Amide Patents (Class 562/455)
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Publication number: 20110313154Abstract: A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c): (a) reacting an acyl phenylalanine derivative represented by the following formula (2): with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative; (b) converting the carboxy-asymmetric urea derivative into the corresponding quinazoline-dione derivative in the presence of a carboxyl group-activating agent: (c) if desired, substituting an N-alkyl group for the hydrogen atom bonded to the nitrogen atom present in the quinazoline-dione ring of the quinazoline-dione derivative using an N-alkylation agent and then deprotecting the resulting product, when the substituent R3? which is a group corresponding to R3 is protected.Type: ApplicationFiled: August 26, 2011Publication date: December 22, 2011Applicant: AJINOMOTO CO., INC.Inventors: Noriyasu KATAOKA, Kotaro OKADO, Tatsuhiro YAMADA, Koichi FUJITA, Tamotsu SUZUKI, Tatsuya OKUZUMI, Masayuki SUGIKI, Akinori TATARA
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Publication number: 20110288066Abstract: The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.Type: ApplicationFiled: February 9, 2010Publication date: November 24, 2011Applicant: MERCK SERONO S.A.Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Christophe Cleva, Adeline Pretre
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Patent number: 8034966Abstract: The present invention provides a process for the synthesis of substituted arylureidophenoxymethylpropionic acid and related compounds including bifunctional and tetrafunctional derivatives. The compounds are useful for inhibiting the formation of AGEs (Aminaglycation end products).Type: GrantFiled: May 15, 2009Date of Patent: October 11, 2011Assignee: Cell Viable CorporationInventors: Iraj Lalezari, Jill Fabricant
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Publication number: 20110245192Abstract: The present invention relates in general to a compound (activator) which is characterized by a formula selected from the following formulas A, B and/or C or a pharmaceutically acceptable salt thereof. The present invention further relates to pharmaceutical composition comprising the activator(s) of the invention and to their use in the treatment of (for treating) and/or preventing diseases or medical conditions which benefit from an increased transport of hyaluronan across a lipid bilayer. The present invention also relates to a method for manufacturing a pharmaceutical composition comprising the steps of formulating the activator defined herein in a pharmaceutically acceptable form.Type: ApplicationFiled: December 14, 2009Publication date: October 6, 2011Inventor: Peter Prehm
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Patent number: 7999132Abstract: An anthranilic acid derivative represented by the general formula (X) [wherein R1 represents hydrogen or a carboxy-protecting group; R2 represents optionally substituted phenyl, a heterocyclic group, etc.; R3 represents optionally substituted phenyl, a monocyclic heterocyclic group, etc.; X1 represents carbonyl, etc.; X2 represents optionally substituted alkylene group, a bond, etc.; X3 represents oxygen, a bond, etc.; and X4 represents a group represented by the general formula —X5—X6— or —X6—X5— (wherein X5 means oxygen, a bond, etc.; and X6 means optionally substituted alkylene, a bond, etc.)] or a salt of the derivative. The derivative or salt has the inhibitory activity of MMP-13 production and is hence useful as a therapeutic agent for articular rheumatism, osteoarthritis, cancer, etc.Type: GrantFiled: December 6, 2005Date of Patent: August 16, 2011Assignee: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Yoichi Taniguchi, Eiji Hara, Hitoshi Akitsu, Yukie Tada
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Patent number: 7989657Abstract: The invention is concerned with novel anthranilic acid derivatives of formula (I) wherein R1 to R14, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds are HM74A agonists and can be used as medicaments.Type: GrantFiled: June 3, 2009Date of Patent: August 2, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Uwe Grether, Nicole A Kratochwil, Robert Narquizian, Constantinos Panousis, Jens-Uwe Peters
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Publication number: 20110176998Abstract: The present invention features compositions and methods for detecting, selecting a treatment method for, monitoring, and treating a neoplasia associated with a viral infection.Type: ApplicationFiled: October 13, 2010Publication date: July 21, 2011Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Martin G. Pomper, Richard Ambinder, Jun O. Liu, Curtis R. Chong, Jianmeng Chen
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ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
Publication number: 20110152290Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: November 4, 2010Publication date: June 23, 2011Applicant: SANOFI-AVENTISInventors: Matthias SCHAEFER, Josef PERNERSTORFER, Dieter KADEREIT, Hartmut STROBEL, Werngard CZECHTIZKY, L. Charlie CHEN, Alena SAFAROVA, Aleksandra WEICHSEL, Marcel PATEK -
Publication number: 20110142765Abstract: Pharmaceutical compositions comprising at least one compound of the formula (I) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning —X— is e.g. and Y being e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or selectin binding.Type: ApplicationFiled: February 23, 2011Publication date: June 16, 2011Applicant: REVOTAR BIOPHARMACEUTICALS AGInventors: Ewald M. AYDT, Remo Kranich
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Publication number: 20110130438Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: ApplicationFiled: October 20, 2010Publication date: June 2, 2011Inventors: David Robert Bolin, Matthew Michael Hamilton
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Publication number: 20110130445Abstract: The present application relates to novel 3-phenylpropionic acid derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: October 28, 2010Publication date: June 2, 2011Applicant: Bayer Schering Pharma AktiengesellschaftInventors: Thomas LAMPE, Michael HAHN, Johannes-Peter STASCH, Karl-Heinz SCHLEMMER, Frank WUNDER, Sherif EL SHEIKH, Volkhart Min-Jian LI, Eva-Maria BECKER, Friederike STOLL, Andreas KNORR
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Publication number: 20110112187Abstract: The present invention relates to the use of tranilast and derivatives thereof for the preparation of a pharmaceutical composition for treating and/or preventing a neuronal condition where there is a need of neuroprotection and neuroregeneration. The invention furthermore relates to the use of tranilast and derivatives thereof for the in vitro differentiation of neuronal stem cells and the use of such pre-treated cells for stem cell therapy von neurological conditions.Type: ApplicationFiled: August 15, 2008Publication date: May 12, 2011Inventors: Armin Schneider, Anja Moraru, Carola Krüger, Rice Laage, Claudia Pitzer
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Publication number: 20110112140Abstract: The present invention relates to a novel compound having plasminogen activator inhibitor-1 (PAI-1) inhibitory activity, and a PAI-1 inhibitor comprising the compound as an active ingredient. The present invention further relates to a pharmaceutical composition that has an inhibitory action on PAI-1 activity and is useful in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. The novel compound is represented by the following general formula. Each symbol is defined as those in the specification.Type: ApplicationFiled: March 31, 2009Publication date: May 12, 2011Applicant: RENASCIENCE CO., LTD.Inventors: Toshio Miyata, Nagahisa Yamaoka, Hidehiko Kodama, Kenji Murano
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Publication number: 20110082209Abstract: A series of novel salt forms of (4-{[(5-{[(3-chlorophenyl)methyl]oxy}-2-methylphenyl)carbonyl]amino}-3-methylphenyl)acetic acid, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.Type: ApplicationFiled: June 8, 2009Publication date: April 7, 2011Inventors: Trevor Raymond Keel, Sarah Vallance
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Publication number: 20110077298Abstract: The invention relates to a retinoid derivative and pharmaceutical composition and use thereof. The compound of the invention is capable of preventing or treating hematological tumours, such as acute leukemia, chronic leukemia, multiple myeloma and lymphoma, solid tumours, such as liver cancer, rectal cancer, mammary cancer and esophagus cancer, and skin disorders, such as psoriasis and acne.Type: ApplicationFiled: May 31, 2009Publication date: March 31, 2011Applicants: ANHUI MEDICAL UNIVERSITY, Anhui New Star Pharmaceutical Development Co., LtdInventors: Feihu Chen, Jingbo Shi, Yuan Wang, Jun Li, Juan Shen, Jingjing Ruan, Fanrong Wu
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Patent number: 7888532Abstract: A two-photon probe for real-time monitoring of intracellular magnesium ions is provided. Specifically, the two-photon probe is represented by Formula 1: wherein R is H or CH2OCOCH3. The two-photon probe is very suitable for real-time imaging of intracellular magnesium ions. The two-photon probe shows 17-fold two-photon excited fluorescence enhancement in response to Mg2+, which is 7-fold stronger than commercial probes, thus enabling staining of cells in a greatly reduced amount. In addition, the two-photon probe has a sufficiently low molecular weight to stain cells and is very suitable for monitoring Mg2+ ions present in the deep tissue. Furthermore, the two-photon probe can be effectively used for the quantitative as well as qualitative detection of intracellular magnesium ions. Further provided are a method for preparing the two-photon probe and a method for real-time monitoring of intracellular magnesium ions using the two-photon probe.Type: GrantFiled: December 14, 2007Date of Patent: February 15, 2011Assignee: Korea University Industry and Academy Cooperation FoundationInventor: Bong-Rae Cho
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Publication number: 20110021815Abstract: The present invention relates to halogenated compounds of formula (I) with the substituents as described within the specification. The compounds may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation.Type: ApplicationFiled: December 19, 2008Publication date: January 27, 2011Applicants: Fibrotech Therapeutics Pty Ltd, The University of MelbourneInventors: Darren James Kelly, Spencer John Williams, Steven Zammit
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Publication number: 20100298436Abstract: An EP2-receptor agonist of the following structure is disclosed: which is useful in the treatment of pain, inflammation and lowering intraocular pressure.Type: ApplicationFiled: May 19, 2010Publication date: November 25, 2010Applicant: ALLERGAN, INC.Inventors: David F. Woodward, Jenny W. Wang
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Publication number: 20100298200Abstract: The present invention relates to the field of therapeutic methods to screen for compounds on the basis of their ability to influence Wnt activity. The screening process is applied to both a physical library of a series of compounds and a virtual library of compounds that affect Wnt activity. In one aspect, the virtual screening process could be carried out where a permutational library of small peptides is substituted for the small organic molecules. The inventive methods may be used to empirically test for effects on Wnt activity and may also be applied to any pair of proteins involved in protein-protein interactions.Type: ApplicationFiled: May 22, 2009Publication date: November 25, 2010Inventors: Dakai Liu, Xiaofeng Li, Richard Jin, Yuaxin Liang, Wei Cheng, Riddhi Bhattacharyya, Guangrong Zhang
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Publication number: 20100292215Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxy-steroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.Type: ApplicationFiled: March 27, 2007Publication date: November 18, 2010Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Soren Ebdrup, Henrik Sune Andersen
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Publication number: 20100285467Abstract: The present invention relates to a method of biological labeling that occurs via a free radical chain reaction. The labeling occurs due to deposition of a detectable reporter molecule from a media comprising a substance comprising at least two moieties of a peroxidase enzyme substrate (termed herein ‘cross-linker’) in a target site comprising peroxidase activity and a biological marker. The labeling reaction described herein may generally be used to detect targets in a host of experimental schemes for detecting and visualizing a biological or chemical target, including immunohistochemistry (IHC), in situ hybridization (ISH), antibody-based staining methods such as ELISA, Southern, Northern, and Western blotting, and others.Type: ApplicationFiled: September 16, 2008Publication date: November 11, 2010Applicant: DAKO DENMARK A/SInventors: Jesper Lohse, Kenneth Heesche Petersen
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Publication number: 20100286427Abstract: A compound represented by the following general formula (I): [R1 to R5 represent hydrogen atom, an alkyl group, or a trialkylsilyl group, X represents —NH—CO—, —CO—NH—, —N(COR6)—CO—, —CO—N(COR7)— (R6 and R7 represent a lower alkoxy group, or a carboxy-substituted phenyl group) etc.; and Z represents —Y—CH(R12)—COOH, —CHO, —CH?CH—COOH, or —COOR13 (Y represents a single bond, —CH2—, —CH(OH)—, —CO—, —CO—NH—, or —CO—NH—CH2—CO—NH—, R12 represents hydrogen atom or a lower alkyl group, and R13 represents hydrogen atom, —CH(R14)—COOH(R14 represents hydrogen atom, a lower alkyl group, or hydroxy group), —[CH2CH2—O]n—CH2—CH2—OH, —CH2—O—[CH2CH2—O]m—CH2—OH, or —[CH(CH3)—CO—O]p—CH(CH3)—COOH (m, n and p represent an integer of 1 to 100))], a salt thereof or an ester thereof, which has a property of being converted into a retinoid after absorption in vivo.Type: ApplicationFiled: October 31, 2007Publication date: November 11, 2010Applicant: RESEARCH FOUNDATION ITSUU LABORATORYInventors: Hideaki Muratake, Koichi Shudo
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Publication number: 20100280081Abstract: The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, for the use as a medicament.Type: ApplicationFiled: May 3, 2010Publication date: November 4, 2010Applicant: 4SC AGInventors: Daniel VITT, Manfred GROEPPEL, Roland BAUMGARTNER, Johann LEBAN
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Publication number: 20100280034Abstract: The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;Type: ApplicationFiled: December 28, 2007Publication date: November 4, 2010Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20100267778Abstract: The present invention relates to a compound represented by formula (I): wherein ring A, ring B and ring D each independently represents a cyclic group which may have a substituent(s); W is a spacer having 1 to 8 atom(s) in its main chain; X is a spacer having 1 to 2 atom(s) in its main chain; Y is a binding bond or a spacer having 1 to 8 atom(s) in its main chain; and Z is an acidic group, or a salt thereof, a solvate thereof or a prodrug thereof. The compound represented by formula (I) has a PPAR ? agonistic action and is useful as a preventive and/or treating agent for diseases where sugar and lipid metabolisms are abnormal (diabetes, hyperlipemia, arteriosclerosis, cardiovascular diseases, obesity and metabolic syndrome or the like), hypertension, circulatory diseases and skin inflammation diseases.Type: ApplicationFiled: August 3, 2004Publication date: October 21, 2010Inventors: Shinya Kusuda, Yoshisuke Nakayama, Masaki Ima, Hisao Tajima, Sachiko Kato
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Patent number: 7807445Abstract: Fermentation of a nutrient medium with a eubacterium Streptomyces sp. yields a novel antibacterial compound of structural formula (I).Type: GrantFiled: May 20, 2005Date of Patent: October 5, 2010Assignees: Merck Sharp and Dohme de Espana, S.A., Merck Sharp & Dohme Corp.Inventors: Angela Basilio, Olga Genilloud, Hiranthi Jayasuriya, Ignacio Gonzalez, Sheo B. Singh, Oscar Salazar, Jun Wang
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Patent number: 7803951Abstract: Substituted aryl and heteroaryl derivatives are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: March 24, 2006Date of Patent: September 28, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Rui Liang, Emma R. Parmee
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Publication number: 20100233097Abstract: Compounds of formula (I) RA—CO—N(R2)—(CR12)n—N(R5)—RB and salts or optical active isomers thereof, wherein each R1 independently are the same or different and denotes a hydrogen atom, a hydroxyl group, a C1 to C4 straight of branched alkyl group or a C1 to C4 straight of branched oxyalkyl group; R2 denotes a hydrogen atom or a C1 to C4 straight of branched alkyl group; R5 independently are the same or different and denotes a acyl moiety; RA and RB independently are the same or different and denote a triiodinated phenyl group, preferably a 2,4,6-triiodinated phenyl group further substituted by two groups R3 in the 3 and 5 positions wherein each R3 are the same or different and denote a hydrogen atom or a non-ionic hydrophilic moiety, provided that at least one R3 group in the compound of formula (I) is a hydrophilic moiety; and n denotes a positive integer of 1 to 6.Type: ApplicationFiled: November 6, 2008Publication date: September 16, 2010Inventors: Veronique Morrison-Iverson, Duncan George Wynn
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Publication number: 20100173955Abstract: Compounds of Formula (I): in which R1, R2, R7, R8, R9, R10 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.Type: ApplicationFiled: August 21, 2007Publication date: July 8, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: George Doherty, Adam Cook
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Publication number: 20100113462Abstract: The present invention relates to novel compounds of the formula I: wherein in any of its stereoisomeric forms or a mixture of stereoisomeric forms in any ratio, or a physiologically acceptable salt thereof, wherein the substituents are as described herein. The inventive compounds have CXCR5 inhibitory activity are particularly useful in treating or preventing various inflammatory diseases, such as rheumatoid arthritis, multiple sclerosis, lupus, Crohn's Disease, associated with the modulation of the human CXCR5 receptor.Type: ApplicationFiled: November 30, 2009Publication date: May 6, 2010Applicant: SANOFI-AVENTISInventors: Thomas J. CAULFIELD, Jennifer Williford CLEMENS, Robert S. FRANCIS, Brian S. FREED, Stanly JOHN, Tieu-Binh LE, Brian PEDGRIFT, Antonio D. RAMOS, Gerard Charles ROSSE, Martin SMRCINA, David S. THORPE, William WIRE, Jianhong ZHAO
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Publication number: 20100022650Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R1, R2, R3, R4, R5, m, n and X are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.Type: ApplicationFiled: December 12, 2007Publication date: January 28, 2010Inventors: Alessandra Gaiba, Mark Patrick Healy, Christopher Norbert Johnson, Susan Roomans, Steven James Stanway, Martin Edward Swarbrick
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Publication number: 20090312519Abstract: A bismaleamic acid obtained by reacting a bifunctional phenylene ether oligomer diamine, obtained by introducing aromatic amino groups into both terminals of a specific bifunctional phenylene ether oligomer, with maleic anhydride, a bismaleimide obtained from the bismaleamic acid as a raw material, which bismaleimide has high heat resistance, low dielectric characteristics and excellent solvent solubility and exhibits only a small change in dielectric characteristics even in high humidity, a curable resin composition containing the above bismaleimide and a cured product obtained by curing the curable resin composition.Type: ApplicationFiled: June 9, 2009Publication date: December 17, 2009Inventors: Kazuyoshi Uera, Daisuke Ohno, Kenji Ishii
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Publication number: 20090264664Abstract: Mast cell degranulation inhibitors having a carboxyl group have not been developed as external preparations due to the low transdermal permeability thereof. By formulating external preparations thereof, side effects on the internal organs by oral administration can be avoided. Some of the mast cell degranulation inhibitors show drastically inferior photostability, which is also one cause of suppressed development of the drug as an external preparation. The present invention aims at improving the transdermal permeability and photostability of mast cell degranulation inhibitors by forming a salt of the mast cell degranulation inhibitor with an organic amine. Consequently, an external preparation of a mast cell degranulation inhibitor can be provided and the photostability of the mast cell degranulation inhibitor itself, and a preparation containing same can be improved.Type: ApplicationFiled: October 20, 2006Publication date: October 22, 2009Applicant: MEDRX CO., LTD.Inventors: Mitsuru Endo, Hidetoshi Hamamoto, Keiko Yamasaki, Sueko Matsumura
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Publication number: 20090239951Abstract: The invention relates to novel crystalline forms of 3-[[3,5-dibromo-4-[4-hydroxy-3-(1-methylethyl)-phenoxy]-phenyl]-amino]-3-oxopropanoic acid, said crystalline forms being characterised by a powder X-ray diffraction pattern having major peaks at either 2?=16.1±0.2, 20.1±0.2, 20.7±0.2, and 24.2+0.2; or 2?=9.0±0.2, 14.7±0.2, 19.6±0.2, 21.6±0.2, and 24.3+0.2.Type: ApplicationFiled: March 27, 2007Publication date: September 24, 2009Inventors: Ramakrishnan Chidambaram, Neeraj Garg, Ake Rasmuson, Sandra Gracin
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Patent number: 7589232Abstract: The present invention is related to alkynyl aryl carboxamides of Formula (I?) and use thereof for the treatment and/or prevention of an inflammatory disorder, obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia-hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkynyl aryl carboxamides of Formula (I?) to modulate, notably to inhibit the activity of PTPs. (I?) A is a C2-C15 alkynyl, C2-C6-alkynyl aryl, C2-C6-alkynyl heteroaryl. Cy is an aryl, heteroaryl, cycloalkyl or heterocycle group; n is either 0 or 1. Cy? is an aryl, which may optionally be fused by a 3-8 membered cycloalkyl. R1 and R2 are independently from each other is selected from the group consisting of hydrogen or (C1-C6)alkyl. R4 and R5 are each independently from each other selected from the group consisting of H, hydroxy.Type: GrantFiled: July 20, 2004Date of Patent: September 15, 2009Assignee: Laboratories Serono S.A.Inventors: Dominique Swinnen, Patrick Gerber, Jerome Gonzalez, Agnes Bombrun, Catherine Jorand-Lebrun
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Publication number: 20090215827Abstract: The invention relates to compounds of the formula I in which R1, R2, X, A, B and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: ApplicationFiled: December 17, 2008Publication date: August 27, 2009Applicant: SANOFI-AVENTISInventors: Stephanie HACHTEL, Juergen DEDIO, Stephen SHIMSHOCK, Carolina LANTER
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Publication number: 20090215780Abstract: This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: ApplicationFiled: April 18, 2006Publication date: August 27, 2009Applicant: Bayer Pharmaceuticals CorporationInventors: Roger Smith, Derek Lowe, Philip Coish, Ann-Marie Campbell, Gan Wang, Manoj Patel, Gerogiy Bondar
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Publication number: 20090062269Abstract: The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: February 2, 2007Publication date: March 5, 2009Inventors: Subharekha Raghavan, Darby Rye Schmidt, Steven L. Colletti, Abigail Lee Smenton
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Patent number: 7495030Abstract: (5-(2-hydroxy-4-chlorobenzoyl) aminovaleric acid, salts thereof, and compositions containing the same for the delivery of active agents are provided. Methods of administration, treatment of disease and preparation are provided as well.Type: GrantFiled: September 5, 2001Date of Patent: February 24, 2009Assignee: Emisphere Technologies, Inc.Inventor: David Gschneidner
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Patent number: 7351741Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provide as well.Type: GrantFiled: June 29, 2001Date of Patent: April 1, 2008Assignee: Emisphere Technologies, Inc.Inventors: John J. Weidner, Bruce F. Variano, Shingai Majuru, Satej Bhandarkar, William E. Bay, Lynn Sheilds
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Patent number: 7279597Abstract: Phenyl amine carboxylic acid compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: November 6, 2000Date of Patent: October 9, 2007Assignee: Emisphere Technologies, Inc.Inventors: Andrea Leone-Bay, Kelly Kraft, Maria A. P. Boyd
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Patent number: 7247654Abstract: The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel 3,4-disubstituted benzamidines and benzylamines, or a stereoisomer or pharmaceutically acceptable salt form thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor Xa, factor XIa, factor IXa, and/or factor VIIa. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.Type: GrantFiled: June 1, 2004Date of Patent: July 24, 2007Assignee: Bristol-Myers Squibb CompanyInventors: E. Scott Priestley, Xiaojun Zhang
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Patent number: 7223882Abstract: A process for a preparation of Compound (V), a pharmaceutically acceptable salt or a solvate thereof, said process comprising the steps represented by the following formula: wherein R1 and R2 are each independently C1–C8 alkyl.Type: GrantFiled: March 18, 2003Date of Patent: May 29, 2007Assignee: Shionogi & Co., Ltd.Inventors: Haruo Koike, Katsuo Oda, Yutaka Nishino, Makoto Kakinuma
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Patent number: 7199265Abstract: This invention relates to compounds of the formula (I) which are thyroid receptor ligands, and are preferably selective for the thyroid hormone receptor ?, to methods of preparing such compounds and to methods for using such compounds such as in the regulation of metabolism.Type: GrantFiled: June 15, 2001Date of Patent: April 3, 2007Assignee: Karo Bio ABInventors: Li Yi-Lin, Johan Malm, Chris Litten, Ana Maria Garcia Collazo, Neeraj Garg
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Patent number: 7151191Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: January 12, 2001Date of Patent: December 19, 2006Assignee: Emisphere Technologies, Inc.Inventors: Maria Aurora P. Boyd, Andrea Leone-Bay, Doris C. O'Toole
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Patent number: 7067119Abstract: Modified amino acid compounds useful in the delivery of active agents are provided. The active agents can be peptides. Methods of administration, such as oral, subcutaneous, sublingual, and intranasal administration and methods of preparation of the modified amino acid compounds are also provided.Type: GrantFiled: July 9, 2003Date of Patent: June 27, 2006Assignee: Emisphere Technologies, Inc.Inventors: Andrea Leone-Bay, Koc-Kan Ho, Donald J. Sarubbi, Sam J. Milstein
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Patent number: 7056707Abstract: The present invention relates to a novel compound having a molecular formula C13H15NO5 having molecular structure of Formula I and a process for the isolation of said compound. The present invention also relates to a method of inhibiting 13-lipoxygenase and having free radical scavenging activity.Type: GrantFiled: December 2, 2003Date of Patent: June 6, 2006Assignee: Council of Scientific and Industrial ResearchInventors: Avinash Prahlad Sattur, Chandrasekhar Rao Kadiyala, Divakar Soundar, Karanth Naikanakatte Ganesh, Tumkur Ramachandraiah Shamala, Appu Rao Appu Rao Gopal Rao
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Patent number: 7053245Abstract: This invention relates to N-acylamino aryl derivatives of the formula where R1, R21, R22, R23, R24, R3, R4, R5, R6, R7, R8, R, and n are as defined herein and where X is —CHRO, —OCHR—, —CH2S—, —SCH2—, —CH2CH2—, —CH?CH— or —C?C—. The compounds of the invention are selective monoamine oxidase B inhibitors, and they are therefore useful in the treatment of diseases mediated by monoamine oxidase B, for example, for the treatment of Alzheimer's disease or senile dementia.Type: GrantFiled: May 5, 2004Date of Patent: May 30, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Patent number: 7030133Abstract: The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become disturbed by these modifications and can result in severe consequences. The compounds of the present invention can be used to inhibit this process of nonenzymatic glycation and therefore to inhibit some of the ill effects caused by diabetes or by aging. The compounds are also useful for preventing premature aging, spoilage of proteins in food and can prevent discoloration of teeth.Type: GrantFiled: February 5, 2003Date of Patent: April 18, 2006Assignee: City of HopeInventors: Samuel Rahbar, Iraj Lalezari
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Patent number: 7026510Abstract: (R)-Enantiomers of quaternary ammonium salts of general formula (I) are described: where R, R1, R2, R3, X and Z are as defined in the description. The process for their preparation and pharmaceutical preparations thereof are also described. The quaternary salts of the invention are useful in the inhibition of chemotaxis of neutrophils and monocytes induced by the fraction C5a of the complement and are used in the treatment of psoriasis, pemphigus and pemphigoid, rheumatoid arthritis, intestinal chronic inflammatory pathologies including ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, cystic fibrosis, chronic obstructive pulmonary disease and glomerulonephritis. The compounds of the invention are advantageously used in the prevention and the treatment of injury caused by ischemia and reperfusion.Type: GrantFiled: September 25, 2002Date of Patent: April 11, 2006Assignee: Dompé S.p.A.Inventors: Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta