Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-&bgr;. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.
Type:
Grant
Filed:
February 27, 2002
Date of Patent:
February 3, 2004
Assignee:
Signal Pharmaceuticals, Inc.
Inventors:
Shripad S. Bhagwat, Leah M. Gayo-Fung, Qi Chao
Abstract: This invention pertains to compounds which specifically inhibit the adenosine A3 receptor and the use of these compounds to treat a disease associated with A3 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
Type:
Grant
Filed:
December 2, 1999
Date of Patent:
February 3, 2004
Assignee:
OSI Pharmaceuticals, Inc.
Inventors:
Arlindo L. Castelhano, Bryan McKibben, David J. Witter
Abstract: A compound of formula (I):
wherein:
R1 represents hydrogen, halogen, alkyl or alkoxy,
X represents oxygen, sulphur or NR wherein R represents hydrogen or alkyl,
A represents any one of the groups described in the description,
their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as metalloprotease inhibitor.
Type:
Grant
Filed:
December 21, 2001
Date of Patent:
February 3, 2004
Assignee:
Les Laboratoires Servier
Inventors:
Guillaume De Nanteuil, Alain Benoist, Philippe Pastoureau, Massimo Sabatini, John Hickman, Alain Pierre, Gordon Tucker
Abstract: The present invention relates to carboxylic acid derivatives of the formula
where the radicals have the meanings stated in the description, to the preparation of these compounds and to their use as drugs.
Type:
Grant
Filed:
October 8, 1998
Date of Patent:
February 3, 2004
Assignee:
Abbott GmbH & Co., KG
Inventors:
Dagmar Klinge, Wilhelm Amberg, Ernst Baumann, Andreas Kling, Hartmut Riechers, Liliane Unger, Manfred Raschack, Stefan Hergenröder, Sabine Schult
Abstract: The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I,
the substituents being defined in the specification;
as well as to new phthalazine derivatives; processes for the preparation thereof; the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularization, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.
Type:
Grant
Filed:
September 26, 2001
Date of Patent:
February 3, 2004
Assignee:
Novartis AG
Inventors:
Guido Bold, Janet Dawson King, Jörg Frei, Richard Heng, Paul William Manley, Bernhard Wietfeld, Jeanette Marjorie Wood
Abstract: A compound of formula (I):
wherein:
R1 represents hydrogen, or linear or branched (C1-C6)alkyl optionally substituted by one or more identical or different groups selected from aryl, heteroaryl, cycloalkyl and heterocycloalkyl,
represents a saturated ring having from 4 to 7 ring members that may contain, in addition to nitrogen, one or two hetero atoms selected from O, S and —NR3 groups, wherein R3 represents hydrogen or linear or branched (C1-C6)alkyl,
n represents an integer such that 1≦n≦6,
R2 represents any one of the groups described in the description,
their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as inhibitor of trypsin-related serine proteases and thrombin.
Type:
Grant
Filed:
December 14, 2001
Date of Patent:
February 3, 2004
Assignee:
Les Laboratoires Servier
Inventors:
Guillaume De Nanteuil, Philippe Gloanec, Tony Verbeuren, Alain Rupin, Marie-Odile Vallez
Abstract: According to the inventive method, the hydroformylation of the olefinically unsaturated compounds is carried out in the presence of an aqueous, water-soluble catalyst solution containing rhodium complex compounds, in a reaction column.
Abstract: A method for treating cognitive impairments associated with aging or Alzheimer's disease which comprises treating a patient at risk for having the cognitive impairment with an effective amount of a highly selective butyrylcholinesterase inhibitor which is N8-benzylnorcymserine, N1-phenethylnorcymserine, N1, N8-bisnorcymserine, N1-N8-bisbenzylnorphysostigmine, N1, N8-bisbenzylnorphenserine, N1, N8-bisbenzylnorcymserine, or pharmaceutical acceptable salts thereof.
Type:
Grant
Filed:
February 7, 2002
Date of Patent:
January 27, 2004
Assignee:
Axonyx, Inc.
Inventors:
Nigel H. Greig, Qian-Sheng Yu, Arnold Brossi, Timothy T. Soncrant, Marvin Hausman
Abstract: The invention relates to novel guanidine derivatives of the formula (I)
in which
A, R1, R2, R3 and Z are as defined in the description, to a process for their preparation and to their use for controlling animal pests.
Type:
Grant
Filed:
August 17, 2001
Date of Patent:
January 27, 2004
Assignee:
Bayer Aktiengesellschaft
Inventors:
Klaus Wagner, Christoph Erdelen, Andreas Turberg, Norbert Mencke, Olaf Hansen
Abstract: Disclosed herein is a method for suppressing the growth of cancer cells in a mammal in need of such treatment comprising administering to said mammal a cancer cell suppressing amount of a diphenylmethylpiperazine represented by the following general formula [1]:
wherein R represents:
or a pharmaceutically acceptable salt thereof.
Compared with conventional anticancer agents, these agents are less toxic and exert an excellent carcinostatic effect on various solid cancers. Moreover, these anticancer agents inhibit the proliferation of fibroblasts, which makes them efficacious against pulmonary fibrosis and proliferative keloid lesions.
Abstract: The invention relates to the use of derivatives of 3-amidinophenylalanine as urokinase inhibitors for treating malignant tumors and the formation of metastases.
Type:
Grant
Filed:
July 26, 2002
Date of Patent:
January 20, 2004
Assignee:
Wilex AG
Inventors:
Olaf Wilhelm, Viktor Magdolen, Jörg Stürzebecher, John Foekens, Verena Lutz
Abstract: This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.
Type:
Grant
Filed:
December 1, 2000
Date of Patent:
January 20, 2004
Assignee:
OSI Pharmaceuticals, Inc.
Inventors:
Arlindo L. Castelhano, Bryan McKibben, David J. Witter
Abstract: The present invention is to provide a compound or a salt thereof represented by the formula:
wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, X′ is an optionally substituted alkylene chain, Y is an optionally substituted divalent cyclic group, X is a chemical bond or an optionally substituted alkylene chain, and Z is (1) an optionally substituted amino group, (2) an optionally substituted imidoyl group or (3) an optionally substituted nitrogen-containing heterocyclic group, or a pro-drug thereof, which has activated coagulation factor X inhibitory activity and which are useful as anti-coagulants.
Abstract: A new process for the preparation of diethylenetriaminepentaacetic-monoamides in which amines can be reacted with sensitive groups, a higher mono/diamide selectivity is achieved, a higher yield of monoamide is achieved and has a simple reaction scheme and working-up.
Abstract: A method for production of pivalic acid comprising the steps of: (a) reacting isobutylene, carbon monoxide, and a first catalyst to produce a reaction mixture; (b) contacting the reaction mixture with water, thereby producing a crude acid product having pivalic acid and oligomeric neo-carboxylic acid; (c) then separating the pivalic acid and the oligomeric neo-carboxylic acid from the crude acid product; (d) then reacting the oligomeric neo-carboxylic acid with a source of carbon monoxide at a temperature of less than 200° C. in the presence of a second catalyst to produce a C5 carbocation product, wherein the first and second catalyst are either the same or different; and (e) reacting the C5 carbocation product with water; thereby producing pivalic acid having an overall yield of at least 80 wt. %.
Type:
Grant
Filed:
July 9, 2001
Date of Patent:
January 13, 2004
Assignee:
ExxonMobil Chemical Patents Inc.
Inventors:
Edmund J. Mozeleski, Richard H. Schlosberg, Dennis J. Davoren, Carl Robert Beck, Linda J. Broadbelt, Ned C. Haubein
Abstract: A new process is described for the preparation of a compound of the formula I
wherein
R1, R2, R3 and R4, independently of each other, are C1-C8alkyl or C1-C5hydroxyalkyl, or R1 and R2 together with the carbon atom they are attached to are C5-C12cycloalkyl, or R3 and R4 together with the carbon atom they are attached to are C5-C12cycloalkyl;
R5, R6, R7, R8 and R9, independently of each other, are H, C1-C8alkyl, C2-C8alkenyl, C5-C12aryl, C1-C4haloalkyl, an electron withdrawing group, or C6-C12aryl which is substituted by a residue selected from C1-C4alkyl, C1-C4alkoxy, halogen; and R7 and R8 together may also form a chemical bond; and
R is an organic linking group containing 2-500 carbon atoms and forming, together with the carbon atoms it is directly connected to and the nitrogen atom, a substituted, 5-, 6 or 7-membered cyclic ring structure; characterized in that a compound of the formula II
is oxidized.
Type:
Grant
Filed:
November 20, 2001
Date of Patent:
January 13, 2004
Assignee:
Ciba Specialty Chemicals Corporation
Inventors:
Alessandro Zedda, Gianluca Ferri, Massimiliano Sala
Abstract: The present invention provides a novel compound having an excellent acetylcholinesterase inhibitory effect. That is, it provides a 4-substituted piperidine compound fluoride represented by the following formula, a pharmaceutically acceptable salt thereof or hydrates thereof (provided that 1-benzyl-4-[(5,6-dimethoxy-2-fluoro-1-indanon)-2-yl]methylpiperidine, a pharmaceutically acceptable salt thereof and hydrates thereof are excluded).
wherein R1 and R2 represent substituents.
Abstract: The present invention relates to 4-arylindolinones, as well as pharmaceutical compositions thereof, capable of modulating protein kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. The present invention also relates to methods for treating protein kinase related disorders.
Type:
Grant
Filed:
December 20, 2001
Date of Patent:
January 13, 2004
Assignee:
Sugen, Inc.
Inventors:
Jingrong Cui, Ruofei Zhang, Hong Shen, Ji Yu Chu, Fang-Jie Zhang, Marcel Koenig, Steven Huy Do, Xiaoyuan Li, Chung Chen Wei, Peng Cho Tang
Abstract: The compounds of formulas (I) and (II) are radiopharmaceuticals that bind to the CCR1 receptor and are able to pass through the blood-brain barrier, and are therefore useful in diagnosing Alzheimer's disease, preferably at an early stage of the disease,
wherein X1, X2, R1, R2, R3, R4 and R5 are as defined herein.
Type:
Grant
Filed:
November 6, 2001
Date of Patent:
January 13, 2004
Assignee:
Schering Aktiengesellschaft
Inventors:
Christoph-Stephan Hilger, Bernd Johannsen, Joerg Steinbach, Peter Maeding, Meredith Halks-Miller, Richard Horuk, Harald Dinter, Raju Mohan, Joseph E. Hesselgesser
Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:
wherein R1, R2, R3a, R3b, R4, R5, and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.