Plural Acyclic Nitrogens Bonded Directly To The Same Carbon Or Single Bonded Directly To Each Other Patents (Class 546/231)
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Patent number: 11274079Abstract: The disclosure relates to a 2-(2,2-diarylethyl)-cyclic amine derivative or salt, a synthesis method, an application and a composition thereof. Biological activity test shows that this kind of 2-(2,2-diarylethyl)-cyclic amine derivative has good M-receptor antagonistic activity; and can be used as an active component of drugs for the treatment of the diseases mediated or regulated by muscarinic receptors, such as asthma, chronic obstructive pulmonary disease (COPD), overactive bladder (OAB), bronchospasm with chronic obstructive pulmonary disease, visceral spasm, irritable bowel syndrome, Parkinson's disease, depression or anxiety, schizophrenia and related mental diseases.Type: GrantFiled: April 11, 2019Date of Patent: March 15, 2022Assignee: Dalian Institute of Chemical Physics, Chinese Academy of SciencesInventors: Xinmiao Liang, Yaopeng Zhao, Yanfang Liu, Jixia Wang, Changjian Wang, Zhiwei Wang, Nana Du, Xiuli Zhang, Zhimou Guo, Chaoran Wang
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Patent number: 10590081Abstract: The present invention relates to guanidine compounds for inhibiting mitochondrial oxidative phosphorylation (OXPHOS) and use thereof. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating a OXPHOS-related disease, particularly cancer by inhibiting mitochondrial oxidative phosphorylation and reprogramming cellular metabolism.Type: GrantFiled: April 30, 2015Date of Patent: March 17, 2020Assignee: ImmunoMet Therapeutics Inc.Inventors: Sung Wuk Kim, Hong Woo Kim, Sang Hee Yoo, Ji Sun Lee, Hye Jin Heo, Hong Bum Lee, Ji Ae Kook, Young Woo Lee
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Patent number: 9884821Abstract: 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: GrantFiled: February 6, 2014Date of Patent: February 6, 2018Assignee: ImmunoMet Therapeutics Inc.Inventors: Chang Hee Min, Yong Eun Kim, Byung Kyu Oh, Ji Sun Lee, Hye Jin Heo, Ju Hoon Oh, Woong Cho
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Publication number: 20150126518Abstract: 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: ApplicationFiled: October 30, 2014Publication date: May 7, 2015Applicant: 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
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Patent number: 8877749Abstract: 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: GrantFiled: October 6, 2010Date of Patent: November 4, 2014Assignee: Bristol-Myers Squibbs CompanyInventors: T. G. Murali Dhar, John V. Duncia, Daniel S. Gardner, Weiwei Guo, John Hynes
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Publication number: 20140200225Abstract: 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: ApplicationFiled: March 27, 2014Publication date: July 17, 2014Applicant: ORION CORPORATIONInventors: Rajeev GOSWAMI, Anil Kumar VUPPALA, Ramesh VELUDANDI, Ramesh SISTLA, Chakshusmathi GHADIYARAM, Muralidhara RAMACHANDRA
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Publication number: 20140194433Abstract: 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: ApplicationFiled: March 12, 2014Publication date: July 10, 2014Applicant: BASF SEInventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
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Publication number: 20140179661Abstract: 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: ApplicationFiled: April 8, 2012Publication date: June 26, 2014Applicant: 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
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Publication number: 20140179660Abstract: 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: ApplicationFiled: August 8, 2012Publication date: June 26, 2014Applicant: 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
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Publication number: 20140073573Abstract: 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: ApplicationFiled: October 31, 2013Publication date: March 13, 2014Applicant: THE MEDICINES COMPANY (LEIPZIG) GMBHInventors: Peter HEROLD, Mohammed DAGHISH, Stjepan JELAKOVIC, Friedrich-Alexander LUDWIG, Claudia REICHELT, Alexander SCHULZE, Andrea SCHWEINITZ
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Publication number: 20140073795Abstract: 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: ApplicationFiled: November 13, 2013Publication date: March 13, 2014Applicant: Janssen Pharmaceutica NVInventors: 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
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Publication number: 20140011996Abstract: 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: ApplicationFiled: August 29, 2013Publication date: January 9, 2014Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Hassan Pajouhesh, Ramesh Kaul, Yanbing Ding, Yongbao Zhu, Lingyun Zhang, Nagasree Chakka, MIchael Edward Grimwood, Jason Tan, Yuanxi Zhou
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Patent number: 8536343Abstract: 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: GrantFiled: December 27, 2006Date of Patent: September 17, 2013Assignee: Toyama Chemical Co., Ltd.Inventor: Kazuya Hayashi
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Publication number: 20130237541Abstract: 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: ApplicationFiled: September 14, 2012Publication date: September 12, 2013Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Bradley Teegarden, Honnappa Jayakumar, Hongmei Li, Sonja Strah-Pleynet, Peter Ian Dosa
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Publication number: 20130172388Abstract: 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: ApplicationFiled: December 14, 2012Publication date: July 4, 2013Applicant: University of Pittsburgh -- Of the Commonwealth System of Higher EducationInventor: University of Pittsburgh -- Of the Commonwealth System of Higher Education
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Patent number: 8440833Abstract: 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: GrantFiled: November 20, 2008Date of Patent: May 14, 2013Assignee: Anaconda PharmaInventors: Marta Blumenfeld, Delphine Compere, Jean-Michel Gauthier
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Patent number: 8436188Abstract: 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: GrantFiled: October 26, 2007Date of Patent: May 7, 2013Assignee: CJ Cheiljedang CorporationInventors: Seog Beom Song, Il Hwan Cho, Yong Sik Youn, Dong Kwon Lim
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Patent number: 8404693Abstract: 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: GrantFiled: January 17, 2011Date of Patent: March 26, 2013Assignee: Adolor CorporationInventors: Roland E. Dolle, Bertrand Le Bourdonnec
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Patent number: 8343963Abstract: 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: GrantFiled: January 29, 2010Date of Patent: January 1, 2013Assignee: 4SC AGInventor: Stefano Pegoraro
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Patent number: 8198304Abstract: 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: GrantFiled: September 9, 2011Date of Patent: June 12, 2012Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Patent number: 8173157Abstract: 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: GrantFiled: October 3, 2007Date of Patent: May 8, 2012Assignee: Toyama Chemical Co., Ltd.Inventor: Hiroshi Nishikawa
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Patent number: 8158800Abstract: 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: GrantFiled: July 2, 2008Date of Patent: April 17, 2012Assignee: Toyama Chemical Co., Ltd.Inventors: Junichi Mitsuyama, Naokatsu Aoki
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Patent number: 8153669Abstract: 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: GrantFiled: December 22, 2005Date of Patent: April 10, 2012Assignee: Novartis AGInventors: Neil John Press, Stephen Paul Collingwood
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Publication number: 20110145970Abstract: 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: ApplicationFiled: August 26, 2009Publication date: June 23, 2011Applicant: BASF SEInventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
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Patent number: 7947730Abstract: 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: GrantFiled: June 23, 2004Date of Patent: May 24, 2011Assignee: Novartis AGInventors: Stephen Paul Collingwood, Urs Baettig, Clive McCarthy
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Publication number: 20110098392Abstract: 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: ApplicationFiled: March 24, 2009Publication date: April 28, 2011Applicant: BLUESTAR SILICONES FRANCEInventors: Georges Barrandon, Delphine Blanc, Christian Maliverney, Hervé Parisot
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Publication number: 20110046381Abstract: 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: ApplicationFiled: July 2, 2008Publication date: February 24, 2011Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Mitsuyama, Naokatsu Aoki
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Patent number: 7884102Abstract: 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: GrantFiled: April 28, 2008Date of Patent: February 8, 2011Assignee: Adolor CorporationInventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
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Patent number: 7875603Abstract: The present application describes isoindoles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful inhibitors of VEGFR.Type: GrantFiled: September 21, 2007Date of Patent: January 25, 2011Assignee: Nova Southeastern UniversityInventors: Appu Rathinavelu, Sivanesan Dakshanamurthy, Nagarajan Pattabiraman
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Publication number: 20100305090Abstract: 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: ApplicationFiled: March 5, 2008Publication date: December 2, 2010Inventors: Torsten Steinmetzer, Andrea Schweinitz, Daniel Donnecke
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Publication number: 20100093798Abstract: 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: ApplicationFiled: October 3, 2007Publication date: April 15, 2010Inventor: Percy H. Carter
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Patent number: 7585858Abstract: 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: GrantFiled: May 26, 2005Date of Patent: September 8, 2009Assignee: Abbott LaboratoriesInventors: Steven W. Elmore, Milan Bruncko, Cheol-Min Park
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Patent number: 7582656Abstract: 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: GrantFiled: June 28, 2005Date of Patent: September 1, 2009Assignee: Merck Patent GesellschaftInventors: Didier Roche, Bruno Roux, Isabelle Berard
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Publication number: 20090209586Abstract: 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: ApplicationFiled: May 18, 2007Publication date: August 20, 2009Inventors: Marta Blumenfeld, Delphine Compere, Jean-Michel Gauthier
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Publication number: 20090186921Abstract: 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: ApplicationFiled: January 16, 2009Publication date: July 23, 2009Applicant: ACADIA PHARMACEUTICALS, INC.Inventors: Carl-Magnus A. Andersson, Glenn Croston, E. L. Hansen, Allan Kjaersgaard Uldam
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Patent number: 7550486Abstract: 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: GrantFiled: January 11, 2008Date of Patent: June 23, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Soo S. Ko, George V. Delucca
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Patent number: 7541468Abstract: 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: GrantFiled: June 9, 2005Date of Patent: June 2, 2009Assignee: Bristol-Myers Squibb CompanyInventor: Percy H. Carter
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Patent number: 7473779Abstract: 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: GrantFiled: September 12, 2003Date of Patent: January 6, 2009Assignee: 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
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Publication number: 20080293722Abstract: 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: ApplicationFiled: March 15, 2005Publication date: November 27, 2008Applicant: WyethInventors: Robert Zelle, Christopher Todd Baker, Paul Will, Vincent P. Galullo
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Patent number: 7452891Abstract: 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: GrantFiled: January 28, 2005Date of Patent: November 18, 2008Assignee: Schering CorporationInventors: John W. Clader, Hubert B. Josien, Anandan Palani, Tin Yau Chan
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Publication number: 20080261952Abstract: 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: ApplicationFiled: August 16, 2005Publication date: October 23, 2008Inventors: 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
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Publication number: 20080139585Abstract: The present application describes isoindoles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful inhibitors of VEGFR.Type: ApplicationFiled: September 21, 2007Publication date: June 12, 2008Applicant: NOVA SOUTHEASTERN UNIVERSITYInventors: Appu Rathinavelu, Sivanesan Dakshanamurthy, Nagarajan Pattabiraman
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Publication number: 20080132523Abstract: 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: ApplicationFiled: January 11, 2008Publication date: June 5, 2008Inventors: Soo S. Ko, George V. Delucca
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Patent number: 7365070Abstract: 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: GrantFiled: December 4, 2003Date of Patent: April 29, 2008Assignee: Ore Pharmaceuticals Inc.Inventors: Tricia J. Vos, Michael Patane, Michael E. Solomon, Christopher Blackburn, Mihaela D. Danca
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Patent number: 7259157Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.Type: GrantFiled: April 2, 2002Date of Patent: August 21, 2007Assignee: 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
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Patent number: 7214714Abstract: 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: GrantFiled: April 26, 2002Date of Patent: May 8, 2007Assignee: Taisho Pharmaceutical Co. Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Matsunaga, Hideaki Amada
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Patent number: 7074820Abstract: 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: GrantFiled: April 23, 2001Date of Patent: July 11, 2006Assignee: AstraZeneca ABInventor: Thomas Antonsson
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Patent number: 7064210Abstract: 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: GrantFiled: September 29, 2003Date of Patent: June 20, 2006Assignee: Samsung Electronics Co., Ltd.Inventors: Yeon-kyoung Jung, Seung-min Ryu
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Patent number: 6946477Abstract: 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: GrantFiled: November 5, 2002Date of Patent: September 20, 2005Assignee: Sepracor Inc.Inventors: Brian M. Aquila, Gregory D. Cuny, James R. Hauske, Liming Shao, Xinhe Wu
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Patent number: 6919356Abstract: 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: GrantFiled: September 25, 2003Date of Patent: July 19, 2005Assignee: Bristol Myers Squibb CompanyInventor: Douglas G. Batt