Five-membered Hetero Ring Containing At Least One Nitrogen Ring Atom (e.g., 1,2,3-triazoles, Etc.) Patents (Class 514/359)
  • Patent number: 10266526
    Abstract: The present disclosure provides carboxamides and sulfonamides having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, Y, B, X, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.
    Type: Grant
    Filed: September 9, 2015
    Date of Patent: April 23, 2019
    Assignee: EPIZYME, INC.
    Inventors: Megan Alene Cloonan Foley, Kevin Wayne Kuntz, James Edward John Mills, Lorna Helen Mitchell, Michael John Munchhof, Darren Martin Harvey
  • Patent number: 10232049
    Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
    Type: Grant
    Filed: August 30, 2016
    Date of Patent: March 19, 2019
    Assignee: MADRIGAL PHARMACEUTICALS, INC.
    Inventors: Dinesh U. Chimmanamada, Weiwen Ying
  • Patent number: 10172829
    Abstract: Disclosed are methods and compositions for reducing toxicity associated with infection by Clostridium difficile by inhibiting Clostridium difficile toxin B (TcdB) and/or toxin A (TcdA). Such compounds include ebselen compounds, namely ebselen and its salts, ebselen functional analogues and ebselen structural analogues, as well as certain amide derivatives. This includes Formula I, e.g. 1-methyl-3-phenylpropylamine, Formula II, e.g., 2,2?-diselane-1,2-diylbis[N-(2,4-difluorophenyl)benzamide]; and Formula III, e.g. 2-(2-methoxy-5-methylphenyl)-1, 2-benzoselenazol-3-one. The present compositions may be comprised in a colon-retentive formulation that increases residence of and/or release of the compound in the area where the infection is active.
    Type: Grant
    Filed: June 23, 2015
    Date of Patent: January 8, 2019
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Kristina Oresic Bender, Aaron Puri, Aimee Shen, Matthew S. Bogyo
  • Patent number: 10125102
    Abstract: Disclosed are compounds of formula I as described herein, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also disclosed are pharmaceutical compositions comprising at least one such compound, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
    Type: Grant
    Filed: March 9, 2015
    Date of Patent: November 13, 2018
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Pravin L. Kotian, Yarlagadda S. Babu, Minwan Wu, Venkat R. Chintareddy, V. Satish Kumar, Weihe Zhang
  • Patent number: 10064411
    Abstract: The invention provides an ectoparasiticidal formulation which comprises an ectoparasiticidal agent, preferably the pyrethroid permethrin, as the pesticidally-active ingredient, together with a crystallization inhibitor selected from the group consisting of alkyl-substituted pyrrolidones, and optionally, one or more organic solvents and/or co-solvents. Preferably, the crystallization inhibitor is N-octyl pyrrolidone, and the organic solvent, if present, preferably comprises diethylene glycol monoethyl ether. The ectoparasiticidal formulation surprisingly yields a significantly enhanced speed of kill. Methods for manufacturing the formulation, as well as methods for treating animals infested with ectoparasites, are also disclosed.
    Type: Grant
    Filed: April 9, 2018
    Date of Patent: September 4, 2018
    Assignee: THE HARTZ MOUNTAIN CORPORATION
    Inventors: W. Lance Hemsarth, Keith Goldman, Ellen McGarvey
  • Patent number: 10059704
    Abstract: A compound having the following general formula (I): wherein: X is a nitrogen atom and Y is a carbon atom; or X is a carbon atom and Y is a nitrogen atom; the Ar group is an aryl or heteroaryl group; and the RN and RN? groups, together with the carbon atoms to which they are bound, form a monocyclic or bicyclic azacycloalkane group. The pharmaceutically acceptable salts thereof, the hydrates or polymorphic crystalline structures thereof, and to the racemates, diastereoisomers, or enantiomers thereof are also described.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: August 28, 2018
    Assignees: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (C.N.R.S.), INSTITUT NATIONAL DE LA SANTA ET DE LA RECHERCHE MEDICALE (INSERM)
    Inventors: Sylvain Routier, Franck Suzenet, Frederic Pin, Sylvie Chalon, Johnny Vercouillie, Denis Guilloteau
  • Patent number: 10040761
    Abstract: A branched hetero polyethylene glycol according to the present invention is represented by the formula [1]: wherein X and Y represent each an atomic group containing at least a functional group which reacts with a functional group present in a bio-functional molecule to form a covalent bond and the functional group contained in the atomic group X and the functional group contained in the atomic group Y are different from each other; s is an integer of 2 to 8, which represents the number of polyethylene glycol chains; n is the number of average added moles for the polyethylene glycol chain and 20?n?2000; and E is a branching linker moiety having s-valent bonding valency for the polyethylene glycol chains and having monovalent bonding valency for the functional group Y.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: August 7, 2018
    Assignee: NOF CORPORATION
    Inventors: Yuji Yamamoto, Hiroki Yoshioka, Fumiaki Manabe
  • Patent number: 9999593
    Abstract: The present invention relates to an ophthalmic aqueous composition containing PGF2? analogs for treating ocular hypertension and glaucoma, to a method for treating ocular hypertension and glaucoma by administering said composition to a subject in need of such treatment, and to a method for increasing aqueous solubility and stability of PGF2? analogs in an aqueous composition.
    Type: Grant
    Filed: May 28, 2009
    Date of Patent: June 19, 2018
    Assignees: SANTEN PHARMACEUTICAL CO., LTD., ASAHI GLASS CO., LTD.
    Inventors: Timo Reunamaki, Pertti Pellinen, Olli Oksala, Kari Lehmussaari
  • Patent number: 9956243
    Abstract: The present invention relates to a pharmaceutical product comprising a) as a first component an inhibitor of the MDM2-p53 interaction such as, for example: and b) as a second component cytarabine; as a combined preparation for the sequential or simultaneous use in the treatment of cancer.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: May 1, 2018
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Brian Higgins, Gwen Nichols, Kathryn E. Packman
  • Patent number: 9955696
    Abstract: The invention provides an ectoparasiticidal formulation which comprises an ectoparasiticidal agent, preferably the pyrethroid tetramethrin, as the pesticidally-active ingredient, together with a crystallization inhibitor selected from the group consisting of alkyl-substituted pyrrolidones, and optionally, one or more organic solvents and/or co-solvents. Preferably, the crystallization inhibitor is N-octyl pyrrolidone, and the organic solvent, if present, preferably comprises diethylene glycol monoethyl ether. The ectoparasiticidal formulation surprisingly yields a significantly enhanced speed of kill. Methods for manufacturing the formulation, as well as methods for treating animals infested with ectoparasites, are also disclosed.
    Type: Grant
    Filed: August 11, 2016
    Date of Patent: May 1, 2018
    Assignee: THE HARTZ MOUNTAIN CORPORATION
    Inventors: W. Lance Hemsarth, Keith Goldman, Ellen McGarvey
  • Patent number: 9938272
    Abstract: Provided is a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein X is selected from a 3-9 membered carbon ring or a ring which is formed by 3-9 membered carbocyclic ring fused with benzo ring, and a 4-10 membered heterocyclic ring or a ring which is formed by 4-10 membered heterocyclic ring fused with benzo ring; Y and Z are independently selected from 4-9 membered saturated heterocyclic rings respectively; R1-3 are independently selected from H, F, Cl, Br, I, CN, OH, SH, NH2, CHO, COOH respectively, or selected from the group, optionally substituted by R01, consisting of C1-10 alkyl, C1-10 heteroalkyl, C3-10 cyclohydrocarbyl, C3-10 heterocyclohydrocarbyl, C1-10 alkyl substituted by C3-10 cyclohydrocarbyl or C3-10 heterocyclohydrocarbyl, and C1-10 heteroalkyl substituted by C3-10 cyclohydrocarbyl or C3-10 heterocyclohydrocarbyl.
    Type: Grant
    Filed: May 18, 2015
    Date of Patent: April 10, 2018
    Assignee: North China Pharmaceutical Company., Ltd.
    Inventors: Zhaozhong Ding, Guanghua Lai, Shuhui Chen, Xiaobing Yan
  • Patent number: 9926295
    Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing hepatitis C virus (HCV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment or prevention of HCV infection.
    Type: Grant
    Filed: April 15, 2015
    Date of Patent: March 27, 2018
    Assignees: Cocrystal Pharma, Inc., Emory University
    Inventors: Steven J. Coats, Richard Anthony Whitaker, Tamara Rosario McBrayer, Junxing Shi, Franck Amblard, Hongwang Zhang, Longhu Zhou, Raymond F. Schinazi
  • Patent number: 9907752
    Abstract: Provided herein are pharmaceutical compositions comprising nitrogen mustard, for example bendamustine hydrochloride, solid dispersions substantially free of degradants. Also provided are methods of producing and administering nitrogen mustards and in particular bendamustine hydrochloride solid dispersions substantially free of degradants. The pharmaceutical compositions can be used for any disease that is sensitive to treatment with bendamustine hydrochloride, such as neoplastic diseases.
    Type: Grant
    Filed: April 20, 2016
    Date of Patent: March 6, 2018
    Inventor: Vasilios Voudouris
  • Patent number: 9877955
    Abstract: Methods and compositions for treating disorders of the nail and nail bed. Such compositions contain a vehicle in which all components of the composition are dissolved, suspended, dispersed, or emulsified, a non-volatile solvent, a wetting agent, and a pharmaceutically active ingredient that is soluble in the non-volatile solvent and/or a mixture of the vehicle and the non-volatile solvent, and which composition is effective in treating a disorder of the nail or nail bed.
    Type: Grant
    Filed: October 24, 2016
    Date of Patent: January 30, 2018
    Assignee: Dow Pharmaceutical Sciences, Inc.
    Inventors: Gareth Winckle, Gregory T. Fieldson
  • Patent number: 9861698
    Abstract: Methods and compositions for treating disorders of the nail and nail bed. Such compositions contain a vehicle in which all components of the composition are dissolved, suspended, dispersed, or emulsified, a non-volatile solvent, a wetting agent, and a pharmaceutically active ingredient that is soluble in the non-volatile solvent and/or a mixture of the vehicle and the non-volatile solvent, which composition has a surface tension of 40 dynes/cm or less and has continuing spreadability, and which composition is effective in treating a disorder of the nail or nail bed.
    Type: Grant
    Filed: September 19, 2014
    Date of Patent: January 9, 2018
    Assignee: DOW PHARMACEUTICAL SCIENCES, INC.
    Inventors: Gareth Winckle, Gregory T. Fieldson
  • Patent number: 9713613
    Abstract: The present invention relates to methods of treating a disease related to cell hyper-proliferation via administration of a therapeutically effective amount of a compound having a general tripartite structure A-B-C. In the tripartite structure A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. The methods may utilize particular compounds, for example, having a piperidinyl, a pyrrolinyl or pyridinyl A ring, a thiazole B ring, and a phenyl C ring which may be further substituted independently.
    Type: Grant
    Filed: November 13, 2015
    Date of Patent: July 25, 2017
    Inventors: Motonari Uesugi, Salih J. Wakil, Lutfi Abu-Elheiga, Mizuki Watanabe
  • Patent number: 9707273
    Abstract: Peptides with a sequence length from 13 to 50 amino acids, the N-terminal region of said peptides consisting in the sequence HXaa1EGTFTSDXaa2SXaa3Xaa4 (SEQ ID NO: 1) wherein: Xaa1 is an amino acid selected from alanine and glycine; Xaa2 is an amino acid selected from valine and leucine; Xaa3 is an amino acid selected from serine and lysine; Xaa4 is an amino acid selected from tyrosine and glutamine; and Hystidine is the N-terminal residue; for use in the topical treatment and/or prevention of retinal neurodegenerative diseases, in particular diabetic retinopathy are described. Pharmaceutical topical compositions for use in the topical treatment and/or prevention of these diseases are also described.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: July 18, 2017
    Assignee: FUNDACIÓ HOSPITAL UNIVERSITARI VALL D'HEBRON—INSTITUT DE RECERCA
    Inventors: Rafael Simó Canonge, Cristina Hernández Pascual
  • Patent number: 9566272
    Abstract: Methods and compositions for treating disorders of the nail and nail bed. Such compositions contain a vehicle in which all components of the composition are dissolved, suspended, dispersed, or emulsified, a non-volatile solvent, a wetting agent, and a pharmaceutically active ingredient that is soluble in the non-volatile solvent and/or a mixture of the vehicle and the non-volatile solvent, and which composition is effective in treating a disorder of the nail or nail bed.
    Type: Grant
    Filed: June 30, 2015
    Date of Patent: February 14, 2017
    Assignee: DOW PHARMACEUTICAL SCIENCES, INC.
    Inventors: Gareth Winckle, Gregory T. Fieldson
  • Patent number: 9540322
    Abstract: The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.
    Type: Grant
    Filed: May 4, 2011
    Date of Patent: January 10, 2017
    Assignee: Yale University
    Inventors: William L. Jorgensen, Richard J. Bucala
  • Patent number: 9505727
    Abstract: The present invention provides compounds of formula I which are capable of inhibition of the activation of hNav1.1 or hNav1.6 sodium channels in neurons. Pharmaceutical compositions comprising these compounds are also provided. Methods for prevention and treatment of neurological disorders, including, for example, seizures and seizure disorders, including Lennox-Gastaut Syndrome, Dravet syndrome, epileptic encephalopathies, autism, Familial hemiplegic migraine (FHM), anxiety disorders, including Post-traumatic stress disorder (PTSD), panic disorder and obsessive-compulsive disorder, neuropathic pain, and Rett syndrome by administration of these compounds are also provided.
    Type: Grant
    Filed: July 31, 2015
    Date of Patent: November 29, 2016
    Assignee: The Johns Hopkins University
    Inventors: Frank Bosmans, Dimpy Kalia
  • Patent number: 9468641
    Abstract: Disclosed herein is an anti-inflammatory pharmaceutical composition comprising a benzopyranyl tetracycle compound represented by Chemical Formula 1 as an active ingredient. The compound exhibits excellent anti-inflammatory activity by perturbing the post-translational modification of the inflammation mediator HMGB, and thus finds applications in pharmaceutical compositions superior in the treatment or prevention of inflammation-related diseases.
    Type: Grant
    Filed: April 16, 2015
    Date of Patent: October 18, 2016
    Assignees: SEOUL NATIONAL UNIVERSITY R&DB FOUNDATION, KYUNGPOOK NATIONAL UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION, KYUNGPOOK NATIONAL UNIVERSITY HOSPITAL
    Inventors: Seung Bum Park, Sanghee Lee, Ja Young Koo, Donghyun Lim, Jongmin Park, Kyoungho Suk, Youngpyo Nam
  • Patent number: 9464049
    Abstract: The present invention relates to compounds of general formula wherein R1, R2, R3, R4, R5 and R6 are as defined herein are useful for the treat of neurological and neuropsychiatric conditions.
    Type: Grant
    Filed: March 10, 2016
    Date of Patent: October 11, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ravi Jagasia, Roland Jakob-Roetne, Jens-Uwe Peters, Juergen Wichmann
  • Patent number: 9453048
    Abstract: There are disclosed compounds of formula (I) that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing said compounds.
    Type: Grant
    Filed: August 6, 2013
    Date of Patent: September 27, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Heidi L. Perez, Donna D. Wei, Kyoung S. Kim
  • Patent number: 9383348
    Abstract: The present invention relates to methods of treating subjects with alveolar capillary membrane injury or methods of preventing alveolar capillary membrane injury in subjects, with the methods comprising administering to the subjects a therapeutically effective amount of ergothioneine and a pharmaceutically acceptable carrier. The invention also relates to methods of screening candidate compounds for their ability to mitigate the effects of alveolar capillary membrane injury.
    Type: Grant
    Filed: June 22, 2009
    Date of Patent: July 5, 2016
    Inventor: John E. Repine
  • Patent number: 9316631
    Abstract: The invention relates to methods for identifying ER-stress inducing compounds that target cancer stem cells. In some aspects, the invention relates to treatment methods that use ER-stress inducing compounds that specifically target cancer stem cells for inhibiting the growth and/or survival of cancer stem cells in a subject in need thereof. Other aspects of the invention relate to the use of cancer stem cell biomarkers in the selection of a treatment for inhibiting the growth and/or survival of cancer stem cells in a subject in need thereof.
    Type: Grant
    Filed: October 18, 2013
    Date of Patent: April 19, 2016
    Inventors: Piyush Gupta, Yuxiong Feng
  • Patent number: 9302009
    Abstract: Methods and compositions for treating disorders of the nail and nail bed. Such compositions contain a vehicle in which all components of the composition are dissolved, suspended, dispersed, or emulsified, a non-volatile solvent, a wetting agent, and a pharmaceutically active ingredient that is soluble in the non-volatile solvent and/or a mixture of the vehicle and the non-volatile solvent, which composition has a surface tension of 40 dynes/cm or less and has continuing spreadability, and which composition is effective in treating a disorder of the nail or nail bed.
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: April 5, 2016
    Assignee: Dow Pharmaceutical Sciences, Inc.
    Inventors: Gareth Winckle, Gregory T. Fieldson
  • Patent number: 9303104
    Abstract: A process for photopolymerizing a photopolymerizable compound having at least one ethylenically unsaturated double bond, comprises contacting said photopolymerizable compound with a photoactive oxide and irradiating it, wherein the photoactive oxide includes one or more moieties together with a moiety wherein there are at least 2 atoms between moiety I and moiety II in the additive and where X represents an oxygen or sulphur atom. Novel compounds which exhibit beneficial effects on cure in the presence of oxygen, which may be especially advantageous when LEDs are used, are also described.
    Type: Grant
    Filed: July 17, 2013
    Date of Patent: April 5, 2016
    Assignee: LAMBSON LIMITED
    Inventors: David George Anderson, Kevin Harper, Alan Thomas Rose, Petr Sehnal
  • Patent number: 9249135
    Abstract: Provided are an agent for the treatment and/or prophylaxis of a mood disorder comprising, as an active ingredient, a thiazole derivative represented by the formula (I) wherein R1 represents aryl or the like, and R2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof, and the like.
    Type: Grant
    Filed: September 2, 2010
    Date of Patent: February 2, 2016
    Assignee: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Koji Yamada, Tomoyuki Kanda
  • Patent number: 9220273
    Abstract: Provided are mosquito larvicide compositions comprising a mineral oil and a methylated coconut oil. The compositions may further comprise a silicone and at least one surfactant. The compositions can kill mosquito larvae in swamps, floodwater areas, and other areas where mosquitoes develop. Further provided are methods for mosquito control. The methods may comprise coating the surface of a body of water.
    Type: Grant
    Filed: March 13, 2015
    Date of Patent: December 29, 2015
    Assignee: Clarke Mosquito Control Products, Inc.
    Inventors: Marie Elizabeth Saunders, Jonathan David Ostrowski, Michael Dean Willis, Darryl Ramoutar, Joanna Maria Tyszko
  • Patent number: 9139573
    Abstract: Methods of treating a TRPC5 mediated disorder in a subject by administering an effective amount of a TRPC5 antagonist, such as a compound disclosed herein, are described.
    Type: Grant
    Filed: December 10, 2013
    Date of Patent: September 22, 2015
    Assignee: HYDRA BIOSCIENCES, INC.
    Inventors: Jayhong A. Chong, Christopher Fanger, Magdalene M. Moran, Elisha Singer, Timothy Strassmaier, Howard Ng
  • Patent number: 9107812
    Abstract: The present invention relates to a liquid pharmaceutical composition containing an N-phenylpyrazole derivative as active ingredient and alpha-(tetrahydrofuranyl)-omega-hydroxypoly(oxy-1,2-ethanediyl) as solvent for the treatment and/or prevention of infestations with fleas in domestic animals.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: August 18, 2015
    Assignee: VIRBAC
    Inventor: Guy Derrieu
  • Patent number: 9089570
    Abstract: This invention provides methods and compositions useful for treating early and late stage metastatic cancer to prevent or treat acquired resistance due to gene amplification or mutation in response to chemotherapeutic and/or targeted drugs. In particular, the methods and compositions include carboxiamidotriazole orotate (CTO) alone or in combination with specific regimens of chemotherapeutic and/or targeted drugs designed to overcome the genomic resistance raised to prior therapy.
    Type: Grant
    Filed: April 1, 2013
    Date of Patent: July 28, 2015
    Assignee: TACTICAL THERAPEUTICS INC
    Inventor: Rashida A Karmali
  • Patent number: 9051281
    Abstract: The present invention relates to substituted triazole compounds of the formula (I): and pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for modulating SCD activity.
    Type: Grant
    Filed: June 21, 2013
    Date of Patent: June 9, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: Anne Marie Jeanne Bouillot, Alain Laroze, Lionel Trottet
  • Publication number: 20150133511
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, pulmonary fibrosis . . . .
    Type: Application
    Filed: June 17, 2013
    Publication date: May 14, 2015
    Inventors: Stephen Deems Gabriel, Matthew Michael Hamilton, Matthew C. Lucas, Yimin Qian, Achyutharao Sidduri
  • Publication number: 20150133512
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, pulmonary fibrosis.
    Type: Application
    Filed: June 17, 2013
    Publication date: May 14, 2015
    Inventors: Stephen Deems Grabriel, Matthew Michael Hamilton, Yimin Qian, Achyutharao Sidduri
  • Patent number: 9023850
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: May 5, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: George Philip Lahm, Thomas Francis Pahutski, Jr.
  • Patent number: 9024041
    Abstract: There is provided a compound of formula (I): wherein: J represents (A): or (B): compositions comprising same, processes for preparing said compounds and use thereof in treatment, particularly in the treatment of inflammatory disease, such as asthma, COPD and 15 rheumatoid arthritis.
    Type: Grant
    Filed: April 8, 2011
    Date of Patent: May 5, 2015
    Assignee: Respivert Ltd.
    Inventors: John King-Underwood, Peter John Murray, Jonathan Gareth Williams, Ildiko Buck, Stuart Thomas Onions
  • Patent number: 9018207
    Abstract: The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of neuropathic pain, including mechanical hyperalgesia, thermal or mechanical allodynia, diabetic pain and entrapment pain, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of neuropathic conditions.
    Type: Grant
    Filed: March 28, 2014
    Date of Patent: April 28, 2015
    Assignee: Spinifex Pharmaceuticals Pty Ltd
    Inventors: Maree Therese Smith, Bruce Douglas Wyse
  • Publication number: 20150111888
    Abstract: The present invention provides a small compound targeting at TACC3. The present invention further provides a drug, particularly, an anticancer agent, comprising the small compound targeting at TACC3. A compound represented by the general formula (I) or a pharmaceutically acceptable salt, solvate, or ester derivative thereof binds to TACC3 and inhibits cell growth. Thus, these compounds can be used as drugs, particularly, anticancer agents.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 23, 2015
    Inventors: Ryoji Yao, Hiroyuki Osada, Yasumitsu Kondoh
  • Patent number: 9012480
    Abstract: The invention is directed to formulations and methods of treating a migraine and/or cluster headache with a serotonin agonist, pharmaceutically acceptable salt thereof, or derivative thereof.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: April 21, 2015
    Assignee: AFGIN Pharma LLC
    Inventor: Ronald Aung-Din
  • Publication number: 20150105378
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20150105403
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 16, 2015
    Inventors: Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Jackaline D. Julien, Johnny Y. Nagasawa, Karensa L. Douglas, Celine Bonnefous, Andiliy G. Lai
  • Publication number: 20150105324
    Abstract: The invention described herein pertains to compositions and methods for treating PTSD and related diseases. In particular, the invention described herein pertains to compositions and methods for treating PTSD and related diseases by administering modulators of NMDA NR2-PSD95-nNOS signaling.
    Type: Application
    Filed: April 26, 2013
    Publication date: April 16, 2015
    Inventors: Anantha Shekhar, Yvonne Lai
  • Publication number: 20150104387
    Abstract: Prostate-specific membrane antigen (PSMA) targeting compounds are described. Uses of the compounds for imaging, therapy, cell sorting, and tumor mapping are also described.
    Type: Application
    Filed: April 2, 2014
    Publication date: April 16, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: MARTIN G. POMPER, RONNIE C. MEASE, YING CHEN, Sangeeta Ray
  • Publication number: 20150099696
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed to compounds suitable for the treatment of Disease conditions such as hyperlipidemia.
    Type: Application
    Filed: June 26, 2012
    Publication date: April 9, 2015
    Applicant: Cadila Healthcare Limited
    Inventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pandya, Sairam V.V.M. Kalapatapu
  • Publication number: 20150099781
    Abstract: Described herein are compounds, and pharmaceutically acceptable salts and prodrugs thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound of the invention selectively inhibits a parasitic IMPDH versus a host IMPDH. Further, the invention provides pharmaceutical compositions comprising one or more compounds of the invention. The invention also relates to methods of treating various parasitic and bacterial infections in mammals. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.
    Type: Application
    Filed: December 16, 2014
    Publication date: April 9, 2015
    Inventors: Lizbeth K. Hedstrom, Gregory D. Cuny, Deviprasad R. Gollapalli, Sivapriya Kirubakaran, Sushil K. Maurya, Boris Striepen, Suresh K. Gorla, Corey R. Johnson, Mandapati Kavitha, Jihan Khan
  • Publication number: 20150094337
    Abstract: The present invention provides a heterocyclic group contained amino-methanol derivative, and salt, a preparation method and use thereof, and belongs to the medical field. The heterocyclic group contained amino-methanol derivative and the salt thereof of the present invention are used for preparing medicines for immune suppression and for the treatment of organ transplant rejection, or medicines for treating immune mediated inflammatory diseases, such as multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis.
    Type: Application
    Filed: December 8, 2014
    Publication date: April 2, 2015
    Inventors: Xingmin Zhang, Ensi Wang, Jing Guo, Shengxiu Niu, Zhuolin Dai, Nan Zheng, Liping Ji, Zhenfang Wang, Tie Liang
  • Publication number: 20150094294
    Abstract: The present disclosure provides compounds, specifically pyrimidin-4,6-dicarboxylic acid amide derivatives, or pharmaceutically acceptable salts thereof and pharmaceutical compositions containing said compounds. Also provided are methods for treating a mammal having malaria, or killing or inhibiting the growth of a Plasmodium species, comprising administering to said mammal or contacting said Plasmodium species with, an effective amount of a pyrimidin-4,6-dicarboxylic acid amide derivative.
    Type: Application
    Filed: February 28, 2013
    Publication date: April 2, 2015
    Inventors: Richard W. Scott, Robert W. Kavash, Wenxi Pan, Katie Freeman, Michael J. Costanzo, Doron Greenbaum, Yongjiang Xu, Trevor Young
  • Patent number: 8993612
    Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: March 31, 2015
    Assignee: Rhizen Pharmaceuticals SA
    Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Kanthikiran V S Varanasi, Gayatri Swaroop Merikapudi, Swaroop Kumar V. S. Vakkalanka
  • Patent number: 8993614
    Abstract: There are provided compounds of the formula wherein X, Y, Z, R1, R2, R3 and R4 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: March 31, 2015
    Assignee: F. Hoffmann-La Roche AG
    Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Binh Thanh Vu, Chunlin Zhao, Daniel Fishlock