Method of lowering low-density lipoprotein cholesterol or preventing a cardiac event in a subject who has atherosclerotic cardiovascular disease or who is atherosclerotic cardiovascular disease risk equivalent, involving administering to the subject a prophylactically effective amount of an RN Ai agent. Also, a method of preventing development of atherosclerotic cardiovascular disease in a subject involving administering to the subject a prophylactically effective amount of an RNAi agent. Further, a method of treating a subject who has atherosclerotic cardiovascular disease or who is atherosclerotic cardiovascular di sease risk equivalent involving administering to the subject a therapeutically effective amount of an RNAi agent.
A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
A61K 31/4174 - Arylalkylimidazoles, p. ex. oxymétazoline, naphazoline, miconazole
C07D 207/02 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec uniquement des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle
C07D 207/30 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec uniquement des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle comportant deux liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques
C07D 207/34 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec uniquement des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle comportant deux liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
3.
Pharmaceutical formulations comprising high purity cangrelor and methods for preparing and using the same
The present invention relates to high purity cangrelor, pharmaceutical formulations comprising high purity cangrelor as an active ingredient, methods for preparing such compounds and formulations, and methods for using the pharmaceutical formulations in the inhibition of platelet activation and aggregation.
A61K 31/70 - Hydrates de carboneSucresLeurs dérivés
A61K 31/7076 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées contenant des purines, p. ex. adénosine, acide adénylique
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
4.
HIGH PURITY ORITAVANCIN AND METHOD OF PRODUCING SAME
Drug substance preparations of oritavancin having high purity are disclosed, along with pharmaceutical compositions comprising such oritavancin drug substance preparations, and drug products or dosage forms comprising such pharmaceutical compositions.
Provided is a pharmaceutical composition comprising clevidipine in a sterile, ready to use, physically stable, aqueous dispersion of nanoparticles that stabilizes clevidipine against formation of impurities and is suitable for parenteral administration.
Methods of treating, reducing the incidence of, and/or preventing an ischemic event in a patient undergoing percutaneous coronary intervention (PCI), comprising administering to the patient a pharmaceutical composition comprising cangrelor. The method may further comprise administering an additional therapeutic agent to the patient, the additional therapeutic agent comprising bivalirudin or a P2Y12 inhibitor. Pharmaceutical compositions useful for treating, reducing the incidence of, and/or preventing an ischemic event in a patient undergoing PCI. The pharmaceutical compositions comprise cangrelor, and optionally bivalirudin. Methods of preparing a pharmaceutical composition for treating, reducing the incidence of, and/or preventing an ischemic event in a patient undergoing PCI, comprising admixing cangrelor with one or more pharmaceutically acceptable excipients. An ischemic event may include stent thrombosis, myocardial infarction, ischemia-driven revascularization, and mortality.
A61K 31/35 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à six chaînons avec un oxygène comme seul hétéro-atome d'un cycle
A61K 38/16 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
8.
METHODS FOR TREATING BACTERIAL INFECTIONS USING ORITAVANCIN AND POLYMYXINS
A61K 31/35 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à six chaînons avec un oxygène comme seul hétéro-atome d'un cycle
A61K 38/00 - Préparations médicinales contenant des peptides
A method for reducing or maintaining platelet inhibition in a patient by administering cangrelor prior to an invasive procedure is described. The method of this invention can be used for patients in need of antiplatelet therapy or at risk of thrombosis. The method can further be used in patients who were previously treated with long-acting platelet inhibitors without increasing the risk of excessive bleeding.
A method for reducing or maintaining platelet inhibition in a patient by administering cangrelor prior to an invasive procedure is described. The method of this invention can be used for patients in need of antiplatelet therapy or at risk of thrombosis. The method can further be used in patients who were previously treated with long-acting platelet inhibitors without increasing the risk of excessive bleeding.
Methods of treating, reducing the incidence of, and/or preventing an ischemic event in a patient undergoing percutaneous coronary intervention (PCI), comprising administering to the patient a pharmaceutical composition comprising cangrelor. The method may further comprise administering an additional therapeutic agent to the patient, the additional therapeutic agent comprising a P2Yi2 inhibitor. Pharmaceutical compositions useful for treating, reducing the incidence of, and/or preventing an ischemic event in a patient undergoing PCI. The pharmaceutical compositions comprise cangrelor. Methods of preparing a pharmaceutical composition for treating, reducing the incidence of, and/or preventing an ischemic event in a patient undergoing PCI, comprising admixing cangrelor with one or more pharmaceutically acceptable excipients. An ischemic event may include stent thrombosis, myocardial infarction, ischemia-driven revascularization, and mortality.
A61P 9/10 - Médicaments pour le traitement des troubles du système cardiovasculaire des maladies ischémiques ou athéroscléreuses, p. ex. médicaments antiangineux, vasodilatateurs coronariens, médicaments pour le traitement de l'infarctus du myocarde, de la rétinopathie, de l'insuffisance cérébro-vasculaire, de l'artériosclérose rénale
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p. ex. phosphate de pyridoxal
13.
METHODS OF TREATING, REDUCING THE INCIDENCE OF, AND/OR PREVENTING ISCHEMIC EVENTS
Methods of treating, reducing the incidence of, and/or preventing an ischemic event in a patient undergoing percutaneous coronary intervention (PCI), comprising administering to the patient a pharmaceutical composition comprising cangrelor. The method may further comprise administering an additional therapeutic agent to the patient, the additional therapeutic agent comprising a P2Y12 inhibitor. Pharmaceutical compositions useful for treating, reducing the incidence of, and/or preventing an ischemic event in a patient undergoing PCI. The pharmaceutical compositions comprise cangrelor. Methods of preparing a pharmaceutical composition for treating, reducing the incidence of, and/or preventing an ischemic event in a patient undergoing PCI, comprising admixing cangrelor with one or more pharmaceutically acceptable excipients. An ischemic event may include stent thrombosis, myocardial infarction, ischemia-driven revascularization, and mortality.
A61K 31/7064 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées
14.
METHODS FOR CONTROLLING BLOOD PRESSURE AND REDUCING DYSPNEA IN HEART FAILURE
Methods for controlling, maintaining, or reducing blood pressure, and/or for treating, preventing, or alleviating symptoms such as dyspnea, in a patient suffering from or susceptible to acute heart failure. The methods involve the administration of an effective amount of a pharmaceutical composition comprising a short acting dihydropyridine compound such as clevidipine. The pharmaceutical composition may be administered at an initial dose, and if blood pressure is not controlled or maintained within a target blood pressure range or reduced to within a target blood pressure range, the initial dose may be titrated to achieve a blood pressure within the target blood pressure range. The patient may have a systolic blood pressure of about 120 mmHg or above.
A01N 37/30 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés organiques comportant un atome de carbone possédant trois liaisons à des hétéro-atomes, avec au plus deux liaisons à un halogène, p. ex. acides carboxyliques contenant le groupe —CO—N, p. ex. amides ou imides d'acide carboxyliqueLeurs thio-analogues contenant les groupes —CO—N et , les deux étant liés directement par leur atome de carbone au même squelette carboné, p. ex. H2N—NH—CO—C6H4—COOCH3Leurs thio-analogues
15.
METHODS OF BLOCKING PLATELET ACTIVATION DURING EXTRACORPOREAL CIRCULATION USING CANGRELOR
The present invention is directed to methods of protecting platelets during medical procedures that include extracorporeal circulation (ECC) or hypothermia, or both. The methods comprise administering a pharmaceutical composition comprising the P2Y12 ADP receptor blocker cangrelor to a subject undergoing a medical procedure that includes ECC or hypothermia, or both. The protection of platelets through the methods of the present invention includes inhibiting activation of platelets, inhibiting platelet granule release, inhibiting platelet- leukocyte aggregation and inhibiting platelet loss from the blood of the subject.
Methods of inhibiting, treating or preventing blood loss in a subject undergoing surgery through the administration of an effective amount of the novel serine protease inhibitor MDCO-2010 or its salts or esters are disclosed.
A61K 31/166 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome de carbone d'un groupe carboxamide lié directement au cycle aromatique, p. ex. procaïnamide, procarbazine, métoclopramide, labétalol
The present invention relates to methods for treating or preventing a properd related disease or disorder in a subject in need thereof, or for reducing mortality of a subject suffering from a properdin-related disease or disorder, comprising administering to the subject an effective amount of a pharmaceutical composition comprising a properdin protein. Also provided are related medicaments, pharmaceutical compositions, and methods for preparing the medicaments.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
C07K 14/47 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains provenant de vertébrés provenant de mammifères
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
18.
MAINTENANCE OF PLATELET INHIBITION DURING ANTIPLATELET THERAPY
A method for reducing or maintaining platelet inhibition in a patient by administering cangrelor prior to an invasive procedure Is described. The method of this invention can be used for patients in need of antipiatelet therapy or at risk of thrombosis. The method can further be used in patients who were previously treated with long-acting platelet inhibitors without increasing the risk of excessive bleeding.
A01N 43/04 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un ou plusieurs atomes d'oxygène ou de soufre comme uniques hétéro-atomes du cycle avec un hétéro-atome
The present invention is directed to a disk diffusion assay for determining susceptibility of bacteria to a glycopeptide antibiotic. The assay includes improvements over conventional assays due to the inclusion of polysorbate 80 and Span 80 in the antibacterial solution used to impregnate paper disks used in the assay.
C12Q 1/18 - Test de l'activité antimicrobienne d'un matériau
C12Q 1/04 - Détermination de la présence ou du type de micro-organismeEmploi de milieux sélectifs pour tester des antibiotiques ou des bactéricidesCompositions à cet effet contenant un indicateur chimique
20.
SHORT -ACTING DIHYDROPYRIDINES (CLEVIDIPINE) FOR USE IN REDUCING STROKE DAMAGE
The present invention relates to methods for lowering stroke damages and/or lowering blood pressure in a subject with a stroke in need thereof, comprising administering to the subject an effective amount of a pharmaceutical composition comprising a short acting dihydropyridine compound, preferably clevidipine or a pharmaceutically acceptable salt or ester thereof. Also provided are related medicaments, pharmaceutical compositions, and methods for preparing the medicaments.
The present invention relates to methods for treating or preventing pulmonary hypertension, reducing mortality in a subject experiencing pulmonary hypertension, or inhibiting ADP-mediated vasoconstriction of pulmonary arteries in a subject, comprising administering to the subject an effective amount of a pharmaceutical composition comprising a reversible P2Yi2 receptor antagonist. Also provided are related medicaments, pharmaceutical compositions, and methods for preparing the medicaments.
Pharmaceutical formulations comprising clevidipine and an antimicrobial agent exhibit a reduced propensity for microbial growth and provide increased convenience to health care workers administering clevidipine-containing formulations to patients.
A01N 37/30 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés organiques comportant un atome de carbone possédant trois liaisons à des hétéro-atomes, avec au plus deux liaisons à un halogène, p. ex. acides carboxyliques contenant le groupe —CO—N, p. ex. amides ou imides d'acide carboxyliqueLeurs thio-analogues contenant les groupes —CO—N et , les deux étant liés directement par leur atome de carbone au même squelette carboné, p. ex. H2N—NH—CO—C6H4—COOCH3Leurs thio-analogues
A61K 31/205 - Sels d'addition d'acides organiques avec des aminesSels d'ammonium quaternaire internes, p. ex. bétaïne, carnitine
The present invention is directed to the following: methods of treating or preventing stent thrombosis using pharmaceutical compositions comprising cangrelor and optionally bivalirudin; methods of reducing mortality in a subject undergoing stent implantation using pharmaceutical compositions comprising cangrelor and optionally bivalirudin; medicaments comprising cangrelor and optionally bivalirudin useful for treating or preventing stent thrombosis, or useful for reducing mortality in a subject undergoing stent implantation; pharmaceutical compositions comprising cangrelor and bivalirudin; and methods of preparing a medicament comprising cangrelor and optionally bivalirudin useful for treating or preventing stent thrombosis, or useful for reducing mortality in a subject undergoing stent implantation.
A61F 2/82 - Dispositifs maintenant le passage ou évitant l’affaissement de structures tubulaires du corps, p. ex. stents
A61L 33/04 - Utilisation de matériaux organiques, p. ex. d'acide acétylsalicylique
A61K 31/4365 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique ayant le soufre comme hétéro-atome du cycle, p. ex. ticlopidine
A61L 27/54 - Matériaux biologiquement actifs, p. ex. substances thérapeutiques
The invention relates to derivatives of glycopeptide and lipoglycopeptide antibiotics possessing an altered ionization state with respect to the parent glycopeptide or lipoglycopeptide antibiotic, and having the ability to be regenerated as the parent glycopeptide or lipoglycopeptide antibiotic under physiological conditions. These compounds are useful as antibiotics for the prevention and/or the treatment of bacterial infections.
Pharmaceutical compositions, and a method of stabilizing pharmaceutical compositions having clevidipine, or any pharmaceutically acceptable salt thereof, as the active ingredient is descried. The method includes the slowing down or inhibiting of the oxidation pathway of clevidipine. This can be accomplished by reducing the amount the pharmaceutical composition is exposed to oxygen and/or light during the, manufacturing and storing processes. According to this method, oxygen must be removed or replaced, or light must be sufficiently blocked such that light energy cannot reach the active ingredient of the composition, or is reduced to a level that the light-induced oxidation reaction converting clevidipine to H324nS is minimized, such that the total detectable level of H324nS in a given composition sample does not exceed about 0 2% on a weight-by-weight basis.
A01N 43/90 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant plusieurs hétérocycles déterminants condensés entre eux ou avec un système carbocyclique commun
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
27.
PHARMACEUTICAL COMPOSITIONS AND METHODS FOR PRODUCING LOW IMPURITY CONCENTRATIONS OF THE SAME
A composition having clevidipine as an active ingredient is described. The composition includes clevidipine as an active ingredient and an amount of the impurity H168/79 that is no greater than about 1.5%, or where the ratio between clevidipine and H168/79 is equal or above 60 to 1.
A01N 43/90 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant plusieurs hétérocycles déterminants condensés entre eux ou avec un système carbocyclique commun
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
28.
MAINTENANCE OF PLATELET INHIBITION DURING ANTIPLATELET THERAPY
A method of treating or preventing a disease or condition in a subject that was previously treated with at least one thienopyhdine is described. The method includes administering to the subject an effective amount of at least one reversible, short-acting P2Yi2 inhibitor. The described method can be used for subjects diagnosed with symptoms such as stable or unstable angina, vascular ischemic events, atherosclerosis, acute coronary syndrome, as well as STEMi or N-STEMI. The described method can also be used for patients having previously received a stent, such as a bare metal stent or a drug-eluting stent, and the treatment or prevention of stent thrombosis. The method can be used prior to, during, or after an invasive procedure such as coronary artery bypass grafting, percutaneous coronary intervention, or other genera! surgical procedure.
A method of treating or preventing a disease or condition in a subject in need of an invasive procedure that was previously treated with at least one thienopyridine is described. The method includes administering to the subject prior to such invasive procedure an effective amount of at ieast one reversible, short-acting P2Y12 inhibitor. The described method can be used for subjects diagnosed with symptoms such as stable or unstable angina, vascular ischemic events, atherosclerosis, acute coronary syndrome, as well as STEMI or N- STEMI. The described method can also be used for patients having previously received a stent, such as a bare metal stent or a drug-eluting stent, and the treatment or prevention of stent thrombosis. The method can be used prior to invasive procedures such as coronary artery bypass grafting, percutaneous coronary intervention, or other general surgical procedure.
brevets
