Chalcogen Attached Directly To The Nitrogen By Nonionic Bonding Patents (Class 514/238.2)
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Publication number: 20040192688Abstract: This invention relates to novel {overscore (&ohgr;)}-substituted-naphthyloxy-amino alkanes, their preparation and use as antihyperglycemic agents and for the treatment and prevention of cardiovascular disorders (CVS) such as lipid lowering effects.Type: ApplicationFiled: October 27, 2003Publication date: September 30, 2004Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Devdutt Chaturvedi, Atul Kumar, Reema Rastogi, Arvind Srivastava, Priti Tewari, Rehan Ahmad, Ramesh Chander, Anju Puri, Geetika Bhatia, Farhan Rizvi, Anil Kumar Rastogi, Suprabhat Ray
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Publication number: 20040180871Abstract: The present invention provides compositions and their use in the treatment of inflammatory diseases caused by T-cell proliferation such as sepsis, inflammatory bowel diseases, autoimmune encephalomyelitis, or lupus.Type: ApplicationFiled: December 23, 2003Publication date: September 16, 2004Applicant: Genzyme CorporationInventors: Mark M. Staveski, Robert J. Miller, Sharon R. Nahill
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Publication number: 20040180884Abstract: The present invention discloses a dibenzocycloheptene compound represented by the formula (I): 1Type: ApplicationFiled: December 23, 2003Publication date: September 16, 2004Inventors: Yoshiaki Kuroki, Hitoshi Ueno, Tetsushi Katsube, Tetsuo Kawaguchi, Eiji Okanari, Ichiro Tanaka, Masayuki Tanaka, Masahiko Hagihara
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Publication number: 20040157817Abstract: The present invention provides certain cycloalkenylsulfonamide derivatives of the formula: 1Type: ApplicationFiled: November 6, 2003Publication date: August 12, 2004Inventors: Buddy Eugene Cantell, Dennis Michael Zimmermann
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Publication number: 20040121997Abstract: A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 24, 2003Publication date: June 24, 2004Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Matsunaga, Hideaki Amada
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Publication number: 20040110755Abstract: The present invention relates to pharmaceutical combinations therapies based on p38 kinase inhibitors and another active ingredient, pharmaceutical compositions comprising such combinations, processes for preparing them and their use in the treatment of cytokine mediated diseases.Type: ApplicationFiled: August 11, 2003Publication date: June 10, 2004Applicants: Boehringer Ingelheim Pharmaceuticals, Inc., Boehringer Ingelheim FranceInventors: Stefan Simianer, Pascal Bilbault, Michael L. Cappola, Susan Lynn Way
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Patent number: 6747027Abstract: This invention is directed to proteinase (protease) inhibitors, and more particularly to thiol sulfonamide inhibitors for matrix metalloproteinase 13(MMP-13), compositions of proteinase inhibitors, intermediates for the syntheses of proteinase inhibitors, processes for the preparation of proteinase inhibitors and processes for treating pathological conditions associated with pathological matrix metalloproteinase activity related to MMP-13.Type: GrantFiled: July 22, 1997Date of Patent: June 8, 2004Assignee: Pharmacia CorporationInventors: Gary DeCrescenzo, Zaheer S. Abbas, John N. Freskos, Daniel P. Getman, Robert M. Heintz, Brent V. Mischke, Joseph J. McDonald
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Publication number: 20040092519Abstract: This patent application describes a method for treating or preventing hot flashes in a patient suffering therefrom comprising administering a therapeutically effective dose of a compound selected from reboxetine, S,S-reboxetine, pharmaceutically acceptable salts thereof, derivatives thereof, or prodrugs thereof to the patient.Type: ApplicationFiled: August 4, 2003Publication date: May 13, 2004Inventor: Fred Hassan
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Publication number: 20040087585Abstract: Nobel PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: August 28, 2003Publication date: May 6, 2004Inventors: Jia-Ning Xiang, Siegfried B Christensen, Jinhwa Lee, Daniel J Mercer
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Patent number: 6730783Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: April 22, 2003Date of Patent: May 4, 2004Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan
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Publication number: 20040082564Abstract: The present invention relates to methods of treatment of certain metabolic diseases, and to the use of compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, the invention relates to the use of compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the following formulae: (I) and (II) Wherein Y, C, R1, R2, R6, and R7 are defined herein.Type: ApplicationFiled: August 19, 2003Publication date: April 29, 2004Inventors: Thomas Arrhenius, Jie Fei Cheng, Mark E. Wilson, Rossy Serafimov, Masahiro Nishimoto, David Mark Wallace, Sovouthy Tith, Steve Joel Brown, Charles Stanford Harmon
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Publication number: 20040077647Abstract: Disclosed are compounds of formula (I): 1Type: ApplicationFiled: August 1, 2003Publication date: April 22, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Abdelhakim Hammach, Victor Kamhi, Neil Moss, Paul S. Riska, Christopher Pargellis
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Patent number: 6716844Abstract: An aromatic sulfonyl aipha-hydroxy hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: December 3, 2001Date of Patent: April 6, 2004Assignee: Pharmacia CorporationInventors: John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
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Publication number: 20040058907Abstract: There are provided according to the invention, novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, X a, b, and Z are as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.Type: ApplicationFiled: July 21, 2003Publication date: March 25, 2004Inventors: Rachael Anne Ancliff, Caroline Mary Cook, Colin David Eldred, Paul Martin Gore, Lee Andrew Harrison, Simon Teanby Hodgson, Duncan Bruce Judd, Suzanne Elaine Keeling, Xiao Qing Lewell, Graeme Michael Robertson, Stephen Swanson
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Publication number: 20040053925Abstract: The invention relates to new products of formula (I): 1Type: ApplicationFiled: September 30, 2003Publication date: March 18, 2004Inventors: Pierre Deprez, Marcel Patek
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Patent number: 6706712Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.Type: GrantFiled: December 20, 2001Date of Patent: March 16, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Robert Cherney
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Patent number: 6706715Abstract: The present invention relates to compounds of the formula I, in which R1, R2, R4, R5, D1, D2, X1, X2, X3, A and B have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: June 26, 2002Date of Patent: March 16, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Manfred Schudok, Otmar Klingler, Hans-Peter Nestler, Hans Matter, Herman Schreuder, Hauke Szillat
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Publication number: 20040028716Abstract: This invention is directed to a stent for implantation in a blood vessel, wherein the stent is coated with Y-27632. The invention also provides a method of treating restenosis in a subject which comprises implanting in the subject a stent coated with Y-27632.Type: ApplicationFiled: June 12, 2003Publication date: February 12, 2004Inventors: Andrew R. Marks, Steven O. Marx
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Publication number: 20040006081Abstract: Compounds of formula (I), compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).Type: ApplicationFiled: December 10, 2002Publication date: January 8, 2004Inventors: Jeremy Burrows, Anne Cooper, John Cumming, Thomas McInally, Howard Tucker
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Publication number: 20040002494Abstract: The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.Type: ApplicationFiled: June 19, 2003Publication date: January 1, 2004Applicant: Pharmacia CorporationInventors: Michael S. South, Brenda Case, Danny J. Garland, Michael J. Hayes, Horng-Chih Huang, Wei Huang, Darin E. Jones, William L. Neumann, John J. Parlow, David B. Reitz, Melvin L. Rueppel, Ronald K. Webber
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Publication number: 20030236230Abstract: The present invention relates to compounds which comprise a 4-substituted piperidine ring linked to a substituted or unsubstituted hydrocarbyl ring.Type: ApplicationFiled: April 9, 2003Publication date: December 25, 2003Applicant: The Procter & Gamble CompanyInventors: Frank Hallock Ebetino, Xuewei Liu, Mark Gregory Solinsky, John August Wos
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Publication number: 20030225085Abstract: This invention provides neuroprotective pharmaceutical compositions comprising 2-pyridinamines. This invention also provides methods of using these compositions to prevent ischemic cell death, particularly neuronal cell death, and reduce the likelihood of neuronal cell death in a subject due to a traumatic event. Finally, this invention provides an apparatus for administering to a subject the instant pharmaceutical compositions.Type: ApplicationFiled: March 28, 2003Publication date: December 4, 2003Inventors: Elfrida R. Grant, Frank K. Brown, Robert Allan Zivin, Michael McMillian, Zhong Zhong, Daniel Benjamin
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Publication number: 20030216382Abstract: The present invention provides compounds of formula (I) 1Type: ApplicationFiled: February 10, 2003Publication date: November 20, 2003Inventors: Markus Boehringer, Bernd Michael Loeffler, Jens-Uwe Peters, Matthias Steger, Peter Weiss
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Publication number: 20030216393Abstract: Substituted 1-aminobutane-3-ol compounds, methods for producing them, pharmaceutical compounds containing them, and the use of substituted 1-aminobutane-3-ol compounds for producing pharmaceutical compounds.Type: ApplicationFiled: March 28, 2003Publication date: November 20, 2003Applicant: Gruenenthal GmbHInventors: Helmut Buschmann, Corinna Maul, Bernd Sundermann, Utz-Peter Jagusch, Michael Haurand, Boris Chizh
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Publication number: 20030216375Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: ApplicationFiled: September 17, 2002Publication date: November 20, 2003Inventors: Michael R. Palovich, Katherine L. Widdowson, Hong Nie
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Publication number: 20030212069Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: ApplicationFiled: March 5, 2003Publication date: November 13, 2003Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Marta Maria Pineiro-Nunez, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6638931Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: November 28, 2000Date of Patent: October 28, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
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Publication number: 20030181441Abstract: A compound of the formula 1Type: ApplicationFiled: August 12, 1999Publication date: September 25, 2003Inventors: KIM MCCLURE, MARK C. NOE, MICHAEL A. LETAVIC, LOUIS S. CHUPAK
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Patent number: 6608061Abstract: A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof: Ar1—S—R1—S—Ar2 wherein R1 represents a nonmetal bridging group; Ar1 and Ar2 independently represent a group selected from the group consisting of an aryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group and said aryl group may have one to three substituents other than hydroxyl group on its ring; and a heteroaryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group, and said heteroaryl group may have one to three substituents other than hydroxyl group on its ring.Type: GrantFiled: February 14, 2000Date of Patent: August 19, 2003Assignees: Kyoma Hakko Kogyo Co., Ltd., Fuji Photo Film Co., Ltd.Inventors: Yoshiyuki Yonetani, Takeshi Takahashi, Yuko Kanda, Tamio Mizukami, Tatsuya Tamaoki, Shun-ichi Ikeda, Masanobu Takashima, Naoki Asanuma, Tadashi Inaba, Hiroshi Takeuchi, Hiroshi Kawamoto, Yoshihisa Tsukada, Masato Satomura, Hiroshi Kitaguchi
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Publication number: 20030149020Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.Type: ApplicationFiled: May 13, 2002Publication date: August 7, 2003Inventors: Ulf Bremberg, Patrizia Caldirola, Annika J. Jensen, Gary Johansson, Andrew Mott, Lori Sutin, Jan Tejbrant
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Patent number: 6596716Abstract: The present invention relates to the potentiation of glutamate receptor function using certain 2-propane-sulphonamide derivatives. It also relates to novel 2-propane-sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.Type: GrantFiled: July 25, 2001Date of Patent: July 22, 2003Assignee: Eli Lilly and CompanyInventors: Tracey E McKennon, Paul L Ornstein, Edward C. R. Smith, Hamideh Zarrinmayeh, Dennis M Zimmerman
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Publication number: 20030109527Abstract: The invention relates to novel hydroxy diphenylurea sulfonamides, compositions and intermediates thereof. The hydroxy diphenylurea sulfonamides are useful in the treatment of disease states mediated by the chemokine, Interleukin-8.Type: ApplicationFiled: November 18, 2002Publication date: June 12, 2003Applicant: SmithKline Beecham CorporationInventors: Qi Jin, Brent W. McCleland, Michael R. Palovich, Katherine L. Widdowson
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Publication number: 20030105092Abstract: Prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: ApplicationFiled: September 26, 2002Publication date: June 5, 2003Inventors: Kimberley Q. Cameron, Hua Z. Ke, Bruce A. Lefker, Robert L. Rosati, David D. Thompson
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Patent number: 6531472Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, X and Y have the meanings defined in the specification. The compounds have histone deacetylase (HDAC) inhibitory activity which is useful in cancer treatment. Also provided is a process for making a compound of formula I by reacting a compound of formula III with a compound of formula IV wherein A is a displaceable group and PG is a protecting group.Type: GrantFiled: December 4, 2001Date of Patent: March 11, 2003Assignee: Hoffman-La Roche Inc.Inventors: Guy Georges, Adelbert Grossmann, Tim Sattelkau, Wolfgang Schaefer, Ulrich Tibes
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Patent number: 6531471Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: December 14, 2001Date of Patent: March 11, 2003Assignee: Synaptic Pharmaceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
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Patent number: 6525099Abstract: The present invention provides certain N-substituted sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.Type: GrantFiled: January 23, 2001Date of Patent: February 25, 2003Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6518310Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: March 16, 2001Date of Patent: February 11, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L Fedde, Carl R Illig, Thomas P. Markotan, Thomas P Stagnaro
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Patent number: 6500983Abstract: Novel hydroxamic acid compounds, e.g., of formula I, wherein R1, R2, R3 and R4 are as defined, are found to be useful as pharmaceuticals, e.g., for the suppression of TNF release and the treatment of autoimmune and inflammatory diseases, e.g., multiple sclerosis and rheumatoid arthritis. Methods of making the compounds, novel intermediates, and pharmaceutical compositions comprising the compounds are provided.Type: GrantFiled: October 9, 2001Date of Patent: December 31, 2002Assignee: Novartis AGInventors: Georg Kottirsch, Ulf Neumann
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Patent number: 6500825Abstract: This invention is related to substituted 2-aminoacetamides represented by Formula II: or a pharmaceutically acceptable salt or prodrug thereof, wherein: R1, R2, R3 and R4 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; R5, R6 and R7 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl, or R5, is defined as above, and R6 and R7 together with the nitrogen atom to which they are attached form a heterocycle, including piperidine, piperazine, morpholine; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR8, CH2, C(O), NR8C(O), C(O)NR8, SO, SO2 or a covalent bond; where R8 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl orType: GrantFiled: August 21, 2001Date of Patent: December 31, 2002Assignee: Euro-Celtique S.A.Inventors: Nancy C. Lan, Yan Wang, Sui Xiong Cai
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Publication number: 20020193365Abstract: Compounds of the formula 1Type: ApplicationFiled: April 25, 2002Publication date: December 19, 2002Applicant: WyethInventors: Gary P. Stack, Megan Tran
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Patent number: 6482827Abstract: A compound, which is an amine derivative of formula (I) wherein W is —CNHOH or —COOH: R1 and R2 are each hydrogen or an organic residue, R3 is an organic group, Q is a secondary or tertiary acyclic or cyclic amido group, and the pharmaceutically acceptable salts, solvates and hydrates thereof, are inhibitors of matrix metalloproteinases (MMPs) and of the release of tumor necrosis factor-alpha (TNF) from cells. They are therefore useful in the prevention, control and treatment of diseases in which MMPs or TNF are involved, especially tumoral and inflammatory diseases. Processes for their preparation and pharmaceutical compositions containing them are also described.Type: GrantFiled: March 10, 1999Date of Patent: November 19, 2002Assignee: Pharmacia & Upjohn S.p.A.Inventors: Marco Alpegiani, Pierluigi Bissolino, Francesca Abrate, Ettore Perrone, Riccardo Corigli, Daniela Jabes
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Patent number: 6479491Abstract: The present invention relates to compounds of formula (I), any of it enantiomers, or any mixture thereof, or a pharmaceutically acceptable acid addition salt thereof, wherein R1, R2, R3, R4, R11, R12, R13, R14 and R15 each independently are hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, nitro, cyano, amino, acyl, alkylamino, dialkylamino, aminocarbonyl, or acylamino; R5 is hydrogen, alkyl, alkoxyalkyl, or phenylalkyl; X is —CH2—Z—, Z—CH2—, NH—CO—, —CO—NH—, or —CH═CH—; wherein Z is O, S, CH2, or NH; Y is O, —CH2—W—, —W—CH2—; wherein W is O, or S; and n is 0, 1 or 2. The compounds are useful in the treatment of psychotic disorders.Type: GrantFiled: November 13, 2000Date of Patent: November 12, 2002Assignee: Neurosearch A/SInventors: Oskar Axelsson, Dan Peters, Jorgen Scheel-Kruger, Elsebet Ostergaard Nielsen
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Patent number: 6472423Abstract: The invention relates to a composition comprising of a first component (a) which is (R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide in the form of the free base, pharmaceutically acceptable salts and/or solvates thereof, and a second component (b) which is a monoamine oxidase (MAO) inhibitor in the form of the free base, pharmaceutically acceptable salts and/or solvates thereof, the preparation thereof, pharmaceutical formulations containing said composition, a kit containing said composition, use of and a method of treatment of affective disorders such as mood disorders and anxiety disorders with said composition.Type: GrantFiled: January 11, 2000Date of Patent: October 29, 2002Assignee: AstraZeneca ABInventors: Svante Ross, Seth-Olov Thorberg
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Publication number: 20020156064Abstract: This invention relates to certain benzenesulfonamides and their use as PDE7 inhibitorsType: ApplicationFiled: February 28, 2002Publication date: October 24, 2002Applicant: SmithKline Beecham CorpInventors: Kelly M. Aubart, Siegfried B. Christensen, Jack D. Leber
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Patent number: 6455569Abstract: The use of Matrix Metalloproteinase Inhibitors in the prevention or treatment of connective tissue softening and also for the maintenance of sutures in such connective tissues. The connective tissue may be a tendon, ligament or cartilage.Type: GrantFiled: August 17, 2001Date of Patent: September 24, 2002Assignee: Renovo LTDInventor: Mark W. J. Ferguson
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Patent number: 6451791Abstract: An amidoaromatic ring sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a contemplated amidoaromatic ring sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 4, 1999Date of Patent: September 17, 2002Assignee: Monsanto CompanyInventors: Robert M. Heintz, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard, S. Zaheer Abbas
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Patent number: 6451792Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.Type: GrantFiled: March 20, 2001Date of Patent: September 17, 2002Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
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Publication number: 20020082249Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.Type: ApplicationFiled: November 30, 2001Publication date: June 27, 2002Applicant: Vertex Pharmaceuticals IncorporatedInventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Andrew Spaltenstein, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski
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Patent number: 6407120Abstract: The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.Type: GrantFiled: January 28, 2000Date of Patent: June 18, 2002Assignee: Pfizer Inc.Inventors: Philip A. Carpino, Marlys Hammond, Richard F. Hank
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Publication number: 20020068737Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: ApplicationFiled: December 14, 2001Publication date: June 6, 2002Applicant: Synaptic Pharamceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski