HUP0302866A2 - 3-(3-Amidinofenil)-5-[({[1-(1-iminoetil)-4-piperidil]metil}amino)metil]benzoesav-dihidroklorid és eljárás előállítására - Google Patents
3-(3-Amidinofenil)-5-[({[1-(1-iminoetil)-4-piperidil]metil}amino)metil]benzoesav-dihidroklorid és eljárás előállításáraInfo
- Publication number
- HUP0302866A2 HUP0302866A2 HU0302866A HUP0302866A HUP0302866A2 HU P0302866 A2 HUP0302866 A2 HU P0302866A2 HU 0302866 A HU0302866 A HU 0302866A HU P0302866 A HUP0302866 A HU P0302866A HU P0302866 A2 HUP0302866 A2 HU P0302866A2
- Authority
- HU
- Hungary
- Prior art keywords
- methyl
- amidinophenyl
- piperidyl
- amino
- iminoethyl
- Prior art date
Links
- KLQNJBAFEFFWQZ-UHFFFAOYSA-N benzoic acid;dihydrochloride Chemical compound Cl.Cl.OC(=O)C1=CC=CC=C1 KLQNJBAFEFFWQZ-UHFFFAOYSA-N 0.000 title 1
- 238000004519 manufacturing process Methods 0.000 title 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 title 1
- 239000013078 crystal Substances 0.000 abstract 2
- WGMHMVLZFAJNOT-UHFFFAOYSA-N 1-ethoxyethylideneazanium;chloride Chemical compound [Cl-].CCOC(C)=[NH2+] WGMHMVLZFAJNOT-UHFFFAOYSA-N 0.000 abstract 1
- ABMFWXJGCAUFCN-UHFFFAOYSA-N 3-(3-carbamimidoylphenyl)-5-[[(1-ethanimidoylpiperidin-4-yl)methylamino]methyl]benzoic acid;dihydrochloride Chemical compound Cl.Cl.C1CN(C(=N)C)CCC1CNCC1=CC(C(O)=O)=CC(C=2C=C(C=CC=2)C(N)=N)=C1 ABMFWXJGCAUFCN-UHFFFAOYSA-N 0.000 abstract 1
- DAMYQCUMFDXPJR-UHFFFAOYSA-N 3-(3-carbamimidoylphenyl)-5-[[(1-ethanimidoylpiperidin-4-yl)methylamino]methyl]benzoic acid;hydrate;dihydrochloride Chemical compound O.Cl.Cl.C1CN(C(=N)C)CCC1CNCC1=CC(C(O)=O)=CC(C=2C=C(C=CC=2)C(N)=N)=C1 DAMYQCUMFDXPJR-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000003750 conditioning effect Effects 0.000 abstract 1
- WVRIPJVXRAKYPL-UHFFFAOYSA-N methyl 3-(3-carbamimidoylphenyl)-5-[(piperidin-4-ylmethylamino)methyl]benzoate Chemical compound C=1C(C=2C=C(C=CC=2)C(N)=N)=CC(C(=O)OC)=CC=1CNCC1CCNCC1 WVRIPJVXRAKYPL-UHFFFAOYSA-N 0.000 abstract 1
- HSQHZNCFJYNCEH-UHFFFAOYSA-N methyl 3-(3-carbamimidoylphenyl)-5-[[(1-ethanimidoylpiperidin-4-yl)methylamino]methyl]benzoate Chemical compound C=1C(C=2C=C(C=CC=2)C(N)=N)=CC(C(=O)OC)=CC=1CNCC1CCN(C(C)=N)CC1 HSQHZNCFJYNCEH-UHFFFAOYSA-N 0.000 abstract 1
- 238000006386 neutralization reaction Methods 0.000 abstract 1
- 239000000843 powder Substances 0.000 abstract 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
- 238000000746 purification Methods 0.000 abstract 1
- 238000001953 recrystallisation Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
- C07D211/08—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/26—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hydrogenated Pyridines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
A találmány (I) képletű 3-(3-amidinofenil)-5-[({[1-(1-iminoetil)-4-piperidil]metil}amino)metil]-benzoesav-dihidroklorid-hidrátkristályára vonatkozik, amelynek por röntgendiffraktometriásvizsgálata során 2 q (°) diffrakciós szögnél a fő csúcsok akövetkezők: 12,2, 13,5, 16,5, 18,5, 19,2, 20,5, 22,0, 22,8, 23,6,24,7, 25,1, 25,5, 26,1, 29,8, 33,1 és 33,7. A találmány továbbá a 3-(3-amidinofenil)-5-[({[1-(1-iminoetil)-4-piperidil]metil}amino)metil]benzoesav-dihidroklorid kristályáravonatkozik, amelynek por röntgendiffrakciós vizsgálatánál 2q (°)diffrakciós szögnél a fő csúcsai a következők: 16,2, 17,1, 18,3, 19,0,20,5, 21,1, 22,7, 23,2, 24,7, 25,6, 28,4, 29,5, 33,2, 34,3 és 35,8. Azelőbbi kristályt adó vegyület úgy állítható elő, hogy a (II) képletűmetil-3-(3-amidinofenil)-5-({[(4-piperidil)metil]amino}metil)benzoátotvagy ennek valamelyik sóját etilacetoimidát-hidrokloriddalreagáltatják, majd az így kapott (III) képletű metil-3-(3-amidinofenil)-5-[({[1-(1-iminoetil)-4-piperidil]metil}amino)metil]benzoátot - a képletben xértéke 0, 1, 2vagy 3 - egy savval hidrolizálják, ezután a kapott hidrolizátumotsemlegesítésnek, átkristályosítással tisztításnak és nedvesítéseskondicionálásnak vetik alá. Ó
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2001021475 | 2001-01-30 | ||
| PCT/JP2002/000606 WO2002060873A1 (en) | 2001-01-30 | 2002-01-28 | 3-(3-amidinophenyl)-5-[({[1-(1-(-iminoethyl)-4-piperidyl}amino)methyl]benzoic acid dihydrochloride and process for preparing the same |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0302866A2 true HUP0302866A2 (hu) | 2003-12-29 |
| HUP0302866A3 HUP0302866A3 (en) | 2007-05-02 |
Family
ID=18887035
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0302866A HUP0302866A3 (en) | 2001-01-30 | 2002-01-28 | 3-(3-amidinophenyl)-5-[({[1-(1-iminoethyl)-4-piperidyl}amino)methyl]benzoic acid dihydrochloride and process for preparing the same |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20040053967A1 (hu) |
| EP (1) | EP1363882A4 (hu) |
| JP (1) | JP2004518683A (hu) |
| KR (1) | KR20040016837A (hu) |
| CN (1) | CN1489578A (hu) |
| AR (1) | AR035425A1 (hu) |
| CA (1) | CA2436265A1 (hu) |
| HU (1) | HUP0302866A3 (hu) |
| NZ (1) | NZ527138A (hu) |
| PE (1) | PE20020918A1 (hu) |
| WO (1) | WO2002060873A1 (hu) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003235236A1 (en) * | 2002-05-13 | 2003-11-11 | Daiichi Pharmaceutical Co., Ltd. | Lyophilization product |
| JPWO2010041569A1 (ja) | 2008-10-09 | 2012-03-08 | 旭化成ファーマ株式会社 | インダゾール化合物 |
| CN102171191A (zh) * | 2008-10-09 | 2011-08-31 | 旭化成制药株式会社 | 吲唑衍生物 |
| US20100222404A1 (en) * | 2008-11-04 | 2010-09-02 | Asahi Kasei Pharma Corporation | Indazole derivative dihydrochloride |
| EP3307725A1 (en) | 2015-06-11 | 2018-04-18 | Basilea Pharmaceutica International AG | Efflux-pump inhibitors and therapeutic uses thereof |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4102024A1 (de) * | 1991-01-24 | 1992-07-30 | Thomae Gmbh Dr K | Biphenylderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung |
| US5463116A (en) * | 1991-07-30 | 1995-10-31 | Ajinomoto Co., Inc. | Crystals of N- (trans-4-isopropylcyclohexlycarbonyl)-D-phenylalanine and methods for preparing them |
| EP0526171B1 (en) * | 1991-07-30 | 1997-03-05 | Ajinomoto Co., Inc. | Crystals of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine and methods for preparing them |
| JPH101467A (ja) * | 1996-06-13 | 1998-01-06 | Banyu Pharmaceut Co Ltd | ビフェニルアミジン誘導体 |
| EE04564B1 (et) * | 1997-11-20 | 2005-12-15 | Teijin Limited | Bifenlamidiini derivaadid, eelravim, vere koagulatsiooniinhibiitor ning proflaktiline ja terapeutiline toimeaine tromboosi v?i emboolia vastu |
| CA2360686A1 (en) * | 1999-01-28 | 2000-08-03 | Teijin Limited | Release-regulating preparations |
-
2002
- 2002-01-25 AR ARP020100278A patent/AR035425A1/es unknown
- 2002-01-28 CA CA002436265A patent/CA2436265A1/en not_active Abandoned
- 2002-01-28 NZ NZ527138A patent/NZ527138A/en unknown
- 2002-01-28 CN CNA028043162A patent/CN1489578A/zh active Pending
- 2002-01-28 KR KR10-2003-7010019A patent/KR20040016837A/ko not_active Application Discontinuation
- 2002-01-28 EP EP02716418A patent/EP1363882A4/en not_active Withdrawn
- 2002-01-28 WO PCT/JP2002/000606 patent/WO2002060873A1/en not_active Application Discontinuation
- 2002-01-28 US US10/470,383 patent/US20040053967A1/en not_active Abandoned
- 2002-01-28 JP JP2002561024A patent/JP2004518683A/ja not_active Withdrawn
- 2002-01-28 HU HU0302866A patent/HUP0302866A3/hu unknown
- 2002-01-29 PE PE2002000069A patent/PE20020918A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| HUP0302866A3 (en) | 2007-05-02 |
| EP1363882A4 (en) | 2005-11-30 |
| EP1363882A1 (en) | 2003-11-26 |
| CN1489578A (zh) | 2004-04-14 |
| CA2436265A1 (en) | 2002-08-08 |
| JP2004518683A (ja) | 2004-06-24 |
| PE20020918A1 (es) | 2002-10-21 |
| AR035425A1 (es) | 2004-05-26 |
| KR20040016837A (ko) | 2004-02-25 |
| NZ527138A (en) | 2005-01-28 |
| US20040053967A1 (en) | 2004-03-18 |
| WO2002060873A1 (en) | 2002-08-08 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD9A | Lapse of provisional protection due to non-payment of fees |