Abstract: The present invention concerns methods, pharmaceutical compounds, and compositions for stimulating neuroite outgrowth in nerve cells leading to nerve regeneration. These methods, compounds and compositions inhibit rotamase enzyme activity associated with binding proteins.
Type:
Application
Filed:
December 1, 2000
Publication date:
May 23, 2002
Inventors:
Chuangxing Guo, Liming Dong, Xinjun J. Hou, Darin Vanderpool, Jesus Ernest Villafranca
Abstract: The invention provides a method of treatment or prophylaxis of obesity, comprising administering to a patient in need of such treatment a therapeutically effective amount of an aryl sulfonamide compound of formula (I) or formula (II) 1
Type:
Application
Filed:
July 20, 2001
Publication date:
May 16, 2002
Inventors:
Patrizia Caldirola, Sukhwinder Jossan, Kjell S. Sakariassen, Jan Svartengren
Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
Type:
Application
Filed:
September 25, 2001
Publication date:
May 9, 2002
Inventors:
Rajashehar Betageri, Steffen Breitfelder, Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, Thomas M. Kirrane, Monica H. Moriak, Neil Moss, Usha R. Patel, John R. Proudfoot, John R. Regan, Rajiv Sharma, Sanxing Sun, Alan D. Swinamer, Hidenori Takahashi
Abstract: Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.
Type:
Application
Filed:
July 20, 2001
Publication date:
May 9, 2002
Inventors:
Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.
Type:
Application
Filed:
August 10, 2001
Publication date:
April 25, 2002
Applicant:
GPI NIL HOLDINGS, INC.
Inventors:
Gregory S. Hamilton, Jai-He Li, Wei Huang
Abstract: The present application describes novel amides and derivatives thereof of formula I:
or pharmaceutically acceptable salt forms thereof, wherein these compounds are useful as inhibitors of matrix metalloproteinases, TNF-&agr;, and aggrecanase.
Type:
Grant
Filed:
March 31, 2000
Date of Patent:
April 23, 2002
Inventors:
Jingwu Duan, Carl P. Decicco, David J. Nelson, Chu-Biao Xue
Abstract: The present application describes novel substituted aryl hydroxamic acids of formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing from 0-1 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.
Type:
Grant
Filed:
May 13, 1999
Date of Patent:
April 2, 2002
Inventors:
Matthew E. Voss, Carl P. Decicco, Ruth R. Wexler
Abstract: The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma.
Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, wherein the disease may be, for example, asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
Type:
Grant
Filed:
July 31, 1998
Date of Patent:
March 26, 2002
Assignees:
Athena Neurosciences, Inc., American Home Products
Inventors:
Eugene D. Thorsett, Christopher M. Semko, Michael A. Pleiss, Louis John Lombardo, Andrei W. Konradi, Francine S. Grant, Darren B. Dressen, Michael S. Dappen
Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflmatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.
Type:
Application
Filed:
July 3, 2001
Publication date:
March 14, 2002
Applicant:
American Cyanamid Company
Inventors:
Aranapakam Mudumbai Venkatesan, Jannie Lea Baker, Jeremy Ian Levin
Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.
Type:
Application
Filed:
June 6, 2001
Publication date:
March 14, 2002
Applicant:
Vertex Pharmaceuticals Incorporated
Inventors:
Roger D. Tung, Scott L. Harbeson, David D. Deininger, Mark A. Murcko, Govinda R. Bhisetti, Luc J. Farmer
Abstract: The invention relates to novel compounds of the formula
in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.
Abstract: This invention provides compounds of formula I having the structure
wherein R1, Ar, Ar′, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof, which are useful as contraceptive agents.
Type:
Grant
Filed:
March 24, 2000
Date of Patent:
March 12, 2002
Assignee:
American Home Products Corporation
Inventors:
Jay E. Wrobel, John F. Rogers, Daniel M. Green, Wenling Kao, James W. Jetter
Abstract: The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma.
Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.
Type:
Application
Filed:
July 28, 2001
Publication date:
January 24, 2002
Inventors:
Ben C. Askew, Paul J. Coleman, Mark E. Duggan, Wasyl Halczenko, George D. Hartman, Cecilia A. Hunt, John H. Hutchinson, Robert S. Meissner, Michael A. Patane, Garry R. Smith, Jiabing Wang
Abstract: A process of forming the cis- or the trans-isomers of thiazine-indigo compounds comprising the step of reacting o-aminomercapto-carbocyclic or -heterocyclic compounds with a maleic acid or fumaric acid derivative in the presence of an aqueous system.
The invention further relates to a process of converting cis-isomers of thiazine-indigo compounds into the trans-isomers being pigments.
The invention also relates to the cis-isomers of thiazine-indigo compounds of formula I as defined in claim 14 which are new compounds.
Abstract: The present invention relates to compounds of the formula I
wherein A1, A2, R1, R2, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.
Type:
Grant
Filed:
July 8, 1999
Date of Patent:
January 1, 2002
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Ursula Schindler, Karl Schönafinger, Hartmut Strobel
Abstract: A phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative represented by formula (I)
effective against diseases in which histamine, leukotrienes, etc. participate and effective in preventing or treating diseases in which chemical mediators such as histamine and leukotrienes participate, for example, asthma, allergic rhinitis, atopic dermatitis, urticaria, hay fever, gastrointestinal allergy and food allergy.
Abstract: Disclosed are novel succinate derivative compounds of the formula (I)/(Ia): 1
Type:
Application
Filed:
May 22, 2001
Publication date:
November 15, 2001
Inventors:
Younes Bekkali, Rajashehar Betageri, Michel Jose Emmanuel, Eugene Richard Hickey, Weimin Liu, Usha R. Patel, Denice Mary Spero, David S. Thomson, Yancey David Ward, Erick Richard Roush Young
Abstract:
The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma.
Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-oxides of heterocyclic esters amides, thioesters, and ketones having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.
Type:
Application
Filed:
April 26, 2001
Publication date:
November 1, 2001
Inventors:
Gregory S. Hamilton, Joseph P. Steiner, Eric S. Burak
Abstract: The present invention relates to the use of known agonists of the central cannabinoid receptor CB1 for the prophylaxis and treatment of neurodegenerative disorders, in particular for the treatment of cerebral apoplexy and craniocerebral trauma.
Type:
Application
Filed:
May 29, 2001
Publication date:
October 25, 2001
Inventors:
Joachim Mittendorf, Jurgen Dressel, Michael Matzke, Jurgen Franz, Peter Spreyer, Verena Vohringer, Joachim Schuhmacher, Arno Friedl, Ervin Horvath, Frank Mauler, Jean-Marie-Viktor De Vry, Reinhard Jork
Abstract: Novel arylalkylamino compounds exhibiting calcilytic properties are provided.
Type:
Grant
Filed:
October 1, 1999
Date of Patent:
September 25, 2001
Assignee:
SmithKline Beecham Corporation
Inventors:
Robert M. Barmore, Pradip Kumar Bhatnagar, William M. Bryan, Joelle Lorraine Burgess, James Francis Callahan, Raul Rolando Calvo, Eric G. Del Mar, Maria Amparo Lago, Thomas The Nguyen, Derek Sheehan, Robert Lawrence Smith, Linda Sue Southall, Bradford C. Van Wagenen
Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
Type:
Grant
Filed:
July 30, 1998
Date of Patent:
September 18, 2001
Assignees:
Athena Neurosciences, Inc., American Home Products Corp.
Inventors:
Susan Ashwell, Francine S. Grant, Andrei W. Konradi, Anthony Kreft, Louis John Lombardo, Michael A. Pleiss, Dimitrios Sarantakis, Christopher M. Semko, Eugene D. Thorsett
Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
August 7, 2001
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Bruce A. Dressman, James E. Fritz, Stephen W. Kaldor, Vincent J. Kalish, Siegfried Heinz Reich, Michael J. Rodriguez, Timothy A. Shepherd, John H. Tatlock, Louis Nickolaus Jungheim
Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a mammal related to supranormal intracellular enzyme activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound is activated selectively within cells having such supranormal intracellular enzyme activity.
Abstract: Compounds having fungicidal activities and represented by general formula (I) and salts and hydrates thereof
wherein R1 represents an optionally substituted aryl, an optionally substituted alkyl or the like; R2 represents an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted aryl, an optionally substituted heterocyclic group or the like; R3 represents an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted arylsulfonyl, an optionally substituted heterocyclic group or the like; R4 and R5, which may be the same or different, represent each a hydrogen atom, an optionally substituted alkyl, or an optionally substituted alkoxy, or R4 and R5 may form together with the adjacent nitrogen atom an optionally substituted monocycle or polycycle; X and Y, which may be the same or different, represents each an oxygen atom or NR6 wherein R6 represents a hydroge
Abstract: The invention relates to new compounds of general formula I
and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R1, R2, R3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.
Type:
Grant
Filed:
February 16, 1999
Date of Patent:
May 22, 2001
Assignee:
Boehringer Ingelheim KG
Inventors:
Horst Dollinger, Gerd Schnorrenberg, Hans Briem, Birgit Jung, Georg Speck
Abstract: The present invention relates to the use of compounds capable of displacing tritiated cis-N-cyclohexyl-N-ethyl [3-(3-chloro-4-cyclohexylphenyl)-allyl]amine from its receptors for the preparation of pharmaceutical compositions intended to combat cell proliferation.
Type:
Grant
Filed:
April 12, 1999
Date of Patent:
May 22, 2001
Assignee:
Sanofi-Synthelabo
Inventors:
Jean Claude Breliere, Pascual Ferrara, Christine Lebouteiller, Raymond Paul, Jorge Rosenfeld, Didier Van Broeck
Abstract: Compounds of the formula:
are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
Type:
Grant
Filed:
January 27, 2000
Date of Patent:
May 1, 2001
Assignee:
American Cyanamid Company
Inventors:
Jeremy I. Levin, James M. Chen, Derek C. Cole, Mila T. Du, Leif M. Laakso
Abstract: In accordance with the present invention, there is provided a class of compounds which are capable of modulating processes mediated by peroxisome proliferator activated receptor-gamma (PPAR-&ggr;). The identification of such compounds makes it possible to intervene in PPAR-&ggr; mediated pathways.
Type:
Grant
Filed:
February 22, 1999
Date of Patent:
April 10, 2001
Assignee:
The Salk Institute for Biological Studies
Abstract: This invention relates to neurotrophic low molecular weight, small molecule heterocyclic esters and amides having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.
Abstract: This invention relates to methods and compositions for treating pain and nociception in a patient by administering a combination of a morpholine or thiomorpholine tachykinin antagonist and an opioid analgesic.