AR036048A1 - Compuesto de piperazina; composiciones farmaceuticas formuladas con dicho compuesto y uso de las sales difumarato de dicho compuesto, en la preparacion de composiciones farmaceuticas para el tratamiento de trastornos tromboticos - Google Patents
Compuesto de piperazina; composiciones farmaceuticas formuladas con dicho compuesto y uso de las sales difumarato de dicho compuesto, en la preparacion de composiciones farmaceuticas para el tratamiento de trastornos tromboticosInfo
- Publication number
- AR036048A1 AR036048A1 ARP020102199A ARP020102199A AR036048A1 AR 036048 A1 AR036048 A1 AR 036048A1 AR P020102199 A ARP020102199 A AR P020102199A AR P020102199 A ARP020102199 A AR P020102199A AR 036048 A1 AR036048 A1 AR 036048A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- pharmaceutical compositions
- crystallization
- treatment
- difumarate
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 238000011282 treatment Methods 0.000 title abstract 3
- -1 PIPERAZINE COMPOUND Chemical class 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title 2
- 239000002131 composite material Substances 0.000 title 1
- GLUUGHFHXGJENI-UHFFFAOYSA-N diethylenediamine Natural products C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 title 1
- 230000001732 thrombotic effect Effects 0.000 title 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract 4
- 238000002425 crystallisation Methods 0.000 abstract 4
- 230000008025 crystallization Effects 0.000 abstract 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 abstract 3
- 206010003178 Arterial thrombosis Diseases 0.000 abstract 1
- 206010008088 Cerebral artery embolism Diseases 0.000 abstract 1
- 108010074860 Factor Xa Proteins 0.000 abstract 1
- 208000010378 Pulmonary Embolism Diseases 0.000 abstract 1
- 108010022999 Serine Proteases Proteins 0.000 abstract 1
- 102000012479 Serine Proteases Human genes 0.000 abstract 1
- 208000007536 Thrombosis Diseases 0.000 abstract 1
- 206010047249 Venous thrombosis Diseases 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 230000003750 conditioning effect Effects 0.000 abstract 1
- 239000013078 crystal Substances 0.000 abstract 1
- 238000010586 diagram Methods 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 201000010849 intracranial embolism Diseases 0.000 abstract 1
- 239000000843 powder Substances 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 230000002685 pulmonary effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
- 208000019553 vascular disease Diseases 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se describe y reivindica una sal cristalina estable, farmacéuticamente aceptable, del difumarato de 1-(indol-6-carbonil-D-fenilglicinil)-4-(1-metilpiperidin-4-il)pirazina, compuesto cuya cristalización conduce a la obtención de dos formas cristalinas diferentes, según el medio solvente utilizado en la etapa de cristalización: metanol o etanol (95%). Este condicionamiento conduce a la formación de cristales circulares (finos) - p.f. 213°C (forma 1) con picos en el diagrama de difracción RX en polvo a 6,280; 7,830 y 19,513 A. La otra forma cristalina se obtiene por cristalización en etanol 50%, forma cuyo patrón de difracción a 8,833; 20,810 y 23,824 A (forma 2), morfológicamente estable en condiciones de elevada humedad relativa (> 70%). Esta forma también puede obtenerse por cristalización de la forma 1 en agua. Dicho compuesto posee propiedades inhibitorias de la serina proteasa, factor Xa, útil en el tratamiento de trastornos vasculares. Conforme a las experiencias realizadas, dicho compuesto es potencialmente útil en el tratamiento o profilaxis de estados de trombosis; por ejemplo, trombosis venosa o arterial, embolias pulmonares y cerebral.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/GB2001/002553 WO2001096323A1 (en) | 2000-06-13 | 2001-06-12 | Serine protease inhibitors |
| US33929501P | 2001-12-12 | 2001-12-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR036048A1 true AR036048A1 (es) | 2004-08-04 |
Family
ID=41210812
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020102199A AR036048A1 (es) | 2001-06-12 | 2002-06-11 | Compuesto de piperazina; composiciones farmaceuticas formuladas con dicho compuesto y uso de las sales difumarato de dicho compuesto, en la preparacion de composiciones farmaceuticas para el tratamiento de trastornos tromboticos |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20040162295A1 (es) |
| EP (1) | EP1397348B1 (es) |
| JP (1) | JP2004534062A (es) |
| AR (1) | AR036048A1 (es) |
| AT (1) | ATE305452T1 (es) |
| AU (1) | AU2002348501A1 (es) |
| DE (1) | DE60206376T2 (es) |
| ES (1) | ES2248618T3 (es) |
| MY (1) | MY137876A (es) |
| PE (1) | PE20030198A1 (es) |
| SV (1) | SV2003001085A (es) |
| TW (1) | TWI257389B (es) |
| WO (1) | WO2002100847A2 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1409479B1 (en) * | 2001-07-26 | 2008-01-23 | Eli Lilly And Company | 1-glycinyl-4-(1-methylpiperidin-4-yl)piperazines and -piperidines as factor xa antagonists |
| EA007300B1 (ru) | 2002-04-01 | 2006-08-25 | Эли Лилли Энд Компани | Некоторые производные 1-(d-циклопропилглицинил)-4-(пиперидин-4-ил) пиперазина в качестве ингибиторов серинпротеазы фактора ха |
| CA2570634A1 (en) * | 2004-06-30 | 2006-02-02 | Eli Lilly And Company | 1 (indole-6-carbonyl-d-phenylglycinyl) -4- (1-methylpiperidin-4-yl) piperazine d-tartrate |
| KR100849242B1 (ko) * | 2004-06-30 | 2008-07-29 | 일라이 릴리 앤드 캄파니 | 1(인돌-6-카르보닐-ｄ-페닐글리시닐)-4-(1-메틸피페리딘-4-일) 피페라진 ｄ-타르트레이트 |
| DE102007028407A1 (de) | 2007-06-20 | 2008-12-24 | Bayer Healthcare Ag | Substituierte Oxazolidinone und ihre Verwendung |
| DE102007028319A1 (de) | 2007-06-20 | 2008-12-24 | Bayer Healthcare Ag | Substituierte Oxazolidinone und ihre Verwendung |
| DE102007028406A1 (de) | 2007-06-20 | 2008-12-24 | Bayer Healthcare Ag | Substituierte Oxazolidinone und ihre Verwendung |
| EP2875020B1 (en) * | 2012-07-19 | 2017-09-06 | Boehringer Ingelheim International GmbH | Process for the preparation of a fumaric acid salt of 9-[4-(3-chloro-2-fluoro-phenylamino)-7-methoxy- chinazolin-6-yloxy]-1,4-diaza-spiro[5.5]undecan-5-one |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6855715B1 (en) * | 1999-06-14 | 2005-02-15 | Eli Lilly And Company | Serine protease inhibitors |
| GB0030304D0 (en) * | 2000-12-13 | 2001-01-24 | Lilly Co Eli | Compounds |
-
2002
- 2002-06-05 TW TW091112134A patent/TWI257389B/zh not_active IP Right Cessation
- 2002-06-06 JP JP2003503615A patent/JP2004534062A/ja active Pending
- 2002-06-06 WO PCT/US2002/016569 patent/WO2002100847A2/en not_active Ceased
- 2002-06-06 AT AT02778933T patent/ATE305452T1/de not_active IP Right Cessation
- 2002-06-06 EP EP02778933A patent/EP1397348B1/en not_active Expired - Lifetime
- 2002-06-06 AU AU2002348501A patent/AU2002348501A1/en not_active Abandoned
- 2002-06-06 DE DE60206376T patent/DE60206376T2/de not_active Expired - Fee Related
- 2002-06-06 US US10/477,192 patent/US20040162295A1/en not_active Abandoned
- 2002-06-06 ES ES02778933T patent/ES2248618T3/es not_active Expired - Lifetime
- 2002-06-10 MY MYPI20022155A patent/MY137876A/en unknown
- 2002-06-10 PE PE2002000496A patent/PE20030198A1/es not_active Application Discontinuation
- 2002-06-11 AR ARP020102199A patent/AR036048A1/es unknown
- 2002-06-11 SV SV2002001085A patent/SV2003001085A/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| AU2002348501A1 (en) | 2002-12-23 |
| WO2002100847A3 (en) | 2003-08-21 |
| DE60206376D1 (de) | 2006-02-09 |
| SV2003001085A (es) | 2003-03-18 |
| US20040162295A1 (en) | 2004-08-19 |
| MY137876A (en) | 2009-03-31 |
| TWI257389B (en) | 2006-07-01 |
| PE20030198A1 (es) | 2003-03-12 |
| DE60206376T2 (de) | 2006-06-22 |
| ATE305452T1 (de) | 2005-10-15 |
| ES2248618T3 (es) | 2006-03-16 |
| EP1397348A2 (en) | 2004-03-17 |
| JP2004534062A (ja) | 2004-11-11 |
| EP1397348B1 (en) | 2005-09-28 |
| WO2002100847A2 (en) | 2002-12-19 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |