Three-membered Ring In R Patents (Class 514/624)
  • Publication number: 20140357722
    Abstract: Provided herein are compounds and pharmaceutical compositions for use in the treatment of neuropathic pain and the neuropathic pain syndromes.
    Type: Application
    Filed: July 10, 2014
    Publication date: December 4, 2014
    Inventors: Birgit Hasse, Guido Koopmans
  • Publication number: 20140343108
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel amidated derivatives of oleanolic acid according to formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 20, 2014
    Inventors: Frank Rong, Rongzhen Xu, Fuwen Xie, Hongxi Lai
  • Patent number: 8835472
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 17, 2011
    Date of Patent: September 16, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerald Juergen Roth, Martin Fleck, Niklas Heine, Joerg Kley, Thorsten Lehmann-Lintz, Heike Neubauer, Bernd Nosse
  • Publication number: 20140171315
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140121187
    Abstract: Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.
    Type: Application
    Filed: June 18, 2012
    Publication date: May 1, 2014
    Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN K.U. LEUVEN R & D, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Young Sik Jung, Chong Kgo Lee, Ihl Young Choi, Hae Soo Kim, Pil Ho Kim, Soo Bong Han, Johan Neyts, Hendrik Jan Thibaut
  • Publication number: 20140121217
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein A, Y, L, R1, W1 and W2 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: January 2, 2014
    Publication date: May 1, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Lijun Sun, Jun Jiang, Yu Xie
  • Patent number: 8518979
    Abstract: Novel Alpha-halo- and Alpha-alkyl-cyclopropylcarboxy compounds, and uses of these and related compounds in the treatment of a variety of neurological diseases and disorders, and particularly epilepsy, are provided.
    Type: Grant
    Filed: February 19, 2008
    Date of Patent: August 27, 2013
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.
    Inventors: Meir Bialer, Boris Yagen, Neta Pessah
  • Publication number: 20130217737
    Abstract: Provided herein are compounds and pharmaceutical compositions for use in the treatment of neuropathic pain and the neuropathic pain syndromes.
    Type: Application
    Filed: October 28, 2011
    Publication date: August 22, 2013
    Applicant: AL-GIAX PHARMACEUTICALS GMBH
    Inventors: Birgit Hasse, Guido Koopmans
  • Publication number: 20130184279
    Abstract: Compounds of formula Ia and Ib wherein A, B, C, R1 and R14 are described herein.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 18, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Patent number: 8314270
    Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.
    Type: Grant
    Filed: September 9, 2010
    Date of Patent: November 20, 2012
    Assignee: Abbott Laboratories
    Inventors: James T. Link, Qi Shuai, Martin Winn, Hong Yong
  • Publication number: 20120252733
    Abstract: Provided herein are compositions and related methods useful for accelerating bone healing and growth. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity.
    Type: Application
    Filed: June 4, 2010
    Publication date: October 4, 2012
    Applicant: UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
    Inventors: Michael W. Epperly, Abhay Sudhir Gokhale, Joel S. Greenberger, Peter Wipf, Julianne Glowacki
  • Publication number: 20120214858
    Abstract: Imidamide (amidine) analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumors.
    Type: Application
    Filed: August 16, 2010
    Publication date: August 23, 2012
    Applicant: University of Virginia Patent Foundation
    Inventors: Kevin R. Lynch, Timothy L. Macdonald, Thomas P. Mathews, Andrew Kennedy, Yugesh Kharel
  • Patent number: 7947852
    Abstract: Compounds of formula (I): wherein: R1 represents alkyl, alkenyl, haloalkyl, polyhaloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, X represents a group N—OR2 wherein R2 represents a hydrogen atom or an alkyl group. Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.
    Type: Grant
    Filed: July 1, 2008
    Date of Patent: May 24, 2011
    Assignee: Les Laboratoires Servier
    Inventors: Said Yous, Mohamed Ettaoussi, Ahmed Sabaouni, Pascal Berthelot, Michael Spedding, Philippe Delagrange, Daniel-Henri Caignard, Mark Millan
  • Publication number: 20100160443
    Abstract: The invention relates to the use of compounds for the preparation of a medicament for treating neuropathic pain, migraine, psychiatric disorder and/or neuronal degeneration. The invention additionally relates to a pharmaceutical composition comprising compounds for treating neuropathic pain, migraine, psychiatric disorder and/or neuronal degeneration. A method for treating neuropathic pain, migraine, psychiatric disorder and/or neuronal degeneration is also provided.
    Type: Application
    Filed: March 2, 2010
    Publication date: June 24, 2010
    Applicant: Yissum Research Development Company of The Hebrew University of Jerusalem
    Inventors: Meir Bialer, Boris Yagen, Ilan Winkler, Marshall Devor
  • Publication number: 20100152254
    Abstract: Novel Alpha-halo- and Alpha-alkyl-cyclopropylcarboxy compounds, and uses of these and related compounds in the treatment of a variety of neurological diseases and disorders, and particularly epilepsy, are provided.
    Type: Application
    Filed: February 19, 2008
    Publication date: June 17, 2010
    Applicant: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.
    Inventors: Meir Bialer, Boris Yagen, Neta Pessah
  • Patent number: 7632972
    Abstract: Compounds and related methods for synthesis, and the use of compounds and combination therapies for the treatment of cancer and modulation of apoptosis in cells are disclosed. The generation of synthetic combinatorial libraries and the evaluation of library member compounds regarding induction of apoptosis selectively in cancer cells are disclosed. Compounds, methods of making the compounds, and therapeutic methods with application against breast cancer cells, melanoma cancer cells, colon cancer cells, and other cancer cells are described.
    Type: Grant
    Filed: October 27, 2004
    Date of Patent: December 15, 2009
    Assignee: The Board of Trustees of the University of Illionis
    Inventors: Paul J. Hergenrother, Vitaliy Nesterenko, Karson Putt, Brittany Joy Allen, Robin Shane Dothager, Benjamin James Leslie
  • Publication number: 20090182048
    Abstract: The invention relates to the use of compounds for the preparation of a medicament for treating neuropathic pain, migraine, psychiatric disorder and/or neuronal degeneration. The invention additionally relates to a pharmaceutical composition comprising compounds for treating neuropathic pain, migraine, psychiatric disorder and/or neuronal degeneration. A method for treating neuropathic pain, migraine, psychiatric disorder and/or neuronal degeneration is also provided.
    Type: Application
    Filed: March 20, 2009
    Publication date: July 16, 2009
    Applicant: Yissum Research Development Company of The Hebrew University of Jerusalem
    Inventors: Meir BIALER, Boris YAGEN, IIan WINKLER, Marshall DEVOR
  • Patent number: 7524885
    Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells: wherein W, Cyc, p, Y, X, Z, R, R1, R2, R3, R4, I, m and n are as defined for Formula (I) herein. The invention also relates to pharmaceutical compositions comprising compounds capable of stimulation of glucose oxidation, methods for increasing glucose oxidation rates in myocardial cells, and methods of treatment of myocardial ischemia.
    Type: Grant
    Filed: February 23, 2005
    Date of Patent: April 28, 2009
    Assignee: The Governors of the University of Alberta
    Inventors: Gary D. Lopaschuk, John C Vederas, Jason R. Dyck
  • Patent number: 7511175
    Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.
    Type: Grant
    Filed: January 5, 2006
    Date of Patent: March 31, 2009
    Assignee: Abbott Laboratories
    Inventors: Jyoti R. Patel, Qi Shuai, James T. Link, Jeffrey J. Rohde, Jurgen Dinges, Bryan K. Sorensen, Martin Winn, Hong Yong, Peer B. Jacobson, Michael E. Brune
  • Publication number: 20090048233
    Abstract: Provided are combinations of pharmaceutical agents capable of eliciting a therapeutic effect. A first therapeutic agent in the combination has 5HT2/5HT3 antagonist and alpha-2 antagonist activity. A second therapeutic agent possesses both serotonin reuptake inhibitory activity and norepinephrine reuptake inhibitory activity or is a reversible inhibitor of monoamine oxidase A (RIMA). In some embodiments, a combination of a first therapeutic agent and a second therapeutic agent results in reduction in one or deleterious side effects associated with the first therapeutic agent, the second therapeutic agent or both. Also provided are methods of treatment employing a first therapeutic agent and a second therapeutic agent. Also provided are kits containing a first therapeutic agent, a second therapeutic agent and instructions for administering the first therapeutic agent and the second therapeutic agent.
    Type: Application
    Filed: August 15, 2008
    Publication date: February 19, 2009
    Applicant: CYPRESS BIOSCIENCES, INC.
    Inventors: Srinivas RAO, Jay Kranzler, Jeffery J. Anderson
  • Patent number: 7473706
    Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells: wherein W, Cyc, p, Y, X, Z, R, R1, R2, R3, R4, i and n are as defined for Formula (I) herein. The invention also relates to pharmaceutical compositions comprising compounds capable of stimulation of glucose oxidation, methods for increasing glucose oxidation rates in myocardial cells, and methods of treatment of myocardial ischemia.
    Type: Grant
    Filed: March 6, 2006
    Date of Patent: January 6, 2009
    Assignee: The Governors of the University of Alberta
    Inventors: Gary D. Lopaschuk, John C. Vederas, Jason R. Dyck
  • Patent number: 7459585
    Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: March 24, 2005
    Date of Patent: December 2, 2008
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
  • Patent number: 7432302
    Abstract: Proliferative cutaneous disease states or conditions are treated by administering a polyamine transport inhibitor R-X-L-polyamine wherein R is a straight or branched C10-50 saturated or unsaturated aliphatic, carboxyalkyl, carbalkoxyalkyl, or alkoxy; a C1-8 alicyclic; a single or multiring aryl substituted or unsubstituted aliphatic; and aliphatic-substituted or unsubstituted single or multiring aromatic; a single or multiring heterocyclic; a single or multiring heterocyclic aliphatic; an aryl sulfonyl; X is —CO—, —SO2—, or —CH2—; and L is a covalent bond or a naturally occurring amino acid, lysine, ornithine, 2,4-diaminobutyric acid, or pharmaceutically acceptable salts thereof or prodrug thereof, and a polyamine biosynthesis inhibitor.
    Type: Grant
    Filed: February 23, 2005
    Date of Patent: October 7, 2008
    Assignee: MediQuest Therapeutics, Inc.
    Inventors: Mark R. Burns, Gerard F. Graminski, Nand Baindur, Reitha S. Weeks
  • Patent number: 7414152
    Abstract: Cooling compounds are provided having the formula: wherein, m is 0 or 1, Y and Z are selected independently from the group consisting of H, OH, C1-C4 straight or branched alkyl, and a C1-C4 straight or branched alkoxy, X is (CH2)n—R, where n is 0 or 1 and R is a group with non-bonding electrons, with the provisos that: (a) when Y and Z are H, X is not F, OH, MeO or NO2 in the 4-position and is not OH in the 2 or 6-position (b) when Y or Z is H then X, Y and Z are such that (i) the groups in the 3- and 4-positions are not both OMe, (ii) the groups in the 4- and 5-positions are not both OMe, (iii) the groups in 3- and 5-positions are not OMe if the group in the 4-position is OH, and (iv) the groups in the 3- and 5-positions are not OH if the group in the 4-position is methyl.
    Type: Grant
    Filed: May 19, 2006
    Date of Patent: August 19, 2008
    Assignee: Givaudan, SA
    Inventors: Christophe C. Galopin, Pablo Victor Krawec, Jay Patrick Slack, Lori W. Tigani
  • Patent number: 7074833
    Abstract: A method for treating or preventing a disorder or a condition by double inhibition of serotonin (5-HT) and noradrenaline (NA) reuptake in a subject in need thereof, while limiting the risks of cardiovascular disturbances and/or organ and/or tissue toxicity, comprising the step of administering to said subject a mixture of enantiomers of milnacipran enriched in the (1S,2R) enantiomer of milnacipran and/or of at least one of its metabolites, as well as their pharmaceutically-acceptable salts.
    Type: Grant
    Filed: March 22, 2004
    Date of Patent: July 11, 2006
    Assignee: Pierre Fabre Medicament
    Inventors: Jean Deregnaucourt, Richard Grosse
  • Patent number: 7053071
    Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis or apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: May 30, 2006
    Assignee: The Burnham Institute
    Inventors: Marcia Dawson, Joseph A. Fontana, Xiao-kun Zhang, Mark Leid, Ling Jong, Peter D. Hobbs
  • Patent number: 7038085
    Abstract: The present invention relates generally to the enantiomers of para-hydroxy-milnacipran or congeners thereof. Biological assays revealed that racemic para-hydroxy-milnacipran is approximately equipotent in inhibiting serotonin and norepinephrine uptake (IC50=28.6 nM for norepinephrine, IC50=21.7 nM for serotonin). Interestingly, (+)-para-hydroxy-milnacipran is a more potent inhibitor of norepinephrine uptake than serotonin uptake (IC50=10.3 nM for norepinephrine, IC50=22 nM for serotonin). In contrast, (?)-para-hydroxy-milnacipran is a more potent inhibitor of serotonin uptake compared to norepinephrin uptake (IC50=88.5 nM for norepinephrine, IC50=40.3 nM for serotonin). The invention also relates to salts and prodrug forms of the aforementioned compounds. In certain embodiments, the compounds of the present invention and a pharmaceutically acceptable excipient are combined to prepare a formulation for administration to a patient.
    Type: Grant
    Filed: October 22, 2003
    Date of Patent: May 2, 2006
    Assignee: Collegium Pharmaceutical, Inc.
    Inventors: Roman V. Rariy, Michael Heffernan, Stephen L. Buchwald, Timothy M. Swager
  • Patent number: 7034057
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-? or combinations thereof.
    Type: Grant
    Filed: November 19, 2003
    Date of Patent: April 25, 2006
    Assignee: Schering Corporation
    Inventors: Zhaoning Zhu, Robert Mazzola, Zhuyan Guo, Brian J. Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih
  • Patent number: 7005452
    Abstract: The present invention concerns the use of a mixture of enantiomers enriched in the dextrogyral enantiomer of milnacipran and/or of at least one of its metabolites, as well as their pharmaceutically-acceptable salts, for the preparation of a drug intended to prevent or to treat disorders that can be managed by double inhibition of serotonin (5-HT) and norepinephrine (NE) reuptake, while limiting the risks of cardiovascular disturbances and/or organ and/or tissue toxicity.
    Type: Grant
    Filed: June 3, 2003
    Date of Patent: February 28, 2006
    Assignee: Pierre Fabre Medicament
    Inventors: Jean Deregnaucourt, Richard Grosse
  • Patent number: 6995285
    Abstract: The present invention provides compounds that elevate cellular expression of the ABCA-1 gene, promoting cholesterol efflux from cells and increasing HDL levels in the plasma of a mammal, in particular humans. The compounds are useful for treating coronary artery disease.
    Type: Grant
    Filed: June 4, 2002
    Date of Patent: February 7, 2006
    Assignee: CV Therapeutics, Inc.
    Inventors: Prabha N. Ibrahim, Robert Jiang, Christopher Morrison, Kevin Shenk, Jeff A. Zablocki
  • Patent number: 6960687
    Abstract: New derivatives of N-Hydroxyalkyl-tetramethylcyclopropane carboxamide, pharmaceutical compositions thereof, methods for their preparation, and use thereof for the treatment of epilepsy, neurological, affective and psychotic disorders and for the treatment of pain and migraine.
    Type: Grant
    Filed: December 29, 2002
    Date of Patent: November 1, 2005
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventors: Meir Bialer, Nina Isoherranen, Boris Yagen
  • Patent number: 6872751
    Abstract: The present invention relates to methods for prevention and/or treatment of diseases or conditions caused by deficiency in the adult isoform of a given protein wherein said method comprises administering to a patient in need thereof a composition containing NO or at least one compound able to release, induce and/or promote NO formation in cells, said administration resulting in augmenting or restoring the production of the fetal isoform of said protein in said patient.
    Type: Grant
    Filed: April 29, 2002
    Date of Patent: March 29, 2005
    Assignee: Centre National de la Recherche Scientifique - CNRS
    Inventors: Maurice Israël, Sabine De La Porte, Philippe Fossier, Emmanuel Chaubourt, Gérard Baux, Christiane Leprince
  • Publication number: 20040225015
    Abstract: A carba-sugar amine derivative represented by the following formula (1) or (2) is used as the active ingredient of a &bgr;-galactosidase inhibitor or a glycolipid metabolic disorder treating agent.
    Type: Application
    Filed: March 8, 2004
    Publication date: November 11, 2004
    Applicant: Seikagaku Corporation
    Inventors: Seiichiro Ogawa, Yoshiyuki Suzuki, Eiji Nanba, Junichiro Matsuda, Kousaku Ohno
  • Publication number: 20040102418
    Abstract: This invention relates to compounds of the Formula (I): 1
    Type: Application
    Filed: November 19, 2003
    Publication date: May 27, 2004
    Inventors: Zhoaning Zhu, Robert Mazzola, Zhuyan Guo, Brian J. Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih
  • Patent number: 6730635
    Abstract: The invention relates to microcapsule suspensions containing (A) a particulate disperse phase of microcapsules comprising: (1) sleeves that are reaction products of mixtures of toluylene diisocyanate and 4,4′-methylenebis-(cyclohexyl isocyanate) with at least one diamine and/or polyamine, and (2) a capsule filling comprising: (i) at least one solid insecticidally and/or herbicidally active compound, (ii) at least one liquid aliphatic hydrocarbon having a boiling point above 160° C., (iii) at least one oil-soluble polymeric dispersing agent, and (iv) optional agrochemically active compounds that are liquid at room temperature, and (B) a liquid aqueous phase comprising water, optional additives, and optional agrochemically active compounds in non-encapsulated form that are solid at room temperature.
    Type: Grant
    Filed: September 12, 2002
    Date of Patent: May 4, 2004
    Assignee: Bayer AG
    Inventors: Hilmar Wolf, Norbert Schick, Björn Christensen, Anne Suty-Heinze
  • Publication number: 20040077616
    Abstract: The present invention relates to the use of compounds of formula (I) 1
    Type: Application
    Filed: October 22, 2002
    Publication date: April 22, 2004
    Inventors: Youssef L. Bennani, William H. Bunnelle, Sou-Jen Chang, Sanjay R. Chemburkar, Jinhua Chen, Michael J. Dart, Dilinie P. Fernando, Yi-Yin Ku, Mark Lockwood, Lei Wang
  • Publication number: 20040077617
    Abstract: The present invention relates to the use of compounds of formula (I) 1
    Type: Application
    Filed: October 22, 2002
    Publication date: April 22, 2004
    Inventors: Youssef L. Bennani, Sou-Jen Chang, Sanjay R. Chemburkar, Michael J. Dart, Dilinie P. Fernando, Timothy A. Grieme
  • Patent number: 6703379
    Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: March 12, 2001
    Date of Patent: March 9, 2004
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
  • Patent number: 6683114
    Abstract: Norepinephrine reuptake inhibitors are used to treat psoriasis.
    Type: Grant
    Filed: August 7, 2002
    Date of Patent: January 27, 2004
    Assignee: Eli Lilly and Company
    Inventor: Holly Read Thomasson
  • Publication number: 20040002521
    Abstract: The present invention provides an NF-kappa B activation inhibitor, an inflammatory cytokine production inhibitor, a matrix metalloprotease production inhibitor, an inflammatory cell adhesion factor expression inhibitor, and an anti-inflammatory agent, an antirheumatic agent, an immuno-suppressive agent, an antiallergic agent, an antiviral agent, or a therapeutic agent for arteriosclerosis, which comprise, as the active ingredient, a cyclopropanecarboxylic acid amide compound or a pharmaceutically acceptable salt thereof effective for the treatment of inflammatory diseases.
    Type: Application
    Filed: April 30, 2003
    Publication date: January 1, 2004
    Applicant: AJINOMOTO CO. INC
    Inventors: Yukio Iino, Takashi Yamamoto, Tsuyoshi Kobayashi
  • Patent number: 6670400
    Abstract: Phenoxyethylamine derivatives of general formula (I) having high affinity for the 5-HT1A receptor, methods for preparing same, pharmaceutical compositions containing said derivatives, and their use, in particular as gastric acid secretion inhibitors or as antiemetics, are disclosed. In general formula (I), Ar is phenyl substituted by one or more substituents; and R is a C1-10 hydrocarbon radical selected from straight or branched alkyl, alkenyl or alkynyl radicals, saturated or unsaturated mono- or polycyclic cycloalkyl, cycloalkylalkyl or alkylcycloalkyl radicals; a pyridyl or isoquinolyl radical, phenyl optionally substituted by one or more substituents, and salts thereof.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: December 30, 2003
    Assignee: Societe de Conseils de Recherches et D'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Dennis Bigg, Jacques Pommier, Christiane Martin, Pierre Roubert, Jean Pierre Defaux
  • Patent number: 6602911
    Abstract: The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject. The method generally involves administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and an equal or greater inhibition of norepinephrine reuptake than serotonin reuptake. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.
    Type: Grant
    Filed: December 19, 2001
    Date of Patent: August 5, 2003
    Assignee: Cypress Bioscience, Inc.
    Inventors: Jay D. Kranzler, Srinivas G. Rao
  • Patent number: 6504058
    Abstract: Compounds of Formula I are disclosed which are useful as fungicides wherein R1 is hydrogen; halogen; C1-C2 alkoxy; C1-C2 haloalkoxy; cyano; or C1-C2 alkyl optionally substituted with halogen, C1-C2 alkoxy or cyano; R2 is hydrogen; halogen; or C1-C4 alkyl optionally substituted with halogen, C1-C2 alkoxy or cyano; R3 is hydrogen; halogen; C1-C4 alkoxy; C1-C4 haloalkoxy; or C1-C4 alkyl optionally substituted with halogen, C1-C2 alkoxy or cyano; or R2 and R3 can be taken together as —CH2CH2—; R4 is C1-C2 alkyl; R5 is R6, CH(R8)OR6, CH(R8)CH(R7)R6 or C(R8)═C(R7)R6; and R6, R7 and R8 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula I.
    Type: Grant
    Filed: February 6, 2002
    Date of Patent: January 7, 2003
    Assignee: The Board of Trustees of the University of Arkansas
    Inventors: Gregory S. Basarab, Lee Dalton Jennings, Dennis R. Rayner
  • Publication number: 20020161053
    Abstract: The present invention discloses biscyclopropanecarboxamide compounds and pharmaceutically acceptable salts thereof; and also NF-kappa B activation inhibitors, Inflammatory cytokine production inhibitors, matrix metalloprotease production inhibitors, inflammatory cell adhesion molecules incidence inhibitors, antiinflammatory agents, antirheumatic agents, immunosuppressive agents, cancerous metastasis inhibitors or antiviral agents each containing such a compound as the active ingredient.
    Type: Application
    Filed: March 1, 2002
    Publication date: October 31, 2002
    Applicant: AJINOMOTO CO. INC.
    Inventors: Yukio Iino, Kohichi Fujita, Takashi Yamamoto, Kenji Takehana, Tsuyoshi Kobayashi
  • Patent number: 6441044
    Abstract: The present invention relates to cycloalkylcarboxamides of formula I where: A is optionally substituted C3-C6-cycloalkyl; Alk is straight-chain or branched C1-C6-alkylene; R1 is optionally substituted C1-C6-alkyl or C2-C6-alkenyl; R2, R3 is hydrogen, or is optionally halogenated C1-C6-alkyl or C2-C6-alkenyl; W is an optionally substituted fused bicyclic ring system having in each case six ring atoms, where one or two carbon ring atoms may be replaced by nitrogen atoms; and their agriculturally useful salts. Furthermore, the invention relates to fungicidal compositions comprising a compound of formula I as crop protection agent.
    Type: Grant
    Filed: February 26, 2001
    Date of Patent: August 27, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Ingo Rose, Frank Wetterich, Karl Eicken, Joachim Rheinheimer, Gisela Lorenz, Eberhard Ammermann, Thomas Grote, Siegfried Strathmann
  • Publication number: 20020035095
    Abstract: Hydroxyeicosatetraenoic acid analogs and methods of their use in treating dry eye disorders are disclosed.
    Type: Application
    Filed: September 10, 2001
    Publication date: March 21, 2002
    Inventors: Peter G. Klimko, Mark R. Hellberg, John R. Falck, Raymond E. Conrow
  • Patent number: 6313163
    Abstract: Compounds of formula 1 wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, Y is cyclopropyl optionally substituted with one or two R4 groups, the divalent Y radical being substituted by the Z and —CR1═CR1—CR1═CR1 groups on adjacent carbons; X is S, O, or NR5; n is 1 or 2; R1 and R2 independently are H, lower alkyl or fluoroalkyl; R3 is hydrogen, lower alkyl, Cl or Br; R4 is lower alkyl, fluoroalkyl or halogen; R5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR8, CONR9R10, —CH2OH, CH2OR11, CH2OCOR11, CHO, CH(OR12)2, CHOR13O, 13 COR7, CR7(OR12)2, CR7OR13O, or tri-lower alkylsilyl, where R7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R8 is an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or R8 is phenyl or lower alkylphenyl, R9 and R10 indep
    Type: Grant
    Filed: August 17, 2000
    Date of Patent: November 6, 2001
    Assignee: Allergen Sales, Inc.
    Inventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Patent number: RE42700
    Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis of apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: September 13, 2011
    Assignees: Sanford-Burnham Medical Research Institute, Oregon State University, SRI International, Molecular Medicine Research Institute, Department of Veterans Affairs, Wayne State University
    Inventors: Marcia Dawson, Joseph A. Fontana, Xiao-Kun Zhang, Mark Leid, Ling Jong, Peter D. Hobbs
  • Patent number: RE43879
    Abstract: The present invention concerns the use of a mixture of enantiomers enriched in the dextrogyral enantiomer of milnacipran and/or of at least one of its metabolites, as well as their pharmaceutically-acceptable salts, for the preparation of a drug intended to prevent or to treat disorders that can be managed by double inhibition of serotonin (5-HT) and norepinephrine (NE) reuptake, while limiting the risks of cardiovascular disturbances and/or organ and/or tissue toxicity.
    Type: Grant
    Filed: February 27, 2012
    Date of Patent: December 25, 2012
    Assignee: Pierre Fabre Medicament
    Inventors: Jean Deregnaucourt, Richard Grosse
  • Patent number: RE44339
    Abstract: Cooling compounds are provided having the formula: wherein, m is 0 or 1, Y and Z are selected independently from the group consisting of H, OH, C1-C4 straight or branched alkyl, and a C1-C4 straight or branched alkoxy, X is (CH2)n—R, where n is 0 or 1 and R is a group with non-bonding electrons, with the provisos that: (a) when Y and Z are H, X is not F, OH, MeO or NO2 in the 4-position and is not OH in the 2 or 6-position (b) when Y or Z is H then X, Y and Z are such that (i) the groups in the 3- and 4-positions are not both OMe, (ii) the groups in the 4- and 5-positions are not both OMe, (iii) the groups in 3- and 5-positions are not OMe if the group in the 4-position is OH, and (iv) the groups in the 3- and 5-positions are not OH if the group in the 4-position is methyl.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: July 2, 2013
    Assignee: Givaudan S.A.
    Inventors: Christophe C. Galopin, Pablo Victor Krawec, Jay Patrick Slack, Lori W. Tigani