Bicyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 544/376)
  • Publication number: 20130053369
    Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.
    Type: Application
    Filed: October 26, 2012
    Publication date: February 28, 2013
    Applicant: Astellas Pharma Inc.
    Inventor: Astellas Pharma Inc.
  • Publication number: 20130029973
    Abstract: A compound has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating hyperphosphatemia, preventing hyperphosphatemia, or both. The compound is a tetrahydrobenzothiophene compound. A pharmaceutical composition for treating hyperphosphatemia includes the compound or salt thereof. A method of treating hyperphosphatemia includes administering to a subject an effective amount of the compound or salt thereof.
    Type: Application
    Filed: April 27, 2011
    Publication date: January 31, 2013
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Shunichiro Hachiya, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
  • Publication number: 20130029978
    Abstract: There is a need for FAAH inhibitors capable of oral administration and having excellent efficacy, particularly agents for the prevention and treatment of pain. Disclosed are novel arylurea compounds represented by formula (I), salts or solvates thereof, and pharmaceutical compositions comprising the same as an active ingredient. The pharmaceutical composition is used primarily for FAAH inhibitors, or agents for prevention and treatment of pain.
    Type: Application
    Filed: December 24, 2010
    Publication date: January 31, 2013
    Inventors: Tomoyuki Kamino, Yoshitaka Maeda
  • Patent number: 8362000
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Grant
    Filed: April 22, 2010
    Date of Patent: January 29, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Publication number: 20120264764
    Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.
    Type: Application
    Filed: June 11, 2012
    Publication date: October 18, 2012
    Inventors: John S. Kovach, Francis Johnson
  • Patent number: 8288390
    Abstract: The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted homopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R5 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloalkyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, or a salt thereof.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: October 16, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Taiichi Ohra
  • Patent number: 8278290
    Abstract: The present invention relates to compounds of general formula (I) as tublin polymerization inhibitors and methods for preparing such compounds.
    Type: Grant
    Filed: February 14, 2006
    Date of Patent: October 2, 2012
    Assignee: Biononics Limited
    Inventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
  • Publication number: 20120245165
    Abstract: The present invention relates to the novel benzofuran derivatives, the preparation thereof and the composition comprising the same. The benzofuran derivatives of the present invention showed potent inhibiting activity of beta-amyloid aggregation and cell cytotoxicity resulting in stimulating the proliferation of neuronal cells as well as recovering activity of memory learning injury caused by neuronal cell injury using transformed animal model with beta-amyloid precursor gene, therefore the compounds can be useful in treating or preventing cognitive function disorder.
    Type: Application
    Filed: June 5, 2012
    Publication date: September 27, 2012
    Applicants: DAEWOONG PHARMACEUTICAL CO., LTD, MEDIFRON DBT CO., LTD.
    Inventors: Dong Wook KANG, Jee Woo LEE, Young Ho KIM, Hee KIM, Hee Jin HA, Eun Joo NAM, Chan Mi JOUNG
  • Patent number: 8273905
    Abstract: Compounds corresponding to formula I, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n have the meanings given in the description, and also a process for the preparation of these compounds and intermediate products of this process. Furthermore, pharmaceutical compositions comprising the compounds of Formula I and related methods of treatment.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: September 25, 2012
    Assignee: Abbott Products GmbH
    Inventors: Brian Moloney, Lester Marrison, Dieter Ziegler, Michael Mlinaric, Christiane Boecker, Reinhard Brueckner, Michael Weske, Klaus Witte, Yvan Fischer
  • Publication number: 20120238541
    Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
    Type: Application
    Filed: September 17, 2010
    Publication date: September 20, 2012
    Applicant: Almac Discovery Limited
    Inventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
  • Publication number: 20120232096
    Abstract: The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted homopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R5 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloalkyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, or a salt thereof.
    Type: Application
    Filed: May 24, 2012
    Publication date: September 13, 2012
    Inventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Taiichi Ohra
  • Publication number: 20120232095
    Abstract: The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted homopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R5 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloalkyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, or a salt thereof.
    Type: Application
    Filed: May 24, 2012
    Publication date: September 13, 2012
    Inventors: Tetsuya TSUKAMOTO, Takeshi WAKABAYASHI, Taiichi OHRA
  • Publication number: 20120214770
    Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.
    Type: Application
    Filed: May 1, 2012
    Publication date: August 23, 2012
    Applicant: BIONOMICS LIMITED
    Inventors: JASON HUGH CHAPLIN, GURMIT SINGH GILL, DAMIAN WOJCIECH GROBELNY, BERNARD LUKE FLYNN, GABRIEL KREMMIDIOTIS
  • Patent number: 8227473
    Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: July 24, 2012
    Assignee: Lixte Biotechnology, Inc.
    Inventors: John S. Kovach, Francis Johnson
  • Publication number: 20120178934
    Abstract: The present invention relates to novel benzene-carboxamide compounds having a structure that corresponds to the general formula (I), and also to their method of synthesis and to their use in pharmaceutical compositions intended for use in human or veterinary medicine or else to their use in cosmetic compositions.
    Type: Application
    Filed: September 16, 2010
    Publication date: July 12, 2012
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Sandrine Chambon, Laurence Clary, Marlene Schuppli
  • Publication number: 20120157463
    Abstract: The present invention relates to chromone derivatives, their preparation, their pharmaceutical compositions and their application as D3 dopaminergic ligands as a medicament for disorders of the central nervous system.
    Type: Application
    Filed: August 31, 2010
    Publication date: June 21, 2012
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Pierre Sokoloff, Thierry Imbert, Jean-François Patoiseau, Jean-Pierre Rieu
  • Patent number: 8198280
    Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: June 12, 2012
    Assignee: Merck Serono SA
    Inventors: Dominique Swinnen, Jerome Gonzalez
  • Publication number: 20120108815
    Abstract: A precursor for the deposition of a thin film by atomic layer deposition is provided. The compound has the formula MxLy where M is a metal and L is an amidrazone-derived ligand or an amidate-derived ligand. A process of forming a thin film using the precursors is also provided.
    Type: Application
    Filed: April 21, 2010
    Publication date: May 3, 2012
    Applicant: WAYNE STATE UNIVERSITY
    Inventor: Aloke K. Dutta
  • Publication number: 20120095020
    Abstract: The present invention provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof. Also, the present invention provides a pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable diluent or carrier. The present invention further provides methods for treating abdominal aortic aneurysm, plaque instability, atherosclerosis, or autoimmune disorders such as rheumatoid arthritis, psoriasis, and lupus comprising administering a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable diluent or carrier.
    Type: Application
    Filed: October 14, 2011
    Publication date: April 19, 2012
    Applicant: Eli Lilly and Company
    Inventors: Gary G. DENG, Konstantinos GAVARDINAS, Prabhakar Kondaji JADHAV, Euibong Jemes KIM, Matthew Allen SCHIFFLER
  • Patent number: 8153682
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.
    Type: Grant
    Filed: July 18, 2008
    Date of Patent: April 10, 2012
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
  • Patent number: 8148422
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: April 3, 2012
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Mark J. Macielag, James J. McNally
  • Publication number: 20120046277
    Abstract: The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted bromopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R3 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloakyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, wherein R2 and R3 do not exist when carbon atoms respectively adjacent to R2: and R3 form a double bond, and there is no
    Type: Application
    Filed: March 9, 2010
    Publication date: February 23, 2012
    Inventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Taiichi Ohra
  • 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
  • Publication number: 20120022062
    Abstract: The present invention relates to flavanoid compounds of general formula (X1) wherein: R1 is selected from a group consisting of morpholinyl, N-methyl piperizinyl, piperidinyl and N,N?-dimethylamino groups, and n ranges from 3 to 6, and process for preparation thereof. The present invention relates to the demonstration of anti Helicobacter pylori activity and gastric antisecretory activity of semisynthetically designed flavonoid compounds, to be used for the prevention and treatment of gastroduodenal disorders in general and peptic ulcer diseases in particular. The present invention also relates to a hetero-dimeric bi-functional molecule that can be used as monotherapy substituting/replacing/overcoming currently used triple/quadruple therapy, thereby implicating/anticipating/envisaging its commercial applicability.
    Type: Application
    Filed: February 26, 2010
    Publication date: January 26, 2012
    Inventors: Pratap Kumar Dab, Suchandra Goswami, Annalaskhmi Chinniah, Janaswamy Madusudana Rao, Suresh Babu Katragadda
  • Publication number: 20110319448
    Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Application
    Filed: September 9, 2011
    Publication date: December 29, 2011
    Applicant: THERAVANCE, INC.
    Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
  • Patent number: 8076328
    Abstract: Process for the protection of fish and invertebrates and all their stages of development against or for the treatment of mycoses caused by fungi of the genera Saprolegnia, Aphanomyces, Achlyaflagellata and other species important in aquacultures by use of 2-[[[[1-[3-(1-fluoro-2-phenylethyl)oxy]phenyl]ethylidene]amino]oxy]methyl]alpha-(methoxyimino)-N-methyl-alphaE-benzeneacetamide, amisulbrom, cyazofamid, enestrobin, famoxadone, fenamidone, fluoxastrobin, orysastrobin, picoxystrobin and pyribencarb. This use leads to an inhibition or destruction of pathogenic fungi. The composition, comprising at least one fungicide selected from the abovementioned group for use in fish farming and keeping is suitable for the prophylaxis and therapy of diseases of fish in aquaculture, in breeding ponds, breeding tanks, aquariums, natural stretches of game fish waters, ponds, and marine fish farms. Addition to the water and feed and direct application are the associated use forms.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: December 13, 2011
    Assignee: Bayer CropScience AG
    Inventors: Isolde Häuser-Hahn, Klaus Stenzel, Ulrike Wachendorff-Neumann
  • Patent number: 8071600
    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: Grant
    Filed: August 31, 2006
    Date of Patent: December 6, 2011
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    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: 8067594
    Abstract: The invention provides a process for producing a compound of formula (I), wherein Y is selected from the group consisting of CH3, CH2OH, CH2CH2OH, CH2Br and Br; comprising the steps of: (i) reacting a compound of formula (II), wherein OX represents hydroxy or O?M+, in which M+ is a cation selected from Li+, Na+ and K+, and Y is as defined above; with trans-cinnamaldehyde (III), in the presence of a secondary amine compound; then (ii) treating the product of the preceding step with acid to afford the compound of formula (I). The above process may also be used in the production of tolterodine and fesoterodine, which are useful in the treatment of overactive bladder.
    Type: Grant
    Filed: May 21, 2007
    Date of Patent: November 29, 2011
    Assignee: Pfizer Inc.
    Inventors: Jens Bertil Ahman, Barry Richard Dillon, Alan John Pettman
  • Publication number: 20110262352
    Abstract: Compounds of formula (I), wherein X, Z, A, B, D, E, R1-R4 and m are as defined in the claims, exhibit alpha2C antagonistic activity and are thus useful as alpha2 antagonists.
    Type: Application
    Filed: November 20, 2009
    Publication date: October 27, 2011
    Inventors: David Din Belle, Patrik Holm, Arto Tolvanen, Gerd Wohlfahrt
  • Publication number: 20110217335
    Abstract: Disclosed are macrocyclic compounds of formulae I, I?, II, II?, III, III?, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.
    Type: Application
    Filed: January 15, 2009
    Publication date: September 8, 2011
    Applicant: UNIVERSITE DE STRASBOURG
    Inventors: Nicolas Winssinger, Sofia Barluenga, Martin Karplus
  • Patent number: 8008302
    Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof, in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
    Type: Grant
    Filed: July 25, 2005
    Date of Patent: August 30, 2011
    Assignee: Merck Serono SA
    Inventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
  • Publication number: 20110207729
    Abstract: An object of the present invention is to provide a novel and excellent agent for treating or preventing dementia, schizophrenia, and the like, based on the serotonin 5-HT5A receptor modulating action. It was confirmed that a bicyclic acylguanidine derivative which has a characteristic structure that guanidine is bonded to one ring of a bicyclic structure such as chromene and dihydronaphthalene through a carbonyl group and a cyclic group is bonded on the other ring, has a potent 5-HT5A receptor modulating action and an excellent pharmacological action based on this mechanism. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder.
    Type: Application
    Filed: August 7, 2008
    Publication date: August 25, 2011
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Isao Kinoyama, Satoshi Miyamoto, Takehiro Miyazaki, Yohei Koganemaru, Yuichiro Kawamoto, Nobuyuki Shiraishi, Hiroaki Hoshii, Akio Kuroda, Mayako Yamazaki, Minoru Yasuda, Hiroaki Mizuno
  • Patent number: 7998963
    Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein Ar is indolyl, indazolyl or dihydroindolyl, and R1, R2, R3 and R4 are as defined herein. Also provided are pharmaceutical compositions, methods of using the compounds in the treatment of depressive, anxiolytic and other disorders associated with inhibition of the reuptake of norepinephrine, serotonin, and dopamine, and methods of preparing the compounds.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: August 16, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: David Scott Carter, Matthew C. Lucas, Ryan Craig Schoenfeld, Robert James Weikert
  • Publication number: 20110172244
    Abstract: The invention provides compounds, of Formula I: pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.
    Type: Application
    Filed: February 20, 2009
    Publication date: July 14, 2011
    Applicant: IRM LLC
    Inventors: Phillip B. Alper, Robert Epple, Pierre-Yves Michellys, Daniel Mutnick, Victor Nikulin
  • Patent number: 7973030
    Abstract: A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided.
    Type: Grant
    Filed: February 25, 2005
    Date of Patent: July 5, 2011
    Assignee: Asahi Kasei Pharma Corporation
    Inventors: Takehiko Sasahara, Mitsunobu Mohri, Ken-Ichi Kasahara
  • Patent number: 7960385
    Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: September 5, 2008
    Date of Patent: June 14, 2011
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
  • Publication number: 20110118263
    Abstract: The invention discloses benzothiophene alkanol piperazine derivatives and their use as antidepressants. The invention discloses the said benzothiophene alkanol piperazine derivative having triple inhibition effect on the reuptake of 5-HT, NA and DA. Compared with clinical used antidepressants so far having single target, e.g. desipramine and fluoxetine, and clinical used antidepressants so far having double targets, e.g venlafaxine and duloxetine, the said benzothiophene alkanol piperazine derivatives of the present invention may have a broader indication range and less toxic and side effects to nervous system. The benzothiophene alkanol piperazine derivatives are the compounds with the following formula or their pharmaceutically acceptable salts, wherein Ar1, R1-R4, X, Y, m and n have the same definition as defined in claim 1.
    Type: Application
    Filed: June 30, 2009
    Publication date: May 19, 2011
    Applicant: CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co. Ltd.
    Inventors: Jianqi Li, Kai Gao, Na Lv
  • Publication number: 20110105475
    Abstract: The present invention relates to compounds of formula (I) wherein the substituents are as defined in the claims, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention and/or amelioration of one or more symptoms of disease or disorders related to the activity of FXR. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).
    Type: Application
    Filed: March 30, 2009
    Publication date: May 5, 2011
    Applicant: MERXCK PATENT GESELLSCHAFT
    Inventors: Didier Roche, Giséle Mautino, Ingo Kober, Francis Contard, Serge Christmann-Franck, Saumitra Sengupta, Ramesh Sistla, Gummadi Venkateshwar Rao
  • Publication number: 20110092700
    Abstract: The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y1 and Y2 are selected from —N? etc., Y3 and Y4 are selected from —CH? etc., A is selected from sulfamide etc., R1 is selected from hydrogen etc., and R2 is selected from C1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.
    Type: Application
    Filed: December 3, 2010
    Publication date: April 21, 2011
    Inventors: Hitoshi Iikura, Ikumi Hyoudoh, Toshihiro Aoki, Noriyuki Furuichi, Masayuki Matsushita, Fumio Watanabe, Sawako Ozawa, Masahiro Sakaitani, Pil-Su Ho, Yasushi Tomii, Kenji Takanashi, Naoki Harada
  • Patent number: 7915253
    Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
    Type: Grant
    Filed: September 4, 2008
    Date of Patent: March 29, 2011
    Assignee: Kalypsys, Inc
    Inventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen K. Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steve P. Govek
  • Publication number: 20110015185
    Abstract: The present invention relates to compounds of formula (I): wherein P, R3, W1, and W2 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.
    Type: Application
    Filed: September 28, 2010
    Publication date: January 20, 2011
    Applicant: BIOVITRUM AB
    Inventors: Gary Johansson, Peter Brandt, Björn M. Nilsson
  • Publication number: 20110003830
    Abstract: The invention relates to a novel process for the preparation of 3-amino-8-(1-piperazinyl)-2H-1-benzopyran-2-one, a broad spectrum 5-HT receptor binding ligand having potent 5-HT1A-agonistic as well as 5-HT1D-antagonistic activity. The invention also relates to novel salts and solvates, in particular hydrates of salts of said compound, as well as to their use as medicaments.
    Type: Application
    Filed: July 2, 2010
    Publication date: January 6, 2011
    Applicant: Solvay Pharmaceuticals B.V.
    Inventor: Cornelis BAKKER
  • Publication number: 20100298323
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: June 3, 2010
    Publication date: November 25, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Milan Bruncko, Yujia Dai, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Todd M. Hansen
  • Publication number: 20100292190
    Abstract: The present invention relates to compounds of general formula (I) as tublin polymerisation inhibitors and methods for preparing such compounds.
    Type: Application
    Filed: February 14, 2006
    Publication date: November 18, 2010
    Applicant: Bionomics Limited
    Inventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
  • Publication number: 20100286123
    Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Application
    Filed: April 27, 2010
    Publication date: November 11, 2010
    Inventors: Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Nardos H. Teumelsan, Lihu Yang, Yuping Zhu, Shawn P. Walsh
  • Publication number: 20100286152
    Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof,
    Type: Application
    Filed: June 5, 2008
    Publication date: November 11, 2010
    Applicant: Glaxo Group Limited
    Inventors: Giovanni Bernasconi, Steven Mark Bromidge, Andrew James Carpenter, Lucilla D'Adamo, Romano Di Fabio, Sebastien Guery, Francesca Pavone, Alfonso Pozzan, Marilisa Rinaldi, Fabio Maria Sabbatini, Yves St-Denis
  • Patent number: 7820675
    Abstract: The present invention relates to compounds of formula (I): wherein P, R3, W1, and W2 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.
    Type: Grant
    Filed: December 20, 2004
    Date of Patent: October 26, 2010
    Assignee: Biovitrum AB
    Inventors: Gary Johansson, Peter Brandt, Björn M. Nilsson
  • Publication number: 20100256142
    Abstract: A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.
    Type: Application
    Filed: September 25, 2009
    Publication date: October 7, 2010
    Inventors: Jeffrey Aube, Bryan L. Roth, Partha Ghosh, Kevin J. Frankowski
  • Publication number: 20100249094
    Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Application
    Filed: March 10, 2010
    Publication date: September 30, 2010
    Inventors: Kap-Sun Yeung, Kyle E. Parcella, John A. Bender, Brett R. Beno, Katharine A. Grant-Young, Ying Han, Piyasena Hewawasam, John F. Kadow, Andrew Nickel
  • Publication number: 20100234391
    Abstract: Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I) wherein X, Y, R1 and R2 are as defined herein.
    Type: Application
    Filed: May 26, 2010
    Publication date: September 16, 2010
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Beth Anne Lorsbach, James Melvin Ruiz, Thomas Clarence Sparks, Michael Thomas Sullenberger, Irene Mae Morrison, Jeffery Dale Webster