JP5254602B2 - 2−((4−(1−メチル−4−(ピリジン−4−イル)−1h−ピラゾール−3−イル)フェノキシ)メチル)キノリンのコハク酸塩 - Google Patents
2−((4−(1−メチル−4−(ピリジン−4−イル)−1h−ピラゾール−3−イル)フェノキシ)メチル)キノリンのコハク酸塩 Download PDFInfo
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P25/16—Anti-Parkinson drugs
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A61P25/00—Drugs for disorders of the nervous system
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- A61P25/32—Alcohol-abuse
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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Description
2−((4−(1−メチル−4−(ピリジン−4−イル)−1H−ピラゾール−3−イル)フェノキシ)メチル)キノリンの遊離塩基化合物(3.0g、7.6mmol)を酢酸エチル(75ml)に溶かした25℃の溶液に、900mg(7.6mmol)のコハク酸の入った25℃の酢酸エチル75mlを加えた。混合物を25℃で12時間攪拌した。得られる沈殿を濾過し、ジエチルエーテルで洗浄し、減圧下で乾燥させて、3.13gの表題化合物を白色のプリズム形結晶として得た。
1H−NMR:(400MHz、CD3OD)δ8.38(d,J=8.3Hz,1H)、8.32(m,2H)、8.03(d,J=8.3Hz,1H)、8.00(m,1H)、7.94(d,J=7.9Hz,1H)、7.75(m,1H)、7.74(d,J=8.7Hz,1H)、7.60(m,1H)、7.35(dd,J=8.7,2.1Hz,2H)、7.28(m,2H)、7.10(dd,J=8.7,2.1Hz,2H)、5.37(s,2H)、3.93(s,3H)、2.54(s,4H);
13C−NMR(100MHz、CD3OD)δ175.0 158.9 157.9 149.5 148.6 147.2 142.8 137.9 132.0 130.2 130.0 128.0 127.9 127.8 126.9 125.9 122.7 119.6 117.2 114.9 70.7 37.9 28.7;
無水コハク酸塩について算出した成分分析値:C,68.22、H,5.13、N,10.97。実測値:C,68.05、H,4.99、N,10.87。融点:184±3℃
粉末X線回折(PXRD)パターン
実施例1の塩の粉末X線回折パターンを、銅放射線源、固定されたスリット(発散1.0mm、散乱防止1.0mm、および受光0.6mm)、およびKevex固体状態検出器を備え付けたBruker D5000回折計(米国ウィスコンシン州マディソン)を使用して収集した。データは、θ−2θゴニオメーター配置で、0.040度のステップサイズおよび1秒のステップ時間を使用して、平らなプレートサンプル保持器から、3.0〜40.0度2θの銅波長Kα1=1.54056およびKα2=1.54439(相対強度0.5)で収集した。X線管の電圧およびアンペア数は、それぞれ40kVおよび30mAに設定した。データの収集および分析は、Bruker DIFFRAC Plusソフトウェアを使用して行った。サンプルは、石英保持器に入れて準備した。(Bruker D5000回折計の操作は、SiemansのD5000モデルと同様であることを留意されたい。)結果は表1に要約するが、反射幅0.30および閾値1.0を使用して相対強度が6%以上である反射(線)すべてについての2θ値および相対強度を示す。
Claims (7)
- 銅放射線を用いて測定したとき、2θが15.8、21.0および26.6の±0.1°で特徴的なX線粉末回折ピークを有する、請求項1に記載の塩。
- 銅放射線を用いて測定したとき、2θが15.8、16.7、21.0、24.2および26.6の±0.1°で特徴的なX線粉末回折ピークを有する、請求項1に記載の塩。
- 融解開始温度が184±3℃である、請求項1に記載の塩。
- 湿度約1%〜90%(±2%)で行った等温(25.1±0.1℃)水分吸着試験において、90±2%の相対湿度で0.5%未満重量が増加する、請求項1に記載の塩。
- 無水である、請求項1に記載の塩。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US87126006P | 2006-12-21 | 2006-12-21 | |
US60/871260 | 2006-12-21 |
Publications (3)
Publication Number | Publication Date |
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JP2008208114A JP2008208114A (ja) | 2008-09-11 |
JP2008208114A5 JP2008208114A5 (ja) | 2011-02-03 |
JP5254602B2 true JP5254602B2 (ja) | 2013-08-07 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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JP2007327323A Expired - Fee Related JP5254602B2 (ja) | 2006-12-21 | 2007-12-19 | 2−((4−(1−メチル−4−(ピリジン−4−イル)−1h−ピラゾール−3−イル)フェノキシ)メチル)キノリンのコハク酸塩 |
Country Status (25)
Country | Link |
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US (1) | US8283471B2 (ja) |
EP (1) | EP2125786B1 (ja) |
JP (1) | JP5254602B2 (ja) |
KR (2) | KR20120043775A (ja) |
CN (1) | CN101611029B (ja) |
AR (1) | AR064417A1 (ja) |
AT (1) | ATE502028T1 (ja) |
AU (1) | AU2007343135B2 (ja) |
BR (1) | BRPI0720936A2 (ja) |
CA (1) | CA2673435C (ja) |
CY (1) | CY1111919T1 (ja) |
DE (1) | DE602007013294D1 (ja) |
DK (1) | DK2125786T3 (ja) |
ES (1) | ES2360014T3 (ja) |
HK (1) | HK1134670A1 (ja) |
IL (1) | IL199389A (ja) |
MX (1) | MX2009006528A (ja) |
NZ (1) | NZ577716A (ja) |
PL (1) | PL2125786T3 (ja) |
PT (1) | PT2125786E (ja) |
RU (1) | RU2430918C2 (ja) |
SI (1) | SI2125786T1 (ja) |
TW (1) | TWI359660B (ja) |
WO (1) | WO2008084299A1 (ja) |
ZA (1) | ZA200904230B (ja) |
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WO2010033045A1 (en) * | 2008-09-16 | 2010-03-25 | Igor Anatolievich Pomytkin | Compositions and methods for prevention or treatment of beta amyloid deposition |
TWI396689B (zh) * | 2008-11-14 | 2013-05-21 | Amgen Inc | 作為磷酸二酯酶10抑制劑之吡衍生物 |
US20120214842A1 (en) | 2011-02-18 | 2012-08-23 | Exonhit Therapeutics Sa | Methods for treating diseases of the retina |
EP2975037A4 (en) | 2013-03-15 | 2016-08-10 | Daiichi Sankyo Co Ltd | BENZOTHIOPHENE DERIVATIVE |
US10039764B2 (en) | 2013-07-12 | 2018-08-07 | University Of South Alabama | Treatment and diagnosis of cancer and precancerous conditions using PDE10A inhibitors and methods to measure PDE10A expression |
KR102233916B1 (ko) * | 2019-05-28 | 2021-03-30 | 주식회사 엘지생활건강 | Pq1 숙신산을 포함하는 피부 보습, 주름 개선 및 탄력 증진용 조성물 |
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US5795909A (en) * | 1996-05-22 | 1998-08-18 | Neuromedica, Inc. | DHA-pharmaceutical agent conjugates of taxanes |
ATE369330T1 (de) * | 2001-02-12 | 2007-08-15 | Wyeth Corp | O-desmethyl-venlafaxine succinat salz |
ES2258652T3 (es) * | 2001-11-29 | 2006-09-01 | Pfizer Products Inc. | Sales de succinato de 5,8,14-triazatetraciclo(10.3.1.02,11.04,9)-hexadeca-2(11),3,5,7,9-pentaeno y composiciones farmaceuticas de los mismos. |
UA75482C2 (en) * | 2001-12-12 | 2006-04-17 | Pfizer Prod Inc | Salts of e-2-methoxy-n-(3-{4-[3-methyl-4-(6-methylpyridine-3-yloxy)phenylamino]quinozaline -6-yl}alyl)acetamide, a method for the preparation and use thereof for the treatment of cancer |
BRPI0413595B8 (pt) * | 2003-08-18 | 2021-05-25 | H Lundbeck As | sal de malonato, composição farmacêutica, uso de um sal de malonato, e, método de fabricação de um composto |
PL1841757T3 (pl) * | 2005-01-07 | 2010-10-29 | Pfizer Prod Inc | Heteroaromatyczne związki chinoliny i ich zastosowanie jako inhibitorów PDE10 |
WO2006078825A2 (en) | 2005-01-21 | 2006-07-27 | Cabot Corporation | Processes for forming nanoparticles |
BRPI0619962A2 (pt) * | 2005-12-16 | 2011-10-25 | Wyeth Corp | composições liofilizadas de um composto triazolopirimidina |
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- 2007-12-03 CN CN200780051566.5A patent/CN101611029B/zh not_active Expired - Fee Related
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- 2007-12-18 AR ARP070105692A patent/AR064417A1/es not_active Application Discontinuation
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Also Published As
Publication number | Publication date |
---|---|
RU2430918C2 (ru) | 2011-10-10 |
TW200833337A (en) | 2008-08-16 |
TWI359660B (en) | 2012-03-11 |
KR20120043775A (ko) | 2012-05-04 |
JP2008208114A (ja) | 2008-09-11 |
CA2673435A1 (en) | 2008-07-17 |
EP2125786A1 (en) | 2009-12-02 |
DK2125786T3 (da) | 2011-05-09 |
ES2360014T3 (es) | 2011-05-31 |
PL2125786T3 (pl) | 2011-07-29 |
ZA200904230B (en) | 2010-04-28 |
WO2008084299A1 (en) | 2008-07-17 |
US8283471B2 (en) | 2012-10-09 |
BRPI0720936A2 (pt) | 2014-03-11 |
CY1111919T1 (el) | 2015-11-04 |
DE602007013294D1 (de) | 2011-04-28 |
KR20090092338A (ko) | 2009-08-31 |
NZ577716A (en) | 2012-10-26 |
CN101611029A (zh) | 2009-12-23 |
ATE502028T1 (de) | 2011-04-15 |
PT2125786E (pt) | 2011-04-21 |
CA2673435C (en) | 2012-10-09 |
HK1134670A1 (en) | 2010-05-07 |
US20100063089A1 (en) | 2010-03-11 |
AU2007343135B2 (en) | 2013-03-21 |
AU2007343135A1 (en) | 2008-07-17 |
SI2125786T1 (sl) | 2011-05-31 |
EP2125786B1 (en) | 2011-03-16 |
CN101611029B (zh) | 2014-09-10 |
IL199389A (en) | 2014-01-30 |
MX2009006528A (es) | 2009-06-26 |
AR064417A1 (es) | 2009-04-01 |
RU2009123347A (ru) | 2011-01-27 |
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