The Five-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/373)
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Patent number: 11945809Abstract: A method of treating cancer can include administering one or more of the isatin derivatives to a patient in need thereof. In an embodiment, the cancer is selected from the group consisting of breast cancer, non-small cell lung cancer, renal cancer and melanoma.Type: GrantFiled: July 19, 2020Date of Patent: April 2, 2024Assignee: KING SAUD UNIVERSITYInventors: Ahmed Bari, Saeed Ali Syed, Mohammad A. Altamimi
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Patent number: 10125122Abstract: The invention relates to a method of synthesizing methyl (Z)-3-[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl] amino]phenylmethylene)-oxindole-6-carboxylate of formula (1), known under the generic name of intedanib or nintedanib. The present method comprises a) a reaction of methyl oxindole-6-carboxylate with acetic anhydride at a temperature of 130-140° C.Type: GrantFiled: July 28, 2016Date of Patent: November 13, 2018Assignee: Zentiva k.s.Inventor: Ludek Meca
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Patent number: 9682946Abstract: Provided herein are novel, commercially viable and industrially advantageous processes for the preparation of benzofuran-2-carboxamide derivatives and their intermediates, or a pharmaceutically acceptable salt thereof, in high yield and purity. Provided particularly herein are novel, commercially viable and industrially advantageous processes for the preparation of vilazodone or a pharmaceutically acceptable salt thereof in high yield and purity. Provided also herein is an improved and commercially viable process for the preparation of 3-(4-hydroxybutyl)-1H-indole-5-carbonitrile, in high yield and purity, using novel intermediate compound 3-(4-hydroxybutyryl)-1H-indole-5-carbonitrile.Type: GrantFiled: October 5, 2015Date of Patent: June 20, 2017Assignee: Symed Labs LimitedInventors: Mohan Rao Dodda, Jithender Aadepu
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Patent number: 9580415Abstract: The compound of formula (I) are inhibitors of SSAO activity (Formula (I)) wherein the terms Y, Z, W, R1 and R2 are defined in the claims.Type: GrantFiled: March 13, 2014Date of Patent: February 28, 2017Assignee: Proximagen LimitedInventors: Lee Patient, David Evans, Iain Simpson, Allison Powell
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Patent number: 9448242Abstract: The present invention relates to treating and preventing pain. More particularly the present invention demonstrates the involvement of K2P potassium channels in the antalgic effect of morphine. The present invention therefore provides a screening method for identifying antalgics.Type: GrantFiled: September 21, 2010Date of Patent: September 20, 2016Assignee: UNIVERSITE D'AUVERGNE CLERMONT IInventors: Alain Eschalier, Jéröme Busserolles, Abdelkrim Alloui, Michel Lazdunski
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Patent number: 9428498Abstract: The present invention relates to compounds which are inhibitors of SSAO activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumor growth.Type: GrantFiled: March 13, 2014Date of Patent: August 30, 2016Assignee: Proximagen LimitedInventors: Max Espensen, Lee Patient, David Evans, Edward Savory, Iain Simpson
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Patent number: 9399630Abstract: Provided herein are novel, commercially viable and industrially advantageous processes for the preparation of benzofuran-2-carboxamide derivatives and their intermediates, or a pharmaceutically acceptable salt thereof, in high yield and purity. Provided particularly herein are novel, commercially viable and industrially advantageous processes for the preparation of vilazodone or a pharmaceutically acceptable salt thereof in high yield and purity. Provided also herein is an improved and commercially viable process for the preparation of 3-(4-hydroxybutyl)-1H-indole-5-carbonitrile, in high yield and purity, using novel intermediate compound 3-(4-hydroxybutyryl)-1H-indole-5-carbonitrile.Type: GrantFiled: July 1, 2013Date of Patent: July 26, 2016Assignee: Symed Labs LimitedInventors: Mohan Rao Dodda, Jithender Aadepu
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Patent number: 9382233Abstract: Vilazodone hydrochloride benzyl alcohol solvates are provided as well as processes for the preparation thereof.Type: GrantFiled: June 13, 2013Date of Patent: July 5, 2016Assignee: Apotex Inc.Inventors: Gamini Weeratunga, Murali Kondamreddy, Allan W. Rey, Cameron L. McPhail, Yajun Zhao
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Publication number: 20150126526Abstract: Co-crystal of a serotonin reuptake inhibitor, in stable form.Type: ApplicationFiled: November 4, 2014Publication date: May 7, 2015Applicant: DIPHARMA FRANCIS S.R.L.Inventors: Nicolas TESSON, Jordi de Mier VINUÉ
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Publication number: 20150126525Abstract: Provided are crystalline and amorphous vilazodone hydrochloride. Further provided are amorphous solid dispersions of vilazodone hydrochloride with pharmaceutically acceptable carries. Also provided is a process for the preparation of form I of vilazodone free base.Type: ApplicationFiled: May 10, 2013Publication date: May 7, 2015Inventors: Javed Iqbal, Srinivas Oruganti, Rajesh Kumar Rapolu, Vishweshwar Peddy, Rajesham Boge, Deepika Pathivada, Dharma Jagannadha Rao Velaga, Sesha Reddy Yarraguntla, Sudhakar Reddy Baddam, Anitha Naredla, Kiran Kumar Doniparthi, Ramesh Kumar Nadgoud, Narasimha Rao Pagadala, Syam Kumar Unniaran, Srividya Ramakrishnan
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Patent number: 9018214Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: April 20, 2012Date of Patent: April 28, 2015Assignee: Astex Therapeutics LimitedInventors: Alison Jo-Anne Woolford, Steven Howard, Ildiko Maria Buck, Gianni Chessari, Christopher Norbert Johnson, Emiliano Tamanini, James Edward Harvey Day, Elisabetta Chiarparin, Thomas Daniel Heightman, Martyn Frederickson, Charlotte Mary Griffiths-Jones
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Publication number: 20150105548Abstract: The present invention relates to anti-HCV compounds, compositions comprising the same and methods of using the same to treat HCV infection.Type: ApplicationFiled: May 25, 2012Publication date: April 16, 2015Inventors: Allan Krueger, Warren M. Kati, Clarence J. Maring, Rolf Wagner, Charles W. Hutchins
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Publication number: 20150099746Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: October 16, 2014Publication date: April 9, 2015Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone
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Patent number: 8999994Abstract: The present invention relates to a compound of formula (I): wherein: R1 and R2 are selected from among H and C1-C10 alkyl; R3 is selected from among H, —OR4, N, —CN, —C(O)R4, —C(O)OR4, —C(O)NR4R5, —C?NR4, —OC(O)R4, —NR4R5, —NR4C(O)R5, —NO2, —N?CR4R5, halogen and C1-C10 alkyl, wherein R4 and R5 are selected from among H, alkyl, alkenyl, cycloalkyl and aryl; X, Y, Z1, Z2 and Z3 are selected independently from among CH and N; A is selected from among (CH2)n, NH, O and CO, wherein n is an integer between 1 and 6, to the procedure for the obtainment of said compounds, to a pharmaceutical composition comprising said compound, and to the use thereof in the treatment of a neurodegenerative disease, more particularly treatment of Alzheimer's or Parkinson's disease.Type: GrantFiled: March 18, 2011Date of Patent: April 7, 2015Assignees: Consejo Superior de Investigaciones Cientificas, Universitat Autonoma de Barcelona, Universidad de BarcelonaInventors: Abdelouahid Samadi, José Luis Marco Contelles, Irene Bolea Tomás, Francisco Javier Luque Garriga, Mercedes Unzeta López
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Publication number: 20150090936Abstract: Provided herein are heptamethine cyanine dyes having a large Stokes shift, and the salts and conjugates thereof. Also provided are methods of using and making such large Stokes shift dyes as fluorescence resonance energy transfer (FRET) acceptors or donors.Type: ApplicationFiled: December 10, 2014Publication date: April 2, 2015Inventors: Yi-Zhen HU, Hee Chol KANG
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Patent number: 8993762Abstract: Improved synthetic methods for the production of thaxtomin analogs, particularly thaxtomin A, and intermediates therefore such as substituted tryptophans and in particular, 4-nitro-L-tryptophan, and substituted phenyl acrylic acids are disclosed. Bioassays show that the synthetic thaxtomin A is not significantly different from the natural one in herbicidal activity.Type: GrantFiled: March 15, 2013Date of Patent: March 31, 2015Assignee: Marrone Bio Innovations, Inc.Inventors: Huazhang Huang, Dong Yan, Zhijie Xue, Hongbo Zhang
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Publication number: 20150087835Abstract: The present invention relates to an improved process for the preparation of vilazodone Hydrochloride and a process for preparation of novel pure amorphous form of vilazodone hydrochloride.Type: ApplicationFiled: April 5, 2013Publication date: March 26, 2015Applicant: ALEMBIC PHARMACEUTICALS LIMITEDInventors: Venkat Raman Jayaraman, Dhiraj Rathod, Irfan Vohra, Vinayak Bhujade, Viral Modi, Mayur Budh, Ojas Gandhi
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Publication number: 20150080411Abstract: The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypertension, cerebral disorders, chronic pain, acromegaly, hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.Type: ApplicationFiled: November 21, 2014Publication date: March 19, 2015Applicant: MERCK PATENTGESELLSCHAFTInventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Bottcher
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Publication number: 20150080316Abstract: The invention relates to new functionalized thieno-indole derivatives of formula (I) or (II) which have cytotoxic activity and are useful in treating diseases such as cancer and cellular proliferation disorders. The invention also relates to the use of these functionalized thieno-indole derivatives in the preparation of conjugates.Type: ApplicationFiled: March 28, 2013Publication date: March 19, 2015Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Italo Beria, Michele Caruso, Vittoria Lupi, Paolo Orsini, Matteo Salsa
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Publication number: 20150073148Abstract: The present invention relates to a process for the preparation of crystalline vilazodone hydrochloride.Type: ApplicationFiled: April 16, 2013Publication date: March 12, 2015Inventors: Prasenjit Prafulla Das, Bindu Srivastava, Nitin Maheshwari, Hashim Nizar Poovanathil Nagoor Meeran, Mohan Prasad, Sudershan Kumar Arora
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Publication number: 20150064623Abstract: A novel compound having satisfactory sensitivity (base generating performance), a photosensitive resin composition containing the compound as a photo-initiator, and a cured product of the composition are provided. Specifically, a compound represented by general formula (1) (compound (1)), a photosensitive resin composition containing (A) a photo-initiator including at least one compound (1) and (B) a photosensitive resin are provided. Preferred are the compound (1) in which R1 is an unsubstituted or substituted C6-C20 aromatic hydrocarbon group, the compound (1) in which at least one of R5, R6, R7, R8, R9, R10, and R11 is nitro, and the compound (1) in which n is 0. The symbols in general formula (1) are as defined in the description.Type: ApplicationFiled: March 5, 2013Publication date: March 5, 2015Inventors: Takeo Oishi, Koichi Kimijima, Nobuhide Tominaga, Hirokatsu Shinano, Daisuke Sawamoto
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Publication number: 20150057248Abstract: Embodiments of the invention are directed to compounds that are positive allosteric modulators of AMPA receptors.Type: ApplicationFiled: September 1, 2014Publication date: February 26, 2015Applicant: The Board of Regents of The University of Texas SystemInventors: Jia Zhou, Haijun Chen, Kenneth M. Johnson, Cheng Z. Wang
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Publication number: 20150051144Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as hyperlipidemia and also have a beneficial effect on cholesterol.Type: ApplicationFiled: September 26, 2012Publication date: February 19, 2015Inventors: Harikishore Pingali, Vrajesh Pandya
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Publication number: 20150051154Abstract: The present invention relates to a novel class of alkylating agents comprising a thieno-indole moiety linked to a DNA-binding moiety, which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds or the pharmaceutical composition containing them. The invention also relates to the use of this novel class of alkylating agents in the preparation of conjugates.Type: ApplicationFiled: March 28, 2013Publication date: February 19, 2015Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Italo Beria, Michele Caruso, Vittoria Lupi, Paolo Orsini, Matteo Salsa, Achille Panzeri
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Publication number: 20150045362Abstract: The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.Type: ApplicationFiled: August 25, 2014Publication date: February 12, 2015Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford
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Publication number: 20150018370Abstract: The invention relates to a new solvate, Vilazodone hydrochloride monoethanol monohydrate solvate, and to a process for the preparation of polymorphic form III of Vilazodone hydrochloride via the Vilazodone hydrochloride monoethanol monohydrate solvate.Type: ApplicationFiled: July 9, 2014Publication date: January 15, 2015Inventors: Marijan Stefinovic, Clemens Haefele, Ulrich J. Griesser
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Publication number: 20150018310Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: September 29, 2014Publication date: January 15, 2015Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone, Julie Wurster
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Publication number: 20150018339Abstract: Compounds having the general formula II, III, or IV wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.Type: ApplicationFiled: February 21, 2014Publication date: January 15, 2015Inventors: Christopher R. MCCURDY, Christophe Mesangeau, Bonnie Ann Avery, Ahmed Hassan Amin Abdelazeem, Frederick T. Chin, Jacques Henri Poupaert
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Patent number: 8927552Abstract: The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.Type: GrantFiled: October 23, 2012Date of Patent: January 6, 2015Assignee: Merck PatentgesellschaftInventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Böttcher
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Patent number: 8927546Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.Type: GrantFiled: September 22, 2010Date of Patent: January 6, 2015Assignee: Dart Neuroscience (Cayman) Ltd.Inventors: Alan P. Kaplan, Terence P. Keenan, Michael I. Weinhouse, Mark E. Wilson, Andrew K. Lindstrom, William C. Ripka, Mi Chen
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Patent number: 8921375Abstract: The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypertension, cerebral disorders, chronic pain, acromegaly, hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.Type: GrantFiled: May 30, 2014Date of Patent: December 30, 2014Assignee: Merck PatentgesellschaftInventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Bottcher
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Publication number: 20140378472Abstract: The present invention relates to amorphous vilazodone hydrochloride, its process of preparation and pharmaceutical composition thereof.Type: ApplicationFiled: December 12, 2012Publication date: December 25, 2014Inventors: Poonam Kaushik, Ram Thaimattam, Mohan Prasad, Sudershan Kumar Arora
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Patent number: 8912199Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: October 21, 2013Date of Patent: December 16, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
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Patent number: 8912195Abstract: Compounds of Formula (I), including pharmaceutically acceptable salts thereof, wherein A is selected from the group (II), are useful as HIV attachment inhibitors.Type: GrantFiled: December 1, 2011Date of Patent: December 16, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, Zhongxing Zhang, Zhiwei Yin, John F. Kadow, Nicholas A. Meanwell
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Publication number: 20140364610Abstract: The present invention relates to certain heteroaromatic compounds of Formula (Ia), or pharmaceutically acceptable salts thereof, and uses of such compounds in the treatment of synucleopathies.Type: ApplicationFiled: August 21, 2014Publication date: December 11, 2014Inventors: Eliezer MASLIAH, Edward M. ROCKENSTEIN, Wolfgang WRASIDLO, Igor Flint TSIGELNY
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Publication number: 20140349986Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.Type: ApplicationFiled: July 24, 2014Publication date: November 27, 2014Applicant: SANOFIInventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
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Publication number: 20140350255Abstract: The present invention relates to a process for the preparation of vilazodone or its pharmaceutically acceptable salts. The present invention further provides a crystalline form of vilazodone free base.Type: ApplicationFiled: February 1, 2013Publication date: November 27, 2014Inventors: Prasenjit Prafulla Das, Bindu Srivastava, Nitin Maheshwari, Hashim Nizar Poovanathil Nagoor Meeran, Mohan Prasad, Sudershan Kumar Arora
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Publication number: 20140336200Abstract: Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.Type: ApplicationFiled: July 23, 2014Publication date: November 13, 2014Applicant: ADAMED SP. Z O.O.Inventors: Marcin KOŁACZKOWSKI, Piotr KOWALSKI, Jolanta Jaskowska, Monika MARCINKOWSKA, Katarzyna MITKA, Adam BUCKI, Anna WESOŁOWSKA, Maciej PAWŁOWSKI
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Patent number: 8877772Abstract: Provided are compounds having an inhibitory effect on Mixed Lineage Kinases, having a structural Formula, Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders which comprise the inhibition of Mixed Lineage Kinases.Type: GrantFiled: November 25, 2009Date of Patent: November 4, 2014Assignee: University of RochesterInventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Colin Loweth, Torsten Wiemann
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Patent number: 8877923Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: December 20, 2012Date of Patent: November 4, 2014Assignee: Allergan, Inc.Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone
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Patent number: 8877927Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof (I), wherein: one of R1 and R2 is H, and the other is selected from F and Cl, or R1 and R2 are both F; R3 is selected from cyclopentyl and cyclohexyl; R4 is an optionally substituted 5- or 6-membered monocyclic or an 8- to 10-membered bicyclic aryl or heteroaryl ring which includes up to four heteroatoms. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.Type: GrantFiled: January 8, 2009Date of Patent: November 4, 2014Assignee: Grunenthal GmbHInventors: Martin Quibell, John Paul Watts
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Publication number: 20140323498Abstract: The present invention provides solid state forms of Vilazodone and Vilazodone hydrochloride, processes for preparing these solid state forms, and pharmaceutical compositions comprising one or more of these solid state formsType: ApplicationFiled: November 21, 2012Publication date: October 30, 2014Inventors: Edislav Leksic, Dubravka Pavlicic, Dijana Skalec Samec, Jasna Dogan
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Patent number: 8865130Abstract: The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the disclosed compositions for diagnosing (i.e., by imaging) a target cell and/or treating a disorder associated with a cyclooxygenase-2 biological activity.Type: GrantFiled: March 27, 2012Date of Patent: October 21, 2014Assignee: Vanderbilt UniversityInventors: Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
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Patent number: 8859534Abstract: The present invention relates to compounds of formula (I), wherein R1 is heteroaryl or heterocyclyl, optionally substituted; R2 is C1-4alkyl, heterocyclyl, C1-4alkylaryl, C1-4alkylheteroaryl, carbocyclyl, C1-4alkylheterocyclyl, heterocyclyl-heteroaryl, aryl-heterocyclyl, carbocyclyl-heteroaryl, heterocyclyl-aryl, optionally substituted; R3 is hydrogen or C1-4alkyl, or R2 and R3 may together with the nitrogen atom, form a saturated ring system containing 4, 5 or 6 ring forming atoms, and optionally substituted; R4 is hydrogen, halogen, methyl or methoxy; to pharmaceutical composition containing said compounds and to the use of said compounds in therapy, for instance in treating cognitive disorders. The present invention further relates to new intermediates useful in the preparation thereof.Type: GrantFiled: February 4, 2013Date of Patent: October 14, 2014Assignee: Acturum Life Science ABInventors: Johan Andersson, Helena Gyback, Anh Johansson, Christian Erik Linde, Jonas Malmstrom, Gunnar Nordvall, Tatjana Weigelt, Gitte Terp
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Publication number: 20140303185Abstract: The present invention relates to novel crystalline polymorphic forms of Vilazodone hydrochloride of formula (I). This present invention further provides the process for the preparation of novel polymorphic forms of Vilazodone hydrochloride.Type: ApplicationFiled: April 9, 2014Publication date: October 9, 2014Inventors: Buchi Reddy REGURI, Venkateshwar Goud THIRUMANI, Srinivasa Rao MANNAVA, Suresh DEVINENI
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Publication number: 20140303138Abstract: The present invention relates to novel substituted oxindole derivatives of the formula (I), pharmaceutical agents containing said derivatives, and the use thereof for the treatment of vasopressin-dependent illnesses.Type: ApplicationFiled: December 3, 2013Publication date: October 9, 2014Inventors: Wilfried Braje, Astrid Netz, Thorsten Oost, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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Patent number: 8841299Abstract: There are provided compounds of the formula wherein R1 and R2 are as described herein. The compounds are useful as anticancer agents.Type: GrantFiled: June 19, 2013Date of Patent: September 23, 2014Assignee: Genentech, Inc.Inventors: Johannes Hermann, Ann Catherine Petersen, Jutta Wanner, Lin Yi
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Patent number: 8841324Abstract: Compounds of the formula (I), in which Het, R, X, Y, R1 and p have the meanings indicated in claim 1, are autotaxin inhibitors and can be employed for the treatment of tumors.Type: GrantFiled: March 3, 2010Date of Patent: September 23, 2014Assignee: Merck Patent GmbHInventors: Wolfgang Staehle, Kai Schiemann, Melanie Schultz
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Publication number: 20140275076Abstract: Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, R1 is optionally substituted heteroaryl etc.; R2 is hydrogen etc.; R3 and R4 are each independently hydrogen etc., R5 is the following group: (wherein Y is optionally substituted five membered heteroaryl etc., R9a is optionally substituted aryl etc., R9b and R9c are each dependently hydrogen etc., and m is the integral 0 etc.) etc.; R6 is hydrogen etc.; and R7 is hydrogen etc.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Katsunori Tsuboi, Yosuke Takanashi, Shingo Tojo, Tomohiro Kodama, Katsumi Kubota, Toshio Kanai
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Publication number: 20140275033Abstract: The invention provides novel inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, and methods of making such compounds and compositions.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Chiang Jia Li, Ji-Feng Liu, Wei Li, Amanda Gibeau, Harry Rogoff