Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/393)
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Patent number: 11607423Abstract: The present invention in the field of cancer therapeutics is based on the finding (illustrated in FIG. 4) that when cannabinoids are administered to cancer cells after a chemotherapeutic agent has been administered, the combined treatment leads to lower cancer cell viability than administration of the chemotherapeutic agent alone. There is provided a pharmaceutical composition comprising a chemotherapeutic agent for use in the treatment of breast cancer, wherein said treatment comprises a first phase in which the chemotherapeutic agent is administered, and a subsequent second phase in which a cannabinoid is administered.Type: GrantFiled: April 4, 2019Date of Patent: March 21, 2023Assignee: Akos Biosciences, Inc.Inventors: Angus Dalgleish, Wai Liu, Nadine Hall
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Patent number: 11576846Abstract: A dispersion stabiliser precursor composition including one or more of cucurbituril, a variant or a derivative thereof, and one or more oil-in-water macromolecular amphiphilic emulsifier, wherein the composition is in the form of a free flowing powder; and an oil-in-water emulsion composition including one or more of cucurbituril, a variant or a derivative thereof, and one or more oil-in-water macromolecular amphiphilic emulsifier.Type: GrantFiled: March 22, 2019Date of Patent: February 14, 2023Assignee: AQDOT LIMITEDInventors: Benjamin Cheesman, Roger Coulston, Andrew Howe, Jennifer Efua Kwansima Quansah, Michael Pedder
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Patent number: 11490622Abstract: The present invention provides a compound substituted with an excellent control effect against a harmful arthropod, which is represented by formula (I) Het-Q??(I) wherein Q represents a group represented by Q1, etc., Het represents a group represented by Het1, etc., R2 represents a C1-C6 alkyl group, etc., G1 represents a nitrogen atom or CR3a, G2 represents a nitrogen atom or CR3b, G3 represents a nitrogen atom or CR3c, G4 represents a nitrogen atom or CR3d, R3a, R3b, R3c, and R3d are identical to or different from each other and represent a C1-C6 chain hydrocarbon group, etc., n represents 0, 1, or 2, T represents a C1-C10 chain hydrocarbon group substituted with one or more halogen atoms, etc., A2 represents a nitrogen atom or CR4a, A3 represents a nitrogen atom or CR4b, R4a and R4b are identical to or different from each other and represent a C1-C6 chain hydrocarbon group, W1 represents an oxygen atom, etc., and R6 represents a C1-C6 chain hydrocarbon group, etc.Type: GrantFiled: December 21, 2018Date of Patent: November 8, 2022Assignee: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Kohei Orimoto, Yuji Nakajima, Risa Kono, Ryota Maehata, Masayuki Tashiro
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Patent number: 11479554Abstract: A pharmaceutical composition is provided which includes perillyl alcohol conjugated with a therapeutic agent and further includes and a hydrolyzable acylated aliphatic tail. A method of using the pharmaceutical composition is also provided for treating a condition or disease of a patient, e.g., cancer.Type: GrantFiled: May 18, 2020Date of Patent: October 25, 2022Assignee: NeOnc Technologies, Inc.Inventors: Thomas Chen, Daniel Levin, Satish Puppali
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Patent number: 11450812Abstract: The present invention relates to compounds of formula a process for their production and their use in electronic devices, especially electroluminescent devices. When used as host material for phasphorescent emitters in electroluminescent devices, the compounds of formula I may provide improved efficiency, stability, manufacturability, or spectral characteristics of electroluminescent devices.Type: GrantFiled: May 17, 2019Date of Patent: September 20, 2022Assignee: UDC IRELAND LIMITEDInventors: Thomas Schaefer, Teresa Marina Figueira Duarte, Christian Schildknecht, Nicolle Langer, Ute Heinemeyer, Heinz Wolleb, Soichi Watanabe, Christian Lennartz, Gerhard Wagenblast, Annemarie Wolleb, Kristina Bardon, Flavio Luiz Benedito
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Patent number: 11345708Abstract: The present invention relates to compounds of formula I wherein L is a bond, a triple bond, —C(O)NH— or —NHC(O)—; R1 is phenyl or a five or six-membered heteroaryl group, optionally substituted by lower alkyl, lower alkyl substituted by halogen or lower alkoxy substituted by halogen; R2 is fluoro; R3 is fluoro or chloro; R4 is hydrogen, lower alkyl, halogen, lower alkyl substituted by hydroxy, S(O)2CH3, or is a five or six-membered heteroaryl group or a heterocycloalkyl group, which are optionally substituted by lower alkyl, hydroxy or ?O; R5 and R6 are both methyl and the dotted line is a bond, or R5 and R6 are both methyl and the dotted line is nothing, or one of R5 and R6 is hydrogen and the other is methyl, and the dotted line is nothing; or to a pharmaceutically acceptable salt or acid addition salt, to all possible tautomeric forms, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.Type: GrantFiled: February 13, 2020Date of Patent: May 31, 2022Assignee: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Fionn O'Hara, Eric Vieira
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Patent number: 11306361Abstract: The invention relates to a method for the prognosis a person's susceptibility to environmental stress. The method includes: a step of determining the sequence for initiating the translation of at least one of the genes from the CCND family, and a step of quantifying the expression of the protein encoded by said gene, the translation initiation sequence of which was sequenced in the previous step, and comparing said expression with the expression level of said protein from a reference sample.Type: GrantFiled: July 18, 2016Date of Patent: April 19, 2022Inventor: Frederic Bienvenu
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Patent number: 10995094Abstract: A temozolomide compound according to formula (I) is described, wherein R1, L1, and X are defined herein. The temozolomide compound can be used to prepare polymers comprising temozolomide. Additionally, the polymers comprising temozolomide can be particularly useful in the treatment of certain diseases.Type: GrantFiled: January 7, 2020Date of Patent: May 4, 2021Assignee: THE UNIVERSITY OF MASSACHUSETTSInventors: Todd Emrick, Matthew Skinner, Sarah M. Ward, Banishree Saha
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Patent number: 10889571Abstract: Provided herein are compounds of formula (I) or formula (Ia) that inhibit tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and/or symptomology of the disease.Type: GrantFiled: September 17, 2019Date of Patent: January 12, 2021Assignee: Terns, Inc.Inventors: F. Anthony Romero, Thorsten A. Kirschberg, Randall Halcomb, Yingzi Xu
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Patent number: 10800780Abstract: Presently provided are inhibitors of cellularly expressed TDO2 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.Type: GrantFiled: December 23, 2016Date of Patent: October 13, 2020Assignees: Genentech, Inc., NewLink Genetics CorporationInventors: Xingyu Lin, Po-wai Yuen, Rohan Mendonca, Brendan Parr, Richard Pastor, Zhonghua Pei, Lewis Gazzard, Firoz Jaipuri, Sanjeev Kumar, Xiaokai Li, Roheeth Pavana, Hima Potturi, Venkata Velvadapu, Jesse Waldo, Zuhui Zhang, Guosheng Wu, Benjamin Douglas Sellers
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Patent number: 10696680Abstract: A pharmaceutical composition is provided which includes perillyl alcohol conjugated with a therapeutic agent and further includes and a hydrolyzable acylated aliphatic tail. A method of using the pharmaceutical composition is also provided for treating a condition or disease of a patient, e.g., cancer.Type: GrantFiled: September 10, 2018Date of Patent: June 30, 2020Assignee: NeOnc Technologies, Inc.Inventors: Thomas Chen, Daniel Levin, Satish Puppali
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Patent number: 9931325Abstract: The present invention provides new methods and kits for treating IBS; treating IBS in females; treating IBS in older subjects; and treating IBS in non-white subjects.Type: GrantFiled: January 4, 2017Date of Patent: April 3, 2018Assignee: Salix Pharmaceuticals, Ltd.Inventors: William Forbes, Enoch Bortey
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Patent number: 9890166Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: May 26, 2014Date of Patent: February 13, 2018Assignee: NOVARTIS AGInventors: Jutta Blank, Guido Bold, Simona Cotesta, Vito Guagnano, Heinrich Rueeger, Andrea Vaupel
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Patent number: 9809558Abstract: Compounds useful for affinity chromatography as presented, more particularly for use in affinity chromatography to purify serum albumin, especially human serum albumin (HSA) and fusion proteins thereof. Methods for extending the half-life of therapeutic agents are also presented, particularly therapeutic peptide agents and small molecules, such as by conjugation of compounds described herein to the therapeutic peptide or small molecule, which upon administration, binds to HSA, thereby providing a prolonged release of the therapeutic agent.Type: GrantFiled: October 1, 2014Date of Patent: November 7, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Peter Kumpalume, Oliver Schon, Christine Patricia Donahue, Ghotas Evindar, David I. Israel, David Paolella, Letian Kuai, Ninad V. Prabhu
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Patent number: 9765088Abstract: The present invention relates to an improved and industrially advantageous process for the preparation of Rifaximin with high purity and yield. Particularly, the present invention relates to improved processes for the preparation of Rifaximin from Rifamycin O and S. More particularly the present invention relates to a process for the preparation of Rifaximin through 3-halorifamycin S. The present invention further relates to a novel polymorph of Rifaximin and process for its preparation.Type: GrantFiled: April 19, 2015Date of Patent: September 19, 2017Assignee: GRANULES INDIA LIMITEDInventors: Prasada Raju Vetukuri Vnkv, Goverdhan Gilla, Ambaiah Boini, Krishna Prasad Chigurupati
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Patent number: 9765081Abstract: A pharmaceutical composition is provided which includes perillyl alcohol conjugated with a therapeutic agent and further includes and a hydrolyzable acylated aliphatic tail. A method of using the pharmaceutical composition is also provided for treating a condition or disease of a patient, e.g., cancer.Type: GrantFiled: March 17, 2017Date of Patent: September 19, 2017Assignee: NeOnc Technologies, Inc.Inventors: Thomas Chen, Daniel Levin, Satish Puppali
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Patent number: 9725425Abstract: Provided are small molecule inhibitors of ubiquitin specific protease 2, 8 and 12 (USP2 and USP8 and USP12) activity and methods for their use in treating cancers. The small molecule inhibitors of the invention are particularly useful in the treatment of non-small cell lung cancers that are resistant to tyrosine kinase inhibitors and in the treatment of prostate cancer that is resistant to AR inhibitor therapy.Type: GrantFiled: February 25, 2015Date of Patent: August 8, 2017Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Alan D. D'Andrea, Nathanael Gray, Sara Jean Buhrlage, Kalindi Parmar
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Patent number: 9657026Abstract: A pharmaceutical composition is provided which includes perillyl alcohol conjugated with a therapeutic agent and further includes and a hydrolyzable acylated aliphatic tail. A method of using the pharmaceutical composition is also provided for treating a condition or disease of a patient, e.g., cancer.Type: GrantFiled: June 24, 2016Date of Patent: May 23, 2017Assignee: NeOnc Technologies Inc.Inventors: Thomas Chen, Daniel Levin, Satish Pupalli
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Patent number: 9624219Abstract: The present invention relates to a compound of Formula (I) having pharmacological activity, processes for its preparation, pharmaceutical compositions and their use in the treatment of certain parasitic certain parasitic protozoal infections such as malaria, in particular infection by Plasmodium falciparum. (S)—N-(2-fluoropyridin-4-yl)-3-methyl-2-(5-methyl-2,4-dioxo-1,2-dihydropyrido[3,4-d]pyrimidin-3(4H)-yl)butanamide.Type: GrantFiled: April 19, 2016Date of Patent: April 18, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Jose-Miguel Coteron Lopez, Esther Pilar Fernandez Velando, Jorge Fernandez-Molina, Maria Luisa Leon-Diaz, David Matthew Wilson
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Patent number: 9556188Abstract: The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.Type: GrantFiled: November 25, 2015Date of Patent: January 31, 2017Assignee: BeiGene, Ltd.Inventors: Zhiwei Wang, Yunhang Guo
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Patent number: 9504674Abstract: Compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering a 7,8-dihydroxyflavone derivative with modified flavone or heterocyclic ring to a subject in need thereof. Methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided.Type: GrantFiled: March 5, 2015Date of Patent: November 29, 2016Assignee: Emory UniversityInventor: Keqiang Ye
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Patent number: 9388159Abstract: This invention provides for compounds of the Formula II: wherein A, B, Het, R1, R2 and R3 are as described herein. These compounds are androgen receptor modulators useful for the treatment of androgen receptor-associated conditions.Type: GrantFiled: June 27, 2014Date of Patent: July 12, 2016Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Michael E. Jung, Charles L. Sawyers, Samedy Ouk, Chris Tran, John Wongvipat
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Patent number: 9284281Abstract: Disclosed are naphtho[2,3-f]quinoxaline compounds and pharmaceutical composition thereof. The compounds of the invention have been demonstrated as having analgesic effects and therefore may be applicable for use as a novel agent in relieving acute or chronic pain.Type: GrantFiled: September 16, 2014Date of Patent: March 15, 2016Assignee: NATIONAL CENTRAL UNIVERSITYInventors: Wei-Hsin Sun, Shir-Ly Huang, Hsu-Shan Hunag
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Patent number: 9050246Abstract: The present invention concerns an injectable composition comprising a filler or a botulinum toxin and an adrenergic receptor agonist, and its use for diminishing, decreasing or avoiding skin reactions due to injection, specially redness, ecchymosis, bruising, bleeding, erythema, oedema, necrosis, ulceration, swelling and/or inflammation.Type: GrantFiled: May 28, 2010Date of Patent: June 9, 2015Assignee: Galderma Research & DevelopmentInventors: Isabelle Bertholon, Florence Brunel, Benjamin Herbage, Sylviane Villard
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Publication number: 20150148391Abstract: The present invention relates to stabilized pharmaceutical formulations prepared from solutions comprising an antineoplastic compound having a cyclic or non-cyclic hydrazine, triazine, or tetrazine group, or a pharmaceutically acceptable salt thereof, and a stabilizer, wherein the stabilizer is an antioxidant and/or more susceptible to nucleophilic attack than the antineoplastic compound.Type: ApplicationFiled: February 3, 2015Publication date: May 28, 2015Inventors: Mahmoud S. AlSwisi, Mahmoud A.A. Ghannam
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Publication number: 20150148390Abstract: The present invention relates to glioblastoma inhibiting compounds, in particular gambogic acid amid and derivatives thereof for the treatment of glioblastoma. Moreover, methods for determining whether a treatment with the compounds of the invention is suitable for a patient are disclosed.Type: ApplicationFiled: June 15, 2012Publication date: May 28, 2015Applicant: Life & Brain GmbHInventors: Björn Scheffler, Martin Glas, Matthias Simon, Sabine Gogolok, Daniel Trageser, Roman Reinartz, Anja Wieland
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Publication number: 20150141418Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.Type: ApplicationFiled: January 26, 2015Publication date: May 21, 2015Applicant: PTC Therapeutics, Inc.Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
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Publication number: 20150133366Abstract: C. difficile infection (CDI) is the most common cause of antibiotic-associated diarrhea. Unfortunately, antibiotic therapy remains as the standard treatment for this antibiotic-induced disease and relapses are common. Antibiotic treatment typically is given for 10 to 14 days for initial or second episode of CDI. For recurrent episodes, more prolonged courses are recommended. It is disclosed herein that lower dose or shorter course of the antimicrobial treatment is sufficient to treat the disease and prevent recurrent disease by enabling a good immunologic response to infection, and perhaps also by better preserving normal flora, thus protecting against relapses or reinfection.Type: ApplicationFiled: November 12, 2014Publication date: May 14, 2015Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Richard L. Guerrant, Cirle Alcantara Warren, John Hudson Moore, II, Edward van Opstal
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Patent number: 9029561Abstract: Compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering a 7,8-dihydroxyflavone derivative with modified flavone or heterocyclic ring to a subject in need thereof. Methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided.Type: GrantFiled: June 8, 2011Date of Patent: May 12, 2015Assignee: Emory UniversityInventor: Keqiang Ye
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Publication number: 20150111907Abstract: The invention relates to methods of predicting the clinical outcome of brain cancer patients based on the LOH levels of the PTEN gene and on the expression levels or the polysomy/amplification levels of EGFR gene in a sample from said patients.Type: ApplicationFiled: December 23, 2014Publication date: April 23, 2015Inventors: Michael J. DONOVAN, Anna Colomer Valero, Nadina Erill Sagales, Isidre Ferrer Abinzanda, Susana Boluda Casas
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Patent number: 9005670Abstract: The present invention provides methods for treating cancer comprising inhibiting the activity of p300/CBP histone acetyltransferase (HAT). Also provided are p300/CBP HAT inhibitors for treating a subject having cancer. In addition, the present invention includes biomarkers for p300/CBP HAT inhibition, which are used to i) monitor the effectiveness of cancer therapy, and ii) identify anti-cancer agents for use in combination therapy.Type: GrantFiled: January 5, 2011Date of Patent: April 14, 2015Assignee: The Johns Hopkins UniversityInventors: Rhoda Myra Alani, Philip A. Cole, Gai Yan, Erin M. Bowers
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Patent number: 9006258Abstract: The present invention relates to a new use for compounds that inhibit phosphodiesterase 1 (PDE1), e.g., that inhibit PDE1-mediated suppression of the dopamine D1 receptor and/or progesterone signaling pathways, including, e.g., methods of treatment or prophylaxis for conditions which may be ameliorated by enhancing the progesterone signaling response, particularly female sexual dysfunction.Type: GrantFiled: December 5, 2007Date of Patent: April 14, 2015Assignee: Intra-Cellular Therapies, Inc.Inventors: Allen A. Fienberg, Sharon Mates, Lawrence P. Wennogle
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Patent number: 8993607Abstract: The invention provides compounds of formula I, II, and III as defined herein, as well as salts thereof. The compounds may have activity as anti-proliferative agents.Type: GrantFiled: August 1, 2008Date of Patent: March 31, 2015Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Joseph E. Rice
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Patent number: 8980920Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56.Type: GrantFiled: May 28, 2010Date of Patent: March 17, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
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Publication number: 20150064252Abstract: Disclosed are solid dispersions comprising a compound having the formula: wherein the compound is dispersed within a polymer matrix formed by a pharmaceutically acceptable polymer, and further wherein the compound is substantially amorphous. Also disclosed are pharmaceutical compositions comprising the compound and methods of use for the compound.Type: ApplicationFiled: January 30, 2014Publication date: March 5, 2015Inventors: Eric Gorman, Erik Mogalian, Reza Oliyai, Dimitrios Stefanidis, Vahid Zia
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Patent number: 8969372Abstract: Therapeutically effective 2,4,5-trisubstituted imidazole compounds are provided. Also provided are methods of preparing the compounds and pharmaceutical compositions comprising the compounds alone or in combination with other agents.Type: GrantFiled: November 15, 2004Date of Patent: March 3, 2015Assignee: Aptose Boisciences Inc.Inventors: Mario Huesca, Raed Al-Qawasmeh, Aiping H. Young, Yoon Lee
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Publication number: 20150051257Abstract: Sulphonamide derivatives of benzylamine of formula (I), wherein A represents phenyl unsubstituted or substituted; or 9- or 10-membered bicyclic group, linked to —(O)x—(CH2)y— through one of its aromatic carbon atoms, consisting of benzene ring fused with -membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from the group consisting of N and O, wherein such bicyclic group is unsubstituted or substituted or with 5- or 6-membered non-aromatic heterocyclic ring having 1 or 2 O atoms, wherein heterocyclic ring is unsubstituted or substituted with one or more C1-C3-alkyls; D represents a group selected from: phenyl unsubstituted or substituted; naphthyl unsubstituted or substituted; thiophene unsubstituted or substituted; bicyclic group consisting of imidazolering fused with 5-membered non-aromatic carbocyclic ring; bicyclic group consisting of benzene ring fused with 5-membered heteroaromatic ring, having 1 or 2 heteroatoms independently selected from the group consisting of N, O andType: ApplicationFiled: March 20, 2013Publication date: February 19, 2015Applicant: ADAMED SP. ZO.OInventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Tomasz Lysakowski, Maciej Pawlowski
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Publication number: 20150038501Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: October 20, 2014Publication date: February 5, 2015Inventors: Leping LI, Min ZHONG
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Patent number: 8946274Abstract: Methods of improving skin quality are disclosed. Generally, the methods include topically administering an IRM compound to a treatment area of skin for a period of time and in an amount effective for improving the quality of the skin. Suitable IRM compound compounds include agonists of one or more TLRs.Type: GrantFiled: September 10, 2012Date of Patent: February 3, 2015Assignee: Medicis Pharmaceutical CorporationInventors: Richard L. Miller, James H. Lee, Mary L. Owens
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Publication number: 20150030579Abstract: Hydroxytyrosol or olive juice containing hydroxytyrosol in combination with at least one of the compounds selected from the group consisting of: creatine, coenzyme Q10, resveratrol, caffeine, carnitine, B vitamins (B1, B2, B3, B5, B6, and/or B12) and ginseng (preferably: root) extract. can be used to maintain or increase mitochondrial biogenesis in cardiac muscle, skeletal muscles, and liver tissue.Type: ApplicationFiled: August 1, 2014Publication date: January 29, 2015Applicant: DSM IP ASSETS B.V.Inventors: Ann FOWLER, Angelika FRIEDEL, Darko KNUTTI, Karin KURATLI, Daniel RAEDERSTORFF, Ying WANG-SCHMIDT, Karin WERTZ
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Publication number: 20150005288Abstract: The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: January 22, 2013Publication date: January 1, 2015Applicants: Bayer Pharma Aktiengesellschaft, Bayer Intellectual Property GmbHInventors: Frank Süssmeier, Mario Lobell, Sylvia Grünewald, Michael Härter, Bernd Buchmann, Joachim Telser, Hannah Jörissen, Melanie Heroult, Antje Kahnert, Klemens Lustig, Niels Lindner
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Publication number: 20140371235Abstract: A method for treating prostate cancer in a subject, comprising administering a therapeutically effective amount of at least one agent to the subject, wherein the agent is selected from: (a) a phenyl-substituted imidazole, or a pharmaceutically acceptable salt or ester thereof; or (b) a compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: wherein R20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; R21 is an alkanediyl or a substituted alkanediyl; a is 0 or 1; c is 0 or 1; X is C or S; R22 is a moiety that includes at least one divalent amino radical; and R23 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containingType: ApplicationFiled: October 10, 2012Publication date: December 18, 2014Applicant: University of Pittsburgh - Of the Commonweath System of Higher EducationInventors: Zhou Wang, Joel Byron Nelson, Minh Mindy Bao Nguyen, John S. Lazo, Paul A. Johnston, Peter Wipf
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Publication number: 20140364470Abstract: The invention relates to a phosphate salt or a nitrate salt of 4-(R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl-3-fluoro-benzonitrile, especially in crystalline form, and specific forms of these salts, as well as related invention embodiments. The salts and salt forms allow for the prophylactic and/or therapeutic treatment of aldosterone synthase and/or aromatase mediated diseases or disorders.Type: ApplicationFiled: January 15, 2013Publication date: December 11, 2014Applicant: Novartis AGInventors: Paul Alan Sutton, Eric Loeser
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Publication number: 20140364472Abstract: The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene (or sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.Type: ApplicationFiled: August 8, 2014Publication date: December 11, 2014Inventors: Thomas Chen, Daniel Levin, Satish Pupalli
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Publication number: 20140364471Abstract: The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene for sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.Type: ApplicationFiled: August 8, 2014Publication date: December 11, 2014Inventors: Thomas Chen, Daniel Levin, Satish Pupalli
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Publication number: 20140357621Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.Type: ApplicationFiled: August 14, 2014Publication date: December 4, 2014Applicant: Novartis AGInventors: Gary Michael Ksander, Erik Meredith, Lauren Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
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Patent number: 8895599Abstract: The present invention provides pharmaceutical compositions containing benzene compound(s) represented by General Formula (1) below and, particularly, LPL-activating compositions for use in hyperlipidemia therapeutic and preventive agents, anti-obesity agents, and the like: wherein R1, R2, R3 and R4 are as defined in the specification.Type: GrantFiled: June 28, 2013Date of Patent: November 25, 2014Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Irina Neagu, Michael Ohlmeyer, Vidyadhar M. Paradkar, Kurt W. Saionz, Koushi Iwata, Takashi Okamura, Tadao Shibutani
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Patent number: 8895597Abstract: The additive effect of combined intracranial carmustine (“BCNU”) with intracranial temozolomide (“TMZ”), and particularly in combination with radiation (“XRT”), in the treatment of two rat intracranial glioma models, the 9L gliosarcoma and the F98 glioma, demonstrates that local delivery of both drugs, especially in combination with radiation, is far more effective than delivery of either drug alone or one systemically and one locally, either with or without radiation. The triple therapy showed a significant improvement in survival when compared to controls (p=0.0004), local BCNU (p=0.0043), oral TMZ (p=0.0026), local TMZ (p=0.0105), and the combinations of either BCNU and XRT (p=0.0378) or oral TMZ and local BCNU (p=0.0154).Type: GrantFiled: June 17, 2011Date of Patent: November 25, 2014Inventors: Violette Renard Recinos, Betty Tyler, Sarah Brem Sunshine, Henry Brem
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Publication number: 20140343045Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: ApplicationFiled: May 23, 2014Publication date: November 20, 2014Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
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Patent number: 8883826Abstract: The present invention relates to novel compounds of formula I wherein W, n, X and W? are defined in the description; invention compounds are modulators of metabotropic glutamate receptors—subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.Type: GrantFiled: December 20, 2011Date of Patent: November 11, 2014Assignee: Addex Pharma SAInventors: Anne-Sophie Bessis, Christelle Bolea, Beatrice Bonnet, Mark Epping-Jordan, Nicolas Poirier, Sonia-Maria Poli, Jean-Philippe Rocher, Yves Thollon