Oxy In Acid Moiety Patents (Class 560/42)
  • Patent number: 11878956
    Abstract: The present invention relates to metal salts of 2-[3-[(3R)-3-[[2-chloro-3-(trifluoromethyl)phenyl]methyl-(2,2-diphenylethyl)amino]butoxy]phenyl]acetic acid which exhibit improved physical properties and stability. The invention also relates to pharmaceutical compositions including an effective amount of the metal salts, as well as methods of treating cancer including administration of a pharmaceutical composition including a salt of the invention to a subject in need thereof.
    Type: Grant
    Filed: August 23, 2022
    Date of Patent: January 23, 2024
    Assignee: Inspirna, Inc.
    Inventors: Stephen Wald, Eduardo J. Martinez, Samuel Stratford, Amanda Buist, Joseph Benson, Jonathan Loughrey
  • Patent number: 11174220
    Abstract: The present invention relates to metal salts of 2-[3-[(3R)-3-[[2-chloro-3-(trifluoromethyl)phenyl]methyl-(2,2-diphenylethyl)amino]butoxy]phenyl]acetic acid which exhibit improved physical properties and stability. The invention also relates to pharmaceutical compositions including an effective amount of the metal salts, as well as methods of treating cancer including administration of a pharmaceutical composition including a salt of the invention to a subject in need thereof.
    Type: Grant
    Filed: December 11, 2020
    Date of Patent: November 16, 2021
    Assignee: Inspirna, Inc.
    Inventors: Stephen Wald, Eduardo J. Martinez, Samuel Stratford, Amanda Buist, Joseph Benson, Jonathan Loughrey
  • Patent number: 9422228
    Abstract: 3,3-diphenylpropylamines of general formula (I), particularly Fesoterodine, as well as their enantiomers, solvates and salts, can be produced by treating a compound of formula (II) with a chiral alcohol to yield the diastereomeric esters of formula (IV) and (IV?), which can be further transformed into a compound of formula (I), or an enantiomer, solvate or salt thereof, wherein R1 is C1-C8 alkyl; and R2 and R3, independently of one another, represent H or C1-C6 alkyl, or together form a ring of 3 to 7 members with the nitrogen to which they are bound.
    Type: Grant
    Filed: April 26, 2013
    Date of Patent: August 23, 2016
    Assignee: CRYSTAL PHARMA, S.A.U.
    Inventors: Antonio Lorente Bonde-Larsen, Francisco Javier Gallo Nieto, Juan José Ferreiro Gil, Pablo Martín Pascual
  • Publication number: 20150094485
    Abstract: 3,3-diphenylpropylamines of general formula (I), particularly Fesoterodine, as well as their enantiomers, solvates and salts, can be produced by treating a compound of formula (II) with a chiral alcohol to yield the diastereomeric esters of formula (IV) and (IV?), which can be further transformed into a compound of formula (I), or an enantiomer, solvate or salt thereof, wherein R1 is C1-C8 alkyl; and R2 and R3, independently of one another, represent H or C1-C6 alkyl, or together form a ring of 3 to 7 members with the nitrogen to which they are bound.
    Type: Application
    Filed: April 26, 2013
    Publication date: April 2, 2015
    Inventors: Antonio Lorente Bonde-Larsen, Francisco Javier Gallo Nieto, Juan José Ferreiro Gil, Pablo Martín Pascual
  • Patent number: 8927659
    Abstract: The invention provides biocompatible resorbable polymers, comprising monomer units having formula (I), formula (II), formula (III) or formula (IV). The polymers degrade over time when implanted in the body, and are useful as components of implantable medical devices.
    Type: Grant
    Filed: April 22, 2013
    Date of Patent: January 6, 2015
    Assignee: TYRX, Inc.
    Inventors: Arikha Moses, Satish Pulapura, Arthur Schwartz, Qing Ge, Irene Shatova
  • Publication number: 20140350227
    Abstract: The present invention relates to a novel coumarin derivative, to a method for preparing the same, and a multi-fluorescent substance that includes a plurality of the coumarin derivatives and is able to emit light using an LED light source. A novel coumarin derivative multi-fluorescent substance according to the present invention has an optimal emission wavelength band of 512 nm to 590 nm and thereby is effective in improving a signal intensity and stability since light emission using an LED light source is possible. In addition, higher fluorescence reactivity is exhibited compared to coumarin fluorescent substances known in the related arts since one molecule has a plurality of fluorescent substances, and the problem of the coumarin fluorescent substance possibly binding to a binding site of the antigen of the antibody is solved since fluorescence detection is possible even when a minimum number of fluorescent substance molecules bind to an antibody.
    Type: Application
    Filed: March 5, 2012
    Publication date: November 27, 2014
    Applicants: ACCOBIOTECH SDN BHD., GENBODY INC.
    Inventors: Hyun Park, Hak Sung Kim, Hyun Ok Song, Chom Kyu Chong, Sung Yeon Kim
  • Patent number: 8859539
    Abstract: A dual thyrointegrin antagonist and a method for treating an angiogenesis-mediated disorder and/or a hyperthyroidism disorders by introducing the dual thyrointegrin antagonist into animals (e.g., mammals, human beings). The dual thyrointegrin antagonist includes a chemical structure having a thyroid hormone antagonist and ?v?3 integrin antagonist in the same molecule.
    Type: Grant
    Filed: November 1, 2010
    Date of Patent: October 14, 2014
    Assignee: Vascular Vision Pharmaceutical Company
    Inventor: Shaker A. Mousa
  • Publication number: 20140287200
    Abstract: To provide a curable composition which has favorable insulating property and liquid repellency, and from which a cured film having liquid repellency capable of being sufficiently converted to be liquid-philic even by irradiation with ultraviolet light having a wavelength of at least 300 nm, can be formed; an article having a cured film obtained by curing the curable composition and its production process. A cured film is formed by using a curable composition comprising a polymer having units (u1) based on a compound represented by the following formula (m1): wherein R1=a hydrogen atom, a methyl group or the like; R2=a bivalent organic group or the like; Cf=a C1-20 fluoroalkyl group or the like, X?O, S, N or NH; m=1 to 2; n=0 to 4; k=0 to 1; and Z=a (meth)acryloyl group or the like.
    Type: Application
    Filed: June 5, 2014
    Publication date: September 25, 2014
    Applicant: ASAHI GLASS COMPANY, LIMITED
    Inventors: MASAHIRO ITO, KAORI TSURUOKA, YASUHIRO KUWANA, YUSUKE NAGAI, MIYAKO SASAKI
  • Publication number: 20140155439
    Abstract: Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ?CH— or ?N—; W is —CH?CH— Or —CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-natural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(C?O)—, —S(?O)2—, —C(C?O)O—, —C(C?O)NR?—, —C(?S)—NR?, —C(?NH)NR? or —S(?O)2NR— wherein R? is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)(Alk2)p— wherein in, n, p, Q, AIk1 and AIk2 are as defined in the claims; X1 represents a bond; —C(?O); or —S(?O)2—; —NR4C(?O)—, —C(C?O)NR4—, —NR4C(?O)NR5—, —NR4S(?O)2—, or —S(?O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1
    Type: Application
    Filed: February 7, 2014
    Publication date: June 5, 2014
    Applicant: Chroma Therapeutics Ltd.
    Inventors: Alastair David Graham Donald, David Festus Charles Moffat, Andrew James Belfield, Carl Leslie North, Stewart Andrew Wayne Jones
  • Publication number: 20140128614
    Abstract: To provide pesticidal allylAryl heterocycle derivatives that are useful as a pesticidal compound. Pesticidal allylAryl heterocycle derivatives that are expressed by the Formula (I), and pesticides and an agent for controlling animal parasites which include the allylAryl heterocycle derivatives as an effective component.
    Type: Application
    Filed: April 24, 2012
    Publication date: May 8, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Mamoru Hatazawa, Tetsuya Murata, Peter Bruechner, Daiei Yamazaki, Eiichi Shimojo, Teruyuki Ichihara, Katsuhiko Shibuya, Tadashi Ishikawa
  • Patent number: 8710255
    Abstract: Sitagliptin intermediate compounds of formula (f) and methods of preparation and use thereof are disclosed. Compounds of formula (f) are prepared by the following steps: compounds of formula (a) are subjected to electrophilic reaction with benzyl halides to form compounds of formula (b), which then react with compounds of formula (i) to form novel compounds of formula (e). Gignard agents formed from 2,4,5-trifluoro bromobenzene and magnesium metal react with compounds of formula (e) to afford compounds of formula (f), which are novel intermediates for the preparation of Sitagliptin intermediates of formula (g). Compounds of formula (f) are subjected to reduction by Pd/C, debenzylation, substitution of protecting group to form compounds of formula (g). Compounds of formula (a), (b), (i), (e), (f), and (g) have the following structures, in which R is protecting group of carboxyl and R2 is (substituted) hydrocarbyl.
    Type: Grant
    Filed: March 22, 2011
    Date of Patent: April 29, 2014
    Assignee: Zhejiang Jiuzhou Pharmaceutical Co., Ltd.
    Inventors: Hongjun Gao, Min Li
  • Publication number: 20140107166
    Abstract: The present invention provides novel compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of a compound of the invention to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
    Type: Application
    Filed: February 13, 2012
    Publication date: April 17, 2014
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Ralph Mazitschek, James E. Bradner, Melissa Grachan Harman
  • Publication number: 20140045936
    Abstract: The disclosure relates to cyclopropyl derivatives and methods of use. In some embodiments, the disclosure relates to methods of managing medical disorders with pharmaceutical compositions disclosed herein administered to subject in need thereof. In certain embodiments, the disclosure relates to methods of managing mental disorders, mood disorders, pain, and fibromyalgia and related conditions with pharmaceutical compositions disclosed herein.
    Type: Application
    Filed: April 13, 2012
    Publication date: February 13, 2014
    Applicants: WAKE FOREST UNIVERSITY HEALTH SCIENCES, EMORY UNIVERSITY
    Inventors: Huw M. Davies, Spandan Chennamadhavuni, Thomas J. Martin, Steven R. Childrens
  • Publication number: 20140038910
    Abstract: Disclosed herein are novel pharmaceutical agents which are useful as integrin receptor antagonists that mediate the pathologic processes of angiogenesis and fibrosis and as such are useful in pharmaceutical compositions and in methods for treating conditions mediated by these integrins by inhibiting or antagonizing these integrins. The novel pharmaceutical agents include those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods and intermediates useful for making the pharmaceutical agents and methods of using the pharmaceutical agents are also provided.
    Type: Application
    Filed: July 17, 2013
    Publication date: February 6, 2014
    Applicant: Saint Louis University
    Inventors: Peter RUMINSKI, David GRIGGS
  • Publication number: 20130345466
    Abstract: The invention provides crystalline solid forms of (S)-4-((2S,3S)-7-carbamoyl-1,1-diethyl-3-methoxy-1,2,3,4-tetrahydronaphthalen-2-ylamino)-2-cyclohexylmethyl-butyric acid. The invention also provides pharmaceutical compositions comprising such crystalline solid forms, methods of using such crystalline solid forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline solid forms.
    Type: Application
    Filed: June 17, 2013
    Publication date: December 26, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Sean M. Dalziel, Miroslav Rapta
  • Patent number: 8586631
    Abstract: Novel calcilytic compounds and methods of using them are provided.
    Type: Grant
    Filed: February 11, 2013
    Date of Patent: November 19, 2013
    Assignee: GlaxoSmithKline, LLC
    Inventors: Robert W. Marquis, Linda N. Casillas, Joshi M. Ramanjulu, James Francis Callahan
  • Publication number: 20130281652
    Abstract: The present invention relates to compounds of formula I, which are functionalized phenolic compounds, and polymers formed from the same. Ar—[O—(X)p—R?]q??I Polymers formed from the functionalized phenolics 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 17, 2012
    Publication date: October 24, 2013
    Inventor: Rao S. Bezwada
  • Patent number: 8530691
    Abstract: A process for the preparation of (R)-2-(3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)-phenol isobutyrate (Fesoterodine), its (S)-enantiomer, and novel intermediates useful in the synthesis.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: September 10, 2013
    Assignee: Dipharma Francis s.r.l.
    Inventors: Simone Mantegazza, Pietro Allegrini, Emanuele Attolino
  • Publication number: 20130210828
    Abstract: The present disclosure provides novel poly(phenylene ethynylene) (PPE) compounds, methods for synthesizing these compounds, and materials and substances incorporating these compounds. The various PPEs show antibacterial, antiviral and antifungal activity.
    Type: Application
    Filed: July 13, 2011
    Publication date: August 15, 2013
    Inventors: David G. Whitten, Kirk S. Sehanze, Anand Parthsaray, Eunkyung Ji, Motokatsu Ogawa, Thomas S. Corbitt, Dimitri Dascier, Ying Wang, Linnea K. Ista
  • Patent number: 8471054
    Abstract: The invention provides biocompatible resorbable polymers, comprising monomer units having formula (I), formula (II), formula (III) or formula (IV). The polymers degrade over time when implanted in the body, and are useful as components of implantable medical devices.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: June 25, 2013
    Assignee: Tyrx, Inc.
    Inventors: Arikha Moses, Satish Pulapura, Arthur Schwartz, Qing Ge, Irene Shatova
  • Publication number: 20130158114
    Abstract: Novel calcilytic compounds and methods of using them are provided.
    Type: Application
    Filed: February 11, 2013
    Publication date: June 20, 2013
    Applicant: GlaxoSmithKline, LLC
    Inventor: GlaxoSmithKline, LLC
  • Patent number: 8445714
    Abstract: The present invention provides novel cycloalkylmethylamine analogs, and methods of preparing cycloalkylmethylamine analogs. The present invention also provides methods of using cycloalkylmethylamine analogs and compositions of cycloalkylmethylamine analogs. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications.
    Type: Grant
    Filed: July 5, 2011
    Date of Patent: May 21, 2013
    Assignee: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan Bhat, Seema Rani Bhat
  • Publication number: 20130123356
    Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof,
    Type: Application
    Filed: October 18, 2012
    Publication date: May 16, 2013
    Applicant: UNIVERSITY COLLEGE LONDON
    Inventors: Masahiro Okuyama, David Selwood, Cristina Visintin, David Baker, Gareth Pryce
  • Publication number: 20130116437
    Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.
    Type: Application
    Filed: September 14, 2012
    Publication date: May 9, 2013
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Eric Dowdy, Xi Chen, Steven Pfeiffer
  • Publication number: 20130072520
    Abstract: Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)— or ?N—; R1 is hydrogen or an optional substituent and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2—, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z is —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C(?O)—, —O—(C?O)—, —C(?O)—O—, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic heterocyclic radical having 5 to 10 ring atoms; Alk1 and Alk2 are optionally substituted C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals, which may optionally terminate with or be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, or —N(CH2CH3)—; and Q is hydrogen, halogen, nit
    Type: Application
    Filed: November 28, 2011
    Publication date: March 21, 2013
    Applicant: Biota Scientific Management Pty Ltd
    Inventors: David BROWN, Ian COLLINS, Lloyd CZAPLEWSKI, David HAYDON
  • Publication number: 20120301552
    Abstract: A compound represented by the following formula (1), a pharmaceutically acceptable salt thereof or an optically active form thereof: wherein each symbol is as defined in the specification. A compound having a calcium-sensing receptor antagonistic action, a pharmaceutical composition comprising the compound, particularly a calcium receptor antagonist and a therapeutic drug for osteoporosis are provided.
    Type: Application
    Filed: December 23, 2011
    Publication date: November 29, 2012
    Applicant: JAPAN TOBACCO INC.
    Inventors: Yuko Shinagawa, Teruhiko Inoue, Toshihiro Kiguchi, Taku Ikenogami, Naoki Ogawa, Kenji Fukuda, Takashi Nakagawa, Masanori Shindo, Yuki Soejima
  • Publication number: 20120302637
    Abstract: A method of treating tachycardia while minimizing and/or controlling hypotension associated with such treatment includes administering a therapeutically effective amount of a pharmaceutical composition comprising the S-isomer of esmolol to a subject in need thereof.
    Type: Application
    Filed: January 26, 2012
    Publication date: November 29, 2012
    Applicants: BAXTER HEALTHCARE S.A., BAXTER INTERNATIONAL INC.
    Inventors: Barrett Rabinow, Jeff McKee
  • Publication number: 20120296074
    Abstract: The problem of the present invention is provision of a method of producing an n+p-mer oligonucleotide efficiently in a high yield, which includes use of, as a starting material, an n-mer oligonucleotide wherein the 3?-terminal hydroxyl group is protected, and the 5?-terminal hydroxyl group is protected by a temporary protecting group, and continuously performing, in a solution, (1) a deprotection step of the 5?-terminal hydroxyl group, (2) a 5?-terminal elongation step by the addition of a p-mer oligonucleotide wherein the 3?-position is phosphoramidited, and (3) an oxidation step or a sulfurization step of a phosphite triester moiety. It has been found that the above-mentioned problem can be solved by adding a particular cation scavenger during the deprotection step, applying a neutralization treatment after completion of the deprotection reaction, and using a particular oxidizing agent or sulfurizing agent in the oxidation step or sulfurization step.
    Type: Application
    Filed: May 17, 2012
    Publication date: November 22, 2012
    Applicant: AJINOMOTO CO., INC.
    Inventors: Kunihiro HIRAI, Satoshi KATAYAMA
  • Publication number: 20120277309
    Abstract: A pharmaceutical composition comprising (S)-methyl-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate in a concentration between about 75 mM and about 150 mM, which is substantially free of the R-isomer or pharmaceutically acceptable salt thereof, is provided. A method of treating a cardiac disorder is also provided and includes administering to a subject in need thereof a therapeutically effective amount of a pharmaceutical composition comprising (S)-methyl-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate hydrochloride, wherein the (S)-methyl-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate hydrochloride is present at a concentration between about 75 mM and about 150 mM and wherein the pharmaceutical composition is substantially free of (R)-methyl-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate or pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: January 26, 2012
    Publication date: November 1, 2012
    Applicants: BAXTER HEALTHCARE S.A., BAXTER INTERNATIONAL INC.
    Inventors: Jerome H. Gass, Jeff McKee, Barrett Rabinow
  • Patent number: 8207370
    Abstract: It is an objective of the present invention to produce an anti-form of an optically active ?-hydroxy-?-aminocarboxylic acid ester efficiently, simply and industrially advantageously. The objective can be accomplished by directly and selectively producing the anti-form of the optically active ?-hydroxy-?-aminocarboxylic acid ester by asymmetric reduction of a ?-keto-?-aminocarboxylic acid ester using an optically active amine complex as a catalyst. Further, the ?-keto-?-aminocarboxylic acid ester as a raw material can be produced at a high yield by reacting a glycine derivative with a carboxylic acid derivative.
    Type: Grant
    Filed: September 26, 2007
    Date of Patent: June 26, 2012
    Assignee: Kaneka Corporation
    Inventors: Tatsuya Honda, Tatsuyoshi Tanaka, Masaru Mitsuda
  • Publication number: 20120149736
    Abstract: Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ?CH— or ?N—; W is —CH?CH— Or —CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intra-cellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-nat-ural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(?O)—, —S(?O)2—, —C(?O)O—, —C(?O)NR?—, —C(?5)—NR?, —C(?NH)NR? or —S(?O)2NR — wherein R? is hydrogen or optionally substituted C1—C6 alkyl; L1 is a divalent radical of formula —(Alk1)m,(Q)n(Alk2)p— wherein m, n, p, Q, Alk1 and Alk2 are as defined in the claims; X1 represents a bond; —C(?O); or —S(?O)2—; —NR4C(?O)—, —C(?O)NR4—,— NR4C(?O)NR5—, —NR4S(?O)2—, or —S(?O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1
    Type: Application
    Filed: February 25, 2010
    Publication date: June 14, 2012
    Applicant: Chroma Therapeutics Ltd.
    Inventors: Alastair David Graham Donald, David Festus Charles Moffat, Andrew James Belfield, Carl Leslie North, Stewart Andrew Wayne Jones
  • Publication number: 20120149707
    Abstract: The present invention relates to an alpha-arylmethoxyacrylate derivative, a preparation method thereof and a pharmaceutical composition comprising the same, and the alpha-arylmethoxyacrylate derivative is inhibitory of HIF, which plays an important role in the regulation of genes associated with energy metabolism, vasomotion, angiogenesis and apoptosis and in the response of cells under hypoxic conditions, so that it can be used for preventing or treating of diseases such as cancer, arthritis, psoriasis, diabetic retinopathy and macular degeneration.
    Type: Application
    Filed: April 21, 2011
    Publication date: June 14, 2012
    Applicant: OSCOTEC INC.
    Inventors: Se-Won Kim, Jung Ho Kim, Se-Nyum Kim, Dae-Pil Kang, Youn Ho Han, Guo Fan Jin, Dong-Sik Jung, Sung-Ho Park, Ji Min Kim, Jhi Zheng
  • Publication number: 20120129894
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
    Type: Application
    Filed: May 19, 2011
    Publication date: May 24, 2012
    Applicant: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Feng Hong
  • Publication number: 20120122918
    Abstract: Compounds of formula (1) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)-Q.
    Type: Application
    Filed: November 28, 2011
    Publication date: May 17, 2012
    Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTD
    Inventors: David Ryall BROWN, Ian COLLINS, Lloyd George CZAPLEWSKI, David John HAYDON
  • Publication number: 20120088782
    Abstract: A compound of the general formula (I): (wherein the symbols are as defined in the description), or a non-toxic salt thereof.
    Type: Application
    Filed: December 19, 2011
    Publication date: April 12, 2012
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Masahiko Terakado, Shinji Nakade, Takuya Seko, Yoshikazu Takaoka
  • Patent number: 8153837
    Abstract: The invention provides biocompatible resorbable polymers, comprising monomer units having formula (I), formula (II), formula (III) or formula (IV). The polymers degrade over time when implanted in the body, and are useful as components of implantable medical devices.
    Type: Grant
    Filed: November 3, 2006
    Date of Patent: April 10, 2012
    Assignee: TYRX, Inc.
    Inventors: Arikha Moses, Satish Pulapura, Arthur Schwartz, Qing Ge, Irene Shatova
  • Patent number: 8093420
    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: Grant
    Filed: October 10, 2006
    Date of Patent: January 10, 2012
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S. Bezwada
  • Publication number: 20110319359
    Abstract: Compounds exhibiting calcium receptor antagonist activity that are safe and orally administrable having Formula (I) or pharmaceutically acceptable salts thereof:
    Type: Application
    Filed: June 23, 2011
    Publication date: December 29, 2011
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Akira Nakao, Kentoku Gotanda, Kazumasa Aoki, Shimpei Hirano, Yoshiharu Hiruma, Takeshi Shiiki
  • 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: 20110301179
    Abstract: A compound (particularly useful for inhibiting cancer) according to formula I: or a pharmaceutically acceptable salt thereof, wherein: x is 0 or 1; R1-R6 are each independently H, —CN, —NO2, —NO, —OH, halogen, hydroxyalkyl, carboxyl, substituted carboxyl, aminocarbonyl, alkoxy, carbonyl or substituted carbonyl; R7 is H, alkyl, alkyl amino, aminoacyl, hydroxyacyl, heteroaryl, heterocycloalkyl, alkyl heteroaryl or alkyl heterocycloalkyl; R8 is H or alkyl; A is O or N; and Ar is an aryl, substituted aryl, heteroaryl, or substituted heteroaryl, provided that if R7 is H then Ar is aryl substituted with alkyl amino.
    Type: Application
    Filed: October 21, 2009
    Publication date: December 8, 2011
    Inventors: Xiangshu Xiao, Bingbing Li
  • Publication number: 20110263888
    Abstract: The present invention provides novel cycloalkylmethylamine analogs, and methods of preparing cycloalkylmethylamine analogs. The present invention also provides methods of using cycloalkylmethylamine analogs and compositions of cycloalkylmethylamine analogs. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications.
    Type: Application
    Filed: July 5, 2011
    Publication date: October 27, 2011
    Applicant: REVIVA PHARMACEUTICALS, INC.
    Inventors: Laxminarayan Bhat, Seema Rani Bhat
  • Publication number: 20110245494
    Abstract: The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (I): wherein X is alkyl, substituted alkyl, alkenyl, substituted alkenyl, heteroalkyl, substituted heteroalkyl, heteroalkenyl, or substituted heteroalkenyl.
    Type: Application
    Filed: July 29, 2009
    Publication date: October 6, 2011
    Applicant: SENOMYX, INC.
    Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Qing Chen, Peter Leeming, Tayyab Rashid, Daniel Levin
  • Patent number: 8017613
    Abstract: The present invention relates to new compounds, ligands of the beta-3 adrenergic receptor, their preparation and their use in therapy or as research tools for said receptor; the invention also relates to a process for the preparation of the compounds of the invention and the use of inverse agonists of the beta-3 adrenergic receptor as medicaments.
    Type: Grant
    Filed: August 3, 2007
    Date of Patent: September 13, 2011
    Assignee: Universita' Degli Studi Di Bari
    Inventors: Antonio Scilimati, Maria Grazia Perrone, Ernesto Santandrea
  • Patent number: 8003689
    Abstract: This invention provides metabolites of SARM compounds including inter alia glucuronidated metabolites and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, muscle wasting disease and/or disorder, a bone related disease and/or disorder, metabolic syndrome, diabetes and associated diseases, and others.
    Type: Grant
    Filed: June 19, 2009
    Date of Patent: August 23, 2011
    Assignee: GTx, Inc.
    Inventor: Karen A. Veverka
  • Patent number: 8003695
    Abstract: Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: Formula (A) and (B) wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is (a) a radical of formula R1R2CHNH—Y-L1-X1—(CH2)z— wherein: z is 0 or 1; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(?O)—, —S(?P)2-, —C(?O)O—, —C(?O)NR3-, —C(?S)—NR3, —C(?NH)—NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L is a divalent linker radical of formula -(Alk1)m(Q)(Alk2)p- wherein m, n, p, Q, AIk1 and AIk2 are as defined in the claims.
    Type: Grant
    Filed: October 29, 2007
    Date of Patent: August 23, 2011
    Assignee: Chroma Therapeutics Ltd.
    Inventors: David Festus Charles Moffat, Stephen John Davies, Michael Hugh Charlton, Simon Christopher Hirst, Stuart Thomas Onions, Jonathan Gareth Williams
  • Patent number: 8003694
    Abstract: The present invention provides ethyl (?)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate hydrochloride ¼ hydrate or a crystal thereof which can be determined by characteristic diffraction peaks of the powder X-ray diffraction, thermogravimetry-differential thermal analysis or the like, and obtained by manufacturing ethyl (?)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methyl-ethyl]amino]ethyl]-2,5-dimethylphenoxyacetate by a specific method.
    Type: Grant
    Filed: April 24, 2006
    Date of Patent: August 23, 2011
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Hidetoshi Isawa, Michio Toda
  • Patent number: 7947735
    Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. Formula (I), wherein n is 1 or 2; m is 0, 1, 2, 3, or 4; q is 0 or 1; t is 0 or 1; R1 is hydrogen, halo, hydroxy, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; R2 is alkyl having from 1 to 3 carbon atoms; R3 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; one of R4 and R5 is hydrogen or hydroxy and the other is hydrogen; or R4 and R5 together are ?O; R6 is hydrogen or alkyl having one, two, three, four or five carbon atoms; or a pharmaceutically acceptable salt of the compound. Alternatively, the agent can be a pharmaceutically acceptable salt of the compound of Formula (I).
    Type: Grant
    Filed: January 22, 2007
    Date of Patent: May 24, 2011
    Assignee: Wellstat Therapeutics Corporation
    Inventors: Shalini Sharma, Reid W. von Borstel
  • Publication number: 20110105783
    Abstract: A process for the preparation of (R)-2-(3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)-phenol isobutyrate (Fesoterodine), its (S)-enantiomer, and novel intermediates useful in thei synthesis.
    Type: Application
    Filed: October 28, 2010
    Publication date: May 5, 2011
    Applicant: DIPHARMA FRANCIS S.r.I.
    Inventors: Simone Mantegazza, Pietro Allegrini, Emanuele Attolino
  • Publication number: 20110105482
    Abstract: A dual thyrointegrin antagonist and a method for treating an angiogenesis-mediated disorder and/or a hyperthyroidism disorders by introducing the dual thyrointegrin antagonist into animals (e.g., mammals, human beings). The dual thyrointegrin antagonist includes a chemical structure having a thyroid hormone antagonist and ?v?3 integrin antagonist in the same molecule.
    Type: Application
    Filed: November 1, 2010
    Publication date: May 5, 2011
    Applicant: VASCULAR VISION PHARMACEUTICAL COMPANY
    Inventor: Shaker A. Mousa
  • Patent number: RE43984
    Abstract: A process for making optically Optically pure (R) and (S) salbutamol comprises obtaining the (R) or (S) isomer of either salbutamol or a salbutamol precursor in substantially optically pure form is obtained by resolving a racemic or optically impure mixture of enantiomers of salbutamol or of said a salbutamol precursor with either (L) or (D) tartaric acid, and where necessary converting said isomer of said precursor into either (R) or (S) salbutamol respectively; then optionally converting said optically pure (R) and/or (S) salbutamol into a pharmaceutically acceptable salt.
    Type: Grant
    Filed: December 10, 2001
    Date of Patent: February 5, 2013
    Assignee: Cipla Limited
    Inventors: Yusuf Khwaja Hamied, Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao