CN1582282A - 新颖的取代的四环系四氢呋喃衍生物的扁桃酸盐化合物 - Google Patents
新颖的取代的四环系四氢呋喃衍生物的扁桃酸盐化合物 Download PDFInfo
- Publication number
- CN1582282A CN1582282A CNA02821918XA CN02821918A CN1582282A CN 1582282 A CN1582282 A CN 1582282A CN A02821918X A CNA02821918X A CN A02821918XA CN 02821918 A CN02821918 A CN 02821918A CN 1582282 A CN1582282 A CN 1582282A
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- CN
- China
- Prior art keywords
- mandelate
- compound
- dibenzo
- furans
- hydrogen
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D307/93—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
-
- 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
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Addiction (AREA)
- Anesthesiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Plural Heterocyclic Compounds (AREA)
- Furan Compounds (AREA)
Abstract
Description
盐 | 条件 | TGA<100℃ | IR | DSCMax ΔH(℃) (J/g) | 外观 | |
酒石酸盐 | 0天 | 0.0 | Ref | 158.8 | 85.9 | 白色 |
RT/<5%RH | 0.0 | ~Ref | 160.3 | 86.4 | 白色 | |
RT/<56%RH | 0.1 | ~Ref | 159.0 | 86.2 | 白色 | |
RT/<75%RH | 0.0 | ~Ref | 159.0 | 98.5 | 白色 | |
扁桃酸盐 | 0天 | 0.1 | Ref | 229.5 | 141.1 | 白色 |
RT/<5%RH | 0.1 | ~Ref | 229.1 | 140.2 | 白色 | |
25℃/60%RH | 0.1 | ~Ref | 229.1 | 139.0 | 白色 | |
RT/75%RH | 0.1 | ~Ref | 229.4 | 137.6 | 白色 | |
柠檬酸盐 | 0天 | (*) | Ref | 无定形 | 带黄色 | |
RT/<5%RH | (*) | (*) | (*) | 液化 | ||
(+)二甲苯酰酒石酸盐 | 0天 | 0.2 | Ref | 173.7 | 71.9 | 白色 |
RT/<5%RH | 0.3 | ~Ref | 175.6 | 78.7 | 白色 | |
25℃/60%RH | 0.1 | ~Ref | 177.6 | 74.7 | 白色 | |
RT/75%RH | 0.2 | ~Ref | 178.6 | 70.8 | 白色 |
盐 | 条件 | HPLC杂质总和 | 外观 | ||||
2星期 | 4星期 | 8星期 | 2星期 | 4星期 | 8星期 | ||
酒石酸盐 | 参考值 | 0.72 | - | - | 白色 | ||
人工光线 | 0.79 | - | - | 白色 | |||
40℃/75%RH | 0.72 | 0.83 | 0.93 | 白色 | 白色 | 几乎白色 | |
50℃ | 0.72 | 0.77 | 0.79 | 白色 | 白色 | 几乎白色 | |
日光 | 0.75 | 0.85 | 0.91 | 白色 | 几乎白色 | 略呈黄色 | |
RT/<5%RH | - | 0.73 | 0.75 | 白色 | 白色 | ||
25℃/60%RH | - | 0.75 | 0.77 | 白色 | 白色 | ||
RT/75%RH | - | 0.72 | 0.80 | 白色 | 白色 | ||
扁桃酸盐 | 参考值 | 1.72 | - | - | 白色 | ||
人工光线 | 1.70 | - | - | 白色 | |||
0.3daICH光 | 1.70 | - | - | 白色 | |||
40℃/75%RH | 1.73 | 1.73 | 1.70 | 白色 | 白色 | 白色 | |
50℃ | 1.74 | 1.75 | 1.70 | 白色 | 白色 | 白色 | |
日光 | 1.73 | 1.71 | 1.72 | 白色 | 白色 | 白色 | |
RT/<5%RH | - | 1.73 | 1.72 | 白色 | 白色 | ||
25℃/60%RH | - | 1.71 | 1.69 | 白色 | 白色 | ||
RT/75%RH | - | 1.75 | 1.76 | 白色 | 白色 |
盐 | 条件 | HPLC杂质总和 | 外观 | ||||
2星期 | 4星期 | 8星期 | 2星期 | 4星期 | 8星期 | ||
柠檬酸盐 | 参考值 | 4.76 | - | - | 黄色 | ||
人工光线 | 8.99 | - | - | 黄褐色 | |||
40℃/75%RH | 4.83 | 7.91 | 10.62 | 液化 | 液化 | 液化 | |
50℃ | 6.29 | 7.47 | 9.07 | 黄褐色 | 黄褐色 | 橘色-棕色 | |
日光 | 5.81 | 5.99 | 6.31 | 黄褐色 | 黄褐色 | 橘色-棕色 | |
RT/75%RH | - | 4.69 | 4.98 | - | 液化 | 液化 | |
(+)二甲苯酰酒石酸盐 | 参考值 | 1.01 | - | - | 白色 | - | - |
人工光线 | 1.57 | - | - | 白色 | - | - | |
0.3daICH光 | 1.41 | - | - | 白色 | - | - | |
40℃/75%RH | 0.98 | 1.00 | 1.09 | 白色 | 白色 | 白色 | |
50℃ | 1.06 | 1.22 | 1.25 | 白色 | 白色 | 白色 | |
日光 | 1.26 | 1.65 | 1.74 | 白色 | 白色 | 白色-黄色 |
Claims (10)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP01204465.7 | 2001-11-09 | ||
EP01204465 | 2001-11-09 | ||
PCT/EP2002/011136 WO2003040122A1 (en) | 2001-11-09 | 2002-11-08 | Novel mandelate salts of substituted tetracyclic tetrahydrofuran derivatives |
Publications (2)
Publication Number | Publication Date |
---|---|
CN1582282A true CN1582282A (zh) | 2005-02-16 |
CN1582282B CN1582282B (zh) | 2012-06-06 |
Family
ID=8181272
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN02821918XA Expired - Fee Related CN1582282B (zh) | 2001-11-09 | 2002-11-08 | 取代的四环系四氢呋喃衍生物的扁桃酸盐化合物 |
Country Status (25)
Country | Link |
---|---|
US (1) | US7317115B2 (zh) |
EP (1) | EP1446397B1 (zh) |
JP (1) | JP2005508988A (zh) |
KR (1) | KR100962325B1 (zh) |
CN (1) | CN1582282B (zh) |
AR (1) | AR037285A1 (zh) |
AT (1) | ATE299138T1 (zh) |
AU (1) | AU2002349327B2 (zh) |
BR (1) | BR0212770A (zh) |
CA (1) | CA2465043C (zh) |
DE (1) | DE60204982T2 (zh) |
EA (1) | EA006980B1 (zh) |
ES (1) | ES2244818T3 (zh) |
HR (1) | HRP20040395A2 (zh) |
HU (1) | HUP0402224A3 (zh) |
IL (2) | IL161866A0 (zh) |
MX (1) | MXPA04004365A (zh) |
MY (1) | MY128237A (zh) |
NO (1) | NO328548B1 (zh) |
NZ (1) | NZ531739A (zh) |
PL (1) | PL368456A1 (zh) |
TW (1) | TW200407117A (zh) |
UA (1) | UA79248C2 (zh) |
WO (1) | WO2003040122A1 (zh) |
ZA (1) | ZA200403454B (zh) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE60203937T2 (de) * | 2001-12-07 | 2006-05-11 | Janssen Pharmaceutica N.V. | Herstellung von trans-kondensierte 3,3a,8,12b-tetrahydro-2h-dibenzo[3,4:6,7]cyclohepta[1,2-b]furan derivaten |
WO2005013969A1 (en) * | 2003-07-15 | 2005-02-17 | Janssen Pharmaceutica N.V. | Antipsychotic agent with socializing properties |
RU2401257C2 (ru) | 2004-12-07 | 2010-10-10 | Янссен Фармацевтика Н.В. | Новые замещенные тетрациклические производные тетрагидрофурана, пирролидина и тетрагидротиофена |
MX2007009092A (es) | 2005-01-27 | 2007-09-12 | Janssen Pharmaceutica Nv | Derivados de tetrahidrofurano tetraciclicos heterociclicos como inhibidores de 5ht2 en el tratamiento de trastornos del sistema nervioso central. |
AU2006259020C1 (en) | 2005-06-17 | 2012-01-19 | Janssen Pharmaceutica N.V. | Novel tetracyclic tetrahydrofuran derivatives containing a cyclic amine side chain |
US8765223B2 (en) * | 2008-05-08 | 2014-07-01 | Air Products And Chemicals, Inc. | Binary and ternary metal chalcogenide materials and method of making and using same |
US8507040B2 (en) | 2008-05-08 | 2013-08-13 | Air Products And Chemicals, Inc. | Binary and ternary metal chalcogenide materials and method of making and using same |
US8962675B1 (en) * | 2013-09-12 | 2015-02-24 | Abbvie Inc. | Atrasentan mandelate salts |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3644462A1 (de) * | 1986-12-24 | 1988-07-07 | Basf Ag | Verfahren zur herstellung von 5h-dibenzo(a,d)cyclohepten-5-onen |
JP2656720B2 (ja) * | 1992-12-09 | 1997-09-24 | 武田薬品工業株式会社 | 光学活性アミノクマラン誘導体 |
ATE201680T1 (de) * | 1994-03-16 | 2001-06-15 | Cenes Ltd | 2,3,4,5-tetrahydro-1h-3-benzazepin säure- additions-salze |
DE69720709T2 (de) * | 1996-04-12 | 2004-03-11 | Janssen Pharmaceutica N.V. | Substituierte tetracyclische tetrahydrofuranderivate |
KR19990044257A (ko) | 1996-05-20 | 1999-06-25 | 디르크 반테 | 생체이용율이 개선된 항진균성 조성물 |
UA52778C2 (uk) * | 1997-10-10 | 2003-01-15 | Янссен Фармацевтика Н.В. | Галогенозаміщені тетрациклічні похідні тетрагідрофурану, спосіб їх отримання та композиція на їх основі |
US6281247B1 (en) * | 1998-03-03 | 2001-08-28 | Novo Nordisk A/S | Salt forms of (2E)-5-amino-5-methylhex-2-enoic acid N-methyl-N-((1R)-1-(N-methyl-N-((1R)-1-(methylcarbamoyl)-2-phenylethyl)carbamoyl)-2-(2-naphthyl)ethyl)amide |
HUP9904624A2 (hu) * | 1999-12-17 | 2002-01-28 | Sanofi-Synthelabo | Szacharinszármazékok, eljárás előállításukra, az ezeket tartalmazó gyógyszerkészítmények és intermedierjeik |
EP1186303A3 (en) * | 2000-09-06 | 2003-12-10 | Pfizer Products Inc. | Pharmaceutical combinations, for the treatment of stroke and traumatic brain injury, containing a neutrophil inhibiting factor and an selective NMDA-NR2B receptor antagonist |
-
2002
- 2002-08-11 UA UA20040604168A patent/UA79248C2/uk unknown
- 2002-11-07 MY MYPI20024166A patent/MY128237A/en unknown
- 2002-11-08 BR BR0212770-9A patent/BR0212770A/pt not_active IP Right Cessation
- 2002-11-08 IL IL16186602A patent/IL161866A0/xx unknown
- 2002-11-08 NZ NZ531739A patent/NZ531739A/en not_active IP Right Cessation
- 2002-11-08 ES ES02781214T patent/ES2244818T3/es not_active Expired - Lifetime
- 2002-11-08 EA EA200400656A patent/EA006980B1/ru not_active IP Right Cessation
- 2002-11-08 HU HU0402224A patent/HUP0402224A3/hu unknown
- 2002-11-08 US US10/491,799 patent/US7317115B2/en not_active Expired - Fee Related
- 2002-11-08 DE DE60204982T patent/DE60204982T2/de not_active Expired - Lifetime
- 2002-11-08 TW TW091132840A patent/TW200407117A/zh unknown
- 2002-11-08 JP JP2003542168A patent/JP2005508988A/ja active Pending
- 2002-11-08 CN CN02821918XA patent/CN1582282B/zh not_active Expired - Fee Related
- 2002-11-08 EP EP02781214A patent/EP1446397B1/en not_active Expired - Lifetime
- 2002-11-08 PL PL02368456A patent/PL368456A1/xx unknown
- 2002-11-08 KR KR1020047002379A patent/KR100962325B1/ko not_active IP Right Cessation
- 2002-11-08 CA CA2465043A patent/CA2465043C/en not_active Expired - Fee Related
- 2002-11-08 AU AU2002349327A patent/AU2002349327B2/en not_active Ceased
- 2002-11-08 AT AT02781214T patent/ATE299138T1/de not_active IP Right Cessation
- 2002-11-08 AR ARP020104298A patent/AR037285A1/es unknown
- 2002-11-08 WO PCT/EP2002/011136 patent/WO2003040122A1/en active IP Right Grant
- 2002-11-08 MX MXPA04004365A patent/MXPA04004365A/es active IP Right Grant
-
2004
- 2004-05-05 NO NO20041848A patent/NO328548B1/no not_active IP Right Cessation
- 2004-05-05 HR HR20040395A patent/HRP20040395A2/hr not_active Application Discontinuation
- 2004-05-06 ZA ZA200403454A patent/ZA200403454B/en unknown
- 2004-05-06 IL IL161866A patent/IL161866A/en not_active IP Right Cessation
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