The present invention provides a method of treating symptoms associated with Androgen Deprivation Therapy comprising administering to a patient in need of such treatment an effective amount of a compound of Formula I:
The present invention provides a method of treating symptoms associated with Androgen Deprivation Therapy comprising administering to a patient in need of such treatment an effective amount of a compound of Formula I:
The present invention provides a method of treating symptoms associated with Androgen Deprivation Therapy comprising administering to a patient in need of such treatment an effective amount of a compound of Formula I:
or a pharmaceutically acceptable salt thereof.
A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
C07D 209/94 - [b, c]- or [b, d]-condensed containing carbocyclic rings other than six-membered
C07D 401/06 - Heterocyclic 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 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 493/22 - Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 309/20 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hydrogen atoms and substituted hydrocarbon radicals directly attached to ring carbon atoms
C07C 1/34 - Preparation of hydrocarbons from one or more compounds, none of them being a hydrocarbon starting from compounds containing hetero atoms other than, or in addition to, oxygen or halogen reacting phosphines with aldehydes or ketones, e.g. Wittig reaction
C07C 45/29 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by oxidation of hydroxy groups
C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
A compound having the general structure shown in Formula I:
1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
C07D 515/00 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups , or
C07D 401/04 - Heterocyclic 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 containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 211/66 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4 having a hetero atom as the second substituent in position 4
C07D 211/76 - Oxygen atoms attached in position 2 or 6
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
A61K 31/4523 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
The invention relates to pharmaceutical compositions and dosage forms having a piperidine carbonitrile as an active ingredient for the treatment of various diseases and conditions. The preferred compound is a crystalline form of a trifluoromethylphenylalkoxyalkylheteroarylaryl piperidine carbonitrile. Methods of treating diseases and conditions are disclosed as well as processes to make crystalline forms of the above compounds.
A61K 31/54 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
6.
Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds
This application discloses a process to synthesize 8-({1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy)-methyl]-8-pheny-1,7-diazaspiro[4.5]decan-2-one comprising reacting a compound of the Formula 27a-sulfonate with zinc in the presence of acetic acid.
Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds
This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.
C07D 207/267 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the ring nitrogen atom
C07C 217/46 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and unsaturated
C07C 217/48 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing rings
8.
Hydrochloride salts of 8-[1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxymethyl]-8-phenyl-1,7-diazaspiro[4,5]decan-2-one and preparation process therefor
Disclosed are hydrochloride and tosylate crystalline salt forms of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I and methods of preparing the same.
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
A61K 31/435 - 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
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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human growth hormone, and pharmaceutical preparations
containing human growth hormone, or for the treatment of
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[ chemical preparations for scientific purposes; chemical preparations, namely, diagnostic reagents for scientific or research use ] [ diagnostic agents, preparations and substances for medical purposes; ] pharmaceutical preparations for the treatment of kidney diseases; pharmaceutical preparations for the treating diseases and disorders of the parathyroid, and for treating secondary hyper-parathyroidism; pharmaceutical preparations for the treatment of vitamin D deficiency [ ; pharmaceutical preparations for use in renal dialysis and in the treatment of renal diseases and kidney ailments; pharmaceutical preparations in the nature of phosphate binders for use in the treatment of hyperphosphataemial; human growth hormone; medical diagnostic kits comprised of medical diagnostic reagents and assays for testing body fluids ] [ computer software for analyzing medical test results, the software relating to the scientific, pharmaceutical, genetic, medical and medical diagnostic fields; computer software for operating medical diagnostic apparatus, the software relating to at least one of the scientific, pharmaceutical, genetic, medical and medical diagnostic fields ] [ in-vitro diagnostic testing medical instruments for testing blood and other bodily fluids and tissues; medical instruments for use in monitoring the content of bodily fluids; medical apparatus for testing for the presence of particular substances in blood; medical devices for detecting cancer; medical devices for diagnosing vitamin D deficiencies; medical diagnostic apparatus in the nature of a diagnostic card containing medical diagnostic reagents and immunoassays sold together as a kit for at least one of the following: testing body fluids, diagnosing urological disease, kidney disease, cancer, and vitamin deficiencies ]
A compound having the general structure shown in Formula I:
1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 211/66 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4 having a hetero atom as the second substituent in position 4
C07D 211/76 - Oxygen atoms attached in position 2 or 6
C07D 401/04 - Heterocyclic 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 containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
A61K 31/4523 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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Drug testing kits comprised of medical diagnostic reagents and assays for testing body fluids; medical diagnostic reagents and assays for testing of body fluids and biologic samples; assays, reagents and antibodies and compounds for testing patient samples for diseases and medical conditions; preparations for clinical and medical laboratory use, namely assay controls and standards for medical diagnostic testing; medical diagnostic reagents and assays. Computer software; computer programs; all relating to the scientific, pharmaceutical, genetic, medical or medical diagnostic fields; computer software for use in the operation of diagnostic apparatus and instruments; computer software for analysis and reporting of medical and laboratory test results; Communications software for providing medical diagnostic test information; automated laboratory testing apparatus for the analysis of bodily fluids; Computerized instruments for use in the clinical laboratory for analyzing blood and biological samples. Surgical apparatus and instruments; medical apparatus and instruments; parts and fittings for the aforesaid goods; medical instruments for use in in-vitro diagnostic testing, monitoring and/or treatment; microfluidic cards with channels having medical diagnostic reagents and antibodies for testing patient samples; diagnostic cards and cartridges containing diagnostic solutions and reagents; microfluidic cards for blood testing; diagnostic cards and cartridges containing medical diagnostic reagents and immunoassays, sold together as a kit; medical diagnostic instruments, medical diagnostic kits. Printed reports featuring laboratory, clinical and diagnostic testing information and results; printed information, namely, reports, pamphlets, brochures and leaflets featuring diagnostic testing, medical and health information; printed information, namely, reports, pamphlets, brochures and leaflets providing information on medical, hospital, insurance, and billing records; and instruction sheets regarding medical testing procedures and testing results. Computerized database management for tracking patient information for diagnostic and medical testing; product demonstration services in the field of medical diagnostic testing; computerized data base management of diagnostic testing and results; computerized data base management of medical, hospital, insurance and accounting records. Pharmaceutical and diagnostic research and development; scientific consultation services; computer services, namely, electronic storage and retrieval of messages and data in the fields of diagnostic testing and preparations for the treatment, monitoring or diagnosis of disease; computer services, namely, electronic storage and retrieval of medical and biological specimens and of diagnostic assays. Referral services in the fields of medical, health and clinical care; providing information regarding hospital records, namely, information relating to personal medical history records; medical and testing information services, namely, providing information regarding diagnostic testing results, testing procedures, disease conditions and disease prevention; providing information regarding medical and hospital records; and medical consultation services, including the taking and analysing of blood.
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Chemical preparations; chemical reagents; diagnostic test kits and reagents for scientific and research use; assays and reagents for use in genetic testing; biochemicals. Pharmaceutical preparations and compounds; Therapeutic preparations and compounds; Veterinary preparations; Biologics and modified proteins; nutritional supplements, vitamin supplements, pharmaceutical preparations for the treatment of diseases and disorders of the parathyroid, secondary hyper-parathyroidism; preparations for the treatment of vitamin D deficiency; pharmaceutical and veterinary preparations for use in renal dialysis and in the treatment of renal diseases and kidney ailments; phosphate binders for use in the treatment of hyperphosphataemial; human growth hormone, and pharmaceutical preparations containing human growth hormone, or for the treatment of growth hormone disorders, medical diagnostic reagents, assays, solutions and compounds; reagents and assays for testing blood; Immunoassays; medical diagnostic kits; Preparations for detecting genetic disorders and predispositions, preparations for treating genetic disorders and diseases, gene therapy products. Computer software; computer programs; all relating to the scientific, pharmaceutical, genetic, medical and medical diagnostic fields; computer software for use in the operation of diagnostic apparatus and instruments. Surgical apparatus and instruments; medical apparatus and instruments; parts and fittings for the aforesaid goods; medical instruments for use in in-vitro diagnostic testing, monitoring and/or treatment; microfluidic cards with channels having medical diagnostic reagents and antibodies for testing patient samples; Diagnostic cards containing diagnostic solutions and reagents; Microfluidic cards for blood testing; Diagnostic card containing medical diagnostic reagents and immunoassays, sold together as a kit.
19.
Pharmaceutical formulations: salts of 8-[1-3,5-bis-(trifluoromethyl)phenyl)-ethoxy-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one and treatment methods using the same
Pharmaceutical formulations containing salts of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl]-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I, are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.
A61K 31/435 - 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
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
20.
Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds
This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.
C07D 207/267 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the ring nitrogen atom
C07C 217/48 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing rings
Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds
This application discloses a process to synthesize 8-({1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy)-methyl]-8-pheny-1.7-diaza-spiro[4.5]decan-2-one comprising reacting a compound of the Formula 27a-sulfonate with zinc in the presence of acetic acid.
Hypersulfated disaccharides with utility in asthma or asthma related disorders are disclosed. The compounds are formulated with agents that enhance the oral delivery of the hypersulfated disaccharides. The delivery agents are selected from the group consisting of natural or synthetic polymers having ionic side chains as well as other compounds or types of compounds that improve the bioavailability of the disaccharides relative to delivery of the drug without such agents. The hypersulfated disaccharides are made from heparin or salts thereof.
A compound having the general structure shown in Formula I:
1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
C07D 215/12 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
C07D 215/16 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 213/02 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
C07D 405/00 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
Hypersulfated disaccharides of formula I and other hypersulfated disaccharides disclosed herein are used to treat diseases or conditions associated with human neutrophil elastase imbalances. The disaccharides and/or intermediates useful to prepare such compounds are prepared from heparin. The diseases and conditions which are treated with a compound of formula I include chronic obstructive pulmonary disorder (COPD) and cystic fibrosis (CF). The formulations are delivered to the lungs in an aerosol formulation or dry powder means or via nebulization. Oral forms are also suitable.
A01N 43/04 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom
A61K 31/715 - Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkagesDerivatives thereof, e.g. ethers, esters
28.
Pharmaceutical formulations:salts of 8-[1-3,5-bis-(trifluoromethyl)phenyl)-ethoxymethyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one and treatment methods using the same
Pharmaceutical formulations containing salts of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl]-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I, are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.
A61K 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
C07D 219/00 - Heterocyclic compounds containing acridine or hydrogenated acridine ring systems
Hypersulfated disaccharides, preferably octasulfated sucrose, with -utility in asthma or asthma related disorders are disclosed. The compounds may optionally be formulated with pharmaceutically acceptable excipients or delivery agents. The delivery agents are selected from the group consisting of natural or synthetic polymers, aerosol s or other vehicles that facilitate the delivery or administration of the drug. The hypersulfated disaccharides are made from carbohydrate starting materials, ion exchange or other suitable synthetic processes may be utilized to prepare the pharmaceuticals. The hypersulfated disaccharides are useful as anti-inflammatory agents.
A01N 43/16 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom six-membered rings with oxygen as the ring hetero atom
A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
A61K 31/35 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
30.
METHODS AND COMPOSITIONS FOR REDUCING PARATHYROID LEVELS
Methods and compositions for reducing serum parathyroid levels in, for example, chronic kidney disease patients are disclosed. In these methods, an effective amount of a modified release formulation of 25 -hydroxy vitamin D is orally administered to a patient suffering from secondary hyperparathyroidism to lower the patient' s serum intact parathyroid hormone (iPTH) level, while avoiding a surge in serum total 25 -hydroxy vitamin D.
Methods and compositions for reducing serum parathyroid levels in, for example, chronic kidney disease patients are disclosed. In these methods, an effective amount of a modified release formulation of 25 -hydroxy vitamin D is orally administered to a patient suffering from secondary hyperparathyroidism to lower the patient' s serum intact parathyroid hormone (iPTH) level, while avoiding a surge in serum total 25 -hydroxy vitamin D.
Hypersulfated disaccharides with utility in asthma or asthma related disorders are disclosed. The compounds are formulated with agents that enhance the oral delivery of the hypersulfated disaccharides. The delivery agents are selected from the group consisting of natural or synthetic polymers having ionic side chains as well as other compounds or types of compounds that improve the bioavailability of the disaccharides relative to delivery of the drug without such agents. The hypersulfated disaccharides are made from heparin or salts thereof.
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
Hypersulfated disaccharides with utility in asthma or asthma related disorders are disclosed. The compounds are formulated with agents that enhance the oral delivery of the hypersulfated disaccharides. The delivery agents are selected from the group consisting of natural or synthetic polymers having ionic side chains as well as other compounds or types of compounds that improve the bioavailability of the disaccharides relative to delivery of the drug without such agents. The hypersulfated disaccharides are made from heparin or salts thereof.
A01N 43/04 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom
A61K 31/715 - Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkagesDerivatives thereof, e.g. ethers, esters
Hypersulfated disaccharides with utility in asthma or asthma related disorders are disclosed. The compounds are formulated with agents that enhance the oral delivery of the hypersulfated disaccharides. The delivery agents are selected from the group consisting of natural or synthetic polymers having ionic side chains as well as other compounds or types of compounds that improve the bioavailability of the disaccharides relative to delivery of the drug without such agents. The hypersulfated disaccharides are made from heparin or salts thereof.
A01N 43/04 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom
Disclosed herein are siRNA compositions and methods useful for inhibiting expression of vascular endothelial growth factor (VEGF) isoforms. Diseases which involve angiogenesis stimulated by overexpression of VEGF, such as diabetic retinopathy, age related macular degeneration and many types of cancer, can be treated by administering small interfering RNAs as disclosed.
An ophthalmic shunt implantable in an eye having an elongate body (10) and a branched conduit (40) for conducting aqueous humor from an anterior chamber of the eye to the suprachoroidal space of the eye and the subconjunctival space, and a plate extending from an upper surface of the elongate body.
Pharmaceutical compositions for intravenous administration comprising the compound of Formula I
or pharmaceutically acceptable salts, hydrates or prodrugs thereof are described herein. Methods of preparing the pharmaceutical compositions and methods for treating nausea and/or emesis with the pharmaceutical compositions are also described herein.
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
38.
INTRAVENOUS FORMULATIONS OF NEUROKININ-1 ANTAGONISTS
Pharmaceutical compositions for intravenous administration comprising the compound of Formula I, or pharmaceutically acceptable salts, hydrates or prodrugs thereof are described herein. Methods of preparing the pharmaceutical compositions and methods for treating nausea and/or emesis with the pharmaceutical compositions are also described herein.
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
A61K 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61P 1/08 - Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigoAntiemetics
Pharmaceutical compositions for intravenous administration comprising the compound of Formula I, or pharmaceutically acceptable salts, hydrates or prodrugs thereof are described herein. Methods of preparing the pharmaceutical compositions and methods for treating nausea and/or emesis with the pharmaceutical compositions are also described herein.
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM (USA)
OPKO HEALTH, INC. (USA)
Inventor
Moola, Reddy
German, Dwight
Connell, Steven
Wilson, Rosemary
Wilson, Johnnie
Kodadek, Thomas
Abstract
The present invention provides for the identification of individuals having neurodegenerative diseases (ND). Peptoids recognized by Parkinson's Disease- and Alzheimer's Disease-specific antibodies are identified, allowing one to diagnose or predict ND in subjects.
THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM (USA)
OPKO HEALTH, INC. (USA)
Inventor
Moola, Reddy
German, Dwight
Connell, Steven
Wilson, Rosemary
Wilson, Johnnie
Kodadek, Thomas
Abstract
The present invention provides for the identification of individuals having neurodegenerative diseases (ND). Peptoids recognized by Parkinson's Disease- and Alzheimer's Disease-specific antibodies are identified, allowing one to diagnose or predict ND in subjects.
The Board of Regents of the University of Texas System (USA)
OPKO Health, Inc. (USA)
Inventor
Moola, Muralidhar Reddy
German, Dwight
Connell, Steven
Wilson, Rosemary
Wilson, Johnnie
Kodadek, Thomas
Abstract
The present invention provides for the identification of individuals having neurodegenerative diseases (ND). Peptoids recognized by Parkinson's Disease- and Alzheimer's Disease-specific antibodies are identified, allowing one to diagnose or predict ND in subjects.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
C07K 16/44 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material not provided for elsewhere
C07C 237/20 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
C07D 317/58 - Radicals substituted by nitrogen atoms
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
C40B 30/04 - Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
G01N 33/564 - ImmunoassayBiospecific binding assayMaterials therefor for pre-existing immune complex or autoimmune disease
43.
PEPTOID LIGANDS FOR ISOLATION AND TREATMENT OF AUTOIMMUNE T-CELLS
THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM (USA)
OPKO HEALTH, INC. (USA)
Inventor
Gocke, Anne, R.
Udugamasooriya, D., Gomika
Kodadek, Thomas
Abstract
The present invention provides for the identification of autoreactive T cell populations from individuals having autoimmune diseases, such as multiple sclerosis and EAE. Peptoids recognized by autoreactive T cells can be used to identify various types of autoimmune disease, and can also be used to target therapies against such populations.
G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
C07K 7/00 - Peptides having 5 to 20 amino acids in a fully defined sequenceDerivatives thereof
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
44.
STRUCTURES FOR CONTROLLING LIGHT INTERACTION WITH MICROFLUIDIC DEVICES
Systems and methods for improved measurement of absorbance/transmission through fluidic systems are described. Specifically, in one set of embodiments, optical elements are fabricated on one side of a transparent fluidic device opposite a series of fluidic channels. The optical elements may guide incident light passing through the device such that most of the light is dispersed away from specific areas of the device, such as intervening portions between the fluidic channels. By decreasing the amount of light incident upon these intervening portions, the amount of noise in the detection signal can be decreased when using certain optical detection systems. In some embodiments, the optical elements comprise triangular grooves formed on or in a surface of the device. The draft angle of the triangular grooves may be chosen such that incident light normal to the surface of the device is redirected at an angle dependent upon the indices of refraction of the external medium (e.g., air) and the device material. Advantageously, certain optical elements described herein may be fabricated along with the fluidic channels of the device in one step, thereby reducing the costs of fabrication. Furthermore, in some cases the optical elements do not require alignment with a detector and, therefore, facilitate assembly and/or use by an end user.
A compound having the general structure shown in Formula I:
1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
C07D 215/12 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
C07D 215/16 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 213/02 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
C07D 211/02 - Preparation by ring-closure or hydrogenation
C07D 405/00 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
46.
IMPROVED REAGENT STORAGE IN MICROFLUIDIC SYSTEMS AND RELATED ARTICLES AND METHODS
Fluidic devices and methods including those that provide storage and/or facilitate fluid handling of reagents are provided. Fluidic devices described herein may include channel segments positioned on two sides of an article, optionally connected by an intervening channel passing through the article. The channel segments may be used to store reagents in the device prior to first use by an end user. The stored reagents may include fluid plugs positioned in linear order so that during use, as fluids flow to a reaction site, they are delivered in a predetermined sequence. The specific geometries of the channel segments and the positions of the channel segments within the fluidic devices described herein may allow fluid reagents to be stored for extended periods of time without mixing, even during routine handling of the devices such as during shipping of the devices, and when the devices are subjected to physical shock or vibration.
Disclosed herein are siRNA compositions and methods useful for inhibiting expression of vascular endothelial growth factor (VEGF) isoforms. Such compositions and methods further involve siRNA capable of selectively targeting angiogenic VEGF isoforms while selectively sparing anti-angiogenic isoforms. Diseases which involve angiogenesis stimulated by overexpression of VEGF, such as diabetic retinopathy, age related macular degeneration and many types of cancer, can be treated by administering small interfering RNAs as disclosed.
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
A61P 9/10 - 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
48.
Pharmaceutical formulations: salts of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-Ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one and treatment methods using the same
Pharmaceutical formulations containing salts of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl]-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I, are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.
C07D 215/00 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
C07D 491/00 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or
49.
Tablet formulations containing 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one salts and tablets made therefrom
Pharmaceutical formulations containing a salt of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I, which are suitable for forming into a tablet dosage form, as well as tablet dosage forms are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
C07D 491/00 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or
C07D 495/00 - Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
C07D 215/00 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
C07D 219/00 - Heterocyclic compounds containing acridine or hydrogenated acridine ring systems
50.
Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds
This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations.
PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF 8-[{1-(3,5-BIS-(TRIFLUOROMETHYL)PHENYL)-ETHOXY}-METHYL]-8-PHENYL-1,7-DIAZA-SPIRO[4.5]DECAN-2-ONE COMPOUNDS
This application discloses a novel process to synthesize 8-[{1-(3,5-Bis- (trifluoromethyl)phenyl)-ethoxy}-nnethyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes. IM=102123
PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF 8-[{1-(3,5-BIS-(TRIFLUOROMETHYL)PHENYL)-ETHOXY}-METHYL]-8-PHENYL-1,7-DIAZA-SPIRO[4.5]DECAN-2-ONE COMPOUNDS
This application discloses a novel process to synthesize 8-[{1-(3,5-Bis- (trifluoromethyl)phenyl)-ethoxy}--nnethyl]-8-phenyl-1,7-diaza- spiro[4.5]decan-2-one compounds, which maybe used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes. IM=102123
Hydrochloride salts of 8-[{1-(3,5-Bis-trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one and preparation process therefor
Disclosed are hydrochloride and tosylate crystalline salt forms of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I and methods of preparing the same.
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
A01N 45/00 - Biocides, pest repellants or attractants, or plant growth regulators containing compounds having three or more carbocyclic rings condensed among themselves, at least one ring not being a six-membered ring
A61K 31/59 - Compounds containing 9,10-seco-cyclopenta[a]hydro- phenanthrene ring systems
Microfluidic systems and methods including those that provide control of fluid flow are provided. Such systems and methods can be used, for example, to control pressure-driven flow based on the influence of channel geometry and the viscosity of one or more fluids inside the system. One method includes flowing a plug of a low viscosity fluid and a plug of a high viscosity fluid in a channel including a flow constriction region and a non-constriction region. In one embodiment, the low viscosity fluid flows at a first flow rate in the channel and the flow rate is not substantially affected by the flow constriction region. When the high viscosity fluid flows from the non-constriction region to the flow constriction region, the flow rates of the fluids decrease substantially, since the flow rates, in some systems, are influenced by the highest viscosity fluid flowing in the smallest cross-sectional area of the system (e.g., the flow constriction region). This causes the fluids to flow at the same flow rate at which the high viscosity fluid flows in the flow constriction region. Accordingly, by designing microfluidic systems with flow constriction regions positioned at particular locations and by choosing appropriate viscosities of fluids, a fluid can be made to speed up or slow down at different locations within the system without the use of valves and/or without external control.
Methods for diagnosing, treating, and preventing catabolism-related vitamin D deficiency and related disorders; related compositions, apparatus and kits, are disclosed. A method involves measuring CYP24 expression and/or activity, or a proxy thereof such as FGF23 level, in a patient and correlating abnormally elevated CYP24 expression and/or activity with catabolism-related vitamin D deficiency or with susceptibility for catabolism-related vitamin D deficiency. In response to abnormally elevated CYP24 expression and/or activity, the method further includes administering a CYP24 inhibitor to the vitamin D deficient or at-risk patient, and preferably avoiding activation of the vitamin D binding receptor, such as by avoiding administration of active vitamin D compounds to such patients. Optionally, a vitamin D prohormone or prohormone can be administered.
C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
C12Q 1/6809 - Methods for determination or identification of nucleic acids involving differential detection
A61K 31/593 - 9,10-Secocholestane derivatives, e.g. cholecalciferol, vitamin D3
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 5/16 - Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
G01N 33/543 - ImmunoassayBiospecific binding assayMaterials therefor with an insoluble carrier for immobilising immunochemicals
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
G01N 33/92 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving lipids, e.g. cholesterol
57.
METHODS, COMPOSITIONS, USES, AND KITS USEFUL FOR VITAMIN D DEFICIENCY AND RELATED DISORDERS
Methods for diagnosing, treating, and preventing catabolism-related vitamin D deficiency and related disorders; related compositions, apparatus and kits, are disclosed. A method involves measuring CYP24 expression and/or activity, or a proxy thereof such as FGF23 level, in a patient and correlating abnormally elevated CYP24 expression and/or activity with catabolism- related vitamin D deficiency or with susceptibility for catabolism-related vitamin D deficiency. In response to abnormally elevated CYP24 expression and/or activity, the method further includes administering a CYP24 inhibitor to the vitamin D deficient or at-risk patient, and preferably avoiding activation of the vitamin D binding receptor, such as by avoiding administration of active vitamin D compounds to such patients. Optionally, a vitamin D prohormone or prohormone can be administered.
The invention provides a novel polymorphic form I of crystalline bimatoprost, method for preparation thereof and new crystalline intermediates in the preparation. This form I of crystalline bimatoprost is used in purification of crude bimatoprost and in storage of bimatoprost as active pharmaceutical intermediate. Use of the physical form of bimatoprost in the manufacture of a medicament is also disclosed.
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
C07C 235/34 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
Microfluidic systems including liquid containment regions (1206) and methods associated therewith for performing chemical, biological, or biochemical analyses are provided. Liquid containment regions (1206) of a microfluidic device may include regions that capture one or more liquids flowing in the device, while allowing gases or other fluids in the device to pass through the region. This may be achieved, in some embodiments, by positioning one or more absorbent materials (1208) in the liquid containment region (1206) for absorbing the liquids. This configuration may be useful for removing air bubbles from a stream of fluid and/or for separating hydrophobic liquids from hydrophilic liquids. In certain embodiments, the liquid containment region (1206) prevents any liquid from passing through the region. In some such cases, the liquid containment region may act as a waste area by capturing substantially all of the liquid in the device, thereby preventing any liquid from exiting the device. This arrangement may be useful when the device is used. as a diagnostic tool, as the liquid containment region may prevent a user from being exposed to potentially-harmful fluids in the device.
An ophthalmic shunt implantable in an eye has an elongate body (20) and a conduit (40) for conducting aqueous humor from an anterior chamber of the eye to the suprachoroidal space of the eye. The elongate body has a forward end (22), a spaced back end (24), and an insertion head (26) that extends from- the forward end. The insertion head defines a shearing edge suitable for cutting eye tissue engage thereby. The elongate body can define at least one slot that is configured for operative receipt of a surgical tool such as an obturator. In another aspect, at least a portion of the conduit can be configured for operative receipt of a surgical tool such as an obturator (121).
A61F 9/00 - Methods or devices for treatment of the eyesDevices for putting in contact-lensesDevices to correct squintingApparatus to guide the blindProtective devices for the eyes, carried on the body or in the hand
Fluidic connectors, methods, and devices for performing analyses (e.g., immunoassays) in microfluidic systems are provided. In some embodiments, a fluidic connector having a fluid path is used to connect two independent channels formed in a substrate so as to allow fluid communication between the two independent channels. One or both of the independent channels may be pre-filled with reagents (e.g., antibody solutions, washing buffers and amplification reagents), which can be used to perform the analysis. These reagents may be stored in the channels of the substrate for long periods amounts of time (e.g., 1 year) prior to use. Prior to connection of the fluid connector and the substrate, the fluid path may be filled with a sample (e.g., blood). The sample may be obtained, for example, by pricking a finger of a user until blood is drawn from the finger into the fluid path (e.g., by capillary forces). Upon connection of the fluidic connector and the channels of the substrate, the sample can pass through a reaction area within the first channel of the substrate. This process can allow components of the sample to interact with components disposed in the reaction area. Afterwards, reagents from the second channel can flow to the reaction area via the fluid path, allowing components in the reaction area to be processed (e.g., amplified to produce detectable signal). Components in the reaction area can then be determined using various methods of detection.
Methods and compositions comprising 1,25-dihydroxyvitamin D2 are disclosed. A method for lowering or maintaining lowered serum parathyroid hormone in human patients including administering to said patients an effective amount of 1,25-dihydroxyvitamin D2 to lower or maintain lowered serum parathyroid hormone levels is disclosed. Dosage forms and dosing regimens are also disclosed.
A stable, controlled release formulation for oral dosing of vitamin D compounds is disclosed. The formulation is prepared by incorporating one or more vitamin D compounds into a solid or semi-solid mixture of waxy materials. Oral dosage forms can be prepared by melt-blending the components described herein and filling gelatin capsules with the formulation.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/593 - 9,10-Secocholestane derivatives, e.g. cholecalciferol, vitamin D3
A61K 47/06 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
64.
METHOD OF SAFELY AND EFFECTIVELY TREATING AND PREVENTING SECONDARY HYPERPARATHYROIDISM IN CHRONIC KIDNEY DISEASE
A method of treating and preventing secondary hyperparathyroidism in CKD by increasing or maintaining blood concentrations of both 25-hydroxyvitamin D and 1,25-dihydroxyvitamin D in a patient by administering 25-hydroxyvitamin D3 with or without 25-hydroxyvitamin D2 and, as necessary, 1,25-dihydroxyvitamin D2 as a Vitamin D hormone replacement therapy.
A61K 31/59 - Compounds containing 9,10-seco-cyclopenta[a]hydro- phenanthrene ring systems
65.
TABLET FORMULATIONS CONTAINING 8-[{1-(3,5-BIS-(TRIFLUOROMETHYL)PHENYL)-ETHOXY}-METHYL]-8-PHENYL-1,7-DIAZA-SPIRO[4.5]DECAN-2-ONE SALTS AND TABLETS MADE THEREFROM
Pharmaceutical formulations containing a salt of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I, which are suitable for forming into a tablet dosage form, as well as tablet dosage forms are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.
PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF 8-[{1-(3,5-BIS-(TRIFLUOROMETHYL)PHENYL)-ETHOXY}-METHYL]-8-PHENYL-1,7-DIAZA-SPIRO[4.5]DECAN-2-ONE COMPOUNDS
This application discloses a process to synthesize 8-({1-(3,5-Bis- (trifluoromethyl)phenyl)-ethoxy)-methyl]-8-pheny-1.7-diaza-s.rho.iro[4.5]decan-2-one comprising reacting a compound of the Formula 27a-sulfonate with zinc in the presence of acetic acid.
TABLET FORMULATIONS CONTAINING 8-[{1-(3,5-BIS-(TRIFLUOROMETHYL)PHENYL)-ETHOXY}-METHYL]-8-PHENYL-1,7-DIAZA-SPIRO[4.5]DECAN-2-ONE SALTS AND TABLETS MADE THEREFROM
Pharmaceutical formulations containing a salt of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I, which are suitable for forming into a tablet dosage form, as well as tablet dosage forms are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.
Double-stranded RNA of about 19 to about 25 nucleotides in length capable of regulating gene expression by RNA interference is provided. Such double-stranded RNA are particularly useful for treating disease or conditions associated with a target mRNA or gene. Methods of manufacture and methods of use of the double-stranded RNA are also provided.
A method of treating elevated blood levels of iPTH by increasing or maintaining blood concentrations of both 25 -hydroxy vitamin D and 1, 25-dihydroxyvitamin D in a patient by administering, as necessary, both Vitamin D repletion and Vitamin D hormone replacement therapies, is disclosed. The blood concentrations of 25 -hydroxy vitamin D are increased to and maintained at or above 30 ng/mL, and blood concentrations of 1, 25-dihydroxyvitamin D are increased to or maintained within a patient's normal historical physiological range for 1, 25-dihydroxyvitamin D without causing substantially increased risk of hypercalcemia, hyperphosphatemia or over suppression of plasma iPTH in the patient. The blood levels of 25- hydroxyvitamin D are maintained at or above 30 ng/mL between doses of Vitamin D repletion therapies, and the blood levels of 1, 25-dihydroxyvitamin D are maintained in the patient's normal historical physiological range between doses of Vitamin D hormone replacement therapies. In one aspect, the disclosure includes methods wherein the blood concentration of 25- hydroxyvitamin D during treatment comprises predominantly 25 -hydroxy vitamin D3, and/or wherein the method includes administering predominantly or solely 25-hydroxyvitamin D3 for 25 -hydroxy vitamin D repletion and/or maintenance
A method of treating elevated blood levels of iPTH, secondary hyperparathyroidism, and/or Vitamin D deficiency by increasing or maintaining blood concentrations of both 25-hydroxy vitamin D and 1, 25-dihydroxyvitamin D in a patient by administering, as necessary, both Vitamin D repletion and Vitamin D hormone replacement therapies, is disclosed. The blood concentrations of 25-hydroxy vitamin D are increased to and maintained at or above 30 ng/mL, and blood concentrations of 1, 25-dihydroxyvitamin D are increased to or maintained within a patient's normal historical physiological range for 1, 25-dihydroxyvitamin D without causing substantially increased risk of hypercalcemia, hyperphosphatemia or over suppression of plasma iPTH in the patient. The blood levels of 25-hydroxyvitamin D are maintained at or above 30 ng/mL between doses of Vitamin D repletion therapies, and the blood levels of 1, 25-dihydroxyvitamin D are maintained in the patient's normal historical physiological range between doses of Vitamin D hormone replacement therapies. In one aspect, the disclosure includes methods wherein the blood concentration of 25-hydroxyvitamin D during treatment comprises predominantly 25-hydroxy vitamin D3, and/or wherein the method includes administering predominantly or solely 25-hydroxyvitamin D3 for 25-hydroxy vitamin D repletion and/or maintenance.
A61K 31/59 - Compounds containing 9,10-seco-cyclopenta[a]hydro- phenanthrene ring systems
A61P 5/20 - Drugs for disorders of the endocrine system of the parathyroid hormones for decreasing, blocking or antagonising the activity of PTH
71.
Pharmaceutical formulations: salts of 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one and treatment methods using the same
Pharmaceutical formulations containing salts of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl]-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro [4.5]decan-2-one, represented by Formula I, are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.
HYDROCHLORIDE SALTS OF 8-[{1-(3,5-BIS-(TRIFLUOROMETHYL)PHENYL)-ETHOXY}-METHYL]-8-PHENYL-1,7-DIAZA-SPIRO[4.5]DECAN-2-ONE AND PREPARATION PROCESS THEREFOR
Disclosed are hydrochloride and tosylate crystalline salt forms of (5S,8S)-8- [{(1R)-1 -(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7- diazaspiro[4.5]decan-2-one, represented by Formula I and methods of preparing the same.
A61K 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61P 1/08 - Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigoAntiemetics
73.
Hydrochloride salts of 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy)-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one and preparation process therefor
Disclosed are hydrochloride and tosylate crystalline salt forms of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I and methods of preparing the same.
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
C07D 215/00 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
C07D 217/00 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
C07D 219/00 - Heterocyclic compounds containing acridine or hydrogenated acridine ring systems
C07D 221/00 - Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups
74.
PHARMACEUTICAL FORMULATIONS: SALTS OF 8-[{1-(3,5-BIS-(TRIFLUOROMETHYL)PHENYL)-ETHOXY}-METHYL]-8-PHENYL-1,7-DIAZA-SPIRO[4.5]DECAN-2-ONE AND TREATMENT METHODS USING THE SAME
Pharmaceutical formulations containing salts of (5S,8S)-8-[{(1R)-1- (3,5-Bis- trifluoromethyl)phenyl]-ethoxy}-methyl]-8-phenyl-1,7- diazaspiro[4.5]decan-2- one, represented by Formula I, are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.
A61K 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
Methods and compositions for treating 25-hydiOxyvitamin D insufficiency and deficiency in a patient are described herein. The method includes orally administering to the patient a delayed, sustained release formulation including a first ingredient selected from the group consisting of 25-hydroxyvitamin D2, 25-hydroxyvitamin D3, or a combination of 25-hydroxyvitamin D2 and 25-hydroxyvitamin D3, or it inchides gradually administering to the patient an sterile intravenous formulation including a first ingredient selected from the group consisting of 25-hydroxyvitamin D2, 25- hydroxyvitamin D3, or a combination of 25-hydroxyvitamin D2 and 25-hydroxyvitamin D3.
A controlled-release pha&pgr;naceutical formulation including cholecalciferol and/or ergocalciferol, a method of making the formulation, and a method of administering the formulation to treat 25-hydroxyvitamin D insufficiency or deficiency, are disclosed. The composition and method of administration preferably result in delayed release of the • vitamin(s) in the ileum of the small intestine and sustained, substantially constant, release of the vitamin(s) over an extended period, e.g., at least 4 hours or more. Individual and combined dosages of 500 IU to 50,000 IU per dosage form, preferably daily, are disclosed. The compositions and methods are contemplated to exhibit one or more advantages including, but not limited to efficiency of vitamin D repletion and maintenance; mitigation or avoidance of first pass effects of the Vitamin D compounds on the duodenum; mitigation or avoidance of adverse supraphysiological surges in intralumenal, intracellular and blood levels of cholecalciferol, ergocalciferol and 25- hydroxyvitamin D and their consequences; and mitigation or avoidance of serious side effects associated with Vitamin D supplementation, namely Vitamin D toxicity.
A compound having the general structure shown in Formula I:
1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
C07D 215/12 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
C07D 215/16 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 213/02 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
C07D 211/02 - Preparation by ring-closure or hydrogenation
C07D 405/00 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
