Abstract: Methods of reversing local anesthesia are disclosed. The methods comprise administering a local anesthetic and alpha adrenergic receptor agonist to induce local anesthesia followed by reversing anesthesia with a low dose of an alpha adrenergic receptor antagonist. Also disclosed are kits comprising a local anesthetic, an alpha adrenergic receptor agonist and a low dose of an alpha adrenergic receptor antagonist.
Abstract: This invention relates to novel 3-substituted quinuclidine derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters.
Type:
Application
Filed:
May 9, 2003
Publication date:
March 4, 2004
Inventors:
Dan Peters, Gunnar M. Olsen, Elsebet Ostergaard Nielsen, Philip K. Ahring, Tino Dyhring Jorgensen
Abstract: This invention relates to the use of a CYP2D6 inhibitor in combination with a drug having CYP2D6 catalyzed metabolism, wherein the drug and the CYP2D6 inhibitor are not the same compound; and pharmaceutical compositions for said use.
Abstract: The present invention discloses novel cholinergic receptor ligands. The present invention also relates to the synthesis of substituted derivatives of aza-bridged bicyclic amines for use as muscarinic receptor ligands as well as methods of regulating function of certain cholinergic receptors, and hence acting as antagonists, agonists and partial agonists at certain specific cholinergic receptor subtypes. The present invention also relates to methods for treating disorders associated with cholinergic receptors.
Type:
Application
Filed:
August 6, 2002
Publication date:
February 12, 2004
Inventors:
Harold Kohn, T. Kendall Harden, Myoung Goo Kim, Erik Bodor
Abstract: The present invention relates to bicylic derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
Abstract: This invention relates to the use of a CYP2D6 inhibitor in combination with a drug having CYP2D6 catalyzed metabolism, wherein the drug and the CYP2D6 inhibitor are not the same compound; and pharmaceutical compositions for said use.
Abstract: Compounds of the general formula I
wherein A represents:
D represents oxygen, or sulfur and R1, R2 and R3 are as defined in the specification, enantiomers thereof, pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders.
Type:
Grant
Filed:
May 17, 2002
Date of Patent:
January 27, 2004
Assignee:
Astrazeneca AB
Inventors:
Michael Balestra, George Mullen, Eifion Phillips, Richard Schmiesing
Abstract: The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C1-4 alkyl. The substituent at the 3-position of the 1-azabicycloalkane is a carbonyl group-containing moiety, such as an amide, carbamate, urea, thioamide, thiocarbamate, thiourea or similar functionality. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the &agr;7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission.
Type:
Application
Filed:
February 21, 2003
Publication date:
January 1, 2004
Inventors:
Anatoly A. Mazurov, Jozef Klucik, Lan Miao, Angela S. Seamans, Teresa Youngpeter Phillips, Jeffrey Daniel Schmitt, Craig Harrison Miller
Abstract: The invention provides compounds of Formula I: 1
Type:
Application
Filed:
February 14, 2003
Publication date:
December 25, 2003
Inventors:
Eric Jon Jacobsen, Jason K. Myers, Daniel Patrick Walker, Donn G. Wishka, Steven Charles Reitz, David W. Piotrowski, Brad A. Acker, Vincent E. Groppi
Abstract: The present invention relates to bicylic derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
Abstract: A diversity of inflammatory diseases can be treated via local delivery to the patient of a composition containing a therapeutically effective amount of an anti-malarial agent. In a preferred embodiment of the method of the invention, a pulmonary inflammatory condition, such as asthma, is treated by inhalation of an aerosolized anti-malarial agent, such as hydroxychloroquine.
Abstract: The invention relates to a combination of a nicotinamide derivative and tiotropium or a derivative thereof, compositions containing it and the uses of, such a combination. The combination according to the present invention is useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
Type:
Application
Filed:
February 6, 2003
Publication date:
November 27, 2003
Inventors:
Simon Bailey, Elisabeth C. L. Gautier, Alan J. Henderson, Thomas V. Magee, Anthony Marfat, John P. Mathias, Dale G. McLeod, Sandra M. Monaghan, Blanda L. C. Stammen
Abstract: The present invention provides methods for purifying, identifying and using optically active isomers of quinine and quinidine as well as compositions comprising such optically active isomers. Such optically active isomers having desired actions on cardiac sodium and potassium channel function substantially separable from undesirable effects on GI motility can be useful for more effective therapy of cardiac arrhythmias. Also disclosed are methods for assaying the levels of such isomers present in the biological fluids.
Abstract: The invention provides compounds of Formula I:
Type:
Application
Filed:
November 6, 2002
Publication date:
November 6, 2003
Inventors:
David W. Piotrowski, Jason K. Myers, Bruce N. Rogers, Eric Jon Jacobsen, Alice L. Bodnar, Vincent E. Groppi, Daniel Patrick Walker, Brad A. Acker
Abstract: Compounds of formula I
wherein A represents:
and R, R1, R2, R3 and R4 are as defined in the specification, pharmaceutically-cceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders.
Abstract: The invention describes novel nitric oxide donors and novel compositions comprising at least one nitric oxide donor. The invention also provides novel compositions comprising at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for treating cardiovascular diseases, for the inhibition of platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device, for treating pathological conditions resulting from abnormal cell proliferation; transplantation rejections, autoimmune, inflammatory, proliferative, hyperproliferative, vascular diseases; for reducing scar tissue or for inhibiting wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis by administering the nitric oxide donor optionally in combination with at least one therapeutic agent.
Type:
Application
Filed:
April 7, 2003
Publication date:
October 30, 2003
Inventors:
Xinqin Fang, David S. Garvey, Ricky D. Gaston, Chia-En Lin, Ramani R. Ranatunga, Stewart K. Richardson, Tiansheng Wang, Weiheng Wang, Shiow-Jyi Wey
Abstract: The present invention relates to novel fluoroalkoxybenzylamino derivatives of nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula 1
Abstract: Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia) are treated by administering an endo or exo form of a 1-aza-2-(3-pyridyl)bicyclo[2.2.1]heptane, a 1-aza-2-(3-pyridyl)bicyclo [2.2.2]octane, a 1-aza-2-(3-pyridyl)bicyclo[3.2.2]nonane, a 1-aza-7-(3-pyridyl) bicyclo[2.2.1]heptane, a 1-aza-3-(3-pyridyl)bicyclo[3.2.2]nonane, or a 1-aza-7-(3-pyridyl)bicyclo[3.2.2]nonane.
Type:
Grant
Filed:
June 30, 1997
Date of Patent:
September 23, 2003
Assignee:
Targacept, Inc.
Inventors:
Peter Anthony Crooks, Gary Maurice Dull, William Scott Caldwell, Balwinder Singh Bhatti, Niranjan Madhukar Deo, Alain Ravard
Abstract: The invention provides compounds of formula (I) wherein n, A, R1, R2 and R3 are as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals.
Abstract: The present invention relates to novel aminomethylene substituted non-aromatic heterocycles and, specifically, to compounds of formula (Ia) or (Ib) wherein W, R1, R2, R3, A, X′, Y′ and Z′ are as defined in the specification, and to intermediates used in the syntheses of such compounds. The novel compounds of formulae (Ia) and (Ib) are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.
Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering inositol hexaphospahte (IHP) to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.
Type:
Grant
Filed:
August 1, 2001
Date of Patent:
August 26, 2003
Assignee:
GMP Oxycell, Inc.
Inventors:
Jean-Marie Lehn, Yves Claude Nicolau, Stephane P. Vincent
Abstract: Novel medicinal compositions aiming at delivering a medicine to a specific site of the large intestine; and preparations for intestinal administration with the use of the same. Namely, medicinal compositions, whereby a medicine can be delivered to a specific site of the large intestine, characterized by containing a P-glycoprotein modifier; and preparations for intestinal administration with the use of the same.
Abstract: This invention relates to the use of a CYP2D6 inhibitor in combination with a drug having CYP2D6 catalyzed metabolism, wherein the drug and the CYP2D6 inhibitor are not the same compound; and pharmaceutical compositions for said use.
Abstract: The present invention relates, in general, to quinone reductase 2 (QR2) and aldehyde dehydrogenase (ALDH), and, in particular, to methods of screening compounds for their ability to modulate the activity of QR2 and/or ALDH and thereby to function as anti-malarial, anti-arthritic and/or anti-lupus agents. The invention further relates to the use of compounds that inhibit ALDH in the production of stem cells en masse.
Abstract: The present invention provides an excellent squalene synthesizing enzyme inhibitor. Specifically, it provides a compound (I) represented by the following formula, a salt thereof or a hydrate of them.
Abstract: The invention provides compounds of Formula I:
These compounds may be in the form of pharmaceutical salts or compositions, and racemic mixtures or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which &agr;7 is known to be involved.
Type:
Grant
Filed:
August 17, 2001
Date of Patent:
July 29, 2003
Assignee:
Pharmacia & Upjohn Company
Inventors:
Jason K. Myers, Bruce N. Rogers, Vincent E. Groppi, Jr., David W. Piotrowski, Alice L. Bodnar, Eric Jon Jacobsen, Jeffrey W. Corbett
Abstract: The present invention relates to a method of treating abnormal anxiety behavior in companion animals comprising administering to a companion animal in need thereof a therapeutically effective amount of an NK-1 receptor antagonist.
Type:
Application
Filed:
July 19, 2002
Publication date:
July 24, 2003
Inventors:
Brian Scott Bronk, Mary Anne Hickman, Carolyn Rose Kilroy
Abstract: The invention relates to a pharmaceutical composition for relieving pelvic pain or infertility associated with uterine dysrhythmia. The composition includes a locally-administered anti-dysrhythmic treating agent and a bioadhesive extended-release carrier. The composition may be delivered in an extended release formulation that includes a bioadhesive, water-swellable, water-insoluble, cross-linked polycarboxylic acid polymer, such as polycarbophil. The treating agent may be a local anesthetic, such as lidocaine. The invention also relates to a method of treating or preventing pelvic pain, or treating or improving infertility, by inserting a mixture of an anti-dysrhythmic treating agent and a bioadhesive carrier into the vagina of the patient to be treated.
Type:
Application
Filed:
October 24, 2002
Publication date:
June 19, 2003
Inventors:
Howard L. Levine, William J. Bologna, Dominique De Ziegler
Abstract: The present invention relates to methods of treating various CNS and other disorders by adminstering fluoroalkoxybenzylamino derivatives of nitrogen containing heterocyclic compounds, and specifically, by administering compounds of the formula 1
Type:
Application
Filed:
July 29, 2002
Publication date:
June 19, 2003
Applicant:
Pfizer Inc.
Inventors:
Phillip Branch Chappell, Brian Thomas O'Neill, Mario David Saltarelli
Abstract: Methods of lowering the levels of A&bgr;40, A&bgr;42 and tau protein in a mammal comprising administering to the mammal an effective amount of talsaclidine, or a physiologically acceptable acid addition salt thereof, and methods of treating diseases associated with the formation of diffuse and senile plaques or A&bgr;40-, A&bgr;42- and tau-containing plaques are disclosed.
Type:
Grant
Filed:
April 30, 2002
Date of Patent:
June 3, 2003
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Christoph Hock, Andreas Raschig, Marion Wienrich, Roger Nitsch, Klaus Mendla, Dieter Horst Meier, Klaus Bornemann, Cornelia Dorner-Ciossek
Abstract: The present invention relates to the use of cilansetron for the treatment of non-obstipative male IBS patients.
Type:
Grant
Filed:
July 20, 2001
Date of Patent:
May 20, 2003
Assignee:
Solvay Pharmaceuticals GmbH
Inventors:
Werner L. M. Cautreels, Claus Rudolf Steinborn, Heinz Guenter Krause, Steven David Caras, Egbertus Hendrikus Evert Biesheuvel, Albertus Hermannus Dirk Plekkenpol
Abstract: The present invention relates compounds of the formula (I):
wherein
X represents hydrogen or a C1-4alkyl group optionally substituted by a hydroxy group;
Y represents hydrogen, C1-6alkyl or C3-7cycloalkyl;
Z is —CR9R10CH2— or —CH2CR9R10—;
R represents hydrogen, fluorine, hydroxy, C1-6alkyl or C1-6alkoxy;
and R1, R2, R3, R4, R5 and R6 are as defined herein.
The compounds are of particular use in the treatment of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
Type:
Grant
Filed:
April 1, 2002
Date of Patent:
April 29, 2003
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Janusz Jozef Kulagowski, Piotr Antoni Raubo, Christopher George Thomson
Abstract: The present invention is concerned with the use of 5HT3 antagonists for promoting intestinal lavage, especially in combination with an osmotic agent.
Abstract: A new method is described for the treatment of cancer. The method utilizes two main parts. The first part is Soma, a healing herb described in the Rig Veda, the sacred scriptures of the Hindus. The second part is a composite of plant-derived substances and a mineral. When they are administered to cancer patients following the recommended therapeutic regimen, regression of the cancer results.
Abstract: Pharmaceutical compositions include aryl substituted amine compounds, and in particular, carbon-linked aromatic azabicyclo compounds, and in particular, aromatic alkylene azabicyclo compounds and aromatic alkyl azabicyclo compounds.
Type:
Application
Filed:
June 4, 2002
Publication date:
March 6, 2003
Inventors:
Jeffrey Daniel Schmitt, Peter Anthony Crooks, Gary Maurice Dull
Abstract: The invention relates to pharmaceutical compositions containing cinchonine dihydrochloride as active ingredient with a purity of at least 95%. The invention also relates to a process for preparing cinchonine dihydrochloride from cinchonine and the use of pharmaceutical compositions containing cinchonine dihydrochloride for treating multiple drug resistance.
Abstract: Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia) are treated by administering an endo or exo form of a 1-aza-2-(3-pyridyl)bicyclo[2.2.1]heptane, a 1-aza-2-(3-pyridyl)bicyclo[2.2.2]octane, a 1-aza-2-(3-pyridyl)bicyclo[3.2.2]nonane, a 1-aza-7-(3-pyridyl)bicyclo[2.2.1]heptane, a 1-aza-3-(3-pyridyl)bicyclo[3.2.2]nonane, or a 1-aza-7-(3-pyridyl)bicyclo[3.2.2]nonane.
Type:
Grant
Filed:
June 30, 1997
Date of Patent:
February 25, 2003
Assignee:
Targacept, Inc.
Inventors:
William Scott Caldwell, Merouane Bencherif, Gary Maurice Dull, Peter Anthony Crooks, Patrick Michael Lippiello
Abstract: The present invention relates to the delivery of muscle relaxants through an inhalation route. Specifically, it relates to aerosols containing a muscle relaxant that is used in inhalation therapy. In a composition aspect of the present invention, the aerosol comprises particles comprising at least 5 percent by weight of muscle relaxant. In a method aspect of the present invention, a muscle relaxant 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 a muscle relaxant, 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 15, 2002
Publication date:
January 9, 2003
Inventors:
Joshua D. Rabinowitz, Alejandro C. Zaffaroni
Abstract: The invention provides compounds of Formula I:
These compounds may be in the form of pharmaceutical salts or compositions, and racemic mixtures or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which &agr;7 is known to be involved.
Type:
Grant
Filed:
August 17, 2001
Date of Patent:
December 31, 2002
Assignee:
Pharmacia & Upjohn Company
Inventors:
Jason K. Myers, Bruce N. Rogers, Vincent E. Groppi, Jr., David W. Piotrowski, Alice L. Bodnar, Eric Jon Jacobsen, Jeffrey W. Corbett
Abstract: The invention provides compounds of Formula I:
These compounds may be in the form of pharmaceutical salts or compositions, and racemic mixtures or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which &agr;7 is known to be involved.
Type:
Grant
Filed:
August 17, 2001
Date of Patent:
December 10, 2002
Assignee:
Pharmacia & Upjohn Company
Inventors:
Jason K. Myers, Bruce N. Rogers, Vincent E. Groppi, Jr., David W. Piotrowski, Alice L. Bodnar, Eric Jon Jacobsen, Jeffrey W. Corbett
Abstract: Methods are disclosed for increasing the effectiveness of dextromethorphan in treating chronic or intractable pain, for treating tinnitus and for treating sexual dysfunction comprising administering dextromethorphan in combination with a therapeutically effective dosage of a debrisoquin hydroxylase inhibitor. A preferred combination is dextromethorphan and the oxidative inhibitor quinidine.