Sulfur Containing Hetero Ring Patents (Class 548/527)
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Patent number: 7417062Abstract: Substituted benzamide compounds are provided along with methods for the use of those compounds for treating cancer.Type: GrantFiled: August 11, 2005Date of Patent: August 26, 2008Assignee: ChemoCentryx, Inc.Inventors: Anita Melikian, John J. Kim Wright
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Patent number: 7393846Abstract: The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.Type: GrantFiled: September 28, 2006Date of Patent: July 1, 2008Assignee: Glenmark Pharmaceuticals, S.A.Inventors: Balasubramanian Gopalan, Laxmikant Atmaram Gharat, Aftab Dawoodbhai Lakdawala, Usha Karunakaran
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Publication number: 20080045560Abstract: Compounds of the following structure are described: wherein R1-R6, R11, R12, m, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.Type: ApplicationFiled: August 13, 2007Publication date: February 21, 2008Applicant: WyethInventors: Thomas Joseph Commons, Andrew Fensome, Gavin David Heffernan, Casey Cameron McComas, Richard Page Woodworth, Michael Byron Webb, Michael Anthony Marella, Edward George Melenski
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Patent number: 7326729Abstract: The present invention is directed to a compound having the general structure of formula (1): useful for the treatment, prevention or amelioration of a CXCR1 or CXCR2 chemokine-mediated disease.Type: GrantFiled: May 11, 2005Date of Patent: February 5, 2008Assignee: Schering CorporationInventors: Jianhua Chao, Arthur G. Taveras, Cynthia J. Aki
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Patent number: 7312179Abstract: A fungicidally active compound of formula (I): where X is (X1), (X2) or (X3); Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, provided that the ring is not 1,2,3-triazole, the ring being substituted by groups R4, R5 and R6; R1 and R2 are each, independently, hydrogen, halo or methyl; R3 is optionally substituted C2-12 alkyl, optionally substituted C2-12 alkenyl, optionally substituted C2-12 alkynyl, optionally substituted C3?12 cycloalkyl, optionally substituted phenyl or optionally substituted heterocyclyl; R4, R5 and R6 are each, independently, selected from hydrogen, halo, cyano, nitro, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy(C1-4)alkylene and C 1-4 haloalkoxy(C1-4)alkylene, provided that at least one of R4, R5 and R6 is not hydrogen; and R7 and R8 are each, independently, hydrogen, halogen, C1-4 alkyl or Clue haloalkyl; the invention also relates to the preparation of these compounds, to novel intermediates useType: GrantFiled: October 24, 2003Date of Patent: December 25, 2007Assignee: Syngenta Crop Protection, Inc.Inventors: Josef Ehrenfreund, Hans Tobler, Harald Walter
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Patent number: 7307173Abstract: Electron acceptor compounds, nonlinear optical chromophores, methods for making the compounds and chromophores, and materials and electro-optic devices that include the chromophores.Type: GrantFiled: February 22, 2005Date of Patent: December 11, 2007Assignee: University of WashingtonInventors: Kwan-Yue Jen, Sei-Hum Jang, Bart Kahr
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Publication number: 20070281981Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: May 11, 2007Publication date: December 6, 2007Inventors: DAVID W. OLD, Danny T. Dinh
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Patent number: 7301037Abstract: Charged compounds are provided that comprise one or more regions of localized positive charge, compositions comprising such compounds, methods of synthesizing such compounds, methods of screening such compounds to identify those having anti-infective activity, and methods of using such compounds to prevent or inhibit infections. These compounds, and compositions containing them, have multiple applications, including use in human and animal medicine and in agriculture.Type: GrantFiled: July 14, 2006Date of Patent: November 27, 2007Assignee: Genesoft, Inc.Inventors: Yigong Ge, Matthew J. Taylor, Eldon E. Baird, Heinz E. Moser, Roland W. Burli
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Publication number: 20070270440Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.Type: ApplicationFiled: May 18, 2007Publication date: November 22, 2007Applicant: WyethInventors: Derek Cecil Cole, Magda Asselin, Joseph Raymond Stock, Jin-In Kim
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Patent number: 7294650Abstract: Compounds of formula (I): and salts, solvates, and physiologically functional derivatives thereof, useful for the prophylaxis or treatment of a clinical condition for which a selective ?2-adrenoreceptor agonist is indicated, for example asthma or chronic obstructive pulmonary disease (COPD).Type: GrantFiled: December 15, 2004Date of Patent: November 13, 2007Assignee: Glaxo Group LimitedInventor: Keith Biggadike
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Patent number: 7288538Abstract: The present invention relates to urotensin II receptor antagonists, CCR-9 antagonists, pharmaceutical compositions containing them and their use.Type: GrantFiled: August 23, 2004Date of Patent: October 30, 2007Assignee: Encysive Pharmaceuticals, Inc.Inventors: Chengde Wu, Daxin Gao, Ronald Biediger, Jie Chen, Robert V. Market
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Patent number: 7282510Abstract: This invention relates to neurotrophic N-glyoxyl-prolyl ester compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.Type: GrantFiled: June 27, 2005Date of Patent: October 16, 2007Assignee: GliaMed, Inc.Inventors: Gregory S. Hamilton, Joseph P. Steiner
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Publication number: 20070232679Abstract: There is provided a series of substituted N-aryl pyrrolidine derivatives of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R5?, R6, R7, and p as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.Type: ApplicationFiled: March 29, 2007Publication date: October 4, 2007Inventors: Kenneth M. Boy, Shirong Zhu, John E. Macor, Shuhao Shi, Samuel Gerritz
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Patent number: 7276531Abstract: A gamma-lactam diene of Formula I: which is particularly useful as a medicament for the treatment of various disorders such as asthma, hypertension, osteoporosis, sexual dysfunction and fertility disorders.Type: GrantFiled: March 2, 2004Date of Patent: October 2, 2007Assignee: Applied Research Systems ARS Holding N.V.Inventors: Gian Luca Araldi, Srinivasa Karra, Zhong Zhao, Nadia Brugger
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Patent number: 7273940Abstract: Bisimine compounds of the formula (I) where the symbols have the following meanings: A is a nonmetal selected from among N, S, O and P, R1 is a radical of the formula NR5R6, R2 is a radical of the formula NR5R6 or NR7R8, alkyl, aryl or cycloalkyl, R5 and R6 together with the N atom form a 5-, 6- or 7-membered ring in which one or more of the —CH— or —CH2— groups may be replaced by suitable heteroatom groups and which may be saturated or unsaturated and unsubstituted or substituted or be fused with further carbacyclic or heterocarbacyclic 5- or 6-membered rings which may in turn be saturated or unsaturated and substituted or unsubstituted, and R7 and R8 are, independently of one another, alkyl, aryl or cycloalkyl radicals, and R3, R4 are, independently of one another, H or alkyl, aryl or cycloalkyl radicals, and n is 1 or 2, are used to prepare bisimidinato complexes which can be used in the polymerization of unsaturated compounds.Type: GrantFiled: October 7, 2004Date of Patent: September 25, 2007Assignee: Basell Polyolefine GmbHInventors: Marc Oliver Kristen, Andrei Gonioukh, Dieter Lilge, Stephan Lehmann, Benno Bildstein, Christoph Amort, Michael Malaun
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Publication number: 20070219265Abstract: A compound comprising or a pharmaceutically acceptable salt thereof, or a prodrug thereof is disclosed herein. Y, A, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.Type: ApplicationFiled: March 20, 2007Publication date: September 20, 2007Inventors: David W. Old, Danny T. Dinh
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Patent number: 7250415Abstract: The present application describes 1,1-disubstitutedcycloalkyl-, glycinamidyl-, sulfonyl-amidino-, and tetrahydropyrimidinyl-containing diaminoalkyl, ?-aminoacids, ?-aminoacids and derivatives thereof of Formula I: P-M-M1I or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein M is a linear core. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: June 1, 2004Date of Patent: July 31, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Jennifer X. Qiao, Donald J. Pinto
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Patent number: 7250414Abstract: This invention provides compounds of formula I: wherein a, b, c, e, m, n, Ar1, R1, R2, R3, R4a, R4b, R5 and R6 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: GrantFiled: March 10, 2005Date of Patent: July 31, 2007Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, Yan Chen, Craig Husfeld
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Patent number: 7244851Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.Type: GrantFiled: July 5, 2005Date of Patent: July 17, 2007Assignee: Genentech, Inc.Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
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Patent number: 7238725Abstract: The present invention relates to novel tricyclic compounds useful for the treatment of inflammatory conditions, diseases of the central nervous and insulin resistant diabetes.Type: GrantFiled: October 8, 2003Date of Patent: July 3, 2007Assignee: Glenmark Pharmaceuticals Ltd.Inventors: Gopalan Balasubramanian, Laxmikant A. Gharat, Aftab D. Lakdawala, Raghu R. Anupindi
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Patent number: 7235579Abstract: Selective PDE4 inhibition is achieved by 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds like rolipram and show selectivity with regard to inhibition of other classes of PDEs. The compounds of the present invention are of formula I: wherein R1, R2, and R3 are as defined herein.Type: GrantFiled: October 16, 2002Date of Patent: June 26, 2007Assignee: Memory Pharmaceuticals Corp.Inventors: Ruiping Liu, Mike De Vivo, Hans-Jurgen Ernst Hess, Allen Hopper, Erik Kuester, Ashok Tehim
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Patent number: 7235544Abstract: The invention relates to compounds of formula (I): wherein substituents are as defined.Type: GrantFiled: June 17, 2004Date of Patent: June 26, 2007Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, John David Harling, Wendy Rebecca Irving, Savvas Kleanthous, Nigel Stephen Watson, Robert John Young
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Patent number: 7205318Abstract: The present application describes lactam-containing cyclic diamines and derivatives thereof of Formula I: P4-M-M4I or pharmaceutically acceptable salt forms thereof, wherein M is a non-aromatic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: March 16, 2004Date of Patent: April 17, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Jennifer X. Qiao, Tammy C. Wang, Gren Z. Wang, Timur Gungor
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Patent number: 7199149Abstract: The present application describes monocyclic and bicyclic lactams and derivatives thereof of Formulae Ia–e: wherein one of one of T1 and T2 is carbonyl, thiocarbonyl, or sulfonyl or pharmaceutically acceptable salt forms thereof. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: September 28, 2004Date of Patent: April 3, 2007Assignee: Bristol Myers Squibb CompanyInventors: Wei Han, Jennifer X. Qiao, Zilun Hu
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Patent number: 7192978Abstract: New pyrrolidinium derivatives having the chemical structure of general formula (I) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as antagonists of M3 muscarinic receptors.Type: GrantFiled: April 11, 2003Date of Patent: March 20, 2007Assignee: Almirall Prodesfarma AGInventors: Maria Prat Quinones, Maria Dolors Fernandez Forner
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Patent number: 7186735Abstract: The present invention relates to acylated arylcycloalkylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.Type: GrantFiled: August 7, 2003Date of Patent: March 6, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Hartmut Strobel, Paulus Wohlfart, Peter Below
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Patent number: 7186722Abstract: Novel ?1-pyrrolines of the Formula (I) in which R1, R2, R3 and Het have the meanings given in the description, a plurality of processes for preparing these compounds and their use for controlling pests, and also novel intermediates and processes for their preparation.Type: GrantFiled: January 31, 2002Date of Patent: March 6, 2007Assignee: Bayer Cropscience AGInventors: Andrew Plant, Rüdiger Fischer, Thomas Seitz, Christoph Erdelen, Andreas Turberg, Olaf Hansen
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Patent number: 7183260Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: GrantFiled: August 25, 2004Date of Patent: February 27, 2007Assignee: Idun Pharmaceuticals, Inc.Inventors: Donald S Karanewsky, Robert J Ternansky, Steven D Linton, Thang Dinh
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Patent number: 7183277Abstract: Novel compounds of the formula I in which D, W, X, Y, T and R1 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.Type: GrantFiled: March 31, 2003Date of Patent: February 27, 2007Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Werner Mederski, Johannes Gleitz, Bertram Cezanne, Christos Tsaklakidis, Christopher Barnes
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Patent number: 7179835Abstract: The invention relates to compounds of formula (I) pharmaceutical compositions containing the same as well as methods of treating patients suffering from a condition susceptible to amelioration by a Factor Xa inhibitor using the same.Type: GrantFiled: November 13, 2002Date of Patent: February 20, 2007Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, Matthew Campbell, Chuen Chan, Henry Anderson Kelly, Nigel Paul King, Savvas Kleanthous, Andrew McMurtrie Mason, Stefan Senger, Paul William Smith, Nigel Stephen Watson, Robert John Young
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Patent number: 7144902Abstract: The present invention relates to prodrugs of pharmacologically active five-membered heterocyclic amidines from which are produced in vivo compounds which are competitive inhibitors of trypsin-like serine proteases, in particular thrombin and kininogenases such as kallikrein, to the preparation thereof and to the use thereof as medicines. The invention also relates to pharmaceutical compositions which comprise the prodrugs of the active compounds as ingredients, and to the use of the compounds as thrombin inhibitors, anticoagulants and as antiinflammatory agents.Type: GrantFiled: April 5, 2000Date of Patent: December 5, 2006Assignee: Abbott GmbH & Co. KGInventors: Dorit Baucke, Helmut Mack, Werner Seitz, Wilfried Hornberger, Gisela Backfisch, Juergen Delzer
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Patent number: 7138426Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.Type: GrantFiled: April 18, 2003Date of Patent: November 21, 2006Assignee: Merck & Co., Inc.Inventors: Frank P. DiNinno, Timothy Allen Blizzard, Jerry Dwain Morgan, II
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Patent number: 7138075Abstract: The synthesis of thiophene based conducting polymer molecular actuators, exhibiting electrically triggered molecular conformational transitions is reported. Actuation is believed to be the result of conformational rearrangement of the polymer backbone at the molecular level, not simply ion intercalation in the bulk polymer chain upon electrochemical activation. Molecular actuation results from ?—? stacking of thiophene oligomers upon oxidation, producing a reversible molecular displacement that leads to surprising material properties, such as electrically controllable porosity and large strains. The existence of active molecular conformational changes is supported by in situ electrochemical data. Single molecule techniques have been used to characterize the molecular actuators.Type: GrantFiled: March 19, 2003Date of Patent: November 21, 2006Assignee: Massachusetts Institute of TechnologyInventors: Patrick A. Anquetil, Ian W. Hunter, John D. Madden, Peter G. Madden, Anthony E. Pullen, Timothy M. Swager, Bing Xu, Hsiao-hua Yu
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Patent number: 7094801Abstract: 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: December 19, 2002Date of Patent: August 22, 2006Assignee: Atherogenics, Inc.Inventors: James A. Sikorski, Charles Q. Meng, M. David Weingarten, Kimberly J. Worsencroft, Liming Ni
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Patent number: 7091204Abstract: The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.Type: GrantFiled: May 7, 2002Date of Patent: August 15, 2006Assignee: SmithKline Beecham CorporationInventors: Dashyant Dhanak, Timothy F. Gallagher, Steven D. Knight
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Patent number: 7087638Abstract: Novel pyrrole derivatives of formula I wherein X is oxygen or sulfur; R1 is C1–C4alkyl unsubstituted or substituted, with the exception of CF3; C3–C6cycloalkyl unsubstituted or substituted; or halogen; R2 is hydrogen, C1–C4alkyl unsubstituted or substituted, C1–C4alkoxy unsubstituted or substituted, cyano or halogen; R3 is C1–C4alkyl unsubstituted or substituted; and A is orthosubstituted aryl; orthosubstituted heteroaryl; bicycloaryl unsubstituted or substituted; or bicycloheteroaryl unsubstituted or substituted. The novel compounds have plant-protective properties and are suitable for protecting plants against infestations by phytopathogenic microorganisms.Type: GrantFiled: October 7, 2003Date of Patent: August 8, 2006Assignee: Syngenta Crop Protection, Inc.Inventors: Harald Walter, Hermann Schneider
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Patent number: 7078536Abstract: Charged compounds are provided that comprise one or more regions of localized positive charge, compositions comprising such compounds, methods of synthesizing such compounds, methods of screening such compounds to identify those having anti-infective activity, and methods of using such compounds to prevent or inhibit infections. These compounds, and compositions containing them, have multiple applications, including use in human and animal medicine and in agriculture.Type: GrantFiled: October 22, 2002Date of Patent: July 18, 2006Assignee: Genesoft Pharmaceuticals, Inc.Inventors: Yigong Ge, Matthew J. Taylor, Eldon E. Baird, Heinz E. Moser, Roland W. Bürli
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Patent number: 7074785Abstract: Novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, A, R4 and m have the meanings given in the description, a number of processes for preparing these substances, and their use for controlling pests, and also novel intermediates and their preparation.Type: GrantFiled: September 4, 2002Date of Patent: July 11, 2006Assignee: Bayer Cropscience AGInventors: Thomas Seitz, Martin Füsslein, Johannes Rudolf Jansen, Udo Kraatz, Angelika Lubos-Erdelen, legal representative, Andreas Turberg, Olaf Hansen, Christoph Erdelen, deceased
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Patent number: 7053056Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: GrantFiled: January 16, 2001Date of Patent: May 30, 2006Assignee: Idun Pharmaceuticals, Inc.Inventors: Donald S. Karanewsky, Robert J. Ternansky, Steven D. Linton, Thang Dinh
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Patent number: 7022677Abstract: Disclosed are the novel compounds as growth hormone secretagogues represented by structural Formula (I), wherein R1 is, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryl, or substituted or unsubstituted amino, X is —CO— or —SO2—, Y is Formula (II), wherein n is an integer from 0–4, R4 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, R5 and R6 are independently selected from hydrogen, substituted or unsubstituted alkyl, or R5 and R6 or R4 and R5 are taken together to form substituted or unsubstituted alkylene, R2 is hydrogen, or substituted or unsubstituted alkyl, R3 is substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, D is substituted or unsubstituted amino, substituted or unsubstituted alkoxy, or substituted or unsubstituted alkylthio, * represents an asymmetric center, and phType: GrantFiled: February 17, 2000Date of Patent: April 4, 2006Assignees: Kaken Pharmaceutical Co., Ltd., Molecular Research InstituteInventors: Nobuo Ishiyama, Hirohide Ishige, Mitsuo Mimura, Tadashi Okuno, Kiyoharu Ukai, Takeshi Kiyofuji, Shinji Tauchi, Kiyoshi Inoguchi, Ping Huang, Linda J. Maki, legal representative, Gilda H. Loew, deceased
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Patent number: 6962942Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.Type: GrantFiled: September 16, 2002Date of Patent: November 8, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan José Marugán Sánchez, Kristin D. Haslow, Jonathan Hall
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Patent number: 6939007Abstract: The invention provides photochromic bis-naphthopyran compounds as well as methods for their manufacture and their use. The bis-naphthopyran compounds of the invention exhibit a wide range of color, i.e., from pink to purple to blue gray, upon activation by a source of UV light. Additionally, the bis-naphthopyran compounds of the present invention exhibit broad coloration ability, fast response as to both color change on activation and return to original color, and good fatigue-resistance.Type: GrantFiled: October 28, 2003Date of Patent: September 6, 2005Inventors: Weili Zhao, Erick M. Carreira
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Patent number: 6936633Abstract: The present invention provides pharmaceutical compositions and novel compounds useful in the treatment of conditions mediated by CCR2, MCP-1 or the interaction thereof. The compounds of the present invention are pyrrolidinones and pyrrolidine-thiones.Type: GrantFiled: December 31, 2003Date of Patent: August 30, 2005Assignee: UCB S.A.Inventors: Dong Zou, Olivier Dasse, Janelle Evans, Paul Higgins, Jeremy Kintigh, Rama Kondru, Eric Schwartz, Laurent Knerr, Hai-Xiao Zhai
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Patent number: 6916831Abstract: Compounds are described having a structure according to Formula I or Formula II: wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O and S; m is from 1 to 3; n is from 1 to 5; R1 and R3 are each independently selected from the group consisting of H, hydroxy, lower alky, lower alkoxy, halo, amino, aminoalkyl, nitro, heteroaryl, —OC(?O)R6, —O(C?O)OR6; and —O(C?O)N(R6)2; and R2 is side chain such as an acetic acid side chain, where p is O to 4, R5 is hydroxy, alkoxy or amino, and R6 is H or lower alkyl, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer.Type: GrantFiled: February 24, 2003Date of Patent: July 12, 2005Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Yi Xia, Zheng-Yu Yang, Kenneth F. Bastow, Sheng-Chu Kuo
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Patent number: 6911461Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives of formula I, wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy.Type: GrantFiled: October 28, 2003Date of Patent: June 28, 2005Assignee: UCB, S.A.Inventors: Edmond Differding, Benoît Kenda, Bénédicte Lallemand, Alain Matagne, Philippe Michel, Patrick Pasau, Patrice Talaga
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Patent number: 6903131Abstract: Disclosed are compounds of the formula (I) or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.Type: GrantFiled: October 11, 2002Date of Patent: June 7, 2005Assignees: Schering Corporation, Pharmacopeia Drug Discovery, Inc.Inventors: Arthur G. Taveras, Michael Dwyer, Johan A. Ferreira, Viyyoor M. Girijavallabhan, Jianping Chao, John J. Baldwin, J. Robert Merritt, Ge Li
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Patent number: 6900338Abstract: The present invention provides novel compounds having scavenging and anti-ROS properties and pharmaceutical composition comprising these compounds for treatment of conditions associated with oxidative stress or free radical injury. The compounds of the invention are of general formula (I).Type: GrantFiled: November 25, 1999Date of Patent: May 31, 2005Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventor: Abdullah Haj-Yehia
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Patent number: 6897319Abstract: This invention is directed to aroyl pyrrole heteroaryl methanone and methanol compounds pharmaceutically useful as agents for treating or modulating a central nervous system disorder and methods for treating or modulating a central nervous system disorder.Type: GrantFiled: December 10, 2002Date of Patent: May 24, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: John R. Carson, Ellen E. Codd, Philip M. Pitis
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Patent number: 6875776Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: October 24, 2002Date of Patent: April 5, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Soo S. Ko, Cheryl McArdle Clark, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
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Patent number: 6852752Abstract: Novel hydroxamic acid compounds are disclosed. These hydroxamates inhibit peptide deformylase (PDF), an enzyme present in prokaryotes and are therefore useful as antimicrobials and antibiotics. Methods of synthesis and of use of the compounds are also disclosed.Type: GrantFiled: December 13, 2000Date of Patent: February 8, 2005Assignee: Vicuron Pharmaceuticals Inc.Inventors: Jeffrey W. Jacobs, Dinesh Patel, Jason Lewis, Zhi-Jie Ni