The Six-membered Hetero Ring And Another Ring Bonded Directly To The Same Carbon Patents (Class 546/333)
  • Patent number: 9638690
    Abstract: This invention provides compound having a structure of Formula I: Uses of such compounds and compositions comprising the compounds as alkylating agent sensors.
    Type: Grant
    Filed: October 30, 2015
    Date of Patent: May 2, 2017
    Assignee: THE UNIVERSITY OF BRITISH COLUMBIA
    Inventors: Jennifer Ann Love, Philip Andrew Provencher
  • Patent number: 8987465
    Abstract: A compound of formula (I) (I), wherein R1 to R4 are, for example, each hydrogen, R5 is pyridyl, which has one or more substituents at least one of which is, for example, a 5 membered heterocycle; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 are, independently selected, from, for example, N, and C—H; and its use as a pesticidal agent.
    Type: Grant
    Filed: October 31, 2012
    Date of Patent: March 24, 2015
    Assignee: Syngenta Participation AG
    Inventors: Thomas Pitterna, Olivier Loiseleur, Anthony Cornelius O'Sullivan, Torsten Luksch
  • Patent number: 8883850
    Abstract: The present invention is directed to naphthalene carboxamide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimers disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: May 23, 2011
    Date of Patent: November 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Douglas C. Beshore, Christina Ng DiMarco, Scott D. Kukuk
  • Publication number: 20140288040
    Abstract: The invention provides compounds of the formula (6): or a salt, N-oxide or tautomer thereof, wherein A is CH, CF or nitrogen; E is CH, CF or nitrogen; and R0 is hydrogen or C1-2 alkyl; R1a is selected from CONH2; CO2H; an optionally substituted acyclic C1-8 hydrocarbon group; and an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1, 2, 3 or 4 are heteroatom ring members selected from O, N and S; R2 is selected from hydrogen and a group R2a; R2a is selected from an optionally substituted acyclic C1-8 hydrocarbon group; an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1 or 2 ring members are heteroatom ring members selected from O, N and S; and an optionally substituted bicyclic heterocyclic group of 9 or 10 ring members, of which 1 or 2 ring members are nitrogen atoms; wherein at least one of R1 and R2 is other than hydrogen; R3 is an optionally substituted 3- to 10-membered monocyclic or bicyc
    Type: Application
    Filed: October 31, 2012
    Publication date: September 25, 2014
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Andrew James Woodhead, Gianni Chessari, Gilbert Ebai Besong, Maria Grazia Carr, Steven Douglas Hiscock, Michael Alistair O'Brien, David Charles Rees, Susanne Maria Saalau-Bethell, Hendrika Maria Gerarda Willems, Neil Thomas Thompson
  • Publication number: 20140221286
    Abstract: It is discovered that sodium-channel blockers inhibit the secretion of glucagon from pancreatic alpha cells. The present disclosure, based on such discoveries, provides compositions and methods for the treatment of hyperglycemia and related diseases and conditions with Na-channel blockers.
    Type: Application
    Filed: September 20, 2012
    Publication date: August 7, 2014
    Inventors: Luiz Belardinelli, Arvinder Dhalla
  • Publication number: 20140171639
    Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: February 24, 2014
    Publication date: June 19, 2014
    Applicant: AMGEN INC.
    Inventors: Kaustav Biswas, James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Vu Van Ma, Holger Monenschein, Thomas T. Nguyen, David J. St. Jean, JR., Chester Chenguang Yuan, Wenge Zhong
  • Publication number: 20140148487
    Abstract: The present invention is directed to compositions useful for antimicrobial applications. These compositions comprise amphiphilic compounds.
    Type: Application
    Filed: October 20, 2011
    Publication date: May 29, 2014
    Applicant: James Madison Innovations, Inc,
    Inventors: Kevin P. Minbiole, Kevin l Caren, Kyle n Seifert
  • Publication number: 20140128408
    Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
    Type: Application
    Filed: January 31, 2012
    Publication date: May 8, 2014
    Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Alan Kozikowski, Jay H. Kalin, Kyle V. Butier, Joel Bergman, Wayne W. Hancock
  • Publication number: 20140100371
    Abstract: A process for preparing azomethines of the general formula (V) where R is an optionally substituted carbocyclic aromatic radical having 6 to 24 carbon atoms or an optionally substituted alkyl radical or an optionally substituted heteroaromatic radical having 5 to 24 carbon atoms, and R1 is an optionally substituted carbocyclic aromatic radical having 6 to 24 carbon atoms or an optionally substituted heteroaromatic radical having 5 to 24 carbon atoms, R2 is hydrogen or an optionally substituted carbocyclic aromatic radical having 6 to 24 carbon atoms or an optionally substituted alkyl radical or an optionally substituted cycloalkyl radical N or an optionally substituted heteroaromatic radical having 5 to 24 carbon atoms by reacting alpha-oxo carboxylates of the general formula (I) where n is a number in the range from 1 to 6, M(n+) is a cation, with aryl bromides of the general formula (IV) and amines of the general formula (II) via the alpha-iminocarboxylate intermediate of the general formula (III), in the p
    Type: Application
    Filed: November 18, 2011
    Publication date: April 10, 2014
    Applicant: Saltigo GmbH
    Inventors: Alain Cotte, Matthias Cotta, Felix Rudolph, Bingrui Song, Lukas Goossen
  • Publication number: 20140094492
    Abstract: Derivatives of sulindac that lack cyclooxygenase inhibitory activity are provided along with pharmaceutical compositions containing them and use for treatment or prevention of cancer. The derivatives of sulindac are also suitable for treating chronic inflammatory conditions. A method for preparing the derivatives is also provided.
    Type: Application
    Filed: March 30, 2012
    Publication date: April 3, 2014
    Applicant: Southern Research Institute
    Inventors: Robert Reynolds, Bini Mathew, Gary A. Piazza
  • Publication number: 20130252947
    Abstract: The present disclosure relates to a method to stimulate endogenous BMP-2 up-regulation in a subject which method comprises administering to a subject an effective amount of an H1 receptor antagonist, whereby endogenous BMP-2 up-regulation is stimulated in said subject. Also provided is a pharmaceutical formulation including an H1 receptor antagonist present in an effective amount to stimulate BMP-2 up-regulation in a subject and a kit.
    Type: Application
    Filed: May 17, 2013
    Publication date: September 26, 2013
    Applicant: Southwest Research Institute
    Inventor: Jorge Gianny ROSSINI
  • Publication number: 20130225643
    Abstract: It relates to an endogenous repair factor production accelerator which comprises one or at least two selected from prostaglandin (PG) I2 agonist, EP2 agonist and EP4 agonist. Since prostaglandin (PG) I2 agonist, EP2 agonist or EP4 agonist has various endogenous repair factor production accelerating action, angiogenesis acceleration action and stem cell differentiation induction action, it is useful as preventive and/or therapeutic agents for ischemic organ diseases (e.g., arteriosclerosis obliterans, Buerger disease, Raynaud disease, myocardial infarction, angina pectoris, diabetic neuropathy, spinal canal stenosis, cerebrovascular accidents, cerebral infarction, pulmonary hypertension, bone fracture, Alzheimer disease, etc.) and various cell and organ diseases.
    Type: Application
    Filed: April 4, 2013
    Publication date: August 29, 2013
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventor: ONO PHARMACEUTICAL CO., LTD.
  • Publication number: 20130059860
    Abstract: The present invention is directed to naphthalene carboxamide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimers disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: May 23, 2011
    Publication date: March 7, 2013
    Inventors: Douglas C. Beshore, Chirstina Ng Dimarco, Scott D. Kuduk
  • Publication number: 20120270885
    Abstract: The use of a compound of formula I Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; the ring is a 6 membered aromatic ring or is a 5 or 6 membered heteroaromatic ring; Z and Z? are provided that both are not N; R1, R2, R3, R3a, R4, R8 and Ra are specified organic groups and n and p are independently 0, 1, 2, 3 or 4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.
    Type: Application
    Filed: February 10, 2012
    Publication date: October 25, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Peter Maienfisch, Louis-Pierre Molleyres, Jérôme Cassayre, Fredrik Cederbaum, Camilla Corsi, Thomas Pitterna
  • Publication number: 20120101097
    Abstract: The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases.
    Type: Application
    Filed: March 10, 2011
    Publication date: April 26, 2012
    Inventors: Solomon Ungashe, John Jessen Wright, Andrew Pennell
  • Publication number: 20120101327
    Abstract: The present invention concerns an apparatus and a method for stimulating brain tissue with pulsed electromagnetic fields weaker than the limit for elicitation of the action potentials of the cells of the tissue to be stimulated, the apparatus comprising: at least one electrically conducting coil positioned at a bitemporal position such that hippocampus is stimulated by at least one magnetic field upon supplying a pulse to said coil as well as a coil positioned at a occipital and parietal position; and a pulse generation means operationally connected to said at least one coil for supplying a series of current pulses for conduction, allowing generation of pulsed electromagnetic fields sufficiently strong to cause protein activation, and weaker than the limit for elicitation of the action potentials of the cells of the tissue to be stimulated.
    Type: Application
    Filed: June 22, 2010
    Publication date: April 26, 2012
    Inventors: Steen Dissing, Mogens Unden
  • Publication number: 20110245493
    Abstract: The present invention relates to the delivery of drug amines through an inhalation route. Specifically, it relates to aerosols containing drug amines that are used in inhalation therapy. In one aspect of the present invention, a method of delivering an amine drug in an aerosol form is provided. The method comprises: a) heating a coating, which includes an amine drug salt on a substrate contained in a device to a temperature sufficient to volatilize the amine drug from the coating, h) by said heating, forming an amine drug vapor, and c) during said heating, drawing air through said device, condensing said vapor to form aerosol particles containing less than 10% degradation products of the compound.
    Type: Application
    Filed: April 1, 2011
    Publication date: October 6, 2011
    Applicant: ALEXZA PHARMACEUTICALS, INC.
    Inventors: Joshua D. RABINOWITZ, Alejandro C. Zaffaroni
  • Publication number: 20110201610
    Abstract: The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases.
    Type: Application
    Filed: March 10, 2011
    Publication date: August 18, 2011
    Inventors: Solomon Ungashe, John Jessen Wright, Andrew Pennell
  • Patent number: 7994329
    Abstract: Compounds that are ligands for the growth hormone secretagogue receptor type 1A (GHS-R 1A), as well as pharmaceutically acceptable salts of such compounds, are useful for the manufacture of medicaments for the regulation of food intake.
    Type: Grant
    Filed: June 19, 2006
    Date of Patent: August 9, 2011
    Assignee: Helsinn Therapeutics (U.S.), Inc.
    Inventor: Michael Ankerson
  • Publication number: 20110098431
    Abstract: This invention relates to Group 4 dialkyl compounds supported by a pyridyl-amido-aryl (“PAA”), an anisole-amido-aryl (“AAA”), a phenoxy-amido-pyridyl (“PAPY”), an anisole-amido-phenoxy (“AAP”) or a anisole-amido-phenoxy (“AAP”) tridentate ligand. Such compounds can polymerize olefins, such as ethylene.
    Type: Application
    Filed: October 20, 2010
    Publication date: April 28, 2011
    Inventors: Garth R. GIESBRECHT, Timothy M. Boller, Alexander Z. Voskoboynikov, Andrey F. Asachenko, Mikhail V. Nikulin, Alexey A. Tsarev
  • Patent number: 7932252
    Abstract: The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases.
    Type: Grant
    Filed: May 12, 2005
    Date of Patent: April 26, 2011
    Assignee: ChemoCentryx, Inc.
    Inventors: Solomon Ungashe, John Jessen Wright, Andrew Pennell
  • Publication number: 20100298122
    Abstract: The present invention discloses single site catalyst systems having anionic scorpion-like three dimensional structure, that are suitable for oligomerising or polymerising ethylene and alpha-olefins.
    Type: Application
    Filed: November 9, 2007
    Publication date: November 25, 2010
    Applicant: TOTAL PETROCHEMICALS RESEARCH FELUY
    Inventors: Guillaume Michaud, Caroline Hillairet, Sabine Sirol
  • Patent number: 7829587
    Abstract: Substituted 2-aminotetralin derivatives as selective alpha 2B agonists can be incorporated in a pharmaceutical composition and can be used in methods of treating an alpha 2B receptor mediated diseases or conditions. The compounds are represented by Formula 1: wherein R1=H, methyl, ethyl, propyl, or cyclobutyl; R2=methyl or H; R3=pyridinyl X=C or O.
    Type: Grant
    Filed: January 9, 2008
    Date of Patent: November 9, 2010
    Assignee: Allergan, Inc.
    Inventors: John R. Cappiello, Dario G. Gomez, Ken Chow, Michael E. Garst, Daniel W. Gil, Larry A. Wheeler
  • Publication number: 20100280074
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: December 3, 2009
    Publication date: November 4, 2010
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
  • Patent number: 7799824
    Abstract: Quaternary salt compounds of Formula (I) or pharmaceutically acceptable forms thereof, which are CCR2 antagonists and are useful in preventing, treating or ameliorating CCR2 mediated inflammatory syndromes, disorders or diseases in a subject in need thereof.
    Type: Grant
    Filed: June 22, 2005
    Date of Patent: September 21, 2010
    Assignee: OraPharma, Inc.
    Inventors: Bharat Lagu, Michael Wachter
  • Publication number: 20100041717
    Abstract: Compounds of formula (Ia) and (Ib), wherein A, B, C, R1and R14 are described herein.
    Type: Application
    Filed: November 28, 2007
    Publication date: February 18, 2010
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Mark E. Salvati, James A. Johnson, Ningning Xu
  • Patent number: 7629367
    Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner.
    Type: Grant
    Filed: June 3, 2005
    Date of Patent: December 8, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Barbara Hanney, Yuntae Kim, Michael R. Krout, Robert S. Meissner, Helen J. Mitchell, Jeffrey Musselman, James J. Perkins, Jiabing Wang
  • Publication number: 20090253684
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, COPD.
    Type: Application
    Filed: December 2, 2008
    Publication date: October 8, 2009
    Inventors: Romyr Dominique, Robert Alan Goodnow, JR., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
  • Patent number: 7488848
    Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
    Type: Grant
    Filed: March 17, 2006
    Date of Patent: February 10, 2009
    Assignee: Virobay, Inc.
    Inventors: Michael Graupe, John O. Link, Michael G. Roepel
  • Publication number: 20090023735
    Abstract: The invention relates to sulphonamide derivatives of formula (I), where RC is selected from a group consisting of dialkylamino, NO2, CN, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkanoyl, oxazol-2-yl, oxazolylaminocarbonyl, aryl, aroyl, aryl-CH(OH)—, arylaminocarbonyl, furanyl, where the aryl, aroyl and furanyl moieties may be substituted, guanidinyl-(CH2)z—N(R?)—, Het-(CH2)z—N(R?)—, Het-CO—N(R?)—, Het-CH(OH)— and Het-CO—, where Het is an optionally substituted 4-6-membered heterocyclic ring containing one or more heteroatoms sleeted from N, S and O, R? is hydrogen or alkyl, and z is an integer 1 to 5; RA is a group of formula (A), (B), (C) or (D) as defined in the claims; and RB is hydrogen, alkyl, alkanoyl, hydroxyalkyl, alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, aminoalkyl, mono- or dialkylaminoalkyl or Het-alkyl, where Het is as defined above.
    Type: Application
    Filed: September 15, 2006
    Publication date: January 22, 2009
    Inventors: Jyrki Heino, Mark Johnson, Jarmo Kapyla, Anne Marjamaki, Tommi Nyronen, Marika Ojala, Olli Pentikainen, Marjo Pihlavisto, Liisa Nissinen
  • Publication number: 20080299089
    Abstract: It relates to an endogenous repair factor production accelerator which comprises one or at least two selected from prostaglandin (PG) 12 agonist, EP2 agonist and EP4 agonist. Since prostaglandin (PG) 12 agonist, EP2 agonist or EP4 agonist has various endogenous repair factor production accelerating action, angiogenesis acceleration action and stem cell differentiation induction action, it is useful as preventive and/or therapeutic agents for ischemic organ diseases (e.g., arteriosclerosis obliterans, Buerger disease, Raynaud disease, myocardial infarction, angina pectoris, diabetic neuropathy, spinal canal stenosis, cerebrovascular accidents, cerebral infarction, pulmonary hypertension, bone fracture, Alzheimer disease, etc.) and various cell and organ diseases.
    Type: Application
    Filed: February 20, 2008
    Publication date: December 4, 2008
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Yoshiki SAKAI, Akio Nishiura, Teppei Ogata
  • Publication number: 20080221175
    Abstract: The present invention provides N-cyclohexyl benzamide and benzeneacetamide compounds according to formula (I): where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, m, n, p, and q are as defined in the description; as well as pharmaceutical compositions comprising the same, methods of use of the compounds and compositions of the invention for the treatment of conditions associated with hydroxysteroid dehydrogenases (e.g., 11?-HSD1), and the use of the compounds of the invention in the preparation of medicaments for the treatment of hydroxysteroid dehydrogenase-associated conditions.
    Type: Application
    Filed: December 12, 2007
    Publication date: September 11, 2008
    Inventors: Chester Chenguang Yuan, Nianhe Han, Qingyian Liu, Dustin McMinn, Jay Powers
  • Publication number: 20080125468
    Abstract: The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
    Type: Application
    Filed: May 13, 2005
    Publication date: May 29, 2008
    Inventors: Mark Donald Chappell, Scott Eugene Conner, Isabel Cristina Gonzalez Valcarcel, Jason Eric Lamar, Jianke Li, Julie Sue Moyers, Rebecca Anne Owens, Allie Edward Tripp, Guoxin Zhu
  • Patent number: 7332608
    Abstract: The present invention is related to a process for preparing anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).
    Type: Grant
    Filed: November 9, 2006
    Date of Patent: February 19, 2008
    Assignee: SANOFI-AVENTIS Deutschland GmbH
    Inventors: Joachim Brendel, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
  • Patent number: 7268153
    Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner.
    Type: Grant
    Filed: June 3, 2005
    Date of Patent: September 11, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Barbara Hanney, Yuntae Kim, Michael R. Krout, Robert S. Meissner, Helen J. Mitchell, Jeffrey Musselman, James J. Perkins, Jiabing Wang
  • Patent number: 7235690
    Abstract: The present invention is related to anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: June 26, 2007
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Joachim Brendel, Bernard Pirard, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
  • Patent number: 7230018
    Abstract: Substituted propane-1,3-diamine derivatives, methods for producing such derivatives, and medicaments and pharmaceutical compositions containing such derivatives useful for the treatment or prophylaxis of pain, urinary incontinence, itching, tinitus aurium, or diarrhea are provided.
    Type: Grant
    Filed: August 21, 2003
    Date of Patent: June 12, 2007
    Assignee: Gruenenthal GmbH
    Inventors: Bernd Sundermann, Helmut Buschmann, Babette-Yvonne Koegel, Beatrix Merla, Nikolaus Risch
  • Patent number: 7205305
    Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
    Type: Grant
    Filed: July 17, 2003
    Date of Patent: April 17, 2007
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Guy W Bemis, Francesco G Salituro, John P Duffy, John E Cochran, Edmund M Harrington, Mark A Murcko, Keith P Wilson, Michael Su, Vincent P Galullo
  • Patent number: 7071358
    Abstract: Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases.
    Type: Grant
    Filed: January 29, 2003
    Date of Patent: July 4, 2006
    Assignee: Amgen Inc.
    Inventors: Xian Yun Jiao, Frank Kayser, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
  • Patent number: 6953811
    Abstract: A description is given of compounds of the formula in which R1 and R2 independently of one another are halogen, C1-C6alkyl, halo-C1-C6alkyl, C1-C6alkoxy, halo-C1-C6alkoxy, or SF5, R3 is hydrogen, OH, halogen, C1-C6alkoxy or —O—C(?O)—C1-C6alkyl, R4 is for example hydrogen, halogen, C1-C6alkyl, halo-C1-C6alkyl, C1-C6alkoxy, halo-C1-C6alkoxy or SCN; R5 and R6 independently of one another are for example hydrogen, C1-C12alkyl, halo-C1-C12alkyl, C2-C12alkenyl, halo-C2-C12alkenyl or C2-C12alkynyl; and q is 0 or 1; and, where appropriate, E/Z isomers, E/Z isomer mixtures and/or tautomers, each in free form or in salt form; a process for the preparation of these compounds and their use, pesticide compositions whose active ingredient is selected from these compounds, or an agrochemically useable salt thereof, a process for preparing these compositions, and their use, plant propagation material treated with these compositions, and a method of combating pests.
    Type: Grant
    Filed: February 4, 2002
    Date of Patent: October 11, 2005
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Stephan Trah, Josef Ehrenfreund, Peter Maienfisch, André Jeanguenat, Saleem Farooq
  • Patent number: 6881744
    Abstract: The invention pertains to carbinoxamine tannate and to a method for preparing carbinoxamine tannate by reacting carbinoxamine free base at a temperature of about 50 to about 150° C. with tannic acid neat or as an aqueous slurry containing about 5 to about 30 wt. % water.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: April 19, 2005
    Assignee: Jame Fine Chemicals, Inc.
    Inventors: Sham N. Redkar, Dina Donatiello, Timothy N. Truong, Vilas M. Chopdekar
  • Patent number: 6638940
    Abstract: Compounds of formula are described, wherein R1 and R2 are for example, independently of each other, halogen, C1-C6-alkyl, C3-C6-cycloalkyl, halogen-C1-C6-alkyl, halogen-C3-C6-cycloalkyl, C2-C4-alkenyl, C2-C4-alkinyl, halogen-C2-C4-alkenyl and halogen-C2-C4-alkinyl; R3 is hydrogen, OH, halogen, C1-C6-alkoxy, or —O—C(═O)—C1-C6-alkyl; R4 is for example phenyl, benzyl, phenoxy or benzyloxy, which is substituted by substituents selected from the group consisting of halogen, cyano, NO2, C1-C6-alkyl, C3-C8-cycloalkyl, C3-C8-cyclalkyl-C1-C6-alkyl, halogen-C1-C6-alkyl, C1-C6-alkoxy, C3-C8-cycloalkoxy, C3-C8-cycloalkoxy-C1-C6-alkyl, C3-C8-cycloalkoxy-C1-C6-alkoxy, halogen-C1-C6-alkoxy, C2-C4-alkenyl, C2-C4-alkinyl, halogen-C2-C4-alkenyl, halogen-C2-C4-alkinyl, C2-C6-alkenyloxy, C2-C6-alkinyloxy, halogen-C2-C6-alkenyloxy, halogen-C2-C6-alkenyloxy, —NR6—C(═O)—O—C1-C6-alkyl, —NR6—C(═O)—O-halogen-C1-C6-alkyl, —C(R7)═N&
    Type: Grant
    Filed: February 25, 2002
    Date of Patent: October 28, 2003
    Assignee: Syngenta Crop Protection, Inc.
    Inventor: Stephan Trah
  • Patent number: 6632823
    Abstract: In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of modulating acetylcholine receptors. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: October 14, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Jean-Michel Vernier, Nicholas D. P. Cosford, Ian A. McDonald
  • Patent number: 6610854
    Abstract: Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes are useful for inducing or promoting apotosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasias, including precancerous and cancerous lesions.
    Type: Grant
    Filed: July 26, 2002
    Date of Patent: August 26, 2003
    Assignees: Cell Pathways, Inc., University of Arizona
    Inventors: Gerhard J. Sperl, Paul Gross, Klaus Brendel, Gary A. Piazza, Rifat Pamukcu
  • Patent number: 6608060
    Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
    Type: Grant
    Filed: June 14, 1999
    Date of Patent: August 19, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Guy W. Bemis, Francesco Gerald Salituro, John Patrick Duffy, John E. Cochran, Edmund Martin Harrington, Mark A. Murko, Keith P. Wilson, Michael Su, Vincent P. Galullo
  • Patent number: 6545160
    Abstract: Disclosed are compounds which bind &agr;4&bgr;7 integrin. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by &agr;4&bgr;7 integrin. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: May 20, 2002
    Date of Patent: April 8, 2003
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett
  • Patent number: 6503905
    Abstract: The present invention relates to compounds of the formula I, wherein Z1, Z2, X, Q, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.
    Type: Grant
    Filed: August 6, 1999
    Date of Patent: January 7, 2003
    Assignee: Pfizer Inc
    Inventors: Spiros Liras, Martin P. Allen, Barbara E. Segelstein
  • Patent number: 6432990
    Abstract: The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds with polyether substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of the 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds as the active ingredient.
    Type: Grant
    Filed: January 30, 2002
    Date of Patent: August 13, 2002
    Assignee: Dow AgroSciences LLC
    Inventors: Emily J. Canada, Carl P. Denny, Christopher S. Galka, Neil V. Kirby, Marc McKennon, Mary E. Pieczko, Rebecca L. Rezac, Brent J. Rieder, John K. Swayze, Chrislyn M. Carson, David D. Johnson, Gregory M. Kemmitt
  • Patent number: 6426349
    Abstract: Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes are useful for inducing or promoting apotosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasias, including precancerous and cancerous lesions.
    Type: Grant
    Filed: December 20, 2000
    Date of Patent: July 30, 2002
    Assignee: Cell Pathway and the University of Arizona
    Inventors: Gerhard J. Sperl, Paul Gross, Klaus Brendel, Gary A. Piazza, Rifat Pamukeu
  • Patent number: 6410781
    Abstract: Disclosed are compounds which bind &agr;4&bgr;7 integrin. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by &agr;4&bgr;7 integrin. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: February 28, 2000
    Date of Patent: June 25, 2002
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett