Chalcogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 548/243)
  • Publication number: 20150133658
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: August 15, 2014
    Publication date: May 14, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
  • Patent number: 9029400
    Abstract: The present invention relates to 5-oxoisoxazole derivatives of the formula I, the pharmaceutically usable salts thereof and the use thereof as medicinal substances.
    Type: Grant
    Filed: October 5, 2009
    Date of Patent: May 12, 2015
    Assignee: Sanofi
    Inventors: Stefan Petry, Manfred Seidel, Gerhard Zoller, Gunter Müller, Karl-Heinz Baringhaus, Hubert Heuer
  • Publication number: 20150080576
    Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the ?4?2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Inventors: Anatoly Mazurov, Lan Miao, Yunde Xiao, Philip S. Hammond, Craig H. Miller, Srinivasa Rao Akireddy, Srinivasa V. Murthy, Regina C. Whitaker, Scott R. Breining, Matt S. Melvin
  • Patent number: 8952176
    Abstract: Disclosed is a compound useful as a type I 11?hydroxysteroid dehydrogenase inhibitor. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkenyl or the like, One of R2 and R3 is a group of the formula: —C(?O)—Y—R4, wherein Y is —NR9— or the like, R4 is optionally substituted cycloalkyl or the like, R9 is hydrogen or optionally substituted alkyl, W is optionally substituted alkylene, The other is a group of the formula: —V—R5, wherein V is a bond, —O— or the like, R6 is hydrogen or optionally substituted alkyl, R5 is hydrogen, optionally substituted alkyl or the like, X is a bond, —S—, —SO— or the like, U is a bond or optionally substituted alkylene, R7 is hydrogen or optionally substituted alkyl, Z is —S—, —O— or —NR8—, R8 is hydrogen, optionally substituted alkyl or the like.
    Type: Grant
    Filed: June 6, 2006
    Date of Patent: February 10, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Tomoyuki Ogawa, Noriyuki Kurose, Satoru Tanaka, Koichi Nishi
  • Publication number: 20150030618
    Abstract: The present application relates to new binder-drug conjugates (ADCs) of N,N-dialkylauristatins that are directed against the target C4.4a, to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for treating and/or preventing illnesses, and also to the use of these ADCs for producing medicaments for treating and/or preventing illnesses, more particularly hyperproliferative and/or angiogenic diseases such as, for example, cancer diseases. Such treatments may be practised as a monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Application
    Filed: May 5, 2014
    Publication date: January 29, 2015
    Applicant: SEATTLE GENETICS, INC.
    Inventors: Hans-Georg LERCHEN, Lars Linden, Sherif El Sheikh, Jörg Willuda, Charlotte C. Kopitz, Joachim Schuhmacher, Simone Greven, Christoph Mahlert, Beatrix Stelte-Ludwig, Sven Golfier, Rudolf Beier, Iring Heisler, Axel Harrenga, Karl-Heinz Thierauch, Sandra Bruder, Heike Petrul, Hannah Jörissen, Sandra Borkowski
  • Patent number: 8921572
    Abstract: A process for preparing 5,5-disubstituted 4,5-dihydroisoxazole-3-thiocarboxamidine salts of the formula (I), wherein 3-unsubstituted 4,5-dihydroisoxazoles are first reacted with a chlorinating or brominating reagent to give 3-halogenated 4,5-dihydroisoxazoles and the latter then react with thiourea to give the compounds of the formula (I).
    Type: Grant
    Filed: November 26, 2009
    Date of Patent: December 30, 2014
    Assignee: BASF SE
    Inventor: Timo Frassetto
  • Patent number: 8907104
    Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.
    Type: Grant
    Filed: November 11, 2013
    Date of Patent: December 9, 2014
    Assignee: President and Fellows of Harvard College
    Inventors: Andrew G. Myers, Jason D. Brubaker
  • Patent number: 8895471
    Abstract: The invention relates to 3-(benzylsulfinyl)-5,5-dimethyl-4,5-dihydroisoxazole derivatives and 5,5-dimethyl-3-[(1H-pyrazol-4-ylmethyl)sulfinyl]-4,5-dihydroisoxazole derivatives of the formula (I) and their salts processes for their preparation and their use as herbicides and plant growth regulators, in particular as herbicides for the selective control of harmful plants in crops of useful plants.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: November 25, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Hansjoerg Dietrich, Arianna Martelletti, Christopher Hugh Rosinger, Jan Dittgen, Dieter Feucht
  • Patent number: 8871792
    Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: October 28, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Adam D. Hughes, Melissa Fleury
  • 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: 20140221351
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: April 8, 2014
    Publication date: August 7, 2014
    Applicant: ALLERGAN, INC.
    Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
  • Patent number: 8784835
    Abstract: A method for producing muscimol and or/reducing ibotenic acid from Amanita tissue, and or producing a nutritional supplement therefrom.
    Type: Grant
    Filed: July 2, 2013
    Date of Patent: July 22, 2014
    Inventor: Trent Austin
  • Publication number: 20140179929
    Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.
    Type: Application
    Filed: November 11, 2013
    Publication date: June 26, 2014
    Applicant: President and Fellows of Harvard College
    Inventors: Andrew G. Myers, Jason D. Brubaker
  • Publication number: 20140162997
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, ring A, and G are defined herein.
    Type: Application
    Filed: August 16, 2013
    Publication date: June 12, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Mark Wall, Nalin Subasinghe, Zhihua Sui, Christopher Flores
  • 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
  • Patent number: 8722887
    Abstract: This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description.
    Type: Grant
    Filed: February 16, 2010
    Date of Patent: May 13, 2014
    Assignee: Abbvie Bahamas, Ltd.
    Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A. W. Van Der Neut, Cornelis G. Kruse
  • Patent number: 8697696
    Abstract: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, u, v, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. The compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: April 15, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Stephen Deems Gabriel, Andrew Thomas
  • Patent number: 8680290
    Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Grant
    Filed: August 17, 2005
    Date of Patent: March 25, 2014
    Assignee: Syngenta Limited
    Inventors: Andrew Plant, Jutta Elisabeth Boehmer, Janice Black, Timothy David Sparks
  • Publication number: 20140051688
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Q, and G are defined herein.
    Type: Application
    Filed: August 16, 2013
    Publication date: February 20, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Michael WINTERS, Zhihua Sui
  • Publication number: 20140051682
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: September 24, 2013
    Publication date: February 20, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing Yuan, Richard L. Beard, Michael E. Garst, Xiaoxia Liu, John E. Donello, Veena Viswanath
  • Publication number: 20140045906
    Abstract: In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: August 7, 2013
    Publication date: February 13, 2014
    Inventors: Melissa Fleury, Adam D. Hughes
  • Publication number: 20140046053
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: October 10, 2013
    Publication date: February 13, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Roland Gendron, Melissa Fleury, Adam D. Hughes
  • Publication number: 20140038919
    Abstract: This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: December 16, 2011
    Publication date: February 6, 2014
    Applicant: AbbVie Inc.
    Inventors: Clarence J. Maring, John K. Pratt, William A. Carroll, Dachun Liu, David A. Betebenner, Douglas K. Hutchinson, Michael D. Tufano, Todd W. Rockway, Uwe Schoen, Axel Pahl, Andreas Witte
  • Publication number: 20140031231
    Abstract: New formulations of clomazone are provided, as well as new methods for making formulations of clomazone. The new formulations provide improved efficacy, decreased volatility, and/or increased loading of clomazone over the clomazone formulations in the prior art.
    Type: Application
    Filed: June 18, 2013
    Publication date: January 30, 2014
    Inventors: Hong Liu, Michael R. Welch, Paul Nicholson, Jeffrey A. Cook, Catherine Ranin, Sandra L. Shinn, Robert F. Pepper
  • Publication number: 20140011997
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: September 12, 2013
    Publication date: January 9, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Cameron Smith, Melissa Fleury, Roland Gendron, Ryan Hudson, Adam D. Hughes
  • Publication number: 20130330365
    Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Adam D. Hughes, Melissa Fleury
  • Publication number: 20130330366
    Abstract: In one aspect, the invention relates to compounds having the formula XII: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Adam D. Hughes, Melissa Fleury
  • Publication number: 20130324529
    Abstract: The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.
    Type: Application
    Filed: August 6, 2013
    Publication date: December 5, 2013
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Henricus Jacobus Maria Gijsen, Michel Anna Jozef De Cleyn, Michel Surkyn, Bie Maria Pieter Verbist
  • Publication number: 20130323271
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R7, R8, Z, X, b, and c are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are nitric oxide donors and have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: May 30, 2013
    Publication date: December 5, 2013
    Inventors: Mathai Mammen, Adam D. Hughes
  • Publication number: 20130316904
    Abstract: The invention relates to 3-(benzylsulfinyl)-5,5-dimethyl-4,5-dihydroisoxazole derivatives and 5,5-dimethyl-3-[(1H-pyrazol-4-ylmethyl)sulfinyl]-4,5-dihydroisoxazole derivatives of the formula (I) and their salts processes for their preparation and their use as herbicides and plant growth regulators, in particular as herbicides for the selective control of harmful plants in crops of useful plants.
    Type: Application
    Filed: March 15, 2013
    Publication date: November 28, 2013
    Applicant: BAYER CROPSCIENCE AG
    Inventor: Bayer Cropscience AG
  • Patent number: 8580969
    Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: November 12, 2013
    Assignee: President and Fellows of Harvard College
    Inventors: Andrew G. Myers, Jason D. Brubaker
  • Publication number: 20130274230
    Abstract: The present invention relates to (2-ureidoacetamido)alkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2.
    Type: Application
    Filed: April 16, 2013
    Publication date: October 17, 2013
    Applicant: Allergan, Inc.
    Inventors: Richard L. Beard, Tien Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20130259897
    Abstract: The invention provides crystalline forms of (R)-3-[N-(3?-chlorobiphenyl-4-ylmethyl)-N?—(3-hydroxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionic acid isopropyl ester. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases.
    Type: Application
    Filed: March 27, 2013
    Publication date: October 3, 2013
    Inventors: Venkat R. Thalladi, Jerry Nzerem, Miroslav Rapta
  • Patent number: 8524913
    Abstract: ?-Trifluoromethyl-?-substituted-?-amino acids can be produced by allowing ?-trifluoromethyl-?-substituted-?,?-unsaturated esters to react with hydroxylamine to convert ?-trifluoromethyl-?-substituted-?,?-unsaturated esters into dehydrogenated closed-ring body of ?-trifluoromethyl-?-substituted-?-amino acid, and by hydrogenolyzing the dehydrogenated closed-ring body. According to this production process, novel ?-trifluoromethyl-?-substituted-?-amino acids which are free amino acids whose functional groups are not protected can be produced, in which ?-position substituent is not limited to aromatic ring group or substituted aromatic ring group while the relative stereochemistry of ?-position and ?-position can be also controlled.
    Type: Grant
    Filed: August 27, 2009
    Date of Patent: September 3, 2013
    Assignee: Central Glass Company, Limited
    Inventors: Akihiro Ishii, Manabu Yasumoto, Takako Yamazaki, Kaori Mogi, Takashi Masuda
  • Publication number: 20130225600
    Abstract: The present invention relates to compounds of Formula (I) along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC of Formula (I).
    Type: Application
    Filed: October 31, 2011
    Publication date: August 29, 2013
    Applicant: LUPIN LIMITED
    Inventors: Nageswara Rao Irlapati, Gokul Keruji Deshmukh, Vijay Pandurang Karche, Santosh Madhukar Jachak, Neelima Sinha, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20130217886
    Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.
    Type: Application
    Filed: September 14, 2012
    Publication date: August 22, 2013
    Applicant: President and Fellows of Harvard College
    Inventors: Andrew G. Myers, Jason D. Brubaker
  • Publication number: 20130217702
    Abstract: The present invention relates to the indole derivatives of formula (I), wherein R1-R6 and X are defined in the claims and optical antipodes or racemates and/or salts thereof which are selective antagonists of bradykinin B1 to process for producing these compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
    Type: Application
    Filed: November 4, 2011
    Publication date: August 22, 2013
    Inventors: Gyula Beke, Gyula Attila Bényei, István Borza, Éva Bozó, Sándor Farkas, Katalin Hornok, Andrea Papp, István Vágó, Mónika Vastag
  • Patent number: 8513462
    Abstract: The invention disclosed in this document is related to field of pesticides and their use in controlling pests. In particular compounds having the following formula are disclosed.
    Type: Grant
    Filed: September 10, 2012
    Date of Patent: August 20, 2013
    Assignee: Dow AgroSciences LLC
    Inventors: Benjamin M. Nugent, Ann M. Buysse, Jonathan M. Babcock, Matthias S. Ober, Timothy P. Martin
  • Patent number: 8431699
    Abstract: There is provided a method for manufacture of 2-oxoimidazolidines of Formula I comprising one or more of the steps of converting an amine to an acylation agent, condensation of the acylation agent with a bi-functional compound of structure L-C(R4)(R5)—C(R2)(R3)—NHR1, wherein L is a leaving group, and ring closure of the resulting urea. In this manner, certain 2-oxoimidazolidines may be manufactured that are useful intermediates for the production of Pramiconazole and structurally related compounds.
    Type: Grant
    Filed: March 1, 2010
    Date of Patent: April 30, 2013
    Assignee: Vertichem Corporation
    Inventors: John R. Peterson, Christopher M. Yost
  • Patent number: 8420570
    Abstract: The invention relates to 3-(benzylsulfinyl)-5,5-dimethyl-4,5-dihydroisoxazole derivatives and 5,5-dimethyl-3-[(1H-pyrazol-4-ylmethyl)sulfinyl]-4,5-dihydroisoxazole derivatives of the formula (I) and their salts processes for their preparation and their use as herbicides and plant growth regulators, in particular as herbicides for the selective control of harmful plants in crops of useful plants.
    Type: Grant
    Filed: November 8, 2008
    Date of Patent: April 16, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Hansjoerg Dietrich, Arianna Martelletti, Christopher Hugh Rosinger, Jan Dittgen, Dieter Feucht
  • Patent number: 8415378
    Abstract: or a pharmaceutically suitable salt thereof, wherein, R1 and R2 independently are hydrogen, deuterium, aryl, hetero aryl, C1-C8 alkyl, optionally being substituted with one or more substituents independently being R3, R3 is an aryl, hetero aryl, fluorine(s), a C1-C6 alkyl containing one or more fluorine, a C1-C6 alkyl containing one or more deuterium, a C1-C6 alkyl containing hydroxy, the aryl and heteroaryl optionally being substituted with one or more halogen, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium, a C1-6 alkyl, a C1-6 alkoxy, a nitrile, or R3 is a C1-6 alkyl optionally substituted with one or more of the following groups: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; wherein, R4 is a C1-10 alkyl optionally substituted with one or more fluorine, deuterium, alkoxy, arylcarboxylate, alkyl carboxylate; R5 and R6 are independently selected from hydrogen, alkyl or they may together form a 4-8 membered carbon ring; or R1 and R2 form a 3-10 membered carbon ring optionally compris
    Type: Grant
    Filed: April 6, 2010
    Date of Patent: April 9, 2013
    Assignee: AstraZeneca AB
    Inventors: Jonas Boström, Leifeng Cheng, Tomas Fex, Michael Karle, Daniel Pettersen, Peter Schell
  • Publication number: 20120309724
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, X, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: May 18, 2012
    Publication date: December 6, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
  • Patent number: 8299048
    Abstract: The present invention is directed to hexahydrocyclopentylf]indazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: February 24, 2009
    Date of Patent: October 30, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: William P. Dankulich, Mildred L. Kaufman, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
  • Patent number: 8293920
    Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.
    Type: Grant
    Filed: March 9, 2011
    Date of Patent: October 23, 2012
    Assignee: President and Fellows of Harvard College
    Inventors: Andrew G. Myers, Jason D. Brubaker
  • Publication number: 20120264947
    Abstract: A process for preparing 5,5-disubstituted 4,5-dihydroisoxazole-3-thiocarboxamidine salts of the formula (I), wherein 3-unsubstituted 4,5-dihydroisoxazoles are first reacted with a chlorinating or brominating reagent to give 3-halogenated 4,5-dihydroisoxazoles and the latter then react with thiourea to give the compounds of the formula (I).
    Type: Application
    Filed: November 26, 2009
    Publication date: October 18, 2012
    Applicant: BASF SE
    Inventor: Timo Frasetto
  • Patent number: 8288589
    Abstract: The invention disclosed in this document is related to field of pesticides and their use in controlling pests. In particular compounds having the following formula are disclosed.
    Type: Grant
    Filed: July 11, 2008
    Date of Patent: October 16, 2012
    Assignee: Dow AgroSciences, LLC
    Inventors: Benjamin M. Nugent, Ann M. Buysse, Jonathan M. Babcock, Matthias S. Ober, Timothy P. Martin
  • Publication number: 20120238517
    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: December 1, 2010
    Publication date: September 20, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
  • Patent number: 8263624
    Abstract: The invention relates to aryl-substituted heterocycles, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.
    Type: Grant
    Filed: May 25, 2007
    Date of Patent: September 11, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Michael Härter, Tobias Wunberg, Swen Allerheiligen, Marcus Bauser, Ulrich Rester, Stefan Heitmeier
  • Publication number: 20120225909
    Abstract: [Objective] To provide a drug that selectively stimulates the ?3-adrenergic receptors, particularly a drug capable of preferentially stimulating the ?3-adrenergic receptors over the ?1-adrenergic receptors. This drug can be used in the treatment and prevention of diabetes, obesity, hyperlipidemia, depression, cholelithiasis, diseases caused by biliary hyperkinesia, diseases caused by hyperfunction of the gastrointestinal tract, interstitial cystitis, overactive bladder or urinary incontinence, diseases associated with decreased lacrimation, and the like. [Solution] Indazole analogs represented by the general formula (I) or a salt thereof. Drugs that contains these indazole analogs or a salt thereof as the active ingredient.
    Type: Application
    Filed: September 30, 2010
    Publication date: September 6, 2012
    Applicant: ASAHI KASEI PHARMA CORPORATION
    Inventors: Yasuhiro Wada, Akifumi Morimoto
  • Publication number: 20120220772
    Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of solving the problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is a specific cyclic group; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is —CH2—, O, —S(O)i— (i is 0 to 2), or —NR7—; R1 to R6 are specific groups), a salt of the compound, or a solvate of the salt or the compound.
    Type: Application
    Filed: October 29, 2010
    Publication date: August 30, 2012
    Inventors: Akihiro Okano, Munetaka Ohkouchi