Plural Ring Hetero Atoms In The Tetracyclo Ring System Patents (Class 548/421)
  • Patent number: 11053255
    Abstract: Disclosed herein are methods of synthesizing mahanine and related compounds. The synthesis features an intramolecular aryl-alkyne isomerization, transition metal catalyzed cross-coupling and intramolecular carbazole forming reaction.
    Type: Grant
    Filed: June 22, 2016
    Date of Patent: July 6, 2021
    Assignee: GEORGETOWN UNIVERSITY
    Inventors: Milton L. Brown, Shujie Hou
  • Patent number: 9303036
    Abstract: Novel crystalline HCl salts of Asenapine, methods of their preparation and related pharmaceuticals and treatments are disclosed.
    Type: Grant
    Filed: May 15, 2012
    Date of Patent: April 5, 2016
    Assignee: Sandoz AG
    Inventors: Fritz Blatter, Katharina Reichenbächer
  • Publication number: 20150112083
    Abstract: The present invention provides a process for the preparation of asenapine maleate of Formula (I), comprising: intra-molecular cyclization of the intermediate of Formula (II) to obtain the intermediate of Formula (III) using aluminium halide.
    Type: Application
    Filed: July 17, 2012
    Publication date: April 23, 2015
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Ram Chander Aryan, Anamika Mishra, Pudi Giri Jagannadha Naidu, Ramnik Sharma
  • Patent number: 8987462
    Abstract: Provided are a compound of Formula 1 and an organic light-emitting device including the compound of Formula 1: The compounds of Formula 1 are particularly useful as fluorescent dopants in the emission layer of the organic light-emitting device.
    Type: Grant
    Filed: September 25, 2013
    Date of Patent: March 24, 2015
    Assignees: Samsung Display Co., Ltd., Pusan National University Industry—University Cooperation Foundation
    Inventors: Soung-Wook Kim, Myeong-Suk Kim, Jae-Hong Kim, Jin-Soo Hwang, Hong-Suk Suh
  • Publication number: 20150045560
    Abstract: Described herein are heterocyclic organic compounds of following formulae: More specifically, described herein are fused heterocyclic naphthalene compounds, polymers based on fused heterocyclic naphthalene compounds, methods for making these compounds, and uses thereof. The compounds described have improved polymerization and stability properties that allow for improved material processibility for use as organic semiconductors (OSCs).
    Type: Application
    Filed: March 28, 2013
    Publication date: February 12, 2015
    Inventors: Mingqian He, Jieyu Hu, Weijun Niu, Adama Tandia
  • Patent number: 8933114
    Abstract: Are disclosed new crystalline forms of asenapine maleate, useful in the production of pharmaceutical formulations for the treatment of diseases of the central nervous system, in particular schizophrenia; processes for the production of these new crystalline forms are also disclosed.
    Type: Grant
    Filed: December 12, 2011
    Date of Patent: January 13, 2015
    Assignee: Chemo Iberica, S.A.
    Inventors: Gianpiero Ventimiglia, Giuseppe Barreca, Domenico Magrone
  • Publication number: 20140374724
    Abstract: The present invention relates to a novel indole-based compound having superior hole injection and transport capabilities, light-emitting capabilities, and the like, and an organic electroluminescent device which comprises the indole-based compound in one or more organic layers thereof so as to thereby achieve improved characteristics, such as light-emitting efficiency, driving voltage, and lifespan characteristics.
    Type: Application
    Filed: December 7, 2012
    Publication date: December 25, 2014
    Applicant: DOOSAN CORPORATION
    Inventors: Hoe Moon Kim, Sung Moo Kim, Young Bae Kim, Tae Hyung Kim, Ho Cheol Park, Chang Jun Lee, Young Mi Baek, Jin Yong Shin
  • Patent number: 8895604
    Abstract: Solid forms of (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine hydrochloride, in particular crystalline forms and/or amorphous forms thereof, pharmaceutical compositions and medicaments containing these solid forms, the use of these solid forms, and a process for obtaining such solid forms.
    Type: Grant
    Filed: December 11, 2012
    Date of Patent: November 25, 2014
    Assignee: Gruenenthal GmbH
    Inventors: Michael Gruss, Stefan Kluge, Andreas Sieber
  • Publication number: 20140336391
    Abstract: The present invention provides a process for the preparation of the asenapine intermediate of Formula (III) using a magnesium-methanol-acetic acid mixture.
    Type: Application
    Filed: November 7, 2012
    Publication date: November 13, 2014
    Inventors: Ramnik Sharma, Senkara Rao Allu, Ram Chander Aryan
  • Publication number: 20140306197
    Abstract: Provided are a compound of Formula 1 and an organic light-emitting device including the compound of Formula 1: The compounds of Formula 1 are particularly useful as fluorescent dopants in the emission layer of the organic light-emitting device.
    Type: Application
    Filed: September 25, 2013
    Publication date: October 16, 2014
    Inventors: Soung-Wook Kim, Myeong-Suk Kim, Jae-Hong Kim, Jin-Soo Hwang, Hong-Suk Suh
  • 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: 20140239275
    Abstract: An organic light emitting compound includes the compound of Formula 1 below: Descriptions of substituents of Formula 1 are as described in the detailed description.
    Type: Application
    Filed: December 23, 2013
    Publication date: August 28, 2014
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventor: Jung-Sub Lee
  • Publication number: 20140213782
    Abstract: A pharmaceutical intermediate including a first indole moiety which is associated with an optionally carboxylated hexahydroazepino moiety, an optionally carboxylated azonane moiety, or a second, optionally carboxylated indole moiety, having an alkyl, allyl, phenylallyl, cinnamyl, alkenyl, and/or alkyl-alkenyl substituent pendant from a nitrogen atom of the same.
    Type: Application
    Filed: March 28, 2014
    Publication date: July 31, 2014
    Inventor: William Allen Boulanger
  • Publication number: 20140213783
    Abstract: A pharmaceutical intermediate including a first indole moiety which is associated with an optionally carboxylated hexahydroazepino moiety, an optionally carboxylated azonane moiety, or a second, optionally carboxylated indole moiety, having an alkyl, allyl, phenylallyl, cinnamyl, alkenyl, and/or alkyl-alkenyl substituent pendant from a nitrogen atom of the same.
    Type: Application
    Filed: March 28, 2014
    Publication date: July 31, 2014
    Inventor: William Allen Boulanger
  • Publication number: 20140213797
    Abstract: A pharmaceutical intermediate including a first indole moiety which is associated with an optionally carboxylated hexahydroazepino moiety, an optionally carboxylated azonane moiety, or a second, optionally carboxylated indole moiety, having an alkyl, allyl, phenylallyl, cinnamyl, alkenyl, and/or alkyl-alkenyl substituent pendant from a nitrogen atom of the same.
    Type: Application
    Filed: March 28, 2014
    Publication date: July 31, 2014
    Inventor: William Allen Boulanger
  • Publication number: 20140213571
    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: Application
    Filed: August 20, 2012
    Publication date: July 31, 2014
    Inventors: Nigel J. Liverton, Casey Cameron McComas, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Shuwen He, Xing Dai, Hong Liu, Zhong Lai, Clare London, Dong Xiao, Nicolas Zorn, Ravi Nargund
  • Patent number: 8779161
    Abstract: Aspects of the present application relate to a microcrystalline monoclinic form of asenapine maleate represented by structural Formula (I); processes for its preparation; and pharmaceutically acceptable dosage forms thereof.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: July 15, 2014
    Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.
    Inventors: Srinivas Katkam, Srinivas Polavarapu, Venkata Madhavi Yaddanapudi, Krishna Vinigari, Narasimha Rao Pagadala, Rajeshwar Reddy Sagyam
  • Patent number: 8766248
    Abstract: Provided are a nitrogen-containing aromatic heterocyclic compound useful as an organic semiconductor material and an organic electronic device using this compound. The nitrogen-containing aromatic heterocyclic compound has a fused indole skeleton represented by the following formula (1), the organic semiconductor material contains the compound, and the organic electronic device uses the organic semiconductor material. In general formula (1), X is N-A?, O, S, or Se; A is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group exclusive of a fused heterocycle consisting of 4 rings or more; and R is a hydrogen atom, an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group exclusive of a fused heterocycle consisting of 4 rings or more.
    Type: Grant
    Filed: July 7, 2011
    Date of Patent: July 1, 2014
    Assignee: Nippon Steel & Sumikin Chemical Co., Ltd.
    Inventors: Masanori Hotta, Yuichi Sawada, Atsushi Kawada, Masana Jikumaru, Megumi Matsumoto
  • Patent number: 8765738
    Abstract: Compounds of the general structural formula (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents are disclosed. Treatable diseases and conditions include cancers, inflammatory diseases and conditions, and immunodeficiency diseases.
    Type: Grant
    Filed: October 5, 2009
    Date of Patent: July 1, 2014
    Assignee: Incuron, LLC
    Inventors: John Tucker, Sergey Sviridov, Leonid Brodsky, Catherine Burkhart, Andrei Purmal, Katerina Gurova, Andrei Gudkov
  • Patent number: 8766249
    Abstract: Provided are a novel nitrogen-containing aromatic heterocyclic compound and an organic electronic device using the compound. This nitrogen-containing aromatic compound is represented by the general formula (1). Further, the present invention relates to organic electronic devices such as a light-emitting device, a thin-film transistor, and a photovoltaic device each using the nitrogen-containing aromatic compound. (L represents an m+n-valent aromatic hydrocarbon group or aromatic heterocyclic group, or a group arising from a triarylamine or a diaryl sulfone; X represents N-A, O, S, or Se; A represents an alkyl group or the like; R represent hydrogen, an alkyl group, an aromatic group, or the like; and m+n is an integer of 2 to 4.
    Type: Grant
    Filed: October 3, 2011
    Date of Patent: July 1, 2014
    Assignee: Nippon Steel & Sumikin Chemical Co., Ltd.
    Inventors: Yuichi Sawada, Masanori Hotta, Megumi Matsumoto
  • Publication number: 20140163083
    Abstract: Crystalline Asenapine salts of tartaric acid or succinic acid, wherein the salts are e.g. selected from the group consisting of Asenapine D, L-tartrate hydrate form A, Asenapine D, L-tartrate hydrate form B, Asenapine D, L-tartrate anhydrous form, Asenapine succinate form X, Asenapine succinate form, and Asenapine succinate form II are described as well as related pharmaceutical compositions and related treatment of psychotic diseases or disorders.
    Type: Application
    Filed: May 15, 2012
    Publication date: June 12, 2014
    Applicant: SANDOZ AG
    Inventors: Fritz Blatter, Katharina Reichenbächer
  • Publication number: 20140142158
    Abstract: A stable micronised monoclinic form of asenapine maleate is described, which comprises 5% by weight or less of orthorhombic form or any other crystalline form of asenapine maleate, wherein the asenapine maleate has a particle size distribution characterised by a d90 equal to or below 40 ?m. Processes for preparing the stable micronised monoclinic form of asenapine maleate are also described. Formula (I).
    Type: Application
    Filed: May 18, 2012
    Publication date: May 22, 2014
    Applicant: LABORATORIOS LESVI S.L.
    Inventors: Agustì Bertran, Josep Terradas
  • Publication number: 20140128444
    Abstract: Novel crystalline salts of Asenapine (I) with organic di-acids and tri-acids and to methods of their preparation are disclosed along with related pharmaceutical compositions and methods of treating psychotic diseases or disorders.
    Type: Application
    Filed: May 15, 2012
    Publication date: May 8, 2014
    Applicant: SANDOZ AG
    Inventors: Fritz Blatter, Katharina Reichenbächer
  • Publication number: 20140121259
    Abstract: Novel crystalline HCl salts of Asenapine, methods of their preparation and related pharmaceuticals and treatments are disclosed.
    Type: Application
    Filed: May 15, 2012
    Publication date: May 1, 2014
    Applicant: SANDOZ AG
    Inventors: Fritz Blatter, Katharina Reichenbächer
  • Patent number: 8703951
    Abstract: The present invention provides a series of 2,3-bis(hydroxymethyl)-4H-benzo[d]pyrrolo-[1,2-a]thiazoles and 1,2-bis(hydroxymethyl)indolizino[6,7-b]indole derivatives and their bis(alkylcarbamates) derivatives. These derivatives were designed as bi-functional DNA cross-linking agents. The in vitro cytotoxicity study of these compounds revealed that they exhibit significant anti-proliferative activity in inhibiting human lymphoblastic leukemia and various solid tumor cell growth. The compounds also exhibit therapeutic efficacy against human breast carcinoma and lung cancer in xenograft model. The compounds generally possess potent antitumor activity to kill various human solid tumors and have high potential for clinical applications.
    Type: Grant
    Filed: July 16, 2012
    Date of Patent: April 22, 2014
    Assignee: Academia Sinica
    Inventors: Tsann-Long Su, Ting-Chao Chou, Te-Chang Lee
  • Publication number: 20140051741
    Abstract: Disclosed is asenapine phosphate of formula (I) and its enantiomer (I) which can be used to prepare asenapine maleate. Further disclosed is a monoclinic crystalline form of asenapine maleate.
    Type: Application
    Filed: April 30, 2012
    Publication date: February 20, 2014
    Applicant: OLON SPA
    Inventors: Samuele Frigoli, Davide Longoni, Tamara Danelli, Marco Alpegiani
  • Patent number: 8637679
    Abstract: The present invention relates to two main components, mahanine and mahanimbine (dehydroxy-mahanine) from Murraya koenigii for the treatment of glioblastoma and cervical carcinoma. Mahanimbine exhibited anti-cancer activity against lymphoid leukemia, myeloid leukemia, glioma, cervical carcinoma, pancreatic, colon and lung cancers in nineteen cells of different genetic status. C-3 hydroxy and NH groups are responsible contributing groups for their cytotoxicity. Mahanine reduced the doses of cisplatin and paclitaxel in cervical cancer showing better efficacy and useful as an adjunct chemotherapeutic agent to reduce toxicity these two drugs. A new cheap process for this preparation was established. EtOAc extract containing alkaloids enriched with mahanimbine and mahanine, is active against glioma and cervical cancers.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: January 28, 2014
    Assignee: Council of Scientific and Industrial Research
    Inventors: Chitra Mandal, Bikas Chandra Pal, Kaushik Bhattacharya, Suman Kumar Samanta, Sayantani Sarkar, Ranjita Das
  • Publication number: 20140010784
    Abstract: The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.
    Type: Application
    Filed: May 29, 2013
    Publication date: January 9, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Luc J. Farmer, Janos Pitlik, Robert B. Perni, John H. van Drie, JR.
  • Patent number: 8580972
    Abstract: This invention provides improved processes for the preparation of 5-chloro-2-methyl-2,3,3a 12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole, asenapine. These processes allow the preparation of asenapine at industrial scale in good yields and high stereoselectivity.
    Type: Grant
    Filed: December 23, 2011
    Date of Patent: November 12, 2013
    Assignee: Medichem, S.A.
    Inventors: Jordi Bosch i Lladó, Ernesto Duran Lopez
  • Patent number: 8580840
    Abstract: The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.
    Type: Grant
    Filed: February 17, 2010
    Date of Patent: November 12, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Zhihua Sui, Xuqing Zhang, Xiaojie Li
  • Publication number: 20130274466
    Abstract: A process for preparation of a compound of formula I or a pharmaceutically acceptable salt thereof, is disclosed. The process involves subjecting a compound of formula II to Ullmann-type conditions to effect an intra-molecular ring closure reaction to form the compound of formula I. The different substituents are as described in the specification. Further, the process can provide an alternate route for the synthesis of asenapine from starting materials that can be readily available.
    Type: Application
    Filed: September 26, 2011
    Publication date: October 17, 2013
    Applicant: Alphora Research Inc.
    Inventors: Boris Gorin, Craig Edward Dixon, Yang Qu
  • Publication number: 20130267574
    Abstract: Are disclosed new crystalline forms of asenapine maleate, useful in the production of pharmaceutical formulations for the treatment of diseases of the central nervous system, in particular schizophrenia; processes for the production of these new crystalline forms are also disclosed.
    Type: Application
    Filed: December 12, 2011
    Publication date: October 10, 2013
    Inventors: Gianpiero Ventimiglia, Giuseppe Barreca, Domenico Magrone
  • Publication number: 20130225835
    Abstract: The present invention is directed to novel compounds of formula (I) as well as to the process for their preparation. Novel compounds of formula (I) can be converted into asenapine through an efficient process. The invention also relates to novel intermediates used in this process and their use in the preparation of compounds of formula (I).
    Type: Application
    Filed: July 29, 2011
    Publication date: August 29, 2013
    Applicant: LABORATORIOS LESVI, S.L.
    Inventors: Pere Dalmases Barjoan, Juan Huguet Clotet, Jordi Peirats Masia
  • Publication number: 20130211099
    Abstract: Aspects of the present application relate to a microcrystalline monoclinic form of asenapine maleate represented by structural Formula (I); processes for its preparation; and pharmaceutically acceptable dosage forms thereof.
    Type: Application
    Filed: June 16, 2011
    Publication date: August 15, 2013
    Applicants: DR. REDDY'S LABORATORIES, INC., DR. REDDY'S LABORATORIES LTD.
    Inventors: Srinivas Katkam, Srinivas Polavarapu, Venkata Madhavi Yaddanapudi, Krishna Vinigari, Narasimha Rao Pagadala, Rajeshwar Reddy Sagyam
  • Publication number: 20130184458
    Abstract: Provided are a novel nitrogen-containing aromatic heterocyclic compound and an organic electronic device using the compound. This nitrogen-containing aromatic compound is represented by the general formula (1). Further, the present invention relates to organic electronic devices such as a light-emitting device, a thin-film transistor, and a photovoltaic device each using the nitrogen-containing aromatic compound. (L represents an m+n-valent aromatic hydrocarbon group or aromatic heterocyclic group, or a group arising from a triarylamine or a diaryl sulfone; X represents N-A, O, S, or Se; A represents an alkyl group or the like; R represent hydrogen, an alkyl group, an aromatic group, or the like; and m+n is an integer of 2 to 4.
    Type: Application
    Filed: October 3, 2011
    Publication date: July 18, 2013
    Inventors: Yuichi Sawada, Masanori Hotta, Megumi Matsumoto
  • Publication number: 20130178618
    Abstract: A pharmaceutical intermediate including a first indole moiety which is associated with an optionally carboxylated hexahydroazepino moiety, an optionally carboxylated azonane moiety, or a second, optionally carboxylated indole moiety, having an alkyl, allyl, phenylallyl, cinnamyl, alkenyl, and/or alkyl-alkenyl substituent pendant from a nitrogen atom of the same.
    Type: Application
    Filed: January 10, 2012
    Publication date: July 11, 2013
    Inventor: William Allen Boulanger
  • Patent number: 8481586
    Abstract: The invention relates to pyrrolo[2,3-a]carbazole derivatives, to a method for preparing the same, and to the use thereof as PIM kinase inhibitors. The invention can particularly be used in the pharmaceutical field.
    Type: Grant
    Filed: June 25, 2009
    Date of Patent: July 9, 2013
    Assignees: Centre National de la Recherche Scientifique, Universite Blaise Pascal-Clermont-Ferrand II
    Inventors: Fabrice Anizon, Pascale Moreau, Michelle Prudhomme, Philip Cohen, Bettina Aboab, Rufine Akue-Gedu, Emilie Rossignol
  • Publication number: 20130150576
    Abstract: Provided are a nitrogen-containing aromatic heterocyclic compound useful as an organic semiconductor material and an organic electronic device using this compound. The nitrogen-containing aromatic heterocyclic compound has a fused indole skeleton represented by the following formula (1), the organic semiconductor material contains the said compound, and the organic electronic device uses the said organic semiconductor material. In general formula (1), X is N-A?, O, S, or Se; A is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group exclusive of a fused heterocycle consisting of 4 rings or more; and R is a hydrogen atom, an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group exclusive of a fused heterocycle consisting of 4 rings or more.
    Type: Application
    Filed: July 7, 2011
    Publication date: June 13, 2013
    Inventors: Masanori Hotta, Yuichi Sawada, Atsushi Kawada, Masana Jikumaru, Megumi Matsumoto
  • Publication number: 20130126792
    Abstract: The present invention relates to compounds of the formula (I), to the use of compounds of the formula (I) in electronic devices and electronic devices comprising one or more compounds of the formula (I). The invention furthermore relates to the preparation of the compounds of the formula (I) and to formulations comprising one or more compounds of the formula (I).
    Type: Application
    Filed: July 12, 2011
    Publication date: May 23, 2013
    Applicant: Merck Patent GmbH
    Inventors: Irina Martynova, Adam W. Franz, Christof Pflumm, Amir Hossain Parham, Arne Buesing, Rémi Manouk Anémian, Anja Gerhard
  • Patent number: 8426610
    Abstract: Disclosed are novel amino acid derivatives of formula (I) and (II) processes for the preparation thereof, and their use in the preparation of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino-[4,5-c]pyrrole.
    Type: Grant
    Filed: May 2, 2011
    Date of Patent: April 23, 2013
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Gerardus Johannes Kemperman, Jacobus Johannes Maria Van Der Linden, Michael R. Reeder
  • Publication number: 20130065932
    Abstract: The present invention relates to two main components, mahanine and mahanimbine (dehydroxy-mahanine) from Murraya koenigii for the treatment of glioblastoma and cervical carcinoma. Mahanimbine exhibited anti-cancer activity against lymphoid leukemia, myeloid leukemia, glioma, cervical carcinoma, pancreatic, colon and lung cancers in nineteen cells of different genetic status. C-3 hydroxy and NH groups are responsible contributing groups for their cytotoxicity. Mahanine reduced the doses of cisplatin and paclitaxel in cervical cancer showing better efficacy and useful as an adjunct chemotherapeutic agent to reduce toxicity these two drugs. A new cheap process for this preparation was established. EtOAc extract containing alkaloids enriched with mahanimbine and mahanine, is active against glioma and cervical cancers.
    Type: Application
    Filed: March 9, 2012
    Publication date: March 14, 2013
    Applicant: Council of Scientific and Industrial Research
    Inventors: Chitra Mandal, Bikas Chandra Pal, Kaushik Bhattacharya, Suman Kumar Samanta, Sayantani Sarkar, Ranjita Das
  • Patent number: 8288564
    Abstract: The invention provides a process for production of trans-dibenzoxenopyrrole compounds, in which reduction, leaving group conversion, hydrogenation and methylation are carried out in that order. The process of the invention allows trans-dibenzoxenopyrrole compounds to be produced by a simpler procedure than conventional processes. The invention further provides novel compounds obtained as intermediates in the process, and a process for their production.
    Type: Grant
    Filed: July 7, 2008
    Date of Patent: October 16, 2012
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Weiqi Wang, Tetsuya Ikemoto
  • Publication number: 20120252859
    Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).
    Type: Application
    Filed: June 18, 2012
    Publication date: October 4, 2012
    Applicant: ATHERSYS, INC.
    Inventors: Youssef L. Bennani, Bayard Huck, Michael J. Robarge
  • Publication number: 20120237561
    Abstract: The present invention provides a formulation comprising asenapine hemipamoate suspended particles, which formulation can be administered via a Depot provided by an IM injection of the formulation, and which depot does not display a particle-size dependent release rate. The present invention provides also methods of treatment using the same.
    Type: Application
    Filed: June 24, 2010
    Publication date: September 20, 2012
    Inventors: Werenfridus Adrianus Faassen, Gerardus Johannes Huissen Kemperman, Johannes Antonius Hendrikus van Laarhoven
  • Publication number: 20120196889
    Abstract: The present invention relates to novel catecholamine derivatives of Formula I, to processes for their preparation, pharmaceutical compositions containing them and to their use in therapy.
    Type: Application
    Filed: February 24, 2010
    Publication date: August 2, 2012
    Applicant: H. Lundbeck A/S
    Inventors: Benny Bang-Andersen, Mogens Larsen, Klaus Gundertofte, Morten Jorgensen, Jennifer Larsen, Niels Mork, HåKan Wikström
  • Patent number: 8232311
    Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).
    Type: Grant
    Filed: March 25, 2011
    Date of Patent: July 31, 2012
    Assignee: Athersys, Inc.
    Inventors: Youssef L. Bennani, Bayard Huck, Michael J. Robarge
  • Publication number: 20120165545
    Abstract: This invention provides improved processes for the preparation of 5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole, asenapine. These processes allow the preparation of asenapine at industrial scale in good yields and high stereoselectivity.
    Type: Application
    Filed: December 23, 2011
    Publication date: June 28, 2012
    Applicant: Medichem, S.A.
    Inventors: Jordi BOSCH i LLADÓ, Ernesto DURAN LOPEZ
  • Patent number: 8198447
    Abstract: A fused tricyclic compound having aldose reductase inhibitory activity and shown by the following formula, wherein R1 represents 1 to 3 atoms or substituents selected from a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl, cycloalkyl, alkylene, or alkoxy group, and a protected or unprotected hydroxyl or carboxyl group, R2 represents a protected or unprotected carboxyl group, R3 represents 1 or 2 atoms or substituents selected from a hydrogen atom, a halogen atom, an oxo group, a substituted or unsubstituted alkyl or alkoxy group, and a protected or unprotected carboxyl group, A represents an alkylene group, and B represents an oxygen atom, a sulfur atom, or a group shown by the following formula, wherein R4 represents an alkyl or aryl group substituted by an aryl, cycloalkyl, or heterocyclic group, and X represents an oxygen atom or a sulfur atom, provided that, when B represents a group shown by the following formula: wherein R4 represents an alkyl or aryl group substituted
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: June 12, 2012
    Assignee: National University Corporation University of Toyama
    Inventors: Naoki Toyooka, Atsushi Kato, Isao Adachi
  • Patent number: 8153671
    Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly diseases or disorders that involve thrombocytopenia.
    Type: Grant
    Filed: July 14, 2006
    Date of Patent: April 10, 2012
    Assignee: IRM LLC
    Inventors: Phillip B. Alper, Thomas Marsilje, Arnab Chatterjee, Wenshuo Lu, Daniel Mutnick, Michael Roberts, Yun He