Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/156)
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Patent number: 11939314Abstract: Compounds of the formula I in which X1, X2, X3, X4, R1, R2, R3, Q and Y have the meanings indicated in claim 1, are inhibitors of c-Kit kinase, and can be employed for the treatment of cancer.Type: GrantFiled: October 12, 2021Date of Patent: March 26, 2024Assignee: MERCK PATENT GMBHInventors: Dieter Dorsch, Mathilde Muzerelle, Lars Burgdorf, Margarita Wucherer-Plietker, Paul Czodrowski, Christina Esdar, Christos Tsaklakidis
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Patent number: 11932637Abstract: The present invention relates to monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof. The present invention also relates to compositions which comprise a monobactam compound of structural formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of structural formula I, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.Type: GrantFiled: November 16, 2022Date of Patent: March 19, 2024Assignee: Merck Sharp & Dohme LLCInventors: Helen Y. Chen, Shuzhi Dong, Zhiyong Hu, Jing Su, Tao Yu, Yong Zhang
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Patent number: 11787768Abstract: In one aspect, compounds and compositions that modulate a bromodomain and methods of making and using same are disclosed. The disclosed compounds and compositions can be useful for disorders associated with inhibition of a bromodomain such as, for example, cancer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: March 4, 2021Date of Patent: October 17, 2023Assignee: ST. JUDE CHILDREN'S RESEARCH HOSPITALInventors: R. Kip Guy, P Jake Slavish, William Robert Shadrick, Brandon M. Young, Vincent A. Boyd, Nagakumar Bharatham, Jeanine E. Price, Anang Shelat
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Patent number: 11746116Abstract: The invention relates to antibiotic compounds of formula (A1) and pharmaceutically acceptable salts, solvates, tautomers and combinations thereof, wherein X and L are optional linkers and one of RA or R1 comprises Ar1, wherein Ar1 is an antibiotic resistance breaker moiety which comprises an optionally substituted C6-10 aryl, C7-13 aralkyl, C5-10 heteroaryl, C6-13 heteroaralkyl, C5-10 heterocyclyl, C6-13 heterocyclalkyl, C3-10 carbocyclyl, C4-13 carbocyclalkyl, —C(?NR?)—NR?R? or —CH2—CH?CH2 group; wherein after administration of the compound to a bacterial infection this moiety reduces or prevents efflux. The invention also discloses pharmaceutical compositions comprising compounds of formula (A1) and the use of such compounds as medicaments, in particular, to treat bacterial infections, such as drug-resistant bacterial infections.Type: GrantFiled: May 30, 2018Date of Patent: September 5, 2023Assignees: King's College London, Secretary of State for Health and Social CareInventors: Khondaker Mirazur Rahman, Shirin Jamshidi, Mark Benjamin Laws, Kazi Nahar, John Mark Sutton, Charlotte Hind
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Patent number: 11708331Abstract: The disclosure provides processes for synthesizing compounds for use as CFTR modulators.Type: GrantFiled: November 30, 2018Date of Patent: July 25, 2023Assignee: Vertex Pharmaceuticals IncorporatedInventors: Berenice Lemercier Lewandowski, Robert Lewis, Adam Looker, Adam Morgan, Stefanie Roeper, Michael Ryan, Juan Gabriel Solsona Rocabert, Nathan Wilde
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Patent number: 11220498Abstract: Disclosed herein are methods and compositions comprising compounds capable of activating and increasing protein SUMOylation. Disclosed herein are methods and compositions comprising compounds capable of showing neuroprotective and cytoprotective effects when administered to injured cells. Also disclosed are methods comprising these compounds for treating neuronal or neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, fronto-temporal dementia, chronic traumatic encepholopathy, traumatic brain injury, or stroke.Type: GrantFiled: December 1, 2019Date of Patent: January 11, 2022Inventor: Russell Dahl
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Patent number: 11174241Abstract: Compounds of the formula I in which X1, X2, X3, X4, R1, R2, R3, Q and Y have the meanings indicated in Claim 1, are inhibitors of c-Kit kinase, and can be employed for the treatment of cancer.Type: GrantFiled: February 20, 2020Date of Patent: November 16, 2021Assignee: MERCK PATENT GMBHInventors: Dieter Dorsch, Mathilde Muzerelle, Lars Burgdorf, Margarita Wucherer-Plietker, Paul Czodrowski, Christina Esdar, Christos Tsaklakidis
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Patent number: 10662192Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: June 12, 2018Date of Patent: May 26, 2020Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Patent number: 10532984Abstract: A pyridonecarboxylic acid derivative or a salt thereof is represented by Formula (1), where R1 is hydrogen, a halogen atom, a lower alkyl group, or an amino group; R2 is —NH—R6, where R6 is hydrogen, a lower alkyl group, an amino lower alkyl group, or the like; —O—R7, where R7 is hydrogen, a lower alkyl group, or the like; —(CH2)m—R8, where R8 is an amino group or the like, m is 1, 2, 3 or 4; or a cyclic amino group of Formula (2), where Y represents NH or C—R9aR9b, where R9a and R9b are each independently hydrogen, a lower alkyl group, an amino group, a lower alkyl amino group, or the like; n and p are 1 or 2; R3 is hydrogen, a halogen atom, a lower alkyl group, or the like; R4 is hydrogen or a carboxyl group-protecting group; and R5 is hydrogen or a hydroxyl group-protecting group.Type: GrantFiled: June 14, 2017Date of Patent: January 14, 2020Assignee: WAKUNAGA PHARMACEUTICAL CO., LTD.Inventors: Tomohiko Kinoshita, Yasuhiro Kuramoto, Satoshi Inoue, Kouji Nishimura, Tatsuya Hirano, Mai Arai, Asuka Sakurai, Daichi Kazamori, Ayuka Sasaki
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Patent number: 10517865Abstract: Disclosed herein are compounds of Formula I wherein R1, R2, X, and Y are defined herein. These compounds are type II topoisomerase inhibitors and can be used in methods for treating infections caused by gram-positive pathogens, gram-negative pathogens, and drug-resistant strains thereof.Type: GrantFiled: April 13, 2018Date of Patent: December 31, 2019Assignee: Emergent Product Development Gaithersburg Inc.Inventors: Patrick Roussel, Jutta Heim, Peter Schneider, Christian Bartels, Yaoquan Liu, Glenn Dale, Daniel Milligan
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Patent number: 10329276Abstract: A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.Type: GrantFiled: December 18, 2017Date of Patent: June 25, 2019Assignee: ABBVIE INC.Inventors: Geoff G. Z. Zhang, Michael F. Bradley, David M. Barnes, Rodger Henry
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Patent number: 10167278Abstract: The present invention relates to new cyclopropanecarboxamide modulators of cystic fibrosis transmembrane conductance regulator proteins, pharmaceutical compositions thereof, and methods of use thereof.Type: GrantFiled: December 27, 2015Date of Patent: January 1, 2019Assignee: Auspex Pharmaceuticals, Inc.Inventors: Chengzhi Zhang, Justin Chakma
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Patent number: 9956213Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, Y, and n have any of the values described herein and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting MAO, and MAO-B selectively, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders (including obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.Type: GrantFiled: May 23, 2017Date of Patent: May 1, 2018Assignee: Dart NeuroScience (Cayman) Ltd.Inventors: Jillian Basinger, Graeme Freestone, Varsha Gupta, Alan Kaplan, Chi Ching Mak, Benjamin Pratt, Vincent Santora, Dipanjan Sengupta, Lino Valdez
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Patent number: 9949970Abstract: Disclosed are compounds of general formula A useful as potential anti-tubercular agents.Type: GrantFiled: March 1, 2016Date of Patent: April 24, 2018Assignee: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Ahmed Kamal, Rajesh Vcrnc Shetti, Ponnampalli Swapna, Shaik Azeeza, A. Malla Reddy, Inshad Ali Khan, Sheikh Tasduq Abdullah, Sandeep Sharma, Nitin Pal Kalia
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Patent number: 9931334Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.Type: GrantFiled: May 2, 2017Date of Patent: April 3, 2018Assignee: Vertex Pharmaceuticals IncorporatedInventors: Patricia Hurter, William Rowe, Christopher R. Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawiec, Yuchuan Gong, Yushi Feng, Martin Trudeau
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Patent number: 9873681Abstract: A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.Type: GrantFiled: November 23, 2016Date of Patent: January 23, 2018Assignee: ABBVIE INC.Inventors: Geoff G. Z. Zhang, Michael F. Bradley, David M. Barnes, Rodger Henry
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Patent number: 9809551Abstract: Provided herein is a polymorphic form of Ivacaftor, namely APO-I, as well as processes for the preparation and pharmaceutical compositions of the same. Also, provided is a new solvate of Ivacaftor, processes for its preparation and use in the preparation of pure Ivacaftor.Type: GrantFiled: November 13, 2014Date of Patent: November 7, 2017Assignee: Apotex Inc.Inventors: Padiyath Mohammed Akbarali, Kintali Venkata Ramana, Heggadde Nanjunda Bhatta Shreenivasa Murthy, Sankaran Suresh Kumar, Ekkaluru Vijaya Bhaskar, Nechipadappu Sunil Kumar, Karad Manjunath
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Patent number: 9776969Abstract: Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, {[(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibittors or for treating conditions wherein prolyl hydroxylase inhibition is desired.Type: GrantFiled: August 24, 2015Date of Patent: October 3, 2017Assignee: Akebia Therapeutics, Inc.Inventors: Christopher M. Lanthier, Boris Gorin, Jan Oudenes, Craig Edward Dixon, Alan Quigbo Lu, James Densmore Copp, John Michael Janusz
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Patent number: 9676722Abstract: The present invention relates to an improved process for the preparation of Ivacaftor intermediates. The present invention is also provides industrial applicable, commercially and eco-friendly viable process for the preparation of Ivacaftor.Type: GrantFiled: August 24, 2016Date of Patent: June 13, 2017Assignee: Optimus Drugs Private LimitedInventors: Srinivas Reddy Desi Reddy, Dnyandev Ragho Rane, Venkata Srinivasa Rao Velivela
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Patent number: 9670163Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.Type: GrantFiled: September 14, 2015Date of Patent: June 6, 2017Assignee: Vertex Pharmaceuticals IncorporatedInventors: Patricia Hurter, William Rowe, Christopher R. Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawiec, Yuchuan Gong, Yushi Feng, Martin Trudeau
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Patent number: 9539250Abstract: A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.Type: GrantFiled: February 3, 2015Date of Patent: January 10, 2017Assignee: ABBVIE INC.Inventors: Geoff G. Z. Zhang, Michael F. Bradley, David M. Barnes, Rodger Henry
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Patent number: 9422432Abstract: The present document describes a composition which comprises about 25% to about 40% (v/v) plasticizers such as 2-ethylhexyl benzoate and butyl benzyl phthalate, about 0.5% to about 2% (v/v) of monoethanolamine as degasser, about 5% to about 20% (w/w) of pH adjusting agents such as calcium carbonate and ammonium carbonate, and from about 30% to about 45% (v/v) of a phenol formaldehyde resin based adhesive comprising an epoxy consisting of epichlorohydrin. The document also describes processes of making the composition as well as methods of using the composition for the pretreatment of surfaces, for example wood surface, metal rock or plastic surfaces prior to further treatment.Type: GrantFiled: November 26, 2013Date of Patent: August 23, 2016Assignee: BRYSON PATENTS INC.Inventor: Bryan Christopher Farnum
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Patent number: 9371287Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.Type: GrantFiled: May 23, 2014Date of Patent: June 21, 2016Assignee: Vertex Pharmaceuticals IncorporatedInventors: John DeMattei, Adam R. Looker, Bobbianna Neubert-Langille, Martin Trudeau, Stefanie Roeper, Michael P. Ryan, Dahrika Milfred Yap Guerette, Brian R. Krueger, Peter D. J. Grootenhuis, Fredrick F. Van Goor, Martyn C. Botfield, Gregor Zlokarnik
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Patent number: 9273039Abstract: The present disclosure provides compounds of general formula A: useful as potential anti-tubercular agents.Type: GrantFiled: September 14, 2011Date of Patent: March 1, 2016Assignee: Council of Scientific and Industrial ResearchInventors: Ahmed Kamal, Rajesh Vcrnc Shetti, Ponnampalli Swapna, Shaik Azeeza, A Malla Reddy, Inshad Ali Khan, Sheikh Tasduq Abdullah, Sandeep Sharma, Nitin Pal Kalia
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Patent number: 9233927Abstract: The subject invention provides a mixture of crystalline laquinimod sodium particles, wherein (i) 90% or more of the total amount by volume of the laquinimod sodium particles have a size of 40 microns or less or (ii) 50% or more of the total amount by volume of the laquinimod sodium particles have a size of 15 microns or less, and wherein: a) the mixture has a bulk density of 0.2 g/mL to 0.4 g/mL; b) the mixture has a tapped density of 0.40 g/mL to 0.7 g/mL; c) an amount of heavy metal in the mixture is no more than 0.002% of heavy metal relative to the amount by weight of laquinimod sodium; d) an amount of 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline (MCQ) in the mixture is no more than 0.15% relative to the amount of laquinimod sodium as measured by HPLC; e) an amount of 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroqunoline-3-carboxylic acid (MCQCA) in the mixture is no more than 0.Type: GrantFiled: March 14, 2014Date of Patent: January 12, 2016Assignee: TEVA PHARMACEUTICAL INDUSTRIES, LTD.Inventors: Anton Frenkel, Avital Laxer
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Patent number: 9181192Abstract: This invention relates to compounds of Formula I: and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CFTR potentiator.Type: GrantFiled: September 19, 2014Date of Patent: November 10, 2015Assignee: Concert Pharmaceuticals, Inc.Inventor: Adam J. Morgan
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Publication number: 20150148344Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula I wherein R1, R2, R3, R4, R7, W, X, and Z are as described herein.Type: ApplicationFiled: November 21, 2014Publication date: May 28, 2015Inventors: Kerim Babaoglu, Britton K. Corkey, Robert H. Jiang, David Sperandio, Hai Yang
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Publication number: 20150126487Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, and useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, a sleep disorder and the like. The present invention relates to a compound represented by the formula (I): wherein R1 is an optionally substituted amino group or an optionally substituted cyclic amino group, R2 and R3 are each independently a hydrogen atom or a substituent, X is —CH? or —N?, and ring A is an optionally substituted 5- to 10-membered ring, or a salt thereof.Type: ApplicationFiled: February 28, 2013Publication date: May 7, 2015Inventors: Hiroki Sakamoto, Takahiro Sugimoto
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Publication number: 20150111886Abstract: The invention relates to a compound of formula (I) wherein A1, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: December 22, 2014Publication date: April 23, 2015Applicant: Hoffmann-La Roche Inc.Inventors: Atsushi Kimbara, Uwe Grether, Matthias Nettekoven, Bernd Puellmann, Mark Rogers-Evans, Tanja Schulz-Gasch
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Publication number: 20150099780Abstract: This invention relates to compounds of Formula I: and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CFTR potentiator.Type: ApplicationFiled: September 19, 2014Publication date: April 9, 2015Inventor: Adam J. Morgan
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Patent number: 8993767Abstract: The present invention relates to multiphoton activable organic compounds responding to the following formula (I). The present invention also relates to a method of synthesizing the compounds of the invention, to an aqueous solution comprising at least one compound of the invention, and to their specific uses. The present invention also concerns a method of liberating organic ligands, said method involving the step of irradiating a compound according to the invention.Type: GrantFiled: January 12, 2011Date of Patent: March 31, 2015Assignee: Centre National de la Recherche ScientifiqueInventors: Peter Dalko, Morgane Petit, David Ogden, Francine Acher
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Publication number: 20150087886Abstract: This invention relates to novel cancer treatment compositions and associated therapeutic methods. More particularly, this invention relates in part to small chemical bifunctional inhibitors of DNA replication and repair proteins Metnase and/or Intnase (also termed Gypsy Integrase, Gypsy Integrease-1, Gypsy Retransposon Integrase 1, or GIN-1) that simultaneously damage DNA, and to a therapeutic method that utilizes the inhibitors to increase the effectiveness of cancer treatment protocols, including radiation therapy. In preferred embodiments, compounds, compositions and methods of treatment of the invention are used to treat a patient suffering from leukemia (e.g. acute myeloid leukemia (AML) and related cancers.Type: ApplicationFiled: October 9, 2014Publication date: March 26, 2015Inventors: Robert Hromas, Andrei Leitao, Tudor I. Oprea, Larry A. Sklar, Elizabeth A. Williamson, Justin Wray, Wei Wang
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Publication number: 20150080377Abstract: The present invention relates to deuterium-enriched pyridinonecarboxamides and their derivatives of the formula 1, and pharmaceutically acceptable salts thereof, are partial or full agonists of serotonin (5-Hydroxytryptamine or 5-HT) receptor subtype 4 (5-HT4), and are useful compounds for the prevention and treatment of Alzheimer's disease, cognitive and memory dysfunction, mild cognition impairment, memory decline, cognitive impairment associated with schizophrenia, cognitive impairment associated with age-related dementia or Alzheimer's disease, cognitive impairment associated with post-coronary bypass surgery, attention deficit hyperactivity disorder, Obsessive compulsive disorder, depression, speech improvement in autistic children, sleep apnea in Alzheimer's patients, Age-related macular degeneration (AMD), irritable bowel syndrome, gastroesophageal reflux disease, Crohn's disease, emesis, nausea, vomiting, prokinesia, non-ulcer dyspepcia, anxiety, depression, pain, migraine, urinary incontinence, aType: ApplicationFiled: August 31, 2013Publication date: March 19, 2015Inventor: Daljit Singh Dhanoa
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Patent number: 8981103Abstract: Provision of a stabilized crystal of 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound A). A crystal of compound A, which shows a particular X-ray powder diffraction pattern of a characteristic diffraction peaks at diffraction angles 2?(°) as measured by X-ray powder diffractometry.Type: GrantFiled: August 10, 2009Date of Patent: March 17, 2015Assignee: Japan Tobacco Inc.Inventors: Koji Ando, Koji Matsuda, Shuji Miyake, Hideto Uehara
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Publication number: 20150073015Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.Type: ApplicationFiled: May 23, 2014Publication date: March 12, 2015Inventors: John DeMattei, Adam R. Looker, Bobbianna Neubert-Langille, Martin Trudeau, Stefanie Roeper, Michael P. Ryan, Dahrika Milfred Yap Guerette, Brian R. Krueger, Peter D.J. Grootenhuis, Fredrick F. Van Goor, Martyn C. Botfield, Gregor Zlokarnik
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Publication number: 20150065487Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: November 11, 2014Publication date: March 5, 2015Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fred Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Patent number: 8969569Abstract: A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.Type: GrantFiled: February 7, 2014Date of Patent: March 3, 2015Assignee: AbbVie Inc.Inventors: Geoff G. Z. Zhang, Michael F. Bradley, David M. Barnes, Rodger Henry
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Patent number: 8946430Abstract: The present invention provides compounds of Formula (I): 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: GrantFiled: September 24, 2012Date of Patent: February 3, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
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Publication number: 20150031722Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: October 6, 2014Publication date: January 29, 2015Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Patent number: 8927723Abstract: A process for making 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid, and therapeutically acceptable salts thereof, and intermediates used in the process are disclosed.Type: GrantFiled: February 10, 2014Date of Patent: January 6, 2015Assignee: AbbVie, Inc.Inventors: Anthony Haight, David M. Barnes, Geoff G. Z. Zhang
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Publication number: 20150005287Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.Type: ApplicationFiled: February 28, 2014Publication date: January 1, 2015Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
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Publication number: 20140357650Abstract: The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.Type: ApplicationFiled: January 17, 2013Publication date: December 4, 2014Applicant: Fox Chase Cancer CenterInventors: Koen Jansen, Ingrid De Meester, Leen Heirbaut, Jonathan D. Cheng, Jurgen Joossens, Koen Augustyns, Pieter Van Der Veken
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Patent number: 8884018Abstract: The present invention relates to processes for preparing solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, including Compound 1 Form A, Compound 1 Form A-HCl, Compound 1 Form B, and Compound 1 Form B-HCl, any combination of these forms, pharmaceutical compositions thereof, and methods of treatment therewith.Type: GrantFiled: March 7, 2014Date of Patent: November 11, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Narendra Bhalchandra Ambhaikar, Robert Hughes, Dennis James Hurley, Elaine Chungmin Lee, Benjamin Littler, Mehdi Numa, Stefanie Roeper, Urvi Sheth
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Publication number: 20140329855Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.Type: ApplicationFiled: July 18, 2014Publication date: November 6, 2014Inventors: Sneha G. Arekar, Steven C. Johnston, Mariusz Krawiec, Ales Medek, Praveen Mudunuri, Mark Jeffrey Sullivan
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Patent number: 8877931Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.Type: GrantFiled: August 1, 2013Date of Patent: November 4, 2014Assignee: Gilead Sciences, Inc.Inventors: Dominika Pcion, Carrie Tomasi, Mark Charles Whitcomb, Eric D. Dowdy, Wenyi Fu, Patricia MacLeod
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Patent number: 8877752Abstract: Provided are 4(1H)-quinolone derivatives effective in inhibiting or eliminating the viability of at least one of the stages in the life-cycle of the malarial parasite, and to show a reduced propensity to induce resistance to the compound by the target parasite. In particular, the compounds can be derivatives of phenoxyethoxy-quinolones, and including, but not only, 7-(2-phenoxyethoxy)quinolin derivatives. These compounds may be administered by themselves, with at least one other derivative compound, or with other antimalarial compounds, to an animal or human subject. The therapeutic compositions can be and formulated to reduce the extent of a Plasmodium infection in the recipient subject, or to reduce the likelihood of the onset or establishment of a Plasmodium infection if administered prior to the parasite contacting the subject. The therapeutic compositions can be formulated to provide an effective single dose amount of an antimalarial compound or multiple doses for administering over a period of time.Type: GrantFiled: October 26, 2012Date of Patent: November 4, 2014Assignee: University of South FloridaInventors: Roman Manetsch, Richard Matthew Cross, Niranjan Kumar Namelikonda, Dennis Edward Kyle, Tina Susanna Mutka, Alexis Nichole LaCrue, Jordany Richarlson Maignan, Fabian Ernesto Saenz
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Patent number: 8865902Abstract: This invention relates to compounds of Formula I: and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CFTR potentiator.Type: GrantFiled: November 18, 2013Date of Patent: October 21, 2014Assignee: Concert Pharmaceuticals, Inc.Inventor: Adam J. Morgan
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Publication number: 20140303150Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.Type: ApplicationFiled: December 22, 2011Publication date: October 9, 2014Applicant: LEO Laboratories LimitedInventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø, Thomas Vifian
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Publication number: 20140303205Abstract: This invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein R is COOH or CH2OH.Type: ApplicationFiled: June 20, 2014Publication date: October 9, 2014Inventors: Xiaoqing Yang, Sara Sabina Hadida Ruah, Peter Diederik Jan Grootenhuis, Fredrick F. Van Goor, Martyn Curtis Botfield, Gregor Zlokarnik
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Publication number: 20140303204Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.Type: ApplicationFiled: June 6, 2014Publication date: October 9, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Lev T.D. Fanning, Dennis Hurley, Urvi Sheth, Alina Silina, Xiaoqing Yang, Martyn Botfield, Peter D.J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa