CA2392979A1 - 4-carboxyamino-2-substituted-1,2,3,4-tetrahydroquinoline crystal - Google Patents
4-carboxyamino-2-substituted-1,2,3,4-tetrahydroquinoline crystal Download PDFInfo
- Publication number
- CA2392979A1 CA2392979A1 CA002392979A CA2392979A CA2392979A1 CA 2392979 A1 CA2392979 A1 CA 2392979A1 CA 002392979 A CA002392979 A CA 002392979A CA 2392979 A CA2392979 A CA 2392979A CA 2392979 A1 CA2392979 A1 CA 2392979A1
- Authority
- CA
- Canada
- Prior art keywords
- crystal
- trifluoromethyl
- formula
- rel
- dihydro
- 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.)
- Abandoned
Links
- 239000013078 crystal Substances 0.000 title claims abstract description 100
- -1 4-carboxyamino-2-substituted-1,2,3,4-tetrahydroquinoline Chemical class 0.000 title description 6
- 238000000034 method Methods 0.000 claims abstract description 49
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 78
- 241000124008 Mammalia Species 0.000 claims description 70
- 150000001875 compounds Chemical class 0.000 claims description 40
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- 239000003085 diluting agent Substances 0.000 claims description 28
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical class CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 claims description 28
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- 208000000563 Hyperlipoproteinemia Type II Diseases 0.000 claims description 18
- 201000001386 familial hypercholesterolemia Diseases 0.000 claims description 18
- HHFAWKCIHAUFRX-UHFFFAOYSA-N ethoxide Chemical compound CC[O-] HHFAWKCIHAUFRX-UHFFFAOYSA-N 0.000 claims description 17
- CMSGWTNRGKRWGS-NQIIRXRSSA-N torcetrapib Chemical compound COC(=O)N([C@H]1C[C@@H](CC)N(C2=CC=C(C=C21)C(F)(F)F)C(=O)OCC)CC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 CMSGWTNRGKRWGS-NQIIRXRSSA-N 0.000 claims description 17
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- 239000012964 benzotriazole Substances 0.000 description 1
- YGBQZFPEMRCQRY-UHFFFAOYSA-N benzyl n-ethenylcarbamate Chemical compound C=CNC(=O)OCC1=CC=CC=C1 YGBQZFPEMRCQRY-UHFFFAOYSA-N 0.000 description 1
- 239000003613 bile acid Substances 0.000 description 1
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- 230000015572 biosynthetic process Effects 0.000 description 1
- ZTQSAGDEMFDKMZ-UHFFFAOYSA-N butyric aldehyde Natural products CCCC=O ZTQSAGDEMFDKMZ-UHFFFAOYSA-N 0.000 description 1
- 239000001506 calcium phosphate Substances 0.000 description 1
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- 229940038472 dicalcium phosphate Drugs 0.000 description 1
- 229910000390 dicalcium phosphate Inorganic materials 0.000 description 1
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- 239000013583 drug formulation Substances 0.000 description 1
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- RIFGWPKJUGCATF-UHFFFAOYSA-N ethyl chloroformate Chemical compound CCOC(Cl)=O RIFGWPKJUGCATF-UHFFFAOYSA-N 0.000 description 1
- 125000004494 ethyl ester group Chemical group 0.000 description 1
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- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 230000014509 gene expression Effects 0.000 description 1
- BHEPBYXIRTUNPN-UHFFFAOYSA-N hydridophosphorus(.) (triplet) Chemical compound [PH] BHEPBYXIRTUNPN-UHFFFAOYSA-N 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
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- 239000008101 lactose Substances 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
- C07D215/38—Nitrogen atoms
- C07D215/42—Nitrogen atoms attached in position 4
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- 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
-
- 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
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Cephalosporin Compounds (AREA)
- Quinoline Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16805199P | 1999-11-30 | 1999-11-30 | |
| US60/168,051 | 1999-11-30 | ||
| PCT/IB2000/001650 WO2001040190A1 (en) | 1999-11-30 | 2000-11-14 | 4-carboxyamino-2-ethyl-1,2,3,4-tetrahydroquinoline crystal as cetp inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2392979A1 true CA2392979A1 (en) | 2001-06-07 |
Family
ID=22609901
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002392979A Abandoned CA2392979A1 (en) | 1999-11-30 | 2000-11-14 | 4-carboxyamino-2-substituted-1,2,3,4-tetrahydroquinoline crystal |
Country Status (28)
| Country | Link |
|---|---|
| EP (1) | EP1246804A1 (es) |
| JP (1) | JP2003515592A (es) |
| KR (1) | KR20020058057A (es) |
| CN (1) | CN1402711A (es) |
| AP (1) | AP2002002531A0 (es) |
| AU (1) | AU1048801A (es) |
| BG (1) | BG106854A (es) |
| BR (1) | BR0015836A (es) |
| CA (1) | CA2392979A1 (es) |
| CO (1) | CO5271716A1 (es) |
| EA (1) | EA200200510A1 (es) |
| EC (1) | ECSP003792A (es) |
| EE (1) | EE200200277A (es) |
| GT (1) | GT200000199A (es) |
| HU (1) | HUP0203521A2 (es) |
| IL (1) | IL149097A0 (es) |
| IS (1) | IS6338A (es) |
| MA (1) | MA26845A1 (es) |
| MX (1) | MXPA02005354A (es) |
| NO (1) | NO20022558L (es) |
| OA (1) | OA12099A (es) |
| PA (1) | PA8506301A1 (es) |
| PE (1) | PE20010904A1 (es) |
| PL (1) | PL355892A1 (es) |
| TN (1) | TNSN00231A1 (es) |
| TR (1) | TR200201446T2 (es) |
| UY (1) | UY26454A1 (es) |
| WO (1) | WO2001040190A1 (es) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7115279B2 (en) | 2000-08-03 | 2006-10-03 | Curatolo William J | Pharmaceutical compositions of cholesteryl ester transfer protein inhibitors |
| OA12619A (en) | 2001-06-21 | 2006-06-12 | Pfizer Prod Inc | Self-emulsifying formulations of cholesteryl estertransfer protein inhibitors. |
| GT200200170A (es) | 2001-09-28 | 2003-05-23 | Preparacion de inhibidor de cetp anhidro | |
| DE60320940D1 (de) | 2002-02-01 | 2008-06-26 | Pfizer Prod Inc | Pharmazeutische zusammensetzungen amorpher dispersionen von wirkstoffen und lipophiler mikrophasenbildender materialien |
| EP1920766B1 (en) * | 2002-02-01 | 2017-08-23 | Bend Research, Inc | Pharmaceutical compositions of amorphous dispersions of drugs and lipophilic microphase-forming materials |
| WO2003063822A2 (en) * | 2002-02-01 | 2003-08-07 | Pfizer Products Inc. | Method for making homogeneous spray-dried solid amorphous drug dispersions utilizing modified spray-drying apparatus |
| BR0306208A (pt) | 2002-08-30 | 2004-10-13 | Japan Tobacco Inc | Compostos de dibenzilamina e seu uso farmacêutico |
| JP2006508077A (ja) | 2002-10-04 | 2006-03-09 | ミレニアム・ファーマシューティカルズ・インコーポレイテッド | 炎症疾患を治療するためのｐｇｄ２レセプタアンタゴニスト |
| US7504508B2 (en) | 2002-10-04 | 2009-03-17 | Millennium Pharmaceuticals, Inc. | PGD2 receptor antagonists for the treatment of inflammatory diseases |
| US20040132771A1 (en) * | 2002-12-20 | 2004-07-08 | Pfizer Inc | Compositions of choleseteryl ester transfer protein inhibitors and HMG-CoA reductase inhibitors |
| CA2508840A1 (en) | 2002-12-20 | 2004-07-08 | Pfizer Products Inc. | Dosage forms comprising a cetp inhibitor and an hmg-coa reductase inhibitor |
| MXPA05010456A (es) * | 2003-03-28 | 2006-03-21 | Pfizer Prod Inc | Compuestos de quinolina y quinoxalina. |
| BRPI0413277A (pt) | 2003-08-04 | 2006-10-10 | Pfizer Prod Inc | composições farmacêuticas de adsorvatos de medicamentos amorfos e materiais que formam microfases lipofìlicas |
| MXPA06003927A (es) | 2003-10-08 | 2008-02-07 | Lilly Co Eli | Compuestos y metodos para tratar dislipidemia. |
| JP4922924B2 (ja) * | 2004-04-13 | 2012-04-25 | メルク・シャープ・エンド・ドーム・コーポレイション | Ｃｅｔｐ阻害薬 |
| JP2008504266A (ja) * | 2004-06-24 | 2008-02-14 | イーライ リリー アンド カンパニー | 異脂肪血症を治療するための化合物及び方法 |
| US20070149567A1 (en) * | 2004-09-23 | 2007-06-28 | Pfizer Inc | Quinoline compounds |
| WO2006033001A1 (en) * | 2004-09-23 | 2006-03-30 | Pfizer Products Inc. | Quinoline compounds |
| CA2598133A1 (en) | 2005-02-24 | 2006-08-31 | Millennium Pharmaceuticals, Inc. | Pgd2 receptor antagonists for the treatment of inflammatory diseases |
| WO2006098394A1 (ja) * | 2005-03-14 | 2006-09-21 | Japan Tobacco Inc. | 脂質吸収抑制方法および脂質吸収抑制剤 |
| US7737155B2 (en) | 2005-05-17 | 2010-06-15 | Schering Corporation | Nitrogen-containing heterocyclic compounds and methods of use thereof |
| EP2134169A2 (en) | 2007-03-09 | 2009-12-23 | Indigene Pharmaceuticals Inc. | Combination of metformin r-(+) lipoate and antihyperlipidemic agents for the treatment of diabetic hyperglycemia and diabetic complications |
| US20110245209A1 (en) | 2008-12-16 | 2011-10-06 | Schering Corporation | Pyridopyrimidine derivatives and methods of use thereof |
| US20110243940A1 (en) | 2008-12-16 | 2011-10-06 | Schering Corporation | Bicyclic pyranone derivatives and methods of use thereof |
| AR077208A1 (es) | 2009-06-30 | 2011-08-10 | Lilly Co Eli | Derivados del acido trans-4-[[(5s)-5-[[[3,5-bis(trifluorometil) fenil] metil] (2-metil-2h-tetrazol-5-il) amino) -2,3,4,5-tetrahidro-7,9-dimetil-1h-1-benzazepin-1-il) metil)-ciclohexancarboxilico y sus formas cristalinas, composiciones farmaceuticas que los comprenden, su uso para preparar un medicam |
| CN106559998B (zh) | 2014-07-30 | 2022-01-25 | 豪夫迈·罗氏有限公司 | 预测对hdl升高剂或hdl模拟剂疗法的应答性的遗传标记 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5231102A (en) * | 1989-03-08 | 1993-07-27 | Merck Sharp & Dohme, Ltd. | Tetrahydroquinoline derivatives useful for neurodegenerative disorders |
| AU5731098A (en) * | 1997-02-03 | 1998-08-25 | American Home Products Corporation | 2-substituted-1-acyl-1,2-dihydroquinoline derivatives to increase hdl-cholesterol level |
| US6197786B1 (en) * | 1998-09-17 | 2001-03-06 | Pfizer Inc | 4-Carboxyamino-2-substituted-1,2,3,4-tetrahydroquinolines |
-
2000
- 2000-11-09 CO CO00085285A patent/CO5271716A1/es unknown
- 2000-11-13 PA PA20008506301A patent/PA8506301A1/es unknown
- 2000-11-14 AU AU10488/01A patent/AU1048801A/en not_active Abandoned
- 2000-11-14 PL PL00355892A patent/PL355892A1/xx not_active Application Discontinuation
- 2000-11-14 TR TR2002/01446T patent/TR200201446T2/xx unknown
- 2000-11-14 KR KR1020027006914A patent/KR20020058057A/ko not_active Application Discontinuation
- 2000-11-14 EA EA200200510A patent/EA200200510A1/ru unknown
- 2000-11-14 IL IL14909700A patent/IL149097A0/xx unknown
- 2000-11-14 BR BR0015836-4A patent/BR0015836A/pt not_active IP Right Cessation
- 2000-11-14 HU HU0203521A patent/HUP0203521A2/hu unknown
- 2000-11-14 OA OA1200200158A patent/OA12099A/en unknown
- 2000-11-14 WO PCT/IB2000/001650 patent/WO2001040190A1/en not_active Application Discontinuation
- 2000-11-14 EP EP00971662A patent/EP1246804A1/en not_active Withdrawn
- 2000-11-14 AP APAP/P/2002/002531A patent/AP2002002531A0/en unknown
- 2000-11-14 CA CA002392979A patent/CA2392979A1/en not_active Abandoned
- 2000-11-14 CN CN00816463A patent/CN1402711A/zh active Pending
- 2000-11-14 EE EEP200200277A patent/EE200200277A/xx unknown
- 2000-11-14 JP JP2001541875A patent/JP2003515592A/ja active Pending
- 2000-11-14 MX MXPA02005354A patent/MXPA02005354A/es unknown
- 2000-11-28 PE PE2000001267A patent/PE20010904A1/es not_active Application Discontinuation
- 2000-11-28 UY UY26454A patent/UY26454A1/es not_active Application Discontinuation
- 2000-11-29 GT GT200000199A patent/GT200000199A/es unknown
- 2000-11-29 EC EC2000003792A patent/ECSP003792A/es unknown
- 2000-11-29 TN TNTNSN00231A patent/TNSN00231A1/fr unknown
-
2002
- 2002-04-12 IS IS6338A patent/IS6338A/is unknown
- 2002-05-27 MA MA26653A patent/MA26845A1/fr unknown
- 2002-05-29 NO NO20022558A patent/NO20022558L/no not_active Application Discontinuation
- 2002-06-20 BG BG106854A patent/BG106854A/bg unknown
Also Published As
| Publication number | Publication date |
|---|---|
| BR0015836A (pt) | 2002-08-06 |
| OA12099A (en) | 2006-05-04 |
| PE20010904A1 (es) | 2001-09-10 |
| TR200201446T2 (tr) | 2002-11-21 |
| IS6338A (is) | 2002-04-12 |
| BG106854A (bg) | 2002-12-29 |
| ECSP003792A (es) | 2002-04-23 |
| CN1402711A (zh) | 2003-03-12 |
| KR20020058057A (ko) | 2002-07-12 |
| IL149097A0 (en) | 2002-11-10 |
| GT200000199A (es) | 2002-05-23 |
| EP1246804A1 (en) | 2002-10-09 |
| NO20022558D0 (no) | 2002-05-29 |
| MXPA02005354A (es) | 2002-12-11 |
| UY26454A1 (es) | 2001-07-31 |
| PA8506301A1 (es) | 2002-08-26 |
| CO5271716A1 (es) | 2003-04-30 |
| PL355892A1 (en) | 2004-05-31 |
| HUP0203521A2 (hu) | 2003-02-28 |
| MA26845A1 (fr) | 2004-12-20 |
| NO20022558L (no) | 2002-05-29 |
| WO2001040190A1 (en) | 2001-06-07 |
| TNSN00231A1 (fr) | 2002-05-30 |
| JP2003515592A (ja) | 2003-05-07 |
| EE200200277A (et) | 2003-10-15 |
| AU1048801A (en) | 2001-06-12 |
| AP2002002531A0 (en) | 2002-06-30 |
| EA200200510A1 (ru) | 2002-10-31 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| FZDE | Discontinued |