The Nitrogen Is Bonded Directly To A Ring And Is In Same Side Chain As Ester Function Patents (Class 560/43)
-
Patent number: 7592373Abstract: Compounds of formula (I) wherein A, B, b, W, X, Y, Z, R1, R2, and R3 have the meanings given in claim 1, pharmaceutical compositions these compounds, and methods of preventing or treating metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia, and diabetes using these compounds.Type: GrantFiled: December 23, 2004Date of Patent: September 22, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Thorsten Lehmann-Lintz, Ralf R. H. Lotz, Philipp Lustenberger, Stephan Georg Mueller, Gerald Juergen Roth, Klaus Rudolf, Marcus Schindler, Dirk Stenkamp, Leo Thomas
-
Publication number: 20090221669Abstract: The present invention relates to a novel class of disubstituted aniline compounds. These compounds can inhibit hi-stone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: April 20, 2007Publication date: September 3, 2009Inventors: Richard Heidebrecht, Joey Methot, Dawn Mampreian, Thomas Miller, Phieng Siliphaivanh
-
Publication number: 20090163588Abstract: This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.Type: ApplicationFiled: February 25, 2009Publication date: June 25, 2009Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Philip Stewart Turnbull, Rodolfo Cadilla, David John Cowan, Andrew Lamont Larkin, Istvan Kaldor, Eugene Lee Stewart
-
Publication number: 20090151091Abstract: Disclosed are triarylmethane dyes of formula (1) D1-(Z1J)r-Y1—S-A, wherein A is hydrogen; a radical of formula (1b) *—S—Y2-(Z2)-D2; or a radical of formula (1c) *—S—Y3; Y1 and Y2 independently from each other are unsubstituted or substituted, straight-chain or branched, interrupted or uninterrupted C1-C10alkylene; C5-C10cycloalkylene; C5-C10arylene; or —C5-C10arylene-(C1-C10alkylene); Y3 is an unsubstituted or substituted, straight-chain or branched, interrupted or uninterrupted C1C10alkyl; C5-C10cycloalkyl; C5-C10aryl; or —C5-C10aryl-(C1-C10alkyl); Z1 and Z2 independently from each other are *—(CH2)p—C(O)—**; *—(CH2CH2—O)—**; *—(CH2)p—C(O)O—**; *—(CH2)p—OCO—**; —(CH2)p—N(R1)—**; —(CH2)p—CON(R1)—**; —(CH2)p—(R1)NC(O)—**; -0-; —S—; —S(O)—; —S(O)2—; or a cationic biradical of a substituted or unsubstituted aromatic or heteroaromatic compound of the formula (1a); (1b); (1c); (1d); or (1e); wherein the asterix * indicates the linkage to D1 and/or D2; the asterix ** indicates the linkage to Y1 and/or Y2; W1 is N oType: ApplicationFiled: September 27, 2006Publication date: June 18, 2009Inventors: Christian Cremer, Olof Wallquist
-
Publication number: 20090143330Abstract: The present invention relates to crystalline polymorphic forms of monosodium N-[8-(2-hydroxybenzoyl)amino] caprylate (“SNAC”), including two hydrates, a methanol solvate, and an ethanol solvate, of SNAC. More specifically, the present invention provide six polymorphic forms of SNAC (hereafter referred to as Forms I-VI). The present invention also provides an amorphous form of SNAC.Type: ApplicationFiled: May 6, 2005Publication date: June 4, 2009Applicant: Emisphere Technologies, Inc.Inventors: Halina Levchik, Shingai Majuru, Brahma Singh, Jamila Harris
-
Publication number: 20090137803Abstract: The present invention provides a production method of 5-aminopyrimidine compound represented by the formula (5) by reacting a glycine compound represented by the formula (1) with t-butoxybisdimethylaminomethane, dimethylformamidedimethylacetal or dimethylformamidediethylacetal to produce a dialkylaminomethylene compound represented by the formula (2), reacting the compound of formula (2) in the presence of an acid to produce a hydroxymethylene compound represented by the formula (3), and reacting the compound of formula (3) with an amidine compound represented by the formula (4) or a salt thereof.Type: ApplicationFiled: January 29, 2009Publication date: May 28, 2009Applicant: Ajinomoto Co., Inc.Inventors: Daisuke TAKAHASHI, Kunisuke IZAWA
-
Publication number: 20090136473Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: November 20, 2008Publication date: May 28, 2009Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Alexander Kiselyov, Munagala Rao, Timothy Hagen
-
Publication number: 20090111983Abstract: Cycloalkylcarbonylamino acid derivatives, which are raw material intermediates of a novel cycloalkane carboxamide derivative that selectively inhibits cathepsin K, and a production process thereof, are provided. A cycloalkylcarbonylamino acid derivative represented by the following general formula (I), or a pharmaceutically acceptable salt thereof: (wherein, R1 and R2 represent alkyl groups, alkenyl groups, alkynyl groups, aromatic hydrocarbon groups, heterocyclic groups or the like, and ring A represents a cyclic alkylidene group having 5, 6 or 7 carbon atoms).Type: ApplicationFiled: July 10, 2007Publication date: April 30, 2009Applicant: SEIKAGAKU CORPORATIONInventors: Nobuo Kobayashi, Tsuneo Koji, Hisatomo Kunii
-
Publication number: 20090105474Abstract: 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: ApplicationFiled: March 14, 2006Publication date: April 23, 2009Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Yoichi Taniguchi, Eiji Hara, Hitoshi Akitsu, Hidehiko Tanaka, Shuzo Anzai
-
Publication number: 20090105237Abstract: A method of conferring a cooling effect on the skin or mucous membranes by applying thereto at least one compound of the Formula I: (a) wherein B is selected from H, CH3, C2H5, OCH3, OC2H5; and OH; and (b) wherein A is a moiety of the formula —CO-D, wherein D is selected from the following moieties: (i) —NR1R2, wherein R1 and R2 are independently selected from H and C1-C8 straight or branched-chain aliphatic, alkoxyalkyl, hydroxyalkyl, araliphatic and cycloalkyl groups, or R1 and R2 together with the nitrogen atom to which they are attached form part of an optionally-substituted, five- or six-membered heterocyclic ring; (ii) —NHCH2COOCH2CH3, —NHCH2CONH2, —NHCH2CH2OCH3, —NHCH2CH2OH, —NHCH2CH(OH)CH2OH and (iii) a moiety selected from the group consisting of: The compounds are useful for providing cooling effects in a variety of products, such as foodstuffs, confectionery, tobacco products, beverages, cosmetics, dentifrices, medicinal preparations, mouthwashes and toiletries.Type: ApplicationFiled: May 24, 2006Publication date: April 23, 2009Inventors: Karen Ann Bell, Stefan Michael Furrer, Christophe C. Galopin, Pablo Victor Krawec, Jay Patrick Slack
-
Patent number: 7514578Abstract: The invention relates to a method for producing enantiomeris form of 2, 3-diaminopropionic acid derivatives of formula (I) by asymetric hydrogenation from compounds of formula (II).Type: GrantFiled: January 10, 2007Date of Patent: April 7, 2009Assignee: sanofi-aventis Deutschland GmbHInventors: Joerg Rieke-Zapp, Guenter Billen
-
Publication number: 20090076113Abstract: Novel biphenylcarboxamides of the formula (I) There is further provided a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: ApplicationFiled: December 5, 2006Publication date: March 19, 2009Applicant: Bayer CropScience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jorg Nico Greul, Herbert Gayer, Arnd Voerste, Ulrike Wachendorff-Neumann, Peter Dahmen
-
Publication number: 20090076145Abstract: The present application describes deuterium-enriched amibegron, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 22, 2008Publication date: March 19, 2009Applicant: Protia, LLCInventor: Anthony W. Czarnik
-
Publication number: 20090041955Abstract: This invention provides alignment materials for liquid crystal display device of vertical alignment mode and methods for the preparation of the same, and more particularly, it provides diaminobenzene derivatives represented by the following formula 1: wherein n is an integer of 1 to 5 and R is an alkyl or alkoxy group of 3 to 5 carbon atoms, which align liquid crystal in uniform and vertical way, have not only excellent mechanical properties such as heat resistance and surface strength but also high pretilt angles of liquid crystal and in particular, can make response rate of liquid crystal fast, methods for the preparation of the same and liquid crystal alignment films using the same.Type: ApplicationFiled: February 9, 2007Publication date: February 12, 2009Applicant: Dongjin Semichem Co., Ltd.Inventors: Jin wook Choi, Eung jae Park, Jae cheol Park, Yong bae Kim
-
Patent number: 7485742Abstract: A new class of non-glycosidic and non-peptidic inhibitors of selectins with low molecular weight according to the general formula 1 is described, as well as methods for their production. These compounds represent a new class of non-toxic, in vivo anti-inflammatory effective inhibitors of selectins, and do not exhibit the disadvantages of the glycosidic inhibitor complexes, and are furthermore more potent in vitro, compared to the known drug bimosiamose. Furthermore, medicaments containing the compounds and their uses in the treatment of diseases are described.Type: GrantFiled: July 26, 2005Date of Patent: February 3, 2009Assignee: Johannes Gutenberg-Universität MainzInventors: Gerd Dannhardt, Holger Ulbrich, Philip Prech, Andreas Luxenburger
-
Publication number: 20090023786Abstract: The present invention is directed to prodrugs of hydroxamic acid based histone deacetylase (HDAC) inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The prodrugs are acylated derivatives having increased aqueous solubility and cellular permeability as compared with the free hydroxamic acid, and are useful for inhibiting HDACs, and for selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the prodrugs of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The prodrugs of the invention are also useful in the prevention and treatment of thioredoxin (TRX)-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: April 5, 2005Publication date: January 22, 2009Applicant: Alton Pharma, Inc.Inventors: Thomas A. Miller, David J. Witter, Sandro Belvedere
-
Publication number: 20080305477Abstract: The present invention relates to novel iminecalixarene derivatives, method of preparation thereof, and self-assembled monolayer prepared by the method, fixing method of oligo-DNA by using the self-assembled monolayer, and oligo-DNA chip prepared by the method. Also, the present invention relates to novel aminocalixarene derivatives, method of preparation thereof, and self-assembled monolayer prepared by the method, fixing method of oligo-DNA wherein the oligo-DNA is voluntarily fixed by molecular recognition on said self-assembled monolayer in a liquid phase, and oligo-DNA chip prepared by the method.Type: ApplicationFiled: May 11, 2006Publication date: December 11, 2008Inventors: Tae Sun Kim, Keum Soo Song, Jung Hoon Kim, Hyung Sub Kim
-
Publication number: 20080269220Abstract: A compound represented by the formula (1): wherein each symbol is as defined in the specification, and a salt thereof and a prodrug thereof unexpectedly have superior GPR40 receptor agonist activity, superior in the properties as a pharmaceutical product such as stability and the like, and can be a safe and useful pharmaceutical agent as a drug for the prophylaxis or treatment of GPR40 receptor related pathology or diseases such as diabetes and the like.Type: ApplicationFiled: March 14, 2005Publication date: October 30, 2008Inventors: Tsuneo Yasuma, Nobuyuki Negoro, Shinobu Sasaki
-
Publication number: 20080255367Abstract: The present invention discloses processes for the preparation and isolation of the individual stereoisomers of 1-amino, 3-substituted phenylcyclopentane-carboxylates.Type: ApplicationFiled: December 21, 2007Publication date: October 16, 2008Inventors: Thomas D. Gordon, Grier A. Wallace, Martin E. Hayes, Kirill A. Lukin, Lei Wang, Dilinie P. Fernando
-
Publication number: 20080249107Abstract: Pharmaceutical compositions comprising at least one compound of the formulas (Ia) or (Ib) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols, indices and substituents have the following meaning R1?H, CN, NO2, CF3, F, Cl, Br, I, CH3 R2?H, CN, NO2, CF3, F, Cl, Br, I, CH3, Et, n-Pr, i-Pr, n-Bu, t-Bu, phenyl, thienyl, furyl, thiazolyl and either R1 or R2 must be H R3?H, CN, NO2, CF3, F, Cl, Br, I, CH3, Et, n-Pr, i-Pr, n-Bu, t-Bu, phenyl, thienyl, furyl, thiazolyl then X is e.g. with R4 being H, CH3, CH2CH3 or and Y being or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds of formulas (Ia) or (Ib). The compounds are applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.Type: ApplicationFiled: March 18, 2005Publication date: October 9, 2008Applicant: REVOTAR BIOPHARMACEUTICALS AGInventors: Remo Kranich, Ewald Mirko Aydt
-
Publication number: 20080221210Abstract: The invention provides compounds of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition mediated by a thyroid receptor. Formula (I), wherein R1, R2, n, Y, Y?, R3, R4, W and R5 are as defined in the specification.Type: ApplicationFiled: March 22, 2005Publication date: September 11, 2008Applicant: Karo Bio ABInventors: Ana Maria Garcia Collazo, Thomas Anders Wilson Norin, Neerai Garg, Anton Joakim Lofstedt, Tomas Fredrik Hansson, Lars Jesper Hallberg, Peter Brandt
-
Patent number: 7414040Abstract: Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.Type: GrantFiled: June 6, 2003Date of Patent: August 19, 2008Assignee: SmithKline Beecham CorporationInventor: Dirk A. Heerding
-
Publication number: 20080194445Abstract: Provided are compounds of formula wherein R1 is t-octyl, AR is phenyl, R2 is an alkyl substituted carboxyl and m is 0, 1, or 2. Lubricating oils and hydraulic fluids comprising a polyol ester lubricant in combination with one or more compounds of formula I and methods for their use are also provided.Type: ApplicationFiled: October 24, 2007Publication date: August 14, 2008Inventor: Eugene P. DiBella
-
Patent number: 7408078Abstract: The present invention provides pharmaceutical compositions useful in treating hepatitis C infection. The present invention also provides methods of treating hepatitis C infection by administering to a mammal the pharmaceutical compositions of the present invention.Type: GrantFiled: October 8, 2003Date of Patent: August 5, 2008Assignees: Wyeth, ViroPharma IncorporatedInventors: Jonathan D. Bloom, Thomas R. Bailey
-
Publication number: 20080178763Abstract: 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: ApplicationFiled: November 29, 2007Publication date: July 31, 2008Applicant: Sun Chemical CorporationInventors: Russell Schwartz, Don DeRussy, Daniel F. Gloster, Stephen Postle, Rakesh Vig, Ewell Cook, Tatiana Romanova
-
Patent number: 7381831Abstract: Disclosed is a compound of the formula and dimers thereof, wherein R, R2, X and Z are as described herein. The compounds are useful as colorants, particularly in applications such as phase change inks.Type: GrantFiled: April 4, 2007Date of Patent: June 3, 2008Assignee: Xerox CorporationInventors: Jeffrey H. Banning, Rina Carlini, James D. Mayo
-
Publication number: 20080125424Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.Type: ApplicationFiled: July 10, 2007Publication date: May 29, 2008Inventors: Pierre DePrez, Sarah E. Lively, Taoues Temal
-
Patent number: 7371867Abstract: One aspect of the invention relates to hexafluoroleucine and congeners thereof, and methods of making the compounds. Another aspect of the invention relates to the synthesis of protein cores comprising hexafluoroleucine and congeners thereof. Certain peptides comprising hexafluoroleucine and congeners thereof have been characterized using comparative biophysical studies. In general, the fluorinated peptides show higher thermal stability and enhanced resistance to chemical denaturation. Further, mixed hydrocarbon-fluorocarbon cores self-sort into homogeneous bundles, suggesting new avenues for the design and manipulation of protein-protein interfaces.Type: GrantFiled: November 6, 2006Date of Patent: May 13, 2008Assignee: Trustees of Tufts CollegeInventors: Alfio Fichera, Zihni Bilgicer, Krishna Kumar, Xuechao Xing
-
Patent number: 7351719Abstract: The present invention relates to amide compounds of general formula I wherein the groups and residues A, B, b, W, X, Y, Z, R1, R2 and R3 have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one amide according to the invention. In view of the MCH receptor-antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.Type: GrantFiled: October 31, 2003Date of Patent: April 1, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Dirk Stenkamp, Stephan Georg Mueller, Gerald Juergen Roth, Philipp Lustenberger, Klaus Rudolf, Thorsten Lehmann-Lintz, Kirsten Arndt, Ralf Lotz, Martin Lenter, Heike-Andrea Wieland
-
Patent number: 7351849Abstract: The present invention is to provide a method for producing the desired optically active ?-amino acid derivatives of high optical purities in high yields, without requiring a step of deprotection. More particularly, the present invention relates to a method for producing an optically active ?-amino acid derivative or a salt thereof represented by the formula (2): which comprises reacting an ?,?-unsaturated carboxylic acid derivative or a salt thereof represented by the formula (1): with an amines or a salt thereof in the presence of a chiral catalyst and in the presence or absence of an acid.Type: GrantFiled: August 18, 2004Date of Patent: April 1, 2008Assignee: Takasago International CorporationInventors: Mikiko Sodeoka, Yoshitaka Hamashima
-
Publication number: 20080015383Abstract: A process for the preparation of delapril and intermediates useful in its preparation.Type: ApplicationFiled: July 12, 2007Publication date: January 17, 2008Applicant: DIPHARMA FRANCIS s.r.l.Inventors: Pietro ALLEGRINI, Simone Mantegazza, Gabriele Razzetti
-
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
-
Patent number: 7244864Abstract: The invention relates to a process for the preparation of a compound of formula (I), wherein R represents a 2,3-dihydroxy-1-propyl or a 1,3-dihydroxy-2-propyl radical, via direct amidation of a dialkyl ester of 5-amino-1,3-benzenedicarboxylic acid of formula (V), wherein R1 represents a straight or branched (C1-C4)-alkyl group, with at least the stoichiometric amount of an amine of formula H2NR.Type: GrantFiled: November 28, 2001Date of Patent: July 17, 2007Assignee: Bracco Imaging S.p.A.Inventors: Pier Lucio Anelli, Marino Brocchetta, Giovanna Lux, Enrico Cappelletti
-
Patent number: 7145030Abstract: The present invention provides an effective method for the production of optically active N-aryl-?-amino acid compounds, which at the same time is suitable for industrial production. In the method of the present invention optically active sulfonylated ?-hydroxycarboxylic acid compounds, which are readily derived from ?-keto carboxylic acid compounds, are reacted with aromatic amines to produce optically active N-aryl-?-amino acid compounds.Type: GrantFiled: April 19, 2004Date of Patent: December 5, 2006Assignee: Ajinomoto Co., Inc.Inventors: Takayuki Hamada, Kunisuke Izawa
-
Patent number: 7138539Abstract: Disclosed are novel colorant compounds which contain one or more ethylenically-unsaturated (vinyl), photopolymerizable radicals which may be copolymewrized (or cured) with ethylenically-unsaturated monomers to produce colored compositions such as colored acrylic coatings and polymers, e.g., coatings and polymers produced from acrylate and methacrylate esters, colored polystyrenes, and similar colored polymeric materials derived from other ethylenically-unsaturated monomers. The present invention also pertains to processes for the preparation of certain of the photopolymerizable colorant compounds.Type: GrantFiled: October 13, 2005Date of Patent: November 21, 2006Assignee: Eastman Chemical CompanyInventors: Michael John Cyr, Max Allen Weaver, Gerry Foust Rhodes, Jason Clay Pearson, Phillip Michael Cook
-
Patent number: 7132559Abstract: One aspect of the invention relates to hexafluoroleucine and congeners thereof, and methods of making the compounds. Another aspect of the nvention relates to the synthesis of protein cores comprising hexafluoroleucine and congeners thereof. Certain peptides comprising hexafluorleucine and congeners thereof have been characterized using comparative biophysical studies. In general, the fluorinated peptides show higher thermal stability and enhanced resistance to chemical denaturation. Further, mixed hydrocarbonfluorocarbon cores self-sort into homogeneous bundles, suggesting new avenues for the design and manipulation of protein-protein interfaces.Type: GrantFiled: February 25, 2002Date of Patent: November 7, 2006Assignee: Trustees of Tufts CollegeInventors: Alfio Fichera, Zihni Bilgicer, Krishna Kumar, Xuechao Xing
-
Patent number: 7125991Abstract: The invention relates to novel compounds of formula (I) wherein R1 represents a polymer, aryl or alkyl group, R2 represents a hydrogen atom, a halogen atom, a radical CN, CF3, OH, OCF3, COOH, R7, OR7 or OCOR7, R3 represents an represents an alkyl radical. The invention also relates to a cosmetic composition comprising said compounds and to the use thereof to reduce and/or curb hair loss i.e.Type: GrantFiled: December 13, 2004Date of Patent: October 24, 2006Assignee: L'Oreal S.A.Inventors: Jean-Baptiste Galey, Maria Dalko, Lionel Breton
-
Patent number: 7115767Abstract: The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by ghrelin including anorexia, cancer cachexia, eating disorders, age-related decline in body composition, weight gain, obesity, and diabetes mellitus.Type: GrantFiled: July 16, 2004Date of Patent: October 3, 2006Assignee: Abbott LaboratoriesInventors: Bo Liu, Gang Liu, Lissa T. J. Nelson, Jyoti R. Patel, Hing L. Sham, Zhili Xin, Hongyu Zhao
-
Patent number: 7087778Abstract: Processes for producing antibacterial agents and intermediates useful in producing antibacterial agents are provided and include producing compound (VI-a) in accordance with the following reaction schema, as well as production intermediates thereofType: GrantFiled: August 23, 2004Date of Patent: August 8, 2006Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Kouji Sato, Yoshihiro Takayanagi, Katsuhiko Okano, Keiji Nakayama, Akihiro Imura, Mikihiro Itoh, Tsutomu Yagi, Yukinari Kobayashi, Tomoyuki Nagai
-
Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
-
Patent number: 6989384Abstract: Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.Type: GrantFiled: July 23, 2003Date of Patent: January 24, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Ye Hua, Hiep The Luu, Fora P. Chan, Theodore O. Johnson, Jr., Siegfried Heinz Reich, Donald James Skalitzky, Yi Yang, Thomas F. Hendrickson, Shao Song Chu, Brian Walter Eastman
-
Patent number: 6949575Abstract: The present invention provides compounds of Formula (I) and a method of treating Alzheimer's disease using a compound of Formula (I), wherein: R1 and R2 include alkyl and phenylalkyl; R3 is hydrogen or alkyl; and R4 and R5 include alkyl, alkoxy, carboxyl, alkoxycarbonyl, and nitro. Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of Formula (I) and a method of imaging amyloid deposits using compounds of Formula (I).Type: GrantFiled: April 25, 2001Date of Patent: September 27, 2005Assignee: Pfizer Inc.Inventors: Nancy Sue Barta, Christopher Franklin Bigge
-
Patent number: 6861391Abstract: Trifluoromethyl-substituted spirocyclic ketoenols of the formula (I) are provided wherein Het represents one of the groups and G, V, W, X, Y, and Z are as defined in the specification. Also provides are processes for the preparation of the compounds. The compounds of formula (I) find use as pesticides.Type: GrantFiled: September 19, 2000Date of Patent: March 1, 2005Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht
-
Patent number: 6852876Abstract: The novel compound of the disclosure is 4-chloro-4-(4-ethoxy-phenyl)-2-(fluoren-9-ylidene-hydrazono)-but-3-enoic acid methyl ester (3F-19), and it alone or in combination with 4-(4-Ethoxy-phenyl)-2-(N?-fluoren-9-ylidene-hydrazino)-2-hydroxy-4-oxo-butyric acid methyl ester (OF-13), appears useful in humans as therapeutic means for the eradication of tumors from the human's colon.Type: GrantFiled: June 7, 2002Date of Patent: February 8, 2005Assignee: University of Central FloridaInventors: D. Howard Miles, Solodnikov Sergey Yurjevich, Lisovskaja Natalja Anatoljevna, Elena A. Goun
-
Patent number: 6844003Abstract: The invention relates to novel compounds of formula (I) wherein R1 represents a polymer, aryl or alkyl group, R2 presents a hydrogen atom, a halogen atom, a radical CN, CF3, OH, OCF3, COOH, R7, OR7 or OCOR7, R3 represents an aryl or alkyl halogen, R4 represents an alkyl radical. The invention also relates to a cosmetic composition comprising said compounds and to the use thereof to reduce and/or curb hair loss i.e.Type: GrantFiled: April 4, 2003Date of Patent: January 18, 2005Assignee: L'OrealInventors: Jean-Baptiste Galey, Maria Dalko, Lionel Breton
-
Patent number: 6835848Abstract: The present invention relates to a new and industrially advantageous one-pot process for the preparation of alkyl 3-cyclopropyl amino-2-[2,4-dibromo-3-(difluoromethoxy) benzoyl]-2-propenoates of in which R represents methyl or ethyl, which are valuable intermediates for the production of highly active antibacterial quinolone medicaments.Type: GrantFiled: January 6, 2003Date of Patent: December 28, 2004Assignees: Ranbaxy Laboratories Limited, Toyama Chemical Co., Ltd.Inventors: Prosenjit Bose, Naresh Kumar, Taro Kiyoto
-
Patent number: 6806381Abstract: Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.Type: GrantFiled: October 17, 2002Date of Patent: October 19, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Ramakrishnan Chidambaram, Joydeep Kant, Raymond E. Weaver, Jurong Yu, Arun Ghosh
-
Patent number: 6787562Abstract: Compounds of the formula I; useful for the treatment of pain wherein A, Z, B, R1, X and D are as defined in the specification, methods of making such compounds, methods of using such compounds and pharmaceutical compositions containing such compounds.Type: GrantFiled: October 31, 2002Date of Patent: September 7, 2004Assignee: Zeneca Ltd.Inventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
-
Patent number: 6780874Abstract: Enamine derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in, which Ar1 is an aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(Rw) group; Rx is a oxo, thioxo, or imino group; Rw and Rz is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.Type: GrantFiled: June 10, 2003Date of Patent: August 24, 2004Assignee: Celltech R & D LimitedInventors: Timothy John Norman, John Robert Porter, Brian Woodside Hutchinson, Andrew James Ratcliffe, John Clifford Head, Rikki Peter Alexander, Barry John Langham, Graham John Warrellow, Sarah Catherine Archibald, Janeen Marsha Linsley
-
Patent number: 6765021Abstract: This invention provides compounds of formula I having the structure wherein: B, D, C, and R1 as defined herein.Type: GrantFiled: August 9, 2002Date of Patent: July 20, 2004Assignee: WyethInventors: John A. Butera, Craig E. Caufield, Russell F. Graceffa, Alexander Greenfield, Eric G. Gundersen, Lisa Marie Havran, Alan H. Katz, Joseph R. Lennox, Scott C. Mayer, Robert E. McDevitt