Abstract: Methods and compositions of tricyclic antidepressants for inducing local long-lasting anesthesia and analgesia are provided. The methods and compositions are useful for alleviating acute and chronic pain, particularly useful for treating a localized pain.
Abstract: The present invention provides substituted 11-phenyl-dibenzazepine compounds that are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.
Type:
Grant
Filed:
September 22, 2000
Date of Patent:
March 18, 2003
Assignees:
Nuchem Pharmaceuticals, Inc., Children's Medical Center Corporation, Presidents and Fellows of Harvard College
Inventors:
Carlo Brugnara, Jose Halperin, Rudolf Fluckiger, Emile M. Bellott, Jr., Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft, Michael H. Zeldin
Abstract: The present invention relates to the use of a particular class of chemical compounds as modulators of SKCa, IKCa and BKCa channels, and to pharmaceutical compositions comprising the SK/IK/BK channel modulating agents.
Type:
Grant
Filed:
October 25, 2001
Date of Patent:
February 25, 2003
Assignee:
NeuroSearch A/S
Inventors:
Bo Skaaning Jensen, Lene Teuber, Dorte Strobaek, Palle Christophersen, Soren Peter Olesen
Abstract: The present invention relates to the delivery of antipsychotics through an inhalation route. Specifically, it relates to aerosols containing antipsychotics that are used in inhalation therapy. In a composition aspect of the present invention, the aerosol comprises particles comprising at least 5 percent by weight of an antipsychotic. In a method aspect of the present invention, an antipsychotic is delivered to a mammal through an inhalation route. The method comprises: a) heating a composition, wherein the composition comprises at least 5 percent by weight of an antipsychotic, to form a vapor; and, b) allowing the vapor to cool, thereby forming a condensation aerosol comprising particles, which is inhaled by the mammal.
Type:
Application
Filed:
May 20, 2002
Publication date:
January 23, 2003
Inventors:
Joshua D. Rabinowitz, Alejandro C. Zaffaroni
Abstract: Compounds of the formula (I) in which R1 is C1-10 allyl; C2-10 alkenyl; C2-10 alkynyl; phenyl-C2-10 alkyl or phenyl-C2-10 alkenyl; and salts and esters thereof, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous system
Type:
Grant
Filed:
November 16, 2001
Date of Patent:
January 7, 2003
Assignee:
Eli Lilly and Company
Inventors:
Ivan Collado Cano, Concepcion Pedregal Tercero, Alicia Marcos Llorente
Abstract: The present invention provides for new crystal forms of oxcarbazepine, more particularly oxcarbazepine Forms B, C, D and E. The present invention further provides processes for preparation of these forms. Form B is prepared by evaporating the solvents from a solution of oxcarbazepine in toluene and dichloromethane. Form B is also obtained by immediately cooling the solution of oxcarbazepine and toluene. Cooling the same solution at a slower rate, but still fairly rapidly, results in oxcarbazepine Form C. Cooling the same solution at even a slower rate results in another Form, oxcarbazepine Form D. Oxcarbazepine Form E, a solvate of chloroform, is obtained by precipitating a solution of oxcarbazepine and chloroform. The present invention also provides processes for converting one of the newly discovered crystal forms of oxcarbazepine into another crystal form, including Form A, which is in the prior art.
Type:
Application
Filed:
February 12, 2002
Publication date:
January 2, 2003
Inventors:
Judith Aronhime, Ben-Zion Dolitzky, Yana Berkovich, Nissim Garti
Abstract: The present invention provides a composition for neurotrophic action which comprises a compound of the formula:
wherein
Ar is an optionally condensed phenyl group which may be substituted;
n is an integer of 1 to 10;
R is a hydrogen atom or a hydrocarbon group which may be substituted; and
Y is an amino group which may be substituted or a nitrogen-containing saturated heterocyclic group which may be substituted; or a salt thereof,
which compounds are useful for preventing and/or treating (1) neurodegenerative diseases (e.g. senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, Creutzfelt-Jakob disease, amyotrophic lateral sclerosis, diabetic neuropathy, etc.), (2) neuropathy in cerebrovascular diseases (e.g. impairment of cerebral blood flow based on cerebral infarction, cerebral hemorrhage, cerebral sclerosis, etc.), brain trauma, spinal cord injury, cerebritis sequela and cerebral palsy, (4) mental diseases (e.g.
Type:
Grant
Filed:
October 10, 2000
Date of Patent:
December 31, 2002
Assignee:
Takeda Chemical Industries, Ltd.
Inventors:
Masaomi Miyamoto, Koki Kato, Yuji Ishihara
Abstract: A therapeutic formulation comprises a topically acceptable semisolid vehicle and carbamazepine, the vehicle consisting of components that are compatible with the carbamazepine, and the carbamazepine being in a concentration sufficient to permit a therapeutically effective amount of the carbamazepine to be absorbed from the formulation into the skin of a patient. The vehicle may be a cream, ointment, or gel. A method of treating a skin condition of a patient such as psoriasis comprises applying carbamazepine topically to the patient's skin until the condition improves. A method of administering carbamazepine to a patient comprises applying a formulation comprising carbamazepine topically to the patient's skin.
Abstract: This invention relates to proliposomal drug-delivery systems for medicaments. In particular, it relates to enteric-coated proliposomal formulations for poorly water soluble drugs and methods for making the same. The drug delivery system comprises a pharmaceutical agent, a phospholipid and a coating material. The present invention provides enhanced stability and bioavailability for pharmaceutical formulations.
Abstract: This invention relates to a method of inhibiting tumor cell adhesion, pain, and inflammation at a wound during a surgical procedure by delivering an irrigation solution containing a tumor cell anti-adhesion agent and a plurality of additional agents to an operative site during the surgical procedure. In addition, methods of inhibiting tumor cell attachment and implantation during a surgical procedure as well as inhibiting tumor metastasis during a surgical procedure are also provided.
Type:
Grant
Filed:
September 11, 2000
Date of Patent:
December 10, 2002
Assignee:
Omeros Corporation
Inventors:
Gregory A. Demopulos, Pamela Pierce-Palmer, Jeffrey M. Herz, Darrell L. Tanelian
Abstract: A therapeutic formulation comprises a topically acceptable semisolid vehicle and carbamazepine, the vehicle consisting of components that are compatible with the carbamazepine, and the carbamazepine being in a concentration sufficient to permit a therapeutically effective amount of the carbamazepine to be absorbed from the formulation into the skin of a patient. The vehicle may be a cream, ointment, or gel. A method of treating a skin condition of a patient such as psoriasis comprises applying carbamazepine topically to the patient's skin until the condition improves. A method of administering carbamazepine to a patient comprises applying a formulation comprising carbamazepine topically to the patient's skin.
Abstract: A process for preparing amorphous paroxetine hydrochloride or sertraline hydrochloride is provided, which comprises preparing a solution in which paroxetine hydrochloride or sertraline hydrochloride and a water-soluble polymer are dissolved in a co-solvent of a volatile organic solvent and water. Said solution is dried to obtain a composition comprising amorphous paroxetine hydrochloride or sertraline hydrochloride and the water-soluble matrix.
Abstract: Gamma aminobutyric acid (GABA) is a potent inhibitory neurotransmitter that binds to hetero-oligomeric receptors in the mammalian brain. In a previous study, we documented specific GABA binding to isolated rat hepatocytes which resulted in inhibition of hepatocyte proliferation. The purpose of the present study was to define the nature of hepatic GABAA receptors and document their expression during rapid liver growth (post-partial hepatectomy). Polymerase chain reactions (PCR) with gene-specific primers derived from published sequences were performed with marathon-ready human and rat liver cDNA. Two GABAA receptor subunit types (&bgr;3 and &egr;) were expressed in the human liver and one (&bgr;3) in the rat liver. PCR amplification of the human GABAA receptor &bgr;3 subunit produced a single product (m.w. 53-59 kDa). In the case of the &egr; subunit, two PCR products were identified.
Abstract: The present invention provides a pyrrolidine compound of the formula (I)
wherein each symbol is as defined in the specification, an optically active compound thereof and a pharmaceutically acceptable salt thereof. The present invention further provides a pharmaceutical composition containing a compound of the formula (I), an optically active compound thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable additive. The compound of the present invention has a serotonin 2 receptor antagonistic action along with a platelet aggregation suppressive action, a peripheral circulation improving action and a lacrimation promoting action. Therefore, the compound of the present invention can be a useful medicine showing effect against thrombotic embolism, dry eye and the like.
Abstract: This invention relates to a composition and method for alleviating neuropathic pain and/or its symptoms. The composition comprises (1) a compound that inhibits the reuptake of both norepinephrine and dopamine or inhibits the reuptake of norepinephrine alone in combination with (2) a compound that acts as a sodium channel blocker. The method involves the administration of the composition in an effective amount to alleviate neuropathic pain and/or its symptoms.
Type:
Application
Filed:
April 3, 2002
Publication date:
October 10, 2002
Inventors:
Steven Noel Quessy, George David Rudd, Michael Fredrik Winnem
Abstract: Medicaments comprising a compound represented by the following formulas:
wherein, R1 represents hydrogen atom or a C1-6 alkyl group; R2 and R3 represent hydrogen atom or a C1-6 alkyl group, or R2 and R3 may combine together with the carbon atoms of the phenyl ring to which R2 and R3 bind to represent a 5- or 6-membered ring; R4 represents hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxyl group etc.; R5 represents hydrogen atom, a C1-6 alkyl group, or an aryl-substituted C1-6 alkyl group; R6 represents hydrogen atom or a C1-6 alkyl group; X represents —NR7—, —NO—, —O— etc. in which R7 represents hydrogen atom, a C1-6 alkyl group etc.; and Y represents a phenylene group or a pyridinediyl group, which are useful for preventive and therapeutic treatments of diabetes and complications of diabetes.
Type:
Grant
Filed:
September 1, 2000
Date of Patent:
October 1, 2002
Assignee:
Institute of Medicinal Molecular Design, Inc.
Abstract: The invention is concerned with a parenteral formulation comprising a 5H-dibenz(b,f)azepine-5-carboxamide and an aqueous-based solvent. The parenteral formulation is useful in the treatment of seizures resulting from, e.g. epileptic attack.
Abstract: A method of treating pain by the co-administration of an antidepressant together with one or more precursors or inducers of neurotransmitters, particularly amino acids selected from L-phenylalanine, L-tyrosine, L-tryptophan and L-DOPA.
Type:
Grant
Filed:
January 4, 2000
Date of Patent:
September 17, 2002
Assignee:
The WWK Trust of 225-235 High Street
Inventors:
David Frederick Horrobin, Cari Loder, Graham Cooper
Abstract: A method of treatment of disorders of neurological origin and drug formulations for use in the method are disclosed. These conditions comprise fatigue and associated syndromes of pain, weakness and depressed mood which are associated with chronic fatigue syndrome, brain injury and stroke, stress, fibromyalgia, and irritable bowel syndrome. The treatment comprises administering to a patient in need thereof a selective inhibitor of noradrenaline reuptake combined with either phenylalanine or tyrosine in the same dosage form or the same pack.#
The noradrenergic drug may be selected from lofepramine, desipramine or reboxetine. The selective inhibitor may be a combined inhibitor of both noradrenaline and serotonin reuptake such as venlafaxine, duloxetine or milnacipran, or an inhibitor of both noradrenaline and dopamine reuptake such as bupropion.
Abstract: Methods and compositions of tricyclic antidepressants for inducing local long-lasting anesthesia and analgesia are provided. The methods and compositions are useful for alleviating acute and chronic pain, particularly useful for treating a localized pain.
Abstract: Compounds, compositions, and methods for treating multidrug resistance are disclosed. Suitable compounds are 2-substituted heterocyclic compounds.
Type:
Application
Filed:
December 19, 2000
Publication date:
July 11, 2002
Inventors:
Charles Raymond Degenhardt, David Joseph Eickhoff
Abstract: This invention relates to pharmaceutical compositions comprising combinations of a GABA agonist, a prodrug thereof or a pharmaceutically acceptable salt of said GABA agonist or said prodrug and a SDI, a prodrug thereof or a pharmaceutically acceptable salt of said SDI or said prodrug, kits containing such combinations and methods of using such combinations to treat mammals, including humans, suffering from diabetic complications such as diabetic neuropathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic retinopathy, diabetic microangiopathy, diabetic macroangiopathy, cataracts or foot ulcers.
Abstract: The present invention relates to methods and compositions for treating selected conditions of the central and peripheral nervous systems employing non-synaptic mechanisms. More specifically, one aspect of the present invention relates to methods and materials for treating seizure and seizure disorders, epilepsy, status epilepticus, migraine, spreading depression, intracranial hypertension; for treating the pathophysiological effects of head trauma, stroke, ischemia and hypoxia; for treating or protecting from the pathophysiological effects of neurotoxic agents such as ethanol; and for treating neurophsyciatric disorders and central nervous system edema by administering agents that modulate ionic concentrations and/or ionic gradients in the brain, particularly ion-dependent or cation-chloride cotransporter antagonists. Electrolyte cotransport antagonists and combinations of such compositions with other agents for treating various conditions are disclosed.
Abstract: A method for treating obsessive-compulsive disorders, somatoform disorders, dissociative disorders, eating disorders, impulse control disorders, and autism is disclosed. These disorders are treated by administering an effective amount of a D1/D5 antagonist.
Abstract: This invention relates to pharmaceutical compositions comprising combinations of a GABA agonist, a prodrug thereof or a pharmaceutically acceptable salt of said GABA agonist or said prodrug and an ARI, a prodrug thereof or a pharmaceutically acceptable salt of said ARI or said prodrug, kits containing such combinations and methods of using such combinations to treat mammals, including humans, suffering from diabetic complications such as diabetic neuropathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic retinopathy, diabetic microangiopathy, diabetic macroangiopathy, cataracts or foot ulcers.
Abstract: Norepinephrine uptake 2 inhibitors (or their precursors) are administered to enhance the effect of norepinephrine reuptake inhibitors and other antidepressants. The uptake 2 inhibitor may be combined in a single medication with a norepinephrine reuptake inhibitor, such as imipramine, desipramine, or reboxetine, in order to inhibit both uptake mechanisms. The norepinephrine uptake 2 inhibitors may also be combined with MAO inhibitors or with selective serotonin reuptake inhibitors. Alternatively, the norepinephrine uptake 2 inhibitors may be useful antidepressants in their own right, without the need for co-administration of other antidepressants.
Type:
Grant
Filed:
March 16, 2001
Date of Patent:
June 11, 2002
Assignee:
President and Fellows of Harvard College
Abstract: The present invention relates to the use of a particular class of chemical compounds as modulators of SKCa, IKCa and BKCa channels, and to pharmaceutical compositions comprising the SK/IK/BK channel modulating agents.
Type:
Application
Filed:
October 25, 2001
Publication date:
May 30, 2002
Inventors:
Bo Skaaning Jensen, Lene Teuber, Dorte Strobaek, Palle Christophersen, Soren Peter Olesen
Abstract: A method of treating Alzheimer's disease is disclosed, not just with palliatives, but in a manner that prevents the progressive degeneration caused by Alzheimer's disease. Certain types of “safener” drugs, which can reduce the neurotoxic damage caused by a potent NMDA antagonist drug such as dizocilpine maleate (also known as MK-801) can also retard the type of corticolimbic damage which, in the brain of a patient who suffers from Alzheimer's disease, results from over-excitation of corticolimbic neurons. This over-excitation is caused or aggravated by NMDA receptor dysfunction in neuronal circuits which normally limit and control excitatory neurotransmitter release within those corticolimbic regions. Safener drugs include various known drugs that can suppress activity at muscarinic acetylcholine receptors, sigma receptors, kainic acid receptors, or AMPA receptors. They also include various drugs which can stimulate activity at alpha-2 adrenergic or 5HT-2A serotonin receptors.
Abstract: A method of treating an obsessive-compulsive spectrum disorder comprises the step of administering an effective amount of tramadol to an individual.
Type:
Grant
Filed:
March 24, 2000
Date of Patent:
May 14, 2002
Assignee:
University of Cincinnati
Inventors:
Nathan A. Shapira, Toby D. Goldsmith, Paul E. Keck, Jr.
Abstract: This invention is concerned with a parenteral formulation comprising a 5H-dibenz(b,f)azepine-5-carboxamide and an aqueous-based solvent. The parenteral formulation is useful in the treatment of seizures resulting from, e.g. epileptic attack.
Abstract: Compounds of the formula (I) are disclosed which are dual fibrinogen receptor and vitronectin receptor antagonists and are useful in the treatment of atherosclerosis, in the prevention of restenosis and in the prevention of tumor metastasis and tumor growth: 1
Abstract: Benzoazepines of the following formula
wherein R1, R1a, R2, R9k, L, Q, X, Y and Z are as described herein, and analogs thereof are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.
Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
February 3, 1999
Date of Patent:
June 4, 2002
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler