Plural Acyclic Nitrogens Bonded Directly To The Same Carbon Or Single Bonded Directly To Each Other Patents (Class 546/231)
  • Patent number: 9884821
    Abstract: The present invention provides an N1-cyclic amine-N5-substituted biguanide derivative compound represented by Formula 1, a method of preparing the same and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient. The biguanide derivatives have an effect of inhibiting cancer cell proliferation, cancer metastasis and cancer recurrence by activation of AMPK, even when administered in a small dose compared with conventional drugs.
    Type: Grant
    Filed: February 6, 2014
    Date of Patent: February 6, 2018
    Assignee: ImmunoMet Therapeutics Inc.
    Inventors: Chang Hee Min, Yong Eun Kim, Byung Kyu Oh, Ji Sun Lee, Hye Jin Heo, Ju Hoon Oh, Woong Cho
  • Publication number: 20150126518
    Abstract: The present invention relates to biguanide compounds and use thereof, more particularly, to biguanide derivatives exhibiting excellent effects for inhibition of cancer cell proliferation and inhibition of cancer metastasis and recurrence, a method for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and a method of prevention or treatment of cancer comprising the step of administering an effective amount of the composition to a subject in need thereof.
    Type: Application
    Filed: October 30, 2014
    Publication date: May 7, 2015
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Hong Woo KIM, Ji Sun LEE, Hye Jin HEO, Hong Bum LEE, Jae Kap JEONG, Ji Hyun PARK, Seo-il KIM, Young Woo LEE
  • Patent number: 8877749
    Abstract: The present application describes modulators of chemokine receptor activity of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: November 4, 2014
    Assignee: Bristol-Myers Squibbs Company
    Inventors: T. G. Murali Dhar, John V. Duncia, Daniel S. Gardner, Weiwei Guo, John Hynes
  • Publication number: 20140200225
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 17, 2014
    Applicant: ORION CORPORATION
    Inventors: Rajeev GOSWAMI, Anil Kumar VUPPALA, Ramesh VELUDANDI, Ramesh SISTLA, Chakshusmathi GHADIYARAM, Muralidhara RAMACHANDRA
  • Publication number: 20140194433
    Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.
    Type: Application
    Filed: March 12, 2014
    Publication date: July 10, 2014
    Applicant: BASF SE
    Inventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
  • 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
  • Publication number: 20140073795
    Abstract: The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.
    Type: Application
    Filed: November 13, 2013
    Publication date: March 13, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Sergio Cesco-Cancian, Hongfeng Chen, Jeffrey S. Grimm, Neelakandha S. Mani, Christopher M. Mapes, David C. Palmer, Daniel J. Pippel, Kirk L. Sorgi, Tong Xiao
  • Publication number: 20140073573
    Abstract: The invention provides compounds that are effective as inhibitors of human plasmin and plasma kallikrein, and that are useful for the prevention of blood loss and as components of fibrin adhesives. The invention further provides methods of making and using the compounds.
    Type: Application
    Filed: October 31, 2013
    Publication date: March 13, 2014
    Applicant: THE MEDICINES COMPANY (LEIPZIG) GMBH
    Inventors: Peter HEROLD, Mohammed DAGHISH, Stjepan JELAKOVIC, Friedrich-Alexander LUDWIG, Claudia REICHELT, Alexander SCHULZE, Andrea SCHWEINITZ
  • Publication number: 20140011996
    Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).
    Type: Application
    Filed: August 29, 2013
    Publication date: January 9, 2014
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan Pajouhesh, Ramesh Kaul, Yanbing Ding, Yongbao Zhu, Lingyun Zhang, Nagasree Chakka, MIchael Edward Grimwood, Jason Tan, Yuanxi Zhou
  • Patent number: 8536343
    Abstract: Disclosed is an arylamidine derivative represented by the following general formula: (wherein R1 and R2 independently represent an optionally substituted C3-4 alkyl group) or a salt thereof, which is useful as an antifungal agent.
    Type: Grant
    Filed: December 27, 2006
    Date of Patent: September 17, 2013
    Assignee: Toyama Chemical Co., Ltd.
    Inventor: Kazuya Hayashi
  • Publication number: 20130237541
    Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders and the like.
    Type: Application
    Filed: September 14, 2012
    Publication date: September 12, 2013
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Bradley Teegarden, Honnappa Jayakumar, Hongmei Li, Sonja Strah-Pleynet, Peter Ian Dosa
  • Publication number: 20130172388
    Abstract: Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 are independently H, alkyl, or alkenyl; R3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; R4 and R5 are independently a bond, alkylenyl, or alkenylenyl; each R6 and R7 is independently selected from the group consisting of OH, F, Cl, Br, I, (C1-C6)alkyl, alkoxy, amino, COOH, CONH2, SO3H, PO3H2, CN, SH, NO2 and CF3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma.
    Type: Application
    Filed: December 14, 2012
    Publication date: July 4, 2013
    Applicant: University of Pittsburgh -- Of the Commonwealth System of Higher Education
    Inventor: University of Pittsburgh -- Of the Commonwealth System of Higher Education
  • Patent number: 8440833
    Abstract: HPV inhibitors of formula (I) in which G1 is —NHCO(CH2)n-, where n is an integer between 1 and 4, R3 is —CW(CH2)m—NR4R5 or —CW(CH2)mCH3 or —CN, where W is O, S or NH and m is an integer between 0 and 5, or R3 is one of the following groups: and A is an optionally substituted aryl group and B is an aryl group, preferably a phenyl which is substituted.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: May 14, 2013
    Assignee: Anaconda Pharma
    Inventors: Marta Blumenfeld, Delphine Compere, Jean-Michel Gauthier
  • Patent number: 8436188
    Abstract: Disclosed is a method for the separation of S-(?)-amlodipine from a racemic amlodipine. Featuring the use of inexpensive L-tartaric acid as an optical resolution agent and DMAC as a solvent, the separation method allows the resolution of S-(?)-amlodipine from racemic amlodipine at high yield and to a satisfactory enantiomeric excess and thus is economically favorable and applicable to the mass production of the optical isomer.
    Type: Grant
    Filed: October 26, 2007
    Date of Patent: May 7, 2013
    Assignee: CJ Cheiljedang Corporation
    Inventors: Seog Beom Song, Il Hwan Cho, Yong Sik Youn, Dong Kwon Lim
  • Patent number: 8404693
    Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.
    Type: Grant
    Filed: January 17, 2011
    Date of Patent: March 26, 2013
    Assignee: Adolor Corporation
    Inventors: Roland E. Dolle, Bertrand Le Bourdonnec
  • Patent number: 8343963
    Abstract: The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: January 1, 2013
    Assignee: 4SC AG
    Inventor: Stefano Pegoraro
  • Patent number: 8198304
    Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: September 9, 2011
    Date of Patent: June 12, 2012
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
  • Patent number: 8173157
    Abstract: A pharmaceutical composition comprising a phenylamidine derivative or a salt thereof, represented by a general formula, wherein R1 and R2 may be same or different, and represent an optionally substituted C3-4alkyl group; and one or more agents selected from azole antifungal agents, polyene antifungal agents, candin antifungal agents and fluoropyrimidine antifungal agents, and a method for combination use of the phenylamidine derivative or a salt thereof and the agents are useful for treating fungal infections caused by a fungal pathogen.
    Type: Grant
    Filed: October 3, 2007
    Date of Patent: May 8, 2012
    Assignee: Toyama Chemical Co., Ltd.
    Inventor: Hiroshi Nishikawa
  • Patent number: 8158800
    Abstract: To provide novel crystals of 4-{3-[4-(3-{4-[amino(butoxycarbonylimino)methyl]phenoxy}propyl)-1-piperidinyl]propoxy}-N?-(butoxycarbonyl)benzamidine. Means for Solving the Problems The type II crystal, the type III crystal and the type IV crystal of 4-{3-[4-(3-{4-[amino(butoxycarbonylimino)methyl]phenoxy}propyl)-1-piperidinyl]propoxy}-N?-(butoxycarbonyl)benzamidine are useful as excellent drug substances of antifungal agents.
    Type: Grant
    Filed: July 2, 2008
    Date of Patent: April 17, 2012
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Junichi Mitsuyama, Naokatsu Aoki
  • Patent number: 8153669
    Abstract: Compounds of formula (I), in salt or zwitterionic form, wherein J, L, M, R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
    Type: Grant
    Filed: December 22, 2005
    Date of Patent: April 10, 2012
    Assignee: Novartis AG
    Inventors: Neil John Press, Stephen Paul Collingwood
  • Publication number: 20110145970
    Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.
    Type: Application
    Filed: August 26, 2009
    Publication date: June 23, 2011
    Applicant: BASF SE
    Inventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
  • Patent number: 7947730
    Abstract: Compounds of formula I in salt or zwitterionic form wherein, wherein R1, R2, R3, R4, R5, J, L and M have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
    Type: Grant
    Filed: June 23, 2004
    Date of Patent: May 24, 2011
    Assignee: Novartis AG
    Inventors: Stephen Paul Collingwood, Urs Baettig, Clive McCarthy
  • Publication number: 20110098392
    Abstract: The present invention relates to an organopolysiloxane composition that can be vulcanized at room temperature into an elastomer that is crosslinked by polycondensation and that does not contain alkyltin-based catalysts which exhibit toxicity problems. The invention also relates to novel polycondensation catalysts having a guanidine structure, in silicone chemistry, and to the uses thereof as catalysts for the organopolysiloxane polycondensation reaction.
    Type: Application
    Filed: March 24, 2009
    Publication date: April 28, 2011
    Applicant: BLUESTAR SILICONES FRANCE
    Inventors: Georges Barrandon, Delphine Blanc, Christian Maliverney, Hervé Parisot
  • Publication number: 20110046381
    Abstract: Problems To provide novel crystals of 4-{3-[4-(3-{4-[amino(butoxycarbonylimino)methyl]phenoxy}propyl)-1-piperidinyl]propoxy}-N?-(butoxycarbonyl)benzamidine. Means for Solving the Problems The type II crystal, the type III crystal and the type IV crystal of 4-{3-[4-(3-{4-[amino(butoxycarbonylimino)methyl]phenoxy}propyl)-1-piperidinyl]propoxy}-N?-(butoxycarbonyl)benzamidine are useful as excellent drug substances of antifungal agents.
    Type: Application
    Filed: July 2, 2008
    Publication date: February 24, 2011
    Applicant: Toyama Chemical Co., Ltd.
    Inventors: Junichi Mitsuyama, Naokatsu Aoki
  • Patent number: 7884102
    Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.
    Type: Grant
    Filed: April 28, 2008
    Date of Patent: February 8, 2011
    Assignee: Adolor Corporation
    Inventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
  • Patent number: 7875603
    Abstract: The present application describes isoindoles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful inhibitors of VEGFR.
    Type: Grant
    Filed: September 21, 2007
    Date of Patent: January 25, 2011
    Assignee: Nova Southeastern University
    Inventors: Appu Rathinavelu, Sivanesan Dakshanamurthy, Nagarajan Pattabiraman
  • Publication number: 20100305090
    Abstract: The invention relates to meta-substituted phenyl sulfonyl amides of secondary amino acid amides according to the general formula (I), (II), or (III), the production thereof, and the use thereof as matriptase inhibitors, in particular the use thereof as drugs for inhibiting tumor growth and/or metastasization.
    Type: Application
    Filed: March 5, 2008
    Publication date: December 2, 2010
    Inventors: Torsten Steinmetzer, Andrea Schweinitz, Daniel Donnecke
  • Publication number: 20100093798
    Abstract: The present application describes modulators of MIP-1? or CCR-1 of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n, ring A, T, V, X, R1, R2 and R8, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
    Type: Application
    Filed: October 3, 2007
    Publication date: April 15, 2010
    Inventor: Percy H. Carter
  • Patent number: 7585858
    Abstract: Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
    Type: Grant
    Filed: May 26, 2005
    Date of Patent: September 8, 2009
    Assignee: Abbott Laboratories
    Inventors: Steven W. Elmore, Milan Bruncko, Cheol-Min Park
  • Patent number: 7582656
    Abstract: Compounds of the formula (I): in which the radicals R and R1 to R10 are as defined in the description, processes for the preparation of them, use thereof for the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: June 28, 2005
    Date of Patent: September 1, 2009
    Assignee: Merck Patent Gesellschaft
    Inventors: Didier Roche, Bruno Roux, Isabelle Berard
  • Publication number: 20090209586
    Abstract: HPV inhibitors with formula (I) where G1 represents a hydrocarbonated bond or chain possibly substituted by one or two alkyl groups, G2 represents a group (see formula Ia+Ib) or R represents a hydrogen, an alkyl, halogenoalkyl, or a prodrug radical such as carbamate, acetyl or dialkylaminomethyl, G represents a bond or a hydrocarbonated chain possibly substituted by one or two alkyls, W represents an oxygen or sulphur, R1 and R2 each represent a group chosen from among hydrogen, halogen, hydroxyl, thio, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, amino, monoalkylamino, dialkylamino, cycloalkyl, alkyl or halogenoalkyl, R3 represents an acid or a prodrug radical of the acid function or a bioisostere of the acid function, A represents an aryl, cycloalkyl, cycloalkenyl or a heterocycle, each possibly substituted, and B represents an aryl or a heterocycle with 6 chains, each possibly substituted, and pharmaceutically acceptable salts.
    Type: Application
    Filed: May 18, 2007
    Publication date: August 20, 2009
    Inventors: Marta Blumenfeld, Delphine Compere, Jean-Michel Gauthier
  • Publication number: 20090186921
    Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is administered to a patient in need of such treatment.
    Type: Application
    Filed: January 16, 2009
    Publication date: July 23, 2009
    Applicant: ACADIA PHARMACEUTICALS, INC.
    Inventors: Carl-Magnus A. Andersson, Glenn Croston, E. L. Hansen, Allan Kjaersgaard Uldam
  • Patent number: 7550486
    Abstract: The present application describes modulators of chemokine receptor activity of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis, including methods of preparing and intermediates thereof.
    Type: Grant
    Filed: January 11, 2008
    Date of Patent: June 23, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Soo S. Ko, George V. Delucca
  • Patent number: 7541468
    Abstract: The present application describes a process of preparing a compound of formula (IV), or salt or stereoisomer thereof: wherein Pg, at each occurrence, is independently selected from an amine protecting group; comprising the steps of reacting a compound of Formula with a reducing agent to give a compound of Formula III: reacting the compound of formula (III) with an amine of formula (IIa) using reductive amination to give the compound of formula (III)
    Type: Grant
    Filed: June 9, 2005
    Date of Patent: June 2, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventor: Percy H. Carter
  • Patent number: 7473779
    Abstract: Novel derivatives of amidines of formula wherein the substituents are defined as in the specification which are useful for inhibiting activity on NO-synthase enzymes producing nitrogen mono oxide and/or trapping the reactive oxygen species (ROS) making them useful for treating various diseases.
    Type: Grant
    Filed: September 12, 2003
    Date of Patent: January 6, 2009
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Serge Auvin, Pierre-Etienne Chabrier de Lassauniere, Jeremiah Harnett, Dominique Pons, Gérard Ulibarri
  • Publication number: 20080293722
    Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.
    Type: Application
    Filed: March 15, 2005
    Publication date: November 27, 2008
    Applicant: Wyeth
    Inventors: Robert Zelle, Christopher Todd Baker, Paul Will, Vincent P. Galullo
  • Patent number: 7452891
    Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
    Type: Grant
    Filed: January 28, 2005
    Date of Patent: November 18, 2008
    Assignee: Schering Corporation
    Inventors: John W. Clader, Hubert B. Josien, Anandan Palani, Tin Yau Chan
  • Publication number: 20080261952
    Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.
    Type: Application
    Filed: August 16, 2005
    Publication date: October 23, 2008
    Inventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Andrew Simon Swain, Phillppe Wong-Kai-In
  • Publication number: 20080139585
    Abstract: The present application describes isoindoles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful inhibitors of VEGFR.
    Type: Application
    Filed: September 21, 2007
    Publication date: June 12, 2008
    Applicant: NOVA SOUTHEASTERN UNIVERSITY
    Inventors: Appu Rathinavelu, Sivanesan Dakshanamurthy, Nagarajan Pattabiraman
  • Publication number: 20080132523
    Abstract: The present application describes modulators of chemokine receptor activity of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis, including methods of preparing and intermediates thereof.
    Type: Application
    Filed: January 11, 2008
    Publication date: June 5, 2008
    Inventors: Soo S. Ko, George V. Delucca
  • Patent number: 7365070
    Abstract: This invention provides compounds and methods for treating melanocortin receptor associated disorders, such as weight loss disorders including cachexia resulting from cancer and other chronic illnesses. The compounds are represented by formula I: wherein X is oxygen or sulfur; G is G1 or G2: L1, L2, L3 and Q are linker groups, and Rings A, B and C, and R1-R14 are described in the specification. The compounds are antagonists of melanocortin receptors.
    Type: Grant
    Filed: December 4, 2003
    Date of Patent: April 29, 2008
    Assignee: Ore Pharmaceuticals Inc.
    Inventors: Tricia J. Vos, Michael Patane, Michael E. Solomon, Christopher Blackburn, Mihaela D. Danca
  • Patent number: 7259157
    Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
    Type: Grant
    Filed: April 2, 2002
    Date of Patent: August 21, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Nigel J. Liverton, John W. Butcher, Charles McIntyre, Christopher F. Claiborne, David A. Claremon, John A. McCauley, Joseph J. Romano, Wayne Thompson, Peter M. Munson
  • 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: 7074820
    Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
    Type: Grant
    Filed: April 23, 2001
    Date of Patent: July 11, 2006
    Assignee: AstraZeneca AB
    Inventor: Thomas Antonsson
  • Patent number: 7064210
    Abstract: A light resistant colorant is obtained by coupling a dye or a pigment with a light resistant material. A light resistant colorant-containing composition has no additional light stabilizer. Therefore, side effects caused by the addition of a light stabilizer, such as precipitate generation, may be prevented. Furthermore, substrates to which the composition is applied preserve excellent light resistance for a long term.
    Type: Grant
    Filed: September 29, 2003
    Date of Patent: June 20, 2006
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Yeon-kyoung Jung, Seung-min Ryu
  • Patent number: 6946477
    Abstract: One aspect of the present invention relates to novel heterocyclic compounds comprising urea functionality. A second aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as ligands for various cellular receptors, including opioid 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 comprising urea functionality as analgesics.
    Type: Grant
    Filed: November 5, 2002
    Date of Patent: September 20, 2005
    Assignee: Sepracor Inc.
    Inventors: Brian M. Aquila, Gregory D. Cuny, James R. Hauske, Liming Shao, Xinhe Wu
  • Patent number: 6919356
    Abstract: The present application describes modulators of chemokine receptors of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: September 25, 2003
    Date of Patent: July 19, 2005
    Assignee: Bristol Myers Squibb Company
    Inventor: Douglas G. Batt
  • Patent number: 6911477
    Abstract: This invention relates to a novel class of partial or full muscarinic receptor agonists intermediates for their preparation, and pharmaceutical compositions and methods of use for the treatment or prevention of diseases the treatment or prevention of which is mediated by muscarinic receptor agonism.
    Type: Grant
    Filed: February 28, 2003
    Date of Patent: June 28, 2005
    Assignee: Pfizer Inc.
    Inventors: Anabella Villalobos, Daniel Yohannes, Jolanta Nowakowski, Dane R. Liston
  • Patent number: 6906066
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: June 19, 2003
    Date of Patent: June 14, 2005
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker, Paul S. Watson, Jeffrey G. Varnes, Wenqing Yao