The Chalcogen And The Nitrogen Are In The 1,5-positions Of The Bicyclo Ring System (e.g., 1,5-benzothiazepinone, Etc.) Patents (Class 540/491)
  • Publication number: 20150038488
    Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I wherein X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.
    Type: Application
    Filed: July 31, 2014
    Publication date: February 5, 2015
    Inventors: Kevin S. Currie, Zhimin Du, Julie Farand, Juan A. Guerrero, Ashley A. Katana, Darryl Kato, Scott E. Lazerwith, Jiayao Li, John O. Link, Nicholas Mai, Gregory Notte, Hyung-Jung Pyun, Michael Sangi, Aaron C. Schmitt, Adam J. Schrier, Kirk L. Stevens, Chandrasekar Venkataramani, William J. Watkins, Zheng-Yu Yang, Jeff Zablocki, Sheila Zipfel
  • Publication number: 20150038489
    Abstract: Described herein is a method of treating long QT syndrome by administration of an effective amount of a potent and selective late sodium ion channel blocker
    Type: Application
    Filed: July 31, 2014
    Publication date: February 5, 2015
    Applicant: Gilead Sciences, Inc.
    Inventors: Luiz Belardinelli, Sridharan Rajamani, Dewan Zeng
  • Patent number: 8895545
    Abstract: In part, the present invention is directed to antibacterial compounds.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: November 25, 2014
    Assignee: Debiopharm International SA
    Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
  • Publication number: 20140343277
    Abstract: The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N? or —CH?; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.
    Type: Application
    Filed: June 25, 2014
    Publication date: November 20, 2014
    Inventors: Shinichi TAIRA, Kunio OSHIMA, Takashi OSHIYAMA, Yasuhiro MENJO, Yasuo KOGA, Hokuto YAMABE, Sunao NAKAYAMA, Kenji TSUJIMAE, Toshiyuki ONOGAWA, Kuninori TAI, Motohiro ITOTANI
  • Patent number: 8685960
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).
    Type: Grant
    Filed: May 5, 2009
    Date of Patent: April 1, 2014
    Assignee: Elexopharm GmbH
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Publication number: 20140031334
    Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 30, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi YAMASHITA, Hideaki KURODA, Nobuaki ITO, Kunio OSHIMA, Jun MATSUBARA, Tae FUKUSHIMA, Satoshi SHIMIZU, Kazumi KONDO, Motohiro ITOTANI
  • Patent number: 8609648
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). 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: Grant
    Filed: June 15, 2010
    Date of Patent: December 17, 2013
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Lu Ying, Xiaowen Peng, Datong Tang, Ce Wang, Yao-Ling Qiu
  • Publication number: 20130261101
    Abstract: The present invention provides bicyclic azaheterocyclobenzylamines of Formula I: wherein the variables are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Application
    Filed: April 1, 2013
    Publication date: October 3, 2013
    Inventors: Andrew P. Combs, Richard B. Sparks, Thomas P. Maduskuie, Jr.
  • Patent number: 8541404
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.
    Type: Grant
    Filed: November 3, 2010
    Date of Patent: September 24, 2013
    Assignee: ElexoPharm GmbH
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Publication number: 20130237523
    Abstract: In part, the present invention is directed to antibacterial compounds.
    Type: Application
    Filed: October 4, 2012
    Publication date: September 12, 2013
    Applicant: AFFINIUM PHARMACEUTICALS, INC.
    Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
  • Patent number: 8501727
    Abstract: The present invention relates to short-acting calcium channel blocking compounds and their use to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension in general, hypertension been.) fore, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.
    Type: Grant
    Filed: August 20, 2009
    Date of Patent: August 6, 2013
    Assignee: Milestone Pharmaceuticals Inc.
    Inventors: Martin P. Maguire, Dominik Herbart, Harry J. Leighton
  • Publication number: 20130172215
    Abstract: This disclosure concerns methods for producing a spinosyn producing strain that comprises modifying a nucleic acid molecule encoding for spinactin by introducing, mutating, deleting, replacing or inactivating a nucleic acid sequence encoding one or more activities encoded by said nucleic acid molecule. Methods for producing a modified Saccharopolyspora spinosa organism are also disclosed.
    Type: Application
    Filed: December 13, 2012
    Publication date: July 4, 2013
    Applicant: DOW AGROSCIENCES LLC
    Inventor: DOW AGROSCIENCES LLC
  • Publication number: 20120328599
    Abstract: The present invention provides moieties that bind to the asymmetric contact interface of a receptor tyrosine kinase (RTK), wherein the moieties inhibit ligand induced trans autophosphorylation of the RTK. The present invention also provides methods of treating or preventing an RTK-associated disease and methods for identifying moieties that bind to an asymmetric contact interface of an RTK.
    Type: Application
    Filed: January 13, 2011
    Publication date: December 27, 2012
    Applicant: YALE UNIVERSITY
    Inventors: Jae Hyun Bae, Irit Lax, Joseph Schlessinger
  • Patent number: 8318720
    Abstract: In part, the present invention is directed to antibacterial compounds.
    Type: Grant
    Filed: July 19, 2007
    Date of Patent: November 27, 2012
    Assignee: Affinium Pharmaceuticals, Inc.
    Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
  • Publication number: 20120028920
    Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Application
    Filed: October 11, 2011
    Publication date: February 2, 2012
    Inventors: Hiroshi YAMASHITA, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
  • Patent number: 7994161
    Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide derivatives, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.
    Type: Grant
    Filed: November 10, 2008
    Date of Patent: August 9, 2011
    Assignee: Sanofi-Aventis
    Inventors: Jidong Zhang, Yannick Benedetti, Alain Commerçon
  • Publication number: 20110144087
    Abstract: The present invention relates to short-acting calcium channel blocking compounds and their use to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension in general, hypertension been.) fore, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.
    Type: Application
    Filed: August 20, 2009
    Publication date: June 16, 2011
    Applicant: Milestone Pharmaceuticals Inc.
    Inventors: Martin P. Maguire, Dominik Herbart, Harry J. Leighton
  • Publication number: 20110136788
    Abstract: [Problem] The present invention aims to provide an agent for the prophylaxis or treatment of irritable bowel syndrome. [Solving Means] An agent for the prophylaxis or treatment of irritable bowel syndrome, containing a compound having a TGR5 receptor agonist activity, a fused ring compound represented by the formula wherein ring A is an optionally substituted aromatic ring, and ring B? is a 5- to 9-membered ring having one or more substituents, or a salt thereof as an active ingredient.
    Type: Application
    Filed: August 6, 2009
    Publication date: June 9, 2011
    Inventor: Minoru Maruyama
  • Publication number: 20110118232
    Abstract: The invention relates to novel pyrimidine compounds of general formula (I), in which: A represents a group C?W or CRfRg; B represents a chemical bond or a group CRhRi; X represents O, S, a group N—Rk or a group CRmRn; D represents C?O or a chemical bond; E represents a linear or branched 2- to 10-membered alkylene chain that, as members of a chain, can have 1 or 2 non-adjacent heteroatom group(s) K, which is selected among O, S, S(O), S(O)2 and N—Rp and which can comprise a carbonyl group and/or a cycloalkanediyl group and/or a double or triple bond; W represents oxygen or sulfur; Z, together with the carbon atoms, to which it is bound, represents a condensed, optionally substituted 5-, 6- or 7-membered carbocyclic compound or heterocyclic compound that has 1, 2, 3 or 4 heteroatoms, which are selected among N, O and S; J represents CH2, CH2—CH2 or CH2—CH2—CH2; M represents CH or N; Y represents CH2, CH2—CH2 or CH2—CH2—CH2 or M-X, together, represent CH?C or CH2—CH?C; n is 0 or 1, and; Ra, Rb, Rc, Rd, Re, Rf,
    Type: Application
    Filed: July 23, 2010
    Publication date: May 19, 2011
    Applicant: Abbott GmbH & Co. KG
    Inventors: Hervè Geneste, Andreas Haupt, Wilfried Braje, Wilfried Lubisch, Gerd Steiner
  • Publication number: 20110112067
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.
    Type: Application
    Filed: November 3, 2010
    Publication date: May 12, 2011
    Applicant: Universitat des Saarlandes
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Publication number: 20110098273
    Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.
    Type: Application
    Filed: September 3, 2008
    Publication date: April 28, 2011
    Applicant: Nektar Therapeutics
    Inventors: Zhongxu Ren, Bo-Liang Deng, Jennifer Riggs-Sauthier, Micah Harvey
  • Publication number: 20110053910
    Abstract: Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.
    Type: Application
    Filed: July 3, 2006
    Publication date: March 3, 2011
    Inventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
  • Publication number: 20110008288
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). 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: Application
    Filed: June 15, 2010
    Publication date: January 13, 2011
    Inventors: Yat Sun Or, Lu Ying, Xiaowen Peng, Datong Tang, Ce Wang, Yao-Ling Qiu
  • Patent number: 7858776
    Abstract: Compounds having the formula (I) pharmaceutical compositions containing them and their methods of use for the treatment of neurological disorders related to amyloid ? protein production and neurological disorders such as Alzheimer's disease. These compounds inhibit ? secretase and thereby inhibit the production of amyloid ? protein, thereby acting to prevent the formation of neurological deposits of amyloid protein.
    Type: Grant
    Filed: January 26, 2009
    Date of Patent: December 28, 2010
    Assignee: AstraZeneca AB
    Inventors: Bruce Thomas Dembofsky, Robert Jacobs, Cyrus Ohnmacht
  • Patent number: 7842686
    Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.
    Type: Grant
    Filed: January 21, 2009
    Date of Patent: November 30, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Corey Don Anderson, Andreas P. Termin, Pramod Joshi, Sara S. Hadida Ruah, Daniele Bergeron, Sanghee Yoo, Jingrong Cao
  • Patent number: 7829713
    Abstract: The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function in animals.
    Type: Grant
    Filed: February 27, 2007
    Date of Patent: November 9, 2010
    Assignee: Helicon Therapeutics, Inc.
    Inventors: Terrence P. Keenan, Alan P. Kaplan
  • Patent number: 7786105
    Abstract: The invention relates to pyrimidine compounds of general formula (I), and to the use of these compounds of general formula (I) and of the physiologically compatible acid addition salts of compounds (I) for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D3 receptor antagonists or agonists.
    Type: Grant
    Filed: June 3, 2005
    Date of Patent: August 31, 2010
    Assignee: Abbott GmbH & Co. KG
    Inventors: Herve Geneste, Andreas Haupt, Wilfried Braje, Wilfried Lubisch, Gerd Steiner
  • Publication number: 20100203135
    Abstract: Methods of forming soft connective tissue compositions such as skin equivalents, compositions made by the methods and their uses.
    Type: Application
    Filed: March 14, 2006
    Publication date: August 12, 2010
    Inventors: Paul Kemp, David Shering, Andrew Shering, Penny Johnson, Damian Marshall
  • Publication number: 20100160627
    Abstract: Compounds having the formula (I) pharmaceutical compositions containing them and their methods of use for the treatment of neurological disorders related to amyloid ? protein production and neurological disorders such as Alzheimer's disease. These compounds inhibit ? secretase and thereby inhibit the production of amyloid ? protein, thereby acting to prevent the formation of neurological deposits of amyloid protein.
    Type: Application
    Filed: January 26, 2009
    Publication date: June 24, 2010
    Applicant: ASTRAZENECA AB
    Inventors: Bruce Thomas Dembofsky, Robert Jacobs, Cyrus Ohnmacht
  • Publication number: 20100144715
    Abstract: The present invention is directed to substituted benzodiazepinones, benzoxazepinones and benzothiazepinones compounds that are sodium channel blockers useful for the treatment of chronic and neuropathic pain. The compounds of the present invention are also useful for the treatment of other conditions, including disorders of the CNS such as anxiety, depression, epilepsy, manic depression and bipolar disorder. This invention also provides pharmaceutical compositions comprising a compound of the present invention, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. This invention further comprises methods for the treatment of acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain and disorders of the CNS including, but not limited to, epilepsy, manic depression, depression, anxiety and bipolar disorder comprising administering the compounds and pharmaceutical compositions of the present invention.
    Type: Application
    Filed: February 25, 2008
    Publication date: June 10, 2010
    Inventors: Scott B. Hoyt, Dong Ok, Hyun Ok, Clare London, Joseph I. Duffy
  • Publication number: 20100137282
    Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials. Z1 and Z2 are independently selected from CH and N.
    Type: Application
    Filed: April 16, 2008
    Publication date: June 3, 2010
    Inventors: David Evan Davies, David Thomas Davies, Ilaria Giordano, Alan Joseph Hennessy, Neil David Pearson
  • Publication number: 20100130470
    Abstract: In part, the present invention is directed to antibacterial compounds.
    Type: Application
    Filed: July 19, 2007
    Publication date: May 27, 2010
    Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
  • Patent number: 7718646
    Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen
    Type: Grant
    Filed: June 24, 2008
    Date of Patent: May 18, 2010
    Assignee: Sanofi-Aventis
    Inventors: Philippe R. Bovy, Roberto Cecchi, Gilles Courtemanche, Tiziano Croci, Ambrogio Oliva, Nunzia Viviani
  • Patent number: 7622460
    Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen
    Type: Grant
    Filed: June 24, 2008
    Date of Patent: November 24, 2009
    Assignee: sanofi-aventis
    Inventors: Philippe R. Bovy, Roberto Cecchi, Gilles Courtemanche, Tiziano Croci, Ambrogio Oliva, Nunzia Viviani
  • Patent number: 7550453
    Abstract: The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: June 23, 2009
    Assignee: Aventis Pharma SA
    Inventors: Jidong Zhang, Neerja Bhatnagar, Jean-Marie Ruxer
  • Publication number: 20090156578
    Abstract: In part, the present invention is directed towards compounds with FabI inhibiting properties. Such compounds may also inhibit other enzymes, including those similar to FabI either structurally or functionally, for example, Fab K. Kits and compositions that include the disclosed compounds are also provided. Methods of treating a subject with a bacterial illness is also disclosed.
    Type: Application
    Filed: December 1, 2006
    Publication date: June 18, 2009
    Inventors: Henry Pauls, Judd M. Berman
  • Patent number: 7541131
    Abstract: The invention provides a resist composition for use in the production process of a semiconductor such as IC, in the production of a circuit substrate of liquid crystal, thermal head and the like or in other photofabrication processes, a compound for use in the resist composition and a pattern forming method using the resist composition, which are a resist composition comprising (A) a sulfonium salt represented by the following formula (I); and a pattern forming method using the resist composition: wherein R1 represents an alkyl group or an aryl group, R2 to R9 each independently represents a hydrogen atom or a substituent and may combine with each other to form a ring, Z represents an electron-withdrawing divalent linking group, Xn? represents an n-valent anion, n represents an integer of 1 to 3, and m represents the number of anions necessary for neutralizing the electric charge.
    Type: Grant
    Filed: February 17, 2006
    Date of Patent: June 2, 2009
    Assignee: FUJIFILM Corporation
    Inventor: Yasutomo Kawanishi
  • Publication number: 20090093459
    Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide benzothiazepine compounds, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds and to intermediate precursors to such compounds.
    Type: Application
    Filed: November 10, 2008
    Publication date: April 9, 2009
    Applicant: SANOFI-AVENTIS
    Inventors: Jidong ZHANG, Yannick BENEDETTI, Frederico NARDI, Alain COMMERCON
  • Publication number: 20090093457
    Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: December 10, 2008
    Publication date: April 9, 2009
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Roland MAIER, Michael MARK, Mohammad TADAYYON, Ralf R. H. LOTZ
  • Publication number: 20090075971
    Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide derivatives, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.
    Type: Application
    Filed: November 10, 2008
    Publication date: March 19, 2009
    Applicant: SANOFI-AVENTIS
    Inventors: Jidong Zhang, Yannick Benedetti, Alain Commercon
  • Publication number: 20090042858
    Abstract: The present invention discloses novel methods and compositions for viral inhibition, particularly inhibition of HCV and SARS. The invention also provides compositions including novel oxoazepanylacetamide derivatives useful for viral inhibition.
    Type: Application
    Filed: June 16, 2006
    Publication date: February 12, 2009
    Inventors: Paul Barsanti, Nathan Brammier, Bryan Chang, Zhi-Jie Ni, Weibo Wang, Amy Weiner
  • Publication number: 20080311609
    Abstract: The present invention relates to novel molecular probes having the formula (I) (I) useful for the characterization, detection, localization and isolation of the ?-secretase enzyme.
    Type: Application
    Filed: December 14, 2005
    Publication date: December 18, 2008
    Applicant: ASTRAZENECA AB
    Inventors: Barry Greenberg, Daniel C. Hill, Robert Jacobs, Sangram S. Sisodia
  • Publication number: 20080261949
    Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen a
    Type: Application
    Filed: June 24, 2008
    Publication date: October 23, 2008
    Applicant: SANOFI-AVENTIS
    Inventors: Philippe R. Bovy, Roberto Cecchi, Gilles Courtemanche, Tiziano Croci, Ambrogio Oliva, Nunzia Viviani
  • Patent number: 7425550
    Abstract: A compound of formula I is provided having the structure wherein W is as defined herein; X is —CHR5O—; Y is a bond; Z is an aryl or heteroaryl group; and R1, and R2, are as described herein. Further provided is a method for treating diabetes and related diseases employing the above compound, either alone or in combination with another therapeutic agent.
    Type: Grant
    Filed: February 13, 2006
    Date of Patent: September 16, 2008
    Assignee: Bristol-Meyers Squibb Company
    Inventors: Philip Sher, Gang Wu, Terry Stouch, Bruce Ellsworth
  • Patent number: 7390798
    Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.
    Type: Grant
    Filed: February 9, 2005
    Date of Patent: June 24, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Theresa M. Williams, Christopher S. Burgey, Thomas J. Tucker, Craig A. Stump, Ian M. Bell
  • Patent number: 7361648
    Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
    Type: Grant
    Filed: August 22, 2006
    Date of Patent: April 22, 2008
    Assignee: Roche Palo Alto LLC
    Inventors: Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, III, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
  • Patent number: 7354914
    Abstract: This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Grant
    Filed: November 29, 2004
    Date of Patent: April 8, 2008
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: Richard E. Olson
  • Patent number: 7294622
    Abstract: Compounds having the formula (I) pharmaceutical compositions containing them and their methods of use for the treatment of neurological disorders related to amyloid ? protein production and neurological disorders such as Alzheimer's disease. These compounds inhibit ? secretase and thereby inhibit the production of amyloid ? protein, thereby acting to prevent the formation of neurological deposits of amyloid protein.
    Type: Grant
    Filed: October 2, 2003
    Date of Patent: November 13, 2007
    Assignee: Astrazeneca AB
    Inventors: Christopher Becker, Bruce Dembofsky, Robert Jacobs, James Kang, Cyrus Ohnmacht, James Rosamond, Ashokkumar Bhikkappa Shenvi, Thomas Simpson, James Woods
  • Patent number: 7211573
    Abstract: The invention relates to compounds of the formula I wherein R, R1, R2, R3, X, and n are defined in the specification. The invention also provides pharmaceutically suitable acid addition salts thereof and all forms of optically pure enantiomers, recemates or diastereomers and diastereomeric mixtures thereof. Compounds of the invention are useful for the treatment of Alzheimer's disease.
    Type: Grant
    Filed: November 30, 2005
    Date of Patent: May 1, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Roland Jakob-Roetne, Wolfgang Wostl
  • Patent number: 7141562
    Abstract: Compound of the Formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein: X is CH or N, Y is C or S, Z is —SO2— or —(CRaRb)r—, n is 1 or 2, R2 is aryl or heteroaryl, and R1, R3, R4, R5, R6, R7, R8, R9, Ra, Rb, m, p, q and r, are as defined herein. The compounds are modulators of the 5-HT6 receptor and are useful for treatment of central nervous system disorders. Also provided are methods for preparing, compositions comprising, and methods for using Compounds of Formula I.
    Type: Grant
    Filed: November 6, 2003
    Date of Patent: November 28, 2006
    Assignee: Roche Palo Alto LLC
    Inventors: Hans Maag, Meng Sui, Shu-Hai Zhao