Plural Ring Chalcogens In The Polycyclo Ring Sytem (e.g., Methylenedioxyphenyl Containing, Etc.) Patents (Class 548/526)
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Patent number: 7897635Abstract: Compounds useful for inhibiting HIV protease are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating wild-type HIV and of multidrug-resistant strains of HIV, also are disclosed.Type: GrantFiled: November 7, 2006Date of Patent: March 1, 2011Assignee: The Board of Trustees of the University of IllinoisInventors: Arun K. Ghosh, Geoffrey M. Bilcer, Thippeswamy Devasamudram
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Publication number: 20110028476Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof.Type: ApplicationFiled: September 1, 2010Publication date: February 3, 2011Inventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
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Publication number: 20110003987Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.Type: ApplicationFiled: July 6, 2010Publication date: January 6, 2011Inventors: Bradford H. Hirth, Craig Siegel
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TETRACYCLIC DIPYRANO-COUMARIN COMPOUNDS WITH ANTI-HIV AND ANTI-MYCOBACTERIUM TUBERCULOSIS ACTIVITIES
Publication number: 20100324067Abstract: The present invention relates to tetracyclodipyrano-coumarin compounds of general formula (I), wherein the substituents are defined herein. These compounds exihibit dual biological activities of anti human immunodeficiency virus type 1 (HIV-1) infection and anti-Mycobacterium Tuberculosis (TB) infection.Type: ApplicationFiled: November 5, 2007Publication date: December 23, 2010Inventors: Gang Liu, Hai Xue, Tao Ma, Ziwei Chen, Lin Wang -
Patent number: 7834001Abstract: Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidino carbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.Type: GrantFiled: November 8, 2005Date of Patent: November 16, 2010Assignee: Piramal Life Sciences LimitedInventors: Bansi Lal, Swati Bal-Tembe, Usha Ghosh, Arun Kumar Jain, Tulsidas More
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Publication number: 20100256216Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 30, 2008Publication date: October 7, 2010Inventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
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Patent number: 7803836Abstract: The present invention concerns substituted aminophenylsulfonamide compounds and derivatives, their use as protease inhibitors, in particular as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present substituted aminophenylsulfonamide compounds and derivatives with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.Type: GrantFiled: November 28, 2006Date of Patent: September 28, 2010Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Herman Augustinus De Kock, Tim Hugo Maria Jonckers, Stefaan Julien Last, Paul Jozef Gabriel Maria Boonants, Dominique Louis Nestor Ghislain Surleraux, Piet Tom Bert Paul Wigerinck
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Publication number: 20100216813Abstract: The present invention relates to a compound represented by the following formula I or a pharmaceutically acceptable salt thereof; wherein R1, R2, and y are defined herein. The present invention further relates to compositions that include the compound of the present invention as well as a method of treating a patient from endometreosis or uterine fibroids.Type: ApplicationFiled: November 29, 2006Publication date: August 26, 2010Inventor: James S. Frazee
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Publication number: 20100216806Abstract: Compounds of formula are HDAC inhibitors. These compounds are useful for the treatment of diseases such as cancer in humans or animals.Type: ApplicationFiled: February 19, 2010Publication date: August 26, 2010Inventors: Chungen Liang, Guozhi Tang, Jason Christopher Wong, Xihan Wu, Zhenshan Zhang
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Patent number: 7763738Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.Type: GrantFiled: August 24, 2007Date of Patent: July 27, 2010Assignee: Genzyme CorporationInventors: Bradford H. Hirth, Craig Siegel
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Publication number: 20100173905Abstract: The invention discloses a new use of a class of heptacyclic compounds in the preparation of formulations for the prevention and treatment of diabetes and metabolic syndromes; the present invention also discloses a new class of heptacyclic compounds; the present invention also discloses a process for preparing the heptacyclic compounds and a composition containing the same. The heptacyclic compounds of the present invention can be used to effectively preventing or treating diseases such as diabetes and metabolic syndromes.Type: ApplicationFiled: May 29, 2007Publication date: July 8, 2010Inventors: Jianhua Shen, Ying Leng, Hualiang Jiang, Junhua Chen
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Publication number: 20100168088Abstract: The present invention relates to a compound of formula I wherein Ar1, Ar2, R1, R2, R3, n, o, and p are as described herein or to a pharmaceutically active salt, to all stereoisomeric forms, including individual diastereoisomers and enantiomers as well as to racemic and non-racemic mixtures thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: October 2, 2009Publication date: July 1, 2010Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Matthias Nettekoven, Angélique Patiny-Adam, Hasane Ratni, Claus Riemer
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Patent number: 7745481Abstract: Certain cyclooxygenase-2 inhibitors are useful for the treatment and prevention of tumors and tumor-related disorders and cachexia.Type: GrantFiled: August 13, 2004Date of Patent: June 29, 2010Assignee: Daiichi Sankyo Company, LimitedInventors: Shinichi Kurakata, Masaharu Hanai, Saori Kanai, Tomio Kimura
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Publication number: 20100120760Abstract: A compound of the formula (I): as defined herein, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing a compound of the formula (I) for use in inhibiting hepatitis C virus polymerase and/or of treating or preventing an illness due to hepatitis C virus,Type: ApplicationFiled: March 25, 2008Publication date: May 13, 2010Applicant: ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGInventors: Uwe Koch, Angela Claire Mackay, Frank Narjes, Ian Stansfield
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Patent number: 7678904Abstract: The present invention provides compounds of the formula (I) wherein: X1, X2 and X3 are heteroatoms; R4, R5, R6, R7, R8, R9 and R10 are independently selected from H, halo, —OH, —NO2, —CN and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and Z is optionally substituted C1-8 straight-chained or branched aliphatic, optionally containing 1 or more double or triple bonds, wherein one or more carbons are optionally replaced by R* wherein R* is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; an amino acid residue, H, —CN, —C(O)—, —C(O)C(O)—, —C(O)NR1—, —C(O)NR1NR2—, —C(O)O—, —OC(O)—, —NR1CO2—, —O—, —NR1C(O)NR2—, —OC(O)NR1—, —NR1NR2—, —NR1C(O)—, —S—, —SO—, —SO2—, —NR1—, —SO2NR1—, —NR1R2, or —NR1SO2—, wherein R1 and R2 are independently selected from H and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or where R* is NR1R2, R1 and R2 optionally together with the nitrogen atom form an optionally substituted 5-12 meType: GrantFiled: January 7, 2005Date of Patent: March 16, 2010Assignee: University of KentuckyInventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
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Publication number: 20100035849Abstract: The present invention provides novel methylenedioxy phenolic compounds and their derivatives, methods of making them and methods of using them to treat or prevent cardiovascular disease, vascular disease and/or inflammatory disease, as well as Type I and Type II Diabetes and Dyslipidemia patients at risk for hypertension, stroke, cardiovascular and renal disease.Type: ApplicationFiled: August 5, 2009Publication date: February 11, 2010Applicants: OHIO STATE UNIVERSITY RESEARCH FOUNDATION, INVASC THERAPEUTICS, INC.Inventors: Sampath Parthasarathy, Sanjay Rajagopalan, Desikan Rajagopal
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Patent number: 7652060Abstract: This invention relates to neurotrophic compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.Type: GrantFiled: October 12, 2007Date of Patent: January 26, 2010Assignee: Glia Med, IncInventors: Gregory S. Hamilton, Joseph P. Steiner
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Patent number: 7645789Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: October 18, 2007Date of Patent: January 12, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Djamel Numa
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Publication number: 20090298881Abstract: Water-soluble artemisinin derivatives, their preparation methods, the pharmaceutical compositions containing the same derivatives and the use thereof are disclosed. The artemisinin derivatives have following formula I. It has been proved by pharmacological tests that these compounds and compositions have evident immuno-suppressive activities, and may be used in the preparation of novel immuno-suppressants for treating the diseases caused by hyperfunction of human immunity (e.g. the auto-immune diseases such as lupus erythematosus, rheumatoid arthritis, multiple sclerosis and the like), and for inhibiting the graft rejection after cell or organ transplantation.Type: ApplicationFiled: July 20, 2006Publication date: December 3, 2009Inventors: Ying Li, Jianping Zuo, Zhongshun Yang, Junxia Wang, Yu Zhang, Wei Tang, Jianxin Zhang
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Patent number: 7615573Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.Type: GrantFiled: February 5, 2007Date of Patent: November 10, 2009Assignees: The Regents of the University of Michigan, Genzyme CorporationInventors: Craig Siegel, James A. Shayman, Carol A. Nelson, David J. Harris, Diane P. Copeland
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Patent number: 7608592Abstract: The present invention is directed to compounds that are antiviral agents. Specifically the compounds of the present invention inhibit replication of HCV and are therefore useful in treating hepatitis C infections. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: GrantFiled: June 28, 2006Date of Patent: October 27, 2009Assignee: ViroBay, Inc.Inventors: Michael Graupe, John O. Link, Chandrasekar Venkataramani
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Publication number: 20090253684Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, COPD.Type: ApplicationFiled: December 2, 2008Publication date: October 8, 2009Inventors: Romyr Dominique, Robert Alan Goodnow, JR., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
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Publication number: 20090220662Abstract: The present invention provides isosorbide derivatives having the formula shown below and certain subgenera or species thereof, as flavor or taste modifiers, particularly, savory (“umami”) taste modifiers, savory flavoring agents and savory flavor enhancers in foods, beverages, and other comestible compositions,Type: ApplicationFiled: March 3, 2009Publication date: September 3, 2009Inventors: Catherine TACHDJIAN, Donald S. Karanewsky, Sara L. Adamski-Werner, Jeffrey M. Yamamoto, Guy Servant
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Publication number: 20090069402Abstract: The present application describes deuterium-enriched atrasentan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 21, 2008Publication date: March 12, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090047224Abstract: The present invention relates to the use of at least one compound capable of cleaving the diketone crosslinking bonds between two proteins, in a composition applied topically to the skin, as an agent for preventing or treating the signs of ageing of the skin or the orange-peel appearance. The above compound is preferably a N-hydroxy imide of formula (I). These N-hydroxy imides have inhibitory properties on the glycation of proteins and also antioxidant properties. The invention also relates to novel N-hydroxy imides included in formula (I) above.Type: ApplicationFiled: November 8, 2004Publication date: February 19, 2009Applicant: L'OREALInventors: Maria Dalko, Herve Pageon
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Patent number: 7465751Abstract: This invention generally relates to the derivatives of 1-substituted-3-pyrroli dines having the structure of Formula (I): The compounds of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of the compounds of the present invention. pharmaceutical compositions containing the compounds of the present invention and the methods for treating the diseases mediated through muscarinic receptors.Type: GrantFiled: December 23, 2002Date of Patent: December 16, 2008Assignee: Ranbaxy Laboratories LimitedInventors: Anita Mehta, Jang Bahadur Gupta, Pakala Kumara Savithru Sarma
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Publication number: 20080306061Abstract: The present invention concerns substituted aminophenylsulfonamide compounds and derivatives, their use as protease inhibitors, in particular as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present substituted aminophenylsulfonamide compounds and derivatives with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.Type: ApplicationFiled: November 28, 2006Publication date: December 11, 2008Inventors: Herman Augustinus De Kock, Tim Hugo Maria Jonckers, Stefaan Julien Last, Paul Jozef Gabriel Maria Boonants, Dominique Louis Nestor Ghislain Surleraux, Piet Tom Bert Paul Wigerinck
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Publication number: 20080300254Abstract: Compounds of Formula I are described: preferably subject to the proviso that either (a) R2 and R3 together form —O—CH(R10)—O—, or (b) R5 and R6 together form —O—CH(R10)—O—, wherein R10 is H, halo, or loweralkyl. Pharmaceutical salts, formulations, and methods of using the same in the treatment of cancer are also described.Type: ApplicationFiled: December 20, 2006Publication date: December 4, 2008Inventors: Kuo-Hsiung Lee, Linyi Wei, Kenneth F. Bastow, Arnold Brossi, Tian-Shung Wu
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Patent number: 7452999Abstract: Improved processes for preparing intermediates useful for preparing antibacterial N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl}-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, which have one or more of the following features: (1) make use of a particular ?-lactam intermediate; (2) which make use of a particular resolving agents, enantiomerically pure substituted propionic acids, especially (R)-2-butyl-3-hydroxy-propionic acid; (3) which avoid the use of hydrogen peroxide; and (4) which facilitate selective debenzylation reducing production of waste by-products.Type: GrantFiled: February 20, 2004Date of Patent: November 18, 2008Assignee: Novartis AGInventors: Mahavir Prashad, Hong-Yong Kim, Bin Hu, Joel Slade, Prasad Koteswara Kapa, Michael John Girgis
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Publication number: 20080274082Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 24, 2008Publication date: November 6, 2008Inventors: Yonghua Gai, Ying Sun, Yat Sun Or, Zhe Wang
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Publication number: 20080214648Abstract: The present invention provides new prodrugs which are conjugates of a therapeutic compound and a peptide wherein the conjugate is cleavable by dipeptidyl-peptidases, more preferably by CD26, also known as DPPIV (dipeptidyl aminodipeptidase IV).Type: ApplicationFiled: May 10, 2004Publication date: September 4, 2008Inventors: Herman Augustinus De Kock, Piet Tom Bert Paul Wigerinck, Jan Balzarini
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Publication number: 20080176864Abstract: The present invention provides a compound of the Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly frailty, osteoporosis, osteopenia, and male and female sexual dysfunction comprising administering to a patient in need thereof an effective amount of a compound of Formula (I).Type: ApplicationFiled: May 10, 2006Publication date: July 24, 2008Inventors: Konstantinos Gavardinas, Prabhakar Kondaji Jadhav, Douglas Richard Stack, Ian Roger Clemens
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Publication number: 20080139625Abstract: Formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogType: ApplicationFiled: April 29, 2005Publication date: June 12, 2008Inventors: Libuse Jaroskova, Joannes Theodorus Maria Linders, Christophe Francis Robert Nestor Buyck, Louis Jozef Elizabeth Van Der Veken, Vladimir Dimichev Dimitrov, Theo Teofanov Nikiforov
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Patent number: 7378436Abstract: A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R1 is H, C1-6alkyl, —C(X)Y, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R2 is aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R3 is C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy —C1-6alkyl and C1-4alkyl-S—C1-4alkyl; X is S oType: GrantFiled: June 17, 2004Date of Patent: May 27, 2008Assignee: Pfizer Inc.Inventors: Paul Vincent Fish, Michael Jonathan Fray, Alan Stobie, Florian Wakenhut, Gavin Alistair Whitlock, Mark David Andrews, Alan Daniel Brown, Mark Ian Lansdell
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Patent number: 7378419Abstract: The invention relates to compounds of formula (I), wherein R1 is a group selected from hydrogen, alkyl, aryl, aryalkil, heteroaryl, heteroarylalkyl, alkylcarbonyl, arylcarbonyl, arylalkylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, arylalkoxycarbonyl, heterocycloalkoxycarbonyl, alkylsulfonyl, arylsulfonyl, arylalkylsulfonyl, phosphonic and Si(Ra)2Rb, Y is a group selected from HN—NH and N—R2, R3 is a hydrogen atom, an alkyl, cycloalkyl, aryl, arylalkyl group, R4 is hydrogen atom or an alkyl group, enantiomers, diastereoisomers and the salts thereofType: GrantFiled: September 1, 2004Date of Patent: May 27, 2008Assignees: Les Laboratoires Servier, Centre National de la Recherche Scientifique (CNRS)Inventors: Claude Monneret, Daniel Dauzonne, John Hickman, Alain Pierre, Laurence Kraus-Berthier, Bruno Pfeiffer, Pierre Benard
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Patent number: 7365093Abstract: A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.Type: GrantFiled: February 23, 2005Date of Patent: April 29, 2008Assignee: Abbott LaboratoriesInventors: Martin Winn, Steven A. Boyd, Charles W. Hutchins, Hwan-Soo Jae, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Bryan K. Sorensen, Bruce G. Szczepankiewicz, Kenneth J. Henry, Gang Liu, Steven J. Wittenberger, Steven A. King
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Patent number: 7342114Abstract: 4-O esters of podophyllotoxin and 4?-demethylepipodophyllotoxin are provided. The compounds are 4-O esters of an alkanoic acid or substituted alkanoic acid and podophyllotoxin and 4?-demethylepipodophyllotoxin. The compounds are useful for treating cancer.Type: GrantFiled: July 1, 2003Date of Patent: March 11, 2008Assignees: California Pacific Medical Center, Catholic Healthcare West, DBA St. Mary's Medical CenterInventor: Li-Xi Yang
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Patent number: 7329654Abstract: The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders mediated by one or more estrogen receptors and processes for their preparation. The compounds of the invention are useful in the treatment and/or prevention of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.Type: GrantFiled: December 2, 2002Date of Patent: February 12, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Ramesh M. Kanojia, Nareshkumar F. Jain, Raymond Ng, Zhihua Sui, Jiayi Xu
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Patent number: 7312242Abstract: Compounds of the formula having anti-tumor activity, wherein R1 and R2 are as described hereinType: GrantFiled: July 9, 2004Date of Patent: December 25, 2007Assignee: University of KentuckyInventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
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Patent number: 7265228Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.Type: GrantFiled: August 12, 2004Date of Patent: September 4, 2007Assignee: Genzyme CorporationInventors: Bradford H. Hirth, Craig Siegel
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Patent number: 7208512Abstract: The present invention provides benzodifuran imidazoline derivatives and benzofuran imidazoline derivatives for lowering intraocular pressure and providing ocular neuroprotection.Type: GrantFiled: December 9, 2002Date of Patent: April 24, 2007Assignee: Alcon, Inc.Inventors: Zixia Feng, Mark R. Hellberg
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Patent number: 7196205Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.Type: GrantFiled: March 28, 2005Date of Patent: March 27, 2007Assignees: The Regents of the University of Michigan, Genzyme CorporationInventors: Craig Siegel, James A. Shayman, Carol A. Nelson, David J. Harris, Diane P. Copeland
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Patent number: 7186722Abstract: Novel ?1-pyrrolines of the Formula (I) in which R1, R2, R3 and Het have the meanings given in the description, a plurality of processes for preparing these compounds and their use for controlling pests, and also novel intermediates and processes for their preparation.Type: GrantFiled: January 31, 2002Date of Patent: March 6, 2007Assignee: Bayer Cropscience AGInventors: Andrew Plant, Rüdiger Fischer, Thomas Seitz, Christoph Erdelen, Andreas Turberg, Olaf Hansen
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Patent number: 7169907Abstract: Compounds including haptens, intermediates, and immunogens that are useful in the production of antibodies specific for the methylenedioxy class of amphetamine derivatives are described. Antibodies specific for the methylenedioxy class of amphetamine derivatives, reagent kits containing antibodies specific for the methylenedioxy class of amphetamine derivatives, methods of producing antibodies specific for the methylenedioxy class of amphetamine derivatives, and methods of detecting analytes including members of the methylenedioxy class of amphetamine derivatives are also described.Type: GrantFiled: March 1, 2002Date of Patent: January 30, 2007Assignee: Roche Diagnostics Operations, Inc.Inventor: Raymond A. Hui
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Patent number: 7160877Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower-alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.Type: GrantFiled: June 22, 2004Date of Patent: January 9, 2007Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
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Patent number: 7157124Abstract: A compound represented by formula (1) or (2) and a polymer obtained by polymerizing the compound are provided: wherein Ra is one of the groups represented by Formulas (3-1) to (3-5); Rb is hydrogen, halogen, or a side chain such as —CN, —NCO, —NCS or alkyl having a carbon number of 1 to 20; A is a cyclic diyl group such as 1,4-cyclohexylene, 1,4-cyclohexenylene, 1,4-phenylene, naphthalene-2,6-diyl, tetrahydronaphthalene-2,6-diyl, fluorene-2,7-diyl, bicyclo[2.2.2]oct-1,4-diyl or bicyclo[3.1.0]hex-3,6-diyl, wherein at least one A is substituted 1,4-phenylene represented by Formula (4-1) or (4-2); Z is a single bond or a bonding group such as alkylene having a carbon number of 1 to 20; Rc is hydrogen, halogen, —CF3 or alkyl having a carbon number of 1 to 5; m is an integer of 1 to 6, and q is 0 or 1.Type: GrantFiled: January 5, 2004Date of Patent: January 2, 2007Assignees: Chisso Petrochemical Corporation, Chisso CorporationInventors: Yasuyuki Sasada, Kazuhiko Saigusa
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Patent number: 7148242Abstract: N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl]-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes or imidazacyclo4-7alkanes have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by peptidyl deformylase inhibitors such as treatment of bacterial infections.Type: GrantFiled: June 14, 2002Date of Patent: December 12, 2006Assignee: Novartis AGInventors: Jeffrey Jacobs, Rakesh K. Jain, Dinesh V. Patel, Zhengyu Yuan
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Patent number: 7138426Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.Type: GrantFiled: April 18, 2003Date of Patent: November 21, 2006Assignee: Merck & Co., Inc.Inventors: Frank P. DiNinno, Timothy Allen Blizzard, Jerry Dwain Morgan, II
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Patent number: 7060725Abstract: The present invention is directed to novel compounds of the formula (I) wherein X, R1, R2, R3, R4, R5 and R6 are as described in the specification, processes for the preparation of and pharmaceutical compositions comprising said derivatives. The compounds of the present invention are useful for the treatment of epilepsy. The invention is further directed to a process for the preparation of compounds of formula (XX), wherein X, R3, R4, R5 and R6 are as described in the specification.Type: GrantFiled: May 8, 2003Date of Patent: June 13, 2006Assignee: Janssen Pharmaceutica N.V.Inventors: Ahmed Abdel-Magid, Cynthia Maryanoff, Steven Mehrman, Kirk Sorgi, Frank Villani, Cheryl Kordik, Allen B. Reitz, Bruce Maryanoff
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Patent number: RE39420Abstract: Compounds of formula (I) and (II): [wherein R is hydrogen, halogen or alkyl; R1 is alkyl, amino or substituted amino; R2 is optionally substituted phenyl; R3 is hydrogen, halogen or optionally substituted alkyl; R4 is hydrogen, optionally substituted alkyl, cycloalkyl, aryl, or aralkyl] have valuable analgesic, anti-inflammatory, anti-pyretic and anti-allergic activities and have the ability to inhibit the production of leukotrienes and to inhibit bone resorption. They are relatively free from the side effects which generally result from the administration of compounds having these kinds of activities.Type: GrantFiled: September 29, 2000Date of Patent: December 5, 2006Assignee: Sankyo Company, LimitedInventors: Tomio Kimura, Yasuo Noguchi, Akira Nakao, Keisuke Suzuki, Shigeru Ushiyama, Akihiro Kawara, Masaaki Miyamoto