1,3-diazole Ring (including Hydrogenated) Patents (Class 544/139)
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Patent number: 6566509Abstract: Disclosed are multibinding compounds which include macrolide antibiotics, aminoglycosides, lincosamides, oxazolidinones, streptogramins, tetracycline and/or other compounds at which bind to bacterial ribosomal RNA and/or to one or more proteins involved in ribosomal protein synthesis in the bacterium, which are useful in treating bacterial infections. The compounds adversely affect protein expression and have an antibacterial effect. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is macrolide antibiotic, aminoglycoside, lincosamide, oxazolidinone, streptogramin, tetracycline or other compound which binds to bacterial ribosomal RNA and/or one or more proteins involved in ribosomal protein synthesis in the bacterium.Type: GrantFiled: June 8, 1999Date of Patent: May 20, 2003Assignee: Theravance, Inc.Inventors: John H. Griffin, John L. Pace
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Patent number: 6562817Abstract: The present invention provides a compound of the formula (I): wherein A ring, B ring and C ring are each independently optionally substituted aromatic carbocycle or optionally substituted 5- or 6-membered heterocycle which may fuse with benzene ring, W1, W2 and/or W3 represents a bond when A ring, B ring and/or C ring is optionally substituted 5-membered heterocycle, X is —O—, —NR1— wherein R1 is hydrogen, lower alkyl etc. or the like, Y is hydrogen, lower alkyl, lower alkenyl or the like, one of V1 and V2 is a bond, and the other is a bond, —O— or the like, and a pharmaceutical composition comprising the same.Type: GrantFiled: July 21, 2000Date of Patent: May 13, 2003Assignee: Shionogi & Co., Ltd.Inventors: Norihiko Tanimoto, Yasushi Hasegawa, Nobuhiro Haga
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Publication number: 20030083352Abstract: The invention provides a method for synthesis of compounds of formula 1Type: ApplicationFiled: July 25, 2002Publication date: May 1, 2003Applicant: Pfizer Inc.Inventor: Christopher J. Helal
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Patent number: 6541499Abstract: The invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts, as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula (I), and the use of the compounds of formula (I) as thrombin inhibitors.Type: GrantFiled: January 21, 2000Date of Patent: April 1, 2003Assignee: Eli Lilly and CompanyInventors: Jolie A Bastian, Nickolay Y Chirgadze, Michael L Denney, Matthew J Fisher, Robert J Foglesong, Richard W Harper, Mary G Johnson, Valentine J Klimkowski, Ho-Shen Lin, Michael P Lynch, Jefferson R McCowan, Shawn C Miller, Jeffrey T Mullaney, Michael E Richett, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Jennifer M Tinsley, Michael R Wiley, Minsheng Zhang
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Publication number: 20030055055Abstract: The present invention relates to novel benzimidazole derivatives, pharmaceutical composition containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABA receptor complex, and in particular for inducing and maintaining anesthesia, sedation and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.Type: ApplicationFiled: December 12, 2001Publication date: March 20, 2003Inventors: Lene Teuber, Frank Watjen
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Publication number: 20030055057Abstract: The invention relates to novel benzimidazole derivatives with general formula I, whereby radicals R1, R2, R3, A, B and Y have the meanings that are indicated in the description and the claims, the use of these compounds for the production of a pharmaceutical agent for treating and for preventing diseases that are associated with microglia activation, as well as pharmaceutical preparations that contain these compounds.Type: ApplicationFiled: July 5, 2002Publication date: March 20, 2003Applicant: Schering AGInventors: Thorsten Blume, Wolfgang Halfbrodt, Joachim Kuhnke, Ursula Moenning, Herbert Schneider, Bernd Elger
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Publication number: 20030050311Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.Type: ApplicationFiled: September 3, 2002Publication date: March 13, 2003Inventors: Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, David Lee Varie
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N,N'-disubstituted benzimidazolone derivatives with affinity at the serotonin and dopamine receptors
Publication number: 20030027823Abstract: A compound of formula (I) 1Type: ApplicationFiled: August 21, 2001Publication date: February 6, 2003Inventors: Enzo Cereda, Luciano Maiocchi, Alessandro Brambilla, Ettore Giraldo, Eugenia Monferini, Giovanni Battista Schiavi -
Patent number: 6511978Abstract: The present invention relates to a novel pyrrole derivative which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof; to a process for preparation of said compound; and to a pharmaceutical composition such as anti-cancer composition, etc. comprising said compound as an active ingredient together with pharmaceutically acceptable carrier.Type: GrantFiled: October 11, 2001Date of Patent: January 28, 2003Assignee: LG Life Sciences, Ltd.Inventors: Jong-Sung Koh, Hyun-Il Lee, You-Seung Shin, Hak-Joong Kim, Jin-Ho Lee, Jong-Hyun Kim, Hyun-Ho Chung, Shin-Wu Jeong, Tae-Saeng Choi, Jung-Kwon Yoo, Chung-Mi Kim, Kwi-Hwa Kim, Sun-Hwa Lee, Sang-Kyun Lee
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Publication number: 20030018022Abstract: Compounds, compositions and methods are provided that are useful in the treatment of chemokine receptor-mediated conditions and diseases. In particular, the invention provides compounds which modulate CCR4 function or a CCR4-mediated response. The subject compounds and compositions are useful for the treatment or prevention of inflammatory conditions and diseases.Type: ApplicationFiled: May 22, 2002Publication date: January 23, 2003Applicant: Tularik Inc.Inventors: Tassie Collins, Hossen Mahmud, Jonathan Houze, Alan Xi Huang, Julio C. Medina, Xuemei Wang, Feng Xu, Qingge Xu, Liusheng Zhu
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Patent number: 6506738Abstract: The present invention concerns antiviral compounds, their compositions, and use in the treatment of viral infections. More particularly, the invention provides benzimidazolone derivatives for the treatment of respiratory syncytial virus infection.Type: GrantFiled: September 14, 2001Date of Patent: January 14, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Kuo-Long Yu, Rita Civiello, Keith Combrink, Hatice Belgin Gulgeze, Bradley C. Pearce, Xiangdong Wang, Nicholas A. Meanwell, Yi Zhang
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Patent number: 6503905Abstract: The present invention relates to compounds of the formula I, wherein Z1, Z2, X, Q, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.Type: GrantFiled: August 6, 1999Date of Patent: January 7, 2003Assignee: Pfizer IncInventors: Spiros Liras, Martin P. Allen, Barbara E. Segelstein
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Publication number: 20030004342Abstract: The present invention is directed to imidazolyl derivatives of formula (II), wherein the variables are defined in the specification, which are useful as prenyl transeferase inhibitors.Type: ApplicationFiled: May 20, 2002Publication date: January 2, 2003Applicant: Biomeasure, Inc., a Massachusetts corporationInventors: Zheng Xin Dong, Yeelana Shen
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Publication number: 20020198378Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: ApplicationFiled: December 11, 2001Publication date: December 26, 2002Applicant: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 6492394Abstract: A compound of the Formula (I): wherein Z, R1, R, and Ar2 are as defined in the specification. This invention also relates to sulfonamide compounds of the Formula (I) that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use, and methods for preparing the compounds.Type: GrantFiled: December 22, 1999Date of Patent: December 10, 2002Assignee: Syntex (U.S.A.) LLCInventors: Roland Joseph Billledeau, Chris Allen Broka, Jeffrey Allen Campbell, Jian Jeffrey Chen, Sharon Marie Dankwardt, Nancy Delaet, Leslie Ann Robinson, Keith Adrian Murray Walker
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Publication number: 20020169314Abstract: The present invention provides a novel sulfonamide derivative of general formula (I) useful as an inhibitor of matrix metalloproteinase (MMP), its isomers, pharmaceutically acceptable salts thereof and a process for preparing the same. Since the sulfonamide derivatives of the present invention selectively inhibit MMP activity in vitro, the MMP inhibitors comprising the sulfonamide derivatives as an effective ingredient can be practically applied for the prevention and treatment of all sorts of diseases caused by overexpression and overactivation of MMP.Type: ApplicationFiled: December 6, 2001Publication date: November 14, 2002Inventors: Young-Jun Park, Hae-Young Bae, Ji-Uk Yoo, Myeong-Yun Chae, Sang-Hyun Paek, Hye-Kyung Min, Hyun-Gyu Park, Choon-Ho Ryu, Kyung-Chul Kim, Jeoung-Wook Lee
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Publication number: 20020161022Abstract: Indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating, e.g., kinases-dependent diseases to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: ApplicationFiled: January 18, 2001Publication date: October 31, 2002Inventors: Siegfried Heinz Reich, Ted Michael Bleckman, Susan Elizabeth Kephart, William Henry Romines, Michael B. Wallace
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Patent number: 6472414Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) —O—; or (3) B is: and wherein L2, L1, R1, R2, R3, R3′, R3a, R3b, R4, R4′, R5, X, are as defined herein.Type: GrantFiled: May 18, 1999Date of Patent: October 29, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
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Patent number: 6472526Abstract: The present invention relates to a novel imidazole derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof, in which A, n1 and Y are defined in the specification; to a process for preparation of the compound of formula (1); to intermediates which are used in the preparation of the compound of formula (1): and to a pharmaceutical composition comprising the compound of formula (1) as an active ingredient.Type: GrantFiled: December 3, 2001Date of Patent: October 29, 2002Assignee: LG Chemical Ltd.Inventors: Hyun Il Lee, Jong Sung Koh, Jin Ho Lee, Won Hee Jung, You Seung Shin, Hyun Ho Chung, Jong Hyun Kim, Seong Gu Ro, Tae Saeng Choi, Shin Wu Jeong, Tae Hwan Kwak, In Ae Ahn, Hyun Sung Kim, Sun Hwa Lee, Kwi Hwa Kim, Jung Kwon Yoo
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Patent number: 6469002Abstract: Disclosed are novel compounds and a method of treating inflammatory diseases. The method comprises administering to an individual in need an effective amount of an imidazolidine compound represented by Structural Formula (I): and physiologically or pharmaceutically acceptable salts thereof.Type: GrantFiled: April 19, 2001Date of Patent: October 22, 2002Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Hiroki Sone, Osamu Kotera, Rie Komatsu, Gregory J. LaRosa, Jay R. Luly
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Patent number: 6465484Abstract: The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tryrosine kinase-dependent diseases/conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.Type: GrantFiled: February 28, 2001Date of Patent: October 15, 2002Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, Randall W. Hungate, April M. Cunningham, Timothy J. Koester
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Publication number: 20020137931Abstract: Compounds of formula I 1Type: ApplicationFiled: January 11, 2002Publication date: September 26, 2002Inventors: Yousseff L. Bennani, Ramin Faghih, Wesley J. Dwight, Anil Vasudevan, Scott E. Conner
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Patent number: 6448281Abstract: A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl, cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (CType: GrantFiled: July 3, 2001Date of Patent: September 10, 2002Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, James Gillard, George Kukolj, Volkhard Austel
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Patent number: 6437121Abstract: The present invention is directed to new cationic lipids and intermediates in their synthesis that are useful for transfecting nucleic acids or peptides into prokaryotic or eukaryotic cells. The lipids comprise one or two substituted histidine residues, or similar compounds, linked to a lipophilic moiety. The lipids form a complex when mixed with polyanions such as nucleic acids or peptides. The complexes permit efficient transfer of polyanions into cells, usually without significant toxicity to the cells.Type: GrantFiled: April 25, 2000Date of Patent: August 20, 2002Assignee: ISIS Pharmaceuticals, Inc.Inventors: Kuei-Ying Lin, Mark D. Mattuecci
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Publication number: 20020107274Abstract: The present invention relates to 3-(2,4-dimethylthiazol-5-yl)indeno[1,2-c]pyrazol-4-ones of formula 1Type: ApplicationFiled: November 30, 2001Publication date: August 8, 2002Inventor: Eddy W. Yue
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Publication number: 20020099208Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.Type: ApplicationFiled: November 16, 2001Publication date: July 25, 2002Inventors: Kuo-Long Yu, Rita L. Civiello, Keith D. Combrink, Hatice Belgin Gulgeze, Ny Sin, Xiangdong Wang, Nicholas Meanwell, Brian Lee Venables, Yi Zhang, Bradley C. Pearce, Zhiwei Yin, Jan Willem Thuring
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Patent number: 6423712Abstract: The present invention relates to imidazolidine compounds of the formula I, The compounds of the formula I are valuable pharmaceutical active compounds, which are suitable, for example, for the therapy and prophylaxis of inflammatory disorders, for example of rheumatoid arthritis, or of allergic disorders. The compounds of the formula I are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the therapy or prophylaxis of illnesses which are caused by an undesired extent of leucocyte adhesion and/or leucocyte migration or are associated therewith, or in which cell-cell or cell-matrix interactions which are based on interactions of VLA-4 receptors with their ligands play a part.Type: GrantFiled: September 18, 1998Date of Patent: July 23, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Volkmar Wehner, Hans Ulrich Stilz, Wolfgang Schmidt, Dirk Seiffge
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Patent number: 6420555Abstract: The present invention is directed to imidazolyl derivatives of formula (I), wherein the variables are defined in the specification, which are useful as prenyl transferase inhibitors.Type: GrantFiled: May 22, 2001Date of Patent: July 16, 2002Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques, S.A.S.Inventors: Zheng Xin Dong, Yeelana Shen
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Patent number: 6417186Abstract: This invention relates to compounds which are generally IP receptor modulators, particularly IP receptor antagonists, and which are represented by Formula I: wherein A, R1 and R2 are as defined in the specification; and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: November 13, 2001Date of Patent: July 9, 2002Assignee: Syntex (U.S.A.) LLCInventor: Alam Jahangir
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Patent number: 6414145Abstract: The present invention relates to inhibitors of ras farnesylation of Formula (I), wherein T is of Formula (1) or (2) or (3); A is aryl or heteroaryl; B is aryl or heteroaryl; X and Y represent hydrogen, or both X and Y can represent a single bond (so as to form a double bond); R1 represents a group of Formula (II) or (III), the group of Formula (II) or Formula (III) (having L or D configuration at the chiral alpha carbon in the corresponding free amino acid); R2 represents hydrogen, aryl or heteroaryl; Z represents a direct bond, methylene, ethylene, vinylene, oxy, —CH2—O— or —O—CH2—; and R3—R4, p and r are as defined in the specification or a pharmaceutically-acceptable salt, prodrug or solvate thereof. Processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.Type: GrantFiled: July 28, 1999Date of Patent: July 2, 2002Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventors: Francis Thomas Boyle, Gareth Morse Davies, James Michael Wardleworth, Jean-Claude Arnould
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Patent number: 6407105Abstract: Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.Type: GrantFiled: September 26, 2000Date of Patent: June 18, 2002Assignee: The Procter & Gamble CompanyInventors: James C. Quada, Jr., Joseph K. Agyin, James Berger Camden
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Patent number: 6403791Abstract: A compound of the formula wherein R1 is C1-3 alkyl optionally substituted with one or more fluorines; R2 is C1-6 alkyl, cycloalkyl or NR4R5; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) NR4R5 is a nitrogen-containing heterocyclic ring; R6 is C1-3 alkyl; and R7 and R8, which are the same or different, each represents C1-3 alkyl, halogen, CF3 or CN; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: February 9, 2001Date of Patent: June 11, 2002Assignee: Darwin Discovery, Ltd.Inventors: Hazel Joan Dyke, Alan Findlay Haughan, Christopher Lowe, George Martin Buckley, Richard John Davenport, Andrew Sharpe, Hannah Jayne Kendall, Verity Margaret Sabin, John Gary Montana, Catherine Louise Picken
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Patent number: 6399782Abstract: Novel benzimidazole compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is describedType: GrantFiled: April 11, 2000Date of Patent: June 4, 2002Assignee: Metabasis Therapeutics, Inc.Inventors: Srinivas Rao Kasibhatla, K. Raja Reddy, Mark D. Erion, Qun Dang, Gerard R. Scarlato, M. Rami Reddy
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Publication number: 20020065274Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.Type: ApplicationFiled: November 28, 2001Publication date: May 30, 2002Inventors: Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck,, David Lee Varie
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Patent number: 6395724Abstract: Disclosed are multibinding compounds which inhibit cyclooxygenase-2 (COX-2), an enzyme which catalyzes the first committed step in the biosynthesis of prostaglandins. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to COX-2. The multibinding compounds of this invention are useful in the treatment inflammation, pain, fever and the like.Type: GrantFiled: June 7, 1999Date of Patent: May 28, 2002Assignee: Advanced Medicine, Inc.Inventors: J. Kevin Judice, Deborah L. Higgins, John H. Griffin
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Patent number: 6395897Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.Type: GrantFiled: November 5, 1999Date of Patent: May 28, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Michel J. Emmanuel, Leah L. Frye, Denice M. Spero, David S. Thomson, Yancey D. Ward
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Publication number: 20020061913Abstract: The present invention provides compounds of formula (I): 1Type: ApplicationFiled: June 22, 2001Publication date: May 23, 2002Inventors: Christopher John Urch, Terence Lewis, Raymond Leo Sunley, Roger Salmon, Christopher Richard Ayles Godfrey, Christopher Ian Brightwell, Matthew Brian Hotson
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Publication number: 20020052368Abstract: Novel compounds of formula I: 1Type: ApplicationFiled: March 26, 2001Publication date: May 2, 2002Inventors: Charles K. Marlowe, Kim A. Kane-Maguire, Bing-Yan Zhu, Robert M. Scarborough
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Publication number: 20020052343Abstract: The present invention provides novel compounds of Formula I: 1Type: ApplicationFiled: December 14, 2000Publication date: May 2, 2002Inventors: Darin Arthur Allen, Danny Peter Claude McGee, Jeffrey R. Spencer
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Publication number: 20020049316Abstract: The present invention provides compounds of formula (I) which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia or malignancy; and metabolic bone disease therewith.Type: ApplicationFiled: December 17, 2001Publication date: April 25, 2002Inventors: Stacie Marie Halbert, Evelyne Michaud, Scott Kevin Thompson, Daniel Frank Veber
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Patent number: 6376666Abstract: 2-mercaptobenzimidazole derivatives of the general formula wherein: N=0,2,3; R-hydrogen atom, aralkyls; R1-lower alkyls, alkenyls, dialkylamino, a saturated amine monocyclic residue which may contain an additional heteroatom; R2 and R3 are equal or different and stand for hydrogen atoms, lower alkyls, alkoxy in various positions, and their pharmaceutically acceptable salts, according to the results of pharmacological research study exhibit a pronounced anxiolytic, sedative, antiischemia and antiarrhythmia effect and have certain advantages over popular clinic preparations. These can find a wide variety of application for treatment of patients suffering from various mental derangements and heart ischemia.Type: GrantFiled: December 9, 1996Date of Patent: April 23, 2002Assignee: Nauchno-Issledovatelsky Institut Farmakologii Rossiiskoi Akademii Meditsinskikh NaukInventors: Sergei Borisovich Seredenin, Jury Alexeevich Blednov, Vladimir Leonidovich Saveliev, Tatyana Yakovlevna Mozhaeva, Eleonora Konstantinovna Orlova, Khagani Sabir Ogly Ragimov, Milada Alnordovna Yarkova, Gennady Georgievich Chichkanov, Natalia Veniaminova Kaverina, Iosif Borisovich Tsorin, Galina Jurievna Kirsanova, Grigory Georgievich Neznamov
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Publication number: 20020044963Abstract: Novel 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: ApplicationFiled: December 15, 2000Publication date: April 18, 2002Inventor: John J. Gaudino
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Patent number: 6369034Abstract: The present invention provides compounds of Formula (I). The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula (I).Type: GrantFiled: September 13, 2000Date of Patent: April 9, 2002Assignee: Warner-Lambert CompanyInventors: Annette Marian Doherty, James Stanley Kaltenbronn, Daniele Marie Leonard, Dennis Joseph McNamara, John Quin, III
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Patent number: 6365584Abstract: Arylsulphonamide-substituted benzimidazole derivatives of formula (I) having tryptase-inhibiting activity. Exemplary are: 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethylaminoethyl)-benzenesulphonylamino]-benzimidazole; 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethlylaminoethyl)-benzylsulfonylamino]-benzimidazole; and, 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(3-diethylaminopropyl)-benzenesulphonylamino]-benzimidazole.Type: GrantFiled: September 21, 2000Date of Patent: April 2, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Ralf Anderskewitz, Christine Braun, Hans Briem, Bernd Disse, Christoph Hoenke, Hans Michael Jennewein, Georg Speck
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Patent number: 6362183Abstract: An aromatic sulfonyl alpha-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: June 4, 1999Date of Patent: March 26, 2002Assignee: G. D. Searle & CompanyInventors: 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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Patent number: 6358885Abstract: This invention relates to certain phenylheterocyclic compounds, herbicidal compositions thereof and a method for their use as general and selective preemergent or postemergent herbicides or plant growth regulants.Type: GrantFiled: April 15, 1999Date of Patent: March 19, 2002Assignees: Mississippi State University, Research Technology Corporation Mississippi StateInventors: Thomas P. Selby, Thomas M. Stevenson
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Patent number: 6358949Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: A, B, C and D are N or CH; X is a bond or (un)substituted CH2; R1 is lower alkenyl or (un)substituted lower alkyl; R3 is lower alkyl; and R2, R4, R5, and R6 are variables defined herein; which compounds are useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatroy disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility or glaucoma, or for the increase of permeability of blood-brain barrier, pain, asthma, and rhinitis.Type: GrantFiled: March 31, 2000Date of Patent: March 19, 2002Assignee: Neurogen CorporationInventors: Robert W. DeSimone, Alan Hutchison, Kenneth Shaw, George D. Maynard, John M. Peterson, Richard Lew, Harry L. Brielmann
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Patent number: 6352985Abstract: A benzimidazole compound represented by the formula (I): wherein R3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable salts. Because of their blood sugar-depressing effect or PDE5 inhibitory effect, these compounds or salts thereof are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin resistance, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, or hypertension; or stenocardia, hypertension, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, atherosclerosis, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, diabetic complications, nephritis, cancerous cachexia, or restenosis after PTCA.Type: GrantFiled: January 28, 2000Date of Patent: March 5, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Noritsugu Yamasaki, Takafumi Imoto, Yoshiyuki Murai, Takahiro Hiramura, Teruo Oku, Kouzou Sawada
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Publication number: 20020019395Abstract: Novel compounds of general formula I: 1Type: ApplicationFiled: February 1, 2001Publication date: February 14, 2002Inventors: Bing-Yan Zhu, Robert M. Scarborough
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Publication number: 20010056090Abstract: One aspect of the present invention relates to novel heterocyclic compounds comprising urea functionality. A second aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as ligands for various cellular receptors, including opioid receptors, other G-protein-coupled receptors and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as analgesics.Type: ApplicationFiled: February 23, 2001Publication date: December 27, 2001Inventors: Brian M. Aquila, Gregory D. Cuny, James R. Hauske, Liming Shao, Xinhe Wu