CA2589886A1 - Crystalline forms of a factor xa inhibitor - Google Patents
Crystalline forms of a factor xa inhibitor Download PDFInfo
- Publication number
- CA2589886A1 CA2589886A1 CA002589886A CA2589886A CA2589886A1 CA 2589886 A1 CA2589886 A1 CA 2589886A1 CA 002589886 A CA002589886 A CA 002589886A CA 2589886 A CA2589886 A CA 2589886A CA 2589886 A1 CA2589886 A1 CA 2589886A1
- Authority
- CA
- Canada
- Prior art keywords
- ang
- crystalline
- pyridin
- phenyl
- compound
- 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
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- 229920006324 polyoxymethylene Polymers 0.000 description 1
- 229920006316 polyvinylpyrrolidine Polymers 0.000 description 1
- 229910000160 potassium phosphate Inorganic materials 0.000 description 1
- 235000011009 potassium phosphates Nutrition 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 230000035935 pregnancy Effects 0.000 description 1
- 230000000019 pro-fibrinolytic effect Effects 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- FVSKHRXBFJPNKK-UHFFFAOYSA-N propionitrile Chemical compound CCC#N FVSKHRXBFJPNKK-UHFFFAOYSA-N 0.000 description 1
- 230000017854 proteolysis Effects 0.000 description 1
- 108010014806 prothrombinase complex Proteins 0.000 description 1
- 238000010926 purge Methods 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 239000012429 reaction media Substances 0.000 description 1
- 239000002464 receptor antagonist Substances 0.000 description 1
- 229940044551 receptor antagonist Drugs 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 208000037803 restenosis Diseases 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 239000012047 saturated solution Substances 0.000 description 1
- 238000007873 sieving Methods 0.000 description 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
- 235000010234 sodium benzoate Nutrition 0.000 description 1
- 239000004299 sodium benzoate Substances 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
- 235000010265 sodium sulphite Nutrition 0.000 description 1
- 239000008247 solid mixture Substances 0.000 description 1
- 238000000371 solid-state nuclear magnetic resonance spectroscopy Methods 0.000 description 1
- 239000003549 soybean oil Substances 0.000 description 1
- 235000012424 soybean oil Nutrition 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 238000012306 spectroscopic technique Methods 0.000 description 1
- 238000004611 spectroscopical analysis Methods 0.000 description 1
- 238000009987 spinning Methods 0.000 description 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 229960005202 streptokinase Drugs 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 238000000859 sublimation Methods 0.000 description 1
- 230000008022 sublimation Effects 0.000 description 1
- HXJUTPCZVOIRIF-UHFFFAOYSA-N sulfolane Chemical compound O=S1(=O)CCCC1 HXJUTPCZVOIRIF-UHFFFAOYSA-N 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 239000011885 synergistic combination Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- WMOVHXAZOJBABW-UHFFFAOYSA-N tert-butyl acetate Chemical compound CC(=O)OC(C)(C)C WMOVHXAZOJBABW-UHFFFAOYSA-N 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- UEUXEKPTXMALOB-UHFFFAOYSA-J tetrasodium;2-[2-[bis(carboxylatomethyl)amino]ethyl-(carboxylatomethyl)amino]acetate Chemical compound [Na+].[Na+].[Na+].[Na+].[O-]C(=O)CN(CC([O-])=O)CCN(CC([O-])=O)CC([O-])=O UEUXEKPTXMALOB-UHFFFAOYSA-J 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 239000003868 thrombin inhibitor Substances 0.000 description 1
- 230000002537 thrombolytic effect Effects 0.000 description 1
- 229960000187 tissue plasminogen activator Drugs 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 229960005356 urokinase Drugs 0.000 description 1
- 238000001291 vacuum drying Methods 0.000 description 1
- 238000003828 vacuum filtration Methods 0.000 description 1
- MWOOGOJBHIARFG-UHFFFAOYSA-N vanillin Chemical compound COC1=CC(C=O)=CC=C1O MWOOGOJBHIARFG-UHFFFAOYSA-N 0.000 description 1
- FGQOOHJZONJGDT-UHFFFAOYSA-N vanillin Natural products COC1=CC(O)=CC(C=O)=C1 FGQOOHJZONJGDT-UHFFFAOYSA-N 0.000 description 1
- 235000012141 vanillin Nutrition 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
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- 238000005406 washing Methods 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
-
- 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
-
- 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
- A61P9/06—Antiarrhythmics
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Vascular Medicine (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63638704P | 2004-12-15 | 2004-12-15 | |
| US60/636,387 | 2004-12-15 | ||
| US73798505P | 2005-11-18 | 2005-11-18 | |
| US60/737,985 | 2005-11-18 | ||
| PCT/US2005/045158 WO2006065853A2 (en) | 2004-12-15 | 2005-12-14 | Crystalline forms of a factor xa inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2589886A1 true CA2589886A1 (en) | 2006-06-22 |
Family
ID=36384503
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002589886A Abandoned CA2589886A1 (en) | 2004-12-15 | 2005-12-14 | Crystalline forms of a factor xa inhibitor |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US7371864B2 (enExample) |
| EP (1) | EP1828187A2 (enExample) |
| JP (1) | JP2008524228A (enExample) |
| KR (1) | KR20070087606A (enExample) |
| AR (1) | AR053990A1 (enExample) |
| AU (1) | AU2005317158A1 (enExample) |
| BR (1) | BRPI0519331A2 (enExample) |
| CA (1) | CA2589886A1 (enExample) |
| IL (1) | IL183825A0 (enExample) |
| MX (1) | MX2007006919A (enExample) |
| NO (1) | NO20072666L (enExample) |
| PE (1) | PE20060739A1 (enExample) |
| RU (1) | RU2007126770A (enExample) |
| TW (1) | TW200634011A (enExample) |
| WO (1) | WO2006065853A2 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2636757B1 (en) | 2008-05-27 | 2016-11-23 | Dako Denmark A/S | Compositions and methods for detection of chromosomal aberrations with novel hybridization buffers |
| US9303287B2 (en) | 2009-02-26 | 2016-04-05 | Dako Denmark A/S | Compositions and methods for RNA hybridization applications |
| WO2013046033A1 (en) | 2011-09-30 | 2013-04-04 | Dako Denmark A/S | Hybridization compositions and methods using formamide |
| EP3252173A1 (en) | 2011-10-21 | 2017-12-06 | Dako Denmark A/S | Hybridization compositions and methods |
| UY38438A (es) | 2018-11-02 | 2020-05-29 | Biocryst Pharm Inc | Sales cristalinas de un inhibidor de calicreína plasmática |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI331526B (en) * | 2001-09-21 | 2010-10-11 | Bristol Myers Squibb Pharma Co | Lactam-containing compounds and derivatives thereof as factor xa inhibitors |
| GEP20074098B (en) * | 2001-09-21 | 2007-05-10 | Bristol Myers Squibb Co | Lactam-containing compounds and derivatives thereof as factor xa inhibitors |
| US20060069085A1 (en) * | 2004-09-28 | 2006-03-30 | Rulin Zhao | Preparation of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones |
| US20060069260A1 (en) * | 2004-09-28 | 2006-03-30 | Huiping Zhang | Preparation of N-aryl pyridones |
| US7388096B2 (en) | 2004-09-28 | 2008-06-17 | Bristol-Myers Squibb Company | Crystalline forms of a factor Xa inhibitor |
| US7304157B2 (en) * | 2004-09-28 | 2007-12-04 | Bristol-Myers Squibb Company | Efficient synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones |
-
2005
- 2005-12-14 RU RU2007126770/04A patent/RU2007126770A/ru not_active Application Discontinuation
- 2005-12-14 WO PCT/US2005/045158 patent/WO2006065853A2/en not_active Ceased
- 2005-12-14 BR BRPI0519331-1A patent/BRPI0519331A2/pt not_active IP Right Cessation
- 2005-12-14 MX MX2007006919A patent/MX2007006919A/es active IP Right Grant
- 2005-12-14 EP EP05853961A patent/EP1828187A2/en not_active Withdrawn
- 2005-12-14 TW TW094144289A patent/TW200634011A/zh unknown
- 2005-12-14 CA CA002589886A patent/CA2589886A1/en not_active Abandoned
- 2005-12-14 JP JP2007546841A patent/JP2008524228A/ja active Pending
- 2005-12-14 US US11/302,692 patent/US7371864B2/en active Active
- 2005-12-14 KR KR1020077013364A patent/KR20070087606A/ko not_active Withdrawn
- 2005-12-14 AU AU2005317158A patent/AU2005317158A1/en not_active Abandoned
- 2005-12-14 PE PE2005001450A patent/PE20060739A1/es not_active Application Discontinuation
- 2005-12-14 AR ARP050105253A patent/AR053990A1/es unknown
-
2007
- 2007-05-25 NO NO20072666A patent/NO20072666L/no unknown
- 2007-06-10 IL IL183825A patent/IL183825A0/en unknown
-
2008
- 2008-04-09 US US12/099,906 patent/US20080188517A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| BRPI0519331A2 (pt) | 2009-01-20 |
| US7371864B2 (en) | 2008-05-13 |
| JP2008524228A (ja) | 2008-07-10 |
| TW200634011A (en) | 2006-10-01 |
| US20060148846A1 (en) | 2006-07-06 |
| WO2006065853A3 (en) | 2006-08-24 |
| NO20072666L (no) | 2007-09-07 |
| KR20070087606A (ko) | 2007-08-28 |
| AR053990A1 (es) | 2007-05-30 |
| MX2007006919A (es) | 2007-06-26 |
| WO2006065853A2 (en) | 2006-06-22 |
| EP1828187A2 (en) | 2007-09-05 |
| PE20060739A1 (es) | 2006-08-16 |
| AU2005317158A1 (en) | 2006-06-22 |
| RU2007126770A (ru) | 2009-01-27 |
| US20080188517A1 (en) | 2008-08-07 |
| IL183825A0 (en) | 2007-09-20 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| FZDE | Discontinued |