Sulfohydroxamate Esters Or Chalcogen Analogues Thereof (i.e., Compounds Having The -s(=o)(=o)-nh-x- Group, Wherein X Is Chalcogen And Substitution May Be Made For Hydrogen Only, And Wherein The X Is Bonded Directly To Carbon, Which Carbon May Be Single Bonded To Any Atom But May Be Multiple Bonded Only To Carbon) Patents (Class 560/303)
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Patent number: 9115087Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: April 1, 2014Date of Patent: August 25, 2015Assignee: Novartis AGInventors: Urs Baettig, Anne-Marie D'Souza, Peter Hunt, Neil John Press, Simon James Watson
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Publication number: 20140221657Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.Type: ApplicationFiled: April 7, 2014Publication date: August 7, 2014Applicant: PRISM BioLab CorporationInventors: Hiroyuki Kouji, Yuji Kogami, Takenao Odagami
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Patent number: 8722925Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: September 12, 2012Date of Patent: May 13, 2014Assignee: Novartis AGInventors: Urs Baettig, Anne-Marie D'souza, Peter Hunt, Neil John Press, Simon James Watson
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Publication number: 20130005735Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: September 12, 2012Publication date: January 3, 2013Inventors: Urs Baettig, Anne-Marie D'souza, Peter Hunt, Neil John Press, Simon James Watson
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Patent number: 7674930Abstract: To prepare a polyester polyol in which a lactone is ring-opening addition polymerized with the compound represented by formula (I). (wherein each of A1 and A2 represents an alkylene group having not less than 2 carbon atoms, A3 represents an alkylene group, X represents a cationic component, and each of n and m represents an integer of not less than 1.) The polyester polyol has a high hydrophilic group and high solubility in a solvent (particularly, a low-boiling organic solvent used in the production of a polyurethane) and can design an aqueous polyurethane desirably and produce the aqueous polyurethane.Type: GrantFiled: August 3, 2006Date of Patent: March 9, 2010Assignee: Daicel Chemical Industries, Ltd.Inventors: Kazunori Nakao, Nobuyuki Watanabe
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Plasminogen Activator Inhibitor-1 Inhibitors And Methods Of Use Thereof To Modulate Lipid Metabolism
Publication number: 20090011055Abstract: The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels.Type: ApplicationFiled: April 16, 2008Publication date: January 8, 2009Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Daniel A. Lawrence, Dudley Strickland, Jacqueline Cale, Enming J. Su, Cory Emal, Mark Warnock -
Patent number: 7271188Abstract: The present invention provides a compound represented by formula (I): [Formula 1] wherein n is an integer selected from 1 to 20, and R1 and R2, which may be the same or different, each represent a hydrogen atom, or a linear or branched C1-C6 alkyl group, or a salt, a prodrug or a solvate thereof, as well as a drug, a pharmaceutical composition containing the compound, and the like.Type: GrantFiled: June 11, 2004Date of Patent: September 18, 2007Assignee: Chugai Seikayu Kabushiki KaishaInventors: Kazutaka Tachibana, Haruhiko Sato, Masateru Ohta, Mitsuaki Nakamura, Takuya Shiraishi, Ikuhiro Imaoka, Hitoshi Yoshino, Masahiro Nagamuta, Hiromitsu Kawata
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Patent number: 6465684Abstract: A diastereomer complex obtained via a process for the separation of enantiomers is disclosed, wherein separation can be rapidly effected such that enantiomers are obtained with high e.e. values. The process permits the separation of mixtures of enantiomers in which more than one resolving agent is used, of which at least one resolving agent is optically active, and which yields a diastereomer complex containing at least two resolving agents in optically active form. The process provides for, inter alia, a diastereomer complex having at least three compounds of which at least two compounds are resolving agents in optically active form, and at least one compound is an enantiomer in optically active form. Also provided is a diastereomer complex having at least three compounds of which at least one compound is a resolving agent in optically active form, and at least two compounds which are enantiomers in optically active form.Type: GrantFiled: February 16, 2001Date of Patent: October 15, 2002Assignee: DSM N.V.Inventors: Ton R. Vries, Hans Wijnberg, Erik Van Echten, Lumbertus A. Hulshof, Quirinus B. Broxterman
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Patent number: 6455582Abstract: Sulfohydroxamic acid diarylamines of formula (I), in which the variables are as defined in the claims, are inhibitors of MEK and are effective in the treatment of proliferative diseases, cancer, stroke, heart failure, xenograft rejection, arthritis, cystic fibrosis, hepatomegaly, cardiomegaly, Alzheimer's disease, complications of diabetes, septic shock, and viral infection.Type: GrantFiled: July 11, 2001Date of Patent: September 24, 2002Assignee: Warner-Lambert CompanyInventor: Haile Tecle
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Patent number: 6355805Abstract: The present invention is directed to multibinding compounds which are &bgr;3 adrenergic receptor agonists and are therefore useful in the treatment and prevention of metabolic disorders such as obesity, diabetes, and the like.Type: GrantFiled: June 8, 1999Date of Patent: March 12, 2002Assignee: Advanced Medicine, Inc.Inventors: Seok-Ki Choi, Edmund J. Moran
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Patent number: 5891909Abstract: Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: March 27, 1997Date of Patent: April 6, 1999Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Bruce E. Tomczuk, Carl Illig
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Patent number: 5475006Abstract: .beta.-Carotene and canthaxanthin, as representative carotenoids, and to a lesser extent, retinoic acid, a representative retinoid, undergo extensive oxidation to yield substances, insofar as oxidized .beta.-carotene is a model, which have properties useful as non-toxic agents active against cell proliferation, tumors, and tumorigenic viruses, and useful as promoters of cell differentiation. It is evident from chemical analysis of the highly oxidized .beta.-carotene product mixture that none of the various forms of vitamin A are present or are present only in minor amounts. Furthermore, the biological activities of oxidized canthaxanthin and retinoic acid, which cannot form, vitamin A, indicate the presence of active substances that are different from vitamin A. Although the anti-proliferative and differentiation promotion activities of oxidized .beta.-carotene resemble those of vitamin A itself, generally the effects are more powerful for oxidized .beta.-carotene in a wide variety of circumstances.Type: GrantFiled: August 10, 1994Date of Patent: December 12, 1995Assignee: National Research Council of CanadaInventors: Graham Burton, Janusz Daroszewski, Jenny Phipps
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Patent number: 5154912Abstract: The peroxides which include the O.sup.17 isotope, especially the hydrogen peroxides and peroxides and hydroperoxides prepared therefrom, are well adapted as nonradioactive labeled compounds for use in the medicinal and biological arts.Type: GrantFiled: September 20, 1990Date of Patent: October 13, 1992Assignee: AtochemInventors: Jean-Pierre Schirmann, Jean-Jacques Barieux
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Patent number: 5097063Abstract: The present invention relates to a process for the preparation of astaxanthin having the formula ##STR1## comprising the step of oxidizing a dienolether, a dienamine, or a dienolate anion of canthaxanthin with an oxaziridine oxidant to produce an astaxanthin dihemiaminal, and then decomposing the dihemiaminal to produce astaxanthin. The process advantageously involves two less steps than the best known prior art process for the preparation of astaxanthin.The invention also relates to important intermediates in the preparation of astaxanthin, which is itself an important additive in the fish industry, the most important of which intermediates is the astaxanthin dihemiaminal.Type: GrantFiled: December 24, 1990Date of Patent: March 17, 1992Assignee: NeuroSearch A/SInventor: Peter Moldt
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Patent number: 4985417Abstract: Method and formulation useful in treatment of glaucoma in a mammal wherein an effective amount of an active water soluble carbonic anhydrase inhibitor is administered, said inhibitor being a compound having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is selected from the group consisting of H, NH.sub.2 CH.sub.2 --, --CH(Me)NH.sub.2, --CH(NH.sub.2)CHMe.sub.2, --CH(NH.sub.2)CH.sub.2 CHMe.sub.2, --CH(NH.sub.2)CH(Me)CH.sub.2 Me, 2-pyrrolidinyl residues wherein the R.sup.1 CO-- constitutes an .alpha.-aminoacyl group, N-acetylaminoacyl derivatives and the corresponding dipeptidyl radicals wherein R.sup.1 CO-- is a dipeptidyl residue containing two amino acid residues of the formula where R.sup.1 is --CHR.sup.7 NHCOCHR.sup.8 NH.sub.2, R.sup.6 NHCHR.sup.5 --, ##STR2## and R.sup.6 NHCH.sub.2 CHR.sup.5 --; R.sup.2 is selected from the group consisting of H, alkyl having from 1 to 6 carbon atoms, alkenyl having from 2 to 6 carbon atoms, and cycloalkyl;R.sup.Type: GrantFiled: May 2, 1989Date of Patent: January 15, 1991Inventors: Seymour F. Trager, G. Michael Blackburn