Ring Chalcogen In The Additional Hetero Ring Patents (Class 544/374)
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Patent number: 7419980Abstract: The present invention is directed to fused-aryl and heteroaryl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: GrantFiled: October 12, 2004Date of Patent: September 2, 2008Assignee: WyethInventors: Eugene John Trybulski, Paige Erin Mahaney, Lori Krim Gavrin, Joseph Peter Sabatucci, Gary Paul Stack
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Patent number: 7417042Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.Type: GrantFiled: August 8, 2005Date of Patent: August 26, 2008Assignee: Proteolix, Inc.Inventors: Mark S. Smyth, Guy J. Laidig
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Publication number: 20080176841Abstract: Provided herein are novel epoxide inhibitors of cysteine proteases, compositions comprising the epoxide inhibitors, and packaged pharmaceuticals. Also provided are methods of inhibiting a papain-family cysteine protease and methods of treating or preventing a disease by administering a composition containing an epoxide inhibitor of the invention. The compositions may be administered in combination with another therapeutic agent.Type: ApplicationFiled: June 13, 2007Publication date: July 24, 2008Applicant: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITYInventors: Matthew S. Bogyo, Amir M. Sadaghiani, Steven Verhelst
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Patent number: 7351822Abstract: Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovascular disorders.Type: GrantFiled: March 18, 2004Date of Patent: April 1, 2008Assignee: Eli Lilly and CompanyInventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson, Peter Robert Guzzo, Michael John Mayer
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Patent number: 7312211Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases.Type: GrantFiled: August 26, 2004Date of Patent: December 25, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, Yancey David Ward
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Patent number: 7294628Abstract: The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4) alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents the aromatic group 1,3-thiazol-2-yl of formula: Preparation process and therapeutic application.Type: GrantFiled: June 5, 2003Date of Patent: November 13, 2007Assignee: Sanofi-AventisInventors: Françoise Bono, Michaël Bosch, Victor Dos Santos, Jean-Marc Herbert, Dino Nisato, Bernard Tonnerre, Jean Wagnon
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Patent number: 7285664Abstract: A compound having a formula selected from the group consisting of wherein the substituents are as defined in the specification. The compounds are useful as intermediates in the preparation of compounds of formula (I), which are useful for inhibiting NO synthase and regenerate antioxidants.Type: GrantFiled: June 8, 2005Date of Patent: October 23, 2007Assignee: S.C.R.A.S. Societe de Conseils de Recherches et d'Applications ScientifiquesInventors: Jeremiah Harnett, Michel Auguet
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Patent number: 7276499Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.Type: GrantFiled: January 13, 2006Date of Patent: October 2, 2007Assignee: Immunogen Inc.Inventors: Ravi V. J. Chari, Walter A. Blattler
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Patent number: 7253172Abstract: Compounds having Formula I, including pharmaceutically acceptable salts and prodrugs thereof: (I) are inhibitors of the dipeptidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of DP-IV mediated diseases and conditions, such as non-insulin dependent diabetes mellitusType: GrantFiled: June 19, 2002Date of Patent: August 7, 2007Assignee: Merck & Co., Inc.Inventors: Linda Brockunier, Emma Parmee, Ann E. Weber
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Patent number: 7250389Abstract: Disclosed are novel compounds useful for prevention or control of diseases derived from fungi, a process for producing the same, and novel antifungal agents using the novel compounds. The compounds useful for prevention and treatment of diseases derived from fungi according to the present invention include novel compounds represented by formula (I). The compounds represented by formula (I) have potent antifungal activity against diseases derived from fungi, and do not have phytotoxicity to mammals and agricultural and garden plants, from which diseases should be eliminated, and, even when applied to agricultural and garden plants, have high photostability.Type: GrantFiled: February 8, 1999Date of Patent: July 31, 2007Assignee: Meiji Seika Kaisha, Ltd.Inventors: Osamu Sakanaka, Koichi Mitomo, Takayoshi Tamura, Yasushi Murai, Katsuharu Iinuma, Takeshi Teraoka, Kikuko Kuzuhara, Haruki Mikoshiba, Makoto Taniguchi
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Publication number: 20070173501Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: January 23, 2007Publication date: July 26, 2007Applicant: ALLERGAN, INC.Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone
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Publication number: 20070173511Abstract: The present invention relates to compounds of formula I wherein R1 to R3 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: ApplicationFiled: January 16, 2007Publication date: July 26, 2007Inventors: Matthias Nettekoven, Olivier Roche
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Publication number: 20070167436Abstract: The present invention relates to compounds of formula I wherein s, R1a and R1 to R3 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: ApplicationFiled: January 4, 2007Publication date: July 19, 2007Inventors: Matthias Nettekoven, Jean-Marc Plancher, Olivier Roche, Tadakatsu Takahashi, Sven Taylor
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Patent number: 7241764Abstract: Compounds of general formula:[Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared.Type: GrantFiled: November 5, 2003Date of Patent: July 10, 2007Assignee: AstraZeneca ABInventors: William Brown, Andrew Griffin
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Patent number: 7232818Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.Type: GrantFiled: April 14, 2005Date of Patent: June 19, 2007Assignee: Proteolix, Inc.Inventors: Mark S. Smyth, Guy J. Laidig, Ronald T. Borchardt, Barry A. Bunin, Craig M. Crews, John H. Musser
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Patent number: 7217819Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.Type: GrantFiled: August 16, 2005Date of Patent: May 15, 2007Assignee: ImmunoGen, Inc.Inventors: Ravi V. J. Chari, Walter A. Blättler
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Patent number: 7196106Abstract: The present invention addresses substituted cyanothiophene derivatives of the formula I: as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are glucagon antagonists. The compounds block the action of glucagon at its receptor and thereby decrease the levels of plasma glucose providing a treatment of diabetes.Type: GrantFiled: November 4, 2003Date of Patent: March 27, 2007Assignee: Merck & Co., IncInventors: Joseph L. Duffy, Elizabeth Louise Campbell, Brian A. Kirk, Rui Liang, James R. Tata, Kevin T. Chapman, Zenon Konteatis
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Patent number: 7173129Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.Type: GrantFiled: June 7, 2004Date of Patent: February 6, 2007Assignee: Athero Genics, Inc.Inventors: Kimberly J. Worsencroft, Liming Ni, Zhihong Ye, Charles Q. Meng, M. David Weingarten, Jacob E. Simpson, James A. Sikorski
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Patent number: 7141570Abstract: The present invention provides antibacterial agents having the formula I described herein.Type: GrantFiled: November 19, 2003Date of Patent: November 28, 2006Assignee: Pharmacia & Upjohn CompanyInventors: Jackson Boling Hester, Jr., Christina R. Harris
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Patent number: 7119203Abstract: This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.Type: GrantFiled: April 25, 2003Date of Patent: October 10, 2006Assignee: Pharmacia CorporationInventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, David L. Brown, Jeffery N. Carroll, Yiyuan Chen, Yvette M. Fobian, John N. Freskos, Alan F. Gasiecki, Margaret L. Grapperhaus, Robert M. Heintz, Susan L. Hockerman, Darren J. Kassab, Ish K. Khanna, Stephen A. Kolodziej, Mark A. Massa, Joseph J. McDonald, Brent V. Mischke, Deborah A. Mischke, Patrick B. Mullins, Mark A. Nagy, Monica B. Norton, Joseph G. Rico, Michelle A. Schmidt, Nathan W. Stehle, John J. Talley, William F. Vernier, Clara I. Villamil, Lijuan J. Wang, Thomas A. Wynn
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Patent number: 7115610Abstract: Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, diabetes, and myocardial infarction.Type: GrantFiled: December 17, 2004Date of Patent: October 3, 2006Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Kenneth Rehder, Jeffrey Zablocki
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Patent number: 7105507Abstract: The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.Type: GrantFiled: May 16, 2001Date of Patent: September 12, 2006Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain
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Patent number: 7026323Abstract: Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.Type: GrantFiled: September 22, 2004Date of Patent: April 11, 2006Assignee: Schering AktiengesellschaftInventors: Judi A. Bryant, Brad O. Buckman, Imadul Islam, Raju Mohan, Michael M. Morrissey, Guo Ping Wei, Wei Xu, Shendong Yuan
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Patent number: 7019007Abstract: The invention provides compounds of Formula (I): wherein: R1–R4, A, D, and L have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.Type: GrantFiled: November 27, 2002Date of Patent: March 28, 2006Assignee: Syntex (U.S.A.) LLCInventors: Daisy Joe Du Bois, Beihan Wang
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Patent number: 7008942Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.Type: GrantFiled: October 15, 2003Date of Patent: March 7, 2006Assignee: Immunogen, Inc.Inventors: Ravi V. J. Chari, Walter A. Blättler
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Patent number: 6995269Abstract: Compounds of formula IIA and IIB are novel guanidine compounds where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.Type: GrantFiled: March 4, 2003Date of Patent: February 7, 2006Assignee: Chiron CorporationInventors: Paul A. Renhowe, Daniel Chu, Rustum S. Boyce, David Duhl
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Patent number: 6949538Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: GrantFiled: July 17, 2003Date of Patent: September 27, 2005Assignees: Cytokinetics, Inc., Smithkline Beecham CorporationInventors: Andrew McDonald, Gustave Bergnes, David J. Morgans, Jr., Dashyant Dhanak, Steven David Knight
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Patent number: 6936611Abstract: Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovascular disorders.Type: GrantFiled: January 12, 2004Date of Patent: August 30, 2005Assignee: Eli Lilly and CompanyInventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson, Peter Robert Guzzo, Michael John Mayer
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Patent number: 6936715Abstract: Compounds of the formulae wherein the substituents are as defined in the specification useful for inhibiting NO synthase and regenerate antioxidants.Type: GrantFiled: March 15, 2001Date of Patent: August 30, 2005Assignee: Societe de Conseils de Recherches et d'Applications ScientifiquesInventors: Jeremiah Harnett, Michel Auguet
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Patent number: 6927217Abstract: The present invention relates to novel dihydropyrones of Formula I wherein X is NH or NR8, which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS.Type: GrantFiled: October 16, 2002Date of Patent: August 9, 2005Assignee: Warner-Lambert CompanyInventors: Frederick Earl Boyer, Jr., John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Elizabeth Ann Lunney, Alexander Pavlovsky, Vara Prasad Venkata Nagendra Josyula, Bradley Dean Tait
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Patent number: 6916926Abstract: (±) 3-(4-Phenyl-1-piperazinyl)-1,2-propanediol cyclic acetals, a process for the optical resolution thereof and their use as intermediates for the preparation of (?) 3-(4-phenyl-1-piperazinyl)-1,2-propanediol (levodropropizine) and salts thereof are described herein.Type: GrantFiled: July 18, 2001Date of Patent: July 12, 2005Assignee: DOMPE S.p.A.Inventors: Marcello Allegretti, Maria Candida Cesta, Roberto Curti, Luca Nicolini
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Patent number: 6906073Abstract: The invention provides compounds of Formula (I): wherein: R1-R4, A, L, and X have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.Type: GrantFiled: November 29, 2002Date of Patent: June 14, 2005Assignee: Roche Palo Alto LLCInventors: Daisy Joe Du Bois, Denis John Kertesz, Eric Brian Sjogren, David Bernard Smith, Beihan Wang
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Patent number: 6906191Abstract: Provided are a borosuccinimide compound obtained through reaction of (a) a succinic acid/anhydride substituted with an alkyl or alkenyl group having a number-average molecular weight of from 200 to 5,000, (b) a polyalkylene-polyamine of which at least 5 mol % has a terminal cyclic structure, and (c) a boron compound; and a succinimide compound obtained through reaction of (A) a succinic acid/anhydride substituted with an alkyl or alkenyl group having a molecular weight of from 200 to 5,000, with (D) a hydrocarbon-substituted polyalkylene-polyamine. These compounds are stable even at high temperatures and have good high-temperature detergency, and they are useful for ashless detergent dispersants having the ability to disperse fine particles. Also provided are a mixture of any of these compounds and a specific ester derivative; a lubricant additive and a fuel oil additive comprising the mixture as the essential ingredient; and a lubricant and a fuel oil composition containing the additive.Type: GrantFiled: December 26, 2000Date of Patent: June 14, 2005Assignee: Idemitsu Kosan Co., Ltd.Inventors: Hiroaki Koshima, Izumi Terada
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Patent number: 6900213Abstract: The invention relates to bisaryl derivatives of the formula I, wherein (R,R) is selected from (H,H), O, (H,CH3), (H,OH) and (H,CN); Ar is substituted phenyl and A is a group of formula II, III, IV or V: An example is (3S,6S)-1-N-(7-phenylheptyl)-3-(4-(3,4,5-trimethoxyphenyl)benzyl)-4-N-methyl-6-methyl-2,5-dioxo-1,4-piperazine: The compounds of the invention have FSH receptor modulatory activity and can be used for the control of fertility, for contraception or for treatment of hormone-dependent disorders.Type: GrantFiled: July 21, 2003Date of Patent: May 31, 2005Assignee: Pharmacopeia Drug Discovery, Inc.Inventors: Tao Guo, Koc-Kan Ho, Edward McDonald, Roland Ellwood Dolle, Kurt W. Saionz, Steven G. Kultgen, Ruiyan Liu, Guizhen Dong, Peng Geng, Anton Egbert Peter Adang, Nicole Corine Renee Van Straten
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Patent number: 6884803Abstract: Disclosed are substituted phenylalkynes of formula (I), wherein R1, R2, R3, R4, R5 and n are as defined, compositions containing them, and methods of making and using them to treat histamine-mediated conditions.Type: GrantFiled: December 2, 2002Date of Patent: April 26, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Richard Apodaca, Wei Xiao, Jill A. Jablonowski
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Patent number: 6846825Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1-C6 alkoxy, C1-C4 alkenyloxy, amino, C1-C4 alkylamino, or di-(C1-C6 alkyl)amino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.Type: GrantFiled: August 10, 2000Date of Patent: January 25, 2005Assignee: British Biotech Pharmaceuticals LimitedInventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
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Patent number: 6835734Abstract: (S)-3-(4-Phenyl-1-piperazinyl)-1,2-propanediol cyclic acetals useful as antitussive agents and as intermediates for the preparation of levodropropizine and the salts thereof, as well as a process for the preparation of said acetals, are disclosed.Type: GrantFiled: May 12, 2003Date of Patent: December 28, 2004Assignee: Dompé S.p.A.Inventors: Marcello Allegretti, Maria Candida Cesta, Roberto Curti, Luigi Pellegrini, Gabriella Melillo
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Publication number: 20040249147Abstract: Methods for producing azole compounds useful as intermediates for antifungal compounds and compositions including reaction of epoxy alcohols with reactants having active hydrogen attached to nitrogen, oxygen or sulfur in the presence of redox coupling agents. In some embodiments, a procedure known as a Mitsunobu reaction is utilized for the transformations.Type: ApplicationFiled: July 2, 2004Publication date: December 9, 2004Inventors: Jitendra Sattigeri, Jasbir Singh Arora, Sanjay Malhotra, Ashwani Kumar Verma, Mohammad Salman
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Publication number: 20040242573Abstract: The invention relates to thiophene carboxanmides of formula (I). wherein A, R1, R2, R3, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: January 22, 2004Publication date: December 2, 2004Inventors: Alan Faull, Craig Johnstone, Andrew Morley, Jeffrey Philip Poyser
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Publication number: 20040198978Abstract: A composition having immunosuppressant activity comprises at least one compound of the formula (I) in which R is an acyl group of the formula (II) wherein one of R1 and R2 is H and the other is selected from OR4, SR4 and NHR4, wherein R4 is H or 1-6C alkyl, or R1 and R2 together with the carbon atom to which they are joined form a keto group, and R3 is a straight or branched chain, saturated or unsaturated aliphatic hydrocarbyl group containing from 8 to 11 carbon atoms and is optionally substituted by one or more substituent groups selected from halo, 1-6C alkoxy, carboxy, 1-6C alkoxycarbonyl and NR5R6 wherein each of R5 and R6 is selected from H and 1-6C alkyl or R5 and R6 together with the N atom form a morpholino or piperazino group, or any enantiomer thereof; and at least one compound of the formula (III): wherein R7 is a straight or branched chain, saturated or ethylenically-unsaturated aliphatic hydrocarbyl group containing from 1 to 18 carbon atoms which may optionally be substituted by one or more suType: ApplicationFiled: May 18, 2004Publication date: October 7, 2004Inventor: David Idris Pritchard
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Publication number: 20040192676Abstract: Compounds which function as melanocortin receptor ligands and having utility in the treatment of melanocortin receptor-based disorders.Type: ApplicationFiled: December 19, 2003Publication date: September 30, 2004Applicant: Neurocrine Biosciences, Inc.Inventors: Chen Chen, Fabio C. Tucci, Joe Anh Tran, Caroline Chen, Nicole White
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Patent number: 6797711Abstract: Benzofuran derivatives represented by formula (I) or salts thereof: (wherein R1 represents a phenyl group or a hydrogen atom; k is 0 or 1; each of m, n, o, p, and q is an integer of 0 to 5; and each of R2 and R3 represents a hydrogen atom or a hydroxyl group, or R2 and R3 together represent an oxygen atom, with proviso that k, q, and m, or n, o, and p are not simultaneously 0). The compounds inhibit phosphorylation of STAT 6 and are useful in the treatment or prevention of allergic diseases.Type: GrantFiled: June 26, 2003Date of Patent: September 28, 2004Assignee: Pola Chemical Industries, Inc.Inventors: Nobuyuki Kawakatsu, Takayuki Namiki, Norihisa Yamazaki, Masayuki Yuasa, Toyohiko Miki, Noriko Suenobu, Tomomasa Shimanuki
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Patent number: 6787543Abstract: A compound of the formula (I): in which Z, R1, R2, R8, R10, R11, R12, R13 and R14 are each as defined in the description, or a salt thereof. The object compound of the present invention has pharmacological activities such as Tachykinin antagonism, and is useful for manufacture of a medicament for treating or preventing Tachykinin-mediated diseases.Type: GrantFiled: December 20, 2002Date of Patent: September 7, 2004Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kazuhiko Take, Chiyoshi Kasahara, Shinji Shigenaga, Hidenori Azami, Yoshiteru Eikyu, Kazuo Nakai, Masataka Morita
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Publication number: 20040152698Abstract: Compounds of general formula (I), in which Het represents a five or six membered saturated, partially unsaturated or aromatic ring containing between one and six heteroatoms of the group N, O, S, in which the heterocycle is substituted in an adjacent manner with -P-Qi-T-Q2, -GZ and Y, such that the substituant -GZ is adjacent to both, the other substituants being as defined in the description, process for preparing this compound, fungicidal composition comprising this compound, method for treating plants by applying this compound or composition.Type: ApplicationFiled: April 1, 2004Publication date: August 5, 2004Inventors: Stephanie Gary, Tim Lange, Benoit Muller, Christopher Richard Steele, Geoffrey Gower Briggs, Joseph Perez, Alain Villier, Brian Hill
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Patent number: 6770649Abstract: Novel 1-[1-(hetero)aryl-1-perhydroxyalkylmethyl]-piperazine compounds which are antagonistic to tachykinin receptors, of the general formula I, wherein R6, R7, A and Z have the meanings given in the description, and pharmaceutical compositions containing these compounds, as well as a process for the preparation of such compounds and intermediate products of this process.Type: GrantFiled: September 13, 2002Date of Patent: August 3, 2004Assignee: Solvay Pharmaceuticals GmbHInventors: Daniel Jasserand, Ulf Preuschoff, Jochen Antel, Samuel David, Holger Sann, Reinhard Brueckner, Dania Reiche, Christian Eeckhout
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Publication number: 20040147526Abstract: Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, and pyridine N-oxide; R2 is independently selected from ethyl and isopropyl; R3 is independently selected from hydrogen and fluoro; R4 is independently selected from —OH, —NH2 and —NHSO2R5; and R5 is independently selected from hydrogen, —CF3 and C1-C6 alkyl, or salts thereof or separate enantiomers and salts thereof; where each R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo.Type: ApplicationFiled: November 13, 2003Publication date: July 29, 2004Inventors: William Brown, Christopher Walpole, Niklas Plobeck
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Publication number: 20040142939Abstract: The present invention provides antibacterial agents having the formula I described herein.Type: ApplicationFiled: November 19, 2003Publication date: July 22, 2004Inventors: Jackson Boling Hester, Christina R. Harris
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Patent number: 6762300Abstract: Process for the preparation of 5-(1-piperazinyl)benzofuran-2-carboxamide in which, as intermediate step, 5-bromosalicylaldehyde or one of its derivatives is reacted in a transition metal-catalysed amination with R2-piperazine, in which R2 is as defined in claim 1.Type: GrantFiled: October 10, 2002Date of Patent: July 13, 2004Assignee: Merck Patent GmbHInventors: Andreas Bathe, Steffen Emmert, Bernd Helfert, Henning Boettcher
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Patent number: 6750233Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.Type: GrantFiled: September 17, 2001Date of Patent: June 15, 2004Assignee: Pharmacia CorporationInventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Yvette M. Fobian, John N. Freskos, Daniel P. Getman, Joseph J. McDonald, Susan L. Hockerman, Susan C. Howard, Steve A. Kolodziej, Hui Li, Deborah A. Mischke, Joseph G. Rico, Nathan W. Stehle, Michael B. Tollefson, William F. Vernier, Clara I. Villamil
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Publication number: 20040097734Abstract: The invention relates to novel aryl- and heteroarylcarboxamides of the general formula (1), their preparation and use as medicaments, in particular for the treatment of tumors.Type: ApplicationFiled: June 27, 2003Publication date: May 20, 2004Inventors: Matthias Gerlach, Peter Emig, Emmanuel Polymeropoulos, Gilbert Muller, Peter Schmidt, Silke Baasner, Eckhard Gunther