Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
Type:
Application
Filed:
October 7, 2002
Publication date:
August 14, 2003
Inventors:
James E. Audia, Richard C. Thompson, Stephen C. Wilkie, Thomas C. Britton, Warren J. Porter, George W. Huffman, Lee H. Latimer
Abstract: Vasopeptidase inhibitors, especially omapatrilat, are useful in reducing central and peripheral pulse pressure and vascular stiffness in hypertensive patients. The vasopeptidase inhibitor may be used in combination with other pharmaceutically active agents.
Abstract: A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.
Type:
Grant
Filed:
February 13, 2002
Date of Patent:
June 24, 2003
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Christopher R. Butler, Hui Cai, James P. Edwards, Cheryl A. Grice, Yin Gu, Darin J. Gustin, Lars Karlsson, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Clark A. Sehon, Siquan Sun, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei
Abstract: Two new crystalline forms of 1S-[1alpha(2S*,3R*), 9alpha]6,10-dioxo-N-(2-ethoxy-5-oxo-tetrahydro-3-furanyl)-9 [[(1-isoquiinolyl)carbonyl]amino]octahydro-6H-pyridazino[1,2-a][1,2]diazepin-1-carboxamide (anhydrous or hydrated), their preparation process and the pharmaceutical compositions containing them.
Abstract: This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents, hypotriglyceridemic agents, antiatherosclerosis agents, antifungal agents, anti-Alzheimer's agents or anti-acne agents.
Abstract: Compounds of formula I
as well as pharmaceutically usable salts and esters thereof, inhibit the binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. They can be used in the form of pharmaceutical preparations for the treatment or prevention of neoplasms, tumor metastasis, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure as well as infection caused by viruses, bacteria or fungi.
Type:
Grant
Filed:
July 7, 2000
Date of Patent:
January 14, 2003
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Leo Alig, Alexander Chucholowski, Thomas Weller
Abstract: The invention is directed to nonpeptide substituted benzodiazepines of Formula I,
wherein A, X, Z, Bp, W, n, R1 and R2 are as described in the specification, which are useful as vasopressin receptor antagonists for treating conditions involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, or water retention are also disclosed.
Abstract: The present invention relates to benzoxazepinones of formula I:
or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same and methods of using the same for treating viral infection or as an assay standard or reagent.
Abstract: Methods and compositions are disclosed utilizing N-desmethylolanzapine for the treatment of psychosis in humans. N-Desmethylolanzapine exhibits a lessened liability toward drug-drug interactions than olanzapine and a more predictable dosing regimen than olanzapine. N-Desmethylolanzapine is also useful for the treatment of acute mania, mild anxiety states, anxiety disorders, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder, autistic disorder, excessive aggression, substance abuse, depressive signs and symptoms, tic disorder, functional bowel disorder and fungal dermatitis.
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: The present invention provides a compound of the formula:
wherein ring A is an optionally substituted aromatic hydrocarbon ring or aromatic heterocyclic ring; ring B is an optionally substituted aromatic hydrocarbon ring or aromatic heterocyclic ring; Z is an optionally substituted cyclic group or linear hydrocarbon group; R1 is a hydrogen atom, an optionally substituted hydrocarbon group or heterocyclic ring; R2 is an optionally substituted amino group; D is a bond or an optionally substituted divalent hydrocarbon group; E is a bond, —CON(Ra)—, —N(Ra)CO—, —N(Rb)CON(Rc)—, —N(Rd)COO—, —N(Re)SO2—, —COO—, —N(Rf)—, —O—, —S— —SO—, —SO2—,
(in which Ra, Rb, Rc, Rd, Re and Rf are respectively a hydrogen atom or an optionally substituted hydrocarbon group); G is a bond or an optionally divalent substituted hydrocarbon group; L is a divalent group;
ring
Abstract: This invention relates generally to heteroaryl-phenyl substituted compounds that are inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.
Abstract: Methods and compositions are disclosed utilizing N-desmethylolanzapine for the treatment of psychosis in humans. N-Desmethylolanzapine exhibits a lessened liability toward drug-drug interactions than olanzapine and a more predictable dosing regimen than olanzapine. N-Desmethylolanzapine is also useful for the treatment of acute mania, mild anxiety states, anxiety disorders, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder, autistic disorder, excessive aggression, substance abuse, depressive signs and symptoms, tic disorder, functional bowel disorder and fungal dermatitis.
Abstract: The present invention relates to modified amino acids of general formula
wherein
A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.
Type:
Grant
Filed:
October 12, 1999
Date of Patent:
February 5, 2002
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Helmut Pieper, Henri Doods, Gerhard Hallermayer, Michael Entzeroth, Wolfgang Wienen
Abstract: Vasopeptidase inhibitors, especially omapatrilat, are useful in treating and/or slowing the progression of cognitive dysfunction and treating and/or preventing dementia of the Alzheimer's type and vascular dementia. The vasopeptidase inhibitor may be used in combination with other pharmaceutically active agents.
Abstract: A method of treating hyperproliferation diseases in mammals in need of such treatment which method includes administering to said mammal a therapeutically effective amount of a compound of the formula:
or a pharmaceutically acceptable salt, hydrate or prodrug thereof, wherein R1, R2, R3, R4, W, X, Y, Z and t are as defined herein.
Type:
Grant
Filed:
April 13, 2000
Date of Patent:
November 20, 2001
Assignee:
Pfizer Inc.
Inventors:
Steven W. Goldstein, Kelly P. Longo, Arthur A. Nagel, John A. Lowe, III
Abstract: A compound represented by the formula (I) or (II) or a salt thereof wherein R1 represents hydrogen atom or a C1-6 alkyl group; R2 and R3 independently represent a hydrogen atom or a C1-6 alkyl group, or R2 and R3 may combine together to represent a 5- or 6-membered cycloalkyl group; R4 represents, for example, a hydrogen atom or a C1-6 alkyl group; R5 represents, for example, a hydrogen atom or a C1-6 alkyl group; R6 represents a hydrogen atom or a C-1-6 alkyl group; X represents —NR7—, —O—, —CHR7— or —S— in which R7 represents, for example, a hydrogen atom or a C1-6 alkyl group; and Y represents a phenylene group or a pyridinediyl group. The compounds are useful as agents for enhancing the activities of retinoid compounds.
Abstract: A method of treating or improving intermittent claudication, which comprises administering, to a patient with intermittent claudication, a pyrroloazepine derivative or a pharmacologically acceptable salt thereof, said pyrroloazepine derivative being represented by the following formula (I):
wherein the dotted line indicates existence or nonexistence of a bond; when the bond of the dotted line exists, X does not exist, and, when the bond of the dotted line does not exist, X represents a hydrogen atom, a hydroxy group or a group OR1 in which R1 represents a substituted or unsubstituted alkyl group; Y represents a linear or branched, substituted or unsubstituted alkyl group; Z1 and Z2 are the same or different and each independently represent a hydrogen atom, a hydroxy group or a halogen atom; and W represents a hydrogen atom or a methyl group.
Abstract: The present invention relates to benzazepine derivatives and their use as &agr;v 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.
Abstract: Vitronectin receptor antagonists, their preparation and their use
The present invention relates to compounds of the formula I
A—B—D—E—F—G (I)
in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.
Type:
Grant
Filed:
October 5, 1999
Date of Patent:
March 27, 2001
Assignees:
Hoechst Atkiengesellschaft, Genentech, Inc.
Inventors:
Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel LeFrancois, Thomas Richard Gadek, Robert McDowell
Abstract: A benzoxazepine derivative having the general formula (I) and its salts and medicaments containing the same as effective ingredients:
wherein, n is an integer of 2 to 5, R1 indicates a hydrogen atom, halogen atom, C1 to C4 lower alkyl group, C1 to C4 lower alkoxyalkyl group, C1 to C4 halogenoalkyl group, cyano group, or ester group, R2 indicates a hydrogen atom, halogen atom, C1 to C4 lower alkyl group, C1 to C4 lower alkoxy group, or hydroxy group, a dotted line indicates the presence or absence of a binding bond, W indicates C, CH, or CH2 or a nitrogen atom, provided that, when W is a nitrogen atom, Z is bonded to W and the dotted line indicates the absence of a bond, and Z indicates an unsubstituted or substituted aromatic hydrocarbon ring group or an unsubstituted or substituted heterocyclic group).