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1. WO2006100565 - CRYSTALLINE FORMS OF A KNOWN PYRROLIDINE FACTOR XA INHIBITOR

Publication Number WO/2006/100565
Publication Date 28.09.2006
International Application No. PCT/IB2006/000633
International Filing Date 13.03.2006
Chapter 2 Demand Filed 06.06.2006
IPC
C07D 401/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
A61P 7/02 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
CPC
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 3/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
A61P 31/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04Antibacterial agents
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
A61P 7/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
Applicants
  • WARNER-LAMBERT COMPANY LLC [US]/[US] (AllExceptUS)
  • SAMAS, Brian, Matthew [US]/[US] (UsOnly)
  • VRIEZE, Derek, Clinton [US]/[US] (UsOnly)
Inventors
  • SAMAS, Brian, Matthew
  • VRIEZE, Derek, Clinton
Agents
  • FULLER, Grover, F., Jr.
Priority Data
60/664,87024.03.2005US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) CRYSTALLINE FORMS OF A KNOWN PYRROLIDINE FACTOR XA INHIBITOR
(FR) FORMES CRISTALLINES D'UN INHIBITEUR PYRROLIDINE CONNU DU FACTEUR XA
Abstract
(EN)
Disclosed are crystalline forms A, B and C of 1 ,2-Pyrrolidinedicarboxamide, N1 -(4- chlorophenyl)-N2-[2-fluoro-4-(2-oxo-1 (2H)-pyridinyl)phenyÊ]-4-methoxy-, (2R,4R)- (9Cl). These crystalline forms are characterized by their powder X-ray diffraction, solid-state NMR, as well as methods for the preparation and pharmaceutical compositions of the same which are useful for the treatment of acute, subacute, or chronic thrombotic disorders including treatment of venous thrombosis, arterial thrombosis, pulmonary embolism, myocardial infarction, cerebral infarction, restenosis, atherosclerosis, angina, primary and secondary deep vein thrombosis, thromboembolism associated with cardiovascular disease, including, but not limited to, acute coronary syndrome, atrial fibrillation, cardiac valve replacement and deep vein thrombosis. The crystalline forms of the present invention are also useful for the treatment of cancer, sepsis and diabetes.
(FR)
L'invention concerne les formes cristallines A, B et C de 1,2-Pyrrolidinedicarboxamide, N1 -(4- chlorophényl)-N2-[2-fluoro-4-(2-oxo-1 (2H)-pyridinyl)phényl]-4-méthoxy-, (2R,4R)- (9Cl). Ces formes cristallines sont caractérisées par leur diffraction des rayons X sur poudre et par leur RMN en phase solide. L'invention concerne également des procédés de préparation de ces formes cristallines, et des compositions pharmaceutiques de ces formes cristallines, qui peuvent servir au traitement des troubles thrombotiques aigus, subaigus ou chroniques, notamment au traitement des thromboses veineuses, des thromboses artérielles, des embolies pulmonaires, des infarctus du myocarde, des infarctus cérébraux, des resténoses, de l'athérosclérose, de l'angine de poitrine, des thromboses veineuses profondes primaires et secondaires, des thromboembolies associées à des maladies cardiovasculaires, notamment mais non exclusivement au syndrome coronarien aigu, à la fibrillation auriculaire, au remplacement des valvules cardiaques, et aux thromboses veineuses profondes. Les formes cristallines décrites conviennent également pour le traitement du cancer, des sepsies et du diabète.
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