The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/187)
-
Publication number: 20100130572Abstract: The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.Type: ApplicationFiled: January 28, 2010Publication date: May 27, 2010Inventors: John W. LAMPE, Robert Plourde, JR., Jin She, Jason L. Vittitow, Paul S. Watson, Michael T. Crimmins, David J. Slade
-
Publication number: 20100120784Abstract: Heteroaromatic compounds of structural formula (I) or a pharmaceutically acceptable salt thereof, wherein W is a substituted heteroaryl, X and Y are each independently a bond, —O—, —S—, —S(O)—, —S(O)2—, —NR6—, —C(O)—, —C(CH3)(OH)— or —C(CH3)?CH—, u (I) is an integer from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis, obesity, Type 2 diabetes, insulin resistance, hyperglycemia, Metabolic Syndrome, neurological disease, cancer, and liver steatosisType: ApplicationFiled: April 17, 2008Publication date: May 13, 2010Inventors: Nicolas Lachance, Chun Sing Li, Jean-Philppe Leclerc, Yeeman K. Ramtohul
-
Patent number: 7705019Abstract: In its many embodiments, the present invention provides a novel class of compounds of structural formula IA or IB where R1-R8 are as disclosed herein as inhibitors of the CCR5 receptors, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with CCR5 using such compounds or pharmaceutical compositions. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v.Type: GrantFiled: February 21, 2006Date of Patent: April 27, 2010Assignee: Schering CorporationInventors: Tze-Ming Chan, Kathleen Cox, Wenqing Feng, Michael W. Miller, Daniel Weston, Stuart W. McCombie
-
Publication number: 20100093809Abstract: A compound having a structure is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: December 15, 2009Publication date: April 15, 2010Applicant: ALLERGAN, INC.Inventor: David W. Old
-
Patent number: 7674827Abstract: Indanyl- and Tetrahydronaphtyl-amino-thiourea compounds for combating animal pests The present invention relates to Indanyl- and Tetrahydronaphtyl-amino-thiourea compounds of formula I wherein the variables R1 to R4 are as in the description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection.Type: GrantFiled: November 15, 2006Date of Patent: March 9, 2010Assignee: BASF SEInventors: Markus Kordes, Christopher Koradin, Deborah L. Culbertson
-
Publication number: 20100048891Abstract: Thiazolidinones of general formula (I) production thereof and use as inhibitors of polo like kinase (PLK) for the treatment of various diseases.Type: ApplicationFiled: April 29, 2009Publication date: February 25, 2010Inventors: Klause SCHULZE, Knut Eis, Lars Wortmann, Dirk Kosemund, Olaf Prien, Gerhard Siemeister, Holger Hess-Stumpp, Uwe Eberspaecher, Dominic E.A. Brittain, Imadul Islam
-
Publication number: 20100041708Abstract: An N-phenylarylsulfonylamide compound of formula (I) (R1 is COOH etc.; R2 is hydrogen, methyl, etc.; R3 and R4 are a combination of methyl and methyl, etc.; R5 is isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin E2 receptor, especially an EP1 subtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.Type: ApplicationFiled: October 21, 2009Publication date: February 18, 2010Applicant: ONO PHARMACEUTICAL Co., Ltd.Inventors: Atsushi NAGANAWA, Tetsuji Saito, Kaoru Kobayashi, Takayuki Maruyama, Yoshihiko Nakai, Shinsuke Hashimoto
-
Publication number: 20090318481Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.Type: ApplicationFiled: August 28, 2009Publication date: December 24, 2009Inventors: Thomas Daniel AICHER, Guillermo S. CORTEZ, Todd Michael GROENDYKE, Albert KHILEVICH, James Allen KNOBELSDORF, Fredrik Pehr MARMSATER, Jeffrey Michael SCHKERYANTZ, Tony Pisal TANG
-
Patent number: 7618961Abstract: The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: GrantFiled: May 22, 2001Date of Patent: November 17, 2009Assignee: Biovitrum ABInventors: Tjeerd Barf, Rikard Emond, Guido Kurz, Jerk Vallgårda, Marianne Nilsson
-
Publication number: 20090233974Abstract: A compound having the formula or a pharmaceutically acceptable salt 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: May 22, 2009Publication date: September 17, 2009Applicant: ALLERGAN, INC.Inventor: David W. Old
-
Patent number: 7579366Abstract: The invention relates to epothilone analog represented by the formula I wherein (i) R2 is absent or oxygen; “a” can be either a single or double bond; “b” can be either absent or a single bond; and “c” can be either absent or a single bond, with the proviso that if R2 is oxygen then “b” and “c” are both a single bond and “a” is a single bond; if R2 is absent then “b” and “c” are absent and “a” is a double bond; and if “a” is a double bond, then R2, “b” and “c” are absent; R3 is a radical selected from the group consisting of hydrogen; lower alkyl; —CH?CH2; —C?CH; —CH2F; —CH2Cl; —CH2—OH; —CH2—O—(C1-C6-alkyl); and —CH2—S—(C1-C6-alkyl); R4 and R5 are independently selected from hydrogen, methyl or a protecting group; and R1 is as defined in the specification, or a salt of a compound of the formula I where a salt-forming group is present. A further aspect of the invention is related to the synthesis of epothilone E.Type: GrantFiled: March 11, 2003Date of Patent: August 25, 2009Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Nigel Paul King, Maurice Raymond Verschoyle Finlay, Yun He, Frank Roschangar, Dionisios Vourloumis, Hans Vallberg, Antony Bigot
-
Publication number: 20090209590Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel inhibitors of histone deacetylases, tubulin deacetylases, and/or aggresome inhibitors, and pharmaceutically acceptable salts and derivatives thereof. The inventive compounds fall into two classes—“isotubacin” class and “isoisotubacin” class—all of which include a 1,3-dioxane core. The present invention further provides methods for treating disorders regulated by histone deacetylase activity, tubulin deacetylase activity, and/or the aggresome (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, protein degradation disorders, protein deposition disorders, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.Type: ApplicationFiled: May 2, 2007Publication date: August 20, 2009Inventors: Ralph Mazitschek, Nicholas Paul Kwiatkowski, James Elliot Bradner
-
Publication number: 20090176837Abstract: Disclosed herein are novel compounds with activity at RAR? 2 receptors. Further disclosed are the use of such compounds for treatment of or to alleviate symptoms of cancer, neurological disorders such as memory deficits and schizophrenia, neurodegenerative disorders such as Parkinson's and Alzheimer's diseases, inflammatory disorders such as psoriasis and rheumatoid arthritis, eye disorders and depression.Type: ApplicationFiled: July 12, 2006Publication date: July 9, 2009Applicant: SONY CORPORATIONInventors: Roger Olsson, Fabrice Piu, Birgitte Lund
-
Publication number: 20090143446Abstract: Substituted thiazolidinone carboxylic acid amides and substituted thiazolidine carboxylic acid amides according to formulae (I) and (II) are disclosed where the various substituent groups are as defined in the specification. Methods of making these compounds, pharmaceutical compositions containing the compounds, and their use, particularly for treating or preventing cancer, are also disclosed.Type: ApplicationFiled: October 22, 2007Publication date: June 4, 2009Applicants: OHIO STATE UNIVERSITY RESEARCH FOUNDATIONInventors: Duane D. Miller, Veeresa Gududuru, James T. Dalton, Eunju Hurh
-
Publication number: 20090105257Abstract: The present invention relates generally to novel therapeutic compounds and more particularly to novel compounds, their use as GPR40 agonists, processes for their manufacture, and intermediates useful in their preparation.Type: ApplicationFiled: November 15, 2004Publication date: April 23, 2009Inventors: David Francis Corbett, Kate Anna Dwornik, Dulce Maria Garrido, Stephen Carl McKeown, Wendy Yoon Mills, Andrew James Peat, Terrence Lee Smalley, JR.
-
Patent number: 7511059Abstract: The invention relates to thiazolidinones of general formula (I) their production and use as inhibitors of polo-like kinases (Plk) for treating various diseases.Type: GrantFiled: February 2, 2006Date of Patent: March 31, 2009Assignee: Schering AgInventors: Volker Schulze, Knut Eis, Lars Wortmann, Dirk Kosemund, Olaf Prien, Gerhard Siemeister, Holger Hess-Stumpp, Uwe Eberspaecher, Damian O Arnaiz
-
Publication number: 20090075819Abstract: The present invention relates to Indanyl- and Tetrahydronaphtyl-amino-thiourea compounds of formula I wherein the variables R1 to R4 are as in the description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection.Type: ApplicationFiled: November 15, 2006Publication date: March 19, 2009Applicant: BASF SEInventors: Markus Kordes, Christopher Koradin, Deborah L. Culbertson
-
Patent number: 7498445Abstract: Disclosed are novel NO-donating compounds, designed such that when NO is released from the compound a residue which is a naturally occurring metabolite is formed, and thus a development of tolerance to the compounds upon repetitive administration is prevented or decreased. Also disclosed are methods of preparing such NO-donating compounds, pharmaceutical compositions and medical devices containing such compounds and methods utilizing such compounds in the treatment of various medical conditions.Type: GrantFiled: November 4, 2005Date of Patent: March 3, 2009Assignee: Renopharm Ltd.Inventors: Peter Assaf, Elham Gazaleen-Mariee, Michael Naveh
-
Publication number: 20090054505Abstract: Disclosed herein is a compound represented by a formula Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: August 15, 2008Publication date: February 26, 2009Applicant: ALLERGAN, INC.Inventor: David W. Old
-
Publication number: 20090048225Abstract: The present invention provides a novel compound of Formula (I) or a pharmaceutically acceptable salt thereof, having histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another, embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.Type: ApplicationFiled: August 15, 2005Publication date: February 19, 2009Inventors: Don Richard Finley, Terry Patrick Finn, Philip Arthur Hipskind, William Joseph Hornback, Cynthia Darshini Jesudason, Takako Takakuwa
-
Publication number: 20080286219Abstract: Skin brightening compositions based on hydroquinone derivatives and methods of making and using the composition. The hydroquinone derivatives are 2-thio-hydroquinone derivatives.Type: ApplicationFiled: May 17, 2007Publication date: November 20, 2008Inventors: Michael Fitzpatrick Wempe, Jeffrey M. Clauson
-
Publication number: 20080167307Abstract: According to the present invention, a compound represented by the following formula (I) having a superior PPAR? agonist action and concurrently showing a hypolipidemic action can be provided, and further, a compound useful as a synthetic intermediate for the compound can be provided.Type: ApplicationFiled: November 4, 2005Publication date: July 10, 2008Applicant: Mitsubishi Phama CorporationInventors: Takashi Tozawa, Osamu Tsuruta, Hiroshi Kitajima, Yoshiyuki Aoki, Naoko Ando, Hiroki Tamakawa
-
Publication number: 20080139505Abstract: The present invention provides compounds of formula (I): pharmaceutical compositions thereof, and methods of using the same, processes or preparing the same, and intermediates thereof.Type: ApplicationFiled: November 15, 2005Publication date: June 12, 2008Inventors: Thomas Daniel Aicher, Guillermo S. Cortez, Todd Michael Groendyke, Albert Khilevich, James Allen Knobelsdorf, Fredrik Pehr Marmsater, Jeffrey Michael Schkeryantz, Tony Pisal Tang, Nicholas Andrew Magnus
-
Publication number: 20080132543Abstract: A compound comprising a prodrug of a prostaglandin EP4 agonist, wherein said prodrug is an ester, ether, or amide of a carbohydrate; or said prodrug is an ester, ether, or amide of an amino acid is disclosed herein. Maintenance of the colonic mucosal barrier by method comprising administering a therapeutically effective amount of a prostaglandin EP4 agonist to a colon of a mammal is also disclosed herein. Dosage forms, medicaments, and compositions, related thereto are also disclosed.Type: ApplicationFiled: October 24, 2005Publication date: June 5, 2008Inventors: Wha Bin Im, Yariv Donde, Mark Holoboski, David W. Old, Karen M. Kedzie, Daniel W. Gil, John E. Donello, Robert M. Burk, Todd Gac
-
Patent number: 7378530Abstract: Disclosed herein are various novel oxazolidinone, imidazolidinone, and thiazolidinone analogs and methods of treating cancer and/or microbial infection using these analogs. Particular 4-oxazolidinone compounds are shown to have anti-cancer and anti-microbial activity.Type: GrantFiled: February 21, 2006Date of Patent: May 27, 2008Assignee: Nereus Pharmaceuticals, Inc.Inventors: Venkata Rami Reddy Macherla, Benjamin Nicholson, Kin Sing Lam
-
Patent number: 7319104Abstract: Compounds of formula (1) or a pharmaceutically acceptable salt, solvate, acid isostere, or hydrolyzable ester thereof, are disclosed. Methods of making and using the compounds are also disclosed.Type: GrantFiled: February 25, 2003Date of Patent: January 15, 2008Assignee: SmithKline Beecham CorporationInventors: Rodolfo Cadilla, Brad Richard Henke, Millard H. Lambert, III, Guangcheng Kevin Liu, Jennifer Susan Smith
-
Patent number: 7300934Abstract: Compounds of the formula (I) wherein m, n, A, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.Type: GrantFiled: June 1, 2004Date of Patent: November 27, 2007Assignee: Roche Palo Alto LLCInventors: Tobias Gabriel, Nancy Elisabeth Krauss
-
Publication number: 20070232660Abstract: A compound comprising a prodrug of a prostaglandin EP4 agonist, wherein said prodrug is an ester, ether, or amide of an amino acid is disclosed herein. Maintenance of the colonic mucosal barrier by method comprising administering a therapeutically effective amount of a prostaglandin EP4 agonist to a colon of a mammal is also disclosed herein. Dosage forms, medicaments, and compositions, related thereto are also disclosed.Type: ApplicationFiled: March 19, 2007Publication date: October 4, 2007Inventors: Wha-Bin Im, Robert M. Burk, Mark Holoboski
-
Publication number: 20070225504Abstract: The present invention is directed to practical high-yielding synthetic processes for preparing 3,4-disubstituted-thiazolidin-2-ones, which do not compromise the absolute stereochemical integrity of the compounds. The present invention is also directed to novel compounds of 3,4-disubstituted-thiazolidin-2-ones. The compounds prepared by the present invention are useful in the synthesis and manufacture of compounds (such as latrunculins and/or their analogs) for treating diseases or conditions associated with inhibiting actin polymerization.Type: ApplicationFiled: March 22, 2007Publication date: September 27, 2007Inventors: Jonathan B. DeCamp, Paul S. Watson, Jin She
-
Patent number: 7173137Abstract: Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancers agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilization of microtubulin assembly. The analogs of epothilone are novel. Several of the analogs are demonstrated to have a superior cytotoxic activity as compared to epothilone A or epothilone B as demonstrated by their enhanced ability to induce the polymerization and stabilization of microtubules.Type: GrantFiled: December 9, 2003Date of Patent: February 6, 2007Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Yun He, Sacha Ninkovic, Joaquin Pastor, Frank Roschangar, Francisco Sarabia, Hans Vallberg, Dionisios Vourloumis, Nicolas Winssinger, Zhen Yang, Nigel Paul King, Maurice Raymond Verschoyle Finlay
-
Patent number: 7169930Abstract: Designed epoxide and cyclopropane epothilone analogs with substituted side-chains are disclosed and characterized with respect to their biological activities against a series of human cancer cell lines. Among the several bioactive analogs, the epothilone B analog with a thiomethyl thiazole ring stands out as the most potent.Type: GrantFiled: August 4, 2003Date of Patent: January 30, 2007Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Andreas Ritzen, Kenji Namoto
-
Patent number: 7166607Abstract: The present invention relates to substituted indoles of formula (I) useful as pharmaceutical compounds for treating respiratory disordersType: GrantFiled: May 27, 2003Date of Patent: January 23, 2007Assignee: AstraZeneca ABInventors: Roger Bonnert, Stephen Brough, Tony Cook, Mark Dickinson, Rukhsana Rasul, Hitesh Sanganee, Simon Teague
-
Patent number: 7166620Abstract: Compounds having general formula (I) are described, together with their use for the control of phytopathogenic fungiType: GrantFiled: December 11, 2002Date of Patent: January 23, 2007Assignee: Isagro Ricerca S.r.l.Inventors: Marilena Gusmeroli, Alessandro Ciapessoni, Franco Bettarini, Samuele Osti, Luigi Mirenna, Giovanni Camaggi, Alexia Elmini, Ramona Gironda
-
Patent number: 7141533Abstract: The present invention relates to novel compounds of the formula (I) in which A, B, W, G and Het are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: May 21, 2004Date of Patent: November 28, 2006Assignee: Bayer CropScience AGInventors: Reiner Fischer, Thomas Bretschneider, Axel Trautwein, Astrid Ullmann, Mark Wilhelm Drewes, Christoph Erdelen, Peter Dahmen, Dieter Feucht, Rolf Pontzen
-
Patent number: 7125863Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.Type: GrantFiled: April 26, 2001Date of Patent: October 24, 2006Assignee: Ferring BVInventors: David Michael Evans, Gary Robert William Pitt
-
Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
-
Patent number: 7084170Abstract: The present invention provides antineoplastic compounds of the formula: and antineoplastic methods.Type: GrantFiled: October 15, 2002Date of Patent: August 1, 2006Assignee: Eli Lilly and CompanyInventors: Cora Sue Grossman, Philip Arthur Hipskind, Ho-Shen Lin, Karen Lynn Lobb, Beatriz Lopez de Uralde Garmendia, Jose Eduardo Lopez, Mary Margaret Mader, Michael Enrico Richett, Chuan Shih, Alfonso De Dios
-
Patent number: 7026491Abstract: Novel compounds composition capable of inhibiting TNF? and having antiimmunoinflammatory and autoimmune properties useful in a pharmaceutical composition, such as for a drug containing this as an active ingredient; and a therapeutic method with the use of these novel compounds.Type: GrantFiled: July 19, 2001Date of Patent: April 11, 2006Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Jie Fei Cheng, Hirotaka Kashiwagi, Thomas Arrhenius, David Wallace, Mi Chen, Sovouthy Tith, Yoshiyuki Ono, Yoshiaki Watanabe
-
Patent number: 6960688Abstract: The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (I), Ring C is phenyl or a carbon linked heteroaryl ring substituted as defined within; R1 is an ortho substituent as defined within; n is 1 or 2; A-B is a linking group as defined within; R2 and R3 are as defined within; R4 is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described.Type: GrantFiled: October 23, 2002Date of Patent: November 1, 2005Assignee: AstraZeneca ABInventors: Roger J Butlin, Thorsten Nowak, Jeremy N Burrows, Michael H Block
-
Patent number: 6890942Abstract: The present invention relates a series of compounds of Formula I wherein R1, R2, R3, and B are as defined in the specification. The compounds are useful for the inhibition of HIV integrase and for the treatment of AIDS or ARC by administering compounds of the formula.Type: GrantFiled: May 5, 2004Date of Patent: May 10, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Walker, Hatice Belgin Gulgeze, Jacques Banville, Roger Remillard, Donald Corson
-
Patent number: 6806369Abstract: PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: November 5, 2002Date of Patent: October 19, 2004Assignee: SmithKline Beecham CorporationInventors: Kelly M. Aubart, Siegfried B. Christensen, IV, Jacques Briand, Maxwell David Cummings
-
Patent number: 6787552Abstract: Compounds of the general formula (I) or salts thereof and activators of PPAR&dgr; (peroxisome proliferator activated receptor &dgr;) containing the compounds or the salts as the active ingredient: wherein R1 and R2 each are hydrogen, C1-8 alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X1 and X2 are each a free valency, oxygen, S(O)p (wherein p is an integer of 0 to 2), C(═O), C(═O)NH, NHC(═O), CH═CH, or the like; Y is optionally substituted C1-8 alkylene; Z is oxygen or sulfur; R3 and R4 are each optionally substituted C1-8 alkyl; and R8 is hydrogen or C1-8 alkyl, with the proviso that when X1 is a free valency, X2 is not O or S(O)p, while when X1 is C(═O)NH, X2 is not a free valency.Type: GrantFiled: February 11, 2003Date of Patent: September 7, 2004Assignee: Nippon Chemiphar Co., Ltd.Inventors: Shogo Sakuma, Tsuyoshi Endo, Atsushi Tendo, Toshihiro Takahashi, Shinichi Yoshida, Kunio Kobayashi, Nobutaka Mochizuki, Tomio Yamakawa, Takashi Kanda, Seiichiro Masui
-
Patent number: 6777418Abstract: The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.Type: GrantFiled: October 1, 2001Date of Patent: August 17, 2004Assignee: Syntex (U.S.A.) LLCInventors: Jean-Marc Lapierre, David Mark Rotstein, Eric Brian Sjogren
-
Patent number: 6770764Abstract: A compound of the formula (I) wherein R1 is a protecting group for N&agr;, R2 is a protecting group for NG, and R3 is aryl, and wherein the compound of formula (I) is a trypsin substrate such that trypsin cleaves the O—C single bond, which liberates R3—OH; a diagnostic device comprising same; a method for preparing the diagnostic device; and a method of using the diagnostic device to detect levels of urinary trypsin inhibitor in a biological sample; and a diagnostic kit for detecting levels of urinary trypsin inhibitor in a biological sample.Type: GrantFiled: April 30, 2001Date of Patent: August 3, 2004Assignee: Bayer CorporationInventors: Paul F. Corey, Steven W. Felman, Gary E. Rehm, Michael J. Pugia
-
Patent number: 6762198Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where J, M, Q, T, W, X, Z, R1, R2, R3, R4, R4′, R5, R6, R6′, R7, m, and n have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also disclosed are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.Type: GrantFiled: March 25, 2003Date of Patent: July 13, 2004Assignee: The Procter & Gamble CompanyInventors: Menyan Cheng, Neil Gregory Almstead, Michael George Natchus, Stanislaw Pikul, Biswanath De
-
Patent number: 6713477Abstract: A hydroxamic acid derivative represented by formula (1) or a prodrug thereof, or a pharmaceutically acceptable salt thereof, which has a matrix metalo-proteinase inhibitor.Type: GrantFiled: November 9, 2001Date of Patent: March 30, 2004Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Gerard Robert Scarlato, Sara Sabina Hadida Ruah, Tamiki Nishimura, Masashi Nakatsuka, Fumio Samizo, Yumiko Kamikawa, Hitoshi Houtigai
-
Patent number: 6696475Abstract: The present invention discloses compounds having the formula wherein the substituents are defined in the application. The compounds are useful as chloride channel blockers.Type: GrantFiled: August 8, 2001Date of Patent: February 24, 2004Assignee: NeuroSearch A/SInventors: Bjarne H. Dahl, Palle Christophersen
-
Patent number: 6696456Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where R1, R2, R3, R4, R5, R6, G and Z have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of Formula I, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions.Type: GrantFiled: October 13, 2000Date of Patent: February 24, 2004Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Norman Eugene Ohler, Kelly Michelle Solinsky, Neil Gregory Almstead, Biswanath De, Michael George Natchus
-
Patent number: 6656910Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: GrantFiled: August 10, 2001Date of Patent: December 2, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
-
Patent number: 6656911Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: GrantFiled: April 18, 2002Date of Patent: December 2, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W Spruce