Plural Hetero Atoms In The Tetracyclo Ring System (e.g., Acronycines, Etc.) Patents (Class 514/285)
  • Patent number: 10624885
    Abstract: Disclosed is the synthesis procedure for benzazolo[3,2-a]quinolinium chloride salts and the inclusion of chloro-substituent, amino-substituent, and nitro-substituent resulting in several compounds. The compounds are further used as markers due to their fluorescent properties including in hypoxic environments. This disclosure further describes anti-cancer screening of two BQS, namely, 7-benzyl-3-aminobenzimidazo[3,2-a]quinolinium chloride (ABQ-48: NSC D-763307) and the corresponding 7-benzyl-3-nitrobenzimidazo[3,2-a]quinolinium chloride (NBQ 48: NSC D-763303).
    Type: Grant
    Filed: February 13, 2018
    Date of Patent: April 21, 2020
    Inventors: Osvaldo Cox, Beatriz Zayas
  • Patent number: 10464919
    Abstract: The present invention relates to novel tricyclic derivative compounds, and more specifically to tricyclic derivative compounds, optical isomers thereof, racemates thereof, or pharmaceutically acceptable salts thereof, which have excellent activity against PARP-1, tankyrase-1 or tankyrase-2. The tricyclic derivative compounds, optical isomers thereof, racemates thereof or pharmaceutically acceptable salts thereof according to the present invention have inhibitory activity against PARP-1, tankyrase-1, or tankyrase-2, and thus can be effectively used for the prevention or treatment of neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic neuropathy, inflammatory diseases, osteoporosis, or cancer.
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: November 5, 2019
    Assignee: Je Il Pharmaceutical Co., Ltd.
    Inventors: Hyunho Lee, Kwangwoo Chun, Bo-Young Joe, Eun Seon Kim, Eun Sung Jang, Hyeongchan Oh, Jeong-Min Kim, Jiseon Park, Hanchang Lee
  • Patent number: 9889128
    Abstract: Disclosed is the synthesis procedure for benzazolo[3,2-a]quinolinium chloride salts and the inclusion of chloro-substituent, amino-substituent, and nitro-substituent resulting in several compounds. The compounds are further used as markers due to their fluorescent properties including in hypoxic environments. This disclosure further describes anti-cancer screening of two BQS, namely, 7-benzyl-3-aminobenzimidazo[3,2-a]quinolinium chloride (ABQ-48: NSC D-763307) and the corresponding 7-benzyl-3-nitrobenzimidazo[3,2-a]quinolinium chloride (NBQ 48: NSC D-763303).
    Type: Grant
    Filed: September 17, 2015
    Date of Patent: February 13, 2018
    Inventors: Osvaldo Cox, Beatriz Zayas
  • Patent number: 9408831
    Abstract: Provided herein are methods for modulating immune responses to a respiratory viral infection (e.g., influenza, rhinovirus, coronavirus, or paramyxovirus) in a subject, wherein the methods comprise administering to the subject a compound (e.g., a PDE4 modulator or an immunomodulatory compound), or a pharmaceutically acceptable salt, solvate, hydrate, or stereoisomer thereof. Also provided herein are methods for treating, preventing, ameliorating, and/or delaying the onset of one or more symptoms associated with or resulting from a respiratory viral infection (e.g., influenza, rhinovirus, coronavirus, or paramyxovirus) in a subject, wherein the methods comprise administering to the subject a compound (e.g., a PDE4 modulator or an immunomodulatory compound), or a pharmaceutically acceptable salt, solvate, hydrate, or stereoisomer thereof.
    Type: Grant
    Filed: April 5, 2011
    Date of Patent: August 9, 2016
    Assignee: Celgene Corporation
    Inventor: Jerome B. Zeldis
  • Patent number: 9296751
    Abstract: Provided are an indolizino[3,2-c]quinoline derivative, pharmaceutically acceptable salt thereof, and a method for preparing the same. The indolizino[3,2-c]quinoline derivative, pharmaceutically acceptable salt thereof may function as an agonist of cystic fibrosis conductance transmembrane regulator, and thus may be useful for an agent for preventing or treating diseases caused by degradation of activity of cystic fibrosis conductance transmembrane regulator and for a pharmaceutical composition for stimulating proliferation of stem cells.
    Type: Grant
    Filed: October 15, 2015
    Date of Patent: March 29, 2016
    Assignee: INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY
    Inventors: Ikyon Kim, Wan Namkung, Jonghyuk Sung
  • Patent number: 9243002
    Abstract: The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Grant
    Filed: February 3, 2014
    Date of Patent: January 26, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xing Dai, Hong Liu, Anandan Palani, Shuwen He, Linda L. Brockunier, Ravi Nargund, Karen Marcantonio, Nicolas Zorn, Dong Xiao, Xuanjia Peng, Peng Li, Tao Guo
  • Patent number: 9133128
    Abstract: The invention provides compounds capable of acting as antagonists at cannabanoid receptors according to the following formula: Such compounds may be used to treat conditions for which the cannabinoid receptor system has been implicated, such as obesity, liver disease, diabetes, pain, and inflammation.
    Type: Grant
    Filed: June 15, 2012
    Date of Patent: September 15, 2015
    Assignee: Research Triangle Institute
    Inventors: Alan Bradley Fulp, Rangan Maitra, Yanan Zhang, Herbert H. Seltzman
  • Publication number: 20150141419
    Abstract: The present invention relates to a diarylo[a,g]quinolizidine compound of formula (I), enantiomer, diastereoisomer, racemate, mixture, pharmaceutically acceptable salt, crystalline hydrate or solvate thereof; the preparation method thereof, and uses thereof in preparing an experimental model drugs related to dopamine receptors and 5-HT receptors or a medicament for treating or preventing a disease related to dopamine receptors and 5-HT receptors.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 21, 2015
    Inventors: Hong Liu, Xuechu Zhen, Haifeng Sun, Liyuan Zhu, Wangke Qian, Leiping Yu, Zeng Li, Shengbin Zhou, Wenxian Cai, Hualiang Jiang, Kaixian Chen
  • Patent number: 9034870
    Abstract: The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase I, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer.
    Type: Grant
    Filed: March 6, 2014
    Date of Patent: May 19, 2015
    Assignees: Purdue Research Foundation, United States Government National Institutes of Health (NIH), U.S. Dept. of Health and Human Services (DHHS), NIH Division of Extramural Inventions and Technology Resources (DEITR)
    Inventors: Mark S. Cushman, Evgeny A. Kiselev, Andrew E. Morrell, Yves George Pommier
  • Publication number: 20150118293
    Abstract: The invention relates to the fabrication of novel and improved delivery system comprising of short-chain-length polyhydroxyalkanoates (scl-PHA) nanoparticles having anticancer drug ellipticine (EPT) encapsulated therein for oral administration. The scl-PHA is synthesized by indigenous bacterial isolate Bacillus cereus FC11 (NCBI GenBank accession number JN593010) using modified GTYN medium.
    Type: Application
    Filed: October 30, 2013
    Publication date: April 30, 2015
    Inventors: Farha Masood, P. Chen, Tariq Yasin, Abdul Hameed
  • Patent number: 9012441
    Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Grant
    Filed: January 9, 2014
    Date of Patent: April 21, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Steven S. Bondy, Carina E. Cannizzaro, Chien-Hung Chou, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
  • Publication number: 20150086491
    Abstract: The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.
    Type: Application
    Filed: November 5, 2014
    Publication date: March 26, 2015
    Inventors: Thomas Subkowski, Michael Backes, Heiko Oertling, Arnold Machinek, Hubert Loges, Ulrike Simchen, Horst Surburg, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel
  • Publication number: 20150079107
    Abstract: Provided herein are methods and assays for isolating and culturing seborrheic keratosis cells ex vivo. Also provided herein are screening assays using cultured seborrheic keratosis cells and methods for treating seborrheic keratosis in a subject.
    Type: Application
    Filed: April 26, 2013
    Publication date: March 19, 2015
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: Anna I. Mandinova, Sam W. Lee, Victor A. Neel
  • Patent number: 8969373
    Abstract: A compound of general formula (I); A is O, S, CH, NH or NR?, when O links with Z3, Z1 is N or CRZ1, Z2 is CRZ2, when Z1 links with O, Z2 is CH, Z3 is C—Ar; Ra, Rb, Rc and Rd independently is H, OH, halogen or —Y1—Rm; A1 is NH or CH2; R1? is alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl; A2 is N, O or linking bond; R1 is hydrogen, or, R1 linking covalently with R3 forms C5-C9 saturated or unsaturated hydrocarbon chain substituted by O or N; R3 is alkyl, cycloalkyl, heterocycloalkyl, alkyl substituted by cycloalkyl etc; R4 is alkoxy-CO, alkyl-NHCO, (alkyl)2NCO, or formyl substituted by aryl, cycloalkyl, heterocycloalkyl.
    Type: Grant
    Filed: July 23, 2012
    Date of Patent: March 3, 2015
    Assignee: Shanghai Tangrun Pharmaceuticals Co., Ltd.
    Inventor: Suoming Zhang
  • Patent number: 8969372
    Abstract: 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: Grant
    Filed: November 15, 2004
    Date of Patent: March 3, 2015
    Assignee: Aptose Boisciences Inc.
    Inventors: Mario Huesca, Raed Al-Qawasmeh, Aiping H. Young, Yoon Lee
  • Publication number: 20150051194
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. WENTLAND
  • Publication number: 20150038438
    Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.
    Type: Application
    Filed: August 29, 2012
    Publication date: February 5, 2015
    Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, Guangming Chen, Olya Ginzburg, Song Huang, Jana Narasimhan, Srinivasa Peddi, Sean Wesley Smith, Anthony Allan Turpoff, Matthew G. Woll, Nanjing Zhang, Xiaoyan Zhang
  • Publication number: 20150025096
    Abstract: The invention is directed, in part, to compositions comprising small molecule compounds to treat or prevent hearing loss. Compositions of the present invention also promote sensory hair cell regeneration. Particular compositions comprise ellipticine derivatives, and optionally one or more small molecules that increase Atoh1 expression or activity, and optionally one or more growth factors.
    Type: Application
    Filed: February 22, 2013
    Publication date: January 22, 2015
    Inventors: Robert Scott Thies, Francine Farouz, Zhiyong Wang, Chin-Chun Jean Lu
  • Publication number: 20150018380
    Abstract: The present invention provides methods for obtaining specific and non-toxic inhibitors of AID nuclear import. The methods comprise a primary screen and a counter screen to identify a pool of AID specific nuclear import inhibitors that do not have off-target of toxic effects. AID specific nuclear import inhibitors identified by the screens of the invention prevent nuclear entry, limit the access of AID to genomic DNA, and inhibit AID mutagenic activity. Preparations, including pharmaceutical preparations, comprising specific nuclear import inhibitors, used for example, to inhibit cancer progression, are also encompassed in the invention.
    Type: Application
    Filed: February 7, 2013
    Publication date: January 15, 2015
    Applicant: University of Rochester
    Inventor: Harold C. Smith
  • Publication number: 20150011516
    Abstract: Pharmaceutical compositions that bind to a predicted FK506 Binding Protein 52 (FKBP52) interaction surface on the androgen receptor hormone binding domain, otherwise known as FKBP52 Targeting Agents (FTAs) are provided. These compositions of the present invention are found to specifically recognize the FKBP52 regulatory surface on the androgen receptor and inhibit FKBP52 from functionally interacting with the androgen receptor. Compositions comprising the pharmaceutical composition, as well as methods of use, treatment and screening are also provided.
    Type: Application
    Filed: July 21, 2014
    Publication date: January 8, 2015
    Inventors: Leonard M. Neckers, Marc B. Cox, Jane B. Neckers, Yeong Sang Kim, Aki Iwai, Yangmin Ning, Johanny Tonos de Leon, Heather A. Balsiger, Robert Fletterick
  • Publication number: 20150005322
    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and 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: Application
    Filed: September 12, 2014
    Publication date: January 1, 2015
    Inventors: Rajendra Parasmal JAIN, Sarvajit Chakravarty
  • Publication number: 20140364443
    Abstract: Disclosed are 1,4-dihydro-naphthyridine derivatives and pharmaceutical composition and uses thereof. The 1,4-dihydro-naphthyridine derivatives are a compound capable of inhibiting acetylcholinesterase activity and preventing extracellular calcium from flowing into a cell via a calcium channel, i.e., having a dual-activity, which are of potential importance as a pharmaceutical and can be used to prepare the drugs for treating cardiovascular diseases, cerebrovascular diseases and dementia.
    Type: Application
    Filed: December 7, 2012
    Publication date: December 11, 2014
    Applicant: Jiangsu Simovay Pharmaceutical Co., Ltd.
    Inventors: Rong Chen, Lin Feng, Zhengping Zhang, Fang Fang, Qingli Dong, Fulong Li, Lei Wang, Yao Hua, Shibao Yang, Peng Wang
  • Patent number: 8895726
    Abstract: The present invention relates to a compound derived from indole corresponding to the following formula II: wherein X represents N, CR8 or N+R8, wherein R8 represents a hydrogen atom, a hydroxyl or alkyl or methoxy group optionally substituted with a phenyl group; R2, R3 and R4 independently represent a hydrogen atom or a halogen atom or an optionally substituted alkyl, amine, alkene, ester, sulfonamide, ether or benzyl group; R5 represents a hydrogen atom or an optionally substituted, saturated or unsaturated alkyl group, amine, benzyl group; R6 represents an optionally substituted C1-C3 alkyl group; R7 represents a hydrogen atom or an optionally substituted C1-C3 alkyl group and R7 is absent when the ring A is in the b position, and A represents a ring; R9 and R10 represent together a carbon bond or independently represent an R11 OR11, SR11 group; wherein R11 represents a hydrogen atom, an optionally substituted, saturated or unsaturated, C1-C3 alkyl group, which may contain one or more sulfur, oxygen or
    Type: Grant
    Filed: February 19, 2008
    Date of Patent: November 25, 2014
    Assignees: The Institut Curie, The University of Montpellier 2 Science and Techniques
    Inventors: Fabrice Lejeune, Jamal Tazi, David Grierson, Christian Rivalle, Florence Mahuteau-Betzer
  • Patent number: 8883818
    Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of atopic eczema.
    Type: Grant
    Filed: April 30, 2013
    Date of Patent: November 11, 2014
    Assignee: Takeda GmbH
    Inventor: Ulrich Kautz
  • Publication number: 20140309182
    Abstract: The present invention relates to an insecticidal enriched extract (biopesticide) isolated from the stem of Nothapodites foetida (Wight) Sleumer (formerly Mappia foetida (Miers) useful for the insect free storage and transport of grains and seed. The insecticidal activity of the enriched extract (biopesticide) of the invention is ascribed to compound/s other than camptothecin. The invention further relates to the process for preparation thereof, containing Compounds of general formula 1 and formula 2 (General formula 1) wherein R1=CH3, CH2OAC and wherein R2=COOH, or (I) and R3=H. OH.
    Type: Application
    Filed: June 21, 2012
    Publication date: October 16, 2014
    Inventors: Swati Pramod Joshi, John Pereira, Phool Kumar Patanjali, Sunita Sharad Kunte, Kiran Babasaheb Sonawane, Suresh Gurappa Mummigatti, Sumithra Devi Sanna, Krishnaiah Eraiah Hullukere, Seema Chaudhary
  • Patent number: 8859561
    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and 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: September 23, 2010
    Date of Patent: October 14, 2014
    Assignee: Medivation Technologies, Inc.
    Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
  • Publication number: 20140303144
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?2B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: October 9, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvajit Chakravarty
  • Publication number: 20140296209
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?1B—The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: October 2, 2014
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventors: Andrew Asher Protter, Sarvajit Chakravarty
  • Publication number: 20140234428
    Abstract: The invention, a transdermal delivery method, relates to penetration-enhancing pharmaceutical compositions comprising a novel, stable mixture of cetylated esters, cetyl or stearyl alcohols, polar solvents and surfactants, which, under appropriate conditions, combine into amphiphilic nanoparticles within a stabilized liquid dispersion for use in delivery of medicinal agents through the skin. The term cetosomes is used to describe these particles in order to differentiate them from other nanoparticles, such as niosomes, cerasomes, polymeric micelles, dendrimers, liposomes, lipoids, solid lipid nanoparticles and other particles. The self-assembling cetosomes, with both ionic and nonionic points of attraction, incorporate and concentrate a variety of different bioactive agents of interest and demonstrate stable properties with similarities to colloidal molecular structures. The compositions enhance topical transdermal fluxes of bioactives without permanently disrupting natural skin barrier function.
    Type: Application
    Filed: February 15, 2013
    Publication date: August 21, 2014
    Applicant: Cymbiotics, Inc.
    Inventors: Raj R. Barathur, Jack Bain Bookout
  • Publication number: 20140228353
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 14, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvvajit Chakravarty
  • Patent number: 8785471
    Abstract: Preparation and usage of a pharmaceutical composition containing ferulic acid and matrine compounds are described. The ingredients ferulic acid and matrine compounds in this pharmaceutical composition have synergistic effects which can obviously improve the pharmacology effects of both the ferulic acid and matrine compounds. Moreover, the pharmaceutical composition can significantly increase the aqueous and fat solubility of the individual ingredients.
    Type: Grant
    Filed: September 9, 2009
    Date of Patent: July 22, 2014
    Assignee: Qingdao Qiyuan Bio-Technologies Co., Ltd.
    Inventors: Xiaojie Sun, Weifu Ma
  • Publication number: 20140187547
    Abstract: The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase I, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer.
    Type: Application
    Filed: March 6, 2014
    Publication date: July 3, 2014
    Applicant: Purdue Research Foundation
    Inventors: Mark S. CUSHMAN, Evgeny A. KISELEV, Andrew E. MORRELL
  • Publication number: 20140162985
    Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: September 6, 2013
    Publication date: June 12, 2014
    Applicant: ABBVIE INC.
    Inventors: Andrew Burchat, Thomas D. Gordon, Kelly D. Mullen, David C. Ihle, Michael J. Morytko, Kevin P. Cusack, Gloria Y. Lo Schiavo, Lei Wang, Michael Friedman
  • Publication number: 20140163012
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described.
    Type: Application
    Filed: October 31, 2013
    Publication date: June 12, 2014
    Applicant: Albany Molecular Research, Inc.
    Inventors: Matthew D. SURMAN, Emily E. FREEMAN, Peter R. GUZZO, Alan J. HENDERSON, Mark HADDEN
  • Publication number: 20140155384
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor a2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2? and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: June 5, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvajit Chakravarty
  • Patent number: 8703181
    Abstract: The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provides methods of making the liposome compositions provided by the present invention.
    Type: Grant
    Filed: October 17, 2012
    Date of Patent: April 22, 2014
    Assignee: Merrimack Pharmaceuticals, Inc.
    Inventors: Keelung Hong, Daryl C. Drummond, Dmitri Kirpotin
  • Publication number: 20140073637
    Abstract: The present invention relates to a new class of benzo[e]pyrido-indole, the amino-substituted-alkyloxy-benzo[e]pyrido[4,3-b]indole derivatives, having a particular kinase inhibition profile and useful as a therapeutic agent, in particular an anti-tumoral agent.
    Type: Application
    Filed: May 30, 2012
    Publication date: March 13, 2014
    Applicants: INSTITUT CURIE, INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Chi-Hung N'Guyen, Annie Molla, Ly-Thuy-Tram Le
  • Publication number: 20140018360
    Abstract: The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase I, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: January 16, 2014
    Inventors: Mark S. CUSHMAN, Evgeny A. KISELEV, Andrew E. MORRELL
  • Patent number: 8629158
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
    Type: Grant
    Filed: July 1, 2010
    Date of Patent: January 14, 2014
    Assignee: Albany Molecular Research, Inc.
    Inventors: Peter R. Guzzo, Matthew David Surman, Alan John Henderson, Mark Hadden, Emily Elizabeth Freeman
  • Publication number: 20130345164
    Abstract: This invention concerns methods of identifying treatments for treating various disorders and related computer products and systems. Also disclosed are methods for treating cellular proliferative disorders and use of compounds identified for such treatment.
    Type: Application
    Filed: April 21, 2011
    Publication date: December 26, 2013
    Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY
    Inventors: Alexei Vazquez, Darren Carpizo, Arnold Levine
  • Patent number: 8604048
    Abstract: Pyridocarbazole-type compounds of formula (I): are provided as a medicament, and more particularly for application in anticancer chemotherapy. Also provided is a pharmaceutical composition with the compound and methods for preventing and/or treating neurodegenerative-type pathologies, such as Alzheimer's disease and schizophrenia, parasitoses, such as malaria, or glaucomas.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: December 10, 2013
    Assignees: Centre National de la Recherche Scientifique, Institut Curie, Commissariat a l'Energie Atomique et aux Energies Alternatives, Universite Paris Sud (Paris XI)
    Inventors: Laurence Lafanechere, Emilie Vassal, Caroline Barette, ChiHung Nguyen, Christian Rivalle, Renaud Prudent
  • Patent number: 8592424
    Abstract: A method of treating a disease state or condition in humans via topical brainstem afferent stimulation therapy via the administration of a drug to the back of the neck of a human patient at the hairline in close proximity to and under or on the area of skin above the brain stem to provide regional neuro-affective therapy is disclosed.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: November 26, 2013
    Assignee: Afgin Pharma LLC
    Inventor: Ronald Aung-Din
  • Patent number: 8580811
    Abstract: Provided herein are compounds that bind to androgen receptors and/or modulate activity of androgen receptors, and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.
    Type: Grant
    Filed: March 6, 2012
    Date of Patent: November 12, 2013
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Bijan Pedram, Cornelis Arjan Van Oeveren, Lin Zhi, Shuo Zhao, Yixing Shen
  • Publication number: 20130266556
    Abstract: Biomass (e.g., plant biomass, animal biomass, microbial, and municipal waste biomass) is processed to produce useful products, such as food products and amino acids.
    Type: Application
    Filed: November 9, 2010
    Publication date: October 10, 2013
    Applicant: XYLECO, INC.
    Inventor: Marshall Medoff
  • Publication number: 20130251757
    Abstract: The present disclosure generally relates to methods of making nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol.
    Type: Application
    Filed: December 13, 2012
    Publication date: September 26, 2013
    Inventors: Gregory Troiano, Michael Figa, Abhimanyu Sabnis
  • Publication number: 20130224310
    Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are noscapine analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers. While the antitussive plant alkaloid, noscapine, binds tubulin, displays anticancer activity, and has a safe pharmacological profile in humans, structure-function analyses pointed to a proton at position 9 of the isoquinoline ring that can be modified without compromising tubulin binding activity. Noscapine analogs with various functional moieties at position 9 on the isoquinoline ring kill human cancer cells resistant to other anti-microtubule agents, such as vincas and taxanes.
    Type: Application
    Filed: June 5, 2012
    Publication date: August 29, 2013
    Applicant: Emory University
    Inventors: Harish C. Joshi, Ritu Aneja, Surya N. Vangapandu
  • Publication number: 20130217673
    Abstract: Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of mixed monoamine reuptake inhibitor locally at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least thirty days. In some embodiments, the relief can be for at least at least fifty days, at least one hundred days, at least one hundred and twenty days, at least one hundred and thirty, at least one hundred fifty days or at least one hundred and eighty days.
    Type: Application
    Filed: February 22, 2012
    Publication date: August 22, 2013
    Applicant: Warsaw Orthopedic, Inc
    Inventor: Jared T. Wilsey
  • Publication number: 20130216520
    Abstract: Biomass (e.g., plant biomass, animal biomass, microbial, and municipal waste biomass) is processed to produce useful products, such as food products and amino acids.
    Type: Application
    Filed: November 9, 2010
    Publication date: August 22, 2013
    Applicant: XYLECO, INC.
    Inventor: Marshall Medoff
  • Publication number: 20130217675
    Abstract: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. 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: Application
    Filed: February 18, 2011
    Publication date: August 22, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20130190294
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
    Type: Application
    Filed: March 7, 2013
    Publication date: July 25, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: Medivation Technologies, Inc