摘要:
The present invention relates to certain pharmaceutical compositions of a 5-HT2A serotonin receptor modulator and methods for preparing pharmaceutical composition related thereto. The pharmaceutical compositions are useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.
摘要:
The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.
摘要:
A compound of formula: ##STR1## in which X.sup.1 is a reactive group that can react to form a covalent bond with a reactive group on the surface of a material to be rendered biocompatible, X.sup.2 is a group --O.sup..crclbar. or a precursor of such a group, n is 2, 3 or 4, Y is a group --N.sup..sym. R.sub.3 A.sup..crclbar. wherein each R, which may be the same or different, is a C.sub.1 -C.sub.4 alkyl group and A.sup..crclbar. is an anion present when X.sup.2 is an electrically neutral group or Y is ##STR2## wherein R.sup.1 together with X.sup.2 forms a direct bond between the nitrogen and the phosphorus atoms.
摘要:
A compound of formula: ##STR1## in which X.sup.1 is a reactive group that can react to form a covalent bond with a reactive group on the surface of a material to be rendered biocompatible, X.sup.2 is a group -O.sup..crclbar. or a precursor of such a group, n is 2, 3 or 4, Y is a group --N.sup..sym. R.sub.3 A.sup..crclbar. wherein each R, which may be the same or different, is a C.sub.1 -C.sub.4 alkyl group and A.sup..crclbar. is an anion present when X.sup.2 is an electrically neutral group or Y is ##STR2## wherein R.sup.1 together with X.sup.2 forms a direct bond between the nitrogen and the phosphorus atoms.
摘要:
A compound of formula: ##STR1## in which X.sup.1 is a reactive group that can react to form a covalent bond with a reactive group on the surface of a material to be rendered biocompatible, X.sup.2 is a group -0.sup..crclbar. or a precursor of such a group, n is 2, 3 or 4, Y is a group --N.sup..sym. R.sub.3 A.sup..crclbar. wherein each R, which may be the same or different, is a C.sub.1 -C.sub.4 alkyl group and A.sup..crclbar. is an anion present when X.sup.2 is an electrically neutral group or Y is ##STR2## wherein R.sup.1 together with X.sup.2 forms a direct bond between the nitrogen and the phosphorus atoms.
摘要:
New phospholipids containing a conjugated di-yne system have the formula: ##STR1## wherein at least one of B.sub.1 and B.sub.2 is a group of the formula--(CO).sub.p --X.sub.1 --C.tbd.C--C.tbd.C--Y.sub.1wherein p is 0 or 1, X.sub.1 is a direct bond or a divalent aliphatic or cycloaliphatic group, Y.sub.1 is H or a monovalent aliphatic or cycloaliphatic group, the total number of carbon atoms in X.sub.1 and Y.sub.1 in each of B.sub.1 and/or B.sub.2 being 8 to 26; and the other of B.sub.1 and B.sub.2 is either (a) the same or a different group of the formula:--(CO).sub.p --X.sub.1 --C.tbd.C--C.tbd.C--Y.sub.1where X.sub.1, Y.sub.1 or p are as defined above;or (b) is an aliphatic or cycloaliphatic group containing at least 8 carbon atoms; n is 0 or 1, m is 2, 3 or 4 and each R independently represents an alkyl group containing 1 to 4 carbon atoms, and are prepared by esterification and/or etherification of glycerol by conventional techniques. The conjugated di-yne systems can be cross-linked by actinic radiation to give intermolecular and, in certain cases, also intramolecular cross-linking. Thin layers of the phospholipids can be coated onto substrates subsequently to be brought into contact with blood or other body fluids and then cross-linked to give polymer coated surfaces which have a reduced tendency to initiate blood coagulation, for example, compared to untreated surfaces. Artificial lenses for the human eye treated in this way have a reduced tendency to cause endothelial damage. The phospholipids of the invention can also be formed into liposomes and the conjugated di-yne system then cross-linked. Physiologically active materials such as drugs, enzymes or antigens can be incorporated into the liposomes which can then be used as prolonged release formulations.
摘要:
The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.
摘要:
The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.
摘要:
The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.