Nitrogen Or Chalcogen Attached Indirectly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/214)
  • Patent number: 9890149
    Abstract: A compound having the structure of Formula II, or a stereoisomer, tautomer, or a pharmaceutically acceptable salt thereof: The compound is useful as CFTR modulator. Further, a method of using the compound and pharmaceutical composition comprising the compound are provided for treating diseases in lungs, pancreas, gastrointestinal system, sinuses, reproductive system, and the sweat glands.
    Type: Grant
    Filed: October 6, 2016
    Date of Patent: February 13, 2018
    Assignee: NuBridge BioSciences
    Inventors: Lin Zhang, Yu Ge
  • Publication number: 20150099728
    Abstract: Substituted phenylureas and phenylamides, processes for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for preparing pharmaceutical compositions.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Inventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM, Derek SAUNDERS, Hannelore STOCKHAUSEN
  • Publication number: 20150099786
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Patent number: 8987265
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof, as well as compositions containing these compounds, have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV:
    Type: Grant
    Filed: November 7, 2013
    Date of Patent: March 24, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Zhiwei Yin, Paul Michael Scola
  • Patent number: 8969584
    Abstract: A Pim kinase inhibitor compound having the structure represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts thereof. The compounds significantly inhibit Pim kinase activity and can be used to prepare drugs for treating Pim kinase mediated diseases, such as cancers, autoimmune diseases, allergic reactions, or organ transplant rejection. Also provided are methods for preparing the compounds represented by Formula I.
    Type: Grant
    Filed: February 10, 2014
    Date of Patent: March 3, 2015
    Assignee: Jikai Biosciences, Inc.
    Inventor: Yu Ge
  • Patent number: 8969583
    Abstract: This invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R, R1, R2, R3, n, X1, X2, L1, and L2 are as defined herein. The compounds of Formula I are useful as receptor tyrosine kinase (RTK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases.
    Type: Grant
    Filed: December 27, 2012
    Date of Patent: March 3, 2015
    Assignee: Allergan, Inc.
    Inventors: Thomas C. Malone, C. Eugene Hull, Sougato Boral, Julie A. Wurster, Michael R. Robinson, Jeffrey L. Edelman
  • Publication number: 20150051199
    Abstract: The invention provides compounds that are useful in the treatment of hepatitis C virus (HCV) infections.
    Type: Application
    Filed: October 31, 2012
    Publication date: February 19, 2015
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Andrew James Woodhead, Christopher Charles Frederick Hamlett, Gilbert Ebai Besong, Gianni Chessari, Maria Grazia Carr, Alessia Millemaggi, David Norton, Susanne Maria Saalau-Bethell, Hendrika Maria Gerarda Willems, Neil Thomas Thompson, Steven Douglas Hiscock
  • Patent number: 8946204
    Abstract: Substituted phenylureas and phenylamides, processes for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for preparing pharmaceutical compositions.
    Type: Grant
    Filed: November 9, 2011
    Date of Patent: February 3, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Nils Damann, Sven Frormann, Bernhard Lesch, Derek John Saunders, Jeewoo Lee, Yong-Soo Kim, Myeong-Seop Kim, Hannelore Stockhausen
  • Publication number: 20150011592
    Abstract: The invention relates to substituted phenylureas and phenylamides, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.
    Type: Application
    Filed: October 24, 2013
    Publication date: January 8, 2015
    Applicant: Gruenenthal GmbH
    Inventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM, Derek SAUNDERS, Hannelore STOCKHAUSEN
  • Publication number: 20150011394
    Abstract: The present invention relates to the use of host defense inducers for controlling selected bacterial harmful organisms in useful plants, wherein the bacterial harmful organisms are selected from the group consisting of Acidovorax avenae, Burkholderia spec., Burkholderia glumae, Candidatus Liberibacter spec., Corynebacterium, Erwinia spec., Pseudomonas syringae, Pseudomonas syringae pv. actinidae, Pseudomonas syringae pv. glycinea, Pseudomonas syringae pv. tomato, Pseudomonas syringae pv. lachrymans, Streptomyces spp., Xanthomonas spp., Xanthomonas axonopodis, Xanthomonas axonopodis pv. citri, Xanthomonas axonopodis pv. glycines, Xanthomonas campestris, Xanthomonas campestris pv. musacearum, Xanthomonas campestris pv. pruni, Xanthomonas fragariae and Xanthomonas transluscens. In a preferred aspect of the invention the host defense inducer is isotianil.
    Type: Application
    Filed: January 17, 2013
    Publication date: January 8, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Miguel Lino Dias, Gilbert Labourdette, Norberto Hernandez, Hiroyuki Hadano, Ingo Wetcholowsky, Matias Pastore, Akihisa Oshima, Karl-Wilhelm Muenks
  • Publication number: 20140378415
    Abstract: The present invention provides compounds of formula (I) wherein P is P0, heterocyclyl or heterocyclyl substituted by one to five Z formula (II); Y1, Y2, Y3 and Y4 are independently of each other C—H, C—R5, or nitrogen; G1 is oxygen or sulfur; X4 is C1-C8 haloalkyl; R4 is aryl or aryl substituted by one to five R9, or heteroaryl or heteroaryl substituted by one to five R9; and R1, R2, R4, R5, R9 and Z are as defined in the claims. The invention also provides compositions comprising the compounds of formula (I), intermediates useful in the preparation of compounds of formula (I) and methods of using the compounds of formula (I) to control insects, acarines, nematodes or molluscs.
    Type: Application
    Filed: August 27, 2012
    Publication date: December 25, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi
  • Publication number: 20140364466
    Abstract: The present invention relates to isothiazoline compounds of formula I wherein the variables are as defined in the claims or the description, which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes, and to a method for producing them. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.
    Type: Application
    Filed: December 21, 2012
    Publication date: December 11, 2014
    Applicant: BASF SE
    Inventors: Pascal Bindschaedler, Wolfgang Von Deyn, Karsten Koerber, Florian Kaiser, Michael Rack, Deborah L. Culbertson, Paul Neese, Franz Josef Braun
  • Patent number: 8883797
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: November 11, 2014
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Robert J. Schotzinger
  • Patent number: 8883180
    Abstract: The invention relates to active compound combinations, in particular a fungicidal and/or insecticidal composition, comprising Isotianil (3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide) and at least one further insecticide of the anthranilamide group and optionally one further insecticide of the neonicotinoids. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms and/or pests of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: November 11, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Heike Hungenberg, Wolfgang Thielert
  • Publication number: 20140323736
    Abstract: The present application relates to known and novel aryl- and hetarylcarboxamides of the formula (I) and to their use as medicaments for controlling endoparasites in animals or humans, and also to parasiticidal compositions, in particular endoparasites, comprising aryl- and hetarylcyclylcarboxamides.
    Type: Application
    Filed: November 23, 2012
    Publication date: October 30, 2014
    Inventors: Hans-Georg Schwarz, Axel Trautwein, Lothar Willms, Maike Hink, Peter Lummen, Ulrich Gorgens, Pierre-Yves Coqueron, Achim Harder, Claudia Welz
  • Patent number: 8846947
    Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: September 30, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
  • Patent number: 8846727
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: September 30, 2014
    Assignee: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Publication number: 20140275179
    Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, G, and Q are defined herein; and wherein R11, R21, R41, RB1 and G1, are defined herein.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 18, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Zhihua Sui, Chaozhong Cai, Xuqing Zhang
  • Publication number: 20140256700
    Abstract: The present invention is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
    Type: Application
    Filed: February 26, 2014
    Publication date: September 11, 2014
    Inventors: Michael A. Poss, David R. Tortolani, Dharmpal S. Dodd, Christopher P. Mussari, John S. Tokarski, Ashvinikumar V. Gavai, Yufen Zhao, George V. Delucca, Daniel O'Malley, Derek J. Norris, Patrice Gill, Claude A. Quesnelle, Wen-Ching Han
  • Publication number: 20140256740
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: September 11, 2014
    Applicant: Tempero Pharmaceuticals, Inc.
    Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt
  • Publication number: 20140228577
    Abstract: The present invention relates to compounds of formula (I): wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: April 22, 2014
    Publication date: August 14, 2014
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Jerome Yves CASSAYRE, Peter RENOLD, Myriem EL QACEMI, Thomas PITTERNA, Julie Clementine TOUEG
  • Publication number: 20140213538
    Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
    Type: Application
    Filed: January 15, 2014
    Publication date: July 31, 2014
    Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert, Shendong Yuan
  • Publication number: 20140200215
    Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
    Type: Application
    Filed: March 12, 2013
    Publication date: July 17, 2014
    Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
  • Publication number: 20140155350
    Abstract: A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.
    Type: Application
    Filed: November 26, 2013
    Publication date: June 5, 2014
    Applicant: SineVir Therapeutics LLC
    Inventors: John Hilfinger, Gordon Amidon
  • Publication number: 20140155413
    Abstract: The present invention is directed to compounds of formula I and 1a: which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Application
    Filed: July 6, 2012
    Publication date: June 5, 2014
    Inventors: Barbara Hanney, Peter Manley, Michael T. Rudd, John M. Sanders, Shawn J. Stachel, Darrell Henze
  • Publication number: 20140148472
    Abstract: Disclosed are compounds able to modulate the activity of the GPR17 receptor in a highly specific way, which are useful in the treatment and diagnosis of diseases or dysfunctions involving the activation of said receptor. In particular, the compounds according to the invention can be used for neuroprotective and/or reparatory purposes, in cerebral, cardiac and renal ischaemia, in cerebral trauma, in chronic neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS), and in demyelinating diseases such as multiple sclerosis.
    Type: Application
    Filed: November 2, 2011
    Publication date: May 29, 2014
    Applicant: CENTRO CARDIOLOGICO MONZINO SpA
    Inventors: Mariapia Abbracchio, Ivano Eberini, Chiara Parravicini, Claudia Martini, Maria Letizia Trincavelli, Simona Daniele
  • Patent number: 8735362
    Abstract: The present invention relates to compounds of formula (I): Wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: May 27, 2014
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
  • Publication number: 20140142143
    Abstract: The invention relates to substituted phenylureas and phenylamides, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.
    Type: Application
    Filed: October 24, 2013
    Publication date: May 22, 2014
    Applicant: Gruenenthal GmbH
    Inventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM, Derek SAUNDERS, Hannelore STOCKHAUSEN
  • Patent number: 8685975
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: April 1, 2014
    Assignee: Omeros Corporation
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
  • Publication number: 20140031331
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: September 19, 2013
    Publication date: January 30, 2014
    Inventors: Wilhelm Amberg, Michael Ochse, Udo Lange, Andreas Kling, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins
  • Patent number: 8633182
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: January 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dieter Hamprecht, Sara Frattini, Iain Lingard, Stefan Peters
  • Patent number: 8629157
    Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain (I).
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: January 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Angela Berry, Rajashekhar Betageri, Eugene Richard Hickey, Someina Khor, Doris Riether, Lifen Wu, Renee M. Zindell
  • Patent number: 8623860
    Abstract: The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: January 7, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Bernd Nosse, Gerald Juergen Roth
  • Publication number: 20130324514
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
    Type: Application
    Filed: May 22, 2013
    Publication date: December 5, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Dieter HAMPRECHT, Sara FRATTINI, Iain LINGARD, Stefan PETERS
  • Publication number: 20130316999
    Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.
    Type: Application
    Filed: August 7, 2013
    Publication date: November 28, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Alexander STRAUB, Thomas LAMPE, Jens POHLMANN, Susanne RÔHRIG, Elisabeth PERZBORN, Karl-Heinz SCHLEMMER, Joseph PERNERSTOFER
  • Publication number: 20130303524
    Abstract: The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, F, G, H, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 14, 2013
    Inventors: Ross Bersot, Paul Humphries
  • Publication number: 20130296310
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.
    Type: Application
    Filed: July 1, 2013
    Publication date: November 7, 2013
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Patent number: 8563745
    Abstract: A process for producing 3,4-dichloro-5-cyanoisothiazole represented by a general formula (3): the process comprising: reacting a nitrile compound represented by a general formula (1): (wherein “n” denotes an integer of 0 to 2), with sulfur chloride represented by a general formula (2): SmCl2??(2) (wherein “m” represents an integer of 1 to 2), or a mixture thereof in an aprotic polar solvent. There is provided a process for producing 3,4-dichloro-5-cyanoisothiazole, which is capable of suppressing by-production of a waste, without using a raw material having a strong toxicity; and is capable of providing a product having a higher purity in a high yield and efficiency in an industrial scale, in a simple manner.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: October 22, 2013
    Assignee: Ihara Chemical Industry Co., Ltd.
    Inventors: Takayuki Nakamura, Hironobu Kumagai, Mahito Ogawa
  • Publication number: 20130252937
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: March 14, 2013
    Publication date: September 26, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Matthias ECKHARDT, Sara FRATTINI, Dieter HAMPRECHT, Frank HIMMELSBACH, Elke LANGKOPF, Iain LINGARD, Stefan PETERS, Holger WAGNER
  • Publication number: 20130236434
    Abstract: A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein the integrin is selected from the group consisting of ?4?1, ?5?1, ?4?7, ?v?3 and ?L?2, and contacting the treated cells with an integrin-binding ligand; integrin agonist compounds having the general formula I; methods of treating integrin-expressing cells with such agonists to enhance binding; and therapeutic methods comprising administering agonist-treated cells or agonist compounds to a mammal.
    Type: Application
    Filed: November 16, 2011
    Publication date: September 12, 2013
    Applicant: TEXAS HEART INSTITUTE
    Inventors: Ronald J. Biediger, William C. Gundlach, IV, Robert V. Market, Michael M. Savage, Peter Vanderslice
  • Patent number: 8501794
    Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: November 4, 2009
    Date of Patent: August 6, 2013
    Assignee: AbbVie Inc.
    Inventors: William A. Carroll, Michael J. Dart, Teodozyj Kolasa, Tongmei Li, Derek W. Nelson, Meena V. Patel, Sridhar Peddi, Arturo Perez-Medrano, Xueqing Wang
  • Publication number: 20130172353
    Abstract: This invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R, R1, R2, R3, n, X1, X2, L1, and L2 are as defined herein. The compounds of Formula I are useful as receptor tyrosine kinase (RTK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases.
    Type: Application
    Filed: December 27, 2012
    Publication date: July 4, 2013
    Applicant: Allergan, Inc.
    Inventor: Allergan, Inc.
  • Publication number: 20130172316
    Abstract: The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: December 14, 2012
    Publication date: July 4, 2013
    Inventors: Martin FLECK, Bernd NOSSE, Gerald Juergen ROTH
  • Patent number: 8466182
    Abstract: The present invention relates to compounds of Formula I below and their tautomers or pharmaceutically acceptable salts, compositions and methods of uses thereof.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: June 18, 2013
    Assignees: The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone, University of Maryland, Baltimore
    Inventors: Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
  • Publication number: 20130150326
    Abstract: Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.
    Type: Application
    Filed: August 19, 2011
    Publication date: June 13, 2013
    Applicant: Amira Pharmaceuticals, Inc.
    Inventors: Jeffrey Roger Roppe, Timothy Andrew Parr, Nicholas Simon Stock, Deborah Volkots, John Howard Hutchinson
  • Patent number: 8450304
    Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, and R4 are as defined in the specification. The invention also comprises pharmaceutical compositions comprising the compounds of formula (I) and methods of preventing, treating or ameliorating a CCR2 mediated syndrome, disorder or disease, for example, type II diabetes, obesity or asthma, by administering the compounds of formula (I).
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: May 28, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Xuqing Zhang, Heather Rae Hufnagel, Cuifen Hou, Dana L. Johnson, Zhihua Sui, Barry Fegely, David Breslin
  • Publication number: 20130116240
    Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.
    Type: Application
    Filed: September 26, 2012
    Publication date: May 9, 2013
    Applicant: JAPAN TOBACCO INC.
    Inventor: Japan Tobacco Inc.
  • Publication number: 20130085276
    Abstract: The use of a complex of the form Z—M—OR in the carboxylation of a substrate is described. The group Z is a two-electron donor ligand, M is a metal and OR is selected from the group consisting of OH, alkoxy and aryloxy. The substrate may be carboxylated at a C—H or N—H bond. The metal M may be copper, silver or gold. The two-electron donor ligand may be a phosphine, a carbene or a phosphite ligand. Also described are methods of manufacture of the complexes and methods for preparing isotopically labelled caboxylic acids and carboxylic acid derivatives.
    Type: Application
    Filed: June 9, 2011
    Publication date: April 4, 2013
    Inventors: Steven P. Nolan, Catherine Cazin
  • Patent number: 8410150
    Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: April 2, 2013
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
  • Patent number: 8404728
    Abstract: This disclosure relates to materials and methods for inhibiting Botulinum neurotoxin, and more particularly to materials and methods for inhibiting the zinc endopeptidase of Botulinum neurotoxin serotypes A, D and/or E (BoNTA, BoNTD and/or BoNTE).
    Type: Grant
    Filed: July 29, 2010
    Date of Patent: March 26, 2013
    Assignees: Mayo Foundation for Medical Education and Research, U.S. Army Medical Research and Material Command
    Inventors: Yuan-Ping Pang, Jewn Giew Park, Shaohua Wang, Anuradha Vummenthala, Rajesh K Mishra, Jon Davis, Charles B. Millard, James J. Schmidt