Three Or More Ring Hetero Atoms In The Additional Hetero Ring Patents (Class 514/236.2)
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Patent number: 11926646Abstract: Compounds are provided according to Formula (A): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1A, R1B, n, R2A, R2B, R3, and R4 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.Type: GrantFiled: September 15, 2021Date of Patent: March 12, 2024Assignee: Sage Therapeutics, Inc.Inventors: Francesco G. Salituro, Albert Jean Robichaud, Gabriel Martinez Botella, Andrew Griffin, Boyd L. Harrison, Daniel La
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Patent number: 11597721Abstract: Compounds having the following formula (I) or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFN?, by acting on Tyk-2 to cause signal transduction inhibition.Type: GrantFiled: March 20, 2019Date of Patent: March 7, 2023Assignee: Bristol-Myers Squibb CompanyInventors: Zili Xiao, Michael G. Yang, Chunjian C. Liu, Trevor C. Sherwood, John L. Gilmore, David S. Weinstein
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Patent number: 11541018Abstract: An adhesive matrix and adhesive formulation are described. The adhesive matrix is comprised of a hydrophilic domain and a hydrophobic domain, and a therapeutically active agent contained in the matrix in a supersaturated, stable, condition. The hydrophilic domain and the hydrophobic domain are co-soluble in a solvent system, to provide a homogeneous blend in which the active agent is solubilized. The proportion of the hydrophilic domain and hydrophobic domain is selected to optimize, or maximize, solubility of active agent in the matrix.Type: GrantFiled: June 23, 2017Date of Patent: January 3, 2023Assignee: Corium, LLCInventors: Eun Soo Lee, Amit K. Jain, Parminder Singh
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Patent number: 11517574Abstract: The present invention relates to injectable, thermosensitive hydrogel compositions comprising linezolid for relieving and/or treating chronic low back pain (CLBP).Type: GrantFiled: November 16, 2018Date of Patent: December 6, 2022Assignee: Persica Pharmaceuticals Ltd.Inventors: Lloyd Czaplewski, Sarah Guest
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Patent number: 11491145Abstract: 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: GrantFiled: June 19, 2018Date of Patent: November 8, 2022Assignee: MADRIGAL PHARMACEUTICALS, INC.Inventors: Weiwen Ying, Dinesh U. Chimmanamada, David Proia
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Patent number: 11214538Abstract: Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.Type: GrantFiled: May 12, 2020Date of Patent: January 4, 2022Assignee: METACRINE, INC.Inventors: Nicholas D. Smith, Steven P. Govek, Johnny Y. Nagasawa
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Patent number: 10988458Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, ester, stereoisomer, tautomer, solvate, hydrate, or combination thereof: which inhibit the Apoptosis signal-regulating kinase 1 (ASK-1), which associated with autoimmune disorders, neurodegenerative disorders, inflammatory diseases, chronic kidney disease, cardiovascular disease. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from ASK-1 related disease. The invention also relates to methods of treating an ASK-1 related disease in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention specifically relates to methods of treating ASK-1 associated with hepatic steatosis, including non-alcoholic fatty liver disease (NAFLD) and non-alcohol steatohepatitis disease (NASH).Type: GrantFiled: May 5, 2020Date of Patent: April 27, 2021Assignee: Enanta Pharmaceuticals, Inc.Inventors: Guoqiang Wang, Ruichao Shen, Jiang Long, Jun Ma, Xuechao Xing, Yong He, Brett Granger, Jing He, Bin Wang, Yat Sun Or
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Patent number: 10836760Abstract: The invention provides compositions and methods for the treatment of presbyopia. The methods preferably comprise storing an aceclidine composition in a container having a headspace at a temperature from about 2 to about 8 degrees Celsius. The methods further comprise filling the container under an inert gas overlay and/or enclosing the container an anti-leaching material or disposing the container in a second container containing an anti-leaching material.Type: GrantFiled: October 8, 2019Date of Patent: November 17, 2020Assignee: Presbyopia Therapies LLCInventor: Gerald Horn
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Patent number: 10703712Abstract: Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.Type: GrantFiled: September 16, 2016Date of Patent: July 7, 2020Assignee: METACRINE, INC.Inventors: Nicholas D. Smith, Steven P. Govek, Johnny Y. Nagasawa
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Patent number: 10683279Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, ester, stereoisomer, tautomer, solvate, hydrate, or combination thereof: which inhibit the Apoptosis signal-regulating kinase 1 (ASK-1), which associated with autoimmune disorders, neurodegenerative disorders, inflammatory diseases, chronic kidney disease, cardiovascular disease. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from ASK-1 related disease. The invention also relates to methods of treating an ASK-1 related disease in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention specifically relates to methods of treating ASK-1 associated with hepatic steatosis, including non-alcoholic fatty liver disease (NAFLD) and non-alcohol steatohepatitis disease (NASH).Type: GrantFiled: May 14, 2018Date of Patent: June 16, 2020Assignee: Enanta Pharmaceuticals, Inc.Inventors: Guoqiang Wang, Ruichao Shen, Jiang Long, Jun Ma, Xuechao Xing, Yong He, Brett Granger, Jing He, Bin Wang, Yat Sun Or
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Patent number: 10611732Abstract: This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N?N—, —O—, —C(?O)—, C1-4alkanediyl,Type: GrantFiled: July 2, 2019Date of Patent: April 7, 2020Assignee: Janssen Pharmaceutica NVInventors: Jérôme Emile Georges Guillemont, Patrice Palandjian, Marc René de Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desiré Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Paul Adriaan Jan Janssen
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Patent number: 10463670Abstract: Use of the non-peptide NK1 receptor antagonist, preferably Aprepitant, for the treatment of cancer in predetermined doses. The present invention also describes pharmaceutical compositions comprising said agents, alone or in combination with at least one other active principle, for the treatment of cancer.Type: GrantFiled: June 27, 2017Date of Patent: November 5, 2019Assignee: SERVICIO ANDALUZ DE SALUDInventor: Manuel Vicente Salinas Martín
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Patent number: 10336702Abstract: The invention is directed to compounds of general formula (I), and pharmaceutical compositions containing such compounds. The compounds and compositions have valuable pharmaceutical properties. In particular, they may be used for the treatment of cancer. Novel intermediates and novel methods of preparation are also disclosed.Type: GrantFiled: December 23, 2015Date of Patent: July 2, 2019Assignee: BerGenBio ASAInventors: Jason John Shiers, John Paul Watts, Stuart Thomas Onions, Mohammed Abdul Quddus, Joseph William Wrigglesworth, Colin Peter Sambrook-Smith, Alan Naylor, Derek Londesbrough
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Patent number: 10317417Abstract: Described herein are, inter alia, methods for diagnosing and treating arrhythmogenic cardiomyopathy (ACM) by detecting cardiac intercalated disk proteins, e.g., desmosomal proteins, mechanical and gap junction proteins, in buccal cells. Exemplary desmosomal and gap junction proteins that can be evaluated in the methods described herein include plakoglobin, plakophilin 1, desmoplakin, and Cx43. The methods can also include selecting and/or administering a treatment for ACM to the subject.Type: GrantFiled: May 14, 2018Date of Patent: June 11, 2019Assignee: Beth Israel Deaconess Medical Center, Inc.Inventors: Jeffrey E. Saffitz, Angeliki Asimaki
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Patent number: 10251872Abstract: There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of kallikrein, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of kallikrein.Type: GrantFiled: November 13, 2017Date of Patent: April 9, 2019Assignee: VERSEON CORPORATIONInventors: Kevin Michael Short, Son Minh Pham, David Charles Williams, David Ben Kita
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Patent number: 10227527Abstract: There are disclosed nanoemulsion optical materials, methods of making nanoemulsion optical materials and optical articles comprising nanoemulsion optical materials. A nanoemulsion optical material includes a polymer matrix and a plurality of nano-droplets, comprising an optically interactive material, directly dispersed within the polymer matrix.Type: GrantFiled: December 14, 2015Date of Patent: March 12, 2019Assignees: INDIZEN OPTICAL TECHNOLOGIES OF AMERICA, LLC, FUTURECHROMES S.L., CONSEJO SUPERIOR DE INVESTIGACIONES CIENTIFICAS (CSIC), INSTITUT CATALA DE NANOCIENCIA I NANOTECHNOLOGIA (ICN2)Inventors: Claudio Roscini, Héctor Torres-Pierna, Daniel Ruiz-Molina
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Patent number: 10159747Abstract: The disclosure describes prodrugs and derivatives of prostaglandins, carbonic anhydrase inhibitors, kinase inhibitors, beta-adrenergic receptor antagonists and other drugs, as well as controlled delivery formulations containing such prodrugs and derivatives, for the treatment of ocular disorders.Type: GrantFiled: December 14, 2017Date of Patent: December 25, 2018Assignee: Graybug Visioon, Inc.Inventors: Jeffrey L. Cleland, Ming Yang, John G. Bauman, Nu Hoang, Emmett Cunningham
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Patent number: 9995756Abstract: Described herein are, inter alia, methods for diagnosing and treating arrhythmogenic cardiomyopathy (ACM) by detecting cardiac intercalated disk proteins, e.g., desmosomal proteins, mechanical and gap junction proteins, in buccal cells. Exemplary desmosomal and gap junction proteins that can be evaluated in the methods described herein include plakoglobin, plakophilin 1, desmoplakin, and Cx43. The methods can also include selecting and/or administering a treatment for ACM to the subject.Type: GrantFiled: September 27, 2016Date of Patent: June 12, 2018Assignee: Beth Israel Deaconess Medical Center, Inc.Inventors: Jeffrey E. Saffitz, Angeliki Asimaki
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Patent number: 9914736Abstract: The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (Formula (I)) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.Type: GrantFiled: March 23, 2015Date of Patent: March 13, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Helen Mitchell, Mark E. Fraley, Andrew J. Cooke, Craig A. Stump, Xu-Fang Zhang, Casey C. McComas, Kathy Schirripa, Melody McWherter, Ping Liu, Dann Parker, Chun Sing Li, Qinghua Mao
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Patent number: 9718790Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having an analgesic effect or an improving effect of urination disorder comprising a compound of the formula (I): wherein Rh and Ri are taken together to form a bond; Ra and Rb and/or Rd and Re are taken together to form oxo or the like; Rc is hydrogen, substituted or unsubstituted alkyl or the like; Rf is —(CR4aR4b)n—R2; R4a and R4b are hydrogen, substituted or unsubstituted alkyl or the like; R2 is substituted or unsubstjtuted cycloalkyl or the like; n is an integer of 1 to 4; —Rg is —X—R3; —X— is —O—, —S— or the like; R3 is substituted or unsubstituted cycloalkyl or the like, or its pharmaceutically acceptable salt or a solvate thereof.Type: GrantFiled: August 9, 2011Date of Patent: August 1, 2017Assignee: SHIONOGI & CO., LTD.Inventors: Hiroyuki Kai, Tohru Horiguchi, Kentaro Asahi, Yasuhiko Fujii
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Patent number: 9706776Abstract: Compounds of the formula (I) and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, including all stereoisomers and tautomeric forms, and wherein the substituents are as defined in claim 1, are useful for controlling animal pests and can be prepared in a manner known per se.Type: GrantFiled: December 19, 2014Date of Patent: July 18, 2017Assignee: Syngenta Participations AGInventors: Michel Muehlebach, Andrew Edmunds, Andre Stoller, Natalie Anne Miller, Ottmar Franz Hueter
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Patent number: 9687479Abstract: There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of kallikrein, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of kallikrein.Type: GrantFiled: November 17, 2016Date of Patent: June 27, 2017Assignee: VERSEON CORPORATIONInventors: Kevin Michael Short, Son Minh Pham, David Charles Williams, David Ben Kita
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Patent number: 9642850Abstract: A method of effectively treating pain in humans is achieved by administering buprenorphine in accordance with first order kinetics over an initial three-day dosing interval, such that a maximum plasma concentration from about 20 pg/ml to about 1052 pg/ml is attained, and thereafter maintaining the administration of buprenorphine for at least an additional two-day dosing interval in accordance with substantially zero order kinetics, such that the patients experience analgesia throughout the at least two-day additional dosing interval.Type: GrantFiled: November 15, 2016Date of Patent: May 9, 2017Assignee: PURDUE PHARMA L.P.Inventors: Robert F. Reder, Paul D. Goldenheim, Robert F. Kaiko
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Patent number: 9635857Abstract: A tetrazolinone compound represented by formula (1): wherein R1 and R2 each represents a hydrogen atom, a halogen atom, or a C1-C3 alkyl group; R3 represents a C1-C3 alkyl group optionally having one or more halogen atoms; R4, R5, and R6 each represents a hydrogen atom or a halogen atom; R7 represents a C1-C3 alkyl group; Q represents a divalent group selected from Group P4; and A represents a C7-C18 aralkyloxy group optionally having one or more atoms or groups selected from Group P3, has excellent control activity against pests.Type: GrantFiled: October 23, 2014Date of Patent: May 2, 2017Assignee: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Takayuki Shioda, Yuya Yoshimoto
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Patent number: 9540337Abstract: Compositions that are effective in inhibiting gamma-glutamyl transpeptidase are disclosed. Methods of producing and using these compositions are also disclosed.Type: GrantFiled: August 23, 2013Date of Patent: January 10, 2017Assignee: The Board of Regents of the University of OklahomaInventors: Marie H. Hanigan, Pui Kai Li
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Patent number: 9533970Abstract: There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of kallikrein, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of kallikrein.Type: GrantFiled: March 17, 2014Date of Patent: January 3, 2017Assignee: VERSEON CORPORATIONInventors: Kevin Michael Short, Son Minh Pham, David Charles Williams, David Ben Kita
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Patent number: 9403798Abstract: There is provided a novel triazinone compound that has an excellent T-type voltage-dependent calcium channel inhibitory activity and is specifically useful for treatment of pain. A compound of Formula (I), a tautomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof: where each substituent is defined in detail in the description or claims, for example R1 is H or C1-6 alkoxy, etc., each of L1 and L2 is independently a single bond or NR2, etc., L3 is C1-6 alkylene, etc., A is C6-14 aryl or 5 to 10-membered heteroaryl which is optionally substituted, etc., B is C3-11 cycloalkylene, etc., D is C6-14 aryl or 5 to 10-membered heteroaryl which is optionally substituted, etc.Type: GrantFiled: March 29, 2013Date of Patent: August 2, 2016Assignee: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Noriko Saito, Jun Egi, Hiroshi Nagai, Megumi Ueno, Yusuke Shintani, Yusuke Inaba, Michiaki Adachi, Yuichi Hirai, Takeshi Kawazu, Koichi Yasutake, Daiki Takahashi
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Patent number: 9393218Abstract: The subject of this application is the use of film-forming polyurethanes that are used in hair care agents or mixtures of these polyurethanes with other polymers in pharmaceutical preparations for dermal or transdermal administration of active ingredients, as well as patches and pharmaceutical preparations that contain these hair care polyurethanes.Type: GrantFiled: December 22, 2006Date of Patent: July 19, 2016Assignee: EPINAMICS GMBHInventors: Ines Zurdo Schroeder, Patrick Franke, Stefan Bracht, Claus-Michael Lehr, Ulrich Schäfer
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Patent number: 9346798Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.Type: GrantFiled: February 12, 2013Date of Patent: May 24, 2016Assignee: AMGEN INC.Inventors: Christiane Boezio, Alessandro Boezio, Howard Bregman, Nagasree Chakka, James R. Coats, Katrina Woodin Copeland, Erin F. Dimauro, Thomas Dineen, Hua Gao, Daniel La, Isaac E. Marx, Hanh Nho Nguyen, Emily Anne Peterson, Matthew Weiss
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Patent number: 9328076Abstract: Disclosed herein is a compound having Formula I: or a salt thereof, in which R1, R2 and R3 are as defined herein. Also disclosed are processes to prepare compounds of Formula I and use of Formula I to prepare stable glassy phases.Type: GrantFiled: February 24, 2015Date of Patent: May 3, 2016Assignee: HER MAJESTY IN THE RIGHT OF CANADA AS REPRESENTED BY THE MINISTER OF DEFENSEInventor: Olivier Lebel
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Patent number: 9161938Abstract: Biocompatible intraocular implants include an alpha-2 adrenergic receptor agonist and a polymer associated with the alpha-2 adrenergic receptor agonist to facilitate release of the alpha-2 adrenergic receptor agonist into an eye for an extended period of time. The alpha-2 adrenergic receptor agonist may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants may be placed in an eye to treat one or more ocular conditions, such as an ocular vasculopathy or glaucoma, among others.Type: GrantFiled: January 31, 2008Date of Patent: October 20, 2015Assignee: Allergan, Inc.Inventors: Glenn T. Huang, Brittany Jackson, James A. Burke, Ton Lin, Patrick M. Hughes, Larry A. Wheeler, Rosy Sheng Donn
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Publication number: 20150148346Abstract: Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.Type: ApplicationFiled: January 28, 2015Publication date: May 28, 2015Applicant: PTC Therapeutics Inc.Inventors: Gary Mitchell Karp, Seongwoo Hwang, Guangming Chen, Neil Gregory Almstead, Young-Choon Moon
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Publication number: 20150133414Abstract: It was determined whether SNPs in SLC4A5 are associated with salt sensitivity of blood pressure (BP). Subjects consumed an isocaloric constant diet with a randomized order of 7 days low Na+ (10 mmol/d) and 7 days high Na+ (300 mmol/d) intake. Salt sensitivity was defined as a ?7 mm Hg increase in mean arterial pressure (MAP). 35 polymorphisms in 17 candidate genes were assayed. Association analyses with salt sensitivity revealed three variants that associated with salt sensitivity, two in SLC4A5 (rs7571842, rs10177833; P<0.001), and one in GRK4 (rs1801058; P=0.020). Paradoxical changes in blood pressure in response to changes in salt intake were also found associated with a SNP for DRD2 (rs6276). In conclusion, SLC4A5 variants are strongly associated with salt sensitivity of BP in Caucasian and a DRD2 SNP is a marker for paradoxical response to salt intake.Type: ApplicationFiled: April 22, 2013Publication date: May 14, 2015Applicant: University of Virginia Patent FoundationInventors: Robin A. Felder, Robert M. Carey, John E. Jones, Pedro A. Jose, Scott M. Williams
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Publication number: 20150133411Abstract: Compounds, compositions and methods useful for treating ocular diseases are provided. In particular, antagonists of TRPV4, their synthesis, pharmaceutical compositions thereof and methods of treating ocular diseases such as glaucoma, are disclosed. Compounds of the invention include N-(3-(trifluoromethyl)phenyl)-2-methyl-1-(3-morpholinopropyl)-5-phenyl-1 H-pyrrole-3-carboxamide, as well as other 2-phenyl-pyrrole carboxamide derivates and indole carboxamide derivatives.Type: ApplicationFiled: March 15, 2013Publication date: May 14, 2015Inventors: David Krizaj, Glenn D. Prestwich, Peter Barabas, Yong Xu, Daniel Ryskamp
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Publication number: 20150126510Abstract: The present invention relates to the field of HIV-1 infections, and in particular provides novel compounds containing triazine rings and suitable spacers. The compounds according to this invention are very suitable for the prevention and/or treatment of HIV-1 infection and in particular show improved activity against NNRTI-resistant viruses of HIV-1.Type: ApplicationFiled: March 18, 2013Publication date: May 7, 2015Applicants: Universiteit Antwerpen, Shakturana CVInventors: Jan Heeres, Koen Augustyns, Pieter Van Der Veken, Jurgen Joossens, Venkatraj Muthusamy, Kevin Karel Florentina Arien, Guido Louis Emile Vanham, Paulus Lewi (deceased)
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Publication number: 20150126499Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.Type: ApplicationFiled: January 7, 2015Publication date: May 7, 2015Inventors: Joseph Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
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Patent number: 9023846Abstract: The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.Type: GrantFiled: February 4, 2014Date of Patent: May 5, 2015Assignee: Janssen Pharmaceutica NVInventors: Mark R Player, Raul Calvo, Jinsheng Chen, Sanath Meegalla, Daniel J. Parks, William J Parsons, Scott Ballentine, Shawn Branum
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Publication number: 20150119395Abstract: The present invention relates to novel triazole Hsp90 inhibitors that possess significant inhibitory activity against Hsp90, which are suitable for the treatment of hyperproliferative diseases such as cancer, infections, immune disorders, inflammation, and CNS related disorders. Furthermore, pharmaceutical compositions, including combination products, are also provided in the present application. Further provided are methods of using the pharmaceutical compositions and/or combination products.Type: ApplicationFiled: April 4, 2013Publication date: April 30, 2015Inventors: Dinesh U. Chimmanamada, Weiwen Ying
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Patent number: 9018205Abstract: The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.Type: GrantFiled: February 13, 2013Date of Patent: April 28, 2015Assignee: The Scripps Research InstituteInventors: Theodore Mark Kamenecka, Rong Jiang, Xinyi Song, Philip LoGrasso, Michael Darin Cameron, Derek R. Duckett
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Publication number: 20150111893Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.Type: ApplicationFiled: May 9, 2013Publication date: April 23, 2015Inventors: Vincent P. Sandanayaka, Sharon Shechter, Sharon Shacham, Dilara McCauley, Erkan Baloglu
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Publication number: 20150111857Abstract: Compounds and compositions useful for treating disorders related to KIT and PDFGR are described herein.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Applicant: BLUEPRINT MEDICINES CORPORATIONInventors: Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Douglas Wilson, Yulian Zhang
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Publication number: 20150104491Abstract: The present invention provides a sustained release implant for intraocular use to treat elevated intraocular pressure, which implant is configured for intracameral or anterior vitreal administration to a patient with elevated intraocular pressure (IOP), said implant comprising a core of an antihypertensive agent surrounded by a polymer, which limits the rate of passage of the antihypertensive agent from the implant into the eye of said patient and said implant provides a linear rate of release of therapeutically effective amounts of said anti-hypertensive agent into the eye for a period of time of between 14 days and 365 days.Type: ApplicationFiled: September 10, 2014Publication date: April 16, 2015Inventors: Ruiwen Shi, Patrick M. Hughes, James A. Burke, Michael R. Robinson, Hui Liu
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Patent number: 9006228Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: June 11, 2012Date of Patent: April 14, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Michael Miller, Andrew Stamford, Kallol Basu, Harold B. Wood, Duane DeMong, Wanying Sun, Joie Garfunkle, Christopher Moyes, Zhiyong Hu, Ping Liu, Scott D. Edmondson, Xing Dai, Byron Gabriel DuBois
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Publication number: 20150099750Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: December 1, 2014Publication date: April 9, 2015Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger
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Publication number: 20150099004Abstract: A liquid pharmaceutical compositions comprising Aprepitant is preferably prepared as an oral suspension dosage form for the prevention and control of acute and delayed chemotherapy induced nausea and vomiting, and/or for prevention of postoperative nausea and vomiting.Type: ApplicationFiled: October 8, 2014Publication date: April 9, 2015Inventors: Udaya Toti, Shyamprasad Mukundan, Sasank Chaitanya Kunadharaju, Tushar Hingorani, Kumaresh Soppimath, Satish Pejaver, Navneet Puri
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Patent number: 9000153Abstract: The invention relates to compounds of the formulae (I) and (II) in which R1, R2, R3, R4, R5, R8, X and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I).Type: GrantFiled: July 26, 2011Date of Patent: April 7, 2015Assignee: Merck Patent GmbHInventors: Thomas Fuchss, Werner Mederski, Frank Zenke
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Publication number: 20150087647Abstract: Disclosed are pharmaceutical compositions comprising brimonidine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.Type: ApplicationFiled: April 28, 2014Publication date: March 26, 2015Applicant: Allergan Sales, LLCInventors: Chin-Ming Chang, Gary J. Beck, Cynthia C. Pratt, Amy L. Batoosingh
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Publication number: 20150087646Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.Type: ApplicationFiled: June 10, 2013Publication date: March 26, 2015Applicant: GLENMARK PHARMACEUTICALS S.A.Inventors: Laxmikant Atmaram Gharat, Nagarajan Muthukaman, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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Publication number: 20150086646Abstract: Embodiments of the invention relates to decreasing effects of local and/or regional anesthesia by administering to a patient in need thereof an agent selected from the group of agents consisting of reactive nitrogen species (RNS), reactive oxygen species (ROS) and/or an agent which induces formation of RNS and/or ROS. Exemplary agents which may be used include peroxynitrite and hydrogen peroxide.Type: ApplicationFiled: April 7, 2013Publication date: March 26, 2015Inventors: Sagi Polani, Asher Polani, Roee Atlas
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Patent number: 8987262Abstract: The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroïds, interferon or vincristine, generally used for the treatment of hemangiomas.Type: GrantFiled: November 16, 2012Date of Patent: March 24, 2015Assignees: Universite de Bordeaux, Centre Hospitalier Universitaire de BordeauxInventors: Christine Leaute-Labreze, Eric Dumas De La Roque, Alain Taieb, Jean-Benoit Thambo