Amide Patents (Class 562/455)
  • Patent number: 10995060
    Abstract: The present invention provides for crystalline Form B1 of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenyl-methyl)-4-amino-2R-methyl butanoic acid ethyl ester sodium salt, crystalline Form B2 of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-2R-methyl butanoic acid ethyl ester sodium salt, a novel process for the preparation of crystalline Form B of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-2R-methyl butanoic acid ethyl ester sodium salt.
    Type: Grant
    Filed: October 28, 2017
    Date of Patent: May 4, 2021
    Assignee: BIOCON LIMITED
    Inventors: Palle Venkata Raghavendra Charyulu, Pratik Rameshchandra Patel, Thirunelimada Devaiah Venu, Reddy Avathu Vidyasagar, Rajmahendra Shanmughasamy
  • Patent number: 9765017
    Abstract: Allosteric hemoglobin (Hb) modifiers of hemoglobin which contain nitric oxide (NO) moieties allowing for the release of NO in vivo. The compounds retain the oxygen delivery capability of the allosteric hemoglobin modifier to bind Hb and enhance Hb's ability to deliver oxygen to cells and tissues, and also release NO from the NO moiety. Methods of delivering oxygen and/or NO to cells and tissues are also provided.
    Type: Grant
    Filed: December 22, 2014
    Date of Patent: September 19, 2017
    Assignee: VIRGINIA COMMONWEALTH UNIVERSITY
    Inventors: Martin K. Safo, Richmond Danso-Danquah, Mohini Ghatge, Jurgen Venitz, Martin Mangino, Kevin R. Ward
  • Patent number: 9040553
    Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: May 26, 2015
    Assignee: CELL VIABLE CORPORATION
    Inventors: Iraj Lalezari, Jill Fabricant
  • Publication number: 20150126707
    Abstract: A method for the synthesis of daptomycin or a daptomycin analogue is carried out on a resin to form a linear precursor followed by a serine ligation macrocyclization in solution. Daptomycin analogues can differ from daptomycin by substitution of amino acids residues and/or deletion or addition of amino acid residues. Daptomycin analogues can include a different fatty acid in the side arm of the daptomycin analogue.
    Type: Application
    Filed: November 6, 2013
    Publication date: May 7, 2015
    Applicant: THE UNIVERSITY OF HONG KONG
    Inventors: Xuechen Li, Hiu Yung Lam
  • Publication number: 20150119428
    Abstract: Mew tranilast complexes and new tranilast cocrystals are disclosed. These include all tranilast nicotinamide complex, a 1:1 tranilast nicotinamide cocrystal, a 1:1 tranilast saccharin complex, a 1:1 tranilast saccharin cocrystal, a 1:1 tranilast gentisic acid complex, a 1:1 tranilast gentisic acid cocrystal, a 1:1 tranilast salicylic acid complex, a 1:1 tranilast salicylic acid cocrystal, a 1:1 tranilast urea complex, a 1:1 tranilast urea cocrystal, a 1:1 tranilast 4-amtnoben2oic acid complex, a 1:1 tranilast 4-am!nobers2oic acid cocrystal, a 1:1 tranilast 2,4-di?hydroxybenzoic acid complex and a 1:1 tranilast 2,4-dihydroxybenzoic acid cocrystal. Also disclosed are pharmaceutical compositions containing a tranilast complex or cocrystal of the invention and a pharmaceutically acceptable carrier. Methods of treatment using the tranilast complexes and cocrystais as well as the pharmaceutical compositions are disclosed.
    Type: Application
    Filed: March 29, 2013
    Publication date: April 30, 2015
    Inventors: Joanne Holland, Christopher Frampton
  • Publication number: 20150087758
    Abstract: The invention provides a compound conforming to the structure of Formula (CX) The invention also provides a thermoplastic polymer composition comprising a polyolefin polymer and a compound conforming to the structure of Formula (CX) as a nucleating agent.
    Type: Application
    Filed: September 22, 2014
    Publication date: March 26, 2015
    Inventors: Haihu Qin, Darin L. Dotson, Eduardo Torres, Sanjeev K. Dey, Francisco Alvarez
  • Publication number: 20150080400
    Abstract: The compounds of formula (1) in which R1, R4, A and X have the meanings as given in the description, are novel effective EP2 agonists.
    Type: Application
    Filed: April 30, 2013
    Publication date: March 19, 2015
    Applicant: TAKEDA GMBH
    Inventors: Angelika Hoffmeyer, Rainer Boer, Manuela Hessmann, Andreas Pahl, Torsten Dunkern, Simone Hartung, Christof Zitt, Jurgen Volz, Christiane Praechter, Mahindra Makhija, Hiteshkumar Jain, Sandip Gavade, Arati Prabhu, Manojkumar Tiwari, Ashish Keche, Sarvesh Patel
  • Publication number: 20150051407
    Abstract: The present invention relates to a novel process for preparing cis-alkoxy-substituted spirocyclic phenylacetylamino acid esters and cis-alkoxy-substituted spirocyclic 1H-pyrrolidine-2,4-dione derivatives, and also to novel intermediates and starting materials which are produced and/or used in the process according to the invention.
    Type: Application
    Filed: March 25, 2013
    Publication date: February 19, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Taraneh Farida, Berndt Maiwald, Martin Littmann, Winfried Etzel
  • Publication number: 20140357628
    Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof, with the proviso that the compound is no Tranilast.
    Type: Application
    Filed: June 27, 2014
    Publication date: December 4, 2014
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, David Stapleton, Steven Zammit, Darren James Kelly, Richard Ernest Gilbert, Henry Krum
  • Publication number: 20140350045
    Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
    Type: Application
    Filed: July 11, 2013
    Publication date: November 27, 2014
    Inventors: IRAJ LALEZARI, JILL FABRICANT
  • Publication number: 20140343151
    Abstract: The present invention provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof. Also, the present invention provides a pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. The present invention further provides methods for treating abdominal aortic aneurysm or atherosclerosis comprising administering a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of Formula (I) or pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: January 4, 2013
    Publication date: November 20, 2014
    Inventor: Douglas Richard Stack
  • Publication number: 20140329845
    Abstract: The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: March 4, 2014
    Publication date: November 6, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Pierre-Jean Colson, Miroslav Rapta, Ying Yu
  • Publication number: 20140309307
    Abstract: The present application relates to novel 3-phenylpropionic acid derivatives which carry a branched or cyclic alkyl substituent in the 3-position, 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 diseases.
    Type: Application
    Filed: June 13, 2014
    Publication date: October 16, 2014
    Inventors: Michael HAHN, Thomas LAMPE, Johannes-Peter STASCH, Karl-Heinz SCHLEMMER, Frank WUNDER, Volkhart Min-Jian LI, Eva-Maria BECKER, Friederike STOLL, Andreas KNORR, Elisabeth WOLTERING
  • Publication number: 20140235592
    Abstract: The present invention relates to substituted 6-methoxy-4-amino-N-phenyl-2-naphtamides derivatives, processes for preparing them, pharmaceutical compositions to containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 19, 2014
    Publication date: August 21, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im
  • Publication number: 20140221435
    Abstract: The invention relates to amide compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.
    Type: Application
    Filed: January 29, 2014
    Publication date: August 7, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
  • Publication number: 20140220050
    Abstract: The present invention provides dihydroorotate dehydrogenase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders wherein the inhibition of Dihydroorotate dehydrogenase is known to show beneficial effect.
    Type: Application
    Filed: February 4, 2014
    Publication date: August 7, 2014
    Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SA
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Prashant Kashinath Bhavar, Srikant Viswanadha, Swaroop Kumar V.S. Vakkalanka, Gayatri Swaroop Merikapudi
  • Patent number: 8754127
    Abstract: Disclosed herein are compounds that may be specific to PPAR and/or EGF receptors, and methods of making and using same.
    Type: Grant
    Filed: February 16, 2010
    Date of Patent: June 17, 2014
    Assignee: Nogra Pharma Limited
    Inventors: Sergio Baroni, Salvatore Bellinvia, Francesca Viti
  • Publication number: 20140088158
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, 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: Application
    Filed: November 27, 2013
    Publication date: March 27, 2014
    Applicant: SANOFI
    Inventors: Josef PERNERSTORFER, Heinz-Werner KLEEMANN, Matthias SCHAEFER, Alena SAFAROVA, Marcel PATEK
  • Patent number: 8552033
    Abstract: 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: Grant
    Filed: December 17, 2008
    Date of Patent: October 8, 2013
    Assignee: SANOFI
    Inventors: Stephanie Hachtel, Juergen Dedio, Stephen Shimshock, Carolina Lanter
  • Publication number: 20130261185
    Abstract: 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: Application
    Filed: October 8, 2012
    Publication date: October 3, 2013
    Applicant: Glaxo Group Limited
    Inventors: Alessandra Gaiba, Mark Patrick Healy, Christopher Norbert Johnson, Susan Roomans, Steven James Stanway, Martin Edward Swarbrick
  • Publication number: 20130237573
    Abstract: A mGlu2/3 receptor antagonist of the formula: its uses, and methods for its preparation are described.
    Type: Application
    Filed: November 15, 2011
    Publication date: September 12, 2013
    Applicant: ELI LILLY AND COMPANY
    Inventors: Bruce Anthony Dressman, Mark Donald Chappell, Adam Michael Fivush, Charles Howard Mitch, Paul Leslie Ornstein, Eric George Tromiczak, Tatiana Natali Vetman
  • Publication number: 20130237542
    Abstract: The present invention relates to a compound inhibiting HF-1 activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention demonstrates anticancer activity not by non-selective cytotoxicity but by inhibiting the activity of HIF-1, the transcription factor playing an important role in cancer cell growth and metastasis. Accordingly, the compound or the pharmaceutically acceptable salt thereof according to the present invention inhibits HIF-1 activity, and therefore can be used as a therapeutic agent for solid tumors such as colon cancer, liver cancer, stomach cancer and breast cancer. In addition, the compound or the pharmaceutically acceptable salt thereof according to the present invention can be used as an active ingredient for a therapeutic agent for diabetic retinopathy or arthritis which may become worse when hypoxia-induced VEGF expression by HIF-1 increases.
    Type: Application
    Filed: October 17, 2011
    Publication date: September 12, 2013
    Applicants: DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION, KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
    Inventors: Kyeong Lee, Mi Sun Won, Hwan Mook Kim, Song Kyu Park, Kiho Lee, Ki Hoon Lee, Chang Woo Lee, Jung Joon Lee, Kyung Sook Chung, Bo Kyung Kim, Yinglan Jin, Seung-hee Lee
  • Publication number: 20130225605
    Abstract: 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: Application
    Filed: April 22, 2013
    Publication date: August 29, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • Patent number: 8492437
    Abstract: 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: Grant
    Filed: April 17, 2012
    Date of Patent: July 23, 2013
    Assignee: Array BioPharma Inc.
    Inventors: George A. Doherty, Adam Cook
  • Patent number: 8492582
    Abstract: The invention relates to an N-acyl anthranilic acid derivative or it's salt having collagen production inhibitory action.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: July 23, 2013
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe
  • Publication number: 20130184343
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.
    Type: Application
    Filed: March 4, 2013
    Publication date: July 18, 2013
    Applicants: Syngenta Crop Protection LLC, Syngenta Participations AG
    Inventor: Syngenta Participations AG
  • Publication number: 20130079412
    Abstract: The present application relates to novel 3-phenylpropionic acid derivatives which carry a branched or cyclic alkyl substituent in the 3-position, 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 diseases.
    Type: Application
    Filed: March 27, 2012
    Publication date: March 28, 2013
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Michael HAHN, Thomas LAMPE, Johannes-Peter STASCH, Karl-Heinz SCHLEMMER, Frank WUNDER, Volkhart Min-Jian LI, Eva-Maria BECKER, Friederike STOLL, Andreas KNORR, Elisabeth WOLTERING
  • Publication number: 20130030061
    Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Application
    Filed: October 8, 2012
    Publication date: January 31, 2013
    Applicant: BEZWADA BIOMEDICAL, LLC
    Inventor: BEZWADA BIOMEDICAL, LLC
  • Publication number: 20120322717
    Abstract: 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: Application
    Filed: May 22, 2009
    Publication date: December 20, 2012
    Inventors: Dakai Liu, Xiaofeng Li, Richard Jin, Yuaxin Liang, Wei Cheng, Riddhi Bhattacharyya, Guangrong Zhang
  • Patent number: 8327467
    Abstract: The anthranilic acid derivative or the salt thereof represented by the general formula wherein R1 and R2 are hydrogen atom, or the like; R3 is a phenyl, cycloalkyl or bicyclic heterocyclic group which may be substituted, or the like; R4 is a phenyl, cycloalkyl or pyridyl group which may be substituted, or the like; X1 is an alkylene or alkenylene group which may be substituted or a bond; X2 is the general formula —X3—X4— or —X4—X3—, wherein X3 is a sulfur atom, an imino group or a bond, or the like; X4 means an alkylene or alkenylene group which may be substituted or a bond; is useful for a remedy such as rheumatoid arthritis, osteoarthritis and carcinoma, because it shows MMP—13 production inhibitory effect.
    Type: Grant
    Filed: March 14, 2006
    Date of Patent: December 11, 2012
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Junichi Yokotani, Yoichi Taniguchi, Eiji Hara, Hitoshi Akitsu, Hidehiko Tanaka, Shuzo Anzai
  • Patent number: 8304538
    Abstract: A method of producing a compound represented by Formula (I), which comprises a step A of reacting an anthranilic acid compound with a carboxylic halide in the absence of a base, but does not comprise a step of isolating of an amide intermediate compound represented by Formula (II): wherein R1 represents a substituent; n1 is an integer of 0 to 4; R2 represents an n2-valent substituent or a linking group; and n2 is an integer of 1 to 4.
    Type: Grant
    Filed: September 25, 2008
    Date of Patent: November 6, 2012
    Assignee: FUJIFILM Corporation
    Inventors: Keizo Kimura, Takashi Kitagawa, Osamu Uchida
  • Publication number: 20120277223
    Abstract: The present invention relates to compounds of formula (I): wherein Q, G1, G2, and G3, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.
    Type: Application
    Filed: July 16, 2012
    Publication date: November 1, 2012
    Inventors: Andrew S. Judd, Mathew M. Mulhern, Rajesh R. lyengar, Philip R. Kym, Andrew J. Souers
  • Patent number: 8273794
    Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.
    Type: Grant
    Filed: May 16, 2005
    Date of Patent: September 25, 2012
    Assignee: Emisphere Technologies, Inc.
    Inventors: Maria Isabel Gomez-Orellana, David Gschneidner, Andrea Leone-Bay, Destardi Moye-Sherman, Stephen V. Pusztay, Parshuram Rath, Pingwah Tang, John J. Weidner, Jianfeng Song
  • Publication number: 20120232150
    Abstract: The invention provides antimicrobial compounds and compositions, and methods of using them. The compounds and compositions include, for example, a compound of any one of Formulas I-X. The invention further provides methods of preparing the compounds, and useful intermediates for their preparation. The compounds can possess highly specific and selective activity, such as antibacterial activity and/or enzymatic inhibitory activity. Accordingly, the compounds and compositions can be used to treat bacterial infections, or to inhibit or kill bacteria, either in vitro or in vivo.
    Type: Application
    Filed: August 31, 2010
    Publication date: September 13, 2012
    Inventors: Shahriar Mobashery, Dusan Hesek, Mayland Chang
  • Publication number: 20120232120
    Abstract: A compound of the formula: where X is phenyl substituted at the 3, 4 and 5 positions with R1, R2 or R3 which are selected from hydrogen, chloro, lower alkyl of 1 to 5 carbons, phenoxy, phenyl, naphthyl, or phenyl (lower) alkyl where the lower alkyl group has 1-5 carbon atoms and m is 0 or 1; Y is —CONH— or —NHCONH— where the nitrogen atoms are unsubstituted or substituted with other phenoxyisobutyric acid derivatives, or the residue of a phenoxyisobutyric acid and n is 0 or 1; Z is unsubstituted phenyl when m is 1 and n is 1; when Y is 0, X is 0; Z is also substituted.
    Type: Application
    Filed: March 8, 2012
    Publication date: September 13, 2012
    Inventors: IRAJ LALEZARI, JILL FABRICANT
  • Patent number: 8211333
    Abstract: Certain poly(oxyalkylene) colorants are disclosed along with method of preparation thereof. A method of using these colorants as fluorescent security taggants is also disclosed.
    Type: Grant
    Filed: February 22, 2011
    Date of Patent: July 3, 2012
    Assignee: Sun Chemical Corp.
    Inventors: Russell Schwartz, Don DeRussy, Dan Gloster, Steve Postle, Rakesh Vig, Ewell Cook, Tatiana Romanova
  • Patent number: 8203016
    Abstract: The use of specific compounds of the Formula 1 (and also corresponding mixtures) in particular as cosmetic agents for the inhibition of the substance P-induced release of histamine from mast cells is described.
    Type: Grant
    Filed: November 20, 2003
    Date of Patent: June 19, 2012
    Assignee: Symrise AG
    Inventors: Gerhard Schmaus, Holger Joppe, Martinia Herrmann, Christopher Sabater-Lüntzel, Tobias Vössing
  • Publication number: 20120149737
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-amido-aryl compounds of the following formula (for convenience, collectively referred to herein as “AAA compounds”), which, inter alia, are (selective) retinoic acid receptor ? (RAR?) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RAR?, and in the treatment of diseases and conditions that are mediated by RAR?, that are ameliorated by the activation of RAR?, etc., including cognitive disorders, memory impairment, memory deficit, senile dementia, Alzheimer's disease, early stage Alzheimer's disease, intermediate stage Alzheimer's disease, late stage Alzheimer's disease, cognitive impairment, and mild cognitive impairment.
    Type: Application
    Filed: September 1, 2010
    Publication date: June 14, 2012
    Applicant: KING'S COLLEGE LONDON
    Inventors: Jonathan Patrick Thomas Corcoran, Sarkis Barret Kalindjian, Alan David Borthwick, David Reginald Adams, Jane Theresa Brown, David Michel Adrien Taddei, Jason John Shiers
  • Patent number: 8183289
    Abstract: 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: Grant
    Filed: August 21, 2007
    Date of Patent: May 22, 2012
    Assignee: Array BioPharma Inc.
    Inventors: George Doherty, Adam Cook
  • Publication number: 20120071502
    Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
    Type: Application
    Filed: September 13, 2011
    Publication date: March 22, 2012
    Applicant: CELL VIABLE CORPORATION
    Inventors: Iraj Lalezari, Jill Fabricant
  • Publication number: 20120059188
    Abstract: 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: Application
    Filed: December 19, 2008
    Publication date: March 8, 2012
    Applicants: The University of Melbourne, Fibrotech Therapeutics Pty Ltd
    Inventors: Darren James Kelly, Spencer John Williams, Steven Zammit
  • Publication number: 20120053244
    Abstract: Disclosed herein are compounds that may be specific to PPAR and/or EGF receptors, and methods of making and using same.
    Type: Application
    Filed: February 16, 2010
    Publication date: March 1, 2012
    Inventors: Sergio Baroni, Salvatore Bellinvia, Francesca Viti
  • Publication number: 20120046293
    Abstract: The present invention relates to renin inhibitor compounds having the structure and their use in treating cardiovascular events and renal insufficiency.
    Type: Application
    Filed: October 10, 2011
    Publication date: February 23, 2012
    Applicant: Merck Frosst Canada Ltd.
    Inventors: CHRISTOPHER I. BAYLY, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
  • Publication number: 20120035175
    Abstract: The present invention relates to a salt selected from the group comprising the N-methyl-D-glucamine salt (NMG), the diethylamine salt (DEA) salt, the magnesium salt, the tromethamine salt, the choline salt, the L-arginine salt, the zinc salt, and the 4-(2-hydroxyethyl)morpholine (HEM) salt of compounds of the general formula (I) wherein X is selected from the group consisting of CH2, S, or O; D is O or S; R8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1; and q is 0 or 1; with the proviso that compounds wherein X?CH2, q=0, Y=unsubstituted phenyl and E=unsubstituted phenylene are excluded; or a hydrate thereof.
    Type: Application
    Filed: July 1, 2011
    Publication date: February 9, 2012
    Applicant: 4SC AG
    Inventors: Aldo AMMENDOLA, Julia DIEDERICHS, Johann LEBAN, Daniel VITT
  • Publication number: 20120028985
    Abstract: The present invention relates to the treatment and prevention of immunological and inflammatory disorders with a compound of formula (I) in combination with methotrexate,
    Type: Application
    Filed: November 6, 2009
    Publication date: February 2, 2012
    Applicant: 4SC AG
    Inventors: Manfred Gröppel, Johann Leban
  • Publication number: 20120015978
    Abstract: This invention provides well defined 6-alkyl or hydroxyalkyl-1-naphthamide or quinoline compounds for treating glaucoma or ocular hypertension.
    Type: Application
    Filed: June 27, 2011
    Publication date: January 19, 2012
    Applicant: ALLERGAN, INC.
    Inventor: David W. Old
  • Publication number: 20120004405
    Abstract: The present invention relates to a compound which is characterized by the formula (I) or a pharmaceutically acceptable salt, solvate, hydrate thereof, wherein the ring systems A and B are independently selected from a monosaccharide, aryl (preferably phenyl), a heteroaryl or cycloalkyl (preferably cyclohexan), preferably with all substituents in equatorial configurations; R1 is independently selected from alkyl (preferably C1 to C6), a substituted or unsubstituted phenyl, preferably CH3; R2 is H, alkyl (preferably C1 to C6), a carbohydrate in a glycosidic ?-linkage, preferably H; R3, R4, R5, and R6 are independently selected from H, (OH) hydroxy, alkyl preferably C1 to C6, alkoxy (preferably C1 to C6), amino, alkylamino (preferably C1 to C6), halogen, benzylamino, or benzoylamino; X is O, NH, alkylamino (NR), CO, S; and Y is O, NH, alkylamino (NR), CO, S.
    Type: Application
    Filed: December 14, 2009
    Publication date: January 5, 2012
    Inventor: Peter Prehm
  • Publication number: 20120004167
    Abstract: The invention relates to substituted (2-aryloxyacetylamino)phenylpropionic acid derivatives, and to the physiologically acceptable salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, R9 and A are each defined as specified, and the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.
    Type: Application
    Filed: July 5, 2011
    Publication date: January 5, 2012
    Applicant: SANOFI
    Inventors: Elisabeth DEFOSSA, Stefanie KEIL, Viktoria DIETRICH, Siegfried STENGELIN, Andreas HERLING, Guido HASCHKE, Thomas KLABUNDE
  • Publication number: 20110313154
    Abstract: 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: Application
    Filed: August 26, 2011
    Publication date: December 22, 2011
    Applicant: AJINOMOTO CO., INC.
    Inventors: Noriyasu KATAOKA, Kotaro OKADO, Tatsuhiro YAMADA, Koichi FUJITA, Tamotsu SUZUKI, Tatsuya OKUZUMI, Masayuki SUGIKI, Akinori TATARA
  • Publication number: 20110288066
    Abstract: 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: Application
    Filed: February 9, 2010
    Publication date: November 24, 2011
    Applicant: MERCK SERONO S.A.
    Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Christophe Cleva, Adeline Pretre