Plural Hetero Atoms In The Tetracyclo Ring System (e.g., Acronycines, Etc.) Patents (Class 514/285)
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Patent number: 11760758Abstract: The present invention provides a compound having the structure: or a pharmaceutically acceptable salt or ester thereof, and a method of treating a subject afflicted with pain, a depressive disorder, a mood disorder or an anxiety disorder by administering the compound to the subject.Type: GrantFiled: February 16, 2021Date of Patent: September 19, 2023Assignees: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK, THE RESEARCH FOUNDATION FOR MENTAL HYGIENE, INC., SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Andrew C. Kruegel, Dalibor Sames, Srijita Bhowmik, Vaclav Havel, Juraj Galeta, Jonathan A. Javitch, Susruta Majumdar
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Patent number: 11311531Abstract: 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: GrantFiled: April 20, 2020Date of Patent: April 26, 2022Inventors: Osvaldo Cox, Beatriz Zayas
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Patent number: 11046692Abstract: Described herein are compounds of Formulae (I?)-(II?), compounds of Formulae (I)-(II) and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful for modulating opioid receptor activity. The provided compounds may have both agonistic and antagonistic effect on one or more opioid receptors. Methods of using the compounds for treating or managing pain are also described.Type: GrantFiled: April 29, 2016Date of Patent: June 29, 2021Assignee: Memorial Sloan-Kettering Cancer CenterInventors: Gavril Pasternak, Susruta Majumdar, Rashad Karimov, Andras Varadi
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Patent number: 10624885Abstract: 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: GrantFiled: February 13, 2018Date of Patent: April 21, 2020Inventors: Osvaldo Cox, Beatriz Zayas
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Patent number: 10464919Abstract: 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: GrantFiled: June 3, 2016Date of Patent: November 5, 2019Assignee: 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
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Patent number: 9889128Abstract: 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: GrantFiled: September 17, 2015Date of Patent: February 13, 2018Inventors: Osvaldo Cox, Beatriz Zayas
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Patent number: 9408831Abstract: 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: GrantFiled: April 5, 2011Date of Patent: August 9, 2016Assignee: Celgene CorporationInventor: Jerome B. Zeldis
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Patent number: 9296751Abstract: 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: GrantFiled: October 15, 2015Date of Patent: March 29, 2016Assignee: INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITYInventors: Ikyon Kim, Wan Namkung, Jonghyuk Sung
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Patent number: 9243002Abstract: 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: GrantFiled: February 3, 2014Date of Patent: January 26, 2016Assignee: 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
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Patent number: 9133128Abstract: 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: GrantFiled: June 15, 2012Date of Patent: September 15, 2015Assignee: Research Triangle InstituteInventors: Alan Bradley Fulp, Rangan Maitra, Yanan Zhang, Herbert H. Seltzman
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Publication number: 20150141419Abstract: 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: ApplicationFiled: May 9, 2013Publication date: May 21, 2015Inventors: Hong Liu, Xuechu Zhen, Haifeng Sun, Liyuan Zhu, Wangke Qian, Leiping Yu, Zeng Li, Shengbin Zhou, Wenxian Cai, Hualiang Jiang, Kaixian Chen
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Patent number: 9034870Abstract: 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: GrantFiled: March 6, 2014Date of Patent: May 19, 2015Assignees: 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
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Publication number: 20150118293Abstract: 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: ApplicationFiled: October 30, 2013Publication date: April 30, 2015Inventors: Farha Masood, P. Chen, Tariq Yasin, Abdul Hameed
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Patent number: 9012441Abstract: 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: GrantFiled: January 9, 2014Date of Patent: April 21, 2015Assignee: 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
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Publication number: 20150086491Abstract: The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.Type: ApplicationFiled: November 5, 2014Publication date: March 26, 2015Inventors: Thomas Subkowski, Michael Backes, Heiko Oertling, Arnold Machinek, Hubert Loges, Ulrike Simchen, Horst Surburg, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel
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Publication number: 20150079107Abstract: 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: ApplicationFiled: April 26, 2013Publication date: March 19, 2015Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Anna I. Mandinova, Sam W. Lee, Victor A. Neel
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Patent number: 8969372Abstract: Therapeutically effective 2,4,5-trisubstituted imidazole compounds are provided. Also provided are methods of preparing the compounds and pharmaceutical compositions comprising the compounds alone or in combination with other agents.Type: GrantFiled: November 15, 2004Date of Patent: March 3, 2015Assignee: Aptose Boisciences Inc.Inventors: Mario Huesca, Raed Al-Qawasmeh, Aiping H. Young, Yoon Lee
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Patent number: 8969373Abstract: 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: GrantFiled: July 23, 2012Date of Patent: March 3, 2015Assignee: Shanghai Tangrun Pharmaceuticals Co., Ltd.Inventor: Suoming Zhang
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Publication number: 20150051194Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.Type: ApplicationFiled: October 31, 2014Publication date: February 19, 2015Applicant: RENSSELAER POLYTECHNIC INSTITUTEInventor: Mark P. WENTLAND
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Publication number: 20150038438Abstract: 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: ApplicationFiled: August 29, 2012Publication date: February 5, 2015Inventors: 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
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Publication number: 20150025096Abstract: 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: ApplicationFiled: February 22, 2013Publication date: January 22, 2015Inventors: Robert Scott Thies, Francine Farouz, Zhiyong Wang, Chin-Chun Jean Lu
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Publication number: 20150018380Abstract: 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: ApplicationFiled: February 7, 2013Publication date: January 15, 2015Applicant: University of RochesterInventor: Harold C. Smith
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Publication number: 20150011516Abstract: 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: ApplicationFiled: July 21, 2014Publication date: January 8, 2015Inventors: 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
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Publication number: 20150005322Abstract: 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: ApplicationFiled: September 12, 2014Publication date: January 1, 2015Inventors: Rajendra Parasmal JAIN, Sarvajit Chakravarty
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Publication number: 20140364443Abstract: 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: ApplicationFiled: December 7, 2012Publication date: December 11, 2014Applicant: 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
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Patent number: 8895726Abstract: 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 orType: GrantFiled: February 19, 2008Date of Patent: November 25, 2014Assignees: The Institut Curie, The University of Montpellier 2 Science and TechniquesInventors: Fabrice Lejeune, Jamal Tazi, David Grierson, Christian Rivalle, Florence Mahuteau-Betzer
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Patent number: 8883818Abstract: 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: GrantFiled: April 30, 2013Date of Patent: November 11, 2014Assignee: Takeda GmbHInventor: Ulrich Kautz
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Publication number: 20140309182Abstract: 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: ApplicationFiled: June 21, 2012Publication date: October 16, 2014Inventors: 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
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Patent number: 8859561Abstract: 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: GrantFiled: September 23, 2010Date of Patent: October 14, 2014Assignee: Medivation Technologies, Inc.Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
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Publication number: 20140303144Abstract: 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: ApplicationFiled: February 17, 2012Publication date: October 9, 2014Applicant: Medivation Technologies, Inc.Inventors: Andrew Asher Protter, Sarvajit Chakravarty
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Publication number: 20140296209Abstract: 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: ApplicationFiled: February 17, 2012Publication date: October 2, 2014Applicant: MEDIVATION TECHNOLOGIES, INC.Inventors: Andrew Asher Protter, Sarvajit Chakravarty
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Publication number: 20140234428Abstract: 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: ApplicationFiled: February 15, 2013Publication date: August 21, 2014Applicant: Cymbiotics, Inc.Inventors: Raj R. Barathur, Jack Bain Bookout
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Publication number: 20140228353Abstract: 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: ApplicationFiled: February 17, 2012Publication date: August 14, 2014Applicant: Medivation Technologies, Inc.Inventors: Andrew Asher Protter, Sarvvajit Chakravarty
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Patent number: 8785471Abstract: 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: GrantFiled: September 9, 2009Date of Patent: July 22, 2014Assignee: Qingdao Qiyuan Bio-Technologies Co., Ltd.Inventors: Xiaojie Sun, Weifu Ma
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Publication number: 20140187547Abstract: 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: ApplicationFiled: March 6, 2014Publication date: July 3, 2014Applicant: Purdue Research FoundationInventors: Mark S. CUSHMAN, Evgeny A. KISELEV, Andrew E. MORRELL
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Publication number: 20140162985Abstract: 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: ApplicationFiled: September 6, 2013Publication date: June 12, 2014Applicant: 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
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Publication number: 20140163012Abstract: 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: ApplicationFiled: October 31, 2013Publication date: June 12, 2014Applicant: Albany Molecular Research, Inc.Inventors: Matthew D. SURMAN, Emily E. FREEMAN, Peter R. GUZZO, Alan J. HENDERSON, Mark HADDEN
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Publication number: 20140155384Abstract: 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: ApplicationFiled: February 17, 2012Publication date: June 5, 2014Applicant: Medivation Technologies, Inc.Inventors: Andrew Asher Protter, Sarvajit Chakravarty
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Patent number: 8703181Abstract: 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: GrantFiled: October 17, 2012Date of Patent: April 22, 2014Assignee: Merrimack Pharmaceuticals, Inc.Inventors: Keelung Hong, Daryl C. Drummond, Dmitri Kirpotin
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Publication number: 20140073637Abstract: 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: ApplicationFiled: May 30, 2012Publication date: March 13, 2014Applicants: INSTITUT CURIE, INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Chi-Hung N'Guyen, Annie Molla, Ly-Thuy-Tram Le
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Publication number: 20140018360Abstract: 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: ApplicationFiled: July 13, 2012Publication date: January 16, 2014Inventors: Mark S. CUSHMAN, Evgeny A. KISELEV, Andrew E. MORRELL
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Patent number: 8629158Abstract: 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: GrantFiled: July 1, 2010Date of Patent: January 14, 2014Assignee: Albany Molecular Research, Inc.Inventors: Peter R. Guzzo, Matthew David Surman, Alan John Henderson, Mark Hadden, Emily Elizabeth Freeman
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Publication number: 20130345164Abstract: 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: ApplicationFiled: April 21, 2011Publication date: December 26, 2013Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventors: Alexei Vazquez, Darren Carpizo, Arnold Levine
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Patent number: 8604048Abstract: 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: GrantFiled: February 19, 2010Date of Patent: December 10, 2013Assignees: 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
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Patent number: 8592424Abstract: 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: GrantFiled: June 29, 2009Date of Patent: November 26, 2013Assignee: Afgin Pharma LLCInventor: Ronald Aung-Din
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Patent number: 8580811Abstract: 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: GrantFiled: March 6, 2012Date of Patent: November 12, 2013Assignee: Ligand Pharmaceuticals IncorporatedInventors: Bijan Pedram, Cornelis Arjan Van Oeveren, Lin Zhi, Shuo Zhao, Yixing Shen
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Publication number: 20130266556Abstract: 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: ApplicationFiled: November 9, 2010Publication date: October 10, 2013Applicant: XYLECO, INC.Inventor: Marshall Medoff
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Publication number: 20130251757Abstract: 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: ApplicationFiled: December 13, 2012Publication date: September 26, 2013Inventors: Gregory Troiano, Michael Figa, Abhimanyu Sabnis
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Publication number: 20130224310Abstract: 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: ApplicationFiled: June 5, 2012Publication date: August 29, 2013Applicant: Emory UniversityInventors: Harish C. Joshi, Ritu Aneja, Surya N. Vangapandu
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Publication number: 20130217673Abstract: 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: ApplicationFiled: February 22, 2012Publication date: August 22, 2013Applicant: Warsaw Orthopedic, IncInventor: Jared T. Wilsey