JP2010195828A - ムスカリン性レセプターアンタゴニストの安定水和物 - Google Patents
ムスカリン性レセプターアンタゴニストの安定水和物 Download PDFInfo
- Publication number
- JP2010195828A JP2010195828A JP2010126865A JP2010126865A JP2010195828A JP 2010195828 A JP2010195828 A JP 2010195828A JP 2010126865 A JP2010126865 A JP 2010126865A JP 2010126865 A JP2010126865 A JP 2010126865A JP 2010195828 A JP2010195828 A JP 2010195828A
- Authority
- JP
- Japan
- Prior art keywords
- bladder
- hydrate
- darifenacin
- solution
- dihydrobenzofuran
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
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- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
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- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- 239000008109 sodium starch glycolate Substances 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
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- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A61P13/00—Drugs for disorders of the urinary system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
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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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- Chemical Kinetics & Catalysis (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
【解決手段】ダリフェナシンの安定固体水和物の提供により上記課題を解決する。
【選択図】なし
Description
LRMS (電子スプレー、陽イオン):m/z [MH+] 263.
1H NMR (300 MHz, CDCl3):δ = 1.85-2.20 (2H, m), 3.16 & 3.18 (2H, t, J 9 Hz), 3.20-3.85 (7H, m), 4.54 & 4.55 (2H, t, J 9 Hz), 6.68 & 6.70 (1H, d, J 9 Hz), 6.83 & 6.94 (1H, d, J 9 Hz), 7.05 & 7.12 (1H, s), 7.22-7.48 (10H, m).
LRMS (電子スプレー、陽イオン):m/z [MH+] 423.
LRMS (電子スプレー、陽イオン):m/z [MH+] 409
LRMS (電子スプレー、陽イオン):m/z [MH+] 409.
トルエンに関して、2.3に1のモル比に相当するシグナルが観察され、これは(S)−2−{1−[2−(2,3−ジヒドロベンゾフラン−5−イル)エチル]−3−ピロリジニル}−2,2−ジフェニルアセトアミドの芳香族領域に重なって存在する。
カール・フィッシャー(Karl Fischer)法による含水率:2.7% w/w
Claims (1)
- ダリフェナシンの安定固体水和物。
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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GBGB0207104.1A GB0207104D0 (en) | 2002-03-26 | 2002-03-26 | Stable hydrate of a muscarinic receptor antagonist |
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JP2003578353A Division JP2005524678A (ja) | 2002-03-26 | 2003-03-17 | ムスカリン性レセプターアンタゴニストの安定水和物 |
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EP (2) | EP1490357B1 (ja) |
JP (2) | JP2005524678A (ja) |
KR (4) | KR101026283B1 (ja) |
CN (1) | CN100345840C (ja) |
AR (1) | AR042608A1 (ja) |
AT (1) | ATE495169T1 (ja) |
AU (1) | AU2003209921A1 (ja) |
BR (2) | BRPI0308706B8 (ja) |
CA (1) | CA2480287C (ja) |
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GB (1) | GB0207104D0 (ja) |
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PA (1) | PA8569701A1 (ja) |
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WO (1) | WO2003080599A1 (ja) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
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GB0207104D0 (en) * | 2002-03-26 | 2002-05-08 | Pfizer Ltd | Stable hydrate of a muscarinic receptor antagonist |
US7244765B2 (en) * | 2004-06-25 | 2007-07-17 | Cytokine Pharmasciences, Inc | Guanylhydrazone salts, compositions, processes of making and methods of using |
CN101203217A (zh) * | 2005-04-24 | 2008-06-18 | 惠氏公司 | 调节膀胱功能的方法 |
US20070203221A1 (en) * | 2005-12-27 | 2007-08-30 | Valeriano Merli | Processes for preparing darifenacin hydrobromide |
EP2109601A2 (en) * | 2007-01-05 | 2009-10-21 | Dr. Reddy's Laboratories Ltd. | Preparation of darifenacin and its salts |
CA2675942C (en) * | 2007-02-23 | 2016-04-12 | Theravance, Inc. | Quaternary ammonium diphenylmethyl compounds useful as muscarinic receptor antagonists |
WO2008144602A1 (en) * | 2007-05-18 | 2008-11-27 | Auspex Pharmaceuticals, Inc. | Deuterated zamifenacin derivatives |
WO2009007853A2 (en) * | 2007-06-08 | 2009-01-15 | Actavis Group Ptc Ehf | Novel polymorphs of darifenacin free base and its hydrobromide salt |
US20090005431A1 (en) * | 2007-06-30 | 2009-01-01 | Auspex Pharmaceuticals, Inc. | Substituted pyrrolidines |
US20090018346A1 (en) * | 2007-07-13 | 2009-01-15 | Medichem, S.A. | Amorphous Form Of Darifenacin Hydrobromide And Processes For The Preparation Thereof |
CZ200845A3 (cs) * | 2008-01-28 | 2009-09-02 | Zentiva, A. S. | Zpusob prípravy Darifenacinu |
WO2009125426A2 (en) * | 2008-02-08 | 2009-10-15 | Neuland Laboratories Ltd | NOVEL PROCESS FOR THE PREPARATION OF (3SM-[2-(2 J-DIHYDRO-5- BENZOFURANYLϊETHYL]-α.α -DIPHENYL-3-PYRROLIDINEACETAMIDE HYDROBROMIDE |
CN101983187A (zh) | 2008-04-02 | 2011-03-02 | 株式会社钟化 | (s)-3-(1-氰基-1,1-二苯基甲基)吡咯烷的制备方法 |
WO2010032225A2 (en) * | 2008-09-22 | 2010-03-25 | Watson Pharma Private Limited | Process for preparation of darifenacin and intermediates used in the process |
EP2236509A1 (en) | 2009-04-01 | 2010-10-06 | Ragactives, S.L. | Method for obtaining 1,3-difunctionalized pyrrolidine derivatives |
WO2011070419A1 (en) | 2009-12-10 | 2011-06-16 | Aurobindo Pharma Limited | An improved process for the preparation of darifenacin hydrobromide |
JP6440625B2 (ja) | 2012-11-14 | 2018-12-19 | ザ・ジョンズ・ホプキンス・ユニバーシティー | 精神分裂病を処置するための方法および組成物 |
CN108463224A (zh) * | 2015-12-14 | 2018-08-28 | 铁木医药有限公司 | sGC刺激剂用于胃肠功能障碍治疗的应用 |
KR102430610B1 (ko) * | 2016-08-12 | 2022-08-08 | 바이엘 크롭사이언스 악티엔게젤샤프트 | 치환된 스티렌 유도체의 제조 방법 |
Citations (3)
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JPH02282360A (ja) * | 1989-03-17 | 1990-11-19 | Pfizer Inc | ピロリジン誘導体 |
JPH10511112A (ja) * | 1995-09-15 | 1998-10-27 | ファイザー・インコーポレーテッド | ダリフェナシン含有製剤 |
JP2005524678A (ja) * | 2002-03-26 | 2005-08-18 | ノバルティス・インターナショナル・ファーマシューティカル・リミテッド | ムスカリン性レセプターアンタゴニストの安定水和物 |
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US5233053A (en) * | 1989-03-17 | 1993-08-03 | Pfizer Inc. | Pyrrolidine derivatives |
US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
GB9400600D0 (en) | 1994-01-14 | 1994-03-09 | Pfizer Ltd | Treatment of motion seckness |
GB9612710D0 (en) * | 1996-06-18 | 1996-08-21 | Pfizer Ltd | Method of treatment |
AU4421697A (en) * | 1996-09-19 | 1998-04-14 | American Home Products Corporation | Method of treating urinary incontinence |
GB9711643D0 (en) | 1997-06-05 | 1997-07-30 | Janssen Pharmaceutica Nv | Glass thermoplastic systems |
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