TW527354B - Crystalline forms of (R)-(+)-N-[[3-[1-benzoyl-3-(3,4dichlorophenyl)piperidine-3-y1]prop-1-y1]-4-phenyl piperidine-4-y1]-N-methyl acetamide (osanetant) and a process for preparing them - Google Patents
Crystalline forms of (R)-(+)-N-[[3-[1-benzoyl-3-(3,4dichlorophenyl)piperidine-3-y1]prop-1-y1]-4-phenyl piperidine-4-y1]-N-methyl acetamide (osanetant) and a process for preparing them Download PDFInfo
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- TW527354B TW527354B TW088113235A TW88113235A TW527354B TW 527354 B TW527354 B TW 527354B TW 088113235 A TW088113235 A TW 088113235A TW 88113235 A TW88113235 A TW 88113235A TW 527354 B TW527354 B TW 527354B
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/56—Nitrogen atoms
- C07D211/58—Nitrogen atoms attached in position 4
-
- 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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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
527354 案號88113235 年月日 修正
O:\59\59659.ptc 第23頁
Claims (1)
- 527351113235 月 a 修正 六、申請專利範圍 」 1 · 一種結晶奥沙田(〇 s a n c t a n t)-結晶型I之方法,其特 徵在於奥沙田於乙醇中之溶液中加入水,然後加熱其至溫 度為6 0 t:至75 t ,然後冷卻至2〇。〇至25 t,然後開始結晶 作用或等至第1個結晶出現,然後增加溫度至4 5 - 5 0 t ,然 後冷卻至〇 t並保持此溫度。 … 2 ·—種結晶奥沙田-結晶型I之方法,其特徵在於將水加 。至奥沙田於乙醇中之溶液,然後加熱其至溫度為6 〇。〇至7 5 ’然後冷卻至4 0 °C,開始結晶作用,繼續冷卻至2 〇 - 2 5 c ’加熱該形成之奥沙田懸浮液至4 5 - 5 0 °C,然後冷卻至 2 0 - 2 5 〇C。、3 · 一種結晶奥沙田-結晶型I之方法,其特徵在於加熱奥 沙田於異丙醇中之溶液至溫度6 〇 _ 8 〇。〇,然後冷卻至溫度 。介於0和5 0 t:,然後開始結晶作用;該混合物然後冷卻至〇 C,保持此溫度。 4 · 一種結晶奥沙田-結晶型I丨之方法,其特徵在於加入 異丙基醚與水至奥沙田於乙醇中之溶液,然後於回流下加 熱,然後冷卻。5 · —種結晶奥沙田-結晶型丨丨之方法,其特徵在於回流 加熱奥沙田於乙醇/異丙基醚之混合物之溶液,加入異丙 基趟與水,使其冷卻至4 〇 - 5 〇,然後開始結晶作用或等 至第一個結晶出現於冷卻至2 〇 一 2 5 t之前。 6 ·根據申請專利範圍第1至5項中任一項之方法,其特徵 在於結晶出之奥沙田係經中和其苯石黃酸鹽以製得。 7 · —種奥沙田-結晶型I ,其特徵在於其顯示:527354 _案號88113235 年/月 日 修正_^ 六、申請專利範圍 -具有最大峰值為1 4 3. 6 ± 0 . 5 °C之熔點 - 68.5±0.5J /克之炫化熱函 - 其粉末X-ray繞射圖顯示17.81 ° 、11.04°與16. 84° 之Bragg 2 (9射線之特性。 8 ·根據申請專利範圍第7項之奥沙田-結晶型I ,其可由 根據申請專利範圍第1至3項中任一項之方法而製得。 9 · 一種奥沙田-結晶型I I ,其特徵在於其顯示: -具有最大峰值為141. 8± 0.5 °C之熔點 - 65.5±0.5J /克之炫化熱函 - 其粉末X-ray繞射圖顯示18.35° 、18. 58°與18.97° 之B r a g g 2 0射線之特性。 1 0 .根據申請專利範圍第9項之奥沙田-結晶型I I ,其可 由根據申請專利範圍第4或5項之方法而製得。 1 1 . 一種用作NK-3拮抗劑之醫藥組合物,其包括根據申 請專利範圍第7至1 0項中任一項之化合物做為活性主成 份。 1 2 .根據申請專利範圍第1 1項之醫藥組合物,其特徵在 於其劑量單位之形式包含0. 5至5 0 0毫克之活性主成份。 1 3.根據申請專利範圍第1 2項之醫藥組合物,其特徵在 於該劑量單位包含介於1至2 5 0毫克之活性主成份。O:\59\59659-920103.ptc 第25頁
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR9810107A FR2782082B3 (fr) | 1998-08-05 | 1998-08-05 | Formes cristallines de (r)-(+)-n-[[3-[1-benzoyl-3-(3,4- dichlorophenyl)piperidin-3-yl]prop-1-yl]-4-phenylpiperidin-4 -yl]-n-methylacetamide (osanetant) et procede pour la preparation dudit compose |
Publications (1)
Publication Number | Publication Date |
---|---|
TW527354B true TW527354B (en) | 2003-04-11 |
Family
ID=9529458
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
TW088113235A TW527354B (en) | 1998-08-05 | 1999-08-04 | Crystalline forms of (R)-(+)-N-[[3-[1-benzoyl-3-(3,4dichlorophenyl)piperidine-3-y1]prop-1-y1]-4-phenyl piperidine-4-y1]-N-methyl acetamide (osanetant) and a process for preparing them |
Country Status (32)
Country | Link |
---|---|
US (1) | US7041679B2 (zh) |
EP (1) | EP1102747B1 (zh) |
JP (1) | JP3807938B2 (zh) |
KR (1) | KR100571944B1 (zh) |
CN (1) | CN1114592C (zh) |
AR (1) | AR019953A1 (zh) |
AT (1) | ATE243197T1 (zh) |
AU (1) | AU748177B2 (zh) |
BR (1) | BR9913357A (zh) |
CA (1) | CA2339007A1 (zh) |
CO (1) | CO5070576A1 (zh) |
DE (1) | DE69908951T2 (zh) |
DK (1) | DK1102747T3 (zh) |
DZ (1) | DZ3074A1 (zh) |
EA (1) | EA003205B1 (zh) |
EE (1) | EE04274B1 (zh) |
ES (1) | ES2200535T3 (zh) |
FR (1) | FR2782082B3 (zh) |
HK (1) | HK1035535A1 (zh) |
HU (1) | HUP0103134A3 (zh) |
IS (1) | IS5821A (zh) |
MY (1) | MY121447A (zh) |
NO (1) | NO320645B1 (zh) |
NZ (1) | NZ509561A (zh) |
PL (1) | PL345999A1 (zh) |
PT (1) | PT1102747E (zh) |
SK (1) | SK1742001A3 (zh) |
TR (1) | TR200100261T2 (zh) |
TW (1) | TW527354B (zh) |
UA (1) | UA72890C2 (zh) |
WO (1) | WO2000007987A1 (zh) |
YU (1) | YU8601A (zh) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SE0100902D0 (sv) | 2001-03-15 | 2001-03-15 | Astrazeneca Ab | Compounds |
SE0202539D0 (sv) | 2002-08-27 | 2002-08-27 | Astrazeneca Ab | Compounds |
SE0401762D0 (sv) * | 2004-07-05 | 2004-07-05 | Astrazeneca Ab | Novel compounds |
US7648992B2 (en) * | 2004-07-05 | 2010-01-19 | Astrazeneca Ab | Hydantoin derivatives for the treatment of obstructive airway diseases |
SE0403086D0 (sv) * | 2004-12-17 | 2004-12-17 | Astrazeneca Ab | Compounds |
SE0403085D0 (sv) * | 2004-12-17 | 2004-12-17 | Astrazeneca Ab | Novel componds |
TW200800954A (en) * | 2006-03-16 | 2008-01-01 | Astrazeneca Ab | Novel crystal modifications |
TW200831488A (en) * | 2006-11-29 | 2008-08-01 | Astrazeneca Ab | Novel compounds |
TW202317533A (zh) * | 2021-07-02 | 2023-05-01 | 美商雅斯治療公司 | 奧沙奈坦(osanetant)之固體形式 |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2719311B1 (fr) * | 1994-03-18 | 1998-06-26 | Sanofi Sa | Composés antagonistes sélectifs du récepteur NK3 humain et leur utilisation comme médicaments et outils de diagnostic. |
JPH1053576A (ja) * | 1996-06-07 | 1998-02-24 | Eisai Co Ltd | 塩酸ドネペジルの多形結晶およびその製造法 |
EP0915849A2 (en) * | 1996-08-05 | 1999-05-19 | Smithkline Beecham S.p.A. | Process for the preparation of 3,3-disubstituted piperidines |
US6040316A (en) * | 1996-09-16 | 2000-03-21 | Warner-Lambert Company | 3-alkyl-3-phenyl-piperidines |
FR2757543B1 (fr) * | 1996-12-23 | 1999-04-02 | Sanofi Sa | Procede pour la cristallisation d'un derive de tetrahydropyridine et formes cristallines ainsi obtenues |
-
1998
- 1998-08-05 FR FR9810107A patent/FR2782082B3/fr not_active Expired - Lifetime
-
1999
- 1999-07-25 DZ DZ990156A patent/DZ3074A1/xx active
- 1999-07-28 AR ARP990103741A patent/AR019953A1/es unknown
- 1999-08-03 MY MYPI99003297A patent/MY121447A/en unknown
- 1999-08-03 EP EP99936672A patent/EP1102747B1/fr not_active Expired - Lifetime
- 1999-08-03 YU YU8601A patent/YU8601A/sh unknown
- 1999-08-03 UA UA2001010591A patent/UA72890C2/xx unknown
- 1999-08-03 WO PCT/FR1999/001914 patent/WO2000007987A1/fr not_active Application Discontinuation
- 1999-08-03 PT PT99936672T patent/PT1102747E/pt unknown
- 1999-08-03 DK DK99936672T patent/DK1102747T3/da active
- 1999-08-03 CN CN99810182A patent/CN1114592C/zh not_active Expired - Fee Related
- 1999-08-03 ES ES99936672T patent/ES2200535T3/es not_active Expired - Lifetime
- 1999-08-03 BR BR9913357-1A patent/BR9913357A/pt not_active IP Right Cessation
- 1999-08-03 KR KR1020017001460A patent/KR100571944B1/ko not_active IP Right Cessation
- 1999-08-03 EE EEP200100070A patent/EE04274B1/xx not_active IP Right Cessation
- 1999-08-03 PL PL99345999A patent/PL345999A1/xx not_active Application Discontinuation
- 1999-08-03 AT AT99936672T patent/ATE243197T1/de not_active IP Right Cessation
- 1999-08-03 DE DE69908951T patent/DE69908951T2/de not_active Expired - Fee Related
- 1999-08-03 JP JP2000563621A patent/JP3807938B2/ja not_active Expired - Fee Related
- 1999-08-03 HU HU0103134A patent/HUP0103134A3/hu unknown
- 1999-08-03 NZ NZ509561A patent/NZ509561A/xx unknown
- 1999-08-03 EA EA200100096A patent/EA003205B1/ru not_active IP Right Cessation
- 1999-08-03 CA CA002339007A patent/CA2339007A1/en not_active Abandoned
- 1999-08-03 SK SK174-2001A patent/SK1742001A3/sk unknown
- 1999-08-03 TR TR2001/00261T patent/TR200100261T2/xx unknown
- 1999-08-03 AU AU51685/99A patent/AU748177B2/en not_active Ceased
- 1999-08-04 TW TW088113235A patent/TW527354B/zh not_active IP Right Cessation
- 1999-08-04 CO CO99049286A patent/CO5070576A1/es unknown
-
2001
- 2001-01-23 IS IS5821A patent/IS5821A/is unknown
- 2001-02-01 NO NO20010553A patent/NO320645B1/no unknown
- 2001-09-04 HK HK01106232A patent/HK1035535A1/xx not_active IP Right Cessation
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2003
- 2003-08-28 US US10/651,313 patent/US7041679B2/en not_active Expired - Fee Related
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