Nitrogen Or C(=x), Wherein X Is Chalcogen, Attached Indirectly To The Seven-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 514/217.12)
  • Patent number: 10167295
    Abstract: Provided herein, inter alia, are methods and compositions for achieving an analgesic effect in subjects in need thereof.
    Type: Grant
    Filed: September 11, 2015
    Date of Patent: January 1, 2019
    Assignee: The Regents of the University of California
    Inventors: Jon D. Levine, Alejandra Gallardo-Godoy
  • Patent number: 9427422
    Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a cardiovascular disease in an individual using such pharmaceutical compositions.
    Type: Grant
    Filed: October 21, 2014
    Date of Patent: August 30, 2016
    Assignee: Infirst Healthcare Limited
    Inventors: Robin Mark Bannister, John Brew, Suzanne Jane Dilly, Gregory Alan Stoloff, Wilson Caparros-Wanderley
  • Publication number: 20140377219
    Abstract: Chemical compounds that inhibit retroviruses are presented herein. More particularly, this disclosure provides small molecule compounds that inhibit infection with, or treat infection caused by, human immunodeficiency viruses.
    Type: Application
    Filed: September 6, 2012
    Publication date: December 25, 2014
    Applicant: New York Blood CEnter, Inc.
    Inventors: Asim Kumar Debnath, Francesca Curreli, Peter D. Kwong, Young Do Kwon
  • Patent number: 8841290
    Abstract: Disclosed is a tetrahydronapthalene compound having Formula I the variables of which are as described herein, methods of preparing same and their use.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: September 23, 2014
    Assignee: Sanofi
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
  • Patent number: 8791102
    Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particular, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: July 29, 2014
    Assignee: Exelixis, Inc.
    Inventors: Mohamed Abdulkader Ibrahim, Joon Won Jeong, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Gary L. Lewis, Robin Tammie Noguchi, John M. Nuss
  • Publication number: 20140206666
    Abstract: Pharmaceutical compositions of the invention comprise sulfamoylbenzamide derivative useful as pregenomic RNA encapsidation inhibitors, useful for the treatment of Hepatitis B virus (HBV) infection.
    Type: Application
    Filed: June 29, 2012
    Publication date: July 24, 2014
    Applicants: Philadelphia Helath & Education Corporation d/b/a Drexel University College of Medicine, Institute for Hepatitis and Virus Research
    Inventors: Ju-Tao Guo, Xiaodong Xu, Timothy M. Block
  • Publication number: 20140179661
    Abstract: A N1-cyclic amine-N5-substituted biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.
    Type: Application
    Filed: April 8, 2012
    Publication date: June 26, 2014
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Sung Wuk Kim, Chang Hee Min, Se Hwan Park, Duck Kim, Ji Sun Lee, Yong Eun Kim, Ju Hoon Oh
  • Publication number: 20140179660
    Abstract: An N1-cyclic amine-N5-substituted phenyl biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.
    Type: Application
    Filed: August 8, 2012
    Publication date: June 26, 2014
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Sung Wuk Kim, Chang Hee Min, Se Hwan Park, Duck Kim, Ji Sun Lee, Yong Eun Kim, Ju Hoon Oh
  • Patent number: 8729069
    Abstract: The invention relates to compounds of structural formula (Ia): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, X4, X6, X10, R1, Y, Z, L, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: September 28, 2010
    Date of Patent: May 20, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Gary Bohnert, Shoujun Chen, Yu Xie
  • Publication number: 20130196978
    Abstract: Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.
    Type: Application
    Filed: March 14, 2013
    Publication date: August 1, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • Publication number: 20130102591
    Abstract: The invention provides compositions and methods for prevention, treatment, or management of pulmonary hypertension using piperidine, pyrrolidine, or azepane derivatives comprising one to four nitric oxide (NO) donor groups and a reactive oxygen species (ROS) degradation catalyst. The invention further provides a water dispersible powder comprising nanoparticles comprising said derivatives, as well as pharmaceutical compositions thereof and methods of use.
    Type: Application
    Filed: January 26, 2011
    Publication date: April 25, 2013
    Inventors: Andrew Lurie Salzman, Shlomo Magdassi, Katrin Margulis-Goshen
  • Publication number: 20130059829
    Abstract: A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme activity.
    Type: Application
    Filed: July 20, 2012
    Publication date: March 7, 2013
    Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Yixian Chen, Jurgen Dinges, Karla Drescher, Peer Jacobson, Hwan-soo Jae, Ravi Kurukulasuriya, James T. Link, David J. Madar, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Lynne E. Rueter, Qi Shuai, Bryan K. Sorensen, Jiahong Wang, Karsten M. Wicke, Martin Winn, Dariusz Wodka, Vince Yeh, Hong Yong
  • Patent number: 8372841
    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: August 25, 2011
    Date of Patent: February 12, 2013
    Assignee: Abbott Laboratories
    Inventors: Marina A. Pliushchev, Dariusz Wodka, Bryan K. Sorensen, James T. Link
  • Publication number: 20120308608
    Abstract: Provided herein are Compounds that induce interferon production and methods for identifying such Compounds. Also provided herein are compositions comprising such Compounds and methods of using such Compounds to treat interferon-sensitive diseases such as viral infections, cancer, and multiple sclerosis.
    Type: Application
    Filed: January 31, 2011
    Publication date: December 6, 2012
    Inventors: Megan Shaw, Mila Ortigoza, Adolfo Garcia-Sastre, Peter Palese
  • Patent number: 8163735
    Abstract: The present invention is directed to compounds of formula (I) that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. Wherein R3 is -alkylene-SO2NR5R6.
    Type: Grant
    Filed: December 1, 2005
    Date of Patent: April 24, 2012
    Assignee: Virobay, Inc.
    Inventors: Soon H. Woo, Randall W. Vivian, John O. Link
  • Publication number: 20120046276
    Abstract: A method of preventing or treating diseases caused by Mycobacterium, comprising administering to a subject in need of such treatment an effective amount of a pleuromutilin.
    Type: Application
    Filed: October 25, 2011
    Publication date: February 23, 2012
    Applicant: Nabriva Therapeutics AG
    Inventors: Gerd Ascher, Heinz Berner, Rosemarie Mang
  • Publication number: 20120015936
    Abstract: The invention relates to substituted tetrahydronaphthalenes, to derivatives thereof, to physiologically acceptable salts thereof, to physiologically functional derivatives, to the production thereof, to drugs containing at least one substituted tetrahydronaphthalene according to the invention or derivative thereof, and to the use of the substituted tetrahydronaphthalenes according to the invention and to derivatives thereof as MCH antagonists.
    Type: Application
    Filed: February 12, 2010
    Publication date: January 19, 2012
    Applicant: SANOFI
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
  • Publication number: 20110306603
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: August 23, 2011
    Publication date: December 15, 2011
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. Wentland
  • Publication number: 20110288076
    Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particularly, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.
    Type: Application
    Filed: October 16, 2009
    Publication date: November 24, 2011
    Applicant: EXELIXIS, INC.
    Inventors: Mohamed Abdulkader Ibrahim, Joon Won Jeong, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Gary L. Lewis, Robin Tammie Noguchi, John M. Nuss
  • Publication number: 20110281847
    Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.
    Type: Application
    Filed: June 23, 2011
    Publication date: November 17, 2011
    Applicant: ELI LILLY AND COMPANY
    Inventors: Robert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Timothy Alan Shepherd, Owen Brendan Wallace
  • Publication number: 20110275615
    Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH?CH—, —C?C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by a maximum of two R8 radicals, where R8 is hydrogen, C1-C4-alkyl, branched or un
    Type: Application
    Filed: October 29, 2010
    Publication date: November 10, 2011
    Inventors: Hans-Jörg Treiber, Monika Knopp, Wilfried Lubisch, Achim Moeller
  • Publication number: 20110129542
    Abstract: In its many embodiments, the present invention relates to a novel class of substituted azepine- and diazepine-sulfonamide compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: August 12, 2008
    Publication date: June 2, 2011
    Inventors: Santhosh Neelamkavil, Craig D. Boyle, Samuel Chackalamannil
  • Publication number: 20110065686
    Abstract: Use of chemical compounds obtained in silico for the preparation of pharmaceutical compositions to attenuate or inhibit Dengue virus infection. Particularly, through the interference or the modulation of several stages of viral replication cycle related with the entry of virus into host cells and the assembly of mature progeny virions. The invention also comprises the use of such pharmaceutical compositions for prophylactic and/or therapeutic treatment of infection caused by all four serotypes of Dengue virus and other flaviviruses.
    Type: Application
    Filed: February 27, 2009
    Publication date: March 17, 2011
    Inventors: Yuliet Mazola Reyes, Glay Chinea Santiago, Osmany Guirola Cruz, Roberto Vera Alvarez, Vivian Huerta Galindo, Noralvis Fleitas Salazar, Alexis Musacchio Lasa
  • Publication number: 20110021505
    Abstract: The present invention relates to the use of sulfonyl-substituted 2-sulfonylaminobenzoic acid N-phenylamides of the formula I, wherein A and R1 to R6 have the meanings indicated in the claims, for treating pain and for manufacturing a medicament for the treatment of pain.
    Type: Application
    Filed: March 30, 2010
    Publication date: January 27, 2011
    Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBH
    Inventors: Karl RUDOLPHI, Martin MICHAELIS, Hans GUEHRING
  • Publication number: 20100324025
    Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
    Type: Application
    Filed: September 21, 2009
    Publication date: December 23, 2010
    Applicant: University of Washington
    Inventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
  • Publication number: 20100298299
    Abstract: The present invention relates to new non-peptide derivatives of formula (I), wherein R1-R5, Q and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, to pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
    Type: Application
    Filed: October 27, 2007
    Publication date: November 25, 2010
    Inventors: Istvan Vago, Sandor Farkas, Katalin Hornok, Gyula Beke, Eva Bozo, Monika Vastag, Eva Szentirmay, Gyorgy Keseru, Eva Schmidt
  • Publication number: 20100286125
    Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of 4-phenyl-4-hydroxy-butyric acid and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.
    Type: Application
    Filed: March 28, 2008
    Publication date: November 11, 2010
    Inventors: Alan T. Johnson, Seongjin Kim
  • Publication number: 20100222316
    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: Application
    Filed: March 17, 2010
    Publication date: September 2, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Marina A. Pliushchev, Dariusz Wodka, Bryan K. Sorensen, James T. Link
  • Publication number: 20100173880
    Abstract: Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.
    Type: Application
    Filed: December 22, 2009
    Publication date: July 8, 2010
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Antonio Caligiuri, Mauro Riccaboni, Gabriele Amari
  • Publication number: 20100158818
    Abstract: The present application relates to N-chlorinated cationic compounds of Formula I or a salt thereof, and associated compositions and methods of use as antimicrobial agents.
    Type: Application
    Filed: November 6, 2009
    Publication date: June 24, 2010
    Inventors: Rakesh K. Jain, Eddy Low, Charles Francavilla, Timothy P. Shiau, Satheesh K. Nair
  • Patent number: 7700585
    Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.
    Type: Grant
    Filed: April 30, 2007
    Date of Patent: April 20, 2010
    Assignee: sanofi-aventis
    Inventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Florence Medaisko, Nathalie Rakotoarisoa
  • Patent number: 7687489
    Abstract: A pharmaceutical composition for the treatment and/or prevention of cerebral ischemic diseases, which comprises two components, i.e. an astrocyte function-improving agent, preferably a compound represented by the formula (I): (wherein R6 is hydroxy, etc., (1) n is 1, R11 is hydrogen and R5 is (alkyl of which one carbon atom is substituted by fluorine)-CH2— or (2) n is 0 or 1, R11 is hydrogen, etc., and R5 is alkyl, etc.) and a thrombolytic agent, preferably tissue plasminogen activator, as active ingredients. The pharmaceutical composition of the present invention exhibits a synergistic therapeutic effect compared to independent administration of an astrocyte function-improving agent and a thrombolytic agent.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: March 30, 2010
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Kaneyoshi Honjo, Narito Tateishi, Nobuo Katsube
  • Publication number: 20090247506
    Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
    Type: Application
    Filed: August 20, 2007
    Publication date: October 1, 2009
    Inventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
  • Publication number: 20090233909
    Abstract: The present invention is directed to compounds of formula (I) that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. Wherein R3 is -alkylene-SO2NR5R6.
    Type: Application
    Filed: December 1, 2005
    Publication date: September 17, 2009
    Applicant: Virobay, Inc.
    Inventors: Soon H. Woo, Randall W. Vivian, John O. Link
  • Publication number: 20090137561
    Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
    Type: Application
    Filed: October 3, 2008
    Publication date: May 28, 2009
    Applicant: Amgen Inc.
    Inventors: Sean P. Brown, Qiong Cao, Paul John Dransfield, Xiaohui Du, Jonathan Houze, Xian Yun Jiao, Yong-Jae Kim, Todd J. Kohn, SuJen Lai, An-Rong Li, Daniel Lin, Jian Luo, Julio C. Medina, Jeffrey D. Reagan, Vatee Pattaropong, Margrit Schwarz, Wang Shen, Yongli Su, Gayathri Swaminath, Marc Vimolratana, Xiang Wang, Yumei Xiong, Li Yang, Ming Yu, Jie Zhang, Liusheng Zhu
  • Publication number: 20090036420
    Abstract: The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.
    Type: Application
    Filed: July 28, 2008
    Publication date: February 5, 2009
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Publication number: 20080275028
    Abstract: The present invention relates to compounds with ?7 nAChR agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological, psychiatric, cognitive, immunological and inflammatory disorders.
    Type: Application
    Filed: July 19, 2005
    Publication date: November 6, 2008
    Inventors: Giovanni Gaviraghi, Chiara Ghiron, Hendrik Bothmann, Renza Roncarati, Georg Christian Terstappenn
  • Publication number: 20080255095
    Abstract: A compound of the formula (I): wherein R1 is C1-C6 alkyl, amino, (C1-C6 alkyl)amino, di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are hydrogen or C1-C6 alkyl; Arom is phenyl, idenyl, napthyl, phenanthrenyl, furyl, thiolyl, pyrrolyl, azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1,2,3 oxadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or quinolyl; A is C1-C6 alkylene; Ra is hydrogen, C1-C6 alkyl or C2-C6 alkenyl; E is a single bond, oxygen, sulfur or —NR4—, wherein R4 is hydrogen or C1-C7 alkanoyl; X1 and X2 are oxygen or sulfur; or a pharmacologically acceptable salt or ester thereof.
    Type: Application
    Filed: June 18, 2007
    Publication date: October 16, 2008
    Applicant: BTG INTERNATIONAL LIMITED
    Inventors: Kazuo Koyama, Shinji Marumoto, Narihiro Toda, Hiroshi Kogen, Keiko Suzuki
  • Publication number: 20080234247
    Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.
    Type: Application
    Filed: March 17, 2008
    Publication date: September 25, 2008
    Applicant: Sepracor, Inc.
    Inventors: Brian M. Aquila, James R. Hauske, Liming Shao
  • Publication number: 20080227767
    Abstract: Methods and compositions which are useful in the treatment of amyloidosis. In particular, methods and compositions are provided for inhibiting, preventing and treating amyloid deposition, e.g., in pancreatic islets, wherein the amyloidotic deposits are islet amyloid polypeptide (IAPP)-associated amyloid deposition or deposits. The methods of the invention involve administering to a subject a therapeutic compound which inhibits IAPP-associated amyloid deposits. Accordingly, the compositions and methods of the invention are useful for inhibiting IAPP-associated amyloidosis in disorders in which such amyloid deposition occurs, such as diabetes.
    Type: Application
    Filed: May 22, 2008
    Publication date: September 18, 2008
    Applicant: Neurochem (International) Limited
    Inventors: Walter A. Szarek, Donald F. Weaver, Xianqi Kong, Ajay Gupta, David Migneault
  • Publication number: 20080153808
    Abstract: Disclosed herein is a pharmaceutical composition comprising a serotonin-norepinephrine reuptake inhibitor and a pan-alpha-2 receptor agonist. The composition is effective for treating chronic pain, and methods of treating pain using the composition and compounds comprising it are also disclosed.
    Type: Application
    Filed: December 12, 2007
    Publication date: June 26, 2008
    Applicant: Allergan, Inc.
    Inventors: Daniel W. Gil, John E. Donello
  • Patent number: 7307074
    Abstract: To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such as 4-[(3-carbamimidoylphenylamino)methyl]-3-[4-(4-methyl-1,4-diazepan-1-yl)benzoylamino]benzoic acid and 3-hydroxy-4?-methoxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzanilide or a salt thereof is an effective ingredient.
    Type: Grant
    Filed: September 8, 2003
    Date of Patent: December 11, 2007
    Assignee: Astellas Pharma Inc.
    Inventors: Fukushi Hirayama, Hiroyuki Koshio, Tsukasa Ishihara, Norio Seki, Shunichiro Hachiya, Keizo Sugasawa, Ryota Shiraki, Yuji Koga, Yuzo Matsumoto, Takeshi Shigenaga, Souichirou Kawazoe
  • Publication number: 20070232581
    Abstract: There is provided a series of substituted oxime-containing acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Application
    Filed: March 29, 2007
    Publication date: October 4, 2007
    Inventors: Yong-Jin Wu, Samuel Gerritz, Shuhao Shi, Shirong Zhu
  • Patent number: 7271161
    Abstract: The present invention concerns the use of methods and compositions for the treatment of cancer and other hyperproliferative diseases. In certain embodiments, methods are described for the treatment of cancer and/or hyperproliferative diseases by administration of compositions containing at least one platinum complex alone or in combination with a modulator of glutathione. In particular, the methods may be used to treat cisplatin or carboplatin resistant tumor cells.
    Type: Grant
    Filed: September 5, 2003
    Date of Patent: September 18, 2007
    Assignee: Board of Regents, the University of Texas System
    Inventors: Zahid H. Siddik, Abdul R. Khokhar
  • Patent number: 7238685
    Abstract: The invention relates to novel benzo-fused heterocycles and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.
    Type: Grant
    Filed: July 31, 2002
    Date of Patent: July 3, 2007
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Martin Bolli, Christoph Boss, Martine Clozel, Walter Fischli, Thomas Weller, Judith Marfurt
  • Patent number: 7226917
    Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.
    Type: Grant
    Filed: April 17, 2006
    Date of Patent: June 5, 2007
    Assignee: Sanofi-Aventis
    Inventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Florence Medaisko, Nathalie Rakotoarisoa
  • Patent number: 7214714
    Abstract: A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof [wherein R1 represents a substituted morpholino group, a substituted piperidino group, a piperazin-1-yl group, a substituted piperazin-1-yl group, a thiomorpholin-1-yl group, a perhydroazepin-1-yl group, a perhydroazocin-1-yl group, a tetrahydropyridin-1-yl group, a pyrrolin-1-yl group, etc.; X represents a nitrogen atom or a group represented by CR5; and R2 to R5 are the same or different and each represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a trifluoromethyl group or a halogen atom.] There is provided a drug which inhibits an enzyme producing 20-HETE participating in a contracting or dilating action for microvessels and an inducing action for cell proliferation in main organs such as kidney and cerebrovascular vessels.
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: May 8, 2007
    Assignee: Taisho Pharmaceutical Co. Ltd.
    Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Matsunaga, Hideaki Amada
  • Patent number: 7199158
    Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein R1–R6, R7, R7?, R8, R30–R34, X?, Y, Y?, t, x, and n are as defined herein, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: July 18, 2005
    Date of Patent: April 3, 2007
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 7141560
    Abstract: The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these alanine 2,6-dialkoxyphenyl ester derivatives as hypnotics for the induction and maintenance of general anaesthesia.
    Type: Grant
    Filed: January 17, 2002
    Date of Patent: November 28, 2006
    Assignee: Akzo Nobel N.V.
    Inventors: Niall Morton Hamilton, David Jonathan Bennett
  • Patent number: RE43481
    Abstract: To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such as 4-[(3-carbamimidoylphenylamino)methyl]-3-[4-(4-methyl-1,4-diazepan-1-yl)benzoylamino]benzoic acid and 3-hydroxy-4?-methoxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzanilide or a salt thereof is an effective ingredient.
    Type: Grant
    Filed: September 3, 2008
    Date of Patent: June 19, 2012
    Assignee: Astellas Pharma Inc.
    Inventors: Fukushi Hirayama, Hiroyuki Koshio, Tsukasa Ishihara, Norio Seki, Shunichiro Hachiya, Keizo Sugasawa, Ryota Shiraki, Yuji Koga, Yuzo Matsumoto, Takeshi Shigenaga, Souichirou Kawazoe