Nitrogen Or A -c(=x)- Group, Wherein X Is Chalcogen, Attached Directly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 549/57)
  • Publication number: 20100137298
    Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.
    Type: Application
    Filed: June 13, 2008
    Publication date: June 3, 2010
    Applicant: Wyeth
    Inventors: Jeremy Ian Levin, Thomas Saltmarsh Rush, III, Frank Lovering, Yonghan Hu, Jianchang Li, Wei Li, Jun Jun Wu, Rajeev Hotchandani, Jason Shaoyun Xiang, Xuemei Du, Derek Cecil Cole, Steve Yikkai Tam
  • Publication number: 20100130737
    Abstract: The present invention provides a GPR receptor function regulator comprising the compound represented by the formula: [wherein ring A is an optionally substituted isocyclic or heterocyclic ring, P is a bond or spacer, ring D is an optionally substituted monocyclic aromatic ring which may be condensed with a 5- to 7-membered ring, V is a bond or the group represented by the formula —CR14?CR15— or —N?CR16— (wherein R14, R15 and R16 each represents a hydrogen atom or optionally substituted hydrocarbon group), Q is a bond or spacer, and W is a carboxyl or a group biologically equivalent to a carboxyl] or its salt or a prodrug thereof.
    Type: Application
    Filed: February 17, 2006
    Publication date: May 27, 2010
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Fumio Itoh, Eiji Kimura, Yumi Imai, Masaaki Mori, Yoshio Aramaki, Yasuhisa Kohara, Tsukasa Sugo, Yoji Hayase, Hiromi Kobayashi, Kazuhiro Ogi
  • Publication number: 20100125090
    Abstract: The present invention provides compounds of Formula I useful as modulators of ABC transporter activity, or a pharmaceutically acceptable salt thereof, wherein RB, n, B, RC, RD, RE, A, and Z are described generally and in classes and subclasses below. The present invention also provides pharmaceutical compositions, methods and kits associated with Formula I, useful for as modulators, and for the treatments of disease and disease conditions associated with ABC transporter proteins.
    Type: Application
    Filed: August 14, 2009
    Publication date: May 20, 2010
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara S. Hadida Ruah, Mark Miller, Ashvani Singh, Matthew Hamilton, Peter D.J. Grootenhuis
  • Publication number: 20100063068
    Abstract: The disclosure provides compounds of formula I, II, III, IV, and V, 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: August 28, 2009
    Publication date: March 11, 2010
    Inventors: Richard Pracitto, John F. Kadow, John A. Bender, Brett R. Beno, Katharine A. Grant-Young, Ying Han, Piyasena Hewawasam, Andrew Nickel, Kyle E. Parcella, Kap-Sun Yeung, Louis S. Chupak
  • Patent number: 7674815
    Abstract: Compounds of formula I processes for their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 29, 2007
    Date of Patent: March 9, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christoph Faeh, Holger Kuehne, Thomas Luebbers, Patrizio Mattei, Cyrille Maugeais, Philippe Pflieger
  • Patent number: 7666866
    Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: November 15, 2005
    Date of Patent: February 23, 2010
    Assignee: Eli Lilly and Company
    Inventors: Jeffry Bernard Franciskovich, David Kent Herron, Valentine Joseph Klimkowski, Angela Lynn Marquart, John Joseph Masters, David Mendel, Andrew Michael Ratz, Gerald Floyd Smith, Michael Robert Wiley, Ying Kwong Yee
  • Publication number: 20100015053
    Abstract: The present invention is directed to radiolabelled ligands, useful for the labeling and imaging of TRP M8 (transient receptor potential M8 channel) functionality. The present invention is further directed to pharmaceutical compositions comprising the radiolabelled ligands and methods for the preparation of the radiolabelled ligands.
    Type: Application
    Filed: July 9, 2009
    Publication date: January 21, 2010
    Inventors: Paul D. Acton, Dennis J. Hlasta, Jay M. Matthews, James J. McNally
  • Publication number: 20090318541
    Abstract: The present invention relates to a novel class of hydroxamic acid derivatives carbamate, urea, amide and sulfonamide substitutions. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: April 14, 2006
    Publication date: December 24, 2009
    Inventors: Joey Methot, Thomas A. Miller, David J. Witter
  • Publication number: 20090299074
    Abstract: The invention provides benzo[b]thiophene derivatives useful as production intermediates for chymase inhibitors, and a process for their production. The invention relates to benzo[b]thiophene derivatives represented by the following formula, and a process for their production.
    Type: Application
    Filed: October 27, 2006
    Publication date: December 3, 2009
    Applicant: TEIJIN PHARMA LIMITED
    Inventors: Naoki Yajima, Yaoshinori Sato, Hiroshi Yoshino, Tatsuya Koizumi, Yasuhiro Hiroki
  • Publication number: 20090298924
    Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers: wherein Y1 is a bond, —(C?O)—, —S(O2)—, —C(?O)O—, —OC(?O)—, —(C?O)NR3—, —NR3(C?O)—, —S(O2)NR3—, —NR3S(O2)—, or —NR3(C?O)NR5—, wherein R3 and R5 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent radical of formula -(Alk1)m(O)n(Alk2)p— wherein m, n, p, Alk1, Alk2 and Q are as defined in the claims; z is 0 or 1; A represents an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker]- represents a divalent linker radical; R is a radical of formula (X) or (Y): wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, —(C?O)R3, —(C?O)OR3, or —(C?O)NR3 wherein R
    Type: Application
    Filed: May 4, 2006
    Publication date: December 3, 2009
    Applicant: Chroma Therapeutics Ltd
    Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, David Festus Charles Moffat
  • Patent number: 7625944
    Abstract: The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.
    Type: Grant
    Filed: July 30, 2007
    Date of Patent: December 1, 2009
    Assignee: Activesite Pharmaceuticals, Inc.
    Inventors: Sukanto Sinha, Tamie Jo Chilcote
  • Publication number: 20090291978
    Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, C(?O)—, —S(?O)2—, —C(—O)O—, —C(O)NR3—, —C(?S)—NR3, —C(?NH)NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L is a divalent radical of formula -(Alk1)m(O)n(Alk2)p— wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X2-Q1- or -Q1-X2— wherein X2 is —O—, S— or NRA— wherein RA is hydrogen or optionally substituted C1-C3 alkyl, and Q1 is an optionally substituted divalent mono- or bicyclic carbocyclic or hetero-cyclic r
    Type: Application
    Filed: May 4, 2006
    Publication date: November 26, 2009
    Applicant: CHROMA THERAPEUTICS LTD.
    Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Moffat, Kenneth William John Baker, Alistair David Graham Donald
  • Publication number: 20090280483
    Abstract: The present invention provides methods for screening compounds which inhibit activation of a member of the IL-6 signaling pathways, comprising: (a) a positive screening step using a cell capable of being killed by IL-6 stimulation to select compounds which inhibit death of the cell when it is stimulated by IL-6; and then (b) a biochemical screening step to further select compounds which inhibit activation of a member of the IL-6 signaling pathways by a biochemical means from the compounds selected in step (a). The present invention also provides compounds which inhibit activation of a member of the IL-6 signaling pathways identified using said methods.
    Type: Application
    Filed: November 22, 2005
    Publication date: November 12, 2009
    Inventors: Toshio Kitamura, Toshiyuki Kawashima
  • Patent number: 7598417
    Abstract: The present patent application is directed to novel fluoroethyl urea compounds and compositions and their therapeutic use in the treatment of pain and other conditions.
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: October 6, 2009
    Assignee: Allergan, Inc.
    Inventors: Ken Chow, Wenkui K. Fang, Evelyn G. Corpuz, Daniel W. Gil, Michael E. Garst
  • Publication number: 20090186916
    Abstract: Provided is a compound that is an NMDA receptor antagonist having a broader safety margin, and is useful as an agent for treating or preventing Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, or pain. A novel compound or a salt thereof, which is characterized in that it has an amino group and R1 (lower alkyl, cycloalkyl, -lower alkylene-aryl, aryl which may be substituted, and the like) on carbon atoms of indane, cyclopenta[b]thiophene, cyclopenta[b]furan, cyclopenta[b]pyridine, or cyclopenta[c]pyridine ring, or 2,3-dihydrdo-1-benzofuran, 2,3-dihydrdo-1-benzothiophene, indoline ring, or the like, and has R2 and R3 (the same or different, each lower alkyl or aryl) on carbon atoms beside them, and an NMDA receptor antagonist comprising the same as an active component.
    Type: Application
    Filed: July 17, 2007
    Publication date: July 23, 2009
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Satoshi Hayashibe, Shingo Yamasaki, Kazushi Watanabe, Nobuyuki Shiraishi, Daisuke Suzuki, Hiroaki Hoshii, Junya Ohmori, Takatoshi Kanayama
  • Publication number: 20090156805
    Abstract: Novel cycloalkane carboxamide derivatives having an action that selectively inhibits cathepsin K, and a production process thereof, are provided. A cycloalkane carboxamide derivative represented by the following general formula (I), or a pharmaceutically acceptable salt thereof: (wherein R1 and R2 represent (substituted) alkyl groups, (substituted) alkenyl groups, (substituted) alkynyl groups, (substituted) aromatic hydrocarbon groups or (substituted) heterocyclic groups, ring A represents an alkylidene group having 5 to 7 carbon atoms, and ring B represents a formyl group or a hydroxymethyl group).
    Type: Application
    Filed: January 10, 2007
    Publication date: June 18, 2009
    Applicant: SEIKAGAKU CORPORATION
    Inventors: Nobuo Kobayashi, Tsuneo Koji, Hisatomo Kunii, Mizuho Kataoka
  • Publication number: 20090143411
    Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.
    Type: Application
    Filed: October 18, 2005
    Publication date: June 4, 2009
    Applicant: COMPASS PHARMACEUTICALS LLC
    Inventors: John Ward, Rama Jain, Donald R. James, Herman J. Verheij, Jan C.C. Schultz
  • Publication number: 20090137799
    Abstract: Cycloalkylcarbonylamino acid ester derivatives, which are raw material intermediates for a novel cycloalkane carboxamide derivative having an action that selectively inhibits cathepsin K, and a production process thereof, are provided. A cycloalkylcarbonylamino acid ester derivative represented by formula (I), or a pharmaceutically acceptable salt thereof: (wherein, R1 and R2 represent alkyl groups, alkenyl groups, alkynyl groups, aromatic hydrocarbon groups, heterocyclic groups, etc., R8 represents an alkyl group having 1 to 6 carbon atoms, and ring A represents a cyclic alkylidene group having 5, 6 or 7 carbon atoms).
    Type: Application
    Filed: January 10, 2007
    Publication date: May 28, 2009
    Applicant: SEIKAGAKU CORPORATION
    Inventors: Nobuo Kobayashi, Tsuneo Koji, Hisatomo Kunii
  • Publication number: 20090137659
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: August 15, 2008
    Publication date: May 28, 2009
    Applicant: CALCIMEDICA, INC.
    Inventors: Gonul VELICELEBI, Kenneth A. STAUDERMAN, David P.M. PLEYNET, Song CHENG, Jeffrey P. WHITTEN
  • Publication number: 20090105259
    Abstract: This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain acyclic diamines, which are agonists of TRPV4 channel receptors.
    Type: Application
    Filed: September 8, 2006
    Publication date: April 23, 2009
    Inventors: Jae U. Jeong, Robert W. Marquis
  • Publication number: 20090087409
    Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; represents either a single or a double bond; R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4; M is N or CR7, wherein R7 has the same definition as R4; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; and R6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het; or R6 is wherein R7 and R8 and Q are as defined herein; Y2 is O or S; R9 is H, (C1-6 alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl, aryl, Het, (C1-6)alkyl-aryl or (C1-6)alkyl-Het, al
    Type: Application
    Filed: November 26, 2008
    Publication date: April 2, 2009
    Applicant: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Pierre Louis Beaulieu, Gulrez Fazal, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos, Eric Jolicoeur, James Gillard, Marc-Andre Poupart, Jean Rancourt
  • Publication number: 20090082308
    Abstract: The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: April 14, 2006
    Publication date: March 26, 2009
    Inventors: Jed Lee Hubbs, Dawn M. Mampreian, Joey L. Methot, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
  • Publication number: 20090069391
    Abstract: The present invention relates to a novel class of hydroxamic acid derivatives. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: April 14, 2006
    Publication date: March 12, 2009
    Inventors: Jed Lee Hubbs, Sam Kattar, Joey Methot, Thomas Miller, Phieng Siliphaivanh, Matthew Stanton, Kevin Wilson, David J. Witter
  • Publication number: 20090062297
    Abstract: The present invention relates to a novel class of hydroxyalkylarylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: January 8, 2007
    Publication date: March 5, 2009
    Inventors: Richard W. Heidebrecht, Thomas A. Miller, Kevin J. Wilson, David J. Witter, Jonathan Grimm
  • Publication number: 20090048286
    Abstract: Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted bicyclic fused-thiophene compounds can inhibit PTP1B and thereby induce greater insulin sensitivity. Accordingly, PTP1B inhibition can provide an alternate treatment for PTPase-mediated disorders such as diabetes.
    Type: Application
    Filed: September 23, 2008
    Publication date: February 19, 2009
    Applicant: Wyeth
    Inventors: Jinbo Lee, Steven J. Kirincich, Michael J. Smith, Douglas P. Wilson, Bruce C. Follows, Zhao-Kui Wan, Diane M. Joseph-McCarthy, David V. Erbe, Yan-Ling Zhang, Weixin Xu, Steve Y. Tam
  • Publication number: 20090023799
    Abstract: The present invention provides crystal forms of (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)(4-chlorophenyl)methanone of the formula processes for the production of such crystal forms; pharmaceutical compositions comprising such crystal forms; and methods of treating diseases or conditions modulated by the adenosine A1 receptor, in particular neuropathic pain, in a mammal in need thereof, by employing such crystal forms, or pharmaceutical compositions comprising such.
    Type: Application
    Filed: July 18, 2008
    Publication date: January 22, 2009
    Inventors: George Laurence, Allan R. Moorman, Aeri Park
  • Publication number: 20090012075
    Abstract: The present invention relates to a novel class of fluorinated arylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: January 8, 2007
    Publication date: January 8, 2009
    Inventors: Thomas A. Miller, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
  • Publication number: 20080300294
    Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.
    Type: Application
    Filed: November 22, 2006
    Publication date: December 4, 2008
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jorg Velker
  • Publication number: 20080261952
    Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.
    Type: Application
    Filed: August 16, 2005
    Publication date: October 23, 2008
    Inventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Andrew Simon Swain, Phillppe Wong-Kai-In
  • Publication number: 20080221194
    Abstract: The invention relates to compounds of Formula (1) for use in modulating potassium channel activity in cells.
    Type: Application
    Filed: March 15, 2006
    Publication date: September 11, 2008
    Inventors: Andrew J. Harvey, Jonathan B. Baell, Heike Wulff
  • Patent number: 7417066
    Abstract: The invention relates to compounds of general Formula I, the production thereof, and the use thereof as a medicinal product.
    Type: Grant
    Filed: June 7, 2006
    Date of Patent: August 26, 2008
    Assignee: Schering AG
    Inventors: Bernd Buchmann, Martin Fritsch, Duy Nguyen, Bernd Menzenbach, Ulf Boemer
  • Patent number: 7417065
    Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.
    Type: Grant
    Filed: May 19, 2004
    Date of Patent: August 26, 2008
    Assignee: IRM LLC
    Inventors: Yuan Mi, Shifeng Pan, Nathanael Schiander Gray, Wenqi Gao, Yi Fan, Tao Jiang
  • Publication number: 20080193423
    Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened or hedgehog activity.
    Type: Application
    Filed: November 2, 2007
    Publication date: August 14, 2008
    Applicant: Curis, Inc.
    Inventors: Shirley Ann Brunton, Oivin M. Guicherit, Lawrence I. Kruse
  • Publication number: 20080182859
    Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened or hedgehog activity.
    Type: Application
    Filed: November 2, 2007
    Publication date: July 31, 2008
    Applicant: Curis, Inc.
    Inventors: Shirley Ann Brunton, Oivin M. Guicherit, Lawrence I. Kruse
  • Publication number: 20080176926
    Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.
    Type: Application
    Filed: March 20, 2006
    Publication date: July 24, 2008
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Jorg Velker, Thomas Weller
  • Publication number: 20080146632
    Abstract: The present invention provides compounds capable of binding to an Fc receptor and modulating Fc receptor activity comprising a core lipophilic group in the form of an Aryl zing substituted with a group rich in p-electrons. The invention further provides for a method of treating an autoimmune disease involving Fc receptor activity using such compounds. A method for obtaining a compound which modulates Fc receptor activity is also provided, the method comprising: (a) providing or designing compounds having structural characteristics to fit in the groove of the Fc?RIIa structure; and (b) screening the compounds for modulating activity on the Fc receptor.
    Type: Application
    Filed: February 1, 2008
    Publication date: June 19, 2008
    Applicant: TRILLIUM THERAPEUTICS, INC.
    Inventors: Mark Phillip Hogarth, Geoffrey Allan Pietersz, Gerard Peter Moloney
  • Publication number: 20080139547
    Abstract: The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
    Type: Application
    Filed: February 7, 2008
    Publication date: June 12, 2008
    Applicant: PHARMACYCLICS, INC.
    Inventor: Martin SENDZIK
  • Patent number: 7351735
    Abstract: This invention relates to novel benzofuran and benzothiophene derivatives of the general table formula and their use for the treatment of hyper-proliferative disorders
    Type: Grant
    Filed: February 21, 2003
    Date of Patent: April 1, 2008
    Assignee: Bayer Pharmaceuticals Corporation
    Inventors: Chengzhi Zhang, Michael Burke, Zhi Chen, Jacques Dumas, Dongping Fan, Jianmei Fan, Holia Hatoum-Mokdad, Benjamin D. Jones, Gaetan Ladouceur, Wendy Lee, Barton Phillips
  • Patent number: 7329765
    Abstract: Benzothiophene compounds such as are DNA binding compounds exhibiting antibacterial activity.
    Type: Grant
    Filed: November 30, 2004
    Date of Patent: February 12, 2008
    Assignee: GeneSoft Pharmaceuticals, Inc.
    Inventors: Roland W. Burli, Eldon E. Baird, Matthew J. Taylor, Jacob A. Kaizerman, Wenhao Hu
  • Patent number: 7300952
    Abstract: The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-? phosphorylation of I?B. In so doing these aminothiophene inhibitors block pathological activation of transcription factor NF-?B in which diseases excessive activation of NF-?B is implicated.
    Type: Grant
    Filed: May 29, 2003
    Date of Patent: November 27, 2007
    Assignee: SmithKline Beecham Corporation
    Inventors: James F. Callahan, Zehong Wan
  • Patent number: 7276612
    Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
    Type: Grant
    Filed: April 6, 2004
    Date of Patent: October 2, 2007
    Assignee: Pharmacyclics, Inc.
    Inventors: Eric J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
  • Patent number: 7271264
    Abstract: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl- 1-pyrrolidinyl, dimethyl-1-pyrrolidiny, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3 X is —S— or —HC?CH—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5 is —H or C1-C4 alkyl; and Y is —O—, —S—, —NH—, —NMe—, or —CH2—; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.
    Type: Grant
    Filed: July 18, 2003
    Date of Patent: September 18, 2007
    Assignee: Eli Lilly and Company
    Inventors: Ronald Jay Hinklin, Owen Brendan Wallace
  • Patent number: 7265130
    Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: December 30, 2003
    Date of Patent: September 4, 2007
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yasuyuki Kawanishi, Hideyuki Takenaka, Kohji Hanasaki, Tetsuo Okada
  • Patent number: 7208491
    Abstract: Mono-acylated o-phenylendiamines derivatives of formula I wherein X and R are as described herein, have been found useful for the treatment of diseases mediated by the inhibition of histone deacetylase, such as cancer.
    Type: Grant
    Filed: February 3, 2004
    Date of Patent: April 24, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
  • Patent number: 7144885
    Abstract: This invention relates to a novel fused tricyclic heterocycle of the formula (Ia, Ib) and its use for the treatment of hyper-proliferative disorders
    Type: Grant
    Filed: February 21, 2003
    Date of Patent: December 5, 2006
    Assignee: Bayer Pharmaceuticals Corporation
    Inventors: Chengzhi Zhang, Michael Burke, Zhi Chen, Jacques Dumas, Dongping Fan, Benjamin D. Jones, Gaetan Ladouceur, Wendy Lee, Barton Phillips, Scott M. Wilhelm, Qian Zhao
  • Patent number: 7141674
    Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:
    Type: Grant
    Filed: October 21, 2003
    Date of Patent: November 28, 2006
    Assignee: Johnson & Johnson Consumer Companies, Inc.
    Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
  • Patent number: 7138411
    Abstract: A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I? wherein X, A1, A2, A3, A4, R, R?, R1 and R2 are as described in the specification.
    Type: Grant
    Filed: November 22, 2002
    Date of Patent: November 21, 2006
    Assignee: G.D. Searle & Co.
    Inventors: Jeffery S Carter, Mark G Obukowicz, Balekudru Devadas, John J Talley, David L Brown, Matthew J Graneto, Stephen R Bertenshaw, Donald J Rogier, Jr., Srinivasan Raj Nagarajan, Cathleen E Hanau, Susan J Hartmann, Cindy L Ludwig, Suzanne Metz, Donald E Korte
  • Patent number: 7126012
    Abstract: The invention concerns compounds of formula (I): R-A-R? wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R? represents a —(CH2)t-R5 group wherein t and R5 are as defined in the description
    Type: Grant
    Filed: September 23, 2004
    Date of Patent: October 24, 2006
    Assignee: Les Laboratoires Servier
    Inventors: Daniel Lesieur, Frederique Klupsch, Gerald Guillaumet, Marie-Claude Viaud, Michel Langlois, Caroline Bennejean, Pierre Renaud, Philippe Delagrange
  • Patent number: 7115653
    Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as the compounds depicted in FIGS. 32 and 33. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.
    Type: Grant
    Filed: September 17, 2002
    Date of Patent: October 3, 2006
    Assignee: Curis, Inc.
    Inventors: Anthony David Baxter, Edward Andrew Boyd, Maria Frank-Kamenetsky, Oivin Guicherit, Jeffery Porter, Stephen Price, Lee L. Rubin, John Harry Alexander Stibbard
  • Patent number: 7105513
    Abstract: The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.
    Type: Grant
    Filed: July 31, 2003
    Date of Patent: September 12, 2006
    Assignee: Sanofi-Avertis Deutschland GmbH
    Inventors: Hartmut Strobel, Paulus Wohlfart