Abstract: The use of compounds that are antagonists of the pain enhancing effects of E-type prostaglandins for the treatment or prevention of neuropathic pain are described. The use of a compound that is an antagonist of the pain enhancing effects of E-type prostaglandins in the production of a medicament for use in the treatment or prevention of neuropathic pain, and a method of treating or preventing neuropathic pain by administration of an effective amount of an antagonist of the pain enhancing effects of E-type prostaglandins to a warm blooded animal such as man are also described.
Abstract: A method of treating, preventing, or inhibiting pain, inflammation or inflammation-associated disorder in a subject in need of such treatment or prevention provides for treating the subject with glucosamine and a cyclooxygenase-2 selective inhibitor or prodrug thereof, wherein the amount of glucosamine and the amount of a cyclooxygenase-2 selective inhibitor or prodrug thereof together constitute a pain or inflammation suppressing treatment or prevention effective amount of the composition. Compositions and pharmaceutical compositions that contain glucosamine and a cyclooxygenase-2 selective inhibitor are also disclosed.
Abstract: Novel heterocyclic compounds of formula I and the salts, solvates and prodrugs thereof, wherein the meanings of the various substituents are as disclosed in the description. Said compounds are useful as anti-inflammatories.
Type:
Application
Filed:
October 25, 2002
Publication date:
June 19, 2003
Inventors:
Carmen Almansa Rosales, Concepcion Gonzalez Gonzalez, MaCarmen Torres Barreda
Abstract: The present invention relates to novel pyridazinone compounds, pharmaceutical compositions comprising those compounds and to methods of using such compounds and compositions to inhibit aldose reductase, lower sorbitol levels and, thus, lower fructose levels, and/or treat or prevent diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. This invention also relates to methods of affording cardioprotection to subjects not suffering from diabetes. This invention also relates to pharmaceutical compositions and kits comprising a combination of an aldose reductase inhibitor (ARI) of this invention and a sorbitol dehydrogenase inhibitor and to methods of using such compositions or kits to treat or prevent the above diabetic complications in mammals.
Abstract: This invention relates to compounds which are IP receptor antagonists and which are represented by Formula (I):
wherein G2 is a heteroaryl group containing one or two nitrogen atoms substituted with a carboxylic acid group, said heteroaryl ring containing one or two nitrogen atoms, and G1 is as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
Type:
Grant
Filed:
March 1, 2002
Date of Patent:
May 27, 2003
Assignee:
Roćhe Palo Alto LLC
Inventors:
Francisco Javier Lopez-Tapia, Dov Nitzan, Counde O'Yang
Abstract: N-Heterocyclic derivatives of the formula (I): 1
Type:
Application
Filed:
April 12, 2002
Publication date:
May 15, 2003
Applicant:
Berlex Laboratories, Inc.
Inventors:
Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H.J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
Abstract: N-Heterocyclic derivatives of the formula (I): 1
Type:
Application
Filed:
April 12, 2002
Publication date:
May 1, 2003
Applicant:
Berlex Laboratories, Inc.
Inventors:
Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
Abstract: N-Heterocyclic derivatives of the formula (I): 1
Type:
Application
Filed:
April 12, 2002
Publication date:
April 24, 2003
Applicant:
Berlex Laboratories, Inc.
Inventors:
Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
Abstract: N-Heterocyclic derivatives of the formula (I): 1
Type:
Application
Filed:
April 12, 2002
Publication date:
April 10, 2003
Applicant:
Berlex Laboratories, Inc.
Inventors:
Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
Abstract: Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian Factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
Type:
Application
Filed:
April 1, 2002
Publication date:
April 10, 2003
Inventors:
Bing-Yan Zhu, Penglie Zhang, Erick A. Goldman, Zhaozhong Jon Jia, Shawn Bauer, Wenrong Huang, John Woolfrey, Robert M. Scarborough
Abstract: N-Heterocyclic derivatives of the formula (I): 1
Type:
Application
Filed:
April 12, 2002
Publication date:
March 27, 2003
Applicant:
Berlex Laboratories, Inc.
Inventors:
Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
Abstract: The invention provides a novel pest control agent having a high systemic activity and a high safety with reduced adverse influences on the environment neighboring the place to which the agent is applied, and a process for producing the same.
Abstract: Efficacious remedies for male sterility which are in the form of preparations containing as the active ingredient an adenosine A1 antagonist.
Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CERP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
Type:
Application
Filed:
December 12, 2001
Publication date:
February 6, 2003
Inventors:
James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
Abstract: N-Heterocyclic derivatives of the formula (I): 1
Type:
Application
Filed:
April 12, 2002
Publication date:
February 6, 2003
Applicant:
Berlex Laboratories, Inc.
Inventors:
Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
Abstract: The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.
Type:
Application
Filed:
September 21, 2001
Publication date:
February 6, 2003
Inventors:
Pascal Druzgala, Peter G. Milner, Jurg R. Pfister
Abstract: 5-Arylidene-4-oxo-2-thioxo-3-thiazolidinecarboxylic acids of formula I
in which the symbols R1, R2, A, A1 and A2 have the significance given in the description as medicaments for the treatment of cancer diseases.
Abstract: N-Heterocyclic derivatives of the formula (I): 1
Type:
Application
Filed:
April 12, 2002
Publication date:
January 2, 2003
Applicant:
Berlex Laboratories, Inc.
Inventors:
Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H.J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
Abstract: The invention relates to heterocyclic derivatives, or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The, invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, formula (I).
Type:
Application
Filed:
June 27, 2002
Publication date:
December 19, 2002
Applicant:
ZENECA LIMITED
Inventors:
Peter Warner, Roger James, Thorsten Nowak
Abstract: Provided is a method of treating or ameliorating certain fibrotic diseases or other indications in an animal, including a human, comprising administering an effective amount of a compound of the formula I:
Type:
Application
Filed:
December 31, 2001
Publication date:
December 5, 2002
Inventors:
Dilip Wagle, Martin Gall, Stanley C. Bell, Edmond J. LaVoie
Abstract: N-Heterocyclic derivatives of the formula (I): 1
Type:
Application
Filed:
April 12, 2002
Publication date:
December 5, 2002
Applicant:
Berlex Laboratories, Inc.
Inventors:
Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
Abstract: Provided is a method of treating or ameliorating a number of indications in an animal, including a human, comprising administering an effective amount of a compound of the formula I or IA, 1
Type:
Application
Filed:
December 31, 2001
Publication date:
December 5, 2002
Inventors:
Dilip Wagle, Martin Gall, Stanley C. Bell, Edmond J. LaVoie
Abstract: Provided, among other things, is a method of treating or ameliorating or preventing an indication of the invention in an animal, including a human comprising administering an effective amount of a compound of the formula I: 1
Type:
Application
Filed:
December 31, 2001
Publication date:
November 28, 2002
Inventors:
John J. Egan, Dilip Wagle, Sara Vasan, Martin Gall, Stanley Bell, Edmond J. LaVoie
Abstract: This invention relates to compounds of formula (1), wherein substituents are defined in the description, that inhibit farnesylation of mutant ras gene products tough inhibition of the enzyme farnesyl-protein transferase (FPTase). The invention also relates to methods of manufacturing the compounds, pharmaceutical compositions and methods of treating diseases, especially cancer, which are mediated through farnesylation of ras.
Abstract: Compounds that inhibit DNA-dependent protein kinase, compositions comprising the compounds, methods to inhibit the DNA-PK biological activity, methods to sensitize cells the agents that cause DNA lesions, and methods to potentiate cancer treatment are disclosed.
Type:
Application
Filed:
August 28, 2001
Publication date:
November 7, 2002
Inventors:
James Halbrook, Edward A. Kesicki, Laurence E. Burgess, Stephen T. Schlachter, Charles T. Eary, Justin G Schiro, Hongmei Huang, Michael Evans, Yongxin Han
Abstract: Provided is a method of treating or ameliorating or preventing glaucoma, decreasing intraocular pressure or improving or amemliorting ocular accommodation in an animal, including a human comprising administering an intraocular pressure decreasing or accommodation improving amount of a compound of the formula I: 1
Type:
Application
Filed:
December 31, 2001
Publication date:
October 31, 2002
Inventors:
John J. Egan, Dilip Wagle, Sara Vasan, Martin Gall, Stanley Bell, Edmond Joseph LaVoie
Abstract: Provided is a method of treating, ameliorating or preventing certain fibrotic diseases or other indications in an animal, including a human, comprising administering an intraocular pressure decreasing or accommodation improving amount of (A) a compound of formula (I):
Type:
Application
Filed:
December 31, 2001
Publication date:
October 24, 2002
Inventors:
Dilip Wagle, Martin Gall, Stanley C. Bell, Edmond J. LaVoie
Abstract: Compounds having Formula 4 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
Type:
Application
Filed:
February 21, 2002
Publication date:
October 24, 2002
Inventors:
Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Roshantha A. Chandraratna
Abstract: A pyridazinone derivative represented by formula (I):
a pharmaceutically acceptable salt thereof, or a derivative thereof, or a pharmaceutical composition comprising as an active ingredient the derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent.
Abstract: The present invention relates to novel pyridazinone compounds, pharmaceutical compositions comprising those compounds and to methods of using such compounds and compositions to inhibit aldose reductase, lower sorbitol levels and, thus, lower fructose levels, and/or treat or prevent diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. This invention also relates to methods of affording cardioprotection to subjects not suffering from diabetes. This invention also relates to pharmaceutical compositions and kits comprising a combination of an aldose reductase inhibitor (ARI) of this invention and a sorbitol dehydrogenase inhibitor and to methods of using such compositions or kits to treat or prevent the above diabetic complications in mammals.
Abstract: Compounds of formula (I) which are optionally substituted 2-(&ohgr;,&ohgr;-diarylalkyl)-4,5-dihydro-1H-imidazoles and 2-(&ohgr;,&ohgr;-diarylalkyl)-1,4,5,6-tetrahydropyrimidines and salts thereof with inorganic and organic acids have interesting pharmacological properties. Thus, the compounds are useful in the treatment of type 2 diabetes.
Type:
Application
Filed:
November 9, 2001
Publication date:
September 19, 2002
Inventors:
Henrik Sune Andersen, Palle Jakobsen, Peter Madsen
Abstract: Provided is a method of decreasing intraocular pressure or improving ocular accommodation in an animal, including a human, comprising administering an intraocular pressure decreasing amount or ocular accommodation improving amount of a compound of the formula I or IA, 1
Type:
Application
Filed:
December 31, 2001
Publication date:
August 29, 2002
Inventors:
Dilip Wagle, Martin Gall, Stanley C. Bell, Edmond J. LaVoie
Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.
Type:
Grant
Filed:
October 5, 2001
Date of Patent:
July 23, 2002
Assignee:
UCB, S.A.
Inventors:
Gurmit Grewal, Anna Toy-Palmer, Xiong Cai, George Mark Latham
Abstract: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
Type:
Grant
Filed:
November 21, 2000
Date of Patent:
July 23, 2002
Assignee:
ICOS Corporation
Inventors:
Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Edward A. Kesicki, Amy Oliver, Laurence E. Burgess, John J. Gaudino, Zachary S. Jones, Bradley J. Newhouse, Stephen T. Schlachter
Abstract: The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities.
Type:
Grant
Filed:
April 17, 2000
Date of Patent:
July 9, 2002
Assignee:
GPI NIL Holdings, Inc.
Inventors:
Yong-Qian Wu, Wei Huang, Gregory S. Hamilton
Abstract: The invention provides certain 1,2,4-triazole-3-thione compounds, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Application
Filed:
December 10, 2001
Publication date:
July 4, 2002
Applicant:
AstraZeneca AB
Inventors:
Andrew Baxter, Colin Bennion, Peter Cage, Nicholas Kindon, Michael Mortimore, Bryan Roberts
Abstract: The present invention relates to a compound of Formula (1) wherein Ar1 represent (A) or (B) or (C); R1 is hydrogen, C1-4alkyl or C1-4alkanoyl; R12 and R13 are independently hydrogen or C1-4alkyl; Ar2 is phenyl or heteroaryl; p is 0 or 1; Ar3 is of formula (I) wherein W, X, Y and Z are independently CH or N, provided that at least two of W, X, Y and Z are CH and R2 and —(CH2)nR3 are attached to ring carbon atoms; R2 is a group of Formula (II) or R2 represents a lactone of Formula (III) the group of Formula (II) or (III) having L or D configuration at the chiral alpha carbon in the corresponding free amino acid; n is 0, 1 or 2; R3 is phenyl or heteroaryl; provided that: when n is 0, Ar3 is substituted by R2 in the 4-position and —(CH2)nR3 in the 3- or 5-position; and when n is 1 or 2, Ar3 is substituted by R2 in the 3- or 5-position and —(CH2)nR3 in the 4-position; and R5-R9, m and n are as defined in the specification; or a pharmaceutically-acceptable salt, prodrug or solvate thereof.
Type:
Grant
Filed:
March 24, 2000
Date of Patent:
June 25, 2002
Assignees:
Astrazenca UK Limited, Zeneca Pharma SA