Nitrogen Attached Directly Or Indirectly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 549/55)
  • Publication number: 20150025068
    Abstract: A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound.
    Type: Application
    Filed: December 21, 2012
    Publication date: January 22, 2015
    Inventors: Jessica Martinsson, Katarina Faernegardh, Mattias Joensson, Rune Ringom
  • Publication number: 20140235702
    Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having sulfonamido-1-hydroxynaphthalene structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Application
    Filed: October 8, 2012
    Publication date: August 21, 2014
    Inventors: Zaneta Nikolovska-Coleska, Hollis D. Showalter, Chenzhong Liao, Ramzi Mohammad, Fardokht Abulwerdi
  • Publication number: 20140024608
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Application
    Filed: March 14, 2013
    Publication date: January 23, 2014
    Applicant: METHYLGENE INC.
    Inventors: Robert Deziel, Alain Ajamian
  • Patent number: 8574607
    Abstract: Compounds of the formula (I) useful as pesticides are disclosed, wherein the substituents are as defined in claim 1.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: November 5, 2013
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Jürgen Harry Schaetzer, Thomas Pitterna, Long Lu, Yaming Wu, Peter Renold, Francesca Perruccio, Jérome Yves Cassayre, Michel Mueglebach
  • Publication number: 20130289057
    Abstract: The invention relates to N-arylaminomethylenebenzothiophenones of General Formula (I) for use as a drug for the treatment of cardiovascular diseases: wherein E is S, O, or CH2, D is CH or NH, and Ar is a phenyl or naphtyl moiety substituted by an electron-withdrawing group, an unsubstituted heteroaryl residue, or a heteroaryl residue substituted by alkyl or an electron-withdrawing group.
    Type: Application
    Filed: January 12, 2012
    Publication date: October 31, 2013
    Applicants: FORSCHUNGSVERBUND BERLIN E.V., MAX-DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZIN
    Inventors: Enno Klussmann, Walter Rosenthal, Jelena Milic, Martin W. Bergmann
  • Patent number: 8530512
    Abstract: The present invention provides compounds and methods of using of the compounds as anti-infective and anthelminitc agents. In a preferred embodiment, the present invention provides the following compound of Formula III: wherein: R1 is not H when R2 is H and R2 is not H when R1 is H, further wherein R1 is OH or CH(2n+1)O, wherein n is 1-10; R2 is OH or CH(2n+1)O, where n is 1-10; W is alkyl, phenyl, halophenyl, pyridyl, piperidyl, or a substituted or unsubstituted aryl group, including unsubstituted and substituted aromatic heterocycles; and L is an optional linker or linking group selected from O, S, NH, CF2, or CH2, and x=0 or 1, i.e., if x=0, no linking group is present and when x=0, W is not phenyl.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: September 10, 2013
    Inventors: Aaron P. Monte, M. Shahjahan Kabir, Marc A. Rott, William R. Schwan, James M. Cook, III, Jennifer A. Miskowski, Ranjit Verma, Leah Defoe
  • Publication number: 20130172339
    Abstract: A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer.
    Type: Application
    Filed: September 19, 2011
    Publication date: July 4, 2013
    Applicant: KANCERA AB
    Inventors: Styrbjorn Bystrom, Charles Hedgecock, Evert Homan, Thomas Lundback, Jessica Martinsson, Meral Sari, Katarina Farnegardh, Mattias Jonsson
  • Publication number: 20130017491
    Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 17, 2013
    Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Sen Liu, Pushkara R. Varanasi
  • Publication number: 20130017490
    Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 17, 2013
    Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Sen Liu, Pushkara R. Varanasi
  • Publication number: 20130017489
    Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 17, 2013
    Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Sen Liu, Pushkara R. Varanasi
  • Publication number: 20130011789
    Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Sen Liu, Pushkara R. Varanasi
  • Publication number: 20130011788
    Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 10, 2013
    Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Sen Liu, Pushkara R. Varanasi
  • Publication number: 20130011787
    Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 10, 2013
    Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Sen Liu, Pushkara R. Varanasi
  • Publication number: 20130011786
    Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 10, 2013
    Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Sen Liu, Pushkara R. Varanasi
  • Publication number: 20130011790
    Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Sen Liu, Pushkara R. Varanasi
  • Patent number: 8283479
    Abstract: The invention relates to compounds of the formula I: in which R1, R2, X, A, B, D and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.
    Type: Grant
    Filed: April 4, 2011
    Date of Patent: October 9, 2012
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Stephanie Hachtel, Juergen Dedio, Holger Heitsch, Werngard Czechtizky, Sven Grueneberg, Stephen J. Shimshock, Raymond W. Kosley, Jr., Carolina L. Lanter, Hui Li, Rosy Sher, Aleksandra Weichsel
  • Publication number: 20110306614
    Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.
    Type: Application
    Filed: August 19, 2011
    Publication date: December 15, 2011
    Applicants: THE JOHNS HOPKINS UNIVERSITY, CARDIOXYL PHARMACEUTICALS, INC.
    Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
  • Publication number: 20110183259
    Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.
    Type: Application
    Filed: January 25, 2010
    Publication date: July 28, 2011
    Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Sen Liu, Pushkara R. Varanasi
  • Publication number: 20110184177
    Abstract: The invention relates to compounds of the formula I: in which R1, R2, X, A, B, D and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.
    Type: Application
    Filed: April 4, 2011
    Publication date: July 28, 2011
    Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBH
    Inventors: Stephanie Hachtel, Juergen Dedio, Holger Heitsch, Werngard Czechtizky, Sven Grueneberg, Stephen J. Shimshock, Raymond W. Kosley, JR., Carolina L. Lanter, Hui Li, Rosy Sher, Aleksandra Weichsel
  • Publication number: 20110092578
    Abstract: The present invention provides compounds and methods of using of the compounds as anti-infective and anthelminitc agents. In a preferred embodiment, the present invention provides the following compound of Formula III: wherein: R1 is not H when R2 is H and R2 is not H when R1 is H, further wherein R1 is OH or CH(2n+1)O, wherein n is 1-10; R2 is OH or CH(2n+1)O, where n is 1-10; W is alkyl, phenyl, halophenyl, pyridyl, piperidyl, or a substituted or unsubstituted aryl group, including unsubstituted and substituted aromatic heterocycles; and L is an optional linker or linking group selected from O, S, NH, CF2, or CH2, and x=0 or 1, i.e., if x=0, no linking group is present.
    Type: Application
    Filed: December 20, 2010
    Publication date: April 21, 2011
    Inventors: Aaron P. Monte, M. Shahjahan Kabir, Marc A. Rott, William R. Schwan, James M. Cook, III, Jennifer A. Miskowski
  • Patent number: 7655641
    Abstract: The present invention is directed to a compound of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates or stereoisomers thereof, which are useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.
    Type: Grant
    Filed: February 10, 2004
    Date of Patent: February 2, 2010
    Assignee: Eli Lilly and Company
    Inventors: Scott Eugene Conner, Lynn Stacy Gossett, Jonathan Edward Green, Winton Dennis Jones, Jr., Nathan Bryan Mantlo, Donald Paul Matthews, Daniel Ray Mayhugh, Daryl Lynn Smith, Jennifer Ann Vance, Xiaodong Wang, Alan M Warshawsky, Leonard Larry Winneroski, Jr., Yanping Xu, Guoxin Zhu
  • Publication number: 20090227667
    Abstract: Compounds of Formula (I), are provided where T is CHO, COR8, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y=C, or substituted diene fused to Y when Y=C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.
    Type: Application
    Filed: May 5, 2009
    Publication date: September 10, 2009
    Applicant: Wyeth
    Inventors: Anthony Frank Kreft, Lynn Resnick, Scott Christian Mayer, George Diamantidis, Derek Cecil Cole, Boyd Lynn Harrison, Minsheng Zhang, Molly Hoke, Tingzhong Wang, Rocco John Galante
  • Publication number: 20090227625
    Abstract: The invention relates to compounds of the formula I in which R1, R2, X, A, B, Z and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.
    Type: Application
    Filed: December 17, 2008
    Publication date: September 10, 2009
    Applicant: sanofi-aventis
    Inventors: Stephanie HACHTEL, Juergen DEDIO, Elisabeth DeFOSSA, Sven GRUENEBERG, Holger HEITSCH, William BOCK, Charlie CHEN, Raymond KOSLEY, Chung-Yi KUNG, Marcel PATEK, Rosy SHER, Stephen SHIMSHOCK, Aleksandra WEICHSEL
  • Patent number: 7582673
    Abstract: Embodiments of the present invention provide bissulfonamide compounds that are agonists of GalR1. The present invention further provides compositions comprising bissulfonamide compounds that are agonists of GalR1, and methods of use of such compounds and compositions.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: September 1, 2009
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Adnan M. M. Mjalli, Bapu Gaddam, Mohan Rao, Muralidhar Bondlela, Ramesh Gopalaswamy, Robert C. Andrews, Stephen Davis, Suvi Simila, Tan Ren
  • Publication number: 20090192213
    Abstract: The present invention relates to benzo[b]furane and benzo[b]thiophene derivatives of the general formula IV as the free base or salts thereof and their use.
    Type: Application
    Filed: February 20, 2009
    Publication date: July 30, 2009
    Applicant: H. Lundbeck A/S
    Inventors: Jan Kehler, Karsten Juhl, Morten Bang Norgaard
  • Publication number: 20090163547
    Abstract: The present invention makes reference to new indene derivatives with general formula (I), as well as to their preparation procedures, their application as medicament and the pharmaceutical compositions containing them. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.
    Type: Application
    Filed: November 7, 2006
    Publication date: June 25, 2009
    Inventors: Maria De Las Ermitas Alcalde-Pais, Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal, Maria De Les Neus Mesquida-Estevez, Sara Lopez-Perez
  • Patent number: 7417066
    Abstract: The invention relates to compounds of general Formula I, the production thereof, and the use thereof as a medicinal product.
    Type: Grant
    Filed: June 7, 2006
    Date of Patent: August 26, 2008
    Assignee: Schering AG
    Inventors: Bernd Buchmann, Martin Fritsch, Duy Nguyen, Bernd Menzenbach, Ulf Boemer
  • Publication number: 20080146623
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Application
    Filed: December 18, 2007
    Publication date: June 19, 2008
    Applicant: METHYLGENE INC.
    Inventors: Robert Deziel, Alain Ajamian
  • Patent number: 7282595
    Abstract: The present invention provides antitumor compounds of the formula (I); and antitumor methods.
    Type: Grant
    Filed: November 13, 2003
    Date of Patent: October 16, 2007
    Assignee: Eli Lilly and Company
    Inventors: Mary Margaret Mader, Luisa Maria Martin-Cabrejas, Michael Enrico Richett
  • Patent number: 7217723
    Abstract: The present invention provides a compound that has an excellent inhibitory activity on STAT6 activation and is effective against allergic diseases, and a medicinal composition thereof. According to the present invention, disclosed is the compound represented by the General Formula (I) [where R1 and R2 independently represent a C1-6 alkyl group and the like that may have a hydrogen atom or a substituent; R3 represents a C1-6 alkyl group and the like that may have a substituent; R4 and R5 independent represents a hydrogen atom or a C1-6 alkyl group and the like that may have a substituent; R6 represents a hydrogen atom and the like; W represents —SO2—and the like; and X represents a sulphur atom and the like.] or a salt thereof, or a hydrate thereof.
    Type: Grant
    Filed: February 2, 2005
    Date of Patent: May 15, 2007
    Assignee: Eisai Co., Ltd.
    Inventors: Ichiro Yoshida, Shuichi Suzuki
  • Patent number: 7179896
    Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.
    Type: Grant
    Filed: July 15, 2005
    Date of Patent: February 20, 2007
    Assignee: Panagene, Inc.
    Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
  • Patent number: 7157454
    Abstract: The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B1 receptors; they may be used for the preparation of medicinal products intended for treating or preventing inflammation pathologies and persistent or chronic inflammatory diseases.
    Type: Grant
    Filed: March 27, 2002
    Date of Patent: January 2, 2007
    Assignee: Sanofi-Aventis
    Inventors: Bernard Ferrari, Jean Gougat, Yvette Muneaux, Pierre Perreaut, Lionel Sarran
  • Patent number: 7148240
    Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular system.
    Type: Grant
    Filed: August 23, 2001
    Date of Patent: December 12, 2006
    Assignee: Sanofi-Aventis
    Inventors: Jean-Louis Assens, Claude Bernhart, Frédérique Cabanel-Haudricourt, Dino Nisato
  • Patent number: 7126012
    Abstract: The invention concerns compounds of formula (I): R-A-R? wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R? represents a —(CH2)t-R5 group wherein t and R5 are as defined in the description
    Type: Grant
    Filed: September 23, 2004
    Date of Patent: October 24, 2006
    Assignee: Les Laboratoires Servier
    Inventors: Daniel Lesieur, Frederique Klupsch, Gerald Guillaumet, Marie-Claude Viaud, Michel Langlois, Caroline Bennejean, Pierre Renaud, Philippe Delagrange
  • Patent number: 7071225
    Abstract: Arylaminopropane analogues are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.
    Type: Grant
    Filed: November 26, 2003
    Date of Patent: July 4, 2006
    Assignee: Alcon, Inc.
    Inventors: Mark R. Hellberg, Abdelmoula Namil
  • Patent number: 7019024
    Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: March 28, 2006
    Assignee: Allelix Neuroscience Inc.
    Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
  • Patent number: 6969766
    Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.
    Type: Grant
    Filed: April 25, 2003
    Date of Patent: November 29, 2005
    Assignee: Panagene, Inc.
    Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
  • Patent number: 6861444
    Abstract: Compounds of the general formula (I): or a salt thereof, wherein R1 is hydrogen, hydroxyl or halogen; R2 is NHSO2CH3, SO2NHCH3 or the like; R5 and R6 each independently is hydrogen, C1-6 alkyl, optionally substituted phenyl or optionally substituted benzyl; X is NH, sulfur, oxygen or methylene; Y is oxygen, NR7, sulfur, methylene or a bond; and * represents an asymmetric carbon atom. The compounds are useful as a medicine for treating or preventing diabetes, obesity, hyperlipidemia, digestive diseases, depression or urinary disturbances.
    Type: Grant
    Filed: April 25, 2001
    Date of Patent: March 1, 2005
    Assignee: Asahi Kasei Pharma Corporation
    Inventors: Shunichi Ikuta, Shiro Miyoshi, Kohei Ogawa
  • Publication number: 20040223909
    Abstract: A method for assessing levels of soluble A-beta as an indicator of Alzheimer's disease, and other amyloid-related diseases, in vitro, ex vivo, in vivo, and in situ which employs an imaging agent binds specifically to soluble A-beta and is labeled for detection.
    Type: Application
    Filed: December 26, 2003
    Publication date: November 11, 2004
    Inventors: Michael Christopher Montalto, Eric Dustin Agdeppa, Tiberiu Mircea Siclovan, Amy Casey Williams
  • Publication number: 20040225006
    Abstract: Compounds of formula (I) wherein R is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl or heterocyclyl; and R1 is bicyclyl or heterobicyclyl; are useful in the treatment and prophylaxis of conditions mediated by s-CD23 or TNF.
    Type: Application
    Filed: May 14, 2004
    Publication date: November 11, 2004
    Applicant: SmithKline Beecham p.l.c.
    Inventors: Gordon Bruton, Andrew Faller, Barry Sidney Orlek, Kishore Kalidas Rana, Graham Walker
  • Publication number: 20040176435
    Abstract: There is provided a heretoaryloxy 3-substituted propanamine compound of formula (I): wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents selected from halo, C1-C4 alkyl and C1-C4 alkoxy, and thienyl optionally substituted with up to 3 substituents selected from halo and C1-C4 alkyl; Y is selected from benzothienyl, indolyl and benzofuranyl, optionally substituted with up to 5 substituents selected from halo, C1-C4 alkyl, C1-C4 alkoxy, nitro, acetyl and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: October 23, 2003
    Publication date: September 9, 2004
    Inventors: Peter Gallagher, Richard Edmund Rathmell, Maria Ann Fagan
  • Publication number: 20040127546
    Abstract: Compounds of the general formula (I): 1
    Type: Application
    Filed: January 22, 2004
    Publication date: July 1, 2004
    Applicant: ASAHI KASEI PHARMA CORPORATION
    Inventors: Shunichi Ikuta, Shiro Miyoshi, Kohei Ogawa
  • Publication number: 20040110791
    Abstract: Arylaminopropane analogues are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.
    Type: Application
    Filed: November 26, 2003
    Publication date: June 10, 2004
    Inventors: Mark R. Hellberg, Abdelmoula Namil
  • Patent number: 6723848
    Abstract: Process for the preparation of benzo-fused heterocycles of general formula I: in which X, R1, R2, R3, R4, R5 and n are as defined in claim 1, by reacting tetrahydrobenzo-fused heterocycles of formula II: in which X, R1, R2, R3, R4, R5, n and Ac are as defined in claim 1, with a catalytic amount of a noble metal catalyst in the presence of a hydrogen acceptor and then deacylating the acylated amino group by the addition of an amine.
    Type: Grant
    Filed: October 9, 2002
    Date of Patent: April 20, 2004
    Assignee: Merck Patent Gesellschaft mit Beschränkter Haftung
    Inventors: Frank-Hardi Wartenberg, Thomas Koppe, Walter Wetzel, Markus Wydra, Achim Benz
  • Patent number: 6710071
    Abstract: This invention relates to a series of difluoromethylene aromatic ethers of the formula wherein ring A and X and Y are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.
    Type: Grant
    Filed: August 15, 2002
    Date of Patent: March 23, 2004
    Assignee: Pfizer Inc
    Inventor: John Adams Lowe, III
  • Publication number: 20040044224
    Abstract: The present invention relates to a one pot process for preparing a compound of formula I: I; from a compound of formula II and III: I; III.
    Type: Application
    Filed: September 2, 2003
    Publication date: March 4, 2004
    Inventors: Preston Charles Conrad, John Paul Gardner
  • Patent number: 6699860
    Abstract: This invention is related to novel di-substituted aminomethyl chroman derivatives which are useful in the treatment of beta-3 receptor-mediated conditions.
    Type: Grant
    Filed: December 7, 2001
    Date of Patent: March 2, 2004
    Assignee: Bayer Pharmaceuticals Corporation
    Inventors: Gaetan H. Ladouceur, William H. Bullock, Steven R. Magnuson, Stephen J. O'Connor, Roger A. Smith, Quanrong Shen, Qingjie Liu, Ning Su, Emil J. Velthuisen, Ann-Marie Campbell, Paul P. Ehrlich
  • Publication number: 20040010029
    Abstract: This invention discloses and claims a new class of indole derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cell lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. It has now been found that the compounds of this invention are capable of modulating T helper (Th) cells, Th1/Th2, and thereby capable of inhibiting the transcription of interleukin-4 (IL-4) message, IL-4 release or IL-4 production.
    Type: Application
    Filed: April 23, 2003
    Publication date: January 15, 2004
    Inventors: Gregory H. Merriman, Philip M. Weintraub, Jeffrey S. Sabol, Ramalinga M. Dharanipragada, Nicholas J. Hrib, John G. Jurcak, Alexandre Gross, Brian Whiteley, Kwon Yon Musick, Joseph T. Klein
  • Publication number: 20030220367
    Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented.
    Type: Application
    Filed: May 9, 2003
    Publication date: November 27, 2003
    Inventors: Richard Leo Cournoyer, Paul Francis Keitz, Lee Edwin Lowrie, Alexander Victor Muehldorf, Counde O'Yang, Dennis Mitsugu Yasuda
  • Publication number: 20030199702
    Abstract: The present invention provides an efficient process for the preparation of benzothiophenecarboxamide PGD2 antagonist, S-5751.
    Type: Application
    Filed: June 6, 2003
    Publication date: October 23, 2003
    Inventors: Robert Larsen, Dongwei Cai, Michel Journet, Kevin Campos