof |
| EP2837632B1 (en) | 2012-04-13 | 2016-05-18 | Lianyungang Jinkang Hexin Pharmaceutical Co. Ltd. | Derivatives of triazabicyclo[3.2.1]octane useful for the treatment of proliferative diseases |
| BR112017008097B1 (pt) | 2014-10-20 | 2023-03-28 | Oyster Point Pharma, Inc | Método para tratar condições oculares |
| DK3439661T3 (da) | 2016-04-07 | 2021-10-18 | Oyster Point Pharma Inc | Fremgangsmåder til behandling af øjenlidelser |
| WO2019027920A1 (en) | 2017-08-01 | 2019-02-07 | Gilead Sciences, Inc. | CRYSTALLINE FORMS OF ETHYL ((S) - (((((2R, 5R) -5- (6-AMINO-9H-PURIN-9-YL) -4-FLUORO-2,5-DIHYDROFURAN-2-YL) OXY ) METHYL) (PHENOXY) PHOSPHORYL) -L-ALANINATE (GS-9131) FOR THE TREATMENT OF VIRAL INFECTIONS |
| WO2018154395A2 (en) | 2018-06-11 | 2018-08-30 | Alvogen Malta Operations (Row) Ltd | Controlled release pharmaceutical composition of varenicline |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1044189T4 (en) * | 1997-12-31 | 2015-03-30 | Pfizer Prod Inc | Aryl-fused fused azapolycyclic connections |
| JP2003509341A (ja) | 1999-08-27 | 2003-03-11 | イネックス ファーマスーティカルズ コーポレイション | サイトカインの分泌刺激および免疫応答の誘導組成物 |
| TWI236930B (en) * | 2000-05-26 | 2005-08-01 | Pfizer Prod Inc | Reactive crystallization method to improve particle size |
-
2002
- 2002-10-21 DE DE60209929T patent/DE60209929T2/de not_active Expired - Fee Related
- 2002-10-21 CA CA002468705A patent/CA2468705A1/en not_active Abandoned
- 2002-10-21 KR KR10-2004-7008116A patent/KR20040066140A/ko not_active Ceased
- 2002-10-21 MX MXPA04003192A patent/MXPA04003192A/es active IP Right Grant
- 2002-10-21 EP EP02775143A patent/EP1461040B1/en not_active Expired - Lifetime
- 2002-10-21 PL PL02374325A patent/PL374325A1/xx not_active Application Discontinuation
- 2002-10-21 IL IL16132602A patent/IL161326A0/xx unknown
- 2002-10-21 CN CNA028229304A patent/CN1589148A/zh active Pending
- 2002-10-21 AU AU2002341327A patent/AU2002341327A1/en not_active Abandoned
- 2002-10-21 WO PCT/IB2002/004380 patent/WO2003045394A1/en not_active Ceased
- 2002-10-21 JP JP2003546896A patent/JP4196829B2/ja not_active Expired - Fee Related
- 2002-10-21 BR BRPI0214559-6A patent/BR0214559A/pt not_active IP Right Cessation
- 2002-10-21 AT AT02775143T patent/ATE320256T1/de not_active IP Right Cessation
- 2002-10-21 RU RU2004116311/04A patent/RU2004116311A/ru not_active Application Discontinuation
- 2002-10-21 ES ES02775143T patent/ES2258652T3/es not_active Expired - Lifetime
- 2002-11-13 DO DO2002000512A patent/DOP2002000512A/es unknown
- 2002-11-22 GT GT200200236A patent/GT200200236A/es unknown
- 2002-11-25 TW TW091134190A patent/TW200300345A/zh unknown
- 2002-11-25 PE PE2002001130A patent/PE20030738A1/es not_active Application Discontinuation
- 2002-11-26 UY UY27548A patent/UY27548A1/es not_active Application Discontinuation
- 2002-11-27 US US10/305,845 patent/US6794388B2/en not_active Expired - Fee Related
- 2002-11-27 HN HN2002000332A patent/HN2002000332A/es unknown
- 2002-11-27 AR ARP020104558A patent/AR037677A1/es unknown
- 2002-11-28 SV SV2002001413A patent/SV2004001413A/es not_active Application Discontinuation
- 2002-11-29 PA PA20028559401A patent/PA8559401A1/es unknown
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2004
- 2004-04-07 ZA ZA200402720A patent/ZA200402720B/en unknown
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2527970C2 (ru) * | 2008-12-11 | 2014-09-10 | Селл Терапьютикс,Инк. | Цитрат 11-(2-пирролидин-1-ил-этокси)-14,19-диокса-5,7,26-триазатетрацикло[19.3.1.1(2,6).1(8,12)]гептакоза-1(25),2(26),3,5,8,10,12(27),16,21,23-декаена |
Also Published As
| Publication number | Publication date |
|---|---|
| ATE320256T1 (de) | 2006-04-15 |
| HN2002000332A (es) | 2003-12-11 |
| US6794388B2 (en) | 2004-09-21 |
| PL374325A1 (en) | 2005-10-17 |
| JP4196829B2 (ja) | 2008-12-17 |
| DOP2002000512A (es) | 2003-05-31 |
| BR0214559A (pt) | 2007-03-13 |
| SV2004001413A (es) | 2004-05-07 |
| CN1589148A (zh) | 2005-03-02 |
| WO2003045394A1 (en) | 2003-06-05 |
| AU2002341327A1 (en) | 2003-06-10 |
| PA8559401A1 (es) | 2004-02-07 |
| US20030149044A1 (en) | 2003-08-07 |
| ES2258652T3 (es) | 2006-09-01 |
| EP1461040B1 (en) | 2006-03-15 |
| DE60209929T2 (de) | 2006-11-16 |
| GT200200236A (es) | 2003-06-25 |
| CA2468705A1 (en) | 2003-06-05 |
| JP2005513032A (ja) | 2005-05-12 |
| ZA200402720B (en) | 2005-05-18 |
| AR037677A1 (es) | 2004-12-01 |
| PE20030738A1 (es) | 2003-08-28 |
| DE60209929D1 (de) | 2006-05-11 |
| UY27548A1 (es) | 2003-06-30 |
| TW200300345A (en) | 2003-06-01 |
| MXPA04003192A (es) | 2004-07-27 |
| EP1461040A1 (en) | 2004-09-29 |
| IL161326A0 (en) | 2004-09-27 |
| KR20040066140A (ko) | 2004-07-23 |
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| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
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