Plural Hetero Atoms In The Polycyclo Ring System Patents (Class 514/338)
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Patent number: 10130618Abstract: This invention is a novel pharmaceutical composition comprising dabigatran or a pharmaceutically acceptable salt thereof in combination with a proton pump inhibitor for use in the antithrombotic treatment with preventing or reducing the risk of a gastrointestinal disorder.Type: GrantFiled: April 9, 2015Date of Patent: November 20, 2018Assignee: SANOVEL ILAC SANAYI VE TICARET ANONIM SIRKETIInventors: Ali Türkyilmaz, Mehtap Saydam, Yildiz Gülkok, Nur Kirat Uzunogullari, Sevgi Gökcek
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Patent number: 10117840Abstract: This application describes a compound represented by Formula (I): (I) wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X1 is a covalent bond or —CH2CH2—, X2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.Type: GrantFiled: June 5, 2015Date of Patent: November 6, 2018Assignee: The Scripps Research InstituteInventors: Jiajia Dong, K. Barry Sharpless, Jeffery W. Kelly, Wentao Chen
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Patent number: 10065962Abstract: The present disclosure relates to an amino pyran ring derivative and a composition and use thereof, and in particular, to an amino pyran ring derivative represented by general formula (I) or a stereoisomer, a pharmaceutically acceptable salt or a prodrug thereof, a pharmaceutical composition comprising the derivative, and their medical use in the manufacture of a di-peptidyl peptidase IV (DPP-IV) inhibitor, in formula (I) the substituents are defined the same as those in the specification.Type: GrantFiled: May 14, 2015Date of Patent: September 4, 2018Assignee: SICHUAN HAISCO PHARMACEUTICAL CO., LTDInventors: Chen Zhang, Jianmin Wang, Caihu Li, Yonggang Wei
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Patent number: 10045973Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising an acid labile proton pump inhibitor and a buffering agent and to use of such compositions in treating nocturnal acid breakthrough.Type: GrantFiled: January 15, 2016Date of Patent: August 14, 2018Assignee: THE CURATORS OF THE UNIVERSITY OF MISSOURIInventor: Jeffrey Owen Phillips
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Patent number: 9969710Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.Type: GrantFiled: September 16, 2016Date of Patent: May 15, 2018Assignee: Merck Patent GmbHInventors: Catherine Jorand-Lebrun, Ruoxi Lan, Austin Chen, Ryan C. Clark
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Patent number: 9970938Abstract: Use of BUBR1 as a biomarker for predicting the response to a compound, preferably resistance of a disease such as cancer in a subject, wherein the compound is a compound of general formula I wherein R represents phenyl, thienyl or pyridinyl wherein phenyl is optionally substituted by one or two substituents independently selected from alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, monoalkylamino, dialkylamino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, cyano, halogen, and nitro; and wherein two adjacent substituents are methylenedioxy; and wherein pyridinyl is optionally substituted by lower alkoxy, amino or halogen; X represents a group C?Y, wherein Y stands for oxType: GrantFiled: March 4, 2016Date of Patent: May 15, 2018Assignee: BASILEA PHARMACEUTICA AGInventors: Heidi Alexandra Lane, Felix Bachmann, Madlaina Breuleux, Michael Boutros, Daniel Gilbert, Xian Zhang
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Patent number: 9938270Abstract: The present invention relates to crystalline and amorphous forms of 6-fluoro-2-[4-(pyridin-2-yl)but-3-yn-1-yl]imidazo[1,2-a]pyridine mono-phosphate salt and methods of making these solid forms thereof. The invention compounds are modulators of mGlu5 which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGlu5 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGlu5 is involved.Type: GrantFiled: September 25, 2014Date of Patent: April 10, 2018Assignee: Addex Pharma S.A.Inventors: Béatrice Bonnet, Sonia Maria Poli
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Patent number: 9924712Abstract: The present invention relates to a liquid concentrate formulation comprising a pyripyropene pesticide of the formula I as defined below and an alkoxylated aliphatic alcohol as an adjuvant. Moreover, the invention relates to the use of the formulations for the treatment of plants and seed and to corresponding methods.Type: GrantFiled: March 11, 2013Date of Patent: March 27, 2018Assignee: BASF SEInventors: Wen Xu, Matthias Pohlman
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Patent number: 9926290Abstract: This invention describes the development of targeted small molecule inhibitors of the inv(16) fusion, the causative agent in ˜12% of acute myeloid leukemia (AML). The inv(16) fusion results in expression of the CBF?-SMMHC fusion protein in the blood cells of afflicted patients. The present invention provides compounds which inhibit the function of both CBF? and the CBF?-SMMHC fusion. These compounds block the growth of an inv(16) leukemia cell line as well as increase its apoptosis, while showing minimal effects against non inv(16) cell lines. As a mechanism to develop inhibitors with selectivity for the CBF?-SMMHC fusion protein, the present invention further provides dimeric derivatives of these compounds which show both increased potency as well as selectivity for CBF?-SMMHC. These compounds show potent inhibition of an inv(16) leukemia cell line with minimal effects on non inv(16) cell lines.Type: GrantFiled: December 14, 2015Date of Patent: March 27, 2018Assignee: University of Virginia Patent FoundationInventors: John H. Bushweller, Jolanta Grembecka, Anuradha Illendula, Lauren Mishra
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Patent number: 9920145Abstract: The present invention relates to tackifier compounds and methods of using the same. In various embodiments, the present invention provides a tackifier compound including independently substituted or unsubstituted fused rings A and B each independently chosen from (C5-C10)cycloalkyl and (C2-C10)heterocyclyl. Fused ring A is substituted with (R1)1-8 and fused ring B is substituted with —(OC(O)R?C(O)R2)1-8. At each occurrence R? is independently chosen from (C2-C10)alkanylene, (C2-C10)alkenylene, (C2-C10)alkynylene, C5-C20(arylene), and (C1-C20)heteroarylene, wherein R? is unsubstituted or substituted. At each occurrence R1 is independently selected from —OH, —OR3, and —OC(O)R?C(O)R2. At each occurrence R2 is independently chosen from —OH, —OR3, —NH2, —NHR3, and —NR32. At each occurrence R3 is independently chosen from (C1-C10)alkanyl, (C2-C10)alkenyl, (C2-C10)alkynyl, C5-C20(aryl), and (C1-C20)heteroaryl, wherein R3 is unsubstituted or substituted.Type: GrantFiled: April 28, 2017Date of Patent: March 20, 2018Assignee: IOWA STATE UNIVERSITY RESEARCH FOUNDATION, INC.Inventors: Jason Shih-Hao Chen, Michael Richard Kessler, Michael Dennis Zenner
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Patent number: 9907751Abstract: Oral liquid colchicine formulations are described herein. Methods of using the oral liquid colchicine formulations are also provided.Type: GrantFiled: November 22, 2016Date of Patent: March 6, 2018Assignee: RxOMEG Therapeutics LLCInventors: Indu Muni, Naomi Vishnupad
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Patent number: 9834527Abstract: The present invention relates to macrocydic urea derivatives of the formula I (I) in which R1, R2, R3, V and Y are as defined below. The compounds of the formula I are inhibitors of the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor). The invention further relates to the process for the preparation of the compounds of formula I and to the use thereof as medicaments.Type: GrantFiled: June 5, 2014Date of Patent: December 5, 2017Assignee: SANOFIInventors: Andreas Evers, Christopher Kallus, Michael Wagner, Hermut Wehlan
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Patent number: 9820977Abstract: Pharmaceutically acceptable single parasiticidal agent compositions of imidacloprid for oral delivery to mammals to systemically control targeted blood-sucking or blood-consuming parasites, such as fleas, ticks and certain species of helminthes and scabies.Type: GrantFiled: May 22, 2009Date of Patent: November 21, 2017Assignee: BAYER HEALTHCARE LLCInventors: Roland H. Johnson, Douglas I. Hepler, Kathleen G. Palma, William R. Campbell
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Patent number: 9751890Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: October 19, 2016Date of Patent: September 5, 2017Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
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Patent number: 9737510Abstract: The patent discloses novel indazole compounds of general formula 1 and analogues thereof, use thereof for the treatment of diabetes, diabetic complications, cardiovascular dysfuntion or related diseases, pharmaceutical compositions comprising them and processes for their preparation.Type: GrantFiled: July 31, 2014Date of Patent: August 22, 2017Assignees: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH, SHANTANI PROTEOME ANALYTICS PVT. LTDInventors: Dumbala Srinivasa Reddy, Chaitanya Saxena, Kashinath Komirishetty
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Patent number: 9718771Abstract: A compound having an S1P1 receptor antagonistic activity. A compound represented by general formula (I): (in the formula, R1, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group or the like, R4 is a C1-6 alkyl group or the like, R5 is a C1-6 alkyl group or the like, R6 is a C1-6 alkyl group or the like, R7 is a hydrogen atom, a halogen atom, a C1-6 alkyl group or the like, R8 is a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group, a C1-6 alkoxy group or the like, and R9 is a hydrogen atom or a C1-6 alkyl group.) or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same, and use thereof. The compounds have an excellent S1P1 receptor antagonistic activity and are useful for the treatment or prevention of autoimmune diseases.Type: GrantFiled: February 27, 2015Date of Patent: August 1, 2017Assignee: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Hitoshi Inoue, Kohsuke Ohno, Tetsuya Nakamura, Yusuke Ohsawa
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Patent number: 9718802Abstract: The present invention relates to novel crystal forms M and N of dabigatran etexilate mesylate and preparation method and uses thereof, wherein the X-Ray powder diffractogram of the crystal form M has characteristic peaks at the following 2? diffraction angles: 5.7±0.2°, 6.2±0.2°, 11.2±0.2°, 12.4±0.2°, 18.2±0.2°, 21.4±0.2°, 21.8±0.2° and 23.6±0.2°; and the X-Ray powder diffractogram of the crystal form N has characteristic peaks at the following 2? diffraction angles: 6.0±0.2°, 11.8±0.2°, 18.2±0.2°, 21.6±0.2°, 24.4±0.2°, 27.7±0.2° and 29.7±0.2°. The crystal forms of the present invention have excellent properties in the aspects of leaching time, biological release, chemical stability and processing adaptability.Type: GrantFiled: March 4, 2015Date of Patent: August 1, 2017Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.Inventors: Liang Zhang, Chuan Liu, Jinyi Xu, Zhaozhao Zhang, Zhi Chen, Jian Chai, Zhiqing Yang, Hairong Luo, Xiangyang Zhang
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Patent number: 9688794Abstract: The present invention relates to tackifier compounds and methods of using the same. In various embodiments, the present invention provides a tackifier compound including independently substituted or unsubstituted fused rings A and B each independently chosen from (C5-C10)cycloalkyl and (C2-C10)heterocyclyl. Fused ring A is substituted with (R1)1-8 and fused ring B is substituted with —(OC(O)R?C(O)R2)1-8. At each occurrence R? is independently chosen from (C2-C10)alkanylene, (C2-C10)alkenylene, (C2-C10)alkynylene, C5-C20(arylene), and (C1-C20)heteroarylene, wherein R? is unsubstituted or substituted. At each occurrence R1 is independently selected from —OH, —OR3, and —OC(O)R?C(O)R2. At each occurrence R2 is independently chosen from —OH, —OR3, —NH2, —NHR3, and —NR32. At each occurrence R3 is independently chosen from (C1-C10)alkanyl, (C2-C10)alkenyl, (C2-C10)alkynyl, C5-C20(aryl), and (C1-C20)heteroaryl, wherein R3 is unsubstituted or substituted.Type: GrantFiled: October 15, 2013Date of Patent: June 27, 2017Assignee: Iowa State University Research Foundation, Inc.Inventors: Jason Shih-Hao Chen, Michael Richard Kessler, Michael Dennis Zenner
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Patent number: 9670223Abstract: A compound having the structural formula (I) and pharmaceutically acceptable salt and/or hydrates thereof, (I) wherein Y is an arylester or an C1-C8 alkylaryl ester, selected from the group consisting of: benzene, toluene, xylene, benzoic acid, benzoate, nicotinate, isonicotinate and halobenzene, which can be unsubstituted or substituted with at least one nitric oxide releasing group; and/or at least one of hydroxide, —Cl, —Br, a C1-C8 alkyl, benzyl, a C1-C8 alkoxy, benzyloxy, —NHC(O)R, —NH2, —NO2, —ONO2, —(CH2)nONO2, —OC(O)[(CH2)m], cyclic ONO2, —OCOArONO2, —OCOAr(CH2)nONO2 or a C1-C5 haloalkyl ester, wherein R is a C1-C8 alkyl or a C1-C8 alkoxy group, n=1-8 and m=3-10, to produce a super-aspirin effect.Type: GrantFiled: April 8, 2015Date of Patent: June 6, 2017Assignee: SOLVOTRIN THERAPEUTICS LTD.Inventors: John Francis Gilmer, Mark Ledwidge, Pat O'Flynn, Shona Harmon, Marek Radomski, Carlos Medina Martin
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Patent number: 9598370Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: GrantFiled: September 15, 2015Date of Patent: March 21, 2017Assignee: Akebia Therapeutics, Inc.Inventors: Richard Masaru Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
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Patent number: 9573963Abstract: A fused heterocyclic compound represented by formula (1) or an N-oxide thereof has an excellent control effect on pests: wherein A1 represents N or the like, A2 represents NR6 or the like, A3 represents CR12 or the like, R1 represents a C1 to C6 chain hydrocarbon group or the like, R2, R4 and R5 are the same or different and represent a C1 to C3 alkyl group optionally having one or more halogen atoms or the like, R3 represents a C1 to C6 chain hydrocarbon group or the like, R6 represents a C1 to C6 chain hydrocarbon group or the like, any one set of R9 and R10, R10 and R11, and R11 and R12 in R9, R10, R11 and R12, together with the carbon atoms to which they are bound, forms a ring, and n represents 0, 1 or 2.Type: GrantFiled: February 19, 2014Date of Patent: February 21, 2017Assignee: Sumitomo Chemical Company, LimitedInventors: Takamasa Tanabe, Mai Ito, Chie Shimizu, Yoshihiko Nokura
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Patent number: 9567328Abstract: The present invention provides a compound, that is a 1-({halo-2-[(2-hydrocarbyl or substituted hydrocarbyl)oxy]phenyl}methyl)-(fused bicyclic nitrogen heteroaryl) carboxylic acid or an ester or sulfonamide thereof. The compound may be represented by the following formula Wherein R1, R2, R3, R4 A, X, W, Z and Y are as defined in the specification. The compounds may be administered to treat DP, FP, EP1, TP and/or EP4 receptor-mediated diseases or conditions.Type: GrantFiled: December 19, 2012Date of Patent: February 14, 2017Assignee: ALLERGAN, INC.Inventors: William R. Carling, Jose L. Martos, Jussi J. Kangasmetsa, Jenny W. Wang, David F. Woodward
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Patent number: 9463186Abstract: The present invention provides systems, compositions and methods for treatment of dopaminergic disorders (e.g., Parkinson's disease) using the combination of a first compound that inhibits a voltage-gated calcium channel of the type Cav1.3 (e.g., a dihydropyridine such as isradipine), and a second compound that is monoamine oxidase inhibitor and/or is a nitric oxide synthase inhibitor (e.g., rasagiline or derivative thereof).Type: GrantFiled: April 15, 2014Date of Patent: October 11, 2016Assignee: Northwestern UniversityInventors: Dalton J. Surmeier, Javier Sanchez, Jaime Guzman, Enrico Zampese, Daniel Galtieri, Ema Ilijic
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Patent number: 9402835Abstract: Compositions and methods for the treatment and control of various conditions in an animal which comprises administering to said animal an effective amount of a immediate release composition of about 0.5% to 50% wt/wt of active ingredient together with excipients to a total of about 100%, wherein said composition dissolves in a relatively short period of time, e.g., 75 seconds or less, 5 seconds or less, or 3 seconds or less, upon administration to said animal.Type: GrantFiled: May 12, 2014Date of Patent: August 2, 2016Assignee: NEWMARKET PHARMACEUTICALS LLCInventors: David Rock, Mark Ridall
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Patent number: 9381177Abstract: The present invention relates to: combinations of: component A: one or more omega-carboxyaryl-substituted diphenyl urea compounds of general formula (I), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; component B: one or more N-(2-arylamino)aryl sulfonamide compounds of general formula (II), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; and, optionally, component C: one or more further pharmaceutical agents; in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially. dependently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route; use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer; and a kit comprising such a combination.Type: GrantFiled: September 29, 2011Date of Patent: July 5, 2016Assignee: BAYER INTELLECTUAL PROPERTY GMBHInventors: Florian Pühler, Marion Hitchcock
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Patent number: 9370184Abstract: 6-Pyridone-2-carbamoylazoles of the general formula (I) are described as herbicides. In this formula (I), W, X and Z represent radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q represents a 5-membered radical such as oxadiazyl.Type: GrantFiled: April 30, 2013Date of Patent: June 21, 2016Assignee: Bayer Cropscience AGInventors: Ralf Braun, Stefan Lehr, Arnim Koehn, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger, Dirk Schmutzler
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Patent number: 9365554Abstract: The present invention relates to viral polymerase inhibitors of formula (I) or salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections.Type: GrantFiled: April 11, 2013Date of Patent: June 14, 2016Assignee: AVIRAGEN THERAPEUTICS, INC.Inventors: Silas Bond, Rosliana Halim, Tyrone Pieter Jeynes, Alistair George Draffan, Michael Harding
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Patent number: 9327031Abstract: Buffer solutions for pharmaceutical preparations that have bactericidal activity preferentially against gram negative bacteria are provided. The buffers have a pH of greater than about 10 or less than about 4.5 with low buffer capacity. Methods of their use in reducing the occurrence of blood stream infections in a mammal is also provided.Type: GrantFiled: January 17, 2014Date of Patent: May 3, 2016Assignee: United Therapeutics CorporationInventors: Roger Andrew Jeffs, David Zaccardelli
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Patent number: 9278983Abstract: A fused heterocyclic compound the formula (1): wherein A1 represents —NR8—, and the like; A2 represents a nitrogen atom, and the like; A3 represents a nitrogen atom, and the like; R1 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R2, R3, R4, and R5 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more halogen atoms, and the like; R6 and R7 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R8 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group W, and the like; n represents 0, 1 or 2. The compound has an excellent activity of controlling pests.Type: GrantFiled: August 21, 2014Date of Patent: March 8, 2016Assignee: Sumitomo Chemical Company, LimitedInventors: Hayato Takyo, Masaki Takahashi, Takamasa Tanabe, Yoshihiko Nokura, Mai Ito, Atsushi Iwata
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Patent number: 9273055Abstract: The present disclosure relates to the field of tyrosine kinase enzyme inhibition, in particular anaplastic lymphoma kinase (ALK) inhibition using novel small molecules. Provided are compounds capable to modulate ALK activity, compositions that comprise the compounds, and methods of using the compounds for the treatment or prevention of diseases or conditions that are characterized by ALK activity or expression.Type: GrantFiled: June 18, 2014Date of Patent: March 1, 2016Assignee: CHEMBRIDGE CORPORATIONInventor: Vlad Edward Gregor
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Patent number: 9238029Abstract: Herein provided are dosage forms (variously referred to as “formulations”) comprising a PPI that is released from the dosage form as a first and a second dose. Each dose of PPI is present in an amount sufficient to raise the plasma levels of the PPI to at least 100 ng/ml.Type: GrantFiled: April 30, 2013Date of Patent: January 19, 2016Assignee: Takeda Pharmaceuticals U.S.A., Inc.Inventors: Rajneesh Taneja, Majid Vakilynejad
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Patent number: 9221764Abstract: This invention describes the development of targeted small molecule inhibitors of the inv(16) fusion, the causative agent in ˜12% of acute myeloid leukemia (AML). The inv(16) fusion results in expression of the CBF?-SMMHC fusion protein in the blood cells of afflicted patients. The present invention provides compounds which inhibit the function of both CBF? and the CBF?-SMMHC fusion. These compounds block the growth of an inv(16) leukemia cell line as well as increase its apoptosis, while showing minimal effects against non inv(16) cell lines. As a mechanism to develop inhibitors with selectivity for the CBF?-SMMHC fusion protein, the present invention further provides dimeric derivatives of these compounds which show both increased potency as well as selectivity for CBF?-SMMHC. These compounds show potent inhibition of an inv(16) leukemia cell line with minimal effects on non inv(16) cell lines.Type: GrantFiled: May 7, 2014Date of Patent: December 29, 2015Assignee: University of Virginia Patent FoundationInventors: John H. Bushweller, Jolanta Grembecka, Anuradha Illendula, Lauren Dixon
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Patent number: 9205078Abstract: The present invention relates to a method of treating chronic myelogenous leukemia in a subject comprising administering to the subject a compound, such as N-methyl-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]-benzamide, that inhibits the T315I mutation in BCR-ABL tyrosine kinase, or a pharmaceutically acceptable salt thereof. The present invention also relates to a pharmaceutical composition comprising a compound such as N-methyl-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]-benzamide, that inhibits the T315I mutation in BCR-ABL tyrosine kinase, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent.Type: GrantFiled: November 5, 2012Date of Patent: December 8, 2015Assignee: PFIZER INC.Inventor: Brion William Murray
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Patent number: 9192606Abstract: The present invention relates to formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in Form I, pharmaceutical packs or kits thereof, and methods of treatment therewith.Type: GrantFiled: March 19, 2014Date of Patent: November 24, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventor: Christopher Young
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Patent number: 9181234Abstract: The present invention provides a compound of the following formula and salts thereof: Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.Type: GrantFiled: October 7, 2011Date of Patent: November 10, 2015Assignee: Biota Europe Ltd.Inventors: James T Palmer, Christopher James Lunnis, Daniel A Offermann, Lorraine Claire Axford, Michael Blair, Dale Mitchell, Nicholas Palmer, Christopher Steele, John Atherall, David Watson, David Haydon, Lloyd Czaplewski, David Davies, Ian Collins, Edward Malcolm Tyndall, Laura Andrau, Gary Robert William Pitt
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Patent number: 9156834Abstract: The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C1-C4 alkyl, or linear or branched C1-C4 alkoxy, A represents oxygen or sulphur, B represents nitrogen when n=1 or 2 and D represents —C(?O)—, or B represents CH when n=0 and D represents —CH2O— or when n=1 and D represents —O—, R2 represents a hydrogen, a methyl, a fluorine or chlorine atom or a methoxy, HetAr represents a pyridyl or quinolyl group, possibly substituted by a group such as a linear or branched C1-C4 alkyl, a linear or branched C1-C4 alkoxy, a halogen, or a trifluoromethyl, and to their pharmaceutically acceptable salts.Type: GrantFiled: August 15, 2014Date of Patent: October 13, 2015Assignee: PIERRE FABRE MEDICAMENTInventors: Elisabeth Dupont-Passelaigue, Isabelle Le Roy, Christophe Pignier
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Patent number: 9145389Abstract: A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.Type: GrantFiled: October 7, 2014Date of Patent: September 29, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Akira Fujishima, Isao Aoki
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Patent number: 9138426Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: January 7, 2015Date of Patent: September 22, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Ann E. Weber
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Patent number: 9115118Abstract: The present invention relates to process for the resolution of omeprazole. The present invention further provides a novel compound of enantiomers of omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a solid of (R)- or (S)-omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a process for the preparation of esomeprazole magnesium dehydrate substantially free of its trihydrate form. The present invention also provides a process for the preparation of recovery of chiral BINOL.Type: GrantFiled: April 29, 2014Date of Patent: August 25, 2015Assignee: Hetero Research FoundationInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Bandi Vamsi Krishna, Voggu Ramesh Reddy
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Patent number: 9095578Abstract: The present invention relates to a method of preventing or treating a disease caused by infection by a eukaryotic pathogen, wherein the method comprises administering an effective amount of a modulator of a eukaryotic pathogen's adenylyl cyclase. The invention also provides pharmaceutical compositions useful for preventing or treating a disease, with the compositions containing a therapeutically effective amount of a modulator of a eukaryotic pathogen's adenylyl cyclase. The invention also provides screening methods for identifying selective modulators of a eukaryotic pathogen's adenylyl cyclase that do not substantially modulate an adenylyl cyclase of the subject. The invention also provides methods for culturing eukaryotic pathogens and methods for inducing the pathogenic state in vitro.Type: GrantFiled: January 11, 2008Date of Patent: August 4, 2015Assignee: CORNELL RESEARCH FOUNDATION, INC.Inventors: Lonny Levin, Jochen Buck, Leo Brizuela, Michael Pinnisi
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Patent number: 9096587Abstract: The present invention relates to compounds of formula (I), to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy: Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway and increased presence of nuclear ?-catenin. For example, these may be used in preventing and/or retarding proliferation of tumor cells and metastasis, for example carcinomas such as colon carcinomas.Type: GrantFiled: December 8, 2011Date of Patent: August 4, 2015Assignee: OSLO UNIVERSITY HOSPITAL HFInventors: Daniel Holsworth, Jo Waaler, Ondrej Machon, Stefan Krauss, Andrey Edward Voronkov
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Patent number: 9085556Abstract: The present invention relates to the salts of dexlansoprazole in amorphous form. The present invention further relates to processes for the preparation of salts of dexlansoprazole.Type: GrantFiled: March 29, 2011Date of Patent: July 21, 2015Assignee: RANBAXY LABORAOTORIES LIMITEDInventors: Anu Mittal, Anmol Kumar Ray, Mahavir Singh Khanna, Rajesh Kumar Thaper, Mohan Prasad
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Patent number: 9067914Abstract: Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-related kinase B (TrkB), tropomyosin-related kinase C (TrkC), and/or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)).Type: GrantFiled: December 9, 2014Date of Patent: June 30, 2015Assignee: Genzyme CorporationInventors: John L. Kane, Jr., Gloria Matthews, Markus Metz, Michael Kothe, Jinyu Liu, Andrew Scholte
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Publication number: 20150148334Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: June 27, 2014Publication date: May 28, 2015Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
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Patent number: 9040565Abstract: There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.Type: GrantFiled: September 25, 2009Date of Patent: May 26, 2015Assignee: Orexo ABInventors: Roland Pfau, Kirsten Arndt, Henri Doods, Norbert Hauel, Klaus Klinder, Raimund Kuelzer, Juergen Mack, Dirk Stenkamp
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Patent number: 9040564Abstract: It is intended to provide a pharmaceutical composition which contains a proton pump inhibitor and is stable even if it is stored for a long time. It is also intended to provide a pharmaceutical composition which contains a proton pump inhibitor susceptible to acid, and does not dissolve in the stomach but dissolves in the intestine to release a primary drug product promptly. The object could be achieved by the pharmaceutical composition characterized in that a layer containing a proton pump inhibitor and ethyl cellulose, a layer containing an enteric polymer, and if necessary an intermediate layer composed of one or more layers are formed on a pharmacologically inactive core substance. The intermediate layer is composed of a water-insoluble polymer, a water-soluble polymer, a lubricant and the like.Type: GrantFiled: November 8, 2007Date of Patent: May 26, 2015Assignee: EISAI R&D MANAGEMENT CO., LTD.Inventors: Koji Ukai, Norishige Takami
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Publication number: 20150139909Abstract: The present invention relates to the field of osteoarthritis. More specifically, the present invention provides compositions and methods useful for treating or preventing osteoarthritis. In one embodiment, a method for treating or preventing osteoarthritis in a patient comprises the step of administering to the patient a therapeutically effective amount of a transforming growth factor beta (TGF-beta) inhibitor.Type: ApplicationFiled: May 1, 2013Publication date: May 21, 2015Inventor: Xu Cao
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Publication number: 20150140094Abstract: A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a binder, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering an oral pharmaceutical formulation of Compound 1 to the patient.Type: ApplicationFiled: November 14, 2014Publication date: May 21, 2015Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Marinus Jacobus Verwijs, Rossitza Gueorguieva Alargova, Ritu Rohit Kaushik, Irina Nikolaevna Kadiyala, Christopher Young
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Publication number: 20150141464Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit cdk5 -mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: ApplicationFiled: November 20, 2012Publication date: May 21, 2015Inventors: Amy S. RIPKA, Jeffrey O. SAUNDERS
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Publication number: 20150141423Abstract: Disclosed are pesticidally active pyridyl- and pyrimidyl-substituted thiazole derivatives, processes for their preparation, compositions comprising those compounds, and their use for controlling insects.Type: ApplicationFiled: June 4, 2013Publication date: May 21, 2015Applicant: Syngenta Participations AGInventors: Ruifang Chen, Laura Quaranta, Andrew Edmunds, Andre Jeanguenat, Aurelien Bigot, Sebastian Rendler, Roger Graham Hall, Long Lu, Peter Renold