Patents Assigned to King Pharmaceuticals Research and Development, Inc.
-
Publication number: 20130136693Abstract: The present invention provides novel crystalline polymorphic forms of 2-cyclohexylmethylidenehydrazino adenosine, also known as binodenoson, methods of making the same, and methods for the manufacture of a pharmaceutical composition by employing such crystal forms, in particular, for the use of binodenoson in a subject, in need thereof, as a pharmacological stress agent to produce coronary vasodilation.Type: ApplicationFiled: July 11, 2012Publication date: May 30, 2013Applicant: King Pharmaceuticals Research and Development, IncInventors: Allan R. Moorman, Michael H. O'Neal
-
Patent number: 7897596Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.Type: GrantFiled: November 12, 2007Date of Patent: March 1, 2011Assignee: King Pharmaceuticals Research & Development, Inc.Inventors: Pier Giovanni Baraldi, Allan R. Moorman, Romeo Romagnoli
-
Patent number: 7855209Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.Type: GrantFiled: November 12, 2007Date of Patent: December 21, 2010Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Allan R. Moorman, Romeo Romagnoli
-
Patent number: 7767685Abstract: The present invention provides compounds of the formula which are adenosine A2B receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2B receptor activity. Such conditions include, but are not limited to, chronic and acute inflammatory diseases involving degranulation of mast cells, e.g., asthma, allergic rhinitis and allergic dermatitis; impaired sensitivity to insulin, e.g., type 2 diabetes, pre-diabetic state, and impaired glucose tolerance; diseases in which angiogenesis is a key component of pathogenesis, e.g., solid tumors and angiogenic retinopathies; apnea of preterm infants; myocardial reperfusion injury; inflammatory bowel disease; autoimmune diseases, such as rheumatoid arthritis, multiple sclerosis, and lupus erythematosis; diseases involving microvascular abnormalities of the retina that are mediated by adenosine A2B receptors, e.g.Type: GrantFiled: June 25, 2007Date of Patent: August 3, 2010Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Allan Moorman, Mojgan Aghazadeh Tabrizi
-
Patent number: 7723343Abstract: The present invention provides compounds of the formula wherein R1 and R2 have meaning as defined herein in the specification. The compounds of formula (I) are adenosine A2A receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2A receptor activity. Such conditions include, but are not limited to, diseases of the central nervous system such as depression, cognitive function diseases and neurodegenerative diseases such as Parkinson's disease, senile dementia as in Alzheimer's disease or psychoses and stroke. The compounds of the present invention may also be employed for the treatment of attention related disorders such as attention deficit disorder (ADD) and attention deficit hyperactivity disorder (ADHD), extra pyramidal syndrome, e.g.Type: GrantFiled: March 27, 2008Date of Patent: May 25, 2010Assignee: King Pharmaceuticals Research and Development, Inc.Inventor: Allan R. Moorman
-
Patent number: 7714006Abstract: A method of increasing the bioavailability, and decreasing the effect of age on the bioavailability, of metaxalone, by administration of an oral dosage form with food is provided, as well as an article of manufacture comprising an oral dosage form of metaxalone in a suitable container and associated with printed labeling which describes the increased bioavailability, and decreased effect of age on bioavailability, of the medication in the container, when taken with food.Type: GrantFiled: July 15, 2005Date of Patent: May 11, 2010Assignee: King Pharmaceuticals Research & Development, Inc.Inventors: Michael C. Scaife, Charles C. Davis
-
Patent number: 7691825Abstract: The present invention provides compounds of the formula wherein R1, R2, R3 and n have meaning as described in the specification, methods for their preparation, and pharmaceutical compositions containing them. The compounds of formula (I) are adenosine A2B receptor agonists and, thus, may be employed for the treatment of diseases in mammals that are mediated by the A2B receptor including, but not limited to, septic shock, cystic fibrosis, impotence, diarrhea, and cardiac diseases. Cardiac diseases include hyperplasia consequent to hypertension, arteriosclerosis, and heart attack. The present invention also provides methods for the induction of pharmacological stress to facilitate coronary imaging of areas of ischemia by employing compounds of formula (I). The compounds of formula (I) may be labeled, e.g., with radioactive isotopes, and therefore are useful in kinetic binding experiments.Type: GrantFiled: June 4, 2007Date of Patent: April 6, 2010Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Allan R. Moorman, Delia Preti
-
Patent number: 7691869Abstract: The present invention provides compounds of the formula wherein R1 and R2 have meaning as defined herein in the specification. The compounds of formula (I) are adenosine A2A receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2A receptor activity. Such conditions include, but are not limited to, diseases of the central nervous system such as depression, cognitive function diseases and neurodegenerative diseases such as Parkinson's disease, senile dementia as in Alzheimer's disease or psychoses and stroke. The compounds of the present invention may also be employed for the treatment of attention related disorders such as attention deficit disorder (ADD) and attention deficit hyperactivity disorder (ADHD), extra pyramidal syndrome, e.g.Type: GrantFiled: March 27, 2008Date of Patent: April 6, 2010Assignee: King Pharmaceuticals Research and Development, Inc.Inventor: Allan R. Moorman
-
Patent number: 7511133Abstract: The compounds of the following formula: wherein Ar, R and R1 have the meanings given in the specification. This series of sulfonamido derivatives with a conserved uronamide group at the 5? position provide superior A3 receptor affinity as well as selectivity. These new adenosine agonists are sulfonamido derivatives N-substituted with aliphatic groups (cyclic or linear) or aromatic radicals.Type: GrantFiled: September 17, 2004Date of Patent: March 31, 2009Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Allan R. Moorman, Pier A. Borea
-
Patent number: 7470698Abstract: The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A3 receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A3 receptor. The compounds can be labeled, for example with fluorescent or radiolabels, and the labels used in vivo or in vitro to determine the presence of tumor cells which possess a high concentration of adenosine A3 receptors.Type: GrantFiled: July 9, 2007Date of Patent: December 30, 2008Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea
-
Patent number: 7449490Abstract: New fused thiophene compounds are provided and methods of using those compounds for a variety of therapeutic indications. Compounds of the invention are particularly useful for treatment of neuropathic pain.Type: GrantFiled: April 11, 2006Date of Patent: November 11, 2008Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Allan R. Moorman, Romeo Romagnoli, Pier Giovanni Baraldi
-
Patent number: 7435740Abstract: A class of novel antagonists for the adenosine A3 receptor are disclosed. These compounds are useful as therapeutic agents for a number of diseases and medical conditions that are mediated by the A3 receptor. The compounds of this invention are also useful as diagnostic agents for the A3 receptor.Type: GrantFiled: January 31, 2006Date of Patent: October 14, 2008Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Delia Preti, Mojgan Aghazadeh Tabrizi
-
Patent number: 7342003Abstract: Provided is a method for the synthesis of an aralkyloxyadenosine or an alkoxyadenosine. The method includes protecting the hydroxyl sugar groups with a protecting group to produce a protected halogenated adenosine. The protected halogenated adenosine is alkoxylated, and the hydroxyl sugar groups of the protected halogenated adenosine are deprotected to provide the aralkyloxyadenosine or alkoxyadenosine.Type: GrantFiled: June 16, 2005Date of Patent: March 11, 2008Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Allan R. Moorman, Michael Scannell, Thiagarajan Balasubramanian, Russell Outcalt, Edward Leung
-
Patent number: 7335655Abstract: The present invention relates generally to compounds of formula (I): wherein X is a five or six-membered heteroaromatic ring, containing one to four heteroatoms, selected from nitrogen, oxygen, or sulfur, provided that at least one heteroatom is nitrogen; and G1 and G2 are independently CH or N. The present invention also relates to the preparation of the compounds, pharmaceutical formulations thereof, and their use in medicine as potent or selective A2B adenosine receptor antagonists and their uses for treating asthma, autoimmune diseases and retinal vascular diseases.Type: GrantFiled: February 22, 2006Date of Patent: February 26, 2008Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Pier A. Borea
-
Patent number: 7271171Abstract: The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A3 receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A3 receptor. The compounds can be labeled, for example with fluorescent or radiolabels, and the labels used in vivo or in vitro to determine the presence of tumor cells which possess a high concentration of adenosine A3 receptors.Type: GrantFiled: June 27, 2005Date of Patent: September 18, 2007Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea
-
Patent number: 7205403Abstract: The present invention relates generally to compounds of the formula (I): wherein: X is a five or six-membered heteroaromatic ring, containing one to four heteroatoms, selected from nitrogen, oxygen, or sulfur, provided that at least one heteroatom is nitrogen; and G1 and G2 are independently CH or N. The present invention also relates to the preparation of the compounds, pharmaceutical formulations thereof, and their use in medicine as potent or selective A2B adenosine receptor antagonists and their uses for treating asthma, autoimmune diseases and retinal vascular diseases.Type: GrantFiled: February 3, 2003Date of Patent: April 17, 2007Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Pier A. Borea
-
Patent number: 7112607Abstract: The present invention relates to compounds of formula (IA): the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including protection against hypoxia and ischemia induced injury and treatment of adenosine-sensitive cardiac arrhythmias.Type: GrantFiled: March 20, 2002Date of Patent: September 26, 2006Assignee: King Pharmaceuticals Research & Development, Inc.Inventor: Pier Giovanni Baraldi
-
Patent number: 7101905Abstract: New fused thiophene compounds are provided and methods of using those compounds for a variety of therapeutic indications. Compounds of the invention are particularly useful for treatment of neuropathic pain.Type: GrantFiled: March 29, 2002Date of Patent: September 5, 2006Assignee: King Pharmaceuticals Research & Development, Inc.Inventors: Allan R. Moorman, Romeo Romagnoli, Pier Giovanni Baraldi
-
Patent number: 7094895Abstract: The present invention relates to compounds of the formula wherein R1 and R2 are independently hydrogen, C1–C4 alkyl, C1–C4 substituted alkyl, C1–C4 alkoxy, C1–C4 substituted alkoxy, C1–C4 acyl, halogen, cyano, nitro, amino, alkylamino, or dialkylamino; R3, R4, R5, R6, R7, and R8 are independently CH or nitrogen; R9 is hydrogen or methyl; R10 is C?O or (CH2)n; where n is 0, 1, 2, 3, or 4; R11 and R12 are independently nitrogen or CH; X1 and X2 are independently hydrogen, deuterium, tritium or halogen; and X3 is N; and their pharmaceutically acceptable salts; compositions thereof. Methods of preparing the compounds are also described. The compounds are useful in the treatment of diseases in mammals that are mediated by the action of the P2X7 receptor.Type: GrantFiled: December 23, 2002Date of Patent: August 22, 2006Assignee: King Pharmaceuticals Research & Development, Inc.Inventors: Pier Giovanni Baraldi, Pier A. Borea
-
Patent number: 7067148Abstract: A pharmaceutical composition with ?-sheet microcrystalline cellulose with improved potency life and methods of preparation therefor. Improved thyroid hormone pharmaceutical compositions comprising 50 weight % or more of ?-sheet microcrystalline cellulose.Type: GrantFiled: February 15, 2002Date of Patent: June 27, 2006Assignee: King Pharmaceutical Research & Development, Inc.Inventors: G. Andrew Franz, Elaine A. Strauss, Philip A. DiMenna, Rocco L. Gemma