Ring Nitrogen In The Polycyclo Ring System Patents (Class 514/323)
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Patent number: 9637471Abstract: The present invention relates to hydroxyindalpine derivatives of formula (I) as defined herein and pharmaceutical compositions comprising these compounds, as well as their medical use, particularly in the treatment or prevention of gastrointestinal diseases/disorders, such as constipation and functional dyspepsia.Type: GrantFiled: February 14, 2014Date of Patent: May 2, 2017Assignee: Technische Universitat MunchenInventors: Arne Skerra, Michael Muller, Michael Schemann, Thomas Berger
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Patent number: 9498472Abstract: Methods of treating, preventing or managing leukemias are disclosed. The methods encompass the administration of an immunomodulatory compound of the invention known as Revlimid® or lenalidomide. The invention further relates to methods of treatment using this compound with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods of the invention are also disclosed.Type: GrantFiled: June 3, 2015Date of Patent: November 22, 2016Assignee: Celgene CorporationInventor: Jerome B. Zeldis
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Patent number: 9458130Abstract: The disclosure provides a novel polymorph of Compound (I): 2-((1-(2-(4-Fluorophenyl)-2-oxoethyl)piperidin-4-yl)methyl)isoindolin-1-one monohydrochloride dihydrate, i.e., Form (A) of Compound (I).HCl.2H2O. Pharmaceutical compositions comprising Form (A) of Compound (I).HCl.2H2O and related methods of treatment are also disclosed.Type: GrantFiled: November 30, 2015Date of Patent: October 4, 2016Assignee: Minerva Neurosciences, Inc.Inventor: Remy Luthringer
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Patent number: 9458155Abstract: This disclosure is directed to pyrido[4,3-b]indoles having rigid moieties. The compounds in one embodiment are pyrido[4,3-b]indoles having an unsaturated hydrocarbon moiety. The compounds in another embodiment are pyrido[4,3-b]indoles having a cycloalkyl, cycloalkenyl or heterocyclyl moiety. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: GrantFiled: November 3, 2014Date of Patent: October 4, 2016Assignee: MEDIVATION TECHNOLOGIES, INCInventors: David T. Hung, Andrew A. Protter, Rajendra Parasmal Jain, Sarvajit Chakravarty
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Patent number: 9447070Abstract: This invention relates to 5-substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: GrantFiled: September 18, 2014Date of Patent: September 20, 2016Assignee: Celgene CorporationInventors: George W. Muller, Roger Shen-Chu Chen, Alexander L. Ruchelman
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Patent number: 9403867Abstract: The present invention relates to particulate forms of anamorelin monohydrochloride or a composition comprising anamorelin monohydrochloride having controlled chloride content, preferably isolated in an amorphous and/or fine particulate state, processes for making the particulate forms, and pharmaceutical compositions comprising the particulate forms.Type: GrantFiled: November 12, 2014Date of Patent: August 2, 2016Assignees: Ono Pharmaceuticals Co., Ltd., Helsinn Healthcare SAInventors: Shin-Itsu Kuwabe, Takehiko Yanagimachi, Hideyuki Yoshiyama, Seemon Pines, Eleanor De Groot, Silvina Garcia Rubio, Peter Manini
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Patent number: 9393255Abstract: The present disclosure provides pharmaceutical compositions comprising cytidine analogs for parenteral administration. Also provided are methods of preparing the compositions and methods of treating diseases and disorders using the compositions provided herein.Type: GrantFiled: January 31, 2012Date of Patent: July 19, 2016Assignee: Celgene CorporationInventors: Anthony Tutino, Mei Lai, Jeffrey B. Etter
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Patent number: 9382227Abstract: Described herein are enhanced N-methyl-D-aspartate (NMDA) receptor antagonists, pharmaceutical compositions thereof, and their methods of use and treatment, e.g., of Formula (I): wherein one or more of R1, R2, R3, R4, R5, or the ring formed by the joining of R1 and R2, is a hydrophobic moiety which confers enhanced antagonist activity as compared to existing NMDA receptor antagonists, e.g., ifenprodil. Compounds described herein are designed based on the discovery that ifenprodil binds within the allosteric domain of the GluN1/GluN2B NMDA receptor, particularly at the interface between GluN1 and GluN2B subunits. In silico methods are further described herein.Type: GrantFiled: January 2, 2014Date of Patent: July 5, 2016Assignee: Cold Spring Harbor LaboratoryInventors: Hiro Furukawa, Erkan Karakas
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Patent number: 9371309Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.Type: GrantFiled: September 22, 2011Date of Patent: June 21, 2016Assignee: Celgene CorporationInventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller
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Patent number: 9365538Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.Type: GrantFiled: January 14, 2009Date of Patent: June 14, 2016Assignee: Celgene CorporationInventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller
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Patent number: 9353080Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.Type: GrantFiled: September 22, 2011Date of Patent: May 31, 2016Assignee: Celgene CorporationInventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller
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Patent number: 9284299Abstract: In one aspect, the invention relates to substituted 1H-benzo[d][1,2,3]triazol-1-ol analgoues, derivatives thereof, and related compound; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders, e.g. various tumors and cancers, associated with ?-catenin/Tcf protein-protein interaction dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: February 10, 2013Date of Patent: March 15, 2016Assignee: University of Utah Research FoundationInventors: Haitao Ji, Binxun Yu, Min Zhang, Wenxing Guo
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Patent number: 9283215Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: GrantFiled: March 7, 2014Date of Patent: March 15, 2016Assignee: Celgene CorporationInventor: Jerome B. Zeldis
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Patent number: 9206156Abstract: Substituted indole derivatives, processes for the preparation thereof, medicinal products and pharmaceutical compositions containing these compounds and the use of substituted indole derivatives to treat pain and other conditions and for other medical purposes.Type: GrantFiled: December 11, 2012Date of Patent: December 8, 2015Assignee: GRÜNENTHAL GMBHInventors: Stefan Schunk, Stefan Oberbörsch, Werner Englberger, Bernd Sundermann
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Patent number: 9192662Abstract: Provided herein are methods of treating, preventing or managing disorders associated with low CD59 levels. The methods encompass the administration of an immunomodulatory compound provided herein, such as 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione or 1,3-dioxo-2-(2,6-dioxopiperidin-3-yl)-4-aminoisoindoline. Further described are methods of treatment using the immunomodulatory compounds in combination with other therapeutic agents or therapies. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods provided herein are also disclosed.Type: GrantFiled: January 29, 2009Date of Patent: November 24, 2015Assignee: Celgene CorporationInventors: Helen A. Brady, Kyle Chan
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Patent number: 9181216Abstract: Provided are 4?-O substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: GrantFiled: November 18, 2013Date of Patent: November 10, 2015Assignee: Celgene CorporationInventors: Alexander L. Ruchelman, George W. Muller, Hon-Wah Man, Roger Shen-Chu Chen
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Patent number: 9139555Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.Type: GrantFiled: January 14, 2009Date of Patent: September 22, 2015Assignee: Celgene CorporationInventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller
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Patent number: 9139556Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.Type: GrantFiled: September 22, 2011Date of Patent: September 22, 2015Assignee: Celgene CorporationInventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller, Manohar T. Saindane, Louise M. Cameron
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Patent number: 9108945Abstract: Anhydrous polymorphic form-I of anti cancer drug, Lenalidomide whose chemical name is 3-(4-amino-1-oxo-1,3-dihydro-isoindole-2-yl)-piperidine-2,6-dione, is disclosed. Alternate methods for making anhydrous polymorphic form-I of Lenalidomide are also disclosed.Type: GrantFiled: January 9, 2014Date of Patent: August 18, 2015Assignee: Natco Pharma LimitedInventors: Durga Prasad Konakanchi, Buchappa Gongalla, Kotayya Babu Sikha, Chandrasekar Kandaswamy, Kali Satya Bhujanga Rao Adibhatla, Venkaiah Chowdary Nannapaneni
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Patent number: 9101622Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: GrantFiled: September 10, 2014Date of Patent: August 11, 2015Assignee: Celgene CorporationInventor: Jerome B. Zeldis
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Patent number: 9090585Abstract: The present application describes 2-(2?,6?-dioxo-3?-deutero-piperidin-3?-yl)isoindoles, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: GrantFiled: March 28, 2012Date of Patent: July 28, 2015Assignee: DeuteRx, LLCInventor: Sheila DeWitt
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Patent number: 9085530Abstract: The present invention discloses methods for synthesizing 3-(substituted dihydroisoindolinone-2-yl)-2,6-dioxopiperidine and intermediates thereof, namely, the synthesis of compounds of the Formula (I), with each substitutional group defined in the patent specification. Owing to the advantages of high productivity, little influence to the environment and material accessibility, the methods of the present invention is suitable for industrial production.Type: GrantFiled: June 1, 2010Date of Patent: July 21, 2015Assignees: Nanjing Cavendish Bio-Engineering Technology Co., Ltd.Inventors: Rong Yan, Hao Yang, Yongxiang Xu
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Patent number: 9085551Abstract: Solid forms comprising crystalline 3-(4-nitro-1-oxoisoindolin-2-yl)piperidine-2,6-dione are disclosed. Compositions comprising the solid forms, methods of making the solid forms and methods of their use are also disclosed.Type: GrantFiled: February 20, 2013Date of Patent: July 21, 2015Assignee: Celgene CorporationInventors: Ying Li, Jean Xu, Kevin J. Klopfer
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Patent number: 9084783Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein A, B and D are each oxygen or sulfur, provided that least one of A, B and D is sulfur; and R1-R8 are each independently hydrogen, hydroxyl, acyl, substituted acyl, acyloxy, substituted acyloxy, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, aryl, substituted aryl, amino, substituted amino, halogen, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, substituted heteroaryl, or a thio-containing group.Type: GrantFiled: December 15, 2014Date of Patent: July 21, 2015Assignee: THE UNITED STATES OF AMERICA, as represented by the Secretary, Department of Health and Human ServicesInventors: Nigel H. Grieg, Weiming Luo, David Tweedie, Harold W. Holloway, Qian-Sheng Yu, Edward J. Goetzl
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Patent number: 9056103Abstract: Methods of treating, preventing or managing leukemias are disclosed. The methods encompass the administration of an immunomodulatory compound of the invention known as Revlimid® or lenalidomide. The invention further relates to methods of treatment using this compound with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods of the invention are also disclosed.Type: GrantFiled: December 31, 2013Date of Patent: June 16, 2015Assignee: Celgene CorporationInventor: Jerome B. Zeldis
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Patent number: 9056120Abstract: Methods of treating, preventing and/or managing myelodysplastic syndromes are disclosed. Specific methods encompass the administrations of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidin-2,6-dione in combination with 5-azacytidine.Type: GrantFiled: March 13, 2013Date of Patent: June 16, 2015Assignee: Celgene CorporationInventor: Jerome B. Zeldis
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Patent number: 9050324Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: GrantFiled: March 25, 2014Date of Patent: June 9, 2015Assignee: Celgene CorporationInventor: Jerome B. Zeldis
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Patent number: 9045453Abstract: This invention relates to novel substituted dioxopiperidinyl phthalimide derivatives and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an immunomodulatory agent.Type: GrantFiled: May 13, 2011Date of Patent: June 2, 2015Assignee: Concert Pharmaceuticals, Inc.Inventor: Roger Tung
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Publication number: 20150139905Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.Type: ApplicationFiled: October 9, 2014Publication date: May 21, 2015Inventors: Dinesh Chimmanamada, Weiwen Ying
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Publication number: 20150133422Abstract: The present invention embodiments relate to compound of Formula I or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates in certain embodiments to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates in certain embodiments to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates in certain embodiments to a process for manufacturing compounds of Formula I.Type: ApplicationFiled: November 8, 2013Publication date: May 14, 2015Inventors: Stefano Crosignani, Sandra Cauwenberghs, Frederik Deroose
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Patent number: 9029548Abstract: The invention relates to fatty acid lenalidomide derivatives; compositions comprising an effective amount of a fatty acid lenalidomide derivative; and methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid lenalidomide derivative.Type: GrantFiled: May 4, 2012Date of Patent: May 12, 2015Assignee: Catabasis Pharmaceuticals, Inc.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu, Amal Ting
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Patent number: 9029379Abstract: Methods for treating Down syndrome and improving cognitive function of a patient with an intellectual disability are disclosed. 5-hydroxytryptamine sub-receptor six (5-HT6) receptor antagonists are provided for improving the cognition of a Down syndrome patient.Type: GrantFiled: March 15, 2013Date of Patent: May 12, 2015Assignee: The University of Utah Research FoundationInventors: Julie Ruth Korenberg, Karen Sue Wilcox, Peter Jeffrey West, Raymond Pierre Kesner
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Patent number: 9023868Abstract: The present application describes deuterium-enriched lenalidomide, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: GrantFiled: January 24, 2014Date of Patent: May 5, 2015Assignee: Deuteria Pharmaceuticals, Inc.Inventor: Anthony W. Czarnik
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Patent number: 9018231Abstract: The present invention relates to novel sulfone compounds as 5-HT6 receptor ligands of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. These compounds are useful in the treatment/prevention of various disorders that are related to 5-HT6 receptor functions.Type: GrantFiled: March 24, 2010Date of Patent: April 28, 2015Assignee: Suven Life Sciences LimitedInventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Rama Sastri Kambhampati, Rajesh Kumar Badange, Veena Reballi, Anil Kashinath Chindhe, Rambabu Namala, Mohamad Sadik Abdulhamid Mulla, Ishtiyaque Ahmad, Renny Abraham, Venkateswarlu Jasti
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Patent number: 9018200Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: GrantFiled: October 18, 2012Date of Patent: April 28, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Milana Maletic, Harold B. Wood, Wanying Sun
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Patent number: 9017735Abstract: Disclosed herein are compositions and methods for treating a psychiatric disorder or symptoms thereof in a patient. The compositions comprise a compound that modulates KCNQ (Kv7) potassium channel activity and the methods include administering an effective amount of the compound that modulates KCNQ (Kv7) potassium channel activity.Type: GrantFiled: June 3, 2010Date of Patent: April 28, 2015Assignee: Marquette UniversityInventor: Mohammadhossein Behnam Ghasemzadeh
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Publication number: 20150110713Abstract: A method for treating cancer, preventing cancer or delaying the progression of a cancer in an animal or human comprising the step of: administering to the animal or the human having a cancer a composition in an amount effective to treat cancer, prevent cancer or delay the progression of cancer in the animal or the human. The composition comprises a pharmaceutically acceptable excipient, and ascorbate which is joined to a carrier structure containing an anti-cancer active agent, said carrier structure being capable of releasing the anti-cancer agent in the presence of a reactive oxygen species.Type: ApplicationFiled: December 22, 2014Publication date: April 23, 2015Inventors: Anthony Manganaro, Karen Rockwell
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Patent number: 9006267Abstract: Pharmaceutical compositions and single unit dosage forms of thalidomide and pharmaceutically acceptable stereoisomers, prodrugs, salts, solvates, hydrates, or clathrates are disclosed. Also disclosed are methods of treating, managing, and preventing diseases and conditions such as, but not limited to, leprosy, chronic graft-vs-host disease, rheumatoid arthritis, sarcoidosis, an inflammatory condition, inflammatory bowel disease, and cancer using the novel dosage forms disclosed herein.Type: GrantFiled: March 21, 2006Date of Patent: April 14, 2015Assignee: Celgene CorporationInventors: Paul D'Angio, John McCarty
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Patent number: 9006276Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.Type: GrantFiled: September 23, 2011Date of Patent: April 14, 2015Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
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Publication number: 20150099709Abstract: The present invention relates to a use of a compound having ghrelin receptor agonistic activity, a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof for the manufacture of a medicament for treatment of diseases including achlorhydria in which abnormal gastric acid secretion is involved. In addition, the present invention relates to the method of treatment including administering to a human or animal. The compound, the pharmaceutically acceptable salt thereof, or pharmaceutical compositions containing them, may be used in combination with one or more second active agents. Further, the present invention relates to pharmaceutical compositions and kits comprising a compound of the present invention or a pharmaceutically acceptable salt thereof for the treatment of said diseases.Type: ApplicationFiled: May 27, 2013Publication date: April 9, 2015Inventors: Nobuyuki Takahashi, Masaki Sudo, Kaoru Shimada, Hiroaki Wakabayashi
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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: 9000175Abstract: The present invention relates to compounds of Formula (I) that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods of treating, preventing and/or managing diseases, disorders syndromes or conditions associated with the modulation of GPR119 receptor by using either alone or in combinations of Formula (I).Type: GrantFiled: November 24, 2011Date of Patent: April 7, 2015Assignee: Lupin LimitedInventors: Rajesh Thotapally, Onkar Gangaram Kachi, Atish Harishchandra Rodge, Ashok Bhau Pathak, Bhavana Shrirang Kardile, Milind Dattatraya Sindkhedkar, Venkata P. Palle, Rajender Kumar Kamboj
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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: 20150094336Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: ApplicationFiled: December 9, 2014Publication date: April 2, 2015Inventor: Jerome B. Zeldis
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Publication number: 20150094335Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: ApplicationFiled: December 8, 2014Publication date: April 2, 2015Inventor: Jerome B. Zeldis
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Publication number: 20150087628Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.Type: ApplicationFiled: April 10, 2013Publication date: March 26, 2015Inventors: Jonathan Ostrem, Ulf Peters, Kevan M. Shokat
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Patent number: 8987305Abstract: The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.Type: GrantFiled: February 27, 2013Date of Patent: March 24, 2015Assignee: Aptose Biosciences Inc.Inventors: Raed H. Al-Qawasmeh, Aiping H. Young, Mario Huesca, Yoon S. Lee
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Publication number: 20150065498Abstract: The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: May 11, 2012Publication date: March 5, 2015Inventors: Scott D. Kuduk, Douglas C. Beshore, Zhi-Qiang Yang, Youheng Shu, Daniel Pitts
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Patent number: 8969340Abstract: The present invention provides methods and compositions for treating chronic pelvic pain syndrome. In particular, the present invention provides methods and compositions for treating chronic pelvic pain syndrome with an agent that targets MCP-1, MIP-1?, or the CCR-2 receptor.Type: GrantFiled: July 8, 2013Date of Patent: March 3, 2015Assignee: Northwestern UniversityInventors: Anthony J. Schaeffer, David Klumpp, Praveen Thumbikat
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Patent number: RE45685Abstract: Isoindolin-1-one and Isoindoline-1,3-dione substituted in the 2-position with an ?-(3,4-disubstituted phenyl)alkyl group and in the 4- and/or 5-position with a nitrogen-containing group are inhibitors of, and thus useful in the treatment of disease states mediated by, TNF? and phosphodiesterase. A typical embodiment is 2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4,5-diaminoisoindoline-1,3-dione.Type: GrantFiled: October 4, 2013Date of Patent: September 29, 2015Assignee: Celgene CorporationInventors: Hon-Wah Man, George W. Muller