JP2001508077A - 2−アミノ−4−(4−フルオルベンジルアミノ)−1−エトキシカルボニル−アミノベンゼンの新規変態ならびにその製造法 - Google Patents
2−アミノ−4−(4−フルオルベンジルアミノ)−1−エトキシカルボニル−アミノベンゼンの新規変態ならびにその製造法Info
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- JP2001508077A JP2001508077A JP53362698A JP53362698A JP2001508077A JP 2001508077 A JP2001508077 A JP 2001508077A JP 53362698 A JP53362698 A JP 53362698A JP 53362698 A JP53362698 A JP 53362698A JP 2001508077 A JP2001508077 A JP 2001508077A
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- Prior art keywords
- modification
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- process according
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- 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.)
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/26—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
- C07C271/28—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pain & Pain Management (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Biomedical Technology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Rheumatology (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.X線回折図によって特性決定され、その際に別の2つの変態の反射とは一緒 に起こらない反射は、特に6.97°2θ(12.67Å)、18.02°2θ (4.92Å)および19.94°2θ(4.45Å)の際に観察される化合物 I の変態。 2.X線回折図によって特性決定され、その際に2つの変態の反射とは一緒に起 こらない反射は、特に15.00°2θ(5.90Å)、19.29°2θ(4 .60Å)および19.58°2θ(4.53Å)の際に観察される化合物Iの 変態B。 3.X線回折図によって特性決定され、その際に別の2つの変態の反射とは一緒 に起こらない反射は、特に9.70°2θ(9.11Å)および21.74°θ (4.09Å)の際に観察される化合物Iの変態C。 4.請求項1記載の変態Aの製造法において、化合物Iの過飽和の溶液からプロ トン性、双極性の非プロトン性または非極性の溶剤中で純粋な結晶形を晶出 させることを特徴とする、請求項1記載の変態Aの製造法。 5.溶液からの結晶化を−20℃〜110℃、特に20℃〜50℃の温度で実施 する、請求項4記載の変態Aの製造法。 6.プロトン性溶剤として低級アルコール、例えばエタノール、2−プロパノー ルまたはn−ブタノールを使用することができ、双極性の非プロトン性溶剤とし てアセトニトリルまたはアセトンを使用することができ、かつ非極性の溶剤とし てトルオールを使用することができる、請求項4または5記載の変態Aの製造法 。 7.有利に低級アルコールを溶剤として使用する、請求項6記載の方法。 8.変態BおよびCの物質をプロトン性、双極性の非プロトン性または非プロト ン性の溶剤を用いて低い温度で、特に室温で処理する、請求項1記載の変態Aの 製造法。 9.プロトン性または非極性の溶剤中の化合物Iの飽和溶液から純粋な結晶形を 80℃を上廻る温度で晶出させる、請求項2記載の変態Bの製造法。 10.有利にプロトン性溶剤として水を使用し、非極性の溶剤としてトルオール を使用する、請求項9記載の変態Bの製造法。 11.変態Bを熱的相転移によって特に変態Aから8 0℃を上廻る温度で製造する、請求項2記載の変態Bの製造法。 12.プロトン性または非極性の溶剤中の化合物Iの飽和溶液から純粋な結晶形 を有利に50℃〜70℃の温度で晶出させる、請求項3記載の変態Cの製造法。 13.プロトン性溶剤として有利にエタノールまたはプロパノールを使用し、非 極性の溶剤としてトルオールを使用する、請求項12記載の変態Cの製造法。 14.溶液からの結晶化を有利に60℃〜70℃の温度で実施する、請求項12 記載の変態Cの製造法。 15.製薬学的製剤を製造するための化合物Iの変態A、BおよびCの使用。 16.化合物Iの変態A、BまたはCおよび場合により担持剤および/または助 剤を含有する医薬品。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE19701694.4 | 1997-01-20 | ||
DE19701694A DE19701694A1 (de) | 1997-01-20 | 1997-01-20 | Neue Modifikationen des 2-Amino-4-(4-fluorbenzylamino)-l-ethoxycarbonyl-aminobenzen sowie Verfahren zu ihrer Herstellung |
PCT/EP1998/000086 WO1998031663A1 (de) | 1997-01-20 | 1998-01-09 | Neue modifikationen des 2-amino-4-(4-fluorbenzylamino)-1-ethoxycarbonyl-aminobenzen sowie verfahren zu ihrer herstellung |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2001508077A true JP2001508077A (ja) | 2001-06-19 |
JP4138886B2 JP4138886B2 (ja) | 2008-08-27 |
Family
ID=7817756
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP53362698A Expired - Lifetime JP4138886B2 (ja) | 1997-01-20 | 1998-01-09 | 2−アミノ−4−(4−フルオルベンジルアミノ)−1−エトキシカルボニル−アミノベンゼンの新規変態ならびにその製造法 |
Country Status (31)
Country | Link |
---|---|
US (2) | US5914425A (ja) |
EP (1) | EP0956281B1 (ja) |
JP (1) | JP4138886B2 (ja) |
CN (1) | CN1125812C (ja) |
AR (1) | AR015349A1 (ja) |
AT (1) | ATE222235T1 (ja) |
AU (1) | AU730776B2 (ja) |
BG (1) | BG63893B1 (ja) |
BR (1) | BR9806784A (ja) |
CA (3) | CA2634811C (ja) |
CZ (1) | CZ301778B6 (ja) |
DE (2) | DE19701694A1 (ja) |
DK (1) | DK0956281T3 (ja) |
EG (1) | EG21239A (ja) |
ES (1) | ES2178152T3 (ja) |
HK (1) | HK1024230A1 (ja) |
HU (1) | HU227625B1 (ja) |
ID (1) | ID22645A (ja) |
IL (1) | IL130384A (ja) |
IS (1) | IS2115B (ja) |
NO (2) | NO311642B1 (ja) |
NZ (1) | NZ336205A (ja) |
PL (1) | PL195956B1 (ja) |
PT (1) | PT956281E (ja) |
RU (1) | RU2186765C2 (ja) |
SK (1) | SK285303B6 (ja) |
TR (1) | TR199901674T2 (ja) |
TW (1) | TW531527B (ja) |
UA (1) | UA63937C2 (ja) |
WO (1) | WO1998031663A1 (ja) |
ZA (1) | ZA98319B (ja) |
Families Citing this family (35)
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US6348486B1 (en) | 2000-10-17 | 2002-02-19 | American Home Products Corporation | Methods for modulating bladder function |
US6589986B2 (en) | 2000-12-20 | 2003-07-08 | Wyeth | Methods of treating anxiety disorders |
US20020183395A1 (en) * | 2001-04-04 | 2002-12-05 | Wyeth | Methods for treating hyperactive gastric motility |
US20050089559A1 (en) * | 2003-10-23 | 2005-04-28 | Istvan Szelenyi | Combinations of potassium channel openers and sodium channel inhibitors or sodium channel-influencing active compounds for treating pains |
US7960436B2 (en) * | 2006-06-05 | 2011-06-14 | Valeant Pharmaceuticals International | Substituted arylamino-1,2,3,4-tetrahydro naphthalenes and-2,3-dihydro-1H-indenes as potassium channel modulators |
US20080045534A1 (en) * | 2006-08-18 | 2008-02-21 | Valeant Pharmaceuticals North America | Derivatives of 1,3-diamino benzene as potassium channel modulators |
US8993593B2 (en) * | 2006-08-23 | 2015-03-31 | Valeant Pharmaceuticals International | N-(4-(6-fluoro-3,4-dihydroisoquinolin-2(1H)-yl)-2,6-dimethylphenyl)-3,3-dimethylbutanamide as potassium channel modulators |
CN101563085A (zh) * | 2006-08-23 | 2009-10-21 | 威朗国际制药公司 | 作为钾通道调节剂的4-(n-氮杂环烷基)酰苯胺的衍生物 |
US8722929B2 (en) * | 2006-10-10 | 2014-05-13 | Valeant Pharmaceuticals International | N-[2-amino-4-(phenylmethoxy)phenyl] amides and related compounds as potassium channel modulators |
AU2007325629A1 (en) * | 2006-11-28 | 2008-06-05 | Valeant Pharmaceuticals International | 1,4 diamino bicyclic retigabine analogues as potassium channel modulators |
US8367684B2 (en) * | 2007-06-13 | 2013-02-05 | Valeant Pharmaceuticals International | Derivatives of 4-(N-azacycloalkyl) anilides as potassium channel modulators |
US8563566B2 (en) | 2007-08-01 | 2013-10-22 | Valeant Pharmaceuticals International | Naphthyridine derivatives as potassium channel modulators |
US7786146B2 (en) * | 2007-08-13 | 2010-08-31 | Valeant Pharmaceuticals International | Derivatives of 5-amino-4,6-disubstituted indole and 5-amino-4,6-disubstituted indoline as potassium channel modulators |
MX2011000636A (es) * | 2008-07-18 | 2011-08-03 | Valeant Pharmaceuticals Int | Formulacion de liberacion modificada y metodos de uso. |
US20100323015A1 (en) * | 2008-07-18 | 2010-12-23 | Biljana Nadjsombati | Modified release formulation and methods of use |
US20100323016A1 (en) * | 2008-07-18 | 2010-12-23 | Biljana Nadjsombati | Modified release formulation and methods of use |
DE102009013611A1 (de) | 2009-03-17 | 2010-09-23 | Ratiopharm Gmbh | Festes Retigabin in nicht-kristalliner Form |
DE102009013613A1 (de) | 2009-03-17 | 2010-09-23 | Ratiopharm Gmbh | Trockenverarbeitung von Retigabin |
DE102009013612A1 (de) | 2009-03-17 | 2010-09-23 | Ratiopharm Gmbh | Retigabin-Tabletten, bevorzugt mit modifizierter Freisetzung |
WO2011039369A2 (en) | 2009-10-02 | 2011-04-07 | Medichem S.A. | Amorphous forms of a 2-amino-4-(4-fluorobenzylamino)phenylcarbamate derivative |
CN102802615A (zh) | 2010-01-20 | 2012-11-28 | 葛兰素集团有限公司 | 新瑞替加滨组合物 |
WO2011101456A2 (en) * | 2010-02-19 | 2011-08-25 | Medichem S.A. | Stabilized phenylcarbamate derivative in solid state |
CN202095728U (zh) * | 2010-10-29 | 2012-01-04 | 假日集团控股有限公司 | 行李箱把手 |
CN102464233A (zh) * | 2010-11-18 | 2012-05-23 | 江苏邦威机械制造有限公司 | 一种卧式差速缠丝机用应力发生装置 |
WO2012098075A1 (en) | 2011-01-18 | 2012-07-26 | Glaxo Group Limited | Process for the preparation of retigabine |
CN102241608A (zh) * | 2011-05-12 | 2011-11-16 | 天津市汉康医药生物技术有限公司 | 瑞替加滨化合物及其组合物 |
WO2013008250A2 (en) * | 2011-07-01 | 2013-01-17 | Dr.Reddys Laboratories Limited. | Crystalline form of retigabine and processes for mixture of retigabine crystalline modifications |
WO2013011518A1 (en) | 2011-07-21 | 2013-01-24 | Arch Pharmalabs Limited | Process for the preparation of retigabine of the formula i and pharmaceutically acceptable salts thereof |
CN102531966B (zh) * | 2011-12-23 | 2013-07-24 | 山东创新药物研发有限公司 | 瑞替加滨的晶型d及其制备方法 |
WO2013114379A1 (en) * | 2012-01-30 | 2013-08-08 | Symed Labs Limited | Novel polymorphs of n-[2-amino-4-(4-fluorobenzylamino)-phenyl] carbamic acid ethyl ester and processes thereof |
CN103373941B (zh) * | 2012-04-11 | 2016-08-17 | 浙江九洲药物科技有限公司 | 瑞替加滨及其中间体的制备方法 |
WO2013179298A2 (en) * | 2012-04-23 | 2013-12-05 | Cadila Healthcare Limited | A process for preparation of phenyl carbamate derivative and polymorphic forms thereof |
WO2014023270A1 (en) | 2012-08-09 | 2014-02-13 | Zentiva, K.S. | Salts or co-crystals of ethyl n-[2-amino-4-[(4-fluorophenyl)methylamino]-phenyl]carbamate |
CN102964273B (zh) * | 2012-12-06 | 2014-04-02 | 北京英科博雅科技有限公司 | 瑞替加滨的新晶型f及其制备方法 |
USD773819S1 (en) | 2015-05-27 | 2016-12-13 | Travelpro Products, Inc. | Handle for luggage |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE4200259A1 (de) * | 1992-01-08 | 1993-07-15 | Asta Medica Ag | Neue 1,2,4-triaminobenzol-derivate und verfahren zu deren herstellung |
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1997
- 1997-01-20 DE DE19701694A patent/DE19701694A1/de not_active Ceased
-
1998
- 1998-01-09 DE DE59805186T patent/DE59805186D1/de not_active Expired - Lifetime
- 1998-01-09 BR BR9806784-2A patent/BR9806784A/pt not_active Application Discontinuation
- 1998-01-09 SK SK956-99A patent/SK285303B6/sk not_active IP Right Cessation
- 1998-01-09 HU HU0000944A patent/HU227625B1/hu active Protection Beyond IP Right Term
- 1998-01-09 CZ CZ0250899A patent/CZ301778B6/cs not_active IP Right Cessation
- 1998-01-09 RU RU99118590/04A patent/RU2186765C2/ru not_active IP Right Cessation
- 1998-01-09 DK DK98904048T patent/DK0956281T3/da active
- 1998-01-09 EP EP98904048A patent/EP0956281B1/de not_active Expired - Lifetime
- 1998-01-09 TR TR1999/01674T patent/TR199901674T2/xx unknown
- 1998-01-09 NZ NZ336205A patent/NZ336205A/xx not_active IP Right Cessation
- 1998-01-09 PT PT98904048T patent/PT956281E/pt unknown
- 1998-01-09 AT AT98904048T patent/ATE222235T1/de active
- 1998-01-09 CA CA2634811A patent/CA2634811C/en not_active Expired - Lifetime
- 1998-01-09 US US09/004,926 patent/US5914425A/en not_active Expired - Lifetime
- 1998-01-09 CA CA2632585A patent/CA2632585C/en not_active Expired - Lifetime
- 1998-01-09 WO PCT/EP1998/000086 patent/WO1998031663A1/de active IP Right Grant
- 1998-01-09 ES ES98904048T patent/ES2178152T3/es not_active Expired - Lifetime
- 1998-01-09 JP JP53362698A patent/JP4138886B2/ja not_active Expired - Lifetime
- 1998-01-09 PL PL98335647A patent/PL195956B1/pl unknown
- 1998-01-09 CA CA002278201A patent/CA2278201C/en not_active Expired - Lifetime
- 1998-01-09 ID IDW990520A patent/ID22645A/id unknown
- 1998-01-09 AU AU62081/98A patent/AU730776B2/en not_active Ceased
- 1998-01-09 CN CN98801733A patent/CN1125812C/zh not_active Expired - Lifetime
- 1998-01-09 IL IL13038498A patent/IL130384A/xx not_active IP Right Cessation
- 1998-01-10 EG EG3098A patent/EG21239A/xx active
- 1998-01-15 ZA ZA9800319A patent/ZA98319B/xx unknown
- 1998-01-15 TW TW087100485A patent/TW531527B/zh not_active IP Right Cessation
- 1998-01-20 AR ARP980100249A patent/AR015349A1/es active IP Right Grant
- 1998-09-01 UA UA99084740A patent/UA63937C2/uk unknown
- 1998-10-29 US US09/181,671 patent/US6538151B1/en not_active Expired - Lifetime
-
1999
- 1999-06-29 IS IS5098A patent/IS2115B/is unknown
- 1999-07-13 NO NO19993452A patent/NO311642B1/no not_active IP Right Cessation
- 1999-08-10 BG BG103657A patent/BG63893B1/bg unknown
-
2000
- 2000-06-16 HK HK00103629A patent/HK1024230A1/xx not_active IP Right Cessation
-
2011
- 2011-09-16 NO NO2011017C patent/NO2011017I2/no unknown
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