Phosphorus Attached Directly Or Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 540/542)
  • Patent number: 10913767
    Abstract: This invention relates to an oligonucleotide comprising one or more abasic nucleoside monomers of formula V: These monomers are useful for modifying of oligonucleotides at one or more positions. This invention also relates to a method of inhibiting the expression of a target gene in a cell. The method comprises contacting the cell with an oligonucleotide having one or more of the above formula (V).
    Type: Grant
    Filed: April 22, 2011
    Date of Patent: February 9, 2021
    Assignee: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Jeremy Lackey, Narayanannair K. Jayaprakash
  • Patent number: 10130627
    Abstract: A pharmaceutical composition includes a pharmaceutical polysaccharide and phenylephrine hydrochloride. The ratio of said polysaccharide to phenylephrine hydrochloride is sufficient to dilute the composition such that phenylephrine hydrochloride is stable at high temperature and humidity.
    Type: Grant
    Filed: June 3, 2015
    Date of Patent: November 20, 2018
    Assignee: GlaxoSmithKine Consumer Healthcare S.A.
    Inventors: Timothy Dungan, Brian Warrington
  • Publication number: 20150037261
    Abstract: The present invention relates to a new class of diazepine-derivatives as chelating agents for paramagnetic metal ions, the process for their preparation, and use of such paramagnetic complexes as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis.
    Type: Application
    Filed: March 13, 2013
    Publication date: February 5, 2015
    Applicant: BRACCO IMAGING S.P.A.
    Inventors: Lorena Beltrami, Luciano Lattuada, Alessandro Maiocchi, Massimo Visigalli, Loredana Sini
  • Publication number: 20140330006
    Abstract: Functionally-modified oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3? and/or 5?-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.
    Type: Application
    Filed: November 15, 2012
    Publication date: November 6, 2014
    Applicant: Sarepta Therapeutics, Inc.
    Inventors: Gunnar J. Hanson, Dwight D. Weller, Bao Zhong Cai, Ming Zhou
  • Publication number: 20140088303
    Abstract: Disclosed is a method for highly efficiently obtaining an optically active alcohol from a carbonyl compound highly enantioselectively. Also disclosed is a ligand used in such a method. Specifically, an optically active alcohol is obtained by reacting a carbonyl compound and an organozinc compound by using a ligand (L) shown below.
    Type: Application
    Filed: November 27, 2013
    Publication date: March 27, 2014
    Applicants: Sekisui Medical Co., Ltd., National University Corporation Nagoya University
    Inventors: Kazuaki ISHIHARA, Manabu HATANO, Takashi MIYAMOTO
  • Publication number: 20140024619
    Abstract: The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein R1 represents a —CO—(CH2)n—COR2 group (wherein n is an integer of 1 to 4, and R2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxol-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.
    Type: Application
    Filed: September 24, 2013
    Publication date: January 23, 2014
    Applicant: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Kazumi KONDO, Yasuhiro MENJO, Takahiro TOMOYASU, Shin MIYAMURA, Yuso TOMOHIRA, Takakuni MATSUDA, Keigo YAMADA, Yusuke KATO
  • Publication number: 20130331358
    Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.
    Type: Application
    Filed: August 12, 2013
    Publication date: December 12, 2013
    Applicant: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Makoto KOMATSU, Fumitaka GOTO, Yasuhiro MENJO, Keigo YAMADA, Takakuni MATSUDA, Yusuke KATO
  • Publication number: 20130274465
    Abstract: Immunopotentiators can be adsorbed to insoluble metal salts, such as aluminium salts, to modify their pharmacokinetics, pharmacodynamics, intramuscular retention time, and/or immunostimulatory effect. Immunopotentiators are modified to introduce a moiety, such as a phosphonate group, which can mediate adsorption. These modified compounds can retain or improve their in vivo immunological activity even when delivered in an adsorbed form.
    Type: Application
    Filed: September 1, 2011
    Publication date: October 17, 2013
    Applicants: IRM LLC, NOVARTIS AG
    Inventors: Manmohan Singh, David A.G. Skibinski, Tom Yao-Hsiang Wu, Yongkai Li, Alex Cortez, Xiaoyue Zhang, Yefen Zou, Timothy Z. Hoffman, Jianfeng Pan, Kathy Yue
  • Publication number: 20130253185
    Abstract: The present invention provides novel compounds and ligands that are useful in transition metal catalyzed cross-coupling reactions. For example, the compounds and ligands of the present invention are useful in palladium or gold catalyzed cross-coupling reactions.
    Type: Application
    Filed: November 17, 2011
    Publication date: September 26, 2013
    Applicant: Dalhousie University
    Inventors: Rylan J. Lundgren, Mark Stradiotto
  • Publication number: 20130165414
    Abstract: Disclosed herein are phosphate esters of noribogaine and dihydronoribogaine, and esters and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the methods of their use, including in the treatment of addiction and/or pain.
    Type: Application
    Filed: December 7, 2012
    Publication date: June 27, 2013
    Applicant: DEMERX, INC.
    Inventor: DemeRx, Inc.
  • Publication number: 20130053346
    Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
    Type: Application
    Filed: August 23, 2012
    Publication date: February 28, 2013
    Applicant: Endo Pharmaceuticals Inc
    Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
  • Publication number: 20130029938
    Abstract: Compounds of Formula I and methods for treating metabolic disorders are disclosed.
    Type: Application
    Filed: April 27, 2011
    Publication date: January 31, 2013
    Applicant: GlaxoSmithKline LLC
    Inventors: Christopher Joseph Aquino, Jon Loren Collins, David John Cowan, Yulin Wu
  • Publication number: 20120276051
    Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.
    Type: Application
    Filed: July 9, 2012
    Publication date: November 1, 2012
    Applicant: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Publication number: 20120277188
    Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.
    Type: Application
    Filed: May 1, 2012
    Publication date: November 1, 2012
    Inventors: Makoto KOMATSU, Fumitaka Goto, Yasuhiro Menjo, Keigo Yamada, Takakuni Matsuda, Yusuke Kato
  • Publication number: 20120277189
    Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.
    Type: Application
    Filed: May 1, 2012
    Publication date: November 1, 2012
    Inventors: Makoto Komatsu, Fumitaka Goto, Yasuhiro Menjo, Keigo Yamada, Takakuni Matsuda, Yusuke Kato
  • Patent number: 8283354
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: August 31, 2005
    Date of Patent: October 9, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Dean Wilson, Andreas Termin, Jesus Gonzalez, Lev Fanning, Timothy Neubert, Paul Krenitsky, Pramod Joshi, Dennis Hurley, Urvi Sheth
  • Publication number: 20120251497
    Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.
    Type: Application
    Filed: April 25, 2012
    Publication date: October 4, 2012
    Inventors: Min Zhong, Leping Li
  • Publication number: 20120214988
    Abstract: Disclosed is a method for highly efficiently obtaining an optically active alcohol from a carbonyl compound highly enantioselectively. Also disclosed is a ligand used in such a method. Specifically, an optically active alcohol is obtained by reacting a carbonyl compound and an organozinc compound by using a ligand (L) shown below.
    Type: Application
    Filed: April 27, 2012
    Publication date: August 23, 2012
    Applicants: Sekisui Medical Co., Ltd., National University Corporation Nagoya University
    Inventors: Kazuaki ISHIHARA, Manabu Hatano, Takashi Miyamoto
  • Publication number: 20120177681
    Abstract: Immunopotentiators can be adsorbed to insoluble metal salts, such as aluminium salts, to modify their pharmacokinetics, pharmacodynamics, intramuscular retention time, and/or immunostimulatory effect. Immunopotentiators are modified to introduce a moiety, such as a phosphonate group, which can mediate adsorption. These modified compounds can retain or improve their in vivo immunological activity even when delivered in an adsorbed form.
    Type: Application
    Filed: September 1, 2011
    Publication date: July 12, 2012
    Inventors: Manmohan Singh, David A.G. Skibinski, Tom Yao-Hsiang Wu, Yongkai Li, Alex Cortez, Xiaoyue Zhang, Yefen Zou, Timothy Z. Hoffman, Jianfeng Pan, Kathy Yue
  • Publication number: 20120116074
    Abstract: The present invention is directed to processes associated with the preparation of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)ethyl]phosphonic acid (perzinfotel).
    Type: Application
    Filed: March 19, 2010
    Publication date: May 10, 2012
    Inventors: Thomas Gerard Cullen, Giuseppe Angelo Miralia, Stefania Sapienza, Machael Joseph O'neill, Jignesh Patel, Rosa Norato, Luisa Borrello
  • Publication number: 20120028926
    Abstract: This invention relates to methods and small molecules having a phosphate group that can be used to inhibit phosphate transport and to treat or prevent diseases that are related to disorders in the maintenance of normal serum phosphate levels.
    Type: Application
    Filed: January 26, 2010
    Publication date: February 2, 2012
    Applicant: CYTOCHROMA INC.
    Inventors: Uttam Saha, Christian F. Helvig, P. Martin Petkovich
  • Publication number: 20110257130
    Abstract: Compounds are provided which can be useful in reducing the activity of an angiotensin-converting enzyme and thus be used to treat or prevent a renin-angiotensin aldosterone system-related disorder. These compounds include lipoic acid derivatives such as prolyl lipoic acid and pipecolinyl lipoic acid, and other compounds, and these compounds are useful in treating hypertension, stroke, or other renin-angiotensin aldosterone system-related disorders in human or animal patients. Pharmaceutical compositions prepared using these compounds and methods of treatment using these compounds are also provided.
    Type: Application
    Filed: October 16, 2009
    Publication date: October 20, 2011
    Inventor: Desikan Rajagopal
  • Publication number: 20110172190
    Abstract: The present invention provides compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells.
    Type: Application
    Filed: November 2, 2010
    Publication date: July 14, 2011
    Inventors: Andrew Robert Marks, Donald W. Landry, Shixian Deng
  • Publication number: 20110098250
    Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.
    Type: Application
    Filed: December 28, 2010
    Publication date: April 28, 2011
    Inventors: Makoto Komatsu, Fumitaka Goto, Yasuhiro Menjo, Keigo Yamada, Takakuni Matsuda, Yusuke Kato
  • Publication number: 20110082110
    Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.
    Type: Application
    Filed: December 13, 2010
    Publication date: April 7, 2011
    Inventors: Makoto Komatsu, Fumitaka Goto, Yasuhiro Menjo, Keigo Yamada, Takakuni Matsuda, Yusuke Kato
  • Publication number: 20110071084
    Abstract: The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein R1 represents a —CO—(CH2)n—COR2 group (wherein n is an integer of 1 to 4, and R2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxo-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.
    Type: Application
    Filed: June 26, 2008
    Publication date: March 24, 2011
    Inventors: Kazumi Kondo, Yasuhiro Menjo, Takahiro Tomoyasu, Shin Miyamura, Yuso Tomohira, Takakuni Matsuda, Keigo Yamada, Yusuke Kato
  • Patent number: 7879825
    Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided where at least one of R2 or R3 is not hydrogen. The compounds of the present invention are N-methyl-D-aspartate (NMDA) receptor antagonists and are useful in treating a variety of conditions present in a mammal that benefit from inhibiting the NMDA receptor.
    Type: Grant
    Filed: June 1, 2007
    Date of Patent: February 1, 2011
    Assignee: Wyeth LLC
    Inventors: Reinhardt B. Baudy, John A. Butera
  • Patent number: 7879826
    Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided: wherein: A is alkylenyl of 1 to 4 carbon atoms, or alkenylenyl of 2 to 4 carbon atoms; R1 and R2 are, independently, hydrogen or a C5 to C7 aryl optionally substituted with 1 to 2 substituents, independently, selected from the group consisting of —C(O)R3, halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy, with the proviso that at least one of R1 and R2 is not hydrogen; R3 is, independently, hydrogen, —OR4, alkyl, aryl, or heteroaryl; R4 is hydrogen, alkyl, aryl, or heteroaryl; R5 and R6 are, independently, hydrogen, alkyl, hydroxyl, alkoxy, or C5 to C7 aryl; wherein any R3 to R6 group having an aryl or heteroaryl moiety can optionally be substituted on the aryl or heteroaryl moiety with 1 to about 5 substituents, independently, selected from the group consisting of halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy.
    Type: Grant
    Filed: June 5, 2007
    Date of Patent: February 1, 2011
    Assignee: Wyeth LLC
    Inventor: Reinhardt Bernhard Baudy
  • Patent number: 7807828
    Abstract: The invention relates to novel compounds and methods of using them for modulating sleep.
    Type: Grant
    Filed: August 10, 2006
    Date of Patent: October 5, 2010
    Assignee: Hypnion, Inc.
    Inventors: Michael Solomon, Dale Edgar, David Hangauer, Kazumi Shiosaki, James White
  • Publication number: 20100210594
    Abstract: The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
    Type: Application
    Filed: July 25, 2008
    Publication date: August 19, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
  • Patent number: 7718658
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: August 31, 2005
    Date of Patent: May 18, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Dean Wilson, Lev Fanning, Paul Krenitsky, Joshua Boger
  • Publication number: 20100112061
    Abstract: A mutual prodrug of a MRA and a (?-agonist for formulation for delivery by aerosolization to inhibit pulmonary bronchoconstriction is described. The mutual prodrug is preferably formulated in a small volume solution (10-500 ?L) dissolved in a quarter normal saline having pH between 5.0 and 7.0 for the treatment of respiratory tract bronchoconstriction by an aerosol having mass median average diameter predominantly between 1 to 5?, produced by nebulization or by dry powder inhaler.
    Type: Application
    Filed: December 12, 2007
    Publication date: May 6, 2010
    Inventors: William Baker, Marcin Stasiak, Sundaramoorthi Swaminathan, Musong Kim
  • Publication number: 20100004206
    Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.
    Type: Application
    Filed: December 22, 2006
    Publication date: January 7, 2010
    Inventors: Makoto Komatsu, Fumitaka Goto, Yasuhiro Menjo, Keigo Yamada, Takakuni Matsuda, Yusuke Kato
  • Publication number: 20090253654
    Abstract: The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g., galantamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as “pro-drugs”, in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. The compounds of this invention may be used as medicaments.
    Type: Application
    Filed: April 13, 2009
    Publication date: October 8, 2009
    Applicant: GALANTOS PHARMA GMBH
    Inventor: Alfred Maelicke
  • Publication number: 20090054689
    Abstract: The present invention provides a production method of an allylic amine represented by the formula (III): wherein R3 is as defined in the specification, which comprises reacting by an allylic alcohol represented by the formula (II): wherein R3 is as defined in the specification, with sulfamic acid, in the presence of a phosphoramidite ligand represented by the formula (I): wherein each symbol is as defined in the specification, and an iridium complex. According to the present invention, a primary allylic amine can be produced directly from an allylic alcohol, without use of an activator for an allylic alcohol and conversion of an allylic alcohol into an activated compound thereof.
    Type: Application
    Filed: March 10, 2008
    Publication date: February 26, 2009
    Applicants: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Erick M. CARREIRA
  • Patent number: 7419969
    Abstract: The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates useful for making the pyrimidone compounds. Additionally, pharmaceutical compositions and methods for treating those infected with HIV are encompassed.
    Type: Grant
    Filed: November 14, 2005
    Date of Patent: September 2, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: B. Narasimhulu Naidu, Timothy P. Connolly, Yasutsugu Ueda
  • Patent number: 7355042
    Abstract: The invention is directed to compositions and methods useful for treating Central Nervous System (CNS) disorders. Furthermore, the invention provides compositions and methods of treating sleep disorders. More specifically, the invention is directed to the compositions and use of derivatized, histamine antagonists for the treatment of sleep disorders.
    Type: Grant
    Filed: April 23, 2004
    Date of Patent: April 8, 2008
    Assignee: Hypnion, Inc.
    Inventors: Dale M. Edgar, David G. Hangauer, Harry Jefferson Leighton, Emmanuel J. M. Mignot, James F. White, Michael Solomon, Kazumi Shiosaki
  • Patent number: 7345032
    Abstract: The present invention provides methods for the preparation of {2-[(8,9)-dioxo-2,6-diaza-bicyclo[5.2.0]-non-1(7)-en-2-yl]ethyl}phosphonic acid, and esters thereof.
    Type: Grant
    Filed: October 20, 2004
    Date of Patent: March 18, 2008
    Assignee: Wyeth
    Inventors: Bogdan K. Wilk, Galina Vid, Weiguo Liu, Xinxu Shi
  • Patent number: 7268123
    Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided: wherein: A is alkylenyl of 1 to 4 carbon atoms, or alkenylenyl of 2 to 4 carbon atoms; R1 and R2 are, independently, hydrogen or a C5 to C7 aryl optionally substituted with 1 to 2 substituents, independently, selected from the group consisting of —C(O)R3, halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy, with the proviso that at least one of R1 and R2 is not hydrogen; R3 is, independently, hydrogen, —OR4, alkyl, aryl, or heteroaryl; R4 is hydrogen, alkyl, aryl, or heteroaryl; R5 and R6 are, independently, hydrogen, alkyl, hydroxyl, alkoxy, or C5 to C7 aryl; wherein any R3 to R6 group having an aryl or heteroaryl moiety can optionally be substituted on the aryl or heteroaryl moiety with 1 to about 5 substituents, independently, selected from the group consisting of halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy.
    Type: Grant
    Filed: October 6, 2005
    Date of Patent: September 11, 2007
    Assignee: Wyeth
    Inventor: Reinhardt Bernhard Baudy
  • Patent number: 7253153
    Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided where at least one of R2 or R3 is not hydrogen. The compounds of the present invention are N-methyl-D-aspartate (NMDA) receptor antagonists and are useful in treating a variety of conditions present in a mammal that benefit from inhibiting the NMDA receptor.
    Type: Grant
    Filed: April 7, 2004
    Date of Patent: August 7, 2007
    Assignee: Wyeth
    Inventors: Reinhardt B. Baudy, John A. Butera
  • Patent number: 7157447
    Abstract: The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS.
    Type: Grant
    Filed: November 29, 2005
    Date of Patent: January 2, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: B. Narasimhulu Naidu, Jacques Banville, Francis Beaulieu, Timothy P. Connolly, Mark R. Krystal, John D. Matiskella, Carl Ouellet, Serge Plamondon, Roger Remillard, Margaret E. Sorenson, Yasutsugu Ueda, Michael A. Walker
  • Publication number: 20040092388
    Abstract: Phosphine compounds represented by the following formula (1): 1
    Type: Application
    Filed: November 6, 2003
    Publication date: May 13, 2004
    Applicant: TAKASAGO INTERNATIONAL CORPORATION
    Inventors: Hideo Shimizu, Takao Saito, Izuru Nagasaki
  • Patent number: 6699855
    Abstract: The present invention relates to compounds of Formula (I): wherein A1 is methylene, ethylene or propylene group and A2 is N or CR5, or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HCV NS3 protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: March 2, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Xiaojun Zhang, Wei Han
  • Patent number: 6673781
    Abstract: The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is (a) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is CONH2 or CONHNH2; one of R3 and R4 is —(L2)-(acidic group) wherein L2 is a group connecting with an acid group and the length of the connecting groups 1 to 5 atoms, and the other is a hydrogen atom; its prodrug, their pharmaceutically acceptable salt, or solvate thereof.
    Type: Grant
    Filed: February 1, 2002
    Date of Patent: January 6, 2004
    Assignee: Shionogi & Co., Ltd.
    Inventors: Mitsuaki Ohtani, Masahiro Fuji, Tetsuo Okada, Makoto Adachi, Tomoyuki Ogawa
  • Publication number: 20030207842
    Abstract: Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have at a group having a guanidino moiety or derivative thereof. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.
    Type: Application
    Filed: December 4, 2002
    Publication date: November 6, 2003
    Inventors: Amir P. Tamiz, L. Josue Alfaro-Lopez, Odile Esther Levy, Joseph Edward Semple
  • Publication number: 20030166927
    Abstract: The present invention relates to compounds of formula (I) wherein R1 and R2 are independently selected from C1-6alkyl; one of R4 and R5 is a group of formula (IA): R3, R6, R7, R8, R9, R10 and R11 and the other of R4 and R5 are as defined within, pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and there use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described.
    Type: Application
    Filed: September 6, 2002
    Publication date: September 4, 2003
    Inventors: Ingemar Starke, Mickael Dahlstrom, David Blomberg
  • Publication number: 20030153096
    Abstract: A water-soluble reference standard is useful for immunoassays of a lipophilic drugs.
    Type: Application
    Filed: January 25, 2002
    Publication date: August 14, 2003
    Inventors: Min Li, Robert S. Wu, Jane S.C. Tsai
  • Publication number: 20030153533
    Abstract: Novel phospholipid derivatives of the General Formula I: 1
    Type: Application
    Filed: November 8, 2002
    Publication date: August 14, 2003
    Applicant: Zentaris AG
    Inventors: Gerhard Nossner, Bernhard Kutscher, Jurgen Engel, Wolfgang Schumacher, Jurij Stekar, Peter Hilgard
  • Publication number: 20030119785
    Abstract: The present invention relates to compounds of the formula I,
    Type: Application
    Filed: November 19, 2002
    Publication date: June 26, 2003
    Applicant: Hoechst Aktiengesellschaft and Genentech Inc.
    Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
  • Patent number: 6521769
    Abstract: Chiral ligands and transition metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The chiral ligands include chiral C1-C6 TunaPhos ligands. The ruthenium TunaPhos complex reduces ketones to the corresponding alcohols with 95-99.6% enantioselectivity. The transition metal complexes of the chiral ligands are useful in asymmetric reactions such as asymmetric hydrogenation, hydride transfer, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, hydrocarboxylation, isomerization, allylic alkylation, cyclopropanation, Diels-Alder reaction, Heck reaction, isomerization, Aldol reaction, Michael addition and epoxidation reactions.
    Type: Grant
    Filed: September 19, 2000
    Date of Patent: February 18, 2003
    Assignee: The Penn State Research Foundation
    Inventor: Xumu Zhang