Ring Oxygen In The Additional Hetero Ring Patents (Class 514/254.1)
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Publication number: 20080064680Abstract: The present application discloses methods of detecting and treating cancer which express MUC1 aberrantly.Type: ApplicationFiled: September 14, 2005Publication date: March 13, 2008Inventor: Cynthia C. Bamdad
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Patent number: 7282519Abstract: The invention describes novel nitrosated and/or nitrosylated diuretic compounds or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated diuretic compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one diuretic compound of the invention, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor compound and/or at least one therapeutic agent.Type: GrantFiled: August 20, 2004Date of Patent: October 16, 2007Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, Manuel Worcel, Richard A. Earl, Maiko Ezawa, Xinqin Fang, Subhash P. Khanapure, Chia-En Lin, Ramani R. Ranatunge, Cheri A. Stevenson
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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: 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: 7229994Abstract: 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: GrantFiled: May 16, 2002Date of Patent: June 12, 2007Assignee: AstraZeneca ABInventors: William Brown, Christopher Walpole, Niklas Plobeck
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Patent number: 7160886Abstract: Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: February 27, 2004Date of Patent: January 9, 2007Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Liangqin Guo, Qingmei Hong, Ravi P. Nargund, Patrick G. Pollard, Iyassu K. Sebhat, Feroze Ujjainwalla, Zhixiong Ye
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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: 7115658Abstract: Compounds of formula I are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virusType: GrantFiled: May 9, 2003Date of Patent: October 3, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Allen J. Borchardt, Peter Scott Dragovich, Javier Gonzalez, Tanya Michelle Jewell, Hui Li, Maria Angelica Linton, John Howard Tatlock, Ru Zhou, Thomas Jay Prins, Melwyn A. Abreo
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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: 7084144Abstract: A compound having the general formula (I): wherein: X is N or C; R0 is H, a lower alkyl group, a lower O-alkyl group, lower alkyl group, a benzyl group, a phenyl group, a heterocyclic amine group, a cycloalkyl group, a cycloalkyl group substituted with O-alkyl or, a furyl group; R1 and R2 are, independently, H, an amine group, a lower alkyl group, a lower O-alkyl group, a lower S-alkyl group or a lower N-alkyl group, or R1 and R2 taken together with the carbon atoms to which they are attached form a five-membered carbocyclic or heterocyclic ring, where the heteroatoms of the heterocyclic ring are one or two oxygen atoms, and/or where any substituent on said carbocyclic or heterocyclic ring is chosen from O, S and N; n is 0,1,2,3 or 4; m is 0 or 1; and pharmaceutically acceptable salts thereof; with the proviso that said compound is not 1-[(4-methoxyphenyl)sulfonyl]piperazine or 1-(1,3-benzodioxol-5-ylsulfonyl)piperazine.Type: GrantFiled: May 19, 2004Date of Patent: August 1, 2006Assignee: The Jordanian Pharmaceutical MFG & Medical Equipment CO LTDInventor: Adnan Badwan
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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: 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: 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: 6916797Abstract: The invention relates to new ?-arylethylpiperazine of the formula wherein Z represents 0 or S; n? represents 1 or 2; R2 represents a hydrogen atom or a methyl group; W, Ar1 and Ar2 represent various substituents as defined herein; or non-toxic pharmaceutically acceptable salt, individual optical isomer, or individual diastereoisomer thereof, which are useful as neurokinin receptor antagonists (NK1 antagonists). It also relates to processes for their preparation and use in methods for treatment of asthma and/or allergic rhinitis.Type: GrantFiled: December 14, 2000Date of Patent: July 12, 2005Assignee: UCB, S.A.Inventors: Françoise Stiernet, Christophe Genicot, Marie-Agnes Lassoie, Florence Moureau, Thomas Ryckmans, Thierry Taverne, Jean-Pierre Henichart, Michel Neuwels, Solo Goldstein
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Patent number: 6916812Abstract: Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of the melanocortin receptors. The compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders such as obesity, diabetes, and sexual dysfunction.Type: GrantFiled: October 4, 2002Date of Patent: July 12, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Graham S. Poindexter, Guanglin Luo, Ling Chen
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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: 6903120Abstract: New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, OSO2CH3, SOR3, SO2R3, COR3, NO2, or CONHR3 and when X is CH or C R1 may also be CF3, CN, F, Cl, Br, or I; R2 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4,-trifluorobutyl, or —(CH2)—R4; R3 is a C1-C3 alkyl CF3, or N(R2)2; R4 is a C3-C6 cycloalkyl, 2-tetrahydrofurane or 3-tetra-hydrofurane, as well as pharmaceutically acceptable salts thereof are disclosed.Type: GrantFiled: December 22, 2000Date of Patent: June 7, 2005Assignee: A. Carlsson Research ABInventors: Clas Sonesson, Ingela Marianne Svan, Anders Kristoffer Lilja, Liselott Lilja Rönnqvist, Jenny Maria Carlberg, Susanna Waters, Nicholas Waters, Joakim Tedroff, Bengt Andersson
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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: 6861432Abstract: This invention relates to new piperazine derivatives of general formula I, in which V, W, n, R, R?, i, j, Y and Z have the meaning that is indicated in the description. The compounds according to the invention are distinguished by a diazacycloalkane substituent. They have at their disposal a special action with respect to the action that destabilizes the androgen receptor and can be used, for example, for treating prostrate cancer.Type: GrantFiled: November 22, 2002Date of Patent: March 1, 2005Assignee: Schering AktiengesellschaftInventors: Arwed Cleve, Christoph Huwe, Volker Schulze, Helmut Morack, Dieter Zopf, Jens Hoffmann, Andreas Reichel
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Patent number: 6849660Abstract: Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1? is —C(O)NR5R5?, —C(O)—Q—NR5R5?, —CH2NR5R5? or —S(O)2NR5R5? and the other is H or R3. One of R2 and R2? is —NHC(O)R6 or —NHS(O)2R6 and the other is H or R4. Q is an amino acid or peptide. R3 is H, halogen, —NR5R5? or —NHC(O)R6; and R4 is selected from the group consisting of H, halogen, hydroxyl, amino, carboxyl, alkyl, alkenyl and alkynyl. R5 is selected from the group consisting of H, alkyl, alkenyl or alkynyl optionally substituted with halogen, OH, amino, amidinyl, guanidinyl, urea, alkyl, carboxyl, oxo, carboxamide; R5? is H or R5 and R5? together form a 5-16 member heterocycle optionally substituted with halogen, OH, amino, alkyl, carboxyl, carbonyl or carboxamide.Type: GrantFiled: August 1, 2000Date of Patent: February 1, 2005Assignee: ISIS Pharmaceuticals, Inc.Inventors: Elizabeth Jefferson, Eric Swayze
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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: 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: 6770650Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: August 29, 2001Date of Patent: August 3, 2004Assignee: Syntex (U.S.A.) LLCInventors: Leyi Gong, Donald Roy Hirschfeld, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
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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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Publication number: 20040106606Abstract: The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently 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. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.Type: ApplicationFiled: November 19, 2002Publication date: June 3, 2004Inventors: Frederick Earl Boyer, John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Susan Elizabeth Hagen, Michael James Lovdahl, Elizabeth Ann Lunney, Larry James Markoski, Josyula Venkata Nagendra Vara Prasad, Bradley Dean Tait
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Patent number: 6706719Abstract: 4-(4-(-Chlorophenyl)piperazin-1-yl)sulfonylmethyl)-tetrahydor yran-4-carboxylic acid and the corresponding N-hydroxy amide, and derivatives thereof, are useful as therapeutic agents.Type: GrantFiled: June 25, 2001Date of Patent: March 16, 2004Assignee: Darwin Discovery, Ltd.Inventors: Andrew Douglas Baxter, David Alan Owen, Robert John Watson
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Publication number: 20040038989Abstract: (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: ApplicationFiled: May 12, 2003Publication date: February 26, 2004Inventors: Marcello Allegretti, Maria Candida Cesta, Roberto Curti, Luigi Pellegrini, Gabriella Melillo
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Patent number: 6696447Abstract: The present application describes compounds of general formula I where R1 is selected from any one of pyridinyl, thienyl, furanyl, imidazolyl, and triazolyl; and 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. The substitutions on the heteroaromatic ring may take place in any position on the ring system. The invention also includes enantiomers, salts and pharmaceutical compositions containing the compounds. The compounds may be used in treating patients for pain.Type: GrantFiled: September 27, 2002Date of Patent: February 24, 2004Assignee: AstraZeneca ABInventors: William Brown, Niklas Plobeck, Christopher Walpole
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Publication number: 20040029812Abstract: The invention relates to a method of treating with furanone derivatives and the phmaceutically acceptable salts therof, one or more conditions of the skin, in particular regulating skin condition, regulating signs of skin aging, treating a number of conditions suchas contact dermatitis, skin irritation, rosacea, acne, psoriasis, and preventing and protecting skin tissue against age-related damage or damage resulting from insults such as harmful (UV) radiation or environmental pollution, stress and fatigue.Type: ApplicationFiled: July 30, 2003Publication date: February 12, 2004Inventors: Sekhar Boddupalli, Gail Walkinshaw, Bing Wang
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Patent number: 6689785Abstract: Novel epoxysuccinamide derivatives represented by the general formula (1) or physiologically acceptable salts thereof, which are useful particularly as remedies for bone diseases and arthritis, wherein R1 and R3 are each hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, a heterocyclic group, or a heterocyclic-alkyl group; R2 is alkyl, alkenyl, alkynyl, aryl, aralkyl, a heterocyclic group, or a hetericyclic-alkyl group; X is —O— or —NR4— (wherein R4 is hydrogen, alkyl, aryl, aralkyl, a heterocyclic group, or a heterocyclic-alkyl group; Y1 is OR5, SR6, or NR7R8 (wherein each of R5, R6 and R7 is hydrogen, alkyl, aryl, aralkyl, acyl, a heterocyclic group, or a heterocyclic-alkyl group, and R8 is the same as defined for R4); and Y2 is hydrogen or alkyl, or alternatively Y1 and Y2 can be combined to form ═O, ═S, ═N—R9, or ═N—OR10 (wherein each of R9 and R10 is the same as defined for R4), provided that each of the alkyl, aryl and heterocyclic groups defined foType: GrantFiled: January 8, 2002Date of Patent: February 10, 2004Assignee: Nippon Chemiphar Co., Ltd.Inventors: Yutaka Nomura, Toshihiro Takahashi, Yasushi Yoshino, Koichiro Nishioka
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Publication number: 20040019039Abstract: A novel class of substituted piperazines and diazepanes, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.Type: ApplicationFiled: June 27, 2002Publication date: January 29, 2004Inventors: Florencio Zaragoza Dorwald, Knud Erik Andersen, Jan Lindy Sorensen
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Patent number: 6680321Abstract: Compounds of the formula (I) as well as their pharmaceutically acceptable salts, and pharmaceutical compositions comprising the novel compounds. The novel compounds of the formula (I) are useful in the management of pain.Type: GrantFiled: August 2, 2000Date of Patent: January 20, 2004Assignee: AstraZeneca Canada, Inc.Inventors: Edward Roberts, Niklas Plobeck, Claes Wahlestedt
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Publication number: 20030216404Abstract: The invention encompasses novel compounds which are inhibitors of matrix metalloproteinase, ADAM or ADAM-TS enzymes, and which are useful for the treatment of diseases mediated by those enzymes, including degenerative diseases and certain cancers.Type: ApplicationFiled: June 12, 2003Publication date: November 20, 2003Inventors: Duncan Robert Hannah, Hazel Joan Dyke, Andrew Sharpe, Andrew Douglas Baxter
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Patent number: 6649611Abstract: A compound of the formula or the pharmaceutically acceptable salt thereof; wherein a, b, c, d, e, j, R1, R2, R3, and R4 are as defined herein and are useful to treat inflammation and other immune disorders.Type: GrantFiled: March 29, 2001Date of Patent: November 18, 2003Assignee: Pfizer, Inc.Inventors: Laura C. Blumberg, Matthew F. Brown, Ronald P. Gladue, Molly A. McGlynn, Christopher S. Poss
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Patent number: 6642238Abstract: The present invention provides a compound of formula I which have potent activities against gram-positive and gram-negative bacteria.Type: GrantFiled: January 9, 2002Date of Patent: November 4, 2003Assignee: Pharmacia and Upjohn CompanyInventor: Jackson B. Hester, Jr.
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Publication number: 20030203900Abstract: Cathepsin S is a highly active cysteine protease belonging to the papain superfamily. It is found mainly in lymph nodes, spleen, and macrophages and this limited occurrence suggests the potential involvement of this enzyme in the pathogenesis of degenerative disease. The invention relates to novel protease inhibitors, particularly inhibitors of the cysteine proteases of the papain superfamily and more particularly to Cathepsin S. The inhibitors are Furanone derivatives of Formula (II) which have a characteristic non-hydrogen substituent R5. They are selective over other members of the family and in particular show selectivity over other members of the Cathepsin family such as L and K.Type: ApplicationFiled: November 16, 2001Publication date: October 30, 2003Inventors: Martin Quibell, Steven Taylor, Urszula Grabowska, Magnus Nilsson, Veronique Morisson
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Patent number: 6638927Abstract: Compounds of formula IA and IB are new 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: August 31, 2001Date of Patent: October 28, 2003Assignee: Chiron CorporationInventors: Paul A. Renhowe, Daniel Chu, Rustum S. Boyce, Zhi-Jie Ni, David Duhl, Effie Tozzo, Kirk Johnson, David C. Myles
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Publication number: 20030186962Abstract: of the formula (IV): 1Type: ApplicationFiled: November 16, 2001Publication date: October 2, 2003Inventors: Martin Quibell, Steven Taylor, Urszula Grabowska, Magnus Nilsson, Veronique Morrison
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Publication number: 20030176446Abstract: (±) 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.Type: ApplicationFiled: May 13, 2003Publication date: September 18, 2003Inventors: Marcello Allegretti, Maria Candida Cesta, Roberto Curti, Luca Nicolini
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Publication number: 20030176441Abstract: The invention provides compounds of Formula (I): 1Type: ApplicationFiled: November 29, 2002Publication date: September 18, 2003Inventors: Daisy Joe Du Bois, Denis John Kertesz, Eric Brian Sjogren, David Bernard Smith, Beihan Wang
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Patent number: 6620782Abstract: The present invention is directed to novel 2-aminobenzamide thereof, represented by the general Formula I: where R1-R3, X, and A—D are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.Type: GrantFiled: March 16, 2000Date of Patent: September 16, 2003Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Yan Wang
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Publication number: 20030171371Abstract: New N-acyl homoserine lactone compounds of the formula (I) in whichR 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 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, carbamoyl optionally mono- or disubstituted at the N atom by 1-6C alkyl 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 and enantiomer thereof, with the proviso that R is not a 3-oxododecanoyl group, having immuosuppressant properties are disclosed. The compounds are shown to have an inhibitory effect on lymphocyte proliferation and down-regulate TNF-&agr; secretion by monocytes/macrophages in the animal body, including the human body.Type: ApplicationFiled: February 12, 2003Publication date: September 11, 2003Inventors: Barrie Walsham Bycroft, David Idris Pritchard, Siri Ram Chhabra, Doreen Hooi
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Patent number: 6602874Abstract: A compound of the formula wherein X, Y, Z, R2 and R3 are as defined above, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1, agonist or antagonist is indicated.Type: GrantFiled: May 22, 2001Date of Patent: August 5, 2003Assignee: Pfizer Inc.Inventor: Harry R. Howard
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Publication number: 20030139421Abstract: Compounds of general formula I 1Type: ApplicationFiled: September 27, 2002Publication date: July 24, 2003Inventors: William Brown, Niklas Plobeck, Christopher Walpole
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Publication number: 20030139423Abstract: New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, OSO2CH3, SOR3, SO2R3, COR3, NO2, or CONHR3 and when X is CH or C R1 may also be CF3, CN, F, Cl, Br, or I; R2 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, or —(CH2)—R4; R3 is a C1-C3 alkyl, CF3, or N(R2)2; R4 is a C3-C6 cycloalkyl, 2-tetrahydrofurane or 3-tetra-hydrofurane, as well as pharmaceutically acceptable salts thereof are disclosed. Also pharmaceutical compositions comprising the above compounds and methods wherein the above compounds are used for treatment of disorders in the central nervous system are disclosed.Type: ApplicationFiled: November 21, 2002Publication date: July 24, 2003Inventors: Clas Sonesson, Bengt Andersson, Ingela Marianne Svan, Anders Kristoffer Lilja, Liselott Lilja Ronnqvist, Jenny Maria Carlberg, Susanna Waters, Nicholas Waters, Joakim Tedroff