The Additional Hetero Ring Contains Ring Nitrogen Patents (Class 514/210.2)
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Patent number: 10544108Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.Type: GrantFiled: November 28, 2018Date of Patent: January 28, 2020Assignee: Karyopharm Therapeutics Inc.Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
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Patent number: 10500195Abstract: Compounds of Formula (I), or a stereoisomer or a pharmaceutically acceptable salt thereof, their preparation, pharmaceutical compositions comprising such compounds and their use in treating and/or preventing bacterial infections are disclosed.Type: GrantFiled: April 24, 2017Date of Patent: December 10, 2019Assignee: WOCKHARDT LIMITEDInventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Piyush Ambalal Patel, Rajib Bhuniya, Sachin Bhagwat, Swapna Shripad Takalkar, Rajesh Chavan, Anusuya Patel, Vipul Rane, Mahesh Vithalbhai Patel
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Patent number: 10471051Abstract: The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R1 to R8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.Type: GrantFiled: September 1, 2017Date of Patent: November 12, 2019Assignee: Asana BioSciences, LLCInventors: Aranapakam M. Venkatesan, Scott K. Thompson, Roger A. Smith, Sanjeeva P. Reddy, Raghava Reddy Kethiri, Purushottam M. Dewang, Gurulingappa Hallur, Chandrika Mulakala, Ramesh Mullangi, Mohd Zainuddin
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Patent number: 10457826Abstract: A polymer-bound lead refill for writing, drawing and/or painting devices, in particular for pencils or colored pencils, including at least one binding agent, at least one wax, at least one coloring agent and at least one filling agent. The lead refill including at least one surfactant.Type: GrantFiled: November 7, 2014Date of Patent: October 29, 2019Assignee: STAEDTLER MARS GMBH & CO. KGInventor: Johannes Herbolsheimer
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Patent number: 10441572Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.Type: GrantFiled: May 2, 2018Date of Patent: October 15, 2019Assignee: Aptinyx Inc.Inventors: John A. Lowe, III, M. Amin Khan
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Patent number: 10441571Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.Type: GrantFiled: May 2, 2018Date of Patent: October 15, 2019Assignee: Aptinyx Inc.Inventors: John A. Lowe, III, M. Amin Khan
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Patent number: 10421761Abstract: Compounds active on protein kinases and methods for regulating protein kinase pathways are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: GrantFiled: December 11, 2017Date of Patent: September 24, 2019Assignee: Plexxikon Inc.Inventors: Chao Zhang, Klaus-Peter Hirth, Prabha N. Ibrahim, Marika Nespi, Songyuan Shi, Wayne Spevak, Gaston G. Habets, Elizabeth A. Burton
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Patent number: 10385070Abstract: The invention relates to chroman spirocyclic piperidine amide derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: February 16, 2012Date of Patent: August 20, 2019Assignee: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Sabina Hadida-Ruah, Mark Thomas Miller, Edward Adam Kallel, Brian Richard Bear, Vijayalaksmi Arumugam, Michael Paul Deninno, Jinglan Zhou, Johnny Uy, Bryan A. Frieman
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Patent number: 10369130Abstract: The present invention relates to novel antibacterial compounds, pharmaceutical compositions containing them and their use as antimicrobials.Type: GrantFiled: December 11, 2015Date of Patent: August 6, 2019Assignee: AZIEN DE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.Inventors: Rosella Ombrato, Barbara Garofalo, Giorgina Mangano, Alessandra Capezzone De Joannon, Gaia Corso, Gabriele Magaro′, Guido Furlotti, Tommaso Iacoangeli
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Patent number: 10343992Abstract: The present invention relates to novel compounds and method for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (II) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R8, R9, R10, R12, Z, Y and m are as defined herein.Type: GrantFiled: March 24, 2016Date of Patent: July 9, 2019Assignee: Missions Therapeutics LimitedInventors: Alison Jones, Mark Kemp, Martin Stockley, Karl Gibson, Gavin Whitlock
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Patent number: 10344020Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.Type: GrantFiled: October 13, 2016Date of Patent: July 9, 2019Assignee: Bristol-Myers Squibb CompanyInventors: Imadul Islam, Srinivasan Thangathirupathy, Jayakumar Sankara Warrier, Srinivas Cheruku, Poornima Shetty, Grandhi Venkat Ram Krishna Mohan Gupta, John E. Macor
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Patent number: 10301289Abstract: The present invention relates to a process for preparing 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5-ol (I—enol form) or 2-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1,2-dihydro-3H-pyrazol-3-one (I—keto form) and sodium 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5-olate (II) from 1,2,3-triazole (III), methyl bromoacetate (IV-Me-Br) or ethyl bromoacetate (IV-Et-Br), 4,6-dichloropyrimidine (VIII), morpholine (IX) and hydrazine (XII).Type: GrantFiled: May 6, 2013Date of Patent: May 28, 2019Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Hans-Christian Militzer, Johannes Eggert
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Patent number: 10280160Abstract: The invention relates to a compound of Formula I and methods of treating CFTR (cystic fibrosis transmembrane conductance regulator) mediated diseases, in particular cystic fibrosis, comprising the step of administering a therapeutically effective amount of a compound of Formula I to a patient in need thereof:Type: GrantFiled: June 6, 2017Date of Patent: May 7, 2019Assignee: FLATLEY DISCOVERY LAB, LLCInventor: Bridget M. Cole
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Patent number: 10258621Abstract: Certain adjunctive therapies comprising a kynurenine-3-monooxygenase inhibitor and an antiviral agent for treating HIV-related disorders are provided herein. These disorders include AIDS dementia complex, AIDS-induced encephalopathy, HIV-associated neurocognitive disorder, asymptomatic neurocognitive impairment, minor neurocognitive disorder, minor cognitive motor disorder, vacuolar myelopathy, peripheral neuropathies, and polymyositis. Also provided are pharmaceutical compositions comprising a kynurenine-3-monooxygenase inhibitor and an antiviral agent.Type: GrantFiled: July 17, 2015Date of Patent: April 16, 2019Assignee: CHDI Foundation, Inc.Inventors: Celia Dominguez, Ignacio Muñoz-Sanjuán, Leticia Toledo-Sherman
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Patent number: 10172952Abstract: The invention relates to inhibitory compounds of a p38 MAP kinase having a structure of type (I)-(VII) which can be used for the treatment or prophylaxis of adhesion. Pharmaceutical compositions are disclosed containing an effective amount of the substance SB203580 or one or more of the conjugated compounds of type (I)-(VII) or a combination thereof, and a pharmaceutically acceptable carrier, a diluent or an excipient. Also disclosed is the use of the substance SB203580 as an agent having anti-adhesion activity. Also disclosed is a method for the prophylaxis and/or treatment of a disease or a condition in which there is a possibility of the formation and/or growth of adhesions, which makes it possible to dispense with the additional administration of a preparation in the post-operative period.Type: GrantFiled: November 18, 2013Date of Patent: January 8, 2019Assignee: Joint Stock Company “Pharmasyntez”Inventors: Mikhail Gennadievich Shurygin, Irina Aleksandrovna Shurygina
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Patent number: 10173995Abstract: The present invention is directed to novel pyridines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The present invention discloses compounds of Formulas I and II. The compounds and compositions of the present invention have protein kinases inhibitory activities and are expected to be useful for the treatment of protein kinases mediated diseases and conditions.Type: GrantFiled: January 11, 2014Date of Patent: January 8, 2019Assignee: Teligene Ltd.Inventor: Dawei Zhang
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Patent number: 10174038Abstract: Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.Type: GrantFiled: June 9, 2017Date of Patent: January 8, 2019Assignee: Gilead Sciences, Inc.Inventors: Hon Chung Hui, Jay P. Parrish, Michael Sangi, Dustin Siegel, David Sperandio, Hai Yang
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Patent number: 10174002Abstract: A compound having the structure of Formula II, or a stereoisomer, tautomer, or a pharmaceutically acceptable salt thereof that is useful as CFTR modulator. Further, a method of using the compound and pharmaceutical composition comprising the compound are provided for treating diseases in lungs, pancreas, gastrointestinal system, sinuses, reproductive system, and the sweat glands.Type: GrantFiled: October 6, 2016Date of Patent: January 8, 2019Assignee: NuBridge BioSciencesInventors: Lin Zhang, Yu Ge
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Patent number: 10160744Abstract: The present invention relates to quinoline compounds of formula I wherein the variables are defined as in the claims and the description. The invention further relates to a pharmaceutical composition containing such compounds, to their use as modulators of the 5-HT6 receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of the 5-HT6 receptor, and to methods for preventing or treating conditions and disorders which respond to the modulation of the 5-HT6 receptor.Type: GrantFiled: March 14, 2017Date of Patent: December 25, 2018Assignee: ABBVIE DEUTSCHLAND GMBH & CO. KGInventors: Hervé Geneste, Andreas Haupt, Frauke Pohlki, Ana Lucia Relo, Liliane Unger, Karsten Wicke
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Patent number: 10155777Abstract: A substituted trans-cycloheptene according to formula (I); wherein: a) Z and L are each selected from the group consisting of SiR1R2, CH2, CHOH, and CHR2; R1 is phenyl or CH3; R2 is phenyl, CH3, (CH2)nCN, or (CH2)nOH, wherein n is an integer from 1 to 5; Ra and Rb are each individually selected from the group consisting of H, OH, and CH3; and Z and L are not both SiR1R2; or b) Z is BocN, L is CH2, Ra is H, and Rb is H; or c) Z is C=0, L is CH2, Ra is H, and Rb is H.Type: GrantFiled: April 7, 2016Date of Patent: December 18, 2018Assignee: UNIVERSITY OF DELAWAREInventors: Joseph Fox, Han Zhang, Yinzhi Fang
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Patent number: 10125130Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein A, L, D, R1-R15, w, x, y, and z are defined herein. The novel cycloalkyl-linked diheterocycle derivatives that are useful in the treatment of abnormal cell growth, such as cancer, in mammals. The present invention also relates to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.Type: GrantFiled: November 29, 2017Date of Patent: November 13, 2018Assignee: Pfizer Inc.Inventors: Aaron Craig Burns, Michael Raymond Collins, Samantha Elizabeth Greasley, Robert Louis Hoffman, Peter Qinhua Huang, Robert Steven Kania, Pei-Pei Kung, Maria Angelica Linton, Lakshmi Sourirajan Narasimhan, Paul Francis Richardson, Daniel Tyler Richter, Graham Smith
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Patent number: 10071957Abstract: The invention provides novel compounds having the general formula (I) and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, ring D, R1, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.Type: GrantFiled: July 5, 2013Date of Patent: September 11, 2018Assignees: GENENTECH, INC., XENON PHARMACEUTICALS INC.Inventors: Christoph Martin Dehnhardt, Sultan Chowdhury, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Brian Safina, Daniel P. Sutherlin
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Patent number: 10059667Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.Type: GrantFiled: February 3, 2015Date of Patent: August 28, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Harry Chobanian, Duane DeMong, Yan Guo, Zhiyong Hu, Michael Miller, Barbara Pio, Christopher W. Plummer, Dong Xiao, Cangming Yang
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Patent number: 10059687Abstract: The present disclosure relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyridine derivative compounds, and compositions (including pharmaceutical compositions) that include these compounds. The subject compounds and compositions are useful for inhibition of at least one histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer or neoplastic disease, such as prostate cancer, breast cancer, bladder cancer, lung cancer, melanoma, retinoblastoma, or multiple endocrine neoplasia type 1.Type: GrantFiled: December 27, 2016Date of Patent: August 28, 2018Assignee: Celgene Quanticel Research, Inc.Inventors: Young K. Chen, Michael Brennan Wallace
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Patent number: 10052308Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.Type: GrantFiled: October 28, 2016Date of Patent: August 21, 2018Assignee: Aptinyx Inc.Inventors: John A. Lowe, III, M. Amin Khan
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Patent number: 10017477Abstract: The present invention provides kinase inhibitors, such as compounds of Formula (I) and Formula (II). The compounds may covalently or non-covalently bind a kinase (e.g., Janus kinase 3 (JAK3)). Also provided are pharmaceutical compositions, kits, methods, and uses that involve the compounds for reducing the activity of a kinase and/or treating and/or preventing a condition associated with aberrant activity of a kinase (e.g., a proliferative disease, inflammatory disorder, autoimmune disorder, painful condition, and/or viral infection).Type: GrantFiled: April 23, 2015Date of Patent: July 10, 2018Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Li Tan
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Patent number: 9981945Abstract: A compound having the structure of Formula II, or a stereoisomer, tautomer, or a pharmaceutically acceptable salt thereof: The compound is useful as CFTR modulator. Further, a method of using the compound and pharmaceutical composition comprising the compound are provided for treating diseases in lungs, pancreas, gastrointestinal system, sinuses, reproductive system, and the sweat glands.Type: GrantFiled: October 6, 2016Date of Patent: May 29, 2018Assignee: NuBridge BioSciencesInventors: Lin Zhang, Yu Ge
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Patent number: 9938257Abstract: The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.Type: GrantFiled: September 7, 2016Date of Patent: April 10, 2018Assignees: CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.Inventors: Ning Xi, Minxiong Li, Xiaobo Li, Wuhong Chen, Tao Zhang, Haiyang Hu, Weilong Dai, Yanjun Wu
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Patent number: 9908875Abstract: The present application relates to compounds having the inhibitory activity to apoptosis signal-regulating kinase (ASK1), thus are thus useful in treating ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.Type: GrantFiled: December 15, 2014Date of Patent: March 6, 2018Assignee: GILEAD SCIENCES, INC.Inventor: Gregory Notte
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Patent number: 9895308Abstract: Provided are certain pharmaceutical formulations of omecamtiv mecarbil and methods for their preparation and use.Type: GrantFiled: March 14, 2014Date of Patent: February 20, 2018Assignee: AMGEN INC.Inventor: William Brett Caldwell
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Patent number: 9896445Abstract: The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R1 to R8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.Type: GrantFiled: June 15, 2016Date of Patent: February 20, 2018Assignee: Ansana BioSciences, LLCInventors: Aranapakam M. Venkatesan, Scott K. Thompson, Roger A. Smith, Sanjeeva P. Reddy, Raghava Reddy Kethiri, Purushottam M. Dewang, Gurulingappa Hallur, Chandrika Mulakala, Ramesh Mullangi, Mohd Zainuddin
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Patent number: 9879001Abstract: Compounds of formula (I) wherein X1, X2, W, R1 to R5, L and m have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.Type: GrantFiled: March 10, 2014Date of Patent: January 30, 2018Assignee: Merck Patent GmbHInventors: Henry Yu, Lesley Liu-Bujalski, Theresa L. Johnson
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Patent number: 9868700Abstract: The present invention relates to carbamoyl hydrazine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the FPR receptor.Type: GrantFiled: March 13, 2017Date of Patent: January 16, 2018Assignee: Allergan, Inc.Inventors: Vidyasagar Vuligonda, Thong Vu, Veena Viswanath, John E. Donello, Richard L. Beard
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Patent number: 9868723Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: GrantFiled: July 29, 2016Date of Patent: January 16, 2018Assignee: Celgene CAR LLCInventors: Kwangho Lee, Deqiang Niu, Matthew Frank Baevsky
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Patent number: 9862688Abstract: The present invention provides Janus kinase inhibitors, such as compounds of Formula (I) and Formula (II) wherein RY1 and RY2 comprise a tagged hydrophobic moiety RH. The compounds may covalently or non-covalently bind a kinase (e.g., Janus kinase 3 (JAK3)). The hydrophobic moiety RH may signal to the intracellular protein homeostasis machinery to induce degradation of the targeted kinase. Also provided are pharmaceutical compositions, kits, methods, and uses that involve the compounds for reducing the activity of a kinase and/or treating and/or preventing a condition associated with aberrant activity of a kinase (e.g., a proliferative disease, inflammatory disorder, autoimmune disorder, painful condition, and/or viral infection).Type: GrantFiled: April 23, 2015Date of Patent: January 9, 2018Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Li Tan
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Patent number: 9809573Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.Type: GrantFiled: November 3, 2014Date of Patent: November 7, 2017Assignee: Bristol-Myers Squibb CompanyInventors: Guanglin Luo, Ling Chen, Gene M. Dubowchik, Swanee E. Jacutin-Porte, Prasanna Sivaprakasam, John E. Macor
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Patent number: 9771332Abstract: Myeloperoxidase inhibitor, pharmaceutical compositions containing the inhibitor and the use of the inhibitor to treat, for example, cardiovascular conditions.Type: GrantFiled: May 2, 2016Date of Patent: September 26, 2017Assignee: Pfizer Inc.Inventor: Roger Ruggeri
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Patent number: 9751863Abstract: Provided are compounds useful for treating cancer and methods of making the compounds and intermediates described herein.Type: GrantFiled: August 4, 2016Date of Patent: September 5, 2017Assignee: Agios Pharmaceuticals, Inc.Inventor: Shijie Zhang
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Patent number: 9738625Abstract: Provided are isocitrate dehydrogenase 2 (IDH2) inhibitor compounds useful for treating cancer and methods of treating cancer, comprising administering to a subject in need thereof a compound described herein. Also provided are polymorphic forms of the IDH2 inhibitor compounds characterized by X Ray powder diffraction patterns, having improved physicochemical properties that influence in vivo dissolution rate for formulation purposes.Type: GrantFiled: August 1, 2014Date of Patent: August 22, 2017Assignee: Agios Pharmaceuticals, Inc.Inventors: Samuel V. Agresta, Chong-Hui Gu, David Schenkein, Hua Yang, Liting Guo, Zhen Tang, Jianming Wang, Yanfeng Zhang, Yan Zhou
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Patent number: 9732087Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: GrantFiled: August 14, 2014Date of Patent: August 15, 2017Assignee: JANSSEN PHARMACEUTICA N.V.Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xiaohu Zhang
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Patent number: 9701659Abstract: Insecticidally active amide derivatives with sulfur-substituted phenyl- and pyridine groups of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.Type: GrantFiled: May 18, 2015Date of Patent: July 11, 2017Assignee: Syngenta Participations AGInventors: Andrew Edmunds, Roger Graham Hall, Michel Muehlebach, Daniel Emery, Pierre Joseph Marcel Jung, Andre Stoller
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Patent number: 9695169Abstract: Provided herein are intermediates and processes useful for facile synthesis of biologically active molecules.Type: GrantFiled: August 28, 2015Date of Patent: July 4, 2017Assignee: Plexxikon Inc.Inventor: Prabha N. Ibrahim
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Patent number: 9688930Abstract: A method for marking a petroleum hydrocarbon or a liquid biologically derived fuel by adding to the petroleum hydrocarbon or liquid biologically derived fuel at least one compound having formula Ar(R2)m(OR1)n, wherein Ar is an aromatic ring system having from six to twenty carbon atoms, R1 is C1-C12 alkyl or C2-C12 alkenyl, R2 is C1-C12 alkyl or C3-C12 alkenyl, m is an integer from zero to five and n is an integer from one to three; wherein each compound of formula Ar(R2)m(OR1)n is present at a level from 0.01 ppm to 100 ppm.Type: GrantFiled: November 5, 2013Date of Patent: June 27, 2017Assignee: Dow Global Technologies LLCInventors: George David Green, Raymond J. Swedo, Ronda L. Gras, Jim C. Luong
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Patent number: 9687485Abstract: The invention relates to methods of treating cancer, myeloproliferative diseases, or immunological or neurological diseases with a combination of a glutaminase inhibitor and an anticancer agent such as an enzyme inhibitor (such as a kinase inhibitor), a mitotic inhibitor, a DNA-modifying agent, or a cytidine analog. The invention further relates to methods of treating cancer, myeloproliferative diseases, or immunological or neurological diseases that are resistant to one or more anticancer agents.Type: GrantFiled: June 12, 2015Date of Patent: June 27, 2017Assignee: Calithera Biosciences, Inc.Inventors: Susanne M. Steggerda, Andrew L. MacKinnon, Mirna L. Rodriguez, Dong Zhang, Francesco Parlati
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Patent number: 9663504Abstract: The present disclosure relates to salts of heterocyclic compounds and methods that inhibit HIF pathway activity. The compounds are designed to treat or prevent cancer and other hypoxia-mediated diseases.Type: GrantFiled: February 25, 2015Date of Patent: May 30, 2017Assignee: Board of Regents, The University of Texas SystemInventors: Philip Jones, Maria Emilia Di Francesco, Timothy McAfoos
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Patent number: 9663457Abstract: The present invention relates to carbamoyl hydrazine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the FPR receptor.Type: GrantFiled: April 6, 2015Date of Patent: May 30, 2017Assignee: Allergan, Inc.Inventors: Richard L. Beard, Vidyasagar Vuligonda, Thong Vu, Veena Viswanath, John E. Donello
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Patent number: 9663454Abstract: The present invention relates to a process for labeling compounds comprising thiol moieties with 3-arylpropiolonitrile compounds, to 3-arylpropiolonitrile compounds substituted with tag moieties and to specific 3-arylpropiolonitrile linkers.Type: GrantFiled: July 4, 2014Date of Patent: May 30, 2017Assignees: Universite De Strasbourg, Centre National De La Recherche ScientifiqueInventors: Alain Wagner, Oleksandr Koniev
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Patent number: 9624199Abstract: The invention relates to novel substituted bipiperidinyl derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of diabetic microangiopathies, diabetic ulcers on the extremities, in particular for promoting wound healing of diabetic foot ulcers, diabetic heart failure, diabetic coronary microvascular heart disorders, peripheral and cardial vascular disorders, thromboembolic disorders and ischaemias, peripheral circulatory disturbances, Raynaud's phenomenon, CREST syndrome, microcirculatory disturbances, intermittent claudication, and peripheral and autonomous neuropathies.Type: GrantFiled: December 16, 2014Date of Patent: April 18, 2017Assignee: Bayer Pharma AktiengesellschaftInventors: Eva Maria Becker-Pelster, Philipp Buchgraber, Anja Buchmüller, Karen Engel, Andreas Göller, Herbert Himmel, Raimund Kast, Joerg Keldenich, Carsten Schmeck, Hanna Tinel, Frank Wunder
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Patent number: 9604946Abstract: The present invention relates to compounds and methods for the treatment of bacterial infections. The compounds and methods involve the disruption of the QseC signaling pathway which modulates the virulence of some bacteria. This methodology for treatment of bacterial infections reduces evolutionary pressure to develop resistance because the bacteria are not killed in the process.Type: GrantFiled: March 10, 2014Date of Patent: March 28, 2017Assignee: The Board of Regents of the University of Texas SystemInventors: Vanessa Sperandio, John R. Falck
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Patent number: 9604967Abstract: The invention provides certain azetidinyloxyphenylpyrrolidine compounds, particularly compounds of formula I wherein R is hydrogen or methyl, and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat overactive bladder.Type: GrantFiled: January 15, 2016Date of Patent: March 28, 2017Assignee: Eli Lilly and CompanyInventors: Danwen Huang, Joshua O. Odingo