Ring Nitrogen In The Additional Hetero Ring (e.g., Oxazole, Etc.) Patents (Class 514/340)
The additional hetero ring consists of two nitrogens and three carbons (Class 514/341)
Ring sulfur in the additional hetero ring (Class 514/342)
The additional hetero ring consists of one nitrogen and four carbons (e.g., nicotine, etc.) (Class 514/343)
  • Fungicide hydroximoyl-tetrazole derivatives
    Patent number: 8557849
    Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: March 18, 2009
    Date of Patent: October 15, 2013
    Assignee: Bayer CropScience AG
    Inventors: Christian Beier, Jürgen Benting, Isabelle Christian, Pierre-Yves Coqueron, Christophe Dubost, Pierre Genix, Benoît Hartmann, Daniela Portz, Arnd Voerste, Ulrike Wachendorff-Neumann
  • ARYL SULFONAMIDES
    Publication number: 20130267492
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: March 28, 2013
    Publication date: October 10, 2013
    Applicant: ChemoCentryx, Inc.
    Inventors: Solomon Ungashe, John J. Wright, Andrew Pennell, Zheng Wei
  • HETEROARYLS AND USES THEREOF
    Publication number: 20130267563
    Abstract: This invention provides compounds of formula IA or IB: wherein HY, R1, R2, G1, W, n, and A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: August 10, 2011
    Publication date: October 10, 2013
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Masaaki Hirose, Yongbo Hu, Zhigen Hu, Hong Myung Lee, Zhan Shi, Stephan Vyskocil, Tianlin Xu
  • COMPOSITIONS AND METHODS FOR CANCER TREATMENT
    Publication number: 20130259800
    Abstract: The invention described herein pertains to the use of oxazolidinone antibiotics, alone or in combination, in the treatment of cancer. In particular, the invention pertains to the treatment of malignant gliomas, thyroid cancer or melanoma, or borderline forms of malignant glioma, thyroid cancer or melanoma.
    Type: Application
    Filed: December 15, 2011
    Publication date: October 3, 2013
    Applicant: BIOVISTA, INC.
    Inventors: Andreas Persidis, Spyros Deftereos
  • NOVEL HETEROCYCLIC COMPOUNDS AS PESTICIDES
    Publication number: 20130261141
    Abstract: The present application relates to novel heterocyclic compounds, to processes for preparation thereof and to the use thereof for controlling animal pests, which also include arthropods and especially insects.
    Type: Application
    Filed: October 17, 2011
    Publication date: October 3, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Thomas Bretschneider, Adeline Köhler, Joachim Kluth, Martin Füsslein, Peter Jeschke, Reiner Fischer, Friedrich August Mühlthau, Olga Malsam, Arnd Voerste, Klaus-Helmut Müller, Yoshitaka Sato
  • Substituted hydroxamic acids and uses thereof
    Patent number: 8546588
    Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: October 1, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Amino-tetrazoles analogues and methods of use
    Patent number: 8546374
    Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: October 1, 2013
    Assignee: Abbvie Inc.
    Inventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biquin C. Li
  • ISOXAZOLE, ISOTHIAZOLE, FURANE AND THIOPHENE COMPOUNDS AS MICROBICIDES
    Publication number: 20130252972
    Abstract: The present invention relates to a compound of formula I: (I) wherein the substituents have the definitions as defined in claim 1 or a salt or a N-oxide thereof, their use and methods for the control and/or prevention of microbial infection, particularly fungal infection, in plants and to processes for the preparation of these compounds.
    Type: Application
    Filed: July 19, 2011
    Publication date: September 26, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Carla Bobbio, Camilla Corsi, Stephane Andre Marie Jeanmart, Sebastian Volker Wendeborn
  • Lysophosphatidic acid receptor antagonists
    Patent number: 8541587
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Grant
    Filed: April 4, 2012
    Date of Patent: September 24, 2013
    Assignee: Amira Pharmaceuticals, Inc.
    Inventors: Thomas Jon Seiders, Jeffrey Roger Roppe, Timothy Andrew Parr
  • HETEROCYCLIC COMPOUNDS AND METHODS OF USE
    Publication number: 20130243754
    Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.
    Type: Application
    Filed: December 20, 2012
    Publication date: September 19, 2013
    Applicant: TARGEGEN, INC.
    Inventors: Wolfgang WRASIDLO, Elena DNEPROVSKAIA
  • Multiheteroaryl compounds as inhibitors of H-PGDS and their use for treating prostaglandin D2 mediated diseases
    Patent number: 8536185
    Abstract: Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D2 mediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: September 17, 2013
    Assignee: Cayman Chemical Company, Incorporated
    Inventors: Gregory W. Endres, Pil Heui Lee, Kirk Lang Olson, James Bernard Kramer, Fred Lawrence Ciske, Stephen Douglas Barrett
  • Pharmaceutical compounds
    Patent number: 8536203
    Abstract: This invention relates to novel substituted nitrocatechol derivatives, their use in the treatment of some central and peripheral nervous system disorders and pharmaceutical compositions containing them.
    Type: Grant
    Filed: April 10, 2007
    Date of Patent: September 17, 2013
    Assignee: Bial-Portela & CA, S.A.
    Inventors: David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto Dos Santos Ferreira, Patricio Manuel Vieira Araujo Soares da Silva
  • Azabiphenylaminobenzoic acid derivatives as DHODH inhibitors
    Patent number: 8536165
    Abstract: The present disclosure relates to new azabiphenylaminobenzoic acid derivatives of formula (I); as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).
    Type: Grant
    Filed: August 8, 2008
    Date of Patent: September 17, 2013
    Assignee: Almirall, S.A.
    Inventors: Julio Cesar Castro Palomino Laria, Emma Terricabras Belart, Montserrat Erra Sola, Eloisa Navarro Romero, Silvia Fonquerna Pou, Aranzazu Cardus Figueras, Maria Estrella Lozoya Toribio
  • ARYLCYCLOPROPYLAMINE BASED DEMETHYLASE INHIBITORS OF LSD1 AND THEIR MEDICAL USE
    Publication number: 20130231342
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).
    Type: Application
    Filed: July 27, 2011
    Publication date: September 5, 2013
    Applicant: Oryzon Fenomics S.A.
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Iñigo Tirapu Fernandez de la Cuesta, Maria de los Ángeles Estirate-Martinez
  • METHODS OF CONTROLLING NEONICOTINOID RESISTANT APHIDS
    Publication number: 20130231334
    Abstract: The invention relates to a method of controlling aphids that are resistant to neonicotinoid insecticides, using a trifluoromethylpyri(mi)dine derivative in free form or in agrochemically acceptable salt form as well as the use of compositions comprising said compound to control neonicontinoid resistant insects. In particular the methods relate to controlling neonicotinoid resistant insects in the Aphididae family, that are resistant to one or more neonicotinoid insecticides. Methods of the invention find particular use in controlling neonicotinoid resistant insects in crops of useful plants. Furthermore, the invention extends to methods of controlling plant viruses spread by neonicotinoid resistant insects.
    Type: Application
    Filed: April 18, 2011
    Publication date: September 5, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Russell Slater, Peter Maienfisch, Patrik Hoegger, Alfred Rindlisbacher
  • Dosage regimen for COMT inhibitors
    Patent number: 8524746
    Abstract: The invention relates to the use of an oxodiazolyl compound (I) for the preparation of a medicament for the prevention or treatment of central and peripheral nervous system associated disorders, wherein said medicament is administered according to a dosing regimen having a dosing periodicity ranging from about twice a day to about once every other day.
    Type: Grant
    Filed: October 10, 2007
    Date of Patent: September 3, 2013
    Assignee: Bial-Portela & Ca., S.A.
    Inventors: David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto dos Santos Ferreira, Patricio Manuel Vieira Araujo Soares da Silva
  • Substituted dihydropyrazolones and use thereof as HIF-prolyl-4-hydroxylase inhibitors
    Patent number: 8524699
    Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.
    Type: Grant
    Filed: October 26, 2007
    Date of Patent: September 3, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Metin Akbaba, Mario Jeske
  • OXAZOLINE AND ISOXAZOLINE DERIVATIVES AS CRAC MODULATORS
    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
  • Isoxazolo-pyridine derivatives
    Patent number: 8518974
    Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.
    Type: Grant
    Filed: February 10, 2012
    Date of Patent: August 27, 2013
    Assignee: Hoffmann-La Roche Inc
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
  • c-MET protein kinase inhibitors
    Patent number: 8518938
    Abstract: The present invention relates to compounds of formula I useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative disorders.
    Type: Grant
    Filed: April 20, 2011
    Date of Patent: August 27, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David J. Lauffer, Pan Li, Kira McGinty, Steven M. Ronkin, Qing Tang, Anne-Laure Grillot, Nathan D. Waal
  • PARASITICIDAL DIHYDROISOXAZOLE COMPOUNDS
    Publication number: 20130217699
    Abstract: Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.
    Type: Application
    Filed: May 8, 2012
    Publication date: August 22, 2013
    Applicant: ELI LILLY AND COMPANY
    Inventors: Zengyun An, Liang Chen, Shuhui Chen, Jean Marie Defauw, Scott Dale Holmstrom, Ping Hu, Chongzhi Tang, William Hunter White, Wentao Wu, Yang Zhang
  • Arylethynyl derivatives
    Patent number: 8513273
    Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Grant
    Filed: February 28, 2013
    Date of Patent: August 20, 2013
    Assignee: Hoffmann-LaRoche Inc.
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • ADENOSINE A1 AGONISTS FOR THE TREATMENT OF GLAUCOMA AND OCULAR HYPERTENSION
    Publication number: 20130210797
    Abstract: The present invention relates to the use of selective adenosine A1 agonists, in particular the dicyanopyridines of formula (I), for the treatment and/or prophylaxis of glaucoma and ocular hypertension as well as the their use for the production of a medicament for the treatment and/or prophylaxis of glaucoma and ocular hypertension.
    Type: Application
    Filed: August 29, 2011
    Publication date: August 15, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jürgen Klar, Georges Von Degenfeld, Hans-Georg Lerchen, Barbara Albrecht-Küpper, Andreas Knorr, Peter Sandner, Daniel Meiibom
  • Novel Heterocyclic Compounds and Uses Thereof
    Publication number: 20130210818
    Abstract: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
    Type: Application
    Filed: February 14, 2012
    Publication date: August 15, 2013
    Inventors: Zilin Huang, Jeff Jin, Timothy Machajewski, William R. Antonios-McCrea, Maureen McKenna, Daniel Poon, Paul A. Renhowe, Martin Sendzik, Cynthia Shafer, Aaron Smith, Yongjin Xu, Qiong Zhang, Zheng Chen
  • MICROBICIDES
    Publication number: 20130210836
    Abstract: The present invention relates to a compound of formula (I): wherein the substituents have the definitions as defined in claim 1 or a salt or a N-oxide thereof, their use and methods for the control and/or prevention of microbial infection, particularly fungal infection, in plants and to processes for the preparation of these compounds.
    Type: Application
    Filed: July 19, 2011
    Publication date: August 15, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Carla Bobbio, Camilla Corsi, Stephane Andre Marie Jeanmart, Sebastian Volker Wenderborn
  • Methyl-pyrrolidine ether derivatives
    Patent number: 8507535
    Abstract: The invention relates to a compound of formula wherein A is defined herein or to pharmaceutically active salts, stereoisomeric forms, including individual diastereoisomers and enantiomers of the compound of formula I as well as racemic and non-racemic mixtures thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: June 29, 2011
    Date of Patent: August 13, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthias Nettekoven, Hasane Ratni, Walter Vifian
  • Isoxazole compounds as inhibitors of heat shock proteins
    Patent number: 8507480
    Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C?O)—, —(C?S)—, —SO.sub.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: August 13, 2013
    Assignees: Vernalis (R&D) Limited, Cancer Research Technology Limited, The Institute of Cancer Research
    Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
  • Novel Inhibitors of LYN Kinase
    Publication number: 20130203817
    Abstract: The invention includes novel compounds that inhibit LYN kinase activity. The invention further includes a method of treating, ameliorating or preventing cancer in a subject in need thereof, wherein the cancer is dependent on LYN kinase activity.
    Type: Application
    Filed: February 8, 2013
    Publication date: August 8, 2013
    Applicant: VASSA INFORMATICS
    Inventor: VASSA INFORMATICS
  • Pyridine Compounds for Controlling Invertebrate Pests II
    Publication number: 20130203821
    Abstract: The present invention relates to novel pyridine compounds of the formulae I and II, to their salts, to their tautomers, to their N-oxides, and to the salts of these N-oxides or tautomers. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests. The invention also relates to a method for controlling in-vertebrate pests by using these compounds. The invention further relates to plant propagation material and to agricultural compositions comprising said compounds. wherein A is a radical of the formulae A1, A2, A3, A4, A5 or A6 wherein # denotes the binding site to the remainder of formulae I or II; Z is O, S or N—RN; X1 is S, O or NR1a; X2 is OR2a, NR2bR2c, S(O)mR2d; X3 is a lone pair or oxygen; R1, R2 and R3 are, inter alia, hydrogen, and RA1, RA2RA3RA4, RA5, RA6 and RN, are as defined in claim 1.
    Type: Application
    Filed: September 12, 2011
    Publication date: August 8, 2013
    Applicant: BASF SE
    Inventors: Sebastian Soergel, Christian Defieber, Ronan Le Vezouet, Steffen Gross, Karsten Koerber, Deborah L. Culbertson, Douglas D. Anspaugh
  • Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists
    Patent number: 8501786
    Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: March 23, 2009
    Date of Patent: August 6, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Bart Harper, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Harvey Wendt, Cheng Zhu
  • Sodium salt of 5-cyclopropyl-2-{[2-(2,6-difluorophenyl)pyrimidin-5-yl]amino}benzoic acid as DHODH inhibitor
    Patent number: 8501943
    Abstract: The present disclosure is directed to the sodium salt of 5-cyclopropyl-2-{[2-(2,6-difluorophenyl)pyrimidin-5-yl]amino}benzoic acid, pharmaceutically acceptable solvates thereof, pharmaceutical combinations thereof, and methods of treatment.
    Type: Grant
    Filed: March 11, 2010
    Date of Patent: August 6, 2013
    Assignee: Almirall, S.A.
    Inventors: Nuria Garcia Gonzalez, Francesc Carrera Carrera, Monserrat Julia Jane, Laurent Debethune, Xavier Serra Masia
  • HETEROCYCLIC DERIVATIVES FOR THE TREATMENT OF DISEASES
    Publication number: 20130196952
    Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.
    Type: Application
    Filed: May 4, 2011
    Publication date: August 1, 2013
    Applicant: PFIZER INC.
    Inventors: Mark Edward Bunnage, Andrew Simon Cook, Jingrong Jean Cui, Kevin Nell Dack, Judith Gail Deal, Danlin Gu, Mingying He, Patrick Stephen Johnson, Ted William Johnson, Phuong Thi Quy Le, Cynthia Louise Palmer, Hong Shen
  • DUAL-ACTING OXAZOLE ANTIHYPERTENSIVE AGENTS
    Publication number: 20130196997
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and 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: November 20, 2012
    Publication date: August 1, 2013
    Inventors: Paul R. Fatheree, Ryan Hudson, Robert Murray McKinnell
  • SUBSTITUTED OXADIAZOLE COMPOUNDS
    Publication number: 20130190361
    Abstract: Disclosed are compounds of Formula (I): or stereoisomers, N-oxides, salts, or prodrugs thereof; wherein: Ring A is phenyl or 5- to 6-membered heteroaryl; (i) R1 and R2 are independently C1-C4 alkyl; or (ii) R1 and R2 together with the carbon atom to which they are attached, form a cyclic group; Q is phenyl or 5- to 6-membered heteroaryl substituted with zero to 3 substituents; and R3, L1, L2, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Application
    Filed: September 23, 2011
    Publication date: July 25, 2013
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Jagabandhu Das, Soo Sung Ko
  • BISARYL-BONDED ARYLTRIAZOLONES AND USE THEREOF
    Publication number: 20130190330
    Abstract: The present application relates to novel bisaryl-linked 5-aryl-1,2,4-triazolone derivatives, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: February 25, 2011
    Publication date: July 25, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Chantal Furstner, Joerg Keldenich, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Ingo Pluschkell, Elisabeth Pook, Carsten Schmeck, Hubert Trubel
  • B-RAF KINASE INHIBITORS
    Publication number: 20130190286
    Abstract: The present invention encompasses compounds of general formula (1) where in the groups R0to R3 and L are defined as in claim 1, which are suitable for the 5 treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.
    Type: Application
    Filed: March 25, 2011
    Publication date: July 25, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
  • Pyridine derivatives as sphingosine 1-phosphate (S1P) receptor modulators
    Patent number: 8492410
    Abstract: The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: February 6, 2013
    Date of Patent: July 23, 2013
    Assignee: Allergan, Inc.
    Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
  • Fungicide hydroximoyl-tetrazole derivatives
    Patent number: 8492388
    Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. wherein A represents a tetrazoyl group, Het represents a pyridyl group or a thiazolyl group and X represents various substituents.
    Type: Grant
    Filed: July 3, 2009
    Date of Patent: July 23, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Christian Beier, Jürgen Benting, David Bernier, Isabelle Christian, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
  • 1-substituted pyridyl-pyrazolyl amide compounds and uses thereof
    Patent number: 8492409
    Abstract: The present invention discloses a kind of 1-substituted pyridyl-pyrazolyl amide compounds and uses thereof. The compounds have structures as represented by the general formula I, wherein the definitions of each substituent showed in the specification. The compounds of formula I are novel and have excellent insecticidal and fungicidal activities and can be used for controlling insect pest and diseases.
    Type: Grant
    Filed: July 3, 2009
    Date of Patent: July 23, 2013
    Assignees: Sinochem Corporation, Shenyang Research Institute of Chemical Industry Co., Ltd.
    Inventors: Bin Li, Huibin Yang, Junfeng Wang, Haibo Yu, Hong Zhang, Zhinian Li, Yuquan Song
  • ADAMANTYL DIAMIDE DERIVATIVES AND USES OF SAME
    Publication number: 20130184277
    Abstract: The present invention provides adamantyl diamide derivatives of formula (I): wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
    Type: Application
    Filed: February 1, 2013
    Publication date: July 18, 2013
    Applicant: H. Lundbeck A/S
    Inventor: H. Lundbeck A/S
  • Substituted oxazolidinones and their use
    Patent number: 8487111
    Abstract: The invention relates to novel substituted oxazolidinones, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.
    Type: Grant
    Filed: June 7, 2008
    Date of Patent: July 16, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Swen Allerheiligen, Marcus Bauser, Hartmut Schirok, Ulrich Rester, Stefan Heitmeier, Christoph Gerdes, Georges Von Degenfeld, Elke Dittrich-Wengenroth, Uwe Saatmann, Julia Straβburger, Klaus Münter, Mark Jean Gnoth, Dieter Lang
  • Non-nucleoside reverse transcriptase inhibitors
    Patent number: 8486975
    Abstract: Heteroaromatic compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: March 28, 2011
    Date of Patent: July 16, 2013
    Assignee: Merck Canada Inc.
    Inventors: Jason Burch, Bernard Cote
  • N-HYDROXYAMIDINOHETEROCYCLES AS MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE
    Publication number: 20130177590
    Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as pharmaceutical compositions thereof and methods of use thereof relating to the treatment of cancer and other diseases.
    Type: Application
    Filed: February 28, 2013
    Publication date: July 11, 2013
    Applicant: INCYTE CORPORATION
    Inventor: INCYTE CORPORATION
  • ARYLETHYNYL DERIVATIVES
    Publication number: 20130178456
    Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: February 28, 2013
    Publication date: July 11, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • c-MET protein kinase inhibitors
    Patent number: 8481524
    Abstract: The present invention relates to compounds of formula I useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative disorders.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: July 9, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Lauffer, Pan Li, Nathan Waal, Kira Mcginty, Qing Tang, Steven Ronkin, Luc Farmer, Dean Shannon, Dylan Jacobs
  • FORMULATION AND DOSING OF HSP90 INHIBITORY COMPOUNDS
    Publication number: 20130172333
    Abstract: Provided is a pharmaceutical composition comprising a pharmaceutically acceptable organic solvent, a pharmaceutically acceptable surfactant, and a compound according to the following formula: wherein the variables are defined herein. Optionally, the pharmaceutical composition further comprises a co-solvent. Also provided is a method of using the pharmaceutical composition disclosed herein for the treatment of a patient in need thereof.
    Type: Application
    Filed: May 20, 2011
    Publication date: July 4, 2013
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Neera Jain, Suresh R. Babu, Shweta Kotecha, Hong Yang
  • BENZAMIDES AND RELATED INHIBITORS OF FACTOR XA
    Publication number: 20130172310
    Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.
    Type: Application
    Filed: September 12, 2012
    Publication date: July 4, 2013
    Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
  • Isoxazole derivatives for use as fungicides
    Patent number: 8476446
    Abstract: The present invention relates to isoxazole compounds of formula (I) having fungicidal activity, to agricultural compositions comprising them, and to the use of said compounds and compositions in agriculture for the control of microbial pests, particularly fungal pests, on plants.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: July 2, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Camilla Corsi, Sebastian Volker Wendeborn, Carla Bobbio, Jilali Kessabi, Peter Schneiter, Valeria Grasso, Shy-Fuh Lee, Ulrich Johannes Haas, Micah Gliedt
  • Viral polymerase inhibitors
    Patent number: 8476257
    Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
    Type: Grant
    Filed: December 3, 2008
    Date of Patent: July 2, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Joly, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
  • HETEROARYLS AND USES THEREOF
    Publication number: 20130165483
    Abstract: This invention provides compounds of formula IB: wherein HY, R1, R2, R3, R15, G5, G6, G7, G8, and G9 are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: December 20, 2012
    Publication date: June 27, 2013
    Applicant: MILLENNIUM PHARMACEUTICALS, INC.
    Inventor: Millennium Pharmaceuticals, Inc.