The Hetero Ring Contains Plural Nitrogens (e.g., 1,3-diazepines, Etc.) Patents (Class 540/553)
  • Patent number: 8940731
    Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: January 27, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: John M. Keith, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
  • Patent number: 8785628
    Abstract: A series of substituted [1,3,5]triazin-2-yl derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
    Type: Grant
    Filed: March 2, 2010
    Date of Patent: July 22, 2014
    Assignee: UCB Pharma, S.A.
    Inventors: Daniel Rees Allen, Roland Bürli, Alan Findlay Haughan, Jonathan David MacDonald, Mizio Matteucci, David John Nash, Andrew Pate Owens, Gilles Raphy, Elizabeth Anne Saville-Stones, Andrew Sharpe
  • Publication number: 20140163221
    Abstract: The invention relates to a process for the synthesis of cyclic alkylene ureas comprising reacting in the presence of a basic catalyst, a difunctional amine A having two primary amino groups, and an aliphatic organic carbonate component C selected from the group consisting of dialkyl carbonates CD and of alkylene carbonates CA, wherein the ratio of the amount of substance Ji(—NH2) of primary amino groups —NH2 in the difunctional amine A to the sum M(C) of the amount of substance n(CD) of carbonate groups of a dialkyl carbonate CD and the amount of substance n(CA) of carbonate groups in an alkylene carbonate CA, is at least more than 2, and to the product obtained by this process.
    Type: Application
    Filed: July 19, 2012
    Publication date: June 12, 2014
    Applicant: Allnex USA Inc.
    Inventors: Ram Gupta, Irina Kobylanska, Urvee Treasurer, Lawrence Flood
  • Patent number: 8637520
    Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
    Type: Grant
    Filed: July 1, 2010
    Date of Patent: January 28, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: John M. Keith, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
  • Patent number: 8603947
    Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: December 10, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
  • Patent number: 8563779
    Abstract: A description is given of (4-trifluoromethyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 19, 2011
    Date of Patent: October 22, 2013
    Assignee: Bayer CropScience AG
    Inventors: Hartmut Ahrens, Andreas Van Almsick, Elmar Gatzweiler, Dieter Feucht, Isolde Haeuser-Hahn, Stefan Lehr, Christopher Hugh Rosinger
  • Patent number: 8394789
    Abstract: The invention relates to 5,6-dihydropyrrolo[2,1-?]isoquinoline and pyrrolo[2,1-?]isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
    Type: Grant
    Filed: February 6, 2009
    Date of Patent: March 12, 2013
    Assignee: MSD Oss B.V.
    Inventors: Rachel Deborah van Rijn, Hubert Jan Josef Loozen, Cornelis Marius Timmers, Lars Anders van der Veen, Willem Frederik Johan Karstens
  • Patent number: 8362030
    Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.
    Type: Grant
    Filed: March 13, 2009
    Date of Patent: January 29, 2013
    Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti S.R.L.
    Inventors: Raffaele Ingenito, Philip Jones, Laura Llauger Bufi, Jesus Maria Ontoria Ontoria, Rita Scarpelli
  • Patent number: 8329900
    Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C?NR9; and each L, X, R1, R2, and R3 are as defined herein.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: December 11, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Zhiyuan Zhang, Bruce J. Elder, Paul K. Isbester, Grant J. Palmer, Jonathon S. Salsbury, Luckner G. Ulysse
  • Publication number: 20120270855
    Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.
    Type: Application
    Filed: April 25, 2012
    Publication date: October 25, 2012
    Inventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
  • Patent number: 8283354
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: August 31, 2005
    Date of Patent: October 9, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Dean Wilson, Andreas Termin, Jesus Gonzalez, Lev Fanning, Timothy Neubert, Paul Krenitsky, Pramod Joshi, Dennis Hurley, Urvi Sheth
  • Patent number: 8222243
    Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B 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 monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.
    Type: Grant
    Filed: August 26, 2008
    Date of Patent: July 17, 2012
    Assignee: Dart NeuroScience (Cayman) Ltd
    Inventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
  • Patent number: 8158628
    Abstract: Sulfonylated tetrahydroazolopyrazine compounds corresponding to the formula I wherein R1, R2a, R2b, R3a, R3b, R4, R8, R9a, R9b, R10, R11, A, B, W1, W2 and W3 have the meanings defined herein, pharmaceutical compositions containing such compounds, a method for the preparation of such compounds, and the use of such compounds for treating or inhibiting various types of pain and/or other conditions mediated at least in part by the bradykinin 1 receptor (B1R).
    Type: Grant
    Filed: March 4, 2010
    Date of Patent: April 17, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Beatrix Merla, Stefan Oberboersch, Melanie Reich, Stefan Schunk, Ruth Jostock, Sabine Hees, Michael Engels, Tieno Germann, Edward Bijsterveld
  • Patent number: 8048877
    Abstract: This invention relates to novel guanidine derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: March 22, 2007
    Date of Patent: November 1, 2011
    Assignee: Neurosearch A/S
    Inventors: Ulrik Svane Sørensen, Birgitte L. Eriksen, Lene Teuber, Dan Peters, Dorte Strøbæk, Tina Holm Johansen, Palle Christophersen
  • Publication number: 20110245156
    Abstract: Compounds are disclosed. Compositions that include the compounds are disclosed. Methods of making and using the compounds are also disclosed.
    Type: Application
    Filed: December 9, 2009
    Publication date: October 6, 2011
    Applicant: CYTOKINE PHARMASCIENCES, INC.
    Inventor: Thais M. Sielecki-Dzurdz
  • Publication number: 20110178292
    Abstract: The invention relates to an innovative method for synthesis of cyclic amidines. The synthesis starts from a ?-, ?- or ?-lactone which is twofold brominated. After esterification of the carboxyl function, the bromine atoms are nucleophilically substituted and the corresponding diamino compound is obtained. The ring closure to the cyclic amidine is accomplished subsequently by reaction with orthoester, imidate or thioimidate. Owing to interposing additional steps for recovery of the diamino compound in enantiomerically pure form, the enantiomers of the cyclic amidines can be stereoselectively synthesized.
    Type: Application
    Filed: July 16, 2009
    Publication date: July 21, 2011
    Inventors: George Lentzen, Thorsten Neuhaus
  • Patent number: 7947675
    Abstract: Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: February 16, 2006
    Date of Patent: May 24, 2011
    Assignee: Merck Patent GmbH
    Inventors: Bruno Roux, Isabelle Berard
  • Patent number: 7939523
    Abstract: Imidazolidinone and imidazolinethione compounds of formula (I): wherein R1, R2, R3, A1, A2, X, Y, Z, m, n, p, x, and y are defined herein. Also disclosed is a method of treating hepatitis C virus infection with these compounds.
    Type: Grant
    Filed: January 5, 2009
    Date of Patent: May 10, 2011
    Assignee: National Health Research Institutes
    Inventors: Jyh-Haur Chern, Tsu-An Hsu, Iou-Jiun Kang, Li-Wen Wang, Chung-Chi Lee, Yen-Chun Lee, Yen-Shian Wu, Sheng-Ju Hsu, Yueh Andrew Yueh, Yu-Sheng Chao
  • Publication number: 20110071139
    Abstract: This invention relates to novel compounds of the Formula (I), any of the formulas I1-I26 Ia1-3-Ij1-3 or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Application
    Filed: February 13, 2009
    Publication date: March 24, 2011
    Inventors: David A. Claremon, Linghang Zhuang, Yuanjieq Ye, Suresh B. Singh, Colin M. Tice, Robert D. Simpson
  • Patent number: 7879834
    Abstract: The present invention relates to spiroindoline modulators of muscarinic receptors. The present invention also provides compositions comprising such spiroindoline modulators, and methods therewith for treating muscarinic receptor mediated diseases.
    Type: Grant
    Filed: August 19, 2005
    Date of Patent: February 1, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Lewis R. Makings, Miguel Garcia-Guzman Blanco, Dennis R. Hurley, Ioana Drutu, Gabriel Raffai, Daniele J. Bergeron, Akiko Nakatani, Andreas P. Termin, Alina Silina
  • Publication number: 20100297034
    Abstract: The present invention relates to osmolyte-containing preparations for the local treatment of dry mucous membranes. It describes the use of osmolytes for the production of a medicament, medical product or cosmetic product for the prevention, therapy and/or care of dry mucous membranes. The present invention relates to topical compositions based on osmolytes to which sodium chloride and/or moisturizers can optionally be added. The group of osmolytes proposed by the invention embraces various low-molecular substances, in particular ectoine, homoectoine, hydroxyectoine, di-myo-inositol phosphate (DIP), cyclic 2,3-diphosphoglycerate (cDPG), 1,1-di-glycerol phosphate (DGP), ?-mannosylglycerate (Firoin), ?-mannosylglyceramide (Firoin-A), di-mannosyl di-inositol phosphate (DMIP), glucosylglycerol and/or a derivative, e.g. an acid, salt or ester, of these compounds.
    Type: Application
    Filed: October 29, 2008
    Publication date: November 25, 2010
    Applicant: BITOP AG
    Inventor: Hans Bernd Schmittmann
  • Patent number: 7777031
    Abstract: Processes are disclosed for making certain compounds of Formula (II): or their pharmaceutically active salts, that are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases. In one embodiment, the process comprises reacting a compound of formula (7-1): with a compound of formula (B3): in the presence of at least one equivalent of a first base, in a first organic solvent, to give a compound of Formula (II).
    Type: Grant
    Filed: May 25, 2007
    Date of Patent: August 17, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
  • Patent number: 7763602
    Abstract: Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).
    Type: Grant
    Filed: June 11, 2008
    Date of Patent: July 27, 2010
    Assignee: Lupin Limited
    Inventors: Sudershan Kumar Arora, Neelima Sinha, Sanjay Jain, Ram Shankar Upadhayaya, Gourhari Jana, Shankar Ajay, Rakesh Kumar Sinha
  • Patent number: 7750150
    Abstract: This invention relates to a method for preparing an acid addition salt of a polyacidic basic compound, or a water adduct having basic site(s) stronger than pyridine. The method comprises reacting the polyacidic basic compound with an acid salt of pyridine. By the present invention, the number of moles of an added acid in the acid addition salt of the polyacidic basic compound can be readily changed to a number suited for the polyacidic basic compound as needed.
    Type: Grant
    Filed: February 27, 2004
    Date of Patent: July 6, 2010
    Assignee: Kowa Co., Ltd.
    Inventors: Kimiyuki Shibuya, Tadaaki Ohgiya, Takayuki Matsuda
  • Publication number: 20100152168
    Abstract: The present invention relates to novel benzimidazolone derivatives of the general formula (I) in which the substituents R1, R2, R3, A1, A2, and B are as defined in claim 1, medicaments comprising these, and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent diseases.
    Type: Application
    Filed: August 24, 2007
    Publication date: June 17, 2010
    Applicant: ABBOTT GMBH & CO. KG
    Inventors: Torsten Arndt, Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Juliana Ruiz Caro
  • Patent number: 7737272
    Abstract: Transition metal complexes include a diazaphosphacycle of formula III and a transition metal. The phosphorus atom of the diazaphosphacycle is bonded to the transition metal and the diazaphosphacycle of formula III has the following structure where the variables have the values set forth herein.
    Type: Grant
    Filed: February 15, 2008
    Date of Patent: June 15, 2010
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Clark R. Landis, Wiechang Jin, Jonathan S. Owen, Thomas P. Clark
  • Patent number: 7691837
    Abstract: Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).
    Type: Grant
    Filed: September 20, 2002
    Date of Patent: April 6, 2010
    Assignee: Lupin Limited
    Inventors: Sudershan Kumar Arora, Neelima Sinha, Sanjay Jain, Ram Shankar Upadhayaya, Gourhari Jana, Shankar Ajay, Rakesh Kumar Sinha
  • Patent number: 7678785
    Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.
    Type: Grant
    Filed: July 24, 2007
    Date of Patent: March 16, 2010
    Assignee: UCB Pharma S.A.
    Inventors: Andrew David Carr, Judi Charlotte Neuss, Michael Glen Orchard, David William Porter
  • Patent number: 7674899
    Abstract: This invention relates to novel azacyclic derivatives and their use as pharmaceuticals. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Grant
    Filed: February 1, 2005
    Date of Patent: March 9, 2010
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen, Daniel B Timmermann
  • Patent number: 7674789
    Abstract: The present invention is directed to compounds of formula (I), (Ia),(Ic) and (Id), compositions, and uses thereof as an inhibitor of the p38 kinase, and wherein, inter alia R1 is C(Z)N(R10?)(CR10R20)vRb, C(Z)O(CR10R20)vRb, N(R10?)C(Z)(CR10R20)vRb; N(R10?)C(Z)N(R10?)(CR10R20)vRb; or N(R10?)OC(Z)(CR10R20)vRb; R3 is C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroarylC1-10 alkyl, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted; X is R2, OR2?, S(O)mR2?, (CH2)n?N(R10?)S(O)mR2?, (CH2)n?N(R10?)C(O)R2?, (CH2)n?NR4R14, (CH2)n?N(R2 ?)(R2?), or N(R10?)—Rh—NH—C(?N—CN)NRqRq?; and R2 is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 24, 2006
    Date of Patent: March 9, 2010
    Assignee: Glaxo Group Limited
    Inventors: James F. Callahan, Zehong Wan, Hongxing Yan, Xichen Lin
  • Publication number: 20100048578
    Abstract: Disclosed is a hydrazine compound represented by the formula (1) below, which has an excellent control activity against a harmful arthropod. (1) (In the formula, R1, R5, R6 and R7 represent a hydrogen atom or the like; R2 and R3 are bonded together at their ends to form a 5- to 8-membered ring together with two nitrogen atoms; R4 represents a halogen atom or the like; J represents 1-(3-chloro-2-pyridyl)-3-bromo-1H-pyrazol-5-yl group or the like; and M represents a hydrogen atom, an optionally halogenated C1-C6 alkyl group, or the like.
    Type: Application
    Filed: April 10, 2008
    Publication date: February 25, 2010
    Inventors: Markus Jachmann, Hiroshi Ikegami, Yoshihiko Nokura
  • Publication number: 20090233907
    Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE 4 mediated disease state.
    Type: Application
    Filed: March 20, 2007
    Publication date: September 17, 2009
    Applicant: ASTRAZENECA AB
    Inventors: Rupert Austin, Roger Victor Bonnert, Simon Fraser Hunt, Grigorios Nikitidis, Hitesh Jayantilal Sanganee, Peter Olof Sjo, Dan Warner
  • Patent number: 7557098
    Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
    Type: Grant
    Filed: August 20, 2007
    Date of Patent: July 7, 2009
    Assignee: Wyeth
    Inventors: Michael Gerard Kelly, Derek Cecil Cole
  • Publication number: 20090124604
    Abstract: The invention concerns a compound of the Formula (I) wherein m is 1-2 and each R1 is a group such as cyano, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is trifluoromethyl or (1-6C)alkyl; R3 is hydrogen or halogeno; and R4 is isoxazolyl; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
    Type: Application
    Filed: February 23, 2006
    Publication date: May 14, 2009
    Inventors: Ian Alun Nash, Jonathan Erle Finlayson, Caroline Rachel Thompson
  • Patent number: 7531543
    Abstract: The present invention is directed to phenylpiperazine cycloalkanol derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
    Type: Grant
    Filed: October 12, 2004
    Date of Patent: May 12, 2009
    Assignee: Wyeth
    Inventors: Paige Erin Mahaney, Eugene John Trybulski, Lori Krim Gavrin, An Thien Vu
  • Publication number: 20090093464
    Abstract: The present invention relates to naphthalene derivatives of formula (I) that are modulators of the glucocorticoid receptor, and to processes for the preparation and use of the same.
    Type: Application
    Filed: February 21, 2006
    Publication date: April 9, 2009
    Applicant: SMITHKLINE BEECHMA CORPORATION
    Inventors: Stephen William Rafferty, Philip Stewart Turnbull, Eugene Lee Stewart, Richard Dana Caldwell
  • Publication number: 20080319188
    Abstract: A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH?, nitrogen or the like.
    Type: Application
    Filed: August 23, 2006
    Publication date: December 25, 2008
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Tomohiro Matsushima, Keiko Takahashi, Setsuo Funasaka, Hiroshi Obaishi, Shuji Shirotori
  • Patent number: 7459552
    Abstract: The present invention is directed to a method for producing a cyclic diamine compound (3) or a salt thereof through the following scheme: (wherein Ar represents a phenyl group, a pyridyl group, or a pyrimidinyl group, any of which may have a substituent; X represents NH, S, or O; ring A represents a benzene ring or a pyridine ring, which may have a substituent; 1 represents an integer of 1 or 2; m represents an integer of 1 or 2; and n represents an integer of 1 to 6). The method enables synthesis of a cyclic diamine compound (3) or a salt thereof, which serves as an ACAT inhibitor, in an industrially useful manner.
    Type: Grant
    Filed: May 27, 2004
    Date of Patent: December 2, 2008
    Assignee: Kowa Co., Ltd.
    Inventors: Kimiyuki Shibuya, Tadaaki Ohgiya, Toru Miura
  • Patent number: 7371753
    Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups R1 to R5, Ra to Rc, W, Q1 and Q2 have the meanings given in the claims and specification, the isomers thereof and the use thereof for preparing a pharmaceutical composition for the treatment of diseases characterised by excessive or abnormal cell proliferation.
    Type: Grant
    Filed: August 25, 2005
    Date of Patent: May 13, 2008
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heinz Stadtmueller, Harald Engelhardt, Andreas Schoop, Martin Steegmaier, Matthias Hoffmann, Matthias Grauert
  • Patent number: 7365063
    Abstract: Compounds of the formula I: and pharmaceutically acceptable salts thereof wherein X is N, Y is S, Z is —(CRaRb)r—, A is —NR3, m is 2, n is 1, q is 2, R2 is optioinally substituted aryl or optionally substituted heteroaryl, and p, R1, R3, R4, R5, R6, R7, R8, R9, and R10, are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I for treatment of central nervous system diseases.
    Type: Grant
    Filed: February 7, 2007
    Date of Patent: April 29, 2008
    Assignee: Roche Palo Alto LLC
    Inventors: Nancy Elisabeth Krauss, Meng Sui, Shu-Hai Zhao
  • Patent number: 7348347
    Abstract: Substituted 4,5,6,7-tetrahydrobenzothiazol-2-ylamine compounds, a method for their production; pharmaceutical compositions comprising them, and methods of use for modulating biological functions and/or treating or inhibiting various medical conditions such as, e.g., depression and pain.
    Type: Grant
    Filed: August 11, 2006
    Date of Patent: March 25, 2008
    Assignee: Gruenenthal GmbH
    Inventors: Stefan Oberboersch, Corinna Sundermann, Bernd Sundermann, Edward Bijsterveld
  • Publication number: 20080051578
    Abstract: The present invention relates to compounds of general formula (I) wherein A, B, L, R1, R2, R3a and R3b are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Application
    Filed: August 24, 2006
    Publication date: February 28, 2008
    Inventors: Georg Dahmann, Kai Gerlach, Roland Pfau, Henning Priepke, Wolfgang Wienen, Annette Schuler-Metz, Herbert Nar
  • Patent number: 7312209
    Abstract: Compounds having the formula (I), wherein R3 is selected from H, OH and NH2; R30 is selected from ?O and ?S; W is —C(?O)—, —S(?O)—, or —S(O)2—; or W may be —CH2— if X is —C(?O)—; X is selected from —CH2—, —N(R4)—, and —O—, except that when W is —CH2—, X is —C(?O)—; Y is a bond or —C(R40)(R45)—; Q is a linker; Z is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl; and R1, R2, R24, and R25 are as defined in the specification.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: December 25, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Edwin J. Iwanowicz, Scott H. Watterson, Ping Chen, T. G. Murali Dhar, Henry H. Gu, Yufen Zhao
  • Patent number: 7268128
    Abstract: Pyrazolopyrimidinone derivatives expressed by the following general formula (IA) or (IB): where the symbols are as disclosed in the specification, are provided as desired compounds. These compounds selectively inhibiting PDE7, thereby increasing the intracellular cAMP level and inhibiting the activation of T cells. Thus, these compounds are useful for prevention and treatment of various allergic diseases and inflammatory or immunological diseases.
    Type: Grant
    Filed: June 14, 2004
    Date of Patent: September 11, 2007
    Assignee: Ausbio Pharma Co., Ltd.
    Inventors: Hidekazu Inoue, Hidenobu Murafuji, Yasuhiro Hayashi
  • Patent number: 7259159
    Abstract: The present invention relates to acylguanidino derivatives of formula (I), in which R1, R2, R3, A, B, X, Y and n have the meanings indicated in claim 1, their physiologically tolerable salts and their prodrugs. The compounds of the formula (I) are valuable pharmaceutically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and bone resorption by osteoclasts. This renders them suitable, for example, for the therapy and prophylaxis of illness which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth muscles.
    Type: Grant
    Filed: July 23, 2001
    Date of Patent: August 21, 2007
    Assignees: Sanofi-Aventis Deutschland GmbH, Genentech Inc.
    Inventors: Anuschirwan Peyman, David Will, Thomas R Gadek, Robert McDowell, Jean Francois Gourvest, Jean-Marie Ruxer, Jochen Knolle
  • Patent number: 7253169
    Abstract: The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities.
    Type: Grant
    Filed: April 17, 2001
    Date of Patent: August 7, 2007
    Assignee: Gliamed, Inc.
    Inventors: Yong-Qian Wu, Wei Huang, Gregory S. Hamilton
  • Patent number: 7223752
    Abstract: A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1–C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1–C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1–C6) lower alkoxy, (C1–C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1–C6) lower alkyl], —CON[(C1–C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1–C6) lower alkyl, halogen or (C1–C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1–C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1–C6) lower alkoxy, or (C1–C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1–C6) lower alkyl], —CON[(C1–C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturat
    Type: Grant
    Filed: November 4, 2004
    Date of Patent: May 29, 2007
    Assignee: Wyeth
    Inventors: Amedeo Arturo Failli, John P. Dusza, Thomas Joseph Caggiano, Jay Scott Shumsky, Kevin A. Memoli, Eugene J. Trybulski
  • Patent number: 7196108
    Abstract: The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis.
    Type: Grant
    Filed: March 6, 2003
    Date of Patent: March 27, 2007
    Assignees: Incyte San Diego Inc., Ortho McNeil Pharmaceutical Inc.
    Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul Giachino, Karine Jakubowicz-Jaillardon, Jianhua Guo, Richard M. Fine, Lyle W. Spruce, James W. Zapf
  • Patent number: RE41149
    Abstract: N1-(1,2-cis-2-halogenocyclopropyl)-substituted pyridonecarboxylic acid derivatives represented by the following formula (I) the terms of which are defined in the specification and the salts thereof are disclosed: These compounds have patent antibacterial activities against a wide variety of infectious bacteria and are useful as antibacterial agents by oral or parenteral administration.
    Type: Grant
    Filed: June 3, 2004
    Date of Patent: February 23, 2010
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Isao Hayakawa, Youichi Kimura
  • Patent number: RE44205
    Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted ?m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, ?phenyl-CH(OH)—, or phenyl-C(?NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing comp
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: May 7, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Bernard R. Neustadt, Neil Lindo, William J. Greenlee, Deen Tulshian, Lisa S. Silverman, Yan Xia, Craig D. Boyle, Samuel Chackalamannil