Ring Nitrogen In The Polycyclo Ring System Patents (Class 514/323)
  • Patent number: 10406147
    Abstract: This invention is directed to derivatives of piperidine-2,6-dione, or their organic or inorganic salts thereof, a methods of synthesis of these derivatives, and their application as active pharmaceutical ingredient as inhibitors of TNF? releasing in cells, the derivative of piperidine-2,6-dione being of the general formula (I): wherein n represents 1, 2, 3, 4, 5 or 6; R1 represents from one to four of the same or different substituents selected from F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, NO2, NHC(O)C1-4 alkyl, NH2, NH(C1-4 alkyl), N(C1-4 alkyl)2; R2 represents OR3, NR3R4, N(R3)COR4, O2CR5; R3 and R4 represent independently and at each occurrence H or C1-4 alkyl; R5 represents CHR6NR7R8, CHR6NR9C(O)CHR10NR7R8, a heterocycle W or CHR6NR9C(O)W; R6, R9, R10 represent independently and at each occurrence H, or C1-4 alkyl; R7 and R8 represent independently and at each occurrence H, C1-4 alkyl, or R7 and R8 taken together represent 1,3-propylene, 1,4-butylene, 1,5-pentylene, or 1,6-hexylene; W represents four-m
    Type: Grant
    Filed: November 20, 2018
    Date of Patent: September 10, 2019
    Assignee: Tianjin Hemay Bio-Tech Co., Ltd.
    Inventor: Hesheng Zhang
  • Patent number: 10357489
    Abstract: Provided herein is 4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-1-yl)-3-fluorobenzonitrile, or an enantiomer, a mixture of enantiomers, a tautomer, or a pharmaceutically acceptable salt thereof, and methods for treating, preventing or managing multiple myeloma using such compounds. Also provided are pharmaceutical compositions comprising the compounds, and methods of use of the compositions.
    Type: Grant
    Filed: July 9, 2018
    Date of Patent: July 23, 2019
    Assignee: Celgene Corporation
    Inventors: Matthew D. Alexander, Gerald D. Artman, III, James Carmichael, Brian E. Cathers, Matthew D. Correa, Joshua Hansen, Courtney G. Havens, Timothy S. Kercher, Antonia Lopez-Girona, Xiaoling Lu, Hon-Wah Man, Mark A. Nagy, Joseph R. Piccotti, Daniel W. Pierce, Paula A. Tavares-Greco, Brandon W. Whitefield, Lilly L. Wong, Nanfei Zou
  • Patent number: 10287248
    Abstract: The present invention relates to novel processes for the preparation of apremilast of formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 15, 2016
    Date of Patent: May 14, 2019
    Assignee: CIPLA LIMITED
    Inventors: Dharmaraj Ramachandra Rao, Geena Malhotra, Srinivas Laxminarayan Pathi, Ravikumar Puppala, Suryanarayana Durga Yarra
  • Patent number: 10258614
    Abstract: 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: Grant
    Filed: July 17, 2017
    Date of Patent: April 16, 2019
    Assignee: Minerva Neurosciences, Inc.
    Inventors: Remy Luthringer, Nadine Noel, Sandra Werner
  • Patent number: 10220028
    Abstract: 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: Grant
    Filed: March 13, 2017
    Date of Patent: March 5, 2019
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Nigel H. Greig, Weiming Luo, David Tweedie, Harold W. Holloway, Qian-Sheng Yu, Edward J. Goetzl
  • Patent number: 10206914
    Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorder 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: Grant
    Filed: January 3, 2017
    Date of Patent: February 19, 2019
    Assignee: Celgene Corporation
    Inventor: Jerome B. Zeldis
  • Patent number: 10179776
    Abstract: The invention relates to particular 2-((1-(2-hydroxy-2-phenylethyl)piperidin-4-yl)methyl)isoindolin-1-one analogs and pro-drugs, in free, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases that can be therapeutically and/or preventively treated by the nerve control function of sigma ligands.
    Type: Grant
    Filed: June 9, 2015
    Date of Patent: January 15, 2019
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Robert Davis, Peng Li
  • Patent number: 10172920
    Abstract: Provided herein is technology relating to treating sleep apnea and particularly, but not exclusively, to treating sleep apnea with immunotherapeutics and/or anti-inflammatory drugs such as beta-interferons and glatiramer acetate.
    Type: Grant
    Filed: June 14, 2013
    Date of Patent: January 8, 2019
    Assignee: The Regents of The University of Michigan
    Inventors: Tiffany J. Braley, Benjamin Segal, Ronald D. Chervin
  • Patent number: 10058523
    Abstract: Disclosed are novel methods for the therapeutic treatment of cancer and angiogenesis. The enzyme Ape1/Ref-1, via its redox function, enhances the DNA binding activity of transcription factors that are associated with the progression of cancer. The present invention describes the use of agents to selectively inhibit the redox function of Ape1/Ref-1 and thereby reduce tumor cell growth, survival, migration and metastasis. In addition, Ape1/Ref-1 inhibitory activity is shown to augment the therapeutic effects of other therapeutics and protect normal cells against toxicity. Further, Ape1/Ref-1 inhibition is shown to decrease angiogenesis, for use in the treatment of cancer as well other pathologic conditions of which altered angiogenesis is a component.
    Type: Grant
    Filed: April 20, 2015
    Date of Patent: August 28, 2018
    Assignee: Indiana University Research and Technology Corporation
    Inventor: Mark R. Kelley
  • Patent number: 9993467
    Abstract: Pharmaceutical compositions and single unit dosage forms of 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione, or a pharmaceutically acceptable stereoisomer, prodrug, salt, solvate, hydrate, or clathrate, are provided herein. Also provided are methods of treating, managing, or preventing various disorders, such as cancer or an inflammatory disease.
    Type: Grant
    Filed: December 23, 2015
    Date of Patent: June 12, 2018
    Assignee: Celgene Corporation
    Inventors: Anthony J. Tutino, Michael T. Kelly
  • Patent number: 9975872
    Abstract: Provided are processes for the preparation of enantiomerically enriched or enantiomerically pure 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a pharmaceutically acceptable form thereof.
    Type: Grant
    Filed: March 2, 2016
    Date of Patent: May 22, 2018
    Assignee: Celgene Corporation
    Inventors: John F. Traverse, Chengmin Zhang, Gregg B. Feigelson, Benjamin M. Cohen, William W. Leong
  • Patent number: 9975921
    Abstract: Crystalline forms of anamorelin which are useful as pharmaceutical agents are disclosed. Methods of production and isolation of these polymorphs and pharmaceutical compositions which include these polymorphs and pharmaceutical methods of treatment are also disclosed. The crystalline polymorphs of the present invention are useful as they act directly on the pituitary gland cells to release growth hormone.
    Type: Grant
    Filed: October 30, 2015
    Date of Patent: May 22, 2018
    Assignee: HELSINN HEALTHCARE SA
    Inventors: Keith Lorimer, Seemon H Pines, Bernhard Paul, Benjamin Littler
  • Patent number: 9925207
    Abstract: 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: Grant
    Filed: October 17, 2014
    Date of Patent: March 27, 2018
    Assignee: Celgene Corporation
    Inventor: Jerome B. Zeldis
  • Patent number: 9914719
    Abstract: 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: Grant
    Filed: August 25, 2014
    Date of Patent: March 13, 2018
    Assignee: Astex Therapeutics Ltd.
    Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford, Maria Grazia Carr, Robert Downham, Michael Alistair O'Brien, Theresa Rachel Phillips, Andrew James Woodhead
  • Patent number: 9895444
    Abstract: The present invention provides compositions and methods and for increasing the bioavailability of therapeutic agents in a subject. The compositions include at least one alkyl glycoside and at least one therapeutic agent, wherein the alkylglycoside has an alkyl chain length from about 10 to about 16 carbon atoms.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: February 20, 2018
    Assignee: Aegis Therapeutics, LLC
    Inventor: Edward T. Maggio
  • Patent number: 9857359
    Abstract: Use of cereblon-associated proteins as biomarkers for clinical sensitivity to cancer, inflammatory diseases, and patient response to drug treatment.
    Type: Grant
    Filed: June 28, 2013
    Date of Patent: January 2, 2018
    Assignee: CELGENE CORPORATION
    Inventors: Peter H. Schafer, Rajesh Chopra, Antonia Lopez-Girona, Laura Corral, Maria Yinglin Wang, Pilgrim Jackson
  • Patent number: 9828361
    Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Grant
    Filed: February 10, 2016
    Date of Patent: November 28, 2017
    Assignee: Celgene Corporation
    Inventors: Hon-Wah Man, Roger Shen-Chu Chen, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Weihong Zhang
  • Patent number: 9822094
    Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Grant
    Filed: February 10, 2016
    Date of Patent: November 21, 2017
    Assignee: Celgene Corporation
    Inventors: Hon-Wah Man, Roger Shen-Chu Chen, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Weihong Zhang
  • Patent number: 9730920
    Abstract: 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)•HC1•2H2O. Pharmaceutical compositions comprising Form (A) of Compound (I)•HC1•2H2O and related methods of treatment are also disclosed.
    Type: Grant
    Filed: September 28, 2016
    Date of Patent: August 15, 2017
    Assignee: Minerva Neurosciences, Inc.
    Inventors: Remy Luthringer, Nadine Noel, Sandra Werner
  • Patent number: 9701663
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: July 11, 2017
    Assignee: INNOV17 LLC
    Inventors: Anderson Gaweco, Jefferson Tilley, James Blinn
  • Patent number: 9695146
    Abstract: Provided herein are solid forms comprising (a) 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione and (b) a coformer. Pharmaceutical compositions comprising the solid forms (e.g., cocrystals) and methods for treating, preventing and managing various disorders are also disclosed.
    Type: Grant
    Filed: March 25, 2014
    Date of Patent: July 4, 2017
    Assignee: Celgene Corporation
    Inventors: G. Patrick Stahly, David Jonaitis, Ho-Wah Hui, Kevin J. Klopfer
  • Patent number: 9669015
    Abstract: This invention is directed to derivatives of piperidine-2,6-dione, or their organic or inorganic salts thereof, a methods of synthesis of these derivatives, and their application as active pharmaceutical ingredient as inhibitors of TNF? releasing in cells, the derivative of piperidine-2,6-dione being of the general formula (I): wherein n represents 1, 2, 3, 4, 5 or 6; R1 represents from one to four of the same or different substituents selected from F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, NO2, NHC(O)C1-4 alkyl, NH2, NH(C1-4 alkyl), N(C1-4 alkyl)2; R2 represents OR3, NR3R4, N(R3)COR4, O2CR5; R3 and R4 represent independently and at each occurrence H or C1-4 alkyl; R5 represents CHR6NR7R8, CHR6NR9C(O)CHR10NR7R8, a heterocycle W or CHR6NR9C(O)W; R6, R9, R10 represent independently and at each occurrence H, or C1-4 alkyl; R7 and R8 represent independently and at each occurrence H, C1-4 alkyl, or R7 and R8 taken together represent 1,3-propylene, 1,4-butylene, 1,5-pentylene, or 1,6-hexylene; W represents four-m
    Type: Grant
    Filed: June 16, 2015
    Date of Patent: June 6, 2017
    Assignee: Tianjin Hemay Bio-Tech Co., Ltd.
    Inventor: Hesheng Zhang
  • Patent number: 9662321
    Abstract: 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: Grant
    Filed: May 20, 2016
    Date of Patent: May 30, 2017
    Assignee: Celgene Corporation
    Inventor: Jerome B. Zeldis
  • Patent number: 9657020
    Abstract: Provided herein are ergoline compounds and pharmaceutical compositions thereof. In some embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1A, 5-HT1B and 5-HT1D receptors without agonizing the 5-HT2B receptor using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the 5-HT2B adrenergic alpha2A and/or the alpha2B receptors using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the D2 and D3 receptor using the compounds and pharmaceutical compositions disclosed herein.
    Type: Grant
    Filed: January 20, 2016
    Date of Patent: May 23, 2017
    Assignee: Xoc Pharmaceuticals, Inc.
    Inventors: Thomas Armer, Geoff McKinley, Scott Borland, Miguel Guzman, Ármin Szabolcs, János Gerencser
  • Patent number: 9637471
    Abstract: 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: Grant
    Filed: February 14, 2014
    Date of Patent: May 2, 2017
    Assignee: Technische Universitat Munchen
    Inventors: Arne Skerra, Michael Muller, Michael Schemann, Thomas Berger
  • Patent number: 9498472
    Abstract: 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: Grant
    Filed: June 3, 2015
    Date of Patent: November 22, 2016
    Assignee: Celgene Corporation
    Inventor: Jerome B. Zeldis
  • Patent number: 9458155
    Abstract: 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: Grant
    Filed: November 3, 2014
    Date of Patent: October 4, 2016
    Assignee: MEDIVATION TECHNOLOGIES, INC
    Inventors: David T. Hung, Andrew A. Protter, Rajendra Parasmal Jain, Sarvajit Chakravarty
  • Patent number: 9458130
    Abstract: 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: Grant
    Filed: November 30, 2015
    Date of Patent: October 4, 2016
    Assignee: Minerva Neurosciences, Inc.
    Inventor: Remy Luthringer
  • Patent number: 9447070
    Abstract: 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: Grant
    Filed: September 18, 2014
    Date of Patent: September 20, 2016
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Roger Shen-Chu Chen, Alexander L. Ruchelman
  • Patent number: 9403867
    Abstract: 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: Grant
    Filed: November 12, 2014
    Date of Patent: August 2, 2016
    Assignees: Ono Pharmaceuticals Co., Ltd., Helsinn Healthcare SA
    Inventors: Shin-Itsu Kuwabe, Takehiko Yanagimachi, Hideyuki Yoshiyama, Seemon Pines, Eleanor De Groot, Silvina Garcia Rubio, Peter Manini
  • Patent number: 9393255
    Abstract: 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: Grant
    Filed: January 31, 2012
    Date of Patent: July 19, 2016
    Assignee: Celgene Corporation
    Inventors: Anthony Tutino, Mei Lai, Jeffrey B. Etter
  • Patent number: 9382227
    Abstract: 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: Grant
    Filed: January 2, 2014
    Date of Patent: July 5, 2016
    Assignee: Cold Spring Harbor Laboratory
    Inventors: Hiro Furukawa, Erkan Karakas
  • Patent number: 9371309
    Abstract: 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: Grant
    Filed: September 22, 2011
    Date of Patent: June 21, 2016
    Assignee: Celgene Corporation
    Inventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller
  • Patent number: 9365538
    Abstract: 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: Grant
    Filed: January 14, 2009
    Date of Patent: June 14, 2016
    Assignee: Celgene Corporation
    Inventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller
  • Patent number: 9353080
    Abstract: 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: Grant
    Filed: September 22, 2011
    Date of Patent: May 31, 2016
    Assignee: Celgene Corporation
    Inventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller
  • Patent number: 9283215
    Abstract: 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: Grant
    Filed: March 7, 2014
    Date of Patent: March 15, 2016
    Assignee: Celgene Corporation
    Inventor: Jerome B. Zeldis
  • Patent number: 9284299
    Abstract: 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: Grant
    Filed: February 10, 2013
    Date of Patent: March 15, 2016
    Assignee: University of Utah Research Foundation
    Inventors: Haitao Ji, Binxun Yu, Min Zhang, Wenxing Guo
  • Patent number: 9206156
    Abstract: 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: Grant
    Filed: December 11, 2012
    Date of Patent: December 8, 2015
    Assignee: GRÜNENTHAL GMBH
    Inventors: Stefan Schunk, Stefan Oberbörsch, Werner Englberger, Bernd Sundermann
  • Patent number: 9192662
    Abstract: 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: Grant
    Filed: January 29, 2009
    Date of Patent: November 24, 2015
    Assignee: Celgene Corporation
    Inventors: Helen A. Brady, Kyle Chan
  • Patent number: 9181216
    Abstract: 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: Grant
    Filed: November 18, 2013
    Date of Patent: November 10, 2015
    Assignee: Celgene Corporation
    Inventors: Alexander L. Ruchelman, George W. Muller, Hon-Wah Man, Roger Shen-Chu Chen
  • Patent number: 9139556
    Abstract: 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: Grant
    Filed: September 22, 2011
    Date of Patent: September 22, 2015
    Assignee: Celgene Corporation
    Inventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller, Manohar T. Saindane, Louise M. Cameron
  • Patent number: 9139555
    Abstract: 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: Grant
    Filed: January 14, 2009
    Date of Patent: September 22, 2015
    Assignee: Celgene Corporation
    Inventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller
  • Patent number: 9108945
    Abstract: 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: Grant
    Filed: January 9, 2014
    Date of Patent: August 18, 2015
    Assignee: Natco Pharma Limited
    Inventors: Durga Prasad Konakanchi, Buchappa Gongalla, Kotayya Babu Sikha, Chandrasekar Kandaswamy, Kali Satya Bhujanga Rao Adibhatla, Venkaiah Chowdary Nannapaneni
  • Patent number: 9101622
    Abstract: 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: Grant
    Filed: September 10, 2014
    Date of Patent: August 11, 2015
    Assignee: Celgene Corporation
    Inventor: Jerome B. Zeldis
  • Patent number: 9090585
    Abstract: 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: Grant
    Filed: March 28, 2012
    Date of Patent: July 28, 2015
    Assignee: DeuteRx, LLC
    Inventor: Sheila DeWitt
  • Patent number: 9084783
    Abstract: 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: Grant
    Filed: December 15, 2014
    Date of Patent: July 21, 2015
    Assignee: THE UNITED STATES OF AMERICA, as represented by the Secretary, Department of Health and Human Services
    Inventors: Nigel H. Grieg, Weiming Luo, David Tweedie, Harold W. Holloway, Qian-Sheng Yu, Edward J. Goetzl
  • Patent number: 9085530
    Abstract: 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: Grant
    Filed: June 1, 2010
    Date of Patent: July 21, 2015
    Assignees: Nanjing Cavendish Bio-Engineering Technology Co., Ltd.
    Inventors: Rong Yan, Hao Yang, Yongxiang Xu
  • Patent number: 9085551
    Abstract: 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: Grant
    Filed: February 20, 2013
    Date of Patent: July 21, 2015
    Assignee: Celgene Corporation
    Inventors: Ying Li, Jean Xu, Kevin J. Klopfer
  • Patent number: RE45685
    Abstract: 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: Grant
    Filed: October 4, 2013
    Date of Patent: September 29, 2015
    Assignee: Celgene Corporation
    Inventors: Hon-Wah Man, George W. Muller
  • Patent number: RE46639
    Abstract: 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: Grant
    Filed: July 16, 2014
    Date of Patent: December 19, 2017
    Assignee: Celgene Corporation
    Inventors: Alexander L. Ruchelman, George W. Muller, Hon-Wah Man, Roger Shen-Chu Chen